Apoptose

<p>P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.</p>

<p>Moracin N, a ferroptosis inhibitor derived from mulberry leaves, exhibits neuroprotective activity by mitigating oxidative stress [1].</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>SM-164 Hydrochloride: cell-permeable, binds to XIAP (BIR2/3 domains), IC50 of 1.39 nM, potent XIAP antagonist.</p>

<p>Pantinin-1 is an antimicrobial peptide found in the venom of the emperor scorpion (Pandinus imperator). This compound exhibits strong antibacterial activity against Gram-positive bacteria and fungi, but has weaker effects on Gram-negative bacteria. Additionally, Pantinin-1 demonstrates very low hemolytic activity on human red blood cells and possesses anticancer properties, specifically inducing apoptosis in tumor cells.</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>Ac-FEID-CMK: Potent inhibitor for zebrafish GSDMEb, reduces pyroptosis, and lessens septic AKI.</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>Narasin inhibits dengue virus, treats coccidiosis without harm to cells, and induces cancer cell apoptosis.</p>

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

<p>Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .</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>YW-N-7 (TFA) is a PROTAC designed to target, inhibit, and degrade RET kinase, demonstrating a DC50 of 88 nM. It exhibits antitumor activity in xenograft mouse models driven by KIF5B-RET, making it a valuable compound for cancer research.</p>

<p>MPP hydrochloride is a selective estrogen receptor (ERR) modulator.</p>

<p>Reproxalap (NS-2) is a dry eye treatment that neutralizes aldehydes like malondialdehyde.</p>

<p>Prodigiosin hydrochloride is a bioactive red pigment from bacteria with antibacterial, antifungal, anticancer properties, and inhibits Wnt/β-catenin.</p>

<p>JC2-11 is an anti-inflammatory agent blocking NLRC 4, AIM 2, ROS production, caspase-1 activity, and reducing GSDMD, IL-1β, and LDH in vesicles.</p>

<p>ACBI3 is a pan-KRAS degrader with anticancer activity, degrading oncogenic KRAS.</p>

<p>[Au(L4)(CyJohnPhos)]SbF6 is a gold-containing compound that exhibits inhibitory effects on cyclooxygenase-1/2 (COX-1/2), suppresses the proliferation of colon cancer cells Caco2-/TC7 with an IC50 of 0.98 μM, and induces cell apoptosis (apoptosis). Additionally, [Au(L4)(CyJohnPhos)]SbF6 acts as an inhibitor of thioredoxin reductase (TrxR) and demonstrates antioxidative activity by modulating ROS levels.</p>

<p>ECDD-S18 (compound ECDD-S18) induces apoptosis in a dose-dependent manner, effectively targeting the vacuolar ATPase (V-ATPase) and impairing lysosomal acidification.</p>

<p>GGTI298 trifluoroacetate (GGTI298TFA salt) is a geranylgeranyltransferase I inhibitor that causes cell cycle arrest and induces apoptosis.</p>

<p>FOXO4-DRI: a peptide blocking FOXO4/p53 interaction; induces senescent cells' apoptosis.</p>

<p>Thalidomide-O-amido-C6-NH2 is a synthetic E3 ligase used for PROTAC creation, containing cereblon ligand and linker.</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>DPP-4-IN-8 (compound 27) is a potent and selective inhibitor of dipeptidyl peptidase 4 (DPP4), with an inhibition constant (Ki) of 0.96 μM.</p>

<p>PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.</p>

<p>Solasodine hydrochloride (90 μM; 2 days) treatment induced significant budding in P19 cells. This compound strongly stimulated the expression of various neuronal markers, including βIII-tubulin, synaptophysin, MAP2, ChAT, and the neural progenitor marker doublecortin. Predominantly, Solasodine hydrochloride directed the differentiation of P19 cells towards neuronal pathways.</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>RSM3 TFA is a stapled peptide and an inhibitor of METTL3-METTL14, exhibiting a dissociation constant (Kd) of 3.10 μM. It inhibits tumor growth and induces cell apoptosis. RSM3 TFA is utilized in cancer research.</p>

<p>Atibuclimab is a chimeric monoclonal antibody targeting CD14, consisting of a mouse variable region and a human IgG4 Fc region.</p>

<p>KRAS inhibitor-40 (Compound 41) is an inhibitor of KRAS, disrupting the KRAS G12C-BRAF complex and suppressing the phosphorylation of the downstream ERK signaling pathway. This compound also inhibits the proliferation of tumor cells with various KRAS mutations, exhibiting antitumor activity.</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>CDK9-IN-24 (compound 21a) is a potent and selective inhibitor of CDK9 that exhibits a pronounced inhibitory impact on tumor proliferation.</p>

<p>Anticanceragent 272 (Compound 2) is an anticancer agent demonstrating significant activity against bladder cancer cells (T-24) with an IC50 of 2.81 μM. It depletes glutathione (GSH) through a Fenton-like reaction, generating reactive oxygen species (ROS) and hydroxyl radicals (•OH), thereby inducing apoptosis and ferroptosis. Anticanceragent 272 enhances chemodynamic therapy (CDT) and promotes tumor cell death through mitochondrial dysfunction and autophagy. It holds potential for further research in bladder cancer.</p>

<p>HSP90-IN-18 inhibits Hsp90 with 0.39 μM IC50, useful for viral, neurodegenerative, and inflammatory research.</p>

<p>GA-Mk is a triterpenoid from Ganoderma lucidum mycelia, inhibits HeLa cell growth, and induces apoptosis via mitochondria; used in cervical cancer studies.</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>D-CopA3 is an inhibitor of MDM2 and an activator of the p53 signaling pathway. It exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO with IC50 values of 15-18 μM and induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of the cell cycle inhibitor protein p21Cip1/Waf1, enhances mucosal barrier function, and reduces infiltration of inflammatory mediators. It shows anti-inflammatory properties in mouse models of acute enteritis induced by C. difficile toxin A and chronic colitis induced by DSS. Additionally, D-CopA3 demonstrates antitumor activity in a mouse HCT-116 xenograft model.</p>

<p>cis,trans-Germacrone is an antitumor, antioxidant isomer that inhibits lung cancer and affects Akt/MDM2/p53.</p>

<p>PARP1-IN-17 is an inhibitor that targets PARP-1 (IC50=19.24 nM ) with a slightly reduced affinity for PARP-2 (IC50=32.58 nM ) and induces apoptosis.</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>Cereblon ligand for PROTAC R&amp;D; has E3 ligase, alkylC1-PEG3-alkylC3 linker, terminal amine. Part of Arvinas-licensed tool molecules.</p>

<p>Ac-LEVD-CHO, a caspase-4 inhibitor, is a peptide with the sequence Ac-Leu-Glu-Val-Asp-al [1].</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>Anticanceragent 273 (Compound 9q) is an effective anticancer compound identified from matrine. It inhibits cancer cell proliferation, with an IC50 of 4.48 μM against HeLa cells. Anticanceragent 273 exerts its anticancer effects by modulating PI3K/AKT expression and activating activating transcription factor 4 (ATF4), which induces endoplasmic reticulum stress and triggers apoptosis. It holds potential for cancer research, including cervical cancer.</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>RPS6-IN-1 (Compound 22o) inhibits cell migration and induces apoptosis (increasing the expression of Bax, p53, cleaved-caspase 3, and cleaved-PARP). It reduces mitochondrial membrane potential and activates autophagy (Autophagy) through the PI3K-Akt-mTOR signaling pathway, damaging mitochondria and lysosomes within the cell and causing endoplasmic reticulum stress. RPS6-IN-1 also inhibits the phosphorylation of RPS6. Notably, RPS6-IN-1 is a low systemic toxicity anticancer agent.</p>

<p>eIF4E-IN-2 effectively inhibits eIF4e, crucial for research on diseases like cancer.</p>

<p>RIP2 Kinase Inhibitor 4, a selective RIPK2 PROTAC, degrades RIPK2 (pIC50=8), inhibits TNF-α release.</p>