| Identification | Back Directory | [Name]
CDK1/2InhibitorIII | [CAS]
443798-55-8 | [Synonyms]
2 Inhibitor III
CDK1/2InhibitorIII
Cdk-1/2 Inhibitor III,Cdk1/2 Inhibitor III
5-amino-N-(2,6-difluorophenyl)-3-(4-sulfamoylanilino)-1,2,4-triazole-1-carbothioamide
1H-1,2,4-Triazole-1-carbothioamide, 3-amino-5-[[4-(aminosulfonyl)phenyl]amino]-N-(2,6-difluorophenyl)- | [Molecular Formula]
C15H13F2N7O2S2 | [MOL File]
443798-55-8.mol | [Molecular Weight]
425.44 |
| Chemical Properties | Back Directory | [Boiling point ]
649.1±65.0 °C(Predicted) | [density ]
1.72±0.1 g/cm3(Predicted) | [storage temp. ]
+2C to +8C | [solubility ]
DMSO: 10mg/mL
THF: soluble
acetone: soluble | [form ]
White solid | [pka]
6.61±0.70(Predicted) | [color ]
white |
| Hazard Information | Back Directory | [Uses]
Cyclin-dependent kinases (Cdks) are key regulators of cell cycle progression and are therefore promising targets for cancer therapy. Cdk1/2 Inhibitor III is a cell-permeable inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50s = 0.6 and 0.5 nM, respectively). It less potently inhibits CDC2-like kinases 1 and 3, VEGFR2, and GSK-3β (IC50s = 8.9, 29, 32, and 140 nM, respectively) and is without effect against a panel of other kinases. Cdk1/2 Inhibitor III blocks the growth of several cancer cell lines (IC50 values range from 20 to 92 nM). | [Uses]
Cyclin-dependent kinases (CDKs) are protein kinases and involved with the regulation of the cell cycle. CDK 1/2 inhibitor III selectively inhibits CDK1 and CDK2. Studies have shown that CDK 1/2 Inhibitor III can also inhibit in vitro cellular proliferation in various human tumor cells. | [General Description]
A cell-permeable triazolo-diamine compound that displays anti-proliferative properties in various human cancer cells (IC50 = 20 nM, 35 nM and 92 nM in HCT-116, HeLa, and A375 cells, respectively). Acts as a highly potent, reversible, ATP-competitive inhibitor of Cdk1/cyclin B and Cdk2/cyclin A (IC50 = 600 pM and 500 pM, respectively) with selectivity over VEGF-R2 (IC50 = 32 nM), GSK-3β (IC50 = 140 nM), and a panel of eight other kinases (IC50 ≥ 1 μM). | [Biochem/physiol Actions]
Cell permeable: yes | [IC 50]
Cdk1/cyclin B: 2.1 μM (IC50) |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
cjbscvictory
|
| Tel: |
13348960310 |
| Website: |
https://www.weikeqi-biotech.com/ |
| Company Name: |
Enzo Biochem Inc
|
| Tel: |
Enzo Biochem Inc. 13797054060 |
| Website: |
www.enzo.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|