529582

3-MB-PP1

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

• 同義詞: 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
• 經驗公式（希爾表示法）: C₁₇H₂₁N₅
• CAS號碼: 956025-83-5
• 分子量：: 295.38
• 分類程式碼代碼: 12352202
• NACRES: NA.77

屬性

• product name: PP1 Analog III, 3-MB-PP1, PP1 Analog III, 3-MB-PP1 primarily used in Inhibition.
• 品質等級: 100
• 化驗: ≥97% (HPLC)
• 形狀: solid
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: white
• 溶解度: DMSO: 50 mg/mL
• 運輸包裝: ambient
• 儲存溫度: 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 密鑰: FYCOTGCSHZKHPR-UHFFFAOYSA-N

描述

一般說明

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.

包裝

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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.

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable