Panobinostat (LBH589)

Catalog No.S1030 Batch:S103011

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Technical Data

Formula

C21H23N3O2
Molecular Weight 349.43 CAS No. 404950-80-7
Solubility (25°C)* In vitro DMSO 70 mg/mL (200.32 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

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Biological Activity

Description Panobinostat (LBH589, NVP-LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Panobinostat (LBH589) induces autophagy and apoptosis. Panobinostat effectively disrupts HIV latency in vivo. Phase 3.
Targets
HDAC (MOLT-4 cells) [1] HDAC (Reh cells) [1]
5 nM 20 nM
In vitro LBH589 induces apoptosis among MOLT-4 and Reh cells in a time- and dose-dependent manner. Moreover, LBH589 is more potent in MOLT-4 than in Reh cells. LBH589 markedly prevents the growth of both MOLT-4 and Reh cells in a dose-dependent manner at 48 hours. 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. LBH589 is associated with induction of histone H3K9 and histone H4K8 acetylation as well as decreasing levels of c-Myc expression in a dose-dependent manner. LBH589 treatment also increases the levels of p21 expression. LBH589 treatment also decreases the levels of c-Myc after an initial increase at the lowest dose (10 nM) in Reh cells. In addition, LBH589 gives rise to substantial increases in mRNA levels of proapoptosis and DNA repair genes. LBH589 induces increased levels of acetylated histone H3 and H4 at the GADD45G promoter. [1] Besides, LBH589 inhibits growth of non small cell lung cancer cell lines (such as human H1299, L55 and A549 with IC50 of 5 nM, 11 nM and 30 nM, respectively), mesothelioma (such as human OK-6 and Ok-5 with IC50 of 5 nM and 7 nM, respectively) and small cell lung cancer cell lines (such as human RG-1 and LD-T with IC50 of 4 nM and 5 nM, respectively). [2]
In vivo In lung cancer and mesothelioma animal models, LBH589 markedly decreases tumor growth by 62%. LBH589 is equally effective in immunocompetent and severe combined immunodeficien-cymice, suggesting that the inhibition of tumor growth by LBH589 is not due to direct immunologic effects. Daily LBH589, given i.p. at 20 mg/kg for 5 days per week, leading to an average decrease in growth of 70%. Compared with the corresponding control tumors, LBH589 leads to a 53% decrease for H526-derived tumors, an 81% decrease for BK-T-derived tumors, a 76% decrease for RG-1- derived tumors, and a 70% decrease for H69-derived tumors. In contrast to the lack of tumor regression notes in NSCLC and Meso-derived xenografted tumors that are treated under identical conditions and doses, LBH589 results in dramatic tumor regression in SCLC-derived tumors and RG-1-derived tumor. [2]

Protocol (from reference)

Cell Assay:[1]
  • Cell lines

    MOLT-4 cell lines and Reh (pre-B cells)

  • Concentrations

    50 nM

  • Incubation Time

    48 hours

  • Method

    Untreated and LBH589-treated cells [human Ph- acute lymphoblastic leukemia MOLT-4 (T cells) and Reh (pre-B cells)] are stained with annexin V and propidium iodide using annexin V-FITC apoptosis detection kit I. The percentage of apoptotic and nonviable cells is determined by flow cytometry. At least 5 × 104 cells are collected with a CyAn ADP Violet cytometer. Percentage apoptosis is calculated considering all the annexin V-positive plus the annexin V/PI-positive cells; percentage loss of cell viability is calculated considering all the annexin V-positive plus the PI-positive and the annexinV/PI-positive cells.
Animal Study:[2]
  • Animal Models

    Severe combined immunodeficiency (SCID) mice with M30 (107 cells) or A549 (5 × 106 cells), H69 (2.5 × 106 cells), BK-T (6.5 × 106), H526 (10 × 106), and RG1 (10 × 106) cells

  • Dosages

    10 mg/kg, 20 mg/kg

  • Administration

    Administered via i.p. injection

Customer Product Validation

Data from [Breast Cancer Res Treat , 2012, 131, 777-789]

Data from [PLoS One, 2011, 6, e20920]

Data from [PLoS One, 2011, 6, e20920]

Data from [PLoS One, 2011, 6, e17138]

Selleck's Panobinostat (LBH589) has been cited by 435 publications

Acetylation-dependent regulation of core spliceosome modulates hepatocellular carcinoma cassette exons and sensitivity to PARP inhibitors [ Nat Commun, 2024, 15(1):5209] PubMed: 38890388
HDAC activity is dispensable for repression of cell-cycle genes by DREAM and E2F:RB complexes [ Nat Commun, 2024, 15(1):4450] PubMed: 38789411
Effective and targeted latency reversal in CD4+ T cells from individuals on long term combined antiretroviral therapy initiated during chronic HIV-1 infection [ Emerg Microbes Infect, 2024, 13(1):2327371] PubMed: 38444369
Chronic hypoxia stabilizes 3βHSD1 via autophagy suppression [ Cell Rep, 2024, 43(1):113575] PubMed: 38181788
Laminin-associated integrins mediate Diffuse Intrinsic Pontine Glioma infiltration and therapy response within a neural assembloid model [ Acta Neuropathol Commun, 2024, 12(1):71] PubMed: 38706008
Synergistic integration of histone deacetylase inhibitors apparently enhances the cytokine-induced killer cell efficiency in multiple myeloma via the NKG2D pathway [ Clin Transl Immunology, 2024, 13(3):e1500] PubMed: 38529413
Anti-tumour activity of Panobinostat in oesophageal adenocarcinoma and squamous cell carcinoma cell lines [ Clin Epigenetics, 2024, 16(1):102] PubMed: 39097736
Synergistic Cytotoxicity of Histone Deacetylase and Poly-ADP Ribose Polymerase Inhibitors and Decitabine in Breast and Ovarian Cancer Cells: Implications for Novel Therapeutic Combinations [ Int J Mol Sci, 2024, 25(17)9241] PubMed: 39273190
EphA2- and HDAC-Targeted Combination Therapy in Endometrial Cancer [ Int J Mol Sci, 2024, 25(2)1278] PubMed: 38279277
In-Cell Testing of Zinc-Dependent Histone Deacetylase Inhibitors in the Presence of Class-Selective Fluorogenic Substrates: Potential and Limitations of the Method [ Biomedicines, 2024, 12(6)1203] PubMed: 38927410

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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