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Chemical Structure| 64048-12-0 Chemical Structure| 64048-12-0

Structure of GANT 58
CAS No.: 64048-12-0

Chemical Structure| 64048-12-0

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GANT 58 is a potent Gli antagonist that inhibits GLI1-induced transcription (IC50 = 5 μM).

Synonyms: NSC 75503

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Product Details of GANT 58

CAS No. :64048-12-0
Formula : C24H16N4S
M.W : 392.48
SMILES Code : C1(C2=CC=NC=C2)=C(C3=CC=NC=C3)C(C4=CC=NC=C4)=C(C5=CC=NC=C5)S1
Synonyms :
NSC 75503
MDL No. :MFCD01103196
InChI Key :USWLOKMMUTWFMD-UHFFFAOYSA-N
Pubchem ID :253078

Safety of GANT 58

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P332+P313

Related Pathways of GANT 58

Hedgehog

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HuCCT1 cells 10 μM GANT58 significantly inhibited the proliferation of HuCCT1 cells PMC11089446
Human mesenchymal stem cells (hMSCs) 40 μM 14 days To evaluate the effect of GANT58-BTNP on hMSC differentiation toward osteoblasts. Results showed that GANT58-BTNP and control treatments had no negative effect on hMSC differentiation and mineralization. PMC7216559
MDA-MB-231 bone tumor cells 40 μM 7 days To evaluate the effect of GANT58-BTNP on tumor-mediated osteoclastogenesis. Results showed that GANT58-BTNP treatment significantly reduced osteoclast number compared to the no treatment control. PMC7216559
Human mesenchymal stem cells (hMSCs) 0–20 μM 1, 3, 5 days To evaluate the effect of GANT58 on hMSC proliferation, results showed GANT58-NPs did not significantly affect hMSC proliferation PMC7007697
MDA-MB-231 bone cells 0–80 μM 24 h To evaluate the effect of GANT58 on tumor cell proliferation and apoptosis, results showed GANT58 significantly reduced tumor cell proliferation and increased apoptosis PMC7007697
MDA-MB-231 bone cells 0–20 μM 48 h To evaluate the effect of GANT58 on PTHrP mRNA expression, results showed GANT58 significantly reduced PTHrP mRNA levels PMC7007697
LR-MSCs 10 μM 7 days Inhibition of Gli1 expression, thereby suppressing the differentiation of LR-MSCs into myofibroblasts and reducing the activation of the Wnt/β-catenin signaling pathway. PMC5974360
Rat tendon-derived stem cells (TDSCs) 0.25, 2.5, 25 mM 7 and 14 days Under osteogenic induction, GANT58 significantly suppressed the gene expressions of osteogenic markers (e.g., OCN, RUNX2, ALP) in TDSCs. PMC9686894
Hepatic stellate cells (HSCs) 5 μM 24 h Inhibition of Gli1-mediated canonical hedgehog signaling, reducing the expression of VEGF and angiopoietin 1, and suppressing HSC-mediated tubulogenesis capacity. PMC5301045

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Athymic nude mice (female) Breast cancer bone metastasis model Tail vein injection 8 mg/kg 5 times per week for 4 weeks To evaluate the therapeutic effect of GANT58-BTNP in a breast cancer bone metastasis model. Results showed that GANT58-BTNP treatment significantly reduced bone lesion area and improved bone volume fraction. PMC7216559
Athymic female nude mice Breast cancer bone metastasis model Tail vein injection 8 mg/kg 5 days/week for 4 weeks To evaluate the effect of GANT58-NPs on bone destruction in a bone metastasis model, results showed GANT58-NPs significantly reduced bone lesion area and number and increased trabecular bone volume PMC7007697
C57BL/6J mice AKT/YAP-induced HTVi CCA model Intraperitoneal injection 25 mg/kg Every other day for 3 weeks GANT58 significantly reduced the size and weight of subcutaneous xenograft tumors PMC11089446
Mice BLM-induced pulmonary fibrosis model Intraperitoneal injection 25 mg/kg Every other day for 7 days Inhibition of Gli1 expression, reducing pulmonary fibrotic lesions and collagen deposition, decreasing the expression of fibrotic markers α-SMA, Collagen I, and Vimentin, and suppressing the activation of the Wnt/β-catenin signaling pathway. PMC5974360
Female C57BL/6J mice Achilles tenotomy model Intraperitoneal injection 50 mg/kg Daily from day 1 to week 6 post-surgery GANT58 significantly inhibited trauma-induced tendon heterotopic ossification, reduced the formation of ectopic mineralized bones, and decreased the expression of cartilage and bone-related genes. PMC9686894

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.55mL

0.51mL

0.25mL

12.74mL

2.55mL

1.27mL

25.48mL

5.10mL

2.55mL

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