Description
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma.
Product information
CAS Number: 2044953-70-8
Molecular Weight: 547.04
Formula: C21H27ClN4O7S2
Chemical Name: N'-[(1E)-1-(5-chloro-2-hydroxyphenyl)ethylidene]-3-[(4-methylpiperazin-1-yl)sulfonyl]benzohydrazide; methanesulfonic acid
Smiles: CS(O)(=O)=O.C/C(=N\NC(=O)C1=CC(=CC=C1)S(=O)(=O)N1CCN(C)CC1)/C1=CC(Cl)=CC=C1O
InChiKey: JIPBQMGGMHCGBW-CWUUNJJBSA-N
InChi: InChI=1S/C20H23ClN4O4S.CH4O3S/c1-14(18-13-16(21)6-7-19(18)26)22-23-20(27)15-4-3-5-17(12-15)30(28,29)25-10-8-24(2)9-11-25;1-5(2,3)4/h3-7,12-13,26H,8-11H2,1-2H3,(H,23,27);1H3,(H,2,3,4)/b22-14+;
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: To be determined
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
Seclidemstat (72 hours) mesylate inhibits SWI/SNF-mutation-dependent tumor cell proliferation with IC50 ranging from 0.013 to 2.819 μM (COV434, BIN67, SCCOHT-1, TOV21G, SKOV3, A427, H522, A549, H1299, G401, G402, HCC15 cells). Seclidemstat (72 hours) mesylate promotes endogenous retroviruses (ERVs) expression and activation of IFNβ pathway in SCCOHT cell lines (SCCOHT-1, BIN67, and COV434 cells). Seclidemstat (3 μM) mesylate promotes PD-L1 expression in SCCOHT COV 434 pIND 20 BRG1-2.7 cell line.
References:
- Soldi R, et al. The novel reversible LSD1 inhibitor SP-2577 promotes anti-tumor immunity in SWItch/Sucrose-NonFermentable (SWI/SNF) complex mutated ovarian cancer. PLoS One. 2020;15(7):e0235705. Published 2020 Jul 10.
- Dai XJ, et al. Reversible Lysine Specific Demethylase 1 (LSD1) Inhibitors: A Promising Wrench to Impair LSD1 [published correction appears in J Med Chem. 2021 May 13;64(9):6410-6411]. J Med Chem. 2021;64(5):2466-2488.
Products are for research use only. Not for human use.
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