52 Results for "

PKC signaling

" in MedChemExpress (MCE) Product Catalog:
Products (52)

52 Results for "PKC signaling" in MCE Product Catalog:

23
23 Publications Verification
Cat. No.: HY-18980
CAS No.: 82-08-6
Synonyms: Mallotoxin; NSC 56346; NSC 94525
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation . Rottlerin inhibits HIV-1 integration and Rabies virus (RABV) infection .
loading...
    loading...
4
4 Cited Publications
Cat. No.: HY-B1029
CAS No.: 17230-88-5
Target:  

PKC Apoptosis Tyrosinase

Research Areas:  

Endocrinology Cancer

Danazol inhibits the proliferation of cancer cell MDA-MB-231 and MCF-7 with IC50 of 65 µg/mL and 31 µg/mL. Danazol arrests the cell cycle at G1 phase, induces apoptosis in MDA-MB-231 through PKCα signaling pathway .
loading...
    loading...
4
4 Cited Publications
Cat. No.: HY-N0699
CAS No.: 2034-69-7
Synonyms: Dephnoretin; Thymelol
Daphnoretin (Dephnoretin; Thymelol) is a protein kinase C (PKC) activator that inhibits the expression of hepatitis B virus (HBV) surface antigen (HBsAg) and exhibits antiviral activity. Daphnoretin exerts its antitumor effects by inhibiting the activation of the PI3K/AKT signaling pathway and triggers the mitochondrial apoptosis pathway. Daphnoretin alleviates chondrocyte apoptosis and inflammatory responses by inhibiting endoplasmic reticulum stress and activation of the NLRP3 inflammasome. Daphnoretin regulates the differentiation and maturation of dendritic cells, inhibits their immunostimulatory function by downregulating the phosphorylation level of JNK, and thus exerts a protective effect in skin graft rejection .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-18719
CAS No.: 112093-28-4
Endoxifen Z-isomer is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. Endoxifen Z-isomer also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. Endoxifen Z-isomer can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-N5072
CAS No.: 17817-31-1
Synonyms: 4',6,7-Trihydroxyisoflavone
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity . Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1) . Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes .
loading...
    loading...
3
3 Cited Publications
Cat. No.: HY-18719A
CAS No.: 1032008-74-4
Endoxifen Z-isomer hydrochloride is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer hydrochloride binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer hydrochloride inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-N0735
CAS No.: 104112-82-5
Phellodendrine chloride is an orally active plant alkaloid. Phellodendrine chloride inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine chloride promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine chloride can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine chloride suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine chloride inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine chloride has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-N5063
CAS No.: 147331-98-4
Plantainoside D, a phenylethanoid glycosides, is a IKK-β inhibitor with diverse biological activities. Plantainoside D shows inhibitory activity of angiotensin-converting enzyme (ACE) with an IC50 of 2.17 mM. Plantainoside D significantly reduces the release of glutamate from nerve terminals in the cerebral cortex of rats by inhibiting the voltage-dependent calcium channel (VDCCs) and protein kinase C (PKC) signaling cascade. Plantainoside D significantly alleviates cell apoptosis by inhibiting the generation of ROS and the activation of NF-κB. Plantainoside D significantly improves acute lung injury (ALI) induced by sepsis by regulating the Sirt3/NLRP3 signaling pathway. Plantainoside D can be used for the study of neuroprotection, antioxidant, anti-inflammation, antihypertension .
loading...
    loading...
2
2 Cited Publications
Cat. No.: HY-105416
CAS No.: 121263-19-2
Purity:  99.00%
Synonyms: UCN-1028C
Target:  

Antibiotic PKC Apoptosis

Research Areas:  

Metabolic Disease Cancer

Calphostin C is a highly selective PKC inhibitor (IC50=0.05 μM) and tumor apoptosis inducer. Calphostin C competitively binds to PKC and inhibits PKC-mediated phosphorylation signal transduction. Calphostin C restores Na+/K+ ATPase activity in the sciatic nerve of diabetic mice and improves neuropathy. Calphostin C can be used in the study of anti-tumor and diabetic complications .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-N4322
CAS No.: 130848-06-5
Decursinol angelate acts as a PKC activator and GDH inhibitor, with an IC50 of 1.432 μM against human GDH. Decursinol angelate activates PKC, downregulates PKCα and PKCβII isoforms, and exerts cytotoxic activity against cancer cells. Decursinol angelate binds to GDH and inhibits its enzymatic activity. Decursinol angelate inhibits VEGF-induced autophosphorylation of VEGFR2, downstream p42/44 ERK and JNK-MAPK signaling pathways, as well as the angiogenesis process. Decursinol angelate is applicable to research related to cancer and leukemia .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-14604
CAS No.: 90494-79-4
Purity:  98.57%
Synonyms: SR57746A; SR57746 hydrochloride
Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
loading...
    loading...
1
1 Cited Publications
Cat. No.: HY-117393
CAS No.: 137592-43-9
Purity:  98.95%
Research Areas:  

Cancer

Bisindolylmaleimide III is a protein kinase C (PKC) inhibitor with IC50 values of 0.26, 5.7, and 6 μM against PKCα, PKCδ, and PKCμ, respectively. Bisindolylmaleimide III also exhibits inhibitory activity against other off-targets, with IC50 values of 0.17, 1, and 2 μM against SLK, adenosine kinase (AK), and CDK2, respectively; its Ki for NQO2 is 16.5 μM. Bisindolylmaleimide III selectively binds to activated Rsk1 following EGF stimulation, and serves as a tool for detecting the activation status of intracellular Rsk1 and PKCα, as well as for functional analysis of SLK. Bisindolylmaleimide III can be used in studies of signal transduction and colorectal cancer .
loading...
    loading...
Cat. No.: HY-W013242
CAS No.: 5561-99-9
Synonyms: cis-11-Eicosenoic acid
Gondoic acid (cis-11-Eicosenoic acid), a monounsaturated long-chain fatty acid, is contained in a variety of plant oils and nuts. Gondoic acid can exert anti-inflammatory activity by inhibiting the production of ROS and the PKCθ/ERK/STAT3 signaling pathway. Gondoic acid can be used as a raw material for medical supplies and a moisturizing ingredient in cosmetic creams .
loading...
    loading...
Cat. No.: HY-131686
CAS No.: 59247-13-1
Ganglioside GT1b (bovine) ammonium is a member of the ganglioside family. Ganglioside GT1b (bovine) ammonium acts as a protective signal against nerve injury-induced spinal synapse elimination. Ganglioside GT1b (bovine) ammonium induces HA synthesis and the phosphorylation of Akt/mTOR in orbital fibroblasts. Ganglioside GT1b (bovine) ammonium enhances porcine oocyte maturation and induce activation of EGFR and ERK1/2 signaling. Ganglioside GT1b (bovine) ammonium is a putative host cell receptor for the Merkel cell polyomavirus. Ganglioside GT1b (bovine) ammonium can be used for the researches of cancer, infection, immunology, endocrinology and neurological disease, such as Thyroid eye disease .
loading...
    loading...
Cat. No.: HY-143212
CAS No.: 65886-80-8
Synonyms: 1-Stearoyl-2-docosahexaenoyl-sn-glycerol
18:0-22:6 DG (1-Stearoyl-2-docosahexaenoyl-sn-glycerol) is a diacylglycerol (DG) that can interact with RasGRP (Ras guanine nucleotide-releasing protein) (Ki = 8.37 μM) and modulate the activation of MAP kinases (such as ERK1/ERK2), which play a crucial role in cellular signaling processes. 18:0-22:6 DG can also activate protein kinase C (PKC) isozyme. 18:0-22:6 DG can be used for research of cancer, immunology and metabolic disease .
loading...
    loading...
Cat. No.: HY-111083
CAS No.: 931695-79-3
Purity:  99.65%
Synonyms: CID23612552
Target:  

GPR55 PERK PKC ERK p38 MAPK

Research Areas:  

Metabolic Disease Cancer

ML191 (CID23612552) is a GPR55 antagonist. ML191 inhibits ERK phosphorylation and PKC β II translocation downstream of GPR55 signaling. ML191 suppresses LPI-induced activation of ERK1/2 and p38 MAPK signaling, blocks the transcription of RANKL-induced osteoclastogenesis markers, and reduces the bone resorption activity of mature osteoclasts promoted by RANKL. ML191 can be used to investigate diseases associated with bone degradation caused by excessive osteoclast activation, such as osteoporosis and bone damage during the formation stage of bone metastases .
loading...
    loading...
Cat. No.: HY-N0427
CAS No.: 6873-13-8
Phellodendrine is an orally active plant alkaloid. Phellodendrine inhibits the proliferation of KRAS-mutated pancreatic cancer cells by suppressing macropinocytosis and glutamine metabolism, inducing ROS accumulation and mitochondrial apoptosis. Phellodendrine promotes autophagy by activating the AMPK/mTOR pathway, alleviating intestinal damage in ulcerative colitis. Phellodendrine can alleviate gouty arthritis by inhibiting the IL-6/STAT3 signaling pathway. Phellodendrine suppresses allergic reactions by altering the conformation of MRGPRB3/MRGPRX2 protein, thereby inhibiting the activation of PKC and subsequent downstream MAPK and NF-κB signaling. Phellodendrine inhibits the AKT/NF-κB pathway and down-regulates the expression of COX-2, thereby protecting zebrafish embryos from oxidative stress. Phellodendrine has an anti-major depressive disorder (MDD) effect by down-regulating CHRM1, HTR1A, and the PI3K/Akt signaling pathway .
loading...
    loading...
Cat. No.: HY-N8303
CAS No.: 21187-73-5
Gardenin A is an orally active and synthetic PMF analogue with the neurotrophic effect for neurite outgrowth and neuronal differentiation. Gardenin A promotes neuritogenesis via activating MAPK/ERK, PKC, and PKA, but not TrkA, CREB signaling pathways. Gardenin A also has sedative, anxiolytic, antidepressant, and anticonvulsant effects .
loading...
    loading...
Cat. No.: HY-131900
CAS No.: 84477-87-2
Purity:  99.96%
Target:  

PKC PKA PKG Arp2/3 Complex

Research Areas:  

Others

Protein kinase inhibitor H-7 is a selective inhibitor of PKC and cyclic nucleotide-dependent protein kinases, with a Ki value of 6.0 μM for rabbit protein kinase C, a Ki value of 3.0 μM for rabbit cAMP-dependent protein kinase, and a Ki value of 5.8 μM for porcine cGMP-dependent protein kinase. Protein kinase inhibitor H-7 has no effect on Ca 2+-calmodulin-dependent enzymes. Protein kinase inhibitor H-7 regulates the Actin cytoskeleton, inhibits contractility, disrupts stress fibers, induces protrusive activity, stabilizes intercellular junctions, and triggers rapid and reversible cytoskeletal reorganization. Protein kinase inhibitor H-7 serves as a research tool for elucidating the functions of protein kinase C-mediated signaling systems .
loading...
    loading...
Cat. No.: HY-P3012
CAS No.: 107200-92-0
Cathepsin G is a pH-dependent serine protease. Cathepsin G hydrolyzes diverse synthetic and protein substrates and remodels extracellular matrix. Cathepsin G exerts immunomodulatory effects via recruiting phagocytes, enhancing T cell motility, activating ERK1/2 and p38 MAPK signaling, and mediating PKCζ membrane translocation. Cathepsin G regulates inflammatory responses by cleaving inflammatory mediators. Cathepsin G participates in vascular regulation by converting angiotensin I to angiotensin II. Cathepsin G induces PAR4-dependent platelet activation, facilitates platelet-neutrophil aggregation, and mediates VITT-related NETosis, thrombus formation. Cathepsin G can be used for the research of immune thrombotic thrombocytopenia, cardiovascular disease, and select autoimmune and inflammatory diseases .
loading...
    loading...