AMG PERK 44

Pricing Availability Delivery Time Qty
Cat.No. 5517 - AMG PERK 44 | C34H28N4O2.HCl
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)
Datasheet
Citations
Literature

Biological Activity

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

AMG PERK 44 is also offered as part of the Tocriscreen Plus and Tocriscreen Kinase Inhibitor Toolbox II. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 561.07
Formula C34H28N4O2.HCl
Storage Store at -20°C
Purity ≥98% (HPLC)
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.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 52.46 100
water 52.46 100

Preparing Stock Solutions

The following data is based on the product molecular weight 561.07. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.78 mL 8.91 mL 17.82 mL
5 mM 0.36 mL 1.78 mL 3.56 mL
10 mM 0.18 mL 0.89 mL 1.78 mL
50 mM 0.04 mL 0.18 mL 0.36 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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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