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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 Chemical Structure
CAS No. : 1431525-23-3
规格 | 价格 | 是否有货 | 数量 |
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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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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) |
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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. |
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分子量 |
524.59 |
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Formula |
C29H24N4O4S |
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CAS 号 |
1431525-23-3 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
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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
*
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。 |
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参考文献 |
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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. |
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参考文献 |
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