Apoptosis

<p>GDC-2394: Oral, selective NLRP3 inhibitor; blocks IL-1β (human 0.4μM, mouse 0.1μM), spares NLRC4.</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>Anticancer Agent 118, an N‑acylated ciprofloxacin derivative, exhibits antibacterial efficacy against Gram-positive strains and antiproliferative effects on</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>Potent EGFR blocker; acts on WT, L858R/T790M (IC50: 1.7 nM), less on T790M/C797S; stalls cell cycle, induces apoptosis, deters metastasis.</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>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>BMS-561392 (DPC333) is a tumor necrosis factor-α ( TNF-α) Invertase inhibitor.</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>AR420626: selective FA3R agonist, guards against SALS, effects blocked by BHB, a FA3R antagonist.</p>

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

<p>FGFR-IN-8, potent oral FGFR inhibitor for wild-type/mutant types, induces apoptosis with anti-cancer 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>PF-07284892 (ARRY-558) is an orally active allosteric SHP2 inhibitor (IC50 = 21 nM) that reduces pERK expression and may be employed in solid tumour research.</p>

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

<p>Falcarindiol: Activates PPARγ, boosts ABCA1, induces apoptosis/autophagy, has anti-inflammatory/anticancer effects.</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>Cis-3,4',5-Trimethoxy-3'-hydroxystilbene, a stilbene derivative, induces apoptosis through the mitochondrial release of cytochrome c and suppresses tubulin polymerization. It is also noted for its application in leukemic research [1].</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>Cu(II)-Elesclomol is a complex formed by the anticancer agent Elesclomol and Cu(II), which has anticancer activity and can be used in the study of leukemia.</p>

<p>MC2590 is a histone deacetylase (HDAC) inhibitor that inhibits HDAC1-3, -6, -8, and -10 activities, induces cell cycle arrest, and promotes apoptosis.</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>WNY1613: Potent PI3Kδ inhibitor with anti-NHL properties, induces apoptosis in cells, affects phosphorylation in vitro/in vivo.</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>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>S-Adenosyl-L-methionine (SAMe) 1,4-butanedisulfonate functions as an orally active methyl group donor and serves as a dietary supplement known for its</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>LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.</p>

<p>Compound A5b, also known as JMJD3/HDAC-IN-1, is a dual inhibitor that targets both JMJD3 (Jumonji domain-containing protein demethylase 3) and HADC1 (histone</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>Merodantoin induces apoptosis in KRAS-mutant cancer cells via ROS-autophagy and Akt pathway.</p>

<p>SC 67655 is a peptidomimetic that specifically suppresses human leukocyte antigen DRB10401-restricted T cell proliferation.</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>Deoxynybomycin, a selective anti-tumor agent, inhibits topoisomerase I and induces apoptosis.</p>

<p>BET-IN-20 (compound 10), a BRD4 BD1 inhibitor (IC 50 =1.9 nM), exhibits significant anticancer properties. It promotes apoptosis in acute myeloid leukemia (AML) cells and arrests the cell cycle in the G0/G1 phase. Additionally, BET-IN-20 inhibits both c-Myc and CDK6, and enhances PARP cleavage [1].</p>

<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>RET-IN-25 (compound 6b) is an anticancer RET kinase inhibitor that demonstrates efficacy against medullary thyroid carcinoma (MTC), exhibiting half-maximal</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>FLT3-IN-14: FLT3 inhibitor; FLT3-WT IC50=5.6nM, FLT3-ITD IC50=1.4nM; blocks Y591 phosphorylation; G1 arrest; pro-apoptotic.</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>Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).</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>CPUY201112, a novel inhibitor of heat shock protein Hsp90, induces p53-mediated apoptosis in MCF-7 cells.</p>

<p>Ac-Val-Ala-Asp-CHO (Ac-VAD-CHO) serves as a pan-caspase inhibitor and preserves mitochondrial membrane potential (MMP) while preventing the release of</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>Ezatiostat HCl (TLK199) inhibits glutathione S-transferase, GSTP1-1 specifically, and may treat cytopenias.</p>

<p>SM-433: Smac mimetic, blocks IAPs, strong XIAP BIR3 affinity (IC50 &lt;1 μM). See patent WO2008128171A2.</p>

<p>PLK1/BRD4-IN-1 (9b) is an orally active dual inhibitor of PLK1 (IC50: 22 nM) and BRD4 (IC50: 109 nM).</p>

<p>BAI1 hydrochloride is a selective inhibitor of the apoptosis factor BAX, functioning through an allosteric mechanism. By binding to BAX, it allosterically inhibits its activation, showcasing potential applications in the research of diseases mediated by BAX-dependent cell death [1].</p>

<p>Ginsenoside Rk1 is a component created by processing the ginseng plant at high temperatures.</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>YM281 is a potent EZH2 inhibitor, causes apoptosis and G0/G1 arrest, has antitumor activity in vivo, and may be researched for lymphoma.</p>

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

<p>Potent RIP2 kinase inhibitor with 0.03 μM IC50, selective for autoimmune disease treatment.</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>Lactoferrin 17-41 (Lactoferricin B) acetate, a peptide derived from bovine lactoferrin spanning residues 17-41, exhibits broad-spectrum antimicrobial properties against Gram-positive and Gram-negative bacteria, viruses, protozoa, and fungi. Additionally, this compound demonstrates antitumor activities [1] [2].</p>

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

<p>Ethylene glycol dimethacrylate, a methacrylate monomer, demonstrates cytotoxic and genotoxic impacts on human gingival fibroblasts (HGFs), elevating</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>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>PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor demonstrating an inhibition concentration (IC50) of 0.6 ± 0.1 nM.</p>

<p>HS148 selectively inhibits DAPK3 (Ki 119 nM), reducing gastric cancer progression via ULK1-dependent autophagy and tumor suppression pathways.</p>

<p>viFSP1, a species-independent FSP1 inhibitor, effectively induces ferroptosis in FSP1-dependent cells by targeting the highly conserved NAD(P)H binding pocket of FSP1, directly inhibiting its activity. This action results in lipid peroxidation and exhibits anticancer activity [1].</p>

<p>SF5 is an inhibitor of the apoptosis pathway through JNK-p53-caspase apoptotic cascade.</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>IM156, a Metformin derivative, activates AMPK, enhances cognition in aging animals, and inhibits OXPHOS in solid tumor research.</p>

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

<p>Potent γ-secretase inhibitor; IC50: 1.2 nM (cell), 6.2 nM (cell-free); lowers Aβ in mice/guinea pigs' brain, CSF, plasma.</p>

<p>ICL-CCIC-0019 inhibits ChoKα, causes G1 arrest, ER stress, and cancer cell apoptosis.</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>YS-363 is a potent, selective, and orally active inhibitor of the epidermal growth factor receptor (EGFR), exhibiting half-maximal inhibitory concentrations (</p>

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

<p>Ferroptocide is a thioredoxin inhibitor that induces iron death in cancer cells and can be used in breast cancer research.</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>BQZ-485, a potent GDI2 inhibitor, interacts with Tyr245 to disrupt the native GDI2-Rab1A interaction.</p>

<p>Ethylene dimethanesulfonate has selective pro-apoptotic effects on LCs. Ethylene dimethanesulfonate is a mild alkylating, non-volatile methanesulfonic diester</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>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>LB42708 is an orally active farnesyltransferase (FTase) inhibitor (IC50: 0.8/1.2/2.0 nM toward H/N/K-ras).</p>

<p>ZNL 02-096 (Pomalidomide-C3-adavosertib) is a rapid and selective degrader of Wee1 (IC50=3.58 nM).ZNL 02-096 selectively degrades Wee1 at submolar</p>

DuP-697 is an irreversible, specific COX-2 inhibitor with IC50 values ​​of 10 nM and 800 nM for human COX-2 and COX-1.Cost-effective and quality-assured.

<p>GCN2-IN-7 is an inhibitor of the environmental sensing protein GCN2 with antitumor activity for the study of melanoma.</p>

<p>Ac-DEVD-CHO is a specific Caspase-3 inhibitor (Ki: 230 pM).Ac-DEVD-CHO has an inhibitory effect in SLNT-induced apoptosis.</p>

<p>Tefinostat (CHR-2845) is a potent monocyte/macrophage-targeted histone deacetylase (HDAC) inhibitor.</p>

<p>KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP.KSQ-4279 has anticancer activity and is used in the study of non-small cell lung cancer, osteosarcoma,</p>

<p>MC4033 exhibits inhibitory concentration 50 (IC50) values of 39.4 µM in HCT116, 52.1 µM in H1299, 41 µM in A549, and 30.1 µM in U937 [1].</p>

<p>JHU395, an oral prodrug of glutamine antagonist DON, shows stable antitumor effects on MPNST in vitro and vivo.</p>

<p>RH01386, a small molecule, prevents ER stress in β cells, inhibits proapoptotic genes, and may treat type 2 diabetes by restoring insulin secretion.</p>

<p>Elobixibat (A 3309) blocks IBAT in mice/humans/dogs (IC50: 0.13/0.53/5.8 nM); used for constipation research.</p>

<p>NSC-697923 inhibits UBE2N, triggers p53-dependent and JNK-mediated apoptosis, blocks DNA damage and NF-κB signaling in neuroblastoma cells.</p>

<p>GP 1a: potent CB2 receptor agonist (EC50=7.1), 30x CB2 over CB1 preference, boosts P-ERK1/2, aids skin healing, anti-inflammatory.</p>

<p>CDC801 is an inhibitor of PDE4 and TNF-α with IC50s of 1.1 μM and 2.5 μM, respectively.</p>

<p>AZA197 (AZA-197) is a selective Cdc42 inhibitor.</p>

Nanatinostat (CHR-3996) is an HDAC inhibitor with selectivity and oral bioavailability, for HDAC1/2/3 .anti-proliferation apoptosis.