Apoptose

<p>Boc-Asp(OBzl)-CMK, an inhibitor of IL-1 converting enzyme (ICE, caspase1), prevents the death of CHP100 neuroblastoma cells and inhibits IL-1β release induced by the viral coat protein [1].</p>

<p>Human PD-L1 inhibitor III is a human PD-L1 inhibitor.</p>

<p>Cot inhibitor-1 hydrochloride blocks TPL-2 kinase (IC50=28nM) and TNF-α synthesis (IC50=5.7nM) in human blood.</p>

<p>Diprovocim-1: TLR1/2 agonist; triggers TNF-α in THP-1 cells; boosts ovalbumin IgG1 &amp; CTLs against tumors with anti-PD-L1 in mice.</p>

<p>Thalidomide-PEG conjugate for E3 ligase in PROTACs; has cereblon ligand and 3-unit PEG linker.</p>

<p>Pyridinium bisretinoid A2E (A2E) TFA, a fluorophore derived from retinal pigment epithelium (RPE) lipofuscin, initiates blue-light-induced apoptosis, mediates</p>

<p>Beclin1-Bcl-2 Interaction Inhibitor 1 effectively disrupts the binding of Beclin 1 to Bcl-2, and is utilized in cancer and neurodegeneration research [1].</p>

<p>YX0798 is a selective, orally active CDK9 inhibitor (Kd: 0.28 nM). It downregulates the oncogenic protein c-MYC and the pro-survival protein MCL-1. YX0798 disrupts the cell cycle and causes transcriptome reprogramming, ultimately leading to apoptosis. The compound exhibits antitumor activity.</p>

<p>TRAP1-IN-1 is a selective TRAP1 inhibitor, induces degradation of TRAP1 downstream proteins, inhibits OXPHOS, and disrupts mitochondrial membrane potential.</p>

<p>Carbonic anhydrase inhibitor33 (11D) is a dual inhibitor that targets both CA (carbonic anhydrase) IX/XII and CDK6. It exhibits Ki values of 19.7 nM for hCA IX and 26.1 nM for hCA XII. Additionally, Carbonic anhydrase inhibitor33 (11D) can induce G1 phase cell cycle arrest and apoptosis, making it relevant for research in non-small cell lung cancer (NSCLC).</p>

<p>Reproxalap (NS-2) is a dry eye treatment that neutralizes aldehydes like malondialdehyde.</p>

<p>Ac-Trp-Glu-His-Asp-Aldehyde is a powerful and selective inhibitor of caspase-1, demonstrating a K_i value of 56 pM [1] [2].</p>

<p>RLX HCl is anticancer, inhibits tumour proliferation by suppressing the PI3K/Akt/FoxO3a in experimental colon cancer, antiproliferative.</p>

<p>GSK-1070916 (GSK-1070916A) is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM.</p>

<p>PROTACNCOA4 degrader-1 (Compound V3) is a PROTAC-based degrader of NCOA4, exhibiting a DC50 of 3 nM in HeLa cells. Besides acting as a ferroptosis inhibitor, this compound effectively reduces the levels of NCOA4 and decreases intracellular ferrous (Fe2+) levels. Moreover, PROTACNCOA4 degrader-1 ameliorates liver damage in a CCl4-induced acute liver injury model.</p>

<p>ASK1-IN-4 is an ASK1 inhibitor, IC50 = 0.2 μM.</p>

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

<p>RET Ligand-Linker Conjugate-1 consists of a complex formed by a RET ligand and a linker, which can be utilized in the synthesis of QZ2135.</p>

<p>Necroptosis-IN-5 (Compound 26) is an orally active inhibitor of necroptotic cell death (necroptosis). This compound also exhibits potent inhibitory activity against receptor-interacting protein kinase 1 (RIPK1). It can be utilized in research related to inflammatory diseases, neurodegenerative disorders, and cancer associated with necroptosis.</p>

<p>Potent vasopressin blocker, Antagonist G TFA also mildly inhibits GRP &amp; Bradykinin, triggers AP-1, enhances chemo response.</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>TPP-1 TFA is a high-affinity PD-L1 inhibitor (KD=95nM) that boosts T-cell function to curb tumor growth.</p>

<p>HDAC-IN-77 (HL-5s), an HDAC inhibitor, has the capability to induce ferroptosis and suppress the Nrf2/HO-1 signaling pathway. This compound is utilized in cancer research.</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>

<p>TAT-BH4 (Bcl-xL), primarily localized at the mitochondria, inhibits apoptotic cell death.</p>

<p>Ferroptosis-IN-3 (Compound 25), a ferroptosis inhibitor, demonstrates potent activity by inhibiting RSL3-induced ferroptosis in HT-1080 cells (EC50: 8.6 nM).</p>

<p>Caerin 1.1 TFA, a host defense peptide derived from the Australian tree frog Litoria's glandular secretions, exhibits anti-proliferative effects on HeLa cells</p>

<p>XZ338 is a highly selective degrader targeting BCL-XL without degrading BCL-2. It exhibits an IC50 value of 3.7 nM against MOLT-4 cells and possesses antiproliferative properties, making it useful for cancer research.</p>

<p>Compound 2v (Anti-inflammatory agent 45) demonstrates anticancer properties with direct inhibitory impacts on the proliferation of various blood malignancies,</p>

<p>TOFA-Plasmalogen (compound 1), a derivative of glyceraldehyde, exhibits ferroptosis-inducing properties. This compound promotes lipid peroxidation in cell membranes, leading to cytotoxic effects with an inhibition concentration (IC 50 = 32.87 μM).</p>

<p>RO7567132 is a bispecific antibody that binds and agonizes LTBR bivalently while binds and antagonizes FAP monovalently, inducing the formation of local TLS.</p>

<p>Anti-Mouse PD-1 Antibody (D265A) is an IgG2a, κ antibody inhibitor derived from mice, specifically targeting mouse PD-1.</p>

<p>Phenamet is a bioactive chemical.</p>

<p>BAY 1892005 is a p53 protein modulator that targets the p53 condenser for the study of diseases associated with misfolded p53 protein</p>

<p>Baceridin, a cyclic hexapeptide and proteasome inhibitor, can be isolated from the culture medium of Epiphytic Bacillus.</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>RET-IN-26 (compound D5) is a kinase inhibitor that selectively targets the RET protein with an IC50 value of 0.33 μM [1].</p>

<p>DB0614 degrades 26 kinases including AAK1 and CDK6, targeting aberrant activity in disease research.</p>

<p>CWI1-2 HCL: Potent IGF2BP2 inhibitor, induces apoptosis/differentiation, targets leukemia therapy.</p>

<p>Waltonitone is a natural ursane-type pentacyclic triterpene isolated from Gentian waltonii Burkill.</p>

<p>Compound 25b, an FPR1 antagonist, exhibits potent inhibition of the formyl peptide receptor 1 with an IC50 of 70 nM.</p>

<p>84-B10 provides protection in cisplatin-induced acute kidney injury, reversing lipid peroxidation accumulation and downregulation of key ferroptosis inhibitors.</p>

<p>Se-Aspirin (Se-NSAID-8) has anticancer activity and gastroprotective effects, inhibits activation of proinflammatory and pro-survival NF-ĸB pathways, and inhibits the expression of anti-apoptotic targets downstream of NF-ĸB (e.g., Bcl-xL, Mcl-1, and survivin).Se-Aspirin induces Cell cycle arrest and activation of apoptosis accelerates ulcer healing and can be used to study pancreatic and colorectal cancer.</p>

<p>Thalidomide-PEG2-NH2: synthetic E3 ligase ligand-linker, combines Thalidomide-based cereblon and PROTAC linker.</p>

<p>POV-PC is an oxidized phospholipid that inhibits VSMC growth under high serum conditions and induces cell apoptosis under low serum conditions.</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>AUNP-12, a new immune checkpoint modulator, is an inhibitor of the PD-1 pathway.</p>

<p>K-252c is a staurosporine analog isolated from Nocardiopsis sp.</p>

<p>Compound 6b is a synthetic Thalidomide-VHL E3 ligase-linker for PROTACs.</p>

<p>PPIA-IN-1 (Compound 20b) is an inhibitor of peptidyl-prolyl isomerase A (PPIA) with a KD of 0.52 μM. It demonstrates antiproliferative activity across various cancer cell lines, including an IC50 of 0.69 μM in HCT116 cells, induces cell cycle arrest at the G0/G1 phase, and exhibits antimetastatic effects in HCT116 cells. PPIA-IN-1 elevates ROS levels, causing DNA damage, ER stress, and mitochondrial dysfunction, and induces apoptosis in HCT116 cells via the MAPK pathway. Additionally, PPIA-IN-1 shows antitumor activity in a CT26 xenograft mouse model.</p>