ARP 100
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
ARP 100是一种选择性的基质金属蛋白酶2(MMP-2)抑制剂,IC50值为12 nM[1]。
基质金属蛋白酶(MMP)家族的蛋白参与正常生理过程中细胞外基质的分解,如胚胎发育、生殖、组织重构以及疾病过程(关节炎和癌转移)。
体外实验:作为N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids的有效衍生物,在体外纤维肉瘤细胞系HT1080(过表达MMP-2和MMP-9的肿瘤细胞)侵入基质胶模型中,ARP 100具有与类似参考药物CGS27023A相似的抗侵入特性[1]。
硅片实验:ARP 100对MMP-1几乎是无活性的,这可能是由于联苯基的存在,该取代基不能与S10口袋相互作用,这一事实决定了磺酰胺基上的氧原子与Ala182和Leu181相互作用的缺失。ARP 100也是四个已分析的配体中最具选择性的配体,这一事实可能是由于大的P10基的存在,其是刚性的,不能形成H键或与MMP-1-S10口袋相互作用。该分析表明,为了保持对MMP-2/MMP-1的选择性,联苯基作为P10取代基的存在是非常有用的[2]。
临床试验:ARP 100目前正处于临床前开发阶段,没有正在进行中的临床试验。
参考文献:
[1] Rossello A, Nuti E, Orlandini E, Carelli P, Rapposelli S, Macchia M, Minutolo F, Carbonaro L, Albini A, Benelli R, Cercignani G, Murphy G, Balsamo A. New N-arylsulfonyl-N- alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg Med Chem. 2004;12(9):2441-50.
[2] Tuccinardi T, Martinelli A, Nuti E, Carelli P, Balzano F, Uccello-Barretta G, Murphy G, Rossello A. Amber force field implementation, molecular modelling study, synthesis and MMP-1/MMP-2 inhibition profile of (R)- and (S)-N-hydroxy-2-(N-isopropoxybiphenyl-4-ylsulfonamido)- 3-methylbutanamides. Bioorg Med Chem. 2006;14(12):4260-76.
- 1. Tan Ma, Yuan Zhou, et al. "Maternal exposure to di-n-butyl phthalate promotes the formation of testicular tight junctions through downregulation of NF-#B/COX-2/PGE2/MMP-2 in mouse offspring." Environ Sci Technol. 2020 Jul 7;54(13):8245-8258. PMID:32525310
- 2. Qiao, Jie, et al. "Filamin C, a dysregulated protein in cancer revealed by label-free quantitative proteomic analyses of human gastric cancer cells." Oncotarget 6.2 (2015): 1171. PMID:25577646
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 364.42 |
Cas No. | 704888-90-4 |
Formula | C17H20N2O5S |
Solubility | ≥36.4 mg/mL in DMSO |
Chemical Name | N-hydroxy-2-[(4-phenylphenyl)sulfonyl-propan-2-yloxyamino]acetamide |
SDF | Download SDF |
Canonical SMILES | CC(C)ON(CC(=O)NO)S(=O)(=O)C1=CC=C(C=C1)C2=CC=CC=C2 |
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。 |
描述 | ARP 100是一种选择性的基质金属蛋白酶2(MMP-2)抑制剂,IC50值为12 nM。 | |||||
靶点 | MMP-2 | |||||
IC50 | 12 nM |
化学结构
![ARP 100](http://www.apexbt.com//media/diy/images/struct/A4432.png)
相关生物数据
![ARP 100 ARP 100](http://www.apexbt.com/media/diy/images/wb/A4432_1.jpg)
相关生物数据
![ARP 100 ARP 100](http://www.apexbt.com/media/diy/images/wb/A4432_2.jpg)