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FR 236924

 
Catalog No.
B7272
PKC-ε激活剂,选择性
组合的产品项目
规格价格库存 数量
1mg
¥ 981.00
Ship with 10-15 days
5mg
¥ 1,636.00
Ship with 10-15 days
10mg
¥ 2,290.00
Ship with 10-15 days
25mg
¥ 4,581.00
Ship with 10-15 days
50mg
¥ 7,854.00
Ship with 10-15 days

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A

背景

FR 236924 is a selective activator of PKC-ε [1].

PKC is a monomeric Ca2+- and phospholipid-dependent Ser/Thr protein kinase and plays an important role in growth factor-activated signaling and malignant transformation.

FR 236924 (DCP-LA) is a selective PKC-ε activator. In PC-12 cells, DCP-LA (10 nM-100 μM) activated PKC in a concentration dependent way with the maximal effect at 100 nM. In the cell-free system, DCP-LA (100 μM) significantly activated PKC-ε and exhibited >7-fold potency over other PKC isozymes (α,βI, βII, γ, δ, μ, η and ζ), suggesting that DCP-LA was a selective PKC-ε activator. DCP-LA exhibited the maximal effect on PKC-ε at 100 μM. The activation of PKC-ε induced by DCP-LA (100 μM) was inhibited by dioleoyl-phosphatidylserine in a concentration dependent way, suggesting that DCP-LA might bound to the phosphatidylserine binding site on PKC-ε. However, dioleoyl-phosphatidylserine increased DCP-LA (100 μM)-induced PKC-ε activation in a concentration dependent way, suggesting a different activation mechanism [1]. In Xenopus oocytes expressing α7 receptors, FR236924 (10 μM) induced a persistent increased α7 receptor responses to 144% via a PKC pathway. In rat hippocampal slices, FR236924 (10 nM to 10 μM) facilitated hippocampal neurotransmission [2].

In the hippocampus of rats, FR236924 induced glutamate release and facilitated hippocampal synaptic transmission through PKC [3].

References:
[1].  Kanno T, Yamamoto H, Yaguchi T, et al. The linoleic acid derivative DCP-LA selectively activates PKC-epsilon, possibly binding to the phosphatidylserine binding site. J Lipid Res, 2006, 47(6): 1146-1156.
[2].  Tanaka A, Nishizaki T. The newly synthesized linoleic acid derivative FR236924 induces a long-lasting facilitation of hippocampal neurotransmission by targeting nicotinic acetylcholine receptors. Bioorg Med Chem Lett, 2003, 13(6): 1037-1040.
[3].  Yamamoto S, Kanno T, Nagata T, et al. The linoleic acid derivative FR236924 facilitates hippocampal synaptic transmission by enhancing activity of presynaptic alpha7 acetylcholine receptors on the glutamatergic terminals. Neuroscience, 2005, 130(1): 207-213.

文献引用

化学属性

Physical AppearanceColourless oil
StorageStore at -20°C
M.Wt308.5
Cas No.28399-31-7
FormulaC20H36O2
SolubilitySoluble in DMSO
Chemical Name8-((1R,2S)-2-(((1S,2R)-2-pentylcyclopropyl)methyl)cyclopropyl)octanoic acid
SDFDownload SDF
Canonical SMILESOC(CCCCCCC[C@H]1[C@@H](C1)C[C@H]2[C@H](CCCCC)C2)=O
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质量控制

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批次:

化学结构

FR 236924

相关生物数据

FR 236924