Panobinostat (LBH589)

Panobinostat (LBH589)

Catalog Number:
L002369385APE
Mfr. No.:
APE-A8178
Price:
$196
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      • Overview
        • Please contact us at for specific academic pricing.

          Background

          Panobinostat, as known as LBH589, is a novel and potent hydroxamic acid-based deacetylase inhibitor (DACis)that inhibits a broad spectrum of histone deacetylases (HDACs), including all Classes 1, 2 and 4 HDAC enzymes, at low nanomolar concentrations. According to previous studies, it not only induces apoptosis in multiple myeloma (MM) cells via caspase activation and poly(ADP-ribose) polymerase (PARP) cleavage, but also induces potent cell growth inhibition, cell-cycle arrest, and apoptosis in a time- and dose-dependent manner in both Philadelphia chromosome-negative (Ph-) actue lymphoblastic leukemia (ALL) cells lines (T-cell MOLT-4 and pre-B-cell Reh), which are correlated with induction of histone (H3K9 and H4K8) hyperacetylation, activation of p21 and p27, and suppression of c-Myc.

      • Properties
        • Alternative Name
          Panobinostat,LBH589,LBH-589, Faridak, NVP-LBH589,; (E)-N-hydroxy-3-[4-[[2-(2-methyl-1H-indol-3-yl)ethylamino]methyl]phenyl]prop-2-enamide
          CAS Number
          404950-80-7
          Molecular Formula
          C21H23N3O2
          Molecular Weight
          349.43
          Purity
          99.22%
          Solubility
          insoluble in H2O; insoluble in EtOH; ≥17.47 mg/mL in DMSO
          Storage
          Store at -20°C

          * For Research Use Only

      • Reference
        • 1. Jesus Gonzalez Bosquet, Qing Zhang, et al. "Association of a novel endometrial cancer biomarker panel with prognostic risk, platinum insensitivity, and targetable therapeutic options." PLoS One. 2021 Jan 27;16(1):e0245664. PMID:33503056
          2. Sauradip Chaudhuri, Martha Fowler, et al. "β-Cyclodextrin-Poly (β-Amino Ester) Nanoparticles Are a Generalizable Strategy for High Loading and Sustained Release of HDAC Inhibitors." ChemRxiv. Mar 27.2020
          3. Liu W, Song YY, et al. "Dysregulation of FOXO transcription factors in Epstein-Barr virus-associated gastric carcinoma." Virus Res. 2020;276:197808. PMID:31712122
          4. Martins VF, Begur M, et al. "Acute inhibition of protein deacetylases does not impact skeletal muscle insulin action." Am J Physiol Cell Physiol. 2019 Aug 28. PMID:31461343
          5. Simic D, Sang N. "Compounds targeting class II histone deacetylases do not cause panHDACI-associated impairment of megakaryocyte differentiation." Exp Hematol. 2019 Jan 4. pii: S0301-472X(19)30005-0. PMID:30611870
          6. Manna PR, Ahmed AU, et al. "Overexpression of the steroidogenic acute regulatory protein in breast cancer: Regulation by histone deacetylase inhibition." Biochem Biophys Res Commun. 2019 Feb 5;509(2):476-482. PMID:30595381
          7. Hacker KE, Bolland DE, et al. "The DEK Oncoprotein Functions in Ovarian Cancer Growth and Survival." Neoplasia. 2018 Dec;20(12):1209-1218. PMID:30412857
          8. Hari Prasad, Rajini Rao. "The Amyloid Clearance Defect in ApoE4 Astrocytes is Corrected by Epigenetic Restoration of NHE6." bioRxiv. 2018.January. 4.
          9. Lee HM, Lee E, et al. "Drug repurposing screening identifies bortezomib and panobinostat as drugs targeting cancer associated fibroblasts (CAFs) by synergistic induction of apoptosis." Invest New Drugs. 2018 Jan 18. PMID:29349597
          10. Ballante F, Reddy DR, et al. "Structural insights of SmKDAC8 inhibitors: Targeting Schistosoma epigenetics through a combined structure-based 3D QSAR, in vitro and synthesis strategy." Bioorg Med Chem. 2017 Apr 1;25(7):2105-2132. PMID:28259528
          11. Bagnall NH, Hines BM, et al."Insecticidal activities of histone deacetylase inhibitors against a dipteran parasite of sheep, Lucilia cuprina." Int J Parasitol Drugs Drug Resist. 2017 Apr;7(1):51-60. PMID:28110187
          12. Reddy DR, Ballante F, et al. "Design and synthesis of benzodiazepine analogs as isoform-selective human lysine deacetylase inhibitors." Eur J Med Chem. 2017 Feb 15;127:531-553. PMID:28109947
          13. Chatterjee N, Tian M, et al. "Keap1-Independent Regulation of Nrf2 Activity by Protein Acetylation and a BET Bromodomain Protein."PLoS Genet. 2016 May 27;12(5):e1006072. PMID:27233051
          14. Reddy DN, Ballante F, et al. "Design and Synthesis of Simplified Largazole Analogues as Isoform-Selective Human Lysine Deacetylase Inhibitors." J Med Chem. 2016 Feb 25;59(4):1613-33. PMID:26681404

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