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首页-小分子抑制剂&激动剂-Epigenetics-Histone Demethylase-DC551040
DC551040

Chemical Structure : DC551040

CAS No.: 2133291-32-2

DC551040 (DC-551040)

货号: PC-26436Not For Human Use, Lab Use Only.

DC551040 is a potent, selective, irreversible and orally bioavailable LSD1 (KDM1A) inhibitor with IC50 of 2.14 nM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DC551040 is a potent, selective, irreversible and orally bioavailable LSD1 (KDM1A) inhibitor with IC50 of 2.14 nM.
DC551040 exhibits excellent selectivity on LSD1 over LSD2 and MAO.
DC551040 interacts covalently with LSD1, occupies the catalytic site of LSD1.
DC551040 displays significant potency in inhibiting antiproliferative activities in several AML cell lines, including MV-4-11 (IC50 = 79.51 nM), Kasumi-1 (IC50 = 25.77 nM), and HL60 (IC50 = 40.35 nM), while shows weak inhibitory activity against non-AML cell lines, with an IC50 value over 20 uM.
DC551040 shows inhibitory effects in AML patient-derived cells.
DC551040 exhibits a significant anticancer effect on cell differentiation in leukemic MV-4-11 cells, decreases level of H3K4me2 in MV-4-11 cells.
DC551040 (2 mg/kg, 10 mg/kg, oral) demonstrates antitumor effect in Kasumi-1 and MV-4-11 xenograft model.

物理化学性质&存储条件

分子量 389.52
分子式 C22H32FN3O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

piperidin-4-ylmethyl 4-fluoro-4-((((1R,2S)-2-phenylcyclopropyl)amino)methyl)piperidine-1-carboxylate

参考文献

1. Wang J, et al. Signal Transduct Target Ther. 2026 Mar 23;11(1):108.

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