Product Description: Tubastatin A is a potent and selective HDAC6 inhibitor with an IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more). Tubastatin A also inhibits HDAC10 and metallo-β-lactamase domain-containing protein 2 (MBLAC2).
Applications: Cancer-programmed cell death
Formula: C20H21N3O2
Citations: Acta Pharm Sin B. 20 May 2022./Aging. 2021 Mar 19;13(7):9820-9837./Am J Pathol. 2020 Dec;190(12):2376-2386./Antioxidants (Basel). 2022 Apr 7;11(4):732./Antioxidants. 2020 Jul 9;9(7):599./Biochim Biophys Acta Mol Cell Res. 2020 May;1867(5):118676./bioRxiv. 2021 Feb 25./BMC Biol. 2018 Oct 18;16(1):116./J Dermatol Sci. 2022 May 17;S0923-1811(22)00125-6./J Med Chem. 2023 Nov 16./J Mol Neurosci. 2024 Mar 13./J Nutr. 2020 Jul 1;150(7):1790-1798./Medical Science, University of Toronto. 2017 Nov./Mol Cancer Res. 2014 May;12(5):681-93./Mol Cancer Res. 2022 Mar 4;molcanres.0923.2021./Neurotherapeutics. 2023 Jun 2./NPJ Precis Oncol. 2024 Mar 7;8(1):66./Patent. US20180263995A1./Atherosclerosis. 2021 Jan;317:1-9./Cell Death Dis. 2022 Oct 21;13(10):888./Front Pharmacol. 2018 Feb 1;9:34./Hum Mol Genet. 2022 Jan 12;ddac008./Neurotherapeutics. 2023 Jun 2./PLoS Pathog. 2021 Sep 20;17(9):e1009940.
References: [1]Lechner S, Malgapo MIP, Grätz C, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target [published online ahead of print, 2022 Apr 28]. Nat Chem Biol. 2022;10.1038/s41589-022-01015-5. /[2]Géraldy M, Morgen M, Sehr P, et al. Selective Inhibition of Histone Deacetylase 10: Hydrogen Bonding to the Gatekeeper Residue is Implicated. J Med Chem. 2019;62(9):4426-4443./[3]Severin Lechner, et al. Target deconvolution of HDAC pharmacopoeia reveals MBLAC2 as common off-target. Nat Chem Biol. 2022 Apr 28./[4]Ketene AN, et al. Actin filaments play a primary role for structural integrity and viscoelastic response in cells. Integr Biol (Camb). 2012 May;4(5):540-9./[5]Kyle V. Butler et al. Rational Design and Simple Chemistry Yield a Superior, Neuroprotective HDAC6 Inhibitor, Tubastatin A J. Am. Chem. Soc., 2010, 132 (31), pp 10842-10846/[6]Kozyreva VK, et al. NEDD9 regulates actin dynamics through cortactin deacetylation in an AURKA/HDAC6-dependent manner. Mol Cancer Res. 2014 May;12(5):681-93./[7]de Zoeten EF, et al. Histone deacetylase 6 and heat shock protein 90 control the functions of Foxp3(+) T-regulatory cells. Mol Cell Biol. 2011 May;31(10):2066-78./[8]Di Fulvio S, et al. Dysferlin interacts with histone deacetylase 6 and increases alpha-tubulin acetylation. PLoS One. 2011;6(12):e28563/[9]Brijmohan, Angela, et al. Role of HDAC6 in Transcription Factor EB Mediated Clearance of Misfolded Proteins in Chronic Kidney Disease. University of Toronto.Nov-2017.
CAS Number: 1252003-15-8
Molecular Weight: 335.40
Compound Purity: 98.37
Research Area: Cancer
Solubility: DMSO : 12.5 mg/mL (ultrasonic)/H2O : < 0.1 mg/mL
Target: Apoptosis;Autophagy;Beta-lactamase;HDAC
English
Deutsch
