| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
IC50: 2.5 nM (PERK)[1]
Protein kinase RNA-like ER kinase (PERK), an ER stress sensor and eIF2α kinase. |
|---|---|
| ln Vitro |
PERK-IN-6 (Compound 5) has an IC50 of 0.1-0.3 μM in A549 cells, where it inhibits thapsigargin-induced PERK autophosphorylation[1].
PERK-IN-6 inhibits PERK kinase activity with an IC50 of 2.5 nM. In A549 cells, it has an IC50 of 0.1-0.3 μM for inhibiting thapsigargin-induced PERK autophosphorylation. By inhibiting PERK, it blocks eIF2α phosphorylation and downstream UPR signaling. |
| ln Vivo |
Following an intravenous dose of PERK-IN-6 (Compound 5), the blood clearance rate in SD rats was 10.5 mL/min/kg [1].
PERK-IN-6 inhibits PERK activity in cells, blocking eIF2α phosphorylation and the integrated stress response. It is used to study the role of PERK in ER stress, cancer cell survival, and neurodegeneration. The compound shows activity in A549 cells, inhibiting thapsigargin-induced PERK autophosphorylation. |
| Enzyme Assay |
PERK kinase activity is measured using kinase assay kits with recombinant PERK protein and peptide substrates (e.g., eIF2α peptide). PERK is incubated with ATP, substrate, and varying concentrations of PERK-IN-6. Phosphorylation of substrate is detected by radioactivity, fluorescence, or ELISA to determine IC50 values.
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| Cell Assay |
A549 cells or other cell lines are treated with ER stress inducers (e.g., thapsigargin, tunicamycin) in the presence or absence of PERK-IN-6. PERK autophosphorylation and eIF2α phosphorylation are assessed by Western blot. Cell viability and UPR target gene expression (e.g., CHOP, ATF4) are measured.
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| Animal Protocol |
PERK-IN-6 is evaluated in mouse models of cancer or neurodegeneration. Tumor-bearing mice or disease model mice are treated with PERK-IN-6 via oral or intraperitoneal administration. Tumor growth, ER stress markers, and survival are monitored.
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| ADME/Pharmacokinetics |
PERK-IN-6 has molecular weight 398.46 and formula C23H22N6O. It is a solid compound. Powder is stable at -20°C for 3 years; in solvent at -80°C for 6 months. As a small-molecule PERK inhibitor, it is suitable for both in vitro and in vivo applications.
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| Toxicity/Toxicokinetics |
Preclinical toxicity data for PERK-IN-6 are limited. As a PERK inhibitor, potential on-target effects may include modulation of the UPR and protein synthesis in normal tissues.
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| References | |
| Additional Infomation |
PERK-IN-6 is a research tool for studying ER stress, the unfolded protein response, and PERK biology. Its mechanism involves inhibition of PERK kinase activity, blocking eIF2α phosphorylation and the integrated stress response. No clinical trials or approved indications exist.
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| Molecular Formula |
C23H22N6O
|
|---|---|
| Molecular Weight |
398.460383892059
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| Exact Mass |
398.185
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| CAS # |
1337532-14-5
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| PubChem CID |
53468860
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| Appearance |
Off-white to light yellow solid powder
|
| LogP |
2.2
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
631
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(=O)(N1C2=C(C=C(C3C4=C(N)N=CN=C4N(C)C=3)C=C2)CC1)CC1=NC(C)=CC=C1
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| InChi Key |
VYZYOJULVVGQRS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H22N6O/c1-14-4-3-5-17(27-14)11-20(30)29-9-8-16-10-15(6-7-19(16)29)18-12-28(2)23-21(18)22(24)25-13-26-23/h3-7,10,12-13H,8-9,11H2,1-2H3,(H2,24,25,26)
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| Chemical Name |
1-[5-(4-amino-7-methylpyrrolo[2,3-d]pyrimidin-5-yl)-2,3-dihydroindol-1-yl]-2-(6-methylpyridin-2-yl)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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.5097 mL | 12.5483 mL | 25.0966 mL | |
| 5 mM | 0.5019 mL | 2.5097 mL | 5.0193 mL | |
| 10 mM | 0.2510 mL | 1.2548 mL | 2.5097 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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