1. Cell Cycle/DNA Damage Epigenetics
  2. Deubiquitinase PARP
  3. KSQ-4279

KSQ-4279 (USP1-IN-1) is a potent USP1 inhibitor and a selective PARP1 inhibitor. KSQ-4279 is promising for research of cancers.

For research use only. We do not sell to patients.

KSQ-4279 Chemical Structure

KSQ-4279 Chemical Structure

CAS No. : 2446480-97-1

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 894 In-stock
Solution
10 mM * 1 mL in DMSO USD 941 In-stock
Solid
1 mg USD 320 In-stock
5 mg USD 800 In-stock
10 mg USD 1280 In-stock
50 mg   Get quote  
100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of KSQ-4279:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE KSQ-4279

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

KSQ-4279 (USP1-IN-1) is a potent USP1 inhibitor and a selective PARP1 inhibitor. KSQ-4279 is promising for research of cancers[1].

IC50 & Target

USP1

 

PARP1

 

In Vitro

In BRCA1/2-mutated breast cancer cells, KSQ-4279 induces S-phase cell cycle arrest, marked accumulation of gamma-H2A histone family member X (ϒH2AX) and increases apoptosis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

KSQ-4279 shows dose-dependent, robust and durable anti-tumor regression in multiple TNBC and ovarian cancer Patient-derived xenografts (PDXs) with varied genomic status including BRCA1-mutated and -wildtype models[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
NCT NumberSponsorConditionStart DatePhase
NCT05240898KSQ Therapeutics, Inc.
Advanced Solid Tumors
August 16, 2021Phase 1
Molecular Weight

534.54

Formula

C27H25F3N8O

CAS No.
Appearance

Solid

Color

White to light yellow

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 80 mg/mL (149.66 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8708 mL 9.3538 mL 18.7077 mL
5 mM 0.3742 mL 1.8708 mL 3.7415 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2 mg/mL (3.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2 mg/mL (3.74 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, PEG300/PEG400, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Purity & Documentation

Purity: 99.95%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8708 mL 9.3538 mL 18.7077 mL 46.7692 mL
5 mM 0.3742 mL 1.8708 mL 3.7415 mL 9.3538 mL
10 mM 0.1871 mL 0.9354 mL 1.8708 mL 4.6769 mL
15 mM 0.1247 mL 0.6236 mL 1.2472 mL 3.1179 mL
20 mM 0.0935 mL 0.4677 mL 0.9354 mL 2.3385 mL
25 mM 0.0748 mL 0.3742 mL 0.7483 mL 1.8708 mL
30 mM 0.0624 mL 0.3118 mL 0.6236 mL 1.5590 mL
40 mM 0.0468 mL 0.2338 mL 0.4677 mL 1.1692 mL
50 mM 0.0374 mL 0.1871 mL 0.3742 mL 0.9354 mL
60 mM 0.0312 mL 0.1559 mL 0.3118 mL 0.7795 mL
80 mM 0.0234 mL 0.1169 mL 0.2338 mL 0.5846 mL
100 mM 0.0187 mL 0.0935 mL 0.1871 mL 0.4677 mL
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Product Name:
KSQ-4279
Cat. No.:
HY-145471
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