Apoptose

<p>MBM-55 is an effective inhibitor of NIMA related kinase 2 (NEK2) with an IC50 of 1 nM.</p>

<p>TL4-12 is a MAP4K2 (GCK) inhibitor that inhibits IL-1 and TGFβ-induced p38 MAPK phosphorylation in vitro.</p>

<p>BCP-T.A is an iron death inducer that acts by binding to GPX4.</p>

<p>Apostatin-1 (Apt-1) is a novel TRADD inhibitor. Apostatin-1 can bind to a pocket on the N-terminal TRAF2 binding domain of TRADD.</p>

<p>DX3-213B is a potent, orally active inhibitor of oxidative phosphorylation (OXPHOS) complex I with an IC50 of 3.6 nM.</p>

<p>Exisulind (CP248) triggers apoptosis via PKG activation, shows antitumor effects, and inhibits growth in various rodent cancer models.</p>

<p>BCL6-IN-7 (BCL6 inhibitor-7) is a BCL6 corepressor-interaction inhibitor with potential antitumor activity, used in lymphoma research.</p>

<p>Mepazine, a MALT1 inhibitor, blocks GSTMALT1 (IC50: 0.83μM) and GSTMALT1 325-760 (IC50: 0.42μM), promoting apoptosis and reducing cell viability.</p>

<p>GSK854 is a selective TNNI3K inhibitor reducing heart damage and stress post-infarction in mice.</p>

<p>TAI-1 is a potent and specific Hec1 inhibitor, which disrupts Hec1-Nek2 protein interaction.</p>

<p>N6-Cyclopentyladenosine (CPA) is a selective agonist of the adenosine A1 receptor and can be used to mimic the action of the adenosine A1 receptor, with Ki's of</p>

<p>Cot inhibitor-1 selectively blocks Tpl2 kinase, reducing TNF-alpha in blood (IC50: 5.7 nM). It may treat arthritis, IBD, and certain cancers.</p>

<p>AZA1 (Rac1/Cdc42-IN-1) is a potent dual inhibitor of Rac1 and Cdc42.</p>

<p>HS-276, a selective oral TAK1 inhibitor (Ki: 2.5 nM), also targets CLK2, GCK, ULK2, MAP4K5; potential for RA research.</p>

<p>R306465 (JNJ-16241199) is an HDAC 1 inhibitor with broad-spectrum anti-tumor activity, inducing apoptosis, and can be used to study solid tumors.</p>

<p>Vamotinib (PF-114) is a tyrosine kinase inhibitor with antiproliferative and antitumor activity.Vamotinib is used in the study of Alzheimer's disease.</p>

<p>Alethine is a small antitumor compound used to treat cancers and infections, boosting T-cell cytotoxicity by raising TNFα.</p>

<p>Etomoxir is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a) (IC50=5-20 nM), inhibits fatty acid oxidation. High-Quality, Low-Cost!</p>

<p>Epristeride (ONO-9302) is a steroidal 5-alpha-reductase isoform 2 inhibitor that inhibits SR isoform 2. Epristeride reduces prostate size.</p>

<p>The compound is a selective urokinase inhibitor (IC50 = 8.2 μM). It also inhibits clot lysis with no effect on clot formation.</p>

<p>HSK3486 is similar to propofol and is a general anesthetic, which may have therapeutic potential in insomnia, migraine, anxiety, analgesia, and other aspects.</p>

<p>Perphenazine dihydrochloride: Oral dopamine, histamine-1 antagonist; targets D2, D3, 5-HT2A, Alpha-1A; may treat psychiatric disorders, cancer.</p>

<p>Triciribine phosphate (VD 002) is an AKT inhibitor that inhibits neovascularization and can be used in the study of leukemia.</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>BHD, a reversible male contraceptive agent, effectively induces spermatogenic cell apoptosis and causes abnormalities in seminiferous tubules in vivo at doses</p>

<p>Lepadin E, a notably cytotoxic compound, effectively stimulates ferroptosis via the canonical p53-SLC7A11-GPX4 pathway.</p>

<p>Boserolimab (MK-5890) is a chimeric, humanized IgG1κ antibody that targets the signaling regulatory protein CD27 in mice.</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>RIPK1-IN-10 is a potent inhibitor of RIPK1.</p>

<p>BRD4 Inhibitor-18: potent (IC50: 110 nM), impairs MV-4-11 cell growth, disrupts G0/G1 phase, and induces apoptosis.</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>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>ZINC00784494 is a selective inhibitor of LCN2 (lipocalin-2), which inhibits cancer cell proliferation and reduces p-AKT , and promotes apoptosis. IBC.</p>

<p>TL02-59: Fgr inhibitor (IC50=0.03nM), also targets Lyn (0.1nM), Hck (160nM), halts acute myelogenous leukemia growth.</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>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>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>Antiproliferative Against-3 (comp 33) demonstrates significant activity against Hela (IC 50 = 0.21 µM), A549 (IC 50 = 0.39 µM), and MCF-7 (IC 50 = 0.33 µM) cell</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>Tubulin Polymerization-IN-56 (compound 8l), an indazole derivative, potently inhibits tubulin polymerization by targeting the colchicine site, which induces</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>Ataquimast is used in curing advanced receptor-positive breast cancer.</p>

<p>LSD1-IN-25: potent, selective oral LSD1 inhibitor; IC50=46 nM, Ki=30.3 nM; induces cancer cell apoptosis.</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>Methyl 12-methyltridecanoate ((R)-betaxolol hydrochloride), a biosurfactant derived from Brevibacterium casei LS14, enhances the biocompatibility of</p>

<p>Pivanex, an oral HDAC inhibitor, targets metastasis, angiogenesis, reduces Bcr-Abl protein, and promotes apoptosis.</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>BTM-3566 triggers ISR via OMA1, induces apoptosis in cancer cells, and is used to research DLBCL.</p>

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

<p>PARP-1-IN-3 is a potent PARP-1 inhibitor that inhibits PARP-1 and PARP-2 with IC50 values of 0.25 nM and 2.34 nM, respectively.PARP-1-IN-3 has potential anti-</p>

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

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

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

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

<p>Atiprimod Dimaleate is a JAK2 inhibitor.</p>

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

<p>AM-8735 is an inhibitor of MDM2 ( IC50: 25 nM).</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>EAD1 HCL is a potent autophagy inhibitor with antiproliferative activity in lung and pancreatic cancer cells. EAD1 HCL also induces apoptosis</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>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>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>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>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>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>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>BIX selectively induces BiP/GRP78 and ER chaperone, preventing cell death in neurons and retinas.</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>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>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>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>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>Zn(BQTC) inhibits mtDNA and nDNA, damages mitochondria/nuclei, triggers apoptosis, and targets A549R cancer cells.</p>

<p>Erythro-Austrobailignan-6: orally active, anti-cancer, inhibits DNA topoisomerases, induces apoptosis, boosts p38/JNK phosphorylation.</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>CPT-Se4, a seleno-derivative of CPT, effectively kills cancer cells, triggers apoptosis, and is cytotoxic against various cell lines.</p>

<p>GGTI2417 blocks Geranylgeranyltransferase I, targeting RalB for apoptosis and RalA to stop growth.</p>

<p>"HSP90/mTOR-IN-1 is a dual Hsp90/mTOR inhibitor (IC50: 69/29 nM), halting SW780 cell growth and inducing apoptosis/autophagy in cancer research."</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>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>Lepadin H, a marine alkaloid and ferroptosis inducer, exhibits significant cytotoxicity by promoting p53 expression, escalating ROS production, and enhancing</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>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>BTM-3528 is a mitochondrial protease OMA1 activator that induces an overactivation of the mitochondrial integrated stress response (ISR).</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>ERα antagonist 1 is a selective, potent, covalent estrogen receptor alpha (ERα) antagonist that blocks the cell cycle of MCF-7 cells in G0/G1 phase and induces</p>

<p>SD 1008 is a JAK2/STAT3 signaling pathway inhibitor. SD 1008 inhibits activation of STAT3, JAK2, and Src.</p>

<p>Falcarindiol: Activates PPARγ, boosts ABCA1, induces apoptosis/autophagy, has anti-inflammatory/anticancer effects.</p>

<p>eIF4A3-IN-9, a silvestrol analogue, disrupts eIF4F complex assembly; EC50s: 29/450/80 nM (myc/tub-LUC, MB-231 cells); for cancer research.</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>CHMFL-FLT3-122 is a potent and orally available FLT3 kinase inhibitor used to treat FLT3-ITD positive acute myeloid leukemia.</p>

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

<p>c-Met/HDAC-IN-3: dual inhibitor; IC50: c-Met 12.5 nM, HDAC1 26.97 nM; induces apoptosis, G2/M arrest.</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>Potent RIP2 kinase inhibitor with 0.03 μM IC50, selective for autoimmune disease treatment.</p>