Chemical Properties
Crystalline Solid
Uses
TBB is one of the most selective protein kinase inhibitors known, and when tested against a panel of 33 serine/threonine 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.
Uses
TBB is one of the most selective protein kinase inhibitors known, and when tested against a panel of 33 serine/threonine 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.
Biological Activity
A cell-permeable, selective inhibitor of casein kinase-2 (CK2) (IC 50 = 0.9 and 1.6 μ M for rat liver and human recombinant CK2 respectively). Exhibits modest discrimination between CK2 subunits, with K i values ranging from 80 nM to 210 nM. Acts in an ATP/GTP-competitive manner and displays one to two orders of magnitude selectivity over a panel of 33 protein kinases.
Biochem/physiol Actions
TBB binds to the Val66 residue of casein kinase-2 and inhibits the binding of ATP/GTP. TBB is cell permeable; it induces caspase-dependent apoptosis and degrades hematopoietic lineage cell-specific protein 1 in Jurkat cells.
