Company Name: |
Shanghai Rechem science Co., Ltd.
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Tel: |
21-31433387 15618786686 |
Email: |
sales@rechemscience.com |
Products Intro: |
Product Name:WS-383 hydrochloride CAS:2247544-02-9 Purity:0.98 Package:100mg;500mg;1g
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Company Name: |
ChemeGen(Shanghai) Biotechnology Co.,Ltd.
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Tel: |
18818260767 |
Email: |
sales@chemegen.com |
Products Intro: |
Product Name:WS-383 CAS:2247544-02-9 Purity:98% Package:10 mg;50 mg;100 mg;500 mg;1 g;5 g;10 g
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Product Name: | WS-383 | Synonyms: | WS-383 hydrochloride;WS-383;Ubiquitin conjugating enzyme,DCN1-UBC12,WS-383,E1 activating enzyme,WS 383,E3 ligating enzyme,WS383,interaction,KYSE70,E2 conjugating enzyme,cell,Ubiquitin ligase,E1/E2/E3 Enzyme,MGC-803,Inhibitor,Ubiquitin activating enzyme,inhibit | CAS: | 2247544-02-9 | MF: | C18H21Cl2N9S2 | MW: | 498.45 | EINECS: | | Product Categories: | | Mol File: | 2247544-02-9.mol | |
| WS-383 Chemical Properties |
storage temp. | 4°C, away from moisture and light | solubility | DMSO : 7.35 mg/mL (14.75 mM; Need ultrasonic) |
| WS-383 Usage And Synthesis |
Biological Activity | WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2[1].
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[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]. | storage | Store at -20°C | 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. |
| WS-383 Preparation Products And Raw materials |
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