| BMX-IN-1BMX (also termed ETK) kinase inhibitor |

Sample solution is provided at 25 µL, 10mM.
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Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 97.99%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure

| Description | BMX-IN-1 is a highly selective and potent irreversible inhibitor of BMX kinase. | |||||
| Targets | BMX Kinase | |||||
| IC50 | ||||||
| Kinase experiment [1]: | |
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°C. 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 experiment [1]: | |
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. |
References: [1]. Hong Wu, et al. Discovery of a Potent, Covalent BTK Inhibitor for B-Cell Lymphoma. ACS Chem Biol. 2014 May 16; 9(5): 1086–1091. | |

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| Cas No. | 1431525-23-3 | SDF | Download SDF |
| Synonyms | BMX kinase inhibitor | ||
| Chemical Name | N-[5-[9-[4-(methanesulfonamido)phenyl]-2-oxobenzo[h][1,6]naphthyridin-1-yl]-2-methylphenyl]prop-2-enamide | ||
| Canonical SMILES | CC1=C(C=C(C=C1)N2C(=O)C=CC3=CN=C4C=CC(=CC4=C32)C5=CC=C(C=C5)NS(=O)(=O)C)NC(=O)C=C | ||
| Formula | C29H24N4O4S | M.Wt | 524.59 |
| Solubility | ≥5.25 mg/mL in DMSO, <2.35 mg/ml="" in="" etoh,="">2.35><2.16 mg/ml="" in="" h2o="">2.16> | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
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探针的标记方式有放射性标记和非放射性标记。标记物质有放射性元素(如32P等)和非放射性物质(如生物素、地高辛等)。32P是最常用的核苷酸标记同位素,被标记的dNTP本身就带有磷酸基团,便于标记。特点是比活性高,可达9000Ci/mmol;发射的β射线能量高。用它标记的探针自显影时间短,灵敏度高。32P的半寿期短,虽使用不方便,但为废弃物的处理减轻了压力。非放射性标记法有酶标法和化学物标记法。酶标方法与免疫测定ELISA方法相似,只是被标记的核酸代替了被标记的抗体,事实上被标记的抗体也称为探针,现有许多商品是生物素、地高辛标记的。血凝素与生物素有非常高的亲和性,当血凝素标记上过氧化物酶或碱性磷酸酶,经杂交反应最终形成探针-生物素-血凝素酶复合物(ABC法),酶催化底物显色,观察结果。ABC法底物显色生成不溶物,以便观测结果。酶标记法复杂、重复性差,成本高,但便于运输、保存,灵敏度与放射物标记法相当。 ①缺口平移标记法。利用的是DNA聚合酶I能修复DNA链的功能。该法先由DNaseI在DNA双链上随机切出切口,然后DNA聚合酶I沿缺口水解5´端核苷酸,同时在3´端修复加入被标记核苷酸,切口平行推移。缺口平移法快速、简便、成本相对较低、比活性相对较高、标记均匀,多用于大分子DNA标记,(>1000bp最好),但单链DNA、RNA不能用该法标记。
②随机引物法。随机引物是指含有各种可能排列顺序的寡聚核苷酸片断的混合物,因此它可以与任意核苷酸序列杂交,起到聚合酶反应的引物作用。将待标记的DNA探针片断变性后与随机引物一起杂交,然后以此杂交的寡聚核苷酸为引物,在大肠杆菌DNA聚合酶I大断段(KlenowFragment)催化下,合成与探针DNA互补的DNA链,当在反应体系中含有a-32P-dNTP时,即形成放射性同位素标记的DNA探针。具有上述优点,可代替缺口平移法。此外大小、单双DNA均可标记,标记均匀,标记率高,但也不能标记环状DNA。随机引物法标记探针一般长400~600bp。
③末端标记法(又叫尾标)。利用末端转移酶可进行“尾标”,尾标适用于寡核苷酸探针标记,寡核苷酸探针多用于核酸“点”突变的检测,该探针可用核酸合成仪人工合成,克隆出的探针一般较长,特异性好,标记量大,杂交的检出信号强。 1、4—6微米切片,用防脱片胶(多聚赖氨酸)处理过的玻片贴附
2、56—60℃烤片2—16h
3、新鲜二甲苯脱蜡,10minX2(趁热脱蜡)
4、100%乙醇5minX2次,不用浸水,直接空气干燥
5、加入50μl蛋白酶K工作液(蛋白酶K用蒸馏水稀释,浓度为25μg/ml),37℃消化10—15min
6、弃去蛋白酶K工作液,0.1MTBS洗涤3minX3次逐级酒精脱水(85%,95%,100%酒精)1minX3次然后空气干燥
7、加入20μl探针,加盖薄膜。(探针用预杂交液稀释,浓度为5μg/ml)。
8、95℃变性10—12min;立刻置于冰块上,防止复性。
9、37℃杂交16—20h
10、揭去薄膜,每张切片加入以下杂交后洗涤液:
>用2—3滴2XSSC37℃洗涤3minX2次;
>0.5XSSC37℃洗涤3minX2次;
>0.2XSSC37℃洗涤3minX2次;
11、0.1MPBS/TBS缓冲液洗涤,1minX3次
12、滴加小鼠抗地高辛生物素标记的抗体工作液,37℃孵育45—60min;
13、0.1MPBS浸洗,5minX3次
14、滴加高敏碱性磷酸酶链亲和素复合物工作液,37℃孵育45—60min。
15、0.1MPBS浸洗,5minX3次
16、滴加NBT/BCIP显色6—16h,
17、双蒸水终止反应(37℃10min—2h),双蒸水浸洗,5minX2次
18、滴加核固红,30秒—5min;
19、双蒸水浸洗,5minX3次
20、脱水、透明、封片

