WS-383 是高效、选择性、可逆的DCN1-UBC12相互作用抑制剂，IC50为11 nM。它抑制 Cul3/1 的类泛素化修饰，引起 Nrf2，p21和p27 的积累。

WS-383 is a selective, potent and reversible DCN1-UBC12 interaction inhibitor(IC50 of 11 nM).

WS-383 (10 μM) 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.

2247544-02-9

C18H21Cl2N9S2

498.46

DMSO:7.35 mg/mL (14.75 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years