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GANT61

Cat. No. M2448
GANT61 Structure
Synonym:

NSC 136476

Size Price Availability Quantity
10mg USD 90 In stock
50mg USD 350 In stock
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Quality Control
Biological Activity

GANT61 is an inhibitor for GLI1 as well as GLI2-induced transcription, inhibits hedgehog with IC50 of 5 μM, displays selectivity over other pathways, such as TNF and glucocorticoid receptor gene transactivation. 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. 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.

Protocol
Cell Experiment
Cell lines HEK293 cells
Preparation method HEK293 cells were transfected with GLI1 expression plasmid, together with the reporter plasmids 12xGliBS-Luc and R-Luc on 10-cm plates (day 0). Twenty-four hours later, cells were seeded in white 96-well plates with clear bottom at a density of 15,000 cells per well. Cells were allowed to attach, and compounds (Diversity Set, 1990 compounds; National Cancer Institute, Bethesda, MD) were added at a final concentration of 10 μM in DMSO (0.5% final DMSO concentration) (day 1.5). Cells were grown for another 24 h, subsequently lysed, and then analyzed by using the Dual Luciferase kit (Promega, Madison, WI). Plates were read on a Berthold Technologies (Bad Wildbad, Germany) microplate luminometer.
Concentrations 10 μM
Incubation time 24 h
Animal Experiment
Animal models 22Rv1 cells xenograft in female BALB/c nude mice (nu/nu)
Formulation corn oil:ethanol, 4:1
Dosages 50 mg/kg for 16 days
Administration s.c. injections
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 429.6
Formula C27H35N5
CAS Number 500579-04-4
Purity 100.00%
Solubility DMSO
Storage at -20°C
References

GANT-61 inhibits pancreatic cancer stem cell growth in vitro and in NOD/SCID/IL2R gamma null mice xenograft.
Fu J, et al. Cancer Lett. 2013 Mar 1;330(1):22-32. PMID: 23200667.

Targeting the hedgehog signal transduction pathway at the level of GLI inhibits neuroblastoma cell growth in vitro and in vivo.
Wickström M, et al. Int J Cancer. 2013 Apr 1;132(7):1516-24. PMID: 22949014.

Hedgehog signaling drives cellular survival in human colon carcinoma cells.
Mazumdar T, et al. Cancer Res. 2011 Feb 1;71(3):1092-102. PMID: 21135115.

Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists.
Lauth M, et al. Proc Natl Acad Sci U S A. 2007 May 15;104(20):8455-60. PMID: 17494766.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GANT61, NSC 136476 supplier, Hedgehog, inhibitors

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