1. Cell Cycle/DNA Damage Epigenetics GPCR/G Protein
  2. HDAC Adenosine Receptor
  3. A2AAR/HDAC-IN-2

A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor.

For research use only. We do not sell to patients.

A2AAR/HDAC-IN-2 Chemical Structure

A2AAR/HDAC-IN-2 Chemical Structure

CAS No. : 2767560-94-9

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Description

A2AAR/HDAC-IN-2 is a potent A2AAR/HDAC dual inhibitor, with good binding affinity for A2AAR (Ki=10.3 nM) and good inhibitory activity against HDAC1 (IC50=18.5 nM). A2AAR/HDAC-IN-2 can be used in study of antitumor[1].

IC50 & Target

HDAC1

18.5 nM (IC50)

HDAC2

16.0 nM (IC50)

HDAC3

13.6 nM (IC50)

HDAC6

2.1 nM (IC50)

HDAC8

1408.9 nM (IC50)

A1AR

105.6 nM (Ki)

A2AAR

10.3 nM (Ki)

A2BAR

513.0 nM (Ki)

A3AR

>10 μM (IC50)

In Vitro

A2AAR/HDAC-IN-2 (compound 30c) (5 nM-100 µM; 72 h) shows anti-proliferative activity, with GI50s of 12.16 and 12.61 µM for CT26 and MC38 cells, respectively[1].
A2AAR/HDAC-IN-2 (0.1, 1, 5, 10 µM; 24 h) increases histone H3 and H4 acetylation in a concentration-dependent manner in MC38 cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: MC38 and CT26 cells
Concentration: 5 nM-100 µM
Incubation Time: 72 h
Result: Showed good anti-proliferative activity in cancer cell lines, with GI50s of 12.16 and 12.61 µM for CT26 and MC38 cells, respectively.

Western Blot Analysis[1]

Cell Line: MC38 cells
Concentration: 0.1, 1, 5, 10 µM
Incubation Time: 24 h
Result: Significantly increases histone H3 and H4 acetylation at 10 µM and in a concentration-dependent manner.
Molecular Weight

450.49

Formula

C23H26N6O4

CAS No.
SMILES

NC1=NC(C2=CC=CO2)=C3C=NN(C3=N1)CC4=CC=CC(OCCCCCCC(NO)=O)=C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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A2AAR/HDAC-IN-2 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
A2AAR/HDAC-IN-2
Cat. No.:
HY-143325
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