SHP2/HDAC-IN-1,2831230-38-5

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SHP2/HDAC-IN-1

CAS No. : 2831230-38-5

MCE 国际站：SHP2/HDAC-IN-1

产品活性：SHP2/HDAC-IN-1 是一种变构的 SHP2/HDAC 双重抑制剂，IC₅₀ 值分别为 20.4 nM (SHP2) 和 25.3 nM ( HDAC1)。SHP2/HDAC-IN-1 通过激活 T 细胞、增强抗原呈递功能和促进细胞因子分泌来触发抗肿瘤免疫反应。SHP2/HDAC-IN-1 可用于癌症的免疫研究。

研究领域：Protein Tyrosine Kinase/RTK  |  Metabolic Enzyme/Protease  |  Epigenetics  |  Cell Cycle/DNA Damage

作用靶点：SHP2  |  Phosphatase  |  HDAC

In Vitro: SHP2/HDAC-IN-1 (compound 8t, 0-10 μM approximately, 72 h) inhibits the proliferation of BxPC-3, SW1990, AsPC-1and MV4-11 cells.
SHP2/HDAC-IN-1 (0.25-1 μM, 24 h) increases the acetylation of α-tubulin and histone H3 in MV4-11 cells.
SHP2/HDAC-IN-1 (0.25 μM, 24 h) inhibits cell cycle progression in the G1 phase of MV4-11 cells.
SHP2/HDAC-IN-1 (0.25 and 0.5 μM, 24 h) decreases the mitochondrial membrane potential and activats caspase-3.
SHP2/HDAC-IN-1 (2 h) shows good stability in in mouse liver microsome.

In Vivo: SHP2/HDAC-IN-1 (compound 8t, 40 mg/kg, p.o.) inhibits tumor growth in MV4-11 and 4T1 tumor-bearing xenograft mice.
SHP2/HDAC-IN-1 (20 mg/kg p.o., 1 mg/kg i.v.) exhibits good maximum plasma concentrations in rats.

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