CDK9 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S8981 NVP-2

NVP-2, a potent and selective ATP-competitive cyclin dependent kinase 9 (CDK9) probe, inhibits CDK9/CycT activity with IC50 of 0.514 nM and induces cell apoptosis. NVP-2 displays inhibitory effcts on CDK1/CycB, CDK2/CycA and CDK16/CycY kinases with IC50 of 0.584 µM, 0.706 µM, and 0.605 µM, respectively.

Selective CDK9/CycT, IC50: 0.514 nM
S8783 JSH-150

JSH-150 is a highly selective and potent inhibitor of CDK9 with IC50 of 1 nM.

Selective CDK9, IC50: 1 nM
S8730 BAY 1251152

BAY1251152 is a potent PTEFb/CDK9 inhibitor with an IC50 value of 3 nM for CDK9 and an at least 50-fold selectivity against other CDKs in enzymatic assays. BAY1251152 binds to and blocks the phosphorylation and kinase activity of CDK9, thereby preventing PTEFb-mediated activation of RNA Pol II and leading to the inhibition of gene transcription of various anti-apoptotic proteins.

Selective CDK9, IC50: 3 nM
S8719 AZD4573

AZD4573 is a potent inhibitor of CDK9 (IC50 of <0.004 μM) with fast-off binding kinetics (t1/2 = 16 min) and high selectivity versus other kinases, including other CDK family kinases.

Selective CDK9, IC50: <0.004 μM
S8809 MC180295

MC180295 ((rel)-MC180295) is a novel potent and selective CDK9 inhibitor with an IC50 of 5 nM and is at least 22-fold more selective for CDK9 over other CDKs.

Selective CDK9-Cyclin T1, IC50: 5 nM
S8727 Atuveciclib (BAY-1143572)

Atuveciclib (BAY-1143572) is potent and highly selective PTEFb/CDK9 inhibitor with IC50 values of 13 nM for CDK9/CycT and the ratio of IC50 values for CDK2/CDK9 is about 100. Outside the CDK family, It inhibits GSK3 kinase with IC50 values of 45 nM and 87 nM for GSK3α and GSK3β respectively.

Selective CDK9, IC50: 13 nM
S7461 LDC000067

LDC000067 是高度选择性CDK9抑制剂,IC50为44 nM,比作用于CDK2/1/4/6/7的选择性分别高55/125/210/ >227/ >227倍。

Selective CDK9, IC50: 44 nM
S4743 Wogonin

Wogonin,在植物中发现的天然活性黄酮类化合物,是CDK9的抑制剂。在抑制CDK9的浓度下,对CDK2、CDK4和CDK6没有抑制作用。也可抑制N-acetyltransferase

Selective
S8979 THAL-SNS-032

THAL-SNS-032 is a selective CDK9 degrader PROTAC which consists of a CDK-binding SNS-032 ligand linked to a thalidomide derivative that binds the E3 ubiquitin ligase Cereblon (CRBN).

Selective
S2768 Dinaciclib (SCH727965)

Dinaciclib (SCH727965)是一种新型有效的CDK抑制剂,作用于CDK2CDK5CDK1CDK9,无细胞试验中IC50分别为1 nM,1 nM,3 nM和4 nM。它也会阻断胸甘(dThd) DNA整合。Phase 3。

Pan CDK9, IC50: 4 nM
S1145 SNS-032 (BMS-387032)

SNS-032 (BMS-387032)最初被描述为选择性CDK2抑制剂,无细胞试验中IC50为48 nM,比作用于CDK1/CDK4选择性高10和20倍。它也对CDK7/9敏感,IC50为62 nM/4 nM,对CDK6几乎没有抑制效果。 Phase 1。

Pan CDK9/CyclinT, IC50: 4 nM
S7773 CDKI-73

CDKI-73 (LS-007) is a potent CDK inhibitor in vitro with IC50 of 8.17 nM, 3.27 nM, 8.18 nM, and 5.78 nM for CDK1, CDK2, CDK4, and CDK9, respectively. CDKI-73 induces apoptosis in cancer cells. CDKI-73 is an orally bioavailable and highly efficacious CDK9 inhibitor against acute myeloid leukemia.

Pan CDK9, IC50: 5.78 nM
S1524 AT7519

AT7519是多种CDK抑制剂,作用于CDK1, 2, 4, 6和9时,IC50为10-210 nM,对CDK3作用效果稍弱,对CDK7几乎没有抑制活性。Phase 2。

Pan CDK9/CyclinT, IC50: <10 nM
S7808 AT7519 HCl

AT7519 HCl是一种多重CDK抑制剂,作用于CDK1,2,4,6 和 9,无细胞试验中IC50为10-210 nM。它对CDK3作用较弱,而对CDK7几乎没有活性。Phase 2。

Pan CDK9/CyclinT, IC50: <10 nM
S7511 LY2857785

LY2857785是一种I型可逆的、ATP竞争性的CDK9抑制剂(IC50=0.011 μM),还可抑制其他转录激酶如CDK8(IC50=0.016 μM)和CDK7 (IC50=0.246 μM)。

Pan CDK9, IC50: 0.011 μM
S2621 AZD5438

AZD5438是一种有效的CDK1/2/9抑制剂,无细胞试验中IC50为16 nM/6 nM/20 nM。对CDK5/6作用效果稍弱,对GSK3β也有抑制作用。Phase 1。

Pan CDK9, IC50: 20 nM
S8058 Riviciclib hydrochloride (P276-00)

P276-00是一种新型的CDK1CDK4CDK9抑制剂,IC50分别为79 nM, 63 nM和20 nM。Phase 2/3。

Pan CDK9/CyclinT1, IC50: 20 nM
S1230 Flavopiridol (L86-8275)

Flavopiridol (Alvocidib)与ATP竞争性抑制CDKs,包括CDK1CDK2CDK4CDK6CDK9IC50范围为20-100 nM。作用于CDK1, 2, 4, 6,9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Phase 1/2。

Pan CDK9, IC50: 20 nM
S7371 Fadraciclib (CYC065)

Fadraciclib (CYC065) is a novel, orally available ATP-competitive inhibitor of CDK2/CDK9 kinases with IC50 of 5 nM and 26 nM, respectively.

Pan CDK9, IC50: 26 nM
S8568 G1T38

G1T38 (Lerociclib) is a novel, potent, selective, and orally bioavailable CDK4/6 inhibitor with IC50 values of 0.001 μM, 0.002 μM and 0.028 μM for CDK4, CDK6 and CDK9 respectively.

Pan CDK9, IC50: 28 nM
S2742 PHA-767491

PHA-767491是一种有效的,ATP竞争性的,双重Cdc7/CDK9抑制剂,无细胞试验中IC50分别为10 nM和34 nM,比作用于CDK1/2和GSK3-β选择性高20倍左右,比作用于MK2和CDK5选择性高50倍,比作用于PLK1和CHK2选择性高100倍。

Pan CDK9, IC50: 34 nM
S1487 PHA-793887

PHA-793887是一种新型有效的CDK2CDK5CDK7抑制剂,IC50分别为8 nM, 5 nM 和10 nM,作用于CDK2, 5,和7比作用于CDK1, 4,和9选择性高6倍以上。Phase 1。

Pan CDK9/CyclinT1, IC50: 138 nM
S8722 Samuraciclib (ICEC0942)

Samuraciclib (ICEC0942, CT7001) is a new, orally bioavailable CDK7 inhibitor with an IC50 of 40nM. The IC50 values for CDK1, CDK2, CDK5 and CDK9 were 45-, 15-, 230- and 30-fold higher. ICEC0942 (CT7001) promotes cell cycle arrest and apoptosis.

Pan CDK9, IC50: 1.2 μM
S6531 Bohemine

Bohemine is a CDK inhibitor with IC50s of 4.6, 83, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively.

Pan Cdk9/cyclin T1, IC50: 2.7 μM