Apoptosis

<p>Ketorolac (RS37619) hydrochloride is a nonsteroidal anti-inflammatory drug and a non-selective COX inhibitor, exhibiting IC50 values of 20 nM for COX-1 and 120 nM for COX-2. This compound is utilized in a 0.5% ophthalmic solution format for the investigation of allergic conjunctivitis, cystoid macular edema, intraoperative miosis, and post-operative ocular inflammation pain. Additionally, Ketorolac hydrochloride serves as a DDX3 inhibitor, making it pertinent for research in cancer therapies.</p>

<p>Potent oral XIAP/cIAP1 inhibitor with EC50s: XIAP 5.1 nM, cIAP1 0.32 nM; curbs tumor growth in vivo.</p>

<p>BMS 310705, an Epothilone B analog, targets ovarian/renal/bladder/lung cancer, inducing apoptosis via mitochondria.</p>

<p>Potent dual c-Met/HDAC inhibitor, IC50: HDAC1 5.4 nM, c-Met 18.49 nM; anti-cancer, induces apoptosis, G2/M arrest in HCT-116.</p>

<p>Topoisomerase inhibitor4 (compound 45) acts as an effective inhibitor of Topoisomerase1/2, arresting the cell cycle at the G2/M phase and inducing Apoptosis. This compound exhibits potent antitumor activity.</p>

<p>PD-1/PD-L1-IN-15 is a potent inhibitor of PD-1/PD-L1 (IC50: 60.1 nM) and has shown investigational potential for tumor immunotherapy.</p>

<p>MA242 free base is a dual MDM2/NFAT1 inhibitor that triggers apoptosis in pancreatic cancer cells.</p>

<p>eIF4A3-IN-6 is a potent eIF4A inhibitor, potentially used for treating eIF4A-related diseases like cancer. (US20170145026A1)</p>

<p>Belotecan (CKD-602) inhibits DNA topoisomerase I, blocks cell cycle, induces apoptosis, and is a camptothecin-derived anticancer agent.</p>

<p>RSK-IN-2 (Compound 3e) is an inhibitor of RSK, showing IC50 values of 37.89 nM for RSK2, 30.78 nM for RSK1, 20.51 nM for RSK3, and 91.28 nM for RSK4. It suppresses tumor cell proliferation, induces apoptosis, and causes cell cycle arrest at the G2/M phase.</p>

<p>KDM1/CDK1-IN-1 inhibits KDM1 (IC50: 0.096 μM) &amp; CDK1 (IC50: 0.078 μM), blocks HOP-92 G2/M phase, induces apoptosis, toxic to cancer cells.</p>

<p>PROTAC FKBP Degrader-3, with FKBP and VHL binding groups linked, is a potent FKBP degrader.</p>

<p>AK 295, also known as CX 295, is a dipeptide inhibitor of alpha-ketoamide calpain.</p>

<p>XPO1-IN-1: an oral MM.1S cell inhibitor (IC50: 24 nM), induces apoptosis, stable metabolism, good pharmacokinetics.</p>

<p>Anticancer agent 14: a potent breast cancer inhibitor; induces cell death, disrupts mito. membrane potential (IC50: 0.20-0.65 μM).</p>

<p>TNF-α-IN-12, a TNF-α inhibitor with an IC50 of 0.1 μM, can reduce TNF-α blood levels [1].</p>

<p>RIPK1-IN-28 (compound 13) is an orally active inhibitor of RIPK1. It exhibits inhibitory effects on human I2.1 and Hepa1-6 cells, with IC50 values of 0.4 and 1.2 nM, respectively.</p>

<p>NLRP3-IN-28 (compound N77) serves as a potent inhibitor of NLRP3, effectively blocking Nigericin-induced pyroptosis with an EC50 of 0.07μM. Additionally, it mitigates inflammatory reactions in vivo [1].</p>

<p>Lepidozin G blocks cancer growth (IC50=4.2-5.7μM) and triggers apoptosis in PC-3 cells via mitochondria.</p>

<p>GGTI-2154 hydrochloride: selective GGTase I inhibitor, IC50 21 nM, used in cancer research.</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>JAK-2-/3-IN-3 (ST4j) is a potent JAK2/3 inhibitor for leukemia research, with IC50s: JAK2, 13 nM; JAK3, 14.86 nM; induces apoptosis.</p>

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

<p>Spliceostatin A is an anticancer agent and splicing inhibitor that induces apoptosis by inducing cell cycle arrest in the G1 and G2/M phases.</p>

<p>ASP9831 is an orally active PDE4 inhibitor. It suppresses LPS-induced TNF-α production and exhibits anti-inflammatory properties. ASP9831 is useful in the study of steatohepatitis.</p>

<p>Silvestrol is a eukaryotic translation initiation factor 4A inhibitor. Silvestrol causes autophagy and caspase-mediated apoptosis.</p>

<p>CDK4/6-IN-10: Oral CDK4 (IC50: 22 nM) &amp; CDK6 (IC50: 10 nM) inhibitor with anti-cancer potential for MM research.</p>

<p>Multi-kinase-IN-1, a powerful kinase inhibitor, exhibits antitumor properties by inducing cell apoptosis.</p>

<p>WYJ-2, a selective agonist for toll-like receptor 2/1 (TLR2/1), demonstrates an EC50 of 18.57 nM in HEK 293T cells transiently co-transfected with human TLR2 and TLR1. It induces pyroptosis and has shown anticancer activity against non-small cell lung cancer (NSCLC) [1].</p>

<p>microRNA-21-IN-1: microRNA inhibitor, curbs HeLa/HCT-116 growth (IC50: 5.5/2.8 μM), induces HeLa apoptosis, elevates PTEN/EGR1/SLIT2, for cancer research.</p>

<p>TBC-1 is a chlorophyll-a derivative that acts as a photosensitizer for photodynamic therapy (PDT). It efficiently generates type I ROS and targets the endoplasmic reticulum. TBC-1 demonstrates in vitro biocompatibility and PDT effectiveness under both normoxic and hypoxic conditions.</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>JH-XVII-10: potent, oral DYRK1A/B inhibitor (IC50: 3/5 nM), shows antitumor activity in HNSCC.</p>

<p>FLT3/TrKA-IN-1: Potent dual kinase inhibitor for FLT3 &amp; TrKA, promising for AML research.</p>

<p>VEGFR-IN-3 inhibits cancer cell growth (OVCAR-4, MDA-MB-468) with IC50s: 0.29, 0.35μM. Used in cancer research.</p>

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

<p>PARP/NAMPT-IN-1 (Compound 13j) is a dual-target inhibitor of PARP and NAMPT, with IC50 values of 0.8 nM for PARP1 and 18 nM for NAMPT. It suppresses breast cancer cell proliferation and migration, inducing apoptosis. PARP/NAMPT-IN-1 is applicable for research on triple-negative breast cancer.</p>

<p>PARP1-IN-12: potent PARP1 inhibitor, IC50 2.99 nM, triggers cell apoptosis, G2/M arrest, induces DSBs in BRCA-deficient cells.</p>

<p>D-Cl-amidine hydrochloride is a potent and highly selective inhibitor of PAD1. It exhibits excellent tolerance and does not induce significant toxicity [1].</p>

<p>Anticancer agent 53 exhibits potent in vitro cytotoxicity, triggers apoptosis, halts S/G2/M cycle, and has antitumor effects without toxicity.</p>

<p>NiCur is an effective and selective inhibitor of CBP histone acetyltransferase (HAT), with an IC50 of 0.35 μM.</p>

<p>MJC13 is an FKBP52-targeting agent with antitumor activity, suitable for prostate cancer research.</p>

<p>HDAC6/HSP90-IN-2, a cancer research chemical, inhibits HDAC6 &amp; Hsp90 with IC50s of 105.7 &amp; 61 nM.</p>

<p>Enpp-1-IN-25 (Compound 30) is an ENPP1 inhibitor with an IC50 of 8.05 nM and exhibits low oral bioavailability. By inhibiting cGAMP degradation, it effectively activates the intracellular STING pathway. Enpp-1-IN-25 can enhance immune cell infiltration and type I interferon response in the tumor microenvironment, thereby increasing the antitumor efficacy of anti-PD-L1 antibodies. It is applicable for research in cancer immunotherapy.</p>

<p>BRD1991 is a chemical compound that specifically disrupts the interaction between Beclin 1 and Bcl-2, thereby inducing autophagy.</p>

<p>Flizasertib is a serine/threonine kinase inhibitor that acts by inhibiting RIPK1, which has anti-inflammatory and therapeutic effects on immune disorders.</p>

<p>PF-07328948 is a branched-chain keto-acid dehydrogenase kinase (BDK) inhibitor, useful for studying CVD metabolic disorders.</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>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>Tuvusertib (M1774), an oral ATR inhibitor (Ki&lt;1µM), selectively blocks CHK1 phosphorylation, disrupts DNA repair, and induces tumor cell apoptosis.</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>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>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>BCL6-IN-3: potent BCL6 inhibitor, 70 nM GI50 in SU-DHL4, affects cell functions, antitumor.</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>WEHI-539 hydrochloride is a selective Bcl-XL inhibitor with an IC50 of 1.1 nM.</p>

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

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

<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>

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>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>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>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>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>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>Imifoplatin (PT-112) is a platinum compound with antitumor activity and may be used to study prostate cancer and immune system disorders.</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>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>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>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>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>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>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>ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.</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>RRD-251 is an Rb-Raf-1 interaction inhibitor that induces apoptosis in metastatic melanoma cells and synergizes with dacarbazine[1].</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>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-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>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>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>

<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>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>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>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>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>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>