Apoptose

<p>Vamotinib (PF-114) is a tyrosine kinase inhibitor with antiproliferative and antitumor activity.Vamotinib is used in the study of Alzheimer's disease.</p>

<p>Triciribine phosphate (VD 002) is an AKT inhibitor that inhibits neovascularization and can be used in the study of leukemia.</p>

<p>UC-112 is a novel potent IAP inhibitor and potently inhibits cell growth in two human melanoma and two human prostate cancer cell lines (IC50=0.7-3.4 uM).</p>

<p>CUDC-427 (GDC-0917) is an orally bioactive and pan antagonist of inhibitor of apoptosis proteins(IAPs). CUDC-427 can be used in research on cancers.</p>

<p>SYM 2081: Kainate receptor agonist, IC50 of 35 nM, depolarizes muscle, lowers EPSP amplitude.</p>

<p>HSK3486 is similar to propofol and is a general anesthetic, which may have therapeutic potential in insomnia, migraine, anxiety, analgesia, and other aspects.</p>

<p>Cot inhibitor-1 selectively blocks Tpl2 kinase, reducing TNF-alpha in blood (IC50: 5.7 nM). It may treat arthritis, IBD, and certain cancers.</p>

<p>RIPK3-IN-1 is a RIPK3 inhibitor (IC50: 9.1 nM) that inhibits c-Met kinase, RIPK1, and RIPK2 activity and can be used to study apoptosis.</p>

<p>Imipramine (Dimipressin) is a Fascin1 inhibitor with antitumor activity and induces apoptosis.</p>

<p>Atrosab is a humanized IgG1 antibody targeting TNFR1, inhibiting TNF-mediated apoptosis, and can be used to study inflammatory and neurodegenerative diseases.</p>

<p>Ro 08-2750: A non-peptide NGF inhibitor binding NGF (~1 µM IC50) &amp; selectively inhibits p75NTR over TRKA and MSI RNA-binding (2.7 µM IC50).</p>

<p>FA16 is a selective, metabolically stable ferroptosis inducer with an IC50 value of 1.26 μM.FA16 is a derivative of 2-(trifluoromethyl)benzimidazole.FA16</p>

<p>LQZ-7F is a survivin dimerization inhibitor with anticancer activity.LQZ-7F induces proteasome-dependent survivin degradation and inhibits human tumor growth.</p>

<p>Bomedemstat (IMG-7289) is an LSD1 inhibitor for acute myeloid leukemia, MDS, and Myelofibrosis; induces apoptosis by regulating p53, PUMA, and BCLXL.</p>

<p>R306465 (JNJ-16241199) is an HDAC 1 inhibitor with broad-spectrum anti-tumor activity, inducing apoptosis, and can be used to study solid tumors.</p>

<p>Minodronic acid (YM-529) is a P2X2/3 antagonist with anticancer properties, inhibiting cell growth and metastasis, and used in osteoporosis research.</p>

<p>AMG PERK 44 is a PERK inhibitor that induces autophagy.AMG PERK 44 inhibits GCN2 and B-Raf and can be used in cancer research.</p>

<p>TL4-12 is a MAP4K2 (GCK) inhibitor that inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation in vitro.</p>

<p>eIF4A3-IN-1 is an inhibitor of eukaryotic initiation factor 4A3 (eIF4A3). eIF4A3-IN-1 inhibits cytosolic nonsense-mediated RNA decay at high concentrations.</p>

<p>JY-2 is a forkhead transcription factor O1 (FoxO1) inhibitor with antidiabetic activity that inhibits FoxO1 transcription and can be used to study psoriasis.</p>

<p>LDCA inhibits LDH-A, disrupts mitochondrial function, induces apoptosis in cancer cells, and is non-toxic.</p>

<p>The compound is a selective urokinase inhibitor (IC50 = 8.2 μM). It also inhibits clot lysis with no effect on clot formation.</p>

<p>Alethine is a small antitumor compound used to treat cancers and infections, boosting T-cell cytotoxicity by raising TNFα.</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>ST1074, a dual inhibitor of CerS2 and CerS4, promotes apoptosis and is applicable in cancer research [1].</p>

<p>RUNX-IN-2 (Compound Conjugate 3) covalently attaches to RUNX-binding sequences, preventing RUNX proteins from associating with their targets, thereby inhibiting</p>

<p>JNJ-1013 is a selective IRAK1 PROTAC degrader with an IC50 of 72 nM ,antiproliferative and proapoptotic, increases cleaved-PARP expression.</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>HM90822 is an IAP antagonist that inhibits XIAP and cIAP1/2 protein expression, induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.</p>

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

<p>NHWD-870 selectively inhibits BET bromodomains BRD2-4, BRDT; potent anti-cancer effect by inducing apoptosis, halting cell growth.</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>PIM447 (LGH447) is a pan-PIM kinase inhibitor with anti-tumor and bone protective effects. PIM447 reduces the viability, and motility of HuH6 cell.</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>c-Met-IN-10: potent kinase inhibitor (IC50=16 nM), halts cancer cell activity/movement, induces apoptosis, for anticancer research.</p>

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

<p>Tylvalosin (Acetylisovaleryltylosin) is a broad-spectrum macrolide antibiotic with antibacterial and antiviral properties, effective against PRRSV infection.</p>

<p>CPT-Se4, a seleno-derivative of CPT, effectively kills cancer cells, triggers apoptosis, and is cytotoxic against various cell lines.</p>

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

<p>BAX-IN-1 is a potential selective inhibitor of Bcl-2-associated X protein (BAX).</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>MY-673, a colchicine binding site inhibitor (CBSI), impedes tubulin polymerization and disrupts the ERK signaling pathway, consequently modulating SMAD4 protein</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>NSC 48160 is an anti-pancreatic cancersmall molecule that inhibits growth and enhance apoptosis of pancreatic cancer cells through the mitochondrial pathway.</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>Docebenone is a selective and orally active inhibitor of 5-LO.</p>

<p>BMS-561392 formate, the formate derivative of BMS-561392, functions as a TNF alpha-converting enzyme (TACE) inhibitor and an ADAM17 blocker. It is utilized in the research of inflammatory bowel disease [1] [2].</p>

<p>BMS-561392 (DPC333) is a tumor necrosis factor-α ( TNF-α) Invertase inhibitor.</p>

<p>Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.</p>

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

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

<p>SF5 is an inhibitor of the apoptosis pathway through JNK-p53-caspase apoptotic cascade.</p>

<p>HDAC-IN-60 (compound 21a), a potent histone deacetylase (HDAC) inhibitor, promotes intracellular reactive oxygen species (ROS) production, induces DNA damage,</p>

<p>FOXO1-IN-3 is a highly-selective, orally active inhibitor of FOXO1 that diminishes hepatic glucose production and enhances insulin sensitivity and glucose</p>

<p>CPT-Se3, a camptothecin derivative, boosts anticancer activity, triggers apoptosis in Hep G2, and is cytotoxic to various cells with IC50 of 2.19-4.7 μM.</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>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>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>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>A-1293102 is a potent, selective inhibitor of BCL-XL, effective in inducing apoptosis in tumor cells reliant on BCL-XL [1].</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>Sirt1/2-IN-3 (compound PS9) serves as a dual inhibitor of SIRT1/2, exhibiting IC50 values of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respectively.</p>

<p>Ac-YVAD-pNA, a specific substrate for Caspase-1, serves to detect Caspase-1 activity, a crucial mediator of inflammatory processes [1] [2].</p>

<p>FGFR-IN-8, potent oral FGFR inhibitor for wild-type/mutant types, induces apoptosis with anti-cancer properties.</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>SM-1295: IAP antagonist, Kd 3077 nM XIAP-BIR3, 3.2 nM c-IAP1-BIR3, 9.5 nM c-IAP2-BIR3.</p>

<p>RIP2 kinase inhibitor 2 is a receptor-interacting protein-2 kinase inhibitor.</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>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>(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>WF-210 is an effective activator of procaspase-3 that acts by inducing apoptosis in cancer cells and reducing tumor growth.</p>

<p>MTI-31 (LXI-15029) is a potent oral mTORC1/2 inhibitor with a Kd of 0.20 nM, &gt;5,000-fold selectivity, and an IC50 of 39 nM.</p>

<p>RIPK1-IN-8 is an aminoimidazolopyridine and is a selective and potent inhibitor of RIPK1 (IC50: 4 nM).RIPK1-IN-8 has research potential in inflammatory diseases</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>eIF4A3-IN-17, a silvestrol analogue, disrupts eIF4F assembly; EC50: 0.9-15 nM. Used in cancer pathogenesis research.</p>

<p>Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on</p>

<p>YS-363 is a potent, selective, and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting half-maximal inhibitory concentrations (</p>

<p>TMX-2164: strong, irreversible BCL6 inhibitor, IC50=152 nM, long-lasting action, inhibits cell proliferation.</p>

<p>Necrocide 1 is a inducer of cancer cell necrosis that is not inhibited by caspase, BCL2 , or TNFα, and acts through the mitochondrial regulatory pathway.</p>

<p>MP7 (PDK1 inhibitor) is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).</p>

<p>Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).</p>

<p>KRIBB3: novel anticancer microtubule inhibitor; halts MDA-MB-231 cell migration/invasion by targeting Hsp27 phosphorylation.</p>

<p>1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) acts as a cyclin-dependent kinase (CDK) inhibitor, promoting apoptosis and restricting the proliferation of various cancer cell lines [1].</p>

<p>ICL-CCIC-0019 inhibits ChoKα, causes G1 arrest, ER stress, and cancer cell apoptosis.</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>LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.</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>Ponicidin, a diterpenoid from Rabdosia rubescens, has immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer properties.</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>Nalmefene (ORF 11676) is a μ-opioid antagonist and partial κ agonist used to study opioid overdose and alcohol dependence.</p>

<p>RET-IN-17 inhibits RET kinase; may help in IBS pain and RET-activated cancers.</p>

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

<p>Bcl-2-IN-11 (compound 6) is a potent and selective inhibitor of Bcl-2 activity, exhibiting an IC50 of 0.9 nM, and demonstrates minimal inhibition against Bcl-xl</p>

<p>Z-YVAD-CMK is an inhibitor of both caspase-1 and caspase-3, as referenced in [1].</p>

<p>Vatalanib hydrochloride (PTK787 hydrochloride) is a VEGF inhibitor that reduces the number and area of Aβ plaques in the cortex of 5xFAD mice.</p>

<p>GDC-2394: Oral, selective NLRP3 inhibitor; blocks IL-1β (human 0.4μM, mouse 0.1μM), spares NLRC4.</p>

<p>WNY1613: Potent PI3Kδ inhibitor with anti-NHL properties, induces apoptosis in cells, affects phosphorylation in vitro/in vivo.</p>

<p>Potent γ-secretase inhibitor; IC50: 1.2 nM (cell), 6.2 nM (cell-free); lowers Aβ in mice/guinea pigs' brain, CSF, plasma.</p>

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

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