GSK2656157
Based on 65 publication(s) in Google Scholar
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase (PERK) with an IC50 of 0.9 nM.
For research use only. We do not sell to patients.
- Purity: 99.66%
- CAS No.: 1337532-29-2
- Formula: C23H21FN6O
- Molecular Weight:416.45
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
Publications Citing Use of MedChemExpress (MCE) GSK2656157
More- Nature. 2026 Apr;652(8112):1339-1348. [Abstract]
- Cell Metab. 2022 Apr 5;34(4):581-594.e8. [Abstract]
- Mol Cell. 2023 Sep 21;83(18):3303-3313.e6. [Abstract]
- Nat Commun. 2025 Jan 2;16(1):50. [Abstract]
- Nat Commun. 2024 Apr 25;15(1):3481. [Abstract]
- Nat Commun. 2022 Oct 16;13(1):6108. [Abstract]
- Adv Sci (Weinh). 2025 Sep 23:e08245. [Abstract]
- Cell Discov. 2021 Oct 26;7(1):98. [Abstract]
- Sci Adv. 2021 Jun 16;7(25):eabf8577. [Abstract]
- Gut Microbes. 2024 Jan-Dec;16(1):2392877. [Abstract]
- Nano Today. 2026 Jan 14;67:102975.
- J Immunother Cancer. 2025 May 30;13(5):e011398. [Abstract]
- Cardiovasc Diabetol. 2024 Jan 9;23(1):19. [Abstract]
- Pharmacol Res. 2025 Dec:222:108029. [Abstract]
- J Neuroinflammation. 2017 May 11;14(1):104. [Abstract]
- Cell Death Dis. 2021 Nov 1;12(11):1038. [Abstract]
- Free Radic Biol Med. 2021 Nov 1:175:236-248. [Abstract]
- Neoplasia. 2025 Apr 18:65:101165. [Abstract]
- NPJ Breast Cancer. 2022 Jan 10;8(1):2. [Abstract]
- Cell Death Discov. 2026 Feb 26. [Abstract]
- Cell Death Discov. 2024 Mar 12;10(1):134. [Abstract]
- Cell Rep. 2024 Jun 27;43(7):114402. [Abstract]
- Ecotoxicol Environ Saf. 2024 Apr 1:274:116193. [Abstract]
- Ecotoxicol Environ Saf. 2023 Dec:268:115711. [Abstract]
- Ecotoxicol Environ Saf. 2022 Jun 15;238:113595. [Abstract]
- Cancer Cell Int. 2024 Jul 17;24(1):249. [Abstract]
- Cancer Cell Int. 2017 Jan 10:17:12. [Abstract]
- Cell Biol Toxicol. 2025 Jan 18;41(1):33. [Abstract]
- Cell Biol Toxicol. 2023 Jun;39(3):907-928. [Abstract]
- Biochem Pharmacol. 2023 Aug:214:115634. [Abstract]
- J Gastroenterol. 2023 Jul;58(7):668-681. [Abstract]
- J Pathol. 2020 Jun;251(2):123-134. [Abstract]
- Int J Mol Sci. 2023 Nov 12;24(22):16239. [Abstract]
- Int J Mol Sci. 2017 Apr 18;18(4). pii: E854. [Abstract]
- mBio. 2025 Sep 10;16(9):e0143625. [Abstract]
- Int Immunopharmacol. 2024 Jul 29:140:112818. [Abstract]
- Toxicology. 2024 May:504:153800. [Abstract]
- Toxicology. 2023 Aug 1:494:153593. [Abstract]
- J Dairy Sci. 2023 Jul;106(7):5146-5164. [Abstract]
- ACS Omega. 2025 Oct 17;10(42):50208-50217. [Abstract]
- Mol Neurobiol. 2025 Jun 1. [Abstract]
- Appl Microbiol Biotechnol. 2021 Jan;105(1):353-366. [Abstract]
- FASEB J. 2022 Jul;36(7):e22401. [Abstract]
- J Funct Foods. July 2022, 105116.
- Oncol Rep. 2026 Jan;55(1):5. [Abstract]
- J Biol Chem. 2023 Jul;299(7):104857. [Abstract]
- Cytokine. 2026 Jan:197:157068. [Abstract]
- Neural Plast. 2025 Aug 28:2025:6776608. [Abstract]
- Cell Signal. 2025 Jun:130:111702. [Abstract]
- Brain Res Bull. 2020 Sep;162:73-83. [Abstract]
- Brain Res Bull. 2019 Mar:146:28-39. [Abstract]
- Vet Res. 2025 Jul 15;56(1):150. [Abstract]
- Vascul Pharmacol. 2018 Oct:109:36-44. [Abstract]
- J Anim Sci. 2023 Jan 3:101:skad101. [Abstract]
- Fish Shellfish Immunol Rep. 2020 Nov 28:1:100002. [Abstract]
- Vet Microbiol. 2026 Apr:315:110921. [Abstract]
- Animals (Basel). 2021 Nov 28;11(12):3400. [Abstract]
- Tissue Cell. 2024 Feb:86:102289. [Abstract]
- J Steroid Biochem Mol Biol. 2021 Jul:211:105893. [Abstract]
- Biomarkers. 2022 Jul;27(5):470-482. [Abstract]
- bioRxiv. 2025 Aug 22:2025.08.18.670862. [Abstract]
- Auburn University. 2024 May.
- Oxid Med Cell Longev. 2022 Aug 5:2022:3982613. [Abstract]
- Oxid Med Cell Longev. 2020 Jul 27;2020:8291413. [Abstract]
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
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Biological Activity
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EIF2AK3 (PERK) 0.9 nM (IC50) |
EIF2AK1 (HRI) 460 nM (IC50) |
BRK 905 nM (IC50) |
EIF2AK2 (PKR) 905 nM (IC50) |
MEKK3 954 nM (IC50) |
Aurora B 1259 nM (IC50) |
KHS 1764 nM (IC50) |
LCK 2344 nM (IC50) |
MLK2 2796 nM (IC50) |
MEKK3 2847 nM (IC50) |
ALK5 3020 nM (IC50) |
MLCK2 3039 nM (IC50) |
EIF2AK4(GCN2) 3162 nM (IC50) |
c-MER 3431 nM (IC50) |
PI3Kγ 3802 nM (IC50) |
WNK3 5951 nM (IC50) |
LRRK2 6918 nM (IC50) |
ROCK1 7244 nM (IC50) |
MSK1 8985 nM (IC50) |
NEK1 9807 nM (IC50) |
AXL 9808 nM (IC50) |
JAK2 24547 nM (IC50) |
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
0.03 μM
Compound: 6, GSK2656157
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Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis
Inhibition of thapsigargin-induced autophosphorylation of PERK in human A549 cells preincubated for 1 hr followed by thapsigargin-induction measured after 1 hr by Western blotting analysis
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[PMID: 24900593] |
GSK2656157 results in inhibition of PERK activation as well as decreases in the downstream substrates, phospho-eIF2α, ATF4, and CHOP with an IC50 in the range of 10-30 nM in the BxPC3 pancreatic tumor cell line. Cells that are exposed to 1 μM GSK2656157 before UPR induction are able to block this effect on de novo protein synthesis[1].
GSK2656157 causes the activation of another eIF2α kinase to compensate for the loss of PERK activity in HT1080 cells. GSK2656157 inhibits the growth of the HT1080 cells[2].
GSK2656157 inhibits LPS-induced IL-1β production, LPS-induced Caspase 1 activation and LPS-induced eIF-2α phosphorylation, but does not inhibit LPS-induced TNF-α production[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1337532-29-2
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Appearance Solid
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Molecular Weight 416.45
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Formula C23H21FN6O
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Color White to light yellow
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SMILES
CC1=CC=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3F)=O)=N1
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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 1 year -20°C 6 months
Publications (65)
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Journal Impact Factor
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Most Recent
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Nature
2026 Apr;652(8112):1339-1348. PMID: 41813904 -
Cell Metab
The microbial metabolite trimethylamine N-oxide promotes antitumor immunity in triple-negative breast cancer. [Abstract]2022 Apr 5;34(4):581-594.e8. PMID: 35278352 -
Mol Cell
2023 Sep 21;83(18):3303-3313.e6. PMID: 37683648 -
Nat Commun
Liver-specific gene PGRMC1 blocks c-Myc-induced hepatocarcinogenesis through ER stress-independent PERK activation. [Abstract]2025 Jan 2;16(1):50. PMID: 39747098 -
Nat Commun
Loss of TRIM29 mitigates viral myocarditis by attenuating PERK-driven ER stress response in male mice. [Abstract]2024 Apr 25;15(1):3481. PMID: 38664417 -
Nat Commun
2022 Oct 16;13(1):6108. PMID: 36245009 -
Adv Sci (Weinh)
Repurposing Cardiac Glycosides to Potentiate CD47 Blockade through Calreticulin-mediated Phagocytic Effects for Lung Cancer Treatment. [Abstract]2025 Sep 23:e08245. PMID: 40985476 -
Cell Discov
Selective and competitive functions of the AAR and UPR pathways in stress-induced angiogenesis. [Abstract]2021 Oct 26;7(1):98. PMID: 34697290 -
Sci Adv
Targeting highly pathogenic coronavirus-induced apoptosis reduces viral pathogenesis and disease severity. [Abstract]2021 Jun 16;7(25):eabf8577. PMID: 34134991 -
Gut Microbes
Bacterial amyloid curli activates the host unfolded protein response via IRE1α in the presence of HLA-B27. [Abstract]2024 Jan-Dec;16(1):2392877. PMID: 39189642 -
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J Immunother Cancer
Neovascular pruning by IDO1 inhibitors can potentiate immunogenic cytotoxicity of ischemia-targeted agents to synergistically enhance anti-PD-1 responsiveness. [Abstract]2025 May 30;13(5):e011398. PMID: 40447318 -
Cardiovasc Diabetol
Melatonin attenuates diabetic cardiomyopathy by increasing autophagy of cardiomyocytes via regulation of VEGF-B/GRP78/PERK signaling pathway. [Abstract]2024 Jan 9;23(1):19. PMID: 38195474 -
Pharmacol Res
ER stress sensor PERK drives ferroptosis by disrupting MAMs-mediated mitochondrial homeostasis and promoting mtROS accumulation in acute myocardial infarction. [Abstract]2025 Dec:222:108029. PMID: 41205728 -
J Neuroinflammation
Thioredoxin-interacting protein links endoplasmic reticulum stress to inflammatory brain injury and apoptosis after subarachnoid haemorrhage. [Abstract]2017 May 11;14(1):104. PMID: 28490373
GSK2656157 purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2017 May 11;14(1):104. [Abstract]
GSK2656157 treatment suppresses PERK autophosphorylation and TXNIP expression; STF083010 treatment inhibits IRE1α endonuclease activity and TXNIP expression. Representative Western blot and densitometric quantification of protein band optical densities for p-PERK, p-eIF2α/eIF2α, ATF-5, ChREBP, splicing XBP1 (sXBP1) and TXNIP. TXNIP expression is downregulated by GSK2656157 and STF083010 treatment.
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Cell Death Dis
PERK signaling through C/EBPδ contributes to ER stress-induced expression of immunomodulatory and tumor promoting chemokines by cancer cells. [Abstract]2021 Nov 1;12(11):1038. PMID: 34725321 -
Free Radic Biol Med
Endoplasmic reticulum stress-mediated autophagy activation is involved in cadmium-induced ferroptosis of renal tubular epithelial cells. [Abstract]2021 Nov 1:175:236-248. PMID: 34520822 -
Neoplasia
2025 Apr 18:65:101165. PMID: 40252311 -
NPJ Breast Cancer
Endoplasmic reticulum stress inhibits AR expression via the PERK/eIF2α/ATF4 pathway in luminal androgen receptor triple-negative breast cancer and prostate cancer. [Abstract]2022 Jan 10;8(1):2. PMID: 35013318 -
Cell Death Discov
Inhibiting HSP27 activates the XBP1s/CerS1 interplay, which triggers DRP1-driven mitophagy, thereby protecting against cell death and promoting the KSHV lytic cycle in primary effusion lymphoma cells. [Abstract]2026 Feb 26. PMID: 41748537 -
Cell Death Discov
Arnicolide D induces endoplasmic reticulum stress-mediated oncosis via ATF4 and CHOP in hepatocellular carcinoma cells. [Abstract]2024 Mar 12;10(1):134. PMID: 38472168 -
Cell Rep
Translocational attenuation mediated by the PERK-SRP14 axis is a protective mechanism of unfolded protein response. [Abstract]2024 Jun 27;43(7):114402. PMID: 38943644 -
Ecotoxicol Environ Saf
Chlorocholine chloride exposure induced spermatogenic dysfunction via iron overload caused by AhR/PERK axis-dependent ferritinophagy activation. [Abstract]2024 Apr 1:274:116193. PMID: 38460407 -
Ecotoxicol Environ Saf
Mitochondrial dysfunction and endoplasmic reticulum stress induced by activation of PPARα leaded testicular to apoptosis in SD rats explored to di-(2-ethylhexyl) phthalate (DEHP). [Abstract]2023 Dec:268:115711. PMID: 37979351 -
Ecotoxicol Environ Saf
Arsenic induces ferroptosis and acute lung injury through mtROS-mediated mitochondria-associated endoplasmic reticulum membrane dysfunction. [Abstract]2022 Jun 15;238:113595. PMID: 35525119 -
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 -
Cancer Cell Int
HNRNPA2B1 regulates the epithelial-mesenchymal transition in pancreatic cancer cells through the ERK/snail signalling pathway. [Abstract]2017 Jan 10:17:12. PMID: 28077929 -
Cell Biol Toxicol
Deciphering SPP1-related macrophage signaling in the pathogenesis of intervertebral disc degeneration. [Abstract]2025 Jan 18;41(1):33. PMID: 39825191 -
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 -
Biochem Pharmacol
VPS34-IN1 induces apoptosis of ER + breast cancer cells via activating PERK/ATF4/CHOP pathway. [Abstract]2023 Aug:214:115634. PMID: 37290596 -
J Gastroenterol
Mitochondrial stress induces hepatic stellate cell activation in response to the ATF4/TRIB3 pathway stimulation. [Abstract]2023 Jul;58(7):668-681. PMID: 37150773 -
J Pathol
Function and mutual interaction of BiP-, PERK-, and IRE1α-dependent signalling pathways in vascular tumours. [Abstract]2020 Jun;251(2):123-134. PMID: 32166747 -
Int J Mol Sci
GSK2656157, a PERK Inhibitor, Alleviates Pyroptosis of Macrophages Induced by Mycobacterium Bacillus Calmette-Guerin Infection. [Abstract]2023 Nov 12;24(22):16239. PMID: 38003429 -
Int J Mol Sci
Thioredoxin-Interacting Protein Mediates Apoptosis in Early Brain Injury after Subarachnoid Haemorrhage. [Abstract]2017 Apr 18;18(4). pii: E854. PMID: 28420192
GSK2656157 purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2017 Apr 18;18(4). pii: E854. [Abstract]
GSK2656157 treatment suppresses TXNIP expression and the number of TUNEL-positive cells. TXNIP expression is significantly suppressed by the GSK2656157 (300 μg) treatment.
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mBio
The intracellular agent of Q fever, Coxiella burnetii, alters human alveolar macrophage metabolism and mitochondrial physiology. [Abstract]2025 Sep 10;16(9):e0143625. PMID: 40823830 -
Int Immunopharmacol
Ferroptosis is involved in Staphylococcus aureus-induced mastitis through autophagy activation by endoplasmic reticulum stress. [Abstract]2024 Jul 29:140:112818. PMID: 39083924 -
Toxicology
Differential susceptibility of BRL cells with/without insulin resistance and the role of endoplasmic reticulum stress signaling pathway in response to acrylamide-exposure toxicity effects in vitro. [Abstract]2024 May:504:153800. PMID: 38604440 -
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 -
J Dairy Sci
AMPK-endoplasmic reticulum stress axis contributes to lipopolysaccharide-caused mitochondrial dysfunction by regulating mitochondria-associated membrane function in bovine hepatocytes. [Abstract]2023 Jul;106(7):5146-5164. PMID: 37225589 -
ACS Omega
2025 Oct 17;10(42):50208-50217. PMID: 41179162 -
Mol Neurobiol
Sigma-1 Receptor Activation Alleviates iBRB Dysfunction after I/R Injury by Inhibiting Endoplasmic Reticulum Stress-Dependent Autophagy. [Abstract]2025 Jun 1. PMID: 40450632 -
Appl Microbiol Biotechnol
Recombinant Treponema pallidum protein Tp0768 promotes proinflammatory cytokine secretion of macrophages through ER stress and ROS/NF-κB pathway. [Abstract]2021 Jan;105(1):353-366. PMID: 33216161 -
FASEB J
SNAI1 is upregulated during muscle regeneration and represses FGF21 and ATF3 expression by directly binding their promoters. [Abstract]2022 Jul;36(7):e22401. PMID: 35726676 -
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Oncol Rep
LRRC59 inhibits perk pathway‑induced apoptosis and promotes cell proliferation, migration and invasion in colorectal cancer cells. [Abstract]2026 Jan;55(1):5. PMID: 41133451 -
J Biol Chem
Identification of inhibitors for the trans-membrane Trypanosoma cruzi eIF2α kinase relevant for parasite proliferation. [Abstract]2023 Jul;299(7):104857. PMID: 37230387 -
Cytokine
Triptolide impacts CSF1R expression and reprograms the suppressive function of myeloid-derived suppressor cells via targeting the ER stress pathway. [Abstract]2026 Jan:197:157068. PMID: 41197245 -
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 -
Cell Signal
Unfolded protein response-activated NLRP3 inflammasome contributes to pyroptotic and apoptotic podocyte injury in diabetic kidney disease via the CHOP-TXNIP axis. [Abstract]2025 Jun:130:111702. PMID: 40020889 -
Brain Res Bull
Methamphetamine induces GSDME-dependent cell death in hippocampal neuronal cells through the endoplasmic reticulum stress pathway. [Abstract]2020 Sep;162:73-83. PMID: 32544512 -
Brain Res Bull
Inhibition of protein tyrosine phosphatase 1B protects against sevoflurane-induced neurotoxicity mediated by ER stress in developing brain. [Abstract]2019 Mar:146:28-39. PMID: 30553844 -
Vet Res
Glaesserella parasuis infection triggers endoplasmic reticulum stress-mediated pyroptosis via PERK/eIF2α/ATF4 axis and metabolic reprogramming in porcine alveolar macrophages. [Abstract]2025 Jul 15;56(1):150. PMID: 40665414 -
Vascul Pharmacol
Protein tyrosine phosphatase 1B regulates endothelial endoplasmic reticulum stress; role in endothelial dysfunction. [Abstract]2018 Oct:109:36-44. PMID: 29894845 -
J Anim Sci
The endoplasmic reticulum stress and B cell lymphoma-2 related ovarian killer participate in docosahexaenoic acid-induced adipocyte apoptosis in grass carp (Ctenopharyngodon idellus). [Abstract]2023 Jan 3:101:skad101. PMID: 37067261 -
Fish Shellfish Immunol Rep
Protein kinase-like ER kinase (PERK) regulates autophagy of hemocytes in antiviral immunity of Pacific oyster Crassostrea gigas. [Abstract]2020 Nov 28:1:100002. PMID: 36419779 -
Vet Microbiol
Pasteurella multocida toxin induces apoptosis of respiratory epithelial cells by activating the PERK-NF-κB-DR5 signaling axis. [Abstract]2026 Apr:315:110921. PMID: 41637966 -
Animals (Basel)
NEFA Promotes Autophagosome Formation through Modulating PERK Signaling Pathway in Bovine Hepatocytes. [Abstract]2021 Nov 28;11(12):3400. PMID: 34944177 -
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 -
J Steroid Biochem Mol Biol
Elucidation of the mechanism of NEFA-induced PERK-eIF2α signaling pathway regulation of lipid metabolism in bovine hepatocytes. [Abstract]2021 Jul:211:105893. PMID: 33819629
GSK2656157 purchased from MedChemExpress. Usage Cited in: J Steroid Biochem Mol Biol. 2021 Jul:211:105893. [Abstract]
Pretreatment with GSK2656157 (1 μM) alleviated the NEFA-induced increase in protein abundance and mRNA levels of PERK, eIF2α, ATF4, and CHOP vis a vis treatment with 1.2 mM NEFA alone.
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Biomarkers
2022 Jul;27(5):470-482. PMID: 35400257 -
bioRxiv
Ceramide-induced Endoplasmic Reticulum Stress as a Targetable Vulnerability in Endocrine Therapy-Resistant Breast Cancer. [Abstract]2025 Aug 22:2025.08.18.670862. PMID: 40894774 -
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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 -
Oxid Med Cell Longev
Ganoderic Acid D Protects Human Amniotic Mesenchymal Stem Cells against Oxidative Stress-Induced Senescence through the PERK/NRF2 Signaling Pathway. [Abstract]2020 Jul 27;2020:8291413. PMID: 32774686
GSK2656157 purchased from MedChemExpress. Usage Cited in: Oxid Med Cell Longev. 2020 Jul 27;2020:8291413. [Abstract]
GSK2656157 not only inhibits the expression of p-PERK, but also reduces the expression of NRF2 in the nucleus (n-NRF2) and total NRF2 (t-NRF2) proteins.
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Solvent & Solubility
DMSO : 8.33 mg/mL (20.00 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: ≥ 0.5 mg/mL (1.20 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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: ≥ 0.5 mg/mL (1.20 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: 0.5% HPMC/0.2% Tween-80 in Saline water
Solubility: 4.17 mg/mL (10.01 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%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.
Protocol
BxPC3 (human pancreatic adenocarcinoma) or LL/2 (murine lung carcinoma) cells are treated with DMSO or various concentrations of GSK2656157 for 1 hour, followed by addition of 5 μg/mL tunicamycin or 1 μM thapsigargin for an additional 6 hours to induce endoplasmic reticulum-stress. Cells are lysed in cold radioimmunoprecipitation assay (RIPA) buffer [150 mM NaCl, 50 mM Tris-Cl pH 7.5, 0.25% sodium deoxycholate, 1% NP-40, protease inhibitors, and 100 mM sodium orthovanadate]. Clarified lysates are resolved by SDS-PAGE and transferred to nitrocellulose membrane using NuPAGE system. Blots are incubated with antibodies to total PERK, p-eIF-2α Ser51, total eIF-2α, ATF4, and CHOP. IRDye700DX-labeled goat anti-mouse immunoglobulin G (IgG), IRDye800-CW donkey anti-goat IgG, and IRDye800-CW goat anti-rabbit IgG are used as secondary antibodies. Proteins are detected on the Odyssey Infrared Imager.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BxPC3 cells are treated with DMSO or 1 μM GSK2656157 for 1 hour before adding 5 μg/mL tunicamycin for an additional hour. Cells are metabolically labeled with 125 μCi 35S-methionine for the subsequent 1 hour. Cells are lysed in cold RIPA buffer and lysates are resolved by SDS-PAGE, followed by exposure to a phosphorimager screen. Control cells are also pretreated with 100 μM cyclohexamide for 1 hour followed by metabolic labeling. Radioisotope incorporation is quantitated using ImageQuant 5.2 software.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Exponentially growing HPAC (5×106 cells/mouse), Capan-2 (10×106 cells/mouse), or NCI-H929 (1×6 cells/mouse) cells are implanted subcutaneously into the right flank of 8- to 12-week-old female SCID mice. Similarly, 10×106 BxPC3 cells per mouse are implanted in female nude mice. When the tumors reached approximately 200 mm3 in size, the animals are weighed, and block randomized according to tumor size into treatment groups of 8 mice each. Mice are dosed orally with the formulating vehicle or GSK2656157. Mice are weighed and tumors measured by calipers twice weekly. Tumor volumes are calculated. The percentage of tumor growth inhibition is calculated on each day of tumor measurement using the formula: 100× [1 − (average growth of the compound-treated tumors/average growth of vehicle-treated control tumors)].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
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Handling Instructions (2659 KB)
References
[1]. Atkins C, et al. Characterization of a novel PERK kinase inhibitor with antitumor and antiangiogenic activity. Cancer Res. 2013 Mar 15;73(6):1993-2002. [Content Brief]
[2]. Krishnamoorthy J, et al. Evidence for eIF2α phosphorylation-independent effects of GSK2656157, a novel catalytic inhibitor of PERK with clinical implications. Cell Cycle. 2014 Mar 1;13(5):801-6. [Content Brief]
[3]. Ando T, et al. GSK2656157, a PERK inhibitor, reduced LPS-induced IL-1β production through inhibiting Caspase 1 activation in macrophage-like J774.1 cells. Immunopharmacol Immunotoxicol. 2016 Aug;38(4):298-302. [Content Brief]
[4]. Zhao Q, et al. Thioredoxin-interacting protein links endoplasmic reticulum stress to inflammatory brain injury and apoptosis after subarachnoid haemorrhage. J Neuroinflammation. 2017 May 11;14(1):104. [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 | 2.4012 mL | 12.0062 mL | 24.0125 mL | 60.0312 mL |
| 5 mM | 0.4802 mL | 2.4012 mL | 4.8025 mL | 12.0062 mL | |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4012 mL | 6.0031 mL | |
| 15 mM | 0.1601 mL | 0.8004 mL | 1.6008 mL | 4.0021 mL |