WSB1 Degrader 1

SKU: orb1218371

Description

WSB1 Degrader 1 is a poten and orally active WD repeat and SOCS box-containing 1 degrader. WSB1 Degrader 1 has anticancer metastatic effects.

Key Properties

• CAS Number: 2306039-66-5
• MW: 334.41
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₂N₂O₂
• SMILES: NC1=NC(C2=CC=C(OC)C(C)=C2)=C(C3=CC=C(OC)C(C)=C3)C=C1
• Target: WSB1
• Solubility: DMSO:24 mg/mL (71.76 mM; Need ultrasonic)

Bioactivity

• In Vivo:
  WSB1 Degrader 1 (compound 4; 100 mg/kg; p.o. ; daily; for 28 days) treatment can effectively inhibit the pulmonary metastasis of cancer cells. In rats, after 100 mg/kg oral dosing or 160 mg/kg intraperitoneal dosing of WSB1 Degrader 1 (compound 4), the two ways of administration are observed with quick absorption (Tmax), but the former dosing displayed a fast clearance (T1/2). Moreover, Cmax and AUC0-t values of WSB1 Degrader 1 in oral or intraperitoneal dosing groups showed acceptable blood exposure. Animal model: Balb/c (nu/nu) mice bearing highly metastatic 4T1 breast cancer cells. Dosage: 100 mg/kg/day. Administration: p.o. ; daily; for 28 days. Result: Effectively inhibited the pulmonary metastasis of cancer cells.
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• In Vitro:
  WSB1 Degrader 1 (compound 4; 0.25-2500 nM; 2-24 hours; H1299-WSB1 cells) treatment indues WSB1 degradation in time-dependent and dose-dependent manners. WSB1 Degrader 1 (compound 4) exhibits potent antimigration efficacy in both KHOS and H460 cell lines with IC50 values of 39.1 μM and 24.47 μM, respectively. WSB1 Degrader 1 (compound 4) significantly inhibits cancer cell migration under normoxia and hypoxia in KHOS cells. WSB1 Degrader 1 (5 μM) treatment elevates the levels of the RhoGDI2 protein in KHOS cells under hypoxia. The wound-healing of H1299-WSB1 cells is significantly inhibited by treating with WSB1 Degrader 1. WSB1 Degrader 1 can only block the wound-healing capability of wild-type A2780 (A2780-WT) cells but not the A2780-WSB1/KO cells. Western blot analysis. Cell line: H1299-WSB1 cells. Concentration: 0.25 nM, 2.5 nM, 25 nM, 250 nM, 2500 nM Incubation time: 2 hours, 4 hours, 6 hours, 8 hours, 12 hours, 24 hours. Result: Induced WSB1 degradation in time-dependent and dose-dependent manners.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

WSB1