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.
| Molecular Weight | 463.52 |
| Formula | C27H29NO6 |
| CAS Number | 599150-20-6 |
| Form | Solid |
| 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 |
|---|
| 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. |
| GANT58
GANT58 (NSC75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with an IC50 of 5 μM. |
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