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BMX-IN-1
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMX-IN-1图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
2mg电议
5mg电议
10mg电议
50mg电议

产品介绍
BMX-IN-1 是一种选择性、不可逆的 X 染色体上骨髓酪氨酸激酶 (BMX) 抑制剂,靶向 BMX ATP 结合域中的 Cys496,IC50 为 8 nM,还靶向相关的布鲁顿酪氨酸激酶 (BTK),具有IC50 值为 10.4 nM,但对 Blk、JAK3、EGFR、Itk 或 Tec 活性的效力低 47-656 倍以上。

Kinase assay

The serially diluted BMX-IN-1 was added to the BTK kinase. After 30 min incubation at RT, ATP (final concentration: 20μM) was added and incubated for 20 min at 37℃. The reactions were stopped by addition of 5X sample buffer. Then the phosphorylation of BTK was detected by western-blot using a pBTK Y551 antibody (BD).

Cell lines

Ramos cell line

Preparation method

The solubility of this compound in DMSO is >5.3 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

0.3, 1, 3 and 10 uM for 16/24/48 hours.

Applications

In Ramos cell line, BMX-IN-1 significantly inhibited cell cycle progression at G0/G1 in a dose-dependent manner at 24h and strongly induced apoptosis at a concentration of 1 μM at 8h, while with a longer drug exposure (24 hours), a concentration of 300 nM was sufficient to induce apoptosis.

产品描述

BMX-IN-1 is a highly selective and irreversible inhibitor of BMX kinase [1].
BMX, also known as ETK, is a member of Tec family and plays an important role in regulating ischemia-mediated arteriogenesis and lymphangiogenesis. BMX is mainly expressed in arterial endothelia and in myeloid hematopoietic cells and it has been reported that BMX involves in tumor growth [2].
BMX-IN-1 is a potent BMX kinase inhibitor and has an irreversible function on BMX kinase. When tested with prostate cancer cell lines, BMX-IN-1 treatment inhibited the proliferation of Tel-BMX-transformed Ba/F3 cells at lowdose [1].
References:
[1].Liu, F., et al., Discovery of a selective irreversible BMX inhibitor for prostate cancer. ACS Chem Biol, 2013. 8(7): p. 1423-8.
[2].Holopainen, T., et al., Deletion of the endothelial Bmx tyrosine kinase decreases tumor angiogenesis and growth. Cancer Res, 2012. 72(14): p. 3512-21.