Search Result
Results for "Alpha Granule Inhibitors" in MCE Product Catalog:
9864
Inhibitors & Agonists
22
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-U00439
-
-
- HY-N1163
-
-
- HY-N2413
-
|
Gomisin D
|
Others
|
Metabolic Disease
|
|
Gomisin D, a lignan compound isolated from Fructus Schisandra, is a potential antidiabetic and anti-Alzheimer’s agent. Gomisin D inhibits UDP-Glucuronosyltransferases activity and scavenges ABTS(+) radicals. Gomisin D is used as a quality marker of Shengmai San and shenqi Jiangtang Granule.
|
-
- HY-113097
-
-
- HY-123076
-
|
Pifithrin-α, p-Nitro, Cyclic
PFN-α
|
MDM-2/p53
|
Neurological Disease
|
|
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue.
|
-
- HY-P0261
-
-
- HY-N0492
-
-
- HY-N3002
-
|
α-Arbutin
4-Hydroxyphenyl α-D-glucopyranoside
|
Tyrosinase
|
Metabolic Disease
|
|
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor.
|
-
- HY-N0255
-
|
alpha-Hederin
α-Hederin
|
Apoptosis
|
Others
|
|
alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway.
|
-
- HY-15536A
-
-
- HY-12799
-
-
- HY-129389
-
|
Benzyl-α-GalNAc
|
Others
|
Cancer
|
|
Benzyl-α-GalNAc is a potent O-glycosylation inhibitor and is used to reduce mucin on cell surfaces. Benzyl-α-GalNAc inhibits the synthesis of mucin O-glycosylation of cellular models of human pancreatic cancer.
|
-
- HY-19949
-
-
- HY-U00376
-
-
- HY-134471
-
|
TNF-α-IN-2
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis.
|
-
- HY-N6968
-
|
α-Humulene
Humulene; α-Caryophyllene
|
NO Synthase
COX
|
Inflammation/Immunology
|
|
α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 µg/mL). α-Humulene inhibits COX-2 and iNOS expression.
|
-
- 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-N0328
-
-
- HY-112275
-
-
- HY-18370
-
-
- HY-N2514
-
|
α-Lactose
α-D-Lactose
|
Others
|
Others
|
|
α-Lactose (α-D-Lactose) is the major sugar present in milk. Lactose exists in the form of two anomers, α and β. The α form normally crystallizes as a monohydrate.
|
-
- HY-129113
-
|
α-Chaconine
|
COX
|
Inflammation/Immunology
|
|
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
|
-
- HY-N1467
-
|
(-)-α-Terpineol
(S)-α-Terpineol
|
Others
|
Others
|
|
(-)-α-Terpineol ((S)-α-Terpineol), a monoterpene compound, is one of important aroma compounds in white wines.
|
-
- HY-18874
-
-
- HY-136735
-
|
IRE1α kinase-IN-1
|
IRE1
|
Cancer
Neurological Disease
|
|
IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM).
|
-
- HY-N0683A
-
-
- HY-18509
-
|
IRE1α kinase-IN-2
|
IRE1
|
Cancer
|
|
IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines.
|
-
- HY-N0683
-
-
- HY-107641
-
|
α-Cyano-4-hydroxycinnamic acid
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications.
|
-
- HY-P1365
-
|
α-Conotoxin MII
α-CTxMII
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-N0611
-
|
alpha-Boswellic acid
α-Boswellic acid
|
Others
|
Inflammation/Immunology
|
|
alpha-Boswellic acid (α-Boswellic acid) is a pentacyclic triterpene compound from extracts of Frankincense, has anticonvulsant and anti-cancer properties. alpha-Boswellic acid prevents and decreases the progression of Alzheimer’s hallmarks in vivo and can be used for Alzheimer’s disease research.
|
-
- HY-W020044
-
|
DL-alpha-Tocopherol
DL-α-Tocopherol
|
Ferroptosis
|
Others
|
|
DL-alpha-Tocopherol is a synthetic vitamin E, with antioxidation effect. DL-alpha-Tocopherol protects human skin fibroblasts against the cytotoxic effect of UVB.
|
-
- HY-P1264
-
|
α-Bungarotoxin
|
nAChR
|
Neurological Disease
|
|
α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM.
|
-
- HY-12836A
-
-
- HY-12836
-
-
- HY-W089785
-
|
Methyl α-D-galactopyranoside monohydrate
|
Others
|
Others
|
|
Methyl α-D-galactopyranoside monohydrate is an alpha-D-galactoside having a methyl substituent at the anomeric position. Methyl α-D-galactopyranoside inhibits debaryomyces hansenii UFV-1 extracellular and intracellular α-galactosidases with Ki values of 0.82 and 1.12 mM, respectively.
|
-
- HY-N6962
-
|
α-Spinasterol
|
TRP Channel
COX
|
Infection
Neurological Disease
|
|
α-Spinasterol, isolated from Spinacia oleracea, has antibacterial activity. α-Spinasterol is a transient receptor potential vanilloid 1 (TRPV1) antagonist, has anti-inflammatory, antidepressant, antioxidant and antinociceptive effects. α-Spinasterol inhibits COX-1 andCOX-2 activities with IC50 values of 16.17 μM and 7.76 μM, respectively.
|
-
- HY-114423
-
-
- HY-B2193
-
|
α-Amylase
|
Others
|
Others
|
|
α-Amylase is a hydrolase enzyme that catalyses the hydrolysis of internal α-1, 4-glycosidic linkages in starch to yield products like glucose and maltose.
|
-
- HY-136347
-
-
- HY-B0141A
-
-
- HY-130264
-
|
HIF-2α-IN-2
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA).
|
-
- HY-N0710
-
|
alpha-Cyperone
α-Cyperone; (+)-α-Cyperone
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
alpha-Cyperone (α-Cyperone) is associated with the down-regulation of COX-2, IL-6, Nck-2, Cdc42 and Rac1, resulting in reduction of inflammation, which would be highly beneficial for treatment of inflammatory diseases such as AD.
|
-
- HY-N0700
-
-
- HY-123489
-
-
- HY-125833
-
|
Alpha-Naphthoflavone
|
Aromatase
|
Cancer
|
|
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
|
-
- HY-102022
-
|
α-Galactosylceramide
α-GalCer; KRN7000
|
Others
|
Cancer
Inflammation/Immunology
|
|
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).
|
-
- HY-113962
-
|
7α,25-Dihydroxycholesterol
7α,25-OHC
|
EBI2/GPR183
Endogenous Metabolite
|
Inflammation/Immunology
|
|
7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
|
-
- HY-114771
-
-
- HY-13671
-
|
LW6
HIF-1α inhibitor; LW8
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
|
LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 of 4.4 μM. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
|
-
- HY-121618
-
|
α-Thujone
|
GABA Receptor
Reactive Oxygen Species
Parasite
Apoptosis
Autophagy
|
Cancer
Infection
Neurological Disease
|
|
α-Thujone is a monoterpene isolated from Thuja occidentalis essential oil with potent anti-tumor activities. α-Thujone is a reversible modulator of the GABA type A receptor and the IC50 for α-Thujone is 21 μM in suppressing the GABA-induced currents. α-Thujone induces ROS accumulation-dependent cytotoxicity, also induces cell apoptosis and autophagy. α-Thujone has antinociceptive, insecticidal, and anthelmintic activity, and easily penetrates the blood-brain barrier.
|
-
- HY-N6602
-
|
α-Solanine
|
Apoptosis
|
Cancer
|
|
α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in potatoes, has been observed to inhibit growth and induce apoptosis in cancer cells.
|
-
- HY-100542
-
-
- HY-P1365A
-
|
α-Conotoxin MII TFA
α-CTxMII TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
|
-
- HY-19776
-
-
- HY-131005
-
-
- HY-P1268
-
|
α-Conotoxin PIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-126683
-
-
- HY-N7264
-
|
7α-Hydroxycholesterol
|
Others
|
Metabolic Disease
|
|
7α-Hydroxycholesterol is a cholesterol oxide and is formed by both enzymatic and non-enzymatic oxidation. 7α-Hydroxycholesterol can be used as a biomarker for lipid peroxidation.
|
-
- HY-N8531
-
|
4α-Methylcholesterol
|
Others
|
Others
|
|
4α-Methylcholesterol is a Cholesterol derivative. 4α-Methylcholesterol can oxidize 3-hydroxy steroid, with the apparent Km of 12.6 μM.
|
-
- HY-N0728
-
|
α-Linolenic acid
|
PI3K
Akt
|
Cancer
Cardiovascular Disease
|
|
α-Linolenic acid, isolated from seed oils, is an essential fatty acid that cannot be synthesized by humans. α-Linolenic acid can affect the process of thrombotic through the modulation of PI3K/Akt signaling. α-Linolenic acid possess the anti-arrhythmic properties and is related to cardiovascular disease and cancer.
|
-
- HY-N6710
-
-
- HY-Y0191
-
-
- HY-118517
-
|
α-Hydroxytamoxifen
(E)-α-Hydroxy tamoxifen; α-OHTAM
|
Others
|
Cancer
|
|
α-Hydroxytamoxifen is a metabolite of tamoxifen, reacts with DNA in the absence of metabolizing enzymes, and causes formation of DNA adducts.
|
-
- HY-113462
-
|
α-Carotene
|
Others
|
Cancer
|
|
α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer drugs. α-Carotene is isolated from yellow-orange and dark-green vegetables.
|
-
- HY-16686
-
|
α-Tocopherol phosphate
Alpha-Tocopherol phosphate; TocP; vitamin E phosphate
|
Others
|
Others
|
|
α-Tocopherol phosphate is the compound demonstrating the highest vitamin E activity, which is available both in its natural form as RRR-alpha-tocopherol isolated from plant sources.
|
-
- HY-131335
-
|
p38α inhibitor 2
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets.
|
-
- HY-128463
-
-
- HY-P1269
-
|
α-Conotoxin AuIB
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
|
-
- HY-P1860
-
-
- HY-B1203A
-
-
- HY-N2843
-
-
- HY-15484
-
-
- HY-107826
-
-
- HY-100740C
-
|
(1α,1'S,4β)-Lanabecestat
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) is a Beta site APP Cleaving Enzymel (BACE1) inhibitor extracted from patent WO2012087237A1, compound 20a, has IC50s of 2.2 nM (TR-FRET assay) and 0.28 nM (sAPPp release assay), respectively.
|
-
- HY-N1917
-
-
- HY-113038B
-
|
α-Hydroxyglutaric acid
2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid
|
Histone Demethylase
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases.
|
-
- HY-P1268A
-
|
α-Conotoxin PIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
|
-
- HY-W020182
-
|
α-Terpinene
Terpilene
|
Fungal
Parasite
|
Infection
|
|
α-Terpinene (Terpilene) is a monoterpene found in the essential oils of a large variety of foods and aromatic plants such as Mentha piperita. α-Terpinene is active against Trypanosoma evansi and has the potential for trypanosomosis treatment. α-Terpinene has antioxidant and antifungal properties.
|
-
- HY-113038
-
|
D-α-Hydroxyglutaric acid
(R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
Neurological Disease
|
|
D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
|
-
- HY-121222
-
|
alpha-Bisabolol
|
Apoptosis
|
Cancer
|
|
alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
|
-
- HY-115433
-
-
- HY-B1513
-
-
- HY-112535
-
-
- HY-N5142
-
|
α-Terpineol
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
α-Terpineol is isolated from Eucalyptus globulus Labill, exhibits strong antimicrobial activity against periodontopathic and cariogenic bacteria.
α-Terpineol possesses antifungal activity against T. mentagrophytes, and the activity might lead to irreversible cellular disruption.
|
-
- HY-128417
-
-
- HY-P1267
-
|
α-Conotoxin PnIA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-B0225B
-
|
Methyldopa hydrate
L-(-)-α-Methyldopa hydrate; MK-351 hydrate
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa hydrate (L-(-)-α-Methyldopa hydrate), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrate is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
|
-
- HY-B0225A
-
|
Methyldopa hydrochloride
L-(-)-α-Methyldopa hydrochloride; MK-351 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa hydrochloride (L-(-)-α-Methyldopa hydrochloride) hydrochloride, a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa hydrochloride is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
|
-
- HY-B0225
-
|
Methyldopa
L-(-)-α-Methyldopa; MK-351
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Methyldopa (L-(-)-α-Methyldopa), a potent antihyoertensive agent, is an alpha-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopa is a prodrug and is metabolized (α-Methylepinephrine) in the central nervous system.
|
-
- HY-N0642
-
|
α-L-Rhamnose monohydrate
|
Others
|
Infection
Metabolic Disease
Cancer
|
|
α-L-Rhamnose monohydrate is a component of the plant cell wall pectic polysaccharides rhamnogalacturonan I and rhamnogalacturonan II. α-L-Rhamnose monohydrate is also a component of bacterial polysaccharides where it plays an important role in pathogenicity.
|
-
- HY-N7136
-
|
α-Terpinyl acetate
|
Cytochrome P450
|
Metabolic Disease
|
|
α-Terpinyl acetate is a monoterpene ester isolated from Laurus nobilis L. essential oil. α-Terpinyl acetate is a competitive P450 2B6 substrate which binding to the active site of P450 2B6 with a Kd value of 5.4 μM.
|
-
- HY-N0629
-
-
- HY-109564
-
-
- HY-43470
-
-
- HY-P1269A
-
-
- HY-101332
-
|
EGLU
(2S)-α-Ethylglutamic acid; (2S)-α-EGLU
|
mGluR
|
Neurological Disease
|
|
EGLU ((2S)-α-Ethylglutamic acid; (2S)-α-EGLU) is a potent and competitive mGluR-2 receptor antagonist. EGLU interacts with (lS,3S)-ACPD-sensitive site with a Kd value of 66 μM. EGLU is an antidepressant agent.
|
-
- HY-N2842
-
-
- HY-N0548
-
|
α-Angelica lactone
|
Gutathione S-transferase
|
Cancer
|
|
α-Angelica lactone is a naturally occurring anticarcinogen and an vinylogous nucleophile. α-Angelica lactone can give the chiral δ-amino γ,γ-disubstituted butenolide carbonyl derivatives and exhibitselectrophilic trapping at the γ-carbon. α-Angelica lactone exerts strong chemoprotective effects by selective enhancement of glutathione-S-thansferase (GST) and UDP-glucononosyltransferase (UGT) detoxification enzymes.
|
-
- HY-15793
-
-
- HY-113209
-
|
8-Isoprostaglandin F2α
|
Endogenous Metabolite
|
Others
|
|
8-Isoprostaglandin F2α is an isoprostane produced by the non-enzymatic peroxidation of arachidonic acid in membrane phospholipids. 8-Isoprostaglandin F2α is present in human plasma in two distinct forms - esterified in phospholipids and as the free acid. 8-Isoprostaglandin F2α is a weak TP receptor agonist in vascular smooth muscle.
|
-
- HY-B1278
-
-
- HY-13249
-
|
1alpha-Hydroxy VD4
1α-Hydroxy vitamin D4
|
VD/VDR
|
Cancer
|
|
1alpha-Hydroxy VD4 , a 1alpha(OH)D derivative, can effectively induce the differentiation of monoblastic leukaemia U937, P39/TSU and P31/FUJ cells.
|
-
- HY-P1267A
-
|
α-Conotoxin PnIA TFA
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin PnIA TFA, a potent and selective antagonist of the mammalian α7 nAChR, has the potential for the research of neurological conditions such as neuropathic pain and Alzheimer’s disease.
|
-
- HY-N6913
-
|
3α-Hydroxymogrol
|
AMPK
|
Metabolic Disease
|
|
3α-Hydroxymogrol is a triterpenoid isolated from Siraitia grosvenorii Swingle, acts as a potent AMPK activator, and enhances AMPK phosphorylation.
|
-
- HY-B0742
-
|
Hydroxyprogesterone caproate
17α-Hydroxyprogesterone hexanoate; 17α-Hydroxyprogesterone caproate
|
Others
|
Others
|
|
Hydroxyprogesterone caproate is a synthetic, steroidal progestin; an ester derivative of 17α-hydroxyprogesterone formed from caproic acid.
|
-
- HY-110203
-
|
R-7050
TNF-α Antagonist III
|
TNF Receptor
|
Cancer
|
|
R-7050 (TNF-α Antagonist III) is a tumor necrosis factor receptor (TNFR) antagonist with greater selectivity toward TNFα.
|
-
- HY-18733
-
-
- HY-112716
-
-
- HY-P9908
-
-
- HY-118608
-
-
- HY-100999
-
-
- HY-119674
-
|
Xanthopterin
|
DNA/RNA Synthesis
|
Infection
|
|
Xanthopterin, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm. Xanthopterin (XPT) causes renal growth and hypertrophy in rat.
Xanthopterin inhibits RNA synthesis.
|
-
- HY-N6854A
-
-
- HY-N7785
-
-
- HY-121879
-
-
- HY-B0979
-
|
Lobeline hydrochloride
α-Lobeline hydrochloride; L-Lobeline hydrochloride
|
nAChR
|
Neurological Disease
|
|
Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
|
-
- HY-N0549
-
-
- HY-141336
-
-
- HY-119674A
-
|
Xanthopterin (hydrate)
|
DNA/RNA Synthesis
|
Inflammation/Immunology
Cancer
|
|
Xanthopterin hydrate, an unconjugated pteridine compound, is the main component of the yellow granule in the Oriental hornet bear wings, produces a characteristic excitation/emission maximum at 386/456 nm. Xanthopterin hydrate(XPT) causes renal growth and hypertrophy in rat.
Xanthopterin hydrate inhibits RNA synthesis.
|
-
- HY-13331
-
|
Clascoterone
Cortexolone 17 Alpha-propionate; Cortexolone 17α-propionate; CB-03-01
|
Androgen Receptor
|
Endocrinology
|
|
Clascoterone (Cortexolone 17 alpha-propionate;Cortexolone 17α-propionate;CB-03-01) is a new topical and peripherally selective androgen antagonist.
|
-
- HY-135190
-
-
- HY-U00333
-
-
- HY-N6825
-
-
- HY-B1278A
-
-
- HY-128420
-
|
Lobeline sulfate
α-Lobeline sulfate; L-Lobeline sulfate
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation.
|
-
- HY-N7389B
-
|
GDP-α-D-mannose disodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM).
|
-
- HY-129459
-
|
α-Tocotrienol
|
Others
|
Neurological Disease
Cardiovascular Disease
|
|
α-Tocotrienol is an isoform of vitamin E and found in vegetables, fruits, seeds, nuts, grains, and oils. Vitamin E plays a role as an antioxidant, in lowering cholesterol and other lipids, as a neuroprotective and anticancer agent, and in cardiovascular disease protection.
|
-
- HY-B0522A
-
|
Ampicillin sodium
D-(-)-α-Aminobenzylpenicillin sodium salt
|
Bacterial
Antibiotic
|
Infection
|
|
Ampicillin sodium (D-(-)-α-Aminobenzylpenicillin sodium salt) is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
|
-
- HY-128942
-
-
- HY-32350
-
-
- HY-136278
-
|
NOC 18
|
NO Synthase
|
Cardiovascular Disease
|
|
NOC 18 is a nitric oxide donor and activates an inward current in cultured rat cerebellar granules cells. NOC 18 increases cGMP production in cultured vascular smooth muscle cells. NOC 18 reduces contractility of cardiac muscle preparations in vitro.
|
-
- HY-N4215
-
|
11(α)-Methoxysaikosaponin F
|
Others
|
Inflammation/Immunology
|
|
11(α)-Methoxysaikosaponin F is a triterpenoid saponin isolated from Bupleurum marginatum Wall.ex DC(ZYCH) which is a promising therapeutic for liver fibrosis. 11(α)-Methoxysaikosaponin F has an IC50 of 387.7 nM with viability of hepatic stellate cells-T6 (HSCs-T6). Triterpenoid saponins have numerous targets, important network positions, and strong inhibitory activity.
|
-
- HY-W013636
-
|
2-Ketoglutaric acid
Alpha-Ketoglutaric acid
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM).
|
-
- HY-W039897
-
-
- HY-N3802
-
|
Eleutheroside C
Ethyl α-D-galactoside; Ethyl α-D-galactopyranoside
|
Others
|
Others
|
|
Eleutheroside C (Ethyl α-D-galactoside) is a glycoside isolated from the bulbs of Polianthes tuberosa.
|
-
- HY-W013636A
-
|
2-Ketoglutaric acid Sodium
Alpha-Ketoglutaric acid Sodium
|
Tyrosinase
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM).
|
-
- HY-12710A
-
-
- HY-15157
-
|
Calcitetrol
1α, 24, 25-Trihydroxy VD3
|
VD/VDR
|
Metabolic Disease
|
|
Calcitetrol(1α, 24, 25-Trihydroxy VD3) is the hormonally active form of vitamin D with three hydroxyl groups.
|
-
- HY-N0181A
-
|
Lumisterol
9β,10α-Ergosterol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Lumisterol (9β,10α-Ergosterol), a steroid compound, is the (9β,10α)-stereoisomer of Ergosterol. Lumisterol is a photoprotective agent against UVB-induced DNA damage and anti-proliferative activities.
|
-
- HY-P1294
-
-
- HY-12956
-
-
- HY-128747A
-
-
- HY-128747
-
-
- HY-N0173
-
|
Cinchonidine
α-Quinidine
|
Serotonin Transporter
Parasite
|
Infection
|
|
Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
|
-
- HY-N7087
-
|
Tulipalin A
α-Methylene butyrolactone
|
Drug Metabolite
|
|
|
Tulipalin A (α-Methylene butyrolactone) is a toxic glycoside isolated from the tulip bulbs. Tulipalin A is a causative allergen that induces Allergic contact dermatitides. Tulipalin A (α-Methylene butyrolactone) at low dose affects the functionality of immune cells, such as Jurkat T cells.
|
-
- HY-125648
-
|
Euphorbadienol
Alpha-Euphorbol
|
Others
|
Infection
|
|
Euphorbadienol (alpha-Euphorbol), a triterpenic compound, isolated from the latex of Euphorbia resinifera. The derivatives of Euphorbadienol can be used as elicitors of disease resistance, and has antileishmanial and antitrypanosomal activity.
|
-
- HY-113381
-
-
- HY-W010248
-
-
- HY-U00439A
-
|
Protein kinase inhibitors 1 hydrochloride
(E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride
|
DYRK
|
Cancer
|
|
Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
|
-
- HY-128428
-
|
Carboprost
15(S)-15-Methyl Prostaglandin F2α; 15-Methyl-PGF2α
|
Others
|
Endocrinology
|
|
Carboprost (15(S)-15-Methyl Prostaglandin F2α) is a metabolically stable synthetic analog of prostaglandin F2α. Carboprost stimulates uterine contractions and induces abortion. Carboprost is used for postpartum hemorrhage due to uterine atony and for the termination of pregnancy in the second trimester.
|
-
- HY-P1758
-
-
- HY-N2990
-
-
- HY-N2042
-
-
- HY-19373
-
-
- HY-15156
-
-
- HY-104004
-
-
- HY-P0252
-
-
- HY-P1294A
-
-
- HY-P1868
-
|
α2β1 Integrin Ligand Peptide
|
Integrin
|
Infection
|
|
α2β1 Integrin Ligand Peptide interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-113259
-
|
7α-Hydroxy-4-cholesten-3-one
|
Endogenous Metabolite
|
Metabolic Disease
|
|
7α-Hydroxy-4-cholesten-3-one is an intermediate in synthesis of bile acids from cholesterol. 7α-Hydroxy-4-cholesten-3-one is a pregnane X receptor (PXR) agonist. 7α-Hydroxy-cholest-4-en-3-one is a biomarker for bile acid loss, irritable bowel syndrome, and other diseases associated with defective bile acid biosynthesis. 7α-Hydroxy-cholest-4-en-3-one is the physiological substrate for CYP8B1.
|
-
- HY-141126
-
-
- HY-107819
-
-
- HY-14618
-
|
Zingiberene
α-Zingiberene; (-)-Zingiberene
|
Autophagy
|
Cancer
|
|
Zingiberene (α-Zingiberene) is a monocyclic sesquiterpene which is the predominant constituent of ginger with oil content (Zingiber officinale). Neuroprotective potential. Zingiberene triggers autophagy. Anticancer activity.
|
-
- HY-U00141
-
|
ABTL-0812
α-Hydroxylinoleic acid
|
Autophagy
|
Metabolic Disease
|
|
ABTL-0812 (α-Hydroxylinoleic acid) induces endoplasmic reticulum (ER) stress-mediated autophagy. ABTL-0812 is a first-in-class small molecule with anti-cancer activity.
|
-
- HY-B0522B
-
|
Ampicillin trihydrate
D-(-)-α-Aminobenzylpenicillin trihydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Ampicillin trihydrate (D-(-)-α-Aminobenzylpenicillin trihydrate) is a broad-spectrum beta-lactam antibiotic against a variety of gram-positive and gram-negative bacteria.
|
-
- HY-N2048
-
|
2,2':5',2''-Terthiophene
α-Terthiophene; α-Terthienyl; Trithiophene
|
Bacterial
Antibiotic
|
Infection
|
|
2,2':5',2''-Terthiophene (α-Terthiophene) is an oligomer of the heterocycle thiophene. 2,2':5',2''-Terthiophene has been employed as building block for the organic semi-conductor polythiophene.
|
-
- HY-B0216
-
-
- HY-12956A
-
|
Dinoprost tromethamine salt
Prostaglandin F2α tromethamine salt; PGF2α THAM; Prostaglandin F2α THAM
|
Prostaglandin Receptor
Endogenous Metabolite
Autophagy
Apoptosis
|
Endocrinology
|
|
Dinoprost tromethamine salt (Prostaglandin F2α tromethamine salt) is an orally active, potent prostaglandin F (PGF) receptor (FP receptor) agonist. Dinoprost tromethamine salt is a luteolytic hormone produced locally in the endometrial luminal epithelium and corpus luteum (CL). Dinoprost tromethamine salt plays a key role in the onset and progression of labour.
|
-
- HY-108652
-
-
- HY-P1868A
-
|
α2β1 Integrin Ligand Peptide TFA
|
Integrin
|
Others
|
|
α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
|
-
- HY-133887
-
-
- HY-N2994
-
-
- HY-N0179
-
|
Ecdysone
α-Ecdysone
|
Endogenous Metabolite
Apoptosis
|
Metabolic Disease
|
|
Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
|
-
- HY-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-15327
-
-
- HY-100371
-
|
(RS)-MCPG
Alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
|
-
- HY-N6821
-
-
- HY-115292
-
|
Simvastatin hydroxy acid sodium
Tenivastatin sodium; Simvastatin Impurity A sodium
|
HMG-CoA Reductase (HMGCR)
|
Cancer
|
|
Simvastatin hydroxy acid sodium (Tenivastatin sodium; Simvastatin Impurity A sodium) is an active hydrolytic metabolite of Simvastatin (HY-17502). Simvastatin shows a inhibition of HMG-CoA reductase with a Ki value of 0.12 nM.
|
-
- HY-N7433
-
-
- HY-133538
-
-
- HY-N0989
-
-
- HY-112174
-
-
- HY-P2558
-
-
- HY-140960
-
-
- HY-17571
-
|
Oxytocin
α-Hypophamine; Oxytocic hormone
|
Oxytocin Receptor
|
Endocrinology
|
|
Oxytocin (α-Hypophamine; Oxytocic hormone) is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
|
-
- HY-114362
-
-
- HY-12316
-
|
20(S)-Hydroxycholesterol
20α-Hydroxycholesterol
|
Smo
Endogenous Metabolite
|
Cancer
|
|
20(S)-hydroxyCholesterol (20α-Hydroxycholesterol) is an allosteric activator of the oncoprotein smoothened (Smo) that activates the hedgehog (Hh) signaling pathway with an EC50 of 3 μM in a gene transcription reporter assay using NIH3T3 cells.
|
-
- HY-B1060
-
-
- HY-B1065
-
-
- HY-Y0124
-
|
NSC 16590
α,α-Dimethylglycine; α-Aminoisobutanoic acid
|
Endogenous Metabolite
|
Others
|
|
NSC 16590 inhibits the production of endogenous ethylene in the cotyledonary segments of cocklebur.
|
-
- HY-135813
-
|
LtaS-IN-1
|
Bacterial
|
Infection
|
|
LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
|
-
- HY-N6911
-
-
- HY-N4310
-
-
- HY-B0717
-
|
Tocofersolan
TPGS; D-α-Tocopherol polyethylene glycol 1000 succinate; Vitamin E-TPGS
|
Others
|
Metabolic Disease
|
|
Tocofersolan is a synthetic polyethylene glycol derivative of α-tocopherol.
|
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-N5128
-
-
- HY-18728
-
-
- HY-103641
-
-
- HY-103641A
-
-
- HY-141137
-
-
- HY-125957
-
|
A-3 hydrochloride
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
|
-
- HY-P9911
-
|
Vedolizumab
Anti-Human lymphocyte α4β7 integrin, Humanized Antibody
|
Integrin
|
Inflammation/Immunology
|
|
Vedolizumab is a humanized monoclonal antibody that targets the α4β7 integrin for the treatment of ulcerative colitis and Crohn's disease.
|
-
- HY-W018512
-
-
- HY-15583
-
-
- HY-N2174
-
-
- HY-122470
-
|
Stampidine
|
Reverse Transcriptase
HIV
|
Infection
|
|
Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
|
-
- HY-113960
-
|
ERRα antagonist-1
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-1 (Compound A) is a selective and high affinity estrogen-related receptor α (ERRα) antagonist. ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1.
|
-
- HY-11007
-
|
GNF-2
|
Bcr-Abl
SARS-CoV
|
Cancer
|
|
GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
|
-
- HY-101491
-
|
SR-18292
|
PGC-1α
Autophagy
|
Metabolic Disease
|
|
SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
|
-
- HY-110266
-
|
GN44028
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
GN44028 is a hypoxia inducible factor (HIF)-1 inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization.
|
-
- HY-14571
-
|
E7820
ER68203-00
|
Integrin
|
Cancer
|
|
E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity.
|
-
- HY-15438
-
|
SB 415286
|
GSK-3
Apoptosis
|
Metabolic Disease
|
|
SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
|
-
- HY-111507
-
|
PDGFRα kinase inhibitor 1
|
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-111387
-
-
- HY-18371
-
|
TC-S 7009
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ≫ 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression.
|
-
- HY-14929A
-
|
Migalastat hydrochloride
GR181413A
|
Others
|
Others
|
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- HY-N4327
-
|
Eurycomalactone
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Eurycomalactone is a natural product found in Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor, with an IC50 of 0.5 μM. Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.
|
-
- HY-U00459
-
|
GSK2850163
|
IRE1
|
Cancer
|
|
GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- HY-U00459B
-
|
GSK2850163 hydrochloride
|
IRE1
|
Cancer
|
|
GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- HY-125840
-
|
Belzutifan
PT2977; MK-6482
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC).
|
-
- HY-100735
-
-
- HY-107782
-
-
- HY-15672
-
|
FM19G11
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
Neurological Disease
|
|
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions.
|
-
- HY-W019838
-
-
- HY-107532
-
-
- HY-135794
-
|
11-Ketodihydrotestosterone
11-KDHT; 5α-Dihydro-11-keto testosterone
|
Androgen Receptor
|
Endocrinology
|
|
11-Ketodihydrotestosterone (11-KDHT; 5α-Dihydro-11-keto testosterone) is an endogenous steroid and a metabolite of 11β-Hydroxyandrostenedione. 11-Ketodihydrotestosterone is an active androgen and is also a potent androgen receptor (AR) agonist with a Ki of 20.4 nM and an EC50 of 1.35 nM for human AR. 11-Ketodihydrotestosterone drives gene regulation, protein expression and cell growth in androgen-dependent prostate cancer cells.
|
-
- HY-N2143
-
-
- HY-N0242
-
-
- HY-B1203
-
-
- 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-12867
-
-
- HY-17537
-
|
APY29
|
IRE1
|
Cancer
|
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain.
|
-
- HY-107371
-
-
- HY-N2071
-
|
Cedrol
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.
|
-
- HY-B0942
-
-
- HY-112910
-
|
Grp94 Inhibitor-1
|
HSP
|
Cancer
Infection
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
|
-
- HY-112502
-
|
MethADP
Adenosine 5'-(α,β-methylene)diphosphate
|
CD73
|
Cancer
|
|
MethADP is a specific CD73 inhibitor.
|
-
- HY-120675
-
|
SSTC3
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-11087
-
-
- HY-50855B
-
-
- HY-N4162
-
-
- HY-U00313
-
-
- HY-19763
-
|
BEBT-908
PI3Kα inhibitor 1
|
PI3K
|
Cancer
|
|
BEBT-908 (PI3Kα inhibitor 1) is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
|
-
- HY-N1064
-
|
Xanthoplanine
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
|
-
- HY-N1132
-
-
- HY-N0417
-
|
Cucurbitacin E
α-Elaterin; α-Elaterine
|
CDK
Autophagy
|
Cancer
|
|
Cucurbitacin E is a natural compound which from the climbing stem of Cucumic melo L. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
|
-
- HY-U00090
-
-
- HY-U00326
-
|
PI3Kα/mTOR-IN-1
|
PI3K
mTOR
|
Cancer
|
|
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
|
-
- HY-129453
-
|
BOP sodium
|
Integrin
|
Inflammation/Immunology
|
|
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins.
|
-
- HY-121172
-
|
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-50855
-
-
- HY-133807A
-
-
- HY-14975
-
-
- HY-19332
-
|
Kifunensine
FR-900494
|
Others
|
Inflammation/Immunology
|
|
Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.
|
-
- HY-125713
-
|
Ganoderic acid Y
|
Glucosidase
Enterovirus
|
Infection
|
|
Ganoderic acid Y is a α-glucosidase inhibitor with an IC50 of 170 μM for yeast α-glucosidase. Ganoderic acid Y inhibits enterovirus 71 (EV71) replication through blocking EV71 uncoating.
|
-
- HY-15893
-
|
DMOG
Dimethyloxallyl Glycine
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
|
Cancer
|
|
DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation in vitro and in vivo. DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal. DMOG induces cell autophagy.
|
-
- HY-131345
-
|
PI3Kα-IN-4
|
PI3K
|
Cancer
|
|
PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity.
|
-
- HY-N6782
-
|
Oligomycin
|
ATP Synthase
Fungal
Antibiotic
|
Cancer
Infection
|
|
Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
|
-
- HY-15969
-
|
Sal003
|
Phosphatase
Apoptosis
|
Cancer
|
|
Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal.
|
-
- HY-10257
-
-
- HY-10401
-
-
- HY-N2166
-
|
Tomatine
α-Tomatine; Lycopersicin; Tomatin
|
Proteasome
Apoptosis
|
Neurological Disease
|
|
Tomatine is a glycoalkaloid, found in the tomato plant (Lycopersicon esculentum Mill.). Tomatine elicits neurotoxicity in RIP1 kinase and caspase-independent manner. Tomatine promotes the upregulation of nuclear apoptosis inducing factor (AIF) in neuroblastoma cells. Tomatine also inhibits 20S proteasome activity.
|
-
- HY-107406
-
|
Antimycin A1
|
Mitochondrial Metabolism
|
Cancer
|
|
Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
|
-
- HY-14126
-
-
- HY-U00179
-
-
- HY-114368A
-
-
- HY-114368
-
|
Kira8
AMG-18
|
IRE1
|
Inflammation/Immunology
|
|
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM.
|
-
- HY-N0933
-
-
- HY-B0648
-
-
- HY-12285
-
|
Serabelisib
MLN1117; INK1117; TAK-117
|
PI3K
|
Cancer
|
|
Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
|
-
- HY-120874
-
|
PF-06372865
|
GABA Receptor
|
Neurological Disease
|
|
PF-06372865 is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). PF-06372865 is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. PF-06372865 can across the blood-brain barrier (BBB). PF-06372865 has anxiolytic activity and has the potential for epilepsy.
|
-
- HY-B0379A
-
|
Adiphenine hydrochloride
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 µM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has narcotic and anticonvulsant effects.
|
-
- HY-N0877
-
|
Bufalin
|
Na+/K+ ATPase
|
Cancer
|
|
Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively. Anti-cancer activity.
|
-
- HY-16187
-
-
- HY-19707
-
-
- HY-10231
-
-
- HY-103384
-
|
TMCB
|
Casein Kinase
|
Cancer
|
|
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively.
|
-
- HY-103454
-
-
- HY-10328
-
|
Neflamapimod
VX-745
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
|
-
- HY-12012
-
-
- HY-16031
-
-
- HY-N0374
-
-
- 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-133807
-
|
Benpyrine
|
TNF Receptor
|
Inflammation/Immunology
|
|
Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research.
|
-
- HY-19710
-
|
MKC3946
|
IRE1
|
Cancer
|
|
MKC3946 is a potent and soluble IRE1α inhibitor, used for cancer research.
|
-
- HY-N0466
-
-
- HY-13261
-
|
A66
|
PI3K
|
Cancer
|
|
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
|
-
- HY-70073
-
-
- HY-129619
-
|
SNIPER(ER)-87
|
SNIPER
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation.
|
-
- HY-16194
-
-
- HY-14857
-
-
- HY-N2566
-
|
Euscaphic acid
|
DNA/RNA Synthesis
PI3K
Apoptosis
|
Cancer
|
|
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM. Euscaphic acid induces apoptosis.
|
-
- HY-111255
-
|
SPD304
|
TNF Receptor
|
Cancer
|
|
SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
|
-
- HY-111255A
-
|
SPD304 dihydrochloride
|
TNF Receptor
|
Inflammation/Immunology
|
|
SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 µM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α.
|
-
- HY-116446
-
|
Pironetin
|
Microtubule/Tubulin
|
Cancer
|
|
Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity.
|
-
- HY-10801
-
-
- HY-108697A
-
-
- HY-U00037
-
|
Ecopladib
PLA 725
|
Phospholipase
|
Inflammation/Immunology
|
|
Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
|
-
- HY-13281
-
|
PIK-75 hydrochloride
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 hydrochloride induces apoptosis.
|
-
- HY-107834
-
|
PIK-75
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM). PIK-75 induces apoptosis.
|
-
- HY-17538
-
-
- HY-135674
-
|
SR-318
|
p38 MAPK
TNF Receptor
|
Cancer
Inflammation/Immunology
|
|
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity.
|
-
- HY-16294
-
|
LY2090314
|
GSK-3
|
Cancer
|
|
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
|
-
- 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-N6967
-
|
Levomenol
(-)-α-Bisabolol
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
Levomenol is a monocyclic sesquiterpene alcohol found in various plants and mainly in Matricaria chamomilla, which exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol has neuroprotective effects, can attenuate nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain.
|
-
- HY-N6709
-
|
Zeranol
α-Zearalanol
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Zeranol, a metabolite of the mycoestrogen zearalenone, is an estrogen receptor agonist. Zeranol is used as a growth promoter of livestock due to its strong estrogenic activity.
|
-
- HY-N1974
-
-
- HY-B0522
-
-
- HY-B1761
-
|
Santonin
Alpha-Santonin
|
Parasite
|
Infection
|
|
Santonin is an active principle of the plant Artemisia cina, which is formely used to treat worms.
|
-
- HY-115463
-
|
EB-3D
|
AMPK
Apoptosis
|
Cancer
|
|
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity.
|
-
- HY-12519
-
|
Oltipraz
RP 35972; NSC 347901
|
HIF/HIF Prolyl-Hydroxylase
HIV
Keap1-Nrf2
|
Cancer
|
|
Oltipraz has an inhibitory effect on HIF-1α activation in a time-dependent manner, completely abrogating HIF-1α induction at ≥10 μM concentrations, the IC50 of Oltipraz for HIF-1α inhibition is 10 μM. Oltipraz is a potent Nrf2 activator.
|
-
- HY-U00266
-
-
- HY-13864
-
-
- HY-101272
-
|
GDC-0326
|
PI3K
|
Cancer
|
|
GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
|
-
- HY-10403
-
-
- HY-15761
-
|
AZD2858
|
GSK-3
|
Neurological Disease
|
|
AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
|
-
- HY-B0392
-
-
- HY-108431
-
|
MN58b
|
Apoptosis
|
Cancer
|
|
MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity.
|
-
- HY-12398A
-
|
TEI-9648
|
VD/VDR
|
Metabolic Disease
Inflammation/Immunology
|
|
TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research.
|
-
- HY-112023
-
|
Lumisterol 3 (>90%)
9β,10α-Cholesta-5,7-dien-3β-ol; Cholecalciferol EP Impurity A
|
Endogenous Metabolite
|
Others
|
|
Lumisterol 3 (>90%) (9β,10α-Cholesta-5,7-dien-3β-ol) is a normal human secosterooid metabolite from the class of vitamin D3 photoisomer derivatives. Lumisterol 3 (>90%) is used in the preparation of vitamin D.
|
-
- HY-111547
-
|
M1001
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
M1001 is a weak agonist of HIF-2α, directly binds to the HIF-2α PAS-B domain, with a Kd of 667 nM. M1001 enhances the stabilities of HIF-2α-ARNT complex.
|
-
- HY-120111
-
-
- HY-W009009
-
|
L-838417
|
GABA Receptor
|
Neurological Disease
|
|
L-838417 is a selective partial agonist at the α2, α3 and α5 subtypes of the GABAA receptor and an antagonist at the α1, with binding Ki values of 0.79 nM, 0.67 nM, 1.67 nM, 267 nM, 2.25 nM and 2183 nM for α1β3γ2, α2β3γ2, α3β3γ2, α4β3γ2, α5β3γ2 and α6β3γ2.
|
-
- HY-12825
-
|
BHPI
|
Estrogen Receptor/ERR
|
Cancer
|
|
BHPI is a potent inhibitor of nuclear estrogen–ERα-regulated gene expression; elicits sustained ERα-dependent activation of the endoplasmic reticulum (EnR) stress sensor, the unfolded protein response (UPR), and persistent inhibition of protein synthesis.
|
-
- HY-108645
-
|
AL 8697
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity.
|
-
- HY-U00458
-
|
K-80003
TX-803
|
Akt
|
Cancer
|
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-100337
-
-
- HY-16937
-
-
- HY-135385
-
-
- HY-103248
-
|
Toyocamycin
Vengicide
|
IRE1
Fungal
Antibiotic
Apoptosis
|
Cancer
Infection
|
|
Toyocamycin (Vengicide) is an adenosine analog produced by Actinomycete, acts as an XBP1 inhibitor, inhibits IRE1α-induced ATP-dependent XBP1 mRNA cleavage, with an IC50 of 80 nM. Toyocamycin (Vengicide) induces apoptosis. Toyocamycin (Vengicide) shows no effect on IRE1α auto-phosphorylation.
|
-
- HY-110193
-
|
SPP-86
|
RET
|
Cancer
|
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells.
|
-
- HY-N1132A
-
|
D-(+)-Trehalose dihydrate
D-Trehalose dihydrate; α,α-Trehalose dihydrate
|
Others
|
Others
|
|
D-(+)-Trehalose dihydrate, isolated from Saccharomyces cerevisiae, can be used as a food ingredient and pharmaceutical excipient.
|
-
- HY-U00425
-
-
- HY-N4121
-
|
Isocurcumenol
|
Estrogen Receptor/ERR
Apoptosis
|
|
|
Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1µg/mL and 178.2 µg/mL in DLA and KB cells, respectively.
|
-
- HY-12398
-
|
TEI-9647
|
VD/VDR
|
Metabolic Disease
Inflammation/Immunology
|
|
TEI-9647, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget's disease.
|
-
- HY-B1696A
-
|
Methyldopate hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Methyldopate hydrochloride is an ethyl ester hydrochloride prodrug of α-Methyldopa (α-MD; HY-B0225). Methyldopa (L-(-)-α-Methyldopa) is an α-adrenergic agonist (selective for α2-adrenergic receptors). Methyldopate hydrochloride has the potential for severe hypertension research.
|
-
- HY-B0744
-
|
Eflornithine
DFMO; MDL71782; RMI71782; α-difluoromethylornithine
|
Others
|
Infection
|
|
Eflornithine is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-B0744A
-
|
Eflornithine hydrochloride
DFMO hydrochloride; MDL71782 hydrochloride; RMI71782 hydrochloride; α-difluoromethylornithine hydrochloride
|
Others
|
Infection
|
|
Eflornithine hydrochloride is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-101562
-
|
GDC-0077
RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
GDC-0077 (RG6114) is a potent, orally available, and selective PI3Kα inhibitor (IC50=0.038 nM). GDC-0077 (RG6114) exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. GDC-0077 (RG6114) is more selective for mutant versus wild-type PI3Kα.
|
-
- HY-101068
-
-
- HY-N6722
-
-
- HY-U00206
-
-
- HY-128677
-
|
NCC007
|
Casein Kinase
|
Neurological Disease
|
|
NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
|
-
- HY-119307
-
|
Apratastat
|
MMP
TNF Receptor
|
Cancer
|
|
Apratastat is an orally active, potent, and reversible dual inhibitor of tumor necrosis factor-α converting enzyme (TACE) and matrix metalloproteinases (MMPs) . Apratastat can potently inhibit the release of TNF-α in vitro, ex vivo, and in vivo with IC50s of 144 ng/mL in vitro and 81.7 ng/mL ex vivo, respectively.
|
-
- HY-101640
-
-
- HY-B0744B
-
|
Eflornithine hydrochloride hydrate
DFMO hydrochloride hydrate; MDL-71782 hydrochloride hydrate; RMI-71782 hydrochloride hydrate; α-difluoromethylornithine hydrochloride hydrate
|
Others
|
Cancer
|
|
Eflornithine hydrochloride hydrate (DFMO hydrochloride hydrate) is a specific, irreversible inhibitor of the enzyme ornithine decarboxylase. Eflornithine hydrochloride hydrate is a medication for the treatment of African trypanosomiasis and excessive facial hair growth in women.
|
-
- HY-111478
-
-
- HY-13453
-
|
BAY 11-7082
BAY 11-7821
|
IKK
Deubiquitinase
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
|
-
- HY-U00399
-
-
- HY-B0471
-
-
- HY-100300
-
-
- HY-111055
-
|
BIP-135
|
GSK-3
|
Neurological Disease
|
|
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect.
|
-
- HY-110398
-
|
5,6,7-Trimethoxyflavone
Baicalein trimethyl ether
|
p38 MAPK
|
Inflammation/Immunology
Cancer
|
|
5,6,7-Trimethoxyflavone is a novel p38-α MAPK inhibitor with an anti-inflammatory effect. 5,6,7-Trimethoxyflavone is isolated from several plants including Zeyhera tuberculosa, Callicarpa japonica, and Kickxia lanigera.
|
-
- HY-19383
-
|
Ertiprotafib
PTP 112
|
Phosphatase
IKK
PPAR
|
Metabolic Disease
|
|
Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
|
-
- HY-13635A
-
|
Finasteride acetate
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-A0009
-
|
Galanthamine hydrobromide
Galantamine hydrobromide
|
AChE
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD).
|
-
- HY-13635
-
|
Finasteride
MK-906
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia.
|
-
- HY-N0127
-
-
- HY-B0371D
-
|
(S)-Terazosin
|
Adrenergic Receptor
|
Endocrinology
|
|
(S)-Terazosin is an active S-enantiomer of Terazosin. (S)-Terazosin is a potent and high-affinity α-adrenoceptor antagonist with Ki values of 3.91 nM, 0.79 nM and 1.16 nM for α1a, α1b and α1d-adrenoceptor, respectively. (S)-Terazosin also has high-affinity for α2a, α2B and α2c-adrenoceptor with Ki values of 729 nM, 3.5 nM and 46.4 nM, respectively.
|
-
- HY-B0194A
-
-
- HY-100947
-
-
- HY-B0194
-
-
- HY-117771A
-
-
- HY-131345A
-
|
(S)-PI3Kα-IN-4
|
PI3K
|
Cancer
|
|
(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer.
|
-
- HY-13229
-
|
BOC-D-FMK
|
Caspase
Apoptosis
|
Cancer
|
|
Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 µM.
|
-
- HY-122058A
-
|
KRH-3955 hydrochloride
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM.
|
-
- HY-U00244
-
-
- HY-101610
-
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-P9926
-
-
- HY-15483
-
-
- HY-112098
-
|
PROTAC ERα Degrader-1
|
PROTAC
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-1 comprises an ubiquitin E3 ligase binding group, a linker and a protein binding group. PROTAC ERα Degrader-1 extracts from patent WO2017201449A1, compound P1. PROTAC ERα Degrader-1 is an estrogen receptor-alpha (ERα) degrader.
|
-
- HY-101722
-
|
Melinamide
AC 223; DL-N-(α-Methylbenzyl)linoleamide
|
Others
|
Metabolic Disease
|
|
Melinamide, an amide derivative of an unsaturated long-chain fatty acid, is an inhibitor of cholesterol absorption with an IC50 of 20.9 μM.
|
-
- HY-12560A
-
|
PNU-282987
|
nAChR
|
Neurological Disease
|
|
PNU-282987 is a selective α7 nicotinic acetylcholine receptor(α7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
|
-
- HY-U00117
-
-
- HY-111846
-
|
PROTAC ERα Degrader-2
|
SNIPER
PROTAC
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERα Degrader-2 comprises a cIAP1 ligand binding group, a linker and an estrogen receptor α (ERα) binding group. PROTAC ERα Degrader-2 is an ERα degrader. Maximal ERα degradation at 30 μM concentration in human mammary tumor MCF7 cells. Degradation inducers based on cIAP1 are called specific and non-genetic IAP-dependent protein erasers (SNIPERs).
|
-
- HY-17552
-
|
sn-Glycero-3-phosphocholine
Choline Alfoscerate; Alpha-GPC; L-α-GPC
|
AChE
Endogenous Metabolite
|
Neurological Disease
|
|
sn-Glycero-3-phosphocholine (Choline Alfoscerate) is a precursor in the biosynthesis of brain phospholipids and increases the bioavailability of choline in nervous tissue. sn-Glycero-3-phosphocholine (Choline Alfoscerate) has significant effects on cognitive function with a good safety profile and tolerability, and is effective in the treatment of Alzheimer's disease and dementia.
|
-
- HY-101315
-
|
AHN 1-055 hydrochloride
3α-Bis-(4-fluorophenyl) Methoxytropane hydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
AHN 1-055 hydrochloride is a dopamine uptake inhibitor, with an IC50 of 71 nM. AHN 1-055 hydrochloride binds with high affinity to the dopamine transporter (DAT) and may serve as leads for the development of agentia to treat cocaine abuse.
|
-
- HY-108697
-
|
PT2399
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
PT2399 is a potent and selective HIF-2α antagonist, which directly binds to HIF-2α PAS B domain with an IC50 of 6 nM. PT2399 displays potent antitumor activity in vivo.
|
-
- HY-128839
-
-
- HY-12407
-
|
ZK168281
|
VD/VDR
|
Metabolic Disease
|
|
ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor.
|
-
- HY-N0472
-
-
- HY-12050
-
|
CP-673451
|
PDGFR
|
Cancer
|
|
CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-U00460
-
-
- HY-16596
-
|
CNX-1351
|
PI3K
|
Cancer
|
|
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
|
-
- HY-100470
-
-
- HY-U00459A
-
-
- HY-U00125
-
-
- HY-15486
-
|
Salubrinal
|
Phosphatase
HSV
Autophagy
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
|
|
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
|
-
- HY-114454
-
|
INH14
|
IKK
|
Cancer
Inflammation/Immunology
|
|
INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity.
|
-
- HY-P1259
-
|
PR-39
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-120111A
-
|
MW-150 hydrochloride
MW01-18-150SRM hydrochloride
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Neurological Disease
|
|
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
|
-
- HY-128838
-
|
PROTAC ERRα Degrader-1
|
PROTAC
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα Degrader-1 comprises a MDM2 ligand binding group, a linker and an estrogen-related receptor alpha (ERRa) binding group. PROTAC ERRα Degrader-1 is an PROTAC estrogen-related receptor alpha (ERRa) degrader.
|
-
- HY-30216
-
-
- HY-N0613
-
|
Sauchinone
|
NF-κB
|
Inflammation/Immunology
|
|
Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
|
-
- HY-13076
-
|
CHIR-98014
|
GSK-3
|
Metabolic Disease
|
|
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
|
-
- HY-108606
-
|
PI-828
|
PI3K
Casein Kinase
|
Cancer
|
|
PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively.
|
-
- HY-120217
-
|
VH032
|
Ligand for E3 Ligase
|
Cancer
|
|
VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd
|
-
- HY-100689
-
|
Propyl pyrazole triol
PPT
|
Estrogen Receptor/ERR
|
Cancer
|
|
Propyl pyrazole triol (PPT) is a selective estrogen receptor alpha (ERα) agonist. The relative binding affinity of Propyl pyrazole triol for ERα (ERα: 49%) around 410 times higher compared with estrogen receptor beta (ERβ: 0.12%).
|
-
- HY-12152
-
|
PNU-120596
NSC 216666
|
nAChR
|
Inflammation/Immunology
Neurological Disease
|
|
PNU-120596 (NSC 216666) is a potent and selective α7 nAChR positive allosteric modulator (PMA) with an EC50 of 216 nM. PNU-120596 is inactive against α4β2, α3β4, and α9α10 nAChRs. PNU-120596 has the potential for psychiatric and neurological disorders research.
|
-
- HY-16196
-
|
ENMD-1198
IRC-110160
|
Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
|
-
- HY-P1259A
-
|
PR-39 TFA
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-15770
-
|
TR-14035
|
Integrin
|
Inflammation/Immunology
|
|
TR-14035 is a dual α4β7/α4β1 integrin antagonist, with IC50 s of 7 nM and 87 nM for α4β7 and α4β1, respectively. TR-14035 can be used for the research of inflammation and autoimmune disease.
|
-
- HY-112619
-
|
TES-991
|
Others
|
Metabolic Disease
|
|
TES-991 is a potent and selective human α‑Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.
|
-
- HY-N3962
-
-
- HY-16715
-
-
- HY-12019
-
|
SGX-523
|
c-Met/HGFR
|
Cancer
|
|
SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.
|
-
- HY-N3625
-
-
- HY-N0835
-
-
- HY-B1058
-
-
- HY-10626
-
|
T0901317
|
LXR
FXR
ROR
Apoptosis
|
Cancer
Metabolic Disease
Cardiovascular Disease
|
|
T0901317 is an orally active and highly selective LXR agonist with an EC50 of 20 nM for LXRα. T0901317 activates FXR with an EC50 of 5 μM. T0901317 is RORα and RORγ dual inverse agonist with Ki values of 132 nM and 51 nM, respectively. T0901317 induces apoptosis and inhibits the development of atherosclerosis in low-density lipoprotein (LDL) receptor-deficient mice.
|
-
- HY-17034
-
-
- HY-13228
-
-
- HY-B0371B
-
|
(R)-Terazosin
|
Adrenergic Receptor
|
Endocrinology
|
|
(R)-Terazosin is an active R-enantiomer of Terazosin. (R)-Terazosin is a potent α1-adrenoceptor antagonist with Ki values of 6.51 nM, 1.01 nM and 1.97 nM for α1a, α1b and α1d-adrenoceptor, respectively.
|
-
- HY-16134A
-
|
Celgosivir hydrochloride
MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride
|
Glucosidase
HCV
HIV
|
Infection
|
|
Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
|
-
- HY-16134
-
|
Celgosivir
MBI 3253; MDL 28574; MX3253
|
Glucosidase
HCV
HIV
|
Infection
|
|
Celgosivir (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
|
-
- HY-130499
-
|
ERRα Ligand-Linker Conjugates 1
|
Target Protein Ligand-Linker Conjugate
|
Cancer
|
|
ERRα Ligand-Linker Conjugates 1 incorporates a ligand for estrogen-related receptor alpha (ERRα), and a PROTAC linker, which recruit E3 ligases MDM2. ERRα Ligand-Linker Conjugates 1 can be used in the synthesis of a series of PROTACs, such as PROTAC ERRalpha Degrader-1 (HY-128838). PROTAC ERRalpha Degrader-1 is an ERRα degrader.
|
-
- HY-107395
-
-
- HY-13468
-
|
KW-2478
|
HSP
|
Cancer
|
|
KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
|
-
- HY-13535
-
|
ATN-161
|
Integrin
|
Cancer
|
|
ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
|
-
- HY-G0008
-
-
- HY-109190
-
|
Seralutinib
GB002; PK10571
|
PDGFR
|
Cardiovascular Disease
|
|
Seralutinib (GB002) is an inhaled PDGFRα and PDGFRβ inhibitor. Seralutinib (GB002) is used in the study for pulmonary arterial hypertension.
|
-
- HY-10822A
-
|
ONX 0801 trisodium
BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
|
Thymidylate Synthase
|
Cancer
|
|
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors.
|
-
- HY-13535A
-
-
- HY-101028
-
-
- HY-107489
-
|
RO 4938581
|
GABA Receptor
|
Neurological Disease
|
|
RO 4938581 is a potent and selective GABAA α5 inverse agonist, with a Ki of 4.6 nM for GABAA α5β3γ2a, and shows a lower affinity at α1β3γ2a, α2β3γ2a, α3β3γ2a (Ki, 174, 185, 80 nM, respectively); RO 4938581 is used in the research of cognitive dysfunction.
|
-
- HY-B0744C
-
|
L-Eflornithine
L-DFMO; L-RMI71782; L-α-difluoromethylornithine
|
Others
|
Cancer
|
|
L-Eflornithine (L-DFMO) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
|
-
- HY-135902
-
|
Synucleozid
NSC 377363
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
|
-
- HY-135902A
-
|
Synucleozid hydrochloride
NSC 377363 hydrochloride
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein (IC50=1.5 μM). Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease.
|
-
- HY-120111B
-
|
MW-150 dihydrochloride dihydrate
MW01-18-150SRM dihydrochloride dihydrate
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Neurological Disease
|
|
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia.
|
-
- HY-110261
-
|
GS143
|
IKK
E1/E2/E3 Enzyme
NF-κB
|
Inflammation/Immunology
|
|
GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
|
-
- HY-13241A
-
|
Ralimetinib
LY2228820
|
p38 MAPK
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
|
-
- HY-131305
-
|
HBDDE
|
PKC
Apoptosis
|
Neurological Disease
|
|
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis.
|
-
- HY-N1881
-
|
4',5-Dihydroxyflavone
|
Lipoxygenase
Glucosidase
|
Others
|
|
4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase. LOX-1 isshort for Lectin-like oxidized low-density lipoprotein receptor-1.
|
-
- HY-117082
-
|
UTL-5g
GBL-5g
|
TNF Receptor
|
Inflammation/Immunology
|
|
UTL-5g (GBL-5g), an anti-inflammatory TNF-α inhibitor, has chemoprotective and liver radioprotective effects. UTL-5g lowers hepatotoxicity, nephrotoxicity, and myelotoxicity induced by Cisplatin through TNF-α inhibition among other factors.
|
-
- HY-14282
-
|
Lanoconazole
|
Fungal
|
Infection
Inflammation/Immunology
|
|
Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
|
-
- HY-121638A
-
|
(5Z,2E)-CU-3
|
Apoptosis
|
Cancer
|
|
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
|
-
- HY-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-100370
-
|
MRK-016
|
GABA Receptor
|
Cancer
|
|
MRK-016 is a selective, orally bioavailable inverse agonist of GABAA α5 receptor, with an EC50 of 3 nM for GABAA α5, and Kis of 0.83, 0.85, 0.77 and 1.4 nM for human GABAA α1β3γ2, GABAA α2β3γ2, GABAA α3β3γ2, and GABAA α5β3γ2, respectively; MRK-016 also readily penetrates the CNS.
|
-
- HY-15845
-
|
STF-083010
|
IRE1
|
Cancer
|
|
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
|
-
- HY-112182
-
|
UM-164
DAS-DFGO-II
|
Src
p38 MAPK
Autophagy
|
Cancer
|
|
UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
|
-
- HY-15704
-
|
LH846
|
Casein Kinase
|
Cancer
|
|
LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
|
-
- HY-14622
-
|
Necrostatin 2
|
RIP kinase
|
Cancer
|
|
Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM.
Necrostatin 2 is also a RIPK1 inhibitor.
|
-
- HY-B0566
-
-
- HY-107381
-
-
- HY-N2332A
-
-
- HY-126351
-
|
PROTAC ERRα ligand 2
|
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ERRα ligand 2 is an estrogen-related receptor α (ERRα) inverse agonist with an IC50 of 5.67 nM. PROTAC ERRα ligand 2 (IC50=5.67 nM) displays a ~11-fold improved potency than XCT790 (IC50=61.3 nM).
|
-
- HY-N2022
-
|
Castanospermine
|
Glucosidase
|
Cancer
|
|
Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
|
-
- HY-135386
-
-
- HY-N0358
-
-
- HY-N1470
-
|
Plantagoside
|
Others
|
Metabolic Disease
|
|
Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM.
|
-
- HY-134334
-
-
- HY-N2059
-
|
Santalol
|
Others
|
Cancer
|
|
Santalol is a mixture of α and β-isomer santalol. α-santalol is isolated from sandalwood oil. α-santalol is a promising anti-cancer agent against cancers such as oral, breast, prostate and skin cancer.
|
-
- HY-14422
-
|
SR1078
|
ROR
|
Cancer
|
|
SR1078 is a selective agonist of retinoic acid receptor-related orphan receptor α/γ (RORα/RORγ). SR1078 directly binds to the ligand binding domain of RORα and RORγ and increases the transcriptional activity of these receptors, leading to stimulation of RORα/γ target gene transcription.
|
-
- 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-100339
-
|
GSK583
|
RIP kinase
|
Endocrinology
|
|
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
|
-
- HY-119424
-
-
- HY-108006
-
|
Mirogabalin besylate
DS 5565 besylate
|
Calcium Channel
|
Neurological Disease
|
|
Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
|
-
- HY-17034B
-
-
- HY-14652
-
-
- 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-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-101300
-
-
- HY-117147A
-
|
GSK2945 hydrochloride
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-111845
-
-
- HY-117147
-
|
GSK2945
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-124290
-
|
Carotegrast methyl
AJM300
|
Integrin
|
Inflammation/Immunology
|
Carotegrast methyl (AJM300) is an orally active and selective α4 integrin antagonist. HCA2969, an active metabolite of AJM300, is a specific, dual α4β1/α4β7 integrin antagonist. Carotegrast methyl prevents the development of colitis in mice.
|
-
- HY-N1425
-
|
Tiliroside
|
Others
|
Metabolic Disease
|
|
Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2 μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract.
|
-
- HY-15466
-
|
CH5132799
|
PI3K
|
Cancer
|
|
CH5132799 is a selective class I PI3K inhibitor. CH5132799 inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
|
-
- HY-12743A
-
-
- HY-129571
-
-
- HY-12030
-
|
PIK-90
|
PI3K
DNA-PK
|
Cancer
|
|
PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
|
-
- HY-13862
-
|
AZD1080
|
GSK-3
|
Neurological Disease
|
|
AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
|
-
- HY-12743
-
|
K-7174
|
Others
|
Inflammation/Immunology
|
|
K-7174 is a novel cell adhesion inhibitor; inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
|
-
- HY-15453
-
|
Devimistat
CPI-613
|
Apoptosis
|
Cancer
|
|
Devimistat (CPI-613) is a lipoic acid analog that inhibits pyruvate dehydrogenase (PDH) and α-ketoglutarate dehydrogenase, disrupts mitochondrial metabolism and shows strong antitumor activity.
|
-
- HY-10395
-
|
PD173955
|
Bcr-Abl
Src
Apoptosis
|
Cancer
|
|
PD173955 is src family-selective tyrosine kinase inhibitor with IC50 of ~22 nM for Src, Yes and Abl kinase; less potent for FGFRα and no activity on InsR and PKC.
|
-
- HY-102040
-
|
Hispidol
(Z)-Hispidol
|
TNF Receptor
|
Inflammation/Immunology
|
|
Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 µM.
|
-
- HY-111365
-
|
TES-1025
|
Others
|
Metabolic Disease
|
|
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM.
|
-
- HY-15846
-
-
- HY-122464
-
|
(±)-Jasmonic acid
|
Others
|
Others
|
|
(±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
|
-
- HY-10580
-
|
GSK 3 Inhibitor IX
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-103687
-
|
Abiraterone metabolite 1
3β-OH-5α-Abi
|
Drug Metabolite
|
Cancer
|
|
Abiraterone metabolite 1 is a 5β-reduced metabolite of abiraterone. Abiraterone, a steroidal drug, inhibits CYP17A1, blocks androgen synthesis and prolongs survival in prostate cancer.
|
-
- HY-N6630
-
-
- HY-B0659
-
-
- HY-15244A
-
|
Alpelisib hydrochloride
BYL-719 hydrochloride
|
PI3K
|
Cancer
|
|
Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. Alpelisib hydrochloride (BYL-719 hydrochloride) shows antineoplastic activity.
|
-
- HY-116830
-
|
BRD0705
|
GSK-3
|
Cancer
|
|
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research.
|
-
- HY-107531
-
|
A 1070722
|
GSK-3
|
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
|
-
- HY-14649
-
|
Retinoic acid
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-B0391A
-
|
Naftopidil dihydrochloride
KT-611 dihydrochloride; BM-15275 dihydrochloride
|
Adrenergic Receptor
|
Cancer
|
|
Naftopidil dihydrochloride (KT-611 dihydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil dihydrochloride has antiproliferative effects. Naftopidil dihydrochloride can be used for the research of prostate hyperplasia.
|
-
- HY-19505
-
|
TPA-023B
|
GABA Receptor
|
Neurological Disease
|
|
TPA-023B is a high-affinity and orally active GABAA receptor α2/α3 subtype (Kis of 0.73 nM/2 nM) partial agonist and a α1 subtype (Ki of 1.8 nM) antagonist. TPA-023B has non-sedating anxiolytic-like properties.
|
-
- HY-B0391B
-
|
Naftopidil hydrochloride
KT-611 hydrochloride; BM-15275 hydrochloride
|
Adrenergic Receptor
|
Cancer
|
|
Naftopidil hydrochloride (KT-611 hydrochloride) is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil hydrochloride has antiproliferative effects. Naftopidil hydrochloride can be used for the research of prostate hyperplasia.
|
-
- HY-B0391
-
|
Naftopidil
KT-611; BM-15275
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Naftopidil (KT-611) is is a selective alpha1-adrenoceptor antagonist, with Kis of 3.7 nM, 20 nM and 1.2 nM for the cloned human α1a-, α1b- and α1d-adrenoceptor subtypes, respectively. Naftopidil has antiproliferative effects. Naftopidil can be used for the research of prostate hyperplasia.
|
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-32015
-
|
Cot inhibitor-1
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
|
-
- HY-136207
-
|
TC-2559 difumarate
|
nAChR
|
Neurological Disease
|
|
TC-2559 idifumarate is a CNS-selective, orally active α4β2 subtype of nicotinic acetylcholine receptor (nAChR) partial agonist (EC50=0.18 μM). TC-2559 difumarate shows selectivity for α4β2 over α2β4, α4β4 and α3β4 receptors, with EC50s in the range of 10-30 µM. Antinociceptive effect.
|
-
- HY-12338
-
|
ON 146040
|
PI3K
Bcr-Abl
|
Cancer
|
|
ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
|
-
- HY-N7076
-
|
Aleuritic acid
(±)-erythro-Aleuritic acid; α-Aleuritic acid
|
Others
|
Others
|
|
Aleuritic acid ((±)-erythro-Aleuritic acid) is a major ingredient in shellac and used in the perfumery industry.
|
-
- HY-N0334
-
|
(+)-Magnoflorine
Magnoflorine; α-Magnoflorine; Thalictrine
|
Fungal
|
Infection
Metabolic Disease
|
|
(+)-Magnoflorine (Magnoflorine), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm. (+)-Magnoflorine has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-N0535
-
|
(+)-Magnoflorine chloride
Magnoflorine chloride; α-Magnoflorine chloride; Thalictrine chloride
|
Fungal
|
Infection
Metabolic Disease
|
|
Magnoflorine chloride (Magnoflorine chloride), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm. Magnoflorine chloride has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-32348
-
-
- HY-N4328
-
-
- HY-17571A
-
|
Oxytocin acetate
α-Hypophamine acetate; Oxytocic hormone acetate
|
Oxytocin Receptor
|
Endocrinology
|
|
Oxytocin acetate is a pleiotropic, hypothalamic peptide known for facilitating parturition, lactation, and prosocial behaviors. Oxytocin acetate can function as a stress-coping molecule with anti-inflammatory, antioxidant, and protective effects especially in the face of adversity or trauma.
|
-
- HY-N9315
-
-
- HY-111484A
-
|
GDC-0927 Racemate
SRN-927 Racemate
|
Estrogen Receptor/ERR
|
Cancer
|
|
GDC-0927 Racemate (SRN-927 Racemate) is a degrader of estrogen receptor, potently inhibits ER-α activity, with an IC50 of 0.2 nM, and is used in the research of ER-related diseases.
|
-
- HY-120215
-
|
KT203
|
MAGL
|
Metabolic Disease
|
|
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells.
|
-
- HY-120177
-
|
KT182
|
MAGL
|
Others
|
|
KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells.
|
-
- HY-N0694
-
|
Schisantherin A
Gomisin-C; Schizantherin-A; Wuweizi ester-A
|
NF-κB
|
Inflammation/Immunology
|
|
Schisantherin A is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
|
-
- HY-13743
-
|
Roquinimex
Linomide; FCF89; ABR212616
|
TNF Receptor
|
Inflammation/Immunology
|
|
Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.
|
-
- HY-103456
-
-
- HY-126052
-
|
Gnetol
|
COX
Tyrosinase
HDAC
|
Cancer
Metabolic Disease
|
|
Gnetol is a phenolic compound isolated from the root of Gnetum ula Brongn. Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities.
|
-
- HY-128598
-
|
MD2-TLR4-IN-1
|
Toll-like Receptor (TLR)
|
Cancer
Inflammation/Immunology
|
|
MD2-TLR4-IN-1 (compound 22m) is an inhibitor of myeloid differentiation protein 2/toll-like receptor 4 (MD2-TLR4) complex, inhibiting lipopolysaccharides (LPS)-induced expression of tumor necrosis factor alpha (TNF-α) and interleukin-6 (IL-6) in macrophages with IC50 values of 0.89 μM and 0.53 μM, respectively.
|
-
- HY-119940
-
|
MC180295
(rel)-MC180295
|
CDK
|
Cancer
|
|
MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect.
|
-
- HY-110392
-
|
CMP8
|
Estrogen Receptor/ERR
|
Cancer
|
|
CMP8, a selective ligand for estrogen receptor, binds to the mutant estrogen receptor ligand binding domain (ERLBD). CMP8 exhibits IC50 values of 29 nM , 41 nM, 1100 nM and 2200 nM for MGERα, MGRERα, hERα and hERβ, respectively.
|
-
- HY-15295
-
|
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-A0077
-
|
Perphenazine
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
|
-
- HY-125838
-
|
J30-8
|
JNK
|
Neurological Disease
|
|
J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases.
|
-
- HY-14282A
-
|
(Z)-Lanoconazole
|
Fungal
|
Infection
Inflammation/Immunology
|
|
(Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo. Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis.
|
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-109040
-
|
Quilseconazole
VT-1129
|
Fungal
Cytochrome P450
|
Infection
|
|
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes.
|
-
- HY-16988A
-
-
- HY-16989
-
|
SR9009
|
Autophagy
|
Cancer
|
|
SR9009 is a REV-ERBα/β agonist with IC50s of 670 nM and 800 nM for REV-ERBα and REV-ERBβ, respectively.
|
-
- HY-B0659A
-
-
- HY-16988
-
|
SR9011
|
Autophagy
|
Cancer
|
|
SR9011 is a REV-ERBα/β agonist with IC50s of 790 nM and 560 nM for REV-ERBα and REV-ERBβ, respectively.
|
-
- HY-13294
-
-
- HY-P9970
-
-
- HY-16995
-
-
- HY-P0082A
-
|
Glucagon (1-29), bovine, human, porcine hydrochloride
Porcine glucagon hydrochloride
|
Glucagon Receptor
|
Metabolic Disease
|
|
Glucagon (1-29), bovine, human, porcine hydrochloride is a peptide hormone, produced by pancreatic α-cells. Glucagon hydrochloride stimulates gluconeogenesis. Glucagon (1-29), bovine, human, porcine hydrochloride activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-75385
-
-
- HY-P0082
-
|
Glucagon (1-29), bovine, human, porcine
Porcine glucagon
|
Glucagon Receptor
|
Metabolic Disease
|
|
Glucagon (1-29), bovine, human, porcine is a peptide hormone, produced by pancreatic α-cells. Glucagon stimulates gluconeogenesis. Glucagon (1-29), bovine, human, porcine activates HNF4α and increases HNF4α phosphorylation.
|
-
- HY-128671
-
-
- HY-N0014
-
-
- HY-111630
-
|
PluriSIn #2
|
Topoisomerase
|
Cancer
|
|
PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs).
|
-
- HY-11105
-
|
Pilaralisib analogue
XL147 analogue
|
PI3K
Apoptosis
|
Cancer
|
|
Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
|
-
- HY-10215
-
|
Luminespib
VER-52296; AUY922; NVP-AUY922
|
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively.
|
-
- HY-12869
-
|
AZD-8835
|
PI3K
|
Cancer
|
|
AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
|
-
- HY-P2203
-
|
SAHM1
|
Notch
|
|
|
SAHM1 is a Notch pathway inhibitor. SAHM1 stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 targets the protein-protein interface and prevents Notch complex assembly.
|
-
- HY-117771
-
|
DO34
|
Others
|
Metabolic Disease
|
|
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
|
-
- HY-14316A
-
|
Tebanicline dihydrochloride
Ebanicline dihydrochloride; ABT-594 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM.
|
-
- HY-13689
-
|
Go 6983
Gö 6983; Goe 6983
|
PKC
|
Cancer
|
|
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
|
-
- HY-12340
-
|
ETP-46321
|
PI3K
|
Cancer
|
|
ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
|
-
- HY-12437
-
|
BDP5290
|
ROCK
|
Cancer
|
|
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
|
-
- HY-N7637
-
|
Tubuloside B
|
Apoptosis
|
Cancer
|
|
Tubuloside B, one of the phenylethanoids isolated from the stems of Cistanche salsa, inhibits TNFα-induced apoptosis. Tubuloside B possesses antioxidative effects.
|
-
- HY-B2006
-
|
Fenvalerate
|
Phosphatase
Bacterial
|
Infection
|
|
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide.
|
-
- HY-P2324
-
|
Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
Infection
|
|
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
|
-
- HY-U00068
-
-
- HY-112284
-
-
- HY-135590
-
-
- HY-135584
-
|
Raloxifene 6-Monomethyl Ether
|
Estrogen Receptor/ERR
|
|
|
Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6.
|
-
- HY-12085
-
-
- HY-121638
-
|
CU-3
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells.
|
-
- HY-U00165
-
-
- HY-75385A
-
-
- HY-N1987
-
|
Cucurbitacin IIb
|
Apoptosis
|
Inflammation/Immunology
|
|
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
|
-
- HY-101717
-
-
- HY-N2270
-
-
- HY-13469
-
|
Debio 0932
CUDC-305
|
HSP
|
Cancer
|
|
Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively.
|
-
- HY-118266
-
|
BTdCPU
|
Phosphatase
Apoptosis
|
Cancer
|
|
BTdCPU is a potent heme-regulated eIF2α kinase (HRI) activator. BTdCPU promotes eIF2α phosphorylation and induced apoptosis in resistant cell.
|
-
- HY-18719A
-
-
- HY-18719
-
-
- HY-111492
-
|
DIM-C-pPhOCH3
|
Others
|
Cancer
|
|
DIM-C-pPhOCH3 is a Nur77 agonist. Nerve growth factor-induced Bα (NGFI-Bα, Nur77) is an orphan nuclear receptor.
|
-
- HY-18862
-
|
PF-03715455
|
p38 MAPK
|
Inflammation/Immunology
|
|
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease).
|
-
- HY-101855
-
|
Anle138b
|
Amyloid-β
|
Neurological Disease
|
|
Anle138b, an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Anle138b strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Anle138b has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Anle138b blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology.
|
-
- HY-12397
-
|
ZK159222
|
VD/VDR
|
Endocrinology
|
|
ZK159222, a 25-carboxylic ester analogue of 1α,25-(OH)2D3, is a potent 1α,25-(OH)2D3 receptor (VDR) antagonist. The mechanism of ZK159222 antagonistic action is mediated by a lack of ligand-induced vitamin D receptor interaction with coactivators. ZK159222 has a partial agonistic character.
|
-
- HY-14564A
-
|
GTS-21 dihydrochloride
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
|
-
- HY-17444
-
|
Tesaglitazar
|
PPAR
|
Cancer
Metabolic Disease
|
|
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats.
|
-
- HY-16708A
-
|
ZLN024 hydrochloride
|
AMPK
|
Metabolic Disease
|
|
ZLN024 hydrochloride is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-16708
-
|
ZLN024
|
AMPK
|
Metabolic Disease
|
|
ZLN024 is an AMPK allosteric activator. ZLN024 directly activates recombinant AMPK α1β1γ1, AMPK α2β1γ1, AMPK α1β2γ1 and AMPK α2β2γ1 heterotrimer with EC50s of 0.42 µM, 0.95 µM, 1.1 µM and 0.13 µM, respectively.
|
-
- HY-108642
-
|
AMG-548
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
|
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-101438
-
-
- HY-12150
-
|
CCMI
|
nAChR
|
Neurological Disease
|
|
CCMI is a potent and selective α7 nAChR-positive allosteric modulator, does not bind to or activate α7 nAChRs via the orthosteric site, and causes significant positive modulation of agonist-induced currents at α7 nAChRs. CCMI has potential in CNS diseases with cognitive dysfunction.
|
-
- HY-134130
-
|
Integrin modulator 1
|
Integrin
|
Inflammation/Immunology
|
|
Integrin modulator 1 is a potent and selective α4β1 integrin agonist, with an IC50 of 9.8 nM for RGD-binding α4β1. Integrin modulator 1 increases cell adhesion mediated by α4β1 integrin, with an EC50 of 12.9 nM.
|
-
- HY-14414
-
|
GSK4112
SR6452
|
Autophagy
|
Metabolic Disease
|
|
GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.
|
-
- HY-N2024
-
-
- HY-15332
-
|
Alfacalcidol-D6
|
VD/VDR
|
Metabolic Disease
|
|
Alfacalcidol-D6, a deuterated Alfacalcidol (1-hydroxycholecalciferol; Alpha D3; 1.alpha.-Hydroxyvitamin D3), is a non-selective VDR activator medication.
|
-
- HY-10122
-
|
Silodosin
KAD 3213; KMD 3213
|
Adrenergic Receptor
|
Cancer
Endocrinology
|
|
Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH.
|
-
- HY-10683
-
|
PKI-402
|
PI3K
mTOR
|
Cancer
|
|
PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
- HY-16903
-
|
PKC-IN-1
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-100886
-
|
BAY1082439
|
PI3K
Apoptosis
|
Cancer
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.
|
-
- HY-136393
-
|
IKK-IN-4
|
IKK
|
Inflammation/Immunology
|
|
IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively.
|
-
- HY-10527
-
|
Telatinib
Bay 57-9352
|
c-Kit
PDGFR
VEGFR
|
Cancer
|
|
Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
|
-
- HY-10402
-
-
- HY-12299
-
|
WH-4-023
Dual LCK/SRC inhibitor
|
Src
|
Cancer
|
|
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
|
-
- HY-N1200
-
-
- HY-19708
-
-
- HY-10291
-
-
- HY-100315
-
-
- HY-101438A
-
-
- HY-15372
-
-
- HY-107385
-
-
- HY-100850
-
-
- HY-13740
-
-
- HY-106266
-
-
- HY-101106
-
|
AR7
|
RAR/RXR
|
Cancer
Neurological Disease
|
|
AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy.
|
-
- HY-13861
-
-
- HY-32338
-
|
Tacalcitol monohydrate
1,24(R)-Dihydroxyvitamin D3 monohydrate
|
VD/VDR
|
Metabolic Disease
|
|
Tacalcitol monohydrate (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) promotes normal bone development by regulating calcium.
|
-
- HY-32018
-
|
Cot inhibitor-2
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
|
-
- HY-10232
-
|
THIP
Gaboxadol
|
GABA Receptor
|
Neurological Disease
|
|
THIP (Gaboxadol) is a selective δ-aminobutyric acid type A receptor (δ-GABAAR) agonist, functionally selective GABAAR ligand, exhibits agonism at α4β1δ, α4β3δ and weak antagonism at αβγ and α4β2δ GABAARs.
|
-
- HY-114404
-
|
SJFα
|
PROTAC
p38 MAPK
Autophagy
|
Cancer
|
|
SJFα is a 13-atom linker PROTAC. SJFα degrades p38α with a DC50 of 7.16 nM, but is far less effective at degrading p38δ (DC50=299 nM) and does not degrade the other p38 isoforms (β and γ) at concentrations up to 2.5 µM.
|
-
- HY-14951
-
|
Firategrast
SB 683699
|
Integrin
|
Neurological Disease
|
|
Firategrast (SB 683699) is an orally active and specific α4β1/α4β7 integrin antagonist. Firategrast reduces trafficking of lymphocytes into the central nervous system (CNS) and decreases multiple sclerosis (MS) activity.
|
-
- HY-P1397
-
|
RVD-Hpα
|
Cannabinoid Receptor
|
|
|
RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).
|
-
- HY-112611
-
|
H3B-5942
|
Estrogen Receptor/ERR
|
Cancer
|
|
H3B-5942 is a selective, irreversible and orally active estrogen receptor covalent antagonist, inactivates both wild-type and mutant ERα by targeting Cys530, with Kis of 1 nM and 0.41 nM, respectively. H3B-5942 reduces ERα target gene GREB1, shows potent antitumor activity both in multiple cell lines or animals bearing ERα WT or ERα mutations.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-12774
-
-
- HY-13514
-
|
TG 100713
|
PI3K
|
Cancer
|
|
TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively.
|
-
- HY-10527C
-
|
Telatinib mesylate
Bay 57-9352 mesylate
|
VEGFR
PDGFR
c-Kit
|
Cancer
|
|
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively.
|
-
- HY-124646
-
|
KIRA-7
|
IRE1
|
Inflammation/Immunology
|
|
KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect.
|
-
- HY-13493
-
|
AC710
|
PDGFR
c-Kit
FLT3
|
Cancer
|
|
AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
|
-
- HY-17044
-
|
Duvelisib
IPI-145; INK1197
|
PI3K
|
Cancer
|
|
Duvelisib is a selectivite p100δ inhibitor with IC50 of 2.5 nM, 27.4 nM, 85 nM and 1602 nM for p110δ, P110γ, p110β and p110α, respectively.
|
-
- HY-15190
-
|
NVP-HSP990
HSP-990
|
HSP
Apoptosis
|
Cancer
|
|
NVP-HSP990 is a potent and selective Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
|
-
- HY-102076
-
|
0990CL
|
Others
|
Others
|
|
0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP.
|
-
- HY-13613
-
|
Dutasteride
GG 745; GI 198745
|
5 alpha Reductase
Apoptosis
|
Cancer
|
|
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT.
|
-
- HY-N1949
-
|
Homoplantaginin
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
|
-
- HY-107500
-
|
UVI 3003
|
RAR/RXR
Autophagy
|
Others
|
|
UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
|
-
- HY-13493A
-
|
AC710 Mesylate
|
PDGFR
|
Cancer
|
|
AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
|
-
- HY-120793
-
|
CMC2.24
TRB-N0224
|
Ras
Apoptosis
MMP
|
Cancer
Inflammation/Immunology
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis.
|
-
- HY-108642B
-
|
AMG-548 dihydrochloride
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM). AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε.
|
-
- HY-135680
-
|
I-OMe-Tyrphostin AG 538
I-OMe-AG 538
|
IGF-1R
|
Cancer
Metabolic Disease
|
|
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
|
-
- HY-10320
-
|
Doramapimod
BIRB 796
|
p38 MAPK
Raf
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM.
|
-
- HY-101690
-
-
- HY-N7439
-
|
Mogroside VI B
|
PGC-1α
|
Metabolic Disease
|
|
Mogroside VI B, a cucurbitane glucoside, separated from the crude extract of Siraitia grosvenorii. Mogroside VI B shows effect on activating PGC-1α transcription.
|
-
- HY-B0287
-
|
Clofibrate
|
PPAR
|
Metabolic Disease
|
|
Clofibrate is an agonist of PPAR, with EC50s of 50 μM, ∼500 μM for murine PPARα and PPARγ, and 55 μM, ∼500 μM for human PPARα and PPARγ, respectively.
|
-
- HY-10678
-
|
BMS-687453
|
PPAR
|
Cardiovascular Disease
|
|
BMS-687453 is a potent and selective PPARα agonist, with an EC50 and IC50 of 10 nM and 260 nM for human PPARα and 4100 nM and >15000 nM for PPARγ in PPAR-GAL4 transactivation assays.
|
-
- HY-107201
-
|
β-Cyclodextrin
|
Influenza Virus
|
Infection
|
|
β-Cyclodextrin is a cyclic polysaccharide composed of seven units of glucose (α-D-glucopyranose) linked by α-(1,4) type bonds. β-Cyclodextrin has often been used to enhance the solubility of drugs. β-Cyclodextrin has anti-influenza virus H1N1 activities.
|
-
- HY-120051
-
|
Afizagabar
S44819; Egis-13529
|
GABA Receptor
|
Neurological Disease
|
|
Afizagabar (S44819) is a first-in-class, competitive, and selective antagonist at the GABA-binding site of the α5-GABAAR, with an IC50 of 585 nM for α5β2γ2 and a Ki of 66 nM for α5β3γ2. Afizagabar enhances hippocampal synaptic plasticity and exhibits pro-cognitive efficacy.
|
-
- HY-13680
-
|
Meisoindigo
Dian III; N-Methylisoindigotin; Natura-α
|
Apoptosis
|
Cancer
|
|
Meisoindigo (Dian III), a derivative of Indirubin (HY-N0117), halts the cell cycle at the G0/G1 phase and induces apoptosis in primary acute myeloid leukemia (AML) cells. Meisoindigo exhibits high antitumor activity.
|
-
- HY-112542
-
|
Nemadectin
CL-287088; LL-F28249 α
|
Parasite
Antibiotic
|
Infection
|
|
Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity.
|
-
- HY-N1503
-
-
- HY-B0172
-
-
- HY-B0891
-
-
- HY-113079
-
-
- HY-U00110
-
-
- HY-U00123
-
-
- HY-17416A
-
-
- HY-13615A
-
|
EC-17 disodium salt
|
Others
|
Cancer
|
|
EC-17 (disodium salt) is a folate receptor alpha (FRα) targeting contrast agent with fluorescent properties in the visible light spectrum. The peak excitation and emission wavelengths of EC-17 are 470/520 nm.
|
-
- HY-50665
-
|
LY518674
LY-674
|
PPAR
|
Metabolic Disease
|
|
LY518674 is a potent, selective PPARα antagonist, with an EC50 of 42 nM for human PPARα. LY518674 reduces triglycerides in and increased HDL-C and is used for the treatment of atherosclerosis.
|
-
- HY-17416
-
-
- HY-101385
-
-
- HY-12560D
-
-
- HY-15174
-
|
Dactolisib Tosylate
BEZ235 Tosylate; NVP-BEZ 235 Tosylate
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
|
-
- HY-70013
-
|
Abiraterone
CB-7598
|
Cytochrome P450
|
Cancer
|
|
Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
|
-
- HY-12046
-
|
PIK-93
|
PI4K
PI3K
Virus Protease
|
Cancer
|
|
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
|
-
- 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-100398
-
|
PF-04979064
|
PI3K
mTOR
|
Cancer
|
|
PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
|
-
- HY-N7095
-
|
Ceftezole
CTZ
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
|
-
- HY-100207
-
|
CP21R7
CP21
|
GSK-3
|
Cancer
|
|
CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
|
-
- HY-15356
-
-
- HY-N7096
-
|
Ceftezole sodium
CTZ sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftezole sodium (CTZ sodium) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole sodium (CTZ sodium) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity.
|
-
- HY-B0089
-
|
Acarbose
BAY g 5421
|
Glucosidase
|
Metabolic Disease
|
|
Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin.
|
-
- HY-N4095
-
-
- HY-124876
-
|
SynuClean-D
SC-D
|
Others
|
Neurological Disease
|
|
SynuClean-D (SC-D) is an inhibitor of α-synuclein aggregation, disrupts mature amyloid fibrils, prevents fibril propagation, and abolishes the degeneration of dopaminergic neurons in an animal model of Parkinson’s disease.
|
-
- HY-14305A
-
-
- HY-10342
-
|
Enzastaurin
LY317615
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε.
|
-
- HY-136392
-
|
IKK-IN-3
|
IKK
|
Inflammation/Immunology
|
|
IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively.
|
-
- HY-13812
-
-
- HY-W009783
-
|
1-Deoxymannojirimycin hydrochloride
|
HIV
Influenza Virus
|
Infection
|
|
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.
|
-
- HY-11048
-
|
NS11394
|
GABA Receptor
|
Neurological Disease
|
|
NS11394 is an orally active and unique subtype-selective GABAA positive allosteric receptor (PAM), with a Ki of ~0.5 nM. NS11394 shows a selectivity profile in the order of GABAA-5 > α3 > α2 > α1-containing receptors. NS11394 has anxiolytic and anti-inflammatory properties.
|
-
- 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-112769
-
|
EX229
|
AMPK
|
Metabolic Disease
|
|
EX229, a Benzimidazole derivative, is a potent and allosteric activator of AMP-activated protein kinase (AMPK), with Kds of 0.06 μM, 0.06 μM and 0.51 μM for α1β1γ1, α2β1γ1 and α1β2γ1 in biolayer interferometry, respectively.
|
-
- HY-117388
-
|
THI0019
|
Integrin
|
Inflammation/Immunology
|
|
THI0019 is a potent integrin α4β1 (VLA-4) agonist with an EC50 range of 1-2 μM. THI0019 induces stem/progenitor cells adhesion. THI0019 also regulates adhesion mediated by α4β7, α5β1 and αLβ2.
|
-
- HY-107589A
-
|
BIO5192 hydrate
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-116830B
-
|
BRD5648
(R)-BRD0705
|
GSK-3
|
Cancer
|
|
BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML).
|
-
- HY-107589
-
|
BIO5192
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-N6649
-
|
Isotanshinone I
|
Glucosidase
|
Infection
|
|
Isotanshinone I has inhibitory activity against α-glucosidase and formation of AGE, with IC50s of 1.13 μM and 0.432 μM for α-glucosidase and AGE, respectively.
|
-
- HY-12151
-
|
NS 1738
NSC 213859
|
nAChR
|
Neurological Disease
|
|
NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
|
-
- HY-N6964
-
-
- HY-13982
-
|
JSH-23
|
NF-κB
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
|
-
- HY-W015445
-
|
SD-169
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation.
|
-
- HY-A0027
-
-
- HY-100255
-
-
- HY-W015608
-
-
- HY-P0224
-
-
- HY-135307
-
|
SSF-109
Huanjunzuo
|
Fungal
|
Infection
|
|
SSF-109 is a broad-spectrum fungicide which has protective activity against plant disease. SSF-109 inhibits the biosynthesis of ergosterol at the 14α-demethylation step in Botrytis cinerea.
|
-
- HY-B0661A
-
-
- HY-124108
-
|
Eicosatetraynoic acid
ETYA
|
COX
PPAR
|
Others
|
|
Eicosatetraynoic acid (ETYA) is a nonspecific inhibitor of cyclooxygenase and lipoxygenase (ID50=8 μM and 4 μM, respectively). Eicosatetraynoic acid (ETYA) activates PPARα and PPARγ chimeras at 10 µM.
|
-
- HY-19498
-
|
WAY-204688
SIM-688
|
NF-κB
|
Inflammation/Immunology
|
|
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.
|
-
- HY-100779
-
|
Rimacalib
SMP 114
|
CaMK
Autophagy
|
Metabolic Disease
|
|
Rimacalib (SMP 114) is a Ca 2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ.
|
-
- HY-N0042
-
-
- HY-15244
-
|
Alpelisib
BYL-719
|
PI3K
|
Cancer
|
|
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity.
|
-
- HY-123938
-
|
CYH33
|
PI3K
|
Cancer
|
|
CYH33 is an orally active, highly selective PI3Kα inhibitor with IC50s of 5.9 nM/598 nM/78.7 nM/225 nM against α/β/δ/γ isoform, respectively. CYH33 inhibits phosphorylation of Akt, ERK and induces significant G1 phase arrest in breast cancer cells and non-small cell lung cancer (NSCLC) cells. CYH33 has potent activity against solid tumors.
|
-
- HY-P2657
-
|
Verucopeptin
|
HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
|
Cancer
|
|
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
|
-
- HY-12707
-
-
- HY-P0097A
-
-
- HY-112197
-
-
- HY-14565
-
|
Pozanicline
ABT-089
|
nAChR
|
Neurological Disease
|
|
Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM.
Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
|
-
- HY-107684
-
|
3-Bromocytisine
3-Br-cytisine
|
nAChR
|
Neurological Disease
|
|
3-Bromocytisine (3-Br-cytisine) is a potent nACh receptors agonist, with IC50s are 0.28, 0.30 and 31.6 nM for hα4β4, hα4β2, and hα7-nACh, respectively. 3-Bromocytisine (3-Br-cytisine) shows different effects on high (HS) and low (LS) ACh sensitivity α4β2 nAChRs with EC50s are 8 and 50 nM, respectively.
|
-
- HY-P0154
-
|
Epsilon-V1-2
ε-V1-2; EAVSLKPT
|
PKC
|
Inflammation/Immunology
|
|
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC.
|
-
- HY-17406
-
|
Tolcapone
Ro 40-7592
|
COMT
Amyloid-β
|
Neurological Disease
|
|
Tolcapone (Ro 40-7592) is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-100544
-
|
FLLL32
|
STAT
JAK
Apoptosis
|
Cancer
|
|
FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells.
|
-
- HY-136055
-
-
- HY-11068
-
|
SB 239063
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD.
|
-
- HY-110282
-
|
S3QEL-2
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation.
|
-
- HY-B0135A
-
|
Furosemide sodium
|
NKCC
GABA Receptor
|
Cancer
Metabolic Disease
|
|
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-B0135
-
|
Furosemide
|
NKCC
GABA Receptor
|
Metabolic Disease
Cancer
|
|
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2. Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema.
|
-
- HY-N1098
-
|
Velutin
|
Others
|
Inflammation/Immunology
|
|
Velutin is an aglycone extracted from Korean Mistletoe, with inhibitory activity against melanin biosynthesis. Velutin reduces osteoclast differentiation and down-regulates HIF-1α through the NF-κB pathway.
|
-
- HY-117071
-
-
- HY-B0683
-
|
Limaprost
17α,20-dimethyl-δ2-PGE1; ONO1206; OP1206
|
PGE synthase
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Limaprost (OP1206) is a PGE1 analogue and a potent and orally active vasodilator. Limaprost increases blood flow and inhibits platelet aggregation. Limaprost can be used for pain relief, has antianginal effects, and has potential for ischaemic symptoms treatment.
|
-
- HY-N2110
-
|
Phellopterin
|
Others
|
Inflammation/Immunology
|
|
Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
|
-
- HY-N0906
-
-
- HY-N3431
-
-
- HY-13223
-
|
Crenolanib
CP-868596
|
FLT3
PDGFR
Autophagy
|
Cancer
|
|
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-12837
-
|
EN460
|
Others
|
Others
|
|
EN460 is a selective endoplasmic reticulum oxidation 1 (ERO1) inhibitor. EN460 (IC50 of 1.9 μM) interacts selectively with the reduced, active form of ERO1α and prevents its reoxidation.
|
-
- HY-B0089A
-
|
Acarbose sulfate
Bay-g 5421 sulfate
|
Glucosidase
|
Metabolic Disease
|
|
Acarbose (BAY g 5421) sulfate, antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose sulfate can potentiate the hypoglycemic effects of sulfonylureas or insulin.
|
-
- HY-P1453A
-
|
CMD178 TFA
|
STAT
|
Inflammation/Immunology
|
|
CMD178 (TFA) is a lead peptide that consistently reduces the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling. CMD178 (TFA) also is an inhibitor of STAT5 and inhibits Tregcells development.
|
-
- HY-N0191
-
-
- HY-121750
-
|
CCG-222740
|
Ras
ROCK
|
Cancer
|
|
CCG-222740 is an orally active and selective Rho/myocardin-related transcription factor (MRTF) pathway inhibitor. CCG-222740 is also a potent inhibitor of alpha-smooth muscle actin protein expression. CCG-222740 effectively reduces fibrosis in skin and blocks melanoma metastasis.
|
-
- HY-15271
-
|
WYE-687
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-B0475
-
-
- HY-P1847
-
|
IKKγ NBD Inhibitory Peptide
|
NF-κB
|
Cancer
|
|
IKKγ NBD Inhibitory Peptide is a NEMO-binding domain peptide (NBD peptide) corresponding to the NEMO amino-terminal alpha-helical region, which is shown to block TNF-alpha-induced NF-kB activation.
|
-
- HY-B0723
-
|
Ospemifene
FC-1271a
|
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
|
-
- HY-15746
-
-
- HY-10255AS
-
|
Sunitinib D10
SU 11248 D10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-B0661
-
-
- HY-122521
-
|
Sootepin D
|
NF-κB
|
Inflammation/Immunology
|
|
Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity.
|
-
- HY-10721
-
|
PF-AKT400
AKT protein kinase inhibitor
|
Akt
|
Cancer
|
|
PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC50=0.5 nM) than PKA (IC50=450 nM).
|
-
- HY-50094
-
|
Pictilisib
GDC-0941
|
PI3K
Autophagy
Apoptosis
|
Cancer
|
|
Pictilisib (GDC-0941) is a potent inhibitor of PI3Kα/δ with an IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
|
-
- HY-12036
-
|
GSK1059615
|
PI3K
mTOR
Apoptosis
|
Cancer
|
|
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
|
-
- HY-P1872
-
|
OV-1, sheep
|
Bacterial
|
Infection
|
|
OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa.
|
-
- HY-135808
-
|
BIZ 114
|
NF-κB
|
Inflammation/Immunology
|
|
BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases.
|
-
- HY-B0744D
-
|
L-Eflornithine monohydrochloride
L-DFMO monohydrochloride; ; L-RMI71782 monohydrochloride; L-α-difluoromethylornithine monohydrochloride
|
Others
|
Cancer
|
|
L-Eflornithine monohydrochloride (L-DFMO monohydrochloride) is an enantiomer of Eflornithine. L-Eflornithine is an irreversible ornithine decarboxylase (ODC) inhibitor with a KD of 1.3±0.3 µM, and a Kinact of 0.15±0.03 min -1.
|
-
- HY-P1420
-
|
TAT-cyclo-CLLFVY
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM.
|
-
- HY-12085S
-
-
- HY-N2350
-
|
Cynaropicrin
|
MMP
NF-κB
TNF Receptor
|
Cancer
|
|
Cynaropicrin is a sesquiterpene lactone which can inhibit tumor necrosis factor (TNF-α) release with IC50s of 8.24 and 3.18 μM for murine and human macrophage cells, respectively. Cynaropicrin also inhibits the increase of cartilage degradation factor (MMP13) and suppresses NF-κB signaling.
|
-
- HY-N1940
-
|
β-Anhydroicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
|
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties. β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats. β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression.
|
-
- HY-15682
-
|
TTNPB
Ro 13-7410; Arotinoid acid; AGN191183
|
RAR/RXR
Autophagy
Apoptosis
|
Cancer
|
|
TTNPB is a highly potent RAR agonist. Competitive binding assays using human RARs yield IC50s of α=5.1 nM, β= 4.5 nM, and γ=9.3 nM, respectively.
|
-
- HY-117516
-
|
SR10067
|
Others
|
Neurological Disease
|
|
SR10067 is a potent, selective and brain penetrant Rev-Erbα/β agonist, with IC50 values are 160 and 170 nM for Rev-Erbβ and Rev-Erbα, respectively. SR10067 has anxiolytic activity.
|
-
- HY-10912
-
|
Fexaramine
|
FXR
Autophagy
|
Others
|
|
Fexaramine is a potent and selective FXR agonist with an EC50 of 25 nM. Fexaramine has no activity against hRXRα, hPPARαγδ, mPXR, hPXR, hLXRα, hTRβ, hRARβ, mCAR, mERRγ, and hVDR receptors.
|
-
- 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-P1847A
-
-
- HY-16716
-
-
- HY-100273
-
-
- HY-W015326
-
-
- HY-A0066
-
-
- HY-101738A
-
-
- HY-112788
-
-
- HY-P1106
-
|
K41498
|
CRFR
|
Cardiovascular Disease
|
|
K41498 is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 can be used for hypotension study.
|
-
- HY-131972
-
|
PF-06843195
|
PI3K
|
Cancer
|
|
PF-06843195 is a highly selective PI3Kα inhibitor with an IC50 of 18 nM in Rat1 fibroblasts. The Kis of PF-06843195 for PI3Kα and PI3Kδ in biochemical kinase assay are less than 0.018 nM and 0.28 nM, respectively. PF-06843195 has great suppression of the PI3K/mTOR signaling pathway and durable antitumor efficacy.
|
-
- HY-114263
-
|
NXT629
|
PPAR
|
Cancer
|
|
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively. NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models.
|
-
- HY-N7088
-
|
Raffinose
Melitose
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Raffinose (Melitose), a non-digestible short-chain oligosaccharide, is a trisaccharide composed of galactose, glucose, and fructose and can be found in many plants. Raffinose (Melitose) can be hydrolyzed to D-galactose and sucrose by the enzyme α-galactosidase (α-GAL).
|
-
- HY-B1662
-
|
Hexestrol
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Hexestrol is a nonsteroidal synthetic estrogen, with a Ki of 0.06 and 0.06 nM for estrogen receptor alpha (ERα) and ERβ. Hexestrol can be used for the research of the diseases caused by estrogen deficiencym, and it also can increase the weight of cattle.
|
-
- HY-13225A
-
|
Rivanicline
RJR-2403; (E)-Metanicotine
|
nAChR
|
Neurological Disease
|
|
Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).
|
-
- HY-112100
-
|
PAC
|
Estrogen Receptor/ERR
PROTAC-linker Conjugate for PAC
|
Cancer
|
|
PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
|
-
- 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-110160
-
|
Pozanicline dihydrochloride
ABT-089 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
|
-
- HY-111052
-
|
AZD7325
|
GABA Receptor
Cytochrome P450
|
Inflammation/Immunology
Neurological Disease
|
|
AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes. AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro. AZD7325 has the potential for the investigation of anxiety and dravet syndrome. PAM: positive allosteric modulator.
|
-
- HY-N0722
-
-
- HY-15506
-
|
TAK-593
|
PDGFR
VEGFR
|
Cancer
|
|
TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
|
-
- HY-13049
-
|
Cediranib maleate
AZD-2171 maleate
|
VEGFR
Autophagy
PDGFR
|
Cancer
|
|
Cediranib maleate (AZD-2171 maleate) is a highly potent, orally available VEGFR inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-N2821
-
|
(+)-Afzelechin
|
Glucosidase
|
Metabolic Disease
|
|
(+)-Afzelechin, isolated from rhizomes of Bergenia ligulata, is an alpha-glucosidase activity inhibitor with an ID50 (50% inhibition dose) value of 0.13 mM. (+)-Afzelechin can delay the absorption of carbohydrates in food to suppress postprandial hyperglycemia and hyperinsulinemia.
|
-
- HY-B1076
-
-
- HY-P0197
-
-
- HY-10003
-
|
Alfacalcidol
1-hydroxycholecalciferol; 1.Alpha.-Hydroxyvitamin D3
|
VD/VDR
|
Metabolic Disease
|
|
Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.
|
-
- HY-P1545
-
-
- HY-N0164
-
|
Matrine
Matridin-15-one; Vegard; α-Matrine
|
Opioid Receptor
Autophagy
Mitophagy
Ferroptosis
|
Cancer
|
|
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist.
|
-
- HY-103213
-
-
- HY-12720A
-
|
Apraclonidine hydrochloride
ALO 2145
|
Others
|
Neurological Disease
|
|
Apraclonidine hydrochloride (ALO 2145), a selective α2 and weak α1 receptor agonist activity, effectively lowers intraocular pressure (IOP) in human eyes. Apraclonidine hydrochloride is a topical ophthalmic solution and has the ability to elevate the eye lid.
|
-
- HY-108847
-
|
Etanercept
|
TNF Receptor
|
Inflammation/Immunology
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
|
-
- HY-107597
-
|
SU3327
|
JNK
|
Metabolic Disease
Inflammation/Immunology
|
|
SU3327 is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. SU3327 also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. SU3327 shows less active against p38α and Akt kinase.
|
-
- HY-103489
-
|
PI-273
|
PI4K
Apoptosis
|
Cancer
|
|
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
|
-
- HY-100211
-
|
TAPI-2
TNF Protease Inhibitor 2
|
MMP
SARS-CoV
|
Cancer
|
|
TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP. TAPI-2 blocks the entry of infectious SARS-CoV.
|
-
- HY-W010041
-
|
Scyllo-Inositol
|
Amyloid-β
Endogenous Metabolite
|
Neurological Disease
|
|
Scyllo-Inositol, an amyloid inhibitor, potentialy inhibits α-synuclein aggregation. Scyllo-Inositol stabilizes a non-fibrillar non-toxic form of amyloid-β peptide (Aβ42) in vitro, reverses cognitive deficits, and reduces synaptic toxicity and lowers amyloid plaques in an Alzheimer's disease mouse model.
|
-
- HY-A0066A
-
-
- HY-12380
-
-
- HY-12380A
-
-
- HY-B0409A
-
-
- HY-U00404
-
-
- HY-114009
-
-
- HY-10205
-
|
Cediranib
AZD2171
|
VEGFR
Autophagy
PDGFR
|
Cancer
|
|
Cediranib (AZD2171) is a highly potent, orally available VEGFR tyrosine kinase inhibitor with IC50s of <1, <3, 5, 5, 36, 2 nM for Flt1, KDR, Flt4, PDGFRα, PDGFRβ, c-Kit, respectively.
|
-
- HY-126114
-
|
Lupeol acetate
|
Others
|
Inflammation/Immunology
|
|
Lupeol acetate, a derivative of Lupeol, suppresses the progression of rheumatoid arthritis (RA) by inhibiting the activation of macrophages and osteoclastogenesis through downregulations of TNF-α, IL-1β, MCP-1, COX-2, VEGF and granzyme B.
|
-
- HY-20180
-
|
Pictilisib dimethanesulfonate
GDC-0941 dimethanesulfonate; GDC-0941 2 MeSO3H salt
|
PI3K
Autophagy
Apoptosis
|
Cancer
|
|
Pictilisib dimethanesulfonate (GDC-0941 dimethanesulfonate) is a potent inhibitor of PI3Kα/δ with IC50 of 3 nM, with modest selectivity against p110β (11-fold) and p110γ (25-fold).
|
-
- HY-16782
-
|
Pexmetinib
ARRY-614
|
p38 MAPK
Autophagy
|
Cancer
|
|
Pexmetinib is a potent Tie-2 and p38 MAPK dual inhibitor, with IC50s of 1 nM, 35 nM and 26 nM for Tie-2, p38α and p38β, respectively, and can be used in the research of acute myeloid leukemia.
|
-
- HY-103040
-
|
Zuranolone
|
GABA Receptor
|
Neurological Disease
|
|
Zuranolone is an orally active and potent neuroactive steroid positive allosteric modulator of GABAA receptor, with EC50s of 296 and 163 nM for α1β2γ2 and α4β3δ GABAA receptors, respectively.
|
-
- HY-N2160
-
|
6‴-Feruloylspinosin
|
Others
|
Neurological Disease
|
|
6‴-Feruloylspinosin is a flavonoid isolated from seeds of Ziziphus jujuba. 6‴-Feruloylspinosin can across the blood-brain barrier and enhance the expression of GABAAα1, GABAAα5, and GABABR1 mRNA in rat hippocampal neurons.
|
-
- 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-12650
-
|
Mirogabalin
DS5565
|
Calcium Channel
|
Neurological Disease
|
|
Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
|
-
- HY-N6073
-
|
Soyasapogenol A
|
Apoptosis
|
Inflammation/Immunology
|
|
Soyasapogenol A, a triterpene compound, isolated from the roots of Abrus cantoniensis. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
|
-
- HY-B0032S
-
-
- HY-12047
-
|
Ponatinib
AP24534
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
|
Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
|
-
- HY-N7377
-
|
Butyl isobutyl phthalate
|
Glucosidase
|
Metabolic Disease
|
|
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment.
|
-
- HY-101457
-
|
JZP-430
|
MAGL
|
Metabolic Disease
|
|
JZP-430 is a potent, highly selective, irreversible inhibitor of α/β-hydrolase domain 6 (ABHD6) with an IC50 of 44 nM, exhibits ~230-fold selectivity over fatty acid amide hydrolase (FAAH) and lysosomal acid lipase (LAL).
|
-
- HY-100608
-
|
BMS453
BMS-189453
|
RAR/RXR
|
Cancer
|
|
BMS453 (BMS-189453), a synthetic retinoid, is a RARβ agonist and a RARα/RARγ antagonist. BMS453 inhibits breast cell growth predominantly through the induction of active TGFβ.
|
-
- HY-P1106A
-
|
K41498 TFA
|
CFTR
|
Cardiovascular Disease
|
|
K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF2α, CRF2β and CRF1 receptors respectively. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF2α- and hCRF2β-expressing cells. K41498 TFA can be used for hypotension study.
|
-
- HY-15310
-
|
Ivermectin
MK-933
|
Parasite
HIV
Mitophagy
HSV
SARS-CoV
Antibiotic
Autophagy
|
Infection
Cancer
|
|
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
|
-
- HY-Y0932
-
-
- 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-115038
-
-
- HY-B1108
-
-
- HY-12749
-
-
- HY-101683
-
-
- HY-B0006A
-
|
Carvedilol phosphate hemihydrate
BM 14190 phosphate hemihydrate
|
Adrenergic Receptor
Autophagy
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Carvedilol phosphate hemihydrate (BM 14190 phosphate hemihydrate) is a non-selective β/α-1 blocker. Carvedilol phosphate hemihydrate inhibits lipid peroxidation with an IC50 of 5 μM. Carvedilol phosphate hemihydrate is a multiple action antihypertensive agent with potential use in angina and congestive heart failure. Carvedilol phosphate hemihydrate is an autophagy inducer that inhibits the NLRP3 inflammasome.
|
-
- HY-D0162
-
|
Malachite green oxalate
|
IKK
NF-κB
Apoptosis
|
Cancer
|
|
Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
|
-
- HY-17514
-
|
Itraconazole
R51211
|
Fungal
Hedgehog
Cytochrome P450
Autophagy
Antibiotic
|
Infection
Cancer
|
|
Itraconazole (R51211) is a triazole antifungal agent and a potent and orally active Hedgehog (Hh) signaling pathway antagonist with an IC50 of ~800 nM. Itraconazole potently inhibits lanosterol 14α-demethylase (cytochrome P450 enzyme), thereby inhibits the oxidative conversion of lanosterol to ergosterol. Itraconazole has anticancer and antiangiogenic effects.
|
-
- HY-16579
-
|
Etifoxine hydrochloride
HOE 36-801 hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-108434
-
|
Ceapin-A7
|
Others
|
Metabolic Disease
Neurological Disease
|
|
Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings.
|
-
- HY-16579A
-
|
Etifoxine
HOE 36-801
|
GABA Receptor
|
Neurological Disease
|
|
Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents.
|
-
- HY-19411
-
|
SSR180711 hydrochloride
|
nAChR
|
Neurological Disease
|
|
SSR180711 hydrochloride is an orally active, selective and reversible α7 acetylcholine nicotinic receptor (n-AChRs) partial agonist. SSR180711 hydrochloride can act on rat α7 n-AChR (Ki=22 nM; IC50=30 nM) and human α7 n-AChR (Ki=14 nM; IC50=18 nM). SSR180711 hydrochloride increases glutamatergic neurotransmission, ACh release and long-term potentiation (LTP) in the hippocampus.
|
-
- HY-N6733
-
|
Aphidicolin
|
DNA/RNA Synthesis
HSV
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Aphidicolin is an inhibitor of DNA polymerase α and δ, prevents mitotic cell division by interfering with the activity of DNA polymerase.
Aphidicolin is an antibiotic produced by the mold Cephalosporium aphidicola. Aphidicolin is a potent inhibitor of cellular deoxyribonucleic acid synthesis and inhibits the growth of herpes simplex virus.
Aphidicolin potentiates apoptosis induced by arabinosyl nucleosides in a human promyelocytic leukemia cell line.
|
-
- HY-15271A
-
|
WYE-687 dihydrochloride
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 dihydrochloride is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 dihydrochloride concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-131081
-
|
γ-Amanitin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
γ-Amanitin an ADC cytotoxin and isolated from the mushroom. γ-Amanitin inhibits RNA polymerase II and disrupts synthesis of mRNA. γ-Amanitin shows similar effects to α-Amanitin and β-Amanitin.
|
-
- HY-N0604
-
-
- HY-N0029
-
|
Forsythoside B
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Forsythoside B is a phenylethanoid glycoside isolated from the leaves of Lamiophlomis rotata Kudo, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-124607
-
|
(R)-BRD3731
|
GSK-3
|
Neurological Disease
|
|
(R)-BRD3731 is a GSK3 inhibitor extracted from patent US20160375006A1, compound example 273, has IC50s of 1.05 and 6.7 μM for GSK3β and GSK3α, respectively.
|
-
- HY-14860A
-
-
- HY-14860
-
|
1-Deoxynojirimycin
Duvoglustat
|
Glucosidase
PI3K
|
Metabolic Disease
|
|
1-Deoxynojirimycin (Duvoglustat) is a potent and orally active α-glucosidase inhibitor. 1-Deoxynojirimycin suppresses postprandial blood glucose and is widely used for diabetes mellitus. 1-Deoxynojirimycin possesses antihyperglycemic, anti-obesity, and antiviral features.
|
-
- HY-101146
-
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-13225
-
|
Rivanicline oxalate
RJR-2403 oxalate; (E)-Metanicotine oxalate
|
nAChR
|
Neurological Disease
|
|
Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
|
-
- HY-B0637
-
|
Bezafibrate
BM15075
|
PPAR
|
Metabolic Disease
Cardiovascular Disease
|
|
Bezafibrate is an agonist of PPAR, with EC50s of 50 μM, 60 μM, 20 μM for human PPARα, PPARγ and PPARδ, and 90 μM, 55 μM, 110 μM for murine PPARα, PPARγ and PPARδ, respectively; Bezafibrate is used as an hypolipidemic agent.
|
-
- HY-13225B
-
|
Rivanicline hemioxalate
RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate
|
nAChR
|
Neurological Disease
|
|
Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
|
-
- HY-B0192A
-
-
- HY-B0192
-
-
- HY-12749A
-
-
- HY-12721
-
-
- HY-13421
-
-
- HY-B0769
-
-
- HY-126236
-
-
- HY-134333
-
|
ICCB280
|
Apoptosis
|
Cancer
|
|
ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc).
|
-
- HY-14190
-
|
Valategrast
R-411 free base
|
Integrin
|
Inflammation/Immunology
|
|
Valategrast (R-411 free base) is a potent and orally active integrin α4β1 (VLA-4) and α4β7 dual antagonist. Valategrast has the potential for Chronic obstructive pulmonary disease (COPD) and asthma treatment.
|
-
- HY-N5112B
-
|
β,β-Dimethylacrylshikonin
|
Others
|
Cancer
|
|
β,β-Dimethylacrylshikonin is a naphthoquinone derivative isolated from Arnebia nobilis, promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. Arnebin 1 has anti-tumor activity.
|
-
- HY-131997
-
|
2'MeO6MF
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
|
-
- 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-15509A
-
|
Semapimod tetrahydrochloride
CNI-1493; CPSI-2364 tetrahydrochloride
|
TNF Receptor
Interleukin Related
p38 MAPK
|
Inflammation/Immunology
|
|
Semapimod tetrahydrochloride (CNI-1493), an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod tetrahydrochloride inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod tetrahydrochloride inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod tetrahydrochloride has potential in a variety of inflammatory and autoimmune disorders.
|
-
- HY-P1189
-
|
Echistatin
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-B0006
-
-
- HY-108355
-
|
R59949
|
PKC
|
Cancer
|
|
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
|
-
- HY-17406S
-
|
Tolcapone D7
Ro 40-7592 D7
|
COMT
Amyloid-β
|
Neurological Disease
|
|
Tolcapone D7 (Ro 40-7592 D7) is a deuterium labeled Tolcapone. Tolcapone is a selective, potent and orally active COMT inhibitor. Tolcapone is also a potent inhibitor of α-syn and Aβ42 oligomerization and fibrillogenesis and protect against extracellular toxicity induced by the aggregation of both proteins in PC12 cells.
|
-
- HY-108264
-
|
TCS 21311
NIBR3049
|
JAK
PKC
GSK-3
|
Cancer
|
|
TCS 21311 (NIBR3049) is a potent, highly selective JAK3 inhibitor with an IC50 of 8 nM, it displays >100-fold selectivity over JAK1, JAK2 and TYK2. TCS 21311 (NIBR3049) inhibits PKCα, PKCθ, and GSK3β with IC50s of 13, 68, and 3 nM, respectively.
|
-
- HY-70063
-
|
Buparlisib
BKM120; NVP-BKM120
|
PI3K
Apoptosis
|
Cancer
|
|
Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
|
-
- HY-124607B
-
|
BRD3731
|
GSK-3
|
Metabolic Disease
Neurological Disease
|
|
BRD3731 is a selective GSK3β inhibitor, with IC50s of 15 nM and 215 nM for GSK3β and GSK3α, respectively. BRD3731 is potentail for the research of post-traumatic stress disorder (PTSD), psychiatric disorder, diabetes, and neurodegenerative disorders.
|
-
- HY-N0907
-
|
Ginsenoside Rg6
|
NF-κB
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Ginsenoside Rg6 is the component isolated from notoginseng. Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34±2.22 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
|
-
- HY-136198
-
|
SRX3207
|
Syk
PI3K
|
Cancer
|
|
SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.
|
-
- HY-13728
-
|
Plevitrexed
ZD 9331; BGC9331
|
Thymidylate Synthase
|
Cancer
|
|
Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical.
|
-
- HY-B0760
-
|
Fenofibric acid
FNF acid
|
PPAR
COX
|
Metabolic Disease
|
|
Fenofibric acid, an active metabolite of fenofibrate, is a PPAR activitor, with EC50s of 22.4 µM, 1.47 µM, and 1.06 µM for PPARα, PPARγ and PPARδ, respectively; Fenofibric acid also inhibits COX-2 enzyme activity, with an IC50 of 48 nM.
|
-
- HY-13894
-
|
Tyrphostin AG1296
AG1296
|
PDGFR
c-Kit
FLT3
Apoptosis
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Tyrphostin AG1296 is a potent and selective inhibitor of platelet-derived growth factor receptor (PDGFR), with an IC50 of 0.8 μM. Tyrphostin AG1296 inhibits signaling of human PDGF α- and β-receptors as well as of the related stem cell factor receptor (c-Kit). Tyrphostin AG1296 is also a potent inhibitor of FLT3, with an IC50 in the micromolar range.
|
-
- 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-136351
-
|
THZ-P1-2
|
Autophagy
|
Cancer
|
|
THZ-P1-2 is a first-in-class and selective PI5P4K inhibitor, with an IC50 of 190 nM for PI5P4Kα. THZ-P1-2 covalently targets cysteines on a disordered loop in PI5P4Kα/β/γ. THZ-P1-2 causes autophagy disruption and upregulates TFEB signaling. THZ-P1-2 displays anticancer activity in leukemia cell lines.
|
-
- HY-17034A
-
|
Dexmedetomidine hydrochloride
(+)-Medetomidine hydrochloride; (S)-Medetomidine hydrochloride
|
Adrenergic Receptor
|
Neurological Disease
Endocrinology
Cancer
|
|
Dexmedetomidine hydrochloride ((+)-Medetomidine hydrochloride) is a potent, selective and orally active agonist of α2-adrenoceptor, with a Ki of 1.08 nM. Dexmedetomidine hydrochloride shows 1620-fold selectivity against α1-adrenoceptor. Dexmedetomidine hydrochloride exhibits anxiolysis, sedation, and modest analgesia effects.
|
-
- HY-112813
-
|
TUG-1375
|
Others
|
Metabolic Disease
|
|
TUG-1375 is an agonist of free fatty acid receptor 2 (FFA2/GPR43), with a pKi of 6.69. TUG-1375 is inactive on FFA3, FFA4, PPARα, PPARγ, PPARδ, LXRα or LXRβ.
|
-
- HY-B0362A
-
|
Phentolamine mesylate
Phentolamine methanesulfonate
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction.
|
-
- HY-P1014
-
-
- HY-B1258
-
-
- HY-14590
-
-
- HY-12987
-
-
- HY-N7599
-
|
Chrysophanol triglucoside
|
Phosphatase
Glucosidase
|
Metabolic Disease
|
|
Chrysophanol triglucoside is an anthraquinone isolated from Cassia obtusifolia, inhibits protein tyrosine phosphatases 1B (PTP1B) and α-glucosidase with IC50s of 80.17 and 197.06 µM, respectively. Chrysophanol triglucoside has the potential for diabetes research.
|
-
- HY-15177
-
|
PF-04691502
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
PF-04691502 is a potent and selective inhibitor of PI3K and mTOR. PF-04691502 binds to human PI3Kα, β, δ, γ and mTOR with Kis of 1.8, 2.1, 1.6, 1.9 and 16 nM, respectively.
|
-
- HY-B0258
-
-
- HY-N1956
-
|
Rubiadin-1-methyl ether
|
NF-κB
|
Metabolic Disease
|
|
Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.
|
-
- HY-14415
-
|
SR8278
|
Others
|
Metabolic Disease
|
|
SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.
|
-
- HY-N6857
-
|
Armepavine
|
NF-κB
|
Inflammation/Immunology
|
|
Armepavine, an active compound from Nelumbo nucifera, exerts not only anti-inflammatory effects on human peripheral blood mononuclear cells, but also immunosuppressive effects on T lymphocytes and on lupus nephritic mice. Armepavine inhibits TNF-α-induced MAPK and NF-κB signaling cascades.
|
-
- HY-107542
-
-
- HY-19057A
-
-
- HY-B1435
-
-
- HY-B0716
-
-
- 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-108414
-
-
- HY-A0142A
-
-
- HY-12767
-
-
- HY-16737
-
-
- HY-B0061
-
|
Tandospirone citrate
SM-3997 citrate
|
5-HT Receptor
|
Neurological Disease
|
|
Tandospirone citrate is a potent and selective 5-HT1A receptor partial agonist (Ki = 27 nM) that displays selectivity over SR-2, SR-1C, α1, α2, D1 and D2 receptors (Ki values ranging from 1300-41000 nM).
|
-
- HY-10791
-
-
- 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-107427
-
|
PF-3644022
|
MAPKAPK2 (MK2)
p38 MAPK
|
Inflammation/Immunology
|
|
PF-3644022 is a potent, selective, orally active and ATP-competitive MAPKAPK2 (MK2) inhibitor with an IC50 of 5.2 nM and a Ki of 3 nM. PF-3644022 also inhibits MK3 and p38 regulated/activated kinase (PRAK) with IC50s of 53 nM and 5.0 nM, respectively. PF-3644022 potently inhibits TNFα production and has anti-inflammatory effect.
|
-
- HY-11109
-
-
- HY-12034
-
|
WYE-354
|
mTOR
Autophagy
Apoptosis
|
Cancer
|
|
WYE-354 is an ATP-competitive mTOR inhibitor with an IC50 of 5 nM. WYE-354 also inhibits PI3Kα and PI3Kγ with IC50s of 1.89 μM and 7.37 μM, respectively. WYE-354 inhibits both mTORC1 and mTORC2. WYE-354 induces autophagy activation in vitro.
|
-
- HY-130240
-
|
GCN2-IN-6
|
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
GCN2-IN-6 (Compound 6d) is a potent, and orally available GCN2 inhibitor confirmed by in-house enzymatic (IC50 of 1.8 nM) and cellular assays (IC50 of 9.3 nM). GCN2-IN-6 is also a eIF2α kinase PERK inhibitor with an IC50 of 0.26 nM (in enzymatic assay) and 230 nM (in cells).
|
-
- HY-19805
-
|
STO-609
|
CaMK
AMPK
Autophagy
|
Metabolic Disease
|
|
STO-609 is a selective and cell-permeable inhibitor of the Ca 2+/calmodulin-dependent protein kinase kinase (CaM-KK), with Ki values of 80 and 15 ng/mL for recombinant CaM-KKα and CaM-KKβ, respectively. STO-609 inhibits AMP-activated protein kinase kinase (AMPKK) activity in HeLa cell lysates with an IC50 ~0.02 g/ml.
|
-
- HY-P1189A
-
|
Echistatin TFA
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
|
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-111745
-
|
Tyk2-IN-5
|
JAK
|
Inflammation/Immunology
|
|
Tyk2-IN-5 (compound 6) is a highly potent, selective and orally active Tyk2 inhibitor and targets the JH2 domain, with a Ki of 0.086 nM for Tyk2 JH2 and an IC50 of 25 nM for IFNα. Highly effective in inhibiting IFNγ production in a rat pharmacodynamics model and fully efficacious in a rat adjuvant arthritis model.
|
-
- HY-B1367
-
|
Carbenoxolone disodium
|
Gap Junction Protein
|
Infection
Inflammation/Immunology
|
|
Carbenoxolone disodium is the active metabolite of Glycyrrhizic acid (HY-N0184) and the inhibitor of human 11β-HSD and bacterial 3α, 20β-HSD. Carbenoxolone disodium is an uncoupling agent for gap junctions and a potent inhibitor of Vaccinia virus replication. Carbenoxolone disodium is used for the study of peptic, esophageal and oral ulceration and inflammation.
|
-
- HY-N2574
-
|
Gitogenin
|
Glucosidase
|
Metabolic Disease
|
|
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms.
|
-
- HY-15785
-
|
TAS-116
|
HSP
|
Cancer
|
|
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
|
-
- HY-123037
-
|
Triadimefon
|
Fungal
|
Infection
|
|
Triadimefon is a triazole fungicide used to control powdery mildew, rusts, and other fungal pests on grains, fruit and vegetable crops, turf, shrubs, and trees. Triadimefon inhibits lanosterol 14α-demethylase, interfering with oxidative demethylation reactions in the ergosterol biosynthesis pathway of fungi, and also blocks gibberellin biosynthesis.
|
-
- HY-128579
-
|
DW14800
|
Histone Methyltransferase
|
Cancer
|
|
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
|
-
- HY-17547
-
|
NMS-E973
|
HSP
|
Cancer
|
|
NMS-E973 is a potent and selective inhibitor of HSP90. NMS-E973 binds to the ATP binding site of Hsp90α with a DC50 of <10 nM. NMS-E973 is able to cross the blood-brain barrier (BBB). Antitumor efficacy.
|
-
- HY-133680
-
|
β-Tocopherol
|
Tyrosinase
|
Metabolic Disease
|
|
β-Tocopherol is an analogue of vitamin E, exhibits antioxidant properties. β-Tocopherol can inhibit tyrosinase activity and melanin synthesis. β-Tocopherol also can prevent the inhibition of cell growth and of PKC activity caused by d-alpha-tocopherol.
|
-
- HY-13504
-
|
PIK-293
|
PI3K
|
Cancer
Metabolic Disease
|
|
PIK-293, an analog of IC87114, is a PI3K inhibitor, with IC50 values of 0.24 μM, 10 μM, 25 μM and 100 μM for p110δ, p110β, p110γ and p110α, respectively.
|
-
- HY-107222
-
|
Lysionotin
|
Others
|
Inflammation/Immunology
|
|
Lysionotin is a flavonoid isolated from few flower lysionotus herbs. Lysionotin efficiently inhibit α-Toxin (a pore-forming protein) expression and shows significant protection against S. aureus in vitro and in vivo. Lysionotin has the potential for the treatment of S. aureus induced pneumonia.
|
-
- HY-10343
-
|
Sotrastaurin
AEB071
|
PKC
|
Inflammation/Immunology
Cancer
|
|
Sotrastaurin (AEB071) is a potent and orally-active pan-PKC inhibitor, with Kis of 0.22 nM, 0.64 nM, 0.95 nM, 1.8 nM, 2.1 nM and 3.2 nM for PKCθ, PKCβ, PKCα, PKCη, PKCδ and PKCε, respectively.
|
-
- HY-10233
-
|
Gaboxadol hydrochloride
Lu 02-030 hydrochloride; THIP hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Gaboxadol hydrochloride (Lu 02-030 hydrochloride; THIP 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 analgesic and has hypnotic activities.
|
-
- HY-15430A
-
-
- HY-B0431A
-
-
- HY-107824
-
-
- HY-15430
-
-
- HY-108688
-
-
- HY-B0098
-
-
- HY-P0315
-
|
Crosstide
|
Akt
|
Others
|
|
Crosstide is a peptide analog of glycogen synthase kinase α/β fusion protein sequence which is a substrate for Akt.
|
-
- HY-B0098A
-
-
- HY-12715
-
-
- HY-136186
-
-
- HY-128527
-
|
PROTAC ER Degrader-3
|
PROTAC
Estrogen Receptor/ERR
|
Cancer
|
|
PROTAC ER Degrader-3 is an intermediate for synthesis of PAC. PAC, consists the ADCs linker and PROTACs, conjugated to an antibody. PAC extracts from patent WO2017201449A1, compound LP2. PAC conjugated to an antibody is a more marked estrogen receptor-alpha (ERα) degrader compared to PROTAC (without Ab).
|
-
- HY-P9923
-
|
Benralizumab
MEDI-563; BIW-8405
|
Interleukin Related
|
Inflammation/Immunology
|
|
Benralizumab (MEDI-563) is an interleukin-5 receptor α (IL-5Rα)-directed cytolytic monoclonal antibody that induces direct, rapid and nearly complete depletion of eosinophils via enhanced antibody-dependent cell-mediated cytotoxicity. Benralizumab can be used for severe eosinophilic asthma.
|
-
- HY-N1990
-
|
Gypenoside XLIX
|
PPAR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Gypenoside XLIX, a dammarane-type glycoside, is a prominent component of G. pentaphyllum. Gypenoside XLIX is a selective peroxisome proliferator-activated receptor (PPAR)-alpha activator and inhibits cytokine-induced vascular cell adhesion molecule-1 (VCAM-1) overexpression and hyperactivity in human endothelial cells.
|
-
- HY-120272
-
|
SMAP-2
DT-1154
|
Phosphatase
|
Cancer
|
|
SMAP-2 (DT-1154) is an orally bioavailable phosphatase 2A (PP2A) activator which binds to the PP2A Aα scaffold subunit to drive conformational changes in PP2A. SMAP-2 (DT-1154) inhibits the growth of KRAS-mutant lung cancers .
|
-
- HY-15245
-
|
GSK2636771
|
PI3K
|
Cancer
|
|
GSK2636771 is a potent, selective and orally bioavailable inhibitor of PI3Kβ with a Ki of 0.89 nM and an IC50 of 5.2 nM, showing 900-fold selectivity over p110α and p110γ, and 10-fold selectivity over p110δ isoforms.
|
-
- HY-101569
-
|
LXS196
|
PKC
|
Cancer
|
|
LXS196 is a potent, selective and orally active protein kinase C (PKC) inhibitor, with IC50 values of 1.9 nM, 0.4 nM and 3.1 μM for PKCα, PKCθ and GSK3β, respectively. LXS196 has the potential for uveal melanoma research.
|
-
- HY-125263
-
|
OP-1074
|
Estrogen Receptor/ERR
|
Cancer
|
|
OP-1074 is a pure antiestrogen and a selective ER degrader (PA-SERD), shows specific antiestrogenic activity for ERα and ERβ, inhibits 17β-estradiol (E2)-stimulated transcriptional activity with IC50 of 1.6 and 3.2 nM, respectively.
|
-
- HY-N0316
-
|
Mollugin
|
Others
|
Cancer
|
|
Mollugin is a major bioactive component isolated from Rubia cordifolia L.. Mollugin has an anti-cancer therapeutic effect by inhibiting TNF-α-induced NF-κB activation. Mollugin enhances the osteogenic action of BMP-2 via the p38-Smad signaling pathway .
|
-
- HY-121538
-
|
CUDA
|
Epoxide Hydrolase
PPAR
|
Cardiovascular Disease
|
|
CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
|
-
- HY-120877
-
|
MRT199665
|
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370.
|
-
- HY-10230
-
|
Midostaurin
PKC412; CGP 41251
|
PKC
|
Cancer
|
|
Midostaurin (PKC412; CGP 41251) is a multi-targeted protein kinase inhibitor which inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM.
|
-
- HY-12330
-
|
AZD8186
|
PI3K
|
Cancer
|
|
AZD8186 is a PI3K inhibitor, which potently inhibits PI3Kβ (IC50=4 nM) and PI3Kδ (IC5050=12 nM) with selectivity over PI3Kα (IC50=35 nM) and PI3Kγ (IC50=675 nM).
|
-
- HY-113756A
-
|
Latanoprost acid
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
Latanoprost acid, an analog of prostaglandin (PG) F2α, is an selective prostanoid receptor (FP) agonist that specifically activates the FP-PG receptor. Latanoprost acid inhibits RANKL-induced osteoclastgenesis and function by inhibiting ERK, AKT, JNK, and p38 cascade, following by the c-fos/NFATc1 pathway. Latanoprost acid is a medication which works to lower pressure inside the eyes.
|
-
- HY-13241
-
|
Ralimetinib dimesylate
LY2228820 dimesylate
|
p38 MAPK
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Ralimetinib dimesylate (LY2228820 dimesylate) is a selective, ATP-competitive inhibitor of p38 MAPK α/β with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38a MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc.
|
-
- HY-131707
-
|
LEO 39652
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) .
|
-
- HY-111442
-
|
GC 14
|
Others
|
Metabolic Disease
|
|
GC 14 is a selective thyroid hormone receptor antagonist, with IC50 values of 35 nM and 200 nM for hTRβ and hTRα, respectively.
|
-
- HY-N1411
-
-
- HY-B0193
-
-
- HY-B0577
-
-
- HY-B0193A
-
-
- HY-N1495
-
-
- HY-W009301
-
-
- HY-U00402
-
-
- HY-U00237
-
-
- HY-N0246
-
-
- HY-B0354A
-
-
- HY-10426
-
|
XCT790
|
Estrogen Receptor/ERR
Autophagy
|
Cancer
|
|
XCT-790 is a potent and selective inverse agonist for ERRα with an IC50 value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.
|
-
- HY-B0723S
-
|
Ospemifene D4
FC-1271a D4
|
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
|
-
- HY-111226
-
-
- HY-14940
-
|
Volinanserin
MDL100907; M 100907
|
5-HT Receptor
|
Neurological Disease
|
|
Volinanserin is a potent and selective antagonist of 5-HT2 receptor, with a Ki of 0.36 nM, and shows 300-fold selectivity for 5-HT2 receptor over 5-HT1c, alpha-1 and DA D2 receptors. Volinanserin has antipsychotic activity.
|
-
- 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-14650
-
|
DHEA
Prasterone; Dehydroisoandrosterone; Dehydroepiandrosterone
|
Androgen Receptor
Endogenous Metabolite
|
Endocrinology
Cancer
|
|
DHEA (Prasterone) is one of the most abundant steroid hormones. DHEA (Prasterone) mediates its action via multiple signaling pathways involving specific membrane receptors and via transformation into androgen and estrogen derivatives (e.g., androgens, estrogens, 7α and 7β DHEA, and 7α and 7β epiandrosterone derivatives) acting through their specific receptors.
|
-
- HY-13333
-
|
NVP-BAG956
BAG 956
|
PI3K
|
Cancer
|
|
NVP-BAG956 is an ATP-competitive PI3K inhibitor with IC50s of 34, 56, 112 and 444 nM for PI3Kδ, PI3Kα, PI3Kγ and PI3Kβ, respectively.
|
-
- HY-N6775
-
|
Sonolisib
PX-866
|
PI3K
|
Cancer
|
|
Sonolisib (PX-866), an improved Wortmannin analogue, is an oral, irreversible, and pan-isoform inhibitor of PI3K (IC50=0.1 nM (p110α), 1.0 nM (p120γ), 2.9 nM (p110δ)). Antitumor activity.
|
-
- HY-12185
-
-
- HY-120110
-
-
- HY-12235
-
|
PI-3065
|
PI3K
|
Inflammation/Immunology
Cancer
|
|
PI-3065 is a potent inhibitor of PI3K p110δ, with IC50 and Ki values of 5 nM and 1.5 nM, and exhibits less potent activity against p110α, p110β, p110γ with IC50s of 910, 600, >10000 nM.
|
-
- HY-10571A
-
|
Delavirdine mesylate
U 90152 mesylate; BHAP-U 90152 mesylate
|
HIV
Reverse Transcriptase
|
Infection
|
|
Delavirdine (U 90152) mesylate is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine mesylate selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine mesylate is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
|
-
- HY-13335
-
|
PKCβ inhibitor 1
|
PKC
Apoptosis
|
Cancer
|
|
PKCβ inhibitor 1 is a potent, ATP-competitive, and selective PKCβ inhibitor with IC50s of 21 and 5 nM for human PKCβ1 and PKCβ2, respectively. PKCβ inhibitor 1 exhibits selectivity of more than 60-fold in favor of PKCβ2 relative to other PKC isozymes (PKCα, PKCγ, and PKCε).
|
-
- HY-107390A
-
|
AX-024 hydrochloride
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
AX-024 hydrochloride is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 hydrochloride modulates cell signaling by targeting SH3 domains. AX-024 hydrochloride has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-10571
-
|
Delavirdine
U 90152; BHAP-U 90152
|
HIV
Reverse Transcriptase
|
Infection
|
|
Delavirdine (U 90152) is a potent, highly specific and orally active non-nucleoside reverse transcriptase inhibitor (NNRTI). Delavirdine selectively inhibits HIV-1 reverse transcriptase (RT) (IC50=0.26 μM) over DNA polymerase α (IC50=440 μM) and polymerase δ (IC50>550 μM). Delavirdine is an inhibitor of HIV-1 replication and can can be used for the study of AIDs.
|
-
- HY-107390
-
|
AX-024
|
TNF Receptor
Interleukin Related
IFNAR
|
Inflammation/Immunology
|
|
AX-024 is an orally available, first-in-class inhibitor of the TCR-Nck interaction that selectively inhibits TCR-triggered T cell activation with an IC50 ~1 nM. AX-024 modulates cell signaling by targeting SH3 domains. AX-024 has low-acute toxicity and high potency and selectivity, and strongly inhibit the production of IL-6, TNF-α, IFN-γ, IL-10 and IL-17A.
|
-
- HY-107139
-
|
JNJ-10229570
|
Melanocortin Receptor
|
Endocrinology
|
|
JNJ-10229570 is an antagonist of melanocortin receptor 1 (MC1R) and melanocortin receptor 5 (MC5R), which inhibits sebaceous gland differentiation and the production of sebum-specific lipids. JNJ-10229570 inhibits the binding of 125I-NDP-α-MSH to cells expressing human MC1R and MC5R, with IC50 values of 270 nM and 200 nM, respectively.
|
-
- 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-18285
-
|
Longdaysin
|
Casein Kinase
ERK
CDK
|
Cancer
|
|
Longdaysin is a inhibitor of the Wnt/β-catenin signaling pathway, which exerts antitumor effect through blocking CK1δ/ε-dependent Wnt signaling. Longdaysin inhibits CK1α, CK1δ, CDK7, and ERK2 with IC50s of 5.6 µM, 8.8 µM, 29 µM, and 52 µM, respectively.
|
-
- HY-B0986
-
|
Hexylresorcinol
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
|
Cancer
Infection
Metabolic Disease
|
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
|
-
- HY-112613
-
|
UCB9608
|
PI4K
|
Inflammation/Immunology
|
|
UCB9608 is a potent, selective and orally active PI4KIIIβ inhibitor, with an IC50 of 11 nM, selective over PI3KC2 α, β, and γ lipid kinases. UCB9608 improves metabolic stability and exhibits excellent pharmacokinetic profile, acts as a potent immunosuppressive agent.
|
-
- HY-107365
-
|
PQR530
|
PI3K
mTOR
|
Cancer
|
|
PQR530 is a potent, ATP-competitive, orally bioavailable and brain-penetrant dual pan-PI3K/mTORC1/2 inhibitor, with a subnanomolar Kd toward PI3Kα and mTOR (0.84 and 0.33 nM, respectively). Antitumor activity.
|
-
- HY-N0041
-
|
Ginsenoside Rb3
Gypenoside IV
|
NF-κB
COX
NO Synthase
|
Cancer
Inflammation/Immunology
|
|
Ginsenoside Rb3 is extracted from steamed Panax notoginseng. Ginsenoside Rb3 exhibits inhibitory effect on TNFα-induced NF-κB transcriptional activity with an IC50 of 8.2 μM in 293T cell lines. Ginsenoside Rb3 also inhibits the induction of COX-2 and iNOS mRNA.
|
-
- HY-N0633
-
-
- HY-123984
-
|
LTβR-IN-1
|
Others
|
Metabolic Disease
|
|
LTβR-IN-1 is a potent, selective lymphotoxin β receptor (LTβR) inhibitor with an IC50 of 10 μM. LTβR-IN-1 is potent in TWEAK-stimulated p52 translocation assays with an IC50 of 10 μM and did not alter TNF-α–induced p65 nuclear translocation.
|
-
- HY-19717
-
|
DCVC
S-[(1E)-1,2-dichloroethenyl]--L-cysteine
|
TNF Receptor
|
Inflammation/Immunology
|
|
DCVC (S-[(1E)-1,2-dichloroethenyl]--L-cysteine) is a bioactive metabolite of trichloroethylene (TCE). DCVC inhibits pathogen-stimulated pro-inflammatory cytokines IL-1β, IL-8, and TNF-α release from tissue cultures.
|
-
- HY-12047S
-
|
Ponatinib D8
AP24534 D8
|
Bcr-Abl
PDGFR
VEGFR
FGFR
Src
Autophagy
|
Cancer
|
|
Ponatinib D8 (AP24534 D8) is a deuterium labeled Ponatinib. Ponatinib (AP24534) is an orally active multi-targeted kinase inhibitor with IC50s of 0.37 nM, 1.1 nM, 1.5 nM, 2.2 nM, and 5.4 nM for Abl, PDGFRα, VEGFR2, FGFR1, and Src, respectively.
|
-
- HY-19306
-
|
SB-267268
|
Integrin
|
Cancer
|
|
SB-267268 is a selective and nonpeptidic alpha(v)beta3 (αvβ3) and alpha(v)beta5 (αvβ5) integrins antagonist, with Kis of 0.9, 0.5 and 0.7 nM for human αvβ3, monkey αvβ3 and human αvβ5, respectively. SB-267268 inhibits human and mouse αvβ3 with IC50s of 0.68 and 0.29 nM, respectively. SB-267268 reduces angiogenesis and VEGF expression.
|
-
- HY-100513A
-
|
Dehydroaltenusin
|
Apoptosis
DNA/RNA Synthesis
Antibiotic
|
Cancer
|
|
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 µM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 µM). Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis. Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo.
|
-
- HY-N0515
-
|
Ophiopogonin D
|
PPAR
NF-κB
Calcium Channel
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
|
-
- HY-112461A
-
|
NF449 octasodium
|
P2X Receptor
|
Cardiovascular Disease
|
|
NF449 octasodium is a highly potent P2X1 receptor antagonist, with IC50s of 0.28, 0.69, and 120 nM for rP2X1, rP2X1+5, P2X2+3, respectively. NF449 octasodium is a Gsα-selective G Protein antagonist. NF449 octasodium suppresses the rate of GTP[γS] binding to Gsα-s, inhibits the stimulation of adenylyl cyclase activity, and blocks the coupling of β-adrenergic receptors to Gs.
|
-
- HY-B2236
-
|
DL-Lysine
(±)-2,6-Diaminocaproic acid
|
Others
|
Metabolic Disease
|
|
DL-Lysine is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
|
-
- HY-107675
-
-
- HY-B1948
-
|
Diniconazole
Rac-diniconazole
|
Bacterial
|
Infection
|
|
Diniconazole is a newly developed fungicide strongly inhibited lanosterol 14 alpha-demethylation catalyzed by a yeast cytochrome P-450.
|
-
- HY-B0459
-
-
- HY-N4258
-
-
- HY-100217
-
|
DL-3-Indolylglycine
|
Others
|
Others
|
|
DL-3-Indolylglycine is an unnatural amino acid that is very similar to Tryptophan, with the indole moiety directly attached to the α-position.
|
-
- HY-101649
-
-
- HY-W009417
-
-
- HY-P2267
-
|
LDV
|
Integrin
|
|
|
LDV, a non-fluorescent derivative of LDV FITC, is a α4β1 integrin (VLA-4) ligand (Kd ~ 12 nM).
|
-
- HY-B2236A
-
|
DL-Lysine monohydrate
(±)-2,6-Diaminocaproic acid monohydrate
|
Others
|
Metabolic Disease
|
|
DL-Lysine monohydrate is a racemic mixture of the D-Lysine and L-Lysine. Lysine is an α-amino acid that is used in the biosynthesis of proteins.
|
-
- HY-U00250
-
-
- HY-14426
-
-
- HY-19872
-
-
- HY-B0413S
-
|
Fenbendazole-d3
|
Parasite
HIF/HIF Prolyl-Hydroxylase
Antibiotic
|
Infection
|
|
Fenbendazole-d3 is a deuterium labeled Fenbendazole. Fenbendazole is a benzimidazole anthelmintic. Fenbendazole is active against Giardia in vitro (IC50 = 0.3 μM). Fenbendazole (20 mg/kg) prevents infiltration of parasites into the brain in a rabbit model of E. cuniculi infection. Fenbendazole also activates HIF-1α and prevents oxidative stress-induced death in primary neurons in vitro.
|
-
- HY-136187
-
-
- HY-107670
-
|
Dihydro-β-erythroidine hydrobromide
DHβE hydrobromide
|
nAChR
|
Neurological Disease
|
|
Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities.
|
-
- HY-108057A
-
|
Facinicline hydrochloride
RG3487 hydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM.
|
-
- HY-A0019
-
|
Paliperidone
9-Hydroxyrisperidone
|
Dopamine Receptor
5-HT Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
Paliperidone (9-Hydroxyrisperidone), the major active metabolite of Risperidone, is a dopamine D2 antagonist and 5-HT2A antagonist. Paliperidone is also active as an antagonist at α1 and α2 adrenergic receptors and H1-histaminergic receptors. Paliperidone, a antipsychotic agent, shows efficacy against schizophrenia.
|
-
- HY-P1545A
-
-
- HY-B1142
-
|
Lipoamide
(±)-α-Lipoamide; DL-Lipoamide; DL-6,8-Thioctamide
|
Endogenous Metabolite
|
Others
|
|
Lipoamide is a coenzyme, which transfer acetyl and hydrogen in Pyruvate deacylation oxidation Process, used for pharmaceuticals.
|
-
- HY-N3018
-
|
Isomaltose
6-O-α-D-Glucopyranosyl-D-glucose; D-Isomaltose
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Isomaltose is composed of two glucose units and suitable as a non-cariogenic sucrose replacement and is favorable in products for diabetics and prediabetic dispositions.
|
-
- HY-N0334A
-
|
(+)-Magnoflorine iodide
Magnoflorine iodide; α-Magnoflorine iodide; Thalictrine iodide
|
Fungal
|
Infection
Metabolic Disease
|
|
(+)-Magnoflorine iodide (Magnoflorine iodide), an aporphine alkaloid found in Acoruscalamus, reduces the formation of C. albicans biofilm. (+)-Magnoflorine iodide has anti-fungal, anti-antidiabetic and anti-oxidative activity.
|
-
- HY-N0783
-
-
- HY-W001692
-
-
- HY-N2156
-
-
- HY-B0513
-
-
- HY-A0275
-
-
- HY-103683
-
-
- HY-10629
-
-
- HY-16685
-
-
- HY-U00371
-
-
- HY-101953
-
-
- HY-B0528A
-
|
Octopamine hydrochloride
(±)-p-Octopamine hydrochlorid
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
|
|
Octopamine ((±)-p-Octopamine) hydrochloride, a biogenic monoamine structurally related to noradrenaline, acts as a neurohormone, a neuromodulator and a neurotransmitter in invertebrates. Octopamine hydrochloride can stimulate alpha2-adrenoceptors (ARs) in Chinese hamster ovary cells transfected with human alpha2-ARs. Octopamine hydrochloride increased glycogenolysis, glycolysis, oxygen uptake, gluconeogenesis and the portal perfusion pressure.
|
-
- HY-N2587
-
|
Irigenin
|
Integrin
|
Cancer
|
|
Irigenin is a is a lead compound, and mediates its anti-metastatic effect by specifically and selectively blocking α9β1 and α4β1 integrins binding sites on C-C loop of Extra Domain A (EDA). Irigenin shows anti-cancer properties. It sensitizes TRAIL-induced apoptosis via enhancing pro-apoptotic molecules in gastric cancer cells.
|
-
- HY-101489A
-
|
GZD856 formic
|
PDGFR
Bcr-Abl
Apoptosis
|
Cancer
|
|
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
|
-
- HY-101489
-
|
GZD856
|
PDGFR
Bcr-Abl
Apoptosis
|
Cancer
|
|
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
|
-
- HY-18766
-
|
EW-7195
|
TGF-β Receptor
p38 MAPK
|
Cancer
|
|
EW-7195 is a potent and selective ALK5 (TGFβR1) inhibitor with an IC50 of 4.83 nM. EW-7195 has >300-fold selectivity for ALK5 over p38α. EW-7195 efficiently inhibits TGF-β1-induced Smad signaling, epithelial-to-mesenchymal transition (EMT) and breast tumour metastasis to the lung.
|
-
- HY-10204
-
|
OSI-930
|
c-Kit
VEGFR
c-Fms
Apoptosis
|
Cancer
|
|
OSI-930 is an orally selective inhibitor of Kit, KDR and CSF-1R (c-Fms) with IC50s of 80 nM, 9 nM and 15 nM, respectively. OSI-930 also moderately inhibits Flt-1, c-Raf, Lck and low activity against PDGFRα/β, Flt-3 and Abl. OSI-930 has antitumor activity.
|
-
- HY-18303
-
|
AMG-47a
|
Src
VEGFR
p38 MAPK
JAK
|
Inflammation/Immunology
|
|
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
|
-
- HY-10681
-
|
Gedatolisib
PKI-587; PF-05212384
|
PI3K
mTOR
|
Cancer
|
|
Gedatolisib (PKI-587) is a highly potent dual inhibitor of PI3Kα, PI3Kγ, and mTOR with IC50s of 0.4 nM, 5.4 nM and 1.6 nM, respectively. Gedatolisib is equally effective in both complexes of mTOR, mTORC1 and mTORC2.
|
-
- HY-107526
-
|
NFPS
|
GlyT
|
Neurological Disease
|
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively. NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion.
|
-
- HY-10406
-
|
Talmapimod
SCIO-469
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
|
-
- HY-B0062
-
|
Dovitinib lactate hydrate
TKI258 lactate hydrate; CHIR-258 lactate hydrate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib lactate hydrate (TKI258 lactate hydrate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
|
-
- HY-10207
-
|
Dovitinib lactate
CHIR-258 lactate; TKI-258 lactate
|
FLT3
c-Kit
FGFR
VEGFR
PDGFR
|
Cancer
|
|
Dovitinib lactate (TKI258 lactate) is a multi-targeted tyrosine kinase inhibitor with IC50s of 1, 2, 8/9, 10/13/8, 27/210 nM for FLT3, c-Kit, FGFR1/3, VEGFR1/2/3 and PDGFRα/β, respectively.
|
-
- HY-126307
-
|
Urolithin B
|
NF-κB
JNK
ERK
Akt
AMPK
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
|
-
- HY-10406A
-
|
Talmapimod hydrochloride
SCIO-469 hydrochloride
|
p38 MAPK
|
Cancer
|
|
Talmapimod (SCIO-469) hydrochloride is an orally active, selective, and ATP-competitive p38α inhibitor with an IC50 of 9 nM. Talmapimod hydrochloride shows about 10-fold selectivity over p38β, and at least 2000-fold selectivity over a panel of 20 other kinases, including other MAPKs.
|
-
- HY-15180
-
|
Buparlisib Hydrochloride
BKM120 Hydrochloride; NVP-BKM120 Hydrochloride
|
PI3K
Apoptosis
|
Cancer
|
|
Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
|
-
- HY-101755
-
-
- HY-16526
-
|
Pilaralisib
XL-147; SAR245408
|
PI3K
|
Cancer
|
|
Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
|
-
- HY-50904
-
|
Nintedanib
BIBF 1120
|
PDGFR
VEGFR
FGFR
|
Cancer
|
|
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-124760
-
|
hSMG-1 inhibitor 11e
|
mTOR
PI3K
CDK
|
Cancer
|
|
hSMG-1 inhibitor 11e is a potent and selective hSMG-1 kinase inhibitor with an IC50 of <0.05 nM. hSMG-1 inhibitor 11e shows >900-fold selectivity over mTOR (IC50 of 45 nM), PI3Kα/γ (IC50s of 61 nM and 92 nM) and CDK1/CDK2 (IC50s of 32 μM and 7.1 μM).
|
-
- HY-114414
-
|
HDACs/mTOR Inhibitor 1
|
HDAC
mTOR
Apoptosis
|
Cancer
|
|
HDACs/mTOR Inhibitor 1 is a dual Histone Deacetylases (HDACs) and mammalian target of Rapamycin (mTOR) target inhibitor for treating hematologic malignancies, with IC50s of 0.19 nM, 1.8 nM, 1.2 nM and >500 nM for HDAC1, HDAC6, mTOR and PI3Kα, respectively. HDACs/mTOR Inhibitor 1 stimulates cell cycle arrest in G0/G1 phase and induce tumor cell apoptosis with low toxicity in vivo.
|
-
- HY-N1919
-
|
Ajmalicine
Raubasine
|
Adrenergic Receptor
AChE
|
Cardiovascular Disease
Endocrinology
|
|
Ajmalicine (Raubasine) is found in herbs of Catharanthus roseus, is an antihypertensive drug used in the treatment of high blood pressure, decreases peripheral resistance and blood pressure.
Ajmalicine (Raubasine) is an adrenolytic drug which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor.
Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM.
Ajmalicine (Raubasine) acts preferentially at postsynaptic sites, competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptor with a pA2 value of 6.57, blocks the inhibitory effect of clonidine with an pA2 value of 6.2.
|
-
- HY-108415
-
-
- HY-108693
-
-
- HY-N2448
-
