Chemical Structure : HDAC3 PROTAC P7
CAS No.:
HDAC3 PROTAC P7
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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832.12
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Formula
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C45H65N7O6S
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Chunlong Zhao, et al. Angew Chem Int Ed Engl. 2023 Aug 28;e202310059.
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