GANT 61

Hedgehog proteins, important regulators of development, bind the cell-surface protein Patched, allowing activation of Smoothened. In vertebrates, this ultimately leads to the activation of the zinc-finger transcription factors of the Gli family. Overactivation of this pathway contributes to certain cancers, including glioblastoma, for which the Gli proteins are named. GANT 61 is a Gli antagonist, inhibiting Gli1 activation of gene expression with an IC50 value of 5 µM. It does not affect signaling through NF-kappaB, glucocorticoid receptor, MAPK, HGF, C/EBPalpha, or HIF-1, supporting specificity for the Hedgehog pathway. GANT 61 has been shown to inhibit the in vitro proliferation of PANC-1 and 22Rv1 cancer cells, which have elevated Gli1 levels, and prevent the development of 22Rv1 tumors in mice.Formal Name: 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis(N,N-dimethyl-benzenamine). CAS Number: 500579-04-4. Synonyms: NSC 136476. Molecular Formula: C27H35N5. Formula Weight: 429.6. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, Ethanol: 1 mg/ml, Ethanol:PBS (pH 7.2) (1:3): 0.25 mg/ml. lambdamax: 248 nm. SMILES: CN(C)C1=CC=CC=C1CN2CCCN(CC3=CC=CC=C3N(C)C)C2C4=CC=NC=C4. InChi Code: InChI=1S/C27H35N5/c1-29(2)25-12-7-5-10-23(25)20-31-18-9-19-32(27(31)22-14-16-28-17-15-22)21-24-11-6-8-13-26(24)30(3)4/h5-8,10-17,27H,9,18-21H2,1-4H3. InChi Key: KVQOGDQTWWCZFX-UHFFFAOYSA-N.