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Merck
CN

529573

PP2

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

别名:

PP2

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关于此项目

经验公式(希尔记法):
C15H16ClN5
化学文摘社编号:
分子量:
301.77
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
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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).

SMILES string

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

assay

≥95% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze

color

off-white

solubility

DMSO: 20 mg/mL

shipped in

ambient

storage temp.

−20°C

Quality Level

Biochem/physiol Actions

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

Disclaimer

毒性:标准处理(A)

General description

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。

Other Notes

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.


Packaging

用惰性气体包装

Preparation Note

仅在使用前再用水相缓冲液进行稀释。

Legal Information

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

存储类别

11 - Combustible Solids

wgk

WGK 3


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Emily C Suter et al.
Cell reports, 36(8), 109587-109587 (2021-08-26)
Cancer immunotherapies often modulate macrophage effector function by introducing either targeting antibodies that activate Fcγ receptors (FcγRs) or blocking antibodies that disrupt inhibitory SIRPα-CD47 engagement. However, how these competing signals are integrated is poorly understood, raising questions about how to
Zahra Alvandi et al.
Methods in molecular biology (Clifton, N.J.), 2520, 261-264 (2021-10-07)
Embryonic stem cells (ESCs) are a unique model that allows the study of molecular pathways underlying commitment and differentiation. We have studied signaling pathways and their contributions to osteogenic differentiation. In addition to our previously published protocol where we recommended
Elliot Dine et al.
Cell reports, 35(12), 109280-109280 (2021-06-24)
Protein clustering is pervasive in cell signaling, yet how signaling from higher-order assemblies differs from simpler forms of molecular organization is still poorly understood. We present an optogenetic approach to switch between oligomers and heterodimers with a single point mutation.
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Breast cancer research : BCR, 25(1), 41-41 (2023-04-15)
Cell adhesion is indispensable for appropriate tissue architecture and function in multicellular organisms. Besides maintaining tissue integrity, cell adhesion molecules, including tight-junction proteins claudins (CLDNs), exhibit the signaling abilities to control a variety of physiological and pathological processes. However, it
Eun-Ji Lim et al.
Cell death & disease, 13(4), 417-417 (2022-04-30)
Colorectal cancer (CRC) has a 5-year survival rate of <10%, as it can metastasize to the lungs and liver. Anticancer drugs and targeted therapies used to treat metastatic colorectal cancer have insufficient therapeutic efficacy and are associated with complications. Therefore

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