推荐产品
质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 1 mg/mL, clear (warmed)
储存温度
2-8°C
SMILES字符串
[n]21ncc(c2ncc(c1)c5ccc(cc5)N6CCNCC6)c3c4c(nccc4)ccc3
InChI
1S/C25H22N6/c1-3-21(22-4-2-10-27-24(22)5-1)23-16-29-31-17-19(15-28-25(23)31)18-6-8-20(9-7-18)30-13-11-26-12-14-30/h1-10,15-17,26H,11-14H2
InChI key
BBDGBGOVJPEFBT-UHFFFAOYSA-N
生化/生理作用
LDN-212854 也称为 5- [6- [4-（1-哌嗪基）苯基]吡唑并[1,5-a]嘧啶-3-基]-喹啉。LDN-212854 可防止诱导型突变体 ALK2（激活素受体样激酶 2）中的异位骨化。
LDN-212854 是骨形态发生蛋白（BMP）I 型受体激酶的选择性和有效抑制剂，与密切相关的 TGF-β 和激活素 I 型受体相比，对 BMP 的选择性超过 5,000倍。LDN-212854 对 ALK2 具有某些选择性，IC50 为 1.3 nM，优于其他 BMP I 型受体 ALK1（IC50 = 2.4 nM）和 ALK3（IC50 = 85.8 nM）。 在基于细胞的 BMP 信号试验中，LDN-212854 显示出比 LDN193189 更好的选择性。 LDN-212854 抑制 BMP6 诱导的成骨分化（主要通过 ALK2 起作用），而抑制 BMP4 诱导的分化（主要通过 ALK3 起作用）的效能相对较弱，IC50 分别为 10 nM 和 40.5 nM，而 LDN-193189 两者都抑制。针对 198 种激酶的仅有脱靶效应是针对 RIPK2、ABL1 和 PDGFR-β，IC50 值为 <100 nM。
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
从最新的版本中选择一种：
分析证书(COA)
Lot/Batch Number
The Inhibitor Index: A Desk Reference on Enzyme Inhibitors, Receptor Antagonists, Drugs, Toxins, Poisons, Biologics, and Therapeutic Leads (2017)
Hongen Yin et al.
Scientific reports, 10(1), 2967-2967 (2020-02-23)
Primary Sjögren's syndrome (pSS) is a chronic autoimmune disease, with only palliative treatments available. Recent work has suggested that increased bone morphogenetic protein 6 (BMP6) expression could alter cell signaling in the salivary gland (SG) and result in the associated
Huili Zhang et al.
American journal of physiology. Lung cellular and molecular physiology, 313(3), L615-L627 (2017-06-24)
The intracellular signaling mechanisms through which TGF-β regulates pulmonary development are incompletely understood. Canonical TGF-β signaling involves Smad2/3 phosphorylation, Smad2/3·Smad4 complex formation and nuclear localization, and gene regulation. Here, we show that physiologically relevant TGF-β1 levels also stimulate Smad1/5 phosphorylation
Leiming Wang et al.
The Journal of clinical investigation, 130(4), 1782-1792 (2019-12-25)
Recent findings have shown that inhibitors targeting bromodomain and extraterminal domain (BET) proteins, such as the small molecule JQ1, are potent growth inhibitors of many cancers and hold promise for cancer therapy. However, some reports have also revealed that JQ1
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