caspase-dependent

KY-05009 是 ATP 竞争性的、有效的 TNIK 抑制剂，Ki 为 100 nM。KY-05009抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制TNIK 的蛋白表达和Wnt 靶基因的转录活性，并诱导癌细胞凋亡，显示抗癌活性。

PAF (C16) 是有效的 MAPK 和 MEK ERK 激活剂，可诱导血管通透性增加。PAF (C16) (PAF (C16)) 是血小板活化因子，是一种磷脂衍生介质，也是 PAF G 蛋白偶联受体 (PAFR) 的配体。PAF (C16) 在体外实验中显示出抗凋亡和抗炎活性，通过与其受体 （PAF-R） 相互作用以执行细胞信号传导来抑制 caspase 依赖性凋亡。

BIM-46174 是一种5,6,7,8-四氢咪唑[1,2-a]吡嗪衍生物，抑制异源三聚体 Galpha Gbetagamma 蛋白复合物，具有抗癌活性，可抑制大量人类癌细胞系的生长，诱导 caspase-3 依赖性癌细胞凋亡，诱导聚 （ADP-核糖） 聚合酶裂解。

(-)-Anonaine 可从木兰科和安妮科的几个物种中提取出来，具有抗疟、抗菌、抗真菌、抗氧化、抗癌、抗抑郁和血管舒张的活性。(-)-Anonaine 通过 Bax 和 caspase 依赖性途径诱导人类宫颈癌（HeLa）细胞的凋亡，诱导 DNA 损伤并抑制人类肺癌 h1299细胞的生长和迁移。

OUP-186 is a high affinity and human rat species-selective antagonist of histamine H3 receptor. OUP-186 suppressed the proliferation of breast cancer cells. The IC50 values at 48 hours for OUP-186 was approximately 50 μM. OUP-186 potently induced cell dea

Talabostat (PT100, Val-boroPro) is a potent, nonselective and orally available dipeptidyl peptidase IV (DPP-IV) inhibitor with a Ki of 0.18 nM. Talabostat is a nonselective DPP-IV inhibitor, inhibiting DPP8 9, FAP, DPP2 and some other DASH family enzymes essentially as potently as it inhibits DPP-IV[1]. Talabostat stimulates the immune system by triggering a proinflammatory form of cell death in monocytes and macrophages known as pyroptosis. The inhibition of two serine proteases, DPP8 and DPP9, activates the proprotein form of caspase-1 independent of the inflammasome adaptor ASC[2]. Talabostat competitively inhibits the dipeptidyl peptidase (DPP) activity of FAP and CD26 DPP-IV, and there is a high-affinity interaction with the catalytic site due to the formation of a complex between Ser630 624 and the boron of talabostat[3]. Talabostat can stimulate immune responses against tumors involving both the innate and adaptive branches of the immune system. In WEHI 164 fibrosarcoma and EL4 and A20 2J lymphoma models, PT-100 causes regression and rejection of tumors. The antitumor effect appears to involve tumor-specific CTL and protective immunological memory. Talabostat treatment of WEHI 164-inoculated mice increases mRNA expression of cytokines and chemokines known to promote T-cell priming and chemoattraction of T cells and innate effector cells[3]. Talabostat treated mice show significant less fibrosis and FAP expression is reduced. Upon PT100 treatment, significant differences in the MMP-12, MIP-1α, and MCP-3 mRNA expression levels in the lungs are also observed. Treatment with PT100 in this murine model of pulmonary fibrosis has an anti-fibro-proliferative effect and increases macrophage activation[4]. [1]. Connolly BA, et al. Dipeptide boronic acid inhibitors of dipeptidyl peptidase IV: determinants of potencyand in vivo efficacy and safety. J Med Chem. 2008 Oct 9;51(19):6005-13. [2]. Okondo MC, et al. DPP8 and DPP9 inhibition induces pro-caspase-1-dependent monocyte and macrophage pyroptosis. Nat Chem Biol. 2017 Jan;13(1):46-53. [3]. Adams S, et al. PT-100, a small molecule dipeptidyl peptidase inhibitor, has potent antitumor effects and augments antibody-mediated cytotoxicity via a novel immune mechanism. Cancer Res. 2004 Aug 1;64(15):5471-80. [4]. Egger C, et al. Effects of the fibroblast activation protein inhibitor, PT100, in a murine model of pulmonary fibrosis. Eur J Pharmacol. 2017 Aug 15;809:64-72.

Glaucocalyxin A (Leukamenin F) 是来自日本黑纹病菌的一种对映型月桂基二萜，具有抗肿瘤作用。它通过调节PI3K Akt 信号通路抑制 GLI1 的核易位，诱导骨肉瘤凋亡。

CIL62 是一种不依赖 caspase-3 7 的细胞死亡诱导剂。CIL62的作用机制是 Necrostatin-1 依赖性细胞死亡。

BJE6-106 (B106) is a potent, selective PKCδ inhibitor (IC50: 0.05 μM) and targets selectivity over classical PKCα (IC50: 50 μM). BJE6-106 induces caspase-dependent apoptosis with tumor-specific effect.

Destruxin B is a cyclic peptide with insecticidal and anticancer activity isolated from the insect pathogenic fungus Metarhizium isopliae. Destruxin B induces apoptosis of human non-small cell lung cancer cells through the Bcl-2 family-dependent mitochond

Eltanexor (ONO-7706) 是一种具有口服活性的 exportin-1 (XPO1) 抑制剂。它具有有效的抗白血病活性。 Eltanexor 通过直接靶向 XPO1 抑制 XPO1 依赖性核输出 (EC50=60.9 nM)。 Eltanexor 在一组白血病细胞系中引起半胱天冬酶依赖性细胞凋亡。

Mensacarcin, a highly complex polyketide compound, exhibits multifaceted effects on cellular processes. Specifically, it targets mitochondria, perturbs energy metabolism within these organelles, and activates caspase-dependent apoptotic pathways. Functionally, Mensacarcin can serve as a cytotoxic constituent in antibody-drug conjugates (ADCs). Furthermore, this antibiotic compound displays broad-spectrum inhibition of cell growth across various cancer cell lines and demonstrates potent induction of apoptosis in melanoma cells.

PETCM is a caspase-3 activator and acts as an cytochrome c (cyto c)-dependent manner.

15-Acetoxyscirpenol, a member of the acetoxyscirpenol moiety mycotoxins (ASMs), potently induces apoptosis and inhibits the growth of Jurkat T cells in a dose-dependent manner. This effect is mediated through the activation of caspases independent of caspase-3[1].

A-1155905是一种MCL-1抑制剂，表现出抗癌活性，其IC50值为33.5 Nm，Ki值为0.58 nM。该化合物选择性地与MCL-1蛋白结合，能够有效破坏活细胞中的MCL-1-bim复合物。此外，A-1155905诱导MCL-1依赖性细胞系的死亡，该过程依赖于半胱天冬酶蛋白（caspase）并通过凋亡机制（apoptosis）实现。

EGFR-IN-137 (Compound 4c) 是一种抑制芳香化酶 (aromatase) 和 EGFR 的化合物，IC50 值分别为 1.67 μg mL 和 0.08 μg mL。该化合物能抑制 MCF-7 和 MDA-MB-231 癌细胞的增殖，IC50 分别为 1.62 µM 和 4.14 µM。EGFR-IN-137 还可使 MDA-MB-231 细胞周期停滞在 G0 G1 期，并通过 caspase 依赖性途径诱导细胞凋亡 (apoptosis)。

MAPK-IN-3 (Compound 4a) 是一种抗增殖剂，特别对 KYSE 30、HCT 116 和 HGC 27 具有强效抑制作用，其 IC50 分别为 0.57 μM、3.27 μM 和 2.28 μM。通过 p53 依赖机制，MAPK-IN-3 阻滞细胞周期，并通过 p53 非依赖机制诱导细胞凋亡。该化合物下调细胞周期相关蛋白（如 Cyclin D1 和 Cyclin B1）的表达，上调促凋亡蛋白（如裂解 PARP、裂解 caspase-7 和裂解 caspase-9）的表达，减少抗凋亡蛋白（如 Bcl-2）的表达，增加 KYSE 30 细胞内的 ROS 水平，并上调与 ROS 相关的 MAPK 信号通路成员（如 p-ERK、p-p38 和 p-JNK）的表达。

Apoptosisinducer 31 (compound 19) 诱导caspase依赖性细胞凋亡 (apoptosis)，在癌症研究中具有重要作用。

ZIF-8 是抗癌剂，通过 caspase-1 gasdermin D (GSDMD) 依赖途径在细胞内引发焦亡 (pyroptosis)。

MMPSI (Caspase-3 7 Inhibitor I) 是一种新型的、非肽类的小分子 caspase 3 和 caspase 7 抑制剂，可减少离体兔心脏或心肌细胞缺血性损伤的作用，以浓度依赖性方式抑制 H16c2 细胞凋亡 。MMPSI 可用于研究心脏保护和心肌损伤。

PB28 dihydrochloride 是一种具有选择性和高效性的 sigma 2 (σ2) 受体激动剂和 σ1 受体拮抗剂，具有抗 SARS-CoV-2 活性和抗肿瘤活性，通过调节肾癌中的 PI3K-AKT-mTOR 信号通路来抑制细胞增殖和侵袭，抑制 SK-N-SH 神经母细胞瘤细胞内质网中的钙释放，可诱导非 caspase 依赖性的细胞凋亡。

Nolatrexed dihydrochloride (Thymitaq) 是一种非竞争性的胸苷酸合酶抑制剂，能够在癌细胞 S 期诱导细胞周期停滞，具有抗癌活性。它与该酶的叶酸辅因子结合位点相互作用，对人胸苷酸合酶的Ki 值为 11 nM。

Dihydrocelastrol is synthesized by hydrogenation of celastrol, a treterpene isolated from Chinese medicinal plant Tripterygium regelii. Dihydrocelastrol could inhibit cell proliferation and promote apoptosis through caspase-dependent way in vitro. DHCE co

NLRP3-IN-9 (INF-4E) 是 NLRP3 ATPase 和 caspase-1 的抑制剂。 NLRP3-IN-9 通过不可逆地捕获硫醇亲核体发挥作用，以时间和浓度依赖性方式防止 ATP 和尼日利亚菌素触发的人 THP-1 细胞焦亡。