Search Result
Results for "Amino acids with pde Inhibitors" in MCE Product Catalog:
8346
Inhibitors & Agonists
17
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-135298
-
-
- HY-U00427
-
-
- HY-50865
-
-
- HY-101490
-
-
- HY-12813
-
-
- HY-130695
-
-
- HY-U00410
-
-
- HY-U00352
-
-
- HY-W009749
-
|
L-Cystathionine
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
L-Cystathionine is a nonprotein thioether and is a key amino acid associated with the metabolic state of sulfur-containing amino acids. L-Cystathionine protects against Homocysteine-induced mitochondria-dependent apoptosis of vascular endothelial cells (HUVECs). L-Cystathionine plays an important role in cardiovascular protection.
|
-
- HY-103160A
-
-
- HY-30216
-
-
- HY-D0227
-
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Trometamol
Tromethamine
|
Others
|
Metabolic Disease
|
|
Trometamol is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol is an effective amine compound for pH control in the physiological range.
|
-
- HY-D0227A
-
|
Trometamol hydrochloride
Tromethamine hydrochloride
|
Others
|
Metabolic Disease
|
|
Trometamol hydrochloride (Tromethamine hydrochloride) is a biologically inert amino alcohol of low toxicity, which buffers carbon dioxide and acids in vitro and in vivo. Trometamol hydrochloride is an effective amine compound for pH control in the physiological range.
|
-
- HY-W016715
-
|
L-Cysteine hydrochloride hydrate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Cysteine hydrochloride hydrate is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride hydrate suppresses ghrelin and reduces appetite in rodents and humans.
|
-
- HY-70069
-
-
- HY-10469
-
-
- HY-12887
-
-
- HY-B1274
-
-
- HY-U00439
-
-
- HY-100309
-
|
9-amino-CPT
9-Amino-20(S)-camptothecin
|
Topoisomerase
|
Cancer
|
|
9-amino-CPT (9-amino-20(S)-camptothecin) is a topoisomerase I inhibitor with potent anticancer activity.
|
-
- HY-113025A
-
|
L-hydroxylysine dihydrochloride
(2S,5R)-5-Hydroxylysine dihydrochloride
|
Endogenous Metabolite
|
Others
|
|
L-hydroxylysine dihydrochloride ((2S,5R)-5-Hydroxylysine dihydrochloride), an amino acid, is exclusive to collagen protein, which is formed by posttranslational hydroxylation of some lysine residues.
|
-
- HY-Y0123
-
|
DL-Tyrosine
|
Others
|
Neurological Disease
|
|
DL-Tyrosine is an aromatic nonessential amino acid synthesized from the essential amino acid phenylalanine. DL-Tyrosine is a precursor for several important neurotransmitters (epinephrine, norepinephrine, dopamine).
|
-
- HY-14520
-
|
Tetrahydrofolic acid
L-5,6,7,8-Tetrahydrofolic acid; L-Tetrahydrofolic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Tetrahydrofolic acid (L-5,6,7,8-Tetrahydrofolic acid) is the biologically active vitamin B9 folate derivative. Tetrahydrofolic acid is a donor of one-carbon groups for amino acids, nucleic acids, and lipids. Tetrahydrofolic acid serves as an acceptor of free formaldehyde, producing 5,10-methylenetetrahydrofolate-Tetrahydrofolic acid.
|
-
- HY-W017443
-
-
- HY-111643
-
-
- HY-120139
-
|
KMH-233
|
Others
|
Cancer
|
|
KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM).
|
-
- HY-N0717
-
-
- HY-135916
-
-
- HY-131033
-
|
L-Azidonorleucine hydrochloride
|
Others
|
Others
|
|
L-Azidonorleucine hydrochloride, an unnatural amino acid, is A Methionine surrogate. L-Azidonorleucine hydrochloride can be used to label mammalian cell proteins and identify a diverse set of methionyl-tRNA synthetase (MetRS) mutants .
|
-
- HY-113227
-
-
- HY-12597
-
|
Quisqualic acid
L-Quisqualic acid
|
iGluR
mGluR
|
Neurological Disease
|
|
Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis.
|
-
- HY-117109
-
|
Amino Tadalafil
|
Others
|
|
|
Amino Tadalafil is an analog of tadalafil. Tadalafil is a potent inhibitor of phosphodiesterase 5 with applications in several conditions, including erectile dysfunction, pulmonary arterial hypertension, and lower urinary tract dysfunction.
|
-
- HY-140179
-
-
- HY-133334
-
-
- HY-140183
-
-
- HY-140184
-
-
- HY-140182
-
-
- HY-140176
-
-
- HY-140185
-
-
- HY-140178
-
-
- HY-140177
-
-
- HY-140186
-
-
- HY-140180
-
-
- HY-140181
-
-
- HY-59132
-
-
- HY-W010224
-
-
- HY-W016734
-
-
- HY-W002820
-
|
2-Amino-5-phenylpyridine
|
Endogenous Metabolite
|
Cancer
|
|
2-Amino-5-phenylpyridine is a mutagenic heterocyclic aromatic amine that is formed by pyrolysis of phenylalanine in proteins. 2-Amino-5-phenylpyridine is in broiled sardines and is considered as potentially carcinogenic.
|
-
- HY-130166
-
-
- HY-W050026S
-
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Phenylacetylglutamine-D5
NSC 203800-D5; Phenylacetyl-L-glutamine-D5
|
Others
|
Others
|
|
Phenylacetylglutamine-D5 (NSC 203800-D5;Phenylacetyl-L-glutamine-D5) is a deuterated form of Phenylacetylglutamine. Phenylacetylglutamine is a colonic microbial metabolite from amino acid fermentation.
|
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- HY-140002
-
-
- HY-135974
-
-
- HY-140097
-
-
- HY-140187
-
-
- HY-W040165
-
-
- HY-115384
-
-
- HY-W012708
-
-
- HY-114158A
-
|
Pronase E (Activity≥4000 U/mg)
Pronase (Activity≥4000 U/mg)
|
Others
|
Others
|
|
Pronase E (Activity≥4000 U/mg) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-W012982
-
-
- HY-129476
-
|
L-Canaline
|
Parasite
Endogenous Metabolite
|
Cancer
Infection
|
|
L-Canaline is a nonprotein amino acid stored in many leguminous plants. L-Canaline is a cytotoxic metabolite catalyzed by L-canavanine and its arginase. L-Canaline is a potent and irreversible inhibitor of ornithine aminotransferase. L-Canaline inhibits the growth of the malaria parasite Plasmodium falciparum with an IC50 of 297 nM. L-Canaline has anticancer and antiproliferative effects.
|
-
- HY-W040168
-
-
- HY-140397
-
-
- HY-125847
-
|
Salvianolic acid F
|
Others
|
Cancer
|
|
Salvianolic acid F is a kind of Salvianolic Acids. Salvianolic Acids is the most effective and abundant compounds extracted from Salvia miltiorrhiza, with good anti-oxidative activity.
|
-
- HY-114158
-
|
Pronase E (Activity≥7000 U/g)
Pronase (Activity≥7000 U/g)
|
Others
|
Others
|
|
Pronase E (Activity≥7000 U/g) is a mixture of proteolytic enzymes that is obtained from Streptomyces griseus and could digest protein into individual amino acids.
|
-
- HY-N0717A
-
-
- HY-N6030
-
|
(Rac)-Dencichin
2-Amino-3-(carboxyformamido)propanoic acid
|
Others
|
Others
|
|
(Rac)-Dencichin (2-Amino-3-(carboxyformamido)propanoic acid) is the racemate of Dencichin. Dencichin is a non-protein amino acid originally extracted from Panax notoginseng, and can inhibit HIF-prolyl hydroxylase-2 (PHD-2) activity.
|
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- HY-Y0252
-
-
- HY-W012974
-
-
- HY-W016480
-
-
- HY-Y0507
-
|
DL-Serine
|
Others
|
Cancer
Infection
|
|
DL-Serine is a mixture of D-Serine and L-Serine. DL-Serine has antiviral activity against the multiplication of tobacco mosaic virus (TMV).
|
-
- HY-108540
-
|
LAT1-IN-1
BCH
|
Apoptosis
|
Cancer
|
|
LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.
|
-
- HY-B1122
-
-
- HY-136168
-
-
- HY-N0325
-
|
DL-Methionine
|
Parasite
|
Infection
Inflammation/Immunology
|
|
DL-Methionine is an essential amino acid containing sulfur with oxidative stress defense effects. DL-Methionine can be used for animal natural feed. DL-Methionine also kills H. rostochiensis on potato plants.
|
-
- HY-B0863
-
|
Glyphosate
|
Apoptosis
Autophagy
|
Cancer
|
|
Glyphosate is an herbicidal derivative of the amino acid glycine. Glyphosate targets and blocks a plant metabolic pathway not found in animals, the shikimate pathway, required for the synthesis of aromatic amino acids in plants.
|
-
- HY-P1593
-
-
- HY-P1850
-
-
- HY-117519
-
-
- HY-122207
-
-
- HY-P1593A
-
-
- HY-13765
-
-
- HY-W008794
-
-
- HY-W014504
-
-
- HY-W016798
-
-
- HY-128750
-
-
- HY-W008005
-
|
Amino-PEG4-alcohol
|
PROTAC Linker
ADC Linker
|
Cancer
|
|
Amino-PEG4-alcohol is a PEG-based PROTAC linker can be used in the synthesis of PROTACs. Amino-PEG4-alcohol is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-119417
-
|
Chloramben
3-Amino-2,5-dichlorobenzoic acid
|
Others
|
Others
|
|
Chloramben (3-Amino-2,5-dichlorobenzoic acid) is a pre-emergence herbicide used to control the seedlings of annual grasses and broadleaf weeds.
|
-
- HY-B0399
-
|
L-Carnitine
Levocarnitine
|
Endogenous Metabolite
|
Metabolic Disease
Neurological Disease
|
|
L-Carnitine (Levocarnitine) is an endogenous molecule involved in fatty acid metabolism, biosynthesized within the human body using amino acids: L-lysine and L-methionine, as substrates. L-Carnitine functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-carnitine can ameliorate metabolic imbalances in many inborn errors of metabolism.
|
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- HY-W013494
-
-
- HY-N0650
-
|
L-Serine
(-)-Serine; (S)-Serine
|
Endogenous Metabolite
|
Cancer
|
|
L-Serine ((-)-Serine; (S)-Serine), one of the so-called non-essential amino acids, plays a central role in cellular proliferation.
|
-
- HY-112831
-
|
BI-409306
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); BI-409306 can be used in the research of memory enhancement in CNS disorders.
|
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- HY-B2033
-
|
Pyrimethanil
|
Fungal
|
Infection
|
|
Pyrimethanil is an effective broad-spectrum fungicide often used for the prevention of Botrytis cinerea. Pyrimethanil inhibits methionine biosynthesis and other amino acids, thereby affecting protein formation and cell division.
|
-
- HY-16391
-
|
Glasdegib
PF-04449913
|
Smo
|
Cancer
|
|
Glasdegib (PF-04449913) is a potent and orally bioavailable smoothened inhibitor. Glasdegib (PF-04449913) binds to human SMO (amino acids 181-787) with an IC50 of 4 nM.
|
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- HY-16900
-
-
- HY-103050
-
|
ML-030
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
ML-030 is a potent PDE4 inhibitor, with IC50 of 6.7 nM, 12.9 nM, 48.2 nM, 37.2 nM, 452 nM and 49.2 nM for PDE4A, PDE4A1, PDE4B1, PDE4B2, PDE4C1,and PDE4D2, respectively.
|
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- HY-102050
-
-
- HY-109586
-
-
- HY-U00186
-
-
- HY-140204
-
-
- HY-140197
-
-
- HY-140206
-
-
- HY-23105
-
-
- HY-140240
-
-
- HY-140200
-
-
- HY-130659
-
-
- HY-140210
-
-
- HY-130447
-
-
- HY-140199
-
-
- HY-140205
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-
- HY-140196
-
-
- HY-140209
-
-
- HY-140195
-
-
- HY-140198
-
-
- HY-140193
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-
- HY-140207
-
-
- HY-140211
-
-
- HY-140194
-
-
- HY-23212
-
-
- HY-16900A
-
-
- HY-12318
-
-
- HY-18252
-
-
- HY-114672
-
|
MBCQ
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
MBCQ is a potent and selective the type V phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ has IC50s >100 µM for PDE1, PDE2, PDE3, and PDE4, respectively. MBCQ dilates coronary arteries via potent and specific inhibition of cGMP-PDE.
|
-
- HY-140239
-
-
- HY-50071
-
-
- HY-N6704
-
|
Enniatin A1
|
ERK
Apoptosis
|
Cancer
|
|
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
|
-
- HY-131124
-
-
- HY-15455
-
|
Roflumilast
|
Phosphodiesterase (PDE)
RSV
|
Inflammation/Immunology
|
|
Roflumilast is a selective PDE4 inhibitor with IC50s of 0.7, 0.9, 0.7, and 0.2 nM for PDE4A1, PDEA4, PDEB1, and PDEB2, respectively, without affecting PDE1, PDE2, PDE3 or PDE5 isoenzymes from various cells.
|
-
- HY-W019799
-
-
- HY-135410
-
|
ABZ-amine
Amino albendazole
|
Others
|
Infection
|
|
ABZ-amine (Amino albendazole) is an impurity of Albendazole. Albendazole is a member of the benzimidazole compounds used as a drug indicated for the treatment of a variety of worm infestations.
|
-
- HY-126942
-
-
- HY-130298
-
-
- HY-120761
-
-
- HY-B0442
-
|
Vardenafil
|
Phosphodiesterase (PDE)
|
Endocrinology
|
|
Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction.
|
-
- HY-B0442A
-
|
Vardenafil hydrochloride
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Vardenafil hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction.
|
-
- HY-100246
-
-
- HY-15747A
-
-
- HY-131005
-
-
- HY-P1749
-
-
- HY-135717
-
|
Norbiotinamine
|
Others
|
Cancer
|
|
Norbiotinamine is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
|
-
- HY-113063
-
-
- HY-135717A
-
|
Norbiotinamine hydrochloride
|
Others
|
Cancer
|
|
Norbiotinamine hydrochloride is an alternative to biotin. Norbiotinamine can be coupled with a carboxylic group of amino acids to give inverse peptides, having the amide linkage oriented in the opposite direction.
|
-
- HY-130141
-
-
- HY-W008279
-
-
- HY-140224
-
-
- HY-140223
-
-
- HY-130181
-
-
- HY-15426
-
-
- HY-15747
-
-
- HY-122641
-
-
- HY-101661
-
-
- HY-101312
-
-
- HY-10978
-
-
- HY-107830
-
|
Methyl cholate
|
Others
|
Metabolic Disease
|
|
Methyl Cholate is methyl ester form of Cholic acid. Cholic acid is one of the major bile acids produced by the liver, where it is synthesized from cholesterol.
|
-
- HY-14930A
-
-
- HY-136350
-
|
BRD9500
|
Phosphodiesterase (PDE)
|
Cancer
|
|
BRD9500 is an orally active phosphodiesterases 3 (PDE3) inhibitor with IC50s of 10 and 27 nM for PDE3A and PDE3B, respectively. Antitumor activity.
|
-
- HY-14254
-
|
Olprinone Hydrochloride
Loprinone Hydrochloride
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Olprinone (Loprinone) Hydrochloride is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone Hydrochloride is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity.
|
-
- HY-14254A
-
|
Olprinone
Loprinone
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Olprinone (Loprinone) is a potent phosphodiesterase (PDE) 3 inhibitor, with IC50s of 150, 100, 0.35 and 14 μM for PDE1, PDE2, PDE3 and PDE4, respectively. Olprinone is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity.
|
-
- HY-W008097
-
-
- HY-115555
-
-
- HY-119737
-
|
Chlorsulfuron
|
Others
|
Metabolic Disease
|
|
Chlorsulfuron blocks the biosynthesis of the amino acids valine and isoleucine in plants. Chlorsulfuron completely alleviates herbicide-induced growth inhibition. The site of action of Chlorsulfuron is the enzyme acetolactate synthase.
|
-
- HY-P1755
-
-
- HY-D0885B
-
-
- HY-136041
-
-
- HY-130955
-
-
- HY-130972
-
-
- HY-136085
-
-
- HY-10846
-
-
- HY-N0215
-
|
L-Phenylalanine
(S)-2-Amino-3-phenylpropionic acid
|
Calcium Channel
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Phenylalanine ((S)-2-Amino-3-phenylpropionic acid) is an essential amino acid isolated from Escherichia coli. L-Phenylalanine is a α2δ subunit of voltage-dependent Ca + channels antagonist with a Ki of 980 nM. L-phenylalanine is a competitive antagonist for the glycine- and glutamate-binding sites of N-methyl-D-aspartate receptors (NMDARs) (KB of 573 μM ) and non-NMDARs, respectively. L-Phenylalanine is widely used in the production of food flavors and pharmaceuticals.
|
-
- HY-W011819
-
|
Tetradecanedioic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Tetradecanedioic acid is an endogenous metabolite and belongs to the class of organic compounds known as long-chain fatty acids. Tetradecanedioic acid can act as a candidate biomarker for organic anion-transporting polypeptide mediated drug-drug interactions .
|
-
- HY-122942
-
-
- HY-130524
-
|
Amino-PEG4-CH2COOH
|
PROTAC Linker
ADC Linker
|
Cancer
|
|
Amino-PEG4-CH2COOH is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs. Amino-PEG4-CH2COOH is also a non-cleavable 4 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-140188
-
-
- HY-140251
-
-
- HY-140249
-
-
- HY-140250
-
-
- HY-140082
-
-
- HY-B0283
-
|
Acipimox
K-9321
|
Others
|
Metabolic Disease
|
|
Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity.
|
-
- HY-B1258
-
-
- HY-W008437
-
-
- HY-W040270
-
|
Amino-PEG10-amine
|
PROTAC Linker
|
Cancer
|
|
Amino-PEG10-amine, a PEG-based PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer.
|
-
- HY-141147
-
-
- HY-117571
-
-
- HY-100933
-
-
- HY-42619
-
-
- HY-130577
-
-
- HY-133336
-
-
- HY-133335
-
-
- HY-W015088
-
-
- HY-133332
-
-
- HY-133338
-
-
- HY-140189
-
-
- HY-140001
-
-
- HY-133337
-
-
- HY-133333
-
-
- HY-22335
-
-
- HY-130411
-
|
Amino-PEG11-amine
|
PROTAC Linker
|
Cancer
|
|
Amino-PEG11-amine, a PEG-based (12 units) PROTAC linker used to combine two mono diethylstilbestrol (DES)-based ligands, provides an alternative strategy for preparing more selective and active ER antagonists for endocrine therapy of breast cancer.
|
-
- HY-136373
-
|
Metazachlor
|
Others
|
Others
|
|
Metazachlor is a herbicide of the chloroacetamide class. Metazachlor is an inhibitor of the synthesis of long chain fatty acids and has an effect on cell division or tissue differentiation in the germinating and emerging weed target species.
|
-
- HY-131045
-
|
HADA hydrochloride
HCC-Amino-D-alanine hydrochloride
|
Others
|
Others
|
|
HADA Hydrochloride is a blue fluorescent D-amino acid (FDAA). FDAAs are efficiently incorporated into the peptidoglycans (PGs) of diverse bacterial species at the sites of PG biosynthesis, allowing specific and covalent probing of bacterial growth with minimal perturbation.
|
-
- HY-W020086
-
|
2,3-Diaminophenazine
2,3-Phenazinediamine
|
Others
|
Others
|
|
2,3-Diaminophenazine (2,3-Phenazinediamine) is an amino derivative of phenazine with promising luminescence, electrochemical and biochemical applications.
|
-
- HY-N1860
-
|
3-O-Methylquercetin
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
3-O-Methylquercetin (3-MQ), a main constituent of Rhamnus nakaharai, inhibits total cAMP and cGMP-phosphodiesterase (PDE) of guinea pig trachealis. 3-O-Methylquercetin (3-MQ) exhibits IC50 values of 31.9 μM， 86.9 μM， 18.6 μM and 1.6 μM for PDE1, PDE5, PDE2 and PDE4, respectively.
|
-
- HY-112754A
-
|
DOTAP chloride
1,2-Dioleoyl-3-trimethylammonium-propane chloride
|
Others
|
Others
|
|
DOTAP chloride is a useful and effective cationic lipid for transient and stable transfection DNA (plasmids, bacmids) and modified nucleic acids (antisense oligonucleotides) with out the use of helper lipid.
|
-
- HY-15485
-
-
- HY-A0132
-
-
- HY-136134
-
-
- HY-140099
-
-
- HY-101644A
-
-
- HY-10790
-
|
Cilomilast
SB-207499
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Cilomilast (SB-207499) is a potent, selective and orally active inhibitor of Phosphodiesterase 4 (PDE4), with IC50s of ~100 and 120 nM for LPDE4 and HPDE4, respectively. Cilomilast shows selectivity for PDE4 over PDE1, PDE2, PDE3 and PDE5 (IC50=74, 65, >100, and 83 µM, respectively). Cilomilast has anti-inflammatory and immunomodulatory effects and can be used for thr research of asthma and chronic obstructive pulmonary disease (COPD).
|
-
- HY-12501A
-
|
ITI-214
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-140201
-
-
- HY-140202
-
-
- HY-106003
-
-
- HY-D0885
-
|
Phosphocreatine
Creatine phosphate; Creatinephosphoric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phosphocreatine, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives, is a substrate for the determination of creatine kinase and used to regenerate ATP during skeletal muscle contraction..
|
-
- HY-128923
-
|
SKF-34288 hydrochloride
3-Mercaptopicolinic acid hydrochloride
|
Others
|
Metabolic Disease
|
|
SKF-34288 hydrochloride (3-Mercaptopicolinic acid) is a phosphoenolpyruvate carboxykinase (PEPCK) inhibitor.
SKF-34288 hydrochloride is a potent hypoglycemic agent via inhibition of glucose synthesis through the specific inhibition of PEPCK in the gluconeogenesis pathway. SKF-34288 hydrochloride inhibits Asn metabolism and results in an increase in amino acids and amides.
|
-
- HY-140262
-
-
- HY-41461
-
-
- HY-17464
-
-
- HY-100639
-
-
- HY-14252
-
-
- HY-15444
-
-
- HY-D0885C
-
|
Phosphocreatine dipotassium
Creatine phosphate (dipotassium); Creatinephosphoric acid (dipotassium)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phosphocreatine dipotassium, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives, is a substrate for the determination of creatine kinase and used to regenerate ATP during skeletal muscle contraction.
|
-
- HY-14518
-
|
Aminopterin
4-Aminofolic acid; APGA
|
Antifolate
|
Cancer
Inflammation/Immunology
|
|
Aminopterin (4-Aminofolic acid), the 4-amino derivative of folic acid, is a folic acid antagonist. Aminopterin catalyses the reduction of folic acid to tetrahydrofolic acid, and competitively inhibits dihydrofolate reductase (DHFR) with a Ki of 3.7 pM. Aminopterin has anticancer and immunosuppressive activity. Aminopterin is used in treatment of pediatric leukemia.
|
-
- HY-12501
-
|
ITI-214 free base
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
ITI-214 free base is a potent, CNS-active, orally bioavailable PDE1 inhibitor (Ki of 58 pM) with excellent selectivity against other PDE family members and against a panel of enzymes, receptors, transporters and ion channels. ITI-214 free base inhibits recombinant full-length human PDE1A, PDE1B and PDE1C with Kis of 33 pM, 380 pM and 35 pM, respectively. ITI-214 free base shows efficacy in various animal models of motor and cognitive functions.
|
-
- HY-100640
-
-
- HY-12472
-
-
- HY-140190
-
-
- HY-W008568
-
-
- HY-140222
-
-
- HY-140534
-
-
- HY-B1639
-
|
Enoximone
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects.
|
-
- HY-W021401
-
-
- HY-D0885A
-
|
Phosphocreatine disodium tetrahydrate
Creatine phosphate (disodium tetrahydrate); Creatinephosphoric acid (disodium tetrahydrate)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Phosphocreatine disodium tetrahydrate, primarily found in the skeletal muscles of vertebrates and one of organic compounds known as alpha amino acids and derivatives, is a substrate for the determination of creatine kinase and used to regenerate ATP during skeletal muscle contraction.
|
-
- HY-111434A
-
|
UAA crosslinker 1 hydrochloride
|
Others
|
Cancer
|
|
UAA crosslinker 1 hydrochloride is an amber codon used for non-canonical amino acids (ncAAs) incorporation. The ncAAs can be incorporated into proteins in vivo by making use of the promiscuous activity of certain wildtype and engineered aminoacyl-tRNA synthetases.
|
-
- HY-N0014
-
-
- HY-13927
-
-
- HY-B0327A
-
-
- HY-B0327
-
-
- HY-141154
-
-
- HY-131082
-
-
- HY-121879
-
-
- HY-21088
-
-
- HY-A0282
-
|
L-Ornithine L-aspartate
|
Others
|
Metabolic Disease
|
|
L-Ornithine L-aspartate is a stable salt of two natural nonessential L-amino acids: ornithine and aspartic acid. L-Ornithine L-aspartate lowers blood ammonia concentration and to eliminate symptoms of hepatic encephalopathy associated with liver cirrhosis.
|
-
- HY-130968
-
-
- HY-130970
-
-
- HY-100118
-
-
- HY-14550
-
-
- HY-12085
-
-
- HY-128358
-
|
MR-L2
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM.
|
-
- HY-W010062
-
-
- HY-U00374
-
-
- HY-14992
-
-
- HY-141250
-
-
- HY-133298
-
-
- HY-15441
-
-
- HY-W007713
-
-
- HY-111371
-
-
- HY-90009A
-
-
- HY-101826
-
-
- HY-W000450
-
-
- HY-131165
-
-
- HY-136090
-
-
- HY-W021425
-
|
(2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal hydrochloride
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(2S,3R,4S,5R)-2-Amino-3,4,5,6-tetrahydroxyhexanal hydrochloride is an endogenous metabolite.
|
-
- HY-P1306
-
|
Obestatin(rat)
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Obestatin(rat), encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-140087
-
-
- HY-140254
-
-
- HY-140253
-
-
- HY-140255
-
-
- HY-131255
-
-
- HY-50098
-
-
- HY-50098A
-
|
Mardepodect hydrochloride
PF-2545920 hydrochloride
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Mardepodect hydrochloride (PF-2545920 hydrochloride) is a potent, orally active and selective PDE10A inhibitor with an IC50 of 0.37 nM, with >1000-fold selectivity over other PDEs. Mardepodect hydrochloride can cross the blood-brain barrier.
|
-
- HY-122641A
-
-
- HY-122641C
-
-
- HY-15025A
-
-
- HY-B0809
-
-
- HY-100615
-
-
- HY-140191
-
-
- HY-12913
-
-
- HY-122641B
-
-
- HY-B0204A
-
-
- HY-U00254
-
-
- HY-B0204
-
-
- HY-135795
-
|
1-Cyclohexyl-3-dodecyl urea
CDU; N-Cyclohexyl-N-dodecyl urea; NCND
|
Epoxide Hydrolase
|
Metabolic Disease
Cardiovascular Disease
|
|
1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) is a highly selective soluble epoxide hydrolase (sEH) inhibitor. 1-Cyclohexyl-3-dodecyl urea (CDU; N-Cyclohexyl-N-dodecyl urea; NCND) increases epoxyeicosatrienoic acids (EETs) levels and lowers blood pressure in angiotensin II (Ang II) hypertension.
|
-
- HY-19373
-
-
- HY-104028
-
-
- HY-100217
-
|
D,L-3-Indolylglycine
α-Amino-1H-indole-3-acetic acid
|
Others
|
Others
|
|
D,L-3-Indolylglycine is an unnatural amino acid that is very similar to Tryptophan, with the indole moiety directly attached to the α-position.
|
-
- 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-15178
-
|
Oglemilast
GRC 3886
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Oglemilast (GRC 3886) is a potent and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 of 0.5 nM for PDE4D3. Oglemilast inhibits pulmonary cell infiltration, including eosinophilia and neutrophilia in vitro and in vivo. Oglemilast has the potential for inflammatory airway diseases.
|
-
- HY-130957
-
-
- HY-140928
-
-
- HY-140921
-
-
- 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, 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-123210
-
-
- HY-15025
-
-
- HY-117604
-
|
THPP-1
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
|
-
- HY-141056
-
-
- HY-P1306A
-
|
Obestatin(rat) TFA
|
GHSR
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Obestatin(rat) TFA, encoded by the Ghrelin gene, is a cpeptide, comprised of 23 amino acids. Obestatin(rat) TFA suppresses food intake, inhibits jejunal contraction, and decreases body-weight gain. Obestatin is an endogenous ligand of G-protein coupled receptor 39 (GPR39). Obestatin(rat) TFA has anti-inflammatory, anti-myocardial infarction and antioxidant activities.
|
-
- HY-N7384
-
-
- HY-12740
-
-
- HY-16558
-
|
Butein
2’,3,4,4’-tetrahydroxy Chalcone
|
EGFR
Autophagy
Apoptosis
Phosphodiesterase (PDE)
|
Cancer
|
|
Butein, isolated from Dalbergia odorifera T. Chen, is a cAMP-specific PDE inhibitor with an IC50 of 10.4 μM for PDE4. Butein is a specific protein tyrosine kinase inhibitor with IC50s of 16 and 65 μM for EGFR and p60 c-src in HepG2 cells. Butein sensitizes HeLa cells to Cisplatin through AKT and ERK/p38 MAPK pathways by targeting FoxO3a. Butein is a SIRT1 activator (STAC).
|
-
- HY-136569
-
|
DSR-141562
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
|
-
- HY-128879A
-
|
VP3.15 dihydrobromide
|
Phosphodiesterase (PDE)
GSK-3
|
Neurological Disease
|
|
VP3.15 dihydrobromide is a potent, orally bioavailable and CNS-penetrant dual phosphodiesterase (PDE)7- glycogen synthase kinase (GSK)3 inhibitor, with IC50s of 1.59 μM and 0.88 μM for PDE7 and GSK-3, respectively. VP3.15 dihydrobromide has neuroprotective and neuroreparative activities, thus as potential combined anti-inflammatory and pro-remyelinating therapies for multiple sclerosis (MS).
|
-
- HY-133327
-
-
- HY-133329
-
-
- HY-133330
-
-
- HY-133328
-
-
- HY-100530B
-
|
Sp-cAMPS
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Sp-cAMPS, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS binds the PDE10 GAF domain with an EC50 of 40 μM.
|
-
- HY-100530C
-
|
Sp-cAMPS sodium salt
|
PKA
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Sp-cAMPS sodium salt, a cAMP analog, is potent activator of cAMP-dependent PKA I 和 PKA II. Sp-cAMPS sodium salt is also a potent, competitive phosphodiesterase (PDE3A) inhibitor with a Ki of 47.6 µM. Sp-cAMPS sodium salt binds the PDE10 GAF domain with an EC50 of 40 μM.
|
-
- HY-Y0469
-
|
1-Aminohydantoin hydrochloride
|
Others
|
Others
|
|
1-Aminohydantoin hydrochloride is a major metabolite of nitrofurantoin in animal tissues and can be used as a standard for the determination of residues of veterinary agents in meat, milk et.al. 1-Aminohydantoin hydrochloride covalently binds to tissue proteins and is released from the tissues under slightly acidic conditions and derivatized with 2-nitrobenzaldehyde to form nitrophenyl derivatives of AHD before detection.
|
-
- 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-135848
-
-
- HY-19102
-
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid a sulfur-containing flavor component produced by Asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-P2458
-
|
CAP18 (rabbit)
|
Bacterial
|
Infection
|
|
CAP18 (rabbit) is a 37 amino acids antimicrobial peptide originally isolated from rabbit granulocytes. CAP18 (rabbit) has broad antimicrobial activity against both Gram-positive (IC50, 130-200 nM) and Gram-negative (IC50, 20-100 nM) bacteria. CAP18 (rabbit) has the potential for bacterial sepsis research.
|
-
- HY-W003445
-
|
4-Bromo-3-hydroxybenzoic acid
|
Endogenous Metabolite
|
Neurological Disease
|
|
4-Bromo-3-hydroxybenzoic acid is a metabolite of Brocresine and a histidine decarboxylase (HDC) inhibitor with IC50s of 1 mM for both rat fetal and rat gastric HDC. 4-Bromo-3-hydroxybenzoic acid also inhibits aromatic-L-amino acid decarboxylase from hog kidney and rat gastric mucosa in vitro with IC50s of 1 mM for both enzymes.
|
-
- HY-U00136
-
-
- 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-W018555
-
|
D-Cysteine
|
Endogenous Metabolite
Bacterial
|
Infection
Neurological Disease
|
|
D-Cysteine is the D-isomer of cysteine and a powerful inhibitor of Escherichia coli growth. D-cysteine is mediated by D-amino acid oxidase to produce H2S and is a neuroprotectant against cerebellar ataxias. D-Cysteine could inhibit the growth and cariogenic virulence of dual-species biofilms formed by S. mutans and S. sanguinis.
|
-
- HY-P1136
-
|
Gap19
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Gap19, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 has protective effects against myocardial.
|
-
- HY-Y1620
-
-
- HY-121381
-
|
Kuraridine
|
Phosphodiesterase (PDE)
|
Others
|
|
Kuraridine is a prenylated flavonol extract from the roots of Sophora flavescens. Kuraridine has an inhibitory effect on cGMP specific phosphodiesterase type 5 (PDE5) (IC50=0.64 μM).
|
-
- 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-101693
-
-
- HY-P1839
-
|
Angiotensin I/II (1-5)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-5 is a peptide that contains the amino acids 1-5, which is converted from Angiotensin I/II. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-P1829
-
|
Angiotensin I/II (1-6)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-6 contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-18253
-
|
Udenafil
DA8159
|
Phosphodiesterase (PDE)
|
Endocrinology
Others
|
|
Udenafil (DA8159) is a potent, selective and orally active phosphodiesterase type 5 (PDE5) inhibitor. Udenafil also inhibits cGMP hydrolysis and can be used for erectile dysfunction research.
|
-
- HY-P1136A
-
|
Gap19 TFA
|
Gap Junction Protein
|
Cardiovascular Disease
|
|
Gap19 TFA, a peptide derived from nine amino acids of the Cx43 cytoplasmic loop (CL), is a potent and selective connexin 43 (Cx43) hemichannel blocker. Gap19 TFA inhibits hemichannels caused by preventing intramolecular interactions of the C-terminus (CT) with the CL. Gap19 TFA is not blocking GJ channels or Cx40/pannexin-1 hemichannels. Gap19 TFA has protective effects against myocardial.
|
-
- 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-108045
-
-
- HY-W009371A
-
|
D-Ribose 5-phosphate
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Ribose 5-phosphate is an intermediate of the oxidative branch of the pentose phosphate pathway (PPP) and an end product of the nonoxidative branch of the PPP. D-Ribose 5-phosphate is used in the synthesis of nucleotides and nucleic acids.
|
-
- 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-18728
-
-
- HY-U00179
-
-
- HY-90009
-
|
Nortadalafil
Demethyl Tadalafil
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Nortadalafil is demethyl Tadalafil, which is a PDE5 inhibitor, currently marketed in pill form for treating erectile dysfunction (ED) under the name Cialis; and under the name Adcirca for the treatment of pulmonary arterial hypertension.
|
-
- HY-B0559
-
|
Nabumetone
BRL14777
|
COX
|
Inflammation/Immunology
Cancer
|
|
Nabumetone is an orally active non-acidic anti-inflammatory agent, acts as a potent and selective COX-2 inhibitor, and is the prodrug of the active metabolite 6MNA.
|
-
- HY-59354
-
|
Maleic hydrazide
|
DNA/RNA Synthesis
|
Cancer
|
|
Maleic hydrazide is extensively used as a systemic plant growth regulator and as a herbicide. Maleic hydrazide acts as an inhibitor of the synthesis of nucleic acids and proteins.
|
-
- HY-W009371
-
|
D-Ribose 5-phosphate disodium
|
Others
|
Metabolic Disease
|
|
D-Ribose 5-phosphate disodium is an intermediate of the oxidative branch of the pentose phosphate pathway (PPP) and an end product of the nonoxidative branch of the PPP. D-Ribose 5-phosphate disodium is used in the synthesis of nucleotides and nucleic acids.
|
-
- 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-19830
-
-
- HY-13451
-
|
Finafloxacin
|
Bacterial
|
Infection
|
|
Finafloxacin is a fluoroquinolone antimicrobial agent that exhibits optimum efficacy in slightly acidic environments.
|
-
- HY-113298
-
-
- HY-B0140
-
-
- HY-18740A
-
|
Trequinsin hydrochloride
HL 725
|
Phosphodiesterase (PDE)
|
Metabolic Disease
|
|
Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of platelet CAMP phosphodiesterase (PDE), with an IC50 of 0.25 nM. Trequinsin hydrochloride (HL 725) is an extremely potent inhibitor of the aggregation of human platelets induced in vitro by ADP, collagen, thrombin and epinephrine.
|
-
- HY-W016993
-
-
- HY-113201
-
-
- HY-15583
-
-
- HY-112540B
-
|
Acetoacetic acid sodium salt
|
Others
|
Metabolic Disease
|
|
Acetoacetic acid sodium salt is a metabolite of non-esterified fatty acids, involved in the development of human diabetes. Acetoacetic acid sodium salt induces oxidative stress to inhibit the assembly of very low density lipoprotein in bovine hepatocytes.
|
-
- HY-76504
-
-
- HY-113085
-
-
- 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-111412
-
-
- HY-B0392
-
-
- HY-W015641
-
-
- HY-P1695
-
|
Cinnamycin
Ro 09-0198
|
Bacterial
Antibiotic
|
|
|
Cinnamycin is tetracyclic lantibiotic produced from S. cinnamoneus that contains four unusual amino acids: erythro-β-hydroxyaspartic acid, mesolanthionine, threo-β-methyllanthionine, and lysinoalanine.1 Cinnamycin has demonstrated antiviral activity against herpes simplex virus type 1 KOS strain infection in Vero cells via a cytopathic effect reduction assay. Cinnamycin recognizes the structure of phosphatidylethanolamine and forms an equimolar complex with the phospholipid on biological membranes. This peptide has been used as a probe for analyzing the transbilayer movement of phosphatidylethanolamine.
|
-
- HY-15297
-
|
Vesnarinone
OPC-8212
|
Phosphodiesterase (PDE)
HIV
|
Infection
|
|
Vesnarinone is a quinolinone derivative, and its pharmacodynamic effects include inhibition of phosphodiesterase III (PDE3) activity, increases in calcium flux and decreases in potassium flux.
|
-
- HY-B1468
-
-
- HY-N0832
-
-
- HY-100496
-
|
Nucleocidin
4'-Fluoro-5'-O-sulfamoyladenosine; NSC 521007
|
Bacterial
|
Infection
|
|
Nucleocidin is an antitrypanosomal antibiotic, inhibiting the transfer of labeled amino acid from S-RNA to protein.
|
-
- HY-W014502
-
|
D-Kynurenine
|
Aryl Hydrocarbon Receptor
Endogenous Metabolite
|
Cancer
|
|
D-kynurenine, a metabolite of D-tryptophan, can serve as the bioprecursor of kynurenic acid (KYNA) and 3-hydroxykynurenine. D-Kynurenine is an agonist for G protein-coupled receptor, GPR109B. D-Kynurenine is a substrate in a fluorometric assay of D-amino acid oxidase. D-kynurenine promotes epithelial-to-mesenchymal transition via activating aryl hydrocarbon receptor (AHR).
|
-
- 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-P1497
-
-
- HY-W053507
-
|
m-Tolylacetic acid
3-Methylbenzeneacetic acid
|
Others
|
Others
|
|
m-Tolylacetic acid (3-Methylbenzeneacetic acid) is a hydroaromatic dicarboxylic acids excreted in the urine as metabolite of tolueneacetic acid.
|
-
- HY-B0764A
-
|
Bucladesine calcium
Dibutyryl cAMP calcium salt; DBcAMP calcium salt
|
PKA
Phosphodiesterase (PDE)
Apoptosis
|
Others
|
|
Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
|
-
- HY-N6256
-
-
- HY-P1537
-
-
- HY-N2341
-
|
Palmitelaidic Acid
9-trans-Hexadecenoic acid; trans-Palmitoleic acid
|
AMPK
PPAR
Glucokinase
|
Metabolic Disease
|
|
Palmitelaidic Acid (9-trans-Hexadecenoic acid) is the trans isomer of palmitoleic acid. Palmitoleic acid is one of the most abundant fatty acids in serum and tissue.
|
-
- HY-N0473
-
-
- HY-101877
-
|
Statine
(3S,4S)-Statine; (S,S)-Statine
|
Others
|
Endocrinology
|
|
Statine is an unusual amino acid that occurs twice in the sequence of pepstatin, a protease inhibitor that is active against pepsin and other acid proteases.
|
-
- HY-N0771
-
-
- HY-P0198
-
-
- HY-109085
-
|
Difamilast
OPA-15406
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Difamilast (OPA-15406) is a topical, selective and nonsteroidal phosphodiesterase-4 (PDE4) inhibitor with particularly efficient inhibition of subtype B (IC50=11.2 nM). Difamilast can be used for the research of mild to moderate atopic dermatitis (AD).
|
-
- HY-19672
-
|
Lirimilast
BAY 19-8004
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Lirimilast (BAY 19-8004) is a potent, selective and orally active phosphodiesterase-4 (PDE4) inhibitor with an IC50 value of 49 nM. Lirimilast can be used for the treatment of asthma or chronic obstructive pulmonary disease (COPD). Lirimilast has potently anti-inflammatory properties.
|
-
- HY-B0764
-
|
Bucladesine sodium
Dibutyryl cAMP sodium salt; DBcAMP sodium salt
|
PKA
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Bucladesine sodium salt (Dibutyryl-cAMP sodium salt) is a stabilized cyclic AMP (cAMP) analog and a selective PKA activator. Bucladesine sodium salt raises the intracellular levels of cAMP. Bucladesine sodium salt is also a phosphodiesterase (PDE) inhibitor. Bucladesine sodium salt has anti-inflammatory activity and can be used for impaired wound healing.
|
-
- HY-19026
-
|
Siguazodan
SKF 94836
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Siguazodan (SKF 94836) is a potent, selective and orally active phosphodiesterase III (PDE-III) inhibitor with an IC50 of 117 nM. Siguazodan increases cAMP accumulation in intact platelets with an EC50 of 18.88 μM. Siguazodan also inhibits phenylephrine-induced 5-HT release with an IC50 value of 4.2 μM.
|
-
- HY-P1235A
-
-
- HY-10996A
-
-
- HY-A0127
-
|
Etofibrate
|
Others
|
Metabolic Disease
|
|
Etofibrate is the ethandiol-1,2 diester of the nicotinic and clofibric acids. Etofibrate has been shown to be a potent hypolipidemic agent in animal and human.
|
-
- HY-B0404A
-
-
- HY-10914
-
-
- HY-P1271
-
|
Catestatin
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-115661
-
|
Bisdionin C
|
Bacterial
|
Infection
|
|
Bisdionin C is a potent GH18 chitinases inhibitor, with an IC50 of 0.2 μM for A. fumigatus ChiB1 (AfChiB1). Bisdionin C inhibits HCHT (human macrophage chitotriosidase) and acidic mammalian chitinase (AMCase) with IC50s of 8.3 and 3.4 μM, respectively.
|
-
- 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-19675
-
|
Naproxen etemesil
LT-NS 001; MX 1094
|
COX
|
Inflammation/Immunology
|
|
Naproxen etemesil is a lipophilic, non-acidic, inactive prodrug of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
|
-
- HY-W007970
-
-
- HY-107373
-
|
β-Chloro-L-alanine
L-β-Chloroalanine
|
Bacterial
|
Infection
|
|
β-Chloro-L-alanine is a bacteriostatic amino acid analog which inhibits a number of enzymes, including threonine deaminase and alanine racemase.
|
-
- HY-16261
-
|
Aldoxorubicin
INNO-206; DOXO-EMCH
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
Aldoxorubicin (INNO-206) is an albumin-binding prodrug of Doxorubicin (DNA topoisomerase II inhibitor), which is released from albumin under acidic conditions. Aldoxorubicin (INNO-206) has potent antitumor activities in various cancer cell lines and in murine tumor models.
|
-
- HY-N6715
-
|
Tenuazonic acid
|
Influenza Virus
Bacterial
|
Infection
|
|
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate. Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor.
|
-
- HY-Y1055
-
-
- HY-P1271A
-
|
Catestatin TFA
|
nAChR
|
Cardiovascular Disease
|
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
|
-
- HY-P1164
-
-
- HY-W040222
-
-
- HY-P1144
-
-
- HY-P1164A
-
-
- HY-P1127
-
-
- HY-P1144A
-
-
- HY-P0191
-
-
- 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-P1235
-
|
Carperitide
Atrial Natriuretic Peptide (ANP) (1-28), human, porcine
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) is a 28-amino acid hormone, that is normally produced and secreted by the human heart in response to cardiac injury and mechanical stretch. Carperitide (Atrial Natriuretic Peptide (ANP) (1-28), human, porcine) inhibits endothelin-1 secretion in a dose-dependent way.
|
-
- HY-B1453
-
-
- HY-P0324
-
|
Parasin I
|
Bacterial
|
Infection
|
|
Parasin I is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
|
-
- HY-P0191A
-
-
- HY-B1816
-
-
- HY-B0715
-
|
Pentoxifylline
BL-191; PTX; Oxpentifylline
|
Phosphodiesterase (PDE)
Autophagy
HIV
|
Cardiovascular Disease
Cancer
|
|
Pentoxifylline (BL-191), a haemorheological agent, is an orally active non-selective phosphodiesterase (PDE) inhibitor, with immune modulation, anti-inflammatory, hemorheological, anti-fibrinolytic and anti-proliferation effects. Pentoxifylline can be used for the research of peripheral vascular disease, cerebrovascular disease and a number of other conditions involving a defective regional microcirculation.
|
-
- HY-30215
-
-
- HY-B0137A
-
-
- HY-B0137
-
-
- HY-13295
-
-
- HY-N0666B
-
|
Aspartic acid calcium
Calcium L-aspartate
|
Others
|
Cardiovascular Disease
|
|
Aspartic acid calcium (Calcium L-aspartate) is a chelate where calcium is attached to an amino acid naming L-Aspartic acid. L-Aspartic acid is an amino acid and serves as a building block for proteins in the body.
|
-
- HY-113494
-
|
Stigmastanol
|
Others
|
Others
|
|
Stigmastanol is the 6-amino derivative isolated from Hypericum riparium. Hypericum riparium A. Chev. is a Cameroonian medicinal plant belonging to the family Guttiferae.
|
-
- HY-N1477
-
-
- HY-P0324A
-
|
Parasin I TFA
|
Bacterial
|
Infection
|
|
Parasin I (TFA) is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
|
-
- 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-N8092
-
-
- HY-W018678
-
|
8-Aminooctanoic acid
|
Others
|
Metabolic Disease
|
|
8-Aminooctanoic acid is an omega-amino fatty acid that is octanoic acid which carries an amino group at position 8. 8-aminooctanoic acid has a role as a human metabolite.
|
-
- HY-113426
-
-
- HY-131112
-
-
- HY-W004260
-
|
Arachidic acid
Icosanoic acid
|
Endogenous Metabolite
|
Others
|
|
Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue.
|
-
- HY-B0955
-
|
Oxethazaine
Oxetacaine
|
HBV
|
Neurological Disease
|
|
Oxethazaine (Oxetacaine), a precursor of phentermine acidic, is an acid-resistent and orally active analgesic agent. Oxethazaine (Oxetacaine) has the potential for the relief of pain associated with peptic ulcer disease or esophagitis.
|
-
- HY-19688B
-
|
Sitamaquine tosylate
WR 6026 tosylate
|
Parasite
|
Infection
|
|
Sitamaquine (WR 6026) tosylate, an orally active 8-aminoquinoline analog, is an antileishmanial agent. Sitamaquine is a lipophilic weak base that rapidly accumulates in acidic compartments of Leishmania spp., mainly in acidocalcisomes.
|
-
- HY-90009C
-
|
ent-Tadalafil
ent-IC-351
|
Phosphodiesterase (PDE)
|
Cancer
|
|
ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC50 of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM.
|
-
- HY-135746
-
|
OR-1896
|
Potassium Channel
Phosphodiesterase (PDE)
Drug Metabolite
|
Cardiovascular Disease
|
|
OR-1896 is an active long-lived metabolite of Levosimendan. OR-1896 is a highly selective phosphodiesterase (PDE) III isoform inhibitor and a powerful vasodilator. OR-1896 can open ATP-sensitive K + channels and has Ca 2+-sensitizing effect. OR-1896 mitigates cardiomyocyte apoptosis, cardiac remodeling and myocardial inflammation.
|
-
- HY-N2368
-
|
Arecaidine
|
GABA Receptor
|
Neurological Disease
|
|
Arecaidine, a pyridine alkaloid, is a potent GABA uptake inhibitor. Arecaidine is a substrate of H +-coupled amino acid transporter 1 (PAT1, SLC36A1) and competitively inhibits L-proline uptake.
|
-
- HY-W012572
-
-
- HY-104011
-
-
- HY-W010040
-
-
- HY-W050026
-
-
- HY-113079
-
-
- HY-B0931
-
-
- HY-B0236
-
|
6-Aminocaproic acid
EACA; Epsilon-Amino-n-caproic Acid; 6-Aminohexanoic acid
|
Others
|
Metabolic Disease
|
|
6-Aminocaproic acid (EACA), a monoamino carboxylic acid, is a potent and orally active inhibitor of plasmin and plasminogen. 6-Aminocaproic acid is a potent antifibrinolytic agent. 6-Aminocaproic acid prevents clot lysis through the competitive binding of lysine residues on plasminogen, inhibiting plasmin formation and reducing fibrinolysis. 6-Aminocaproic acid can be used for the research of bleeding disorders.
|
-
- HY-P2466
-
-
- HY-N2284
-
|
Sophoflavescenol
|
AChE
Beta-secretase
Phosphodiesterase (PDE)
|
Cancer
|
|
Sophoflavescenol is a prenylated flavonol, which shows great inhibitory activity with IC50 of 0.013 μM against Phosphodiesterase 5 (PDE5), and also inhibits RLAR, HRAR, AGE, BACE1, AChE and BChE with IC50s of 0.30 µM, 0.17 µM, 17.89 µg/mL, 10.98 µM, 8.37 µM and 8.21 µM, respectively.
|
-
- HY-101762
-
|
TyK2-IN-2
|
JAK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
TyK2-IN-2 (Compoud 18) is a potent and selective TYK2 inhibitor with IC50s of 7 nM, 0.1 μM and 0.05 μM for TYK2 JH2, IL-23 and IFNα, respectively. TyK2-IN-2 also inhibits phosphodiesterase 4 (PDE4) with an IC50 of 62 nM. TyK2-IN-2 can be used for the research of inflammatory and autoimmune diseases.
|
-
- HY-N2309
-
-
- HY-P1348
-
-
- HY-P1363
-
-
- HY-131262
-
|
Hydroxychloroquine Impurity E
4-[(7-Chloro-4-quinolinyl)Amino]-1-pentanol
|
Others
|
Others
|
|
Hydroxychloroquine Impurity E is the impurity of Hydroxychloroquine. Hydroxychloroquine is a synthetic antimalarial agent which can also inhibit Toll-like receptor 7/9 (TLR7/9) signaling. Hydroxychloroquine is efficiently inhibits SARS-CoV-2 infection in vitro.
|
-
- HY-Y0127
-
-
- HY-101949
-
-
- HY-100714A
-
|
D-AP5
D-APV; D-2-Amino-5-phosphonovaleric acid
|
iGluR
|
Neurological Disease
|
|
D-AP5 (D-APV) is a selective and competitive NMDA receptor antagonist with a Kd of 1.4 μM. D-AP5 (D-APV) inhibits the glutamate binding site of NMDA receptors.
|
-
- HY-N4237
-
|
Saikogenin D
|
Prostaglandin Receptor
Potassium Channel
|
Inflammation/Immunology
|
|
Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca 2+]i due to Ca 2+ release from intracellular stores.
|
-
- HY-14602
-
|
Tramiprosate
Homotaurine; 3-Amino-1-propanesulfonic acid
|
Amyloid-β
|
Cancer
|
|
Tramiprosate is a small, orally-administered compound that binds to soluble Aβ and reduces amyloid aggregation and subsequent deposition
target: Aβ
In vitro: Tramiprosate provides neuroprotection against Aβ-induced neurotoxicity in neuronal and mouse organotypic hippocampal cultures, and reverses Aβ-induced long-term potentiation (LTP) inhibition in rat hippocampus, in part, through activation of β-aminobutyric acid A (GABA-A) receptors.
|
-
- HY-133126
-
-
- HY-101981
-
|
Uridine 5'-monophosphate
5'-Uridylic acid
|
Endogenous Metabolite
|
Others
|
|
Uridine 5'-monophosphate (5'-Uridylic acid), a monophosphate form of UTP, can be acquired either from a de novo pathway or degradation products of nucleotides and nucleic acids in vivo and is a major nucleotide analogue in mammalian milk.
|
-
- HY-P0122
-
|
iRGD peptide
c(CRGDKGPDC)
|
Integrin
|
Cancer
|
|
iRGD peptide is a 9-amino acid cyclic peptide, triggers tissue penetration of drugs by first binding to av integrins, then proteolytically cleaved in the tumor to produce CRGDK/R to interact with neuropilin-1, and has tumor-targeting and tumor-penetrating properties.
|
-
- HY-P1362
-
|
β-Amyloid (42-1), human
Amyloid β Peptide (42-1)(human)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (42-1), human is the inactive form of Amyloid β Peptide (1-42). Amyloid β Peptide (1-42) is a 42-amino acid peptide which plays a key role in the pathogenesis of Alzheimer disease.
|
-
- HY-112136
-
|
TAO Kinase inhibitor 1
|
Others
|
Cancer
|
|
TAO Kinase inhibitor 1 (compound 43) is a selective, ATP-competitive thousand-and-one amino acid kinases (TAOK) inhibitor with IC50s of 11 to 15 nM for TAOK1 and 2, respectively. TAO Kinase inhibitor 1 delays mitosis and induces mitotic cell death.
|
-
- HY-N0666
-
-
- HY-Y1139
-
-
- HY-P1595
-
-
- HY-P1818
-
-
- HY-Y0511
-
-
- HY-113232
-
-
- HY-B2145
-
|
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-101664
-
|
Ilaprazole
IY-81149
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) is an orally active proton pump inhibitor. Ilaprazole irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of pump inhibitory activity of 6 μM in rabbit parietal cell preparation. Ilaprazole is used for the research of gastric ulcers. Ilaprazole is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-133126A
-
-
- HY-N5057
-
|
Przewalskinic acid A
|
Others
|
Cardiovascular Disease
|
|
Przewalskinic acid A is a rare, water-soluble phenolic acid thus far only found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion.
|
-
- HY-N0511
-
|
Aristolochic acid B
|
Others
|
Cancer
|
|
Aristolochic acid B is one of the major components of Aristolochic acids (AA) which are natural products derived from taxa in the Aristolochiaceae. Aristolochic acid is known to be a potent mutagen and carcinogen. Aristolochic acid B showes more carcinogenic risk than Aristolochic acid A in vivo.
|
-
- HY-P1841
-
-
- HY-P1179
-
-
- HY-N0454
-
-
- HY-B1000
-
-
- HY-101409
-
-
- HY-113080
-
-
- HY-P1601
-
-
- HY-101404
-
-
- HY-N0130
-
-
- HY-113380
-
-
- HY-116100A
-
-
- HY-129357
-
-
- HY-P1179A
-
-
- HY-101708
-
-
- HY-N0658A
-
-
- HY-104026
-
-
- HY-N0394
-
-
- HY-W002292
-
-
- HY-113379
-
-
- HY-W010388
-
-
- HY-N0326
-
-
- HY-Y0444
-
|
D-Tyrosine
|
Tyrosinase
|
Metabolic Disease
|
|
D-Tyrosine is the D-isomer of tyrosine. D-Tyrosine negatively regulates melanin synthesis by inhibiting tyrosinase activity. D-Tyrosine inhibits biofilm formation and trigger the self-dispersal of biofilms without suppressing bacterial growth.
|
-
- HY-112653A
-
|
(±)8-HETE
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(±)8-HETE is one of the six monohydroxy fatty acids produced by the non-enzymatic oxidation of arachidonic acid (HY-109590). The biological activity of (±)8-HETE is likely to resemble that of its constituent enantiomers (8(R)-HETE and 8(S)-HETE).
|
-
- HY-N0623
-
-
- HY-P1895
-
-
- HY-N0230
-
-
- HY-P1903
-
-
- HY-13662
-
-
- HY-131146
-
|
AMOZ
3-Amino-5-morpholinomethyl-2-oxazolidone
|
Antibiotic
|
Infection
|
|
AMOZ, a tissue bound metabolite of Furaltadone, Furaltadone is a synthetic nitrofuran antibiotic widely used
|
-
- HY-117145
-
|
Thiophene-2
TP2
|
Bacterial
|
Infection
|
|
Thiophene-2 (TP2) is a specific polyketide synthase 13 (Pks13) inhibitor. Thiophene-2 inhibits mycolic acid biosynthesis and rapidly leads to mycobacterial cell death. Thiophene-2 is active against Mycobacterium tuberculosis with a MIC value of 1 μM, and has potent anti-tuberculosis activity.
|
-
- HY-P0316
-
|
TP508
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-W017018
-
-
- HY-N0667
-
-
- HY-W017462
-
-
- HY-N0666C
-
-
- HY-N0486
-
-
- HY-P1484
-
-
- HY-16714
-
|
4-Azido-L-phenylalanine
p-Azidophenylalanine; p-Azido-L-phenylalanine
|
Others
|
Others
|
|
4-Azido-L-phenylalanine is an unnatural amino acid, which is used as an effective vibrational reporter of local protein environments.
|
-
- HY-16714A
-
|
4-Azido-L-phenylalanine hydrochloride
p-Azidophenylalanine hydrochloride; p-Azido-L-phenylalanine hydrochloride
|
Others
|
Others
|
|
4-Azido-L-phenylalanine hydrochloride is an unnatural amino acid, which is used as an effective vibrational reporter of local protein environments.
|
-
- HY-N0658
-
-
- HY-112251
-
-
- HY-P1565
-
|
Transdermal Peptide Disulfide
TD 1 Disulfide(peptide)
|
Na+/K+ ATPase
|
Inflammation/Immunology
|
|
Transdermal Peptide Disulfide (TD 1 Disulfide(peptide)) is a 11-amino acid peptide, binds toNa +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide can enhance the transdermal delivery of many macromolecules.
|
-
- HY-100348
-
|
EPI-001
|
Androgen Receptor
PPAR
Apoptosis
|
Cancer
|
|
EPI-001 is a selective inhibitor of Androgen Receptor (AR), and it can inhibit transactivation of the AR amino-terminal domain (NTD), with an IC50 of 6 μM. EPI-001 is also a selective modulator of PPARγ. EPI-001 exhibits anti-tumor activity in vitro and in vivo.
|
-
- HY-N3945
-
|
Glaucine
O,O-Dimethylisoboldine; S-(+)-Glaucine; NSC 34396
|
Phosphodiesterase (PDE)
Calcium Channel
Adrenergic Receptor
Dopamine Receptor
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Glaucine (O,O-Dimethylisoboldine) is an alkaloid isolated from Glaucium flavum Crantz with antitussive, bronchodilation and anti-inflammatory properties. Glaucine is a selective and orally active phosphodiesterase 4 (PDE4) inhibitor with Kis of 3.4 µM in human bronchus and polymorphonuclear leukocytes. Glaucine is also a non-selective α-adrenoceptor antagonist, a Ca 2+ entry blocker, and a weak dopamine D1 and D2 receptor antagonist. Glaucine has antioxidative and antiviral activities.
|
-
- HY-107522
-
|
DL-TBOA
|
EAAT2
|
Neurological Disease
|
|
DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively.
|
-
- HY-78961
-
-
- HY-N7109
-
|
Erucic acid
|
PI3K
Endogenous Metabolite
|
Neurological Disease
|
|
Erucic acid, a monounsaturated fatty acid (MUFA), is isolated from the seed of Raphanus sativus L. Erucic acid can readily cross the blood-brain barrier (BBB), it has been reported to normalize the accumulation of very long-chain fatty acids in the brain. Erucic acid can improve cognitive impairment and be effective against dementia
.
|
-
- HY-D0835
-
|
Hydroxylapatite
Hydroxyapatite
|
Others
|
Others
|
|
Hydroxylapatite (Hydroxyapatite) is a naturally occurring calcium phosphate which is a major mineral component of bone and teeth bones. Nano-scale Hydroxylapatite particles are increasingly being used as carriers for controlled and targeted delivery of bioactive agents like drugs, proteins, and nucleic acids due to their high porosity, negative charge, and biodegradability .
|
-
- HY-W016443
-
-
- HY-100803
-
-
- HY-W016823
-
-
- HY-P1490
-
-
- HY-P0173A
-
|
Chlorotoxin
|
Chloride Channel
|
Cancer
|
|
Chlorotoxin is a 36 amino-acid peptide from the venom of the Israeli scorpion Leiurus quinquestriatus with anticancer activity. Chlorotoxin is a chloride channel blocker.
|
-
- HY-W007606
-
-
- HY-P0316A
-
|
TP508 TFA
|
Thrombin
NO Synthase
|
Cardiovascular Disease
|
|
TP508 TFA is a 23-amino acid nonproteolytic thrombin peptide that represents a portion of the receptor-binding domain of thrombin molecule. TP508 TFA activates endothelial NO synthase (eNOS) and stimulates production of NO in human endothelial cells. TP508 TFA activates endothelial cells and stem cells to revascularize and regenerate tissues.
|
-
- HY-B1478
-
-
- HY-N6998
-
|
Paederosidic acid
|
Apoptosis
|
Cancer
|
|
Paederosidic acid is isolated from P. scandens with anticancer and anti‐inflammation activities. Paederosidic acid inhibits lung caner cells via inducing mitochondria-mediated apoptosis.
|
-
- HY-124527
-
|
HET0016
|
Cytochrome P450
|
Cardiovascular Disease
|
|
HET0016 is a potent and selective 20-hydroxyeicosatetraenoic acid (20-HETE) synthase inhibitor, with IC50 values of 17.7 nM, 12.1 nM and 20.6 nM for recombinant CYP4A1-, CYP4A2- and CYP4A3-catalyzed 20-HETE synthesis, respectively. HET0016 also is a selective CYP450 inhibitor, which has been shown to inhibit angiogenesis and tumor growth.
|
-
- HY-B0033
-
|
Vigabatrin hydrochloride
γ-Vinyl-GABA hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
|
-
- HY-15399
-
|
Vigabatrin
γ-Vinyl-GABA
|
GABA Receptor
|
Neurological Disease
|
|
Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
|
-
- HY-113466
-
|
4-Hydroxynonenal
4-HNE
|
Aldehyde Dehydrogenase (ALDH)
Endogenous Metabolite
|
Cancer
Neurological Disease
Cardiovascular Disease
|
|
4-Hydroxynonenal (4-HNE) is an α,β unsaturated hydroxyalkenal and an oxidative/nitrosative stress biomarker. 4-Hydroxynonenal is a substrate and an inhibitor of acetaldehyde dehydrogenase 2 (ALDH2). 4-Hydroxynonenal can modulate a number of signaling processes mainly through forming covalent adducts with nucleophilic functional groups in proteins, nucleic acids, and membrane lipids. 4-Hydroxynonenal plays an important role in cancer through mitochondria.
|
-
- HY-101903A
-
|
BMS-309403 sodium
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
|
BMS-309403 sodium is a potent, orally active, and selective adipocyte fatty acid binding protein (aFABP, aP2) with a Ki of <2 nM, 250, and 350 nM for aFABP, muscle FABP (mFABP), and epidermal FABP (eFABP), respectively. BMS-309403 sodium interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 sodium improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-101903
-
|
BMS-309403
|
FABP
|
Metabolic Disease
Cardiovascular Disease
|
|
BMS-309403 is a potent, orally active and selective adipocyte fatty acid binding protein (aFABP, aP2) with a Ki of <2 nM, 250, 350 nM for aFABP, muscle FABP (mFABP), and epidermal FABP (eFABP), respectively. BMS-309403 interacts with the fatty-acid-binding pocket within the interior of the protein and competitively inhibits the binding of endogenous fatty acids. BMS-309403 improves endothelial function in apolipoprotein E-deficient mice and in cultured human endothelial cells.
|
-
- HY-135960
-
|
BO-264
|
FGFR
Apoptosis
|
Cancer
|
|
BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 specifically blocks the function of FGFR3-TACC3 fusion protein. BO-264 induces spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis. BO-264 has broad-spectrum antitumor activity.
|
-
- HY-N1478
-
|
Gardenoside
|
Others
|
Neurological Disease
|
|
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
|
-
- HY-103355
-
|
YM022
|
CCR
|
Metabolic Disease
|
|
YM022 is a highly potent, selective and orally active gastrin/cholecystokinin (CCK)-B receptor (CCK-BR) antagonist. YM022 shows the Ki values of 68 pM and 63 nM for CCK-B and CCK-A receptor, respectively. YM022 can inhibit gastrin-induced gastric acid secretion and histidine decarboxylase activation in vivo.
|
-
- HY-19528
-
|
SAH
SAH (S-Adenosylhomocysteine)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
SAH is an amino acid derivative and a modulartor in several metabolic pathways. It is an intermediate in the synthesis of cysteine and adenosine. SAH is an inhibitor for METTL3-METTL14 heterodimer complex (METTL3-14) with an IC50 of 0.9 µM.
|
-
- HY-107383
-
-
- HY-W040245
-
-
- HY-135652
-
|
Hexyl gallate
Hexyl 3,4,5-trihydroxybenzoate
|
Bacterial
Parasite
|
Infection
|
|
Hexyl gallates (Hexyl 3,4,5-trihydroxybenzoate) shows antibacterial activity and inhibits the production of rhamnolipid and pyocyanin by inhibiting RhlR. Hexyl gallate, a alkyl ester derivative of gallic acid, exhibits potent antimalarial activity against Plasmodium falciparum, with IC50 of 0.11 mM.
|
-
- HY-P1565A
-
|
Transdermal Peptide Disulfide TFA
TD 1 Disulfide(peptide) TFA
|
Na+/K+ ATPase
|
Others
|
|
Transdermal Peptide Disulfide TFA (TD 1 Disulfide(peptide) TFA) is a 11-amino acid peptide, binds to Na +/K +-ATPase beta-subunit (ATP1B1), and mainly interacts with the C-terminus of ATP1B1. Transdermal Peptide Disulfide TFA can enhance the transdermal delivery of many macromolecules.
|
-
- HY-B0133
-
|
Natamycin
Pimaricin
|
Fungal
Endogenous Metabolite
Antibiotic
|
Infection
|
|
Natamycin (Pimaricin) is a macrolide antibiotic agent produced by several Streptomyces strains. Natamycin inhibits the growth of fungi via inhibition of amino acid and glucose transport across the plasma membrane. Natamycin is a food preservative, an antifungal agent in agriculture, and is widely used for fungal keratitis research.
|
-
- HY-P1293
-
|
Conantokin G
|
iGluR
|
Neurological Disease
|
|
Conantokin G, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G has neuroprotective properties.
|
-
- HY-16007
-
|
(-)-Hydroxycitric acid
Garcinia acid
|
ATP Citrate Lyase
|
Metabolic Disease
|
|
(-)-Hydroxycitric acid (Garcinia acid) is the principal acid of fruit rinds of Garcinia cambogia. (-)-Hydroxycitric acid is a potent and competitive inhibitor of ATP citrate lyase. (-)-Hydroxycitric acid suppresses the fatty acid synthesis, lipogenesis, food intake, and induced weight loss.
|
-
- 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-B1295
-
|
Citric acid trilithium salt tetrahydrate
Lithium citrate tribasic tetrahydrate; Trilithium citrate tetrahydrate
|
Bacterial
|
Infection
|
|
Citric acid trilithium salt tetrahydrate (Lithium citrate tribasic tetrahydrate) is a pharmaceutical and construction material, used in HPLC gradient elution for quantitative amino acid analysis.
|
-
- HY-N0391
-
|
L-Citrulline
|
Endogenous Metabolite
|
Others
|
|
L-Citrulline is an amino acid derived from ornithine in the catabolism of proline or glutamine and glutamate, or from l-arginine via arginine-citrulline pathway.
|
-
- HY-N0384
-
-
- HY-W012382
-
-
- 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-P1534
-
-
- HY-P1469
-
-
- HY-B0946
-
|
Sulfamonomethoxine
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
|
-
- HY-Y1718
-
|
Tridecanoic acid
N-Tridecanoic acid
|
Endogenous Metabolite
Bacterial
|
Infection
Metabolic Disease
|
|
Tridecanoic acid (N-Tridecanoic acid), a 13-carbon medium-chain saturated fatty acid, can serve as an antipersister and antibiofilm agent that may be applied to research bacterial infections. Tridecanoic acid inhibits Escherichia coli persistence and biofilm formation.
|
-
- HY-136458
-
|
3-ANOT
3-Amino-5-nitro-o-toluamide
|
Parasite
|
Infection
|
|
3-ANOT is a metabolite of Dinitolmide (a nitroamide coccidiostat commonly used in poultry production).
|
-
- HY-Y0445A
-
|
Sodium dichloroacetate
|
PDHK
Reactive Oxygen Species
NKCC
Apoptosis
|
Cancer
|
|
Sodium dichloroacetate is a metabolic regulator in cancer cells' mitochondria with anticancer activity. Sodium dichloroacetate inhibits PDHK, resulting in decreased lactic acid in the tumor microenvironment. Sodium dichloroacetate increases reactive oxygen species (ROS) generation and promotes cancer cell apoptosis. Sodium dichloroacetate also works as NKCC inhibitor.
|
-
- HY-N0229
-
-
- HY-135094
-
-
- HY-I1060
-
|
L-Alloisoleucine
(3R)-LS-Isoleucine; L-Allo-isoleucine
|
Endogenous Metabolite
|
Others
|
|
L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
|
-
- HY-N7031
-
|
(±)-Vasicine
(±)-Peganine
|
Proton Pump
|
Inflammation/Immunology
|
|
(±)-Vasicine is the racemate of Vasicine. Vasicine (Peganine), isolated from Peganum harmala seeds, significantly inhibits H +-K +-ATPase activity in vitro with an IC50 of 73.47 μg/mL. Anti-ulcer activity. Vasicine shows significant anti-secretory, antioxidant and cytoprotective effect.
|
-
- HY-12812
-
|
Autotaxin modulator 1
|
Phosphodiesterase (PDE)
|
Cancer
Neurological Disease
|
|
Autotaxin modulator 1 is an autotaxin (ATX) enzyme inhibitor, extracted from patent WO 2014018881 A1, Compound Example 12b. Autotaxin modulator 1 is expected to be useful for researching demyelination due to injury or disease, as well as for researching proliferative disorders such as cancer.
|
-
- HY-N7539
-
|
Cognac oil
|
Others
|
Metabolic Disease
|
|
Cognac oil, mainly found in wine lees, has unique fatty acid profiles, including Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), Oleic acid (8.3%) and other fatty acids. Cognac oil leads to a general increase in the permeation of R6G (Rhodamine 6G) across all the membranes.
|
-
- HY-N0510
-
|
Aristolochic acid A
Aristolochic acid I; TR 1736
|
NF-κB
|
Cancer
|
|
Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines.
|
-
- HY-B1789A
-
-
- HY-13443
-
-
- HY-114381
-
-
- HY-13443A
-
-
- HY-112052
-
|
Aminomalonic acid
|
Endogenous Metabolite
|
Cancer
|
|
Aminomalonic acid is an amino endogenous metabolite, acts as a strong inhibitor of L-asparagine synthetase from Leukemia 5178Y/AR (Ki= 0.0023 M) and mouse pancreas (Ki= 0.0015 M) in vitro. Aminomalonic acid is a potential biomarker to discriminate between different stages of melanoma metastasis.
|
-
- HY-P1293A
-
|
Conantokin G TFA
|
iGluR
|
Neurological Disease
|
|
Conantokin G TFA, a 17-amino-acid peptide, is a potent, selective and competitive antagonist of N-methyl-D-aspartate (NMDA) receptors. Conantokin G TFA inhibits NMDA-evoked currents in murine cortical neurons with an IC50 of 480 nM. Conantokin G TFA has neuroprotective properties.
|
-
- HY-B0946S
-
|
Sulfamonomethoxine D4
|
Bacterial
|
Infection
|
|
Sulfamonomethoxine D4 is a deuterium labeled Sulfamonomethoxine. Sulfamonomethoxine is a long acting sulfonamide antibacterial agent, used in blood kinetic studies,and blocks the synthesis of folic acid by inhibiting synthetase of dihydropteroate.
|
-
- HY-12511
-
|
SKF-86002
|
p38 MAPK
|
Inflammation/Immunology
|
|
SKF-86002 is an orally active p38 MAPK inhibitor, with anti-inflammatory, anti-arthritic and analgesic activities. SKF-86002 inhibits lipoxygenase- and cyclooxygenase-mediated metabolism of arachidonic acid.
|
-
- HY-107412
-
|
Proteasome inhibitor IX
PS-IX; AM114
|
Proteasome
|
Cancer
|
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
|
-
- HY-107613
-
|
R 59-022
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
|
R 59-022 (DKGI-I) is a diacylglycerol kinase inhibitor (IC50=2.8 μM). R 59-022 is a 5-HTR antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-W012499
-
-
- HY-P1462
-
-
- HY-W015240
-
-
- HY-N0470
-
-
- HY-N0293
-
|
Paeoniflorin
Peoniflorin
|
HSP
|
Neurological Disease
|
|
Paeoniflorin (Peoniflorin), a heat shock protein-inducing compound and a pinane monoterpene glycoside with various bioactivities, such as anticancer effects, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, reducing blood viscosity and anti-inflammatory activity. paeoniflorin protects PC12 cells from MPP + and acidic damage via autophagic pathway.
|
-
- HY-W010629
-
|
2-Chloroacetamide
|
Bacterial
|
Infection
|
|
2-Chloroacetamide is a preservative and is a herbicide for both uplands and paddy fields. 2-Chloroacetamide is a biocide in agriculture, glues, paints and coatings. 2-Chloroacetamide inhibits very-long-chain fatty acid elongase.
|
-
- HY-N3894
-
-
- HY-133595
-
-
- HY-14850
-
|
Sograzepide
Netazepide; YF 476; YM-220
|
Cholecystokinin Receptor
|
Metabolic Disease
Endocrinology
|
|
Sograzepide (Netazepide; YF 476; YM-220) is an extremely potent , highly selective and orally active Gastrin/CCK-B antagonist with an IC50 value of 0.1 nM, has inhibitory effect on Gastrin/CCK-A activity with an IC50 of 502 nM. Sograzepide (Netazepide; YF 476; YM-220) replaces the specific binding of [125I]CCK-8 to the rat brain, cloned canine and cloned human Gastrin/CCK-B receptors, with Ki values of 0.068, 0.62 and 0.19 nM, respectively.
|
-
- HY-Y1362
-
-
- HY-W015410
-
|
Disodium succinate
|
Others
|
Metabolic Disease
|
|
Disodium succinate is the disodium salt of Succinic acid. Succinic acid is an intermediate product of the tricarboxylic acid cycle, as well as one of fermentation products of anaerobic metabolism.
|
-
- HY-N3010
-
-
- HY-76547
-
|
p-Toluic acid
4-Methylbenzoic acid
|
Endogenous Metabolite
|
Others
|
|
p-Toluic acid (4-Methylbenzoic acid) is a substituted benzoic acid and can be used as an intermediate for the synthesis of para-aminomethylbenzoic acid (PAMBA), p-tolunitrile, etc.
|
-
- HY-N2078
-
|
Yamogenin
Neodiosgenin
|
LXR
|
Metabolic Disease
|
|
Yamogenin (Neodiosgenin) is a diastereomer of diosgenin. Yamogenin (Neodiosgenin) antagonizes the activation of the liver X receptor (LXR) in luciferase ligand assay. Yamogenin (Neodiosgenin) inhibits triacylglyceride (TG) accumulation through the suppression of gene expression of fatty acid synthesis in HepG2 hepatocytes.
|
-
- HY-N0122
-
-
- HY-N6848
-
|
Acetylseneciphylline N-oxide
|
Others
|
Infection
|
|
Acetylseneciphylline N-oxide is a pyrrolizine alkaloid that is seneciphylline in which the hydroxy hydrogen is replaced by an acetyl group and the tertiary amino function is oxidised to the corresponding N-oxide.
|
-
- HY-P1170
-
-
- HY-P1462A
-
-
- HY-103228
-
-
- HY-136037
-
-
- HY-B1099
-
|
Hycanthone
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
|
-
- 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-122337
-
|
Streptolydigin
Portamycin
|
DNA/RNA Synthesis
Bacterial
|
Infection
|
|
Streptolydigin (Portamycin) is a 3-acetyltetramic acid antibiotic and a potent bacterial RNA polymerase inhibitor with a Ki of 18 μM and a Kd of 15 μM. Streptolydigin inhibits RNA synthesis by binding to RNA polymerase and does not inhibit eukaryotic RNA polymerases. Streptolydigin possess potent antibacterial activity, particularly against anaerobes and some Gram-positive aerobes.
|
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-140245
-
-
- HY-P0288
-
-
- 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-N2511
-
|
Trimyristin
|
AChE
Phosphatase
Endogenous Metabolite
|
Metabolic Disease
|
|
Trimyristin, an active molluscicidal component of Myristica fragrans Houtt, significantly inhibits acetylcholinesterase (AChE), acid and alkaline phosphatase (ACP/ALP) activities in the nervous tissue of Lymnaea acuminata. IC50s of Trimyristin against AChE, ACP, and ALP are 0.11, 0.16 and 0.18 mM, respectively.
|
-
- HY-119435
-
|
Triallate
|
Others
|
Others
|
|
Triallate is a selective preemergence herbicide for the control of wild oats in barley, spring wheat, Durum wheat, winter wheat, and sugar beets. Triallate inhibits fatty acid elongation and surface lipid (wax) biosynthesis.
|
-
- HY-W010382
-
|
Oxaloacetic acid
2-Oxosuccinic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Oxaloacetic acid (2-Oxosuccinic acid) is a metabolic intermediate involved in several ways, such as citric acid cycle, gluconeogenesis, the urea cycle, the glyoxylate cycle, amino acid synthesis, and fatty acid synthesis.
|
-
- HY-N0469
-
-
- HY-P0199
-
-
- HY-115521
-
|
Jarin-1
|
Others
|
Others
|
|
Jarin-1 is a jasmonic acid-amido synthetase (JAR1) inhibitor with an IC50 of 3.8 μM. Jarin-1 specific inhibits bioactive JA (jasmonoyl-isoleucine, JA-Ile) biosynthesis in Arabidopsis and other plants.
|
-
- HY-14165
-
-
- HY-112683
-
|
V-9302
|
Others
|
Cancer
|
|
V-9302 is a competitive antagonist of transmembrane glutamine flux. V-9302 selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
|
-
- HY-112683A
-
|
V-9302 hydrochloride
|
Others
|
Cancer
|
|
V-9302 hydrochloride is a competitive antagonist of transmembrane glutamine flux. V-9302 hydrochloride selectively and potently targets the amino acid transporter ASCT2 (SLC1A5). V-9302 hydrochloride inhibits ASCT2-mediated glutamine uptake (IC50=9.6 µM) in HEK-293 cells.
|
-
- HY-103700B
-
|
(Rac)-Azide-phenylalanine
|
Others
|
Others
|
|
(Rac)-Azide-phenylalanine is a racemate of Azide-phenylalanine. Azide-phenylalanine is a phenylalanine derivative and a non-natural amino acid. Azide-phenylalanine can be site-specifically incorporated into proteins and used to label proteins.
|
-
- HY-B0342
-
|
Meglumine
Methylglucamine; Meglumin; Methylglucamin
|
Others
|
Others
|
|
Meglumine (Methylglucamine) is an amino sugar derived from sorbitol. Meglumine is often used as an excipient in pharmaceuticals and in conjunction with iodinated compounds in contrast media such as diatrizoate meglumine and iodipamide meglumine.
|
-
- HY-140532
-
-
- HY-P1082
-
-
- HY-W016781
-
|
D-Arginine
H-D-Arg-OH
|
Others
|
Others
|
|
D-arginine (H-D-Arg-OH) is the D-isomer of arginine. Arginine is an α-amino acid that is used in the biosynthesis of proteins. D-Arginine is an inactive form of L-arginine.
|
-
- HY-135747
-
|
Gut restricted-7
GR-7
|
Bacterial
|
Infection
|
|
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice.
|
-
- HY-P1674A
-
|
Murepavadin TFA
POL7080 TFA
|
Bacterial
Antibiotic
|
Infection
|
|
Murepavadin (TFA), a 14-amino-acid cyclic peptide, is a highly potent, specific antibiotic for the treatment of bacterial infections caused by Pseudomonas aeruginosa. Murepavadin (TFA) targets the lipopolysaccharide transport portin D .
|
-
- HY-P1519B
-
-
- HY-P1519
-
-
- HY-P1082A
-
-
- HY-15072
-
|
Zonampanel
YM 872
|
iGluR
|
Metabolic Disease
|
|
Zonampanel (YM 872) is a selective antagonist of the glutamate receptor subtype, α-amino-3-hydroxy-5-methylisoxazole-4-propionic acid (AMPA) receptor.
|
-
- HY-B0762
-
-
- HY-14380
-
|
PF-3845
|
FAAH
Autophagy
|
Inflammation/Immunology
Cancer
|
|
PF-3845 is a potent, selective, irreversible and orally active inhibitor of fatty acid amide hydrolase (FAAH), with a Ki of 0.23 µM. PF-3845 is a covalent inhibitor that carbamylates FAAH's serine nucleophile. PF-3845 can reduce pain sensation, inflammation, and anxiety/depression without substantial effects on motility or cognition.
|
-
- HY-15870
-
|
SR 11302
|
Others
|
Cancer
Inflammation/Immunology
|
|
SR 11302 is an activator protein-1 (AP-1) transcription factor inhibitor. SR 11302 is a retinoid that specifically inhibits AP-1 activity without activating the transcription of retinoic acid response element (RARE).
|
-
- HY-121450
-
|
Lavoltidine
Loxtidine; AH-234844
|
Histamine Receptor
|
Cancer
|
|
Lavoltidine (Loxtidine) is an an orally active, irreversible and highly potent histamine H2-receptor antagonist. Lavoltidine strongly inhibits gastric acid secretion and also induces hypergastrinemia.
|
-
- HY-N0121
-
|
Sesamin
|
Others
|
Neurological Disease
|
|
Sesamin, abundant lignan found in sesame oil, is a potent and selective delta 5 desaturase inhibitor in polyunsaturated fatty acid biosynthesis. Sesamin exerts effective neuroprotection against cerbral ischemia.
|
-
- HY-P1280
-
|
Margatoxin
|
Potassium Channel
|
Neurological Disease
|
|
Margatoxin, an alpha-KTx scorpion toxin, is a high affinity inhibitor of Kv1.3 (Kd=11.7 pM). Margatoxin inhibits the Kv1.2 (Kd=6.4 pM) and Kv1.1 (Kd=4.2 nM). Margatoxin, a 39 amino-acid-long peptide, is isolated from the venom of the scorpion Centruroides margaritatus and widely used in ion channel research.
|
-
- HY-14874
-
|
Topiroxostat
FYX-051
|
Xanthine Oxidase
Cytochrome P450
|
Metabolic Disease
|
|
Topiroxostat (FYX-051) is a potent and orally active xanthine oxidoreductase (XOR) inhibitor with an IC50 value of 5.3 nM and a Ki value of 5.7 nM. Topiroxostat exhibits weak CYP3A4-inhibitory activity (18.6%). Topiroxostat has the potential for hyperuricemia treatment.
|
-
- HY-116214
-
|
Cyprodinil
|
Fungal
Androgen Receptor
|
Infection
Endocrinology
|
|
Cyprodinil is an anilinopyrimidine broad-spectrum fungicide that inhibits the biosynthesis of methionine in phytopathogenic fungi. Cyprodinil inhibits mycelial cell growth of B. cinerea, P. herpotrichoides, and H. oryzae on amino acid-free media (IC50s=0.44, 4.8, and 0.03 µM, respectively). Cyprodinil acts as an androgen receptor (AR) agonist (EC50=1.91 µM) in the absence of the AR agonist DHT and inhibits the androgenic effect of DHT (IC50=15.1 µM).
|
-
- HY-43470
-
-
- HY-125686
-
|
Beesioside Q
|
Others
|
Others
|
|
Beesioside Q is a oleanolic acid triterpene saponin isolated from the rhizome of Beesia calthaefolia (Maxim.) Ulbr.
|
-
- HY-135801
-
|
Arachidonyl alcohol
|
Others
|
Metabolic Disease
|
|
Arachidonyl alcohol is a long-chain primary fatty alcohol. Arachidonyl alcohol is used as a substrate for the production of several ether lipids possessing beneficial functions.
|
-
- HY-133593
-
-
- HY-106579S
-
-
- HY-107395
-
-
- HY-N7606
-
-
- HY-129467
-
|
Minerval
2-Hydroxyoleic acid; 2-OHOA
|
Apoptosis
|
Cancer
|
|
Minerval (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasma membrane and alters lipid organization. Minerval has anti-tumor effect.
|
-
- HY-113478
-
|
3β-Ursodeoxycholic acid
Isoursodeoxycholic acid
|
Others
|
Metabolic Disease
|
|
3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) is a bile acid. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) shows good tolerance and well intestinal absorption by oral adminstation. 3β-Ursodeoxycholic acid (Isoursodeoxycholic acid) can be isomerized by intestinal and hepatic enzymes to yield UDCA.
|
-
- 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-129770A
-
|
D-Methionine sulfoxide hydrochloride
|
Others
|
Metabolic Disease
|
|
D-methionine sulfoxide hydrochloride is the D-isomer of Methionine sulfoxide hydrochloride. Methionine sulfoxide is an oxidation product of methionine. Methionine is the limiting amino acid in milk or leguminous proteins, which is easily oxidized during the course of storage or processing.
|
-
- HY-129770
-
|
D-Methionine sulfoxide
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-methionine sulfoxide is the D-isomer of Methionine sulfoxide. Methionine sulfoxide is an oxidation product of methionine. Methionine is the limiting amino acid in milk or leguminous proteins , which is easily oxidized during the course of storage or processing.
|
-
- HY-N3848
-
-
- HY-Y0337
-
|
L-Cysteine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Cysteine is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine suppresses ghrelin and reduces appetite in rodents and humans.
|
-
- HY-Y0337A
-
|
L-Cysteine hydrochloride
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Cysteine hydrochloride is a conditionally essential amino acid, which acts as a precursor for biologically active molecules such as hydrogen sulphide (H2S), glutathione and taurine. L-Cysteine hydrochloride suppresses ghrelin and reduces appetite in rodents and humans.
|
-
- HY-N0305
-
-
- HY-N7062
-
|
JNJ-1661010
Takeda-25
|
FAAH
|
Neurological Disease
|
|
JNJ-1661010 (Takeda-25) a potent and selective fatty acid amide hydrolase (FAAH) inhibitor with IC50s of 34 and 33 nM for rat FAAH and human FAAH, respectively. JNJ-1661010 can cross the blood-brain barrier and used as broad-spectrum analgesics.
|
-
- HY-135425
-
|
10,12-Tricosadiynoic acid
|
Acyltransferase
|
Metabolic Disease
|
|
10,12-Tricosadiynoic acid is a highly specific, selective, high affinity and orally active acyl-CoA oxidase-1 (ACOX1) inhibitor. 10,12-Tricosadiynoic acid can treat high fat diet- or obesity-induced metabolic diseases by improving mitochondrial lipid and ROS metabolism.
|
-
- HY-P0256
-
-
- HY-111149A
-
|
PS372424 hydrochloride
|
CXCR
|
Inflammation/Immunology
|
|
PS372424 hydrochloride, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 hydrochloride prevents human T-cell migration in a humanized model of arthritic inflammation.
|
-
- HY-N6858
-
|
4-Hydroxyisoleucine
4-Hydroxy-L-isoleucine
|
Others
|
Metabolic Disease
|
|
4-Hydroxyisoleucine (4-Hydroxy-L-isoleucine) is an amino acid which can be extracted and purified from fenugreek seeds. 4-Hydroxyisoleucine (4-Hydroxy-L-isoleucine) displays an insulinotropic activity of great interest.
|
-
- HY-N0390
-
-
- HY-111149
-
|
PS372424
|
CXCR
|
Inflammation/Immunology
|
|
PS372424, a three amino-acid fragment of CXCL10, is a specific human CXCR3 agonist with anti-inflammatory activity. PS372424 prevents human T-cell migration in a humanized model of arthritic inflammation.
|
-
- HY-125801
-
|
3-Oxo-5β-cholanoic acid
Dehydrolithocholic acid; 3-oxoLCA
|
ROR
|
Inflammation/Immunology
|
|
3-Oxo-5β-cholanoic acid (Dehydrolithocholic acid), a bile acid metabolite, inhibits the diferentiation of TH17 cells by directly binding to the key transcription factor RORγt (Kd=1.13 μM).
|
-
- HY-P1418A
-
|
DPC-AJ1951 TFA
|
Thyroid Hormone Receptor
|
Endocrinology
|
|
DPC-AJ1951 TFA, a 14 amino acid peptide that acts as a potent agonist of the parathyroid hormone (PTH)/PTH-related peptide receptor (PPR) , and characterized its activity in ex vivo and in vivo assays of bone resorption.
|
-
- HY-P7060
-
|
NT 13
TPPT
|
iGluR
|
Neurological Disease
|
|
NT 13 (TPPT) is a tetrapeptide having the amino acid sequence L-threonyl-L-prolyl-L-prolyl-L-threonine amide. NT 13 is a partial N-methyl-D-aspartate receptor (NMDAR) agonist used in the study of depression, anxiety, and other related diseases.
|
-
- HY-P0256A
-
-
- HY-P1847A
-
-
- HY-P1340A
-
-
- HY-14739
-
|
Choline Fenofibrate
ABT-335
|
PPAR
COX
|
Cardiovascular Disease
|
|
Choline Fenofibrate (ABT-335) is the choline salt of Fenofibric acid (HY-B0760), which releases free fenofibric acid in the gastrointestinal tract. Fenofibric acid is a PPAR activator with antihyperlipidemic effect.
|
-
- HY-B1514
-
-
- HY-113437
-
-
- HY-130803
-
|
5-Methyl-5,6-dihydrouridine
|
Others
|
Cancer
|
|
5-Methyl-5,6-dihydrouridine is a minor constituent in the chromosomal RNA of the rat ascites tumor. 5-Methyl-5,6-dihydrouridine can be used for nucleic acid modification.
|
-
- HY-113437A
-
-
- 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-135103
-
|
Tauro-β-muricholic acid sodium
T-βMCA sodium
|
FXR
|
Cancer
|
|
Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM.
|
-
- HY-113147
-
-
- HY-W009082
-
|
Methyl behenate
Methyl docosanoate
|
Others
|
Others
|
|
Methyl behenate (Methyl docosanoate) is a naturally fatty acid methyl ester isolated from the plant of Aspidopterys obcordata Lemsl.
|
-
- HY-P1340
-
-
- HY-P2416
-
-
- HY-133022
-
|
trans-2-Undecenoic acid
(E)-2-Undecenoic acid; (E)-Undec-2-enoic acid
|
Others
|
Metabolic Disease
|
|
trans-2-Undecenoic acid ((E)-2-Undecenoic acid) is an α,β-unsaturated carboxylic acid and is characterized by acid dimers. The corresponding dimers are connected via intermolecular hydrogen bonds of the carboxylic groups C=O···H-O.
|
-
- HY-W005178
-
-
- HY-N7354
-
-
- HY-A0143
-
-
- HY-131967
-
|
CD73-IN-4
|
CD73
|
Cancer
Inflammation/Immunology
|
|
CD73-IN-4 is a potent and selective methylenephosphonic acid CD73 inhibitor, with an IC50 of 2.6 nM for human CD73. CD73-IN-4 is potential for the research of cancer immunology.
|
-
- HY-B0351
-
|
Taurine
2-Aminoethanesulfonic acid
|
Autophagy
Endogenous Metabolite
|
Metabolic Disease
|
|
Taurine, a sulphur-containing amino acid and an organic osmolyte involved in cell volume regulation, provides a substrate for the formation of bile salts, and plays a role in the modulation of intracellular free calcium concentration. Taurine has the ability to activate autophagy in adipocytes.
|
-
- HY-N0455
-
|
L-Arginine
(S)-(+)-Arginine
|
NO Synthase
Endogenous Metabolite
|
Cardiovascular Disease
|
|
L-Arginine ((S)-(+)-Arginine) is the substrate for the endothelial nitric oxide synthase (eNOS) to generate NO. L-Arginine is transported into vascular smooth muscle cells by the cationic amino acid transporter family of proteins where it is metabolized to nitric oxide (NO), polyamines, or L-proline.
|
-
- HY-75308
-
|
Azetidine-2-carboxylic acid
|
Others
|
Cancer
|
|
Azetidine-2-carboxylic acid is a non proteinogenic amino acid homologue of proline. Found in common beets. Azetidine-2-carboxylic acid can be misincorporated into proteins in place of proline in many species, including humans. Toxic and teratogenic agent.
|
-
- HY-P1770
-
|
Adrenomedullin (16-31), human
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (16-31), human is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
|
-
- HY-P1298
-
|
Sauvagine
|
CRFR
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Sauvagine, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine is effective at releasing ACTH from rat pituitary cells. Sauvagine possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
|
-
- HY-N0729
-
|
Linoleic acid
|
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
Linoleic acid is a common polyunsaturated (PUFA) is found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism .
|
-
- HY-N7512
-
|
Asimilobine
|
Dopamine Receptor
5-HT Receptor
Parasite
|
Cancer
Infection
|
|
Asimilobine is an aporphine isoquinoline alkaloid isolated from plant species of Magnolia obobata Thun. Asimilobine is a dopamine biosynthesis inhibitor and a serotonergic receptor antagonist. Asimilobine shows an antimalarial and anti-cancer activity.
|
-
- HY-21577
-
-
- HY-P1770A
-
|
Adrenomedullin (16-31), human TFA
|
CGRP Receptor
|
Cardiovascular Disease
|
|
Adrenomedullin (16-31), human TFA is amino acid residues 16-31 fragment of human adrenomedullin (hADM). Adrenomedullin has appreciable affinity for the CGRP1 receptor. Adrenomedullin (16-31), human TFA possesses pressor activity in the systemic vascular bed of the rat, but not the cat.
|
-
- HY-P1298A
-
|
Sauvagine TFA
|
CRFR
|
Endocrinology
Neurological Disease
Cardiovascular Disease
|
|
Sauvagine TFA, a 40-amino-acid neuropeptide from the skin of the frog, is a mammalian CRF agonist. Sauvagine TFA is effective at releasing ACTH from rat pituitary cells. Sauvagine TFA possesses a number of pharmacological actions on diuresis, the cardiovascular system and endocrine glands.
|
-
- HY-B1125
-
-
- HY-N0733
-
-
- HY-13212
-
|
(Z)-2-Decenoic acid
cis-2-Decenoic acid
|
Others
|
Cancer
|
|
(Z)-2-decenoic acid (cis-2-Decenoic acid) is an unsaturated fatty acid produced by Pseudomonas aeruginosa. (Z)-2-decenoic acid induces a dispersion response in biofilms formed by a range of gram-negative bacteria, including P. aeruginosa, and by gram-positive bacteria. (Z)-2-decenoic acid inhibits biofilm development.
|
-
- HY-P1746A
-
|
Protein Kinase C (19-31) (TFA)
PKC (19-31) (TFA)
|
PKC
|
Inflammation/Immunology
|
|
Protein Kinase C (19-31) TFA, a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) TFA is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-P1746
-
|
Protein Kinase C (19-31)
PKC (19-31)
|
PKC
|
Inflammation/Immunology
|
|
Protein Kinase C (19-31), a peptide inhibitor of protein kinase C (PKC), derived from the pseudo-substrate regulatory domain of PKCa (residues 19-31) with a serine at position 25 replacing the wild-type alanine, is used as protein kinase C substrate peptide for testing the protein kinase C activity. Protein kinase C (PKC) is involved in controlling the function of other proteins through the phosphorylation of hydroxyl groups of serine and threonine amino acid residues on these proteins.
|
-
- HY-109124A
-
|
Taniborbactam hydrochloride
VNRX-5133 hydrochloride
|
Bacterial
|
Infection
|
|
Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria.
|
-
- HY-113130
-
-
- HY-W016784
-
-
- HY-124422
-
-
- HY-W018512
-
-
- HY-113972A
-
|
(E/Z)-Methyl mycophenolate
|
Others
|
Inflammation/Immunology
|
|
(E/Z)-Methyl mycophenolate is a racemic compound of (Z)-Methyl mycophenolate and (E)-Methyl mycophenolate isomers. Methyl mycophenolate is a methyl ester of mycophenolic acid. Methyl mycophenolate can be used to synthesize mycophenolic acid β-D-glucuronide and phenolic glycosides.
|
-
- HY-W010832
-
-
- HY-W015495
-
-
- HY-W011688
-
|
Methyl palmitoleate
(Z)-Methyl hexadec-9-enoate; Methyl cis-9-Hexadecenoate
|
Others
|
Others
|
|
Methyl palmitoleate ((Z)-Methyl hexadec-9-enoate), a fatty acid methyl ester, is an analogue of Palmitoleate with cytoprotective and growth-promoting properties.
|
-
- HY-W010820
-
-
- HY-W001959
-
|
D-Allothreonine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Allothreonine is the D type stereoisomer of Allothreonine. D-Allothreonine is a peptido-lipid derived from bacteria. D-Allothreonine, amide-linked to the D-galacturonic acid, is also a constituent in the polysaccharide.
|
-
- HY-N7132
-
|
Menthyl acetate
L-Menthyl acetate; (-)-Menthyl acetate
|
Others
|
Others
|
|
Menthyl acetate (L-Menthyl acetate) is a derivative of L-menthol. Menthyl acetate is effective to enhance 5-aminolevulinic acid (ALA) skin permeation.
|
-
- HY-109854A
-
|
(R)-Lisofylline
(R)-Lisophylline
|
STAT
|
Metabolic Disease
Inflammation/Immunology
|
|
(R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is a lysophosphatidic acid acyltransferase inhibitor with an IC50 of 0.6 µM and interrupts IL-12 signaling-mediated STAT4 activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research.
|
-
- HY-N0487
-
-
- HY-D1117
-
|
NADA-green
NADA hydrochloride
|
Others
|
|
|
NADA-green, a fluorescent D-amino acid, suitable for labeling peptidoglycans in live bacteria. NADA-green is incorporated into bacterial cell walls during synthesis. NADA-green results in strong peripheral and septal labeling of taxonomically diverse bacterial cell populations without affecting growth rate. Excitation/emission λ ~450/555 nm.
|
-
- HY-107784
-
|
Ectoine
|
Bacterial
|
Inflammation/Immunology
|
|
Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis.
|
-
- HY-125845A
-
|
(S,S,S)-AHPC hydrochloride
(S,S,S)-VH032-NH2 hydrochloride
|
Ligand for E3 Ligase
|
Cancer
|
|
(S,S,S)-AHPC hydrochloride is a von Hippel-Lindau (VHL) amino building block. (S,S,S)-AHPC is a ligand used as a negative control for (S,R,S)-AHPC. (S,R,S)-AHPC is the VH032-based VHL ligand used in the recruitment of the VHL protein.
|
-
- HY-P1072
-
|
PHM-27 (human)
|
CGRP Receptor
|
Metabolic Disease
Cardiovascular Disease
|
|
PHM-27 (human) is a human prepro-vasoactive intestinal polypeptide (27 amino acid). PHM-27 (human) is a potent the human calcitonin receptor agonist with an EC50 of 11 nM. PHM-27 (human) efficiently enhances glucose-induced insulin secretion from beta cells by an autocrine mechanism.
|
-
- HY-100808
-
|
(R)-Serine
|
iGluR
Endogenous Metabolite
|
Others
|
|
(R)-Serine, an endogenous amino acid involved in glia-synapse interactions that has unique neurotransmitter characteristics, is a potent co-agonist at the NMDA glutamate receptor. (R)-Serine has a cardinal modulatory role in major NMDAR-dependent processes including NMDAR-mediated neurotransmission, neurotoxicity, synaptic plasticity, and cell migration.
|
-
- HY-106783
-
|
Polymyxin B nonapeptide
|
Bacterial
Antibiotic
|
Infection
|
|
Polymyxin B nonapeptide is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
|
-
- 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-P1525
-
-
- HY-106783A
-
|
Polymyxin B nonapeptide TFA
|
Bacterial
|
Infection
|
|
Polymyxin B nonapeptide TFA is a cyclic peptide obtained from Polymyxin B by proteolytic removal of its terminal amino acyl residue. Polymyxin B nonapeptide TFA is less toxic, lacks bactericidal activity, and retains its ability to render gram-negative bacteria susceptible to several antibiotics by permeabilizing their outer membranes.
|
-
- HY-129388B
-
|
LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-7 benzenesulfonate is a potent and orally active inhibitor of lysine specific demethylase-1 (LSD1) with anticancer activity extracted from patent WO2017079670A1, compound 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile.
|
-
- HY-10108
-
|
LY294002
|
PI3K
Casein Kinase
DNA-PK
Autophagy
Apoptosis
|
Cancer
Infection
|
|
LY294002 is a broad-spectrum inhibitor of PI3K with IC50s of 0.5, 0.57, and 0.97 μM for PI3Kα, PI3Kδ and PI3Kβ, respectively. LY294002 also inhibits CK2 with an IC50 of 98 nM. LY294002 is a competitive DNA-PK inhibitorr that binds reversibly to the kinase domain of DNA-PK with an IC50 of 1.4 μM. LY294002 is an autophagy and apoptosis activator.
|
-
- HY-19886
-
|
F 16915
|
Others
|
Cardiovascular Disease
|
|
F 16915, a Docosahexaenoic Acid (DHA, HY-B2167) derivative, is a potent pro-drug of DHA. F 16915 can prevent heart failure-induced atrial fibrillation.
|
-
- HY-133596
-
|
12,14-Dichlorodehydroabietic acid
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release.
|
-
- HY-A0208
-
|
Rosoxacin
Acrosoxacin
|
Bacterial
Antibiotic
|
Infection
|
|
Rosoxacin (Acrosoxacin) is a potent and orally active quinolone antibiotic. Rosoxacin (Acrosoxacin) has antibacterial activities against a broad spectrum of Gram negative bacteria including Neisseria gonorrhoeae (MIC90=0.03mg/ml). Rosoxacin has the potential for urinary tract infections treatment.
|
-
- HY-19996
-
|
AH-7614
|
GPR120
|
Metabolic Disease
|
|
AH-7614 is a potent and selective FFA4 (GPR120) antagonist, with pIC50s of 7.1, 8.1, and 8.1 for human, mouse, and rat FFA4, respectively. AH-7614 has selectivity for FFA4 over FFA1 (pIC50<4.6). AH-7614 is able to block effects of both the polyunsaturated ω-6 fatty acid linoleic acid and the synthetic FFA4 agonist.
|
-
- HY-B1132
-
|
Clidinium bromide
Ro 2-3773
|
mAChR
|
Neurological Disease
|
|
Clidinium bromide is a quaternary amine antimuscarinic agent. Clidinium bromide may help symptoms of cramping and abdominal/stomach pain by decreasing stomach acid, and slowing the intestines in vivo.
|
-
- HY-N6877
-
|
Purpurogallin carboxylic acid
|
Others
|
Cancer
|
|
Purpurogallin carboxylic acid, isolated from Macleaya microcarpa (Maxim.) Fedde, is an oxidation product of gallic acid in fermented tea. Purpurogallin carboxylic acid has anti-cancer activity.
|
-
- HY-133068
-
|
5-Hydroxyferulic acid
|
COMT
|
Others
|
|
5-Hydroxyferulic acid is a hydroxycinnamic acid and is a metabolite of the phenylpropanoid pathway. 5-Hydroxyferulic acid is a precursor in the biosynthesis of sinapic acid and is also a COMT non-esterifed substrate.
|
-
- HY-76199
-
-
- HY-P1202A
-
|
CYN 154806 TFA
|
Somatostatin Receptor
|
Endocrinology
|
|
CYN 154806 TFA, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
|
-
- HY-N8522
-
-
- HY-W015343
-
|
3-Methoxyphenylacetic acid
m-Methoxyphenylacetic acid
|
Others
|
Infection
|
|
3-Methoxyphenylacetic acid (m-Methoxyphenylacetic acid), a m-hydroxyphenylacetic acid (m-OHPAA) derivative, is a phytotoxin in Rhizoctonia solani. 3-Methoxyphenylacetic acid is used to develop a toxin-mediated bioassay for resistance to rhizoctonia root rot.
|
-
- HY-P1202
-
|
CYN 154806
|
Somatostatin Receptor
|
Endocrinology
|
|
CYN 154806, a cyclic octapeptide, is a potent and selective somatostatin sst2 receptor antagonist, with pIC50 values of 8.58, 5.41, 6.07, 5.76 and 6.48 for human recombinant sst2, sst1, sst3, sst4 and sst5 receptors respectively.
|
-
- HY-N1272
-
|
Secaubryenol
|
Endogenous Metabolite
|
Others
|
|
Secaubryenol is a class of 3,4-secocycloartane triterpenes isolated from Coussarea macrophylla. Secaubryenol does not display any cytotoxic effect at a dose of 10 µg/mL.
|
-
- HY-N7692
-
|
Polyporusterone A
|
Others
|
Others
|
|
Polyporusterone A is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone A has inhibitory effect on free radical-induced lysis of red blood cells.
|
-
- HY-N7693
-
|
Polyporusterone B
|
Others
|
Others
|
|
Polyporusterone B is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone B has inhibitory effect on free radical-induced lysis of red blood cells.
|
-
- HY-12741
-
|
LDN-212320
LDN-0212320; OSU-0212320
|
EAAT2
|
Neurological Disease
|
|
LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1]
|
-
- HY-12598A
-
|
DHPG
(RS)-3,5-DHPG
|
mGluR
|
Neurological Disease
|
|
DHPG ((RS)-3,5-DHPG) is an amino acid, which acts as a selective and potent agonist of group I mGluR (mGluR 1 and mGluR 5), shows no effect on Group II or Group III mGluRs. DHPG ((RS)-3,5-DHPG) is also an effective antagonist of mGluRs linked to phospholipase D.
|
-
- HY-15121
-
|
L-Theanine
L-Glutamic Acid γ-ethyl amide; Nγ-Ethyl-L-glutamine
|
Apoptosis
|
Neurological Disease
|
|
L-Theanine (L-Glutamic Acid γ-ethyl amide）is a non-protein amino acid contained in green tea leaves, which blocks the binding of L-glutamic acid to glutamate receptors in the brain, and with neuroprotective and anti-oxidative activities. L-Theanine causes anti-stress effects via the inhibition of cortical neuron excitation by oral intake.
|
-
- HY-P1525A
-
-
- HY-P2230
-
|
Angstrom6
A6 Peptide
|
PAI-1
|
Cancer
|
|
Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
|
-
- HY-15079
-
|
Talampanel
GYKI-53773; LY-300164
|
iGluR
|
Neurological Disease
|
|
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity. Talampanel (IVAX) has neuroprotective effects in rodent stroke models. Talampanel attenuates caspase-3 dependent apoptosis in mouse brain.
|
-
- HY-N7387
-
-
- HY-135283
-
|
ABT-546
A-216546
|
Endothelin Receptor
|
Endocrinology
Cardiovascular Disease
|
|
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is ＞25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
|
-
- HY-P1125
-
|
4-CMTB
|
Others
|
Others
|
|
4-CMTB is a selective free fatty acid receptor 2 (FFA2/GPR43) agonist and a positive allosteric modulator (pEC50=6.38).
|
-
- HY-N2920
-
|
β-Amyrenonol
11-Oxo-β-amyrin
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
β-Amyrenonol (11-Oxo-β-amyrin), an oleanolic-type triterpenoid in licorice roots, is a precursor of Glycyrrhetinic acid. β-Amyrenonol has anti-proliferative and anti-inflammatory activities, and β-Amyrenonol could function as the skeleton for the synthesis of many triterpenoids.
|
-
- HY-108034
-
|
GET73
|
Others
|
Neurological Disease
|
|
GET73 is a γ-hydroxybutyric acid (GHB) analog, a naturally occurring neurotransmitter. GET73 has anti-alcohol and anxiolytic properties. GET73 significantly affects glutamate transmission in the hippocampus.
|
-
- HY-119358
-
|
Traumatic Acid
|
Others
|
Inflammation/Immunology
|
|
Traumatic Acid is a monounsaturated dicarboxylic acid isolated from Phaseolus vulgaris. Traumatic Acid can cause a decrease in membrane phospholipid peroxidation and show antioxidant and stimulatory effects on collagen biosynthesis. Traumatic Acid is a potential agent for the treatment of many skin diseases connected with collagen biosynthesis disorders and oxidative stress.
|
-
- HY-108529
-
|
BMS493
|
RAR/RXR
|
Metabolic Disease
|
|
BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation.
|
-
- HY-N7431
-
-
- HY-136540
-
-
- HY-133621
-
|
9,10-Dichlorostearic acid
|
Others
|
Cancer
|
|
9,10-Dichlorostearic acid is a chlorinated stearic acid with antimutagenic properties. 9,10-Dichlorostearic acid can cause membrane damage by inducing leakage of adenosine triphosphate (ATP) from mammalian tumour cells in vitro.
|
-
- HY-126995
-
-
- HY-B1716
-
|
L-5-Hydroxytryptophan
L-5-HTP; Oxitriptan
|
Endogenous Metabolite
|
Metabolic Disease
Neurological Disease
|
|
L-5-Hydroxytryptophan (L-5-HTP), a naturally occurring amino acid and a dietary supplement for use as an antidepressant, appetite suppressant, and sleep aid, is the immediate precursor of the neurotransmitter serotonin and a reserpine antagonist. L-5-Hydroxytryptophan (L-5-HTP) is used to treat fibromyalgia, myoclonus, migraine, and cerebellar ataxia.
|
-
- HY-P1051
-
|
β-amyloid (12-28)
Amyloid β-Protein (12-28)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-P1051A
-
|
β-amyloid (12-28) (TFA)
Amyloid β-Protein (12-28) (TFA)
|
Amyloid-β
|
Neurological Disease
|
|
β-amyloid (12-28) TFA is a peptide fragment of β-amyloid protein (β1-42). β1–42 a 42 amino acid protein , is the major component of senile plaque cores. β-amyloid (12-28) shows aggregation properties. β-amyloid (12-28) has the potential for Alzheimer’s disease research.
|
-
- HY-16969
-
|
Dihexa
PNB-0408; N-hexanoic-Try-Ile-(6)-Amino hexanoic amide; Hexanoyl-Tyr-Ile-Ahx-NH2
|
c-Met/HGFR
|
Neurological Disease
|
|
Dihexa, an oligopeptide drug, is an orally active and blood-brain barrier-permeable angiotensin IV analog. Dihexa binds to hepatocyte growth factor (HGF) with high affinity (Kd=65 pM) and potentiates its activity at its receptor, c-Met. Dihexa exhibits excellent antidementia activity and improves cognitive function in animal models. Dihexa may have therapeutic potential as a treatment Alzheimer’s disease.
|
-
- HY-W000434
-
|
Fmoc-NH-PEG4-CH2CH2COOH
Fmoc-15-Amino-4,7,10,13-tetraoxapentadecanoic acid
|
ADC Linker
|
Cancer
|
|
Fmoc-NH-PEG4-CH2CH2COOH is a cleavable ADC linker used in the synthesis of antibody-drug conjugates (ADCs).
|
-
- HY-106224
-
|
Orexin A (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-N2453
-
|
Convallatoxin
|
PPAR
NF-κB
P-glycoprotein
|
Cancer
Inflammation/Immunology
|
|
Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
|
-
- HY-N7426
-
|
3-Deoxyglucosone
3-Deoxy-D-glucosone
|
Others
|
Metabolic Disease
|
|
3-Deoxyglucosone (3-Deoxy-D-glucosone) is a reactive intermediate of the Maillard reaction and the polyol pathway. 3-Deoxyglucosone rapidly reacts with protein amino groups to form advanced glycation end products (AGEs), such as imidazolone, it is the most specific AGE for 3-DG. 3-Deoxyglucosone synergizes with low glucose to potentiate GLP-1 secretion and is considered as a biomarker for diabetes.
|
-
- HY-W011727A
-
|
Pyridoxal 5'-phosphate monohydrate
Pyridoxal phosphate monohydrate
|
Others
|
Neurological Disease
|
|
Pyridoxal 5'-phosphate hydrate, the active form of vitamin B6, is an essential cofactor for multiple enzymes, including aromatic l-amino acid decarboxylase that catalyzes the final stage in the production of the neurotransmitters dopamine and serotonin. Pyridoxal 5'-phosphate hydrate is the most important coenzyme variant in the process of vitamin B6 intracellular phosphorylation and is interconvertible with other variants, including pyridoxine 5′‐phosphate (PNP) and pyridoxamine 5′‐phosphate (PMP).
|
-
- 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-P1854
-
|
β-Amyloid (1-9)
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-9), an N-terminal fragment of beta amyloid, consists of amino acid residues 1 to 9. β-Amyloid (1-9) contains a B cell epitope, but it does not include T cell epitopes. Omission of residues 1 to 9 from the full-length Alzheimer'sβ-Amyloid peptide 1 to 40 does not prevent the peptide from forming amyloid fibrils or eliminate fibril polymorphism .
|
-
- HY-127090
-
|
Muramyl dipeptide
MDP
|
p38 MAPK
ERK
JNK
|
Inflammation/Immunology
|
|
Muramyl dipeptide (MDP) is a synthetic immunoreactive peptide, consisting of N-acetyl muramic acid attached to a short amino acid chain of L-Ala-D-isoGln. Muramyl dipeptide is an inducer of bone formation through induction of Runx2. Muramyl dipeptide directly enhances osteoblast differentiation by up-regulating Runx2 gene expression through MAPK pathways. Muramyl dipeptide indirectly attenuates osteoclast differentiation through a decreased RANKL/OPG ratio.
|
-
- HY-15209
-
-
- 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-B1557A
-
|
Betazole dihydrochloride
Ametazole dihydrochloride
|
Histamine Receptor
|
Metabolic Disease
|
|
Betazole (Ametazole) dihydrochloride, a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole dihydrochloride induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole dihydrochloride has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity.
|
-
- HY-135772
-
-
- HY-103138A
-
|
(Rac)-WAY-161503
|
5-HT Receptor
|
Metabolic Disease
Neurological Disease
|
|
(Rac)-WAY-161503 is a potent, selective, highly affinity 5-HT2C receptor agonist with a Ki of 4 nM and an EC50 of 12 nM. (Rac)-WAY-161503 displays higher affinity for 5-HT2C than 5-HT2A and 5-HT2B receptors. (Rac)-WAY-161503 has anti-obesity and antidepressant effects.
|
-
- HY-B1557
-
|
Betazole
Ametazole
|
Histamine Receptor
|
Metabolic Disease
|
|
Betazole (Ametazole), a pyrazole analogue of histamine, is an orally active H2 receptor agonist. Betazole induces gastric acid secretion, and causes an immediate and significant increase in common bile duct pressure. Betazole has been used as a diagnostic agent known as histalog, for investigating gastric acid secretory capacity.
|
-
- HY-B1124A
-
|
Fipexide hydrochloride
|
Adenylate Cyclase
Dopamine Transporter
|
Neurological Disease
|
|
Fipexide hydrochloride, a parachloro-phenossiacetic acid derivative, is a nootropic drug. Fipexide hydrochloride reduces striatal adenylate cyclase activity. Fipexide hydrochloride has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide hydrochloride is used for senile dementia research.
|
-
- HY-N7624
-
|
Methyl oleanonate
3-Oxoolean-12-en-28-oic acid methyl ester
|
PPAR
|
Cancer
|
|
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.
|
-
- HY-B1124
-
|
Fipexide
|
Adenylate Cyclase
Dopamine Transporter
|
Neurological Disease
|
|
Fipexide, a parachloro-phenossiacetic acid derivative, is a nootropic drug. Fipexide reduces striatal adenylate cyclase activity. Fipexide has positive effect on cognitive performance by dopaminergic neurotransmission. Fipexide is used for senile dementia research.
|
-
- HY-106224A
-
|
Orexin A (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-N7059
-
|
Lactobionic acid
|
Bacterial
|
Infection
|
|
Lactobionic acid is a bionic acid naturally found in the Caspian Sea yogurt and chemically constituted of a gluconic acid bonded to a galactose. Lactobionic acid has antioxidant, antimicrobial, chelating, stabilizer, acidulant, and moisturizing properties.
|
-
- HY-B2246
-
|
L-Carnitine hydrochloride
(R)-Carnitine hydrochloride
|
Endogenous Metabolite
|
Metabolic Disease
|
|
L-Carnitine hydrochloride ((R)-Carnitine hydrochloride), a highly polar, small zwitterion, is an essential co-factor for the mitochondrial β-oxidation pathway. L-Carnitine hydrochloride functions to transport long chain fatty acyl-CoAs into the mitochondria for degradation by β-oxidation. L-Carnitine hydrochloride is an antioxidant. L-Carnitine hydrochloride can ameliorate metabolic imbalances in many inborn errors of metabolism.
|
-
- HY-117549
-
|
Ibrolipim
NO-1886
|
Others
|
Cardiovascular Disease
|
|
Ibrolipim (NO-1886) is an orally active lipoprotein lipase (LPL)-promoting agent. Ibrolipim decreases plasma triglycerides, increases high-density lipoprotein cholesterol levels. Ibrolipim has renoprotective and hypolipidemic effects.
|
-
- HY-126415
-
-
- HY-136066
-
|
Tauro-ω-muricholic acid sodium
TωMCA sodium
|
Others
|
Metabolic Disease
|
|
Tauro-ω-muricholic acid sodium (TωMCA sodium) is a bile acid released by the liver and an analog of tauro-α-muricholic acid. Tauro-ω-muricholic acid sodium is investigated as a potential marker in plasma for early-onset neonatal sepsis (EOS) and cholestasis studies
|
-
- HY-133027
-
|
Myristyl nicotinate
Tetradecyl nicotinate
|
Others
|
Cancer
|
|
Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug and a lipophilic derivative of Nicotinic acid. Myristyl nicotinate is being developed for delivery of Nicotinic acid into the skin for prevention of actinic keratosis and its progression to skin cancer. Myristyl nicotinate shows to stimulate epidermal differentiation in photodamaged skin, increasing skin NAD content and strengthening the skin barrier.
|
-
- HY-B0550
-
|
Bismuth Subsalicylate
Bismuth oxysalicylate; Bismuth(III) salicylate basic
|
PGE synthase
|
Neurological Disease
|
|
Bismuth Subsalicylate is a potent and orally active antacid and anti-diarrheal agent. Bismuth Subsalicylate reduces inflammation/irritation of stomach and intestinal lining through inhibition of prostaglandin synthesis in vivo. Bismuth Subsalicylate is widely used for the research of diarrheal disorders, including indigestion, diarrhoea, nausea, et al.
|
-
- HY-110155
-
|
LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-W019870
-
|
Glufosinate ammonium
|
Others
|
Neurological Disease
|
|
Glufosinate ammonium, a phosphinic acid analogue of glutamic acid, is an herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate ammonium exerts neurotoxic activity.
|
-
- HY-N2417
-
|
Stearyl glycyrrhetinate
|
Bacterial
|
Infection
|
|
Stearyl glycyrrhetinate, a major component in licorice extract, has a MIC against S. aureus strains of more than 256 mg/L. Stearyl glycyrrhetinate has antibacterial effects.
|
-
- HY-N6036
-
|
Ganoderic acid F
|
Others
|
Cancer
|
|
Ganoderic acid F is a ganoderic acid. Ganoderic acid F exhibits antitumor and antimetastatic activities through inhibition of angiogenesis and alteration of proteins involving cell proliferation and/or cell death, carcinogenesis, oxidative stress, calcium signaling, and endoplasmic reticulum stress.
|
-
- HY-131041
-
|
Ned-K
|
Calcium Channel
|
Cardiovascular Disease
|
|
Ned-K is a nicotinic acid adenine dinucleotide phosphate (NAADP) antagonist. Ned-K is effective at dampening simulated ischaemia and reperfusion (sIR)-induced Ca 2+ oscillations in cardiomyocytes.
|
-
- HY-W019870A
-
|
Glufosinate
|
Others
|
Neurological Disease
|
|
Glufosinate, a phosphinic acid analogue of glutamic acid, is a herbicide which is converted by plant cells into PT (L-phosphinothricin). Glufosinate exerts neurotoxic activity.
|
-
- HY-N0301
-
|
Thiocolchicoside
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
Thiocolchicoside is a competitive γ-aminobutyric acid type A (GABAA) receptor antagonist and glycine receptor agonist in the central nervous system. Thiocolchicoside is a semisynthetic sulfur derivative of colchicoside. Thiocolchicoside is a muscle relaxant and has anti-inflammatory, and analgesic properties.
|
-
- HY-131615
-
|
TPC2-A1-P
|
Sodium Channel
|
Others
|
|
TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na 2+ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-B0310
-
|
Nizatidine
|
Histamine Receptor
|
Cancer
Endocrinology
Inflammation/Immunology
|
|
Nizatidine is a potent and orally active histamine H2 receptor antagonist, can be used for the research of stomach and intestines ulcers. Nizatidine works by decreasing the secretion of gastric acid the stomach makes and prevent ulcers from coming back after they have healed in animal models.
|
-
- HY-N1429
-
-
- HY-131614
-
|
TPC2-A1-N
|
Calcium Channel
|
Others
|
|
TPC2-A1-N is a powerful and Ca 2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca 2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-N2027
-
-
- HY-W011404
-
|
Tributyrin
Glyceryl tributyrate
|
Apoptosis
|
Metabolic Disease
|
|
Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. Tributyrin diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into the cell in vivo. Tributyrin has potent antiproliferative, proapoptotic and differentiation-inducing effects.
|
-
- HY-112764
-
|
DMG-PEG 2000
|
Others
|
Metabolic Disease
|
|
DMG-PEG 2000 is used for the preparation of liposome for siRNA delivery with improved transfection efficiency in vitro. DMG-PEG 2000 is also used for the lipid nanoparticle for an oral plasmid DNA delivery approach in vivo through a facile surface modification to improve the mucus permeability and delivery efficiency of the nanoparticles.
|
-
- HY-137471
-
|
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-136121
-
|
Tubulin inhibitor 6
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
|
-
- HY-112812
-
-
- HY-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- HY-18353
-
|
mTOR inhibitor-3
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-112722
-
-
- HY-137497
-
|
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-D0843
-
|
N-Ethylmaleimide
NEM
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
|
-
- HY-101275
-
-
- HY-13278A
-
-
- HY-21141
-
|
Cysteine protease inhibitor-2
|
Cathepsin
|
Cancer
|
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-17541A
-
-
- HY-17541
-
-
- HY-112914
-
-
- HY-70005
-
-
- HY-128703
-
-
- HY-10442
-
-
- HY-12186
-
|
3-Deazaneplanocin A hydrochloride
DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
|
-
- HY-128722
-
-
- HY-110101
-
-
- HY-12202
-
-
- HY-B0543
-
-
- HY-10421
-
-
- HY-B0385
-
-
- HY-P0017
-
-
- HY-112843
-
|
CNT2 inhibitor-1
|
Others
|
Others
|
|
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
|
-
- 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-136279
-
|
TrxR inhibitor D9
|
Apoptosis
|
Cancer
|
|
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-15182
-
-
- HY-112474
-
-
- HY-B0732
-
-
- HY-136920
-
-
- HY-13662A
-
-
- HY-119937
-
-
- HY-15253
-
-
- HY-13973A
-
-
- HY-104051
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-112390A
-
|
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-122723
-
|
GOT1 inhibitor-1
|
Others
|
Cancer
|
|
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
|
-
- HY-114317
-
|
MARK4 inhibitor 1
|
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
|
-
- HY-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-135826
-
|
Necroptosis-IN-1
|
RIP kinase
|
Cancer
|
|
Necroptosis-IN-1, an analog of Necrostatin-1 (HY-15760), is a potent necroptosi inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
|
-
- HY-111408
-
-
- HY-N2033
-
-
- HY-100463
-
-
- HY-112607
-
|
Tubulin inhibitor 1
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
|
-
- HY-124798
-
-
- 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-B0884
-
-
- HY-112569
-
-
- HY-B0884A
-
-
- HY-15167
-
-
- HY-112906
-
-
- HY-50856A
-
-
- HY-117262
-
-
- HY-13276
-
-
- HY-B0218
-
-
- HY-106067A
-
-
- HY-N6717
-
|
Tentoxin
|
Others
|
Infection
|
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-17542
-
|
PLpro inhibitor
|
SARS-CoV
|
Infection
|
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
|
-
- HY-15760
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-13662B
-
|
(R)-Lansoprazole
Dexlansoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-10217
-
-
- HY-P1029
-
-
- HY-15604
-
-
- HY-N0565
-
-
- HY-15183
-
-
- HY-U00387
-
-
- HY-107986
-
-
- HY-10249A
-
-
- HY-100962
-
|
(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
|
-
- HY-N0565A
-
-
- HY-108322
-
-
- HY-50880
-
-
- HY-N2221
-
-
- HY-14657
-
-
- HY-101932
-
-
- HY-N6902
-
-
- HY-U00319
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-112269
-
-
- HY-128723
-
-
- HY-50879
-
-
- HY-104032
-
-
- 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-136270
-
|
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-103310
-
-
- HY-122856
-
|
AZ12601011
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-50900
-
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-101474A
-
|
Zanubrutinib
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
|
-
- HY-16569
-
-
- HY-N7592
-
|
Arjunetin
|
Others
|
Others
|
|
Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
|
-
- HY-W008923
-
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-100110
-
|
KNK437
Heat Shock Protein Inhibitor I
|
HSP
|
Cancer
|
|
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-135384
-
-
- HY-106638
-
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-16657
-
-
- 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-119808
-
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-P2478
-
-
- HY-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2477
-
-
- HY-15358
-
|
ALK inhibitor 2
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
|
-
- HY-10917
-
|
GW2580
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
|
-
- HY-15357
-
|
ALK inhibitor 1
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
|
-
- HY-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-113951
-
-
- HY-124718
-
|
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-P1260
-
-
- HY-19797A
-
-
- HY-14274
-
|
Anastrozole
ZD1033
|
Aromatase
|
Cancer
|
|
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
|
-
- HY-131101
-
|
Nor-Acetildenafil
|
Others
|
Others
|
|
Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
|
-
- HY-18930
-
|
NU6300
|
CDK
|
Cancer
|
|
NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
|
-
- HY-W013478
-
-
- HY-15700
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-N2219
-
-
- HY-19795
-
|
ML240
|
p97
|
Cancer
|
|
ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.
|
-
- HY-112639
-
-
- HY-100600
-
|
BGG463
K03859
|
CDK
|
Others
|
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- HY-136461
-
-
- HY-P2564
-
-
- HY-15222
-
-
- HY-14196
-
-
- HY-17396
-
-
- HY-14440
-
|
MP7
PDK1 inhibitor
|
PDK-1
|
Cancer
|
|
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
|
-
- HY-50670
-
-
- HY-U00145
-
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-12072
-
|
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- 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-111429
-
|
YAP/TAZ inhibitor-1
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-118355
-
|
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-12824
-
|
RNPA1000
|
Antibiotic
Bacterial
|
Infection
|
|
RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC50 of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.
|
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-100932
-
|
ML-9
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-N0565B
-
|
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
MMP
Bacterial
Antibiotic
|
Infection
|
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-15699A
-
-
- HY-B2063
-
|
Chlorobenzuron
|
Others
|
Others
|
|
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
|
-
- HY-N1447
-
-
- HY-15167A
-
-
- HY-112634
-
-
- HY-133248
-
-
- HY-13972
-
-
- HY-15699
-
-
- HY-118165
-
-
- HY-B1596
-
-
- HY-P1260A
-
-
- HY-103593A
-
-
- HY-15842
-
-
- HY-103593
-
|
LCL521
|
Phospholipase
|
Cancer
|
|
LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
|
-
- HY-I0637
-
-
- HY-16187
-
-
- HY-133247
-
-
- HY-D0886
-
-
- HY-18965
-
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-107451
-
-
- HY-107485
-
-
- HY-14174
-
-
- HY-N7511
-
-
- HY-N4294
-
-
- HY-B2007
-
-
- HY-13818
-
-
- HY-100498
-
|
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-14445
-
-
- HY-19707
-
-
- HY-112822
-
|
ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-100456
-
-
- HY-111493
-
-
- HY-50706A
-
|
Selumetinib sulfate
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-13228
-
-
- HY-126288
-
|
ERK1/2 inhibitor 2
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
|
-
- HY-10227
-
|
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- 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-17367
-
|
Atazanavir
BMS-232632
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Infection
Cancer
|
|
Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-13985
-
-
- HY-12031A
-
-
- HY-U00453
-
-
- 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-15339
-
|
CVT-313
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
|
-
- HY-13984
-
|
Mutant EGFR inhibitor
|
EGFR
|
Cancer
|
|
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
|
-
- HY-22166
-
-
- HY-W047428
-
-
- HY-112451
-
-
- HY-15217
-
-
- HY-15859
-
|
Atglistatin
|
ATGL
|
Metabolic Disease
|
|
Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.
|
-
- HY-77521
-
-
- HY-13502
-
-
- HY-107994
-
-
- HY-70027A
-
-
- HY-N2567
-
|
(±)-Decursinol
|
Bacterial
|
Cancer
|
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-13278
-
-
- HY-112860
-
-
- HY-12000
-
-
- HY-A0116S
-
-
- HY-13060
-
-
- HY-101474
-
|
(±)-Zanubrutinib
(±)-BGB-3111
|
Btk
|
Cancer
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
|
-
- HY-19731
-
-
- HY-101462
-
-
- HY-B0902A
-
|
Rufloxacin hydrochloride
MF-934 hydrochloride
|
Bacterial
|
Infection
|
|
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
|
-
- HY-101963
-
-
- HY-70073
-
-
- HY-15775
-
-
- HY-13502A
-
-
- HY-70003
-
-
- HY-112720
-
-
- HY-111784
-
-
- HY-10439
-
|
HPGDS inhibitor 1
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-100816
-
|
Rbin-1
Ribozinoindole-1
|
Phosphatase
|
Metabolic Disease
|
|
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
|
-
- 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-100556
-
|
Tie2 kinase inhibitor 1
|
Others
|
Cancer
|
|
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
|
-
- HY-112715
-
-
- HY-128918
-
|
SIS17
|
HDAC
|
Others
|
|
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
|
-
- HY-124793
-
|
GAK inhibitor 49
|
Others
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.
|
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-100932A
-
|
ML-9 Free Base
|
Myosin
|
Cancer
|
|
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-135318
-
|
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- 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-12364
-
-
- HY-P0081
-
-
- HY-133110
-
|
Afatinib N-Oxide
|
Others
|
Others
|
|
Afatinib N-Oxide is a impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
|
-
- HY-15798
-
-
- HY-114418
-
-
- HY-N5038
-
|
Mauritianin
|
Topoisomerase
|
Cancer
|
|
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.
|
-
- HY-13606
-
|
Dacinostat
NVP-LAQ824; LAQ824
|
HDAC
Autophagy
|
Cancer
|
|
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
|
-
- HY-13256
-
-
- HY-P1452A
-
-
- HY-Y0882
-
-
- HY-16420
-
|
R112
|
Syk
|
Inflammation/Immunology
|
|
R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
|
-
- HY-111919
-
-
- HY-15588
-
-
- HY-B0830
-
|
Isoprocarb
|
AChE
|
Neurological Disease
|
|
Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
|
-
- HY-N1502
-
|
Carboxyatractyloside
Gummiferin
|
Others
|
Cancer
|
|
Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.
|
-
- HY-12054A
-
-
- HY-114423
-
-
- HY-10809
-
|
Bitopertin
RG1678; RO4917838
|
GlyT
|
Neurological Disease
|
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Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
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- HY-19609
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- HY-131268
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- HY-N6619A
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Lycoramine
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AChE
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Neurological Disease
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Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
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- HY-12814
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TH588
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DNA/RNA Synthesis
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Cancer
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TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
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- HY-12054
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- HY-12420
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JNJ-47117096 hydrochloride
MELK-T1 hydrochloride
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MELK
FLT3
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Cancer
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JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
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- HY-16982
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Cercosporamide
(-)-Cercosporamide
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Fungal
MNK
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Cancer
Infection
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Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
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- HY-136347
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- HY-13280
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- HY-N4186
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- HY-103002
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SU5408
VEGFR2 Kinase Inhibitor I
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VEGFR
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Cardiovascular Disease
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SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
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- HY-B0497B
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-
- HY-131446
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Chk1-IN-5
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Checkpoint Kinase (Chk)
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Cancer
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Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
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- HY-50202
-
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Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
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Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
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- HY-19727A
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-
- HY-124416
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ML604086
|
CCR
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Inflammation/Immunology
Endocrinology
|
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ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations.
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-
- HY-103490
-
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Takinib
|
MAP3K
Apoptosis
|
Cancer
|
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Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
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-
- HY-17367A
-
|
Atazanavir sulfate
BMS-232632 sulfate
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Cancer
Infection
|
|
Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
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-
- HY-122866
-
|
ZT-12-037-01
|
Ras
|
Cancer
|
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.
|
-
- HY-100227
-
|
E 64c
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
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-
- HY-66004
-
|
4-Acetamidophenyl acetate
|
Others
|
Inflammation/Immunology
|
|
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-115502
-
|
BCI
(E)-BCI
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
|
-
- HY-80003
-
|
QL47
|
Btk
|
Cancer
Infection
|
|
QL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses. QL47 selectively inhibits eukaryotic translation. QL47 is a potent covalent inhibitor of BTK with an IC50 of 7 nM.
|
-
- HY-15766A
-
|
GNE-617 hydrochloride
|
Nampt
|
Cancer
|
|
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- 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-101053
-
|
Src Inhibitor 1
Src Kinase Inhibitor 1; Src-l1
|
Src
|
Cancer
|
|
Src Inhibitor 1 is a potent and selective dual site Src tyrosine kinase inhibitor with IC50 values of 44 nM for Src and 88nM for Lck.
|
-
- HY-10247
-
|
BRAF inhibitor
|
Raf
|
Cancer
|
|
BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
|
-
- HY-N2522
-
-
- HY-109565
-
|
ASTX660
|
IAP
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-108820
-
-
- HY-108817
-
-
- HY-13452
-
-
- HY-119459
-
|
Fluopyram
|
Fungal
|
Infection
|
|
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
|
-
- HY-135383A
-
-
- HY-A0122
-
-
- HY-17381
-
-
- HY-N6031
-
|
Dendrophenol
|
NF-κB
|
Cancer
|
|
Dendrophenol, isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.
|
-
- HY-Y0172
-
