Nur77 modulator 1

CAS No. 2469975-55-9

Nur77 modulator 1 ( —— )

Catalog No. M28278 CAS No. 2469975-55-9

Nur77 modulator 1 is a good Nur77 binder (K D = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .

Purity : >98% (HPLC)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    Nur77 modulator 1
  • Note
    Research use only, not for human use.
  • Brief Description
    Nur77 modulator 1 is a good Nur77 binder (K D = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .
  • Description
    Nur77 modulator 1 is a good Nur77 binder (K D = 3.58 μM). Nur77 modulator 1 up-regulates Nur77 expression, mediates sub-cellular localization of Nur77, induces Nur77-dependent ER stress and autophagy, and results in cell apoptosis. Anti-hepatoma activity .(In Vitro):Nur77 modulator 1 (10g, 0-20 μM) displays potent and broad-spectrum antiproliferative activity against all tested three hepatoma cell lines (HepG2, QGY-7703, and SMMC-7721), and less cytotoxicity against LO2 cells (human normal liver cell line) . Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner . Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis . Nur77 modulator 1 (10g, 2.0 μM) increased LC3-II and Beclin1 protein levels in a dose-dependent manner (10g treatment does not enhance p62 degradation, indicating that autophagy induced by 10g is incomplete) . Cell Viability Assay . Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721). Concentration: 0-20 μM. Incubation Time: 12-24 hours. Result: Exhibited IC 50 values of 0.6 μM, 0.89 μM, 1.40 μM and >20 μM in HepG2, QGY-7703, SMMC-7721 and LO2 cells, respectively. Reduced the viability in a time-dependent manner. Induced cell morphology alteration, such as cell shrinkage, vesicles accumulated, and reduced cell number.(In Vivo):Nur77 modulator 1 (10g, 10 and 20 mg/kg/day) exhibits significant anti-tumor activity in mouse hepatoma HepG2 xenograft with good tolerability . Animal Model: Nude mouse hepatoma HepG2 xenograft . Dosage: 10 and 20 mg/kg/day. Administration: IP, once every day for 15 days. Result: Lead to substantial suppression of tumor growth. The tumor growth inhibition (TGI) values at doses of 10mg/kg/day and 20 mg/kg/day were 36.74 % and 62.38 %, respectively. Exhibited almost no influence on the body weight of experimental mice.
  • Synonyms
    ——
  • Pathway
    Others
  • Target
    Other Targets
  • Recptor
    IGF-1R;Akt;mTOR
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    2469975-55-9
  • Formula Weight
    495.6
  • Molecular Formula
    C28H25N5O2S
  • Purity
    >98% (HPLC)
  • Solubility
    ——
  • SMILES
    COC1=CC=CC2=C1N=C(C)C=C2NC3=CC=C(NC(C(N/N=C/C4=CC=C(SC)C=C4)=O)=C5)C5=C3
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • Stability
    ≥ 2 years

Reference

1.Seol HS, et al. Loss of miR-100 and miR-125b results in cancer stem cell properties through IGF2 upregulation in hepatocellular carcinoma. Sci Rep. 2020 Dec 8;10(1):21412.
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