Apoptosis

<p>β-Glucuronide-dPBD-PEG5-NH2 is a β-glucuronide-linked pyrrolobenzodiazepine dimer that functions as a proagent for the synthesis of the antibody-drug conjugate</p>

<p>NLRP3-IN-60 (Compound 39) is an orally bioavailable inhibitor of NLRP3. It effectively suppresses pyroptosis in THP-1 cells with an IC50 of 13 nM and inhibits IL-1β release in human whole blood, exhibiting an IC50 of 225 nM.</p>

<p>BM-1244 is a potent Bcl-xL/Bcl-2 inhibitor with Kis of 134 and 450 nM for Bcl- xL and Bcl-2, respectively.</p>

<p>Anticancer Agent 157 (compound 15) is a nitric oxide (NO) inhibitor with IC50 values of 0.62 μg/mL, exhibiting both anti-inflammatory and anticancer effects.</p>

<p>PROTAC LZK-IN-1 (Compound 21A) is a PROTAC molecule that targets the degradation of LZK (leucine zipper kinase, encoded by MAP3K13). At a concentration of 10 μM, PROTAC LZK-IN-1 facilitates the degradation of LZK and inhibits the expression of p53 and c-MYC, leading to reduced viability of global head and neck squamous cell carcinoma (HNSCC) cell lines. This compound is applicable in anticancer research.</p>

<p>TRF2-IN-1 (compound F2) is a potent inhibitor of telomere repeat-binding factor 2 (TRF2). It exhibits antiproliferative activity and induces apoptosis. TRF2-IN-1 binds directly to the TRF2TRFH domain, selectively inhibiting TRF2 protein expression and telomere localization. Additionally, TRF2-IN-1 possesses anticancer properties and shows potential for osteosarcoma research.</p>

<p>TS-IN-5 (Compound 15) is an inhibitor of thymidylate synthase (TS). It induces apoptosis by modulating the proteins Bax, BCL-2, PI3K, and STAT1. TS-IN-5 exhibits antitumor activity against liver cancer, breast cancer, and colon cancer.</p>

<p>Aphidicolin blocks DNA synthesis, hinders herpes virus growth, and stimulates apoptosis in leukemia cells; it's a mold-derived DNA polymerase inhibitor.</p>

<p>DJ4 induces a dose-dependent pro-apoptotic effect in the micromolar range.</p>

<p>Ptd-p65-p1 Peptide TFA inhibits NF-kappaB, has a cell-penetrating antennapedia sequence, and selectively blocks NF-kappaB activation.</p>

<p>Tubulin Inhibitor 34 (compound b5), a potent anticancer agent, inhibits tubulin polymerization and induces G2/M arrest and apoptosis.</p>

<p>Mcl-1 inhibitor 3 shows good pharmacokinetic properties and excellent in vivo efficacy without toxicity.Mcl-1 inhibitor 3 is a highly potent and orally activate</p>

<p>Ferroptosisinducer-4 (Compound 5) is a phospholipid-based ferroptosis inducer featuring a terminal double bond at the sn-2 position. It exhibits significant cytotoxicity towards HT-1080 cells with an IC50 value of 18 μM. The toxicity mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane induced by the terminal double bond. Ferroptosisinducer-4 can be utilized in studies pertaining to the regulation of ferroptosis.</p>

<p>Thalidomide-based cereblon ligand with 2-unit PEG linker for PROTAC, in hydrochloride form.</p>

<p>Cholesteryl Hemisuccinate Tris Salt is a cholesteryl ester with anticancer activity.Cholesteryl hemisuccinate has antitumor activity and inhibits tumor growth.</p>

<p>ZLDI-8 is an inhibitor of Notch activating/cleaving enzyme ADAM-17 and inhibits the cleavage of Notch protein.</p>

<p>Conglobatin is a natural product for research related to life sciences. The catalog number is T36494 and the CAS number is 72263-05-9.</p>

<p>JNK-1-IN-3 (Compound 9e) downregulates JNK1 and phosphorylated JNK1, reduces c-Jun and c-Fos expression in tumours, and restores p53 activity.</p>

<p>DefNEtTrp is an iron bis-chelating ligand composed of Def and Trp groups. It demonstrates potent broad-spectrum antiproliferative and cytotoxic effects in cancer cell lines. DefNEtTrp induces apoptosis and ferroptosis, exhibiting cytotoxicity with an IC50 value of 0.77 μM.</p>

<p>TTQ-SA is a near-infrared spiraling aggregation-induced emitter capable of converting near-infrared light (NIR) into thermal energy, resulting in thermal damage and death of tumor cells. In cancer cells MF-7, TTQ-SA shows cell uptake and targeting capabilities. TTQ-SA binds with DNAzyme to inhibit the expression of the survivin gene, enhancing the sensitivity of tumor cells to photothermal therapy.</p>

<p>Distamycin A (NSC-82150), oligopeptide antibiotic, binds A/T rich DNA, affects cleavage sites, enhances apoptosis.</p>

<p>DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]</p>

<p>CQ627 is a molecular glue that targets the degradation of RIOK2. It effectively recruits the E3 ubiquitin ligase RNF126, inducing the proteasomal degradation of RIOK2 via the ubiquitin-proteasome system (UPS) in MOLT4 leukemia cell lines, with a DC50 value of 410 nM. Additionally, CQ627 induces apoptosis in a dose-dependent manner in these cells, blocking the cell cycle at the G2/M phase, and exhibits antiproliferative activity across various cancer cell lines. It also demonstrates in vivo anticancer activity in MOLT4 xenograft mouse models.</p>

<p>PROTACROR1degrader-1 (Compound 11d) serves as a PROTAC degrader targeting the pseudokinase ROR1, with the capability of degrading ROR1 in NSCLC cells at a DC50 of 40-80 nM. It induces PARP cleavage and apoptosis in NCI-H23 cells. [Pink: ligand for target protein ROR1 ligand-1; Black: linker; Blue: ligand for VHL E3 ligase (S,R,S)-AHPC]</p>

<p>Ledostomig is an immunoglobulin (H-γ1-scFv-L-κ) dimer monoclonal antibody that targets human neurotensin receptor type 5 (NTS5) and programmed death-1 (PD-1). It shows potential for research in various cancer types.</p>

<p>Antitumor agent-196 (Compound 6a (β, β, β)) is an artemisinin-based oligomer with anticancer properties, exhibiting an IC50 of 90 nM against MCF-7 breast cancer cells. This compound induces apoptosis by modulating the Bax-caspase 3 signaling pathway and triggers ferroptosis by regulating key signaling molecules (including GPX4). Antitumor agent-196 shows potential for cancer research applications.</p>

<p>Enpp/Carbonic anhydrase-IN-2 is a potent dual inhibitor of Enpp and carbonic anhydrase, inhibiting NPP1, NPP2, NPP3, CA-IX, CA-XII, with IC50 values of 1.13, 1.</p>

<p>Apoptosisinducer 31 (compound 19) triggers caspase-dependent apoptosis (cell death). It plays a crucial role in cancer research.</p>

<p>AS-99 TFA: potent ASH1L inhibitor, IC50=0.79 μM, combats leukemia, inhibits cell growth, induces apoptosis.</p>

<p>WR-S-462 is a STAT3 inhibitor. It effectively blocks the phosphorylation and biological functions of STAT3 in vitro. The IC50 of WR-S-462 for inhibiting MDA-MB-231 cells is 0.03 μM, and it exhibits a strong binding affinity for STAT3 protein with a Kd of 58 nM. WR-S-462 prevents the nuclear translocation of p-STAT3 and selectively inhibits the expression of p-STAT3Tyr705 in MDA-MB-231 cells, as well as the expression of downstream target genes regulated by STAT3, such as Cyclin D1, Bcl-2, and Bcl-xl. This compound inhibits the growth and metastasis of triple-negative breast cancer (TNBC).</p>

<p>ICy-OH, an iodinated anticancer photosensitizer, excels in deep tissue imaging (640 nm excitation) and triggers pyroptosis in pancreatic cancer cells.</p>

<p>Cannflavin A, isolated from Cannabis sativa L., exhibits anti-cancer, neuroprotective, and anti-inflammatory activities by inhibiting Aβ1-42 aggregation and</p>

<p>KTX-582: potent IRAK4/Ikaros degrader (DC50=4/5nM), induces MYD88 MT DLBCL apoptosis &amp; tumor regression in lymphoma.</p>

<p>TNF-α-IN-9 is an NDM-1 inhibitor-3 analog and is a TNF-α inhibitor.TNF-α-IN-9 shows low inhibitory activity.</p>

<p>Thalidomide-5,6-Cl is a cereblon ligand derivative that recruits CRBN protein and forms PROTACs with a linker.</p>

<p>Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding &amp; osteoclastogenesis, induces PC12 cell apoptosis.</p>

<p>HX009 is a bispecific antibody that targets PD1 and CD47, though its binding to CD47 is attenuated. HX009 functions by blocking PD1/CD47 and can be utilized in research related to non-Hodgkin lymphoma (NHL).</p>

<p>MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.</p>

<p>H-20 is a PD-1 agonist that reduces the required dosage of morphine for analgesia. It can be used in studies related to chronic pain.</p>

<p>VTP50469 fumarate is a highly selective and orally active inhibitor of Menin-MLL interaction (Ki: 104 pM), and has potently anti-leukemia activity.</p>

<p>Thalidomide-O-amido-PEG4-propargyl is a polyethylene glycol (PEG)-based linker employed for the synthesis of proteolysis targeting chimeras (PROTACs)[1].</p>

<p>(Iso)-Z-VAD(OMe)-FMK is an isomer of Z-VAD(OMe)-FMK, which is a pan-caspase inhibitor with irreversible properties. Z-VAD(OMe)-FMK is also an inhibitor UCHL1.</p>

<p>Thalidomide-N-C3-O-C4-O-C3-OH is a conjugate of an E3 ligase ligand and a linker, used in the synthesis of the Aster-APROTAC degrader.</p>

<p>Antitumor agent-170 (Compound C6) inhibits PD-1/PD-L1 interaction and PARP7 with IC50 values of 0.342 μM and 7.05 nM, respectively. It shows high affinity for human PD-L1, with a Ki of 9.31 nM, and can restore T cell function while increasing IFN-γ secretion. In mouse models, Antitumor agent-170 exhibits antitumor effects against melanoma and demonstrates favorable pharmacokinetic properties.</p>

<p>Antitumor Agent-103 (compound 24l) induces apoptosis and possesses antiproliferative and anti-colony formation properties.</p>

<p>Haemanthamine hydrochloride, an alkaloid from Amaryllidaceae, has anticancer, antioxidant, antiviral, antimalarial, and anticonvulsant properties.</p>

<p>ECDD-S16 is a potent inhibitor of pyroptosis. It effectively suppresses pyroptosis in Raw264.7 cells activated by surface and endosomal TLR ligands.</p>

<p>LZFPN-90 (LZ90) is a dual-target compound aimed at NAMPT and PD-L1. It inhibits the interaction between PD-1/PD-L1 and NAMPT activity. LZFPN-90 suppresses cell growth in a NAMPT-dependent manner, blocking the cell cycle and subsequently inducing apoptosis. Additionally, LZFPN-90 exhibits target-dependent antitumor activity, impacting metabolic processes and the immune system.</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>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>