FX-171-C

Chemical Structure : FX-171-C

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货号: PC-23076Not For Human Use, Lab Use Only.

FX-171-C is a specific, small molecule inhibitor Zn2+-dependent JAMM/MPN deubiquitylase (DUB) BRCC36 isopeptidase complex (BRISC) with IC50 of 1.4 uM.

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生物&药学活性

FX-171-C is a specific, small molecule inhibitor Zn2+-dependent JAMM/MPN deubiquitylase (DUB) BRCC36 isopeptidase complex (BRISC) with IC50 of 1.4 uM.
FX-171-C does not inhibit AMSH* (a STAM2 AMSH fusion), the nuclear ARISC complex, UPS2, and BRCC36 Abraxas2 complex.
FX-171-C inhibits BRISC-mediated cleavage of polyubiquitin chains.
FX-171-C acts as molecular glue, stabilises two BRISC octamers to form a BRISC dimer with 16 subunits.
BRCC36 W130A and L169A/R/W mutants showed severely reduced inhibition by FX-171-C (>100 fold over WT complex), whilst BRCC36 R167A remained inhibitor
sensitive.
FX-171-C (2.5 uM) reduces interferon-stimulated gene (ISG) expression in cells MCF10A Cas9 cells expressing BRCC45 wild-type (WT), and in healthy and SSc PBMCs.
BRCC36 is a JAMM (JAB1, MOV34, and MPR1, Pad1 N-terminal (MPN)) metalloenzyme DUB family and selectively cleaves lysine 63-linked ubiquitin (K63-Ub) chains.
BRCC36 is present in two distinct macromolecular assemblies: a cytoplasmic BRCC36 isopeptidase complex (BRISC), and the nuclear Abraxas1 isopeptidase complex (ARISC).
The BRISC complex regulates Type I interferon signalling by deubiquitylating and stabilising Type I interferon (IFNAR1) receptors, whilst the ARISC complex interacts with the tumour suppressor protein BRCA1 and localises to double-stranded DNA breaks to facilitate DNA damage repair.

物理化学性质&存储条件

分子量	553.22
分子式	C23H17Cl4N5O3
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	N-(3-azabicyclo[3.1.0]hexan-6-yl)-4-(2,6-dichlorobenzamido)-1-(2,6-dichlorobenzoyl)-1H-pyrazole-3-carboxamide

参考文献

1. Chandler F, et al. bioRxiv. 2024 Sep 7:2024.09.07.611787.

FX-171-C

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物理化学性质&存储条件

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FX-171-C

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物理化学性质&存储条件

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