Apoptosis

PG-11047 2HCl treats genitourinary, immune, genetic, ocular, blood/lymphatic disorders, and aids lymphoma/prostate cancer research.

hMcl-1-IN-1 (Compound 9) is an hMcl-1 inhibitor based on a His224 arylsulfonyl fluoride, displaying an IC50 value of 5.8 nM.

APG-1387 inhibits IAPs, degrades cIAP1/2, XIAP, boosts chemosensitivity, and induces apoptosis in NPC.

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

CPD-10 is a potent bifunctional PROTAC degrader targeting CCND1 and CDK4 and exhibits antiproliferative effects. It induces apoptosis and reduces the protein expression of Cyclin D1, Cyclin D3, CDK4, and P-Rb(5807/811) in a dose-dependent manner.

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

PROTAC HIF-1α degrader-1 (compound V2) is an effective proteolysis-targeting chimeric (PROTAC) degrader of hypoxia-inducible factor-1α (HIF-1α), with an IC50 value of 7.54 µM. This compound exhibits anti-proliferative activity, reduces HIF-1α protein expression, and induces apoptosis.

NDI-Lyso is an anticancer agent targeting lysosomes, functioning through an enzyme-induced self-assembly (EISA) mechanism catalyzed by Cathepsin B. In cancer cell lysosomes, it forms rigid long fibers, promoting lysosomal swelling, lysosomal membrane permeabilization (LMP), and membrane disruption. This leads to non-classical caspase-independent apoptosis (Apoptosis). NDI-Lyso demonstrates significant selective anticancer activity across various cancer cell lines and drug-resistant cancer cells (IC50 approximately 10 μM), while exhibiting low toxicity to normal cells (IC50 > 60 μM).

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

TPP-resveratrol is a conjugate of Resveratrol and triphenylphosphine (TPP), noted for its anticancer activity. This compound enhances the efficacy of Resveratrol by facilitating its targeted delivery to mitochondria, thus inducing mitochondrial-mediated cell apoptosis (apoptosis).

PEAQX tetrasodium hydrate: potent/selective oral NMDA antagonist, IC50 270 nM (1A/2A), 29600 nM (1A/2B).

PD-1-IN-20 is the less active enantiomer of PD-1-IN-1.

Mechercharmycin A, a cytotoxic compound, was isolated from Thermoactinomyces sp. YM3-251, a marine source. It demonstrates potent antitumor activity.

SCR7, a specific DNA Ligase IV inhibitor, blocks nonhomologous end-joining (NHEJ).

EGFRT790M/L858R-IN-2: selective inhibitor, IC50: 3.5 nM (mutant), 1290 nM (WT); reduces p-EGFR/AKT/ERK1/2, triggers apoptosis, G1 arrest, anti-cancer.

TD1092, a pan-IAP degrader, activates caspase 3/7, induces apoptosis in cancer cells, inhibits NF-κB, and is used in cancer research.

CGP 3466B (Omigapil) is an oral drug inhibiting GAPDH nitrosylation and apoptosis, potentially treating Alzheimer's and CMD.

Oral nitroimidazole antibiotic; treats anaerobic infections; may cause inflammation and muscle contractions with long-term use.

Echitamine chloride, an alkaloid in Alstonia scholaris, has anti-cancer properties and inhibits pancreatic lipase (IC50: 10.92 µM).

TD52 dihydrochloride, an Erlotinib derivative, inhibits protein phosphatase 2A and induces apoptosis in TNBC by disrupting CIP2A/PP2A/p-Akt signaling.

BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2].

Ac-YVAD-CHO acetate, potent reversible ICE and caspase-1 inhibitor; K_i: 3.0 nM (mouse), 0.76 nM (human); blocks IL-lβ production.

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].

Amino-PEG6-Thalidomide is a PEG-based linker for PROTACs which joins two essential ligands, crucial for forming PROTAC molecules.

Thalidomide-NH-PEG8-Ts: a synthesized Thalidomide-PEG8 E3 ligase linker for PROTAC-mediated IDO1 degradation.

Ganoderic acid Mf: antitumor triterpenoid, arrests G1 cell cycle, selective for cancer cells, triggers apoptosis via mitochondria.

Malformin A, from A. niger, is a plant growth regulator and has anti-TMV and cancer cell cytotoxic properties. Intraperitoneal LD50 in mice is 3.1 mg/kg.

Ono 3403, a synthetic serine protease inhibitor, blocks TNF-alpha, NO production, and has antitumor properties.

9,11-Dehydroergosterol peroxide is a useful organic compound for research related to life sciences.

SZUH280 is a potent, selective PROTAC (proteolysis targeting chimera) HDAC8 (histone deacetylase 8) degrader, demonstrating a DC50 of 0.58 μM in A549 cells.

Aviculin, a lignan glycoside, exhibits anticancer properties by inducing apoptosis in breast cancer cells with an IC50 of 75.47 μM.

eIF4A3-IN-5 potently inhibits eIF4AI/II, promising for cancer research.

F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM.

Daporinad hydrochloride (FK 866 hydrochloride) is a NAMPT inhibitor with antitumor and antiangiogenic activity that induces apoptosis in tumor cells.

AM-8553 is potent and selective piperidine the MDM2-p53 interaction inhibitor.

MI-1061 TFA: potent MDM2 inhibitor, orally bioavailable, stable (IC50=4.4 nM, Ki=0.16 nM), activates p53, induces apoptosis in mice tumors.

CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM).

HJC0416 hydrochloride: potent oral STAT3 inhibitor, better anticancer effects than Stattic, promising for breast cancer research.

Tasisulam triggers apoptosis, halts mitosis, and normalizes blood vessels to combat cancer.

BK50164: CD73 inhibitor, IC50=13.089µM; binds CD99, KD=1.5µM; anticancer, induces apoptosis, arrests sub-G1.

Thalidomide-Piperazine-PEG2-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand with a PEG2 linker.

Bcl-2-IN-2 is a highly potent and selective inhibitor targeting Bcl-2 and Bcl-xL.

FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase.

hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 value of 0.11 µM. It operates by competitively binding to the active site of hMAO-B, thereby preventing the oxidative deamination of monoamines and reducing hydrogen peroxide production. Additionally, hMAO-B-IN-11 inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia. This compound holds potential for research in neurodegenerative diseases such as Parkinson's and Alzheimer's.

BCL6-IN-6 is an inhibitor of Bcl-6 and can be used in studies about diffuse large B-cell lymphoma.

SLF TFA, a synthetic FKBP ligand, binds FKBP51 (3.1 μM) and inhibits FKBP12 (IC50 2.6 μM); used in PROTAC synthesis.

STM3006 is an orally active, selective and and potent METTL3 inhibitor with antitumor activity for the study of acute myeloid leukemia (AML).

Didocosahexaenoin, omega-3 diglyceride, disrupts mitochondria, induces ROS, apoptosis, and is cytotoxic to prostate cancer cells.

PROTAC Bcl-xL degrader-1 targets Bcl-xL & IAP E3 ligases, degrades Bcl-xL, toxic to human platelets & MyLa 1929 (IC50: 62 nM, 8.5 μM).

VB-85247 is a STING agonist that, by activating the STING pathway, induces the upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as the maturation and activation of dendritic cells. It can lead to the regression of tumors within the bladder and is applicable in bladder cancer research.

Antitumor agent-201 (Compound 10) is a Golgi apparatus-targeting chloride ion transport activator with an EC50 for promoting transmembrane chloride ion transport of 1.53 mol% and an IC50 against HepG2 cells of 7.13 μM. By selectively acting on the Golgi apparatus, Antitumor agent-201 disrupts chloride ion homeostasis, decreases the expression of key proteins such as GM130 and GRASP55, and alters Golgi structure and function. This process induces Golgi apparatus autophagy, triggers apoptosis in cancer cells, and causes cell cycle arrest at the G2/M phase, thereby exhibiting anticancer activity. Antitumor agent-201 is applicable for research in the field of cancer-related diseases.

Rasfonin, a fungal metabolite from T. terrophilus, halts mouse splenocyte growth; IC50: 0.7 μg/ml (ConA), 0.5 μg/ml (LPS).

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

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

MDM2/4-p53-IN-3 inhibits MDM2/4-p53 PPIs (IC50: 18.5nM MDM2, 14.8nM MDM4), used in cancer research.

Dimethachlor is a pesticide and herbicide used in wetland areas.

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

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

Dimeric Smac mimetic inhibits XIAP, cIAP1/2 (IC50: 15/15/21 nM); binds BIR3 domain; degrades cIAPs; induces apoptosis in cancer cells; shrinks tumors in mice.

Antitumor Agent-41 (Compound N-12) exhibits potent antitumor properties, demonstrating significant antimigration and anti-invasion activities.

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

LSD1-IN-26 (12u) is a potent LSD1 inhibitor (IC50=25.3 nM), also inhibits MAO-A/B, induces apoptosis in MGC-803, for gastric cancer research.

HTH-01-091 TFA: Potent, selective MELK inhibitor (IC50=10.5 nM); also targets PIM1/2/3, RIPK2, DYRK3, smMLCK, CLK2; used in breast cancer research.

Holothurin A is a triterpene glycoside.

Bcl-B inhibitor 1 is a Bcl-B inhibitor with antitumor activity that binds to and inactivates pro-apoptotic proteins in the BH3 structural domain.

NecroIr1, an iridium(III) complex, induces necroptosis in Cisplatin-resistant lung cells, targeting mitochondria and disrupting MMP.

5-LOX-IN-8 is a 5-LOX inhibitor with anti-inflammatory properties. It suppresses IL-6, IL-1β, TNF-α, and IFN-γ in macrophages and reduces IL-8 secretion in SW480 cells. Additionally, 5-LOX-IN-8 decreases the disease activity index in DSS colitis models. This compound is applicable for research in inflammatory bowel disease (IBD).

GPLGIAGQ acetate: MMP2-cleavable peptide; stimulus-sensitive linker for MMP2-targeted liposomal/micellar carriers in photodynamic therapy.

MitoEbselen-2 mitigates radiation, cuts lipid hydroperoxides, blocks cell death, and boosts survival in irradiated mice.

DS-5272 is a potent and orally active inhibitor of p53-MDM2 interaction.

BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM [1].

SM-164 Hydrochloride: Smac mimetic, cell-permeable, binds XIAP BIR2 and BIR3, IC50 of 1.39 nM, potent XIAP antagonist.

Methyl-4-oxoretinoate is a synthetic retinoid with anticancer properties, used for skin conditions and potential ocular treatments.

Pomstafib-2, a potent and selective inhibitor of STAT5b, reduces pSTAT5b expression and effectively induces apoptosis [1] [2].

M24 inhibits Mcl-1 (Ki = 0.33μM), blocks HepG2 cell growth, and triggers apoptosis.

12-HETE ((±)12-HETE) is a regulator of PGE2, having both antithrombotic and prothrombotic effects.

RA-XII is a useful organic compound for research related to life sciences. The catalog number is T125868 and the CAS number is 143343-98-0.

DAPK-IN-2: DAPK inhibitor with anticancer potential. Used in cerebral infarction and ischemia research.

Compound 9a, a withanolide, induces apoptosis and has anti-cancer properties.

Thalidomide-O-C10-NH2: synthetic cereblon-based E3 ligase ligand-linker for PROTACs.

icFSP1 is a mitochondria-associated apoptosis-inducing factor regulator with antitumor activity for the study and treatment of tumor diseases.

RO5353 is a potent and orally active inhibitor of p53-MDM2.

Pyridinium bisretinoid A2E (A2E) is a fluorescent molecule isolated from the lipofuscin of retinal pigment epithelium, a weak photosensitizer.

Thalidomide-O-C2-acid: E3 ligase ligand-linker for PROTAC, with cereblon-derived Thalidomide component.

Schisandronic acid is a triterpenoid acid isolated from the stems of Schisandra propinqua.

eIF4E-IN-1 inhibits eIF4E and boosts immunity by targeting PD-1, PD-L1, LAG3, TIM3, IDO, aiding cancer and infection treatment.

Zapalog: photocleavable dimerizer controlling instant protein interactions.

Thalidomide-NH-PEG3-COOH is a cereblon-based E3 ligase ligand-linker for PROTAC synthesis.

Fascaplysin inhibits CDK4/D1 (IC50=0.35μM), triggers caspase-activated autophagy-apoptosis crosstalk, and blocks PI3K/AKT/mTOR in HL-60 cells.

Anticancer agent 52 exhibits potent cytotoxicity, induces apoptosis, and has potential in bladder cancer research.

INF 195 is an inflammasome NLRP3 inhibitor that can be used to study myocardial ischemia and myocardial infarction.

Thalidomide-Piperazine-PEG3-NH2: a cereblon ligand-linker for PROTAC E3 ligase recruitment.

Antitumor Photosensitizer-3 (Compound I), a chlorin derivative, effectively induces apoptosis and necrosis in tumor cells upon exposure to 650 nm laser

MNK8 is a potent STAT3 inhibitor, impairs DNA binding, and inhibits liver cancer cell growth.

Bursehernin is a useful organic compound for research related to life sciences and the catalog number is T124894.