名称 | TMP269 |
描述 | TMP269 is an effective, specific class IIa HDAC inhibitor for HDAC4 (IC50: 157 nM), HDAC5 (IC50: 97 nM), HDAC7 (IC50: 43 nM), and HDAC9 (IC50: 23 nM), respectively. |
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 | Shipping with blue ice. |
溶解度 | DMSO : 93 mg/mL (180.8 mM) Ethanol : 2 mg/mL (3.88 mM), Heating is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble)
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关键字 | Inhibitor | TMP-269 | HDAC | TMP 269 | Histone deacetylases | TMP269 | inhibit |
相关产品 | Valproic acid sodium salt | 4-Phenylbutyric acid | Valproic Acid | Panobinostat | Methyl L-histidinate dihydrochloride | Theophylline | Acefylline | Curcumin | Theophylline monohydrate | Sodium 4-phenylbutyrate | Vorinostat | Parthenolide |
相关库 | 抑制剂库 | 抗乳腺癌化合物库 | 经典已知活性库 | 已知活性化合物库 | 抗衰老化合物库 | HIF-1化合物库 | 表观遗传库 | DNA 损伤和修复分子库 | 共价抑制剂库 | 内质网应激化合物库 |