Apoptose

<p>OPBP-1 is a D-peptide developed through phage display screening, molecular docking, and molecular dynamics simulations. It exhibits high stability, strong antitumor activity, and oral bioavailability. OPBP-1 selectively binds to the PD-L1 protein, significantly blocking the interaction between PD-1 and PD-L1, which helps restore and enhance T lymphocyte function while reducing the proportion of myeloid-derived suppressor cells (MDSCs), counteracting tumor-induced immune evasion. OPBP-1 is applicable for research in cancer immunotherapy.</p>

<p>RIP1 kinase inhibitor 9 (compound SY-1) is a selective inhibitor of RIP kinase. It effectively reduces central inflammatory responses caused by seizures. RIP1 kinase inhibitor 9 also obstructs Z-VAD-FMK-induced necroptosis in HT-29 cells, with an EC50 of 7.04 nM.</p>

<p>Anticanceragent 178 (compound C2) is a potent anticancer compound. It effectively inhibits the proliferation and metabolic activity of MDA-MB 231 cells, with IC50 values of 1.1 and 4.2 μM, respectively. Additionally, Anticanceragent 178 induces ferroptosis and necroptosis in cells.</p>

<p>c-Met/HDAC-IN-4, a dual inhibitor of c-Met/HDAC, exhibits an IC 50 value of 28.92 nM for c-Met. This compound effectively induces G 0 /G 1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells. Additionally, c-Met/HDAC-IN-4 suppresses both the proliferation and invasion of breast cancer cell lines.</p>

<p>Petromurin C, a bis-indolyl benzenoid from P. muricatus, is cytotoxic to NS-1 cells (IC50=33μg/ml) and active against T. foetus (IC50=100μg/ml).</p>

Apoptosis Inducer 29 (compound Y9) demonstrates anticancer efficacy in non-small cell lung cancer by inducing lysosomal dysfunction and apoptosis, and exhibits superior performance to Gboixn both in vitro and in vivo.

<p>hCAIX-IN-13 (Pt2) inhibits CAIX with 6.57 μM IC50, curbs cancer cell growth, and induces apoptosis for cancer research.</p>

<p>CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.</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>ARI-1 is a receptor tyrosine kinase-like orphan receptor 1 (ROR1) inhibitor that binds to ROR1's extracellular Frizzled domain, effectively inhibiting aberrant</p>

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

<p>TRP-601 is a caspase inhibitor.</p>

<p>SSE1806, a podophyllotoxin derivative (a natural antimitotic agent), functions as a microtubule/tubulin inhibitor, exhibiting potent anticancer and</p>

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

<p>FKBP12 ligand-1 is the target protein ligand for MC-25B, which is a PROTAC targeting FKBP12.</p>

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

<p>Cytostatin: Natural antitumor, inhibits cell adhesion, blocks B16 melanoma, induces apoptosis, selectively targets PP2A (IC50 = 29 nM).</p>

<p>2-Chloronaphthalene is an organochlorine chemical compound and is a chlorinated derivative of naphthalene. The compound is an isomer for 1-chloronaphthalene.</p>

<p>Thalidomide-O-C4-COOH is a synthetic E3 ligase linker derived from Thalidomide for PROTAC tech.</p>

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

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

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>KP1019 is now discontinued.</p>

<p>BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.</p>

<p>LIB3S0280 is a potent inhibitor of TBK1, with an IC50 of 493.9 nM. It suppresses TBK1 downstream signaling by reducing the phosphorylation of IκBα and AKT. LIB3S0280 causes G2/M phase arrest and induces apoptosis in pancreatic cancer cells. Notably, it exhibits significant inhibitory effects on pancreatic cancer cell lines with high TBK1 expression, with a 96-hour IC50 value ranging from 6.64-10.98 μM. LIB3S0280 shows potential for research in pancreatic ductal adenocarcinoma (PDAC).</p>

<p>PD-166285 is an effective and broadly active inhibitor of protein tyrosine kinase.</p>

<p>R1-ICR-5 is a selective PROTAC degrader targeting serine/threonine-protein kinase 1 (RIPK1). Mediated by VHL, R1-ICR-5 promotes the degradation of RIPK1, disrupting the TNFR1 and TLR3/4 signaling hubs, enhancing NF-κB, MAPK, and IFN signal output, and facilitating RIPK3 activation and necroptosis induction. R1-ICR-5 holds potential for research in cancer and inflammatory diseases.</p>

<p>RET-IN-4: Oral RET inhibitor, IC50 ~1 nM for variants. Selective over JAK2/FLT3. Potent anticancer use.</p>

<p>Ac-LEHD-AMC, a fluorogenic caspase-9 substrate, releases fluorescent AMC upon cleavage, aiding caspase-9 activity measurement.</p>

<p>Calphostin C is a protein kinase C inhibitor.</p>

<p>Apoptosisinducer 32 (Compound 7g) is an apoptosis inducer with a KD of 42 μM, demonstrating antitumor activity by causing significant morphological changes, such as membrane blebbing, nuclear fragmentation, and apoptotic body formation, in MDA-MB-231 cells. The IC50 values for Apoptosisinducer 32 are 4.77 μM in MCF-7 cells, 6.56 μM in MDA-MB-231 cells, and 337.8 μM in HEK cells.</p>

<p>Bfl-1-IN-6 (Compound 20) is an orally active inhibitor of Bcl-2-related protein A1 (BFL1) with an IC50 of 19 nM. This compound can stabilize BFL1 protein, activate cleaved caspase 3, and demonstrates antitumor activity in mouse models.</p>

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

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

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

<p>FOXJ1 agonist 1 (compound 16c), an orally effective small molecule, effectively enhances FOXJ1 expression and acts on multiciliated cells (MCC) in the mammalian airway system to prevent chronic obstructive pulmonary disease (COPD). Foxj1-IN-1 induces motile cilia production in the respiratory system of both zebrafish and mammals and inhibits elastase-induced COPD in mouse models. Additionally, Foxj1-IN-1 demonstrates good liver microsomal stability and favorable in vivo pharmacokinetic (PK) curves and area under the curve (AUC). It exhibits negligible inhibition of CYP and hERG and lacks significant cytotoxicity.</p>

<p>Potent PROTAC degrader for FLT3/CDK9, induces apoptosis, and shows promise for FLT3-ITD mutated AML research.</p>

<p>PARP1-IN-27 (Compound 9B) serves as an inhibitor of both PARP1 and PARP2, exhibiting IC 50 values of 2.53 nM and 6.45 nM, respectively, in SUM149PT cells. This compound effectively suppresses the proliferation of BRCA-mutated cancer cell lines such as SUM149PT, HCC1937, and Capan-1, with respective IC 50 values of 0.62, 1.91, and 4.26 μM. Additionally, PARP1-IN-27 exacerbates DNA double-strand breaks, enhances ROS production, causes G2/M phase cell cycle arrest, and triggers apoptosis in SUM149PT cells.</p>

<p>Antiproliferative agent-23: destabilizes microtubules, induces apoptosis in cancer cells via mitochondrial path, and triggers ER stress.</p>

<p>NSC90616 is a mutant p53 rescue compound [1] .</p>

<p>sEH inhibitor-19 (Compound (R)-14i) is an orally active soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 1.2 nM. This compound suppresses the expression of TNF-α and IL-6 and exhibits anti-inflammatory effects in mouse models of acute pancreatitis and Carrageenan-induced edema.</p>

<p>Bursehernin is a useful organic compound for research related to life sciences and the catalog number is T124894.</p>

<p>Claturafenib is a brain-permeable, selective, all-mutant BRAF inhibitor.PF-07799933 has shown antitumor activity, used in combination with MEK inhibitors.</p>

<p>Schisandronic acid is a triterpenoid acid isolated from the stems of Schisandra propinqua.</p>

<p>MYC-RIBOTAC, a ribonuclease-targeting chimera (RIBOTAC) specific to the MYC internal ribosome entry site (IRES), comprises an MYC mRNA-binding element tethered</p>

<p>SRE-II, an amide derivative, serves as an activatable photosensitizer tailored for photodynamic cancer research, exhibiting diminished fluorescence and</p>

<p>Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.</p>

<p>Antitumor agent-36: potent anti-cancer; causes DNA damage, triggers apoptosis, enhances immune response by upregulating T cells.</p>

<p>Oxidosqualene cyclase inhibitor</p>