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CD80 inhibitor 6

Chemical Structure : CD80 inhibitor 6

CAS No.: 848607-77-2

CD80 inhibitor 6 (CD80-IN-6)

Catalog No.: PC-22887Not For Human Use, Lab Use Only.

CD80 inhibitor 6 is a specific small molecule inhibitor of human CD80 with SPR KD of 2.7 nM, antagonize CD28 (TR_FRET EC50=2.4 nM) and CTLA-4 binding to CD80, inhibits the release of the proinflammatory cytokines IL-2, IFNγ, and TNFα at submicromolar doses in T cell costimulation assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

CD80 inhibitor 6 is a specific small molecule inhibitor of human CD80 with SPR KD of 2.7 nM, antagonize CD28 (TR_FRET EC50=2.4 nM) and CTLA-4 binding to CD80, inhibits the release of the proinflammatory cytokines IL-2, IFNγ, and TNFα at submicromolar doses in T cell costimulation assays.
CD80 inhibitor 6 binds specifically to human CD80 but not the related protein, human CD86, nor human CD28-Fc, nor do the compounds bind mouse, rat, or canine CD80.
CD80 inhibitor 6 inhibits IL-2 secretion in the CD4+ T cell assay with IC50 of 0.75 uM in purified peripheral blood CD4+ primary T cells.
CD80 inhibitor 6 also inhibits TNFα and IFNγ secretion with IC50 values of 0.97 μM and 0.15 μM, respectively.

Physicochemical Properties

M.Wt 480.52
Formula C25H26F2N6O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

N-(3-(cyclohexylamino)propyl)-4-(6,9-difluoro-3-oxo-3,5-dihydro-2H-pyrazolo[4,3-c]cinnolin-2-yl)benzamide

References

1. Philip Huxley, et al. Chem Biol. 2004 Dec;11(12):1651-8.

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