3108399-87-4
3108399-87-4
Chemical Structure
APL-11056
- CAS No.: 3108399-87-4
- Formula:C20H14F4N6O2
- Molecular Weight:446.36
InChIKey: KKCIPZFJFPPHIG-GOSISDBHSA-N
SMILES: O=C(NC1=CC=C(N2N=C(C)C3=NC=NC(N)=C32)C(F)=C1F)[C@@H](C4=CC(F)=CC(F)=C4)O
Biological Activity: APL-11056 is an orally active PERK inhibitor (IC50 = 1.63 nM; Ki = 0.86 nM). APL-11056 competitively inhibits PERK kinase activity and reduces eIF2α phosphorylation, with only weak inhibition of HRI-induced eIF2α phosphorylation. APL-11056 exhibits kinome selectivity, shows high passive permeability and low efflux, and has off-target COX-1 inhibition and inhibition of Lck. APL-11056 can be used for PERK-related research[1].
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APL-11056 | APL-11056 is an orally active PERK inhibitor (IC50 = 1.63 nM; Ki = 0.86 nM). APL-11056 competitively inhibits PERK kinase activity and reduces eIF2α phosphorylation, with only weak inhibition of HRI-induced eIF2α phosphorylation. APL-11056 exhibits kinome selectivity, shows high passive permeability and low efflux, and has off-target COX-1 inhibition and inhibition of Lck. APL-11056 can be used for PERK-related research. | |||||||||||||||||||||
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