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Nur77 modulator 1 

Cat. No.: HY-131364
Handling Instructions

Nur77 modulator 1 is a good Nur77 binder (KD = 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.

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

Nur77 modulator 1 Chemical Structure

Nur77 modulator 1 Chemical Structure

CAS No. : 2469975-55-9

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 382 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 580 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1700 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

Nur77 modulator 1 is a good Nur77 binder (KD = 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[1].

IC50 & Target

KD: 3.58 μM (Nur77) [1].

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)[1].
Nur77 modulator 1 (10g, ) could specifically up-regulate the expression of Nur77 in a dose-dependent manner[1].
Nur77 modulator 1 (10g, 2.0 μM) induces Nur77-dependent apoptosis[1].
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)[1].

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

Cell Viability Assay[1].

Cell Line: Liver cancer cell lines (HepG2, QGY-7703, and SMMC-7721).
Concentration: 0-20 μM.
Incubation Time: 12-24 hours.
Result: Exhibited IC50 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[1].

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

Animal Model: Nude mouse hepatoma HepG2 xenograft[1].
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.
Molecular Weight

495.60

Formula

C₂₈H₂₅N₅O₂S

CAS No.
SMILES

CC1=NC2=C(OC)C=CC=C2C(NC3=CC4=C(NC(C(N/N=C/C5=CC=C(SC)C=C5)=O)=C4)C=C3)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (252.22 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0178 mL 10.0888 mL 20.1776 mL
5 mM 0.4036 mL 2.0178 mL 4.0355 mL
10 mM 0.2018 mL 1.0089 mL 2.0178 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: 2.08 mg/mL (4.20 mM); Suspended solution; Need ultrasonic

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.20 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

Nur77 modulator 1OthersERstressautophagyapoptosismitochondriaantitumorgoodtolerabilityInhibitorinhibitorinhibit

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Nur77 modulator 1
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HY-131364
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