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Citarinostat
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Citarinostat
CAS No. : 1316215-12-9
MCE 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 | Trichostatin A | 4-Phenylbutyric acid | Valproic acid | Entinostat | Sulforaphane | Romidepsin | RGFP966 | Tasquinimod | Corin | Tacedinaline | Dacinostat | ITSA-1 | SIS17 | Tubastatin A Hydrochloride | WT-161 | Givinostat hydrochloride monohydrate | Pyroxamide | BRD-6929 | Bufexamac | HDAC8-IN-1 | Scriptaid | Sinapinic acid | Apicidin | BML-210 | M344 | Droxinostat | HDACs/mTOR Inhibitor 1 | CG347B
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