2. Vitamin D Related/Nuclear Receptor Apoptosis Epigenetics Cell Cycle/DNA Damage
  3. Nuclear Hormone Receptor 4A/NR4A Apoptosis PARP
  4. Nur77 modulator 5

Nur77 modulator 5 is a Nur77 modulator. Nur77 modulator 5 induces lysosomal dysfunction, impaired autophagic flux, and apoptosis with increased PARP cleavage, TUNEL positivity, and Annexin V/PI staining. Nur77 modulator 5 can be used for the research of gastric cancer.

For research use only. We do not sell to patients.

Nur77 modulator 5

Nur77 modulator 5 Chemical Structure

CAS No. : 3068830-45-2

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Nur77 modulator 5 Related Antibodies

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Nur77/NR4A1 Nurr1/NR4A2

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PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

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Description

Nur77 modulator 5 is a Nur77 modulator. Nur77 modulator 5 induces lysosomal dysfunction, impaired autophagic flux, and apoptosis with increased PARP cleavage, TUNEL positivity, and Annexin V/PI staining. Nur77 modulator 5 can be used for the research of gastric cancer[1].

IC50 & Target[1]

Nur77/NR4A1

 

In Vitro

Nur77 modulator 5 (Compound 6K) binds directly to the Nur77 ligand-binding domain with an equilibrium dissociation constant (KD) of 0.62 μM, forming stable hydrogen bonds, π-π stacking, and hydrophobic interactions with key residues in the binding pocket[1].
Nur77 modulator 5 (48 h) potently inhibits the growth of multiple human cancer cell lines (most potently HGC-27 gastric cancer cells with an IC50 of 0.53 μM) and exhibits minimal cytotoxicity toward normal GES-1 gastric epithelial cells (IC50 = 24.33 μM)[1].
Nur77 modulator 5 (24-48 h) reduces viability of HGC-27 and AGS gastric cancer cells in a time-dependent manner, with greater potency against HGC-27 cells (IC50 = 1.51 μM) than AGS cells (IC50 = 3.40 μM)[1].
Nur77 modulator 5 (2.5-5 μM; ~2 weeks) inhibits clonogenic survival of HGC-27 and AGS gastric cancer cells in a concentration-dependent manner, with more pronounced effects in HGC-27 cells[1].
Nur77 modulator 5 (4 μM; 5 h) induces prominent cytoplasmic vacuolization in HGC-27 and AGS gastric cancer cells[1].
Nur77 modulator 5 (1.25-5 μM; 24 h) induces apoptosis in HGC-27 gastric cancer cells[1].
Nur77 modulator 5 (0.625-4 μM; 5 h-2 weeks) induces lysosomal dysfunction and impaired autophagic flux in HGC-27 gastric cancer cells, as evidenced by increased LC3-II/p62 levels, reduced Lyso-Tracker fluorescence, and attenuation of vacuolization and growth inhibition by Bafilomycin A1 (HY-100558)[1].
Nur77 modulator 5 (0.625-4 μM; 12 h-2 weeks) reduces Nur77 protein levels in HGC-27 gastric cancer cells in a dose-dependent manner, and Nur77 overexpression attenuates Nur77 modulator 5-induced lysosomal dysfunction, apoptotic signaling, and growth inhibition[1].

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

Nur77 modulator 5 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: human gastric cancer cell lines (HGC-27, AGS)
Concentration: 2.5 μM; 5 μM
Incubation Time: ~2 weeks
Result: Reduced both the size and number of colonies in a concentration-dependent manner.
Caused significant reductions in colony number in HGC-27 cells.
Caused a significant reduction in colony number in AGS cells at 5 μM.

Apoptosis Analysis[1]

Cell Line: human gastric cancer cell line (HGC-27)
Concentration: 1.25 μM; 2.5 μM; 4 μM; 5 μM
Incubation Time: 24 h
Result: Enhanced PARP cleavage in a dose-dependent manner.
Increased the number of TUNEL-positive cells.
Elevated the percentage of apoptotic cells in a dose-dependent manner, as measured by Annexin V/PI staining.

Western Blot Analysis[1]

Cell Line: human gastric cancer cell line (HGC-27)
Concentration: 0.625 μM; 1.25 μM; 2.5 μM
Incubation Time: 24 h
Result: Increased LC3-II and p62 levels in a dose-dependent manner.

Western Blot Analysis[1]

Cell Line: Nur77-overexpressing human gastric cancer cell line (HGC-27)
Concentration: 0.625 μM; 1.25 μM; 2.5 μM; 4 μM
Incubation Time: 12 h; 24 h
Result: Reduced Nur77 protein levels in a dose-dependent manner.
Restored CTSB, LAMP2, LC3, p62, and cleaved PARP, and partially restored clonogenic growth when Nur77 was overexpressed.
In Vivo

Nur77 modulator 5 (Compound 6K) (20 mg/kg; i.p.; once every 3 days; 24 days) significantly suppresses HGC-27 gastric cancer xenograft growth without apparent systemic toxicity[1].

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

Animal Model: BALB/c nude (male, 16-20 g at purchase, subcutaneous xenograft via HGC-27 cell injection to form a xenograft model)[1]
Dosage: 20 mg/kg
Administration: i.p.; once every 3 days; 24 days
Result: Markedly inhibited tumor growth, with endpoint tumor volumes significantly lower than the vehicle control.
Significantly reduced endpoint tumor weights compared to the vehicle control.
Elevated levels of Nur77, CTSB, p62, and LC3 in tumor tissues via immunohistochemistry.
Showed no significant histopathological changes in major organs (heart, liver, spleen, lung, kidney) via hematoxylin and eosin staining.
Molecular Weight

461.36

Formula

C21H18Cl2N4O2S
CAS No.
SMILES

COC1=CC=C(C=C1)C2=CC=C(C(C)=N2)C(NNC(NC3=CC=C(C(Cl)=C3)Cl)=S)=O
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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 5 Related Classifications

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  • Do most proteins show cross-species activity?

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Keywords:

Nur77 modulator 53068830-45-2Nuclear Hormone Receptor 4A/NR4AApoptosisPARPNuclear Hormone Receptor 4ANerve Growth Factor IB-like Receptorpoly ADP ribose polymerasenormal gastric epithelial cellsGES-1Nur77 ligand-binding domainlysosomal dysfunctionAGSxenograft mouse modelgastric cancer cellsapoptotic signalingautophagic fluxHGC-27Inhibitorinhibitorinhibit

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