Apoptosis

Tetrachlorohydroquinone (TCHQ) is a metabolite of the organochlorine biocide pentachlorophenol. It is cytotoxic to RTL-W1 rainbow trout liver cells (EC50 = 1.55 μM in a neutral red assay). TCHQ increases production of reactive oxygen species (ROS), inhibits apoptosis, and induces loss of the mitochondrial membrane potential and necrosis in splenocytes. In vivo, TCHQ induces glutathione (GSH) depletion in mouse liver.

9(E),11(E),13(E)-Octadecatrienoic acid (β-ESA) is a conjugated polyunsaturated fatty acid that is found in plant seed oils and in mixtures of conjugated linolenic acids synthesized by the alkaline isomerization of linolenic acid. It reduces growth of Caco-2 colon cancer cells in a dose-dependent and time-dependent manner. In vitro, β-ESA induces DNA fragmentation and upregulation of pro-apoptotic Bax mRNA. β-ESA decreases protein expression of the apoptosis suppression factor Bcl-2 and induces apoptosis in T24 bladder cancer cells via production of reactive oxygen species. It also inhibits bacterial fatty acid dioxygenase with a Ki value of 49 nM in vitro.

C6 urea ceramide is an inhibitor of neutral ceramidase.1 It increases total ceramide levels in wild-type mouse embryonic fibroblasts (MEFs) and in HT-29 colon cancer cells but not in MEFs lacking neutral ceramidase. It inhibits proliferation of, and induces apoptosis and autophagy in HT-29, but not non-cancerous RIE-1, cells when used at concentrations of 5 and 10 μM. C6 urea ceramide decreases total β-catenin, increases phosphorylated β-catenin, and induces colocalization of β-catenin with the 20S proteasome in HT-29 and HCT116, but not RIE-1, cells. It reduces tumor growth and increases C16, C18, C20, and C24 ceramide levels in tumor tissue in an HT-29 mouse xenograft model when administered at doses of 1.25, 2.5, and 5 mg/kg for five days. |1. García-Barros, M., Coant, N., Kawamori, T., et al. Role of neutral ceramidase in colon cancer. FASEB J. 30(12), 4159-4171 (2016).

GSK-2256098 HCl is a focal adhesion kinase-1 (FAK) inhibitor with potential antiangiogenic and antineoplastic activities.

Ap2A (disodium) 为一种对称双核苷多磷酸化合物，具有促进血管平滑肌细胞增殖的功能。

Cis-4-Hydroxycinnamic Acid is a natural product.

KU-0058948 hydrochloride is a potent and specific PARP1 inhibitor with an IC 50 of 3.4 nM, and it exhibits anticancer effects [1].

Cyclopentenylcytosine（CPC）是一种核苷类似物，通过抑制CTP合成酶来降低白血病细胞中的胞苷三磷酸（CTP）和脱氧胞苷三磷酸（dCTP）水平。此外，Cyclopentenylcytosine 促进 1-β-D-阿拉伯核糖甘露苷胞苷(araC)的磷酸化并增加其插入DNA的活性。Cyclopentenylcytosine 以浓度（50-300 nM）和时间依赖（8-16小时）的方式诱导人T淋巴细胞系MOLT-3的凋亡和坏死。Cyclopentenylcytosine与araC联合使用可以增强对凋亡和坏死的诱导作用及其在T淋巴母细胞中的细胞毒性。

Peanut procyanidin A，一种从花生皮提取的A型原花青素，通过MAPKs信号通路能够保护前列腺DU145细胞，抵御H2O2引起的氧化应激伤害，同时减少细胞周期阻滞和细胞凋亡(apoptosis)。此外，该化合物还能在DSS诱发的溃疡性结肠炎模型小鼠中调节肠道菌群和代谢。

YF-Mo1 (compound 9) acts as a CBR1 inhibitor with an IC 50 value of 1.1 μM [1].

Monomethyl auristatin E (GMP)是 Monomethyl auristatin E 的 GMP 级别试剂。Monomethyl auristatin E 是一种海兔毒素 10 的合成衍生物，是一种抗有丝分裂剂，通过阻断微管蛋白的聚合来抑制细胞分裂，并且还具有抑制抗体-药物偶联物的活性。

PROTACBcl-xL degrader-4 (Compound 2-38-III) 是一种针对Bcl-xL的PROTAC降解剂，在HepG2细胞和HUVEC细胞中展现出显著的抗肿瘤作用。该化合物通过降低线粒体膜电位和激活MAPK信号通路来诱导细胞凋亡 (apoptosis)，并能明显抑制异种移植肿瘤小鼠模型中的肿瘤生长。

FLT3-IN-32 hydrochloride是一种高效且可口服的FLT3抑制剂，针对FLT3-ITD、FLT3-D835Y和FLT-N676K的IC50分别为0.29 nM、0.77 nM和2.07 nM。它通过减少FLT3及其下游信号分子 (STAT5、MAPK、AKT) 的磷酸化，诱导FLT3突变Ba/F3细胞凋亡 (apoptosis)。在MV4-11异种移植模型中，FLT3-IN-32 hydrochloride展现出强大的抗肿瘤效果。此化合物可用于急性髓性白血病 (AML) 的研究。

5,6,7,8,4'-Pentahydroxyflavone (Compound 2b) 是一种具有抗肿瘤活性的黄酮类化合物。5,6,7,8,4'-Pentahydroxyflavone 通过抑制细胞增殖和诱导细胞凋亡，发挥其细胞毒性作用。

ASX-173 是一种口服活性的天冬酰胺合成酶 (ASNS) 抑制剂，其IC50值为0.113 μM，Ki值为0.4 nM。ASX-173 增强L-Asparaginase (ASNase) 的抗癌作用，并与后者协同作用破坏核苷酸合成，诱导白血病细胞的周期停滞、凋亡 (apoptosis) 和自噬 (autophagy)。合并使用ASX-173与ASNase能够延缓OCI-AML2异种移植瘤的增长。该化合物适用于研究急性淋巴细胞白血病、急性髓性白血病以及结直肠癌等癌症。

Mal-N(Me)-C6-N(Me)-PNU-159682 (Compound 27) 是一种用于ADC的活性分子-偶联物，由ADC接头 Mal-N(Me)-C6-N(Me) 和有效的ADC细胞毒素 PNU-159682 组成。此化合物通过组织蛋白酶 B 裂解接头选择性地将有效载荷递送到表达 CD46 的细胞中，释放 PNU-159682，从而诱导 DNA 损伤和细胞凋亡 (apoptosis)。在非小细胞肺癌 (NSCLC) 和结直肠癌 (CRC) 异种移植 (PDX) 模型中，Mal-N(Me)-C6-N(Me)-PNU-159682 表现出持久的肿瘤消退效果。

Glucopiericidin A 是一种天然哌啶菌素化合物，来源于海洋衍生的链霉菌菌株。它作为葡萄糖转运蛋白 (GLUT) 的化学探针，能够抑制糖酵解。Glucopiericidin A 与 Piericidin A (PA) 联合使用时可有效抑制 ATP 依赖性丝状伪足突起，而单独使用则无效果。通过增加 PRDX1，Glucopiericidin A 降低活性氧 (ROS) 水平，诱导细胞凋亡，同时在 ACHN 小鼠异种移植物中表现出显著的抗肿瘤功效。

Nef-M1 (Nef-Motif-1) 是一个针对CXCR4的拮抗多肽和凋亡 (apoptosis) 诱导剂，来源于HIV的nef基因编码的肉豆蔻酰化蛋白。Nef-M1 可以通过提升癌细胞中caspase-3的水平从而激活凋亡通路，抑制肿瘤血管生成和上皮-间质转化 (EMT)。此外，Nef-M1 通过抑制VEGF-A、p-GSK-3β和波形蛋白，同时增强E-钙粘蛋白，从而干扰血管生成和EMT进程。该化合物对结直肠癌和乳腺癌的研究具有应用价值。

RP-182 是一种合成的免疫调节肽，靶向肿瘤相关巨噬细胞 (TAM) 表面的甘露糖受体 CD206 发挥抗肿瘤效应 (Kd= 8 μM)。它诱导 CD206 受体的构象转换，激活高表达 CD206 的 TAM 中的NF-κB信号转导和吞噬作用。RP-182 具备双重功能：通过经典NF-κB信号通路的激活，触发TNFα分泌和TNF受体1 (TNFR1) 的自分泌激活，导致caspase 8激活和细胞凋亡 (apoptosis)。RP-182 被用于胰腺癌和黑色素瘤的研究。

PRMT7-IN-2 (A33) 是一种具选择性的PRMT7抑制剂，其IC0值为0.50 μM。该化合物能够阻滞细胞周期于G0/G1 期并诱导细胞凋亡 (apoptosis)，同时在体内外抑制细胞生长。PRMT7-IN-2 可降低PRMT7的单甲基精氨酸水平，增加上皮标志物E-cadherin的表达，并减少间质标志物N-cadherin、Vimentin和ZEB2的表达。

TM471-1 是一种口服活性良好的共价布鲁顿酪氨酸激酶 (BTK) 抑制剂，对BTKWT的IC0值为1.3 nM，对BTKC481S的IC0值大于40000 nM，对TEC的IC0值为7.9 nM，对TXK的IC0值为12.4 nM。TM471-1 能在体内外抑制细胞生长，阻止细胞周期在G0/G1 期，并诱导细胞凋亡 (apoptosis)。

Apoptotic agent-6 (NSC-647889) 是一种凋亡剂，能够有效诱导多细胞球体 (MCS) 的外周细胞凋亡 (apoptotic)。适用于实体肿瘤研究，特别是播散性实体瘤。

MXC-017 是一种能够穿透血脑屏障的凋亡 (apoptosis) 诱导剂，直接靶向胶质瘤干细胞 (GSCs)。它阻止辐射诱导的 GSC 形成，并增加 G0/G1 细胞周期停滞和细胞凋亡 (apoptosis)。MXC-017 具极小的脱靶效应，在高达 10 µM 的浓度下无显著细胞毒性。此外，MXC-017 显著延长了患者来源的原位异种移植 (PDOX) 胶质母细胞瘤 (GBM) 小鼠模型中配合放射治疗的中位生存期。

RUNX1/ETO-IN-1 是一种抑制RUNX1-ETO致癌融合蛋白的药物，对NHR2寡聚化结构域具有特异性作用。此化合物直接结合于NHR2，并具有KD,app= 39 μM的结合亲和力。通过诱导细胞凋亡和促进分化，RUNX1/ETO-IN-1 在RUNX1/ETO易位型急性髓系白血病 (AML) 细胞中表现出抗白血病活性。此外，在生理pH条件下，RUNX1/ETO-IN-1 基本不带电荷，从而具备出色的细胞膜渗透性。

MET Transcription-IN-1 (Compound C3) 是一种口服活性的MET转录抑制剂，能够高效结合并稳定MET启动子区的G-四链体，从而抑制c-Met的表达，并克服特定c-Met突变导致的耐药性。此化合物能够抑制肿瘤细胞的增殖、迁移和侵袭，并诱导细胞周期阻滞及凋亡 (apoptosis)，具有抗肿瘤活性，适用于非小细胞肺癌等肿瘤研究。

DB2313 is a first-in-class potent small-molecule inhibitor of PU.1. DB2313 disrupts the interaction of PU.1 with target gene promoters and leads to down-regulation of canonical PU.1 transcriptional targets.

3-ATA is a selective cyclin-dependent kinase 4 (Cdk4) inhibitor, attenuating kainic acid-induced apoptosis in neurons.

PC-046 is a potent tubulin-binding agent, which was originally identified for development based on selective activity in deleted in pancreas cancer locus 4 (DPC4/SMAD4) deficient tumors. PC-046 has growth inhibitory activity in a variety of tumor types in vitro, and efficacy in SCID mice was shown in human tumor xenografts of MV-4-11 acute myeloid leukemia, MM.1S multiple myeloma, and DU-145 prostate cancer. Pharmacokinetic studies demonstrated relatively high oral bioavailability (71 %) with distribution to both plasma and bone marrow. No myelosuppression was seen in non-tumor bearing SCID mice given a single dose just under the acute lethal dose. The COMPARE algorithm in the NCI-60 cell line panel demonstrated that PC-046 closely correlated to other known tubulin destabilizing agents (correlation coefficients ≈0.7 for vincristine and vinblastine). Mechanism of action studies showed cell cycle arrest in metaphase and inhibition of tubulin polymerization. Overall, these studi......

APX2009 is a second-generation APE1/Ref-1 redox-specific inhibitor. APX2009 significantly reduces NFkB transcriptional activity, survivin mRNA, and survivin protein levels. APX2009 decreases prostate cancer cell proliferation and induces cell cycle arrest.

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.

Metformin glycinate is an AMP-activated protein kinase (AMPK) activator that improves glycemic control by improving insulin sensitivity and decreasing intestinal absorption of glucose.

PHA-680626 is a potent and selective PLK inhibitor. PHA-680626 exhibits anti-proliferative and pro-apoptotic activity on Imatinib-resistant chronic myeloid leukemia cell lines and primary CD34+ cells by inhibition of both Bcr-Abl tyrosine kinase and Aurora kinases. PHA-680626 inhibits Plk1 (IC50 = 0.53 μM), Plk2 (IC50 = 0.07 μM) and Plk3 (IC50 = 1.61 μM).

BAY 61-3606 HCl is a cell-permeable, reversible inhibitor of spleen tyrosine kinase. BAY 61-3606 HCl can inhibit degranulation and block cytokine release from mast cells. Oral administration of BAY 61-3606 to rats was shown to suppress antigen-induced passive cutaneous anaphylactic reaction, bronchoconstriction, and bronchial edema. It can also sensitize MCF-7 breast cancer cells to TNF-related apoptosis-inducing ligand (TRAIL)-mediated apoptosis by inhibiting Cdk9. This compound has been used in a pre-clinical model to explore the feasibility of targeting Syk in the treatment of retinoblastoma.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

TPP-Ce6 是一种针对线粒体的光敏剂，通过酯键将叶绿素e6 (Ce6) 与三苯基膦 (TPP) 结合。在光照条件下，TPP-Ce6 能够生成ROS，尤其是单线态氧，这些ROS可以引发氧化应激，导致线粒体功能紊乱和细胞凋亡 (apoptosis)。TPP-Ce6 可用于研究涉及线粒体的细胞凋亡 (apoptosis)、能量代谢以及癌症治疗。

PRMT5-targeted fluorescent ligand-1 (Compound 7) 是一种靶向PRMT5的荧光配体，IC50为29.39 nM，能够抑制PRMT5。在MCF-7细胞中，该化合物表现出优良的荧光信号，IC50为29 nM，并可诱导细胞凋亡 (apoptosis)。其最大激发波长为438 nm，最大发射波长为550 nm。