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- 保存条件:
4℃保存
- 保质期:
6个月
- 英文名:
ALK5 Inhibitor
- 库存:
1
- 供应商:
上海信裕
产品描述
ALK5 Inhibitor (RepSox) 是一种细胞渗透性的,ATP竞争的ALK5抑制剂,其IC50为23 nM。ALK5 Inhibitor能阻止ALK5自体磷酸化,IC50为4 nM [1]。RepSox能够在细胞重编程中通过抑制广泛表达的转化生长因子-β(Tgf-β)信号,从而取代Sox2,进而导致Nanog的持续表达,实现无Sox2的细胞重编程 [2]。ALK5 Inhibitor能通过抑制Tgf-β减少Tim-3的表达,并能通过增加抑制AML分化的CXCL12和MYC而减缓CD34(+) AML细胞的衰退[3]。ALK5 Inhibitor产生iPSCs仅需要转入Oct4和Klf4两个因子,成功取代Sox2和c-Myc。在处理被困在部分重新编程状态的稳定中间体细胞(过表达Oct4,Klf5和c-Myc细胞)时,ALK5 Inhibitor被认为是产生iPSCs最有效的小分子 [4]。靶点
| 靶点 | ALK5 |
| IC50(半数有效浓度) | 4 nM [1] |
ALK5 Inhibitor化学特性
| Cas No.: 446859-33-2 | 分子量: 287.32 |
| 分子式: C17H13N5 | 纯度: ≥98% |
| 同义名: RepSox, ALK5 Inhibitor II,E-616452, SJN 2511 | |
| 化学名: 2-[5-(6-methylpyridin-2-yl)-1H-pyrazol-4-yl]-1,5-naphthyridine | |
| 外观: 灰白色固体 | |
| 溶解: 溶于DMSO (up to 100 mM) | |
| 保存::3年 -20℃粉状 | |
储存液配制
| 储存液 (1 ml DMSO体系) | 1 mM | 5 mM | 10 mM | 25 mM | 50 mM | 100 mM |
| 质量(mg) | 0.2873 | 1.4366 | 2.8732 | 7.1830 | 14.3660 | 28.7320 |
ALK5 Inhibitor结构式
参考文献
[1] Gellibert F, et al. Identification of 1,5-naphthyridine derivatives as a novel series of potent and selective TGF-beta type I receptor inhibitors. J Med Chem. 47(18):4494-506(2004).[2] Ichida JK, et al. A small-molecule inhibitor of tgf-Beta signaling replaces sox2 in reprogramming by inducing nanog. Cell Stem Cell.;5(5):491-503(2009).
[3] Jajosky AN, et al. RepSox slows decay of CD34+ acute myeloid leukemia cells and decreases T cell immunoglobulin mucin-3 expression. Stem Cells Transl Med. 3(7):836-48(2014).
[4] Solanki A, Lee KB. A step closer to complete chemical reprogramming for generating iPS cells. Chembiochem.11 (6):755-7(2010).
ALK5 Inhibitor
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文献和实验Similar to the trypsin inhibitor, the chymotrypsin inhibitor also decreases protein degradability in the intestine, resulting in lower availability of amino acids and peptides for production purposes. This adversely affects growth
city directed primarily toward trypsin (Kunitz inhibitor), and (2) those that have a molecular weight of only 6000 to 10,000 Da with a high proportion of cystine residues and are capable of inhibiting chymotrypsin as well as trypsin at independent
-amylases of diverse origin. Three major groups of α-amylase have been characterized, based on molecular weight: 60,000, 24,000, and 12,500 Da. The inhibitor forms a complex with amylase. The complex formation can inactivate the amylase and in turn cause
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