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BIX 02565

Catalog No. T5428   CAS 1311367-27-7

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

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
BIX 02565 Chemical Structure
BIX 02565, CAS 1311367-27-7
Pack Size Availability Price/USD Quantity
1 mg In stock $ 75.00
2 mg In stock $ 108.00
5 mg In stock $ 187.00
10 mg In stock $ 297.00
25 mg In stock $ 553.00
50 mg In stock $ 796.00
1 mL * 10 mM (in DMSO) In stock $ 189.00
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Purity: 97.44%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description BIX 02565 is a potent inhibitor of ribosomal S6 kinase 2 (RSK2, IC50: 1.1 nM).
Targets&IC50 PRKD1:35 nM (cell free), RSK2:1.1 nM (cell free), LRRK2:16 nM (cell free)
In vitro BIX 02565 inhibited RSK2 with IC50 value of 1.1 nM. It also inhibited LRRK2 and PRKD1 with IC50 values of 16 and 35 nM [1]. BIX 02565 elicited >50% inhibition at adrenergic α1A-, α1B-, α1D-, α2A-, β2-, and imidazoline I2 receptors (IC50s: 0.052-1.820 μM) [2].
In vivo Infusion of BIX 02565 (1, 3, and 10 mg/kg) in the rat CV screen resulted in a precipitous decrease in both mean arterial pressure (MAP; to -65 ± 6 mm Hg below baseline) and heart rate (-93 ± 13 beats/min). In telemetry-instrumented rats, BIX 02565 (30, 100, and 300 mg/kg p.o. QD for 4 days) elicited concentration-dependent decreases in MAP after each dose (to -39 ± 4 mm Hg on day 4 at T(max)); analysis by Demming regression demonstrated strong correlation independent of route of administration and influence of anesthesia [2].
Cell Research A monolayer of exponentially growing HLR-CREB cells was prepared and transfected using Effectene with RSK2. Cells were plated into 96-well culture plates, and compounds were added 20 to 24 h after transfection. Luciferase expression (48 h) and activity (5 min) were determined using Steady-Glo per manufacturer's instructions, and results were represented as the percentage luciferase activity relative to the control measured in the absence of inhibitors (percentage of control); the IC50 was fitted to a standard four-parameter logistic equation. Each data point represents an average of triplicate observations [2].
Animal Research Mean arterial pressure was assessed in conscious, freely moving male Sprague-Dawley rats (n = 6/group) instrumented with telemetry transmitters similar to that described previously. BIX 02565 (30, 100, and 300 mg/kg p.o. QD) was administered as a solution (10 ml/kg) in a 20% hydroxy-propyl-β-cyclodextran vehicle as described previously. Mean arterial pressure was reported from 2 h before (baseline) and 90 h after the first dose; compound was administered at 0, 24, 48, and 72 h. A blood sample was 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 [2].
Molecular Weight 458.56
Formula C26H30N6O2
CAS No. 1311367-27-7

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 20 mg/mL

TargetMolReferences and Literature

1. Kirrane TM, et al. Indole RSK inhibitors. Part 2: optimization of cell potency and kinase selectivity. Bioorg Med Chem Lett. 2012 Jan 1;22(1):738-42. 2. Fryer RM, et al. Mitigation of off-target adrenergic binding and effects on cardiovascular function in the discovery of novel ribosomal S6 kinase 2 inhibitors. Journal of Pharmacology and Experimental Therapeutics (2012), 340(3), 492-500.

TargetMolCitations

1. Yuan Y, Xu J, Jiang L, et al. Discovery, Optimization, and Structure–Activity Relationship Study of Novel and Potent RSK4 Inhibitors as Promising Agents for the Treatment of Esophageal Squamous Cell Carcinoma. Journal of Medicinal Chemistry. 2021

Related compound libraries

This product is contained In the following compound libraries:
Reprogramming Compound Library PI3K-AKT-mTOR Compound Library Oxidation-Reduction Compound Library Anti-Neurodegenerative Disease Compound Library MAPK Inhibitor Library Anti-Parkinson's Disease Compound Library Glycometabolism Compound Library

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Keywords

BIX 02565 1311367-27-7 Autophagy MAPK PI3K/Akt/mTOR signaling LRRK2 S6 Kinase Inhibitor Ribosomal S6 Kinase (RSK) S6K inhibit BIX-02565 BIX02565 inhibitor

 

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