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529582 Sigma-AldrichPP1 Analog III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem

PP1 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.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet

同义词: 1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
956025-83-5	C₁₇H₂₁N₅

价格及供货情况

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Description
Overview	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.
Catalogue Number	529582
Brand Family	Calbiochem®
Synonyms	1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor

References
References	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.

Product Information
CAS number	956025-83-5
Form	White solid
Hill Formula	C₁₇H₂₁N₅
Chemical formula	C₁₇H₂₁N₅
Structure formula Image
Quality Level	MQ100

Applications
Application	PP1 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 Instructions	Following 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

Global Trade Item Number
产品目录编号	GTIN
529582-5MGCN	04055977269888

Documentation

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

职位
物料安全数据表 (MSDS)

PP1 Analog III, 3-MB-PP1 - CAS 956025-83-5 - Calbiochem 分析证书

标题	批号
529582	输入批号

参考

参考信息概述
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.

数据表

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.

Revision	23-February-2011 RFH
Synonyms	1-(tert-Butyl)-3-(3-methylbenzyl)-1H-pyrazolo[3,4-d]pyrimidin-4-amine, Plk1 ASKA Inhibitor, Syk ASKA Inhibitor, ZAP-70 ASKA Inhibitor
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.
Form	White solid
Intert gas (Yes/No)	Packaged under inert gas
CAS number	956025-83-5
Chemical formula	C₁₇H₂₁N₅
Structure formula
Purity	≥97% by HPLC
Solubility	DMSO (50 mg/ml)
Storage	Protect from light +2°C to +8°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity	Standard Handling
References	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.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Polo-like Kinase Inhibitors

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