Apoptosis

<p>NHWD-870 selectively inhibits BET bromodomains BRD2-4, BRDT; potent anti-cancer effect by inducing apoptosis, halting cell growth.</p>

<p>FOXO1-IN-3 is a highly-selective, orally active inhibitor of FOXO1 that diminishes hepatic glucose production and enhances insulin sensitivity and glucose</p>

<p>HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4.</p>

<p>HDAC-IN-59 (compound 13a), a potent histone deacetylase (HDAC) inhibitor, enhances intracellular reactive oxygen species (ROS) production, induces DNA damage,</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>

WYE-125132: potent mTOR inhibitor, IC50 0.19 nM, selective over PI3Ks/hSMG1/ATR.

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

<p>Ac-YVAD-pNA, a specific substrate for Caspase-1, serves to detect Caspase-1 activity, a crucial mediator of inflammatory processes [1] [2].</p>

<p>MK-2206 free base is an allosteric Akt inhibitor that is both potent and selective, administered orally, exhibiting IC50 values of 8, 12, and 65 nM for Akt1,</p>

<p>Sirt1/2-IN-3 (compound PS9) serves as a dual inhibitor of SIRT1/2, exhibiting IC50 values of 1.4 μM (SIRT1) and 2.0 μM (SIRT2), respectively.</p>

<p>RET-IN-5 is a potent inhibitor of RET (IC50: 4.57 nM).</p>

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

<p>10-OAHSA is a newly discovered endogenous lipid categorized within the group of branched fatty acid esters of hydroxy fatty acids (FAHFAs). This specific FAHFA comprises oleic acid esterified to 10-hydroxy stearic acid. It stands out among its FAHFA counterparts for its potential bioactive properties, similar to other members of its family such as PAHSAs, which are notably prevalent in the adipose tissue of AG4OX mice exhibiting glucose tolerance due to overexpression of the Glut4 glucose transporter specifically in adipose tissue. Like other FAHFAs, 10-OAHSA may play significant roles in enhancing glucose tolerance, stimulating insulin secretion, and exerting anti-inflammatory effects, which suggests its importance in managing metabolic syndrome and inflammation.</p>

<p>BIX selectively induces BiP/GRP78 and ER chaperone, preventing cell death in neurons and retinas.</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-24 (Compound 26) is a selective inhibitor of RET tyrosine kinase, demonstrating antitumor activity [1].</p>

<p>Lacutoclax (LP-108) is an orally active and selective Bcl-2 inhibitor with antitumor activity both in vivo and ex vivo，lymphoma and leukemia.</p>

<p>PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor demonstrating an inhibition concentration (IC50) of 0.6 ± 0.1 nM.</p>

MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.

<p>MTI-31 (LXI-15029) is a potent oral mTORC1/2 inhibitor with a Kd of 0.20 nM, &gt;5,000-fold selectivity, and an IC50 of 39 nM.</p>

<p>BMS-561392 (DPC333) is a tumor necrosis factor-α ( TNF-α) Invertase inhibitor.</p>

<p>SAFit1 is an inhibitor of FK506 binding protein 51 (FKBP51)-specific (Ki: 4±0.3 nM).</p>

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

<p>2-Chlorophenoxazine is an Akt inhibitor that demonstrates an in vitro inhibitory concentration (IC50) of 2-5 μM and has the capacity to induce apoptosis.</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>APE1-IN-2 (AP1), a Pt(IV) proagent, targets APE1 protein, induces DNA damage, and triggers apoptosis with anticancer effects.</p>

<p>PD-1-IN-1 is a programmed cell dealth-1inhibitor. PD-1-IN-1 can be used as an immune modulator.</p>

<p>INI-43 targets Kpnβ1, disrupting nuclear transport in cervical/esophageal cancers, affecting NFAT, NFκB, AP-1, NF localization.</p>

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

<p>AGN 192870 is a potent retinoic acid receptor (RAR) antagonist.AGN 192870 can be used to study cell growth arrest, differentiation and apoptosis.</p>

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

<p>BMS-561392 formate, the formate derivative of BMS-561392, functions as a TNF alpha-converting enzyme (TACE) inhibitor and an ADAM17 blocker. It is utilized in the research of inflammatory bowel disease [1] [2].</p>

<p>p-Tolylmaleimide (p Tolylmaleimide) is an inhibitor of the water channel and binds to Aquaporin Z.</p>

<p>YM281 is a potent EZH2 inhibitor, causes apoptosis and G0/G1 arrest, has antitumor activity in vivo, and may be researched for lymphoma.</p>

<p>(S)-Sabutoclax ((S)-BI-97C1), an optically pure derivative of apogossypol, serves as a pan-active inhibitor of the antiapoptotic B-cell lymphoma/leukemia-2 (Bcl-2) family proteins. It effectively blocks the binding of BH3 peptides to key proteins in the family, including Bcl-XL, Bcl-2, Mcl-1, and Bfl-1, displaying inhibitory concentration (IC50) values of 0.31, 0.32, 0.20, and 0.62 μM, respectively. Furthermore, (S)-Sabutoclax demonstrates potent efficacy in inhibiting the growth of various cancer cell lines, such as those from human prostate cancer, lung cancer, and lymphoma, with half-maximal effective concentration (EC50) values of 0.13, 0.56, and 0.049 μM, respectively. This compound is utilized in research focusing on apoptosis-based cancer therapies [1].</p>

<p>HDAC-IN-50, a potent FGFR/HDAC inhibitor (IC50: 0.18-13 nM), induces apoptosis, cell cycle arrest, and shows anti-tumor activity.</p>

<p>GDC-2394: Oral, selective NLRP3 inhibitor; blocks IL-1β (human 0.4μM, mouse 0.1μM), spares NLRC4.</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>RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal</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>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>RIP1 Kinase Inhibitor 8 (Compound 77), a potent and highly selective dihydropyrazole (DHP) RIP1 kinase inhibitor, exhibits an IC50 of 20 nM and effectively</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>CPUY201112, a novel inhibitor of heat shock protein Hsp90, induces p53-mediated apoptosis in MCF-7 cells.</p>

<p>N-Oleoyl serinol, a ceramide analog, plays a crucial role in stem cell therapy by inhibiting the development of teratomas in stem cells. It triggers apoptosis in remaining pluripotent embryoid body-derived cells (EBCs), thwarts teratoma formation, and promotes the enrichment of EBC cells that proceed to neural differentiation post-transplantation [1].</p>

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

<p>Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on</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>NBI-961, a potent NEK2 inhibitor, suppresses proteasomal degradation and effectively induces G2/mitosis arrest and apoptosis within diffuse large B cell</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>Ogremorphin (GPR68-IN-1) is a potent inhibitor of GPR68, exhibiting an EC50 of 170 nM.it is utilized in the study of autoimmune chronic inflammatory diseases [1</p>

<p>Artonin E, a prenylated flavonoid, induces apoptosis and S-phase arrest, disrupting the mitochondrial pathway for cancer research.</p>

<p>Cerivastatin is an HMG-CoA reductase inhibitor with anticancer and lipid-lowering effects and can be used to study primary hyperlipidemia.</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>Nedometinib (NFX-179) is a MEK1 inhibitor with anticancer and antitumor activities, which can be used to study malignant tumors.</p>

<p>YM458 inhibits EZH2 (490 nM) and BRD4 (34 nM), curbing tumor cell growth and inducing apoptosis.</p>

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

<p>PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active inhibitor of pyruvate dehydrogenase kinase 4 (PDK4, IC50 value = 84 nM).</p>

<p>CDKI-83, a potent CDK9 inhibitor, inhibits tumor growth with GI50 &lt;1μM and triggers apoptosis in A2780 cells, showing promise as an anti-cancer agent.</p>

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

<p>HDAC-IN-63 (Compound 63) is a dual FLT3/HDAC inhibitor with IC50 values of 0.844 nM for FLT3 and 30.0 nM for HDAC1.</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>Antitumor Agent-110 (Compound 13), an imidazotetrazine anticancer agent, exhibits excellent permeability.</p>

<p>4E2RCat is an inhibitor of eIF4E-eIF4G interaction (IC50 = 13.5 μM) and is capable of blocking coronavirus replication as monitored by viral protein expression</p>

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

<p>Immuno modulator-1 (compound 22) effectively suppresses the secretion of TNFα and IL-2 in human peripheral blood mononuclear cells (hPBMC) with IC50 values of 4</p>

<p>Q-VD-OPh: broad-spectrum, non-toxic caspase inhibitor; cost-effective, specific for apoptotic inhibition.</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>CIL62 is a caspase-3/7-independent inducer of cell death. The mechanism of action of CIL62 is Necrostatin-1 dependent cell death [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>Anticancer agent 128 (compound 1) is an IAP inhibitor that covalently binds to the BIR3 domains of XIAP, cIAP1, and cIAP2, exhibiting IC50 values of 24.9 nM, 19</p>

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

<p>D359-0396 is an orally active NLRP3 inflammasome inhibitor that mitigates pyroptosis and reduces IL-1β release in macrophages by inhibiting the oligomerization</p>

<p>GCN2-IN-6: Potent, oral GCN2/PERK inhibitor; IC50s - GCN2: 1.8 nM (enzymatic), 9.3 nM (cellular); PERK: 0.26 nM (enzymatic), 230 nM (cellular).</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>AR420626: selective FA3R agonist, guards against SALS, effects blocked by BHB, a FA3R antagonist.</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>Ferroptocide is a thioredoxin inhibitor that induces iron death in cancer cells and can be used in breast cancer research.</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>

Docebenone is a selective and orally active inhibitor of 5-LO.

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

<p>CPT-Se4, a seleno-derivative of CPT, effectively kills cancer cells, triggers apoptosis, and is cytotoxic against various cell lines.</p>

GSK2245035: selective nasal TLR7 agonist, boosts Type-1 IFN (pEC50: 9.3 IFNα, 6.5 TFNα), curbs Th2 cytokines in blood cultures.

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

<p>HDAC1/CDK7-IN-1 (compound 8e) serves as a dual inhibitor targeting both CDK7 and HDAC1, with IC50 values of 893 nM and 248 nM , respectively.</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>

"DC_AC50 inhibits Atox1/CCS to reduce cancer cell growth and prevent chemotherapy resistance."

<p>Pivanex, an oral HDAC inhibitor, targets metastasis, angiogenesis, reduces Bcr-Abl protein, and promotes apoptosis.</p>

<p>Necrocide 1 is a inducer of cancer cell necrosis that is not inhibited by caspase, BCL2 , or TNFα, and acts through the mitochondrial regulatory pathway.</p>

<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>NSC194598 is a p53 DNA-binding inhibitor, demonstrating an in vitro IC50 of 180 nM and an in vivo range of 2-40 μM.</p>

<p>Tubulin Polymerization-IN-56 (compound 8l), an indazole derivative, potently inhibits tubulin polymerization by targeting the colchicine site, which induces</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>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>MTP, a PKM2 inhibitor, promotes apoptosis in cancer cells via caspase-3 activation while also inducing autophagy and enhancing ROS generation.</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>SCH79797 dihydrochloride is a PAR1 antagonist with IC50 70 nM, Ki 35 nM, antiproliferative, and pro-apoptotic properties.</p>

<p>WEHI-345 analog is an Src inhibitor.</p>