Apoptosis

<p>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.</p>

<p>PD-L1 inhibitor IV, a polypeptide, competitively blocks hPD-1 with a Kd of 1.38 μM, preventing hPD-1/hPD-L1 interaction.</p>

<p>Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .</p>

<p>Thalidomide-4-C3-NH2 HCl is a cereblon ligand for CRBN recruitment, used to make PROTACs with a linker.</p>

<p>Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.</p>

<p>Ac-LEVD-CHO, a caspase-4 inhibitor, is a peptide with the sequence Ac-Leu-Glu-Val-Asp-al [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>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>Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin &gt; R837 [1].</p>

<p>Trilexium (TRX-E-009-1), a third-generation benzopyran structurally related to TRX-E-002-1, increases p21 protein expression, induces apoptosis, depolymerizes microtubules, and demonstrates broad anti-cancer activity [1] [2].</p>

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

<p>Boc-Asp(OBzl)-CMK, an inhibitor of IL-1 converting enzyme (ICE, caspase1), prevents the death of CHP100 neuroblastoma cells and inhibits IL-1β release induced by the viral coat protein [1].</p>

<p>PBE-AMF is a prodrug that activates H2O2 and exhibits anticancer activity. It impedes tumor proliferation by inhibiting DNA synthesis, reducing ATP levels, inducing cell death (apoptosis), and blocking the cell cycle. PBE-AMF effectively and selectively inhibits the proliferation of MDA-MB-231 cells (IC50=6.4 μM) while sparing non-cancerous MCF-10A cells.</p>

<p>Pep19-2.5: Synthetic antitoxin peptide inhibits LP/LPS signals via PRRs, preventing inflammation and pyroptosis.</p>

<p>TNF-α antagonist is an exocyclic peptide that mimics the critical TNF-α recognition loop on TNF receptor I complex and, thus, prevents ligand interaction with</p>

<p>Nargenicin: a macrolide antibiotic effective against S. aureus, MRSA, M. luteus; inhibits bacterial DnaE and reduces inflammation and leukemia cell growth.</p>

<p>Thalidomide-PEG4-NH2 HCl, a cereblon ligand-linker for PROTAC.</p>

<p>Thalidomide-derived cereblon ligand with PROTAC linker as an E3 ligase ligand-linker conjugate, in hydrochloride form.</p>

<p>Relfovetmab is an anti- NGF monoclonal antibody (mAb) [1] .</p>

<p>Satratoxin G, from Stachybotrys chartarum, triggers apoptosis in nasal and brain OSNs.</p>

<p>Dimethachlor is a pesticide and herbicide used in wetland areas.</p>

<p>Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.</p>

<p>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.</p>

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

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

<p>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.</p>

<p>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.</p>

<p>FAK-IN-25 (4c) is an inhibitor of FAK with an IC50 value of 50.98 nM. It induces apoptosis and causes cell cycle arrest in the G1 phase, making it relevant for cancer research.</p>

<p>YX0798 is a selective, orally active CDK9 inhibitor (Kd: 0.28 nM). It downregulates the oncogenic protein c-MYC and the pro-survival protein MCL-1. YX0798 disrupts the cell cycle and causes transcriptome reprogramming, ultimately leading to apoptosis. The compound exhibits antitumor activity.</p>

<p>CDK2-IN-45 is a CDK2 inhibitor with an IC50 value of 0.64 μM. It effectively inhibits the proliferation of DU-145 and PC-3 cell lines, with IC50 values of 2.20 μM and 4.17 μM, respectively. Additionally, CDK2-IN-45 induces G0/G1 phase cell cycle arrest and apoptosis. It is utilized in prostate cancer research.</p>

<p>Holothurin A is a triterpene glycoside.</p>

<p>TRAP1-IN-1 is a selective TRAP1 inhibitor, induces degradation of TRAP1 downstream proteins, inhibits OXPHOS, and disrupts mitochondrial membrane potential.</p>

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

<p>Thymidine 3',5'-diphosphate tetrasodium inhibits staphylococcal nuclease, SND1 &amp; tyrosyl nuclease; has anti-tumor properties &amp; catalyzes biochemical reactions.</p>

<p>Nerelimomab (BAYX1351), an anti-TNF-α antibody, is utilized in sepsis research [1] [2].</p>

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

<p>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.</p>

<p>Apolizumab (Hu1D10) is a humanized antibody targeting HLA-DR beta-chain; induces apoptosis in CLL cells in vitro.</p>

<p>RO5353 is a potent and orally active inhibitor of p53-MDM2.</p>

<p>4-Nitrothalidomide is a modified form of thalidomide that inhibits the growth and proliferation of HUVEC cells and is commonly used in the synthesis of pomalidomide, which has anticancer potential.</p>

<p>MK-0731 inhibits kinesin spindle protein, disrupting mitosis and triggering apoptosis in KSP-overexpressing tumor cells.</p>

<p>RLX HCl is anticancer, inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a in experimental colon cancer, antiproliferative.</p>

<p>Kurzipene D: anticancer, induces apoptosis, halts HepG2 at S phase, anti-tumor in zebrafish, inhibits tumor growth and spread.</p>

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

<p>Schisandronic acid is a triterpenoid acid isolated from the stems of Schisandra propinqua.</p>

<p>ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.</p>

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

<p>XIAP BIR2/BIR2-3 Inhibitor-3 functions as a dual inhibitor targeting both BIR2 and BIR2-3 domains, exhibiting potent activity with IC50 values below 1 nM. This compound is utilized in cancer research [1].</p>

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

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

<p>Compound Ir5 (Antitumor agent-145) serves as a tumor inhibitor characterized by significant fluorescence and mitochondrial targeting. It promotes anti-cancer activity by inducing necroptosis and stimulating the necroptosis-related immune response [1].</p>

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

<p>PDE4B-IN-4 is an inhibitor of PDE4B (IC50: 2.82 nM) and TNF-α (IC50: 7.20 nM). It demonstrates anti-inflammatory properties by reducing neutrophilia in a mouse model of lipopolysaccharide (LPS)-induced sepsis.</p>

<p>Sodium cyclamate is a carbonic anhydrase inhibitor, artificial sweetener, with anticonvulsant properties, and used in cancer research.</p>

<p>5-(N,N-Hexamethylene)-amiloride (5-HMA) is an amiloride derivative that inhibits TRPA1-mediated calcium signaling (IC50: 35 μM). It functions as an inhibitor of the Na+/H+ exchanger (NHE) with Ki values ranging from 0.013 to 2.4 μM for various NHE isoforms. Additionally, 5-HMA blocks ASIC3 channels by 51% at 20 μM.</p>

<p>Melatonin D5, a deuterium-labeled version of melatonin, is a hormone produced by the pineal gland, known for its role as a selective ATF-6 inhibitor that promotes apoptosis in human hepatoma cells via COX-2 downregulation. Additionally, it activates melatonin receptors and exhibits antioxidative and anti-inflammatory properties.</p>

<p>PARG-IN-4 (compound A) is an orally active and cell-membrane permeable PARG inhibitor (EC50=1.9 nM) that inhibits tumour growth in mice with antitumour .</p>

<p>ML291 triggers UPR, causing apoptosis in solid cancers by activating PERK/eIF2a/CHOP pathway and reducing leukemia cells.</p>

<p>Isoscabertopin has anticancer activity.</p>

<p>(-)-Apomorphine hydrochloride hydrate is a broad-spectrum dopamine agonist and ferroptosis inhibitor.</p>

<p>Thalidomide-O-amido-C4-NH2 is a thalidomide cereblon ligand-linker used for PROTAC synthesis as an E3 ligase.</p>

<p>SLF is a synthetic ligand for FKBP12 and increases Ca2+ efflux and protein synthesis.</p>

<p>(E/Z)-E64FC26 is a protein disulfide isomerase (PDI) family inhibitor with affinity for PDIA1, PDIA3, PDIA4, TXNDC5, and PDIA6.</p>

<p>NU 9056 is an effective and selective inhibitor of KAT5 histone acetyltransferase with an IC50 of 2 µM.</p>

<p>(Rac)-Apremilast D5 is a deuterium-labeled version of the enantiomer (R)-Apremilast, also known as (R)-CC-10004, which itself is one specific form of Apremilast</p>

<p>Sodium catechol sulfate is a bioactive chemical.</p>

<p>Chiisanoside is a useful organic compound for research related to life sciences. The catalog number is T123983 and the CAS number is 89354-01-8.</p>

<p>Gemcitabine elaidate (CP-4126), is a lipophilic, unsaturated fatty acid ester derivative of gemcitabine (dFdC), an antimetabolite deoxynucleoside analogue, with</p>

<p>PGV-1, an oral Curcumin analog, induces apoptosis by inhibiting COX-2, VEGF, and NF-κB activation.</p>

<p>Acyclovir (Aciclovir) hydrochloride is an effective oral antiviral agent with potent anti-herpetic activity. It exhibits IC50 values of 0.85 μM for HSV-1 and 0.86 μM for HSV-2, indicating strong inhibitory effects against these strains. Additionally, Acyclovir hydrochloride induces cell cycle disturbances and apoptosis. This compound also prevents bacterial infections during induction therapy for acute leukemia.</p>

<p>Busulfan-d8 (Sulphabutin-d8) is the 2H-labeled Busulfan. Busulfan is an anticancer agent with immunosuppressive and myeloablative chemotherapy activities.</p>

<p>EIF2α activator 2 is an activator of eIF2α phosphorylation, anti-proliferative in SRB, K562, and PBMC cells, suitable for cancer research.</p>

<p>FMAU (2'-Deoxy-2'-fluoro-5-methyl-beta-D-arabinouridine) is a thymine nucleoside analog with insertional activity on replicating DNA.FMAU can be used to label</p>

<p>Methylisothiazolinone is a powerful synthetic biocide and preservative.</p>

<p>2'-Deoxy-2'-fluoro-beta-D-arabinoguanosine is a purine nucleoside analog with a broad spectrum of antitumor activity, targeting malignant tumors of the inert</p>

<p>Thalidomide-O-amido-PEG4-C2-NH2 hydrochloride is a synthesized E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and a</p>

<p>ODN 1826 is a TLR9 agonist and immunostimulant, which has antitumor effects and promotes cell apoptosis.</p>

<p>1-(2-Deoxy-2-fluoro-beta-D-arabinofuranosyl)uracil is a Nucleoside, fluoro-modified nucleoside; Arabino-nucleosidde.</p>

<p>4-Thiothymidine is a Nucleoside Derivative - Thio-nucleoside, 5-Modified pyrimidine nucleoside.</p>

<p>6-Azauridine is a purine analog with antitumor effects, inhibiting DNA synthesis and inducing apoptosis in lymphatic cancers.</p>

<p>RKI 1447 dihydrochloride: selective ROCK inhibitor, inhibits colorectal cancer growth, promotes apoptosis (ROCK1 IC50=14.5 nM, ROCK2 IC50=6.2 nM).</p>

<p>Traumatic Acid aids wound healing in plants by stimulating cell division to create a callus.</p>

<p>Mycophenolic acid-d3 is a derivative that lowers GTP, affects RNA polymerase II transcription, changes polyadenylation, and counters cordyceps.</p>

<p>MPPa, a PDT photosensitizer derived from chlorophyll a, absorbs at 667/674 nm with no dark cytotoxicity.</p>

<p>Cis-5-Norbornene-exo-2,3-dicarboxylic Anhydride: sensitizing, induces HepG2/SK-Hep1 apoptosis, inhibits PP2A. IC50: HepG2=62μM, SK-Hep1=151μM.</p>

<p>PI-103 Hydrochloride is a dual PI3K/Akt and mTOR inhibitor exhibiting nM-level inhibition of p110α, p110β, p110δ, p110γ, DNA-PK, mTORC1, and mTORC2.</p>

<p>FKBP12 PROTAC RC32 is a PROTAC-like degrader targeting FKBP12. It can degrade FKBP12 in organs after intraperitoneal administration.</p>

<p>Ibuprofen D3 is a deuterium labeled Ibuprofen. Ibuprofen is a COX-1 and COX-2 inhibitor (IC50s: 13 μM and 370 μM).</p>

<p>Sunitinib D10, a deuterium-enriched version, inhibits VEGFR2 and PDGFRβ tyrosine kinases (IC50: 80 nM/2 nM).</p>

<p>Diphenyl disulfide fights breast cancer by inducing cell death and stopping growth.</p>

<p>Celosin K (compound 8), isolated from Semen Celosiae seeds, effectively inhibits t-BHP-induced neuronal injury.</p>