A2AAR/HDAC-IN-1
A2AAR/HDAC-IN-1 (compound 14c) is an orally active, potent and balanced A2AAR/HDAC dual inhibitor, with a Ki of 163.5 nM for A2AAR and an IC50 of 145.3 nM for HDAC1. A2AAR/HDAC-IN-1 shows anticancer activity[1].
Product Specifications
CAS Number
2767560-51-8
UNSPSC
12352005
Target
Adenosine Receptor; HDAC
Type
Reference compound
Related Pathways
Cell Cycle/DNA Damage; Epigenetics; GPCR/G Protein
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/a2aar-hdac-in-1.html
Solubility
10 mM in DMSO
Smiles
NC1=CC=CC=C1NC(C2=CC=C(C=C2)CCN3N=CC4=C(N=C(N=C43)N)C5=CC=CO5)=O
Molecular Formula
C24H21N7O2
Molecular Weight
439.47
References & Citations
[1]Zhang J, et al. Dual-acting antitumor agents targeting the A2A adenosine receptor and histone deacetylases: Design and synthesis of 4- (furan-2-yl) -1H-pyrazolo[3,4-d]pyrimidin-6-amine derivatives. Eur J Med Chem. 2022 Jun 5;236:114326.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Adenosine A1 receptor (A1R) ; Adenosine A2A receptor (A2AR) ; Adenosine A2B receptor (A2BR) ; Adenosine A3 receptor (A3R) ; HDAC1; HDAC2; HDAC3; HDAC6; HDAC8
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