Top Suppliers:I want be here
  • DC Chemicals Limited
  • China
  • Product Name: WS-383
  • Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
  • Purity: 98.0%
  • Stocking Period: 3 Day
  • Contact: Tony Cao
Related CAS#:
2247543-65-1 2247544-02-9
912288-64-3 682730-74-1
145903-06-6 760944-56-7
760162-85-4 2271358-64-4
223645-67-8 71079-08-8

2247543-65-1

2247543-65-1 structure
2247543-65-1 structure
  • Name: WS-383 free base
  • Chemical Name: WS-383
  • CAS Number: 2247543-65-1
  • Molecular Formula: C18H20ClN9S2
  • Molecular Weight: 461.991
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease E1/E2/E3 Enzyme
  • Create Date: 2020-01-11 18:36:51
  • Modify Date: 2024-04-07 20:38:28
  • WS-383 (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
Name WS-383
Description WS-383 (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
Related Catalog
Target

IC50: 11 nM (DCN1–UBC12 interaction)[1]
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]. Western Blot Analysis[1] 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[1] 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.
References

[1]. Wang S, et al. Development of Highly Potent, Selective, and Cellular Active Triazolo[1,5- a]pyrimidine-Based Inhibitors Targeting the DCN1-UBC12 Protein-Protein Interaction.J Med Chem. 2019 Mar 14;62(5):2772-2797.
Molecular Formula C18H20ClN9S2
Molecular Weight 461.991

Chemsrc provides CAS#:2247543-65-1 MSDS, density, melting point, boiling point, structure, formula, molecular weight, synthetic route, etc.
title: CAS No. 2247543-65-1 | Chemsrc address: https://www.chemsrc.com/en/baike/1561653.html

Home | MSDS/SDS Database Search | Journals | Product Classification | Biologically Active Compounds | Selling Leads | About Us | Disclaimer

Copyright © 2024 ChemSrc All Rights Reserved