KSQ 4279 New
Tocris Bioscience, part of Bio-Techne | Catalog # 7746
Potent and selective USP1 allosteric inhibitor
Key Product Details
Description
Potent and selective USP1 allosteric inhibitor
Alternative Names
Ubiquitin-specific Protease 1 Inhibitor 1,USP1-IN-1,USP1 Inhibitor 1,RO7623066
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
Molecular Weight
534.54
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
| 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 all affect the solvent volumes required to prepare stock solutions.
| 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 |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Li Design, synthesis, and biological evaluation of pyrido[2,3-d]pyrimidin-7(8H)-one derivatives as potent USP1 inhibitors. Eur.J.Med.Chem. 2024 PMID: 38889606
- Cadzow The USP1 inhibitor KSQ-4279 overcomes PARP inhibitor resistance in homologous recombination-deficient tumors. Cancer Res. 2024 PMID: 39402989
- Nusawardhana USP1-dependent nucleolytic expansion of PRIMPOL-generated nascent DNA strand discontinuities during replication stress. Nucleic Acids Research 2024 PMID: 38180818
Product Specific Notices for KSQ 4279
For research use only
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