TAPI-1
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.
TAPI-1是肿瘤坏死因子的抑制剂,IC50值为8.09 μM [1].
TAPI-1是TACE/ADAM17的抑制剂,能催化将全长的APP切割成可溶性N-末端片段(sAPPα).sAPPα的释放是一个受体偶联过程,由毒蕈碱受体刺激所增加.在HEK293细胞中,TAPI-1处理导致M3亚型表达诱导的sAPPα增加的抑制.TAPI-1抑制M3提高的sAPPα和组成型释放的sAPPα的IC50值分别为3.61 μM 和 8.09 μM.除了APP,TAPI-1也能够抑制TNF-α\IL6R\TNFRI和TNFRII的释放,IC50值分别为50-100\5-10\5-10和25-50 mM [1, 2].
参考文献:
[1] Slack B, Ma L, Seah C. Constitutive shedding of the amyloid precursor protein ectodomain is up-regulated by tumour necrosis factor-α converting enzyme. Biochem. J, 2001, 357: 787-794.
[2] Hooper N, Karran E, Turner A. Membrane protein secretases. Biochem. J, 1997, 321: 265-279.
- 1. Yi Zhang, Feifei Luo, et al. "Soluble NKG2D Ligands Impair CD8+ T Cell Anti-Tumor Function Dependent Of NKG2D Downregulation In The Neuroblastoma." Research Square. February 25th, 2022.
- 2. Zhang Y, Wang Y, et al. "Angiotensin Ⅱ deteriorates advanced atherosclerosis by promoting MerTK cleavage and impairing efferocytosis through AT1R/ROS/p38MAPK/ADAM17 pathway." Am J Physiol Cell Physiol. 2019 Aug 7. PMID: 31390228
- 3. Zhou J, Sun J, et al. "MicroRNA-145 overexpression attenuates apoptosis and increases matrix synthesis in nucleus pulposus cells." Life Sci. 2019 Mar 15;221:274-283. PMID: 30797016
- 4. Ellis-Connell AL, Balgeman AJ, et al. "ALT-803 transiently reduces SIV replication in the absence of antiretroviral treatment." J Virol. 2017 Nov 8. pii: JVI.01748-17. PMID: 29118125
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 499.6 |
Cas No. | 171235-71-5 |
Formula | C26H37N5O5 |
Solubility | ≥24.98 mg/mL in DMSO; ≥15.77 mg/mL in EtOH with ultrasonic; ≥18.1 mg/mL in H2O |
Chemical Name | N1-((R)-1-(((R)-1-((2-aminoethyl)amino)-1-oxopropan-2-yl)amino)-3-(naphthalen-2-yl)-1-oxopropan-2-yl)-N4-hydroxy-2-isobutylsuccinamide |
SDF | Download SDF |
Canonical SMILES | NCCNC([C@@H](C)NC([C@H](NC(C(CC(C)C)CC(NO)=O)=O)CC1=CC2=CC=CC=C2C=C1)=O)=O |
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: | |
细胞系 |
人肺粘液表皮样癌细胞系NCI-H292细胞 |
溶解方法 |
在DMSO中的溶解度>10 mM。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
30 min,30 μM [1] |
应用 |
TAPI-1是TACE(TNF-α转换酶)的抑制剂,它可以抑制TNF-α、L选择素和p55 TNF-α受体的胞外域折叠。使用TAPI-1处理细胞可抑制PMA诱导的EGFR磷酸化。除此之外,TAPI-1也可以阻断TGF-ɑ释放以及抑制PMA、绿脓杆菌上清和LPS诱导的黏蛋白的产生[1]。TAPI-1也是基质金属蛋白酶(MMP)和ADAM的抑制剂[2]。 |
References: [1]. Shao MX, Ueki IF, Nadel JA. Tumor necrosis factor alpha-converting enzyme mediates MUC5AC mucin expression in cultured human airway epithelial cells. Proc Natl Acad Sci U S A. 2003 Sep 30;100(20):11618-23. [2]. Chen CD, Podvin S, Gillespie E, Leeman SE, Abraham CR. Insulin stimulates the cleavage and release of the extracellular domain of Klotho by ADAM10 and ADAM17. Proc Natl Acad Sci U S A. 2007 Dec 11;104(50):19796-801. |
Description | TAPI-1是ADAM17/TACE的抑制剂. | |||||
靶点 | ADAM17/TACE | |||||
IC50 |
质量控制和MSDS
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