- Chk1
- Chk2
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 is a novel and potent Chk1 inhibitor with IC50 of 0.3 nM in a cell-free assay. It shows 2,000-fold selectivity against Chk2, 500- to 5,000-fold less activity against CDK2/4 and Cdc2. | Selective | Chk1, IC50: 0.3 nM |
| S2904 | PF-477736 | PF-477736 (PF-736, PF-00477736) is a selective, potent and ATP-competitive Chk1 inhibitor with Ki of 0.49 nM in a cell-free assay and also inhibits VEGFR2, Aurora-A, FGFR3, Flt3, Fms (CSF1R), Ret and Yes. It shows ~100-fold selectivity for Chk1 than Chk2. | 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 (SRA737, PNT-737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1. | Selective | Chk1, IC50: 1.4 nM |
| S2735 | MK-8776 (SCH 900776) | MK-8776 (SCH 900776) is a selective Chk1 inhibitor with IC50 of 3 nM in a cell-free assay. It shows 500-fold selectivity against Chk2. Phase 2. | Selective | Chk1, IC50: 3 nM |
| S2626 | Rabusertib (LY2603618) | Rabusertib (LY2603618, IC-83) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated. Rabusertib (LY2603618) induces cell cycle arrest, DNA damage response and autophagy in cancer cells. Rabusertib (LY2603618) induces bak-dependent apoptosis in AML cell lines. | 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 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 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 is a potent Wee1 and Chk1 inhibitor with activity at nanomolar concentrations (IC50=24 nM for Wee1 and 72 nM for Myt1). PD0166285 is also a novel G2 checkpoint abrogator. PD0166285 induces apoptosis. | Selective | Chk1, IC50: 3.4 μM |
| S7178 | Prexasertib HCl (LY2606368) | Prexasertib(LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay. | 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 is a potent and selective inhibitor of Chk1 with IC50 of 5 nM in a cell-free assay. It is equally potent against Chk2 and less potent against CAM, Yes, Fyn, Lyn, Hck and Lck. Phase 1. | Pan | Chk1, IC50: 5 nM |
