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首页-小分子抑制剂&激动剂-Epigenetics-HDAC-TYA-018
TYA-018

Chemical Structure : TYA-018

CAS No.: 2653254-31-8

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TYA-018 (TYA018)

货号: 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).

规格 价格 库存 数量
2 mg ￥1980 In stock
5 mg ￥3480 In stock
10 mg ￥5280 In stock
25 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 434.861
分子式 C15H13ClF2N4O3S2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(3-chlorophenyl)-N-((5-(5-(difluoromethyl)-1,3,4-oxadiazol-2-yl)thiazol-2-yl)methyl)ethanesulfonamide

参考文献

1. Jin Yang, et al. Sci Transl Med. 2022 Jul 6;14(652):eabl5654.

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