Staurosporine (STS)

别名: AM-2282，Antibiotic AM-2282 中文名称：星形孢菌素

目录号：S1421 Purity: 99.61%

Staurosporine (STS)是一种有效的PKC抑制剂，在无细胞试验中作用于PKCα，PKCγ 和PKCη，IC50分别为2 nM，5 nM 和 4 nM，对PKCδ(20 nM)和PKCε(73 nM)作用较弱，对PKCζ (1086 nM)的活性很低。同时对其他的激酶PKA, PKG, S6K, CaMKII, 等也显示抑制活性。Phase 3。

Staurosporine (STS) Chemical Structure

CAS: 62996-74-1

规格	价格	库存
10mM (1mL in DMSO)	1777.23	现货
2mg	794.43	现货
5mg	1466.01	现货
25mg	4398.03	现货
1g	54946.71	现货
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产品质控

批次：纯度： 99.61%

99.61

常与Staurosporine (STS)一起在实验中被使用的化合物

5-FU (5-Fluorouracil)

Staurosporine和5-FU联合使用对Lovo B2细胞的凋亡诱导作用高2倍。

Sigmond J, et al. Nucleosides Nucleotides Nucleic Acids. 2004 Oct;23(8-9):1503-6.

Oxaliplatin

Staurosporine和Oxaliplatin的使用导致DAPI⁺细胞在人非小细胞肺癌A549细胞中积累。

Sauvat A, et al. Oncotarget. 2015 Apr 20;6(11):9467-75.

Prostaglandin E2 (PGE2)

Staurosporine和Prostaglandin E2处理增强了人CD34⁺的转导，增加了人短期NSG再生细胞的转导。

Lewis G, et al. Mol Ther Methods Clin Dev. 2018 Apr 5;9:313-322.

Retinoic acid (Tretinoin)

Staurosporine和Retinoic acid联用可诱导NB4-R1/NB4-R2细胞的粒细胞分化并抑制其增殖。

Ge DZ, et al. Sci Rep. 2014 Apr 28;4:4821.

Z-VAD-FMK

Z-VAD-FMK抑制Staurosporine诱导的SJG2/MT330细胞死亡。

Wang R, et al. Biochem Biophys Res Commun. 2016 Sep 9;478(1):128-134.

Staurosporine (STS)相关产品

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相关化合物库	激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库细胞周期化合物库 TGF-beta/Smad信号通路库	点击展开

细胞实验数据示例

细胞系	实验类型	给药浓度	孵育时间	活性描述	文献信息
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
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
A549 cells	Cytotoxicity assay		72 h	Cytotoxicity against human A549 cells after 72 hrs by sulforhodamine B method, GI50 = 0.0024 μM.	18484775
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
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 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 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 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 1 umol/L ATP, IC50 = 0.005 μM.	17315853
human PBMC	Function assay		24 h	Suppression of IL2 production in human PBMC after 24 hrs by ELISA, IC50=16 nM.	18585046
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
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
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
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
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
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
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
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
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
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
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
U937 cells	Cytotoxicity assay			Cytotoxicity against human U937 cells, IC50 = 2 μM.	17088067
Sf21 cells	Function assay			Inhibition of JAK3 expressed in Sf21 cells, IC50 = 0.006 μM.	17088059
FL5.12-Akt1 cells	Function assay			Activity against GSK3 phosphorylation in FL5.12-Akt1 cells, EC50 = 0.46 μM.	16413780
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 in FL5.12-Akt1 cells, EC50 = 0.46 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	Antiproliferative activity assay			Antiproliferative activity against FL5.12-Akt1 cells by MTT assay, IC50 = 0.29 μM.	16403626
P19 cells	Function assay			Inhibition of Casein kinase 1 in P19 cells, IC50 = 1.4 μM.	15771419
P19 cells	Function assay			Inhibition of Insulin receptor kinase in P19 cells, IC50 = 0.2 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 Vascular endothelial growth factor receptor in P19 cells, IC50 = 0.014 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 Calcium/calmodulin-dependent protein kinase type II in P19 cells, IC50 = 0.006 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 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
HEK293 cells	Function assay			Inhibition of PKC-beta II mediated IL-8 release from HEK293 cells by ELISA, IC50 = 0.077 μM.	12941331
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
ST-486 cells	Antiproliferative activity assay			Antiproliferative activity against burkit lymphoma cell line (ST-486 cells) using MTT assay, IC50 = 0.007 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
LoVo cells	Antiproliferative activity assay			Antiproliferative activity against human colon cancer cell line (LoVo cells) using MTT assay, IC50 = 0.001 μM.	11591505
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
endothelial cells	Function assay			Effective dose against plasminogen activator activity stimulated by phorbol ester in endothelial cells, ED50 = 7.5 μM.	8709095
human colon carcinoma cell line HCT116	Function assay			Concentration required for growth inhibition of human colon carcinoma cell line HCT116, IC50=6 nM.	15537345
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
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
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
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
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
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
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
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
点击查看更多细胞系数据

生物活性

产品描述

靶点

PKCα ^[1] (Cell-free assay)	c-Fgr ^[2] (Cell-free assay)	phosphorylase kinase ^[2] (Cell-free assay)	PKCη ^[1] (Cell-free assay)	PKCγ ^[1] (Cell-free assay)	点击更多
2 nM	2 nM	3 nM	4 nM	5 nM	点击更多

体外研究(In Vitro)
体外研究活性	Staurosporine 也强抑制HeLa S3细胞，IC50为4 nM。^[1]Staurosporine 也抑制多种其他蛋白激酶，包括PKA, PKG, 磷酸激酶, S6 激酶, 肌球蛋白轻链激酶(MLCK), CAM PKII, cdc2, v-Src, Lyn, c-Fgr, 和Syk ， IC50分别为 15 nM, 18 nM, 3 nM, 5 nM, 21 nM, 20 nM, 9 nM, 6 nM, 20 nM, 2 nM, 和 16 nM。^[3] Staurosporine (1 μM) 诱导 PC12细胞90%以上凋亡,这种作用可被过量表达的Bcl-2抑制,或者zVAD-fmk, cycloheximide (10 μM) 及actinomycin D (5 μM)处理也可抑制。相应地, Staurosporine处理，诱导细胞内游离钙水平 [Ca²⁺]_i快速且持久的提升，线粒体活性氧（ROS）的积累,及随后的线粒体功能障碍。^[4]通过caspase-8激活和Bid 分裂，功能性caspase-3的表达可增强Staurosporine诱导MCF7细胞死亡。^[5] 1 μM Staurosporine处理，只部分抑制IL-3刺激的Bcl2 磷酸化，而完全阻断PKC调节的 Bcl2磷酸化。^[6] Staurosporine 诱导人类包皮成纤维细胞AG-1518凋亡,根据溶酶体组织蛋白酶D调节的细胞色素 c释放和 caspase 激活。^[7] 除了激活传统线粒体凋亡通路, Staurosporine触发一种新型内在凋亡通路, 依赖Apaf-1存在时对caspase-9的激活。^[8]
细胞实验	细胞系	PC12
	浓度	溶于DMSO,终浓度为1 μM
	孵育时间	~32 小时
	方法	使用Staurosporine处理细胞32小时。细胞在4%多聚甲醛中混合，然后使用DNA结合染料Hoechst 33342染色。在荧光照明下观察细胞，测定凋亡细胞百分数。
实验图片	检测方法	检测指标	实验图片	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

体内研究(In Vivo)
体内研究活性	在局部贫血前，使用Staurosporine(0.1-10 ng)预处理局部贫血沙鼠和大鼠模型，可防止神经元损伤，这种作用存在剂量依赖性，说明CAl锥体细胞死亡涉及PKC。^[2]
动物实验	Animal Models	短暂局部贫血的雄性Mongolian沙鼠或雄性 Wistar大鼠
	Dosages	~10 ng
	Administration	定向处理到海马双边CA₁子域

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
临床试验信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

参考文献
[1] Tamaoki T, et al. Biochem Biophys Res Commun, 1986, 135(2), 397-402. [2] Meggio F, et al. Eur J Biochem, 1995, 234(1), 317-322. [3] Kruman I, et al. J Neurosci Res, 1998, 51(3), 293-308. [4] Tang D, et al. J Biol Chem, 2000, 275(13), 9303-9307. [5] Deng X, et al. Proc Natl Acad Sci U S A, 2000, 97(4), 1578-1583. [6] Johansson AC, et al. Cell Death Differ, 2003, 10(11), 1253-1259. [7] Manns J, et al. FASEB J, 2011, 25(9), 3250-3261. [8] Hara H, et al. J Cereb Blood Flow Metab, 1990, 10(5), 646-653. + 展开

参考文献

+ 展开

化学信息&溶解度

分子量	466.53	分子式	C₂₈H₂₆N₄O₃
CAS号	62996-74-1	SDF	Download Staurosporine (STS) SDF
Smiles	CC12C(C(CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)NC)OC
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

DMSO : 46 mg/mL ( (98.6 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL ( (199.34 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL ( (199.34 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL ( (199.34 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 93 mg/mL ( (199.34 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩尔浓度计算器

体内溶解度
批次：

现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂

动物体内配方计算器

实验计算

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

动物体内配方计算器（澄清溶液）

第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

计算结果：

工作液浓度： mg/ml；

DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；

体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH₂O，混匀澄清。

体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。

注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。

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操作手册

如果有其他问题，请给我们留言。

* 必填项

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):