CMC2.24是一种口服活性的三羰基甲烷化合物,能够通过抑制 Ras 及其下游 ERK1/2 途径来抑制胰腺肿瘤的生长,同时作为锌依赖性 MMPs 的抑制剂,适用于抗癌、软骨内稳态调节及骨关节炎等疾病的研究。
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产品名称 | MMP ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Marimastat |
+++
MMP-14, IC50: 3 nM MMP-7, IC50: 16 nM |
98% | |||||||||||||||||
Ilomastat |
++++
MMP-2, Ki: 0.1 nM MMP-26, Ki: 0.36 nM |
99%+ | |||||||||||||||||
SB-3CT |
+
MMP-2, Ki: 13.9 nM MMP-9, Ki: 600 nM |
99%+ | |||||||||||||||||
Doxycycline | ✔ | 98% | |||||||||||||||||
Batimastat |
+++
MMP-7, IC50: 4 nM MMP-1, IC50: 3 nM |
99%+ | |||||||||||||||||
Nobiletin | ✔ | 98% | |||||||||||||||||
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。 |
描述 | CMC2.24 is an orally active tricarbonylmethane agent that is effective against pancreatic tumours in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs, with IC50 values ranging from 2-69 μM. CMC2.24 restores chondrogenic homeostasis via the NF-κB/HIF-2α axis and CMC2.24 can restore cartilage homeostasis through the NF-κB/HIF-2α axis and inhibit chondrocyte apoptosis, thereby alleviating the progression of osteoarthritis[1][2][3].CMC2.24 reduces p-STAT3-Ser727 levels and induces mitochondrial reactive oxygen species and mitochondrial cell death in pancreatic cancer cells. CMC2.24 induces mitochondrial reactive oxygen species and intrinsic cell apoptosis. CMC2.24 inhibits the growth of pancreatic cancer in vitro at concentrations of 0-60 μM for 24 hours[1]. |
Animal study | At a dose of 50 mg/kg, administered orally 5 times per week for 17 days, CMC2.24 inhibited the growth of pancreatic cancer xenografts. Growth was reduced by 66.9% compared to baseline[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.34mL 0.47mL 0.23mL |
11.70mL 2.34mL 1.17mL |
23.39mL 4.68mL 2.34mL |
CAS号 | 1255639-43-0 |
分子式 | C26H21NO5 |
分子量 | 427.449 |
别名 | TRB-N0224 |
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,2-8°C |
溶解度 | |
动物实验配方 |