| Description | IM-156 acetate, an activator of NADH dehydrogenase (IC50=2.2 μM) and AMP-activated protein kinase alpha (AMPKα), is an orally available and bioavailable inhibitor of mitochondrial oxidative phosphorylation (OxPhos).IM-156 acetate increases AMPKα activity and inhibits chlorhexadiene-induced peritoneal fibrosis and inhibit tumor growth in rats . |
| In vitro | IM-156 is an inhibitor of mitochondrial complex I, also known as an activator of NADH dehydrogenase (IC50 = 2.2 µM) and AMP-activated protein kinase α (AMPKα).[1][2] |
| In vivo | It reduces the oxygen consumption rate (OCR; IC50 = 3.3 µM) and decreases mitochondrial ATP production in Eµ-Myc mouse lymphoma cells.1 IM-156 (10, 30, and 50 µM) increases AMPKα activity in primary rat peritoneal mesothelial cells and protects against chlorhexidine-induced peritoneal fibrosis in rats when administered at a dose of 1 mg/kg.2 It reduces tumor growth in an AT-84 murine oral cancer model and decreases age-related decline in novel object recognition, spatial working, and contextual memory in mice.[3][4] |
| Target activity | OCR:3.3 µM, NADH dehydrogenase:2.2 µM |
| Synonyms | HL271 acetate |
| molecular weight | 375.35 |
| Molecular formula | C15H20F3N5O3 |
| CAS | 2043654-54-0 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 1.0 mg/mL (3.2 mM) DMF: 1.0 mg/mL (3.2 mM) Ethanol: 1 mg/mL |
| References | 1. Izreig S, et al. Repression of LKB1 by miR-17∼92 Sensitizes MYC-Dependent Lymphoma to Biguanide Treatment. Cell Rep Med. 2020;1(2):100014. 2. Ju KD, et al. HL156A, a novel AMP-activated protein kinase activator, is protective against peritoneal fibrosis in an in vivo and in vitro model of peritoneal fibrosis. Am J Physiol Renal Physiol. 2016;310(5):342-350. 3. Lam TG, et al. New metformin derivative HL156A prevents oral cancer progression by inhibiting the insulin-like growth factor/AKT/mammalian target of rapamycin pathways. Cancer Sci. 2018;109(3):699-709. 4. Bang E, et al. The Improving Effect of HL271, a Chemical Derivative of Metformin, a Popular Drug for Type II Diabetes Mellitus, on Aging-induced Cognitive Decline. Exp Neurobiol. 2018;27(1):45-56. |