GANT61

Catalog No.S8075 Synonyms: NSC 136476

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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Cited by 20 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.
Targets
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 NETmOGVHfW6ldHnvckBie3OjeR?= NGO4[2dKdmirYnn0bY9vKG:oIFjl[IdmcG:pIIPp[45idGmwZzDpckBpfW2jbjDTbIguVDJiY3XscJMtKEmFNUC9OUDPxE1? NWnINXM6OTd2OUS3OlY>
human Rh30 cells MYTGeY5kfGmxbjDhd5NigQ>? NVjwXlRJOjRiaB?= NWjtcZN4UW6qaXLpeIlwdiCxZjDoeY1idiCJbHmxMY1m\GmjdHXkJJRz[W6|Y4LpdJRqd26jbDDhZ5Rqfmm2eTDpckBpfW2jbjDSbFMxKGOnbHzzJIFnfGW{IEK0JIhzeyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIdmdmViYYPzZZktKEmFNUC9OFAh|ryP NXHTVGprOjB4MEW3NlA>
HEK293 cells NHXNS2pHfW6ldHnvckBie3OjeR?= NF;QSZBT\WS3Y4Tpc44hd2ZiR1zJNkBu\WSrYYTl[EB1emGwc3PybZB1cW:wIHnuJGhGUzJ7MzDj[YxteyCkeTDseYNq\mW{YYPlJJJmeG:{dHXyJIF{e2G7 M1nKS|E4PDl2N{[2
human PANC1 cells MonoSpVv[3Srb36gZZN{[Xl? M3\2N|Uh|ryP MW\S[YR2[3Srb36gbY4hT0yLMTDlfJBz\XO|aX;uJIlvKGi3bXHuJHBCVkNzIHPlcIx{KGG2IEWgeW0> NITsVoMyPzR7NEe2Oi=>
mouse NIH3T3 cells MX3GeY5kfGmxbjDhd5NigQ>? Mk\tTY5pcWKrdHnvckBw\iCJTFmxJIlv\HWlZXSgbIVl\2Wqb3egd4lodmGuaX7nJIlvKG2xdYPlJG5KUDOWMzDj[Yxtew>? M2HG[VE4PDl2N{[2
human 22Rv cells NXzP[WNrTnWwY4Tpc44h[XO|YYm= M4f3d3Jm\HWldHnvckBw\iCneIDy[ZN{cW:wIH;mJHBVS0hibWLORUBqdiCqdX3hckAzOlK4IHPlcIx{ MV6xO|Q6PDd4Nh?=
mouse NIH3T3 cells NEnpe3lHfW6ldHnvckBie3OjeR?= M{G2b|ExKM7:TR?= NWn0cmVxUW6qaXLpeIlwdiCxZjDI[YRo\WixZz;HcIkyKG2nZHnheIVlKHS{YX7z[o9zdWG2aX;uJIlvKG2xdYPlJG5KUDOWMzDj[YxteyCjdDCxNEB2VQ>? M1jmc|E4PDl2N{[2
mouse MEF cells M1PsRmZ2dmO2aX;uJIF{e2G7 MUjS[YR2[3Srb36gbY4h\XiycnXzd4lwdiCxZjDI[YRo\WixZzD0ZZJo\XRiZ3Xu[UBJcXBzIHnuJHN2\nViZHXmbYNq\W62IH3veZNmKE2HRjDj[Yxtew>? MlW5NVc1QTR5Nk[=
HEK293 cells MWHGeY5kfGmxbjDhd5NigQ>? MV3Jcohq[mm2aX;uJI9nKGKndHGg[4Ft[WO2b4Pp[IF{\SCrbjDISWszQTNiY3XscJM> NFjFe5MyPzR7NEe2Oi=>

... Click to View More Cell Line Experimental Data

Assay
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
Immunofluorescence
Gli2; 

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. 

24533083
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.

27275540
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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • 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.
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
Formula

C27H35N5

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