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Tubastatin A

Chemical Structure : Tubastatin A

CAS No.: 1252003-15-8

Tubastatin A (HDAC6 inhibitor TSA)

Catalog No.: PC-43451Not For Human Use, Lab Use Only.

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in cell-free assays.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in cell-free assays.
Tubastatin A displays 57-fold selectivity over HDAC8 and >1,000-fold selective against other HDAC isoforms.
Tubastatin A induces an increase in acetylated-α-tubulin levels and the restoration of primary cilia expression in the cholangiocarcinoma cell lines at 10 uM, shows significant inhibition of TNF-α and IL-6 in LPS stimulated human THP-1 macrophages with IC50 of 272 nM and 712 nM.
Tubastatin A reduces the growth of cholangiocarcinoma in vivo.

Physicochemical Properties

M.Wt 335.40
Formula C20H21N3O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 45 mg/mL

Chemical Name/SMILES

Benzamide, N-hydroxy-4-[(1,2,3,4-tetrahydro-2-methyl-5H-pyrido[4,3-b]indol-5-yl)methyl]-

References

1. Butler KV, et al. J Am Chem Soc. 2010 Aug 11;132(31):10842-6.

2. de Zoeten EF, et al. Mol Cell Biol. 2011 May;31(10):2066-78.

3. Gradilone SA, et al. Cancer Res. 2013 Apr 1;73(7):2259-70.

4. Vishwakarma S, et al. Int Immunopharmacol. 2013 May;16(1):72-8.

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