TAS1440 | LSD1 inhibitor | Probechem Biochemicals

Chemical Structure : TAS1440

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TAS1440 (TAS-1440)

货号: PC-26423Not For Human Use, Lab Use Only.

TAS1440 (TAS-1440) is a potent, selectve, histone H3-competitive non-covalent LSD1 inhibitor with IC50 of 4.8 nM, disrupts INSM1-LSD1 complex activating tumor-suppressive pathways.

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生物&药学活性

TAS1440 (TAS-1440) is a potent, selectve, histone H3-competitive non-covalent LSD1 inhibitor with IC50 of 4.8 nM, disrupts INSM1-LSD1 complex activating tumor-suppressive pathways.
TAS1440 shows high selectivity over related amine oxidases (LSD2, MAO‑A, MAO‑B; all IC50> 10,000 nM) and a broader panel of epigenetic enzymes (e.g., JARID1A, DNMT1, EZH1/EED/SUZ12, HDAC1, JMJD2B/3, PRMT4).
TAS1440 engages the H3‑binding pocket of LSD1.
TAS1440 induces a coordinated reprogramming of gene expression (INSM1 and SMAD2) characterized by activation of NOTCH/TGF‑β pathways and suppression of the neuroendocrine program in SCLC‑A.
TAS1440 suppressed proliferation in INSM1/ASCL1-high SCLC-A cells and induced tumor regression in xenografts.

物理化学性质&存储条件

分子量	475.54
分子式	C28H27F2N3O2
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	(S)-5'-(3-aminopyrrolidine-1-carbonyl)-2'',3-difluoro-4''-(2-hydroxy-2-methylpropyl)-[1,1':2',1''-terphenyl]-4-carbonitrile

参考文献

1. Machida T, et al. Nat Commun. 2026 Mar 25. doi: 10.1038/s41467-026-70984-1.

TAS1440 (TAS-1440)

生物&药学活性

物理化学性质&存储条件

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TAS1440 (TAS-1440)

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