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Chemical Structure : TYA-018
CAS No.: 2653254-31-8
Catalog No.: PC-49250Not For Human Use, Lab Use Only.
TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs).
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $358 | In stock | |
| 10 mg | $558 | In stock | |
| 25 mg | $898 | In stock | |
| 50 mg | Get quote | ||
| 100 mg | Get quote |
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TYA-018 (TYA018) is a potent, isoform-selective inhibitor of HDAC6 with IC50 of 10 nM, inhibits tubulin acetylation (Ac-Tubulin) with EC50 of 120 nM in cell-based assay in induced pluripotent stem cell-derived cardiomyocytes (iPSC-CMs).
TYA-018 displays >2500-fold selectivity compared with other zinc-dependent HDACs, shows no any off-target activity of on nuclear HDACs by measuring acetylated lysine on histone H3 and H4.
TYA-018 (15 mg/kg by oral gavage) reduced Nppb expression and sarcomere damage and prevented heart failure in BAG3 cardiomyocyte-knockout (BAG3cKO) mouse model of Dilated cardiomyopathy (DCM), partially restored protein expression of FLNC, PINK1, VDAC2, and p62 to amounts similar to WT mice.
TYA-018 treatment reduces mitochondrial content, decreases apoptotic nuclei, and increases LC3 puncta in hearts of BAG3cKO mice.
TYA-018 treatment enriches targets associated with muscle contraction, protein and fatty acid metabolism, and oxidative phosphorylation in BAG3cKO mice.
| M.Wt | 434.861 | |
| Formula | C15H13ClF2N4O3S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
N-(3-chlorophenyl)-N-((5-(5-(difluoromethyl)-1,3,4-oxadiazol-2-yl)thiazol-2-yl)methyl)ethanesulfonamide |
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1. Jin Yang, et al. Sci Transl Med. 2022 Jul 6;14(652):eabl5654.
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