“Ligand-gated Ion Channels”的搜索结果
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bitter taste receptor TAS2R1 agonist
Amarogentin (AG), a secoiridoid glycoside mainly extracted from Swertia and Gentiana roots, exhibits anti-oxidative, anti-tumour, and anti-diabetic activities. Amarogentin is an agonist for the bitter taste receptor TAS2R1 and inhibits in LAD-2 cells substance P-induced production of newly synthesized TNF-α.
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composition of fatty acid
Palmitoleic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
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immunomodulatory agent
3-Hydroxyanthranilic Acid (3-HAA, 3-HANA), a tryptophan metabolite, has an immunomodulatory effect that may result from inhibition of PI3K/Akt/mTOR and NF-κB activity, thereby decreasing the production of pro-inflammatory mediators.
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anti-inflammatory agent
Acetosyringone is a phenolic natural product with analgesic, antipyretic and anti-inflammatory actions.
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SHP-1 (PTPN6) agonist
SC-43, a Sorafenib derivative, is a potent and orally active SHP-1 (PTPN6) agonist. SC-43 inhibits the phosphorylation of STAT3 and induces cell apoptosis. SC-43 has anti-fibrotic and anticancer effects.
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GK activator
Dorzagliatin (HMS5552), a dual-acting glucokinase (GK) activator, improves glycaemic control and pancreatic β-cell function in type 2 diabetes.
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GLUT1 inhibitor
Lavendustin B is an inhibitor of HIV-1 integrase interaction with LEDGF/p75 with an IC50 of 94.07 μM. Lavendustin B is an ATP-competitive GLUT1 inhibitor with a Ki of 15 ?M. Lavendustin B is also a weak inhibitor of tyrosine kinases.
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JAK3/STAT5 inhibitor
BD750, an effective immunosuppressant and a JAK3/STAT5 inhibitor, inhibits IL-2-induced JAK3/STAT5-dependent T cell proliferation, with IC50 values of 1.5 μM and 1.1 μM in mouse and human T cells, respectively.
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Gβγ subunit signalling inhibitor
Gallein is a G protein βγ (Gβγ) subunit signalling inhibitor. Gallein disrupts the interaction of Gβγ subunits with the PI3Kγ. Anticancer agent.
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Syk/PI3K inhibitor
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
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Anticancer agent
BDTX-189 is a potent, orally active and selective inhibitor of allosteric EGFR and HER2 oncogenic mutations, including EGFR/HER2 exon 20 insertion mutants. BDTX-189 shows KDs of 0.2, 0.76, 13 and 1.2 nM for EGFR, HER2, BLK and RIPK2, reapectively. Anticancer activity.
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BMP signaling inhibitor
LDN193189 HCl (DM-3189) is the hydrochloride salt of LDN193189, which is a selective BMP signaling inhibitor, and inhibits the transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 of 5 nM and 30 nM in C2C12 cell lines, respectively, 200-fold selectivity for BMP versus TGF-β.
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antioxidant
2-Phospho-L-ascorbic acid trisodium acts as an antioxidant and a stimulator of hepatocyte growth factor (HGF) production.
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natural product
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway.
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flavonoid
Loureirin A is a flavonoid extracted from Dragon's Blood, can inhibit Akt phosphorylation, and has antiplatelet activity.
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EGFR inhibitor
Alflutinib is an EGFR inhibitor that targets both EGFR activating mutations and T790M, thus leading to tumor growth inhibition.
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inhibitor of Ras/Raf-1 interaction
MCP110 is an inhibitor of Ras/Raf-1 interaction. MCP110 blocks the interaction of Ras with Raf. MCP110 disrupts this interaction might can be used for the research of human tumors.
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AMPK activator
IM156 (HL156A), a metformin derivative, is a potent activator of AMPK that increases AMPK phosphorylation.
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inhibitor of EGFR and HER2 oncogenic mutants
Mobocertinib (TAK-788) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
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AMPK activator
ASP4132 is an orally active, potent AMPK activator with an EC50 of 18 nM. ASP4132 has anti-cancer activity and makes tumor regression in breast cancer xenograft mouse models.
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nutritional supplement
Chromium picolinate is a coordination complex consisting of chromium(III) and picolinic acid. It is used as a nutritional supplement for optimal insulin function in patients with Type 2 diabetes or promotion of weight loss.
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Antioxidant agent
Dihydrocaffeic acid is a phenolic acid found in Gynura bicolor, reduces phosphorylation of MAPK p38 and prevent UVB-induced skin damage. Antioxidant potential and anti-inflammatory activity.
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MRTF pathway inhibitor
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression.
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Desmethylanethol trithione
ADT-OH is a derivative of anethole dithiolethione (ADT) and synthetic hydrogen sulfide (H2S) donor.
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Inhibitor of U46619-induced Rat Platelet Aggregation
Timosaponin AIII is a potent Inhibitor of U46619-induced Rat Platelet Aggregation, Selectively Inhibiting TxA2-induced Platelet Activation, Preferably Suppressing TP-mediated Activation of Gq, not G12/13, Signaling Pathways.
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neuroprotection agent
Beta-Asarone, found in certain plants such as Acorus and Asarum, could pass the blood-brain barrier and exerts neuroprotection effects.
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anticancer agent
Solamargine, a derivative from the steroidal solasodine in Solanum species, exhibits anticancer activities in numerous types of cancer. Solamargine induces non-selective cytotoxicity and P-glycoprotein inhibition.
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benzodiazepine derivative drug
Remimazolam, also known as CNS-7056, is a benzodiazepine derivative drug, developed by PAION, in collaboration with Japanese licensee Ono Pharmaceutical as an alternative to the short-acting imidazobenzodiazepine midazolam, for use in induction of anaesthesia and conscious sedation for minor invasive procedures.
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TNF inhibitor
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor.
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potent cerebroprotection
Dehydroascorbic acid, a blood-brain barrier transportable form of vitamin C, mediates potent cerebroprotection in experimental stroke.
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protein-protein interaction (PPI) inhibitor
CB-103 is a first-in-class, orally active protein-protein interaction (PPI) inhibitor of the NOTCH transcriptional activation complex. CB-103 has anti-tumor activity.
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anti-psoriatic agent
Periplogenin is a naturally occurring furanocoumarin found in Angelica dahurica roots, with potent anti-psoriatic effects. Periplogenin induces adipocyte differentiation.
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antiplatelet activities
6-Methoxydihydroavicine is an alkaloid isolated from Zanthoxylum integrifoliolum. 6-Methoxydihydroavicine has antiplatelet activities and inhibits AA-, collagen- and PAF-induced platelet aggregation in vitro.
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p18INK inhibitor
NSC23005 is a p18INK inhibitor. NSC23005 potently promotes hematopoietic stem cell (HSC) expansion (ED50 = 5.21 nM).
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fluorescent indicator
MQAE is a fluorescent indicator that is quenched via collision with chloride, and is more sensitive and selective than 36Cl and microelectrode-based methods for chloride measurement in cells.
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activator of Hsp70 expression and HSF-1 activity
ML346 is an activator of Hsp70 expression and HSF-1 activity, with an EC50 of 4.6 μM for Hsp70.
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Isocyclosporin A is a rearranged degradation product formed by acid treatment of cyclosporin A under aqueous and non-aqueous conditions.
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MAT2A inhibitor
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM.
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iron-chelating inhibitor
VLX600 is an iron-chelating inhibitor of oxidative phosphorylation (OXPHOS).
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inhibitor of platelet aggregation
Ticlopidine (Yuclid, Ticlopidinum, Ticlopidina) is an orally active inhibitor of platelet aggregation induced by adenosine diphosphate (ADP).
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inhibitor of quinone reductase 2 (QR2)
S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1.
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cannabinoid (CB2) agonist
LY2828360 is a slowly acting but efficacious G protein-biased cannabinoid (CB2) agonist, inhibiting cAMP accumulation and activating ERK1/2 signaling.
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EGFR inhibitor
Almonertinib (HS-10296) is an orally available, irreversible, third-generation EGFR tyrosine kinase inhibitor with high selectivity for EGFR-sensitizing and T790M resistance mutations.
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DNA replication inhibitor
Enocitabine is a nucleoside analog, and is a potent DNA replication inhibitor, and a DNA chain terminator.
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ROS1/NTRK inhibitor
Taletrectinib (DS-6051b) is a potent, orally active, and new-generation selective ROS1/NTRK inhibitor.
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Menin-MLL interaction inhibitor
VTP50469 is a potent, highly selective and orally active Menin-MLL interaction inhibitor with a Ki of 104 pM. VTP50469 has potently anti-leukemia activity.
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EGFR/HER2 oncogenic mutants inhibitor
Mobocertinib succinate (TAK-788 succinate) is a potent and orally active inhibitor of EGFR and HER2 oncogenic mutants, including exon 20 insertions, with selectivity over WT EGFR. Antitumor activity.
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Positive Allosteric Modulators (PAMs)
ML-254, also known as VU0430644; is Positive Allosteric Modulators (PAMs) of mGlu5 with Competitive MPEP-Site Interaction.
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OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization agonist
ML335 (CYM 51010, CID-23723457) is an agonist for OPRM1(μ-opioid receptor)-OPRD1(δ-opioid receptor) heterodimerization with EC50 of 403 nM demonstrating selectivity over the individual OPRM1 and OPRD1 receptors and the serotonin HT5A receptor with EC50 of 14.9 μM, 1.1 μM, and >40 μM, respectively.
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inhibitor of amyloid-β fibril formation and aggregation
TAE-1 is an inhibitor of amyloid-β fibril formation and aggregation. TAE-1 inhibits cholinesterases AChE and BuChE with IC50 of 0.3 μM and 3.9 μM, respectively.
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