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Romidepsin (FK228) HDAC Inhibitor

Kat.-Nr.S3020

Romidepsin (FK228, Depsipeptid, FR 901228, NSC 630176) ist ein potenter HDAC1- und HDAC2-Inhibitor mit einer IC50 von 36 nM bzw. 47 nM in zellfreien Assays. Diese Verbindung kontrolliert das Wachstum und induziert die Apoptose in Neuroblastom-Tumorzellen.
Romidepsin (FK228) HDAC Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 540.7

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Qualitätskontrolle

Charge: Reinheit: 99.95%
99.95

Zellkultur, Behandlung & Arbeitskonzentration

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
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Chemische Informationen, Lagerung & Stabilität

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

Löslichkeit

In vitro
Charge:

DMSO : 10 mg/mL (18.49 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewichtsrechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie die untenstehenden Informationen ein (Empfohlen: Ein zusätzliches Tier zur Berücksichtigung von Verlusten während des Experiments)

mg/kg g μL

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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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.

Wirkmechanismus

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
  • [4] https://pubmed.ncbi.nlm.nih.gov/11774279/
  • [5] https://pubmed.ncbi.nlm.nih.gov/12234611/
  • [6] https://pubmed.ncbi.nlm.nih.gov/12649137/
  • [7] https://pubmed.ncbi.nlm.nih.gov/16849582/
  • [8] https://pubmed.ncbi.nlm.nih.gov/18223231/
  • [9] https://pubmed.ncbi.nlm.nih.gov/20068080/

Anwendungen

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
S3020-WB0
19682393
Growth inhibition assay Cell viability
S3020-viability1
27444036
Immunofluorescence SS18/TLE1 Cleaved caspase-3
S3020-IF1
27120803

Klinische Studieninformationen

(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

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