JSI-124 White solid. PROTECT FROM LIGHT. PACKAGED UNDER INERT GAS. A cell-permeable, bitter triterpenoid compound (NCI identifier: NSC 521777) that displays anti-proliferative and antitumor properties both in vitro and in vivo. Acts as a potent and highly selective inhibitor of Janus kinase/signal transducer and activator of transcription 3 (JAK/STAT3) signaling pathway. It suppresses STAT3 tyrosine phosphorylation in v-Src-transformed NIH 3T3 cells and human lung adenocarcinoma A549 cells (IC50 = 500 nM), resulting in inhibition of STAT3 DNA-binding and STAT3-mediated gene transcription. Shown to inhibit the growth of STAT3-transformed tumors in nude mice. Does not affect oncogenic pathways mediated by Ras, Akt, Erk1/2, or JNK. Purity: ≥95% by HPLC. RTECS RC6200000, CAS 2222-07-3. Ref.: Blaskovich, M.A., et al. 2003. Cancer Res. 63, 1270. |
