Apoptosis

p53-HDM2-IN-1 is a potent inhibitor of the p53-HDM2 protein-protein interaction, demonstrating an inhibitory concentration (IC 50) of 0.103 μM.

Antitumor agent-61, a potent Irinotecan derivative, exhibits IC50s of 0.92-3.23 μM in 6 cancer cells, inducing apoptosis via mitochondrial pathways.

PNT100: 24-base DNA oligo targeting BCL-2 regulatory region; halts tumor cell growth, induces death.

Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linked E3 ligase used in PROTAC with a 2-unit PEG.

QN523 has drug-like traits, kills cancer cells in vitro, effective in vivo against pancreatic cancer, works via autophagy.

Haemanthamine hydrochloride, an alkaloid from Amaryllidaceae, has anticancer, antioxidant, antiviral, antimalarial, and anticonvulsant properties.

Pexelizumab is a humanized antibody targeting C5 to inhibit apoptosis and treat cerebral IR injury and myocardial infarction.

AMG-7209 is an effective and selective MDM2-p53 interaction inhibitor.

Sanggenon G inhibits XIAP by binding its BIR3 domain; affinity is 34.26 μM, boosting caspase activation.

Chalcones A-N-5, a non-cytotoxic trihydroxy chalcone, aids cell growth & neuroprotection, inhibits ferroptosis, and targets AD research.

Apoptosisinducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is a mononuclear Ag(I) ligand-based autophagy inducer that exhibits antibacterial and anticancer activities against various bacterial strains and cancer cell lines. This compound facilitates the accumulation of Ag(I) ions in the periphery of bacteria, effectively inhibiting the growth of both Gram-positive (+) and Gram-negative (-) bacteria. Additionally, Apoptosisinducer 26 can intercalate between the base pairs of CT DNA, inducing apoptosis in A549 cells. It also possesses radical scavenging properties, which helps prevent oxidative stress.

LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.

c-Met/HDAC-IN-4, a dual inhibitor of c-Met/HDAC, exhibits an IC 50 value of 28.92 nM for c-Met. This compound effectively induces G 0 /G 1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells. Additionally, c-Met/HDAC-IN-4 suppresses both the proliferation and invasion of breast cancer cell lines.

ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.

A-1248767, a derivative of A-1210477, is an MCL-1 inhibitor (IC50=23.9 nM; Ki=0.41 nM) known for its anticancer properties. It binds to MCL-1 with high affinity, induces an increase in MCL-1 protein levels inside cells, and promotes apoptosis in tumor cells.

Ch282-5, an orally active inhibitor targeting the Bcl-2 protein, promotes mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. It demonstrates antiproliferative effects on colorectal cancer cells, effective both in vitro and in vivo, while also inhibiting metastasis. Further, Ch282-5 augments Oxaliplatin-induced autophagy (Autophagy) by downregulating Mcl-1 protein and raising platelet count, which helps mitigate the adverse effects of Navitoclax.

Compound TE3, also known as ROS inducer 4, serves as a mitochondrial inhibitor. This compound induces a variety of mitochondria-related physiological alterations in tumors, including mitochondrial fragmentation, intense generation and accumulation of ROS, reduced mitochondrial membrane potential, and lower ATP content. Additionally, it activates ROS-mediated apoptotic signaling within mitochondria.

HDAC-IN-77 (HL-5s), an HDAC inhibitor, has the capability to induce ferroptosis and suppress the Nrf2/HO-1 signaling pathway. This compound is utilized in cancer research.

Compound AuL9, also known as iNOS/TopoI-IN-1, is a multi-target hybrid molecule possessing anti-tumor, anti-inflammatory, and antioxidant properties. This compound effectively inhibits the growth of MCF-7 and MDA MB-231 breast cancer cells in vitro, exhibiting IC50 values of 3.5 μM and 6.3 μM respectively. It also prompts DNA damage and apoptosis in these cells by inhibiting human topoisomerase I (TopoI) with a K_i of 2.72 μM. Additionally, iNOS/TopoI-IN-1 reduces the expression of iNOS by suppressing the activation of NF-kB, with a K_i of 1.49 μM.

Compound Ru2 (Antitumor photosensitizer-6) exhibits synergistic type I/II photosensitization and photocatalytic activities under illumination at 595 nm. It causes oxidative redox imbalance within cells, affecting biosynthesis and metabolic processes, leading to cell apoptosis (Apoptosis). Compound Ru2 is applicable in studies of photodynamic therapy (PDT).

EGFRkinase inhibitor 7 (compound 18i) is an EGFR inhibitor with an IC50 of 42.3 nM, exhibiting anticancer properties. This compound demonstrates significant in vitro cytotoxicity and capacity to induce apoptosis. Furthermore, EGFRkinase inhibitor 7 displays anti-proliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively.

TOFA-Plasmalogen (compound 1), a derivative of glyceraldehyde, exhibits ferroptosis-inducing properties. This compound promotes lipid peroxidation in cell membranes, leading to cytotoxic effects with an inhibition concentration (IC 50 = 32.87 μM).

PI3K/AKT-IN-4 (compound 3), a diterpenoid extracted from the roots and rhizomes of Salvia castanea Dielsf., exhibits antitumor properties by inhibiting cell viability and proliferation (IC 50 =4.72 μM) and promoting apoptosis in Hep3B cells. This compound obstructs the G0/G1 phase of the cell cycle, triggers mitochondrial dysfunction, and induces oxidative stress. Moreover, PI3K/AKT-IN-4 combats hepatocellular carcinoma through the inhibition of the PI3K-Akt signaling pathway and by interacting with PARP1 and CDK2 targets.

GPX4-IN-14 (compound 2c) acts as a GPX4 inhibitor, exhibiting both free radical scavenging activity (with a maximum scavenging rate of 72.52%) and anti-tumor proliferation activity in vitro. This compound targets GPX4 protein, elevating lipid peroxide and intracellular Reactive Oxygen Species (ROS) levels, which induces ferroptosis and contributes to its anti-tumor proliferation effects.

GBM CSCs-IN-1 (Compound (−)-20), a rocaglate derivative, potently inhibits glioblastoma stem cells (GBM CSCs) and exhibits an EC50 of 45 nM by targeting the RNA helicase DDX3. Additionally, it induces apoptosis in these cells.

Antitumor agent-187 (compound I3), a photosensitizer derived from 5,15-diarylporphyrin, exhibits anticancer activity with a peak absorption wavelength of ~668 nm. This compound induces apoptosis and is applicable in photodynamic therapy (PDP). It selectively accumulates in tumor sites and possesses real-time fluorescence imaging capabilities.

H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.

BTK-IN-37 (compound 8d), a BTK inhibitor, demonstrates potent apoptotic effects on cancer cells by targeting BTK with K_i and IC_50 values of 5.07 nM and 3.6 nM, respectively. Additionally, this compound selectively promotes the enrichment of genes associated with necroptosis and pyroptosis.

A-1208746 is an inhibitor of MCL-1 with a Ki value of 0.454 nM. This compound effectively activates caspase-3/-7, induces apoptosis in H929 cells, and reduces mitochondrial membrane potential. Additionally, A-1208746 synergizes with Navitoclax, making it applicable in cancer research.

hCAIX/XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX/XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2/M phase cell cycle arrest and increasing apoptosis.

1-Methyl-1H-pyrrolo[2,3-b]pyridine exhibits cytotoxicity against MCF-7 cells and can be used in related research in the field of life sciences.

Ferroptosis-IN-16 (Compound 13l) acts as a specific inhibitor of ferroptosis, demonstrating EC50 values of 0.7 nM in ES-2 cells and 0.9 nM in LX-2 cells. It effectively alleviates acute liver injury induced by Acetaminophen in mouse models and shows excellent metabolic stability in mouse liver microsomes.

Cereblon ligand for PROTAC R&D; has E3 ligase, alkylC1-PEG3-alkylC3 linker, terminal amine. Part of Arvinas-licensed tool molecules.

RMC-4998 formic is an orally active inhibitor targeting the GTP-bound state of the KRASG12C mutant. It forms a trimeric complex with intracellular CYPA and the activated KRASG12C mutant, displaying an IC50 value of 28 nM. This compound inhibits ERK signaling and induces apoptosis in KRASG12C mutant cancer cells and is utilized in tumor research.

Anticancer Agent 153 (Compound 3) promotes apoptosis through the generation of Reactive Oxygen Species (ROS) and elevates the loss of Mitochondrial Membrane

p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.

Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.

Compound Rh1 (Anticancer agent 132) acts as an inducer of apoptosis and autophagy, exhibiting both antitumor and antimetastatic activities.

Apoptosisinducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, demonstrating antitumor activity by causing significant morphological changes, such as membrane blebbing, nuclear fragmentation, and apoptotic body formation, in MDA-MB-231 cells. The IC50 values for Apoptosisinducer 32 are 4.77 μM in MCF-7 cells, 6.56 μM in MDA-MB-231 cells, and 337.8 μM in HEK cells.

Compound 29c, a Thalidomide-linker conjugate for potent PROTAC BRD2/BRD4 degrader-1, targets BET proteins.

AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA

Furazolidone (Furoxone), a nitrofuran derivative, inhibits AML1-ETO transformed cells with IC50 value of 12.7 μM.

CPM-1285 induces apoptosis by effectively inhibiting the function of intracellular Bcl-2 and associated death antagonists.

Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties.

Oligomycin B is an antibiotic isolated from marine Streptomyces, is an eukaryotic ATP synthase inhibitor, induces apoptosis.

pdTp is a highly selective, small-molecule miRNA regulatory complex RISC subunit SND1 inhibitor.