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GSK2656157

Cat. No. M2735
GSK2656157 Structure
Size Price Availability Quantity
2mg USD 45  USD45 In stock
5mg USD 65  USD65 In stock
10mg USD 85  USD85 In stock
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Quality Control
Biological Activity

GSK2656157 is an ATP-competitive and highly selective inhibitor of PERK with IC50 of 0.9 nM, 500-fold greater against a panel of 300 kinases.

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 416.45
Formula C23H21FN6O
CAS Number 1337532-29-2
Purity >98%
Solubility DMSO 20 mg/mL
Storage at -20°C
References

[1] Tanusree Sen, et al. Aberrant ER Stress Induced Neuronal-IFNβ Elicits White Matter Injury Due to Microglial Activation and T-Cell Infiltration after TBI

[2] Diego Rojas-Rivera, et al. When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157

[3] Takashi Ando, et al. GSK2656157, a PERK inhibitor, reduced LPS-induced IL-1β production through inhibiting Caspase 1 activation in macrophage-like J774.1 cells

[4] Jeffrey M Axten, et al. Discovery of GSK2656157: An Optimized PERK Inhibitor Selected for Preclinical Development

[5] Jothilatha Krishnamoorthy, et al. Evidence for eIF2α phosphorylation-independent effects of GSK2656157, a novel catalytic inhibitor of PERK with clinical implications

Related PERK Products
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Salubrinal

Salubrinal is a selective inhibitor of eIF2α dephosphorylation and inhibits ER stress-mediated apoptosis with EC50 of ~15 μM.

GSK2606414

GSK2606414 is an orally available, potent, and selective PERK inhibitor with IC50 of 0.4 nM, displaying at least 100-fold selectivity over the other EIF2AKs assayed.

  Catalog
Abmole Inhibitor Catalog




Keywords: GSK2656157 supplier, PERK, inhibitors

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