Non disponible en dehors du Royaume-Uni et de l'Irlande
Biochem/physiol Actions
iHAP1 is a potent activator of protein phosphatase 2A (PP2A) that allosterically facilitates assembly and activation of PP2A holoenzyme complex consisting PPP2R1A, PPP2R5E (B56ε, regulatory), and PPP2CA subunits. iHAP1 induces dephosphorylation of MYBL2 transcription factor on Ser241, causing irreversible cell cycle arrest of leukemia and other cancer cells in prometaphase. iHAP1 exhibits significant antitumor activity and lack of toxicity in T-ALL xenograft mice models. Normal CD34+ HSPCs are appears to be resistant to iHAP1. iHAP1 does not inhibit dopamine receptor D2.
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