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货期:询盘
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MedChemExpress LLC
- CAS号:
2421122-61-2
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询盘
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HDAC-IN-45
CAS No. : 2421122-61-2
MCE 国际站:HDAC-IN-45
产品活性:HDAC-IN -45 (Compound 14) 是一种小分子 HDAC 抑制剂,具有抗癌活性,也可与 Y303 残基形成氢键。HDAC-IN-45 (Compound 14) 对 HDAC1、2 和 3 亚型具有显著的抑制作用, IC50 分别为 0.108、0.585 和 0.563 μM。
研究领域:Cell Cycle/DNA Damage | Epigenetics
作用靶点:HDAC
In Vitro: HDAC-IN-45 (Compound 14) suppresses the growth of triple-negative breast cancer cells MDA-MB-231 (IC50 = 1.48 μM), MDA-MB-468 (IC50= 0.65 μM), and liver cancer cells HepG2 (IC50= 2.44 μM).
HDAC-IN-45 has equally virulent in the HDAC-sensitive cell lines (YCC11) and -resistant gastric cell lines (YCC3/7) and overcome HDACi resistance. HDAC-IN-45 has a high toxicity (IC50= 0.33 μM) in three leukemic cell lines, K-562, KG-1 and THP-1.
HDAC-IN-45 (Compound 14) has substantial inhibitory effects towards HDAC1, 2 and 3 isoforms with IC50 values of 0.108, 0.585 and 0.563 μM respectively.
HDAC-IN-45 (Compound 14) can elevate acetylation level of histone H3 and expression of p21.
HDAC-IN-45 (Compound 14) exerts a dose-dependent upregulation of ac-H3K9 in MDA-MB-231 cells, triggers cell cycle arrest in G1 phase.
HDAC-IN-45 (Compound 14) exhibits a potent antitumor efficacy in xenograft mouse model.
In Vivo: HDAC-IN-45 (Compound 14) (25 mg/kg or 50mg/kg; i.p.; every day) exhibits a potent antitumor efficacy in human MDA-MB-231 breast cancer xenograft mouse model.
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