1-NM-PP1,221244-14-0

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1-NM-PP1

CAS No. : 221244-14-0

MCE 国际站：1-NM-PP1

产品活性：1-NM-PP1，细胞渗透性 PP1 类似物，是一种有效的 Src 家族激酶抑制剂，对 v-Src-as1 与 c-Fyn-as1 的 IC₅₀ 值分别为 4.3 nM、3.2 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Src

In Vitro: Cdk7 from Cdk7^as/as or Cdk7^+/+ cells is immunoprecipitated and tested its kinase activity towards both a Pol II CTD-containing fusion protein (GST-CTD) and human Cdk2. Cdk7 recovered from the mutant, but not the wild-type, cells is inhibited by 1-NM-PP1 (1-NMPP1), with an IC₅₀ of ~50 nM with either substrate. Replacement of wild-type Cdk7 with Cdk7^as/as also rendered growth of HCT116 cells sensitive to 1-NM-PP1. In the absence of 1-NM-PP1, the wild-type andCdk7^as/as cells had population doubling times of ~17.9 and ~20.2 h, respectively, with similar cell-cycle distributions in asynchronous culture, indicating minimal impairment of Cdk7 function by the F91G mutation per se. The homozygous Cdk7^as/as cells are sensitive to 1-NM-PP1, however, with an IC₅₀ ~100 nM measured by cell viability (MTT) assays performed after 96 h of 1-NM-PP1 exposure. In contrast, wild-type HCT116 cells are resistant to 10 μM 1-NM-PP1. Addition of 10 μM 1-NM-PP1 retards G1/S progression by the mutant but not the wild-type cells. When added simultaneously with serum to the Cdk7^as/as cells, 1-NM-PP1 prevents any progression into S phase in the next 15 h. After 24 h, there is evidence of progression into S-phase by a fraction of Cdk7^as/as cells released from serum starvation directly into medium containing 1-NM-PP1, while a fraction remained in G1. The addition of 1-NM-PP1 3 h or 6 h after serum addition delays S-phase entry by ~7 h or by ~3 h, respectively.

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