il 24

Anti-MouseIL-4Antibody (BVD6-24G2) 为源自大鼠的IgG1kappa类小鼠抗体，专一性靶向IL-4。该抗体的同型对照为RatIgG1kappa, Isotype Control。

BI-69A11 ((E)-3-(1H-Benzo[d]imidazol-2-yl)-1-(6-chloro-2-hydroxy-4-phenylquinolin-3-yl)prop-2-en-1-one) 是一种双重 AKT 和 NFkB 通路抑制剂。它通过靶向 Akt 增强结肠癌细胞对 mda-7 IL-24 诱导的生长抑制的敏感性。

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.

Potent NLRP3 inflammasome inhibitor (IC50 = 60-80 nM). Inhibits nigericin- and ATP-induced IL-1β release. Baldwin et al (2017) Boron-Based Inhibitors of the NLRP3 Inflammasome. Cell Chem.Biol. 24 1321 PMID:28943355 |Redondo-Castro et al (2018) Development of a characterised tool kit for the interrogation of NLRP3 inflammasome-dependent responses. Sci.Rep. 8 5667 PMID:29618797

BMS-986251 is a potent and specific RORγt inverse agonist that exerts its action via oral administration. It shows an EC 50 of 12 nM for RORγt GAL4. In human whole blood assay, BMS-986251 effectively inhibits IL-17 with an EC 50 of 24 nM. Furthermore, BMS-986251 exhibits strong therapeutic effects in mouse acanthosis and Imiquimod-induced models, which are commonly used preclinical models for psoriasis.

Anticancer agent 63 (compound 3h) exhibits significant cytotoxic activity against multiple cancer cell lines, including SW480, HeLa, A549, and MCF-7, with IC 50 values of 4.9, 11.5, 9.4, and 3.4 μM, respectively, after 24 hours of treatment. In particular, Anticancer agent 63 induces apoptosis in MCF-7 cells by down-regulating Bcl-2 expression and up-regulating IL-2 and Caspase-3 expression. Additionally, Anticancer agent 63 demonstrates antioxidative properties [1].

JAK-IN-24 是一种 JAK 抑制剂，在 4 μM 或 1 mM ATP 存在时，IC50分别为 0.534 和 24 nM。JAK-IN-24 还抑制 PBMCIL-15诱导的 STAT5磷酸化，IC50为 86.171 nM。

Daclizumab （Zenapax）为人源化单抗，能特异性地抑制IL-2R-HA的α亚单位。Daclizumab （Zenapax）能通过与CD25的特异性结合而抑制IL-2和IL-2R-HA的结合。Daclizumab （Zenapax）研究多发性硬化症 。

STINGagonist-24 (CF504) 是一种非核苷酸小分子STING 激动剂。STINGagonist-23 激活STING，增加STING、TBK1和IRF3的磷酸化。STINGagonist-23 可促进肿瘤细胞中IFN-β、IL-6、CXCL-10、TNF-α、ISG-15和CCL-5的水平。STINGagonist-23 表现出抗SARS-CoV 系列的活性。