Aloisine A  (Synonyms: RP107)

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].

Aloisine A ininhibits erk1 (IC₅₀=18 µM), erk2 (IC₅₀=22 µM), c-Jun N-terminal kinase (JNK; IC₅₀~3-10 µM). Aloisine A has no effect on protein kinase C α, β1, β2, γ, δ, ε, η, ξ (all IC₅₀>100 µM)^[1].
Aloisine A (0.1, 1, 10, 100 µM) completely blocks the proliferation of dividing NT2 cells (IC₅₀=7 μM) and differentiated postmitotic neurons (hNT; IC₅₀=10.5 μM), and very few cells actually die^[1].
Aloisine A acts as a submicromolar activator of wild-type (WT)-CFTR [human airway epithelial Calu-3 and WT-CFTR-Chinese hamster ovary (CHO) cells], G551D-CFTR (G551D-CFTR-CHO cells), and F508del-CFTR (in temperature-corrected human airway epithelial F508del/F508del CF15 cells)^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

267.33

C₁₆H₁₇N₃O

496864-16-5

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.  [Content Brief]