Chk

シグナル伝達経路

研究分野

阻害剤の選択性比較

カタログ番号 製品カタログ 溶解度(25°C)
DMSO アルコール
S1532 AZD7762 <1 mg/mL 50 mg/mL <1 mg/mL
S2626 Rabusertib (LY2603618) <1 mg/mL 13 mg/mL '''<1 mg/mL
S2735 MK-8776 (SCH 900776) <1 mg/mL 3 mg/mL <1 mg/mL
S2683 CHIR-124 <1 mg/mL 7 mg/mL <1 mg/mL
S2904 PF-477736 <1 mg/mL 6 mg/mL ''<1 mg/mL
S9639 VX-803 (M4344) <1 mg/mL 15 mg/mL ''<1 mg/mL
S6740 DB07268 <1 mg/mL 64 mg/mL ''<1 mg/mL
S8526 GDC-0575 (ARRY-575) <1 mg/mL 75 mg/mL 5 mg/mL
S7740 SAR-020106 <1 mg/mL 20 mg/mL 2 mg/mL
S8253 CCT245737 <1 mg/mL 75 mg/mL '''''9 mg/mL
S8148 PD0166285 <1 mg/mL 100 mg/mL '100 mg/mL
S8632 Chk2 Inhibitor II (BML-277) <1 mg/mL 72 mg/mL ''21 mg/mL
S7178 Prexasertib HCl (LY2606368) <1 mg/mL 2 mg/mL <1 mg/mL
S3224 Cinobufagin -1 mg/mL 100 mg/mL ''-1 mg/mL

亜型選択性的な製品

Chk製品

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

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.

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.

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. Phase 1.

S9639

VX-803 (M4344)

VX-803 (M4344) 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.

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.

S8526

GDC-0575 (ARRY-575)

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

S7740

SAR-020106

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 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.

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.

S8632

Chk2 Inhibitor II (BML-277)

Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.

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.

S3224

Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
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.

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.

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.

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.

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. Phase 1.

S9639

VX-803 (M4344)

VX-803 (M4344) 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.

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.

S8526

GDC-0575 (ARRY-575)

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

S7740

SAR-020106

SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 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.

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.

S8632

Chk2 Inhibitor II (BML-277)

Chk2 Inhibitor II (BML-277) is an ATP-competitive inhibitor of Chk2 with IC50 of 15 nM. It is 1000-fold more selective toward Chk2 serine/threonine kinase than for Chk1 and Cdk1/B kinases. Chk2 Inhibitor II (BML-277) dose dependently protects human CD4(+) and CD8(+) T-cells from apoptosis due to ionizing radiation.

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.

製品コード 製品説明 文献中Selleckの製品使用例 お客様のフィードバック
S3224

Cinobufagin

Cinobufagin (Cinobufagine), an active ingredient of Venenum Bufonis, inhibits tumor development. Cinobufagin increases ATM and Chk2 and decreases CDC25C, CDK1, and cyclin B. Cinobufagin inhibits PI3K, AKT and Bcl-2 while increases levels of cleaved caspase-9 and caspase-3. Thus, Cinobufagin induces cell cycle arrest at the G2/M phase and apoptosis.

Tags: Checkpoint activation | Checkpoint kinase | Checkpoint function | Checkpoint activity | Chk1 phosphorylation | Checkpoint pathway | Chk1 pathway | Chk2 pathway | Chk2 phosphorylation | Chk1 inhibitor clinical trial | Chk1 inhibition | Chk1 activation | Chk2 activation | Chk1 assay | Chk inhibitors review