senescence

Rosiglitazone (BRL49653) 是一种 PPARγ 激动剂、TRPC5 激活剂和 TRPM3 抑制剂，具有口服活性。Rosiglitazone 也是一种降糖剂，是噻唑烷二酮类胰岛素增敏剂。

Rosiglitazone hydrochloride (BRL-49653 HCl) 是一种降血糖药物，通过与脂肪细胞中的 PPAR 受体结合来刺激胰岛素分泌。它对 PPARγ1、PPARγ2 和 PPARγ 的EC50值分别为 30 nM、100 nM 和 60 nM。它也是TRPC5的激活剂和TRPM3的抑制剂。

SBI-797812 是在结构上类似于活性位点定向的 NAMPT 抑制剂的化合物，能够阻断这些抑制剂与 NAMPT 的结合。 它将 NAMPT 反应平衡转向 NMN 形成，提高 NAMPT 对 ATP 的亲和力，稳定 His247 处的磷酸化 NAMPT，增加焦磷酸盐副产物的消耗，并通过 NAD+钝化反馈抑制。

Milademetan (DS-3032) 是一种具有口服活性和有效性的 MDM2 抑制剂，具有抗肿瘤活性，诱导 G1 细胞周期阻滞、衰老和凋亡。Milademetan 可用于研究急性髓系白血病和实体肿瘤。

p38 MAPK Inhibitor 是p38 MAPK 激酶的有效抑制剂（IC50＝ 35 nM）。p38 MAPK Inhibitor 抑制癌基因RAS 诱导的衰老。

RH1 (NSC 697726) 是一种生物还原性抗癌化合物，在体外表现出剂量依赖性双相效应，在较高剂量下诱导细胞凋亡，在较低剂量下诱导衰老。

1-Aminocyclopropane-1-carboxylic acid (ACC) 是内源性代谢产物的一种。

D-Galactose (Alpha-D-galactose) 属于天然己糖，与葡萄糖结合构成乳糖。D-Galactose 常被用于构建动物衰老模型。

Rupatadine (UR-12592) is a potent dual PAF H1 antagonist with Ki of 0.55 0.1 uM(rabbit platelet membranes guinea pig cerebellum membranes).IC50 value:Target: PAF H1 antagonistin vitro: Rupatadine competitively inhibited histamine-induced guinea pig ileum contraction (pA2 = 9.29 + - 0.06) without affecting contraction induced by ACh, serotonin or leukotriene D4 (LTD4). It also competitively inhibited PAF-induced platelet aggregation in washed rabbit platelets (WRP) (pA2 = 6.68 + - 0.08) and in human platelet-rich plasma (HPRP) (IC50 = 0.68 microM), while not affecting ADP- or arachidonic acid-induced platelet aggregation [1]. The IC50 for rupatadine in A23187, concanavalin A and anti-IgE induced histamine release was 0.7+ -0.4 microM, 3.2+ -0.7 microM and 1.5+ -0.4 microM, respectively whereas for loratadine the IC50 was 2.1+ -0.9 microM, 4.0+ -1.3 M and 1.7+ -0.5 microM. SR-27417A exhibited no inhibitory effect [2].in vivo: Rupatadine blocked histamine- and PAF-induced effects in vivo, such as hypotension in rats (ID50 = 1.4 and 0.44 mg kg i.v., respectively) and bronchoconstriction in guinea pigs (ID50 = 113 and 9.6 micrograms kg i.v.). Moreover, it potently inhibited PAF-induced mortality in mice (ID50 = 0.31 and 3.0 mg kg i.v. and p.o., respectively) and endotoxin-induced mortality in mice and rats (ID50 = 1.6 and 0.66 mg kg i.v.) [1]. rupatadine treatment improved the declined lung function and significantly decreased animal death. Moreover, rupatadine was able not only to attenuate silica-induced silicosis but also to produce a superior therapeutic efficacy compared to pirfenidone, histamine H1 antagonist loratadine, or PAF antagonist CV-3988 [3]. [1]. Merlos M, et al. Rupatadine, a new potent, orally active dual antagonist of histamine and platelet-activating factor (PAF). J Pharmacol Exp Ther. 1997 Jan;280(1):114-21. [2]. Queralt M, et al. In vitro inhibitory effect of rupatadine on histamine and TNF-alpha release from dispersed canine skin mast cells and the human mast cell line HMC-1. Inflamm Res. 2000 Jul;49(7):355-60. [3]. Lv XX, et al. Rupatadine protects against pulmonary fibrosis by attenuating PAF-mediated senescence in rodents. PLoS One. 2013 Jul 15;8(7):e68631.

TM5441 是口服生物可利用的纤溶酶原激活物抑制剂-1 抑制剂，抑制多个癌症细胞系的 IC50值在 13.9 到 51.1 μM。它诱导几种人类癌症细胞的内在调亡，减弱 Nω-硝基-1-精氨酸甲酯诱导的心脏高血压和血管衰老。

CTX-0124143 是一种组蛋白乙酰转移酶抑制剂，对 KAT6A 的 IC50 值为 1.0μM。CTX-0124143 可用于研究细胞衰老。

FKB04，作为一种端粒重复结合因子2（TRF2）抑制剂，在肝癌研究领域显示出潜力。通过破坏肝癌细胞的端粒维持机制，FKB04 诱导端粒缩短和细胞衰老，因而引发 T 环缺陷，发挥抗肿瘤活性。此外，该化合物还能抑制人肝癌异种移植小鼠模型（Huh-7 细胞植入 BALB c 小鼠）中的肿瘤生长。

SLCB050 是一种抗肿瘤化合物，能够阻断DX2与p14 ARF间的交互作用。该化合物特别针对人类小细胞肺癌细胞，通过p14 ARF依赖机制抑制其活性，并诱导细胞凋亡 (apoptosis) 及衰老。

BIMAX1 acetate 用作实验工具肽，用于研究 RBBP4 与核输入蛋白 (Importin) β1 之间的相互作用，并考察其对核输入途径的影响。此外，该化合物亦被应用于探索 RBBP4 在核输入效率及细胞衰老调控中的功能。

MRTF-A-IN-2（compound 16）作为一种MRTF-A抑制剂，具有抑制细胞增殖并诱导HCC细胞衰老的功能。

Cristacarpin exhibits moderate but selective activity towards DNA repair-deficient yeast mutants. It promotes endoplasmic reticulum (ER) stress, leading to sub-lethal reactive oxygen species (ROS) generation and which eventually terminates by triggering s

1-DCP 是一种抑制果实成熟和衰老作用中乙烯功能的有效乙烯拮抗剂。

TM5441是一种口服生物可利用的PAI-1(纤溶酶原激活物抑制剂-1)抑制剂，其对多种癌症细胞系的IC50值介于13.9到51.1μM之间，能诱导人类癌症细胞的内在凋亡(apoptosis)。此外，TM5441还可减轻Nω-硝基-1-精氨酸甲酯引发的心脏高血压和血管老化。

Sphynolactone-7 (SPL7) acts as an agonist for the Striga hyposensitive to light receptor 7 (ShHTL7) found in the parasitic plant Striga hermonthica. SPL7 selectively targets ShHTL7 with an IC50 of 0.31 µM, demonstrating higher specificity compared to ShHTL2-6, ShHTL9-10, and the strigolactone receptor AtD14 at a concentration of 10 µM, though it still inhibits ShHTL8 and ShHTL11 with IC50s of 1.2 and 7.8 µM, respectively. This compound triggers fatal germination of Striga hermonthica seeds in the absence of a host by inducing suicidal germination at a minimum effective concentration of 10 fM. Additionally, SPL7 can reduce the emergence of this obligate parasite from the soil and alleviate Striga hermonthica-induced senescence in maize when applied at a 10 nM concentration to the soil of maize and Striga hermonthica seed co-cultures.

Sirtuin-1 inhibitor 1 是一种针对去乙酰化酶-1（Sirtuin-1）的抑制剂，可用于研究机体的衰老和细胞的死亡。

Boanmycin 是一种具有抗肿瘤活性的抗生素，可以诱导细胞衰老、凋亡 (apoptosis)。

FAK-IN-12（Compound 12S）为FAK抑制剂，具有47 nM的IC50值。该化合物对MGC-803、HCT-116及KYSE30细胞系的增殖具有抑制作用（IC50值分别为0.24、0.45、0.44 μM），并可诱导细胞凋亡和细胞衰老。

JTP-4819 is a potent and selective prolyl endopeptidase (PEP) inhibitor with potential for treating Alzheimer's disease. At nanomolar concentration, JTP-4819 inhibited the degradation of substance P, arginine-vasopressin, and thyrotropin-releasing hormone by PEP in supernatants of the rat cerebral cortex and hippocampus. Repeated administration of JTP-4819 reversed the aging-induced decrease in brain substance P-like and thyrotropin-releasing hormone-like immunoreactivity, suggesting that this drug may be able to improve the imbalance of peptidergic neuronal systems that develops with senescense by inhibiting PEP activity. JTP-4819 increased acetylcholine release from the frontal cortex and hippocampus, regions closely associated with memory, in both young and aged rats.

BML-278 是一种 SIRT1 激活剂 ，EC150 值为 1 μM。BML-278 增加父本和母本原核中的 H3K9 甲基化并抑制 H3K9 乙酰化，可用于改善早期胚胎发育。BML-278 促使原代人间充质细胞的细胞周期停止在 G1 S 期，可用于延缓衰老。BML-278 减少 U937 细胞中的微管蛋白乙酰化，增加小鼠 C2C12 成肌细胞的线粒体密度。