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

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

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SJB2-043

SJB2-043 Estructura química

No. CAS : 63388-44-3

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Based on 4 publication(s) in Google Scholar

SJB2-043 Related Antibodies

Top Publications Citing Use of Products

Ver todos los productos específicos de isoformas Deubiquitinase:

Ver todas las isoformas
USP1 USP2 USP4 USP7 USP8 USP10 USP21 USP30 UCHL1 USP11 USP15

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Descripciòn

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].

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

SJB2-043 Related Antibodies
Peso molecular

275.26

Fòrmula

C17H9NO3
No. CAS
Appearance

Solid

Color

Green to dark green

SMILES

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

Room temperature in continental US; may vary elsewhere.
Almacenamiento
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvente y solubilidad
In Vitro: 

DMSO : 3.33 mg/mL (12.10 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 3.6329 mL 18.1646 mL 36.3293 mL
5 mM 0.7266 mL 3.6329 mL 7.2659 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Pureza y Documentación
Referencias
Ensayo de quinasas
[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Ensayo celular
[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 no ha confirmado la precisión de estos métodos independientemente. Son solo para referencia.
Referencias

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6329 mL 18.1646 mL 36.3293 mL 90.8232 mL
5 mM 0.7266 mL 3.6329 mL 7.2659 mL 18.1646 mL
10 mM 0.3633 mL 1.8165 mL 3.6329 mL 9.0823 mL
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SJB2-043 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

SJB2-04363388-44-3DeubiquitinaseDUBsInhibitorinhibitorinhibit

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Nombre del producto:
SJB2-043
Cat. No.:
HY-15757
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