Gap 26
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Gap26 (Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg)是一种连接蛋白模拟肽，对应于connexin 43的63-75 aa，是间隙连接的阻断肽。
连接蛋白或间隙连接是一个结构相关的转膜蛋白家族。间隙连接包含允许离子和小分子穿过相邻细胞的通道。钙和磷酸肌醇是可以穿过间隙连接通道的第二信使[1]。据报道，gap26可以衰减兔动脉平滑肌的节律收缩活动，IC50值为28.4 mM。Gap26也可以阻断IP3诱导的ATP和Ca2+穿过连接蛋白半通道，即六聚通道，与相邻细胞对接从而形成间隙连接的管道[2]。
Fig. 1: Formula of Gap26
Fig. 2: Function of Gap26.
参考文献：
1. Boitano, S. and H. Evans Am. J. Physiol. Lung Cell Mol. Physiol. 279, L623 (2000).
2. T. Desplantez, V. Verma, L. Leybaert, W.H. Evans, R. Weingart, Gap26, a connexin mimetic peptide, inhibits currents carried by connexin43 hemichannels and gap junction channels, Pharmacological Research, Volume 65, Issue 5, May 2012, Pages 546-552.
- 1. Chenyu Liang, Qian Zhang, et al. "Human cancer cells generate spontaneous calcium transients and intercellular waves that modulate tumor growth." Biomaterials. 2022 Oct 5;290:121823. PMID: 36209577
- 2. Xuqing Qin, Wenjun He, et al. "Inhibition of Connexin 43 reverses ox-LDL-mediated inhibition of autophagy in VSMC by inhibiting the PI3K/Akt/mTOR signaling pathway." PeerJ. 2022 Mar 16;10:e12969. PMID: 35313522
- 3. Guo-Li Zhao, Hong Zhou, et al. "Modulation of Rac1/PAK1/connexin43-Mediated ATP Release from Astrocytes Contributes to Retinal Ganglion Cell Survival in Experimental Glaucoma." Research Square. rs-770147/v1.
- 4. Rui-Juan Gao, Ai-Mei Zhang, et al. "The promoting role of Cx43 on the proliferation and migration of arterial smooth muscle cells for angiotensin II-dependent hypertension." Pulm Pharmacol Ther. 2021 Oct;70:102072. PMID: 34428599
- 5. Zhou Z, Ni J, et al. "Angiotensin II induces RAW264. 7 macrophage polarization to the M1-type through the connexin 43/NF-κB pathway." Mol Med Rep. 2020;21(5):2103-2112. PMID: 32186758
- 6. Steven Condamine. "Organisation anatomique et rôle du couplage astrocytaire dans l’activité rythmique du noyau sensoriel du trijumeau." Université de Montréal. 2019.
- 7. Wang M, Wu Y, et al. "Rutaecarpine prevented ox-LDL-induced VSMCs dysfunction through inhibiting overexpression of connexin 43." Eur J Pharmacol. 2019 Jun 15;853:84-92. PMID: 30880182
- 8. Mederos S, Hernández-Vivanco A, et al. "Melanopsin for precise optogenetic activation of astrocyte-neuron networks." Glia. 2019 Jan 11. PMID: 30632636
- 9. Zhang X, Chen D, et al. "Involvement of sphingosine-1-phosphate receptors 2/3 in IR-induced sudden cardiac death." Heart Vessels. 2019 Jan 2. PMID: 30604190
- 10. Condamine S, Lavoie R, et al. "Functional Rhythmogenic Domains Defined by Astrocytic Networks in the Trigeminal Main Sensory Nucleus." Glia. 2017 Oct 23. PMID: 29058348
- 11. Yang G, Peng X, et al. "Involvement of connexin 43 phosphorylation and gap junctional communication between smooth muscle cells in vasopressin-induced ROCK-dependent vasoconstriction after hemorrhagic shock." Am J Physiol Cell Physiol. 2017 Oct 1;313(4):C362-C370. PMID: 28974518
- 12. Li X, Jiang S, et al. "Breakthrough Cancer Pain Is Associated with Spinal Gap Junction Activation via Regulation of Connexin 43 in a Mouse Model." Front Cell Neurosci. 2017 Jul 17;11:207. PMID: 28769766
- 13. Chu H, Huang C, et al. "Reduction of Ischemic Brain Edema by Combined use of Paeoniflorin and Astragaloside IV via Down-Regulating Connexin 43." Phytother Res. 2017 Jul 28. PMID: 28752625
- 14. Zhou, Ziyi, et al. "Protection of erythropoietin against ischemic neurovascular unit injuries through the effects of connexin43." Biochemical and biophysical research communications 458.3 (2015): 656-662. PMID: 25684187
| Physical Appearance | A solid |
| Storage | Desiccate at -20°C |
| M.Wt | 1550.79 |
| Cas No. | 197250-15-0 |
| Formula | C70H107N19O19S |
| Synonyms | Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg |
| Solubility | insoluble in EtOH; ≥155.1 mg/mL in H2O with ultrasonic; ≥77.55 mg/mL in DMSO with gentle warming and ultrasonic |
| SDF | Download SDF |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
| 细胞实验[1]： | |
|
细胞系 |
ECV304细胞 |
|
溶解方法 |
在无菌水中的溶解度>10 mM。原液应分装，在-80℃以下可储存几个月。 |
|
反应条件 |
0.25 mg/ml；30 min |
|
应用 |
钙螯合剂BAPTA阻止InsP3触发的钙增加，减少InsP3触发的ATP释放至对照水平。Gap 26与细胞孵育后完全阻断InsP3触发的ATP释放，使ATP释放下降到对照水平以下，表明基底ATP释放也受到影响。 |
| 动物实验[2]： | |
|
动物模型 |
雌性Sprague-Dawley大鼠 |
|
剂量 |
300 μM；45 min |
|
应用 |
在实验前24小时，大鼠安装脑颅窗。在颅骨中线进行10 mm直径的开颅手术，小心移除硬脑膜以保持矢状窦完好，配备三个端口的11 mm直径玻璃窗口用氰基丙烯酸酯胶合在头骨上，缝合覆盖在窗口上的皮肤，使动物恢复。在实验当天，三个不锈钢螺丝沿着脑颅窗的边缘插入头骨，用于脑电图（EEG）记录，然后将插管与三个端口连接。大鼠用于两个神经元激活模型之一：SNS或bicuculline诱导的癫痫发作。在SNS或bicuculline暴露期间测量软脑膜小动脉直径的变化。20 min后，gap-26开始扩散，45 min后，神经元再次被激活。Cx40/Cx37的抑制肽gap-26（300 μM）对bicuculline或SNS诱导的软脑膜小动脉扩张没有影响。 |
|
注意事项 |
请测试所有化合物在室内的溶解度，实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的，属于正常现象。 |
|
References: [1] Braet K, Vandamme W, Martin P E M, et al. Photoliberating inositol-1, 4, 5-trisphosphate triggers ATP release that is blocked by the connexin mimetic peptide gap 26. Cell calcium, 2003, 33(1): 37-48. [2] Xu H L, Mao L, Ye S, et al. Astrocytes are a key conduit for upstream signaling of vasodilation during cerebral cortical neuronal activation in vivo. American Journal of Physiology-Heart and Circulatory Physiology, 2008, 294(2): H622-H632. |
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| Description | Gap26 (Val-Cys-Tyr-Asp-Lys-Ser-Phe-Pro-Ile-Ser-His-Val-Arg)是一种连接蛋白模拟肽，对应于connexin 43的63-75 aa，是间隙连接的阻断肽。 | |||||
| Targets | ||||||
| IC50 | ||||||
质量控制和MSDS
- 批次:
化学结构
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