Chk1 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S2683 CHIR-124

CHIR-124是一种新型有效的Chk1抑制剂,无细胞试验中IC50为0.3 nM。比作用于Chk2选择性高2000倍,比作用于CDK2/4和Cdc2活性高500到5000倍。

Selective Chk1, IC50: 0.3 nM
S2904 PF-477736

PF-477736是一种有效的,选择性的,ATP竞争性Chk1抑制剂,无细胞试验中Ki为0.49 nM,也抑制VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret和Yes。作用于Chk1比作用于Chk2选择性高100倍左右。Phase 1。

Selective Chk1, Ki: 0.49 nM
S8526 GDC-0575 (ARRY-575)

GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM.

Selective Chk1, IC50: 1.2 nM
S8253 CCT245737

CCT245737是一种具有口服活性的CHK1抑制剂,IC50为1.4 nM。对CHK1的选择性比对CHK2和CDK1强1000倍以上。

Selective Chk1, IC50: 1.4 nM
S2735 MK-8776 (SCH 900776)

MK-8776 (SCH 900776)是一种选择性Chk1抑制剂,无细胞试验中IC50为3 nM,比作用于Chk2选择性高500倍。Phase 2。

Selective Chk1, IC50: 3 nM
S2626 Rabusertib (LY2603618)

Rabusertib (LY2603618) 是一种具有高度选择性的Chk1抑制剂,在无细胞试验中具有潜在的抗肿瘤活性, IC50=7 nM,对Chk1的效力比对其他多种检测的蛋白激酶高100倍以上。

Selective Chk1, IC50: 7 nM
S9639 VX-803 (M4344)

VX-803 (M4344, ATR inhibitor 2) is an ATP-competitive, orally active, and selective inhibitor of ataxia telangiectasia and Rad3 related (ATR) kinase with Ki of < 150 pM. VX-803 (M4344) potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (P-Chk1) phosphorylation with IC50 of 8 nM. VX-803 (M4344) exhibits potential antineoplastic activity.

Selective Chk1, IC50: 8 nM
S7740 SAR-020106

SAR-020106是ATP竞争性的、有效的、选择性的CHK1抑制剂,IC50为13.3 nM.

Selective Chk1, IC50: 13.3 nM
S6740 DB07268

DB07268 is a potent and selective JNK1 inhibitor with an IC50 value of 9 nM and exhibits at least 70- to 90-fold greater potency against JNK1 than CHK1, CK2, and PLK.

Selective CHK1, IC50: 0.82 μM
S8148 PD0166285

PD0166285是一种有效的Wee1Chk1抑制剂,IC50分别为24 nM和72 nM。

Selective Chk1, IC50: 3.4 μM
S7178 Prexasertib HCl (LY2606368)

Prexasertib (LY2606368)是CHK1的ATP竞争性抑制剂,Ki值为0.9 nM。在cell-free实验中,LY2606368对CHK2RSK的IC50值分别为8 nM和9 nM。

Pan Chk1, Ki: 0.9 nM
S6385 Prexasertib (LY2606368)

Prexasertib (LY2606368, ACR 368) is a selective ATP competitor inhibitor of Chk1 and Chk2 with IC50s of 1 nM and 8 nM in cell-free assays, respectively. Prexasertib also inhibits RSK1 with an IC50 of 9 nM in cell-free assay.

Pan Chk1, IC50: 1 nM
S1532 AZD7762

AZD7762是一种有效的,选择性Chk1抑制剂,无细胞试验中IC50为5 nM,作用于Chk2也同样有效,对CAM, Yes, Fyn, Lyn, Hck和Lck作用效果稍弱。Phase 1。

Pan Chk1, IC50: 5 nM