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529582 PP1 Analog III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem

529582
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Panoramica

Replacement Information

Tabella delle specifiche principali

Empirical FormulaCAS #
C₁₇H₂₁N₅ 956025-83-5

Products

Numero di catalogoConfezionamento Qtà/conf
529582-5MG 5 mg
Description
OverviewA 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 µM, respectively), ZAP-70C405V M414A/ZAP-70M414A (complete prevention and elimination, respectively, of αTCR-stimulated [Ca2+] elevation in ASKA transfectants when applied before or after αTCR stimulation at 6 µM), and SykM442A 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.
Catalogue Number529582
Brand Family Calbiochem®
Synonyms1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor
References
ReferencesMiller, 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. USA 104, 4383.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.
Product Information
CAS number956025-83-5
FormWhite solid
Hill FormulaC₁₇H₂₁N₅
Chemical formulaC₁₇H₂₁N₅
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
ApplicationPP1 Analog III, 3-MB-PP1, CAS 956025-83-5, is a cell-permeable, potent, ATP-competitive, and highly selective inhibitor of polo-like kinase 1C67V L130G and ZAP-70C405V M414A/ZAP-70M414A.
Biological Information
Purity≥97% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
Product Usage Statements
Storage and Shipping Information
Ship Code Ambient Temperature Only
Toxicity Standard Handling
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

PP1 Analog III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem MSDS

Titolo

Scheda di sicurezza (MSDS) 

PP1 Analog III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem Certificati d'Analisi

TitoloNumero di lotto
529582

Riferimenti bibliografici

Panoramica delle referenze
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. USA 104, 4383.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.
Scheda tecnica

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision23-February-2011 RFH
Synonyms1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor
DescriptionA 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 µM, respectively), ZAP-70C405V M414A/ZAP-70M414A (complete prevention and elimination, respectively, of αTCR-stimulated [Ca2+] elevation in ASKA transfectants when applied before or after αTCR stimulation at 6 µM), and SykM442A 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.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number956025-83-5
Chemical formulaC₁₇H₂₁N₅
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (50 mg/ml)
Storage +2°C to +8°C
Protect from light
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Standard Handling
ReferencesMiller, 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. USA 104, 4383.
Bishop, A.C., et al. 1999. J. Am. Chem. Soc. 121, 627.