From 11:00 pm to 12:00 pm EST ( 8:00 pm to 9:00 pm PST ) on January 6th, the website will be under maintenance. We are sorry for the inconvenience. Please arrange your schedule properly.
Rimegepant (BMS-927711) is an orally bioavailable and blood-brain barrier permeable antagonist of CGRP and AMY1 receptors, with a pIC50 of 8.01 and a Ki of 0.027 nM for human CGRP receptors. Rimegepant antagonizes cAMP production induced by αCGRP, βCGRP and amylin at CGRP and AMY1 receptors in humans, rats and mice, as well as at rat AMY3 receptors. Rimegepant can be used in research related to migraine .
LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
DSPE-PEG 2000-Mannose is a mannose-containing lipid. DSPE-PEG 2000-Mannose is used to prepare mannose-conjugated Liposome (Man-lipo) for siRNA delivery. Mannose-modified liposomes encapsulating IDO siRNA (Man-lipo-siIDO) preferentially knock down IDO expression in the draining lymph nodes and spleens of melanoma-bearing mice. Man-lipo-siIDO delays the onset time of melanoma and reduces tumor volume .
Mouse Serum Albumin is most abundant protein in plasma, which leaks into the brain parenchyma when the blood-brain barrier (BBB) is impaired. Mouse Serum Albumin induces astrocytes to A1 phenotype to remarkably increase levels of Elovl1. Mouse Serum Albumin promotes VLSFAs secretion and causes neuronal lippoapoptosis through endoplasmic reticulum stress response pathway. MSA-activated microglia triggeres remarkable tau phosphorylation at multiple sites (Ser202/Thr205) through NLRP3 inflammasome pathway. Mouse Serum Albumin decreases the spatial learning and memory abilities in mice. Mouse Serum Albumin can be used for the study of neurodegenerative diseases like Alzheimer’s disease (AD) and frontotemporal dementia (FTD) .
Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2 .
Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes .
Trilaurin is an orally active triglyceride. Trilaurin inhibits DMBA-induced, croton oil-promoted skin tumor formation in Swiss Webster mice. Trilaurin increases plasma high-density lipoprotein cholesterol and apolipoprotein A-I concentrations. Trilaurin is used as an occlusive skin conditioning agent and/or non-aqueous thickener in cosmetics .
VK-2019 is an orally bioavailable selective inhibitor of EBNA1. By binding to the protein-DNA interface to interfere with the recruitment and anchoring of the viral DNA replication machinery, VK-2019 effectively blocks the replication and proliferation of EBV in latently infected cells. VK-2019 reduces the copy number and gene expression level of Epstein-Barr virus in tumor cells, decreases the number of EBER-positive cells, and exhibits significant antiviral, immunomodulatory and antiproliferative activities. VK-2019 successfully inhibits tumor growth in EBV-dependent xenograft models. VK-2019 has favorable systemic exposure and acceptable safety profiles, and is widely used in research on advanced nasopharyngeal carcinoma and various EBV-associated cancers .
pGk13a TFA is an azide (azide group can be combined with fluorophore)-containing amphiphilic membrane labeling probe. pGk13a TFA enables high-resolution imaging of cell membranes in the ultrastructural membrane expansion microscopy (umExM) technique, facilitating the observation of membrane-associated structures and proteins. pGk13a TFA can be used for neuronal structural studies .
PFI-653 (Vanin-1-IN-1, compound 3), a chemical probe, is a vanin-1 inhibitor that binds to plasma vanin-1 from mouse, rat, dog, and human. Vanin-1 is a cell surface-associated inositol (GPi) -anchored protein that plays important roles in metabolism and inflammation. PFI-653 inhibits vanin-1 from different species with IC50s of 6.85 nM (human recombinant plasma vanin-1), 9.0 nM (human plasma vanin-1), 24.5 nM (mouse recombinant vanin-1), and 53.4 nM (mouseplasma vanin-1) .
MAC glucuronide phenol-linked SN-38 is a pH-susceptible lactone MAC glucuronide phenol-linked SN-38 (DNA topoisomerase I inhibitor) agent linker. MAC glucuronide phenol-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 113 and 67 ng/mL, respectively.Albumin-coupled MAC glucosidol-linked SN-38 shows good stability in mouseplasma .
Murine Fibrinogen is a native fibrinogen derived from mouseplasma. Murine Fibrinogen acts as a cerebrovascular permeability enhancer. Murine Fibrinogen activates matrix metalloproteinase-9 (MMP-9), downregulates the expression of vascular endothelial cadherin (VE-cadherin), and upregulates the expression of plasmalemmal vesicle-associated protein-1 (PV-1). Murine Fibrinogen increases macromolecular leakage from pial veins, thereby disrupting the microvascular integrity of cerebral blood vessels. Murine Fibrinogen can be used in studies related to cerebrovascular dysfunction .
Zotiraciclib (TG02; SB1317) is an orally active JAK2/FLT3/CDK2 inhibitor with IC50 values of 13 nM, 73 nM and 56 nM , respectively. Zotiraciclib inhibits cancer cell proliferation, tumor growth and the activity of CYP2D6. Zotiraciclib exhibits high plasma protein binding rate, Caco-2 permeability and tissue distribution capacity, as well as metabolic stability in human and canine liver microsomes. Zotiraciclib achieves tumor growth inhibition in nude mouse models of colon cancer and lymphoma xenografts. Zotiraciclib can be used for research related to colon cancer, B-cell lymphoma, advanced leukemia, acute leukemia and multiple myeloma .
PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouseplasma.
ARI-3099 is an oral fibroblast activation protein (FAP) inhibitor. ARI-3099 specifically inhibits the proteolytic activity of FAP and blocks the cleavage of human FGF-21 between residues P171 and S172. ARI-3099 extends the half-life of circulating human FGF-21 in mice. ARI-3099 can be used in the research of type 2 diabetes and metabolic disorders .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histone deacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasmaleptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsin B and other lysosomal proteases to enable payload release following lysosomal internalization.Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
Pantothenate kinase-IN-1 is a PANK3 inhibitor with an IC50 of 0.51 μM. Pantothenate kinase-IN-1 acts as a pantothenate-competitive inhibitor, which occupies the pantothenate-binding site of PANK3 and binds to both protomers in the PANK3 dimer. Pantothenate kinase-IN-1 exhibits metabolic stability in mouse and rat plasma. Pantothenate kinase-IN-1 can be used in the research of pantothenate kinase-associated neurodegenerative diseases and metabolic diseases .
FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
Anti-Mouse OX40L/CD134L Antibody (RM134L) is an anti-mouseOX40L/CD134L IgG2b monoclonal antibody. Anti-Mouse OX40L/CD134L Antibody (RM134L) reduces immune response by inhibiting the OX40/OX40L signaling pathway. Anti-Mouse OX40L/CD134L Antibody (RM134L) can inhibit plasma cell differentiation and antibody secretion. Anti-Mouse OX40L/CD134L Antibody (RM134L) can prolong the survival time of cell transplantation by inhibiting CD4 + T cells. Anti-Mouse OX40L/CD134L Antibody (RM134L) can be used for researches on inflammation and cancer such as graft versus host disease (GVHD), allergic reaction, lupus nephritis and hepatocellular carcinoma (HCC) .
pGk13a is an amphipathic membrane-labeling probe containing an azide group, which can bind to fluorophores. pGk13a enables high-resolution imaging of cell membranes in the ultrastructure expansion microscopy (umExM) technique, facilitating the observation of membrane-associated structures and proteins. pGk13a is applicable to neuronal structure research .
Enpp-1-IN-11 (compound 23) is a potent Ecto-nucleotide pyrophosphatase/phosphodiesterases 1 (ENPP1) inhibitor with an Ki value of 45 nM. Enpp-1-IN-11 exhibits low clearance in human and mouse liver microsomes, good plasma stability in human and mouseplasma. Enpp-1-IN-11 can be used for researching anticancer .
ALD1613 is a potent neutralizing monoclonal antibody against adrenocorticotropic hormone (ACTH). ALD1613 neutralizes ACTH-induced signaling and inhibits ACTH-induced cyclic AMP accumulation in a mouse adrenal cell line (Y1) via all five melanocortin receptors. ALD1613 significantly reduces plasma corticosterone levels in wild-type rats. ALD1613 can be used in the study of diseases associated with elevated ACTH levels .
(S)-β-Aminoisobutyric acid hydrochloride is a cytoprotective agent, which is a non-proteinogenic amino acid enantiomer derived from valine metabolism in skeletal muscle mitochondria. The plasma level of (S)-β-Aminoisobutyric acid hydrochloride increases significantly after acute aerobic exercise (and is not affected by the AGXT2 rs37369 genotype), and it is secreted by mouse extensor digitorum longus and soleus muscles in ex vivo contraction assays. (S)-β-Aminoisobutyric acid hydrochloride specifically protects osteocytes from oxidative stress-induced cell death .
GZNL-P36 is an orally active inhibitor for SARS-CoV-2 papain-like protease (PL pro), with an IC50 of 6.45 nM. GZNL-P36 inhibits SARS-CoV and its variants with EC50 range from 58.2 nM to 2.66 μM. GZNL-P36 exhibits a peak plasma concentration Cmax of 549 ng/mL, a half-life T1/2 of 1.45 h and a bioavailability of 74.7% in CD-1 mouse. GZNL-P36 exhibits antiviral activity in SARS-CoV-2 XXB.1 infection in mouse .
SARM1-IN-4 (Compound 7) is an orally active SARM1 inhibitor. After being orally administered at a dose of 50 mg/kg in a mouse model, it can reduce the level of plasma neurofilament light chain (NfL). SARM1-IN-4 prevents programmed axonal degeneration by inhibiting the NAD+ hydrolase activity of SARM1, and it can be used in research related to neurodegenerative diseases and neurological disorders (such as multiple sclerosis, amyotrophic lateral sclerosis, Parkinson's disease, and peripheral neuropathies, etc.).
Manusiran (Divesiran) is a GalNac-siRNA targeting liver and transmembrane serine protease 6 (Serine protease 6). Manusiran increases hepatic Hepcidin synthesis and plasma levels by silencing TMPRSS6, a negative regulator of hepcidin production, and limits the availability of iron required for erythropoiesis. Combined use of Manusiran with Deferiprone (HY-B0568) reduces ineffective erythropoiesis and hepatic iron overload in a mouse model of β-thalassemia. Manusiran can be used for research on polycythemia vera, type 1 hereditary hemochromatosis, and β-thalassemia .
VIP236 is a small-molecule drug conjugate targeting αvβ3 integrin. VIP236 achieves tumor homing via specific binding to αvβ3 integrin and delivers its payload to the tumor microenvironment. The linker of VIP236 is cleavable by neutrophil elastase, which is highly expressed in the tumor microenvironment, to release the payload 7-ethylcamptothecin. This payload induces DNA damage by inhibiting topoisomerase 1, thereby exerting anti-tumor effects. VIP236 exhibits excellent plasma stability and tumor targeting property, with a tumor/plasma payload ratio 10-fold higher than that of the single administration. It effectively induces tumor regression, reduces metastasis formation, and shows good tolerance in mouse models. VIP236 has been used in studies related to non-small cell lung cancer, clear cell renal cell carcinoma, colon cancer, triple-negative breast cancer, small cell lung cancer, and metastatic solid tumors .
ST-148 is a novel small molecule compound that has potent inhibitory effects against all four dengue virus serotypes. In the nonlethal AG129 mouse dengue virus infection model, ST-148 significantly reduced viremia and viral load in vital organs and tended to reduce plasma cytokine levels. Compound resistance was associated with the dengue virus capsid (C) gene, and the direct interaction of ST-148 with the C protein was presumed to be achieved through the protein's built-in fluorescence change in the presence of the compound. Therefore, ST-148 appears to interact with the dengue virus C protein and inhibit one or more unique steps of the viral replication cycle.
MU1920 is an ATP-competitive, selective inhibitor for haspin with an IC50 of 6 nM. MU1920 exhibits good pharmacokinetic properties and metabolic stability in mouseplasma and microsomes without obvious anticancer effects, which can be used for development of chemical probes .
DOTA-bis(tert-butyl)ester is a DOTA-based metal chelator that can bind to radionuclides and is used to prepare radionuclide conjugates (RDCs). DOTA-bis(tert-butyl)ester can be conjugated with different salts to form different metal chelators, such as (HY-B1244) hydrochloride to obtain DOTA-MN2. DOTA-MN2 can be reacted with [67]Ga-citrate to obtain radiolabeling. When (67)Ga-DOTA-MN2 is incubated in phosphate buffer solution or mouseplasma for 24 hours, it does not undergo significant decomposition. In the biodistribution experiment of NFSa tumor mice, it has high tumor uptake and rapid plasma clearance, and is a good material for SPECT and PET studies.
KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
Encephalitic alphavirus-IN-1 has antiviral activity for VEEV and EEEV with EC50s of 0.24 μM and 0.16 μM, respectively. Encephalitic alphavirus-IN-1 has robust mouseplasma stability, and no obvious cytotoxicity .
ML356 (Compound 16) is an inhibitor for fatty acid synthase (FAS), that inhibits the thioesterase domain of FAS (FAS TE) with an IC50 of 0.334 μM, and blocks the de novo palmitate synthesis in PC-3 cell with an IC50 of 20 μM. ML356 exhibits good membrane permeability, and good stability in human and mouseplasma .
PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouseplasma. PAT-048 reduces dermal fibrosis in vivo .
KLYP961 is a selective and orally active dual inhibitor of inducible and neuronal NO synthase (IC50 = 50-400 nM). KLYP961 can inhibit endotoxin-evoked plasma nitrates increases and attenuate pain behaviors in a mouse formalin model. KLYP961 can attenuate carrageenin-induced edema and inflammatory hyperalgesia and writhing response elicited by Phenylbenzoquinone (HY-W275039). KLYP961 can be used for the research of neurological disease .
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
TLR8 agonist 8 (Compound II-72) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 8 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 8 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 89% .
Stearoyl-L-carnitine-d3 is the deuterium labeled Stearoylcarnitine. Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2 .
GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
C20 Sphingomyelin (d18:1/20:0) (N-eicosanoyl-D-erythro-Sphingosylphosphorylcholine; SM(d18:1/20:0)) is a naturally occurring sphingolipid. C20 Sphingomyelin (d18:1/20:0) levels are upregulated in the hippocampus of streptozotocin (HY-13753)-induced diabetic rats and in human plasma, positively correlating with insulin resistance in obese humans. C20 Sphingomyelin (d18:1/20:0) is also upregulated in the liver of a mouse model of Niemann-Pick C1 disease, a neurodegenerative cholesterol sphingolipid lysosomal storage disorder.
GSK1842799, an alkyl-substituted biaryl amino alcohol, is a selective S1P1 modulator developed for multiple sclerosis (MS). Upon phosphorylation, GSK1842799-P exhibited subnanomolar S1P1 agonist activity with over 1000-fold selectivity over S1P3. The compound showed good oral bioavailability, rapid in vivo conversion to GSK1842799-P, and significant lymphocyte count reduction at 0.1 mg/kg. It matched FTY720 efficacy at 3 mg/kg in the mouse EAE model and achieved comparable plasma levels to FTY-720 phosphate in cynomolgus monkeys. With favorable ADME, PK/PD properties, and toxicology, GSK1842799 advanced to further clinical development .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0))-d3 is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. LacCer (d18:1/16:0) is also upregulated in a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder). LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
AM4085 is an orally active Antagonist for FmlH with an IC50 of 0.19 μM. AM4085 reveals metabolic stability in mouse liver microsomes and blood plasma .
JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
SMP-88480 is an Antibody-Drug Conjugates (ADCs). SMP-88480 is stable in mouse, monkey and human plasma and has in vivo tumor inhibitory effects on ovarian cancer, gastric cancer, and breast cancer .
Acrophylline is an antiallergic compound. Acrophylline inhibits mast cell degranulation. Acrophylline reduces the plasma leakage
in mouse ear in a passive cutaneous anaphylactic (PCA) reaction. Acrophylline is an alkaloid can be isolated from acronychia haplophylla .
BH-Vis is a two-photon fluorescent probe that inhibits cell plasma membrane (CPM). BH-Vis has great potential to accurately identify pyroptosis at the cellular level during AAA development in the mouse abdominal aortic aneurysm AAA model .
RBx-0597 is a potent and selective DPP-IV inhibitor, demonstrating IC50 values of 32, 31, and 39 nM against human, mouse, and rat plasmaDPP-IV, respectively. RBx-0597 shows potential for type 2 diabetes research .
NU6301 is a NU6102 (a CDK2 inhibitor) (HY-15569) prodrug. NU6301 can rapidly generate NU6102 in mouseplasma. NU6301 has anticancer activity against endometrial cancer .
ATM Inhibitor-11 (Compound 1) is an inhibitor for ATM with an IC50 of 0.32 nM. ATM Inhibitor-11 inhibits the KAP1 phosphorylation with an IC50 of 0.97 nM. ATM Inhibitor-11 exhibits high exposure in the brain, heart and plasma of ICR mouse. ATM Inhibitor-11 exhibits anti-tumor efficacy in NCI-H441 xenograft mouse model .
Antidepressant agent 9 (Compound 24) is an orally active and BBB-penetrable NMDAR and SERT inhibitor with IC50 values of 3.50 μM and 1044 nM, respectively. Antidepressant agent 9 has good metabolic stability and plasma exposure. Antidepressant agent 9 can exert antidepressant-like activity in the mouse forced swim test .
C2 3'-Sulfo galactosylceramide (d18:1/2:0) (C2 Sulfatide) is one of the sulfatide class of glycolipids. C2 3'-Sulfo galactosylceramide (d18:1/2:0) can be used in the quantification of lysosulfatides in mouse brain tissue and plasma .
ABCG2-IN-4 (Compound K31) is an orally active inhibitor for ABCG2, which reduces the release of Protoporphyrin IX (PPIX) (HY-B1247) from erythrocytes into plasma, and prevents the reduces phototoxicity. ABCG2-IN-4 exhibits anti-inflammatory and antioxidant activity in mouse models .
FABP4-IN-4 (Compound 30) is an orally active inhibitor for FABP, with IC50 of 1.18 μM for FABP 1. FABP4-IN-4 improves the glucose tolerance, reduces the level of blood glucose, plasma lipids and hepatic inflammatory factors, attenuates hepatic steatosis, and exhibits anti-inflammatory effects in mouse diet-induced obesity models .
σ1 Receptor ligand 1 (compound 5I) is a σ1 receptor ligand with a Ki of 3.9 nM. σ1 Receptor ligand 1 has a high plasma protein binding (89%) and promising metabolic stability in the presence of mouse liver microsomes and NADPH. σ1 Receptor ligand 1 can be utilized in neurological and cancer research .
TLR8 agonist 7 (Compound II-36) is an agonist for Toll-like receptor 8 (TLR8) with EC50 <250 nM. TLR8 agonist 7 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 7 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 98% .
Ferroptosis-IN-12 (Cpd-A1) is a ferroptosis inhibitor. Ferroptosis-IN-12 exhibits effective ferroptosis inhibition in Erastin (HY-15763)-treated mouse tubular epithelial cells (mTECs) and improves kidney function, alleviates renal tubular damage, and reduces inflammation in a dose-dependent manner in acute kidney injury (AKI) mouse models induced by ischemia/reperfusion (I/R) or cecal ligation and puncture (CLP). Ferroptosis-IN-12 demonstrates good plasma stability and high distribution in kidney tissues in pharmacokinetic studies in mice. Ferroptosis-IN-12 holds promise for research in the field of acute kidney injury (AKI) .
ASK1-IN-8 (Compound 35) is an orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1) with an IC50 value of 1.8 nM . In an experimental mouse model of liver injury induced by Acetaminophen (HY-66005), ASK1-IN-8 can significantly reduce the plasma alanine transaminase (ALT) level, protecting the liver . ASK1-IN-8 can be used in research related to liver diseases .
TLR8 agonist 9 (Compound II-77) is an agonist for Toll-like receptor 8 (TLR8) with EC50 of 0.25-1 μM. TLR8 agonist 9 is stable in human and murine plasma, induces secretion of cytokines TNFα, with EC50 <1 μM. TLR8 agonist 9 exhibits antitumor activity in MC38-HER2 xenograft mouse model with a tumor growth inhibition (TGI) rate of 97% .
Stearoyl-L-carnitine-d9 chloride is the deuterium labeled Stearoyl-L-carnitine chloride. Stearoyl-L-carnitine chloride, a fatty ester lipid molecule, is an endogenous metabolite. Stearoyl-L-carnitine chloride can be used as PKC inhibitor. Stearoyl-L-carnitine chloride accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoyl-L-carnitine chloride inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoyl-L-carnitine chloride acts as a metabolomics biomarker for Parkinson’s disease. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2 .
NQO1-responsive prodrug is a prodrug of Gemcitabine (dFdC) (HY-17026) with anti-cancer effect. NQO1-responsive prodrug remains stable in plasma and liver/intestinal S9 fractions, releasing dFdC in an NQO1-dependent manner. NQO1-responsive prodrug induces S-phase arrest and apoptosis. NQO1-responsive prodrug inhibits tumor growth in an A549 xenograft mouse model. NQO1-responsive prodrug can be used for breast and non-small cell lung cancer (NSCLC) research .
Antimicrobial agent-34 (compound 4h) is an antibacterial agent (MIC = 1–4 μg/mL), with a clogP value of 9.14. Antimicrobial agent-34 has good plasma stability (HC50 of 131.1 μg/mL) and good membrane selectivity (HC50/MIC is 65.6), with rapid sterilization capability. Antimicrobial agent-34 destroys the integrity of bacterial cell membranes, induces an increase in intracellular reactive oxygen species, and leaks protein and DNA, ultimately leading to bacterial death. Antimicrobial agent-34 demonstrates significant in vivo antibacterial potency in a mouse sepsis model infected with Staphylococcus aureus ATCC43300 .
Dieugenol is a neolignan that has been found in N. leucantha and has antioxidative and antiprotozoal activities. It inhibits the formation of thiobarbituric acid reactive substances (TBARS) and scavenges superoxide anions, but not hydroxyl radicals, in cell-free assays. It has anti-trypanosomal activity against T. cruzi amastigotes and trypomastigotes (IC50s=15.1 and 11.5 μM, respectively) but is cytotoxic to NCTC L-929 fibroblasts with a 50% cytotoxic concentration (CC50) value of 58.2 μM.2 Dieugenol (15 μM) disrupts the integrity of the T. cruzi trypomastigote plasma membrane but does not induce the production of reactive oxygen species (ROS) in trypomastigotes or LPS-stimulated and unstimulated isolated mouse peritoneal macrophages.
18-Hydroxy-11-deoxy corticosterone (18-OH-DOC) is a mineralocorticoid whose synthesis is regulated by adrenocorticotropic hormone (ACTH) and angiotensin II.
18-Hydroxy-11-deoxy corticosterone is an intermediate in the metabolism of progesterone and plays an important role in regulating blood pressure and water-salt balance. Continuous infusion of
18-Hydroxy-11-deoxy corticosterone can increase systolic blood pressure in rats, and plasma levels of
18-Hydroxy-11-deoxy corticosterone are significantly elevated in the db/db mouse model of type 2 diabetes, suggesting its potential involvement in metabolic dysregulation and diabetes-related regulation.
18-Hydroxy-11-deoxy corticosterone holds promise for research in areas such as hypertension, diabetes, and other related fields .
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
TSR-011-isomer is an isomer of Belizatinib (HY-17603), a ALK inhibitor with an IC50 of 6 nM. TSR-011-isomer acts as a substrate for metabolic hydrolysis and NADPH-dependent metabolism. TSR-011-isomer undergoes enzymatic hydrolysis in mouseplasma and NADPH-dependent metabolism in mouse liver microsomes, thereby supporting clearance processes. TSR-011-isomer can be used in studies related to ALK-driven cancers .
DNA Gyrase/ribosomes-IN-1 is a bacterial ribosome and DNA gyrase inhibitor, with IC50 values of 1.11 μM and 3.31 μM, respectively. DNA Gyrase/ribosomes-IN-1 also inhibits CYP3A4, with an IC50 of 18.5 μM, and exhibits stability in mouseplasma and liver microsomes. DNA Gyrase/ribosomes-IN-1 inhibits bacterial protein synthesis by interacting with ribosomal RNA and associated sites. DNA Gyrase/ribosomes-IN-1 suppresses bacterial DNA replication by interacting with the gyrase complex. DNA Gyrase/ribosomes-IN-1 restores activity against macrolide-resistant, erm-mediated Gram-positive pathogens and enhances activity against Gram-negative bacteria such as Haemophilus influenzae and Moraxella catarrhalis. DNA Gyrase/ribosomes-IN-1 can be used in research on community-acquired bacterial pneumonia .
Neuro-DiO 4-chlorobenzenesulfonate is a hydrophobic C18alkyl chain carbocyanine dye with green fluorescence, commonly used as a vascular marker, cell internalizer and deposition agent. Neuro-DiO 4-chlorobenzenesulfonate inserts its alkyl chain into the endothelial plasma membrane via liposome-mediated perfusion to achieve vascular labeling. Neuro-DiO chlorobenzenesulfonate can also stain the cell membrane and cytoplasm of cancer cells to assist in confocal microscopy observations. Neuro-DiO chlorobenzenesulfonate can be released from nanosponges and accumulate on the surface of mouse retina, then internalize into retinal ganglion cells, which is applicable to researches related to glaucoma and other diseases. It should be noted that during liposome-mediated vascular staining in mice, Neuro-DiO 4-chlorobenzenesulfonate may cause leakage of airway lavage fluid .
LOC14 (Standard) is the analytical standard of LOC14 (HY-100432). This product is intended for research and analytical applications. LOC14 is a potent Protein disulfide isomerase (PDI) inhibitor with EC50 and Kd values of 500 nM and 62 nM, respectively. LOC14 exhibits high stability in mouse liver microsomes and blood plasma, low intrinsic microsome clearance, and low plasma-protein binding .
LOC14 inhibits PDIA3 activity, decreases intramolecular disulfide bonds and subsequent oligomerization (maturation) of HA in lung epithelial cells .
RBP4-IN-2 (Compound 14) is a RBP4 inhibitor. RBP4-IN-2 can reduce RBP4 in mouseplasma by more than 50%. RBP4-IN-2 can be used to study diseases where excessive lipofuscin accumulates in the retina .
PAT-505 (Standard) is the analytical standard of PAT-505 (HY-107781). This product is intended for research and analytical applications. PAT-505 is a potent, selective, noncompetitive and orally available autotaxin inhibitor, with an IC50 of 2 nM in Hep3B cells, 9.7 nM in human blood and 62 nM in mouseplasma.
PI3K-001 is a cathepsin B-responsive prodrug and antifibrotic agent. PI3K-001 undergoes cathepsin B-mediated cleavage of the Val-Ala linker in fibrotic lung lesions to release an active PI3K inhibitor payload, while it remains stable in healthy tissues. PI3K-001 improves collagen deposition, tissue collapse and alveolar injury in fibrotic lung tissues. PI3K-001 is applicable for the research of pulmonary fibrosis .
Piezo1 agonist 2 (Compound PD2) is a blood-brain barrier-permeable Piezo1 agonist and Jedi2 (HY-131018) conjugate that utilizes LAT1. Piezo1 agonist 2 releases Jedi2 in mice. Piezo1 agonist 2 can be used for the research of neurodegenerative diseases .
LY3358966 is an orally active sodium-dependent phosphate cotransporter 2b (NPT2b) inhibitor with a human IC50 of 32.4 nM, mouseIC50 of 43.9 nM, and rat of IC50 26.8 nM. LY3358966 inhibits NPT2b-mediated intestinal phosphate transport, decreases acute phosphate uptake into plasma, and increases fecal phosphate excretion. LY3358966 can be used for the research of renal disease .
TML-2Cl is a dichloro-modified trimethyl lock adapter for antibody-drug conjugates and payload releaser.TML-2Cl undergoes 1,6-elimination followed by rapid self-cyclization to facilitate release of the payload Exatecan after cathepsin B cleavage of the associated linker.TML-2Cl exhibits high stability when conjugated to a drug and high intrinsic hydrophobicity.TML-2Cl can be used for the research of gastric carcinoma .
Z971169476 is a sulfonamide-based protein-RNA interaction inhibitor targeting the KH34 region of insulin-like growth factor 2 mRNA binding protein 2 (IGF2BP2/IMP2) .
Anti-Eastern equine encephalitis virus E2 protein Antibody (EEEV-3) reacts with the B domain of the E2 glycoprotein on the eastern equine encephalitis virus (EEEV). Anti-Eastern equine encephalitis virus E2 protein Antibody (EEEV-3) exhibits a modest inhibition of viral attachment to the plasma membrane of the cells. Recommend Isotype Controls: Mouse IgG2c kappa, Isotype Control (HY-P99981) .
MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer .
Luteolin 7-O-(6-O-malonyl-β-D-glucoside) is an orally active flavonoid free radical scavenger. Luteolin 7-O-(6-O-malonyl-β-D-glucoside) scavenges free radicals, inhibits the activity elevation of aspartate aminotransferase and alanine aminotransferase in mouseplasma, as well as the elevation of liver lipid hydroperoxide content. Luteolin 7-O-(6-O-malonyl-β-D-glucoside) is applicable for liver injury research .
Aminopyridine 2 is an irreversible, selective, and orally active myeloperoxidase (MPO) inhibitor, with an IC50 of 0.16 μM and a Ki of 24 μM against human MPO. Aminopyridine 2 is applicable to research on chronic inflammatory diseases .
SK-129 is a blood-brain barrier-permeable inhibitor of α-synuclein (αS) oligomers with a Kd of 221 nM. SK-129 preferentially binds to neurotoxic αS oligomers over physiological αS monomers, inhibits αS aggregation, blocks the interaction and co-aggregation of αS with tau protein, and prevents the maturation of αS-tau condensates into amyloid aggregates. SK-129 reduces ROS production, rescues dopaminergic neuron degeneration, improves motor function, restores endogenous dopamine synthesis, increases the number of Tyrosine Hydroxylase-positive neurons, prevents brain histopathological changes, alleviates neuroinflammation, and improves survival rates in relevant models. SK-129 can be used in research related to Parkinson's disease (PD) and Lewy body dementia (LBD) .
BHQ‑3 carboxylic acid is an azo‑containing dark fluorescence quencher. BHQ‑3 carboxylic acid is conjugated to an MMP‑cleavable peptide and paired with a fluorophore to form an activatable probe for MMP activity detection in vitro. BHQ‑3 carboxylic acid shows maximal absorption in the 620 to 730 nm range. BHQ‑3 carboxylic acid–based fluorescent probes can be used in the research of arthritis and tumor‑related pathological processes. .
LN5972 is a selective ACKR3 agonist with an EC50 of 3.40 μM, showing higher selectivity for ACKR3 over CXCR4. LN5972 induces β-arrestin recruitment to ACKR3/CXCR7. LN5972 reduces the surface expression of P-selectin. LN5972 is applicable to studies related to platelet-mediated thrombosis .
MC-cBu-Cit-seco-CBI dimer (Compound 10) is a conjugate of an ADC drug toxin molecule and a linker, which consists of a DNA alkylating agent connected to a reactive maleimide via a protease-cleavable peptidomimetic linker .
FAP Ligand 3 (compound 54) is a reagent that binds to FAP, with a Ki value of 0.092 nM against human targets. FAP Ligand 3 acts as a tumor-retaining agent and serves as a FAP-targeted positron emission tomography (PET) tracer for tumor imaging. FAP Ligand 3 is applicable to studies related to U87MG glioma .
SLC6A19-IN-4 is an allosteric-competitive and orally active B 0AT1 inhibitor. SLC6A19-IN-4 inhibits both human and mouseB 0AT1 with IC50 values of 513 nM and 295 nM, respectively. SLC6A19-IN-4 exhibits excellent metabolic stability. SLC6A19-IN-4 significantly increases urinary phenylalanine (Phe) excretion and reduces plasma Phe levels through dual inhibition of B 0AT1 in both the intestine (reducing absorption) and kidney (promoting excretion) in vivo. SLC6A19-IN-4 can be used for phenylketonuria (PKU) and other disorders involving SLC6-family transporters research .
NEK7 degrader-3 is an orally active and brain-penetrant NEK7molecular glue degrader with a DC50 of 33.1 nM. NEK7 degrader-3 mediates interaction between NEK7 and E3 ligase cereblon, promoting proteasomal degradation of NEK7 and attenuating NLRP3 inflammasome-mediated inflammatory responses. NEK7 degrader-3 inhibits caspase-1 activity, cytokine release of IL-1β, IL-1α, and IL-18, and pyroptosis-related plasma membrane permeabilization. NEK7 degrader-3 shows antiinflammatory activity in an LPS (HY-D1056)-induced neuroinflammation mouse model. NEK7 degrader-3 can be used for the research of neuroinflammation .
Autotaxin-IN-8 (Compound 14E) is an orally active Autotaxin inhibitor with an IC50 of 14.2 nM against hAutotaxin. Autotaxin-IN-8 inhibits Autotaxin activity, MAPK activation, LPAR1 and p-ERK1/2. Autotaxin-IN-8 reduces the phosphorylation levels of JNK and p38. Autotaxin-IN-8 decreases collagen deposition in a mouse model of pulmonary fibrosis. Autotaxin-IN-8 can be used in research related to pulmonary fibrosis .
SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
BDM71230 is an orally active inducer of insulin-degrading enzyme (IDE), with an EC50 of 1.9 μM against human IDE. BDM71230 binds to the interface of IDE dimers and enhances the catalytic activity of IDE via steric effects. BDM71230 can potentiate the hydrolytic effect of IDE on insulin and slightly attenuate the hypoglycemic effect of insulin. BDM71230 serves as a pharmacological tool for investigating IDE function and is applicable to studies related to glucose intolerance .
BH-Vis is a two-photon fluorescent probe that inhibits cell plasma membrane (CPM). BH-Vis has great potential to accurately identify pyroptosis at the cellular level during AAA development in the mouse abdominal aortic aneurysm AAA model .
Neuro-DiO 4-chlorobenzenesulfonate is a hydrophobic C18alkyl chain carbocyanine dye with green fluorescence, commonly used as a vascular marker, cell internalizer and deposition agent. Neuro-DiO 4-chlorobenzenesulfonate inserts its alkyl chain into the endothelial plasma membrane via liposome-mediated perfusion to achieve vascular labeling. Neuro-DiO chlorobenzenesulfonate can also stain the cell membrane and cytoplasm of cancer cells to assist in confocal microscopy observations. Neuro-DiO chlorobenzenesulfonate can be released from nanosponges and accumulate on the surface of mouse retina, then internalize into retinal ganglion cells, which is applicable to researches related to glaucoma and other diseases. It should be noted that during liposome-mediated vascular staining in mice, Neuro-DiO 4-chlorobenzenesulfonate may cause leakage of airway lavage fluid .
BHQ‑3 carboxylic acid is an azo‑containing dark fluorescence quencher. BHQ‑3 carboxylic acid is conjugated to an MMP‑cleavable peptide and paired with a fluorophore to form an activatable probe for MMP activity detection in vitro. BHQ‑3 carboxylic acid shows maximal absorption in the 620 to 730 nm range. BHQ‑3 carboxylic acid–based fluorescent probes can be used in the research of arthritis and tumor‑related pathological processes. .
Mouse Serum Albumin is most abundant protein in plasma, which leaks into the brain parenchyma when the blood-brain barrier (BBB) is impaired. Mouse Serum Albumin induces astrocytes to A1 phenotype to remarkably increase levels of Elovl1. Mouse Serum Albumin promotes VLSFAs secretion and causes neuronal lippoapoptosis through endoplasmic reticulum stress response pathway. MSA-activated microglia triggeres remarkable tau phosphorylation at multiple sites (Ser202/Thr205) through NLRP3 inflammasome pathway. Mouse Serum Albumin decreases the spatial learning and memory abilities in mice. Mouse Serum Albumin can be used for the study of neurodegenerative diseases like Alzheimer’s disease (AD) and frontotemporal dementia (FTD) .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
1,2,3-Tripalmitoleoyl-rac-glycerol is a triacylglycerol containing palmitoleic acid at the sn-1, sn-2 and sn-3 positions. It reduces erythrocyte deformability in a concentration-dependent manner in the Reid filtration assay. Hepatic levels of 1,2,3-tripalmitoleoyl-rac-glycerol are increased in a JAK2L mouse model of hepatic steatosis. 1,2,3-Tripalmitoleoyl-rac-glycerol plasma levels are reduced in patients with predialysis renal disease.
H-Gly-Pro-Hyp-OH is a collagen-derived peptide and also a dipeptidyl peptidase-4 inhibitor.\nH-Gly-Pro-Hyp-OH inhibits the activity of dipeptidyl peptidase-4 in vitro. H-Gly-Pro-Hyp-OH binds to the DNA-binding site of the JUN/FOS complex, blocks the formation of the DNA-JUN/FOS complex, and inhibits transcriptional activity. H-Gly-Pro-Hyp-OH is applicable to research related to skin photoaging, UVB-induced skin aging/photoaging, and thrombosis .
pGk13a TFA is an azide (azide group can be combined with fluorophore)-containing amphiphilic membrane labeling probe. pGk13a TFA enables high-resolution imaging of cell membranes in the ultrastructural membrane expansion microscopy (umExM) technique, facilitating the observation of membrane-associated structures and proteins. pGk13a TFA can be used for neuronal structural studies .
Z-Val-Ala-OH is a dipeptide derivative of valine and alanine. Z-Val-Ala-OH undergoes cleavage by cathepsin B and other lysosomal proteases to enable payload release following lysosomal internalization.Z-Val-Ala-OH can be used for the research of antibody-drug conjugate (ADC) development[1] .
pGk13a is an amphipathic membrane-labeling probe containing an azide group, which can bind to fluorophores. pGk13a enables high-resolution imaging of cell membranes in the ultrastructure expansion microscopy (umExM) technique, facilitating the observation of membrane-associated structures and proteins. pGk13a is applicable to neuronal structure research .
KSL 128114, a peptide inhibitor of syntenin, binds the PDZ1 domain of syntenin with nanomolar affinity. KSL 128114 is resistant toward degradation in human plasma and mouse hepatic microsomes and displays a global PDZ domain selectivity for syntenin .
Anticancer peptoid 1 (Peptoid 1) is a peptoid with antitumor activity. Anticancer peptoid 1 exerts cytotoxicity primarily via plasma membrane damage. Anticancer peptoid 1 exerts cytotoxicity against a broad range of cancer cell lines, including those with multidrug resistance. Anticancer peptoid 1 inhibits tumor growth in a human breast cancer xenotransplantation mouse model without noticeable acute adverse effects. Anticancer peptoid 1 can be used for the research of cancer, such as breast cancer, and prostate cancer .
Anti-Mouse OX40L/CD134L Antibody (RM134L) is an anti-mouseOX40L/CD134L IgG2b monoclonal antibody. Anti-Mouse OX40L/CD134L Antibody (RM134L) reduces immune response by inhibiting the OX40/OX40L signaling pathway. Anti-Mouse OX40L/CD134L Antibody (RM134L) can inhibit plasma cell differentiation and antibody secretion. Anti-Mouse OX40L/CD134L Antibody (RM134L) can prolong the survival time of cell transplantation by inhibiting CD4 + T cells. Anti-Mouse OX40L/CD134L Antibody (RM134L) can be used for researches on inflammation and cancer such as graft versus host disease (GVHD), allergic reaction, lupus nephritis and hepatocellular carcinoma (HCC) .
ALD1613 is a potent neutralizing monoclonal antibody against adrenocorticotropic hormone (ACTH). ALD1613 neutralizes ACTH-induced signaling and inhibits ACTH-induced cyclic AMP accumulation in a mouse adrenal cell line (Y1) via all five melanocortin receptors. ALD1613 significantly reduces plasma corticosterone levels in wild-type rats. ALD1613 can be used in the study of diseases associated with elevated ACTH levels .
Anti-Eastern equine encephalitis virus E2 protein Antibody (EEEV-3) reacts with the B domain of the E2 glycoprotein on the eastern equine encephalitis virus (EEEV). Anti-Eastern equine encephalitis virus E2 protein Antibody (EEEV-3) exhibits a modest inhibition of viral attachment to the plasma membrane of the cells. Recommend Isotype Controls: Mouse IgG2c kappa, Isotype Control (HY-P99981) .
MEDI-579 is a fully human monoclonal antibody against PAI-1, with a KD value of 6 pM for human PAI-1 and 105 pM for rat PAI-1. MEDI-579 restores renal plasmin activity and inhibits PAI-1-mediated intracellular signal transduction. MEDI-579 reduces albuminuria, glomerulosclerosis severity, TGF-β1 expression level, and phosphorylated Smad2 level induced in diabetic mice. MEDI-579 decreases the levels of active PAI-1 in plasma and kidneys, and increases plasma plasmin level in a mouse model of lupus nephritis. MEDI-579 can be used in research related to diabetic nephropathy and lupus nephritis. The recommended isotype control is human IgG1 kappa (HY-P99001) .
Adargiminase (NEI-01) is a modified arginine-depleting enzyme and albumin binder. Adargiminase catalyzes the conversion of arginine to citrulline and ammonia, reduces plasma arginine levels to undetectable levels, and binds to serum albumin from Mus musculus (mouse), Rattus norvegicus (rat), Canis lupus familiaris (dog) and Homo sapiens (human) to extend its half-life. Adargiminase inhibits the viability of ASS1-negative pancreatic cancer cells, and reduces tumor volume and weight. Adargiminase can be used for the research of pancreatic cancer .
Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2 .
Trilaurin is an orally active triglyceride. Trilaurin inhibits DMBA-induced, croton oil-promoted skin tumor formation in Swiss Webster mice. Trilaurin increases plasma high-density lipoprotein cholesterol and apolipoprotein A-I concentrations. Trilaurin is used as an occlusive skin conditioning agent and/or non-aqueous thickener in cosmetics .
3-Hydroxyoctanoic acid is a hydroxylated fatty acid that has been found in the LPS of Pseudomonas aeruginosa and in methyl-branched poly(3-hydroxyalkanoate) (PHA) polymers produced by Pseudomonas oleophores. It is an agonist of the orphan receptor GPR109B, increasing intracellular calcium in human neutrophils endogenously expressing GPR109B. 3-Hydroxycaprylic acid prevents lipolysis in human adipocytes and is upregulated in human plasma in response to a ketogenic diet. Plasma levels of 3-hydroxyoctanoic acid were also increased 3.41-fold in human male runners exhausted on a treadmill and in a mouse model of autism spectrum disorder (ASD) fed a high-glycemic diet.
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0)) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). The levels of LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. In a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder), the expression of LacCer (d18:1/16:0) is also upregulated. LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
Acrophylline is an antiallergic compound. Acrophylline inhibits mast cell degranulation. Acrophylline reduces the plasma leakage
in mouse ear in a passive cutaneous anaphylactic (PCA) reaction. Acrophylline is an alkaloid can be isolated from acronychia haplophylla .
Luteolin 7-O-(6-O-malonyl-β-D-glucoside) is an orally active flavonoid free radical scavenger. Luteolin 7-O-(6-O-malonyl-β-D-glucoside) scavenges free radicals, inhibits the activity elevation of aspartate aminotransferase and alanine aminotransferase in mouseplasma, as well as the elevation of liver lipid hydroperoxide content. Luteolin 7-O-(6-O-malonyl-β-D-glucoside) is applicable for liver injury research .
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface.It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin.This underscores the diverse and essential functions of Plasma kallikrein/KLKB1 in various physiological processes.Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-6*His labeled tag.
Plasma kallikrein/KLKB1 enzymatically cleaves Lys-Arg and Arg-Ser bonds, triggering factor XII activation upon binding to a negatively charged surface.It liberates bradykinin from HMW kininogen and is implicated in the renin-angiotensin system, potentially converting prorenin into renin.This underscores the diverse and essential functions of Plasma kallikrein/KLKB1 in various physiological processes.Plasma kallikrein/KLKB1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Plasma kallikrein/KLKB1 protein, expressed by HEK293 , with C-His labeled tag.
RBP4 Protein transports retinol in blood plasma, delivering it from liver stores to peripheral tissues. Binding to all-trans retinol, it transfers it to STRA6 for efficient cell membrane transport. RBP4 interacts with TTR, preventing kidney filtration, and further supports STRA6 in retinol transport. RBP4 Protein, Mouse (HEK293, His) is the recombinant mouse-derived RBP4 protein, expressed by HEK293 , with C-His labeled tag.
PGCP is a carboxypeptidase with a potentially critical role in the hydrolysis of circulating peptides. It catalyzes the cleavage of terminally unsubstituted dipeptides, releasing amino acids. PGCP Protein, Mouse (HEK293, His) is the recombinant mouse-derived PGCP protein, expressed by HEK293 , with C-6*His labeled tag.
Serpin G1 protein, also known as C1 inhibitor, regulates complement activation, coagulation, fibrinolysis, and kinin production. It forms an inactive complex with C1r or C1s protease and controls C1 complex activation. Serpin G1 Protein, Mouse (HEK293, His) is the recombinant mouse-derived Serpin G1 protein, expressed by HEK293 , with C-6*His labeled tag.
Serpin A5 protein is a heparin-dependent serine protease inhibitor that controls proteolytic activity in body fluids. It binds irreversibly to the serine activation site, inactivating serine proteases and regulating intravascular and extravascular proteolysis. Serpin A5 Protein, Mouse (sf9, His) is the recombinant mouse-derived Serpin A5 protein, expressed by sf9 insect cells , with N-10*His labeled tag.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses.It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups.PLA2G7 Protein, Mouse (sf9, His, Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by sf9 insect cells , with C-Myc, N-10*His labeled tag.
The PLA2G7 protein is a lipoprotein-associated calcium-independent phospholipase A2 that plays a key role in phospholipid catabolism during inflammation and oxidative stress responses.It acts at the lipid-water interface and hydrolyzes the ester bond of the fatty acyl group at the sn-2 position, with particular preference for short-chain fatty acyl groups.PLA2G7 Protein, Mouse (HEK293, His, Myc) is the recombinant mouse-derived PLA2G7 protein, expressed by HEK293 , with C-Myc, N-10*His labeled tag.
Stearoyl-L-carnitine-d3 is the deuterium labeled Stearoylcarnitine. Stearoylcarnitine, a fatty ester lipid molecule, is an endogenous metabolite. Stearoylcarnitine can be used as PKC inhibitor. Stearoylcarnitine accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoylcarnitine inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoylcarnitine acts as a metabolomics biomarker for Parkinson’s disease. Stearoylcarnitine is a less potent inhibitor of GlyT2 .
LacCer (d18:1/16:0) (C16 Lactosylceramide (d18:1/16:0))-d3 is the deuterium labeled LacCer (d18:1/16:0) (HY-153830). LacCer (d18:1/16:0) is an endogenous bioactive sphingolipid that can form membrane microdomains with Lyn kinase and the αi subunits of inhibitory G protein-coupled receptors (GPCRs). LacCer (d18:1/16:0) are elevated in the plasma of insulin-resistant cattle. LacCer (d18:1/16:0) is also upregulated in a mouse model of Niemann-Pick type C1 disease (a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder). LacCer (d18:1/16:0) can be used in research on metabolic diseases and neurodegenerative diseases .
Stearoyl-L-carnitine-d9 chloride is the deuterium labeled Stearoyl-L-carnitine chloride. Stearoyl-L-carnitine chloride, a fatty ester lipid molecule, is an endogenous metabolite. Stearoyl-L-carnitine chloride can be used as PKC inhibitor. Stearoyl-L-carnitine chloride accumulates in β cells, leading to arrest of insulin synthesis and energy deficiency in type 2 diabetes mouse. Stearoyl-L-carnitine chloride inhibits lecithin cholesterol acyltransferase (LCAT) in rat and rabbits plasma. Stearoyl-L-carnitine chloride acts as a metabolomics biomarker for Parkinson’s disease. Stearoyl-L-carnitine chloride is a less potent inhibitor of GlyT2 .
FKK6 is a selective agonist for pregnane X receptor (PXR) with an EC50 of 1.2 µM. FKK6 exhibits good affinity with plasma proteins, and good metabolic metabolism in human microsomes. FKK6 inhibits PXR-related NF-κB signaling pathway, inhibits the expression of inflammatory factors, and exhibits anti-inflammatory activity against DSS (HY-116282)-induced colitis in mouse model .
pGk13a is an amphipathic membrane-labeling probe containing an azide group, which can bind to fluorophores. pGk13a enables high-resolution imaging of cell membranes in the ultrastructure expansion microscopy (umExM) technique, facilitating the observation of membrane-associated structures and proteins. pGk13a is applicable to neuronal structure research .
TML-2Cl is a dichloro-modified trimethyl lock adapter for antibody-drug conjugates and payload releaser.TML-2Cl undergoes 1,6-elimination followed by rapid self-cyclization to facilitate release of the payload Exatecan after cathepsin B cleavage of the associated linker.TML-2Cl exhibits high stability when conjugated to a drug and high intrinsic hydrophobicity.TML-2Cl can be used for the research of gastric carcinoma .
DSPE-PEG 2000-Mannose is a mannose-containing lipid. DSPE-PEG 2000-Mannose is used to prepare mannose-conjugated Liposome (Man-lipo) for siRNA delivery. Mannose-modified liposomes encapsulating IDO siRNA (Man-lipo-siIDO) preferentially knock down IDO expression in the draining lymph nodes and spleens of melanoma-bearing mice. Man-lipo-siIDO delays the onset time of melanoma and reduces tumor volume .
Trilaurin is an orally active triglyceride. Trilaurin inhibits DMBA-induced, croton oil-promoted skin tumor formation in Swiss Webster mice. Trilaurin increases plasma high-density lipoprotein cholesterol and apolipoprotein A-I concentrations. Trilaurin is used as an occlusive skin conditioning agent and/or non-aqueous thickener in cosmetics .
Manusiran (Divesiran) is a GalNac-siRNA targeting liver and transmembrane serine protease 6 (Serine protease 6). Manusiran increases hepatic Hepcidin synthesis and plasma levels by silencing TMPRSS6, a negative regulator of hepcidin production, and limits the availability of iron required for erythropoiesis. Combined use of Manusiran with Deferiprone (HY-B0568) reduces ineffective erythropoiesis and hepatic iron overload in a mouse model of β-thalassemia. Manusiran can be used for research on polycythemia vera, type 1 hereditary hemochromatosis, and β-thalassemia .
Inquiry Online
Your information is safe with us. * Required Fields.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
MedchemExpress Validation 03
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
MedchemExpress Validation 04
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedchemExpress Validation
Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred
to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was
used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.
MedChemExpress values your privacy and your trust is important to us. We use cookies to enhance your website experience. Some cookies are necessary to run the website.
Privacy and Cookie Policy
