Art. -Nr.: HY-19767

GSK 3008348

2 Cited Publications

Kundenbewertung

Based on 2 publication(s) in Google Scholar

GSK 3008348 is a small molecule antagonist of integrin αvβ6 with IC₅₀ values for αvβ6, αvβ1, αvβ3, αvβ5, and αvβ8 are 1.50, 2.83, 12.53, 4.00, and 2.26 nM, respectively. GSK 3008348 can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 prevents the binding of the foot-and-mouth disease virus (FMDV) to the αvβ6 integrin receptor on the surface of host cells, thereby inhibiting the entry of the virus. GSK 3008348 can be used for research on pulmonary fibrosis and various types of cancer.

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Reinheit: 98.04%
CAS. Nr.: 1629249-33-7
Formel: C₂₉H₃₇N₅O₂
Molecular Weight:487.64

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

GSK 3008348 Chemical Structure

CAS. Nr.: 1629249-33-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Clinical Trial
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[3]

αvβ6

1.50 nM (IC₅₀)

αvβ1

2.83 nM (IC₅₀)

αvβ3

12.53 nM (IC₅₀)

αvβ5

4.00 nM (IC₅₀)

αvβ8

2.26 nM (IC₅₀)

Alle Integrin Isoform-spezifische Produkte anzeigen :

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

GSK 3008348 antagonizes integrin αvβ6 with an affinity (pIC₅₀) value of 8.1 in the fluorescence polarisation assay, whereas its affinity in the cell adhesion assays (K562 cells) is for:αvβ6 (pIC₅₀ = 8.4); αvβ3 (pIC₅₀ = 6); αvβ5 (pIC₅₀ = 6.9); αvβ8 (pIC₅₀ = 7.7)^[1].
GSK 3008348 (8 h) suppresses FMDV RNA (vRNA) replication and virus production when added prior to or concurrently with virus infection in PK-15 cells^[2].
GSK 3008348 (10 μM, 1 h) decreases TGF-β1-activated procollagen I production in primary human hepatic stellate cells, fails to inhibit TGF-β1 induced SMAD3 and SMAD2 phosphorylation, but inhibits TGF-β-induced phosphorylation of ERK1/2 and STAT3^[3].

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

Western Blot Analysis^[3]

Cell Line:

Hepatic stellate cells
Concentration:

10 μM
Incubation Time:

1 h
Result:

Reversed TGF-β1 induced p-SMAD3 nuclear translocation.
Significantly inhibited TGFβ1 induced ERK1/2 phosphorylation levels.
Significantly inhibited STAT3 phosphorylation in HSCs.
Did not show effects on TGF-β1-induced SMAD3 phosphorylation.

Clinical Trial

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

Chemical Information

CAS. Nr. 1629249-33-7
Appearance Solid
Molecular Weight 487.64
Formel C₂₉H₃₇N₅O₂
Color Brown to orange
SMILES

O=C(O)C[C@@H](C1=CC(N2N=C(C)C=C2C)=CC=C1)CN3C[C@H](CCC(N4)=CC=C5C4=NCCC5)CC3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (2)

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mBio

Heat Shock Protein 60 Is Involved in Viral Replication Complex Formation and Facilitates Foot and Mouth Virus Replication by Stabilizing Viral Nonstructural Proteins 3A and 2C. [Abstract]

2022 Oct 26;13(5):e0143422. PMID: 36106732
Biochem J

Integrin αVβ1 regulates procollagen I production through a non-canonical transforming growth factor β signaling pathway in human hepatic stellate cells. [Abstract]

2021 May 14;478(9):1689-1703. PMID: 33876829

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (51.27 mM; Need ultrasonic; 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

2.0507 mL

10.2535 mL

20.5069 mL

5 mM

0.4101 mL

2.0507 mL

4.1014 mL

10 mM

0.2051 mL

1.0253 mL

2.0507 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, 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.

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: ≥ 2.5 mg/mL (5.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (5.13 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, 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 (278 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)

Verweise

[1]. Anderson Niall Andrew, et al. Preparation of naphthyridine derivatives useful as αvβ6 integrin antagonists. From PCT Int. Appl. (2014), WO 2014154725 A1 20141002.

[2]. Tang J, et al. Heat Shock Protein 60 Is Involved in Viral Replication Complex Formation and Facilitates Foot and Mouth Virus Replication by Stabilizing Viral Nonstructural Proteins 3A and 2C. mBio. 2022 Oct 26;13(5):e0143422. [Content Brief]

[3]. Han Z, et al. Integrin αVβ1 regulates procollagen I production through a non-canonical transforming growth factor β signaling pathway in human hepatic stellate cells. Biochem J. 2021 May 14;478(9):1689-1703. [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, 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	2.0507 mL	10.2535 mL	20.5069 mL	51.2673 mL
	5 mM	0.4101 mL	2.0507 mL	4.1014 mL	10.2535 mL
	10 mM	0.2051 mL	1.0253 mL	2.0507 mL	5.1267 mL
	15 mM	0.1367 mL	0.6836 mL	1.3671 mL	3.4178 mL
	20 mM	0.1025 mL	0.5127 mL	1.0253 mL	2.5634 mL
	25 mM	0.0820 mL	0.4101 mL	0.8203 mL	2.0507 mL
	30 mM	0.0684 mL	0.3418 mL	0.6836 mL	1.7089 mL
	40 mM	0.0513 mL	0.2563 mL	0.5127 mL	1.2817 mL
	50 mM	0.0410 mL	0.2051 mL	0.4101 mL	1.0253 mL

Keywords

GSK 3008348

2 Cited Publications

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GSK 3008348

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Publications Citing Use of MedChemExpress (MCE) GSK 3008348

Alle Integrin Isoform-spezifische Produkte anzeigen

Alle TGF-β Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

GSK 3008348 Related Classifications

HY-19767 Related Classifications