2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Nuclear Hormone Receptor 4A/NR4A Apoptosis
  4. 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.

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Nur77 modulator 6

Nur77 modulator 6 Chemical Structure

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Nur77 modulator 6 Related Antibodies

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Description

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[1].

IC50 & Target[1]

Nur77/NR4A1

 

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.

Nur77 modulator 6 Related Antibodies

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%).
Molecular Weight

374.79

Formula

C20H14ClF3N2
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Nur77 modulator 6 Related Classifications

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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.

Keywords:

Nur77 modulator 6Nuclear Hormone Receptor 4A/NR4AApoptosisNuclear Hormone Receptor 4ANerve Growth Factor IB-like ReceptorMC38 cellscolorectal cancercyclin B1G2/M phase mitotic arrestcolorectal tumor cellsp-S10-H3Nur77-LBDHeLa cellsHCT116 cellsNur77Inhibitorinhibitorinhibit

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