1. GPCR/G Protein MAPK/ERK Pathway Apoptosis Metabolic Enzyme/Protease
  2. Ras Apoptosis MMP
  3. CMC2.24

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.

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CMC2.24 Chemical Structure

CMC2.24 Chemical Structure

CAS No. : 1255639-43-0

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10 mM * 1 mL in DMSO
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Based on 1 publication(s) in Google Scholar

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Description

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)

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].

MedChemExpress (MCE) 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.
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].

MedChemExpress (MCE) 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%.
Molecular Weight

427.45

Formula

C26H21NO5

CAS No.
Appearance

Solid

Color

Light yellow to orange

SMILES

O=C(NC1=CC=CC=C1)C(C(/C=C/C2=CC=C(O)C=C2)=O)C(/C=C/C3=CC=C(O)C=C3)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light

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

Solvent & Solubility
In Vitro: 

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

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Purity & Documentation
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
CMC2.24
Cat. No.:
HY-120793
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