Cat. No. Name Size Price Add Cart
KI3695GANT6110 mg$250
GANT6150 mg$970

Chemical Characteristic

Product NameGANT61
CAS No.500579-04-4
Molecular Weight 429.6
FormulaC27H35N5
Chemical NameBenzenamine, 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethyl-
SmilesC1(N(CCCN1Cc1c(cccc1)N(C)C)Cc1c(cccc1)N(C)C)c1ccncc1
Chemical Structure

Biological activities

GANT61 is a selective GLI1 and 2 inhibitor (IC50 = 5 ?M). It blocks the hedgehog/smoothened signaling pathway with anticancer activity[1]. GANT61 (Gli-ANTagonist 61) was identified from a cell-based screen for inhibitors of Gli-mediated transcription. Recently, GANT61 has been identified as a potent Hh signaling pathway inhibitor for treating various cancers. In vitro, it can be used by 5 ?M in CLL [2]. In vivo, it can be used by 50 mg/kg/day in mice [3].

References

[1] Pan D, et al. Gli inhibitor GANT61 causes apoptosis in myeloid leukemia cells and acts in synergy with rapamycin. Leuk Res. 2012, 36(6):742-748.
[2] Barsoum I,Yao HH. Redundant and differential roles of transcription factors Gli1 and Gli2 in the development of mouse fetal Leydig cells. Biol Reprod. 2011, 84(5):894-899.
[3] Lauth M, et al. Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists. Proc Natl Acad Sci U S A. 2007, 104(20):8455-8460.

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