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

Aloisine A Chemical Structure

CAS No. : 496864-16-5

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规格 价格 是否有货 数量
5 mg ￥3550
3 - 4 周
10 mg ￥4980
3 - 4 周
50 mg   询价  
100 mg   询价  

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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 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

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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)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
150 nM
Compound: K00059, Aloisine
Activity at human wild type CFTR expressed in CHO cells assessed as forskolin stimulated iodide flux
Activity at human wild type CFTR expressed in CHO cells assessed as forskolin stimulated iodide flux
[PMID: 18077363]
Calu-3 EC50
140 nM
Compound: K00059, Aloisine
Activity at human wild type CFTR expressed in Calu3 cells assessed as forskolin stimulated iodide flux
Activity at human wild type CFTR expressed in Calu3 cells assessed as forskolin stimulated iodide flux
[PMID: 18077363]
NT2 IC50
10500 nM
Compound: K00059, Aloisine
Cell cycle arrest in human NT2 cells assessed as accumulation at G2 phase
Cell cycle arrest in human NT2 cells assessed as accumulation at G2 phase
[PMID: 18077363]
NT2 IC50
7000 nM
Compound: K00059, Aloisine
Cell cycle arrest in human NT2 cells assessed as accumulation at G1 phase
Cell cycle arrest in human NT2 cells assessed as accumulation at G1 phase
[PMID: 18077363]
Sf9 IC50
0.65 μM
Compound: 39
Inhibition of glycogen synthase kinase-3 beta, purified from porcine brain or expressed in and purified from insect Sf9 cells
Inhibition of glycogen synthase kinase-3 beta, purified from porcine brain or expressed in and purified from insect Sf9 cells
[PMID: 12519061]
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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  • 稀释计算器

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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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