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首页-小分子抑制剂&激动剂-Epigenetics-Histone Methyltransferase (HMTase)-FCD-11
FCD-11

Chemical Structure : FCD-11

CAS No.: 881490-99-9

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FCD-11 (FCD11)

货号: PC-27770Not For Human Use, Lab Use Only.

FCD-11 is a first-in-class, selective small molecule inhibitor of histone methyltransferases COMPASS (Complex of proteins associated with Set1), specifically inhibits the H3K4me3 activity of SET1A/COMPASS and MLL1/COMPASS with IC50 of 1.32 uM and 3.26 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

FCD-11 is a first-in-class, selective small molecule inhibitor of histone methyltransferases COMPASS (Complex of proteins associated with Set1), specifically inhibits the H3K4me3 activity of SET1A/COMPASS and MLL1/COMPASS with IC50 of 1.32 uM and 3.26 uM.
FCD-11 shows no activity against DOT1L, G9a, PRDM9, and SETDB1.
FCD-11 potently inhibits SET1A/COMPASS-mediated H3K4me3 activity with IC50 of 0.46 uM in in vitro methylation assays, weakly affects SET1B and MLL3 activities.
FCD-11 inhibits MLL4-mediated H3K4me1 activity and MLL1-mediated H3K4me3 activity, with an IC50 of approximately 0.85 uM for MLL1.
FCD-11 disrupts the ASH2L-RBBP5 interaction, which is correlated with SET1A/COMPASS HMTase inhibition.
FCD-11 resembles genetic loss of catalytic SET1A/COMPASS activity in mESCs.
FCD-11 inhibits breast cancer cell viability, diminishes SET1A/COMPASS deposited H3K4me3 peaks, and impairs in vivo tumor growth.

物理化学性质&存储条件

分子量 490.49
分子式 C25H18N2O7S
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

Benzoic acid, 4-[[4-[[(4-carboxyphenyl)sulfonyl]imino]-1,4-dihydro-1-oxo-2-naphthalenyl]amino]-, 1-methyl ester

参考文献

1. Zhao Z, et al. bioRxiv [Preprint]. 2026 Jul 31:2026.07.30.741768.

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