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GANT 61

Catalog No. T3070 CAS 500579-04-4

Synonyms: NSC 136476, GANT61

GANT 61 (GANT61) is an inhibitor for Gli1 and Gli2.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.

GANT 61, CAS 500579-04-4

Pack Size	Availability	Price/USD
2 mg	In stock	$ 33.00
5 mg	In stock	$ 52.00
10 mg	In stock	$ 81.00
25 mg	In stock	$ 169.00
50 mg	In stock	$ 323.00
100 mg	In stock	$ 453.00
500 mg	In stock	$ 1,050.00
1 mL * 10 mM (in DMSO)	In stock	$ 54.00

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Purity: 100%

Purity: 98.31%

Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	GANT 61 (GANT61) is an inhibitor for Gli1 and Gli2.
Targets&IC50	GLI1:5 μM
In vitro	Nude mice bearing SK-N-AS neuroblastoma xenografts administered orally with 50 mg/kg GANT61 exhibited significant tumor growth inhibition on day 12 of the experiment, achieving a 63% reduction in tumor volume compared to the control group. Additionally, in nude mice injected with GLI1-positive 22Rv1 prostate cancer cells, GANT61 induced tumor regression to the point where no discernible tumors were observed.
In vivo	GANT61 effectively inhibits tumor cell proliferation in vitro through a GLI-dependent mechanism. At a concentration of 30μM, GANT61 halts growth and induces apoptosis in acute myeloid leukemia cells. It exhibits potent cytotoxicity towards human colon cancer cell lines, eradicating colony formation. GANT61 specifically targets chronic lymphocytic leukemia cells over normal B lymphocytes, triggering apoptosis. In the early S phase of human colon cancer cell lines, GANT61 induces DNA replication inhibition leading to DNA damage signaling through the ATM-Chk2 axis and consequent cell death. Furthermore, GANT61 inhibits GLI1's DNA binding capability and suppresses the hedgehog signaling pathway with an IC50 of 5μM, displaying higher selectivity over other pathways (such as TNF signaling/NFκB activation, glucocorticoid receptor gene transcription, and the Ras-Raf-Mek-Mapk cascade).
Kinase Assay	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	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)

Synonyms	NSC 136476, GANT61
Molecular Weight	429.6
Formula	C27H35N5
CAS No.	500579-04-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 21.5 mg/mL (50 mM)

Ethanol: 43 mg/mL (100 mM)

References and Literature

1. Lauth M, et al. Proc Natl Acad Sci, 2007, 104(20), 8455-8560 2. Desch P, et al. Oncogene, 2010, 29(35), 4885-4895. 3. Mazumdar Y, et al. Cancer Res, 2011, 71(3), 1092-1102. 4. Mazumdar T, et al. Cancer Res, 2011,71(17), 5904-5914. 5. Pan D, et al. Leuk Res, 2012, 36(6), 742-748. 6. Zheng H T, Fu T, Zhang H Y, et al. Progesterone-regulated Hsd11b2 as a barrier to balance mouse uterine corticosterone[J]. Journal of Endocrinology. 2020, 244(1): 177-187.

Citations

1. Zheng H T, Fu T, Zhang H Y, et al. Progesterone-regulated Hsd11b2 as a barrier to balance mouse uterine corticosterone. Journal of Endocrinology. 2020, 244(1): 177-187 2. Li B, Yan Y P, He Y Y, et al.IHH, SHH, and primary cilia mediate epithelial-stromal cross-talk during decidualization in mice.Science Signaling.2023, 16(774): eadd0645. 3. Lei X, Li Z, Huang M, et al.Gli1-mediated tumor cell-derived bFGF promotes tumor angiogenesis and pericyte coverage in non-small cell lung cancer.Journal of Experimental & Clinical Cancer Research.2024, 43(1): 1-18.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Obesity Compound Library Anti-Prostate Cancer Compound Library Bioactive Compound Library Bioactive Compounds Library Max Stem Cell Differentiation Compound Library GPCR Compound Library Inhibitor Library NO PAINS Compound Library Autophagy Compound Library Wnt/Hedgehog/Notch Compound Library

Related Products

Related compounds with same targets

Dynarrestin SANT-1 Taladegib Naftifine hydrochloride Sonidegib Cyclopamine Tolnaftate HhAntag

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

GANT 61 500579-04-4 Autophagy GPCR/G Protein Stem Cells Hedgehog/Smoothened NSC 136476 Inhibitor Gli GANT-61 NSC-136476 GANT61 NSC136476 inhibit inhibitor

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