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tBID {[allProObj[0].p_purity_real_show]}

货号:A723630

tBID is a potent and selective inhibitor of HIPK2 with an IC50 value of 0.33 μM. It inhibits HIPK2 through ATP competition with a Ki value of 200 nM.

tBID 化学结构 CAS号:1639895-85-4
tBID 化学结构
CAS号:1639895-85-4
tBID 3D分子结构
CAS号:1639895-85-4
tBID 化学结构 CAS号:1639895-85-4
tBID 3D分子结构 CAS号:1639895-85-4
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tBID 纯度/质量文件 产品仅供科研

货号:A723630 标准纯度: {[allProObj[0].p_purity_real_show]}
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tBID 生物活性

描述 Homeodomain-interacting protein kinase 2 (HIPK2) is a serine/threonine protein kinase involved in cell proliferation and survival. tBID is a potent and selective inhibitor of HIPK2 with an IC50 value of 0.33 μM. It inhibits HIPK2 through ATP competition with a Ki value of 200 nM. When tBID was tested at the concentration of 1 μM, the residual activities of HIPK1 and HIPK3 were 39% and 53%, respectively, as compared to HIPK2 (31% residual activity). tBID also displayed inhibitory potential against CK2 with an IC50 value of 5.50 μM. The treatment of HepG2 cells with 10 and 50 μM of TBID led to a reduction of endogenous HIPK2 activity in a dose-dependent manner. TBID treatment (10 and 50 μM) also greatly reduced the level of p53 Ser46 without affecting the amount of p53[1]. Mechanism: tBID is an ATP-competitive inhibitor of HIPK2. It inhibits HIPK2 by interacting with its hinge region through hydrophobic interactions between Val 213, Val 261, Phe 277, Leu 280, Met 331, Ile 345, and the tetrabromine moiety[1].

tBID 参考文献

[1]Cozza G, Zanin S, Determann R, Ruzzene M, Kunick C, Pinna LA. Synthesis and properties of a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2). PLoS One. 2014 Feb 24;9(2):e89176. doi: 10.1371/journal.pone.0089176. PMID: 24586573; PMCID: PMC3933419.

tBID 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.89mL

0.38mL

0.19mL

9.46mL

1.89mL

0.95mL

18.91mL

3.78mL

1.89mL

tBID 技术信息

CAS号1639895-85-4
分子式C11H3Br4N3O2
分子量 528.776
别名
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 18 mg/mL(34.04 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

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