cell maturation

Vacuolin-1 是一种细胞渗透性抑制剂，可抑制 Ca2+ 依赖性溶酶体与细胞膜的融合。它通过抑制溶酶体内容物的释放起作用。它是一种有效的选择性 PIKfyve 抑制剂，通过损害溶酶体成熟来抑制晚期自噬。

1Z105 作为一种TLR4 MD2配体，具备口服活性。该化合物可以促进树突状细胞的成熟和抗原呈递，从而用于预防关节炎。

Lipid N2-3L为一可电离阳离子脂质（pKa = 8.99），常见于超分子脂质纳米粒子（SMLNPs）中，适用于封装mRNA。该类SMLNPs含Lipid N2-3L，可在鼠体注射部位及引流淋巴结积累，此类SMLNPs内包含有萤光素酶报告基因。此外，Lipid N2-3L SMLNPs也封装了卵清蛋白mRNA和Toll样受体7 8（TLR7 8）激动剂R-848，作为佐剂使用，可促进树突状细胞成熟与抗原呈递，有效减小MC-38-OVA结肠癌小鼠模型的肿瘤体积并提升存活率。

MK256是一种新型的CDK8抑制剂，通过抑制STAT通路显示出针对AML的强大抗肿瘤活性。MK256能引发分化和成熟，并抑制AML细胞系的增殖。此外，MK256不仅下调了磷酸化的STAT1(S727)和STAT5(S726)，还减少了AML细胞系中MCL-1和CCL2的mRNA表达。在MOLM-14异种移植模型中, MK256的效能得到了证实，观察到治疗后磷酸化STAT1(S727)和STAT5(S726)的抑制作用。MK256在MOLM-14异种移植模型中的药理动力学研究显示了对STAT通路的剂量依赖性抑制效果。无论是体外还是体内研究都表明，MK256能有效地下调STAT通路。

ARN23765 是一种 F508del-CFTR 校正剂，在人支气管上皮细胞中的EC50为 38 pM。它能够改善细胞膜中 F508del-CFTR 的成熟和功能，影响离子的运输与分泌，从而纠正囊性纤维化 (CF) 的病理机制。

Psora 4 (5-(4-Phenylbutoxy)psoralen) 是一种具有选择性和高效性的 Kv1.3 阻断剂，是热量限制模拟物，具有免疫抑制活性，可增强神经祖细胞的分化和成熟。

Concanamycin B is a macrolide antibiotic that selectively inhibits vacuolar type H+-ATPases, also known as V-ATPases (IC50 = 5 nM). In this way, it blocks the acidification of vacuolar organelles as well as early to late endosomal transport. Concanamycin B interferes with bone resorption and maturation of CD8 T lymphocytes. It also prevents processing of major histocompatibility complex (MHC) class II precursors in human B cells, inhibiting the expression of MHC class II molecules on the cell surface.

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]

Betamethasone 21-phosphate is a synthetic glucocorticoid.1It prevents increases in macrophage and eosinophil numbers in bronchoalveolar lavage fluid (BALF) and decreases in blood leukocyte numbers in a guinea pig model of parainfluenza-3 viral infection when administered at a dose of 8 mg/kg but does not prevent airway hyperresponsiveness after infection.2Betamethasone 21-phosphate inhibits cell infiltration into the aqueous humor in a rat model of endotoxin-induced uveitis when administered topically or subcutaneously at doses of 0.01-1% or 1 mg/kg, respectively.3It increases maximal lung pressure volume curves in fetal sheep when administered to pregnant ewes at 0.75 gestation at doses of 80 and 170 μg/kg.1Betamethasone 21-phosphate increases body weight, impairs learning and memory, increases anxiolytic behavior, and reduces hippocampal neurogenesis in CD-1 mice but reduces body weight and increases neurogenesis with no effect on anxiety in high-anxiety DBA/2 mice when administered at a dose of approximately 25 mg/kg per day in the drinking water for seven weeks.4Formulations containing betamethasone 12-phosphate and betamethasone acetate have been used in the treatment of severe allergic conditions and a variety of immune-related conditions. 1.Loehle, M., Schwab, M., Kadner, S., et al.Dose-response effects of betamethasone on maturation of the fetal sheep lungAm. J. Obstet. Gynecol.202(2)186.e181-186.e187(2010) 2.Leusink-Muis, A., Ten Broeke, R., Folkerts, G., et al.Betamethasone prevents virus-induced airway inflammation but not airway hyperresponsiveness in guinea pigsClin. Exp. Allergy29(Suppl. 2)82-85(1999) 3.Tsuji, F., Sawa, K., Kato, M., et al.The effects of betamethasone derivatives on endotoxin-induced uveitis in ratExp. Eye Res.64(1)31-36(1997) 4.Aiello, R., Crupi, R., Leo, A., et al.Long-term betamethasone 21-phosphate disodium treatment has distinct effects in CD1 and DBA/2 mice on animal behavior accompanied by opposite effects on neurogenesisBehav. Brain Res.278155-166(2015)

BIIB028 is a small-molecule inhibitor of heat shock protein (Hsp) 90 with potential antineoplastic activity. Hsp90 inhibitor BIIB028 blocks the binding of oncogenic client proteins to Hsp90, which may result in the proteasomal degradation of these proteins and so the inhibition of tumor cell proliferation. Hsp90 is a molecular chaperone that plays a key role in the conformational maturation of oncogenic signaling proteins, such as Her2 Erbb2, Akt, Raf1, Bcr-Abl, and mutated p53, in addition to other molecules involved in cell cycle regulation and immune responses.

ZK-Thiazolidinone, also known as TAL, is an ATP-competitive inhibitor of PLK1. In vitro, ZK-Thiazolidinone counteracts the role of Plk1 in previously established functions, notably, sister chromatid separation, centrosome maturation, and bipolar spindle assembly. In vivo, ZK-Thiazolidinone selectively inhibits PLK1 and causes a prometaphase-like mitotic (G2–M) arrest. ZK-Thiazolidinone inhibits human PLK1 (IC50, 19± 12 nM) and various human and mouse tumor cell lines (IC50, 0.2–1.3 μM). ZK-Thiazolidinone impairs centrosome maturation.

Teclistamab(特立妥单抗)是一种人源的双特异性单克隆抗体，靶向t细胞表面表达的CD3受体和恶性多发性骨髓瘤b系细胞表面表达的b细胞成熟抗原（BCMA），用于治疗复发和难治性多发性骨髓瘤。

Pacanalotamab (AMG 420；BI-836909) 是一种双特异性 T 细胞接合剂 (BiTE)，靶向 BCMA 和 CD3ɛ。BCMA 是指 B 细胞成熟抗原，而 Pacanalotamab 会将 T 细胞重定向到细胞表面的 BCMA 表达细胞。Pacanalotamab 可对人多发性骨髓瘤 (MM) 细胞系进行 T 细胞重定向裂解。

Pavurutamab (AMG-701) 是一种抗 CD3和抗 B 细胞成熟抗原 (BCMA) 的双特异性 T 细胞接合剂分子。Pavurutamab 在 Pacanalotamab 的基础上延长了半衰期。Pavurutamab 的 Fc 与分子偶联，可改善药代动力学参数。Pavurutamab 在免疫调节和多发性骨髓瘤 (MM) 中有潜在应用。

Belantamab mafodotin (GSK2857916) 是一种靶向 B 细胞成熟抗原 (BCMA) 的抗体-药物偶联物，可增强肿瘤内免疫细胞浸润和活化，延缓肿瘤生长，可用于研究骨髓瘤。

NDNA4（compound 17）作为Hsp90α选择性抑制剂，具有0.34 μM的IC50值。作为永久带电的类似物，该化合物显示出低膜渗透性，并在Ovcar-8和MCF-10A细胞中表现出较低的细胞毒性（IC50>100 μM）。NDNA4能够保护hERG通道免遭破坏，同时不触发热休克反应或引起对Hsp90α依赖的客户蛋白进行降解。

RIOK2-IN-1 (com 4) 是一种高选择性 RIOK2 抑制剂，Kd 值为 150 nM，但其细胞活性相对低下，IC50 值达 14,600 nM。RIOK2 作为一种非典型激酶，在多种人类癌症中扮演角色，涉及核糖体成熟和细胞周期的进展。基于 RIOK2-IN-1，开发出的新型小分子抑制剂 CQ211 显示出突出的体内外活性，能有效抑制 MKN-1 和 HT-29 癌细胞增殖，并在小鼠异种移植的 MKN-1 模型中抑制了肿瘤的发展。

FF-MAS是一种有效的meiotic maturation激动剂，能促进小鼠卵母细胞在体外成熟，促进其发展到MII阶段，并增强从2细胞阶段到囊胚阶段转变的潜力。

Azintuxizumab 是一种 IgG4 双特异性抗体，专门识别并结合浆细胞恶性肿瘤相关分子标志 BCMA (B-cell maturation antigen)。Azintuxizumab 在复发或难治性多发性骨髓瘤 (RRMM) 的临床前与转化研究中表现出显著潜力，为基于抗体的免疫研究供了双重作用机制。

Elranatamab (PF-06863135) 是针对人源化 B 细胞成熟抗原 (BCMA) 和 CD3 的双特异性抗体。通过靶向骨髓瘤细胞上的 BCMA 和 T 细胞上的 CD3，Elranatamab 能激活 T 细胞并引导其产生针对骨髓瘤细胞的细胞毒性反应。此抗体主要用于研究复发或难治性多发性骨髓瘤。

BCMA72-80 is an HLA-A2-specific B-cell maturation antigen (BCMA) peptide with a strong affinity for HLA-A2, and is employed in research on multiple myeloma or other tumors expressing B-cell maturation antigen.

BCMA72-80 acetate(2293841-58-2 free base) 是一种 HLA-A2 特异性 B 细胞成熟抗原 (BCMA) 肽。它用于研究表达 B 细胞成熟抗原的多发性骨髓瘤和肿瘤。

ABBV-383 (ABBV-383)为BCMA×CD3双特异性T细胞结合器 (BiTE)，旨在抑制B细胞成熟蛋白活性 (BCMA) 并激活T细胞表面的CD3复合体糖蛋白。该化合物主要应用于多发性骨髓瘤、免疫球蛋白轻链淀粉样变性以及心血管疾病的研究领域。