Search Result
Results for "Ang (3-4) Inhibitors" in MCE Product Catalog:
8222
Inhibitors & Agonists
13
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-N1775
-
3',4'-Dihydroxyacetophenone
3,4-DHAP
|
Tyrosinase
|
Cancer
|
3',4'-Dihydroxyacetophenone (3,4-DHAP), isolated from Picea Schrenkiana Needles exhibits a strong suppressive action against tyrosinase activity, with an IC50 of 10 μM. 3',4'-Dihydroxyacetophenone (3,4-DHAP) is a vasoactive agent and antioxidant.
|
-
- HY-111802
-
-
- HY-101667
-
LTURM34
|
DNA-PK
|
Cancer
|
LTURM34 is a specific DNA-PK inhibitor (IC50=34 nM). LTURM34 exhibits 170-fold selectivity for DNA-PK over PI3K. LTURM34 shows potent antiproliferative activity in a wide range of tumor cell lines.
|
-
- HY-N1780
-
3,4-Dimethoxyphenol
|
Tyrosinase
|
Endocrinology
Metabolic Disease
|
3,4-Dimethoxyphenol is a plant-derived phenylpropanoid compound and can use as a whitening agent in cosmetics. 3,4-Dimethoxyphenol has tyrosinase-inhibiting activity. 3,4-Dimethoxyphenol has potent antioxidant effect isolated from the bacterial fermentation broth.
|
-
- HY-12794
-
-
- HY-117570
-
KSC-34
|
Others
|
Neurological Disease
|
KSC-34, a covalent modifier of protein disulfide isomerase A1 (PDIA1), is also a selective and potent a-site inhibitor of PDIA1 with an IC50 of 3.5 μM. KSC-34 displays a 30-fold selectivity for a domain over a′ domain and displays high selectivity for PDIA1 in complex proteomes with minimal engagement of other members of the PDI family.
|
-
- HY-12795
-
Vps34-IN-1
|
PI3K
Autophagy
|
Cancer
|
Vps34-IN-1 is an inhibitor of Vps34 extracted from patent WO2012085815A1, compound example 16a, with an IC50 of 4 nM. Vps34-IN-1 modulates autophagy.
|
-
- HY-Y0935
-
-
- HY-113474
-
-
- HY-12473
-
Vps34-IN-2
|
PI3K
|
Cancer
|
Vps34-IN-2 is a novel, potent and selective inhibitor of Vps34 with IC50s of 2 and 82 nM on the Vps34 enzymatic assay and the GFP-FYVE cellular assay, respectively.
|
-
- HY-13519
-
-
- HY-W001080
-
-
- HY-Y0771
-
-
- HY-13688
-
-
- HY-13688A
-
PJ34
|
PARP
|
Cancer
|
PJ34 is a potent specific inhibitor of PARPl/2 with IC50 of 110 nM and 86 nM, respectively.
|
-
- HY-N0057
-
3,4-Dicaffeoylquinic acid
3,4-Di-O-caffeoylquinic acid; Isochlorogenic acid B
|
Glucosidase
Influenza Virus
Apoptosis
Endogenous Metabolite
|
Cancer
Infection
|
3,4-Dicaffeoylquinic acid (3,4-Di-O-caffeoylquinic acid), naturally isolated from Laggera alata, has antioxidative, DNA protective, neuroprotective and hepatoprotective properties. 3,4-Dicaffeoylquinic acid exerts apoptosis-mediated cytotoxicity and α-glucosidase inhibitory effects. 3,4-Dicaffeoylquinic acid possesses a unique mechanism of anti-influenza viral activity, that is, enhancing viral clearance by increasing TRAIL.
|
-
- HY-128760
-
COH34
|
Others
|
Cancer
|
COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors.
|
-
- HY-W017434
-
-
- HY-P2426
-
-
- HY-106934
-
Peldesine
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
-
- HY-106934A
-
Peldesine dihydrochloride
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Cancer
Infection
Inflammation/Immunology
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research.
|
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- HY-109714
-
3,4-Benzocoumarin
|
Others
|
Inflammation/Immunology
|
3,4-Benzocoumarin is a kind of the expanded structure of coumarin derivatives.Coumarin is a chemical compound in the benzopyrone chemical class that can be found in many natural species. Coumarins possess variety of biological activities and unique photophysical properties. 3,4-Benzocoumarin, a AOH‐like compound , has the sensibility of the antibody with an IC50 of 919.2 ng/mL.
|
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- HY-133611
-
-
- HY-115666
-
COH34 analog 1
|
Others
|
Cancer
|
COH34 analog 1, a metabolite, is an oxidized analog of COH34. COH34 is a potent poly(ADP-ribose) glycohydrolase (PARG) inhibitor.
|
-
- HY-14946
-
Amifampridine
3,4-Diaminopyridine
|
Others
|
Others
|
Amifampridine (3,4-Diaminopyridine) is a drug, predominantly in the treatment of a number of rare muscle diseases.
|
-
- HY-136593
-
(S)-3-(4-Hydroxyphenyl)-2-hydroxypropionic acid
(S)-3-(4-Hydroxyphenyl)lactic acid
|
Others
|
Others
|
(S)-3-(4-Hydroxyphenyl)-2-hydroxypropionic acid (compound 1) is a metabolite isolated from the culture medium of Leuconostoc mesenteroides. (S)-3-(4-Hydroxyphenyl)-2-hydroxypropionic acid has high DPPH radical-scavenging activities and antioxidative activities.
|
-
- HY-117771
-
DO34
|
Others
|
Metabolic Disease
|
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
|
-
- HY-P1322
-
-
- HY-111583
-
RXFP3/4 agonist 1
|
Others
|
Metabolic Disease
|
RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC50s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats.
|
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- HY-117771A
-
-
- HY-P1223
-
-
- HY-113304
-
-
- HY-107575
-
-
- HY-111804
-
-
- HY-135910
-
-
- HY-N1778
-
-
- HY-N7641
-
3',4',7-Trimethoxyquercetin
Quercetin 3′,4′,7-trimethyl ether
|
Others
|
Others
|
3',4',7-Trimethoxyquercetin (Quercetin 3′,4′,7-trimethyl ether) is a polymethoxylated flavone isolated from the plant of genus Taraxacum, has antioxidant activity.
|
-
- HY-N7557
-
-
- HY-131999
-
-
- HY-P1322A
-
-
- HY-111818
-
TH34
|
HDAC
|
Cancer
|
TH34, an HDAC6/8/10 inhibitor with IC50s of 4.6 μM, 1.9 μM, and 7.7 μM respectively, shows high selectivity over HDAC1/2/3.
|
-
- HY-P1225
-
-
- HY-P1252
-
-
- HY-135976
-
P2X3 antagonist 34
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect.
|
-
- HY-W016993
-
-
- HY-W010130
-
-
- HY-P1323
-
-
- HY-P0059
-
Teriparatide
Human parathyroid hormone-(1-34); hPTH (1-34)
|
Others
|
Cancer
|
Teriparatide (Human parathyroid hormone-(1-34)) is a PHT agonist, with an IC50 of 2 nM in HEK293 cells.
|
-
- HY-P1252A
-
-
- HY-N2044
-
Methyl 3,4,5-trimethoxybenzoate
|
Others
|
Others
|
Methyl 3,4,5-trimethoxybenzoate can be synthesized from Gallic acid. Methyl 3,4,5-trimethoxybenzoate is mainly used in the production of Trimethoprim (TMP), Sulfa synergistic intermediates, and many other agents.
|
-
- HY-133598
-
-
- HY-N7427
-
-
- HY-107858
-
Veratryl alcohol
3,4-Dimethoxybenzyl alcohol
|
Others
|
Others
|
Veratryl alcohol (3,4-Dimethoxybenzenemethanol), a secondary metabolite of some lignin degrading fungi, is commonly used nonphenolic substrate for assaying ligninolytic activity.
|
-
- HY-N0871
-
-
- HY-N3023
-
3,4-Dihydroxybenzylamine hydrobromide
NSC 263475 hydrobromide
|
DNA/RNA Synthesis
|
Cancer
|
3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) is an improved dopamine analog cytotoxic and inhibits DNA polymerase activity in melanoma cells. 3,4-Dihydroxybenzylamine hydrobromide (NSC 263475 hydrobromide) displays growth inhibitory activity in melanoma cell lines with varying degrees of tyrosinase activity.
|
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- HY-133606
-
-
- HY-133601
-
-
- HY-P1323A
-
-
- HY-W012123
-
3,4,5-Trimethoxycinnamic acid
|
GABA Receptor
Endogenous Metabolite
|
Neurological Disease
|
3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia
WILLD, with anti-stress effect, prolonging the sleeping time in animals. 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits.
|
-
- HY-Y1620
-
-
- HY-W016289
-
Antiarol
3,4,5-Trimethoxyphenol
|
Others
|
Others
|
Antiarol (3,4,5-Trimethoxyphenol) is a natural compound isolated from Salmaliamalabaricum.
|
-
- HY-111388A
-
SEL120-34A monohydrochloride
|
CDK
|
Cancer
|
SEL120-34A monohydrochloride is an ATP-competitive and selective CDK8 inhibitor, inhibits kinase activities of CDK8/CycC and CDK19/CycC complexes with IC50s of 4.4 nM and 10.4 nM, respectively, with a Kd of 3 nM for CDK8. SEL120-34A monohydrochloride weakly inhibits CDK9 (calculated IC50=1070 nM), but shows no obvious activity against CDK1, 2, 4, 6, 5, 7. SEL120-34A monohydrochloride inhibits phosphorylation of STAT1 S727 and STAT5 S726. Has anti-tumor activity.
|
-
- HY-N7012
-
7,3',4'-Tri-O-methylluteolin
5-Hydroxy-3',4',7-trimethoxyflavone
|
TNF Receptor
Interleukin Related
COX
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
7,3',4'-Tri-O-methylluteolin (5-Hydroxy-3',4',7-trimethoxyflavone) is a flavonoid from the herb Lippia nodiflora L. (Verbenaceae) which has been documented to exhibit anti-inflammatory, antipyretic, antitussive, antidiabetic, anticancer, and antimelanogenesis properties. 7,3',4'-Tri-O-methylluteolin obviously reduces the prodn of pro-inflammatory cytokines, such as TNF-α, IL-6, and IL-1β in a concentration-dependent manner. 7,3',4'-Tri-O-methylluteolin significantly induces reduction in the mRNA expressions of inducible nitric oxide synthase and cyclooxygenase-2, representing that inhibition occurs at the transcriptional level.
|
-
- HY-141007
-
-
- HY-141004
-
-
- HY-141006
-
-
- HY-W022390
-
-
- HY-125907
-
-
- HY-N2007
-
Veratric acid
3,4-Dimethoxybenzoic acid
|
COX
Reactive Oxygen Species
|
Inflammation/Immunology
Cardiovascular Disease
|
Veratric acid (3,4-Dimethoxybenzoic acid) is an orally active phenolic compound derived from vegetables and fruits, has antioxidant and anti-inflammatory activities. Veratric acid also acts as a protective agent against hypertension-associated cardiovascular remodelling. Veratric acid reduces upregulated COX-2 expression, and levels of PGE2, IL-6 after UVB irradiation.
|
-
- HY-125828
-
-
- HY-N7030
-
5,7,3',4'-Tetramethoxyflavone
|
Others
|
Infection
|
5,7,3',4'-Tetramethoxyflavone, one of the major polymethoxyflavones (PMFs) isolated from M. exotica, possesses various bioactivities, including anti-fungal, anti-malarial, anti-mycobacterial, and anti-inflammatory activities. 5,7,3',4'-Tetramethoxyflavone exhibits chondroprotective activity by targeting β-catenin signaling.
|
-
- HY-133610
-
3,4,6-Trichlorocatechol
|
Others
|
Others
|
3,4,6-trichlorocatechol (TCC) is the metabolite produced by industrial pollutant through post-mitochondrial liver fraction from Aroclor-1254 induced rats.
|
-
- HY-141005
-
-
- HY-P2279
-
-
- HY-N1347
-
Robinetin
3,3',4',5',7-Pentahydroxyflavone
|
Fungal
HIV Integrase
Bacterial
|
Infection
|
Robinetin (3,3',4',5',7-Pentahydroxyflavone), a naturally occurring flavonoid with remarkable ‘two color’ intrinsic fluorescence properties, has antifungal, antiviral, antibacterial, antimutagenesis, and antioxidant activity. Robinetin also can inhibit lipid peroxidation and protein glycosylation.
|
-
- HY-111388B
-
SEL120-34A HCl
|
CDK
|
Cancer
|
SEL120-34A HCl is a potent, selective, orally available, ATP-competitive CDK8 inhibitor, with IC50s of 4.4 nM and 10.4 nM for CDK8/CycC and CDK19/CycC, respectively, with antitumor activity.
|
-
- HY-Z0548
-
-
- HY-133604
-
3,4,5-Trichloroveratrole
|
Others
|
Others
|
3,4,5-Trichloroveratrole is one of the biodegradation products of bacterial O-methylation of Tri- and Tetra chloroguaiacols. The Tri- and Tetra chloroguaiacols are formed during bleaching of wood pulp in the paper manufacturing industry.
|
-
- HY-N7690
-
3,5,7,3′,4′-Pentamethoxyflavone
|
Others
|
Metabolic Disease
|
3,5,7,3′,4′-Pentamethoxyflavone is a polymethoxyflavonoid that can be extracted from Kaempferia parviflora. 3,5,7,3′,4′-Pentamethoxyflavone can induce adipogenesis on 3T3-L1 preadipocytes by regulating transcription factors at an early stage of differentiation.
|
-
- HY-Y0084
-
3,4,5-Trimethoxybenzoic acid
Eudesmic acid; Trimethylgallic Acid
|
Others
|
Others
|
3,4,5-Trimethoxybenzoic acid (Eudesmic acid;Trimethylgallic Acid) is a benzoic acid derivative. A building block in medicine and organic synthesis.
|
-
- HY-P1586
-
HIV-1 Rev 34-50
HIV-1 rev Protein (34-50)
|
HIV
|
Infection
|
HIV-1 Rev (34-50) is a 17-aa peptide derived from the Rev-responsive element (RRE)-binding domains of Rev in HIV-1, with anti-HIV-1 activity.
|
-
- HY-N0523
-
-
- HY-N0523A
-
-
- HY-N7428
-
-
- HY-W008437
-
-
- HY-100511
-
Benzophenonetetracarboxylic acid
3,3',4,4'-Benzophenonetetracarboxylic acid
|
Others
|
Others
|
Benzophenonetetracarboxylic acid (3,3',4,4'-Benzophenonetetracarboxylic acid) is particularly useful in the preparation of high performance polyimides and also useful as curing agents for epoxy resins.
|
-
- HY-N2038
-
3,5,6,7,8,3',4'-Heptemthoxyflavone
|
Others
|
Cancer
Neurological Disease
|
3,5,6,7,8,3',4'-heptamethoxyflavone, a flavonoid in C. unshiu peels, exhibits anti-tumor-initiating effect and Anti-neuroinflammatory activity. 3,5,6,7,8,3',4'-heptamethoxyflavone inhibits collagenase activity and increased type I procollagen content in HDFn cells. 3,5,6,7,8,3',4'-heptamethoxyflavone induces brain-derived neurotrophic factor (BDNF) expression via cAMP/ERK/CREB signaling and reduces phosphodiesterase activity in C6 cells.
|
-
- HY-N1753
-
-
- HY-N2009
-
3-O-Methylgallic acid
3,4-Dihydroxy-5-methoxybenzoic acid
|
Apoptosis
|
Cancer
|
3-O-Methylgallic acid (3,4-Dihydroxy-5-methoxybenzoic acid) is an anthocyanin metabolite and has potent antioxidant capacity. 3-O-methylgallic acid inhibits Caco-2 cell proliferation with an IC50 value of 24.1 μM. 3-O-methylgallic acid also induces cell apoptosis and has anti-cancer effects.
|
-
- HY-N4311
-
-
- HY-N7029
-
3',4',5',5,7-Pentamethoxyflavone
|
Others
|
Cancer
|
3',4',5',5,7-Pentamethoxyflavone, a natural flavonoid extracted from Rutaceae plants, sensitizes chemoresistant cancer cells to chemotherapeutic drugs by inhibition of Nrf2 pathway.
|
-
- HY-N6829
-
Retusin
Quercetin-3,3',4',7-tetramethylether
|
Others
|
Infection
Inflammation/Immunology
|
Retusin (Quercetin-3,3',4',7-tetramethylether), a natural compound isolated from the leaves of Talinum triangulare, possesses antiviral and anti-inflammatory activities.
|
-
- 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-B1805
-
Triclocarban
3,4,4′-Trichlorocarbanilide
|
Bacterial
|
Infection
|
Triclocarban (3,4,4′-Trichlorocarbanilide), a broad spectrum antibacterial compound, is widely used in a broad range of applications such as the production of soaps, skin creams, toothpastes and deodorants. Triclocarban is a potential endocrine-disrupting chemical with the capacity to modulate androgen and estrogen activities as well as other hormone-mediated biological processes.
|
-
- HY-P2510
-
-
- HY-12403
-
Angiotensin (1-7)
Ang-(1-7)
|
Angiotensin Receptor
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
Cardiovascular Disease
Endocrinology
|
Angiotensin 1-7 (Ang-(1-7)) is a major active component of the renin-angiotensin system (RAS), produced from cleavage of Ang II by angiotensin-converting-enzyme type 2 (ACE2). Angiotensin 1-7 inhibits purified canine ACE activity (IC50=0.65 μM). Angiotensin 1-7 acts as a local synergistic modulator of kinin-induced vasodilation by inhibiting ACE and releasing nitric oxide. Angiotensin 1-7 blocks Ang II-induced smooth muscle cell proliferation and hypertrophy and shows antiangiogenic and growth-inhibitory effects on the endothelium. Angiotensin 1-7 shows anti-inflammatory activity .
|
-
- HY-N5030
-
8-Hydroxy-3,5,6,7,3',4'-hexamethoxyflavone
|
Others
|
Others
|
8-Hydroxy-3,5,6,7,3',4'-hexamethoxyflavone is a polymethoxyflavone (PMF) isolated from pericarpium citri reticulatae.
|
-
- HY-P1324
-
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide
|
Neuropeptide Y Receptor
|
Neurological Disease
|
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.
|
-
- HY-P1324A
-
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic polypeptide TFA
|
Neuropeptide Y Receptor
|
Neurological Disease
|
[cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide is a potent and selective neuropeptide Y Y5 receptor agonist with an IC50 of 0.24 nM for binding to the hY5 receptor. [cPP1-7,NPY19-23,Ala31,Aib32,Gln34]-hPancreatic Polypeptide induces a high amount of food intake.
|
-
- HY-141137
-
-
- HY-135591
-
-
- HY-N2207
-
-
- HY-19340
-
TMS
(E)-2,3',4,5'-tetramethoxystilbene
|
Cytochrome P450
|
Cancer
|
TMS ((E)-2,3',4,5'-tetramethoxystilbene) is a selective and competitive CYP1B1 inhibitor with an IC50 of 6 nM and a Ki value of 3 nM. TMS shows a lesser extent inhibitory effect on CYP1A1 (IC5050
|
-
- HY-13987
-
-
- HY-141139
-
-
- HY-W040240
-
(3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one
|
Endogenous Metabolite
|
Metabolic Disease
|
(3S,4R,5S)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.
|
-
- 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-N0652
-
2,3,5,4'-Tetrahydroxystilbene 2-O-β-D-glucoside
2,3,4',5-Tetrahydroxystilbene 2-O-D-glucoside
|
Others
|
Others
|
2,3,4',5-tetrahydroxystilbene 2-O-D-glucoside isolats from the roots of Polygonum species, inhibits the formation of 5-HETE, HHT and thromboxane B2, although less strongly.
|
-
- HY-42680
-
(3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one
Tagatose, D- (8CI)
|
Endogenous Metabolite
|
Metabolic Disease
|
(3S,4S,5R)-1,3,4,5,6-Pentahydroxyhexan-2-one is an endogenous metabolite.
|
-
- HY-N0252
-
-
- HY-70061
-
-
- HY-U00439
-
-
- HY-12594
-
Paritaprevir
ABT-450; Veruprevir
|
HCV Protease
HCV
|
Infection
|
Paritaprevir (ABT-450) is a potent non-structural protein 3/4A (NS3/4A) protease inhibitor with EC50s of 1 and 0.21 nM against HCV 1a and 1b, respectively.
|
-
- HY-N0294
-
-
- HY-W050145
-
(1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol
|
Endogenous Metabolite
|
Metabolic Disease
|
(1R,2S,3S,4R,5S)-6,8-Dioxabicyclo[3.2.1]octane-2,3,4-triol is an endogenous metabolite.
|
-
- HY-19677
-
Cipemastat
Ro 32-3555
|
MMP
|
Cancer
|
Cipemastat is a potent, competitive inhibitor of human collagenases 1, 2 and 3 with Kis of 3.0, 4.4 and 3.4 nM, respectively.
|
-
- HY-17634
-
-
- HY-B2136
-
-
- HY-15485
-
-
- HY-101920
-
Autophinib
|
Autophagy
|
Cancer
Neurological Disease
|
Autophinib is a potent, selective autophagy inhibitor with IC50s of 90 nM and 40 nM for starvation- and Rapamycin-induced autophagy, respectively. Autophinib is also an ATP competitive Vacuolar Protein Sorting 34 (VPS34) inhibitor with an IC50 of 19 nM. Autophinib inhibits autophagy induced by starvation or Rapamycin by targeting VPS34.
|
-
- HY-18771
-
-
- HY-N0252A
-
-
- HY-10452
-
Ixazomib citrate
MLN9708
|
Proteasome
Autophagy
|
Cancer
|
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
|
-
- HY-12481A
-
-
- HY-10241
-
Simeprevir
TMC435
|
HCV
HCV Protease
|
Infection
|
Simeprevir (TMC435) is an oral and potent HCV NS3/4A protease inhibitor with a Ki of 0.36 nM, and inhibits HCV replication with an EC50 of 7.8 nM.
|
-
- HY-12873
-
RBC8
|
Ras
|
Cancer
|
RBC8 is a novel small molecule inhibitor of Ral GTPase; has IC50 of 3.5 μM in H2122 cell and 3.4 μM in H358 cell.
|
-
- HY-18563
-
4-Phenoxybenzylamine
|
HCV
|
Infection
|
4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC50 of about 500 μM against FL NS3/4a.
|
-
- HY-10453
-
Ixazomib
MLN2238
|
Proteasome
Autophagy
|
Cancer
|
Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
|
-
- HY-N2406
-
-
- HY-W015346
-
-
- HY-124772
-
-
- 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-112376
-
-
- HY-112377
-
-
- HY-50874
-
-
- HY-19863
-
-
- HY-W008923
-
-
- HY-50875
-
-
- HY-15260A
-
XL413 hydrochloride
|
CDK
|
Cancer
|
XL413 hydrochloride is a potent, selective and ATP competitive inhibitor of Cdc7, with an IC50 of 3.4 nM, and also shows potent effect with IC50s of 215, 42 nM on CK2, PIM1, respectively, and an EC50 of 118 nM on pMCM.
|
-
- HY-141003
-
-
- HY-A0296
-
Chlormethiazole hydrochloride
Clomethiazole hydrochloride
|
Others
|
Neurological Disease
|
Clomethiazole hydrochloride is a sedative and anticonvulsant. Clomethiazole hydrochloride is neuroprotective and prevents the degeneration of serotonergic nerve terminals induced by 3,4-methylenedioxymethamphetamine (MDMA).
|
-
- HY-107377
-
Benzo[a]pyrene
3,4-Benzopyrene
|
Others
|
Cancer
|
Benzo[a]pyrene shows lung carcinogenicity in animal models, and it is frequently used in chemoprevention studies.
|
-
- HY-N0304
-
L-DOPA
Levodopa; 3,4-Dihydroxyphenylalanine
|
Dopamine Receptor
Endogenous Metabolite
|
Neurological Disease
|
L-DOPA (Levodopa) is an orally active metabolic precursor of neurotransmitters dopamine. L-DOPA can cross the blood-brain barrier and is converted into dopamine in the brain. L-DOPA has anti-allodynic effects and the potential for Parkinson's disease.
|
-
- HY-10238
-
Danoprevir
ITMN-191; R7227; RO5190591; RG7227
|
HCV Protease
HCV
|
Infection
|
Danoprevir (ITMN-191) is an orally active NS3/4A protease inhibitor for hepatitis C virus (HCV) with an IC50 of 0.29 nM and is selective for NS3/4A over a panel of 53 proteases (IC50 higher than 10 μM). Danoprevir (ITMN-191) inhibits HCV genotypes 1a, 1b, 4, 5, and 6 (IC50s=0.2-0.4 nM) as well as 2b and 3a (IC50s=1.6, 3.5 nM).
|
-
- HY-P0216
-
-
- HY-15778A
-
-
- HY-111400
-
SR-4370
|
HDAC
|
Cancer
|
SR-4370 is an inhibitor of HDAC, with IC50s of 0.13 μM, 0.58 μM, 0.006 μM, 2.3 μM, and 3.4 μM for HDAC1, HDAC2, HDAC3, HDAC8, and HDAC6, respectively.
|
-
- 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-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-101428
-
NS-638
|
Calcium Channel
|
Neurological Disease
|
NS-638 is a small nonpeptide molecule with Ca 2+-channel blocking properties. K +-stimulated intracellular Ca 2+-elevation is blocked with an IC50 value of 3.4 μM.
|
-
- HY-15472
-
-
- HY-13270
-
ABT-751
E7010
|
Microtubule/Tubulin
Autophagy
|
Cancer
|
ABT-751(E 7010) is a novel bioavailable tubulin-binding and antimitotic sulfonamide agent with IC50 of about 1.5 and 3.4 μM in neuroblastoma and non-neuroblastoma cell lines, respectively.
|
-
- HY-10235
-
Telaprevir
VX-950
|
HCV Protease
HCV
|
Infection
|
Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide.
|
-
- HY-100352
-
BI-9564
|
Epigenetic Reader Domain
|
Cancer
|
BI-9564 is a potent, selective and cell-permeable BRD9/BRD7 bromodomains inhibitor, with IC50s of 75 nM and 3.4 μM and Kds of 14 nM and 239 nM, respectively. BI-9564 has an IC50 of > 100 μM for BET family.
|
-
- HY-10126
-
Barasertib-HQPA
AZD2811; INH-34; AZD1152-HQPA
|
Aurora Kinase
Apoptosis
|
Cancer
|
Barasertib-HQPA (AZD2811) is a highly selective Aurora B inhibitor with an IC50 of 0.37 nM in a cell-free assay. Barasertib-HQPA (AZD2811) induces growth arrest and apoptosis in cancer cells.
|
-
- HY-133553
-
RET-IN-3
|
RET
|
Cancer
|
RET-IN-3 (compound 34) is a selective RETV804M kinase inhibitor, with an IC50 of 19 nM.
|
-
- HY-W008566
-
-
- HY-18772
-
O4I2
|
Oct3/4
|
Others
|
O4I2 is a potent Oct3/4 inducer. O4I2 induces the expression of pluripotent-associated genes Lin28, Sox2 and Nanog, and suppresses Rex1.
|
-
- HY-B0233
-
-
- HY-N1584
-
Halofuginone
RU-19110
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
|
Inflammation/Immunology
Cancer
|
Halofuginone (RU-19110) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity.
|
-
- HY-15895
-
-
- HY-126146
-
-
- HY-U00171
-
SQ28603
SQ28,603; Squibb 28603
|
Neprilysin
|
Metabolic Disease
|
SQ28603 is a potent and selective inhibitor of neutral endopeptidase 3.4.24.11 (NEP), an enzyme that degrades atrial natriuretic peptide (ANP).
|
-
- HY-13461A
-
-
- HY-13783
-
BIBF0775
|
TGF-β Receptor
|
Cancer
|
BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
|
-
- HY-15670
-
BMS-906024
|
γ-secretase
Notch
|
Cancer
|
BMS-906024 is an orally active and selective γ-secretase (gamma secretase) inhibitor. BMS-906024 is a potent pan-Notch receptors inhibitor with IC50s of 1.6 nM, 0.7 nM, 3.4 nM, and 2.9 nM for Notch1, -2, -3, and -4 receptors, respectively. BMS-906024 demonstrates broad-spectrum antineoplastic activity.
|
-
- HY-N1584A
-
Halofuginone hydrobromide
RU-19110 hydrobromide
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
|
Inflammation/Immunology
Cancer
|
Halofuginone hydrobromide (RU-19110 hydrobromide) is a less-toxic form of Febrifugine, which is isolated from the plant Dichroa febrifuga. Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity.
|
-
- HY-N0570
-
-
- HY-10969
-
Obatoclax Mesylate
GX15-070 Mesylate
|
Bcl-2 Family
Autophagy
Parasite
|
Cancer
Infection
|
Obatoclax Mesylate (GX15-070 Mesylate), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax Mesylate induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax Mesylate has anti-cancer and broad-spectrum antiparasitic activity.
|
-
- HY-15298C
-
Grazoprevir sodium salt
MK-5172 (sodium salt)
|
HCV
HCV Protease
|
Infection
|
Grazoprevir sodium salt (MK-5172 sodium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-15298B
-
Grazoprevir hydrate
MK-5172 hydrate
|
HCV
HCV Protease
|
Infection
|
Grazoprevir hydrate (MK-5172 hydrate) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-15298
-
Grazoprevir
MK-5172
|
HCV Protease
HCV
|
Infection
|
Grazoprevir (MK-5172) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-10969A
-
Obatoclax
GX15-070
|
Bcl-2 Family
Autophagy
Parasite
|
Cancer
Infection
|
Obatoclax (GX15-070), a BH3 mimetic, is a pan-BCL-2 family proteins inhibitor with a Ki of 220 nM for BCL-2. Obatoclax induces autophagy-dependent cell death and targets cyclin D1 for proteasomal degradation. Obatoclax has anti-cancer and broad-spectrum antiparasitic activity.
|
-
- HY-15298A
-
Grazoprevir potassium salt
MK-5172 (potassium salt)
|
HCV
HCV Protease
|
Infection
|
Grazoprevir potassium salt (MK-5172 potassium salt) is a selective inhibitor of Hepatitis C virus NS3/4a protease with broad activity across genotypes and resistant variants, with Kis of 0.01 nM (gt1b), 0.01 nM (gt1a), 0.08 nM (gt2a), 0.15 nM (gt2b), 0.90 nM (gt3a), respectively.
|
-
- HY-111663
-
-
- HY-109121
-
Reldesemtiv
CK-2127107
|
Others
|
Cardiovascular Disease
|
Reldesemtiv (CK-2127107) is a selective, orally active and next-generation fast skeletal muscle troponin activator (FSTA). Reldesemtiv selectively activates fast skeletal myofibrils with an EC50 of 3.4 μM. Reldesemtiv increases exercise performance in a heart failure model.
|
-
- HY-N2129
-
-
- HY-15743
-
-
- HY-112065
-
-
- HY-22385
-
-
- 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-15225
-
Telomestatin
|
Telomerase
ADC Cytotoxin
|
Cancer
|
Telomestatin is a very potent telomerase inhibitor and can be isolated from Streptomyces anulatus 3533-SV4. Telomestatin selectively facilitates the formation of intramolecular G-quadruplexes, in particular, that produced from the human telomeric sequence d[T2AG3]4. Telomestatin is an ADC cytotoxin and can be used for cancer research.
|
-
- HY-A0077
-
Perphenazine
|
5-HT Receptor
Adrenergic Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
Perphenazine is a typical antipsychotic drug, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
|
-
- HY-10811
-
GNE-493
|
PI3K
mTOR
|
Cancer
|
GNE-493 is a potent, selective, and orally available dual pan-PI3-kinase/mTOR inhibitor with IC50s of 3.4 nM, 12 nM, 16 nM, 16 nM and 32 nM for PI3Kα, PI3Kβ, PI3Kδ, PI3Kγ and mTOR.
|
-
- HY-19363
-
-
- HY-19840
-
Voxilaprevir
GS-9857
|
HCV Protease
|
Infection
|
Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity. Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively. Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research.
|
-
- HY-10259
-
-
- HY-10259A
-
-
- HY-N7112
-
-
- HY-121526
-
-
- HY-B1490
-
-
- HY-W091541
-
4-Hydroxy-1H-indole-3-carbaldehyde
4-Hydroxyindole-3-carboxaldehyde
|
Others
|
Others
|
4-Hydroxy-1H-indole-3-carbaldehyde is a plant metabolite found in Capparis spinosa L.. 4-Hydroxy-1H-indole-3-carbaldehyde can be used in the synthesis of fluorescent probe.
|
-
- HY-15602
-
Ledipasvir
GS-5885
|
HCV
|
Infection
|
Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50s of 34 pM and 4 pM against genotype 1a and 1b replicon, respectively.
|
-
- HY-108261
-
Tomeglovir
BAY 38-4766
|
CMV
|
Infection
|
Tomeglovir is a potent anti-CMV agent, inhibiting processing of viral DNA-concatemers, with IC50s of 0.34 μM and 0.039 μM for HCMV and MCMV.
|
-
- HY-15591A
-
TMC647055 Choline salt
|
HCV
|
Infection
|
TMC647055 choline salt is a cell-permeating, selective HCV NS5B inhibitor, eliciting a mean IC50 of 34 nM, as assessed in the RdRp primer-dependent transcription assay.
|
-
- HY-131180
-
BMS-986235
LAR-1219
|
Others
|
Cardiovascular Disease
|
BMS-986235 (LAR-1219) is a selective, orally active formyl peptide receptor 2 (FPR2) agonist, with EC50s of 0.41 nM and 3.4 nM for hFPR2 and mFPR2, respectively. BMS-986235 has potential for the prevention of heart failure.
|
-
- HY-N2359
-
Chelerythrine
|
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
|
-
- HY-14542
-
Ziprasidone
CP-88059
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Ziprasidone, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone is an inhibitor of norepinephrine reuptake.
|
-
- HY-19834
-
Fenebrutinib
GDC-0853
|
Btk
|
Cancer
|
Fenebrutinib (GDC-0853) is a potent, selective, orally available, and noncovalent bruton's tyrosine kinase (Btk) inhibitor with Kis of 0.91 nM, 1.6, 1.3, 12.6, and 3.4 nM for WT Btk, and the C481S, C481R, T474I, T474M mutants. Fenebrutinib has the potential for rheumatoid arthritis and systemic lupus erythematosus research.
|
-
- HY-P0227
-
SHU 9119
|
Melanocortin Receptor
|
Metabolic Disease
|
SHU 9119 is a potent human melanocortin 3 and 4 receptors (MC3/4R) antagonist and a partial MC5R agonist; with IC50 values of 0.23, 0.06, and 0.09 nM for human MC3R, MC4R and MC5R, respectively.
|
-
- HY-15895S
-
Aprocitentan D4
ACT-132577 D4
|
Endothelin Receptor
|
Endocrinology
Cardiovascular Disease
|
Aprocitentan D4 (ACT-132577 D4) is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively.
|
-
- HY-12887
-
-
- HY-100517
-
-
- HY-12449
-
Crenigacestat
LY3039478
|
Notch
γ-secretase
|
Cancer
|
Crenigacestat (LY3039478) is an orally active Notch and γ-secretase inhibitor, with an IC50 of 1 nM in most of the tumor cell lines tested.
|
-
- HY-14542A
-
Ziprasidone hydrochloride
CP-88059 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Ziprasidone (CP-88059) hydrochloride, an antipsychotic agent, is a combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone hydrochloride has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone hydrochloride is an inhibitor of norepinephrine reuptake.
|
-
- HY-15602B
-
Ledipasvir D-tartrate
GS-5885 D-tartrate
|
HCV
|
Infection
|
Ledipasvir D-tartrate is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
|
-
- HY-101191
-
Ecteinascidin 770
Ecteinascidine 770; Et-770
|
Apoptosis
|
Cancer
|
Ecteinascidin 770 (ET-770) is a 1,2,3,4-tetrahydroisoquinoline alkaloid with potent anti-cancer activities; inhibits U373MG cells with an IC50 of 4.83 nM.
|
-
- HY-W002587
-
-
- HY-107623
-
TC-MCH 7c
|
MCHR1 (GPR24)
|
Metabolic Disease
|
TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH1R antagonist with an IC50 of 5.6 nM for hMCH1R. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.
|
-
- HY-12031A
-
-
- HY-17407
-
Ziprasidone hydrochloride monohydrate
CP 88059 hydrochloride monohydrate
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
Ziprasidone (CP 88059) hydrochloride monohydrate, an antipsychotic agent, is an orally active combined 5-HT (serotonin) and dopamine receptor antagonist. Ziprasidone hydrochloride monohydrate has high affinity for rat (Ki: 3.4 nM)/human (2.5 nM) 5-HT1A receptors, 5-HT2A (0.42 nM), and dopamine D2 receptors (4.8 nM). Ziprasidone hydrochloride monohydrate is an inhibitor of norepinephrine reuptake.
|
-
- HY-101860
-
-
- HY-B1138
-
Fenbufen
CL-82204
|
COX
Caspase
|
Inflammation/Immunology
|
Fenbufen is an orally active non-steroidal anti-inflammatory drug (NSAID), with analgetic and antipyretic effects. Fenbufen has potent activity in a variety of animal model, including carageenin edema, UV erythema and adjuvant arthritis. Fenbufen has inhibitory activities against COX-1 and COX-2 with IC50s of 3.9 μM and 8.1 μM, respectively. Fenbufen is a caspases (caspase-1, 3, 4, 5, 9) inhibitor.
|
-
- HY-103225
-
-
- HY-125880
-
-
- HY-131005
-
-
- HY-B0879A
-
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
-
- HY-111508
-
PI3K/mTOR Inhibitor-2
|
PI3K
mTOR
|
Cancer
|
PI3K/mTOR Inhibitor-2 is a potent dual pan-PI3K/mTOR inhibitor with IC50s of 3.4/34/16/1 nM for PI3Kα/PI3Kβ/PI3Kδ/PI3Kγ and 4.7 nM for mTOR. Antitumor activity.
|
-
- HY-15843
-
MIR96-IN-1
|
MicroRNA
Apoptosis
|
Cancer
|
MIR96-IN-1 targets the Drosha site in the miR-96 hairpin precursor, inhibiting its biogenesis, derepressing downstream targets, and triggering apoptosis in breast cancer cells. MIR96-IN-1 binds to RNAs with Kds of 1.3, 9.4, 3.4, 1.3 and 7.4 μM for RNA1, RNA2, RNA3, RNA4 and RNA5, respectively.
|
-
- HY-107795
-
-
- HY-N0872
-
-
- HY-11004
-
AZ 628
|
Raf
Apoptosis
|
Cancer
|
AZ 628 is a pan-Raf kinase inhibitor with IC50s of 105, 34 and 29 nM for B-Raf, B-RafV600E, and c-Raf-1, respectively.
|
-
- HY-135317
-
-
- HY-W013706
-
-
- HY-U00122
-
-
- HY-12341
-
ML355
|
Lipoxygenase
|
Inflammation/Immunology
|
ML355 is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 0.34 μM, shows excellent selectivity over related lipoxygenases and cyclooxygenases, and possesses favorable ADME properties.
|
-
- HY-13515
-
-
- HY-12012
-
-
- HY-15301
-
CC0651
|
E1/E2/E3 Enzyme
|
Cancer
|
CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27 Kip1, as confirmed by dose-response analysis.
|
-
- HY-18708
-
Erdafitinib
JNJ-42756493
|
FGFR
Apoptosis
|
Cancer
|
Erdafitinib (JNJ-42756493) is a potent and orally available FGFR family inhibitor; inhibits FGFR1/2/3/4 with IC50s of 1.2, 2.5, 3.0 and 5.7 nM, respectively.
|
-
- HY-126750
-
GNF362
|
Phosphatase
|
Inflammation/Immunology
|
GNF362 is a selective, potent, and orally bioavailable inhibitor of inositol trisphosphate 3’ kinase B (Itpkb) with an IC50 of 9 nM. GNF362 also inhibits Itpka and Itpkc with IC50 values of 20 nM and 19 nM, respectively. Inositol trisphosphate 3’ kinase B (Itpkb) is a Ca 2+-dependent kinase, which phosphorylates the 3’ position of Ins (1,4,5) P3 to generate inositol 1,3,4,5-tetrakisphosphate [Ins (1,3,4,5) P4].
|
-
- HY-N6782
-
Oligomycin
|
ATP Synthase
Fungal
Antibiotic
|
Cancer
Infection
|
Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells.
|
-
- HY-13016
-
-
- HY-120088A
-
-
- HY-101957
-
AG 1295
|
PDGFR
|
Cardiovascular Disease
|
AG 1295 is a selective platelet-derived growth factor receptor (PDGFR) tyrosine-kinase inhibitor. AG1295 abolishes autophosphorylation of the PDGFR whereas not affects the autophosphorylation of the EGF receptor.
|
-
- HY-N2575
-
Hypocrellin A
|
PKC
|
Cancer
Infection
|
Hypocrellin A, a naturally occurring PKC inhibitor, has many biological and pharmacological properties, such as antitumour, antiviral, antibacterial, and antileishmanial activities. Hypocrellin A is a promising photosensitizer for anticancer photodynamic therapy (PDT).
|
-
- HY-130122
-
MG-277
|
PROTAC
Apoptosis
|
Cancer
|
MG-277, a molecular glue degrader, effectively induces degradation of a translation termination factor, GSPT1, with a DC50 of 1.3 nM. MG-277 potently inhibits tumor cell growth in a p53-independent manner, with IC50s of 3.5 nM for RS4;11 cells and 3.4 nM for p53 mutant RS4;11/IRMI-2 cells, respectively. Anticancer activity.
|
-
- 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-N0834
-
-
- HY-10935
-
-
- HY-126525
-
-
- HY-13685
-
Miltefosine
HePC; Hexadecyl phosphocholine
|
Akt
HIV
|
Infection
Cancer
|
Miltefosine is a broad spectrum antimicrobial, anti-leishmanial, phospholipid agent acting by inhibiting the PI3K/Akt activity. Miltefosine is an inhibitor of CTP-phosphocholine cytidyltransferase (CCT).
|
-
- HY-103443
-
HKI-357
|
EGFR
|
Cancer
|
HKI-357 is an irreversible dual inhibitor of EGFR and ERBB2 with IC50s of 34 nM and 33 nM, respectively. HKI-357 suppresses EGFR autophosphorylation (at Y1068), and AKT and MAPK phosphorylation.
|
-
- HY-10460
-
PF-431396
|
Pyk2
FAK
|
Cancer
|
PF-431396 is an orally active dual focal adhesion kinase (FAK) and proline-rich tyrosine kinase 2 (PYK2) inhibitor, with IC50 values of 2 nM and 11 nM, respectively.
|
-
- HY-136610
-
Chlorpyrifos-oxon
|
AChE
|
Neurological Disease
|
Chlorpyrifos-oxon, an active metabolite of Chlorpyrifos, is a potent phosphorylating agent that potently inhibits AChE. Chlorpyrifos-oxon can induce cross-linking between subunits of tubulin and disrupt microtubule function.
|
-
- HY-13564A
-
Batimastat sodium salt
BB-94 sodium salt
|
MMP
|
Cancer
|
Batimastat sodium salt is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
|
-
- HY-B0190A
-
-
- HY-B0190
-
-
- HY-13564
-
Batimastat
BB94
|
MMP
|
Cancer
|
Batimastat is a potent broad spectrum MMP inhibitor with IC50 of 3, 4, 4, 6, and 20 nM for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3, respectively.
|
-
- HY-B0190B
-
-
- HY-B1813A
-
(±)-Vesamicol hydrochloride
(±)-AH5183 hydrochloride
|
Sigma Receptor
|
Neurological Disease
|
(±)-Vesamicol hydrochloride ((±)-AH5183 hydrochloride) is a potent vesicular acetylcholine transport inhibitor with a Ki of 2 nM. (±)-Vesamicol hydrochloride also displays high affinity for σ1 and σ2 receptors with Kis of 26 nM and 34 nM, respectively.
|
-
- HY-12031
-
-
- HY-P1236
-
-
- HY-127039
-
-
- HY-127034
-
-
- HY-136559
-
-
- HY-131059
-
CBS1117
|
Influenza Virus
|
Infection
|
CBS1117 is a virus entry inhibitor with an IC50 of 70 nM for influenza A virus, A/Puerto Rico/8/34 (H1N1). CBS1117 interferes with the hemagglutinin (HA)-mediated fusion process.
|
-
- HY-Y0892
-
-
- HY-B0975
-
Penicillin V Potassium
Phenoxymethylpenicillin potassium salt
|
Bacterial
Antibiotic
|
Infection
|
Penicillin V Potassium (Phenoxymethylpenicillin potassium salt) is an orally active antibiotic. Penicillin V Potassium inhibits the growth of Streptococci, C. difficile and S. aureus. Penicillin V Potassium can be used for the research of otitis, sinusitis, pharyngitis and tonsillitis.
|
-
- HY-10162
-
Olaparib
AZD2281; KU0059436
|
PARP
Autophagy
Mitophagy
|
Cancer
|
Olaparib (AZD2281; KU0059436) is a potent and orally active PARP inhibitor with IC50s of 5 and 1 nM for PARP1 and PARP2, respectively. Olaparib is an autophagy and mitophagy activator.
|
-
- HY-136195
-
TL13-110
|
ALK
|
Cancer
|
TL13-110 is a negative control for TL13-112 (HY-123919) and a potent ALK inhibitor with an IC50 of 0.34 nM. TL13-110 does not degrade ALK in cells.
|
-
- HY-P1204
-
[Ala17]-MCH
|
MCHR1 (GPR24)
|
Metabolic Disease
|
[Ala17]-MCH, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu 3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.
|
-
- HY-130241
-
Reverse transcriptase-IN-1
|
HIV
|
Infection
|
Reverse transcriptase-IN-1 (Compound 12z), a diarylbenzopyrimidine (DABP) analogue, is a potent, orally active HIV-1 nonnucleoside reverse transcriptase inhibitor. Reverse transcriptase-IN-1 has antiviral activity with EC50 values of 3.4 nM, 4.3 nM and 3.6 nM for HIV-1 IIIB, E138K and K103N mutants, respectively. Reverse transcriptase-IN-1 also has an IC50of 13.7 nM against HIV-1 reverse transcriptase enzyme.
|
-
- HY-P1236A
-
-
- HY-12429
-
Beclabuvir
BMS-791325
|
HCV
|
Infection
|
Beclabuvir is an allosteric inhibitor that binds to thumb site 1 of the hepatitis C virus (HCV) NS5B RNA-dependent RNA polymerase, and inhibits recombinant NS5B proteins from HCV genotypes 1, 3, 4, and 5 with IC50 of < 28 nM.
|
-
- HY-13570A
-
-
- HY-13570
-
-
- HY-B0348
-
Liranaftate
Piritetrate; M-732
|
Fungal
|
Infection
|
Liranaftate (Piritetrate) is a squalene epoxidase inhibitor with anti-fungicidal activities. Liranaftate can be used for the research of dermatophytes. Liranaftate also suppresses fungal element-promoted production of IL-8 and experimental inflammation.
|
-
- HY-15602A
-
Ledipasvir (acetone)
GS-5885 acetone
|
HCV
|
Infection
|
Ledipasvir acetone (GS-5885 acetone) is the active ingredient of Ledipasvir. Ledipasvir is an inhibitor of the hepatitis C virus NS5A, with EC50 values of 34 pM against GT1a and 4 pM against GT1b replicon.
|
-
- HY-13524A
-
-
- HY-15141
-
-
- HY-131905S
-
BMS-986144
|
HCV Protease
HCV
|
Cancer
Infection
Inflammation/Immunology
|
BMS-986144 is a third-generation, pan-genotype (GT) NS3/4A protease inhibitor. BMS-986144 inhibits HCV replicon with EC50s of 2.3, 0.7, 1.0, 12, 8.0, and 5.8 nM for GT-1a, GT-1b, GT-2a, GT-3a, 1a R155X, and 1b D168V, respectively. BMS-986144 has the potential for the research of HCV infection.
|
-
- HY-P1204A
-
[Ala17]-MCH TFA
|
MCHR1 (GPR24)
|
Metabolic Disease
|
[Ala17]-MCH TFA, a MCH analogue (HY-P1525A), is a selective ligand for MCHR1 (Ki=0.16 nM) over MCHR2 (Ki=34 nM). [Eu 3+ chelate-labeled [Ala17]-MCH shows high affnity for MCHR1 (Kd=0.37 nM) while has little demonstrable binding affnity for MCHR2.
|
-
- HY-N0720
-
Neobavaisoflavone
|
Apoptosis
DNA/RNA Synthesis
|
Cancer
|
Neobavaisoflavone, a flavonoid, is isolated from the seeds of Psoralea corylifolia. Neobavaisoflavone exhibits anti-inflammatory, anti-cancer and anti-oxidation activities. Neobavaisoflavone inhibits DNA polymerase at moderate to high concentrations. Neobavaisoflavone also inhibits platelet aggregation.
|
-
- HY-B1479C
-
-
- HY-B1479
-
-
- HY-B1479B
-
-
- HY-A0213A
-
Tiludronate disodium
Tiludronic Acid disodium
|
Proton Pump
|
Inflammation/Immunology
|
Tiludronate (Tiludronic Acid) disodium, an orally active bisphosphonate, can act an osteoregulator. Tiludronate is used for the research of the metabolic bone disorders. Tiludronate is a potent inhibitor of the osteoclast vacuolar H(+)-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- HY-41076
-
-
- HY-125658
-
Biotinyl tyramide
|
Others
|
Others
|
Biotinyl tyramide is a biotin derivative used for tyramide signal amplification (TSA), as a reagent to amplify both immunohistochemical signals and in situ hybridization protocols.
|
-
- HY-N0344
-
-
- HY-B1370A
-
-
- HY-12044
-
Cabozantinib S-malate
XL184 S-malate; BMS-907351 S-malate
|
VEGFR
Apoptosis
|
Cancer
|
Cabozantinib S-malate (XL184 S-malate) is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively.
|
-
- HY-114416
-
GS-626510
|
Epigenetic Reader Domain
|
Cancer
|
GS-626510 is a potent, and orally active BET family bromodomains inhibitor, with Kd values of 0.59-3.2 nM for BRD2/3/4, with IC50 values of 83 nM and 78 nM foe BD1 and BD2, respectively.
|
-
- HY-B0640
-
-
- 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-100443A
-
-
- HY-106244A
-
DOTATATE acetate
|
Others
|
Cancer
|
DOTATATE acetate is a DOTA-conjugated peptide. DOTATATE acetate can be labelled with radionuclides for positron emission tomography (PET) imaging and peptide receptor radionuclide therapy (PRRT).
|
-
- HY-B2068
-
-
- HY-10003
-
Alfacalcidol
1-hydroxycholecalciferol; 1.alpha.-Hydroxyvitamin D3
|
VD/VDR
|
Metabolic Disease
|
Alfacalcidol (1-hydroxycholecalciferol) is a vitamin D active metabolites, acts as a non-selective VDR activator medication, and widely be used in the management of osteoporosis.
|
-
- HY-106369
-
-
- HY-12842
-
UC-112
|
IAP
|
Cancer
|
UC-112 is a novel potent IAP(Inhibitor of apoptosis) inhibitor; potently inhibit cell growth in two human melanoma (A375 and M14) and two human prostate (PC-3 and DU145) cancer cell lines(IC50=0.7-3.4 uM).
|
-
- HY-B1370B
-
-
- HY-A0213B
-
Tiludronate disodium hemihydrate
Tiludronic acid disodium hemihydrate
|
Proton Pump
|
Metabolic Disease
|
Tiludronate (Tiludronic Acid) disodium hemihydrate, an orally active bisphosphonate, can act an osteoregulator. Tiludronate disodium hemihydrate is used for the research of the metabolic bone disorders. Tiludronate disodium hemihydrate is a potent inhibitor of the osteoclast vacuolar H +-ATPase. Antiresorptive and anti-inflammatory properties.
|
-
- HY-N0889
-
Ginkgetin
|
Wnt
Apoptosis
Autophagy
|
Inflammation/Immunology
Cancer
|
Ginkgetin, a biflavone, is isolated from Ginkgo biloba leaves. Ginkgetin exhibit anti-tumor, anti-inflammatory, neuroprotective, anti-fungal activities. Ginkgetin is also a potent inhibitor of Wnt signaling, with an IC50 of 5.92 μΜ.
|
-
- HY-B1617A
-
-
- HY-17425
-
Valacyclovir
Valaciclovir
|
HSV
Antibiotic
|
Infection
|
Valacyclovir (Valaciclovir) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir is a prodrug of Aciclovir (HY-17422) [1].
|
-
- HY-101047
-
D-erythro-Sphingosine
Erythrosphingosine; erythro-C18-Sphingosine; trans-4-Sphingenine
|
PKC
Phosphatase
Endogenous Metabolite
|
Cancer
|
D-erythro-Sphingosine (Erythrosphingosine) is a very potent activator of p32-kinase with an EC50 of 8 μM, and inhibits protein kinase C (PKC). D-erythro-Sphingosine (Erythrosphingosine) is also a PP2A activator.
|
-
- HY-17425A
-
Valacyclovir hydrochloride
Valaciclovir hydrochloride
|
HSV
Antibiotic
|
Infection
|
Valacyclovir hydrochloride (Valaciclovir hydrochloride) is an orally active antiviral drug for herpes simplex, herpes zoster, and herpes B. Valacyclovir hydrochloride inhibits HSV-1 W (50=2.9 μg/ml). Valacyclovir hydrochloride is a prodrug of Aciclovir (HY-17422) [1].
|
-
- HY-100228A
-
-
- HY-B0329
-
Isoniazid
INH; Isonicotinic acid hydrazide; Isonicotinic hydrazide
|
Bacterial
Autophagy
Mitophagy
|
Infection
|
Isoniazid (INH) is a prodrug and must be activated by a bacterial catalase-peroxidase enzyme KatG. Isoniazid is bactericidal to rapidly dividing mycobacteria and has anti-tuberculostatic activity.
|
-
- HY-W030545
-
-
- HY-N0809
-
Sesamolin
|
p38 MAPK
JNK
Caspase
|
Metabolic Disease
Neurological Disease
|
Sesaminol, isolated from Justicia orbiculata, has antioxidative activity, Sesaminol inhibits lipid peroxidation and shows neuroprotection effect. Sesaminol potently inhibits MAPK cascades by preventing phosphorylation of JNK, p38 MAPKs, and caspase-3 but not ERK-MAPK expression.
|
-
- HY-13433
-
-
- HY-121879
-
-
- HY-17443
-
Sivelestat
EI546; LY544349; ONO5046
|
Elastase
SARS-CoV
|
Cancer
|
Sivelestat (EI546) is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.
|
-
- HY-17443A
-
Sivelestat sodium
ONO5046-Na; Sodium sivelestat; EI546 sodium; LY544349 sodium
|
Elastase
SARS-CoV
|
Cancer
|
Sivelestat (EI546) sodium is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.
|
-
- HY-117832
-
-
- HY-101146
-
-
- HY-W009156
-
-
- HY-108900
-
Leu-AMS
|
Aminoacyl-tRNA Synthetase
Bacterial
|
Cancer
Infection
|
Leu-AMS (compound 6), a leucine analogue, is a potent inhibitor of leucyl-tRNA synthetase (LRS) with an IC50 of 22.34 nM, which inhibits the catalytic activity of LRS but did not affect the leucine-induced mTORC1 activation. Leu-AMS shows cytotoxicity in cancer cells and normal cells, and inhibits the growth of bacteria.
|
-
- HY-P0118
-
Disitertide
P144
|
TGF-beta/Smad
PI3K
Apoptosis
|
Cancer
|
Disitertide (P144) is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) is also a PI3K inhibitor and an apoptosis inducer.
|
-
- HY-30008
-
Cycloleucine
|
iGluR
|
Cancer
Infection
Metabolic Disease
Neurological Disease
|
Cycloleucine is a specific inhibitor of S-adenosyl-methionine mediated methylation. Cycloleucine is antagonist of NMDA receptor associated glycine receptor, with a Ki of 600 μM. Cycloleucine is also a competitive inhibitor of ATP: L-methionine-S-adenosyl transferase in vitro. Cycloleucine has anxiolytic and cytostatic effects.
|
-
- HY-128855
-
Talsaclidine
|
mAChR
|
Neurological Disease
|
Talsaclidine is a muscarinic agonist with preferential neuron-stimulating properties. Talsaclidine is a full agonist at the M1 subtype, and as a partial agonist at the M2 and M3 subtypes.
|
-
- HY-B0424
-
-
- HY-N0150
-
Monensin sodium salt
Monensin A sodium salt
|
Bacterial
Sodium Channel
Antibiotic
|
Infection
Cancer
|
Monensin sodium salt is an antibiotic secreted by the bacteria Streptomyces cinnamonensis. Monensin sodium salt is an ionophore that mediates Na +/H + exchange. Monensin sodium salt causes a marked enlargement of the MVBs and regulates exosome secretion.
|
-
- HY-12512
-
cGAMP
Cyclic GMP-AMP; 3',3'-cGAMP
|
STING
|
Inflammation/Immunology
|
cGAMP (Cyclic GMP-AMP; 3',3'-cGAMP) is an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA; STING ligand.
|
-
- HY-B0462
-
-
- HY-109041
-
Razuprotafib
AKB-9778
|
Phosphatase
|
Inflammation/Immunology
|
Razuprotafib (AKB-9778) is a potent and selective inhibitor of the catalytic activity of VE-PTP (vascular endothelial protein tyrosine phosphatase) with an IC50of 17 pM. Razuprotafib promotes TIE2 activation, enhances ANG1-induced TIE2 activation, and stimulates phosphorylation of signaling molecules in the TIE2 pathway, including AKT, eNOS, and ERK. Razuprotafib inhibits the structurally related phosphatase PTP1B with an IC50 of 780 nM. Razuprotafib shows excellent selectivity for VE-PTP versus a variety of phosphatases, with the exception of HPTPη (IC50=36 pM) and HPTPγ (100 pM).
|
-
- HY-N6608
-
Physostigmine
Eserine
|
AChE
|
Neurological Disease
|
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning.
|
-
- HY-B1617AS
-
-
- HY-N0907
-
Ginsenoside Rg6
|
NF-κB
Apoptosis
|
Cancer
Inflammation/Immunology
|
Ginsenoside Rg6 is the component isolated from notoginseng. Ginsenoside Rg6 inhibits TNF-α-induced NF-κB transcriptional activity with an IC50 of 29.34±2.22 μM in HepG2 cells. Ginsenoside Rg6 also exhibits apoptosis-inducing effect.
|
-
- HY-114334
-
Glutaminase-IN-1
CB839 derivative
|
Glutaminase
|
Cancer
|
Glutaminase-IN-1 (CB839 derivative), a CB839 derivative, is an allosteric inhibitor of 1,3,4-selenadiazole-containing kidney-type glutaminase (KGA), with an IC50 of 1 nM. Glutaminase-IN-1 (CB839 derivative) shows improved cellular uptake and antitumor activity.
|
-
- HY-10446
-
Pralatrexate
|
Antifolate
Apoptosis
|
Cancer
|
Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment.
|
-
- HY-15416
-
-
- HY-N7699E
-
D-Heptamannuronic acid
|
Others
|
Neurological Disease
|
D-Heptamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Heptamannuronic acid can be used for the research of pain and vascular dementia.
|
-
- HY-N7699C
-
D-Pentamannuronic acid
|
Others
|
Neurological Disease
|
D-Pentamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Pentamannuronic acid can be used for the research of pain and vascular dementia.
|
-
- HY-N1451
-
-
- HY-15744
-
-
- HY-N7699F
-
D-Octamannuronic acid
|
Others
|
Neurological Disease
|
D-Octamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Octamannuronic acid can be used for the research of pain and vascular dementia.
|
-
- HY-N7699G
-
D-Nonamannuronic acid
|
Others
|
Neurological Disease
|
D-Nonamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Nonamannuronic acid can be used for the research of pain and vascular dementia.
|
-
- HY-N7699B
-
D-Tetramannuronic acid
|
Others
|
Neurological Disease
|
D-Tetramannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Tetramannuronic acid can be used for the research of pain and vascular dementia.
|
-
- HY-N7699D
-
D-Hexamannuronic acid
|
Others
|
Neurological Disease
|
D-Hexamannuronic acid, an alginate oligomer, is produced by marine brown algae and by a limited range of Gram negative bacteria. D-Hexamannuronic acid can be used for the research of pain and vascular dementia.
|
-
- HY-107416
-
RHC 80267
U-57908
|
Acyltransferase
mAChR
COX
Phospholipase
|
Metabolic Disease
Neurological Disease
|
RHC 80267 (U-57908) is a potent and selective inhibitor of diacylglycerol lipase (DAGL) (with IC50 of 4 μM in canine platelets). RHC-80267 inhibits cholinesterase activity with an IC50 of 4 μM, thereby enhancing the relaxation evoked by acetylcholine. RHC 80267 also inhibits COX and the hydrolysis of phosphatidylcholine (PC).
|
-
- HY-N4149
-
Quercetagetin
6-Hydroxyquercetin
|
Pim
|
Cancer
Inflammation/Immunology
|
Quercetagetin (6-Hydroxyquercetin) is the major flavonoid isolated from Citrus unshiu (C. unshiu) peel. Quercetagetin is a moderately potent and selective, cell-permeable pim-1 kinase inhibitor (IC50, 0.34 μM). Anti-inflammatory and anticancer properties.
|
-
- HY-14590
-
-
- 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-17443B
-
Sivelestat sodium tetrahydrate
EI546 sodium tetrahydrate; LY544349 sodium tetrahydrate; ONO5046 sodium tetrahydrate
|
Elastase
SARS-CoV
|
Cancer
|
Sivelestat (EI546) sodium tetrahydrate is a competitive inhibitor of human neutrophil elastase, with an IC50 of 44 nM and a Ki of 200 nM. Sivelestat (EI546) sodium tetrahydrate has the potential for the study of acute lung injury/acute respiratory distress syndrome or disseminated intravascular coagulation in COVID-19.
|
-
- HY-10529
-
-
- HY-122898
-
Ru360
|
Calcium Channel
Mitochondrial Metabolism
|
Cardiovascular Disease
|
Ru360, an oxygen-bridged dinuclear ruthenium amine complex, is a selective mitochondrial calcium uptake inhibitor. Ru360 potently inhibits Ca 2+ uptake into mitochondria with an IC50 of 0.184 nM. Ru360 binds to mitochondria with high affinity (Kd of 0.34 nM). Ru360 has antiarrhythmic and cardioprotective effects.
|
-
- HY-N2450
-
Sulforaphene
|
Apoptosis
EGFR
ERK
NF-κB
|
Cancer
|
Sulforaphene, isolated from radish seeds, exhibits an ED50 against velvetleaf seedlings approximately 2 x 10 -4 M. Sulforaphene promotes cancer cells apoptosis and inhibits migration via inhibiting EGFR, p-ERK1/2, NF‐κB and other signals.
|
-
- HY-P0118A
-
Disitertide TFA
P144 TFA
|
TGF-beta/Smad
PI3K
Apoptosis
|
Cancer
|
Disitertide (P144) TFA is a peptidic transforming growth factor-beta 1 (TGF-β1) inhibitor specifically designed to block the interaction with its receptor. Disitertide (P144) TFA is also a PI3K inhibitor and an apoptosis inducer.
|
-
- HY-16952A
-
Bepridil hydrochloride hydrate
(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
|
Calcium Channel
|
Cardiovascular Disease
|
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
|
-
- HY-N2071
-
Cedrol
(+)-Cedrol; α-Cedrol
|
Cytochrome P450
Fungal
|
Infection
Inflammation/Immunology
Cancer
|
Cedrol is a bioactive sesquiterpene, a potent competitive inhibitor of cytochrome P-450 (CYP) enzymes. Cedrol inhibits CYP2B6-mediated bupropion hydroxylase and CYP3A4-mediated midazolam hydroxylation with Ki of 0.9 μM and 3.4 μM, respectively. Cedrol also has weak inhibitory effect on CYP2C8, CYP2C9, and CYP2C19 enzymes. Cedrol is found in cedar essential oil and poetesses anti-septic, anti-inflammatory, anti-spasmodic, tonic, astringent, diuretic, sedative, insecticidal, and anti-fungal activities.
|
-
- HY-15724A
-
Vercirnon sodium
GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium
|
CCR
|
Inflammation/Immunology
Endocrinology
|
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-15724
-
Vercirnon
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-P3124
-
BIM-23190
|
Somatostatin Receptor
|
Cancer
|
BIM-23190, a somatostatin analog, exhibits Ki values of 0.34 nM and 11.1 nM for SSTR2 and SSTR5, respectively. BIM-23190 can be used in the study for cancer and acromegaly.
|
-
- HY-141274
-
-
- HY-14144
-
Aclidinium Bromide
LAS 34273; LAS-W 330
|
mAChR
|
Inflammation/Immunology
|
Aclidinium Bromide (LAS 34273; LAS-W 330) is a long-acting, inhaled muscarinic antagonist. Aclidinium Bromide has the potential for chronic obstructive pulmonary disease (COPD) research.
|
-
- HY-P3124A
-
-
- HY-101731
-
-
- HY-12151
-
NS 1738
NSC 213859
|
nAChR
|
Neurological Disease
|
NS 1738 (NSC 213859) is a novel positive allosteric modulator of the α7 nAChR, with respect to positive modulation of α7 nAChR (EC50=3.4 μM in oocyte experiments).
|
-
- HY-126145
-
-
- HY-B0372A
-
Bromhexine hydrochloride
|
SARS-CoV
Autophagy
HIV
|
Metabolic Disease
|
Bromhexine hydrochloride is a potent and specific TMPRSS2 protease inhibitor with an IC50 of 0.75 μM. Bromhexine hydrochloride can prevent and manage SARS-CoV-2 infection. Bromhexine hydrochloride is an autophagy agonist. Bromhexine hydrochloride is a mucolytic cough suppressant and has the potential for a range of respiratory conditions.
|
-
- HY-140347
-
APN-C3-NH-Boc
tert-Butyl 3-(4-(2-cyanoethynyl)phenylcarbamoyl)propylcarbamate
|
PROTAC Linker
|
Cancer
|
APN-C3-NH-Boc is an alkyl/ether-based PROTAC linker that can be used in the synthesis of PROTACs.
|
-
- HY-112729
-
HC-056456
3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide
|
Others
|
Others
|
HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na +]i rise is slowed by HC-056456 (IC50~3 µM).
|
-
- HY-W016622
-
Watermelon ketone
7-Methyl-2H-1,5-benzodioxepin-3(4H)-one
|
Others
|
Others
|
Watermelon ketone is fragrance chemical compound with special odorant which has been widely used in the fragrance industry, extracted from patent CN 103058984 A.
|
-
- HY-17461A
-
-
- HY-15238A
-
-
- HY-B1410
-
Ioversol
MP-328
|
Others
|
Others
|
Ioversol is a nonionic iodinated contrast medium (CM). Ioversol is used during a CT scan or x-ray in animal experiment. Ioversol does not damage the blood-brain barrier (BBB) in animal.
|
-
- HY-A0088
-
Cefotaxime sodium salt
Cefotaxim sodium salt; HR-756 sodium salt
|
Bacterial
Antibiotic
|
Infection
|
Cefotaxime sodium salt, a β-lactamase stable cephalosporin and a third-generation cephalosporin antibiotic, possesses broad-spectrum antibiotic activity against numerous Gram-positive and Gram-negative bacteria.
|
-
- HY-N0819
-
Raddeanin A
|
Apoptosis
|
Cancer
|
Raddeanin A is a natural triterpenoid saponin component of Anemone raddeana, with anti-cancer activities. Raddeanin A exerts anticancer effect on human osteosarcoma via the ROS/JNK and NF-κB signal pathway.
|
-
- HY-A0088A
-
-
- HY-14171S
-
Bexarotene D4
LGD1069 D4
|
RAR/RXR
Autophagy
|
Cancer
|
Bexarotene D4 is a deuterium labeled Bexarotene (LGD1069). Bexarotene (LGD1069) is a selective retinoid X receptors (RXR) agonist for the treatment of cutaneous T-cell lymphoma.
|
-
- 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-15340
-
LG100268
LG268
|
RAR/RXR
Autophagy
|
Metabolic Disease
|
LG100268 (LG268) is a potent, selective and orally active retinoid X receptor (RXR) agonist with EC50 values of 4 nM, 3 nM, and 4 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 displays >1000-fold selectivity for RXR over RAR, the Ki values are 3.4 nM, 6.2 nM and 9.2 nM for RXR-α, RXR-β, and RXR-γ, respectively. LG100268 activates RXR homodimers to induce transcriptional activation. LG100268 can be used for the study of lung carcinogenesisy.
|
-
- 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-B1866
-
Linuron
|
Androgen Receptor
|
Endocrinology
|
Linuron is a phenylurea herbicide that is widely used to control the growth of grass and weeds in various agriculture crops and in orchards. Linuron is a photosystem II inhibitor. Linuron is also a competitive androgen receptor (AR) antagonist with a Ki of 100 μM. Linuron shows reproductive toxicity in animals that acts as an endocrine disruptor.
|
-
- HY-10046
-
-
- HY-133887
-
-
- HY-126562
-
-
- HY-B0743A
-
Pipecuronium bromide
|
nAChR
|
Neurological Disease
|
Pipecuronium bromide is a potent long-acting nondepolarizing steroidal neuromuscular blocking agent (NMBA), and a bisquaternary ammonium compound. Pipecuronium bromide is a powerful competitive nAChR antagonist with a Kd of 3.06 μM.
|
-
- HY-17363S
-
Dimethyl fumarate D6
DMF D6
|
Keap1-Nrf2
|
Inflammation/Immunology
|
Dimethyl fumarate D6 is a deuterium labeled Dimethyl fumarate. Dimethyl fumarate is a nuclear factor (erythroid-derived)-like 2 (Nrf2) pathway activator and induces upregulation of antioxidant gene expression.
|
-
- HY-15666
-
GZD824
HQP1351
|
Bcr-Abl
|
Cancer
|
GZD824 (HQP1351) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 has antitumor activity.
|
-
- HY-13755
-
Sulforaphane
|
HDAC
Keap1-Nrf2
Apoptosis
|
Cancer
Inflammation/Immunology
|
Sulforaphane is an isothiocyanate present naturally in widely consumed vegetables. Sulforaphane increases tumor suppressor protein transcription and inhibits histone deacetylase activity. Sulforaphane activates Nrf2 and inhibits high glucose-induced progression of pancreatic cancer via AMPK dependent signaling. Sulforaphane has shown anti-cancer and anti-inflammatory activities.
|
-
- HY-119757
-
Tyrphostin AG1433
SU1433; AG1433
|
PDGFR
VEGFR
|
Cancer
|
Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation.
|
-
- HY-P1189
-
Echistatin
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
Echistatin, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-12481
-
SAR405
|
PI3K
Autophagy
|
Cancer
|
SAR405 is a first-in-class, selective, and ATP-competitive PI3K class III (PIK3C3) isoform Vps34 inhibitor (IC50=1.2 nM; Kd=1.5 nM). SAR405 inhibits autophagy induced either by starvation or by mTOR inhibition. Anticancer activity.
|
-
- HY-N0814
-
Phytic acid
Inositol hexaphosphate; myo-Inositol, hexakis(dihydrogen phosphate)
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
Phytic acid is a phosphorus storage compound of seeds and cereal grains. Phytic acid is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- 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-136265
-
BC-LI-0186
|
Aminoacyl-tRNA Synthetase
|
Cancer
|
BC-LI-0186 is a potent and selective inhibitor of Leucyl-tRNA synthetase (LRS; LeuRS) and Ras-related GTP-binding protein D (RagD) interaction (IC50=46.11 nM). BC-LI-0186 competitively binds to the RagD interacting site of LRS (Kd=42.1 nM) and has on effects on LRS-Vps34, LRS-EPRS, RagB-RagD association, mTORC1 complex formation or the activities of 12 kinases. BC-LI-0186 can effectively suppress the activity of cancer-associated MTOR mutants and the growth of rapamycin-resistant cancer cells. BC-LI-0186 is a promising agent for lung cancer research.
|
-
- HY-103354
-
Proglumide sodium
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
Proglumide sodium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide sodium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide sodium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide sodium also has antiepileptic and antioxidant activities.
|
-
- HY-B0986
-
Hexylresorcinol
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
|
Cancer
Infection
Metabolic Disease
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
|
-
- HY-101768
-
PRN1371
|
FGFR
c-Fms
|
Cancer
|
PRN1371 is a highly selective and potent FGFR1-4 and CSF1R inhibitor with IC50s of 0.6, 1.3, 4.1, 19.3 and 8.1 nM for FGFR1, FGFR2, FGFR3, FGFR4 and CSF1R, respectively.
|
-
- HY-B1322A
-
-
- HY-10014
-
R547
|
CDK
GSK-3
Apoptosis
|
Cancer
|
R547 is a potent, selective and oral orally bioavailable ATP-competitive CDK inhibitor, with Kis of 2 nM, 3 nM and 1 nM for CDK1/cyclin B, CDK2/cyclin E and CDK4/cyclin D1, respectively.
|
-
- HY-107856
-
5-Fluorouridine
|
Others
|
Cancer
|
5-Fluorouridine is a metabolite of 5-fluorouracil with anticancer activity. 5-fluorouridine inhibits rRNA synthesis of human colon carcinoma cells. 5-Fluorouridine exhibits cytotoxic effect on growth of L1210 cells with an IC50 of 2 nM.
|
-
- HY-B1266
-
Physostigmine salicylate
Eserine salicylate
|
AChE
|
Neurological Disease
|
Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate salicylatecan crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning.
|
-
- HY-N2320
-
Physostigmine hemisulfate
Eserine hemisulfate
|
AChE
|
Neurological Disease
|
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning.
|
-
- HY-N2435
-
[8]-Shogaol
|
COX
Apoptosis
|
Cancer
|
[8]-Shogaol, one of the pungent phenolic compounds in ginger, exhibits anti-platelet activity (IC50=5 μM) and inhibits COX-2 (IC50=17.5 μM). [8]-Shogaol induces apoptosis in human leukemia cells.
|
-
- HY-B1330
-
Proglumide
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
Proglumide is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide selective blocks CCK’s effects in the central nervous system (CNS). Proglumide has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide also has antiepileptic and antioxidant activities.
|
-
- HY-19373
-
-
- HY-N4308
-
Hexamethylquercetagetin
Hexa-O-methylquercetagetin; Quercetagetin hexamethyl ether; 3,5,6,7,3',4'-Hexamethoxyflavone
|
Others
|
Cancer
|
Hexamethylquercetagetin is a polymethoxylated flavone in peels of citrus cultivars.
|
-
- HY-N0527
-
Pentagalloylglucose
Penta-O-galloyl-β-D-glucose; 1,2,3,4,6-Pentagalloyl glucose
|
Influenza Virus
|
Infection
|
Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is a gallotannin isolated from various plants. It suppressed interleukin (IL)-4 induced signal pathway in B cell, and inhibited IgE production partially caused by increasing a population of Treg cells in conjunction with Treg-inducing factors. Pentagalloylglucose possesses significant anti-rabies virus (RABV) activity.
|
-
- HY-17002
-
Suplatast (Tosilate)
IPD 1151T
|
Interleukin Related
|
Inflammation/Immunology
|
Suplatast Tosilate (IPD 1151T) is an orally active Th2 cytokine inhibitor which can inhibit both IL-4 and IL-5 production from Th2 cells and suppress IgE synthesis. Suplatast Tosilate is an anti-allergic agent. Suplatast Tosilate has antiasthmatic, anti-inflammatory and antifibrotic activity.
|
-
- HY-17507
-
Pantoprazole
BY1023; SKF96022
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
Pantoprazole (BY10232) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-B0116
-
-
- HY-B0116A
-
-
- HY-N0814A
-
Phytic acid dodecasodium salt hydrate
Inositol hexaphosphate dodecasodium salt hydrate; myo-Inositol, hexakis(dihydrogen phosphate) dodecasodium salt hydrate
|
Xanthine Oxidase
Endogenous Metabolite
|
Inflammation/Immunology
Neurological Disease
|
Phytic acid dodecasodium salt hydrate is a phosphorus storage compound of seeds and cereal grains. Phytic acid dodecasodium salt hydrate is known as a food inhibitor, which has a strong ability to chelate multivalent metal ions, specially zinc, calcium, iron and as with protein residue. Phytic acid dodecasodium salt hydrate inhibits the enzymatic superoxide source xanthine oxidase (XO), and has antioxidative, neuroprotective, anti-inflammatory effects.
|
-
- HY-P1189A
-
Echistatin TFA
|
Integrin
|
Metabolic Disease
Inflammation/Immunology
|
Echistatin TFA, the smallest active RGD protein belonging to the family of disintegrins that are derived from snake venoms, is a potent inhibitor of platelet aggregation. Echistatin is a potent inhibitor of bone resorption in culture. Echistatin is a potent antagonist of αIIbβ3, αvβ3 and α5β1.
|
-
- HY-17507B
-
Pantoprazole sodium hydrate
BY1023 sodium hydrate; SKF96022 sodium hydrate
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
Pantoprazole sodium hydrate (BY10232 sodium hydrate) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium hydrate, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium hydrate improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium hydrate significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-17507A
-
Pantoprazole sodium
BY1023 sodium; SKF96022 sodium
|
Proton Pump
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
Pantoprazole sodium (BY10232 sodium) is an orally active and potent proton pump inhibitor (PPI). Pantoprazole sodium, a substituted benzimidazole, is a potent H +/K +-ATPase inhibitor with an IC50 of 6.8 μM. Pantoprazole sodium improves pH stability and has anti-secretory, anti-ulcer activities. Pantoprazole sodium significantly increased tumor growth delay combined with Doxorubicin (HY-15142).
|
-
- HY-15785
-
TAS-116
|
HSP
|
Cancer
|
TAS-116 is an oral bioavailable, ATP-competitive, highly specific HSP90α/HSP90β inhibitor (Kis of 34.7 nM and 21.3 nM, respectively) without inhibiting other HSP90 family proteins such as GRP94. TAS-116 demonstrates less ocular toxicity.
|
-
- HY-135731
-
4-Methylamino antipyrine
|
COX
Drug Metabolite
|
Inflammation/Immunology
|
4-Methylamino antipyrine is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine has analgesic, antipyretic, and relatively weak antiinflammatory properties.
|
-
- HY-17589
-
-
- HY-17589B
-
-
- HY-N5077
-
Sinapine
|
AChE
P-glycoprotein
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-B1836
-
Mildronate
Meldonium; MET-88; Quaterin
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
Mildronate (Meldonium) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.
|
-
- HY-135731A
-
4-Methylamino antipyrine hydrochloride
|
COX
Drug Metabolite
|
Inflammation/Immunology
|
4-Methylamino antipyrine hydrochloride is an active metabolite of Metamizole. Metamizole is a pyrazolone non-steroidal anti-inflammatory drug (NSAID) and inhibits COX. Metamizole is an nonopioid analgesic drug and can be used for pain and fever. 4-Methylamino antipyrine hydrochloride has analgesic, antipyretic, and relatively weak antiinflammatory properties.
|
-
- HY-12278
-
K02288
|
TGF-β Receptor
|
Others
|
K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
|
-
- HY-50904
-
Nintedanib
BIBF 1120
|
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib (BIBF 1120) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-17589A
-
-
- HY-N6779
-
Patulin
Terinin
|
Bacterial
Apoptosis
Autophagy
Antibiotic
|
Infection
|
Patulin (Terinin) is a mycotoxin produced by fungi including the Aspergillus, Penicillium, and Byssochlamys species, is suspected to be clastogenic, mutagenic, teratogenic and cytotoxic. Patulin induces autophagy-dependent apoptosis through lysosomal-mitochondrial axis, and causes DNA damage.
|
-
- HY-107457
-
AZD-8529
|
mGluR
|
Neurological Disease
|
AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
|
-
- HY-17461
-
-
- HY-B0968A
-
Trimetazidine
|
Autophagy
|
Cardiovascular Disease
|
Trimetazidine is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine triggers autophagy. Trimetazidine is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-15463
-
Imatinib
STI571; CGP-57148B
|
Bcr-Abl
PDGFR
c-Kit
SARS-CoV
Autophagy
|
Cancer
|
Imatinib (STI571) is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- HY-B0968
-
Trimetazidine dihydrochloride
|
Autophagy
|
Cardiovascular Disease
|
Trimetazidine dihydrochloride is a selective long chain 3-ketoyl coenzyme A thiolase inhibitor with an IC50 of 75 nM, which can inhibit β-oxidation of free fatty acid (FFA). Trimetazidine dihydrochloride is an effective antianginal agent and a cytoprotective drug, has anti-oxidant, anti-inflammatory, antinociceptive and gastroprotective properties. Trimetazidine dihydrochloride triggers autophagy. Trimetazidine dihydrochloride is also a 3-hydroxyacyl-CoA dehydrogenase (HADHA) inhibitor.
|
-
- HY-P1076
-
CALP2
|
Calcium Channel
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
CALP2 is a calmodulin (CaM) antagonist ( (Kd of 7.9 µM)) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 potently inhibits of adhesion and degranulation. CALP2 is also a strong activator of alveolar macrophages.
|
-
- HY-40136
-
cis-4-Hydroxy-L-proline
|
Endogenous Metabolite
|
Cancer
Metabolic Disease
|
cis-4-Hydroxy-L-proline, a proline analogue, is an inhibitor of collagen production. cis-4-Hydroxy-L-proline could inhibit fibroblast growth by preventing the deposition of triple-helical collagen on the cell layer. cis-4-Hydroxy-L-proline also depresses the growth of primary N-nitrosomethylurea-induced rat mammary tumors.
|
-
- HY-N6840
-
Xylotetraose
|
Others
|
Others
|
Xylotetraose is a hydrolysis product of Xylan. Xylan is a polysaccharide made from units of xylose and contains predominantly β-D-xylose units linked as in cellulose. Xylotetraose can be used for enzyme biochemical analysis.
|
-
- HY-15128
-
-
- HY-B1322
-
-
- HY-11106
-
Nintedanib esylate
BIBF 1120 esylate
|
PDGFR
VEGFR
FGFR
|
Cancer
|
Nintedanib esylate (BIBF 1120 esylate) is a potent triple angiokinase inhibitor for VEGFR1/2/3, FGFR1/2/3 and PDGFRα/β with IC50s of 34 nM/13 nM/13 nM, 69 nM/37 nM/108 nM and 59 nM/65 nM, respectively.
|
-
- HY-103354A
-
Proglumide hemicalcium
|
Cholecystokinin Receptor
|
Cancer
Endocrinology
Neurological Disease
|
Proglumide hemicalcium is a nonpeptide and orally active cholecystokinin (CCK)-A/B receptors antagonist. Proglumide hemicalcium selective blocks CCK’s effects in the central nervous system (CNS). Proglumide hemicalcium has ability to inhibit gastric secretion and to protect the gastroduodenal mucosa. Proglumide hemicalcium also has antiepileptic and antioxidant activities.
|
-
- HY-N5077B
-
Sinapine hydroxide
|
AChE
P-glycoprotein
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Sinapine hydroxide is an alkaloid isolated from seeds of the cruciferous species. Sinapine hydroxide exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine hydroxide is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-10987A
-
ENMD-2076
|
Aurora Kinase
FLT3
VEGFR
FGFR
PDGFR
Src
Apoptosis
|
Cancer
|
ENMD-2076 is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
|
-
- HY-B1322B
-
-
- HY-18641
-
Ki16198
|
LPL Receptor
|
Cancer
|
Ki16198 is a potent and orally active LPA receptor antagonist, the methyl ester of Ki16425 (HY-13285). Ki16198 inhibits LPA1 and LPA3-induced inositol phosphate production with Ki values of 0.34 μM and 0.93 μM, respectively. Ki16198 is effective for pancreatic cancer tumorigenesis and metastasis in vivo.
|
-
- HY-B1836A
-
Mildronate dihydrate
Meldonium dihydrate; MET-88 dihydrate; Quaterin dihydrate
|
Others
|
Metabolic Disease
Cardiovascular Disease
|
Mildronate dihydrate (Meldonium dihydrate) functions as a cardioprotective drug by cpmpetetively inhibiting BBOX1 and OCTN2. Mildronate (Meldonium) exhibits IC50 values of 34-62 μM for human recombinant BBOX and an EC50 of 21 μM for human OCTN2. Mildronate (Meldonium) treatment-induced redirection of long-chain FA metabolism from mitochondria to peroxisomes.
|
-
- HY-N0450
-
Sinapine thiocyanate
|
P-glycoprotein
AChE
|
Cancer
|
Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
|
-
- HY-15486
-
Salubrinal
|
Phosphatase
HSV
Autophagy
Apoptosis
|
Cancer
Infection
Inflammation/Immunology
|
Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation. Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis. Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5.
|
-
- HY-B1640
-
Ethacrynic acid
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Cancer
Inflammation/Immunology
|
Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
|
-
- HY-116767
-
BLT-1
Block lipid transport-1
|
HCV
|
Metabolic Disease
Inflammation/Immunology
|
BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor. BLT-1 has pro-inflammatory functions through neutrophil recruitment.
|
-
- HY-15666A
-
GZD824 dimesylate
HQP1351 dimesylate
|
Bcr-Abl
|
Cancer
|
GZD824 dimesylate (HQP1351 dimesylate) is a potent and orally active pan-Bcr-Abl inhibitor. GZD824 dimesylate potently inhibits a broad spectrum of Bcr-Abl mutants. GZD824 dimesylate strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. GZD824 dimesylate has antitumor activity.
|
-
- HY-79135
-
-
- HY-103642
-
D-myo-Inositol 1,4,5-trisphosphate hexapotassium salt
Inositol 1,4,5-trisphosphate hexapotassium salt; Ins(1,4,5)-P3 hexapotassium salt
|
Others
|
Metabolic Disease
|
D-myo-Inositol 1,4,5-trisphosphate hexapotassium salt is the hexapotassium salt of D-myo-Inositol 1,4,5-trisphosphate (1,4,5-IP3), which is a second messenger that stimulates the discharge of calcium from the endoplasmic reticulum.
|
-
- HY-107457A
-
AZD-8529 mesylate
|
mGluR
|
Neurological Disease
|
AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
|
-
- HY-12445
-
CDKI-73
LS-007
|
CDK
Apoptosis
|
Cancer
Inflammation/Immunology
|
CDKI-73 (LS-007) is an orally active and highly efficacious CDK9 inhibitor, with Ki values of 4 nM, 4 nM and 3 nM for CDK9, CDK1 and CDK2, respectively. CDKI-73 down-regulates the RNAPII phosphorylation. CDKI-73 is also a novel pharmacological inhibitor of Rab11 cargo delivery and innate immune secretion.
|
-
- HY-N6687
-
Calcimycin
A-23187; Antibiotic A-23187
|
Bacterial
Fungal
Apoptosis
Autophagy
Antibiotic
|
Cancer
Infection
|
Calcimycin (A-23187) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin induces apoptosis.
|
-
- HY-P1036
-
Compstatin
|
Complement System
|
Others
|
Compstatin, a 13-residue cyclic peptide, is a potent inhibitor of the complement system C3 with species specificity. Compstatin binds to baboon C3 and is resistant to proteolytic cleavage in baboon blood (similar to humans). Compstatin inhibits only the activation of primates’ complement system. Compstatin exhibits IC50 values of 63 μM and 12 μM for classical and alterative complement pathway, respectively.
|
-
- HY-B0537A
-
Pentamidine dihydrochloride
MP-601205 dihydrochloride
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Cancer
Infection
|
Pentamidine dihydrochloride (MP-601205 dihydrochloride) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine dihydrochloride inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine dihydrochloride is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine dihydrochloride has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-B0537
-
Pentamidine
MP-601205
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Cancer
Infection
|
Pentamidine (MP-601205) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-113365
-
Cholestenone
4-Cholesten-3-one
|
Endogenous Metabolite
|
Metabolic Disease
|
Cholestenone (4-Cholesten-3-one), the intermediate oxidation product of cholesterol, is metabolized primarily in the liver. Cholestenone is highly mobile in membranes and influences cholesterol flip-flop and efflux. Cholestenone may cause long-term functional defects in cells.
|
-
- HY-100530D
-
Rp-cAMPS sodium salt
|
PKA
|
Neurological Disease
|
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-15794
-
Nemorubicin
Methoxymorpholinyl doxorubicin; FCE 23762; PNU 152243
|
Others
|
Cancer
|
Nemorubicin (Methoxymorpholinyl doxorubicin) is a Doxorubicin derivative with potent antitumor activity. Nemorubicin is highly cytotoxic to a variety of tumor cell lines presenting a multidrug-resistant phenotype. Nemorubicin requirs an intact nucleotide excision repair (NER) system to exert its activity.
|
-
- HY-100530A
-
Rp-cAMPS
|
PKA
|
Neurological Disease
|
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-W001187
-
Tempo
|
DNA/RNA Synthesis
Reactive Oxygen Species
Mitochondrial Metabolism
|
Cancer
|
Tempo is a classic nitroxide radical and is a selective scavenger of mitochondrial ROS that dismutases superoxide in the catalytic cycle. Tempo induces DNA-strand breakage. Tempo can be used as an organocatalyst for the oxidation of primary alcohols to aldehydes. Tempo has mutagenic and antioxidant effects.
|
-
- 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-13948
-
Angiotensin II human
Angiotensin II; Ang II; DRVYIHPF
|
Angiotensin Receptor
Apoptosis
|
Cardiovascular Disease
Endocrinology
Cancer
|
Angiotensin II human (Angiotensin II) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human also induces apoptosis.
|
-
- HY-13948A
-
Angiotensin II human acetate
Angiotensin II acetate; Ang II acetate; DRVYIHPF acetate
|
Angiotensin Receptor
Apoptosis
|
Cancer
Endocrinology
Cardiovascular Disease
|
Angiotensin II human acetate (Angiotensin II acetate) is a vasoconstrictor that mainly acts on the AT1 receptor. Angiotensin II human acetate stimulates sympathetic nervous stimulation, increases aldosterone biosynthesis and renal actions. Angiotensin II human acetate induces growth of vascular smooth muscle cells, increases collagen type I and III synthesis in fibroblasts, leading to thickening of the vascular wall and myocardium, and fibrosis. Angiotensin II human acetate also induces apoptosis.
|
-
- HY-B0619
-
Zaltoprofen
CN100
|
COX
|
Inflammation/Immunology
|
Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain.
|
-
- HY-N0587
-
Demethylzeylasteral
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
Demethylzeylasteral is a triterpene compound isolated from Tripterygium wilfordii Hook F, with anti-inflammatory, immunosuppressive and anti-tumor activities. Demethylzeylasteral can significantly alleviates atherosclerosis (AS). Demethylzeylasteral inhibits triple-negative breast cancer invasion by blocking the canonical and non-canonical TGF-β signaling pathways.
|
-
- HY-10071
-
Y-27632
|
ROCK
Apoptosis
|
Cancer
|
Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 induces apoptosis. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
|
-
- HY-100360
-
MS049
|
Histone Methyltransferase
|
Cancer
|
MS049 is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 is not toxic and do not affect the growth of HEK293 cells.
|
-
- HY-W010342
-
6-Aminonicotinamide
|
Others
|
Cancer
|
6-Aminonicotinamide, a potent antimetabolite of nicotinamide, is competitive NADP +-dependent enzyme glucose-6-phosphate dehydrogenase (G6PD) inhibitor (Ki=0.46 μM). 6-Aminonicotinamide interferes with glycolysis, resulting in ATP depletion and synergizes with DNA-crosslinking chemotherapy drugs, such as Cisplatin, in killing cancer cells.
|
-
- HY-10583
-
Y-27632 dihydrochloride
|
ROCK
Apoptosis
|
Cancer
|
Y-27632 dihydrochloride is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 dihydrochloride induces apoptosis. Y-27632 dihydrochloride primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation.
|
-
- HY-10987
-
ENMD-2076 Tartrate
|
Aurora Kinase
FLT3
VEGFR
FGFR
Src
PDGFR
Apoptosis
|
Cancer
|
ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.
|
-
- HY-15652
-
Freselestat
ONO-6818; ONO-PO-736
|
Elastase
|
Inflammation/Immunology
|
Freselestat (ONO-6818) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat has a potent anti-inflammatory activity.
|
-
- HY-131275
-
Imatinib Impurity E
|
Others
|
Others
|
Imatinib Impurity E is the impurity of Imatinib. Imatinib is an orally bioavailable tyrosine kinases inhibitor that selectively inhibits BCR/ABL, v-Abl, PDGFR and c-kit kinase activity. Imatinib (STI571) works by binding close to the ATP binding site, locking it in a closed or self-inhibited conformation, therefore inhibiting the enzyme activity of the protein semicompetitively. Imatinib also is an inhibitor of SARS-CoV and MERS-CoV.
|
-
- 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-P1214
-
-
- HY-125098
-
Illudin S
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
Infection
|
Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cell cycle in human leukemia cells.
|
-
- HY-B0569
-
Hexamethonium Bromide
|
nAChR
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models.
|
-
- HY-79136
-
-
- HY-P1076A
-
CALP2 TFA
|
Calcium Channel
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
CALP2 TFA is a calmodulin (CaM) antagonist (Kd of 7.9 µM) with high affinity for binding to the CaM EF-hand/Ca 2+-binding site. CALP2 TFA inhibits CaM-dependent phosphodiesterase activity and increases intracellular Ca 2+ concentrations. CALP2 TFA potently inhibits of adhesion and degranulation. CALP2 TFA is also a strong activator of alveolar macrophages.
|
-
- HY-13821
-
Epoxomicin
BU-4061T
|
Proteasome
Apoptosis
|
Cancer
Inflammation/Immunology
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
|
-
- HY-106634
-
Mitoguazone
Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
|
HIV
Apoptosis
|
Cancer
Infection
|
Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.
|
-
- 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-108538
-
Ethacrynic acid D5
|
Gutathione S-transferase
NF-κB
Calcium Channel
|
Inflammation/Immunology
|
Ethacrynic acid D5 is a deuterium labeled Ethacrynic acid. Ethacrynic acid is a diuretic. Ethacrynic acid is an inhibitor of glutathione S-transferases (GSTs). Ethacrynic acid is a potent inhibitor of NF-kB-signaling pathway, and also modulates leukotriene formation. Ethacrynic acid also inhibits L-type voltage-dependent and store-operated calcium channel, leading to relaxation of airway smooth muscle (ASM) cells. Ethacrynic acid has anti-inflammatory properties that reduces the retinoid-induced ear edema in mice.
|
-
- HY-13814
-
PR-619
|
Deubiquitinase
Autophagy
Apoptosis
|
Cancer
|
PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.
|
-
- HY-15414S
-
-
- HY-128862
-
EGFR-IN-7
|
EGFR
|
Cancer
|
EGFR-IN-7 (compound 34) is a selective and potent EGFR kinase inhibitor extracted from patent WO2019015655A1, has IC50s of 7.92 nM and 0.218 nM for EGFR (WT) and EGFR (mutant C797S/T790M/L858R) respectively, and shows anti-tumor activity.
|
-
- HY-13716
-
Noscapine
(S,R)-Noscapine
|
Opioid Receptor
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier.
|
-
- HY-103238
-
RSVA405
|
AMPK
STAT
Autophagy
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
RSVA405 is a potent, orally active activator of AMPK, with an EC50 of 1 μM. RSVA405 facilitates CaMKKβ-dependent activation of AMPK, inhibits mTOR, and promotes autophagy to increase Aβ degradation. RSVA405 has anti-inflammatory effects through the inhibition of STAT3 function. RSVA405 also can be used for the research of obesity.
|
-
- HY-10510
-
-
- HY-17589AS
-
-
- HY-126047B
-
(R)-(+)-Anatabine
|
NF-κB
Amyloid-β
nAChR
|
Inflammation/Immunology
Neurological Disease
|
(R)-(+)-Anatabine is an less active R-enantiomer of Anatabine. Anatabine is a potent α4β2 nAChR agonist. Anatabine inhibits NF-κB activation lower amyloid-β (Aβ) production by preventing the β-cleavage of amyloid precursor protein (APP). Anatabine has anti-inflammatory effects and has the potential for neurodegenerative disorders treatment.
|
-
- HY-13716A
-
Noscapine hydrochloride
(S,R)-Noscapine hydrochloride
|
Opioid Receptor
Apoptosis
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Noscapine hydrochloride ((S,R)-Noscapine hydrochloride) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine hydrochloride exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine hydrochloride disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine hydrochloride possesses anticancer, neuroprotective, anti-inflammatory activities, and can crosse the blood-brain barrier.
|
-
- HY-10322
-
Falnidamol
BIBX 1382
|
EGFR
|
Cancer
|
Falnidamol (BIBX 1382) is an orally active, selective EGFR tyrosine kinase inhibitor with an IC50 of 3 nM. Falnidamol displays > 1000-fold lower potency against ErbB2 (IC50=3.4 μM) and a range of other related tyrosine kinases (IC50>10 μM). Falnidamol is a pyrimido-pyrimidine compound and has anti-cancer activity.
|
-
- HY-111415
-
EGFR-IN-5
|
EGFR
|
Cancer
|
EGFR-IN-5 is a EGFR inhibitor with IC50s of 10.4, 1.1, 34, 7.2 nM for EGFR, EGFR L858R, EGFR L858R/T790M, and EGFR L858R/T790M/C797S, respectively.
|
-
- HY-100530
-
Rp-cAMPS triethylammonium salt
|
PKA
|
Neurological Disease
|
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-13676
-
Megestrol acetate
|
Progesterone Receptor
Autophagy
HIV
|
Endocrinology
Cancer
|
Megestrol acetate is a synthetic and orally active progesteronal agent. Megestrol acetate is effective as an appetite stimulant for wasting syndromes such as cachexia. Megestrol acetate decreases nuclear and cytosol androgen receptors human BPH tissue. Megestrol acetate has the potential for HIV study and downregulates autophagic catabolic pathway.
|
-
- HY-135147
-
ONC206
|
Dopamine Receptor
|
Cancer
Neurological Disease
|
ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
|
-
- HY-B0537B
-
Pentamidine isethionate
MP-601205 isethionate
|
Parasite
Fungal
Phosphatase
Bacterial
Antibiotic
|
Infection
Cancer
|
Pentamidine isethionate (MP-601205 isethionate) is an antimicrobial agent and interferes with DNA biosynthetics. Pentamidine isethionate inhibits parasite Leishmania infantum with an IC50 of 2.5 μM. Pentamidine isethionate is a potent and selective protein tyrosine phosphatases (PTPases) and phosphatase of regenerating liver (PRL) inhibitor. Pentamidine isethionate has the potential for Gambian trypanosomiasis, antimony-resistant leishmaniasis, and Pneumocystis carinii pneumonia treatment. Antitumor and antibacterial activities.
|
-
- HY-100999
-
-
- HY-P1214A
-
-
- HY-W020182
-
α-Terpinene
Terpilene
|
Fungal
Parasite
|
Infection
|
α-Terpinene (Terpilene) is a monoterpene found in the essential oils of a large variety of foods and aromatic plants such as Mentha piperita. α-Terpinene is active against Trypanosoma evansi and has the potential for trypanosomosis treatment. α-Terpinene has antioxidant and antifungal properties.
|
-
- HY-128463
-
-
- HY-N0095
-
(S)-10-Hydroxycamptothecin
10-HCPT; 10-Hydroxycamptothecin
|
Topoisomerase
Apoptosis
|
Cancer
|
(S)-10-Hydroxycamptothecin (10-HCPT;10-Hydroxycamptothecin) is a DNA topoisomerase I inhibitor of isolated from the Chinese plant Camptotheca accuminata. (S)-10-Hydroxycamptothecin exhibits a remarkable apoptosis-inducing effect. (S)-10-Hydroxycamptothecin has the potential for hepatoma, gastric carcinoma, colon cancer and leukaemia treatment.
|
-
- HY-17387
-
(-)-Huperzine A
Huperzine A
|
AChE
Apoptosis
iGluR
|
Neurological Disease
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from a Chinese club moss, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease.
|
-
- HY-N1430
-
Oxyresveratrol
trans-Oxyresveratrol
|
Tyrosinase
HSV
Autophagy
|
Others
|
Oxyresveratrol (trans-Oxyresveratrol) is a potent naturally occurring antioxidant and free radical scavenger (IC50 of 28.9 µM against DPPH free radicals). Oxyresveratrol is potent and noncompetitive tyrosinase inhibitor with an IC50 value of 1.2 µM for mushroom tyrosinase. Oxyresveratrol is effective against HSV-1, HSV-2 and varicella-zoster virus, and has neuroprotective effects.
|
-
- HY-17386
-
-
- HY-15652A
-
Freselestat quarterhydrate
ONO-6818 quarterhydrate; ONO-PO-736 quarterhydrate
|
Elastase
|
Inflammation/Immunology
|
Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally active neutrophil elastase inhibitor with a Ki of 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreatic elastase, plasmin, thrombin, collagenase, cathepsin G, and murine macrophage elastase. Freselestat quarterhydrate has a potent anti-inflammatory activity.
|
-
- HY-13317S
-
Oseltamivir D3
|
Influenza Virus
|
Infection
|
Oseltamivir D3 is a deuterium labeled Oseltamivir. Oseltamivir is an influenza virus neuraminidase inhibitor (NAI). Oseltamivir inhibits influenza A/H3N2, A/H1N2, A/H1N1, and B viruses with mean IC50s of 0.67, 0.9, 1.34 and 13 nM, respectively. Anti-influenza A and B agent.
|
-
- HY-10514
-
BX795
|
PDK-1
IKK
Autophagy
|
Cancer
|
BX795 is a potent and selective inhibitor of PDK1, with an IC50 of 6 nM. BX795 is also a potent and relatively specific inhibitor of TBK1 and IKKɛ, with an IC50 of 6 and 41 nM, respectively. BX795 blocks phosphorylation of S6K1, Akt, PKCδ, and GSK3β, and has lower selectivity over PKA, PKC, c-Kit, GSK3β etc. BX795 modulates autophagy.
|
-
- HY-N0498
-
Nitidine chloride
|
Parasite
Apoptosis
STAT
Topoisomerase
ERK
FAK
p38 MAPK
NF-κB
|
Cancer
Inflammation/Immunology
|
Nitidine chloride, a potential anti-malarial lead compound derived from Zanthoxylum nitidum (Roxb) DC, exerts potent anticancer activity through diverse pathways, including inducing apoptosis, inhibiting STAT3 signaling cascade, DNA topoisomerase 1 and 2A, ERK and c-Src/FAK associated signaling pathway. Nitidine chloride inhibits LPS-induced inflammatory cytokines production via MAPK and NF-kB pathway.
|
-
- HY-108485
-
Damnacanthal
|
Src
Apoptosis
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.
|
-
- HY-N6687B
-
Calcimycin hemimagnesium
A-23187 hemimagnesium; Antibiotic A-23187 hemimagnesium
|
Bacterial
Fungal
Apoptosis
Autophagy
|
Cancer
Infection
|
Calcimycin (A-23187) hemimagnesium is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemimagnesium induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemimagnesium inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemimagnesium also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemimagnesium induces apoptosis.
|
-
- HY-N6687A
-
Calcimycin hemicalcium salt
A-23187 hemicalcium salt; Antibiotic A-23187 hemicalcium salt
|
Bacterial
Fungal
Apoptosis
Autophagy
Antibiotic
|
Cancer
Infection
|
Calcimycin hemicalcium salt (A-23187 hemicalcium salt) is an antibiotic and a unique divalent cation ionophore (like calcium and magnesium). Calcimycin hemicalcium salt induces Ca 2+-dependent cell death by increasing intracellular calcium concentration. Calcimycin hemicalcium salt inhibits the growth of Gram-positive bacteria and some fungi. Calcimycin hemicalcium salt also inhibits the activity of ATPase and uncouples oxidative phosphorylation (OXPHOS) of mammalian cells. Calcimycin hemicalcium salt induces apoptosis.
|
-
- HY-113038
-
D-α-Hydroxyglutaric acid
(R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Cancer
Inflammation/Immunology
Neurological Disease
|
D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling.
|
-
- HY-P1932
-
-
- HY-90003A
-
Tianeptine sodium salt
|
5-HT Receptor
|
Neurological Disease
|
Tianeptine sodium salt is a selective facilitator of 5-HT uptake. Tianeptine sodium salt has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine sodium salt has antidepressant, anxiolytic, analgesic and neuroprotective activities.
|
-
- HY-90003
-
Tianeptine
|
5-HT Receptor
|
Neurological Disease
|
Tianeptine is a selective facilitator of 5-HT uptake. Tianeptine has no affinity for a wide range of receptors, including 5-HT and dopamine (IC50>10 μM) and has no effect on noradrenalin or dopamine uptake. Tianeptine has antidepressant, anxiolytic, analgesic and neuroprotective activities.
|
-
- HY-76772
-
Cevimeline hydrochloride hemihydrate
SNI-2011; AF102B hydrochloride hemihydrate
|
mAChR
|
Neurological Disease
|
Cevimeline hydrochloride hemihydrate (SNI-2011) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride hemihydrate stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride hemihydrate can cross the blood-brain barrier (BBB).
|
-
- HY-70020B
-
Cevimeline hydrochloride
AF102B hydrochloride
|
mAChR
|
Neurological Disease
|
Cevimeline hydrochloride (AF102B hydrochloride) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline hydrochloride stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline hydrochloride can cross the blood-brain barrier (BBB).
|
-
- 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-N7665
-
Prosaikogenin G
|
Others
|
Metabolic Disease
|
Prosaikogenin G, isolated from the roots of Buleurum bicaule Helm (Apiaceae), exhibits significant inhibitory effects on rat mesangial cell proliferation induced by Ang II. Prosaikogenin G has protective action on the kidney. Prosaikogenin G is a derivative of Saikosaponin d in the gastrointestinal tract.
|
-
- HY-W010983
-
-
- HY-100867A
-
TAK-659 hydrochloride
|
Syk
FLT3
|
Cancer
|
TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).
|
-
- HY-113498
-
Sphingomyelin
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
Sphingomyelin is a eukaryotic sphingolipid and one of the major constituents of cell membranes and particularly abundant in the myelin sheath that surrounds neuronal axons. Sphingomyelin plays an important role in cell processes, the regulation of inflammatory responses, and signal transduction. Sphingomyelin metabolism is associated with various central nervous system diseases and Niemann–Pick disease.
|
-
- HY-13511A
-
Rupatadine Fumarate
UR-12592 Fumarate
|
Histamine Receptor
Autophagy
|
Inflammation/Immunology
|
Rupatadine (UR-12592) Fumarate is a potent, orally active, long-lasting and dual PAF/H1 antagonist with Ki values of 0.55/0.1 μM(rabbit platelet membranes/guinea pig cerebellum membranes). Rupatadine (UR-12592) Fumarate maintains autophagic flux in fibrotic lung tissue.
|
-
- HY-P1932A
-
-
- HY-14539S
-
Clozapine D8
HF 1854 D8
|
Dopamine Receptor
mAChR
|
Neurological Disease
|
Clozapine D8 (HF 1854 D8) is the deuterium labeled Clozapine. Clozapine, an antipsychotic, is a potent antagonist of dopamine and a number of other receptors, with a Ki of 9.5 nM for muscarinic M1 receptor. Clozapine is also a potent and selective agonist at the muscarinic M4 receptor (EC50=11 nM).
|
-
- HY-70020
-
Cevimeline
AF102B
|
mAChR
|
Neurological Disease
|
Cevimeline (AF-102B) is a quinuclidine derivative of acetylcholine and a selective and orally active muscarinic M1 and M3 receptor agonist. Cevimeline stimulates secretion by the salivary glands and can be used as a sialogogue for xerostomia. Cevimeline can cross the blood-brain barrier (BBB).
|
-
- 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-118480
-
4-MMPB
|
Lipoxygenase
Apoptosis
|
Cancer
|
4-MMPB is a selective inhibitor of 15-lipoxygenase, with an IC50 of 18 μM. 4-MMPB has IC50s of 19.5 μM and 19.1 μM for soybean 15-lipoxygenase (SLO) and human 15-lipoxygenase-1 (15-LOX-1), respectively. 4-MMPB has potential for the research of prostate cancer.
|
-
- HY-12972
-
Mavelertinib
PF-06747775
|
EGFR
|
Cancer
|
Mavelertinib is a selective, orally available and irreversible EGFR tyrosine kinase inhibitor (EGFR TKI), with IC50s of 5, 4, 12 and 3 nM for Del, L858R, and double mutants T790M/L858R and T790M/Del, respectively. Mavelertinib can be used for the research of non-small-cell lung cancer (NSCLC).
|
-
- HY-N7647
-
Methyl brevifolincarboxylate
Brevifolincarboxylic acid methyl ester
|
Influenza Virus
|
Infection
|
Methyl brevifolincarboxylate (Brevifolincarboxylic acid methyl ester) is a potent influenza virus PB2 cap-binding inhibitor. Methyl brevifolincarboxylate exhibits inhibitory activity against influenza virus A/Puerto Rico/8/34 (H1N1) and A/Aichi/2/68 (H3N2) with IC50s of 27.16 μM and 33.41 μM. Anti-oxidant activity.
|
-
- HY-10115
-
PI-103
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
PI-103 is a potent PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 also inhibits DNA-PK with an IC50 of 2 nM. PI-103 induces autophagy.
|
-
- HY-12170
-
Prinomastat
AG3340; KB-R9896
|
MMP
Apoptosis
|
Cancer
|
Prinomastat (AG3340) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat crosses blood-brain barrier. Antitumor avtivity.
|
-
- HY-12170A
-
Prinomastat hydrochloride
AG3340 hydrochloride; KB-R9896 hydrochloride
|
MMP
Apoptosis
|
Cancer
|
Prinomastat hydrochloride (AG3340 hydrochloride) is a broad spectrum, potent, orally active metalloproteinase (MMP) inhibitor with IC50s of 79, 6.3 and 5.0 nM for MMP-1, MMP-3 and MMP-9, respectively. Prinomastat hydrochloride inhibits MMP-2, MMP-3 and MMP-9 with Kis of 0.05 nM, 0.3 nM and 0.26 nM, respectively. Prinomastat hydrochloride can cross blood-brain barrier. Antitumor avtivity.
|
-
- HY-107024
-
Osteogenic Growth Peptide (10-14)
OGP(10-14); Historphin
|
Src
|
Others
|
Osteogenic Growth Peptide (10-14) (OGP(10-14)), the C-terminal truncated pentapeptide of osteogenic growth peptide (OGP), retains the full OGP-like activity. Osteogenic Growth Peptide (10-14) is responsible for the binding to the OGP receptor and activates an intracellular Gi-protein-MAP kinase signaling pathway. Osteogenic Growth Peptide (10-14) is a potent mitogen and stimulator of osteogenesis and hematopoiesis. Osteogenic Growth Peptide (10-14) acts as a Src inhibitor.
|
-
- HY-10115A
-
PI-103 Hydrochloride
|
PI3K
mTOR
DNA-PK
Autophagy
Apoptosis
|
Cancer
|
PI-103 Hydrochloride is a dual PI3K and mTOR inhibitor with IC50s of 8 nM, 88 nM, 48 nM, 150 nM, 20 nM, and 83 nM for p110α, p110β, p110δ, p110γ, mTORC1, and mTORC2. PI-103 Hydrochloride also inhibits DNA-PK with an IC50 of 2 nM. PI-103 Hydrochloride induces autophagy.
|
-
- HY-113952
-
Actinonin
(-)-Actinonin
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Cancer
Infection
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities.
|
-
- 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-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-102022
-
α-Galactosylceramide
α-GalCer; KRN7000
|
Others
|
Cancer
Inflammation/Immunology
|
α-Galactosylceramide (α-GalCer) is a synthetic glycolipid with antitumorial and immunostimulatory. α-Galactosylceramide is a very potent NKT cell agonist and binds effectively to CD1d. The complex of α-Galactosylceramide plus CD1d binds the NKT cell TCR (T cell antigen receptor).
|
-
- HY-136429
-
Ethylhydrocupreine
Optochin
|
Bacterial
Parasite
|
Infection
|
Ethylhydrocupreine (Optochin) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
|
-
- HY-136429A
-
Ethylhydrocupreine hydrochloride
Optochin hydrochloride
|
Bacterial
Parasite
|
Infection
|
Ethylhydrocupreine hydrochloride (Optochin hydrochloride) is a quinine derivate with antimicrobial activity against S. pneumoniae. Ethylhydrocupreine hydrochloride also possesses antimalarial activity against Plasmodium falciparum, with an IC50 of 25.75 nM. Ethylhydrocupreine hydrochloride is a Gallus gallus taste 2 receptors (ggTas2r1, ggTas2r2 and ggTas2r7) agonist.
|
-
- HY-12283
-
Rostafuroxin
PST 2238
|
Na+/K+ ATPase
RSV
|
Cardiovascular Disease
|
Rostafuroxin (PST 2238), a digitoxigenin derivative, is an orally active and potent Na +,K +-ATPase (ATP1A1) antognist. Rostafuroxin binds specifically to the ATP1A1 extracellular domain and blocks respiratory syncytial virus (RSV)-triggered EGFR Tyr845 phosphorylation. Rostafuroxin has antihypertensive and anti-RSV activity.
|
-
- HY-108768
-
Pasireotide pamoate
SOM230 pamoate
|
Somatostatin Receptor
|
Cancer
|
Pasireotide pamoate (SOM230 pamoate) is a stable cyclohexapeptide somatostatin mimic that improves agonist activity at somatostatin receptors (subtypes sst1/2/3/4/5, pKi=8.2/9.0/9.1/<7.0/9.9 respectively). Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.
|
-
- HY-124662
-
IHVR-19029
|
Glucosidase
|
Infection
|
IHVR-19029 is a potent endoplasmic reticulum (ER) α-glucosidases I and II inhibitor, with an IC50 of 0.48 μM for ER a-glucosidase I. IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Dengue virus (DENV), Ebola virus (EBOV) and Rift Valley fever virus. The combination of IHVR-19029 with Favipiravir (HY-14768) improves the antiviral efficacy.
|
-
- HY-101180
-
C2 Ceramide
Ceramide 2
|
Phosphatase
Mitochondrial Metabolism
Apoptosis
|
Endocrinology
Metabolic Disease
|
C2 Ceramide (Ceramide 2) is the main lipid of the stratum corneum and a protein phosphatase 1 (PP1) activator. C2 Ceramide activates PP2A and ceramide-activated protein phosphatase (CAPP). C2 Ceramide induces cells differentiation and apoptosis, inhibits mitochondrial respiratory chain complex III. C2 Ceramide is also a skin conditioning agent that protects the epidermal barrier from water loss.
|
-
- 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-B0268A
-
Enoxacin hydrate
Enoxacin sesquihydrate; AT-2266 hydrate; CI-919 hydrate
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Infection
Cancer
|
Enoxacin hydrate (Enoxacin sesquihydrate), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin hydrate is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin hydrate has potent activities against gram-positive and -negative bacteria. Enoxacin hydrate is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
|
-
- HY-B0268
-
Enoxacin
AT 2266; CI 919
|
Bacterial
DNA/RNA Synthesis
MicroRNA
Antibiotic
|
Cancer
Infection
|
Enoxacin (AT 2266), a fluoroquinolone, interferes with DNA replication and inhibits bacterial DNA gyrase (IC50=126 µg/ml) and topoisomerase IV (IC50=26.5 µg/ml). Enoxacin is a miRNA processing activator and enhances siRNA-mediated mRNA degradation and promotes the biogenesis of endogenous miRNAs. Enoxacin has potent activities against gram-positive and -negative bacteria. Enoxacin is a cancer-specific growth inhibitor that acts by enhancing TAR RNA-binding protein 2 (TRBP)-mediated microRNA processing.
|
-
- HY-W011109
-
CKI-7
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
CKI-7 is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 is a selective Cdc7 kinase inhibitor. CKI-7 also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 has a much weaker effect on casein kinase II and other protein kinases.
|
-
- HY-11009
-
CGP60474
|
CDK
PKC
|
Cancer
|
CGP60474, a highly potent anti-endotoxemic agent, is a potent cyclin-dependent kinase (CDK) inhibitor (IC50 values are 26, 3, 4, 216, 10, 200 and 13 nM for CDK1/B, CDK2/E, CDK2/A, CDK4/D, CDK5/p25, CDK7/H and CDK9/T, respectively). CGP60474 is a selective and ATP-competitive PKC inhibitor.
|
-
- HY-100542
-
-
- HY-12554
-
Terlipressin
|
Vasopressin Receptor
|
Endocrinology
Inflammation/Immunology
Cardiovascular Disease
|
Terlipressin is a vasopressin analogue with potent vasoactive properties. Terlipressin is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin exerts anti-inflammatory and anti-oxidative effects. Terlipressin has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
|
-
- HY-101299A
-
Dihydrexidine
DAR-0100
|
Dopamine Receptor
|
Neurological Disease
|
Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity. Dihydrexidine can stimulate YAP phosphorylation.
|
-
- HY-12554A
-
Terlipressin acetate
|
Vasopressin Receptor
|
Endocrinology
Inflammation/Immunology
Cardiovascular Disease
|
Terlipressin acetate is a vasopressin analogue with potent vasoactive properties. Terlipressin acetate is a highly selective vasopressin V1 receptor agonist that reduces the splanchnic blood flow and portal pressure and controls acute variceal bleeding. Terlipressin acetate exerts anti-inflammatory and anti-oxidative effects. Terlipressin acetate has the potential for hepatorenal syndrome and norepinephrine-resistant septic shock research.
|
-
- HY-13591
-
Piclidenoson
IB-MECA; CF-101
|
Adenosine Receptor
Apoptosis
|
Cancer
|
Piclidenoson (IB-MECA;CF-101) is a first-in-class, orally bioavailable and selective A3 adenosine receptor (A3AR) agonist. Piclidenoson exhibits antiproliferative effect and induces apoptosis in different cancer cell types like melanoma, leukemia. Piclidenoson can be used for the research of autoimmune inflammatory diseases and COVID-19.
|
-
- HY-135416
-
Streptolysin O
|
Endogenous Metabolite
|
Infection
|
Streptolysin O, a group A streptococcal toxin, is a well-characterized oxygen-labile prototype of a cholesterol-binding bacterial exotoxin. Streptolysin O causes both lysis of cells and cardiotoxicity. Streptolysin O is widely used for the controlled permeabilization of cell membranes. Streptolysin O exists in two forms, a reduced active state and an oxidized reversibly inactive state.
|
-
- HY-101299B
-
Dihydrexidine hydrochloride
DAR-0100 hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity. Dihydrexidine hydrochloride can stimulate YAP phosphorylation.
|
-
- HY-113914
-
9-ING-41
|
GSK-3
Apoptosis
Autophagy
|
Cancer
|
9-ING-41 is a maleimide-based ATP-competitive and selective glycogen synthase kinase-3β (GSK-3β) inhibitor with an IC50 of 0.71 μM. 9-ING-41 significantly leads to cell cycle arrest, autophagy and apoptosis in cancer cells. 9-ING-41 has anticancer activity and has the potential for enhancing the antitumor effects of chemotherapeutic drugs.
|
-
- HY-108635
-
-
- HY-19357
-
E3330
APX-3330
|
DNA/RNA Synthesis
|
Cancer
|
E3330 (APX-3330) is a direct, orally active and selective AP endonuclease 1 (APE1; REF-1) inhibitor, which suppresses NF-κB DNA-binding activity. E3330 (APX-3330) blocks TNF-α-induced activation of IL-8 production in liver cancer cell lines. E3330 (APX-3330) shows anticancer properties, such as inhibition of cancer cell growth and migration.
|
-
- HY-13285
-
Ki16425
Debio 0719
|
LPL Receptor
|
Neurological Disease
Cancer
|
Ki16425 (Debio 0719) is a subtype-selective, competitive antagonist of the EDG-family receptors, LPA1 and LPA3 with Kis of 0.34 μM and 0.93 μM, respectively. Ki16425 (Debio 0719) reduces the LPA-induced activation of p42/p44 MAPK. Ki16425 also can inhibits LPA-induced dephosphorylation of Yes-associated protein (YAP)/TAZ in HEK293A cells.
|
-
- HY-19618
-
BRD3308
|
HDAC
HIV
Apoptosis
|
Infection
Metabolic Disease
|
BRD3308 is a highly selective HDAC3 inhibitor with an IC50 of 54 nM. BRD3308 is 23-fold selectivity for HDAC3 over HDAC1 (IC50 of 1.26 μM) or HDAC2 (IC50 of 1.34 μM). BRD3308 suppresses pancreatic β-cell apoptosis induced by inflammatory cytokines or glucolipotoxic stress, and increases functional insulin release. BRD3308 activates HIV-1 transcription and disrupts HIV-1 latency.
|
-
- HY-100972
-
ARV-771
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
ARV-771 is a potent BET degrader based on PROTAC technology with Kds of 34 nM, 4.7 nM, 8.3 nM, 7.6 nM, 9.6 nM, and 7.6 nM for BRD2(1), BRD2(2), BRD3(1), BRD3(2), BRD4(1), and BRD4(2), respectively.
|
-
- 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-34758
-
N-Nitroso-N-methylurea
NMU; MNU; NMH
|
DNA Alkylator/Crosslinker
|
Cancer
|
N-Nitroso-N-methylurea (NMU;MNU;NMH) is a potent carcinogen, mutagen and teratogenand. N-Nitroso-N-methylurea is a direct-acting alkylating agent that interacts with DNA. N-Nitroso-N-methylurea targets multiple animal organs to cause various cancer and/or degenerative disease. N-Nitroso-N-methylurea is also a precursor in the synthesis of diazomethane.
|
-
- HY-128067
-
5-(N,N-Hexamethylene)-amiloride
Hexamethylene amiloride; HMA
|
Sodium Channel
HIV
Apoptosis
|
Cancer
Infection
|
5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) derives from an amiloride and is a potent Na +/H + exchanger inhibitor, which decreases the intracellular pH (pHi) and induces apoptosis in leukemic cells. 5-(N,N-Hexamethylene)-amiloride (Hexamethylene amiloride) is also an inhibitor of the HIV-1 Vpu virus ion channel and inhibits mouse hepatitis virus (MHV) replication and human coronavirus 229E (HCoV229E) replication in cultured L929 cells with EC50s of 3.91 μM and 1.34 μM, respectively.
|
-
- HY-123823
-
Nitroaspirin
NCX 4016
|
COX
Apoptosis
|
Cancer
|
Nitroaspirin (NCX 4016) is a nitric oxide (NO) donor and a nitro-derivative of Aspirin, which combines with Nitroaspirin to inhibit cyclooxygenase. Nitroaspirin (NCX 4016) has antithrombotic and anti-platelet properties and acts as a direct and irreversible inhibitor of COX-1. Nitroaspirin (NCX 4016) causes significant induction of cell cycle arrest and apoptosis in Cisplatin-resistant human ovarian cancer cells via down-regulation of EGFR/PI3K/STAT3 signaling and modulation of Bcl-2 family proteins.
|
-
- HY-16561
-
Resveratrol
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model.
|
-
- HY-15583
-
-
- HY-13453
-
BAY 11-7082
BAY 11-7821
|
IKK
Deubiquitinase
Autophagy
Apoptosis
|
Cancer
Inflammation/Immunology
|
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
|
-
- HY-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-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-15477A
-
YS-49 monohydrate
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
YS-49 (monohydrate) is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-15477
-
YS-49
|
Akt
PI3K
Angiotensin Receptor
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
YS-49 is a PI3K/Akt (a downstream target of RhoA) activator, to reduce RhoA/PTEN activation in the 3-methylcholanthrene-treated cells. YS-49 inhibits angiotensin II (Ang II)-stimulated proliferation of VSMCs via induction of heme oxygenase (HO)-1. YS-49 is also an isoquinoline compound alkaloid, has a strong positive inotropic action through activation of cardiac β-adrenoceptors.
|
-
- HY-100574A
-
Cl-amidine hydrochloride
|
Protein Arginine Deiminase
Apoptosis
MicroRNA
|
Cancer
Inflammation/Immunology
|
Cl-amidine hydrochloride is an orally active peptidylarginine deminase (PAD) inhibitor, with IC50 values of 0.8 μM, 6.2 μM and 5.9 μM for PAD1, PAD3, and PAD4, respectively. Cl-amidine hydrochloride induces apoptosis in cancer cells. Cl-amidine hydrochloride induces microRNA (miR)-16 expression and causes cell cycle arrest. Cl-Amidine hydrochloride prevents histone 3 citrullination and neutrophil extracellular trap formation, and improves survival in a murine sepsis model.
|
-
- HY-103444
-
ARP-100
|
MMP
|
Cancer
|
ARP-100 is a potent and selective matrix metalloproteinase MMP-2 inhibitor (IC50=12 nM). ARP-100 interacts with S1' pocket of MMP-2 and shows anti-invasive properties in an in vitro model of invasion on matrigel. ARP-100 shows the less inhibitory activity towards MMP-1 (>50 μM), MMP-3 (4.5 μM), MMP-7 (>50 μM), and MMP-9 (0.2 μM).
|
-
- HY-32329A
-
Setiptiline maleate
MO-8282
|
5-HT Receptor
|
Neurological Disease
|
Setiptiline (MO-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
|
-
- HY-133028
-
CKI-7 free base
|
Casein Kinase
CDK
SGK
Ribosomal S6 Kinase (RSK)
|
Cancer
|
CKI-7 free base is a potent and ATP-competitive casein kinase 1 (CK1) inhibitor with an IC50 of 6 μM and a Ki of 8.5 μM. CKI-7 free base is a selective Cdc7 kinase inhibitor. CKI-7 free base also inhibits SGK, ribosomal S6 kinase-1 (S6K1) and mitogen- and stress-activated protein kinase-1 (MSK1). CKI-7 free base has a much weaker effect on casein kinase II and other protein kinases.
|
-
- HY-15504A
-
RGB-286638 free base
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-15504
-
RGB-286638
|
CDK
GSK-3
MEK
JAK
|
Cancer
|
RGB-286638 is a CDK inhibitor that inhibits the kinase activity of cyclin T1-CDK9, cyclin B1-CDK1, cyclin E-CDK2, cyclin D1-CDK4, cyclin E-CDK3, and p35-CDK5 with IC50s of 1, 2, 3, 4, 5 and 5 nM, respectively; also inhibits GSK-3β, TAK1, Jak2 and MEK1, with IC50s of 3, 5, 50, and 54 nM.
|
-
- HY-131296
-
5-A-RU-PABC-Val-Cit-Fmoc
|
Others
|
Inflammation/Immunology
|
5-A-RU-PABC-Val-Cit-Fmoc is the prodrug of 5-A-RU. 5-A-RU, a precursor of bacterial Riboflavin, is a mucosal-associated invariant T (MAIT) cells activator. 5-A-RU forms potent MAIT-activating antigens via non-enzymatic reactions with small molecules, such as glyoxal and methylglyoxal, which are derived from other metabolic pathways.
|
-
- HY-N0155
-
Nobiletin
|
ROR
Reactive Oxygen Species
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
Neurological Disease
|
Nobiletin is a poly-methoxylated flavone from the citrus peel that improves memory loss. Nobiletin is a retinoid acid receptor-related orphan receptors (RORs) agonist. Nobiletin can reduce reactive oxygen species (ROS) levels in differentiated C2C12 myotubes and has anti-inflammation and anti-cancer properties, including anti-angiogenesis, anti-proliferation, anti-metastasis and induced apoptosis.
|
-
- HY-108676
-
NF023 hexasodium
|
P2X Receptor
|
Neurological Disease
|
NF023 hexasodium is a selective and competitive P2X1 receptor antagonist, with IC50 values of 0.21 μM, 28.9 μM, > 50 μM and > 100 μM for human P2X1, P2X3, P2X2, and P2X4-mediated responses respectively.
|
-
- HY-W011500
-
TCEP hydrochloride
Tris(2-carboxyethyl)phosphine hydrochloride
|
Others
|
Others
|
TCEP hydrochloride (Tris(2-carboxyethyl)phosphine hydrochloride) is a non-thiol reducing agent that is more stable and produces a faster S-S reductive reaction than other chemical reductants. TCEP hydrochloride is a trialkylphosphine, selectively reduces protein disuldes without altering the properties or interacting with thiol-directed agents in the reaction mixture. TCEP hydrochloride is also a commonly used reducing agent in the DNA/AuNP chemistry.
|
-
- HY-14994
-
SCH79797 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
SCH79797 dihydrochloride is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 dihydrochloride inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes.
|
-
- 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-100609
-
4-P-PDOT
|
Melatonin Receptor
|
Neurological Disease
|
4-P-PDOT is a potent, selective and affinity Melatonin receptor (MT2) antagonist. 4-P-PDOT is >300-fold more selective for MT2 than MT1. 4-P-PDOT significantly counteracts Melatonin-mediated antioxidant effects (GSH/GSSG ratio, phospho-ERK, Nrf2 nuclear translocation, Nrf2 DNA-binding activity).
|
-
- HY-P1077
-
CALP1
|
Calcium Channel
mGluR
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
|
CALP1 is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 activates CaM-dependent phosphodiesterase activity.
|
-
- 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-12882A
-
Ifenprodil tartrate
|
iGluR
Potassium Channel
|
Neurological Disease
|
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM). Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator.
|
-
- HY-136065
-
bpV(phen)
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
bpV(phen), a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-128718
-
Carbodine
|
Influenza Virus
|
Infection
|
Carbodine (Carbocyclic cytidine) is a broad-spectrum antiviral agent active against DNA viruses, (+)RNA viruses, (-)RNA viruses, paramyxo, rhabdo and (+/-)RNA viruses, targets CTP synthetase that converts UTP to CTP. Carbodine (Carbocyclic cytidine) possesses significant antiviral activity against influenza virus types A0/PR-8/34 and A2/Aichi/2/68 in vitro.
|
-
- HY-P1077A
-
CALP1 TFA
|
Calcium Channel
mGluR
Phosphodiesterase (PDE)
Apoptosis
|
Inflammation/Immunology
|
CALP1 TFA is a calmodulin (CaM) agonist (Kd of 88 µM) with binding to the CaM EF-hand/Ca 2+-binding site. CALP1 TFA blocks calcium influx and apoptosis (IC50 of 44.78 µM) through inhibition of calcium channel opening. CALP1 TFA blocks glutamate receptor channels and blocks a store-operated nonselective cation channel. CALP1 TFA activates CaM-dependent phosphodiesterase activity.
|
-
- HY-101202
-
SNC80
NIH 10815
|
Opioid Receptor
|
Neurological Disease
|
SNC80 (NIH 10815) is a potent, highly selective and non-peptide δ-opioid receptor agonist with a Ki of 1.78 nM and an IC50 of 2.73 nM. SNC80 also selectively activates μ-δ heteromer in HEK293 cells with an EC50 of 52.8 nM. SNC80 shows antinociceptive, antihyperalgesic and antidepressant‐like effects. SNC80 has the potential for multiple headache disorders treatment.
|
-
- HY-17366A
-
Clozapine N-oxide dihydrochloride
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
Clozapine N-oxide dihydrochloride is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide dihydrochloride activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide dihydrochloride can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
|
-
- HY-17366
-
Clozapine N-oxide
|
mAChR
Dopamine Receptor
Drug Metabolite
|
Neurological Disease
|
Clozapine N-oxide is a major metabolite of Clozapine and a human muscarinic designer receptors (DREADDs) agonist. Clozapine N-oxide activates the DREADD receptor hM3Dq and hM4Di. Clozapine N-oxide can cross the blood-brain barrier. Clozapine is a potent dopamine antagonist and also a potent and selective muscarinic M4 receptor (EC50=11 nM) agonist.
|
-
- HY-B0639
-
Amifostine
WR2721
|
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Amifostine (WR2721) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine protects cells from damage by scavenging oxygen-derived free radicals. Amifostine reduces renal toxicity and has antiangiogenic action.
|
-
- HY-101392
-
Harmane
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
|
Cancer
Neurological Disease
|
Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect.
|
-
- HY-122818
-
bpV(phen) trihydrate
|
PTEN
Phosphatase
Parasite
Apoptosis
|
Cancer
Infection
Metabolic Disease
Inflammation/Immunology
|
bpV(phen) trihydrate, a insulin-mimetic agent, is a potent protein tyrosine phosphatase (PTP) and PTEN inhibitor with IC50s of 38 nM, 343 nM and 920 nM for PTEN, PTP-β and PTP-1B, respectively. bpV(phen) trihydrate inhibits proliferation of the protozoan parasite Leishmania in vitro. bpV(phen) trihydrate strongly induces the secretion of a large number of chemokines and pro-inflammatory cytokines, and it activates a Th1-type pathway (IL-12, IFNγ). bpV(phen) trihydrate can also induce cell apoptosis, and has anti-angiogenic and anti-tumor activity.
|
-
- HY-108391
-
C8-Ceramide
N-Octanoyl-D-erythro-sphingosine
|
Apoptosis
PKC
Autophagy
|
Cancer
Inflammation/Immunology
|
C8-Ceramide (N-Octanoyl-D-erythro-sphingosine) is a cell-permeable analog of naturally occurring ceramides. C8-Ceramide has anti-proliferation properties and acts as a potent chemotherapeutic agent. C8-Ceramide stimulates dendritic cells to promote T cell responses upon virus infections. C8-Ceramide induces slight activation of protein kinase (PKC) in vitro.
|
-
- HY-107146
-
PZ-128
P1pal-7
|
Protease-Activated Receptor (PAR)
|
Cancer
Cardiovascular Disease
|
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects.
|
-
- HY-14865B
-
Omadacycline tosylate
PTK 0796 tosylate; Amadacycline tosylate
|
Bacterial
Antibiotic
|
Infection
|
Omadacycline (PTK 0796) tosylate, a first-in-class orally active aminomethylcycline antibacterial, is a member of the tetracycline class of antibiotics. Omadacycline tosylate acts through the inhibition of bacterial protein synthesis by binding to the 30S ribosomal subunit. Omadacycline tosylate exhibits activity against a broad spectrum of bacteria, including Gram-positive, Gram-negative, anaerobic, and atypical pathogens. Omadacycline tosylate can be used for the research of acute bacterial skin and skin-structure infections, community-acquired pneumonia, and urinary tract infections.
|
-
- HY-105231
-
Bryostatin 1
|
PKC
HIV
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
|
-
- 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-125593
-
APG-1387
|
IAP
Apoptosis
|
Cancer
|
APG-1387, a bivalent SMAC mimetic and an IAP antagonist, blocks the activity of IAPs family proteins (XIAP, cIAP-1, cIAP-2, and ML-IAP). APG-1387 induces degradation of cIAP-1 and XIAP proteins, as well as caspase-3 activation and PARP cleavage, which leads to apoptosis. APG-1387 can be used for the research of hepatocellular carcinoma, ovarian cancer, and nasopharyngeal carcinoma.
|
-
- HY-N0638
-
Dendrobine
|
Influenza Virus
|
Infection
|
Dendrobine is an alkaloid isolated from Dendrobium nobile. Dendrobine possesses antiviral activity against influenza A viruses, with IC50s of 3.39 μM, 2.16 μM and 5.32 μM for A/FM-1/1/47 (H1N1), A/Puerto Rico/8/34 H274Y (H1N1) and A/Aichi/2/68 (H3N2), respectively.
|
-
- HY-P1416A
-
Foxy-5 TFA
|
Wnt
|
Cancer
|
Foxy-5 TFA, a WNT5A agonist, is a mimicking peptide of WNT5A which is a non-canonical member of the Wnt family. Foxy-5 TFA triggers cytosolic free calcium signaling without affecting β-catenin activation and it impairs the migration and invasion of epithelial cancer cells. Foxy-5 TFA effectively reduces the metastatic spread of WNT5A-low prostate cancer cells in an orthotopic mouse model.
|
-
- HY-B0639A
-
Amifostine trihydrate
WR2721 trihydrate
|
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
Amifostine trihydrate (WR2721 trihydrate) is a broad-spectrum cytoprotective agent and a radioprotector. Amifostine trihydrate selectively protects normal tissues from damage caused by radiation and chemotherapy. Amifostine trihydrate is potent hypoxia-inducible factor-α1 (HIF-α1) and p53 inducer. Amifostine trihydrate protects cells from damage by scavenging oxygen-derived free radicals. Amifostine trihydrate reduces renal toxicity and has antiangiogenic action.
|
-
- HY-15310
-
Ivermectin
MK-933
|
Parasite
HIV
Mitophagy
HSV
SARS-CoV
Antibiotic
Autophagy
|
Infection
Cancer
|
Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
|
-
- HY-108511A
-
PB28
|
Sigma Receptor
Apoptosis
SARS-CoV
|
Cancer
Infection
|
PB28 is a cyclohexylpiperazine derivative and a high affinity and selective sigma 2 (σ2) receptor agonist with a Ki of 0.68 nM. PB28 is also a σ1 antagonist with a Ki of 0.38 nM. PB28 is less affinity for other receptors. PB28 inhibits electrically evoked twitch in guinea pig bladder and ileum with EC50 values of 2.62 μM and 3.96 μM, respectively. PB28 can modulate SARS-CoV-2-human protein-protein interaction. PB28 induces caspase-independent apoptosis and has antitumor activity.
|
-
- HY-P1064
-
Apelin-36(human)
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(human) is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC50=8.61). Apelin-36 has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-108556A
-
RWJ-56110 dihydrochloride
|
Protease-Activated Receptor (PAR)
Apoptosis
|
Cardiovascular Disease
|
RWJ-56110 dihydrochloride is a potent, selective, peptide-mimetic inhibitor of PAR-1 activation and internalization (binding IC50=0.44 uM) and shows no effect on PAR-2, PAR-3, or PAR-4. RWJ-56110 dihydrochloride inhibits the aggregation of human platelets induced by both SFLLRN-NH2 (IC50=0.16 μM) and thrombin (IC50=0.34 μM), quite selective relative to U46619 (HY-108566). RWJ-56110 dihydrochloride blocks angiogenesis and blocks the formation of new vessels in vivo. RWJ-56110 dihydrochloride induces cell apoptosis.
|
-
- HY-13106
-
Olodanrigan
EMA401; PD-126055
|
Angiotensin Receptor
|
Neurological Disease
Endocrinology
|
Olodanrigan (EMA401) is a highly selective, orally active, peripherally restricted angiotensin II type 2 receptor (AT2R) antagonist. It is under development as a neuropathic pain therapeutic agent. Olodanrigan (EMA401) analgesic action appears to involve inhibition of augmented AngII/AT2R induced p38 and p42/p44 MAPK activation, and hence inhibition of DRG neuron hyperexcitability and sprouting of DRG neurons.
|
-
- HY-15589
-
GW9508
|
GPR40
Potassium Channel
|
Metabolic Disease
Inflammation/Immunology
Cardiovascular Disease
|
GW9508 is a potent and selective G protein-coupled receptors FFA1 (GPR40) and GPR120 agonist with pEC50s of 7.32 and 5.46, respectively. GW9508 shows ~100-fold selectivity for GPR40 over GPR120. GW9508 is inactive against other GPCRs, kinases, proteases, integrins and PPARs. GW9508 is a glucose-sensitive insulin secretagogue and an ATP-sensitive potassium (KATP) channels opener. Anti-inflammatory and anti-atherosclerotic activities.
|
-
- HY-12765
-
Losartan Carboxylic Acid
E-3174; EXP-3174
|
Angiotensin Receptor
|
Cardiovascular Disease
|
Losartan Carboxylic Acid (E-3174), an active carboxylic acid metabolite of Losartan, is an angiotensin II receptor type 1 (AT1) antagonist. The Ki values are 0.97, 0.57, 0.67 nM for rat AT1B/AT1A and human AT1, respectively. Losartan Carboxylic Acid blocks the angiotensin II-induced responses in vascular smoothmuscle cells (VSMC). Losartan Carboxylic Acid elevates plasma renin activities and reduces mean arterial pressure.
|
-
- HY-12583
-
A-366
|
Histone Methyltransferase
Epigenetic Reader Domain
|
Cancer
|
A-366 is a potent, highly selective, peptide-competitive histone methyltransferase G9a inhibitor with IC50s of 3.3 and 38 nM for G9a and GLP (EHMT1), respectively. A-366 shows >1000-fold selectivity over 21 other methyltransferases. A-366 is also a potent, nanomolar inhibitor of the Spindlin1-H3K4me3-interaction (IC50=182.6 nM). A-366 displays high affinity at human histamine H3 receptor (Ki=17 nM) and shows subtype selectivity among subsets of the histaminergic and dopaminergic receptor families.
|
-
- HY-P1064A
-
Apelin-36(human) TFA
|
HIV
|
Infection
Metabolic Disease
Cardiovascular Disease
|
Apelin-36(human) TFA is an endogenous orphan G protein-coupled receptor APJ agonist, with an EC50 of 20 nM. Apelin-36(human) TFA shows high affinity to human APJ receptors expressed in HEK 293 cells (pIC550=8.61). Apelin-36(human) TFA has been linked to two major types of biological activities: cardiovascular and metabolic. Apelin-36(human) TFA inhibits the entry of some HIV-1 and HIV-2 into the NP2/CD4 cells expressing APJ.
|
-
- HY-N0515
-
Ophiopogonin D
|
PPAR
NF-κB
Calcium Channel
|
Inflammation/Immunology
Cardiovascular Disease
|
Ophiopogonin D, isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca 2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D has been used to treat inflammatory and cardiovascular diseases for thousands of years.
|
-
- HY-12326A
-
c-di-AMP sodium
Cyclic diadenylate sodium; Cyclic-di-AMP sodium
|
STING
Bacterial
Endogenous Metabolite
|
Inflammation/Immunology
|
c-di-AMP (Cyclic diadenylate) sodium is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP sodium is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP sodium acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
|
-
- HY-122815
-
Fusicoccin
Fusicoccin A
|
Apoptosis
|
Cancer
|
Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity.
|
-
- HY-B1371A
-
-
- HY-15746
-
-
- HY-108357
-
-
- HY-12326
-
c-di-AMP
Cyclic diadenylate; Cyclic-di-AMP
|
STING
Bacterial
Endogenous Metabolite
|
Inflammation/Immunology
|
c-di-AMP (Cyclic diadenylate) is a STING agonist, which binds to the transmembrane protein STING thereby activating the TBK3-IRF3 signaling pathway, subsequently triggering the production of type I IFN and TNF. c-di-AMP (Cyclic diadenylate) is also a bacterial second messenger, which regulates cell growth, survival, and virulence, primarily within Gram-positive bacteria, and also regulates host immune response. c-di-AMP (Cyclic diadenylate) acts as a potent mucosal adjuvant stimulating both humoral and cellular responses.
|
-
- HY-106178
-
PMX-53
3D53
|
Complement System
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
PMX-53 (3D53) is a synthetic peptidic and a potent and orally active complement C5a receptor (CD88) antagonist with an IC50 of 20 nM. PMX-53 is also a low-affinity MrgX2 agonist that stimulates MrgX2-mediated mast cell degranulation. PMX-53 specifically binds to C5aR1 and does not bind to the second C5aR (C5L2) and C3aR. PMX-53 has anti-inflammatory, anticancer and antiatherosclerotic effects.
|
-
- HY-P1454A
-
Fz7-21 TFA
Ac-LPSDDLEFWCHVMY-NH2 TFA
|
Wnt
|
Cancer
|
Fz7-21 (Ac-LPSDDLEFWCHVMY-NH2) TFA , a peptide antagonist of Frizzled 7 (FZD 7) receptors, selectively binds to FZD7 CRD subclass. The EC50 values are 58 and 34 nM for human and mouse FZD7 CRD, respectively. Fz7-21 impairs Wnt/β-catenin signaling in HEK293 cells stimulated with exogenous WNT3A (IC50=100 nM) or transfected with a construct expressing WNT3A or WNT1. Fz7-21 also blocks WNT3A-mediated stabilization of β-catenin in mouse L cells (IC50=50 nM).
|
-
- HY-15295
-
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-100007
-
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-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-131344
-
mTOR inhibitor-8
|
mTOR
Autophagy
|
Cancer
|
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
|
-
- 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-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-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- 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-111412
-
-
- 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-138295
-
KRAS inhibitor-10
|
Ras
|
Cancer
|
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
|
-
- 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-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-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-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-13662
-
-
- HY-13662A
-
-
- HY-128617
-
Legumain inhibitor 1
|
Others
|
Cancer
|
Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC50 of 3.6 nM. Legumain inhibitor 1 can be used for cancer research.
|
-
- HY-119937
-
-
- HY-15253
-
-
- HY-13973A
-
-
- HY-104051
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-15444
-
-
- 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-U00410
-
-
- 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-131705
-
-
- 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-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-10846
-
-
- 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-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
|
Antibiotic
MMP
Bacterial
|
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-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-N8533
-
Sodium Camptothecin
|
DNA/RNA Synthesis
|
Cancer
Infection
|
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA.
|
-
- HY-13985
-
-
- 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-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-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-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-N0822
-
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-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-14165
-
-
- HY-19727A
-
-
- 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-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
|
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
|
-
- HY-19609
-
-
- HY-131268
-
-
- HY-N6619A
-
Lycoramine
|
AChE
|
Neurological Disease
|
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
|
-
- HY-104028
-
-
- HY-12814
-
TH588
|
DNA/RNA Synthesis
|
Cancer
|
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
- HY-12054
-
-
- HY-12420
-
JNJ-47117096 hydrochloride
MELK-T1 hydrochloride
|
MELK
FLT3
|
Cancer
|
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.
|
-
- HY-16982
-
Cercosporamide
(-)-Cercosporamide
|
Fungal
MNK
|
Cancer
Infection
|
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.
|
-
- HY-136347
-
-
- HY-13280
-
-
- HY-N4186
-
-
- HY-103002
-
SU5408
VEGFR2 Kinase Inhibitor I
|
VEGFR
|
Cardiovascular Disease
|
SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
|
-
- HY-B0497B
-
-
- HY-131446
-
Chk1-IN-5
|
Checkpoint Kinase (Chk)
|
Cancer
|
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.
|
-
- HY-50202
-
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
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.
|
-
- 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-124416
-
ML604086
|
CCR
|
Inflammation/Immunology
Endocrinology
|
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.
|
-
- HY-103490
-
Takinib
|
MAP3K
Apoptosis
|
Cancer
|
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.
|
-
- 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).
|
-
- 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-109574
-
Raf inhibitor 2
|
Raf
|
Cancer
|
Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.
|
-
- 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.
|
-
- 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-133019
-
-
- 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-10978
-
-
- 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
-
-
- HY-108941
-
Salicyl-AMS
|
Bacterial
|
Infection
|
Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.
|
-
- HY-15282
-
-
- HY-B0806
-
Proguanil
|
Parasite
Antifolate
|
Infection
|
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
|
-
- HY-N2597
-
-
- HY-B0806A
-
-
- HY-13420
-
-
- HY-100736
-
ML348
GNF-Pf-1127
|
Phospholipase
|
Cancer
|
ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.
|
-
- HY-15202
-
Binimetinib
MEK162; ARRY-162; ARRY-438162
|
MEK
Autophagy
|
Cancer
|
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
|
-
- HY-12726
-
-
- HY-N1724
-
-
- HY-15766
-
GNE-617
|
Nampt
|
Metabolic Disease
Cancer
|
GNE-617 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-111489B
-
-
- HY-126253
-
BI-4916
|
Others
|
Cancer
|
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor.
|
-
- HY-136485
-
-
- HY-B1863
-
Iprobenfos
|
Fungal
|
Infection
|
Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.
|
-
- HY-B0882
-
Edrophonium chloride
|
AChE
|
Neurological Disease
|
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-P1045
-
187-1, N-WASP inhibitor
|
Arp2/3 Complex
|
Others
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-124653
-
HSP27 inhibitor J2
J2
|
HSP
|
Cancer
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
|
-
- HY-P1045A
-
187-1, N-WASP inhibitor TFA
|
Arp2/3 Complex
|
Others
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-P1111A
-
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA 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 TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-135899
-
SIRT7 inhibitor 97491
|
Sirtuin
Apoptosis
|
Cancer
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
|
-
- 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-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-130795
-
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-N7674A
-
Angoline hydrochloride
|
STAT
|
Cancer
|
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-P1290
-
PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-10009
-
-
- HY-N7674
-
Angoline
|
STAT
|
Cancer
|
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-109019
-
Vorolanib
CM082; X-82
|
VEGFR
PDGFR
|
Cancer
Cardiovascular Disease
|
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
|
-
- HY-100734
-
-
- HY-123772
-
CDK5 inhibitor 20-223
|
CDK
|
Cancer
|
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
|
-
- HY-100899
-
-
- HY-101705
-
-
- HY-N6619
-
-
- HY-109877
-
-
- HY-100299
-
-
- HY-P2470
-
-
- HY-B0106
-
-
- HY-50710
-
KU-0063794
|
mTOR
|
Cancer
|
KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
|
-
- HY-137239
-
-
- HY-100303A
-
FR194738
|
Others
|
Metabolic Disease
|
FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
|
-
- HY-50946
-
-
- HY-15886
-
-
- HY-112131
-
-
- HY-19326
-
-
- HY-12971
-
Nampt-IN-1
LSN3154567
|
Nampt
|
Cancer
|
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
|
-
- HY-101479
-