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CAS No.: 891025-25-5

BAMB-4 Catalog No. CSN18531

Synonyms: ITPKA-IN-C14;Bamb-4

BAMB-4 is a membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A ((ITPKA) with IC50 of 37 μM in ADP-Glo Assay.

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技术信息

生物活性

描述BAMB-4 is a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A((ITPKA) with IC50 of 37 μM in ADP-Glo Assay. Only BAMB-4 was nearly completely taken up by H1299 cells and remained stable after cellular uptake, thus exhibiting a robust stability and a high membrane permeability. Determination of the inhibitor type revealed that BAMB-4 belongs to the group of mixed type inhibitors. BAMB-4 is also a membrane-permeable InsP3Kinase inhibitor with IC50-value of 20 μM^[2]. ITPKA inhibitor BAMB-4 exhibit the lowest inhibition frequency among the InsP3- Kinase inhibitors. Only in one from 42 targets tested, BAMB-4 showed an inhibitory effect. Noteworthy, in kinase screens no targets of BAMB-4 were detected, indicating that the compound does not belong to the typical kinase inhibitors. Thus, the relative high specificity and the high cellular uptake of BAMB-4 now for the test provide the possibility to effectively inhibit InsP3kinase in vivo. The InsP3Kinase activity is essentially involved in ITPKA promoted metastasis of lung cancer cells, BAMB-4 is a promising therapeutic approach in lung cancer therapy^[3].
参考文献

[1] Schroder D, Rehbach C, et al. Identification of a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A. Biochem Biophys Res Commun. 2013 Sep 20;439(2):228-34.
[2] Schröder D, Tödter K, Gonzalez B, Franco-Echevarría E, Rohaly G, Blecher C, Lin HY, Mayr GW, Windhorst S. The new InsP3Kinase inhibitor BIP-4 is competitive to InsP3 and blocks proliferation and adhesion of lung cancer cells. Biochem Pharmacol. 2015 Jul 15;96(2):143-50
[3] Schröder D, Rehbach C, Seyffarth C, Neuenschwander M, Kries JV, Windhorst S. Identification of a new membrane-permeable inhibitor against inositol-1,4,5-trisphosphate-3-kinase A. Biochem Biophys Res Commun. 2013 Sep 20;439(2):228-34

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.9640 mL
- 19.8202 mL
- 39.6404 mL
- 5 mM
- 0.7928 mL
- 3.9640 mL
- 7.9281 mL
- 10 mM
- 0.3964 mL
- 1.9820 mL
- 3.9640 mL

技术信息

CAS号

891025-25-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C15H12N2O2

运输

蓝冰

分子量

252.27

别名

ITPKA-IN-C14;Bamb-4

溶解度

DMSO	40.0 mg/mL (158.6 mM)

动物实验配方

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