Tubastatin A TFA

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Tubasatin A 是一种有效的 HDAC6 抑制剂，IC50 值为 15 nM。

Potent, selective HDAC6 inhibitor (IC50 values are 4 and 900 nM for HDAC6 and HDAC8 respectively). Inhibits LPS-induced cytokine production in macrophages (IC50 values are 272 and 712 nM for TNF-α and IL-6 respectively). Induces α-tubulin hyperacetylation. Shows anti-inflammatory and peripheral neuroprotective effects in vivo.

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.

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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Others

Other Targets

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1239262-52-2

449.4

C22H22F3N3O4

>98% (HPLC)

Soluble in 1:10 DMSO:PBS(pH7.2) (~0.1 mg/mL), ethanol (~0.2 mg/mL), DMF (~5 mg/mL), and DMSO (~5 mg/mL).

CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.C(=O)(C(F)(F)F)O

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(-20℃)

With Ice Pack

≥ 2 years