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Staurosporine (STS) Proteinkinase-Inhibitor

Name: Staurosporine (STS)
Brand: Selleck Chemicals
SKU: S1421
Rating: 5 (189 reviews)

Kat.-Nr.S1421

Staurosporine (STS) ist ein potenter PKC-Inhibitor f R PKC R, PKC und PKC mit einer IC50 von 2 nM, 5 nM und 4 nM, weniger potent f R PKC (20 nM), PKC (73 nM) und wenig aktiv f R PKC (1086 nM) in zellfreien Assays. Diese Verbindung zeigt auch hemmende Aktivit ten auf andere Kinasen, wie PKA, PKG, S6K, CaMKII usw. Phase 3.

Staurosporine (STS) Antineoplastic and Immunosuppressive Antibiotics Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 466.53

Springe zu

Qualitätskontrolle

Charge: Reinheit: 99.61%

99.61

Produkte, die oft zusammen verwendet werden mit Staurosporine (STS)

Z-VAD-FMK

Z-VAD-FMK inhibits cell death induced by this compound in SJG2/MT330 cells.

Verwandte Ziele	TGF-beta/Smad PKC ROCK Bcr-Abl
Weitere Antineoplastic and Immunosuppressive Antibiotics Inhibitoren	Cyclosporin A Oligomycin A (MCH 32) Puromycin Dihydrochloride Nigericin sodium salt Geldanamycin (NSC 122750) Honokiol Streptozotocin (STZ) Sodium Monensin (NSC 343257) Cephalomannine Pirarubicin

Zellkultur, Behandlung & Arbeitskonzentration

Zelllinien	Assay-Typ	Konzentration	Inkubationszeit	Aktivitätsbeschreibung	PMID
human colon carcinoma cell line HCT116	Function assay			Concentration required for growth inhibition of human colon carcinoma cell line HCT116, IC50=6 nM.	15537345
human PBMC	Function assay		24 h	Suppression of IL2 production in human PBMC after 24 hrs by ELISA, IC50=16 nM.	18585046
endothelial cells	Function assay			Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50 = 7.5 μM.	8709095
Sf9 insect cells	Function assay			Inhibition of protein kinase C(1:1mixture of PKC alpha & beta) expressed in Sf9 insect cells, IC50 = 0.02 μM.	9873605
LoVo cells	Antiproliferative activity assay			Antiproliferative activity against human colon cancer cell line (LoVo cells) using MTT assay, IC50 = 0.001 μM.	11591505
umbilical vein endothelial cells	Antiproliferative activity assay			Antiproliferative activity against human umbilical vein endothelial cells (HUVECs) using MTT assay, IC50 = 0.004 μM.	11591505
ST-486 cells	Antiproliferative activity assay			Antiproliferative activity against burkit lymphoma cell line (ST-486 cells) using MTT assay, IC50 = 0.007 μM.	11591505
DLD-1 cells	Antiproliferative activity assay			Antiproliferative activity against human colon cancer cell line (DLD-1 cells) using MTT assay, IC50 = 0.009 μM.	11591505
HEK293 cells	Function assay			Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA, IC50 = 0.077 μM.	12941331
P19 cells	Function assay			Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM.	15771419
P19 cells	Function assay			Inhibition of Platelet-derived growth factor receptor in P19 cells, IC50 = 0.002 μM.	15771419
P19 cells	Function assay			Inhibition of Protein Kinase A in P19 cells, IC50 = 0.004 μM.	15771419
P19 cells	Function assay			Inhibition of Calcium/calmodulin-dependent protein kinase type II in P19 cells, IC50 = 0.006 μM.	15771419
P19 cells	Function assay			Inhibition of Cyclin-dependent kinase 1 in P19 cells, IC50 = 0.008 μM.	15771419
P19 cells	Function assay			Inhibition of Vascular endothelial growth factor receptor in P19 cells, IC50 = 0.014 μM.	15771419
HEK293 cells	Function assay			Inhibition of IL-8 release by HEK293 cells expressing PKC-beta2, IC50 = 0.077 μM.	15771419
P19 cells	Function assay			Inhibition of Insulin receptor kinase in P19 cells, IC50 = 0.2 μM.	15771419
P19 cells	Function assay			Inhibition of Casein kinase 1 in P19 cells, IC50 = 1.4 μM.	15771419
FL5.12-Akt1 cells	Antiproliferative activity assay			Antiproliferative activity against FL5.12-Akt1 cells by MTT assay, IC50 = 0.29 μM.	16403626
MiaPaCa-2 cells	Antiproliferative activity assay			Antiproliferative activity against MiaPaCa-2 cells by MTT assay, IC50 = 0.37 μM.	16403626
FL5.12-Akt1 cells	Function assay			Activity against GSK3 in FL5.12-Akt1 cells, EC50 = 0.46 μM.	16403626
MiaPaCa-2 cells	Antiproliferative activity assay			Antiproliferative activity against human MiaPaCa-2 cells, IC50 = 0.37 μM.	16413780
FL5.12-Akt1 cells	Function assay			Activity against GSK3 phosphorylation in FL5.12-Akt1 cells, EC50 = 0.46 μM.	16413780
Sf21 cells	Function assay			Inhibition of JAK3 expressed in Sf21 cells, IC50 = 0.006 μM.	17088059
U937 cells	Cytotoxicity assay			Cytotoxicity against human U937 cells, IC50 = 2 μM.	17088067
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 1 umol/L ATP, IC50 = 0.005 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 1 umol/L ATP, IC50 = 0.015 μM.	17315853
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 10 umol/L ATP, IC50 = 0.036 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 10 umol/L ATP, IC50 = 0.083 μM.	17315853
Sf9 cells	Function assay		1 min	Inhibition of human Fyn expressed in Sf9 cells after 1 min by ELISA in presence of 100 umol/L ATP, IC50 = 0.27 μM.	17315853
Sf9 cells	Function assay		20 mins	Inhibition of human Fyn expressed in Sf9 cells after 20 mins by ELISA in presence of 100 umol/L ATP, IC50 = 0.51 μM.	17315853
A549 cells	Cytotoxicity assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0024 μM.	18484775
MDA-MB-231 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0071 μM.	18484775
HT29 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HT29 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0109 μM.	18484775
MCF7 cells	Function assay			Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, Ki = 0.005 μM.	18656369
MCF7 cells	Function assay			Inhibition of PKA in human MCF7 cells by array-based fluorescence assay, IC50 = 2 μM.	18656369
Sf9 cells	Function assay			Inhibition of human Syk expressed in Sf9 cells, IC50 = 0.003 μM.	18823784
Sf9 cells	Function assay			Inhibition of human ZAP70 expressed in Sf9 cells, IC50 = 0.053 μM.	18823784
insect cells	Function assay			Inhibition of human recombinant Pim1 expressed in insect cells by HTRF, IC50 = 0.01 μM.	19179076
HT-29 cells	Apoptosis assay		2 h	Induction of apoptosis in human HT-29 cells assessed as change in mitochondrial transmembrane potential after 2 hrs by JC1 staining based fluorescence assay, ED50 = 0.0026 μM.	19422206
insect Sf21 cells	Function assay			Inhibition of JAK3 expressed in insect Sf21 cells assessed as inhibition of biotinylated substrate phosphorylation, IC50 = 0.006 μM.	19427203
Jurkat cells	Antiproliferative activity assay			Antiproliferative activity against JAK3 expressing IL2-stimulated human Jurkat cells, IC50 = 0.071 μM.	19427203
Jurkat cells	Antiproliferative activity assay			Antiproliferative activity against JAK3 expressing human resting Jurkat cells, IC50 = 0.311 μM.	19427203
HUE cells	Function assay		90 mins	Inhibition of VEGFR2 in HUE cells assessed as inhibition of VEGF-induced autophosphorylation treated for 90 mins before VEGF challenge by ELISA, IC50 = 0.07 μM.	20170163
Sf9 cells	Function assay		60 mins	Inhibition of human recombinant GST-fused NIK expressed in Sf9 cells after 60 mins by radiometric protein kinase assay, IC50 = 2.3 μM.	20580552
Sf21 cells	Function assay	30 uM		Inhibition of human CHK2 kinase expressed in insect Sf21 cells using phospho-CREBtide as substrate at 30 uM, IC50 = 0.027 μM.	21334796
Sf21 cells	Function assay	30 uM		Inhibition of human recombinant IKK-alpha expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.039 μM.	21334796
Sf21 cells	Function assay	30 uM		Inhibition of human recombinant IKK-beta expressed in insect Sf21 cells using phospho-Ulight-IkappaB-alpha as substrate at 30 uM, IC50 = 0.49 μM.	21334796
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM.	21388191
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM.	21388191
HT-29 cells	Function assay		2 h	Effect on mitochondrial membrane potential in human HT-29 cells after 2 hrs using JC-1 staining by fluorescence assay, IC50 = 0.002 μM.	21428375
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.000004 μM.	21488655
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 0.05 μM.	21488655
HT-29 cells	Function assay			Inhibition of mitochondrial membrane potential in human HT-29 cells using JC1 dye staining by fluorescence plate reader assay, IC50 = 0.0025 μM.	21513293
SF268 cells	Cytotoxicity assay		48 h	Cytotoxicity against human SF268 cells after 48 hrs by SRB assay, GI50 = 0.044 μM.	21513294
CHOK1 cells	Cytotoxicity assay		48 h	Cytotoxicity against human CHOK1 cells after 48 hrs by SRB assay, GI50 = 0.13 μM.	21513294
H460 cells	Cytotoxicity assay		48 h	Cytotoxicity against human H460 cells after 48 hrs by SRB assay, GI50 = 3.6 μM.	21513294
HT-29 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HT-29 cells after 48 hrs by SRB assay, GI50 = 3.6 μM.	21513294
MCF7 cells	Cytotoxicity assay		48 h	Cytotoxicity against human MCF7 cells after 48 hrs by SRB assay, GI50 = 11 μM.	21513294
SW1116 cells	Function assay		24 h	Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.32 μM.	21962523
HT-29 cells	Apoptosis assay		2 h	Induction of apoptosis in human HT-29 cells assessed reduction of mitochondrial membrane potential after 2 hrs by using JC1 staining by fluorescence cell-based assay, ED50 = 0.0026 μM.	21973101
LoVo cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human LoVo cells after 48 to 72 hrs by MTT assay, IC50 = 0.001 μM.	22182929
ST486 cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human ST486 cells after 48 to 72 hrs by MTT assay, IC50 = 0.007 μM.	22182929
DLD1 cells	Antiproliferative activity assay		48 to 72 h	Antiproliferative activity against human DLD1 cells after 48 to 72 hrs by MTT assay, IC50 = 0.009 μM.	22182929
B16F10 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 2.82 μM.	22503364
MCF7 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 3.07 μM.	22503364
A431 cells	Cytotoxicity assay		24 h	Cytotoxicity against human A431 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.07 μM.	22541051
MCF7 cells	Cytotoxicity assay		24 h	Cytotoxicity against human MCF7 cells after 24 hrs using Annexin VeFITC/propidium iodide staining by MTT assay, IC50 = 0.18 μM.	22541051
BJ cells	Cytotoxicity assay		72 h	Cytotoxicity against human BJ cells after 72 hrs by Calcein AM assay, IC50 = 0.002 μM.	22921081
CEM cells	Cytotoxicity assay		72 h	Cytotoxicity against human CEM cells after 72 hrs by Calcein AM assay, IC50 = 0.023 μM.	22921081
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by Calcein AM assay, IC50 = 0.064 μM.	22921081
HeLa cells	Cytotoxicity assay		72 h	Cytotoxicity against human HeLa cells after 72 hrs by Calcein AM assay, IC50 = 0.175 μM.	22921081
HepG2 cells	Function assay		24 h	Inhibition of telomerase in human HepG2 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.14 μM.	23018096
SW1116 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human SW1116 cells after 48 hrs by MTT method, IC50 = 4.95 μM.	23018096
HepG2 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human HepG2 cells after 48 hrs by MTT method, IC50 = 6.73 μM.	23018096
BGC823 cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human BGC823 cells after 48 hrs by MTT method, IC50 = 6.83 μM.	23018096
HeLa cells	Antiproliferative activity assay		48 h	Antiproliferative activity against human HeLa cells after 48 hrs by MTT method, IC50 = 9.12 μM.	23018096
HCT116 cells	Function assay			Inhibition of TNIK-mediated TCF4/beta-casein transcription in human HCT116 cells by beta-lactamase reporter gene assay, IC50 = 0.039 μM.	23232060
HepG2 cells	Function assay		48 h	Inhibition of telomerase in human HepG2 cells after 48 hrs by TRAP-PCR-ELISA, IC50 = 8.3 μM.	23279864
SW1116 cells	Function assay		24 h	Inhibition of telomerase in human SW1116 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 4.18 μM.	24286761
KE-97 cells	Cytotoxicity assay		72 h	Cytotoxicity against human KE-97 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.13 μM.	24328283
Jurkat cells	Cytotoxicity assay		72 h	Cytotoxicity against human Jurkat cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.14 μM.	24328283
HuH7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human HuH7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.23 μM.	24328283
BGC823 cells	Cytotoxicity assay		72 h	Cytotoxicity against human BGC823 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.38 μM.	24328283
MCF7 cells	Cytotoxicity assay		72 h	Cytotoxicity against human MCF7 cells after 72 hrs by CellTitre-Glo luminescent cell viability assay, IC50 = 0.52 μM.	24328283
NIH/3T3 cells	Cytotoxicity assay		96 h	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
A2780 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
HT-29 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
8505C cells	Cytotoxicity assay		96 h	Cytotoxicity against human 8505C cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
518A2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, IC50 = 0.2 μM.	24361521
MCF7 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, IC50 = 0.4 μM.	24361521
A549 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by SRB assay, IC50 = 0.6 μM.	24361521
V79 MZ cells	Function assay			Inhibition of human aldosterone synthase expressed in V79 MZ cells assessed as inhibition of aldosterone synthesis, IC50 = 0.011 μM.	24422519
HEK293 cells	Cytotoxicity assay		72 h	Cytotoxicity against HEK293 cells after 72 hrs by CellTiterGlo assay, IC50 = 0.056 μM.	24763262
HeLa cells	Antiproliferative activity assay		24 to 48 h	Antiproliferative activity against human HeLa cells after 24 to 48 hrs by CCK-8 assay, IC50 = 2.72 μM.	24792811
A549 cells	Antiproliferative activity assay		24 to 48 h	Antiproliferative activity against human A549 cells after 24 to 48 hrs by CCK-8 assay, IC50 = 3.05 μM.	24792811
HepG2 cells	Cytotoxicity assay			Cytotoxicity against human HepG2 cells, EC50 = 2 μM.	25316317
Raji cells	Cytotoxicity assay			Cytotoxicity against human Raji cells, EC50 = 2 μM.	25316317
BJ cells	Cytotoxicity assay			Cytotoxicity against human BJ cells, EC50 = 2 μM.	25316317
HEK293 cells	Cytotoxicity assay			Cytotoxicity against HEK293 cells, EC50 = 2 μM.	25316317
A549 cells	Cytotoxicity assay		48 h	Cytotoxicity against human A549 cells after 48 hrs by MTT assay, IC50 = 0.02 μM.	25825934
HeLa cells	Cytotoxicity assay		48 h	Cytotoxicity against human HeLa cells after 48 hrs by MTT assay, IC50 = 0.025 μM.	25825934
PC3 cells	Cytotoxicity assay		48 h	Cytotoxicity against human PC3 cells after 48 hrs by MTT assay, IC50 = 0.031 μM.	25825934
MGC-803 cells	Function assay		24 h	Inhibition of telomerase in human MGC-803 cells after 24 hrs by TRAP-PCR-ELISA assay, IC50 = 8.97 μM.	26900656
Sf9 insect cells	Function assay		10 mins	Inhibition of N-terminal GST tagged recombinant full-length human CHK1 expressed in baculovirus Sf9 insect cells after 10 mins by luminescent ADP-Glo assay, IC50 = 0.0012 μM.	27089211
Sf21 cells	Function assay		60 mins	Inhibition of human recombinant JAK2 expressed in Sf21 cells assessed as reduction in Ulight-CAGAGAIETDKEYYTVKD phosphorylation pre-incubated before substrate addition and measured after 60 mins by LANCE detection method, IC50 = 0.002 μM.	27137359
Neuro2a cells	Cytotoxicity assay		72 h	Cytotoxicity against mouse Neuro2a cells assessed as cell viability after 72 hrs by MTT assay, IC50 = 0.0113 μM.	28152427
MDA-MB-231 cells	Function assay		16 h	Inhibition of retinoblastoma protein phosphorylation in human MDA-MB-231 cells after 16 hrs by Hoechst 33342 staining based fluorescence assay, IC50 = 0.066 μM.	28431342
Sf9 insect cells	Function assay		20 mins	Inhibition of recombinant human N-terminally GST-tagged EGFR L858R/T790M/C797S triple mutant expressed in baculovirus in Sf9 insect cells preincubated for 20 mins followed by addition of [33P]-ATP measured after 2 hrs by filter-binding method, IC50 = 0.00029 μM.	28482151
HEK293 cells	Cytotoxicity assay		72 h	Cytotoxicity against HEK293 cells assessed as decrease in cell viability after 72 hrs by CellTiter Glo luminescent assay, CC50 = 0.00354 μM.	28624701
BT549 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human BT549 cells incubated for 24 hrs by MTT assay, IC50 = 0.08 μM.	28705432
MDA-MB-468 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay, IC50 = 0.15 μM.	28705432
MDA-MB-231 cells	Cytotoxicity assay		24 h	Cytotoxic activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay, IC50 = 0.24 μM.	28705432
Vero cells	Cytotoxicity assay		2 days	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability after 2 days by cell-titer-glo luminescent assay, TC50 = 0.0024 μM.	28763645
L929 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against mouse L929 cells after 5 days by WST-1 assay, IC50 = 0.2 μM.	28956915
KB-3-1 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against human KB-3-1 cells after 5 days by WST-1 assay, IC50 = 0.2 μM.	28956915
MCF7 cells	Antiproliferative activity assay		5 days	Antiproliferative activity against human MCF7 cells after 5 days by WST-1 assay, IC50 = 1.8 μM.	28956915
FS4-LTM cells	Antiproliferative activity assay		24 h	Antiproliferative activity against human FS4-LTM cells after 24 hrs by WST-1 assay, IC50 = 2.8 μM.	28956915
Vero cells	Cytotoxicity assay		2 days	Cytotoxicity against African green monkey Vero cells after 2 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.0024 μM.	28993106
HepG2 cells	Cytotoxicity assay	100 uM	3 days	Cytotoxicity against human HepG2 cells at 100 uM after 3 days by CellTiter-Glo luminescent cell viability assay, IC50 = 0.018 μM.	28993106
NIH/3T3 cells	Cytotoxicity assay		96 h	Cytotoxicity against mouse NIH/3T3 cells after 96 hrs by SRB assay, EC50 = 0.008 μM.	29197730
518A2 cells	Cytotoxicity assay		96 h	Cytotoxicity against human 518A2 cells after 96 hrs by SRB assay, EC50 = 0.03 μM.	29197730
A549 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A549 cells after 96 hrs by SRB assay, EC50 = 0.04 μM.	29197730
MCF7 cells	Cytotoxicity assay		96 h	Cytotoxicity against human MCF7 cells after 96 hrs by SRB assay, EC50 = 0.1 μM.	29197730
A2780 cells	Cytotoxicity assay		96 h	Cytotoxicity against human A2780 cells after 96 hrs by SRB assay, EC50 = 0.12 μM.	29197730
HT-29 cells	Cytotoxicity assay		96 h	Cytotoxicity against human HT-29 cells after 96 hrs by SRB assay, EC50 = 0.15 μM.	29197730
PC3 cells	Cytotoxicity assay			Cytotoxicity against human PC3 cells by sulforhodamine B assay, IC50 = 0.017 μM.	29389122
HCT116 cells	Cytotoxicity assay			Cytotoxicity against human HCT116 cells by sulforhodamine B assay, IC50 = 0.055 μM.	29389122
insect cells	Function assay		30 mins	Inhibition of recombinant human PDGFRbeta expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 30 mins by LANCE method, IC50 = 0.00076 μM.	29549836
Sf9 insect cells	Function assay		60 mins	Inhibition of recombinant human KDR expressed in Sf9 insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.0021 μM.	29549836
insect cells	Function assay		10 mins	Inhibition of recombinant human Src expressed in insect cells using Ulight-Poly GAT[EAY(1:1:1)]n as substrate after 10 mins by LANCE method, IC50 = 0.005 μM.	29549836
insect cells	Function assay		15 mins	Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM.	29549836
insect cells	Function assay		15 mins	Inhibition of recombinant human CDK1/Cyclin B expressed in insect cells using Ulight-CFFKNIVTPRTPPPSQGK-amide as substrate after 15 mins by LANCE method, IC50 = 0.025 μM.	29549836
Sf9 insect cells	Function assay		15 mins	Inhibition of recombinant human Flt1 expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 15 mins by LANCE method, IC50 = 0.035 μM.	29549836
Sf21 insect cells	Function assay		15 mins	Inhibition of recombinant human Aurora-A expressed in Sf21 insect cells using Ulight-RRRSLLE as substrate after 15 mins by LANCE method, IC50 = 0.039 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human AKT1 expressed in insect cells using CREBtide as substrate after 60 mins by LANCE method, IC50 = 0.056 μM.	29549836
Sf9 insect cells	Function assay		60 mins	Inhibition of recombinant human FAK expressed in Sf9 insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.062 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human ABL expressed in insect cells using Ulight-TK peptide as substrate after 60 mins by LANCE method, IC50 = 0.29 μM.	29549836
insect cells	Function assay		60 mins	Inhibition of recombinant human c-MET expressed in insect cells using Ulight-CAGAGAIETDKEYYTVKD as substrate after 60 mins by LANCE method, IC50 = 0.31 μM.	29549836
PC3 cells	Cytotoxicity assay		72 h	Cytotoxicity against human PC3 cells after 72 hrs by SRB assay, IC50 = 0.039 μM.	29558119
Sf9 cells	Function assay		45 mins	Inhibition of recombinant human C-terminal His-tagged/N-terminal GST-tagged EGFR (668 to 1210 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.047 μM.	29902719
Sf9 cells	Function assay		45 mins	Inhibition of recombinant human N-terminal GST-tagged HER2 (679 to 1255 residues) expressed in baculovirus infected Sf9 cells using Poly-(Glu, Tyr) as substrate measured after 45 minutes by Kinase-Glo luminescent assay, IC50 = 0.0608 μM.	29902719
HT-29 cells	Function assay		3 h	Inhibition of mitochondrial membrane potential in human HT-29 cells after 3 hrs by JC-1 staining based fluorescence assay, IC50 = 0.02 μM.	30057155
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK12 (1 to 1490 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.053 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM.	30067358
Sf9 cells	Function assay			Inhibition of N-terminal FLAG-tagged human full-length CDK13 (1 to 1512 residues)/N-terminal His-tagged CycK (1 to 580 residues) expressed in Sf9 cells assessed as reduction in ATP-dependent ULight-4E-BP1 (Thr37/Thr46) substrate peptide phosphorylation pr, IC50 = 0.057 μM.	30067358
HCT116 cells	Cytotoxicity assay		48 h	Cytotoxicity against human HCT116 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.03 μM.	30106291
Huh7.5 cells	Cytotoxicity assay		48 h	Cytotoxicity against human Huh7.5 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 0.6 μM.	30106291
K562 cells	Cytotoxicity assay		48 h	Cytotoxicity against human K562 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 1.7 μM.	30106291
LO2 cells	Cytotoxicity assay		48 h	Cytotoxicity against human LO2 cells assessed as decrease in cell viability after 48 hrs by MTT assay, IC50 = 9.5 μM.	30106291
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Chemische Informationen, Lagerung & Stabilität

Molekulargewicht	466.53	Formel	C₂₈H₂₆N₄O₃	Lagerung (Ab dem Eingangsdatum)	3 Jahre-20°CPulver
CAS-Nr.	62996-74-1	SDF herunterladen		Lagerung von Stammlösungen	1 Jahr-80°Cin Lösungsmittel 1 Monat-20°Cin Lösungsmittel
Synonyme	AM-2282，Antibiotic AM-2282			Smiles	CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC

Löslichkeit

In vitro
Charge:

DMSO : 46 mg/mL (98.6 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL (199.34 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:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Von Selleck Labs validiert. Sollten Sie Anpassungen an dieser Formulierung benötigen, kontaktieren Sie unser Verkaufsteam für kundenspezifische Tests.	5.000mg/ml (10.72mM)	Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to make it clear; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In-vivo-Formulierungsrechner (Klare Lösung)

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

Dosierung: mg/kg Durchschnittsgewicht der Tiere: g Dosiervolumen pro Tier:μL Anzahl der Tiere:

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

Targets/IC₅₀/Ki	PKCα (Cell-free assay) 2 nM c-Fgr (Cell-free assay) 2 nM phosphorylase kinase (Cell-free assay) 3 nM PKCη (Cell-free assay) 4 nM PKCγ (Cell-free assay) 5 nM S6 kinase (Cell-free assay) 5 nM v-Src (Cell-free assay) 6 nM Cdc2 (Cell-free assay) 9 nM Cdc2 (Cell-free assay) 9 nM PKA (Cell-free assay) 15 nM Syk (Cell-free assay) 16 nM PKG (Cell-free assay) 18 nM PKCδ (Cell-free assay) 20 nM CaMKII (Cell-free assay) 20 nM Lyn (Cell-free assay) 20 nM MLCK (Cell-free assay) 21 nM PKCε (Cell-free assay) 73 nM
In vitro	Staurosporine (STS), ein mikrobielles Alkaloid, hemmt die Proteinkinase C aus Rattenhirn signifikant mit einer IC50 von 2,7 nM. Es zeigt auch eine starke hemmende Wirkung gegenber HeLa S3-Zellen mit einer IC50 von 4 nM. Diese Verbindung hemmt eine Vielzahl anderer Proteinkinasen, einschlielich PKA, PKG, Phosphorylasekinase, S6 Kinase, Myosin-Leichtkettenkinase (MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr und Syk mit einer IC50 von 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM bzw. 16 nM. Bei 1 M induziert es >90% Apoptose in PC12-Zellen. Konsistent induziert diese Behandlung einen schnellen und anhaltenden Anstieg des intrazellul en freien Kalziumspiegels [Ca²⁺]_i, eine Akkumulation von mitochondrialen reaktiven Sauerstoffspezies (ROS) und eine nachfolgende mitochondriale Dysfunktion. Die Apoptose von MCF7-Zellen, die durch STS induziert wird, kann durch die Expression von funktionaler Caspase-3 ber Caspase-8-Aktivierung und Bid-Spaltung verst kt werden. Eine Behandlung mit 1 M hemmt die IL-3-stimulierte Bcl2-Phosphorylierung nur teilweise, blockiert aber die PKC-vermittelte Bcl2-Phosphorylierung vollst dig. Es induziert die Apoptose menschlicher Vorhautfibroblasten AG-1518, abh gig von der lysosomalen Cathepsine D-vermittelten Cytochrom c-Freisetzung und Caspase-Aktivierung. Neben der Aktivierung des klassischen mitochondrialen Apoptosewegs l st STS einen neuartigen intrinsischen Apoptoseweg aus, der auf der Aktivierung von Caspase-9 in Abwesenheit von Apaf-1 beruht.
Kinase-Assay	Enzym- und Bindungsassay
Kinase-Assay	Proteinkinase C wird in einem Reaktionsgemisch (0,25 ml) getestet, das 5 Mol Tris/HCl, pH 7,5, 2,5 Mol Magnesiumacetat, 50 g Histon II S, 20 g Phosphatidylserin, 0,88 g Diolein, 125 nMol CaCl₂, 1,25 nMol [ -³²]ATP (5-10 10⁴ cpm/nMol) und 5 g teilweise gereinigtes Enzym enth lt. Die Bindung von [³H]PDBu an Proteinkinase C wird bestimmt: Das Reaktionsgemisch (200 L) enthielt 4 Mol Tris/Malat, pH 6,8, 20 Mol KCl, 30 nMol CaCl₂, 20 g Phosphatidylserin, 5 g teilweise gereinigte Proteinkinase C, 0,5% (Endkonzentration) DMSO, 10 pMol [³H]PDBu (1-3 10⁴ cpm/pMol) und 10 L verschiedener Mengen Staurosporine (STS).
In vivo	In den Isch mie-Modellen von Gerbil und Ratte verhindert die Vorbehandlung mit Staurosporine (STS) (0,1–10 ng) vor der Isch mie neuronale Sch den dosisabh gig, was auf die Beteiligung von PKC am Tod von CA1-Pyramidenzellen nach Isch mie hindeutet.
Literatur	[1] https://pubmed.ncbi.nlm.nih.gov/3457562/ [2] https://pubmed.ncbi.nlm.nih.gov/8529658/ [3] https://pubmed.ncbi.nlm.nih.gov/9486765/ [4] https://pubmed.ncbi.nlm.nih.gov/10734071/ [5] https://pubmed.ncbi.nlm.nih.gov/10677502/ [6] https://pubmed.ncbi.nlm.nih.gov/14576777/ [7] https://pubmed.ncbi.nlm.nih.gov/21659556/ [8] https://pubmed.ncbi.nlm.nih.gov/2384538/

Anwendungen

Methoden	Biomarker	PMID
Western blot	p-Akt / Akt / PARP /Cleaved PARP FAK / RIP Ambra1	24174874
Growth inhibition assay	Cell viability	25215174
Immunofluorescence	Tubulin / Actin Phalloidin / Type II collagen Pyk2 Annexin cleaved-caspase 3 FAK 4.47	25215174

Klinische Studieninformationen

(Daten von https://clinicaltrials.gov, aktualisiert am 2024-05-22)

NCT-Nummer	Rekrutierung	Erkrankungen	Sponsor/Kooperationspartner	Startdatum	Phasen
NCT05209347	Withdrawn	Ankle Fractures\|Post-traumatic Osteoarthritis\|Osteoarthritis Ankle	University of Iowa	December 2024	Not Applicable
NCT05956990	Not yet recruiting	Colorectal Cancer Survivor\|Rehabilitation\|Quality of Life	Qu Shen\|The First Affiliated Hospital of Xiamen University\|Xiamen University	July 1 2024	Not Applicable
NCT05957289	Not yet recruiting	Rehabilitation\|Colorectal Cancer Survivor\|Quality of Life\|Pilot Study	Qu Shen\|The First Affiliated Hospital of Xiamen University\|Xiamen University	June 1 2024	Not Applicable
NCT06245135	Not yet recruiting	Mobility Limitation	University of Toronto\|University Health Network Toronto\|March of Dimes Canada\|Heart and Stroke Foundation of Canada\|University of Alberta\|University of Manitoba\|Bruyere Research Institute	June 2024	Not Applicable
NCT06374108	Not yet recruiting	Multiple Sclerosis	University of Aarhus\|Aarhus University Hospital\|University of Copenhagen	May 1 2024	Not Applicable

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