A PROTAC that drives HDAC3 degradation
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HD-TAC7

Item No. 45613

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2-amino-4-fluorophenyl)-4-[[5-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]acetyl]-amino]-1-oxopentyl]amino]-benzamide
CAS Number
2978763-95-8
Molecular Formula
C33H32FN7O7
Formula Weight
657.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Slightly Soluble: 0.1-1 mg/mlMethanol: Slightly Soluble: 0.1-1 mg/ml
SMILES
O=C(N1)CCC(N2C(C3=C(C=CC=C3NCC(NCCCCC(NC4=CC=C(C(NC5=CC=C(F)C=C5N)=O)C=C4)=O)=O)C2=O)=O)C1=O
InChi Code
InChI=1S/C33H32FN7O7/c34-19-9-12-23(22(35)16-19)39-30(45)18-7-10-20(11-8-18)38-26(42)6-1-2-15-36-28(44)17-37-24-5-3-4-21-29(24)33(48)41(32(21)47)25-13-14-27(43)40-31(25)46/h3-5,7-12,16,25,37H,1-2,6,13-15,17,35H2,(H,36,44)(H,38,42)(H,39,45)(H,40,43,46)
InChi Key
AMBNMDIPGZXRRW-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    HD-TAC7 is a proteolysis-targeting chimera (PROTAC) composed of a class I histone deacetylase (HDAC) inhibitor linked to the cereblon ligand pomalidomide (Item No. 19877).1 It binds to HDAC1, HDAC2, and HDAC3 (IC50s = 3.6, 4.2, and 1.1 µM, respectively) and induces degradation of HDAC3 in RAW 264.7 cells with a half-maximal degradation concentration (DC50) value of 0.32 µM, without inducing degradation of HDAC1 or HDAC2. HD-TAC7 (10 µM) increases acetylation of histone H3 lysine 27 (H3K27Ac) in RAW 264.7 macrophages but reduces the levels of NF-κB p65 and does not increase the expression of IL10 in LPS- and IFN-γ-stimulated RAW 264.7 macrophages, effects attributed to the pomalidomide moiety.

    WARNING This product is not for human or veterinary use.