529582

3-MB-PP1

≥97% (HPLC), solid, PP1 analog, Calbiochem^®

• Synonym(s): PP1 Analog III, 3-MB-PP1, 1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor, 1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor
• Empirical Formula (Hill Notation): C₁₇H₂₁N₅
• CAS Number: 956025-83-5
• Molecular Weight: 295.38
• UNSPSC Code: 12352202
• NACRES: NA.77

Properties

• product name: PP1 Analog III, 3-MB-PP1, PP1 Analog III, 3-MB-PP1 primarily used in Inhibition.
• Quality Level: 100
• assay: ≥97% (HPLC)
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: DMSO: 50 mg/mL
• shipped in: ambient
• storage temp.: 2-8°C
• InChI: 1S/C17H21N5/c1-11-6-5-7-12(8-11)9-13-14-15(18)19-10-20-16(14)22(21-13)17(2,3)4/h5-8,10H,9H2,1-4H3,(H2,18,19,20)
• InChI key: FYCOTGCSHZKHPR-UHFFFAOYSA-N

Description

General 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 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.

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.

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Reconstitution

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

Other Notes

Miller, A.L., et al. 2009. J. Immunol.182, 988.
Levin, S.E., et al. 2008. J. Biol. Chem.283, 15419.
Burkard, M.E., et al. 2007. Proc. Natl. Acad. Sci. USA104, 4383.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc.121, 627.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable