Apoptose

<p>PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reducing the methylation level of its substrate BAF155. This PROTAC degrader works by degrading IKZF 1/3 via a CRBN-dependent mechanism. It suppresses MYC protein expression, thereby inhibiting the proliferation of various multiple myeloma cells. Additionally, PROTAC CARM1/IKZF3 degrader-1 can induce apoptosis in H929 cells and overcomes resistance to immunomodulatory drugs (IMiDs, such as pomalidomide). It is applicable for cancer and immunology research. (Pink: ligand for target protein CARM1/IKZF3 ligand 1; Active form of target protein ligand: EZM 2302; Black: linker; Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride)</p>

<p>VEGFR-2-IN-53 (Compound 15w) is an inhibitor of VEGFR-2 with an IC50 value of 4.34 μM. It induces cell apoptosis (Apoptosis) and inhibits angiogenesis by blocking VEGFR-2 activity and preventing cell migration. Additionally, it shows an IC50 of 3.87 μM in inhibiting the growth of MCF-7 cells, making it pertinent for research in cancer therapeutics.</p>

<p>LL-K9-3, a selective hydrophobic tagging technology (HyT)-based degrader, specifically targets the CDK9-cyclin T1 complex, displaying DC50 values of 589 nM for</p>

<p>CIGB-300 acetate (P15-Tat acetate) is a peptide that acts as an inhibitor of casein kinase 2 (CK2). It exhibits anticancer properties by disrupting the phosphorylation activity of CK2. CIGB-300 acetate induces apoptosis in various tumor cell lines and is applicable for cancer research.</p>

<p>Thalidomide 4'-oxyacetamide-alkyl-C2-amine HCl is an E3 ligase ligand-linker conjugate containing the E3 ubiquitin ligase cereblon (CRBN) and linker.</p>

<p>Lorigerlimab (MGD019) is a bispecific IgG4 DART that blocks PD-1/CTLA-4, enhancing T-cells for mCRPC research.</p>

<p>KRAS inhibitor-40 (Compound 41) is an inhibitor of KRAS, disrupting the KRAS G12C-BRAF complex and suppressing the phosphorylation of the downstream ERK signaling pathway. This compound also inhibits the proliferation of tumor cells with various KRAS mutations, exhibiting antitumor activity.</p>

<p>Amino acids 17-41 of lactoferrin, lactoferricin B, enhance anti-fungal effects, targeting Candida Albicans.</p>

<p>DB2313 is a potent PU.1 inhibitor (IC50=14 nM) that disrupts gene binding, induces AML cell apoptosis, and has anticancer properties.</p>

<p>PH14, a dual PI3K/HDAC inhibitor, demonstrates potent inhibition with IC50 values of 20.3 nM for PI3Kα and 24.5 nM for HDAC3.</p>

<p>Lisaftoclax, an oral Bcl-2/Bcl-xl inhibitor (IC50: 2 nM &amp; 5.9 nM), treats CLL by promoting leukemia cell death.</p>

<p>F1324: potent BCL6 inhibitor, IC50=1nM, binding t1/2=441s, strongly inhibits BCL6 PPI.</p>

<p>Ferroptosis-IN-17 (Compound 18) is an inhibitor of ferroptosis with an EC50 value of 0.57 μM. It effectively reduces the accumulation of intracellular ferrous ions and lipid peroxidation while restoring levels of glutathione (GSH) and glutathione peroxidase 4 (GPX4). In rat plasma, Ferroptosis-IN-17 demonstrates good solubility and notable metabolic stability. This compound holds potential for research in tumor suppression, neurodegenerative diseases, and cardiovascular disorders.</p>

<p>Thalidomide-O-C8-NH2 is a synthetic cereblon ligand &amp; PROTAC linker, serving as an E3 ligase ligand-linker.</p>

<p>HYS-072 is an orally active derivative of chrysin with antitumor properties. It induces apoptosis (Apoptosis) and autophagy (Autophagy) by inhibiting the PI3K/AKT/mTOR signaling pathway, and suppresses tumor growth in xenograft models in vivo by modulating autophagy-related pathways. HYS-072 is applicable for research in treating triple-negative breast cancer.</p>

<p>GDCNF-11, an HSP90-based HIM-PROTACGPX4 degrader, facilitates the ubiquitination and degradation of GPX4 through the HSP90 chaperone complex. This reduction in endogenous GPX4 induces ferroptosis in HT-1080 cells, with a DC50 value of 0.08 μM.</p>

<p>DD0-2363 (Compound 32d) is a dual-target inhibitor of WDR5-MLL1/HDAC. It can suppress the proliferation of acute myeloid leukemia cells and induce apoptosis. With its antitumor properties, DD0-2363 is applicable for research on acute myeloid leukemia.</p>

<p>Ferroptosisinducer 6 (6d) is an inducer of ferroptosis (ferroptosis) that exhibits potent potential for Type I/II photodynamic therapy by inducing ROS production, oxidative stress, and mitochondrial damage. Additionally, it demonstrates antitumor activity.</p>

<p>Bcl-2-IN-4: potent, selective, oral Bcl-2 inhibitor with 1.5 nM IC50, &gt;200x selectivity over Bcl-xL.</p>

<p>Angiogenesis Inhibitor 3 (compound 8) is a potent anti-cancer agent, blocking HUVEC/HCT-15 cell growth and inducing apoptosis.</p>

<p>This Bim peptide belongs to the pro-apoptotic group of the Bcl-2 family of proteins.</p>

<p>NCT-58 is a potent HSP90 inhibitor that blocks Akt, downregulates HER family, and induces apoptosis in HER2+ breast cancer without triggering HSR.</p>

<p>Pimivalimab (JTX-4014), a PD-1 inhibitor, is utilized in solid tumor research [1].</p>

<p>Fludarabine triphosphate inhibits key enzymes, causing cell death.</p>

<p>Anticancer Agent 157 (compound 15) is a nitric oxide (NO) inhibitor with IC50 values of 0.62 μg/mL, exhibiting both anti-inflammatory and anticancer effects.</p>

<p>Xylopine: an aporphine alkaloid, cytotoxic to cancer cells, induces oxidative stress, G2/M arrest, and apoptosis.</p>

<p>cis-Clovamide is a naturally occurring phenolic compound with noteworthy antioxidant, anti-inflammatory, and antiapoptotic properties.</p>

<p>Azalamellarin N is a pyroptosis inhibitor that exhibits varying inhibitory effects on different pyroptosis inducers. It functions by targeting molecules upstream of NLRP3 inflammasome activation, instead of directly affecting the components of the NLRP3 inflammasome. Its inhibitory potency against various inducers is ranked as follows: Nigericin &gt; R837 [1].</p>

<p>FKBP12 Ligand-Linker Conjugate 1 is a complex comprising a target protein ligand for FKBP12 and a linker, which is utilized in the synthesis of the PROTAC degrader MC-25B.</p>

<p>Lenercept (Ro 45-2081) is a recombinant fusion protein combining the soluble TNF-receptor (p55) with the Fc portion of human IgG1 [1].</p>

<p>Anti-inflammatory agent 42 has anti-inflammatory activity and inhibits the expression of TNF-α and IL-6 in LPS-stimulated macrophages.</p>

<p>USP7-IN-9 is a potent USP7 inhibitor (IC50 = 40.8 nM), induces apoptosis, arrests RS4;11 cells, and modulates key oncoproteins.</p>

<p>EATC, a tetracycline byproduct, combats Pseudomonas to E. coli with MIC50s of 0.75-16 mg/L.</p>

<p>Thalidomide-NH-PEG2-COOH: a synthesized E3 ligase ligand-linker with cereblon ligand and PROTAC linker.</p>

<p>S-Adenosyl-L-methionine (Ademetionine) is an intermediate metabolite of methionine,for treatment of primary biliary cirrhosis and major depressive disorder.</p>

<p>Antitumor Agent-64 (Compound 8d), a diosgenin derivative, exhibits potent cytotoxic activity against the A549 cell line and induces apoptosis in A549 cells</p>

<p>Compound Ir5 (Antitumor agent-145) serves as a tumor inhibitor characterized by significant fluorescence and mitochondrial targeting. It promotes anti-cancer activity by inducing necroptosis and stimulating the necroptosis-related immune response [1].</p>

<p>Cefatrizine inhibits eEF-2 kinase, affecting apoptosis, autophagy, and ER stress in cancers.</p>

<p>FC-116 is a potent Tubulin inhibitor with antitumour activity and inhibits tumour growth in mice.FC-116 induces apoptosis and promotes protein degradation.</p>

<p>Voreloxin (SNS-595) is a potent Topoisomerase II inhibitor with broad-spectrum anti-tumor activity. Phase 2.</p>

<p>SHP1 activator 1 (Compound 3n) is an activator of protein tyrosine phosphatase 1 containing the src homology-2 domain (SHP1), with an EC50 of 17.66 μM. It inhibits the proliferation of ABC-DLBCL cells and induces apoptosis by suppressing the STAT3 signaling pathway. In MDA-MB-231 cells, SHP1 activator 1 emits blue and green fluorescent signals, making it suitable as a cellular imaging agent.</p>

<p>Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.</p>

<p>Odoroside A, from Nerium oleander leaves, induces cancer cell death via ROS/p53, causing apoptosis and cell cycle arrest.</p>

<p>DB818 dihydrochloride is the dihydrochloride salt form of DB818. It acts as an inhibitor of Homeobox A9 (HOXA9). By reducing the formation of the HOXA9-DNA complex, DB818 dihydrochloride inhibits the growth of AML cell lines OCI/AML3, MV4-11, and THP-1 and induces cell apoptosis (apoptosis).</p>

<p>p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a interaction inhibitor between p53 and MDM2 proteins.</p>

<p>Pralnacasan blocks IL-18, IL-1β, IFN-γ. It’s a potent oral enzyme inhibitor with use in arthritis therapy (Ki: 1.4 nM).</p>

<p>PB28: A potent σ2 agonist (Ki 0.68 nM), σ1 antagonist (Ki 0.38 nM), with anti-tumor properties and inhibits SARS-CoV-2 interactions.</p>

<p>CDK/HDAC-IN-4 is a highly selective dual inhibitor of cyclin-dependent kinase (CDK) and histone deacetylase (HDAC), with IC50 values of 88.4 nM and 168.9 nM, respectively. This compound exhibits antiproliferative effects in both hematologic and solid tumor cells. Additionally, CDK/HDAC-IN-4 induces apoptosis and S-phase cell cycle arrest in MV-4-11 cells. It has also demonstrated significant antitumor efficacy in an MV-4-11 xenograft model.</p>

<p>Antiproliferative Agent-25 (Compound 3s4) is a selective PRMT5 inhibitor displaying an IC50 of 0.11 μM.</p>

<p>AZD5582 TFA is a potent IAP antagonist that binds to the BIR3 domain of cIAP1, cIAP2, and XIAP with IC50 values of 15, 21, and 15 nM, respectively.AZD5582 TFA</p>