CMC2.24(Synonyms: TRB-N0224)

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

CMC2.24 (Synonyms: TRB-N0224) 纯度: 96.48%

CMC2.24 (TRB-N0224) 是一种口服活性三羰基甲烷制剂，通过抑制 Ras 及其下游效应子 ERK1/2 途径对小鼠胰腺肿瘤有效。CMC2.24 也是一种有效的锌依赖性 MMPs 抑制剂，IC50 范围为 2.0-69 μM。CMC2.24 通过恢复软骨内稳态和通过NF-κB/HIF-2α 轴抑制软骨细胞凋亡来减轻骨关节炎的进展。

CMC2.24(Synonyms: TRB-N0224)

CMC2.24 Chemical Structure

CAS No. : 1255639-43-0

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥3300 In-stock
5 mg ￥3000 In-stock
10 mg ￥5000 In-stock
25 mg ￥9500 In-stock
50 mg ￥15500 In-stock
100 mg ￥23500 In-stock
200 mg   询价  
500 mg   询价  

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CMC2.24 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
  • Apoptosis Compound Library
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Kinase Inhibitor Library
  • Metabolism/Protease Compound Library
  • NF-κB Signaling Compound Library
  • Anti-Cancer Compound Library
  • Differentiation Inducing Compound Library
  • Ferroptosis Compound Library
  • Orally Active Compound Library
  • Glutamine Metabolism Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Anti-Blood Cancer Compound Library
  • Angiogenesis Related Compound Library
  • Anti-Liver Cancer Compound Library
  • Anti-Colorectal Cancer Compound Library

生物活性

CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor 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 IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis[1][2][3].

IC50 & Target[1][3]

RAS

 

MMP-1

69.8 μM (IC50)

MMP-2

4.8 μM (IC50)

MMP-3

2.9 μM (IC50)

MMP-7

5 μM (IC50)

MMP-8

4.5 μM (IC50)

MMP-9

8 μM (IC50)

MMP-12

2 μM (IC50)

MMP-13

2.7 μM (IC50)

MMP-14

15.3 μM (IC50)

体外研究
(In Vitro)

CMC2.24 (0-60 μM; 24 hours) inhibits pancreatic cancer growth in vitro[1].
CMC2.24 reduces STAT3Ser727 phosphorylation levels, induces mitochondrial reactive oxygen species and mitochondrial cell death in pancreatic cancer cells. CMC2.24 induces mitochondrial reactive oxygen species and intrinsic apoptosis[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: AsPC-1, Panc-1, MIA PaCa-2 and BxPC-3 PC cells
Concentration: 0-60 μM
Incubation Time: 24 hours
Result: Inhibits PC cell growth in a concentration-dependent manner.

体内研究
(In Vivo)

CMC2.24 (50 mg/kg; p.o.; five times per week during 17 days) inhibits the growth of pancreatic cancer xenografts[1].
CMC2.24 inhibits the growth of human PC through a strong cytokinetic effect. CMC2.24 inhibits ERK signaling pathway in PC cells and xenografts[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female immune deficient BALB/c nude mice[1]
Dosage: 50 mg/kg
Administration: P.o.; five times per week during 17 days
Result: Reduced the rate of growth over baseline by 66.9%.

分子量

427.45

Formula

C26H21NO5
CAS 号

1255639-43-0
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

-20°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : < 1 mg/mL (insoluble or slightly soluble)
参考文献

  • [1]. Mallangada NA, et al. A novel tricarbonylmethane agent (CMC2.24) reduces human pancreatic tumor growth in mice by targeting Ras. Mol Carcinog. 2018;57(9):1130-1143.

    [2]. Zhou Y, et al. Chemically modified curcumin (CMC2.24) alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis. J Mol Med (Berl). 2020;98(10):1479-1491.

    [3]. Zhang Y, et al. Design, synthesis and biological activity of new polyenolic inhibitors of matrix metalloproteinases: a focus on chemically-modified curcumins. Curr Med Chem. 2012;19(25):4348-4358.

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