GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. GANT61 inhibits the DNA binding ability of GLI1. GANT61 inhibits hedgehog signaling with IC50 of 5 μM, displays selectivity over other pathways, such as TNF signaling/NFκB activation, glucocorticoid receptor gene transactivation, and the Ras–Raf–Mek–Mapk cascade. GANT61 efficiently inhibited in vitro tumor cell proliferation in a GLI-dependent manner. GANT61 induces inhibition of DNA replication in early S-phase in human colon carcinoma cell lines, leading to DNA damage signaling involving an ATM–Chk2 axis and induction of cell death.
Theranostics. 2022 Mar 28;12(7):3131-3149.
Shh and Olig2 sequentially regulate oligodendrocyte differentiation from hiPSCs for the treatment of ischemic stroke
GANT61 purchased from AbMole
J Oncol. 2022 Jun 29;2022:1399697.
Mechanism of Targeting the Hedgehog Signaling Pathway against Chemotherapeutic Resistance in Multiple Myeloma
GANT61 purchased from AbMole
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Source | Oncotarget (2015). Figure 3. GANT61 |
| Method | apoptosis assay | |
| Cell Lines | MMe cell | |
| Concentrations | 20 μM | |
| Incubation Time | 24 - 72 h | |
| Results | The antiproliferative activity of GANT61 was assessed in MMe cells. GANT61 inhibited cell proliferation in all MMe cell lines in a dose-dependent manner |
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells |
| Preparation method | HEK293 cells were transfected with GLI1 expression plasmid, together with the reporter plasmids 12xGliBS-Luc and R-Luc on 10-cm plates (day 0). Twenty-four hours later, cells were seeded in white 96-well plates with clear bottom at a density of 15,000 cells per well. Cells were allowed to attach, and compounds (Diversity Set, 1990 compounds; National Cancer Institute, Bethesda, MD) were added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells were grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit (Promega, Madison, WI). Plates were read on a Berthold Technologies (Bad Wildbad, Germany) microplate luminometer. |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | 22Rv1 cells xenograft in female BALB/c nude mice (nu/nu) |
| Formulation | corn oil:ethanol, 4:1 |
| Dosages | 50 mg/kg for 16 days |
| Administration | s.c. injections |
| Molecular Weight | 429.6 |
| Formula | C27H35N5 |
| CAS Number | 500579-04-4 |
| Solubility (25°C) | DMSO 20 mg/mL |
| 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 |
|---|
| 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. |
| GANT58
GANT58 (NSC75503) is a potent GLI antagonist that inhibits GLI1-induced transcription with an IC50 of 5 μM. |
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