Apoptosis

<p>FeTPPS, a decomposition catalyst for 5,10,15,20-tetrakis(4-sulfonatophenyl) porphyrin iron(III) chloride peroxynitrite, neuroprotective.</p>

<p>Rosamultic acid is a useful organic compound for research related to life sciences and the catalog number is T125342.</p>

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

<p>PNT100: 24-base DNA oligo targeting BCL-2 regulatory region; halts tumor cell growth, induces death.</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>BCL6-IN-6 is an inhibitor of Bcl-6 and can be used in studies about diffuse large B-cell lymphoma.</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>

NL13, a Polo-like kinase 4 (PLK4) inhibitor, exhibits an IC 50 value of 2.32 μM. It demonstrates the ability to suppress the viability of PC3 and DU145 prostate cancer cells with respective IC 50 values of 3.51 μM and 2.53 μM. NL13 also inhibits tumor growth in prostate cancer mice. Additionally, it deactivates the AKT signaling pathway by reducing CCNB1/CDK1 levels, leading to G2/M cell cycle arrest and initiating apoptosis through caspase-9/caspase-3 cleavage.

<p>Ajoene from garlic has antibacterial, anticancer, antiplatelet, and antioxidant effects; it combats various bacteria, yeasts, and cancer cells.</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>BK50164: CD73 inhibitor, IC50=13.089µM; binds CD99, KD=1.5µM; anticancer, induces apoptosis, arrests sub-G1.</p>

<p>BRD-810 is a highly selective MCL1 inhibitor (Kd=0.3 nM) capable of inducing tumour cell apoptosis, for haematological malignancies and solid tumours.</p>

<p>LH1307 blocks PD-1/PD-L1 interaction, IC50 = 3 nM (HTRF assay), activates Jurkat cells, EC50s: 79 nM (U2OS), 763 nM (CHO).</p>

<p>FLT3-IN-21 (compound LC-3), a potent FLT3 inhibitor with an IC50 value of 8.4 nM, induces apoptosis and arrests the cell cycle in the G1 phase.</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>

MD-222: a first-in-class, highly potent PROTAC that degrades MDM2, activates p53, and exhibits anticancer properties.

<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>8-Aminoadenosine reduces ATP, blocks mRNA synthesis, and Akt/mTOR signaling, triggering autophagy and apoptosis independently of p53, with antitumor effects.</p>

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

<p>Placulumab (ART621), an anti-TNF α monoclonal antibody, targets inflammation, potentially aiding arthritis treatment.</p>

<p>Prodigiosin hydrochloride is a bioactive red pigment from bacteria with antibacterial, antifungal, anticancer properties, and inhibits Wnt/β-catenin.</p>

<p>JC2-11 is an anti-inflammatory agent blocking NLRC 4, AIM 2, ROS production, caspase-1 activity, and reducing GSDMD, IL-1β, and LDH in vesicles.</p>

Kinamycin C is a bacterial metabolite used as an anticancer agent.

<p>Deoxynyboquinone is a potent inducer of cancer cell death with IC(50) values between 16 and 210 nM.</p>

<p>Isoharringtonine, an alkaloid from Cephalotaxus koreana, inhibits and induces apoptosis in cancer cells.</p>

<p>MS41 is a selective eleven-nineteen leukemia (ENL) PROTAC degrader, with DC50s values of 3.50 nM (MV4;11), 2.84 nM (SEMK2), 3.03 nM (Jurkat), and 26.58 nM (KASUMI1). This compound effectively inhibits the growth of ENL-dependent leukemia cells, induces G1 cell cycle arrest, and increases cellular apoptosis (Apoptosis). Additionally, MS41 reduces chromatin occupancy related to ENL-mediated transcription elongation mechanisms and suppresses the expression of oncogenes and the progression of leukemia.</p>

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

<p>S-Adenosyl-L-methionine (Ademetionine) is an intermediate metabolite of methionine,for treatment of primary biliary cirrhosis and major depressive disorder.</p>

<p>Zigakibart (BION-1301) is a humanized monoclonal antibody targeting TNFSF13 with anti-inflammatory activity for the study of immunoglobulin A nephropathy (IgAN)</p>

<p>PARP1/BRD4-IN-3 (compound HF4) is an effective inhibitor of BRD4 and PARP1, with IC50 values of 1210 nM and 2019 nM respectively. The compound exhibits antiproliferative activity, induces apoptosis (apoptosis) and cell cycle arrest at the G0/G1 phase. Additionally, PARP1/BRD4-IN-3 causes DNA damage and reduces the expression of the Rad51 protein, demonstrating anti-tumor activity.</p>

<p>Poly(I:C):Kanamycin (1:1) sodium is a complex.Poly(I:C) is a TLR3 and RIG-I/MDA5 agonist.Kanamycin is an antimicrobial,Gram-negative and positive bacteria.</p>

<p>Anti-inflammatory agent 42 has anti-inflammatory activity and inhibits the expression of TNF-α and IL-6 in LPS-stimulated macrophages.</p>

<p>Aviculin, a lignan glycoside, exhibits anticancer properties by inducing apoptosis in breast cancer cells with an IC50 of 75.47 μM.</p>

<p>PROTAC Bcl-xL degrader-3 is a potent ROTAC Bcl-xL degrader.</p>

<p>Sincalide ammonium, a CCK analog, stimulates bile release, gallbladder contraction, and sphincter relaxation, aiding in diagnoses.</p>

<p>Irofulven is an agent of DNA-damaging and antitumor. It is used for the treatment of advanced solid tumors, including prostate, ovarian, and pancreatic cancers.</p>

<p>Thalidomide-O-amido-C8-NH2 is a thalidomide-based ligand-linker for PROTAC synthesis.</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>Fludarabine triphosphate (F-ara-ATP) trisodium inhibits DNA synthesis; IC50 2.3 μM, Ki 6.1 μM, blocks DNA primase, prompts apoptosis.</p>

<p>EGFR/HER2/DHFR-IN-3 (compound 4c) serves as an efficacious dual inhibitor specifically targeting EGFR/HER2, exhibiting IC50 values of 0.138 μM for EGFR and 0.</p>

<p>Thalidomide-NH-PEG8-Ts: a synthesized Thalidomide-PEG8 E3 ligase linker for PROTAC-mediated IDO1 degradation.</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>DB2313 is a potent PU.1 inhibitor (IC50=14 nM) that disrupts gene binding, induces AML cell apoptosis, and has anticancer properties.</p>

<p>YL5084 is a selective JNK2/3 inhibitor with IC50s: JNK2 (70 nM), JNK3 (84 nM), and antiproliferative, apoptosis-inducing effects.</p>

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

<p>Alkyl phosphates like (E)-C-HDMAPP activate γδ-T cells, resist hydrolysis, and boost TNF-α synthesis and γδ-T cell count in vivo.</p>

<p>intestinal epithelium-specific growth factor</p>

<p>DB818 dihydrochloride is the dihydrochloride salt form of DB818. It acts as an inhibitor of Homeobox A9 (HOXA9). By reducing the formation of the HOXA9-DNA complex, DB818 dihydrochloride inhibits the growth of AML cell lines OCI/AML3, MV4-11, and THP-1 and induces cell apoptosis (apoptosis).</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>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>

Enniatin A1, a cyclic hexadepsipeptide from Fusarium, induces apoptosis and disrupts ERK, inhibiting ACAT (IC50: 49 μM).

<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>Diazepinomicin, from Micromonospora, blocks EGF-Ras-ERK pathway and induces apoptosis; an anti-tumor agent for K-Ras mutants.</p>

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

<p>Uvarigrin induces tumor multidrug resistance cell apoptosis and triggers Caspase-9 activation. Uvarigrin is isolated from the roots of Uvaria calamistrata.</p>

<p>Thalidomide-based E3 ligase linker for PROTACs with a 3-unit PEG chain.</p>

<p>CPTH2 is an inhibitor of the HAT activity of Gcn5.</p>

<p>hCAIX-IN-23 (Compound 27) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 10.4 nM for hCA IX and 8.5 nM for hCA XII. It not only inhibits hCA activity but also releases NO, exerting dual anti-tumor effects. By reducing the expression of hCA IX and iron regulatory proteins, hCAIX-IN-23 regulates mitochondrial caspase activity and the ferroptosis pathway, thereby inducing apoptosis. This compound is utilized in research focused on renal cancer.</p>

<p>iNOs-IN-5 (Compound BN-4) is an inhibitor of iNOS with an IC50 value of 0.1707 μM, effectively reducing NO expression in RAW264.7 cells stimulated by LPS (HT-D1056). It further diminishes the expression of ROS and lactate dehydrogenase induced by hypoxic injury, displaying anti-necrotic and anti-apoptotic properties. In an SD rat model, iNOs-IN-5 exhibits neuroprotective effects against cerebral ischemia and is capable of crossing the blood-brain barrier.</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>Citreoviridin from Penicillium citreoviride blocks brain Na+/K+-ATPase; boosts Na+/K+- and Mg2+-ATPase in microsomes dose-dependently.</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>Thalidomide-based E3 ligase ligand-linker for PROTAC, with cereblon ligand and C8-NH2 hydrochloride.</p>

<p>LIB3S0280 is a potent inhibitor of TBK1, with an IC50 of 493.9 nM. It suppresses TBK1 downstream signaling by reducing the phosphorylation of IκBα and AKT. LIB3S0280 causes G2/M phase arrest and induces apoptosis in pancreatic cancer cells. Notably, it exhibits significant inhibitory effects on pancreatic cancer cell lines with high TBK1 expression, with a 96-hour IC50 value ranging from 6.64-10.98 μM. LIB3S0280 shows potential for research in pancreatic ductal adenocarcinoma (PDAC).</p>

PROTAC RIPK degrader-2 is a nonpeptidic PROTAC ,and potently targets serine-threonine kinase RIPK2 and has highly selective for RIPK2 degradation.

XZ739: Cereblon-based PROTAC, degrades BCL-XL (DC50 2.5 nM in MOLT-4, 16hr), induces caspase apoptosis.

<p>KSRP-IN-1 (compound 8) acts as an inhibitor of KSRP, inducing cell cycle arrest and apoptosis (Apoptosis). This compound demonstrates antitumor activity.</p>

<p>Apoptosisinducer 28 (Compound X1) is an apoptosis inducer with demonstrated in vitro anticancer activity. It arrests the cell cycle at the G1 phase, promoting cell death and inducing apoptosis by disrupting the mitochondrial membrane potential.</p>

<p>HEMTAC CDK4/6 degrader 1, a PROTAC targeting HSP90/CDK4/6, Kd of 35.7 μM, disrupts B16F10 melanoma cell cycle, and induces apoptosis.</p>

<p>Tyroserleutide HCl, a tripeptide from pig spleen, inhibits tumor growth in vivo/vitro.</p>

<p>Pamlectabart is a humanised antibody targeting TNFRSF17/BCMA, (ADC) Pamlectabart tismanitin multiple myeloma.</p>

<p>Thalidomide-PEG3-NH2: a cereblon-based E3 ligase ligand-linker for PROTAC tech.</p>

<p>HDAC6degrader-5 (Compound 6) exhibits inhibitory and degradative activity against HDAC6, with an IC50 of 4.95 nM and a DC50 of 0.96 nM. It suppresses the release of TNF-α, IL-1β, and IL-6, and prevents apoptosis in liver cells. Additionally, HDAC6degrader-5 demonstrates anti-inflammatory properties in a mouse model of APAP-induced liver injury.</p>

<p>Destruxin B: cyclic peptide from Metarhizium fungus, induces apoptosis in lung cancer via mitochondrial pathway.</p>

<p>Methylene Violet 3RAX is a cationic dye that is a potential photosensitizer in photodynamic therapy and has antitumor activity.</p>

<p>ReACp53 acetate could inhibit p53 amyloid formation and rescue p53 function in cancer cell lines.</p>

<p>Antitumor agent-100 hydrochloride (compound A6), serving as both an apoptosis inducer and molecular glue, exhibits superior anti-tumor activity [1].</p>

<p>JAK/HDAC-IN-2, a potent 2-amino-4-phenylaminopyrimidine dual-target inhibitor, effectively suppresses JAK1/2 and HDAC3/6 at nanomolar concentrations.</p>

<p>PRMT5-IN-31 (Compound 3m), a selective PRMT5 inhibitor (IC50: 0.31 μM), increases hnRNP E1 protein levels by occupying the substrate site of PRMT5 and</p>

<p>PD-166285 is an effective and broadly active inhibitor of protein tyrosine kinase.</p>

Bornyl acetate (Isobornyl acetate) has an anti-inflammatory effect. It is the volatile ingredient in some Chinese traditional herbs and numerous conifer oils.

<p>7-Methoxy-1-tetralone may have insecticidal activity.</p>

<p>Anti-Mouse TNF alpha Antibody is a rat-derived IgG inhibitor targeting mouse TNF alpha.</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>Ferroptosisinducer 6 (6d) is an inducer of ferroptosis (ferroptosis) that exhibits potent potential for Type I/II photodynamic therapy by inducing ROS production, oxidative stress, and mitochondrial damage. Additionally, it demonstrates antitumor activity.</p>

<p>PI3K/HDAC-IN-4 (Compound 31f) is a dual inhibitor targeting PI3K and HDAC, with an IC50 of 0.2μM. It demonstrates high selectivity for HDAC1-3, with IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively. As a potent pan-PI3K inhibitor, PI3K/HDAC-IN-4 has IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. This compound effectively induces apoptosis in tumor cells by concurrently inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. It shows significant antiproliferative activity across various tumor cell lines, such as MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively. PI3K/HDAC-IN-4 is applicable in the study of lymphoma and leukemia.</p>

<p>5α-dihydro Levonorgestrel is a metabolite of the synthetic progestin levonorgestrel .</p>

ATWLPPRAANLLMAAS is a chimeric peptide with anti-angiogenic and potent antitumor capabilities. It effectively inhibits the proliferation, viability, migration, and invasion of human hepatocellular carcinoma cells, and induces apoptosis (apoptosis).

<p>Fisetin quarterhydrate, a natural flavonol present in numerous fruits and vegetables, exhibits benefits including antioxidant, anticancer, and neuroprotective</p>

<p>7,3′,5′-Trihydroxyflavanone, a flavanoid derivative, promotes apoptotic cell death in MCF-7 cells by augmenting Bax expression.</p>

<p>ICy-OH, an iodinated anticancer photosensitizer, excels in deep tissue imaging (640 nm excitation) and triggers pyroptosis in pancreatic cancer cells.</p>

<p>3MB-PP1 is a bulky purine analog and a Polo-like kinase 1 (Plk1) inhibitor.</p>

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

<p>DCZ3301 is a novel aryl-guanidino inhibitor.</p>

<p>Thalidomide-O-amido-C3-COOH is a cereblon ligand-linker for PROTACs, melding Thalidomide with a standard linker.</p>

<p>HTR2A antagonist 1 (Compound 15f) is an HTR2A antagonist with an IC50 of 42.79 nM. It induces sub-G1 cell cycle arrest and apoptosis in colorectal cancer cells by activating the p53/p21/caspase 3 signaling pathway. HTR2A antagonist 1 exhibits good liver microsomal stability and is useful for colorectal cancer research.</p>

<p>PAA5, a polynuclear Au(I) cluster, triggers ferroptosis and has anticancer effects by increasing pH2AX over time.</p>

<p>p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a interaction inhibitor between p53 and MDM2 proteins.</p>

<p>TD52 dihydrochloride, an Erlotinib derivative, inhibits protein phosphatase 2A and induces apoptosis in TNBC by disrupting CIP2A/PP2A/p-Akt signaling.</p>