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KSQ 4279

Cat. No. 7746 Submit a Review Datasheet / COA / SDS
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Description: Potent and selective USP1 allosteric inhibitor
Alternative Names: Ubiquitin-specific Protease 1 Inhibitor 1,USP1-IN-1,USP1 Inhibitor 1,RO7623066
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
Purity: ≥98% (HPLC)
Datasheet
Citations
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Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for KSQ 4279

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.

Technical Data for KSQ 4279

M. Wt 534.54
Formula C27H25F3N8O
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for KSQ 4279

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 53.45 100
ethanol 53.45 100

Preparing Stock Solutions for KSQ 4279

The following data is based on the product molecular weight 534.54. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.35 mL 18.71 mL
5 mM 0.37 mL 1.87 mL 3.74 mL
10 mM 0.19 mL 0.94 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

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References for KSQ 4279

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

Nusawardhana et al (2024) USP1-dependent nucleolytic expansion of PRIMPOL-generated nascent DNA strand discontinuities during replication stress. Nucleic Acids Research 52 2340 PMID: 38180818

Li et al (2024) Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7(8H)-one derivatives as potent USP1 inhibitors. Eur.J.Med.Chem. 275 116568 PMID: 38889606

Cadzow et al (2024) The USP1 inhibitor KSQ-4279 overcomes PARP inhibitor resistance in homologous recombination-deficient tumors. Cancer Res. 84 3419 PMID: 39402989

If you know of a relevant reference for KSQ 4279, please let us know.

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Citations for KSQ 4279

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