推荐产品
产品名称
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).
质量水平
方案
≥95% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
off-white
溶解性
DMSO: 20 mg/mL
运输
ambient
储存温度
−20°C
SMILES字符串
Clc1ccc(cc1)c2n[n](c3ncnc(c32)N)C(C)(C)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 key
PBBRWFOVCUAONR-UHFFFAOYSA-N
一般描述
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
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
包装
用惰性气体包装
警告
毒性：标准处理（A）
制备说明
仅在使用前再用水相缓冲液进行稀释。
其他说明
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.
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.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
储存分类代码
11 - Combustible Solids
WGK
WGK 3
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