4567-tetrabromo-2-azabenzimidazole

TBB is one of the most selective protein kinase inhibitors known and when tested against a panel of 33 serinethreonine and tyrosine protein kinases only three exhibited moderate inhibition by TBB with Ki values one to two orders of magnitude higher than that for CK2.

For R&D use onlynot for drug household or other uses.

A cell-permeable benzotriazolo compound that acts as a highly selective ATPGTP-competitive casein kinase II (CKII) inhibitor (IC50 900 nM and 1.6 M for rat liver and human recombinant CKII respectively) and DYRK (IC501 M for DYRK1a). Specificity for CKII has been reported following the screening of 33 kinases including PKA Akt PKC MKK1 ERK2 p38 JNK Lck Lyn and Syk. Also reported to inhibit NS3-associated viral helicase activity in hepatitis C virus (HCV) (IC50 20 and 60 M using DNA and RNA substrates respectively) and West Nile virus (WNV) (IC50 1.7 M and 900 nM using DNA and RNA substrates respectively).