il 16

Sabialimon P (compound 16) 具抗炎功效，为一种有效的NO释放抑制剂（IC50=18.12 μM）。它可以显著抑制LPS诱导RAW264.7细胞中TNF-α、iNOS、IL-6及NF-κB的产生，并减少COX-2与NF-κB p65的表达。

CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression[1]. CC-90005 shows the exquisite selectivity of CC-90005, with IC50s for all other family members of >3 μM[1].CC-90005 is a moderate inhibitor of both CYP2C9 (IC50=8 μM) and CYP2C19 (IC50=5.9 μM) in human liver microsomes[1].CC-90005 inhibits IL-2 expression in LRS_WBC human PBMCs, with an IC50 of 0.15 μM[1].CC-90005 (1-10 μM; 24 h) inhibits T cell proliferation in PBMCs by 51% at 1 μM and 88% at 3 μM[1]. CC-90005 (3-30 mg kg; p.o. twice daily for 4 days) significantly reduces the popliteal lymph node (PLN) size in a model of chronic T cell activation[1].CC-90005 (100 mg kg; a single p.o.) significantly inhibits plasma and spleen IL-2 release by 51 and 54%, respectively[1].CC-90005 exhibits reasonable oral bioavailability (66 and 46%) and Cmax (1.18 and 1.2 μM) following oral administration (10 and 3 mg kg) in rat and dog, respectively[1].CC-90005 exhibits the mean residence time (0.52 and 2.0 h), CL (69.1 and 20.5 mL min kg) and Vss (2.11 and 2.44 L kg) following intravenous administration (2 and 1 mg kg) in rat and dog, respectively[1]. [1]. Papa P, et, al. Discovery of the Selective Protein Kinase C-θ Kinase Inhibitor, CC-90005. J Med Chem. 2021 Aug 26;64(16):11886-11903.

C12 Galactosylceramide is a bioactive sphingolipid. It inhibits IL-4 production by 53.84% in EL4 T cells when used at a concentration of 10 μM. C12 Galactosylceramide reduces the growth of human papillomavirus type 16-associated tumors in mice and reduces tumor recurrence following surgical removal or chemotherapy. It also reduces natural killer T cell activity, delays the onset of proteinuria, and improves survival in a mouse model of systemic lupus.

PAF C-16 is a naturally occurring phospholipid produced upon stimulation through two distinct pathways known as the remodeling and 'de novo' pathways. It is a potent mediator of neutrophil migration and the production of reactive oxygen species and IL-6. Pathological processes involving PAF include necrotizing enterocolitis

C4 Ceramide is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. [1] [2] [3] It inhibits IL-4 production by 16% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. [1] C4 Ceramide is cytotoxic to SK-BR-3 and MCF-7 Adr breast cancer cells (IC50s = 15.9 and 19.9 μM, respectively). [2] C4 Ceramide also increases maturation and stability of cystic fibrosis transmembrane conductance regulator (CFTR) proteins bearing the F508 deletion (F508del) mutation, enhances cAMP-activated chloride secretion, and suppresses secretion of IL-8 in primary epithelial cells isolated from patients with cystic fibrosis.[3]

Anti-inflammatory agent 11 (化合物 16) 是有效的抗结核分枝杆菌剂，可用于结核病(TB)的研究。Anti-inflammatory agent 11 抑制Mtb H37Rv 和M299的生长，MIC50分别为 1.3 和 6.9 μM。Anti-inflammatory agent 11 也是一种抗炎剂，通过抑制 iNOS 的表达抑制NO，同时抑制 TNF-α 和 IL-1β 的产生。

NLRP3-IN-16为高效、选择性NLRP3炎症小体抑制剂。其抑制IL-1β释放的IC50为0.131 μM，适用于炎症相关研究。

VnP-16是一种合成肽段，对应vitronectin的氨基酸270-281，vitronectin是一种具有细胞附着、迁移和扩散等多功能作用的糖蛋白。该肽段在9.1 µg/cm2浓度下应用于细胞板时，能促进人类成骨细胞的附着和扩散，此效应可通过β1整合素的siRNA敲除被逆转。VnP-16诱导人类皮肤来源的间充质前体细胞和MC3T3-E1小鼠颅骨成骨前体细胞的成骨作用。在体内，VnP-16减少IL-1α诱导的骨质流失并减少小鼠颅骨中破骨细胞的数量。它还在卵巢切除引起的骨质疏失小鼠模型中增加骨矿物质密度并减少松质骨流失。

GSK-3β inhibitor 17 (16, 32, 64 µM) 在 HK-2 细胞急性肾损伤 (AKI) 模型中，对剂量敏感地抑制由顺铂引起的 p-p65 和 KIM-1 蛋白表达。在同样的模型中，使用 32 µM 浓度的 GSK-3β inhibitor 17 可以减少顺铂诱导的 TNF-α、IL-1β、IL-6 和 MCP-1 mRNA 的表达水平。