Cat. No.: HY-100506

GLPG0187

18 Cited Publications

Customer Review

Based on 18 publication(s) in Google Scholar

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits α_vβ₁-integrin with an IC₅₀ of 1.3 nM. GLPG0187 inhibits migrasome biogenesis without cytotoxicity.

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

Purity: 99.43%
CAS No.: 1320346-97-1
Formula: C₂₉H₃₇N₇O₅S
Molecular Weight:595.71

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GLPG0187 Chemical Structure

CAS No.: 1320346-97-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (18)
Solvent & Solubility
- In Vitro
- In Vivo
Protocol
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits α_vβ₁-integrin with an IC₅₀ of 1.3 nM^[1]. GLPG0187 inhibits migrasome biogenesis without cytotoxicity^[3].

IC₅₀ & Target

IC50: 1.3 nM (α_vβ₁)^[1]

All Integrin Isoforms :

In Vitro

In a solid-phase assay, GLPG0187 shows selectivity for several RGD integrin receptors with IC₅₀s of 1.3, 3.7, 2.0, 1.4, 1.2, 7.7 nM for α_vβ₁, α_vβ₃, α_vβ₅, α_vβ₆,α_vβ₈, and α₅β₁. GLPG0187 is a potent inhibitor of osteoclastic bone resorption and angiogenesis. Treatment with GLPG0187 dose-dependently increases the E-cadherin/vimentin ratio, rendering the cells a more epithelial, sessile phenotype. GLPG0187 dose-dependently diminishes the size of the aldehyde dehydrogenase high subpopulation of prostate cancer cells^[1]. GLPG0187 treatment results in cell rounding and clumping. GLPG0187 demonstrates a dose-dependent significant reduction in tumour cell migration. GLPG0187 at all concentrations significantly reduces cell proliferation^[2].

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

In Vivo

Blocking α_v-integrins by GLPG0187 markedly reduces their metastatic tumor growth. Bone tumor burden is significantly lower and the number of bone metastases/mouse is significantly inhibited. The progression of bone metastases and the formation of new bone metastases during the treatment period is significantly inhibited^[1].

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 1320346-97-1
Appearance Solid
Molecular Weight 595.71
Formula C₂₉H₃₇N₇O₅S
Color White to off-white
SMILES

O=C(O)[C@H](CNC1=NC(C)=NC(N2CCC(C3=NC4=C(CCCN4)C=C3)CC2)=C1C)NS(=O)(C5=CC=C(OC)C=C5)=O
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (18)

All Cell Imaging/StainingCell Migration/Invasion AssayBio/Physico-chemical AssayWBIF

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Journal Impact Factor

Cell

Directed evolution of a family of AAV capsid variants enabling potent muscle-directed gene delivery across species. [Abstract]

2021 Sep 16;184(19):4919-4938.e22. PMID: 34506722
Cell Res

Localized, highly efficient secretion of signaling proteins by migrasomes. [Abstract]

2024 Aug;34(8):572-585. PMID: 38918584

GLPG0187 purchased from MedChemExpress. Usage Cited in: Cell Res. 2024 Aug;34(8):572-585. [Abstract]

L929 cells stably expressing mCherry-Myo5a and T4-BFP, treated with or without 10 μM GLPG0187, were subjected to time-lapse imaging. Time interval, 10 min. Cyan dashed lines outline the cell body, and yellow dashed lines outline mCherry-Myo5a puncta. Scale bar, 20 μm. Polarization of mCherry-Myo5a was quantified and shown as the means ± SEM for triplicate samples of > 50 cells.

GLPG0187 purchased from MedChemExpress. Usage Cited in: Cell Res. 2024 Aug;34(8):572-585. [Abstract]

L929 cells stably expressing GFP-Rab8a and T4-BFP, treated with or without 10 μM GLPG0187, were subjected to time-lapse imaging. Time interval, 10 min. Cyan dashed lines outline the cell body, and yellow dashed lines outline GFP-Rab8a vesicles, respectively. Scale bar, 20 μm. Polarization of GFP-Rab8a was quantified and shown as the means ± SEM for triplicate samples of > 50 cells. Two-tailed unpaired t-test was used for statistical analyses (right panel).
Gut

Activated intestinal muscle cells promote preadipocyte migration: a novel mechanism for creeping fat formation in Crohn's disease. [Abstract]

2022 Jan;71(1):55-67. PMID: 33468536

GLPG0187 purchased from MedChemExpress. Usage Cited in: Gut. 2022 Jan;71(1):55-67. [Abstract]

Integrin α5 blocking antibody and GLPG0187 (integrin αv antagonist) but not α3 blocking antibody reduced the migration of pre-adipocytes towards HIMC conditioned medium in the Boyden chamber.

GLPG0187 purchased from MedChemExpress. Usage Cited in: Gut. 2022 Jan;71(1):55-67. [Abstract]

Representative tracking of pre-adipocytes seeded on decellularized human muscularis propria was performed for 24 h in the absence (control) and presence of integrin β1 blocking antibody, α5 blocking antibody, and GLPG0187 (integrin αv antagonist).

GLPG0187 purchased from MedChemExpress. Usage Cited in: Gut. 2022 Jan;71(1):55-67. [Abstract]

Distance, displacement, velocity and migration persistence of pre-adipocytes migration on decellularized human intestine with adding integrin β1 and α5 blocking antibody, and GLPG0187 (integrin αv antagonist).
Cancer Commun (Lond)

Galectin 3-binding protein (LGALS3BP) depletion attenuates hepatic fibrosis by reducing transforming growth factor-β1 (TGF-β1) availability and inhibits hepatocarcinogenesis. [Abstract]

2024 Oct;44(10):1106-1129. PMID: 39073023
Clin Mol Hepatol

Ursolic acid targets secreted phosphoprotein 1 to regulate Th17 cells against non-alcoholic fatty liver disease. [Abstract]

2024 Jul;30(3):449-467. PMID: 38623614
Adv Sci (Weinh)

Succinic Acid-Induced Macrophage Endocytosis Promotes Extracellular Vesicle-Based Integrin Beta1 Transfer Accelerating Fibroblast Activation and Sepsis-Associated Pulmonary Fibrosis. [Abstract]

2025 Sep 2:e07411. PMID: 40898357
Biomaterials

CD44 and αV-integrins dual-targeting bimetallic nanozymes for lung adenocarcinoma therapy via NIR-enhanced ferroptosis/apoptosis. [Abstract]

2025 May 13:323:123407. PMID: 40403445
Cell Discov

Packaged release and targeted delivery of cytokines by migrasomes in circulation. [Abstract]

2024 Dec 9;10(1):121. PMID: 39648224
ACS Appl Mater Interfaces

Regulation of Osteogenic Differentiation of hBMSCs by the Overlay Angles of Bone Lamellae-like Matrices. [Abstract]

2024 Oct 23;16(42):56801-56814. PMID: 39389937
Arterioscler Thromb Vasc Biol

Lineage-Specific Induced Pluripotent Stem Cell-Derived Smooth Muscle Cell Modeling Predicts Integrin Alpha-V Antagonism Reduces Aortic Root Aneurysm Formation in Marfan Syndrome Mice. [Abstract]

2023 Jul;43(7):1134-1153. PMID: 37078287

GLPG0187 purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2023 Jul;43(7):1134-1153. [Abstract]

GLPG0187 (10 nM; 24 h) significantly reduces the expression of p-Akt^Thr308 signaling in SHF and NC cells.

GLPG0187 purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2023 Jul;43(7):1134-1153. [Abstract]

GLPG0187 (10 nM; 24 h) significantly reduces the expression of Ki-67 in SHF and NC cells.
J Cell Biol

Migratory autolysosome disposal mitigates lysosome damage. [Abstract]

2024 Dec 2;223(12):e202403195. PMID: 39347717
Breast Cancer Res

Cilengitide sensitivity is predicted by overall integrin expression in breast cancer. [Abstract]

2024 Dec 20;26(1):187. PMID: 39707454
Mol Oncol

ITGAV and SMAD4 influence the progression and clinical outcome of pancreatic ductal adenocarcinoma. [Abstract]

2025 Jul 30. PMID: 40739706
Cancer Sci

Integrin-α5 expression and its role in non-small cell lung cancer progression. [Abstract]

2025 Feb;116(2):406-419. PMID: 39581761
J Pharm Biomed Anal

A stop-flow comprehensive two-dimensional HK-2 and HK-2/CIKI cell membrane chromatography comparative analysis system for screening the active ingredients from Pyrrosia calvata (Bak.) Ching against crystal-induced kidney injury. [Abstract]

2021 Feb 20;195:113825. PMID: 33339641
SSRN

2024 Nov 5.
University of Toronto

2024.
Oxid Med Cell Longev

FNDC5 Attenuates Oxidative Stress and NLRP3 Inflammasome Activation in Vascular Smooth Muscle Cells via Activating the AMPK-SIRT1 Signal Pathway. [Abstract]

2020 May 16;2020:6384803. PMID: 32509148

Solvent & Solubility

In Vitro:

DMSO : 12.5 mg/mL (20.98 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)

H₂O : < 0.1 mg/mL (insoluble)

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

1.6787 mL

8.3933 mL

16.7867 mL

5 mM

0.3357 mL

1.6787 mL

3.3573 mL

10 mM

0.1679 mL

0.8393 mL

1.6787 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 1.25 mg/mL (2.10 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (12.5 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% Corn Oil

Solubility: ≥ 1.25 mg/mL (2.10 mM); Clear solution

This protocol yields a clear solution of ≥ 1.25 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 (12.5 mg/mL) to 900 μL Corn oil, and mix evenly.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: ≥ 0.89 mg/mL (1.49 mM); Clear solution

Protocol 4

Add each solvent one by one: 5% DMSO 95% (20% SBE-β-CD in Saline)

Solubility: ≥ 0.89 mg/mL (1.49 mM); Clear solution

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 50% PEG300 50% Saline

Solubility: 10 mg/mL (16.79 mM); Suspended solution; Need ultrasonic

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

Protocol

Cell Assay^[2]

Tumour cell proliferation is determined using the MTS assay. PC3 cells are seeded at 10,000 cells/well in 96 well plates containing either GLPG0187 (0.5, 5, or 50 ng/mL), vehicle or media control, then cultured in 100 µL medium for 24 hr. Cell proliferation is analysed using 20 µL MTS dye incubated for 3 hr at 37°C in the dark. Absorbance from each well (6/treatment) is quantified at 490 nm and the mean fluorescence calculated. The assay is repeated at 48, 72 and 96 hr, on three independent occasions^[2].

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

Animal Administration^[1]

Mice: The effect of GLPG0187 on bone loss is evaluated in 3-month-old castrated male mice after 4 weeks of treatment with dosing starting immediately after castration (preventive protocol). Two different modes of administration are used: either subcutaneous twice daily with 10, 30, or 100 mg/kg of GLPG0187, either oral, twice daily with 30, 100, or 300 mg/kg of GLPG0187^[1].

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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)

References

[1]. van der Horst G, et al. Targeting of α(v)-integrins in stem/progenitor cells and supportive microenvironment impairs bone metastasis in human prostate cancer. Neoplasia. 2011 Jun;13(6):516-25. [Content Brief]

[2]. Reeves KJ, et al. Prostate cancer cells home to bone using a novel in vivo model: modulation by the integrin antagonist GLPG0187. Int J Cancer. 2015 Apr 1;136(7):1731-40. [Content Brief]

[3]. Puzhong Lu, et al. Chemical screening identifies ROCK1 as a regulator of migrasome formation. Cell Discov. 2020 Aug 4;6(1):51. [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

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.6787 mL	8.3933 mL	16.7867 mL	41.9667 mL
	5 mM	0.3357 mL	1.6787 mL	3.3573 mL	8.3933 mL
	10 mM	0.1679 mL	0.8393 mL	1.6787 mL	4.1967 mL
	15 mM	0.1119 mL	0.5596 mL	1.1191 mL	2.7978 mL
	20 mM	0.0839 mL	0.4197 mL	0.8393 mL	2.0983 mL

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GLPG0187

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Cytoskeleton Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GLPG0187

All Integrin Isoforms

Biological Activity

Chemical Information

Publications (18)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GLPG0187

Immunology/Inflammation Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Cytoskeleton Compound Library

Targeted Diversity Library

Membrane Protein-targeted Compound Library

Extracellular Vesicles (EVs) Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) GLPG0187

All Integrin Isoforms

Biological Activity

Chemical Information

Publications (18)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

GLPG0187 Related Classifications

Cat. No.: HY-100506