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

Aloisine A (RP107) 是一种有效的细胞周期蛋白依赖性激酶 (CDK) 抑制剂，对CDK1/cyclin B、CDK2/cyclin A、CDK2/cyclin E、CDK5/p35 的 IC50 分别为 0.15 μM、0.12 μM、0.4 μM、0.16 μM。Aloisine A 抑制 GSK-3α (IC50=0.5 μM) 和 GSK-3β (IC50=1.5 μM)。Aloisine A 通过独立于 cAMP 的机制，以亚微摩尔亲和力刺激野生型 CFTR 和突变的 CFTR。Aloisine A 具有研究 CFTR 相关疾病的潜力，包括囊性纤维化研究。

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Aloisine A Chemical Structure

Aloisine A Chemical Structure

CAS No. : 496864-16-5

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Aloisine A 相关抗体

Top Publications Citing Use of Products

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85

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GSK-3 GSK-3α GSK-3β

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ERK ERK1 ERK2 ERK5 ERK8

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JNK1 JNK2 JNK3 JNK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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)

体外研究
(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.

Aloisine A 相关抗体:
分子量

267.33

Formula

C16H17N3O
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Aloisine A 相关分类

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  • Do most proteins show cross-species activity?

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Keywords:

Aloisine A496864-16-5RP107RP 107RP-107CDKGSK-3ERKJNKCFTRCyclin dependent kinaseGlycogen synthase kinase-3Glycogen synthase kinase 3Extracellular signal regulated kinasesc-Jun N-terminal kinaseCystic fibrosis transmembrane conductance regulatorcysticfibrosisNT2postmitoticneuronshNTInhibitorinhibitorinhibit

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