| Field | Specification |
|---|---|
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C26H20ClN3O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
GSK621 is a specific activator of AMPK, with IC50 values of 13-30 μM in AML cells. It induces autophagy and apoptosis, and it triggers eiF2α phosphorylation, a hallmark of UPR activation[1]. It is supplied as an off-white to light yellow solid (C26H20ClN3O5, MW 489.91) at 98.03% purity.
Physical & Chemical Properties
| CAS Number | 1346607-05-3 |
|---|---|
| Molecular Formula | C26H20ClN3O5 |
| Molecular Weight | 489.91 g/mol |
| Purity | 98.03% |
| Appearance | Solid |
| Color | Off-white to light yellow |
| 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 |
| Signaling Pathway | Epigenetics; PI3K/Akt/mTOR; Autophagy; Apoptosis |
| Solubility | In Vitro: DMSO: 12.5 mg/mL (25.51 mM; Requires sonication and adjust pH to 1 with HCl; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | Powder: -20°C, 3 years; 4°C, 2 years. In solvent: -80°C, 2 years; -20°C, 1 year. |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 12.5 mg/mL (25.51 mM) | requires sonication and adjust pH to 1 with HCl; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 2 years) or -20°C (up to 1 year); avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | 1.25 mg/mL (2.55 mM); suspension; requires sonication |
| How to prepare | Gives a suspension at 1.25 mg/mL. The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 1.25 mg/mL (2.55 mM); suspension |
| How to prepare | Gives a suspension at ≥ 1.25 mg/mL (saturation not determined). The suspension is suitable for oral and intraperitoneal dosing. For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 1.25 mg/mL (2.55 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 1.25 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (12.5 mg/mL) to 900 μL corn oil. |
Direct preparation of the working solution
These formulations are prepared directly, without a DMSO stock; use them promptly after preparation.
Protocol 4
| Composition | 50% PEG300 + 50% saline |
|---|---|
| Result | 10 mg/mL (20.41 mM); suspension; requires sonication |
Data provided by the manufacturer.
In Vitro
GSK621 at 30 μM induces phosphorylation of AMPKα T172, ACC (S79) and ULK1 (S555)[1]. At 30 μM, GSK621 also induces autophagy and apoptosis[1]. In AML cells, GSK621 treatment additionally induces PERK phosphorylation, a marker of ER stress[1].
Cell Proliferation Assay[1]
| 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. |
|---|---|
| Concentration | 0-30 μM. |
| Incubation Time | 4 d. |
| Result | IC50 values ranged from 13 to 30 μM. Reduced the proliferation of all 20 lines and increased apoptosis in 17 (85%) lines. |
Autophagy assay in cells[1].
| Cell Line | AML cell lines and primary AML samples. |
|---|---|
| Concentration | 30 μM. |
| Incubation Time | 24 h. |
| Result | Induced the formation of numerous intracytoplasmic vacuoles including autophagosomes. |
In Vivo
In a MOLM-14 cell xenograft, GSK621 (30 mg/kg, ip twice daily) shows significant anti-tumor activity[1].
| Animal Model | MOLM-14 cells xenografted into nude mice[1]. |
|---|---|
| Dosage | 30 mg/kg. |
| Administration | IP twice daily. |
| Result | Reduced leukemia growth and significantly extended survival compared to vehicle-treated animals or those treated with 10 mg/kg twice daily. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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Matrix stiffness regulates nucleus pulposus cell glycolysis by MRTF-A-dependent mechanotransduction. Bone Res 2025 Feb 14;13(1):23. PMID: 39952914
AMPK/ SIRT1 signaling pathway activation acts on PGC-1α/ PPARγ to alleviate sepsis-acquired weakness. Cell Death Discov 2026 Jun 23. PMID: 42337228
CARS senses cysteine deprivation to activate AMPK for cell survival. EMBO J 2021 Nov 2;40(21):e108028. PMID: 34472622
GSK621 ameliorates lipid accumulation via AMPK pathways and reduces oxidative stress in hepatocytes in vitro and in obese mice in vivo. Life Sci 2025 Aug 1:374:123687. PMID: 40334907
High-Dosage NMN Promotes Ferroptosis to Suppress Lung Adenocarcinoma Growth through the NAM-Mediated SIRT1-AMPK-ACC Pathway. Cancers (Basel) 2023 Apr 23;15(9):2427. PMID: 37173894
Exercise attenuates hepatic lipid accumulation via VDR/AMPK-mediated autophagy activation in vitamin D-deficient mice. Cell Signal 2026 Feb:138:112260. PMID: 41290053
Poricoic acid a ameliorates high glucose-induced podocyte injury by regulating the AMPKα/FUNDC1 pathway. Mol Biol Rep 2024 Sep 21;51(1):1003. PMID: 39305364
Res Sq. 2026 Jan 28.
Research Square Preprint. 2024 Dec 22.
