2851820-52-3
Chemical Structure
HR-19011
- CAS. Nr.: 2851820-52-3
- Formula:C25H19F6N3O3
- Molecular Weight:523.43
IUPAC Name: (E)-3-(4-(5-carbamoyl-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-7-(3-morpholinopropoxy)-1H-benzo[d]imidazol-1-yl)but-2-en-1-yl)-2-(1-ethyl-3-methyl-1H-pyrazole-5-carboxamido)-3H-thieno[2,3-d]imidazole-5-carboxamide
InChIKey: PYDUAMACJGQTQN-RUCARUNLSA-N
SMILES: N#CC1=CC(C(F)(F)F)=CC(NC2=C(C(C2=O)=O)N[C@@H]3CC[C@@H](OC4=CC=C(C=C4)C(F)(F)F)CC3)=C1
Biological Activity: HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC50 value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia)[1][2].
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HR-19011 | 99.64% | HR-19011 is an eIF2α phosphorylation activator targeting heme-regulated inhibitor HRI (EIF2AK1). HR-19011 exhibits growth inhibitory activity against K562 cells with an IC50 value of 3.91 µM. HR-19011 inhibits the growth of hematologic malignancies by targeting HRI to activate the integrated stress response via the HRI-eIF2α-ATF4 axis. HR-19011 shows good safety in vivo. HR-19011 can be used for research on hematologic malignancies (leukemia). | ||||||||||||||||||||
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References
- [1]. Jinsook Kwak, et al. A bioisosteric approach to the discovery of novel N-aryl-N'-[4-(aryloxy)cyclohexyl]squaramide-based activators of eukaryotic initiation factor 2 alpha (eIF2α) phosphorylation. Eur J Med Chem. 2022 May 29;239:114501. [Content Brief]
- [2]. Min Jung Kim, et al. A Novel eIF2α-Phosphorylating Agent HR-19011 Exhibits Cell Growth Inhibitory Effects in K562 Cells through Hri Activation. Blood. Volume 144, Supplement 1, 5 November 2024, Page 7469
