2. Cell Cycle/DNA Damage TGF-beta/Smad Stem Cell/Wnt Cytoskeleton
  3. ROCK
  4. BDP5290

BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.

For research use only. We do not sell to patients.

BDP5290 Chemical Structure

BDP5290 Chemical Structure

CAS No. : 1817698-21-7

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Customer Review

Based on 1 publication(s) in Google Scholar

BDP5290 Related Antibodies

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ROCK ROCK1 ROCK2

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.

IC50 & Target[1]

ROCK1

5 nM (IC50)

ROCK2

50 nM (IC50)

MRCKα

10 nM (IC50)

MRCKβ

100 nM (IC50)

In Vitro

The Ki of BDP5290 for MRCKα is 10 nM, which is slightly more than the Ki of 4 nM for MRCKβ. 3 μM BDP5290 completely inhibits myosin II light chain (MLC) phosphorylation induced by MRCKβ, but not by ROCK1 or ROCK2. At higher concentrations, BDP5290 reduces MLC phosphorylation (pMLC) to undetectable levels. BDP5290 reduces MDA-MB-231 invasion at all tested concentrations starting from 0.1 μM, with virtually complete inhibition at 10 μM. After 24 hours in the presence of BDP5290 cell viability is slightly reduced with an EC50  >10 μM. Wound closure is inhibited by >60% at 1 μM BDP5290, a concentration that has no effect on cell viability[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BDP5290 Related Antibodies
Molecular Weight

371.82

Formula

C17H18ClN7O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC(C(C(NC1=CNN=C1C2=NC=CC=C2)=O)=N3)=CN3C4CCNCC4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (33.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References
Kinase Assay
[2]

MRCKα, MRCKβ, ROCK1 and ROCK2 assays are performed using an IMAP fluorescence polarization assay format. 8 to 12 nM of each kinase is incubated for 60 min at room temperature with 100 nM FAM-S6-ribosomal protein derived peptide in the presence of 1 μM ATP and 0.5 mM MgCl2 in 20 mM Tris buffer (pH 7.4) containing 0.01% Tween-20 and 1 mM DTT (MRCKα and β); or 1 μM ATP, 10 mM MgCl2 in 20 mM Tris buffer (pH 7.5) containing 0.25 mM EGTA 0.01% Triton X-100 and 1 mM DTT (ROCK1 and ROCK2). Typically, dose response analysis are performed over concentration ranges from 0.005 to 100 μM. Reactions are stopped by adding 2 assay volumes of 0.25% (v/v) IMAP binding reagent in 1×IMAP binding buffer. After 30 min incubation to allow binding reagent to bind phosphorylated peptide, fluorescence polarization is measured on a plate reader at excitation (470 nm) and emission (530 nm) wavelengths. Inhibition is calculated using no inhibitor and no enzyme controls as 0 and 100% inhibition, respectively. Kinase selectivity profiling is performed by Eurofins with 10 μM ATP and 10 μM BDP5290[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay
[2]

MDA MB 231 or SCC12 cells are plated in a 96 well plate and cultured for 24 hours. Cells are then cultured for 24 hours in SCC12 medium with DMSO vehicle or indicated concentrations of BDP5290 in an IncuCyte ZOOM. Pictures are taken every 3 hours and confluence is measured using the IncuCyte analysis software. AlamarBlue is added to the medium and the cells are cultured for an additional day. Absorbances at 570 nm and at 600 nm are measured to assess cell health[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.6895 mL 13.4474 mL 26.8947 mL 67.2368 mL
5 mM 0.5379 mL 2.6895 mL 5.3789 mL 13.4474 mL
10 mM 0.2689 mL 1.3447 mL 2.6895 mL 6.7237 mL
15 mM 0.1793 mL 0.8965 mL 1.7930 mL 4.4825 mL
20 mM 0.1345 mL 0.6724 mL 1.3447 mL 3.3618 mL
25 mM 0.1076 mL 0.5379 mL 1.0758 mL 2.6895 mL
30 mM 0.0896 mL 0.4482 mL 0.8965 mL 2.2412 mL
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BDP5290 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BDP52901817698-21-7BDP 5290BDP-5290ROCKRho-associated protein kinaseRho-associated kinaseRho-kinaseROKInhibitorinhibitorinhibit

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