CCT020312

• CAT Number: I005895
• CAS Number: 324759-76-4
• Molecular Formula: C31H30Br2N4O2
• Molecular Weight: 650.415
• Purity: ≥95%
• Solubility: Soluble in DMSO
• Storage: 0 - 4°C for short term ,or -20 °C for long term
• InChI: InChI=1S/C31H30Br2N4O2/c1-3-36(4-2)17-16-28(38)37-27(20-10-12-22(32)13-11-20)19-26(35-37)30-29(21-8-6-5-7-9-21)24-18-23(33)14-15-25(24)34-31(30)39/h5-15,18,27H,3-4,16-17,19H2,1-2H3,(H,34,39)
• InChIKey: OAXDKXMGESZLKV-UHFFFAOYSA-N
• SMILES: O=C1NC2=C(C=C(Br)C=C2)C(C3=CC=CC=C3)=C1C4=NN(C(CCN(CC)CC)=O)C(C5=CC=C(Br)C=C5)C4

CCT020312 is a potent and selective EIF2AK3 Activator. CCT020312 modulates the biological activity of EIF2AK3. CCT020312 sensitizes cancer cells with defective taxane-induced EIF2A phosphorylation to paclitaxel treatment. CCT020312 is a novel small molecule chemical tool for the selective activation of EIF2A-mediated translation control with utility for proof-of-concept applications in EIF2A-centered therapeutic approaches, and as a chemical starting point for pathway selective agent development. CCT020312 is potent, and EIF2AK3 selective agent and can act as a sensitizer to chemotherapy-associated stresses as elicited by taxanes.

Reference

1:Stockwell SR, Platt G, Barrie SE, Zoumpoulidou G, Te Poele RH, Aherne GW, Wilson SC, Sheldrake P, McDonald E, Venet M, Soudy C, Elustondo F, Rigoreau L, Blagg J, Workman P, Garrett MD, Mittnacht S. Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling. PLoS One. 2012;7(1):e28568. doi: 10.1371/journal.pone.0028568. PubMed PMID: 22253692; PubMed Central PMCID: PMC3257223.