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Biological Activity for Panobinostat
Panobinostat is a potent pan-histone deacetylase (HDAC) inhibitor (IC50 values = 2.1 - 531 nM). Panobinostat induces histone H3 and H4 acetylation and potently inhibits cell proliferation and cell viability in HH, BT474 and HCT116 cells (IC50 are 1.8, 2.6 and 7.1 nM, respectively) in vitro. It leads to significant tumor regression of up to 94% in an HH CTCL mouse xenograft model. Panobinostat inhibits the DNA binding activity of STAT5 in leukemia cell lines and acts synergistically with 17-AAG (Cat. No. 1515) to induce apoptosis. The compound shows potent antimyeloma activity, including in drug-resistant cell lines. Panobinostat also induces a significant increase in cell-associated unspliced (CA-US) HIV-1 RNA from CD4+ T cells and leads to activation of transcription of proviruses. Panobinostat simultaneously suppresses the expression of angiotensin-converting enzyme 2 (ACE2) and ABO in epithelial cell lines. Antimalarial and orally bioavailable.
Technical Data for Panobinostat
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Panobinostat
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for Panobinostat
The following data is based on the product molecular weight 349.43. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.86 mL||14.31 mL||28.62 mL|
|5 mM||0.57 mL||2.86 mL||5.72 mL|
|10 mM||0.29 mL||1.43 mL||2.86 mL|
|50 mM||0.06 mL||0.29 mL||0.57 mL|
References for Panobinostat
References are publications that support the biological activity of the product.
Atadja (2009) Development of the pan-DAC inhibitor panobinostat (LBH589): successes and challenges. Cancer Lett. 280 233 PMID: 19344997
Maiso et al (2006) The histone deacetylase inhibitor LBH589 is a potent antimyeloma agent that overcomes drug resistance. Cancer Res. 66 5781 PMID: 16740717
George et al (2005) 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 PMID: 15514006
Barton et al (2016) Broad activation of latent HIV-1 in vivo. Nat.Commun. 7 12731 PMID: 27605062
Takahashi et al (2021) Histone deacetylase inhibitors suppress ACE2 and ABO simultaneously, suggesting a preventive potential against COVID-19. Sci.Rep. 11 3379 PMID: 33564039
If you know of a relevant reference for Panobinostat, please let us know.
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Keywords: Panobinostat, Panobinostat supplier, pan, histone, deacetylase, HDAC, inhibitor, inhibits, tumor, regression, H3, H4, acetylation, antimyeloma, cell-associated, unspliced, CA-US, HIV-1, RNA, angiotensin-converting, enzyme, 2, ACE2, ABO, COVID-19, antimalarial, malaria, Non-selective, HDACs, Antimalarials, 7629, Tocris Bioscience
Citations for Panobinostat
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics Research Bulletin
Produced by Tocris and updated in 2014, the epigenetics research bulletin gives an introduction into mechanisms of epigenetic regulation, and highlights key Tocris products for epigenetics targets including:
- DNA Methyltransferases
- Histone Deacetylases
- Histone Demethylases
- Histone Methyltransferases
Rheumatoid Arthritis Poster
Rheumatoid arthritis (RA) is a chronic destructive inflammatory autoimmune disease that results from a breakdown in immune tolerance, for reasons that are as yet unknown. This poster summarizes the pathology of RA and the inflammatory processes involved, as well as describing some of the epigenetic modifications associated with the disease and the potential for targeting these changes in the discovery of new treatments.