Description
DMAT is a cell-permeable inhibitor of casein kinase 2 (CK2; IC
50 = 0.13 μM). It also inhibits Pim-1, Pim-3, HIPK2, and HIPK3 (IC
50s = 0.15, 0.097, 0.37, and 0.59 μM, respectively). DMAT blocks cell growth and induces cell death in cancer cells, both in culture and in mouse xenografts.
Uses
2-Dimethylamino-4,5,6,7-tetrabromobenzimidazole is a novel powerful and selective inhibitor of protein kinase CK2.
in vivo
DMAT application in vivo reduces tumor growth in a xenotransplant model by interference with tumor cell proliferation. Biochemical parameters and histology following DMAT administration revealed no alterations in liver tissue[4].
IC 50
CK2: 0.13 μM (IC
50, Human CK2); PIM1: 0.148 μM (IC
50); PIM2: 1.6 μM (IC
50); PIM3: 0.097 μM (IC
50); HIPK2: 0.37 μM (IC
50); HIPK3: 0.59 μM (IC
50); DYRK1a: 0.41 μM (IC
50); DYRK2: 0.35 μM (IC
50); DYRK3: 1.7 μM (IC
50); PKD1: 0.18 μM (IC
50); CDK2: 0.64 μM (IC
50)
References
[1] MARIO A PAGANO. The selectivity of inhibitors of protein kinase CK2: an update.[J]. Biochemical Journal, 2008: 353-365. DOI:
10.1042/bj20080309[2] HANNA LAWNICKA. Anti-neoplastic effect of protein kinase CK2 inhibitor, 2-dimethylamino-4,5,6,7-tetrabromobenzimidazole (DMAT), on growth and hormonal activity of human adrenocortical carcinoma cell line (H295R) in vitro.[J]. Cell and Tissue Research, 2010, 340 2: 371-379. DOI:
10.1007/s00441-010-0960-1[3] GABRIELE SASS. Inhibition of experimental HCC growth in mice by use of the kinase inhibitor DMAT.[J]. International journal of oncology, 2011, 39 2: 433-442. DOI:
10.3892/ijo.2011.1037[4] CHRISTINA WESTMOSE YDE . Induction of cell death in antiestrogen resistant human breast cancer cells by the protein kinase CK2 inhibitor DMAT[J]. Cancer letters, 2007, 256 2: Pages 229-237. DOI:
10.1016/j.canlet.2007.06.010
