Apoptosis

<p>Potent RIP2 kinase inhibitor with 0.03 μM IC50, selective for autoimmune disease treatment.</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>HDAC/JAK/BRD4-IN-1 (compound 25ap) is a potent triple inhibitor targeting HDAC, JAK, and BRD4.</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>Zn(BQTC) inhibits mtDNA and nDNA, damages mitochondria/nuclei, triggers apoptosis, and targets A549R cancer cells.</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>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>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>Lepadin E, a notably cytotoxic compound, effectively stimulates ferroptosis via the canonical p53-SLC7A11-GPX4 pathway.</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>SW IV-52 is an XIAP-inhibitor that acts as a second mitochondria-derived activator of caspases (SMAC) mimetic.</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>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>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>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>Bcl-2-IN-13 is a potent inhibitor of Bcl-2, exhibiting an IC50 of 17 nM, and holds potential for use in cancer research [1].</p>

<p>Mcl-1 Inhibitor 13 (Example 9), with a Ki of 8.2 nM, serves as an MCL-1 inhibitor suitable for cancer research [1].</p>

<p>Thaspine: inhibits topoisomerase IB, reduces VEGF, stops endothelial cell growth via PI3K/MAPK pathways.</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>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>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>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>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>Bcl-2-IN-12 (Compound 1) is a potent Bcl-2 inhibitor with an IC50 value of 6 nM, utilized in cancer research [1].</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>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>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>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>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>IK-862 is a selective TACE inhibitor with potential anti-inflammatory and anticancer activity for the study of neuritis.</p>

<p>Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride), a biosurfactant derived from Brevibacterium casei LS14, enhances the biocompatibility of</p>

<p>Ataquimast is used in curing advanced receptor-positive breast cancer.</p>

<p>eIF4A3-IN-17, a silvestrol analogue, disrupts eIF4F assembly; EC50: 0.9-15 nM. Used in cancer pathogenesis research.</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>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>RIP2 kinase inhibitor 2 is a receptor-interacting protein-2 kinase inhibitor.</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>WEHI-345 analog is an Src inhibitor.</p>

<p>Tubulin Polymerization-IN-56 (compound 8l), an indazole derivative, potently inhibits tubulin polymerization by targeting the colchicine site, which induces</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>GSK2245035: selective nasal TLR7 agonist, boosts Type-1 IFN (pEC50: 9.3 IFNα, 6.5 TFNα), curbs Th2 cytokines in blood cultures.</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>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>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>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>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>AT-9283 L-lactate is an inhibitor of aurora kinase.</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>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>SAFit1 is an inhibitor of FK506 binding protein 51 (FKBP51)-specific (Ki: 4±0.3 nM).</p>

<p>BAX-IN-1 is a potential selective inhibitor of Bcl-2-associated X protein (BAX).</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>BMS-561392 (DPC333) is a tumor necrosis factor-α ( TNF-α) Invertase inhibitor.</p>

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

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

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

<p>PP5-IN-1 is a serine/threonine protein phosphatase-5 (PP5) inhibitor with potential anticancer activity that induces apoptosis in cancer cells.</p>

<p>CDDO-2P-Im shows chemopreventive effect and reduces the size and severity of the lung tumors in the mouse lung cancer model.</p>

<p>CDDO-3P-Im is an orally active inhibitor of necroptosis with chemopreventive effects. CDDO-3P-Im can be used in studies about ischemia/reperfusion.</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>Alrizomadlin is an orally active MDM2 inhibitor. APG-115 shows significant dose-dependent inhibitory effects on TP53wt AML cell lines.Cost-effective and quality-assured.</p>

<p>VU0661013 is an effective and selective inhibitor of MCL-1.</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>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>

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

<p>M3541: an oral ATM inhibitor with antitumor effects, hinders DNA repair and promotes cancer cell death.</p>

<p>JHU395, an oral prodrug of glutamine antagonist DON, shows stable antitumor effects on MPNST in vitro and vivo.</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>PARP1/2/TNKS1/2-IN-1 is a multi-target inhibitor of PARP-1, PARP-2, TNKS1 and TNKS2.PARP1/2/TNKS1/2-IN-1 has anti-tumor activity and induces apoptosis.</p>

<p>Nanatinostat (CHR-3996) is an HDAC inhibitor with selectivity and oral bioavailability, for HDAC1/2/3 .anti-proliferation apoptosis.</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>CPI-360 is a small molecule EZH2 inhibitor (IC50: 0.002 μM, EC50: 0.080 μM) that shows antitumor activity in an EZH200-dependent tumor xenograft model.</p>

<p>GCN2-IN-7 is an inhibitor of the environmental sensing protein GCN2 with antitumor activity for the study of melanoma.</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>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>Elobixibat (A 3309) blocks IBAT in mice/humans/dogs (IC50: 0.13/0.53/5.8 nM); used for constipation research.</p>

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

<p>HM43239: oral FLT3 inhibitor; IC50: FLT3 WT 1.1nM, ITD 1.8nM, D835Y 1.0nM; blocks p-STAT5/p-ERK; affects SYK, JAK1/2, TAK1; halts leukemia cell growth.</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>GLUT-1-IN-4 (Compound 13) is an inhibitor of the GLUT-1 glucose transporter that depends on the p53 protein. It suppresses the proliferation of various cancer cells at submicromolar IC50 levels. Additionally, GLUT-1-IN-4 can halt the cell cycle, induce oxidative stress, and promote apoptosis (cell death).</p>

<p>RET-IN-11 selectively inhibits RET (IC50: 6.20 nM), promotes apoptosis, and hinders cell proliferation and migration.</p>

<p>Lepidozin G blocks cancer growth (IC50=4.2-5.7μM) and triggers apoptosis in PC-3 cells via mitochondria.</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>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>Bomedemstat (IMG-7289) hydrochloride, an oral LSD1 inhibitor, has anticancer properties, blocking cell growth and triggering apoptosis.</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>PF-3837 is an inhibitor of the Mps1 kinase, with a Ki value of 0.33 nM and an IC50 value of 5.5 nM. It disrupts cell cycle checkpoints by inhibiting the catalytic activity of Mps1, thereby reducing genomic stability and leading to cancer cell apoptosis (Apoptosis). PF-3837 is utilized in the study of breast cancer.</p>

<p>Tubulin polymerization-IN-68 (compound 32) serves as a tubulin inhibitor, disrupting cellular microtubule networks by hindering tubulin polymerization. It also upregulates PARP-1 and caspase-3 expression, thereby inducing apoptosis and exhibiting anticancer properties. Notably, Tubulin polymerization-IN-68 effectively suppresses HepG2 cells with an IC50 of 93 nM and markedly reduces the growth of HepG2 xenograft tumors in nude mice through oral administration.</p>

<p>Mps-BAY1, an MPS1 inhibitor, exhibits anticancer activity. It inhibits cell proliferation and induces cell apoptosis by activating mitotic aberrations in cancer cells, leading to overall aneuploidy and polyploidy. Mps-BAY1 is used in research pertaining to colorectal and cervical cancer.</p>

<p>BCL6-IN-9 (compound 1) is a potent inhibitor of B-cell lymphoma 6 protein (BCL6) (IC50: 3.9 nM) and can be used to study cancer.</p>

<p>HDL-16 is a highly effective P2Y14R antagonist with anti-colitis effects, targeting P2Y14R in intestinal epithelial cells to alleviate ulcerative colitis.</p>

<p>ONC213, an αKGDH inhibitor, functions by hindering αKGDH activity, thus suppressing mitochondrial respiration and elevating α-ketoglutarate levels, ultimately inducing apoptosis (Apoptosis) in AML cells. It is utilized in the study of acute myeloid leukemia.</p>

<p>Cernuumolide J (TMJ-105) functions as a JAK2/STAT3 inhibitor and exhibits potent activity against HEL leukemia cells by inhibiting their growth in both time-dependent and concentration-dependent manners, with an IC 50 value of 1.79 μM. This compound effectively induces G2/M phase arrest and apoptosis by downregulating the phosphorylation of JAK2, STAT3, and Erk, while simultaneously upregulating the phosphorylation of JNK and p38 MAPK. Cernuumolide J holds potential for research applications in anti-cancer therapy.</p>

<p>Anticancer agent 65: Effective on A549 cells, IC50 1.07 μM, halts S phase, triggers apoptosis, elevates p53/p21, causes ROS and MMP collapse.</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>

<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>