CTS-1027
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.
CTS-1027是MMP的选择性抑制剂,对MMP-2和MMP-13的IC50值分别为0.4 nM和0.6 nM[1]。
MMPs(基质金属蛋白酶)是锌依赖性内肽酶,在降解各种胞外基质蛋白中发挥重要作用。众所周知,MMPs参与细胞膜受体的裂解、凋亡配体的释放和趋化因子/细胞因子的失活,MMPs还参与细胞的增殖、迁移、分化、血管生成、细胞凋亡和宿主防御[2] [3]。
在C57 / BL6小鼠模型中,胆管结扎(BDL)14天后,灌胃给予CTS-1027可减少肝细胞和胆管梗塞,这两者是肝损伤的组织学指标,同时活化星状细胞,降低肝纤维化[4]。
参考文献:
[1].Barta, T.E., et al., Selective, orally active MMP inhibitors with an aryl backbone. Bioorg Med Chem Lett, 2001. 11(18): p. 2481-3.
[2].Toth, M., A. Sohail, and R. Fridman, Assessment of gelatinases (MMP-2 and MMP-9) by gelatin zymography. Methods Mol Biol, 2012. 878: p. 121-35.
[3].Roomi, M.W., et al., Patterns of MMP-2 and MMP-9 expression in human cancer cell lines. Oncol Rep, 2009. 21(5): p. 1323-33.
[4].Kahraman, A., et al., Matrix metalloproteinase inhibitor, CTS-1027, attenuates liver injury and fibrosis in the bile duct-ligated mouse. Hepatol Res, 2009. 39(8): p. 805-13
.Storage | Store at -20°C |
M.Wt | 425.88 |
Cas No. | 193022-04-7 |
Formula | C19H20ClNO6S |
Synonyms | RS 130830;Ro 1130830;CTS1027;CTS 1027;RS130830;Ro1130830;RS-130830;Ro-1130830 |
Solubility | Soluble in DMSO |
Chemical Name | 4-[[4-(4-chlorophenoxy)phenyl]sulfonylmethyl]-N-hydroxyoxane-4-carboxamide |
SDF | Download SDF |
Canonical SMILES | C1COCCC1(CS(=O)(=O)C2=CC=C(C=C2)OC3=CC=C(C=C3)Cl)C(=O)NO |
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 | CTS-1027是金属蛋白酶(MMPs)的口服可利用的小分子抑制剂,对MMP-2、MMP-13和MMP-1的IC50值分别为0.4 nM、0.6 nM和800 nM。 | |||||
靶点 | MMP-2 | MMP-13 | MMP-1 | |||
IC50 | 0.4 nM | 0.6 nM | 800 nM |