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Nur77 antagonist 2

Nur77 antagonist 2 (Compound 12b) is an orally active Nur77 antagonist with a KD value of 0.42 μM. Nur77 antagonist 2 exhibits proliferative activity on liver cancer cells. Nur77 antagonist 2 stabilizes Nur77 by inhibiting its ubiquitin-proteasomal degradation, leading to Nur77-dependent apoptosis via the ASK1-JNK/p38 pathway. Nur77 antagonist 2 inhibits tumor growth in the HCCLM3 xenograft model. Nur77 antagonist 2 can be used for the study of hepatocellular carcinoma (HCC) [1].

Product Specifications

UNSPSC

12352005

Target

Apoptosis; ASK1; JNK; Nuclear Hormone Receptor 4A/NR4A; p38 MAPK

Related Pathways

Apoptosis; MAPK/ERK Pathway; Vitamin D Related/Nuclear Receptor

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Smiles

O=C(N/N=C/C1=CC(C)=CC=C1)C(N2)=CC3=C2C=CC(NC4=NC=CC(C5=CC=NC=C5)=N4)=C3

Molecular Formula

C26H21N7O

Molecular Weight

447.49

References & Citations

[1]Hu S, et al. Design, synthesis, and evaluation of 5- ((4- (pyridin-3-yl) pyrimidin-2-yl) amino) -1H-indole-2-carboxamide derivatives as anti-HCC agents targeting Nur77. Bioorg Chem. 2025 Oct 18;167:109113.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Nur77/NR4A1

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