CXCR Activator

SB02024 is a potent and orally active VPS34 inhibitor. SB02024 inhibits Vps34 kinase activity. SB02024 induces CCL5 and CXCL10 via STAT1/IRF7. SB02024 shows anticancer activity.

PD-L1-IN-12 is an orally active and potent selenium-containing small-molecule PD-L1 inhibitor (K_D = 9.06 nM). PD-L1-IN-12 can mediate the internalization of PD-L1 and strongly block hPD-1 and hPD-L1 interaction (IC₅₀ = 5.2nM). PD-L1-IN-12 can be used in colorectal cancer immunology research.

STING agonist-50 is an orally active STING agonist with an IC₅₀ of 3.457 μM. STING agonist-50 activates the STING signaling pathway and promotes the phosphorylation of downstream TBK1 and IRF3. STING agonist-50 induces the expression of IFN-β, CXCL10 and IL-6. STING agonist-50 inhibits tumor growth in syngeneic mouse models. STING agonist-50 can be used for the research of colorectal cancer.

mDF6002 is a IL-12R-Fc fusion protein. mDF6002 induces sustained IFNγ production. mDF6002 exerts tumor-suppressive effects in mouse models of colon cancer and melanoma. mDF6002 can be used for research on solid tumors such as colon cancer and melanoma.

SMU-3k is a STING activator and PD-L1 inhibitor, with a PD-L1 IC₅₀ of 106 nM, a K_D of 386 nM for human PD-L1, and a K_D of 352 nM for murine PD-L1. SMU-3k activates the STING pathway, induces phosphorylation of TBK1 and IRF3, and promotes the expression of IFN-β, IL-6 and CXCL10. SMU-3k blocks the PD-1/PD-L1 interaction, reduces PD-L1 levels and induces PD-L1 internalization. Through dual immunomodulation, SMU-3k exerts synergistic tumor growth inhibitory effects in a mouse colon cancer model. SMU-3k can be used for the research of colon cancer.

Herpetin is an active lignan. Herpetin acts as a bone marrow mesenchymal stem cell inducer that activates the SDF-1/CXCR4 axis and the Wnt/β-catenin pathway. Herpetin is applicable to research related to acute liver injury.

WK500B is a potent and orally active BCL6 inhibitor with a K_D of 1.61 μM. WK500B engages intracellular BCL6 and disrupts BCL6‑corepressor interactions to reactivate BCL6 target genes. WK500B exerts cytotoxicity against diffuse large B‑cell lymphoma cells and induces apoptosis and cell cycle arrest. WK500B suppresses germinal center formation in C57BL/6 mice and DLBCL tumor growth in SCID xenograft models without observable toxicity. WK500B can be used for the study of diffuse large B‑cell lymphoma (DLBCL).

LN6023 (hydrochloride) (Compound 27) is a CXCR7 agonist. LN6023 (hydrochloride) induces the recruitment of β-arrestin in HEK293T cells expressing human CXCR7 (EC₅₀ = 3.5 µM). LN6023 (hydrochloride) reduces the surface level of P-selectin in isolated and washed human platelets. LN6023 (hydrochloride) can be used to study platelet-mediated thrombosis.

BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC₅₀ of 101 nM and a pEC₅₀ of 6.99. BAM-12P is a ligand for CXCR7 with an EC₅₀ of 175 nM.