YX862 | HDAC8 degrader | Probechem Biochemicals

Chemical Structure : YX862

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YX862 (YX-862)

货号: PC-22577Not For Human Use, Lab Use Only.

YX862 is a highly potent and selective hydrazide-based HDAC8-PROTAC degrader with DC50 values of 2.6 nM in MDA-MB-231 and 1.8 nM in MCF-7 cells.

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生物&药学活性

YX862 is a highly potent and selective hydrazide-based HDAC8-PROTAC degrader with DC50 values of 2.6 nM in MDA-MB-231 and 1.8 nM in MCF-7 cells.
YX862 does not degrade HDAC1 and HDAC2, and HDAC3.
The proteasome inhibitor MG132 or the neddylation inhibitor MLN4924 blocks the degradation of HDAC8 by YX862.
Degradation of HDAC8 by YX862 triggers SMC3 hyperacetylation in MDA-MB-231 cells, without significantly triggering histone post-translational modification (PTM).
YX862 dose-dependently inhibited cell proliferation of SU-DHL-2 cells (IC50 = 0.72 μM), while PCI-34051 was less effective (IC50 > 5.0 μM).

物理化学性质&存储条件

分子量	873.22
分子式	C48H72N8O5S
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	(2S,4R)-1-((S)-2-(8-(4-(4-(2-Hexylhydrazine-1-carbonyl)phenyl)piperazin-1-yl)octanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide

参考文献

1. Yufeng Xiao, et al. J Med Chem. 2024 Jul 1. doi: 10.1021/acs.jmedchem.4c00761.

YX862 (YX-862)

生物&药学活性

物理化学性质&存储条件

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YX862 (YX-862)

生物&药学活性

物理化学性质&存储条件

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