2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme
  4. WS-383

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.

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WS-383 Chemical Structure

WS-383 Chemical Structure

CAS No. : 2247544-02-9

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Based on 1 publication(s) in Google Scholar

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WS-383 Related Antibodies

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Description

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].

IC50 & Target

IC50: 11 nM (DCN1-UBC12 interaction)[1]
In Vitro

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

WS-383 Related Antibodies

Western Blot Analysis[1]

Cell Line: MGC-803 cells
Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Decreased N8-Cul1 and N8-Cul2 protein expression.

Western Blot Analysis[1]

Cell Line: MGC-803 and KYSE70 cells
Concentration: 0.03 μM; 0.3 μM; 3 μM; 10 μM
Incubation Time: 24 hours
Result: Induced accumulation of p21, p27, and NRF2 in MGC-803 cells.
Molecular Weight

498.46

Formula

C18H21Cl2N9S2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CN(C)CCN1N=NN=C1SC2=CC(C)=NC3=NC(SCC4=CC=C(Cl)C=C4)=NN23.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 7.35 mg/mL (14.75 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0062 mL 10.0309 mL 20.0618 mL
5 mM 0.4012 mL 2.0062 mL 4.0124 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0062 mL 10.0309 mL 20.0618 mL 50.1545 mL
5 mM 0.4012 mL 2.0062 mL 4.0124 mL 10.0309 mL
10 mM 0.2006 mL 1.0031 mL 2.0062 mL 5.0154 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

WS-3832247544-02-9WS383WS 383E1/E2/E3 EnzymeE1 activating enzymeE2 conjugating enzymeE3 ligating enzymeUbiquitin activating enzymeUbiquitin conjugating enzymeUbiquitin ligaseMGC-803KYSE70cellDCN1-UBC12interactionInhibitorinhibitorinhibit

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