GSK621

• CAT Number: I007117
• CAS Number: 1346607-05-3
• Molecular Formula: C26H20ClN3O5
• Molecular Weight: 489.91
• Purity: ≥95%
• Synonyms: GSK621; GSK-621; GSK 621.;6-chloro-5-(2/’-hydroxy-3/’-methoxy-[1,1/’-biphenyl]-4-yl)-3-(3-methoxyphenyl)-1,5-dihydro-2H-pyrrolo[3,2-d]pyrimidine-2,4(3H)-dione
• Target: AMPK
• Solubility: Soluble in DMSO, not in water
• Storage: 2-8°C
• IUPAC Name: 6-chloro-5-[4-(2-hydroxy-3-methoxyphenyl)phenyl]-3-(3-methoxyphenyl)-1H-pyrrolo[3,2-d]pyrimidine-2,4-dione
• InChI: InChI=1S/C26H20ClN3O5/c1-34-18-6-3-5-17(13-18)30-25(32)23-20(28-26(30)33)14-22(27)29(23)16-11-9-15(10-12-16)19-7-4-8-21(35-2)24(19)31/h3-14,31H,1-2H3,(H,28,33)
• InChIKey: KURYSXLJGKKDHT-UHFFFAOYSA-N
• SMILES: COC1=CC=CC(=C1)N2C(=O)C3=C(C=C(N3C4=CC=C(C=C4)C5=C(C(=CC=C5)OC)O)Cl)NC2=O

GSK621（Cat No.:I007117） is a potent and selective agonist of AMP-activated protein kinase (AMPK). It displays an IC50 range of 13-30 μM in acute myeloid leukemia (AML) cell lines. GSK621 has been shown to induce both autophagy and apoptosis, cellular processes involved in maintaining cellular homeostasis and programmed cell death. Additionally, GSK621 activates the unfolded protein response (UPR) pathway by inducing phosphorylation of eIF2α, a key marker of UPR activation.

Reference

1:Targeted activation of AMPK by GSK621 ameliorates H2O2-induced damages in osteoblasts. Liu W, Mao L, Ji F, Chen F, Hao Y, Liu G.Oncotarget. 2017 Feb 7;8(6):10543-10552. doi: 10.18632/oncotarget.14454. PMID: 28060740 Free PMC Article2:GSK621 activates AMPK signaling to inhibit LPS-induced TNFα production. Wu YH, Li Q, Li P, Liu B.Biochem Biophys Res Commun. 2016 Nov 18;480(3):289-295. doi: 10.1016/j.bbrc.2016.10.001. Epub 2016 Oct 3. PMID: 27712936 3:AMPK activation by GSK621 inhibits human melanoma cells in vitro and in vivo. Chen L, Chen Q, Deng G, Kuang S, Lian J, Wang M, Zhu H.Biochem Biophys Res Commun. 2016 Nov 25;480(4):515-521. doi: 10.1016/j.bbrc.2016.10.040. Epub 2016 Oct 15. PMID: 27751856 4:GSK621 Targets Glioma Cells via Activating AMP-Activated Protein Kinase Signalings. Jiang H, Liu W, Zhan SK, Pan YX, Bian LG, Sun B, Sun QF, Pan SJ.PLoS One. 2016 Aug 17;11(8):e0161017. doi: 10.1371/journal.pone.0161017. eCollection 2016. PMID: 27532105 Free PMC Article