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TMCB

Names

[ CAS No. ]:
905105-89-7

[ Name ]:
TMCB

[Synonym ]:
k66

Biological Activity

[Description]:

TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively[1].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase
Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase

[Target]

CK2α:83 nM (Ki)

CK2α':21 nM (Ki)


[In Vitro]

The inhibition of TMCB toward the purified CK2 holoenzyme CK2α2β2 results in a Ki value of 10.1 nM. In addition, Ki values are determined with the surface displayed isoform CK2 holoenzymes and turned out to be of 31.1 nM for CK2α2β2 and 19.6 nM for CK2α'2β2. The surface display of CKα and CK2α', in the context of the corresponding holoenzymes, can be used to identify selective compounds[1].

[References]

[1]. Bollacke A, Nienberg C, Borgne ML, Jose J. Toward selective CK2alpha and CK2alpha' inhibitors: Development of a novel whole-cell kinase assay by Autodisplay of catalytic CK2alpha'. J Pharm Biomed Anal. 2016;121:253-260.

Chemical & Physical Properties

[ Molecular Formula ]:
C11H9Br4N3O2

[ Molecular Weight ]:
534.82400

[ Exact Mass ]:
530.74300

[ PSA ]:
58.36000

[ LogP ]:
4.23690


Related Compounds