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  5. Tocris BioScience™ KSQ 4279

Tocris BioScience™ KSQ 4279

Produktkod. 31900345
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Produktkod. Kvantitet
31900345 50 mg
31900340 10 mg
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Produktkod. 31900345 Leverantör Tocris BioScience™ Leverantörsnummer 7746/50

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Beskrivning

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.

TRUSTED_SUSTAINABILITY

Specifikationer

Kemiskt namn eller 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
Kvantitet 50 mg
Mål Deubiquitinating Enzyme Inhibitors
Molekylformel C27H25F3N8O
Renhet 98%
Produkttitel
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