1. Cell Cycle/DNA Damage
  2. Deubiquitinase
  3. SJB2-043

SJB2-043 

Cat. No.: HY-15757 Purity: 99.25%
Handling Instructions

SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.

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

SJB2-043 Chemical Structure

SJB2-043 Chemical Structure

CAS No. : 63388-44-3

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 308 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 308 In-stock
Estimated Time of Arrival: December 31
Solid
5 mg USD 280 In-stock
Estimated Time of Arrival: December 31
10 mg USD 426 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1009 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1680 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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Based on 1 publication(s) in Google Scholar

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Description

SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.

IC50 & Target

IC50: 544 nM (USP1/UAF1)[1]

In Vitro

SJB2-043 causes a dose-dependent decrease in ubiquitin-specific protease 1 (USP1) levels and a concomitant degradation of inhibitor of DNA-binding-1 (ID1) protein in the K562 cells at a micromolar drug concentration. SJB2-043 also causes a decrease in the levels of other ID proteins, namely ID2 and ID3 in K562 cells. SJB2-043 causes a dose-dependent decrease in the number of viable K562 cells, with an EC50 of approximately 1.07 μM. Moreover, SJB2-043 induces apoptosis of K562 cells in a dose-dependent manner[1].

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

Molecular Weight

275.26

Formula

C₁₇H₉NO₃

CAS No.
SMILES

O=C1C2=C(N=C(C3=CC=CC=C3)O2)C(C4=CC=CC=C41)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 3.33 mg/mL (12.10 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6329 mL 18.1646 mL 36.3293 mL
5 mM 0.7266 mL 3.6329 mL 7.2659 mL
10 mM 0.3633 mL 1.8165 mL 3.6329 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Kinase Assay
[1]

The in vitro enzymatic assays are performed using ubiquitin-AMC (Ub-7-amido-4methylcoumarin) as a substrate in a reaction buffer containing 20 mM HEPES-KOH (pH 7.8), 20 mM NaCl, 0.1 mg/mL ovalbumin, 0.5 mM EDTA and 10 mM dithiothreitol. The fluorescence is measured by FluoStar Galaxy Fluorometer. For the Ub-vinylsulfone (VS) assay, the proteins are incubated with Ub-VS at 0.5 μM final concentration for 45 min at 30°C, followed by the immunoblotting analysis[1].

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

Cell Assay
[1]

Leukemic cell lines are grown in RPMI 1640 medium supplemented with 10% fetal bovine serum and penicillin/streptomycin. Hela cells and U2OS cells are grown in DMEM supplemented with 10% fetal bovine serum and penicillin/streptomycin. USP1 inhibitor C527 and its derivatives (e.g., SJB2-043) are synthesized and the purity is validated by high-performance liquid chromatography. Primary human AML patient samples are collected from DFCI leukemia program under the approval of appropriate protocols. Cells are treated with DMSO or USP1 inhibitors (e.g., SJB2-043) in appropriate medium for 24-72 hrs. The viable cell counts are determined using Trypan blue staining, Cell TiterGlo reagent or MTT assay. The apoptotic cells are detected using AnnexinV and 7AAD staining using flow cytometry. For Benzidine staining, the cells are washed twice with PBS and resuspended in 45 μL of PBS + 5 μL of Benzidine stain solution (0.2% in 0.5 M glacial acetic acid, 3% H2O2). After 45 min incubation at room temperature, the Benzidine positive cells are detected by light microscopy[1].

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

References
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Keywords:

SJB2-043DeubiquitinaseDUBsInhibitorinhibitorinhibit

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Product Name:
SJB2-043
Cat. No.:
HY-15757
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