219491
Cdk/Crk Inhibitor
The Cdk/Crk Inhibitor, also referenced under CAS 784211-09-2, controls the biological activity of Cdk/Crk. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.
Synonym(s):
Cdk/Crk Inhibitor, 1-(2,6-Dichlorophenyl)-1,5-dihydro-6-((4-(2-hydroxyethoxy)phenyl)methyl)-3-(1-methylethyl)-4H-pyrazolo[3,4-d]pyrimidin-4-one, RGB-286147, Cdk7 Inhibitor IV
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About This Item
Empirical Formula (Hill Notation):
C23H22Cl2N4O3
CAS Number:
Molecular Weight:
473.35
MDL number:
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥95% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
Quality Segment
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
−20°C
General description
A cell-permeable pyrazolo-pyrimidinone compound that acts as a potent, selective, and ATP-competitive inhibitor of Cdks (IC50 = 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively). It inhibits Cdk4/D1, Cdk6/D3, and GSK-3β only at much higher concentrations (IC50 = 839 nM, 282 nM, and 754 nM, respectively) and exhibits little activity towards a panel of 60 other kinases. A broad-spectrum growth inhibitor toward tumor cells, but not non-transformed quiescent fibroblasts.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9
Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9
Product competes with ATP.
Reversible: no
Target IC50: 48 nM, 15 nM, 9 nM, 10 nM, 71 nM, and 9 nM for Cdk1/B, Cdk2/E, Cdk3/E, Cdk5/p35, Cdk7/H/MAT1, and Cdk9, respectively
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Caligiuri, M., et al. 2005. Chem. Biol.12, 1103.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
Storage Class
11 - Combustible Solids
wgk
WGK 1
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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