Caspase 8 Inhibitor

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.

Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.

Z-VAD is an irreversible, broad-spectrum pan-caspase inhibitor that can inhibit a variety of caspases including caspase-3, -6, -7, -8, -9, etc. (with a weaker inhibitory effect on caspase-2). Z-VAD can block apoptosis signaling pathways, induce autophagy and necrosis in tumor cells, and has anti-angiogenic activity. Z-VAD can enhance the sensitivity of breast cancer and lung cancer cells to radiotherapy in vitro and in vivo, and prolong the growth delay of tumor xenograft models. Z-VAD is well tolerated and is mainly used in research related to cancer radiosensitization and cell death pathway regulation.

Ac-DEVD-CHO is a Caspase-3 inhibitor with a K_i value of 230 pM.

Citicoline is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline inhibits reactive oxygen species (ROS) and apoptosis. Citicoline can be used for neurological disease and hearing loss study.

Ofirnoflastum (Ofirnoflast) is an orally active first-in-class allosteric NEK7 inhibitor with an IC₅₀ of 46 nM. Ofirnoflastum binds an allosteric site adjacent to NEK7’s ATP-binding pocket, induces conformational shifts, disrupts NEK7-NLRP3 binding, blocks NLRP3 inflammasome assembly, spares NEK7’s physiological functions, and suppresses caspase-1, caspase-8, NF-κB, and TNF activity. Ofirnoflastum reduces pro-inflammatory cytokine production, suppresses ASC specks, IL-1β release, pyroptotic cell death, and leukemic burden, induces apoptosis and erythroid differentiation, restores hematopoiesis, and improves outcomes in colitis models. Ofirnoflastum can be used for the research of myelodysplastic syndromes, chronic myelomonocytic leukemia, and acute myeloid leukemia.

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.

Xelafaslatide (ONL-1204) is a Fas receptor antagonist. Xelafaslatide blocks the Fas receptor signaling pathway and inhibits downstream apoptosis and inflammatory pathways. Xelafaslatide suppresses neuroinflammation and microglial activation in glaucoma models, protects retinal ganglion cells and prevents axonal degeneration. Xelafaslatide is applicable to relevant research on glaucoma.

δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC₅₀ of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research.

Citicoline sodium is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline sodium inhibits reactive oxygen species (ROS) and apoptosis. Citicoline sodium can be used for neurological disease and hearing loss study.

Tabersonine is a selective, orally active NLRP3 inhibitor. Tabersonine 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 also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine 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 is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

Loliolide (Loliolid) is a β-carotene metabolite. Loliolide reduces caspase 3, 8, 9 expression, enhances PI3K, AKT, SIRT1, inhibits ROS, apoptosis, and blocks NF-κB p65 nuclear translocation. Loliolide protects mitochondria, reduces oxidative stress, and increases cell viability in neuroblastoma cells. Loliolide can be used for the research of UV-induced skin damage and Parkinson’s disease.

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.

Caspase-3-IN-1 (compound 11b) is a potent Caspase-3 inhibitor, with an IC₅₀ of 14.5 nM.

ML132 (NCGC-00183434) is a selective caspase 1 inhibitor with an IC₅₀ value of 0.023 nM. ML132 has good stability and can be used as a caspase 1 molecular probe. ML132 is applicable to research in the fields of anticancer and anti-inflammatory studies.

CASP8-IN-1 (Compound 63-R) is a selective inhibitor for caspase 8 (CASP8), with an IC₅₀ of 0.7 μM. CASP8-IN-1 inhibits FasL-induced apoptosis in cell Jurkat.

Citicoline-d₉ (Cytidine diphosphate-choline-d₉) sodium is the deuterium labeled Citicoline sodium (HY-B0739A). Citicoline sodium is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline sodium inhibits reactive oxygen species (ROS) and apoptosis. Citicoline sodium can be used for neurological disease and hearing loss study.

Citicoline (Cytidine diphosphate-choline) (Standard) is the analytical standard of Citicoline. This product is intended for research and analytical applications. Citicoline is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline inhibits reactive oxygen species (ROS) and apoptosis. Citicoline can be used for neurological disease and hearing loss study.

Citicoline sodium (Standard) is the analytical standard of Citicoline sodium. This product is intended for research and analytical applications. Citicoline sodium is an endogenous intermediate in the synthesis of phosphatidylcholine which is a component of cell membranes. Citicoline sodium inhibits reactive oxygen species (ROS) and apoptosis. Citicoline sodium can be used for neurological disease and hearing loss study.

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