| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
IC50: 0.3 nM (PERK)[1]
PERK-IN-4 targets PERK (protein kinase R-like endoplasmic reticulum kinase), a key sensor of ER stress that phosphorylates eukaryotic initiation factor 2 alpha (eIF2α) to attenuate protein translation during ER stress. By inhibiting PERK, the compound disrupts the UPR signaling pathway, which is often dysregulated in cancer and other diseases. |
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| ln Vitro |
PERK-IN-4 demonstrates potent in vitro inhibition of PERK kinase activity. The compound's activity is typically assessed in kinase assays using purified recombinant PERK enzyme and peptide substrates. IC50 values are determined from dose-response curves generated in these enzymatic assays.
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| ln Vivo |
PERK-IN-4 has potential for in vivo efficacy in models of cancer, neurodegenerative diseases, and metabolic disorders where PERK signaling is dysregulated. By modulating the UPR, the compound may affect tumor cell survival, protein folding, and cellular stress responses. Further in vivo studies are needed to evaluate its pharmacokinetic properties, efficacy, and safety.
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| Enzyme Assay |
In vitro enzyme assays for PERK-IN-4 involve measuring its inhibition of PERK kinase activity. The assay typically uses purified recombinant PERK enzyme and measures the phosphorylation of peptide substrates such as eIF2α in the presence of the compound. IC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for PERK-IN-4 involve treating cells with varying concentrations of the compound and measuring PERK activity, eIF2α phosphorylation, and UPR marker expression using Western blotting. Cell viability and proliferation are assessed using MTT or other assays.
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| Animal Protocol |
In vivo animal experiments for PERK-IN-4 would typically involve administering the compound to animal models of cancer, neurodegeneration, or metabolic diseases. Efficacy is evaluated by measuring disease progression, UPR marker expression, and clinical outcomes.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for PERK-IN-4 are limited. The compound has a molecular weight of approximately 483.3. Its absorption, distribution, metabolism, and excretion properties have not been fully characterized. Further pharmacokinetic studies are needed to determine its bioavailability and systemic exposure.
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| Toxicity/Toxicokinetics |
Toxicological data for PERK-IN-4 are limited. As a research compound, comprehensive toxicological studies have not been reported. The compound is intended for research use only and is not for human therapeutic application. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
PERK-IN-4 (CAS#: 1337531-89-1) is a potent inhibitor of PERK kinase, a key regulator of the unfolded protein response during ER stress. The compound has potential applications in cancer research, neurodegenerative diseases, and metabolic disorders. It is for research use only.
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| Molecular Formula |
C24H19F4N5O
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|---|---|
| Molecular Weight |
469.43
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| Exact Mass |
469.152
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| CAS # |
1337531-89-1
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| Related CAS # |
PERK-IN-4-d3
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| PubChem CID |
66561167
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
710.9±60.0 °C at 760 mmHg
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| Flash Point |
383.7±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.660
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| LogP |
4.42
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
34
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| Complexity |
753
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PXVQGBJMIQCDEX-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H19F4N5O/c1-32-11-18(21-22(29)30-12-31-23(21)32)14-2-3-19-15(9-14)4-5-33(19)20(34)8-13-6-16(24(26,27)28)10-17(25)7-13/h2-3,6-7,9-12H,4-5,8H2,1H3,(H2,29,30,31)
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| Chemical Name |
1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-[3-fluoro-5-(trifluoromethyl)phenyl]ethanone
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 20.83 mg/mL (44.37 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.43 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1302 mL | 10.6512 mL | 21.3024 mL | |
| 5 mM | 0.4260 mL | 2.1302 mL | 4.2605 mL | |
| 10 mM | 0.2130 mL | 1.0651 mL | 2.1302 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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