AMG PERK 44 (hydrochloride) |
| Catalog No.GC91790 |
AMG PERK 44 is a protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 6 nM).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
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AMG PERK 44 is a protein kinase R-like ER kinase (PERK) inhibitor (IC50 = 6 nM).[1] It is selective for PERK over general control nonderepressible 2 kinase (GCN2) and B-RAF (IC50s = 7,300 and >1,000 nM, respectively). It inhibits PERK autophosphorylation in a cell-free assay (IC50 = 84 nM) and rescues protein synthesis in U2OS cells (EC50 = 400 nM). AMG PERK 44 (1, 3, 10, and 30 mg/kg) reduces intratumoral PERK autophosphorylation in a doxycycline-inducible PERK Matrigel™ plug assay.
References:
[1].Smith, A.L., Andrews, K.L., Beckmann, H., et al.Discovery of 1H-pyrazol-3(2H)-ones as potent and selective inhibitors of protein kinase R-like endoplasmic reticulum kinase (PERK)J. Med. Chem.58(3)1426-1441(2015).
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