Selonsertib (GS-4997)
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.
Selonsertib(GS-4997)是凋亡信号调节激酶1(ASK1)抑制剂。
ASK1是氧化还原敏感性促分裂原活化蛋白激酶激酶激酶,通过促进有害作用作为关键的信号传导节点。ASK1激活可引起末端MAPK激酶p38和c-Jun N端激酶的下游激活,其刺激炎症细胞因子的产生、诱导纤维化、促进凋亡和坏死性细胞死亡、增加异常细胞增殖,以及引起代谢扰动。
体外:GS-4997已被确定为一种高选择性的和强效的ASK1抑制剂,与ASK1催化激酶结构域中的ATP竞争。此外,研究发现GS-4997引起的ASK1抑制在机制上与bardoxolone methyl显著不同。GS-4997还可以关闭参与发病机制的细胞信号传导,而bardoxolone methyl激活每个暴露于药物的细胞中的mRNA转录。此外,GS-4997可以选择性靶向氧化负荷高的受影响细胞[1]。
体内:迄今为止,尚无动物体内数据发布。
临床试验:基于通过ASK1的氧化应激信号传导的生物学、DKD发病机理的生物学,以及立体统计方法设计了关于描述研究人群、功效结果、治疗期以及用于解决DKD研究的特定挑战的统计方法的II期研究[1]。
参考文献:
[1] Lin JH et al. Design of a phase 2 clinical trial of an ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease. Nephron. 2015;129(1):29-33.
- 1. Guofeng Xu, Shuang Liu, et al. "Cadmium induces apoptosis of human granulosa cell line KGN via mitochondrial dysfunction-mediated pathways." Ecotoxicol Environ Saf. 2021 Sep 1;220:112341. PMID:34020281
- 2. Mingquan Huang, Xingjie Li, et al. "Bisphenol AF induces apoptosis via estrogen receptor beta (ERβ) and ROS-ASK1-JNK MAPK pathway in human granulosa cell line KGN." Environ Pollut. 2020 Nov 9;116051. PMID:33189448
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 445.49 |
Cas No. | 1448428-04-3 |
Formula | C24H24FN7O |
Solubility | ≥44.5 mg/mL in DMSO; insoluble in H2O; ≥88.8 mg/mL in EtOH |
Chemical Name | 5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-4-methylbenzamide |
SDF | Download SDF |
Canonical SMILES | O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F |
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。 |
质量控制和MSDS
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