- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 1337532-29-2] GSK2656157
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-13820 |
| Brand: | MCE |
| CAS: | 1337532-29-2 |
Overview
| MDL | MFCD27997885 |
|---|---|
| Molecular Weight | 416.45 |
| Molecular Formula | C23H21FN6O |
| SMILES | CC1=CC=CC(CC(N2CCC3=C2C=CC(C4=CN(C)C5=NC=NC(N)=C54)=C3F)=O)=N1 |
26 Publications Citing Use of MCE
- [1]Cell Metab. 2022 Mar 8;S1550-4131(22)00054-7.
- [2]Sci Adv. 2021 Jun 16;7(25):eabf8577.
- [3]Nat Commun. 2022 Oct 16;13(1):6108.
- [4]Cell Death Dis. 2021 Nov 1;12(11):1038.
- [5]Cell Biol Toxicol. 2022 Jan 14.
- [6]Cell Discov. 2021 Oct 26;7(1):98.
- [7]Free Radic Biol Med. 2021 Sep 11;S0891-5849(21)00721-8.
- [8]NPJ Breast Cancer. 2022 Jan 10;8(1):2.
- [9]J Pathol. 2020 Jun;251(2):123-134.
- [10]J Neuroinflammation. 2017 May 11;14(1):104.
- [11]Oxid Med Cell Longev. 05 Aug 2022.
- [12]Oxid Med Cell Longev. 2020 Jul 27;2020:8291413.
- [13]FASEB J. 2022 Jul;36(7):e22401.
- [14]Ecotoxicol Environ Saf. 2022 Jun 15;238:113595.
- [15]Int J Mol Sci. 2017 Apr 18;18(4). pii: E854.
- [16]Cancer Cell Int. 2017 Jan 10;17:12.
- [17]Vascul Pharmacol. 2018 Oct;109:36-44.
- [18]J Steroid Biochem Mol Biol. 2021, 105893.
- [19]J Funct Foods. July 2022, 105116.
- [20]Appl Microbiol Biotechnol. 2020 Nov 20;1-14.
- [21]Brain Res Bull. 2020 Sep;162:73-83.
- [22]Brain Res Bull. 2019 Mar;146:28-39.
- [23]Biomarkers. 2022 Apr 21;1-13.
- [24]Animals (Basel). 2021 Nov 28;11(12):3400.
- [25]Fish and Shellfish Immunology Reports. 2020, 100002.
- [26]Methods Mol Biol. 2018;1711:351-398.
Summary
GSK2656157 is a selective and ATP-competitive inhibitor of protein kinase R (PKR)-like endoplasmic reticulum kinase ( PERK ) with an IC 50 of 0.9 nM.
IC50 & Target
|
EIF2AK3 (PERK) 0.9 nM (IC 50 ) |
EIF2AK1 (HRI) 460 nM (IC 50 ) |
BRK 905 nM (IC 50 ) |
EIF2AK2 (PKR) 905 nM (IC 50 ) |
MEKK3 954 nM (IC 50 ) |
Aurora B 1259 nM (IC 50 ) |
||
|
KHS 1764 nM (IC 50 ) |
LCK 2344 nM (IC 50 ) |
MLK2 2796 nM (IC 50 ) |
MEKK3 2847 nM (IC 50 ) |
ALK5 3020 nM (IC 50 ) |
MLCK2 3039 nM (IC 50 ) |
||
|
EIF2AK4(GCN2) 3162 nM (IC 50 ) |
c-MER 3431 nM (IC 50 ) |
PI3Kγ 3802 nM (IC 50 ) |
WNK3 5951 nM (IC 50 ) |
LRRK2 6918 nM (IC 50 ) |
ROCK1 7244 nM (IC 50 ) |
||
|
MSK1 8985 nM (IC 50 ) |
NEK1 9807 nM (IC 50 ) |
AXL 9808 nM (IC 50 ) |
JAK2 24547 nM (IC 50 ) |
||||
In Vitro
GSK2656157 results in inhibition of PERK activation as well as decreases in the downstream substrates, phospho-eIF2α, ATF4, and CHOP with an IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
GSK2656157 (1.5-150 mg/kg, p.o.) results in dose-dependent inhibition of phospho-PERK Thr980, with more than 80% inhibition at 50 and 150 mg/kg. GSK2656157 (50-150 mg/kg, p.o.) results in dose-dependent inhibition of tumor growth in human tumor xenograft models [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
1M HCl : 100 mg/mL ( 240.12 mM ; ultrasonic and adjust pH to 1 with HCl)
DMSO : 8.33 mg/mL ( 20.00 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.4012 mL | 12.0062 mL | 24.0125 mL |
| 5 mM | 0.4802 mL | 2.4012 mL | 4.8025 mL |
| 10 mM | 0.2401 mL | 1.2006 mL | 2.4012 mL |
-
1.
Add each solvent one by one: 0.5% HPMC >> 0.2%Tween80
Solubility: 4.17 mg/mL (10.01 mM); Suspended solution; Need ultrasonic
-
2.
-
3.
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
-
4.
Add each solvent one by one: 10% DMSO >> 90% corn oil
Solubility: ≥ 0.5 mg/mL (1.20 mM); Clear solution
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.
- [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.
- [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.
- [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.
Synonyms
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.