Formulation: A crystalline solid
Formal Name: 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis(N,N-dimethyl-benzenamine)
Purity: ≥98%
Formula Markup: C27H35N5
Formula Weight: 429,6
Shelf life (days): 1460
CAS Number: 500579-04-4
Notes: 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.{18037} It does not affect signaling through NF-κB, glucocorticoid receptor, MAPK, HGF, C/EBPα, or HIF-1, supporting specificity for the Hedgehog pathway.{18037} 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.{18037}
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