172889-26-8|PP1|CsnPharm

CAS No.: 172889-26-8

PP1 Catalog No. CSN11758

Synonyms: AGL 1872;EI 275

PP1 is a selective inhibitor of Src and Lck/Fyn with IC50 of 5 nM, 6 nM, respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 Lck

IC50:5nM Fyn

IC50:6nM
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

Cell Data

Cell Lines	Concentration	Assay Type	Time	Activity Description	Data Sources
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 ... more >> Psychotic Disorders Collapse <<	Phase 3	Active, not recruiting	October 26, 2019	-
NCT03072355	Healthy Volunteers	Not Applicable	Completed	-	Brazil ... more >> Carlos Pastre, PhD Presidente Prudente, Brazil, +551832295528 Collapse <<

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参考文献

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5542 mL
- 17.7711 mL
- 35.5422 mL
- 5 mM
- 0.7108 mL
- 3.5542 mL
- 7.1084 mL
- 10 mM
- 0.3554 mL
- 1.7771 mL
- 3.5542 mL

技术信息

CAS号

172889-26-8

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C16H19N5

运输

蓝冰

分子量

281.36

别名

AGL 1872;EI 275

溶解度

DMSO	4.0 mg/mL (14.2 mM)
Water	Insoluble
Ethanol	Insoluble

动物实验配方

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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 ... more >> Psychotic Disorders Collapse <<	Phase 3	Active, not recruiting	October 26, 2019	-
NCT03072355	Healthy Volunteers	Not Applicable	Completed	-	Brazil ... more >> Carlos Pastre, PhD Presidente Prudente, Brazil, +551832295528 Collapse <<
NCT02185339	Laparoscopic Renal Surgery ... more >> Laparoscopy Muscle Relaxation Collapse <<	Phase 4	Completed	-	Korea, Republic of ... more >> Seoul St. Mary's Hospital Seoul, Korea, Republic of, 137-701 Collapse <<
NCT03206359	-	-	Completed	-	-
NCT00797797	-	-	Completed	-	-
NCT01406496	Type 1 Diabetes Mellitus	Not Applicable	Unknown	December 2013	Israel ... more >> Pediatric Endocrinology Unit, Kaplan Medical Center Recruiting Rehovot, Israel, 76100 Contact: Amnon Zung, MD 972-8-9441260 amnon_z@clalit.org.il Principal Investigator: Amnon Zung, MD Sub-Investigator: Nitza Vazana, RN Sub-Investigator: Lilach Hofi, R.Nutr Collapse <<
NCT02185339	-	-	Completed	-	-
NCT01047605	Healthy	Phase 1	Completed	-	Germany ... more >> Neurocode AG Wetzlar, Germany, D-35578 Collapse <<
NCT01515423	Schizophrenia	Phase 3	Completed	-	-
NCT01515423	-	-	Completed	-	-
NCT00791843	Congestive Heart Failure	Phase 2	Completed	-	United States, Massachusetts ... more >> Massachusetts General Hospital/ Geriatric Research Boston, Massachusetts, United States, 02114 Collapse <<
NCT03713658	Schizophrenia	Phase 4	Recruiting	April 10, 2020	Rwanda ... more >> CARAES Ndera Neuro-Psychiatric Hospital Recruiting Kigali, Rwanda, 423 University Teaching Hospital of Kigali Not yet recruiting Kigali, Rwanda, 655 Ruhengeri Referral Hospital, Public Hospital Recruiting Musanze District, Rwanda, 57 Kibungo Referral Hospital Not yet recruiting Ngoma District, Rwanda, 10 Collapse <<
NCT03666715	-	-	Recruiting	August 15, 2019	Portugal ... more >> Neurobios , Instituto De Neurociências Recruiting Porto, Portugal, Portugal, 4200 - 117 Collapse <<
NCT02713282	Schizophrenia	Phase 3	Completed	-	-
NCT03345342	Schizophrenia	Phase 3	Recruiting	August 31, 2020	-

靶点	Description	IC50
Lck		IC50:5nM
Fyn		IC50:6nM

PP1 Catalog No. CSN11758

靶点选择性

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