2. Cytoskeleton TGF-beta/Smad
  3. Integrin TGF-β Receptor
  4. GSK 3008348 hydrochloride

GSK 3008348 hydrochloride 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 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride 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 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer.

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

GSK 3008348 hydrochloride

GSK 3008348 hydrochloride Chemical Structure

CAS No. : 1629249-40-6

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of GSK 3008348 hydrochloride:

GSK 3008348 hydrochloride Related Antibodies

Top Publications Citing Use of Products

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αvβ1 αvβ3 αvβ5 αvβ6 αvβ8 α5β1 α1β1 α2β1 α4β1 α9β1 αIIbβ3 α4β7 αLβ2

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ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B

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Description

GSK 3008348 hydrochloride 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 hydrochloride can target the αvβ6 integrin, inhibit TGF-β activation, and thereby alleviate the fibrotic process. GSK 3008348 hydrochloride 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 hydrochloride can be used for research on pulmonary fibrosis and various types of cancer[1][2][3][4].

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)

In Vitro

GSK 3008348 hydrochloride 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 hydrochloride (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 hydrochloride (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.

GSK 3008348 hydrochloride Related Antibodies

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
Formula

C29H38ClN5O2
CAS No.
Appearance

Solid

Color

Light yellow to khaki

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.[x].Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 100 mg/mL (Need ultrasonic)

DMSO : 11.66 mg/mL (Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.86%

SDS (393 KB)

COA (251 KB) HNMR (284 KB) LCMS (94 KB)

Handling Instructions (2659 KB)
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GSK 3008348 hydrochloride Related Classifications

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  • 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:

GSK 30083481629249-40-6GSK3008348GSK-3008348IntegrinTGF-β ReceptorTransforming growth factor beta receptorsheart failurecardiac fibrosisTGF-βanti-fibrotic therapyInhibitorinhibitorinhibit

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