storage temp.
2-8°C
InChI key
DYTKVFHLKPDNRW-UHFFFAOYSA-N
InChI
1S/C14H12N6O2S/c1-8-12(23-13(15)17-8)11-5-6-16-14(19-11)18-9-3-2-4-10(7-9)20(21)22/h2-7H,1H3,(H2,15,17)(H,16,18,19)
assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
yellow
solubility
DMSO: 25 mg/mL
shipped in
ambient
Quality Level
General description
A cell-permeable aminopyrimidinyl compound that acts as a potent and ATP-competitive inhibitor of Cdk2/E and Cdk9/T1 (Ki = 2 nM and 4 nM, respectively). It also inhibits GSK-3β, Cdk4/D1, Cdk7/H, Cdk1/B, and Abl at higher concentrations (Ki = 20, 53, 70, 80, and 160 nM, respectively), but exhibits little activity towards 9 other kinases (Ki >1.0 µM). Shown to inhibit phosphorylation of cellular Cdk substrates, pRb and RNA polymerase II, and Cdk2-mediated S-phase transition.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
Cdk2/E and Cdk9/T1
Cdk2/E and Cdk9/T1
Product competes with ATP.
Reversible: no
Target Ki: 2 nM and 4 nM against Cdk2/E and Cdk9/T1, 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
Kontopidis, G., et al. 2006. Chem. Biol.13, 201.
Wang, S., et al. 2004. J. Med. Chem.47, 1662.
Wang, S., et al. 2004. J. Med. Chem.47, 1662.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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