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ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors.

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ERX-41 Chemical Structure

ERX-41 Chemical Structure

CAS No. : 2440087-54-5

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Based on 1 publication(s) in Google Scholar

ERX-41 Related Antibodies

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Description

ERX-41 is an orally active and stereospecific small molecule targeting to lysosomal acid lipase A (LIPA). ERX-41 induces endoplasmic reticulum (ER) stress resulting in cell death, indicating a function independent of LIPA but dependent on its ER localization. ERX-41 involves in a targeted strategy for solid tumors[1].

IC50 & Target

Lysosomal acid lipase A (LIPA)[1]
In Vitro

ERX-41 (1 μM; 0-30 h) induces cell death in MDA-MB-231 without significant effect against normal human mammary epithelial cells (HMECs)[1].
ERX-41 (1 μM; 2 h and 4 h) induces dramatic ER dilation within 4 h, and results disorganization of the peripheral ER network within 2 h[1].
ERX-41 (1 μM; 0.5-4 h) induces downstream unfolded protein response (UPR) pathways via induction of phosphorylated protein kinase R-like ER kinase (p-PERK) and phosphorylated eukaryotic translation initiation factor 2 subunit 1 (p-eIF2-α), and by expression of CCAAT-enhancer-binding homologous protein (CHOP) and phosphorylated inositol-requiring enzyme 1-α (IRE1-α) in TNBC[1].

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

ERX-41 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-231 and HMEC cells
Concentration: 1 μM
Incubation Time: 0, 20 h, 30 h
Result: Showed potent antiproliferative activity against TNBC cell within 30 h.

Western Blot Analysis[1]

Cell Line: SUM-159 cells
Concentration: 1 μM
Incubation Time: 0.5 h, 1 h, 2 h, and 4 h
Result: Increased the protein level of p-PERK, p-eIF2-α and CHOP at 4 h.

Cell Cytotoxicity Assay[1]

Cell Line: SUM-159 and MDA-MB-436
Concentration: 0.125, 0.25, 0.50, 1.0, 2.0, and 4.0 μM
Incubation Time: 0h and 30 h
Result: Caused cell death.
In Vivo

ERX-41 (10 mg/kg; p.o. or i.p.; single dose) is detectable within 1.5 h in established s.c. MDA-MB-231 xenografts after either PO or i.p. administration[1].
ERX-41 (10 mg/kg; p.o.; single dose) significantly inhibits the progression without changing body weight in mouse model with MDA-MB-231 xenografts[1].
ERX-41 (10 mg/kg; p.o. or i.p.; single dose) significantly inhibits the progression in mouse model with MDA-MB-231 s.c. xenografts[1].

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

Animal Model: Mouse models with D2A1 xenografts and MDA-MB-231 xenografts (s.c.), respectively[1]
Dosage: 10 mg/kg
Administration: Oral gavage; once daily for 25 days
Result: Reduced tumor growth against MDA-MB-231 xenograft without affecting body weight. And enhanced p-PERK and p-eIF2-α staining within 24 h.
Significantly reduced the growth of D2A1 xenografts in syngeneic mice without affecting body weight.
Molecular Weight

704.81

Formula

C38H48N4O9
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=CC(OCCO)=C(C=C1)[N+]([O-])=O)NC2=C(C=C(C=C2)C(NC3=C(C=C(C=C3)C(N[C@H]4CC[C@@H](CC4)C)=O)OCC(C)C)=O)OCC(C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light, stored under nitrogen

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

Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (35.47 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.4188 mL 7.0941 mL 14.1882 mL
5 mM 0.2838 mL 1.4188 mL 2.8376 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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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    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (3.55 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 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 (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(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 +
% 
+
%
Tween-80 +
%
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).

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

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 (protect from light, stored under nitrogen). 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 1.4188 mL 7.0941 mL 14.1882 mL 35.4706 mL
5 mM 0.2838 mL 1.4188 mL 2.8376 mL 7.0941 mL
10 mM 0.1419 mL 0.7094 mL 1.4188 mL 3.5471 mL
15 mM 0.0946 mL 0.4729 mL 0.9459 mL 2.3647 mL
20 mM 0.0709 mL 0.3547 mL 0.7094 mL 1.7735 mL
25 mM 0.0568 mL 0.2838 mL 0.5675 mL 1.4188 mL
30 mM 0.0473 mL 0.2365 mL 0.4729 mL 1.1824 mL
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ERX-41 Related Classifications

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:

ERX-412440087-54-5ERX41ERX 41OthersInhibitorinhibitorinhibit

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