Nur77 modulator 6
Nur77 modulator 6 is a Nur77 modulator with a Kd of 0.40 μM. Nur77 modulator 6 functionally modulates Nur77 to induce mitotic arrest and apoptosis in colorectal tumor cells. Nur77 modulator 6 suppresses colorectal cancer cell proliferation via Nur77-dependent mitotic arrest induction. Nur77 modulator 6 exhibits anti-proliferative activity against colorectal tumor cells. Nur77 modulator 6 can be used for the research of colorectal cancer.
For research use only. We do not sell to patients.
- Formula: C20H14ClF3N2
- Molecular Weight:374.79
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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All Nuclear Hormone Receptor 4A/NR4A Isoforms
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Biological Activity
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Nur77/NR4A1 |
Nur77 modulator 6 (Compound a6) (0.05-2.07 μM) binds to purified Nur77-LBD protein with a dissociation constant of 0.40 μM, exhibiting stronger binding affinity than BI1071[1].
Nur77 modulator 6 (0.25-0.5 μM; 48 h) potently inhibits the proliferation of HCT116 cells with an IC50 of 0.53 μM and MC38 cells with an IC50 of 0.16 μM following 48 h incubation, exhibiting stronger anti-proliferative activity than BI1071 (HY-111837)[1].
Nur77 modulator 6 (0.125-1.0 μM; 6 h) induces dose-dependent G2/M phase mitotic arrest in HCT116 cells, with 48.60%, 74.37%, and 79.62% of cells arrested at 0.25, 0.5, and 1.0 μM respectively, and upregulates mitotic markers p-S10-H3 and cyclin B1[1].
Nur77 modulator 6 (0.25-0.5 μM; 6 h) induces dose-dependent G2/M phase mitotic arrest in MC38 cells, with 58.86% and 81.78% of cells arrested at 0.25 and 0.5 μM respectively, and upregulates mitotic markers p-S10-H3 and cyclin B1[1].
Nur77 modulator 6 (0.5 μM; 6 h) induces Nur77-dependent G2/M phase mitotic arrest in HeLa cells[1].
Nur77 modulator 6 (0.5 μM; 6-24 h) induces mitosis-dependent apoptosis in HCT116 cells, with mitotically arrested cells progressing to apoptotic cell death over 24 h of treatment[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:human HCT116 colorectal carcinoma cells, murine MC38 colon carcinoma cells
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Concentration:0.25 μM, 0.5 μM
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Incubation Time:48 h
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Result:Inhibited HCT116 cell proliferation by 33.28% at 0.25 μM.
Inhibited HCT116 cell proliferation by 51.50% at 0.5 μM.
Exhibited an IC50 of 0.53 μM for HCT116 cells and 0.16 μM for MC38 cells, both lower than the IC50 values of BI1071 in these cell lines.
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Cell Line:human HCT116 colorectal carcinoma cells
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Concentration:0.125-1.0 μM
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Incubation Time:6 h
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Result:Induced G2/M phase arrest in 79.62% of HCT116 cells at 1.0 μM.
Induced G2/M phase arrest in 74.37% of HCT116 cells at 0.5 μM.
Induced G2/M phase arrest in 48.60% of HCT116 cells at 0.25 μM.
Upregulated mitotic markers p-S10-H3 and cyclin B1 in a dose-dependent manner, with significant increases observed at 0.25 μM and 0.5 μM compared to control cells.
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Cell Line:murine MC38 colon carcinoma cells
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Concentration:0.25-0.5 μM
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Incubation Time:6 h
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Result:Induced G2/M phase arrest in 58.86% of MC38 cells at 0.25 μM.
Induced G2/M phase arrest in 81.78% of MC38 cells at 0.5 μM.
Upregulated mitotic markers p-S10-H3 and cyclin B1, with the 0.5 μM treatment causing a significant increase in p-S10-H3 levels compared to BI1071 at the same concentration.
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Cell Line:Nur77-knockdown and control HeLa cells
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Concentration:0.5 μM
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Incubation Time:6 h
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Result:Induced G2/M phase arrest in 58.13% of control siRNA-transfected HeLa cells and upregulated p-S10-H3 and cyclin B1.
Reduced the G2/M arrest rate to 34.37% in Nur77-knockdown HeLa cells and significantly suppressed the upregulation of p-S10-H3 and cyclin B1.
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Cell Line:human HCT116 colorectal carcinoma cells
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Concentration:0.5 μM
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Incubation Time:6 h, 12 h, 24 h
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Result:Caused mitotic chromosome disorganization at 6 h.
Induced cleaved caspase-3 staining (indicative of apoptosis) in a substantial number of mitotically arrested cells by 24 h.
Induced mitotic arrest and apoptosis in asynchronous cells, but these effects were abolished in G1/S-synchronized cells, confirming mitosis-dependent cell death.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:wild-type AB strain (2 hours post-fertilization)[1]
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Dosage:0.125 μM; 0.25 μM; 0.5 μM
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Administration:immersion; 24-hour exposure
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Result:Exhibited no apparent toxicity at 0.125 μM and 0.25 μM, with no significant difference in mortality compared to the control group.
Caused only 8.9% mortality at 0.5 μM, which was significantly lower than the mortality induced by the reference compound BI1071 at the same concentration (27.8%).
Chemical Information
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Molecular Weight 374.79
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Formula C20H14ClF3N2
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SMILES
FC(F)(F)C1=CC=CC([C+](C2=CNC3=C2C=CC=C3)C4=CC=CN4)=C1.[Cl-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Nur77 modulator 6 Related Classifications
HY-183758 Related Classifications
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