Aloisine A

Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM) . Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research[1][2].

Product Specifications

CAS Number

[496864-16-5]

Product Name Alternative

RP107

UNSPSC

12352005

Hazard Statement

H302-H312-H332

Target

CDK; CFTR; ERK; GSK-3; JNK

Type

Reference compound

Related Pathways

Cell Cycle/DNA Damage; MAPK/ERK Pathway; Membrane Transporter/Ion Channel; PI3K/Akt/mTOR; Stem Cell/Wnt

Applications

COVID-19-anti-virus

Field of Research

Cancer; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/aloisine-a.html

Solubility

10 mM in DMSO

Smiles

OC1=CC=C(C2=C(CCCC)C3=NC=CN=C3N2)C=C1

Molecular Formula

C16H17N3O

Molecular Weight

267.33

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P330-P363-P501

References & Citations

[1]Yvette Mettey, et al. Aloisines, a new family of CDK/GSK-3 inhibitors. SAR study, crystal structure in complex with CDK2, enzyme selectivity, and cellular effects. J Med Chem. 2003 Jan 16;46 (2) :222-36.|[2]Sabrina Noel, et al. Discovery of pyrrolo[2,3-b]pyrazines derivatives as submicromolar affinity activators of wild type, G551D, and F508del cystic fibrosis transmembrane conductance regulator chloride channels. J Pharmacol Exp Ther. 2006 Oct;319 (1) :349-59.