WS-383 free base
WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
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- CAS No.: 2247543-65-1
- Formule: C18H20ClN9S2
- Masse moléculaire:461.99
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
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Activité biologique
Description
IC50 & Target
IC50: 11 nM (DCN1–UBC12 interaction)[1]
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| BGC-823 | IC50 |
1 μM
Compound: 5
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Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human BGC-823 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38401457] |
| MGC-803 | IC50 |
0.53 μM
Compound: 5
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Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human MGC-803 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38401457] |
| SGC-7901 | IC50 |
0.85 μM
Compound: 5
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Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
Antiproliferative activity against human SGC-7901 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
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[PMID: 38401457] |
In Vitro
WS-383 (10 μM) is against a panel of kinases such as BTK, CDKs, and EGFR [L858R] using staurosporine and afatinib as the positive controls. WS-383 showed weak inhibitory activity at 10.0 μM,it is selective to the DCN1–UBC12 interaction over the selected kinasesr[1]. WS-383 (0.03-3 μM;24 hours) blocks Cul3 neddylation at 3 μM and also has certain inhibition of Cul1 neddylation at 10 μM but was not effective in inhibiting neddylation of other cullin members[1]. WS-383 (0.03-3 μM;24 hours) increases Cul1, Skp1 (adaptor protein), F-box protein, and RBX1/RBX2 RING protein form SCF E3 complex. Cyclin dependent kinase inhibitor 1A (p21) and cyclin dependent kinase inhibitor 1B (p27) expression in a dose-dependent manner in MGC-803 and KYSE70 manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MGC-803 cells
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Concentration:0.03 μM; 0.3 μM; 3 μM; 10 μM
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Incubation Time:24 hours
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Result:Decreased N8-Cul1 and N8-Cul2 protein expression.
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Cell Line:MGC-803 and KYSE70 cells
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Concentration:0.03 μM; 0.3 μM; 3 μM; 10 μM
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Incubation Time:24 hours
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Result:Induced accumulation of p21, p27, and NRF2 in MGC-803 cells.
Chemical Information
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CAS No. 2247543-65-1
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Masse moléculaire 461.99
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Formule C18H20ClN9S2
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SMILES
CN(C)CCN1N=NN=C1SC2=CC(C)=NC3=NC(SCC4=CC=C(Cl)C=C4)=NN23
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
WS-383 free base Related Classifications
HY-126075 Related Classifications
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