2-Cl-IB-MECA

2-Cl-IB-MECA is an adenosine A₃ receptor agonist.¹ It binds selectively to adenosine A₃ receptors (K_i = 0.33 nM) over A₁ and A_2A receptors (K_is = 820 and 470 nM, respectively) and inhibits adenylate cyclase activity with an IC₅₀ value of 66.8 nM in CHO cell membranes expressing rat A₃ receptors. 2-Cl-IB-MECA (10 and 100 nM) inhibits proliferation of B16/F10 melanoma cells and increases proliferation of murine bone marrow cells in vitro, effects that can be blocked by the A₃ receptor antagonist MRS1523 (Item No. 17128).² It induces accumulation of cells in the G₀/G₁ phase of the cell cycle and induces apoptosis when used at a concentration of 100 nM. 2-Cl-IB-MECA (6 µg/mg) prevents the development of lung metastatic foci in a B16/F10 mouse model of lung metastasis and reverses decreases in the number of white blood cells and neutrophils induced by cyclophosphamide (Item No. 13849).

WARNING This product is not for human or veterinary use.

1. Kim, H.O., Ji, X.d., Siddiqi, S.M., et al. 2-Substitution of N6-benzyladenosine-5'-uronamides enhances selectivity for A₃ adenosine receptors. J. Med. Chem. 37(21), 3614-3621 (1994).

2. Fishman, P., Bar-Yehuda, S., Barer, F., et al. The A₃ adenosine receptor as a new target for cancer therapy and chemoprotection. Exp. Cell Res. 269(2), 230-236 (2001).