Cucurbitacin I

Cucurbitacin I is triterpenoid compound that acts as a potent inhibitor of the STAT3/JAK signaling pathway. It specifically suppresses levels of tyrosine phosphorylated STAT3 in v-Src-transformed NIH 3T3 cells and in A549 cells (IC50 = 500 nM) resulting in inhibition of STAT3 DNA binding and reduced STAT3-mediated gene transcription. It also suppresses JAK2 phosphorylation but does not affect Src, ERK, JNK or Akt. In nude mice, cucurbitacin I (1 mg/kg/day) suppressed growth of various tumors expressing constitutively active STAT3. It promotes the differentiation of dendritic cells and macrophages and enhances the effect of cancer immunotherapy. Cucubitacin I (1 µM for 2 hours) reduced clonogenicity of nasopharyngeal carcinoma cells in vitro and suppresses tumor growth in mice (1.3 mg/kg).Formal Name: (10alpha)-2,16alpha,20,25-tetrahydroxy-9beta-methyl-19-norlanosta-1,5,23E-triene-3,11,22-trione. CAS Number: 2222-07-3. Synonyms: Elatericin B, JSI-124, NSC 521777. Molecular Formula: C30H42O7. Formula Weight: 514.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: 5 mg/ml, Ethanol: 10 mg/ml. lambdamax: 234, 268 nm. SMILES: O=C(C1(C)C)C(O)=C[C@]2([H])C1=CC[C@]([C@@](C[C@@H](O)[C@]3([H])[C@](O)(C)C(/C=C/C(C)(O)C)=O)(C)[C@]3(C)C4)([H])[C@@]2(C)C4=O. InChi Code: InChI=1S/C30H42O7/c1-25(2,36)12-11-21(33)30(8,37)23-19(32)14-27(5)20-10-9-16-17(13-18(31)24(35)26(16,3)4)29(20,7)22(34)15-28(23,27)6/h9,11-13,17,19-20,23,31-32,36-37H,10,14-15H2,1-8H3/b12-11+/t17-,19-,20+,23+,27+,28-,29+,30+/m1/s1. InChi Key: NISPVUDLMHQFRQ-MKIKIEMVSA-N.