1. MAPK/ERK Pathway Metabolic Enzyme/Protease Stem Cell/Wnt Immunology/Inflammation NF-κB Apoptosis
  2. Raf HIF/HIF Prolyl-Hydroxylase ERK MEK Reactive Oxygen Species (ROS) Apoptosis Caspase
  3. MO-2097

MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer.

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MO-2097 Chemical Structure

MO-2097 Chemical Structure

CAS No. : 2744300-63-6

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Description

MO-2097 is a RAF-1/HIF-1α inhibitor. MO-2097 induces RAF-1 destabilization, leading to a reduction in EMT-associated transcription factors and mesenchymal markers. MO-2097 inhibits HIF-1a protein expression mediated by hnRNPA2B1 under hypoxic and mimetic hypoxia. MO-2097 induces mitochondrial ROS, which leads to apoptosis in cells. MO-2097 effectively suppresses colorectal cancer metastasis by inhibiting the RAF/MEK/ERK signaling pathway. MO-2097 attenuates tumor growth in a xenograft HCT116 cell mouse model. MO-2097 can be used for the study of colorectal cancer[1][2].

In Vitro

MO-2097 (10-30 μM, 24-48 h) suppresses cell migration in DLD-1 cells and HCT116 cells[1].
MO-2097 (10-50 μM, 1-6 h) inhibits the RAF/MEK/ERK cascade driven by RAF-1 in DLD-1 cells and HCT116 cells[1].
MO-2097 (10-30 μM, 5-9 days) inhibits the invasiveness of colorectal cancer cells (DLD-1 cells and HCT116 cells) in a 3D tumor spheroid[1].
MO-2097 (30-100 μM, 4 h) inhibits angiogenesis by suppressing tube formation in HUVECs[1].
MO-2097 (25-500 μM, 24 h) exhibits low toxicity, directly binds to hnRNPA2B1, and suppresses HIF-1a expression in HeLa CCL2 cells and HCT116 cells[2].
MO-2097 (25-50 μM, 24 h) inhibits the HIF-1a target gene mRNA (HK1, MRP1, SLC1A5, IL-6, and VEGF) expression levels in HeLa CCL2 cells and HCT116 cells under hypoxic conditions[2].
MO-2097 (12.5-50 μM, 24 h) induces mitochondrial ROS, which leads to apoptosis, as shown by cleaved caspase 3 and 9 in HeLa CCL2 cells[2].
MO-2097 (12.5-50 μM, 7-10 days) induces a specific anticancer effect in the hypoxic zone of the 3D culture spheroid model and 3D-cultured human colon cancer organoids[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Migration Assay [1]

Cell Line: DLD-1 and HCT116 cells
Concentration: 10, 20, 30 μM
Incubation Time: 24, 48 h
Result: Suppressed cell migration at 86.5% and 77.5% in DLD-1 cells and HCT116 cells, relative to the control, respectively.

Western Blot Analysis[1]

Cell Line: DLD-1 and HCT116 cells
Concentration: 10, 20, 30, 40, 50 μM
Incubation Time: 1, 2, 4, 6 h
Result: Decreased RAF-1 levels gradually in Cycloheximide (CHX) (HY-12320)-only treated cells.
Prevented RAF-1 accumulation without influencing the proteasomal degradation process.
Reduced the phosphorylation of MEK and ERK.
Decreased the levels of transcription factors Snail, Slug and ZEB1.

Immunofluorescence[2]

Cell Line: HeLa CCL2 cells
Concentration: 12.5, 25, 50 μM
Incubation Time: 24 h
Result: Decreased the amount of HIF-1a protein in the nucleus in a dose-dependent manner under hypoxic conditions.
Induced mitochondrial ROS.

Real Time qPCR[2]

Cell Line: HeLa CCL2 cells and HCT116 cells
Concentration: 25, 50 μM
Incubation Time: 24 h
Result: Inhibited HK1, MRP1, SLC1A5, IL-6, and VEGF expression levels in HeLa CCL2 cells and HCT116 cells under hypoxic conditions.
In Vivo

MO-2097 (25-50 mg/kg, i.p., every other day, 15 days) attenuates tumor growth in a xenograft HCT116 cell mouse model by inducing tumor apoptosis via HIF-1a expression suppression[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male Balb/C nude mice (6 weeks) xenografted HCT116 cells (2 × 105 cells/mouse)[1]
Dosage: 25, 50 mg/kg
Administration: i.p. every other day for 15 days
Result: Reduced the embedded tumor volume by approximately 49 % without any considerable body weight loss.
Decreased HIF-1a expression.
Increased expression of cleaved caspase 3.
Molecular Weight

308.33

Formula

C19H16O4

CAS No.
SMILES

OC1=CC(C2=CC3=C(C=C4OCC(C)=CCC4=C3)O2)=CC(O)=C1

Structure Classification
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MO-2097
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