Toggle Nav

GANT 58

In stock
Catalog No.
A3429
GLI antagonist,novel and potent
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$61.00
In stock
5mg
$51.00
In stock
10mg
$81.00
In stock
50mg
$288.00
In stock
100mg
$420.00
In stock

Tel: +1-832-696-8203

Email: [email protected]

Worldwide Distributors

Background

GANT 58 is an antagonist of GLI that inhibits GLI1-induced transcription with an IC50 value of 5 μM [1].

GLI1 is a human glioblastoma isolated protein which belongs to GLI protein family. GLI proteins act as effectors in Hedgehog signaling pathway and get involved in cell proliferation, determination and patterning during embryo development.

GANT 58 is considered to inhibit GLI1-mediated gene trans-activation with a high selectivity for Hedgehog signaling pathway. When TNF signaling/NFkB activation, glucocorticoid, receptor gene transactivation, and the Ras-Raf-Mek-Mapk cascade were treated with GANT 58, no inhibition was observed. When SAG-treated shh-L2 cells were treated with 10 μM GANT 58 for 48 hr, the reduction of Hedgehog pathway signaling was observed, whereas Gli1 mRNA level reduction was induced by the treatment of 10 μM GANT 58 for 2-3 days. Indeed, GANT 58 was confirmed as inhibitor of Hedgehog signaling pathway downstream Sufu and Smo [1]. Furthermore, GANT 58 treatments for 48 hr resulted in the significant reduction of cell viability in a dose-dependent manner for CCRFeCEM, CEM7e14, CEM1e15 and Jurkat cells. When CCRFeCEM cells were treated with 10 μM GANT 58 for 48 hr, the percentage of cells in G1/S phase increased whereas the percentage in G2/M phase decreased [2].

In mouse model with xenograft, daily s.c. injection of GANT 58 resulted in significant suppression of tumor cell growth. 50 mg/kg/d GANT 58 injections for 18 days induced the suppression of additional xenograft growth and restrict the increase of tumor size. No side effects were observed during the treatment [1].

References:
[1] Lauth M, Bergstr?m ?sa, Shimokawa T, Toftg?rd R.  Inhibition of GLI-mediated transcription and tumor cell growth by small-molecule antagonists.?Proceedings of the National Academy of Sciences of the United States of America. 2007,104(20):8455-8460.
[2] Hou X, Chen X, Zhang P, et al.  Inhibition of hedgehog signaling by GANT58 induces apoptosis and shows synergistic antitumor activity with AKT inhibitor in acute T cell leukemia cells. Biochimie. 2014, 101:50-9

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt392.48
Cas No.64048-12-0
FormulaC24H16N4S
SynonymsNSC 75503;GANT58;GANT-58;NSC-75503
Solubility≥18.95 mg/mL in DMSO, ≥14.9 mg/mL in EtOH with ultrasonic and warming, <2.22 mg/mL in H2O
Chemical Name4-(2,4,5-tripyridin-4-ylthiophen-3-yl)pyridine
SDFDownload SDF
Canonical SMILESC1=CN=CC=C1C2=C(SC(=C2C3=CC=NC=C3)C4=CC=NC=C4)C5=CC=NC=C5
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description GANT 58 is an antagonist of GLI that inhibits GLI1-induced transcription with an IC50 value of 5 μM.
Targets GLI          
IC50 5 μM          

Quality Control