4-Amino-1-tert-butyl-3-(3-methylbenzyl)pyrazolo[3,4-d]pyrimidine

Химические свойства

White Solid

Использование

A highly potent and uniquely specific tyrosine kinase inhibitor of a rationally engineered v-Src tyrosine kinase

Общее описание

A cell-permeable C₃-enlarged PP1 (Cat. No. 567809) analog that is shown to act as a potent, ATP-competitive, and highly ASKA- (analog-sensitive kinase alleles) selective inhibitor against polo-like kinase 1^{C67V L130G} (75% and 94% inhibition in cell-free kinase assays at 0.1 and 1 μM, respectively), ZAP-70^{C405V M414A}/ZAP-70^M414A (complete prevention and elimination, respectively, of αTCR-stimulated [Ca²⁺] elevation in ASKA transfectants when applied before or after αTCR stimulation at 6 μM), and Syk^{M442A S505A} (56% inhibition of phagocytosis of Ab-opsonized SRBC by ASKA macrophages at 6 μM), while exhibiting little or no activity toward the wild-type or other off-target cellular enzymes. Functional analog-sensitive allele mutants are valuable tools in pharmacological validation of drug development and in elucidating enzyme signalings and functions both in cultures in vitro and in animals in vivo when specific inhibitors against naturally occurring target enzymes are unavailable and/or generations of knockout animals/cells lacking the target enzymes appear to be difficult, infeasible, or simply impossible.