TBB

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TBB(NSC 231634) 是一种高选择性、ATP/GTP 竞争性酪蛋白激酶-2 (CK2) 抑制剂，对大鼠肝脏和人重组 CK2 的 IC50 值分别为 0.9 和 1.6 μM。

TBB(NSC 231634) is a highly selective, ATP/GTP-competitive inhibitor of casein kinase-2 (CK2)with IC50s of 0.9 and 1.6 μM for rat liver and human recombinant CK2 respectively).

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.

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).

NSC 231634 | Tetrabromobenzotriazole

Angiogenesis

CDK

CK2| CDK2| GSK-3β

Cancer

——

17374-26-4

434.71

C6HBr4N3

>98% (HPLC)

DMSO, Ethanol: 100 mM

BrC1=C(NN=N2)C2=C(Br)C(Br)=C1Br

4,5,6,7-tetrabromo-1H-benzo[d][1,2,3]triazole

(-20℃)

With Ice Pack

≥ 2 years