Dorsomorphin 是一种选择性、ATP 竞争性的 AMPK 抑制剂 (在没有 AMP 的情况下,Ki 为 109 nM),选择性抑制 BMP I 型受体 ALK2、ALK3 和 ALK6,并可逆转 Urolithin A导致的自噬激活和抗炎作用。
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产品名称 | AMPK ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
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WZ4003 |
++++
NUAK2, IC50: 100 nM NUAK1, IC50: 20 nM |
98+% | |||||||||||||||||
Dorsomorphin |
++
AMPK, Ki: 109 nM |
99% | |||||||||||||||||
HTH-01-015 |
+++
NUAK1 , IC50: 100 nM |
99%+ | |||||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | Dorsomorphin, known as compound C, is a reversible selective ATP-competitive inhibitor of AMPK with Ki of 109 nM. Dorsomorphin can also inhibit the bone morphogenic protein (BMP) signaling and do not effect the expression of several structurally related kinases including ZAPK, SYK, PKCq, PKA, and JAK3[3]. In addition, dorsomorphin could stimulate the oxidation of long chain fatty acids independently in adipocytes by increasing carnitine palmitoyltransferase-1 (CPT1) activity[4] and remarkly reduce the adipogenic Differentiation of 3T3-L1 cells at 10 μM[5]. Compound C induces protective autophagy in cancer cells through AMPK inhibition-independent blockade of Akt/mTOR pathway[6]. In vivo, dorsomorphin induces dorsalization in zebrafish embryos and the differentiation of osteoblast[7]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
mouse C2C12 cells | 4 μM | Function assay | Inhibition of BMPR1-mediated osteoblast differentiation in BMP4-stimulated mouse C2C12 cells assessed as decrease in alkaline phosphatase level at 4 uM by spectrophotometry | 18026094 |
Dose | Mice: 3 mg/kg - 12 mg/kg[3] (i.p.) Rat: 0.2 mg/kg[4] (i.v.) |
Administration | i.p., i.v. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.50mL 0.50mL 0.25mL |
12.52mL 2.50mL 1.25mL |
25.03mL 5.01mL 2.50mL |
CAS号 | 866405-64-3 |
分子式 | C24H25N5O |
分子量 | 399.488 |
别名 | Compound C |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Room Temperature |
溶解度 |
DMSO: 35 mg/mL(87.61 mM),配合低频超声,并调节pH至2,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 1M HCl: 50 mg/mL(125.16 mM),配合低频超声,并调节pH至1 |
动物实验配方 |
IP 2% DMSO+water 0.04 mg/mL clear PO 0.5% CMC-Na 55 mg/mL suspension |