Apoptose

<p>TopoisomeraseIIα-IN-10 (Compound 13r) is a topoisomerase IIα inhibitor that binds to the active site of DNA when complexed with topoisomerase IIα. This binding is stabilized through interactions with DNA base pairs and amino acid residues. By intercalating into DNA, TopoisomeraseIIα-IN-10 induces apoptosis and disrupts the mitochondrial membrane potential in HCT116 cells, effectively inhibiting their growth with an IC50 of 4.37 μM. It is applicable for cancer research studies.</p>

<p>BC13 is a CDK6/BRD4 inhibitor with IC50 values of 234 nM for CDK6 and 36 nM for BRD4. It exhibits antiproliferative properties, induces apoptosis (cell death) and DNA damage, and elevates ROS levels.</p>

<p>VEGFR-2-IN-61 (Compound 7b) is an inhibitor of VEGFR-2 with an IC50 of 2.83 µM. It effectively inhibits the proliferation of various cancer cells, including MCF-7 cells, with an IC50 of 2.12 µM. Additionally, VEGFR-2-IN-61 suppresses cell migration and induces oxidative stress and apoptosis in MCF-7 cells.</p>

<p>AMPK-IN-6 (compound 13a) is a potent AMPK inhibitor with an IC50 value of 0.093 µM. It induces apoptosis and suppresses autophagy. Additionally, AMPK-IN-6 exhibits antiproliferative activity and holds potential for research into pulmonary arterial hypertension.</p>

<p>Dual Galectin-3/EGFR-IN-1 (Compound 29) is a dual inhibitor targeting Galectin-3 and EGFR, with dissociation constants (KD) of 52.29 μM and 3.31 μM, respectively. It inhibits TGF-β-induced hepatic stellate cell (HSC) activation, induces apoptosis in LX-2 cells, and shows antifibrotic activity in the liver.</p>

<p>NSD-IN-4 (Compound A8) is a potent and orally active inhibitor of NSD3, inducing apoptosis in a dose-dependent manner. It demonstrates significant antitumor activity against lung squamous cell carcinoma.</p>

<p>IDOi-Pt(IV) prodrug-1 (Compound 10) is an IDOi-Pt(IV) prodrug that suppresses IDO expression. It induces apoptosis, reduces mitochondrial membrane potential, and inhibits tumor cell migration and invasion. Additionally, IDOi-Pt(IV) prodrug-1 triggers reactive oxygen species-mediated endoplasmic reticulum stress and the secretion of damage-associated molecular patterns (DAMPs), leading to immunogenic cell death (ICD). Compared to cisplatin, IDOi-Pt(IV) prodrug-1 exhibits relatively high efficiency and low toxicity in its antitumor activity.</p>

<p>Cardanol (C15:1), found in cashew nut shell liquid, induces mitochondria-associated apoptosis in human melanoma cells.</p>

<p>PRMT5-IN-33 (compound A8) is a selective inhibitor of PRMT5 that competes with SAM, exhibiting an IC50 of 10.9 nM. It induces apoptosis and inhibits the proliferation of Z-138 and MOLM-13 cells, demonstrating antitumor activity.</p>

<p>H-20 is a PD-1 agonist that reduces the required dosage of morphine for analgesia. It can be used in studies related to chronic pain.</p>

<p>Thevetiaflavone, a natural flavonoid from W. indica, blocks LDH leakage, boosting cell survival.</p>

<p>WK369 is an innovative small molecule inhibitor of BCL6, demonstrating remarkable bioactivity against ovarian cancer by inducing cell cycle arrest and triggering apoptosis. It binds directly to the BCL6-BTB domain, obstructing the interaction between BCL6 and SMRT, which results in the reactivation of p53, ATR, and CDKN1A.</p>

<p>Antimycobacterial agent-5 (compound 27) is an imidazopyridine amide compound that targets the Mycobacterium electron transport chain (ETC) respiratory CIII2CIV2 supercomplex. It acts on Mycobacterium smegmatis CIII2CIV2 with an IC50 of 441 nM.</p>

<p>(R)-1-(2-((2-MeO-4-(piperazin-1-yl)phenyl)amino)pyridin-4-yl)-N-(4-(CF3O)benzyl)piperidine-3-carboxamide HCl is anti-apoptotic and anti-cancer.</p>

<p>TopoisomeraseII inhibitor 17 (compound 4c) is a thiazolopyrimidine-based inhibitor of Topoisomerase II with an IC50 of 0.23 μM. This compound significantly disrupts the cell cycle and induces apoptosis.</p>

<p>WEE1-IN-7 (compound 12h) is a potent, orally active WEE1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and causes cell cycle arrest in the S phase, demonstrating antitumor activity.</p>

<p>LZFPN-90 (LZ90) is a dual-target compound aimed at NAMPT and PD-L1. It inhibits the interaction between PD-1/PD-L1 and NAMPT activity. LZFPN-90 suppresses cell growth in a NAMPT-dependent manner, blocking the cell cycle and subsequently inducing apoptosis. Additionally, LZFPN-90 exhibits target-dependent antitumor activity, impacting metabolic processes and the immune system.</p>

<p>ECDD-S16 is a potent inhibitor of pyroptosis. It effectively suppresses pyroptosis in Raw264.7 cells activated by surface and endosomal TLR ligands.</p>

<p>Necrosis inhibitor 2 hydrochloride (Compound B19) is an agent that inhibits cellular necrosis. It is useful for researching diseases associated with necrotic pathways, including inflammation, cancer, metabolic disorders, and neurodegenerative diseases.</p>

<p>Thalidomide-N-C3-O-C4-O-C3-OH is a conjugate of an E3 ligase ligand and a linker, used in the synthesis of the Aster-APROTAC degrader.</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>FC-116 is a potent Tubulin inhibitor with antitumour activity and inhibits tumour growth in mice.FC-116 induces apoptosis and promotes protein degradation.</p>

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

<p>SB 699551 is a selective 5-HT5A antagonist (Ki=6.31 nM) that enhances 5-HT neuronal function. It inhibits SERT (Ki=25.12 nM),inhibit breast cancer.</p>

<p>SACLAC is a cysteine asparaginase activation inhibitor with antitumor activity used in the study of acute myeloid leukemia and cancer.</p>

<p>Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.</p>

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

<p>Pacmilimab (CX-072) is a Probody immune checkpoint inhibitor targeting programmed death ligand 1 (PD-L1) with anti-tumor activity for the study of solid tumors.</p>

<p>Retifanlimab (MGA-012) is a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Retifanlimab is used in studies of Merkel cell carcinoma.</p>

<p>WF 10129 is a new angiotensin converting enzyme inhibitor generated by a fungus, Doratomyces putredinis.</p>

<p>"Urelumab (BMS-66513), a humanized IgG4 mAb CD137 agonist, boosts T-cell/NK cell-mediated cytotoxicity and anti-tumor activity."</p>

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

<p>Sterigmatocystine, a G1 phase and DNA synthesis inhibitor, curbs p21 and is a mycotoxin precursor from Aspergillus versicolor.</p>

<p>SB-1295, an orally active CDK9/T1 inhibitor with an IC50 of 0.17 μM, exhibits antiproliferative effects on HCT 116 and MIA PaCa-2 cells.</p>

<p>HKB99 suppresses NSCLC growth, metastasis, and overcomes erlotinib resistance.</p>

<p>Tyroserleutide HCl, a tripeptide from pig spleen, inhibits tumor growth in vivo/vitro.</p>

<p>Anti-Mouse PD-1 Antibody (RMP1-14) is an IgG2a antibody inhibitor against mouse PD-1 and can block PD-1/PD-L1 signaling. High-Quality, Low-Cost!</p>

<p>Avotaciclib hydrochloride, a CDK1 inhibitor, is the hydrochloride salt of Avotaciclib and exhibits potential therapeutic use in specific malignancies, including</p>

<p>FOXJ1 agonist 1 (compound 16c), an orally effective small molecule, effectively enhances FOXJ1 expression and acts on multiciliated cells (MCC) in the mammalian airway system to prevent chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 induces motile cilia production in the respiratory system of both zebrafish and mammals and inhibits elastase-induced COPD in mouse models. Additionally, Foxj1-IN-1 demonstrates good liver microsomal stability and favorable in vivo pharmacokinetic (PK) curves and area under the curve (AUC). It exhibits negligible inhibition of CYP and hERG and lacks significant cytotoxicity.</p>

<p>Annonacin is a cytotoxic acetogenin in Graviola leaf extract; it blocks mitochondrial complex and inhibits NKA/SERCA ATPase pumps.</p>

<p>Emavusertib (CA-4948) hydrochloride, a selective and potent IRAK4/FLT3 inhibitor, is designed for oral administration. It achieves an IC 50 of 57 nM against IRAK4 in a FRET kinase assay and demonstrates anti-tumor activity [1] [2] [3].</p>

<p>Ascochlorin, an isoprenoid antibiotic, inhibits STAT3 to combat tumors, induces apoptosis, and reduces inflammation.</p>

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

<p>Antitumor Photosensitizer-4 (compound 10b), a conjugate of dasatinib and imatinib, serves as a potent tyrosine kinase inhibitor (TKI) targeting ABCG2.</p>

<p>AlbA-DCA, a compound of Albiziabioside A and dichloroacetate, boosts ROS and reduces lactic acid in tumors, killing cancer cells and triggering apoptosis.</p>

<p>TAT-GluN2BCTM is a membrane-permeable peptide that selectively targets active DAPK1 (Death-associated protein kinase 1) for lysosomal degradation, thereby</p>

<p>PZ703b hydrochloride, a Bcl-xl PROTAC, triggers apoptosis and halts cancer growth; used in bladder cancer studies.</p>

<p>Thalidomide-O-amido-C8-NH2 hydrochloride, a synthetic cereblon ligand-linker for PROTAC synthesis.</p>

<p>Leucettamol A, from Leucetta microraphis, blocks LTB4 receptor and prevents Ubc13-Uev1A complex formation.</p>

<p>Cholicamideβ (compound 6), a self-assembling small molecule cancer vaccine adjuvant, forms low cytotoxicity virus-like particles and upon binding to peptide</p>

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

<p>Carnitine palmitoyltransferase 2 (CPT2), an enzyme involved in fatty acid oxidation, serves as a prognostic biomarker for colorectal cancer (CRC).</p>

<p>TAT-NEP1-40, a blood-brain barrier (BBB) permeable peptide, confers protection to PC12 cells against oxygen and glucose deprivation (OGD) while promoting</p>

<p>Ac-IEPD-AFC (IEPD) is a fluorescent substrate for granzyme B and can be used to measure granzyme B activity.</p>

<p>Compound 6, fac-[Re(CO)3(L6)(H2O)][NO3], a rhenium(I) tricarbonyl aqua complex, serves as an anticancer agent by disrupting mitochondrial function.</p>

<p>"(±)-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]."</p>

<p>Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial.</p>

<p>Compound Rh2 (Anticancer agent 133) is a cytotoxic and antimetastatic agent that induces cell cycle arrest, apoptosis, and autophagy.</p>

<p>Anticancer Agent 141 (Compound AE), an antimycin alkaloid, exhibits inhibitory potential against HPV-infected cervical cancer.</p>

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

<p>Anticancer Agent 146 (Compound 1.19) acts as a necroptosis inducer and demonstrates anti-tumor efficacy in the MDA-MB-231 mouse xenograft model [1].</p>

<p>PAK4-IN-3 (compound 27e) is a PAK4 inhibitor exhibiting an IC50 of 10 nM and demonstrates antiproliferative effects on A549 cells with an IC50 of 0.61μM.</p>

<p>β-Apopicropodophyllin, a natural product isolated from Hyptis wticillata, promotes apoptosis through mechanisms including microtubule disruption, DNA damage,</p>

<p>Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.</p>

<p>Pegsunercept (PEG sTNF-RI), a pegylated monoclonal antibody, selectively binds to TNFA, incorporating a polyethylene glycol (pegol) moiety [1].</p>

<p>Anticancer agent 136 (compound 22), a C17-triazole analogue of Geldanamycin (GDM), exhibits an IC50 value of 3.38 μM against human dermal fibroblasts (HDF) and</p>

<p>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.</p>

<p>Aromatase-IN-5 (Compound 10) is a potent inhibitor of aromatase with an IC50 value of 0.06 μM. It effectively blocks estrogen production and inhibits the proliferation of breast cancer cell lines such as MCF-7, arresting the cell cycle in the G1 phase and inducing apoptosis. Aromatase-IN-5 shows promise for breast cancer research.</p>

<p>Episilvestrol is a derivative of silvestrol with eIF4A-targeted antitumor properties, found in Aglaia silvestris fruits and twigs.</p>

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

<p>Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding &amp; osteoclastogenesis, induces PC12 cell apoptosis.</p>

<p>MG-277 is a molecular glue compound transformed from PROTAC degradation agent, MG-277 potently inhibits tumor cell growth in a p53-independent manner.</p>

<p>PI3Kδ-IN-16 is a selective and potent PI3Kδ inhibitor with anticancer and antiproliferative activity, induces cell cycle arrest and apoptosis.</p>

<p>LBM22, a CLK2 inhibitor, exhibits an IC50 value of 3.9 nM. It possesses anti-proliferative properties by inhibiting the phosphorylation of SR proteins. Additionally, LBM22 downregulates the expression of Wnt-related proteins and anti-apoptotic proteins, making it applicable in the study of non-small cell lung cancer.</p>

<p>DC 81: Streptomyces-derived antitumor antibiotic, potent nucleic acid synthesis inhibitor, binds DNA sequences, forms covalent adducts.</p>

<p>Sodium 2,4-dichlorophenoxyacetate: selective herbicide, controls broadleaf weeds by disrupting growth and protein/DNA synthesis.</p>

<p>OICR12694 (JNJ-65234637) TFA, an orally active B cell lymphoma 6 (BCL6) inhibitor [1], demonstrates effectiveness in targeting BCL6 pathways.</p>

<p>Galloflavin Potassium is an inhibitor of lactate dehydrogenase.</p>

<p>Cholesteryl Hemisuccinate Tris Salt is a cholesteryl ester with anticancer activity.Cholesteryl hemisuccinate has antitumor activity and inhibits tumor growth.</p>

<p>CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC50 of 0.21 μM. It exhibits cytotoxicity towards Vero cells with an IC50 of 28.52 μM.</p>

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

<p>STK17A/B-IN-1 hydrochloride is a potent, selective, orally active inhibitor of STK17A/B, displaying an IC50 value of 23 nM against STK17A. It is utilized in the research of tumors.</p>

<p>TRAP-1 (XJZ-06-462) is a p53 transcription activator that effectively activates mutant p53 and triggers the transcription of p53 target genes. In the p53Y220C pancreatic cell line, TRAP-1 rapidly upregulates p21 and other p53 target genes. TRAP-1 also inhibits cell proliferation, exhibiting IC50 values of 3.94 μM and 0.531 μM in BxPC-3 and A549 cell lines, respectively. Additionally, TRAP-1 modulates autophagy in lung cancer cells and provides protection against oxidative stress and apoptosis.</p>

<p>SZU-B6, a PROTAC degrader, targets and degrades SIRT6 with DC50 values of 45 nM in SK-HEP-1 cells and 154 nM in Huh-7 cells. It inhibits the proliferation of SK-HEP-1 cells with an IC50 of 1.51 μM and suppresses colony formation in both SK-HEP-1 and Huh-7 cell lines. Additionally, SZU-B6 induces apoptosis in SK-HEP-1 cells and causes cell cycle arrest at the G2/M phase. It demonstrates anti-tumor activity in murine models.</p>

<p>Thalidomide-NH-PEG2-COOH: a synthesized E3 ligase ligand-linker with cereblon ligand and PROTAC linker.</p>

<p>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.</p>

<p>(Rac)-BIO8898 is a chemical compound that serves as an inhibitor of the co-stimulatory interaction between CD40 and CD154.</p>

<p>Thiocolchicine inhibits tubulin polymerization (IC50: 2.5 µM, Ki: 0.7 µM), induces apoptosis, and serves as an ADC cytotoxin.</p>

<p>Lenercept (Ro 45-2081) is a recombinant fusion protein combining the soluble TNF-receptor (p55) with the Fc portion of human IgG1 [1].</p>

<p>CRP protein and its fragment (174-185, RS-83277) boost human monocyte and macrophage cancer-killing effects in vitro.</p>

<p>Tripchlorolide is a useful organic compound for research related to life sciences and the catalog number is T126047.</p>

<p>RMC-7977 is a inhibitor of the active (GTP-bound) forms of KRAS, HRAS, and NRAS with anticancer activity for the study of solid tumors with KRAS G12C mutations.</p>

<p>Rasagiline (AGN1135) is an inhibitor of monamine oxidase used as adjunctive therapy in combination with levodopa and carbidopa in the management of Parkinsons</p>

<p>Poly(I:C):Kanamycin (1:1) sodium is a complex.Poly(I:C) is a TLR3 and RIG-I/MDA5 agonist.Kanamycin is an antimicrobial,Gram-negative and positive bacteria.</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>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>Amino acids 17-41 of lactoferrin, lactoferricin B, enhance anti-fungal effects, targeting Candida Albicans.</p>

<p>P53R3 is a potent reactivator of p53, effectively restoring sequence-specific DNA binding to several p53 hot spot mutants, namely p53 R175H, p53 R248W, and p53</p>

<p>Angiogenesis Inhibitor 3 (compound 8) is a potent anti-cancer agent, blocking HUVEC/HCT-15 cell growth and inducing apoptosis.</p>

<p>Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.</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>Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.</p>

<p>TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor exhibiting a dissociation constant (K D) of 12.06 μM.</p>

<p>Petromurin C, a bis-indolyl benzenoid from P. muricatus, is cytotoxic to NS-1 cells (IC50=33μg/ml) and active against T. foetus (IC50=100μg/ml).</p>

<p>Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.</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>DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.</p>

<p>eIF4E-IN-5 (Compound 6n) is a cell-permeable eIF4E inhibitor that binds to capped mRNA, thereby inhibiting cap-dependent translation [1].</p>

<p>Bcl-xL antagonist 2 is an effective and selective antagonist of Bcl-xL with an IC50 of 91 nM and a Ki of 65 nM.</p>