Art. -Nr.: HY-100432

LOC14

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC₅₀ and K_d values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells.

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Reinheit: 98.0%
CAS. Nr.: 877963-94-5
Formel: C₁₆H₁₉N₃O₂S
Molecular Weight:317.41

Speicherung:

4°C, protect from light

* The compound is unstable in solutions, freshly prepared is recommended.

LOC14 Chemical Structure

CAS. Nr.: 877963-94-5

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC₅₀ and K_d values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding^[1]. LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells^[3].

IC₅₀ & Target

Kd: 62 nM (PDI)^[1]

In Vitro

LOC14 (0.01-100 μM; 24 hours) exhibits the capacity to inhibit recombinant (r)PDIA3 at an IC50 of approximately 5 μM^[3].

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

Cell Viability Assay^[3]

Cell Line:

MTEC cells
Concentration:

0.01 μM; 0.1 μM; 0.5 μM; 1 μM; 5 μM; 10 μM; 100 μM
Incubation Time:

24 hours
Result:

Inhibited recombinant (r)PDIA3 activity.

In Vivo

LOC14 (orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks) significantly improves motor function, attenuated brain atrophy and extended survival in the N171–82Q HD mice^[2].

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

Animal Model:

Male N171–82Q HD mice^[2]
Dosage:

20 mg/kg
Administration:

Orally administered by gavage; 20 mg/kg; once daily; 12-28 weeks
Result:

Improved motor function in HD mice.

Chemical Information

CAS. Nr. 877963-94-5
Appearance Solid
Molecular Weight 317.41
Formel C₁₆H₁₉N₃O₂S
Color White to off-white
SMILES

O=C(C(C=CC=C1)=C1S2)N2CN3CCN(C(C4CC4)=O)CC3
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* The compound is unstable in solutions, freshly prepared is recommended.

Publications (5)

All WBCell Imaging/StainingIn Vivo Efficacy StudyIFCell Proliferation/Viability Assay

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Journal Impact Factor

Adv Sci (Weinh)

Irgm1 Improves Postinfarction Cardiac Repair by Promoting Neutrophil Clearance and Efferocytosis. [Abstract]

2026 Apr;13(21):e14863. PMID: 41738282

LOC14 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Apr;13(21):e14863. [Abstract]

LOC14 (10 μM; 16 h) increased the GRP78 protein expression in WT and Irgm1-cKO neutrophils incubated with LPS (2 µg/mL).

LOC14 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Apr;13(21):e14863. [Abstract]

LOC14 (10 μM; 16 h) increased the GRP78 expression and partial recovery of efferocytosis in WT and Irgm1-cKO neutrophils incubated with LPS (2 µg/mL).

LOC14 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Apr;13(21):e14863. [Abstract]

LOC14 (10 μM; 16 h) contributed to partial recovery of PtdSer exposure and efferocytosis in WT and Irgm1-cKO neutrophils incubated with LPS (2 µg/mL).

LOC14 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Apr;13(21):e14863. [Abstract]

LOC14 (20 mg/kg; po; daily for 7 days) increased survival rate of WT and Irgm1‐cKO mice with myocardial infarction (MI).

LOC14 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Apr;13(21):e14863. [Abstract]

LOC14 (20 mg/kg; po; daily for 7 days) significantly reduced the infarct size in both WT and Irgm1‐cKO mice with myocardial infarction (MI).

LOC14 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2026 Apr;13(21):e14863. [Abstract]

LOC14 (20 mg/kg; po; daily for 7 days) improved efferocytosis of neutrophils in both WT and Irgm1‐cKO mice in the heart in both WT and Irgm1‐cKO mice with myocardial infarction (MI).
Schizophr Bull

Protein Disulfide Isomerase A3, a Stress Response Gene, Is Associated with Cognitive Impairment in Schizophrenia and Linked to Inflammatory Activation. [Abstract]

2025 Oct 30:sbaf194. PMID: 41165200
Int J Antimicrob Agents

Targeting the human protein disulfide isomerase A3 as a broad-spectrum antiviral approach against human respiratory viruses. [Abstract]

2026 Apr 2:107802. PMID: 41935586
Antiviral Res

Venezuelan equine encephalitis virus E1 protein interacts with PDIA6 and PDI inhibition reduces alphavirus production. [Abstract]

2023 Apr:212:105560. PMID: 36822370

LOC14 purchased from MedChemExpress. Usage Cited in: Antiviral Res. 2023 Apr:212:105560. [Abstract]

The CC₅₀ (50% cytotoxic concentration) of LOC14 (0-2.5 µM; 16 h) is 93 μM for Vero cells, 70 μM for U87-MG cells.
Virginia Polytechnic Institute and State University

2023 Mar 31.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (157.52 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.1505 mL

15.7525 mL

31.5050 mL

5 mM

0.6301 mL

3.1505 mL

6.3010 mL

10 mM

0.3150 mL

1.5752 mL

3.1505 mL

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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: ≥ 2.08 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

Protocol 2

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

Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.08 mg/mL (6.55 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Kaplan A, et al. Small molecule-induced oxidation of protein disulfide isomerase is neuroprotective. Proc Natl Acad Sci U S A. 2015 Apr 28;112(17):E2245-52. [Content Brief]

[2]. Chamberlain N, et al. Lung epithelial protein disulfide isomerase A3 (PDIA3) plays an important role in influenza infection, inflammation, and airway mechanics. Redox Biol. 2019 Apr;22:101129. [Content Brief]

[3]. Zhou X, et al. Small molecule modulator of protein disulfide isomerase attenuates mutant huntingtin toxicity and inhibits endoplasmic reticulum stress in a mouse model of Huntington's disease. Hum Mol Genet. 2018 May 1;27(9):1545-1555. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Please refer to the solubility information to select the appropriate solvent. The compound is unstable in solutions, freshly prepared is recommended.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.1505 mL	15.7525 mL	31.5050 mL	78.7625 mL
	5 mM	0.6301 mL	3.1505 mL	6.3010 mL	15.7525 mL
	10 mM	0.3150 mL	1.5752 mL	3.1505 mL	7.8762 mL
	15 mM	0.2100 mL	1.0502 mL	2.1003 mL	5.2508 mL
	20 mM	0.1575 mL	0.7876 mL	1.5752 mL	3.9381 mL
	25 mM	0.1260 mL	0.6301 mL	1.2602 mL	3.1505 mL
	30 mM	0.1050 mL	0.5251 mL	1.0502 mL	2.6254 mL
	40 mM	0.0788 mL	0.3938 mL	0.7876 mL	1.9691 mL
	50 mM	0.0630 mL	0.3150 mL	0.6301 mL	1.5752 mL
	60 mM	0.0525 mL	0.2625 mL	0.5251 mL	1.3127 mL
	80 mM	0.0394 mL	0.1969 mL	0.3938 mL	0.9845 mL
	100 mM	0.0315 mL	0.1575 mL	0.3150 mL	0.7876 mL

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LOC14

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) LOC14

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LOC14

MCE Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) LOC14

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

LOC14 Related Classifications

HY-100432 Related Classifications