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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
15 Results for "
ceramide accumulation
" in MedChemExpress (MCE) Product Catalog:
Products (15)
15 Results for "ceramide accumulation" in MCE Product Catalog:
8
8 Publications Verification
Target:
SphK Dihydroceramide Desaturase 1 (DES1) Apoptosis Reactive Oxygen Species (ROS) mTOR PERK Keap1-Nrf2
Research Areas:
SKI-II is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. In vivo, SKI-II inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway. SKI-II reduces measles virus replication by inhibiting mTORC1 activity. SKI-II binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome .
6
1
1 Cited Publications
Target:
Research Areas:
Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity .
1
1 Cited Publications
Target:
Research Areas:
HPA-12 is a blood-brain barrier-permeable small-molecule inhibitor of ceramide transfer protein (CERT) with four stereoisomers (the (1R,3R)-stereoisomer exhibits the highest activity). HPA-12 blocks the transport of ceramide from the endoplasmic reticulum to the Golgi apparatus by binding to the START domain of CERT, leading to intracellular ceramide accumulation and inhibition of sphingomyelin (SM) synthesis. HPA-12 induces endoplasmic reticulum stress via the GRP78/ATF6/CHOP axis and activates mitochondrial autophagy, thereby inhibiting cell growth and inducing apoptosis. In in vivo experiments, HPA-12 significantly reduces the leukemia burden and splenomegaly in mouse models of acute myeloid leukemia (AML) and prolongs survival. HPA-12 is applicable for the research of lipid metabolism in acute myeloid leukemia and Alzheimer's disease .
Cat. No.: HY-N6723
CAS No.: 116355-84-1
Category:
Infection Human Gut Microbiota Metabolites Antibiotics Microorganism Disease Research Antibacterial Endogenous metabolite Disease Research Fields Other Antibiotics
Target:
Target:
Research Areas:
Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells .
Synonyms: ES-285
Cat. No.: HY-W012846
CAS No.: 2418-52-2
Category:
Other Diseases Disease markers Endocrine diseases Endogenous metabolite Disease Research Fields Saccharides
Target:
Cat. No.: HY-48917
CAS No.: 15049-93-1
Synonyms: C10 Bisphosphonate
Target:
Research Areas:
ARC39 (C10 Bisphosphonate) is a selective acid sphingomyelinase (acid sphingomyelinase, ASM) inhibitor (IC50 = 20 nM) that binds the catalytic zinc center and blocks sphingomyelin hydrolysis. ARC39 shows higher selectivity for acid sphingomyelinase than for neutral sphingomyelinase and Ser/Thr protein phosphatases, while not affecting acid ceramidase, neutral ceramidase, sphingosine kinase 1, and sphingosine kinase 2. ARC39 reduces pulmonary edema, platelet- and ASM-promoted melanoma adhesion, and necroptosis-associated ceramide accumulation, and restores necroptotic viability. ARC39 can be used in research on platelet-activating factor (PAF)-induced pulmonary edema, melanoma, major depressive disorder, and colorectal cancer .
Cat. No.: HY-176568
Research Areas:
LCL768 is a ceramide analog. LCL768 attenuates PARKIN succination to promote PARKIN activation and mitophagy. LCL768 induces CerS1-mediated endogenous C18-ceramide accumulation in mitochondria to mediate mitophagy, which is dependent on DRP1 activation via nitrosylation at C644. LCL768 alters mitochondrial metabolism, resulting in fumarate depletion and leading to tumor suppression. LCL768 improves sensorimotor defects in neurodegenerative diseases like ALS .
Cat. No.: HY-124273
CAS No.: 143615-69-4
Synonyms: L-threo Cer(d18:1/2:0); L-threo ceramide (d18:1/2:0); N-acetyl-L-threo-Sphingosine
Target:
Research Areas:
C2 L-threo Ceramide (d18:1/2:0) (L-threo Cer(d18:1/2:0); L-threo Ceramide (d18:1/2:0)) is a bioactive sphingolipid and cell-permeable analog of naturally occurring ceramides. It stimulates cholesterol efflux in CHO cells expressing the human ABCA1 receptor when used at a concentration of 10 μM, however, this efflux is 50% less than that stimulated by C2 ceramide. C2 L-threo Ceramide inhibits IL-4 production by 17% in EL4 T cells stimulated with phorbol 12-myristate 13-acetate when used at a concentration of 10 μM. It also induces cell cycle arrest in the G0/G1 phase and a 7-fold increase in sphingosine accumulation as well as inhibits growth of HL-60 leukemia cells.
Cat. No.: HY-124134
CAS No.: 366487-89-0
Synonyms: LCL102
Target:
Research Areas:
AD-2646 (LCL102), a ceramide analog, can kill leukemic T cells (EC50: 40 μM). AD-2646 triggers the cleavage of caspase-8, -9 and -3, as well as the caspase substrate PARP. AD-2646 is a ceramidase inhibitor. AD-2646 induces an accumulation of endogenous ceramide owing to perturbed ceramide metabolism .
Synonyms: ES-285-d3
Cat. No.: HY-W012846R
CAS No.: 2418-52-2
Cat. No.: HY-112364
CAS No.: 1177741-83-1
Target:
SphK Dihydroceramide Desaturase 1 (DES1) Apoptosis Reactive Oxygen Species (ROS) mTOR PERK Keap1-Nrf2
Research Areas:
SKI-II hydrochloride is an orally active dual-target inhibitor of SphK1/2 and DES1, with Ki values of 16 µM and 0.3 µM against SphK1 and DES1, respectively. SKI-II hydrochloride activates the PERK-Nrf2 antioxidant pathway by stabilizing Nrf2, and synergizes with Temozolomide (HY-17364) to induce oxidative/endoplasmic reticulum stress and cancer cell death under hypoxic conditions. SKI-II hydrochloride inhibits SphK activity, promotes ceramide accumulation and apoptosis, and synergizes with Cisplatin (HY-17394) to reverse drug resistance via the ras/MAPK pathway in vivo. SKI-II hydrochloride reduces measles virus replication by inhibiting mTORC1 activity. SKI-II hydrochloride binds to VCP to induce M1 polarization, enhances host tolerance to Staphylococcus aureus infection, and exerts radioprotective effects through Nrf2 activation and accelerated DNA repair. SKI-II hydrochloride can be used in research related to glioblastoma, acute myeloid leukemia, gastric cancer, measles virus infection, Staphylococcus aureus infection, and acute radiation syndrome .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
