Apoptosis

<p>UZH1, a mix of active METTL3 inhibitor UZH1a (IC50 280 nM) and inactive UZH1b (IC50 28 μM), modifies epitranscriptomics and has antitumor properties.</p>

<p>Prolgolimab (BCD-100) is an anti-PD-1 antibody used in melanoma research.</p>

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

<p>HDAC6-IN-16 (compound 5c), a quinazolin-4(3H)-one-based inhibitor of histone deacetylase 6 (HDAC6), demonstrates an anticancer effect by inhibiting colony</p>

<p>LZ-07 is an IRAK4 PROTAC degrader (DC50 = 1.14 nM), that, upon degradation of IRAK4, significantly inhibits the expression of cytokines such as IL-6, IL-1β, TNF-α, and IL-10. It is applicable in research related to autoimmune diseases.</p>

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

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

<p>A-1208746 is an inhibitor of MCL-1 with a Ki value of 0.454 nM. This compound effectively activates caspase-3/-7, induces apoptosis in H929 cells, and reduces mitochondrial membrane potential. Additionally, A-1208746 synergizes with Navitoclax, making it applicable in cancer research.</p>

<p>VK-28 is a brain permeable iron chelator with neuroprotection. VK-28 inhibits basal as well as iron-induced mitochondrial lipid peroxidation.</p>

<p>Pomalidomide-PEG3-CO2H is a cereblon ligand-PEG3 linker for PROTACs.</p>

<p>DCZ3301 is a novel aryl-guanidino inhibitor.</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>

<p>BWA-522 is a small molecule, orally available protein-targeting chimera (PROTAC) that potentates the degradation of both full-length androgen receptor (AR-FL)</p>

<p>Onfekafusp alfa (L19TNF), a trimeric fusion of L19 scFv and human TNF, targets malignant glioma.</p>

<p>MEDI-7352 is a human bispecific antibody targeting NGF/bNGF and TNF. It can be utilized in research focused on osteoarthritis (OA) pain.</p>

<p>BTK-IN-37 (compound 8d), a BTK inhibitor, demonstrates potent apoptotic effects on cancer cells by targeting BTK with K_i and IC_50 values of 5.07 nM and 3.6 nM, respectively. Additionally, this compound selectively promotes the enrichment of genes associated with necroptosis and pyroptosis.</p>

<p>3-methoxy-9H-carbazole: photosensitizer, anti-breast cancer, from Klauseneria spp., induces apoptosis.</p>

<p>Os30 is a potent fourth-generation EGFR inhibitor, specifically targeting the EGFRC797S-TK mutation with IC50 values of 18 nM for EGFRDel19/T790M/C797S TK and</p>

<p>MRIA9 inhibits SIK1/2/3 &amp; PAK2/3 with IC50: SIK1 (516 nM), SIK2 (180 nM), SIK3 (127 nM); ATP-competitive.</p>

<p>4-N-Nonyloxyphenol, kaolinite nanotube photosensitizer, degrades phenolic pesticides, and disrupts endocrine.</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>Kusunokinin is a useful organic compound for research related to life sciences and the catalog number is T124612.</p>

<p>HDAC-IN-57 is an orally active pan-inhibitor of histone deacetylase (HDAC), inhibiting HDAC1, HDAC2, HDAC6, and HDAC8 with IC50 values of 2.07 nM, 4.71 nM, 2.4</p>

<p>Thalidomide-O-C4-COOH is a synthetic E3 ligase linker derived from Thalidomide for PROTAC tech.</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>dMCL1-2 is a PROTAC-based MCL1 degrader, binding at 30 nM, and induces apoptosis in leukemia.</p>

<p>CGP 3466B (Omigapil) is an oral drug inhibiting GAPDH nitrosylation and apoptosis, potentially treating Alzheimer's and CMD.</p>

<p>H3R antagonist 4 (compound 11l) serves as a dual inhibitor of cholinesterases and histamine H3 receptors (H3R), demonstrating IC50 values of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible), and 1.09 nM (H3R). It effectively inhibits both self and Cu2+-induced Aβ1-42 aggregation at 95.48% and 88.63%, respectively, and degrades Aβ1-42 protofibrils with 80.16% and 89.30% efficiency under similar conditions. Additionally, H3R antagonist 4 possesses the chelating capability for biometals Cu2+, Zn2+, Al3+, and Fe2+. It significantly reduces tau protein hyperphosphorylation induced by Aβ1-42, inhibits RSL-3 induced apoptosis and ferroptosis in PC12 cells, and shows optimal blood-brain barrier permeability and intestinal absorption characteristics in hCMEC/D3 and hPepT1-MDCK cells, respectively. Moreover, the compound improves learning and memory impairments in an Alzheimer's mouse model induced with scopolamine.</p>

<p>Compound (Ra)-10, also known as Mcl-1 inhibitor 14, is a potent inhibitor of myeloid cell leukemia-1 (MCL-1), exhibiting a K_i of 0.018 nM, and holds potential</p>

<p>PD-1/PD-L1-IN-49 (compound 1c) is a potent inhibitor of PD-1/PD-L1 with an IC50 of 77 nM. This compound can activate Jurkat T cells and effectively block the PD-1/PD-L1 immune checkpoint.</p>

<p>Antitumor agent-187 (compound I3), a photosensitizer derived from 5,15-diarylporphyrin, exhibits anticancer activity with a peak absorption wavelength of ~668 nm. This compound induces apoptosis and is applicable in photodynamic therapy (PDP). It selectively accumulates in tumor sites and possesses real-time fluorescence imaging capabilities.</p>

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

<p>GBM CSCs-IN-1 (Compound (−)-20), a rocaglate derivative, potently inhibits glioblastoma stem cells (GBM CSCs) and exhibits an EC50 of 45 nM by targeting the RNA helicase DDX3. Additionally, it induces apoptosis in these cells.</p>

<p>TAS-117, a PKB/Akt inhibitor, is used potentially for the treatment of solid tumors.</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>3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor.</p>

<p>DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.</p>

<p>RD-23 is an orally active and selective RET PROTAC degrader. It facilitates the ubiquitination and degradation of the RETG810C mutant with a DC50 value of 11.7 nM. Additionally, RD-23 inhibits the activation of downstream Shc signaling and induces apoptosis (Apoptosis). It is useful for studying RET-related cancers.</p>

<p>EGFR-IN-153 (Compound 5l) is an EGFR inhibitor that suppresses the proliferation of MDA-MB-231 cells with an IC50 of 0.73 μM and induces apoptosis. It is applicable for research in breast cancer.</p>

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

<p>Thalidomide-based E3 ligase ligand linked to a PROTAC piperazine-piperidine chain.</p>

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

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

<p>BCL6-IN-10 (Compound WK499) is an inhibitor of BCL6, disrupting its interaction with the SMRT protein and promoting apoptosis, cell cycle arrest, and DNA damage</p>

GPX4-IN-14 (compound 2c) acts as a GPX4 inhibitor, exhibiting both free radical scavenging activity (with a maximum scavenging rate of 72.52%) and anti-tumor proliferation activity in vitro. This compound targets GPX4 protein, elevating lipid peroxide and intracellular Reactive Oxygen Species (ROS) levels, which induces ferroptosis and contributes to its anti-tumor proliferation effects.

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

<p>Galloflavin Potassium is an inhibitor of lactate dehydrogenase.</p>

PI3K/AKT-IN-4 (compound 3), a diterpenoid extracted from the roots and rhizomes of Salvia castanea Dielsf., exhibits antitumor properties by inhibiting cell viability and proliferation (IC 50 =4.72 μM) and promoting apoptosis in Hep3B cells. This compound obstructs the G0/G1 phase of the cell cycle, triggers mitochondrial dysfunction, and induces oxidative stress. Moreover, PI3K/AKT-IN-4 combats hepatocellular carcinoma through the inhibition of the PI3K-Akt signaling pathway and by interacting with PARP1 and CDK2 targets.

<p>β-Glucuronide-dPBD-PEG5-NH2 TFA is a β-glucuronide-linked pyrrolobenzodiazepine dimer employed in the synthesis of the antibody-drug conjugate (ADC) cIRCR201-</p>