ARP 100
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.
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 |