KSQ 4279

Tocris Bioscience | Catalog # 7746

Potent and selective USP1 allosteric inhibitor
Tocris Bioscience

Key Product Details

Description

Potent and selective USP1 allosteric inhibitor
View all Deubiquitinating Enzyme Inhibitors »

Product Description

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.

Product Specifications for KSQ 4279

Formula

C27H25F3N8O

Storage

Store at -20°C

Purity

≥98% (HPLC)

Chemical Name

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 Number

2446480-97-1

PubChem ID

150782011

InChI Key

KCBWAFJCKVKYHO-UHFFFAOYSA-N

SMILES

FC(F)(C1=CN(C(C)C)C(C2=CC=C(CN3N=CC4=C3N=C(C5=C(C6CC6)N=CN=C5OC)N=C4)C=C2)=N1)F

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Solubility Soluble to 53.45mg/ml in DMSO and to 53.45mg/ml in Ethanol

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Background References

References are publications that support the biological activity of the product.

There are currently no references for this product.

Product Documents for KSQ 4279

Certificate of Analysis

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Product Specific Notices for KSQ 4279

For research use only

Related Research Areas

Deubiquitinating Enzymes (DUBs)

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