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Tubastatin A
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Tubastatin A
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简单介绍
Formula:C20H21N3O2.HClMW:371.86Appearance:Off-WhiteSolidPurity:98%byHPLC
Tubastatin A
的详细介绍
Cell-permeable. A potent and selective HDAC6 (histone deacetylase 6) inhibitor. Displays 1093-fold selectivity over HDAC1 (ICvalues of 15 nM for HDAC6 vs 16.4 M 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 M with near complete protection at 10 M.
Additional Information
Synonyms
n-Hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]-indol-5(2H)-yl)methyl)benzamide
Product #
T-2472
Chemical Name
n-Hydroxy-4-((2-methyl-3,4-dihydro-1H-pyrido[4,3-b]-indol-5(2H)-yl)methyl)benzamide
Formula
C
20
H
21
N
3
O
2
.HCl
MW
371.86
Appearance
Off-White Solid
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).
Storage Temp
-20°C
Therapeutic Area
Inflammatory Diseases
Use
Tubastatin A, a selective histone deacetylase 6 inhibitor shows anti-inflammatory and anti-rheumatic effects
Additional Information
MDL Number
MFCD18071463
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
SMILES
CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.Cl
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