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GSK-503

Cat. No. M4804
GSK-503 Structure
Size Price Availability Quantity
10mM*1mL USD 130  USD130 In stock
2mg USD 70  USD70 In stock
5mg USD 105  USD105 In stock
10mg USD 159  USD159 In stock
50mg USD 540  USD540 In stock
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Quality Control
Biological Activity

GSK-503 was designed by performing high-throughput screening for EZH2 methyltransferase inhibiting compounds followed by chemical optimization.In a melanoma mouse model, conditional Ezh2 ablation as much as treatment with the preclinical EZH2 inhibitor GSK503 stabilizes the disease through inhibition of growth and virtually abolishes metastases formation without affecting normal melanocyte biology.GSK-503 inhibits the methyltransferase activity of WT and mutant EZH2 with similar potency and is structurally related to GSK-126 and GSK-343. GSK-503 was > 200 fold selective over EZH1 (Kappi=636nM) and > 4000 fold selective over other histone methyltransferases.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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.

Chemical Information
Molecular Weight 526.67
Formula C31H38N6O2
CAS Number 1346572-63-1
Purity 98.60%
Solubility DMSO 44 mg/mL
Storage at -20°C
References

[1] Zingg D, et al. Nat Commun. The epigenetic modifier EZH2 controls melanoma growth and metastasis through silencing of distinct tumour suppressors.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK-503 supplier, Histone Methyltransferase, inhibitors

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