HR-19011
Based on 1 Customer Validation
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).
For research use only. We do not sell to patients.
- Purity: 99.64%
- CAS No.: 2851820-52-3
- Formula: C25H19F6N3O3
- Molecular Weight:523.43
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
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eIF2 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
4 μM
Compound: 40
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Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human K562 cells incubated for 72 hrs by CCK8 assay
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[PMID: 35716517] |
| PBMC | IC50 |
19.3 μM
Compound: 40
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Antiproliferative activity against human PBMC cells incubated for 72 hrs by CCK8 assay
Antiproliferative activity against human PBMC cells incubated for 72 hrs by CCK8 assay
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[PMID: 35716517] |
HR-19011 (compound 40) (1.25-20 μM, 72 h) shows an anticancer activity with IC50 values of 4 and 19.3 μM in K562 and human peripheral blood mononuclear cells (PBMC) cell, shows a strong cancer cell selectivity with a SI value of 4.83 in PBMC cells[1].
HR-19011 (0-10 μM, 24 h) activate eIF2α phosphorylation in an eIF2α/ATF4/CHOP pathway-dependent manner in K562 cells[1].
HR9011 exhibits cell growth inhibitory activity with an IC50 value of 3.91 µM in K562 cells transfected with nontargeting control shRNA, while the IC50 value increases to 8.03 µM in K562 cells stably transfected with HRI-specific shRNA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 cells
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Concentration:0, 2.5, 5 and 10 μM
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Incubation Time:24 h
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Result:Significantly increased the phosphorylation levels of eIF2α in a dose dependent manner.
Upregulated the expression of the downstream effector proteins ATF4 and CHOP.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2851820-52-3
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Appearance Solid
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Molecular Weight 523.43
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Formula C25H19F6N3O3
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Color White to yellow
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 25 mg/mL (47.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9105 mL | 9.5524 mL | 19.1048 mL | 47.7619 mL |
| 5 mM | 0.3821 mL | 1.9105 mL | 3.8210 mL | 9.5524 mL | |
| 10 mM | 0.1910 mL | 0.9552 mL | 1.9105 mL | 4.7762 mL | |
| 15 mM | 0.1274 mL | 0.6368 mL | 1.2737 mL | 3.1841 mL | |
| 20 mM | 0.0955 mL | 0.4776 mL | 0.9552 mL | 2.3881 mL | |
| 25 mM | 0.0764 mL | 0.3821 mL | 0.7642 mL | 1.9105 mL | |
| 30 mM | 0.0637 mL | 0.3184 mL | 0.6368 mL | 1.5921 mL | |
| 40 mM | 0.0478 mL | 0.2388 mL | 0.4776 mL | 1.1940 mL |
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