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PP1

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Chemical Structure| 172889-26-8 同义名 : EI 275;AGL 1872;PP1 (Src Inhibitor)
CAS号 : 172889-26-8
货号 : A211100
分子式 : C16H19N5
纯度 : 99%+
分子量 : 281.356
MDL号 : MFCD01076570
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(88.86 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • Fyn

    Fyn, IC50:6 nM

  • Lck

    LCK, IC50:5 nM
描述 Src is the best understood member of a family of 9 tyrosine kinases that regulates cellular responses to extracellular stimuli. The Src family of non-receptor tyrosine kinases are integrators of divergent signal transduction pathways which regulate numerous cellular processes, including tumorigenicity and angiogenesis[3]. Dysfunction of Src, through overexpression or increased activation, has profound effects on basic cellular functions. Elevated Src expression and/or activation is evident across a wide range of solid tumour types.[4]. PP1 is a potent, and Src family-selective tyrosine kinase inhibitor with IC50 of 5 and 6 nM for Lck and Fyn, respectively. PP1 inhibits Lck (IC50=5 nM) and FynT (IC50=6 nM) in vitro at concentrations significantly lower than those required to inhibit ZAP-70 (IC50>100 μM), JAK2 (IC50>50 μM), the EGFR kinase, and protein kinase A. PP1 inhibits whole cell tyrosine phosphorylation and proliferation in T cells stimulated with anti-CD3 and mitogens. PP1 selectively inhibits IL-2 gene expression over GM-CSF and IL-2R gene induction in human T cells[5]. PP1 also blocks TGF-β-mediated cellular responses by directly inhibiting type I TGF-β receptors (IC50 = 50 nM) in a manner unrelated to Src signaling[6].
细胞研究
细胞系 浓度 检测类型 检测时间 活动说明 数据源
Jurkat cells Function assay Inhibition of MLR stimulated IL-2 production in Jurkat cells, IC50=0.4 μM 11012021
mouse NIH/3T3 cells 0.08-20 μM Function assay Inhibition of v-Src phosphorylation expressed in mouse NIH/3T3 cells at 0.08 to 20 uM by Western blot analysis 18849971
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00797797 Fibromyalgia Phase 3 Completed - -
NCT02431702 Schizophrenia ... 展开 >> Psychotic Disorders 收起 << Phase 3 Active, not recruiting October 26, 2019 -
NCT03072355 Healthy Volunteers Not Applicable Completed - Brazil ... 展开 >> Carlos Pastre, PhD Presidente Prudente, Brazil, +551832295528 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.55mL

0.71mL

0.36mL

17.77mL

3.55mL

1.78mL

35.54mL

7.11mL

3.55mL
参考文献

[1]Tatton L, Morley GM, et al. The Src-selective kinase inhibitor PP1 also inhibits Kit and Bcr-Abl tyrosine kinases. J Biol Chem. 2003 Feb 14;278(7):4847-53.

[2]Hanke JH, Gardner JP, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem. 1996 Jan 12;271(2):695-701.

[3]Nagaraj S Nagathihalli,et al. Src-mediated regulation of E-cadherin and EMT in pancreatic cancer. Front Biosci (Landmark Ed).2012 Jun 1;17:2059-69.

[4]B Elsberger,et al. Is Src a viable target for treating solid tumours? Curr Cancer Drug Targets. 2010. 10(7), 683-94.

[5]Hanke JH, et al. Discovery of a novel, potent, and Src family-selective tyrosine kinase inhibitor. Study of Lck- and FynT-dependent T cell activation. J Biol Chem. 1996. 271(2), 695-701.

[6]Ungefroren, H., Sebens, S., Groth, S., et al. The Src family kinase inhibitors PP2 and PP1 block TGFβ-mediated cellular responses by direct and differential inhibition of type I and type II TGFβreceptors. Curr. Cancer Drug Targets. 2011. 11(4), 524-535.