Apoptose

<p>Potent GAL2/GAL3 agonist (EC50 = 45.7, 112.2 nM), inactive at GAL1. Reduces appetite, fatty acid uptake in adipocytes, and LH in goldfish; anxiolytic in vivo.</p>

<p>A-1155905 is an MCL-1 inhibitor with anticancer activity, demonstrating a half maximal inhibitory concentration (IC50) of 33.5 Nm and a dissociation constant (Ki) of 0.58 nM. This compound selectively binds to MCL-1 and possesses sufficient affinity to disrupt the MCL-1-Bim complex in live cells. The induction of death in MCL-1-dependent cell lines by A-1155905 is reliant on caspase proteins and occurs through apoptosis.</p>

<p>Tetrathiomolybdate (TM) promotes the dimerization of the metal-binding domain (WLN4) of the cellular copper efflux protein ATP7B through its characteristic</p>

<p>PROTAC RIPK degrader-6 (example 1) is a PROTAC designed for the targeted degradation of RIP Kinase, featuring a RIP2 kinase inhibitor connected through a linker</p>

<p>G-Glu-Val (γ-glutamyl-L-valine, H-Glu-Val -OH), a flavour-regulating dipeptide, is a major contributor to "mellow".</p>

<p>A unique collection of 193 endoplasmic reticulum stress (ER stress) related compounds used for high throughput screening (HTS) and high content screening (HCS);</p>

<p>Vorsetuzumab (Anti-Human CD70 Recombinant Antibody) is a monoclonal antibody targeting the CD70 antibody.</p>

<p>MAO-B-IN-30 is a selective and potent MAO-B inhibitor that crosses the blood-brain barrier with antiproliferative activity and inhibits both MAO-A and MAO-B.MAO-B-IN-30 reduces the levels of TNF-alpha, IL-6, and NF-kB in organisms, and can be used to study Parkinson's-type neurological disorders.</p>

<p>Thalidomide-5-PEG2-Cl is a cereblon ligand that recruits CRBN protein and forms PROTACs through linker conjugation.</p>

<p>DAPK Substrate Peptide is a synthetic peptide substrate for death-associated protein kinase (DAPK) (Km = 9 μM).</p>

<p>PROTAC AR Degrader-8 (Compound NP18) functions as a PROTAC degrader targeting the androgen receptor (AR) and effectively degrades AR-FL in both 22Rv1 and LNCaP cells with DC50 values of 0.018 μM and 0.14 μM, respectively. It also degrades AR-V7 in 22Rv1 cells with a DC50 of 0.026 μM. Additionally, PROTAC AR Degrader-8 inhibits the proliferation of 22Rv1 and LNCaP cancer cells, exhibiting IC50 values of 0.038 μM and 1.11 μM. It induces cell cycle arrest at the G2/M phase and triggers apoptosis in 22Rv1 cells (apoptosis). Demonstrating anticancer efficacy, PROTAC AR Degrader-8 shows activity in both mouse and zebrafish models. [Pink: ligand for target protein AR ligand-33; Black: linker; Blue: ligand for E3 ligase Cereblon]</p>

<p>DTUN: lipophilic radical initiator, starts STY-BODIPY liposome co-autoxidization at 0.2 mM, useful in FENIX assays.</p>

<p>BCL6-IN-10 (Compound WK499) is an inhibitor of BCL6, disrupting its interaction with the SMRT protein and promoting apoptosis, cell cycle arrest, and DNA damage</p>

<p>Biotin-PEG6-Thalidomide is a PROTAC linker based on PEG.</p>

<p>p53-Mdm2 inhibitor 4 inhibits the p53-MDM2 protein-protein interaction.</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>Rasfonin, a fungal metabolite from T. terrophilus, halts mouse splenocyte growth; IC50: 0.7 μg/ml (ConA), 0.5 μg/ml (LPS).</p>

<p>HQY1428 is an orally active CDK12 inhibitor. It impedes DNA replication, causing cell cycle arrest at the G2/M phase in SKOV3 cells, and induces DNA double-strand breaks as well as apoptosis. In the SKOV3 xenograft mouse model, HQY1428 demonstrates antitumor activity. Additionally, when combined with the HER2 inhibitor Lapatinib in the NCI-N87 xenograft mouse model, HQY1428 produces a synergistic therapeutic effect.</p>

<p>Gemcitabine monophosphate disodium salt is a monophosphate derivative of Gemcitabine.</p>

<p>ChoKα Inhibitor-4 is a bioisosteric agent that effectively inhibits human choline kinase α1 (HChoK α1) with an IC50 of 0.66 μM.</p>

<p>Spexin TFA: GAL2/GAL3 agonist (EC50: 45.7/112.2 nM), no activity at GAL1, reduces appetite, fatty acid uptake, and LH secretion; anxiolytic.</p>

<p>Halenaquinone: PI3K inhibitor, stops RAD51 DNA binding &amp; osteoclastogenesis, induces PC12 cell apoptosis.</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>Z-Ala-Ala-Asp-CMK (Z-AAD-CMK) is a selective granzyme B inhibitor that blocks granzyme B protease activity, for inflammatory diseases and tumours.</p>

<p>Oxatomide: Dual H1/P2X7 antagonist, antihistamine, anti-allergic, treats immune diseases, IC50: 0.95 μM (P2X7), 0.43 μM (5-HT).</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>Pamlectabart is a humanised antibody targeting TNFRSF17/BCMA, (ADC) Pamlectabart tismanitin multiple myeloma.</p>

<p>Thalidomide-O-amido-C6-NH2 is a synthetic E3 ligase used for PROTAC creation, containing cereblon ligand and linker.</p>

<p>MEK/PI3K-IN-2 is a potent dual inhibitor (MEK1 IC50: 352 nM, PI3Kα: 107 nM, PI3Kδ: 137 nM) that reduces pAKT, pERK1/2, and hinders tumor cell growth.</p>

<p>AS-99 TFA: potent ASH1L inhibitor, IC50=0.79 μM, combats leukemia, inhibits cell growth, induces apoptosis.</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>KC01 selectively inhibits ABHD16A (IC50: 0.2-0.5 μM), much more potent than KC02 (&gt;10 μM); human ABHD16A IC50: 90±20 nM.</p>

<p>RMC-9805(Zoldonrasib) is a KRAS G12D inhibitor with anti-tumor and anti-proliferative activity for the study of pancreatic cancer.</p>

<p>Apoptolidin, from Nocardiopsis, induces apoptosis, targets mitochondrial ATPase (Ki 4-5 μM), kills glial cells, and has antibiotic and antifungal properties.</p>

<p>KB03-SLF is a protease with the capability to target specific proteins and regulate intracellular protein levels by inducing protein degradation. This mechanism renders KB03-SLF potentially valuable in the suppression of related diseases.</p>

<p>Giloralimab (ABBV-927) is a antibody targeting CD40 with anticancer activity for the study of triple-negative breast cancer and non-small cell lung cancer.</p>

<p>HDAC3-IN-6 (Compound SC26) is a selective HDAC3 inhibitor with an IC50 of 53 nM. It induces PD-L1 expression in a dose-dependent manner and leads to significant apoptosis and reactive oxygen species (ROS) production. HDAC3-IN-6 exhibits strong antitumor efficacy against colorectal cancer.</p>

<p>Anticancer Agent 102, a tetracaine derivative, exhibits anti-cancer activity by inducing apoptosis [1].</p>

<p>TrxR1-IN-2 (Compound 6a) acts as a TrxR1 inhibitor that covalently bonds with the Cys475 and Sec498 sites of TrxR1. This interaction hampers TrxR1 activity, resulting in a redox homeostasis disruption and inducing apoptosis and ferroptosis.</p>

<p>RMC-6291: Oral, covalent KRAS G12C inhibitor, blocks signaling, forms tri-complex with CypA, suppresses RAS activity in tumors.</p>

<p>Conophylline, an alkaloid from Ervatamia microphylla, induces pancreatic cell differentiation and apoptosis, and suppresses HSC.</p>

<p>Azadirone, a limonoid, sensitizes cancer cells to TRAIL by modulating DR4/DR5, survival, and apoptotic proteins.</p>

<p>Nrf2 activator 19 is a compound capable of crossing the blood-brain barrier and acts as an NRF2/HO-1 activator, offering potent antioxidant and neuroprotective effects. It effectively reduces brain damage and minimizes the accumulation of Reactive Oxygen Species (ROS). Additionally, Nrf2 activator 19 inhibits neuronal apoptosis, aiding in the recovery of neural function and motor skills. It has demonstrated significant potential in ischemic stroke research.</p>

<p>Thalidomide-Piperazine 5-fluoride hydrochloride, a derivative of the cereblon (CRBN) inhibitor Thalidomide, serves as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase), facilitating the synthesis of PROTACs [1].</p>

<p>Manelimab is a monoclonal antibody that inhibits programmed death-ligand 1 ( PD-L1 ) [1] .</p>

<p>LS-106 is an orally active, effective epidermal growth factor receptor (EGFR) inhibitor displaying antitumor activity both in vitro and in vivo. It inhibits the kinase activities of EGFR19del/T790M/C797S and EGFRL858R/T790M/C797S, with IC50 values of 2.4 nmol/L and 3.1 nmol/L, respectively, demonstrating stronger inhibition than Osimertinib. LS-106 induces cell apoptosis (Apoptosis), suppresses the proliferation of tumor cells carrying EGFR19del/T790M/C797S, and results in significant tumor reduction in a C797S mutant xenograft model.</p>

<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>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>c-Met/HDAC-IN-4, a dual inhibitor of c-Met/HDAC, exhibits an IC 50 value of 28.92 nM for c-Met. This compound effectively induces G 0 /G 1 phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells. Additionally, c-Met/HDAC-IN-4 suppresses both the proliferation and invasion of breast cancer cell lines.</p>

<p>Chaetoglobosin A, the active compound extracted of Penicillium aquamarinium, is a member of the cytochalasan family. It preferentially induces apoptosis.</p>

<p>ZX782 acts as a GPX4 protein degrader and an inducer of ferroptosis (Ferroptosis), targeting GPX4 for destruction via both the ubiquitin-proteasome system and the autophagy-lysosome pathway. Following the degradation of GPX4 induced by ZX782, there is a significant increase in the accumulation of lipid reactive oxygen species (ROS) in HT1080 cells.</p>

<p>Thalidomide-based E3 ligase ligand with PEG2-C2 linker; used as an immunomodulatory cancer treatment.</p>

<p>Ankaflavin, from red rice fermentation, is a PPARγ agonist with anti-inflammatory properties and selectively kills cancer cells.</p>

<p>TopoisomeraseI/II inhibitor 6 (compound 3i) acts as an effective inhibitor of topoisomerase I and II, with IC50 values of 4.77 µM and 15 µM, respectively. Additionally, it exhibits antiproliferative activity against the human melanoma cell line LOX IMVI, demonstrating IC50 values of 26.7 µM and 25.4 µM.</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>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>Functionalized cereblon ligand with E3 ligase and alkylC5 linker for PROTAC R&amp;D; ready for protein conjugation. Formerly Pomalidomide-linker 4.</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>NQO2-IN-1, a resveratrol analog, is a potent NQO2 inhibito,antitumor,generation of ROS and up-regulation of DR5 (death receptor 5) to promote apoptosis.</p>

<p>Varlilumab (CDX-1127) is a novel human IgG1 anti-CD27 monoclonal antibody. Varlilumab has antitumor activity and can be used to study advanced solid tumors.</p>

<p>BMf-BH3 is a Bcl-2 family peptide, key in HDAC inhibition affecting acetylation balance.</p>

<p>Z-VEID-FMK is a selective caspase-6 peptide inhibitor that irreversibly covalently binds to the enzyme, thereby inhibiting apoptosis and DNA breakage.</p>

<p>SC-2001 inhibits MCL-1 and STAT3, enhances SHP-1, induces apoptosis in breast cancer, and counters STAT3-driven sorafenib resistance in liver cancer.</p>

<p>Albicanol is a biochemical.</p>

<p>Aspochalasin D, isolated from A. microcysticus, shows antibacterial properties and cytotoxicity affecting Ba/F3-V12 cells, with IC50s of 0.49 and 1.9 μg/ml.</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>RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.</p>

<p>N-Acetylpsychosine, also known as α-galactosylated C2-ceramide (d18:1/2:0), exhibits immunostimulatory properties.</p>

<p>Lambertianic acid is a bioactive chemical that has anti-allergic and antibacterial effects.</p>

<p>2-Chloronaphthalene is an organochlorine chemical compound and is a chlorinated derivative of naphthalene. The compound is an isomer for 1-chloronaphthalene.</p>

<p>Fludioxonil (CGA 173506), a phenylpyrrole fungicide, inhibits the growth of B. cinerea from strawberry and blackberry crops.</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>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>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>Ceftiofur hydrochloride (U-67279A) is a stable, broad-spectrum 3rd-gen cephalosporin with antibacterial properties.</p>

<p>Placulumab (ART621), an anti-TNF α monoclonal antibody, targets inflammation, potentially aiding arthritis treatment.</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-amido-C4-N3 (Cereblon Ligand-Linker Conjugates 4) is an E3 ligase ligand-linker conjugate incorporating the Thalidomide-based cereblon ligand and</p>

<p>Ragifilimab (INCAGN-1876), a GITR-targeting agonist antibody, may treat advanced solid tumors.</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>BKM1644 is an effective inhibition of the proliferation of metastatic, castration-resistant PCa (mCRPC) cells.</p>

<p>Anticancer agent 154 (Compound 8h) enhances reactive oxygen species production, causing mitochondrial damage, and promotes cell apoptosis and DNA damage.</p>

<p>Isorhamnetin 3-glucuronide is a useful organic compound for research related to life sciences and the catalog number is T124938.</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>PZ703b is a novel BCL-XL PROTAC degrader with enhanced BCL-2 inhibition.</p>

<p>DHFR-IN-23 (compound 5) is a dual inhibitor of DNA binders/DHFR, exhibiting an IC50 value of 0.08 μM against hDHFR. It serves as an apoptosis inducer and is applicable in research on ER+ breast cancer.</p>

<p>Amorfrutin A is a useful organic compound for research related to life sciences. The catalog number is T124190 and the CAS number is 80489-90-3.</p>

<p>PROTAC EGFR degrader 5 effectively breaks down EGFR Del19 in HCC827 cells at 34.8 nM, inducing apoptosis and G1 arrest.</p>

<p>Fludarabine triphosphate (F-ara-ATP) trisodium inhibits DNA synthesis; IC50 2.3 μM, Ki 6.1 μM, blocks DNA primase, prompts apoptosis.</p>

<p>Solanidine is a cholestane alkaloid isolated from potato species with antitumor effects. Solanidine inhibits proliferation.</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>PI3Kα-IN-14 (compound F8), a potent PI3Kα inhibitor, exhibits an IC50 value of 0.14 nM and markedly diminishes mitochondrial membrane potential, resulting in</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>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>Compound 6b is a synthetic Thalidomide-VHL E3 ligase-linker for PROTACs.</p>

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