Apoptosis

<p>NLRP3-IN-26 (compound 15Z), with an IC50 of 0.13 μM, functions as an inhibitor of NLRP3. It is applicable in studies involving the DSS-induced colitis model [1].</p>

<p>WEHI-539 is a selective Bcl-XL inhibitor (IC50: 1.1 nM).</p>

<p>tDHU, acid is a dihydropyrimidine cereblon ligand consisting of an E3 ligase ligand and a benzoic acid linker. It serves as an E3 ubiquitin ligase ligand-linker conjugate in the development of PROTACs.</p>

<p>GLI1-IN-1 (CBC-1), a GLI-1 inhibitor, exhibits superior water solubility and anticancer properties. It effectively induces apoptosis and inhibits colorectal cancer growth by targeting the Hedgehog (HH) pathway (IC 50 = 1.3 μM) [1].</p>

<p>Compound B6, also known as TOPOI/PARP-1-IN-1, is a dual inhibitor targeting TOPOI and PARP, exhibiting low cytotoxicity and oral activity with a PARP1 IC 50 of 0.09 μM. This compound effectively inhibits cancer cell proliferation and migration, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis. In murine models, TOPOI/PARP-1-IN-1 demonstrated a tumor growth inhibition rate (TGI) of 75.4% [1].</p>

<p>EGFR-IN-3 is an EGFR inhibitor with antitumor activity.EGFR-IN-3 inhibits EGFRwt-TK, induces apoptosis (cell death), and can block cells in the G2/M phase.</p>

<p>Nitrovin is an antimicrobial growth promoter that induces ROS-mediated non-apoptotic and quasi-apoptotic cell death by targeting TrxR1. It exhibits anticancer activity with IC50 values ranging from 1.31 to 6.60 μM for both tumor and normal cells.</p>

<p>BRD-K56819078, a Bcl-2 inhibitor, significantly reduces the burden of senescent cells and the mRNA expression of aging-related genes in the kidneys. It exerts its anti-aging effects by inhibiting cell apoptosis (apoptosis).</p>

<p>Bcl-2-IN-3 (Compound 10) is an inhibitor of Bcl-2, utilized in cancer research.</p>

<p>Bomedemstat (IMG-7289) hydrochloride, an oral LSD1 inhibitor, has anticancer properties, blocking cell growth and triggering apoptosis.</p>

<p>SMIP34 is an inhibitor of PELP1, binding to this target with a dissociation constant (Kd) of 37.4 μM. It demonstrates efficacy in inhibiting the proliferation of cancer cells and tumor progression. Specifically, SMIP34 is effective in breast cancer research, showing activity against wild-type (WT), mutant (MT) estrogen receptor-positive (ER+), and treatment-resistant (TR)-ER+ breast cancers.</p>

<p>MDK-3345 is a reversible covalent inhibitor for Mcl-1.</p>

<p>VEGFR-2-IN-18 is a potent VEGFR-2 inhibitor with a 60 nM IC50, promoting cell apoptosis and anticancer effects.</p>

<p>Ferroptosis-IN-6 is an efficient ferroptosis inhibitor, protecting cells from cell death induced by ferroptosis inducers, and inhibiting STY-BODIPY oxidation.</p>

<p>AQIM-I is a survivin inhibitor that reduces survivin expression and colony formation. It promotes reactive oxygen species (ROS) production, apoptosis, cell cycle arrest, DNA damage, and autophagy. Moreover, AQIM-I effectively inhibits nonsmall cell lung cancer cells A549, with an IC 50 value of 9 nM [1].</p>

Ran-IN-1 (Compound M36) is an orally active and selective inhibitor of Ran GTPase. It binds allosterically with high specificity to the switch II pocket of GDP-bound Ran (RanGDP), stabilizing its inactive state and reducing the formation of active Ran-GTP. Ran-IN-1 induces apoptosis in epithelial ovarian cancer (EOC) cells and inhibits DNA repair pathways such as homologous recombination (HR) and non-homologous end joining (NHEJ). This compound shows potential for research in epithelial ovarian cancer, particularly in high-grade serous carcinoma.

<p>GLS1 Inhibitor-6: IC50=68nM, 220x more selective for GLS2, has anti-tumor and pro-apoptosis effects.</p>

<p>TFCP2L1-IN-1 is a TFCP2L1 transcription factor inhibitor that regulates cell proliferation and promotes antitumor effect of Sorafenib by STAT3/NANOG pathway.</p>

<p>TopoisomeraseI/II inhibitor 8 (Compound Ru7) is a dual catalytic inhibitor of TopoisomeraseI/II that induces DNA damage and activates PARP-1, leading to the activation of RIPK1, RIPK3, and MLKL, ultimately causing necroptosis. It shows significant anticancer activity by effectively targeting cancer cell nuclei and inducing cell death through necroptosis, offering substantial clinical potential in overcoming resistance in cancer treatment.</p>

<p>ZSH-512 is a potent inhibitor of RARγ with antiproliferative properties. It induces apoptosis and reduces the expression of CD133, NANOG, SOX2, and EPCAM proteins. ZSH-512 exhibits anticancer activity and shows potential for colorectal cancer research.</p>

<p>HL001 is an orally active small molecule inhibitor of cyclophilin A (CypA) and a receptor antagonist of lysophosphatidic acid 1 (LPA1). It induces cell cycle arrest and apoptosis in tumor cells via p53. By downregulating G3BP1, HL001 promotes reactive oxygen species production and DNA damage to stabilize p53. It disrupts the interaction between MDM2 and p53-72R in a CypA-dependent manner. HL001 exhibits antitumor activity and can also be used in research on pulmonary fibrosis.</p>

<p>VEGFR-2-IN-15 (Compound 14b) is a potent inhibitor of VEGFR-2. VEGFR-2-IN-15 inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.</p>

<p>NA-17 is a naphthalimide compound with antitumor activity and exhibits lower toxicity to normal cells such as HL-7702 and WI-38. It demonstrates p53-dependent inhibition selectivity in various NSCLC cells, inducing the accumulation of active p53 in the mitochondria and nuclei of these cells. NA-17 causes cell cycle arrest in the G1 phase and promotes apoptosis and cell death.</p>

<p>Ferrostatin-1 diyne (Fer-1 diyne) (compound 2) serves as an inhibitor of ferroptosis, accumulating in cellular lysosomes, mitochondria, and the endoplasmic reticulum. It notably inhibits ferroptosis independently of lysosomal and mitochondrial activity.</p>

<p>HC-7366 (GCN2 modulator-1) is an orally active GCN2 kinase activator with antitumor activity, inducing tumor growth inhibition.</p>

<p>Z-VAD is an irreversible pan-caspase inhibitor, suppressing multiple caspases including caspase-3, -6, -7, -8, and -9. Z-VAD induces autophagy in tumour cells.</p>

<p>Pan-Trk-IN-3: potent Trk inhibitor (IC50: 2-26 nM), effective against drug-resistant mutants, induces apoptosis, anti-tumor effects.</p>

<p>BRD4/CK2-IN-1 is a small-molecule inhibitor targeting BRD4 and CK2, inducing apoptosis and autophagy-related cell death.</p>

<p>Glyphosate isopropylammonium is a broad-spectrum, non-selective systemic biocide derived from the amino acid glycine. It inhibits the enzyme activity of 5-enolpyruvylshikimate-3-phosphate synthase (EPSPS) in the shikimate pathway, blocking the synthesis of aromatic amino acids tyrosine, phenylalanine, and tryptophan. Additionally, Glyphosate isopropylammonium induces oxidative stress, neuroinflammation, and mitochondrial dysfunction, leading to neuronal death through autophagy, necrosis, or apoptosis, resulting in behavioral and motor disturbances.</p>

<p>EGFR-IN-47: strong oral EGFRL858R/T790M/C797S blocker, induces cell death; promising for NSCLC research. IC50: 0.01 μM.</p>

<p>Thalidomide-NH-amido-PEG1-C2-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, used in the synthesis of PROTAC.</p>

<p>ERK1/2 inhibitor 11 (compound L6) is a dual inhibitor of ERK1/2 that promotes the accumulation of DSBs and the degradation of ERK1/2 expression. This compound decreases BCL-2 levels and induces DNA damage by inhibiting PARP and ERK1/2. Additionally, ERK1/2 inhibitor 11 activates caspase 3 to induce apoptosis.</p>

<p>Thalidomide-NH-amido-PEG2-C2-NH2 is a synthetic E3 ligase ligand-linker conjugate comprising a Thalidomide-based cereblon ligand and a linker. It is utilized in the synthesis of PROTACs.</p>

<p>GRP78-IN-1 binds to GRP78 protein, inhibits cell growth, and triggers apoptosis in breast cancer; has -8.07 kcal/mol binding energy.</p>

<p>Compound 5f, a potent tubulin polymerization inhibitor (IC50 = 1.09 μM), blocks cell migration, tube formation, and has anti-angiogenic effects.</p>

<p>DWP-05195 is a TRPV1 antagonist capable of inhibiting pain signal transduction. Additionally, it induces ER stress-dependent apoptosis in human ovarian cancer cells via the ROS-p38-CHOP pathway.</p>

<p>CRI9 effectively inhibits the c-MET/PI3K/Akt/mTOR axis, suppressing the proliferation of hepatocellular carcinoma (HCC) cells. This compound exhibits potent cytotoxicity against HCC cells and induces apoptosis.</p>

<p>MG-B-28, a BTLA-HVEM inhibitor, demonstrates an IC50 value of 906 nM. It promotes T cell activation dose-dependently by inhibiting the interaction between BTLA and HVEM.</p>

<p>RET-IN-10: Potent RET inhibitor, may treat congenital megacolon and tumors (Patent WO2021135938A1, compound 18).</p>

<p>Antiangiogenic agent 7 (Compound 1) induces apoptosis, elevates Reactive Oxygen Species (Reactive Oxygen Species), and inhibits the intracellular enzyme thioredoxin reductase. It exhibits anticancer activity with IC50 values ranging from 0.08 to 3.5 μM against cervical cancer cells (HeLa), prostate cancer cells (PC-3), and non-small cell lung cancer cells (A549). Additionally, Antiangiogenic agent 7 suppresses tumor growth in a mouse xenograft model.</p>

<p>MLS-0053105, a chloromaleimide, functions as a selective inhibitor of BFL-1, exhibiting an IC50 of 0.4 µM against Bfl-1/F-Bid. Its inhibitory potency is over tenfold lower for Bcl-W, Bcl-2, and Bcl-XL, and it shows no activity against Bcl-B and Mcl-1.</p>

<p>DC-U4106: USP8 inhibitor, Kd 4.7μM, IC50 1.2μM, degrades Erα, low-toxicity tumor suppressor for breast cancer research.</p>

<p>Compound 3 (DOR agonist 2) acts as a Delta Opioid Receptor agonist. It inhibits the expression of TNF-α, obstructs NF-κB transportation to the nucleus, and activates the G protein-mediated ERK1/2 pathway. This compound is useful for research into neurodegenerative diseases.</p>

<p>Tubulin/NRP1-IN-1 (compound TN-2) serves as a dual inhibitor targeting both Tubulin and NRP1, exhibiting IC50 values of 0.71 μM and 0.85 μM, respectively. This compound notably reduces the viability of prostate tumor cell lines and triggers apoptosis [1].</p>

<p>Sabialimon P (compound 16), with an IC50 of 18.12 μM, functions as a NO release inhibitor and exhibits anti-inflammatory properties. It effectively diminishes the secretion of TNF-α, iNOS, IL-6, and NF-κB, and suppresses the expression of COX-2 and NF-κB/p65 in LPS-induced RAW264.7 cells.</p>

<p>RIPK1-IN-23 (compound 19) is an RIPK1 inhibitor with potent anti-necroptotic effects in HT-29 cells (EC50 = 1.7 nM). Additionally, RIPK1-IN-23 exhibits anti-inflammatory properties.</p>

<p>BCL6-IN-3: potent BCL6 inhibitor, 70 nM GI50 in SU-DHL4, affects cell functions, antitumor.</p>

<p>Lometrexol (LY 264618) is an antifolate that inhibits GARFT, blocks purine synthesis, induces apoptosis, and has anticancer properties.</p>

<p>Milademetan (DS-3032), an MDM2 inhibitor, exhibits antitumor activity, induces G1 cell cycle arrest and apoptosis, and can be used to study solid tumors.</p>

<p>Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and antitumor properties, inhibiting Sox4 translation and inducing apoptosis.</p>

<p>HC-5404 is a potent and selective PERK inhibitor, blocking the activation of the PERK pathway, anti-tumor effects, advanced solid tumors and renal cell Cancer.</p>

<p>SY-5609 (CDK7-IN-3) is a selective non-covalent CDK7 inhibitor, with weak inhibitory activity against CDK2, CDK9 and CDK12.Cost-effective and quality-assured.</p>

<p>UH15-38 is a potent and selective RIPK3 inhibitor that blocks necroptosis in alveolar epithelial cells triggered by IAV, useful for studying lung inflammation.</p>

<p>Tuvusertib (M1774), an oral ATR inhibitor (Ki&lt;1µM), selectively blocks CHK1 phosphorylation, disrupts DNA repair, and induces tumor cell apoptosis.</p>

<p>Vatalanib hydrochloride (PTK787 hydrochloride) is an orally available and highly potent tyrosine kinase (VEGF) inhibitor that reduces the number and size of Aβ plaques in the cortex of 5xFAD mice, which may be useful in the study of Alzheimer's disease and cancer.</p>

<p>PF-07328948 is a branched-chain keto-acid dehydrogenase kinase (BDK) inhibitor, useful for studying CVD metabolic disorders.</p>

<p>JAK2-IN-7 selectively inhibits JAK2 (IC50: 3 nM), shows 14-fold selectivity over JAK1/3, FLT3, induces G0/G1 arrest, apoptosis, and has antitumor effects.</p>

<p>CP-4126, a lipophilic pro-drug of Gemcitabine, converts to active form by esterases, allowing oral administration with dose-dependent effects.</p>

<p>FX-11: potent LDHA inhibitor (Ki 8 μM), activates PKM2, reduces ATP, induces oxidative stress/ROS, cell death, shows antitumor effects.</p>

<p>AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.</p>

<p>WEHI-539 hydrochloride is a selective Bcl-XL inhibitor with an IC50 of 1.1 nM.</p>

<p>OBAA is a potent inhibitor of phospholipase A2 (PLA2) with an IC 50 of 70 nM. OBAA blocks Melittin-induced Ca 2+ influx in Trypanosoma brucei with an IC 50 of 0.4 μM [1] [2] [3].</p>

<p>PIM-447 dihydrochloride is an orally available and selective inhibitor of pan-PIM kinase(Ki values of 6, 18, and 9 pM for PIM1, PIM2, and PIM3, respectively).</p>

Beta-Zearalenol, a derivative of zearalenone (ZEA) capable of conjugating with glucuronic acid[2], is a mycotoxin produced by Fusarium spp. It induces apoptosis and oxidative stress in mammalian reproductive cells[1].

<p>Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces and a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. It also induces apoptosis and inhibits aminopeptidase M, aminopeptidase N, and leucine aminopeptidase, as well as MMP-1, MMP-3, MMP-8, MMP-9, and meprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin exhibits antiproliferative and antitumor activities [1][2][3][4][5].</p>

<p>(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an inhibitor of P-Glycoprotein.</p>

<p>Carubicin HCl is an anthracycline antineoplastic antibiotic. Through intercalates into DNA and interacts with topoisomerase II, Carubicin inhibits DNA replication and repair and RNA and protein synthesis.</p>

<p>Ciprofloxacin lactate is a useful organic compound for research related to life sciences. The catalog number is T66299 and the CAS number is 97867-33-9.</p>

<p>PGA2 is a naturally occurring prostaglandin in gorgonian corals where it may function in self defense. It is generally not present in mammals. PGA2 has low biological potency in most bioassays, but it does show some antiviral/antitumor activity.[1] At a 25 uM concentration, PGA2 blocks the cell cycle progression of NIH 3T3 cells at the G1 and G2/M phase .[2] It has also been shown to act as a vasodilator with natriuretic properties.[3]</p>

<p>Thalidomide-5-COOH is a useful organic compound for research related to life sciences. The catalog number is T64600 and the CAS number is 1216805-11-6.</p>

<p>Yatein inhibits herpes simplex virus type 1 replication by interruption the immediate-early gene expression. Yatein is a lignan isolated from A. chilensis. It also has antiproliferative activity.</p>

<p>A-192621 is a potent, nonpeptide, orally active, and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. A-192621 promotes apoptosis in PASMCs and elevates both arterial blood pressure and plasma ET-1 levels[1][2][3]. Its selectivity is 636-fold higher for ETB than ETA (IC50 of 4280 nM and Ki of 5600 nM).</p>

<p>XMU-MP-3 is a robust, non-covalent inhibitor of BTK, exhibiting exceptional potency with IC50 values of 10.7 nM and 17.0 nM for BTK WT and BTK C481S mutation, respectively, in the presence of 10 μM ATP. Moreover, XMU-MP-3 elicits apoptosis.</p>

<p>Ingenol 3,20-dibenzoate is a powerful activator of protein kinase C (PKC) isoforms that effectively induces the translocation of nPKC-delta, -epsilon, and -theta, as well as PKC-mu, from the cytosolic fraction to the particulate fraction. Through de novo synthesis of macromolecules, it triggers apoptosis with characteristic morphology. Moreover, Ingenol 3,20-dibenzoate enhances IFN-γ production and degranulation in NK cells, particularly when stimulated by NSCLC cells[1][2].</p>

<p>Thalidomide-O-C6-COOH is a synthetic conjugate that combines a Thalidomide-derived cereblon ligand with a PROTAC technology linker (E3 ligase ligand-linker).</p>

<p>Vatiquinone, also known as EPI 743, is an orally bioavailable para-benzoquinone being developed for inherited mitochondrial diseases. The mechanism of action of EPI-743 involves augmenting the synthesis of glutathione, optimizing metabolic control, enhanc</p>

<p>Imifoplatin (PT-112) is a platinum compound with antitumor activity and may be used to study prostate cancer and immune system disorders.</p>

<p>MI-773 is a potent inhibitor of the MDM2-p53 protein interaction (PPI) with a high affinity for MDM2 and a Kd value of 8.2 nM. MI-773 exhibits antitumour effects.</p>

<p>Thalidomide-O-C5-NH2 hydrochloride is a synthetic compound consisting of a ligand-linker conjugate with E3 ligase activity. It combines a cereblon ligand based on Thalidomide and a linker commonly utilized in PROTAC technology.</p>

<p>Mcl-1 inhibitor 6 binds Mcl-1 with KD 0.23 nM and Ki 0.02 μM, shows strong selectivity over Bcl-2 family, and demonstrates antitumor efficacy.</p>

<p>Swainsonine (Tridolgosir) is an alkaloid isolated from Astragalus membranaceus and is a potent and reversible inhibitor of alpha-mannosidase. swainsonine has antitumour activity and induces apoptosis and cell cycle arrest in the G2/M phase.</p>

<p>Thalidomide-O-amido-C4-NH2 hydrochloride, a synthesized E3 ligase ligand-linker conjugate, combines the cereblon ligand derived from Thalidomide with a linker and is commonly used in the synthesis of PROTACs[1].</p>

<p>DB818 is a synthetic Homeobox A9 (HOXA9) inhibitor and can be used for research on the treatment of acute myeloid leukaemia associated with HOXA9 overexpression.</p>

<p>SCH79797 is a potent and specific protease-activated receptor 1 (PAR1) antagonistwith antimicrobial, anticancer, anti-inflammatory, and neuroprotective effects.</p>

<p>RRD-251 is an Rb-Raf-1 interaction inhibitor that induces apoptosis in metastatic melanoma cells and synergizes with dacarbazine[1].</p>

<p>Ac-IETD-CHO TFA is a granzyme B and caspase-8 inhibitor that inhibits caspase8 activity by blocking caspase3 precursor cleavage.Ac-IETD-CHO TFA inhibits Fas-mediated apoptosis.</p>

<p>ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.</p>

<p>CTB (Cholera Toxin B subunit) is an activator of p300 histone acetyltransferase and induces apoptosis in MCF-7 cells.</p>

<p>Anti-TNBC agent-2 (3j), a purine derivative, acts as an anti-triple negative breast cancer (TNBC) therapeutic.</p>

<p>CHMFL-48, an orally active inhibitor of BCR-ABL kinase, demonstrates efficacy against both the wild-type (wt) and various imatinib-resistant mutants. It exhibits potent inhibitory activity, with IC 50 values of 1 nM for the ABL wild-type and 0.8 nM for the ABL T315I mutant. CHMFL-48 operates by inhibiting the autophosphorylation of both wild-type and mutant BCR-ABL, affecting downstream signaling mediators including STAT5 and CRKL. This disruption leads to cell cycle arrest and triggers apoptosis. Given its properties, CHMFL-48 is a promising candidate for research on chronic myeloid leukemia (CML).</p>

<p>Cyy-272 is an orally active JNK inhibitor with IC50 values of 1.25, 1.07, and 1.24 μM against JNK1, JNK2, and JNK3, respectively. It exerts anti-inflammatory effects by inhibiting the phosphorylation of JNK, thereby alleviating acute lung injury (ALI) induced by lipopolysaccharide (LPS). Moreover, Cyy-272 significantly reduces inflammation in cardiomyocytes and cardiac tissues caused by high lipid concentrations, further mitigating resultant cardiac hypertrophy, fibrosis, and apoptosis. Cyy-272 is utilized in the study of obesity-related myocarditis.</p>

<p>IHMT-MST1-39 is an orally effective MST kinase inhibitor with IC50 values of 42 nM for MST1 and 109 nM for MST2. It activates the AMPK signaling pathway in hepatocytes and inhibits apoptosis in pancreatic β cells. Additionally, IHMT-MST1-39 improves type 1 diabetes in mice induced by Streptozotocin.</p>

<p>SMIP34 is an inhibitor of PELP1 that demonstrates the capability to reduce cell viability and colony formation. Additionally, SMIP34 induces cell apoptosis (apoptosis) and causes cell cycle arrest in the S phase. It reduces the expression of PELP1 and exhibits anti-tumor activity. SMIP34 also has potential for research in triple-negative breast cancer (TNBC).</p>

<p>ZSQ836 is a dual covalent inhibitor of CDK12/CDK13 with oral bioactivity, displaying an EC50 value of 32 nM against CDK12. This compound can induce cell apoptosis (apoptosis) and demonstrates in vivo anticancer properties. ZSQ836 is applicable for research in ovarian cancer.</p>

<p>DETD-35 is a promising chemical compound in anti-melanoma therapy, functioning as an inhibitor of the MEK-ERK, Akt, and STAT3 signaling pathways. It enhances cancer cell apoptosis (Apoptosis) and diminishes resistance to Vemurafenib in cancer cells. The compound exhibits IC 50 values of 2.7, 6.0, 3.9, 3.1, and 2.5 μM against melanoma cell lines B16-F10, MeWo, SK-MEL-2, A2058c, and A375c, respectively. DETD-35 offers significant potential for advancing research in melanoma treatment strategies.</p>

<p>Taltobulin (HTI-286) is a synthetic analog of the tripeptide cysteine, a microtubule protein inhibitor that inhibits liver tumor cell proliferation in vitro and tumor growth in vivo.Taltobulin is cytotoxic, induces mitotic arrest and apoptosis, and may be used in the study of breast cancer and microtubule tissue-related diseases.</p>