GANT 61
Based on 67 publication(s) in Google Scholar
GANT 61 is an inhibitor of Gli1 and Gli2 targeting the Hedgehog/GLI pathway.
For research use only. We do not sell to patients.
- Purity: 99.80%
- CAS No.: 500579-04-4
- Formula: C27H35N5
- Molecular Weight:429.60
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Publications Citing Use of MedChemExpress (MCE) GANT 61
More- Cell Res. 2022 Mar;32(3):288-301. [Abstract]
- Blood. 2016 Dec 8;128(23):2642-2654. [Abstract]
- Nat Commun. 2023 Jun 24;14(1):3766. [Abstract]
- Nat Commun. 2017 Jun 12;8:15773 [Abstract]
- Cell Death Differ. 2021 Jul;28(7):2221-2237. [Abstract]
- J Clin Invest. 2020 Dec 1;130(12):6354-6365. [Abstract]
- J Exp Clin Cancer Res. 2020 Jan 28;39(1):22. [Abstract]
- Sci Adv. 2025 Jan 10;11(2):eads5434. [Abstract]
- J Hazard Mater. 2023 Oct 15:460:132489. [Abstract]
- Cell Rep Med. 2025 Sep 19:102357. [Abstract]
- Cancer Lett. 2018 Apr 28:420:195-207. [Abstract]
- Cancer Lett. 2017 Jan 28:385:128-136. [Abstract]
- Cell Commun Signal. 2024 Feb 15;22(1):123. [Abstract]
- Phytomedicine. 2022 Apr:98:153972. [Abstract]
- ACS Appl Mater Interfaces. 2021 Aug 4;13(30):35248-35265. [Abstract]
- ACS Appl Mater Interfaces. 2017 Dec 13;9(49):42544-42555. [Abstract]
- Br J Pharmacol. 2021 Sep;178(17):3428-3447. [Abstract]
- Biomed Pharmacother. 2025 Nov 6:193:118716. [Abstract]
- Biomed Pharmacother. 2025 Aug 11:191:118435. [Abstract]
- J Transl Med. 2022 Jun 25;20(1):286. [Abstract]
- Stem Cell Res Ther. 2024 Jul 6;15(1):198. [Abstract]
- Stem Cell Res Ther. 2019 Jul 5;10(1):198. [Abstract]
- Cell Rep. 2025 Dec 24;45(1):116797.
- Cell Rep. 2020 Apr.
- Ecotoxicol Environ Saf. 2025 Aug 6:303:118813. [Abstract]
- Cell Prolif. 2021 May;54(5):e13026. [Abstract]
- Cell Proliferat. 2020 May;53(5):e12810. [Abstract]
- J Am Heart Assoc. 2022 Sep 14;e026365. [Abstract]
- Life Sci. 2017 Dec 15:191:82-89. [Abstract]
- Cell Oncol (Dordr). 2023 Apr;46(2):437-450. [Abstract]
- Front Pharmacol. 2018 Jun 26:9:674. [Abstract]
- Int Immunopharmacol. 2025 Mar 24:153:114538. [Abstract]
- Cancer Sci. 2017 May;108(5):918-930. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2023 Nov 16;1870(2):166961. [Abstract]
- J Cell Mol Med. 2021 Jul;25(13):6280-6288. [Abstract]
- FEBS J. 2021 Jun;288(11):3530-3546. [Abstract]
- J Cell Commun Signal. 2025 Sep 3;19(3):e70030. [Abstract]
- Oncol Rep. 2020 Dec;44(6):2610-2620. [Abstract]
- Oncol Rep. 2019 May;41(5):2689-2702. [Abstract]
- Heliyon. 2024 Aug 17;10(16):e36516. [Abstract]
- Stem Cells. 2020 Feb;38(2):261-275. [Abstract]
- Med Oncol. 2025 Mar 11;42(4):98. [Abstract]
- Toxicol Appl Pharmacol. 2020 Jan 15;387:114853. [Abstract]
- Stem Cells Int. 2021 Aug 12:2021:8138374. [Abstract]
- Environ Toxicol. 2021 Feb;36(2):194-203. [Abstract]
- Cancer Med. 2018 Nov;7(11):5704-5715. [Abstract]
- Breast Cancer. 2017 Sep;24(5):683-693. [Abstract]
- Mol Pain. 2025 Jan-Dec:21:17448069251376198. [Abstract]
- Int J Biochem Cell Biol. 2025 Oct:187:106840. [Abstract]
- Brain Sci. 2021 Jan 8;11(1):77. [Abstract]
- Asian J Androl. 2018 Nov-Dec;20(6):608-614. [Abstract]
- Prostate. 2020 Nov;80(15):1328-1340. [Abstract]
- Ann Hematol. 2026 Jan 23;105(2):54. [Abstract]
- Steroids. 2024 Jun:206:109421. [Abstract]
- Biochim Biophys Acta Gen Subj. 2026 Jan;1870(1):130875. [Abstract]
- Biochem Bioph Res Co. 2020 Dec 17;533(4):770-778. [Abstract]
- Cancer Biother Radiopharm. 2021 Dec 31. [Abstract]
- Chemotherapy. 2022;67(2):57-66. [Abstract]
- Int J Pharmacol. 2020 Jan.
- Res Sq. 2024 Oct 16.
- Research Square Print. 2023 Feb 17.
- Hong Kong Polytechnic University. 2022 Feb.
- Research Square Preprint. 2021 Sep.
- Mech Dev. 2018 Dec:154:219-239. [Abstract]
- Chinese Pharmacological Bulletin. 2018, 34(9): 1235-1242.
- University of Colorado. 2016 Aug.
- Oncotarget. 2015 Nov 3;6(34):36700-12. [Abstract]
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WB
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WB
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Cell Proliferation/Viability Assay
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WB
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Biological Activity
Gli1/2[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
6.83 μM
Compound: GANT61
|
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
|
[PMID: 29624387] |
| IMR-32 | GI50 |
5.82 μM
Compound: 32, GANT-61
|
Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay
Cytotoxicity against human IMR32 cells after 72 hrs by fluorometric microculture cytotoxicity assay
|
10.1039/C3MD00334E |
| NIH3T3 | EC50 |
5 μM
Compound: 4; GANT-61
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Inhibition of Hh signaling pathway in Shh-LIGHT2 incorporated mouse NIH 3T3 cells assessed as downregulation of Gli1 gene expression by luciferase reporter gene assay
Inhibition of Hh signaling pathway in Shh-LIGHT2 incorporated mouse NIH 3T3 cells assessed as downregulation of Gli1 gene expression by luciferase reporter gene assay
|
[PMID: 26976215] |
| Shh Light II | IC50 |
5 μM
Compound: 128, GANT61
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Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
Inhibition of SHH in mouse Shh Light2 cells by GLI-responsive firefly luciferase reporter gene assay
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[PMID: 19309080] |
| SH-SY5Y | GI50 |
5.82 μM
Compound: 32, GANT-61
|
Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay
Cytotoxicity against human SH-SY5Y cells after 72 hrs by fluorometric microculture cytotoxicity assay
|
10.1039/C3MD00334E |
| SK-N-AS | GI50 |
5.82 μM
Compound: 32, GANT-61
|
Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay
Cytotoxicity against human SK-N-AS cells after 72 hrs by fluorometric microculture cytotoxicity assay
|
10.1039/C3MD00334E |
| SK-N-DZ | GI50 |
5.82 μM
Compound: 32, GANT-61
|
Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay
Cytotoxicity against human SK-N-DZ cells after 72 hrs by fluorometric microculture cytotoxicity assay
|
10.1039/C3MD00334E |
| SK-N-FI | GI50 |
5.82 μM
Compound: 32, GANT-61
|
Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay
Cytotoxicity against human SK-N-FI cells after 72 hrs by fluorometric microculture cytotoxicity assay
|
10.1039/C3MD00334E |
| SK-N-SH | GI50 |
5.82 μM
Compound: 32, GANT-61
|
Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay
Cytotoxicity against human SK-N-SH cells after 72 hrs by fluorometric microculture cytotoxicity assay
|
10.1039/C3MD00334E |
GANT61 (20 μM) induces greater cell death than targeting Smo (cyclopamine). GANT61 (0, 5, 10, 20 μM) inhibits clonogenic survival of human colon carcinoma cell lines. GANT61 (20 μM, 0-72 hr) down-regulates Gli1 and Gli2 expression in HT29 cells. GANT61 (0, 10 μM or 20 μM) differentially regulates genes involved in the balance between cell death and cell survival[1]. GANT-61 inhibits cell viability and induces apoptosis in pancreatic CSCs. GANT-61 inhibits expression of downstream targets of Shh pathway, decreases Gli-DNA interaction, Gli transcriptional activity and Gli nuclear translocation in pancreatic CSCs. GANT-61 differentially regulates genes involved in cell survival, cell death and pluripotency. GANT-61 inhibits motility, invasion and migration of CSCs[2]. GANT61 sensitivity positively correlates to GLI1 and negatively to MYCN expression in the neuroblastoma cell lines tested. GANT61 downregulates GLI1, c-MYC, MYCN and Cyclin D1 expression and induces apoptosis of neuroblastoma cells[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 500579-04-4
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Appearance Solid
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Molecular Weight 429.60
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Formula C27H35N5
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Color White to light yellow
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SMILES
CN(C)C1=CC=CC=C1CN2C(C3=CC=NC=C3)N(CC4=CC=CC=C4N(C)C)CCC2
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Synonyms
NSC 136476
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (67)
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Journal Impact Factor
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Most Recent
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Cell Res
Cholesterylation of Smoothened is a calcium-accelerated autoreaction involving an intramolecular ester intermediate. [Abstract]2022 Mar;32(3):288-301. PMID: 35121857 -
Blood
Hedgehog pathway activation in T-cell acute lymphoblastic leukemia predicts response to SMO and GLI1 inhibitors. [Abstract]2016 Dec 8;128(23):2642-2654. PMID: 27694322 -
Nat Commun
Hedgehog signaling via its ligand DHH acts as cell fate determinant during skeletal muscle regeneration. [Abstract]2023 Jun 24;14(1):3766. PMID: 37355632 -
Nat Commun
EMT cells increase breast cancer metastasis via paracrine GLI activation in neighbouring tumour cells. [Abstract]2017 Jun 12;8:15773 PMID: 28604738 -
Cell Death Differ
Constitutive GLI1 expression in chondrosarcoma is regulated by major vault protein via mTOR/S6K1 signaling cascade. [Abstract]2021 Jul;28(7):2221-2237. PMID: 33637972 -
J Clin Invest
Tendon-derived cathepsin K-expressing progenitor cells activate Hedgehog signaling to drive heterotopic ossification. [Abstract]2020 Dec 1;130(12):6354-6365. PMID: 32853181 -
J Exp Clin Cancer Res
Hedgehog signaling promotes sorafenib resistance in hepatocellular carcinoma patient-derived organoids. [Abstract]2020 Jan 28;39(1):22. PMID: 31992334 -
Sci Adv
Noncanonical UPR factor CREB3L2 drives immune evasion of triple-negative breast cancer through Hedgehog pathway modulation in T cells. [Abstract]2025 Jan 10;11(2):eads5434. PMID: 39792663 -
J Hazard Mater
Fibroblast-derived CXCL14 aggravates crystalline silica-induced pulmonary fibrosis by mediating polarization and recruitment of interstitial macrophages. [Abstract]2023 Oct 15:460:132489. PMID: 37688871 -
Cell Rep Med
Drug screening in 3D microtumors reveals DDR1/2-MAPK12-GLI1 as a vulnerability in cancer-associated fibroblasts. [Abstract]2025 Sep 19:102357. PMID: 40975064 -
Cancer Lett
Cynanbungeigenin C and D, a pair of novel epimers from Cynanchum bungei, suppress hedgehog pathway-dependent medulloblastoma by blocking signaling at the level of Gli. [Abstract]2018 Apr 28:420:195-207. PMID: 29425683
GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2018 Apr 28:420:195-207. [Abstract]
Shh-Light 2 cells are transfected with Gli1 or Gli2 plasmids and the expression of proteins are analyzed by Western blot. Positive control JQ1, CBC and CBD inhibit Gli1 and Gli2 overexpression induced Gli luciferase activity, GDC-0499 and GANT61 have no effects.
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Cancer Lett
Anti-proliferation of breast cancer cells with itraconazole: Hedgehog pathway inhibition induces apoptosis and autophagic cell death. [Abstract]2017 Jan 28:385:128-136. PMID: 27810405
GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2017 Jan 28:385:128-136. [Abstract]
GANT61 or SHH siRNA treatment alone moderately increases LC3-II, and LC3-II increased in cells co-treated with R51211 and GANT61 or SHH siRNA.
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Cell Commun Signal
TGFβ1-induced hedgehog signaling suppresses the immune response of brain microvascular endothelial cells elicited by meningitic Escherichia coli. [Abstract]2024 Feb 15;22(1):123. PMID: 38360663 -
Phytomedicine
Suppression of colitis-associated colorectal cancer by scutellarin through inhibiting Hedgehog signaling pathway activity. [Abstract]2022 Apr:98:153972. PMID: 35151214 -
ACS Appl Mater Interfaces
Peptide-Targeted High-Density Lipoprotein Nanoparticles for Combinatorial Treatment against Metastatic Breast Cancer. [Abstract]2021 Aug 4;13(30):35248-35265. PMID: 34284582 -
ACS Appl Mater Interfaces
ATG101 Single-Stranded Antisense RNA-Loaded Triangular DNA Nanoparticles Control Human Pulmonary Endothelial Growth via Regulation of Cell Macroautophagy. [Abstract]2017 Dec 13;9(49):42544-42555. PMID: 29154530
GANT 61 purchased from MedChemExpress. Usage Cited in: ACS Appl Mater Interfaces. 2017 Dec 13;9(49):42544-42555. [Abstract]
ATG101 cross-talk with the hedgehog pathway modulates hypoxia-induced HPAEC cell proliferation and apoptosis. Effects of ssATG101-TNP on the hedgehog pathway. HPAECs are pretreated with ssATG101-TNP and GANT61; then, they are under hypoxia for 24 h.
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Br J Pharmacol
Physalin B attenuates liver fibrosis via suppressing LAP2α-HDAC1-mediated deacetylation of the transcription factor GLI1 and hepatic stellate cell activation. [Abstract]2021 Sep;178(17):3428-3447. PMID: 33864382 -
Biomed Pharmacother
Drug target proteome profiling identifies HES1-driven mitotic catastrophe in ovarian serous carcinoma. [Abstract]2025 Nov 6:193:118716. PMID: 41202420 -
Biomed Pharmacother
Amentoflavone inhibits colorectal tumor growth, stemness, and metastasis, prolonging survival through GLI-1/IL6/STAT3 axis targeting. [Abstract]2025 Aug 11:191:118435. PMID: 40795472 -
J Transl Med
Combined treatment with inhibitors of ErbB Receptors and Hh signaling pathways is more effective than single treatment in reducing the growth of malignant mesothelioma both in vitro and in vivo. [Abstract]2022 Jun 25;20(1):286. PMID: 35752861 -
Stem Cell Res Ther
Distraction force promotes the osteogenic differentiation of Gli1+ cells in facial sutures via primary cilia-mediated Hedgehog signaling pathway. [Abstract]2024 Jul 6;15(1):198. PMID: 38971766 -
Stem Cell Res Ther
Hedgehog pathway inhibition causes primary follicle atresia and decreases female germline stem cell proliferation capacity or stemness. [Abstract]2019 Jul 5;10(1):198. PMID: 31277696 -
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Ecotoxicol Environ Saf
Zearalenone at environmental levels promoted ER- positive breast cancer cell lines through the hedgehog pathway. [Abstract]2025 Aug 6:303:118813. PMID: 40773915 -
Cell Prolif
Periodontitis-compromised dental pulp stem cells secrete extracellular vesicles carrying miRNA-378a promote local angiogenesis by targeting Sufu to activate the Hedgehog/Gli1 signalling. [Abstract]2021 May;54(5):e13026. PMID: 33759282 -
Cell Proliferat
Mechanosensing by Gli1+ cells contributes to the orthodontic force-induced bone remodelling. [Abstract]2020 May;53(5):e12810. PMID: 32472648 -
J Am Heart Assoc
Intact Fibroblast Growth Factor 23 Regulates Chronic Kidney Disease-Induced Myocardial Fibrosis by Activating the Sonic Hedgehog Signaling Pathway. [Abstract]2022 Sep 14;e026365. PMID: 36102251 -
Life Sci
Knockdown of HIF-1α inhibits the proliferation and migration of outer root sheath cells exposed to hypoxia in vitro: An involvement of Shh pathway. [Abstract]2017 Dec 15:191:82-89. PMID: 29030089
GANT 61 purchased from MedChemExpress. Usage Cited in: Life Sci. 2017 Dec 15:191:82-89. [Abstract]
ORS cells are exposed to 3% oxygen for 48 h in presence or absence of Shh pathway inhibitor cyclopamine (5 μM) or GANT61 (10 μM). Immunofluorescence assay using anti-PCNA antibody is performed to detect the proliferative ORS cells (red). Cell nuclei are counterstained with DAPI (blue).
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Cell Oncol (Dordr)
Reciprocal FGF19-GLI2 signaling induces epithelial-to-mesenchymal transition to promote lung squamous cell carcinoma metastasis. [Abstract]2023 Apr;46(2):437-450. PMID: 36598638 -
Front Pharmacol
Epigallocatechin-3-Gallate Promotes the Growth of Mink Hair Follicles Through Sonic Hedgehog and Protein Kinase B Signaling Pathways. [Abstract]2018 Jun 26:9:674. PMID: 29997505
GANT 61 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2018 Jun 26:9:674. [Abstract]
Cyclopamine and GANT61 decrease the level of Gli1 as evidenced by western blot.
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Int Immunopharmacol
USP22/BRD4 mediated hedgehog pathway activation contributes to airway remodeling in asthma. [Abstract]2025 Mar 24:153:114538. PMID: 40132456 -
Cancer Sci
Anti-cancer stem cell activity of a hedgehog inhibitor GANT61 in estrogen receptor-positive breast cancer cells. [Abstract]2017 May;108(5):918-930. PMID: 28211214
GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2017 May;108(5):918-930. [Abstract]
Effects of E2 and GANT61 on the protein expression levels of GLI1 and GLI2 in MCF-7 cells. The expression levels are measured with a western blotting as described in the Materials and Methods.
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Biochim Biophys Acta Mol Basis Dis
The sonic hedgehog pathway suppresses oxidative stress and senescence in nucleus pulposus cells to alleviate intervertebral disc degeneration via GPX4. [Abstract]2023 Nov 16;1870(2):166961. PMID: 37979732 -
J Cell Mol Med
2021 Jul;25(13):6280-6288. PMID: 34076957 -
FEBS J
Alveolar epithelial cell-derived Sonic hedgehog promotes pulmonary fibrosis through OPN-dependent alternative macrophage activation. [Abstract]2021 Jun;288(11):3530-3546. PMID: 33314622 -
J Cell Commun Signal
Epigenetic regulation of breast ductal carcinoma in situ by miR-217 through DNMT1 and Hedgehog-GLI pathway. [Abstract]2025 Sep 3;19(3):e70030. PMID: 40909350 -
Oncol Rep
The Hedgehog signaling pathway promotes chemotherapy resistance via multidrug resistance protein 1 in ovarian cancer. [Abstract]2020 Dec;44(6):2610-2620. PMID: 33125122 -
Oncol Rep
Combination of phospholipase Cε knockdown with GANT61 sensitizes castration‑resistant prostate cancer cells to enzalutamide by suppressing the androgen receptor signaling pathway. [Abstract]2019 May;41(5):2689-2702. PMID: 30864728 -
Heliyon
Hedgehog/Gli2 signaling triggers cell proliferation and metastasis via EMT and wnt/β-catenin pathways in oral squamous cell carcinoma. [Abstract]2024 Aug 17;10(16):e36516. PMID: 39253258 -
Stem Cells
CD10 expression identifies a subset of human perivascular progenitor cells with high proliferation and calcification potentials. [Abstract]2020 Feb;38(2):261-275. PMID: 31721342 -
Med Oncol
FBXO32 ubiquitination of SUFU promotes progression and lenvatinib resistance in hepatocellular carcinoma via hedgehog signaling. [Abstract]2025 Mar 11;42(4):98. PMID: 40067532 -
Toxicol Appl Pharmacol
Gant61 ameliorates CCl4-induced liver fibrosis by inhibition of Hedgehog signaling activity. [Abstract]2020 Jan 15;387:114853. PMID: 31816328 -
Stem Cells Int
Gli1+ Cells Residing in Bone Sutures Respond to Mechanical Force via IP3R to Mediate Osteogenesis. [Abstract]2021 Aug 12:2021:8138374. PMID: 34434241 -
Environ Toxicol
2021 Feb;36(2):194-203. PMID: 32996673 -
Cancer Med
Dihydroartemisinin induces apoptosis and inhibits proliferation, migration, and invasion in epithelial ovarian cancer via inhibition of the hedgehog signaling pathway. [Abstract]2018 Nov;7(11):5704-5715. PMID: 30338663
GANT 61 purchased from MedChemExpress. Usage Cited in: Cancer Med. 2018 Nov;7(11):5704-5715. [Abstract]
The Hh signaling pathway is involved in DHA induced inhibition of cell proliferation. A and B, CCK8 assay of SKOV3 and SKOV3-IP cells is conducted following treatment with purmorphamine, DHA or a combination of DHA and purmorphamine for 48 h. C and D, SKOV3 and SKOV3‐IP cells are treated with GANT61, DHA, or a combination of DHA and GATN61 for 48 h, while controls are treated with DMSO. CCK8 assay is used to analyze cell viability of SKOV3 and SKOV3-IP cells.
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Breast Cancer
Anti-cell growth and anti-cancer stem cell activities of the non-canonical hedgehog inhibitor GANT61 in triple-negative breast cancer cells. [Abstract]2017 Sep;24(5):683-693. PMID: 28144905
GANT 61 purchased from MedChemExpress. Usage Cited in: Breast Cancer. 2017 Sep;24(5):683-693. [Abstract]
Effects of GANT61 (0-20μM) on the expression levels of survivin in MDA-MB-231 cells. The cells are treated with the indicated concentrations of GANT61 for two days. The expression levels are tested using western blotting. The deduced molecular weight of surviving is approximately 16 kDa.
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Mol Pain
Inhibition of mTOR/S6K1/Gli1 signaling alleviates morphine-induced thermal hyperalgesia and tolerance. [Abstract]2025 Jan-Dec:21:17448069251376198. PMID: 40968661 -
Int J Biochem Cell Biol
Substrate stiffness modulates osteogenic differentiation of BMMSCs via the hedgehog signaling pathway. [Abstract]2025 Oct:187:106840. PMID: 40712834 -
Brain Sci
Astrocyte-Derived TGFβ1 Facilitates Blood-Brain Barrier Function via Non-Canonical Hedgehog Signaling in Brain Microvascular Endothelial Cells. [Abstract]2021 Jan 8;11(1):77. PMID: 33430164 -
Asian J Androl
Muscarinic acetylcholine receptor M1 mediates prostate cancer cell migration and invasion through hedgehog signaling. [Abstract]2018 Nov-Dec;20(6):608-614. PMID: 30027929 -
Prostate
β2 -adrenergic receptor signaling drives prostate cancer progression by targeting the Sonic hedgehog-Gli1 signaling activation. [Abstract]2020 Nov;80(15):1328-1340. PMID: 32894788 -
Ann Hematol
GANT61 suppresses proliferation and induces apoptosis in ALK-Positive anaplastic large cell lymphoma via modulating the Hh-PIK3IP1-Akt signaling axis. [Abstract]2026 Jan 23;105(2):54. PMID: 41571844 -
Steroids
CBC-1 as a Cynanbungeigenin C derivative inhibits the growth of colorectal cancer through targeting Hedgehog pathway component GLI 1. [Abstract]2024 Jun:206:109421. PMID: 38614233 -
Biochim Biophys Acta Gen Subj
Hyperglycemia accelerated the metastasis of triple-negative breast cancer via promoting TNFα/Gli-1 axis in endothelial cells. [Abstract]2026 Jan;1870(1):130875. PMID: 41183624 -
Biochem Bioph Res Co
Microcystin-leucine-arginine induces liver fibrosis by activating the Hedgehog pathway in hepatic stellate cells. [Abstract]2020 Dec 17;533(4):770-778. PMID: 32988585 -
Cancer Biother Radiopharm
A Noncanonical Hedgehog Signaling Exerts a Tumor-Promoting Effect on Pancreatic Cancer Cells Via Induction of Osteopontin Expression. [Abstract]2021 Dec 31. PMID: 34978897 -
Chemotherapy
miR-142-3p Regulates Tumor Cell Autophagy and Promotes Colon Cancer Progression by Targeting TP53INP2. [Abstract]2022;67(2):57-66. PMID: 34753133 -
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Mech Dev
2018 Dec:154:219-239. PMID: 30086335 -
GANT 61 purchased from MedChemExpress. Usage Cited in: Chinese Pharmacological Bulletin. 2018, 34(9): 1235-1242.
Expression of Gli1/2 (A) and DNA damage proteins (B) at OGD 6 h detected by Western blot.
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GANT 61 purchased from MedChemExpress. Usage Cited in: University of Colorado. 2016 Aug.
Western blot analyses of whole cell lysates (WCLs) collected from MCF7-Ctrl cells cultured in MCF7-Ctrl and Six1 CM for 48 hrs treated with GANT61 or vehicle.
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Oncotarget
INSM1 increases N-myc stability and oncogenesis via a positive-feedback loop in neuroblastoma. [Abstract]2015 Nov 3;6(34):36700-12. PMID: 26456864
GANT 61 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Nov 3;6(34):36700-12. [Abstract]
BE2-M17 NB cells are incubated with GANT-61 (0–40 μM) for 3 days. The cell viability is monitored using an MTS assay. The expression levels of N-myc and INSM1 in the cells treated with 20 μM of GANT-61 is determined by Western blot analysis. Actin is used as a loading control.
Solvent & Solubility
Ethanol : 66.67 mg/mL (155.19 mM; Need ultrasonic)
DMSO : 25 mg/mL (58.19 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: 5 mg/mL (11.64 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.82 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.82 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
Cells (1.5×104) are incubated with 0, 1, 5 and 10 μM of GANT-61 in 250 μL of culture medium in 96-well plate for 48 and 72 h. Cell viability is determined by the XTT assay. In brief, a freshly prepared XTT-PMS labeling mixture (50 μL) is added to the cell culture. The absorbance is measured at 450 nm with λ correction at 650 nm. The cell viability is expressed as ΔOD (OD450 − OD650). The apoptosis is determined by FACS analysis of propidium iodide (PI)-stained cells. In brief, cells are trypsinized, washed with PBS and resuspended in 200 μL PBS with 10 μL RNAase (10 mg/mL) and incubated at 37°C for 30 min. After incubation, 50 μL PI solution is added and cells are analyzed for apoptosis using a flow cytometry.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Humanized NOD/SCID/IL2Rgammanull mice are used for the assay. Before CSC’s injection, mice are humanized with tail vein injection of human normal CD34+ peripheral blood stem/progenitor cells. CD34+peripheral blood stem/progenitor cells (500 cells/mouse, 50-75 μL volume) are injected through tail vein. After 3 days, human pancreatic CSCs (1×103 cells mixed with Matrigel, Becton Dickinson, Bedford, MA, in 75 μL total volume, 50:50 ratio) are injected subcutaneously into the flanks of NOD/SCID IL2Rγnull mice (4–6 weeks old). After two weeks of CSC implantation, mice (10 mice per group) are treated with GANT-61(0 and 40 mg/kg body weight) ip three times per week for 6 weeks. At the end of the experiment, mice are euthanized, and tumors are isolated for biochemical analysis.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Mazumdar T, et al. Hedgehog signaling drives cellular survival in human colon carcinoma cells. Cancer Res. 2011 Feb 1;71(3):1092-102. [Content Brief]
[2]. Fu J, et al. GANT-61 inhibits pancreatic cancer stem cell growth in vitro and in NOD/SCID/IL2R gamma null mice xenograft. Cancer Lett. 2013 Mar 1;330(1):22-32. [Content Brief]
[3]. Wickstrom M, et al. Targeting the hedgehog signal transduction pathway at the level of GLI inhibits neuroblastoma cell growth in vitro and in vivo. Int J Cancer. 2013 Apr 1;132(7):1516-24. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 2.3277 mL | 11.6387 mL | 23.2775 mL | 58.1937 mL |
| 5 mM | 0.4655 mL | 2.3277 mL | 4.6555 mL | 11.6387 mL | |
| 10 mM | 0.2328 mL | 1.1639 mL | 2.3277 mL | 5.8194 mL | |
| 15 mM | 0.1552 mL | 0.7759 mL | 1.5518 mL | 3.8796 mL | |
| 20 mM | 0.1164 mL | 0.5819 mL | 1.1639 mL | 2.9097 mL | |
| 25 mM | 0.0931 mL | 0.4655 mL | 0.9311 mL | 2.3277 mL | |
| 30 mM | 0.0776 mL | 0.3880 mL | 0.7759 mL | 1.9398 mL | |
| 40 mM | 0.0582 mL | 0.2910 mL | 0.5819 mL | 1.4548 mL | |
| 50 mM | 0.0466 mL | 0.2328 mL | 0.4655 mL | 1.1639 mL | |
| Ethanol | 60 mM | 0.0388 mL | 0.1940 mL | 0.3880 mL | 0.9699 mL |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2910 mL | 0.7274 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.5819 mL |