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GNT61

(CAS No:500579-04-4)
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.
CAS No:500579-04-4
Molecular Weight(MW):429.6
Purity:98%+
Specification:500mg;1g;5g;10g;50g;100g
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QC Documents
 COA  MSDS  HPLC  NMR
ChemicalInfomation
CAS No: 500579-04-4
Molecular formula(MF) C27H35N5
Molecular Weight(MW): 429.6
Alias
Solubility
In vitro Ethanol 12 mg/mL (27.93 mM)
DMSO <1 mg/mL
Water <1 mg/mL
In vivo 20% ethanol+80% corn oil 40mg/mL
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 Function assay Inhibition of Hedgehog signaling in human Shh-L2 cells, IC50=5 μM 17494766
human Rh30 cells Function assay 24 h Inhibition of human Gli1-mediated transcriptional activity in human Rh30 cells after 24 hrs by luciferase reporter gene assay, IC50=40 μM 20605720
HEK293 cells Function assay Reduction of GLI2 mediated transcription in HEK293 cells by luciferase reporter assay 17494766
human PANC1 cells Function assay 5 μM Reduction in GLI1 expression in human PANC1 cells at 5 uM 17494766
mouse NIH3T3 cells Function assay Inhibition of GLI1 induced hedgehog signaling in mouse NIH3T3 cells 17494766
human 22Rv cells Function assay Reduction of expression of PTCH mRNA in human 22Rv cells 17494766
mouse NIH3T3 cells Function assay 10 μM Inhibition of Hedgehog/Gli1 mediated transformation in mouse NIH3T3 cells at 10 uM 17494766
mouse MEF cells Function assay Reduction in expression of Hedgehog target gene Hip1 in Sufu deficient mouse MEF cells 17494766
HEK293 cells Function assay Inhibition of beta galactosidase in HEK293 cells 17494766

... 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]