Apoptosis

<p>GGTI298 is a potent GGTase I inhibitor; IC50 3μM for Rap1A, &gt;20μM for Ha-Ras.</p>

<p>Top/HDAC-IN-2 (45b) is a dual inhibitor of Top and HDAC that induces apoptosis and exhibits significant anti-tumour effects.</p>

<p>MA242 is a nuclear factor of activated T cells 1 (NFAT1) for Pancreatic Cancer Therapy and dual inhibitor of murine double minute 2 (MDM2).</p>

<p>Tubulin polymerization-IN-4: inhibits tubulin (IC50=4.6 μM), blocks G2/M phase, induces apoptosis, hinders cell cloning/migration, damages vasculature.</p>

<p>N-ω-chloroacetyl-L-ornithine (NCAO) serves as a powerful reversible competitive inhibitor of ornithine decarboxylase (ODC), displaying cytotoxic and antiproliferative properties against various tumor cell lines, with EC50 values spanning from 1 to 50.6 µM. In vitro studies reveal that NCAO promotes Apoptosis and restricts tumor cell migration. Additionally, it demonstrates significant antitumor efficacy in a mouse model, targeting both solid and ascitic tumors using the myeloma (Ag8) cell line. NCAO holds promise in the development of antitumor agents.</p>

<p>Compound 5a, an anticancer agent, enhances P53 and has antiproliferative effects.</p>

<p>PARP1/BRD4-IN-2, a potent inhibitor of PARP1 and BRD4, halts cell cycle, triggers apoptosis, and has antitumor effects on TNBC.</p>

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

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

<p>ZLMT-12: tacrine derivative, inhibits CDK2/CDK9, weak on AChE/BuChE, anti-proliferative, low toxicity, blocks S/G2/M phase, induces apoptosis.</p>

<p>HER2-IN-10 is a psoralen derivative that induces apoptosis. HER2-IN-10 shows anti-breast cancer activity and light-activated cytotoxicity [1].</p>

<p>JAK2/FLT3-IN-1 (TFA), an oral JAK2/FLT3 inhibitor, shows anticancer properties; IC50: JAK2 (0.7 nM), FLT3 (4 nM), JAK1 (26 nM), JAK3 (39 nM).</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>HDAC-IN-37 inhibits HDACs 1, 3, 8, &amp; 6, induces histone acetylation, halts G1 to S phase, and triggers early apoptosis.</p>

<p>PD-1/PD-L1-IN-16 is a potent inhibitor of PD-1/PD-L1 (IC50: 53.2 nM) and has shown research potential for tumour immunotherapy.</p>

<p>D18: Dual agonist for TLR7/8, boosts PD-L1, aids tumor sensitivity to PD-1/PD-L1 inhibitors, and is a cytotoxin for ADC HE-S2.</p>

<p>Antitumor agent-43 (Compound 4B) is a potent antitumor agent that induces cell cycle arrest at G2/M phase.</p>

<p>Verrucarin A, a mycotoxin from Myrothecium verrucaria, inhibits protein synthesis, leukemia growth, and triggers apoptosis.</p>

<p>Antitumor agent-77 suppresses cancer cell growth, migration, induces apoptosis, and hinders EMT.</p>

<p>HER2-IN-11 is a psoralen derivative that induces apoptosis. HER2-IN-11 shows light-activated cytotoxicity and also exhibits anti-breast cancer activity [1].</p>

<p>eIF4E-IN-4 (Compound 33) is a selective inhibitor of the eukaryotic initiation factor 4E (eIF4E) with a biochemical activity value of 95 nM. It inhibits cap-dependent mRNA translation with an IC50 of 2.5 μM and is applicable in research on breast cancer, colon cancer, and head and neck cancer.</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-134 (compound 3f) is a triazolo[3,4-a]quinoline derivative and functions as a potent EGFR inhibitor with an IC50 of 0.023 µM. It induces apoptosis and necrosis in cells, and causes cell cycle arrest in the G2/M and pre-G1 phases. EGFR-IN-134 modulates the expression of apoptosis-regulating proteins by downregulating anti-apoptotic protein Bcl2 and upregulating pro-apoptotic proteins p53, Bax, and caspases 3, 8, and 9, demonstrating significant antiproliferative and anticancer activities.</p>

<p>3′-Hydroxyflavanone is a cyclized flavonoid with anti-tumor properties that induces apoptosis in HeLa cells.</p>

<p>Oxamic acid is an inhibitor of LDH-A and exhibits antitumor activity. It demonstrates antiproliferative effects on cancer cells and can induce apoptosis.</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>CB-184 is a selective ligand for sigma-2 (σ2) receptors, with Ki values of 7436 nM for sigma-1 (σ1) and 13.4 nM for sigma-2 (σ2), and it promotes apoptosis with antitumor activity.</p>

<p>Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.</p>

<p>Silvestrol is a eukaryotic translation initiation factor 4A inhibitor. Silvestrol causes autophagy and caspase-mediated apoptosis.</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>PROTAC FKBP Degrader-3, with FKBP and VHL binding groups linked, is a potent FKBP degrader.</p>

<p>TNF-α-IN-2 is orally active TNFα inhibitor that distorts the TNFα trimer, causing abnormal signal transduction when it binds to TNFR1, rheumatoid arthritis.</p>

<p>NSC308848 is an effective apoptosis (cell death) inducer that operates in a Myc-dependent manner. It acts by inhibiting Myc transactivation and disrupting the DNA binding activity of Myc family proteins.</p>

<p>MLKL-IN-6 (compound P28) is a mixed lineage kinase inhibitor that specifically targets the Mixed Lineage Kinase domain-like (MLKL) protein.</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>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>

Z-VA-DL-D-FMK (Z-VA-DL-D(OH)-FMK) acts as an inhibitor of caspases. It irreversibly binds to caspases, enhancing the sensitivity to TNF-α and stimulating HIV replication in infected T cells ACH-2.

<p>TH-6, a potent HDAC inhibitor (IC50: HDAC1-0.115, 2-0.135, 3-0.242, 6-0.138, 8-2.120 μM), blocks cell migration, invasion, and has anti-tumor properties.</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>TNF-α-IN-14, a potent TNFα inhibitor, exhibits a selective inhibition profile with an IC50 of 1.1 µM and demonstrates antiinflammatory properties (WO2001072735A2; compound 12) [1].</p>

<p>Pim-1 Kinase Inhibitor 10 (compound 13a) acts as both a competitive and non-competitive inhibitor of PIM-1/2 kinase, promoting cell apoptosis and displaying anticancer properties. Additionally, this compound triggers the activation of caspase 3/7 [1].</p>

<p>CIL-102 is an apoptosis inducer that functions as an MMP-2/MMP-9 inhibitor, effectively reducing both the protein expression and mRNA levels of MMP-2/MMP-9. CIL-102 also demonstrates anticancer activity.</p>

<p>Metamizole (Dipyrone) hemimagnesium is an anti-inflammatory and antioxidant compound known for its ability to reduce fever. It decreases levels of C-reactive protein (CRP) and interleukin 6 (IL-6). Additionally, Metamizole hemimagnesium acts as an orally active cyclooxygenase (COX) inhibitor, suppressing cell proliferation and promoting apoptosis. It is utilized in the study of inflammation and fever.</p>

<p>Potent oral XIAP/cIAP1 inhibitor with EC50s: XIAP 5.1 nM, cIAP1 0.32 nM; curbs tumor growth in vivo.</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>BCL6-IN-3: potent BCL6 inhibitor, 70 nM GI50 in SU-DHL4, affects cell functions, antitumor.</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>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>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>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>Lometrexol (LY 264618) is an antifolate that inhibits GARFT, blocks purine synthesis, induces apoptosis, and has anticancer properties.</p>

<p>Zotatifin (eFT226) is a selective eIF4A inhibitor with antiviral and antitumor properties, inhibiting Sox4 translation and inducing apoptosis.</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>PF-07328948 is a branched-chain keto-acid dehydrogenase kinase (BDK) inhibitor, useful for studying CVD metabolic disorders.</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>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>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>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>AP1867-3-(aminoethoxy) is a synthetic ligand for FKBP and can be used in the synthesis of PROTAC FKBP12 F36V degrader.</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>(R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an inhibitor of P-Glycoprotein.</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>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>ENMD-2076 is an orally active kinase inhibitor. It also has antiangiogenic and antiproliferative mechanisms of action.</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>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>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>Imifoplatin (PT-112) is a platinum compound with antitumor activity and may be used to study prostate cancer and immune system disorders.</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>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>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>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>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>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>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>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>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>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>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>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>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>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>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>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>