GANT61

Catalog No.S8075 Batch:S807504

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Technical Data

Formula

C27H35N5
Molecular Weight 429.6 CAS No. 500579-04-4
Solubility (25°C)* In vitro Ethanol 16 mg/mL (37.24 mM)
DMSO 5 mg/mL (11.63 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description GANT61 (NSC 136476) 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. This compound induces apoptosis and activates protective autophagy in LX-2 cells.
Targets
GLI1 [1]
(HEK293T cells expressing GLI1)
5 μM
In vitro GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription. This compound inhibits the DNA binding ability of GLI1. It 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. This chemical efficiently inhibited in vitro tumor cell proliferation in a GLI-dependent manner. [1] It induces apoptosis in chronic lymphocytic leukemia cells (CLL), but not in normal B lymphocytes. [2] This compound induces robust cytotoxicity and abolishs the clonogenicity in human colon carcinoma cell lines. [3] It 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] This chemical (30 μM) causes growth arrest and apoptosis in acute myeloid leukemia (AML) cells. [5]
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, this compound 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 (from reference)

Kinase Assay:[1]
  • 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 this compound is 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 Assay:[1]
  • 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.
Animal Study:[1]
  • Animal Models

    BALB/c nude mice with 22Rv1 cell xenograft

  • Dosages

    50 mg/kg

  • Administration

    s.c.

References

  • https://pubmed.ncbi.nlm.nih.gov/17494766/
  • https://pubmed.ncbi.nlm.nih.gov/20603613/
  • https://pubmed.ncbi.nlm.nih.gov/21135115/
  • https://pubmed.ncbi.nlm.nih.gov/21747117/
  • https://pubmed.ncbi.nlm.nih.gov/22398221/
  • https://pubmed.ncbi.nlm.nih.gov/22949014/

Customer Product Validation

<p>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.</p>

, , Oncogene, 2017, 36(13): 1849-1861

<p>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).</p>

, , Oncotarget. 2017, 8(30):48701-48710

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.

Data from [ , , Cell Physiol Biochem, 2016, 38(4):1288-302. ]

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).

Data from [ , , J Exp Clin Cancer Res, 2016, 35(1):184. ]

Selleck's GANT61 Has Been Cited by 106 Publications

The O-glycosyltransferase C1GALT1 promotes EWSR1::FLI1 expression and is a therapeutic target for Ewing sarcoma [ Nat Commun, 2025, 16(1):1267] PubMed: 39894896
Endothelial cell-derived SDF-1α elicits stemness traits of glioblastoma via dual-regulation of GLI1 [ Theranostics, 2025, 15(18):9819-9837] PubMed: 41041071
GPR137-RAB8A activation promotes ovarian cancer development via the Hedgehog pathway [ J Exp Clin Cancer Res, 2025, 44(1):22] PubMed: 39856733
PlexinD1 is a driver and a therapeutic target in advanced prostate cancer [ EMBO Mol Med, 2025, 17(2):336-364] PubMed: 39748059
Sonic Hedgehog potentiates BMP9-induced osteogenic differentiation of mesenchymal stem cells [ Genes Dis, 2025, 12(3):101308] PubMed: 40070367
Impact of Hedgehog modulators on signaling pathways in primary murine and human hepatocytes in vitro: insights into liver metabolism [ Arch Toxicol, 2025, 99(3):1105-1116] PubMed: 39714734
Identification of a distal enhancer regulating hedgehog interacting protein gene in human lung epithelial cells [ EBioMedicine, 2024, 101:105026] PubMed: 38417378
Inhibition of primary cilia-hedgehog signaling axis triggers autophagic cell death and suppresses malignant progression of VHL wild-type ccRCC [ Cell Death Dis, 2024, 15(10):739] PubMed: 39389955
Hedgehog pathway orchestrates the interplay of histone modifications and tailors combination epigenetic therapies in breast cancer [ Acta Pharm Sin B, 2023, 13(6):2601-2612] PubMed: 37425067
Hedgehog pathway orchestrates the interplay of histone modifications and tailors combination epigenetic therapies in breast cancer [ Acta Pharm Sin B, 2023, 13(6):2601-2612] PubMed: 37425067

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.