WS-383 free base


Catalog No. Size PriceQuantity
M17178-C Contact sales@xcessbio.com for quotation $100Unavailable

Description

WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.

Product information

CAS Number: 2247543-65-1

Molecular Weight: 461.99

Formula: C18H20ClN9S2

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

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

InChiKey: MGESDQAAIJOGJA-UHFFFAOYSA-N

InChi: InChI=1S/C18H20ClN9S2/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

Technical Data

Appearance: Solid Power

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

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 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. 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.

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

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