Apoptosis

PF-3758309 hydrochloride (PF-03758309 hydrochloride) 是一种口服的、可逆的 ATP 竞争性PAK4抑制剂，Kd 为 2.7 nM，Ki 为 18.7 nM。它抑制锚定独立生长、诱导凋亡、细胞骨架重塑和抑制增殖，具有 PAK4 抑制剂的预期细胞功能。

Thalidomide-NH-C4-NH2 TFA (compound 29c) is a conjugate consisting of an E3 ligase ligand-linker, incorporating the Thalidomide-based cereblon ligand and a linker moiety. This compound, Thalidomide-NH-C4-NH2 TFA, is utilized as a component in PROTAC BRD2/BRD4 degrader-1, which is a highly potent and selective degrader targeting BET proteins BRD4 and BRD2[1].

BR102375 is a non-TZD PPAR γ full agonist (EC50: 0.28 μM) for the treatment of type 2 diabetes.

SH-5 是一种AKT抑制剂，通过抑制IκBα激酶激活调节的抗凋亡、增殖和转移基因产物，增强细胞凋亡并抑制侵袭。

WF-210 is an effective activator of procaspase-3 that acts by inducing apoptosis in cancer cells and reducing tumor growth.

Pamiparib is a highly potent and selective PARP inhibitor. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, pro

Anticancer agent 57 (compound 14) demonstrates potent inhibition of MDA-MB-231, MDA-MB-468, and MCF-7 cell lines, with IC 50 values ranging from 6.43 to 8.00 μM. Additionally, this agent induces cell cycle arrest and promotes apoptosis. In vivo studies using nude mice xenografted with MADMB-231 cells have shown that Anticancer agent 57 effectively inhibits tumor growth. Consequently, Anticancer agent 57 can serve as a valuable tool for researching triple negative breast cancer (TNBC) [1].

HDAC-IN-31 是一种选择性的、有效的、口服具有活力的 HDAC 抑制剂，能够作用于 HDAC1 (IC50: 84.90 nM)、HDAC2 (IC50: 168.0 nM)、HDAC3 (IC50: 442.7 nM)、HDAC8 (IC50>10000 nM)。 HDAC-IN-31 能够将细胞周期阻滞在 G2/M 期，并诱导细胞凋亡 (apoptosis)。HDAC-IN-31 具有良好的抗肿瘤效果。HDAC-IN-31 对弥漫性大 B 细胞淋巴瘤表现出潜在的研究价值。

Topoisomerase II inhibitor 3 (Compound 6 h) is an acridone derivative that acts as a Type II DNA topoisomerase (topo II) inhibitor. It specifically inhibits the topo IIα/β subtypes, with an IC50 value of 0.17 μM for topo IIα and 0.23 μM for topo IIβ. This compound elicits significant DNA damage and induces apoptosis by triggering the loss of mitochondrial membrane potential [1].

Aspirin calcium is the prototypical analgesic used in the treatment of mild to moderate pain. It has anti-inflammatory and antipyretic properties and acts as an inhibitor of cyclooxygenase which results in the inhibition of the biosynthesis of prostaglandins. Aspirin also inhibits platelet aggregation and is used in the prevention of arterial and venous thrombosis. (From Martindale, The Extra Pharmacopoeia, 30th ed, p5)

Anti-osteoporosis agent-1 (comp 4aa) 作为一种高效的复制蛋白 A(RPA) 抑制剂，表现出其IC50值仅为18 μM。

LA-CB1 是一种 Abemaciclib 衍生物，针对 CDK4/6，通过泛素-蛋白酶体途径促进其降解，从而阻断 CDK4/6-Cyclin D1-Rb-E2F 轴，诱导 G0/G1 细胞周期阻滞和细胞凋亡 (Apoptosis)。LA-CB1 对 MDA-MB-231 细胞展现抗增殖活性，IC50 为 0.27 µM，并有效抑制上皮-间充质转化、细胞迁移、侵袭和血管生成。在三阴性乳腺癌 (TNBC) 等高度侵袭性模型中，LA-CB1 明显抑制肿瘤生长，表现出良好的剂量依赖性抗肿瘤活性。该化合物可用于乳腺癌研究。

Apoptosis inducer42 是一种诱导凋亡的化合物，可以激活晚期凋亡并抑制IL-6的分泌。它对癌细胞表现出高细胞毒性，适用于癌症研究，如结肠癌。

HI042 是一种 FMS 类酪氨酸激酶 3 (FLT3) 抑制剂。其在 MOLM-13 细胞中的 IC50 值为 0.62 μM，在 MV4-11 细胞中的 IC50 值为 0.33 μM，在 OCI-AML3 细胞中的 IC50 值为 0.89 μM。HI042 能选择性降低 FIT3-内部串联重复突变 (FLT3-ITD) 阳性细胞系的存活率，诱导细胞凋亡 (apoptosis)，干扰细胞周期，并降低集落形成能力。该化合物可用于急性髓系白血病 (AML) 的研究。

Apoptosis inducer40 是凋亡 (apoptosis) 诱导剂，对 Jurkat 细胞和 NB4 细胞具有显著细胞毒性，其IC50值分别为 4.5 μM 和 3.6 μM。Apoptosis inducer40 能诱导细胞凋亡及阻碍细胞周期，适用于急性髓系白血病 (AML) 等癌症研究。

SL-176 是一种 WIP1 抑制剂，与 GSK-J4 联用能诱导细胞周期阻滞和凋亡 (apoptosis)，从而抑制体内外的肿瘤生长。

FL3 is a novel potent eIF4F inhibitor, it induces the death of cancer cells by an original mechanism that involves the apoptosis-inducing factor and caspase 12.

6,7-Di-O-acetylsinococuline 是一种天然产物，可用于生命科学领域的相关研究。其产品编号为 TN6301，CAS号为 1054312-81-0。

Cidofovir sodium is the salt form of Cidofovir, a Cytomegalovirus Nucleoside Analog DNA Polymerase Inhibitor that is an injectable antiviral medication primarily used as a treatment for cytomegalovirus (CMV) retinitis in people with AIDS. The mechanism of action of cidofovir is as a DNA Polymerase Inhibitor. The chemical classification of cidofovir anhydrous is Nucleoside Analog.

Atiprimod is an orally bioavailable small molecule belonging to the azaspirane class of cationic amphiphilic agents with anti-inflammatory, antineoplastic, and antiangiogenic properties. Atiprimod inhibits the phosphorylation of signal transducer and activator of transcription 3 (STAT3), blocking the signalling pathways of interleukin-6 and vascular endothelial growth factor (VEGF) and downregulating the anti-apoptotic proteins Bcl-2, Bcl-XL, and Mcl-1, thereby inhibiting cell proliferation, inducing cell cycle arrest, and inducing apoptosis.

Jacaric acid is a conjugated polyunsaturated fatty acid first isolated from seeds of Jacaranda plants. Structurally, it is an 18-carbon ω-6 triene isomer of γ-linolenic acid . Jacaric acid induces cell cycle arrest and apoptosis in a variety of cancer cell lines (GI50 = 1-5 μM). It increases the production of reactive oxygen species, and cytotoxicity is abolished by the antioxidant α-tocopherol, suggesting that apoptosis results from oxidative stress. Jacaric acid is metabolized in vivo to conjugated linoleic acid , which is also cytotoxic to cancer cells. Jacaric acid inhibits cyclooxygenase-1 in vitro (Ki = 1.7 μM) and, with long term feeding, decreases stearoyl-CoA desaturase expression and activity in mice.

Antitumor agent-55 (compound 5q) 是一种有效的抗肿瘤剂，能够有效的抑制PC3 (IC50: 0.91 μM)。Antitumor agent-55 能够将 PC3 的细胞周期阻滞 G1/S 期，诱导其凋亡，抑制细胞迁移，阻碍 PC3 的形成。

Sodium catechol sulfate is a bioactive chemical.

hCAIX-IN-12 是有效的hCAIX 抑制剂，抑制 CAIX 和 CAII 的IC50分别为 0.74 和 10.78 μM。hCAIX-IN-12 抗细胞增殖并诱导凋亡 (apoptosis)。hCAIX-IN-12 可以增加ROS 的产生。hCAIX-IN-12在结直肠癌（CRC）中具有研究潜力。

Antitumor agent-44 (Compound 5n) elicits potent antitumor effects by inducing disruption of mitochondrial homeostasis, cell cycle arrest, and apoptosis in human adenocarcinoma cells. Moreover, Antitumor agent-44 demonstrates significant anti-tumor activity in a lung cancer cell xenograft mice model [1].

Lincydomine is a smooth muscle relaxant, beneficial to the treatment of unstable angina pectoris, but also can open the respiratory tract of humans and guinea pigs.

PSF-IN-2 (Compound (C)-30) 是一种PSF抑制剂，IC50 为 0.005 pM，显示出抗癌活性，并对 22Rv1 细胞增殖的抑制IC50为 0.5 μM。其作用机制为通过阻止PSF与RNA的结合，激活p53信号通路，诱导相关基因的表达，促进细胞凋亡 (Apoptosis) 并抑制细胞周期。PSF-IN-2 可用于癌症研究领域。

KMUP-1 是一种黄嘌呤衍生物，具有血管舒张活性。作为磷酸二酯酶 (PDE) 抑制剂和可溶性鸟苷酸环化酶 (sGC) 激活剂，KMUP-1 能激活 NO/sGC/环鸟苷酸环化酶通路，并显示出开放 K+通道的活性。此外，KMUP-1 能减轻缺血诱导的心肌细胞凋亡 (apoptosis)，适用于心血管和抗炎研究。

CDK2-IN-45 是一种 CDK2 抑制剂 (IC50: 0.64 μM)，能够抑制 DU-145 和 PC-3 细胞系的增殖，其IC50值分别为2.20 μM和4.17 μM。CDK2-IN-45 可引起G0/G1期细胞周期停滞并诱导细胞凋亡 (Apoptosis)。此外，CDK2-IN-45 可用于前列腺癌研究。

Trichodermin 是一种天然存在的倍半萜类抗生素 (antibiotic)，具有强效的蛋白质合成 (protein synthesis) 抑制作用。它通过与真核生物核糖体结合并与肽基转移酶相互作用来抑制蛋白质翻译。Trichodermin 通过诱导凋亡 (apoptosis) 性线粒体功能障碍和 HDAC-2 介导的信号传导来阻止口腔癌的生长，对丝状真菌、酵母菌和细菌表现出卓越的抗菌活性。

L-2,5-Dihydrophenylalanine 能诱导人类髓母细胞白血病细胞HL-60发生凋亡。

Vobtusine 是一种生物碱，分布于非洲野豌豆叶中。

Stigmast-5-en-3-ol 通过增加Bax、Caspase-9、p53和PARP裂解的产生，以及降低Bcl-xl表达，诱导癌细胞凋亡 (apoptosis) 和抑制增殖。它对葡萄糖淀粉酶和 α-淀粉酶 (α-amylase) 展现出强效抑制作用，且具备高抗氧化活性。Stigmast-5-en-3-ol 可用于研究白血病、乳腺癌、2 型糖尿病及肥胖症等疾病。

HS-438 inhibits imatinib-resistant BCR-ABL T315I mutation in chronic myeloid leukemia.

Tubulin polymerization-IN-26 (compound 12h) is a chemical compound that inhibits the polymerization of microtubulin. It achieves this by binding to the colchicine binding site of microtubulin, with an IC50 value of 4.64 μM. Additionally, Tubulin polymerization-IN-26 has the ability to induce apoptosis and inhibit cell metastasis or migration. Due to these properties, it holds potential as a valuable compound for researching lung cancer [1].

EGFR-IN-56 (Compound 13a) 是一种 EGFR 的有效抑制剂，能够作用于 EGFRT790M (IC50: 541.7 nM) 和 EGFRT790M/L858R (IC50: 132.1 nM)。EGFR-IN-56 能够将癌细胞的细胞周期阻滞在 G2/M 期，并诱导细胞凋亡 (apoptosis)。