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Cat. No.: HY-183758

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Nur77 modulator 6

Nur77 modulator 6 is a Nur77 modulator with a K_d 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.

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Formule: C₂₀H₁₄ClF₃N₂
Masse moléculaire:374.79

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Please store the product under the recommended conditions in the Certificate of Analysis.

Nur77 modulator 6 Chemical Structure

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
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- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
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Activité biologique

Description

IC₅₀ & Target

^[1]

Nur77/NR4A1

Voir tous les produits spécifiques à Isoform Nuclear Hormone Receptor 4A/NR4A :

In Vitro

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.

Cell Proliferation Assay^[1]

Cell Line:

human HCT116 colorectal carcinoma cells, murine MC38 colon carcinoma cells
Concentration:

0.25 μM, 0.5 μM
Incubation Time:

48 h
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.

Cell Cycle Analysis^[1]

Cell Line:

human HCT116 colorectal carcinoma cells
Concentration:

0.125-1.0 μM
Incubation Time:

6 h
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.

Cell Cycle Analysis^[1]

Cell Line:

murine MC38 colon carcinoma cells
Concentration:

0.25-0.5 μM
Incubation Time:

6 h
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.

Cell Cycle Analysis^[1]

Cell Line:

Nur77-knockdown and control HeLa cells
Concentration:

0.5 μM
Incubation Time:

6 h
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.

Apoptosis Analysis^[1]

Cell Line:

human HCT116 colorectal carcinoma cells
Concentration:

0.5 μM
Incubation Time:

6 h, 12 h, 24 h
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.

In Vivo

Nur77 modulator 6 (Compound a6) (0.125-0.5 μM; 24 h) shows low embryonic toxicity in zebrafish, with 8.9% mortality at the highest tested dose of 0.5 μM, which is substantially lower than the toxicity of BI1071^[1].

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

Animal Model:

wild-type AB strain (2 hours post-fertilization)^[1]
Dosage:

0.125 μM; 0.25 μM; 0.5 μM
Administration:

immersion; 24-hour exposure
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%).

Related Protocols :

Chemical Information

Masse moléculaire 374.79
Formule C₂₀H₁₄ClF₃N₂
SMILES

FC(F)(F)C1=CC=CC([C+](C2=CNC3=C2C=CC=C3)C4=CC=CN4)=C1.[Cl-]
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

Please store the product under the recommended conditions in the Certificate of Analysis.

Pureté et documentation

Instruction de manipulation (2659 KB)

Références

[1]. Zhao Q, et al. Design, synthesis and structure-activity relationship study of novel indole-pyrrole scaffold compounds targeting Nur77 in colorectal tumor cells. Eur J Med Chem. 2026;314:118927. [Content Brief]

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Nur77 modulator 6

Voir tous les produits spécifiques à Isoform Nuclear Hormone Receptor 4A/NR4A

Activité biologique

Description

IC50 & Target

In Vitro

In Vivo

Chemical Information

Pureté et documentation

Références

Calculators

Help & FAQs