IM156
AMPK activator/Mitochondrial protein complex I inhibitor / Potent activator of AMP-activated protein kinase (AMPK) showing greater activity than metformin or AICAR.1 It displayed protective effects in vivo against peritoneal1, liver2, renal3,and pulmonary fibrosis4. IM156 induces metabolic stress in Myc+ lymphoma cells by inhibiting TCA cycle metabolism and mitochondrial respiration (inhibits mitochondrial protein complex 1).4 IM156 acts as an antiproliferative in several cancer models.5-7
Biochemicals & reagents
1422365-93-2
HL156A
1) Ju et al. (2015), 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.,310 F342 2) Lee et al. (2016), AMP-activated protein kinase activator, HL156A reduces thioacetamide-induced liver fibrosis in mice and inhibits the activation of cultured hepatic stellate cells and macrophages; Int. J. Oncol., 49 1407 3) Tsogbadrakh et al. (2018), HL156A, a novel pharmacological agent with potent adenosine-monophosphate-activated protein kinase (AMPK) activator ameliorates renal fibrosis in a rat unilateral ureteral obstruction model; PLoS One, 13 e0201692 4) Izreig et al. (2020), Repression of LKB1 by mi-17`92 Sensitizes MYC-Dependent Lymphoma to Biguanidine Treatment; Cell Rep. Med., 1 100014 5) Choi et al. (2016), Inhibiting stemness and invasive properties of glioblastoma tumorsphere by combined treatment with temozolomide and a newly designed biguanidine (HL156A); Oncotarget, 7 65643 6) Jeong et al. (2020), Metformin Derivative HL156A Reverses Multidrug Resistance by Inhibiting HOXC6/ERK1/2 Signaling in Multidrug-Resistant Human Cancer Cells; Pharmaceuticals (Basel), 13 218 7) Geiger et al. (2022), First-in-human study of IM156, a novel potent biguanidine oxidative phosphorylation (OXPHOS) inhibitor, in patients with advanced solid tumors; Invest. New Drugs, online ahead of print
-20°C
TARGET: Kinase -- PATHWAY: Mitochondrial function; NAD, NADP pathways -- DISEASE AREA: Cancer; Inflammation