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TBB

CAS No. : 17374-26-4

MCE 国际站：TBB

产品活性：TBB是可渗透细胞，ATP竞争型的 CK2 抑制剂，抑制大鼠肝脏CK2的 IC₅₀ 值为0.15 μM。

研究领域：Cell Cycle/DNA Damage  |  Stem Cell/Wnt

作用靶点：Casein Kinase

In Vitro: Investigation of the inhibitory power of TBB with a panel of 33 protein kinases shows highest potency for CK2 (casein kinase 2) (human CK2: IC₅₀=1.6 μM at 100 μM ATP). TBB also inhibits three other kinases with less potency: CDK2 (IC₅₀=15.6 μM), phosphorylase kinase (IC₅₀=8.7 μM) and glycogen synthase kinase 3β (GSK3β) (IC₅₀=11.2 μM). All other kinases tested have IC50 values 50-fold greater than that for CK2. The viability of the androgen insensitive PC-3 cells may be diminished by TBB (60 μM TBB) acting either alone or combined with anticancer agents CPT or TRAIL when a proper time schedule of the administration is applied. The time schedule-dependent activity of TBB does not come from its effect on apoptosis in PC-3 cells. TBB is an ATP/GTP competitive inhibitor of protein kinase casein kinase-2 (CK2), has been examined against a panel of 33 protein kinases, either Ser/Thr- or Tyr-specific. In the presence of 10 μM TBB (and 100 μM ATP) only CK2 is drastically inhibited (>85%) whereas three kinases (phosphorylase kinase, glycogen synthase kinase 3L and cyclin-dependent kinase 2/cyclin A) underwent moderate inhibition, with IC₅₀ values one-two orders of magnitude higher than CK2 (IC₅₀=0.9 μM). TBB also inhibits endogenous CK2 in cultured Jurkat cells.

In Vivo: The extent of retinal neovascularization in a mouse OIR model is reduced by approximately 60% after treatment with TBB (6 days at 60 mg/kg per day).

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