JNJ-16241199

JNJ-16241199 is an orally active, selective hydroxamate-based histone deacetylase (HDAC) inhibitor, with the IC₅₀ of 3.3 nM and 23 nM for HDAC1 and HDAC8, respectively. JNJ-16241199 induces histone 3 acetylation and strongly increases the expression of p21^waf1, ^cip1 in A2780 ovarian carcinoma cells. JNJ-16241199 induces cell apoptosis and shows anticancer activity in a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study^[1]. In Vitro:JNJ-16241199 inhibits proliferation with comparable potency in acute lymphoblastic leukaemia (ALL), AML, chronic lymphoblastic leukaemia (CLL), chronic myeloid leukaemia (CML), lymphoma and myeloma tumour cells (IC₅₀ values = 15–486 nM) ^[1].
JNJ-16241199 inhibits the Primary human mammary epithelial cell (HMEC) proliferation with the IC₅₀ of 32 nM, and is insensitive to quiescent, non-proliferative HMEC cells (IC₅₀ = 7815 nM) ^[1].
JNJ-16241199 (0.1, 0.3, 1 μM, 24-48 h) induces apoptosis and inhibits angiogenesis in A2780 cell line^[1]. In Vivo:JNJ-16241199 (10-40 mpk/day for 28 days, p.o.) inhibits the growth of A2780 ovarian, H460 lung and HCT116 colon carcinomas orthotopic xenograft tumor models ^[1].