An inhibitor of the DCNL1-UBC12 protein-protein interaction
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WS-383

Item No. 45391

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal 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, monohydrochloride
CAS Number
2247544-02-9
Molecular Formula
C18H20ClN9S2 • HCl
Formula Weight
498.5
Purity
≥98%
Formulation (Request formulation change)
A solid
SMILES
ClC1=CC=C(CSC2=NN3C(SC4=NN=NN4CCN(C)C)=CC(C)=NC3=N2)C=C1.Cl
InChi Code
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
InChi Key
LJZUAAKUJAXXHQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $105

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    10 mg

    $168

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    Cayman Chemical
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    Product Description

    WS-383 is an inhibitor of the protein-protein interaction between DCN1-like protein 1 (DCNL1) and ubiquitin-conjugating enzyme 12 (UBC12; IC50 = 11 nM in a cell-free assay).1 It selectively inhibits NEDDylation of the DCNL-1 targets and ubiquitin ligase complex components cullin-3 and -1 over other cullin proteins and increases levels of the cullin-RING ligase complex (CRL) targets p21, p27, and Nrf2 in MGC803 gastric cancer cells at 10 µM. WS-383 inhibits cell growth and migration and induces cell cycle arrest at the G2/M phase and apoptosis in MGC803 cells. It decreases tumor size in an MGC803 mouse xenograft model when administered at doses of 25 or 50 mg/kg. WS-383 also inhibits lysine-specific demethylase 1 (LSD1) activity in a cell-free assay (IC50 = 288 nM).2

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Wang, S., Zhao, L., Shi, X.-J., et al. Development of highly potent, selective, and cellular active triazolo[1,5-α]pyrimidine-based inhibitors targeting the DCN1-UBC12 protein-protein interaction. J. Med. Chem. 62(5), 2772-2797 (2019).

    2. Song, Z., Gao, K., Asmamaw, M.D., et al. Discovery of the antitumor activities of a potent DCN1 inhibitor compound 383 targeting LSD1 in gastric cancer. Eur. J. Pharmacol. 916, 174725 (2022).