Apoptosis

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.

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

Bleomycin A5, or Pingyangmycin, is an oral glycopeptide antibiotic and acts as an antineoplastic and apoptosis inducer.

Pomalidomide-C5-Dovitinib (compound 2) is a PROTAC that links Pomalidomide and Dovitinib via a CRBN connector, exhibiting potent antiproliferative activity in

Tubulin polymerization-IN-45, a tubulin-targeting agent, acts as a tubulin polymerization inhibitor by binding to the tubulin's colchicine site.

Sandalore boosts hair growth, reduces cell death, and raises IGF-1, acting on olfactory receptor OR2AT4.

Diethyl phthalate disrupts endocrine and induces apoptosis in PC12 cells; common in plastics, personal care items.

Apoptosisinducer 24 (Compound 4) inhibits the proliferation of gastric cancer cells with an IC50 range of 1.2-4.8 μM. It arrests the cell cycle at the G2/M phase, induces apoptosis in BGC-823 cells, and causes mitochondrial dysfunction. In mice, Apoptosisinducer 24 exhibits antitumor activity without significant toxicity, having an LD50 of 91.2 mg/kg.

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.

Boanmycin, an antibiotic exhibiting antitumor activity, induces cellular senescence and apoptosis [1] [2] [3].

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.

Halleridone, a natural product, is identified in Teuanchum decipiens and Abeliophyllum distichum.

Lacto-N-fucopentaose I is a milk oligosaccharide.

Tubulin polymerization-IN-79 (Compound C20) acts as an inhibitor of microtubule polymerization. It exhibits significant antiproliferative activity against esophageal cancer cells, such as KYSE450 (IC50=0.36 μM) and EC-109 (IC50=0.63 μM). In esophageal cancer cells, Tubulin polymerization-IN-79 occupies the colchicine binding site, disrupting the microtubule network's integrity, activating the Hippo signaling pathway, downregulating the oncogenic protein YAP, and inducing G2/M phase arrest and apoptosis. This compound shows promise for esophageal cancer research.

BTK ligand 12 is a PROTAC target protein ligand serving as an active control for NRX-0492 (a BTK degradator).

Compound B12, a JOA derivative, collapses MMP to induce apoptosis, inhibits cloning/migration, and has an IC50 of 0.39 μM against HGC-27 cells.

UZH1a: METTL3 inhibitor, IC50 280 nM, used for epitranscriptomic modulation and has antitumor properties.

Eps8 peptide 327 is an HLA-A*2402-restricted peptide antigen derived from the Eps8 protein. It exhibits potent antitumor activity and significant cytotoxicity. Eps8 peptide 327 effectively inhibits cancer cell proliferation, induces apoptosis, and disrupts the EGFR signaling pathway by inhibiting the expression of downstream signals such as IL-2, TNF-α, and IFN-γ, as well as impeding the Eps8/EGFR interaction. It significantly suppresses tumor growth in HT-29 xenograft models.

GPX4-AUTAC is an autophagy-mediated degrader (AUTAC) targeting GPX4. It consists of the inhibitor ML162-yne, a degradation tag FBnG, and a glycol linker. GPX4-AUTAC facilitates the ubiquitination of GPX4 by the E3 ligase TRAF6 and enhances its interaction with GPX4 and p62, leading to selective autophagy-dependent degradation of GPX4. This compound significantly induces ferroptosis and demonstrates potent anticancer activity in breast cancer cells, patient-derived organoids (PDOs), and MDA-MB-231 tumor xenograft mouse models. It shows strong synergy when used in combination with Sulfasalazine (SAS) or chemotherapy drugs (Paclitaxel or Cisplatin).

FHD-286 is an inhibitor of BRM/BRG1 ATPase and can be used for studies on the treatment of BAF-related disorders such as acute myeloid leukemia.

PROTACc-Met degrader-5 (Compound D19) is an orally active c-Met PROTAC degrader, with a DC50 of 0.42 nM in EBC-1 cells and 0.32 nM in Hs746T cells. It effectively induces apoptosis, causes G1 cell cycle arrest, and inhibits cell migration and invasion. This compound shows strong antiproliferative and degradative effects on c-Met-dependent cancer cells and those resistant to Tepotinib.

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

Isorhamnetin 3-glucuronide is a useful organic compound for research related to life sciences and the catalog number is T124938.

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

"(±)-Enterodiol, the racemate of Enterodiol, is metabolized from lignans found in whole-grain cereals, nuts, legumes, flaxseed, and vegetables by human intestinal bacteria. This compound exhibits apoptotic effects in colorectal cancer (CRC) cells and has been identified to possess anti-cancer activities [1] [2]."

Minocycline is a useful organic compound for research related to life sciences. The catalog number is T131626 and the CAS number is 10118-90-8.

BAD (103-127) human peptide from BH3 domain, blocks Bcl-xL, 800x more binding than 16-mer.

Thalidomide-5-propoxyethanamine acts as a cereblon (CRBN) ligand derived from Thalidomide, and it serves the purpose of recruiting the CRBN protein.

CH091138 is a potent and selective KRASG12D PROTAC degrader, exhibiting a DC50 value of 148.3 nM in HeLa cells and 469.8 nM in AsPC-1 cells. It selectively targets both exogenous and endogenous KRASG12D through the VHL-mediated ubiquitin-proteasome system, without affecting KRASWT or other KRAS mutants (G12C/G12S/G12V). CH091138 demonstrates significant antitumor activity by inducing apoptosis (apoptosis) in tumor cells and is applicable for research in pancreatic and colon cancers.

Frangulin B (Compd 11g) exhibits anticancer properties and acts as an effective RecQ helicase inhibitor. It induces apoptosis in both HCT-116 and MDA-MB-231 cells and can arrest HCT-116 cells in the G2/M phase.

Thalidomide-O-C8-Boc: CRBN ligand for PROTAC creation, derived from Thalidomide.

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.

CPTH2 is an inhibitor of the HAT activity of Gcn5.

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.

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

Monactin is a Marcrotetrolide antibiotic produced by cycloheximide producing species of Streptomyces. It is a homolog of nonactin from the same species.

TCHQ, a pentachlorophenol metabolite, toxic to trout liver cells, increases ROS, disrupts mitochondria, and causes necrosis in splenocytes. EC50: 1.55 μM.

GNE-1567 is a potent ERα PROTAC degrader and a selective antagonist of XIAP, with a Kd of 0.03 μM. It is applicable in breast cancer research.

Biotin-DEVD-CHO (TFA) is the biotin-conjugated form of the caspase-3 and caspase-7 inhibitor Ac-DEVD-CHO. It can be utilized for affinity purification of active caspase-3, -6, -7, and -8 and is also applicable for in vitro detection of active caspase-3.

FLT3/IRAK4-IN-1 is a selective inhibitor of FLT3 and IRAK4, exhibiting significant activity against FLT3-WT (IC50= 1.95 nM), FLT3-D835Y (IC50= 3.22 nM), and IRAK4 (IC50= 53.72 nM). It demonstrates low cytotoxicity towards normal bone marrow cells, effectively promotes apoptosis, and has potential to overcome resistance. FLT3/IRAK4-IN-1 can be utilized in studies of acute myeloid leukemia (AML).

Diafenthiuron is a widely utilized thiourea-based pesticide that effectively hinders mitochondrial activity in insect pests.

PF-543 (Sphingosine Kinase 1 Inhibitor II), a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.

Compound 24a, an FPR1 antagonist, demonstrates potent inhibition of the formyl peptide receptor 1 (FPR1) with an IC50 value of 25 nM.

BAY1082439, an orally bioavailable, selective inhibitor of PI3Kα/β/δ, demonstrates high efficacy in inhibiting the growth of Pten-null prostate cancer [1][2].

Perfluorodecanoic acid is a biochemical.

Cefatrizine inhibits eEF-2 kinase, affecting apoptosis, autophagy, and ER stress in cancers.

C-Peptide 1 (rat) is a polypeptide isolated from proinsulin. C-Peptide acts as a β-catenin/GSK-3β activator, influences Na/K-ATPase, regulates apoptosis.

Ferroptosis-IN-12 (Cpd-A1) is an inhibitor of ferroptosis. It effectively suppresses ferroptosis in mouse renal tubular epithelial cells (mTECs) treated with Erastin and improves renal function in dose-dependent manners in mouse models of acute kidney injury (AKI) induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). This compound also reduces renal tubular damage and eliminates inflammation. Exhibiting good plasma stability and high distribution in renal tissues during pharmacokinetic studies in mice, Ferroptosis-IN-12 shows promising potential for research in the field of AKI.

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

ARD-61: potent PROTAC, degrades AR/PR in AR+ cancers, triggers apoptosis, inhibits tumor growth in mice.

BMSpep-57: Macrocyclic peptide, inhibits PD-1/PD-L1, IC50=7.68 nM, binds PD-L1 (Kd=19 nM/MST, 19.88 nM/SPR), boosts T cell IL-2 in PBMCs.

Ganglioside GD3 disodium salt is a melanoma-associated antigen often targeted in immune therapy for melanomas.

[Ru(DIP)2TAP]Cl2, a Ruthenium(II) polypyridyl compound, serves as a photosensitizer and is utilized in photodynamic therapy (PDT) research.

Thujopsene, a sesquiterpene found in T. dolabrata, exhibits a wide range of biological activities. It inhibits Na+/K+-ATPase and cytochrome P450 (CYP) isoform CYP2B6 with IC50 values of 25.9 µg/ml and Ki of 0.8 µM, respectively. Additionally, thujopsene demonstrates antimicrobial efficacy against both Gram-positive and Gram-negative bacteria, such as S. aureus, M. luteus, and S. typhimurium, with MICs ranging from 25-50 µg/ml. It also suppresses antigen-induced β-hexosaminidase release in IgE-sensitized RBL-2H3 mast cells (IC50= 25.1 µM) and shows cytotoxicity against A549 non-small cell lung cancer cells with an LC50 of 35.27 µg/ml. Furthermore, thujopsene causes mortality in mites D. farinae and T. putrescentiae, with LC50s of 9.82 and 10.92 µg/cm2, respectively.

RETligand-3 is the ligand for PROTAC QZ2135, which targets RET.

PROTACPI3Kδ degrader-1 is a covalent PI3Kδ-targeting PROTAC degrader that targets lysine, with a DC50 of 3.98 nM. It exhibits potent antiproliferative activity and selective PI3Kδ inhibition (IC50: 8 nM). Additionally, PROTACPI3Kδ degrader-1 effectively degrades p-AKT, induces cell cycle arrest in the G1 phase, and promotes apoptosis and autophagy. It also significantly suppresses tumor growth in the SU-DHL-6 xenograft mouse model.

Human PD-L1 inhibitor II is a potent PD-L1 inhibitor with anti-cancer activity.

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

BDK-IN-1 (compound (-)-43) is a BDK inhibitor with an IC50 of 0.23 μM and a maximum inhibition rate of 90%. It reduces phosphorylated-E1 levels and is useful in the study of cardiac metabolic diseases.

HMGB1-IN-2 (compound 15) is a selective inhibitor of the highly conserved nuclear protein HMGB1, demonstrating no inhibitory effect at an IC50 of 20.2 μM in

dASK1-VHL is an orally active PROTAC degrader targeting ASK1. It effectively binds to VHL, promoting the selective degradation of ASK1. By reducing ASK1 protein levels, dASK1-VHL inhibits the activation of p38 MAPK and decreases liver lipid content, offering new insights for MASH research.

KB02-SLF, a molecular glue, degrades nuclear FKBP12 by modifying E3 ligase DCAF16 and extends protein degradation.

SB-T-1214 (SBT) is a taxane-based drug known for its ability to effectively suppress the expression of stem cell-related genes (Oct4, Sox2, and c-Myc) and induce apoptosis in drug-resistant tumorigenic CD133+/CD44+ colon cancer spheroids. In Pgp+ DLD-1 human colon tumor xenograft mouse models, SB-T-1214 successfully inhibits tumor growth. This compound is relevant for anti-tumor research, particularly against drug-resistant tumors such as colon, pancreatic, and renal cancers.

Insect repellent M 3535 is a bug repellant.

DP-15 acts as a degrader of GSPT1 and BRD4, with DC50 values of 5.25 nM and 0.48 nM, respectively. This compound exhibits antiproliferative activity in AML and NHL cells, showing IC50 values in the nanomolar range, induces G1 phase cell cycle arrest, and triggers apoptosis in MOLM13 cells. Additionally, DP-15 demonstrates anti-leukemic properties in the MOLM-13 xenograft mouse model. [Pink: ligand for target protein JQ-1 carboxylic acid; Black: linker; Blue: ligand for E3 ligaseCereblonThalidomide-5-OH]

Aloeresin G, a chromone glycoside isolated from Aloe, exhibits a moderate inhibitory effect on TNFα-induced NF-κB transcriptional activity, evidenced by an IC50

CST626 is a PROTAC degrader that targets XIAP, cIAP1, and cIAP2.

GSNOR-IN-1 is a prodrug of GSNOR-IN-2 and functions as an S-nitrosoglutathione reductase (GSNOR) inhibitor capable of crossing the blood-brain barrier. GSNOR-IN-1 offers significant protective effects against damage induced by oxygen-glucose deprivation/reoxygenation (OGD/R). It regulates calcium signaling and synaptic function through Clstn1 S-nitrosylation and inhibits neuronal apoptosis. Additionally, GSNOR-IN-1 markedly reduces infarct volume in rat models of ischemic stroke while enhancing neurological function. With its neuroprotective properties, GSNOR-IN-1 holds potential for ischemic stroke research.

Osajin is the major bioactive iso avone present in the fruit of Maclura pomifera. It has antitumor, antioxidant, and anti-inflammatory activities.

Targaprimir-96 is a potent microRNA-96 (miR-96) processing inhibitor.

GDC-0152-acetamide is a pan-antagonist of apoptosis inhibiting proteins (IAPs). It induces the autoubiquitination and subsequent degradation of cIAP1/2, activates the non-canonical NF-κB pathway, and promotes the secretion of TNF-α, leading to apoptosis in tumor cells. GDC-0152-acetamide holds potential for research in ERα-positive breast cancer.

AMPK-IN-6 (compound 13a) is a potent AMPK inhibitor with an IC50 value of 0.093 µM. It induces apoptosis and suppresses autophagy. Additionally, AMPK-IN-6 exhibits antiproliferative activity and holds potential for research into pulmonary arterial hypertension.

ZS3-046 is a TAF1 PROTAC degrader that facilitates the ubiquitination and subsequent degradation of TAF1. It can activate p53 and induce apoptosis in acute myeloid leukemia (AML) cells. Additionally, ZS3-046 demonstrates anti-tumor efficacy in AML xenograft mouse models.

Phosphocreatine dipotassium, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives.

CQ627 is a molecular glue that targets the degradation of RIOK2. It effectively recruits the E3 ubiquitin ligase RNF126, inducing the proteasomal degradation of RIOK2 via the ubiquitin-proteasome system (UPS) in MOLT4 leukemia cell lines, with a DC50 value of 410 nM. Additionally, CQ627 induces apoptosis in a dose-dependent manner in these cells, blocking the cell cycle at the G2/M phase, and exhibits antiproliferative activity across various cancer cell lines. It also demonstrates in vivo anticancer activity in MOLT4 xenograft mouse models.

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

RSM3 TFA is a stapled peptide and an inhibitor of METTL3-METTL14, exhibiting a dissociation constant (Kd) of 3.10 μM. It inhibits tumor growth and induces cell apoptosis. RSM3 TFA is utilized in cancer research.

STEP-IN-1 (Compound 14b) is a potent and selective inhibitor of STEP, with an IC50 of 5.27 μM. It offers neuroprotective effects by safeguarding neuronal cells from glutamate-induced toxicity, reducing intracellular reactive oxygen species (ROS) accumulation, and inhibiting apoptosis. STEP-IN-1 is applicable in research related to neurodegenerative diseases.

Apoptosis Inducer 29 (compound Y9) demonstrates anticancer efficacy in non-small cell lung cancer by inducing lysosomal dysfunction and apoptosis, and exhibits superior performance to Gboixn both in vitro and in vivo.

ZYH-23 is a potent inhibitor of necroptosis. It targets HSP90 to inhibit the phosphorylation of RIPK1, RIPK3, and MLKL, effectively blocking programmed cell necrosis.

DSTYSLSSTLTLSK TFA detects infliximab, a chimeric IgG1 antibody targeting TNF-α.

hCAIX/XII-IN-13 functions as an inhibitor targeting specific human carbonic anhydrases (hCA) IX and XII, crucial in tumor-related processes. Demonstrating efficacy, this compound offers inhibitory K i values of 0.08 µM for IX and 0.06 µM for XII. Additionally, under hypoxic conditions, hCAIX/XII-IN-13 enhances the effectiveness of Doxorubicin on MCF-7 cells by promoting G2/M phase cell cycle arrest and increasing apoptosis.

PROTACEGFRdegrader 14 is a potent and selective EGFR PROTAC degrader with a DC50 value of approximately 2.9 nM against EGFRL858R/T790M/C797S and a Dmax of 93.1%. It induces the selective degradation of EGFRC797S via a VHL and proteasome-dependent mechanism, downregulating EGFR-related transcriptomes. PROTACEGFRdegrader 14 exhibits high selectivity for EGFRWT, induces cell cycle arrest and apoptosis, and effectively inhibits tumor growth. It is applicable for research on non-small cell lung cancer (NSCLC).

PROTAC XPO1 degrader-1 (Compound 2c) is an XPO1 degrader. It exhibits anti-proliferative effects, induces apoptosis, inhibits NF-κB activity, and causes cell cycle arrest at the G1 phase. PROTAC XPO1 degrader-1 is applicable to research on hematological malignancies.

VTX-0811 is a human IgG4 monoclonal antibody (mAb) that targets PSGL1/CD162. It modulates immune signaling pathways by enhancing TNF-α/NF-κB and chemokine-mediated signaling while reducing oxidative phosphorylation, fatty acid metabolism, and Myc signaling. VTX-0811 increases the proportion of CD8+ T cells among infiltrating T cells and exhibits antitumor activity in humanized mouse PDX models of melanoma.

Obestatin (human) is an endogenous ligand for G-protein eurythmic entity 39 formed by shearing of preproghrelin and can be used to study obesity.

ZZM-1220, a covalent inhibitor of histone lysine methyltransferase G9a/GLP, exhibits IC50 values of 458 nM for G9a and 924 nM for GLP.

PROTACROR1degrader-1 (Compound 11d) serves as a PROTAC degrader targeting the pseudokinase ROR1, with the capability of degrading ROR1 in NSCLC cells at a DC50 of 40-80 nM. It induces PARP cleavage and apoptosis in NCI-H23 cells. [Pink: ligand for target protein ROR1 ligand-1; Black: linker; Blue: ligand for VHL E3 ligase (S,R,S)-AHPC]

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

VK-28 is a brain permeable iron chelator with neuroprotection. VK-28 inhibits basal as well as iron-induced mitochondrial lipid peroxidation.

KWCN-41, Selective RIPK1 inhibitor (IC50=88 nM), inhibits necrosis specifically, anti-inflammatory effects.

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.

VEGFR-2-IN-68 (13b) is an inhibitor of VEGFR-2 with an IC50 value of 41.51 nM. It can induce apoptosis and cause G2/M cell cycle arrest, as well as exhibit anti-cancer metastasis properties.

Met-12 is a peptide inhibitor of the Fas receptor. It suppresses Fas receptor-mediated apoptosis in photoreceptor cells and reduces Caspase activation, making it a potential candidate for research on photoreceptor protectants.

HMGB1-IN-1 (compound 6) exhibits potent inhibition of NO production in RAW264.7 cells, with an IC50 of 15.9 ± 0.6 μM, and effectively disrupts the HMGB1/NF-κB/