For research use only. Not for use in humans.

Catalog No.S8075 Synonyms: NSC 136476

24 publications

GANT61 Chemical Structure

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.

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Selleck's GANT61 has been cited by 24 publications

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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.
GLI1 [1]
(HEK293T cells expressing GLI1)
5 μM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human Shh-L2 cells NF[z[2RHfW6ldHnvckBie3OjeR?= NV\XcGZOUW6qaXLpeIlwdiCxZjDI[YRo\WixZzDzbYdv[WyrbnegbY4hcHWvYX6gV4hpNUx{IHPlcIx{NCCLQ{WwQVUh|ryP MlTINVc1QTR5Nk[=
human Rh30 cells M2W3WGZ2dmO2aX;uJIF{e2G7 MVuyOEBp M4L2bWlvcGmkaYTpc44hd2ZiaIXtZY4hT2yrMT3t[YRq[XSnZDD0doFve2O{aYD0bY9v[WxiYXP0bZZqfHliaX6gbJVu[W5iUnizNEBk\WyuczDh[pRmeiB{NDDodpMh[nlibIXjbYZmemG|ZTDy[ZBwenSncjDn[Y5mKGG|c3H5MEBKSzVyPUSwJO69VQ>? M4XY[VIxPjB3N{Kw
HEK293 cells NXLZfWhUTnWwY4Tpc44h[XO|YYm= NFvwS3JT\WS3Y4Tpc44hd2ZiR1zJNkBu\WSrYYTl[EB1emGwc3PybZB1cW:wIHnuJGhGUzJ7MzDj[YxteyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7 MVuxO|Q6PDd4Nh?=
human PANC1 cells NHLnb4RHfW6ldHnvckBie3OjeR?= NYXOd4N{PSEQvF2= Ml\vVoVlfWO2aX;uJIlvKEeOSUGg[ZhxemW|c3nvckBqdiCqdX3hckBRSU6FMTDj[YxteyCjdDC1JJVO MXWxO|Q6PDd4Nh?=
mouse NIH3T3 cells NEDuVlRHfW6ldHnvckBie3OjeR?= M17tOWlvcGmkaYTpc44hd2ZiR1zJNUBqdmS3Y3XkJIhm\GenaH;nJJNq\26jbHnu[{BqdiCvb4Xz[UBPUUh|VEOgZ4VtdHN? NHOzcHEyPzR7NEe2Oi=>
human 22Rv cells M17xT2Z2dmO2aX;uJIF{e2G7 M1X2O3Jm\HWldHnvckBw\iCneIDy[ZN{cW:wIH;mJHBVS0hibWLORUBqdiCqdX3hckAzOlK4IHPlcIx{ MVGxO|Q6PDd4Nh?=
mouse NIH3T3 cells NYTUOoFrTnWwY4Tpc44h[XO|YYm= M4T2PFExKM7:TR?= NYXmVWxUUW6qaXLpeIlwdiCxZjDI[YRo\WixZz;HcIkyKG2nZHnheIVlKHS{YX7z[o9zdWG2aX;uJIlvKG2xdYPlJG5KUDOWMzDj[YxteyCjdDCxNEB2VQ>? NGC5fGkyPzR7NEe2Oi=>
mouse MEF cells NIXyRWlHfW6ldHnvckBie3OjeR?= M4HGdXJm\HWldHnvckBqdiCneIDy[ZN{cW:wIH;mJGhm\GenaH;nJJRiemendDDn[Y5mKEircEGgbY4hW3WodTDk[YZq[2mnboSgcY92e2ViTVXGJINmdGy| Mm\NNVc1QTR5Nk[=
HEK293 cells M4TzcGZ2dmO2aX;uJIF{e2G7 M1[1NmlvcGmkaYTpc44hd2ZiYnX0ZUBo[WyjY4Tvd4ll[XOnIHnuJGhGUzJ7MzDj[Yxtew>? MlrlNVc1QTR5Nk[=

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
GLI1 / p-STAT3 / STAT3 / SOCS3 ; 

PubMed: 27275540     

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).

GLI2 / Bcl-2 ; 

PubMed: 25544756     

Western blot analysis of GLI1, GLI2, Bcl-2 and β-actin on LO68 cells treated with 10, 20 or 30 μM GANT61 or vehicle for 24 h.

27275540 25544756

PubMed: 24533083     

(C, D) GANT61 inhibits expression of Gli2 in ovarian cancer cells. ES2 and SKOV3 cells were treated with control vehicle (DMSO) or GANT61 (20 µM) for 48 hr. Subsequently, cells were stained with Gli2 and visualized under a confocal microscope. Scale bar, 10 µm. 

Growth inhibition assay
Cell viability; 

PubMed: 27275540     

Cultivation with GANT61 for 48 hours at different concentrations (2.5, 5, 10, 20μM) inhibited the proliferation of Jurkat, karpass299, and Myla3676 cells in a dose-dependent manner. Viability of these cells were evaluated by CCK-8 assay.

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]


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.
Cell Research:[1]
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  • Cell lines: PANC1 or 22Rv1
  • Concentrations: ~5 μM
  • Incubation Time: 48 h
  • Method: BrdU Incorporation Assay. Subconfluent cells are grown in reduced FBS (2.5%) for 48 h in the presence of 5 μM test compound (or DMSO) on white 96-well plates with clear bottom. Subsequently, cells are labeled for 2 h with BrdU, fixed, and analyzed.
    (Only for Reference)
Animal Research:[1]
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  • Animal Models: BALB/c nude mice with 22Rv1 cell xenograft
  • Formulation: corn oil:ethanol,4:1
  • Dosages: 50 mg/kg
  • Administration: s.c.
    (Only for Reference)

Solubility (25°C)

In vitro Ethanol 12 mg/mL (27.93 mM)
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.

* 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


CAS No. 500579-04-4
Storage powder
in solvent
Synonyms NSC 136476

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID