Apoptose

<p>GSK2245035: selective nasal TLR7 agonist, boosts Type-1 IFN (pEC50: 9.3 IFNα, 6.5 TFNα), curbs Th2 cytokines in blood cultures.</p>

<p>(+)-Apogossypol is an antagonist of pan-BCL-2. (+)-Apogossypol binds to Mcl-1(Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 μM, respectively).</p>

<p>PD-1/PD-L1-IN-22 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interactions that blocks PD-1/PD-L1 interactions (IC50: 0.732 μM).</p>

<p>SD 1008 is a JAK2/STAT3 signaling pathway inhibitor. SD 1008 inhibits activation of STAT3, JAK2, and Src.</p>

<p>Colletofragarone A2 from Colletotrichum sp. blocks mutant p53 and HSP90, aiding cancer treatment.</p>

<p>Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM).</p>

<p>WEHI-345 analog is an Src inhibitor.</p>

<p>Prostaglandin A1, a dehydration derivative of Prostaglandin E1, demonstrates inhibitory effects on tumor growth, inflammation, virus replication, platelet aggregation, and excitotoxin-induced neuron apoptosis [1].</p>

<p>YM281 is a potent EZH2 inhibitor, causes apoptosis and G0/G1 arrest, has antitumor activity in vivo, and may be researched for lymphoma.</p>

<p>BAI1 hydrochloride is a selective inhibitor of the apoptosis factor BAX, functioning through an allosteric mechanism. By binding to BAX, it allosterically inhibits its activation, showcasing potential applications in the research of diseases mediated by BAX-dependent cell death [1].</p>

<p>GCN2-IN-6: Potent, oral GCN2/PERK inhibitor; IC50s - GCN2: 1.8 nM (enzymatic), 9.3 nM (cellular); PERK: 0.26 nM (enzymatic), 230 nM (cellular).</p>

<p>PLK1/BRD4-IN-1 (9b) is an orally active dual inhibitor of PLK1 (IC50: 22 nM) and BRD4 (IC50: 109 nM).</p>

<p>Nedometinib (NFX-179) is a MEK1 inhibitor with anticancer and antitumor activities, which can be used to study malignant tumors.</p>

<p>Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide derived from bovine lactoferrin spanning residues 17-41, exhibits broad-spectrum antimicrobial properties against Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi. Additionally, this compound demonstrates antitumor activities [1] [2].</p>

<p>Ethylene glycol dimethacrylate, a methacrylate monomer, demonstrates cytotoxic and genotoxic impacts on human gingival fibroblasts (HGFs), elevating</p>

<p>SM-433: Smac mimetic, blocks IAPs, strong XIAP BIR3 affinity (IC50 &lt;1 μM). See patent WO2008128171A2.</p>

<p>Ezatiostat HCl (TLK199) inhibits glutathione S-transferase, GSTP1-1 specifically, and may treat cytopenias.</p>

<p>RIP2 kinase inhibitor 2 is a receptor-interacting protein-2 kinase inhibitor.</p>

<p>ERα antagonist 1 is a selective, potent, covalent estrogen receptor alpha (ERα) antagonist that blocks the cell cycle of MCF-7 cells in G0/G1 phase and induces</p>

<p>Q-VD-OPh: broad-spectrum, non-toxic caspase inhibitor; cost-effective, specific for apoptotic inhibition.</p>

<p>(S)-Sabutoclax ((S)-BI-97C1), an optically pure derivative of apogossypol, serves as a pan-active inhibitor of the antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. It effectively blocks the binding of BH3 peptides to key proteins in the family, including Bcl-XL, Bcl-2, Mcl-1, and Bfl-1, displaying inhibitory concentration (IC50) values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. Furthermore, (S)-Sabutoclax demonstrates potent efficacy in inhibiting the growth of various cancer cell lines, such as those from human prostate cancer, lung cancer, and lymphoma, with half-maximal effective concentration (EC50) values of 0.13, 0.56, and 0.049 μM, respectively. This compound is utilized in research focusing on apoptosis-based cancer therapies [1].</p>

<p>N-Oleoyl serinol, a ceramide analog, plays a crucial role in stem cell therapy by inhibiting the development of teratomas in stem cells. It triggers apoptosis in remaining pluripotent embryoid body-derived cells (EBCs), thwarts teratoma formation, and promotes the enrichment of EBC cells that proceed to neural differentiation post-transplantation [1].</p>

<p>SCH79797 dihydrochloride is a PAR1 antagonist with IC50 70 nM, Ki 35 nM, antiproliferative, and pro-apoptotic properties.</p>

<p>Delmitide acetate (RDP58) is an orally active d-isomer decapeptide that exhibits potent anti-inflammatory properties.</p>

<p>RET-IN-24 (Compound 26) is a selective inhibitor of RET tyrosine kinase, demonstrating antitumor activity [1].</p>

<p>HS148 selectively inhibits DAPK3 (Ki 119 nM), reducing gastric cancer progression via ULK1-dependent autophagy and tumor suppression pathways.</p>

<p>15-Deoxy-Δ12,14-Prostaglandin A1, a deoxyanalog of prostaglandins, inhibits NF-κB signaling and induces apoptosis. It also prevents TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecules (CAM) and reduces monocyte arrest [1].</p>

<p>AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.</p>

<p>Ataquimast is used in curing advanced receptor-positive breast cancer.</p>

<p>K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM.</p>

<p>ICL-CCIC-0019 inhibits ChoKα, causes G1 arrest, ER stress, and cancer cell apoptosis.</p>

<p>Lacutoclax (LP-108) is an orally active and selective Bcl-2 inhibitor with antitumor activity both in vivo and ex vivo，lymphoma and leukemia.</p>

<p>MI-219 is a human double minute 2 (HDM2) inhibitor.</p>

<p>Z-LLY-FMK (Calpain Inhibitor IV) serves as an inhibitor of calpain, a family of proteases implicated in the apoptosis of various cell systems.</p>

<p>A-1293102 is a potent, selective inhibitor of BCL-XL, effective in inducing apoptosis in tumor cells reliant on BCL-XL [1].</p>

<p>MK-2206 free base is an allosteric Akt inhibitor that is both potent and selective, administered orally, exhibiting IC50 values of 8, 12, and 65 nM for Akt1,</p>

<p>CIL62 is a caspase-3/7-independent inducer of cell death. The mechanism of action of CIL62 is Necrostatin-1 dependent cell death [1].</p>

<p>Ro 41-5253 is a RARα antagonist with antitumor activity that inhibits the proliferation of ZR-75.1 estrogen receptor-positive breast cancer cells.</p>

<p>RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal</p>

<p>Ogremorphin (GPR68-IN-1) is a potent inhibitor of GPR68, exhibiting an EC50 of 170 nM.it is utilized in the study of autoimmune chronic inflammatory diseases [1</p>

<p>NSC194598 is a p53 DNA-binding inhibitor, demonstrating an in vitro IC50 of 180 nM and an in vivo range of 2-40 μM.</p>

<p>PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.</p>

<p>HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4.</p>

<p>C 87: Small-molecule TNF-α inhibitor, binds TNFα, inhibits cytotoxicity with IC50 of 8.73 μM, blocks signaling.</p>

<p>IK-862 is a selective TACE inhibitor with potential anti-inflammatory and anticancer activity for the study of neuritis.</p>

<p>HDAC-IN-59 (compound 13a), a potent histone deacetylase (HDAC) inhibitor, enhances intracellular reactive oxygen species (ROS) production, induces DNA damage,</p>

<p>GNE-900 is an ATP-competitive ChK1 inhibitor with selective and oral activity.GNE-900 inhibits ChKl and ChK2 with IC50 values of 0.0011 and 1.5 µM, respectively</p>

<p>BTM-3528 is a mitochondrial protease OMA1 activator that induces an overactivation of the mitochondrial integrated stress response (ISR).</p>

<p>DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP.</p>

<p>TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1,IC50 = 14 nM). The IC50 value for ASK2 is 0.51 μM.</p>

<p>Deoxynybomycin, a selective anti-tumor agent, inhibits topoisomerase I and induces apoptosis.</p>

<p>MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.</p>

<p>(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells.</p>

<p>NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].</p>

<p>Ferroptocide is a thioredoxin inhibitor that induces iron death in cancer cells and can be used in breast cancer research.</p>

<p>PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4, IC50 value = 84 nM).</p>

<p>BIX selectively induces BiP/GRP78 and ER chaperone, preventing cell death in neurons and retinas.</p>

<p>HDAC-IN-50, a potent FGFR/HDAC inhibitor (IC50: 0.18-13 nM), induces apoptosis, cell cycle arrest, and shows anti-tumor activity.</p>

<p>Mezigdomide (CC-92480) is a potent, novel cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue.Cost-effective and quality-assured.</p>

<p>CR-1-31-B, a synthetic rocaglate, inhibits eIF4A, hinders protein synthesis initiation, and induces apoptosis in cancer cells.</p>

<p>NHWD-870 selectively inhibits BET bromodomains BRD2-4, BRDT; potent anti-cancer effect by inducing apoptosis, halting cell growth.</p>

<p>WYE-125132: potent mTOR inhibitor, IC50 0.19 nM, selective over PI3Ks/hSMG1/ATR.</p>

<p>AR420626: selective FA3R agonist, guards against SALS, effects blocked by BHB, a FA3R antagonist.</p>

<p>RIPK-IN-4 is an effective and selective inhibitor of RIPK2. It also has excellent oral bioavailability (IC50: 3 nM).</p>

<p>AGN 192870 is a potent retinoic acid receptor (RAR) antagonist.AGN 192870 can be used to study cell growth arrest, differentiation and apoptosis.</p>

<p>CNDAC, a nucleoside analog, is a major metabolite of oral drug sapacitabine.</p>

<p>LY303511, a structural analog of LY294002, selectively inhibits mTOR-dependent phosphorylation of S6K, unlike its counterpart, which acts as a phosphatidylinositol 3-kinase (PI3K) inhibitor. It effectively reduces cell proliferation in human lung epithelial adenocarcinoma cells by hindering G2/M phase progression and suppressing casein kinase 2 activity. Additionally, LY303511 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitivity in HeLa cells resistant to TRAIL-induced apoptosis and blocks voltage-gated potassium (Kv) channels.</p>

<p>Pivanex, an oral HDAC inhibitor, targets metastasis, angiogenesis, reduces Bcr-Abl protein, and promotes apoptosis.</p>

<p>eIF4A3-IN-18, a silvestrol analogue with EC50s: 0.8/35/2 nM, inhibits eIF4F complex and is cytotoxic (LC50: 0.06 nM) for cancer research.</p>

<p>Potent EGFR blocker; acts on WT, L858R/T790M (IC50: 1.7 nM), less on T790M/C797S; stalls cell cycle, induces apoptosis, deters metastasis.</p>

<p>Calicheamicin (Calicheamicin γ1) is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.</p>

<p>13h (hGGPPS-IN-3), a strong C2-ThP-BPs hGGPPS blocker, triggers MM cell apoptosis and shows in vivo anti-myeloma effects.</p>

<p>Compound 37b3, an anticancer, halts tumor growth, triggers cell death, and pairs with Trastuzumab to form T-PBA, an ADC with targeted delivery.</p>

<p>Lepadin H, a marine alkaloid and ferroptosis inducer, exhibits significant cytotoxicity by promoting p53 expression, escalating ROS production, and enhancing</p>

<p>c-Met/HDAC-IN-3: dual inhibitor; IC50: c-Met 12.5 nM, HDAC1 26.97 nM; induces apoptosis, G2/M arrest.</p>

<p>Compound A5b, also known as JMJD3/HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone</p>

<p>HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1.</p>

<p>HDAC1/CDK7-IN-1 (compound 8e) serves as a dual inhibitor targeting both CDK7 and HDAC1, with IC50 values of 893 nM and 248 nM , respectively.</p>

<p>Siremadlin R Enantiomer is the R enantiomer of Siremadlin. Siremadlin is a potent and highly specific inhibitor of MDM-2/p53.</p>

<p>WF-210 is an effective activator of procaspase-3 that acts by inducing apoptosis in cancer cells and reducing tumor growth.</p>

<p>Mcl-1 Inhibitor 13 (Example 9), with a Ki of 8.2 nM, serves as an MCL-1 inhibitor suitable for cancer research [1].</p>

<p>Bcl-2-IN-13 is a potent inhibitor of Bcl-2, exhibiting an IC50 of 17 nM, and holds potential for use in cancer research [1].</p>

<p>eIF4A3-IN-9, a silvestrol analogue, disrupts eIF4F complex assembly; EC50s: 29/450/80 nM (myc/tub-LUC, MB-231 cells); for cancer research.</p>

<p>AM-8735 is an inhibitor of MDM2 ( IC50: 25 nM).</p>

<p>Ac-Val-Ala-Asp-CHO (Ac-VAD-CHO) serves as a pan-caspase inhibitor and preserves mitochondrial membrane potential (MMP) while preventing the release of</p>

<p>Anticancer agent 128 (compound 1) is an IAP inhibitor that covalently binds to the BIR3 domains of XIAP, cIAP1, and cIAP2, exhibiting IC50 values of 24.9 nM, 19</p>

<p>4E2RCat is an inhibitor of eIF4E-eIF4G interaction (IC50 = 13.5 μM) and is capable of blocking coronavirus replication as monitored by viral protein expression</p>

<p>Antitumor agent-97 (compound 42), an anticancer agent, effectively inhibits proliferation and autophagy in MGC 803 cells, induces apoptosis, and enhances ROS</p>

<p>Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride), a biosurfactant derived from Brevibacterium casei LS14, enhances the biocompatibility of</p>

<p>INI-43 targets Kpnβ1, disrupting nuclear transport in cervical/esophageal cancers, affecting NFAT, NFκB, AP-1, NF localization.</p>

<p>CUR61414 is a cell-permeable inhibitor of Hedgehog signaling pathway (IC50 =100-200 nM) and selectively binds to smoothened (Ki = 44 nM).</p>

<p>Antiproliferative Against-3 (comp 33) demonstrates significant activity against Hela (IC 50 = 0.21 µM), A549 (IC 50 = 0.39 µM), and MCF-7 (IC 50 = 0.33 µM) cell</p>

<p>Artonin E, a prenylated flavonoid, induces apoptosis and S-phase arrest, disrupting the mitochondrial pathway for cancer research.</p>

<p>Erythro-Austrobailignan-6: orally active, anti-cancer, inhibits DNA topoisomerases, induces apoptosis, boosts p38/JNK phosphorylation.</p>

<p>DLC-50 is a dual inhibitor of PARP-1 and HDAC-1, exhibiting IC50 values of 1.2 nM and 31 nM respectively. It hinders the proliferation of cancer cells such as MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 values of 0.3 μM, 2.7 μM, and 2.41 μM respectively. Additionally, DLC-50 induces apoptosis in MDA-MB-231 cells and causes cell cycle arrest at the G2 phase.</p>

<p>PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting both PI3K and VEGFR2 with IC50 values of 2.21 μM for PI3K and 68 μM for VEGFR2, respectively.</p>

<p>Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures.</p>

<p>D359-0396 is an orally active NLRP3 inflammasome inhibitor that mitigates pyroptosis and reduces IL-1β release in macrophages by inhibiting the oligomerization</p>

<p>RUNX-IN-1, also known as Compound Conjugate 1, covalently attaches to RUNX-binding sequences, thereby preventing RUNX proteins from associating with their</p>

<p>NBI-961, a potent NEK2 inhibitor, suppresses proteasomal degradation and effectively induces G2/mitosis arrest and apoptosis within diffuse large B cell</p>