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  5. R&D Systems™ KSQ 4279

R&D Systems™ KSQ 4279
SDP

Catalog No. RD10188019 Shop All Novus Products
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RD10188019 10 mg
RD10187995 50 mg
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Catalog No. RD10188019 Supplier R&D Systems™ Supplier No. 7746/10

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Description

A Tocris product, part of R&D Systems. Potent and selective USP1 allosteric inhibitor

KSQ 4279 is a potent and selective allosteric inhibitor of the ubiquitin specific protease 1 (USP1) (IC50 = 11 nM; Ki = 1.2 nM), a key regulator of DNA damage repair pathway (distinct from PARP inhibitors). It displays selectivity for USP1 over other USP, UCH and OTU enzymes.

KSQ 4279 has strong antiproliferation effects in vitro. It induces accumulation of mono-ubiquitinated substrates in MDA-MB-436 cells.

In vivo, KSQ 4279 induces anti-tumor response in the BRCA1 mutant ovarian PDX model (mouse). It also displays synergistic effects with PARP inhibitor Olaparib (Cat. No. 7579) leading to significant and durable anti-tumor response in mice. KSQ 4279 is orally bioavailable.

Specifications

Chemical Name or Material 6-(4-Cyclopropyl-6-methoxypyrimidin-5-yl)-1-(4-(1-isopropyl-4-(trifluoromethyl)-1H-imidazol-2-yl)benzyl)-1H-pyrazolo[3,4-d]pyrimidine
CAS 2446480-97-1
Quantity 10 mg
Product Line Tocris
Target Deubiquitinating Enzyme Inhibitors
Molecular Formula C27H25F3N8O
Purity 98%
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