BDP5290
Catalog No.: GC32868Purity:>98.50%
BDP5290 is a potent inhibitor of ROCK and MRCK with IC50 values of 17nM, 230nM, 123nM and 100nM for MRCKβ, ROCK1, ROCK2, respectively.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1817698-21-7
10mM (in 1mL DMSO)In Stock
$110.00
1
2mgIn Stock
$83.00
1
5mgIn Stock
$135.00
1
10mgIn Stock
$225.00
1
50mgIn Stock
$720.00
1
100mgIn Stock
$1,125.00
1
| Pack Size | Price | Availability | Quantity | Action |
|---|---|---|---|---|
| 10mM (in 1mL DMSO) | $110.00 | In Stock | 1 | |
| 2mg | $83.00 | In Stock | 1 | |
| 5mg | $135.00 | In Stock | 1 | |
| 10mg | $225.00 | In Stock | 1 | |
| 50mg | $720.00 | In Stock | 1 | |
| 100mg | $1,125.00 | In Stock | 1 |
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Citations
1 publicationsPublications from researchers using this productDescription
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
| 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 |
|
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). |
|
Product Documents
Purity:>98.50%Appearance:A solid
Chemical Properties
CAS No.
1817698-21-7
SMILES
ClC(C(C(NC1=CNN=C1C2=NC=CC=C2)=O)=N3)=CN3C4CCNCC4
Molecular Formula
C17H18ClN7O
Molecular Weight
371.82
Solubility
DMSO : 12.5 mg/mL (33.62 mM)
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
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