Apoptosis

<p>Cyclamic acid, a synthetic sweetener (NSC-220327), often used as Na/Ca cyclamate. Banned in USA over disputed cancer risk.</p>

<p>Benazepril hydrochloride (CGS 14824A HCl) is an angiotensin-converting enzyme (ACE) inhibitor widely used in the therapy of hypertension.</p>

<p>Chlorhexidine diacetate (Bactigras) is a disinfectant and topical anti-infective agent used also as mouthwash to prevent oral plaque.</p>

<p>Fluvastatin sodium (Fluvastatin sodium salt), a competitive inhibitor of hydroxymethylglutaryl-coenzyme A reductase (HMGCR), is a commonly used cholesterol</p>

Tolperisone hydrochloride (Muscalm) is a muscle relaxant for treating muscle tone disorders from neurological diseases.

<p>Farudodstat (ASLAN003) is an orally active and potent inhibitor of DHODH with antitumor activity. It has the potential to be a first-in-class candidate in AML.</p>

<p>9-ING-41 is a glycogen synthase kinase-3 inhibitor.</p>

<p>Copanlisib dihydrochloride: ATP-competitive PI3K inhibitor, potent for PI3Kα/δ/β/γ, antitumor, 2000x selectivity over other kinases except mTOR.</p>

Roxithromycin (RU-28965) is a semi-synthetic derivative of the macrolide antibiotic erythromycin with antibacterial and anti-malarial activities.

<p>Ceftiofur sodium (Naxcel), an antibiotic of the cephalosporin type (third generation), is used as veterinary medicine.</p>

<p>Mevastatin (ML236B) is an HMG-CoA reductase inhibitor that was initially isolated from the mold Pythium ultimum.</p>

<p>LAT1-IN-1 (BCH) is a selective and competitive inhibitor of L-type amino acid transporter protein 1 (LAT1). LAT1-IN-1 has antitumor activity. Cost-effective and quality-assured.</p>

<p>Mitotane (NCI-C04933) is a derivative of the insecticide dichlorodiphenyldichloroethane that specifically inhibits cells of the adrenal cortex.</p>

<p>Teneliximab (BMS 224819) is a chimeric monoclonal antibody that blocks CD40-CD40L interactions.Cost-effective and quality-assured.</p>

<p>Ketoprofen (RP-19583) is a propionic acid derivate and nonsteroidal anti-inflammatory drug (NSAID) with anti-inflammatory, analgesic and antipyretic effects.</p>

<p>Ritonavir (ABT 538) inhibits HIV-1/2 proteases; serum proteins limit it but it enhances other HIV drugs by hindering P450 degradation.</p>

<p>Salicylic acid (2-Hydroxybenzoic acid), a natural compound extracted from Willow bark, is an anti-inflammatory inhibitor of activity cyclooxygenase.</p>

Dasatinib monohydrate, an oral SRC-kinase inhibitor, counters imatinib-resistant chronic myeloid leukemia.

(S,S)-TAPI-1 FA is a TNF-α processing inhibitor with potential anti-inflammatory effects, blocks TACE, and can inhibit TNF-α signaling can be used to study Staphylococcus aureus arthritis.

<p>Sodium etidronate (Didronel), a bisphosphonate, resists degradation, inhibits osteoclasts, and may boost bone formation.</p>

<p>Risedronate Sodium treats osteoporosis; it's an etidronic acid derivative and blocks calcium channels to prevent bone loss.</p>

Floxuridine (FUDR) is an antimetabolite, floxuridine inhibits thymidylate synthase, resulting in disruption of DNA synthesis and cytotoxicity.

<p>Benzydamine hydrochloride (AF864), a locally-acting nonsteroidal anti-inflammatory drug, has local anaesthetic and analgesic properties.</p>

<p>Ragifilimab (INCAGN-1876), a GITR-targeting agonist antibody, may treat advanced solid tumors.</p>

<p>Bcl-2-IN-4: potent, selective, oral Bcl-2 inhibitor with 1.5 nM IC50, &gt;200x selectivity over Bcl-xL.</p>

<p>Mcl-1 Inhibitor 15 (Compound (Ra)-15), with a K i of 0.02 nM, is utilized in cancer research [1].</p>

<p>Phosphocreatine dipotassium, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives.</p>

<p>Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.</p>

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

<p>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.</p>

<p>HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/</p>

<p>Thalidomide-based E3 ligase ligand with PEG2-C2 linker; used as an immunomodulatory cancer treatment.</p>

<p>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.</p>

<p>Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [1].</p>

<p>1-(4-chloro-3-(trifluoromethyl)phenyl)-3-(7-(1-methyl-1H-pyrazol-4-yl)-2,3,4,9-tetrahydro-1H-carbazol-3-yl)urea 是一种能够激动 TNF-α的化合物，可以诱导细胞分泌 TNF-α。</p>

<p>Pamlectabart is a humanised antibody targeting TNFRSF17/BCMA, (ADC) Pamlectabart tismanitin multiple myeloma.</p>

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

<p>Deoxynyboquinone is a potent inducer of cancer cell death with IC(50) values between 16 and 210 nM.</p>

<p>PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.</p>

<p>Prodigiosin is a secondary metabolite of Symbiotic bacteria. It also has anti-fungal and anti-cancer activity.</p>

<p>LY3415244 is a human bispecific antibody (bsAb) that targets B7-H1/PD-L1/CD274 and TIM-3/HAVCR2/CD366. This compound is applicable in the study of advanced solid tumors.</p>

XZ739: Cereblon-based PROTAC, degrades BCL-XL (DC50 2.5 nM in MOLT-4, 16hr), induces caspase apoptosis.

<p>Xerophilusin B from Isodon xerophilus halts ESCC cell growth, causes G2/M arrest, and induces apoptosis.</p>

<p>PKM2-IN-8 (Compound 9b) is an inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.31 μM. It exhibits potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 induces early apoptosis and reduces lactate levels. This compound is useful for research in glioblastoma.</p>

<p>Tomuzotuximab: fully human, glycoengineered IgG1 anti-EGFR monoclonal antibody with anticancer properties.</p>

<p>Conjugated 18-C ω-6 fatty acid from Jacaranda seeds, induces cancer cell apoptosis via oxidative stress; metabolizes to cytotoxic CLA.</p>

<p>G-Glu-Val (γ-glutamyl-L-valine, H-Glu-Val -OH), a flavour-regulating dipeptide, is a major contributor to "mellow".</p>

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.

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

<p>KP1019 is now discontinued.</p>

<p>VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.</p>

<p>Albicanol is a biochemical.</p>

<p>Z-VEID-FMK is a selective caspase-6 peptide inhibitor that irreversibly covalently binds to the enzyme, thereby inhibiting apoptosis and DNA breakage.</p>

<p>2-deoxy-D-Glucose-13C6 is an internal standard for GC/LC-MS, a glycolysis inhibitor, and induces apoptosis in certain cells at 2 mg/ml.</p>

<p>Ac-Trp-Glu-His-Asp-Aldehyde is a powerful and selective inhibitor of caspase-1, demonstrating a K_i value of 56 pM [1] [2].</p>

<p>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.</p>

<p>PD-1-IN-20 is the less active enantiomer of PD-1-IN-1.</p>

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

<p>N-Acetylpsychosine, also known as α-galactosylated C2-ceramide (d18:1/2:0), exhibits immunostimulatory properties.</p>

<p>Thalidomide-O-C8-Boc: CRBN ligand for PROTAC creation, derived from Thalidomide.</p>

<p>P1D-34 is a Pin1 PROTAC degrader with a DC50 value of 177 nM. It downregulates Pin1 substrate proteins, including Cyclin D1, Rb, Mcl-1, Akt, and c-Myc. Additionally, P1D-34 exhibits antiproliferative activity across various acute myeloid leukemia (AML) cell lines and induces DNA damage and apoptosis by generating reactive oxygen species (ROS).</p>

<p>PPA-904 FA is a cationic photosensitizer with antimicrobial activity that can be used to study chronic leg ulcers and diabetic foot ulcers.</p>

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

<p>Anti-Mouse PD-L1 Antibody (10F.9G2) is an IgG-class antibody against mouse PD-L1.</p>

<p>Tralokinumab: human IgG4 monoclonal antibody, blocks IL-13, may treat atopic dermatitis.</p>

<p>AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity.</p>

<p>TTQ-SA is a near-infrared spiraling aggregation-induced emitter capable of converting near-infrared light (NIR) into thermal energy, resulting in thermal damage and death of tumor cells. In cancer cells MF-7, TTQ-SA shows cell uptake and targeting capabilities. TTQ-SA binds with DNAzyme to inhibit the expression of the survivin gene, enhancing the sensitivity of tumor cells to photothermal therapy.</p>

<p>MS78, an acetylation targeting chimera (AceTAC), specifically acetylates the p53Y220C mutant by recruiting the histone acetyltransferase p300/CBP.</p>

<p>Vallesiachotamine, a recognized monoterpene indole alkaloid, exhibits anti-tumor activity [1].</p>

<p>Ropeginterferon alfa-2b (Ropeginterferon alfa-2b-njft), a monopegylated interferon-alpha (IFN-α), is utilized in the study of myeloproliferative neoplasms [1].</p>

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

<p>MDMX/MDM2-IN-2 is a potent dual inhibitor of p53-MDM2/MDMX, demonstrating dissociation constants (Kis) of 0.23 μM for MDM2 and 2.45 μM for MDMX.</p>

<p>Potent GAL2/GAL3 agonist (EC50 = 45.7, 112.2 nM), inactive at GAL1. Reduces appetite, fatty acid uptake in adipocytes, and LH in goldfish; anxiolytic in vivo.</p>

<p>ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor that binds to ROR1's extracellular Frizzled domain, effectively inhibiting aberrant</p>

<p>DHFR-IN-23 (compound 5) is a dual inhibitor of DNA binders/DHFR, exhibiting an IC50 value of 0.08 μM against hDHFR. It serves as an apoptosis inducer and is applicable in research on ER+ breast cancer.</p>

<p>P-gp inhibitor 16 (compound 14) is an inhibitor of p-glycoprotein. It significantly enhances apoptosis induced by doxorubicin and displays anticancer properties.</p>

Met-12 is a peptide inhibitor of the Fas receptor. It suppresses Fas receptor-mediated apoptosis in photoreceptor cells and reduces Caspase activation, making it a potential candidate for research on photoreceptor protectants.

<p>Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].</p>

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

<p>FB49 is a selective Bcl-2-associated athanogene 3 (BAG3) inhibitor with a Ki of 45 μM.</p>

<p>Cytotoxic and antiproliferative effects of Hellebrin on breast and lung cancer cells.</p>

<p>NCT-58 is a potent HSP90 inhibitor that blocks Akt, downregulates HER family, and induces apoptosis in HER2+ breast cancer without triggering HSR.</p>

<p>YN14-H is a PROTAC degrader that targets KRASG12C. It effectively inhibits the growth of NCI-H358 and MIA PaCa-2 cells, with IC50 values of 0.042 μM and 0.021 μM, respectively, and DC50 values of 28.9 nM and 18.1 nM. YN14-H significantly induces apoptosis and suppresses cell migration. It demonstrates favorable pharmacokinetics and excellent in vivo antitumor activity.</p>

<p>Bromoiodoacetamide (I-HAcAm): cytotoxic, induces ROS &amp; apoptosis in HepG-2 cells.</p>

<p>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.</p>

<p>Biotin-PEG6-Thalidomide is a PROTAC linker based on PEG.</p>

<p>Anticanceragent 178 (compound C2) is a potent anticancer compound. It effectively inhibits the proliferation and metabolic activity of MDA-MB 231 cells, with IC50 values of 1.1 and 4.2 μM, respectively. Additionally, Anticanceragent 178 induces ferroptosis and necroptosis in cells.</p>

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

<p>Chlopynostat (Compound 6c) is an HDAC1 inhibitor with an IC50 value of 67 nM. It induces apoptosis by inhibiting HDAC1, thereby reversing STAT4/p66Shc defects.</p>

<p>Opucolimab is a human antibody targeting PD-L1, used in advanced solid tumor research and antibody-drug conjugate synthesis.</p>

<p>EAD1 is a useful organic compound for research related to life sciences. The catalog number is T35329 and the CAS number is 1644388-26-0.</p>

<p>Thalidomide-O-PEG2-propargyl is a cereblon-based E3 ligase ligand with a PEG linker for PROTAC-induced protein degradation.</p>

<p>Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.</p>

<p>JPS014 TFA, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC</p>

<p>4-hydroperoxy cyclophosphamide (4-OOH-CY) induces hepatotoxicity. It increases ghrelin levels and enhances inflammatory factors and oxidative markers.</p>

CBI1 is a covalent BAX inhibitor. It selectively derivatizes BAX at C126 and inhibits BAX activation by triggering a ligand or through point mutations. CBI1 prevents the lipidation and oligomerization of BAX by t-2-hex. It also inhibits BAX activation induced by BH3 ligands, F116A mutation, or t-2-hex.

<p>Shepherdin 79-87: Amino acid fragment 79-87 of Hsp90/Survivin antagonist with anticancer properties.</p>

<p>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).</p>