受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H21F3N4O3S |
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分子量 | 514.52 | CAS No. | 1314890-29-3 | ||||
Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (194.35 mM) | ||||
Ethanol (warmed with 50ºC water bath) | 2 mg/mL (3.88 mM) | ||||||
Water | Insoluble | ||||||
体内 (毎回新しく調製した物を用意してください) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | TMP269 is a potent, selective class IIa HDAC inhibitor with IC50 of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively. |
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in vitro | TMP269 has no impact on the mitochondrial activity and/or the viability of human CD4+ T cells at 10 μM, and may be used as tools to identify the endogenous substrates of the class IIa HDAC enzymes. [1] In IEC-18 intestinal epithelial cells, TMP269 prevents cell cycle progression, DNA synthesis, and proliferation induced in response to G protein-coupled receptor/PKD1 activation. [2] |
in vivo | TMP269 is a selective class IIa HDAC inhibitor. |
キナーゼアッセイ | HDAC selectivity assays | |
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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. | ||
細胞アッセイ | 細胞株 | Human CD4+ T cells |
濃度 | 10 μM | |
反応時間 | 72 hours | |
実験の流れ | 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. |
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動物実験 | 動物モデル | Nude Mice |
投薬量 | 15 mg/kg | |
投与方法 | i.p. |
Data from [Data independently produced by , , Clin Epigenetics, 2018, 10(1):100]
Data from [Data independently produced by , , THE JOURNAL OF BIOLOGICAL CHEMISTRY, 2016, 291(14):7386-7395.]
Data from [Data independently produced by , , J Cell Biochem, 2018, 119(4):3081-3090]
Improvement of muscle strength in a mouse model for congenital myopathy treated with HDAC and DNA methyltransferase inhibitors [ Elife, 2022, 11e73718] | PubMed: 35238775 |
The p300/CBP inhibitor A485 normalizes psoriatic fibroblast gene expression in vitro and reduces psoriasis-like skin inflammation in vivo [ J Invest Dermatol, 2022, S0022-202X(22)01937-6] | PubMed: 36174717 |
Beta-hydroxybutyrate suppresses hepatic production of the ghrelin receptor antagonist, LEAP2 [ Endocrinology, 2022, bqac038] | PubMed: 35352108 |
Angiogenic adipokine C1q-TNF-related protein 9 ameliorates myocardial infarction via histone deacetylase 7-mediated MEF2 activation [ Sci Adv, 2022, 8(48):eabq0898] | PubMed: 36459558 |
Targeting cancer cell plasticity by HDAC inhibition to reverse EBV-induced dedifferentiation in nasopharyngeal carcinoma [ Signal Transduct Target Ther, 2021, 6(1):333] | PubMed: 34482361 |
IL-4 inhibits regulatory T cells differentiation by HDAC9-mediated epigenetic regulation [ Cell Death Dis, 2021, 12(6):501] | PubMed: 34006836 |
Butyrate and Class I Histone Deacetylase Inhibitors Promote Differentiation of Neonatal Porcine Islet Cells into Beta Cells [ Cells, 2021, 10(11)3249] | PubMed: 34831471 |
Pre-Senescence Induction in Hepatoma Cells Favors Hepatitis C Virus Replication and Can Be Used in Exploring Antiviral Potential of Histone Deacetylase Inhibitors [ Int J Mol Sci, 2021, 22(9)4559] | PubMed: 33925399 |
Effect of HDAC9 inhibition on epithelial-mesenchymal transition in CD133+ prostate cancer cell lines [ J Chemother, 2021, 1-10] | PubMed: 34424139 |
HDAC7 is an actionable driver of therapeutic antibody resistance by macrophages from CLL patients [ Oncogene, 2020, 10.1038/s41388-020-01394-w] | PubMed: 32709923 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
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