LBH589, a hydroxamate analog, is a broad-spectrum HDAC inhibitor. It has been shown to increase acetylation of core histones (H3 and H4) and nonhistone proteins (alpha-tublin, HSP90), leading to the modulation of gene expression (p21, FOXO3A, GADD45A, aromatase, etc) and protein activity involved in cell growth and survival pathways1-4. LBH589 induces apoptosis in MOLT-4 and Reh cells with IC50 between 5 to 20nM1. In lung cancer and mesothelioma animal models, LBH589 markedly decreased tumor growth by 62% when compared with the vehicle control5. The anti-tumor activity of LBH589 has also been demonstrated in many other cancer cell lines, including multiple myeloma, NSCLC and castrate-resistant prostate cancer cell lines. LBH589 is under clinical trials to evaluate its effects in conjunction with chemotherapy and/or targeted therapy in multiple cancer types.
Technical information:
Chemical Formula: | C21H23N3O2 | |
CAS #: | 404950-80-7 | |
Molecular Weight: | 349.43 | |
Purity: | >98% | |
Appearance: | White solid | |
Chemical Name: | (2E)-N-hydroxy-3-[4-({[2-(2-methyl-1H-indol-3-yl)ethyl]amino}methyl)phenyl]acrylamide | |
Solubility: | Up to 50 mM in DMSO |
Shipping Condition: The product is shipped in a glass vial at ambient temperature.
Storage: For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution at -20oC.
Reference:
1. | Scuto, A., et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100. |
2. | Chen, S. et al.The HDAC inhibitor LBH589 (panobinostat) is an inhibitory modulator of aromatase gene expression. Proc Natl Acad Sci U S A 2010 Jun 15; 107(24) :11032-7. |
3. | George, P., et al. "Combination of the histone deacetylase inhibitor LBH589 and the hsp90 inhibitor 17-AAG is highly active against human CML-BC cells and AML cells with activating mutation of FLT-3." Blood 105: 1768-1776 (2005). |
4. | Qian, D.Z., et al. "Targeting tumor angiogenesis with histone deacetylase inhibitors: the hydroxamic acid derivative LBH589." Clin. Cancer Res. 12: 634-642 (2006). |
5. | Crisanti, MC. et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31. |
Other Information:
Product Specification (pdf)
MSDS (pdf)