HDAC3 PROTAC P7

Chemical Structure : HDAC3 PROTAC P7

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货号: PC-21118Not For Human Use, Lab Use Only.

HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%).

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生物&药学活性

HDAC3 PROTAC P7 is a potent and selective HDAC3-directed PROTAC with IC50 of 40 nM (HDAC3 deacetylase activity), effectively induces HDAC3 degradation with DC50 of 0.6 nM in THP-1 cells (Emax=90%).
HDAC3 PROTAC P7 not demonstrate a significant effect on the levels of HDAC1, HDAC2 and HDAC6, while significant effects on HDAC4 at >3.3 uM.
HDAC3 PROTAC P7 is a potent and selective HDAC3 PROTACthat can also trigger HDAC8 degradation at higher concentrations.
HDAC3 PROTAC P7 shows anti-inflammatory activityin THP-1 derivedM1-like macrophage, decreases the secretion of pro-inflammatory cytokines in M1-like macrophages derived from human primary macrophages.

物理化学性质&存储条件

分子量	832.12
分子式	C45H65N7O6S
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	N1-((R)-1-((2S,4R)-4-hydroxy-2-(((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)-carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-N12-(4-(2-propylhydrazine-1-carbonyl)phenyl)dodecanediamide

参考文献

1. Chunlong Zhao, et al. Angew Chem Int Ed Engl. 2023 Aug 28;e202310059.

HDAC3 PROTAC P7

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物理化学性质&存储条件

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HDAC3 PROTAC P7

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