Apoptose

<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>HSP90-IN-10 is a potent HSP90 inhibitor, targeting HCC1954 cells (IC50: 6 μM) and inducing apoptosis, sparing normal cells.</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>WEHI-539 is a selective Bcl-XL inhibitor (IC50: 1.1 nM).</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>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>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>Tubulin inhibitor 13 (E27), IC50 16.1 μM, blocks tubulin polymerization, cancer cell migration, and invasion, induces apoptosis.</p>

<p>Microtubule stabilizer; halts cancer cell growth (IC50: 3-30 nM); arrests cells in prometaphase; prevents bipolar spindle formation.</p>

<p>HDAC-IN-9, a dual tubulin/HDAC inhibitor, impedes A549 cell invasion/migration and shows strong anti-tumor/angiogenic effects.</p>

<p>MNK1/2-IN-6: Strong, selective MNK1/2 inhibitor; IC50s: MNK1 at 2.3 nM, MNK2 at 3.4 nM; triggers dose-dependent apoptosis.</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>Coumarin 9a: Selective inhibitor of hCA IX/XII (Ki 93.3/85.7 nM), blocks cancer cell growth, and induces apoptosis.</p>

<p>RET-IN-1 is a RET kinase inhibitor (IC50s: 1 nM, 7 nM, and 101 nM for RET (WT), RET (V804M) , and RET (G810R), respectively).</p>

<p>Scytonemin, a cyanobacterial pigment, inhibits cancer cell growth by decreasing Plk1 activity, especially effective on U266 myeloma cells.</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>AK 295, also known as CX 295, is a dipeptide inhibitor of alpha-ketoamide calpain.</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>FAK-IN-4 (Compound 7d) has anticancer activities that can induce cell apoptosis. FAK-IN-4 is potential inhibitor of FAK [1].</p>

<p>Lonitoclax is an inhibitor of B-cell lymphoma 2 (Bcl-2). It demonstrates antitumor activity in B-cell and myeloid malignancy models comparable to Venetoclax. Lonitoclax holds potential for research in relapsed or refractory chronic lymphocytic leukemia (CLL), small lymphocytic lymphoma, and certain low-grade lymphomas.</p>

<p>SM-433 hydrochloride, a Smac mimetic &amp; IAP inhibitor, binds XIAP BIR3; potent IC50 &lt;1 μM. (Patent WO2008128171A2)</p>

<p>Keap1-Nrf2-IN-4 hinders MGC-803 cell growth (IC50=2.55μM), migration, and induces apoptosis with low toxicity.</p>

<p>NVP-CGM097 sulfate is a potent and selective inhibitor of MDM2 (hMDM2, IC50 of 1.7±0.1 nM).</p>

<p>HDAC-IN-81 (Compound 11g) is an HDAC inhibitor capable of effectively inhibiting HDAC1 with an IC50 value of 4.5 nM. Additionally, it exhibits anticancer activity by inhibiting cell proliferation and can induce cell apoptosis (apoptosis).</p>

<p>TP-030-2 is a RIPK1 inhibitor (human K i =0.43 nM ; mouse IC 50 =100 nM) .</p>

<p>BRD-K20733377 is a Bcl-2 inhibitor that exhibits selective cytotoxicity toward senescent cells, specifically inhibiting the activity of etoposide-induced senescent IMR-90 cells with an IC50 of 10.7 μM. Additionally, BRD-K20733377 reduces the mRNA expression of aging-related genes p16, p21, and KI67 in aged mouse models.</p>

<p>BRD-K44839765 selectively targets Bcl-2, exhibiting an IC50 of 5.6 μM in IMR-90 cells. This compound is also orally active.</p>

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

<p>BTK-IN-7 is a potent inhibitor for BTK with 4.0 nM IC50, highly selective over ITK and EGFR, showing strong antitumor activity.</p>

<p>NTU281 inhibits transglutaminase-2, lowers creatinine in diabetic rats, reduces proteinuria, and fights glomerulosclerosis.</p>

<p>PI3K-IN-35 (6l) selectively inhibits PI3K-α, β, δ (IC50: 13.98, 7.22, 10.94 μM), blocks G2/M phase, induces apoptosis, and is useful in leukemia research.</p>

<p>Anticancer agent 44 induces apoptosis, is selective, cytotoxic to cancer cells, and minimally toxic to human lymphocytes.</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>YL-1-9 is an inhibitor that prevents the degradation of p53 by MDM2 through tight binding to the crucial hydrophobic pocket of MDM2. It can induce cell cycle arrest and apoptosis in breast cancer cells [1].</p>

<p>FLT3-ITD-IN-3 (13v) is an orally active inhibitor of FLT3-ITD (internal tandem duplication of FLT3), which works by blocking FLT3 signaling. This inhibition leads to cell cycle arrest in the G0/G1 phase and induces apoptosis. The compound is currently employed in studies related to acute myeloid leukemia (AML).</p>

<p>HDAC-IN-27 dihydrochloride (Compound 11h) is a potent, orally active, HDACI class-selective inhibitor, with IC50 values ranging from 0.43 to 3.01 nM for HDAC1-3. This compound exhibits both in vivo and in vitro anticancer activity. HDAC-IN-27 shows significant antiproliferative effects against acute myeloid leukemia (AML) cell lines by inducing apoptosis and histone acetylation (AcHH3 and AcHH4). It is useful for research on acute myeloid leukemia (AML).</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>

<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>RIP1 kinase inhibitor 1 is an orally available and brain-penetrating inhibitor of RIP1 kinase with pKi of 9.04.</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>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>(S)-Purvalanol B is the S enantiomer of Purvalanol B. Purvalanol B is an inhibitor of cyclin-dependent kinase(CDK) .</p>

<p>(S)-JDQ-443, an isomer of JDQ-443, is a selective, potent oral KRAS G12C inhibitor with antitumor properties.</p>

<p>3-AP-Me is the dimethyl derivative of the ribonucleotide reductase inhibitor 3-AP (SML0568). It activates the endoplasmic reticulum (ER) stress pathway by promoting eIF2α phosphorylation and upregulating gene expression of transcription factors ATF4 and ATF6, thereby inducing apoptosis. Additionally, 3-AP-Me activates cellular stress kinases c-Jun N-terminal kinase (JNK) and p38 mitogen-activated protein kinase, leading to the upregulation of spliced mRNA variant XBP1. It is applicable in cancer research.</p>

<p>Tubulin-IN-9 inhibits tubulin (IC50: 1.82 μM), halts K562 cells in G2/M, induces apoptosis, and has anti-cancer 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>PSF-IN-2 (Compound (C)-30) is a PSF inhibitor with an IC50 value of 0.005 pM. It exhibits anticancer properties, inhibiting the proliferation of 22Rv1 cells with an IC50 value of 0.5 μM. PSF-IN-2 activates the p53 signaling pathway by disrupting PSF-RNA binding, inducing expression of related genes, promoting apoptosis, and inhibiting the cell cycle. This compound is applicable in cancer research.</p>

<p>NLRP3-IN-78 (compound 21) is an NLRP3 inhibitor with a 46.72% inhibition rate of GSDMD-induced pyroptosis at 5 μM. It binds to the NLRP3 protein and prevents GSDMD-NT oligomerization. Additionally, NLRP3-IN-78 inhibits GSDMD cleavage and upstream NF-κB signaling, demonstrating anti-inflammatory activity.</p>

<p>RIP3 Activator 1 (compound C8) is an effective RIP3 activator that inhibits cell growth and induces necroptotic cell death (necroptosis) and autophagy through the RIP3/p62/Keap1 signaling pathway. Additionally, this compound enhances the expression of p-MLKL and promotes the accumulation of LC3-II and p62 proteins.</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>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>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>HC-7366 (GCN2 modulator-1) is an orally active GCN2 kinase activator with antitumor activity, inducing tumor growth inhibition.</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>DX3-234 is a OXPHOS inhibitor that acts by inhibiting complex I in the mitochondrial ETC,for cancers dependent on aerobic metabolism, such as pancreatic cancer.</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>Compound W10 is a dual inhibitor of Topo I (IC50: 0.90μM) and COX-2 (IC50: 2.31μM), inducing cancer cell apoptosis via mitochondria.</p>

<p>ZB-R-55 is an oral and highly potent bimodal RIPK1 inhibitor with excellent kinase selectivity in lps-induced sepsis models for the study of SIRS and sepsis.</p>

<p>NF-κB-IN-4 (compound 17) is a potent inhibitor of NF-κB pathway which can cross blood brain barrier (BBB).</p>

<p>OICR12694 (JNJ-65234637) is an orally active inhibitor of B cell lymphoma 6 (BCL6) .</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>Tubulin inhibitor 43 exhibits significant antitumor activity by impeding the proliferation and growth of cancer cells through the inhibition of β-microtubulin activity, ultimately inducing apoptosis [1].</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>hCAIX/XII-IN-1: potent CAIX inhibitor (KI=0.48μM), CAXII (KI=0.83μM), antiproliferative, induces apoptosis in MCF-7 cells.</p>

<p>WEHI-9625 is a tricyclic sulfone small molecule apoptosis inhibitor (EC50: 69 nM).</p>

<p>HR-19011 (Compound 40) is an inducer of eIF2α phosphorylation that increases expression levels of downstream proteins ATF and CHOP,antiproliferative.</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>Urease-IN-20 (compound XBP2) is an inhibitor of Helicobacter pylori (H. pylori), with an IC50 of 0.14 μM for H. pylori inhibition. It effectively decreases apoptosis in GES-1 cells infected with H. pylori and reduces levels of ROS and γH2AX. Urease-IN-20 also demonstrates significant gastric mucosal protective effects, making it suitable for H. pylori research.</p>

<p>PD-1-IN-17 TFA is a potent PD-1 inhibitor, blocking 92% of splenocyte growth at 100 nM.</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>NLRP3-IN-72 (Compound 2) is a benzimidazole derivative. It exhibits anti-inflammatory and antioxidant properties, with an IC50 of 0.3 μM for NLRP3 IL-1β, a PD50 of 0.4 μM for protection against cell pyroptosis, and an EC50 of 0.6 μM for inducing HO-1.</p>

<p>ZIF-8 is an anticancer agent that can inherently trigger pyroptosis through a caspase-1/gasdermin D (GSDMD)-dependent pathway.</p>

<p>CK156 inhibits DAPK with high selectivity; IC50: 182 nM (DRAK1), 34 μM (CK2a1), 39 μM (CK2a2); key in autoimmune/inflammation research.</p>

<p>Apoptosis Inducer 5, a lignan enantiomer extracted from Crataegus pinnatifida, demonstrates cytotoxic properties through inducing apoptosis and autophagy in</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>Casein kinase1δ-IN-29 (Compound 18) is an inhibitor that targets p38α and casein kinase 1 (CK1), exhibiting inhibitory effects on p38α, CK1δ, and CK1ε with IC50 values of 0.041 µM, 0.005 µM, and 0.447 µM, respectively. This compound causes cell cycle arrest at the subG1 phase and induces apoptosis in AC1-M88 cells.</p>

<p>Compound 13, a potent Pim-1 inhibitor, induces apoptosis with potential for cancer research.</p>

<p>DHU-Se1: potent anti-inflammatory, releases reactive selenium from macrophages, inhibits iNOS/TNF-α, blocks M0 to M1 polarization.</p>

<p>Siphonaxanthin is a carotenoid found in green algae, known for targeting the death receptor 5 (DR5) on cancer cells to induce apoptosis. In human leukemia HL-60 cells, it increases DR5 expression, reduces Bcl-2 levels, and activates caspase-3. It also inhibits fibroblast growth factor receptor-1 (FGFR-1) signaling in endothelial cells. Siphonaxanthin suppresses the proliferation, migration, and tubular formation of human umbilical vein endothelial cells (HUVECs), as well as the growth of microvessels in rat aorta rings. Additionally, it has anti-inflammatory properties by blocking the translocation of high-affinity IgE receptors (FcεRI) to lipid rafts in mast cells. Siphonaxanthin shows potential for research into diseases such as cancer, diabetic retinopathy, and rheumatoid arthritis.</p>

<p>Caspase-3-IN-2 (Compound 4d) acts as an inhibitor of α-Chymotrypsin. It also exhibits inhibitory activity against HIV protease and caspase 3, with inhibition rates of 57% and 51% respectively at a concentration of 100 μM.</p>

<p>Ac-DMLD-CMK is a peptide designed to target the caspase3-Gsdme signaling pathway in mice. It specifically inhibits the activation of caspase 3 and Gsdme, preventing the cleavage of Gsdme by caspase 3, which reduces pyroptosis. This process helps alleviate damage to renal tubular epithelial cells and decrease the secretion of inflammatory cytokines. Ac-DMLD-CMK can lower serum creatinine and blood urea nitrogen levels in mice induced by Cisplatin, thereby mitigating the progression of renal dysfunction. It holds potential for research into chemotherapy-induced nephrotoxicity.</p>

<p>KIRA9 inhibits IRE1 with a 4.8 μM IC50, blocking ER-stress-induced mRNA decay and apoptosis by fully binding IRE1's ATP site.</p>

<p>PI3K-IN-58 (Compound 17f) is an inhibitor of PI3Kα with an IC50 value of 0.039 μM. It shows significant antiproliferative effects on PC-3, 22RV1, MDA-MB-231, and MDA-MB-453 cell lines with IC50 values of 3.48 μM, 1.06 μM, 2.21 μM, and 0.93 μM, respectively. PI3K-IN-58 induces apoptosis by downregulating the expression of anti-apoptotic proteins Bcl-XL and Bcl-2 while upregulating the expression of the pro-apoptotic protein BAX. This compound is applicable for research in cancer targeting through PI3K pathways.</p>

<p>Coprostanone (5β-cholestan-3-one) is an active metabolite of hydroxycholesterol and cholesterol. It induces apoptosis in primary gallbladder epithelial cells in dogs. Coprostanone holds potential for research into colon cancer or adenomatous polyps.</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>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>Tubulin polymerization-IN-68 (compound 32) serves as a tubulin inhibitor, disrupting cellular microtubule networks by hindering tubulin polymerization. It also upregulates PARP-1 and caspase-3 expression, thereby inducing apoptosis and exhibiting anticancer properties. Notably, Tubulin polymerization-IN-68 effectively suppresses HepG2 cells with an IC50 of 93 nM and markedly reduces the growth of HepG2 xenograft tumors in nude mice through oral administration.</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>LA-CB1 is a derivative of Abemaciclib that targets CDK4/6 and promotes their degradation via the ubiquitin-proteasome pathway, thereby blocking the CDK4/6-Cyclin D1-Rb-E2F axis and inducing G0/G1 cell cycle arrest and apoptosis (Apoptosis). It demonstrates antiproliferative activity against MDA-MB-231 cells with an IC50 of 0.27 µM and effectively inhibits epithelial-mesenchymal transition, cell migration, invasion, and angiogenesis. In highly invasive models like triple-negative breast cancer (TNBC), LA-CB1 significantly suppresses tumor growth, showing robust dose-dependent antitumor activity. This compound can be utilized in breast cancer research.</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>

<p>PLK1-IN-15 is a PLK1 inhibitor with an IC50 of 38.5 nM. It exhibits antiproliferative effects on HepG2, Huh7, H1299, and A549 cells, with IC50 values of 2.03, 2.08, 4.79, and 17.11 μM, respectively. Additionally, PLK1-IN-15 can induce cell cycle arrest in the G2/M phase and trigger apoptosis (Apoptosis), demonstrating anticancer activity.</p>

<p>Bcl-2-IN-6 suppresses Bcl-2, upregulates p53/Bax/caspase-7, arrests cell cycle, and induces MCF-7 apoptosis; IC50s: MCF-7 20.91 μM, others &lt;48 μM.</p>

<p>HDAC1-IN-5 inhibits HDAC1 (IC50=15 nM) &amp; HDAC6 (IC50=20 nM), promotes apoptosis, damages chromatin, and reduces tumor growth in mice.</p>

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

<p>T0080 is an FPR-1 antagonist. It reduces apoptosis (Apoptosis) and inhibits the production of reactive oxygen species (ROS) and pro-inflammatory cytokines (TNF-α and IL-1β) in plaque macrophages within ApoE−/− mouse models, thereby slowing the progression of atherosclerosis.</p>

<p>Antitumor agent-72 (compound 6w) is a potent anticancer agent that exhibits its anticancer activity by inducing apoptosis via caspase-3 activation and PARP</p>

<p>Tubulin inhibitor 14 blocks NQO2 and microtubule formation, disrupts blood vessels, and may target tumors; IC50 of 1.0 μM.</p>

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

<p>PF-3837 is an inhibitor of the Mps1 kinase, with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, thereby reducing genomic stability and leading to cancer cell apoptosis (Apoptosis). PF-3837 is utilized in the study of breast cancer.</p>

<p>VEGFR-2-IN-14 (Compound 5) is a potent inhibitor of VEGFR-2, which inhibits the growth of HepG2 cells in the Pre-G1 phase and induces apoptosis.</p>

<p>SphK1-IN-2: SphK1 inhibitor, IC50: 19.81 nM; less effective on SphK2. Induces apoptosis, hinders cancer cell growth.</p>

<p>SL-176, a WIP1 inhibitor, when combined with GSK-J4, can induce cell cycle arrest and apoptosis (apoptosis), thereby inhibiting tumor growth both in vitro and in vivo.</p>

<p>MY-875 inhibits microtubule formation, binds like colchicine (IC50: 0.92 μM), activates Hippo pathway, and induces apoptosis with anticancer properties.</p>

<p>Tofacitinib Prodrug-1: an oral prodrug reducing Tofacitinib's side effects, treats ulcerative colitis in mice effectively with low toxicity.</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>