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) | ||
|---|---|---|---|---|
| 水 | 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 |
| S8526 | GDC-0575 (ARRY-575, RG7741) | <1 mg/mL | 75 mg/mL | 5 mg/mL |
| S8253 | CCT245737 | <1 mg/mL | 75 mg/mL | 9 mg/mL |
| S8632 | Chk2 Inhibitor II (BML-277) | <1 mg/mL | 72 mg/mL | 21 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 |
AZD7762AZD7762 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. |
CAL120 cells were either untreated or pretreated with gemcitabine for 24 hours followed by treatment with AZD7762 and/or MK-1775 for an additional 2 hours (top) or 8 hours (bottom), before lysis. Western blot analysis of Cyclin B1, CDK1 (phospho-Y15 and total) expression, and β-tubulin as loading control.
|
|
| S2626 |
Rabusertib (LY2603618)Rabusertib (LY2603618) 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. |
MK-1775 and LY2603618 synergize to induce apoptosis in AML cell lines and primary patient samples. U937 and CTS cells were treated for 8 h. Whole cell lysates were subjected to Western blotting and probed with anti-γH2AX, -pCHK1, -p-cdc25c, -p-CDK1, -p-CDK2, -CDK1, or -β-actin antibody. Densitometry measurements, as described in the Materials and methods section, are shown below the corresponding Western blot.
|
|
| 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. |
Western blots of proteins associated with Chk1 activation and apoptosis.
|
|
| S2683 |
CHIR-124CHIR-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. |
Combined effect of doxorubicin and CHIR-124 dose ranges in U2OS cells; means of triplicates are shown; each graph shows one representative of three independent experiments.
|
|
| S2904 |
PF-477736PF-477736 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. |
Cells were treated at the same concentrations as in Caspase3/7 assay for 16 hours and total cell lysates were prepared for Western blotting. GAPDH was used as a loading control.
|
|
| S8526新 |
GDC-0575 (ARRY-575, RG7741)GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM. |
||
| S8253 |
CCT245737CCT245737 is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1. |
||
| 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. |
| 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 |
AZD7762AZD7762 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. |
CAL120 cells were either untreated or pretreated with gemcitabine for 24 hours followed by treatment with AZD7762 and/or MK-1775 for an additional 2 hours (top) or 8 hours (bottom), before lysis. Western blot analysis of Cyclin B1, CDK1 (phospho-Y15 and total) expression, and β-tubulin as loading control.
|
|
| S2626 |
Rabusertib (LY2603618)Rabusertib (LY2603618) 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. |
MK-1775 and LY2603618 synergize to induce apoptosis in AML cell lines and primary patient samples. U937 and CTS cells were treated for 8 h. Whole cell lysates were subjected to Western blotting and probed with anti-γH2AX, -pCHK1, -p-cdc25c, -p-CDK1, -p-CDK2, -CDK1, or -β-actin antibody. Densitometry measurements, as described in the Materials and methods section, are shown below the corresponding Western blot.
|
|
| 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. |
Western blots of proteins associated with Chk1 activation and apoptosis.
|
|
| S2683 |
CHIR-124CHIR-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. |
Combined effect of doxorubicin and CHIR-124 dose ranges in U2OS cells; means of triplicates are shown; each graph shows one representative of three independent experiments.
|
|
| S2904 |
PF-477736PF-477736 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. |
Cells were treated at the same concentrations as in Caspase3/7 assay for 16 hours and total cell lysates were prepared for Western blotting. GAPDH was used as a loading control.
|
|
| S8526新 |
GDC-0575 (ARRY-575, RG7741)GDC-0575 (ARRY-575, RG7741) is a potent and selective CHK1 inhibitor with an IC50 of 1.2 nM. |
||
| S8253 |
CCT245737CCT245737 is an orally active CHK1 inhibitor with The IC50 of 1.4 nM. It exhibits >1,000-fold selectivity against CHK2 and CDK1. |
||
| 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. |
