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PP1 Src Inhibitor

Catalog # CD0334

Price:  1 mg - $50; 5 mg - $75; 10 mg - $120; 25 mg - $280; 50 mg - $490; 100 mg - $890

Availability:  In stock

 

 

4-Amino-5-(4-methylphenyl)-7-(t-butyl)pyrazolo-d-3,4-pyrimidine

 

White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. Purity: 99% by HPLC. CAS# 172889-26-8. Solubility: DMSO (25 mg/mL). Molecular Formula: C16H19N5. Molecular Weight: 281.36.

 

 

A cell-permeable pyrazolopyrimidine compound that is shown to inhibit Src family tyrosine kinases Lck, Fyn, Hck, and Src (IC50 = 5, 6, 20, and 170 nM, respectively), as well as non-Src family kinases such as CSK, RIP2, and CK1δ (IC50 = 640 nM, 26 nM, 170 nM, respectively), in in vitro kinase assays. At 1 M, in vitro kinase activity is reduced by more than 57% for p38α, p38β, CK1δ, CSK, RIP2, and GAK, while exhibiting much lower activity against more than 60 other kinases. Kinetic studies employing Src and [poly Glu-Tyr 4:1] indicate that the inhibition is mixed competitive with respect to the substrate and non-competitive with respect to ATP. PP1 also demonstrates anti-growth properties in several B lymphoma cultures of human and murine origins (IC50 = 2.5 to 8.0 M) and pediatric brain tumor cells (IC50 = 1.1 to 9.7 M).

 

References: 1. Ke, J., et. al. Mol. Cancer 2009, 8, 132; 2. Sikkema, A.H., et al. Cancer Res. 2009, 69, 5987; 3. Bain, J., et al. Biochem. J. 2007, 408, 297; 4. Bain, J., et al. Biochem. J. 2003, 371, 199; 5. Karni, R., et al. FEBS Lett. 2003, 537, 47; 5. Hanke, J.H., et al. J. Biol. Chem. 1996, 271, 695.

 

 

SAME PRODUCT AS:

Axxora 

Cat. No. ALX-270-177

 

Cayman Chemical  

Cat. No. N/A

Enzo Life Sciences 

Cat. No. ALX-270-177

EMD

Cat. No. 567809

Tocris   

Cat. No. 1397

Sigma

Cat. No. P0040

 

 

Caution Not fully tested. For research use only. Not for human use.

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