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product name
LDN193189 盐酸盐, ≥98% (HPLC)
品質等級
化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
yellow to orange
溶解度
H2O: 5 mg/mL, clear (warmed)
運輸包裝
wet ice
儲存溫度
−20°C
SMILES 字串
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 密鑰
PCCDKTWDGDFRME-UHFFFAOYSA-N
應用
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。
準備報告
The product is water soluble at a minimum of 5 mg/mL.
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 3
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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