Apoptose

<p>WEE1-IN-7 (compound 12h) is a potent, orally active WEE1 inhibitor with an IC50 value of 2.1 nM. This compound induces apoptosis and causes cell cycle arrest in the S phase, demonstrating antitumor activity.</p>

<p>Antitumor Agent-116 (Compound 6C) is an anti-tumor agent that exhibits anti-proliferative properties and induces apoptosis.</p>

<p>Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase.</p>

<p>PROTACGPX4 degrader-2 (compound 18a) is a proteolysis-targeting chimera (PROTAC) that targets the degradation of glutathione peroxidase 4 (GPX4), with a DC50, 48h value of 1.68 μM. It induces the accumulation of lipid peroxides and mitochondrial depolarization, subsequently triggering ferroptosis. Additionally, PROTACGPX4 degrader-2 exhibits antiproliferative activity.</p>

<p>BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2].</p>

<p>Euphornin is a natural product that can be used as a reference standard. The CAS number of Euphornin is 80454-47-3.</p>

<p>GA-Mk is a triterpenoid from Ganoderma lucidum mycelia, inhibits HeLa cell growth, and induces apoptosis via mitochondria; used in cervical cancer studies.</p>

<p>YW-N-7 (TFA) is a PROTAC designed to target, inhibit, and degrade RET kinase, demonstrating a DC50 of 88 nM. It exhibits antitumor activity in xenograft mouse models driven by KIF5B-RET, making it a valuable compound for cancer research.</p>

<p>CST626 is a PROTAC degrader that targets XIAP, cIAP1, and cIAP2.</p>

<p>Top1-IN-2 (Compound 1a) is an inhibitor of topoisomerase 1 (Top1). It suppresses the growth of P-gp drug-resistant tumor cells and induces apoptosis.</p>

<p>p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.</p>

<p>DiPT-4, a dual TOP1/PARP1 inhibitor, effectively induces DNA double-strand breaks (DSBs), cell cycle arrest, and apoptosis in cancer cells, with potential to</p>

<p>hCAIX/XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX/XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2/M phase cell cycle arrest and increasing apoptosis.</p>

<p>SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells.</p>

<p>HDAC3-IN-2 (compound 4i), a pyrazinyl hydrazide-based HDAC3 inhibitor with an IC50 of 14 nM, effectively targets triple-negative breast cancer cells.</p>

<p>HC Toxin: cyclic tetrapeptide, reversible HDAC inhibitor (IC50=30 nM), upregulates 15-lipoxygenase-1, induces fetal hemoglobin, from C. carbonum.</p>

<p>Antimycobacterial agent-5 (compound 27) is an imidazopyridine amide compound that targets the Mycobacterium electron transport chain (ETC) respiratory CIII2CIV2 supercomplex. It acts on Mycobacterium smegmatis CIII2CIV2 with an IC50 of 441 nM.</p>

<p>WK369 is an innovative small molecule inhibitor of BCL6, demonstrating remarkable bioactivity against ovarian cancer by inducing cell cycle arrest and triggering apoptosis. It binds directly to the BCL6-BTB domain, obstructing the interaction between BCL6 and SMRT, which results in the reactivation of p53, ATR, and CDKN1A.</p>

<p>S2/IAPinh is a conjugate composed of an inhibitor of apoptosis proteins inhibitor (IAPinh) and a ligand of sigma 2 SW43. It demonstrates anti-proliferative and apoptosis-inducing activity by degrading inhibitor of apoptosis proteins (clAP-1).</p>

<p>Rosamultic acid is a useful organic compound for research related to life sciences and the catalog number is T125342.</p>

155H1 (Compound 11) is a stapled peptide that covalently binds to hMcl1 (172-323) with an IC50 of 18 nM.

<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>PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.</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>PROTACEGFRdegrader 9 (Compound C6) is an orally active, CRBN-based PROTAC EGFR degrader. It has a DC50 of 10.2 nM and a Kd of 240.2 nM against EGFRL858R/T790M/C797S. PROTACEGFRdegrader 9 demonstrates effective degradation activity against various EGFR mutants while not affecting EGFRWT.</p>

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

<p>PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.</p>

<p>DA5-HTL is a compound that combines dasatinib with the HaloTag system, effectively inhibiting the growth of tumor cells, with a GI50 of 1.923 nM.</p>

<p>PZ703b hydrochloride, a Bcl-xl PROTAC, triggers apoptosis and halts cancer growth; used in bladder cancer studies.</p>

<p>Thailanstatin D blocks AR-V7 splicing, disrupts U2AF65/SAP155 binding, and induces apoptosis in CRPC xenografts.</p>

<p>CUR5-8: potent, oral CUR analog, reduces lipid droplets, boosts autophagy, hinders apoptosis, enhances insulin sensitivity.</p>

<p>Antitumor agent-150 (V10) is a breast cancer treatment that functions as a PROTAC degrader of MDM2.</p>

<p>Verdinexor (KPT-335) (KPT-335), a specific XPO1/CRM1 inhibitor, are orally bioavailable.</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>(R)-JAK2/STAT3-IN-10a is the R-isomer of JAK2/STAT3-IN-1.JAK2/STAT3-IN-1 is a structural domain inhibitor of GP130 D1 with antitumor activity.</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>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>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>UBX1325, a potent Bcl-xL inhibitor, induces cell death in aging cells, useful for age-related eye disease research.</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>YX-02-030M is a PROTACMDM2 degrader. It inhibits the binding of MDM2 to p53 and VHL to HIF1α, with IC50 values of 63 nM and 1.35 μM, respectively. YX-02-030M binds to MDM2 and recruits the VHL E3 ubiquitin ligase to initiate MDM2 degradation, effectively killing p53 mutant or deficient triple-negative breast cancer (TNBC) cells.</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>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>NSC 295642: phosphatase inhibitor, boosts phospho-Erk in cells, aids cancer research.</p>

<p>Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.</p>