Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 526 | 现货 | ||
5 mg | ¥ 928 | 现货 | ||
10 mg | ¥ 1,410 | 现货 | ||
25 mg | ¥ 2,697 | 现货 | ||
50 mg | ¥ 3,540 | 现货 | ||
100 mg | ¥ 5,120 | 现货 | ||
200 mg | ¥ 7,260 | 现货 | ||
500 mg | ¥ 10,700 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 967 | 现货 |
产品描述 | 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. |
靶点活性 | HDAC5:97 nM, HDAC9:23 nM, HDAC7:43 nM, HDAC4:157 nM |
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。 |
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. |
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) |
化合物与蛋白结合的复合物 |
HDAC7 bound with inhibitor TMP269 |
分子量 | 514.52 |
分子式 | C25H21F3N4O3S |
CAS No. | 1314890-29-3 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 93 mg/mL (180.8 mM)
Ethanol: 2 mg/mL (3.88 mM), warmed
H2O: < 1 mg/mL (insoluble or slightly soluble)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO / Ethanol | 1 mM | 1.9436 mL | 9.7178 mL | 19.4356 mL | 48.589 mL |
DMSO | 5 mM | 0.3887 mL | 1.9436 mL | 3.8871 mL | 9.7178 mL |
10 mM | 0.1944 mL | 0.9718 mL | 1.9436 mL | 4.8589 mL | |
20 mM | 0.0972 mL | 0.4859 mL | 0.9718 mL | 2.4294 mL | |
50 mM | 0.0389 mL | 0.1944 mL | 0.3887 mL | 0.9718 mL | |
100 mM | 0.0194 mL | 0.0972 mL | 0.1944 mL | 0.4859 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
TMP269 1314890-29-3 Chromatin/Epigenetic DNA Damage/DNA Repair HDAC Inhibitor TMP-269 TMP 269 Histone deacetylases inhibit inhibitor