1. Cell Cycle/DNA Damage
    Stem Cell/Wnt
    PI3K/Akt/mTOR
    MAPK/ERK Pathway
    Membrane Transporter/Ion Channel
  2. CDK
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    ERK
    JNK
    CFTR
  3. Aloisine A

Aloisine A (Synonyms: RP107)

Cat. No.: HY-112363
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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.

For research use only. We do not sell to patients.

Aloisine A Chemical Structure

Aloisine A Chemical Structure

CAS No. : 496864-16-5

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Description

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].

IC50 & Target[1]

CDK1/cyclinB

0.15 μM (IC50)

CDK2/cyclinA

0.12 μM (IC50)

CDK2/cyclinE

0.4 μM (IC50)

CDK5/p35

0.16 μM (IC50)

GSK-3β

0.5 μM (IC50)

GSK-3α

1.5 μM (IC50)

JNK

3-10 μM (IC50)

ERK1

18 μM (IC50)

ERK2

22 μM (IC50)

In Vitro

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].

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

Molecular Weight

267.33

Formula

C₁₆H₁₇N₃O

CAS No.
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