WIN-55,212-2

WIN-55,212-2 is a potent, synthetic aminoalkylindole derivative that acts as a non-selective agonist at both cannabinoid CB1 and CB2 receptors. While primarily utilized as a high-affinity pharmacological tool in cannabinoid research, it has demonstrated significant antineoplastic potential in preclinical models of hematological malignancies, such as acute myeloid leukemia (AML) and multiple myeloma. Its mechanism of action in these contexts involves the overactivation of Poly (ADP-ribose) polymerase 1 (PARP1), leading to the parylation of key glycolytic enzymes like GAPDH and pyruvate kinase. This metabolic disruption results in NAD+ depletion and the induction of parthanatos, a form of programmed cell death characterized by the nuclear translocation of apoptosis-inducing factor (AIF). Preclinical studies suggest that WIN-55,212-2 selectively targets leukemic cells while sparing normal hematopoietic stem cells.

Other names

(R)-(+)-[2,3-Dihydro-5-methyl-3-(4-morpholinylmethyl)pyrrolo[1,2,3-de]-1,4-benzoxazin-6-yl]-1-naphthalenylmethanone mesylate