A GRK2 and GRK3 inhibitor (IC50s = 18 and 5.4 nM

CMPD101 – 25 mg

Brand:
Cayman
CAS:
865608-11-3
Storage:
-20
UN-No:
Non-Hazardous - /

CMPD101 is an inhibitor of G protein-coupled receptor kinase 2 (GRK2) and GRK3 (IC50s = 18 and 5.4 nM, respectively).{42803} It is selective for GRK2 and GRK3 over GRK1, GRK5, GRK6, and GRK7 (IC50s = 3,100, 2,300, >30,000, and 25,000 nM, respectively), as well as Rho-associated kinase 2 (ROCK-2) and PKCα (IC50s = 1,400 and 8,100 nM, respectively). CMPD101 induces cAMP accumulation in HEK293 cells expressing human β2-adrenergic receptors (EC50 = 10 µM). In isolated human prostate strips, CMPD101 (50 µM) inhibits contractions induced by electrical field stimulation, norepinephrine, phenylephrine, endothelin-1 (Item No. 24127), and U-46619 (Item No. 16450).{42804}  

 

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SKU: 26808 - 25 mg Category:

Description

A GRK2 and GRK3 inhibitor (IC50s = 18 and 5.4 nM, respectively); selective for GRK2 and GRK3 over GRK1, GRK5, GRK6, and GRK7 (IC50s = 3,100, 2,300, >30,000, and 25,000 nM, respectively), as well as ROCK-2 and PKCα (IC50s = 1,400 and 8,100 nM, respectively); induces cAMP accumulation in HEK293 cells expressing human β2-adrenergic receptors (EC50 = 10 µM); inhibits electrical field stimulation-, norepinephrine-, phenylephrine-, endothelin-1-, and U-46619-induced contractions in isolated human prostate strips at 50 µM,

Formal name: 3-[[[4-methyl-5-(4-pyridinyl)-4H-1,2,4-triazol-3-yl]methyl]amino]-N-[[2-(trifluoromethyl)phenyl]methyl]-benzamide

Synonyms: 

Molecular weight: 466.5

CAS: 865608-11-3

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area

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