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.
Antioxidants (Basel). 2022 Nov 16;11(11):2265.
Hedgehog Signalling Contributes to Trauma-Induced Tendon Heterotopic Ossification and Regulates Osteogenesis through Antioxidant Pathway in Tendon-Derived Stem Cells
GANT58 purchased from AbMole
Molecular Weight | 392.48 |
Formula | C24H16N4S |
CAS Number | 64048-12-0 |
Solubility (25°C) | DMSO 20 mM |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.
Related Gli Products |
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GLI antagonist-1
GLI antagonist-1 is a potent GLI antagonist with an IC50 value of 1.1 µM. In addition, GLI antagonist-1 has antiproliferative activity by reducing GLI1 mRNA expression and dose-dependently inhibiting colony formation. |
Glabrescione B
Glabrescione B is a selective GLI1 inhibitor that impairs Gli1 activity by interfering with Gli1-DNA interactions. In addition, Glabrescione B inhibits the growth of Hedgehog-dependent tumor cells and suppresses the self-renewal capacity and clonogenic ability of tumor-derived stem cells. |
GANT61
GANT61 is a Gli1 and Gli2 inhibitor targeting the Hedgehog/GLi pathway that inhibits GLI1- and GLI2-induced transcription with an IC50 of 5 μM. In addition, GANT61 selectively acts on the transcription of other pathways such as TNF and glucocorticoid receptor genes. |
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