Apoptose

<p>Pim-1 kinase inhibitor 4 is a potent Pim-1 kinase inhibitor with an IC50 value of 17.01 nM.Pim-1 kinase inhibitor 4 also possesses antioxidant activity and</p>

<p>(D)-PPA 1 TFA is a hydrolysis-resistant D-peptide antagonist and a potent PD-1/PD-L1 inhibitor, exhibiting an affinity for PD-1 of 0.51 μM and demonstrating</p>

<p>Theophyllol (theophylline sodium acetate) can alter calcium levels in subcellular fractions of rat brain cortex.</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>LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.</p>

<p>c-Met/HDAC-IN-4, a dual inhibitor of c-Met/HDAC, exhibits an IC 50 value of 28.92 nM for c-Met. This compound effectively induces G 0 /G 1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells. Additionally, c-Met/HDAC-IN-4 suppresses both the proliferation and invasion of breast cancer cell lines.</p>

<p>Human membrane-bound PD-L1 polypeptide serves as an antigen for inducing the production of PD-L1 antibodies [1].</p>

<p>Met-12 is a peptide inhibitor of the Fas receptor. It suppresses Fas receptor-mediated apoptosis in photoreceptor cells and reduces Caspase activation, making it a potential candidate for research on photoreceptor protectants.</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>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>JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.</p>

<p>N-Acetylpsychosine, also known as α-galactosylated C2-ceramide (d18:1/2:0), exhibits immunostimulatory properties.</p>

<p>Verdinexor (KPT-335) (KPT-335), a specific XPO1/CRM1 inhibitor, are orally bioavailable.</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>Lambertianic acid is a bioactive chemical that has anti-allergic and antibacterial effects.</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>Silicon naphthalocyanine dichloride is a photosensitizer with potential anti-tumor activity. This compound is employed in photodynamic therapy to inhibit cancer by effectively absorbing specific wavelengths of light, thereby generating oxygen radicals that aid in the destruction of cancer cells. The biocompatibility of Silicon naphthalocyanine dichloride demonstrates promising prospects for medical applications.</p>

<p>FB49 is a selective Bcl-2-associated athanogene 3 (BAG3) inhibitor with a Ki of 45 μM.</p>

<p>MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). This compound effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest, and increases cellular apoptosis (Apoptosis). Additionally, MS41 reduces chromatin occupancy related to ENL-mediated transcription elongation mechanisms and suppresses the expression of oncogenes and the progression of leukemia.</p>

<p>Sodium propionate (Propionic acid sodium salt) has potential anti-inflammatory and anti-apoptotic activities, inhibiting certain signaling pathways.</p>

<p>Fludioxonil (CGA 173506), a phenylpyrrole fungicide, inhibits the growth of B. cinerea from strawberry and blackberry crops.</p>

Apoptosis Inducer 29 (compound Y9) demonstrates anticancer efficacy in non-small cell lung cancer by inducing lysosomal dysfunction and apoptosis, and exhibits superior performance to Gboixn both in vitro and in vivo.

<p>ZMF-24 is an anti-triple-negative breast cancer (TNBC) agent that exhibits IC50 values of 0.22 μM and 0.44 μM against BT-549 and MDA-MB-231 TNBC cell proliferation, respectively. It targets the eukaryotic translation initiation factor 3 subunit D (EIF3D), disrupting TNBC's energy supply by inhibiting glycolysis. Additionally, ZMF-24 induces TNBC cell apoptosis (apoptosis) by stimulating sustained endoplasmic reticulum stress.</p>

<p>UBX1325, a potent Bcl-xL inhibitor, induces cell death in aging cells, useful for age-related eye disease research.</p>

<p>Thalidomide-O-PEG4-NHS ester is a polyethylene glycol (PEG)-based linker, commonly employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].</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>Cuprichydroxide exhibits inhibitory activity against Ralstonia solanacearum and A549 cells and has acute pulmonary toxicity.</p>

<p>2-Chloronaphthalene is an organochlorine chemical compound and is a chlorinated derivative of naphthalene. The compound is an isomer for 1-chloronaphthalene.</p>

<p>PRMT5-IN-45 (compound 36) is a potent and selective inhibitor of PRMT5, exhibiting an IC50 value of 3 nM. This compound effectively reduces the levels of symmetrical dimethylarginine (sDMA) and inhibits the proliferation of the MOLM-13 cell line by inducing apoptosis and causing cell cycle arrest.</p>

<p>Isorhamnetin 3-glucuronide is a useful organic compound for research related to life sciences and the catalog number is T124938.</p>

<p>ARD-61: potent PROTAC, degrades AR/PR in AR+ cancers, triggers apoptosis, inhibits tumor growth in mice.</p>

<p>Ferroptosis-IN-12 (Cpd-A1) is an inhibitor of ferroptosis. It effectively suppresses ferroptosis in mouse renal tubular epithelial cells (mTECs) treated with Erastin and improves renal function in dose-dependent manners in mouse models of acute kidney injury (AKI) induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). This compound also reduces renal tubular damage and eliminates inflammation. Exhibiting good plasma stability and high distribution in renal tissues during pharmacokinetic studies in mice, Ferroptosis-IN-12 shows promising potential for research in the field of AKI.</p>

<p>PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080</p>

<p>Tebentafusp (IMCgp100) is a protein that targets gp100 with potential anti-tumor activity.</p>

<p>VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.</p>

<p>BDK-IN-1 (compound (-)-43) is a BDK inhibitor with an IC50 of 0.23 μM and a maximum inhibition rate of 90%. It reduces phosphorylated-E1 levels and is useful in the study of cardiac metabolic diseases.</p>

<p>STAT3-D11-PROTAC-VHL (Compound D11-PROTAC) is a PROTAC degrader targeting signal transducer and activator of transcription 3 (STAT3). It demonstrates anti-tumor activity with IC50 values of 1335 nM in HeLa cells and 1973 nM in MCF-7 cells. The compound binds to the DNA binding domain of STAT3, recruits the E3 ligase VHL to form a ternary complex, leading to ubiquitination and subsequent proteasomal degradation of STAT3. Additionally, STAT3-D11-PROTAC-VHL inhibits tumor cell growth, induces cell cycle arrest and apoptosis (apoptosis), and suppresses tumor immune evasion.</p>

<p>PROTAC EGFR degrader 6 effectively degrades EGFR Del19 in HCC827 cells (DC50=45.2 nM) and induces apoptosis and G1 arrest.</p>

<p>HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/</p>

<p>2,2-Dimethyl-2,3-dihydrobenzofuran-7-ol inhibits the proliferation of the THP-1 cell line and anti-infective Leishmania and Toxoplasma gondii RH.</p>

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

<p>Phosphocreatine dipotassium, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives.</p>

<p>Aspochalasin D, isolated from A. microcysticus, shows antibacterial properties and cytotoxicity affecting Ba/F3-V12 cells, with IC50s of 0.49 and 1.9 μg/ml.</p>

<p>Vonlerolizumab (MOXR 0916) is a humanized IgG OX40 agonist monoclonal antibody with potential in cancer and immune disease research.</p>

<p>Antiproliferative agent-59 (Compound 14u) acts as an inhibitor of tubulin polymerization. Demonstrating anticancer activity in Huh7, SGC-7901, and MCF-7 cell lines, this compound achieves IC50 values of 0.03, 0.18, and 0.13 μM, respectively. Additionally, it arrests the cell cycle at the G2/M phase and induces apoptosis in Huh7 cells. In a xenograft mouse model utilizing Huh7 cells, Antiproliferative agent-59 exhibits antitumor effects against hepatocellular carcinoma without significant toxicity.</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>(E/Z)-LAQ824 is an inhibitor of histone deacetylase.</p>

<p>MitoTam bromide hydrobromide is an electron transport chain (ETC) inhibitor.</p>

<p>Antitumor photosensitizer-7 (compound 15), a photosensitizer possessing anti-cancer properties, demonstrates substantial cytotoxic effects on the G361 melanoma cell line when exposed to 414 nm blue light irradiation.</p>

<p>1,2,3,4-Tetrahydronaphthalen-2-ol exhibits weak inhibitory activity against Bcl-xL and is widely used in biochemical experiments and drug synthesis research.</p>

<p>Trimebutine (Mebutin) is a spasmolytic agent that regulates intestinal and colonic motility and relieves abdominal pain with antimuscarinic and weak mu-opioid</p>

<p>ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP.</p>

<p>Amorfrutin A is a useful organic compound for research related to life sciences. The catalog number is T124190 and the CAS number is 80489-90-3.</p>

<p>Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC that links Pomalidomide and Dovitinib via a CRBN connector, exhibiting potent antiproliferative activity in</p>

<p>C-Met/Axl-IN-1 (Compound 22a) is an oral, selective type II c-Met/Axl inhibitor with IC50 values of 1 nM and 10 nM, respectively. It effectively suppresses tumor cell proliferation, induces cell cycle arrest, and apoptosis (apoptosis), showcasing potent anti-tumor activity.</p>

<p>Solanidine is a cholestane alkaloid isolated from potato species with antitumor effects. Solanidine inhibits proliferation.</p>

<p>Fuscin, a quinonoid from O. fuscum, inhibits ADP/ATP translocase, depletes glutathione, disrupts NADH oxidation, and blocks MIP-1α/CCR5 binding (IC50: 21µM).</p>

<p>CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP/TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).</p>

<p>Bcl-2-IN-22 (compound 1), a gold (I) NHC complex, exhibits anticancer activity. It induces cell death (apoptosis) via the mitochondrial pathway with an IC50 value of 0.014 μM. Additionally, Bcl-2-IN-22 targets members of the BCL-2 family, promoting apoptosis and sensitization in multidrug-resistant leukemia cells overexpressing BCL-2.</p>

<p>Polyphyllin G (Polyphyllin VII), the the main member of polyphyllin family, shows strong anticancer activity against several carcinomas.</p>

<p>PLD-IN-1 (Compound 3r) is an orally effective inhibitor of phospholipase D (phospholipaseD) with an IC50 of 1.97 μM. It reduces the expression of CD24, CD47, and PD-L1 while enhancing the expression of calreticulin, thereby modulating the immune evasion mechanisms of lung cancer cells by promoting the phagocytosis of cancer cells by macrophages. PLD-IN-1 inhibits the viability of lung cancer cell lines A549, HCC44, H460, and HCC15 with IC50 values of 18.44, 22.31, 24.85, and 21.45 μM, respectively. It induces apoptosis (apoptosis) in A549 cells and inhibits cell migration. Additionally, PLD-IN-1 increases pro-inflammatory M1 macrophage levels and decreases anti-inflammatory M2 macrophage levels, exhibiting anti-tumor activity in mouse models.</p>

<p>Oxidosqualene cyclase inhibitor</p>

<p>CDK-IN-14 (B34) is a CDK2 inhibitor (IC50=0.097 μM) that exhibits anti-hepatocellular carcinoma activity. It inhibits the cell cycle in HepG-2 cancer cells and induces apoptosis (apoptosis) through a caspase-mediated mechanism.</p>

<p>MBC-11 trisodium, a bisphosphonate-Ara-C conjugate, may treat TIBD.</p>

<p>Lipustobart is an IgG4-kappa humanized monoclonal antibody targeting PDCD1 (programmed cell death 1, PD1, PD-1, CD279), with immunostimulant and antineoplastic</p>

<p>DB818 dihydrochloride is the dihydrochloride salt form of DB818. It acts as an inhibitor of Homeobox A9 (HOXA9). By reducing the formation of the HOXA9-DNA complex, DB818 dihydrochloride inhibits the growth of AML cell lines OCI/AML3, MV4-11, and THP-1 and induces cell apoptosis (apoptosis).</p>

<p>FW-1 is a type I inhibitor of FLT3, with an IC50 of approximately 1 μM. It exhibits cytotoxic effects in FLT3-mutant AML cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis in MV4-11 and MOLM-13 cells.</p>

<p>eIF4E-IN-3: potent eIF4e inhibitor with promise for cancer study.</p>

<p>SIN-1 chloride is a moxidomine metabolite with vasodilatory, anti-platelet, and antianginal effects, reducing myocardial ischemia-related damage.</p>

<p>15-acetoxyscirpenol: ASM that induces apoptosis, inhibits Jurkat T cell growth dose-dependently, and activates caspases other than caspase-3.</p>

<p>Functionalized cereblon ligand with E3 ligase and alkylC5 linker for PROTAC R&amp;D; ready for protein conjugation. Formerly Pomalidomide-linker 4.</p>

<p>Maceneolignan A, a natural product isolated from the aril of Myristica fragrans (Myristicaceae), inhibits β-hexosaminidase release in RBL-2H3 cells, exhibiting</p>

<p>Hypoxia inducer-1 (Compound N6) is a NO donor compound that is orally active and activated under hypoxic conditions. It exhibits high selectivity in releasing NO, inhibiting apoptosis, necrosis, and elevated levels of reactive oxygen species (ROS) associated with hypoxia. It modulates vasodilation and shows protective effects in a mouse model of myocardial hypoxic injury, making it useful for coronary heart disease research.</p>

<p>HDAC6-IN-16 (compound 5c), a quinazolin-4(3H)-one-based inhibitor of histone deacetylase 6 (HDAC6), demonstrates an anticancer effect by inhibiting colony</p>

<p>Asaretoclax is an effective inhibitor of B-cell lymphoma 2 (Bcl-2), demonstrating potential for use in cancer research.</p>

<p>Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].</p>

<p>Ac-Pro-Gly-Pro-OH can be used as a CXCR2 agonist with bactericidal and anti-inflammatory activity for the study of sepsis and lung inflammation.</p>

<p>Prolgolimab (BCD-100) is an anti-PD-1 antibody used in melanoma research.</p>

<p>Nofazinlimab (CS1003) is a human anti-PD-1 IgG4 monoclonal antibody for the study of unresectable hepatocellular carcinoma (uHCC).</p>

<p>Scr-IN-1 (Compound 4e) is a tyrosine kinase inhibitor demonstrating inhibitory activity against HCT-116 and MIA-PaCa-2 cells, with IC50 values of 0.16 μM and 1.16 μM, respectively. It shows selectivity towards HCT-116 cells and MIA-PaCa-2 cells, with a selectivity index (SI) greater than 625 and 86. Scr-IN-1 induces apoptosis in HCT-116 colon cancer cells without altering the proportion of necrotic cells and is a potential novel SRC kinase inhibitor for HCT-116 cells. This compound is suitable for cancer research.</p>

<p>Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.</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>Lw13 is a PROTAC targeting Hsp90, exhibiting maximal degradation efficacy at a concentration of 0.05 μM in Siha cells. Lw13 induces apoptosis and demonstrates potent antitumor activity both in vitro and in vivo.</p>

<p>Danburstotug (IMC-001), an immunostimulant and antineoplastic [1], is a humanized IgG1-lambda monoclonal antibody targeting CD274 (PDL1, B7 homologue 1, B7H1).</p>

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

<p>Targaprimir-96 is a potent microRNA-96 (miR-96) processing inhibitor.</p>

<p>Thalidomide-NH-amido-C6-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, designed for the synthesis of PROTAC.</p>

<p>hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 nM for hCA IX and 8.5 nM for hCA XII. It not only inhibits hCA activity but also releases NO, exerting dual anti-tumor effects. By reducing the expression of hCA IX and iron regulatory proteins, hCAIX-IN-23 regulates mitochondrial caspase activity and the ferroptosis pathway, thereby inducing apoptosis. This compound is utilized in research focused on renal cancer.</p>

<p>iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.</p>

<p>NCA029 is a potent activator of human caseinolytic protease P (HsClpP) with an EC50 of 0.15 μM. It targets HsClpPP and triggers an ATF3-dependent integrated stress response, resulting in the death of colon cancer cells.</p>

<p>CYP51/PD-L1-IN-2 (compound L20), a quinazoline with antifungal properties, is a potent dual inhibitor targeting both CYP51 (IC50: 0.263 μM) and PD-L1 (IC50: 0.</p>

<p>Isomahanine is a useful organic compound for research related to life sciences and the catalog number is T125848.</p>

<p>Anticanceragent 178 (compound C2) is a potent anticancer compound. It effectively inhibits the proliferation and metabolic activity of MDA-MB 231 cells, with IC50 values of 1.1 and 4.2 μM, respectively. Additionally, Anticanceragent 178 induces ferroptosis and necroptosis in cells.</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>Rozanolixizumab (RYSTIGGO) is a humanized IgG4 monoclonal antibody that targets FcRn in newborns for autoimmune research.</p>

<p>Antitumor agent-170 (Compound C6) inhibits PD-1/PD-L1 interaction and PARP7 with IC50 values of 0.342 μM and 7.05 nM, respectively. It shows high affinity for human PD-L1, with a Ki of 9.31 nM, and can restore T cell function while increasing IFN-γ secretion. In mouse models, Antitumor agent-170 exhibits antitumor effects against melanoma and demonstrates favorable pharmacokinetic properties.</p>

<p>(R)-HTS-3 is a LPCAT3 inhibitor that remodels the polyunsaturated phospholipid content of human cells and prevents iron death.</p>

<p>EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. It exhibits antiproliferative activity, effectively inhibiting the proliferation of H1975 cells and inducing apoptosis (apoptosis). EGFR-IN-107 is applicable in cancer research.</p>