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Chk
Chk製品
- All (17)
- Chk阻害剤 (16)
- Chk活性剤(1)
- 新製品
| 製品コード | 製品名称 | 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| 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. |
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| S8632 | BML-277 (Chk2 Inhibitor II) | BML-277 (Chk2 Inhibitor II) 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. | ||
| 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. | ||
| S8253 | CCT245737 (SRA737) | CCT245737 (SRA737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1. | ||
| S8526 | GDC-0575 | GDC-0575 is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E1653New | CCT241533 hydrochloride | CCT241533 hydrochloride is an ATP competitive, potent, and selective inhibitor of CHK2 with an IC50 of 3 nM and a Ki of 1.16 nM and shows minimal cross-reactivity against a panel of kinases. CCT241533 inhibits CHK2 activity in human tumor cell lines when subjected to DNA damage. | ||
| S7740 | SAR-020106 | SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM. | ||
| E1667New | LY2880070 | LY2880070 is an orally active inhibitor of CHK1. LY2880070 can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents. | ||
| 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. |
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| 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. |
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| 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. |
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|
| 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. |
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| 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. |
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|
| 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. |
|
|
| S8632 | BML-277 (Chk2 Inhibitor II) | BML-277 (Chk2 Inhibitor II) 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. | ||
| 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. | ||
| S8253 | CCT245737 (SRA737) | CCT245737 (SRA737) is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1. | ||
| S8526 | GDC-0575 | GDC-0575 is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM. | ||
| 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. | ||
| 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. | ||
| 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. | ||
| E1653New | CCT241533 hydrochloride | CCT241533 hydrochloride is an ATP competitive, potent, and selective inhibitor of CHK2 with an IC50 of 3 nM and a Ki of 1.16 nM and shows minimal cross-reactivity against a panel of kinases. CCT241533 inhibits CHK2 activity in human tumor cell lines when subjected to DNA damage. | ||
| S7740 | SAR-020106 | SAR-020106 is an ATP-competitive, potent, and selective CHK1 inhibitor with an IC50 of 13.3 nM. | ||
| E1667New | LY2880070 | LY2880070 is an orally active inhibitor of CHK1. LY2880070 can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents. | ||
| 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. | ||
| E1653New | CCT241533 hydrochloride | CCT241533 hydrochloride is an ATP competitive, potent, and selective inhibitor of CHK2 with an IC50 of 3 nM and a Ki of 1.16 nM and shows minimal cross-reactivity against a panel of kinases. CCT241533 inhibits CHK2 activity in human tumor cell lines when subjected to DNA damage. | ||
| E1667New | LY2880070 | LY2880070 is an orally active inhibitor of CHK1. LY2880070 can be used as an anticancer agent and shows promise in preclinical models of pancreatic ductal adenocarcinoma (PDAC) when used in combination with DNA-damaging agents. |
Chk阻害剤の選択性比較
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
納期 国内在庫品：受注日の翌日（15時までの受注分） ＊北海道、九州、沖縄への配送は受注日より２日以上 を要する場合あり 海外在庫品：受注後１〜２週間