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ML347
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
ML347图片
CAS NO:1062368-49-3
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
ML347 (LDN193719) 是一种高度选择性的 ALK1/ALK2 抑制剂。 ML347 对 ALK1 和 ALK2 的 IC50 值分别为 46 和 32 nM,比 ALK3 选择性高 300 倍以上。 ML347 阻断 TGF-β1 对 Smad1/5 的磷酸化。
Cas No.1062368-49-3
别名LDN 193719
Canonical SMILESCOC1=CC=C(C=C1)C2=CN3C(=C(C=N3)C4=C5C=CC=NC5=CC=C4)N=C2
分子式C22H16N4O
分子量352.39
溶解度≥ 5.87mg/mL in DMSO with gentle warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

ML347 is a potent and selective inhibitor of bone morphogenetic protein (BMP) receptor with IC50 value of 32nM against ALK2 [1].

ML347 is discovered as a selective inhibitor of BMP type-I receptor ALK2 versus ALK3 and is identified as a probe molecule. In the in vitro kinase assay, ML347 shows potent inhibitory activities against ALK1 and ALK2 with IC50 values of 46 and 32 nM, respectively. The IC50 value of it for ALK3 is more than 10μM, demonstrating that ML347 is 300-fold more potent against ALK2. Besides that, ML347 exerts no inhibition effect on other related kinases such as ALK6 and KDR. Moreover, ML347 also shows effective inhibition with IC50 value of 152nM in the BMP4 cell based assay using C2C12BRA cells [1].

References:
[1] Engers D W, Frist A Y, Lindsley C W, et al. Synthesis and structure–activity relationships of a novel and selective bone morphogenetic protein receptor (BMP) inhibitor derived from the pyrazolo [1.5-a] pyrimidine scaffold of Dorsomorphin: The discovery of ML347 as an ALK2 versus ALK3 selective MLPCN probe. Bioorganic & medicinal chemistry letters, 2013, 23(11): 3248-3252.