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ISRIB

Cat. No. M9242
ISRIB Structure
Size Price Availability Quantity
5mg USD 70  USD70 In stock
10mg USD 130  USD130 In stock
25mg USD 260  USD260 In stock
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Quality Control
Biological Activity

ISRIB is a potent and selective PERK inhibitor with IC50 of 5 nM. ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly.

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 451.34
Formula C22H24Cl2N2O4
CAS Number 548470-11-7
Purity >98%
Solubility DMSO 10 mM
Storage at -20°C
References

[1] Sidrauski C, et al. Elife. The small molecule ISRIB reverses the effects of eIF2α phosphorylation on translation and stress granule assembly.

[2] Sidrauski C, et al. Elife. Pharmacological brake-release of mRNA translation enhances cognitive memory.

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trans-ISRIB is a integrated stress response (ISR) inhibitor.

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GSK2656157

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.

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: ISRIB supplier, PERK, inhibitors

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