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tBID

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Chemical Structure| 1639895-85-4 同义名 : -
CAS号 : 1639895-85-4
货号 : A723630
分子式 : C11H3Br4N3O2
纯度 : 98%
分子量 : 528.776
MDL号 : MFCD31382119
存储条件：

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
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
动物实验配方：
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].
实验方案
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
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.