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HDAC8 PROTAC 1

Chemical Structure : HDAC8 PROTAC 1

CAS No.:

HDAC8 PROTAC 1 (HDAC8 PROTAC 4c)

Catalog No.: PC-73287Not For Human Use, Lab Use Only.

HDAC8 PROTAC 1 is a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8) with DC50 of 0.7 uM in T-cell leukemia Jurkat cells.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

HDAC8 PROTAC 1 is a first-in-class proteolysis targeting chimera (PROTAC) for selective degradation of histone deacetylase 8 (HDAC8) with DC50 of 0.7 uM in T-cell leukemia Jurkat cells.
HDAC8 PROTAC 1 does not influence the levels of HDAC1, HDAC2, and HDAC6.
HDAC8 PROTAC 1 strongly inhibits Jurkat cell growth with a GI50 value of 0.78 μM
HDAC8 PROTAC 1 induced degradation of HDAC8 without affecting the levels of other HDACs in cellular assays, and inhibited the growth of T-cell leukemia Jurkat cells more potently than a conventional HDAC8 inhibitor.
HDAC8 PROTAC 1 degrades HDAC8 via PROTAC-mediated UPS

Physicochemical Properties

M.Wt 794.928
Formula C41H46N8O7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(11-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)undecyl)-3-(((1-(3-(hydroxycarbamoyl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)thio)benzamide

References

1. Jiranan Chotitumnavee, et al. Chem Commun (Camb). 2022 Apr 7;58(29):4635-4638.

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