Valproic acid

Valproic acid (VPA) is an orally active HDAC inhibitor, with IC50 in the range of 0.5 and 2 mM. Valproic acid inhibits HDAC1 (IC50, 400 μM), and induces proteasomal degradation of HDAC2. Valproic acid activates Notch1 signaling and inhibits proliferation in small cell lung cancer (SCLC) cells. Valproic acid is used in the epilepsy, bipolar disorder, metabolic disease, HIV infection and prevention of migraine headaches[1][2][3][4][5][6][7].

[1]Han BR, et al. Valproic acid inhibits the growth of HeLa cervical cancer cells via caspase-dependent apoptosis. Oncol Rep. 2013 Dec;30(6):2999-3005.|[2]Zhang ZH, et al. Valproic acid inhibits tumor angiogenesis in mice transplanted with Kasumi 1 leukemia cells. Mol Med Rep. 2013 Nov 28.|[3]Cohen OS, et al. Acute prenatal exposure to a moderate dose of valproic acid increases social behavior and alters gene expression in rats. Int J Dev Neurosci. 2013 Dec;31(8):740-50.|[4]Avery LB, et al. Valproic Acid Is a Novel Activator of AMP-Activated Protein Kinase and Decreases Liver Mass, Hepatic Fat Accumulation, and Serum Glucose in Obese Mice. Mol Pharmacol. 2014 Jan;85(1):1-10.|[5]Valproic acid, et al. Histone deacetylase is a direct target of valproic acid, a potent anticonvulsant, mood stabilizer, and teratogen. J Biol Chem. 2001 Sep 28;276(39):36734-41.|[6]Platta CS, et al. Valproic acid induces Notch1 signaling in small cell lung cancer cells. J Surg Res. 2008 Jul;148(1):31-7.|[7]Routy JP, et al. Valproic acid in association with highly active antiretroviral therapy for reducing systemic HIV-1 reservoirs: results from a multicentre randomized clinical study. HIV Med. 2012 May;13(5):291-6.Acta Pharmacol Sin. 2024 Jun 18.|Biochem Biophys Res Commun. 2022.|Biochim Biophys Acta Gene Regul Mech. 2020 Sep;1863(9):194597.|Biomaterials. 2018 Dec 6;193:30-46.|bioRxiv. 2023 Apr 21.|Biotechnol Bioeng. 2021 Sep 3.|Brain Science Advances. 2022 Feb.|Cell Death Differ. 2023 Jun 15.|EMBO J. 2021 Apr 28;e106771.|FEBS Open Bio.2024 May 1.|Genes. 2024 Sep 13.|Genomics. 2024 May, 116, 3, 110838.|J Agric Food Chem. 2024 Oct 23.|J Biol Chem. 2023 Jan 31;102971.|J Ethnopharmacol. 2023 Feb 17;116258.|J Ethnopharmacol. 2024 Aug 16:118697.|Lett Drug Des Discover. 2019 Nov.|Life Sci. 2023 Jul 8;121921.|Mil Med Res. 2020 Nov 1;7(1):52.|Mil Med Res. 2020 Sep 6;7(1):42. |Nat Commun. 2024 Sep 19;15(1):8221.|Oncogene. 2021 Apr;40(15):2711-2724.|Phytomedicine. 19 August 2022, 154403.|Research Square Preprint. 2022 Jan.|Research Square Preprint. 2022 Jul.|Sci Adv. 2021 Aug 11;7(33):eabf4416.|Sci Rep. 2020 Sep 16;10(1):15201.|Sci Total Environ. 2021, 147014.|Sci Total Environ. 2023 Aug 23;903:166505.|Signal Transduct Target Ther. 2024 Jan 22;9(1):24.|STAR Protoc. 16 September 2022, 101638.|Acta Pharmacol Sin. 2020 Jun 17. |Adv Sci (Weinh). 2023 Dec 12:e2305620.|BMC Cancer. 2022 Aug 8;22(1):864.|Clin Dev Immunol. 2020 Aug 4;2020:4384696.|Ecotoxicol Environ Saf. 2022 Jun 14;241:113752.|J Genet Genomics. 2023 Sep 11;S1673-8527(23)00184-4.|J Interferon Cytokine Res. 2021 Dec;41(12):439-449.|Signal Transduct Target Ther. 2024 Oct 30;9(1):294.|Toxicol Lett. 2021 Apr 24;346:47-56.|Viruses. 2024 Apr 20;16(4):643.