化合物TMP269 T1857

Product Introduction
Bioactivity


英文名: TMP269

描述: TMP269 是一种有效的特异性 IIa 类 HDAC 抑制剂，分别抑制 HDAC 4/HDAC 5/HDAC 7/HDAC 9，IC50值分别为 157 nM，97 nM，43 nM 和 23 nM。

细胞实验: Human CD4+ T cells are isolated from whole blood via negative selection according to manufacturer's instructions (RosetteSep Human CD4+ T cell enrichment kit), re-suspended in T-cell culture medium (10% FBS, 2 mM L-glutamine, 1 mM pyruvate, 10 mM HEPES, 10 U/10 mg penicillin/streptomycin, 0.5% DMSO in RPMI) and plated at 50,000 cells/well with IL-2 (10 BRMP units/mL) and 100,000 human T-expander Dynabeads for 72 h. Determination of mitochondrial function or cell viability is done according to manufacturer's instructions (Cell Proliferation Assay Kit I (MTT)) and is represented as a percent of control (no inhibitor) wells.(Only for Reference)

激酶实验: HDAC selectivity assays: Dose-response studies are done with ten concentrations in a threefold dilution series from a maximum final compound concentration of 100 μM in the reaction mixture and are conducted at Reaction Biology Corp. All assays are based on the same principle as the HDAC9 assay described above: the deacetylation of acetylated or trifluoroacetylated lysine residues on fluorogenic peptide substrates by HDAC. HDAC1, HDAC2, HDAC3, HDAC6, HDAC10 and HDAC11 used a substrate based on residues 379-382 of p53 (Arg-His-Lys-Lys(Ac)). For HDAC8, the diacetylated peptide substrate, based on residues 379–382 of p53 (Arg-His-Lys(Ac)-Lys(Ac)), is used. HDAC4, HDAC5, HDAC7 and HDAC9 assays used the class IIa HDAC–specific fluorogenic substrate (Boc-Lys(trifluoroacetyl)-AMC). All reactions are done with 50 μM HDAC substrate in assay buffer (50 mM Tris-HCl, pH 8.0, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mg/mL BSA) containing 1% DMSO final concentration; incubated for 2 h at 30 °C; and developed with trichostatin A and trypsin.

体内活性: TMP269（10 μM）不影响线粒体活性和/或人CD4+ T细胞的活性,且可用于鉴定IIa类HDAC酶内源性底物。在IEC-18小肠上皮细胞中,TMP269阻止应答G蛋白偶联受体/PKD1活化引起的细胞进程,DNA合成,以及增殖。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 93 mg/mL (180.8 mM)
Ethanol : 2 mg/mL (3.88 mM)
H2O : < 1 mg/mL (insoluble or slightly soluble)


关键字: Inhibitor | TMP-269 | HDAC | TMP 269 | Histone deacetylases | TMP269 | inhibit

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途