Apoptosis

<p>(E/Z)-10-Hydroxy-2-decenoic acid is a useful organic compound for research related to life sciences.</p>

<p>PERK-IN-6 is a novel and highly potent PERK inhibitor (IC50:2.5 nM).</p>

<p>Etoposide phosphate disodium, a prodrug of etoposide, is a powerful anticancer drug inhibiting DNA topoisomerase II.</p>

<p>PUMA BH3 activates Bak, binds Bcl-2; triggers apoptosis via cytochrome C release; Kd 26 nM.</p>

<p>Thalidomide-O-C8-COOH, also known as Cereblon ligand 3, is a Thalidomide-derived compound that serves as a Cereblon (CRBN) ligand for the targeted recruitment</p>

<p>BCL6-IN-6 is an inhibitor of Bcl-6 and can be used in studies about diffuse large B-cell lymphoma.</p>

<p>AEG 3482 blocks JNK, induces HSP70, binds HSP90, and boosts HSP25 expression, preventing cell death.</p>

<p>Eciskafusp alfa, a cis-targeted IL2v immunocytokine, acts on programmed cell death 1 (PDCD1, commonly known as PD-1), preferentially targeting antigen-specific</p>

<p>AP1867-2-(carboxymethoxy), a moiety based on the synthetic FKBP12F36V-directed ligand AP1867, connects to the CRBN ligand through a linker to generate dTAG</p>

<p>YB-0158 inhibits Wnt, targets colorectal CSCs, disrupts Sam68/Src, induces apoptosis, and has anti-cancer properties.</p>

<p>(E/Z)-LAQ824 is an inhibitor of histone deacetylase.</p>

<p>HG-7-85-01 is a novel ATP-competitive and type II tyrosine kinase inhibitor targeting both wild-type and watchman mutant BCR-ABL, PDGFRα, Kit, and Src kinases.</p>

<p>EM 163是一种 TIR-TIR 相互作用抑制剂，它是MyD88蛋白的TIR（Toll/白细胞介素-1受体）结构域拟态。EM 163针对IL-1受体中的TIR 结构域，阻断与MyD88的相互作用。EM 163抑制葡萄球菌肠毒素B（SEB）引起的体内炎症细胞因子的产生。EM 163能保护小鼠免受SEB 冲击引起的死亡。在体外的大鼠海马神经元中，EM 163阻断p38的激活和IL-1β对化学诱导的长期电位（LTP）引发的蛋白质合成的抑制作用。</p>

<p>Tubulin/MMP-IN-3 (Compound 15j) is a dual inhibitor of tubulin polymerization and MMP, effectively inhibiting MMP-2 and MMP-9 with IC50 values of 21.13 μM and 19.24 μM, respectively. It disrupts the NF-κB signaling pathway, leading to mitochondrial dysfunction and mitochondrial-dependent apoptosis. Tubulin/MMP-IN-3 shows antiproliferative activity in various cancer cells by causing cell cycle arrest at the G2/M phase and demonstrates antitumor effects in mouse models.</p>

<p>Zalypsis, a transcription factor inhibitor, is used potentially for the treatment of lymphoma, and cervical carcinoma.</p>

<p>Solanidine is a cholestane alkaloid isolated from potato species with antitumor effects. Solanidine inhibits proliferation.</p>

<p>Anti-TNBC agent-8 (Compound TP2) is a photodynamic therapeutic compound that targets mitochondrial DNA G-quadruplexes (mtG4). Under white light exposure, it exhibits an IC50 of 0.42 μM against 4T1 cells. Anti-TNBC agent-8 tightly binds to mtG4, leading to the production of substantial reactive oxygen species (ROS) under illumination. This results in the loss of mitochondrial membrane potential (MMP), reduced ATP production, elevated ROS levels, and significant apoptosis in triple-negative breast cancer (TNBC) cells, thus demonstrating its tumor growth inhibitory activity. Anti-TNBC agent-8 is applicable for research in TNBC.</p>

<p>CSN5-IN-2 (Compound 31) is a CSN5 inhibitor with an IC50 of 0.36 μM. It increases Cullin 1 neddylation levels in cancer cells and downregulates the expression of RAD51 and PD-L1. CSN5-IN-2 exhibits antitumor activity, which is enhanced when used in combination with Talazoparib.</p>

<p>MBC-11 trisodium, a bisphosphonate-Ara-C conjugate, may treat TIBD.</p>

<p>Sasanlimab (PF-06801591), a humanized IgG4-κ antibody, selectively targets PD-1 and is primarily produced in Chinese Hamster Ovary (CHO) cells [1].</p>

<p>Antitumor photosensitizer-7 (compound 15), a photosensitizer possessing anti-cancer properties, demonstrates substantial cytotoxic effects on the G361 melanoma cell line when exposed to 414 nm blue light irradiation.</p>

<p>MBC-11 triethylamine, a first-in-class etidronate-araC conjugate, may treat TIBD.</p>

<p>MYC-RIBOTAC, a ribonuclease-targeting chimera (RIBOTAC) specific to the MYC internal ribosome entry site (IRES), comprises an MYC mRNA-binding element tethered</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>Besufetamig is a bispecific antibody targeting programmed cell death protein 1 (PD-1) and the CD3ε chain. It modulates immune cell activity, exerting both immunosuppressive and antitumor effects. Besufetamig holds promise for cancer research.</p>

<p>4-Nitro-3-cresol exhibits ciliate toxicity against Tetrahymena pyriformis and is widely used in biochemical experiments and drug synthesis research.</p>

<p>Odoroside A, from Nerium oleander leaves, induces cancer cell death via ROS/p53, causing apoptosis and cell cycle arrest.</p>

<p>ATPase-IN-3 is an ATPase (ATPase) inhibitor that can be used in the study of metabolism-related diseases.</p>

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

<p>Bcl-2-IN-15 (Compound 13d) is a Bcl-2 inhibitor with an IC50 of 363 nM, which impedes the proliferation of the NCI leukemia cancer cell line [1].</p>

<p>RMC-4998 formic is an orally active inhibitor targeting the GTP-bound state of the KRASG12C mutant. It forms a trimeric complex with intracellular CYPA and the activated KRASG12C mutant, displaying an IC50 value of 28 nM. This compound inhibits ERK signaling and induces apoptosis in KRASG12C mutant cancer cells and is utilized in tumor research.</p>

<p>Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linker for PROTACs with a 3-unit PEG.</p>

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

<p>DPH: antihistamine for cough, nausea, itching, allergy, Parkinson's, sleep aid, cold remedy.</p>

<p>Thalidomide-O-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and</p>

<p>Acrixolimab is a humanized IgG4-κ monoclonal antibody that selectively targets PD-1 [1] [2].</p>

<p>Pacmilimab (CX-072) is a Probody immune checkpoint inhibitor targeting programmed death ligand 1 (PD-L1) with anti-tumor activity for the study of solid tumors.</p>

<p>Feladilimab (GSK3359609) is an IgG4 monoclonal antibody that is an ICOS agonist.</p>

<p>Prolgolimab (BCD-100) is an anti-PD-1 antibody used in melanoma research.</p>

<p>CYP51/PD-L1-IN-4 (compound 14a-2) is a potent dual-target inhibitor of CYP51/PD-L1, displaying IC50 values of 0.17 and 0.021 μM, respectively.</p>

<p>Poly (I:C):Kanamycin (1:1) is an equimolar mixture of Poly(I:C) and kanamycin. TLR3 agonist commonly used as a vaccine adjuvant; enhanced Poly(I:C) stability.</p>

<p>Bcl-2-IN-5: BCL-2 inhibitor, IC50: 0.12 nM (wt), 0.14 nM (D103Y), 0.22 nM (G101V); Cell growth IC50: 0.2 nM, 0.44 nM (RS4;11).</p>

<p>SIN-1 chloride is a moxidomine metabolite with vasodilatory, anti-platelet, and antianginal effects, reducing myocardial ischemia-related damage.</p>

<p>Thalidomide-O-C8-Boc: CRBN ligand for PROTAC creation, derived from Thalidomide.</p>

<p>Lw13 is a PROTAC targeting Hsp90, exhibiting maximal degradation efficacy at a concentration of 0.05 μM in Siha cells. Lw13 induces apoptosis and demonstrates potent antitumor activity both in vitro and in vivo.</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>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>RIPK2-IN-4 is a potent and specific inhibitor of RIPK2 with an IC50 value of 5 nM.</p>

<p>Thalidomide-O-C7-NH2 is a cereblon ligand-linked E3 ligase for PROTAC use.</p>

<p>Chlopynostat (Compound 6c) is an HDAC1 inhibitor with an IC50 value of 67 nM. It induces apoptosis by inhibiting HDAC1, thereby reversing STAT4/p66Shc defects.</p>

<p>MALT1-IN-13 (compound 10m) is an inhibitor of the mucosa-associated lymphoid tissue lymphoma translocation protein (MALT1), forming a covalent and irreversible bond with the MALT1 protease, thereby inhibiting its activity with an IC50 of 1.7 μM. It suppresses the proliferation of ABC-DLBCL and induces apoptosis in ABC-DLBCL HBL1 cells. Additionally, MALT1-IN-13 regulates the mTOR and PI3K-Akt pathways.</p>

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

<p>8-Bromo-cAMP is a cell-permeable cAMP analogue and activator of CAMP-dependent protein kinase A that induces cell death and reduces proliferation.</p>

<p>LC-1-40 is a PROTAC that selectively degrades NUDT1 (DC50=0.97 nM). In mouse models, LC-1-40 selectively inhibits tumor growth induced by MYCN and induces nucleotide damage and apoptosis (cell death) in MYCN-associated tumors. It is applicable for cancer research.</p>

<p>Tauro-β-muricholic acid (TβMCA), a trihydroxylated bile acid, acts as a competitive and reversible FXR antagonist (IC 50 = 40 μM) and exhibits antiapoptotic</p>

<p>Mangafodipir trisodium can enhance contrast in magnetic resonance imaging (MRI) of the liver, is a contrast agent delivered intravenously.</p>

<p>Bcl-B inhibitor 1 is a Bcl-B inhibitor with antitumor activity that binds to and inactivates pro-apoptotic proteins in the BH3 structural domain.</p>

<p>2,4,6-trichloroanisole inhibits the cell viability of CHO and C32 cell lines and apoptosis, antibacterial activity against Plasmodium falciparum.</p>

<p>NCA029 is a potent activator of human caseinolytic protease P (HsClpP) with an EC50 of 0.15 μM. It targets HsClpPP and triggers an ATF3-dependent integrated stress response, resulting in the death of colon cancer cells.</p>

<p>BIO8898: potent CD40-CD154 inhibitor, IC50 of 25 µM, prevents CD40L-induced apoptosis.</p>

<p>Cu(I) chelator 1 (Compound LH2) is a chelating agent specifically targeting the Cu(I) redox state. It inhibits the production of ROS.</p>

<p>AKT-IN-18, an Akt inhibitor, demonstrates an IC50 value of 69.45 μM in A549 cells, effectively impeding Akt activity.</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>

<p>Peptide is p53's amino acids 17-26, contacts Mdm-2 binding domain, also called p53N.</p>

<p>1-Methyl-1H-pyrrolo[2,3-b]pyridine exhibits cytotoxicity against MCF-7 cells and can be used in related research in the field of life sciences.</p>

<p>SB 699551 is a selective 5-HT5A antagonist (Ki=6.31 nM) that enhances 5-HT neuronal function. It inhibits SERT (Ki=25.12 nM),inhibit breast cancer.</p>

<p>S65487 (VOB560) sulfate, a potent and selective Bcl-2 inhibitor, demonstrates activity against BCL-2 mutations, including G101V and D103Y.</p>

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

<p>JAK05 exhibits inhibitory activity against Helicobacter pylori, effectively suppressing strains J63, J196, and J107, with a MIC of 3-5 µg/mL. It shows affinity for binding to H+/K+-ATPase, COX-1/2, TNF-α, and PGE2, and possesses antioxidant and anti-inflammatory properties. In a rat model of ethanol-induced gastric ulcers, JAK05 demonstrates anti-ulcer activity.</p>

<p>Nofazinlimab (CS1003) is a human anti-PD-1 IgG4 monoclonal antibody for the study of unresectable hepatocellular carcinoma (uHCC).</p>

<p>Latikafusp (AMG 256) is a fusion protein that is a PD-1 blocker and IL-21R agonist with antitumor activity.</p>

<p>Thalidomide-derived cereblon ligand linked to a PROTAC technology linker, Thalidomide-O-amido-C3-NH2, is a synthetic E3 ligase ligand-linker.</p>

<p>The compound is a negative control peptide for the Bax inhibitor peptides V5 and P5.</p>

<p>EGFR/BRAFV600E-IN-4 (Compound 10f) is a dual inhibitor of EGFR and BRAFV600E, with IC50 values of 61 nM and 43 nM, respectively. It halts the cell cycle, induces apoptosis in both early and late stages, and inhibits cancer cell growth in vitro, showing broad-spectrum anticancer activity.</p>

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

<p>D-Trimannuronic acid from seaweed induces TNF-α in mouse macrophages; useful in pain, dementia studies.</p>

<p>HDAC6-IN-28 (compound 10C) is a potent inhibitor of HDAC6 with an IC50 of 261 nM. It significantly induces apoptosis in B16-F10 cells and causes S phase arrest. Additionally, HDAC6-IN-28 effectively increases the expression of acetylated-α-tubulin both in vitro and in vivo.</p>

<p>BU 224 hydrochloride is a selective imidazoline I(2) binding site ligand and has antinociceptive and antidepressant-like activities.</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>Cytostatin: natural antitumor, inhibits cell adhesion, blocks melanoma, induces apoptosis, targets PP2A selectively, IC50s: 1.3-3.1 µg/ml &amp; 29 nM.</p>

<p>P-gp inhibitor 16 (compound 14) is an inhibitor of p-glycoprotein. It significantly enhances apoptosis induced by doxorubicin and displays anticancer properties.</p>

<p>Retifanlimab (MGA-012) is a monoclonal antibody targeting programmed cell death protein 1 (PD-1). Retifanlimab is used in studies of Merkel cell carcinoma.</p>

<p>RETligand-1 is a target protein ligand that specifically interacts with RET and can be utilized in the synthesis of the PROTAC LDD39.</p>

<p>BRAFV600E/JNK-IN-1 (Compound 14c) is an inhibitor of JNK1, JNK2, JNK3, and BRAFV600E, with IC50 values of 0.51 μM, 0.53 μM, 1.02 μM, and 0.009 μM, respectively. It also inhibits the phosphorylation of MEK1/2 and ERK1/2. Additionally, BRAFV600E/JNK-IN-1 suppresses tumor cell proliferation, NO release, and PGE2 production, exhibiting both antitumor and anti-inflammatory activities.</p>

<p>Citreoviridin from Penicillium citreoviride blocks brain Na+/K+-ATPase; boosts Na+/K+- and Mg2+-ATPase in microsomes dose-dependently.</p>

<p>MX106-4C is a survivin inhibitor that selectively targets ABCB1-positive colorectal cancer cells. It can work synergistically with Doxorubicin for enhanced anticancer effects or restore Doxorubicin sensitivity in drug-resistant ABCB1 cells.</p>

<p>ADAM-17 (TACE) and MMP inhibitor; attenuates TNF-α processing. Acts in concert with GM6001 to inhibit Chlamydia trachomatis growth.</p>

<p>Pro-GA is a cell-permeable γ-glutamylcyclotransferase (γ-GGCT) inhibitor that inhibit proliferation in multiple bladder cancer cell lines. antitumour.</p>

<p>Lipustobart is an IgG4-kappa humanized monoclonal antibody targeting PDCD1 (programmed cell death 1, PD1, PD-1, CD279), with immunostimulant and antineoplastic</p>

<p>Lacto-N-fucopentaose I is a milk oligosaccharide.</p>

<p>Xerophilusin B from Isodon xerophilus halts ESCC cell growth, causes G2/M arrest, and induces apoptosis.</p>

<p>WD6305 is an effective and selective METTL3-METTL14 PROTAC degrader, with DC50 values of 140 nM and 194 nM for METTL3 and METTL14, respectively. It inhibits m6A modification and the proliferation of acute myeloid leukemia cells while inducing apoptosis. WD6305 also exhibits antitumor activity.</p>

<p>CNDAC hydrochloride, a nucleoside analog, is a metabolite of the sapacitabine.</p>

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

<p>Anticanceragent 204 (Compound 6) is a fluorinated derivative of cinnamamides with anticancer activity. It can arrest the cell cycle of HepG2 cells in the G1 phase and induces apoptosis by reducing mitochondrial membrane polarization (MMP) levels.</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>AUNP-12, a new immune checkpoint modulator, is an inhibitor of the PD-1 pathway.</p>

<p>GPLGIAGQ, a MMP2-cleavable polypeptide, is used as a stimulus-sensitive linker in both liposomal and micellar nanocarriers for MMP2-triggered tumor targeting.</p>

<p>RIP1 kinase inhibitor 9 (compound SY-1) is a selective inhibitor of RIP kinase. It effectively reduces central inflammatory responses caused by seizures. RIP1 kinase inhibitor 9 also obstructs Z-VAD-FMK-induced necroptosis in HT-29 cells, with an EC50 of 7.04 nM.</p>

<p>PROTACPD-L1 degrader-1 is a CRBN-based PD-L1-PROTAC degrader with significant PD-L1 protein degradation capacity. It demonstrates strong PD-L1 degradation activity in 4T1 cells, with a DC50 of 0.609 μM. This compound is applicable to breast cancer research.</p>