Caspase Inhibitor

Antiproliferative agent-42 (compound 7m) is a dihydrodipyrrolo compound. Antiproliferative agent-42 showed antiproliferative activity against Panc-1 cell line with an IC₅₀ value of 12.54 μM.

Ac-VEID-CHO is a peptide-derived caspase inhibitor and has potency of inhibition for Caspase-6, Caspase-3 and Caspase-7 with IC₅₀ values of 16.2 nM, 13.6 nM and 162.1 nM, respectively. Ac-VEID-CHO also inhibits VEIDase activity an IC₅₀ value of 0.49 µM. Ac-VEID-CHO can be used for the research of neurodegenerative conditions including Alzheimer’s and Huntington’s disease.

Moroxydine (ABOB) hydrochloride (Standard) is the analytical standard of Moroxydine (ABOB) hydrochloride (HY-B0420A). Moroxydine (ABOB) hydrochloride 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 hydrochloride 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 hydrochloride blocks the GCRV-induced cytopathic effects and eliminates nucleocapsids in ctenopharyngodon idella kidney (CIK) cells to keep the normal morphological structure. Moroxydine hydrochloride significantly inhibits the apoptosis, the caspase 3 activity, Bax expression and down-regulates Bcl-2 levels.

Necrosulfonamide (Standard) is the analytical standard of Necrosulfonamide (HY-100573). This product is intended for research and analytical applications. Necrosulfonamide is a MLKL and Gasdermin D (GSDMD) inhibitor, capable of separately inhibiting necroptosis and pyroptosis of cells. Necrosulfonamide does not affect the activation of upstream signals, but specifically inhibits the downstream executor oligomerization step. Necrosulfonamide reduces the expression of the key kinases NLRP3 and caspase-1 involved in necroptosis and pyroptosis, activate the Nrf2 pathway and the downstream antioxidant enzymes, and also downregulates a variety of inflammatory factors. Necrosulfonamide plays significant roles in various diseases such as neurodegenerative diseases (such as Parkinson’s disease), tissue damage and ischemia-reperfusion injury, inflammatory bowel disease, osteoarthritis and fracture repair, and hair loss by regulating two important programmed necrosis pathways.

Boc-Asp(OMe)-fluoromethyl ketone (Standard) is the analytical standard of Boc-Asp(OMe)-fluoromethyl ketone (HY-103348). This product is intended for research and analytical applications. Boc-Asp(OME)-Fluoromethyl Ketone is a broad range caspase inhibitor that inhibits Fas-mediated phagocytosis and oxidative rupture inhibition, but does not affect the chemotactic activity of IL-8.

LPT-99 is an antagonist of apoptotic protease activating factor 1 (APAF-1). LPT-99 suppresses the activation of procaspase-9. LPT99 suppresses Cisplatin (HY-17394)-induced apoptosis. LPT99 can effectively mitigate cisplatin-induced hearing loss in rats.

PQ-1 succinate is an inhibitor for gap junction, which suppresses the gap junction dye transfer activity in retinal neurosensory R28 cells, and inhibits the CoCl₂-induced ischemic apoptosis in retinal cell.

Z-VA-DL-D-FMK (Z-VA-DL-D(OH)-FMK) is an inhibitor for caspase. Z-VA-DL-D-FMK binds irreversibly to caspases, increases the sensitivity of TNF-α, and activates HIV replication in infected T cell ACH-2.

Epimedin A (Standard) is the analytical standard of Epimedin A (HY-N0257). This product is intended for research and analytical applications. Epimedin A, one of the main flavonoid active components in Herba Epimedii, is orally active. Epimedin A can inhibit osteoclastogenesis, differentiation, and bone resorption. Epimedin A also possesses anti-inflammatory activity. Epimedin A can be used in the research of osteoporosis and inflammatory diseases.

Pinusolide is an AMPK activator and PAF receptor antagonist. Pinusolide activates AMPK, phosphorylates ACC, enhances IRS-1 tyrosine phosphorylation, boosts glucose uptake, and modulates insulin signaling. Pinusolide inhibits caspase-3/7 activation, intracellular calcium elevation, reactive oxygen species overproduction, lipid peroxidation, and tumor cell proliferation. Pinusolide stabilizes superoxide dismutase activity, reduces apoptotic hallmarks, induces mitochondrial pathway apoptosis, and triggers DNA fragmentation. Pinusolide can be used for the research of type 2 diabetes, neurodegenerative diseases, acute lymphoblastic leukemia, acute myeloid leukemia, and Burkitt lymphoma.

Agnuside (Standard) is the analytical standard of Agnuside. This product is intended for research and analytical applications. Agnuside is used in the study of asthma, inflammation, and angiogenic diseases. Agnuside is an orally active compound that can be extracted from Vitex negundo.

Fenbufen (Standard) is the analytical standard of Fenbufen. This product is intended for research and analytical applications. Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC₅₀s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.

Hibiscetin is an orally active anti-inflammatory, antioxidant, antihyperglycemic, hypolipidemic, hepatoprotective and neuroprotective agent. Hibiscetin reduces the levels of TNF-α, IL-1β and IL-6. Hibiscetin inhibits lipid peroxidation, reduces MDA levels, and induces the activities of antioxidant enzymes CAT, GSH and SOD. Hibiscetin lowers blood glucose, reverses reduced insulin levels, regulates adipokine levels, and reduces elevated AST and ALT levels. Hibiscetin alleviates Rotenone (HY-B1756)-induced akinesia and catalepsy, normalizes neurotransmitter levels, and modulates the activities of activated caspase 3 and BDNF. Hibiscetin can be used in the research of type 2 diabetes, Parkinson's disease and Huntington's disease.

Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

Licoflavanone (3′-Prenylnaringenin) is a flavanone with antioxidant, anti-inflammatory and anticancer activities. Licoflavanone can be isolated from the leaf extract of Glycyrrhiza glabra. Licoflavanone downregulates the mTOR/PI3K/AKT signaling pathway to inhibit the proliferation, migration and invasion of cancer cells, while activates Bax, Bad and multiple caspase enzymes to induce apoptosis. Its anti-inflammatory effect is manifested by reducing the nuclear translocation of NF-κB, decreasing the phosphorylation levels of p38, JNK and ERK1/2, thereby inhibiting the expression of nitric oxide, proinflammatory cytokines, COX-2 and iNOS. Licoflavanone is used in studies on nasopharyngeal carcinoma and related mechanisms.

N-(p-Coumaroyl) Serotonin (Standard) is the analytical standard of N-(p-Coumaroyl) Serotonin (HY-129440). This product is intended for research and analytical applications. N-(p-Coumaroyl) Serotonin is an orally active polyphenol found in safflower seeds with potent anti-inflammatory, antioxidant, and antitumor activities. N-(p-Coumaroyl) Serotonin suppresses NF‑κB, TLR4/MyD88 and MAPK signaling, activates NQO1/HO‑1 pathways, and inhibits pro‑inflammatory cytokines, iNOS and COX‑2 and ROS production. N-(p-Coumaroyl) Serotonin induces S‑phase arrest and apoptosis in glioblastoma cells, reduces atherosclerotic lesions, and alleviates renal and vascular injuries. N-(p-Coumaroyl) Serotonin acts as a vasodilator, regulates calcium dynamics. N-(p-Coumaroyl) Serotonin can be used for the research of neurodegenerative diseases, atherosclerosis, glioblastoma, and acute renal failure.

(-)-Isoproterenol (Levisoprenalinel) is the R-isomer of Isoproterenol. (-)-Isoproterenol can reduce the cleavage of caspase 3 and TNFα levels in retinal endothelial cells (REC). (-)-Isoproterenol can be used for the study of diabetic retinopathy.

Tauroursodeoxycholate (dihydrate) (Standard) is the analytical standard of Tauroursodeoxycholate (dihydrate). This product is intended for research and analytical applications. Tauroursodeoxycholate (Tauroursodeoxycholic acid; TDUCA) dihydrate is an endoplasmic reticulum (ER) stress inhibitor. Tauroursodeoxycholate significantly reduces expression of apoptosis molecules, such as caspase-3 and caspase-12. Tauroursodeoxycholate also inhibits ERK.

Orsellinic acid (Standard) is an analytical standard of Orsellinic acid (HY-N3126). This product is intended for research and analytical applications. Orsellinic acid is a Benzoic acid (HY-N0216) derivative. Orsellinic acid can be isolated from Chaetomium globosum endophytic on Ephedra fasciculata (Mormon tea). Orsellinic acid blocks PAF-mediated Apoptosis, inhibits caspase-3/7 activation, and PARP cleavage. Orsellinic acid can be used in research of neurons and various tumors (non-small cell lung cancer, breast cancer, neuroblastoma, pancreatic cancer).

β-carotene-15,15ʹ-epoxide is a XIAP antagonist with apoptosis-inducing and antitumor activity, found in the leaves of Spondias mombin. In a DMBA (HY-W011845)-induced rat model of breast cancer, β-carotene-15,15ʹ-epoxide binds to the BIR3 domain of the anti-apoptotic protein XIAP, blocking its interaction with caspase-9 and thereby promoting tumor cell apoptosis. In addition, β-carotene-15,15ʹ-epoxide significantly downregulates the expression of BCL-2, COX-2, and TNF-α in tumor tissues, reduces MDA levels, increases catalase activity, and modulates serum levels of LDH, ALP, and ALT, demonstrating strong antioxidant, anti-inflammatory, and metabolic protective effects. β-carotene-15,15ʹ-epoxide may be used in research on inflammation-related conditions and cancers such as breast cancer.