1. Epigenetics
  2. MicroRNA
  3. RJW100

RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter.

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RJW100 Chemical Structure

RJW100 Chemical Structure

CAS No. : 1276664-20-0

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Description

RJW100 is a potent liver receptor homolog 1 (LRH-1, NR5A2) and steroidogenic factor-1 (SF-1, NR5A1) agonist with pEC50s of 6.6 and 7.5, respectively[1]. RJW100 also causes strong activation of the miR-200c (miRNA-200c, microRNA-200c) promoter[2].

IC50 & Target

pEC50: 6.6 (LRH-1) and 7.5 (SF-1)[1]

Cellular Effect
Cell Line Type Value Description References
HeLa EC50
1.5 μM
Compound: RJW100
Agonist activity at human full length LRH1 transfected in human HeLa cells incubated for 24 hrs by renilla luciferase reporter gene assay
Agonist activity at human full length LRH1 transfected in human HeLa cells incubated for 24 hrs by renilla luciferase reporter gene assay
[PMID: 31419141]
In Vitro

RJW100 (compound 24-exo) treatment induces a significant dose-dependent increase in small/short heterodimer partner (SHP) transcripts beginning at 5 µM[1].
RJW100 (compound 24-exo) clearly displaces the bound PIP2 phospholipid from SF-1 almost completely at 1 µM[1].
Using hLRH-1 LBD alone that had not been complexed with any phospholipids, the result shows a clear dose-dependent shift in hLRH-1 LBD (ligand binding domain) native PAGE migration upon RJW100 (compound 24-exo; 0-100 µM) binding[1].
RJW100 causes strong activation of the miR-200c promoter and exhibits strong ability to downregulate ZEB1 and ZEB2 proteins[2].

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

RT-PCR[1]

Cell Line: HEK293 cells
Concentration: 1 µM, 5 µM, 10 µM
Incubation Time: 24 hours
Result: Induced a significant dose-dependent increase in SHP transcripts beginning at 5 µM.
Molecular Weight

386.58

Formula

C28H34O

CAS No.
Appearance

Oil

Color

Colorless to light yellow

SMILES

O[C@@H]1CC[C@@]2(C(C3=CC=CC=C3)=C)C(C4=CC=CC=C4)=C(CCCCCC)C[C@@]12[H].[Relative stereochemistry]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Pure form -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 180 mg/mL (465.62 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5868 mL 12.9339 mL 25.8679 mL
5 mM 0.5174 mL 2.5868 mL 5.1736 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 4.5 mg/mL (11.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 4.5 mg/mL (11.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (45.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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g

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5868 mL 12.9339 mL 25.8679 mL 64.6697 mL
5 mM 0.5174 mL 2.5868 mL 5.1736 mL 12.9339 mL
10 mM 0.2587 mL 1.2934 mL 2.5868 mL 6.4670 mL
15 mM 0.1725 mL 0.8623 mL 1.7245 mL 4.3113 mL
20 mM 0.1293 mL 0.6467 mL 1.2934 mL 3.2335 mL
25 mM 0.1035 mL 0.5174 mL 1.0347 mL 2.5868 mL
30 mM 0.0862 mL 0.4311 mL 0.8623 mL 2.1557 mL
40 mM 0.0647 mL 0.3233 mL 0.6467 mL 1.6167 mL
50 mM 0.0517 mL 0.2587 mL 0.5174 mL 1.2934 mL
60 mM 0.0431 mL 0.2156 mL 0.4311 mL 1.0778 mL
80 mM 0.0323 mL 0.1617 mL 0.3233 mL 0.8084 mL
100 mM 0.0259 mL 0.1293 mL 0.2587 mL 0.6467 mL
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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.

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RJW100
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