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Formula | C20H21N3O2 |
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Molecular Weight | 335.4 | CAS No. | 1252003-15-8 | |
Solubility (25°C)* | In vitro | DMSO | 5 mg/mL (14.9 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.) |
Description | Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay. It is selective against all the other isozymes (1000-fold) except HDAC8 (57-fold). Tubastatin A promotes autophagy and increases apoptosis. | ||
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In vitro | Tubastatin A is selective at all isozymes except HDAC8 and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. Tubastatin A preferentially induces α-tubulin hyperacetylation at 2.5 μM. Slight induction of histone hyperacetylation is seen for Tubastatin A at 10 μM. Tubastatin A displays dose-dependent protection against homocysteic acid-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM. [1] Tubastatin A (10 μM) induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines (18-fold); and the restoration of primary cilia correlated with downregulated Hedgehog (Hh) and MAPK signaling pathways, as well as decreased cell proliferation rates (in average by 50%) and invasion (by 40%). [2] Tubastatin A shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with an IC50 of 272 nM and 712 nM. Tubastatin A inhibits nitric oxide (NO) secretion in murine Raw 264.7 macrophages dose depenndently with an IC50 of 4.2 μM. [3] | ||
In vivo | Tubastatin A reduces the growth of cholangiocarcinoma in vivo. Tubastatin A (10 mg/kg) induces a 6-fold lower mean tumor weights in syngeneic rat orthotopic model of cholangiocarcinoma, and reduction of the ratios of tumor weight to liver weight and body weight (5- and 5.6-fold, respectively), as well as a greater frequency of ciliated cholangiocytes compared with controls (29% vs 1.4%). Tubastatin A significantly decreases the amount of PCNA-positive cells in the treated tumors compared with vehicle controls (34% vs 65%). [2] Tubastat A shows significant inhibition of paw volume at 30 mg/kg i.p. in a Freund's complete adjuvant (FCA) induced animal model of inflammation. Tubastat A (30 mg/kg i.p.) significant attenuates clinical scores (~ 70%), and IL-6 expression in paw tissues of collagen induced arthritis DBA1 mouse. [3] |
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Data from [Data independently produced by Nat Commun, 2014, 5, 3479]
Data from [Data independently produced by Int J Cancer, 2014, 134(11):2560-71]
Data from [J Biol Chem, 2013, 288(20), 14400-7]
Data from [J Biol Chem, 2013, 288(20), 14400-7]
Integrated drug response prediction models pinpoint repurposed drugs with effectiveness against rhabdomyosarcoma [ PLoS One, 2024, 19(1):e0295629] | PubMed: 38277404 |
HDAC Inhibition Induces CD26 Expression on Multiple Myeloma Cells via the c-Myc/Sp1-mediated Promoter Activation [ Cancer Res Commun, 2024, 4(2):349-364] | PubMed: 38284882 |
α-Tubulin detyrosination links the suppression of MCAK activity with taxol cytotoxicity [ J Cell Biol, 2023, 222(2)e202205092] | PubMed: 36459065 |
Selectivity of Hydroxamate- and Difluoromethyloxadiazole-Based Inhibitors of Histone Deacetylase 6 In Vitro and in Cells [ Int J Mol Sci, 2023, 24(5)4720] | PubMed: 36902164 |
Shortening of primary cilia length is associated with urine concentration in the kidneys [ Kidney Res Clin Pract, 2023, 42(3):312-324] | PubMed: 37313611 |
Protective effect of HDACIs in improves survival and organ injury after CLP-induced sepsis [ Surg Open Sci, 2023, 12:35-42] | PubMed: 36936452 |
Protective effects of histone deacetylase 6 specific inhibitor tubastatin A on subarachnoid hemorrhage in rats and the underlying mechanisms [ Zhong Nan Da Xue Xue Bao Yi Xue Ban, 2023, 48(2):172-181] | PubMed: 36999463 |
Reprogramming Short-Chain Fatty Acid Metabolism Mitigates Tissue Damage for Streptococcus pyogenes Necrotizing Skin Infection [ Res Sq, 2023, rs.3.rs-3689163] | PubMed: 38196634 |
Corroborating evidence for aberrant expression of histone deacetylase 8 in endometriosis [ Reprod Med Biol, 2023, 22(1):e12527] | PubMed: 37476367 |
Corroborating evidence for aberrant expression of histone deacetylase 8 in endometriosis [ Reprod Med Biol, 2023, 10.1002/rmb2.12527] | PubMed: 37476367 |
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