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ARP 101
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
ARP 101图片
CAS NO:849773-63-3
包装:5mg
市场价:2573元

产品介绍
ARP 101 是一种有效的选择性抑制剂基质金属蛋白酶 2 (MMP-2)。 ARP 101 在癌细胞中诱导自噬相关的细胞死亡。 ARP 101 可有效诱导自噬体的形成和 LC3I 转化为 LC3II。
Cas No.849773-63-3
化学名(R)-N-hydroxy-2-(N-isopropoxy-[1,1'-biphenyl]-4-ylsulfonamido)-3-methylbutanamide
Canonical SMILESCC(C)[C@@H](N(OC(C)C)S(=O)(C1=CC=C(C2=CC=CC=C2)C=C1)=O)C(NO)=O
分子式C20H26N2O5S
分子量406.5
溶解度<40.65mg/ml in DMSO;<10.16mg/ml in ethanol
储存条件Desiccate at 4℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ARP 101 is a selective MMP-2 inhibitor with IC50 value of 0.81nM.
MMP-2 is an enzyme and involved in the breakdown of extracellular matrix in normal physiological processes, such as embryonic development, reproduction and tissue remodeling, as well as in disease processes, such as arthritis and metastasis [1].
ARP 101 shows inhibition of fibrosarcoma HT1080 cell growth in vitro. ARP 101 has shown ~250 fold selectivity of MMP-2 over MMP-1 and ~100 fold of MMP-9 over MMP-1 [2]. ARP 101 proved to be 15.3 and 24.7 times more potent than compound a and CGS 27023A on MMP-2, maintaining a different selectivity and potency of MMP-2/MMP-1 compared with inhibitor Prinomastat and CGS 27023A [3].
Reference:
[1]. Page-McCaw A, Ewald AJ, Werb Z. Matrix metalloproteinases and the regulation of tissue remodelling. Nat Rev Mol Cell Biol, 2007, 8(3): 221-33.
[2]. Rossello A, Nuti E, Orlandini E, et al. New N-arylsulfonyl-N-alkoxyaminoacetohydroxamic acids as selective inhibitors of gelatinase A (MMP-2). Bioorg Med Chem, 2004, 12(9): 2441-50.
[3]. Tuccinardi T, Martinelli A, Nuti E, et al. 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, 2004, 14: 4260-4276.