HDAC8 PROTAC Z16 (CZH-726) | HDAC8 PROTAC | Probechem Biochemicals

Chemical Structure : HDAC8 PROTAC Z16

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HDAC8 PROTAC Z16 (CZH-726, CZH726)

货号: PC-22803Not For Human Use, Lab Use Only.

HDAC8 PROTAC Z16 (CZH-726) is a potent, selective HDAC8 PROTAC degrader with DC50 of 0.32 nM, Dmax=97% in Jurkat cells.

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生物&药学活性

HDAC8 PROTAC Z16 (CZH-726) is a potent, selective HDAC8 PROTAC degrader with DC50 of 0.32 nM, Dmax=97% in Jurkat cells.
HDAC8 PROTAC Z16 also shows low nanomolar DC50 values (0.2-3.1 nM) in HCT116, THP-1 and A549 cells.
HDAC8 PROTAC Z16 induces structural maintenance of chromosomes protein 3 (SMC3) hyperacetylation at low concentrations and histone hyperacetylation at high concentrations, which can be explained by HDAC8 degradation and off-target HDAC inhibition, respectively.
HDAC8 PROTAC Z16 potently inhibited proliferation of various cancer cell lines with IC50 of 1.7-7.7 uM for Jurkat , HCT116, THP-1 and A549 cells.
HDAC8 PROTAC Z16 does not significantly affect the intracellular levels of IKZF1, IKZF3, and GSPT1 in Jurkat cells, which are the neo-substrates of CRBN.
HDAC8 PROTAC Z16 shows no obvious degradation of HDAC1, HDAC2, HDAC3, HDAC4, HDAC6, HDAC7, and HDAC11.
HDAC8 degradation induced by Z16 proceeds via formation of a ternary complex and depends on proteasomal activity.

物理化学性质&存储条件

分子量	576.74
分子式	C32H44N6O4
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	2-(4-(4-((2,6-Dioxopiperidin-3-yl)amino)phenyl)piperidin-1-yl)-N-(4-(2-hexylhydrazine-1-carbonyl)benzyl)acetamide

参考文献

1. Zhao C, et al. J Med Chem. 2024 Aug 1. doi: 10.1021/acs.jmedchem.4c00836.

HDAC8 PROTAC Z16 (CZH-726, CZH726)

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HDAC8 PROTAC Z16 (CZH-726, CZH726)

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物理化学性质&存储条件

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