CCT020312
Based on 42 publication(s) in Google Scholar
CCT020312 is a selective EIF2AK3/PERK activator. CCT020312 elicits EIF2A phosphorylation in cells.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.05%
- No. CAS: 324759-76-4
- Fòrmula: C31H30Br2N4O2
- Peso molecular:650.40
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 1 year , -20°C, 6 months
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
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Publications Citing Use of MedChemExpress (MCE) CCT020312
More- Signal Transduct Target Ther. 2025 Dec 17;10(1):413. [Abstract]
- Cell Metab. 2021 Mar 2;33(3):598-614.e7. [Abstract]
- Adv Sci (Weinh). 2023 Jul;10(20):e2205949. [Abstract]
- Cell Death Dis. 2020 Oct 13;11(10):847. [Abstract]
- Phytomedicine. 2026 Jan:150:157589. [Abstract]
- J Transl Med. 2023 Feb 6;21(1):89. [Abstract]
- World J Gastroenterol. 2025 Aug 28;31(32):108654. [Abstract]
- Cancer Cell Int. 2024 Jul 17;24(1):249. [Abstract]
- CNS Neurosci Ther. 2025 Nov;31(11):e70620. [Abstract]
- Biochem Pharmacol. 2024 Mar:221:116038. [Abstract]
- EMBO Rep. 2024 Oct;25(10):4488-4514. [Abstract]
- Commun Biol. 2024 Sep 5;7(1):1091. [Abstract]
- Cell Biol Toxicol. 2025 Jan 18;41(1):33. [Abstract]
- Pharmaceuticals (Basel). 2024 Aug 29;17(9):1139. [Abstract]
- Cell Biol Toxicol. 2023 Jun;39(3):907-928. [Abstract]
- Int J Mol Sci. 2022 Dec 29;24(1):544. [Abstract]
- Front Pharmacol. 2020 May 19:11:737. [Abstract]
- Front Cell Dev Biol. 2021 Aug 4:9:700854. [Abstract]
- ACS Omega. 2025 Apr 7;10(15):15461-15470. [Abstract]
- Toxicology. 2023 Aug 1:494:153593. [Abstract]
- Sci Rep. 2025 May 5;15(1):15659. [Abstract]
- Mediators Inflamm. 2021 Aug 21:2021:2481907. [Abstract]
- Neoplasia. 2025 Jul:65:101165. [Abstract]
- Oncol Rep. 2024 May;51(5):71. [Abstract]
- Fish Shellfish Immunol. 2024 Dec:155:110020. [Abstract]
- J Photochem Photobiol B. 2025 Sep:270:113209. [Abstract]
- Toxicol Appl Pharmacol. 2026 Jun 27:514:117927. [Abstract]
- Toxicol Appl Pharmacol. 2024 Feb:483:116800. [Abstract]
- Immun Inflamm Dis. 2026 Apr;14(4):e70418. [Abstract]
- Hum Exp Toxicol. 2024 Jan-Dec:43:9603271241251447. [Abstract]
- Neural Plast. 2025 Aug 28:2025:6776608. [Abstract]
- Tissue Cell. 2024 Feb:86:102289. [Abstract]
- Vet Microbiol. 2025 Aug:307:110559. [Abstract]
- PLoS One. 2023 May 18;18(5):e0283943. [Abstract]
- Biochem Biophys Res Commun. 2021 Jun 11:557:316-322. [Abstract]
- Exp Ther Med. 2023 Jul 24;26(3):433. [Abstract]
- Oncol Lett. 2026 Apr 14;31(6):234. [Abstract]
- Authorea. 2025 Aug 5.
- bioRxiv. 2025 May 7:2025.04.28.650846. [Abstract]
- Research Square Preprint. 2025 Jan 12.
- Research Square Print. December 29th, 2022.
- Oxid Med Cell Longev. 2022 Aug 5:2022:3982613. [Abstract]
Customer Validation & Images
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Flow Cytometry
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WB
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Bio/Physico-chemical Assay
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RT-PCR
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Cell Migration/Invasion Assay
Actividad biológica
Treatment of HT29 cells with CCT020312 for 24 hours reveals a concentration-dependent loss of P-S608-pRB signal, with a linear response between 1.8 and 6.1 μM[1].
CCT020312 treatment effectively inhibits cell proliferation (as measured at 96 hours) even if treatment is for 2 hours only with subsequent compound washout, indicating that CCT020312 is capable of eliciting durable rather than transient cytostasis[1].
Treatment of HT29 cells with 10 μM CCT020312 for 24 hours reduces the amount of the G1/S cyclins D1, D2, E and A as well as the CDK catalytic subunit CDK2 and increased the level of the CDK inhibitor p27KIP1 present in such cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
P301S transgenic mice treated with CCT020312 (2 mg/kg; i.p.; once daily for 6 weeks) performes significantly better in Morris water maze[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:9-week-old P301S tau transgenic mice[2]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection; once daily for 6 weeks
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Result:P301S transgenic mice treated with CCT020312 performed significantly better in Morris water maze.
Chemical Information
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No. CAS 324759-76-4
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Appearance Solid
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Peso molecular 650.40
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Fòrmula C31H30Br2N4O2
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Color Light yellow to yellow
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SMILES
O=C1NC2=C(C(C3=CC=CC=C3)=C1C4=NN(C(C4)C5=CC=C(C=C5)Br)C(CCN(CC)CC)=O)C=C(C=C2)Br
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 1 year -20°C 6 months
Publications (42)
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Journal Impact Factor
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Most Recent
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Signal Transduct Target Ther
Disruption of heme homeostasis by nuclear receptor Nur77 induces pyroptosis through granzyme B-dependent GSDMC cleavage. [Abstract]2025 Dec 17;10(1):413. PMID: 41407678 -
Cell Metab
A cold-stress-inducible PERK/OGT axis controls TOM70-assisted mitochondrial protein import and cristae formation. [Abstract]2021 Mar 2;33(3):598-614.e7. PMID: 33592173 -
Adv Sci (Weinh)
PERK-Mediated Cholesterol Excretion from IDH Mutant Glioma Determines Anti-Tumoral Polarization of Microglia. [Abstract]2023 Jul;10(20):e2205949. PMID: 37166058
CCT020312 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Jul;10(20):e2205949. [Abstract]
CCT020312 (CCT) (2 μM，48 h) markedly increased cholesterol efflux from IDHwt U87 cells into the culture medium.
CCT020312 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Jul;10(20):e2205949. [Abstract]
CCT020312 (CCT) (2 μM，48 h) significantly upregulated M1-associated gene markers, CD86, IL12, and IL6, but downregulated the expression of M2-associated genes, CD163 and MCR1 in HMC3 cells.
CCT020312 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2023 Jul;10(20):e2205949. [Abstract]
CCT020312 (CCT) (2 μM，48 h) activated PERK and promoted M1-like microglia, leading to anti-tumoral effects that inhibited glioma progression.
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Cell Death Dis
PERK controls bone homeostasis through the regulation of osteoclast differentiation and function. [Abstract]2020 Oct 13;11(10):847. PMID: 33051453 -
Phytomedicine
MARCH5-mediated MIEF2 ubiquitination and degradation contribute to gigantol to against hepatic steatosis and mitochondrial fission in alcoholic liver disease. [Abstract]2026 Jan:150:157589. PMID: 41353882
CCT020312 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jan:150:157589. [Abstract]
The ethanol-induced AML12 cells with MIEF2 knockdown or overexpression were treated with CCT020312 (5 μM), and then the apoptosis of the AML12 cells was detected using flow cytometry.
CCT020312 purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2026 Jan:150:157589. [Abstract]
The expression of PERK, CHOP, and Cleaved caspase-3 in the transfected AML12 cells treated with or without CCT020312 (5 μM) was detected by Western blotting. CCT020312 effectively reversed the impacts of MIEF2 on ER stress-associated proteins.
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J Transl Med
Young and undamaged recombinant albumin alleviates T2DM by improving hepatic glycolysis through EGFR and protecting islet β cells in mice. [Abstract]2023 Feb 6;21(1):89. PMID: 36747238 -
World J Gastroenterol
Melatonin-induced ferroptosis in pancreatic cancer cells by stimulating endoplasmic reticulum stress and inhibiting alanine-serine-cysteine transporter 2-driven glutamine metabolism. [Abstract]2025 Aug 28;31(32):108654. PMID: 40900769 -
Cancer Cell Int
Activation of the PERK/eIF2α axis is a pivotal prerequisite of taxanes to cancer cell apoptosis and renders synergism to overcome paclitaxel resistance in breast cancer cells. [Abstract]2024 Jul 17;24(1):249. PMID: 39020371 -
CNS Neurosci Ther
Aerobic Exercise Training Exerts Neuroprotective Effects in Alzheimer's Disease Mice by Regulating Endoplasmic Reticulum Stress-Autophagy Pathway-Mediated Pyroptosis. [Abstract]2025 Nov;31(11):e70620. PMID: 41249871 -
Biochem Pharmacol
CCT020312 exerts anti-prostate cancer effect by inducing G1 cell cycle arrest, apoptosis and autophagy through activation of PERK/eIF2α/ATF4/CHOP signaling. [Abstract]2024 Mar:221:116038. PMID: 38286211 -
EMBO Rep
CaMKII suppresses proteotoxicity by phosphorylating BAG3 in response to proteasomal dysfunction. [Abstract]2024 Oct;25(10):4488-4514. PMID: 39261742 -
Commun Biol
Small GTP-binding protein GDP dissociation stimulator influences cisplatin-induced acute kidney injury via PERK-dependent ER stress. [Abstract]2024 Sep 5;7(1):1091. PMID: 39237614 -
Cell Biol Toxicol
Deciphering SPP1-related macrophage signaling in the pathogenesis of intervertebral disc degeneration. [Abstract]2025 Jan 18;41(1):33. PMID: 39825191 -
Pharmaceuticals (Basel)
Maltol Improves Peripheral Nerve Function by Inhibiting Schwann Cell Apoptosis via the PERK/eIF2α/CHOP Pathway and MME Upregulation in Diabetic Peripheral Neuropathy. [Abstract]2024 Aug 29;17(9):1139. PMID: 39338303 -
Cell Biol Toxicol
Shikonin inhibits neuronal apoptosis via regulating endoplasmic reticulum stress in the rat model of double-level chronic cervical cord compression. [Abstract]2023 Jun;39(3):907-928. PMID: 35028790 -
Int J Mol Sci
Geraniol-Mediated Suppression of Endoplasmic Reticulum Stress Protects against Cerebral Ischemia-Reperfusion Injury via the PERK-ATF4-CHOP Pathway. [Abstract]2022 Dec 29;24(1):544. PMID: 36613992 -
Front Pharmacol
CCT020312 Inhibits Triple-Negative Breast Cancer Through PERK Pathway-Mediated G1 Phase Cell Cycle Arrest and Apoptosis. [Abstract]2020 May 19:11:737. PMID: 32508655
CCT020312 purchased from MedChemExpress. Usage Cited in: Front Pharmacol. 2020 May 19:11:737. [Abstract]
CCT020312 increases the protein levels of cleaved PARP and the pro-apoptosis protein Bax and decreases the protein levels of the anti-apoptosis protein Bcl-2 in MDA-MB-453 and CAL-148 cells.
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Front Cell Dev Biol
2021 Aug 4:9:700854. PMID: 34422821 -
ACS Omega
Activation of the PERK Branch of the UPR as a Strategy for Improving Outcomes in Acute Ischemic Stroke. [Abstract]2025 Apr 7;10(15):15461-15470. PMID: 40290914 -
Toxicology
Selenium nanoparticles alleviate deoxynivalenol-induced intestinal epithelial barrier dysfunction by regulating endoplasmic reticulum stress in IPEC-J2 cells. [Abstract]2023 Aug 1:494:153593. PMID: 37442268 -
Sci Rep
USP18 attenuates endoplasmic reticulum stress via the PERK-eIF2α-ATF4 axis to reduce apoptosis in hepatocellular carcinoma cells. [Abstract]2025 May 5;15(1):15659. PMID: 40325079 -
Mediators Inflamm
Artesunate Restrains Maturation of Dendritic Cells and Ameliorates Heart Transplantation-Induced Acute Rejection in Mice through the PERK/ATF4/CHOP Signaling Pathway. [Abstract]2021 Aug 21:2021:2481907. PMID: 34462628 -
Neoplasia
2025 Jul:65:101165. PMID: 40252311 -
Oncol Rep
Butyrate increases methylglyoxal production through regulation of the JAK2/Stat3/Nrf2/Glo1 pathway in castration‑resistant prostate cancer cells. [Abstract]2024 May;51(5):71. PMID: 38577936 -
Fish Shellfish Immunol
Grass Carp Reovirus (GCRV) infection activates the PERK-eIF2α pathway to promote the viral replication. [Abstract]2024 Dec:155:110020. PMID: 39528019 -
J Photochem Photobiol B
Photobiomodulation mediates endoplasmic reticulum-mitochondria contact and ameliorates lipotoxicity in MASLD via Mfn2 upregulation. [Abstract]2025 Sep:270:113209. PMID: 40633245 -
Toxicol Appl Pharmacol
Dexmedetomidine antagonizes cisplatin-induced ototoxicity in Cochlear hair cells by alleviating endoplasmic reticulum stress via the PERK pathway. [Abstract]2026 Jun 27:514:117927. PMID: 42364780 -
Toxicol Appl Pharmacol
Esketamine induces apoptosis of nasopharyngeal carcinoma cells through the PERK/CHOP pathway. [Abstract]2024 Feb:483:116800. PMID: 38219984 -
Immun Inflamm Dis
The Bufei Nashen Pill Alleviates COPD by Targeting Endoplasmic Reticulum Stress Through the PERK/eIF2α Signaling Pathway. [Abstract]2026 Apr;14(4):e70418. PMID: 41969244 -
Hum Exp Toxicol
Acacetin inhibits activation of microglia to improve neuroinflammation after subarachnoid hemorrhage through the PERK signaling pathway mediated autophagy. [Abstract]2024 Jan-Dec:43:9603271241251447. PMID: 38720657 -
Neural Plast
Activation of the PERK/MANF/STAT3 Pathway in Astrocytes Promotes Synaptic Remodeling and Neurological Recovery in the Acute Phase After Stroke in Mice. [Abstract]2025 Aug 28:2025:6776608. PMID: 40919080 -
Tissue Cell
Sevoflurane postconditioning alleviates hypoxic-ischemic brain damage in rats by inhibiting the endoplasmic reticulum stress PERK/ATF4/CHOP pathway. [Abstract]2024 Feb:86:102289. PMID: 38194851 -
Vet Microbiol
PERK-mediated eIF2α phosphorylation suppresses porcine epidemic diarrhea virus replication by attenuating global protein synthesis and inducing IFN-Ⅰ production. [Abstract]2025 Aug:307:110559. PMID: 40494050 -
PLoS One
Development of a cell-free screening assay for the identification of direct PERK activators. [Abstract]2023 May 18;18(5):e0283943. PMID: 37200357 -
Biochem Biophys Res Commun
PERK activation by CCT020312 chemosensitizes colorectal cancer through inducing apoptosis regulated by ER stress. [Abstract]2021 Jun 11:557:316-322. PMID: 33894420 -
Exp Ther Med
Resveratrol‑mediated activation of SIRT1 inhibits the PERK‑eIF2α‑ATF4 pathway and mitigates bupivacaine‑induced neurotoxicity in PC12 cells. [Abstract]2023 Jul 24;26(3):433. PMID: 37602306 -
Oncol Lett
Thrombospondin-1 triggers calreticulin expression in human mucoepidermoid carcinoma MC-3 cells via the PERK/CHOP pathway. [Abstract]2026 Apr 14;31(6):234. PMID: 42038351 -
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bioRxiv
2025 May 7:2025.04.28.650846. PMID: 40654759 -
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Oxid Med Cell Longev
Biogenic Selenium Nanoparticles Alleviate Intestinal Epithelial Barrier Damage through Regulating Endoplasmic Reticulum Stress-Mediated Mitophagy. [Abstract]2022 Aug 5:2022:3982613. PMID: 36035212
Solvente y solubilidad
DMSO : 100 mg/mL (153.75 mM; Need ultrasonic; 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.20 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.08 mg/mL (3.20 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (280 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)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Stockwell SR, et al.Mechanism-based screen for G1/S checkpoint activators identifies a selective activator of EIF2AK3/PERK signalling. PLoS One. 2012;7(1):e28568. [Content Brief]
[2]. Bruch J, et al. PERK activation mitigates tau pathology in vitro and in vivo. EMBO Mol Med. 2017 Mar;9(3):371-384. [Content Brief]
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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.5375 mL | 7.6876 mL | 15.3752 mL | 38.4379 mL |
| 5 mM | 0.3075 mL | 1.5375 mL | 3.0750 mL | 7.6876 mL | |
| 10 mM | 0.1538 mL | 0.7688 mL | 1.5375 mL | 3.8438 mL | |
| 15 mM | 0.1025 mL | 0.5125 mL | 1.0250 mL | 2.5625 mL | |
| 20 mM | 0.0769 mL | 0.3844 mL | 0.7688 mL | 1.9219 mL | |
| 25 mM | 0.0615 mL | 0.3075 mL | 0.6150 mL | 1.5375 mL | |
| 30 mM | 0.0513 mL | 0.2563 mL | 0.5125 mL | 1.2813 mL | |
| 40 mM | 0.0384 mL | 0.1922 mL | 0.3844 mL | 0.9609 mL | |
| 50 mM | 0.0308 mL | 0.1538 mL | 0.3075 mL | 0.7688 mL | |
| 60 mM | 0.0256 mL | 0.1281 mL | 0.2563 mL | 0.6406 mL | |
| 80 mM | 0.0192 mL | 0.0961 mL | 0.1922 mL | 0.4805 mL | |
| 100 mM | 0.0154 mL | 0.0769 mL | 0.1538 mL | 0.3844 mL |
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