Apoptosis

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

<p>cRIPGBM chloride is a pro-apoptotic derivative found in GBM cancer stem cells with anti-tumor activity, inducing caspase-1-dependent apoptosis.</p>

<p>Ciglitazone: potent PPARγ agonist, EC50 3 μM, oral hypoglycemic; reduces insulin, blood pressure, Th17 cells, VEGF; halts gastric cancer growth.</p>

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

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

PARP/PI3K-IN-1 is a PARP and PI3K dual inhibitor with anticancer and antiproliferative activities for the study of breast, pancreatic and lung cancers.

<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>NecroX-7 (LC-280126) is a potent free radical scavenger and a HMGB1 (high-mobility group box 1) inhibitor.</p>

<p>F16 ((E)-4-(3-indolylvinyl)-N-methylpyridinium iodide) inhibits the growth of neu-overexpressing cells and the proliferation of mammary epithelial.</p>

<p>Potent, oral Tubulin inhibitor 11 hinders polymerization, targets Colchicine site, induces mitotic block, and apoptosis.</p>

<p>CMLD-2 is a HuR-ARE inhibitor (Ki: 350 nM) that promotes apoptosis, has antitumor properties, and reduces thyroid cancer cell viability.</p>

<p>NM-3, an oral anti-angiogenic and anti-tumor agent, modulates radiation and blocks VEGF to curb endothelial growth and induce apoptosis.</p>

<p>Brigimadlin (BI 907828) is an orally active and highly potent antagonist of the E3 ubiquitin-protein ligase MDM2-p53 with antitumor activity.</p>

<p>iCRT-5 is a potent inhibitor of the Wnt pathway. iCRT-5 has antiproliferative activity and can be used in the study of multiple myeloma.</p>

<p>SLMP53-1 is a p53 activator with anti-tumor activity, activates reprogramming of glucose metabolism, and interferes with angiogenesis and migration</p>

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

<p>SB 699551 dihydrochloride is a 5-ht5a receptor antagonist.</p>

<p>Ro 90-7501, an amyloid β42 (Aβ42) protofibril and TPR-dependent PP5 inhibitor, is a novel cervical cancer cell radiosensitizer that inhibits HCMV.</p>

<p>Lanperisone (NK433) is a potent, long-lasting muscle relaxant that inhibits spinal reflexes via noradrenergic system suppression.</p>

<p>K-8012 is a modulator of the N-terminally truncated RXRα and improves anticancer activities in an RXRα-dependent manner.</p>

<p>SarCNU is an alkylating anticancer drug targeting prostate cancer through p53 pathways and selects P140K MGMT-transduced CD34(+) cells.</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>EM-12, a Thalidomide analogue, is more active, stable, and boosts rat colon cancer studies.</p>

<p>NSC49652 triggers apoptotic cell death dependent on p75NTR and JNK activity in neurons and melanoma cells, and inhibits tumor growth in a melanoma mouse model.</p>

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

<p>Bomedemstat (IMG-7289) is an LSD1 inhibitor for acute myeloid leukemia, MDS, and Myelofibrosis; induces apoptosis by regulating p53, PUMA, and BCLXL.</p>

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

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

<p>Ro24-7429: oral HIV-1 Tat antagonist, RUNX1 inhibitor with anti-HIV, antifibrotic, and anti-inflammatory properties.</p>

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

<p>W146 is an S1PR1 antagonist that induces a significant but transient decrease in blood lymphocytes in mice.</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>DB1976: Selenophene DB270 analog, inhibits PU.1 (IC50=10 nM), disrupts PU.1/DNA (KD=12 nM), induces apoptosis, cell-permeable.</p>

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

<p>MI-219 is a human double minute 2 (HDM2) inhibitor.</p>

<p>c-Met-IN-10: potent kinase inhibitor (IC50=16 nM), halts cancer cell activity/movement, induces apoptosis, for anticancer research.</p>

<p>Immunosuppressant-1 (Compound 31) suppresses T-cell proliferation triggered by anti-CD3/anti-CD28 co-stimulation and demonstrates immunosuppressive effects,</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>Nalmefene (ORF 11676) is a μ-opioid antagonist and partial κ agonist used to study opioid overdose and alcohol dependence.</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>MAO-B-IN-26 (Compound IC9) serves as both a MAO-B and acetylcholinesterase inhibitor.</p>

C 87: Small-molecule TNF-α inhibitor, binds TNFα, inhibits cytotoxicity with IC50 of 8.73 μM, blocks signaling.

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

<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>TC ASK 10 is a potent, selective and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1,IC50 = 14 nM). The IC50 value for ASK2 is 0.51 μM.</p>

<p>Agerafenib hydrochloride is a highly potent inhibitor of BRAFV600E (Kd: 14 nM).</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>INCB3619 is a selective and potent inhibitor of ADAM with antitumour effects, inhibiting ADAM10, ADAM17, MMP12 and MMP15.</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>BRD4 Inhibitor-18: potent (IC50: 110 nM), impairs MV-4-11 cell growth, disrupts G0/G1 phase, and induces apoptosis.</p>

<p>Pelcitoclax (APG-1252) is a powerful inhibitor of the Bcl-2 and Bcl-xl proteins, displaying significant antineoplastic and pro-apoptotic properties[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>NSC 689534 forms a chelate with copper (Cu 2+), resulting in the NSC 689534/Cu 2+ complex, which is a potent inducer of oxidative stress and exhibits antitumor activity [1].</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>BTM-3566 triggers ISR via OMA1, induces apoptosis in cancer cells, and is used to research DLBCL.</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>Zn(BQTC) inhibits mtDNA and nDNA, damages mitochondria/nuclei, triggers apoptosis, and targets A549R cancer cells.</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>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>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>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>A-1293102 is a potent, selective inhibitor of BCL-XL, effective in inducing apoptosis in tumor cells reliant on BCL-XL [1].</p>

<p>Lepadin E, a notably cytotoxic compound, effectively stimulates ferroptosis via the canonical p53-SLC7A11-GPX4 pathway.</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>CHM-1 is an inducer of apoptosis, and displays potent antitumor ability in human hepatocellular carcinoma by activation of Cdc2 kinase activity.</p>

<p>Q-VD-OPh: broad-spectrum, non-toxic caspase inhibitor; cost-effective, specific for apoptotic inhibition.</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>Siremadlin R Enantiomer is the R enantiomer of Siremadlin. Siremadlin is a potent and highly specific inhibitor of MDM-2/p53.</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>DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor on mitochondrial complex I function in galactose-containing media, resulting in reduced ATP.</p>

<p>Z-YVAD-CMK is an inhibitor of both caspase-1 and caspase-3, as referenced in [1].</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>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>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>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>SM-1295: IAP antagonist, Kd 3077 nM XIAP-BIR3, 3.2 nM c-IAP1-BIR3, 9.5 nM c-IAP2-BIR3.</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>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>CP-24879 HCl, a Δ5D/Δ6D dual-inhibitor, reduces liver lipid buildup and inflammation.</p>

<p>SCH79797 dihydrochloride is a PAR1 antagonist with IC50 70 nM, Ki 35 nM, antiproliferative, and pro-apoptotic properties.</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>Cerivastatin is an HMG-CoA reductase inhibitor with anticancer and lipid-lowering effects and can be used to study primary hyperlipidemia.</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>NBI-961, a potent NEK2 inhibitor, suppresses proteasomal degradation and effectively induces G2/mitosis arrest and apoptosis within diffuse large B cell</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>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>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>Ethylene glycol dimethacrylate, a methacrylate monomer, demonstrates cytotoxic and genotoxic impacts on human gingival fibroblasts (HGFs), elevating</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>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>BTM-3528 is a mitochondrial protease OMA1 activator that induces an overactivation of the mitochondrial integrated stress response (ISR).</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>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>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>