ARN3236

ARN3236 is an inhibitor of salt-inducible kinase 2 (SIK2, IC50 = 50s = 21.63 and 6.63 nM, respectively). It inhibits TNF-alpha secretion in RAW 264.7 cells (IC50 = ~2.5 µM) and reduces phosphorylation of the SIK2 targets CRTC3 and HDAC4 in macrophages when used at a concentration of 3 µM. ARN3236 inhibits growth of 10 ovarian cancer cell lines (IC50s = 0.8-2.6 µM) and increases the sensitivity of eight of them to paclitaxel (Cay-10461). It halts the cell cycle at the G2/M phase and induces apoptosis and tetraploidy in SKOV3 cells when used at a concentration of 1 µM. ARN3236 (60 mg/kg per day) has an additive effect on reducing tumor growth when used in combination with paclitaxel in an ovarian cancer mouse xenograft model.Formal Name: 3-(2,4-dimethoxyphenyl)-4-(3-thienyl)-1H-pyrrolo[2,3-b]pyridine. CAS Number: 1613710-01-2. Molecular Formula: C19H16N2O2S. Formula Weight: 336.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:4): 0.20 mg/ml. SMILES: COC1=CC(OC)=C(C=C1)C2=CNC3=C2C(C4=CSC=C4)=CC=N3. InChi Code: InChI=1S/C19H16N2O2S/c1-22-13-3-4-15(17(9-13)23-2)16-10-21-19-18(16)14(5-7-20-19)12-6-8-24-11-12/h3-11H,1-2H3,(H,20,21). InChi Key: WEHOIIGXTMKVRG-UHFFFAOYSA-N.