GSK621
Based on 9 publication(s) in Google Scholar
GSK621 is a specific AMPK activator, with IC50 values of 13-30 μM for AML cells. GSK621 induces autophagy and apoptosis. GSK621 induces eiF2α phosphorylation-a hallmark of UPR activation.
For research use only. We do not sell to patients.
- Purity : 98.03%
- CAS No.: 1346607-05-3
- Formula: C26H20ClN3O5
- Molecular Weight:489.91
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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DorsomorphinAMPK Inhibitor -
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HTH-01-015NUAK1/ARK5 Inhibitor -
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Bempedoic acidACL Inhibitor/AMPK Activator -
HY-13417R
AICAR (Standard)AMPK Activator
Publications Citing Use of MedChemExpress (MCE) GSK621
More- Bone Res. 2025 Feb 14;13(1):23. [Abstract]
- Cell Death Discov. 2026 Jun 23. [Abstract]
- EMBO J. 2021 Nov 2;40(21):e108028. [Abstract]
- Life Sci. 2025 Aug 1:374:123687. [Abstract]
- Cancers (Basel). 2023 Apr 23;15(9):2427. [Abstract]
- Cell Signal. 2026 Feb:138:112260. [Abstract]
- Mol Biol Rep. 2024 Sep 21;51(1):1003. [Abstract]
- Res Sq. 2026 Jan 28.
- Research Square Preprint. 2024 Dec 22.
Customer Validation & Images
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Cell Proliferation/Viability Assay
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WB
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Cell Proliferation/Viability Assay
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WB
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Cell Imaging/Staining
All AMPK Isoforms
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Biological Activity
Description
In Vitro
GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation[1].
GSK621 (30 μM) induces autophagy and apoptosis[1].
GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MV4-11, OCI-AML3, OCI-AML2, HL-60, Kasumi, HEL, UT7, NB4, TF-1, KG1A, Nomo p28, SKM-1, U937, YHP1, MOLM-14, Mo7e, K562, MOLM-13, EOL-1, SET-2 AML cell lines. 0-30 μM.
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Concentration:0-30 μM.
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Incubation Time:4 d.
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Result:IC50 values ranged from 13 to 30 μM.
Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines.
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Cell Line:AML cell lines and primary AML samples.
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Concentration:30 μM.
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Incubation Time:24 h.
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Result:Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:MOLM-14 cells xenografted into nude mice[1].
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Dosage:30 mg/kg.
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Administration:IP twice daily.
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Result:Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily.
Chemical Information
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CAS No. 1346607-05-3
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Appearance Solid
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Molecular Weight 489.91
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Formula C26H20ClN3O5
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Color Off-white to light yellow
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SMILES
O=C1NC2=C(N(C3=CC=C(C4=CC=CC(OC)=C4O)C=C3)C(Cl)=C2)C(N1C5=CC=CC(OC)=C5)=O
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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 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Bone Res
Matrix stiffness regulates nucleus pulposus cell glycolysis by MRTF-A-dependent mechanotransduction. [Abstract]2025 Feb 14;13(1):23. PMID: 39952914 -
Cell Death Discov
AMPK/ SIRT1 signaling pathway activation acts on PGC-1α/ PPARγ to alleviate sepsis-acquired weakness. [Abstract]2026 Jun 23. PMID: 42337228 -
EMBO J
2021 Nov 2;40(21):e108028. PMID: 34472622
GSK621 purchased from MedChemExpress. Usage Cited in: EMBO J. 2021 Nov 2;40(21):e108028. [Abstract]
The crystal violet assay were performed in 293T cells transfected with shRNAs targeting NTC, CARS, CaMKK2 or AMPKγ2 and further treated with cystine‐deficient medium for 24 h with or without 100 μM PT1 or 30 μM GSK621.
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Life Sci
GSK621 ameliorates lipid accumulation via AMPK pathways and reduces oxidative stress in hepatocytes in vitro and in obese mice in vivo. [Abstract]2025 Aug 1:374:123687. PMID: 40334907
GSK621 purchased from MedChemExpress. Usage Cited in: Life Sci. 2025 Aug 1:374:123687. [Abstract]
Detection of HepG2 (left) and AML12 (right) cell proliferation under GSK621 stimulation. GSK621 was diluted to 5 μM, 10 μM and 20 μM and treated for 6 hours. Cell proliferation rate was detected by CCK8 assay.
GSK621 purchased from MedChemExpress. Usage Cited in: Life Sci. 2025 Aug 1:374:123687. [Abstract]
Expression of AMPK and p-AMPK at different GSK621 concentrations. HepG2 cells were treated with 5 μM, 10 μM and 20 μM GSK621 for 6 hours, and the expression of AMPK and p-AMPK was detected by Western blot analysis.
GSK621 purchased from MedChemExpress. Usage Cited in: Life Sci. 2025 Aug 1:374:123687. [Abstract]
EdU assay was used to detect HepG2 cell proliferation. The middle column was used to stimulate HepG2 cells with 0.25 μM FFAs for 24 h (10x magnification). The right column was used to stimulate HepG2 cells with 10 μM GSK621 for 6 h before FFA treatment.
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Cancers (Basel)
High-Dosage NMN Promotes Ferroptosis to Suppress Lung Adenocarcinoma Growth through the NAM-Mediated SIRT1-AMPK-ACC Pathway. [Abstract]2023 Apr 23;15(9):2427. PMID: 37173894
GSK621 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Apr 23;15(9):2427. [Abstract]
A549 and SPCA1 cells were treated with the SIRT1 agonist (CAY10602) or inhibitor (Selisistat), AMPK agonist (GSK621: 10 μM) or inhibitor (dorsomorphin), or combinations of the above agents, followed by high-dose NMN treatment for various intervals as indicated. Results of Western blot analysis of NAMPT, SIRT1, p-AMPK, and p-ACC protein expressions.
GSK621 purchased from MedChemExpress. Usage Cited in: Cancers (Basel). 2023 Apr 23;15(9):2427. [Abstract]
AMPK agonist (GSK621: 10 μM). Representative images of colony formation for A549 and SPCA1 cells in indicated groups.
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Cell Signal
Exercise attenuates hepatic lipid accumulation via VDR/AMPK-mediated autophagy activation in vitamin D-deficient mice. [Abstract]2026 Feb:138:112260. PMID: 41290053 -
Mol Biol Rep
Poricoic acid a ameliorates high glucose-induced podocyte injury by regulating the AMPKα/FUNDC1 pathway. [Abstract]2024 Sep 21;51(1):1003. PMID: 39305364 -
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Solvent & Solubility
In Vitro:
DMSO : 12.5 mg/mL (25.51 mM; ultrasonic and adjust pH to 1 with HCl; 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: 1.25 mg/mL (2.55 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 1.25 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 (12.5 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: ≥ 1.25 mg/mL (2.55 mM); Suspended solution
This protocol yields a suspended solution of ≥ 1.25 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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: 50% PEG300 50% Saline
Solubility: 10 mg/mL (20.41 mM); Suspended solution; Need ultrasonic
In Vivo Dissolution Calculator
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.
Protocols
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Kinase activity and phosphorylation assays
Kinase activity assays measure the ability of kinases to transfer phosphate groups from ATP to specific substrates, while phosphorylation assays detect the presence and levels of phosphorylated proteins. Common methods include radiolabeled ATP incorporation (e. g. ,), ADP release detection via bioluminescence (e. g. ,[3]), enzyme-linked immunosorbent assays (ELISA) for phospho-specific epitopes (e. g. ,[6]), and microtiter-based formats for high-throughput screening (e. g. ,[8]). The ADP-Glo assay quantifies kinase activity by measuring ADP produced during phosphorylation using a luciferase-based system. Radiometric assays involve autoradiography or scintillation counting after incorporation of 32P-labeled ATP into substrate proteins. ELISA-based approaches rely on phospho-specific antibodies to detect activated kinases in cell lysates or purified samples.
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Western Blot
Western blotting (WB) is a commonly used experimental method in molecular biology, biochemistry, and immunogenetics for identifying and quantifying target proteins. It combines gel electrophoresis with immunoassay, enabling researchers to analyze protein expression, post-translational modifications, and molecular weight.
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Autophagy
Autophagy is a process in which eukaryotic cells use lysosomes to degrade their own cytoplasmic proteins and damaged organelles under the regulation of autophagy related gene (Atg). Microtubule-associated proteins light chain 3 (LC3) is recognized as autophagy marker, which transfers from cytoplasmic LC3 (LC3-I) to membrane type (LC3-II). LC3-II/I ratio could be detected by Western Blot and fluorescence microscopy.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Lysosome and acidic-vesicle live-cell staining
Lysosome and acidic-vesicle live-cell staining detects acidic intracellular compartments by using membrane-permeant acidotropic probes that accumulate in low-pH vesicles, including lysosomes, late endosomes, autolysosomes, and acidic phagosomes. LysoTracker staining is commonly used as an intensity-based readout of acidic lysosomal compartment abundance or enlargement, while acridine orange produces green fluorescence in less concentrated compartments and red fluorescence after concentration-dependent accumulation in acidic vesicular organelles. Loss or reduction of acridine-orange red signal can be used as a readout of lysosomal membrane permeabilization or reduced acidic-vesicle integrity. This protocol is designed for live cultured cells and can be adapted for fluorescence microscopy, high-content imaging, plate-reader readout, or flow cytometry when the selected literature supports the readout. Because these dyes report acidotropic accumulation rather than lysosome identity alone,
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Protocol for Kinase activity and phosphorylation assays
Kinase activity assays measure transfer of phosphate from ATP to a protein or peptide substrate, generating phosphorylated substrate, ADP, or incorporated radiolabeled phosphate as the readout; phosphorylation assays measure site-specific phosphorylation in cells or tissues as a proxy for kinase-pathway activation, inhibition, or substrate regulation. Phosphorylation can be detected by phospho-specific Western blot, immunoprecipitation kinase assay, phospho-immunofluorescence, phospho-flow cytometry, luminescent ADP detection, radiolabeled ATP incorporation, or reporter-based pathway assays, and these readouts can be applied to cancer cells, primary neurons, mouse tumors, organoids, inflammatory macrophages, ferroptosis studies, and mitophagy studies when the kinase target is biologically relevant.
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Macroautophagy Solutions
Macroautophagy is a conserved lysosome-dependent degradation pathway in which cytoplasmic material is sequestered into double-membrane autophagosomes and delivered to lysosomes for degradation and recycling. The pathway supports cellular homeostasis during nutrient limitation, organelle stress, protein-aggregate accumulation, infection, differentiation, and tissue remodeling by coupling cargo sequestration, autophagosome maturation, lysosomal fusion, and degradation of cargo-derived macromolecules. The core molecular sequence includes initiation by nutrient- and stress-regulated autophagy machinery, autophagosome nucleation, LC3/ATG8-family conjugation to autophagosomal membranes, cargo selection through receptors such as SQSTM1/p62, autophagosome-lysosome fusion, and lysosomal degradation. LC3 was identified as a mammalian homolog of yeast Atg8 that localizes to autophagosomal membranes after processing, and p62/SQSTM1 was shown to connect ubiquitinated cargo with autophagic degradati
Purity & Documentation
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.0412 mL | 10.2060 mL | 20.4119 mL | 51.0298 mL |
| 5 mM | 0.4082 mL | 2.0412 mL | 4.0824 mL | 10.2060 mL | |
| 10 mM | 0.2041 mL | 1.0206 mL | 2.0412 mL | 5.1030 mL | |
| 15 mM | 0.1361 mL | 0.6804 mL | 1.3608 mL | 3.4020 mL | |
| 20 mM | 0.1021 mL | 0.5103 mL | 1.0206 mL | 2.5515 mL | |
| 25 mM | 0.0816 mL | 0.4082 mL | 0.8165 mL | 2.0412 mL |
GSK621 Related Classifications
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