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BDP5290

رقم الكتالوجGC32868

BDP5290 هو مثبط قوي لكل من ROCK و MRCK مع IC50s من 5 نانومتر و 50 نانومتر و 10 نانومتر و 100 نانومتر لـ ROCK1 و ROCK2 و MRCKα و MRCKβ ، على التوالي

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BDP5290 التركيب الكيميائي

Cas No.: 1817698-21-7

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
110٫00
متوفر
2mg
83٫00
متوفر
5mg
135٫00
متوفر
10mg
225٫00
متوفر
50mg
720٫00
متوفر
100mg
1125٫00
متوفر

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مراجعات العميل

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Sample solution is provided at 25 µL, 10mM.

Product has been cited by 1 publications

Description of BDP5290

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).

Protocol of BDP5290

Cell experiment [1]:

Cell lines

Alveolar epithelial type II cells (ATII)

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.

Reaction Conditions

2 µM for 24 hours

Applications

Consistent with siRNA silencing, baseline TEER was decreased upon MRCKα inhibition. BDP5290 treatment prevented the β1 subunit-induced increase of barrier integrity

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).

Chemical Properties of BDP5290

Cas No. 1817698-21-7 SDF
Canonical SMILES ClC(C(C(NC1=CNN=C1C2=NC=CC=C2)=O)=N3)=CN3C4CCNCC4
Formula C17H18ClN7O M.Wt 371.82
الذوبان DMSO : 12.5 mg/mL (33.62 mM) Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of BDP5290

Prepare stock solution
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
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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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