GSK621

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.

Product information

CAS Number: 1346607-05-3

Molecular Weight: 489.91

Formula: C26H20ClN3O5

Chemical Name: 6-chloro-5-{2'-hydroxy-3'-methoxy-[1, 1'-biphenyl]-4-yl}-3-(3-methoxyphenyl)-1H, 2H, 3H, 4H, 5H-pyrrolo[3, 2-d]pyrimidine-2, 4-dione

Smiles: COC1=CC(=CC=C1)N1C(=O)NC2C=C(Cl)N(C=2C1=O)C1C=CC(=CC=1)C1=CC=CC(OC)=C1O

InChiKey: KURYSXLJGKKDHT-UHFFFAOYSA-N

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)

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO : 12.5 mg/mL (25.51 mM; ultrasonic and adjust pH to 1 with HCl)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥360 days if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

GSK621 (30 μM) induces AMPKα T172, ACC (S79) and ULK1 (S555) phosphorylation. GSK621 (30 μM) induces autophagy and apoptosis. GSK621 treatment also induces PERK phosphorylation, a marker of ER stress, in AML cells.

In Vivo:

GSK621 (30 mg/kg, ip twice daily) exhibits significant anti-tumor activity in MOLM-14 cells xenograft.

References:

1. Pierre Sujobert, et al. Co-activation of AMPK and mTORC1 Induces Cytotoxicity in Acute Myeloid Leukemia. Cell Rep. 2015 Jun 9;11(9):1446-57.

Products are for research use only. Not for human use.