| Identification | Back Directory | [Name]
CAY10574 | [CAS]
140651-18-9 | [Synonyms]
CAN-508
CAY10574
Cdk9 Inhibitor II
CAN-508
(CAN508)
4-[2-(3,5-diamino-1H-pyrazol-4-yl)diazen-1-yl]phenol
CaMKII Inhibitor, CK59 - CAS 140651-18-9 - Calbiochem | [Molecular Formula]
C9H10N6O | [MDL Number]
MFCD09262258 | [MOL File]
140651-18-9.mol | [Molecular Weight]
218.22 |
| Chemical Properties | Back Directory | [Boiling point ]
638.3±55.0 °C(Predicted) | [density ]
1.67±0.1 g/cm3(Predicted) | [storage temp. ]
+2C to +8C | [solubility ]
DMF: 0.5 mg/ml; DMSO: 0.5 mg/ml | [form ]
Yellow semi-solid | [pka]
8.52±0.30(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
Cdk9 Inhibitor II is an ATP-competitive inhibitor of Cdk9 and moderate inhibitor of similar enzymes. | [Definition]
ChEBI: CAN-508 is a member of the class of pyrazoles that is 1H-pyrazole substituted by amino, (4-hydroxyphenyl)diazenyl, and amino groups at positions 3, 4 and 5, respectively. It is a CDK9 inhibitor (IC50 = 0.35 muM) with 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. It has a role as an angiogenesis inhibitor, an EC 2.7.11.22 (cyclin-dependent kinase) inhibitor, an antineoplastic agent and an apoptosis inducer. It is a member of pyrazoles, a member of phenols, an aromatic amine and a monoazo compound. | [General Description]
A cell-permeable Olomoucine (Cat. Nos. 495620 & 495624) analog that acts as a CaMKII inhibitor (IC50<10 μM) and inhibits insulin-stimulated glucose uptake (IC50 ≤5 μM) and GLUT4 membrane translocation (IC50 = 100 μM) in 3T3-L1 adipocytes. | [Biological Activity]
Cell permeable: yes', 'Primary Target
Cdk9', 'Product competes with ATP.', 'Reversible: no', 'Target IC50: 350 nM, using Cdk9/T1 | [in vivo]
CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts[1]. | Animal Model: | 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts)[1] | | Dosage: | 60 mg/kg | | Administration: | I.p.; daily for 10 days | | Result: | Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.
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| [IC 50]
CDK9/cyclinT1: 0.35 μM (IC50); CDK2/cyclinE: 20 μM (IC50); cdk2/cyclin A: 69 μM (IC50); Cdk4/cyclin D1: 13.5 μM (IC50); CDK7/cyclin H: 26 μM (IC50); Cdk1/cyclin B: 44 μM (IC50) |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
Sigma-Aldrich
|
| Tel: |
021-61415566 800-8193336 |
| Website: |
https://www.sigmaaldrich.cn |
| Company Name: |
BOC Sciences
|
| Tel: |
16314854226 |
| Website: |
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/ |
|