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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 MedComm (2020). 2024 May 13;5(5):e535.
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. ACS Nano. 2020 Jan 28;14(1):311-327.
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. ACS Nano. 2020 Jan 28;14(1):311-327.
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 J Control Release. 2019 Oct;311-312:257-272.
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 J Control Release. 2019 Oct;311-312:257-272.
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 J Control Release. 2019 Oct;311-312:257-272.
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. Cell Death Dis. 2018 May 29;9(6):639.
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. Antioxidants (Basel). 2022 Nov 16;11(11):2265.
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. Br J Pharmacol. 2017 Mar;174(5):409-423.

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. ACS Nano. 2020 Jan 28;14(1):311-327.
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 J Control Release. 2019 Oct;311-312:257-272.
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 MedComm (2020). 2024 May 13;5(5):e535.
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. Cell Death Dis. 2018 May 29;9(6):639.
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. Antioxidants (Basel). 2022 Nov 16;11(11):2265.

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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