529582

3-MB-PP1

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

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₁₇H₂₁N₅
• Número de CAS: 956025-83-5
• Peso molecular: 295.38
• Código UNSPSC: 12352202
• NACRES: NA.77

Propiedades

• product name: PP1 Analog III, 3-MB-PP1, PP1 Analog III, 3-MB-PP1 primarily used in Inhibition.
• Nivel de calidad: 100
• Análisis: ≥97% (HPLC)
• formulario: solid
• fabricante / nombre comercial: Calbiochem^®
• condiciones de almacenamiento: OK to freeze; protect from light
• color: white
• solubilidad: DMSO: 50 mg/mL
• Condiciones de envío: ambient
• temp. de almacenamiento: 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)
• Clave InChI: FYCOTGCSHZKHPR-UHFFFAOYSA-N

Descripción

Descripción general

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.

Envase

Packaged under inert gas

Advertencia

Toxicity: Standard Handling (A)

Reconstitución

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

Otras notas

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.

Información legal

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

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable