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GSK2606414

Cat. No. M2734
GSK2606414 Structure
Size Price Availability Quantity
2mg USD 65  USD65 In stock
5mg USD 100  USD100 In stock
10mg USD 140  USD140 In stock
25mg USD 280  USD280 In stock
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Quality Control
Biological Activity

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.

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 451.44
Formula C24H20F3N5O
CAS Number 1337531-36-8
Purity 99.93%
Solubility DMSO 80 mg/mL
Storage at -20°C
References

[1] Kornlia Szebnyi, et al. Human ALS/FTD brain organoid slice cultures display distinct early astrocyte and targetable neuronal pathology

[2] Jiachao Guo, et al. PERK controls bone homeostasis through the regulation of osteoclast differentiation and function

[3] Martin McLaughlin, et al. The PERK Inhibitor GSK2606414 Enhances Reovirus Infection in Head and Neck Squamous Cell Carcinoma via an ATF4-Dependent Mechanism

[4] Mohamed Mahameed, et al. The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors

[5] Xintong Jiang, et al. Effects of GSK2606414 on cell proliferation and endoplasmic reticulum stress‑associated gene expression in retinal pigment epithelial cells

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Keywords: GSK2606414 supplier, PERK, inhibitors

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