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CAS No.: 221244-14-0

1-NM-PP1 Catalog No. CSN15942

Synonyms: PP1 Analog II

1NM-PP1 is a cell-permeable PP1 analog that acts as a potent and selective inhibitor of mutant kinases over their wild-type progenitors with IC50 of 28 μM for vSrc and 4.2 nM for v-Src-as1 I338G.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 v-Src

IC50:28μM v-Src (I338G)

IC50:4.2nM
描述1-NM-PP1, a cell-permeable PP1 analog, is a potent Src family kinases inhibitor with IC50s of 4.3 nM and 3.2 nM for v-Src-as1 and c-Fyn-as1, respectively^[2]. A high dose of 1NM-PP1, by intraperitoneal injection, just before the parasite inoculation effectively reduced the parasite load in the brains, livers, and lungs of T. gondii-infected mice, however, a low dose of 1NM-PP1 with oral administration didn't change the survival rates of infected mice^[3]. Bumped kinase inhibitor 1NM-PP1 inhibits the growth of T. gondii by targeting TgCDPK1. Host cell lysis of RH/ku80(-)/HA-TgMAPKL-1(S191A) was completely inhibited at 250 nM 1NM-PP1, whereas that of RH/ku80(-)/HA-TgMAPKL-1(S191Y) was not^[4]. By injecting a small molecule derivative of the protein kinase inhibitor protein phosphatase 1 (1NM-PP1), it is possible to produce highly selective inhibition of TrkB autophosphorylation in adult mice, without interfering with the activity of other protein kinases. Oral administration of 1NM-PP1, at doses that blocked phosphorylation of TrkB in the spinal cord, had no effect in behavioral tests of acute heat, mechanical, or chemical pain sensitivity^[5].
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
- 3.0174 mL
- 15.0869 mL
- 30.1737 mL
- 5 mM
- 0.6035 mL
- 3.0174 mL
- 6.0347 mL
- 10 mM
- 0.3017 mL
- 1.5087 mL
- 3.0174 mL

技术信息

CAS号

221244-14-0

储存条件

粉末: Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H21N5

运输

蓝冰

分子量

331.41

别名

PP1 Analog II

溶解度

DMSO	27.5 mg/mL (83.0 mM)

动物实验配方

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靶点	Description	IC50
v-Src		IC50:28μM
v-Src (I338G)		IC50:4.2nM

1-NM-PP1 Catalog No. CSN15942

靶点选择性

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