An antagonist of the transcription factor Gli

GANT 61 – 5 mg

Brand:
Cayman
CAS:
500579-04-4
Storage:
-20
UN-No:
Non-Hazardous - /

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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Description

An antagonist of the transcription factor Gli, inhibiting Gli1 activation of gene expression with an IC50 value of 5 μM; does not affect signaling through several other pathways, supporting specificity for the Hedgehog pathway; has been shown to inhibit the proliferation of cancer cells, both in vitro and in mice

Formal name: 2,2′-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis(N,N-dimethyl-benzenamine)

Synonyms:  NSC 136476

Molecular weight: 429.6

CAS: 500579-04-4

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Research Area|Cancer|Cell Signaling|Hedgehog Signaling

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