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TMCB

Names

[ CAS No. ]:
1085822-09-8

[ Name ]:
TMCB

Biological Activity

[Description]:

CK2/ERK8-IN-1 is a dual casein kinase 2 (CK2) (Ki of 0.25 µM) and ERK8 inhibitor with IC50s of 0.50 μM. CK2/ERK8-IN-1 also binds to PIM1, HIPK2 (homeodomain-interacting protein kinase 2), and DYRK1A with Kis of 8.65 µM, 15.25 µM, and 11.9 µM, respectively. CK2/ERK8-IN-1 has pro-apoptotic efficacy[1].

[Related Catalog]:

Signaling Pathways >> Apoptosis >> Apoptosis
Research Areas >> Cancer
Signaling Pathways >> JAK/STAT Signaling >> Pim
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> DYRK
Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase
Signaling Pathways >> MAPK/ERK Pathway >> ERK
Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase
Signaling Pathways >> Stem Cell/Wnt >> ERK

[Target]

CK2:0.5 μM (IC50)

CK2:0.25 μM (Ki)

ERK8:0.5 μM (IC50)

PIM1:8.65 μM (Ki)

HIPK2:15.25 μM (Ki)

DYRK1A:11.9 μM (Ki)

Apoptosis


[In Vitro]

CK2/ERK8-IN-1 (Compound K66; 0-50 µM; 24 hours; Jurkat cells) treatment displays cytotoxic activity in Jurkat cells[1]. Cell Viability Assay[1] Cell Line: Jurkat cells Concentration: 0-50 µM Incubation Time: 24 hours Result: Inhibited cell growth in a dose-dependent manner.

[References]

[1]. Pagano MA, et al. The selectivity of inhibitors of protein kinase CK2: an update. Biochem J. 2008 Nov 1;415(3):353-65.

Chemical & Physical Properties

[ Molecular Formula ]:
C11H9Br4N3O2

[ Molecular Weight ]:
534.82

Related Compounds