WS 383

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

Product information

CAS Number: 2247544-02-9

Molecular Weight: 498.46

Formula: C18H21Cl2N9S2

Synonym:

WS-383

WS383

Chemical Name: (2-{5-[(2-{[(4-chlorophenyl)methyl]sulfanyl}-5-methyl-[1, 2, 4]triazolo[1, 5-a]pyrimidin-7-yl)sulfanyl]-1H-1, 2, 3, 4-tetrazol-1-yl}ethyl)dimethylamine hydrochloride

Smiles: Cl.CN(C)CCN1N=NN=C1SC1=CC(C)=NC2=NC(=NN21)SCC1=CC=C(Cl)C=C1

InChiKey: LJZUAAKUJAXXHQ-UHFFFAOYSA-N

InChi: InChI=1S/C18H20ClN9S2.ClH/c1-12-10-15(30-18-22-24-25-27(18)9-8-26(2)3)28-16(20-12)21-17(23-28)29-11-13-4-6-14(19)7-5-13;/h4-7,10H,8-9,11H2,1-3H3;1H

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO: 7.35 mg/mL (14.75 mM), Need ultrasonic

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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.

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.

Products are for research use only. Not for human use.