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Product Details
| Alternate Name | n-Hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]-indol-5(2H)-yl)methyl)benzamide |
|---|---|
| Appearance | Off-white solid |
| CAS # | 1239262-52-2 |
| Molecular Formula | C₂₀H₂₁N₃O₂.HCl |
| Molecular Weight | 371.86 |
| Purity | ≥98% by HPLC |
| Solubility | DMSO (~90 mg/ml) or Water (~ 4mg/ml) or 2% TWEEN-80/water (~2 mg/ml) or 30% PEG (avg. MW = 400 g/mol)/50 mM phosphate buffer (pH = 2.25) (25 mg/ml) (heating is required to initially dissolve the compound). |
| SMILES | CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.Cl |
| InChi | InChI=1S/C20H21N3O2.ClH/c1-22-11-10-19-17(13-22)16-4-2-3-5-18(16)23(19)12-14-6-8-15(9-7-14)20(24)21-25;/h2-9,25H,10-13H2,1H3,(H,21,24);1H |
| InChi Key | LJTSJTWIMOGKRJ-UHFFFAOYSA-N |
| PubChem CID | 57336514 |
| MDL Number | MFCD18071463 |
| Handling | Protect from air and light |
| Storage Conditions | -20°C |
| Shipping Conditions | Gel Pack |
| USAGE | For Research Use Only! Not For Use in Humans. |
Details
Cell-permeable. A potent and selective HDAC6 (histone deacetylase 6) inhibitor. Displays 1093-fold selectivity over HDAC1 (IC₅₀ values of 15 nM for HDAC6 vs 16.4 µM for HDAC1). Tubastatin A was substantially more selective than the known HDAC6 inhibitor Tubacin at all isozymes except HDAC8. In addition, it displayed over 1000-fold selectivity against all HDAC isoforms excluding HDAC8, where it displayed 54-fold selectivity. Tubastatin A displayed dose-dependent protection against HCA (homocysteic acid)-induced neuronal cell death starting at 5 µM with near complete protection at 10 µM.
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Nanduri et al., Chaperone-mediated 26S Proteasome Remodeling Facilitates Free K63 Ubiquitin Chain Production and Aggresome Clearance. J. Biol. Chem., Apr 2015; 290: 9455 - 9464.
Rajasingh et al., Combinatorial Treatment with HDAC6 and DNA Methylation Modifiers in Attenuating Lung Vascular Hyperpermeability in LPS-induced Inflammatory Lung Injury. Circulation, Nov 2014; 130: A15604.
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