Apoptosi

<p>Apoptosis Inducer 5, a lignan enantiomer extracted from Crataegus pinnatifida, demonstrates cytotoxic properties through inducing apoptosis and autophagy in</p>

<p>PI4KIII beta inhibitor 4 (Compound 16) is a selective inhibitor of PI4KIIIβ with an IC50 of 0.005 μM. By inhibiting the PI3K/AKT pathway, PI4KIII beta inhibitor 4 induces apoptosis, causes cell cycle arrest, and triggers autophagy in tumor cells. This compound is applicable for tumor research.</p>

<p>HDAC/PSMD14-IN-1 is a derivative of gambogic acid. It serves as an orally active dual inhibitor targeting PSMD14 and HDAC1, with IC50 values of 238.7 nM and 141.2 nM, respectively. The compound exhibits significant cytotoxicity against ESCC cell lines (IC50: 30-250 nM) and effectively reverses epithelial-mesenchymal transition (EMT). Additionally, HDAC/PSMD14-IN-1 can induce apoptosis. In KYSE30 cell xenograft models in mice, it displays antitumor activity. HDAC/PSMD14-IN-1 is useful for researching esophageal cancer treatment.</p>

<p>JR5-26B is an orally active apoptosis (apoptosis) inducer. It induces cell death via copper-mediated apoptosis and necroptosis (necroptosis). JR5-26B exhibits antiproliferative activity against MIA PaCa-2, PANC-1, PAN02, SU.86.86, and KPC-2 cells, with IC50 values of 0.6, 4.4, 8.0, 1.1, and 3.4 μM, respectively.</p>

<p>Thalidomide-Piperazine-PEG1-NH2 is a synthetic E3 ligase ligand-linker conjugate, featuring a cereblon ligand based on Thalidomide and a single linker.</p>

<p>PDEδ/NAMPT IN-1 (Compound 17d) is a dual inhibitor targeting phosphodiesterase 6 (PDE6) with a dissociation constant (KD) of 0.410 nM and nicotinamide phosphoribosyltransferase (NAMPT) with an inhibitory concentration (IC50) of 2.21 nM. It disrupts KRAS-related signaling by inhibiting NAMPT's role in the synthesis of nicotinamide adenine dinucleotide (NAD+), consequently inducing apoptosis in pancreatic cancer cells with KRAS mutations. This compound holds potential for research in KRAS-mutant pancreatic cancer.</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>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>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>PIM-1/HDAC-IN-1 (4d): inhibits PIM-1 (IC50: 343.87nM), HDAC1 (63.65nM), HDAC6 (62.39nM); induces apoptosis in MCF-7 cells.</p>

<p>MTDH-SND1 blocker 2 (compound C19) is an effective MTDH-SND1 inhibitor with an IC50 value of 487 nM. It binds to the SND1 protein with a Kd of 279 nM and can degrade the SND1 protein. Additionally, MTDH-SND1 blocker 2 exhibits antiproliferative activity and induces apoptosis, showing potential for breast cancer research.</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>GGTI298 is a potent GGTase I inhibitor; IC50 3μM for Rap1A, &gt;20μM for Ha-Ras.</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>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>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>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>Antitumor agent-77 suppresses cancer cell growth, migration, induces apoptosis, and hinders EMT.</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>Tubulin inhibitor 14 blocks NQO2 and microtubule formation, disrupts blood vessels, and may target tumors; IC50 of 1.0 μM.</p>

<p>GI-Y2 is a GSDMD inhibitor that suppresses macrophage pyroptosis induced by oxidized low-density lipoprotein (ox-LDL). In vivo, GI-Y2 dose-dependently reduces atherosclerotic plaques and decreases lesion size and fibrosis in the aortic root of ApoE-/- mice. GI-Y2 holds potential for research in pyroptosis and cardiovascular diseases, such as atherosclerosis.</p>

<p>Compound 8a, a dual PARP10 &amp; PARP15 inhibitor, has IC50s: PARP10 at 0.14μM &amp; PARP15 at 0.40μM; it's cell-permeable &amp; anti-apoptotic.</p>

<p>Minnelide is a prodrug of triptolide,and shows potent antitumor activity in a number of tumor types.</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>17-Demethoxy-reblastatin (17-DR) acts as an inhibitor of heat shock protein 90 (Hsp90). It suppresses the proliferation of HepG2 and SMMC7721 cancer cells, diminishes colony formation, and triggers apoptosis via a mitochondria and caspase-mediated pathway.</p>

<p>Elocalcitol is a calcitriol analog for inhibition of prostate cell growth.</p>

<p>Apoptosisinducer 25 (Compound 4H) demonstrates potent anticancer capabilities by inhibiting the proliferation of BGC-823 cancer cells with an IC50 of 0.37 μM. It induces apoptosis in BGC-823 cells, causes mitochondrial dysfunction, and arrests the cell cycle at the G2/M phase. Additionally, Apoptosisinducer 25 exhibits favorable pharmacokinetic properties in rats.</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>BMI-135, a selective estrogen mimic, demonstrates agonist activity for the estrogen receptor and induces a rapid endoplasmic reticulum stress response (UPR) alongside apoptosis in breast cancer cells.</p>

<p>Anticancer agent 69 targets PC3 cells (IC50=26 nM), raises ROS, lowers EGFR, and induces apoptosis.</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>ASK1-IN-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM. In a mouse liver injury model induced by Acetaminophen, ASK1-IN-8 significantly reduces plasma alanine aminotransferase (ALT) levels, offering liver protection. This compound is useful for research in liver disease-related fields.</p>

<p>Cetzole (Compound 1) acts as an inducer of ferroptosis (iron-dependent cell death) through the accumulation of ROS, leading to cell death. The compound exhibits varying half-maximal cytotoxic concentrations (CC50) against several cell lines: 2.56 μM in NCI-H522, 10.31 μM in NCI-H522 GFP-SCL7A11 #8, 2.71 μM in NCI-H522 RV-GFP, 3.07 μM in HT-1080, 14.9 μM in NARF2, and 6.28 μM in MDA-MB-231. This highlights Cetzole's potential for research in cancer therapeutics.</p>

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

<p>AZD0424: oral Src/Abl kinase inhibitor; potential anticancer; induces apoptosis, cell cycle arrest in lymphoma.</p>

<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>EGFR-IN-161 (Compound DD-8) is a potent and reversible inhibitor of the L858R/T790M/C797S mutant EGFR kinase, with an IC50 value of 0.87 nM. EGFR-IN-161 effectively inhibits tumor cell apoptosis, G1 phase arrest, and migration.</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>SLCB050 is a compound with anticancer activity that inhibits the interaction between DX2 and p14/ARF. It decreases the viability of human lung cancer cells, particularly small cell lung cancer cells, in a p14/ARF-dependent manner, and induces cell apoptosis (apoptosis) and senescence.</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>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>Sampangine, an alkaloid, induces apoptosis by causing cell cycle arrest at the G0/G1 phase and inhibits the biosynthesis of heme.</p>

<p>Caspase-3 Activator 4 (compound 4o) is an effective caspase-3 activator that can cross the blood-brain barrier. This compound exhibits antiproliferative activity and can induce cell apoptosis (apoptosis). Additionally, Caspase-3 Activator 4 enhances the gene expression of TNF-α and reduces the expression of cleaved caspase-3/caspases 3.</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>GPD-1116 is an orally active inhibitor of phosphodiesterase (PDE)4 and PDE1. The compound effectively reduces smoke-induced apoptosis in lung cells. Additionally, GPD-1116 has shown efficacy in various animal disease models, including emphysema, acute lung injury, chronic obstructive pulmonary disease (COPD), asthma, and pulmonary arterial hypertension.</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>CP-31398 stabilizes the active conformation of p53 in cancer cells with either mutated or wild-type p53, enhancing its activity. Additionally, CP-31398 upregulates target genes of p53 such as p21WAF1/Cip1 and KILLER/DR5. This compound possesses tumor-suppressive properties.</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>GP130-IN-1 (compound 49) is an effective inhibitor of GP130, demonstrating significant in vitro anti-tumor activity and higher selectivity compared to Bazedoxifene. It induces ultrastructural changes in cells, leading to a time-dependent arrest of the cell cycle at the G0/G1 phase, and triggers both apoptosis and autophagy. GP130-IN-1 is useful for research on triple-negative breast cancer.</p>

<p>TI17 is a selective TRIP13 inhibitor with anticancer activity and inhibits proliferation of multiple myeloma (MM) cells</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>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>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>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>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>BHA536 is an orally effective inhibitor of PKCα/β and the NF-kB signaling pathway. This compound inhibits the proliferation of ABC DLBCL cells harboring CD79 mutations by causing cell cycle arrest in the G1 phase and induces apoptosis in TMD8 cells. Additionally, BHA536 exhibits antitumor activity in mice.</p>

<p>LQB-118, an orally active compound sourced from sandalwood, demonstrates multiple therapeutic capabilities. It has shown proficiency in inhibiting glioblastoma cell migration and inducing apoptosis. Additionally, LQB-118 can curtail both migration and invasion of prostate cancer cells by modulating the AKT/GSK3β pathway and regulating MMP-9/reck gene expression. The compound is also effective against yeast polysaccharide-induced inflammation in both in vivo and in vitro settings. Notably, LQB-118 specifically triggers ROS-mediated and mitochondrial-dependent apoptosis in Leishmania amazonensis, highlighting its potential in studies focusing on inflammation, infections, and various cancers.</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>SPI-001 is a selective inhibitor of PPM1D (IC50=0.48 µM) that exhibits anticancer activity. The compound inhibits the phosphatase activity of PPM1D in human breast cancer cells overexpressing PPM1D and enhances the phosphorylation of p53. Additionally, SPI-001 suppresses cell proliferation by inducing apoptosis.</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>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>Bomedemstat (IMG-7289) hydrochloride, an oral LSD1 inhibitor, has anticancer properties, blocking cell growth and triggering apoptosis.</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>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>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>eIF4A3-IN-4 is a novel inhibitor of eIF4A (IC50: 8.6 μM).</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>Compound 2c is a potent p38α MAPK inhibitor with antitumor effects, enhancing apoptosis and ROS.</p>

<p>YCW-E11 is an antiapoptotic Bcl-2 family proteins inhibitor.</p>

<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>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>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>ADH-6, a tripyridylamide, disrupts mutant p53 aggregates in cancer cells, reviving its function and inducing apoptosis.</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>Lometrexol hydrate, an antipurine antifolate, inhibits GARFT and purine synthesis, leading to cancer cell apoptosis without causing DNA breaks.</p>

<p>GPX4-IN-3 (26a) is a potent GPX4 inhibitor, inducing selective ferroptosis with 71.7% inhibition at 1 μM.</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>LSD1/ER-IN-1 inhibits ER &amp; LSD1 (IC50: 1.55 μM), and fights MCF-7 breast cancer (IC50: 8.79 μM).</p>

<p>Spicamycin can be used as a potent inducer of differentiation of human myeloid leukemia cells (HL-60) and murine myeloid leukemia cells (M1).</p>

<p>Bim-IN-1 is a potent inhibitor of Bim expression with low toxicity, Bim-IN-1 reduces Bim expression levels with little inhibition of protein kinase A.</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>Akt/NF-κB/JNK-IN-1 (Compound 2i) is an inhibitor of Akt, NF-κB and JNK signalling pathways.Akt/NF-κB/JNK-IN-1 exhibits an inhibitory effect on nitric oxide</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>HAC-Y6 exerts its anticancer effects by inducing cell cycle arrest. It prompts apoptosis in COLO 205 cells with an IC50 of 0.52 µM.</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>CDK4/6-IN-10: Oral CDK4 (IC50: 22 nM) &amp; CDK6 (IC50: 10 nM) inhibitor with anti-cancer potential for MM research.</p>

<p>GLS1 Inhibitor-6: IC50=68nM, 220x more selective for GLS2, has anti-tumor and pro-apoptosis effects.</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>EGFR-IN-47: strong oral EGFRL858R/T790M/C797S blocker, induces cell death; promising for NSCLC research. IC50: 0.01 μM.</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>Antitumor agent-58 suppresses tumor growth, colony formation, cell migration, and induces mitochondrial dysfunction in MGC-803 cells.</p>

<p>Compound 3b inhibits tubulin polymerization, IC50 12.38 µM, with anticancer properties and promotes cell apoptosis.</p>

<p>Antitumor agent-42 inhibits microtubule multimerisation and NO release, exhibiting anti-angiogenic, colony-forming and apoptosis-inducing effects.</p>

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

<p>XIAP degrader-1 is a small primary amine molecule that promotes the degradation of X-linked apoptosis inhibitory protein (XIAP).</p>

<p>Thalidomide-NH-C5-NH2 is a synthetic E3 ligase ligand-linker conjugate, consisting of a Thalidomide-based cereblon ligand and a linker, used in the synthesis of PROTACs.</p>

<p>PD-1-IN-17 TFA is a potent PD-1 inhibitor, blocking 92% of splenocyte growth at 100 nM.</p>

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

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>AKN-028 acetate: an oral TK inhibitor for AML research, targets FLT3 with IC50 of 6 nM, inhibits autophosphorylation, and induces apoptosis.</p>

<p>YK5 is an allosteric inhibitor pocket of Hsp70 and represents a previously unknown chemical tool to investigate cellular mechanisms associated with Hsp70.</p>

<p>MD102, with an IC50 value of 0.35 μM, is a potent TG2 inhibitor that stabilizes p53 by inhibiting TG2. This results in a decrease in p-AKT and p-mTOR downstream signaling, ultimately inducing tumor cell apoptosis [1].</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>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>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>mTOR/HDAC6-IN-1 inhibits HDAC6 (IC50: 56 nM) &amp; mTOR (IC50: 133.7 nM), may treat TNBC by inducing autophagy and apoptosis.</p>