Apoptose

<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>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>dTAG-7 selectively degrades BRD4 and FKBP12F36V by linking BET bromodomains to E3 ligase CRBN; it's a heterobifunctional degrader.</p>

<p>EGFRkinase inhibitor 7 (compound 18i) is an EGFR inhibitor with an IC50 of 42.3 nM, exhibiting anticancer properties. This compound demonstrates significant in vitro cytotoxicity and capacity to induce apoptosis. Furthermore, EGFRkinase inhibitor 7 displays anti-proliferative activity against human colon cancer cell line HCT116 and human non-small cell lung cancer cell line A549, with IC50 values of 4.82 µM and 1.43 µM, respectively.</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>WEHI-3773 is an inhibitor of the interaction between VDAC2 and either BAK or BAX. It prevents BAX-mediated apoptosis (Apoptosis) by blocking the recruitment of BAX to the mitochondria through VDAC2. Conversely, WEHI-3773 promotes BAK-mediated apoptosis (Apoptosis) by limiting VDAC2's inhibitory sequestration of BAK. This compound shows promise for research in the field of cancer therapy.</p>

<p>Mcl-1 Inhibitor 16 (Compound 9), a platinum-based mitochondrial-targeting agent, inhibits Mcl-1 and induces Bax/Bak-dependent apoptosis in cancer cells.</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>PZ703b is a novel BCL-XL PROTAC degrader with enhanced BCL-2 inhibition.</p>

<p>1-Alaninechlamydocin, a fungal metabolite from Tolypocladium sp., inhibits HDACs and reduces cell proliferation with GI50s 5.3-14 nM.</p>

<p>FAK-IN-25 (4c) is an inhibitor of FAK with an IC50 value of 50.98 nM. It induces apoptosis and causes cell cycle arrest in the G1 phase, making it relevant for cancer research.</p>

<p>Eldecalcitol, orally active vitamin D analog, boosts bone density and treats osteoporosis.</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>Cell-permeable CaM agonist; activates phosphodiesterase, binds to Ca2+ channels, inhibits cytotoxicity (IC50=52μM), protects cells, reduces inflammation.</p>

<p>PL120131 is a PD-1/PD-L1 inhibitory peptide that disrupts the interaction between PD-1 and PD-L1 by binding to PD-1. This compound can inhibit the apoptosis signaling pathway mediated by PD-1, thereby preventing apoptosis (apoptosis) in Jurkat cells and primary lymphocytes. Additionally, PL120131 supports cytotoxic T lymphocytes (CTL) in exhibiting antitumor activity.</p>

<p>ERK-IN-6, a potent agent, inhibits ESCC growth and induces apoptosis through the ERK pathway.</p>

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

<p>RIPK3-IN-3 (compound 20) is a selective RIPK3 inhibitor that demonstrates potent activity with an IC50 value of 10 nM.</p>

<p>Thalidomide-NH-amido-C6-NH2 hydrochloride is a synthetic E3 ligase ligand-linker conjugate that includes a thalidomide-based cereblon ligand and a linker, designed for the synthesis of PROTAC.</p>

<p>Raptinal activates caspase-3 directly and initiates intrinsic caspase-dependent apoptosis pathway in multiple cell lines.</p>