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GSK481

Cat. No. M5209

GSK481 Structure
Size Price Availability Quantity
2mg USD 100 In stock
5mg USD 150 In stock
10mg USD 250 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

GSK481 is a highly potent and monoselective Receptor Interacting Protein 1 kinase inhibitor. GSK481 can inhibit RIP1 WT S166 phosphorylation in human vs mouse plasmids overexpressed in HEK293T cells. GSK481 has approximately equivalent RIP1 FP potencies against human and cynomolgus monkey RIP1 but was >100-fold less potent against nonprimate RIP.

In vitro: GSK481(benzoxazepinone) not only showed an increase in biochemical activity but also exhibited excellent translation in the U937 cellular assay with IC50 = 10 nM.

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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 377.39
Formula C21H19N3O4
CAS Number 1622849-58-4
Purity >99%
Solubility DMSO 70 mg/mL
Storage at -20°C
References

DNA-Encoded Library Screening Identifies Benzo[b][1,4]oxazepin-4-ones as Highly Potent and Monoselective Receptor Interacting Protein 1 Kinase Inhibitors.
Harris PA, et al. J Med Chem. 2016 Mar 10;59(5):2163-78. PMID: 26854747.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: GSK481 supplier, TNF-alpha, inhibitors

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