Apoptosis

Anticanceragent 268 (Compound 4k) is a potential antitumor agent. It exhibits antiproliferative effects on HepG2 cells, with an IC50 value of 6.08 μM. Additionally, Anticanceragent 268 induces apoptosis and inhibits colony formation and migration of HepG2 cells.

(R)-Q-VD-OPh is the less active enantiomer of Q-VD-OPha. Q-VD-OPha is an irreversible inhibitor of pan-caspase, with potent antiapoptotic properties.

ElteN378: potently inhibits FKBP12 (Ki=0.5 nM), low weight, similar affinity to Rapamycin.

EGFR/COX-2-IN-1 is an EGFR/COX-2 inhibitor that effectively targets EGFRWT, EGFRT790M, COX-1, and COX-2 with IC50 values of 0.12, 0.076, 20.1, and 1.52 μM, respectively. It inhibits MCF-7, HT-29, and A-549 cells with IC50 values of 1.20, 5.14, and 14.81 μM, respectively. The compound induces apoptosis by upregulating Bax protein and downregulating Bcl-2 protein levels. Additionally, EGFR/COX-2-IN-1 significantly increases the proportion of cells in the G2/M phase in MCF-7 cells, demonstrating a broad-spectrum antitumor effect.

PTP1B-IN-30 (Compound 3j) is an inhibitor of PTP1B with an IC50 of 0.51 µM. It suppresses the proliferation of T47D cancer cells with an IC50 of 21.21 µM, induces cell cycle arrest at the S phase, and triggers apoptosis in T47D cells.

BRD6257 is an orally active inhibitor of protein phosphatase 1D (proteinphosphatase, Mg2+/Mn2+ dependent 1D, PPM1D) with an IC50 of 5 nM. It activates the p53 signaling pathway (EC50 of 51 nM), enhances p21 expression, and inhibits the proliferation of cancer cells MOLM13 (IC50 = 2.8 μM). BRD6257 demonstrates good metabolic stability in human and rat liver microsomes.

CQ1373 is a potent RET inhibitor that demonstrates cellular activity against BaF3 cells expressing CCDC6-RET, CCDC6-RET-G810C, and CCDC6-RET-G810R, with IC50 values of 13.0, 25.7, and 28.4 nM, respectively. It shows excellent selectivity for wild-type RET and solvent front mutants G810C/R, with IC50 values of 4.2, 7.1, and 32.4 nM. CQ1373 inhibits RET phosphorylation and downstream signaling through SHC. Additionally, it induces apoptosis (Apoptosis) and cell cycle arrest in BaF3 cells. CQ1373 possesses antitumor efficacy, making it a candidate for cancer research.

Nur77 modulator 4 (Compound 15h) is a Nur77 inducer with a KD of 0.477 μM. It significantly promotes Nur77 expression and apoptosis, exhibiting excellent growth inhibitory effects on HepG2 and MCF-7 cells, with an IC50 of less than 5 μM. Nur77 modulator 4 activates Nur77-mediated ER stress through the PERK-ATF4 and IRE1 signaling pathways, leading to apoptosis. This compound is applicable in cancer research.

Hypoxia inducer-1 (Compound N6) is a NO donor compound that is orally active and activated under hypoxic conditions. It exhibits high selectivity in releasing NO, inhibiting apoptosis, necrosis, and elevated levels of reactive oxygen species (ROS) associated with hypoxia. It modulates vasodilation and shows protective effects in a mouse model of myocardial hypoxic injury, making it useful for coronary heart disease research.

PD-L1/VISTA-IN-2 (Compound S8) is an orally active dual inhibitor targeting PD-L1 and VISTA, with an IC50 of 1.4 μM for PD-L1 and a KD of 2.1 μM for VISTA. This compound can activate the tumor immune microenvironment, exerting anticancer effects.

Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.

Caspase-3 activator 3 (compound 2h) effectively induces apoptosis in HL-60 and K562 cells by substantially activating caspase-3, demonstrating antileukemic

BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)

Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.

dMCL1-2 is a PROTAC-based MCL1 degrader, binding at 30 nM, and induces apoptosis in leukemia.

ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.

Boanmycin, an antibiotic exhibiting antitumor activity, induces cellular senescence and apoptosis [1] [2] [3].

UZH1a: METTL3 inhibitor, IC50 280 nM, used for epitranscriptomic modulation and has antitumor properties.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

7-Methoxy-1-tetralone may have insecticidal activity.

FLT3-IN-29 (Compound MY-10) is an FLT3 inhibitor with IC50 values of 6.5 nM and 10.3 nM for FLT3-ITD and FLT3-D835Y mutants, respectively. It induces cell cycle arrest at the G0/G1 phase and effectively triggers apoptosis (Apoptosis). Additionally, FLT3-IN-29 reduces reactive oxygen species (ROS) and mitochondrial membrane potential (MMP), displaying anti-leukemic properties.

Antagonist G is an anticancer peptide and is also a broad spectrum neuropeptide growth factor antagonist.

Aloeresin G, a chromone glycoside isolated from Aloe, exhibits a moderate inhibitory effect on TNFα-induced NF-κB transcriptional activity, evidenced by an IC50

Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linker for PROTACs with a 3-unit PEG.

KWCN-41, Selective RIPK1 inhibitor (IC50=88 nM), inhibits necrosis specifically, anti-inflammatory effects.

JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.

GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-

HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4

Compound (Ra)-10, also known as Mcl-1 inhibitor 14, is a potent inhibitor of myeloid cell leukemia-1 (MCL-1), exhibiting a K_i of 0.018 nM, and holds potential

Mcl1-IN-26 is an effective and selective myeloid cell leukemia 1 inhibitor.

H3B-8800 is an SF3B1 modulator that can be used to study transfusion-dependent anemia.

8-hydroxy Efavirenz, a main efavirenz metabolite by CYP2B6, causes apoptosis in rat neurons at 0.01 μM.

Vonlerizumab (Anti-TNFRSF4/OX40/CD134 Antibody) is a humanized monoclonal antibody targeting OX40, used in tumor research.

Desmethyl-WEHI-345 analog, a protein kinase inhibitor, holds potential for colon cancer research.

Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19/T790M/C797S TK and

Topoisomerase II inhibitor 14: powerful anticancer agent that induces apoptosis, halts S phase, and lowers GSH, MDA, and NO levels.

Platycoside G3 is a useful organic compound for research related to life sciences. The catalog number is T124100 and the CAS number is 849758-44-7.

Tubulin Inhibitor 34 (compound b5), a potent anticancer agent, inhibits tubulin polymerization and induces G2/M arrest and apoptosis.

RWJ-56110 dihydrochloride is a potent PAR-1 inhibitor (IC50=0.44μM), blocking platelet aggregation, angiogenesis, and induces apoptosis. No PAR-2/3/4 effect.

Conglobatin is a natural product for research related to life sciences. The catalog number is T36494 and the CAS number is 72263-05-9.

Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2/M cell cycle arrest and apoptosis.

EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.

CDK9-Cyclin T1 PPI-IN-1 (Compound B19) is a selective inhibitor of the CDK9-Cyclin T1 protein-protein interaction (PPI), suppressing cell proliferation in TNBC

DiPT-4, a dual TOP1/PARP1 inhibitor, effectively induces DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells, with potential to

Antitumor Agent-116 (Compound 6C) is an anti-tumor agent that exhibits anti-proliferative properties and induces apoptosis.

4-oxo-27-TBDMS Withaferin A, a withaferin A derivative, is an anticancer agent cytotoxic to A2780, not A2780/CP70.

Thalidomide-O-amido-PEG4-azide is a polyethylene glycol (PEG) derivative serving as a linker for Proteolysis Targeting Chimeras (PROTACs) synthesis [1].

CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor.

VEGFR-2-IN-36 (compound 15) serves as a potent VEGFR-2 inhibitor, exhibiting an IC50 value of 0.067 μM, and acts as an apoptosis inducer with demonstrated

Cannflavin A, isolated from Cannabis sativa L., exhibits anti-cancer, neuroprotective, and anti-inflammatory activities by inhibiting Aβ1-42 aggregation and

Hexapeptide-11 is a novel proteostasis network modulator in human diploid fibroblasts.

Thalidomide-5,6-Cl is a cereblon ligand derivative that recruits CRBN protein and forms PROTACs with a linker.

Thalidomide-O-C7-NH2 is a cereblon ligand-linked E3 ligase for PROTAC use.

p53 and MDM2 proteins-interaction-inhibitor (racemic) is an inhibitor of the interaction between p53 and MDM2 proteins.

Cell-permeable CaM agonist; activates phosphodiesterase, binds to Ca2+ channels, inhibits cytotoxicity (IC50=52μM), protects cells, reduces inflammation.

MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.

Galloflavin Potassium is an inhibitor of lactate dehydrogenase.

Antitumor agent-100 hydrochloride (compound A6), serving as both an apoptosis inducer and molecular glue, exhibits superior anti-tumor activity [1].

PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.

F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.

CRM1-IN-2 (Compound KL2) is a noncovalent inhibitor that targets CRM1, localizing it to the nuclear periphery, depleting its nuclear presence, and inhibiting

Nauclefine, a plant alkaloid, triggers cancer cell death through PDE3A-SLFN12, binding but not inhibiting PDE3A.

BRD4 Inhibitor-38 (Compound 25) is an orally active BRD4 inhibitor, exhibiting IC50 values of 3.64 μM for BRD4 BD1 and 0.12 μM for BRD4 BD2. It also demonstrates anti-inflammatory properties, with an IC50 value of 1.98 μM for nitric oxide (NO) production.

HDSI-18 is an orally active selective inhibitor of HDAC6 with an IC50 of 1.6 nM. It exhibits cytotoxic effects against K562, MV4-11, MOLM-13, THP-1, and Jurkat cells with IC50 values of 0.48, 0.58, 0.91, 1.79, and 4.31 μM, respectively. HDSI-18 can activate Caspase-3, induce mitochondrial depolarization, and trigger apoptosis (Apoptosis), demonstrating antitumor activity.

α-Tubulin polymerization-IN-1 (Compound 8l) functions as an inhibitor of α-tubulin polymerization. This compound modulates the NRF2/KEAP-1 signaling pathway and induces ROS production in PC-3 cells, leading to apoptosis. It inhibits the proliferation of PC-3 cells with a GI50 of 0.17 µM, causing cell cycle arrest in the G2/M phase. Additionally, α-Tubulin polymerization-IN-1 demonstrates antitumor activity in mouse models.

PROTAC AR-NTD antagonist 1 (compound 18) is a small molecule belonging to the protein-targeting chimeras (PROTACs) that selectively targets the N-terminal

Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.

PD-L1/LpxC-IN-1 (Compound 12b) is an inhibitor of PD-L1 and LpxC, with IC50 values of 5.2 μM and 0.081 μM, respectively. This compound disrupts bacterial lipopolysaccharide biosynthesis, leading to bacterial cell lysis and death. It effectively inhibits Gram-negative bacteria, exhibiting a minimum inhibitory concentration (MIC) of 0.25-0.5 μg/mL against K. pneumoniae ATCC 13883, E. coli ATCC 8739, S. typhimurium ATCC 14028, and P. aeruginosa ATCC 9027. Additionally, PD-L1/LpxC-IN-1 modulates the immune response by downregulating the expression of inflammatory cytokines IL-2 and IFN-γ, and upregulating CD4+ and CD8+ cells, thus activating the immune system and mitigating excessive inflammatory responses. In a mouse model of K. pneumoniae ATCC 13883 infection, PD-L1/LpxC-IN-1 demonstrated antibacterial activity.

Thalidomide-O-C8-Boc: CRBN ligand for PROTAC creation, derived from Thalidomide.

Thalidomide-O-C8-COOH, also known as Cereblon ligand 3, is a Thalidomide-derived compound that serves as a Cereblon (CRBN) ligand for the targeted recruitment

IRAK4-IN-27 (Compound 22) is a potent and selective IRAK4 inhibitor, demonstrating an IC50 of 8.7 nM.

Humulone is a natural product and has a wide range of applications in life science related research.

Tubulysin B: a potent, cytotoxic microtubule-disrupting peptide from Archangium geophyra and Angiococcus disciformis.

Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.

Psalmotoxin 1 is a potent and selective acid-sensing ion channel 1a (ASIC1a) blocker.

SP3N hydrochloride is a specific degrader of the prolyl isomerase (FKBP12). Its alkylamine moiety is metabolized into an active aldehyde (SP3CHO), which recruits the SCFFBXO22 ligase for the degradation of FKBP12. SP3N hydrochloride is applicable in cancer research.

Suramin is an RdRp and PTPase inhibitor with anti-parasitic, anti-tumor, and anti-angiogenic activities, inhibiting sirtuins and DNA topoisomerase II.

MET/PDGFRA-IN-1 (compound 8c) serves as an inhibitor of MET and PDGFRA proteins, displaying an IC50 of 36 μM against MET.

SDH-IN-26 (Compound C3) is a succinate dehydrogenase (SDH) inhibitor with significant inhibitory activity against various plant pathogenic fungi, including solanrhizoctonia and Botrytis cinerea. It exhibits an EC50 value of 0.270 μg/mL against solanrhizoctonia. SDH-IN-26 compromises fungal cell membrane integrity, increases membrane permeability, disrupts cell structure, reduces mitochondrial count, and affects normal hyphal growth. It also decreases mitochondrial membrane potential, inducing apoptosis. SDH-IN-26 holds potential for studying plant diseases caused by fungi.

PL120131 is a PD-1/PD-L1 inhibitory peptide that disrupts the interaction between PD-1 and PD-L1 by binding to PD-1. This compound can inhibit the apoptosis signaling pathway mediated by PD-1, thereby preventing apoptosis (apoptosis) in Jurkat cells and primary lymphocytes. Additionally, PL120131 supports cytotoxic T lymphocytes (CTL) in exhibiting antitumor activity.

RIPK3-IN-3 (compound 20) is a selective RIPK3 inhibitor that demonstrates potent activity with an IC50 value of 10 nM.

"(±)-Enterodiol, the racemate of Enterodiol, is metabolized from lignans found in whole-grain cereals, nuts, legumes, flaxseed, and vegetables by human intestinal bacteria. This compound exhibits apoptotic effects in colorectal cancer (CRC) cells and has been identified to possess anti-cancer activities [1] [2]."

MSU-42011: oral RXR-like agonist, inhibits iNOS & p-ERK, antitumor in lung cancer model, effective preclinical treatment.

MAO-B-IN-30 is a selective and potent MAO-B inhibitor that crosses the blood-brain barrier with antiproliferative activity and inhibits both MAO-A and MAO-B.MAO-B-IN-30 reduces the levels of TNF-alpha, IL-6, and NF-kB in organisms, and can be used to study Parkinson's-type neurological disorders.

IC 86621: DNA-PK ATP-competitive inhibitor, IC50 120 nM, enhances DSB antitumor effects, EC50 68 µM for repair.

NecroIr2, an iridium(III) compound, induces necroptosis in Cisplatin-resistant A549R lung cancer cells and disrupts mitochondria.

Tengonermin (ARENEGYR), a vascular agent, is TNF-α fused with CNGRCG peptide, enhancing chemo and T-cell access in tumors.

ChoKα Inhibitor-5, a sulfur-containing choline kinase inhibitor, effectively inhibits HChoKα1 with an IC50 value of 0.64 μM and induces apoptosis.

7,3′,5′-Trihydroxyflavanone, a flavanoid derivative, promotes apoptotic cell death in MCF-7 cells by augmenting Bax expression.

Inuviscolide induces apoptosis, G2/M arrest in melanoma, and has anti-cancer, anti-inflammatory effects.

Chol-CTPP targets the BBB and glioma cells; when combined with Chol-TPP, forms Lip-CTPP, enhancing anti-glioma drug efficacy.

HEMTAC CDK4/6 degrader 1, a PROTAC targeting HSP90/CDK4/6, Kd of 35.7 μM, disrupts B16F10 melanoma cell cycle, and induces apoptosis.

Delmitide, a TNF-alpha production inhibitor, is used potentially for the treatment of Crohn's disease and ulcerative colitis.

AZT triphosphate TFA, a Zidovudine metabolite, inhibits HIV & HBV replication and triggers mitochondrial apoptosis.

Mofarotene (Ro-40-8757) is a small molecule compound that shows considerable antitumor activity in many cancer cell lines and can be used for the treatment of

Mcl-1 Inhibitor 12 (Example 10), with a K i of 0.22 nM, functions as an MCL-1 inhibitor. It is utilized in cancer research [1].