BDP5290
目录号 : GC32868
BDP5290对MRCKβ、ROCK1、ROCK2的IC50值分别为17nM、230nM、123nM和100nM，是ROCK和MRCK的有效抑制剂。
Cas No.:1817698-21-7
Sample solution is provided at 25 µL, 10mM.
BDP5290 is a potent inhibitor of ROCK and MRCK with IC50 values of 17nM, 230nM, 123nM and 100nM for MRCKβ, ROCK1, ROCK2, respectively [1].
BDP5290 (2 µM, 24h) treated ATII cells decreased baseline TEER, and prevented the β1 subunit-induced increase of barrier integrity [2]. 3 µM BDP5290 completely inhibited MLC phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2 [1]. BDP5290 treated parental MDA-MB-231 breast cancer cells at varying concentrations, and showed endogenous MRCK and ROCK inhibition effect of pMLC with EC50 of 316 nM [1]. application of 0.5 µM BDP5290 lessened both cytoplasmic and cortical pMLC levels in MDA-MB-231 cells [1]. BDP5290 reduced MDA-MB-231 invasion at concentrations starting from 0.1 µM, with virtually complete inhibition at 10 µM [1]. 2-µM BDP5290 strongly inhibited the ability of human SCC12 squamous cell carcinoma cells to invade a 3D collagen matrix [1].
References:
[1]. Unbekandt M, Croft D R, Crighton D, et al. A novel small-molecule MRCK inhibitor blocks cancer cell invasion[J]. Cell Communication and Signaling, 2014, 12(1): 1-15.
[2]. Bai H, Zhou R, Barravecchia M, et al. The Na+, K+-ATPase β1 subunit regulates epithelial tight junctions via MRCKα[J]. JCI insight, 2021, 6(4).
| Cell experiment [1]: | |
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Cell lines |
Alveolar epithelial type II cells (ATII) |
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Preparation Method |
ATII cells were cotransfected with plasmids (CMV-tet and Tet-β1) 24 hours after isolation and treated immediately with 2 µM MRCKα inhibitor BDP5290. transepithelial electrical resistance (TEER) was measured 24 hours later. |
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Reaction Conditions |
2 µM for 24 hours |
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Applications |
Consistent with siRNA silencing, baseline TEER was decreased upon MRCKα inhibition. BDP5290 treatment prevented the β1 subunit-induced increase of barrier integrity |
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References: [1]: Bai H, Zhou R, Barravecchia M, et al. The Na+, K+-ATPase β1 subunit regulates epithelial tight junctions via MRCKα[J]. JCI insight, 2021, 6(4). |
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| Cas No. | 1817698-21-7 | SDF | |
| Canonical SMILES | ClC(C(C(NC1=CNN=C1C2=NC=CC=C2)=O)=N3)=CN3C4CCNCC4 | ||
| 分子式 | C17H18ClN7O | 分子量 | 371.82 |
| 溶解度 | DMSO : 12.5 mg/mL (33.62 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.6895 mL | 13.4474 mL | 26.8947 mL |
| 5 mM | 0.5379 mL | 2.6895 mL | 5.3789 mL |
| 10 mM | 0.2689 mL | 1.3447 mL | 2.6895 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet