WS-383 hydrochloride

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

WS-383 盐酸盐 (WS383) 是一种高效、选择性和细胞活性的 DCN1-UBC12 相互作用抑制剂，IC50 为 11 nM。

WS-383 hydrochloride (WS383) is a highly potent, selective, and cellular active inhibitor of DCN1-UBC12 interaction with IC50 of 11 nM; inhibits Cul3/1 neddylation selectively over other cullins and also induces accumulation of p21, p27 and NRF2; exhibits cellular target engagement to DCN1 in MGC-803 cells, enhances the thermal stability of cellular DCN1 protein even at 1 uM.

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. Western Blot Analysis Cell 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 Analysis Cell 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.

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WS383 | WS 383

Proteasome/Ubiquitin

E2

E2

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2247544-02-9

498.449

C18H21Cl2N9S2

>98% (HPLC)

In Vitro:?DMSO : 7.35 mg/mL (14.75 mM)

CN(C)CCN1N=NN=C1SC2=CC(C)=NC3=NC(SCC4=CC=C(Cl)C=C4)=NN23.Cl

2-(5-((2-((4-Chlorobenzyl)thio)-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl)thio )-1H-tetrazol-1-yl)-N,N-dimethylethan-1-amine hydrochloride

(-20℃)

With Ice Pack

≥ 2 years