KSQ 4279

Tocris Bioscience | Catalog # 7746

Potent and selective USP1 allosteric inhibitor
Tocris Bioscience

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
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

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.

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

Calculators

Calculate the mass, volume, or concentration required for a solution.

=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Calculate the dilution required to prepare a stock solution.

x
=
x

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Background References

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

Product Documents for KSQ 4279

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for KSQ 4279

For research use only

Related Research Areas

Deubiquitinating Enzymes (DUBs)

Customer Reviews for KSQ 4279

There are currently no reviews for this product. Be the first to review KSQ 4279 and earn rewards!

Have you used KSQ 4279?

Submit a review and receive an Amazon gift card!

$25/€18/£15/$25CAN/¥2500 Yen for a review with an image

$10/€7/£6/$10CAN/¥1110 Yen for a review without an image

Submit a review
Amazon Gift Card