2. MAPK/ERK Pathway
  3. Ribosomal S6 Kinase (RSK)
  4. BIX 02565

BIX 02565 is a potent ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM.

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

BIX 02565 Chemical Structure

BIX 02565 Chemical Structure

CAS No. : 1311367-27-7

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 192 In-stock
Solution
10 mM * 1 mL in DMSO USD 192 In-stock
Solid
2 mg USD 88 In-stock
5 mg USD 156 In-stock
10 mg USD 245 In-stock
50 mg USD 660 In-stock
100 mg USD 990 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 6 publication(s) in Google Scholar

BIX 02565 Related Antibodies

Top Publications Citing Use of Products

View All Ribosomal S6 Kinase (RSK) Isoform Specific Products:

View All Isoforms
p70S6K RSK1 RSK2 RSK3 RSK4

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BIX 02565 is a potent ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM.

IC50 & Target

IC50: 1.1 nM (RSK2)[1]
In Vitro

BIX 02565, a potent RSK2 inhibitor (IC50=1.1 nM) targets for the treatment of heart failure secondary to myocardial infarction through indirect NHE inhibition[1]. BIX 02565, a second Rsk inhibitor, protects enzyme active sites from reaction with biotinylated nucleotide acyl phosphates[2].

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

BIX 02565 Related Antibodies
In Vivo

In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicits concentration-dependent decreases in MAP after each dose (to -39±4 mm Hg on day 4 at Tmax). BIX 02565 produces concentration-dependent relaxation ex vivo in the phenylephrine-constricted rat aortic ring at concentrations above 0.03 μM with a calculated EC50 of 3.1 μM. Subsequently, BIX 02565 is infused in the anesthetized rat in a low-dose (0.1, 0.3, and 1.0 mg/kg per 20 min) and high-dose (1.0, 3.0, and 10.0 mg/kg per 20 min) series of continuous infusions to test the effect of compound on hemodynamics in vivo[1].

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

458.56

Formula

C26H30N6O2
CAS No.
Appearance

Solid

Color

White to light yellow

SMILES

O=C(C1=CC2=C(C=C1)C=C3N2[C@H](C)CCNC3=O)NC4=NC5=CC=CC=C5N4CCCN(C)C
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 : 20.75 mg/mL (45.25 mM; Need ultrasonic and warming; 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 2.1807 mL 10.9037 mL 21.8074 mL
5 mM 0.4361 mL 2.1807 mL 4.3615 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
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 1.67 mg/mL (3.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 1.67 mg/mL (3.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 1.67 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (16.7 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.61%

COA (256 KB) LCMS (105 KB)

Handling Instructions (2659 KB)
References
Kinase Assay
[1]

Radioligand binding studies are performed at MDS Pharma Services. Mean percentage inhibition of specific binding or activity is shown for each assay tested, and in selected assays (for BIX 02565) when inhibition of adrenergic binding generally exceeded 50%, an IC50 is determined by a nonlinear least-squares regression analysis. In brief, human RSK2 protein is used to measure kinase activity utilizing Kinase GloPlus that uses a luciferin-luciferase based detection reagent to quantify residual ATP. The relative light unit signal is measured on an LJL Analyst in luminescence mode using 384 aperture; relative light unit signals are converted to percentage of control; the IC50 is fitted to a standard four-parameter logistic equation[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Rats[1]
Mean arterial pressure is assessed in conscious, freely moving male Sprague-Dawley rats (n=6/group) instrumented with telemetry transmitters. BIX 02565 (30, 100, and 300 mg/kg p.o. QD) is administered as a solution (10 mL/kg) in a 20% hydroxy-propyl-β-cyclodextran vehicle. Mean arterial pressure is reported from 2 h before (baseline) and 90 h after the first dose; compound is administered at 0, 24, 48, and 72 h. A blood sample is collected from satellite rats (n=3/group) at 1-h after dose (Tmax) on days 1 and 4 for analysis of plasma drug concentrations by mass spectrometry.

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 2.1807 mL 10.9037 mL 21.8074 mL 54.5185 mL
5 mM 0.4361 mL 2.1807 mL 4.3615 mL 10.9037 mL
10 mM 0.2181 mL 1.0904 mL 2.1807 mL 5.4518 mL
15 mM 0.1454 mL 0.7269 mL 1.4538 mL 3.6346 mL
20 mM 0.1090 mL 0.5452 mL 1.0904 mL 2.7259 mL
25 mM 0.0872 mL 0.4361 mL 0.8723 mL 2.1807 mL
30 mM 0.0727 mL 0.3635 mL 0.7269 mL 1.8173 mL
40 mM 0.0545 mL 0.2726 mL 0.5452 mL 1.3630 mL
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

BIX 02565 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:

BIX 025651311367-27-7BIX02565BIX-02565Ribosomal S6 Kinase (RSK)S6KInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
BIX 02565
Cat. No.:
HY-16104
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.