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CCR

CC chemokine receptor (CCR) antagonists block G protein-coupled receptors that guide leukocyte migration. CCR2, a receptor for monocyte chemoattractant protein 1 (MCP-1), was cloned in 1994 as two splice variants. CCR5 was identified in 1996 as a fusion cofactor for macrophage-tropic human immunodeficiency virus type 1 (HIV-1). Maraviroc, described in 2005 as a selective small-molecule CCR5 inhibitor, blocks this route of viral entry. Other CCR5 antagonists include vicriviroc malate and aplaviroc, while INCB3344 and MK-0812 target CCR2. Cenicriviroc blocks both CCR2 and CCR5, and GSK2239633A is a CCR4 antagonist for studies of T cell trafficking.

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  • LUF7996
    Cat. No.
    A59586
    CAS No.
    3104736-80-0

    LUF7996

    LUF7996 is a potent CCR2 PROTAC degrader that selectively targets and degrades CCR2 with a DC50 value of 2.6 μM. This compound effectively engages with the E3 ligase cereblon, promoting sustained and concentration-dependent degradation of CCR2 via the lysosomal pathway. LUF7996 is particularly valuable for research applications involving the inhibition of monocyte migration in vitro, facilitating studies in inflammation and immune response modulation.

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