Cat. No. Name Size Price Add Cart
KI0145LBH-58910 mg$144
LBH-58950 mg$432
LBH-589200 mg$1072

Chemical Characteristic

Product NameLBH-589
SynonymsPanobinostat
CAS No.404950-80-7
Molecular Weight 349.43
FormulaC21H23N3O2
Chemical Name(E)-N-hydroxy-3-(4-((2-(2-methyl-1H-indol-3-yl)ethylamino)methyl)phenyl)acrylamide
SmilesC(=O)(/C=C/c1ccc(cc1)CNCCc1c([nH]c2c1cccc2)C)NO
Chemical Structure

Biological activities

LBH589 is a novel histone deacetylase (HDAC) inhibitor with an IC50 value of 30 nM. LBH589 inhibits human ether-a-go-go-related-gene (hERG) channel with an IC50 value of 3.9 µM. LBH589 induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. The maximum effect in MOLT-4 cells is at 20 nM LBH589 with 85% apoptosis at 72 hours, and in Reh cells the maximum effect is at 50 nM LBH589 with 80% apoptosis at 72 hours. The IC50 value of LBH589 for inhibition of proliferation in MOLT-4 cells is approximately 5 nM and for Reh cells is approximately 20 nM. In both MOLT-4 and Reh cells, LBH589 treatment causes a 2- to 3-fold increase in the number of cells in the G2/M phase of the cell cycle compared with the control cells. In MOLT-4 cells, LBH589 induces the expression of histone H3K9 and histone H4K8 acetylation as well as decreasing levels of c-Myc expression in a dose-dependent manner. Low doses of LBH589 (10 nM) increases the levels of p27 and then higher doses of LBH589 (20 and 50 nM) decreases the levels of p27. In Reh cells, LBH589 also induces histone H3K9 and histone H4K8 acetylation and increases p27 expression in a dose-dependent manner. LBH589 treatment (50 nM) increases mRNA levels of proapoptosis, growth arrest, and DNA damage repair genes including FANCG, FOXO3A, GADD45A, GADD45B, and GADD45G in both MOLT-4 and Reh cells. LBH589 treatment (50 nM) increases histone H3 and H4 acetylation associated with the GADD45G promoter region from+567 to 6, which encompasses the stress-responsive sequences in the core promoter. Besides, treatment of MOLT-4 and Reh cells with LBH589 (10 nM) induces expression of GADD45γ protein. LBH589 induces H2A.X phosphorylation in a dose-dependent manner in both MOLT-4 and Reh cells. Furthermore, treatment with LBH589 is active against cultured primary Philadelphia chromosome??egative (Ph-) acute lymphoblastic leukemia (ALL) cells, inducing loss of cell viability (up to 70%) and induction of GADD45G mRNA expression (up to 35-fold).[1] In the human Meso cell line M30, the mouse Meso cell line AE17, the human NSCLC line A549 and the mouse NSCLC line TC1 tumor models, LBH589 significantly slows tumor growth when compared with vehicle control for all four different in vivo models, and by an average of almost 60%. In four human small cell lung cancer (SCLC) cell lines (H526, BKT, RG1 and H89) xenografts models, LBH589 (20 mg/kg) results in an average decrease in growth of 70% at the end of all the experiments. Compared with the corresponding control tumors, LBH589 results in a 53% decrease for H526-derived tumors, a 81% decrease for BK-T??erived tumors, a 76% decrease for RG-1??erived tumors and a 70% decrease for H69-derived tumors.[2]

Protocols

LBH589 is prepared as a 5 mM stock in DMSO and stored at -80°C. [1]

References

[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, 111(10): 5093-5100.
[2] 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, 8(8): 2221-2231.
[3] Geng L, et al. Histone Deacetylase (HDAC) Inhibitor LBH589 Increases Cytoplasm in Irradiated Non-Small Cell Lung Cancer Duration of γ-H2AX Foci and Confines HDAC4 to the Cytoplasm in Irradiated Non -Small Cell Lung Cancer. Cancer Res. 2006, 66(23): 11298-11304.

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