Apoptosis

<p>(E/Z)-Eltrombopag 13C4 is a mix of E/Z isotopologues, both 13C-labeled TPO receptor agonists for thrombocytopenia.</p>

<p>Potent vasopressin blocker, Antagonist G TFA also mildly inhibits GRP &amp; Bradykinin, triggers AP-1, enhances chemo response.</p>

<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>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>JAK-IN-40 (Compound 46) is an inhibitor of JAK, effectively targeting JAK1, JAK2, and JAK3 with IC50 values of 0.022, 0.759, and 1.601 μM, respectively. It reduces the phosphorylation of STAT3 and inhibits the proliferation of cancer cells Ba/F3 and JAK1-TEL Ba/F3 with GI50 values of 0.614 μM and 0.193 μM. JAK-IN-40 arrests cell cycle progression at the G2/M phase in H1975 and H2087 cells, leading to apoptosis. Additionally, JAK-IN-40 exhibits a synergistic anti-tumor effect when used in combination with Osimertinib.</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>Vonlerizumab (Anti-TNFRSF4/OX40/CD134 Antibody) is a humanized monoclonal antibody targeting OX40, used in tumor research.</p>

<p>Desmethyl-WEHI-345 analog, a protein kinase inhibitor, holds potential for colon cancer research.</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>Zamzetoclax (compound 1) acts as a potential inhibitor of Mcl-1.</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>CDC20-IN-2 (14c) is an inhibitor of Cdc20 with a KD of 7.65 μM, inducing G2/M phase arrest, promoting DNA damage accumulation, and stabilizing key substrates such as Cyclin B1 and Bim. This leads to enhanced apoptosis, as well as inhibition of tumor cell proliferation and migration.</p>

<p>BMSpep-57: Macrocyclic peptide, inhibits PD-1/PD-L1, IC50=7.68 nM, binds PD-L1 (Kd=19 nM/MST, 19.88 nM/SPR), boosts T cell IL-2 in PBMCs.</p>

<p>HSP70-IN-6 (Compound JL-15) acts as an inhibitor of the Hsp70-Bim protein-protein interactions (PPI) with an IC50 value of 70 nM. It induces apoptosis in chronic myeloid leukemia (CML) cells with EC50 values of 0.43 μM (BV173), 0.88 μM (K562), and 0.19 μM (K562-R3).</p>

<p>CYP51/PD-L1-IN-3 (compound L21), a quinazoline with antifungal properties, serves as a dual inhibitor targeting CYP51 (IC50: 0.205 μM) and PD-L1 (IC50: 0.039 μM</p>

<p>PKM2-IN-8 (Compound 9b) is an inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.31 μM. It exhibits potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 induces early apoptosis and reduces lactate levels. This compound is useful for research in glioblastoma.</p>

<p>JPS014 TFA, a benzamide-based Von Hippel-Lindau (VHL) E3-ligase proteolysis targeting chimera (PROTAC), effectively degrades class I histone deacetylase (HDAC</p>

<p>Anticancer agent 137 (8q), a potent PI3k inhibitor, exhibits broad-spectrum anticancer activity by inducing G2/M cell cycle arrest and apoptosis.</p>

<p>eIF4E-IN-5 (Compound 6n) is a cell-permeable eIF4E inhibitor that binds to capped mRNA, thereby inhibiting cap-dependent translation [1].</p>

<p>EGFR/BRAFV600E-IN-3 is an inhibitor targeting EGFR, BRAFV600E, and EGFRT790M with IC50 values of 57 nM, 68 nM, and 9.70 nM, respectively.</p>

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

U7D-1: First-class USP7 PROTAC degrader, DC50 33 nM, anticancer, induces apoptosis in Jeko-1.

<p>Cytostatin: Natural antitumor, inhibits cell adhesion, blocks B16 melanoma, induces apoptosis, selectively targets PP2A (IC50 = 29 nM).</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>Toremifene citrate is a selective estrogen receptor modulator (SERM). It is an estrogen agonist for bone tissue and cholesterol metabolism but is antagonistic on the mammary and uterine tissue.</p>

<p>Fludarabine triphosphate inhibits key enzymes, causing cell death.</p>

cytoplasmic peptide of the neurotrophin receptor p75NTR

<p>Thalidomide-O-amido-PEG4-azide is a polyethylene glycol (PEG) derivative serving as a linker for Proteolysis Targeting Chimeras (PROTACs) synthesis [1].</p>

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

<p>CRA-026440 hydrochloride is a potent and broad-spectrum HDAC inhibitor.</p>

<p>EMB-02 is a bispecific antibody targeting both PD-1 and LAG-3. It inhibits the downregulation of T cell activation and proliferation mediated by PD-1 and LAG-3, showing potent anti-cancer properties.</p>

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

Hexapeptide-11 is a novel proteostasis network modulator in human diploid fibroblasts.

<p>Monensin, from Streptomyces cinnamonensis, inhibits Wnt/β-catenin. Potential anticancer agent.</p>

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

<p>Cholicamideβ (compound 6), a self-assembling small molecule cancer vaccine adjuvant, forms low cytotoxicity virus-like particles and upon binding to peptide</p>

<p>PDE4-IN-1 is a PDE4 inhibitor characterized by high potency (IC50: 8.6 nM) and superior selectivity over other PDE subtypes. This compound inhibits the release of inflammatory cytokines and chemokines. Additionally, PDE4-IN-1 significantly restores the damaged cAMP-CREB signaling pathway, inhibits proliferation, and promotes differentiation to reverse psoriasis formation.</p>

<p>Bcl-2-IN-4: potent, selective, oral Bcl-2 inhibitor with 1.5 nM IC50, &gt;200x selectivity over Bcl-xL.</p>

Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding & osteoclastogenesis, induces PC12 cell apoptosis.

<p>This Bim peptide belongs to the pro-apoptotic group of the Bcl-2 family of proteins.</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>NSD-IN-4 (Compound A8) is a potent and orally active inhibitor of NSD3, inducing apoptosis in a dose-dependent manner. It demonstrates significant antitumor activity against lung squamous cell carcinoma.</p>

<p>MDM2-IN-21 is a potent MDM2 inhibitor. MDM2-IN-21 can be used for the research of cancer.</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>TAT-GluN2BCTM is a membrane-permeable peptide that selectively targets active DAPK1 (Death-associated protein kinase 1) for lysosomal degradation, thereby</p>

<p>P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.</p>

Arg-Gly-Asp-D-Phe-Val (TFA) has anti-tumor activity and is an inhibitor of integrin αvβ3.

<p>Moflerafusp alfa is a fusion protein that targets the human signal-regulatory protein alpha (SIRPα) variant V2 D1 domain and human programmed death-ligand 1 (PD-L1). It shows potential for research in various cancer treatments.</p>