基本信息

产品描述

TAPI-1 是一种ADAM17/TACE抑制剂, 其对细胞因子受体有抑制作用。

靶点（IC50 & Targe）

ADAM17/TACE [1]

体外研究

TAPI-1防止未受激的和PMA诱导的可溶性TNF-alpha，p60 TNFR，和IL-6R从单核细胞系，THP-1，以及人外周血单核细胞中释放。[1] TAPI-1抑制TACE依赖性组成型共转染APP(695)的释放。[2]在人造血干细胞系LI90中， TAPI-1减弱Ang II诱导的EGFR反式激活和细胞增殖。[3]在pSS唾液腺衍生的上皮细胞中，TAPI-1与EGFR抑制剂AG1478使AREG/EGFR/ERK信号通路失活，并减少促炎性细胞因子释放。[4]

细胞实验

Cell lines: LI90 细胞

Concentrations: 20 μM

Incubation Time: 60小时

Method: 五千个细胞接种到96孔板中，它们的活性通过CellTiter-Glo发光细胞活性测定法评估。除去血清24小时后，用每种抑制剂和拮抗剂预处理和没有预处理过的细胞用Ang II处理60小时。然后在板的每个孔中加入测定底物 ，样品使用光度计进行评估。

(Only for Reference)

参考文献

[1] Müllberg J, et al. J Immunol. 1995, 155(11), 5198-5205

[2] Slack BE, et al. Biochem J. 2001, 357(Pt 3), 787-794.

[3] Oikawa H, et al. Life Sci. 2014, 97(2), 137-144.

[4] Sisto M, et al. 2014. DOI 10.1007/s10238-014-0279-4.

安全信息

图形或危害标志
危险说明	H302 H410
防范说明	P264 P270 P273 P301+P312 P330 P391 P501
UN号码	3077
危险分类	9
包装等级	III

基本信息

分子量
499.6

产品说明

一般描述

A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α convertase; ADAM17). However, TAPI-1 is more stable in serum than TAPI-0. TAPI-1 Blocks the shedding of several cell surface proteins such as TNF-α, IL-6 receptor, and p60 and p80 TNF receptors. Inhibits constitutive (IC₅₀ = 8.09 µM) and muscarinic receptor-stimulated (IC₅₀ = 3.61 µM) sAPPa release in HEK-293 cells expressing muscarinic receptors. Also blocks the TACE-dependent constitutive release of co-transfected APP(695) (IC₅₀ = 920 nM).
A structural analog of TAPI-0 (Cat. No. 579050) with similar in vitro efficacy for the inhibition of MMPs and TACE (TNF-α converting enzyme/ADAM17). TAPI-1 also blocks the shedding of several cell surface proteins such as IL-6 receptor, p60 TNF receptor, and p80 TNF receptor. Blocks constitutive (IC₅₀ = 8.09 µM) and muscarinic receptor-stimulated (IC₅₀ = 3.61 µM) sAAPα release in HEK 293 cells expressing M3 muscarinic receptors. A 10 mM (500 µg/100 µl) solution of TAPI-1 (Cat. No. 579050) in DMSO is also available.

包装

1 mg in Plastic ampoule
Packaged under inert gas

生化/生理作用

Primary Target
MMPs and TACE
Product does not compete with ATP.
Target IC₅₀: 8.09 µM and 3.61 µM blocking constitutive and muscarinic receptor-stimulated sAAPα release in HEK 293 cells expressing M3 muscarinic receptors, respectively
Reversible: no
Cell permeable: no

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 1 month at -20°C.

其他说明

Slack, B.E., et al. 2001. Biochem. J.357, 787.
Vincent, B., et al. 2001. J. Biol. Chem.276, 37743.
Hooper, N.M., et al. 1997. Biochem. J.321, 265.
Crowe, P.D., et al. 1995. J. Exp. Med.181, 1205.
Mullberg, J., et al. 1995. J. Immunol.155, 5198.
Mohler, K.M., et al. 1994. Nature370, 218.

法律信息

Manufactured exclusively by Peptides International, Louisville, Kentucky, USA.
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

产品性质

安全信息