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Key Documents

529573

Sigma-Aldrich

PP2

≥95% (HPLC), solid, Src protein tyrosine kinase inhibitor, Calbiochem®

同義詞:

PP2

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About This Item

經驗公式(希爾表示法):
C15H16ClN5
CAS號碼:
分子量::
301.77
分類程式碼代碼:
12352200
NACRES:
NA.77

product name

PP2, PP2, CAS 172889-27-9, is a potent, reversible, ATP-competitive, inhibitor of the Src family of protein tyrosine kinases (IC₅₀ = 4, 5, 5, &100 nM for p56lck, p59fynT, Hck, & Src, respectively).

品質等級

化驗

≥95% (HPLC)

形狀

solid

製造商/商標名

Calbiochem®

儲存條件

OK to freeze

顏色

off-white

溶解度

DMSO: 20 mg/mL

運輸包裝

ambient

儲存溫度

−20°C

InChI

1S/C15H16ClN5/c1-15(2,3)21-14-11(13(17)18-8-19-14)12(20-21)9-4-6-10(16)7-5-9/h4-8H,1-3H3,(H2,17,18,19)

InChI 密鑰

PBBRWFOVCUAONR-UHFFFAOYSA-N

一般說明

蛋白酪氨酸激酶Src家族的一种有效、可逆、ATP竞争性和选择性抑制剂。抑制p56lck (IC50=4 nM),p59fynT(IC50=5 nM),Hck(IC50=5 nM)和Src(IC50=100 nM)。不会显著影响EGFR激酶(IC50=480 nM),JAK2(IC50 >50 µM)或ZAP-70(IC50 >100 µ M)的活性。抑制黏着斑激酶的活化及其在Tyr577位点的磷酸化。还有效抑制人T细胞的抗CD3刺激的酪氨酸磷酸化(IC50=600 nM)。也可购买10 mM(1 mg/331 µl)PP2 (目录号529576)DMSO溶液。
酪氨酸激酶src家族的一种有效、可逆、ATP竞争性和选择性抑制剂,类似于PP1。与其他酪氨酸激酶(例如EGF-R(IC50=480 nM),JAK2(IC50 >50 µM)或ZAP-70(IC50 >100 µM))相比,选择性抑制p56lck(IC50 =4 nM),p59fynT (IC50=5 nM),Hck(IC50=5 nM)和Src(IC50 =100 nM)。还有效抑制人T细胞的抗CD3刺激的酪氨酸磷酸化(IC50=600 nM)。

生化/生理作用

主要靶标
p56lck
产物与ATP竞争。
可逆性:是
细胞渗透性:否
靶标IC50:针对p56lck,p59fynT,Hck和Src分别为4 nM,5 nM,5 nM,100 nM;人T细胞的CD3刺激的酪氨酸磷酸化为600 nM

包裝

用惰性气体包装

警告

毒性:标准处理(A)

準備報告

仅在使用前再用水相缓冲液进行稀释。

其他說明

Karni, R., et al. 2003.FEBS Lett.537, 47.
Salazar, E.P., and Rozengurt, E. 1999.J. Biol. Chem. 274, 28371.
Hanke, J.H., et al. 1996.J. Biol. Chem.271, 695.



Selected Citations
Lee, J., et al. 2009.Cell Stem Cell5, 76.


法律資訊

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

儲存類別代碼

11 - Combustible Solids

水污染物質分類(WGK)

WGK 3


分析證明 (COA)

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