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GANT58

Cat. No. M1812
GANT58 Structure
Synonym:

NSC75503

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 62  USD62 In stock
2mg USD 36  USD36 In stock
5mg USD 54  USD54 In stock
10mg USD 85  USD85 In stock
50mg USD 293  USD293 In stock
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Quality Control & Documentation
Biological Activity

GANT58 is a cell-permeable GLI antagonist that inhibits GLI1-induced transcription (IC50 = 5 μM). Acts as a blocker of Hedgehog (Hh) pathway downstream of SMO and SUFU causing Gli1 nuclear accumulation. It also targets Gli-mediated gene transactivation (IC50 ~ 5 µM in SAG-stimulated Shh-L2 cells) and displays anti-proliferative and antitumor activity in vivo.

Product Citations
Customer Product Validations & Biological Datas
Source Biochimie (2014). Figure 3. GANT58
Method CCK8 assays
Cell Lines T-ALL cells
Concentrations 5 and 10 μM
Incubation Time 48 h
Results Furthermore, incubation of CCRFeCEM with 10 μM GANT58 for 48 h caused an increase in the percentage of cells in G1 and S phase and a decrease in the percentage of cells in G2/M phase relative to controls
Chemical Information
Molecular Weight 392.48
Formula C24H16N4S
CAS Number 64048-12-0
Solubility (25°C) DMSO 20 mM
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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 Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 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 Compound A of 10 mg/kg.

References

[1] Hassounah NB, et al. Clin Cancer Res. Molecular pathways: the role of primary cilia in cancer progression and therapeutics with a focus on Hedgehog signaling.

[2] Stanton BZ, et al. Mol Biosyst. Small-molecule modulators of the Sonic Hedgehog signaling pathway.

[3] Katoh Y, et al. Curr Mol Med. Hedgehog target genes: mechanisms of carcinogenesis induced by aberrant hedgehog signaling activation.

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GANT61

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Keywords: GANT58, NSC75503 supplier, Gli, inhibitors, activators


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