BIX 02565
Based on 8 publication(s) in Google Scholar
BIX 02565 is a potent ribosomal S6 kinase 2 (RSK2) inhibitor with IC50 of 1.1 nM.
Para uso exclusivo en investigación. No vendemos a pacientes.
The BIX 02565 was designed by Boehringer Ingelheim and could be obtained free of charge through the Boehringer Ingelheim open innovation portal opnMe.com, associated with its negative control.
- Pureza : 99.61%
- No. CAS: 1311367-27-7
- Fòrmula: C26H30N6O2
- Peso molecular:458.56
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) BIX 02565
More- Nat Commun. 2026 Feb 12;17(1):1214. [Abstract]
- Adv Sci (Weinh). 2022 Oct;9(30):e2200717. [Abstract]
- Phytomedicine. 2025 Dec:149:157524. [Abstract]
- EMBO J. 2024 Oct;43(20):4752-4785. [Abstract]
- J Invest Dermatol. 2023 Jan;143(1):26-36.e8. [Abstract]
- J Invest Dermatol. 2022 Dec;142(12):3175-3183.e5. [Abstract]
- PLoS One. 2024 Nov 1;19(11):e0308647. [Abstract]
- Biomed Pharmacother. 2024 May:174:116477. [Abstract]
Actividad biológica
Descripciòn
IC50 & Target
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RSK2 |
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.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1311367-27-7
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Appearance Solid
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Peso molecular 458.56
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Fòrmula C26H30N6O2
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Color White to light yellow
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SMILES
O=C(C1=CC2=C(C=C1)C=C3N2[C@H](C)CCNC3=O)NC4=NC5=CC=CC=C5N4CCCN(C)C
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (8)
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Journal Impact Factor
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Most Recent
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Nat Commun
Human iPSC-based Modeling of Pulmonary Fibrosis Reveals p300/CBP Inhibition Suppresses Alveolar Transitional Cell State. [Abstract]2026 Feb 12;17(1):1214. PMID: 41680175 -
Adv Sci (Weinh)
Functional Phosphoproteomics in Cancer Chemoresistance Using CRISPR-Mediated Base Editors. [Abstract]2022 Oct;9(30):e2200717. PMID: 36045417 -
Phytomedicine
Icariin rescues immune dysfunction in sepsis through RSK2-driven YAP-cGAS-IFN-β signaling activation. [Abstract]2025 Dec:149:157524. PMID: 41240541 -
EMBO J
2024 Oct;43(20):4752-4785. PMID: 39256562 -
J Invest Dermatol
δ-Catenin Requirement in Keratinocyte Proliferation and DNA Repair Identifies a Therapeutic Target for Photoaging. [Abstract]2023 Jan;143(1):26-36.e8. PMID: 35940223 -
J Invest Dermatol
2022 Dec;142(12):3175-3183.e5. PMID: 35853487 -
PLoS One
A novel small molecule screening assay using normal human chondrocytes toward osteoarthritis drug discovery. [Abstract]2024 Nov 1;19(11):e0308647. PMID: 39485774 -
Biomed Pharmacother
2024 May:174:116477. PMID: 38522235
Solvente y solubilidad
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocolo
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].
MedChemExpress (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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
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 |
BIX 02565 Related Classifications
HY-16104 Related Classifications
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