Apoptose

<p>PRMT6-IN-3 is a selective PRMT6 inhibitor with an IC50 value of 192 nM.PRMT6-IN-3 has anticancer activity and induces apoptosis in cancer cells.</p>

<p>Purinostat mesylate, a selective HDAC inhibitor (IC50: 0.81-11.5 nM), induces apoptosis and has potent anti-leukemic effects.</p>

<p>RIPK3-IN-4 (Compound 42) is a RIPK3 inhibitor that mitigates necroptosis, inflammatory responses, and HK-2 cell damage.</p>

<p>Fasnall, a fatty acid synthase (FASN) inhibitor, exhibits an IC50 of 3.71 μM against the human recombinant enzyme. It halts tritiated acetate incorporation into lipids (IC50= 5.84 μM), boosts ceramide levels, and triggers lipid droplet formation in BT474 HER2+ breast cancer cells. Demonstrating antiproliferative effects on various breast cancer cell lines, including non-tumorigenic MCF-10A and tumorigenic MCF-7, MDA-MB-468, BT474, and SK-BR-3, its efficacy is directly linked to FASN expression in vitro. In murine models of HER2+ breast cancer, particularly the MMTV-Neu model, Fasnall significantly reduces tumor volume and extends survival. Furthermore, it enhances the efficacy of carboplatin in vivo, bolstering the objective response rate of stable disease from 25% with carboplatin alone to 88% when paired with Fasnall.</p>

<p>AR420626: selective FA3R agonist, guards against SALS, effects blocked by BHB, a FA3R antagonist.</p>

<p>SM-1295: IAP antagonist, Kd 3077 nM XIAP-BIR3, 3.2 nM c-IAP1-BIR3, 9.5 nM c-IAP2-BIR3.</p>

<p>iMAC2 hydrochloride, a potent inhibitor of the mitochondrial apoptosis-induced channel (MAC), demonstrates an IC50 of 28 nM and an LD50 of 15000 nM. It exhibits an anti-apoptotic effect by blocking the release of cytochrome c [1].</p>

<p>Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on</p>

<p>BHD, a reversible male contraceptive agent, effectively induces spermatogenic cell apoptosis and causes abnormalities in seminiferous tubules in vivo at doses</p>

<p>TM5441, an orally bioavailable plasminogen activator inhibitor-1 (PAI-1) inhibitor with IC50 values ranging from 13.9 to 51.1 μM, effectively induces intrinsic apoptosis across multiple human cancer cell lines. Additionally, it mitigates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence [1] [2].</p>

<p>GDC-2394: Oral, selective NLRP3 inhibitor; blocks IL-1β (human 0.4μM, mouse 0.1μM), spares NLRC4.</p>

<p>TMX-2164: strong, irreversible BCL6 inhibitor, IC50=152 nM, long-lasting action, inhibits cell proliferation.</p>

<p>AMRI-59 is a potent inhibitor of PrxI with anti-tumor activity.</p>

<p>Eeyarestatin I blocks ER protein degradation, hinders p97/atx3 processes, and induces anticancer proteins.</p>

<p>AT-9283 L-lactate is an inhibitor of aurora kinase.</p>

<p>BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM).</p>

<p>Sirt1/2-IN-2 (compound hsa55) serves as a dual inhibitor for SIRT1 with an IC50 of 1.8 μM and SIRT2 with an IC50 of 2.4 μM, respectively.</p>

<p>MAO-B-IN-26 (Compound IC9) serves as both a MAO-B and acetylcholinesterase inhibitor.</p>

<p>HJC0152 (free base) is an orally active, potent STAT3 inhibitor that impedes cell cycle progression, induces apoptosis, and notably reduces MDA-MB-231 xenograft</p>

<p>Ro 41-5253 is a RARα antagonist with antitumor activity that inhibits the proliferation of ZR-75.1 estrogen receptor-positive breast cancer cells.</p>

<p>HDAC-IN-46 inhibits HDAC1 &amp; HDAC6, affects p-p38, Bcl-xL &amp; cyclin D1, blocks G2 phase &amp; induces apoptosis in TNBC research.</p>

<p>RET-IN-17 inhibits RET kinase; may help in IBS pain and RET-activated cancers.</p>

<p>Nalmefene (ORF 11676) is a μ-opioid antagonist and partial κ agonist used to study opioid overdose and alcohol dependence.</p>

<p>KRIBB3: novel anticancer microtubule inhibitor; halts MDA-MB-231 cell migration/invasion by targeting Hsp27 phosphorylation.</p>

<p>BAX-IN-1 is a potential selective inhibitor of Bcl-2-associated X protein (BAX).</p>

<p>Lepadin H, a marine alkaloid and ferroptosis inducer, exhibits significant cytotoxicity by promoting p53 expression, escalating ROS production, and enhancing</p>

<p>Ponicidin, a diterpenoid from Rabdosia rubescens, has immunoregulatory, anti-inflammatory, anti-viral, and anti-cancer properties.</p>

<p>MY-673, a colchicine binding site inhibitor (CBSI), impedes tubulin polymerization and disrupts the ERK signaling pathway, consequently modulating SMAD4 protein</p>

<p>MP7 (PDK1 inhibitor) is a inhibitor of phosphoinositide-dependent kinase-1 (PDK1).</p>

<p>FGFR-IN-8, potent oral FGFR inhibitor for wild-type/mutant types, induces apoptosis with anti-cancer properties.</p>

<p>AAPK-25, a dual Aurora/PLK inhibitor, disrupts mitosis, induces apoptosis, and has antitumor properties.</p>

<p>NSC 48160 is an anti-pancreatic cancersmall molecule that inhibits growth and enhance apoptosis of pancreatic cancer cells through the mitochondrial pathway.</p>

<p>Tylvalosin (Acetylisovaleryltylosin) is a broad-spectrum macrolide antibiotic with antibacterial and antiviral properties, effective against PRRSV infection.</p>

<p>Topoisomerase II inhibitor 15 (compound 2g) serves as a potent apoptotic inducer, exhibiting heightened selectivity for head and neck tumors [1].</p>

<p>EAD1 HCL is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 HCL also induces apoptosis</p>

<p>SCH79797 dihydrochloride is a PAR1 antagonist with IC50 70 nM, Ki 35 nM, antiproliferative, and pro-apoptotic properties.</p>

<p>HM90822 is an IAP antagonist that inhibits XIAP and cIAP1/2 protein expression, induces IAP ubiquitination and promotes proteasome-dependent IAP degradation.</p>

<p>Nedometinib (NFX-179) is a MEK1 inhibitor with anticancer and antitumor activities, which can be used to study malignant tumors.</p>

<p>MRT199665, a selective MARK/SIK/AMPK inhibitor, blocks SIK CRTC3 S370 phosphorylation and triggers apoptosis in AML cells.</p>

<p>CNDAC, a nucleoside analog, is a major metabolite of oral drug sapacitabine.</p>

<p>CR-1-31-B, a synthetic rocaglate, inhibits eIF4A, hinders protein synthesis initiation, and induces apoptosis in cancer cells.</p>

<p>Compound 37b3, an anticancer, halts tumor growth, triggers cell death, and pairs with Trastuzumab to form T-PBA, an ADC with targeted delivery.</p>

<p>13h (hGGPPS-IN-3), a strong C2-ThP-BPs hGGPPS blocker, triggers MM cell apoptosis and shows in vivo anti-myeloma effects.</p>

<p>BIX selectively induces BiP/GRP78 and ER chaperone, preventing cell death in neurons and retinas.</p>

<p>MI-219 is a human double minute 2 (HDM2) inhibitor.</p>

<p>HDAC-IN-60 (compound 21a), a potent histone deacetylase (HDAC) inhibitor, promotes intracellular reactive oxygen species (ROS) production, induces DNA damage,</p>

<p>(S)-Verapamil hydrochloride is an inhibitor of leukotriene C4 (LTC4) and calcein transport by MRP1,and leads to the death of potentially resistant tumor cells.</p>

<p>Ferroptocide is a thioredoxin inhibitor that induces iron death in cancer cells and can be used in breast cancer research.</p>

<p>SF5 is an inhibitor of the apoptosis pathway through JNK-p53-caspase apoptotic cascade.</p>

<p>DLC-50 is a dual inhibitor of PARP-1 and HDAC-1, exhibiting IC50 values of 1.2 nM and 31 nM respectively. It hinders the proliferation of cancer cells such as MDA-MB-436, MDA-MB-231, and MCF-7 with IC50 values of 0.3 μM, 2.7 μM, and 2.41 μM respectively. Additionally, DLC-50 induces apoptosis in MDA-MB-231 cells and causes cell cycle arrest at the G2 phase.</p>

<p>CPT-Se3, a camptothecin derivative, boosts anticancer activity, triggers apoptosis in Hep G2, and is cytotoxic to various cells with IC50 of 2.19-4.7 μM.</p>

<p>1-Stearoyl-2-Adrenoyl-sn-glycero-3-PC (PC(18:0/22:4)) acts as a cyclin-dependent kinase (CDK) inhibitor, promoting apoptosis and restricting the proliferation of various cancer cell lines [1].</p>

<p>(Rac)-Lisaftoclax ((Rac)-APG-2575), a Bcl-2 inhibitor, is utilized in hematologic malignancy research (CN112898295A) [1].</p>

<p>Deoxynybomycin, a selective anti-tumor agent, inhibits topoisomerase I and induces apoptosis.</p>

<p>Mcl-1 Inhibitor 17 is a compound that functions as an inhibitor of the Mcl-1 protein, specifically designed for use in cancer and other disease research [1].</p>

<p>HDAC-IN-53 inhibits HDAC1-3 with IC50s: 47, 125, 450 nM. Inactive on class II HDACs; triggers apoptosis; reduces tumor growth in mice.</p>

<p>RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal</p>

<p>SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.</p>

<p>NWP-0476 is a modified BCL-2/BCL-xL inhibitor with enhanced specificity for BCL-xL, suitable for research on relapsed T-acute lymphoblastic leukemia (T-ALL) [1</p>

<p>15-Deoxy-Δ12,14-Prostaglandin A1, a deoxyanalog of prostaglandins, inhibits NF-κB signaling and induces apoptosis. It also prevents TNF-α-induced upregulation of inflammatory endothelial cell adhesion molecules (CAM) and reduces monocyte arrest [1].</p>

<p>INCB3619 is a selective and potent inhibitor of ADAM with antitumour effects, inhibiting ADAM10, ADAM17, MMP12 and MMP15.</p>

<p>Famitinib malate (SHR1020) is a potent oral kinase inhibitor targeting c-kit, VEGFR-2, and PDGFRβ, with IC50s 2.3, 4.7, 6.6 nM, useful for cancer research.</p>

<p>Immunosuppressant-1 (Compound 31) suppresses T-cell proliferation triggered by anti-CD3/anti-CD28 co-stimulation and demonstrates immunosuppressive effects,</p>

<p>Pelcitoclax (APG-1252) is a powerful inhibitor of the Bcl-2 and Bcl-xl proteins, displaying significant antineoplastic and pro-apoptotic properties[1].</p>

<p>JNJ-1013 is a selective IRAK1 PROTAC degrader with an IC50 of 72 nM ,antiproliferative and proapoptotic, increases cleaved-PARP expression.</p>

<p>Compound G-5b, an estrogen receptor modulator 10, functions as an estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM).</p>

<p>RUNX-IN-2 (Compound Conjugate 3) covalently attaches to RUNX-binding sequences, preventing RUNX proteins from associating with their targets, thereby inhibiting</p>

<p>USP7-IN-3 is a potent and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7).</p>

<p>ST1074, a dual inhibitor of CerS2 and CerS4, promotes apoptosis and is applicable in cancer research [1].</p>

<p>RIPK1-IN-8 is an aminoimidazolopyridine and is a selective and potent inhibitor of RIPK1 (IC50: 4 nM).RIPK1-IN-8 has research potential in inflammatory diseases</p>

<p>AM-8735 is an inhibitor of MDM2 ( IC50: 25 nM).</p>

<p>BQZ-485, a potent GDI2 inhibitor, interacts with Tyr245 to disrupt the native GDI2-Rab1A interaction.</p>

<p>IM156, a Metformin derivative, activates AMPK, enhances cognition in aging animals, and inhibits OXPHOS in solid tumor research.</p>

<p>RET-IN-24 (Compound 26) is a selective inhibitor of RET tyrosine kinase, demonstrating antitumor activity [1].</p>

<p>RUNX-IN-1, also known as Compound Conjugate 1, covalently attaches to RUNX-binding sequences, thereby preventing RUNX proteins from associating with their</p>

<p>RIPK1-IN-10 is a potent inhibitor of RIPK1.</p>

<p>Antitumor agent-97 (compound 42), an anticancer agent, effectively inhibits proliferation and autophagy in MGC 803 cells, induces apoptosis, and enhances ROS</p>

<p>K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 µM and Ki of 6.4 µM.</p>

<p>Z-LLY-FMK (Calpain Inhibitor IV) serves as an inhibitor of calpain, a family of proteases implicated in the apoptosis of various cell systems.</p>

<p>A-1293102 is a potent, selective inhibitor of BCL-XL, effective in inducing apoptosis in tumor cells reliant on BCL-XL [1].</p>

<p>C 87: Small-molecule TNF-α inhibitor, binds TNFα, inhibits cytotoxicity with IC50 of 8.73 μM, blocks signaling.</p>

<p>AGN194204 (IRX4204), an oral RXR agonist, inactive against RAR, has Kd 0.4-3.8 nM &amp; EC50 0.08-0.8 nM, with anti-inflammatory and anticarcinogenic properties.</p>

<p>DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP.</p>

<p>PD-1/PD-L1-IN-22 is a small molecule inhibitor of PD-1/PD-L1 protein-protein interactions that blocks PD-1/PD-L1 interactions (IC50: 0.732 μM).</p>

<p>Delmitide acetate (RDP58) is an orally active d-isomer decapeptide that exhibits potent anti-inflammatory properties.</p>

<p>YS-363 is a potent, selective, and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting half-maximal inhibitory concentrations (</p>

<p>BCL6-IN-4, a potent inhibitor of B-cell lymphoma 6 (BCL6), exhibits anti-tumor activities with an inhibitory concentration 50 (IC50) value of 97 nM[1].</p>

<p>Z-YVAD-CMK is an inhibitor of both caspase-1 and caspase-3, as referenced in [1].</p>

<p>BPR1J-340, a novel potent FLT3 inhibitor, shows anticancer promise, with IC50 ~25 nM and GC50 ~5 nM, causing apoptosis in AML cells.</p>

<p>LY303511, a structural analog of LY294002, selectively inhibits mTOR-dependent phosphorylation of S6K, unlike its counterpart, which acts as a phosphatidylinositol 3-kinase (PI3K) inhibitor. It effectively reduces cell proliferation in human lung epithelial adenocarcinoma cells by hindering G2/M phase progression and suppressing casein kinase 2 activity. Additionally, LY303511 enhances tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) sensitivity in HeLa cells resistant to TRAIL-induced apoptosis and blocks voltage-gated potassium (Kv) channels.</p>

<p>Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).</p>

<p>Bcl-2-IN-11 (compound 6) is a potent and selective inhibitor of Bcl-2 activity, exhibiting an IC50 of 0.9 nM, and demonstrates minimal inhibition against Bcl-xl</p>

<p>Calicheamicin (Calicheamicin γ1) is an antitumor antibiotic and is a DNA synthesis inhibitor. It also is a cytotoxic agent that causes double-strand DNA breaks.</p>

<p>PI3K/VEGFR2-IN-1 is a potent dual inhibitor targeting both PI3K and VEGFR2 with IC50 values of 2.21 μM for PI3K and 68 μM for VEGFR2, respectively.</p>

<p>Met-F-AEA is a metabolically stable analogue of anandamine that exhibits antitumor activity by inhibiting cell growth through the activation of apoptosis [1].</p>

<p>(+)-Apogossypol is an antagonist of pan-BCL-2. (+)-Apogossypol binds to Mcl-1(Bcl-2 and Bcl-xL with EC50s of 2.6, 2.8 and 3.69 μM, respectively).</p>

<p>Erythro-Austrobailignan-6: orally active, anti-cancer, inhibits DNA topoisomerases, induces apoptosis, boosts p38/JNK phosphorylation.</p>

<p>SWS1, a d-(+)-biotin-conjugated PD-L1 inhibitor (IC50: 1.8 nM), displays anticancer activity by augmenting tumor-infiltrating lymphocytes and demonstrating anti</p>

<p>RMC-4998 is an orally available KRASG12C mutant inhibitor that targets the active or GTP-bound state of the KRASG12C mutant,inhibit ERK and apoptosis.</p>

<p>INU-152: pan-RAF inhibitor with potent anti-tumor effects on BRAFV600E cancers, inhibits MAPK in mutant cells, minimal side effects on RAS-mutant melanoma.</p>