Cas No.: | 1034895-42-5 |
Chemical Name: | 3-(5-fluorobenzofuran-3-yl)-4-(5-methyl-5H-[1,3]dioxolo[4,5-f]indol-7-yl)-1H-pyrrole-2,5-dione |
Synonyms: | 9ING41;9-ING 41 |
SMILES: | N1C(=O)C(C2=COC3C2=CC(=CC=3)F)=C(C2=CN(C)C3C=C4C(=CC2=3)OCO4)C1=O |
Formula: | C22H13FN2O5 |
M.Wt: | 404.34 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Publication: | [1]. Ugolkov AV, et al. 9-ING-41, a small-molecule glycogen synthase kinase-3 inhibitor, is active in neuroblastoma. Anticancer Drugs. 2018 Sep;29(8):717-724. [2]. Wu X, et al. Targeting glycogen synthase kinase 3 for therapeutic benefit in lymphoma. B |
Description: | 9-ING-41 is a potent glycogen synthase kinase-3 (GSK-3) inhibitor[1]. 9-ING-41 induces apoptosis and cell cycle arrest at prophase by targeting centrosomes and microtubule-bound GSK-3β. 9-ING-41 has anticancer activity[2]. |
In Vivo: | 9-ING-41 (40 mg/kg/every other day; for 17 days) has single-agent antitumor activity in a mouse model of MCL[2]. Animal Model: NSG (NOD.Cg-PrkdcscidIl2rgtm1Wjl/SzJ) mice[2] Dosage: 40 mg/kg Administration: Every other day; for 17 days Result: Had single-agent antitumor activity in a mouse model of MCL. |
In Vitro: | 9-ING-41 (2, 4 μM; 48 hours) decreases neuroblastoma cell viability induces apoptosis[2]. 9-ING-41 (1, 2 μM; 24 hours) is a potent cell cycle-blocking agent for lymphoma cells[2]. 9-ING-41 (0.1-1 µM) inhibits GSK-3 leading to a decreased expression of the NF-κB target XIAP and significant apoptosis in neuroblastoma cells as shown by PARP cleavage, an apoptosis marker[1]. 9-ING-41 (0.5, 1.0, 1.5, 2.0 μM) inhibits the proliferation rate of all TCL and MCL lines with concentrations as low as 1.0 mM[2]. Cell Viability Assay[2] Cell Line: TCL and MCL lines Concentration: 2, 4 μM Incubation Time: 48 hours Result: Induced apoptosis. Cell Cycle Analysis[2] Cell Line: Lymphoma cells (Jeko, Mino, and OCI-Ly cell lines) Concentration: 1, 2 μM Incubation Time: 24 hours Result: Led to cell cycle arrest in G2/M. Western Blot Analysis[1] Cell Line: SK-N-DZ and SK-N-BE neuroblastoma cells Concentration: 0.1, 1 µM Incubation Time: 48 hours Result: Inhibited GSK-3 leading to a decreased expression of the NF-κB target XIAP. |