GSK 3008348 hydrochloride

Name: GSK 3008348 hydrochloride
Brand: MedChemExpress
SKU: HY-19767A
Rating: 5.0 (2 reviews)

Cat. No.: HY-19767A Purity: 99.86%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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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.

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GSK 3008348 hydrochloride 화학구조

CAS No. : 1629249-40-6

사이즈	재고	수량
1 mg	해외재고보유	Estimated Time of Arrival: December 31
5 mg	해외재고보유	Estimated Time of Arrival: December 31
10 mg	해외재고보유	Estimated Time of Arrival: December 31
25 mg	해외재고보유	Estimated Time of Arrival: December 31
50 mg	해외재고보유	Estimated Time of Arrival: December 31
100 mg	해외재고보유	Estimated Time of Arrival: December 31
200 mg	견적 받기
500 mg	견적 받기

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This product is a controlled substance and not for sale in your territory.

고객리뷰

Based on 2 publication(s) in Google Scholar

Other Forms of GSK 3008348 hydrochloride:

GSK 3008348 In-stock

2 Publications Citing Use of MCE GSK 3008348 hydrochloride

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•Related Screening Libraries:

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View All Integrin Isoform Specific Products:

View All Isoforms

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

View All TGF-β Receptor Isoform Specific Products:

View All Isoforms

ALK1 ALK2 ALK3 ALK4 ALK5 ALK6 ALK7 TGFβR2 ACVR2A ACVR2B BMP

Biological Activity
순도&문서
References
고객리뷰

제품 설명

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.

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.

화학식

C₂₉H₃₈ClN₅O₂

CAS No.

1629249-40-6

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

선적

Room temperature in continental US; may vary elsewhere.

보관

4°C, sealed storage, away from moisture

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

용액&용해도

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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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).

순도&문서

Purity: 99.86%

Select Batch:

Data Sheet (276 KB) SDS (394 KB)

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

Handling Instructions (2659 KB)

References

[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]