Search Result
Results for "A level biology kinesin Inhibitors" in MCE Product Catalog:
9453
Inhibitors & Agonists
16
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-D0859
-
|
MOPS
|
Others
|
Others
|
|
MOPS is commonly used as a buffering agent in biology. MOPS buffer can maintain the pH of mammalian cell culture media.
|
-
- HY-16062
-
|
ARQ 621
|
Kinesin
|
Cancer
|
|
ARQ 621 is an allosteric, potent and selective inhibitor of Eg5, a microtubule-based ATPase motor protein involved in cell division. Anti-tumor activity. ARQ 621 is a kinesin inhibitor.
|
-
- HY-15187
-
|
Filanesib
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity.
|
-
- HY-U00439
-
-
- HY-15000
-
|
EMD534085
|
Kinesin
|
Cancer
|
|
EMD534085 is a potent and selective inhibitor of the mitotic kinesin-5 with an IC50 of 8 nM.
|
-
- HY-12839
-
-
- HY-133541
-
|
Glucopiericidin A
|
GLUT
ADC Cytotoxin
Apoptosis
|
Cancer
|
|
Glucopiericidin A is a natural piericidin compound obtained from a marine-derived Streptomyces strain. Glucopiericidin A serves as a glucose transporter (GLUT) chemical probe and suppresses glycolysis. Glucopiericidin A inhibits ATP-dependent filopodia protrusion with Piericidin A (PA; HY-114936) and has no effect alone. Glucopiericidin A induces cell apoptosis through reducing the reactive oxygen species (ROS) level by increasing PRDX1 and exhibits potent antitumor efficacy in ACHN mice xenografts.
|
-
- HY-19944
-
-
- 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-50759
-
-
- HY-D0850
-
|
Tartaric acid disodium dihydrate
Sodium tartrate dibasic dihydrate; Sodium tartrate dihydrate
|
Phosphatase
|
Cancer
|
|
Tartaric acid disodium dihydrate is a Acid phosphatase inhibitor, is a sodium salt used in buffers for molecular biology and cell culture applications.
|
-
- HY-108618
-
|
BC11-38
|
Phosphodiesterase (PDE)
|
Endocrinology
|
|
BC11-38 is a potent, selective, and biologically active PDE11 inhibitor, with IC50s of 0.28 µM and >100 µM for PDE11 and PDE1-10, respectively. BC11-38 elevates cAMP levels, PKA-mediated ATF-1 phosphorylation, and cortisol production in H295R cells.
|
-
- 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-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-N0686
-
-
- HY-P1290A
-
|
PKA Inhibitor Fragment (6-22) amide TFA
PKI-(6-22)-amide TFA
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide TFA is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide TFA can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-12069
-
|
SB-743921
|
Kinesin
|
Cancer
|
|
SB-743921 is a potent inhibitor of the mitotic kinesin KSP (Eg5), with a Ki of 0.1 nM.
|
-
- HY-14846A
-
|
Litronesib Racemate
LY2523355 Racemate
|
Kinesin
|
Others
|
|
Litronesib Racemate (LY2523355 Racemate) is the racemate of litronesib. Litronesib is a selective, allosteric inhibitor of kinesin Eg5.
|
-
- HY-101071A
-
|
Monastrol
(±)-Monastrol
|
Kinesin
Apoptosis
|
Cancer
|
|
Monastrol is a potent and cell-permeable inhibitor of the mitotic kinesin Eg5 with an IC50 value of 14 μM.
|
-
- HY-19966
-
-
- HY-N0857
-
-
- HY-14846
-
|
Litronesib
LY2523355
|
Kinesin
|
Cancer
|
|
Litronesib (LY2523355) is a selective mitosis-specific kinesin Eg5 inhibitor, with antitumor activity.
|
-
- HY-15949
-
-
- HY-103632
-
-
- HY-12455
-
|
Duocarmycin A
|
ADC Cytotoxin
Apoptosis
Caspase
|
Cancer
|
|
Duocarmycin A, which is one of well-known antitumor antibiotics, is a DNA alkylator and efficiently alkylates adenine N3 at the 3′ end of AT-rich sequences in the DNA. Duocarmycin A, as a chemotherapeutic agent, results HLC-2 cells typically apoptotic changes, including chromatin condensation, sub-G1 accumulation in DNA histogram pattern, and decrease in procaspase-3 and 9 levels.
|
-
- HY-12241
-
|
AZ82
|
Kinesin
|
Cancer
|
|
AZ82 is a selective kinesin-like protein KIFC1 (HSET/KIFC1) inhibitor, with a Ki of 43 nM and an IC50 of 300 nM for KIFC1.
|
-
- HY-15948
-
-
- HY-133777
-
|
Ciprofibrate impurity A
|
PPAR
|
Cancer
|
|
Ciprofibrate impurity A is an impurity of Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha.
|
-
- HY-112915
-
-
- HY-131005
-
-
- HY-N0023
-
|
Cistanoside A
|
Others
|
Inflammation/Immunology
|
|
Cistanoside A is a phenylethanoid isolated from Cistanche deserticola, reduces NO accumulation, but shows no effect on iNOS mRNA, iNOS protein levels or iNOS activity. Anti-inflammatory effect.
|
-
- HY-120295
-
|
A-192621
|
Endothelin Receptor
Apoptosis
|
Endocrinology
Cardiovascular Disease
|
|
A-192621 is a potent, nonpeptide, orally active and selective endothelin B (ETB) receptor antagonist with an IC50 of 4.5 nM and a Ki of 8.8 nM. The selectivity of A-192621 is 636-fold higher than ETA (IC50 of 4280 nM and Ki of 5600 nM). A-192621 promotes apoptosis in PASMCs. A-192621 alos causes elevation of arterial blood pressure and an elevation in the plasma ET-1 level.
|
-
- HY-110173
-
|
TC-G 1005
|
GPCR19
|
Metabolic Disease
|
|
TC-G 1005 is a potent, selective and orally active agonist of the BA receptor Takeda G protein-coupled receptor 5 (TGR5), with EC50s of 0.72 and 6.2 nM for hTGR5 and mTGR5, respectively. TC-G 1005 can reduce glucose levels in vivo.
|
-
- HY-N2638
-
|
Ilexsaponin A
|
Others
|
Cardiovascular Disease
|
|
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes.
|
-
- HY-15187A
-
|
(R)-Filanesib
(R)-ARRY-520
|
Kinesin
|
Cancer
|
|
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomer of Filanesib (HY-15187). Filanesib is a synthetic kinesin spindle protein (KSP) inhibitor with an IC50 of 6 nM.
|
-
- HY-115570
-
|
GW406108X
GW108X
|
Kinesin
ULK
Autophagy
|
Cancer
|
|
GW406108X is a specific Kif15 (Kinesin-12) inhibitor with an IC50 of 0.82 uM in ATPase assays. GW406108X, a potent autophagy inhibitor, shows ATP competitive inhibition against ULK1 with a pIC50 of 6.37 (427 nM). GW406108X inhibits ULK1 kinase activity and blocks autophagic flux, without affecting the upstream signaling kinases mTORC1 and AMPK.
|
-
- HY-B1025
-
|
Digoxigenin
Lanadigenin
|
Others
|
Inflammation/Immunology
|
|
Digoxigenin is a hapten, a small molecule with high antigenicity, that is used in many molecular biology applications, as an alternative probe labeling for in situ hybridization
|
-
- HY-130853
-
|
Thalidomide-NH-PEG2-C2-NH-Boc
|
E3 Ligase Ligand-Linker Conjugate
|
Cancer
|
|
Thalidomide-NH-PEG2-C2-NH-Boc is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a PEG linker used for dBRD9 (compound 6) synthesis. dBRD9 is a selective BRD9 probe PROTAC degrader for the study of BAF complex biology.
|
-
- HY-10299
-
|
GSK-923295
|
Kinesin
Apoptosis
|
Cancer
|
|
GSK-923295 is a special, allosteric inhibitor of centromere-associated protein-E (CENP-E) kinesin motor ATPase activity, with Ki of 3.2±0.2 nM and 1.6± 0.1 nM for human and canine, respectively.
|
-
- HY-121879
-
-
- HY-101298
-
|
Paprotrain
|
Kinesin
|
Neurological Disease
|
|
Paprotrain is a cell-permeable inhibitor of the kinesin MKLP-2, inhibits the ATPase activity of MKLP-2 with an IC50 of 1.35 μM and a Ki of 3.36 μM and shows a moderate inhibition activity on DYRK1A with an IC50 of 5.5 μM.
|
-
- HY-12691
-
|
BFCAs-1
|
Others
|
Cancer
|
|
BFCAs-1 is a polyamino polycarboxylic bifunctional chelating agent(BFCAs); a broad range of applications in chemistry, biology and medicine and diagnostic imaging (MRI, SPECT, PET).
|
-
- HY-14414
-
|
GSK4112
SR6452
|
Autophagy
|
Metabolic Disease
|
|
GSK4112 is a Rev-erbα agonist with EC50 of 0.4 μM, also is a small molecule chemical probe for the cell biology of the nuclear heme receptor Rev-erbα.
|
-
- HY-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-19373
-
-
- HY-B0853
-
|
Paclobutrazol
|
Fungal
|
Infection
|
|
Paclobutrazol is a triazole-containing plant growth retardant that is known to inhibit the biosynthesis of gibberellins. Paclobutrazol also has antifungal activities. Paclobutrazol, transported acropetally in plants, can also suppress the synthesis of abscisic acid and induce chilling tolerance in plants. Paclobutrazol is typically used to support research on the role of gibberellins in plant biology.
|
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- HY-N0045
-
-
- HY-112715
-
-
- 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-B0389
-
|
D-Glucose
Glucose; D-(+)-Glucose; Dextrose
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Glucose (Glucose), a monosaccharide, is an important carbohydrate in biology. D-Glucose is a carbohydrate sweetener and critical components of the general metabolism, and serve as critical signaling molecules in relation to both cellular metabolic status and biotic and abiotic stress response.
|
-
- HY-N6607
-
|
Tryptanthrin
|
Others
|
Inflammation/Immunology
|
|
Tryptanthrin is a potent and orally active cellular Leukotriene (LT) biosynthesis inhibitor. Tryptanthrin inhibits LT formation in human whole blood (IC50 = 10 µM) and reduces LTB4 levels in the rat pleurisy model.
|
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-115510
-
|
SPR inhibitor 3
SPRi3
|
Others
|
Inflammation/Immunology
|
|
SPR inhibitor 3 (SPRi3) is a potent sepiapterin reductase (SPR) inhibitor. SPR inhibitor 3 (SPRi3) displays high binding affinity to human SPR in a cell-free assay (IC50=74 nM) and efficiently reduces biopterin levels in a cell-based assay (IC50=5.2 μM). SPR inhibitor 3 (SPRi3) reduces neuropathic and inflammatory pain through a reduction of BH4 levels.
|
-
- HY-N6264
-
|
27-Deoxyactein
|
Others
|
Metabolic Disease
|
|
27-Deoxyactein is a constituent isolated from Cimicifuga racemosa, prevents TCDD-induced osteoblasts damage. 27-Deoxyactein inhibits increased AhR, CYP1A1 and ERK levels.
|
-
- HY-N4288
-
-
- HY-101606
-
-
- HY-101873S
-
-
- HY-112543
-
|
S119-8
|
Influenza Virus
|
Infection
|
|
S119-8 is a broad spectrum inhibitor of influenza A and B viruses, showing activity against multiple influenza B viruses and an oseltamivir-resistant influenza A virus, but does not inhibit a non-influenza virus, vesicular stomatitis nirus (VSV).
|
-
- HY-113794
-
-
- 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-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-N4115
-
-
- HY-101918
-
|
DS-1040 Tosylate
|
Others
|
Cardiovascular Disease
|
|
DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
|
-
- HY-16787
-
|
ICA-121431
|
Sodium Channel
|
Cardiovascular Disease
|
|
ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
|
-
- HY-18728
-
-
- HY-N6677
-
|
β-Apo-8'-carotenal
Apocarotenal
|
Cytochrome P450
|
Cancer
|
|
β-Apo-8'-carotenal (Apocarotenal), a provitamin A carotenoid, is an inducer of CYPlA1 and CYPlA2 in rat. β-Apo-8'-carotenal is present in many fruits and vegetables.
|
-
- HY-B1558A
-
|
Bifemelane hydrochloride
MCI-2016
|
Monoamine Oxidase
|
Neurological Disease
|
|
Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease.
|
-
- HY-B0939
-
|
Etebenecid
|
Others
|
Metabolic Disease
|
|
Etebenecid is a uricosuric agents, lower uric acid levels in the body by increasing the elimination of uric acid by the kidneys, also inhibits penicillin tubular secretion.
|
-
- HY-P2273
-
-
- HY-16210
-
|
Forodesine
BCX-1777; Immucillin-H
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
Forodesine (BCX-1777) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine is a potent human lymphocyte proliferation inhibitor. Forodesine could induce apoptosis in leukemic cells by increasing the dGTP levels.
|
-
- HY-16209
-
|
Forodesine hydrochloride
BCX-1777 hydrochloride; Immucillin-H hydrochloride
|
Nucleoside Antimetabolite/Analog
Apoptosis
|
Cancer
|
|
Forodesine hydrochloride (BCX-1777 hydrochloride) is a highly potent and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50 values ranging from 0.48 to 1.57 nM for human, mouse, rat, monkey and dog PNP. Forodesine hydrochloride is a potent human lymphocyte proliferation inhibitor. Forodesine hydrochloride could induce apoptosis in leukemic cells by increasing the dGTP levels.
|
-
- HY-76648
-
|
NBD-556
|
HIV
|
Infection
|
|
NBD-556, a CD4 mimetic, is a potent HIV-1 entry inhibitor that blocks the gp120-CD4 interaction. NBD-556 shows potent cell fusion and virus-cell fusion inhibitory activity at low micromolar levels.
|
-
- HY-107396
-
|
YM-750
|
Acyltransferase
|
Cardiovascular Disease
|
|
YM-750 is a potent acyl-CoA:cholesterol acyltransferase (ACAT) inhibitor (IC50=0.18 μM). ACAT catalyzes the formation of cholesteryl esters from cholesterol and long-chain fatty-acyl-coenzyme A.
|
-
- HY-N6741
-
|
β-Zearalenol
|
Others
|
Infection
Endocrinology
|
|
β-Zearalenol is a non-steroidal estrogenic mycotoxin synthesized by Fusarium species. β-Zearalenol potentially influences transcription and effects gene expression on translational level.
|
-
- HY-109101
-
|
Risdiplam
RG7916; RO7034067
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
Risdiplam (RG7916) is an orally administered, centrally and peripherally distributed SMN2 pre-mRNA splicing modifier that increases survival motor neuron (SMN) protein levels.
|
-
- HY-B0260
-
-
- HY-15583
-
-
- HY-129113
-
|
α-Chaconine
|
COX
|
Inflammation/Immunology
|
|
α-Chaconine, isolated from a Solanum tuberosum L. cv Jayoung, inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects.
|
-
- HY-12054A
-
-
- HY-12054
-
-
- HY-N1967
-
|
Dihydrocurcumin
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
|
Dihydrocurcumin, a major metabolites of curcumin, reduces lipid accumulation and oxidative stress. Dihydrocurcumin regulates mRNA and protein expression levels of SREBP-1C, PNPLA3 and PPARα, increases protein expression levels of pAKT and PI3K, and reduced the levels of cellular NO and ROS via Nrf2 signaling pathways.
|
-
- HY-P0035
-
-
- HY-112819
-
-
- 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-N0693
-
-
- HY-23119
-
-
- HY-19657
-
-
- HY-15720B
-
|
Glycyl H-1152 hydrochloride
|
ROCK
Aurora Kinase
CaMK
|
Neurological Disease
|
|
Glycyl H-1152 hydrochloride (compound 18) is a glycyl derivative of Rho-kinase inhibitors H-1152 dihydrochloride. Glycyl H-1152 hydrochloride inhibits ROCKII, Aurora A, CAMKII and PKG, with IC50s of 0.0118, 2.35, 2.57 and 3.26 μM respectively. Glycyl H-1152 hydrochloride has higher selective than H-1152 hydrochloride.
|
-
- HY-13503
-
-
- HY-14899
-
|
Taprenepag
CP-544326
|
Prostaglandin Receptor
|
Endocrinology
|
|
Taprenepag (CP-544326) is a potent and selective prostaglandin EP(2) agonist with IC50s of 10 and 15 nM for human and rat EP2, respectively. Taprenepag shows selectivity for EP2 over other EP receptors (IC50s>3200 nM for EP1, EP3, and EP4) and a panel of 37 G protein-coupled receptors.
|
-
- HY-103236
-
|
NSC232003
|
E1/E2/E3 Enzyme
|
Cancer
|
|
NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
|
-
- HY-122464
-
|
(±)-Jasmonic acid
|
Others
|
Others
|
|
(±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
|
-
- HY-107426
-
|
Verrucarin A
Muconomycin A
|
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Verrucarin A (Muconomycin A), a Type D macrocyclic mycotoxin derived from the pathogen fungus Myrothecium verrucaria, is an inhibitor of protein synthesis. Verrucarin A inhibits growth of leukemia cell lines and activates caspases and apoptosis and inflammatory signaling in macrophages. Verrucarin A effectively increased the phosphorylation of p38 MAPK and diminished the phosphorylation of ERK/Akt. Verrucarin A caused cell cycle deregulation through the induction of p21 and p53.
|
-
- HY-N2221
-
-
- HY-13271
-
|
Tubastatin A Hydrochloride
Tubastatin A HCl; TSA HCl
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
Tubastatin A (Hydrochloride) is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
|
-
- HY-B1041
-
|
Aminoguanidine hydrochloride
Pimagedine hydrochloride; GER-11; Aminoguanidinium chloride
|
Others
|
Endocrinology
|
|
Aminoguanidine hydrochloride is a diamine oxidase and NO synthase inhibitor, reduces levels of advanced glycation end products (AGEs) through interacting with 3-deoxyglucosone, is an investigational drug for the treatment of diabetic nephropathy.
|
-
- HY-129605
-
|
Ferulenol
|
Mitochondrial Metabolism
|
Infection
|
|
Ferulenol, a sesquiterpene prenylated coumarin derivative, specifically inhibits succinate ubiquinone reductase at the level of the ubiquinonecycle. Ferulenol shows good antimycobacterial activity and haemorrhagic action.
|
-
- HY-N1457
-
|
Chrysosplenetin
|
P-glycoprotein
Cytochrome P450
Ferroptosis
|
Metabolic Disease
|
|
Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A.
|
-
- 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-10038
-
|
A 922500
DGAT-1 Inhibitor 4a
|
Acyltransferase
|
Metabolic Disease
|
|
A 922500 (DGAT-1 Inhibitor 4a) is a potent, selective, and orally bioavailable diacylglycerol acyltransferase 1 (DGAT-1) inhibitor with IC50s of 9 and 22 nM against human and mouse DGAT-1, respectively.
|
-
- HY-N1447
-
-
- HY-18983
-
|
Calyculin A
(-)-Calyculin A
|
Phosphatase
|
Cancer
|
|
Calyculin A ((-)-Calyculin A) is a potent and cell-permeable protein phosphatase 1 (PP1) and protein phosphatase 2A (PP2A) inhibitor with IC50s of 2 nM and 0.5-1 nM, respectively.
|
-
- HY-138294
-
|
RAS/RAS-RAF-IN-1
|
Ras
Raf
|
Cancer
|
|
RAS/RAS-RAF-IN-1 is a potent RAS and RAS-RAF inhibitor. RAS/RAS-RAF-IN-1 has a KD of 5.0 μΜ-15 μΜ for cyclophilin A (CYPA) binding affinity. RAS/RAS-RAF-IN-1 has antitumor activity.
|
-
- HY-N0897
-
|
Corylifol A
Corylifol-A; Corylinin
|
STAT
|
Others
|
|
Corylifol A inhibits IL-6-induced STAT3 activation and phosphorylation, with an IC50 of 0.81 μM.
|
-
- HY-N2433
-
|
Paederosidic acid methyl ester
|
Potassium Channel
|
Neurological Disease
|
|
Paederosidic acid methyl ester is a ATP‐sensitive K + channel activator, isolated from P. scandens. Paederosidic acid methyl ester exhibits significant central analgesic activity, and enhances the threshold of pain by activating ATP‐sensitive K + channel in the brain and spinal cord level.
|
-
- HY-N2150
-
|
Psammaplin A
|
HDAC
DNA Methyltransferase
DNA/RNA Synthesis
Bacterial
|
Cancer
Infection
|
|
Psammaplin A, a marine metabolite, is a potent inhibitor of HDAC and DNA methyltransferases. Psammaplin A ia a highly potent and selective DAC1 inhibitor with an IC50 of 0.9 nM. Psammaplin A possess the antimicrobial effect on the Gram-positive bacteria and inhibits DNA synthesis and DNA gyrase activity. Antitumor Activity.
|
-
- HY-108486
-
|
Herbimycin A
|
Bacterial
Antibiotic
|
Infection
|
|
Herbimycin A, an ansamycin antibiotic, acts as a Src family kinase inhibitor. Herbimycin A binds to the SH domain and inhibits the activity of p60 v-src and p210 BCR-ABL Herbimycin A inhibits Hsp90 and impairs recovery from heat shock. Herbimycin A exhibits antiangiogenic activity in endothelial cells in vitro.
|
-
- HY-133019
-
-
- HY-B0283
-
|
Acipimox
K-9321
|
Others
|
Metabolic Disease
|
|
Acipimox (K-9321), a nicotinic acid analogue, is an antilipolytic compound. Acipimox acutely inhibits lipolysis and suppresses systemic levels of free fatty acids (FFAs) and improves insulin sensitivity.
|
-
- HY-15681
-
-
- HY-131907
-
|
LpxC-IN-5
|
Bacterial
|
Infection
|
|
LpxC-IN-5 is a potent non-hydroxamate LpxC (UDP-3-O-acyl-N-acetylglucosamine deacetylase) inhibitor with an IC50 of 20 nM. LpxC-IN-5 shows antibacterial activity against E. coli ATCC25922, P. aeruginosa ATCC27853, K. pneumoniae ATCC13883 and P. aeruginosa 5567 with MIC of 16, 4, 64, and 4 μg/mL, respectively.
|
-
- HY-N2065
-
|
Withaferin A
|
NF-κB
Ferroptosis
|
Cancer
Inflammation/Immunology
|
|
Withaferin A is a steroidal lactone isolated from Withania somnifera, inhibits NF-kB activation and targets vimentin, with potent antiinflammatory and anticancer activities. Withaferin A is an inhibitor of endothelial protein C receptor (EPCR) shedding.
|
-
- HY-120400
-
|
KDM5-C70
|
Histone Demethylase
|
Cancer
|
|
KDM5-C70 is an ethyl ester derivative of KDM5-C49 and a potent, cell-permeable and pan-KDM5 histone demethylase inhibitor. KDM5-C70 has an antiproliferative effect in myeloma cells, leading to genome-wide elevation of H3K4me3 levels.
|
-
- HY-134539
-
|
IMT1
|
Mitochondrial Metabolism
DNA/RNA Synthesis
|
Cancer
Metabolic Disease
|
|
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases.
|
-
- HY-16670
-
|
Dafadine-A
|
Cytochrome P450
|
Others
|
|
Dafadine-A, an analog of dafadine, is a novel inhibitor of DAF-9 cytochrome P450 in the nematode Caenorhabditis elegans; also inhibits the mammalian ortholog of DAF-9(CYP27A1).
|
-
- HY-16929
-
|
Latrunculin A
LAT-A
|
Arp2/3 Complex
|
Others
|
|
Latrunculin A (LAT-A) is a toxin isolated from the red sea sponge Latrunculia magnifica, binds to actin monomers, inhibits polymerization of actin, with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively.
|
-
- HY-P0092
-
-
- HY-125916
-
|
Pseurotin A
|
Others
|
Cancer
|
|
Pseurotin A, a secondary metabolite of Aspergillus and other fungi, is a competitive inhibitor of chitin synthase and a neuritogenic agent. Pseurotin A inhibits IgE production (IC50=3.6 μM). Antitumor activity.
|
-
- HY-130248
-
|
BAY-899
|
Others
|
Endocrinology
|
|
BAY-899 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 185 nM and 46nM for hLH (human LH) and rLH (rat LH), respectively. BAY-899 can reduce sex hormone levels.
|
-
- HY-124330
-
|
Tripolin A
(E)-Tripolin A
|
Aurora Kinase
|
Others
|
Tripolin A ((E)-Tripolin A) is a specific non-ATP competitive Aurora A kinase inhibitor, with IC50 values of 1.5 μM and 7 μM for Aurora A and Aurora B, respectively.
|
-
- HY-13254A
-
-
- HY-130841
-
|
Apcin-A
|
APC
Ligand for Target Protein for PROTAC
|
Cancer
|
|
Apcin-A, an Apcin derivative, is an anaphase-promoting complex (APC) inhibitor. Apcin-A interacts strongly with Cdc20, and inhibits the ubiquitination of Cdc20 substrates. Apcin-A can be used to synthesize the PROTAC CP5V (HY-130257).
|
-
- HY-107531
-
|
A 1070722
|
GSK-3
|
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain.
|
-
- HY-116090
-
|
Conoidin A
|
Parasite
|
Infection
Neurological Disease
Cardiovascular Disease
|
|
Conoidin A is a cell permeable inhibitor of T. gondii enzyme peroxiredoxin II (TgPrxII) with nematicidal properties. Conoidin A covalently binds to the peroxidatic Cys47 of TgPrxII, irreversibly inhibiting its hyperperoxidation activity with an IC50 of 23 µM. Conoidin A also inhibits hyperoxidation of mammalian PrxI and PrxII (but not PrxIII). Conoidin A has antioxidant, neuroprotective effects and can be used for the research of ischaemic heart disease.
|
-
- HY-13271A
-
|
Tubastatin A
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
Tubastatin A is a potent and selective HDAC6 inhibitor with IC50 of 15 nM in a cell-free assay, and is selective (1000-fold more) against all other isozymes except HDAC8 (57-fold more).
|
-
- HY-127002A
-
|
Squarunkin A hydrochloride
|
Src
|
Cancer
|
|
Squarunkin A hydrochloride is a potent and selective UNC119-cargo interaction inhibitor (IC50 of 10 nM for inhibiting the UNC119A-myristoylated Src N-terminal peptide interaction). Squarunkin A hydrochloride interferes with the activation of Src kinase in cells.
|
-
- HY-N2498
-
-
- HY-11011
-
|
A-770041
|
Src
|
Inflammation/Immunology
|
|
A-770041 is selective and orally active Src-family Lck inhibitor; A-770041 is a 147 nM inhibitor of Lck (1 mM ATP) and is 300-fold selective against Fyn, the other Src family kinase involved in T-cell signaling.
|
-
- HY-136194
-
|
TL13-22
|
ALK
|
Cancer
|
|
TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells.
|
-
- HY-N0694
-
|
Schisantherin A
Gomisin-C; Schizantherin-A; Wuweizi ester-A
|
NF-κB
|
Inflammation/Immunology
|
|
Schisantherin A is a dibenzocyclooctadiene lignan isolated from the fruit of Schisandra sphenanthera. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
|
-
- HY-N6787
-
-
- HY-107589A
-
|
BIO5192 hydrate
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-107589
-
|
BIO5192
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels.
|
-
- HY-103359
-
|
Ceranib1
|
Others
|
Cancer
|
|
Ceranib1 is a ceramidase inhibitor. Ceranib1 inhibits ceramidase activity toward an exogenous ceramide analog, induces the accumulation of multiple ceramide species, decreases levels of sphingosine and S1P. Ceranib1 inhibits the proliferation of ovarian cancer cells.
|
-
- HY-42849
-
-
- HY-42849A
-
-
- HY-N6796
-
|
Manumycin A
|
Farnesyl Transferase
Ras
Apoptosis
Phospholipase
|
Cancer
Infection
|
|
Manumycin A is an antibiotic. Manumycin A acts as a selective, competitive inhibitor of protein farnesyltransferase (FTase) with respect to farnesylpyrophosphate (Ki =1.2 μM), and as a noncompetitive inhibitor with respect to the Ras protein. Manumycin A induces apoptosis and exerts antitumor activity . Manumycin A suppresses exosome biogenesis and secretion via targeted inhibition of Ras/Raf/ERK1/2 signaling. Manumycin A is a nSMase inhibitor (EC50=0.25 μM).
|
-
- HY-N0466
-
-
- HY-13261
-
|
A66
|
PI3K
|
Cancer
|
|
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
|
-
- HY-129337
-
|
Reveromycin A
|
Antibiotic
Fungal
Apoptosis
|
Cancer
Infection
|
|
Reveromycin A, a benzoquinoid antibiotic isolated from the genus Streptomyces, is a selective inhibitor of protein synthesis in eukaryotic cells. Reveromycin A inhibits bone resorption by inducing apoptosis specifically in osteoclasts. Reveromycin A has antiproliferative activity against tumor cell lines and antifungal activity.
|
-
- HY-N6773
-
|
Cytochalasin A
|
HIV Protease
Fungal
|
Infection
|
|
Cytochalasin A is a cell-permeable fungal toxin that is an oxidized derivative of cytochalasin B. Cytochalasin A is an inhibitor of HIV-1 protease (IC50=3 μM) and inhibits actin polymerization and interferes with microtubule assembly by reacting with sulfhydryl groups. Antibiotic and fungicidal activitives.
|
-
- 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-N0505
-
|
Rosiridin
|
Monoamine Oxidase
|
Neurological Disease
|
|
Rosiridin, which is isolated from Rhodiola rosea L., inhibits MAO A and MAO B with potential beneficial effect in depression and senile dementia. Rosiridin shows an inhibition of 83.8% against MAO B at 10 μM (pIC50=5.38).
|
-
- HY-19563
-
-
- HY-16699
-
|
Nexturastat A
|
HDAC
|
Cancer
|
|
Nexturastat A is a potent and selective HDAC6 inhibitor with IC50 of 5 nM; no inhibition on other HDAC forms.
|
-
- HY-N3417
-
|
Kongensin A
|
HSP
RIP kinase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Kongensin A is a natural product isolated from Croton kongensis. Kongensin A is an effective, covalent HSP90 inhibitor that blocks RIP3-dependent necroptosishas. Kongensin A is a potent necroptosis inhibitor and an apoptosis inducer. Kongensin A has potential anti-necroptosis and anti-inflammation applications.
|
-
- HY-113427
-
-
- HY-113313
-
|
Aldosterone
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
|
-
- HY-19376
-
|
NAMI-A
|
FAK
|
Cancer
|
|
NAMI-A is a ruthenium-based drug characterised by the selective activity against tumour metastases, inhibits the adhesion and migration.
|
-
- HY-19741
-
-
- HY-N1505
-
-
- HY-B1228
-
|
Ribostamycin sulfate
Vistamycin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Ribostamycin sulfate (Vistamycin sulfate) is a broad-spectrum antimicrobial, inhibits bacterial protein synthesis at the level of 30S and 50S ribosomal subunit binding, also inhibits the chaperone activity of protein disulfide isomerase (PDI), used in pharmacokinetic and nephrotoxicity studies
|
-
- HY-136072
-
|
QPX7728-OH disodium
|
Bacterial
|
Infection
|
|
QPX7728-OH disodium (compound 13) is a boronic acid β-lactamase inhibitor, exacted from WO2018005662A1, compound 13. QPX7728-OH disodium inhibits cleavage of Nitrocefin (HY-108913) by purified class A, C and D enzymes, with Kis less than 0.1 µΜ.
|
-
- HY-103397
-
|
Nanaomycin A
|
DNA Methyltransferase
Parasite
|
Cancer
Infection
|
|
Nanaomycin A is the first selective DNMT3B inhibitor with an IC50 of 500 nM. Nanaomycin A, a quinone antibiotics, reactivates silenced tumor suppressor genes in human cancer cells. Nanaomycin A inhibits in vitro growth of the human malaria parasite Plasmodium falciparum with an IC80 value of 33.1 nM.
|
-
- HY-110096
-
-
- HY-126406
-
-
- HY-15595A
-
|
360A iodide
360 A iodide
|
G-quadruplex
Telomerase
|
Cancer
|
|
360A iodide is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
|
-
- HY-19725
-
-
- HY-N6584
-
-
- HY-W033577
-
|
Tricarbonyldichlororuthenium(II) dimer
CORM-2
|
Others
|
Inflammation/Immunology
|
|
Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level.
|
-
- HY-12458
-
|
Pyrindamycin A
|
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Pyrindamycin A is an antibiotic that inhibits DNA synthesis. Pyrindamycin A shows antitumor activities against murine leukemia, exhibits stronger cytotoxic activities towards murine and human tumor cell lines and especially towards doxorubicin-resistant cells, inhibits P388 and P388/ADR cells with the same IC50 of 3.9 μg/ml.
|
-
- HY-136071
-
-
- HY-136070
-
-
- 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-N2392
-
-
- HY-B0856
-
|
Validamycin A
|
Fungal
Tyrosinase
|
Infection
|
|
Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL. Validamycin A shows potent inhibitory activity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM. Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM.
|
-
- HY-14454
-
|
TPh A
Triphenyl Compound A
|
Others
|
Cancer
|
|
TPh A (Triphenyl Compound A) is a potent inhibitor of the nuclear protein pirin and binds specifically to pirin with a Ki of 0.6 uM. TPh A disrupts the formation of the bcl3–pirin complex. TPh A can be used as a novel small molecule tool to regulate pirin in cells.
|
-
- HY-114316
-
-
- HY-15595
-
|
360A
|
G-quadruplex
Telomerase
|
Cancer
|
|
360A is a selective stabilizer of G-quadruplex, and also inhibits telomerase activity with an IC50 of 300 nM for telomerase in TRAP-G4 assay.
|
-
- HY-16014
-
|
A-385358
|
Bcl-2 Family
|
Cancer
|
|
A-385358 is a selective inhibitor of Bcl-XL with Kis of 0.80 and 67 nM for Bcl-XL and Bcl-2, respectively.
|
-
- HY-Y0202
-
-
- HY-B1269
-
-
- HY-19759
-
|
SRT 2183
|
Sirtuin
Apoptosis
|
Cancer
|
|
SRT 2183 is a selective Sirtuin-1 (SIRT1) activator with an EC1.5 value of 0.36 μM. SRT 2183 induces growth arrest and apoptosis, concomitant with deacetylation of STAT3 and NF-κB, and reduction of c-Myc protein levels.
|
-
- HY-N6793
-
|
Phomopsin A
|
Microtubule/Tubulin
|
Cancer
|
|
Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis. Phomopsin A is a noncompetitive inhibitor of the binding of radiolabeled vincristine to tubulin.
|
-
- HY-10614
-
|
A-966492
|
PARP
|
Cancer
|
|
A-966492 is a novel and potent inhibitor of PARP1 and PARP2 with Ki of 1 nM and 1.5 nM, respectively.
|
-
- HY-N2300
-
-
- HY-100201
-
|
A-196
|
Histone Methyltransferase
|
Cancer
|
|
A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity.
|
-
- HY-A0122
-
-
- HY-118773
-
|
MreB Perturbing Compound A22 hydrochloride
A22 hydrochloride
|
Bacterial
|
Inflammation/Immunology
|
|
MreB Perturbing Compound A22 hydrochloride is a benzylisothiourea compound that interacts with the ATP binding site of MreB rapidly and reversibly. MreB Perturbing Compound A22 hydrochloride blocks normal rod shape formation and inhibits chromosome partitioning in E. coli, inhibiting growth (MIC=3.1 µg/ml).
|
-
- HY-N3389
-
-
- HY-130249
-
|
BAY-298
|
Others
|
Endocrinology
|
|
BAY-298 is an orally active and selective luteinizing hormone receptor (LH-R) antagonist with IC50s of 96 nM, 23 nM and 78 nM for hLH (human LH) and rLH (rat LH) and cLH (cynomolgus monkey LH), respectively. BAY-298 can reduce sex hormone levels.
|
-
- HY-129441
-
-
- HY-107433
-
-
- HY-N7452
-
-
- HY-50709
-
-
- HY-107833
-
|
A40926
|
Bacterial
|
Infection
|
|
A40926, the precursor of Dalbavancin, is a second-generation glycopeptide antibiotic. A40926 inhibits gram-positive bacteria, and is very active against Neisseria gonorrhoeae.
|
-
- HY-N6862
-
|
Lucideric acid A
|
MMP
|
Cancer
|
|
Lucideric acid A is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-12628
-
|
GNE-618
|
NAMPT
|
Cancer
|
|
GNE-618 is a potent, orally active nicotinamide phosphoribosyl transferase (NAMPT) inhibitor with an IC50 of 6 nM. GNE-618 depletes NAD levels and induces tumor cell death. Anti-tumor activity.
|
-
- HY-P2657
-
|
Verucopeptin
|
HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
|
Cancer
|
|
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
|
-
- HY-110195
-
|
Smurf1-IN-A01
A01
|
Others
|
Others
|
|
Smurf1-IN-A01 (A01) is an ubiquitin ligase Smad ubiquitination regulatory factor-1 (Smurf1) inhibitor with a kd of 3.664 nM, which increases BMP-2 responsiveness by inhibiting Smurf1-mediated Smad1/5 degradation.
|
-
- HY-N6781
-
|
Ophiobolin A
|
Phosphodiesterase (PDE)
|
Cancer
Infection
|
|
Ophiobolin A, a fungal metabolite and a phytotoxin, is a potent and irreversibly inhibitor of calmodulin-activated cyclic nucleotide phosphodiesterase, with an IC50 value of 9 μM. Ophiobolin A antimicrobial and anticancer activity.
|
-
- HY-N0754
-
|
Eupalinolide A
|
HSP
|
Inflammation/Immunology
|
|
Eupalinolide A, isolated from Eupatorium lindleyanum, induces the expression of HSP70 via the activation of HSF1 by inhibiting the interaction between HSF1 and HSP90.
|
-
- HY-N6702
-
-
- HY-113957
-
|
MPI_5a
|
HDAC
|
Cancer
|
|
MPI_5a is a potent and selective HDAC6 inhibitor (IC50=36 nM). MPI_5a weakly inhibits other HDAC isoforms. MPI_5a inhibits acyl-tubulin accumulation in cells with an IC50 value of 210 nM.
|
-
- HY-W010031
-
-
- HY-14682
-
|
GSK319347A
|
IKK
|
Inflammation/Immunology
|
|
GSK319347A is a dual inhibitor of TBK1 and IKKε with IC50s of 93 nM and 469 nM, respectively. GSK319347A also inhibits IKK2 with an IC50 of 790 nM.
|
-
- HY-137473
-
|
Methyl pyropheophorbide-a
Pyropheophorbide-a methyl ester
|
Apoptosis
|
Cancer
|
|
Methyl pyropheophorbide-a (Pyropheophorbide-a methyl ester), a chlorophyll-a derivative, is a potent photosensitizer that can be used in photodynamic therapy (PDT) of cancer. Methyl pyropheophorbide-a has photodynamic activity and can induce apoptosis and inhibit tumor growth.
|
-
- HY-17388
-
|
(±)-Huperzine A
|
AChE
|
Neurological Disease
|
|
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
|
-
- HY-N4185
-
-
- HY-10425
-
|
A-443654
|
Akt
|
Cancer
|
|
A-443654 is a pan-Akt inhibitor and has equal potency against Akt1, Akt2, or Akt3 within cells (Ki=160 pM).
|
-
- HY-13020
-
-
- HY-B0033
-
|
Vigabatrin hydrochloride
γ-Vinyl-GABA hydrochloride
|
GABA Receptor
|
Neurological Disease
|
|
Vigabatrin hydrochloride (γ-Vinyl-GABA hydrochloride), a inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin hydrochloride is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
|
-
- HY-15399
-
|
Vigabatrin
γ-Vinyl-GABA
|
GABA Receptor
|
Neurological Disease
|
|
Vigabatrin (γ-Vinyl-GABA), an inhibitory neurotransmitter GABA vinyl-derivative, is an orally active and irreversible GABA transaminase inhibitor. Vigabatrin is an antiepileptic agent, which acts by increasing GABA levels in the brain by inhibiting the catabolism of GABA by GABA transaminase.
|
-
- HY-100599
-
-
- HY-N6017
-
|
Bakkenolide A
|
Others
|
Cancer
|
|
Bakkenolide A is a natural product extracted from Petasites tricholobus. Bakkenolide A inhibits leukemia by regulation of HDAC3 and PI3K/Akt-related signaling pathways.
|
-
- HY-N0365
-
|
Sennoside A
|
HIV
|
Infection
|
|
Sennoside A is an anthraquinone glycoside, found in large quantities in leaves and pods of Senna (Cassia angustifolia). Sennoside A is a HIV-1 inhibitor effective on HIV-1 replication.
|
-
- HY-101835
-
-
- 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-N4096
-
|
Tsugaric acid A
|
Others
|
Inflammation/Immunology
|
|
Tsugaric acid A can significantly inhibit superoxide anion formation. Tsugaric acid A also protects human keratinocytes against damage induced by ultraviolet B (UV B) light. Tsugaric acid A can protect keratinocytes from photodamage.
|
-
- HY-N3925
-
-
- HY-116477
-
|
URB937
|
FAAH
|
Inflammation/Immunology
Neurological Disease
|
|
URB937 is an orally active and peripherally restricted FAAH inhibitor (IC50=26.8 nM) and increases anandamide levels. URB937 fails to affect FAAH activity in the brain (not penetrate the blood-brain barrier).
|
-
- HY-105755
-
|
Antimycin A3
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
Infection
|
|
Antimycin A3, an antibiotic isolated from a number of Streptomyces species, shows antifungal activities. Antimycin A3 is a potent inhibitor of respiration. Antimycin A3 inhibits the electron transfer activity of ubiquinol-cytochrome c oxidoreductase. Antimycin A3 inhibits ATP-citrate lyase with a Ki value of 60.1 µM.
|
-
- HY-114305
-
|
A1874
|
PROTAC
Epigenetic Reader Domain
|
Cancer
|
|
A1874 is a nutlin-based and BRD4-degrading PROTAC with a DC50 of 32 nM (induce BRD4 degradation in cells). Effective in inhibiting many cancer cell lines proliferation.
|
-
- HY-122135
-
-
- 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-101945
-
|
A-69412
|
Lipoxygenase
|
Inflammation/Immunology
|
|
A-69412 is a reversible, specific inhibitor of the hydrophilic 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
|
-
- HY-135985
-
|
DCLK1-IN-1
|
Others
|
Cancer
|
|
DCLK1-IN-1 is a selective, oral bioavailability in vivo-compatible chemical probe of the doublecortin like kinase 1 (DCLK1 kinase) domain. DCLK1-IN-1 inhibits DCLK1 and DCLK2 kinases (IC50: DCLK1=9.5/57.2 nM and DCLK2=31/103 nM in binding and kinase assay, respectively). DCLK1-IN-1 shows low toxicity, and can investigate DCLK1 biology and establish its role in cancer, like DCLK1 + pancreatic ductal adenocarcinoma (PDAC).
|
-
- HY-W040129
-
|
Chromomycin A3
|
Bacterial
Fungal
Antibiotic
|
Cancer
Infection
|
|
Chromomycin A3 is an aureolic acid-type antitumor antibiotic. Chromomycin A3 forms dimeric complexes with divalent cations, such as Mg 2+, which strongly binds to the GC rich sequence of DNA to inhibit DNA replication and transcription. Chromomycin A3 has a variety of utilities as a staining agent for human sperm chromatin, autophagy inducing agent, and apoptosis inhibitor.
|
-
- HY-15405
-
|
Teriflunomide
A77 1726
|
Others
|
Inflammation/Immunology
|
|
Teriflunomide is the active metabolite of leflunomide, an approved therapy for rheumatoid arthritis. It inhibits pyrimidine synthesis and therefore potently decreases T cell and B cell proliferation.
|
-
- HY-112205
-
-
- HY-P0002A
-
-
- HY-B0388
-
|
Probucol
DH-581
|
Virus Protease
|
Metabolic Disease
|
|
Probucol (DH-581) is an anti-hyperlipidemic drug by lowering the level of cholesterol in the bloodstream by increasing the rate of LDL catabolism.
|
-
- HY-B0554
-
-
- HY-P0002
-
-
- HY-U00323
-
|
Carbazole derivative 1
2-Fluoro-7-[(3-pyridinyl)methyl]-9H-carbazole
|
Others
|
Endocrinology
|
|
Carbazole derivative 1 is a carbazole derivative which can be used to reduce androgen or oestrogen levels in mammals, including humans.
|
-
- HY-N2998
-
|
Ganoderenic acid A
|
Others
|
Metabolic Disease
|
|
Ganoderenic acid A is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid A is a potent inhibitor of β-glucuronidase. Ganoderenic acid A has a potent hepatoprotective effect against CCl4-induced liver injury.
|
-
- HY-N2344
-
|
Procyanidin A1
Proanthocyanidin A1
|
PKC
|
Inflammation/Immunology
|
|
Procyanidin A1 (Proanthocyanidin A1) is a procyanidin dimer, which inhibits degranulation downstream of protein kinase C activation or Ca 2+ influx from an internal store in RBL-213 cells. Procyanidin A1 has antiallergic effects.
|
-
- HY-136460
-
|
Calcium ionophore I
ETH 1001
|
Calcium Channel
|
Others
|
|
Calcium ionophore I (ETH 1001) is a selective Ca 2+ ionophore for biological membranes. Calcium ionophore I can be used in Ca2+-selective microelectrodes that can be used for quantitative intracellular measurements of resting Ca2+-activities and of slowly changing Ca2+-levels.
|
-
- HY-128784
-
|
PK11007
|
MDM-2/p53
Reactive Oxygen Species
|
Cancer
|
|
PK11007 is a mild thiol alkylator with anticancer activity. PK11007 stabilizes p53 via selective alkylation of two surface-exposed cysteines without compromising its DNA binding activity. PK11007 induces mutant p53 cancer cell death by increasing reactive oxygen species (ROS) levels.
|
-
- HY-P1687
-
|
Siomycin A
|
Bacterial
Apoptosis
|
Cancer
|
|
Siomycin A is a thiopeptide antibiotic and is a Forkhead box M1(FOXM1) selective inhibitor without affecting other members of the Forkhead box family. Siomycin A has anti-tumor and promotes apoptosis.
|
-
- HY-100558
-
|
Bafilomycin A1
|
Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
|
Cancer
Infection
|
|
Bafilomycin A1 is a specific inhibitor of vacuolar H +-ATPase (V-ATPase) with I50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis.
|
-
- HY-11000
-
-
- HY-N5012
-
|
Eurycomanone
Pasakbumin A
|
Others
|
Endocrinology
|
|
Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
|
-
- HY-B1856
-
|
Haloxyfop
|
Others
|
Metabolic Disease
|
|
Haloxyfop is an aryloxyphenoxypropionic acid herbicide and is widely used in grass weeds in broad-leaf crops. Haloxyfop inhibits the acetyl coenzyme A carboxylase (EC 6.4.1.2) from corn seedling chloroplasts with an IC50 of 0.5 μM, but has no effect on this enzyme in pea.
|
-
- HY-107455
-
-
- HY-19356
-
|
Rocaglamide
Roc-A
|
NF-κB
HSP
Eukaryotic Initiation Factor (eIF)
|
Cancer
|
|
Rocaglamide (Roc-A) is isolated from the genus Aglaia and can be used for coughs, injuries, asthma and inflammatory skin diseases. Rocaglamide is a potent inhibitor of NF-κB activation in T-cells. Rocaglamide is a potent and selective heat shock factor 1 (HSF1) activation inhibitor with an IC50 of ~50 nM. Rocaglamide inhibits the function of the translation initiation factor eIF4A. Rocaglamide also has anticancer properties in leukemia.
|
-
- HY-107406
-
|
Antimycin A1
|
Mitochondrial Metabolism
|
Cancer
|
|
Antimycin A1 is a specific electron transfer inhibitor of ubiquinol-cytochrome c oxidoreductase. Antimycin A1 inhibits angiogenesis through decrease in VEGF production caused by inhibition of HIF-1α activation.
|
-
- HY-16968
-
|
SW033291
|
15-PGDH
|
Others
|
|
SW033291 is a potent and high-affinity inhibitor of 15-PGDH with a Ki of 0.1 nM. SW033291 increases prostaglandin PGE2 levels in bone marrow and other tissues. SW033291 also promotes tissue regeneration.
|
-
- HY-N6744
-
|
Chaetoglobosin A
|
Apoptosis
|
Cancer
Infection
|
|
Chaetoglobosin A, the active principle within the extract of Penicillium aquamarinium, is a member of the cytochalasan family. Chaetoglobosin A preferentially induces apoptosis. Chaetoglobosin A targets filamentous actin in CLL cells and thereby induces cell-cycle arrest and inhibits membrane ruffling and cell migration.
|
-
- HY-101512
-
|
A-395
|
Histone Methyltransferase
|
Cancer
|
|
A-395 is an antagonist of polycomb repressive complex 2 (PRC2) protein-protein interactions that potently inhibits the trimeric PRC2 complex (EZH2-EED-SUZ12) with an IC50 of 18 nM.
|
-
- HY-N6936
-
|
Sennidin A
|
HCV
Akt
GLUT
|
Infection
|
|
Sennidin A, isolated from the leaves of Cassia angustifolia, inhibits HCV NS3 helicase, with an IC50 of 0.8 μM. Sennidin A induces phosphorylation of Akt and glucose transporter 4 (GLUT4) translocation. Sennidin A stimulates the glucose incorporation.
|
-
- HY-12507
-
-
- HY-N6073
-
|
Soyasapogenol A
|
Apoptosis
|
Inflammation/Immunology
|
|
Soyasapogenol A, a triterpene compound, isolated from the roots of Abrus cantoniensis. Soyasapogenol A directly prevents apoptosis of hepatocytes, and secondly, inhibits the elevation of plasma TNF-α, which consequently results in the prevention of liver damage in the Concanavalin A-induced hepatitis model.
|
-
- HY-117832
-
-
- HY-12468
-
|
A-1210477
|
Bcl-2 Family
Apoptosis
|
Cancer
|
|
A-1210477 is a potent and selective inhibitor of MCL-1 with a Ki of 0.45 nM. A-1210477 specifically binds MCL-1 and promotes apoptosis of cancer cells in an MCL-1-dependent manner.
|
-
- HY-120944
-
|
BAY-7598
|
MMP
|
Inflammation/Immunology
|
|
BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
|
-
- HY-18990
-
|
GSK180736A
|
ROCK
|
Cardiovascular Disease
|
|
GSK180736A is potent Rho-associated coiled-coil kinase 1 (ROCK1) inhibitor with an IC50 of 100 nM. GSK180736A is also a selective and ATP-competitive G protein-coupled receptor kinase 2 (GRK2) inhibitor with an IC50 of 0.77 μM.
|
-
- HY-100226
-
|
A-205804
|
Integrin
|
Inflammation/Immunology
|
|
A-205804 is an orally bioavailable, potent and selective lead inhibitor of E-selectin and ICAM-1 expression, with an IC50 of 20 nM and 25 nM for E-selectin and ICAM-1, respectively. A-205804 can be used in the research of chronic inflammatory diseases.
|
-
- HY-N6795
-
|
Leptomycin A
|
CRM1
HIV
|
Infection
|
|
Leptomycin A, a Streptomyces metabolite, is an inhibitor of CRM1 (exportin 1) that blocks CRM1 interaction with nuclear export signals, preventing the nuclear export of a broad range of proteins. Leptomycin A suppresses HIV-1 replication. Less potent than Leptomycin B.
|
-
- HY-100540
-
|
Golgicide A
|
Enterovirus
|
Cancer
Infection
|
|
Golgicide A is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF), GBF1. Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species.
|
-
- HY-50880
-
-
- HY-137563
-
|
A2793
|
Potassium Channel
|
Neurological Disease
|
A2793 is an efficient dual TWIK-related acid-sensitive K + channel (TASK)-1/TRESK inhibitor, with an IC50 of 6.8 μM for mTRESK. A2764 is more selective for TRESK, and it only moderately influences TREK-1 and TALK-1.
|
-
- HY-101812
-
|
Terbufibrol
|
Others
|
Metabolic Disease
|
|
Terbufibrol has been shown highly active in reducing serum total cholesterol (TC) levels in the normal and hypercholesterolemic male rat.
|
-
- HY-N1483
-
|
Guanfu base A
|
Potassium Channel
|
Cardiovascular Disease
|
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes. Guanfu base A also inhibits HERG channel current.
|
-
- HY-13995B
-
|
Sevelamer carbonate
|
Others
|
Metabolic Disease
|
|
Sevelamer carbonate is an orally active and non-calcium-based phosphate binding agent and used for the hyperphosphatemia of chronic kidney disease (CKD)research. Sevelamer carbonate effectively lowers serum phosphorus levels hile having minimal effect on serum calcium or serum chloride levels in vivo. Sevelamer carbonate is considered as an improved, buffered form of sevelamer (HY-13995).
|
-
- HY-15764A
-
|
A 419259 trihydrochloride
RK 20449 trihydrochloride
|
Src
|
Cancer
|
|
A 419259 trihydrochloride is a Src family kinases inhibitor with IC50s of 9 nM, 3 nM and 3 nM for Src, Lck and Lyn, respectively.
|
-
- HY-110150
-
|
UNC3230
|
Others
|
Cancer
Inflammation/Immunology
|
|
UNC3230 is a potent, selective and ATP-competitive PIP5K1C inhibitor with an IC50 of ~41 nM. UNC3230 also inhibits PIP4K2C and does not inhibit any of the other lipid kinases that regulate phosphoinositide levels. UNC3230 has antinociceptive and anticancer effects.
|
-
- HY-13808
-
|
UNC 0631
|
Histone Methyltransferase
|
Cancer
|
|
UNC 0631 is a potent histone methyltransferase G9a inhibitor with an IC50 of 4 nM. UNC 0631 potently reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 25 nM.
|
-
- HY-N2112
-
|
Glaucocalyxin A
|
PI3K
Akt
Apoptosis
|
Cancer
|
|
Glaucocalyxin A, an ent-kauranoid diterpene from Rabdosia japonica var., induces apoptosis in osteosarcoma by inhibiting nuclear translocation of Five-zinc finger Glis 1 (GLI1) via regulating PI3K/Akt signaling pathway. Glaucocalyxin A has antitumor effect.
|
-
- 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-P0018
-
|
Pepstatin
Pepstatin A
|
Proteasome
HIV Protease
Autophagy
|
Infection
Cancer
|
|
Pepstatin (Pepstatin A) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-136532
-
|
ZT-1a
|
Others
|
Neurological Disease
|
|
ZT-1a is a potent, non-ATP-competitive and selective SPAK inhibitor. ZT-1a inhibits SPAK activity with IC50s of 44.3, 35.0, 46.7 μM at ATP concentrations of 0.01, 0.1 and 1 mM, respectively.
|
-
- HY-P0018A
-
|
Pepstatin Trifluoroacetate
Pepstatin A Trifluoroacetate
|
Proteasome
HIV Protease
|
Infection
|
|
Pepstatin Trifluoroacetate (Pepstatin A Trifluoroacetate) is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-N7043
-
|
Isosilybin A
|
Apoptosis
|
Cancer
|
|
Isosilybin A, a flavonolignan isolated from silymarin, has anti-prostate cancer (PCA) activity. Isosilybin A inhibits proliferation and induces G1 phase arrest and apoptosis in cancer cells, which activates apoptotic machinery in PCA cells via targeting Akt-NF-κB-androgen receptor (AR) axis.
|
-
- HY-N2298
-
|
Camellianin A
|
Apoptosis
|
Cancer
|
|
Camellianin A, the main flavonoid in A. nitida leaves, displays anticancer activity and angiotensin converting enzyme (ACE)-inhibitory activity. Camellianin A inhibits the proliferation of the human Hep G2 and MCF-7 cell lines and induces the significant increase of the G0/G1 cell population.
|
-
- HY-111417
-
-
- HY-111458
-
-
- HY-100368A
-
-
- HY-100522
-
|
FMK 9a
|
Autophagy
|
Cancer
|
|
FMK 9a is an autophagin-1 inhibitor with IC50 values of 80 and 73 μM in FRET and LRA assay.
|
-
- HY-N2306A
-
|
Aclacinomycin A hydrochloride
Aclarubicin hydrochloride
|
Proteasome
Topoisomerase
|
Cancer
|
|
Aclacinomycin A hydrochloride (Aclarubicin hydrochloride), a fluorescent molecule and the first described non-peptidic inhibitor showing discrete specificity for the CTRL (chymotrypsin-like) activity of the 20S proteasome. Aclacinomycin A hydrochloride is also a dual inhibitor of topoisomerase I and II. An effective anthracycline chemotherapeutic agent for hematologic cancers and solid tumors.
|
-
- HY-14164
-
-
- HY-101143
-
-
- HY-18009
-
|
LFM-A13
|
Btk
Polo-like Kinase (PLK)
JAK
|
Cancer
|
|
LFM-A13 is a potent BTK, JAK2, PLK inhibitor, inhibits recombinant BTK, Plx1 and PLK3 with IC50s of 2.5 μM, 10 μM and 61 μM; LFM-A13 shows no effects on JAK1 and JAK3, Src family kinase HCK, EGFR and IRK.
|
-
- HY-N5025
-
|
Bullatine A
|
P2X Receptor
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses. Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed.
|
-
- HY-15144
-
|
Trichostatin A
TSA
|
HDAC
|
Cancer
|
|
Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
|
-
- HY-B1217
-
|
Bronopol
BNPD; BNPK
|
Bacterial
|
Infection
|
|
Bronopol is an antimicrobial, with low mammalian toxicity (at in-use levels) and high activity against bacteria (especially the troublesome Gram-negative species).
|
-
- HY-P2279
-
-
- HY-10079
-
|
CHS-828
GMX1778
|
NAMPT
Apoptosis
|
Cancer
|
|
CHS-828 (GMX1778) is a competitive inhibitor of nicotinamide phosphoribosyltransferase (NAMPT), with an IC50 less than 25 nM. CHS-828 (GMX1778) exerts a cytotoxic effect by decreasing the cellular level of NAD+ and exhibits a potent anticancer activity.
|
-
- HY-112316
-
|
BAY1238097
|
Epigenetic Reader Domain
|
Cancer
|
|
BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome (IC50 <100 nM).
|
-
- HY-114395
-
|
NVS-ZP7-4
|
Others
|
Inflammation/Immunology
|
|
NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
|
-
- HY-14164A
-
-
- HY-100681
-
-
- 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-128553
-
-
- HY-100611
-
-
- HY-18303
-
|
AMG-47a
|
Src
VEGFR
p38 MAPK
JAK
|
Inflammation/Immunology
|
|
AMG-47a is a potent and orally active lymphocyte-specific protein tyrosine kinase (Lck) inhibitor, with an IC50 of 0.2 nM. AMG-47a also inhibits VEGF2, p38α, Jak3 and MLR and IL-2 with IC50s of 1 nM, 3 nM, 72 nM, 30 nM and 21 nM, respectively. AMG-47a has anti-inflammatory activity.
|
-
- HY-B0764A
-
|
Bucladesine calcium
Dibutyryl cAMP calcium salt; DBcAMP calcium salt
|
PKA
Phosphodiesterase (PDE)
Apoptosis
|
Others
|
|
Bucladesine calcium salt (Dibutyryl-cAMP calcium salt;DC2797 calcium salt) is a cell-permeable cyclic AMP (cAMP) analog and selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine calcium salt acts as a phosphodiesterase (PDE) inhibitor.
|
-
- HY-120813
-
|
ARN 077
URB913
|
Others
|
Inflammation/Immunology
|
|
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA. ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats.
|
-
- HY-N2959
-
|
Brevilin A
|
JAK
STAT
Apoptosis
Autophagy
|
Cancer
|
|
Brevilin A is a sesquiterpene lactone isolated from Centipeda minima with anti-tumor activity. Brevilin A is a selective inhibitor of JAK-STAT signal pathway by attenuating the JAKs activity and blocking STAT3 signaling (IC50 = 10.6 µM) in Cancer Cells. Brevilin A induces apoptosis and autophagy via mitochondrial pathway and PI3K/AKT/mTOR inactivation in colon adenocarcinoma cell CT26.
|
-
- HY-B0664S
-
|
Ciprofibrate D6
|
PPAR
|
Metabolic Disease
|
|
Ciprofibrate D6 is deuterium labeled Ciprofibrate. Ciprofibrate (Win35833) is a potent peroxisome proliferator, increases the phosphorylation level of the PPARalpha.
|
-
- HY-107850
-
-
- HY-N2102
-
|
Tenacissoside I
|
Others
|
Cancer
|
|
Tenacissoside I is a C21 steroid from the Marsdenia tenacissima, which is detected at relatively high level in M. tenacissima.
|
-
- HY-I1060
-
|
L-Alloisoleucine
(3R)-LS-Isoleucine; L-Allo-isoleucine
|
Endogenous Metabolite
|
Others
|
|
L-Alloisoleucine is a branched chain amino acid and is a stereo-isomer of L-isoleucine. L-Alloisoleucine is a common constituent of human plasma (albeit at low levels).
|
-
- HY-17504A
-
|
Rosuvastatin
ZD 4522
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
Rosuvastatin (ZD 4522) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-14347
-
|
EBE-A22
|
Others
|
Cancer
|
|
EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
|
-
- HY-N0619
-
|
Mulberroside A
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory antiapoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- HY-10029
-
|
Nutlin-3a
|
MDM-2/p53
E1/E2/E3 Enzyme
Autophagy
Apoptosis
|
Cancer
|
|
Nutlin-3a, an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
|
-
- HY-15005C
-
|
Sofosbuvir impurity A
|
HCV
|
Infection
|
|
Sofosbuvir impurity A, an diastereoisomer of Sofosbuvir, is the impurity of Sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
|
-
- HY-78349
-
|
A 77-01
|
TGF-β Receptor
|
Cancer
|
|
A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
|
-
- HY-15613
-
|
Maritoclax
Marinopyrrole A
|
Bcl-2 Family
|
Cancer
|
|
Maritoclax (Marinopyrrole A) is a novel and specific Mcl-1 inhibitor with an IC50 value of 10.1 μM, and shows >8 fold selectivity than BCL-xl (IC50 > 80 μM).
|
-
- HY-100528
-
|
Nanchangmycin
Nanchangmycin A
|
Bacterial
Antibiotic
|
Infection
|
|
Nanchangmycin, a polyether antibiotic produced by Streptomyces nanchangensis NS3226, inhibits gram-positive bacteria. Nanchangmycin is a broad spectrum antiviral active against Zika virus.
|
-
- HY-N2204
-
|
Swertiajaponin
|
Tyrosinase
|
Inflammation/Immunology
|
|
Swertiajaponin is a tyrosinase inhibitor, forms multiple hydrogen bonds and hydrophobic interactions with the binding pocket of tyrosinase, with an IC50 of 43.47 μM. Swertiajaponin also inhibits oxidative stress-mediated MAPK/MITF signaling, leading to decrease in tyrosinase protein level. Swertiajaponin suppresses melanin accumulation and exhibits strong anti-oxidative activity.
|
-
- HY-N7514
-
|
Strictosidinic acid
|
5-HT Receptor
|
Neurological Disease
|
|
Strictosidinic acid, an orally active glycoside indole monoterpene alkaloid isolated from Psychotria myriantha leaves, inhibits precursor enzymes of 5-HT biosynthesis and reduces the 5-HT levels. Strictosidinic acid has peripheral analgesic and antipyretic activities in mice.
|
-
- HY-129586
-
|
AT-007
|
Aldose Reductase
|
Metabolic Disease
|
|
AT-007 is an orally active central nervous system (CNS) penetrant Aldose Reductase inhibitor for treatment of Galactosemia with an IC50 value of 100 pM. AT-007 reduces toxic galactitol levels and prevents disease complications in GALT deficiency rats.
|
-
- HY-N2625A
-
|
Harmalol hydrochloride
|
Others
|
Others
|
|
Harmalol hydrochloride, a beta carboline alkaloid, presents in several medicinal plants such as Peganum harmala. Harmalol hydrochloride, main metabolite of Harmaline, significantly inhibits the dioxin-mediated induction of CYP1A1 at the transcriptional and posttranslational levels. Harmalol hydrochloride possesses antioxidant and hydroxyl radical-scavenging properties.
|
-
- HY-13746B
-
-
- HY-N6954
-
|
Garcinone C
|
ATM/ATR
STAT
CDK
|
Cancer
|
|
Garcinone C, a xanthone derivative, is a natural compound extracted from Garcinia oblongifolia Champ that is used as an anti-inflammatory, analgesia, astringency and granulation-promoting medicine, and has potential cytotoxic effects on certain cancers. Garcinone C stimulates the expression levels of ATR and 4E-BP1, while efficiently inhibiting the expression levels of cyclin B1, cyclin D1, cyclin E2, cdc2, Stat3 and CDK7. Garcinone C significantly inhibits cell viability of the human Nasopharyngeal carcinoma (NPC) cell lines CNE1, CNE2, HK1 and HONE1 in a time‑ and dose‑dependent manner.
|
-
- HY-13237
-
-
- HY-100183
-
-
- HY-N0288
-
-
- HY-135809
-
|
A2764 dihydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
A2764 dihydrochloride is a highly selective inhibitor of TRESK (TWIK-related spinal cord K + channel, K2P18.1), which has moderate inhibitory effects on TREK-1 and TALK-1. A2764 dihydrochloride is more sensitive to the activated mTRESK channels (IC50=6.8 μM) than the basal current. A2764 dihydrochloride can lead to cell depolarization and increased excitability in native cells, it has the potential for probing the role of TRESK channel in migraine and nociception.
|
-
- HY-108706
-
|
KDM2A/7A-IN-1
|
Histone Demethylase
|
Cancer
|
|
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases.
|
-
- HY-131013
-
|
GSHtracer
|
Others
|
Others
|
|
GSHtracer is a ratiometric probe for measuring of GSH levels. GSHtracer exhibits Ex/Em from 520/580 nm to 430/510 nm (upon GSH binding) .
|
-
- HY-U00340
-
|
PPAR agonist 1
|
PPAR
|
Metabolic Disease
|
|
PPAR agonist 1 is an agonist of PPAR α and PPAR γ, used for reducing blood glucose, lipid levels, lowering cholesterol and reducing body weight.
|
-
- HY-B2165
-
|
Bendazac L-Lysine
|
Others
|
Others
|
|
Bendazac L-Lysine is one of agents that have been introduced for the management of cataracts, protecting the level of vision in patients, thus delaying the need for surgical intervention.
|
-
- HY-100118
-
-
- HY-112468
-
|
PNU112455A hydrochloride
|
CDK
|
Cancer
|
|
PNU112455A hydrochloride is an ATP-competitive CDK2 and CDK5 inhibitor. PNU112455A hydrochloride binds to the ATP site of CDK2 and CDK5 with Kms of 3.6 and 3.2 μM, respectively.
|
-
- HY-12521
-
|
GSK-5498A
|
CRAC Channel
|
Inflammation/Immunology
|
|
GSK-5498A is a selective small molecule blocker of CARC (IC50, 1 μM); inhibits mediator release from mast cells, and pro-inflammatory cytokine release from T-cells in a variety of species.
|
-
- HY-108254
-
|
Bisindolylmaleimide IV
Arcyriarubin A
|
PKC
CMV
|
Infection
|
|
Bisindolylmaleimide IV (Arcyriarubin A) is a potent protein kinase C (PKC) inhibitor, with IC50s ranging from 0.1 to 0.55 μM. Bisindolylmaleimide IV also inhibits PKA (IC50=3.1-11.8μM). Bisindolylmaleimide IV is a potent, selective inhibitor of human cytomegalovirus (HCMV) replication in cell culture with an IC50 of 0.2 μM.
|
-
- HY-N6601
-
|
Pomolic acid
Randialic acid A
|
Apoptosis
|
Cancer
|
|
Randialic acid A (Pomolic acid) is a pentacyclic triterpene isolated from Euscaphis japonica (Tunb.). Randialic acid A (Pomolic acid) inhibits tumor cells growth and induces cell apoptosis. Randialic acid A (Pomolic acid) has a potential for the treatment of prostate cancer (PC).
|
-
- HY-114936
-
|
Piericidin A
AR-054
|
Bacterial
ADC Cytotoxin
Antibiotic
|
Cancer
Infection
Neurological Disease
|
|
Piericidin A (AR-054) is a natural mitochondrial NADH-ubiquinone oxidoreductase (complex I) inhibitor. Piericidin A is a potent neurotoxin and inhibits mitochondrial respiration by disrupting the electron transport system through its action on NADH-ubiquinone reductase. Piericidin A is also a potential quorum-sensing inhibitor that suppresses the expression of the virulence genes of Erwinia carotovora subsp. atroseptica (Eca). Piericidin A is an ADC cytotoxin and has anti-bacterial, anticancer, insecticidal activity.
|
-
- HY-13036A
-
|
IBT6A
|
Btk
|
Cancer
|
|
IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
|
-
- HY-19794
-
|
MP-A08
|
SPHK
|
Cancer
|
|
MP-A08 is a highly selective ATP competitive sphingosine kinase (SPHK1) inhibitor that targets both SphK1 and SphK2 with Ki values of 6.9 ± 0.8 μM and 27 ± 3 μM, respectively.
|
-
- HY-13036B
-
|
IBT6A hydrochloride
|
Btk
|
Cancer
|
|
IBT6A hydrochloride is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
|
-
- HY-A0150
-
|
Alclometasone
7a-Chloro-16a-methyl prednisolone
|
Glucocorticoid Receptor
|
Inflammation/Immunology
|
|
Alclometasone (7a-Chloro-16a-methyl prednisolone) is a glucocorticoid and inhibits the release of pro-inflammatory mediators from leukocytes. Alclometasone can be used to relieve corticosteroid-responsive dermatoses, including atopic dermatitis, eczema, psoriasis and allergic dermatitis.
|
-
- HY-100228A
-
-
- HY-106080A
-
|
Furegrelate sodium
U-63557A
|
Others
|
Cardiovascular Disease
|
|
Furegrelate Sodium (U-63557A) is a potent, orally available, and selective thromboxane synthase inhibitor. Furegrelate Sodium inhibits human platelet microsomal thromboxane A2 (TxA2) synthase with an IC50 of 15 nM. Furegrelate Sodium is being developed as an antiplatelet agent.
|
-
- 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-114267
-
|
Cbz-B3A
|
mTOR
|
Others
|
|
Cbz-B3A is a potent and selective inhibitor of mTORC1 signaling that appear to bind to ubiquilins 1, 2, and 4, and Cbz-B3A inhibits the phosphorylation of eIF4E-binding protein 1 (4EBP1).
|
-
- HY-17504
-
|
Rosuvastatin Calcium
Rosuvastatin hemicalcium; ZD 4522 Calcium
|
HMG-CoA Reductase (HMGCR)
Autophagy
Potassium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
Rosuvastatin Calcium (Rosuvastatin hemicalcium) is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin Calcium potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM, delayed cardiac repolarization, and thereby prolonged action potential durations (APDs) and corrected QT interval (QTc) intervals. Rosuvastatin Calcium reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin Calcium is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-17504C
-
|
(3R,5R)-Rosuvastatin
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Metabolic Disease
Cardiovascular Disease
|
|
(3R,5R)-Rosuvastatin is the (3R,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-17504D
-
|
(3S,5R)-Rosuvastatin
|
HMG-CoA Reductase (HMGCR)
Potassium Channel
Autophagy
|
Metabolic Disease
Cardiovascular Disease
|
|
(3S,5R)-Rosuvastatin is the (3S,5R)-enantiomer of Rosuvastatin. Rosuvastatin is a competitive HMG-CoA reductase inhibitor with an IC50 of 11 nM. Rosuvastatin potently blocks human ether-a-go-go related gene (hERG) current with an IC50 of 195 nM. Rosuvastatin reduces the expression of the mature hERG and the interaction of heat shock protein 70 (Hsp70) with the hERG protein. Rosuvastatin is very effective in lowering low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein levels.
|
-
- HY-104064
-
|
1A-116
|
Ras
|
Cancer
|
|
1A-116 is a Rac1 inhibitor, with antitumoral and antimetastatic effects in several types of cancer, such as breast cancer. 1A-116 prevents Rac1-regulated processes involved in the primary tumorigenesis and metastastic processes .
|
-
- HY-B1202A
-
-
- HY-13339
-
-
- HY-B0093A
-
-
- HY-B0422
-
|
Nateglinide
A4166; Senaglinide
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-30220
-
-
- HY-14781
-
-
- HY-N0398
-
-
- HY-116147
-
|
Ceranib-2
|
LPL Receptor
Apoptosis
|
Cancer
|
|
Ceranib-2 is a potent and nonlipid ceramidase inhibitor that inhibits cellular ceramidase activity with an IC50 of 28 μM in SKOV3 cells. Ceranib-2 induces the accumulation of multiple ceramide species, decreases levels of sphingosine and sphingosine-1-phosphate (S1P), and induces cell apoptosis. Anticancer activity.
|
-
- HY-U00235
-
|
SR121566A
|
Integrin
|
Inflammation/Immunology
|
|
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
|
-
- HY-120994B
-
|
Sp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
|
Sp-8-CPT-cAMPS, a cAMP analog, is a potent and selective activator of the cAMP-dependent protein kinas A (PKA I and PKA II). Sp-8-CPT-cAMPS selects site A of RI compares to site A of RII by 153-fold and site B of RII compares to site B of RI by 59-fold.
|
-
- HY-120994A
-
|
Rp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
|
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.
|
-
- HY-120994
-
-
- HY-134673A
-
|
UZH1a
|
Apoptosis
|
Cancer
|
|
UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1a can be used for epitranscriptomic modulation of cellular processes. UZH1a has antitumor activity. UZH1a also can be used as a chemical probe for studying METTL3.
|
-
- HY-125827
-
|
13-Methylberberine chloride
13-Methylberberinium chloride
|
Others
|
Cancer
Metabolic Disease
|
|
13-Methylberberine chloride (13-Methylberberinium chloride), a berberine analogue, has anti-adipogenic and antitumor activities. 13-Methylberberine chloride (13-Methylberberinium chloride) increases production of IL-12 and inhibits the expression of iNOS at posttranscriptional level in macrophages activated with LPS.
|
-
- 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-10432A
-
|
A 83-01 sodium salt
|
TGF-β Receptor
ALK
|
Cancer
|
|
A 83-01 sodium salt is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-N0931
-
|
Santacruzamate A
CAY-10683
|
HDAC
|
Cancer
|
|
Santacruzamate A (CAY-10683) is a potent and selective HDAC2 inhibitor with an IC50 of 119 pM.
|
-
- HY-100790
-
|
Ciliobrevin A
HPI-4
|
Hedgehog
|
Cancer
|
|
Ciliobrevin A is a hedgehog (Hh) signaling pathway inhibitor with median inhibitory concentration (IC50) less than 10 μM.
|
-
- HY-P1184
-
-
- HY-109120
-
|
Odevixibat
A4250
|
Others
|
Metabolic Disease
|
|
Odevixibat (A4250) is a potent, selective and orally active inhibitor of the ileal bile acid transporter (IBAT). Odevixibat (A4250)decreases cholestatic liver and bile duct injury in mice model. Odevixibat (A4250) has the potential for the treatment of primary biliary cirrhosis.
|
-
- HY-16592
-
|
Brefeldin A
BFA; Cyanein; Decumbin
|
Autophagy
CRISPR/Cas9
Mitophagy
HSV
Antibiotic
|
Cancer
Infection
|
|
Brefeldin A (BFA) is a lactone antibiotic and a specific inhibitor of protein trafficking. Brefeldin A blocks the transport of secreted and membrane proteins from endoplasmic reticulum to Golgi apparatus. Brefeldin A is also an autophagy and mitophagy inhibitor. Brefeldin A is a CRISPR/Cas9 activator. Brefeldin A inhibits HSV-1 and has anti-cancer activity.
|
-
- HY-15790
-
|
Elobixibat
A 3309; AZD 7806
|
Others
|
Metabolic Disease
|
|
Elobixibat is a potent ileal bile acid transporter (IBAT) inhibitor with IC50 values of 0.53 ± 0.17 nM, 0.13 ± 0.03 nM, and 5.8 ± 1.6 nM for human IBAT, mouse IBAT, and canine IBAT.
|
-
- HY-131182
-
|
DS-1971a
|
Sodium Channel
|
Neurological Disease
|
|
DS-1971a is a potent, selective, and orally active NaV1.7 inhibitor, with IC50s of 22.8 and 59.4 nM for hNaV1.7 and mNaV1.7, respectively. DS-1971a exerts analgesic effects.
|
-
- HY-103633
-
-
- HY-N0361
-
|
Dihydrocapsaicin
|
TRP Channel
|
Metabolic Disease
|
|
Dihydrocapsaicin is a natural capsaicin, acts as a selective TRPV1 agonist, and also increases p-Akt levels. Dihydrocapsaicin enhances the hypothermia-induced neuroprotection.
|
-
- HY-107929
-
|
Calcium polystyrene sulfonate
Poly(styrenesulfonic acid) calcium salt
|
Others
|
Cardiovascular Disease
|
|
Calcium polystyrene sulfonate is an ion-exchange resin used for reducing blood levels of potassium. Calcium polystyrene sulfonate is used to treat hyperkalemia in patients with chronic kidney disease (CKD).
|
-
- HY-B1136
-
|
Menbutone
Genabilic acid
|
Others
|
Inflammation/Immunology
|
|
Menbutone is an oxobutyric acid derivative, and is a choleretic.Menbutone has a rapid onset of action, reaching its maximum plasma level within 1 hour and lasting for roughly 10 hours.
|
-
- HY-17474A
-
|
Parecoxib Sodium
SC 69124A
|
COX
|
Inflammation/Immunology
Cancer
|
|
Parecoxib Sodium (SC 69124A) is a highly selective and orally active COX-2 inhibitor, the prodrug of Valdecoxib (HY-15762). Parecoxib Sodium is a nonsteroidal anti-inflammatory agent (NSAID) and inhibits prostaglandin (PG) synthesis. Parecoxib Sodium can be used for the relief of acute postoperative pain and symptoms of chronic inflammatory conditions such as osteoarthritis and rheumatoid arthritis in vivo.
|
-
- HY-100431A
-
|
IMR-1A
|
Notch
Drug Metabolite
|
Cancer
|
|
IMR-1A, a acid metabolite of IMR-1, is a Notch inhibitors with an IC50 of 0.5 μM. IMR-1A has a 50-fold increase in potency with respect to IMR-1. IMR-1 can metabolize in vivo to IMR-1A.
|
-
- HY-B0220E
-
|
Erythromycin A dihydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Erythromycin dihyrate dihydrate is a macrolide antibiotic produced by actinomycete Streptomyces erythreus with a broad spectrum of antimicrobial activity. Erythromycin dihyrate acts by binding to bacterial 50S ribosomal subunits and inhibits RNA-dependent protein synthesis by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid.
|
-
- HY-109785A
-
|
(R)-Gyramide A hydrochloride
|
|
Infection
|
|
(R)-Gyramide A hydrochloride is a bacterial DNA gyrase inhibitor that disrupts supercoiling activity with an IC50 value of 3.3 µM. (R)-Gyramide A hydrochloride demonstrates antibacterial activity against E. coli, P. aeruginosa, and S. enterica (MICs of 10-80 µM). (R)-Gyramide A hydrochloride does not affect the closely related enzyme topoisomerase IV.
|
-
- HY-128579
-
|
DW14800
|
Histone Methyltransferase
|
Cancer
|
|
DW14800 is a protein arginine methyltransferase 5 (PRMT5) inhibitor, with an IC50 of 17 nM. DW14800 reduces H4R3me2s levels and enhances the transcription of HNF4α, but does not alter PRMT5 expression. Anti-cancer activity.
|
-
- HY-126250
-
|
NPD-1335
|
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
|
|
NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death.
|
-
- HY-116042
-
|
FSCPX
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
FSCPX is a potent and selective irreversible antagonist of A1 adenosine receptor (A1AR), with low nanomolar potency for binding to the A1AR. FSCPX could modify the effect of NBTI, a nucleoside transport inhibitor, by reducing the interstitial adenosine level in the guinea pig atrium.
|
-
- HY-18299A
-
|
Purvalanol A
NG-60
|
CDK
Autophagy
Apoptosis
|
Cancer
|
|
Purvalanol A is a potent CDK inhibitor, which inhibits cdc2-cyclin B, cdk2-cyclin A, cdk2-cyclin E, cdk4-cyclin D1, and cdk5-p35 with IC50s of 4, 70, 35, 850, 75 nM, resepctively.
|
-
- HY-P2265
-
|
SAH-SOS1A
|
Ras
|
|
|
SAH-SOS1A is a KRas/son of sevenless 1 (SOS1) interaction inhibitor. SAH-SOS1A binds within nucleotide binding pocket of KRas (Kd values ranges from 106 - 176 nM for wild type KRas and KRas mutants). SAH-SOS1A inhibits nucleotide binding to KRas in a concentration dependent manner.
|
-
- HY-16576
-
|
TCS-PIM-1-4a
SMI-4a
|
Pim
Apoptosis
|
Cancer
|
|
TCS-PIM-1-4a (SMI-4a) is a pan-Pim kinases inhibitor that blocks mTORC1 activity via activation of AMPK. TCS-PIM-1-4a kills a wide range of both myeloid and lymphoid cell lines (IC50 values ranging from 0.8 μM to 40 μM).
|
-
- HY-10442
-
-
- HY-10432
-
|
A 83-01
|
ALK
TGF-β Receptor
|
Cancer
|
|
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-130242
-
|
PXS-5120A
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-5120A is a potent, irreversible fluoroallylamine inhibitor of Lysyl Oxidase-like 2/3 (LOXL2/3) with anti-fibrotic activity. PXS-5120A is >300-fold selective for LOXL2 (Ki of 83 nM; pIC50 of 8.4) over LOXL (pIC50 of 5.8).
|
-
- HY-111620
-
|
Ervogastat
PF-06865571
|
Acyltransferase
|
Metabolic Disease
Inflammation/Immunology
|
|
Ervogastat (PF-06865571) is a potent and well-tolerated diacylglycerol acyltransferase 2 inhibitor (DGAT2i). Ervogastat alone reduces steatosis and hepatic triglyceride levels in non-alcoholic steatohepatitis (NASH). Ervogastat combination with Clesacostat (an acetyl CoA-carboxylase inhibitor (ACCi)) can be used for the research of NASH with liver fibrosis therapy.
|
-
- HY-109523
-
|
Cerivastatin sodium
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cancer
Cardiovascular Disease
|
|
Cerivastatin sodium is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin sodium reduces low-density lipoprotein cholesterol levels. Cerivastatin sodium also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
|
-
- HY-N0462
-
|
Corilagin
|
Reverse Transcriptase
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Corilagin, a gallotannin, is isolated from Caesalpinia coriaria (Jacq.) Willd. Corilagin inhibits activity of reverse transcriptase of RNA tumor viruses. Corilagin inhibits the growth of Staphylococcus aureus with a MIC of 25 μg/mL. Corilagin shows good anti-tumor activity on hepatocellular carcinoma and ovarian cancer. Corilagin shows a low level of toxicity toward normal cells and tissues.
|
-
- HY-108355
-
|
R59949
|
PKC
|
Cancer
|
|
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol.
|
-
- HY-129458
-
|
Cerivastatin
|
HMG-CoA Reductase (HMGCR)
Ferroptosis
|
Cancer
Cardiovascular Disease
|
|
Cerivastatin is a synthetic lipid-lowering agent and a highly potent, well-tolerated and orally active HMG-CoA reductase inhibitor, with a Ki of 1.3 nM/L. Cerivastatin reduces low-density lipoprotein cholesterol levels. Cerivastatin also inhibits proliferation and invasiveness of MDA-MB-231 cells, mainly by RhoA inhibition, and has anti-cancer effect.
|
-
- HY-N7613
-
-
- HY-103000
-
|
HSF1A
|
HSP
|
Cancer
Cardiovascular Disease
|
|
HSF1A is a cell-permeable activator of heat shock transcription factor 1 (HSF1). HSF1A also acts as a specific inhibitor of TRiC/CCT. Chaperonin TCP-1 ring complex (TRiC)/chaperonin containing TCP-1 (CCT) plays a pivotal role in toxin translocation and/or refolding.
|
-
- HY-N6704
-
|
Enniatin A1
|
ERK
Apoptosis
|
Cancer
|
|
Enniatin A1 isolated from Fusarium mycotoxins is a cyclic hexadepsipeptide consisting of alternating D-α-hydroxyisovaleric acids and N-methyl-L-amino acids. Enniatin A1 possesses anticarcinogenic properties by induction of apoptosis and disruption of ERK signalling pathway. Enniatin A1 inhibits ACAT with an IC50 of 49 μM in rat liver microsomes.
|
-
- HY-B0597
-
-
- HY-N0853
-
-
- HY-13954
-
|
A 839977
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
A 839977 is a P2X7 selective antagonist; it blocks BzATP-evoked calcium influx at recombinant human, rat and mouse P2X7 receptors (IC50 values are 20 nM, 42 nM and 150 nM respectively) and reduces inflammatory and neuropathic pain in animal models; the antihyperalgesic effects of P2X7 receptor blockade are mediated by blocking the release of IL-1beta.
|
-
- HY-N3557
-
|
Cauloside A
Leontoside A
|
Fungal
|
Infection
|
|
Cauloside A (Leontoside A) is a saponin isolated from Dipsacus asper roots. Cauloside A has potent antifungal activity.
|
-
- HY-N2252
-
-
- HY-N0372
-
|
Licochalcone A
Licochalcone-A
|
Autophagy
|
Cancer
|
|
Licochalcone A, a flavonoid isolated from the famous Chinese medicinal herb Glycyrrhiza uralensis Fisch, presents obvious anti-cancer effects.
|
-
- HY-N0873
-
|
Sagittatoside A
Icariin-A
|
Others
|
Others
|
|
Sagittatoside A is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii).
|
-
- HY-P0216
-
-
- HY-15488
-
-
- HY-N1924
-
|
Crassicauline A
Crassicaulin A
|
Others
|
Neurological Disease
|
|
Crassicauline A (Crassicaulin A) is a bioactive alkaloid found in roots of Aconitum carmichaeli. Crassicauline A (Crassicaulin A) possesses feeding deterrent activity against T. castaneum adults with an EC50 of 1134.5 ppm.
|
-
- HY-107633
-
|
A 1120
|
Others
|
Metabolic Disease
|
|
A 1120 is a high-affinity nonretinoid retinol-binding protein 4 (RBP4) antagonist with a Ki value of 8.3 nM. A 1120 disrupts the interaction between RBP4 and its binding partner transthyretin.
|
-
- HY-15488A
-
-
- HY-109592
-
-
- HY-14929A
-
|
Migalastat hydrochloride
GR181413A
|
Others
|
Others
|
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
|
-
- HY-114286
-
|
PXS-5153A
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-5153A is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A could reduce crosslinks and ameliorates fibrosis.
|
-
- HY-N0712
-
|
Typhaneoside
|
Autophagy
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Typhaneoside, extracted from Typha angustifolia L., Typhaneoside can inhibit the excessive autophagy of hypoxia/reoxygenation cells and increase the phosphorylation of Akt and mTOR. Typhaneoside has certain effects on the cardiovascular system, including lowering blood lipid levels, promoting antiatherosclerosis activities, as well as improving immune and coagulation function.
|
-
- HY-12219B
-
|
MSI-1701
|
Others
|
Metabolic Disease
|
|
MSI-1701 is an analogue of MSI-1436 which can control weight gain and blood glucose level extracted from patent US 7410959 B1.
|
-
- HY-N3514
-
|
Kuwanon E
|
Others
|
Cancer
|
|
Kuwanon E is a flavonoid isolated from Morus alba, cytotoxic to human monocytic leukemic cell lines, and reduces the level of IL-1β.
|
-
- HY-P1742
-
-
- HY-120722
-
|
TCH-165
|
Proteasome
|
Cancer
|
|
TCH-165 is a small molecule modulator of proteasome assembly, which increases 20S levels and facilitates 20S-mediated protein degradation.
|
-
- HY-14595
-
|
Biochanin A
4-Methylgenistein; Olmelin
|
FAAH
Autophagy
|
Neurological Disease
Cancer
|
|
Biochanin A is a naturally occurring fatty acid amide hydrolase (FAAH) inhibitor, which inhibits FAAH with IC50s of 1.8, 1.4 and 2.4 μM for mouse, rat, and human FAAH, respectively.
|
-
- HY-128553A
-
|
(Rac)-Antineoplaston A10
|
Ras
Apoptosis
|
Cancer
|
|
(rac)-Antineoplaston A10 is the racemate of Antineoplaston A10. Antineoplaston A10 is a Ras inhibitor potentially for the treatment of glioma, lymphoma, astrocytoma and breast cancer.
|
-
- HY-12843
-
|
Bohemine
|
CDK
ERK
|
Cancer
|
|
Bohemine is a purine analogue and is a synthetic and selective CDK inhibitor with IC50s of 4.6 μM, 83 μM, and 2.7 μM for Cdk2/cyclin E, Cdk2/cyclin A, and Cdk9/cyclin T1, respectively. Bohemine also inhibits ERK2 with an IC50 of 52 μM and has less inhibitory effect on CDK1, CDK4 and CDK6. Bohemine has a broad spectrum anti-cancer activities.
|
-
- HY-B0579
-
-
- HY-16677A
-
-
- HY-N0134
-
-
- HY-14531
-
|
Talarozole
R115866
|
RAR/RXR
Cytochrome P450
Autophagy
|
Inflammation/Immunology
|
|
Talarozole (R115866) is an oral systemic all-trans retinoic acid metabolism blocking agent (RAMBA) which increases intracellular levels of endogenous all-trans retinoic acid (RA). Talarozole inhibits both CYP26A1 and CYP26B1 with IC50s of 5.4 and 0.46 nM, respectively.
|
-
- HY-15858A
-
|
AP-III-a4 hydrochloride
ENOblock hydrochloride
|
Enolase
|
Cancer
|
|
AP-III-a4 hydrochloride (ENOblock hydrochloride) is a novel small molecule which is the first, nonsubstrate analogue that directly binds to enolase and inhibits its activity (IC50=0.576 uM); inhibit cancer cell metastasis in vivo.
|
-
- HY-N2278
-
|
Kushenol A
Leachianone E
|
Tyrosinase
Glucosidase
|
Cancer
|
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively. Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase. Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging.
|
-
- HY-10524
-
|
GSK1904529A
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
GSK1904529A is a potent, selective, orally active, and ATP-competitive inhibitor of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR), with IC50s of 27 and 25 nM, respectively. GSK1904529A shows poor activity (IC50>1 μM) in 45 other serine/threonine and tyrosine kinases. GSK1904529A exhibits anti-tumor activity.
|
-
- HY-B0765
-
-
- HY-B1747
-
|
Pyrithione
|
Bacterial
Fungal
|
Infection
|
|
Pyrithione, a Transition metal complexe, is a zinc ionophore that causes increased zinc levels within mammalian cells. Pyrithione has potent bactericidal and anti-fungal activity.
|
-
- HY-N2232
-
|
N-Feruloyloctopamine
|
Akt
p38 MAPK
|
Cancer
|
|
N-Feruloyloctopamine, isolated from Garlic skin, is an antioxidant constituent. N-Feruloyloctopamine significantly decreases the phosphorylation levels of Akt and p38 MAPK.
|
-
- HY-106101
-
|
Echinomycin
Quinomycin A; NSC-13502
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Echinomycin (Quinomycin A) is potent small-molecule and cell-permeable inhibitor of hypoxia-inducible factor-1 (HIF-1) DNA-binding activity. Echinomycin selectively inhibits the cancer stem cells (CSCs) with an IC50 of 29.4 pM.
|
-
- HY-106376A
-
|
L-Buthionine-(S,R)-sulfoximine
L-Buthionine sulfoximine; L-BSO
|
Ferroptosis
|
Cancer
|
|
L-Buthionine-(S,R)-sulfoximine is a cell-permeable, potent, fast acting and irreversible inhibitor of g-glutamylcysteine synthetase and depletes cellular glutathione levels. The IC50 value of L-Buthionine-(S,R)-sulfoximine on melanoma, breast and ovarian tumor specimens are 1.9 μM, 8.6 μM, and 29 μM, respectively.
|
-
- HY-135747
-
|
Gut restricted-7
GR-7
|
Bacterial
|
Infection
|
|
Gut restricted-7 (GR-7) is a potent, covalent and orally active pan-bile salt hydrolase (BSH) inhibitor. Gut restricted-7 has a tissue-selective and is restricted to the gut. Gut restricted-7 decreases gut bacterial BSHs and decreases deconjugated bile acid levels in feces of mice.
|
-
- HY-N0633
-
-
- HY-135199
-
|
Ubiquitination-IN-1
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Ubiquitination-IN-1 (compound 24) is a ubiquitination and Cksl-Skp2 protein-protein interaction (IC50=0.17 μM) inhibitor. Ubiquitination-IN-1 increases levels of p27. Ubiquitination-IN-1 has the potential for treatment disease by blocking the degradation of tumor suppressors.
|
-
- HY-N0643
-
|
Carnosol
|
Ribosomal S6 Kinase (RSK)
Keap1-Nrf2
|
Cancer
|
|
Carnosol is a potent Ribosomal S6 Kinase (RSK2) inhibitor that could be useful for treating gastric cancer, with an IC50 of ~5.5 μM. Carnosol, a Nrf2 activator, increases the nuclear levels of Nrf2 and can promote the expression of heme oxygenase 1 (HMOX1).
|
-
- HY-14137
-
-
- HY-111174
-
-
- HY-B0958
-
|
Mupirocin
BRL-4910A; Pseudomonic acid
|
Bacterial
Antibiotic
|
Infection
|
|
Mupirocin (BRL-4910A) is an orally active antibiotic isolated from Pseudomonas fluorescens. Mupirocin (BRL-4910A) apparently exerts its antimicrobial activity by reversibly inhibiting isoleucyl-transfer RNA, thereby inhibiting bacterial protein and RNA synthesis.
|
-
- HY-W002585
-
|
O6-Benzylguanine
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
O6-Benzylguanine, a guanine analog, is the DNA repair enzyme O6-alkylguanine-DNA alkyltransferase (MGMT/AGT) inhibitor. O6-Benzylguanine acts as an AGT substrate, which transfers its benzyl group to the AGT cysteine residue, thereby irreversibly inactivating AGT and preventing DNA repair. O6-Benzylguanine induces tumor cell apoptosis. Antineoplastic activity.
|
-
- 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-N1713
-
-
- HY-103128
-
-
- HY-P0018B
-
|
Pepstatin Ammonium
Pepstatin A Ammonium
|
Proteasome
HIV Protease
|
Cancer
Infection
|
|
Pepstatin Ammonium is a specific aspartic protease inhibitor produced by actinomycetes, with IC50s of 4.5 nM, 6.2 nM, 150 nM, 290 nM, 520 nM and 260 nM for hemoglobin-pepsin, hemoglobin-proctase, casein-pepsin, casein-proctase, casein-acid protease and hemoglobin-acid protease, respectively. Pepstatin Ammonium also inhibits HIV protease.
|
-
- HY-N1441
-
|
Afzelin
Kaempferol-3-O-rhamnoside
|
Mitochondrial Metabolism
PTEN
Bacterial
Autophagy
|
Infection
Inflammation/Immunology
|
|
Afzelin (Kaempferol-3-O-rhamnoside) is is a flavonol glycoside found in Houttuynia cordata Thunberg and is widely used in the preparation of antibacterial and antipyretic agents, detoxicants and for the treatment of inflammation. Afzelin attenuates the mitochondrial damage, enhances mitochondrial biogenesis and decreases the level of mitophagy-related proteins, parkin and PTEN-induced putative kinase 1. Afzelin improves the survival rate and reduces the serum levels of alanine aminotransferase and pro-inflammatory cytokines in D-galactosamine (GalN)/LPS -treated mice.
|
-
- HY-N2118
-
|
Bilobetin
|
PPAR
PKA
|
Metabolic Disease
|
|
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity.
|
-
- HY-130609A
-
|
Aβ42-IN-1 free base
|
γ-secretase
|
Neurological Disease
|
|
Aβ42-IN-1 free base (compound 1v) is an orally active, high brain exposure γ-secretase modulator. Aβ42-IN-1 free base potently reduces Aβ42 levels with an IC50 value of 0.091 µM, and significantly reduces brain Aβ42 levels in mice. Aβ42-IN-1 free base is a promising compound for the treatment of Alzheimer’s disease.
|
-
- HY-100612
-
|
T16Ainh-A01
|
Chloride Channel
|
Others
|
|
T16Ainh-A01, an aminophenylthiazole, is a potent transmembrane protein 16A (TMEM16A) inhibitor, inhibiting TMEM16A-mediated chloride currents with an IC50 value of ~1 µM. TMEM16A (ANO1) functions as a calcium-activated chloride channel (CaCC).
|
-
- HY-N7394A
-
|
(-)-Zuonin A
D-Epigalbacin
|
JNK
|
Cancer
|
|
(-)-Zuonin A (D-Epigalbacin), a naturally occurring lignin, is a potent, selective JNKs inhibitor, with IC50s of 1.7 μM, 2.9 μM and 1.74 μM for JNK1, JNK2 and JNK3, respectively.
|
-
- HY-80012
-
|
SJB3-019A
|
Deubiquitinase
|
Cancer
|
|
SJB3-019A is a potent and novel USP1 inhibitor, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.
|
-
- HY-122614
-
|
S29434
NMDPEF
|
Autophagy
|
Neurological Disease
|
|
S29434 (NMDPEF) is a potent, competitive, selective and cell-permeable inhibitor of quinone reductase 2 (QR2), with IC50s ranging from 5 to 16 nM for human QR2 at different organizational levels, and has good selectivity for QR2 over QR1. S29434 (NMDPEF) induces autophagy and inhibits QR2-mediated ROS production.
|
-
- HY-112205A
-
|
RR-11a analog
|
Parasite
|
Infection
|
|
RR-11a analog is a potent and selective inhibitors of asparaginyl endopeptidases (AE) (Legumain), with IC50 values of 4.5 nM, 4.5 nM and 31 nM for AE1 in Trichomonas Vaginalis, AE in Ixodes ricinus and AE in Schistosoma mansoni, respectively.
|
-
- HY-14521
-
|
Lometrexol
DDATHF
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol (DDATHF), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol has anticancer activity. Lometrexol also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-14521B
-
|
Lometrexol hydrate
DDATHF hydrate
|
Antifolate
Apoptosis
|
Cancer
|
|
Lometrexol hydrate (DDATHF hydrate), an antipurine antifolate, can inhibit the activity of glycinamide ribonucleotide formyltransferase (GARFT) but do not induce detectable levels of DNA strand breaks. Lometrexol hydrate can further inhibit de novo purine synthesis, causing abnormal cell proliferation and apoptosis, even cell cycle arrest. Lometrexol hydrate has anticancer activity. Lometrexol hydrate also is a potent human Serine hydroxymethyltransferase1/2 (hSHMT1/2) inhibitor.
|
-
- HY-111388
-
|
SEL120-34A
|
CDK
|
Cancer
|
|
SEL120-34A 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-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-18963
-
|
Lavendustin A
RG-14355
|
EGFR
|
Cancer
|
|
Lavendustin A (RG-14355), isolated from Streptomyces Griseolavendus, is a potent, specific and ATP-competitive inhibitor of tyrosine kinase, with an IC50 of 11 ng/mL for EGFR-associated tyrosine kinase. It suppresses VEGF-induced angiogenesis and blocks the induction of LTPGABA-A.
|
-
- HY-107018
-
|
AR-A 2
AR-A 000002
|
5-HT Receptor
|
Neurological Disease
|
|
AR-A 2 is a selective 5-HT1B receptor antagonist, with high affinity to guinea pig cortex 5HT1B/1D and recombinant guinea pig 5-HT1B receptors (Ki=0.24 and 0.47 nM) and with 10-fold lower affinity to guinea pig 5-HT1D receptor (Ki, 5 nM), and shows an EC50 of 4.5 nM for the guinea pig 5-HT1B receptor; AR-A 2 can be used in the research of depression and anxiety.
|
-
- HY-50877
-
-
- HY-131179
-
|
Influenza A virus-IN-1
|
Influenza Virus
|
Infection
|
|
Influenza A virus-IN-1 is a dihydropyrrolidones derivative and is a potent inhibitor against wide subtypes of influenza A virus (IAV) with IC50 values from 3.11 μM to 7.13 μM. Influenza A virus-IN-1 efficiently inhibits replication of IAV, up-regulates the expression of key antiviral cytokines IFN-β and antiviral protein MxA.
|
-
- HY-100155
-
|
4-IBP
|
Sigma Receptor
|
Cancer
|
|
4-IBP is a selective σ1 agonist with a high level of affinity for the σ1 receptor (Ki = 1.7 nM) and a moderate affinity for the σ2 receptor (Ki = 25.2 nM) .
|
-
- HY-133629
-
|
1,1,1,3-Tetrachloroacetone
|
Others
|
Others
|
|
1,1,1,3-Tetrachloroacetone is a halogenated ozone-chlorine and ozone chloramine disinfection byproducts (DBPs) at elevated bromide levels when chlorine or chloramine is used as a secondary disinfectant.
|
-
- HY-B0664
-
|
Ciprofibrate
Win35833
|
PPAR
|
Metabolic Disease
|
|
Ciprofibrate (Win35833) is a potent peroxisome proliferator and increases the phosphorylation level of the PPARalpha. Ciprofibrate acts as an orally active hypolipidaemic agent and can be used for the research of primary hyperlipidaemias.
|
-
- HY-13036
-
|
(Rac)-IBT6A
|
Btk
|
Cancer
|
|
(Rac)-IBT6A is a racemate of IBT6A. IBT6A is an impurity of Ibrutinib. IBT6A can be used in synthesis of IBT6A Ibrutinib dimer and IBT6A adduct. Ibrutinib is a selective, irreversible Btk inhibitor with an IC50 of 0.5 nM.
|
-
- HY-122909
-
-
- HY-13470
-
-
- HY-10985
-
|
Marizomib
Salinosporamide A; NPI-0052
|
Proteasome
|
Cancer
|
|
Marizomib (Salinosporamide A) is a second-generation, irreversible, brain-penetrant, pan-proteasome inhibitor. Marizomib inhibits the CT-L (β5), CT-T-laspase-like (C-L, β1) and trypsin-like (T-L, β2) activities of the 20S proteasome (IC50=3.5, 28, and 430 nM, respectively).
|
-
- HY-13235
-
-
- HY-N0204
-
|
Pulchinenoside A
Anemoside A3
|
Others
|
Others
|
|
Pulchinenoside A is a natural triterpenoid saponin that enhances synaptic plasticity in the adult mouse hippocampus and facilitates spatial memory in adult mice.
|
-
- HY-N0476
-
|
Wilforlide A
Regelide; Abruslactone A
|
Others
|
Inflammation/Immunology
|
|
Wilforlide A is a bioactive triterpene isolated from Tripterygium wilfordii Hook f. Wilforlide A has anti-inflammatory and immune suppressive effects.
|
-
- HY-N0123
-
|
Aloin
Aloin-A; Barbaloin-A
|
Others
|
Cancer
|
|
Aloin(Aloin-A; Barbaloin-A) is a natural antitumor anthraquinone glycoside with iron chelating and non-atherogenic activities.
|
-
- HY-N2995
-
|
Poricoic acid A
Poricoic acid A(F)
|
Others
|
Cancer
|
|
Poricoic acid A, isolated from Poria cocos, possesses anti-tumor activity. Poricoic acid A enhances melatonin inhibition of AKI-to-CKD transition by regulating Gas6/AxlNFκB/Nrf2 axis.
|
-
- HY-133556
-
|
IQZ23
|
AMPK
|
Metabolic Disease
|
|
IQZ23 inhibits adipocyte differentiation via AMPK pathway activation. IQZ23 exerts a high efficacy in decreasing the triglyceride level (EC50=0.033 μM) in 3T3-L1 adipocytes. IQZ23 could be used for the research of obesity and related metabolic disorders.
|
-
- HY-112316A
-
|
(R)-BAY1238097
|
Epigenetic Reader Domain
|
Cancer
|
|
(R)-BAY1238097 is the R-isomer with lower activity of BAY1238097. BAY1238097 is a potent and selective inhibitor of BET binding to histones and has strong anti-proliferative activity in different AML (acute myeloid leukemia) and MM (multiple myeloma) models through down-regulation of c-Myc levels and its downstream transcriptome.
|
-
- HY-A0060
-
|
Malotilate
NKK 105
|
Lipoxygenase
|
Cancer
|
|
Malotilate (NKK 105), an orally active hepatotropic agent and an anti-fibrotic substance, selectively inhibits the 5-lipoxygenase (5-LOX) (IC50=4.7 μM). Malotilate prevents the development of hepatocytic injury in alcohol-pyrazole hepatitis by decreasing hepatic acetaldehyde levels and preventing the retention of transferrin in the hepatocytes.
|
-
- HY-112569
-
-
- HY-U00387
-
-
- HY-78727
-
-
- HY-N0801
-
|
Polygalacic acid
|
MMP
AChE
|
Inflammation/Immunology
Neurological Disease
|
|
Polygalacic acid, is a triterpene, isolated from the root of Polygala tenuifolia Willd. Polygalacic acid inhibits MMP expression. Polygalacic acid may have a therapeutic effect in Osteoarthritis (OA) treatment .
Polygalacic acid exerts a significant neuroprotective effect on cognitive impairment, PA improves cholinergic system reactivity by inhibiting acetylcholinesterase (AChE) activity, increasing choline acetyltransferase (ChAT) activity, and elevating levels of acetylcholine (Ach) in the hippocampus and frontal cortex.
|
-
- HY-N0603
-
-
- HY-19828
-
|
Herboxidiene
GEX1A
|
DNA/RNA Synthesis
|
Cancer
|
|
Herboxidiene (GEX1A) is a potent phytotoxic polyketide from Streptomyces sp. A7847 with a diverse range of activities, including herbicidal, anti-cholesterol, anti-tumor effects. Herboxidiene inhibits the pre-mRNA splicing process by binding to spliceosome-associated protein (SAP) 155, a subunit of SF3b, in the splicesome.
|
-
- HY-P1184A
-
-
- HY-N4195
-
|
Resveratroloside
trans-Resveratrol 4'-O-β-D-glucopyranoside
|
Glucosidase
|
Metabolic Disease
Cardiovascular Disease
|
|
Resveratroloside is a competitive inhibitior of α-glucosidase with an IC50 of 22.9 μM. Resveratroloside has the ability to regulate PBG (postprandial blood glucose) levels. Resveratroloside exhibits cardioprotective effect.
|
-
- HY-113303
-
-
- HY-13863
-
|
Hydroxy-Dynasore
Dyngo-4a
|
Dynamin
|
Neurological Disease
|
|
Hydroxy Dynasore (Dyngo-4a), a structural analog of Dynasore (HY-15304), is an potency improved, low cytotoxicity and non‐specific binding dynamin inhibitor with IC50 values of 0.38 μM and 2.3 μM for brain dynamin I and recombinant rat dynamin II, respectively. Hydroxy Dynasore inhibits dynamin‐dependent endocytosis of transferrin with an IC50 of 5.7 μM in vitro.
|
-
- HY-117391
-
-
- HY-12143
-
-
- HY-15403
-
-
- HY-15403A
-
-
- HY-113402A
-
|
Gamma-glutamylcysteine TFA
γ-Glutamylcysteine TFA
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Gamma-glutamylcysteine (γ-Glutamylcysteine) TFA, an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine TFA also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β). Gamma-glutamylcysteine TFA attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes.
|
-
- HY-12993
-
|
RSV604
A-60444
|
RSV
|
Infection
|
|
RSV604 (A-60444) is an inhibitor of respiratory syncytial virus (RSV) replication. RSV604 targets the nucleocapsid protein, with a Kd of 1.6 μM. RSV604 displays submicromolar activity against numerous clinical isolates of both the A and B subtypes of RSV (average EC50s=0.8 μM).
|
-
- HY-106410A
-
|
Zabofloxacin hydrochloride
DW-224a
|
Bacterial
Topoisomerase
|
Infection
|
|
Zabofloxacin hydrochloride (DW-224a) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin hydrochloride has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin hydrochloride is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
|
-
- HY-133987
-
|
AP-1/NF-κB activation inhibitor 1
|
NF-κB
|
Inflammation/Immunology
|
|
AP-1/NF-κB activation inhibitor 1 is a potent AP-1 and NF-κB mediated transcriptional activation inhibitor (IC50=1 μM), without blocking basal transcription driven by the β-actin promoter. AP-1/NF-κB activation inhibitor 1 has a similar inhibitory effect on the production of IL-2 and IL-8 levels in stimulated cells.
|
-
- HY-13646A
-
-
- HY-13646
-
-
- HY-70044
-
|
GSK-1070916
GSK-1070916A
|
Aurora Kinase
Apoptosis
|
Cancer
|
|
GSK-1070916 is a potent and selective ATP-competitive inhibitor of aurora B and aurora C with Kis of 0.38 and 1.5 nM, respectively, and is >250- fold selective over Aurora A.
|
-
- HY-15891A
-
-
- HY-N1356
-
|
Reticuline
|
JAK
STAT
NF-κB
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Reticuline, isolated from Litsea cubeba, shows anti-inflammatory effects through JAK2/STAT3 and NF-κB signaling pathways. Reticuline inhibits mRNA expressions of TNF-α, and IL-6 and reduces the phosphorylation levels of JAK2 and STAT3. Reticuline exhibits cardiovascular effects.
|
-
- HY-112179
-
|
GSK180
|
Others
|
Inflammation/Immunology
|
|
GSK180 is a selective, competitive, and potent inhibitor of kynurenine-3-monooxygenase (KMO), a key enzyme of tryptophan metabolism (IC50, ~6 nM), but shows negligible activity against other enzymes on the tryptophan pathway. GSK180 rapidly changes levels of kynurenine pathway metabolites, and acts as a useful tool to probe the therapeutic potential of KMO inhibition.
|
-
- HY-114395A
-
|
(R)-NVS-ZP7-4
|
Others
|
Inflammation/Immunology
|
|
(R)-NVS-ZP7-4 is the R-isomer of NVS-ZP7-4. NVS-ZP7-4 is a Zinc transporter SLC39A7 (ZIP7) inhibitor that is also the first reported chemical tool to probe the impact of modulating ER zinc levels and investigate ZIP7 as a novel druggable node in the Notch pathway.
|
-
- HY-114286A
-
|
PXS-5153A monohydrochloride
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
PXS-5153A monohydrochloride is a potent, selective, orally active and fast-acting lysyl oxidase like 2/3 enzymatic (LOXL2/LOXL3) inhibitor, with an IC50 of <40 nM for LOXL2 across all mammalian species and an IC50 of 63 nM for human LOXL3. PXS-5153A monohydrochloride could reduce crosslinks and ameliorates fibrosis.
|
-
- HY-133625
-
|
1,1-Dibromo-3-chloroacetone
|
Others
|
Others
|
|
1,1-Dibromo-3-chloroacetone is a halogenated ozone-chlorine and ozone chloramine disinfection byproducts (DBPs) at elevated bromide levels when chlorine or chloramine is used as a secondary disinfectant.
|
-
- HY-B0360
-
-
- HY-N0268
-
|
Irisflorentin
|
NO Synthase
|
Inflammation/Immunology
|
|
Irisflorentin, a naturally occurring isoflavone, is an abundant active constituent in Rhizoma Belamcandae. Irisflorentin markedly reduces the transcriptional and translational levels of inducible nitric oxide synthase (iNOS) as well as the production of NO. Anti-inflammatory activity.
|
-
- HY-B0442
-
|
Vardenafil
|
Phosphodiesterase (PDE)
|
Endocrinology
|
|
Vardenafil is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil can be used for the research of erectile dysfunction.
|
-
- HY-B0442A
-
|
Vardenafil hydrochloride
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Vardenafil hydrochloride is a selective, orally active, potent inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows selectivity over PDE1 (180 nM), PDE6 (11 nM), PDE2, PDE3, and PDE4 (>1000 nM). Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil hydrochloride can be used for the research of erectile dysfunction.
|
-
- HY-112131
-
-
- HY-B0381B
-
-
- HY-131447
-
|
KY19382
A3051
|
GSK-3
|
Metabolic Disease
|
|
KY19382 is a potent and orally active dual inhibitor of CXXC5-DVL and GSK3β, with IC50s of 19 and 10 nM, respectively. KY19382 activates Wnt/β-catenin signaling through inhibitory effects on both CXXC5-DVL interaction and GSK3β activity. KY19382 can be used for the research of high fat diet (HFD) induced metabolic diseases.
|
-
- HY-133628
-
|
1,1,3-Tribromo-3-chloroacetone
|
Others
|
Others
|
|
1,1,3-Tribromo-3-chloroacetone is a halogenated ozone-chlorine and ozone chloramine disinfection byproducts (DBPs) at elevated bromide levels when chlorine or chloramine is used as a secondary disinfectant.
|
-
- HY-B1057
-
|
Nefopam hydrochloride
Fenazoxine hydrochloride
|
β-catenin
|
Neurological Disease
|
|
Nefopam hydrochloride (Fenazoxine hydrochloride) is a centrally-acting but non-opioid analgesic drug, for the relief of moderate to severe pain. Nefopam hydrochloride targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.
|
-
- HY-133626
-
|
1,1-Dibromo-3,3-dichloroacetone
|
Others
|
Others
|
|
1,1-Dibromo-3,3-dichloroacetone is a halogenated ozone-chlorine and ozone chloramine disinfection byproducts (DBPs) at elevated bromide levels when chlorine or chloramine is used as a secondary disinfectant.
|
-
- HY-N2429
-
|
Sphondin
|
COX
|
Inflammation/Immunology
|
|
Sphondin, isolated from Heracleum laciniatum, possesses an inhibitory effect on IL-1β-induced increase in the level of COX-2 protein and PGE2 release in A549 cells.
|
-
- HY-133627
-
|
1,3-Dibromo-1,3-dichloroacetone
|
Others
|
Others
|
|
1,3-Dibromo-1,3-dichloroacetone is a halogenated ozone-chlorine and ozone chloramine disinfection byproducts (DBPs) at elevated bromide levels when chlorine or chloramine is used as a secondary disinfectant.
|
-
- HY-125741
-
|
GW768505A free base
|
VEGFR
|
Cancer
|
|
GW768505A free base is a potent dual inhibitor of VEGFR2 (KDR) and Tie-2, with a pIC50 of 7.81 for VEGFR2. GW768505A free base has anti-angiogenic activity。
|
-
- HY-15881
-
|
TCS JNK 5a
JNK Inhibitor IX
|
JNK
Apoptosis
|
Cancer
|
|
TCS JNK 5a is a potent JNK3 inhibitor with a pIC50 of 6.7. TCS JNK 5a also inhibits JNK2 with a pIC50 of 6.5.
|
-
- HY-N0853A
-
-
- HY-129707
-
|
AMG 837 hemicalcium
|
GPR40
|
Metabolic Disease
|
|
AMG 837 hemicalcium is a potent, orally bioavailable and partial agonist of GPR40/FFA1, inhibits specific [ 3H]AMG 837 binding at the human FFA1 receptor with a pIC50 of 8.13. AMG 837 hemicalcium could enhance insulin secretion and lower glucose levels in rodents.
|
-
- HY-102078
-
|
ZINC69391
|
Ras
Apoptosis
|
Cancer
|
|
ZINC69391, a specific Rac1 inhibitor, interferes with Rac1-GEF interaction by masking Trp56 residue on Rac1 surface. ZINC69391 interferes with the interaction of Rac1 with Dock180 and reduces Rac1-GTP levels. ZINC69391 induces apoptosis, and shows antiproliferative and antimetastatic effects.
|
-
- 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-100360A
-
|
MS049 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
MS049 dihydrochloride is a potent, selective, and cell-active dual inhibitor of PRMT4 and PRMT6 with IC50s of 34 nM and 43 nM, respectively. MS049 dihydrochloride reduces levels of Med12me2a and H3R2me2a in HEK293 cells. MS049 dihydrochloride is not toxic and do not affect the growth of HEK293 cells.
|
-
- HY-N0875
-
-
- HY-U00185
-
-
- HY-N5120
-
|
Dihydrowithaferin A
2,3-Dihydrowithaferin A
|
AChE
|
Cancer
|
|
Dihydrowithaferin A (2, 3-dihydrowithaferin A) is a withanolide isolated from Withania somnifera. Dihydrowithaferin A is active against acetylcholinesterase (AChE).
|
-
- HY-N0567
-
-
- HY-136466
-
|
A2ti-2
|
Virus Protease
|
Infection
|
|
A2ti-2 is a selective and low-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 230 μM. A2ti-2 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-2 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-136465
-
|
A2ti-1
|
Virus Protease
|
Infection
|
|
A2ti-1 is a selective and high-affinity annexin A2/S100A10 heterotetramer (A2t) inhibitor with an IC50 of 24 μM. A2ti-1 specifically disrupts the protein-protein interaction (PPI) between A2 and S100A10. A2ti-1 prevents human papillomavirus type 16 (HPV16) infection.
|
-
- HY-B0492A
-
-
- HY-17448
-
-
- HY-B0035
-
|
Sulfamethazine
Sulfadimidine; Sulfadimerazine
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamethazine (Sulfadimidine) is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections). In China and the European Commission, the maximum residue level for Sulfamethazine in animal product is set at 100 µg/kg.
|
-
- HY-B0035A
-
|
Sulfamethazine sodium
Sulfadimidine sodium; Sulfadimerazine sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Sulfamethazine sodium (Sulfadimidine sodium) is an antimicrobial that is widely used to treat and prevent various animal diseases (such as gastrointestinal and respiratory tract infections). In China and the European Commission, the maximum residue level for Sulfamethazine sodium in animal product is set at 100 µg/kg.
|
-
- HY-B1057S2
-
|
Nefopam D3
Fenazoxine D3
|
β-catenin
|
Neurological Disease
|
|
Nefopam D3 (Fenazoxine D3) is a deuterium labeled Nefopam (Fenazoxine). Nefopam is a centrally-acting but non-opioid analgesic drug, and Nefopam targets β-catenin protein level in mesenchymal cells.
|
-
- HY-P1333
-
|
Dynorphin A
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-N2025
-
|
Oroxin A
|
PARP
Glucosidase
|
Metabolic Disease
|
|
Oroxin A is the major component of an ethanol-water Oroxylum indicum (L.) Kurz (Bignoniaceae) seed extract (OISE), activates peroxisome proliferator-activated receptor γ (PPARγ) by docking into the PPARγ protein ligand-binding domain. Oroxin A exhibits an inhibitory activity against α-glucosidase and an antioxidant capacity. Oroxin A exerts anti-breast cancer effects by inducing ER stress-mediated senescence.
|
-
- HY-N2420
-
|
Flavokawain A
|
Apoptosis
|
Cancer
|
|
Flavokawain A, a proming anticarcinogenic agent, is a chalcone from kava extract with anti-tumor activity. Flavokawain A induces cell apoptosis by involvement of Bax protein-dependent and mitochondria-dependent apoptotic pathway. Flavokawain A has the potential for the study of bladder cancer.
|
-
- HY-N7496
-
|
Odoroside A
|
Apoptosis
|
Cancer
|
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-N0239
-
-
- HY-N3051
-
-
- HY-50697
-
-
- HY-130993
-
|
Isatropolone A
|
Parasite
|
Infection
|
|
Isatropolone A, a natural product containing a 1,5-diketone moiety, is reisolated from Streptomyces Gö66. Isatropolone A shows potent activity against Leishmania donovani with an IC50 of 0.5 μM.
|
-
- HY-N7621
-
|
Bryonamide A
|
Others
|
Others
|
|
Bryonamide A is a natural compound isolated from red algae Bostrychia radicans (Rhodomelaceae).
|
-
- HY-N2416
-
|
Taccalonolide A
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Taccalonolide A is a microtubule stabilizer, which is a steroid isolated from Tacca chantrieri, with cytotoxic and antimalarial activities. Taccalonolide A causes G2-M accumulation, Bcl-2 phosphorylation and initiation of apoptosis. Taccalonolide A is effective in vitro against cell lines that overexpress P-glycoprotein (Pgp) and multidrug resistance protein 7 (MRP7), with an IC50 of 622 nM for SK-OV-3 cells.
|
-
- HY-100080
-
|
A-887826
|
Sodium Channel
|
Neurological Disease
|
|
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo.
|
-
- HY-N7680
-
|
Neopuerarin A
|
Others
|
Metabolic Disease
|
|
Neopuerarin A is an isoflavones isolated from the water extraction of the dried roots of Pueraria lobata (Willd.). Neopuerarin A shows significant hepatoprotective effect.
|
-
- HY-N2606
-
-
- HY-N6065
-
|
Praeruptorin A
|
NF-κB
|
Inflammation/Immunology
|
|
Praeruptorin A is a main bioactive constituent of Peucedanum praeruptorum (also known as Bai-Hua Qian Hu). Praeruptorin A exerts anti-inflammatory effects in vitro through inhibition of NF-κB activation.
|
-
- HY-N7028
-
|
Withanolide A
|
Others
|
Neurological Disease
|
|
Withanolide A, isolated from the indian herbal drug Ashwagandha (root of Withania somnifera), could regenerate neurites and reconstruct synapses in severely damaged neurons.
|
-
- HY-N0318
-
-
- HY-131098
-
|
Enduracidin A
|
Antibiotic
|
Infection
|
|
Enduracidin A is a major component of Enduracidin. Enduracidin is a polypeptide antibiotic produced by Streptomyces fungicides.
|
-
- HY-N3201
-
-
- HY-N6820
-
-
- HY-N0581
-
-
- HY-N0257
-
-
- HY-11079
-
-
- HY-P1539
-
-
- HY-N7679
-
-
- HY-N0659
-
-
- HY-113673
-
|
A-935142
|
Potassium Channel
|
Cardiovascular Disease
|
|
A-935142 is a human ether-a-go-go-related gene (hERG, Kv 11.1) channel activator. A-935142 enhances hERG current in a complex manner by facilitation of activation, reduction of inactivation, and slowing of deactivation, and abbreviates atrial and ventricular repolarization.
|
-
- HY-N5104
-
-
- HY-116941
-
|
A-381393
|
Dopamine Receptor
|
Neurological Disease
|
|
A-381393 is a potent, selective, brain penetrate dopamine D4 receptor antagonist, with Kis of 1.5, 1.9 and 1.6 nM for human dopamine D4.4, D4.2, and D4.7 receptor, respectively, >2700-fold selectivity over D1, D2, D3 and D5 dopamine receptors. A-381393 shows moderate affinity for 5-HT2A (Ki, 370 nM).
|
-
- HY-N6992
-
-
- HY-N1508
-
|
Ecliptasaponin A
|
Others
|
Inflammation/Immunology
|
|
Ecliptasaponin A , a pentacyclic triterpenoid saponin, is one of major compounds separated from Eclipta prostrate. Eclipta prostrate is considered as a nourishing herbal medicine with pleiotropic effects, including anti-inflammatory, hepatoprotective, antioxidant, and immunomodulatory.
|
-
- HY-N2175
-
-
- HY-N2440
-
-
- HY-N0081
-
|
(±)-Praeruptorin A
|
Calcium Channel
|
Infection
|
|
(±)-Praeruptorin A is the di-esterified product of cis-khellactone (CKL) and the major active ingredient in Peucedani Radix which consists of the dried roots of Peucedanum praeruptorumDunn (Apiaceae). (±)-Praeruptorin A has been widely employed as one of the famous traditional Chinese medicines (TCMs) for the treatment of cough with thick sputum and dyspnea, nonproductive cough and upper respiratory infections for centuries in China. (±)-Praeruptorin A has dramatically therapeutic effects on hypertension mainly through acting as a Ca 2+-influx blocker.
|
-
- HY-P2324
-
|
Gramicidin A
|
Bacterial
HIF/HIF Prolyl-Hydroxylase
|
Infection
|
|
Gramicidin A is a peptide component of gramicidin, an antibiotic mixture originally isolated from B. brevis. Gramicidin A is a highly hydrophobic channel-forming ionophore that forms channels in model membranes that are permeable to monovalent cations. Gramicidin A induces degradation of hypoxia inducible factor 1 α (HIF-1α).
|
-
- HY-N2626
-
|
Epimedoside A
|
Others
|
Infection
|
|
Epimedoside A is a flavonoid isolated from the roots of Epimedium wushanense. Epimedoside A exhibits significant antioxidant activity in vitro.
|
-
- HY-N2281
-
-
- HY-N5057
-
|
Przewalskinic acid A
|
Others
|
Cardiovascular Disease
|
|
Przewalskinic acid A is a rare, water-soluble phenolic acid thus far only found in the Salvia przewalskii Maxim herb. Phenolic acids show potent antioxidant activities and potential effects in protecting against brain and heart damage caused by ischemia reperfusion.
|
-
- HY-N0237
-
-
- HY-N5087
-
-
- HY-N1472
-
|
Levistolide A
|
Apoptosis
|
Cancer
|
|
Levistolide A (LA), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is used for treating cancer. Levistolide A can induce apoptosis via ROS-mediated ER stress pathway.
|
-
- HY-N1371
-
-
- HY-N6930
-
-
- HY-N0028
-
-
- HY-P1581
-
|
Ceratotoxin A
|
Bacterial
|
Infection
|
|
Ceratotoxin A, a 29-residue peptide isolated from the accessory gland secretion fluid, with strong anti-bacterial activity.
|
-
- HY-N4210
-
|
Yadanziolide A
|
Others
|
Cancer
Infection
|
|
Yadanziolide A, isolated from the cultivated dry seeds of Brucea javanica, has strong antiviral activities with IC50 of 5.5 μM against tobacco mosaic virus. Yadanziolide A shows significant antitumor effects.
|
-
- HY-108463
-
|
A-967079
|
TRP Channel
|
Inflammation/Immunology
|
|
A-967079 is a selective TRPA1 receptor antagonist with IC50s of 67 nM and 289 nM at human and rat TRPA1 receptors, respectively, and has good penetration into the CNS.
|
-
- HY-N2155
-
-
- HY-131058
-
|
Muscotoxin A
|
ADC Cytotoxin
|
Cancer
|
|
Muscotoxin A is an ADC cytotoxin. Muscotoxin A is a cytotoxic lipopeptide that permeabilizes mammalian cell membranes and induces necrotic cell death.
|
-
- HY-N2331
-
-
- HY-50662
-
-
- HY-N6776
-
|
Penitrem A
|
Potassium Channel
|
Cancer
Neurological Disease
|
|
Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals.
|
-
- HY-N4084
-
|
Thonningianin A
|
Apoptosis
|
Cancer
|
|
Thonningianin A, an ellagitannin, is isolated from the methanolic extract of the African medicinal herb, Thonningia sanguinea. The antioxidant properties of Th A involve radical scavenging, anti-superoxide formation and metal chelation. Anti-cancer activities.
|
-
- HY-15568A
-
|
A-317491 sodium salt hydrate
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A-317491 sodium salt hydrate is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 sodium salt hydrate is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 sodium salt hydrate reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
|
-
- HY-N2637
-
-
- HY-N2109
-
|
Macranthoidin A
|
Others
|
Metabolic Disease
|
|
Macranthoidin A is an orally active saponin from Flos Lonicerae. Macranthoidin A possess protection effects on hepatic injury caused by Acetaminophen, Cd, and CCl4, and conspicuous depressant effects on swelling of ear croton oil.
|
-
- HY-N4236
-
|
Angelol A
|
Others
|
Others
|
|
Angelol A is a coumarin isolated from the roots of Angelica pubescens f. biserrata, which is passive diffusion as the dominating process in Caco-2 cell monolayer model.
|
-
- HY-N2249
-
-
- HY-N2524
-
-
- HY-108421
-
|
Xinjiachalcone A
|
Bacterial
|
Infection
|
|
Xinjiachalcone A is an active principle of Glycyrrhiza inflata Batalin. Xinjiachalcone A shows both a low MIC and a strong bactericidal activity against H. pylori, with MIC values ranged from 12.5 to 50 µM for seventeen H. pylori strains.
|
-
- HY-133168
-
|
Englerin A
|
TRP Channel
|
Cancer
|
|
Englerin A is a potent and selective activator of TRPC4 and TRPC5 channels, with EC50s of 11.2 and 7.6 nM, respectively. Englerin A can induce renal carcinoma cells death by elevated Ca 2+ influx and Ca 2+ cell overload.
|
-
- HY-59201A
-
|
A-582941 dihydrochloride
|
nAChR
5-HT Receptor
|
Neurological Disease
|
|
A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research.
|
-
- HY-N0743
-
|
Senkyunolide A
|
Others
|
Cancer
|
|
Senkyunolide A, isolated from Ligusticum chuanxiong Hort, has cytoprotective and antiproliferative activities. Anti-tumor activity.
|
-
- HY-N7499
-
-
- HY-136293
-
|
Mechercharmycin A
|
Apoptosis
|
Cancer
|
|
Mechercharmycin A is a cytotoxic substance isolated from marine-derived Thermoactinomyces sp. YM3-251. Mechercharmycin A exhibits relatively strong antitumor activity.
|
-
- HY-N6076
-
|
Tenuifoliside A
|
ERK
|
Neurological Disease
|
|
Tenuifoliside A is isolated from Polygala tenuifolia, has anti-apoptotic and antidepressant-like effects. Tenuifoliside A exhibits its neneurotrophic effects and promotes cell proliferation through the ERK/CREB/BDNF signal pathway in C6 cells.
|
-
- HY-N4316
-
-
- HY-N4257
-
-
- HY-108013
-
-
- HY-125531
-
|
Dactylorhin A
|
Others
|
Others
|
|
Dactylorhin A, a succinate derivative ester, is isolated from rhizomes of Gymnadenia conopsea. Dactylorhin A exhibits moderate inhibitory effects on NO production effects in RAW 264.7 macrophage cells.
|
-
- HY-N2441
-
-
- HY-N2111
-
-
- HY-N2505
-
-
- HY-126252
-
|
A-9758
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation.
|
-
- 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-P2123
-
|
Colistin A
|
Bacterial
Antibiotic
|
Infection
|
|
Colistin A is a major component of Colistin. Colistin is a polymyxin antibiotic and can be used to combat infections caused by problematic gram-negative bacteria.
|
-
- HY-128851
-
|
Coenzyme A
|
Endogenous Metabolite
|
Cancer
Neurological Disease
|
|
Coenzyme A is is an obligatory cofactor in all living cells synthesised from pantothenate (Vitamin B5), adenosine triphosphate (ATP) and cysteine. Covalent binding of Coenzyme A to Peroxiredoxin 5 (Prdx5) results in complete inhibition of its peroxidase activity, which is reversed by reduction with DTT.Coenzyme A and its thioester derivatives are key players in major catabolic and anabolic pathways and the regulation of gene expression. Many human pathologies, including cancer, diabetes and neurodegeneration, have been associated with abnormal biosynthesis and homeostasis of CoA and its derivatives.
|
-
- HY-12428
-
-
- HY-N0632
-
|
Esculentoside A
|
COX
NF-κB
|
Inflammation/Immunology
|
|
Esculentoside A (EsA), a kind of triterpene saponin isolated from roots of Phytolacca esculenta.
Esculentoside A (EsA) possesses anti-inflammatory activity in acute and chronic experimental models, has selective inhibitory activity towards cyclooxygenase-2 (COX-2).
Esculentoside A (EsA) suppresses inflammatory responses in LPS-induced acute lung injury (ALI) through inhibition of the nuclear factor kappa B (NF-ΚB) and mitogen activated protein kinase (MAPK) signaling pathways.
|
-
- HY-12761
-
-
- HY-N7644
-
|
Comanthoside A
|
Others
|
Others
|
|
Comanthoside A is a plant derived natural flavonoid glycoside isolated from the leaves of Comanthosphace japonica. Comanthoside A also serves as a key intermediate for the synthesis of Comanthoside B and Linaroside.
|
-
- HY-N4278
-
|
Huangjiangsu A
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Huangjiangsu A, pseudoprotodioscin, methyl protobioside, protodioscin, and protodeltonin, isolated from D. villosa.
Huangjiangsu A has hepatoprotective potential against H2O2-induced cytotoxicity and ROS generation and could be promising as potential therapeutic agents for liver diseases.
|
-
- HY-131448
-
|
A3334
|
Others
|
Metabolic Disease
|
|
A3051 is a potent and orally active inhibtor of CXXC5-DVL extracted from patent WO2020079569, has an IC50 of 63.06 nM. A3334 can be used for the research of high fat diet (HFD)-induced and methionine-choline deficient diet (MCD)-induced phenotypes such as obesity, diabetes, and NASH.
|
-
- HY-U00225
-
-
- HY-126708
-
|
Luisol A
|
ADC Cytotoxin
|
Infection
|
|
Luisol A, an aromatic tetraol, is a major metabolite of an estuarine marine actinomycete of the genus Streptomyces. Luisol A, anthraquinone antibiotic analog, is an ADC Cytotoxin.
|
-
- HY-N4019
-
|
Maohuoside A
|
Others
|
Metabolic Disease
|
|
Maohuoside A, a single compound isolated from the E. koreanum that potently promotes osteogenesis. Maohuoside A enhances the osteogenesis of bone marrow-derived mesenchymal stem cells via bone morphogenetic protein (BMP) and MAPK signaling pathways.
|
-
- HY-18260
-
|
Bisphenol A
|
Endogenous Metabolite
|
Endocrinology
|
|
Bisphenol A is a phenolic, organic synthetic compound widely used in the production of polycarbonate plastics and epoxy resins. Bisphenol A is a reproductive, developmental, and systemic toxicant, often classified as an endocrine-disrupting compound (EDC). Bisphenol A is associated with many diseases, including cardiovascular diseases, respiratory diseases, diabetes, kidney diseases, obesity, and reproductivedisorders.
|
-
- HY-100483
-
|
A-804598
|
P2X Receptor
|
Cancer
|
|
A-804598 is a CNS penetrant, competitive and selective P2X7 receptor antagonist with IC50s of 9 nM, 10 nM and 11 nM for mouse, rat and human P2X7 receptors, respectively.
|
-
- HY-15568
-
|
A-317491
|
P2X Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
A-317491 is a potent, selective and non-nucleotide antagonist of P2X3 and P2X2/3 receptors, with Kis of 22, 22, 9, and 92 nM for hP2X3, rP2X3, hP2X2/3, and rP2X2/3, respectively. A-317491 is highly selective (IC50>10 μM) over other P2 receptors and other neurotransmitter receptors, ion channels, and enzymes. A-317491 reduces inflammatory and neuropathic pain by blocking P2X3 and P2X2/3 receptor-mediated calcium flux.
|
-
- HY-N2017
-
-
- HY-N4318
-
-
- HY-N6593
-
-
- HY-N4223
-
|
Sibirioside A
|
Others
|
Metabolic Disease
|
|
Sibirioside A is a phenylpropanoid glycoside isolated from Scrophulariae Radix. Sibirioside A has the potential for the treatment of diabetes.
|
-
- HY-N4274
-
-
- HY-U00142
-
|
A-802715
|
Others
|
Cancer
|
|
A802715 is a methylxanthine derivative. A802715 has a TD50 (toxic dose of 50%) of 0.9-1.1 mM.
|
-
- HY-N6994
-
|
Isoasatone A
|
Others
|
Infection
|
|
Isoasatone A is a natural product isolated from the plant Heterotropa takaoi M., with anti-insect activity. Isoasatone A againsts S. litura by acting on cytochrome P450 monoxygenases and glutathione transferases.
|
-
- HY-P1629
-
|
Temporin A
|
Bacterial
Fungal
Antibiotic
|
Infection
|
|
Temporin A is a short alpha-helical antimicrobial peptide isolated from the skin of the frog Rana temporaria. Temporin A is effective against a broad spectrum of Gram-positive bacteria. Temporin A interacts directly with the cell membrane of the microorganism and it is non-toxic to erythrocytes at concentrations that are antimicrobial. Temporin A also has antifungal activities (against yeast-like Candida albicans).
|
-
- HY-N2437
-
-
- HY-N2238
-
|
Dipsanoside A
|
Others
|
Metabolic Disease
|
|
Dipsanoside A is a novel tetrairidoid glucoside from Dipsacus asper. Dipsacus asper Wall., a perennial plant widespread in China, has been used in traditional Chinese medicine for hundreds of years as a tonic for refreshment, as a fissiparism promoter of the osseous cells, and as an embryo security agent, etc.
|
-
- HY-N0246
-
-
- HY-14364
-
-
- HY-N6917
-
-
- HY-N2326
-
|
(±)-Anatoxin A fumarate
|
nAChR
|
Neurological Disease
|
|
(±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
|
-
- HY-131103
-
-
- HY-N7692
-
|
Polyporusterone A
|
Others
|
Others
|
|
Polyporusterone A is a triterpene carboxylic acid isolated from Polyporus umbellatus Fries. Polyporusterone A has inhibitory effect on free radical-induced lysis of red blood cells (hemolysis).
|
-
- HY-P2322
-
|
Iturin A
|
Fungal
|
|
|
IturinA exhibits strong antifungal activity against pathogenic yeast and fungi. Iturin A interacts with the cytoplasmic membrane of the target cell forming ion conducting pores.
|
-
- HY-12149
-
|
A-867744
|
nAChR
Autophagy
|
Neurological Disease
|
|
A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
|
-
- HY-N0673
-
|
Pseudolaric Acid A
|
Fungal
|
Infection
|
|
Pseudolaric Acid A is a diterpene acid isolated from Pseudolarix kaempferi, has antifungal, cytotoxic and antifertile activities.
|
-
- HY-N6997
-
|
Ceratamine A
|
Microtubule/Tubulin
|
Cancer
|
|
Ceratamine A is an antimitotic heterocyclic alkaloid isolated from the marine sponge Pseudoceratina sp., acts as a microtubule-stabilizing agent. Ceratamine A exhibits cytotoxicity against human cancer cell lines.
|
-
- HY-N3163
-
-
- HY-117549
-
|
Ibrolipim
NO-1886
|
Others
|
Cardiovascular Disease
|
|
Ibrolipim (NO-1886) is an orally active lipoprotein lipase (LPL)-promoting agent. Ibrolipim decreases plasma triglycerides, increases high-density lipoprotein cholesterol levels. Ibrolipim has renoprotective and hypolipidemic effects.
|
-
- HY-17473
-
|
Embelin
Embelic acid; Emberine; NSC 91874
|
IAP
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Embelin (Embelic acid), a potent, nonpeptidic XIAP inhibitor (IC50=4.1 μM), inhibits cell growth, induces apoptosis, and activates caspase-9 in prostate cancer cells with high levels of XIAP. Embelin blocks NF-kappaB signaling pathway leading to suppression of NF-kappaB-regulated antiapoptotic and metastatic gene products. Embelin also induces autophagic and apoptotic cell death in human oral squamous cell carcinoma cells.
|
-
- HY-B1639
-
|
Enoximone
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
Cardiovascular Disease
|
|
Enoximone is an inotropic vasodilating agent and a selective and orally active phosphodiesterase III (PDE3) inhibitor with an IC50 of 5.9 μM. Enoximone induces vasodilatation and increases intracellular levels of cAMP by inhibiting cGMP-inhibited PDE. Enoximone also exhibits PDE4 inhibitory effect with an IC50 of 21.1 μM for myocardial PDE4A. Enoximone has the potential for congestive heart failure research and has bronchodilatory, antiasthma and anti-inflammatory effects.
|
-
- HY-112584
-
|
JBSNF-000088
6-Methoxynicotinamide
|
Endogenous Metabolite
|
Metabolic Disease
|
|
JBSNF-000088 (6-Methoxynicotinamide), a analog of nicotinamide (NA), is a potent Nicotinamide N-methyltransferase (NNMT) inhibitor with IC50s of 1.8 µM, 2.8 µM, and 5.0 µM for human NNMT, monkey NNMT and mouse NNMT, respectively. JBSNF-000088 inhibits NNMT activity, reduces MNA levels and drives insulin sensitization, glucose modulation and body weight reduction in animal models of metabolic disease.
|
-
- HY-13807
-
|
UNC0646
|
Histone Methyltransferase
|
Cancer
|
|
UNC0646 is a potent and selective histone methyltransferase G9a inhibitor with an IC50 of 6 nM. UNC0646 is also a potent GLP inhibitor (IC50 <15 nM) and highly selective for G9a/GLP over SETD7, SUV39H2, SETD8 and PRMT3. UNC0646 reduces H3K9me2 levels in MDA-MB-231 cells with an IC50 of 26 nM.
|
-
- HY-15478
-
|
WZ811
|
CXCR
|
Cancer
Endocrinology
|
|
WZ811 is an orally active, highly potent competitive antagonist of CXCR4. WZ811 efficiently inhibits CXCR4/SDF-1 (or CXCL12)-mediated modulation of cAMP levels (EC50=1.2 nM) and SDF-1 induced Matrigel invasion in cells (EC50=5.2 nM).
|
-
- HY-100421
-
|
CPI-455
|
Histone Demethylase
|
Cancer
|
|
CPI-455 is a specific, pan-KDM5 inhibitor with an IC50 of 10 nM for KDM5A. CPI-455 mediates KDM5 inhibition, elevates global levels of H3K4me3, and decreases the number of drug-tolerant persister cancer cells in multiple cancer cell line models treated with standard chemotherapy or targeted agents.
|
-
- HY-N1987
-
|
Cucurbitacin IIb
|
Apoptosis
|
Inflammation/Immunology
|
|
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
|
-
- HY-16589
-
-
- HY-N6732
-
|
K-252a
SF2370; Antibiotic K 252a; Antibiotic SF 2370
|
PKC
PKA
CaMK
Trk Receptor
Autophagy
|
Infection
|
|
K-252a, a staurosporine analog isolated from Nocardiopsis sp. soil fungi, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca 2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene.
|
-
- HY-14247
-
|
Fadrozole hydrochloride
CGS 16949A; (Rac)-FAD286 hydrochloride
|
Aromatase
|
Cancer
|
|
Fadrozole hydrochloride (CGS 16949A) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
|
-
- HY-N6013
-
|
Aloin(mixture of A&B)
|
MMP
Bacterial
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Aloin (mixture of A&B) is anthraquinone derivative isolated from Aloe vera. Aloin (mixture of A&B) has diverse biological activities such as anti-inflammatory, immunity, antidiabetic, antioxidant, antibacterial, antifungal, and antitumor activities. Aloin (mixture of A&B) also an effective inhibitor of stimulated granulocyte matrix metalloproteinases (MMPs).
|
-
- HY-100501
-
|
M2698
MSC2363318A
|
Ribosomal S6 Kinase (RSK)
Akt
|
Cancer
|
|
M2698 (MSC2363318A) is an orally active, ATP competitive, selective p70S6K and Akt dual-inhibitor with IC50s of 1 nM for p70S6K, Akt1 and Akt3. M2698 can cross the blood-brain barrier and has anti-cancer activity.
|
-
- HY-B1071
-
-
- HY-B1071A
-
|
Lasalocid sodium
Lasalocid-A sodium; Ionophore X-537A sodium; Antibiotic X-537A sodium
|
Bacterial
Autophagy
Antibiotic
|
Cancer
Infection
|
|
Lasalocid sodium (Lasalocid-A sodium) treatment led to an increase in cell wall thickness, whilst the quantity and sugar composition of the cell wall remained unchanged in BY-2 cells.
|
-
- HY-14660
-
|
Dabrafenib
GSK2118436A; GSK2118436
|
Raf
|
Cancer
|
|
Dabrafenib (GSK2118436A) is an ATP-competitive inhibitor of Raf with IC50s of 5 nM and 0.6 nM for C-Raf and B-Raf V600E, respectively.
|
-
- HY-104051
-
-
- HY-133246
-
-
- HY-B1209
-
|
Etofylline
7-(β-Hydroxyethyl)theophylline
|
Others
|
Cardiovascular Disease
|
|
Etofylline (7-(β-Hydroxyethyl)theophylline) is a N-7-substituted derivative of Theophylline. Etofylline is a bronchodilator which can be used for the research of asthma. Etofylline is also an anticholesteremic and reduces total cholesterol level in the blood.
|
-
- HY-N2342
-
|
Procyanidin C1
|
Apoptosis
|
Cancer
|
|
Procyanidin C1 is a natural polyphenol, causes DNA damage, cell cycle arrest, and induces apoptosis. Procyanidin C1 decreases the level of Bcl-2, but enhances BAX, caspase 3 and 9 expression in cancer cells.
|
-
- HY-101938
-
-
- HY-B0069
-
-
- HY-14852A
-
|
Tafamidis meglumine
Fx-1006A
|
Others
|
Neurological Disease
|
|
Tafamidis meglumine (Fx-1006A) is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis meglumine inhibits amyloidogenesis.
|
-
- HY-101785
-
-
- HY-B0492
-
-
- HY-131973
-
-
- HY-19487A
-
|
Ribocil B
Ribocil S enantiomer; ent-Ribocil A
|
Bacterial
|
Infection
|
|
Ribocil-B is the active S-isomer of ribocil which can inhibit flavin mononucleotide (FMN) with a KD of 6.6 nM.
|
-
- HY-111174A
-
-
- HY-102026
-
-
- HY-117319
-
-
- HY-17408
-
-
- HY-100764
-
|
YUKA1
|
Histone Demethylase
|
Cancer
|
|
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity.
|
-
- HY-13960
-
-
- HY-W012946
-
-
- HY-N3063
-
|
Pimaric acid
|
Others
|
Cardiovascular Disease
|
|
Pimaric acid is a resin acid that has been found in A. cordata and various pines. Pimaric acid reduces mRNA expression, protein levels, and promoter activity of matrix metalloproteinase-9 (MMP-9) in TNF-α-stimulated human aortic smooth muscle cells (HASMCs).
|
-
- HY-12424
-
|
Zotarolimus
ABT-578; A 179578
|
Others
|
Cancer
Cardiovascular Disease
|
|
Zotarolimus (ABT-578) is a derivative of rapamycin (HY-10219), with anti-proliferative activity. Zotarolimus is an immunosuppressant. Zotarolimus is developed specifically for local delivery from stents for the prevention of coronary artery restenosis.
|
-
- HY-N1913
-
-
- HY-17590
-
-
- HY-13746
-
|
Sardomozide
CGP 48664; SAM-486A
|
Others
|
Cancer
|
|
Sardomozide is an S-adenosylmethionine decarboxylase (SAMDC) inhibitor with an IC50 of 5 nM.
|
-
- HY-B1311
-
-
- HY-18649
-
|
Galidesivir hydrochloride
BCX4430 hydrochloride; Immucillin-A hydrochloride
|
DNA/RNA Synthesis
SARS-CoV
Filovirus
|
Infection
|
|
Galidesivir (BCX4430) hydrochloride, an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir hydrochloride is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir hydrochloride inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
|
-
- HY-18649A
-
|
Galidesivir
BCX4430; Immucillin-A
|
DNA/RNA Synthesis
SARS-CoV
Filovirus
|
Infection
|
|
Galidesivir (BCX4430), an adenosine analog and a direct-acting antiviral agent, disrupts viral RNA-dependent RNA polymerase (RdRp) activity. Galidesivir is active in vitro against many RNA viral pathogens, including the filoviruses and emerging infectious agents such as MERS-CoV, SARS-CoV, and SARS-CoV-2. Galidesivir inhibits some negative-sense RNA viruses with EC50s ranging from ~3 to ~68 μM.
|
-
- 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-100877
-
-
- HY-P1252
-
-
- HY-N7206
-
|
5-O-Methylvisamminol
|
Others
|
Metabolic Disease
|
|
5-O-Methylvisamminol, a (furo) chromone identified in the extract of T. glauca, has a limited occurrence in the plant kingdom. 5-O-Methylvisamminol is useful in (chemical) phylogeny and is a possible excellent chemotaxonomic marker (family and/or subfamily level) for Apiaceae.
|
-
- HY-13768A
-
-
- HY-100900
-
|
ML364
|
Deubiquitinase
|
Cancer
|
|
ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
|
-
- 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-N0619A
-
|
cis-Mulberroside A
Mulberroside D
|
TNF Receptor
Interleukin Related
Tyrosinase
|
Inflammation/Immunology
|
|
cis-Mulberroside A (Mulberroside D) is the cis-isomer of Mulberroside A. Mulberroside A is one of the main bioactive constituent in mulberry (Morus alba L.). Mulberroside A decreases the expressions of TNF-α, IL-1β, and IL-6 and inhibits the activation of NALP3, caspase-1, and NF-κB and the phosphorylation of ERK, JNK, and p38, exhibiting anti-inflammatory and anti-apoptotic effects. Mulberroside A shows inhibitory activity against mushroom tyrosinase with an IC50 of 53.6 μM.
|
-
- 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-15511
-
|
Tyrphostin A9
Tyrphostin 9; Malonoben
|
VEGFR
Influenza Virus
|
Cancer
Infection
|
|
Tyrphostin A9, a PDGFR inhibitor, is a potent inducer of mitochondrial fission. Tyrphostin A9 emerged as the most potent and selective of 51 tyrosine kinase inhibitors tested against the TNF-induced respiratory burst. Tyrphostin A9 has anti-influenza virus activities.
|
-
- HY-P1252A
-
-
- HY-133115
-
|
N-Desmethylnefopam
|
β-catenin
|
Neurological Disease
|
|
N-Desmethylnefopam is the main metabolite of Nefopam. N-Desmethylnefopam is a centrally-acting but non-opioid analgesic agent, for the relief of moderate to severe pain. Nefopam targets β-catenin protein level in mesenchymal cells in-vitro and in-vivo.
|
-
- HY-15439
-
|
(24S)-24,25-Dihydroxyvitamin D3
(24S)-24,25-Dihydroxycholecalciferol
|
VD/VDR
|
Others
|
|
(24S)-24,25-Dihydroxyvitamin D3 ((24S)-24,25-Dihydroxycholecalciferol) is an inactive form of vitamin D3 which undergoes various levels of hydroxylation to form active vitamin D3 analogs.
|
-
- HY-N0582
-
|
Qingyangshengenin B
|
Others
|
Neurological Disease
|
|
Qingyangshengenin B, a C-21 steroidal glycoside isolated from Qingyangshen. Qingyangshengenin B protects against Aβ toxicity, which decreases Aβ deposition by decreasing the expression of Aβ at the mRNA level. Qingyangshengenin B has antiepileptic activity.
|
-
- 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-10895
-
|
SB-334867
SB 334867A
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 (SB 334867A) is an excellent,selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
|
-
- HY-100014
-
|
KDM5A-IN-1
|
Histone Demethylase
|
Cancer
|
|
KDM5A-IN-1 is a potent, orally bioavailable pan-histone lysine demethylases 5 (KDM5) inhibitor with IC50s of 45 nM, 56 nM and 55 nM for KDM5A, KDM5B and KDM5C, respectively, and with an EC50 value of 960 nM for PC9 H3K4Me3. KDM5A-IN-1 is significantly less potent against other KDM5B enzymes (1A, 2B, 3B, 4C, 6A, 7B).
|
-
- HY-N6791
-
|
KT5823
|
PKA
PKC
Bacterial
Apoptosis
Antibiotic
|
Infection
Inflammation/Immunology
|
|
KT5823, a selective the cGMP-dependent protein kinase (PKG) inhibitor with an Ki value of 0.23 μM, it also inhibits PKA and PKC with Ki values of 10 μM and 4 μM, respectively. KT5823 is a staurosporine-related protein kinase inhibitor, increases thyroid-stimulating hormone-induced (Na +/I - symporter) NIS expression, and iodide uptake in thyroid cells. KT5823 arrests cells after the G0/G1 boundary and causes increases in the levels of apoptotic DNA fragmentation.
|
-
- HY-101496
-
|
MT-DADMe-ImmA
MTDIA; Methylthio-DADMe-Immucillin A
|
Others
|
Cancer
|
|
MT-DADMe-ImmA is an inhibitor of human 5'-methylthioadenosine phosphorylase (MTAP) with a Ki of 90 pM.
|
-
- HY-124596
-
|
CD161
NKR-P1A
|
Epigenetic Reader Domain
|
Cancer
|
|
CD161 (NKR-P1A) is a potent, selective and orally bioavailable bromodomain and extra-terminal (BET) bromodomain inhibitor with an IC50s of 28.2 nM and 7.2 nM for BRD4 BD1 and BRD4 BD2, respectively. CD161 has good anticancer activity.
|
-
- HY-128946
-
|
CL2A-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
Inflammation/Immunology
|
|
CL2A-SN-38 is a drug-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody drug conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A is a nonclaevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond.
|
-
- HY-122487
-
|
Troriluzole
BHV-4157
|
Others
|
Neurological Disease
|
|
Troriluzole, a third-generation, tripeptide prodrug of Riluzole (HY-B0211), is an orally active glutamate modulator. Troriluzole reduces synaptic glutamate level and increases the synaptic glutamate absorption. Troriluzole has the potential for Alzheimer disease and generalized anxiety disorder (GAD).
|
-
- HY-N1094
-
|
Verminoside
|
PARP
MDM-2/p53
|
Inflammation/Immunology
|
|
Verminoside is an iridoid isolated from Kigelia africana, exhibits anti-inflammatory and remarkable antioxidant activity with a radical-scavenging activity of 2.5 μg/mL. The genotoxicity of Verminoside on human lymphocytes is associated with elevated levels of PARP-1 and p53 proteins.
|
-
- HY-100581
-
|
CORM-3
|
NF-κB
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
CORM-3, a carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels. CORM-3 reduces NLRP3 inflammasome activation.
|
-
- HY-B0360S
-
-
- HY-135594
-
|
4'-Raloxifene-β-D-glucopyranoside
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
4'-Raloxifene-β-D-glucopyranoside, a metabolite of Raloxifene, is a benzothiophene glucuronidated at the 4' postion. 4'-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 4'-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 4'-Raloxifene-β-D-glucopyranoside, example 5, is extracted from patent US5567820A.
|
-
- HY-135595
-
|
6-Raloxifene-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Drug Metabolite
|
Metabolic Disease
|
|
6-Raloxifene-β-D-glucopyranoside, a derivative of Raloxifene, is a benzothiophene glucuronidated at the 6' postion. 6-Raloxifene-β-D-glucopyranoside is a selective and orally active estrogen receptor antagonist. 6-Raloxifene-β-D-glucopyranoside can be used for inhibiting bone loss and resorption, and lowering lipid levels. 6'-Raloxifene-β-D-glucopyranoside, compound Ia, is extracted from patent US5567820A.
|
-
- HY-N6682
-
|
Cytochalasin D
Zygosporin A; NSC 209835
|
Arp2/3 Complex
Bacterial
Antibiotic
YAP
|
Infection
|
|
Cytochalasin D (Zygosporin A; NSC 209835) is a potent and cell-permeable inhibitor of actin polymerization derived from fungus, inhibits the G-actin–cofilin interaction by binding to G-actin. Cytochalasin D (Zygosporin A; NSC 209835) also inhibits the binding of cofilin to F-actin and decreases the rate of both actin polymerization and depolymerization in living cells.Cytochalasin D can reduce exosome release, in turn reducing the amount of survivin present in the tumour environment. Cytochalasin D induces phosphorylation and cytoplasmic retention of YAP.
|
-
- HY-15308
-
-
- HY-106410
-
|
Zabofloxacin
DW-224a Free base
|
Bacterial
Topoisomerase
|
Infection
|
|
Zabofloxacin (DW-224a Free base) is a potent and seletive inhibitor of the bacterial type II and IV topoisomerases. Zabofloxacin has excellent activity against gram-positive pathogens including Steptococcus aureus, Streptococcus pyogenes and S.pneumonia. Zabofloxacin is a novel fluoronaphthyridone quinolone that is considered as an alternative antibiotic for treatment of quinolone-susceptible (QSSP) and quinolone-resistant gonorrhea (QRSP).
|
-
- HY-14261
-
-
- HY-128910
-
-
- HY-N1724
-
-
- HY-103023
-
|
CLP290
|
Potassium Channel
|
Neurological Disease
|
|
CLP290 is an orally available activator of the neuron-specific K +-Cl − cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ rats.
|
-
- HY-135279
-
|
CFTR corrector 4
|
CFTR
|
Inflammation/Immunology
|
|
CFTR corrector 4 (Compound 13), an active (R,R)-form enantiomer, is a highly potent and orally active cystic fibrosis transmembrane conductance regulator (CFTR) corrector. CFTR corrector 4 can increase CFTR levels at the cell surface and have the potential for treatment of cystic fibrosis.
|
-
- HY-125355
-
|
SEC
|
Apoptosis
|
Cancer
|
|
SEC induces activation of ANXA7 GTPase via the AMPK/mTORC1/STAT3 signaling pathway. SEC selectively promotes apoptosis in cancer cells, expressing a high level of ITGB4 by inducing ITGB4 nuclear translocation.
|
-
- HY-128671
-
-
- HY-B1245
-
|
Salsalate
Salicylsalicylic acid; Disalicylic acid
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Salsalate, a non-acetylated salicylate, is an effective antirheumatic drug that bypasses gastric absorption and also avoids cyclooxygenase inhibition. Salsalate has anti-inflammatory activity and reduces glucose levels, insulin resistance, and cytokine expression. Salsalate can be used in the research of type 2 diabetes.
|
-
- 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-15556A
-
-
- HY-15556
-
-
- HY-15662
-
|
Tulathromycin A
Tulathromycin; CP 472295
|
Antibiotic
Bacterial
|
Infection
|
|
Tulathromycin A (Tulathromycin), a macrolide antibiotic, inhibits protein synthesis (IC50=0.26 µM) by targeting bacterial ribosome. Tulathromycin A is used for the research of respiratory disease in cattle and swine. Immunomodulatory effects.
|
-
- HY-112398
-
-
- HY-111098
-
-
- HY-N4146
-
-
- HY-19608
-
-
- HY-N6982
-
-
- HY-N7597
-
|
Epimedoside
Korepimedoside A
|
Others
|
Others
|
|
Epimedoside is a flavonol glycoside, isolated from the aerial parts of Epimedium koreanum Nakai (Berberidaceae).
|
-
- 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-75041
-
|
Calcitriol Impurities A
|
VD/VDR
|
Metabolic Disease
|
|
Calcitriol Impurities A is the impurity of Calcitriol, Calcitriol is the hormonally active form of vitamin D, Calcitriol is the active metabolite of vitamin D3 that activates the vitamin D receptor (VDR).
|
-
- HY-N4133
-
-
- HY-B0911
-
|
Sodium copper chlorophyllin A
|
Others
|
Cancer
|
|
Sodium copper chlorophyllin A is a semi-synthetic mixture of water-soluble sodium copper salts derived from chlorophyll, primarily used as a food additive and in alternative medicine.
|
-
- HY-N5045
-
|
Jionoside A1
|
Others
|
Inflammation/Immunology
|
|
Jionoside A1 isolated from Radix Rehmanniae Praeparata displays dose dependent immune-enhancement activity and possesses moderate protective activities on H2O2-treated SH-SY5Y cells.
|
-
- HY-N0568
-
-
- HY-13032A
-
|
GSK 525768A
|
Others
|
Cancer
|
|
GSK 525768A is the inactive enantiomer of GSK525762A. GSK 525768A has no activity towards BET.
|
-
- HY-B0343A
-
-
- HY-N6950
-
|
Hederacolchiside A1
|
PI3K
Akt
mTOR
Parasite
Apoptosis
|
Cancer
Infection
|
|
Hederacolchiside A1, isolated from Pulsatilla chinensis, suppresses proliferation of tumor cells by inducing apoptosis through modulating PI3K/Akt/mTOR signaling pathway. Hederacolchiside A1 has antischistosomal activity, affecting parasite viability both in vivo and in vitro.
|
-
- HY-N2264
-
|
Wulignan A1
|
Influenza Virus
|
Infection
|
|
Wulignan A1 is isolated from the stems of Schisandra henryi. Wulignan A1 exhibits anti-influenza virus H1N1 and H1N1-TR (a Tamiflu drug resistant virus strain) activities.
|
-
- HY-P1539A
-
-
- HY-12361
-
|
PF 1022A
|
Parasite
|
Infection
|
|
PF 1022A is a cyclooctadepsipeptide with broadspectrum anthelmintic properties produced by fermentation of the fungus Mycelia sterilia. PF 1022A is a channel-forming ionophore. PF 1022A showes strong anthelmintic activities against Ascaridia galli in chickens. PF 1022A also can be used for angiostrongyliasis research.
|
-
- HY-107676
-
|
SIB-1553A
|
nAChR
|
Neurological Disease
|
|
SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
|
-
- HY-B1802A
-
-
- HY-100454
-
-
- HY-P2123A
-
-
- HY-107273
-
-
- HY-N5064
-
-
- HY-P1333A
-
|
Dynorphin A TFA
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A TFA, an endogenous opioid peptide, is a highy potent kappa opioid receptor (KOR) activator. Dynorphin A TFA also serve as an agonist for other opioid receptors, such as mu (MOR) and delta (DOR).
|
-
- HY-15442
-
-
- HY-N7438
-
|
Mogroside VI A
|
Others
|
Others
|
|
Mogroside VI A, an isomer of Mogroside VI isolated from Luo Han Guo, exerts sweetness property. Mogroside VI A can be used for sweetener and/or taste modifier research.
|
-
- HY-112091
-
-
- HY-N5106
-
|
(E)-Flavokawain A
|
Apoptosis
|
Cancer
|
|
(E)-Flavokawain A, a chalcone extracted from Kava, has anticarcinogenic effect. (E)-Flavokawain A induces apoptosis in bladder cancer cells by involvement of bax protein-dependent and mitochondria-dependent apoptotic pathway and suppresses tumor growth in mice.
|
-
- HY-N2343
-
-
- HY-113573
-
|
Protosappanin A
PTA
|
JAK
STAT
|
Inflammation/Immunology
|
|
Protosappanin A (PTA), an immunosuppressive ingredient and major biphenyl compound isolated from Caesalpinia sappan L, suppresses JAK2/STAT3-dependent inflammation pathway through down-regulating the phosphorylation of JAK2 and STAT3.
|
-
- HY-103200
-
-
- HY-128973
-
-
- HY-136151
-
|
UNC10217938A
|
Others
|
Others
|
|
UNC10217938A is a 3-deazapteridine analog with strong oligonucleotide enhancing effects. UNC10217938A enhances oligonucleotides effects by modulating their intracellular trafficking and release from endosomes. UNC10217938A also enhances the effects of antisense and siRNA oligonucleotides.
|
-
- HY-N2172
-
-
- HY-111828
-
|
TTA-A2
|
Calcium Channel
|
Neurological Disease
|
|
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
|
-
- HY-N0495
-
|
Aloenin
Aloenin A
|
Beta-secretase
|
Neurological Disease
|
|
Aloenin (Aloenin A) is a class of anthraquinones isolated from Aloe arborescens. Aloenin has potent peroxyl radical-scavenging activities and moderate inhibitory active on β-secretase (BACE).
|
-
- HY-15995
-
-
- 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-103129
-
|
SB-200646A
|
5-HT Receptor
|
Neurological Disease
|
|
SB-200646A is the first selective 5-HT2B/2C over 5-HT2A receptor antagonist with pKi values of 7.5, 6.9 and 5.2 for 5-HT2B, 5-HT2C and 5-HT2A, respectively. SB-200646A is orally active and has electrophysiological and anxiolytic properties in vivo.
|
-
- HY-112152
-
-
- HY-101582
-
-
- HY-101746
-
|
GSK376501A
|
PPAR
|
Metabolic Disease
|
|
GSK376501A is a selective peroxisome proliferator-activated receptor gamma (PPARγ) modulator for the treatment of type 2 diabetes mellitus.
|
-
- HY-19243
-
-
- HY-19477
-
-
- HY-101192
-
-
- HY-108434
-
|
Ceapin-A7
|
Others
|
Metabolic Disease
Neurological Disease
|
|
Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings.
|
-
- HY-111398
-
-
- HY-113263
-
-
- HY-102064
-
|
SR 57227A
|
5-HT Receptor
|
Neurological Disease
|
|
SR 57227A is a potent, orally active and selective 5-HT3 receptor agonist, with ability to cross the blood brain barrier. SR 57227A has affinities (IC50) varying between 2.8 and 250 nM for 5-HT3 receptor binding sites in rat cortical membranes and on whole NG 108-15 cells or their membranes. Anti-depressant effects.
|
-
- HY-N6915
-
-
- HY-N6079
-
-
- HY-N6942
-
|
Mogroside IV-A
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside IV-A, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-N2167
-
-
- HY-124906
-
|
JAMI1001A
|
iGluR
|
Neurological Disease
|
|
JAMI1001A is a positive allosteric modulator of AMPA receptor. JAMI1001A efficaciously modulates AMPA receptor deactivation and desensitization of both flip and flop receptor isoforms.
|
-
- HY-B0519A
-
|
Tylosin
Tylosin A
|
Bacterial
Antibiotic
|
Infection
|
|
Tylosin (Tylosin A) is a macrolide antibiotic found naturally as a fermentation product of Streptomyces fradiae. Tylosin exerts potent antimicrobial activity against Gram-positive bacteria. Tylosin is widely used as a feed additive for promoting animal growth. Tylosin is used for veterinary purposes against bacterial dysentery and respiratory diseases in poultry, pigs and cattle.
|
-
- HY-128945
-
|
CL2A
|
ADC Linker
|
Cancer
Inflammation/Immunology
|
|
CL2A is a claevable complicated PEG8- and triazole-containing PABC-peptide-mc linker. CL2A is cleavable through pH sensitivity, giving rise to bystander effect, and binds the antibody at a cysteine residue via a disulfide bond. Labetuzumab govitecan used this linker.
|
-
- HY-14467
-
-
- HY-100672
-
-
- HY-N6680
-
|
Virginiamycin S1
|
Bacterial
Antibiotic
|
Infection
|
|
Virginiamycin S1 is a cyclic hexadepsipeptide antibiotic, inhibits bacterial protein synthesis at the level of aminoacyl-tRNA binding and peptide bond formation. Virginiamycin S1 belongs to the type B compounds in the streptogramin family and is produced by Streptomyces virginiae, shows a strong bactericidal activity against a wide range of Gram-positive bacteria. Virginiamycin S1 together with virginiamycin M1 is more effective in treat multidrug-resistant bacterial infections[1][2].
|
-
- HY-12993B
-
|
RSV604 (R enantiomer)
A-60444 (R enantiomer)
|
RSV
|
Infection
|
|
RSV604 R enantiomer is the R-enantiomer of RSV604. RSV604 is an inhibitor of respiratory syncytial virus (RSV) replication. R-enantiomer is less active against RSV.
|
-
- HY-N0368
-
|
Linalool
|
iGluR
Apoptosis
Endogenous Metabolite
|
Cancer
Cardiovascular Disease
|
|
Linalool is natural monoterpene in essential olis of coriander, acts as a competitive antagonist of Nmethyl d-aspartate (NMDA) receptor, with anti-tumor, anti-cardiotoxicity activity.Linalool is a PPARα ligand that reduces plasma TG levels and rewires the hepatic transcriptome and plasma metabolome.
|
-
- HY-116330A
-
|
Hyperforin dicyclohexylammonium salt
Hyperforin DCHA
|
TRP Channel
Calcium Channel
|
Neurological Disease
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
|
-
- HY-136310
-
|
PIP4K-IN-a131
|
Others
|
Cancer
|
|
PIP4K-IN-a131 is PIP4K lipid kinases inhibitor, with IC50s of 1.9 µM and 0.6 µM for purified PIP4K2A and PIP4Ks, respectively. PIP4K-IN-a131 exhibits cancer-selective lethality via dual blockade of the lipid kinase PIP4Ks and mitotic pathways.
|
-
- HY-N0729
-
|
Linoleic acid
|
Endogenous Metabolite
|
Metabolic Disease
Cardiovascular Disease
|
|
Linoleic acid is a common polyunsaturated (PUFA) found in plant-based oils, nuts and seeds. Linoleic acid is a part of membrane phospholipids, and functions as a structural component to maintain a certain level of membrane fluidity of the transdermal water barrier of the epidermis. Linoleic acid induces red blood cells and hemoglobin damage via oxidative mechanism .
|
-
- HY-N0201
-
|
Atractylenolide I
|
Toll-like Receptor (TLR)
JAK
STAT
|
Cancer
|
|
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
|
-
- HY-B0245S
-
|
Busulfan-D8
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
Busulfan-D8 is a deuterium labeled Busulfan. Busulfan is an alkyl sulfonate that acts as an alkylating antineoplastic agent. Busulfan forms both intra- and interstrand crosslinks on DNA. In mammals, Busulfan causes profound and prolonged reduction in the generation of hematopoietic progenitors without significantly affecting lymphocyte levels or humoral antibody responses.
|
-
- HY-14247A
-
|
Fadrozole
CGS 16949A free base; (Rac)-FAD286
|
Aromatase
|
Cancer
|
|
Fadrozole (CGS 16949A free base) is a potent, selective and nonsteroidal inhibitor of aromatase with an IC50 of 6.4 nM.
|
-
- HY-19644
-
|
GSK2256294A
GSK 2256294
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
GSK2256294A is a potent, reversible, tight binding inhibitor of isolated recombinant human sEH (soluble epoxide hydrolase) (IC50 = 27 pM; t1/2 = 121 min) and displays potent inhibition against the rat (IC50 = 61 pM) and murine (IC50 = 189 pM) orthologs of sEH.
|
-
- HY-N7614
-
|
Anemarrhenasaponin A2
Schidigerasaponin F2; Timosaponin AII
|
Others
|
Cardiovascular Disease
|
|
Anemarrhenasaponin A2 (Schidigerasaponin F2) is a steroidal saponin isolated from the rhizomes of Anemarrhena asphodeloides. Anemarrhenasaponin A2 inhibits ADP-induced platelet aggregation.
|
-
- HY-N0692
-
|
Schisandrol B
Gomisin-A; TJN-101; Wuweizi alcohol-B
|
Reactive Oxygen Species
Cytochrome P450
Autophagy
|
Cancer
|
|
Schisandrol B (Gomisin-A) is a major active constituent of Schisandra sphenanthera with hepato-protective effects. Schisandrol B inhibits reactive oxygen species (ROS) production. Schisandrol B inhibits the activity of P-glycoprotein and CYP3A and also has anti-inflammatory, anti-diabetic and antioxidant activities.
|
-
- HY-N6707
-
|
Triacsin C
WS 1228A; FR 900190
|
Others
|
Infection
|
|
Triacsin C (WS 1228A), a natural intracellular long-chain acyl-CoA synthetases (ACSL) inhibitor, is from Streptomyces aureofaciens. Triacsin C inhibits TAG accumulation into lipid droplets (LD) by suppressing ACSL activity. Triacsin C is found to be highly effective against rotavirus replication.
|
-
- HY-101513
-
|
eIF4A3-IN-1
|
Eukaryotic Initiation Factor (eIF)
Autophagy
|
Cancer
|
|
eIF4A3-IN-1 (compound 53a) is a selective eukaryotic initiation factor 4A3 (eIF4A3) inhibitor (IC50=0.26 μM; Kd=0.043 μM), which binds to a non-ATP binding site of eIF4A3 and shows significant cellular nonsense-mediated RNA decay (NMD) inhibition at 10 and 3 μM and can be as a probe for further study of eIF4A3, the exon junction complex (EJC), and NMD.
|
-
- HY-N0811
-
|
Anemarsaponin B
|
NO Synthase
COX
NF-κB
|
Inflammation/Immunology
|
|
Anemarsaponin B is a steroidal saponin isolated from the rhizomes of A. asphodeloides (Liliaceae). Anemarsaponin B decreases the protein and mRNA levels of iNOS and COX-2. Anemarsaponin B reduces the expressions and productions of pro-inflammatory cytokines, including TNF-a and IL-6. Anemarsaponin B inhibits the nuclear translocation of the p65 subunit of NF-κB by blocking the phosphorylation of IκBα. Anemarsaponin B also inhibits the phosphorylation of MAP kinase kinases 3/6 (MKK3/6) and mixed lineage kinase 3 (MLK3). Anti-inflammatory effect .
|
-
- HY-13032
-
-
- HY-111518
-
|
JH-XI-10-02
|
PROTAC
CDK
|
Cancer
|
|
JH-XI-10-02 is a highly potent and selective PROTAC CDK8 degrader, with an IC50 of 159 nM. JH-XI-10-02 causes proteasomal degradation, does not affect CDK8 mRNA levels. JH-XI-10-02 shows no effect on CDK19.
|
-
- HY-14649
-
|
Retinoic acid
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-P9805
-
|
Anti-MERS-3A1 mAb
MERS-3A1; MERS Antibody-3A1
|
SARS-CoV
|
Infection
|
|
Anti-MERS-3A1 mAb (MERS-3A1) is a human monoclonal IgG1 antibody with the high binding affinity produced in CHO cells.
Anti-MERS-3A1 mAb bocks the binding of MERS-CoV spike protein to DPP4 receptor.
|
-
- HY-P1328
-
|
TAT-14
|
Keap1-Nrf2
|
Others
|
|
TAT-14 is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-B0673
-
|
Pirfenidone
AMR69
|
TGF-beta/Smad
CCR
|
Inflammation/Immunology
Cancer
|
|
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities.
|
-
- HY-N1535
-
|
Ponicidin
Rubescensine B
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Ponicidin (Rubescensine B) is a diterpenoid derived from Rabdosia rubescens, and exhibits immunoregulatory, anti-inflammatory, anti-viral and anti-cancer activity. Ponicidin (Rubescensine B) induces apoptosis of gastric carcinoma cell, decreases the phosphorylation of JAK2 and STAT3, and shows no effect on protein levels of JAK2 and STAT3.
|
-
- HY-136093
-
|
HL271
IM156 hydrochloride; HL156A hydrochloride
|
AMPK
|
Cancer
Neurological Disease
|
|
HL271 (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. HL271 attenuates aging-associated cognitive impairment in animal model. HL271 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
|
-
- HY-10252
-
|
NVP-ADW742
ADW742; GSK 552602A; ADW
|
IGF-1R
Insulin Receptor
Apoptosis
|
Cancer
Endocrinology
|
|
NVP-ADW742 (ADW742) is an orally active, selective IGF-1R tyrosine kinase inhibitor with an IC50 of 0.17 μM. NVP-ADW742 inhibits insulin receptor (InsR) with an IC50 of 2.8 μM. NVP-ADW742 induces pleiotropic antiproliferative/proapoptotic biologic sequelae in tumor cells.
|
-
- HY-136093A
-
|
IM156
HL156A; HL271 acetate
|
AMPK
|
Cancer
Neurological Disease
|
|
IM156 (HL156A; HL271 acetate), a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. IM156 attenuates aging-associated cognitive impairment in animal model. IM156 is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors.
|
-
- HY-12838
-
|
Mirk-IN-1
Dyrk1B/A-IN-1
|
DYRK
|
Cancer
|
|
Mirk-IN-1 is a potent inhibitor of Dyrk1B(Mirk kianse) and Dyrk1A with IC50 of 68±48 nM and 22±8 nM respectively.
|
-
- HY-111532
-
|
(3R,4R)-A2-32-01
|
Bacterial
|
Infection
|
|
(3R,4R)-A2-32-01 (compound 2), an anti-virulence drug, is a specific caseinolytic protein proteases (ClpP) inhibitor with an EC50 of 4.5 μM, and shows a tolerable cytotoxicity.
|
-
- HY-138298
-
|
Trastuzumab deruxtecan
DS-8201; DS-8201a
|
EGFR
|
Cancer
|
|
Trastuzumab deruxtecan (DS-8201a) is an anti-human epidermal growth factor receptor 2 (HER2) antibody-drug conjugate (ADC). Trastuzumab deruxtecan is composed of a humanized anti-HER2 antibody, an enzymatically cleavable peptide-linker, and a topoisomerase I inhibitor. Trastuzumab deruxtecan can be used for the research of HER2-positive breast cancer and gastric cancer.
|
-
- HY-120006A
-
|
(rel)-AR234960
|
ERK
|
Cardiovascular Disease
|
|
(rel)-AR234960 is an active relative configuration of AR234960. AR234960, a non-peptide MAS (a G protein-coupled receptor) agonist, increases both mRNA and protein levels of CTGF via ERK1/2 signaling in HEK293-MAS cells and adult human cardiac fibroblasts.
|
-
- HY-P1852
-
-
- HY-P1428
-
|
RFRP-1(human)
|
Neuropeptide Y Receptor
|
|
|
RFRP-1(human) is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-P1328A
-
|
TAT-14 TFA
|
Keap1-Nrf2
|
Others
|
|
TAT-14 TFA is a 14-mer peptide that acts as Nrf2 activator with an anti-inflammatory effect. TAT-14 TFA has no effect on Nrf2 mRNA expression, but increases Nrf2 protein level due to targeting the Nrf2 binding site on Keap1.
|
-
- HY-P1397
-
|
RVD-Hpα
|
Cannabinoid Receptor
|
|
|
RVD-Hpα is the N-terminally extended form of human hemopressin that acts as a selective CB1 receptor agonist. RVD-Hpα increases intracellular Ca 2+ levels in cells expressing CB1 receptors in vitro. RVD-Hpα also high affinity CB2 positive allosteric modulator (Ki=50 nM).
|
-
- HY-P1505
-
-
- HY-P1788
-
-
- HY-101947
-
|
SMI-16a
PIM1/2 Kinase Inhibitor VI
|
Pim
|
Cancer
|
|
SMI-16a is a selective Pim kinase inhibitor with IC50 values of 0.15, 0.02 and 48 μM for Pim1, Pim2 and PC3 cells, respectively.
|
-
- HY-B0422S
-
|
Nateglinide D5
A4166 D5; Senaglinide D5
|
Potassium Channel
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Nateglinide D5 is a deuterium labeled Nateglinide. Nateglinide, a D-phenylalanine derivative, is an orally active and short-acting insulinotropic agent and a DPP IV inhibitor. Nateglinide inhibits ATP-sensitive K + channels in pancreatic β-cells. Nateglinide is used for the treatment of type 2 (non-insulin-dependent) diabetes mellitus.
|
-
- HY-16668
-
-
- HY-14262
-
|
Vilazodone
EMD 68843; SB659746A
|
5-HT Receptor
Serotonin Transporter
|
Neurological Disease
|
|
Vilazodone (EMD 68843; SB 659746A) is a potent, selective and orally active serotonin reuptake inhibitor (SSRI) and partial 5-HT1A receptor agonist. Vilazodone exhibits antidepressant efficacy in vivo can be used for the research of major depressive disorder (MDD) and affective disorders.
|
-
- HY-114495
-
|
Caerulomycin A
Cerulomycin; Caerulomycin
|
Fungal
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Caerulomycin A (Cerulomycin; Caerulomycin), an antifungal compound, induces generation of T cells, enhances TGF-β-Smad3 protein signaling via suppressing interferon-γ-induced STAT1 signaling. Antifungal and antibiotic activity, and used in autoimmune diseases.
|
-
- HY-126937
-
|
Ivermectin B1a
|
Parasite
SARS-CoV
|
Infection
|
|
Ivermectin B1a, a derivative of Avermectin B1a (HY-15308), is a main component of Ivermectin (HY-15310). Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
|
-
- HY-112667
-
-
- HY-19555
-
|
Seco Rapamycin
Secorapamycin A
|
Others
|
Others
|
|
Seco Rapamycin (Secorapamycin A) is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.
|
-
- HY-12993A
-
|
RSV604 racemate
A-60444 racemate
|
RSV
|
Others
|
|
RSV604 (A-60444) racemate is a racemic mixture, shows less potency against strains of respiratory syncytial virus (RSV) than the S-isomer.
|
-
- HY-B0355
-
-
- HY-110155
-
|
LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
|
-
- HY-101437
-
-
- HY-P9904
-
|
Atezolizumab
MPDL3280A
|
PD-1/PD-L1
|
Cancer
|
|
Atezolizumab (MPDL3280A) is a selective humanized monoclonal IgG1 antibody against programmed death ligand 1 (PD-L1), used for cancer research.
|
-
- HY-108272
-
|
Mogroside II-A2
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside II-A2, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-101437A
-
-
- HY-100638
-
|
RPR132595A
NPC
|
Others
|
Cancer
|
|
RPR132595A (NPC) is an active metabolite of CPT-11, which is generated by cytochrome P-450 3A4 (CYP3A4) and finally excreted through urine.
|
-
- HY-100673
-
-
- HY-N3502
-
-
- HY-B0395C
-
|
Sitafloxacin hydrate
DU6859a hydrate
|
Bacterial
Antibiotic
|
Infection
|
|
Sitafloxacin (DU6859a) hydrate is a potent, orally active fluoroquinolone antibiotic with in vitro activity against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection.
|
-
- HY-N0679
-
|
Retinyl acetate
Retinol acetate; Vitamin A acetate
|
Others
|
Cancer
|
|
Retinyl acetate is a synthetic acetate ester form derived from retinol and has potential antineoplastic and chemo preventive activities.
|
-
- HY-B0197A
-
-
- HY-135283
-
|
ABT-546
A-216546
|
Endothelin Receptor
|
Endocrinology
Cardiovascular Disease
|
|
ABT-546 (A-216546) is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively.
|
-
- HY-N6940
-
|
Prosapogenin A
Progenin III
|
Apoptosis
|
Cancer
|
|
Prosapogenin A, a natural product from Veratrum, induces apoptosis in human cancer cells in vitro via inhibition of the STAT3 signaling pathway and glycolysis.
|
-
- HY-B0284
-
-
- HY-N2214
-
|
7-O-Methylaloeresin A
|
Bacterial
|
Inflammation/Immunology
|
|
7-O-Methylaloeresin A is 5-methylchromone glycoside isolated from Commiphora socotrana (Burseraceae).
7-O-Methylaloeresin A exhibits good activity against multiple drug resistant Staphylococcus aureus (NCTC 11994) and Salmonella typhimurium (ATCC 1255) with MIC values of 0.72 and 0.18 mM, respectively.
7-O-Methylaloeresin A has antioxidant activities, gives IC50 values of 0.026 mM and 0.021 mM for DPPH and 2-deoxyribose degradation assay, respectively.
|
-
- HY-B0523A
-
-
- HY-P2159
-
|
Dynorphin A (1-8)
|
Opioid Receptor
|
Neurological Disease
|
|
Dynorphin A (1-8) is the predominant opioid peptide identified in placental tissue extracts. Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. The binding of 3H-Bremazocine to the purified kappa receptor is inhibited by Dynorphin A (1-8) (IC50=303 nM).
|
-
- HY-108385
-
|
Ochratoxin A-D4
|
Others
|
Cancer
|
|
Ochratoxin A-D4 is the deuterium labeled Ochratoxin A. Ochratoxin A, a mycotoxin produced by several fungal species, causes nephrotoxicity and renal tumors in a variety of animal species.
|
-
- HY-108593
-
-
- HY-18679
-
|
TC-N 22A
|
mGluR
|
Neurological Disease
|
|
TC-N 22A is a potent, selective, orally active and brain-permeable mGlu4 PAM with an EC50 of 9 nM in human mGlu4-expressing BHK cells. TC-N 22A is less active (EC50>10 μM) in agonist and PAM model at mGlu 1, 2, 3, 5, and 7 receptors. TC-N 22A has the potential for research of CNS disease in vivo.
|
-
- HY-N1964
-
|
Gibberellic acid
Gibberellin A3
|
Others
|
Others
|
|
Gibberellic Acid is named after a fungus Gibberella fujikuroi . Gibberellic Acid regulates processes of plant development and growth, including seed development and germination, stem and root growth, cell division, and flowering time.
|
-
- HY-131103S
-
-
- HY-B0395
-
|
Sitafloxacin
DU6859a
|
Bacterial
Antibiotic
|
Infection
|
|
Sitafloxacin (DU6859a) is a potent, orally active fluoroquinolone antibiotic with in vitro activity against a broad range of gram-positive and gram-negative bacteria, including anaerobic bacteria, as well as against atypical pathogens. Sitafloxacin can be used for the research of respiratory tract infection and urinary tract infection.
|
-
- HY-P0236
-
-
- HY-N6854
-
|
Mogroside I A1
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside I A1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-N1118
-
-
- HY-136408
-
|
Malonyl Coenzyme A lithium
|
Others
|
Metabolic Disease
|
|
Malonyl Coenzyme A (lithium) is a coenzyme A derivative that is utilized in fatty acid and polyketide synthesis and in the transport of α-ketoglutarate across the mitochondrial membrane. Malonyl Coenzyme A (lithium) is formed by the Acetyl CoA Carboxylase-mediated carboxylation of acetyl CoA. Malonyl Coenzyme A (lithium) is exclusively used as the extender unit in the synthesis of bacterial aromatic polyketides.
|
-
- HY-B1017
-
-
- HY-N6993
-
|
25-O-Methylalisol A
|
Others
|
Metabolic Disease
|
|
25-O-Methylalisol A is a protostane triterpenoids isolated from Alisma orientale. The dried rhizomes of the aquatic plant Alisma orientale known as Rhizoma Alismatis is a common traditional Chinese medicine used for diuretic, anti-inflammatory, and hypolipidemic purposes, as well as the treatment of diabetes.
|
-
- HY-B0780
-
-
- HY-B0071A
-
-
- HY-B0723
-
|
Ospemifene
FC-1271a
|
Estrogen Receptor/ERR
|
Cancer
|
|
Ospemifene is a non-estrogen selective estrogen receptor modulator (SERM), with Kis of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene can be used for the research of vaginal atrophy and breast cancer.
|
-
- HY-N2220
-
-
- HY-P1594
-
-
- HY-P2318
-
|
Bac2A TFA
|
Fungal
|
|
|
Bac2A TFA is an antimicrobial and immunomodulatory peptide. Bac2A TFA is a linear variant of bactenecin and is very effective against fungal pathogens.
|
-
- HY-N1988
-
|
Cucurbitacin IIa
Hemslecin A
|
Survivin
Apoptosis
|
Cancer
|
|
Cucurbitacin IIa is a triterpene isolated from Hemsleya amalils Diels, induces apoptosis of cancer cells, reduces expression of survivin, reduces phospho-Histone H3 and increases cleaved PARP in cancer cells.
|
-
- HY-108271
-
|
Mogroside III-A1
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside III-A1, a triterpenoid glycoside isolated from the extracts of Luo Han Guo, is a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-B0197
-
-
- HY-103207
-
-
- HY-N2449
-
|
(±)-Licarin A
(±)-trans-Dehydrodiisoeugenol
|
Parasite
|
Infection
|
|
(±)-Licarin A ((±)-trans-Dehydrodiisoeugenol) is a dihydrobenzofuran neolignan, the resultant of an oxidative coupling reaction of isoeugenol and horseradish peroxidase (HRP) enzyme. (±)-Licarin A displays 58.7% parasite lysis and has an IC50 value of 100.8 µM for trypanocidal activity against trypomastigote forms of T. cruzi. And (±)-Licarin A shows 100% parasites mortality at 200 µM.
|
-
- HY-N2115
-
|
Araloside A
Chikusetsusaponin IV
|
Renin
|
Cardiovascular Disease
|
|
Araloside A (Chikusetsusaponin IV) is a component of Panax japonicus, with low-renin-inhibitory activity, with an IC50 of 77.4 μM.
|
-
- HY-B0455A
-
-
- HY-N6694
-
-
- HY-113215
-
|
Allotetrahydrocortisol
5a-Tetrahydrocortisol
|
Endogenous Metabolite
|
Others
|
|
Allotetrahydrocortisol (5a-Tetrahydrocortisol) is a metabolite of Cortisol. Cortisol is the main glucocorticoid in human. It is produced in adrenal cortex and plays a crucial role in many physiological processes.
|
-
- HY-122207
-
-
- HY-P1112
-
-
- HY-U00188
-
-
- HY-B0417A
-
-
- HY-115376
-
|
Z62954982
ZINC08010136
|
Ras
|
Inflammation/Immunology
|
|
Z62954982 (ZINC08010136) is a potent, selective and cell-permeable Rac1 (IC50=12 μM) inhibitor that is 4 times more effective than NSC23766 (HY-15723A) (IC50=50 μM). Z62954982 disrupts the Rac1/Tiam1 complex and decreases cytoplasmic levels of active Rac1 (GTP-bound Rac1), without affecting the activity of other Rho GTPases (such as Cdc42 or RhoA).
|
-
- HY-122218
-
|
JHU-083
|
Glutaminase
|
Neurological Disease
|
|
JHU-083, a prodrug of 6-diazo-5-oxo-L-norleucine (DON; HY-108357), is an orally active and selective glutaminase antagonist. JHU-083 blocks glutaminase activity in brain CD11b + cells and experimental cerebral malaria (ECM) resulting in a net decrease of glutamate levels in the animals.
|
-
- HY-17364
-
|
Temozolomide
NSC 362856; CCRG 81045; TMZ
|
DNA Alkylator/Crosslinker
Autophagy
Apoptosis
|
Cancer
|
|
Temozolomide (NSC 362856) is an oral active DNA alkylating agent that crosses the blood-brain barrier. Temozolomide is also a proautophagic and proapoptotic agent. Temozolomide is effective against tumor cells that are characterized by low levels of O6-alkylguanine DNA alkyltransferase (OGAT) and a functional mismatch repair system. Temozolomide has antitumor and antiangiogenic effects.
|
-
- HY-12741
-
|
LDN-212320
LDN-0212320; OSU-0212320
|
EAAT2
|
Neurological Disease
|
|
LDN-212320 (LDN-0212320) is a glutamate transporter (GLT-1)/excitatory amino acid transporter 2 (EAAT2) activator (at translational level). LDN-212320 (LDN-0212320) prevents nociceptive pain by upregulating astroglial GLT-1 expression in the hippocampus and ACC[1]
|
-
- HY-P2320
-
|
IDR-1
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release.
|
-
- HY-15176A
-
|
Pyridostatin hydrochloride
RR82 hydrochloride
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) hydrochloride is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin hydrochloride promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin hydrochloride targets the proto-oncogene Src. Pyridostatin hydrochloride reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
|
-
- HY-113056A
-
|
N1-Acetylspermidine hydrochloride
|
Endogenous Metabolite
|
Cancer
|
|
N1-Acetylspermidine hydrochloride is an acetyl derivative of polyamine. N1-acetylspermine is the substrate for the polyamine oxidase (PAO). N1-Acetylspermidine hydrochloride selectively elevates its level in human colorectal adenocarcinomas. N1-acetylspermidine shows cleavage efficiency at apurinic sites in DNA.
|
-
- HY-133129
-
|
MS1943
|
Histone Methyltransferase
Apoptosis
|
Cancer
|
|
MS1943 is a first-in-class, orally bioavailable EZH2 selective degrader, with an IC50 of 120 nM. MS1943 significantly reduces EZH2 protein levels in numerous triple-negative breast cancer (TNBC) and other cancer and noncancerous cell lines. MS1943 effectively blocks proliferation of multiple TNBC and other cancer cell lines.
|
-
- HY-13768
-
|
Topotecan
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
|
Cancer
|
|
Topotecan (SKF 104864A; NSC 609669) is a Topoisomerase I inhibitor. The IC50 values of Topotecan at 24 h are 2.73±0.25 μM of U251 cells, 2.95±0.23 μM of U87 cells, 5.46±0.41 μM of GSCs-U251 and 5.95±0.24 μM of GSCs-U87.
|
-
- HY-102024
-
-
- HY-12692
-
|
DO3A tert-Butyl ester
DO3A tert-butyl; DO3A-t-Bu-ester
|
Others
|
Others
|
|
DOTA tert-Butyl ester is a benxyl derivative of the cyclic tosamide; can be nitrated directly; is more convenient to incorporate the nitro group after deprotection lithium aluminum hydride.
|
-
- HY-P0088
-
-
- HY-113462
-
|
α-Carotene
|
Others
|
Cancer
|
|
α-Carotene, a precursor of vitamin A, is used as an anti-metastatic agent or as an adjuvant for anti-cancer drugs. α-Carotene is isolated from yellow-orange and dark-green vegetables.
|
-
- HY-123033A
-
|
Nicotinamide riboside chloride
|
Sirtuin
|
Metabolic Disease
Neurological Disease
|
|
Nicotinamide riboside Chloride, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside Chloride is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside Chloride reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
|
-
- HY-P1792
-
|
Angiotensin II (1-4), human
|
Angiotensin Receptor
|
Metabolic Disease
Endocrinology
|
|
Angiotensin II (1-4), human is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-117147A
-
|
GSK2945 hydrochloride
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 hydrochloride is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 hydrochloride enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-117147
-
|
GSK2945
|
Cytochrome P450
|
Metabolic Disease
|
|
GSK2945 is a class of tertiary amine, and is a highly specific Rev-erbα/REV-ERBα (mouse/human reverse erythroblastosis virus α) antagonist with EC50s of 21.5 μM and 20.8 μM, respectively. GSK2945 enhances cholesterol 7α-hydroxylase (CYP7A1) level and cholesterol metabolism.
|
-
- HY-123033
-
|
Nicotinamide riboside
|
Sirtuin
|
Metabolic Disease
Neurological Disease
|
|
Nicotinamide riboside, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
|
-
- HY-131334
-
|
AMPK activator 4
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
|
-
- HY-100260
-
|
beta-L-D4A
2'3'-didehydro-2'3'-dideoxyadenosine
|
HIV
|
Infection
|
|
beta-L-D4A is a nucleoside HIV-1 reverse transcriptase inhibitor.
|
-
- HY-P1792A
-
|
Angiotensin II (1-4), human TFA
|
Angiotensin Receptor
|
Endocrinology
Metabolic Disease
|
|
Angiotensin II (1-4), human (TFA) is an endogenous peptide produced from AT I by angiotensin-converting-enzyme (ACE). Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-P1769
-
|
Angiotensin II (5-8), human
|
Angiotensin Receptor
|
Metabolic Disease
Endocrinology
|
|
Angiotensin II (5-8), human is an endogenous C-terminal fragment of the peptide vasoconstrictor angiotensin II. Angiotensin II binds the AT II type 1 (AT1) receptor, stimulating GPCRs in vascular smooth muscle cells and increasing intracellular Ca 2+ levels. Angiotensin II also acts at the Na +/H + exchanger in the proximal tubules of the kidney.
|
-
- HY-B0673S
-
|
Pirfenidone D5
AMR69 D5
|
TGF-beta/Smad
CCR
|
Cancer
Inflammation/Immunology
|
|
Pirfenidone D5 (AMR69 D5) is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities.
|
-
- HY-P1505A
-
-
- HY-100008
-
|
Peretinoin
NIK333
|
RAR/RXR
SPHK
Autophagy
HCV
|
Cancer
Infection
|
|
Peretinoin is an oral acyclic retinoid retinoid with a vitamin A-like structure that targets retinoid nuclear receptors such as retinoid X receptor (RXR) and retinoic acid receptor (RAR). Peretinoin reduces the mRNA level of sphingosine kinase 1 (SPHK1) in vitro by downregulating a transcription factor, Sp1. Peretinoin prevents the progression of non-alcoholic steatohepatitis (NASH) and the development of hepatocellular carcinoma (HCC) through activating the autophagy pathway by increased Atg16L1 expression. Peretinoin inhibits HCV RNA amplification and virus release by altering lipid metabolism with a EC50 of 9 μM.
|
-
- HY-131615
-
|
TPC2-A1-P
|
Sodium Channel
|
Others
|
|
TPC2-A1-P is a powerful and membrane permeable agonist of two pore channel 2 (TPC2) with an EC50 of 10.5 μM. TPC2-A1-P plays its role by mimicking the physiological actions of PI(3,5)P2. TPC2-A1-P also shows higher potency to induce Na 2+ mobilisation from TPC2 than TPC-A1-N (HY-131614). TPC2-A1-P can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-17442
-
-
- HY-103090
-
-
- HY-N0691
-
|
Schisandrin
Schizandrin; Schizandrol; Schizandrol-A
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Schisandrin (Schizandrin), a dibenzocyclooctadiene lignan, is isolated from the fruit of Schisandra chinensis Baill. Schisandrin exhibits antioxidant, hepatoprotective, anti-cancer and anti-inflammatory activities. Schisandrin also can reverses memory impairment in rats.
|
-
- HY-129995A
-
-
- HY-16973
-
|
Fluralaner
A1443; AH252723
|
Parasite
|
Infection
|
|
Fluralaner (INN) is a systemic insecticide and acaricide Fluralaner through potent blockage of GABA and L-glutamate gated chloride channels.
|
-
- HY-14111
-
-
- HY-P2230
-
|
Angstrom6
A6 Peptide
|
PAI-1
|
Cancer
|
|
Angstrom6 (A6 Peptide) is an 8 amino-acid peptide derived from single-chain urokinase plasminogen activator (scuPA) and interferes with the uPA/uPAR cascade and abrogates downstream effects. Angstrom6 binds to CD44 resulting in the inhibition of migration, invasion, and metastasis of tumor cells, and the modulation of CD44-mediated cell signaling.
|
-
- HY-12405
-
-
- HY-10171
-
|
NPS-2143 hydrochloride
SB-262470A hydrochloride
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 hydrochloride (SB-262470A hydrochloride), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 hydrochloride (SB-262470A hydrochloride) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-106224
-
|
Orexin A (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-10007
-
|
NPS-2143
SB-262470A
|
CaSR
|
Metabolic Disease
|
|
NPS-2143 (SB-262470A), an orally active calcilytic agent, is a selective and potent calcium ion-sensing receptor (CaSR) antagonist. NPS-2143 (SB-262470A) blocks increases in cytoplasmic Ca 2+ concentrations (IC50=43 nM) elicited by activating the Ca 2+ receptor in HEK 293 cells expressing the human Ca 2+ receptor.
|
-
- HY-B0012A
-
-
- HY-P1112A
-
-
- HY-U00230
-
-
- HY-17621
-
-
- HY-10847B
-
|
SB-277011 hydrochloride
SB-277011A hydrochloride
|
Dopamine Receptor
5-HT Receptor
|
Neurological Disease
|
|
SB-277011 hydrochloride (SB-277011A hydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor (D3R) antagonist with Ki values of 10.7 nM and 11.2 nM at rodent and human D3R, respectively. SB-277011 hydrochloride displays 80- to 100-fold selectivity over other dopamine receptors with pKis of 8.0, 6.0, <5.2, and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-19555A
-
|
Seco Rapamycin sodium salt
Secorapamycin A monosodium
|
Others
|
Others
|
|
Seco Rapamycin sodium salt is the ring-opened product of Rapamycin. Seco-rapamycin is reported not to affect the mTOR function.
|
-
- HY-107723
-
-
- HY-16566A
-
-
- HY-18776
-
-
- HY-18233
-
|
E1210
APX001A
|
Fungal
|
Infection
|
|
E1210 is a first-in-class, broad-spectrum and orally active antifungal. E1210 has a mechanism of action-inhibition of fungal glycosylphosphatidylinositol (GPI) biosynthesis.
|
-
- HY-10847
-
-
- HY-15370A
-
-
- HY-N0258
-
-
- HY-110155A
-
|
(Rac)-LM11A-31 dihydrochloride
|
Others
|
Neurological Disease
|
|
(Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
|
-
- HY-101105A
-
-
- HY-131614
-
|
TPC2-A1-N
|
Calcium Channel
|
Others
|
|
TPC2-A1-N is a powerful and Ca 2+-permeable agonist of two pore channel 2 (TPC2), which plays its role by mimicking the physiological actions of NAADP. TPC2-A1-P reproducibly evokes significant Ca 2+ responses from TPC2 (EC50=7.8 μM), and the effect can be blocked by several TPC blockers. TPC2-A1-N can be used to probe different functions of TPC2 channels in intact cells.
|
-
- HY-131152
-
-
- HY-N7401
-
-
- HY-13748
-
|
Silibinin
Silibinin A; Silymarin I
|
Autophagy
Reactive Oxygen Species
|
Cancer
|
|
Silibinin (Silibinin A), an effective anti-cancer and chemopreventive agent, has been shown to exert multiple effects on cancer cells, including inhibition of both cell proliferation and migration.
|
-
- HY-136269
-
-
- HY-P0236A
-
-
- HY-B0292A
-
-
- HY-101809
-
-
- HY-P1594A
-
-
- HY-N0841
-
|
Bruceine A
Dihydrobrusatol; NSC310616
|
Parasite
Antibiotic
|
Infection
|
|
Bruceine A(NSC310616; Dihydrobrusatol) is a natural quassinoid compound extracted from the dried fruits of Brucea javanica (L.
|
-
- HY-N0812
-
-
- HY-103090A
-
-
- HY-12100
-
-
- HY-110258
-
|
ML334
LH601A
|
Keap1-Nrf2
|
Cancer
|
|
ML334 is a potent, cell permeable activator of NRF2 by inhibition of Keap1-NRF2 protein-protein interaction. ML334 binds to Keap1 Kelch domain with a Kd of 1 μM. ML334 stimulates NRF2 expression and nuclear translocation and induces antioxidant response elements (ARE) activity.
|
-
- HY-10847A
-
|
SB-277011 dihydrochloride
SB-277011A dihydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
|
-
- HY-N6696
-
|
Aflatoxin B2
|
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Aflatoxin B2 is a major naturally produced aflatoxin. Aflatoxin B2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
-
- HY-15176B
-
|
Pyridostatin TFA
RR82 TFA
|
G-quadruplex
|
Cancer
|
|
Pyridostatin (RR82) TFA is a G-quadruplex DNA stabilizing agent (Kd=490 nM). Pyridostatin TFA promotes growth arrest in human cancer cells by inducing replication- and transcription-dependent DNA damage. Pyridostatin TFA targets the proto-oncogene Src. Pyridostatin TFA reduced SRC protein levels and SRC-dependent cellular motility in human breast cancer cells.
|
-
- HY-N6698
-
|
Aflatoxin G2
|
Bacterial
Antibiotic
|
Cancer
Infection
|
|
Aflatoxin G2 is a major naturally produced aflatoxin. Aflatoxin G2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus.The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
-
- HY-123033B
-
|
Nicotinamide riboside tartrate
|
Sirtuin
|
Metabolic Disease
Neurological Disease
|
|
Nicotinamide riboside tartrate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside tartrate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside tartrate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
|
-
- HY-123033C
-
|
Nicotinamide riboside malate
|
Sirtuin
|
Metabolic Disease
Neurological Disease
|
|
Nicotinamide riboside malate, an orally active NAD + precursor, increases NAD + levels and activates SIRT1 and SIRT3. Nicotinamide riboside malate is a source of vitamin B3 (niacin) and enhances oxidative metabolism, protection against high fat diet-induced metabolic abnormalities. Nicotinamide riboside malate reduces cognitive deterioration in a transgenic mouse model of Alzheimer’s disease.
|
-
- HY-15644
-
|
Tyrphostin 23
Tyrphostin A23; RG-50810; AG 18
|
EGFR
|
Cancer
|
|
Tyrphostin 23 (Tyrphostin A23) is an EGFR inhibitor with an IC50 and Kiof 35 and 11 μM, respectively.
|
-
- HY-N6700
-
|
Aflatoxin M2
|
Others
|
Cancer
|
|
Aflatoxin M2 is a major metabolite of Aflatoxin B1. Aflatoxin M2 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
-
- 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-128895
-
|
KL1333
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
KL1333, a derivative of β-lapachone, is an orally available NAD+ modulator. KL1333 reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, resulting in increases in intracellular NAD+ levels via NADH oxidation. KL1333 improves energy metabolism and mitochondrial dysfunction in MELAS fibroblasts. KL1333 protects against Cisplatin-induced ototoxicity in mouse cochlear cultures.
|
-
- 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-130259
-
|
LC3-mHTT-IN-AN2
|
Autophagy
|
Neurological Disease
|
|
LC3-mHTT-IN-AN2 (Compound AN2) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN2 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
-
- HY-N6699
-
|
Aflatoxin M1
|
Bacterial
|
Cancer
Infection
|
|
Aflatoxin M1 is a major metabolite of Aflatoxin B1. Aflatoxin M1 is a mycotoxin produced by the fungi Aspergillus flavus and Aspergillus parasiticus. The level of toxicity associated with Aflatoxin is Aflatoxin B1>Aflatoxin M1>Aflatoxin G1>Aflatoxin B2>Aflatoxin M2>Aflatoxin G2.
|
-
- HY-126124
-
|
AP39
|
Others
|
Neurological Disease
Cardiovascular Disease
|
|
AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury and protects against Alzheimer's disease in mice model.
|
-
- HY-130258
-
|
LC3-mHTT-IN-AN1
|
Autophagy
|
Neurological Disease
|
|
LC3-mHTT-IN-AN1 (Compound AN1) is a mHTT-LC3 linker compound, which interacts with both mutant huntingtin protein (mHTT) and LC3B but not with wtHTT or irrelevant control proteins. LC3-mHTT-IN-AN1 reduces the levels of mHTT in an allele-selective manner in cultured Huntington disease (HD) mouse neurons.
|
-
- HY-N2481
-
|
Oroxylin A-7-O-glucuronide
Oroxyloside; Oroxylin A-7-O-β-D-glucuronide
|
Others
|
Neurological Disease
|
|
Oroxylin A-7-O-glucuronide (Oroxyloside; Oroxylin A-7-O-β-D-glucuronide) is a flavonoid glucuronide isolated from the dried root of Scutellaria baicalensis, with prolyl oligopeptidase (POP) inhibitory activity.
|
-
- HY-10895A
-
|
SB-334867 free base
SB334867A free base
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
Endocrinology
|
|
SB-334867 free base (SB334867A free base) is an excellent, selective and blood–brain barrier permeable orexin-1 (OX1) receptor antagonist, shows selectivity over OX2 (pKb=7.4), 100-fold over 5-HT2B, 5-HT2C with pKi values of 5.4 and 5.3, respectively. SB-334867 reduces ethanol consumption and inhibits the acquisition of morphine-induced sensitization to locomotor activity in vivo.
|
-
- HY-N6953
-
|
Garcinone D
|
STAT
Keap1-Nrf2
Reactive Oxygen Species
|
Neurological Disease
|
|
Garcinone D, a natural xanthone from mangosteen, promotes the proliferation of C17.2 neural stem cell. Garcinone D increases the protein levels of phosphorylated signal transducer and activator of transcription 3 (p-STAT3), Cyclin D1 and nuclear factor erythroid 2-related factor (Nrf2), heme oxygenase-1 (HO-1) in concentration- and time- dependent manners.
|
-
- HY-19835
-
|
LY2922470
|
GPR40
|
Metabolic Disease
|
|
LY2922470 is a potent, selective and orally available agonist of the G protein-coupled receptor 40 (GPR40), with EC50s of 7 nM, 1 nM and 3 nM for human GPR40, mouse GPR40 and rat GPR40, respectively. LY2922470 reduces glucose levels along with significant increases in insulin and GLP-1, is potential for the treatment of type 2 diabetes mellitus (T2DM).
|
-
- HY-13777
-
|
Zoledronic Acid
Zoledronate; CGP 42446; CGP42446A; ZOL 446
|
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
|
Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.
|
-
- HY-13777A
-
|
Zoledronic acid monohydrate
Zoledronate monohydrate; CGP 42446 monohydrate; CGP42446A monohydrate; ZOL 446 monohydrate
|
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
|
|
Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.
|
-
- HY-12614
-
|
AMG-1694
|
Glucokinase
|
Metabolic Disease
|
|
AMG-1694 is a potent glucokinase–glucokinase regulatory protein (GK-GKRP) disruptors and promotes the dissociation of the GK-GKRP complex with an IC50 of 7 nM, indirectly increasing GK enzymatic activity. AMG-1694 potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation. AMG-1694 normalizes blood glucose levels in several rodent models of diabetes and lowes blood glucose restricted to diabetic and not normoglycaemic animals.
|
-
- HY-N0407
-
|
Picroside I
6'-Cinnamoylcatalpol
|
STAT
|
Inflammation/Immunology
|
|
Picroside I is the major ingredient of Picrorhiza kurroa. Picrorhiza kurroa is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II. Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ.
|
-
- HY-115461
-
|
MID-1
|
Insulin Receptor
|
Metabolic Disease
|
|
MID-1 is a disruptor of MG53-IRS-1 (Mitsugumin 53-insulin receptor substrate-1) interaction. MID-1 disrupts molecular association of MG53 with IRS-1 and abolishes MG53-induced IRS-1 ubiquitination and degradation in skeletal muscle, leading to elevated IRS-1 expression level and increased insulin signaling and glucose uptake.
|
-
- HY-N2557
-
|
Euphorbia Factor L1
|
Apoptosis
|
Cancer
Cardiovascular Disease
|
|
Euphorbia Factor L1 is a diterpenoid from Euphorbia lathyris L., reduces the expression of Bcl-2, PI3K, AKT and mTOR protein and mRNA, upregulates cleaved caspase-9 and caspase-3 levels, buts shows no effect on pro-caspase-9 and pro-caspase-3. Euphorbia Factor L1 induces apoptosis, has anticancer, antiadipogenesis, antiosteoclastogenesis and multidrug resistance-modulating effect.
|
-
- HY-N0604
-
-
- 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-14604
-
|
Xaliproden hydrochloride
SR57746A; SR57746 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases.
|
-
- HY-N7087
-
|
Tulipalin A
α-Methylene butyrolactone
|
Drug Metabolite
|
|
|
Tulipalin A (α-Methylene butyrolactone) is a toxic glycoside isolated from the tulip bulbs. Tulipalin A is a causative allergen that induces Allergic contact dermatitides. Tulipalin A (α-Methylene butyrolactone) at low dose affects the functionality of immune cells, such as Jurkat T cells.
|
-
- HY-W006492
-
-
- HY-N7495
-
-
- HY-112057
-
-
- HY-14564A
-
|
GTS-21 dihydrochloride
DMXB-A; DMBX-anabaseine
|
nAChR
5-HT Receptor
|
Inflammation/Immunology
|
|
GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti‑inflammatory and cognition‑enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist.
|
-
- HY-106224A
-
|
Orexin A (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
|
-
- HY-136294
-
|
Cryptophycin 1
Cryptophycin A
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Cryptophycin 1 is a potent cytotoxic antimicrotubule agent which is isolated from Nostoc sp. Cryptophycin 1 can induce cells apoptosis, and exhibits antitumor activity and exceptional antiproliferative potency.
|
-
- HY-N2146
-
-
- HY-N0234
-
|
Bavachinin
7-O-Methylbavachin; Bavachinin A
|
Others
|
Inflammation/Immunology
|
|
Bavachinin(7-O-Methylbavachin) is a natural compound isolated from the Chinese herb Fructus Psoraleae;has potent anti-angiogenic activity.
|
-
- HY-N0541
-
|
Pseudoginsenoside F11
Ginsenoside A1
|
Endogenous Metabolite
|
Others
|
|
Pseudoginsenoside F11 (Ginsenoside A1), a component of Panax quinquefolium (American ginseng), has been demonstrated to antagonize the learning and memory deficits induced by scopolamine, morphine and methamphetamine in mice.
|
-
- HY-N4088
-
-
- HY-15978
-
|
P7C3-A20
|
Others
|
Neurological Disease
|
|
P7C3-A20 is a derivative of P7C3 with potent proneurogenic and neuroprotective activity. P7C3-A20 exerts an antidepressant-like effect. P7C3-A20 can cross the blood-brain barrier and therefore has the potential for brain injury treatment.
|
-
- HY-B0426A
-
-
- HY-B0515
-
-
- HY-100176
-
-
- HY-B0005
-
|
Toremifene citrate
Z-Toremifene citrate; NK 622; FC-1157a
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
Infection
|
|
Toremifene citrate (Z-Toremifene citrate) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-117482
-
|
BPN-15606
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance.
|
-
- HY-B0005A
-
|
Toremifene
Z-Toremifene; NK 622 free base; FC-1157a free base
|
Estrogen Receptor/ERR
|
Cancer
Infection
|
|
Toremifene (Z-Toremifene) is a second-generation selective estrogen-receptor modulator (SERM) in development for the prevention of osteoporosis. Toremifene also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC50 of 0.07 µM and 2.6 µM, respectively.
|
-
- HY-131183
-
|
PROTAC PD-1/PD-L1 degrader-1
|
PROTAC
PD-1/PD-L1
|
Inflammation/Immunology
|
|
PROTAC PD-1/PD-L1 degrader-1, a PD-1/PD-L1 degrader, inhibits PD-1/PD-L1 interaction with an IC50 of 39.2 nM. PROTAC PD-1/PD-L1 degrader-1 significantly restores the immunity repressed in a co-culture model of Hep3B/OS-8/hPD-L1 and CD3 T cells. PROTAC PD-1/PD-L1 degrader-1 moderately reduces the protein levels of PD-L1 in a lysosome-dependent manner.
|
-
- HY-109619
-
|
D4-abiraterone
Δ4-Abiraterone; CB-7627; Abiraterone D4A metabolite
|
Androgen Receptor
Cytochrome P450
|
Cancer
|
|
D4-abiraterone is a major metabolite of abiraterone. D4-abiraterone is an inhibitor of CYP17A1, 3b-hydroxysteroid dehydrogenase (3βHSD) and steroid-5a-reductase (SRD5A) and also an antagonist of androgen receptor.
|
-
- HY-106199
-
-
- HY-124873
-
|
SERCA2a activator 1
|
Calcium Channel
|
Cardiovascular Disease
|
|
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure.
|
-
- HY-B1384
-
|
Retinyl palmitate
Vitamin A palmitate; Retinol palmitate
|
Endogenous Metabolite
|
Others
|
|
Retinyl palmitate is an ester of Retinol and is the major form of vitamin A found in the epidermis. Retinyl palmitate has been widely used in pharmaceutical and cosmetic formulations.
|
-
- HY-101915
-
-
- HY-14336A
-
|
SB 271046 Hydrochloride
SB 271046A
|
5-HT Receptor
|
Neurological Disease
|
|
SB 271046 Hydrochloride (SB 271046A) is a potent, selective and orally active 5-HT6 receptor antagonist with pKi of 9.02, 8.55, and 8.81 for rat, pig and human, respectively. SB 271046 Hydrochloride is over 200 fold selective for the 5-HT6 receptor vs 55 other receptors, binding sites and ion channels. Anticonvulsant activity (EC50=0.16 μM).
|
-
- HY-101325
-
-
- HY-B1050
-
|
Gemifloxacin mesylate
SB-265805S; LB-20304a
|
Bacterial
|
Infection
|
|
Gemifloxacin mesylate is an oral broad-spectrum quinolone antibacterial agent, used in the treatment of acute bacterial exacerbation of chronic bronchitis, and mild-to-moderate pneumonia.
|
-
- HY-N0834
-
-
- HY-19995
-
-
- 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-N6686
-
|
Virginiamycin M1
Pristinamycin IIA; Ostreogrycin A
|
Bacterial
Antibiotic
|
Infection
|
|
Pristinamycin IIA (RP 12536) is a macrocyclic lactone peptolide antibiotic, derived from Streptomyces pristinaespiralis, which is a member of the streptogramin A group of antibiotics.
|
-
- HY-N0855
-
|
Alisol G
Alisol-G; 25-Anhydroalisol A
|
Others
|
Others
|
|
Alisol G is a natural product extracted from Rhizoma Alismatis.
|
-
- HY-B2209A
-
|
Hydroxocobalamin monohydrochloride
Vitamin B12a monohydrochloride
|
Others
|
Metabolic Disease
|
|
Hydroxocobalamin monohydrochloride (Vitamin B12a monohydrochloride) is an injectable naturally occurring form of vitamin B12 with a favorable adverse effect profile, used as a dietary supplement in the treatment of vitamin B12 deficiency including pernicious anemia.
|
-
- HY-19655
-
-
- HY-N0206
-
|
Ardisiacrispin A
Deglucocyclamin; LTS-4; Saxifragifolin B
|
Others
|
Cancer
|
|
Ardisiacrispin A (Deglucocyclamin) is a common triterpenoid saponin from Ardisia species. Ardisiacrispin A has similar biological properties with some triterpenoid saponins in A. crenata which is one of the species of genus Ardisia and exhibits cytotoxic effect on tumor cells, immunomodulatory and antiviral activities.
|
-
- HY-B0976A
-
|
Fenoterol hydrobromide
Th-1165a; Phenoterol hydrobromide
|
Adrenergic Receptor
|
Inflammation/Immunology
Endocrinology
|
|
Fenoterol hydrobromide (Th-1165a), a sympathomimetic agent, is a selective and orally active β2-adrenoceptor agonist. Fenoterol hydrobromide is an effective bronchodilator and can be used for bronchospasm associated with asthma, bronchitis and other obstructive airway diseases research.
|
-
- HY-113596
-
|
Acetyl Coenzyme A trisodium
Acetyl-CoA trisodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Acetyl Coenzyme A trisodium (Acetyl-CoA trisodium) is a central metabolic intermediate. Acetyl Coenzyme A trisodium is the actual molecule through which glycolytic pyruvate enters the tricarboxylic acid (TCA) cycle, is a key precursor of lipid synthesis, and is the sole donor of the acetyl groups for acetylation. Acetyl Coenzyme A trisodium acts as a potent allosteric activator of pyruvate carboxylase (PC).
|
-
- HY-101913
-
-
- HY-16940
-
|
24(S)-Hydroxycholesterol
24S-OHC; 24S-HC; Cerebrosterol
|
LXR
iGluR
Endogenous Metabolite
|
Metabolic Disease
|
|
24(S)-Hydroxycholesterol (24S-OHC), the major brain cholesterol metabolite, plays an important role to maintain homeostasis of cholesterol in the brain. 24(S)-Hydroxycholesterol (24S-OHC) is one of the most efficient endogenous LXR agonist known and is present in the brain and in the circulation at relatively high levels. 24(S)-Hydroxycholesterol (24S-OHC) is a very potent, direct, and selective positive allosteric modulator of NMDARs with a mechanism that does not overlapthat of other allosteric modulators.
|
-
- HY-10512
-
-
- HY-10965
-
|
Rolofylline
KW-3902
|
Adenosine Receptor
|
Neurological Disease
|
|
Rolofylline (KW-3902) is a potent, selective adenosine A1 receptor antagonist that is under development for the treatment of patients with acute congestive heart failure and renal impairment.
Rolofylline is metabolized primarily to the pharmacologically active M1-trans and M1-cis metabolites by cytochrome P450 (CYP450).
Rolofylline is alleviating the presynaptic dysfunction and restores neuronal activity as well as dendritic spine levels in vitro, is an interesting candidate to combat the hypometabolism and neuronal dysfunction associated with Tau-induced neurodegenerative diseases.
|
-
- HY-P2161
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TAK-683
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Others
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Cancer
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TAK-683 is a potent full KISS1 receptor (KISS1R) agonist (IC50=170 pM) with improved metabolic stability. TAK-683 is a nonapeptide metastin analog, exhibits agonistic activities to KISS1R with EC50 values of 0.96 nM and 1.6 nM for human and rat, respectively. TAK-683 depletes GnRH in the hypothalamus and reduces plasma FSH, LH, and testosterone levels in vivo, it has the potential for the study of hormone-dependent prostate cancer.
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- HY-136272
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- HY-14778
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- HY-14601
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- HY-A0167
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Gadopentetate dimeglumine
SH-L-451A; Gadopentetic acid dimeglumine salt
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Others
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Cancer
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Gadopentetate dimeglumine (SH-L-451A) is used in combination with magnetic resonance imaging (MRI) to allow blood vessels, organs, and other non-bony tissues to be seen more clearly on the MRI.
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- HY-U00321
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- HY-B0723S
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Ospemifene D4
FC-1271a D4
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Estrogen Receptor/ERR
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Cancer
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Ospemifene D4 (FC-1271a D4) is a deuterium labeled Ospemifene. Ospemifene is a selective and orally active estrogen receptor modulator for the prevention of osteoporosis with IC50 values of 827 nM and 1633 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene has bone-sparing, antitumor, and cholesterol-lowering effects.
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- HY-100290
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- HY-N0056
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- HY-136621
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- HY-N0411
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β-Carotene
Provitamin A; beta-Carotene
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Endogenous Metabolite
ROS
Apoptosis
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Cancer
Metabolic Disease
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β-Carotene (Provitamin A), a carotenoid compound, is a naturally-occurring vitamin A precursor. β-Carotene is a modulator of reactive oxygen species (ROS), with antioxidant and antiinflammatory activities. β-Carotene may serve as an antioxidant or as a prooxidant, depending on its intrinsic properties as well as on the redox potential of the biological environment in which it acts. β-Carotene induces breast cancer cells apoptosis, with anticancer activities.
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- HY-B0284S
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- HY-136273
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- HY-N0560
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- HY-P0197
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- HY-U00286
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- HY-124874
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(rel)-Asperparaline A
(rel)-Aspergillimide; (rel)-VM55598
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nAChR
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Neurological Disease
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(rel)-Asperparaline A ((rel)-Aspergillimide), an anthelmintic metabolite, is isolated from okara that has been fermented with Aspergillus japonicas JV-23. (rel)-Asperparaline A is also a potent and selective antagonist of nAChR. (rel)-Asperparaline A exhibits paralytic activity in silk worms.
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- HY-B0933
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Gadoteridol
SQ-32692; Gd-HP-DO3A
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Others
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Others
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Gadoteridol is a gadolinium-based MRI contrast agent, used in the imaging of the central nervous system.
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- HY-136274
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