Adenosine Receptor

Inhibitory Selectivity

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Notes:
2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Catalog No. Information Product Use Citations Product Validations
S8105New

ZM241385

ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.

S8314New

5-Iodotubercidin

5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.

S8104New

SCH58261

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.

S2153

CGS 21680 HCl

CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.

S2790

Istradefylline

Istradefylline is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.

S7588

Reversine

Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.

Catalog No. Information Product Use Citations Product Validations
S8105New

ZM241385

ZM-241385 is a high affinity antagonist ligand selective for the adenosine A2A receptor.

S8314New

5-Iodotubercidin

5-Iodotubercidin is a potent adenosine kinase inhibitor with IC50 of 26 nM. It inhibits nucleoside transporter, CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2 and PKC.

S8104New

SCH58261

SCH 58261 is a potent and selective A2a adenosine receptor antagonist with Ki of 2.3 nM and 2 nM for rat A2a and bovine A2a, respectively.

Catalog No. Information Product Use Citations Product Validations
S2790

Istradefylline

Istradefylline is a selective adenosine A2A receptor (A2AR) antagonist with Ki of 2.2 nM. Phase 3.

2015, 27(3):229-45

S7588

Reversine

Reversine is a potent human A3 adenosine receptor antagonist with Ki of 0.66 μM, and a pan-aurora A/B/C kinase inhibitor with IC50 of 12 nM/13 nM/20 nM, respectively. Also used for stem cell dedifferentiation.

2015, 522(7557):492-6

2013, 80(7):522-34

Catalog No. Information Product Use Citations Product Validations
S2153

CGS 21680 HCl

CGS 21680 HCl is an adenosine A2 receptor agonist with IC50 of 22 nM, exhibits 140-fold over A1 receptor.

2016, 289(1):109-16