Caspase Inhibitor

Z-YVAD-CMK is a caspase-1 and caspase-3 inhibitor.

Cytochalasin H is a nature product that could be isolated from fungus Phomopsis sp. Cytochalasin H inhibits cell growth and induces apoptosis. Cytochalasin H has anti-angiogenic activity. Cytochalasin H is an antibiotic and has antibacterial activity.

Berkeleyamide B is a dual matrix metalloproteinase-3 (MMP-3) and caspase-1 inhibitor. Berkeleyamide B is promising for research of cancers and inflammatory disease (e.g., rheumatoid arthritis).

Caspase-3-IN-3 (compound 7) is a caspase 3 inhibitor. Caspase-3-IN-3 increases cellular ATP levels, inhibits caspase-3 activity, decreases nitrite production, suppresses cytokine-induced apoptosis, and restores Glucose (HY-B0389)-stimulated insulin secretion.

Fluorescein-6-carbonyl-Asp(OMe)-Glu(OMe)-Val-DL-Asp(OMe)-fluoromethylketone is a cell-permeable, non-toxic inhibitor that binds irreversibly to activated caspase-3 in apoptotic cells. The fluorescence intensity can be measured by flow cytometry, microwell plate reader, or fluorescence microscopy.

MAPK-IN-6 is a blood-brain barrier-permeable MAPK inhibitor. MAPK-IN-6 inhibits oxidative stress-induced activation of the MAPK signaling cascade, including the phosphorylation of ERK1/2, p38 and JNK. MAPK-IN-6 eliminates intracellular reactive oxygen species (ROS) accumulation, stabilizes mitochondrial membrane potential and inhibits cell apoptosis. MAPK-IN-6 can be used for the research of ischemic stroke.

VX-166, a pan caspase inhibitor, can be used for the research of Non- Alcoholic Fatty Liver Disease (NAFLD), nonalcoholic steatohepatitis (NASH), alcoholic steatohepatitis (ASH), and other diseases involving fibrosis, steatosis, or inflammation of the liver.

Topoisomerase I-IN-23 is a topoisomerase I inhibitor with anticancer activity. Topoisomerase I-IN-23 competitively binds to the hydrophobic pocket at the Topo I-DNA interface, stabilizes the covalent DNA-Topo I complex, downregulates Topo I protein expression in a concentration-dependent manner, induces S-phase cell cycle arrest in tumor cells, regulates the expression of apoptosis-related proteins Bax, Bcl-2 and cleaved caspase-3 to trigger apoptosis, and inhibits the migration and invasion of tumor cells. Topoisomerase I-IN-23 exhibits in vivo antitumor efficacy in xenograft models. Topoisomerase I-IN-23 can be used in research related to colorectal cancer, lung cancer and hepatocellular carcinoma.

IETD-CHO TFA (Caspase-8-IN-1) is a potent caspase-8 inhibitor.

MAPK-IN-5 is a potent MAPK inhibitor with an IC₅₀ of 1.35 μM against HeLa cells. MAPK-IN-5 inhibits HeLa cell proliferation by inducing ROS-mediated DNA damage and mitochondrial apoptosis via the MAPK pathway. MAPK-IN-5 significantly inhibits colony formation, reduces the number of live cells, suppresses cell migration, and causes cell cycle arrest in the G2/M phase in HeLa cells. MAPK-IN-5 can be used for the study of cervical cancer.

PI3K/Akt/mTOR-IN-7 is an AKT/mTOR and JAK2/STAT3 inhibitor. PI3K/Akt/mTOR-IN-7 restores p-Akt, p-mTOR, and p-STAT3 expression, reduces pro-apoptotic Caspase-3 mRNA expression. PI3K/Akt/mTOR-IN-7 reduces intracellular ROS accumulation and inhibits NO production. PI3K/Akt/mTOR-IN-7 can be used for research on stroke, Alzheimer's disease and Parkinson's disease.

Bax activator-2 is a pro-apoptotic agent targeting BAX, with an IC₅₀ of 0.30 μM against human BAX. Bax activator-2 binds to the trigger site of BAX and induces its conformational change. Bax activator-2 induces mitochondrial depolarization, cytochrome c release, cleavage of caspase-3/9 and PARP, thereby initiating apoptosis. Bax activator-2 exhibits cytotoxicity against a variety of cancer cell lines. Bax activator-2 can be used in research related to acute myeloid leukemia and solid tumors.

Q-VD-OPh (GMP) is Q-VD-OPh (HY-12305) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC₅₀ of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.

Xiap-casp7 PPI-IN-1 is a reversible XIAP: CASP7 inhibitor with specifically disrupting the interaction between XIAP and CASP7. XIAP-CASP7 PPI-IN-1 selectively induce MCF-7 and other caspase-3 down-regulation (CASP3/DR) triple-negative breast cancer cell apoptosis. XIAP-CASP7 PPI-IN-1 overcomes chemoresistance via down-regulating β-catenin and its associated ABC transporters in Paclitaxel (HY-B0015)-resistant MCF-7 cells. XIAP-CASP7 PPI-IN-1 can be used for the study of breast cancer.

ZM484 is a potent dual p53-MDM2/TOP1 inhibitor that exhibits antiproliferative and antitumor activity both in vitro and in vivo. ZM484 effectively upregulates p53 and MDM2 proteins and maintains TOP1 inhibitory activity by the release of camptothecin (CPT) and a potent p53-MDM2 inhibitor. ZM484 induces cell cycle arrest and apoptosis by regulating the expression of key apoptosis- and cycle-related proteins, including caspase-3, Bcl-2, and Cyclin B1. ZM484 can be used for colorectal cancer research.

Moroxydine (ABOB) is a broad-spectrum agent with multi-antiviral activities against DNA and RNA viruses, including influenza virus, herpes simplex, varicella zoster, measles, mumps disease, hepatitis C virus, etc. Moroxydine exhibits excellent antiviral activity and shows low cytotoxicity to cells infected by dsRNA viruses (grass carp reovirus, GCRV) and large DNA viruses (giant salamander iridovirus, GSIV). Moroxydine blocks the GCRV-induced cytopathic effects and eliminates nucleocapsids in ctenopharyngodon idella kidney (CIK) cells to keep the normal morphological structure. Moroxydine significantly inhibits the apoptosis, the caspase 3 activity, Bax expression and down-regulates Bcl-2 levels^[1][2][3].

ZX079 is a dual BRD4 and CBP PROTAC degrader with a BRD4 DC₅₀ value of 0.035 nM and a CBP DC₅₀ value of < 0.02 nM. ZX079 induces dose- and time-dependent degradation of BRD4 and CBP proteins through recruitment of the cereblon E3 ligase. ZX079 induces apoptosis in MV4-11 and MOLM-13 cells, reduces tumor growth in an acute myeloid leukemia xenograft model. ZX079 can be used for the research of acute myeloid leukemia.

CAY10406 is an inhibitor for caspase 3/7. CAY10406 inhibits the expression of 28-kDa IL-1β fragment, without significant cytotoxicity (10 μM).

20-5,14-HEDE-d₂-1 (WIT003-d₂-1) is the deuterated-labeled 20-5,14-HEDE (HY-160099). 20-5,14-HEDE (WIT003) is an analog of 20-HETE. 20-5,14-HEDE activates PI3K/Akt signaling pathway, thereby exhibiting anti-apoptotic and cell survival promoting effects. 20-5,14-HEDE is the agonist for 20-HETE that increases intracellular Ca²⁺ concentrations, thereby enhancing vasoconstriction.

Casp4 Rat Pre-designed siRNA Set A contains three designed siRNAs for Casp4 gene (Rat), as well as a negative control, a positive control, and a FAM-labeled negative control.