A potent RSK2 inhibitor (IC50 = 1.1 nM) that also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A

BIX 02565 – 1 mg

Brand:
Cayman
CAS:
1311367-27-7
Storage:
-20
UN-No:
De Minimis - 3077 / 9

The 90 kDa ribosomal S6 kinases (RSKs) are a group of serine/threonine kinases involved in diverse cellular processes, including growth, survival, and motility. Phosphorylation of the sodium-hydrogen exchanger (NHE) in cardiac tissue by RSK has been shown to activate NHE during cellular stresses, such as myocardial infarction, as a mechanism to maintain pH. BIX 02565 is a RSK2 inhibitor with an IC50 value of 1.1 nM.{30925,30924} It also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A, α1B, α1D, α2A, β2, and imidazoline I2 receptors.{30925,30924} BIX 02565 can also inhibit LRRK2 and PRKD1 with IC50 values of 16 and 35 nM, respectively).{30925} In rats, BIX 02565 at 1, 3, and 10 mg/kg was shown to significantly decrease heart rate and mean arterial pressure.{30924}  

 

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Description

A potent RSK2 inhibitor (IC50 = 1.1 nM) that also demonstrates off-target binding at multiple adrenergic receptor subtypes that are important for vascular tone and cardiac function (IC50s = 0.052-1.820 μM for adrenergic α1A, α1B, α1D, α2A, β2, and imidazoline I2 receptors); also inhibits LRRK2 and PRKD1 (IC50s = 16 and 35 nM, respectively)

Formal name: (5R)-N-[1-[3-(dimethylamino)propyl]-1H-benzimidazol-2-yl]-2,3,4,5-tetrahydro-5-methyl-1-oxo-1H-[1,4]diazepino[1,2-a]indole-8-carboxamide

Synonyms: 

Molecular weight: 458.6

CAS: 1311367-27-7

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Receptor Pharmacology||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cardiovascular System|Heart||Research Area|Cardiovascular System|Vasculature|Vasodilation||Research Area|Cell Biology|Cell Signaling

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