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ML339

ML339 is a selective CXCR6 antagonist with an IC50 of 140 nM. ML339 antagonizes β-arrestin recruitment and cAMP signaling pathway of human CXCR6 receptor induced by CXCL16, with IC50 of 0.3 μM and 1.4 μM, respectively. ML339 shows weaker activity against the recruitment of β-arrestin in mouse CXCR6 receptors, with an IC50 of 18 μM. ML339 has no inhibitory effect on CXCR5, CXCR4, CXCR6 and apelin receptor (APJ), with IC50 >79 μM. ML339 has the potential to promote the development of prostate cancer research[1][2].

Product Specifications

CAS Number

[2579689-83-9]

UNSPSC

12352005

Target

Apelin Receptor (APJ) ; Arrestin; CXCR

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/ml339.html

Purity

99.88

Solubility

DMSO : 75 mg/mL (ultrasonic)

Smiles

O=C(C1=CC(OC)=C(C(OC)=C1)OC)N[C@@H]2C[C@@H](CCC[C@H]3C2)N3CC(NC4=CC=CC=C4Cl)=O

Molecular Formula

C26H32ClN3O5

Molecular Weight

502.00

References & Citations

[1]Paul M Hershberger, et al. Probing the CXCR6/CXCL16 Axis: Targeting Prevention of Prostate Cancer Metastasis.|[2]Peddibhotla S, et al. Discovery of small molecule antagonists of chemokine receptor CXCR6 that arrest tumor growth in SK-HEP-1 mouse xenografts as a model of hepatocellular carcinoma. Bioorg Med Chem Lett. 2020 Feb 15;30 (4) :126899.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

CXCR6

Available Sizes

Curated Selection

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