pd-1/pd-l1-in-10

PD-1/PD-L1-IN-10 是一种口服有效的PD-1/PD-L1抑制剂 (IC50值为2.7 nM)，显示出抗肿瘤活性。

PLD1 inhibitor是一种磷脂酶D1 (PLD1) 的抑制剂。在PLD1过表达的A549细胞中抑制PLD活性（IC50 = 1.97 µM）。PLD1 inhibitor降低A549肺癌和HCT116结直肠癌细胞的活力（IC50分别为18和29 µM）。它还抑制A549细胞的增殖、迁移和侵袭，并诱导这些细胞的凋亡。在小鼠Lewis肺癌模型中，PLD1 inhibitor (10 mg/kg，每隔一天) 可减少肿瘤生长，诱导肿瘤内凋亡，并降低Ras、CD47、CD24和程序性死亡配体1 (PD-L1) 的水平。

INCB086550 (PD-1/PD-L1-IN-8) (example 24) 是 PD-1/PD-L1 的抑制剂，其IC50 值为 <= 10 nM。

Diprovocim-1 is an agonist of the toll-like receptor 1/2 heterodimer.1It induces TNF-α release in THP-1 cells (EC50= 110 pM), an effect that can be inhibited by anti-TLR1 or anti-TLR2 antibodies. Diprovocim-1 (10 mg/kg) increases the production of ovalbumin-specific IgG1 in wild-type, but notTLR2-/-, mice sensitized to ovalbumin.2It also enhances anti-PD-L1 antibody-induced activation of cytotoxic T lymphocytes, reduction of tumor growth, and increases in survival in a B16/F10 murine melanoma model. 1.Morin, M.D., Wang, Y., Jones, B.T., et al.Diprovocims: A new and exceptionally potent class of toll-like receptor agonistsJ. Am. Chem. Soc.140(43)14440-14454(2018) 2.Wang, Y., Su, L., Morin, M.D., et al.Adjuvant effect of the novel TLR1/TLR2 agonist Diprovocim synergizes with anti-PD-L1 to eliminate melanoma in miceProc. Natl. Acad. Sci. U.S.A.115(37)E8698-E8706(2018)