2978763-95-8
Chemical Structure
HD-TAC7
- CAS No.: 2978763-95-8
- Formula:C33H32FN7O7
- Molecular Weight:657.65
IUPAC Name: 4,4,5,5-tetramethyl-2-(6-methylbenzo[d][1,3]dioxol-5-yl)-1,3,2-dioxaborolane
InChIKey: AMBNMDIPGZXRRW-UHFFFAOYSA-N
SMILES: NC1=CC(F)=CC=C1NC(C2=CC=C(C=C2)NC(CCCCNC(CNC3=C4C(N(C(C4=CC=C3)=O)C5CCC(NC5=O)=O)=O)=O)=O)=O
Biological Activity: HD-TAC7 is a selective HDAC3 PROTAC degrader with an IC50 of 1.1 μM. By recruiting the CRBN E3 ligase, HD-TAC7 induces ubiquitin-proteasome degradation and selective downregulation of HDAC3, which in turn increases H3K27 acetylation levels and downregulates the NF-κB subunit p65, exerting anti-inflammatory activity. HD-TAC7 is used in research on COVID-19, SARS-CoV-2 infection, asthma, chronic obstructive pulmonary disease, and colon cancer[1][2][3][4].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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HD-TAC7 | 98.53% | HD-TAC7 is a selective HDAC3 PROTAC degrader with an IC50 of 1.1 μM. By recruiting the CRBN E3 ligase, HD-TAC7 induces ubiquitin-proteasome degradation and selective downregulation of HDAC3, which in turn increases H3K27 acetylation levels and downregulates the NF-κB subunit p65, exerting anti-inflammatory activity. HD-TAC7 is used in research on COVID-19, SARS-CoV-2 infection, asthma, chronic obstructive pulmonary disease, and colon cancer. | ||||||||||||||||||||
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References
- [1]. Cao F, et al. Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC). European journal of medicinal chemistry. 2020 Dec 15;208:112800. [Content Brief]
- [2]. Fangyuan Cao, et al. Induced protein degradation of histone deacetylases 3 (HDAC3) by proteolysis targeting chimera (PROTAC), European Journal of Medicinal Chemistry, Volume 208, 2020, 112800, ISSN 0223-5234
- [3]. Zahid S, et al. Structural-based design of HD-TAC7 PROteolysis TArgeting chimeras (PROTACs) candidate transformations to abrogate SARS-CoV-2 infection. J Biomol Struct Dyn. 2023;41(23):14566-14581.
- [4]. Pichlak M, et al. Targeting reversible post-translational modifications with PROTACs: a focus on enzymes modifying protein lysine and arginine residues. J Enzyme Inhib Med Chem. 2023 Dec;38(1):2254012.
