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CAS No. : 1314890-29-3
MCE 国际站:TMP269
产品活性: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。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:HDAC
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.
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.
相关产品:Covalent Screening Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Anti-Aging Compound Library | Covalent Screening Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Endoplasmic Reticulum Stress Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Targeted Diversity Library | Anti-Liver Cancer Compound Library | Osteogenesis Compound Library | Heterocyclic Compound Library | Highly Selective Inhibitors Library | YF479 | KD 5170 | HDAC-IN-48 | Remetinostat | HDAC-IN-30 | HDAC-IN-52 | CG347B | Psammaplin A | JPS016 | HDAC6-IN-9 | Splitomicin | TNG260 | Tacedinaline | G4/HDAC-IN-1 | HPOB | Tubacin | HDAC-IN-37 | Vorinostat-d5 | Resminostat | MAO A/HDAC-IN-1 | NCC-149 | Tubulin/HDAC-IN-1 | PI3K/HDAC-IN-1 | HDAC1-IN-4 | HDAC6/HSP90-IN-1 | Entinostat-d4 | UF010 | MOCPAC | Ivaltinostat | HDAC-IN-56
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