现货,AR-42 (HDAC-42),selleck,美国进口,HDAC 抑制剂

AR-42 is a novel HDAC inhibitor with an IC50 of 0.61 μM for acute lymphoblastic leukemia (697) cell lines.
In chronic lymphocytic leukemia (CLL) cells, the 48-hr LC50 of AR-42  is 0.76 μM. AR-42 produces dose- and time-dependent acetylation both of histones and tubulin, and induces caspase-dependent apoptosis that is not reduced in the presence of stromal cells. AR-42  significantly reduced leukocyte counts and/or prolonged survival in three separate mouse models of B-cell malignancy without evidence of toxicity. AR-42 has in vitro and in vivo efficacy at tolerable doses. In additon, AR-42 promoted hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21. Down-regulation of Kit occurred after AR-42  treatment via inhibition of Kit transcription. ^[1][2]

• The novel deacetylase inhibitor AR-42 demonstrates pre-clinical activity in B-cell malignancies in vitro and in vivo. Lucas DM et al. PLoS One. 2010 Jun 3;5(6):e10941.
• AR-42, a novel HDAC inhibitor, exhibits biologic activity against malignant mast cell lines via down-regulation of constitutively activated Kit. Lin TY et al. Blood. 2010 May 27;115(21):4217-25.

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