所有图片(3)
别名:
4-[6-[4-(1-哌嗪基)苯基]吡唑并[1,5-a]嘧啶-3-基]-喹啉 盐酸盐, DM-3189
经验公式（希尔记法）:
C25H22N6 · xHCl
CAS号:
分子量:
406.48 (free base basis)
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
推荐产品
质量水平
检测方案
≥98% (HPLC)
形式
powder
储存条件
desiccated
颜色
yellow to orange
溶解性
H2O: 5 mg/mL, clear (warmed)
运输
wet ice
储存温度
−20°C
SMILES字符串
C(C=N1)(C2=CC=C(N3CCNCC3)C=C2)=CN4C1=C(C5=CC=NC6=C5C=CC=C6)C=N4.Cl
InChI
1S/C25H22N6.ClH/c1-2-4-24-22(3-1)21(9-10-27-24)23-16-29-31-17-19(15-28-25(23)31)18-5-7-20(8-6-18)30-13-11-26-12-14-30;/h1-10,15-17,26H,11-14H2;1H
InChI key
PCCDKTWDGDFRME-UHFFFAOYSA-N
应用
LDN193189盐酸盐已被用作ALK2/3（I型受体丝氨酸-苏氨酸激酶）抑制剂，用于研究TGFβ1/2/3（肿瘤生长因子β）和BMP（骨形态生成蛋白）信号传导通路对斑马鱼脊髓发育的影响。它还被用于抑制SMAD（果蝇抗生物皮肤生长因子蛋白），以防止非神经元分化。
生化/生理作用
LDN193189是Dorsomorphin的衍生物，是BMP受体ALK2和ALK3的高选择性拮抗剂（IC50：5和30 nM）。 LDN193189对ALK2/3的选择性比对TGF-B型受体ALK-4、-5和-7的选择性高200倍。 在小鼠平滑肌细胞中，该化合物能抑制BMP-4诱导的SMAD 1/5/8磷酸化，IC50 为5 nM。
尽管LDN193189是Dorsomorphin的结构类似物，但这两种药物可产生不同的细胞反应。体外分析 显示，LDN193189能够抑制许多细胞内激酶，如丝裂原活化蛋白激酶14和8（分别为p38和c-Jun N末端激酶），以及与AKT（丝氨酸/苏氨酸激酶）和mTOR（哺乳动物雷帕霉素靶标）信号传导机制相关的激酶。已知LDN193189可提高血红蛋白水平，从而有助于预防炎症性贫血的发作。
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
Oral administration of a bone morphogenetic protein type I receptor inhibitor prevents the development of anemia of inflammation.
Mayeur C, et al.
Haematologica, 100(2), e68-e71 (2015)
Differential cellular responses induced by dorsomorphin and LDN?193189 in chemotherapy?sensitive and chemotherapy?resistant human epithelial ovarian cancer cells.
Ali J L, et al.
International Journal of Cancer. Journal International Du Cancer, 136(5), E455-E469 (2015)
Misexpression of BRE gene in the developing chick neural tube affects neurulation and somitogenesis.
Guang Wang et al.
Molecular biology of the cell, 26(5), 978-992 (2015-01-09)
The brain and reproductive expression (BRE) gene is expressed in numerous adult tissues and especially in the nervous and reproductive systems. However, little is known about BRE expression in the developing embryo or about its role in embryonic development. In
Giorgia Giacomazzi et al.
Nature communications, 8(1), 1249-1249 (2017-11-03)
Muscular dystrophies (MDs) are often characterized by impairment of both skeletal and cardiac muscle. Regenerative strategies for both compartments therefore constitute a therapeutic avenue. Mesodermal iPSC-derived progenitors (MiPs) can regenerate both striated muscle types simultaneously in mice. Importantly, MiP myogenic
Ashraf Al Madhoun et al.
Stem cell research & therapy, 7(1), 165-165 (2016-11-18)
Wharton's jelly-derived mesenchymal stem cells (WJ-MSCs) are gaining increasing interest as an alternative source of stem cells for regenerative medicine applications. Definitive endoderm (DE) specification is a prerequisite for the development of vital organs such as liver and pancreas. Hence
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