| Molecular Formula | C27H35N5 |
| Molar Mass | 429.6 |
| Density | 1.134±0.06 g/cm3(Predicted) |
| Melting Point | 110 - 113°C |
| Boling Point | 549.0±50.0 °C(Predicted) |
| Solubility | DMSO: >2mg/mL |
| Appearance | powder |
| Color | white to off-white |
| pKa | 5.97±0.10(Predicted) |
| Storage Condition | 2-8°C |
| In vitro study | GANT61 inhibits GLI1 and GLI2 induced transcription. GANT61 inhibits the DNA binding ability of gli1. GANT61 Inhibits hedgehog signaling with an IC50 of 5 μm, which is more selective than other pathways, such as TNF signaling/NFκB activation, glucocorticoid receptor gene transcription, and the Ras-Raf-Mek-Mapk cascade. GANT61 effectively inhibits tumor cell proliferation in vitro, and this effect is GLI dependent. GANT61 acts on chronic lymphocytic leukemia cells (CLL), while abnormal B lymphocytes induce apoptosis. GANT61 acts on human colon cancer cell lines, is strongly cytotoxic, and abrogates colony formation. GANT61 acts in the early S phase of the human colon cancer cell line, inhibits DNA replication, generates a DNA damage signal involving the ATM-Chk2 signaling axis, and induces cell death. GANT61 (30 μm) acts on acute myeloid leukemia (AML) cells, resulting in growth arrest and apoptosis. GANT61 inhibits GLI1 and GLI2-induced transcription. GANT61 inhibits the DNA binding ability of gli1. GANT61 Inhibits hedgehog signaling with an IC50 of 5 μm, which is more selective than other pathways, such as TNF signaling/NFκB activation, glucocorticoid receptor gene transcription, and the Ras-Raf-Mek-Mapk cascade. GANT61 effectively inhibits tumor cell proliferation in vitro, and this effect is GLI dependent. GANT61 acts on chronic lymphocytic leukemia cells (CLL), while abnormal B lymphocytes induce apoptosis. GANT61 acts on human colon cancer cell lines, is strongly cytotoxic, and abrogates colony formation. GANT61 acts in the early S phase of the human colon cancer cell line, inhibits DNA replication, generates a DNA damage signal involving the ATM-Chk2 signaling axis, and induces cell death. GANT61 (30 μm) acts on acute myeloid leukemia (AML) cells, resulting in growth arrest and apoptosis. |
| In vivo study | GANT61 treatment of nude mice injected with gli1-positive 22Rv1 prostate cancer cells induced a regression in tumor growth until no significant tumor was observed. GANT61 orally fed at a dose of 50 mg/kg to nude mice carrying SK-N-AS neuroblastoma xenografts significantly inhibited tumor growth on day 12 of the experiment, with a 63% reduction in tumor volume compared to the control group. GANT61 treatment of nude mice injected with gli1-positive 22Rv1 prostate cancer cells induced tumor growth decline until no significant tumor was observed. GANT61 orally fed at a dose of 50 mg/kg to nude mice carrying SK-N-AS neuroblastoma xenografts significantly inhibited tumor growth on day 12 of the experiment, with a 63% reduction in tumor volume compared to the control group. |
| WGK Germany | 3 |
| HS Code | 29349990 |
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.328 ml | 11.639 ml | 23.277 ml |
| 5 mM | 0.466 ml | 2.328 ml | 4.655 ml |
| 10 mM | 0.233 ml | 1.164 ml | 2.328 ml |
| 5 mM | 0.047 ml | 0.233 ml | 0.466 ml |
| biological activity | GANT61 inhibits GLI1 and GLI2-induced transcription, inhibits hedgehog,IC50 is 5 μM, and selectively acts on other pathways, such as TNF and glucocorticoid receptor gene transcription. GANT61 (NSC 136476) is a GLI1 and GLI2 induced transcription inhibitor, which inhibits hedgehog. IC50 is 5 μM in HEK293T cells expressing GLI1. It selectively acts on other pathways, such as TNF and glucocorticoid receptor gene transcription. GANT61 can induce apoptosis and activate protective autophagy in LX-2 cells. |
| in vitro study | GANT61 inhibits GLI1 and GLI2 induced transcription. GANT61 inhibits the DNA binding ability of GLI1. GANT61 inhibits hedgehog signal with IC50 of 5 μM, which is more selective than other pathways, such as TNF signal/NFκB activation, glucocorticoid receptor gene transcription, and Ras-Raf-Mek-Mapk cascade. GANT61 effectively inhibits tumor cell proliferation in vitro, and this effect is GLI-dependent. GANT61 acts on chronic lymphocytic leukemia cells (CLL), but not normal B lymphocytes, inducing apoptosis. GANT61 acts on human colon cancer cell lines, has strong cytotoxicity, and abolishes colony formation. GANT61 acts on the early S phase of human colon cancer cell lines, inhibits DNA replication, generates DNA damage signals involving ATM-Chk2 signal axes, and induces cell death. GANT61 (30 μM) acts on acute myeloid leukemia (AML) cells, resulting in growth arrest and apoptosis. GANT61 inhibits GLI1 and GLI2-induced transcription. GANT61 inhibits the DNA binding ability of GLI1. GANT61 inhibits hedgehog signal with IC50 of 5 μM, which is more selective than other pathways, such as TNF signal/NFκB activation, glucocorticoid receptor gene transcription, and Ras-Raf-Mek-Mapk cascade. GANT61 effectively inhibits tumor cell proliferation in vitro, and this effect is GLI-dependent. GANT61 acts on chronic lymphocytic leukemia cells (CLL), but not normal B lymphocytes, inducing apoptosis. GANT61 acts on human colon cancer cell lines, has strong cytotoxicity, and abolishes colony formation. GANT61 acts on the early S phase of human colon cancer cell lines, inhibits DNA replication, generates DNA damage signals involving ATM-Chk2 signal axes, and induces cell death. GANT61 (30 μM) acts on acute myeloid leukemia (AML) cells, resulting in growth arrest and apoptosis. |
| in vivo study | GANT61 treated nude mice injected with GLI1-positive 22Rv1 prostate cancer cells to induce tumor growth and decline until no obvious tumor was observed. GANT61 was orally fed at a dose of 50 mg/kg to treat nude mice carrying SK-N-AS neuroblastoma transplantation tumor. On the 12th day of the experiment, the tumor growth was significantly inhibited. Compared with the control group, the tumor volume was reduced by 63%. GANT61 treated nude mice injected with GLI1-positive 22Rv1 prostate cancer cells to induce tumor growth and decline until no obvious tumor was observed. GANT61 was orally fed at a dose of 50 mg/kg to treat nude mice carrying SK-N-AS neuroblastoma transplantation tumor. On the 12th day of the experiment, the tumor growth was significantly inhibited. Compared with the control group, the tumor volume was reduced by 63%. |
| target | TargetValue GLI1 (HEK293T cells expressing GLI1) 5 μM |
| Target | Value |
| GLI1 (HEK293T cells expressing GLI1) | 5 μM |