1. MAPK/ERK Pathway
  2. Ribosomal S6 Kinase (RSK)

BIX 02565 

Cat. No.: HY-16104 Purity: 98.48%
Data Sheet SDS Handling Instructions

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
10 mM * 1 mL in DMSO $192 In-stock
2 mg $120 In-stock
5 mg $190 In-stock
10 mg $300 In-stock
50 mg $900 In-stock
100 mg $1500 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

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].

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].

References
Preparing Stock Solutions
Concentration Volume 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
10 mM 0.2181 mL 1.0904 mL 2.1807 mL
Please refer to the solubility information to select the appropriate solvent.
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]

BIX 02565 is prepared in DMSO and diluted with saline or PBS[1].

Rat[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
Molecular Weight

458.56

Formula

C₂₆H₃₀N₆O₂

CAS No.

1311367-27-7

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

Solvent & Solubility

DMSO: 20.75 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BIX 02565
Cat. No.:
HY-16104
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