Apoptosis

<p>Fuscin, a quinonoid from O. fuscum, inhibits ADP/ATP translocase, depletes glutathione, disrupts NADH oxidation, and blocks MIP-1α/CCR5 binding (IC50: 21µM).</p>

<p>INF 195 is an inflammasome NLRP3 inhibitor that can be used to study myocardial ischemia and myocardial infarction.</p>

<p>Thalidomide-Piperazine-PEG3-NH2: a cereblon ligand-linker for PROTAC E3 ligase recruitment.</p>

<p>KWCN-41, a RIPK1 inhibitor with 88 nM IC50, blocks necrosis, spares apoptosis, and is anti-inflammatory.</p>

<p>MS105 is an orally active, selective protein tyrosine kinase 6 (PTK6) PROTAC degrader. It recruits the VHL E3 ligase through a VHL ligand fragment, facilitating ubiquitination and proteasomal degradation of PTK6, thereby inhibiting the proliferation and migration of breast cancer cells and inducing apoptosis (apoptosis). MS105 is a promising compound for breast cancer research.</p>

<p>FGA139 is an inhibitor of cysteine proteases, specifically targeting cathepsin B and L with IC50 values of 4.98 μM and 3.14 μM, respectively. It reduces the production of NO in LPS-induced RAW264.7 cells and lowers TNFα levels in microglia, demonstrating antioxidant and anti-inflammatory properties. Additionally, FGA139 enhances the secretion of neuroprotective metabolites such as purines and linoleic acid in LPS-stimulated microglia. This compound is applicable in the study of neuroinflammatory diseases.</p>

<p>VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.</p>

<p>MKC-1 (Ro-31-7453) is an oral bisindolylmaleimide inhibitor that disrupts tubulin polymerization, potentially halting cancer cell division.</p>

<p>ASR-488, an activator of the mRNA-binding protein CPEB1, promotes apoptosis and suppresses the growth of bladder cancer [1].</p>

<p>Zeluvalimab (AMG-404) is a monoclonal antibody designed to target the PD-1 receptor, and is utilized in cancer research [1].</p>

<p>Dehydrobruceine B, from Brucea javanica, enhances Cisplatin-induced apoptosis by affecting AIF, Bax, and Keap1-Nrf2.</p>

<p>HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/</p>

<p>OICR12694 (JNJ-65234637) TFA, an orally active B cell lymphoma 6 (BCL6) inhibitor [1], demonstrates effectiveness in targeting BCL6 pathways.</p>

<p>Thalidomide-O-PEG4-NHS ester is a polyethylene glycol (PEG)-based linker, commonly employed for the synthesis of proteolysis-targeting chimeras (PROTACs)[1].</p>

<p>Vinepidine (LY-119863) sulfate, a derivative of vincristine, exhibits antitumor activity .</p>

<p>Tubulin polymerization-IN-67 (Compound 5h) serves as an inhibitor of microtubule protein polymerization at the colchicine binding site, exhibiting an IC50 value of 2.92 μM. It effectively inhibits the proliferation of various cancer cell lines including HT29, A549, U2OS, MG-63, and HeLa, with IC50 values ranging from 0.12 to 4.13 μM. Additionally, Tubulin polymerization-IN-67 induces cell cycle arrest at the G2/M phase and triggers apoptosis in U2OS cells. It also inhibits cell migration in A549 and reduces mitochondrial membrane potential (MMP) while increasing intracellular ROS levels, thereby suppressing angiogenesis in HUVEC cells. Furthermore, this compound demonstrates antitumor activity in mice.</p>

<p>Thalidomide-based E3 ligase ligand for PROTAC degrader MI-389 synthesis, linked to cereblon and Boc.</p>

<p>Human PD-L1 inhibitor III is a human PD-L1 inhibitor.</p>

<p>Thalidomide derivative for CRBN protein recruitment, used in PROTACs production for protein degradation.</p>

<p>Anticancer agent 104 has anticancer activity, and induces cancer cell apoptosis [1] .</p>

<p>TAS-117, a PKB/Akt inhibitor, is used potentially for the treatment of solid tumors.</p>

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

<p>BIO8898: potent CD40-CD154 inhibitor, IC50 of 25 µM, prevents CD40L-induced apoptosis.</p>

<p>Bromoiodoacetamide (I-HAcAm): cytotoxic, induces ROS &amp; apoptosis in HepG-2 cells.</p>

<p>SC-2001 inhibits MCL-1 and STAT3, enhances SHP-1, induces apoptosis in breast cancer, and counters STAT3-driven sorafenib resistance in liver cancer.</p>

<p>KP1019 is now discontinued.</p>

<p>eIF4A3-IN-7: Potent eIF4A3 inhibitor, potential cancer/dysproliferation research (WO2019161345A1, Compound 8).</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>JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.</p>

<p>BODIPY FL thalidomide is a fluorescent probe that binds human cereblon protein with high affinity, exhibiting a dissociation constant (Kd) of 3.6 nM [1].</p>

<p>Fac-[Re(CO)3(L3)(H2O)][NO3] (Compound 3), a rhenium(I) tricarbonyl aqua complex, acts as an anticancer agent through the induction of mitochondrial dysfunction.</p>

<p>Thalidomide-Piperazine 5-fluoride hydrochloride, a derivative of the cereblon (CRBN) inhibitor Thalidomide, serves as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase), facilitating the synthesis of PROTACs [1].</p>

<p>(R)-HTS-3 is a LPCAT3 inhibitor that remodels the polyunsaturated phospholipid content of human cells and prevents iron death.</p>

<p>Diprovocim-1: TLR1/2 agonist; triggers TNF-α in THP-1 cells; boosts ovalbumin IgG1 &amp; CTLs against tumors with anti-PD-L1 in mice.</p>

<p>Conjugated 18-C ω-6 fatty acid from Jacaranda seeds, induces cancer cell apoptosis via oxidative stress; metabolizes to cytotoxic CLA.</p>

<p>MG-C-30 is an orally active CD27 agonist with an EC50 of 0.84 μM. It activates co-stimulatory signaling in NK cells and T cells, thereby enhancing the immune response. In the EG7-OVA mouse model, MG-C-30 demonstrates antitumor activity.</p>

<p>Terrain (NSC 291308), a fungal metabolite, reduces age-related inflammation via Nrf2/ERK1/2/HO-1 and inhibits IL-6 in human fibroblasts.</p>

<p>SM-164 Hydrochloride: Smac mimetic, cell-permeable, binds XIAP BIR2 and BIR3, IC50 of 1.39 nM, potent XIAP antagonist.</p>

<p>Compound B12, a JOA derivative, collapses MMP to induce apoptosis, inhibits cloning/migration, and has an IC50 of 0.39 μM against HGC-27 cells.</p>

<p>Mcl-1 Inhibitor 15 (Compound (Ra)-15), with a K i of 0.02 nM, is utilized in cancer research [1].</p>

<p>PD-1/PD-L1-IN-48 (compound HD10) is an effective inhibitor of the PD-1/PD-L1 interaction, exhibiting an IC50 of 3.1 nM. It plays a vital role in cancer research.</p>

<p>BcI-2/BcI-xI ligand 1, functioning as a BcI-2/BcI-xI ligand, is utilized in the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 .</p>

<p>RET Ligand-Linker Conjugate-1 consists of a complex formed by a RET ligand and a linker, which can be utilized in the synthesis of QZ2135.</p>

<p>Necroptosis-IN-5 (Compound 26) is an orally active inhibitor of necroptotic cell death (necroptosis). This compound also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). It can be utilized in research related to inflammatory diseases, neurodegenerative disorders, and cancer associated with necroptosis.</p>

<p>CDC20-IN-2 (14c) is an inhibitor of Cdc20 with a KD of 7.65 μM, inducing G2/M phase arrest, promoting DNA damage accumulation, and stabilizing key substrates such as Cyclin B1 and Bim. This leads to enhanced apoptosis, as well as inhibition of tumor cell proliferation and migration.</p>

<p>FOXO4-DRI: a peptide blocking FOXO4/p53 interaction; induces senescent cells' apoptosis.</p>

<p>Potent vasopressin blocker, Antagonist G TFA also mildly inhibits GRP &amp; Bradykinin, triggers AP-1, enhances chemo response.</p>

<p>(E/Z)-Eltrombopag 13C4 is a mix of E/Z isotopologues, both 13C-labeled TPO receptor agonists for thrombocytopenia.</p>

<p>4-Nitrothalidomide is a modified form of thalidomide that inhibits the growth and proliferation of HUVEC cells and is commonly used in the synthesis of pomalidomide, which has anticancer potential.</p>

<p>MMRi62, a MDM2-MDM4 inhibitor, induces ferroptosis and autophagy in PDAC, degrades FTH1 and mutant p53, and inhibits KRAS/TP53 mutant PDAC in mice.</p>