Search Result
Results for "
Immunology
" in MCE Product Catalog:
5584
Inhibitors & Agonists
25
Biochemical Assay Reagents
484
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-147283
-
-
- HY-131967
-
CD73-IN-4
|
CD73
|
Cancer
Inflammation/Immunology
|
CD73-IN-4 is a potent and selective methylenephosphonic acid CD73 inhibitor, with an IC50 of 2.6 nM for human CD73. CD73-IN-4 is potential for the research of cancer immunology.
|
-
- HY-132230
-
GSK040
|
Epigenetic Reader Domain
|
Cancer
Inflammation/Immunology
|
GSK040 is a potent and highly selective BET BD2 inhibitor, with a pIC50 of 8.3. GSK040 shows more than 5000-fold selectivity for BET BD2 over BET BD1 (pIC50=4.6). GSK040 can be used for the research of oncology and immunology diseases.
|
-
- HY-P1263
-
-
- HY-P1263A
-
-
- HY-B0227
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Ketoprofen
RP-19583
|
COX
|
Metabolic Disease
Inflammation/Immunology
|
Ketoprofen (RP-19583) is a non-steroidal anti-inflammatory agent. Ketoprofen can inhibits the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity.
|
-
- HY-B0227A
-
Ketoprofen (lysinate)
RP-19583 (lysinate)
|
COX
|
Metabolic Disease
Inflammation/Immunology
|
Ketoprofen (RP-19583) lysinate is a non-steroidal anti-inflammatory agent. Ketoprofen lysinate can inhibit the activity of cyclooxygenase with IC50 values of 2 nM (COX-1) and 26 nM (COX-2). which is potential in the research of inflammation, immunology, and metabolic disease such as obesity.
|
-
- HY-78131
-
Ibuprofen
(±)-Ibuprofen
|
COX
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
Ibuprofen ((±)-Ibuprofen) is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen ((±)-Ibuprofen) can be used in the research of pain, swelling, inflammation, infection, immunology, cancers.
|
-
- HY-78131C
-
Ibuprofen sodium
(±)-Ibuprofen sodium
|
COX
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
Ibuprofen ((±)-Ibuprofen) sodium is an orally active, selective COX-1 inhibitor with an IC50 value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers.
|
-
- HY-P9902
-
Pembrolizumab
MK-3475; Lambrolizumab; Keytruda
|
PD-1/PD-L1
|
Cancer
|
Pembrolizumab (MK-3475) is a humanized IgG4 antibody inhibiting the programmed cell death 1 (PD-1) receptor, used in cancer immunotherapy.
|
-
- HY-134911
-
HS-243
|
IRAK
CDK
|
Cancer
Inflammation/Immunology
|
HS-243 is a potent and selective IRAK-4 and IRAK-1 inhibitor, with IC50 values of 20 and 24 nM. HS-243 shows minimal TAK1 (transforming growth factor β-activated kinase 1) inhibition activity, with a IC50 of 0.5 μM. HS-243 shows anti-inflammatory and anticancer activity.
|
-
- HY-101311
-
UPF-523
AIDA
|
mGluR
|
Inflammation/Immunology
|
UPF-523 (AIDA), a rigid (carboxyphenyl) glycine derivative, is a relatively potent and selective antagonist of group I metabotropic glutamate receptors (mGlu1a) with an IC50 of 214 μM. But UPF-523 has no effect on group II (mGlu2), group III (mGlu4) receptors or ionotropic glutamate receptors. UPF-523 has the potential for the research of the acute arthritis.
|
-
- HY-102052
-
DCEBIO
|
Potassium Channel
|
Inflammation/Immunology
|
DCEBIO, a derivative of 1-EBIO, is an extremely potent activator of Cl - secretion in T84 colonic cells. DCEBIO stimulates Cl - secretion via the activation of hIK1 K + channels and the activation of an apical membrane Cl - conductance.
|
-
- HY-118139S1
-
Desmethyl Celecoxib-d4
|
COX
|
Inflammation/Immunology
|
Desmethyl Celecoxib-d4 is the deuterium labeled Desmethyl Celecoxib. Desmethyl Celecoxib (compound 3b) is a selective cyclooxygenase-2 (COX-2) inhibitor (IC50=32 nM) with anti-inflammatory activities. Desmethyl Celecoxib is an analog of Celecoxib and with the optimal yield of 75%.
|
-
- HY-145890
-
-
- HY-17476
-
-
- HY-146479
-
-
- HY-B0482
-
Acemetacin
TVX 1322
|
COX
|
Inflammation/Immunology
|
Acemetacin (TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
|
-
- HY-150553
-
-
- HY-145776
-
ALV1
|
Casein Kinase
Ligands for E3 Ligase
|
Inflammation/Immunology
|
ALV1 is a potent Ikaros and Helios degrader. ALV1 potently reduces the protein abundance of IKZF1-4, CK1α (casein kinase 1α, CSNK1A1) and ribosomal protein RPL4. ALV1 shows similar degradation activity towards IKZF1/2/3. ALV1 induced Helios/CRBN dimerization. ALV1 promoted IL-2 secretion to a great extent.
|
-
- HY-11087
-
-
- HY-W010708S
-
-
- HY-112921
-
-
- HY-N2556
-
Tirucallol
|
Others
|
Inflammation/Immunology
|
Tirucallol, a tetracyclic triterpene, is isolated from Euphorbia lacteal latex. Tirucallol has topical anti-inflammatory effect. Tirucallol can suppress ear edema in the mouse model and inhibit nitrite production in lipopolysaccharide-stimulated macrophages.
|
-
- HY-111269
-
-
- HY-122624
-
MMP13-IN-2
|
MMP
|
Inflammation/Immunology
|
MMP13-IN-2 is a potent, selective and orally active MMP-13 inhibitor. MMP13-IN-2 exhibits excellent potency for MMP-13 (IC50=0.036 nM) and selectivities (greater than 1,500-fold) over MMP-1, 3, 7, 8, 9, 14, and TACE. MMP13-IN-2 has the ability to block the release of collagen from cartilage in vitro. MMP13-IN-2 has the potential for collagenase related disease research.
|
-
- HY-150732
-
IRAK4-IN-18
|
IRAK
|
Inflammation/Immunology
|
IRAK4-IN-18 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 15 nM. IRAK4-IN-18 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-18 can be used for researching arthritis disease.
|
-
- HY-N0136
-
Taxifolin
(+)-Dihydroquercetin; (+)-Taxifolin
|
Autophagy
Tyrosinase
|
Inflammation/Immunology
|
Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
|
-
- HY-107587
-
A-286982
|
Integrin
|
Inflammation/Immunology
|
A-286982 is a potent and allosteric LFA-1/ICAM-1 interaction inhibitor with IC50s of 44 nM and 35 nM in an LFA-1/ICAM-1 binding and LFA-1-mediated cellular adhesion assay, respectively.
|
-
- HY-12836A
-
-
- HY-13568
-
Benoxaprofen
LRCL 3794
|
COX
|
Inflammation/Immunology
|
Benoxaprofen (LRCL 3794) is a potent and long-acting anti-inflammatory and antipyretic compound. Benoxaprofen is a relatively weak inhibitor of cyclooxygenase in in vitro systems, inhibits lipoxygenase in other systems, and inhibits monocyte migration in some animal models of inflammation.
|
-
- HY-N2572
-
Nepetin
6-Methoxyluteolin
|
Others
|
Inflammation/Immunology
|
Nepetin (6-Methoxyluteolin) is a natural flavonoid isolated from Eupatorium ballotaefolium HBK with potent anti-inflammatory activities. Nepetin inhibits IL-6, IL-8 and MCP-1 secretion with IC50 values of 4.43 μM, 3.42 μM and 4.17 μM, respectively in ARPE-19 cells.
|
-
- HY-138139A
-
AXC-715 hydrochloride
T785 hydrochloride
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
AXC-715 (T785) hydrochloride is a TLR7/TLR8 dual agonist, extracted from patent WO2020168017 A1. AXC-715, compound D from WO2020190734A1, can be used for synthesis of antibody-adjuvant immunoconjugates, comprising an antibody construct that binds programmed death-ligand 1 (PD-L1) linked to one or more adjuvants.
|
-
- HY-147908
-
Adenosine receptor inhibitor 2
|
Adenosine Receptor
|
Inflammation/Immunology
|
Adenosine receptor inhibitor 2 (compound 14b) is a potent AR (adenosine receptor) inhibitor. Adenosine receptor inhibitor 2 shows dual affinity toward A1/A2A ARs with higher affinity for the A1- than the A2AAR. Adenosine receptor inhibitor 2 has Ki values of 52.2 nM for the A1AR and 167 nM for the A2AAR.
|
-
- HY-14180
-
PHA 408
|
IKK
|
Inflammation/Immunology
|
PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation.
|
-
- HY-Y0189
-
Methyl Salicylate
Wintergreen oil
|
COX
|
Inflammation/Immunology
|
Methyl Salicylate (Wintergreen oil) is a topical analgesic and anti-inflammatory agent. Also used as a pesticide, a denaturant, a fragrance ingredient, and a flavoring agent in food and tobacco products. A systemic acquired resistance (SAR) signal in tobacco. A topical nonsteroidal anti-inflammatory drug (NSAID). Methyl salicylate lactoside is a COX inhibitor.
|
-
- HY-114181
-
-
- HY-139206
-
-
- HY-B1521
-
Aluminum Hydroxide
|
Others
|
Inflammation/Immunology
|
Aluminum Hydroxide is an orally active main form of aluminum used as adjuvant. Aluminum hydroxide-based adjuvant researches include the repository effect, pro-phagocytic effect, and activation of the pro-inflammatory NLRP3 pathway. Aluminum Hydroxide also acts as adjuvant to compensate low inherent immunogenicity of subunit vaccines.
|
-
- HY-N7576
-
Anemarrhenasaponin Ia
|
Others
|
Inflammation/Immunology
|
Anemarrhenasaponin Ia, isolated from Anemarrhenae rhizome, inhibits N-formyl-methionyl-leucyl-phenylalanine (fMLP)-induced superoxide generation. Anemarrhenasaponin Ia is an useful anti-inflammation reagent.
|
-
- HY-129529
-
6-Hydroxyluteolin 7-glucoside
|
Others
|
Inflammation/Immunology
|
6-Hydroxyluteolin 7-glucoside is a flavonoid from Tanacetum parthenium and T. vulgare. 6-Hydroxyluteolin 7-glucoside inhibits the major pathways of arachidonate metabolism in leukocytes. 6-Hydroxyluteolin 7-glucoside has anti-inflammatory effect.
|
-
- HY-N6895
-
-
- HY-132304
-
CC-90005
|
PKC
|
Inflammation/Immunology
|
CC-90005 is a potent, selective and orally active inhibitor of protein kinase C-θ (PKC-θ), with an IC50 of 8 nM. CC-90005 shows selectivity for PKC-θ over PKC-δ (IC50=4440 nM). CC-90005 can inhibit T cell activation by IL-2 expression.
|
-
- HY-147404
-
-
- HY-N1570
-
-
- HY-16981
-
SB-332235
|
CXCR
|
Inflammation/Immunology
|
SB-332235 is a potent, orally active nonpeptide CXCR2 antagonist, with an IC50 of 7.7 nM. SB-332235 displays 285-fold selectivity for CXCR2 over CXCR1. SB-332235 inhibits acute and chronic models of arthritis in the rabbit. SB-332235 inhibits viability of AML cells.
|
-
- HY-16984
-
GNE-4997
|
Itk
|
Inflammation/Immunology
|
GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a Ki of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.
|
-
- HY-112629
-
-
- HY-139847
-
-
- HY-18166
-
NIBR0213
|
LPL Receptor
|
Inflammation/Immunology
|
NIBR-0213 is a potent and selective S1P1 antagonist with efficacy in experimental autoimmune encephalomyelitis. NIBR-0213 displays potent and comparable potency on human and rat S1P1 (IC50 of 2.0 nM and 2.3 nM, respectively) in GTPγ 35S assays.
|
-
- HY-P1398
-
-
- HY-133159
-
-
- HY-P1111
-
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-120878
-
CXCR2-IN-2
|
CXCR
|
Inflammation/Immunology
|
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
|
-
- HY-18709
-
-
- HY-17357
-
-
- HY-19569A
-
Upadacitinib tartrate tetrahydrate
ABT-494 tartrate tetrahydrate
|
JAK
|
Inflammation/Immunology
|
Upadacitinib (ABT-494) tartrate tetrahydrate is a potent, orally active and selective Janus kinase 1 (JAK1) inhibitor (IC50=43 nM). Upadacitinib tartrate tetrahydrate displays approximately 74 fold selective for JAK1 over JAK2 (200 nM) in cellular assays dependent on specific, relevant cytokines. Upadacitinib tartrate tetrahydrate can be used for several autoimmune disorders research.
|
-
- HY-P1314
-
-
- HY-130440
-
-
- HY-P1076A
-
CALP2 TFA
|
Calcium Channel
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
|
-
- HY-136527
-
BMS-986251
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
BMS-986251 is an orally active and selective RORγt inverse agonist with an EC50 of 12 nM for RORγt GAL4. BMS-986251 inhibits IL-17 with an EC50 of 24 nM in human whole blood assay. BMS-986251 demonstrates robust efficacy in mouse acanthosis and Imiquimod-induced (HY-B0180) models (preclinical models of psoriasis).
|
-
- HY-131259
-
-
- HY-B0890S
-
Zomepirac-d4 sodium salt
|
PGE synthase
|
Inflammation/Immunology
|
Zomepirac-d4 sodium salt is the deuterium labeled Zomepirac sodium salt. Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury.
|
-
- HY-108259
-
HQL-79
|
PGE synthase
|
Inflammation/Immunology
|
HQL-79, a potent, selective and orally active human hematopoietic prostaglandin D synthase (H-PGDS) inhibitor, highly selectively inhibits the synthesis of PGD2, and acts as an anti-allergic agent, with a Kd of 0.8 μM and an IC50 of 6 μM. Shows no obvious effect on COX-1, COX-2, m-PGES, or L-PGDS.
|
-
- HY-U00444
-
-
- HY-D1056
-
Lipopolysaccharides
LPS
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Lipopolysaccharides (LPS) is an endotoxin derived from the outer leaflet of the outer membrane of Gram-negative bacteria. Lipopolysaccharides consists of an antigen O-specific chain, a core oligosaccharide and lipid A. Lipopolysaccharides is a pathogenic associated molecular pattern (PAMP) that activates the immune system. Lipopolysaccharides activates TLR-4 on immune cells. This product is derived from Escherichia coli O55:B5.
|
-
- HY-N2406
-
-
- HY-111457A
-
BAY-678
|
Elastase
|
Inflammation/Immunology
|
BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
|
-
- HY-136301
-
Acid secretion-IN-1
|
Others
|
Inflammation/Immunology
|
Acid secretion-IN-1 is a polycyclic compound extracted from patent WO2018024188A1, Compound Example 17.4. Acid secretion-IN-1 is synthesized and used in the IDO inhibitor synthetic experiment.
|
-
- HY-138067
-
SSAA09E2
|
SARS-CoV
|
Inflammation/Immunology
|
SSAA09E2 is an inhibitor of SARS-CoV (Severe acute respiratory syndrome-Coronavirus) replication, acting by blocking early interactions of SARS-S with the receptor for SARS-CoV, Angiotensin Converting Enzyme-2 (ACE2) .
|
-
- HY-I0501
-
2'-Aminoacetophenone
|
Bacterial
|
Inflammation/Immunology
|
2'-Aminoacetophenone is an aromatic compound containing a ketone substituted by one alkyl group, and a phenyl group. 2'-Aminoacetophenone can be used as a breath biomarker for the detection of Ps. Aeruginosa infections in the cystic fibrosis lung.
|
-
- HY-147642
-
-
- HY-15879
-
-
- HY-139025
-
-
- HY-N0875
-
-
- HY-107563
-
ROS 234
|
Histamine Receptor
|
Inflammation/Immunology
|
ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access.
|
-
- HY-W281862
-
-
- HY-N0101
-
-
- HY-128523
-
-
- HY-N0759
-
-
- HY-N6073
-
Soyasapogenol A
|
Apoptosis
|
Inflammation/Immunology
|
Soyasapogenol A, a triterpene compound, isolated from the roots of Abrus cantoniensis. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
|
-
- HY-N4280
-
-
- HY-100640
-
-
- HY-N2516
-
-
- HY-145261
-
hDHODH-IN-8
|
Lactate Dehydrogenase
|
Inflammation/Immunology
|
hDHODH-IN-8 is a potent inhibitor of human dihydroorotate dehydrogenase (hDHODH) with an IC50 of 16 nM. hDHODH-IN-8 has potent antiproliferative activity and excellent aqueous solubility. hDHODH-IN-8 has the potential for the research of tumor disease, especially lymphoma.
|
-
- HY-100977
-
-
- HY-147077
-
-
- HY-112558
-
-
- HY-131104S
-
-
- HY-P1310
-
-
- HY-B0926A
-
Sodium diatrizoate
Diatrizoic acid sodium salt; Sodium amidotrizoate
|
Apoptosis
|
Inflammation/Immunology
|
Sodium diatrizoate (Diatrizoic acid sodium salt) is an iodinated radiocontrast agent and has the potential for radiographic imaging of the airways. Sodium diatrizoate induces mitochondrial turnover and oxidative stress, and activating apoptosis by dysregulating calcium.
|
-
- HY-N3595S
-
Cleomiscosin A-d3
|
TNF Receptor
|
Inflammation/Immunology
|
Cleomiscosin A-d3 is the deuterium labeled Cleomiscosin A. Cleomiscosin A is a coumarino-lignoid from branch of Macaranga adenantha. Cleomiscosin A is active against TNF-alpha secretion of the mouse peritoneal macrophages.
|
-
- HY-B1203S
-
-
- HY-N4150
-
Quercetagitrin
Quercetagetin-7-O-glucoside
|
Others
|
Inflammation/Immunology
|
Quercetagitrin (Quercetagetin-7-O-glucoside), isolated from the flowers of the African Marigold (Tagetes erecta), has anti-inflammatory activity.
|
-
- HY-113919
-
Nothofagin
|
Calcium Channel
|
Inflammation/Immunology
|
Nothofagin, a dihydrochalcone, is isolated from rooibos (Aspalathus linearis). Nothofagin downregulates NF-κB translocation through blocking calcium influx. Nothofagin has antioxidant activity and ameliorates various inflammatory responses such as the septic response and vascular inflammation.
|
-
- HY-114368A
-
-
- HY-119580
-
Leucocyanidin
|
Others
|
Inflammation/Immunology
|
Leucocyanidin is an active anti-ulcerogenic ingredient was extracted from unripe plantain banana. Leucocyanidin demonstrates a significant protective effect against Aspirin-induced erosions in rat models.
|
-
- HY-N5054
-
5,7-Dimethoxyflavanone
|
TNF Receptor
|
Inflammation/Immunology
|
5,7-Dimethoxyflavanone shows potent antimutagenic activity against MeIQ mutagenesis in Ames test using the S. typhimurium TA100 and TA98 strains. And 5,7-Dimethoxyflavanone significantly and dose-dependently inhibits the inflammatory mediato
|
-
- HY-N7378A
-
N-Hydroxypipecolic acid potassium
1-Hydroxy-2-piperidinecarboxylic acid potassium; NHP potassium
|
Others
|
Inflammation/Immunology
|
N-Hydroxypipecolic acid potassium (1-Hydroxy-2-piperidinecarboxylic acid potassium), a plant metabolite and a systemic acquired resistance (SAR) regulator, orchestrates SAR establishment in concert with the immune signal salicylic acid. N-Hydroxypipecolic acid potassium accumulates systemically in the plant foliage in response to pathogen attack. N-Hydroxypipecolic acid potassium induces SAR to bacterial and oomycete infection.
|
-
- HY-125415
-
PF-4693627
|
PGE synthase
|
Inflammation/Immunology
|
PF-4693627 is a potent, selective and orally bioavailable microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50=3 nM) for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).
|
-
- HY-145922
-
-
- HY-N0444
-
-
- HY-N2035
-
-
- HY-N7937
-
-
- HY-N0774
-
Isofraxidin
|
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells. Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation.
|
-
- HY-19837
-
-
- HY-12290
-
Arg-Gly-Asp-Ser
RGDS peptide; Fibronectin tetrapeptide
|
Integrin
|
Inflammation/Immunology
|
Arg-Gly-Asp-Ser is an integrin binding sequence that inhibits integrin receptor function. Arg-Gly-Asp-Ser directly and specifically bind pro-caspase-8, pro-caspase-9 and pro-caspase-3, while it does not bind pro-caspase-1.
|
-
- HY-N2358
-
-
- HY-18978
-
GR79236
|
Adenosine Receptor
|
Inflammation/Immunology
|
GR79236 is a highly potent, selective and orally active adenosine A1 receptor agonist with a Kis of 3.1 nM and 1300 nM for A1 and A2 receptors, respectively. GR79236 has anti-nociceptive and anti-inflammatory actions.
|
-
- HY-N0469S
-
-
- HY-131249
-
MK2-IN-3
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
MK2-IN-3 is a potent and selective inhibitor of MAPKAP-K2 (MK-2), with an IC50 of 8.5 nM. MK2-IN-3 shows selectivity for MK-2 over MK-3, MK-5, ERK2, MNK1, p38a (IC50s=0.21, 0.081, 3.44, 5.7, and >100 μM, respectively) and MSK1, MSK2, CDK2, JNK2, IKK2 (IC50s>200 μM). MK2-IN-3 can reduce TNFα production in both U937 cells and in vivo.
|
-
- HY-N4099
-
-
- HY-17350
-
-
- HY-N0348
-
-
- HY-N6692
-
Diacetoxyscirpenol
|
Others
|
Inflammation/Immunology
|
Diacetoxyscirpenol (DAS) is a trichothecene mycotoxin, a secondary metabolite product of fungi. Diacetoxyscirpenol (DAS) consumption induces haematological disorders (neutropenia, aplastic anemia) in human and animals.
|
-
- HY-17042AS
-
Cetirizine D4 dihydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
|
Cetirizine D4 dihydrochloride is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
|
-
- HY-107563A
-
ROS 234 dioxalate
|
Histamine Receptor
|
Inflammation/Immunology
|
ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access.
|
-
- HY-B1042
-
Oxolamine citrate
SKF-9976 citrate; AF-438 citrate
|
Others
|
Inflammation/Immunology
|
Oxolamine citrate (SKF-9976 citrate) is a cough suppressant that can be used for the research of respiratory tract diseases. Oxolamine citrate also exhibits anti-inflammatory effect.
|
-
- HY-N0120
-
(E/Z)-Polydatin
(E/Z)-Piceid
|
Others
|
Inflammation/Immunology
|
(E/Z)-Polydatin ((E/Z)-Piceid) is a monocrystalline compound originally isolated from the root and rhizome of Polygonum cuspidatum. (E/Z)-Polydatin has anti-platelet aggregation, anti-oxidative action of low-density lipoprotein (LDL), cardioprotective activity, anti-inflammatory and immune-regulating functions.
|
-
- HY-114771
-
-
- HY-145640
-
AZD4721
RIST4721
|
CXCR
|
Inflammation/Immunology
|
AZD4721 (RIST4721) is the potent and orally active antagonist of acidic CXC chemokine receptor 2 (CXCR2). AZD4721 has the potential for the research of inflammatory disease.
|
-
- HY-101868
-
-
- HY-109170
-
Eliapixant
BAY 1817080
|
P2X Receptor
|
Inflammation/Immunology
|
Eliapixant (BAY 1817080) is a potent and selective antagonist of P2X3 receptor, with an IC50 of 8 nM. Eliapixant can be used for the research of refractory chronic cough.
|
-
- HY-117726
-
-
- HY-135731
-
4-Methylamino antipyrine
|
COX
Drug Metabolite
|
Inflammation/Immunology
|
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.
|
-
- HY-116442
-
Azapropazone
|
Others
|
Inflammation/Immunology
|
Azapropazone is a nonsteroidal anti-inflammatory drug (NSAID). Azapropazone can be used for the research of rheumatoid arthritis and other rheumatoid conditions.
|
-
- HY-N4231
-
-
- HY-N8803
-
-
- HY-W008956
-
Myoseverin
|
Microtubule/Tubulin
|
Inflammation/Immunology
|
Myoseverina, a microtubule-binding molecule, induces the reversible fission of multinucleated myotubes into mononucleated fragments. Myoseverina affects the expression of a variety of growth factor, immunomodulatory, extracellular matrix-remodeling, and stress response genes, consistent with the activation of pathways involved in wound healing and tissue regeneration.
|
-
- HY-112582
-
-
- HY-121851
-
Revaprazan
SB 641257
|
Proton Pump
|
Inflammation/Immunology
|
Revaprazan (SB 641257) is a reversible proton pump inhibitor with significant anti-inflammatory effects. Revaprazan can be used for chronic gastric inflammation research.
|
-
- HY-100639
-
-
- HY-D0861A
-
EGTA tetrasodium
|
Others
|
Inflammation/Immunology
|
EGTA tetrasodium is a specific calcium ion chelator. EGTA tetrasodium has an apparent calcium dissociation constant (Kd) of 60.5 nM at physiological pH (7.4) and has very high specificity for Ca 2+ over Mg 2+ (Mg 2+ Kd 1-10 mM). EGTA tetrasodium significantly inhibits the substrate adherence capacity of inflammatory macrophages.
|
-
- HY-13660
-
-
- HY-136393
-
IKK-IN-4
|
IKK
|
Inflammation/Immunology
|
IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively.
|
-
- HY-145195
-
-
- HY-146662
-
HPGDS inhibitor 3
|
PGE synthase
|
Inflammation/Immunology
|
HPGDS inhibitor 3 is an orally active and highly potent peripherally restricted hematopoietic prostaglandin D synthase (H-PGDS) inhibitor with IC50 value of 9.4 nM and EC50 of 42 nM, respectively. HPGDS inhibitor 3 exhibits good selectivity, good pharmacokinetic parameters in mouse, rat, and dog, and no CNS toxicity. HPGDS inhibitor 3 has anti-inflammatory activity.
|
-
- HY-W011471S
-
-
- HY-W011085
-
CP-471474
|
MMP
|
Inflammation/Immunology
|
CP-471474 is an orally active and pan MMP inhibitor, with IC50 values of 1170 nM (MMP-1), 0.7 nM (MMP-2), 16 nM (MMP-3), 13 nM (MMP-9) and 0.9 nM (MMP-13), respectively.
|
-
- HY-P1860
-
-
- HY-145960
-
-
- HY-128410
-
-
- HY-N4146
-
-
- HY-144683
-
-
- HY-N2266
-
-
- HY-115620
-
AQX-016A
|
Phosphatase
PI3K
TNF Receptor
|
Inflammation/Immunology
|
AQX-016A is an orally active and potent SHIP1 agonist. AQX-016A can activate recombinant SHIP1 enzyme in vitro and stimulate SHIP1 activity. AQX-016A also can inhibit the PI3K pathway and TNFa production, can be useful for various inflammatory diseases research.
|
-
- HY-143456
-
Anti-inflammatory agent 18
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 18 (compound 3b) shows NO inhibitory activity, with an IC50 of 15.94 μM. Anti-inflammatory agent 18 inhibits HMGB1-induced later inflammation. Anti-inflammatory agent 18 can be used for the research of later inflammation diseases such as coronavirus diseases (COVID-19) and sepsis, etc.
|
-
- HY-16903
-
PKC-IN-1
|
PKC
|
Inflammation/Immunology
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-17635
-
-
- HY-109182
-
-
- HY-139557
-
-
- HY-125801
-
3-Oxo-5β-cholanoic acid
Dehydrolithocholic acid; 3-oxoLCA
|
ROR
|
Inflammation/Immunology
|
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
|
-
- HY-N4125
-
-
- HY-100754B
-
-
- HY-P1844A
-
Chemerin-9 (149-157) (TFA)
|
Akt
ERK
Reactive Oxygen Species
Amyloid-β
|
Inflammation/Immunology
|
Chemerin-9 (149-157) TFA is a potent agonist of chemokine-like receptor 1 (CMKLR1) . Chemerin-9 (149-157) TFA has anti-inflammatory activity. Chemerin-9 (149-157) TFA stimulates phosphorylation of Akt and ERK as well as ROS production. Chemerin-9 (149-157) TFA ameliorates Aβ1-42-induced memory impairmen. Chemerin-9 (149-157) TFA regulates immune responses, adipocyte differentiation, and glucose metabolism.
|
-
- HY-N1098
-
Velutin
|
Others
|
Inflammation/Immunology
|
Velutin is an aglycone extracted from Korean Mistletoe, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway.
|
-
- HY-17477
-
Guacetisal
|
Others
|
Inflammation/Immunology
|
Guacetisal is obtained from the esterification of acetylsalicylic acid with guaiacol which has the potential for chronic bronchitis treatment extracted from patent CN 106866420 A.
|
-
- HY-U00359
-
-
- HY-100139
-
-
- HY-146561
-
S-HP210
|
Glucocorticoid Receptor
NF-κB
|
Inflammation/Immunology
|
S-HP210 is a potent and selective glucocorticoid receptor (GR) with an IC50 value of 1.92 μM for NF-κB transrepression (TR). S-HP210 represses the LPS-induced transcription of a variety of proinflammatory genes such as IL-1β, IL-6 and COX-2. S-HP210 is nontoxic at effective doses against mouse fibroblasts 3T3 cells.
|
-
- HY-138300
-
-
- HY-120934
-
C25-140
|
TNF Receptor
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.
|
-
- HY-N0613
-
Sauchinone
|
NF-κB
|
Inflammation/Immunology
|
Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
|
-
- HY-N1981
-
-
- HY-13463A
-
Avatrombopag maleate
AKR-501 maleate; E5501 maleate; YM477 maleate
|
Thrombopoietin Receptor
|
Inflammation/Immunology
|
Avatrombopag maleate (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag maleate mimics the biological activities of TPO. Avatrombopag maleate increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag maleate is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
|
-
- HY-N2286
-
-
- HY-112553
-
HZ52
|
Lipoxygenase
|
Inflammation/Immunology
|
HZ52 is a potent, reversible 5-lipoxygenase inhibitor, blocking leukotriene synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes.
|
-
- HY-W050088
-
Isoxepac
HP 549
|
Others
|
Inflammation/Immunology
|
Isoxepac (HP 549) is a nonsteroidal anti-inflammatory agent (NSAID) with anti-inflammatory, analgesic and antipyretic activity. Isoxepac has been studied in rat, rabbit, dog, rhesus monkey, etc.
|
-
- HY-12341
-
ML355
|
Lipoxygenase
|
Inflammation/Immunology
|
ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.
|
-
- HY-N0516
-
Casticin
Vitexicarpin
|
STAT
|
Inflammation/Immunology
|
Casticin is a methyoxylated flavonol isolated from Viticis Fructus, with antimitotic and anti-inflammatory effect. Casticin inhibits the activation of STAT3.
|
-
- HY-N0608B
-
-
- HY-118773
-
MreB Perturbing Compound A22 hydrochloride
A22 hydrochloride
|
Bacterial
|
Inflammation/Immunology
|
MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
|
-
- HY-145245
-
-
- HY-107627
-
MCL0020
|
Melanocortin Receptor
|
Inflammation/Immunology
|
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake.
|
-
- HY-15322
-
PRT062607
P505-15; PRT-2607; BIIB-057
|
Syk
|
Inflammation/Immunology
|
PRT062607(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.
|
-
- HY-136179
-
ZAP-180013
|
Tyrosinase
|
Inflammation/Immunology
|
ZAP-180013 is a zeta-chain-associated protein kinase 70 (ZAP-70) inhibitor with an IC50 of 1.8 μM. ZAP-180013 inhibits the interaction of ZAP-70 SH2 domain with immunoreceptor tyrosine-based activation motif (ITAMs).
|
-
- HY-141843
-
-
- HY-18787
-
-
- HY-P2478
-
-
- HY-147712
-
PKC-IN-4
|
PKC
|
Inflammation/Immunology
|
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature.
|
-
- HY-N7018
-
20-Hydroxyganoderic Acid G
|
Others
|
Inflammation/Immunology
|
20-Hydroxyganoderic Acid G is a lanostane triterpenoid obtained from the EtOH extract of fruiting bodies of the Ganoderma curtisii. 20-Hydroxyganoderic Acid G inhibits BV-2 microglia cells activated by LPS with an IC50 of 21.33 μM. 20-Hydroxyganoderic Acid G has therapeutic potential in the drug discovery of nerve inflammation diseases associated with microglia activated by LPS.
|
-
- HY-P1717B
-
AMY-101 acetate
Cp40 acetate
|
Complement System
SARS-CoV
|
Inflammation/Immunology
|
AMY-101 acetate (Cp40 acetate), a peptidic inhibitor of the central complement component C3 (KD = 0.5 nM), inhibits naturally occurring periodontitis in non-human primates (NHPs). AMY-101 acetate (Cp40 acetate) exhibits a favorable anti-inflammatory activity in models with COVID-19 severe pneumonia with systemic hyper inflammation.
|
-
- HY-119447S
-
Mavacoxib-d4
|
COX
|
Inflammation/Immunology
|
Mavacoxib-d4 is the deuterium labeled Mavacoxib. Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.
|
-
- HY-111767
-
BAY-545
|
Adenosine Receptor
|
Inflammation/Immunology
|
BAY-545 is a potent and selective A2B adenosine receptor antagonist, with an IC50 of 59 nM. BAY-545 also exhibits IC50s of 66, 400, 280 nM for human, mouse, rat A2B adenosine receptor in cells, respectively, and a Ki of 97 nM for human A2B adenosine receptor, with more selectivity over A1, A2A, and A3 adenosine receptor.
|
-
- HY-138281
-
Complement factor D-IN-2
|
Complement System
|
Inflammation/Immunology
|
Complement factor D-IN-2 is an inhibitor of complement factor D extracted from patent WO2015130838A1, compound 190. Complement factor D-IN-2 targets factor D and inhibits the complement cascade at an early and essential point in the alternative complement pathway. Complement factor D-IN-2 can be used for the research of autoimmune diseases.
|
-
- HY-146068
-
-
- HY-121046S
-
Flunixin-d3
|
COX
|
Inflammation/Immunology
|
Flunixin-d3 is the deuterium labeled Flunixin. Flunixin Meglumine is a potent inhibitor of COX used as analgesic agent with anti-inflammatory and antipyretic activity.
|
-
- HY-101023
-
-
- HY-A0178S
-
-
- HY-N1072
-
Wilforgine
|
Others
|
Inflammation/Immunology
|
Wilforgine is a bioactive sesquiterpene alkaloid in Tripterygium wilfordii Hook. F. Wilforgine can induce microstructural and ultrastructural changes in the muscles of Mythimna separata larvae, and the sites of action are proposed to be calcium receptors or channels in the muscular system.
|
-
- HY-129997
-
Luteolinidin chloride
|
Others
|
Inflammation/Immunology
|
Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
|
-
- HY-125538
-
-
- HY-N6607
-
Tryptanthrin
|
Others
|
Inflammation/Immunology
|
Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin inhibits LT formation in human whole blood (IC50 = 10 µM) and reduces LTB4 levels in the rat pleurisy model.
|
-
- HY-112126
-
KRN5
|
Others
|
Inflammation/Immunology
|
KRN5, a derivative of KRN2, is an oral active Nuclear factor of activated T cells 5 (NFAT5) suppressor, with an IC50 of 750 nM. KRN5 has potential to treat NFAT5-mediated Chronic Arthritis.
|
-
- HY-109085
-
Difamilast
OPA-15406
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD).
|
-
- HY-150745
-
ODN 24987
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
ODN 24987 is a Guanine-modified inhibitory oligonucleotides (ODN), targeting TLR9. ODN 24987 can inhibit IL-6 and IFN-α release. ODN 24987 can be used for research immune disorders. ODN 24987 sequence: 5’-C-C-T-G-G-C-c7G-G-G-G-3’.
|
-
- HY-B1015
-
Etosalamide
Ethosalamide
|
Others
|
Inflammation/Immunology
|
Etosalamide (Ethosalamide) is an antipyretic and analgesic agent. Etosalamide has anti-inflammatory activity and can be used for allergic disease research.
|
-
- HY-N0731
-
-
- HY-15874A
-
Fiboflapon sodium
GSK2190915 sodium salt; AM-803 sodium
|
FLAP
Leukotriene Receptor
|
Inflammation/Immunology
|
Fiboflapon sodium (GSK2190915; AM-803) is a potent and orally bioavailable 5-lipoxygenase-activating protein (FLAP) inhibitor with a potency of 2.9 nM in FLAP binding, an IC50 of 76 nM for inhibition of LTB4 in human blood.
|
-
- HY-143718
-
JAK3/BTK-IN-3
|
JAK
Btk
|
Inflammation/Immunology
|
JAK3/BTK-IN-3 is a potent inhibitor of JAK3/BTK. BTK and JAK3 are two important targets for autoimmune diseases. Simultaneous inhibition of the BTK/JAK3 signalling pathway exhibits synergistic effects. JAK3/BTK-IN-3 has the potential for the research of JAK3 kinase and/or BTK-related diseases (extracted from patent WO2021147952A1, compound 009)
|
-
- HY-126154
-
L48H37
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
L48H37 is an analog of Curcumin (HY-N0005) with improved chemical stability. L48H37 is a potent and specific myeloid differentiation protein 2 (MD2) inhibitor and inhibits the interaction and signaling transduction of LPS-TLR4/MD2. L48H37 is used for the research of sepsis or lung injury treatment.
|
-
- HY-101098
-
-
- HY-N7962
-
-
- HY-14670
-
Firocoxib
ML 1785713
|
COX
|
Inflammation/Immunology
|
Firocoxib (ML 1785713) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 0.13 μM. Firocoxib shows 58-fold more selective for COX-2 than COX-1 (IC50 of 7.5 μM). Firocoxib has anti-inflammatory effects.
|
-
- HY-116282D
-
-
- HY-P0154
-
Epsilon-V1-2
ε-V1-2; EAVSLKPT
|
PKC
|
Inflammation/Immunology
|
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
|
-
- HY-N8200
-
-
- HY-107781
-
-
- HY-N6878
-
Cauloside D
|
Others
|
Inflammation/Immunology
|
Cauloside D is a triterpene glycoside isolated from Caulophyllum robustum Max. Cauloside D exerts anti-inflammatory effects through the inhibition of expression of iNOS and proinflammatory cytokines.
|
-
- HY-111021
-
ASP-4058
|
LPL Receptor
|
Inflammation/Immunology
|
ASP-4058 is a next-generation, selective and oral bioactive agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
|
-
- HY-145351
-
-
- HY-145801
-
XT2
|
Others
|
Inflammation/Immunology
|
XT2 is a potent, orally active, and selective inhibitor of NF-κB-inducing kinase (NIK) with an IC50 of 9.1 nM. XT2 suppresses CCl4-induced upregulation of ALT, a key biomarker of acute liver injury. XT2 also decreases immune cell infiltration into the injured liver tissue. XT2 has the potential for the research of liver inflammatory diseases.
|
-
- HY-12326A
-
c-di-AMP disodium
Cyclic diadenylate disodium; Cyclic-di-AMP disodium
|
STING
Bacterial
Endogenous Metabolite
|
Inflammation/Immunology
|
c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
|
-
- HY-12885C
-
ADU-S100 enantiomer ammonium salt
MIW815 enantiomer ammonium salt; ML RR-S2 CDA enantiomer ammonium salt
|
Others
|
Inflammation/Immunology
|
ADU-S100 enantiomer ammonium salt (MIW815 enantiomer ammonium salt) is the less active enantiomer of ADU-S100. ADU-S100 is an activator of stimulator of interferon genes (STING).
|
-
- HY-N7656
-
5,7,8-Trimethoxyflavone
Norwogonin 5,7,8-trimethyl ether
|
Others
|
Inflammation/Immunology
|
5,7,8-Trimethoxyflavone (Norwogonin 5,7,8-trimethyl ether), isolated from Andrographis echioides, inhibits NO with an IC50 of 39.1 μM. 5,7,8-Trimethoxyflavone has anti-inflammatory activity.
|
-
- HY-N7012
-
7,3',4'-Tri-O-methylluteolin
5-Hydroxy-3',4',7-trimethoxyflavone
|
TNF Receptor
Interleukin Related
COX
|
Inflammation/Immunology
|
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone), a flavonoid compound, possesses potent anti-inflammatory effects in LPS-induced macrophage cell line mediated by inhibition of release of inflammatory mediators, NO, PGE2, and pro-inflammatory cytokines. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2.
|
-
- HY-P1740
-
RGD peptide (GRGDNP)
|
Integrin
Apoptosis
|
Inflammation/Immunology
|
RGD peptide (GRGDNP) acts as an inhibitor of integrin-ligand interactions and plays an important role in cell adhesion, migration, growth, and differentiation. RGD peptide (GRGDNP) promote apoptosis through activation of conformation changes that enhance pro-caspase-3 activation and autoprocessing.
|
-
- HY-10037
-
Quiflapon
MK-591
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
Quiflapon (MK-591) is a selective and specific 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.6 nM in a FLAP binding assay. Quiflapon is also a potent and orally active Leukotriene biosynthesis (LT) inhibitor, shows IC50 values of 3.1 and 6.1 nM in intact human and elicited rat PMNLs, respectively. Quiflapon induces cell apoptosis.
|
-
- HY-112907
-
-
- HY-18673
-
PROTO-1
|
Others
|
Inflammation/Immunology
|
PROTO-1 shows significant protection of hair cells, with HC50(concentration that would produce 50% hair cell survival) of 1 μM-10 μM (1 μM≤HC50≤10 μM).
|
-
- HY-131952
-
-
- HY-P1052
-
Myelin Basic Protein(87-99)
|
Others
|
Inflammation/Immunology
|
Myelin Basic Protein(87-99) is an encephalitogenic peptide that induces basic protein-specific T cell proliferation. Myelin Basic Protein(87-99) causes a Th1 polarization in peripheral blood mononuclear cells with is implicated of multiple sclerosis (MS).
|
-
- HY-107427
-
PF-3644022
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
|
-
- HY-P2294
-
pm26TGF-β1 peptide
|
TGF-β Receptor
|
Inflammation/Immunology
|
pm26TGF-β1 peptide is a peptide that mimics a portion of the human TGF-β1 molecule. pm26TGF-β1 peptide shows high affinity for the TGF-β1 receptor. pm26TGF-β1 peptide displays potent anti-inflammatory properties and does not exhibit neutrophils’ chemoattraction.
|
-
- HY-114419
-
Zetomipzomib
KZR-616
|
Proteasome
|
Inflammation/Immunology
|
Zetomipzomib (KZR-616), a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. Zetomipzomib has the potential for the research of multiple autoimmune diseases.
|
-
- HY-30235A
-
-
- HY-109069
-
-
- HY-109151
-
Milategrast
E6007
|
Others
|
Inflammation/Immunology
|
Milategrast is useful as cell adhesion inhibitor or cell infiltration inhibitor. Milategrast in vitro inhibites the adhesion of Jurkat cells to human fibronectin with an IC50 of <5 μM.
|
-
- HY-P3450
-
-
- HY-N3524
-
-
- HY-15455S1
-
Roflumilast-d4 N-Oxide
|
Phosphodiesterase (PDE)
RSV
|
Inflammation/Immunology
|
Roflumilast-d4 N-Oxide is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
|
-
- HY-N0919
-
-
- HY-116374
-
-
- HY-U00161
-
-
- HY-145870
-
Anti-inflammatory agent 13
|
Others
|
Inflammation/Immunology
|
Anti-inflammatory agent 13 (Compound 3) is a pentacyclic triterpene compound. Anti-inflammatory agent 13 exhibits a considerable inhibitory effect on inflammation models. Anti-inflammatory agent 13 has the potential for the research of either DAMPs or PAMPs triggered inflammation.
|
-
- HY-P1081
-
-
- HY-131340
-
LASSBio-1632
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
LASSBio-1632 is a new anti-asthmatic lead candidate associated with selective inhibition of PDE4A and PDE4D isoenzymes and blockade of airway hyper-reactivity (AHR) and TNF-α production in the lung tissue. LASSBio-1632 (7j) displays high experimental BBB permeability across BBB through passive diffusion.
|
-
- HY-103186
-
-
- HY-142920
-
-
- HY-113331
-
-
- HY-U00318
-
JAK-IN-11
|
JAK
|
Inflammation/Immunology
|
JAK-IN-11 is a potent and selective JAK inhibitor extracted from patent WO2012122452A1, Compound II, has the potential for the skin disorders (such as cutaneous lupus) treatment.
|
-
- HY-N0508
-
-
- HY-N2144
-
-
- HY-100831
-
YM-58483
BTP2
|
CRAC Channel
|
Inflammation/Immunology
|
YM-58483 (BTP2) is the first selective and potent inhibitor of CRAC channels and subsequent Ca 2+ signals. YM-584832 is a blocker of store-operated Ca 2+ entry (SOCE).
|
-
- HY-128831
-
-
- HY-17606
-
Cenerimod
ACT-334441
|
LPL Receptor
|
Inflammation/Immunology
|
Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36‐fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous.
|
-
- HY-N1120
-
Triptoquinone B
(+)-Triptoquinone B
|
Interleukin Related
|
Inflammation/Immunology
|
Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1 inhibitor. Triptoquinone B shows potent inhibitory activities against interleukin 1α and β releases for human peripheral mononuclear cells.
|
-
- HY-119101
-
AZD-5672
|
CCR
Potassium Channel
P-glycoprotein
|
Inflammation/Immunology
|
AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis.
|
-
- HY-144619
-
TLR7/8 antagonist 2
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
TLR7/8 antagonist 2 (Compound 15) is a potent and orally active agonist of TLR7/8 with IC50s of 4.9 and 0.6 nM, respectively. Inappropriate activation of TLR7 and TLR8 is linked to several autoimmune diseases, such as lupus erythematosus. TLR7/8 antagonist 2 has the potential for the research of autoimmune diseases.
|
-
- HY-N0683A
-
-
- HY-115967
-
COX-1/2-IN-2
|
COX
|
Inflammation/Immunology
|
COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 9.7 ± 0.09 µM and 4.6 ± 1.45 µM, respectively.
|
-
- HY-134753
-
Teriflunomide impurity 3
4-Amino-N-(4-trifluoromethylphenyl)benzamide
|
COX
|
Inflammation/Immunology
|
Teriflunomide impurity 3 (4-Amino-N-(4-trifluoromethylphenyl)benzamide) is a selective COX-1 inhibitor with an IC50 of 30 µM. Teriflunomide impurity 3 is less active against COX-2 (IC50>100 µM).
|
-
- HY-17358S
-
Loteprednol Etabonate D5
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
Loteprednol Etabonate D5 is a deuterium labeled Loteprednol etabonate. Loteprednol etabonate (LE) is an orally active "soft" steroid belonging to a unique class of glucocorticoids. Loteprednol etabonate (LE) exhibits anti-inflammatory activity and has been used in optometry and ophthalmology.
|
-
- HY-112457
-
MK2-IN-3 hydrate
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
MK2-IN-3 hydrate (compound 16) is an orally active, selective, and ATP-competitive MAPKAP-K2 (MK-2) inhibitor with an IC50 of 0.85 nM.MK2-IN-3 hydrate is exceptional selectivity against MK-3 (IC50=0.21 μM), MK-5 (IC50=0.081 μM), ERK2 (IC50=3.44 μM), MNK1(IC50=5.7 μM) as well as CDK2, JNK2, IKK2, MSK1, and MSK2.
|
-
- HY-115732
-
PKA-IN-1
|
PKA
|
Inflammation/Immunology
|
PKA-IN-1 is a potent and selective cyclic AMP-dependent protein kinase (PKA) catalytic subunit (cAK) inhibitor with an IC50 of 0.03 μM.
|
-
- HY-109590S2
-
-
- HY-N6864
-
Isovanillic acid
3-Hydroxy-4-methoxybenzoic acid
|
Others
|
Inflammation/Immunology
|
Isovanillic acid (3-Hydroxy-4-methoxybenzoic acid) is a phenolic acid isolated from isolated from S. frutescens, with Anti-inflammatory activity.
|
-
- HY-B1053
-
-
- HY-50175A
-
-
- HY-122700
-
Factor D inhibitor 6
|
Complement System
|
Inflammation/Immunology
|
Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases.
|
-
- HY-138936
-
SSK1
|
p38 MAPK
Apoptosis
|
Inflammation/Immunology
|
SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted prodrug attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of apoptosis.
|
-
- HY-113972
-
-
- HY-107013
-
-
- HY-B1221
-
Flufenamic acid
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca 2+ channels, modulating non-selective cation channels (NSC), activating K + channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-115913
-
PDE4-IN-6
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects.
|
-
- HY-11059
-
sPLA2 inhibitor 1
|
Phospholipase
|
Inflammation/Immunology
|
sPLA2 inhibitor 1, a D-tyrosine derivative, is an orally active, potent secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 29 nM for human nonpancreatic secretory PLA2 isoform IIa (hnpsPLA2-IIa). sPLA2 inhibitor 1 has anti-inflammatory activity.
|
-
- HY-123967
-
RNF5 inhibitor inh-02
|
Others
|
Inflammation/Immunology
|
RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research.
|
-
- HY-137455
-
-
- HY-13827
-
JAK-IN-1
|
JAK
|
Inflammation/Immunology
|
JAK-IN-1 is a JAK1/2/3 inhibitor with IC50s of 0.26, 0.8 and 3.2 nM, respectively. JAK-IN-1 shows improved selectivity for JAK3 over JAK1.
|
-
- HY-143727
-
RIPK1-IN-9
|
RIP kinase
|
Inflammation/Immunology
|
RIPK1-IN-9 (example 45), a dihydronaphthyridone compound, is a potent and selective RIPK1 inhibitor. RIPK1-IN-9 inhibits U937 cell (IC50=2 nM) and L929 cell (IC50=1.3 nM).
|
-
- HY-N0804
-
Narirutin
|
Bacterial
|
Inflammation/Immunology
|
Narirutin, one of the active constituents isolated from Citrus unshiu, has antioxidant and anti-inflammatory activities. Narirutin is a shikimate kinase inhibitor with anti-tubercular potency.
|
-
- HY-113827
-
THPN
|
Others
|
Inflammation/Immunology
|
THPN is a potent Nur77 agonist. THPN specifically binds the LBD of Nur77 (TR3) but not that of retinoic acid receptor α and PPARγ with a Kd of 270 nM. THPN leads to Nur77 translocation to the mitochondria to induce autophagic cell death in melanoma.
|
-
- HY-17481
-
-
- HY-116814
-
ML401
|
EBI2/GPR183
|
Inflammation/Immunology
|
ML401, a potent chemical probe, selectively antagonizes EBI2 (also known as GPR183) with an IC50 of 1.03 nM. ML401 displays activity in a chemotaxis assay (IC50=6.24 nM). ML401 shows good stability and no toxicity.
|
-
- HY-145192
-
-
- HY-N5080
-
-
- HY-B0580S
-
Ketorolac-d5
|
COX
|
Inflammation/Immunology
|
Ketorolac D5 is a deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
|
-
- HY-18667
-
-
- HY-12836
-
-
- HY-17490
-
Oxaceprol
N-Acetyl-L-hydroxyproline
|
Others
|
Inflammation/Immunology
|
Oxaceprol (N-Acetyl-L-hydroxyproline), an orally active derivative of L-proline, possesses distinct anti-inflammatory activity. Oxaceprol is usually used for the research of osteoarthritis and rheumatoid arthritis.
|
-
- HY-116609
-
-
- HY-143455
-
-
- HY-N2083
-
Handelin
|
NF-κB
|
Inflammation/Immunology
|
Handelin is a guaianolide dimer from Chrysanthemum boreale that has potent anti-inflammatory activity by down-regulating NF-κB signaling and pro-inflammatory cytokine production.
|
-
- HY-101041
-
-
- HY-N0469S1
-
-
- HY-121481
-
Cucurbitadienol
10α-Cucurbitadienol
|
Others
|
Inflammation/Immunology
|
Cucurbitadienol (10α-Cucurbitadienol) is a natural product that can be found in the seeds of Trichosanthes kirilowii. Cucurbitadienol exhibits anti-inflammatory effect.
|
-
- HY-108458
-
-
- HY-B0494
-
-
- HY-16780
-
-
- HY-N10438
-
-
- HY-18791
-
-
- HY-118561
-
Bermoprofen
AD-1590
|
Others
|
Inflammation/Immunology
|
Bermoprofen (AD-1590) is an orally active non-steroidal anti-inflammatory agent. Bermoprofen has potent antipyretic activities with a short biological half-life. Bermoprofen is a potent antagonist of LPS-induced fever in rabbits.
|
-
- HY-18779
-
PF-4840154
|
TRP Channel
|
Inflammation/Immunology
|
PF-4840154 is a potent, selective agonist of the rat and human TrpA1 channel with EC50s of 97 and 23 nM, respectively. PF-4840154 elicits TrpA1-mediated nocifensive behaviour in mouse.
|
-
- HY-N4264
-
Vinaginsenoside R3
|
Others
|
Inflammation/Immunology
|
Vinaginsenoside R3 is a saponin composition of roots of Panax ginseng. Ginsengs have been not only used as therapeutic agents with tonic, anti-fatigue, and anti-gastric ulcer effect but also marketed as dietary supplements and raw materials of health food.
|
-
- HY-133608
-
-
- HY-147815
-
COX-2-IN-21
|
COX
|
Inflammation/Immunology
|
COX-2-IN-21 (Compound 5c) is a selective and orally active COX-2 inhibitor with an IC50 of 0.039 μM. COX-2-IN-21 shows promising anti-inflammatory potential.
|
-
- HY-128799
-
-
- HY-108609
-
-
- HY-101265
-
S1p receptor agonist 1
|
LPL Receptor
|
Inflammation/Immunology
|
S1p receptor agonist 1 is a potent and orally active S1P receptor agonist, exhibits an activity of inducing S1P1 internalization (EC50=9.83 nM). S1p receptor agonist 1 has the potential for the study of arthritis and EAE (experimental autoimmune encephalitis). S1p receptor agonist 1 is extracted from patent WO2015039587A1, Compound 2.
|
-
- HY-125997
-
BTK inhibitor 10
|
Btk
|
Inflammation/Immunology
|
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
|
-
- HY-120323
-
DRI-C21045
|
TNF Receptor
|
Inflammation/Immunology
|
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively.
|
-
- HY-N2344
-
Procyanidin A1
Proanthocyanidin A1
|
PKC
|
Inflammation/Immunology
|
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
|
-
- HY-14277A
-
-
- HY-N4096
-
Tsugaric acid A
|
Others
|
Inflammation/Immunology
|
Tsugaric acid A can significantly inhibit superoxide anion formation. Tsugaric acid A also protects human keratinocytes against damage induced by ultraviolet B (UV B) light. Tsugaric acid A can protect keratinocytes from photodamage.
|
-
- HY-N2909
-
Aurantiamide
|
Others
|
Inflammation/Immunology
|
Aurantiamide is an orally active constituent of Portulaca oleracea L and has various biological activities, including antioxidant, antiplatelet, anti-inflammatory, and antitumor activities.
|
-
- HY-15495
-
-
- HY-139719
-
IMD-biphenylC
|
NF-κB
|
Inflammation/Immunology
|
IMD-biphenylC is a novel imidazoquinolinone-NF-κB immunomodulator dimer that inhibits tumor proliferation while induces low systemic inflammation and reduces adjuvant toxicity.
|
-
- HY-145561
-
-
- HY-U00260
-
-
- HY-B1203
-
-
- HY-18710
-
-
- HY-P1505A
-
-
- HY-150746
-
ODN 24991
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
ODN 24991, a guanine-modified inhibitory oligonucleotide (INH-ODN), is a TLR3, TLR7 and TLR9 (Toll-like receptor) inhibitor, and its parent is INH-ODN 2088. ODN 24991 disrupts TLR3-, TLR7- and TLR9-mediated immune cell immune responses. ODN 24991 sequence: 5'-C-C-T-G-G-C-c7rGm-G-G-G-3'.
|
-
- HY-B1893
-
-
- HY-146220
-
-
- HY-128695
-
-
- HY-108631
-
EB-47 dihydrochloride
|
PARP
|
Inflammation/Immunology
|
EB-47 dihydrochloride, a potent and selective PARP-1/ARTD-1 inhibitor with an IC50 value of 45 nM, shows modest potency against ARTD5 with an IC50 value of 410 nM. EB-47 mimics the substrate NAD + and extends from the nicotinamide to the adenosine subsite.
|
-
- HY-13315S1
-
Montelukast-d6 sodium
MK0476-d6
|
Leukotriene Receptor
|
Inflammation/Immunology
|
Montelukast-d6 sodium (MK0476-d6) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
|
-
- HY-146547
-
Anti-inflammatory agent 17
|
|
Inflammation/Immunology
|
Anti-inflammatory agent 17 is a potent and orally active anti-inflammatory agent. Anti-inflammatory agent 17 inhibits the release of IL-6 and TNF-α in vitro experiments without cytotoxicity. Anti-inflammatory agent 17 exhibits anti-inflammatory activity in vivo. Anti-inflammatory agent 17 has the potential for the research of Acute lung injury (ALI).
|
-
- HY-B1060
-
-
- HY-146486
-
P2Y2R/GPR17 antagonist 1
|
P2Y Receptor
|
Inflammation/Immunology
|
P2Y2R/GPR17 antagonist 1 (Compound 14m) is a dual P2Y2R and GPR17 antagonist with IC50 values of 3.17 µM and 1.67 µM against P2Y2R and GPR17, respectively. P2Y2R/GPR17 antagonist 1 shows excellent metabolic stability in human liver microsomes.
|
-
- HY-128113
-
-
- HY-N9312
-
-
- HY-145373
-
BMS-986143
|
Btk
|
Inflammation/Immunology
|
BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases.
|
-
- HY-N6020
-
(-)-Butin
|
Others
|
Inflammation/Immunology
|
(-)-Butin is the S enantiomer of Butin. Butin is a major biologically active flavonoid isolated from the heartwood of Dalbergia odorifera, with strong antioxidant, antiplatelet and anti-inflammatory activities.
|
-
- HY-113134
-
-
- HY-N2156
-
-
- HY-111866
-
-
- HY-U00157
-
Meseclazone
W2395; NSC297623
|
Others
|
Inflammation/Immunology
|
Meseclazone (W2395;NSC297623) exhibits inhibitory potency of secondary phase ADP aggregation. Meseclazone possesses anti-inflammatory, analgesic and antipyretic activity.
|
-
- HY-12815A
-
-
- HY-N8209
-
-
- HY-119720
-
-
- HY-116835
-
BI-6901
|
CCR
|
Inflammation/Immunology
|
BI 6901 is a potent, selective CCR10 antagonist (pIC50=9.0). BI 6901 shows high selectivity over other GPCRs, including a number of other chemokine receptors. BI 6901 is efficacious in the murine DNFB model of contact hypersensitivity and can be used for inflammation research.
|
-
- HY-141644
-
PY-60
|
YAP
|
Inflammation/Immunology
|
PY-60 is a robust and specific activator of YAP transcriptional activity that targets annexin A2 (ANXA2) with a Kd of 1.4 µM. PY-60 directly binds to ANXA2 and antagonizes its normal cellular function of repressing YAP activity.
|
-
- HY-136339
-
-
- HY-16754
-
-
- HY-12657
-
-
- HY-150551
-
COX-2-IN-27
|
COX
|
Inflammation/Immunology
|
COX-2-IN-27 is a potent and selective COX-2 inhibitor with IC50 values of 13.22, 0.045, 1.67 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-27 shows anti-inflammatory activity.
|
-
- HY-135490
-
-
- HY-U00258
-
-
- HY-147972
-
NF-κB/MAPK-IN-1
|
NF-κB
p38 MAPK
NO Synthase
COX
|
Inflammation/Immunology
|
NF-κB/MAPK-IN-1 (compound 11a) is a potent inhibitor of NF-κB and MAPK pathway. NF-κB/MAPK-IN-1 shows inhibitory activity against NO production, with an IC50 of 6.96 µM. NF-κB/MAPK-IN-1 suppresses LPS-induced iNOS, COX-2, ERΚ and P38 signaling activation. NF-κB/MAPK-IN-1 can prevent LPS induced inflammatory response in macrophages. NF-κB/MAPK-IN-1 can be used for rheumatoid arthritis (RA) research.
|
-
- HY-117610AS
-
Bisindolylmaleimide XI-d6 hydrochloride
Ro 32-0432-d6; Ro 31-8830-d6 hydrochloride
|
PKC
|
Inflammation/Immunology
|
Bisindolylmaleimide XI-d6 hydrochloride (Ro 32-0432-d6) is the deuterium labeled Bisindolylmaleimide XI hydrochloride. Bisindolylmaleimide XI hydrochloride (Ro 32-0432) is a potent, selective and orally active PKC inhibitor with IC50s of 9 nM, 28 nM, 31 nM, 37 nM, and 108 nM for PKCα, PKCβI, PKCβII, PKCγ, and PKCε, respectively.
|
-
- HY-103332
-
N-Arachidonylglycine
NA-Gly
|
GlyT
Endogenous Metabolite
|
Inflammation/Immunology
|
N-Arachidonylglycine (NA-Gly), a carboxylic analog of the endocannabinoid anandamide (AEA), is a GPR18 agonist (EC50 = 44.5 nM). Unlike AEA, N-Arachidonylglycine has no activity at either CB1 or CB2 receptors. N-Arachidonylglycine inhibits GLYT2 (IC50 = 5.1 μM). N-Arachidonylglycine also is an effective activator of endometrial cell migration.
|
-
- HY-131870
-
-
- HY-N0481
-
Roburic acid
|
COX
|
Inflammation/Immunology
|
Roburic acid, a tetracyclic triterpenoid found in Gentiana macrophylla, acts as an inhibitor of COX, with IC50s of 5 and 9 μM for COX-1 and COX-2, respectively.
|
-
- HY-N9834
-
-
- HY-115770
-
8-Methylsulfinyloctyl isothiocyanate
|
Others
|
Inflammation/Immunology
|
8-Methylsulfinyloctyl isothiocyanate, an isothiocyanate, has antimicrobial activity and remarkable inhibitory activity against plant growth. 8-Methylsulfinyloctyl isothiocyanate impair COX-2 mediated inflammatory responses in LPS stimulated raw macrophages.
|
-
- HY-N2263
-
Skimmin
Umbelliferone glucoside
|
Others
|
Inflammation/Immunology
|
Skimmin (Umbelliferone glucoside) is a coumarin found in Hydrangea paniculata, inhibits immune complex deposition, with anti-inflammatory activity.
|
-
- HY-N0579
-
Fraxin
Fraxoside
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Fraxin isolated from Acer tegmentosum, F. ornus or A. hippocastanum, is a glucoside of fraxetin and reported to exert potent anti-oxidative stress action, anti-inflammatory and antimetastatic properties. Fraxin shows its antioxidative effect through inhibition of cyclo AMP phosphodiesterase enzyme.
|
-
- HY-126397
-
MnTBAP chloride
|
NF-κB
|
Inflammation/Immunology
|
MnTBAP chloride is a superoxide dismutase (SOD) mimetic and peroxynitrite scavenger. MnTBAP chloride is a manganic porphyrin complex and has anti-oxidative property. MnTBAP chloride mediates anti-inflammatory effects through upregulation of BMPR-II and inhibition of the NFκB signaling. MnTBAP chloride has the potential for the fibrotic response in chronic kidney diseases (CKDs) research.
|
-
- HY-19989AS
-
MK-571-d6 sodium
L-660711-d6 sodium
|
Leukotriene Receptor
|
Inflammation/Immunology
|
MK-571-d6 (L-660711-d6) sodium is the deuterium labeled MK-571 sodium salt. MK-571 sodium is a selective, orally active leukotriene D4 receptor antagonist, with Kis of 0.22 and 2.1 nM in guinea pig and human lung membranes.
|
-
- HY-144223
-
NLRP3/AIM2-IN-2
|
Others
|
Inflammation/Immunology
|
NLRP3 / aim2-in-2 is a new potent inhibitor with different species-specific effects on NLRP3 and aim2 inflammasome dependent cell death. Its < b > IC < sub > 50 < / sub > < / b > value is 0.2392 ± 0.0233 μ M。
|
-
- HY-114170
-
ML604440
|
Proteasome
|
Inflammation/Immunology
|
ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
ML604440 impairs MHC class I cell surface expression, IL-6 secretion and differentiation of naïve T helper cells to T helper 17 cells. ML604440 strongly ameliorates disease in experimental colitis and EAE.
|
-
- HY-16040
-
-
- HY-B1718
-
-
- HY-19989A
-
-
- HY-112675
-
-
- HY-123522
-
PAT-048
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
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 mouse plasma. PAT-048 reduces dermal fibrosis in vivo.
|
-
- HY-137561
-
Bexotegrast
|
Integrin
|
Inflammation/Immunology
|
Bexotegrast is a potent inhibitor of ανβ6 integrin. Bexotegrast can be used for researching fibrosis such as idiopathic pulmonary fibrosis (IPF) and nonspecific interstitial pneumonia (NSIP) (extracted from patent WO2020210404A1, compound 5).
|
-
- HY-120813A
-
-
- HY-B1063
-
Terpin hydrate
Terpin monohydrate; cis-Terpin hydrate
|
Others
|
Inflammation/Immunology
|
Terpin hydrate is an expectorant, commonly used to loosen mucus in patients presenting with acute or chronic bronchitis, and related conditions.
|
-
- HY-142941
-
Glucocorticoid receptor-IN-1
|
Glucocorticoid Receptor
MMP
|
Inflammation/Immunology
|
Glucocorticoid receptor-IN-1 (Compound WX002) is a selective glucocorticoid receptor (GR) modulator with anti-inflammatory effect. Glucocorticoid receptor-IN-1 exhibits very good transcriptional repressive activity with an IC50 of 2.11 nM against hMMP1, and transcriptional activation activity with an EC50 of 5.59 nM against MMTV.
|
-
- HY-142618
-
-
- HY-102046
-
FM-381
|
JAK
|
Inflammation/Immunology
|
FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
|
-
- HY-135642
-
SMS1-IN-1
|
Others
|
Inflammation/Immunology
|
SMS1-IN-1, compound SAPA 1j, is a novel and the most potent sphingomyelin synthase 1 (SMS1) inhibitor with an IC50 value of 2.1 μM. SMS1-IN-1 has the potential for the treatment of atherosclerosis.
|
-
- HY-P99004
-
hMC1R agonist 1
|
Melanocortin Receptor
|
Inflammation/Immunology
|
(EC50=3 nM). hMC1R agonist 1 shows at least 300-fold selectivity for hMC1R over hMC3R (b>EC50=902 nM), hMC4R (b>EC50=915 nM), and hMC5R (b>EC50=>1000 nM). hMC1R agonist 1 has the potential for the therapeutic intervention of melanocortin family.
|
-
- HY-P3434
-
Ac-FEID-CMK
|
Pyroptosis
|
Inflammation/Immunology
|
Ac-FEID-CMK is a potent zebrafish-specific GSDMEb-derived peptide inhibitor.
Ac-FEID-CMK can attenuate the mortality and kidney injury during septic shock. Ac-FEID-CMK inhibits pyroptosis and attenuates septic AKI (acute kidney injury) in vivo. Ac-FEID-CMK can suppress the caspy2-mediated noncanonical inflammasome pathway.
|
-
- HY-125197
-
BRD5631
|
Autophagy
|
Inflammation/Immunology
|
BRD5631 is an autophagy enhancer, enhances autophagy through an mTOR-independent pathway. BRD5631 affects several cellular disease phenotypes previously linked to autophagy, including protein aggregation, cell survival, bacterial replication, and inflammatory cytokine production.
|
-
- HY-145726
-
ISIS 104838
|
TNF Receptor
|
Inflammation/Immunology
|
ISIS 104838 is an antisense oligonucleotide drug that reduces the production of tumor necrosis factor (TNF-alpha), a substance that contributes to joint pain and swelling in rheumatoid arthritis.
|
-
- HY-108538
-
Ethacrynic acid D5
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
|
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
|
-
- HY-108249
-
Tribenoside
|
Others
|
Inflammation/Immunology
|
Tribenoside is a vasoprotective agent, can be used for the research of hemorrhoids. Tribenoside has mild anti-inflammatory, analgesic, and wound healing properties.
|
-
- HY-139807
-
JAK-IN-14
|
JAK
|
Inflammation/Immunology
|
JAK-IN-14 is a potent and selective JAK1 inhibitor, with an IC50 of <5 μM. JAK-IN-14 is >8-fold more selective for JAK1 than JAK2 and JAK3 (Patent WO2016119700A1, compound 16).
|
-
- HY-115936
-
COX-2-IN-9
|
COX
|
Inflammation/Immunology
|
COX-2-IN-9 (compound 7a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 10.17 uM. COX-2-IN-9 has higher COX-2 selectivity than Celecoxib. COX-2-IN-9 shows good in vivo anti-inflammatory and low ulcerogenic activity.
|
-
- HY-101766
-
-
- HY-102036
-
G-744
|
Btk
|
Inflammation/Immunology
|
G-744 is a highly potent, selective and orally active Btk inhibitor with an IC50 of 2 nM. G-744 is metabolically stable, well tolerated and efficacious to treat arthritis.
|
-
- HY-11092
-
-
- HY-N7036
-
-
- HY-147606
-
-
- HY-118827
-
Vedaprofen
Quadrisol; CERM 10202; PM 150
|
COX
|
Inflammation/Immunology
|
Vedaprofen (Quadrisol) is a COX-1 selective nonsteroidal anti-inflammatory drug (NSAID) for serum TxB2 and exudate PGE2 inhibition . Vedaprofen is a Escherichia coli (E. coli) sliding clamp (SC) inhibitor with the IC50 of 222 μM.
|
-
- HY-15651
-
Alvelestat
AZD9668
|
Elastase
|
Inflammation/Immunology
|
Alvelestat (AZD9668) is an orally bioavailable, affinity and selective inhibitor of neutrophil elastase (NE) with a pIC50 value of 7.9 nM, a Ki value of 9.4 nM and a Kd value of 9.5 nM.
|
-
- HY-134471
-
TNF-α-IN-2
|
TNF Receptor
|
Inflammation/Immunology
|
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.
|
-
- HY-U00352
-
-
- HY-146745
-
-
- HY-W012399
-
-
- HY-147774
-
NAAA-IN-2
|
Others
|
Inflammation/Immunology
|
NAAA-IN-2 (Compound 9) is a potent and selective inhibitor of NAAA with an IC50 of 50 nM. NAAA is a cysteine amidase which preferentially hydrolyzes the endogenous biolipids palmitoylethanolamide (PEA) and oleoylethanolamide (OEA). NAAA-IN-2 has the potential for the research of inflammation and pain.
|
-
- HY-N1955
-
-
- HY-131910
-
IHMT-PI3Kδ-372
|
PI3K
Cytochrome P450
|
Inflammation/Immunology
|
IHMT-PI3Kδ-372 is a potent and selective PI3Kδ inhibitor with an IC50 of 14 nM. IHMT-PI3Kδ-372 shows high selectivity over other class I PI3Ks (56∼83 fold) and other protein kinases. IHMT-PI3Kδ-372 can be uesd for chronic obstructive pulmonary disease (COPD) research.
|
-
- HY-B1320
-
Meclofenamic acid sodium
Meclofenamate sodium
|
Gap Junction Protein
Endogenous Metabolite
|
Inflammation/Immunology
|
Meclofenamic acid (Meclofenamate) sodium is a nonsteroidal anti-inflammatory drug (NSAID) approved for use in arthritis (osteo and rheumatoid), analgesia (mild to moderate pain), dysmenorrhea, and heavy menstrual blood loss (menorrhagia). Meclofenamic acid sodium is a non-selective gap-junction blocker and a highly selective inhibitor of fat mass and obesity-associated (FTO) enzyme inhibitor.
|
-
- HY-N3007
-
Naringenin chalcone
|
Others
|
Inflammation/Immunology
|
Naringenin chalcone is an intermediate in flavonol biosynthesis and is spontaneously metabolized into naringenin (NAR) by chalcone isomerase. Naringenin chalcone has anti-inflammatory and antiallergic activities.
|
-
- HY-U00197
-
Tilmacoxib
JTE522; JTP19605; RWJ57504
|
COX
|
Inflammation/Immunology
|
Tilmacoxib (JTE522) is a highly selective, time-dependent and irreversible human COX-2 inhibitor with an IC50 of 85 nM in an enzyme assay.
|
-
- HY-112256
-
-
- HY-109175
-
-
- HY-19672
-
Lirimilast
BAY 19-8004
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties.
|
-
- HY-W019940
-
-
- HY-124772
-
-
- HY-141550
-
BPK-25
|
Others
|
Inflammation/Immunology
|
BPK-25, an active acrylamide, promotes degradation of nucleosome remodeling and deacetylation (NuRD) complex proteins by a post-translational mechanism involving covalent protein engagement. BPK-25 inhibits TMEM173 activation by the cyclic dinucleotide ligand cGAMP.
|
-
- HY-137976
-
Penehyclidine hydrochloride
Penequinine hydrochloride
|
mAChR
NF-κB
|
Inflammation/Immunology
|
Penehyclidine (Penequinine) hydrochloride, a anticholinergic drug, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation.
|
-
- HY-132808
-
Atuzabrutinib
SAR 444727; PRN473
|
Btk
|
Inflammation/Immunology
|
Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling.
|
-
- HY-125171
-
IAXO-102
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development.
|
-
- HY-146757
-
RIPK1-IN-13
|
RIP kinase
|
Inflammation/Immunology
|
RIPK1-IN-13 (Compound 8) is a potent inhibitor of RIPK1 with an IC50 value of 1139 nM. RIPK1-IN-13 blocks the activation of the necroptosis pathway via the inhibition of RIPK1. RIPK1-IN-13 has the potential for the research of inflammation diseases.
|
-
- HY-108672
-
NF157
|
P2Y Receptor
|
Inflammation/Immunology
|
NF157 is a highly selective nanomolar P2Y11 antagonist with a pKi of 7.35. The IC50s are 463 nM, 1811 µM, 170 µM for P2Y11 (Ki=44.3 nM), P2Y1 (Ki=187 µM), P2Y2 (Ki=28.9 µM), respectively. NF157, significantly reduces expression of metalloproteinase (MMP)-3, MMP-13, can be used in the treatment of osteoarthritis (OA).
|
-
- HY-P1377
-
-
- HY-118423
-
SJ-3366
IQP-0410
|
HIV
|
Inflammation/Immunology
|
SJ-3366 (IQP-0410) is a potent inhibitor of HIV nonnucleoside reverse transcriptase. SJ-3366 (IQP-0410) inhibits HIV at sub-nanomolar concentrations primarily through a typical non-nucleoside mechanism.
|
-
- HY-N0131S1
-
-
- HY-142940
-
RORγt modulator 5
|
ROR
|
Inflammation/Immunology
|
RORγt modulator 5 is a RORγt modulator with a Ki value of <100 nM. RORγt modulator 5 has the potential for inflammatory, metabolic, autoimmune and other diseases mediated by RORy study (WO2017132432A1; compound 2).
|
-
- HY-N7176
-
Kaempferol 3-O-β-D-glucuronide
Kaempferol-3-glucuronide; Kaempferol-3-O-glucuronide
|
Interleukin Related
|
Inflammation/Immunology
|
Kaempferol 3-O-β-D-glucuronide (Kaempferol-3-glucuronide), one conjugated kaempferol metabolite, has anti-inflammatory effect. Kaempferol 3-O-β-D-glucuronide significantly inhibits various pro-inflammatory mediators like IL-1β, NO, PGE2, and LTB4. Kaempferol 3-O-β-D-glucuronide upregulates the secretion of anti-inflammatory cytokine IL-10.
|
-
- HY-B0004S1
-
-
- HY-147311
-
-
- HY-U00129
-
-
- HY-144373
-
-
- HY-113849
-
MLS-573151
MLS000573151
|
Ras
|
Inflammation/Immunology
|
MLS-573151 (MLS000573151) is a selective GTPase Cdc42 inhibitor with an EC50 of 2 μM. MLS-573151 is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to Cdc42.
|
-
- HY-117602
-
-
- HY-111674
-
-
- HY-146295
-
COX-2/5-LOX-IN-2
|
COX
|
Inflammation/Immunology
|
COX-2/5-LOX-IN-2 (5b) is a potent and dual inhibitor of COX-2/5-LOX. COX-2/5-LOX-IN-2 is a benzothiophen-2-yl pyrazole carboxylic acid derivative. COX-2/5-LOX-IN-2 shows the most potent analgesic and anti-inflammatory activities surpassing that of Celecoxib and Indomethacin. COX-2/5-LOX-IN-2 shows potent COX-1, COX-2 and 5-LOX inhibitory activity with IC50s of 5.40, 0.01 and 1.78 μM, respectively.
|
-
- HY-116282C
-
-
- HY-N3114
-
-
- HY-N2243
-
-
- HY-108944
-
LYP-IN-1
|
Phosphatase
|
Inflammation/Immunology
|
LYP-IN-1 is a potent, selective and specific LYP inhibitor with a Ki and an IC50 of 110 nM and 0.259 μM, respectively. LYP-IN-1 also has selectivity for a large panel of PTPs, such as SHP1 (IC50=5 μM) and SHP2 (IC50=2.5 μM). LYP-IN-1 exhibits highly efficacious cellular activity in T- and mast cells. LYP-IN-1 can be used for the study of autoimmune disorders.
|
-
- HY-B1079
-
-
- HY-117819
-
TMP920
|
ROR
|
Inflammation/Immunology
|
TMP920 is a highly potent and selective RORγt antagonist. TMP920 inhibits RORγt binding to the SRC1 peptide with an IC50 of 0.03 μM.
|
-
- HY-17479A
-
-
- HY-N1912
-
Andropanolide
|
NF-κB
|
Inflammation/Immunology
|
Andrographolide (Andro) is a small antagonist for NF-κB activation by covalent modifying reduced cysteine 62 of p50. Andrographolide is a bicyclic diterpenoid lactone mainly produced from the plant Andrographis (Andrographis paniculate).
Andrographolide suppresses the activation of NF-κB in stimulated endothelial cells, which reduces the expression of cell adhesion molecule E-selectin and prevents E-selectin-mediated leukocyte adhesion, but has no effect on IκBα degradation, p50 and p65 nuclear translocation.
|
-
- HY-145893
-
-
- HY-12507
-
-
- HY-123763
-
MLN3126
|
CCR
|
Inflammation/Immunology
|
MLN3126 is an orally active and potent CCR9 antagonist. MLN3126 inhibits CCL25-induced calcium mobilization and chemotaxis of mouse primary thymocytes, wiht an IC50 value of 6.3 nM for calcium influx.
|
-
- HY-112879
-
-
- HY-P1110
-
AF12198
|
Interleukin Related
|
Inflammation/Immunology
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
|
-
- HY-112650
-
-
- HY-N2012
-
-
- HY-111811
-
Homomangiferin
|
Others
|
Inflammation/Immunology
|
Homomangiferin is mangiferin monomethyl ether. Homomangiferin has important medicinal properties and is widely used to relieve many symptoms, for example coughing and asthma.
|
-
- HY-P9908A
-
-
- HY-114330A
-
-
- HY-143493
-
Influenza virus-IN-2
|
Influenza Virus
|
Inflammation/Immunology
|
Influenza virus-IN-2 (compound 19) is a potent influenza virus inhibitor with an EC50 of 2.58 µM and CC50 of 150.85 µM. Influenza virus-IN-2 shows a concentration dependent inhibition activity for PAN endonuclease with EC50 of 489.39 nM. Influenza virus-IN-2 shows shows anti-influenza A virus activities.
|
-
- HY-13283
-
-
- HY-103177
-
PSB-10 hydrochloride
|
Adenosine Receptor
|
Inflammation/Immunology
|
PSB-10 hydrochloride is a potent and selective antagonist of human adenosine A3 receptor (A3AR), with a Ki of 0.44 nM. PSB-10 hydrochloride shows more than 800-fold selectivity for hA3 over rA1, rA2A, hA1, hA2A and hA2B receptors (Ki=805, 6040, 1700, 2700, 30000 nM, respectively). PSB-10 hydrochloride produces thermal hyperalgesia in mice.
|
-
- HY-A0221
-
Ridogrel
R 68070
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
Ridogrel (R 68070) is an orally active combined thromboxane A2 synthetase inhibitor and thromboxane A2/prostaglandin endoperoxide receptor blocker. Ridogrel is potent antiplatelet agent. Anti-inflammatory activities.
|
-
- HY-129393
-
AB928
|
Adenosine Receptor
|
Inflammation/Immunology
|
AB928 is an orally bioavailable, selective dual adenosine receptor (A2aR/A2bR) antagonist. AB928 relieves adenosine-mediated immune suppression. AB928 has immunomodulatory and antitumor activities.
|
-
- HY-N7703
-
D-Mannuronic acid sodium
|
Others
|
Inflammation/Immunology
|
D-Mannuronic acid sodium, isolated from Macrocystis pyrifera, has the potential in autoimmune encephalomyelitis (EAE), adjuvant induced arthritis (AIA), nephrotic syndrome, and acute glomerulonephritis studies.
|
-
- HY-101526
-
-
- HY-101092
-
QS-21
Stimulon
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
QS-21, an immunostimulatory saponin, could be used as a potent vaccine adjuvant. QS-21 stimulates Th2 humoral and Th1 cell-mediated immune responses through action on antigen presenting cells (APCs) and T cells. QS-21 can activate the NLRP3 inflammasome with subsequent release of caspase-1 dependent cytokines, IL-1β and IL-18.
|
-
- HY-101922
-
-
- HY-100474
-
-
- HY-17470
-
Mizoribine
NSC 289637; HE 69
|
HCV
SARS-CoV
|
Inflammation/Immunology
|
Mizoribine (NSC 289637), an imidazole nucleoside, inhibits HCV RNA replication with IC50 of approximately 100 μM for anti-HCV activity. Immunosuppressant. Mizoribine, an IMPDH inhibitor, inhibits replication of SARS-CoV with IC50s of 3.5 μg/mL and 16 μg/mL for SARS-CoV Frankfurt-1 and SARS-CoV HKU39849, respectively.
|
-
- HY-N4265
-
Vinaginsenoside R4
|
Others
|
Inflammation/Immunology
|
Vinaginsenoside R4, isolated from the leaves of hydroponic Panax ginseng. It has an inhibitory effect on melanin biosynthesis without any cytotoxic effects on the melan-a cells, and enhances the depigmentation on the zebrafish.
|
-
- HY-12245
-
-
- HY-17569S
-
Difluprednate-d3
|
|
Inflammation/Immunology
|
Difluprednate-d3 is the deuterium labeled Difluprednate. Difluprednate (Durezol), a corticosteroid, is thought to act by the induction of phospholipase A2 inhibitory proteins (lipocortins). Difluprednate is approved difluprednate for the treatment of post-operative ocular inflammation and pain.
|
-
- HY-144634
-
DDO-7263
|
Keap1-Nrf2
|
Inflammation/Immunology
|
DDO-7263, a 1,2,4-Oxadiazole derivative, is a potent Nrf2 activator. DDO-7263 upregulates Nrf2 through binding to Rpn6 to block the assembly of 26S proteasome and the subsequent degradation of ubiquitinated Nrf2. DDO-7263 activates the Nrf2-ARE signaling pathway and exerts anti-inflammatory activity.
|
-
- HY-B1390B
-
-
- HY-N9315
-
-
- HY-144126
-
S1P1 agonist 5
|
LPL Receptor
|
Inflammation/Immunology
|
S1P1 agonist 5 is a selective and orally active S1P1 agonist. S1P1 agonist 5 inhibits the lymphocyte egress from the lymphoid tissue to the peripheral blood. S1P1 agonist 5 has the potential for the research of multiple sclerosis (MS).
|
-
- HY-112667
-
-
- HY-17002
-
Suplatast (Tosilate)
IPD 1151T
|
Interleukin Related
|
Inflammation/Immunology
|
Suplatast Tosilate (IPD 1151T) is an orally active Th2 cytokine inhibitor which can inhibit both IL-4 and IL-5 production from Th2 cells and suppress IgE synthesis. Suplatast Tosilate is an anti-allergic agent. Suplatast Tosilate has antiasthmatic, anti-inflammatory and antifibrotic activity.
|
-
- HY-132196
-
-
- HY-106765
-
Thymotrinan
RGH-0205; TP3
|
Others
|
Inflammation/Immunology
|
Thymotrinan (RGH-0205) is a biologically active fragment of the naturally occurring thymus hormone thymopoietin and a immunomodulating peptide. Thymotrinan exerts similar immunomodulatory activities to TP5 and to affect humoral as well as cellular responses.
|
-
- HY-108323
-
CCR2 antagonist 4
Teijin compound 1
|
CCR
|
Inflammation/Immunology
|
CCR2 antagonist 4 (Teijin compound 1) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-B1727
-
Phenanthrene
|
Others
|
Inflammation/Immunology
|
Phenanthrene is a polycyclic aromatic hydrocarbon (PAH) and has been frequently used as an indicator for monitoring PAH contaminated matrices. Phenanthrene induces oxidative stress and inflammation.
|
-
- HY-N10404
-
Junceellolide C
|
HBV
|
Inflammation/Immunology
|
Junceellolide C is a transcription inhibitor of cccDNA. Junceellolide C inhibits HBV DNA replication and significantly decreases the level of supernatant HBV RNA with EC50 values of 5.19, 3.52 μM respectively in HepAD38 cells. Junceellolide C is a potent anti-HBV agent.
|
-
- HY-16039
-
AM095
|
LPL Receptor
|
Inflammation/Immunology
|
AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
|
-
- HY-U00263
-
-
- HY-100162
-
-
- HY-100954
-
-
- HY-145352
-
-
- HY-134771
-
YM-341619
AS1617612
|
STAT
|
Inflammation/Immunology
|
YM-341619 (AS1617612) is a potent and orally active STAT6 inhibitor with an IC50 of 0.70 nM. YM-341619 inhibits Th2 differentiation in mouse spleen T cells induced by IL-4 (IC50=0.28 nM) without affecting Th1 cell differentiation. YM-341619 is a promising compound for the the research of allergic diseases, such as allergic asthma.
|
-
- HY-103267A
-
-
- HY-144194
-
MIF-IN-2
|
Others
|
Inflammation/Immunology
|
MIF-IN-2 is a migration inhibitory factor (MIF) inhibitor extracted from patent WO2021258272A1 compound 1. MIF-IN-2 can be used for the research of immune inflammation-related diseases.
|
-
- HY-136651
-
BNTA
|
Others
|
Inflammation/Immunology
|
BNTA, a potent extracellular matrix (ECM) modulator, facilitates cartilage structural molecule synthesis on chondrocytes by activating superoxide dismutase 3 (SOD3). BNTA shows a promising potential for osteoarthritis alleviation by modulating cartilage generation.
|
-
- HY-132850
-
-
- HY-131064
-
RIPK3-IN-1
|
RIP kinase
|
Inflammation/Immunology
|
RIPK3-IN-1 is a RIPK3 type II DFG-out inhibitor with an IC50 of 9.1 nM. RIPK3-IN-1 inhibits RIPK1 and RIPK2 with IC50s of 5.5 and >10 μM. RIPK3-IN-1 is also a c-Met kinase inhibitor with an IC50 of 1.1 μM.
|
-
- HY-12117
-
-
- HY-N9011
-
-
- HY-100250
-
-
- HY-107046
-
UK-432097
|
Adenosine Receptor
|
Inflammation/Immunology
|
UK-432097 is a highly potent and selective A2AAR agonist with a pKi of 8.4 for human A2AAR. UK-432097 has anti-inflammatory and anti-aggregatory properties. UK-432097 has the potential for COPD (Chronic Obstructive Pulmonary Disease) research.
|
-
- HY-N0710
-
alpha-Cyperone
α-Cyperone; (+)-α-Cyperone
|
Endogenous Metabolite
|
Inflammation/Immunology
|
alpha-Cyperone (α-Cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1, resulting in reduction of inflammation, which would be highly beneficial for treatment of inflammatory diseases such as AD.
|
-
- HY-113556
-
-
- HY-101915
-
-
- HY-147748
-
COX-2-IN-17
|
COX
|
Inflammation/Immunology
|
COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC50 of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase.
|
-
- HY-123854
-
-
- HY-N1193
-
Sulfuretin
|
NF-κB
|
Inflammation/Immunology
|
Sulfuretin inhibits the inflammatory response by suppressing the NF-κB pathway. Sulfuretin can be used for the research of allergic airway inflammation. Sulfuretin reduces oxidative stress, platelet aggregation, and mutagenesis. Sulfuretin is a competitive and potent inhibitor of monophenolase and diphenolase activities with the IC50 of 13.64 μM.
|
-
- HY-15315
-
Baricitinib
LY3009104; INCB028050
|
JAK
|
Inflammation/Immunology
|
Baricitinib (LY3009104; INCB028050) is a selective and orally bioavailable JAK1 and JAK2 inhibitor with IC50s of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-17625
-
-
- HY-N6065
-
Praeruptorin A
|
NF-κB
|
Inflammation/Immunology
|
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
|
-
- HY-D0054
-
-
- HY-142644
-
-
- HY-N2106
-
Dehydroevodiamine
|
NF-κB
COX
PGE synthase
NO Synthase
|
Inflammation/Immunology
|
Dehydroevodiamine is a major bioactive quinazoline alkaloid isolated from Evodiae Fructus, has an antiarrhythmic effect in guinea-pig ventricular myocytes. Dehydroevodiamine inhibits LPS-induced iNOS, COX-2, prostaglandin E2 (PGE2) and nuclear factor-kappa B (NF-κB) expression in murine macrophage cells.
|
-
- HY-141549
-
BPK-21
|
Others
|
Inflammation/Immunology
|
BPK-21, an active acrylamide, suppresses T cell activation through blockade of ERCC3 function. BPK-21 specifically targets C342 in the helicase ERCC3.
|
-
- HY-N8816
-
-
- HY-124597
-
ARN726
|
Others
|
Inflammation/Immunology
|
ARN726 is a potent NAAA (N-acylethanolamine acid amidase) inhibitor with an IC50 of 0.073 µM. ARN726 decreases alcohol self-administration in a dose-dependent manner.
|
-
- HY-106139
-
Bimosiamose
TBC-1269
|
Others
|
Inflammation/Immunology
|
Bimosiamose (TBC-1269) is a nonoligosaccharide pan-selectin antagonist with IC50s of 88 μM, 20 μM, and 86 μM for E-selectin, P-selectin, and L-selectin, respectively. Bimosiamose has anti-inflammatory effects.
|
-
- HY-N0427
-
Phellodendrine
|
Akt
NF-κB
|
Inflammation/Immunology
|
Phellodendrine, a isoquinoline alkaloid, is one of important characteristic ingredients in the Phellodendri chinensis cortex. phellodendrine is against AAPH-induced oxidative stress through regulating the AKT/NF-κB pathway. Phellodendrine has good antioxidant, and anti-inflammatory effect .
|
-
- HY-B1026
-
-
- HY-108645
-
AL 8697
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.
|
-
- HY-111409
-
-
- HY-113008A
-
cis-Urocanic acid
(Z)-Urocanic acid; cis-UCA
|
5-HT Receptor
|
Inflammation/Immunology
|
cis-Urocanic acid is a 5-HT2A receptor agonist. cis-Urocanic acid binds to 5-HT receptor with relatively high affinity (Kd=4.6 nM). cis-Urocanic acid is an immune modulator that induces immunosuppression by binding to the 5-HT2A receptor.
|
-
- HY-128523A
-
-
- HY-108251
-
-
- HY-19303
-
-
- HY-15036A
-
Diclofenac diethylamine
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac diethylamine is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac diethylamine induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-B1279
-
-
- HY-135474
-
-
- HY-U00347
-
-
- HY-127090
-
Muramyl dipeptide
MDP
|
p38 MAPK
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide is an inducer of bone formation through induction of Runx2. Muramyl dipeptide directly enhances osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide is a NLRP1 agonist.
|
-
- HY-111820
-
CK1-IN-1
|
Casein Kinase
|
Inflammation/Immunology
|
CK1-IN-1 is a casein kinase 1 (CK1) inhibitor extracted from patent WO2015119579A1, compound 1c, has IC50s of 15 nM, 16 nM, 73 nM for CK1δ, and CK1ε, p38σ MAPK, respectively.
|
-
- HY-109091B
-
Lanraplenib succinate
GS-9876 succinate
|
Syk
|
Inflammation/Immunology
|
Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases. Lanraplenib succinate (GS-9876 succinate) inhibits SYK activity in platelets via the glycoprotein VI (GPVI) receptor without prolonging bleeding time (BT) in monkeys or humans.
|
-
- HY-130252
-
YQ128
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
YQ128 is a potent and selective second-generation NLRP3 (NOD-like receptor P3) inflammasome inhibitor with an IC50 of 0.30 µM. YQ128 significantly and selectively suppresses the production of IL-1β, but not TNF-α, and it can cross the BBB to reach the CNS. YQ128 has anti-inflammatory activity.
|
-
- HY-47228
-
KB-5492 free base
|
Sigma Receptor
|
Inflammation/Immunology
|
KB-5492 free base is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 free base is an anti-ulcer agent.
|
-
- HY-14351
-
-
- HY-15455S
-
Roflumilast-d4
|
Phosphodiesterase (PDE)
RSV
|
Inflammation/Immunology
|
Roflumilast-d4 is the deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
|
-
- HY-N4312
-
-
- HY-150739
-
-
- HY-106087
-
-
- HY-N4311
-
-
- HY-P0224
-
-
- HY-W004291
-
-
- HY-14126
-
-
- HY-N0318
-
-
- HY-N2605
-
-
- HY-14900
-
Tedalinab
GRC-10693
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
Tedalinab (GRC-10693) is a potent, orally active, and selective cannabinoid receptor 2 (CB2) agonist. Tedalinab has >4700-fold functional selectivity for CB2 over CB1. Tedalinab has potential for neuropathic pain and osteoarthritis treatment.
|
-
- HY-N0212
-
Peimine
Verticine; Dihydroisoimperialine
|
Others
|
Inflammation/Immunology
|
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.
|
-
- HY-102075B
-
TMP780
|
ROR
|
Inflammation/Immunology
|
TMP780 is an inverse agonist of RORγt with an IC50 of 13 nM. RORγt is a tractable drug target for the treatment of cutaneous inflammatory disorders.
|
-
- HY-139024
-
-
- HY-P1098
-
Ac2-26
|
NF-κB
|
Inflammation/Immunology
|
Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue.
|
-
- HY-W010708
-
-
- HY-108908A
-
Modipafant
UK-80067
|
Others
|
Inflammation/Immunology
|
Modipafant (UK-80067), the (+)-enantiomer of UK-74505, is a potent, orally active, and selective platelet-activating factor (PAF) antagonist. Modipafant exhibits approximately double the intrinsic potency of UK-74505.
|
-
- HY-115644
-
BMS-470539 dihydrochloride
|
Melanocortin Receptor
|
Inflammation/Immunology
|
BMS-470539 dihydrochloride is a highly potent and selective melanocortin-1 receptor (MC-1R) agonist with an IC50 of 120 nM, an EC50 of 28 nM. BMS-470539 dihydrochloride does not activate MC-3R and is a very weak partial agonist at MC-4R and MC-5R. BMS-470539 dihydrochloride has potently anti-inflammatory properties.
|
-
- HY-W040055
-
-
- HY-143714
-
Cathepsin K inhibitor 2
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K. Cathepsin K, Cat K is a cysteine protease expressed under the control of CTSK gene and closely related to osteoporosis, whose main function is to hydrolyze collagen. Cathepsin K inhibitor 2 has the potential for the research of osteoarthfitis (extracted from patent WO2021147882A1, compound 78).
|
-
- HY-20457
-
-
- HY-U00146
-
-
- HY-101015A
-
-
- HY-P1309
-
-
- HY-102075A
-
-
- HY-B0138
-
Ketorolac tromethamine salt
Ketorolac Tromethamine; Ketorolac tris salt; RS37619 tromethamine salt
|
COX
|
Inflammation/Immunology
|
Ketorolac tromethamine salt (RS37619 tromethamine salt) is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
|
-
- HY-144276
-
RIPK1-IN-11
|
RIP kinase
|
Inflammation/Immunology
|
RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity.
|
-
- HY-66005S1
-
Acetaminophen-d3
Paracetamol-d3; 4-Acetamidophenol-d3; 4'-Hydroxyacetanilide-d3
|
COX
Histone Acetyltransferase
Endogenous Metabolite
|
Inflammation/Immunology
|
Acetaminophen-d3 (Paracetamol-d3) is the deuterium labeled Acetaminophen. Acetaminophen (Paracetamol) is a selective cyclooxygenase-2 (COX-2) inhibitor with an IC50 of 25.8 μM; is a widely used antipyretic and analgesic agent. Acetaminophen is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-120785
-
SR1555
|
ROR
|
Inflammation/Immunology
|
SR1555 is a specific retinoic acid receptor-related orphan nuclear receptor γ (RORγ) inverse agonist with an IC50 value of 1 μM. SR1555 not only inhibits TH17 cell development and function but also increases the frequency of T regulatory cells, as well as inhibits the expression of IL-17. SR1555 can be used for researching autoimmune diseases.
|
-
- HY-14164A
-
-
- HY-U00156
-
-
- HY-N2414
-
Periplogenin
|
Others
|
Inflammation/Immunology
|
Periplogenin is a naturally occurring furanocoumarin found in Angelica dahurica roots, with potent anti-psoriatic effects. Periplogenin induces adipocyte differentiation.
|
-
- HY-122524
-
-
- HY-70069
-
-
- HY-15315A
-
Baricitinib phosphate
LY3009104 phosphate; INCB028050 phosphate
|
JAK
|
Inflammation/Immunology
|
Baricitinib phosphate (LY3009104 phosphate; INCB028050 phosphate) is a selective orally bioavailable JAK1/JAK2 inhibitor with IC50 of 5.9 nM and 5.7 nM, respectively.
|
-
- HY-19819
-
-
- HY-108776
-
-
- HY-105221
-
-
- HY-112318
-
-
- HY-136239
-
Beclomethasone 17-propionate
Beclomethasone-17-monopropionate; 17-BMP
|
Glucocorticoid Receptor
Drug Metabolite
|
Inflammation/Immunology
|
Beclomethasone 17-propionate (Beclomethasone-17-monopropionate), an active metabolite of Beclomethasone dipropionate (HY-13571), is a glucocorticoid receptor (GR) agonist. Beclomethasone 17-propionate exhibits greater affinity for GR than Beclomethasone dipropionate. Beclomethasone 17-propionate effectively suppresses cytokine production in chronic obstructive pulmonary disease (COPD) lung macrophages.
|
-
- HY-112451
-
-
- HY-137454
-
-
- HY-N10066
-
-
- HY-110047
-
-
- HY-12995A
-
(S)-BI 665915
|
FLAP
|
Inflammation/Immunology
|
(S)-BI 665915 is an orally active oxadiazole-containing 5-lipoxygenase-activating protein (FLAP) inhibitor with an IC50 of 1.7 nM for FLAP binding. (S)-BI 665915 inhibits FLAP functional in human whole blood with an IC50 of 45 nM. (S)-BI 665915 demonstrates an excellent cross-species drug metabolism and pharmacokinetics (DMPK) profile and a dose-dependent inhibition of LTB4 production.
|
-
- HY-113465A
-
11-trans Leukotriene E4
|
Others
|
Inflammation/Immunology
|
11-trans Leukotriene E4 is an isomer of Leukotriene E4 (LTE4). Slow isomerization of the C-11 double bond of LTE4 leads to the formation of 11-trans LTE4. 11-trans Leukotriene E4 is equipotent to LTE4 in contracting guinea pig ileum.
|
-
- HY-146723
-
IKKβ-IN-1
|
IKK
|
Inflammation/Immunology
|
IKKβ-IN-1 is a potent and orally active IkappaB (IKK-β) inhibitor with IC50 of 0.20 μM. IKKβ-IN-1 can reduce PGE2 and TNF-α production in mouse macrophage cells. IKKβ-IN-1 has the ability to protect mice against septic shock induced mortality.
|
-
- HY-135676
-
-
- HY-103183
-
-
- HY-101988
-
-
- HY-W020215
-
-
- HY-100164
-
SDZ-MKS 492
MKS 492
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats.
|
-
- HY-146334
-
DFBTA
|
Chloride Channel
|
Inflammation/Immunology
|
DFBTA is an orally active, potent and little brain penetrated ANO1 (Calcium-activated chloride channel anoctamin-1) inhibitor, with an IC50 of 24 nM. DFBTA shows analgesic efficacy for inflammatory pain.
|
-
- HY-U00239
-
-
- HY-U00132
-
-
- HY-N5045
-
Jionoside A1
|
Others
|
Inflammation/Immunology
|
Jionoside A1 isolated from Radix Rehmanniae Praeparata displays dose dependent immune-enhancement activity and possesses moderate protective activities on H2O2-treated SH-SY5Y cells.
|
-
- HY-13511
-
-
- HY-150608
-
-
- HY-13988
-
AT-56
|
PGE synthase
|
Inflammation/Immunology
|
AT-56 is a potent, selective and orally active inhibitor of lipocalin-type prostaglandin D synthase (L-PGDS), with an IC50 of 95 μM and Ki of 75 μM. AT-56 could selectively suppress the drowsiness or pain reaction mediated by L-PGDS-catalyzed PGD2.
|
-
- HY-N1921
-
-
- HY-N0023
-
Cistanoside A
|
NO Synthase
|
Inflammation/Immunology
|
Cistanoside A is a phenylethanoid isolated from Cistanche deserticola, reduces NO accumulation, but shows no effect on iNOS mRNA, iNOS protein levels or iNOS activity. Anti-inflammatory effect.
|
-
- HY-N0754
-
Eupalinolide A
|
HSP
|
Inflammation/Immunology
|
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
|
-
- HY-P1077A
-
CALP1 TFA
|
Calcium Channel
mGluR
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
|
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.
|
-
- HY-101058
-
-
- HY-138454
-
MEG hemisulfate
Mercaptoethylguanidine hemisulfate
|
NO Synthase
|
Inflammation/Immunology
|
MEG (Mercaptoethylguanidine) hemisulfate is a potent and selective inhibitor of the inducible NO synthase (iNOS), with EC50s of 11.5, 110, and 60 μM for iNOS, ecNOS, and bNOS respectively in tissue homogenates. MEG hemisulfate is also a potent scavenger of peroxynitrite and inhibits peroxynitrite-induced oxidative processes. MEG hemisulfate has a protective effect in many experimental models of inflammation, including ischemia/reperfusion injury, periodontitis, hemorrhagic shock, inflammatory bowel disease, and endotoxic and septic shock.
|
-
- HY-113066A
-
Guanosine 5'-diphosphate disodium salt
GDP disodium salt
|
Endogenous Metabolite
Potassium Channel
|
Inflammation/Immunology
|
Guanosine 5'-diphosphate (GDP) disodium salt is a nucleoside diphosphate that activates adenosine 5'-triphosphate-sensitive K + channel. Guanosine 5'-diphosphate disodium salt is a potential iron mobilizer, which prevents the hepcidin-ferroportin interaction and modulates the interleukin-6 (IL-6)/stat-3 pathway. Guanosine 5'-diphosphate disodium salt can be used in the research of inflammation, such as anemia of inflammation (AI).
|
-
- HY-135399
-
-
- HY-136556
-
-
- HY-118861AS1
-
-
- HY-W013331
-
-
- HY-W017389
-
-
- HY-139504
-
CC-99677
|
MAPKAPK2 (MK2)
|
Inflammation/Immunology
|
CC-99677 is a potent, covalent, and irreversible inhibitor of the mitogen-activated protein (MAP) kinase-activated protein kinase-2 (MK2) pathway in both biochemical (IC50=156.3 nM) and cell based assays (EC50=89 nM). CC-99677 is extracted from patent WO2020236636, compound 1.
|
-
- HY-149004
-
SLF1081851
|
LPL Receptor
|
Inflammation/Immunology
|
SLF1081851 (16 d) is an effective Sphingolipid Transporter 2 (Spns2) (S1P transporter) inhibitor with an IC50 value of 1.93 μM (S1P), SLF1081851 inhibits SphK2 with an IC50 value of ≈ 30 μM (SphK2), and is at least 15-fold more selective for SphK2 than SphK1. SLF1081851 has the potential to investigate Spns2 biology and can be used for autoimmune encephalomyelitis (EAE) research.
|
-
- HY-126378
-
-
- HY-P1308
-
-
- HY-N5043
-
-
- HY-139019
-
-
- HY-143890
-
-
- HY-142687
-
-
- HY-12680
-
PRN694
|
Itk
|
Inflammation/Immunology
|
PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo.
|
-
- HY-135400
-
-
- HY-12116
-
-
- HY-101056
-
-
- HY-17478A
-
-
- HY-P9911
-
Vedolizumab
Anti-Human lymphocyte α4β7 integrin, Humanized Antibody
|
Integrin
|
Inflammation/Immunology
|
Vedolizumab is a humanized IgG1 monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
|
-
- HY-18992
-
AS2444697
|
IRAK
|
Inflammation/Immunology
|
AS2444697 is an orally active IRAK-4 inhibitor with an IC50 of 21 nM. AS2444697 potently inhibits human and rat IRAK-4 activity. AS2444697 exhibits renoprotective effects through anti-inflammatory action.
|
-
- HY-16715
-
-
- HY-114309
-
-
- HY-N2188
-
-
- HY-B1046S
-
Clofazimine-d7
|
Bacterial
Antibiotic
|
Inflammation/Immunology
|
Clofazimine-d7 is deuterium labeled Clofazimine. Clofazimine is an iminophenazine dye, has a marked anti-inflammatory effect, has been used in combination with other antimycobacterial drugs to treat AIDS and Crohn's disease.
|
-
- HY-146577
-
-
- HY-15037S
-
Diclofenac-13C6 sodium heminonahydrate
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac-13C6 sodium heminonahydrate is the 13C-labeled Diclofenac Sodium. Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-108741A
-
Plecanatide acetate
|
Guanylate Cyclase
|
Inflammation/Immunology
|
Plecanatide acetate, an analogue of Uroguanylin, is an orally active guanylate cyclase-C (GC-C) receptor agonist. Plecanatide acetate activates GC-C receptors to stimulate cGMP synthesis with an EC50 of 190 nM in T84 cells assay. Plecanatide acetate can be used for the research of chronic idiopathic constipation, and it also shows anti-inflammatory activity in models of murine colitis.
|
-
- HY-142937
-
RORγt agonist 2
|
ROR
|
Inflammation/Immunology
|
RORγt agonist 2 is a potent agonist of RORγt. RORγt agonist 2 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 2 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136339A1, compound 17).
|
-
- HY-N0586A
-
Norisoboldine hydrochloride
(+)-Laurelliptine hydrochloride
|
Adenosine Receptor
|
Inflammation/Immunology
|
Norisoboldine hydrochloride is an orally active natural aryl hydrocarbon receptor (AhR) agonist. Norisoboldine hydrochloride, as a major isoquinoline alkaloid present in Radix Linderae, can be used for the research of Rheumatoid arthritis and Ulcerative colitis.
|
-
- HY-B0355
-
-
- HY-B1138
-
Fenbufen
CL-82204
|
COX
Caspase
|
Inflammation/Immunology
|
Fenbufen (CL-82204) is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.
|
-
- HY-109083
-
Cilofexor
GS-9674
|
FXR
Autophagy
|
Inflammation/Immunology
|
Cilofexor (GS-9674) is a potent, selective and orally active nonsteroidal FXR agonist with an EC50 of 43 nM. Cilofexor has anti-inflammatory and antifibrotic effects. Cilofexor has the potential for primary sclerosing cholangitis (PSC) and nonalcoholic steatohepatitis (NASH) research.
|
-
- HY-N10112
-
-
- HY-N7630
-
-
- HY-109520
-
Glatiramer acetate
|
Others
|
Inflammation/Immunology
|
Glatiramer acetate, a synthetic analogue of myelin basic protein and an immunomodulating agent, can be used for the research of multiple sclerosis. Glatiramer acetate exhibits strong and promiscuous binding to MHC molecules and consequent competition with various myelin antigens for their presentation to T cells. A further aspect of its action is potent induction of specific suppressor cells of the T helper 2 (Th2) type that migrate to the brain and lead to in situ bystander suppression.
|
-
- HY-136587
-
Oxomemazine
|
Histamine Receptor
mGluR
|
Inflammation/Immunology
|
Oxomemazine is a phenothiazine-based histamine H1-receptor blocker with pronounced antimuscarinic properties. Oxomemazine is a selective antagonist for muscarinic M1 receptor, displays about 20-fold difference in the affinity for high (Ki = 84 nM, M1 receptor) and low (Ki = 1.65 μM, M2 receptor) affinity sites. Oxomemazine an antihistamine and anticholinergic agent used for the study of cough treatment.
|
-
- HY-146581
-
Cathepsin C-IN-4
|
Cathepsin
|
Inflammation/Immunology
|
Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC50 of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC50 values of 203.4 and 177.6 nM, respectively.
|
-
- HY-119708
-
Ensifentrine
RPL-554
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
Ensifentrine (RPL-554) is an inhaled first-in-class dual inhibitor of phosphodiesterase 3 (PDE3) and PDE4 with IC50s of 0.4 nM and 1479 nM, respectively. Ensifentrine has bronchoprotective and anti-inflammatory activities. Ensifentrine can be used for chronic obstructive pulmonary disease (COPD) research.
|
-
- HY-120944
-
BAY-7598
|
MMP
|
Inflammation/Immunology
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
|
-
- HY-146168
-
Nrf2 activator-5
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities.
|
-
- HY-112401
-
-
- HY-120689
-
-
- HY-108847
-
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-17485
-
Alminoprofen
EB-382
|
Phospholipase
COX
|
Inflammation/Immunology
|
Alminoprofen (EB-382) is a nonsteroidal anti-inflammatory drug (NSAID) of the phenylpropionic acid class. Alminoprofen possesses a dual anti-inflammatory action, by inhibiting both secretory phospholipase A2 (sPLA2) and COX-2.
|
-
- HY-15036
-
Diclofenac
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-133968
-
24-Methylenecholesterol
Ostreasterol
|
Acyltransferase
|
Inflammation/Immunology
|
24-Methylenecholesterol (Ostreasterol), a natural marine sterol, stimulates cholesterol acyltransferase in human macrophages. 24-Methylenecholesterol possess anti-aging effects in yeast. 24-methylenecholesterol enhances honey bee longevity and improves nurse bee physiology.
|
-
- HY-131912
-
-
- HY-147811
-
-
- HY-19830
-
-
- HY-114041
-
Resolvin E1
RvE1
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production.
|
-
- HY-108693
-
-
- HY-N1871
-
-
- HY-P1558
-
-
- HY-142843
-
-
- HY-128171
-
Diflapolin
|
FLAP
Epoxide Hydrolase
|
Inflammation/Immunology
|
Diflapolin is a highly active dual 5-lipoxygenase-activating protein (FLAP)/soluble epoxide hydrolase (sEH) inhibitor with marked anti-inflammatory efficacy and high target selectivity. Diflapolin inhibits 5-LOX product formation in intact human monocytes and neutrophils with IC50s of 30 and 170 nM, respectively, and suppressed the activity of isolated sEH (IC50=20 nM).
|
-
- HY-N1178
-
-
- HY-N9182
-
Zeaxanthin dipalmitate
Physalien
|
Adiponectin Receptor
P2X Receptor
Autophagy
|
Inflammation/Immunology
|
Zeaxanthin dipalmitate (Physalien) is a wolfberry-derived carotenoid, has anti-inflammatory and anti-oxidative stress effects. Zeaxanthin dipalmitate directly interact with p2X7 receptor (Kd=81.2 nM) and adiponectin receptor 1 (AdipoR1; Kd=533 nM) in a positive dose-dependent manner. Zeaxanthin dipalmitate restores mitochondrial autophagy functions suppressed by ethanol intoxication. Zeaxanthin dipalmitate can be used in the research of alcoholic fatty liver disease (AFLD) and retinitis pigmentosa (RP).
|
-
- HY-101443
-
-
- HY-N10317
-
-
- HY-P9931
-
Guselkumab
CNTO 1959
|
Interleukin Related
|
Inflammation/Immunology
|
Guselkumab is a recombinant human IgG1 monoclonal antibody against the IL-23p19 subunit. Guselkumab binds to human and cynomolgus monkey IL-23 with Kd values of 3.3 and 1.9 pmol/L, respectively. Guselkumab inhibits production of cytokines lying downstream of the IL-23 signaling pathway and can be used for psoriatic arthritis research.
|
-
- HY-U00187
-
NCX1022
|
Others
|
Inflammation/Immunology
|
NCX1022 is an NO-releasing derivative of Hydrocortisone, which is the most widely used anti-inflammatory drug for the treatment of skin inflammation.
|
-
- HY-109177
-
Icenticaftor
QBW251
|
CFTR
|
Inflammation/Immunology
|
Icenticaftor (QBW251) is an orally active CFTR channel potentiator, with EC50s of 79 nM and 497 nM for F508del and G551D CFTR, respectively. Icenticaftor can be used for chronic obstructive pulmonary disease (COPD) and cystic fibrosis research.
|
-
- HY-50937
-
ST 2825
|
MyD88
|
Inflammation/Immunology
|
ST 2825 is a specific MyD88 dimerization inhibitor. ST2825 interferes with recruitment of IRAK1 and IRAK4 by MyD88, causing inhibition of IL-1β-mediated activation of NF-κB transcriptional activity.
|
-
- HY-N2110
-
Phellopterin
|
Others
|
Inflammation/Immunology
|
Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
|
-
- HY-133013
-
GLPG-3221
|
CFTR
|
Inflammation/Immunology
|
GLPG-3221 is a potent, orally active corrector of CFTR (cystic fibrosis transmembrane conductance regulator), with an EC50 of 105 nM. GLPG-3221 can be uesd for the treatment of cystic fibrosis.
|
-
- HY-147010
-
-
- HY-10456
-
TAK-715
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
TAK-715 is an orally active and potent p38 MAPK inhibitor with IC50s of 7.1 nM, 200 nM for p38α and p38β, respectively. TAK-715 inhibits casein kinase I (CK1δ/ε) to regulate activation of Wnt/β-catenin signaling. TAK-715 shows good significant efficacy in a rat arthritis model.
|
-
- HY-17042S
-
Cetirizine D4
|
Histamine Receptor
|
Inflammation/Immunology
|
Cetirizine D4 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
|
-
- HY-W010708S1
-
-
- HY-N8149
-
-
- HY-13315S
-
Montelukast-d6
MK0476-d6 free acid
|
Leukotriene Receptor
|
Inflammation/Immunology
|
Montelukast-d6 (MK0476-d6 free acid) is the deuterium labeled Montelukast (sodium). Montelukast sodium is a potent, selective and orally active antagonist of cysteinyl leukotriene receptor 1 (Cysltr1). Montelukast sodium can be used for the reseach of asthma and liver injury. Montelukast sodium also has an antioxidant effect in intestinal ischemia-reperfusion injury, and could reduce cardiac damage.
|
-
- HY-131705
-
-
- HY-19676
-
Pralnacasan
VX-740; HMR 3480
|
Caspase
|
Inflammation/Immunology
|
Pralnacasan (VX-740) is a potent, selective, non-peptide and orally active interleukin-1β converting enzyme (ICE, caspase 1) inhibitor with a Ki of 1.4 nM. Pralnacasan inhibits proinflammatory cytokines IL-18, IL-1β , and IFN-γ. Pralnacasan has the potential for osteoarthritis and rheumatoid arthritis treatment.
|
-
- HY-107004A
-
-
- HY-P1209
-
-
- HY-15898
-
-
- HY-144255
-
-
- HY-144397
-
LEO 134310
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
LEO 134310 is a selective, non-steroidal glucocorticoid receptor (GR) agonist optimized for topical treatment., LEO 134310 showed high affinity (EC50 of 14 nM) in a GR binding assay. LEO 134310 can be used for skin diseases.
|
-
- HY-N2114
-
-
- HY-B0890
-
Zomepirac sodium salt
McN-2783-21-98
|
PGE synthase
|
Inflammation/Immunology
|
Zomepirac sodium salt (McN-2783-21-98) is a potent prostaglandin biosynthesis inhibitor. Zomepirac sodium salt is a non-steroidal anti-inflammatory drug (NSAID). Zomepirac sodium salt can cause immune-mediated liver injury.
|
-
- HY-101410
-
-
- HY-10644
-
Lck inhibitor 2
|
Src
|
Inflammation/Immunology
|
Lck inhibitor 2 is a bis-anilinopyrimidine inhibitor of tyrosine kinases including LCK, BTK, LYN, SYK, and TXK. The IC50 values are 13nM, 9nM, 3nM, 26nM and 2nM for Lck, Btk, Lyn, Btk and Txk respectively
|
-
- HY-150747
-
ODN 6016
|
IFNAR
|
Inflammation/Immunology
|
ODN 6016 is a CpG-A oligonucleotides. ODN 6016 can induce IFN-α production, can be used for researching immune disorders including immunodeficiency caused by HIV-1. ODN 6016 sequence: T-sp-C-G-A-C-G-T-C-G-T-G-G-sp-G-sp-G-sp-G.
|
-
- HY-145990
-
FABPs ligand 6
MF6
|
FABP
|
Inflammation/Immunology
|
FABPs ligand 6 (MF6) is an FABP5 and FABP7 inhibitor with KD values of 874 nM and 20 nM, respectively. FABPs ligand 6 can be used for multiple sclerosis research.
|
-
- HY-B0574
-
Mefenamic acid
|
COX
|
Inflammation/Immunology
|
Mefenamic acid is a non-steroidal anti-inflammatory agent, acting as a competitive inhibitor of hCOX-1 and hCOX-2, with IC50s of 40 nM and 3 μM for hCOX-1 and hCOX-2, respectively.
|
-
- HY-100084
-
-
- HY-11067
-
-
- HY-B2179
-
-
- HY-111140
-
YS121
|
PGE synthase
Lipoxygenase
|
Inflammation/Immunology
|
YS121 is a dual inhibitor of microsomal prostaglandin E2 synthase-1 (mPGES-1; IC50=3.4 μM) and 5-lipoxygenase (5-LOX; IC50=6.5 μM). YS121 dose- dependently reduces PGE2 production with EC50=12 μM in IL-1β-stimulated A549 cells.
|
-
- HY-13075
-
-
- HY-N8217
-
-
- HY-N9969
-
-
- HY-103362
-
CCR2 antagonist 4 hydrochloride
Teijin compound 1 hydrochloride
|
CCR
|
Inflammation/Immunology
|
CCR2 antagonist 4 hydrochloride (Teijin compound 1 hydrochloride) is a potent and specific CCR2 antagonist, with IC50s of 180 nM for CCR2b. CCR2 antagonist 4 hydrochloride potently inhibits MCP-1-induced chemotaxis with an IC50 of 24 nM.
|
-
- HY-103483
-
-
- HY-145255
-
-
- HY-145310
-
-
- HY-W040265
-
Fenamic acid
N-Phenylanthranilic acid
|
Chloride Channel
|
Inflammation/Immunology
|
Fenamic acid (N-Phenylanthranilic acid, NPAA) is an orally active chloride channel blocker. Fenamic acid is the basic constituent of non-steroidal anti-inflammatory agents (NSAIA), and derives into mefenamic, tofenacin, flufenac acid and melofenac acid. Fenamic acid also acts as antibacterial and analgesic agent -.
|
-
- HY-N2055
-
-
- HY-N0904
-
Ginsenoside C-K
Ginsenoside compound K; Ginsenoside K
|
COX
NO Synthase
Cytochrome P450
|
Inflammation/Immunology
|
Ginsenoside C-K, a bacterial metabolite of G-Rb1, exhibits anti-inflammatory effects by reducing iNOS and COX-2. Ginsenoside C-K exhibits an inhibition against the activity of CYP2C9 and CYP2A6 in human liver microsomes with IC50s of 32.0±3.6 μM and 63.6±4.2 μM, respectively.
|
-
- HY-124029
-
MMP13-IN-3
|
MMP
|
Inflammation/Immunology
|
MMP13-IN-3 is a potent, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis. MMP13-IN-3 is >1000 selective over other MMPs.
|
-
- HY-126294
-
AZD4604
JAK1-IN-7
|
JAK
|
Inflammation/Immunology
|
AZD4604 (JAK1-IN-7) is a Janus-associated kinase 1 (JAK1) inhibitor extracted from patent WO2018134213A1, Example 63, has an anti-inflammatory effect.
|
-
- HY-113252S2
-
-
- HY-103046
-
UbcH5c-IN-1
|
E1/E2/E3 Enzyme
|
Inflammation/Immunology
|
UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
|
-
- HY-P99025
-
-
- HY-110133
-
JTE-607
|
Interleukin Related
|
Inflammation/Immunology
|
JTE-607, a highly selective inflammatory cytokine synthesis inhibitor, protects from endotoxin shock in mice. JTE-607 inhibits inflammatory cytokine production, including TNF-α, IL-1β, IL-6, IL-8 and IL-10, from LPS-stimulated human PBMCs, with IC50s of 11, 5.9, 8.8, 7.3 and 9.1 nM, respectively. Cleavage and Polyadenylation Specificity Factor 3 (CPSF3) is the target of JTE-607.
|
-
- HY-13402A
-
Varespladib sodium
LY315920 sodium
|
Phospholipase
|
Inflammation/Immunology
|
Varespladib sodium (LY315920 sodium) is a potent and selective group IIA, secretory phospholipase A2 (sPLA2) inhibitor with an IC50 of 9 nM. Varespladib sodium exhibits the significant inhibitory effect on sPLA2 activity in serum from various species including rat, rabbit, guinea pig and human with IC50s of 8.1 nM, 5.0 nM, 3.2 nM and 6.2 nM, respectively.
|
-
- HY-147733
-
-
- HY-100864
-
mPGES1-IN-3
|
PGE synthase
|
Inflammation/Immunology
|
mPGES1-IN-3 (Compound 17d) is a potent and selective microsomal prostaglandin E2 synthase-1 (mPGES-1) inhibitor, which exhibits excellent mPGES-1 enzyme (IC50: 8 nM), cell (A549 IC50: 16.24 nM) and human whole blood potency (IC50: 249.9 nM).
|
-
- HY-135678
-
-
- HY-101786
-
KZR-504
|
Proteasome
|
Inflammation/Immunology
|
KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
|
-
- HY-19223
-
-
- HY-103360
-
J-113863
|
CCR
|
Inflammation/Immunology
|
J-113863 is a potent and selective CCR1 (CD18) antagonist with IC50 values of 0.9 nM and 5.8 nM for human and mouse CCR1 receptors, respectively. J-113863 is also a potent antagonist of the human CCR3 (IC50 of 0.58 nM) , but a weak antagonist of the mouse CCR3 (IC50 of 460 nM). J-113863 is inactive against CCR2, CCR4 and CCR5, as well as the LTB4 or TNF-α receptors. Anti-inflammatory effect.
|
-
- HY-126145
-
-
- HY-N10196
-
-
- HY-113357
-
-
- HY-147922
-
hCAI/II-IN-2
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
hCAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with Ki values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
|
-
- HY-144738
-
Dual FAAH/sEH-IN-1
|
Epoxide Hydrolase
FAAH
|
Inflammation/Immunology
|
Dual FAAH/sEH-IN-1 (compound 3) is a high affinity dual sEH (soluble epoxide hydrolase) and FAAH (fatty acid amide hydrolase) inhibitor, with IC50 values of 9.6 and 7 nM, respectively. Dual FAAH/sEH-IN-1 shows antinociception against the inflammatory phase.
|
-
- HY-102084
-
LMT-28
|
Interleukin Related
|
Inflammation/Immunology
|
LMT-28 is an orally active and the first synthetic IL-6 inhibitor that functions through direct binding to gp130. LMT-28 shows low toxicity and selectively inhibits IL-6-induced phosphorylation of STAT3, JAK2, and gp130.
|
-
- HY-N0604
-
-
- HY-N1374
-
Magnolin
|
ERK
|
Inflammation/Immunology
|
Magnolin, a major component of Magnolia flos (Shin-Yi), inhibits the Ras/ERKs/RSK2 signaling axis by targeting the active pocket of ERK1 and ERK2 with IC50s of 87 nM and 16.5 nM, respectively.
|
-
- HY-B0288B
-
-
- HY-N4182
-
-
- HY-115466
-
-
- HY-N1429
-
-
- HY-142703
-
RORγt inverse agonist 28
|
ROR
|
Inflammation/Immunology
|
RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .
|
-
- HY-15762
-
Valdecoxib
SC 65872
|
COX
|
Inflammation/Immunology
|
Valdecoxib is a highly potent and selective inhibitor of COX-2, with IC50s of 5 nM and 140 μM for COX-2 and COX-1, respeceively. Valdecoxib can be used in the research of arthritis and pain.
|
-
- HY-W015600
-
-
- HY-B0580S1
-
Ketorolac D4
|
COX
|
Inflammation/Immunology
|
Ketorolac D4 (RS37619 D4) is the deuterium labeled Ketorolac. Ketorolac is a non-steroidal anti-inflammatory agent, acting as a nonselective COX inhibitor, with IC50s of 20 nM for COX-1 and 120 nM for COX-2.
|
-
- HY-138779
-
ICCB-19 hydrochloride
|
Autophagy
RIP kinase
Apoptosis
|
Inflammation/Immunology
|
ICCB-19 hydrochloride is a TRADD (TNFRSF1A associated via death domain) inhibitor. ICCB-19 hydrochloride binds with N-terminal domain of TRADD (TRADD-N), disrupting its binding to both TRADD-C and TRAF2. ICCB-19 hydrochloride is indirect inhibitor of RIPK1 kinase activity. ICCB-19 hydrochloride effectively induces autophagy and the degradation of long-lived proteins.
|
-
- HY-107784
-
Ectoine
|
Bacterial
|
Inflammation/Immunology
|
Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis.
|
-
- HY-P2519
-
-
- HY-111675
-
Ac-FLTD-CMK
|
Caspase
Pyroptosis
|
Inflammation/Immunology
|
Ac-FLTD-CMK, a gasdermin D (GSDMD)-derived inhibitor, is a specific inflammatory caspases inhibitor. Ac-FLTD-CMK is effective against caspases-1 (IC50 of 46.7 nM), caspases-4 (IC50 of 1.49 μM), caspases-5 (IC50 of 329 nM), and caspases-11 , but not the apoptotic caspases such as caspase-3.
|
-
- HY-121376
-
-
- HY-N1389
-
Carmine
Carmine red
|
Others
|
Inflammation/Immunology
|
Carmine (Carmine red), a natural red dye extracted from the dried females of the insect Dactylopius coccus var. Costa (cochineal). Carmine is a widely used food additive. Carmine provokes both an immediate hypersensitivity and a delayed systemic response with cutaneous expression.
|
-
- HY-150583
-
Chitin synthase inhibitor 2
|
Fungal
Antibiotic
|
Inflammation/Immunology
|
Chitin synthase inhibitor 2 (compound 2b) is a potent inhibitor of chitin synthase with the IC50 value of 0.09 mM and the Ki value of 0.12 mM. Chitin synthase inhibitor 2 has antimicrobial activities in vitro and shows synergistic or additive effects with fluconazole or polyoxin B.
|
-
- HY-101189B
-
JNJ-39758979 dihydrochloride
|
Histamine Receptor
|
Inflammation/Immunology
|
JNJ-39758979 dihydrochloride is a selective, orally active, and high-affinity histamine H4 receptor antagonist, with Kis of 12.5, 5.3, and 25 nM for human, mouse, and monkey histamine H4 receptor, respectively. JNJ-39758979 dihydrochloride functionally antagonizes histamine-induced cAMP inhibition with a pA2 of 7.9 in transfected cells. JNJ-39758979 dihydrochloride shows good anti-inflammatory and antipruritic activity.
|
-
- HY-16902
-
-
- HY-N0618
-
Sanggenon D
|
Others
|
Inflammation/Immunology
|
Sanggenon D is a Diels-Alder-type adduct from Chinese crude drug root bark of Morus cathayana. Sanggenon D possesses antioxidant and inhibits Pancreatic lipase (PL) with the an IC50 of 0.77 μM.
|
-
- HY-P9926
-
-
- HY-N7679
-
-
- HY-N0611
-
alpha-Boswellic acid
α-Boswellic acid
|
Others
|
Inflammation/Immunology
|
alpha-Boswellic acid (α-Boswellic acid) is a pentacyclic triterpene compound from extracts of Frankincense, has anticonvulsant and anti-cancer properties. alpha-Boswellic acid prevents and decreases the progression of Alzheimer’s hallmarks in vivo and can be used for Alzheimer’s disease research.
|
-
- HY-79128S
-
-
- HY-N0688
-
-
- HY-B1153A
-
-
- HY-N6588
-
3,4,5-Tricaffeoylquinic acid
3,4,5-triCQA
|
Akt
NF-κB
|
Inflammation/Immunology
|
3,4,5-Tricaffeoylquinic acid (3,4,5-triCQA) inhibits tumor necrosis factor-α-stimulated production of inflammatory mediators in keratinocytes via suppression of Akt- and NF-κB-pathways. 3,4,5-Tricaffeoylquinic acid induces cell cycle arrest at G0/G1, actin cytoskeleton organization, chromatin remodeling, neuronal differentiation, and bone morphogenetic protein signaling in human neural stem cells. 3,4,5-Tricaffeoylquinic acid has the potential for the research of aging-associated diseases.
|
-
- HY-122906
-
JTE-952
|
c-Fms
|
Inflammation/Immunology
|
JTE-952 is a potent, oral active and selective Type II inhibitor of colony stimulating factor-1 receptor (CSF-1R or cFMS, type III receptor tyrosine kinase), with IC50 values of 13 nM and 261 nM for CSF1R and TrkA , respectively. Effective against a mouse collagen-induced model of arthritis.
|
-
- HY-N0396
-
-
- HY-146382
-
-
- HY-146435
-
Anti-inflammatory agent 22
|
TNF Receptor
|
Inflammation/Immunology
|
Anti-inflammatory agent 22 (compound 14a) is an orally active anti-inflammatory agent. Anti-inflammatory agent 22 inhibits LPS-induced TNF-α production with an IC50 value of 14.6 μM. Anti-inflammatory agent 22 has preventive effects on lymphedematous tissue via suppression of adipogenesis. Anti-inflammatory agent 22 suppresses limb lymphedema volume in mice.
|
-
- HY-131945
-
-
- HY-U00275
-
-
- HY-124646
-
KIRA-7
|
IRE1
|
Inflammation/Immunology
|
KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect.
|
-
- HY-107390A
-
AX-024 hydrochloride
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-P3342
-
-
- HY-50674A
-
INCB3344 R-isomer
|
Others
CCR
|
Inflammation/Immunology
|
INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
|
-
- HY-111940
-
LUT014
|
Raf
|
Inflammation/Immunology
|
LUT014 is a B-Raf inhibitor with an IC50 of 11.7 nM, and developed to reduce dose-limiting acneiform lesions associated EGFR Inhibitors treatment. Extracted from patent WO 2019026065A2 .
|
-
- HY-129524
-
-
- HY-N3011
-
-
- HY-B2191
-
Sodium gualenate
Guaiazulenesulfonate sodium
|
Others
|
Inflammation/Immunology
|
Sodium gualenate (Guaiazulenesulfonate sodium) is a hydrophilic derivative of guaiazulene with excellent anti-inflammatory and wound-healing effects mainly used for the treatment of duodenal ulcer, gastric ulcer and gastritis.
|
-
- HY-137941
-
Roxatidine
|
Histamine Receptor
|
Inflammation/Immunology
|
Roxatidine is an active metabolite of Roxatidine acetate hydrochloride, is a histamine H2-receptor antagonist. Roxatidine, an anti-ulcer agent, suppresses histamine release (thus inhibiting proton secretion) and inhibits the production of VEGF-1, an important marker of inflammation and angiogenesis. Anti-allergic inflammatory effect.
|
-
- HY-106555
-
Protizinic acid
|
Phospholipase
|
Inflammation/Immunology
|
Protizinic acid is an orally active non-steroidal antiinflammatory agent with antiinflammatory and antipyretic activity. Protizinic acid inhibits phospholipase A2 (PLA2) activity, and the IC50 value is 210 μM.
|
-
- HY-135892
-
GNE-1858
|
MAP4K
|
Inflammation/Immunology
|
GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
|
-
- HY-16268S
-
Kartogenin-d4
KGN-d4
|
TGF-beta/Smad
|
Inflammation/Immunology
|
Kartogenin-d4 (KGN-d4) is the deuterium labeled Kartogenin. Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC50 of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).
|
-
- HY-122616
-
-
- HY-N1089
-
-
- HY-Y1250S5
-
Fmoc-Gly-OH-13C2
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Fmoc-Gly-OH-13C2 is a 13C-labeled Xanthine. Xanthine, a plant alkaloid found in tea, coffee, and cocoa, is a mild stimulant of the central nervous system. Xanthine also acts as an intermediate product on the pathway of purine degradation[1][2][3].
|
-
- HY-N2988A
-
-
- HY-119517
-
-
- HY-W173309
-
-
- HY-138651
-
-
- HY-146421
-
Anti-inflammatory agent 21
|
NO Synthase
NF-κB
Reactive Oxygen Species
|
Inflammation/Immunology
|
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model.
|
-
- HY-147660
-
IMMH001
|
LPL Receptor
|
Inflammation/Immunology
|
IMMH001, also called SYL930, is an orally active, potent and selective S1P1 (sphingosine-1-phosphate receptor 1) agonist. IMMH001 decreased levels of both chemokines and proinflammatory cytokines, including IL-1β, IL-5, IL-18, IP10, CCL3, and CCL5. IMMH001 can be used for rheumatoid arthritis (RA) research.
|
-
- HY-147742
-
Thi-DPPY
|
JAK
|
Inflammation/Immunology
|
Thi-DPPY (compound 8e) is a potent and orally active JAK3 inhibitor with IC50 values of 62.4, 1.38 nM for BTK, JAK, respectively. Thi-DPPY shows anti-proliferative activity against HBE cells. Thi-DPPY shows anti-inflammatory activity in vivo. Thi-DPPY has the potential for the research of idiopathic pulmonary fibrosis (IPF).
|
-
- HY-111748
-
-
- HY-146309
-
iNOS-IN-2
|
NO Synthase
|
Inflammation/Immunology
|
iNOS-IN-2 (Compound 53) is a potent down-regulator of inducible nitric oxide synthase (iNOS) protein. iNOS-IN-2 effectively inhibits the NO production (IC50=6.4 μM). iNOS-IN-2 has a potential therapeutic effect on chronic inflammation.
|
-
- HY-115966
-
COX-1/2-IN-1
|
COX
|
Inflammation/Immunology
|
COX-1/2-IN-2 is a potent COX1/2 inhibitor. COX-1/2-IN-2 exhibits significant inhibitory effect against COX-1 and COX-2 inhibitor with IC50 values of 13.9 ± 3.21 µM and 6.4±0.74 µM, respectively.
|
-
- HY-50949
-
-
- HY-100518
-
T-26c
|
MMP
|
Inflammation/Immunology
|
T-26c is highly potent and selective matrix metalloproteinase-13 (MMP-13) inhibitor with an IC50 of 6.75 pM and more than 2600-fold selectivity over the other related metalloenzymes.
|
-
- HY-N6927
-
Isoforskolin
Coleonol B
|
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
Isoforskolin is the principle active component of C. forskohlii native to China. Isoforskolin reduces the secretion of lipopolysaccharide (LPS)-induced cytokines, namely TNF-α, IL-1β, IL-6 and IL-8, in human mononuclear leukocytes. Isoforskolin acts as an anti-inflammatory agent for the treatment of Lyme arthritis.
|
-
- HY-12370
-
-
- HY-120878A
-
(R,R)-CXCR2-IN-2
|
CXCR
|
Inflammation/Immunology
|
(R,R)-CXCR2-IN-2, diastereoisomer of CXCR2-IN-2 (compound 68), is a brain penetrant CXCR2 antagonist with a pIC50 of 9 and 6.8 in the Tango assay and d in the HWB Gro-α induced CD11b expression assay, respectively.
|
-
- HY-16692
-
-
- HY-100754
-
-
- HY-15455S2
-
Roflumilast-d3
|
Phosphodiesterase (PDE)
RSV
|
Inflammation/Immunology
|
Roflumilast-d3 is deuterium labeled Roflumilast. Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
|
-
- HY-146134
-
-
- HY-18900
-
-
- HY-12453
-
-
- HY-N1094
-
Verminoside
|
PARP
MDM-2/p53
|
Inflammation/Immunology
|
Verminoside is an iridoid isolated from Kigelia africana, exhibits anti-inflammatory and remarkable antioxidant activity with a radical-scavenging activity of 2.5 μg/mL. The genotoxicity of Verminoside on human lymphocytes is associated with elevated levels of PARP-1 and p53 proteins.
|
-
- HY-109073
-
-
- HY-B1221S1
-
Flufenamic acid-13C6
|
COX
AMPK
Potassium Channel
Chloride Channel
Calcium Channel
Parasite
|
Inflammation/Immunology
|
Flufenamic acid-13C6 is the 13C6 labeled Flufenamic acid. Flufenamic acid is a non-steroidal anti-inflammatory agent, inhibits cyclooxygenase (COX), activates AMPK, and also modulates ion channels, blocking chloride channels and L-type Ca2+ channels, modulating non-selective cation channels (NSC), activating K+ channels. Flufenamic acid binds to the central pocket of TEAD2 YBD and inhibits both TEAD function and TEAD-YAP-dependent processes, such as cell migration and proliferation.
|
-
- HY-13463
-
Avatrombopag
AKR-501; E5501; YM477
|
Thrombopoietin Receptor
|
Inflammation/Immunology
|
Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A.
|
-
- HY-114412A
-
-
- HY-N0860
-
-
- HY-107091
-
Aspartyl-alanyl-diketopiperazine
DA-DKP
|
Others
|
Inflammation/Immunology
|
Aspartyl-alanyl-diketopiperazine (DA-DKP) is an immunomodulatory molecule generated by cleavage and cyclization from the N-terminus of human albumin and can modulate the inflammatory immune response through a molecular pathway implicated in T- lymphocyte anergy.
|
-
- HY-U00148
-
-
- HY-106628
-
Sudoxicam
|
COX
|
Inflammation/Immunology
|
Sudoxicam is a reversible and orally active COX antagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity.
|
-
- HY-N0029
-
Forsythoside B
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-112847A
-
Sulfosuccinimidyl oleate sodium
Sulfo-N-succinimidyl oleate sodium
|
Mitophagy
|
Inflammation/Immunology
|
Sulfosuccinimidyl oleate sodium (Sulfo-N-succinimidyl oleate sodium) is a long chain fatty acid that inhibits fatty acid transport into cells. Sulfosuccinimidyl oleate sodium is a potent and irreversible inhibitor of mitochondrial respiratory chain. Sulfosuccinimidyl oleate sodium binds the CD36 receptor on the surface of microglia. Anti-inflammatory effect.
|
-
- HY-104059
-
-
- HY-122168
-
-
- HY-122762
-
Cetraxate hydrochloride
DV-1006
|
Ser/Thr Protease
|
Inflammation/Immunology
|
Cetraxate hydrochloride (DV-1006), an orally active anti-ulcer agent with mucosal protective effects, can be used for gastric ulcers research. Cetraxate hydrochloride is a potent acrosomal proteinase acrosin inhibitor with a Ki and an IC50 of 0.94 μM and 3.3 μM, respectively.
|
-
- HY-135386
-
-
- HY-101872A
-
GSK-872 hydrochloride
|
RIP kinase
|
Inflammation/Immunology
|
GSK-872 hydrochloride is a RIPK3 inhibitor, which binds RIP3 kinase domain with an IC50 of 1.8 nM, and inhibits kinase activity with an IC50 of 1.3 nM. GSK-872 hydrochloride decreases the RIPK3-mediated necroptosis and subsequent cytoplasmic translocation and expression of HMGB1, as well as ameliorates brain edema and neurological deficits in early brain injury.
|
-
- HY-19120
-
KB-5492 anhydrous
|
Sigma Receptor
|
Inflammation/Immunology
|
KB-5492 anhydrous is a potent and selective inhibitor of sigma receptor, inhibits specific [ 3H]1,3-di(2-tolyl)guanidine (DTG) binding to the sigma receptor with an IC50 of 3.15 μM. KB-5492 anhydrous is an anti-ulcer agent.
|
-
- HY-N10114
-
-
- HY-N2204
-
Swertiajaponin
|
Tyrosinase
|
Inflammation/Immunology
|
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity.
|
-
- HY-114017
-
-
- HY-N2170
-
-
- HY-U00273
-
-
- HY-110177
-
SP-100030
|
NF-κB
|
Inflammation/Immunology
|
SP-100030 is a potent NF-κB and activator protein-1 (AP-1) double inhibitor (IC50s=50 and 50 nM, respectively). SP-100030 inhibits IL-2, IL-8, and TNF-alpha production in Jurkat and other T cell lines. SP-100030 decreases murine collagen-induced arthritis (CIA).
|
-
- HY-B0230S
-
Phenylbutazone(diphenyl-d10)
|
COX
|
Inflammation/Immunology
|
Phenylbutazone-d10 (diphenyl) is the deuterium labeled Phenylbutazone. Phenylbutazone is an efficient reducing cofactor for the peroxidase activity of prostaglandin H synthase (PHS). Phenylbutazone, a hepatotoxin, is a nonsteroidal anti-inflammatory drug (NSAID). Phenylbutazone induces muscle blind-like protein 1 (MBNL1) expression and has the potential for ankylosing spondylitis research.
|
-
- HY-N8469
-
-
- HY-100241
-
-
- HY-N1471
-
-
- HY-108659
-
NF340
|
P2Y Receptor
|
Inflammation/Immunology
|
NF340 is a potent and selective P2Y11 receptor antagonist. NF340 inhibits the activity of P2Y11R by completely combining with ATP-binding amino acid residues. NF340 ameliorates inflammation in human fibroblast-like synoviocytes and can be used for rheumatoid arthritis research.
|
-
- HY-B0553
-
Methazolamide
L584601
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
Methazolamide (L584601) is a sulfonamide derivative used as a carbonic anhydrase inhibitor with a Ki of 14 nM for human carbonic anhydrase II. Methazolamide, an intraocular pressure-lowering agent, reduces intraocular pressure elevations associated with glaucoma and other ocular disorders.
|
-
- HY-112179
-
GSK180
|
Others
|
Inflammation/Immunology
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition.
|
-
- HY-115976
-
COX-2-IN-10
|
COX
|
Inflammation/Immunology
|
COX-2-IN-10 is a potent COX-2 inhibitor. COX-2-IN-10 inhibits the production of PGE2 in concentration dependent manner (IC50=2.54 µM). COX-2-IN-10 inhibits the expression of iNOS and COX-2 on mRNA and protein level . COX-2-IN-10 inhibits the production of IL-6, TNF-α and IL-1β.
|
-
- HY-142847
-
-
- HY-121406
-
-
- HY-N0608A
-
(Rac)-Myrislignan
|
NF-κB
|
Inflammation/Immunology
|
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation.
|
-
- HY-P2319A
-
-
- HY-N4128
-
4''-methyloxy-Daidzin
Daidzein 7-O-Β-D-glucoside 4''-O-methylate
|
Others
|
Inflammation/Immunology
|
4''-methyloxy-Daidzin (Daidzein 7-O-Β-D-glucoside 4''-O-methylate), an isoflavone methyl-glycoside, is isolated from Cordyceps militaris grown on germinated soybeans. Isoflavones possess immunomodulating and antiallergic activities.
|
-
- HY-N2586
-
-
- HY-B0606
-
-
- HY-101427
-
-
- HY-10978
-
-
- HY-P3149B
-
LEESGGGLVQPGGSMK acetate
|
TNF Receptor
|
Inflammation/Immunology
|
LEESGGGLVQPGGSMK acetate, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK acetate can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.
|
-
- HY-N10217
-
-
- HY-Y0520S
-
Itaconic acid-13C5
|
Endogenous Metabolite
|
Inflammation/Immunology
|
Itaconic acid-13C5 is the 13C labeled Itaconic acid. Itaconic acid, a precursor of polymers, chemicals, and fuels, can be synthesized by many fungi. Itaconic acid also is a macrophage-specific metabolite. Itaconic acid mediates crosstalk between macrophage metabolism and peritoneal tumors.
|
-
- HY-N2279
-
Kurarinone
|
Others
|
Inflammation/Immunology
|
Kurarinone, a flavanoid derived from shrub Sophora flavescens, inhibits the process of experimental autoimmune encephalomyelitis via blocking Th1 and Th17 cell differentiation.
|
-
- HY-N0031
-
Plantamajoside
|
Others
|
Inflammation/Immunology
|
Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation.
|
-
- HY-107495
-
-
- HY-W014605
-
-
- HY-145896
-
-
- HY-103637
-
Vimirogant
VTP-43742
|
ROR
|
Inflammation/Immunology
|
Vimirogant (VTP-43742) is a potent, selective, and orally active RORγt inhibitor (Ki=3.5 nM; IC50=17 nM). Vimirogant exhibits >1000-fold selectivity versus the RORα and RORβ isotypes. Vimirogant inhibits Th17 differentiation and IL-17A secretion from mouse splenocytes (IC50=57 nM) without affecting Th1, Th2, or Treg cell differentiation. Vimirogant has the potential for autoimmune disorders research.
|
-
- HY-112267
-
-
- HY-P1194A
-
Spantide I TFA
|
Neurokinin Receptor
|
Inflammation/Immunology
|
Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
|
-
- HY-142032
-
RBM10-8
|
LPL Receptor
|
Inflammation/Immunology
|
RBM10-8 is irreversible inhibitor of recombinant human sphingosine-1-phosphate lyase (hS1PL) . Sphingosine-1-phosphate (S1P) is a sphingolipid (SL) that acts as a signaling molecule regulating diverse cellular processes such as cell proliferation and differentiation, angiogenesis, immune function, inflammation, and development.
|
-
- HY-124270
-
Sibenadet hydrochloride
AR-C68397AA
|
Dopamine Receptor
Adrenergic Receptor
|
Inflammation/Immunology
|
Sibenadet hydrochloride (AR-C68397AA) is a dual D2 dopamine receptor, beta2-adrenoceptor agonist with bronchodilator activity. Investigation in animal models of key chronic obstructive pulmonary disease (COPD) symptoms has demonstrated that Sibenadet hydrochloride effectively inhibits sensory nerve activity, thereby reducing reflex cough, mucus production and tachypnoea.
|
-
- HY-15035
-
S-Diclofenac
ACS 15; ATB-337
|
COX
|
Inflammation/Immunology
|
S-Diclofenac is a hybrid molecule of an H2S donor and the NSAID diclofenac. S-Diclofenac spares the gastric mucosa of injury despite markedly suppressing prostaglandin synthesis.
|
-
- HY-144773
-
-
- HY-143885
-
JAK1/TYK2-IN-3
|
JAK
|
Inflammation/Immunology
|
JAK1/TYK2-IN-3 is a potent, selective and orally active dual TYK2/JAK1 inhibitor with IC50 values of 6 and 37 nM, respectively. JAK1/TYK2-IN-3 also shows selectively relative to JAK2 (IC50=140 nM) and JAK3 (IC50=362 nM). JAK1/TYK2-IN-3 shows anti-inflammatory effect by regulating the expression of related TYK2/JAK1-regulated genes, as well as the formation of Th1, Th2, and Th17 cells.
|
-
- HY-120824
-
Mofezolac
|
COX
|
Inflammation/Immunology
|
Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities.
|
-
- HY-147923
-
hCAI/II-IN-3
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
hCAI/II-IN-3 (compound 5b) is a potent dual hCA I/II inhibitor with Ki values of 51.25, 13.15 and 42.18 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
|
-
- HY-P1505
-
-
- HY-147078
-
-
- HY-15123
-
-
- HY-100495
-
-
- HY-B0619
-
Zaltoprofen
CN100
|
COX
|
Inflammation/Immunology
|
Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
|
-
- HY-B1179
-
-
- HY-B0270S
-
-
- HY-120628
-
BMS-587101
|
Integrin
|
Inflammation/Immunology
|
BMS-587101 is a potent and orally active antagonist of leukocyte function associated antigen-1 (LFA-1). BMS-587101 has anti-inflammatory effects and can be used for rheumatoid arthritis research.
|
-
- HY-75035
-
-
- HY-130243
-
RORγt Inverse agonist 6
|
ROR
|
Inflammation/Immunology
|
RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo.
|
-
- HY-126675A
-
AS2863619
|
CDK
STAT
|
Inflammation/Immunology
|
AS2863619 enables conversion of antigen-specific effector/memory T cells into Foxp3 + regulatory T (Treg) cells for the treatment of various immunological diseases. AS2863619 is a potent, orally active cyclin-dependent kinase 8 (CDK8) and CDK19 inhibitor with IC50s of 0.61 nM and 4.28 nM, respectively. STAT5 activation enhanced by AS2863619 inhibition of CDK8/19, which consequently activates the Foxp3 gene.
|
-
- HY-50714
-
Quiflapon sodium
MK-591 sodium
|
FLAP
Apoptosis
|
Inflammation/Immunology
|
Quiflapon sodium (MK-591 sodium) is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor. Quiflapon sodium is an orally active Leukotriene biosynthesis inhibitor. Induces apoptosis.
|
-
- HY-107980
-
-
- HY-144277
-
-
- HY-11999
-
-
- HY-108528
-
-
- HY-N0037
-
-
- HY-111021A
-
ASP-4058 hydrochloride
|
LPL Receptor
|
Inflammation/Immunology
|
ASP-4058 hydrochloride is a next-generation, selective and orally active agonist for Sphingosine 1-Phosphate receptors 1 and 5 (S1P1 and S1P5), ameliorates rodent experimental autoimmune encephalomyelitis with a favorable safety profile.
|
-
- HY-130622
-
LT052
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
LT052 is a highly selective BET BD1 inhibitor with an IC50 of 87.7 nM. LT052 exhibits nanomolar BRD4 BD1 potency and 138-fold selectivity over BRD4 BD2 (IC50=12.130 μM). LT052 has anti-inflammatory activity and can be used for acute gout arthritis research.
|
-
- HY-120056
-
-
- HY-142938
-
RORγt agonist 3
|
ROR
|
Inflammation/Immunology
|
RORγt agonist 3 is a potent agonist of RORγt. RORγt agonist 3 promotes the differentiation of Th17 cells and enhances the levels of pro-inflammatory cytokines, thereby increasing the cytotoxicity of lymphocytes. RORγt agonist 3 inhibits the production of regulatory T cells, which suppresses the immune response (extracted from patent WO2021136326A1, compound 23).
|
-
- HY-138564
-
NOS-IN-1
|
NO Synthase
|
Inflammation/Immunology
|
NOS-IN-1 is a potent and orally active NO synthase (NOS) isoforms inhibitor with IC50s of 0.1 μM, 1.1 μM, and 0.2 μM for human iNOS (hiNOS), heNOS and hnNOS, respectively.
|
-
- HY-129944A
-
MJ33-OH lithium
|
Phospholipase
|
Inflammation/Immunology
|
MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6.
|
-
- HY-N4230
-
-
- HY-126329
-
AZD9898
|
Gutathione S-transferase
|
Inflammation/Immunology
|
AZD9898 is an orally active leukotriene-C4 synthetase (LTC4S, glutathione S-transferase II) inhibitor, with an IC50 of 0.28 nM. AZD9898 mitigates the GABA binding and hepatic toxicity signal. AZD9898 has the potential to treat asthma.
|
-
- HY-N0795
-
-
- HY-108346
-
JX401
|
p38 MAPK
|
Inflammation/Immunology
|
JX401 is a potent inhibitor of p38alpha, containing a 4-benzylpiperidine motif. p38alpha is hyperactive in inflammatory diseases, and various indications suggest that its inhibition would reverse inflammation. JX401 has the potential for the research of inflammation.
|
-
- HY-U00222
-
-
- HY-N0773
-
Isovitexin
Saponaretin; Homovitexin
|
JNK
NF-κB
|
Inflammation/Immunology
|
Isovitexin is a flavonoid isolated from rice hulls of Oryza sativa, possesses anti-inflammatory and anti-oxidant activities; Isovitexin acts like a JNK1/2 inhibitor and inhibits the activation of NF-κB.
|
-
- HY-W062109
-
Olopatadine
|
Endogenous Metabolite
Histamine Receptor
|
Inflammation/Immunology
|
Olopatadine is an orally active and selective histamine 1 (H1) receptor antagonist and a mast cell stabilizer. Olopatadine prevents immunologically stimulated pro-inflammatory mediator release from human conjunctival mast cells. Olopatadine can be used for researching allergic conjunctivitis.
|
-
- HY-101473
-
-
- HY-W092043
-
-
- HY-P1320A
-
[Nphe1]Nociceptin(1-13)NH2 TFA
|
Opioid Receptor
|
Inflammation/Immunology
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent.
|
-
- HY-107824
-
-
- HY-145686
-
ANKRD22-IN-1
|
Others
|
Inflammation/Immunology
|
ANKRD22-IN-1 is a potent inhibitor of ANKRD22. ANKRD22-IN-1 promotes the expansion of gastrointestinal mucosal epithelial stem cells and indirectly activates the Wnt classical pathway, which helps the recovery of damaged gastrointestinal mucosal tissues in the body (extracted from patent CN111205231B).
|
-
- HY-U00409
-
-
- HY-117959
-
TAK-615
|
LPL Receptor
|
Inflammation/Immunology
|
TAK-615 is a negative allosteric modulator (NAM) of the LPA1 receptor for the research of pulmonary fibrosis. TAK-615 binds the LPA1 receptor with high affinity (Kd high affinity of 1.7 nM and Kd low affinity of 14.5 nM).
|
-
- HY-147518
-
p38-α MAPK-IN-5
|
p38 MAPK
|
Inflammation/Immunology
|
p38-α MAPK-IN-5 (compound 4e) is a potent p38α inhibitor with IC50s of 0.1 nM, 0.2 nM, 944 nM, 4100 nM for p38α, p38 β, p38γ, p38δ, respectively. p38-α MAPK-IN-5 has anti-inflammatory effect. p38-α MAPK-IN-5 has the potential for asthma and chronic obstructive pulmonary disease (COPD) research.
|
-
- HY-104021
-
GSK840
GSK'840
|
RIP kinase
|
Inflammation/Immunology
|
GSK840 (GSK'840) is a receptor-interacting protein kinase 3 (RIP3 or RIPK3) inhibitor, which binds RIP3 kinase domain with an IC50 of 0.9 nM, and inhibits kinase activity with an IC50 of 0.3 nM.
|
-
- HY-N2478
-
Taraxasteryl acetate
|
Others
|
Inflammation/Immunology
|
Taraxasteryl acetate is isolated from P. sagittalis,and has a broad spectrum of anti-inflammatory activity. Taraxasteryl acetate relieves dextran, zymosan and arachidonic acid induced rat hind-paw edema. Taraxasteryl acetate can be used for the topical inflammation treatment[1] .
|
-
- HY-109804
-
CORM-401
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
CORM-401 is an oxidant-sensitive CO-releasing molecule. CORM-401 induces NO increase in the regulation of endothelial calcium signalling. CORM-401 reduces TNF-α/CHX and H2O2-induced ROS production. CORM-401 uncouples mitochondrial respiration and inhibits glycolysis.
|
-
- HY-N3602
-
Cleroindicin F
(-)-Rengyolone
|
Bacterial
|
Inflammation/Immunology
|
Cleroindicin F ((-)-Rengyolone), a cleroindicin, is an antimicrobial agent. Cleroindicin F shows relatively high anticandidal activity against Candida strains with a MIC value down to 12.5 µg/mL.
|
-
- HY-U00235
-
SR121566A
|
Integrin
|
Inflammation/Immunology
|
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
|
-
- HY-124759
-
-
- HY-N1981S
-
-
- HY-145434
-
-
- HY-B0619S1
-
Zaltoprofen-13C,d3
|
COX
|
Inflammation/Immunology
|
Zaltoprofen-13C,d3 is the 13C- and deuterium labeled Zaltoprofen. Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
|
-
- HY-145997
-
MRGPRX4 modulator-1
|
Others
|
Inflammation/Immunology
|
MRGPRX4 modulator-1 (compound 31-2) is a potent mas-related g-protein receptor X4 (MRGPR X4) modulator, with antagonist activity of IC50 < 100 nM for MRGPR4. MRGPRX4 modulator-1 can be used for researching MRGPR X4 dependent diseases such as itch, pain, and autoimmune disorders.
|
-
- HY-15642
-
-
- HY-N6710
-
-
- HY-N0358
-
-
- HY-P2477
-
-
- HY-17042S1
-
Cetirizine D8
|
Histamine Receptor
|
Inflammation/Immunology
|
Cetirizine D8 is a deuterium labeled Cetirizine. Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.
|
-
- HY-15307A
-
Belumosudil mesylate
KD025 mesylate; SLx-2119 mesylate
|
ROCK
|
Inflammation/Immunology
|
Belumosudil mesylate (KD025 mesylate) is a selective inhibitor of ROCK2 with IC50s of 105 nM and 24 µM for ROCK2 and ROCK1, respectively. Anti-fibrotic properties.
|
-
- HY-13577A
-
Oclacitinib maleate
PF-03394197 maleate
|
JAK
|
Inflammation/Immunology
|
Oclacitinib maleate (PF-03394197 maleate) is a novel JAK inhibitor. Oclacitinib maleate (PF-03394197 maleate) is most potent at inhibiting JAK1 (IC50=10 nM).
|
-
- HY-19427A
-
-
- HY-100958
-
-
- HY-13205
-
Belnacasan
VX-765
|
Caspase
|
Inflammation/Immunology
|
Belnacasan (VX-765) is an orally bioactive prodrug of VRT-043198, which is a potent and selective inhibitor of IL-converting enzyme (ICE)/caspase-1 with Kis of 0.8 nM and less than 0.6 nM for caspase-1 and caspase-4, respectively. Belnacasan (VX-765) inhibits the release of LPS-induced IL-1β and IL-18 by human PBMCs with an IC50 of ~0.7 μM.
|
-
- HY-147936
-
TP0556351
|
MMP
|
Inflammation/Immunology
|
TP0556351 is a potent and selective matrix metalloproteinase-2 (MMP2) inhibitor with an IC50 value of 0.2 nM. TP0556351 reduces the amount of collagen in the lungs of a Bleomycin-induced pulmonary fibrosis mouse model. TP0556351 can be used for researching idiopathic pulmonary fibrosis (IPF).
|
-
- HY-108666
-
-
- HY-146371
-
COX-2-IN-13
|
COX
|
Inflammation/Immunology
|
COX-2-IN-13 (compound 13e) is a potent and selective inhibitor of COX-2 with an IC50 of 0.98 μM. COX-2-IN-13 is an anti-inflammatory agent. COX-2-IN-13 shows safety in-vivo acute toxicity study.
|
-
- HY-B0758
-
Troxipide
|
Others
|
Inflammation/Immunology
|
Troxipide is an orally active defensive factor-enhancing therapeutic agent for gastritis and gastric ulcer (GU). Troxipide is a non-antisecretory gastro protective agent with antiulcer, anti-inflammatory and mucus-secreting properties.
|
-
- HY-N1508
-
Ecliptasaponin A
|
Others
|
Inflammation/Immunology
|
Ecliptasaponin A , a pentacyclic triterpenoid saponin, is one of major compounds separated from Eclipta prostrate. Eclipta prostrate is considered as a nourishing herbal medicine with pleiotropic effects, including anti-inflammatory, hepatoprotective, antioxidant, and immunomodulatory.
|
-
- HY-133672
-
-
- HY-N0594
-
Deacetylasperulosidic Acid
|
Interleukin Related
|
Inflammation/Immunology
|
Deacetylasperulosidic acid (DAA) is a major phytochemical constituent of Morinda citrifolia fruit. Deacetylasperulosidic acidhas antioxidant activity by increasing superoxide dismutase activity. Deacetylasperulosidic acid has anticlastogenic activity, suppressing the induction of chromosome aberrations in hamster ovary cells and mice. Deacetylasperulosidic acid prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells.
|
-
- HY-15234
-
Fluticasone furoate
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
Fluticasone furoate is a topical, intranasal, enhanced-affinity synthetic trifluorinated corticosteroid with a Kd of 0.3 nM. Fluticasone furoate has potent anti-inflamatory and anti-asthmatic activity, and low systemic exposure. Fluticasone furoate has the potential for allergic rhinitis treatment.
|
-
- HY-108330
-
AG126
Tyrphostin AG126
|
ERK
|
Inflammation/Immunology
|
AG126 is a tyrosine kinase inhibitor which can prevent the activation of mitogen-activated protein kinase p42MAPK (ERK2).
|
-
- HY-101793
-
-
- HY-78131A
-
(S)-(+)-Ibuprofen
(S)-Ibuprofen
|
COX
|
Inflammation/Immunology
|
(S)-(+)-Ibuprofen ((S)-Ibuprofen), a S(+)-enantiomer of Ibuprofen, is a potent COX-1 and COX-2 inhibitor with IC50s of 2.1 μM and 1.6 μM, respectively. (S)-(+)-Ibuprofen has analgesic, anti-inflammatory, anticancer and antipyretic effects.
|
-
- HY-N3003
-
-
- HY-141537
-
ABR-238901
|
Others
|
Inflammation/Immunology
|
ABR-238901 is an orally active and potent S100A8/A9 blocker and inhibits S100A8/A9 interaction with its receptors RAGE (receptor for advanced glycation endproducts) and TLR4 (toll-like receptor 4). ABR-238901 has the potential for myocardial infarction (MI) research.
|
-
- HY-15546
-
BMS-817399
|
CCR
|
Inflammation/Immunology
|
BMS-817399 is a potent, selective, and orally bioavailable CCR1 antagonist. BMS-817399 exhibits CCR1 binding affinity and chemotaxis inhibition potencies of 1 and 6 nM (IC50), respectively. BMS-817399 can be used for the research of rheumatoid arthritis.
|
-
- HY-108617
-
YM976
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
YM976 is a phosphodiesterase 4 (PDE4) inhibitor with an IC50 of 2.2 nM. YM976 shows the dissociation of anti-inflammatory activities from emetic effects and inhibits the antigen-induced airway responses.
|
-
- HY-16268
-
Kartogenin
KGN
|
TGF-beta/Smad
|
Inflammation/Immunology
|
Kartogenin (KGN) is an inducer of differentiation of human mesenchymal stem cells into chondrocytes, with an EC50 of 100 nM. Kartogenin binds filamin A, disrupts its interaction with the transcription factor core-binding factor β subunit (CBFβ), and induces chondrogenesis by regulating the CBFβ-RUNX1 transcriptional program. Kartogenin can be used for the research of osteoarthritis (OA).
|
-
- HY-10408
-
Ki20227
|
c-Fms
VEGFR
c-Kit
PDGFR
|
Inflammation/Immunology
|
Ki20227 is an orally active and highly selective c-Fms tyrosine kinase (CSF1R) inhibitor with IC50s of 2 nM, 12 nM, 451 and 217 nM for CSF1R, VEGFR2 (vascular endothelial growth factor receptor-2), c-Kit (stem cell factor receptor) and PDGFRβ (platelet-derived growth factor receptor β). Ki20227 suppresses osteoclast differentiation and osteolytic bone destruction.
|
-
- HY-131342
-
BIIB068
|
Btk
|
Inflammation/Immunology
|
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research.
|
-
- HY-12326B
-
c-di-AMP diammonium
Cyclic diadenylate diammonium; Cyclic-di-AMP diammonium
|
STING
Bacterial
Endogenous Metabolite
|
Inflammation/Immunology
|
c-di-AMP diammonium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP diammonium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP diammonium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
|
-
- HY-19562
-
-
- HY-116282A
-
-
- HY-143892
-
-
- HY-139675
-
-
- HY-P9927
-
Secukinumab
AIN457
|
Interleukin Related
|
Inflammation/Immunology
|
Secukinumab (AIN457) is a high affinity, human monoclonal antibody targeted against interleukin (IL)-17A. Secukinumab is the first-in-class anti-IL-17 agent used for the research of plaque psoriasis, ankylosing spondylitis and psoriatic arthritis.
|
-
- HY-139588
-
-
- HY-D0803
-
Thymoquinone
|
Others
|
Inflammation/Immunology
|
Thymoquinone is a nature product isolated from N. sativa. Thymoquinone possess antioxidant, anti-inflammatory, anti-cancer, antitumor activities and hepatoprotective properties.
|
-
- HY-119447
-
Mavacoxib
|
COX
|
Inflammation/Immunology
|
Mavacoxib is a selective, oral long-acting cyclooxygenase-2 (COX-2) inhibitor and a long-acting non-steroidal anti-inflammatory drug (NSAID). Mavacoxib is used to treat pain and inflammation associated with degenerative joint disease in dogs.
|
-
- HY-N10297
-
-
- HY-143420
-
ATX inhibitor 15
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model.
|
-
- HY-14113
-
-
- HY-15427
-
GDC-0834
|
Btk
|
Inflammation/Immunology
|
GDC-0834 is a potent and selective BTK inhibitor. GDC-0834 inhibits BTK with an in vitro IC50 of 5.9 and 6.4 nM in biochemical and cellular assays, respectively, and in vivo IC50 of 1.1 and 5.6 μM in mouse and rat, respectively.
|
-
- HY-19778A
-
-
- HY-103715
-
NLRP3 modulators 1
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
NLRP3 modulators 1 is the potent modulator of NLRP3. NLRP3 modulators 1 agonizes or partially agonizes NLRP3 that are useful for researching a condition, disease or disorder in which a decrease in LRP3 activity contributes to the pathology (extracted from patent WO2017184746A1, compound 107).
|
-
- HY-10569
-
Ponesimod
ACT-128800
|
LPL Receptor
|
Inflammation/Immunology
|
Ponesimod (ACT-128800) is a potent, selective and orally active agonist of S1P1, with an IC50 of 6 nM in a radioligand binding assay. Ponesimod activates S1P1-mediated signal transduction with high potency (EC50=5.7 nM). Ponesimod can protect against lymphocyte-mediated tissue inflammation.
|
-
- HY-132599
-
Lademirsen
SAR339375; RG-012
|
MicroRNA
|
Inflammation/Immunology
|
Lademirsen (SAR339375; RG-012) is a single stranded, chemically modified oligonucleotide that binds to and inhibits the function of miR-21. Lademirsen has the potential for Alport nephropathy research.
|
-
- HY-135654
-
-
- HY-121362
-
-
- HY-131579
-
-
- HY-N0131
-
-
- HY-105028
-
Tenidap
CP-66248
|
COX
|
Inflammation/Immunology
|
Tenidap, a non-steroidal anti-inflammatory drug, is a selective COX-1 inhibitor, with IC50 values of 0.03 µM and 1.2 µM for COX-1 and COX-2, respectively. Tenidap has anti-inflammatory and antirheumatic properties. Tenidap is also a specific SLC26A3 inhibitor.
|
-
- HY-144058
-
JAK-IN-18
|
JAK
|
Inflammation/Immunology
|
JAK-IN-18 is a potent inhibitor of JAK. JAK-IN-18 is useful for the research of multiple diseases, particularly ocular, skin, and respiratory diseases (extracted from patent WO2018204238A1, compound 1).
|
-
- HY-143452
-
MtTMPK-IN-4
|
Tyrosinase
Bacterial
|
Inflammation/Immunology
|
MtTMPK-IN-4 (compound 2), a para-piperidine, is a potent mycobacterium tuberculosis thymidylate kinase (MtTMPK) inhibitor with an IC50 of 6.1 μM. MtTMPK-IN-4 is a potent tyrosinase inhibitor. MtTMPK-IN-4 is a potent antibacterial agent.
|
-
- HY-17482
-
Difenpiramide
Z-876
|
Others
|
Inflammation/Immunology
|
Difenpiramide (Z-876) is a bisphenylalcanoic derivative with marked anti-inflammatory, analgesic, antipyretic and uricosuric properties. Difenpiramide has platelet anti-aggregation activity.
|
-
- HY-108966
-
Kushenol C
|
Beta-secretase
|
Inflammation/Immunology
|
Kushenol C, isolated from the roots of Sophora flavescens, shows anti-Inflammatory and anti-oxidative stress activities. Kushenol C inhibits BACE1 (β-site APP cleaving enzyme 1) with an IC50 of 5.45 µM.
|
-
- HY-P0266B
-
-
- HY-142834
-
-
- HY-119721
-
-
- HY-115510
-
SPR inhibitor 3
SPRi3
|
Others
|
Inflammation/Immunology
|
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
|
-
- HY-N1940
-
β-Anhydroicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
|
-
- HY-13278A
-
-
- HY-W440039
-
-
- HY-19359
-
ZED-1227
|
Glutaminase
|
Inflammation/Immunology
|
ZED-1227 is a specific and orally active transglutaminase 2 (TG2) inhibitor, with an IC50 of 45 nM. ZED-1227 can block inflammation-induced TG2 expression and activity. ZED-1227 can be used for the research of celiac disease (CeD).
|
-
- HY-N2169
-
Polygalasaponin V
|
Others
|
Inflammation/Immunology
|
Polygalasaponin V is a triterpenoid saponin isolated from the aerial parts of Polygala japonica. Polygala japonica has been a folk medicine herb used as expectorant, anti-inflammatory, antibacterial and antidepressant agents in the south of China.
|
-
- HY-111360
-
SPL-707
|
γ-secretase
|
Inflammation/Immunology
|
SPL-707 is an orally active, selective signal peptide peptidase-like 2a (SPPL2a) inhibitor with an IC50 of 77 nM for hSPPL2a. SPL-707 inhibits γ-secretase (IC50=6.1 μM) and SPP (IC50=3.7 μM). SPL-707 has the potential for autoimmune diseases research by targeting B cells and dendritic cells.
|
-
- HY-18325
-
-
- HY-139202
-
XVA143
|
Integrin
|
Inflammation/Immunology
|
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo.
|
-
- HY-150751
-
ODN TTAGGG
ODN A151
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
ODN TTAGGG (A151), inhibitory oligonucleotide (ODN), is a TLR9, AIM2 and cGAS antagonist. ODN TTAGGG is immunosuppressive and inhibits AIM2 inflammasome activation, as well as cGAS activation, by competing with DNA. ODN TTAGGG can be used in the study of lupus erythematosus and other related autoimmune diseases. ODN TTAGGG sequence: 5'-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-T-T-A-G-G-G-3'.
|
-
- HY-141692A
-
-
- HY-113953
-
Z-Asp-CH2-DCB
|
Caspase
|
Inflammation/Immunology
|
Z-Asp-CH2-DCB is an irreversible broad spectrum caspase inhibitor. Z-Asp-CH2-DCB also inhibits proteases with caspase-like activity. Z-D-CH2-DCB blocks the production of IL-1β, TNF-α, IL-6, and IFN-γ in staphylococcal enterotoxin B (SEB)-stimulated peripheral blood mononuclear cells (PBMC), and reduces SEB-1-stimulated T-cell proliferation in a dose-dependent manner. Z-Asp-CH2-DCB prevents SU5416-induced septal cell apoptosis and emphysema development.
|
-
- HY-N2285
-
-
- HY-N10214
-
-
- HY-13452
-
-
- HY-N7036S
-
Rhamnetin-d3
|
Phospholipase
|
Inflammation/Immunology
|
Rhamnetin-d3 is the deuterium labeled Rhamnetin. Rhamnetin is a quercetin derivative found in Coriandrum sativum, inhibits secretory phospholipase A2, with antioxidant and anti-inflammatory activity.
|
-
- HY-N7518
-
-
- HY-103672
-
-
- HY-142686
-
SGK1-IN-3
|
SGK
|
Inflammation/Immunology
|
SGK1-IN-3 (compound 3a) is a potent and orally active inhibitor of SGK1. The serine/threonine kinase SGK1 is an activator of the β-catenin pathway and a powerful stimulator of cartilage degradation that is found to be upregulated under genomic control in diseased osteoarthritic cartilage. SGK1-IN-3 has the potential for the research of osteoarthritis.
|
-
- HY-100444
-
SIS3 free base
|
TGF-beta/Smad
|
Inflammation/Immunology
|
SIS3 free base is a potent and selective inhibitor of Smad3 phosphorylation. SIS3 free base inhibits the myofibroblast differentiation of fibroblasts by TGF-β1. SIS3 free base does not affect the phosphorylation of Smad2.
|
-
- HY-78131AS
-
(S)-(+)-Ibuprofen D3
(S)-Ibuprofen D3
|
COX
|
Inflammation/Immunology
|
(S)-(+)-Ibuprofen D3 ((S)-Ibuprofen D3) is a deuterium labeled (S)-(+)-Ibuprofen. (S)-(+)-Ibuprofen is the S(+)-enantiomer of Ibuprofen that inhibits COX-1 and COX-2 activity with IC50s of 2.1 μM and 1.6 μM. (S)-(+)-Ibuprofen has analgesic, antiinflammatory and antipyretic effects.
|
-
- HY-15028
-
Otenaproxesul
ATB-346
|
COX
Apoptosis
|
Inflammation/Immunology
|
Otenaproxesul (ATB-346), an orally active non-steroidal anti-inflammatory drug (NSAID), inhibits cyclooxygenase-1 and 2 (COX-1 and 2). Otenaproxesul possesses antiinflammatory and antinociceptive activities.
|
-
- HY-114307
-
-
- HY-W020790
-
Sialyl-Lewis X
sLeX
|
Others
|
Inflammation/Immunology
|
Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin). Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability to inhibits CD62-mediated neutrophil recruitment to sites of inflammation.
|
-
- HY-114286A
-
PXS-5153A monohydrochloride
|
Monoamine Oxidase
|
Inflammation/Immunology
|
PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.
|
-
- HY-114286
-
PXS-5153A
|
Monoamine Oxidase
|
Inflammation/Immunology
|
PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.
|
-
- HY-137451A
-
-
- HY-N0768
-
-
- HY-N0181
-
-
- HY-19017
-
-
- HY-149025
-
DPTIP-prodrug 18
P18
|
Phospholipase
|
Inflammation/Immunology
|
DPTIP-prodrug 18 (P18) is a orally active and brain-penetrable prodrug of DPTIP (HY-131002). DPTIP-prodrug 18 is a potent nSMase2 inhibitor. DPTIP-prodrug 18 significantly inhibits IL-1β-induced EV (extracellular vesicle) release by inhibition of nSMase2 (neutral sphingomyelinase-2) activity. DPTIP-prodrug 18 can be used for brain injury research.
|
-
- HY-139703
-
-
- HY-N5042
-
-
- HY-N0924
-
(±)-Stylopine
Tetrahydrocoptisine
|
Others
|
Inflammation/Immunology
|
(±)-Stylopine (Tetrahydrocoptisine) is an alkaloid compound originally isolated from Corydalis tubers that exhibits anti-inflammatory and anti-parasitic activities.
|
-
- HY-112050
-
-
- HY-19622
-
PF-9184
|
PGE synthase
|
Inflammation/Immunology
|
PF-9184 is a potent and highly selective inhibitor of human microsomal prostaglandin E synthase-1 (mPGES-1), with an IC50 of 16.5 nM. PF-9184 inhibits IL-1β-induced PGE2 synthesis in vitro.
|
-
- HY-114200
-
Imrecoxib
BAP-909
|
COX
|
Inflammation/Immunology
|
Imrecoxib (BAP-909) is a novel and selective cyclooxygenase 2 (COX-2) inhibitor with an IC50 value of 18 nM, it also inhibits COX1- activity with an IC50 value of 115 nM. Imrecoxib (BAP-909) has anti-inflammatory effect.
|
-
- HY-B0482S
-
Acemetacin-d4
|
COX
|
Inflammation/Immunology
|
Acemetacin-d4 is the deuterium labeled Acemetacin. Acemetacin (TVX 1322) is a non-steroidal anti-inflammatory drug and a glycolic acid ester of indometacin that is a cyclooxygenase inhibitor.
|
-
- HY-111582
-
BBIQ
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
BBIQ is a imidazoquinoline compound and a potent and selectively toll-like receptor 7 (TLR7) agonist with an EC50 of 59.1 nM for human TLR7. BBIQ is a powerful vaccine adjuvant that enhances innate immune responses.
|
-
- HY-B0578S
-
Loxoprofen-d4
|
COX
|
Inflammation/Immunology
|
Loxoprofen-d4 is deuterium labeled Loxoprofen. Loxoprofen is a non-steroidal anti-inflammatory agent with analgesic and anti-pyretic properties. Loxoprofen sodium is a nonselective COX inhibitor with IC50s of 6.5 and 13.5 μM for COX-1 and COX-2, respectively.
|
-
- HY-12791
-
-
- HY-107355
-
Letosteine
|
|
Inflammation/Immunology
|
Letosteine is an orally active, potent and safe expectorant. Letosteine dissolves bronchial mucus and reduces respiratory inflammation symptoms, and restores gas exchanges and natural defense mechanisms in the lung. Letosteine can be used for acute or chronic respiratory diseases (such as bronchopneumopathies) research.
|
-
- HY-145988
-
COX-2-IN-11
|
COX
|
Inflammation/Immunology
|
COX-2-IN-11 (compound 7b2) is a potent and selective inhibitor of COX-2. COX-2-IN-11 has the potential for the research of inflammation diseases.
|
-
- HY-N0184A
-
-
- HY-W002484
-
3-Hydroxy-4-methoxyacetophenone
Acetoisovanillone; Isoacetovanillone
|
Others
|
Inflammation/Immunology
|
3-Hydroxy-4-methoxyacetophenone(Acetoisovanillone; Isoacetovanillone) is an active compound isolated from P. spinosa. Isoacetovanillone possesses anti-inflammatory activity and prevented injuries due to administration of acetic acid in the colon.
|
-
- HY-N6261
-
Epimagnolin B
|
Others
|
Inflammation/Immunology
|
Epimagnolin B is a bisepoxylignan isolated from Magnolia fargesii, with anti-inflammatory activity and antiallergic effects. Epimagnolin B inhibits NO production in LPS-activated microglia. Epimagnolin B exhibited antiallergic effects.
|
-
- HY-108642B
-
AMG-548 dihydrochloride
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
|
-
- HY-117433S
-
-
- HY-N7688
-
-
- HY-131974
-
-
- HY-120438
-
TASP0415914
|
PI3K
Akt
|
Inflammation/Immunology
|
TASP0415914 is a potent and orally active PI3Kγ inhibitor with an IC50 of 29 nM. TASP0415914 also shows potent Akt inhibitory activities with an IC50 of 294 nM. TASP0415914 can be used for inflammatory diseases research.
|
-
- HY-139709
-
-
- HY-N1521
-
Rehmannic acid
Lantadene A
|
Others
|
Inflammation/Immunology
|
Rehmannic acid (lantadene A) is a compound isolated from Lantana camara. Rehmannic acid shows considerable in vitro antioxidant, free radical scavenging capacity activities in a dose dependant manner. Rehmannic acid is a promising candidate for use as an antioxidant and hepatoprotective agent.
|
-
- HY-103386
-
FR122047
|
COX
|
Inflammation/Immunology
|
FR122047 (hydrochloride) is a selective and oral active inhibitor of COX-1 with an IC50 of 28 nM. FR122047 hydrochloride has antiplatelet, analgesic and anti-inflammatory effects in vivo.
|
-
- HY-U00405
-
-
- HY-138161
-
JR14a
|
Complement System
|
Inflammation/Immunology
|
JR14a is a potent thiophene antagonist of human complement C3a receptor. JR14a shows selectivity for the human C3a receptor over C5a receptor. JR14a can suppress C3aR-mediated inflammation.
|
-
- HY-N2488
-
-
- HY-10405S
-
Pamapimod-d4
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
Pamapimod-d4 (Ro4402257-d4) is the deuterium labeled Pamapimod. Pamapimod (Ro4402257) is a potent, selective and orally active p38 MAPK inhibitor with IC50s of 14 nM and 480 nM and Kis of 1.3 nM and 120 nM for p38α and p38β, respectively. Pamapimod has no activity against p38δ or p38γ isoforms. Pamapimod has the potential for rheumatoid arthritis and other autoimmune diseases treatment.
|
-
- HY-N0272
-
-
- HY-N10386
-
-
- HY-D1287
-
-
- HY-13662BS
-
(R)-Lansoprazole-d4
Dexlansoprazole-d4
|
Proton Pump
|
Inflammation/Immunology
|
(R)-Lansoprazole-d4 is deuterium labeled (R)-Lansoprazole. (R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-145728
-
Alicaforsen
ISIS-2302
|
Integrin
|
Inflammation/Immunology
|
Alicaforsen is a 20-base antisense oligonucleotide inhibiting ICAM-1 production, which is an important adhesion molecule involved in leukocyte migration and trafficking to the site of inflammation.
|
-
- HY-108642
-
AMG-548
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
|
-
- HY-112390A
-
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-117432
-
-
- HY-N2367
-
-
- HY-126361
-
ZK824190
|
Ser/Thr Protease
PAI-1
|
Inflammation/Immunology
|
ZK824190 is an orally available and selective urokinase plasminogen activator (uPA) inhibitor as a potential treatment for multiple sclerosis. IC50s of 237, 1600 and 1850 nM for uPA, tPA, and Plasmin, respectively.
|
-
- HY-B0367S
-
-
- HY-N0056
-
-
- HY-100173
-
-
- HY-B1365
-
-
- HY-U00302
-
CHF5407
|
mAChR
|
Inflammation/Immunology
|
CHF5407 is a selective, long-acting and competitive muscarinic M3 receptor antagonist. CHF5407 shows subnanomolar affinities for human muscarinic M1 (hM1), M2 (hM2) and M3 (hM3) receptors. CHF5407 shows a prolonged antibronchospastic activity.
|
-
- HY-N0214A
-
Peimisine hydrochloride
Ebeiensine hydrochloride
|
mAChR
|
Inflammation/Immunology
|
Peimisine (Ebeiensine) hydrochloride non-competitively antagonizes tracheal smooth muscle muscarinic M receptor and inhibits smooth muscle contraction caused by Ach. Peimisine hydrochloride excits β-receptor, restrains the release of internal calcium, and promotes to releaseing NO in order to relax tracheal smooth muscle and relieve asthma.
|
-
- HY-111950
-
(-)-Ibuprofenamide
(R)-Ibuprofenamide
|
Others
|
Inflammation/Immunology
|
(-)-Ibuprofenamide is an amide prodrug of Ibuprofen with anti-inflammatory activity. Ibuprofen is an anti-inflammatory inhibitor targeting COX-1 and COX-2 with IC50s of 13 μM and 370 μM, respectively.
|
-
- HY-15037S2
-
Diclofenac-13C6 Sodium
GP 45840-13C6
|
COX
Apoptosis
|
Inflammation/Immunology
|
Diclofenac-13C6 (Sodium) is the 13C6 labeled Diclofenac (Sodium). Diclofenac Sodium (GP 45840) is a potent and nonselective anti-inflammatory agent, acts as a COX inhibitor, with IC50s of 4 and 1.3 nM for human COX-1 and COX-2 in CHO cells, and 5.1 and 0.84 μM for ovine COX-1 and COX-2, respectively. Diclofenac Sodium induces apoptosis of neural stem cells (NSCs) via the activation of the caspase cascade.
|
-
- HY-115934
-
COX-2-IN-7
|
COX
|
Inflammation/Immunology
|
COX-2-IN-7 (compound 4a) is a potent, selective, and orally active inhibitor of COX-2 with an IC50 of 6.585 uM. COX-2-IN-7 has higher COX-2 selectivity than Celecoxib. COX-2-IN-7 shows good in vivo anti-inflammatory and low ulcerogenic activity.
|
-
- HY-111457
-
BAY-677
|
Others
|
Inflammation/Immunology
|
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM. BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC).
|
-
- HY-D1286
-
-
- HY-113756A
-
Latanoprost acid
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
|
-
- HY-144215
-
TLR8 agonist 4
|
HBV
|
Inflammation/Immunology
|
TLR8 agonist 4 showed effective inhibition on wild-type and drug-resistant (lamivudine and entecavir) HBV strains. The IC50 values are 0.15 and 0.10 respectively μM.
|
-
- HY-W039897
-
-
- HY-137992
-
Aucuparin
|
Others
|
Inflammation/Immunology
|
Aucuparin, a natural product found in Sorbus aucuparia, inhibits pulmonary fibrosis in a bleomycin (BLM)-induced lung fibrosis mouse model. Anti-inflammatory activity.
|
-
- HY-B1125
-
-
- HY-146748
-
-
- HY-19864
-
Aganepag
AGN 210937
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
Aganepag is a potent Prostanoid EP2 receptor agonist, with an EC50 of 0.19 nM, and shows no activity at EP4 receptor. Aganepag can be used in the research of wound healing, scar reduction, scar prevention and wrinkle treatment and prevention.
|
-
- HY-122620
-
-
- HY-100286
-
-
- HY-147719
-
COX-2-IN-16
|
COX
|
Inflammation/Immunology
|
COX-2-IN-16 (compound 2b) is a potent, selective and orally active COX-2 inhibitor with an IC50 of 102 µM. COX-2-IN-16 inhibits the NO production. COX-2-IN-16 shows anti-inflammatory activity.
|
-
- HY-100597
-
Saponins
Saponin
|
Fungal
Bacterial
|
Inflammation/Immunology
|
Saponins (Saponin) is a class of chemical compound of glycosides found in particular abundance in various plant species. In plants, Saponins may serve as anti-feedants, and to protect the plant against microbes and fungi.
|
-
- HY-N0474
-
-
- HY-139716
-
IMD-catechol
|
NF-κB
|
Inflammation/Immunology
|
IMD-catechol is a novel imidazoquinolinone-NF-κB immunomodulator dimer that improves efficacy in a CT26 mouse colon carcinoma tumor model while eliciting minimal adjuvant toxicity.
|
-
- HY-N3472
-
-
- HY-P3149A
-
LEESGGGLVQPGGSMK TFA
|
TNF Receptor
|
Inflammation/Immunology
|
LEESGGGLVQPGGSMK TFA, a proteolysis peptide, is a component of Infliximab. LEESGGGLVQPGGSMK TFA can be used for quantitative analysis of Infliximab. Infliximab is a chimeric monoclonal IgG1 antibody that specifically binds to TNF-α.
|
-
- HY-110261
-
GS143
|
IKK
E1/E2/E3 Enzyme
NF-κB
|
Inflammation/Immunology
|
GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
|
-
- HY-B2070
-
-
- HY-N7108
-
7-Hydroxyflavone
|
Others
|
Inflammation/Immunology
|
7-Hydroxyflavone is a flavonoid isolated from M. indica, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway.
|
-
- HY-W011890
-
-
- HY-N2267
-
-
- HY-108623
-
-
- HY-135677
-
-
- HY-16420
-
R112
|
Syk
|
Inflammation/Immunology
|
R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
|
-
- HY-14564A
-
GTS-21 dihydrochloride
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
|
-
- HY-50948
-
-
- HY-N0631
-
Cornuside
|
p38 MAPK
NF-κB
|
Inflammation/Immunology
|
Cornuside is a secoiridoid glucoside isolated from the fruit of Cornus officinalis Sieb. et Zucc., which is a traditional oriental medicine for treating inflammatory diseases and invigorating blood circulation. Cornuside inhibits mast cell-mediated allergic response by down-regulating MAPK and NF-κB signaling pathways. Cornuside has anti-allergic effects in vivo and in vitro which suggests a therapeutic application of this agent in inflammatory allergic diseases.
|
-
- HY-12839
-
-
- HY-U00278
-
Deloxolone
(3β,20β)-3-(3-Carboxy-1-oxopropoxy)olean-9(11)-en-29-oic acid
|
Others
|
Inflammation/Immunology
|
Deloxolone has the potential for inflammatory, ischemic and proliferative diseases treatment.
|
-
- HY-109082A
-
-
- HY-103363
-
-
- HY-122521
-
Sootepin D
|
NF-κB
|
Inflammation/Immunology
|
Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity.
|
-
- HY-102040
-
Hispidol
(Z)-Hispidol
|
TNF Receptor
|
Inflammation/Immunology
|
Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
|
-
- HY-N4244
-
Kakkalide
|
Others
|
Inflammation/Immunology
|
Kakkalide is an isoflavone derived from the flowers of Pueraria lobata. Kakkalide ameliorates endothelial insulin resistance by suppressing reactive oxygen species (ROS)-associated inflammation.
|
-
- HY-114388
-
QM385
|
Others
|
Inflammation/Immunology
|
QM385 is a potent sepiapterin reductase (SPR) inhibitor with an IC50 of 1.49 nM, which blocks T-cell proliferation and autoimmunity at nanomolar potency and with good oral bioavailability.
|
-
- HY-147590
-
CD73-IN-9
|
CD73
|
Inflammation/Immunology
|
CD73-IN-9 is a potent inhibitor of CD73. CD73 can catalyze the production of adenosine from extracellular 5'-phosphate adenosine (5'-AMP), and adenosine can induce immunosuppressive effects and promote tumor proliferation and/or metastasis. CD73-IN-9 be used for preparing a medicament for tumor-related diseases (extracted from patent WO2022068929A1, compound 2).
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- HY-112137
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- HY-N8104
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- HY-N7031
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(±)-Vasicine
(±)-Peganine
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Proton Pump
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Inflammation/Immunology
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(±)-Vasicine is the racemate of Vasicine. Vasicine (Peganine) significantly inhibits H +-K +-ATPase activity in vitro with an IC50 of 73.47 μg/mL. Anti-ulcer activity. Vasicine shows significant anti-secretory, antioxidant and cytoprotective effect.
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- HY-P0178A
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LXW7 TFA
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Integrin
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Inflammation/Immunology
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LXW7 TFA, a cyclic peptide containing Arg-Gly-Asp (RGD), is an integrin αvβ3 inhibitor. LXW7 has a high binding affinity to αvβ3 integrin with an IC50 of 0.68 μM. LXW7 TFA increases phosphorylation of VEGFR-2 and activation of ERK1/2. Anti-inflammatory effect.
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- HY-100694
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- HY-114041S1
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Resolvin E1-d4-1
RvE1-d4-1
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Endogenous Metabolite
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Inflammation/Immunology
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Resolvin E1-d4-1 (RvE1-d4-1) is the deuterium labeled Resolvin E1. Resolvin E1 (RvE1), a potent endogenous pro-resolving mediator of inflammation, is derived from omega-3 fatty acid eicosapentaenoic acid (EPA). Resolvin E1 is endogenously biosynthesized from EPA in the presence of Aspirin during the spontaneous resolution phase of acute inflammation, where specific cell-cell interactions occur. Resolvin E1 possesses unique counterregulatory actions that inhibit polymorphonuclear leukocyte (PMN) transendothelial migration. Resolvin E1 also acts as a potent inhibitor of leukocyte infiltration, dendritic cell migration, and IL-12 production.
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- HY-42034
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Hydroquinine
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Others
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Inflammation/Immunology
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Hydroquinine is a cinchona alkaloid, can be used in the preparation of its derivatives such as C9 epihydroquinine, 9-acetoxy-10,11-dihydroquinine and 10,11-dihydroquinine monohydrochloride.
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- HY-147692
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COX-2-IN-14
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COX
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Inflammation/Immunology
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COX-2-IN-14 (compound 2a) is a potent and selective COX-2 (cyclooxygenase-2) inhibitor. COX-2-IN-14 shows effective binding at the active site of COX-2 co-crystal. COX-2-IN-14 exhibits a high level of in vivo anti-inflammatory activity, reducing ear edema and myeloperoxidase (MPO) activity in mice.
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- HY-N0136B
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(-)-Taxifolin
(-)-Dihydroquercetin
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Tyrosinase
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Inflammation/Immunology
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(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
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- HY-103370
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Talniflumate
BA 7602-06
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Chloride Channel
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Inflammation/Immunology
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Talniflumate (BA 7602-06) is the prodrug of Niflumic acid (HY-B0493), exerting its activity in the body through conversion to niflumic acid by esterase. Talniflumate is an orally active Ca 2+-activated Cl - channel (CaCC) blocker. Talniflumate can be used as an analgesic and anti-inflammatory agent in cystic fibrosis mouse model of distal intestinal obstructive syndrome.
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- HY-139578
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- HY-B0227S1
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Ketoprofen-d4
RP-19583-d4
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COX
Apoptosis
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Inflammation/Immunology
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Ketoprofen-d4 (RP-19583-d4) is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC50s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively.
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- HY-N8979
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Kanshone A
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Others
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Inflammation/Immunology
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Kanshone A is a sesquiterpene isolated from the roots of Nardostachys chinensis (Valerianaceae). Kanshone A shows cytotoxic with an IC50 value of 7.0 µg/ml in P388 cells.
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- HY-N9324
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- HY-N8167
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Plantanone B
Kaempferol 3-O-rhamnosylgentiobioside
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COX
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Inflammation/Immunology
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Plantanone B is a moderate antioxidant-agent with an IC50 of 169.8±5.2 μM. Plantanone B shows significant ovine COX-1 and moderate COX-2 inhibitory activities. Plantanone B has the potential for inflammation-related diseases research.
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- HY-75035S
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- HY-147025
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- HY-13419
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- HY-N1860S
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3-O-Methylquercetin-d3
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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3-O-Methylquercetin-d3 is the deuterium labeled 3-O-Methylquercetin. 3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC50 values of 31.9 μM, 86.9 μM, 18.6 μM and 1.6 μM for PDE1, PDE5, PDE2 and PDE4, respectively.
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- HY-125390
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SM-360320
CL-087
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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SM-360320 (CL-087) is a potent, oral actively TLR7 agonist. SM-360320 is a mmuno-modulator and exerts an antitumor effect. SM-360320 can act in synergy with DNA vaccines leading to an enhanced Th1 antibody response. SM-360320 can inhibit HCV replication in hepatocytes via a type I IFN-independent mechanism in addition to its IFN-mediated activity.
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- HY-N0476
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Wilforlide A
Regelide; Abruslactone A
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Others
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Inflammation/Immunology
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Wilforlide A is a bioactive triterpene isolated from Tripterygium wilfordii Hook f. Wilforlide A has anti-inflammatory and immune suppressive effects.
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- HY-N8096
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Raddeanoside R17
Pulchinenoside E3
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Others
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Inflammation/Immunology
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Raddeanoside R17 (Pulchinenoside E3) is a saponin compound that can be isolated from the root of Pulsatilla koreana. Raddeanoside R17 shows anti-inflammatory effects.
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- HY-136427
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KRM-III
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Others
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Inflammation/Immunology
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KRM-III is a potent and orally active T-cell antigen receptor (TCR) inhibitor. KRM-III inhibits TCR- and phorbol myristate acetate/ionomycin-induced activation of nuclear factor of activated T cells (NFAT) and T-cell proliferation with an IC50 of ~5 μM. Anti-inflammatory activity.
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- HY-W009248
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