Description
InformationiHAP1 iHAP1 is an activator of protein phosphatase 2A (PP2A) enzymes that activates PP2A-B56ε and potently kills malignant cells.TargetsPP2AIn vitroPhenothiazine analog iHAP1 activates PP2A-B56ε and potently kills malignant cells. iHAP1 does not inhibit dopamine signaling or cause prohibitive neurologic toxicity. The PP2A complex activated by iHAP1 dephosphorylates the MYBL2 transcription factor on Ser241, causing irreversible arrest of leukemia and other cancer cells in prometaphase.In vivoIn preclinical testing against T-ALL xenografts, iHAP1 emerges as a much more promising compound than PPZ, showing improved antitumor activity and lack of toxicity.Cell Research(from reference)Cell lines：HEK293T cells Concentrations：0.5 µM Incubation Time：3 h