JW74

SKU: orb1308166

Description

JW74 is a potent small molecule inhibitor of canonical Wnt signaling, exhibiting an IC50 of 420 nM against LiCl-induced pathway activation. This tool compound is valuable for in vitro and in vivo research investigating Wnt/β-catenin signaling in development, oncology, and stem cell biology.

Research Area

Signal Transduction, Stem Cell & Developmental Biology

Key Properties

• CAS Number: 863405-60-1
• MW: 456.52
• Purity: 95.99% (May vary between batches)
• Formula: C₂₄H₂₀N₆O₂S
• SMILES: COc1ccc(cc1)-n1c(SCc2nc(no2)-c2ccc(C)cc2)nnc1-c1ccncc1
• Target: Wnt/beta-catenin
• Solubility: DMSO:45 mg/mL (98.57 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.38 mM)

Bioactivity

• Target IC50:
  Wnt:420 nM
• In Vivo:
  The in vivo efficacy of JW74 is evaluated using SW480 cell xenografts, with high doses (150 or 300 mg/kg) administered due to rapid degradation in the organism, as shown by human liver microsome analysis (t1/2=2.5 minutes) and pharmacokinetic analyses (t1/2=30 minutes after peroral injections and t1/2=15 minutes after intravenous injections). JW74 concentrations in tumors range from 4.2 to 72.1 μmol/kg for 150 mg/kg, 1.9 to 11.1 μmol/kg for 300 mg/kg, and reach 2.8 μM in plasma for both doses .
• In Vitro:
  Ki-67 expression is reduced from 97.5% in DMSO-treated cells to 86.7% in JW74-treated cells. Relative to DMSO-treated cells, the cellular viability of U2OS cells treated for 72 h treatment with 10 μM JW74 is reduced to 80%. The effect of tankyrase inhibition on cellular viability is tested by performing an MTS assay. Flow cytometry is also performed to determine the expression marker Ki-67 in U2OS following 48 h treatment with DMSO or 10 uM JW74 . JW74 displays a reduction of canonical Wnt signaling in the ST-Luc assay (IC50: 790 nM) .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Wnt, Wnt/b-catenin, Wnt/β-catenin, Wnt/betacatenin, βcatenin, JW 74, JW74, JW-74, inhibit, Inhibitor, bcatenin, beta-catenin, betacatenin

Compound Identifiers

PubChem CID

16013152