Apoptosis

<p>A-1155905 is an MCL-1 inhibitor with anticancer activity, demonstrating a half maximal inhibitory concentration (IC50) of 33.5 Nm and a dissociation constant (Ki) of 0.58 nM. This compound selectively binds to MCL-1 and possesses sufficient affinity to disrupt the MCL-1-Bim complex in live cells. The induction of death in MCL-1-dependent cell lines by A-1155905 is reliant on caspase proteins and occurs through apoptosis.</p>

<p>NL13, a Polo-like kinase 4 (PLK4) inhibitor, exhibits an IC 50 value of 2.32 μM. It demonstrates the ability to suppress the viability of PC3 and DU145 prostate cancer cells with respective IC 50 values of 3.51 μM and 2.53 μM. NL13 also inhibits tumor growth in prostate cancer mice. Additionally, it deactivates the AKT signaling pathway by reducing CCNB1/CDK1 levels, leading to G2/M cell cycle arrest and initiating apoptosis through caspase-9/caspase-3 cleavage.</p>

<p>RMC-6291: Oral, covalent KRAS G12C inhibitor, blocks signaling, forms tri-complex with CypA, suppresses RAS activity in tumors.</p>

<p>Z-WEHD-FMK is a cell-permeable and irreversible inhibitor of caspase-1/5. It also shows a robust inhibitory effect on cathepsin B activity (IC50: 6 μM).</p>

<p>Nrf2 activator-11 (compound M11) is a Nrf2 activator that possesses blood-brain barrier permeability and offers anti-oxidation, anti-inflammation, anti-ferroptosis, and anti-apoptosis properties. It is applicable for use in studying cerebral ischemia-reperfusion (CI/R) injury models.</p>

<p>c-Met-IN-24 (compound 3g) serves as a dual-target inhibitor for STAT-3 (=4.7 μM) and c-MET (=12.67 μM), exhibiting anticancer properties. It arrests the G2/M cell cycle and induces apoptosis in SNB-75 cells, making it applicable in the research of central nervous system cancers.</p>

<p>Mechercharmycin A, a cytotoxic compound, was isolated from Thermoactinomyces sp. YM3-251, a marine source. It demonstrates potent antitumor activity.</p>

<p>EGFRT790M/L858R-IN-2: selective inhibitor, IC50: 3.5 nM (mutant), 1290 nM (WT); reduces p-EGFR/AKT/ERK1/2, triggers apoptosis, G1 arrest, anti-cancer.</p>

<p>AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity.</p>

<p>Ub4ix, a DUB/26S proteasome inhibitor, safeguards K48-linked Ub chains against cleavage by deubiquitinating enzymes (DUBs) and inhibits the proteasomal degradation of Ub-tagged proteins. Additionally, it diminishes the viability of Hela cells and triggers apoptosis, exhibiting an IC 50 value of 1.6 μM.</p>

<p>Thalidomide-PEG2-NH2: synthetic E3 ligase ligand-linker, combines Thalidomide-based cereblon and PROTAC linker.</p>

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

<p>FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.</p>

<p>Apoptosisinducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with an IC50 range of 1.2-4.8 μM. It arrests the cell cycle at the G2/M phase, induces apoptosis in BGC-823 cells, and causes mitochondrial dysfunction. In mice, Apoptosisinducer 24 exhibits antitumor activity without significant toxicity, having an LD50 of 91.2 mg/kg.</p>

<p>Iparomlimab: anti-PD-1 IgG4κ antibody, targets PSB103 γ4/κ-chains, forms dimers, used in cancer research.</p>

<p>Canfosfamide, a prodrug activated by GSTP1-1, induces apoptosis and inhibits DNA-PK, producing an alkylating agent for cancer research.</p>

<p>Sorafenib D4 is deuterium-labeled Sorafenib, a multi-kinase inhibitor (Raf-1, B-Raf, VEGFR-3) with IC50s: 6, 20, 22 nM.</p>

<p>ATPase-IN-3 is an ATPase (ATPase) inhibitor that can be used in the study of metabolism-related diseases.</p>

<p>Echitamine chloride, an alkaloid in Alstonia scholaris, has anti-cancer properties and inhibits pancreatic lipase (IC50: 10.92 µM).</p>

<p>Ac-YVAD-CHO acetate, potent reversible ICE and caspase-1 inhibitor; K_i: 3.0 nM (mouse), 0.76 nM (human); blocks IL-lβ production.</p>