Apoptosis

<p>icFSP1 is a mitochondria-associated apoptosis-inducing factor regulator with antitumor activity for the study and treatment of tumor diseases.</p>

<p>Arisostatin A is a secondary metabolite produced by microorganisms, recognized as an antibiotic (antibiotic) with activity against Gram-positive bacteria. This compound also exhibits potent antitumor properties. It induces apoptosis (apoptosis) by activating caspase-3 and generating reactive oxygen species (ROS) in AMC-HN-4 cells.</p>

<p>DAPK-IN-2: DAPK inhibitor with anticancer potential. Used in cerebral infarction and ischemia research.</p>

<p>XZ739: Cereblon-based PROTAC, degrades BCL-XL (DC50 2.5 nM in MOLT-4, 16hr), induces caspase apoptosis.</p>

<p>GPX4-IN-6 is a GPX4 inhibitor with antitumor activity.GPX4-IN-6 induces iron death and is used for the treatment and prevention of triple-negative breast cancer</p>

<p>(±)-Indoxacarb is a pyrazoline insecticide with insecticidal activity and cytotoxicity, blocks sodium channels in insect neurons, and can induce apoptosis.</p>

<p>S65487 (VOB560) hydrochloride, a potent and selective Bcl-2 inhibitor, is effective against BCL-2 mutations, including G101V and D103Y.</p>

<p>Thalidomide-based E3 ligase ligand with PEG2-C2 linker; used as an immunomodulatory cancer treatment.</p>

<p>MSU-42011: oral RXR-like agonist, inhibits iNOS &amp; p-ERK, antitumor in lung cancer model, effective preclinical treatment.</p>

<p>MKC-1 (Ro-31-7453) is an oral bisindolylmaleimide inhibitor that disrupts tubulin polymerization, potentially halting cancer cell division.</p>

<p>G-Glu-Val (γ-glutamyl-L-valine, H-Glu-Val -OH), a flavour-regulating dipeptide, is a major contributor to "mellow".</p>

<p>Thalidomide-based cereblon ligand linked to PROTAC technology as E3 ligase ligand-linker.</p>

<p>4-N-Nonyloxyphenol, kaolinite nanotube photosensitizer, degrades phenolic pesticides, and disrupts endocrine.</p>

<p>Antitumor agent-198 (Compound A3) exhibits cytotoxicity in head and neck squamous cell carcinoma (HNSCC) cells, effectively inhibiting the proliferation of CAL27, HN6, HN30, SCC9, and SCC25, with an IC50 ranging from 4 nM to 77 nM. Additionally, Antitumor agent-198 suppresses HNSCC cell migration, arrests the cell cycle, and induces apoptosis.</p>

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

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

<p>Cefatrizine inhibits eEF-2 kinase, affecting apoptosis, autophagy, and ER stress in cancers.</p>

<p>Tubulin polymerization-IN-43 disrupts microtubules, arrests cell cycle, and induces apoptosis in leukemia by targeting colchicine sites.</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>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>UAMC-4821 is a ferroptosis inhibitor with an IC50 of 5.2 nM. It effectively scavenges free radicals, inhibits lipid peroxidation, and prevents ML162-induced ferroptosis, providing protective effects on HT-1080 cells. With favorable pharmacokinetic properties in mice, UAMC-4821 presents an oral bioavailability of 63% and demonstrates blood-brain barrier permeability.</p>

<p>TG101209 analog 1 (Compound 8h) serves as an inhibitor of BUB1B, exhibiting an IC50 of 10.36 μM. It also possesses cytotoxic properties, demonstrated by an IC50 of 1.347 μM against Caki-1 cells, and can induce necrosis and apoptosis.</p>

<p>VPC-70063 (Thiourea, N-[3,5-bis(trifluoromethyl)phenyl]-N'-(phenylmethyl)-) is an inhibitor of c-Myc-MAX.</p>

<p>Methyl-4-oxoretinoate is a synthetic retinoid with anticancer properties, used for skin conditions and potential ocular treatments.</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>CDK2-IN-41 (Compound 7a) is a CDK2 inhibitor that impedes the cell cycle by binding to CDK2, leading to cytotoxicity, increased ROS production, and apoptosis (Apoptosis). It exhibits anticancer activity with an IC50 of 10 µM against acute myeloid leukemia (AML) HL-60 cells. CDK2-IN-41 is applicable in research related to AML-associated cancers.</p>

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

<p>CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target inhibitor of CYP51/PD-L1, displaying IC50 values of 0.17 and 0.021 μM, respectively.</p>

<p>Thevetiaflavone, a natural flavonoid from W. indica, blocks LDH leakage, boosting cell survival.</p>

<p>TopoII/tubulin-IN-1 (Compound 1B8) is an inhibitor of TopoII/tubulin. It effectively suppresses the proliferation of tumor cells and reduces ROS levels, while inducing apoptosis and cell cycle arrest, without showing significant cytotoxicity to normal cells. TopoII/tubulin-IN-1 exhibits antitumor activity.</p>

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

<p>PZ703b is a novel BCL-XL PROTAC degrader with enhanced BCL-2 inhibition.</p>

<p>Violacein, a purple antibacterial and antiprotozoal compound from C. violaceum, effective against Gram-positive bacteria and P. falciparum.</p>

<p>Shepherdin 79-87: Amino acid fragment 79-87 of Hsp90/Survivin antagonist with anticancer properties.</p>

<p>Anticanceragent 204 (Compound 6) is a fluorinated derivative of cinnamamides with anticancer activity. It can arrest the cell cycle of HepG2 cells in the G1 phase and induces apoptosis by reducing mitochondrial membrane polarization (MMP) levels.</p>

<p>PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)</p>

<p>MX106-4C is a survivin inhibitor that selectively targets ABCB1-positive colorectal cancer cells. It can work synergistically with Doxorubicin for enhanced anticancer effects or restore Doxorubicin sensitivity in drug-resistant ABCB1 cells.</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>Ac-VDVAD-CHO (TFA) is a caspase-2/3 inhibitor with IC50 values of 46 nM and 15 nM, respectively.</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>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>Thalidomide-NH-(CH2)2-NH2 TFA is an alkyl-modified derivative of Thalidomide serving as a Cereblon ligand to recruit CRBN proteins and a pivotal intermediate in</p>

<p>DHFR-IN-23 (compound 5) is a dual inhibitor of DNA binders/DHFR, exhibiting an IC50 value of 0.08 μM against hDHFR. It serves as an apoptosis inducer and is applicable in research on ER+ breast cancer.</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>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>MS1943 is a orally bioavailable EZH2 selective degrader(IC50 of 120 nM).</p>

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

<p>NF-κB-IN-19 (Compound 8) is an NF-κB inhibitor. It effectively induces DNA damage in tumor cells through the NF-κB signaling pathway and promotes the production of reactive oxygen species (ROS), as well as induces autophagy and apoptosis. Additionally, NF-κB-IN-19 inhibits levels of VEGF and HIF-1α, exerting antiproliferative effects in tumor cells through the PI3K/AKT and STAT-3 pathways. It is also effective in overcoming cisplatin resistance and exhibits antitumor activity.</p>

<p>Z-VEID-FMK is a selective caspase-6 peptide inhibitor that irreversibly covalently binds to the enzyme, thereby inhibiting apoptosis and DNA breakage.</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>HPOB is an effective and specific HDAC6 inhibitor (IC50: 56 nM), &gt;30-fold selectivity over other HDACs.</p>

<p>TS-24 is a cysteine protease histone S (CTSS) inhibitor that promotes BRCA1-mediated apoptosis.</p>

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

<p>Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist.</p>

<p>UCM-1336 (3,3′-(Octylimino)bis[N-phenylpropanamide]) is a potent ICMT inhibitor with an IC50 of 2 μM which is selective against the other enzymes involved in</p>

<p>SDH-IN-26 (Compound C3) is a succinate dehydrogenase (SDH) inhibitor with significant inhibitory activity against various plant pathogenic fungi, including solanrhizoctonia and Botrytis cinerea. It exhibits an EC50 value of 0.270 μg/mL against solanrhizoctonia. SDH-IN-26 compromises fungal cell membrane integrity, increases membrane permeability, disrupts cell structure, reduces mitochondrial count, and affects normal hyphal growth. It also decreases mitochondrial membrane potential, inducing apoptosis. SDH-IN-26 holds potential for studying plant diseases caused by fungi.</p>

<p>Thalidomide-O-amido-C8-NH2 hydrochloride, a synthetic cereblon ligand-linker for PROTAC synthesis.</p>

<p>PTP1B-IN-30 (Compound 3j) is an inhibitor of PTP1B with an IC50 of 0.51 µM. It suppresses the proliferation of T47D cancer cells with an IC50 of 21.21 µM, induces cell cycle arrest at the S phase, and triggers apoptosis in T47D cells.</p>

<p>YCH3124 (compound Z33) is an inhibitor of USP7, exhibiting anti-tumor activity with an IC50 value of 41.9 nM. This compound demonstrates substantial in vitro anti-proliferative effects on various tumor cells, including LNCaP (IC50= 3.6 nM) and CHP-212 (IC50=9.9 nM). Moreover, YCH3124 induces apoptosis in CHP-212 cells by disrupting the cell cycle process during the G1 phase.</p>

<p>RO7567132 is a bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, inducing the formation of local TLS.</p>

<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>

<p>Eldecalcitol, orally active vitamin D analog, boosts bone density and treats osteoporosis.</p>

<p>Thalidomide-O-PEG2-propargyl is a cereblon-based E3 ligase ligand with a PEG linker for PROTAC-induced protein degradation.</p>

<p>ROCK/HDAC-IN-2 (Compound C-9) is a dual inhibitor of ROCK/HDAC, characterized by IC50 values of 0.185 µM for HDAC6, 0.8 µM for ROCK1, and 0.7 µM for ROCK2. It effectively induces apoptosis and mitochondrial membrane potential alterations in cancer cells and demonstrates notable antitumor activity, making it useful for research in pancreatic ductal adenocarcinoma (PDAC) and triple-negative breast cancer (TNBC).</p>

<p>Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.</p>

<p>Narasin (sodium salt) (HainanMycin) induces tumor necrosis factor-related apoptosis-induced ligand (TRAIL)-mediated apoptosis by ER stress in glioma cells and</p>

<p>SI-2, a SRC-3 inhibitor, triggers breast cancer cell death (IC50: 3-20 nM), sparing normal cells.</p>

<p>Mcl-1 antagonist 1 is a Mcl-1 protein antagonist.</p>

<p>pdTp is a highly selective, small-molecule miRNA regulatory complex RISC subunit SND1 inhibitor.</p>

<p>EPZ020411 hydrochloride is a selective and potent small molecule PRMT6 inhibitor with an IC50 value of 10 nM.</p>

<p>cytoplasmic peptide of the neurotrophin receptor p75NTR</p>

<p>C188, a naphthol-based STAT3 inhibitor, blocks IL-6-induced STAT3 activity in HepG2 cells, sparing STAT1.</p>

<p>Oligomycin B is an antibiotic isolated from marine Streptomyces, is an eukaryotic ATP synthase inhibitor, induces apoptosis.</p>

<p>Anti-Mouse PD-1 Antibody (D265A) is an IgG2a, κ antibody inhibitor derived from mice, specifically targeting mouse PD-1.</p>

<p>anti-TNBC agent-1 targets TNBC effectively, with IC50 of 0.20-0.27 μM, inducing apoptosis and G1 arrest in SUM-159 cells.</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>dFKBP-1 is a potent and PROTAC-based FKBP12 degrader. dFKBP-1 incorporates the ligand SLF of FKBP12, the Thalidomide based cereblon ligand and a linker[1].</p>

<p>Phenamet is a bioactive chemical.</p>

<p>PZ703b hydrochloride, a Bcl-xl PROTAC, triggers apoptosis and halts cancer growth; used in bladder cancer studies.</p>

<p>RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.</p>

<p>Z-LEHD-FMK is a selective and potent caspase-9 inhibitor that protects against reperfusion injury and slows apoptosis.Z-LEHD-FMK exhibits antitumor and</p>

<p>Secalonic acid D, from Aspergillus aculeatus, is anti-tumor, activates GSK3-β, degrades β-catenin, inhibits c-Myc, and induces apoptosis.</p>

<p>Thalidomide-based E3 ligase ligand-linker for PROTAC, with cereblon ligand and C8-NH2 hydrochloride.</p>

<p>DB2313 is a potent PU.1 inhibitor (IC50=14 nM) that disrupts gene binding, induces AML cell apoptosis, and has anticancer properties.</p>

<p>LIB3S0280 is a potent inhibitor of TBK1, with an IC50 of 493.9 nM. It suppresses TBK1 downstream signaling by reducing the phosphorylation of IκBα and AKT. LIB3S0280 causes G2/M phase arrest and induces apoptosis in pancreatic cancer cells. Notably, it exhibits significant inhibitory effects on pancreatic cancer cell lines with high TBK1 expression, with a 96-hour IC50 value ranging from 6.64-10.98 μM. LIB3S0280 shows potential for research in pancreatic ductal adenocarcinoma (PDAC).</p>

<p>MPT0B014 is a potent tubulin polymerization inhibitor. MPT0B014 can induce cancer cell apoptosis.</p>

<p>PD-166285 is an effective and broadly active inhibitor of protein tyrosine kinase.</p>

<p>Baceridin, a cyclic hexapeptide and proteasome inhibitor, can be isolated from the culture medium of Epiphytic Bacillus.</p>

<p>"MRT-2359: Oral GSPT1 reducer, anti-cancer, targets NSCLC/SCLC, effective on MYC-driven cells."</p>

<p>INF200 (compound 5), a sulfonylurea-based inhibitor of NLRP3 and associated pyroptosis, exhibits cardiometabolic benefits in a rat model of high-fat diet (HFD)-</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>Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.</p>

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

<p>Apoptosisinducer 33 (compound H2) is a hydrazone derivative. It exhibits antioxidant and antimicrobial properties, capable of inhibiting the growth of Staphylococcus aureus, Escherichia coli, and Candida albicans. Additionally, Apoptosisinducer 33 can suppress tumor cell proliferation and induce apoptosis (apoptosis), making it useful for tumor research.</p>

<p>(R)-MIK665 is the less active enantiomer of MIK665. MIK665 is a special inhibitor of Mcl-1(IC50 of 1.81 nM).</p>

<p>PKM2-IN-8 (Compound 9b) is an inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.31 μM. It exhibits potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 induces early apoptosis and reduces lactate levels. This compound is useful for research in glioblastoma.</p>

<p>Furazolidone (Furoxone), a nitrofuran derivative, inhibits AML1-ETO transformed cells with IC50 value of 12.7 μM.</p>

<p>Z-Asp-CH2-DCB is an irreversible inhibitor of broad spectrum caspase.</p>

<p>Ajoene from garlic has antibacterial, anticancer, antiplatelet, and antioxidant effects; it combats various bacteria, yeasts, and cancer cells.</p>

<p>Mepacrine (Erion) is an acridine derivative formerly widely used as an antimalarial.</p>

<p>FTO-IN-14 (Compound F97) is an inhibitor of the RNA demethylase Fat mass and obesity-associated protein (FTO), with an IC50 of 0.45 μM. It modulates the expression of the ASB2, RARA, and MYC proteins. FTO-IN-14 demonstrates antiproliferative activity in AML cancer cells, with IC50 values of 0.7-5.5 μM against MOLM13, NB4, HEL, OCI-AML3, MV4-11, and MONOMAC6, and induces apoptosis in NB4 cells. Additionally, FTO-IN-14 exhibits antitumor activity in a mouse NB4 xenograft model.</p>

<p>Thalidomide 4'-oxyacetamide-alkyl-C2-amine HCl is an E3 ligase ligand-linker conjugate containing the E3 ubiquitin ligase cereblon (CRBN) and linker.</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>

<p>Thalidomide-NH-C6-NH2 is a synthetic conjugate compound designed as an E3 ligase ligand-linker.</p>

<p>PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.</p>