BMX-IN-1(Synonyms: BMX kinase inhibitor)

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BMX-IN-1 (Synonyms: BMX kinase inhibitor) 纯度: 98.82%

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。

BMX-IN-1(Synonyms: BMX kinase inhibitor)

BMX-IN-1 Chemical Structure

CAS No. : 1431525-23-3

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥1960 In-stock
2 mg ¥900 In-stock
5 mg ¥1700 In-stock
10 mg ¥3000 In-stock
50 mg ¥7500 In-stock
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200 mg   询价  

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BMX-IN-1 相关产品

相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • Kinase Inhibitor Library
  • Protein Tyrosine Kinase Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Chemical Probe Library
  • Anti-Blood Cancer Compound Library
  • Targeted Diversity Library

生物活性

BMX-IN-1 is a selective, irreversible inhibitor of bone marrow tyrosine kinase on chromosome X (BMX) that targets Cys496 in the BMX ATP binding domain with an IC50 of 8 nM, also targets the related Bruton’s tyrosine kinase (BTK) with an IC50 value of 10.4 nM, but is more than 47-656-fold less potent against Blk, JAK3, EGFR, Itk, or Tec activity.

IC50 & Target

IC50: 8 nM (BMX), 10.4 nM (BTK)

体外研究
(In Vitro)

BMX-IN-1 inhibits the proliferation of Tel-BMX-transformed Ba/F3 cells and RV-1 cells with IC50s of 25 nM and 2.53 μM. BMX-IN-1 exhibits remarkable selectivity with an S(10) score of 0.01. BMX-IN-1 inhibits only wild-type BMX with an IC50 of 138 nM. BMX-IN-1 requires covalent modification of Cys496 of BMX to achieve potent inhibition[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

524.59

Formula

C29H24N4O4S

CAS 号

1431525-23-3

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMF : 10 mg/mL (19.06 mM; Need ultrasonic)

DMSO : 8.33 mg/mL (15.88 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9063 mL 9.5313 mL 19.0625 mL
5 mM 0.3813 mL 1.9063 mL 3.8125 mL
10 mM 0.1906 mL 0.9531 mL 1.9063 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [1]. Feiyang Liu , et al. Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer. ACS Chem. Biol., DOI: 10.1021/cb4000629

Cell Assay
[1]

RV-1 cells in complete or serum-reduced DMEM are treated with DMSO, BMX-IN-1 (2.5 μM), MK2206 (200 nM), or the combination of BMX-IN-1 and MK2206 for 5 days before cells are harvested by trypsin and washed with cold PBS. The cells are then fixed in 70% cold ethanol (prechilled at −20°C) and incubated at 4°C overnight. On the day of flow cytometry, cells are collected by centrifugation, washed with PBS, and stained in 50 μg/mL propidium iodide + 0.5 mg/mL RNase in PBS + 0.5% Triton-X100 for 30 min at RT and moved to 4°C until the time of analysis. Flow cytometry is performed using a BD FACScan, and results are analyzed by ModFit software in the Flow Cytometry Core Facility in Dana-Faber Cancer Institute.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Feiyang Liu , et al. Discovery of a Selective Irreversible BMX Inhibitor for Prostate Cancer. ACS Chem. Biol., DOI: 10.1021/cb4000629

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