WS-383 - ≥99% , CAS No.2247544-02-9

CAS: 2247544-02-9 Cat. No.: W648916 Molecular Weight: 498.46 PubChem CID: 138319703

GRADE & PURITY ≥99%

Storage

Store at 2-8°C,Protected from light,Desiccated

Shipped In

Wet ice

Overview

WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC 50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2

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. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell 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 AnalysisCell 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.

Form:Solid

IC50& Target:IC50: 11 nM (DCN1-UBC12 interaction)

Specifications

Specifications & Purity

≥99%

Biochemical and Physiological Mechanisms

WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC 50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.

Storage

Store at 2-8°C, Protected from light, Desiccated

Shipped In

Wet ice

This product requires cold chain shipping. Ground and other economy services are not available.

Purity

≥99%

Names and Identifiers

• Canonical Smiles: CC1=NC2=NC(=NN2C(=C1)SC3=NN=NN3CCN(C)C)SCC4=CC=C(C=C4)Cl.Cl
• IUPAC Name: 2-[5-[[2-[(4-chlorophenyl)methylsulfanyl]-5-methyl-[1,2,4]triazolo[1,5-a]pyrimidin-7-yl]sulfanyl]tetrazol-1-yl]-N,N-dimethylethanamine;hydrochloride
• InChIKey: LJZUAAKUJAXXHQ-UHFFFAOYSA-N
• 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
• PubChem CID: 138319703
• Molecular Weight: 498.46

Chemical and Physical Properties

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