目錄:MedChemExpress LLC>>生化試劑>> Tubastatin A | MCE
CAS | 1252003-15-8 | 純度 | 98.37% |
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分子量 | 335.4 | 分子式 | C??H??N?O? |
供貨周期 | 現(xiàn)貨 | 規(guī)格 | 5 mg |
貨號 | HY-13271A | 應(yīng)用領(lǐng)域 | 醫(yī)療衛(wèi)生,化工,生物產(chǎn)業(yè),制藥 |
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CAS No. : 1252003-15-8
產(chǎn)品活性: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).
研究領(lǐng)域:Cell Cycle/DNA Damage | Epigenetics | Autophagy | Apoptosis
作用靶點:HDAC | Autophagy | Apoptosis
In Vitro: Tubastatin A is substantially selective for all 11 HDAC isoforms and maintains over 1000-fold selectivity against all isoforms excluding HDAC8, where it has approximately 57-fold selectivity. In homocysteic acid (HCA) induced neurodegeneration assays, Tubastatin A displays dose-dependent protection against HCA-induced neuronal cell death starting at 5 μM with near complete protection at 10 μM.?At 100 ng/mL Tubastatin A increases Foxp3+ T-regulatory cells (Tregs) suppression of T cell proliferation in vitro.?Tubastatin A treatment in CC12 cells would lead to myotube formation impairment when alpha-tubulin is hyperacetylated early in the myogenic process; however, myotube elongation occurs when alpha-tubulin is hyeperacetylated in myotubes.?A recent study indicates that Tubastatin A treatment increases cell elasticity as revealed by atomic force microscopy (AFM) tests without exerting drastic changes to the actin microfilament or microtubule networks in mouse ovarian cancer cell lines, MOSE-E and MOSE-L.
In Vivo: Daily treatment of Tubastatin A at 0.5 mg/kg inhibits HDAC6 to promote Tregs suppressive activity in mouse models of inflammation and autoimmunity, including multiple forms of experimental colitis and fully major histocompatibility complex (MHC)-incompatible cardiac allograft rejection.
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