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Submit ReviewAMG PERK 44
Description: Potent and selective PERK inhibitor; orally bioavailable
Chemical Name: 4-[2-Amino-4-methyl-3-(2-methyl-6-quinolinyl)benzoyl]-1,2-dihydro-1-methyl-2,5-diphenyl-3H-pyrazol-3-one hydrochloride
Purity: ≥98% (HPLC)
Biological Activity for AMG PERK 44
AMG PERK 44 is a potent and selective PERK inhibitor (IC50 = 6 nM). Exhibits >160-fold selectivity for PERK over B-Raf and GCN2, as well as a panel of 387 other kinases. Orally bioavailable.
Licensing Information
By permission of the authors
Compound Libraries for AMG PERK 44
AMG PERK 44 is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.
Technical Data for AMG PERK 44
| M. Wt | 561.07 |
| Formula | C34H28N4O2.HCl |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1883548-84-2 |
| PubChem ID | 121513867 |
| InChI Key | RNAKBTDDCHJCMT-UHFFFAOYSA-N |
| Smiles | CC2=NC1=CC=C(C3=C(N)C(C(C4=C(C5=CC=CC=C5)N(C)N(C6=CC=CC=C6)C4=O)=O)=CC=C3C)C=C1C=C2.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for AMG PERK 44
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.22 | 20 |
Preparing Stock Solutions for AMG PERK 44
The following data is based on the product molecular weight 561.07. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 8.91 mL | 44.56 mL | 89.12 mL |
| 1 mM | 1.78 mL | 8.91 mL | 17.82 mL |
| 2 mM | 0.89 mL | 4.46 mL | 8.91 mL |
| 10 mM | 0.18 mL | 0.89 mL | 1.78 mL |
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Product Datasheets for AMG PERK 44
References for AMG PERK 44
References are publications that support the biological activity of the product.
Smith et al (2015) 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 1426 PMID: 25587754
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Keywords: AMG PERK 44, AMG PERK 44 supplier, AMGPERK44, PERK, inhibitors, inhibits, potent, selective, protein, kinase, R-like, PKR, ER, orally, bioavailable, 5517, Tocris Bioscience
8 Citations for AMG PERK 44
Citations are publications that use Tocris products. Selected citations for AMG PERK 44 include:
Emilie et al (2020) FOXO1 promotes HIV latency by suppressing ER stress in T cells. Nat Microbiol 5 1144-1157 PMID: 32541947
Carolyn G et al (2020) Endorepellin evokes an angiostatic stress signaling cascade in endothelial cells. J Biol Chem 295 6344-6356 PMID: 32205445
Shikhar et al (2020) The Unfolded Protein Response Mediator PERK Governs Myeloid Cell-Driven Immunosuppression in Tumors through Inhibition of STING Signaling. Immunity 52 668-682.e7 PMID: 32294407
Roberto et al (2023) The endoplasmic reticulum kinase PERK interacts with the oxidoreductase ERO1 to metabolically adapt mitochondria. Cell Rep 42 111899 PMID: 36586409
Rojas-Rivera et al (2017) When PERK inhibitors turn out to be new potent RIPK1 inhibitors: critical issues on the specificity and use of GSK2606414 and GSK2656157. Cell Death Differ 24 1100 PMID: 28452996
Roest et al (2018) The ER Stress Inducer l-Azetidine-2-Carboxylic Acid Elevates the Levels of Phospho-eIF2α and of LC3-II in a Ca2+-Dependent Manner. Cells 7 PMID: 30513588
Viviana et al (2021) Cholinergic neurons constitutively engage the ISR for dopamine modulation and skill learning in mice. Science 372 PMID: 33888613
Mahameed et al (2019) The unfolded protein response modulators GSK2606414 and KIRA6 are potent KIT inhibitors. Cell Death Dis 10 300 PMID: 30931942
Do you know of a great paper that uses AMG PERK 44 from Tocris? Please let us know.
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Cell Cycle and DNA Damage Research Product Guide
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