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.

Size Price Stock Quantity  
USD 147 In stock
USD 570 In stock

Free Overnight Delivery on orders over $ 500
Next day delivery by 10:00 a.m. Order now.

7 Customer Reviews

  • 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, 2016.. 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, 2016. . GANT61 purchased from Selleck.

  • 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.

  • 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.

  • 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

Click to view more

Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 M37ESmZ2dmO2aX;uJIF{e2G7 Mmj3TY5pcWKrdHnvckBw\iCKZXTn[Yhw\yC|aXfuZYxqdmdiaX6gbJVu[W5iU3joMWwzKGOnbHzzMEBKSzVyPUWg{txO MUmxO|Q6PDd4Nh?=
human Rh30 cells MV3GeY5kfGmxbjDhd5NigQ>? Ml;UNlQhcA>? Mn2wTY5pcWKrdHnvckBw\iCqdX3hckBIdGlzLX3l[IlifGWmIITyZY5{[3KrcITpc45idCCjY4Tpeol1gSCrbjDoeY1idiCUaEOwJINmdGy|IHHmeIVzKDJ2IHjyd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHflcoUh[XO|YYmsJGlEPTB;NECg{txO NUDPUGdzOjB4MEW3NlA>
HEK293 cells MVzGeY5kfGmxbjDhd5NigQ>? MXXS[YR2[3Srb36gc4YhT0yLMjDt[YRq[XSnZDD0doFve2O{aYD0bY9vKGmwIFjFT|I6OyClZXzsd{BjgSCudXPp[oVz[XOnIILldI9zfGW{IHHzd4F6 NGfBTYcyPzR7NEe2Oi=>
human PANC1 cells M4f4SmZ2dmO2aX;uJIF{e2G7 NIrUO|k2KM7:TR?= M4LxVnJm\HWldHnvckBqdiCJTFmxJIV5eHKnc4Ppc44hcW5iaIXtZY4hWEGQQ{GgZ4VtdHNiYYSgOUB2VQ>? MYexO|Q6PDd4Nh?=
mouse NIH3T3 cells M3vwW2Z2dmO2aX;uJIF{e2G7 M3PuV2lvcGmkaYTpc44hd2ZiR1zJNUBqdmS3Y3XkJIhm\GenaH;nJJNq\26jbHnu[{BqdiCvb4Xz[UBPUUh|VEOgZ4VtdHN? M1XNR|E4PDl2N{[2
human 22Rv cells NXTGRnJbTnWwY4Tpc44h[XO|YYm= NGDqcoNT\WS3Y4Tpc44hd2ZiZYjwdoV{e2mxbjDv[kBRXEOKIH3SUmEhcW5iaIXtZY4hOjKUdjDj[Yxtew>? Mnj2NVc1QTR5Nk[=
mouse NIH3T3 cells MW\GeY5kfGmxbjDhd5NigQ>? NFjBcZQyOCEQvF2= MWTJcohq[mm2aX;uJI9nKEinZHflbI9oN0euaUGgcYVlcWG2ZXSgeJJidnOob4LtZZRqd25iaX6gcY92e2ViTlnIN3Q{KGOnbHzzJIF1KDFyIIXN NXjRTZlHOTd2OUS3OlY>
mouse MEF cells MmLxSpVv[3Srb36gZZN{[Xl? NXTlPZE2WmWmdXP0bY9vKGmwIHX4dJJme3Orb36gc4YhUGWmZ3Xoc4chfGG{Z3X0JIdmdmViSHnwNUBqdiCVdX\1JIRm\mmlaXXueEBud3W|ZTDNSWYh[2WubIO= MnfmNVc1QTR5Nk[=
HEK293 cells NXf6VlhlTnWwY4Tpc44h[XO|YYm= MlizTY5pcWKrdHnvckBw\iCkZYThJIdidGGldH;zbYRie2ViaX6gTGVMOjl|IHPlcIx{ M2DUNlE4PDl2N{[2

... Click to View More Cell Line Experimental Data

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 <1 mg/mL
Water <1 mg/mL
In vivo 5% DMSO+95% Corn oil 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* 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

Bio Calculators

Molarity Calculator

Molarity Calculator

Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

  • Mass
    Concentration
    Volume
    Molecular Weight

*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

Dilution Calculator

Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

Concentration (start) x Volume (start) = Concentration (final) x Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

  • C1
    V1
    C2
    V2

* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).

The Serial Dilution Calculator Equation

  • Serial Dilutions

  • Computed Result

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
Molecular Weight Calculator

Molecular Weight Calculator

Enter the chemical formula of a compound to calculate its molar mass and elemental composition:

Total Molecular Weight: g/mol

Tip: Chemical formula is case sensitive. C10H16N2O2 c10h16n2o2

Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter its chemical formula and click 'Calculate'.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

  • * Indicates a Required Field

Hedgehog/Smoothened Signaling Pathway Map

Related Hedgehog/Smoothened Products

Tags: buy GANT61 | GANT61 supplier | purchase GANT61 | GANT61 cost | GANT61 manufacturer | order GANT61 | GANT61 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID