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MedChemExpressModel Nexinhib20 -331949-35-0

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Nexinhib20 is a specific Rab27a-JFC1 interaction inhibitor with a calculated IC50 of 2.6 μM. Nexinhib20 significantly inhibits superoxide anion production. Nexinhib20 efficiently decreases exocytosis of azurophilic granules in neutrophils stimulated with fMLP, GM-CSF or both. Nexinhib20 has a significant anti-inflammatory activity[1].
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Nexinhib20

MCE China:Nexinhib20

Brand:MedChemExpress (MCE)

Cat. No.HY-125792

CAS:331949-35-0

Purity:99.69%

Storage:Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Nexinhib20 is an inhibitor that targets the interactions of Rab27a-JFC1 (IC50: 2.6 μM) and Rac-1-GTP. Nexinhib20 can inhibit neutrophil exocytosis, adhesion, and β2 integrin activation, and has anti-inflammatory activity. Nexinhib20 can be used in the research of diseases such as systemic inflammation and myocardial ischemia-reperfusion injury.

In Vitro:Nexinhib20 (10 μM; 1 h) can inhibit the secretion of myeloperoxidase, the production of superoxide anions, and also inhibit the upregulation of adhesion molecules and receptors, such as CD11b and CD66b in neutrophils[1]. Nexinhib20 (10 μM; 1 h) can inhibit the IL-8-induced adhesion of human neutrophils to P-selectin and ICAM-1, the exocytosis and activation of β2 integrin, as well as the intracellular calcium flux and the activation of Rac-1[2].

In Vivo:Nexinhib20 (100 mM; 10 μL; intraperitoneal injection; single dose) has a protective effect in a mouse model of myocardial I/R injury[2].

IC50 & Target:IC50: 2.6 μM (Rab27a-JFC1 interaction)[1] In Vitro Nexinhib20 (10 μM; 1 h) can inhibit the secretion of myeloperoxidase, the production of superoxide anions, and also inhibit the upregulation of adhesion molecules and receptors, such as CD11b and CD66b in neutrophils[1]. Nexinhib20 (10 μM; 1 h) can inhibit the IL-8-induced adhesion of human neutrophils to P-selectin and ICAM-1, the exocytosis and activation of β2 integrin, as well as the intracellular calcium flux and the activation of Rac-1[2]. MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> Nexinhib20 Related Antibodies

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References:

[1]. Johnson JL, et al. Identification of Neutrophil Exocytosis Inhibitors (Nexinhibs), Small Molecule Inhibitors of Neutrophil Exocytosis and Inflammation: DRUGGABILITY OF THE SMALL GTPase Rab27a. J Biol Chem. 2016 Dec 9;291(50):25965-25982.  [Content Brief]

[2]. Liu W, et al. Nexinhib20 Inhibits Neutrophil Adhesion and β2 Integrin Activation by Antagonizing Rac-1-Guanosine 5'-Triphosphate Interaction. J Immunol. 2022 Oct 15;209(8):1574-1585.  [Content Brief]

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