Name | GANT61 |
Synonyms | GNT61 GANT61 CS-867 GANT 61 NSC 136476 2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine Benzenamine, 2,2'-[[dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethyl- 2,2'-[[Dihydro-2-(4-pyridinyl)-1,3(2H,4H)-pyrimidinediyl]bis(methylene)]bis[N,N-dimethylbenzenamine] GANT61 |
CAS | 500579-04-4 |
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 |