产品说明
一般描述
A cell-permeable benzotriazolo compound that acts as a highly selective, ATP/GTP-competitive casein kinase II (CKII) inhibitor (IC50 = 900 nM and 1.6 µM for rat liver and human recombinant CKII, respectively) and DYRK (IC50<1 µM for DYRK1a). Specificity for CKII has been reported following the screening of 33 kinases, including PKA, Akt, PKC, MKK1, ERK2, p38, JNK, Lck, Lyn, and Syk. Also reported to inhibit NS3-associated viral helicase activity in hepatitis C virus (HCV) (IC50 = 20 and 60 µM using DNA and RNA substrates, respectively) and West Nile virus (WNV) (IC50 = 1.7 µM and 900 nM using DNA and RNA substrates, respectively).
A cell-permeable benzotriazolo compound that acts as a higly selective, reversible, and ATP/GTP-competitive inhibitor of casein kinase-2 (CK2) (IC50 = 900 nM and 1.6 M, using rat liver and human recombinant CK2, respectively) and DYRK (IC50<1 M for DYRK1a). Its specificity has been demonstrated using a panel of 33 kinases, including PKA, PKB, PKC, MKK1, Erk2, p38, JNK, Lck, Lyn, and Syk. Also shown to inhibit NS3-associated viral helicase activities in HCV (IC50 = 20 and 60 M, using DNA and RNA substrate, respectively) and WNV (IC50 = 1.7 and 900 nM, using DNA and RNA substrate, respectively). A 10 mM (5 mg/1.15 ml) solution of Casein Kinase II Inhibitor I in DMSO, is also available.
包装
10 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Product competes with ATP.
Target IC50: 900 nM and 1.6 µM, using rat liver and human recombinant CK2, respectively; <1 µM for DYRK1a
Reversible: yes
警告
Toxicity: Carcinogenic / Teratogenic (D)
其他说明
Borowski, P., et al. 2003. Eur. J. Biochem.270, 1645.
Sarno, S., et al. 2003. Biochem. J.374, 639.
Zien, P., et al. 2003. Biochem. Biophys. Res. Commun.306, 129.
Ruzzene, M., et al. 2002. Biochem. J.364, 41.
Sarno, S., et al. 2001. FEBS Lett.496, 44.
Szyszka, R., et al. 1995. Biochem. Biophys. Res. Commun.208, 418.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
经验(实验)分子式 | C6HBr4N3 |
分子量 | 434.71 |
MDL编号 | MFCD06411399 |
产品性质
质量水平 | 100 |
测定 | ≥99% (HPLC) |
形式 | solid |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | white |
溶解性 | DMSO: 10 mg/mL |
运输 | ambient |
储存温度 | 2-8℃ |
InChI | 1S/C6HBr4N3/c7-1-2(8)4(10)6-5(3(1)9)11-13-12-6/h(H,11,12,13) |
InChI key | OMZYUVOATZSGJY-UHFFFAOYSA-N |