Chemical Structure : TAS1440
CAS No.:
2098585-77-2
TAS1440
(TAS-1440)
Catalog No.: 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.
Bulk size, bulk discount!
E-mail: sales@probechem.com
Tech Support: tech@probechem.com
Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
|
M.Wt
|
475.54
|
|
Formula
|
C28H27F2N3O2
|
|
Appearance
|
Solid
|
|
CAS No.
|
|
|
Storage
|
- Solide Powder
-
-20°C 12 Months; 4°C 6 Months
|
- In Solvent
-
-80°C 6 Months; -20°C 6 Months
|
|
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
|
References
1. Machida T, et al. Nat Commun. 2026 Mar 25. doi: 10.1038/s41467-026-70984-1.
Contact Us
sales@probechem.com
