Search Result
Results for "
Aldehyde Dehydrogenase (ALDH) Agonists
" in MCE Product Catalog:
2586
Inhibitors & Agonists
3
Biochemical Assay Reagents
274
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-126003
-
|
ALDH1A1-IN-2
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH1A1-IN-2 is a potent inhibitor of aldehyde dehydrogenase 1a1 (aldh1a1). Aldehyde dehydrogenases (ALDH) constitute a family of enzymes that play a critical role in oxidizing various cytotoxic xenogenic and biogenic aldehydes. ALDH1A1-IN-2 has the potential for the research of cancer, inflammation, or obesity (extracted from patent WO2019089626A1, compound 295).
|
-
- HY-135841
-
|
CM10
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
Metabolic Disease
|
|
CM10 is a potent and selective aldehyde dehydrogenase 1A (ALDH1A) family inhibitor, with IC50s of 1700, 740, and 640 nM for ALDH1A1, ALDH1A2, and ALDH1A3, respectively. CM10 does not inhibit any of the other ALDH family members. CM10 can regulate metabolism and has anti-cancer activity.
|
-
- HY-144669
-
|
ALDH1A3-IN-2
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH1A3-IN-2 (Compound 15) is a potent inhibitor of ALDH1A3 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH1A3-IN-2 has the potential for the research of cancer diseases.
|
-
- HY-144671
-
|
ALDH3A1-IN-2
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH3A1-IN-2 (Compound 19) is a potent inhibitor of ALDH3A1 with an IC50 of 1.29 μM. Aldehyde dehydrogenases (ALDHs) are overexpressed in various tumor types including prostate cancer. ALDH3A1-IN-2 has the potential for the research of cancer diseases.
|
-
- HY-76006
-
-
- HY-107030
-
-
- HY-19801
-
|
CVT-10216
|
Aldehyde Dehydrogenase (ALDH)
|
Neurological Disease
|
|
CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects.
|
-
- HY-115757
-
-
- HY-110294
-
-
- HY-112278
-
-
- HY-W016645
-
-
- HY-W017186
-
|
ALDH1A3-IN-3
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH1A3-IN-3 (compound 16) is a potent inhibitor of ALDH1A3, with an IC50 of 0.26 μM. ALDH1A3-IN-3 is also a good ALDH3A1 substrate. ALDH1A3-IN-3 can be used for the research of prostate cancer.
|
-
- HY-144667
-
-
- HY-W012570
-
-
- HY-122577
-
-
- HY-144670
-
|
ALDH3A1-IN-1
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
ALDH3A1-IN-1 (Compound 18) is a potent inhibitor of ALDH3A1 with an IC50 of 1.61 μM. ALDH3A1-IN-1 is more potent than DEAB against patient-derived primary prostate tumor epithelial cells, as single agents or in combination treatment with docetaxel.
|
-
- HY-131633A
-
-
- HY-18768
-
|
NCT-501
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
NCT-501 is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
|
-
- HY-139031
-
-
- HY-18768A
-
|
NCT-501 hydrochloride
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
NCT-501 hydrochloride is a potent and selective theophylline-based inhibitor of aldehyde dehydrogenase 1A1 (ALDH1A1), inhibits hALDH1A1 with IC50 of 40 nM, typically shows better selectivity over other ALDH isozymes and other dehydrogenases (hALDH1B1, hALDH3A1, and hALDH2, IC50 >57 μM).
|
-
- HY-136594
-
|
BODIPY aminoacetaldehyde
BAAA
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
BODIPY aminoacetaldehyde (BAAA) is a fluorescent substrate for both murine and human aldehyde dehydrogenase (ALDH). BODIPY aminoacetaldehyde consists of an aminoacetaldehyde moiety bonded to the BODIPY fluorochrome and can be used to label stem cells.
|
-
- HY-146682
-
|
KS100
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS100 is a potent ALDH inhibitor with IC50s of 230, 1542, 193 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS100 shows antiproliferative and anticancer effects with low low toxic. KS100 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS10600 induces apoptosis and cell cycle arrest at the G2/M phase.
|
-
- HY-124011
-
-
- HY-146683
-
|
KS106
|
Aldehyde Dehydrogenase (ALDH)
Apoptosis
|
Cancer
|
|
KS106 is a potent ALDH inhibitor with IC50s of 334, 2137, 360 nM for ALDH1A1, ALDH2, and ALDH3A1, respectively. KS106 shows antiproliferative and anticancer effects with low low toxic.KS106 significantly increases ROS activity, lipid peroxidation and toxic aldehyde accumulation. KS106 induces apoptosis and cell cycle arrest at the G2/M phase.
|
-
- HY-138518
-
-
- HY-140620
-
-
- HY-133456
-
-
- HY-W020014
-
-
- HY-136051
-
-
- HY-136077
-
-
- HY-136074
-
-
- HY-136054
-
-
- HY-117041
-
-
- HY-133457
-
-
- HY-135977
-
-
- HY-136076
-
-
- HY-112277
-
|
NCT-505
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
NCT-505 is a potent and selective aldehyde dehydrogenase (ALDH1A1) inhibitor, with an IC50 of 7 nM, and weakly inhibits hALDH1A2, hALDH1A3, hALDH2, hALDH3A1 (IC50s, >57, 22.8, 20.1, >57 μM).
|
-
- HY-136140
-
-
- HY-113165A
-
-
- HY-133465
-
-
- HY-12465
-
-
- HY-N8016
-
-
- HY-138064
-
|
4-APC hydrobromide
|
Others
|
Others
|
|
4-APC hydrobromide is a highly sensitive and selective derivatization agent for aldehydes. 4-APC hydrobromide possesses an aniline moiety for a fast selective reaction with aliphatic aldehydes as well as a quaternary ammonium group for improved MS sensitivity. 4-APC hydrobromide allows highly sensitive and selective MS detection of aldehydes.
|
-
- HY-W004305
-
-
- HY-18936
-
-
- HY-N1177
-
-
- HY-108680
-
-
- HY-B0240
-
|
Disulfiram
Tetraethylthiuram disulfide; TETD
|
Aldehyde Dehydrogenase (ALDH)
Interleukin Related
Pyroptosis
|
Metabolic Disease
Cancer
|
|
Disulfiram (Tetraethylthiuram disulfide) is a specific inhibitor of aldehyde-dehydrogenase (ALDH1), used for the treatment of chronic alcoholism by producing an acute sensitivity to alcohol. Disulfiram inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells. Disulfiram + Cu 2+ increases intracellular ROS levels triggering apoptosis of ovarian cancer stem cells[1-6].
|
-
- HY-33914
-
-
- HY-N2597
-
-
- HY-Z0031
-
-
- HY-N0018
-
|
Daidzin
Daidzoside; NPI-031D; Daidzein 7-O-glucoside
|
Mitochondrial Metabolism
Reverse Transcriptase
|
Others
|
|
Daidzin is an isoflavone that has anti-oxidant, anti-carcinogenic, and anti-atherosclerotic activities; directly inhibits mitochondrial aldehyde dehydrogenase 2 (IC50 = 80 nM) and is an effective anti-dipsotropic isoflavone.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-136736
-
|
β-Secretase Inhibitor II
|
Beta-secretase
|
Neurological Disease
|
|
β-Secretase Inhibitor II is a β-Secretase inhibitor. β-Secretase Inhibitor II is a simple tripeptide aldehyde (IC50=700 nM for inhibition of total Aβ and IC50=2.5 μM for Aβ1–42). β-Secretase Inhibitor II can be used for the research of Alzheimer's disease.
|
-
- HY-114950
-
|
EXP3179
Losartan CarboxAldehyde; DuP 167
|
COX
|
Inflammation/Immunology
Cardiovascular Disease
|
|
EXP3179 is an important intermediate aldehyde metabolite of Losartan. EXP3179 has no AT1-R–blocking activity, but potently inhibits the expression of endothelial cyclooxygenase (COX)-2. EXP3179 exerts potent anti-inflammatory actions.
|
-
- HY-W012926
-
-
- HY-103391
-
|
Qc1
|
Others
|
Metabolic Disease
|
|
Qc1 is a reversible and noncompetitive threonine dehydrogenase (TDH) inhibitor. Qc1 can be used for the research of Metabolic disease.
|
-
- HY-135658
-
-
- HY-126241
-
|
RV01
|
Aldehyde Dehydrogenase (ALDH)
|
Inflammation/Immunology
|
|
RV01 is an analogue of resveratrol, inhibits DNA damage, reduces acetaldehyde dehydrogenase 2 (ALDH2) mRNA expression induced by ethanol, and exhibits hydroxyl radical scavenging activity. RV01 decreases iNOS expression, with anti-neuroinflammatory activity.
|
-
- HY-135282
-
-
- HY-13259
-
|
MG-132
Z-Leu-Leu-Leu-al; MG132
|
Proteasome
Autophagy
Apoptosis
|
Cancer
|
|
MG-132 (Z-Leu-Leu-Leu-al) is a potent proteasome and calpain inhibitor with IC50s of 100 nM and 1.2 μM, respectively. MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132, a peptide aldehyde, also is an autophagy activator. MG-132 also induces apoptosis.
|
-
- HY-145985
-
|
CBR-3465
|
Bacterial
|
Infection
|
|
CBR-3465 is a mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase inhibitor, with the MIC of 0.16 μM against Mtb.
|
-
- HY-145986
-
|
CBR-6672
|
Bacterial
|
Infection
|
|
CBR-6672 is a mycobacterium tuberculosis (Mtb) type II NADH dehydrogenase inhibitor, with the MIC of 0.14 μM against Mtb.
|
-
- HY-114702
-
|
M77976
|
PDHK
|
Metabolic Disease
|
|
M77976 is a specific ATP-competitive inhibitor of PDK4 (pyruvate dehydrogenase kinase isoforms 4), with an IC50 of 648 μM. M77976 is potential for the research of obesity and diabetes.
|
-
- HY-139319
-
|
LDHA-IN-3
|
Lactate Dehydrogenase
|
Cancer
|
|
LDHA-IN-3, as a selenobenzene compound, is a potent, noncompetitive lactate dehydrogenase (LDHA) inhibitor (IC50=145.2 nM). LDHA-IN-3 can be used for the research of cancer.
|
-
- HY-116934
-
|
5-Pentadecylresorcinol
Adipostatin A
|
Others
|
Cancer
Infection
|
|
5-Pentadecylresorcinol (Adipostatin A) is a glycerol-3-phosphate dehydrogenase (GPDH) inhibitor with an IC50 of 4.1 µM. Adipostatin A shows good larvicidal activity against Aedes aegypti.
|
-
- HY-144075
-
|
JAK-IN-19
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-19 is a potent JAK inhibitor (PBMC IFNγ pIC50=7.2 and HLF Eotaxin pIC50=7.7). JAK-IN-19 has good retentive properties in the lung via mitigating being metabolized by Aldehyde Oxidase (AO), with diminished VEGFR2 selectivity (VEGFR2 pIC50=7.0, Aurora B pIC50=5.8).
|
-
- HY-34154
-
|
4-(Dimethylamino)phenol
|
Others
|
Metabolic Disease
|
|
4-(Dimethylamino)phenol increases the extracellular lactate dehydrogenase (LDH) without markedly affecting gluconeogenesis. 4-(Dimethylamino)phenol cannot decreases the ATP content until the membrane becomes permeable to LDH.
|
-
- HY-135667
-
-
- 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-B0876
-
|
Fomepizole
4-Methylpyrazole
|
Cytochrome P450
|
Metabolic Disease
|
|
Fomepizole (4-Methylpyrazole) is a potent cytochrome P450 (CYP2E1) inhibitor. Fomepizole is a competitive inhibitor of the enzyme alcohol dehydrogenase. Fomepizole blocks further conversion of methanol and ethylene glycol to toxic metabolites. Fomepizole has the potential for an antidote for ethylene glycol or methanol poisoning.
|
-
- HY-122737
-
-
- HY-130797
-
-
- HY-103665
-
|
STING agonist-3
|
STING
|
Cancer
|
|
STING agonist-3, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pIC50 of 7.5 and 9.5, respectively. STING agonist-3 has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
|
-
- HY-128888
-
|
WT IDH1 Inhibitor 2
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
WT IDH1 Inhibitor 2 (Compound 3) is a wild-type isocitrate dehydrogenase 1 (WT IDH1) inhibitor with an IC50 value of 120 nM. WT IDH1 Inhibitor 2 as a mutant R132H IDH1 inhibitor, is an isomer of GSK321 with some wild-type cross reactivity.
|
-
- HY-15394
-
-
- HY-139586A
-
-
- HY-107327
-
|
Carazolol
(±)-Carazolol; DL-Carazolol; Suacron
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Carazolol is a β1/β2 adrenoceptor antagonist of high potency used in the research of hypertension. Carazolol is also a potent, selective β3-adrenoceptor agonist.
|
-
- HY-143896
-
|
STING agonist-7
|
STING
|
Cancer
|
|
STING agonist-7 is a non-nucleotide STING agonist. STING agonist-7 binds selectively to mouse STING but not human STING. STING agonist-7 penetrates cell membrane poorly.
|
-
- HY-P1333A
-
-
- HY-113013
-
|
Hydroxypyruvic acid
β-Hydroxypyruvic acid; 3-Hydroxypyruvic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid (β-Hydroxypyruvic acid) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-P1480
-
-
- HY-P1334A
-
-
- HY-B0421
-
-
- HY-113013A
-
|
Hydroxypyruvic acid lithium hydrate
β-Hydroxypyruvic acid lithium hydrate; 3-Hydroxypyruvic acid lithium hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Hydroxypyruvic acid lithium hydrate (β-Hydroxypyruvic acid lithium hydrate) is an intermediate in the metabolism of glycine, serine and threonine. Hydroxypyruvic acid lithium hydrate is a substrate for serine-pyruvate aminotransferase and glyoxylate reductase/hydroxypyruvate reductase. Hydroxypyruvic acid lithium hydrate is involved in the metabolic disorder which is the dimethylglycine dehydrogenase deficiency pathway.
|
-
- HY-113466
-
|
4-Hydroxynonenal
4-HNE
|
Aldehyde Dehydrogenase (ALDH)
Endogenous Metabolite
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
|
-
- HY-N0084
-
|
Betulinaldehyde
Betulinic Aldehyde; Betunal
|
Bacterial
|
Infection
Cancer
|
|
Betulinaldehyde(Betunal) belongs to pentacyclic triterpenoids and was reported to exhibit antimicrobial activities against bacteria and fungi, including S.
|
-
- HY-144124
-
|
5-C-heptyl-DNJ
|
Others
|
Others
|
|
5-heptyl-DNJ is a potent GAA agonist with a Ki of 0.0047 μM. 5-C-heptyl-DNJ increases GAA activities by chaperrone effects.
|
-
- HY-N2548
-
-
- HY-17462
-
|
Adrenosterone
(+)-Adrenosterone
|
Androgen Receptor
Endogenous Metabolite
|
Cancer
Endocrinology
|
|
Adrenosterone ((+)-Adrenosterone) is a competitive hydroxysteroid (11-beta) dehydrogenase 1 (HSD11β1) inhibitor.
Adrenosterone is a steroid hormone with weak androgenic effect. Adrenosterone is a dietary supplement that can decrease fat and increase muscle mass. Adrenosterone acts as a suppressor of metastatic progression of human cancer cells.
|
-
- HY-137434
-
-
- HY-135280
-
-
- HY-124697
-
|
BMP signaling agonist sb4
|
TGF-β Receptor
|
Cancer
|
|
BMP signaling agonist sb4 is a potent benzoxazole bone morphogenetic protein 4 (BMP4) signaling agonist with a EC50 value of 74 nM, activates BMP signaling by stabilizing intracellular p-SMAD-1/5/9. BMP signaling agonist sb4 activates BMP4 target genes (inhibitors of DNA binding, Id1 and Id3) canonical BMP signaling.
|
-
- HY-108656
-
|
MRS2365
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2365 is a potent and selective P2Y1 receptor agonist with an EC50 of 0.4 nM. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors.
|
-
- HY-W005629
-
|
Leelamine
|
Cannabinoid Receptor
PDHK
|
Cancer
|
|
Leelamine is a weak agonist of cannabinoid receptors CB1 and CB2. Leelamine also inhibits pyruvate dehydrogenase kinases (PDKs). Leelamine exhibits anti-tumor activity.
|
-
- HY-146135
-
-
- HY-N0295
-
|
Protocatechualdehyde
CatechAldehyde; Protocatechuic Aldehyde; Rancinamycin IV
|
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
|
|
Protocatechualdehyde (Catechaldehyde), a natural polyphenol compound isolated from the roots of radix Salviae Miltiorrhizae, is associated with a wide variety of biological activities and has been widely used in medicine as an antioxidant, anti-aging, an antibacterial and anti-inflammatory agent.
|
-
- HY-107150
-
|
Reproxalap
ADX-102; NS-2
|
Others
|
Inflammation/Immunology
|
|
Reproxalap (ADX-102) is a reactive aldehyde species (RASP) sequestering agent for the treatment of dry eye. Reproxalap (ADX-102) covalently binds aldehydes including malondialdehyde and 4-hydroxynonenal.
|
-
- HY-W107464
-
|
G6PDi-1
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells.
|
-
- HY-79494
-
-
- HY-A0144
-
-
- HY-117196
-
-
- HY-113165
-
-
- HY-12745A
-
|
Nalfurafine hydrochloride
TRK-820 hydrochloride
|
Opioid Receptor
|
Neurological Disease
|
|
Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine hydrochloride (TRK-820 hydrochloride) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
|
-
- HY-12745
-
|
Nalfurafine
TRK-820
|
Opioid Receptor
|
Neurological Disease
|
|
Nalfurafine (TRK-820) is a potent selective and orally active G protein-biased kappa opioid receptor (KOR)-agonist with high translational potential. Nalfurafine (TRK-820) enhances the therapeutic potential of MOR-targeting analgesics, has the potential for uremic pruritis treatment.
|
-
- HY-146288
-
|
LXR agonist 2
|
LXR
|
Metabolic Disease
|
|
LXR agonist 2 (compound 18rr) is a potent LXR (liver X receptor) agonist. LXR agonist 2 can stabilize NCOA1 (co-activator), leading to LXR agonism.
|
-
- HY-W007330
-
-
- HY-10019
-
|
Varenicline
CP 526555
|
nAChR
|
Neurological Disease
|
|
Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
|
-
- HY-W008393
-
-
- HY-W004307
-
-
- HY-103221
-
-
- HY-114524
-
|
(E)-4-Oxo-2-nonenal
4-ONE
|
TRP Channel
|
Cardiovascular Disease
|
|
(E)-4-Oxo-2-nonenal (4-ONE) is one of the major hemolytic decomposition products of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a major product of the FeII-mediated breakdown of lipid hydroperoxides. (E)-4-Oxo-2-nonenal is a potent transient receptor potential ankyrin 1 (TRPA1) agonist.
|
-
- HY-20457
-
-
- HY-110087
-
-
- HY-147542
-
-
- HY-113466S
-
|
4-Hydroxynonenal-d3
4-HNE-d3
|
Aldehyde Dehydrogenase (ALDH)
Endogenous Metabolite
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
4-Hydroxynonenal-d3 (4-HNE-d3) is the deuterium labeled 4-Hydroxynonenal. 4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
|
-
- HY-113076
-
-
- HY-I0637
-
-
- HY-N8015
-
-
- HY-116247
-
|
ST247
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ.
|
-
- HY-113165AS
-
-
- HY-B0051
-
-
- HY-113165AS1
-
-
- HY-18761
-
|
Cobalt phthalocyanine
Cobalt(II) phthalocyanine; Cobaltous phthalocyanine; Phthalocyanine cobalt complex
|
Others
|
Others
|
|
Cobalt phthalocyanine is a catalyst of redox reaction, catalyzes aerobic regenerations of aldehydes and ketones from aldoximes and ketoximes has been developed.
|
-
- HY-76224
-
|
3-Furaldehyde
|
Others
|
Others
|
|
3-Furaldehyde is a member of furans and an aldehyde, and can be used to synthesize the neoclerodane diterpene Salvinorin A.
|
-
- HY-125996
-
|
NR1H4 activator 1
|
FXR
|
Inflammation/Immunology
|
|
NR1H4 activator 1 is a potent and selective Famesoid X Receptor (FXR) agonist, extracted from patent WO2018152171A1, example 4. NR1H4 activator 1 shows strong FXR agonistic potency with a EC50 value of 1 nM in a Human FXR (NR1H4) Assay. NR1H4 activator 1 has the potential for treatment of gastrointestinal disease.
|
-
- HY-145885
-
|
TLR7/8 agonist 6
|
Toll-like Receptor (TLR)
|
Cancer
Infection
Inflammation/Immunology
|
|
TLR7/8 agonist 6 (Compound 4) is the potent agonist of TLR7/8 with IC50s of 0.18 and 5.34 μM, respectively. TLR7/8 agonist 6 is an imidazoquinoline derivative compound. Toll-like receptors (TLRs) 7 and 8 are key targets in the development of immunomodulatory drugs for treating infectious disease, cancer, and autoimmune disorders.
|
-
- HY-10063
-
|
Ispronicline
TC-1734; ACD3480
|
nAChR
|
Neurological Disease
|
|
Ispronicline (TC-1734), an orally active, brain-selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist, has shown memory-enhancing properties in rodents and a good tolerability profile. Ispronicline binds to the α4β2 nAChR with high affinity (Ki=11 nM) and is highly selective to other nAChRs such as α7 nAChR and α3β4 nAChR.
|
-
- HY-W011417
-
|
Cinnabarinic acid
|
mGluR
Apoptosis
|
Others
|
|
Cinnabarinic acid is a specific orthosteric agonist of mGlu4 by interacting with residues of the glutamate binding pocket of mGlu4, has no activity at other mGlu receptors. Cinnabarinic acid is an endogenous metabolite of the kynurenine pathway of tryptophan. Cinnabarinic acid induces cell apoptosis.
|
-
- HY-139032
-
-
- HY-137061
-
-
- HY-12399
-
|
MKC9989
|
IRE1
|
Cancer
|
|
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
|
-
- HY-14302
-
-
- HY-17453
-
-
- HY-135119
-
|
Salmeterol-D3
|
Adrenergic Receptor
|
Endocrinology
Inflammation/Immunology
|
|
Salmeterol-D3 is a deuterium labeled Salmeterol. Salmeterol is a potent and selective human β2 adrenoceptor agonist. Salmeterol shows potent stimulation of cAMP accumulation in CHO cells expressing human β2, β1 and β3 adrenoceptors with pEC50s of 9.6, 6.1, and 5.9, respectively.
|
-
- HY-N7624
-
|
Methyl oleanonate
3-Oxoolean-12-en-28-oic acid methyl ester
|
PPAR
|
Cancer
|
|
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.
|
-
- HY-130074
-
-
- HY-113076S
-
-
- HY-133112
-
-
- HY-12959
-
|
Repinotan
BAY x 3702 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects.
|
-
- HY-Y0790
-
|
Cuminaldehyde
|
Endogenous Metabolite
|
Cancer
|
|
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity.
|
-
- HY-101198
-
|
Clobenpropit dihydrobromide
|
Histamine Receptor
Apoptosis
|
Cancer
Neurological Disease
|
|
Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR. Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM). Clobenpropit dihydrobromide increases apoptosis.
|
-
- HY-Y0015
-
|
p-Dimethylaminobenzaldehyde
4-DimethylaminobenzAldehyde
|
Others
|
Others
|
|
p-Dimethylaminobenzaldehyde (4-Dimethylaminobenzaldehyde) is an organic compound containing amine and aldehyde moieties which is used in Ehrlich's reagent and Kovac's reagent to test for indoles.
|
-
- HY-101603
-
-
- HY-129545
-
-
- HY-110157
-
|
AC-186
|
Estrogen Receptor/ERR
|
Neurological Disease
|
|
AC-186 is a selective non-steroidal estrogen receptor β (ERβ) agonist with EC50s of 6 nM and 5000 nM for ERβ and ERα, respectively. AC-186 shows gender specific neuroprotection in a Parkinson’s Disease rat model.
|
-
- HY-14153
-
-
- HY-144699
-
|
ERRα antagonist-2
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo.
|
-
- HY-B1833
-
|
Afloqualone
HQ-495
|
GABA Receptor
|
Neurological Disease
|
|
Afloqualone (HQ-495) is a GABAergic agent and has agonist activity at the β subtype of the GABAα receptor. Afloqualone has antivertiginous effects thought to be attributable to the increased sensitivity of GABA receptors of the LVN neuron site.
|
-
- HY-P1201
-
|
Cyclosomatostatin
|
Somatostatin Receptor
|
Cancer
|
|
Cyclosomatostatin is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-W012530
-
-
- HY-129527
-
|
GNE-9278
|
iGluR
|
Neurological Disease
|
|
GNE-9278 is a highly selective positive allosteric modulator of NMDAR that acts at the GluN1 transmembrane domain (TMD). GNE-9278 acts on activated NMDARs to increase peak current and agonist affinity.
|
-
- HY-100369A
-
|
DMCM hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 receptors, respectively.
|
-
- HY-W008129
-
-
- HY-145295
-
|
Flupyradifurone
|
nAChR
|
Infection
|
|
Flupyradifurone is a systemic nAChR agonist that interferes with signal transduction in the central nervous system of sucking pests. Flupyradifurone can be used as a butenolide insecticide.
|
-
- HY-P1201A
-
|
Cyclosomatostatin TFA
|
Somatostatin Receptor
|
Cancer
|
|
Cyclosomatostatin TFA is a potent somatostatin (SST) receptor antagonist. Cyclosomatostatin TFA can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cells.
|
-
- HY-N2498
-
-
- HY-139851
-
-
- HY-147678
-
|
GPR40 agonist 5
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice.
|
-
- HY-110217
-
|
BMS-566419
|
Others
|
Others
|
|
BMS-566419 is an acridone-based inhibitors of inosine 5'-monophosphate dehydrogenase (IMPDH). Inosine monophosphate dehydrogenase (IMPDH) is a key enzyme in the de novo synthesis of guanosine nucleotides. BMS-566419 has clinical utility for the research of transplant rejection.
|
-
- HY-101966
-
|
NCT-503
|
Others
|
Cancer
|
|
NCT-503 is a phosphoglycerate dehydrogenase (PHGDH) inhibitor with an IC50 of 2.5 µM.
|
-
- HY-112645
-
-
- HY-146661
-
-
- HY-117851
-
|
AC-265347
|
CaSR
|
Metabolic Disease
Endocrinology
|
|
AC-265347 is a calcium-sensing receptor (CaSR) agonist and positive allosteric modulator (ago-PAM) with the functional affinity (pKB) of 5.1. AC-265347 can be used for the research of hyperparathyroidism and related diseases.
|
-
- HY-100020
-
-
- HY-103476
-
|
Ro15-4513
|
GABA Receptor
|
Neurological Disease
|
|
Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR). Ro15-4513 is a potent ethanol antagonist. Ro15-4513 has anti-anxiety effect.
|
-
- HY-118933
-
|
Calpain Inhibitor VI
SJA6017
|
Proteasome
|
Others
|
|
Calpain Inhibitor VI (SJA6017) is a synthesized peptide aldehyde inhibitor of calpain. Calpain Inhibitor VI inhibits purified m-calpain with the IC50 of 80 nM. Calpain Inhibitor VI can be used for the research of cataract.
|
-
- HY-B0083
-
-
- HY-146317
-
-
- HY-103454B
-
|
MPP hydrochloride
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
MPP hydrochloride is a potent and selective ER (estrogen receptor) modulator. MPP hydrochloride induces significant apoptosis in the endometrial cancer and oLE cell lines. MPP hydrochloride reverses the positive effects of beta-estradiol. MPP hydrochloride has mixed agonist/antagonist action on murine uterine ERalpha in vivo.
|
-
- HY-17038A
-
|
Agomelatine hydrochloride
S-20098 hydrochloride
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine hydrochloride (S-20098 hydrochloride) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine hydrochloride is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-17038
-
|
Agomelatine
S-20098
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine (S-20098) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-P2161
-
|
TAK-683
|
Others
|
Cancer
|
|
TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
|
-
- HY-W011094
-
|
Win 18446
|
Aldehyde Dehydrogenase (ALDH)
|
Endocrinology
|
|
Win 18446 is an orally active testes-specific enzyme ALDH1a2 inhibitor, with an IC50 of 0.3 μM. Win 18446 reversibly inhibits spermatogenesis in many species and inhibits Retinoic acid (HY-14649) biosynthesis from Retinol (HY-B1342) within the testes.
|
-
- HY-14281
-
|
Trilostane
Win 24540
|
Others
|
Endocrinology
Cancer
|
|
Trilostane(Win 24540; Modrastane) is an inhibitor of 3 β-hydroxysteroid dehydrogenase used in the treatment of Cushing's syndrome.
|
-
- HY-13673
-
|
Goserelin
ICI 118630
|
GnRH Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
Goserelin (ICI 118630), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
|
-
- HY-B1021
-
|
Vincamine
|
Free Fatty Acid Receptor
|
Metabolic Disease
Cardiovascular Disease
|
|
Vincamine is a monoterpenoid indole alkaloid extracted from the Madagascar periwinkle. Vincamine is a peripheral vasodilator and exerts a selective vasoregulator action on the brain microcapilar circulation. Vincamine is a GPR40 agonist and acts as a β-cell protector by ameliorating β-cell dysfunction and promoting glucose-stimulated insulin secretion (GSIS). Vincamine improves glucose homeostasis in vivo, and has the potential for the type 2 diabetes mellitus (T2DM) research.
|
-
- HY-13673A
-
|
Goserelin acetate
ICI-118630 acetate
|
GnRH Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
Goserelin acetate (ICI-118630 acetate), a decapeptide analogue of gonadotropin-releasing hormone (GnRH/LHRH), functions as a GnRH agonist. Goserelin acetate can be used for the research of breast cancer, epithelial ovarian cancer and prostate cancer.
|
-
- HY-100742B
-
-
- HY-13986
-
|
Merimepodib
VX-497; MMPD
|
HBV
HCV
|
Infection
|
|
Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.
|
-
- HY-139189
-
-
- HY-77521
-
-
- HY-139839
-
|
Y12196
|
Others
|
Infection
|
|
Y12196 is a novel succinate dehydrogenase inhibitor (SDHI) which exhibits strong fungicidal activity against F. graminearum.
|
-
- HY-W014787
-
-
- HY-17038B
-
|
Agomelatine (L(+)-Tartaric acid)
S-20098 L(+)-Tartaric acid
|
Melatonin Receptor
5-HT Receptor
|
Neurological Disease
|
|
Agomelatine L(+)-Tartaric acid (S-20098 L(+)-Tartaric acid) is a specific agonist of MT1 and MT2 receptors with Kis of 0.1, 0.06, 0.12, and 0.27 nM for CHO-hMT1, HEK-hMT1, CHO-hMT2, and HEK-hMT2, respectively. Agomelatine L(+)-Tartaric acid is a selective 5-HT2C receptor antagonist with pKis of 6.4 and 6.2 at native (porcine) and cloned, human 5-HT2C receptors, respectively.
|
-
- HY-100991
-
|
FG 7142
ZK 39106; LSU-65
|
GABA Receptor
|
Neurological Disease
|
|
FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex.
|
-
- HY-133023
-
|
Indium(III) isopropoxide
|
Others
|
Others
|
|
Indium(III) Isopropoxide is an organo-metallic compound. Indium(III) Isopropoxide uesd as a hydrogen transfer catalyst for conversion of benzylic alcohols into aldehydes or ketones via Oppenauer oxidation. Indium(III) Isopropoxide also can be used as metal precursor.
|
-
- HY-124062
-
|
TAS-114
|
Others
|
Cancer
|
|
TAS-114 is a dual dUTPase/dihydropyrimidine dehydrogenase (DPD) inhibitor, can improving the therapeutic efficacy of fluoropyrimidine.
|
-
- HY-108571
-
|
CP-775146
|
PPAR
|
Metabolic Disease
|
|
CP-775146 is a selective PPARα agonist that binds strongly to the PPARα ligand. CP-775146 efficiently alleviates obesity-induced liver damage, prevents lipid accumulation by activating the liver fatty acid β-oxidation pathway.
|
-
- HY-105286
-
|
BI-135585
|
Others
|
Metabolic Disease
|
|
BI-135585 is a potent, selective and orally active 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitor with an IC50 of 13 nM. BI-135585 exhibits >1000-fold selectivity over other hydroxysteroid dehydrogenases. BI-135585 can be used for type 2 diabetes research.
|
-
- HY-142521
-
|
BLT2 probe 1
|
Others
|
Metabolic Disease
|
|
BLT2 probe 1 (compound 13) is a fluorescent probe based on the synthetic BLT2 agonist CAY10583. BLT2 is a promising target for diabetic wound healing and gastrointestinal lesions. BLT2 probe 1 is suitable to investigate the pharmacology of BLT2 receptor ligands in a variety of assay systems.
|
-
- HY-100681
-
-
- HY-135676
-
-
- HY-103096
-
|
R162
|
Others
|
Cancer
|
|
R162 is a potent inhibitor of glutamate dehydrogenase 1 (GDH1/GLUD1), with anti-cancer properties.
|
-
- HY-18968
-
-
- HY-119459
-
|
Fluopyram
|
Fungal
|
Infection
|
|
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
|
-
- HY-135675
-
-
- HY-N6736
-
|
K-252c
|
PKC
Bacterial
Apoptosis
|
Cancer
Infection
|
|
K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase.
|
-
- HY-W001187
-
-
- HY-111108
-
|
LDH-IN-1
|
Lactate Dehydrogenase
|
Cancer
|
|
LDH-IN-1 is a novel pyrazole-based inhibitor of human lactate dehydrogenase (LDH) with IC50s of 32 and 27 nM for LDHA and LDHB, respectively.
|
-
- HY-113304
-
-
- HY-W001941
-
|
D-Cystine
|
Others
|
Others
|
|
D-Cystine is the D-enantiomer of L-Cystine. D-Cystine inhibits L-aspartate-β-semialdehyde dehydrogenase (ASADH) from Escherichia coli.
|
-
- HY-120338
-
-
- HY-113128
-
-
- HY-146289
-
|
LXR antagonist 2
|
LXR
|
Metabolic Disease
|
|
LXR antagonist 2 (compound 10rr) is a potent LXR (liver X receptor) inverse agonist, with IC50 values of 0.36 and 2.25 μM for LXRβ and LXRα, respectively. LXR antagonist 2 is a lipogenesis inhibitor through down-regulating LXR target genes SREBP-1c, ACC, FAS and SCD-1. LXR antagonist 2 shows lipid-lowering effects in mice with Triton WR-1339-induced hyperlipidemia.
|
-
- HY-N7961
-
-
- HY-18055
-
-
- HY-113128A
-
-
- HY-18053
-
-
- HY-113166
-
-
- HY-113128B
-
-
- HY-12688
-
|
Succinyl phosphonate
|
Endogenous Metabolite
Reactive Oxygen Species
|
Neurological Disease
|
|
Succinyl phosphonate is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-16214
-
|
FX-11
LDHA Inhibitor FX11
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
|
FX-11 (LDHA Inhibitor FX11) is a potent lactate dehydrogenase A (LDHA) inhibitor with an IC50 of 23.3 μM for HeLa cell and a Ki value of 8 μM.
|
-
- HY-17469
-
|
Gimeracil
Gimestat
|
Others
|
Cancer
|
|
Gimeracil, a component of an oral fluoropyrimidine derivative S-1, inhibits DNA DSB repair and is a potent inhibitor of DPYD (dihydropyrimidine dehydrogenase, DPD).
|
-
- HY-B2004
-
|
Thifluzamide
|
Fungal
|
Infection
|
|
Thifluzamide, a broad-spectrum succinate dehydrogenase inhibitor (SDHI) fungicide, has been widely used in the controlling of a variety of fungal diseases in rice fields.
|
-
- HY-N7114A
-
-
- HY-135570
-
-
- HY-12688A
-
|
Succinyl phosphonate trisodium salt
|
Endogenous Metabolite
Reactive Oxygen Species
|
Cancer
Metabolic Disease
Neurological Disease
|
|
Succinyl phosphonate trisodium salt is an α-ketoglutarate dehydrogenase (KGDHC) inhibitor, effective inhibits (KGDHC) in muscle, bacterial, brain, and cultured human fibroblasts. Succinyl phosphonate trisodium salt is an 2-oxoglutarate dehydrogenase (OGDH) inhibitor, impairs viability of cancer cells in a cell-specific metabolism-dependent manner. Succinyl phosphonate trisodium salt inhibits the glutamate-induced ROS production in glutamate-stimulated hippocampal neurons in situ.
|
-
- HY-113304A
-
-
- HY-135664
-
-
- HY-145326
-
|
Antibacterial agent 67
|
Fungal
|
Others
|
|
Antibacterial agent 67 (IC50 = 0.03 μM) has a great enzyme-inhibiting activity increase toward succinate dehydrogenase in comparison with fluxapyroxad (IC50 = 4.40 μM).
|
-
- HY-114570
-
|
Tiazofurin
NSC 286193; Riboxamide
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Tiazofurin is a synthetic nucleoside analogue with antineoplastic activity. Tiazofurin is anabolized intracellularly to tiazole-4-carboxamide adenine dinucleotide (TAD), a potent inhibitor of IMP dehydrogenase (IMPDH).
|
-
- HY-W040073
-
|
Nifurtimox
|
Parasite
Lactate Dehydrogenase
|
Cancer
Infection
|
|
Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
|
-
- HY-N2337
-
-
- HY-129630
-
-
- HY-Y1771
-
|
2-Carboxybenzaldehyde
|
Others
|
Cancer
Infection
|
|
2-Carboxybenzaldehyde is a chemical compound. 2-Carboxybenzaldehyde consists of a benzene ring, with an aldehyde and a carboxylic acid as substituents that are ortho to each other. 2-Carboxybenzaldehyde can be used to form ligands with metal ions. Ni(II) and Cu(II) complexes of 2-Carboxybenzaldehyde thiosemicarbazone has anticancer and antibacterial activities.
|
-
- HY-18717
-
-
- HY-100742
-
-
- HY-132170
-
-
- HY-137463
-
-
- HY-B0199A
-
|
Mycophenolate mofetil hydrochloride
RS 61443 hydrochloride; TM-MMF hydrochloride
|
Others
Endogenous Metabolite
|
Cancer
|
|
Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-131943
-
|
DS44960156
|
Others
|
Others
|
|
DS44960156 is a selective Methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor, with IC50 values of 1.6 μM and >30 μM for MTHFD2 and MTHFD1, respectively.
|
-
- HY-128578
-
-
- HY-126256
-
|
PRMT5-IN-1
|
Histone Methyltransferase
|
Cancer
|
|
PRMT5 IN-1, a hemiaminal, is a covalent protein arginine methyltransferase 5 (PRMT5) inhibitor with an IC50 of 11 nM for PRMT5/MEP50. PRMT5 IN-1 can be converted to aldehydes and react with C449 to form covalent adducts under physiological conditions.
|
-
- HY-135654
-
-
- HY-107977
-
-
- HY-W017522
-
|
Adipic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Adipic acid is found to be associated with HMG-CoA lyase deficiency, carnitine-acylcarnitine translocase deficiency, malonyl-Coa decarboxylase deficiency, and medium Chain acyl-CoA dehydrogenase deficiency, which are inborn errors of metabolism.
|
-
- HY-135648
-
-
- HY-77521S
-
-
- HY-W012875
-
-
- HY-147105
-
|
LRH-1 modulator-1
|
Others
|
Inflammation/Immunology
|
|
LRH-1 modulator-1 (compound 6N) is a potent LRH-1 (liver receptor homolog-1) modulator/agonist. LRH-1 modulator-1 shows anti-inflammatory effects in intestinal organoids. LRH-1 modulator-1 induces anti-inflammatory cytokine IL-10, and reduces inflammatory cytokine IL-1b and TNFa.
|
-
- HY-D0845
-
-
- HY-120924
-
-
- HY-113212
-
|
Ursocholic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Ursocholic acid, a bile acid found predominantly in bile of mammals, is transformed into deoxycholic acid by the intestinal microflora in mice. Ursodeoxycholic acid is an inhibitor of 7α-hydroxysteroid dehydrogenase and hepatocyte nuclear factor 1α.
|
-
- HY-136498
-
|
T-705RMP
|
Drug Metabolite
|
Infection
|
|
T-705RMP, a phosphorylated metabolite of T-705, exhibits a very weak inhibitory effect on the IMP dehydrogenase (IMPDH) activities of the host cells, with an IC50 of 601 μM.
|
-
- HY-N3115
-
|
Palbinone
|
Others
|
Inflammation/Immunology
|
|
Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity.
|
-
- HY-101943
-
|
LY 345899
|
Others
|
Cancer
|
|
LY 345899 is a Folate analog and is a methylene tetrahydrofolate dehydrogenase (MTHFD1; DC301) and MTHFD2 inbhibitor with IC50 values of 96 nM and 663 nM, respectively and a Ki of 18 nM for MTHFD1.
|
-
- HY-117240
-
|
NCT-502
|
Others
|
Cancer
|
|
NCT-502 is a human phosphoglycerate dehydrogenase (PHGDH) inhibitor, cytotoxic to PHGDH-dependent cancer cells, and reduces glucose-derived serine production, with an IC50 of 3.7 μM against PHGDH.
|
-
- HY-16082
-
|
AZD7545
|
PDHK
|
Metabolic Disease
|
|
AZD7545 is a potent, competitive, selective PDHK2 (pyruvate dehydrogenase kinase 2) inhibitor with IC50s of 36.8 nM, 6.4 nM for PDHK1 and PDHK2, respectively.
|
-
- HY-113108
-
|
(R)-3-Hydroxyisobutyric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(R)-3-Hydroxyisobutyric acid is an intermediate in the pathways of l-valine and thymine and plays an important role in the diagnosis of the very rare inherited metabolic diseases 3-hydroxyisobutyric aciduria and methylmalonic semialdehyde dehydrogenase deficiency.
|
-
- HY-108012
-
|
ME1111
|
Fungal
|
Infection
|
|
ME1111 is an antifungal agent that is active against dermatophytes. ME1111 is an inhibitor of the succinate dehydrogenase of Trichophyton species. ME1111 has an excellent ability to penetrate human nails and is used for onychomycosis research.
|
-
- HY-132171
-
|
DSM705
|
Dihydroorotate Dehydrogenase
Parasite
|
Infection
|
|
DSM705 is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites, with no inhibition of mammalian DHODHs. DSM705 is a potent antimalarial compound.
|
-
- HY-128787
-
-
- HY-100742A
-
|
(R)-GNE-140
|
Lactate Dehydrogenase
|
Cancer
|
|
(R)-GNE-140 is a potent lactate dehydrogenase A (LDHA) inhibitor, with IC50s of 3 nM and 5 nM for LDHA and LDHB, respectively; (R)-GNE-140 is 18-fold more potent than S enantiomer.
|
-
- HY-W040073S
-
|
Nifurtimox-d4
|
Parasite
Lactate Dehydrogenase
|
Cancer
Infection
|
|
Nifurtimox-d4 is deuterium labeled Nifurtimox. Nifurtimox, an antiprotozoal agent, which is generally used for the treatment of infections with Trypanosoma cruzi, has been used in the therapy of neuroblastoma. Nifurtimox affects enzyme activity of lactate dehydrogenase (LDH).
|
-
- HY-129630S
-
|
Tetrahydrocortisol-d5
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Tetrahydrocortisol-d5 is the deuterium labeled Tetrahydrocortisol. Tetrahydrocortisol is cortisol metabolite. The urinary Tetrahydrocortisol/Tetrahydrocortisone ratio decreases with increasing 11β-hydroxysteroid dehydrogenase (11β-HSD) activity.
|
-
- HY-108325
-
-
- HY-138097
-
|
α-NETA
|
Aldehyde Dehydrogenase (ALDH)
AChE
Apoptosis
|
Cancer
|
|
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity.
|
-
- HY-101930
-
|
BMS-816336
|
Others
|
Metabolic Disease
|
|
BMS-816336 is a novel, potent and orally bioavailable inhibitor against human 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with an IC50 of 3.0 nM.
|
-
- HY-19540
-
-
- HY-W040118
-
|
Galloflavin
|
Lactate Dehydrogenase
|
Cancer
|
|
Galloflavin is a potent lactate dehydrogenase (LDH) inhibitor. The calculated Kis for pyruvate are 5.46 µM (LDH-A) and 15.06 µM (LDH-B). Galloflavin hinders the proliferation of cancer cells by blocking glycolysis and ATP production.
|
-
- HY-B0083S
-
|
Leflunomide-d4
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
Leflunomide-d4 (HWA486-d4) is the deuterium labeled Leflunomide. Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase (DHODH), and acts as a disease-modifying antirheumatic drug.
|
-
- HY-W051723
-
|
(R)-3-Hydroxybutanoic acid
(R)-(-)-3-Hydroxybutanoic acid; (R)-3-Hydroxybutyric acid
|
Endogenous Metabolite
|
Others
|
|
(R)-3-Hydroxybutanoic acid is a metabolite, and converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid has applications as a nutrition source and as a precursor for vitamins, antibiotics and pheromones.
|
-
- HY-W078844
-
|
PfDHODH-IN-2
|
Dihydroorotate Dehydrogenase
Parasite
|
Infection
|
|
PfDHODH-IN-2, a dihydrothiophenone derivative (Compound 11), is a potent Plasmodium falciparum dihydroorotate dehydrogenase (PfDHODH) inhibitor with an IC50 of 1.11 µM. PfDHODH-IN-2 acts as an antimalarial agent and can be used for the research of malaria.
|
-
- HY-10533
-
|
Eniluracil
5-Ethynyluracil; GW776C85
|
Others
|
Cancer
|
|
Eniluracil (5-Ethynyluracil), a uracil analogue and a mechanism-based irreversible inhibitor of dihydropyrimidine dehydrogenase (DPD), increases the oral bioavailability of 5-fluorouracil (5-FU) to 100%, facilitating uniform absorption and predictable toxicity.
|
-
- HY-12492
-
|
VER-246608
|
PDHK
|
Cancer
|
|
VER-246608 is a potent and ATP-competitive inhibitor of pyruvate dehydrogenase kinase (PDK) with IC50s of 35 nM, 40 nM, 84 nM, and 91 nM for PDK-1, PDK-3, PDK-2, and PDK-4, respectively.
|
-
- HY-100184
-
-
- HY-135549
-
|
Fluxapyroxad
|
Fungal
Antibiotic
|
Infection
|
|
Fluxapyroxad is a synthetic broad-spectrum fungicide for the control of fungal diseases. It works by inhibiting succinate dehydrogenase in complex II of the mitochondrial respiratory chain, resulting in inhibition of spore germination, germ tubes and mycelia growth within the fungus target species.
|
-
- HY-114009
-
-
- HY-135678
-
-
- HY-135677
-
-
- HY-135679
-
-
- HY-135619
-
-
- HY-135618
-
|
DHODH-IN-3
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
|
Infection
|
|
DHODH-IN-3 (compound 3) is a potent inhibitor of Human Dihydroorotate Dehydrogenases (HsDHODH) with an IC50 value of 261 nM. DHODH-IN-3 binds to the the ubiquinone binding cavities in DHODH with a Ki app of 32 nM. DHODH-IN-3 has the potential for malaria treatment.
|
-
- HY-123962
-
|
G6PD activator AG1
|
Others
|
Metabolic Disease
|
|
G6PD activator AG1 is a potent and selective glucose-6-phosphate dehydrogenase (G6PD) activator with an EC50 of 3 µΜ. G6PD activator AG1 reduces hemolysis of human erythrocytes.
|
-
- HY-B1729
-
|
Phenoxyethanol
|
Bacterial
|
Infection
|
|
Phenoxyethanol has a broad spectrum of antimicrobial activity against various gram-negative and gram-positive bacteria. Phenoxyethanol is an uncouple agent in oxidative phosphorylation from respiration and competitively inhibits malate dehydrogenase. Phenoxyethanol is used as a preservative in cosmetic, vaccine, and textile, et al.
|
-
- HY-100688
-
|
ML390
|
Dihydroorotate Dehydrogenase
|
Cancer
|
|
ML390 is a potent dihydroorotate dehydrogenase (DHODH) inhibitor. ML390 is an inducer of myeloid differentiation and causes myeloid differentiation in murine (ER-HoxA9) and human (U937 and THP1) acute myeloid leukemia (AML) models.
|
-
- HY-109619
-
|
D4-abiraterone
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-N2177
-
|
3-Dehydrotrametenolic acid
|
Lactate Dehydrogenase
Apoptosis
|
Cancer
|
|
3-Dehydrotrametenolic acid, isolated from the sclerotium of Poria cocos, is a lactate dehydrogenase (LDH) inhibitor. 3-Dehydrotrametenolic acid promotes adipocyte differentiation in vitro and acts as an insulin sensitizer in vivo. 3-Dehydrotrametenolic acid induces apoptosis and has anticancer activity.
|
-
- HY-N7393
-
|
Isomalt
Palatinitol
|
Lactate Dehydrogenase
|
Metabolic Disease
|
|
Isomalt (Palatinitol), a well-tolerated, non-toxic polyol and a protein-stabilizing excipient, stabilizes lactate dehydrogenase (LDH) moderately during freeze-drying, and performs better during storage. Isomalt is traditionally used as a sweetening agent in the food industry and as a tabletting excipient for pharmaceutical purposes.
|
-
- HY-W040307
-
|
Saccharopine
L-Saccharopine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Saccharopine (L-Saccharopine), a lysine degradation intermediate, is a mitochondrial toxin. Lysine and α-ketoglutarate are converted into Saccharopine by the lysine-ketoglutarate reductase. Saccharopine is then oxidized to α-aminoapidate semialdehyde and glutamate by the saccharopine dehydrogenase. Saccharopine impairs development by disrupting mitochondrial homeostasis.
|
-
- HY-W015851
-
|
(R)-3-Hydroxybutanoic acid sodium
(R)-(-)-3-Hydroxybutanoic acid sodium; (R)-3-Hydroxybutyric acid sodium
|
Endogenous Metabolite
|
Neurological Disease
|
|
(R)-3-Hydroxybutanoic acid sodium ((R)-3-Hydroxybutyric acid) is a metabolite converted from acetoacetic acid catalyzed by 3-hydroxybutyrate dehydrogenase. (R)-3-Hydroxybutanoic acid sodium can function as a nutrition source, and as a precursor for vitamins, antibiotics and pheromones.
|
-
- HY-Y0445A
-
|
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-114459
-
-
- HY-139983
-
|
SDH-IN-1
|
Fungal
|
Infection
|
|
SDH-IN-1 (compound 4i) is a succinate dehydrogenase (SDH) inhibitor with an IC50 of 4.53 μM. SDH-IN-1 has potent antifungal activities. SDH-IN-1 displays potent activity against S. sclerotiorum (EC50 of 0.14 mg/L).
|
-
- HY-126254
-
|
BI-4924
|
Others
|
Cancer
|
|
BI-4924 is a lipophilic, highly plasma protein bound selective phosphoglycerate dehydrogenase (PHGDH) inhibitor (IC50=3 nM) with excellent microsomal, as well as hepatocytic stability. Intracellular trapping of BI-4924 disrupts serine biosynthesis with an IC50 of 2200 nM at 72 h.
|
-
- HY-103394
-
|
TC HSD 21
|
Others
|
Cancer
|
|
TC HSD 21 is a potent 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitor with an IC50 of 14 nM. TC HSD 21 shows excellent selectivity over 17β-HSD isoenzymes and nuclear receptors.
|
-
- HY-145848
-
-
- HY-B0199
-
|
Mycophenolate Mofetil
RS 61443; TM-MMF
|
Drug Metabolite
Apoptosis
|
Cancer
|
|
Mycophenolate mofetil (RS 61443) is the morpholinoethylester prodrug of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation.
|
-
- HY-135666
-
-
- HY-138686
-
-
- HY-101232
-
|
Tiotidine
ICI 125211
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Tiotidine (ICI 125211) is a potent and selective antagonist of histamine H2-receptor (pA2=7.3-7.8 for guinea-pig right atrium). Tiotidine has low affinity for both the H1 and the H3 receptors.
|
-
- HY-132171A
-
|
DSM705 hydrochloride
|
Dihydroorotate Dehydrogenase
Parasite
|
Infection
|
|
DSM705 hydrochloride, an orally active antimalarial compound, is a pyrrole-based Dihydroorotate Dehydrogenase (DHODH) inhibitor. DSM705 hydrochloride exhibits nanomolar potency against Plasmodium DHODH and Plasmodium parasites (IC50=95, 52 nM for P. falciparum and P. vivax DHODH, respectively), with no inhibition of mammalian DHODHs.
|
-
- HY-146733
-
-
- HY-145364
-
-
- HY-13423
-
-
- HY-130251
-
|
DS18561882
|
Others
|
Cancer
|
|
DS18561882 is a highly potent, isozyme-selective methylenetetrahydrofolate dehydrogenase 2 (MTHFD2) inhibitor with an IC50 value of 0.0063 μM. DS18561882 also has inhibitory effect on MTHFD1 (IC50=0.57 μM). DS18561882 exhibits a good oral pharmacokinetic profile.
|
-
- HY-N0157
-
|
Orotic acid
6-Carboxyuracil; Vitamin B13
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats.
|
-
- HY-129239
-
|
Farudodstat
ASLAN003
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Farudodstat (ASLAN003) is an orally active and potent Dihydroorotate Dehydrogenase (DHODH) inhibitor with an IC50 of 35 nM for human DHODH enzyme. Farudodstat inhibits protein synthesis via activation of AP-1 transcription factors. Farudodstat induces apoptosis and substantially prolongs survival in acute myeloid leukemia (AML) xenograft mice.
|
-
- HY-N0157A
-
|
Orotic acid zinc
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (zinc), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid (zinc) is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid (zinc) can induce hepatic steatosis and hepatomegaly in rats.
|
-
- HY-121488
-
-
- HY-146275
-
|
LXRβ agonist-3
|
LXR
|
Cancer
|
|
LXRβ agonist-3 (compound 4-13) is a potent and selective LXRβ (liver X receptor β) agonist, with an EC50 of 0.095 μM. LXRβ agonist-3 efficiently inhibits U87EGFRvIII cell, with an IC50 of 3.75 μM. LXRβ agonist-3 shows antitumor activity, and can inhibit glioblastoma.
|
-
- HY-133898
-
-
- HY-146552
-
|
PDHK-IN-4
|
PDHK
|
Cancer
Metabolic Disease
|
|
PDHK-IN-4 (Compound 30) is a potent inhibitor of PDHK with IC50s of 0.0051 and 0.0122 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating drug targets for numerous diseases, including diabetes and cancers. PDHK-IN-4 has the potential for the research of cancer diseases.
|
-
- HY-10545
-
|
Taribavirin
|
HBV
HCV
|
Infection
|
|
Taribavirin is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin, is a ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
|
-
- HY-18767
-
|
Ivosidenib
AG-120
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
Metabolic Disease
|
|
Ivosidenib (AG-120) is an orally active inhibitor of isocitrate dehydrogenase 1 mutant (mIDH1) enzyme, it exhibits profound d-2-hydroxyglutatrate (2-HG) lowering in vivo. Ivosidenib (AG-120) has the potential for AML therapy due to its acceptable safety profile and clinical activity.
|
-
- HY-145381
-
|
11β-HSD1-IN-6
|
Others
|
Metabolic Disease
|
|
11β-HSD1-IN-6 is a an 11β-HSD-1 inhibitor. The 11β hydroxysteroid dehydrogenase enzymes (11β-HSDs) mediate the interconversion of the glucocorticoid (GC) corticosterone or cortisol to an inactive form, 11-dehydrocorticosterone (11-DHC) or Cortisone, respectively.
|
-
- HY-10545A
-
|
Taribavirin hydrochloride
|
HBV
HCV
|
Infection
|
|
Taribavirin hydrochloride is an orally active inosine monophosphate dehydrogenase inhibitor, has activity against a wide range of viruses, especially the hepatitis C virus and influenza virus. Taribavirin hydrochloride is a Ribavirin prodrug, is designed to concentrate within the liver to target HCV-infected hepatocytes while minimizing distribution within red blood cells (RBCs) and the development of hemolytic anemia.
|
-
- HY-146554
-
|
PDHK-IN-5
|
PDHK
|
Cancer
|
|
PDHK-IN-5 (Compound 19) is a potent inhibitor of PDHK with IC50s of 0.006 and 0.0329 μM for PDHK2 and PDHK4, repectively. Pyruvate dehydrogenase kinases (PDHKs) are fascinating drug targets for numerous diseases, including diabetes and cancers. PDHK-IN-5 has the potential for the research of cancer diseases.
|
-
- HY-101930B
-
|
(R)-BMS-816336
|
Others
|
Metabolic Disease
|
|
(R)-BMS-816336 (Compound 6n-1) is a potent and orally active inhibitor of human, mouse and cynomolgus monkey 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 14.5 nM, 50.3 nM and 16 nM, respectively .
|
-
- HY-147628
-
-
- HY-147626
-
-
- HY-P3376
-
-
- HY-14234
-
-
- HY-107539
-
|
GPR35 agonist 4
|
Others
|
Others
|
|
GPR35 agonist 4 (compound 10) is a potent GPR35 agonist with an pEC50 of 5.86. GPR35 agonist 4 shows high potency human and rat GPR35. Mutation of arginine 3.36 eliminates agonist function of GPR35 agonist 4.
|
-
- HY-123943
-
|
STING agonist-4
|
STING
|
Cancer
|
|
STING agonist-4 is an stimulator of Interferon Genes (STING) receptor agonist with an apparent inhibitory constant (IC50) of 20 nM. STING agonist-4 is a two symmetry-related amidobenzimidazole (ABZI)-based compound to create linked ABZIs (diABZIs) with enhanced binding to STING and cellular function.
|
-
- HY-145393
-
-
- HY-12762
-
|
QS11
|
Others
|
Cancer
|
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 µM. QS11 modulates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells.
|
-
- HY-12721
-
-
- HY-10555
-
|
AMG-221
|
Others
|
Metabolic Disease
|
|
AMG-221 is an inhibitor of 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) with a Ki of 12.8 nM in vitro biochemical scintillation proximity assay (SPA) and an IC50 of 10.1 nM in cell-based assays. AMG-221 can be used for the research of type 2 diabetes.
|
-
- HY-N0108
-
|
Physcion
Parietin; Rheochrysidin
|
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Physcion (Parietin) is an anthraquinone isolated from traditional Chinese medicine Radix et Rhizoma Rhei, acts as an inhibitor of 6-phosphogluconate dehydrogenase, with an IC50 and a Kd of 38.5 μM and 26.0 μM, respectively. Physcion (Parietin) exhibits laxative, hepatoprotective, anti-inflammatory, anti-microbial, anti-proliferative and anti-tumor effects.
|
-
- HY-113377
-
|
L-Glyceric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Glyceric acid is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid excretion to distinguish PH1 from PH2.
|
-
- HY-113377A
-
|
L-Glyceric acid sodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Glyceric acid sodium is a mainly urinary metabolite accumulating in rare inherited metabolic disease L-glyceric aciduria. L-Glyceric acid sodium can be used to diagnose primary hyperoxaluria type 2 (PH2). L-Glyceric acid sodium excretion to distinguish PH1 from PH2.
|
-
- HY-17354
-
-
- HY-131145
-
-
- HY-139586
-
-
- HY-112921B
-
-
- HY-112921A
-
-
- HY-131974
-
-
- HY-146141
-
-
- HY-147028
-
-
- HY-126321
-
|
RORγt agonist 1
|
ROR
|
Cancer
|
|
RORγt agonist 1 (compound 14) is a potent, orally bioavailable RORγt agonist with an EC50 of 20.8 nM. RORγt agonist 1 showes high metabolic stability, improved aqueous solubility and excellent mouse PK profile. RORγt agonist 1 is a potential candidate of RORγt agonist for cancer immunotherapy.
|
-
- HY-103665A
-
|
STING agonist-3 trihydrochloride
|
STING
|
Cancer
|
|
STING agonist-3 trihydrochloride, extracted from patent WO2017175147A1 (example 10), is a selective and non-nucleotide small-molecule STING agonist with a pEC50 and pEC50 of 7.5 and 9.5, respectively. STING agonist-3 trihydrochloride has durable anti-tumor effect and tremendous potential to improve treatment of cancer.
|
-
- HY-113308A
-
-
- HY-100699
-
-
- HY-17354A
-
-
- HY-139575
-
-
- HY-128127
-
|
NAEPA
|
LPL Receptor
|
Others
|
|
NAEPA, a phosphate-mimetic derivative, is a lysophosphatidic acid (LPA) receptor agonist.
|
-
- HY-118539
-
-
- HY-135954A
-
|
PDK4-IN-1 hydrochloride
|
PDHK
Apoptosis
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
PDK4-IN-1 hydrochloride is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 hydrochloride potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 hydrochloride has antidiabetic, anticancer and anti-allergic activity.
|
-
- HY-10617
-
|
Rucaparib phosphate
AG-014699 phosphate; PF-01367338 phosphate
|
PARP
|
Cancer
|
|
Rucaparib (AG014699) phosphate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib phosphate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib phosphate has the potential for castration-resistant prostate cancer (CRPC) research.
|
-
- HY-B0199S
-
|
Mycophenolate Mofetil-d4
|
Drug Metabolite
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Mycophenolate Mofetil-d4 is the deuterium labeled Mycophenolate Mofetil. Mycophenolate mofetil (RS 61443) is the morpholinoethylester prodrug of Mycophenolic acid. Mycophenolate mofetil inhibits de novo purine synthesis via the inhibition of inosine monophosphate dehydrogenase (IMPDH). Mycophenolate mofetil shows selective lymphocyte antiproliferative effects involve both T and B cells, preventing antibody formation.
|
-
- HY-101813
-
|
Laflunimus
HR325
|
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Laflunimus (HR325) is an immunosuppressive agent and an analogue of the Leflunomide-active metabolite A77 1726. Laflunimus is an orally active inhibitor of dihydroorotate dehydrogenase (DHODH). Laflunimus suppresses immunoglobulin (Ig) secretion, with IC50 values of 2.5 and 2 µM for IgM and IgG, respectively. Laflunimus also is a prostaglandin endoperoxide H synthase (PGHS) -1 and -2 inhibitor.
|
-
- HY-10617A
-
|
Rucaparib
AG014699; PF-01367338
|
PARP
|
Cancer
|
|
Rucaparib (AG014699) is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib has the potential for castration-resistant prostate cancer (CRPC) research.
|
-
- HY-W010342
-
|
6-Aminonicotinamide
|
Others
|
Cancer
|
|
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells.
|
-
- HY-135954
-
|
PDK4-IN-1
|
PDHK
Apoptosis
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
PDK4-IN-1 is an anthraquinone derivative and a potent and orally active pyruvate dehydrogenase kinase 4 (PDK4) inhibitor with an IC50 value of 84 nM. PDK4-IN-1 potently represses cellular transformation and cellular proliferation and induces apoptosis. PDK4-IN-1 has antidiabetic, anticancer and anti-allergic activity.
|
-
- HY-132174
-
|
CHIKV-IN-2
|
Dihydroorotate Dehydrogenase
|
Infection
|
|
CHIKV-IN-2 is a potent inhibitor against Chikungunya virus (CHIKV), with excellent cellular antiviral activity (EC90=270 nM) and improved liver microsomal stability. CHIKV-IN-2 shows inhibitory activity against a cellular target Dihydroorotate Dehydrogenase (DHODH), which interacts with various viruses and regulate their replication via depleting intracellular pyrimidine pools.
|
-
- HY-124593
-
|
PTC299
|
VEGFR
Dihydroorotate Dehydrogenase
DNA/RNA Synthesis
|
Cancer
|
|
PTC299 is an orally active inhibitor of VEGFA mRNA translation that selectively inhibits VEGF protein synthesis at the post-transcriptional level. PTC299 is also a potent inhibitor of dihydroorotate dehydrogenase (DHODH). PTC299 shows good oral bioavailability and lack of off-target kinase inhibition and myelosuppression. PTC299 can be useful for the research of hematologic malignancies.
|
-
- HY-18056
-
|
PF-915275
|
Others
|
Metabolic Disease
|
|
PF-915275 is a potent, selective and orally active human 11β-hydroxysteroid dehydrogenase type 1 (11βHSD1) inhibitor with a Ki of 2.3 nM and an EC50 of 15 nM (in HEK293 cells). The dose-dependent effect of PF-915275 on conversion of cortisone to cortisol in primary human and monkey hepatocytes, with an EC50 of 20 and 100 nM, respectively.
|
-
- HY-146482
-
|
PPARγ agonist 6
|
PPAR
|
Cancer
|
|
PPARγ agonist 6 (Compound 12) is a potent and selective agonist of PPARγ. PPARγ agonist 6 has the potential for the research of cancer diseases.
|
-
- HY-146480
-
|
PPARγ agonist 5
|
PPAR
|
Cancer
|
|
PPARγ agonist 5 (Compound 1) is a potent and selective agonist of PPARγ. PPARγ agonist 5 has the potential for the research of cancer diseases.
|
-
- HY-114400A
-
-
- HY-146438
-
|
PPARγ agonist 3
|
PPAR
|
Cancer
|
|
PPARγ agonist 3 (Compound 18a) is a potent and selective agonist of PPARγ. PPARγ agonist 3 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 3 exerts antitumor potency only in combination with Imatinib.
|
-
- HY-B2245
-
-
- HY-107399
-
-
- HY-N10123
-
-
- HY-115762
-
-
- HY-19923
-
-
- HY-P0236A
-
-
- HY-139126
-
-
- HY-110304
-
-
- HY-136435
-
-
- HY-112921
-
-
- HY-146439
-
|
PPARγ agonist 4
|
PPAR
|
Cancer
|
|
PPARγ agonist 4 (Compound 18b) is a potent and selective agonist of PPARγ. PPARγ agonist 4 is not cytotoxic neither on non-resistant nor on resistant cells. PPARγ agonist 4 exerts antitumor potency only in combination with Imatinib.
|
-
- HY-147736
-
|
GABAA receptor agonist 2
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor agonist 2 (compound 4c) is a potent GABAA receptor agonist. GABAA receptor agonist 2 shows anti-depression activities in classical mouse models of depression of FST and TST. GABAA receptor agonist 2 binds at the GABA binding site of GABAA receptor in order to produce GABAergic effects. GABAA receptor agonist 2 has the potential for the research of depression.
|
-
- HY-147501
-
|
TRβ agonist 3
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
TRβ agonist 3 (Compound 3) is a potent agonist of TRβ. TRβ agonist 3 reduces lipid accumulation in HepG2 and promote lipolysis with comparable effects. TRβ agonist 3 is a new potential TRβ-selective thyromimetics.
|
-
- HY-147500
-
|
TRβ agonist 2
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
TRβ agonist 2 (Compound 1) is a potent agonist of TRβ. TRβ agonist 2 reduces lipid accumulation in HepG2 and promote lipolysis with comparable effects. TRβ agonist 2 is a new potential TRβ-selective thyromimetics.
|
-
- HY-142697
-
|
SGC agonist 1
|
Others
|
Cardiovascular Disease
|
|
SGC agonist 1 is a potent agonist of soluble guanylate cyclase (SGC). SGC agonist 1 improves solubility combined with high cell permeability. SGC agonist 1 has the potential for the research of cardiovascular disease (extracted from patent WO2016030354A1, compound 18A).
|
-
- HY-114400
-
-
- HY-P3366
-
-
- HY-111358
-
-
- HY-132909
-
-
- HY-101492
-
-
- HY-147511
-
|
PPARγ agonist 7
|
PPAR
|
Others
|
|
PPARγ agonist 7 (Compound 3a) is a potent and selective agonist of PPARγ. PPARγ agonist 7 promotes adiponectin production in human bone marrow mesenchymal stem cells (hBM-MSCs) as a novel PPARγ full agonist (EC50, 4.34 μM).
|
-
- HY-128855
-
|
Talsaclidine
|
mAChR
|
Neurological Disease
|
|
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.
|
-
- HY-19574
-
-
- HY-100012
-
|
CBR-5884
|
Others
|
Cancer
|
|
CBR-5884 is an active, selective inhibitor of phosphoglycerate dehydrogenase (PHGDH) with an IC50 of 33 μM. CBR-5884 inhibits de novo serine synthesis in cancer cells and is selectively toxic to cancer cell lines with high serine biosynthetic activity. CBR-5884 selectively inhibits the proliferation of melanoma and breast cancer lines that have a high propensity for serine synthesis.
|
-
- HY-101930A
-
|
(Rac)-BMS-816336
|
Others
|
Metabolic Disease
|
|
(Rac)-BMS-816336 (Compound 6n) is a racemate of BMS-816336. (Rac)-BMS-816336 is a potent inhibitor of human and mouse 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) enzyme with IC50s of 10 nM and 68 nM, respectively. (Rac)-BMS-816336 has good metabolic stability.
|
-
- HY-18173
-
|
AZD8329
|
Others
|
Metabolic Disease
|
|
AZD8329 is a potent 11β-Hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor with an IC50 of 9 nM for human 11β-HSD1, displays excellent selectivity versus 11β-HSD2, 17β-HSD1 and 17β-HSD3.
|
-
- HY-126293
-
|
Apelin agonist 1
|
Others
|
Cardiovascular Disease
|
|
Apelin agonist 1 is an oral selective apelin agonist AM-2995, a agonist of the APJ (APLNR, angiotensin receptor like-1) receptor, may be used in the treatment of cardiovascular conditions. Apelin agonist 1 is extracted from patent WO 2018097944 (210.0), Example 210.0.
|
-
- HY-W014325
-
-
- HY-135400
-
-
- HY-143227
-
-
- HY-10448A
-
-
- HY-139017
-
-
- HY-144339
-
|
AhR agonist 2
|
Others
|
Others
|
|
AhR agonist 2 (Compound 12a) is a potent agonist of aryl hydrocarbon receptor (AhR) with an EC50 of 0.03 nM. AhR agonist 2 induces rapid nuclear enrichment of AhR, triggers the transcription of downstream genes and promote skin barrier repair. AhR agonist 2 has the potential for the research of psoriasis.
|
-
- HY-120273
-
-
- HY-139017A
-
-
- HY-139876
-
-
- HY-13239
-
-
- HY-N9333
-
-
- HY-112597
-
-
- HY-132900
-
|
RORγ agonist 1
|
ROR
|
Cancer
|
|
RORγ agonist 1 is a potent and orally bioavailable RORγ agonist (EC50 = 21 nM) with antitumor activity.
|
-
- HY-107673
-
-
- HY-131105S
-
-
- HY-100120
-
-
- HY-P1738
-
-
- HY-109131
-
-
- HY-13653
-
-
- HY-15510B
-
|
Tenovin-6 Hydrochloride
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6 Hydrochloride, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 Hydrochloride inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 Hydrochloride also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-114226
-
|
Olutasidenib
FT-2102
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
Inflammation/Immunology
|
|
Olutasidenib (FT-2102) is a highly potent, orally active, brain penetrant and selective inhibitor of mutant Isocitrate dehydrogenase 1 (IDH1), with IC50 values of 21.2 nM and 114 nM for IDH1- R132H and IDH1- R132C, respectively . Olutasidenib (FT-2102) is under the study in the treatment of acute myeloid leukemia (AML) or myelodysplastic syndrome (MDS) .
|
-
- HY-114855
-
|
BT2
|
Bcl-2 Family
|
Metabolic Disease
|
|
BT2 is a BCKDC kinase (BDK) inhibitor with an IC50 of 3.19 μM. BT2 binding to BDK triggers helix movements in the N-terminal domain, resulting in the dissociation of BDK from the branched-chain α-ketoacid dehydrogenase complex (BCKDC). BT2 (compound 4) is also a potent and selective Mcl-1 inhibitor with a Ki value of 59 μM.
|
-
- HY-15510
-
|
Tenovin-6
|
MDM-2/p53
Dihydroorotate Dehydrogenase
Sirtuin
Autophagy
|
Cancer
|
|
Tenovin-6, an analog of Tenovin-1 (HY-13423), is an activator of p53 transcriptional activity. Tenovin-6 inhibits the protein deacetylase activities of purified human SIRT1, SIRT2, and SIRT3 with IC50s of 21 μM, 10 μM, and 67 μM, respectively. Tenovin-6 also inhibits dihydroorotate dehydrogenase (DHODH).
|
-
- HY-102003
-
|
Rucaparib monocamsylate
AG014699 monocamsylate; PF-01367338 monocamsylate
|
PARP
|
Cancer
|
|
Rucaparib (AG014699) monocamsylate is an orally active, potent inhibitor of PARP proteins (PARP-1, PARP-2 and PARP-3) with a Ki of 1.4 nM for PARP1. Rucaparib monocamsylate is a modest hexose-6-phosphate dehydrogenase (H6PD) inhibitor. Rucaparib monocamsylate has the potential for castration-resistant prostate cancer (CRPC) research.
|
-
- 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-146731
-
|
PPARγ agonist 1
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
|
PPARγ agonist 1 (compound 15) is a potent agonist of PPARγ. PPARγ agonist 1 shows high efficacy to activate hPPARγ without raising a full agonism and probably avoiding adverse effects. PPARγ agonist 1 has the potential for the research of cardiovascular diseases associated with metabolic disorders.
|
-
- HY-145284
-
|
APJ receptor agonist 4
|
Others
|
Cardiovascular Disease
|
|
APJ receptor agonist 4 is a potent and orally active agonist of apelin receptor (APJ) with EC50 and Ki of 0.06 nM and 0.07 nM respectively. APJ receptor agonist 4 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 4 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 4 leads to improved cardiac function and can be used for researching the HF disease.
|
-
- HY-145285
-
|
APJ receptor agonist 5
|
Others
|
Cardiovascular Disease
|
|
APJ receptor agonist 5 (compound 3) is a potent and orally active agonist of apelin receptor (APJ) with an EC50 of 0.4 nM. APJ receptor agonist 5 displays excellent pharmacokinetic profiles in the rodent heart failure (HF) model. APJ receptor agonist 5 also shows an acceptable safety profile in preclinical toxicology studies. APJ receptor agonist 5 leads to improved cardiac function and can be used for researching the HF disease.
|
-
- HY-102053
-
-
- HY-135399
-
-
- HY-N2992
-
-
- HY-145279
-
-
- HY-12721S
-
-
- HY-100815A
-
-
- HY-132217
-
-
- HY-144549
-
|
LXR agonist 1
|
LXR
|
Cardiovascular Disease
|
|
LXR (Liver X receptor) agonist 1 is potent LXR agonist with AC50s of 1.5 nM and 12 nM for LXR-α and LXR-β, respectively. LXR agonist 1 has the potential for the research of atherosclerosis.
|
-
- HY-144168
-
-
- 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-142806
-
|
RORγt inverse agonist 26
|
ROR
|
Inflammation/Immunology
|
|
RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .
|
-
- HY-111353
-
-
- HY-139709
-
-
- HY-139710
-
-
- HY-145961
-
-
- HY-107581
-
-
- HY-146742
-
-
- HY-19673A
-
-
- HY-135982
-
|
GPR81 agonist 1
|
Others
|
Metabolic Disease
|
|
GPR81 agonist 1 is a potent and highly selective GPR81 agonist, with EC50s of 58 nM and 50 nM for human and mouse GPR81, respectively. GPR81 agonist 1 inhibits lipolysis in differentiated 3T3-L1 adipocytes. GPR81 agonist 1 suppresses lipolysis in mice without cutaneous flushing. GPR81 agonist 1 displays remarkable selectivity for GPR81 over GPR109a.
|
-
- HY-141454A
-
-
- HY-141454
-
-
- HY-107688A
-
|
UB-165 fumarate
|
nAChR
|
Neurological Disease
|
|
UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for nicotine binding in rat brain.
|
-
- HY-10020
-
|
Varenicline Hydrochloride
CP 526555 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.
|
-
- HY-B0968A
-
|
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-B0968
-
|
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-131104S
-
-
- HY-111748
-
-
- HY-103039
-
-
- HY-136449
-
-
- HY-121404A
-
|
Muscarine chloride
(+)-Muscarine chloride
|
mAChR
|
Neurological Disease
|
|
Muscarine ((+)-Muscarine) chloride is a toxin that can stimulate the parasympathetic nervous system. Muscarine is a prototype muscarinic acetylcholine receptor agonist.
|
-
- HY-100699S
-
-
- HY-P1144
-
-
- HY-U00395
-
-
- HY-131104AS
-
-
- HY-100087
-
-
- HY-147637
-
|
EphA2 agonist 1
|
Ephrin Receptor
|
Cancer
|
|
EphA2 agonist 1 (Compound 7bg) is a potent EphA2 receptor agonist. EphA2 agonist 1 shows great potency and selectivity toward EphA2 overexpressed glioblastoma cells and stimulates EphA2 phosphorylation.
|
-
- HY-119943B
-
|
(R)-PF-06256142
|
Others
|
Neurological Disease
|
|
(R)-PF-06256142 is the R enantiomer of PF-06256142 with low active. PF-06256142 is a potent and selective orthosteric D1 receptor agonist that can reduce receptor desensitization relative to dopamine and other catechol-containing agonists.
|
-
- 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-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-132195
-
|
RORγt inverse agonist 14
|
ROR
|
Inflammation/Immunology
|
|
RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis.
|
-
- HY-139847
-
-
- HY-115765
-
-
- HY-139694
-
-
- HY-142159
-
-
- HY-111359
-
-
- HY-103083
-
-
- HY-113308AS
-
-
- HY-P1144A
-
-
- HY-137320
-
|
diABZI-C2-NH2
|
STING
|
Cancer
|
|
diABZI-C2-NH2, an active analogue containing a primary amine functionality, is a STING agonist.
|
-
- HY-101039A
-
-
- HY-112679
-
-
- HY-141873
-
|
Wnt/β-catenin agonist 2
|
β-catenin
|
Others
|
|
Wnt/β-catenin agonist 2 is a potent Wnt agonist. Wnt/β-catenin agonist 2 activates Wnt/β-catenin signaling and can be used in the research of diseases related to the signal transduction. (From patent WO2007078113A1, compound 39)
|
-
- HY-139702
-
|
α5β1 integrin agonist-1
|
Integrin
|
Cancer
|
|
α5β1 integrin agonist-1, acting as α5β1 integrin agonist, is able to selectively deliver 5-FU into tumor cells, successfully leading to cancer cell death.
|
-
- HY-147625
-
-
- HY-133036
-
|
APJ receptor agonist 1
|
Others
|
Cardiovascular Disease
|
|
APJ receptor agonist 1, a biphenyl acid derivative, is a potent APJ receptor (APJ-R) agonist (EC50s 0.093 and 0.12 nM for human and rat APJ-R, respectively). APJ receptor agonist 1 displays in vitro potency to apelin-13, the endogenous peptidic ligand for the APJ receptor. APJ receptor agonist 1 has the potential for the research of heart failure.
|
-
- HY-13288
-
-
- HY-138695
-
-
- HY-108415
-
-
- HY-147623
-
-
- HY-136435S1
-
-
- HY-113308AS2
-
-
- HY-115763
-
-
- HY-19522
-
|
Seladelpar
MBX-8025
|
PPAR
|
Metabolic Disease
|
|
Seladelpar (MBX-8025) is an orally active, potent (50% effect concentration EC50 2 nM), and specific PPAR-δ agonist.
|
-
- HY-107654
-
|
Muscarine iodide
(+)-Muscarine iodide
|
mAChR
|
Neurological Disease
|
|
Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist.
|
-
- HY-113308AS1
-
-
- HY-U00340
-
|
PPAR agonist 1
|
PPAR
|
Metabolic Disease
|
|
PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.
|
-
- HY-111583
-
|
RXFP3/4 agonist 1
|
Others
|
Metabolic Disease
|
|
RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC50s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats.
|
-
- HY-19711
-
|
STING agonist-1
G10
|
STING
Virus Protease
|
Infection
|
|
STING agonist-1 (G10) is human-specific STING agonist that elicits antiviral activity against emerging Alphaviruses. G10 potently blocks replication of Alphavirus species Venezuelan Equine Encephalitis Virus (VEEV) with IC90 of 24.57 μM.
|
-
- HY-128353
-
|
ROR agonist-1
|
ROR
|
Inflammation/Immunology
|
|
ROR agonist-1 is a potent and orally bioavailable inverse agonist of the retinoic acid receptor-related orphan receptor C2 (RORC2), inhibition of IL-17A production from human primary TH 17 cells with a pIC50 of 7.5.
|
-
- HY-146997
-
|
TRβ agonist 1
|
Thyroid Hormone Receptor
|
Metabolic Disease
|
|
TRβ agonist 1 is a selective and mutation-sensitive thyroid hormone receptor β (TRβ) agonist, with an EC50 value of 21 nM. TRβ agonist 1 can be used for researching dyslipidemia, nonalcoholic steatohepatitis (NASH), and resistance to thyroid hormone (RTH).
|
-
- HY-147512
-
|
CB1/2 agonist 1
|
Cannabinoid Receptor
|
Inflammation/Immunology
|
|
CB1/2 agonist 1 is a potent and cross the blood-brain barrier CB1/2 agonist with EC50s of 56.15, 11.63 nM for CB1R and CB2R, respectively. CB1/2 agonist 1 reduces glutamate release and LPS-induced activation of microglial cells. CB1/2 agonist 1 shows anti-inflammatory and antinociceptive effects. CB1/2 agonist 1 has the potential for the research of multiple sclerosis.
|
-
- HY-100469
-
|
LXRβ agonist-2
|
LXR
|
Cardiovascular Disease
|
|
LXRβ agonist-2 is a highly potent and β-selective liver X receptor (LXRβ) agonist with EC50 of 7 nM, displays 28.5-fold selectivity over LXRα (EC50=200 nM) and used in the treatment of atherosclerosis.
|
-
- HY-141494
-
|
Pparδ agonist 5
|
PPAR
|
Metabolic Disease
|
|
Pparδ agonist 5, an orally active PPARδ-selective agonist (EC50=0.335 μM), is much greater than that of the prototypical standard GW0742. Pparδ agonist 5 promotes improvements in bone density and microarchitecture in vivo.
|
-
- HY-12405
-
-
- HY-147629
-
-
- HY-108711
-
-
- HY-136608
-
-
- HY-136609
-
-
- HY-114321
-
-
- HY-138996
-
|
GLP-1 receptor agonist 8
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 8 is a potent agonist of GLP-1 R. GLP-1 receptor agonist 8 has the potential for the research of diabetes, obesity, and nonalcoholic fatty liver disease (NAFLD) (extracted from patent WO2019239319A1, compound 17).
|
-
- HY-17405
-
-
- HY-100810
-
-
- HY-B0968S
-
|
Trimetazidine-d8 dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
|
Trimetazidine-d8 dihydrochloride is the deuterium labeled Trimetazidine dihydrochloride. Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-145286
-
|
IMPDH2-IN-2
|
Others
|
Cancer
Infection
|
|
IMPDH2-IN-2 is a potent inhibitor of inosine 5’-monophosphate dehydrogenase (IMPDH) with a Ki,app value of 14 μM, respectively. IMPDH2-IN-2 displays moderate antibacterial activity (MIC = 6.3 and 11 μM in minimal GAST/Fe and rich 7H9/ADC/Tween media, respectively). IMPDH2-IN-2 is a potential anti-tuberculosis agent.
|
-
- HY-111262
-
|
ABT-384
|
Others
|
Metabolic Disease
Neurological Disease
|
|
ABT-384 is a potent, selective 11-β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor. ABT-384 exhibits high affinity (Ki 0.1-2.7 nM) against rodent, monkey, and human 11β-HSD1. ABT-384 blocks regeneration of active cortisol. ABT-384 can be used for the research of Alzheimer’s disease (AD).
|
-
- HY-145458
-
-
- HY-B1161
-
|
Methoprene
ZR-515
|
Others
|
Others
|
|
Methoprene, an insect juvenile growth hormone mimic, is a growth-regulating insecticide that manifests its toxicity to target organisms by acting as a juvenile hormone agonist.
|
-
- HY-12835
-
-
- HY-107471
-
|
CB2 receptor agonist 3
GP2a
|
Cannabinoid Receptor
|
Cancer
|
|
CB2 receptor agonist 3 is a robust and selective CB2 cannabinoid agonist with Kis of 7.6 and 900 nM for CB2 and CB1, respectively. CB2 receptor agonist 3 significantly increases P-ERK 1/2 expression in HL-60 cells.
|
-
- HY-142701
-
|
SSTR4 agonist 4
|
Others
|
Neurological Disease
|
|
SSTR4 agonist 4 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 4 has the potential for the research of pain (extracted from patent WO2021233428A1, compound 14).
|
-
- 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-144111
-
|
PPARα/δ agonist 1
|
PPAR
|
Inflammation/Immunology
|
|
PPARα/δ agonist 1 is a potent PPARα/PPARδ dual agonist (PPARα EC50=7.0 nM; PPARδ EC50=8.4 nM). PPARα/δ agonist 1 is a high selectivity over PPARγ (PPARγ EC50=1316.1 nM). PPARα/δ agonist 1 has the potential for the research of nonalcoholic steatohepatitis.
|
-
- HY-142700
-
|
SSTR4 agonist 3
|
Others
|
Neurological Disease
|
|
SSTR4 agonist 3 is a potent agonist of SSTR4. SSTR4 is expressed at relatively high levels in the hippocampus and neocortex, memory and learning regions, and Alzheimer's disease pathology. SSTR4 agonists are potent in rodent models of pain associated with acute and chronic associated anti-peripheral nociceptive and anti-inflammatory activity. SSTR4 agonist 3 has the potential for the research of pain (extracted from patent WO2021233427A1, compound 14).
|
-
- HY-13660
-
-
- HY-100234A
-
-
- HY-109136
-
|
Runcaciguat
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Runcaciguat is an orally active stimulator of soluble guanylate cyclase, and is used in the research of cardiovascular and renal diseases combined with selective partial adenosine A1 receptor agonists.
|
-
- HY-112185
-
-
- HY-144133
-
-
- HY-100234
-
-
- HY-W002116
-
-
- 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-142699
-
|
SSTR4 agonist 2
|
Others
|
Inflammation/Immunology
|
|
SSTR4 agonist 2 is a potent agonist of somatostatin receptor subtype 4 (SSTR4). SSTR4 pathway inhibits nociceptive and inflammatory processes. SSTR4 agonist 2 has the potential for the research of medical disorders related to SSTR4 (extracted from patent WO2014184275A1, compound 107).
|
-
- HY-114310
-
|
VDR agonist 1
|
VD/VDR
Apoptosis
|
Cancer
|
|
VDR agonist 1 (compound 28) is a nonsteroidal Vitamin D receptor (VDR) agonist, with an IC50 of 690 nM in MCF-7 cells. VDR agonist 1 arrests the cell cycle through the up-regulation of p21 and p27, promotes apoptosis by increasing the expression of BAX and decrease the expression of Bcl-2.
|
-
- HY-42068
-
-
- HY-B1829A
-
-
- HY-101717
-
-
- HY-U00281
-
-
- HY-U00227
-
-
- HY-17354S
-
-
- HY-147627
-
-
- HY-108566
-
-
- HY-144136
-
-
- HY-135400S
-
-
- HY-144034
-
|
GLP-1R agonist 3
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1R agonist 3 is a potent agonist of GLP-1R. GLP-1R agonist 3 is a thickened imidazole derivative compound. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 3 has the potential for the research of diabetes (extracted from patent WO2021197464A1, compound 1).
|
-
- HY-144033
-
|
GLP-1R agonist 1
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1R agonist 1 is a potent agonist of GLP-1R. GLP-1R agonist 1 is a thickened imidazole derivative compound. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 1 has the potential for the research of diabetes (extracted from patent WO2021197464A1, compound 4).
|
-
- HY-143614
-
|
THR-β agonist 3
|
Others
|
Metabolic Disease
|
|
THR-β agonist 3 is a potent agonist of THR-β. THR-β agonist 3 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021129827A1, compound 6).
|
-
- HY-143613
-
|
THR-β agonist 2
|
Others
|
Metabolic Disease
|
|
THR-β agonist 2 is a potent agonist of THR-β. THR-β agonist 2 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021121210A1, compound 3).
|
-
- HY-142917
-
|
THR-β agonist 4
|
Others
|
Metabolic Disease
|
|
THR-β agonist 4 is a potent agonist of THR-β. THR-β agonist 4 has the potential for the research of metabolic diseases such as obesity, hyperlipidemia, hypercholesterolemia, diabetes and other conditions such as steatosis and non-alcoholic steatohepatitis (NASH), atherosclerosis and other related conditions and diseases (extracted from patent WO2021143706A1, compound 72).
|
-
- HY-129657
-
|
GLP-1 receptor agonist 4
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 4 is a glucagon-like peptide-1 receptor (GLP-1R) agonist extracted from patent WO2009111700A2, compound 87, has an EC50 of 64.5 nM. GLP-1 receptor agonist 4 can be used in the research for treatment of diabetes.
|
-
- HY-10559
-
|
Nelotanserin
APD125
|
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
|
-
- HY-100380
-
-
- HY-115764
-
-
- HY-104026S
-
-
- HY-18776
-
-
- HY-U00396
-
-
- HY-114411
-
-
- HY-B1540
-
-
- HY-135460
-
-
- HY-P1000
-
-
- HY-19065
-
-
- HY-P0187
-
-
- HY-P1504
-
-
- HY-B0716S
-
-
- HY-10013
-
|
Taranabant
MK-0364
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
Taranabant is a highly potent and selective cannabinoid 1 (CB1) receptor inverse agonist that inhibits the binding and functional activity of various agonists, with a binding Ki of 0.13 nM for the human CB1R in vitro.
|
-
- HY-P2518
-
-
- HY-144604
-
|
FPR2 agonist 2
|
Others
|
Infection
Neurological Disease
|
|
FPR2 agonist 2 is a potent and permeates the blood−brain barrier FPR2 agonist with an EC50 of 0.13 µM, 1.1 µM for FPR2 and FPR1, respectively. FPR2 agonist 2 inhibits the production of pro-inflammatory cytokines, counterbalances the changes in mitochondrial function, and inhibits caspase-3 activity.
|
-
- HY-143880
-
|
MRGPRX1 agonist 4
|
Others
|
Neurological Disease
|
|
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain.
|
-
- HY-U00391
-
-
- HY-144135
-
-
- HY-107901
-
|
Pparδ agonist 1
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
|
Pparδ agonist 1 is a PPAR-δ agonist, with an EC50 of 5.06 nM, used in the research of PPAR-delta related diseases, such as mitochondrial diseases, muscular diseases, vascular diseases, demyelinating diseases and metabolic diseases.
|
-
- HY-P1504A
-
-
- HY-15705
-
-
- HY-B0354AS
-
-
- HY-130118
-
|
MRGPRX1 agonist 1
|
Others
|
Neurological Disease
|
|
MRGPRX1 agonist 1 is a highly potent agonist of MRGPRX1 (Mas-related G-protein-coupled receptor X1), with an EC50 of 50 nM, and is inactive on MRGPRC11. Analgesic effect.
|
-
- HY-110018
-
-
- HY-14304
-
-
- HY-B0418A
-
-
- HY-131338
-
-
- HY-14340
-
|
WAY-181187
SAX-187
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY181187 mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
|
-
- HY-P2518A
-
-
- HY-145278
-
|
RXFP3/4 agonist 2
|
Others
|
Neurological Disease
|
|
RXFP3/4 agonist 2 is a potent, nonpeptide dual RXFP3/4 agonist (EC50=3.1 and 2.7 nM). RXFP3/4 agonist 2 also potently promotes interactions between RXFP3 and β-arrestin-2 with EC50 values in the range of 10-22 nM.
|
-
- HY-G0021
-
|
N-Desmethylclozapine
Norclozapine; Desmethylclozapine; Normethylclozapine
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
|
N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
|
-
- HY-U00205
-
-
- HY-N3216
-
-
- HY-50108
-
-
- HY-U00066
-
-
- HY-A0173
-
-
- HY-17416A
-
-
- HY-A0129
-
-
- HY-N1415
-
-
- HY-103548
-
|
GSK9027
|
Glucocorticoid Receptor
|
Endocrinology
|
|
GSK9027, as a non-steroidal glucocorticoid receptor (GR) agonist, behaves as a partial agonist on the 2×glucocorticoid response element (GRE) reporter system, and achieves intrinsic activities relative to dexamethasone.
|
-
- HY-N0808
-
-
- HY-A0008
-
-
- HY-135399S
-
|
Tauro-Obeticholic acid-d5 sodium
|
FXR
|
Inflammation/Immunology
|
|
Tauro 6-Ethlchenodeoxycholic Acid-d5 (sodium salt) is deuterium labeled Tauro-Obeticholic acid. Tauro-Obeticholic acid is an active metabolite of Obeticholic acid. Obeticholic acid is an orally bioavailable farnesoid-X receptor (FXR) agonist.
|
-
- HY-B0316
-
|
Avobenzone
|
Estrogen Receptor/ERR
Apoptosis
|
Others
|
|
Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
|
-
- HY-139018
-
-
- HY-142441
-
|
THR-β agonist 1
|
Others
|
Endocrinology
|
|
THRβ Agonist 1 is a potent and selective agonist of THRβ. Thyroid hormone receptor mediates the physiological activity of thyroid hormones which plays a key role in normal growth and development of the body and in maintaining metabolic balance. THRβ Agonist 1 has the potential for the research of thyroid hormone receptor-related diseases (extracted from patent WO2021104288A1, compound 2).
|
-
- HY-110366
-
|
WAY-181187 oxalate
SAX-187 oxalate
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-181187 (SAX-187) oxalate is a potent and selective full 5-HT6 receptor agonist with a Ki of 2.2 nM and an EC50 of 6.6 nM. WAY-181187 oxalate mediates 5-HT6 receptor-dependent signal pathways, such as cAMP, Fyn and ERK1/2 kinase, as specific agonist.
|
-
- HY-139018A
-
-
- HY-145412
-
|
GLP-1 receptor agonist 7
|
Glucagon Receptor
|
Metabolic Disease
|
|
GLP-1 receptor agonist 7 is a potent agonist of glucagon-like peptide-1 (GLP-1). GLP-1 receptor agonist 7 has the potential for the research of GLP-1-associated diseases, disorders, and conditions including diabetes mellitus (extracted from patent WO2021219019A1, compound 130b).
|
-
- HY-100113
-
-
- HY-14773S
-
-
- HY-17599
-
|
Piperazine citrate
1,4-Diazacyclohexane citrate
|
GABA Receptor
|
Infection
|
|
Piperazine (1,4-Diazacyclohexane) citrate is a gamma-aminobutyric acid (GABA) agonist. Piperazine citrate is a vital building block and is an essential core in numerous marketed drugs with diverse pharmacological activities.
|
-
- HY-P0108
-
-
- HY-B2215
-
-
- HY-14917
-
-
- HY-19998
-
-
- HY-15108
-
-
- HY-145618
-
-
- HY-16722
-
-
- HY-17633
-
-
- HY-U00230
-
-
- HY-N2309
-
-
- HY-107480
-
-
- HY-14799
-
-
- HY-107541
-
-
- HY-14864A
-
-
- HY-P0236
-
-
- HY-B0380A
-
-
- HY-B0380
-
-
- HY-14864
-
-
- HY-101585
-
-
- HY-P1013
-
-
- HY-17355BS
-
-
- HY-128922
-
-
- HY-108472
-
-
- HY-144698
-
|
mGlu4 receptor agonist 1
|
mGluR
|
Neurological Disease
|
|
mGlu4 receptor agonist 1 (compound 62) is a potent mGlu4 receptor positive allosteric modulator, with an EC50 of 308 nM. mGlu4 receptor agonist 1 shows significant anxiolytic- and antipsychotic-like effect.
|
-
- HY-P1313A
-
-
- HY-101366
-
-
- HY-142698
-
|
SGC agonist 2
|
Others
|
Cardiovascular Disease
|
|
SGC agonist 2 is a potent agonist of soluble guanylate cyclase (SGC). Soluble guanylate cyclase is a key signal transduction enzyme in the NO-sGC-cGMP signaling pathway. SGC agonist 2 has the potential for the research of cardiovascular disease (heart failure, pulmonary hypertension, angina, myocardial infarction) and fibrotic diseases (renal fibrosis, systemic sclerosis) (extracted from patent WO2021219088A1, compound 031).
|
-
- HY-144035
-
|
GLP-1R agonist 4
|
Glucagon Receptor
|
Cancer
|
|
GLP-1R agonist 4 is a potent agonist of GLP-1R. Glucagon-like peptide-1 (GLP-1) is an intestinal hypoglycemic hormone secreted by L-cells in the lower gastrointestinal tract. GLP-1R agonist 4 has the potential for the research of diabetes (extracted from patent WO2019239319A1, compound 96).
|
-
- HY-114464
-
|
11-Beta-hydroxyandrostenedione
4-Androsten-11β-ol-3,17-dione
|
Endogenous Metabolite
|
Endocrinology
|
|
11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.
|
-
- HY-131312
-
|
Mutant IDH1-IN-6
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Mutant IDH1-IN-6 is a potent, selective and orally active mutant isocitrate dehydrogenase (IDH) inhibitor with IC50s of 6.27 nM, 3.71 nM, 36.9 nM and 11.5 nM for IDH1 R132H, IDH1 R132C, IDH2 R140Q and IDH2 R172K mutant enzymes, respectively. Mutant IDH1-IN-6 is less active at inhibiting the IDH wild-type enzymes.
|
-
- HY-101033
-
|
GPR35 agonist 1
|
Others
|
Cancer
Endocrinology
|
|
GPR35 agonist 1 (compound 50) is a potent and specific G protein-coupled receptor-35 (GPR35)/CXCR8 agonist with an EC50 of 5.8 nM, displays good druggability.
|
-
- HY-N2411
-
-
- HY-19320
-
-
- HY-109527
-
-
- HY-16713A
-
-
- HY-U00216
-
-
- HY-13201
-
-
- HY-100532
-
-
- HY-103173
-
-
- HY-11076
-
-
- HY-P0080
-
-
- HY-16713
-
-
- HY-B0189
-
-
- HY-33353
-
-
- HY-111132
-
-
- HY-B0570
-
-
- HY-145589
-
-
- HY-U00226
-
-
- HY-13201A
-
-
- HY-U00293
-
-
- HY-B0475
-
-
- HY-U00038
-
-
- HY-12451
-
-
- HY-P1481
-
-
- HY-145960
-
-
- HY-117602
-
-
- HY-108258
-
|
PSN 375963
|
GPR119
|
Endocrinology
|
|
PSN 375963 is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
|
-
- HY-125556
-
|
Tetragastrin
Cholecystokinin tetrapeptide; CCK-4
|
Cholecystokinin Receptor
|
Metabolic Disease
|
|
Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin. Tetragastrin can stimulate gastric secretion. Tetragastrin is a Cholecystokinin (CCK-4) receptor agonist. Gastric mucosal protection.
|
-
- HY-108258A
-
|
PSN 375963 hydrochloride
|
GPR119
|
Endocrinology
|
|
PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
|
-
- HY-41076
-
-
- HY-143862
-
|
Pparδ agonist 7
|
PPAR
|
Metabolic Disease
|
|
Pparδ agonist 7 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 7 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2019105234A1, compound TM4).
|
-
- HY-143863
-
|
PPARδ agonist 8
|
PPAR
|
Metabolic Disease
|
|
Pparδ agonist 8 is a potent agonist of Pparδ. The peroxisome proliferator-activated receptor (PPAR) is a member of the intranuclear receptor transcription factor superfamily that plays a key role in the regulation of metabolic homeostasis, inflammation, cell growth and differentiation in vivo. Pparδ agonist 8 has the potential for the research of non-alcoholic fatty liver disease (NAFLD) (extracted from patent WO2021169769A1, compound TM2).
|
-
- HY-135572
-
-
- HY-B0735AS
-
-
- HY-P0080A
-
-
- HY-101864
-
-
- HY-13736A
-
-
- HY-P1337
-
-
- HY-14299
-
-
- HY-19661
-
-
- HY-113035
-
-
- HY-P1470
-
-
- HY-P1336
-
-
- HY-14299A
-
-
- HY-17355A
-
-
- HY-101274
-
-
- HY-B0188
-
-
- HY-100273
-
-
- HY-B0189A
-
-
- HY-P1532
-
-
- HY-W015326
-
-
- HY-111068
-
-
- HY-17622
-
-
- HY-P1211A
-
-
- HY-21098A
-
-
- HY-12664
-
-
- HY-101973
-
-
- HY-B0374A
-
-
- HY-U00233
-
-
- HY-144134
-
-
- HY-14958A
-
-
- HY-14958
-
-
- HY-138953
-
|
Epiboxidine
|
nAChR
|
Neurological Disease
|
|
Epiboxidine is a potent and selective neural nAChR agonist with Kis of 0.46 nM and 1.2 nM for rat and human α4β2 nAChRs, respectively. Epiboxidine is a methylisoxazole analog of the alkaloid Epibatidine, and is also an analog of another nAChR agonist, ABT 418.
|
-
- HY-P1123
-
|
MEDICA16
|
ATP Citrate Lyase
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
MEDICA16, an ATP-citrate lyase inhibitor, significantly reduces intracellular TG content in gastrocnemius muscle, and this reduction is accompanied by an increase in insulin sensitivity. MEDICA16 is a selective agonist for GPR40 as well as selective partial agonists for GPR120.
|
-
- HY-19434A
-
|
cis-ACPD
|
iGluR
mGluR
|
Neurological Disease
|
|
cis-ACPD is a potent agonist of NMDA receptor, with an IC50 of 3.3 μM. cis-ACPD is also a selective agonist of group II mGluR, with EC50s of 13 μM and 50 μM for mGluR2 and mGluR4, respectively.
|
-
- HY-P1198
-
-
- HY-112606
-
|
ML-290
|
Others
|
Others
|
|
ML-290 is a first-in-class and potent relaxin/insulin-like family peptide receptor (RXFP1) agonist and activator of anti-fibrotic genes, with an EC50 of 94 nM. ML290 is a biased allosteric agonist at the relaxin receptor RXFP1.
|
-
- HY-107654S
-
|
Muscarine-d9 iodide
(+)-Muscarine-d9 iodide
|
mAChR
|
Neurological Disease
|
|
Muscarine-d9 iodide ((+)-Muscarine-d9 iodide) is the deuterium labeled Muscarine iodide. Muscarine ((+)-Muscarine) iodide is a toxin that can stimulate the parasympathetic nervous system. Muscarine iodide is a prototype muscarinic acetylcholine receptor agonist.
|
-
- HY-143864
-
|
S1PR1 agonist 1
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1PR1 agonist 1 is a potent agonist of S1PR1. Sphingosine-1-phosphate (S1P) is a cell membrane-derived lysophospholipid signalling molecule that exerts its physiological functions mainly by stimulating some members of the G protein-coupled receptor family. S1PR1 agonist 1 has the potential for the research of autoimmune diseases (extracted from patent WO2021175223A1, compound 22).
|
-
- HY-143865
-
|
S1PR1 agonist 2
|
LPL Receptor
|
Inflammation/Immunology
|
|
S1PR1 agonist 2 is a potent agonist of S1PR1. Sphingosine-1-phosphate (S1P) is a cell membrane-derived lysophospholipid signalling molecule that exerts its physiological functions mainly by stimulating some members of the G protein-coupled receptor family. S1PR1 agonist 2 has the potential for the research of autoimmune diseases (extracted from patent WO2021175225A1, compound 1).
|
-
- HY-N8200
-
-
- HY-P1192
-
-
- HY-108530
-
|
MM11253
|
RAR/RXR
|
Cancer
|
|
MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists.
|
-
- HY-128573
-
-
- HY-115766
-
|
Anabaseine
|
nAChR
|
Neurological Disease
|
|
Anabaseine is a non-selective nicotinic agonist. Anabaseine stimulates all AChRs, preferentially stimulates skeletal muscle and brain α7 subtypes. Anabaseine is also a weak partial agonist at α4β2 nAChRs.
|
-
- HY-P3137
-
|
TRV056
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV056 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV056 is efficacious in stimulating cellular Gq-mediated signaling. TRV056 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-P3136
-
|
TRV055
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
TRV055 is a Gq-biased ligand of the angiotensin II receptor type 1 (AT1R). TRV055 is efficacious in stimulating cellular Gq-mediated signaling. TRV055 can be used to develop the Gq-biased AT1R agonists.
|
-
- HY-145351
-
-
- HY-114146
-
-
- HY-100124
-
-
- HY-P1087
-
-
- HY-B0452
-
-
- HY-101038A
-
-
- HY-145369
-
-
- HY-100428
-
-
- HY-109111
-
-
- HY-U00400
-
-
- HY-11077
-
-
- HY-113035A
-
-
- HY-106181
-
-
- HY-116521
-
-
- HY-14734B
-
-
- HY-P1578
-
-
- HY-108449
-
-
- HY-100327
-
-
- HY-79593
-
-
- HY-B0409A
-
-
- HY-101582
-
-
- HY-19250
-
-
- HY-103704
-
-
- HY-107216
-
-
- HY-N2371
-
-
- HY-B0648
-
-
- HY-12499
-
-
- HY-19468
-
-
- HY-P1337A
-
-
- HY-P1013A
-
-
- HY-100775
-
-
- HY-100775A
-
-
- HY-P1405
-
-
- HY-B0418AS1
-
-
- HY-G0021S
-
|
N-Desmethylclozapine-d8
Norclozapine-d8; Desmethylclozapine-d8; Normethylclozapine-d8
|
mAChR
Opioid Receptor
Drug Metabolite
Virus Protease
|
Infection
|
|
N-Desmethylclozapine-d8 (Norclozapine-d8) is the deuterium labeled N-Desmethylclozapine. N-Desmethylclozapine is a major active metabolite of the atypical antipsychotic drug Clozapine. N-Desmethylclozapine is a potent, allosteric and partial M1 receptors agonist (EC50=115 nM) and is able to potentiate hippocampal N-methyl-d-aspartate (NMDA) receptor currents through M1 receptor activation. N-Desmethylclozapine is also a δ-opioid agonist.
|
-
- HY-N0166
-
-
- HY-P1198A
-
-
- HY-14304A
-
|
Zinterol hydrochloride
MJ 9184 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Zinterol hydrochloride (MJ 9184 hydrochloride) is a potent and selective β2-adrenoceptor agonist. Zinterol hydrochloride increases ICa in a concentration-dependent manner with an EC50 of 2.2 nM. Zinterol hydrochloride induces ventricular arrhythmias in conscious heart failure rabbits.
|
-
- HY-143878
-
|
MRGPRX1 agonist 2
|
Others
|
Neurological Disease
|
|
MRGPRX1 agonist 2 (compound 1a) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.48 μM. MRGPRX1 agonist 2 can be used for researching neuropathic pain.
|
-
- HY-P0078
-
|
TRAP-6
PAR-1 agonist peptide; Thrombin Receptor Activator Peptide 6
|
Protease-Activated Receptor (PAR)
|
Inflammation/Immunology
|
|
TRAP-6 (PAR-1 agonist peptide), a peptide fragment, is a selective protease activating receptor 1 (PAR1) agonist. TRAP-6 activates human platelets via the thrombin receptor. TRAP-6 shows no activity at PAR4.
|
-
- HY-112486
-
|
TA-316
Megakaryocytes/platelets inducing agent
|
Others
|
Cardiovascular Disease
|
|
TA-3166 (Megakaryocytes/platelets inducing agent) is a novel chemically synthesized c-MPL agonist (CMA) and thrombopoietin (TPO) receptor agonist. TA-316 enhances ex vivo platelet generation from human-induced pluripotent stem (iPS) cells.
|
-
- HY-14773
-
-
- HY-103273
-
|
Muristerone A
|
Others
|
Others
|
|
Muristerone A is a phytoecdysteroid analog of ecdysone and a potent agonist of ecdysteroid receptor with a Kd of 1 nM.
|
-
- HY-100676
-
-
- HY-W014666
-
-
- HY-109197
-
-
- HY-101639A
-
-
- HY-102075A
-
-
- HY-100336
-
-
- HY-10475
-
|
AM580
CD336; NSC608001; Ro 40-6055
|
RAR/RXR
Autophagy
|
Cancer
|
|
AM580 is a selective RARα agonist with IC50 and EC50 of 8 nM and 0.36 nM, respectively.
|
-
- HY-101384A
-
-
- HY-P1331
-
-
- HY-109032
-
-
- HY-100140
-
-
- HY-41700
-
-
- HY-107319
-
-
- HY-12749
-
-
- HY-B1403
-
-
- HY-101299
-
-
- HY-16972
-
|
SR9243
|
LXR
|
Cancer
|
|
SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
|
-
- HY-N6629
-
-
- HY-104026
-
-
- HY-100291
-
-
- HY-P1578A
-
-
- HY-101987
-
-
- HY-13101
-
-
- HY-P0226
-
-
- HY-19883
-
-
- HY-107538
-
-
- HY-N0178
-
-
- HY-A0040
-
-
- HY-P1515
-
-
- HY-115777
-
-
- HY-120973A
-
-
- HY-101639
-
-
- HY-13788B
-
-
- HY-10002
-
-
- HY-B0436
-
-
- HY-14229
-
-
- HY-143879
-
|
MRGPRX1 agonist 3
|
Others
|
Neurological Disease
|
|
MRGPRX1 agonist 3 (compound 1f) is a potent Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.22 μM. MRGPRX1 agonist 3 can be used for researching neuropathic pain.
|
-
- HY-120879
-
|
PF2562
|
Dopamine Receptor
|
Neurological Disease
|
|
PF2562 (Example 6), a dopamine D1 ligand, ascts as a dopamine D1 agonist or partial agonist. PF2562 binds to human D1 receptor with a Ki of 113 nM. PF2562 exhibits activity against human D1 cAMP with an EC50 of 568 nM in HTRF assay.
|
-
- HY-N0808S
-
|
Camphor-d6
(±)-Camphor-d6
|
TRP Channel
Influenza Virus
|
Cancer
Infection
Inflammation/Immunology
|
|
Camphor-d6 ((±)-Camphor-d6) is the deuterium labeled Camphor. Camphor ((±)-Camphor) is a topical anti-infective and anti-pruritic and internally as a stimulant and carminative. However, Camphor is poisonous when ingested. Antiviral, antitussive, and anticancer activities. Camphor is a TRPV3 agonist.
|
-
- HY-103229
-
|
Cl-HIBO
|
iGluR
|
Neurological Disease
|
|
Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties.
|
-
- HY-112289
-
|
IDH889
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
IDH889 is an orally available, brain penetrant, allosteric and mutant specific inhibitor of isocitrate dehydrogenase 1 (IDH1). IDH889 has potent selectivity for IDH1 R132* mutations, with IC50s of 0.02 μM, 0.072 μM and 1.38 μM for IDH1 R132H, IDH1 R132C and IDH1 wt, respectively. IDH889 shows potent cellular inhibition of R-2-hydroxyglutarate (2-HG) production with an IC50 of 0.014 μM.
|
-
- HY-10233
-
|
Gaboxadol hydrochloride
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 µM, a full agonist efficacy at α5 subunit (ED50=28-129 µM) and a superagonist efficacy at α4β3δ (ED50=6 µM). Gaboxadol hydrochloride is a non-opioid agent.
|
-
- HY-136258
-
|
nAChR agonist CMPI hydrochloride
|
nAChR
|
Neurological Disease
|
|
nAChR agonist CMPI hydrochloride is a potent and selective positive allosteric modulator (PAM) of nAChR containing a α4:α4 subunit interface. nAChR agonist CMPI hydrochloride enhances the response of (α4)3(β2)2 nAChR to ACh (10 µM) with an EC50 of 0.26 µM. nAChR agonist CMPI hydrochloride has potential for the research of nicotine dependence and many neuropsychiatric conditions associated with decreased brain cholinergic activity.
|
-
- HY-133011
-
|
nAChR agonist 1
|
nAChR
|
Neurological Disease
|
|
nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor (α7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
|
-
- HY-B0188A
-
-
- HY-100140A
-
-
- HY-14785
-
-
- HY-14785A
-
-
- HY-P0079
-
-
- HY-114116
-
-
- HY-109181
-
-
- HY-10838
-
-
- HY-120687
-
-
- HY-P0297
-
-
- HY-15306
-
-
- HY-P1477
-
-
- HY-12749A
-
-
- HY-B1540S
-
-
- HY-16465
-
-
- HY-103431
-
-
- HY-18939
-
-
- HY-14648A
-
-
- HY-107418
-
-
- HY-P1515A
-
-
- HY-P1478
-
-
- HY-10922A
-
-
- HY-P2321
-
-
- HY-101271
-
-
- HY-P0088
-
-
- HY-132814
-
-
- HY-100166
-
-
- HY-10480
-
-
- HY-111454
-
-
- HY-15677
-
-
- HY-13421
-
-
- HY-16086
-
-
- HY-P0226A
-
-
- HY-15388
-
-
- HY-B0374
-
-
- HY-B0769
-
-
- HY-10922
-
-
- HY-B0316S
-
|
Avobenzone-13C,d3
|
Estrogen Receptor/ERR
Apoptosis
|
Others
|
|
Avobenzone-13C,d3 is the 13C- and deuterium labeled. Avobenzone, a dibenzoylmethane compound, is one of the most widely used filters in sunscreens for skin photoprotection in the UVA band. Avobenzone is an endocrine disruptor that directly binds to estrogen receptor β and acts as an estrogen agonist.
|
-
- HY-115400
-
|
1V209
TLR7 agonist T7
|
Toll-like Receptor (TLR)
|
Cancer
|
|
1V209 (TLR7 agonist T7) is a Toll-like receptor 7 (TLR7) agonist and has anti-tumor effects. 1V209 can be conjugated with various polysaccharides to improve its water solubility, and enhance its efficacy, and maintain low toxicity.
|
-
- HY-101630
-
|
Deramciclane
EGIS-3886
|
5-HT Receptor
|
Neurological Disease
|
|
Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
|
-
- HY-107601
-
|
UBP316
ACET
|
iGluR
|
Neurological Disease
|
|
UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist.
|
-
- HY-P1309
-
-
- HY-129656
-
-
- HY-114978
-
|
VU0424465
|
mGluR
PERK
|
Neurological Disease
|
|
VU0424465 is a potent and partial PAM (positive allosteric modulator)-agonist for mGlu5 mediated iCa 2+ mobilization. VU0424465 exhibits high affinity at MPEP allosteric binding site, with a Ki value of 11.8 nM. VU0424465 is also a agonist for pERK1/2 in cortical neurons.
|
-
- HY-103005S
-
-
- HY-P1145
-
-
- HY-70037
-
-
- HY-139904
-
-
- HY-107542
-
-
- HY-105074
-
|
Farglitazar
GI262570; GI262570X
|
PPAR
|
Metabolic Disease
|
|
Farglitazar is a PPARγ agonist that has significant therapeutic benefits such as glycemic control in type 2 diabetic patients.
|
-
- HY-112627
-
-
- HY-111786
-
-
- HY-102016
-
-
- HY-101540
-
-
- HY-B0716
-
-
- HY-14870
-
-
- HY-108003
-
-
- HY-76772A
-
-
- HY-15885
-
-
- HY-B0206
-
-
- HY-14734
-
-
- HY-107395
-
-
- HY-15291
-
-
- HY-19919
-
|
BMS-779788
EXEL04286652; XL-652; BMS-788
|
LXR
|
Metabolic Disease
|
|
BMS-779788 is a LXR partial agonist with IC50 values of 68 nM for LXRα and 14 nM for LXRβ.
|
-
- HY-103098
-
-
- HY-15566
-
|
APD597
JNJ-38431055
|
GPR119
|
Metabolic Disease
|
|
APD597 is a GPR119 agonist intended for the treatment of type 2 diabetes, with EC50 of 46 nM for hGPR119.
|
-
- HY-108414
-
-
- HY-18723
-
-
- HY-14734A
-
-
- HY-19942A
-
-
- HY-101822
-
-
- HY-19308
-
-
- HY-U00215
-
-
- HY-16737
-
-
- HY-19434
-
|
trans-ACPD
Trans-(±)-ACP
|
mGluR
|
Metabolic Disease
|
|
trans-ACPD, a metabotropic receptor agonist, produces calcium mobilization and an inward current in cultured cerebellar Purkinje neurons.
|
-
- HY-135905
-
-
- HY-P1334
-
-
- HY-17551
-
-
- HY-131103
-
-
- HY-P2321A
-
-
- HY-103107
-
-
- HY-14735
-
-
- HY-76772B
-
-
- HY-P1477A
-
-
- HY-16998
-
|
SR2211
|
ROR
|
Inflammation/Immunology
|
|
SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
|
-
- HY-30006
-
-
- HY-147622
-
-
- HY-19511
-
|
GSK2018682
|
LPL Receptor
|
Inflammation/Immunology
|
|
GSK2018682 is an agonist for S1P1 and S1P5 receptor with pEC50s of 7.7 and 7.2, respectively, and has no agonist activity towards human S1P2, S1P3, or S1P4. GSK2018682 is used in the research of multiple sclerosis.
|
-
- HY-114464S1
-
|
11-Beta-hydroxyandrostenedione-d7
4-Androsten-11β-ol-3,17-dione-d7
|
Endogenous Metabolite
|
Others
|
|
11-Beta-hydroxyandrostenedione-d7 is the deuterium labeled 11-Beta-hydroxyandrostenedione. 11-Beta-hydroxyandrostenedione (4-Androsten-11β-ol-3,17-dione) is a steroid mainly found in the the adrenal origin (11β-hydroxylase is present in adrenal tissue, but absent in ovarian tissue). 11-Beta-hydroxyandrostenedione is a 11β-hydroxysteroid dehydrogenase (11βHSD) isozymes inhibitor. As 4-androstenedione increases, measuring plasma 11-Beta-hydroxyandrostenedione can distinguish the adrenal or ovarian origin of hyperandrogenism.
|
-
- HY-121744
-
|
PS10
|
PDHK
|
Inflammation/Immunology
|
|
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
|
-
- HY-15430A
-
-
- HY-106094
-
-
- HY-B0084
-
-
- HY-136586
-
-
- HY-P1533
-
-
- HY-B1583
-
-
- HY-17457
-
-
- HY-P1031
-
-
- HY-B0735
-
-
- HY-112322
-
-
- HY-108557
-
-
- HY-100728
-
-
- HY-19945
-
|
DAA-1106
|
GABA Receptor
|
Neurological Disease
|
|
DAA1106 is a potent and selective ligand for peripheral benzodiazepine receptor (PBR), as a potent and selective agonist at the peripheral benzodiazepine receptor.
|
-
- HY-12111
-
-
- HY-B0566
-
-
- HY-100673
-
-
- HY-P1145A
-
-
- HY-101331
-
-
- HY-114025
-
-
- HY-70037A
-
-
- HY-17355B
-
-
- HY-U00206
-
-
- HY-111271
-
-
- HY-15430
-
-
- HY-12584
-
-
- HY-108533
-
|
CD2314
|
RAR/RXR
|
Cancer
|
|
CD2314 is a potent and selective RARβ receptor agonist with a Kd of 195 nM in S91 melanoma cells.
|
-
- HY-B0735A
-
-
- HY-131286A
-
-
- HY-B0726
-
-
- HY-135259
-
-
- HY-50935
-
-
- HY-103314
-
-
- HY-108560
-
|
(+)-Fluprostenol
|
Others
|
Others
|
|
(+)-Fluprostenol is a potent agonist of PTGER2. (+)-Fluprostenol decreases the expression of Oviductal glycoprotein 1 (OVGP1).
|
-
- HY-130115
-
|
IACS-8803
|
STING
|
Cancer
|
|
IACS-8803 is a highly potent cyclic dinucleotide STING agonist with robust systemic antitumor efficacy.
|
-
- HY-100347A
-
-
- HY-B1832
-
-
- HY-P1339
-
-
- HY-101273
-
-
- HY-121415
-
-
- HY-P1545
-
-
- HY-111498
-
-
- HY-16162
-
|
D-3263
|
TRP Channel
|
Cancer
|
|
D-3263 is an agonist of transient receptor potential melastatin member 8 (TRPM8) with potential antineoplastic activity.
|
-
- HY-100347
-
-
- HY-B1752A
-
-
- HY-P1577
-
-
- HY-W015878
-
-
- HY-B0468
-
-
- HY-114610
-
-
- HY-136429
-
|
Ethylhydrocupreine
Optochin
|
Bacterial
Parasite
|
Infection
|
|
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
|
-
- HY-133552
-
|
RORγt Inverse agonist 10
|
ROR
|
Inflammation/Immunology
|
|
RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
|
-
- HY-136429A
-
|
Ethylhydrocupreine hydrochloride
Optochin hydrochloride
|
Bacterial
Parasite
|
Infection
|
|
Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
|
-
- HY-N0175
-
|
Cytisinicline
Cytisine; Sophorine; Baptitoxine
|
nAChR
|
Metabolic Disease
|
|
Cytisinicline (Cytisine) is an alkaloid that occurs naturally in several plant genera, such as Laburnum and Cytisus. Cytisinicline (Cytisine) is a partial agonist of α4β2 nAChRs, and partial to full agonist at β4 containing receptors and α7 receptors. Has been used medically to help with smoking cessation.
|
-
- HY-14546
-
-
- HY-14261
-
-
- HY-130116
-
|
IACS-8779
|
STING
|
Cancer
|
|
IACS-8779 is a highly potent stimulator of interferon genes (STING) agonist with robust systemic antitumor efficacy.
|
-
- HY-103225
-
-
- HY-17034B
-
-
- HY-W008613
-
-
- HY-114165
-
-
- HY-P0059
-
|
Teriparatide
Human parathyroid hormone-(1-34); hPTH (1-34)
|
Others
|
Cancer
|
|
Teriparatide (Human parathyroid hormone-(1-34)) is a PHT agonist, with an IC50 of 2 nM in HEK293 cells.
|
-
- HY-100328
-
-
- HY-18100A
-
-
- HY-B1006
-
-
- HY-101950
-
-
- HY-B0194A
-
-
- HY-101420
-
-
- HY-103187
-
-
- HY-17030
-
-
- HY-12199
-
-
- HY-B0197A
-
-
- HY-P1021
-
-
- HY-W106234
-
-
- HY-P1339A
-
-
- HY-12520A
-
-
- HY-16162A
-
-
- HY-B0577
-
-
- HY-109096
-
-
- HY-12199B
-
-
- HY-B0194
-
-
- HY-101386
-
-
- HY-15601
-
-
- HY-P1467
-
-
- HY-B0823S
-
-
- HY-15778
-
-
- HY-P1545A
-
-
- HY-P0098
-
-
- HY-B0197
-
-
- HY-112152
-
-
- HY-101609
-
-
- HY-14149
-
-
- HY-16465A
-
-
- HY-B0197AS
-
-
- HY-B0354A
-
-
- HY-50911
-
-
- HY-145237
-
|
BM213
|
Others
|
Cancer
|
|
BM213, a potent and selective agonist for C5aR1, shows antitumor activity in a mouse model of mammary carcinoma.
|
-
- HY-15306A
-
-
- HY-13788C
-
-
- HY-133528
-
-
- HY-19774
-
-
- HY-B0189S1
-
-
- HY-146066
-
|
α7 nAchR-JAK2-STAT3 agonist 1
|
nAChR
JAK
STAT
NO Synthase
|
Inflammation/Immunology
|
|
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis.
|
-
- HY-101300
-
-
- HY-P1309A
-
-
- HY-A0007
-
-
- HY-131961
-
|
Triciferol
|
VD/VDR
HDAC
|
Cancer
|
|
Triciferol functions as a multiple ligand with combined VDR agonist and HDAC antagonist activities. Triciferol binds directly to the VDR (IC50=87 nM), and functions as an agonist with 1,25D-like potency on several 1,25D target genes. Triciferol induces marked tubulin hyperacetylation, and augments histone acetylation. Antiproliferative and cytotoxic activities.
|
-
- HY-P1467A
-
-
- HY-107675
-
-
- HY-15401
-
-
- HY-16728
-
|
Rapastinel
GLYX-13
|
iGluR
|
Neurological Disease
|
|
Rapastinel (GLYX-13) is an N-methyl-D-aspartate receptor (NMDAR) modulator that has characteristics of a glycine site partial agonist.
|
-
- HY-P1164
-
-
- HY-B0459
-
-
- HY-100907
-
|
(±)-Acetylcarnitine chloride
Acetyl dl-carnitine chloride
|
Others
|
Neurological Disease
|
|
(±)-Acetylcarnitine chloride (Acetyl dl-carnitine chloride) is a weak cholinergic agonist with cholinergic properties. (±)-Acetylcarnitine chloride is an important intermediate in lipid metabolism.
|
-
- HY-101586
-
-
- HY-14351
-
-
- HY-12199A
-
-
- HY-16916
-
-
- HY-101649
-
-
- HY-103498
-
-
- HY-P1588
-
-
- HY-13510
-
-
- HY-N0382
-
|
Galangin
Norizalpinin; 3,5,7-Trihydroxyflavone
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
|
-
- HY-13788
-
-
- HY-13788A
-
-
- HY-B1666B
-
-
- HY-P1261
-
-
- HY-124073
-
-
- HY-103410
-
-
- HY-137452
-
-
- HY-145620
-
-
- HY-P0244
-
-
- HY-100856
-
-
- HY-B0383A
-
-
- HY-14953
-
|
Imepitoin
AWD 131-138
|
GABA Receptor
|
Neurological Disease
|
|
Imepitoin (AWD 131-138) is a new low-affinity partial benzodiazepine receptor agonist with potent anticonvulsant and anxiolytic properties in rodent models.
|
-
- HY-14652
-
-
- HY-101419
-
-
- HY-14426
-
-
- HY-101787
-
-
- HY-U00014
-
|
AVE-8134
|
PPAR
|
Metabolic Disease
|
|
AVE-8134 is a potent PPARα agonist, with EC50 values of 100 and 3000 nM for human and rodent PPARα receptor, respectively.
|
-
- HY-14831
-
|
Arhalofenate
MBX 102; JNJ 39659100
|
PPAR
|
Metabolic Disease
|
|
Arhalofenate (MBX 102) is a selective partial agonist of peroxisome proliferator-activated receptor (PPAR)-γ, used for the treatment of type 2 diabetes.
|
-
- HY-19317
-
-
- HY-15243
-
-
- HY-107555
-
-
- HY-P1262
-
-
- HY-137440
-
-
- HY-N2311
-
|
Ibotenic acid
(RS)-Ibotenic acid; DL-Ibotenic acid
|
iGluR
|
Neurological Disease
|
|
Ibotenic acid has agonist activity at both the N-methyl-D-aspartate (NMDA) and trans-ACPD or metabolotropic quisqualate (Qm) receptor sites.
|
-
- HY-19583
-
-
- HY-B0802
-
-
- HY-14562
-
|
TBPB
|
mAChR
|
Neurological Disease
|
|
TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.
|
-
- HY-14413
-
|
SR3335
ML 176
|
ROR
|
Metabolic Disease
|
|
SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM.
|
-
- HY-125703
-
|
Ferutinin
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Infection
Endocrinology
Inflammation/Immunology
|
|
Ferutinin, a natural terpenoid compound, is an estrogen receptor ERα agonist and estrogen ERβ-receptor agonist/antagonist with IC50s of 33.1 nM and 180.5 nM, respectively. Ferutinin acts as an electrogenic Ca 2+-ionophore that increases calcium permeability of lipid bilayer membranes, mitochondria. Ferutinin possesses estrogenic, antitumor, antibacterial and antiinflammatory activities.
|
-
- HY-14441
-
|
ML 10302
|
5-HT Receptor
|
Neurological Disease
|
|
ML 10302 is a potent agonist 5-HT4 receptor with Ki of 1.07 nM. 5-Hydroxytryptamine (5-HT4) receptor agonists stimulate gut motility through cholinergic pathways. ML10302 induces significant prokinesia both in the small bowel and colon through activation of cholinergic pathways. ML 10302 also has the potential for the research of neurology diseases.
|
-
- HY-106100
-
|
Roxindole
EMD 49980
|
Dopamine Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Roxindole (EMD 49980), an indot-alkyl-pipenidine, is a potent agonist at dopamine autoreceptors, with an affinity for the D2-like subtype in the low nanomolar range. Roxindole can be used for the research of positive and negative schizophrenic symptoms. Roxindole is a 5-HT1A agonist and 5-HT uptake inhibitor. Antipsychotic and antidepressant activities.
|
-
- HY-126047B
-
|
(R)-(+)-Anatabine
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-117829
-
|
UNC9994
|
Dopamine Receptor
5-HT Receptor
Histamine Receptor
|
Neurological Disease
|
|
UNC9994, an analog of Aripiprazole, is a functionally selective β-arrestin-biased dopamine D2 receptor (D2R) agonist with EC50 <10 nM for β-arrestin-2 recruitment to D2 receptors. UNC9994 is simultaneously partial agonists of β-arrestin-2 translocation and antagonists of Gi-regulated cAMP production. Antipsychotic Activity.
|
-
- HY-111406
-
|
Omidenepag isopropyl
DE-117
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Omidenepag isopropyl is a selective EP2 receptor agonist. Omidenepag isopropyl is converted to the active product Omidenepag during corneal penetration, and Omidenepag is a highly selective EP2 receptor agonist. Omidenepag isopropyl shows only weak affinity for EP1, EP2, and FP receptors. Omidenepag isopropyl is under development for the treatment of glaucoma as an intraocular pressure (IOP)-lowering drug.
|
-
- HY-A0182A
-
-
- HY-B0545
-
-
- HY-100171
-
-
- HY-N0783
-
-
- HY-100443B
-
-
- HY-19365
-
-
- HY-P1164A
-
-
- HY-P0177
-
-
- HY-P0244A
-
-
- HY-17501
-
|
Bambuterol
(±)-Bambuterol; KWD-2183
|
Adrenergic Receptor
|
Endocrinology
|
|
Bambuterol ((±)-Bambuterol; KWD-2183) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
|
-
- HY-P1127
-
-
- HY-10629
-
-
- HY-17584
-
|
Linaclotide
|
Guanylate Cyclase
|
Others
|
|
Linaclotide is a potent and selective guanylate cyclase C agonist; developed for the treatment of constipation-predominant irritable bowel syndrome (IBS-C) and chronic constipation.
|
-
- HY-110164
-
-
- HY-P1012
-
-
- HY-128604
-
|
XY101
|
ROR
|
Cancer
|
|
XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM.
|
-
- HY-P1262A
-
-
- HY-111200
-
-
- HY-108526
-
-
- HY-P1261A
-
-
- HY-B0380S
-
-
- HY-17501A
-
|
Bambuterol hydrochloride
(±)-Bambuterol hydrochloride; KWD-2183 hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
|
Bambuterol hydrochloride ((±)-Bambuterol hydrochloride; KWD-2183 hydrochloride) is a long acting beta-adrenoceptor agonist (LABA) used in the treatment of asthma; it also is a prodrug of terbutaline.
|
-
- HY-109104
-
-
- HY-16685
-
-
- HY-15536A
-
-
- HY-B0189S
-
-
- HY-101357A
-
-
- HY-101777
-
-
- HY-P0210
-
-
- HY-10487
-
-
- HY-13338S
-
-
- HY-12216
-
-
- HY-W017500
-
-
- HY-U00371
-
-
- HY-101239
-
-
- HY-A0182
-
-
- HY-N5016
-
-
- HY-P0090
-
|
Calcitonin (salmon)
Salmon calcitonin
|
CGRP Receptor
|
Cancer
|
|
Calcitonin salmon, a calcium regulating hormone, is a dual-action amylin and calcitonin receptor agonist, could stimulate bone formation and inhibit bone resorption.
|
-
- HY-B0659
-
-
- HY-19863
-
-
- HY-103307
-
-
- HY-101192
-
-
- HY-B0383
-
-
- HY-P0014
-
-
- HY-N1415S
-
-
- HY-18687
-
-
- HY-75502
-
-
- 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-N0322
-
|
Cholesterol
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Metabolic Disease
|
|
Cholesterol is the major sterol in mammals and is makes up 20-25% of structural component of the plasma membrane. Plasma membranes are highly permeable to water but relatively impermeable to ions and protons. Cholesterol plays an important role in determining the fluidity and permeability characteristics of the membrane as well as the function of both the transporters and signaling proteins. Cholesterol is also an endogenous estrogen-related receptor α (ERRα) agonist.
|
-
- HY-111269
-
-
- HY-P1021A
-
-
- HY-111098
-
-
- HY-15848
-
-
- HY-13773
-
-
- HY-101205
-
-
- HY-P0298
-
-
- HY-13443
-
-
- HY-B1893
-
-
- HY-126653
-
-
- 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-17030S
-
-
- HY-P1012A
-
-
- HY-14601
-
-
- HY-19134
-
-
- HY-B0606
-
-
- HY-14557
-
-
- HY-B0418AS
-
-
- HY-111999A
-
|
E7766 diammonium salt
|
STING
|
Cancer
|
|
E7766 diammonium salt is a macrocycle-bridged STING agonist with a Kd of 40 nM. E7766 diammonium salt shows potent pan-genotypic and antitumor activities.
|
-
- HY-119384
-
-
- HY-19946
-
-
- HY-P3282
-
|
MM 419447
|
Guanylate Cyclase
|
Metabolic Disease
|
|
MM 419447, a linaclotide metabolite, is a guanylate cyclase-C agonist. MM 419447 has the potential for the research of the irritable bowel syndrome with constipation (IBS-C).
|
-
- HY-106568
-
-
- HY-P0210B
-
-
- HY-109044
-
-
