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CAS No. : 1316215-12-9
MCE 国际站:Citarinostat
产品活性:Citarinostat (ACY241) 是第二代有效的,口服活性,高选择性的 HDAC6 抑制剂,IC50 为 2.6 nM (HDAC1,HDAC2,HDAC3 和 HDAC8 的 IC50 分别为 35 nM,45 nM,46 nM 和 137 nM)。Citarinostat 具有抗癌作用。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:HDAC
In Vitro: Citarinostat (ACY241; 0-3 μM; 24 hours; A2780 cells) treatment with 300 nM results in increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. In contrast, hyperacetylation of histone H3, a target of Class I HDACs, is only observed at doses above 1 μM. Low exposures of Citarinostat result in selective inhibition of HDAC6, while higher exposures lead to inhibition of Class I HDAC isozymes.
The single agent viability IC50 of Citarinostat (ACY241) ranged from 4.6-6.1 μM in A2780 and TOV-21G ovarian cancer and MDA-MD-231 breast cancer cells. Consistent with the viability assay, single agent Citarinostat modestly reduces proliferation at doses up to 3 μM without inducing apoptosis, while 10 μM of Citarinostat causes significant induction of apoptosis and completely suppresses proliferation.
In Vivo: Citarinostat (ACY241; 50 mg/kg; intraperitoneal injection; once daily for five days, followed by two days off; for 3 weeks; female athymic nude mice) significantly suppresses tumor growth in combination with NSC 125973.
相关产品:Clinical Compound Library Plus | Bioactive Compound Library Plus | Cell Cycle/DNA Damage Compound Library | Epigenetics Compound Library | Histone Modification Research Compound Library | Anti-Cancer Compound Library | Clinical Compound Library | Anti-Aging Compound Library | Reprogramming Compound Library | Oxygen Sensing Compound Library | Orally Active Compound Library | Anti-Breast Cancer Compound Library | Anti-Pancreatic Cancer Compound Library | Anti-Blood Cancer Compound Library | Anti-Liver Cancer Compound Library | Anti-Pulmonary Fibrosis 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
热门产品线:重组蛋白 | 化合物库 | 天然产物 | 荧光染料 | PROTAC | 同位素标记物 | 寡核苷酸 | 抗体 | 点击化学
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货号: HY-15994
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