GANT58 is a cell-permeable GLI antagonist that inhibits GLI1-induced transcription (IC50 = 5 μM). Acts as a blocker of Hedgehog (Hh) pathway downstream of SMO and SUFU causing Gli1 nuclear accumulation. It also targets Gli-mediated gene transactivation (IC50 ~ 5 µM in SAG-stimulated Shh-L2 cells) and displays anti-proliferative and antitumor activity in vivo.
|Source||Biochimie (2014). Figure 3. GANT58|
|Cell Lines||T-ALL cells|
|Concentrations||5 and 10 μM|
|Incubation Time||48 h|
|Results||Furthermore, incubation of CCRFeCEM with 10 μM GANT58 for 48 h caused an increase in the percentage of cells in G1 and S phase and a decrease in the percentage of cells in G2/M phase relative to controls|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 20 mM|
Molecular pathways: the role of primary cilia in cancer progression and therapeutics with a focus on Hedgehog signaling.
Hassounah NB, et al. Clin Cancer Res. 2012 May 1;18(9):2429-35. PMID: 22415315.
Small-molecule modulators of the Sonic Hedgehog signaling pathway.
Stanton BZ, et al. Mol Biosyst. 2010 Jan;6(1):44-54. PMID: 20024066.
Hedgehog target genes: mechanisms of carcinogenesis induced by aberrant hedgehog signaling activation.
Katoh Y, et al. Curr Mol Med. 2009 Sep;9(7):873-86. PMID: 19860666.
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Smoothened Agonist (SAG) HCl is a cell-permeable Smoothened (Smo) agonist with EC50 of 3 nM in Shh-LIGHT2 cells.
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Jervine is a naturally occuring steroidal alkaloid that causes cyclopia by blocking sonic hedgehog signaling.
GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM.
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