Pricing Availability   Qty
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)
Citations (8)
Literature (1)

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
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
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.

Select a batch to recalculate based on the batch molecular weight:
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

Certificate of Analysis / Product Datasheet
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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

If you know of a relevant reference for AMG PERK 44, please let us know.

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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

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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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.

Cell Cycle and DNA Damage Research Product Guide

Cell Cycle and DNA Damage Research Product Guide

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