TMP269

製品コードS7324 バッチS732402

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder 1 years -80°C in solvent
	化学式	C₂₅H₂₁F₃N₄O₃S
	分子量	514.52	CAS No.	1314890-29-3
Solubility (25°C)*	体外	DMSO	100 mg/mL (194.35 mM)
		Ethanol	3 mg/mL warmed with 50ºC water bath (5.83 mM)
		Water	Insoluble
* <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.

溶剤液（一定の濃度）を調合する

生物活性

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.
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.

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.

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.

プロトコル(参考用のみ)

キナーゼアッセイ	HDAC selectivity assays
キナーゼアッセイ	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.
動物実験	動物モデル	Nude Mice
	投薬量	15 mg/kg
	投与方法	i.p.

参考

カスタマーフィードバック

: 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]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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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