1883548-84-2
1883548-84-2
Chemical Structure
AMG PERK 44
- CAS. Nr.: 1883548-84-2
- Formula:C34H29ClN4O2
- Molecular Weight:561.07
IUPAC Name: 4-(2-amino-4-methyl-3-(2-methylquinolin-6-yl)benzoyl)-1-methyl-2,5-diphenyl-1,2-dihydro-3H-pyrazol-3-one hydrochloride
InChIKey: RNAKBTDDCHJCMT-UHFFFAOYSA-N
SMILES: O=C1N(C2=CC=CC=C2)N(C)C(C3=CC=CC=C3)=C1C(C4=CC=C(C)C(C5=CC=C6N=C(C)C=CC6=C5)=C4N)=O.[H]Cl
Biological Activity: AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy[1][2].
| Art. -Nr. | Produktname | Reinheit | Beschreibung | Pricing | |||||||||||||||||||
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AMG PERK 44 | 99.67% | AMG PERK 44 is an orally active and highly selective PERK inhibitor with an IC50 of 6 nM. AMG PERK 44 has 1000-fold and 160-fold selectivity over GCN2 (IC50=7300 nM) and B-Raf (IC50 >1000 nM), respectively. AMG PERK 44 induces autophagy. | ||||||||||||||||||||
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Structural Analogs
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Similarity Score 0.78
HY-175880AMG-34 -
Similarity Score 0.54
HY-145867EGFR-IN-45 -
Similarity Score 0.53
HY-100509RNPS-1034 (Standard) -
Similarity Score 0.52
HY-182400AGI-25696 -
Similarity Score 0.50
HY-147576Axl-IN-9 -
Similarity Score 0.50
HY-107145ANingetinib -
Similarity Score 0.49
HY-18307SYN1143 -
Similarity Score 0.49
HY-179105Axl-IN-20 -
Similarity Score 0.49
HY-147577Axl-IN-10 -
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References
- [1]. Smith AL, 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. 2015 Feb 12;58(3):1426-41. [Content Brief]
- [2]. Roest G, et al. 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. 2018 Nov 30;7(12). pii: E239. [Content Brief]
