Caspase 3 Activator

Swerchirin is an orally active, plant-derived xanthone that acts as an inhibitor of the Raf/MEK/ERK signaling pathway. Swerchirin downregulates the expression of phosphorylated MEK and phosphorylated ERK, induces mitochondrial apoptosis and cell cycle arrest, regulates Bcl-2 family proteins, triggers cytochrome c release, activates caspases, and drives PARP cleavage. Swerchirin reduces blood glucose levels in rat models under fasting, fed, glucose-loaded conditions, and following treatment with Tolbutamide (HY-B0401). Swerchirin can be used in research related to ovarian cancer, liver injury, and diabetes.

GUT-70, a tricyclic coumarin, is a Hsp90 inhibitor. GUT-70 activates the caspase 2, 3, 8 and 9, and induces the apoptosis in leukemic cells. GUT-70 inhibits HIV-1 replication in chronically infected cells via suppression of the NF-κB pathway. GUT-70 can be used for the study of leukemic, mantle cell lymphoma (MCL) and HIV-1 infection.

GEA 3162 hydrochloride is an orally active compound that acts as a NO/ONOO⁻ donor. GEA 3162 hydrochloride significantly inhibits the activation of human polymorphonuclear leukocytes (PMNs) through the cGMP pathway, inhibits the release of inflammatory mediators, and exerts anti-inflammatory and protective effects. GEA 3162 hydrochloride induces apoptosis of neutrophils and bone marrow cells by activating caspase-2/3/8/9 through the ONOO⁻ pathway. GEA 3162 hydrochloride has a bidirectional effect in the rat gastric ulcer model: at low doses, it significantly reduces gastric mucosal damage, while at high doses, it aggravates the ulcer area. GEA 3162 hydrochloride can be used for research on inflammatory conditions such as gastric ulcers.

CDK9/EZH2-IN-2 is a potent dual CDK9 and EZH2 inhibitor with an IC₅₀ of 8.9 nM against EZH2. CDK9/EZH2-IN-2 inhibits anti-apoptotic proteins and induces DNA damage by blocking the activity of CDK9 and EZH2, ultimately leading to tumor cell apoptosis. CDK9/EZH2-IN-2 can be used for research on diffuse large B-cell lymphoma.

Antioxidant agent-22 is a paraben derivative tetracyclic spermine cyclotriphosphazene compound. Antioxidant agent-22 exhibits antioxidant, anti-Inflammatory, and apoptotic activities. Antioxidant agent-22 significantly upregulates CAT, SOD, caspase-3 and IL-6 expression, suppresses GSH, IL-1β, and reduces BCL-2 and BAX levels. Antioxidant agent-22 can be used for the research of cancer, such as lung cancer.

ERK5-IN-7 is an orally active ERK5 inhibitor with an IC₅₀ of 403.4 nM. ERK5-IN-7 directly inhibits ERK5 kinase activity, and downregulates the phosphorylation level and total protein expression of ERK5. ERK5-IN-7 induces Apoptosis (upregulates Bax, downregulates Bcl-2, and induces Caspase-3 cleavage). ERK5-IN-7 induces ROS accumulation. ERK5-IN-7 exhibits anticancer effects against Lewis lung cancer.

FGFR-IN-25 (Compound 19E) is a FGFR inhibitor (IC₅₀s: 1.30 nM and 0.85 nM for FGFR1 and FGFR2, respectively) and radiosensitizer. FGFR-IN-25 effectively reduces the phosphorylation of FGFR1 and its key downstream effectors, pAKT and pERK. FGFR-IN-25 exerts broad-spectrum antitumor activity against gastric cancer, colorectal carcinoma, hepatocellular carcinoma, breast cancer, triple-negative breast cancer, and glioblastoma. FGFR-IN-25, when combined with radiotherapy, synergistically activates the ROS-Caspase-3-GSDME axis, downregulates PD-L1 expression, and induces immunogenic cell death (ICD). FGFR-IN-25 combined with radiotherapy improves the antitumor efficacy.

RR-171 is an amino acid polypeptide and an inhibitor of the Wnt signaling pathway. RR-171 reduces the expression levels of Wnt-1, GSK3β and β-catenin. RR-171 induces apoptosis (Apoptosis) in pancreatic cancer cells, which is characterized by an increased Bax/Bcl-2 ratio, activation of Caspase-3/7/9, and increased Cleaved-PARP; this pro-apoptotic effect can be partially reversed by Z-VAD-FMK (HY-16658B). RR-171 also induces pyroptosis (Pyroptosis) in pancreatic cancer cells, which is manifested by activation of the NLRP-3 inflammasome, activation of Caspase-1, cleavage of GSDMD, upregulation of IL-1β and IL-18, and increased LDH release; this pro-pyroptotic effect can be partially reversed by VX-765 (HY-13205). RR-171 inhibits the viability, proliferation and colony formation of pancreatic cancer cells, with low cytotoxicity against normal cells. RR-171 downregulates the expression of Ki-67 and PCNA in tumor tissues in vivo, with favorable biosafety. RR-171 can be used in studies related to pancreatic cancer.

Caspase-3/7 activator 3 is an effective activator of Caspase-3/7. Caspase-3/7 activator 3 has tumor selectivity, anti-proliferative activity and high Apoptosis-inducing ability.

PbQ is a tubulin inhibitor (with an IC₅₀ of 5 μM against goat tubulin) and a fluorescent probe for cuprous ions Cu (I). PbQ can penetrate the membrane of peripheral blood mononuclear cells, form a stable 1:1 complex with Cu⁺ ions, and exhibits low toxicity and good biocompatibility toward macrophage cell lines. In addition, PbQ promotes tubulin degradation and disrupts the microtubule network in lung epithelial cells without affecting actin. PbQ also possesses genotoxicity by forming DNA base adducts, and it can activate caspase-3 and apoptosis-related genes, induce loss of mitochondrial membrane potential, and trigger cell apoptosis. PbQ can be used in studies related to chronic obstructive pulmonary disease.

Jolkinolide B (Standard) is the analytical standard of Jolkinolide B (HY-N0732). This product is intended for research and analytical applications. Jolkinolide B is a bioactive diterpene isolated from the roots of Euphorbia fischeriana Steud with oral activity. Jolkinolide B downregulates XIAP, cIAP1, cIAP2, and phosphorylated Akt, upregulates Smac, activates caspase-3 and caspase-9, and inhibits NF-κB, TGFβ/smad3 and JAK/STAT3 pathways. Jolkinolide B exerts comprehensive biological effects including inducing cancer cell apoptosis, suppressing inflammatory responses, improving lung function, alleviating hepatic steatosis and eliminating intracellular Mycobacterium tuberculosis. Jolkinolide B can be used for the research of leukemia, histiocytic lymphoma, asthma, metabolic dysfunction-associated steatotic liver disease and tuberculosis.

MRTX849-amide-C4-(o)-carborane is a KRAS^G12C inhibitor with mutation selectivity for cells expressing KRAS^G12C. MRTX849-amide-C4-(o)-carborane shows low intrinsic cytotoxicity in cancer cells. MRTX849-amide-C4-(o)-carborane covalently binds to Cys12 of KRAS^G12C, recruits Hsp70, promotes ubiquitination, and induces proteasome-dependent degradation of the target protein. MRTX849-amide-C4-(o)-carborane inhibits the activity of the downstream ERK signaling pathway and induces apoptosis signaling in cancer cells. MRTX849-amide-C4-(o)-carborane is applicable for the research of KRAS^G12C-positive cancers.

Ganoderic acid Mk (GA-Mk) is a triterpenoid acid, that can be isolated from the mycelia of Ganoderma lucidum. Ganoderic acid Mk is efficiently anti-proliferative and can induce apoptosis of HeLa cells by mitochondria-mediated pathway. Ganoderic acid Mk can be used for cervical cancer research.

FLC-8 is an orally active FLT3 inhibitor with IC₅₀ values of 10.2 nM, 11.6 nM and 24.10 nM against human FLT3-WT, FLT3-G697R and FLT3-N676D, respectively. FLC-8 inhibits FLT3 autophosphorylation and downstream STAT5, AKT and ERK signaling pathways, and induces apoptosis in acute myeloid leukemia (AML) cells. FLC-8 exhibits potent antitumor activity in the MV4-11 xenograft model. FLC-8 can be used for the research of acute myeloid leukemia.

MN33-47 is a multi-target anti-tumor compound with broad-spectrum anti-proliferative activity. MN33-47 relieves the inhibition of the mitochondrial apoptosis pathway by downregulating the anti-apoptotic protein Bcl-2, while activating caspase-3 and inhibiting Topoisomerase I activity, thereby promoting its degradation through the ubiquitin-proteasome and autophagy-lysosome pathways. MN33-47 can also induce DNA cross-linking and G2/M cell cycle arrest, inhibit cancer cell migration and activate the mitochondrial apoptosis pathway, thus exerting potent anti-tumor effects. MN33-47 can improve the water solubility of SN-38 (HY-13704), and exhibits dose-dependent tumor growth inhibition effects in CT26 tumor-bearing mouse models without obvious toxic and side effects. MN33-47 can be used in related studies on colorectal adenocarcinoma, cervical adenocarcinoma, hepatocellular carcinoma, alveolar basal epithelial adenocarcinoma, gastric cancer and colon cancer.

PARP1-IN-58 is a ROS-responsive prodrug constructed based on a natural stilbene scaffold, and its active parent nucleus 24c acts as a selective PARP-1 inhibitor. PARP1-IN-58 only hydrolyzes to release the active parent compound in the high-ROS microenvironment of tumors; the active parent compound competitively binds to PARP-1 and blocks DNA single-strand damage repair, upregulates intracellular ROS levels, reduces mitochondrial membrane potential, and thereby induces cell cycle arrest and mitochondria-dependent apoptosis. PARP1-IN-58 exerts potent proliferation-inhibiting effects on BRCA-deficient breast cancer cells under simulated tumor oxidative stress conditions, and exhibits tumor growth inhibitory activity in breast cancer xenograft models. PARP1-IN-58 can be used in cancer-related research.

Neosolaniol is an orally active type A trichothecene mycotoxin, and it is a metabolite of T-2 Toxin (HY-N6792) in human cancer cells and renal epithelial cells. Neosolaniol targets Bax, Bcl-2, caspase 3, caspase 8, and cytochrome c, thereby inducing apoptosis, emesis and anorexia. Neosolaniol reduces intracellular ATP levels, elevates ROS levels, decreases mitochondrial membrane potential, induces mitochondrial damage, and exerts toxicity on Leydig cells. Neosolaniol downregulates the expression of intestinal tight junction proteins in broilers and increases the load of Salmonella enteritidis in the cecum of broilers. Neosolaniol can be used in research related to anorexia, lymphoma, Fusarium melonis rot, and Salmonella infection.

Clausenidin is a selective inhibitor targeting apoptosis-related pathways, including the mitochondrial pathway and death receptor pathway, and vascular endothelial growth factor (VEGF). Clausenidin induces mitochondrial membrane depolarization by activating caspase-3, caspase-8 and caspase-9, upregulating the pro-apoptotic protein Bax and downregulating the anti-apoptotic protein Bcl-2. Clausenidin also inhibits VEGF expression and blocks angiogenesis, exerting anti-tumor activity. Clausenidin has inhibitory effects against Mycobacterium tuberculosis (MIC=200 μg/mL). Clausenidin can induce apoptosis in liver cancer cells, arrest the cell cycle in the G2/M phase, and inhibit tumor angiogenesis. Clausenidin can be used in the research of malignant tumors such as liver cancer.

2-Hexadecanol is a fatty acid based compound. 2-Hexadecanol can be isolated from marine organism Sea pen. 2-Hexadecanol induces Apoptosis, elevates the expression of caspase-3 and caspase-8. 2-Hexadecanol exhibits anticancer activity against breast cancer and cervical cancer.

Bfl-1-IN-7 is an orally active and selective Bfl-1 inhibitor with an IC₅₀ value of 0.015 μM. Bfl-1-IN-7 activates caspase 3/7, and when combined with the Mcl-1 inhibitor AZD5991 (HY-101533), it reduces the viability of lymphoma cells. Bfl-1-IN-7 can be used in lymphoma-related studies.