Apoptosis

KPT-6566 is a covalent PIN1 inhibitor that selectively targets cancer cells by a dual mechanism of action.

AFG206 is the novel first-generation type II" FLT3 inhibitor."

Mitochondrial release of cytochrome c triggers apoptosis via the assembly of a multimeric complex including caspase-9, Apaf-1, and other components, sometimes called the apoptosome. Library screens have identified small molecules that activate the apoptosome by binding to one or more of its components. CAY10443 is one such molecule. In a cell free, multi-component assay, it activated caspase-3 with an EC50 of 5 μM. These apoptotic activators represent therapeutic lead compounds for the development of antitumor drugs.

Dapivirine HCl is the salt form of Dapivirine, also known as TMC120, a non-nucleoside inhibitor for HIV reverse transcriptase with IC50 of 24 nM. The HIV-1 replication inhibitor dapivirine (DPV) is one of the most promising drug candidates being used in topical microbicide products for prevention of HIV-1 sexual transmission.

ABI-231 is a potent, orally bioavailable tubulin inhibitor that interacts with the colchicine binding site and is currently undergoing clinical trials for prostate cancer. ABI-231, has an average IC50 = 5.2 nM against panels of melanoma and prostate cancer cell lines, is orally bioavailable, and strongly suppress melanoma tumors in vivo. ABI-231 holds great promise as a new generation of orally available tubulin inhibitor.

Dichloroacetate (DCA) is an inhibitor of all pyruvate dehydrogenase kinase (PDHK) isoforms, which are enzymes that phosphorylate and inhibit PDH in mitochondria. Inhibition of PDHK shifts cell metabolism from glycolysis to mitochondrial glucose oxidation, an effect that has relevance to cancer, type 2 diabetes, and other diseases. CAY10703 is a DCA trimer that is at least 10-fold more cytotoxic against leukemia cell lines than DCA. It is approximately 3-fold less cytotoxic than DCA against peripheral blood mononuclear cells from healthy blood donors. CAY10703 significantly reduces both basal and maximal respiration in leukemia cells. It is stable in vivo after subcutaneous inoculation, remaining in circulation for more than five hours after injection.

Inhibitor of microtubule polymerization in vitro. Interacts with tubulin dimers and promotes the accumulation of mammalian cells in apoptosis. Potentiates antiproliferative effects of vinblastine in H2B-GFP HeLa cells. Originally thought to inhibit CENP-E ATPase activity. Tcherniuk et al (2011) UA62784 is a cytotoxic inhibitor of microtubules, not CENP-E. Chem.Biol. 18 631 PMID:21609844 |Maiato and Logarinho et al (2011) Motor-dependent and -independent roles of CENP-E at kinetochores: the cautionary tale of UA62784. Chem.Biol. 18 679 PMID:21700202

Tomatine hydrochloride is an alkaloid that occurs in the extract of leaves of wild tomato plants. It inhibits the growth of many fungi and bacteria. It is used as a precipitating agent for steroids.

AG-205 is a potent inhibitor of FabK, the enoyl-ACP reductase in Streptococcus pneumoniae.

CHS-828 nicotinate is a CHS-828 salt with Nicotinic acid.. CHS-828 also known as GMX-1778, is a potent and selective NAMPT inhibitor. CHS-828 inhibits cellular synthesis of NAD. CHS 828 kill tumour cells by inhibiting the nuclear factor-kappaB translocation but unlikely through down-regulation of proteasome. CHS 828 has shown promising anticancer activity in experimental tumor models and primary cultures of cancer cells from patients. CHS 828 showed a synergistic effect with melphalan in 67%, doxorubicin in 47%, etoposide in 38% and Ara-C in 14% of AML samples.

Ethylene glycol dimethacrylate 是一种具有细胞毒性和基因毒性作用的甲基丙烯酸酯单体。它可增加人牙龈成纤维细胞 (HGF) 内的活性氧 (ROS) 产生，引发 DNA 损伤和细胞凋亡 (apoptosis)，并使细胞周期在 G1/G0 期停滞。

Luteolin (monohydrate) is the hydrated form of Luteolin, a flavonoid that acts as a potent Nrf2 inhibitor. It possesses anti-inflammatory and anticancer properties, induces apoptosis and cell cycle arrest in multiple human cancer cell lines, including non-small lung cancer cells, and inhibits cell metastasis and angiogenesis [1].

Lambertianic acid is a bioactive chemical that has anti-allergic and antibacterial effects.

ALC67 has a promising anticancer activity that results in the recent discovery of a series of 3-propionyl thiazolidine-4-carboxylic acid ethyl esters as a family of novel antiproliferative agents. It is an activator of the caspase-9 involved apoptotic pat

Deoxynybomycin, a selective anti-tumor agent, inhibits topoisomerase I and induces apoptosis.

MEB55, an anticancer agent, acts by disrupting DNA repair and halting growth in prostate, colon, lung and breast cancer cells.

SMBA2 is a Bax activator. It acts by specifically targeting the binding pocket at S184.

INU-152 is a pan-RAF inhibitor. INU-152 has potent anti-tumor activity in preclinical models of BRAFV600E mutant cancer. INU-152 inhibits all RAF isoforms and inhibits MAPK pathways in mutant BRAF cells. INU-152 exhibits minimal paradoxical pathway activa

WF 10129 is a new angiotensin converting enzyme inhibitor generated by a fungus, Doratomyces putredinis.

Antitumor agent-184 (compound 12aa) 通过诱导细胞凋亡 (apoptosis) 显示出显著的抗肿瘤活性，其在 B16-F10 细胞、4T1 细胞和 CT26 细胞中的IC50值分别达到 2.35 μM、7.32 μM 和 10.31 μM。

SPI-001作为PPM1D特异性抑制剂（IC50=0.48 μM），展现出其抗癌能力。它能够抑制PPM1D过表达的人类乳腺癌细胞里的PPM1D磷酸酶活性，并促进p53的磷酸化。此外，SPI-001通过诱导细胞凋亡(apoptosis)的方式来抑制癌细胞的增殖。

Stellettin B，一种从海洋海绵 Jaspis stellifera 分离的三萜化合物，通过阻断 PI3K/Akt/mTOR 通路，能诱导人非小细胞肺癌 A549 细胞的 G1期阻滞、凋亡 (apoptosis) 及自噬 (autophagy)。此外，该化合物还能通过抑制 MAPK 和 FAK/PI3K/AKT/mTOR 信号通路来减少肝癌细胞的迁移和侵袭。Stellettin B 主要应用于多种肿瘤的研究领域。

5-Fluoroindole 是一种抗菌剂，能抑制 Mycobacterium tuberculosis，MIC 为 4.7 μM。在大鼠肝微粒体中，5-Fluoroindole 表现出代谢稳定性，并且在小鼠体内展现出抗结核活性。

Thalidomide-5-PEG4-NH2 是一类合成的 E3 连接酶配体-linker 偶联物，结合了基于 Thalidomide 的 cereblon 配体以及一个 linker。

Thalidomide-PEG5-NH2 是一种合成的 E3 连接酶配体-linker 偶联物，由基于 Thalidomide 的 cereblon 配体和一个 linker 组成。

Thalidomide-NH-amido-C3-NH2 是一种合成的 E3 连接酶配体-linker 偶联物，由 Thalidomide 基于 cereblon 的配体和一个 linker 组成，适用于PROTAC的合成。

Thalidomide-5-PEG3-NH2 是一种合成的 E3 连接酶配体-linker 偶联物，包含 Thalidomide 衍生的 cereblon 配体和一个 linker。

Thalidomide-O-amide-C5-NH2 TFA 是一种合成的 E3 连接酶配体-linker 偶联物，由 Thalidomide 衍生的 cereblon 配体组成，并结合了一个 linker，可用于合成 PROTAC。

Thalidomide-PEG3-NH2 hydrochloride 是一种Thalidomide基础上的cereblon配体，用于招募CRBN蛋白。它能够通过linker与目标蛋白配体结合，生成PROTAC分子，例如THAL-SNS-032。

Danshensu (Dan shen suan A) sodium 是一种口服生物活性的酚类化合物，能够激活Nrf2/HO-1通路并抑制NF-κB信号。它可降低活性氧 (ROS) 的生成，提升抗氧化防御系统，并阻断内在细胞凋亡途径。Danshensu sodium 对SARS-CoV-2展示出显著抗病毒效果，EC50为0.97 μM。它兼具抗氧化、抗凋亡和抗肺炎症的特性，具备用于研究COVID-19和心脑血管疾病的应用潜力。

Axl-IN-18 (compound 25c) 是一种高效、选择性的 II 型 AXL 抑制剂，展现出卓越的AXL抑制活性 (IC50=1.1 nM)，其选择性比具高度同源性的激酶 MET (IC50=377 nM) 高343倍。Axl-IN-18 能显著抑制由 AXL 驱动的细胞增殖，并剂量依赖性地抑制 4T1 细胞的迁移和侵袭，还可诱导细胞凋亡。在 BaF3/TEL-AXL 异种移植模型中，Axl-IN-18 显示出显著的抗肿瘤效能。

Glyphosate isopropylammonium 是非选择性、广谱活性的系统性杀生物剂，是氨基酸甘氨酸的除草衍生物。它通过抑制莽草酸途径中 5-内丙酮酰莽草酸 3-磷酸合酶 (EPSPS) 的酶活性，阻止芳香族氨基酸如酪氨酸、苯丙氨酸和色氨酸的合成。Glyphosate isopropylammonium 会引发氧化应激、神经炎症以及线粒体功能障碍，导致神经元由于自噬、坏死或凋亡而死亡，并引发行为和运动障碍。

2E-3-F16 是一种抗癌剂。在 NCI-H446 癌细胞和 HBE 细胞之间，2E-3-F16 显示出对肿瘤细胞的选择性。此外，2E-3-F16 可增强 A549 细胞对 Cisplatin 的敏感性。

PROTACPI3K/110β degrader-2 是一种针对PI3K/p110β的选择性PROTAC降解剂。该化合物能够有效降解110β蛋白，抑制P-糖蛋白的表达，并提升活性氧(ROS)水平。同时，PROTACPI3K/110β degrader-2 通过激活内质网应激 (ERS) 所介导的线粒体凋亡路径以及抑制AKT/Bcl-2信号通路，发挥其抗肿瘤作用。此化合物适用于癌症研究。

NEP162 是一种BRD4 PROTAC降解剂，在 SW480 和 U2OS 细胞中的DC50值分别为 1.2 μM 和 1.6 μM。它展现出抗增殖活性，能够有效抑制肿瘤生长并诱导细胞凋亡 (apoptosis)。NEP162 可用于骨肉瘤、结直肠癌和非小细胞肺癌等癌症的研究。

PROTACHER2 degrader-1 是一种高度选择性的HER2 PROTAC降解剂，具有DC50比值为69 nM，Dmax为96%。它通过持续降解HER2并有效抑制下游通路（AKT和ERK），从而抑制HER2阳性细胞的增殖和肿瘤生长，同时可诱导BT-474细胞凋亡（apoptosis）。该化合物可用于HER2阳性癌症的研究。