Apoptosis

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.

Apoptosisinducer 26 (compound [AgCl(dap2SH)(PPh3)2]) is a mononuclear Ag(I) ligand-based autophagy inducer that exhibits antibacterial and anticancer activities against various bacterial strains and cancer cell lines. This compound facilitates the accumulation of Ag(I) ions in the periphery of bacteria, effectively inhibiting the growth of both Gram-positive (+) and Gram-negative (-) bacteria. Additionally, Apoptosisinducer 26 can intercalate between the base pairs of CT DNA, inducing apoptosis in A549 cells. It also possesses radical scavenging properties, which helps prevent oxidative stress.

Phenamet is a bioactive chemical.

Ferroptosisinducer-4 (Compound 5) is a phospholipid-based ferroptosis inducer featuring a terminal double bond at the sn-2 position. It exhibits significant cytotoxicity towards HT-1080 cells with an IC50 value of 18 μM. The toxicity mechanism involves the generation of lipid peroxides and oxidative damage to the cell membrane induced by the terminal double bond. Ferroptosisinducer-4 can be utilized in studies pertaining to the regulation of ferroptosis.

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

anti-TNBC agent-1 targets TNBC effectively, with IC50 of 0.20-0.27 μM, inducing apoptosis and G1 arrest in SUM-159 cells.

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.

Enniatin complex: fungal cyclohexadepsipeptides inhibit enzymes, induce cancer cell apoptosis, and have ionophoric, antibiotic, and hypolipidemic effects.

Compound 25b, an FPR1 antagonist, exhibits potent inhibition of the formyl peptide receptor 1 with an IC50 of 70 nM.

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

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

Solanidine is a cholestane alkaloid isolated from potato species with antitumor effects. Solanidine inhibits proliferation.

Sorafenib D4 is deuterium-labeled Sorafenib, a multi-kinase inhibitor (Raf-1, B-Raf, VEGFR-3) with IC50s: 6, 20, 22 nM.

"(±)-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]."

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

EGFR-IN-83 (Compound 9), an EGFR inhibitor with an IC50 of 2.53 nM, exhibits antiproliferative effects on MCF-7 and MDA-MB-231 cell lines, with respective IC50

AlbA-DCA, a compound of Albiziabioside A and dichloroacetate, boosts ROS and reduces lactic acid in tumors, killing cancer cells and triggering apoptosis.

VEGFR-2-IN-64 (Compound 28) is an inhibitor of VEGFR2 with an IC50 of 27.8 nM. It suppresses the proliferation of cancer cells A549, T-47D, and Caco-2, exhibits anti-migration and anti-colony formation activities in T-47D cells, and induces apoptosis in T-47D cells.

VB-85247 is a STING agonist that, by activating the STING pathway, induces the upregulation of inflammatory cytokines IFNα/β, TNFα, IL6, and CXCL10, as well as the maturation and activation of dendritic cells. It can lead to the regression of tumors within the bladder and is applicable in bladder cancer research.

MET/PDGFRA-IN-1 (compound 8c) serves as an inhibitor of MET and PDGFRA proteins, displaying an IC50 of 36 μM against MET.

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

Apoptosisinducer 27 (compound 1c) is a potent inhibitor of MDA-MB-231 breast cancer cells, demonstrating an IC50 of 12.8 μM and inducing early apoptosis in these cells. Additionally, it can bind to DNA molecules as well as Bax and Bcl-2 proteins, thereby inducing DNA damage.

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.

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.

PROTAC Bcl-xL degrader-1 targets Bcl-xL & IAP E3 ligases, degrades Bcl-xL, toxic to human platelets & MyLa 1929 (IC50: 62 nM, 8.5 μM).

Ferroptosis-IN-16 (Compound 13l) acts as a specific inhibitor of ferroptosis, demonstrating EC50 values of 0.7 nM in ES-2 cells and 0.9 nM in LX-2 cells. It effectively alleviates acute liver injury induced by Acetaminophen in mouse models and shows excellent metabolic stability in mouse liver microsomes.

SBP-0636457: SMAC mimetic, IAP inhibitor, binds BIR-domains (Ki=0.27μM), potential in tumor/cancer research.

CXCR4-IN-2 (compound A1), a potent bifunctional fluorinated small molecule, inhibits CXCR4 and exhibits anticancer properties by exerting cytotoxicity (IC 50:

RIP1-IN-1 is an orally bioavailable RIP1 inhibitor with a high binding affinity (Kd: 110 nM). This compound exhibits significant activity against necroptosis and effectively suppresses necrosome formation by inhibiting the phosphorylation of RIP1, RIP3, and MLKL pathways. RIP1-IN-1 can inhibit necroptosis and is applicable in research on acute liver injury.

[1,1'-Biphenyl]-3-amine is an inhibitor of MAO-A and MAO-B and can inhibit the cell viability of HT-29, HEK 293, and MCF-7 cells.

M24 inhibits Mcl-1 (Ki = 0.33μM), blocks HepG2 cell growth, and triggers apoptosis.

XZ338 is a highly selective degrader targeting BCL-XL without degrading BCL-2. It exhibits an IC50 value of 3.7 nM against MOLT-4 cells and possesses antiproliferative properties, making it useful for cancer research.

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.

FLT3/HDAC-IN-1 is a dual inhibitor targeting FLT3 and HDAC, with IC50 values of 30.4 nM for FLT3 and 52.4, 14.7 nM for HDAC1/3, respectively. It induces apoptosis in MV-4-11 cells and exhibits antiproliferative effects against BaF3 cells transformed by FLT3 mutations. FLT3/HDAC-IN-1 is useful for research on refractory solid tumors and hematological malignancies.

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

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.

p53-HDM2-IN-1 is a potent inhibitor of the p53-HDM2 protein-protein interaction, demonstrating an inhibitory concentration (IC 50) of 0.103 μM.

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

Conjugated 18-C ω-6 fatty acid from Jacaranda seeds, induces cancer cell apoptosis via oxidative stress; metabolizes to cytotoxic CLA.

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.

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.

SF1126 is a first-in-class PI3K/BRD4 inhibitor and RGDS-conjugated LY294002 prodrug, enhancing solubility and targeting tumor integrins.

EGFR-IN-107 (compound 3r) is an orally active EGFR inhibitor with IC50 values of 0.4333 μM for EGFRWT and 0.0438 μM for EGFRL858R/T790M. It exhibits antiproliferative activity, effectively inhibiting the proliferation of H1975 cells and inducing apoptosis (apoptosis). EGFR-IN-107 is applicable in cancer research.

p38α inhibitor6 (compound 19) is a p38α inhibitor with an IC50 value of 0.68 μM. It induces apoptosis, arrests the cell cycle in the G0 and G2/M phases, reduces TNF-α concentration, upregulates the expression of the tumor suppressor gene p53, increases the Bax/BCL-2 ratio, and activates caspase3/7.

DRI-C21041 DIEA serves as an inhibitor of CD40/CD40L interaction, exhibiting an inhibitory concentration (IC50) of 0.31 μM.

PG-11047 2HCl treats genitourinary, immune, genetic, ocular, blood/lymphatic disorders, and aids lymphoma/prostate cancer research.

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.

eIF4E-IN-2 effectively inhibits eIF4e, crucial for research on diseases like cancer.

Pipernonaline is a useful organic compound for research related to life sciences. The catalog number is T124000 and the CAS number is 88660-10-0.

PRDX1-IN-2 (compound 15) is a selective inhibitor of the antioxidant enzyme Peroxiredoxin 1 (PRDX1) with an IC50 of 0.35 μM. It reduces mitochondrial membrane potential in SW620 cells, potentially due to increased ROS resulting from PRDX1 inhibition, leading to apoptosis. PRDX1-IN-2 is applicable in colorectal cancer research.

P53/TLR2 modulator-1 (Compound Z9) is an agent that targets both the P53 pathway and TLR2, exhibiting radioprotective properties. It mitigates apoptosis by inhibiting radiation-induced expression of P53 and Bax. Concurrently, it enhances the TLR2 pathway by upregulating downstream proteins MyD88 and P65, which promotes secretion of cytokines like IL-6, providing radioprotective effects. P53/TLR2 modulator-1 shows significant radioprotective activity in AHH-1 and HUVECs cells, enhances survival rates in C57BL/6J mice exposed to lethal radiation doses, and alleviates radiation-induced damage to their hematopoietic system, intestinal villi, and spleen. It is applicable for research on radiation-related diseases.

DS-5272 is a potent and orally active inhibitor of p53-MDM2 interaction.

RIPK2-IN-2, a RIP2 kinase PROTAC inhibitor, blocks proinflammatory signaling in autoinflammatory diseases.

Anticanceragent 273 (Compound 9q) is an effective anticancer compound identified from matrine. It inhibits cancer cell proliferation, with an IC50 of 4.48 μM against HeLa cells. Anticanceragent 273 exerts its anticancer effects by modulating PI3K/AKT expression and activating activating transcription factor 4 (ATF4), which induces endoplasmic reticulum stress and triggers apoptosis. It holds potential for cancer research, including cervical cancer.

Cereblon ligand for PROTAC R&D; has E3 ligase, alkylC1-PEG3-alkylC3 linker, terminal amine. Part of Arvinas-licensed tool molecules.

ECDD-S16 is a potent inhibitor of pyroptosis. It effectively suppresses pyroptosis in Raw264.7 cells activated by surface and endosomal TLR ligands.

USP7-IN-9 is a potent USP7 inhibitor (IC50 = 40.8 nM), induces apoptosis, arrests RS4;11 cells, and modulates key oncoproteins.

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

Trichostatin C, a natural glycosylated hydroxamate, is a histone deacetylase inhibitor with antifungal properties and can induce cell differentiation.

eIF4A3-IN-5 potently inhibits eIF4AI/II, promising for cancer research.

D-CopA3 is an inhibitor of MDM2 and an activator of the p53 signaling pathway. It exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO with IC50 values of 15-18 μM and induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of the cell cycle inhibitor protein p21Cip1/Waf1, enhances mucosal barrier function, and reduces infiltration of inflammatory mediators. It shows anti-inflammatory properties in mouse models of acute enteritis induced by C. difficile toxin A and chronic colitis induced by DSS. Additionally, D-CopA3 demonstrates antitumor activity in a mouse HCT-116 xenograft model.

BM-1074 is a potent and highly efficacious inhibitor of Bcl-2/Bcl-xL with Ki value of < 1nM [1].

F1324 TFA is a potent, high affinity peptidic inhibitor of B cell lymphoma 6 (BCL6), with an IC50 of 1 nM.

PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC) and an Mcl-1 inhibitor, useful in cancer research.

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

MDMX/MDM2-IN-2 is a potent dual inhibitor of p53-MDM2/MDMX, demonstrating dissociation constants (Kis) of 0.23 μM for MDM2 and 2.45 μM for MDMX.

Compound 5b (Anti-inflammatory agent 61) is a potent anti-inflammatory agent that diminishes TNF-α expression in LPS-induced inflammation within RAW 264.7 cells

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.

HSP90-IN-18 inhibits Hsp90 with 0.39 μM IC50, useful for viral, neurodegenerative, and inflammatory research.

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.

Ac-Pro-Gly-Pro-OH can be used as a CXCR2 agonist with bactericidal and anti-inflammatory activity for the study of sepsis and lung inflammation.

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.

CDK9-IN-24 (compound 21a) is a potent and selective inhibitor of CDK9 that exhibits a pronounced inhibitory impact on tumor proliferation.

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

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).

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.

Nrf2 activator-9 (compound D-36) is an agent that mitigates oxidative stress by inhibiting the apoptosis of HUVEC cells induced by oxidized low-density

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

Anti-TNBC agent-9 (Compound 3as) is an anticancer agent used for treating triple-negative breast cancer (TNBC). It exhibits significant inhibitory activity against MDA-MB-453 cells, with an IC50 value of 8.5 μM. Anti-TNBC agent-9 impedes tumor cell migration by upregulating E-cadherin and downregulating N-cadherin, matrix metalloproteinase 2 (MMP2), and MMP9. Additionally, it inhibits tumor cell proliferation by inducing apoptosis, achieved through the increased expression of pro-apoptotic protein BAX and decreased expression of anti-apoptotic protein BCL-2.

Maceneolignan A, a natural product isolated from the aril of Myristica fragrans (Myristicaceae), inhibits β-hexosaminidase release in RBL-2H3 cells, exhibiting

8-hydroxy Efavirenz, a main efavirenz metabolite by CYP2B6, causes apoptosis in rat neurons at 0.01 μM.

Reveromycin A from Streptomyces sp. inhibits epidermal growth, tumors, and C. albicans; affects osteoclasts. IC50: 0.7-1.9 μg/ml; MIC: 2 μg/ml.

p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is a interaction inhibitor between p53 and MDM2 proteins.

β-Glucuronide-dPBD-PEG5-NH2 is a β-glucuronide-linked pyrrolobenzodiazepine dimer that functions as a proagent for the synthesis of the antibody-drug conjugate

Secalonic acid D, from Aspergillus aculeatus, is anti-tumor, activates GSK3-β, degrades β-catenin, inhibits c-Myc, and induces apoptosis.

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

LZFPN-90 (LZ90) is a dual-target compound aimed at NAMPT and PD-L1. It inhibits the interaction between PD-1/PD-L1 and NAMPT activity. LZFPN-90 suppresses cell growth in a NAMPT-dependent manner, blocking the cell cycle and subsequently inducing apoptosis. Additionally, LZFPN-90 exhibits target-dependent antitumor activity, impacting metabolic processes and the immune system.

Annonacin is a cytotoxic acetogenin in Graviola leaf extract; it blocks mitochondrial complex and inhibits NKA/SERCA ATPase pumps.

Avotaciclib hydrochloride, a CDK1 inhibitor, is the hydrochloride salt of Avotaciclib and exhibits potential therapeutic use in specific malignancies, including

CV-4-26 (Compound 22) acts as a covalent inhibitor of TEAD. By inhibiting YAP/TEAD-driven transcription, it diminishes the expression of CTGF and CYR61. Furthermore, CV-4-26 impedes colony formation in Huh7 and HepG2 cells, inducing cell cycle arrest and apoptosis (apoptosis). This compound demonstrates anti-tumoral activity against hepatocellular carcinoma (HCC) and hepatoblastoma (HB).

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.

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.

Polyphyllin G (Polyphyllin VII), the the main member of polyphyllin family, shows strong anticancer activity against several carcinomas.

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.

PD-1/PD-L1-IN-39 (X 14) is an orally active PD-1/PD-L1 inhibitor with an IC50 value of 15.73 nM. It exhibits strong binding affinity to human and mouse PD-L1, with KD values of 14.62 and 392 nM, respectively. PD-1/PD-L1-IN-39 also demonstrates antitumor activity.