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TMP269

目录号: PL04803 纯度: ≥98%

CAS No. :1314890-29-3

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中文名称	TMP269
中文别名	N-[[四氢-4-(4-苯基-2-噻唑基)-2H-吡喃-4-基]甲基]-3-[5-(三氟甲基)-1,2,4-恶二唑-3-基]苯甲酰胺;TMP269 抑制剂;恩拉霉素
英文名称	TMP269
英文别名	N-{[4-(4-Phenyl-1,3-thiazol-2-yl)tetrahydro-2H-pyran-4-yl]methyl} -3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide;TMP269;-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide;BenzaMide, N-[[tetrahydro-4-(4-phenyl-2-thiazolyl)-2H-pyran-4-yl]Methyl]-3-[5-(trifluoroMethyl)-1,2,4-oxadiazol-3-yl]-;TMP-269;N-((4-(4-Phenylthiazol-2-yl)tetrahydro-2H-pyran-4-yl)methyl)-3-(5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl)benzamide;TMP 269;N-{[4-(4-phenyl-1,3-thiazol-2-yl)oxan-4-yl]methyl}-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benzamide;C25H21F3N4O3S;N-{[4-(4-Phenyl-1,3-Thiazol-2-Yl)tetrahydro-2h-Pyran-4-Yl]methyl}-3-[5-(Trifluoromethyl)-1,2,4-Oxadiazol-3-Yl]benzamide;TMFO1;compound 1 [PMID: 23524983];BenzaMide, N-[[tetrahydro-4-(4-phenyl-2-thiazolyl)-2H-pyran-4-;N-[[4-(4-Phenyl-1,3-thiazol-2-yl)oxan-4-yl]methyl]-3-[5-(trifluoromethyl)-1,2,4-oxadiazol-3-yl]benza
Cas No.	1314890-29-3
分子式	C₂₅H₂₁F₃N₄O₃S
分子量	514.52
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情	TMP269 是一种有效的，选择性的脱乙酰化酶 (HDAC) 抑制剂，能够抑制 HDAC 4/HDAC 5/HDAC 7/HDAC 9，IC₅₀ 值分别为 157 nM，97 nM，43 nM 和 23 nM。
生物活性	TMP269 is a novel and selective class IIa histone deacetylase (HDAC) inhibitor with IC 50 s of 157 nM, 97 nM, 43 nM and 23 nM for HDAC4, HDAC5, HDAC7 and HDAC9, respectively.
性状	Solid
IC50 & Target[1][2]	HDAC9 23 nM (IC50) HDAC7 43 nM (IC50
体外研究(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. 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. As with HDAC4 knockdown, TMP269 significantly enhances cytotoxicity induced by CFZ in MM cell lines, upregulating ATF4 and CHOP and inducing apoptosis. TMP269 does not hyperacetylate histone H3K9 or α-tubulin in MM cell lines, confirming that it has no inhibitory effects on class I or IIb HDACs. In a dosedependent manner, TPM269-induced cytotoxicity is associated with cleavage of caspase-8, -9, -3 and PARP, consistent with apoptosis. has not independe
体内研究(In Vivo)	In vivo angiogenesis assay, MDA-MB-231 cells are mixed with growth factor-reduced Matrigel and implanted subcutaneously into the flanks of nude mice. TMP269 (subcutaneous injection; 15 mg/kg; every other day; 10 days) shows an obvious antiangiogenic effect with 76% inhibition of angiogenesis in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Lobera M, et al. Selective class IIa histone deacetylase inhibition via a nonchelating zinc-binding group. Nat Chem Biol. 2013 May;9(5):319-25. [2]. Sinnett-Smith J, et al. Protein kinase D1 mediates class IIa histone deacetylase phosphorylation and nuclear extrusion in intestinal epithelial cells: role in mitogenic signaling. Am J Physiol Cell Physiol. 2014 May 15;306(10):C961-71.

溶解度数据	In Vitro: DMSO : 100 mg/mL (194.36 mM; Need ultrasonic)配制储备液

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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