LBH589 (Panobinostat, NVP-LBH589) is a novel deacetylase inhibitor and has been shown to induce acetylation of histone H3 and H4, increase p21 levels, disrupt the chaperone function of hsp90, and induce cell-cycle G1 phase accumulation and apoptosis of K562 cells and acute leukemia MV4-11 cells. LBH589 (Panobinostat, NVP-LBH589) has also recently been found to significantly increase in vitro the survival of motor neuron (SMN) protein levels in cells of patients suffering from spinal muscular atrophy.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Source||PLoS One (2015). Figure 2. LBH589|
|Cell Lines||SK-NEP-1 and G401 cells|
|Incubation Time||24 h|
|Results||The result showed that among cells treated with LBH589 50nM and 100nM for 24 hours, many more cells showed apoptotic feature compared with control group, for both SK-NEP-1 and G401 cells|
ING1 and 5-Azacytidine Act Synergistically to Block Breast Cancer Cell Growth.
Thakur et al. PLoS One. 2012;7(8):e43671. PMID: 22916295.
The prostate cancer blocking potential of the histone deacetylase inhibitor LBH589 is not enhanced by the multi receptor tyrosine kinase inhibitor TKI258.
Vallo et al. Invest New Drugs. 2012 Jul 17. PMID: 22801803.
LBH589 Enhances T Cell Activation In Vivo and Accelerates Graft-versus-Host Disease in Mice.
Wang et al. Biol Blood Marrow Transplant. 2012 Aug;18(8):1182-1190. PMID: 22698484.
HDAC gene expression in pancreatic tumor cell lines following treatment with the HDAC inhibitors panobinostat (LBH589) and trichostatine (TSA).
Mehdi et al. Pancreatology. 2012 Mar;12(2):146-55. PMID: 22487525.
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