1. Cell Cycle/DNA Damage
    TGF-beta/Smad
    Stem Cell/Wnt
  2. ROCK

BDP5290 

Cat. No.: HY-12437 Purity: >98.0%
Handling Instructions

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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 177 In-stock
Estimated Time of Arrival: December 31
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 216 In-stock
Estimated Time of Arrival: December 31
10 mg USD 360 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2280 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

Solvent & Solubility
In Vitro: 

DMSO : 12.5 mg/mL (33.62 mM; Need ultrasonic)

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
10 mM 0.2689 mL 1.3447 mL 2.6895 mL
*Please refer to the solubility information to select the appropriate solvent.
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
Molecular Weight

371.82

Formula

C₁₇H₁₈ClN₇O

CAS No.

1817698-21-7

SMILES

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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
BDP5290
Cat. No.:
HY-12437
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BDP5290

Cat. No.: HY-12437