Apoptose

<p>TLBC, a borane-chalcone derivative, exhibits dose-dependent inhibitory effects across various glioma cell lines with IC50 values ranging from 5.5 to 25.5 μM. TLBC induces apoptosis independently of alterations in the tumor suppressor factor p53.</p>

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

<p>DNMT1-IN-5 (Compound 55) is an inhibitor of DNMT, specifically targeting DNMT1 and DNMT3A, with IC50 values of 2.42 μM and 14.4 μM, respectively. It demonstrates antiproliferative effects across various cancer cell lines (TMD-8, DOHH2, MOLM-13, THP-1, RPIM-8226, and HCT116) with IC50 values ranging from 0.19 to 2.37 μM. The compound induces G2/M phase cell cycle arrest and apoptosis in TMD-8 and DOHH2 cells. Additionally, DNMT1-IN-5 exhibits antitumor efficacy in a TMD-8 xenograft mouse model.</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>FTO-IN-13 (compound 8t) is a potent FTO inhibitor with antiproliferative properties. It induces apoptosis (cell apoptosis) and reduces the expression of Bcl-2 and Caspase 3 active proteins. Additionally, FTO-IN-13 lowers the expression of MYC and CEBPA genes and demonstrates anticancer activity.</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>Mcl-1 inhibitor22 (Example 36) is an MCL-1 inhibitor that suppresses its anti-apoptotic function by blocking the interaction between MCL-1 and pro-apoptotic proteins. It exhibits antiproliferative activity against various cancer cell lines and can be utilized for cancer research.</p>

<p>RIP1 kinase inhibitor 1 is an orally available and brain-penetrating inhibitor of RIP1 kinase with pKi of 9.04.</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>TI17 is a selective TRIP13 inhibitor with anticancer activity and inhibits proliferation of multiple myeloma (MM) cells</p>

<p>Ganoderic acid R: potent anticancer, induces apoptosis, cytotoxic to MDR and sensitive tumor cells.</p>

<p>GL0388, a Bax activator, induces apoptosis, hinders breast cancer growth, and has IC50 of 0.299-1.57 μM.</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>Anticancer agent 65: Effective on A549 cells, IC50 1.07 μM, halts S phase, triggers apoptosis, elevates p53/p21, causes ROS and MMP collapse.</p>

<p>CCT369260 (compound 1), an orally active inhibitor targeting B-cell lymphoma 6 (BCL6), demonstrates anti-tumor efficacy with an IC50 value of 520 nM [1].</p>

<p>RET-IN-11 selectively inhibits RET (IC50: 6.20 nM), promotes apoptosis, and hinders cell proliferation and migration.</p>

<p>EGFR-IN-45: Strong EGFR/CDK2 inhibitor (IC50s: 0.4 &amp; 1.6 μM), halts cancer cell cycle pre-G1, prompts apoptosis, also targets Topo I/II.</p>

<p>Ph-Ph+ is a dimerized phenanthroline derivative with antitumor, antibacterial, and antifungal effects.</p>

<p>Microtubule inhibitor 2: potent, selective, oral, induces ferroptosis, strong antitumor effect.</p>

<p>p53 Stabilizer 2 (Compound 17a16) is a p53 stabilizing agent. It can induce S-phase arrest and apoptosis in both p53-functional and p53-deficient cancer cells. Additionally, p53 Stabilizer 2 triggers mitochondrial stress and activates two immune checkpoint pathways: NA-PKcs dependent p53 stabilization and the ATR-Chk1 axis activation. It also inhibits tumor growth in p53-deficient xenograft models.</p>

<p>ERK-MYD88 Interaction Inhibitor 1, an agent that disrupts the interaction between ERK and MYD88, has demonstrated the ability to trigger an HRI-mediated integrated stress response (ISR) that specifically promotes immunogenic cell apoptosis (apoptosis) in cancer cells. Additionally, in models using Lewis lung cancer mice, this compound has been shown to stimulate anti-tumor T cell responses, thereby exhibiting significant anti-tumor activity.</p>

<p>GGTI-2154 hydrochloride: selective GGTase I inhibitor, IC50 21 nM, used in cancer research.</p>

<p>MC3629, an inhibitor of the histone methyltransferase (EZH2), exhibits antitumor activity. This compound effectively inhibits the proliferation and self-renewal of SHH MB cancer cells while inducing cell apoptosis (apoptosis). MC3629 is also useful in research on tumor aggressiveness and resistance.</p>

<p>β-Carotene-13C10 (Provitamin A-13C10) is a form of β-Carotene labeled with 13C. It is a carotenoid compound and serves as a natural precursor to vitamin A. This compound acts as a regulator of reactive oxygen species (ROS), exhibiting both antioxidant and anti-inflammatory properties. Depending on its intrinsic characteristics and the redox potential of the biological environment, β-Carotene can function either as an antioxidant or a pro-oxidant. It also possesses anticancer activity, inducing apoptosis in breast cancer cells.</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>EGFR-IN-62: IC50 of 10-242 nM for various EGFR mutations, blocks A549/H1975 cell cycle, induces apoptosis, and inhibits cell motility and proliferation.</p>

<p>Microtubule stabilizer; halts cancer cell growth (IC50: 3-30 nM); arrests cells in prometaphase; prevents bipolar spindle formation.</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>eIF4A3-IN-6 is a potent eIF4A inhibitor, potentially used for treating eIF4A-related diseases like cancer. (US20170145026A1)</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>PD-L1-IN-1, potent PD-L1 inhibitor with 115 nM IC50, suppresses tumors, boosts immune response, and spares healthy cells.</p>

<p>06:0 PE (PE(6:0/6:0)) is a water-soluble phospholipid characterized by its short acyl chains. It possesses notable antitumor activity and can inhibit tumor progression in the body. Additionally, it exhibits antiproliferative and pro-apoptotic properties, and serves as a precursor for phosphatidylcholine and phosphatidylethanolamine.</p>

<p>PAK4-IN-5 (Compound 12i) is a potent inhibitor of PAK4 (IC50: PAK4 at 7.68 nM, PAK1 at 1872.01 nM) that forms stable interactions with the PAK4 enzyme. This compound effectively inhibits the proliferation and migration potential of MDA-MB-231 cells by hindering the phosphorylation of PAK4 and LIMK1. Additionally, PAK4-IN-5 arrests the cell cycle in the G0/G1 phase, induces apoptosis, and prompts the production of reactive oxygen species. The LD50 in mice is greater than 500 mg/kg (oral).</p>

<p>ASK1-IN-7 (Compound 4c) is an ASK1 inhibitor and a derivative of the ASK1 inhibitor scaffold 5-(5-Phenyl-furan-2-ylmethylene)-2-thioxo-thiazolidin-4-one. This compound is potentially applicable in research involving ASK1 signaling pathways, including studies on cellular stress response, inflammatory response, neurodegenerative diseases, and cardiovascular diseases.</p>

<p>FKBP12 PROTAC dTAG-13 is a PROTAC and selective degrader for target validation by splicing FKBP12 F36V with CRBN and thereby degrading FKBP12 F36V.</p>

<p>L5-DA, a G-quadruplex ligand, stabilizes G4s in HeLa cells, induces apoptosis, and is cytotoxic with an IC50 of 4.3 μM.</p>

<p>RET-IN-7 exhibits strong inhibitory effects against RET kinase in vitro and shows significant efficacy in treating RET-driven tumor xenografts in mice through</p>

<p>Compound 28 is a nonsteroidal VDR agonist with 690 nM potency, inducing cell cycle arrest and apoptosis in MCF-7 cells.</p>

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

<p>TRPM7-IN-1 (compound SUD) is a benzamide-urea derivative and an effective inhibitor of TRPM7. This compound induces cell cycle arrest and apoptosis in MCF-7 and BGC-823 cells, reducing their migration capabilities. It decreases vimentin expression while increasing E-cadherin expression. TRPM7-IN-1 reduces TRPM7-like currents and inhibits TRPM7 expression by activating the PI3K/Akt signaling pathway. This compound shows potential as a therapeutic agent for reducing breast and gastric cancer metastasis by targeting TRPM7 expression and activity.</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>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>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>Tandutinib (MLN518) sulfate is an effective and selective inhibitor of FLT3, with an IC50 value of 0.22 μM. It also inhibits c-Kit and PDGFR, displaying IC50 values of 0.17 μM and 0.20 μM respectively. This compound can be utilized in the treatment of acute myeloid leukemia and has the capability to cross the blood-brain barrier.</p>

NDs-IN-1 (Compound 3g) is a novel non-covalent multi-target inhibitor that inhibits the activities of key enzymes such as hBACE-1, hAChE, and hMAO-B, and is primarily used in the study of neurodegenerative diseases [1].

<p>STAT3-IN-9 hinders STAT3 at Tyr705, doesn't affect STAT1 Tyr701, induces apoptosis, and arrests cells in G2/M phase.</p>

A signal-specific JNK/p38 pathway and TAK 1 inhibitor

<p>FAK-IN-2: potent oral FAK inhibitor, IC50 35 nM, reduces tumor growth, migration, and induces cell death.</p>

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

<p>VNPP433-3β acts as a molecular glue degrader, targeting the androgen receptor (AR) and its splice variants (AR-Vs) as well as MAP kinase-interacting serine/threonine protein kinase Mnk1/2. It effectively inhibits the proliferation of cancer cells LNCaP, C4-2B, and CWR22Rv1, with GI50 values of 0.2, 0.3, and 0.31 μM, respectively. Additionally, VNPP433-3β shows favorable pharmacokinetics in CD-1 mice and suppresses tumor growth in the CWR22Rv1 xenograft mouse model.</p>

Antitumor Agent-184 (compound 12aa) triggers apoptosis in various cell lines, exhibiting IC50 values of 2.35 μM in B16-F10 cells, 7.32 μM in 4T1 cells, and 10.31 μM in CT26 cells.

<p>NSD2-IN-1: potent, selective NSD2-PWWP1 inhibitor, IC50 0.11 μM, induces gene expression changes, apoptosis, cell cycle arrest.</p>

<p>PD-1/PD-L1-IN-17 (Compound P20) is a potent PD-1/PD-L1 inhibitor (IC50: 26.8 nM).</p>

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

<p>SSB-2548 is a CXCR-4 inhibitor that suppresses the proliferation and migration of acute myeloid leukemia cells and induces apoptosis (apoptosis). It is well absorbed in the gastrointestinal tract and can be used for leukemia research.</p>

<p>TZEP7 functions as an EGFR kinase inhibitor in cancer cells. It exhibits cytotoxicity and induces apoptosis within these cells. TZEP7 downregulates the anti-apoptotic protein Bcl-2, upregulates the pro-apoptotic protein Bax, and increases caspase levels. This compound holds potential for research in anticancer drug development.</p>

<p>TrxR/EGFR-IN-1 (Compound L1Au2) is a TrxR/EGFR inhibitor with activity against both gefitinib-sensitive and -resistant lung cancer, effectively suppressing tumor proliferation and promoting apoptosis. It enhances GPX4 degradation through autophagosome-lysosome and proteasome pathways, leading to ferroptosis. Additionally, it induces endoplasmic reticulum stress and triggers immunogenic cell death, making it applicable for studies on gefitinib-resistant lung cancer.</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>

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

<p>Anticancer agent 44 induces apoptosis, is selective, cytotoxic to cancer cells, and minimally toxic to human lymphocytes.</p>

<p>Mcl-1 inhibitor21 (Example 1-36) is an Mcl-1 inhibitor with an IC50 of 328 nM. It exhibits pro-apoptotic and anti-proliferative activity against SUDHL5 and SUDHL10 cell lines, making it applicable for cancer research.</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>Top/HDAC-IN-1: Dual Top/HDAC inhibitor, potent against HDAC1-3,6,8 and HCT116 cells; blocks G2 phase, induces apoptosis.</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>WEHI-9625 is a tricyclic sulfone small molecule apoptosis inhibitor (EC50: 69 nM).</p>

<p>CDK-IN-9: A potent CDK inhibitor, gels to enhance CDK12/DDB1 binding, targets CDK2/E (IC50: 4 nM), induces apoptosis via dephosphorylation.</p>

<p>VDX-111, an analog of vitamin D, exhibits cytotoxicity in ovarian cancer cells by upregulating the RIPK1/RIPK3 pathway and inducing necroptosis. It also promotes the expression of cytokines and demonstrates antitumor activity in a mouse model [1].</p>

<p>Antitumor agent-202 is a stabilizer of the p53Y220C mutant, selectively inhibiting the proliferation of tumor cells carrying the p53Y220C mutation. It is applicable for research focused on cancers associated with the p53 Y220C mutation.</p>

<p>RIPK1-IN-24 is an inhibitor of receptor-interacting protein kinase 1 (RIPK1) with an IC50 of 1.3 μM. It is utilized in research on inflammatory diseases.</p>

<p>Mcl-1 Inhibitor 9 (Example 2) is a potent inhibitor of myeloid cell leukemia 1 (Mcl-1), demonstrating anti-tumor activity with an IC50 value of 0.21889 nM.</p>

<p>Tubulin polymerization-IN-61 (Compound 9a), a tubulin polymerization inhibitor, disrupts the microtubule skeleton, arrests the cell cycle at the G2/M phase, induces Apoptosis, and impedes cancer cell migration and colony formation. This compound demonstrates antitumor efficacy in vivo within the 4T1 xenograft model [1].</p>

Topo II/HDAC-IN-1 (7d) demonstrates potent dual inhibitory effects on Topo II and HDAC, while Topo II/HDAC-IN-1 (8d) effectively induces apoptosis [1].

<p>Compound 2c is a potent p38α MAPK inhibitor with antitumor effects, enhancing apoptosis and ROS.</p>

<p>Samuraciclib (CT7001) is a potent oral CDK7 inhibitor (IC50: 41 nM) with anti-breast cancer properties.</p>

<p>Bayer-18 is an inhibitor of TYK2. It inhibits the viability of anaplastic large cell lymphoma cells, including K299, SR786, Mac1, and Mac2a, with an IC50 ranging from 2-3 µM. Additionally, Bayer-18 induces apoptosis in K299 and SR786 cells.</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>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>Bcl-2-IN-7 inhibits Bcl-2, encourages apoptosis in cancer cells, and has anti-tumor activity with various IC50 values.</p>

<p>Tubulin inhibitor 41 (Compd D19) is a promising lead compound for glioblastoma treatment, known for its ability to penetrate the blood-brain barrier (BBB). It functions as a tubulin inhibitor, inducing G2/M phase arrest, leading to cell apoptosis, and inhibiting the migration of U87 cells [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>

HC-5404-Fu is an inhibitor of PERK with anti-tumor activity. This compound inhibits the signaling pathway of the endoplasmic reticulum stress response. Additionally, HC-5404-Fu increases the sensitivity of renal cell carcinoma cells to vascular endothelial growth factor (VEGF) receptor tyrosine kinase inhibitors (TKIs). It holds potential for research into renal cell carcinoma, stomach cancer, metastatic breast cancer, small cell lung cancer, and other solid tumors.

<p>XSJ05, a derivative of camptothecin (CPT), exhibits anti-cancer activity by inhibiting topoisomerase I (Topo I). This compound induces DNA double-strand breaks, leading to DNA damage. Furthermore, XSJ05 stifles the growth of colorectal cancer (CRC), halts the cell cycle in the G2/M phase, and induces apoptosis.</p>

<p>YLL545 is an inhibitor of Vascular Endothelial Growth Factor Receptor 2 (VEGFR2). It inhibits VEGF-induced phosphorylation of VEGFR2 and the activation of downstream signaling mediators (such as phosphorylated STAT3 and phosphorylated ERK1/2) in human umbilical vein endothelial cells (HUVEC). Additionally, YLL545 suppresses HUVEC proliferation, migration, invasion, and angiogenesis. It also induces apoptosis and inhibits tumor growth in a mouse model of breast cancer.</p>

<p>Cernuumolide J (TMJ-105) functions as a JAK2/STAT3 inhibitor and exhibits potent activity against HEL leukemia cells by inhibiting their growth in both time-dependent and concentration-dependent manners, with an IC 50 value of 1.79 μM. This compound effectively induces G2/M phase arrest and apoptosis by downregulating the phosphorylation of JAK2, STAT3, and Erk, while simultaneously upregulating the phosphorylation of JNK and p38 MAPK. Cernuumolide J holds potential for research applications in anti-cancer therapy.</p>

<p>ONC213, an αKGDH inhibitor, functions by hindering αKGDH activity, thus suppressing mitochondrial respiration and elevating α-ketoglutarate levels, ultimately inducing apoptosis (Apoptosis) in AML cells. It is utilized in the study of acute myeloid leukemia.</p>

<p>Mps-BAY1, an MPS1 inhibitor, exhibits anticancer activity. It inhibits cell proliferation and induces cell apoptosis by activating mitotic aberrations in cancer cells, leading to overall aneuploidy and polyploidy. Mps-BAY1 is used in research pertaining to colorectal and cervical cancer.</p>

<p>WK88-1, an inhibitor of Hsp90, effectively induces the degradation of various oncogenic signaling molecules, including EGFR, ErbB2, and ErbB3, in the gefitinib-resistant H1975 cell line. This leads to subsequent growth arrest and apoptosis.</p>

<p>Compound Z15 (ZNU-IMB-Z15) acts as an antagonist and degrader of the androgen receptor (AR). It inhibits the proliferation of castration-resistant prostate cancer (CRPC) cell lines that are AR-positive and induces apoptosis. Compound Z15 exhibits anticancer activity both in vivo and in vitro.</p>

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

<p>TrxR-IN-8 (Compound 6f) is a selective inhibitor of TrxR with an IC50 of 10.2 μM. It induces apoptosis through oxidative stress by stimulating the production of reactive oxygen species, reducing intracellular thiols, and lowering the glutathione/glutathione disulfide ratio. TrxR-IN-8 exhibits significant cytotoxicity against non-small cell lung cancer (NSCLC) cells.</p>

<p>c-Myc inhibitor16 iodide (Compound W11) is a selective inhibitor of the c-MycG-quadruplex (c-MycG4). It suppresses the transcription and translation of the c-Myc gene, disrupts the tumor cell cycle by halting growth at the G0/G1 phase, and activates mitochondrial apoptotic pathways, leading to early apoptosis in cancer cells. This compound shows potential for research in breast cancer.</p>

<p>PARP10/15-IN-2 (Compound 8h) blocks PARP10/15, has IC50s: 0.15μM/0.37μM, cell-permeable, prevents apoptosis.</p>

<p>Soquelitinib (CPI-818) is a selective ITK inhibitor， inhibits tumor growth,T-cell, up-regulatCXCR3, IFNγ, TNFα, and CD107a expression in normal CD8 cells.</p>

Etalocib (LY293111) sodium is an orally active leukotriene B4 (LTB4) receptor antagonist with a Ki value of 25 nM for inhibiting [3H]LTB4 binding. It exhibits an IC50 of 20 nM against LTB4-induced calcium mobilization. Additionally, Etalocib sodium can induce apoptosis.

<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>ZLHQ-5f inhibits CDK2/Topo I, with IC50 of 0.145μM for CDK2/CycA2, and promotes apoptosis by arresting HCT116 cells in S phase.</p>

<p>RIPK1-IN-14 inhibits RIPK1 with 92 nM IC50 and reduces necrotic apoptosis in U937 cells.</p>

<p>Bcl-2-IN-3 (Compound 10) is an inhibitor of Bcl-2, utilized in cancer research.</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>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>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>AK 295, also known as CX 295, is a dipeptide inhibitor of alpha-ketoamide calpain.</p>

<p>Antitumor agent-76 is a water-soluble, orally active, rapid-release prodrug of Triptolide that exhibits anticancer effects.</p>

<p>Casuarinin, an ellagitannin found in pomegranates and certain Casuarina/Stachyurus plants, is a carbonic anhydrase inhibitor and astringent.</p>