Apoptosi

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

<p>AS-99 is a first-in-class, potent and selective ASH1L histone methyltransferase inhibitor (IC50= 0.79 μM, Kd= 0.89 μM) with anti-leukemic activity.</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>BMf-BH3 is a Bcl-2 family peptide, key in HDAC inhibition affecting acetylation balance.</p>

<p>Sudubrilimab (HS636) is an IgG1-κ monoclonal antibody targeting PDL1, fused with TGFBR2-ECD to block PD-1/PDL1 and TGF-β in tumors.</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>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>Pimagedine is a prototype therapeutic agent for the prevention of formation of advanced glycation endproducts.</p>

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

<p>TRK-IN-30 (Compound C11) is an inhibitor of tropomyosin receptor kinases (TRK), effectively inhibiting TRKA, TRKB, TRKC, and the resistant mutant TRKAG595R, with IC50 values of 1.8, 0.98, 3.8, and 54 nM, respectively. It also suppresses the activation of downstream PI3K/AKT and MEK/ERK signaling pathways. TRK-IN-30 hinders colony formation and cell migration of Km-12, induces cell cycle arrest at the G0/G1 phase, and triggers apoptosis in Km-12 cells.</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>Z-Asp-CH2-DCB is an irreversible inhibitor of broad spectrum caspase.</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>LD4172 is a PROTAC degrader capable of degrading RIP kinase (RIPK1) with a DC50 in the nanomolar range. When used in combination with TNF-α, LD4172 can induce apoptosis in B16F10 cells. In mouse models, it demonstrates antitumor activity. (Pink: ligand for target protein; Black: linker; Blue: ligand for E3 ligase VHL)</p>

<p>GBM CSCs-IN-1 (Compound (−)-20), a rocaglate derivative, potently inhibits glioblastoma stem cells (GBM CSCs) and exhibits an EC50 of 45 nM by targeting the RNA helicase DDX3. Additionally, it induces apoptosis in these cells.</p>

<p>AXL/Angiokinase-IN-1 (compound 11b) is an inhibitor of AXL/triple angiokinase, with an IC50 of 3.75 nM for AXL expression. This compound suppresses epithelial-mesenchymal transition (EMT) in Bxpc-3 cells and prevents metastasis in lung cancer cells. Additionally, AXL/Angiokinase-IN-1 impairs the functions of vascular and fibroblast cells and induces apoptosis in both cancer and fibroblast cells. It is characterized by low toxicity and favorable metabolic stability.</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>TNF-α (31-45), human is a peptide of tumor necrosis factor-α.</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>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>NSC90616 is a mutant p53 rescue compound [1] .</p>

<p>LZ-07 is an IRAK4 PROTAC degrader (DC50 = 1.14 nM), that, upon degradation of IRAK4, significantly inhibits the expression of cytokines such as IL-6, IL-1β, TNF-α, and IL-10. It is applicable in research related to autoimmune diseases.</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>Antitumor Agent-116 (Compound 6C) is an anti-tumor agent that exhibits anti-proliferative properties and induces apoptosis.</p>

<p>SH-5, an AKT inhibitor potentiates apoptosis and inhibits invasion through the suppression of anti-apoptotic, proliferative and metastatic gene products</p>

<p>AMG-7209 is an effective and selective MDM2-p53 interaction inhibitor.</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>1-Alaninechlamydocin, a fungal metabolite from Tolypocladium sp., inhibits HDACs and reduces cell proliferation with GI50s 5.3-14 nM.</p>

<p>(Rac)-BIO8898 is a chemical compound that serves as an inhibitor of the co-stimulatory interaction between CD40 and CD154.</p>

<p>Onfekafusp alfa (L19TNF), a trimeric fusion of L19 scFv and human TNF, targets malignant glioma.</p>

<p>VEGFR/PARP-IN-1 (Compound 14b) is a dual inhibitor of VEGFR and PARP with IC50 values of 191 nM and 60.9 nM, respectively.</p>

<p>A947 is a potent and selective SMARCA2 PROTAC that induces the degradation of SMARCA2, with significant antitumor activity in SMARCA4-mutant NSCLC cells.</p>

<p>4-N-Nonyloxyphenol, kaolinite nanotube photosensitizer, degrades phenolic pesticides, and disrupts endocrine.</p>

<p>Oxybenzone-d3 (Benzophenone 3-d3) is a deuterium-labeled form of Oxybenzone. Commonly used as a UV filter in tanning and skin protection products, Oxybenzone (Benzophenone 3) acts as an endocrine-disrupting chemical (EDC) that can cross both the placental and blood-brain barriers. It impairs autophagy, alters epigenetic states, and disrupts retinoid X receptor signaling in apoptotic neuronal cells.</p>

<p>Antitumor agent-201 (Compound 10) is a Golgi apparatus-targeting chloride ion transport activator with an EC50 for promoting transmembrane chloride ion transport of 1.53 mol% and an IC50 against HepG2 cells of 7.13 μM. By selectively acting on the Golgi apparatus, Antitumor agent-201 disrupts chloride ion homeostasis, decreases the expression of key proteins such as GM130 and GRASP55, and alters Golgi structure and function. This process induces Golgi apparatus autophagy, triggers apoptosis in cancer cells, and causes cell cycle arrest at the G2/M phase, thereby exhibiting anticancer activity. Antitumor agent-201 is applicable for research in the field of cancer-related diseases.</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>Antiproliferative Agent-25 (Compound 3s4) is a selective PRMT5 inhibitor displaying an IC50 of 0.11 μM.</p>

<p>Opucolimab is a human antibody targeting PD-L1, used in advanced solid tumor research and antibody-drug conjugate synthesis.</p>

<p>SL-01, an oral gemcitabine derivative, potently induces apoptosis to hinder breast cancer more effectively than gemcitabine.</p>

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

<p>Flu-BakBH3 peptide, derived from Bak's BH3 domain, binds tightly to a crucial pocket of Bcl-XL, essential for its anti-death role.</p>

<p>3-Hydroxykynurenine (3-hydroxy-DL-Kynurenine) is an active metabolite of tryptophan and inhibits yeast and rat liver aldehyde dehydrogenase by 97 and 69%.</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>icFSP1 is a mitochondria-associated apoptosis-inducing factor regulator with antitumor activity for the study and treatment of tumor diseases.</p>

<p>Hematein blocks Akt/PKB, Wnt signaling, promotes apoptosis in lung cancer, is a dye from hematoxylin, and inhibits casein kinase II (IC50: 0.74 μM).</p>

<p>Compound 7, also known as RAR/RXR agonist-1, is a chlorinated isomer of retinoic acid and acts as a selective RARα agonist and a partial RXRα agonist. It is capable of activating RXRα, thereby inducing G2/M arrest and apoptosis in cancer cells.</p>

<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>EAD1 is a useful organic compound for research related to life sciences. The catalog number is T35329 and the CAS number is 1644388-26-0.</p>

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

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

<p>12-Deoxyphorbol 13-palmitate, a monomer derived from the roots of Euphorbia fischeriana, exhibits notable antitumor activity. This compound induces cell cycle arrest and apoptosis in gastric cancer cells by modulating key cell cycle regulators, such as cyclin B, cyclin A, and CDC2. Additionally, 12-Deoxyphorbol 13-palmitate significantly diminishes liver fibrosis by targeting APOL2 and impairing the APOL2–SERCA2–PERK–HES1 signaling pathway.</p>

Photosensitizer-5, a photodynamic agent, exhibits cytotoxicity towards HeLa and HepG2 cells, with IC50 values of 10.4 nM and 6.9 nM, respectively. It induces cell death through lipid peroxidation via an iron-independent ferroptosis pathway. Additionally, Photosensitizer-5 displays antitumor activity in HeLa-tumor-bearing mice.

<p>9,11-Dehydroergosterol peroxide is a useful organic compound for research related to life sciences.</p>

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

Antiangiogenic agent 6 (Pt-1) effectively inhibits angiogenesis and induces necroptosis in tumor cells.

<p>YW-N-7 (TFA) is a PROTAC designed to target, inhibit, and degrade RET kinase, demonstrating a DC50 of 88 nM. It exhibits antitumor activity in xenograft mouse models driven by KIF5B-RET, making it a valuable compound for cancer research.</p>

<p>Compound 13b, a potent EGFR degrader, inhibits and induces apoptosis in NSCLC cells with a DC50 of 13.2 nM.</p>

<p>Lisaftoclax, an oral Bcl-2/Bcl-xl inhibitor (IC50: 2 nM &amp; 5.9 nM), treats CLL by promoting leukemia cell death.</p>

<p>Oxidosqualene cyclase inhibitor</p>

<p>PB28: A potent σ2 agonist (Ki 0.68 nM), σ1 antagonist (Ki 0.38 nM), with anti-tumor properties and inhibits SARS-CoV-2 interactions.</p>

<p>Nargenicin: a macrolide antibiotic effective against S. aureus, MRSA, M. luteus; inhibits bacterial DnaE and reduces inflammation and leukemia cell growth.</p>

<p>FGFR1/VEGFR2-IN-2 (compound 6) is a dual inhibitor targeting both VEGFR2 and FGFR1 with IC50 values of 0.025 µM and 0.026 µM, respectively. This compound also exhibits inhibitory effects on EGFR and PDGFR-β, with IC50 values of 0.106 µM and 0.077 µM, respectively. FGFR1/VEGFR2-IN-2 demonstrates significant anticancer activity in the NCI-60 cell lines, showing a growth inhibition (GI) of 60.38%. In T-47D cell lines, it achieves an IC50 of 8.51 µM, exhibits anti-migratory properties, induces cell cycle arrest in the G1 phase, and promotes both apoptosis and necrosis. Additionally, while it has an IC50 greater than 100 µM in MCF-7 cell lines, it does so with an IC50 of 69.17 µM in MDA-MB-231 cell lines and shows no toxicity to normal cells.</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>FW-1 is a type I inhibitor of FLT3, with an IC50 of approximately 1 μM. It exhibits cytotoxic effects in FLT3-mutant AML cells, causes cell cycle arrest at the G0/G1 phase, and induces apoptosis in MV4-11 and MOLM-13 cells.</p>

<p>Sodium 2,4-dichlorophenoxyacetate: selective herbicide, controls broadleaf weeds by disrupting growth and protein/DNA synthesis.</p>

<p>Garivulimab (BGB-A333), a humanized IgG1 monoclonal antibody, binds to PD-L1, blocking PD-1 interaction and exhibiting antitumor activity.</p>

<p>ABBV-167 is a phosphate prodrug of the BCL-2 inhibitor venetoclax.</p>

<p>Enpp/Carbonic anhydrase-IN-1 (compound 1e) is a potent inhibitor of Enpp and carbonic anhydrase.</p>

<p>Thalidomide-PEG4-NH2 HCl, a cereblon ligand-linker for PROTAC.</p>

<p>Dehydroaltenusin is a selective eukaryotic DNA polymerase α inhibitor and a type of antibiotic produced by a fungus (IC50: 0.68 μM).</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>A-1248767, a derivative of A-1210477, is an MCL-1 inhibitor (IC50=23.9 nM; Ki=0.41 nM) known for its anticancer properties. It binds to MCL-1 with high affinity, induces an increase in MCL-1 protein levels inside cells, and promotes apoptosis in tumor cells.</p>

Thalidomide-NH-PEG7, a chemical for creating PROTAC iRucaparib-AP6, selectively degrades PARP1 and is used in ADCs.

<p>Ch282-5, an orally active inhibitor targeting the Bcl-2 protein, promotes mitochondria-dependent apoptosis (Apoptosis) by disrupting mitophagy and the mTOR pathway. It demonstrates antiproliferative effects on colorectal cancer cells, effective both in vitro and in vivo, while also inhibiting metastasis. Further, Ch282-5 augments Oxaliplatin-induced autophagy (Autophagy) by downregulating Mcl-1 protein and raising platelet count, which helps mitigate the adverse effects of Navitoclax.</p>

<p>HDAC6-IN-16 (compound 5c), a quinazolin-4(3H)-one-based inhibitor of histone deacetylase 6 (HDAC6), demonstrates an anticancer effect by inhibiting colony</p>

<p>TRP-601 is a caspase inhibitor.</p>

<p>SA-VA, an intracellular self-assembled PROTAC featuring azide and alkyne groups, selectively degrades VEGFR-2 and EphB4 proteins within U87 cells.</p>

<p>Compound AuL9, also known as iNOS/TopoI-IN-1, is a multi-target hybrid molecule possessing anti-tumor, anti-inflammatory, and antioxidant properties. This compound effectively inhibits the growth of MCF-7 and MDA MB-231 breast cancer cells in vitro, exhibiting IC50 values of 3.5 μM and 6.3 μM respectively. It also prompts DNA damage and apoptosis in these cells by inhibiting human topoisomerase I (TopoI) with a K_i of 2.72 μM. Additionally, iNOS/TopoI-IN-1 reduces the expression of iNOS by suppressing the activation of NF-kB, with a K_i of 1.49 μM.</p>

<p>GPLGIAGQ acetate: MMP2-cleavable peptide; stimulus-sensitive linker for MMP2-targeted liposomal/micellar carriers in photodynamic therapy.</p>

<p>Eldecalcitol, orally active vitamin D analog, boosts bone density and treats osteoporosis.</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>

GPX4-IN-14 (compound 2c) acts as a GPX4 inhibitor, exhibiting both free radical scavenging activity (with a maximum scavenging rate of 72.52%) and anti-tumor proliferation activity in vitro. This compound targets GPX4 protein, elevating lipid peroxide and intracellular Reactive Oxygen Species (ROS) levels, which induces ferroptosis and contributes to its anti-tumor proliferation effects.

<p>Isomahanine is a useful organic compound for research related to life sciences and the catalog number is T125848.</p>

β-ESA, a polyunsaturated fatty acid in seed oils, inhibits Caco-2 cell growth dose- and time-dependently.

<p>EATC, a tetracycline byproduct, combats Pseudomonas to E. coli with MIC50s of 0.75-16 mg/L.</p>

<p>sEH inhibitor-19 (Compound (R)-14i) is an orally active soluble epoxide hydrolase (sEH) inhibitor with an IC50 of 1.2 nM. This compound suppresses the expression of TNF-α and IL-6 and exhibits anti-inflammatory effects in mouse models of acute pancreatitis and Carrageenan-induced edema.</p>

<p>Anticancer agent 130 (compound 8d) significantly induces apoptosis in A549 cells [1].</p>

<p>MDM2ligand 4 is a ligand of MDM2 and can be used in the synthesis of the PROTAC degrader [KT-253].</p>

<p>2,2'-Dihydroxy chalcone inhibits β-glucuronidase (IC50=1.6 μM) and lysozyme (IC50=1.4 μM), and fights E. coli, S. fowleri, S. albicans, S. aureus.</p>

PROTAC GPX4 Degrader-1 (DC-2) is a PROTAC-based compound that efficiently degrades GPX4, demonstrating a degradation concentration (DC 50) of 0.03 μM in HT1080

<p>BRD4 Inhibitor-39 (compound 12m) is an orally active inhibitor of BRD4 with an IC50 of 0.02 μM. It can induce apoptosis and demonstrates antitumor activity.</p>

<p>DC 81: Streptomyces-derived antitumor antibiotic, potent nucleic acid synthesis inhibitor, binds DNA sequences, forms covalent adducts.</p>

<p>Chloranthalactone B, a sesquiterpenoid from Sarcandra glabra, inhibits inflammation via AP-1 &amp; p38 MAPK.</p>

<p>Thalidomide-O-amido-PEG3-C2-NH2 is a cereblon ligand-linked E3 ligase used in PROTAC with a 2-unit PEG.</p>

<p>WEHI-3773 is an inhibitor of the interaction between VDAC2 and either BAK or BAX. It prevents BAX-mediated apoptosis (Apoptosis) by blocking the recruitment of BAX to the mitochondria through VDAC2. Conversely, WEHI-3773 promotes BAK-mediated apoptosis (Apoptosis) by limiting VDAC2's inhibitory sequestration of BAK. This compound shows promise for research in the field of cancer therapy.</p>

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

<p>Aspidin BB, a phloroglucinol from Dryopteris, inhibits cancer by causing cell cycle arrest and apoptosis in HO-8910 cells.</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>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>