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化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 1 mg/mL, clear (warmed)
儲存溫度
2-8°C
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 密鑰
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。
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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