nur für Forschungszwecke
Kat.-Nr.S3020
| Zelllinien | Assay-Typ | Konzentration | Inkubationszeit | Formulierung | Aktivitätsbeschreibung | PMID |
|---|---|---|---|---|---|---|
| SU-DHL4 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| U2932 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| OCI-LY7 | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| Farage | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| LY7/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| U2932/EBV | Cell Viability Assay | 2.5-15 nM | 72 h | induces cytotoxicity in a concentration-dependent manner | 25790907 | |
| HCT116 | Growth Inhibition Assay | 5-5000 nM | 24 h | DMSO | induces cell death in a concentration-dependent manner | 25492515 |
| ACH-2 | Function Assay | 1-9 nM | 24 h | induces HIV-1 Env expression | 25149467 | |
| MCF-10A | Growth Inhibition Assay | IC50=0.17±0.01 nM | 24954856 | |||
| MCF-7 | Growth Inhibition Assay | IC50=1.10±0.20 nM | 24954856 | |||
| SK-BR-3 | Growth Inhibition Assay | IC50=1.00±0.35 nM | 24954856 | |||
| MDA-MB-231 | Growth Inhibition Assay | IC50=0.68±0.14 nM | 24954856 | |||
| PC3 | Growth Inhibition Assay | IC50=1.65±0.35 nM | 24954856 | |||
| HCT116 | Growth Inhibition Assay | IC50=1.00±0.00 nM | 24954856 | |||
| HCT116-p21-/- | Growth Inhibition Assay | IC50=1.26±0.37 nM | 24954856 | |||
| S1 | Growth Inhibition Assay | IC50=7.67±0.29 nM | 24954856 | |||
| SW620 | Growth Inhibition Assay | IC50=0.93±0.29 nM | 24954856 | |||
| LOX-IMVI | Growth Inhibition Assay | IC50=0.87±0.03 nM | 24954856 | |||
| UACC-62 | Growth Inhibition Assay | IC50=0.56±0.16 nM | 24954856 | |||
| MDA-MB-435 | Growth Inhibition Assay | IC50=0.90±0.06 nM | 24954856 | |||
| SF-295 | Growth Inhibition Assay | IC50=0.88±0.15 nM | 24954856 | |||
| A549 | Growth Inhibition Assay | IC50=1.26±0.24 nM | 24954856 | |||
| H460 | Growth Inhibition Assay | IC50=2.58±0.80 nM | 24954856 | |||
| EKVX | Growth Inhibition Assay | IC50=1.33±0.34 nM | 24954856 | |||
| H146 | Growth Inhibition Assay | IC50=0.22±0.07 nM | 24954856 | |||
| H526 | Growth Inhibition Assay | IC50=0.15±0.03 nM | 24954856 | |||
| HuT-78 | Growth Inhibition Assay | IC50=1.73±0.44 nM | 24954856 | |||
| HA | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 | |
| MS-275 | Growth Inhibition Assay | 0.625-10nM | 48 h | induces a significantly stronger inhibition of cell proliferation co-treated with bortezomib | 24771510 | |
| CD4 T | Growth Inhibition Assay | 48 h | EC50=4.5±1.0 nM | 24722454 | ||
| CD4 T | Growth Inhibition Assay | 48 h | CC50=107±126 nM | 24722454 | ||
| CD4+ T | Growth Inhibition Assay | EC50=3 nM | 24495105 | |||
| A549 | Growth Inhibition Assay | 10–100 nM | 24/36/48 h | inhibits cell growth in both concentration- and time-dependent manner | 24485799 | |
| JJN3 | Growth Inhibition Assay | 24/48 h | EC50<1 nM; 48 h | 24030150 | ||
| OPM-2 | Growth Inhibition Assay | 24/48 h | EC50s=1 nM; 48 h | 24030150 | ||
| RPMI-8226 | Growth Inhibition Assay | 24/48 h | EC50s=1.8 nM; 48 h | 24030150 | ||
| U266 | Growth Inhibition Assay | 24/48 h | EC50s=10 nM; 48 h | 24030150 | ||
| CA46 | Apoptosis Assay | 6 h | induces blunt apoptosis | 23966164 | ||
| DG75 | Apoptosis Assay | 6 h | induces no apoptosis | 23966164 | ||
| Ramos | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | ||
| ST486 | Apoptosis Assay | 6 h | induces extensive apoptosis | 23966164 | ||
| HuT78 | Apoptosis Assay | 1/10/100 nM | 48 h | induces apoptosis at 1 nM | 23532732 | |
| DpVp35 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| DpVp50 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| DpP75 | Apoptosis Assay | 1/10/100 nM | 48 h | induces blunt apoptosis | 23532732 | |
| SKOV-3 | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 WT | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| Brca1 Null | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| OVCAR-8 | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| NCI/ADR-RES | Growth Inhibition Assay | 1–20nM | 72 h | DMSO | reduces cell viability alone and combined with cisplatin | 23010348 |
| HCT116 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| RKO | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| CO115 | Growth Inhibition Assay | 5 nM-50 μM | 24 h | DMSO | inhibits cell growth in a concentration-dependent manner | 22924958 |
| HFS | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| LNCaP | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| A549 | Growth Inhibition Assay | 5 nM | 24/48/72 h | inhibits cell growth time-dependently | 22106282 | |
| 697 | Growth Inhibition Assay | IC50 = 2.5 nM | 21538216 | |||
| 697-R | Growth Inhibition Assay | IC50 = 8.6 nM | 21538216 | |||
| HUT78 | Growth Inhibition Assay | IC50=1 nM | 21198545 | |||
| THJ-16T | Growth Inhibition Assay | 1 nM | 24 h | inhibits cell growth | 20810568 | |
| HCT116 | Function Assay | 20 nM | 8 h | modulates transcript levels for hundreds of genes in either direction | 20739454 | |
| B104 | Function Assay | 2 nM | 24/48/72 h | increases the surface expression of CD20 | 20686505 | |
| HL-60 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 | |
| HP100 | Cytotoxicity Assay | 1-500 nM | 24 h | induces cytotoxicity in a concentration-dependent manner | 20624163 | |
| HL-60 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 | |
| HP100 | Function Assay | 10 nM | 4/6/16 h | induces the generation of hydrogen peroxide from 4h | 20624163 | |
| HL-60 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 | |
| HP100 | Function Assay | 10-500 nM | 4 h | decreases the histone deacetylase (HDAC) activity | 20624163 | |
| 11z | Kinase Assay | 3-100 nM | reduces HDAC enzymatic activity (IC50 = 6.5 ± 0.6 nmol/L) | 20605144 | ||
| SKOV-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 | |
| OVCAR-3 | Growth Inhibition Assay | 4/8/16 nM | 48 h | inhibits cell growth in a concentration-dependent manner | 20404564 | |
| HBL-2 | Growth Inhibition Assay | 2-10 nM | 24 h | IC50=4.3 nM | 20068080 | |
| Jeko-1 | Growth Inhibition Assay | 2-50 nM | 24 h | IC50=11 nM | 20068080 | |
| Granta-519 | Growth Inhibition Assay | 5-40 nM | 24 h | IC50=58.5 nM | 20068080 | |
| L1236 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.07 μM | 19233470 | |
| L428 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.43 μM | 19233470 | |
| KM-H2 | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.58 μM | 19233470 | |
| L540Cy | Cytotoxicity Assay | 1 nM-100 μM | 48 h | EC50=0.16 μM | 19233470 | |
| G401 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| STM91-01 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| SJSC | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| BT16 | Function Assay | 10 nM | 24/48/72 h | DMSO | increases CDKN1C expression | 19221586 |
| NCI-H1299 | Growth Inhibition Assay | IC50=4.6±0.2 ng/ml | 19179890 | |||
| NCI-2882 | Growth Inhibition Assay | IC50=1.6±0.04 ng/ml | 19179890 | |||
| HCC95 | Growth Inhibition Assay | IC50=2.5±0.05 ng/ml | 19179890 | |||
| NCI-H23 | Growth Inhibition Assay | IC50=2.9±0.2 ng/ml | 19179890 | |||
| NCI-H157 | Growth Inhibition Assay | IC50=1.6±0.02 ng/ml | 19179890 | |||
| NCI-H460 | Growth Inhibition Assay | IC50=2.1±0.07 ng/ml | 19179890 | |||
| NCI-H1975 | Growth Inhibition Assay | IC50=1.3±0.04 ng/ml | 19179890 | |||
| NCI-H820 | Growth Inhibition Assay | IC50=2.4±0.1 ng/ml | 19179890 | |||
| NCI-H1650 | Growth Inhibition Assay | IC50=4.9±0.3 ng/ml | 19179890 | |||
| DTC1 | Growth Inhibition Assay | IC50=0.51 nM | 18566246 | |||
| KAO | Growth Inhibition Assay | IC50=0.91 nM | 18566246 | |||
| SU-CCS-1 | Growth Inhibition Assay | IC50=0.89 nM | 18566246 | |||
| SYO-1 | Growth Inhibition Assay | IC50=0.67 nM | 18566246 | |||
| FUJI | Growth Inhibition Assay | IC50=1.31 nM | 18566246 | |||
| SKNMC | Growth Inhibition Assay | IC50=1.17 nM | 18566246 | |||
| 402-91 | Growth Inhibition Assay | IC50=1.26 nM | 18566246 | |||
| 1765-92 | Growth Inhibition Assay | IC50=1.77 nM | 18566246 | |||
| JN-DSRCT-1 | Growth Inhibition Assay | IC50=1.25 nM | 18566246 | |||
| NMS-2PC | Growth Inhibition Assay | IC50=0.81 nM | 18566246 | |||
| HL60 | Growth Inhibition Assay | IC50=1.86 nM | 18566246 | |||
| A549 | Growth Inhibition Assay | IC50=3.24 nM | 18566246 | |||
| SW480 | Growth Inhibition Assay | IC50=2.69 nM | 18566246 | |||
| MCF7 | Growth Inhibition Assay | IC50=3.55 nM | 18566246 | |||
| PC-3 | Growth Inhibition Assay | IC50=2.51 nM | 18566246 | |||
| MMRU | Growth Inhibition Assay | IC50=2.57 nM | 18566246 | |||
| Hs68 | Growth Inhibition Assay | IC50=>10 nM | 18566246 | |||
| hMSC-001F | Growth Inhibition Assay | IC50=>10 nM | 18566246 | |||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 4 in mammalian cells, IC50 = 0.51 μM. | 14584932 | |||
| mammalian cells | Function assay | Inhibition of Histone deacetylase 1 induced acetylated histone in mammalian cells., EC50 = 36 μM. | 14584932 | |||
| MCF7 | Growth inhibition assay | Growth inhibition of MCF7 cells, IC50 = 0.00075 μM. | 17958342 | |||
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, TGI = 0.028 μM. | 21967146 | ||
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | ||
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, TGI = 0.031 μM. | 21967146 | ||
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, TGI = 0.062 μM. | 21967146 | ||
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, TGI = 0.09 μM. | 21967146 | ||
| COLO205 | Cytotoxicity assay | 6 days | Cytotoxicity against human COLO205 cells after 6 days by MTT assay, LC50 = 0.092 μM. | 21967146 | ||
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, TGI = 0.095 μM. | 21967146 | ||
| U251 | Cytotoxicity assay | 6 days | Cytotoxicity against human U251 cells after 6 days by MTT assay, LC50 = 0.13 μM. | 21967146 | ||
| A498 | Cytotoxicity assay | 6 days | Cytotoxicity against human A498 cells after 6 days by MTT assay, LC50 = 0.2 μM. | 21967146 | ||
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, TGI = 0.23 μM. | 21967146 | ||
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, TGI = 0.25 μM. | 21967146 | ||
| RXF393 | Cytotoxicity assay | 6 days | Cytotoxicity against human RXF393 cells after 6 days by MTT assay, LC50 = 0.3 μM. | 21967146 | ||
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, TGI = 0.33 μM. | 21967146 | ||
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, TGI = 0.34 μM. | 21967146 | ||
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, TGI = 0.35 μM. | 21967146 | ||
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, TGI = 0.73 μM. | 21967146 | ||
| SN12C | Cytotoxicity assay | 6 days | Cytotoxicity against human SN12C cells after 6 days by MTT assay, LC50 = 1.5 μM. | 21967146 | ||
| UO31 | Cytotoxicity assay | 6 days | Cytotoxicity against human UO31 cells after 6 days by MTT assay, TGI = 1.55 μM. | 21967146 | ||
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, TGI = 1.89 μM. | 21967146 | ||
| NCI60 | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI60 cells after 6 days by MTT assay, LC50 = 3.5 μM. | 21967146 | ||
| MDA-MB-231 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-231 cells after 6 days by MTT assay, LC50 = 4.08 μM. | 21967146 | ||
| MDA-MB-468 | Cytotoxicity assay | 6 days | Cytotoxicity against human MDA-MB-468 cells after 6 days by MTT assay, LC50 = 4.14 μM. | 21967146 | ||
| ACHN | Cytotoxicity assay | 6 days | Cytotoxicity against human ACHN cells after 6 days by MTT assay, LC50 = 5.37 μM. | 21967146 | ||
| UACC257 | Cytotoxicity assay | 6 days | Cytotoxicity against human UACC257 cells after 6 days by MTT assay, LC50 = 5.46 μM. | 21967146 | ||
| NCI-H322M | Cytotoxicity assay | 6 days | Cytotoxicity against human NCI-H322M cells after 6 days by MTT assay, LC50 = 9.02 μM. | 21967146 | ||
| SF295 | Cytotoxicity assay | 6 days | Cytotoxicity against human SF295 cells after 6 days by MTT assay, LC50 = 10.2 μM. | 21967146 | ||
| Caki1 | Cytotoxicity assay | 6 days | Cytotoxicity against human Caki1 cells after 6 days by MTT assay, LC50 = 20.9 μM. | 21967146 | ||
| NCI-H23 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H23 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| NCI-H522 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human NCI-H522 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| OVCAR5 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVCAR5 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| SW620 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SW620 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| MDA-MB-435 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-435 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| COLO205 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human COLO205 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| LOXIMVI | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human LOXIMVI cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| UACC62 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human UACC62 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| MDA-MB-231 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human MDA-MB-231 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| SF295 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human SF295 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| U251 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human U251 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| OVRAC3 | Antitumor assay | 1.6 to 2.4 mg/kg | up to 5 days | Antitumor activity against human OVRAC3 cells implanted intraperitoneally in mouse assessed as inhibition of tumor cell growth at 1.6 to 2.4 mg/kg, ip administered on day 1 to 4 measured on day 5 by hollow fiber assay | 21967146 | |
| LLC | Function assay | Inhibition of HDAC-mediated HIF-1alpha activity in mouse LLC cells, IC50 = 2 μM. | 22305612 | |||
| NCI-H522 | Growth inhibition assay | Growth inhibition of human NCI-H522 cells by sulforhodamine B colorimetric method, GI50 = 0.0018 μM. | 23313638 | |||
| LOXIMVI | Growth inhibition assay | Growth inhibition of human LOXIMVI cells by sulforhodamine B colorimetric method, GI50 = 0.0025 μM. | 23313638 | |||
| A549 | Growth inhibition assay | Growth inhibition of human A549 cells by sulforhodamine B colorimetric method, GI50 = 0.0026 μM. | 23313638 | |||
| OVCAR5 | Growth inhibition assay | Growth inhibition of human OVCAR5 cells by sulforhodamine B colorimetric method, GI50 = 0.0028 μM. | 23313638 | |||
| MKN74 | Growth inhibition assay | Growth inhibition of human MKN74 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | |||
| NCI-H460 | Growth inhibition assay | Growth inhibition of human NCI-H460 cells by sulforhodamine B colorimetric method, GI50 = 0.003 μM. | 23313638 | |||
| HCT116 | Growth inhibition assay | Growth inhibition of human HCT116 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | |||
| HCC2998 | Growth inhibition assay | Growth inhibition of human HCC2998 cells by sulforhodamine B colorimetric method, GI50 = 0.0031 μM. | 23313638 | |||
| MKN1 | Growth inhibition assay | Growth inhibition of human MKN1 cells by sulforhodamine B colorimetric method, GI50 = 0.0032 μM. | 23313638 | |||
| SKOV3 | Growth inhibition assay | Growth inhibition of human SKOV3 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | |||
| HT-29 | Growth inhibition assay | Growth inhibition of human HT-29 cells by sulforhodamine B colorimetric method, GI50 = 0.0033 μM. | 23313638 | |||
| KM12 | Growth inhibition assay | Growth inhibition of human KM12 cells by sulforhodamine B colorimetric method, GI50 = 0.0034 μM. | 23313638 | |||
| DMS114 | Growth inhibition assay | Growth inhibition of human DMS114 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | |||
| SF539 | Growth inhibition assay | Growth inhibition of human SF539 cells by sulforhodamine B colorimetric method, GI50 = 0.0036 μM. | 23313638 | |||
| U251 | Growth inhibition assay | Growth inhibition of human U251 cells by sulforhodamine B colorimetric method, GI50 = 0.0039 μM. | 23313638 | |||
| SF295 | Growth inhibition assay | Growth inhibition of human SF295 cells by sulforhodamine B colorimetric method, GI50 = 0.004 μM. | 23313638 | |||
| MCF7 | Growth inhibition assay | Growth inhibition of human MCF7 cells by sulforhodamine B colorimetric method, GI50 = 0.0042 μM. | 23313638 | |||
| NCI-H23 | Growth inhibition assay | Growth inhibition of human NCI-H23 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | |||
| OVCAR3 | Growth inhibition assay | Growth inhibition of human OVCAR3 cells by sulforhodamine B colorimetric method, GI50 = 0.0046 μM. | 23313638 | |||
| MKN7 | Growth inhibition assay | Growth inhibition of human MKN7 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | |||
| SF268 | Growth inhibition assay | Growth inhibition of human SF268 cells by sulforhodamine B colorimetric method, GI50 = 0.0049 μM. | 23313638 | |||
| MDA-MB-231 | Growth inhibition assay | Growth inhibition of human MDA-MB-231 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | |||
| OVCAR8 | Growth inhibition assay | Growth inhibition of human OVCAR8 cells by sulforhodamine B colorimetric method, GI50 = 0.0055 μM. | 23313638 | |||
| DMS273 | Growth inhibition assay | Growth inhibition of human DMS273 cells by sulforhodamine B colorimetric method, GI50 = 0.0058 μM. | 23313638 | |||
| DU145 | Growth inhibition assay | Growth inhibition of human DU145 cells by sulforhodamine B colorimetric method, GI50 = 0.006 μM. | 23313638 | |||
| RXF631L | Growth inhibition assay | Growth inhibition of human RXF631L cells by sulforhodamine B colorimetric method, GI50 = 0.0066 μM. | 23313638 | |||
| HBC4 | Growth inhibition assay | Growth inhibition of human HBC4 cells by sulforhodamine B colorimetric method, GI50 = 0.0069 μM. | 23313638 | |||
| SNB75 | Growth inhibition assay | Growth inhibition of human SNB75 cells by sulforhodamine B colorimetric method, GI50 = 0.0072 μM. | 23313638 | |||
| BSY1 | Growth inhibition assay | Growth inhibition of human BSY1 cells by sulforhodamine B colorimetric method, GI50 = 0.0085 μM. | 23313638 | |||
| NCI-H226 | Growth inhibition assay | Growth inhibition of human NCI-H226 cells by sulforhodamine B colorimetric method, GI50 = 0.0089 μM. | 23313638 | |||
| SNB78 | Growth inhibition assay | Growth inhibition of human SNB78 cells by sulforhodamine B colorimetric method, GI50 = 0.0096 μM. | 23313638 | |||
| HBC5 | Growth inhibition assay | Growth inhibition of human HBC5 cells by sulforhodamine B colorimetric method, GI50 = 0.013 μM. | 23313638 | |||
| MKN45 | Growth inhibition assay | Growth inhibition of human MKN45 cells by sulforhodamine B colorimetric method, GI50 = 0.014 μM. | 23313638 | |||
| MKN28 | Growth inhibition assay | Growth inhibition of human MKN28 cells by sulforhodamine B colorimetric method, GI50 = 0.017 μM. | 23313638 | |||
| PC3 | Growth inhibition assay | Growth inhibition of human PC3 cells by sulforhodamine B colorimetric method, GI50 = 0.018 μM. | 23313638 | |||
| ACHN | Growth inhibition assay | Growth inhibition of human ACHN cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | |||
| OVCAR4 | Growth inhibition assay | Growth inhibition of human OVCAR4 cells by sulforhodamine B colorimetric method, GI50 = 0.02 μM. | 23313638 | |||
| St-4 | Growth inhibition assay | Growth inhibition of human St-4 cells by sulforhodamine B colorimetric method, GI50 = 0.022 μM. | 23313638 | |||
| HCT15 | Growth inhibition assay | Growth inhibition of human HCT15 cells by sulforhodamine B colorimetric method, GI50 = 0.45 μM. | 23313638 | |||
| CD4+ T | Function assay | 7 days | Reactivation of latent HIV1 NL4-3-Luc expression in human naive CD4+ T cells treated 7 days post-infection measured after 48 hrs by luminescence plate reader analysis, EC50 = 0.003 μM. | 24495105 | ||
| NCI-H522 | Cytotoxicity assay | Cytotoxicity against human NCI-H522 cells by SRB assay, GI50 = 0.0018 μM. | 24589486 | |||
| LOXIMVI | Cytotoxicity assay | Cytotoxicity against human LOXIMVI cells by SRB assay, GI50 = 0.0025 μM. | 24589486 | |||
| A549 | Cytotoxicity assay | Cytotoxicity against human A549 cells by SRB assay, GI50 = 0.0026 μM. | 24589486 | |||
| OVCAR5 | Cytotoxicity assay | Cytotoxicity against human OVCAR5 cells by SRB assay, GI50 = 0.0028 μM. | 24589486 | |||
| NCI-H460 | Cytotoxicity assay | Cytotoxicity against human NCI-H460 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | |||
| MKN74 | Cytotoxicity assay | Cytotoxicity against human MKN74 cells by SRB assay, GI50 = 0.003 μM. | 24589486 | |||
| HCC2998 | Cytotoxicity assay | Cytotoxicity against human HCC2998 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | |||
| HCT116 | Cytotoxicity assay | Cytotoxicity against human HCT116 cells by SRB assay, GI50 = 0.0031 μM. | 24589486 | |||
| MKN1 | Cytotoxicity assay | Cytotoxicity against human MKN1 cells by SRB assay, GI50 = 0.0032 μM. | 24589486 | |||
| HT-29 | Cytotoxicity assay | Cytotoxicity against human HT-29 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | |||
| SKOV3 | Cytotoxicity assay | Cytotoxicity against human SKOV3 cells by SRB assay, GI50 = 0.0033 μM. | 24589486 | |||
| KM12 | Cytotoxicity assay | Cytotoxicity against human KM12 cells by SRB assay, GI50 = 0.0034 μM. | 24589486 | |||
| SF539 | Cytotoxicity assay | Cytotoxicity against human SF539 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | |||
| 293T | Function assay | 30 mins | Inhibition of human HDAC1 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.0036 μM. | 24589486 | ||
| DMS114 | Cytotoxicity assay | Cytotoxicity against human DMS114 cells by SRB assay, GI50 = 0.0036 μM. | 24589486 | |||
| U251 | Cytotoxicity assay | Cytotoxicity against human U251 cells by SRB assay, GI50 = 0.0039 μM. | 24589486 | |||
| SF295 | Cytotoxicity assay | Cytotoxicity against human SF295 cells by SRB assay, GI50 = 0.004 μM. | 24589486 | |||
| MCF7 | Cytotoxicity assay | Cytotoxicity against human MCF7 cells by SRB assay, GI50 = 0.0042 μM. | 24589486 | |||
| OVCAR3 | Cytotoxicity assay | Cytotoxicity against human OVCAR3 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | |||
| NCI-H23 | Cytotoxicity assay | Cytotoxicity against human NCI-H23 cells by SRB assay, GI50 = 0.0046 μM. | 24589486 | |||
| SF268 | Cytotoxicity assay | Cytotoxicity against human SF268 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | |||
| MKN7 | Cytotoxicity assay | Cytotoxicity against human MKN7 cells by SRB assay, GI50 = 0.0049 μM. | 24589486 | |||
| OVCAR8 | Cytotoxicity assay | Cytotoxicity against human OVCAR8 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | |||
| MDA-MB-231 | Cytotoxicity assay | Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50 = 0.0055 μM. | 24589486 | |||
| DMS273 | Cytotoxicity assay | Cytotoxicity against human DMS273 cells by SRB assay, GI50 = 0.0058 μM. | 24589486 | |||
| DU145 | Cytotoxicity assay | Cytotoxicity against human DU145 cells by SRB assay, GI50 = 0.006 μM. | 24589486 | |||
| RXF631L | Cytotoxicity assay | Cytotoxicity against human RXF631L cells by SRB assay, GI50 = 0.0066 μM. | 24589486 | |||
| HBC4 | Cytotoxicity assay | Cytotoxicity against human HBC4 cells by SRB assay, GI50 = 0.0069 μM. | 24589486 | |||
| SNB75 | Cytotoxicity assay | Cytotoxicity against human SNB75 cells by SRB assay, GI50 = 0.0072 μM. | 24589486 | |||
| BSY1 | Cytotoxicity assay | Cytotoxicity against human BSY1 cells by SRB assay, GI50 = 0.0085 μM. | 24589486 | |||
| NCI-H226 | Cytotoxicity assay | Cytotoxicity against human NCI-H226 cells by SRB assay, GI50 = 0.0089 μM. | 24589486 | |||
| SNB78 | Cytotoxicity assay | Cytotoxicity against human SNB78 cells by SRB assay, GI50 = 0.0096 μM. | 24589486 | |||
| HBC5 | Cytotoxicity assay | Cytotoxicity against human HBC5 cells by SRB assay, GI50 = 0.013 μM. | 24589486 | |||
| MKN45 | Cytotoxicity assay | Cytotoxicity against human MKN45 cells by SRB assay, GI50 = 0.014 μM. | 24589486 | |||
| MKN28 | Cytotoxicity assay | Cytotoxicity against human MKN28 cells by SRB assay, GI50 = 0.017 μM. | 24589486 | |||
| PC3 | Cytotoxicity assay | Cytotoxicity against human PC3 cells by SRB assay, GI50 = 0.018 μM. | 24589486 | |||
| ACHN | Cytotoxicity assay | Cytotoxicity against human ACHN cells by SRB assay, GI50 = 0.02 μM. | 24589486 | |||
| OVCAR4 | Cytotoxicity assay | Cytotoxicity against human OVCAR4 cells by SRB assay, GI50 = 0.02 μM. | 24589486 | |||
| St-4 | Cytotoxicity assay | Cytotoxicity against human St-4 cells by SRB assay, GI50 = 0.022 μM. | 24589486 | |||
| 293T | Function assay | 30 mins | Inhibition of mouse HDAC6 expressed in human 293T cells using Ac-KGLGK(Ac)-MCA as substrate after 30 mins by fluorescence assay, IC50 = 0.39 μM. | 24589486 | ||
| HCT15 | Cytotoxicity assay | Cytotoxicity against human HCT15 cells by SRB assay, GI50 = 0.45 μM. | 24589486 | |||
| mink Mv1Lu | Function assay | 24 hrs | Increase in human wild type p21 protein expression in mink Mv1Lu cells after 24 hrs by p21 promoter assay in presence of 0.1 mM dithiothreitol, EC1000 = 0.0157 μM. | 24997578 | ||
| HCT116 | Antiproliferative assay | 48 hrs | Antiproliferative activity against human HCT116 cells after 48 hrs in presence of DTT by MTT assay, IC50 = 0.003 μM. | 25147612 | ||
| MOLT4 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay, GI50 = 0.00206 μM. | 26331334 | ||
| DU145 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay, GI50 = 0.00255 μM. | 26331334 | ||
| U937 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay, GI50 = 0.00341 μM. | 26331334 | ||
| HLF | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HLF cells after 72 hrs by CCK8 assay, GI50 = 0.00489 μM. | 26331334 | ||
| WI38 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human WI38 cells after 72 hrs by CCK8 assay, GI50 = 0.00539 μM. | 26331334 | ||
| U937 | Function assay | 24 hrs | Inhibition of HDAC6 in human U937 cells assessed as reduction of alpha-tubilin acetylation at 5 nM to 5 uM after 24 hrs by Western blot analysis | 26331334 | ||
| HCT116 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.028 μM. | 26481659 | ||
| IGROV1/Pt1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1/Pt1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.08 μM. | 26481659 | ||
| IGROV1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human IGROV1 cells assessed as cell viability incubated for 72 hrs by coulter counter method, IC50 = 0.22 μM. | 26481659 | ||
| Klicken Sie hier, um weitere experimentelle Daten zu Zelllinien anzuzeigen | ||||||
| Molekulargewicht | 540.7 | Formel | C24H36N4O6S2 |
Lagerung (Ab dem Eingangsdatum) | |
|---|---|---|---|---|---|
| CAS-Nr. | 128517-07-7 | -- | Lagerung von Stammlösungen |
|
|
| Synonyme | FK228, Depsipeptide, FR 901228, NSC 630176, | Smiles | CC=C1C(=O)NC(C(=O)OC2CC(=O)NC(C(=O)NC(CSSCCC=C2)C(=O)N1)C(C)C)C(C)C | ||
|
In vitro |
DMSO
: 10 mg/mL
(18.49 mM)
Water : Insoluble Ethanol : Insoluble |
|
In vivo |
|||||
Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)
Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, keine Formulierung. Bitte kontaktieren Sie uns zuerst, wenn es im Abschnitt "Löslichkeit" keine In-vivo-Formulierung gibt.)
Berechnungsergebnisse:
Arbeitskonzentration: mg/ml;
Methode zur Herstellung der DMSO-Stammlösung: mg Wirkstoff vorgelöst in μL DMSO ( Konzentration der Stammlösung mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der Wirkstoffcharge überschreitet. )
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügenμL PEG300, mischen und klären, dann hinzufügenμL Tween 80, mischen und klären, dann hinzufügen μL ddH2O, mischen und klären.
Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammlösung, dann hinzufügen μL Maisöl, mischen und klären.
Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, das/die Lösungsmittel der Reihe nach hinzuzufügen. Sie müssen sicherstellen, dass die bei der vorherigen Zugabe erhaltene Lösung eine klare Lösung ist, bevor Sie mit der Zugabe des nächsten Lösungsmittels fortfahren. Physikalische Methoden wie Vortex, Ultraschall oder ein heißes Wasserbad können zur Unterstützung des Lösens verwendet werden.
| Merkmale |
More effective than other classical HDAC inhibitors such as TSA, TPX, and butyrate.
|
|---|---|
| Targets/IC50/Ki |
HDAC1
(Cell-free assay) 36 nM
HDAC2
(Cell-free assay) 47 nM
|
| In vitro |
Im Gegensatz zu TSA hemmt die aktive Form redFK von Romidepsin HDAC1 und HDAC2 stark mit IC50 von 1,6 nM bzw. 3,9 nM, ist aber relativ schwach in der Hemmung von HDAC4 und HDAC6 mit IC50 von 25 nM bzw. 790 nM. Diese Verbindung ist 17-23 Mal schwächer als redFK bei der Hemmung dieser HDACs mit IC50 von 36 nM, 47 nM, 510 nM und 14 μM. Die Behandlung mit dieser Chemikalie in HeLa-Zellen induziert Histonacetylierung und p21-Expression mit einer EC50 von 3,0 nM, stärker als redFK mit einer EC50 von 11 nM aufgrund der Instabilität von redFK. Zusätzlich zum G2/M-Arrest bewirkt diese Verbindung eine Herunterregulierung von Cyclin D1 und eine p53-unabhängige p21-Induktion, die zur Hemmung von CDK und zur Dephosphorylierung von Rb führt, was zu einem Wachstumsarrest in der frühen G1-Phase führt. Es ist 100-mal wirksamer als TSA und 1.000.000-mal wirksamer als Butyrat bei der Hemmung der Proliferation von A549-Zellen. Dieses Mittel hemmt das Wachstum von U-937-, K562- und CCRF-CEM-Zellen mit IC50 von 5,92 nM, 8,36 nM bzw. 6,95 nM. Es fördert die Apoptose in chronisch lymphatischer Leukämie (CLL)-Zellen in einer Konzentration, die derjenigen entspricht, bei der die H3- und H4-Acetylierung und HDAC-Hemmung auftritt, wobei selektiv die Aktivierung von Caspase 8 und Effektor-Caspase 3 sowie die Herunterregulierung des c-FLIP-Proteins involviert sind. In 11 von 13 (85%) Nierenzellkarzinom-Zelllinien und in 16 von 37 (43%) anderen Krebszelllinien reguliert diese Verbindung Tumortodesrezeptoren hoch und verstärkt die natürliche Killer (NK)-vermittelte Tumortötung. Es zeigt eine konzentrationsabhängige Zytotoxizität gegen eine Reihe von Mantelzelllymphom (MCL)-Zelllinien.
|
| Kinase-Assay |
HDAC-inhibitorische Aktivität
|
|
Für den Enzymtest werden 10 μL von [3H]acetylmarkierten Histonen (25.000 cpm/10 μg) zu 90 μL der HDAC-Enzymfraktion gegeben, die aus 293T-Zellen extrahiert wurde, die HDAC1 oder HDAC2 überexprimieren, in Gegenwart steigender Konzentrationen von Romidepsin, und die Mischung wird 15 Minuten bei 37 °C inkubiert. Die Enzymreaktion ist mindestens 1 Stunde lang linear. Die Reaktion wird durch Zugabe von 10 μL konzentrierter HCl gestoppt. Die freigesetzte [3H]Essigsäure wird mit 1 mL Ethylacetat extrahiert, und 0,9 mL der Lösungsmittelschicht werden in 5 mL wässrige Zählszintillator-II-Lösung zur Bestimmung der Radioaktivität gegeben. Die IC50-Werte werden aus mindestens drei unabhängigen Dosis-Wirkungs-Kurven bestimmt.
|
|
| In vivo |
Die Behandlung mit Romidepsin hemmt die Neovaskularisation von Hühnerembryonen und erwachsenen Mäusen im Matrigel-Plug-Assay potent. Die Verabreichung dieser Verbindung in einer Dosis von 0,1-1 mg/kg zweimal pro Woche verlängert das Überleben von Mäusen mit U-937-Lymphom signifikant, mit medianen Überlebenszeiten von 30,5 (0,56 mg/kg) bzw. 33 Tagen (0,32 mg/kg) (im Vergleich zu 20 Tagen bei Kontrollmäusen).
|
Literatur |
|
| Methoden | Biomarker | Bilder | PMID |
|---|---|---|---|
| Western blot | p21 / Cyclin D1 AcH3(K9) / Ac-α-Tubulin(K40) / Ac-NFκB2(K310) p65 / 3MeH3(K27) HDAC3 / HDAC4 / HDAC6 / HDAC2 γH2AX / PARP1 / Cleaved caspase3 / BAK / p21(waf1/cip1) / XIAP Cyclin E1 / BRCA1 / E2F1 / Cleaved PARP / H3Ac pAKT(S473) / pAKT(T308) / AKT |
|
19682393 |
| Growth inhibition assay | Cell viability |
|
27444036 |
| Immunofluorescence | SS18/TLE1 Cleaved caspase-3 |
|
27120803 |
(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)
| NCT-Nummer | Rekrutierung | Erkrankungen | Sponsor/Kooperationspartner | Startdatum | Phasen |
|---|---|---|---|---|---|
| NCT03770000 | Completed | T Cell Lymphoma |
Rhizen Pharmaceuticals SA |
March 12 2019 | Phase 1|Phase 2 |
| NCT02616965 | Active not recruiting | Cutaneous T-cell Lymphoma (CTCL) |
Fox Chase Cancer Center|Seagen Inc.|Celgene Corporation |
February 22 2017 | Phase 1 |
| NCT02616874 | Completed | HIV |
IrsiCaixa|Germans Trias i Pujol Hospital|Fundación FLS de Lucha Contra el Sida las Enfermedades Infecciosas y la Promoción de la Salud y la Ciencia|Hospital Clinic of Barcelona|Hospital de Sant Pau|HIVACAT|University of Oxford|BCN Checkpoint |
February 2016 | Phase 1 |
Tel: +1-832-582-8158 Ext:3
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