Tubastatin A TFA

SKU: orb1220181

Description

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.

Images & Validation

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Key Properties

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CAS Number	1239262-52-2
MW	449.4
Purity	>98% (HPLC)
Formula	C₂₂H₂₂F₃N₃O₄
SMILES	CN1CCC2=C(C1)C3=CC=CC=C3N2CC4=CC=C(C=C4)C(=O)NO.C(=O)(C(F)(F)F)O
Solubility	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).

Bioactivity

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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.

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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

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Tubastatin A TFA (orb1220181)

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CAS Number:	1239262-52-2
MW:	449.42
Formula:	C₂₂H₂₂F₃N₃O₄

Purity:	98.23%
CAS Number:	1239034-70-8
MW:	334.41
Formula:	C₂₁H₂₂N₂O₂

Tubastatin A TFA

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

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