Apoptosis

<p>1G244 is an inhibitor of DPP8/9 with antiatherosclerotic and antimyeloma properties.</p>

<p>UCB-5307 inhibits TNFR1, binds TNFα with 9 nM KD, shows slow kinetics (KD=6 nM), and penetrates hTNF/hTNFR1 complexes.</p>

<p>AQ4 is a topoisomerase II inhibitor and DNA-inserting agent that inhibits proliferation and induces apoptosis in two cell lines.</p>

<p>EB1 is an MNK kinase inhibitor that inhibits cancer cell growth, promotes apoptosis, and inhibits eIF4E phosphorylation.</p>

<p>Antifolate C2 (AGF 154) inhibits tumor growth with 0.14 nM IC, useful in cancer/autoimmune research.</p>

<p>TNIK-IN-3 is a highly potent and orally active inhibitor of Traf2- and Nck-interacting protein kinase (TNIK).</p>

<p>RS1-PDK1 inhibitor (RS 1) is a selective inhibitor of the protein kinase PDK1 that can be used to treat and prevent disease or disorders.</p>

<p>Necrostatin-5 (Nec-5) inhibits RIP1 kinase, prevents cell necrosis, and protects Fadd-deficient Jurkat cells with an EC50 of 240 nM.</p>

<p>T025 inhibits CLK1-4 (Kds: 0.074-6.5 nM), shows anti-cancer effects (IC50: 30-300 nM), useful for MYC-related disease research.</p>

<p>HS38: DAPK-specific ATP-competitive inhibitor; Kds: DAPK1 (300 nM), PIM3 (200 nM), ZIPK (280 nM); useful in smooth muscle disorder research.</p>

<p>CBS9106 (SL-801) is a CRM1 inhibitor with CRM1-degrading and anti-tumor activity that inhibits CRM1-dependent nuclear export.</p>

<p>SYM 2081: Kainate receptor agonist, IC50 of 35 nM, depolarizes muscle, lowers EPSP amplitude.</p>

<p>Dasatinib hydrochloride is an oral Src/Bcr-Abl inhibitor with potent antitumor effects, Ki values of 16 pM (Src) and 30 pM (Bcr-Abl).</p>

<p>SCFSkp2-IN-2, a Skp2 inhibitor, exhibits a dissociation constant (K_D) of 28.77 μM.</p>

<p>NLRP3/AIM2-IN-3 selectively blocks NLRP3/AIM2 inflammasomes; IC50 for cell lysis is 0.077 μM, disrupting ASC oligomerization.</p>

<p>AOH1160 is an inhibitor of proliferating cell nuclear antigen (PCNA).</p>

<p>Tiomolibdate diammonium (NSC-286644) blocks SOD1 and COX, acting as an antiangiogenic and antitumor agent.</p>

<p>D609 (Tricyclodecan-9-yl-Xanthogenate) has antiviral and antiproliferative activities.D609 acts through competitive inhibition of PC, PC-P and SMS.</p>

<p>EM-12, a Thalidomide analogue, is more active, stable, and boosts rat colon cancer studies.</p>

<p>GS-9191 is a potent inhibitor of DNA polymerase alpha and ß , a prodrug of the novel nucleoside analogue 9-(2-phosphonomethoxyethyl)guanine (PMEG) , which</p>

<p>DCG066 is an inhibitor of lysine methyltransferase G9a with anticancer activity and may be used in the study of leukemia.</p>

<p>CCT020312 (0-9 µM, 24 h) treatment of medium HT29 cells for 24 h resulted in a concentration-dependent loss of P-S608-pRB.Cost-effective and quality-assured.</p>

<p>Stemazole activates human stem cell growth, boosts survival, reduces cell death, and aids myelin repair, with therapeutic potential in demyelinating diseases.</p>

<p>Boserolimab (MK-5890) is a chimeric, humanized IgG1κ antibody that targets the signaling regulatory protein CD27 in mice.</p>

<p>IK-862 is a selective TACE inhibitor with potential anti-inflammatory and anticancer activity for the study of neuritis.</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>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>EAD1 HCL is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 HCL also induces apoptosis</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>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>Immunosuppressant-1 (Compound 31) suppresses T-cell proliferation triggered by anti-CD3/anti-CD28 co-stimulation and demonstrates immunosuppressive effects,</p>

<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>RIP2 kinase inhibitor 2 is a receptor-interacting protein-2 kinase inhibitor.</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>Prostaglandin A1, a dehydration derivative of Prostaglandin E1, demonstrates inhibitory effects on tumor growth, inflammation, virus replication, platelet aggregation, and excitotoxin-induced neuron apoptosis [1].</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>Tubulin Polymerization-IN-56 (compound 8l), an indazole derivative, potently inhibits tubulin polymerization by targeting the colchicine site, which induces</p>

<p>WYE-125132: potent mTOR inhibitor, IC50 0.19 nM, selective over PI3Ks/hSMG1/ATR.</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>CP-24879 HCl, a Δ5D/Δ6D dual-inhibitor, reduces liver lipid buildup and inflammation.</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>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>RUNX-IN-2 (Compound Conjugate 3) covalently attaches to RUNX-binding sequences, preventing RUNX proteins from associating with their targets, thereby inhibiting</p>

<p>Docebenone is a selective and orally active inhibitor of 5-LO.</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>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>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>Nalmefene (ORF 11676) is a μ-opioid antagonist and partial κ agonist used to study opioid overdose and alcohol dependence.</p>

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

<p>IM156, a Metformin derivative, activates AMPK, enhances cognition in aging animals, and inhibits OXPHOS in solid tumor research.</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>NSC 48160 is an anti-pancreatic cancersmall molecule that inhibits growth and enhance apoptosis of pancreatic cancer cells through the mitochondrial pathway.</p>

<p>Merodantoin induces apoptosis in KRAS-mutant cancer cells via ROS-autophagy and Akt pathway.</p>

<p>GNE-900 is an ATP-competitive ChK1 inhibitor with selective and oral activity.GNE-900 inhibits ChKl and ChK2 with IC50 values of 0.0011 and 1.5 µM, respectively</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>Siremadlin R Enantiomer is the R enantiomer of Siremadlin. Siremadlin is a potent and highly specific inhibitor of MDM-2/p53.</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>BI-0252 is an inhibitor of MDM2-p53 (IC50:4 nM).</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>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>LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.</p>

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

<p>RIPK-IN-4 is an effective and selective inhibitor of RIPK2. It also has excellent oral bioavailability (IC50: 3 nM).</p>

<p>Protein kinase D (PKD), a serine/threonine protein kinase activated by diacylglycerol downstream of PKC signaling, has three human isoforms that modulate cell proliferation, survival, invasion, and protein transport. CRT0066101 acts as an inhibitor of these three PKD isoforms, with IC50 values of 1, 2.5, and 2 nM for PKD1, PKD2, and PKD3, respectively. It demonstrates selectivity for PKD over a range of more than 90 protein kinases, including PKCα, PKBα, MEK, ERK, c-Raf, c-Src, and c-Abl. This specificity allows CRT0066101 to inhibit cell proliferation, induce apoptosis, and notably reduce the viability of pancreatic cancer cells both in vitro and in vivo.</p>

<p>Mezigdomide (CC-92480) is a potent, novel cereblon E3 ubiquitin ligase modulator (CELMoD) that acts as a molecular glue.Cost-effective and quality-assured.</p>

<p>BAX-IN-1 is a potential selective inhibitor of Bcl-2-associated X protein (BAX).</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>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>HDAC-IN-59 (compound 13a), a potent histone deacetylase (HDAC) inhibitor, enhances intracellular reactive oxygen species (ROS) production, induces DNA damage,</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>

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

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

<p>CR-1-31-B, a synthetic rocaglate, inhibits eIF4A, hinders protein synthesis initiation, and induces apoptosis in cancer cells.</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>CNDAC, a nucleoside analog, is a major metabolite of oral drug sapacitabine.</p>

<p>Ferroptocide is a thioredoxin inhibitor that induces iron death in cancer cells and can be used in breast cancer research.</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>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>SM-1295: IAP antagonist, Kd 3077 nM XIAP-BIR3, 3.2 nM c-IAP1-BIR3, 9.5 nM c-IAP2-BIR3.</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>Potent RIP2 kinase inhibitor with 0.03 μM IC50, selective for autoimmune disease treatment.</p>

<p>Q-VD-OPh: broad-spectrum, non-toxic caspase inhibitor; cost-effective, specific for apoptotic inhibition.</p>

<p>Antitumor agent-60 inhibits growth by targeting RAS-RAF, binding CRAF (Kd: 721.3 nM), boosting p53/ROS, causing apoptosis, and arresting G2/M phase.</p>

<p>FGFR-IN-8, potent oral FGFR inhibitor for wild-type/mutant types, induces apoptosis with anti-cancer properties.</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>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>INI-43 targets Kpnβ1, disrupting nuclear transport in cervical/esophageal cancers, affecting NFAT, NFκB, AP-1, NF localization.</p>

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

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

<p>MS-177 is a PROTAC EZH2 degrader that promotes cholangiocarcinoma growth through the EZH2-mediated WNT7B/β-catenin pathway.</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>Topoisomerase II inhibitor 15 (compound 2g) serves as a potent apoptotic inducer, exhibiting heightened selectivity for head and neck tumors [1].</p>

<p>BRD4 Inhibitor-18: potent (IC50: 110 nM), impairs MV-4-11 cell growth, disrupts G0/G1 phase, and induces apoptosis.</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>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>PARP1-IN-14 (compound 19k) is a potent PARP1 inhibitor demonstrating an inhibition concentration (IC50) of 0.6 ± 0.1 nM.</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>