2. Vitamin D Related/Nuclear Receptor Apoptosis
  3. Nuclear Hormone Receptor 4A/NR4A Apoptosis
  4. Nur77 antagonist 1

Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KDSPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells.

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Nur77 antagonist 1 Chemical Structure

Nur77 antagonist 1 Chemical Structure

CAS No. : 2378780-25-5

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Nur77 antagonist 1 Related Antibodies

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Description

Nur77 antagonist 1(Compound ja) is a selective Nur77 antagonist(KDSPRNur77 = 91 nM). Nur77 antagonist 1 induces cancer cell apoptosis. ja displays excellent antitumor against triple-negative breast cancer (TNBC) cells[1].

IC50 & Target

Nur77/NR4A1

 

In Vitro

Nur77 antagonist 1(Compound ja), shows selectivity against tumor cells from different tissues, possesses highly selective antiproliferative activity toward all tested TNBC cell lines (IC50: 0.40 ± 0.03, 0.38 ± 0.08, 2.12 ± 0.15 for MDA-MB-231,HCC-1806, and BT549) compared to the human normal breast cell line (IC50: 48.01 ± 2.86 for MCF-10A)[1].
Nur77 antagonist 1 (0-2 μM, 6 h) induces MDA-MB-231-sictr cells apoptosis in a Nur77-dependent manner[1].
Nur77 antagonist 1 (0-5 μM, 6 h) induces Nur77-dependent cell-cycle arrest and apoptosis by mediating the TP53 phosphorylation pathway in MDA-MB-231 cells[1].

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

Nur77 antagonist 1 Related Antibodies

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0-5 μM
Incubation Time: 6 h
Result: Induced extrinsic Nur77 degradation.
Induced PARP cleavage in a dose- and time-dependent manner in MDA-MB-231 cells.

Apoptosis Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.32-5 μM
Incubation Time: 5 h
Result: Exhibited the apoptotic cells accounted for 15.10, 25.38, 40.01, 54.83, and 74.62% at 0.32, 0.63, 1.25, 2.5, and 5.0 μM.
In Vivo

Nur77 antagonist 1(Compound ja) (10 mg/kg, i.p) has excellent antitumor efficiency and good in vivo tolerance in the breast cancer MDA-MB-231 xenograft nude mice model[1].
Nur77 antagonist 1 (1.25-5 μM) has good in vivo safety in zebrafish embryo model[1].

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

Animal Model: the breast cancer MDA-MB-231 xenograft nude mice model[1]
Dosage: 10 mg/kg
Administration: i.p
Result: Reduced tumor weight and volume with tumor growth inhibition (TGI) of 99.95%.
Increased cleaved caspase 3 and decreased the proliferation marker Ki67 expression in tumor tissues.
Molecular Weight

492.64

Formula

C25H32N8OS
CAS No.
SMILES

CCN(CC)CCCNC(C1=CC2=C(N1)C=CC(NC3=NC=CC(C4=C(N=C(S4)NC)C)=N3)=C2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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Nur77 antagonist 1 Related Classifications

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Help & FAQs
  • 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 antagonist 12378780-25-5Nuclear Hormone Receptor 4A/NR4AApoptosisNerve Growth Factor IB-like ReceptorNur77 AntagonistTNBCAnticancerMDA-MB-231HCC-1806BT549Inhibitorinhibitorinhibit

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