GANT61
Catalog No.S8075 Synonyms: NSC 136476
Molecular Weight(MW): 429.6
GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation.
7 Customer Reviews
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Apoptosis evaluation of UACC62R, SK-MEL-28 R and R3 cells treated with Gant61 (10 μM) for 48 h by flow cytometry detection of Annexin V staining.
Oncogene, 2017, 36(13): 1849-1861. GANT61 purchased from Selleck.
Western blot revealed that the expression levels of p-STAT3, and SOCS3 decreased accompanied with the inhibition of GLI1 by GANT61 in the three cells. Statistical data represent the means ± SEM of three independent experiments. (*P < 0.05, compared with solvent group).
Oncotarget. 2017, 8(30):48701-48710. GANT61 purchased from Selleck.
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GANT61 suppresses AML cell growth. (A) AML cell lines were treated with different concentrations of GANT61 for 48 h. Cell viability was assessed by WST-8 assay. (B) The line graph showed the effect of GANT61 on colony formation capacity in AML cell lines. * P < 0.05, ** P< 0.01, *** P < 0.001.
Cell Physiol Biochem, 2016, 38(4):1288-302.. GANT61 purchased from Selleck.
GANT61 enhanced the DNA damage effect initiated by TMZ treatment. Representative comet staining images in U87 and U251 cells after different treatments (5 μM GANT61, 100 μM TMZ or both).
J Exp Clin Cancer Res, 2016, 35(1):184.. GANT61 purchased from Selleck.
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Pharmacologic inhibition of GLI1 reduces tumor cell growth. A, LM3 tumor cells were treated with GANT61 at s concentration of 20 μm for 72 h. Cell viability was then measured using resazurin (left panel), and antiapoptotic gene expression was measured by q-PCR. *, p < 0.05 versus control group. B, mice implanted with LM3 cells were treated with GANT61 (50 mg/kg), and tumor size was measured as in Fig. 8. *, p < 0.01 versus control group. Bars and error bars represent means and S.E., respectively.
J Biol Chem, 2016, 291(4):1933-47. . GANT61 purchased from Selleck.
The GBC cell line was incubated with 20 μM cyclopamine or Gant-61. At different time points, the caspase signal was measured using the Caspase-Glo assay.
Mol Cell Biochem, 2014, 396(1-2): 257-68. GANT61 purchased from Selleck.
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The GBC cell line was incubated with 20 μM cyclopamine or Gant-61. At different time points, the nuclear fragmentation was measured using the fluorescence microscopy.
Mol Cell Biochem, 2014, 396(1-2): 257-68. GANT61 purchased from Selleck.
Purity & Quality Control
Choose Selective Hedgehog/Smoothened Inhibitors
Biological Activity
| Description | GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM in GLI1 expressing HEK293T cell, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. | ||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription. 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. [1] GANT61 induces apoptosis in chronic lymphocytic leukemia cells (CLL), but not in normal B lymphocytes. [2] GANT61 induces robust cytotoxicity and abolishs the clonogenicity in human colon carcinoma cell lines. [3] 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. [4] GANT61 (30 μM) causes growth arrest and apoptosis in acute myeloid leukemia (AML) cells. [5] |
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| Cell Data |
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| In vivo | In nude mice injected with GLI1-positive 22Rv1 prostate cancer cells, GANT61 induces growth regression until no tumor is palpable. [1] In nude mice carrying SK-N-AS neuroblastoma xenografts, GANT61 treatment (oral gavage, 50 mg/kg) significantly inhibits tumor growth at Day 12 , as the tumor volume is reduced to 63% compared with controls. [6] |
Protocol
| Kinase Assay:[1] |
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Dual Luciferase Assay: HEK293 cells are transfected with GLI1 expression plasmid, together with the reporter plasmids 12×GliBSLuc and R-Luc on 10-cm plates (day 0). Twenty-four hours later, cells are seeded in white 96-well plates with clear bottom at a density of 15,000 cells per well. Cells are allowed to attach, and compounds are added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells are grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit. |
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| Cell Research:[1] |
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| Animal Research:[1] |
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Solubility (25°C)
| In vitro | Ethanol | 12 mg/mL (27.93 mM) |
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| DMSO | Insoluble | |
| Water | Insoluble | |
| In vivo | Add solvents to the product individually and in order(Data is from Selleck tests instead of citations): 20% ethanol+80% corn oil For best results, use promptly after mixing. |
40mg/mL |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 429.6 |
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| Formula | C27H35N5 |
| CAS No. | 500579-04-4 |
| Storage | powder |
| in solvent | |
| Synonyms | NSC 136476 |
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