Apoptosis

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

<p>FeTPPS, a decomposition catalyst for 5,10,15,20-tetrakis(4-sulfonatophenyl) porphyrin iron(III) chloride peroxynitrite, neuroprotective.</p>

<p>9,11-Dehydroergosterol peroxide is a useful organic compound for research related to life sciences.</p>

<p>RIPK2-IN-2, a RIP2 kinase PROTAC inhibitor, blocks proinflammatory signaling in autoinflammatory diseases.</p>

<p>CAY10726, an arylurea fatty acid, cuts ATP by 28% and promotes apoptosis in breast cancer cells by depleting mitochondrial lipids.</p>

<p>Taxamairin B is a potent anti-inflammatory compound that inhibits the expression of proinflammatory cytokines (TNF-α, IL-1β, and IL-6) and reduces the</p>

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

<p>DB2115 (tertahydrochloride) inhibits PU.1, key in leukemia; potential for cancer research.</p>

<p>RMC-6291: Oral, covalent KRAS G12C inhibitor, blocks signaling, forms tri-complex with CypA, suppresses RAS activity in tumors.</p>

<p>GDCNF-11, an HSP90-based HIM-PROTACGPX4 degrader, facilitates the ubiquitination and degradation of GPX4 through the HSP90 chaperone complex. This reduction in endogenous GPX4 induces ferroptosis in HT-1080 cells, with a DC50 value of 0.08 μM.</p>

<p>Photosensitizer-3, generates single-linear oxygen upon near-infrared light excitation in combination with FAP,potent and selective killing cancer cells.</p>

<p>p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.</p>

<p>Bfl-1-IN-6 (Compound 20) is an orally active inhibitor of Bcl-2-related protein A1 (BFL1) with an IC50 of 19 nM. This compound can stabilize BFL1 protein, activate cleaved caspase 3, and demonstrates antitumor activity in mouse models.</p>

<p>Ferroptosis-IN-16 (Compound 13l) acts as a specific inhibitor of ferroptosis, demonstrating EC50 values of 0.7 nM in ES-2 cells and 0.9 nM in LX-2 cells. It effectively alleviates acute liver injury induced by Acetaminophen in mouse models and shows excellent metabolic stability in mouse liver microsomes.</p>

<p>SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.</p>

<p>Betamethasone (NSC-39470), a glucocorticoid steroid, has immunosuppressive and anti-inflammatory properties.</p>

<p>D-Trimannuronic acid from seaweed induces TNF-α in mouse macrophages; useful in pain, dementia studies.</p>

<p>XZ338 is a highly selective degrader targeting BCL-XL without degrading BCL-2. It exhibits an IC50 value of 3.7 nM against MOLT-4 cells and possesses antiproliferative properties, making it useful for cancer research.</p>

<p>intestinal epithelium-specific growth factor</p>

<p>RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.</p>

<p>AChE-IN-81 (compound 22) is a reversible, selective inhibitor of AChE with an 80.0% inhibition rate and an IC50 of 3.7 μM. It binds to AChE with an affinity (Kd) of 5.37 μM. AChE-IN-81 effectively reduces apoptosis in zebrafish brain cells and shows potential neuroprotective activity in an H2O2-induced SH-SY5Y cell damage model.</p>

<p>Tubulin polymerization-IN-72 (Compound 4a4) is a microtubule synthesis inhibitor with anticancer properties. By binding to the colchicine site, it disrupts the polymerization of tubulin, resulting in the arrest of cancer cells at the G2/M phase and inducing apoptosis (Apoptosis). The IC50 for its activity against cancer cells is 0.4-2.7 nM.</p>

<p>dMCL1-2 is a PROTAC-based MCL1 degrader, binding at 30 nM, and induces apoptosis in leukemia.</p>

Photosensitizer-5, a photodynamic agent, exhibits cytotoxicity towards HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. It induces cell death through lipid peroxidation via an iron-independent ferroptosis pathway. Additionally, Photosensitizer-5 displays antitumor activity in HeLa-tumor-bearing mice.

<p>HJC0416 hydrochloride: potent oral STAT3 inhibitor, better anticancer effects than Stattic, promising for breast cancer research.</p>

<p>Estradiol cypionate (Depofemin), the 17 β-cyclopentylpropinate ester of estradiol, inhibits ET-1 synthesis via estrogen receptor.</p>

<p>Lacto-N-fucopentaose I is a milk oligosaccharide.</p>

cytoplasmic peptide of the neurotrophin receptor p75NTR

<p>Anti-inflammatory agent 95 (Compound 2e) is a compound with potent anti-inflammatory properties, showing significant inhibition of NO production in LPS-induced RAW 264.7 mouse macrophages, with an IC50 of 8.8 μM. It also effectively suppresses the secretion of TNF-α and IL-1β, achieving inhibition rates of 60% and greater than 90% at 100 μM, respectively. Anti-inflammatory agent 95 holds promise for research into inflammatory diseases.</p>

<p>GSK-3β inhibitor 15 (Compound 54), with an IC50 of 3.4 nM, effectively suppresses Aβ 1-42-induced phosphorylation of GSK-3β and tau protein, as well as LPS-</p>

<p>12-Deoxyphorbol 13-palmitate, a monomer derived from the roots of Euphorbia fischeriana, exhibits notable antitumor activity. This compound induces cell cycle arrest and apoptosis in gastric cancer cells by modulating key cell cycle regulators, such as cyclin B, cyclin A, and CDC2. Additionally, 12-Deoxyphorbol 13-palmitate significantly diminishes liver fibrosis by targeting APOL2 and impairing the APOL2–SERCA2–PERK–HES1 signaling pathway.</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>Curzerene, a sesquiterpene compound derived from the rhizome of Curculigo orchioides Gaertn, possesses potent anti-cancer properties.</p>

<p>Compound 7, also known as RAR/RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2/M arrest and apoptosis in cancer cells.</p>

<p>3-methoxy-9H-carbazole: photosensitizer, anti-breast cancer, from Klauseneria spp., induces apoptosis.</p>

<p>CYP51/PD-L1-IN-1 (compound L11), a quinazoline with antifungal properties, simultaneously inhibits CYP51 (IC50: 0.884 μM) and PD-L1 (IC50: 0.083 μM).</p>

<p>ILS-920, a Rapamycin analog, has reduced immunosuppression, enhanced neuroprotection, and preferentially binds FKBP52 and L-type VGCC β1.</p>

<p>Anti-MousePD-1(LALA-PG) Antibody (RMP1-14) is an IgG2a, κ antibody inhibitor derived from mice that targets and inhibits mouse PD-1.</p>

<p>FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.</p>

Antiangiogenic agent 6 (Pt-1) effectively inhibits angiogenesis and induces necroptosis in tumor cells.

<p>hMAO-B-IN-11 (Compound 12) is a selective and reversible inhibitor of human monoamine oxidase B (hMAO-B) with an IC50 value of 0.11 µM. It operates by competitively binding to the active site of hMAO-B, thereby preventing the oxidative deamination of monoamines and reducing hydrogen peroxide production. Additionally, hMAO-B-IN-11 inhibits pro-inflammatory mediators (NO, TNF-α, IL-1β) in activated microglia. This compound holds potential for research in neurodegenerative diseases such as Parkinson's and Alzheimer's.</p>

<p>[1,1'-Biphenyl]-3-amine is an inhibitor of MAO-A and MAO-B and can inhibit the cell viability of HT-29, HEK 293, and MCF-7 cells.</p>

<p>Monensin, from Streptomyces cinnamonensis, inhibits Wnt/β-catenin. Potential anticancer agent.</p>

<p>Nemorosone, a PPAP from C. rosea, inhibits neuroblastoma and pancreatic cancer cell growth, induces apoptosis, and reduces mouse xenograft tumors.</p>

<p>A-1155905 is an MCL-1 inhibitor with anticancer activity, demonstrating a half maximal inhibitory concentration (IC50) of 33.5 Nm and a dissociation constant (Ki) of 0.58 nM. This compound selectively binds to MCL-1 and possesses sufficient affinity to disrupt the MCL-1-Bim complex in live cells. The induction of death in MCL-1-dependent cell lines by A-1155905 is reliant on caspase proteins and occurs through apoptosis.</p>

NL13, a Polo-like kinase 4 (PLK4) inhibitor, exhibits an IC 50 value of 2.32 μM. It demonstrates the ability to suppress the viability of PC3 and DU145 prostate cancer cells with respective IC 50 values of 3.51 μM and 2.53 μM. NL13 also inhibits tumor growth in prostate cancer mice. Additionally, it deactivates the AKT signaling pathway by reducing CCNB1/CDK1 levels, leading to G2/M cell cycle arrest and initiating apoptosis through caspase-9/caspase-3 cleavage.

<p>PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and markedly diminishes mitochondrial membrane potential, resulting in</p>

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

<p>FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase.</p>

<p>Biotin-PEG6-Thalidomide is a PROTAC linker based on PEG.</p>

<p>Thalidomide-Piperazine-PEG2-NH2 is a synthetic E3 ligase ligand-linker for PROTAC, combining cereblon ligand with a PEG2 linker.</p>

<p>VEGFR2/HDAC1-IN-1 (compound 13) is a potent dual inhibitor of VEGFR-2 and HDAC, with IC50 values of 57.83 nM for VEGFR-2 and 9.82 nM for HDAC.</p>

<p>Gemcitabine monophosphate disodium salt is a monophosphate derivative of Gemcitabine.</p>

<p>(+)-Mcl-1 inhibitor 22 (Example 37) is an MCL-1 inhibitor that impedes the anti-apoptotic function of MCL-1 by blocking its interaction with pro-apoptotic proteins. It demonstrates antiproliferative activity against various cancer cell lines and is applicable for cancer research.</p>

<p>HC Toxin: cyclic tetrapeptide, reversible HDAC inhibitor (IC50=30 nM), upregulates 15-lipoxygenase-1, induces fetal hemoglobin, from C. carbonum.</p>

<p>RET-IN-26 (compound D5) is a kinase inhibitor that selectively targets the RET protein with an IC50 value of 0.33 μM [1].</p>

<p>FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.</p>

<p>ADH-6 TFA disrupts mutant p53 self-assembly in cancer, restores function, and induces cell cycle arrest and apoptosis.</p>

<p>SRE-II, an amide derivative, serves as an activatable photosensitizer tailored for photodynamic cancer research, exhibiting diminished fluorescence and</p>

<p>GPLGIAGQ acetate: MMP2-cleavable peptide; stimulus-sensitive linker for MMP2-targeted liposomal/micellar carriers in photodynamic therapy.</p>

<p>P-gp inhibitor 16 (compound 14) is an inhibitor of p-glycoprotein. It significantly enhances apoptosis induced by doxorubicin and displays anticancer properties.</p>

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

<p>Thalidomide-4-C3-NH2 HCl is a cereblon ligand for CRBN recruitment, used to make PROTACs with a linker.</p>

<p>mTORinhibitor-27 (Compound 7e) is an inhibitor of mammalian target of rapamycin (mTOR) with an IC50 value of 5.47 μM. It can induce apoptosis in tumor cells and arrest the cell cycle in the S phase, thereby inhibiting cancer cell growth. mTORinhibitor-27 presents potential for research in cancer, including skin cancer.</p>

<p>Minocycline is a useful organic compound for research related to life sciences. The catalog number is T131626 and the CAS number is 10118-90-8.</p>

<p>HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4</p>

<p>HDAC3-IN-2 (compound 4i), a pyrazinyl hydrazide-based HDAC3 inhibitor with an IC50 of 14 nM, effectively targets triple-negative breast cancer cells.</p>

Chaetoglobosin A, the active compound extracted of Penicillium aquamarinium, is a member of the cytochalasan family. It preferentially induces apoptosis.

<p>VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively.</p>

Disitertide (P144) is an inhibitor of TGF-β1.

Bornyl acetate (Isobornyl acetate) has an anti-inflammatory effect. It is the volatile ingredient in some Chinese traditional herbs and numerous conifer oils.

<p>Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.</p>

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

<p>Top1-IN-2 (Compound 1a) is an inhibitor of topoisomerase 1 (Top1). It suppresses the growth of P-gp drug-resistant tumor cells and induces apoptosis.</p>

<p>KSRP-IN-1 (compound 8) acts as an inhibitor of KSRP, inducing cell cycle arrest and apoptosis (Apoptosis). This compound demonstrates antitumor activity.</p>

<p>Apoptosisinducer 28 (Compound X1) is an apoptosis inducer with demonstrated in vitro anticancer activity. It arrests the cell cycle at the G1 phase, promoting cell death and inducing apoptosis by disrupting the mitochondrial membrane potential.</p>

<p>Balstilimab (AGEN2034) is a fully human monoclonal IgG4 antibody against PD-1 [1] .</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>NYY-6a is a ferroptosis (Ferroptosis) inhibitor, demonstrating significant suppression of RSL3-induced ferroptosis in 786-O and HT-1080 cells, with EC50 values of 52 nM and 50 nM, respectively. As a radical-trapping antioxidant (RTA), NYY-6a effectively reduces lipid peroxidation, comparable to ferrostatin-1 and liproxstatin-1, making it useful for research into ferroptosis-related pathologies.</p>

<p>Zalypsis, a transcription factor inhibitor, is used potentially for the treatment of lymphoma, and cervical carcinoma.</p>

<p>ADAM-17 (TACE) and MMP inhibitor; attenuates TNF-α processing. Acts in concert with GM6001 to inhibit Chlamydia trachomatis growth.</p>

<p>TAT-BH4 (Bcl-xL), primarily localized at the mitochondria, inhibits apoptotic cell death.</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>Carnitine palmitoyltransferase 2 (CPT2), an enzyme involved in fatty acid oxidation, serves as a prognostic biomarker for colorectal cancer (CRC).</p>

<p>Methylene Violet 3RAX is a cationic dye that is a potential photosensitizer in photodynamic therapy and has antitumor activity.</p>

<p>ReACp53 acetate could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.</p>

F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.

<p>HSP70-IN-6 (Compound JL-15) acts as an inhibitor of the Hsp70-Bim protein-protein interactions (PPI) with an IC50 value of 70 nM. It induces apoptosis in chronic myeloid leukemia (CML) cells with EC50 values of 0.43 μM (BV173), 0.88 μM (K562), and 0.19 μM (K562-R3).</p>

<p>BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein</p>

<p>BK60106 is a selective and direct inhibitor of the transmembrane protein CD99, which causes cell death in Ewing Sarcoma cells.</p>

<p>Compound 2v (Anti-inflammatory agent 45) demonstrates anticancer properties with direct inhibitory impacts on the proliferation of various blood malignancies,</p>

<p>TRBP-IN-1 (Compound 13j) is an orally active inhibitor of TAR RNA-binding protein 2 (TRBP) with an IC50 of 12.72 μM. It exhibits significant anti-hepatocellular carcinoma (HCC) activity, effectively suppressing proliferation and metastasis of HCC cells [HCCLM3 cells (IC50: 18.96 μM) and SK-Hep-1 cells (IC50: 16.45 μM)]. TRBP-IN-1 modulates miRNA biosynthesis by targeting TRBP, inhibiting the expression of oncogenic miRNAs. It induces apoptosis and pyroptosis in HCC cells by decreasing miRNA levels. TRBP-IN-1 is suitable for research on targeted HCC therapy.</p>

<p>PROTAC 20S proteasome subunit β5 degrader 1 (compound 12f) serves as a targeted degrader of the 20S proteasome subunit β5, exhibiting a DC50 value of 0.11 μM in FaDu cells. This compound disrupts the cell cycle and promotes apoptosis (apoptosis), while inhibiting cell proliferation and migration in both FaDu and KM3/BTZ cells. It is applicable for research into resistance to Bortezomib in pharyngeal carcinoma and multiple myeloma.</p>

<p>PRLX-93936 HCL is an analog of erastin and demonstrated synergistic effects against non-small cell lung cancer (NSCLC) cells with cisplatin.</p>

<p>PG-11047 2HCl treats genitourinary, immune, genetic, ocular, blood/lymphatic disorders, and aids lymphoma/prostate cancer research.</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>CWI1-2 HCL: Potent IGF2BP2 inhibitor, induces apoptosis/differentiation, targets leukemia therapy.</p>

<p>PARP-1/2-IN-2-IN-1 (Compound 12e) effectively inhibits PARP1/2 and CDK12 with IC 50 values of 34 nM, 30 nM, and 285 nM respectively, impairing DNA damage repair</p>

<p>BCL6-IN-6 is an inhibitor of Bcl-6 and can be used in studies about diffuse large B-cell lymphoma.</p>

<p>84-B10 provides protection in cisplatin-induced acute kidney injury, reversing lipid peroxidation accumulation and downregulation of key ferroptosis inhibitors.</p>

<p>Lesigercept is a humanized antibody that targets IGHE.</p>

<p>PROTACNCOA4 degrader-1 (Compound V3) is a PROTAC-based degrader of NCOA4, exhibiting a DC50 of 3 nM in HeLa cells. Besides acting as a ferroptosis inhibitor, this compound effectively reduces the levels of NCOA4 and decreases intracellular ferrous (Fe2+) levels. Moreover, PROTACNCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model.</p>

<p>SDU-071 is a BRD4-p53 inhibitor, suppressing MDA-MB-231 cell proliferation, inducing cell cycle arrest and apoptosis.</p>

CLEFMA has anti-proliferative activity. CLEFMA inhibits tumor growth associated with NF-κB-regulated anti-inflammatory and anti-metastatic effects.

<p>KHKI-01215 is a NUAK2 inhibitor with anticancer activity, inhibiting the proliferation of SW480 cancer cells and inducing apoptosis.</p>

<p>IC 86621: DNA-PK ATP-competitive inhibitor, IC50 120 nM, enhances DSB antitumor effects, EC50 68 µM for repair.</p>

Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial.

<p>Oxythiamine (Hydroxythiamin) is a TK inhibitor that inhibits cancer cell proliferation, induces cell cycle arrest, and induces 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>