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HDAC-IN-52

Names

[ CAS No. ]:
2075787-77-6

[ Name ]:
HDAC-IN-52

Biological Activity

[Description]:

HDAC-IN-52 is a pyridine-containing HDAC inhibitor, with IC50s of 0.189, 0.227, 0.440 and 0.446 μM for HDAC1, HDAC2, HDAC3, and HDAC10, respectively. HDAC-IN-52 can be used for the research of cancer[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> HDAC
Signaling Pathways >> Epigenetics >> HDAC

[Target]

hHDAC1:0.189 μM (IC50)

hHDAC2:0.227 μM (IC50)

hHDAC3:0.440 μM (IC50)

hHDAC10:0.446 μM (IC50)


[In Vitro]

HDAC-IN-52 (compound 8f) (72 hours) 抑制 HCT116,A549 和 K562 细胞的增殖,IC50 值分别为 0.43,1.28 和 0.37 μM[1 ]。 HDAC-IN-52 (1-5 μM; 24-48 h) 在 48 小时后显着诱导白血病 U937 细胞死亡,G1 前期阻滞分别为 76% 和 100%[1]。 HDAC-IN-52 (1-5 μM; 48 h) 增加 p21,BAX 和 BAK 的 mRNA 表达,下调细胞周期蛋白 D1 和 BCL-2[1]。

[References]

[1]. Bello ED, et, al. Novel pyridine-containing histone deacetylase inhibitors strongly arrest proliferation, induce apoptosis and modulate miRNAs in cancer cells. Eur J Med Chem. 2022 Dec 15;247:115022.  

Chemical & Physical Properties

[ Molecular Formula ]:
C24H20N4O2

[ Molecular Weight ]:
396.44

[ Storage condition ]:
-20°C


Related Compounds

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