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Description

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 1C67V L130G (75% and 94% inhibition in cell-free kinase assays at 0.1 and 1 µ,M, respectively), ZAP-70C405V M414A/ZAP-70M414A (complete prevention and elimination, respectively, of alphaTCR-stimulated [Ca2+] elevation in ASKA transfectants when applied before or after alphaTCR stimulation at 6 µ,M), and SykM442A S505A (56% inhibition of phagocytosis of Ab-opsonized SRBC by ASKA macrophages at 6 µ,M), 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., 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 1C67V L130G (75% and 94% inhibition in cell-free kinase assays at 0.1 and 1 µ,M, respectively), ZAP-70C405V M414A/ZAP-70M414A (complete prevention and elimination, respectively, of alphaTCR-stimulated [Ca2+] elevation in ASKA transfectants when applied before or after alphaTCR stimulation at 6 µ,M), and SykM442A S505A (56% inhibition of phagocytosis of Ab-opsonized SRBC by ASKA macrophages at 6 µ,M), 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.