Home / Pharmacology / Enzymes / Ligases / Ubiquitin E3 Ligases / Ubiquitin E3 Ligase Inhibitors / WS 383

WS 383

Cat. No. 7055 Submit a Review Datasheet / COA / SDS
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Description: Potent, selective and reversible DCN1-UBC12 interaction inhibitor
Chemical Name: 5-[[2-[[(4-Chlorophenyl)methyl]thio]-5-methyl[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]thio]-N,N-dimethyl-1H-tetrazole-1-ethanamine hydrochloride
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (3)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for WS 383

WS 383 is a potent and reversible DCN1-UBC12 interaction inhibitor (IC50 = 11 nM). The compound displays selectivity for DCN1-UBC12 over inhibition of a panel of kinases. including Bruton's tyrosine kinase (BTK), cyclin-dependent kinases (CDKs) and epidermal growth factor receptor (EGFR). In vitro, WS 383 selectively inhibits cullin-3 neddylation over other cullins, and induces accumulation of p21, p27 and NRF2.

Compound Libraries for WS 383

WS 383 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Epigenetics Library. Find out more about compound libraries available from Tocris.

Technical Data for WS 383

M. Wt 498.45
Formula C18H20ClN9S2.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2247544-02-9
PubChem ID 138319703
InChI Key LJZUAAKUJAXXHQ-UHFFFAOYSA-N
Smiles CN(CCN1N=NN=C1SC2=CC(C)=NC3=NC(SCC4=CC=C(C=C4)Cl)=NN23)C.Cl

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for WS 383

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 49.84 100

Preparing Stock Solutions for WS 383

The following data is based on the product molecular weight 498.45. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.01 mL 10.03 mL 20.06 mL
5 mM 0.4 mL 2.01 mL 4.01 mL
10 mM 0.2 mL 1 mL 2.01 mL
50 mM 0.04 mL 0.2 mL 0.4 mL

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References for WS 383

References are publications that support the biological activity of the product.

Wang et al (2019) 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. 62 2772 PMID: 30803229

If you know of a relevant reference for WS 383, please let us know.

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Keywords: WS 383, WS 383 supplier, WS383, ubiquitin, E3, E2, ligase, interaction, inhibitor, inhibits, protein-protein, Cul3/1, neddylation, CRL, cullin-RING, ligases, Ubiquitin, Ligases, Ubiquitin/Ubl, Conjugating, Enzymes, 7055, Tocris Bioscience

Citations for WS 383

Citations are publications that use Tocris products.

Currently there are no citations for WS 383. Do you know of a great paper that uses WS 383 from Tocris? Please let us know.

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Literature in this Area

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