WS-383 - 10mM in DMSO , CAS No.2247544-02-9

CAS: 2247544-02-9 Cat. No.: W655629 Summenformel: C₁₈H₂₁Cl₂N₉S₂ Molekulargewicht: 498.46 PubChem CID: 138319703

GRADE & PURITY 10mM in DMSO

Storage

Protected from light,Desiccated,Store at -80°C

Shipped In

Dry ice packs + Cold packs

Übersicht

WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC 50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2

In Vitro

WS-383 (10 μM) is against a panel of kinases such as BTK, CDKs, and EGFR [L858R] using staurosporine and BIBW 2992 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. 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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: MGC-803 cells Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM Incubation Time: 24 hours Result: Decreased N8-Cul1 and N8-Cul2 protein expression. Western Blot AnalysisCell Line: MGC-803 and KYSE70 cells Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM Incubation Time: 24 hours Result: Induced accumulation of p21, p27, and NRF2 in MGC-803 cells.

IC50& Target:IC50: 11 nM (DCN1-UBC12 interaction)

Specifications

Spezifikationen & Reinheit

10mM in DMSO

Biochemische und physiologische Mechanismen

WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC 50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.

Storage

Protected from light,Desiccated,Store at -80°C

Verschickt in

Dry ice packs + Cold packs

Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.

Namen und Kennungen

• PubChem CID: 138319703
• Molekulargewicht: 498.46