Search Result
Results for "All natural aromatase Inhibitors" in MCE Product Catalog:
9635
Inhibitors & Agonists
24
Biochemical Assay Reagents
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-W004500
-
|
All-trans-retinal
|
Endogenous Metabolite
|
Others
|
|
All-trans-retinal is a one of the major vitamin A metabolites in the retina. In physiological conditions, all-trans-RAL is regenerated to the visual chromophore, 11-cis-retinal.
|
-
- HY-13632
-
|
Exemestane
FCE 24304; EXE
|
Aromatase
|
Cancer
Endocrinology
|
|
Exemestane (FCE 24304) is a selective, irreversible and orally active steroidal aromatase inhibitor with IC50s of 30 nM and 40 nM for human placental and rat ovarian aromatase, respectively. Exemestane can be used for hormone-dependent breast cancer research.
|
-
- HY-14248
-
|
Letrozole
CGS 20267
|
Aromatase
Autophagy
|
Cancer
|
|
Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer.
|
-
- HY-N7495
-
-
- HY-107494A
-
-
- HY-N0292
-
|
Oleuropein
|
PPAR
Apoptosis
Aromatase
|
Cancer
Inflammation/Immunology
Cardiovascular Disease
|
|
Oleuropein, found in olive leaves and oil, exerts antioxidant, anti-inflammatory and anti-atherogenic effects through direct inhibition of PPARγ transcriptional activity. Oleuropein induces apoptosis in breast cancer cells via the p53-dependent pathway and through the regulation of Bax and Bcl2 genes. Oleuropein also inhibits aromatase.
|
-
- HY-N0716
-
-
- HY-U00439
-
-
- HY-136063
-
|
Mefentrifluconazole
|
Fungal
Cytochrome P450
|
Infection
|
|
Mefentrifluconazole is a novel azole derivative and used as an agrochemical broad-spectrum antifungal agent. Mefentrifluconazole is a potent, selective and orally active fungal CYP51 (Kd= 0.5 nM) inhibitor, but shows less inhibitory activity on human aromatase (IC50=0.92 μM).
|
-
- HY-17577
-
-
- HY-14274
-
|
Anastrozole
ZD1033
|
Aromatase
|
Cancer
|
|
Anastrozole is a potent, highly selective aromatase inhibitor, which inhibits human placental aromatase with an IC50 of 15 nM.
|
-
- HY-N0116
-
|
Hematoxylin
natural Black 1; Haematoxylin
|
Amyloid-β
|
Others
|
|
Hematoxylin (Natural Black 1), a naturally occurring flavonoid compound derived from the logwood tree, Haematoxylon campechianum. Hematoxylin is a nuclear stain in histology and is also a potent Aβ42 fibrillogenesis inhibitor with an IC50 of 1.6 µM.
|
-
- HY-136175
-
|
SNDX-5613
|
Epigenetic Reader Domain
|
Cancer
|
|
SNDX-5613 is a potent and specific Menin-MLL inhibitor with a binding Ki of 0.149 nM and a cell based IC50 of 10-20 nM. SNDX-5613 can be used for the research of MLL-rearranged (MLL-r) acute leukemias, including acute lymphoblastic leukemia (ALL) and acute myeloid leukemia (AML).
|
-
- 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-N6609
-
-
- HY-A0143
-
-
- HY-U00176
-
-
- HY-15087A
-
-
- HY-136064
-
-
- HY-N7609
-
-
- HY-N6046
-
-
- HY-N7128
-
|
Flavanone
|
Aromatase
|
Cancer
|
|
Flavanone is a naturally occurring flavone. Flavanone has inhibitory activity for human estrogen synthetase (aromatase).
|
-
- HY-N2318
-
-
- HY-N5012
-
|
Eurycomanone
Pasakbumin A
|
Others
|
Endocrinology
|
|
Eurycomanone could increases spermatogenesis by inhibiting the activity of phosphodiesterase and aromatase in steroidogenesis.
|
-
- HY-N9326
-
|
Uralenol
|
Phosphatase
|
Metabolic Disease
|
|
Uralenol is a natural PTP1B inhibitor (IC50=21. 5 μM) from Broussonetia papyrifera. PTP1B have been shown to play a major role in the dephosphorylation of the insulin receptor in many cellular and biochemical studies.
|
-
- 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-B0845
-
|
Prochloraz
BTS 40542
|
Fungal
Estrogen Receptor/ERR
Androgen Receptor
Aryl Hydrocarbon Receptor
|
Infection
|
|
Prochloraz is an imidazole antifungal that inhibits ergosterol biosynthesis via inhibition of the cytochrome P450-dependent 14α-demethylation of lanosterol, which results in disruption of the fungal cell membrane and cell death. Prochloraz inhibits human placenta microsomal aromatase in vitro (IC50=40 nM). Prochloraz also acts as an antagonist of the estrogen receptor (ER) and androgen receptor (AR) (IC50s=25 μM and 4 μM, respectively) as well as activates the aryl hydrocarbon receptor (AhR; EC50=1 μM).
|
-
- HY-N0005
-
|
Curcumin
Diferuloylmethane; natural Yellow 3; Turmeric yellow
|
Histone Acetyltransferase
Epigenetic Reader Domain
Keap1-Nrf2
Autophagy
Mitophagy
Influenza Virus
Ferroptosis
|
Cancer
|
|
Curcumin (Diferuloylmethane), a natural phenolic compound, is a p300/CREB-binding protein-specific inhibitor of acetyltransferase, represses the acetylation of histone/nonhistone proteins and histone acetyltransferase-dependent chromatin transcription. Curcumin shows inhibitory effects on NF-κB and MAPKs, and has diverse pharmacologic effects including anti-inflammatory, antioxidant, antiproliferative and antiangiogenic activities. Curcumin induces stabilization of Nrf2 protein through Keap1 cysteine modification.
|
-
- HY-79635
-
|
Methyl indole-3-carboxylate
|
Bacterial
|
Infection
|
|
Methyl indole-3-carboxylate is a natural product isolated from Sorangium cellulosum strain Soce895. Methyl indole-3-carboxylate shows a weak activity against the Gram-positive Nocardia sp with a MIC value of 33.33 μg/mL.
|
-
- 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-112542
-
|
Nemadectin
CL-287088; LL-F28249 α
|
Parasite
Antibiotic
|
Infection
|
|
Nemadectin (CL-287088), an orally active broad-spectrum endectocide, is highly efficacious against natural infections of all the major canine gastrointestinal helminthes. Anthelmintic activity.
|
-
- HY-N1438
-
|
Hydroxygenkwanin
7-O-Methylluteolin
|
Others
|
Cancer
|
|
Hydroxygenkwanin (7-O-Methylluteolin), a natural flavonoid compound, is one of the main components of Lilac Daphne. Hydroxygenkwanin has anti-oxidant ability, anti-glioma ability and anticancer effect.
|
-
- HY-125833
-
|
Alpha-Naphthoflavone
|
Aromatase
|
Cancer
|
|
Alpha-Naphthoflavone is a synthetic flavonoid, acts as a potent and competitive aromatase inhibitor with an IC50 and a Ki of 0.5 and 0.2 μM, respectively.
|
-
- HY-131005
-
-
- HY-N2302
-
-
- 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-130640
-
-
- HY-108485
-
|
Damnacanthal
|
Src
Apoptosis
Fungal
|
Cancer
Infection
Inflammation/Immunology
|
|
Damnacanthal is an anthraquinone isolated from the root of Morinda citrifolia. Damnacanthal is a highly potent, selective inhibitor of p56 lck tyrosine kinase activity. Natural Damnacanthal inhibits p56 lck autophosphorylation and phosphorylation of exogenous substrates with IC50s of 46 nM and 220 nM, respectively. Damnacanthal is a potent inducer of apoptosis with anticancer activity. Damnacanthal also has antinociceptive, anti-inflammatory effects in mice and anti-fungal activity against Candida albicans.
|
-
- HY-W012653
-
|
4'-Methylacetophenone
|
Others
|
Others
|
|
4′-methylacetophenone can be used as a fragrance material. 4′-Methylacetophenone is wildly occurs in volatile compounds in food and in some natural complex substances (NCS).
|
-
- HY-N0005S
-
-
- HY-18258
-
-
- HY-18719B
-
-
- HY-18719E
-
-
- 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-41404
-
|
Piperonylic acid
|
Cytochrome P450
|
Infection
|
|
Piperonylic acid is a natural molecule bearing a methylenedioxy function that closely mimics the structure of trans-cinnamic acid. Piperonylic Acid is a selective, mechanism-based inactivator of the trans-cinnamate 4-Hydroxylase.
|
-
- HY-N3517
-
-
- HY-N3516
-
-
- HY-121879
-
-
- HY-N0325
-
|
DL-Methionine
|
Parasite
|
Infection
Inflammation/Immunology
|
|
DL-Methionine is an essential amino acid containing sulfur with oxidative stress defense effects. DL-Methionine can be used for animal natural feed. DL-Methionine also kills H. rostochiensis on potato plants.
|
-
- HY-N7591
-
|
Millepachine
|
Apoptosis
|
Cancer
|
|
Millepachine is a bioactive natural chalcone from Chinese herbal medicine Millettia pachycarpa Benth, exhibits strong antitumor effects against numerous human cancer cells both in vitro and in vivo.
|
-
- HY-13022
-
-
- HY-13022A
-
|
CC-401
|
JNK
|
Cancer
|
|
CC-401 is a potent inhibitor of all three forms of JNK with Ki of 25 to 50 nM.
|
-
- HY-B1960
-
-
- HY-N8405
-
|
Isolimonexic acid
|
Aromatase
|
Cancer
|
|
Isolimonexic acid is a limonoid isolated from lemon (Citrus lemon L. Burm) seed, has anti-cancer and anti-aromatase (IC50=25.60 μM) properties.
|
-
- HY-135235
-
|
Cysteine thiol probe
|
Others
|
Others
|
|
Cysteine Thiol Probe is a thiol-based probe designed to label electrophilic natural products. Cysteine Thiol Probe possesses each of the characteristics of an ideal pharmacophore probe, and has a chromophore. Cysteine Thiol Probe is capable of engaging enone-, β-lactam-, and β-lactone-based electrophilic metabolites.
|
-
- HY-W017212
-
|
Methyl cinnamate
Methyl 3-phenylpropenoate
|
Tyrosinase
Bacterial
AMPK
|
Infection
Metabolic Disease
|
|
Methyl cinnamate (Methyl 3-phenylpropenoate), an active component of Zanthoxylum armatum, is a widely used natural flavor compound. Methyl cinnamate (Methyl 3-phenylpropenoate) possesses antimicrobial activity and is a tyrosinase inhibitor that can prevent food browning. Methyl cinnamate (Methyl 3-phenylpropenoate) has antiadipogenic activity through mechanisms mediated, in part, by the CaMKK2-AMPK signaling pathway.
|
-
- HY-19373
-
-
- HY-P0244
-
-
- HY-P0244A
-
-
- HY-101541
-
-
- HY-12808
-
-
- 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-W012037
-
|
8-Hydroxyquinoline hemisulfate
8-Quinolinol hemisulfate
|
Bacterial
Antibiotic
|
Infection
|
|
8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
|
-
- HY-50730
-
|
Asparagusic acid
|
Parasite
|
Infection
|
|
Asparagusic acid is a sulfur-containing flavor component produced by asparagus plants, with anti-parasitic effect. Asparagusic acid is a plant growth inhibitor.
|
-
- HY-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-14802
-
|
Talarozole (R enantiomer)
(R)-Talarozole
|
Cytochrome P450
|
Cancer
|
|
Talarozole R enantiomer is a potent and selective inhibitor of cytochrome P450 26-mediated breakdown of endogenous all-trans retinoic acid for the treatment of psoriasis and acne.
|
-
- HY-N2022
-
|
Castanospermine
|
Glucosidase
|
Cancer
|
|
Castanospermine inhibits all forms of α- and β-glucosidases, especially glucosidase l (required for glucoprotein processing by transfer of mannose and glucose from asparagine-linked lipids).
|
-
- HY-N0149
-
-
- HY-D0889
-
-
- 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-N1201
-
-
- HY-P9906
-
|
Bevacizumab
Anti-Human VEGF, Humanized Antibody
|
VEGFR
|
Cancer
|
|
Bevacizumab, a humanized monoclonal antibody, specifically binds to all VEGF-A isoforms with high affinity.
|
-
- 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-15981
-
-
- HY-B0134
-
-
- 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-113159
-
-
- HY-16911
-
|
AFN-1252
API-1252; Debio 1452
|
Bacterial
Antibiotic
|
Infection
|
|
AFN-1252(Debio 1452) is a potent inhibitor of enoyl-acyl carrier protein reductase (FabI), inhibited all clinical isolates of Staphylococcus aureus and Staphylococcus epidermidis at concentrations of ≤0.12 μg/ml.
|
-
- 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-136092
-
|
Androsta-1,4,6-triene-3,17-dione
|
Aromatase
|
Endocrinology
Neurological Disease
|
|
Androsta-1,4,6-triene-3,17-dione is a lipophilic and specific aromatase inhibitor with a Ki of 0.18 μM. Androsta-1,4,6-triene-3,17-dione inhibits estrogen biosynthesis and shows antifertility effects. Androsta-1,4,6-triene-3,17-dione induces impairment of spatial memory.
|
-
- HY-121324
-
|
Prometryn
|
Others
|
Others
|
|
Prometryn could improves the control of all weed species and increased lint yield compared with the systems.
|
-
- 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-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-N1377
-
|
Nevadensin
|
Bacterial
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Nevadensin is a naturally occurring selective inhibitor of human carboxylesterase 1 (hCE1) with an IC50 of 2.64 μM. Nevadensin has a variety of pharmacological effects such as anti-mycobacterium tuberculosis activities, antitussive, anti-inflammatory and anti-hypertensive.
|
-
- HY-12866
-
|
Larotrectinib
LOXO-101; ARRY-470
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib (LOXO-101) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-B1216
-
-
- HY-N0726
-
|
Dracorhodin perchlorate
Dracohodin perochlorate
|
Apoptosis
|
Cancer
|
|
Dracorhodin perchlorate (Dracohodin perochlorate) is a natural product extracted from a natural medicine Dragon's blood. Dracorhodin perchlorate inhibits cell proliferation and induces cell cycle arrest and apoptosis.
|
-
- HY-128607
-
|
Mcl1-IN-9
|
Bcl-2 Family
|
Cancer
|
|
Mcl1-IN-9 is a potent myeloid cell leukemia-1 (Mcl-1) Inhibitor with an IC50 of 446 nM in reengineered BCR-ABL+ B-ALL cells and a Ki of 0.03 nM.
|
-
- HY-106019C
-
|
Liarozole dihydrochloride
R75251 dihydrochloride
|
Cytochrome P450
|
Cancer
Inflammation/Immunology
|
|
Liarozole dihydrochloride (R75251; R85246) is a cytochrome P450 (CYP450) dependent inhibitor, orally active, it also a potent inhibitor of estrogen (via inhibition of aromatase) and testicular androgen synthesis (inhibition of 17 ,20-lyase). Liarozole dihydrochloride prevents the catabolism of retinoic acid via inhibition of 4-hydroxylase and exhibits retinoid sparing and retinoid-mimetic effects in vivo. Liarozole dihydrochloride is an imidazole derivative; it is being investigated as a non-hormonal agent in prostate cancer and in the treatment of various other cancers and skin disorders.
|
-
- HY-N7039
-
-
- HY-111904
-
|
EHMT2-IN-2
|
Histone Methyltransferase
|
Cancer
|
|
EHMT2-IN-2 is a potent EHMT inhibitor, with IC50s of all <100 nM for EHMT1 peptide, EHMT2 peptide and cellular EHMT2. Used in the research of blood disease or cancer.
|
-
- HY-N0243
-
-
- HY-N0077
-
|
Ginkgolic Acid
Ginkgolic acid (15:1); Ginkgolic acid I; Romanicardic acid
|
E1/E2/E3 Enzyme
|
Cancer
|
|
Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
|
-
- HY-15583
-
-
- HY-W017770
-
|
S-Adenosyl-L-methionine disulfate tosylate
Ademetionine disulfate tosylate; S-Adenosyl methionine disulfate tosylate; AdoMet disulfate tosylate
|
Others
|
Neurological Disease
|
|
S-Adenosyl-L-methionine disulfate tosylate (Ademetionine disulfate tosylate) is the principal biological methyl donor synthesized in all mammalian cells but most abundantly in the liver.
|
-
- HY-12824
-
|
RNPA1000
|
Antibiotic
Bacterial
|
Infection
|
|
RNPA1000, an antibiotic, is a potent RnpA inhibitor and inhibits RnpA-mediated cellular RNA degradation. RNPA1000 inhibits tRNA maturation with an IC50 of 175 μM. RNPA1000 displays broad-spectrum antimicrobial activities and inhibits staphylococcal and all Gram-positive bacterial pathogens activity.
|
-
- HY-136522
-
|
S2116
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S2116, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2116 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2116 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2116 significantly retardes the growth of T-ALL cells in xenotransplanted mice.
|
-
- 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-Y0258
-
-
- HY-107383
-
-
- HY-113325
-
|
NADP
|
Endogenous Metabolite
|
Others
|
|
NADP is nicotinamide adenine dinucleotide phosphate, acting as a key cofactor for electron transfer in the metabolism of all organisms, being alternately oxidized (NADP +) and reduced (NADPH).
|
-
- HY-18732A
-
|
L-NMMA acetate
Tilarginine acetate; Methylarginine acetate
|
NO Synthase
|
Cardiovascular Disease
|
|
L-NMMA acetate is a nitric oxide synthase inhibitor of all NOS isoforms including NOS1, NOS2, and NOS3. The Ki values for nNOS (rat), eNOS (human), and iNOS (mouse) are approximately 0.18, 0.4, and 6 µM, respectively.
|
-
- HY-120548
-
|
KBU2046
|
Others
|
Cancer
|
|
KBU2046 is an oral, highly selective inhibitor of cell motility and cell invasion in vitro. KBU2046 binds chaperone heterocomplexes, selectively alters binding of client proteins that regulate motility, and lacks all of the hallmarks of classical HSP90 inhibitors. KBU2046 inhibits cancer metastasis and prolongs life.
|
-
- HY-N1502
-
|
Carboxyatractyloside
Gummiferin
|
Others
|
Cancer
|
|
Carboxyatractyloside is a toxic natural product, acts as an inhibitor of ADP/ATP carrier, inhibits mitochondrial ADP/ATP transport.
|
-
- HY-B0183
-
-
- HY-N0913
-
|
Manninotriose
|
Others
|
Others
|
|
Manninotriose is a novel and important player in the RFO(Raffinose family oligosaccharides) metabolism of red dead deadnettle; potential to improve the side effects of MTX for ALL treatment.
|
-
- HY-N2522
-
-
- HY-12866A
-
|
Larotrectinib sulfate
LOXO-101 sulfate; ARRY-470 sulfate
|
Trk Receptor
Apoptosis
|
Cancer
|
|
Larotrectinib sulfate (LOXO-101 sulfate; ARRY-470 sulfate) is an ATP-competitive oral, selective inhibitor of the tropomyosin-related kinase (TRK) family receptors, with low nanomolar 50% inhibitory concentrations against all three isoforms (TRKA, B, and C).
|
-
- HY-N0859
-
|
Schisanhenol
Schizanhenol; Gomisin-K3
|
Others
|
Cancer
|
|
Schisanhenol is a natural compound solated from Schisandra rubriflora; UGT2B7 UDP-glucuronosyltransferases inhibitor.
|
-
- HY-B0216
-
-
- HY-14817
-
-
- HY-P1486
-
-
- 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-N2033
-
-
- HY-128602
-
|
c-Kit-IN-2
|
c-Kit
|
Cancer
|
|
c-Kit-IN-2 is a c-KIT inhibitor with an IC50 of 82 nM, shows superior antiproliferative activities against all the three GIST cell lines, GIST882, GIST430, and GIST48, with GI50s of 3, 1, and 2 nM, respectively.
|
-
- HY-N0168
-
-
- HY-A0210
-
-
- 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-136523
-
|
S2157
|
Histone Demethylase
Apoptosis
|
Cancer
|
|
S2157, a N-alkylated tranylcypromine (TCP) derivative, is a potent lysine-specific demethylase 1 (LSD1) inhibitor. S2157 increases H3K9 methylation and reciprocal H3K27 deacetylation at super-enhancer regions. S2157 induces apoptosis in TCP-resistant T-cell acute lymphoblastic leukemia (T-ALL) cells by repressing transcription of the NOTCH3 and TAL1 genes. S2157 efficiently pass through the blood-brain barrier and can almost completely eradicate CNS leukemia in mice transplanted with T-ALL cells.
|
-
- HY-111791
-
|
ACY-1083
|
HDAC
|
Cancer
|
|
ACY-1083 is a selective and brain-penetrating HDAC6 inhibitor with an IC50 of 3 nM and is 260-fold more selective for HDAC6 than all other classes of HDAC isoforms. ACY-1083 effectively reverses chemotherapy-induced peripheral neuropathy.
|
-
- HY-B0183A
-
-
- HY-N0184A
-
-
- HY-N1950
-
|
Hispidulin
Dinatin
|
Pim
|
Cancer
|
|
Hispidulin is a natural flavone with a broad spectrum of biological activities. Hispidulin is a Pim-1 inhibitor with an IC50 of 2.71 μM.
|
-
- HY-N2392
-
-
- HY-N0125
-
-
- HY-N1405
-
|
Cucurbitacin I
Elatericin B; JSI-124; NSC-521777
|
STAT
JAK
|
Cancer
|
|
Cucurbitacin I is a natural selective inhibitor of JAK2/STAT3, with potent anti-cancer activity.
|
-
- HY-N2182
-
-
- HY-12949
-
|
ML204
|
TRP Channel
|
Neurological Disease
|
|
ML204 is a potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-11012
-
|
TDZD-8
GSK-3β Inhibitor I; NP 01139
|
GSK-3
|
Cancer
|
|
TDZD-8 is an inhibitor of GSK-3β, with an IC50 of 2 μM; TDZD-8 shows less potent activities against Cdk-1/cyclin B, CK-II, PKA, and PKC, with all IC50s of >100 μM.
|
-
- HY-120508
-
|
Pivanex
AN-9; Pivalyloxymethyl butyrate
|
HDAC
Bcr-Abl
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Pivanex (AN-9), a derivative of Butyric acid, is an orally active HDAC inhibitor. Pivanex down-regulates bcr-abl protein and enhances apoptosis. Pivanex has antimetastic and antiangiogenic properties.
|
-
- HY-N2181
-
|
Acetylshikonin
|
Cytochrome P450
AChE
|
Cancer
Inflammation/Immunology
|
|
Acetylshikonin, derived from the root of Lithospermum erythrorhizon, has anti-cancer and antiinflammation activity. Acetylshikonin is a non-selective cytochrome P450 inhibitor against all P450s (IC50 values range from 1.4-4.0 μM). Acetylshikonin is an AChE inhibitor and exhibits potent antiapoptosis activity.
|
-
- HY-N0853
-
-
- HY-N0935
-
-
- HY-N0788
-
-
- HY-N0787
-
-
- HY-N0915
-
-
- HY-N0426
-
-
- HY-N0916
-
-
- HY-N0321
-
-
- HY-N0410
-
-
- HY-12949A
-
|
ML204 hydrochloride
|
TRP Channel
|
Neurological Disease
|
|
ML204 hydrochloride is a novel, potent, selective TRPC4/TRPC5 channel inhibitor, with at least 19-fold selectivity against TRPC6 and no appreciable effect on all other TRP channels, nor on voltage-gated sodium, potassium, or Ca 2+ channels.
|
-
- HY-U00189
-
-
- HY-N0867
-
-
- HY-N1765
-
-
- HY-N0862
-
-
- HY-115475
-
|
SW-100
|
HDAC
|
Neurological Disease
|
|
SW-100, a selective histone deacetylase 6 (HDAC6) inhibitor with an IC50 of 2.3 nM, shows at least 1000-fold selectivity for HDAC6 relative to all other HDAC isozymes. SW-100 displays a significantly improved ability to cross the blood-brain-barrier.
|
-
- HY-W004260
-
|
Arachidic acid
Icosanoic acid
|
Endogenous Metabolite
|
Others
|
|
Arachidonic acid (Icosanoic acid), a long-chain fatty acid, is present in all mammalian cells, typically esterified to membrane phospholipids, and is one of the most abundant polyunsaturated fatty acids present in human tissue.
|
-
- HY-14608
-
-
- HY-N0856
-
|
Alisol C 23-acetate
23-O-Acetylalisol C; Alisol C monoacetate
|
Others
|
Cardiovascular Disease
|
|
Alisol C 23-acetate, a natural product extracted from Alisma orientale, can significantly and strongly inhibit DTH response after oral administration.
|
-
- HY-N7207
-
-
- HY-N0237
-
-
- HY-N0457
-
-
- 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-14608A
-
-
- HY-N1369
-
|
Menthol
|
Others
|
Neurological Disease
|
|
Menthol is a natural analgesic compound. Menthol could cause a feeling of coolness due to stimulation of ‘cold’ receptors by inhibiting Ca ++ currents of neuronal membranes.
|
-
- HY-N0174
-
|
Cryptotanshinone
Cryptotanshinon; Tanshinone c
|
STAT
Autophagy
|
Cancer
|
|
Cryptotanshinone is a natural compound extracted from the root of Salvia miltiorrhiza Bunge that shows antitumor activities. Cryptotanshinone inhibits STAT3 with an IC50 of 4.6 μM.
|
-
- HY-N0054
-
-
- HY-N3033
-
-
- HY-100580
-
|
Asaraldehyde
Asaronaldehyde; Asaraldehyde; 2,4,5-trimethoxy-Benzaldehyde
|
COX
|
Inflammation/Immunology
|
|
Asarylaldehyde is a natural COX-2 inhibitor, which isolated from carrot (Daucus carota L.) seeds significantly inhibits cyclooxygenase II (COX-2) activity at IC50 value 100 μg/mL.
|
-
- HY-N0881
-
-
- HY-W012185
-
-
- HY-N1484
-
-
- HY-N0561
-
-
- HY-N0433
-
-
- HY-114672
-
|
MBCQ
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
MBCQ is a potent and selective cGMP-specific phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ lacks inhibitory activity toward other PDE isozymes (all IC50s>100 μM). MBCQ dilates coronary arteries via specific inhibition of cGMP-PDE.
|
-
- 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-N4317
-
|
Ethoxysanguinarine
|
Apoptosis
|
Cancer
|
|
Ethoxysanguinarine is a benzophenanthridine alkaloid natural product that is mainly found in Macleaya cordata. Ethoxysanguinarine inhibits viability and induces apoptosis of colorectal cancer cells by inhibiting protein phosphatase 2A (CIP2A).
|
-
- HY-N0696
-
|
Sipeimine
Imperialine
|
Others
|
Others
|
|
Sipeimine is a natural product isolated from Fritillaria ussuriensis.
|
-
- HY-N0257
-
-
- HY-113268
-
-
- HY-15733
-
|
Lucidin
NSC 30546
|
Others
|
Cancer
|
|
Lucidin (NSC 30546) is a natural component of Rubia tinctorum L.
|
-
- HY-N4101
-
-
- HY-133642
-
-
- HY-N2476
-
-
- HY-N0843
-
-
- HY-N0560
-
-
- HY-N4234
-
-
- HY-N0772
-
-
- HY-N0434
-
-
- HY-N1387
-
-
- HY-N9315
-
-
- HY-N6860
-
|
Lucidenic acid C
|
MMP
|
Cancer
|
|
Lucidenic acid C is a natural compound isolated from Ganoderma lucidum, inhibits PMA-induced MMP-9 activity, with anti-invasive effect on hepatoma cells.
|
-
- HY-100765
-
|
BI-0252
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
|
-
- HY-N6903
-
-
- HY-113440
-
-
- HY-N0668
-
|
Rubusoside
|
Others
|
Others
|
|
Rubusoside is a natural sweetener and a solubilizing agent with antiangiogenic and antiallergic properties.
|
-
- HY-N6817
-
-
- HY-N0855
-
|
Alisol G
Alisol-G; 25-Anhydroalisol A
|
Others
|
Others
|
|
Alisol G is a natural product extracted from Rhizoma Alismatis.
|
-
- HY-N0213
-
-
- HY-N1118
-
-
- HY-Y0585
-
-
- HY-N4325
-
-
- HY-N2469
-
-
- HY-N0144
-
-
- HY-N0168A
-
-
- HY-13595
-
|
Chrysophanol
Chrysophanic acid
|
EGFR
|
Cancer
|
|
Chrysophanol (Chrysophanic acid) is a natural anthraquinone, which inhibits EGF-induced phosphorylation of EGFR and suppresses activation of AKT and mTOR/p70S6K.
|
-
- HY-N6985
-
|
Baccatin III
|
Others
|
Cancer
|
|
Baccatin III is a natural product isolated from Pacific yew tree and related species. Baccatin III reduces tumor progression by inhibiting the accumulation and suppressive function of MDSCs.
|
-
- HY-N0086
-
-
- HY-21088
-
-
- HY-18061
-
|
Ochromycinone
(Rac)-STA-21
|
STAT
Bacterial
|
Cancer
Infection
|
|
Ochromycinone ((Rac)-STA-21) is a natural antibiotic and a STAT3 inhibitor. Ochromycinone can inhibits STAT3 DNA binding activity, STAT3 dimerization. Ochromycinone has anticancer and antimicrobial activity.
|
-
- HY-N1455
-
|
Falcarinol
Panaxynol; Carotatoxin
|
HSP
|
Cancer
|
|
Falcarinol (Panaxynol) is a natural, orally active Hsp90 inhibitor targeting both the N-terminal and C-terminal of Hsp90 with limited toxicities. Falcarinol (Panaxynol) induces apoptosis.
|
-
- 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-B1030
-
|
Lanatoside C
|
Autophagy
Enterovirus
|
Cardiovascular Disease
Cancer
|
|
Lanatoside C is a cardiac glycoside, can be used in the treatment of congestive heart failure and cardiac arrhythmia.Lanatoside C has an IC50 of 0.19 μM for dengue virus infection in HuH-7 cells. Lanatoside C can effectively inhibit all four serotypes of dengue virus, flavivirus Kunjin, alphavirus Chikungunya, Sindbis virus and the human enterovirus 71.
|
-
- HY-138061
-
|
DENV-IN-2
|
DNA/RNA Synthesis
|
Infection
|
|
DENV-IN-2 is a potent dengue viral replication inhibitor extracted from patent WO2018215315A1, compound 6AB, has an EC50 of 0.016 nM. DENV-IN-2 shows high potent activity against all four serotypes of the Dengue virus with EC50s ranging from 0.013 to 0.029 nM.
|
-
- HY-137892
-
|
GSK620
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
GSK620 is a potent and orally active pan-BD2 inhibitor with excellent broad selectivity, developability and in vivo oral pharmacokinetics. GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fold selectivity over all other bromodomains. GSK620 shows an anti-inflammatory phenotype in human whole blood.
|
-
- HY-108472
-
-
- HY-N3841
-
|
ε-Viniferin
epsilon-Viniferin
|
Cytochrome P450
|
Inflammation/Immunology
|
|
ε-Viniferin, the dimer of Resveratrol and isolated from Vitis vinifera, displays a potent inhibitory for all the CYP activities, with Ki values from 0.5-20 μM. ε-Viniferin possesses potent antioxidant capacity.
|
-
- HY-N0046
-
-
- HY-N0167
-
-
- HY-N0597
-
|
Panaxatriol
|
Others
|
Others
|
|
Panaxatriol is a natural product that can relieve myelosuppression induced by radiation injury.
|
-
- HY-N3524
-
-
- HY-113293A
-
-
- HY-N7704
-
-
- HY-N0156
-
-
- HY-N1366
-
|
Herniarin
7-Methoxycoumarin; Methyl umbelliferyl ether
|
Others
|
Cancer
|
|
Herniarin is a natural coumarin occurs in some flowering plants, with antitumor effect.
|
-
- HY-N0796
-
-
- HY-N0879
-
-
- HY-N5027
-
|
Oxyberberin
Berlambine; 8-Oxoberberine; Ketoberberine
|
Others
|
Infection
|
|
Berlambine is a natural alkaloid isolated from many plants.
|
-
- HY-N1958
-
-
- HY-N2285
-
-
- HY-N6930
-
-
- HY-N0210
-
-
- HY-N0853A
-
-
- HY-N6907
-
-
- HY-N6859
-
-
- HY-N7037
-
-
- HY-N0900
-
-
- 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-N0737
-
-
- HY-N4296
-
-
- HY-N0442
-
-
- HY-N0212
-
|
Peimine
Verticine; Dihydroisoimperialine
|
Others
|
Inflammation/Immunology
|
|
Peimine(Dihydroisoimperialine; Verticine) is a natural compound with good anti-inflammatory effects in vivo.
|
-
- HY-N0519
-
|
Calycosin
Cyclosin
|
Apoptosis
|
Cancer
|
|
Calycosin (Cyclosin) is a natural active compound with anti-oxidative and anti-inflammation activity.
|
-
- HY-N7257A
-
-
- HY-N2440
-
-
- HY-N7257
-
-
- HY-N6912
-
-
- HY-N2186
-
-
- HY-N2161
-
-
- HY-N1155
-
-
- HY-N7522
-
-
- HY-N2559
-
-
- HY-N2089
-
-
- HY-N0871
-
-
- HY-N0260
-
-
- HY-N7250
-
-
- HY-N6915
-
-
- HY-N0868
-
-
- HY-N1234
-
-
- HY-119931
-
-
- HY-100233
-
|
IQ-1S free acid
|
JNK
|
Cancer
Inflammation/Immunology
|
|
IQ-1S free acid is a prospective inhibitor of NF-κB/activating protein 1 (AP-1) activity with an IC50 of 2.3±0.41 μM. IQ-1S free acid has binding affinity (Kd values) in the nanomolar range for all three JNKs with Kds of 100 nM, 240 nM, and 360 nM for JNK3, JNK1, and JNK2, respectively.
|
-
- HY-110135A
-
|
NBI-31772 hydrate
|
IGF-1R
|
Neurological Disease
|
|
NBI-31772 hydrate is a potent inhibitor of interaction between insulin-like growth factor (IGF) and IGF-binding proteins (IGFBPs). NBI-31772 hydrate is also a nonpeptide ligand that releases bioactive IGF-I from the IGF-I/IGFBP-3 complex (Kis=1-24 nM for all six human subtypes). Anxiolytic and antidepressant-like effects.
|
-
- 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-N0139
-
-
- HY-N1599
-
-
- HY-N2286
-
-
- HY-N3637
-
-
- HY-B0927
-
|
Hydrastine
(-)-β-Hydrastine; (1R,9S)-β-Hydrastine
|
Others
|
Others
|
|
Hydrastine is a natural alkaloid which is present in Hydrastis canadensis and other plants of the ranunculaceae family.
|
-
- HY-N2212
-
-
- HY-B1000
-
-
- HY-N0873
-
|
Sagittatoside A
Icariin-A
|
Others
|
Others
|
|
Sagittatoside A is a natural compound isolated from traditional Chinese herb Yinyanghuo (Herba Epimdii).
|
-
- HY-N0056
-
-
- HY-13930
-
|
Miquelianin
Quercetin 3-O-glucuronide; Quercetin 3-glucuronide
|
Endogenous Metabolite
|
Cancer
|
|
Miquelianin (Quercetin 3-O-glucuronide) is a metabolite of quercetin and a type of natural flavonoid.
|
-
- HY-N0695
-
-
- HY-N2200
-
-
- HY-N0744
-
-
- HY-W016289
-
|
Antiarol
3,4,5-Trimethoxyphenol
|
Others
|
Others
|
|
Antiarol (3,4,5-Trimethoxyphenol) is a natural compound isolated from Salmaliamalabaricum.
|
-
- HY-N0903
-
|
Dihydrochelerythrine
12,13-Dihydrochelerythrine
|
Fungal
|
Infection
|
|
Dihydrochelerythrine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal activity.
|
-
- HY-N6874
-
-
- HY-N1372
-
-
- HY-N4167
-
|
3-O-Methylgalangin
Galangin 3-methyl ether; 3-Methylgalangin
|
Others
|
Infection
|
|
3-O-Methylgalangin (Galangin 3-methyl ether) is a natural flavonoid compound from the rhizome of Alpinia officinarum (AO) with antibacterial activities, which also inhibits pancreatic lipase.
|
-
- HY-N8395
-
|
Tunicamycin V
Tunicamycin A
|
Bacterial
|
Infection
|
|
Tunicamycin V (Tunicamycin A) is a nucleoside natural product that inhibits bacterial phospho-N-acetylmuramyl-pentapeptide transferase (MraY) with an IC50 of 0.35 μM. Tunicamycin V has antibacterial activties.
|
-
- HY-P0219
-
|
Microcystin-LA
|
Phosphatase
|
Cancer
|
|
Microcystin LA, a natural toxin, exerts its cytotoxic exects by inhibiting the serine-threonine protein phosphatases PP1 and PP2A with IC50s of 0.3 and 0.3 nM, respectively.
|
-
- HY-N4288
-
-
- HY-N7621
-
|
Bryonamide A
|
Others
|
Others
|
|
Bryonamide A is a natural compound isolated from red algae Bostrychia radicans (Rhodomelaceae).
|
-
- HY-N0007
-
|
Bisdemethoxycurcumin
Curcumin III; Didemethoxycurcumin
|
Apoptosis
Autophagy
|
Cancer
|
|
Bisdemethoxycurcumin(Curcumin III; Didemethoxycurcumin) is a natural derivative of curcumin with anti-inflammatory and anti-cancer activities.
|
-
- HY-131108
-
-
- HY-N1944
-
-
- HY-N0669
-
|
Stevioside
|
Others
|
Cancer
|
|
Stevioside is a natural sweetener extracted from leaves of Stevia rebaudiana, with anticancer activity.
|
-
- HY-N4279
-
|
Gentisin
|
Others
|
Others
|
|
Gentisin is a natural compound isolated from Gentianae radix (Gentianaceae) with mutagenic activities.
|
-
- HY-128387
-
-
- HY-123100
-
-
- HY-N2446
-
|
Kakuol
|
Fungal
|
Infection
|
|
Kakuol is a natural compound isolated from the rhizomes of Asarum sieboldii. Antifungal activity.
|
-
- HY-N0902
-
|
Dihydrosanguinarine
13,14-Dihydrosanguinarine
|
Others
|
Infection
|
|
Dihydrosanguinarine is a natural compound isolated from the leaves of Macleaya microcarpa; has antifungal and anticancer activity.
|
-
- HY-N7631
-
|
Combretol
|
Others
|
Others
|
|
Combretol is a natural compound isolated from the roots and leaves of the plant Cassipourea madagascariensis.
|
-
- HY-N0467
-
-
- HY-N1276
-
-
- 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-N6068
-
-
- HY-N0874
-
-
- HY-N4202
-
-
- HY-12076
-
|
BMS 777607
BMS 817378
|
c-Met/HGFR
TAM Receptor
|
Cancer
|
|
BMS 777607 is a Met-related inhibitor for c-Met, Axl, Ron and Tyro3 with IC50s of 3.9 nM, 1.1 nM, 1.8 nM and 4.3 nM, respectively, and 40-fold more selective for Met-related targets than Lck, VEGFR-2, and TrkA/B, with more than 500-fold greater selectivity versus all other receptor and non receptor kinases.
|
-
- HY-P1783
-
|
M2e, human
|
Influenza Virus
|
Infection
|
|
M2e, human, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A, which is a valid and versatile vaccine candidate to protect against any strain of human influenza A.
|
-
- HY-112724
-
|
SHR0302
|
JAK
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
SHR0302 is a potent and orally active all members of the JAK family inhibitor, particularly JAK1. The selectivity of SHR0302 for JAK1 is >10-fold for JAK2, 77-fold for JAK3, 420-fold for Tyk2. SHR0302 inhibits JAK1-STAT3 phosphorylation and induces the apoptosis of hepatic stellate cells. SHR0302 has anti-proliferative and anti-inflammatory effects.
|
-
- HY-N2110
-
|
Phellopterin
|
Others
|
Inflammation/Immunology
|
|
Phellopterin is a natural product isolated from P. trifoliata. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium.
|
-
- HY-120140
-
-
- HY-N0182
-
-
- HY-N4324
-
-
- HY-N1428
-
-
- HY-15459
-
-
- HY-W025371
-
-
- HY-N0870
-
-
- HY-N6889
-
-
- HY-W004263
-
-
- HY-N0662
-
-
- HY-N4123
-
-
- HY-N4319
-
-
- HY-N7662
-
-
- HY-N0078
-
|
Ginkgolic Acid (C13:0)
Ginkgolic acid (13:0); Ginkgoneolic Acid; 6-Tridecylsalicylic acid
|
Others
|
Infection
|
|
Ginkgolic Acid (C13:0) is a natural anticariogenic agent in that it exhibits antimicrobial activity against S.
|
-
- HY-N1127
-
|
Tricin
|
CMV
|
Cancer
Infection
|
|
Tricin is a natural flavonoid present in large amounts in rice bran. Tricin can inhibit human cytomegalovirus (HCMV) replication by inhibiting CDK9. Tricin inhibits the proliferation and invasion of C6 glioma cells via the upregulation of focal-adhesion-finase (FAK)-targeting microRNA-7.
|
-
- HY-122586
-
|
BRD6989
|
CDK
Interleukin Related
|
Inflammation/Immunology
|
|
BRD6989, an analog of the natural product cortistatin A (dCA), inhibits CDK8 and upregulates IL-10. BRD6989 selectively binds a complex of CDK8 with an IC50 of ~200 nM. BRD6989 inhibits the kinase activity of recombinant CDK8 or CDK19 complexes.
|
-
- 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-N0592
-
|
Demethyleneberberine
|
NF-κB
AMPK
|
Metabolic Disease
Inflammation/Immunology
|
|
Demethyleneberberine is a natural mitochondria-targeted antioxidant. Demethyleneberberine alleviates mice colitis and inhibits the inflammatory responses by inhibiting NF-κB pathway and regulating the balance of Th cells. Demethyleneberberine could serve as a AMPK activator for treating non-alcoholic fatty liver disease (NAFLD).
|
-
- HY-W016586
-
|
Acivicin
AT-125; U-42126
|
Parasite
|
Cancer
Infection
|
|
Acivicin (AT-125), a natural product produced by Streptomyces sviceus is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-N0737A
-
|
Harmine
Telepathine
|
DYRK
5-HT Receptor
|
Cancer
Neurological Disease
|
|
Harmine is a natural dual-specificity tyrosine phosphorylation-regulated kinase (DYRK) inhibitor with anticancer and anti-inflammatory activities. Harmine has a high affinity of 5-HT2A serotonin receptor, with an Ki of 397 nM.
|
-
- HY-W016586A
-
|
Acivicin hydrochloride
AT-125 hydrochloride; U-42126 hydrochloride
|
Parasite
|
Cancer
Infection
|
|
Acivicin hydrochloride (AT-125 hydrochloride), a natural product produced by Streptomyces sviceus, is a γ-glutamyl transpeptidase (GGT) inhibitor. Acivicin hydrochloride can across the blood-brain barrier and has anti-cancer, anti-parasitic properties.
|
-
- HY-N6022
-
|
Byakangelicin
|
Others
|
Metabolic Disease
|
|
Byakangelicin, one of the active compounds found in the roots of Angelica gigas, can serve as a modulator to improve brain accumulation of diverse active compounds (Umb, Cur, and Dox) and enhance therapeutic effects. Byakangelicin is likely to increase the expression of all PXR target genes (such as MDR1) and induce a wide range of drug-drug interactions. Byakangelicin can inhibit the effects of sex hormones, it may increase the catabolism of endogenous hormones.
|
-
- HY-W008350
-
-
- HY-N0875
-
-
- HY-116284
-
-
- HY-W001963
-
-
- HY-19531
-
-
- HY-N6820
-
-
- HY-N0860
-
-
- HY-N0571
-
-
- HY-N0537
-
|
Xylose
D-(+)-Xylose; (+)-Xylose; Wood sugar
|
Endogenous Metabolite
|
Others
|
|
Xylose, a natural product, can be catalyzed into xylulose by xylose isomerase, and it is the key step for anaerobic ethanolic fermentation of xylose.
|
-
- HY-N1899
-
-
- HY-N6260
-
-
- HY-N0852
-
-
- HY-138638
-
|
Sephadex LH 20
|
Others
|
Others
|
|
Sephadex LH 20 could be used for the isolation of natural compounds and food, such as red wine and pigments.
|
-
- HY-W017241
-
-
- HY-W012980
-
-
- HY-N0887
-
-
- HY-17583
-
-
- HY-N0658
-
-
- HY-N2176
-
-
- HY-129997
-
|
Luteolinidin chloride
|
Others
|
Inflammation/Immunology
|
|
Luteolinidin is a natural deoxyanthocyanidin, isolated from mosses and ferns. Luteolinidin is a potent CD38 inhibitor which can protect the heart against I/R injury with preservation of eNOS function and prevention of endothelial dysfunction in vivo.
|
-
- HY-N0836
-
|
Jervine
11-Ketocyclopamine
|
Hedgehog
Smo
|
Cancer
Inflammation/Immunology
|
|
Jervine (11-Ketocyclopamine) is a potent Hedgehog (Hh) inhibitor with an IC50 of 500-700 nM. Jervine is a natural teratogenic sterodial alkaloid from rhizomes of Veratrum album. Jervine has anti-inflammatory and antioxidant properties.
|
-
- HY-12686
-
-
- 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-N0573
-
-
- HY-N2114
-
-
- HY-N6067
-
|
Primin
|
Bacterial
|
Cancer
Infection
|
|
Primin is a natural product stored in trichomes on leaves and stems of Primula obconica, with antimicrobial and antitumour properties.
|
-
- HY-N4106
-
-
- HY-N0140
-
-
- HY-N0362
-
-
- HY-N0418
-
-
- HY-N2505
-
-
- HY-N1318
-
-
- HY-N5098
-
-
- 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-W050154
-
|
Kojic acid
|
Parasite
|
Infection
|
|
Kojic acid is a natural substance produced by Aspergillus oryzae, also used as an anti-oxidant and radio-protective agent.
|
-
- HY-P1577
-
-
- HY-120323
-
|
DRI-C21045
|
TNF Receptor
|
Inflammation/Immunology
|
|
DRI-C21045 (compound 10) is a potent and selective inhibitor of the CD40-CD40L costimulatory protein-protein interaction (PPI) with an IC50 of 0.17 µM. DRI-C21045 shows concentration-dependent inhibition of the activation of NF-κB and B cell proliferation all induced by CD40L with IC50s of 17.1 µM and 4.5 µM, respectively.
|
-
- HY-112831
-
|
BI-409306
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
BI-409306 is a potent and selective PDE9A inhibitor, with an IC50 of 52 nM, and shows weak activity against other PDEs, such as PDE1A (IC50, 1.4 µM), PDE1C (IC50, 1.0 µM), PDE2A, PDE3A, PDE4B, PDE5A, PDE6AB, PDE7A, and PDE10A (IC50 all > 10 μM); BI-409306 can be used in the research of memory enhancement in CNS disorders.
|
-
- HY-77813
-
-
- HY-N0722
-
-
- 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-N8356A
-
|
9-cis-Vitamin A palmitate
9-cis-Retinyl palmitate
|
Endogenous Metabolite
|
Others
|
|
9-cis-Vitamin A palmitate (9-cis-Retinyl palmitate) is a 9-cis isomer formed by vitamin A palmitate in corn flakes. 9-cis-Vitamin A palmitate has a biological activity of 26% of all-trans-vitamin A palmitate, the most biologically ac-tive form of vitamin A.
|
-
- HY-N8356
-
|
13-cis-Vitamin A palmitate
13-cis-Retinyl palmitate
|
Endogenous Metabolite
|
Others
|
|
13-cis-Vitamin A palmitate (13-cis-Retinyl palmitate) is a 13-cis isomer formed by vitamin A palmitate in corn flakes. 13-cis-Vitamin A palmitate has a biological activity of 75% of all-trans-vitamin A palmitate, the most biologically ac-tive form of vitamin A.
|
-
- HY-P1783A
-
|
M2e, human TFA
|
Influenza Virus
|
Infection
|
|
M2e, human TFA, consisting of the 23 extracellular residues of M2 (the third integral membrane protein of influenza A), has been remarkably conserved in all human influenza A. M2e, human TFA is a valid and versatile vaccine candidate to protect against any strain of human influenza A.
|
-
- HY-118743
-
|
KMN-80
|
Prostaglandin Receptor
|
Metabolic Disease
|
|
KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors.
|
-
- HY-N0628
-
-
- HY-N2239
-
-
- HY-N3373
-
|
Loganetin
|
Bacterial
|
Infection
|
|
Loganetin is a non-toxic natural product that may be applied in the antibacterial drug development for treating multidrug-resistant Gram negative infections.
|
-
- HY-N7657
-
-
- HY-N2842
-
-
- HY-N7035
-
-
- HY-W010178
-
|
4-Methyloctanoic acid
|
Others
|
Others
|
|
4-Methyloctanoic acid is a natural compound mainly responsible for the characteristic goaty sheepy flavour of sheep and goat milk.
|
-
- HY-N0523
-
-
- HY-N0523A
-
-
- HY-A0126A
-
|
Epoprostenol sodium
Prostaglandin I2 sodium salt; Prostacyclin sodium salt; Flolan
|
Others
|
Cardiovascular Disease
|
|
Epoprostenol sodium (Prostaglandin I2 (sodium salt)), the synthetic form of the natural prostaglandin derivative prostacyclin (prostaglandin I2), is registered worldwide for the treatment of Pulmonary arterial hypertension (PAH). Epoprostenol sodium is used in pulmonary hypertension and transplantation as a potent inhibitor of platelet aggregation.
|
-
- HY-N0211
-
|
Cyasterone
|
EGFR
Apoptosis
|
Cancer
|
|
Cyasterone, a natural EGFR inhibitor, mainly isolated from Ajuga decumbens Thunb (Labiatae). Cyasterone manifests anti-proliferation effect by induced apoptosis and cell cycle arrests. Cyasterone may serves as a therapeutic anti-tumor agent against human tumors.
|
-
- HY-N7058
-
|
cis-Jasmone
|
Others
|
Others
|
|
Cis-Jasmone is a plant-derived natural product. Cis-Jasmone is constitutively released by many flowers and sometimes by leaves as an attractant for pollinators or as a chemical cue for host location by insect flower herbivores. Cis-Jasmone treatment of crop plants not only induces direct defense against herbivores, but also induces indirect defense by releasing VOCs that attract natural enemies.
|
-
- HY-N0288
-
-
- HY-110105
-
|
NS8593 hydrochloride
|
Potassium Channel
|
Neurological Disease
|
|
NS8593 hydrochloride is a potent and selective small conductance Ca 2+-activated K + channels (SK channels) inhibitor. NS8593 hydrochloride reversibly inhibits SK3-mediated currents with a Kd value of 77 nM. NS8593 hydrochloride inhibits all the SK1-3 subtypes Ca 2+-dependently (Kds of 0.42, 0.60, and 0.73 μM, respectively, at 0.5 μM Ca 2+), and does not affect the Ca 2+-activated K + channels of intermediate and large conductance (hIK and hBK channels, respectively).
|
-
- HY-N2345
-
|
Procyanidin B3
|
Histone Acetyltransferase
|
Cancer
|
|
Procyanidin B3 is a natural product, acts as a specific HAT inhibitor, binds to the other site of p300 instead of the active site, selectively inhibits p300-mediated androgen receptor acetylation. Procyanidin B3 has no effect on HDAC or HMT (histone methyltransferase).
|
-
- HY-N6715
-
|
Tenuazonic acid
|
Influenza Virus
Bacterial
|
Infection
|
|
Tenuazonic acid, belonging to tetramic acids that are the largest family of natural products, is a putative nonhost-selective mycotoxin isolated from Alternaria alternate. Tenuazonic acid blocks electron transport beyond primary quinone acceptor (QA) by interacting with D1 protein and it is a broad-spectrum and effective photosystem II (PSII) inhibitor.
|
-
- HY-N4053
-
|
Heraclenin
|
Others
|
Inflammation/Immunology
|
|
Heraclenin, a natural furanocoumarin, isolated from the root parts of the plant Prangos pabularia. Heraclenin significantly inhibits T cell receptor-mediated proliferation in human primary T cells in a concentration-dependent manner by targeting nuclear factor of activated T-cells (NFAT).
|
-
- HY-32736
-
|
Triptonide
NSC 165677; PG 492
|
Wnt
β-catenin
Apoptosis
Autophagy
|
Cancer
Inflammation/Immunology
|
|
Triptonide (NSC 165677; PG 492) is a natural product identified in Tripterygium wilfordii Hook F.. Triptonide is a Wnt signaling inhibitor with an IC50 of appropriately 0.3 nM. Triptonide has immunosuppression, anti-inflammatory, anti-fertility, neuroprotective and anti-lymphoma effects.
|
-
- HY-N3670
-
|
Cycloolivil
Isoolivil
|
Others
|
Cardiovascular Disease
|
|
Cycloolivil (Isoolivil) is a natural polyphenolic compound with a significant radical scavenging activity present in olive tree. Antioxidant and Antiaggregant effects.
|
-
- HY-N0891
-
|
Tubeimoside II
Tubeimoside-B
|
Others
|
Cancer
|
|
Tubeimoside II(Tubeimoside-B) is a natural analogue of oleanane type of triterpenoid saponin; show anti-inflammatory, antitumor, and antitumor-promoting effects.
|
-
- HY-N6069
-
-
- HY-N5128
-
-
- HY-B0923
-
|
Danthron
Dantron; Chrysazin; 1,8-Dihydroxyanthraquinone
|
AMPK
Autophagy
Bacterial
Virus Protease
|
Cancer
|
|
Danthron is a natural product extracted from the traditional Chinese medicine rhubarb. Danthron functions in regulating glucose and lipid metabolism by activating AMPK.
|
-
- HY-W005327
-
-
- HY-N7539
-
|
Cognac oil
|
Others
|
Metabolic Disease
|
|
Cognac oil, mainly found in wine lees, has unique fatty acid profiles, including Palmitic acid (59.26%), Linoleic acid (11.92%), Myristic acid (8.97%), Oleic acid (8.3%) and other fatty acids. Cognac oil leads to a general increase in the permeation of R6G (Rhodamine 6G) across all the membranes.
|
-
- HY-P1852
-
-
- HY-P2315
-
|
Human β-defensin-1
HβD-1
|
Antibiotic
Bacterial
|
Infection
|
|
Human β-defensin-1 (HβD-1) is a cysteine-rich cationic skin-antimicrobial peptide (SAP) produced by all epithelial surfaces, but also by circulatory cells and cells of the reproductive tract. Human β-defensin-1 has antimicrobial activities against a broad-sperm bacteria.
|
-
- HY-B0228
-
-
- HY-B0389A
-
|
D-Glucose-13C6
Glucose-13C6; D-(+)-Glucose-13C6; Dextrose-13C6
|
Endogenous Metabolite
|
Metabolic Disease
|
|
D-Glucose-13C6 (Glucose-13C6) is a tracer used to trace glucose-related synthetic catabolism, is a low-cost alternative with the significant advantage that the sixth isotope of natural glucose has virtually zero natural abundance, which facilitates isotopomer analysis with <1% labeled glucose in the infusate.
|
-
- HY-118482
-
|
Sauristolactam
Saurolactam
|
Others
|
Neurological Disease
|
|
Sauristolactam, a natural aristolactam isolated from aerial portions of Saururus chinensis, has significant neuroprotective activity against glutamate-induced toxicity in primary cultured rat cortical cells. Sauristolactam also inhibits the receptor activator of nuclear factor-κB ligand (RANKL)-induced osteoclastogenesis and has the potential to inhibit osteoclast differentiation.
|
-
- HY-N2491
-
|
Deoxyelephantopin
|
NF-κB
|
Cancer
|
|
Deoxyelephantopin, a natural bioactive sesquiterpene lactone from Elephantopus scaber, has shown promising anticancer effects against a broad spectrum of cancers. Deoxyelephantopin inhibits NF-κB, MAPK, PI3K/Akt, and β-catenin signaling.
|
-
- HY-N0563
-
|
Alizarin
|
Others
|
Others
|
|
Alizarin is a natural dye extracted from the roots of madder plant and has been widely used as a pigment in textile fabrics and paintings.
|
-
- HY-N0882
-
|
Desacetylcinobufotalin
Deacetylcinobufotalin
|
Apoptosis
|
Cancer
|
|
Desacetylcinobufotalin is a natural compound; apoptosis inducer and shows the marked inhibition effect to HepG2 cells and the IC50 value is 0.0279μmol/ml.
|
-
- HY-N0989
-
-
- HY-N6890
-
-
- HY-121295
-
|
Roseoflavin
|
Bacterial
|
Infection
|
|
Roseoflavin, a natural pigment originally isolated from Streptomyces davawensis, is an antimetabolite analog of Riboflavin and flavin mononucleotide that has antimicrobial properties.
|
-
- HY-N2622
-
|
Oxypeucedanin hydrate
(+)-Oxypeucedanin hydrate
|
Others
|
Cancer
|
|
Oxypeucedanin hydrate ((+)-Oxypeucedanin hydrate) is a natural product isolated from D. anethifolia. Prangol exhibits mild toxicity on fibroblasts and parental lymphoma cells.
|
-
- HY-B0433A
-
|
Quinine hydrochloride dihydrate
|
Parasite
|
Infection
|
|
Quinine Hydrochloride Dihydrate is a natural white crystalline alkaloid having antipyretic (fever-reducing), antimalarial, analgesic (painkilling), anti-inflammatory properties and a bitter taste.
|
-
- HY-N0714
-
|
Berbamine
|
NF-κB
Autophagy
|
Cancer
|
|
Berbamine is a natural compound extracted from traditional Chinese medicine Barberry with anti-tumor, immunomodulatory and cardiovascular effects. Berbamine is a calcium channel blocker.
|
-
- HY-N1956
-
|
Rubiadin-1-methyl ether
|
NF-κB
|
Metabolic Disease
|
|
Rubiadin-1-methyl ether is a natural anthraquinone isolated from Morinda officinalis How, and inhibits osteoclastic bone resorption via inhibition on the phosphorylation of NF-κB p65 and the degradation of IκBα as well as decrease in the nuclear translocation of p65.
|
-
- HY-10529
-
-
- HY-15257
-
|
Mavoglurant
AFQ056
|
mGluR
|
Neurological Disease
|
|
Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease.
|
-
- HY-N4100
-
|
Trilobatin
|
HIV
SGLT
|
Infection
|
|
Trilobatin, a natural sweetener derived from Lithocarpus polystachyus Rehd, Trilobatin is an HIV-1 entry inhibitor targeting the HIV-1 Gp41 envelope. Neuroprotective effects. Trilobatin is also a SGLT1/2 inhibitor that selectively induces the proliferation of human hepatoblastoma cells.
|
-
- HY-N2533
-
-
- HY-N0610
-
-
- HY-B0914A
-
-
- HY-111911
-
-
- HY-W040471
-
|
3′,5′-Dimethoxyacetophenone
|
Others
|
Others
|
|
3′,5′-Dimethoxyacetophenone is a natural ketone compound with antioxidant activities. 3′,5′-Dimethoxyacetophenone is a building block in the chemical synthesis.
|
-
- HY-B2188
-
-
- HY-U00097
-
-
- HY-109044
-
-
- HY-N3521
-
|
Platycoside G1
Deapi-platycoside E
|
Others
|
Others
|
|
Platycoside G1, a natural product found in Platycodon grandiflorum, is a triterpenoid saponin. Platycoside G1 has potent antioxidant activities.
|
-
- 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-N1166
-
|
Tephrosin
Deguelinol I; Hydroxydeguelin
|
EGFR
|
Cancer
|
|
Tephrosin is a natural rotenoid which has potent antitumor activities. Tephrosin induces degradation of of EGFR and ErbB2 by inducing internalization of the receptors.
|
-
- HY-W010533
-
-
- HY-W012999
-
|
Tiglic acid
|
Endogenous Metabolite
|
Others
|
|
Tiglic acid is a monocarboxylic unsaturated organic acid found in croton oil and in several other natural products. Tiglic aci has a role as a plant metabolite.
|
-
- HY-Y0152
-
|
Cinchonine
(8R,9S)-Cinchonine; LA40221
|
Apoptosis
Parasite
|
Cancer
|
|
Cinchonine is a natural compound present in Cinchona bark. Cinchonine activates endoplasmic reticulum stress-induced apoptosis in human liver cancer cells.
|
-
- HY-16059
-
-
- HY-122872
-
|
MKK7-COV-9
|
p38 MAPK
|
Cancer
|
|
MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
|
-
- HY-109172
-
|
Ezeprogind
AZP-2006
|
Amyloid-β
|
Neurological Disease
|
|
Ezeprogind (AZP-2006) is an orally active neurotrophic inducer. Ezeprogind targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.
|
-
- HY-N7434
-
|
N-Nitrosodiethylamine
|
DNA/RNA Synthesis
|
Cancer
|
|
N-Nitrosodiethylamine is a potent hepatocarcinogenic dialkylnitrosoamine. N-Nitrosodiethylamine is mainly present in tobacco smoke, water, cheddar cheese, cured, fried meals and many alcoholic beverages. N-Nitrosodiethylamine is responsible for the changes in the nuclear enzymes associated with DNA repair/replication. N-Nitrosodiethylamine results in various tumors in all animal species. The main target organs are the nasal cavity, trachea, lung, esophagus and liver.
|
-
- HY-Y0790
-
|
Cuminaldehyde
|
Endogenous Metabolite
|
Cancer
|
|
Cuminaldehyde is the major component of Cuminum cyminum, a natural aldehyde with inhibitory effect on alpha-synuclein fibrillation and cytotoxicity. Cuminaldehyde shows anticancer activity.
|
-
- HY-N0012
-
|
Glycitin
Glycitein 7-O-β-glucoside
|
Influenza Virus
Bacterial
|
Cancer
Infection
|
|
Glycitin is a natural isoflavone isolated from legumes; promotes the proliferation of bone marrow stromal cells and osteoblasts and suppresses bone turnover.Glycitin is antibacterial, antiviral and estrogenic.
|
-
- HY-N9312
-
-
- HY-N0452
-
-
- HY-N0224
-
|
Epigoitrin
|
Influenza Virus
|
Infection
Cancer
|
|
Epigoitrin is a natural alkaloid from Isatis indigotica, with antiviral activities. Epigoitrin reduces susceptibility to influenza virus via mitochondrial antiviral signaling.
|
-
- HY-N2868
-
|
Andropanoside
|
Others
|
Metabolic Disease
|
|
Andropanoside is a natural product isolated and purified from the herbs of Andrographis paniculata. Andrographis paniculata possesses a protective activity against various liver disorders.
|
-
- HY-N4068
-
|
Glucoraphanin
|
Reactive Oxygen Species
|
Cancer
|
|
Glucoraphanin, a natural glucosinolate found in cruciferous vegetable, is a stable precursor of the Nrf2 inducer sulforaphane, which possesses antioxidant, anti-inflammatory, and anti-carcinogenic effects.
|
-
- HY-N2997
-
|
Ganoderic acid LM2
|
Others
|
Cancer
|
|
Ganoderic acid LM2 is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid LM2 possesses potential anti-tumor activity.
|
-
- HY-W007856
-
|
5-Methoxysalicylic acid
5-MeOSA
|
Others
|
Others
|
|
5-Methoxysalicylic acid (5-MeOSA) is a natural compound, used as a useful matrix in the MALDI MS analysis of oligonucleotides when combined with spermine.
|
-
- 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-N0713
-
-
- HY-14781
-
-
- HY-N0207
-
-
- HY-N0398
-
-
- HY-19336
-
|
BAZ2-ICR
|
Epigenetic Reader Domain
|
Cancer
|
|
BAZ2-ICR is a potent, selective, cell active and orally active BAZ2A/B bromodomains inhibitor with IC50s of 130 nM and 180 nM, and Kds of 109 nM and 170 nM, respectively. BAZ2-ICR shows 10-15-fold selectivity for binding BAZ2A/B over CECR2 and >100-fold selectivity over all other bromodomains. BAZ2-ICR is an epigenetic chemical probe.
|
-
- HY-N4205
-
|
Tetrahydropiperine
|
Cytochrome P450
|
Cancer
|
|
Tetrahydropiperine, a cyclohexyl analogue of piperine, is the first natural aryl pentanamide from Piper longum. Tetrahydropiperine (compound 14) inhibits the cytochrome P450 (CYP) isoform CYP1A1/arylhydrocarbon hydroxylase (AHH; IC50=23 µM).
|
-
- HY-N7422
-
|
Kauran-16,17-diol
ent-Kauran-16β,17-diol
|
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Kauran-16,17-diol (ent-Kauran-16β,17-diol), a natural diterpene, posseses anti-tumor and inducing-apoptosis activity, with a IC50 of 17 μM on inhibiting NO production in LPS-stimulated RAW 264.7 macrophages.
|
-
- HY-N4327
-
|
Eurycomalactone
|
NF-κB
|
Infection
Inflammation/Immunology
|
|
Eurycomalactone is a natural product found in Eurycoma longifolia Jack., acts as a potent NF-κB inhibitor, with an IC50 of 0.5 μM. Eurycomalactone inhibits protein synthesis, depletes cyclin D1, but does not affect TNFα-induced degradation of IκBα or the phosphorylation of IKKα/β and IκBα.
|
-
- HY-N2574
-
|
Gitogenin
|
Glucosidase
|
Metabolic Disease
|
|
Gitogenin is a natural steroid isolated from the whole plant of Tribulus longipetalus. Gitogenin is a selective inhibitor of UDP-glucuronosyltransferase 1A4 (UGT1A4) and enzyme α-glucosidase with IC50 values of 0.69 μM (use trifluoperazine as a substrate) and 37.2 μM, respectively, and does not inhibit the activities of major human cytochrome P450 isoforms.
|
-
- HY-N0346A
-
-
- HY-N9350
-
|
Ganoderic acid ε
|
Others
|
Cancer
|
|
Ganoderic acid ε is a natural terpenoid isolated from the Fungus Ganoderma lucidum. Ganoderic acid ε exhibits an ED50 of 12.2 μg/mL in Meth-A tumor cells
|
-
- HY-N3442
-
-
- HY-129405
-
-
- 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-17434
-
-
- HY-W015307
-
|
4-Ethyloctanoic acid
|
Others
|
Others
|
|
4-Ethyloctanoic acid is a natural compound first isolated from Saussurea lappa Clarke, widely used as a safe flavoring compound and acts as food additive.
|
-
- HY-N2487
-
-
- HY-N0777
-
-
- HY-N2370
-
-
- HY-121471
-
|
Chrysoeriol
|
Others
|
Metabolic Disease
|
|
Chrysoeriol, a natural flavonoid extracted from the tropical plant Coronopus didymus, exhibits potent antioxidant activity. Chrysoeriol shows significant inhibition of lipid peroxidation.
|
-
- HY-W012634
-
-
- HY-N0238
-
|
Atractylodin
Atractydin
|
Others
|
Infection
|
|
Atractylodin (Atractydin) is an active component of the essential oil contained in the rhizomes of Atractylodes lancea and A. chinensis. Atractylodin is natural insecticide and is active against Tribolium castaneum.
|
-
- HY-P1259
-
|
PR-39
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-114236
-
|
Ezeprogind disulfate
AZP-2006 disulfate
|
Amyloid-β
|
Neurological Disease
|
|
Ezeprogind (AZP-2006) disulfate is an orally active neurotrophic inducer. Ezeprogind disulfate targets all causes of neurodegeneration and is not only aiming at markers such as Abeta protein or tau protein. Ezeprogind disulfate is a potent neuroprotectant and can be used for the research of neurological disorders, including progressive supranuclear palsy (PSP), tauopathies, alzheimer’s and parkinson’s diseases, et al.
|
-
- HY-121744
-
|
PS10
|
PDHK
|
Inflammation/Immunology
|
|
PS10 is a novel, potent and ATP-competitive pan-PDK inhibitor, inhibits all PDK isoforms with IC50 of 0.8 μM, 0.76 μM, 2.1 μM and 21.3 μM for PDK2, PDK4, PDK1, and PDK3, respectively. PS10 shows high affinity for PDK2 (Kd= 239 nM) than for Hsp90 (Kd= 47 μM). PS10 improves glucose tolerance, stimulates myocardial carbohydrate oxidation in diet-induced obesity. PS10 has the potential for the investigation of diabetic cardiomyopathy.PDK: pyruvate dehydrogenase kinase
|
-
- HY-18085
-
-
- HY-B0986
-
|
Hexylresorcinol
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
|
Cancer
Infection
Metabolic Disease
|
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage.
|
-
- HY-N5111
-
-
- HY-N2840
-
|
Allitol
Allodulcitol
|
Others
|
Cancer
Metabolic Disease
|
|
Allitol is a rare natural polyol that can be used as a sweetener. Allitol is an important intermediate for the preparation of the agents which against diabetes, cancer, and viral infections, including AIDS.
|
-
- HY-N9320
-
|
13,21-Dihydroeurycomanone
|
Parasite
|
Infection
|
|
13,21-Dihydroeurycomanone, a natural compound isolated from Eurycoma longifolia root, possesses anti-parasite activity for Plasmodium falciparum and Toxoplasma gondii.
|
-
- HY-N0805
-
|
Alisol B 23-acetate
23-Acetylalismol B; 23-O-Acetylalisol B; Alisol B monoacetate
|
Others
|
Others
|
|
Alisol B 23-acetate (23-Acetylalismol B), a natural triterpenoid, produces protective effects against EE-induced cholestasis, due to FXR-mediated gene regulation.
|
-
- HY-N2561
-
|
Seneciphylline N-Oxide
|
Others
|
Cancer
|
|
Seneciphylline N-Oxide is a dehydrogenation product of Senecionine N-oxide. Seneciphylline N-Oxide is a natural compound isolated from root cultures of Senecio erucifolius (Asteraceae).
|
-
- HY-N0124
-
|
Dioscin
Collettiside III; CCRIS 4123
|
Autophagy
Apoptosis
|
Cancer
|
|
Dioscin(CCRIS 4123; Collettiside III) is a natural steroid saponin derived from several plants, showing potent anti-cancer effect against a variety of tumor cell lines.
|
-
- HY-16686
-
|
α-Tocopherol phosphate
alpha-Tocopherol phosphate; TocP; vitamin E phosphate
|
Others
|
Others
|
|
α-Tocopherol phosphate is the compound demonstrating the highest vitamin E activity, which is available both in its natural form as RRR-alpha-tocopherol isolated from plant sources.
|
-
- HY-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-P1259A
-
|
PR-39 TFA
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice.
|
-
- HY-15295
-
|
Vonoprazan Fumarate
TAK-438
|
Proton Pump
|
Metabolic Disease
|
|
Vonoprazan Fumarate (TAK-438), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan Fumarate inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan Fumarate is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-100007
-
|
Vonoprazan
TAK-438 free base
|
Proton Pump
|
Endocrinology
|
|
Vonoprazan (TAK-438 free base), a proton pump inhibitor (PPI), is a potent and orally active potassium-competitive acid blocker (P-CAB), with antisecretory activity. Vonoprazan inhibits H +,K +-ATPase activity in porcine gastric microsomes with an IC50 of 19 nM at pH 6.5. Vonoprazan is developed for the research of acid-related diseases, such as gastroesophageal reflux disease and peptic ulcer disease.
|
-
- HY-133646
-
|
Bromochloroacetonitrile
|
DNA/RNA Synthesis
|
Others
|
|
Bromochloroacetonitrile is a by-product of the chlorine disinfection of water containing natural organic material. Bromochloroacetonitrile possesses direct acting mutagenic activity and is capable of inducing DNA strand breakage.
|
-
- HY-N6018
-
-
- HY-N4000
-
|
Digitonin
|
Others
|
Cancer
|
|
Digitonin, a glycoside obtained from Digitalis purpurea, could increase cell permeability by binding to cholesterol molecules and reduce tumor growth. Digitonin is an natural detergent.
|
-
- HY-13938
-
|
Iretol
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Iretol (2,4,6-trihydroxyanisole) is a a degradation product of a glucoside obtained from Iris Jorentina. Iretol is an intermediate in the synthesis of natural isoflavones, such as Tectorigenin, Irigenin and Caviunin.
|
-
- HY-N6965
-
-
- HY-N6829
-
|
Retusin
Quercetin-3,3',4',7-tetramethylether
|
Others
|
Infection
Inflammation/Immunology
|
|
Retusin (Quercetin-3,3',4',7-tetramethylether), a natural compound isolated from the leaves of Talinum triangulare, possesses antiviral and anti-inflammatory activities.
|
-
- HY-N1181
-
-
- HY-N2338
-
-
- HY-N5029
-
|
Isofebrifugine
|
Parasite
|
Infection
|
|
Isofebrifugine, isolated from a Chinese medicinal plant, Chang Shan (Dichroa febrifuga), is a natural quinazolinone alkaloid with important physiological activities and good pharmacological effects. Antimalarial effect.
|
-
- HY-U00450
-
-
- HY-N7011
-
-
- 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-N7624
-
|
Methyl oleanonate
3-Oxoolean-12-en-28-oic acid methyl ester
|
PPAR
|
Cancer
|
|
Methyl oleanonate is a natural triterpene PPARγ agonist isolated from the species of Pistacia. Methyl oleanonate is a modified oleanolic acid derivative with anti-cancer effects.
|
-
- HY-15464D
-
|
(S)-Gossypol acetic acid
(S)-(+)-Gossypol acetic acid
|
Bcl-2 Family
|
Cancer
|
|
(S)-Gossypol is the isomer of a natural product Gossypol. (S)-Gossypol binds to the BH3-binding groove of Bcl-xL and Bcl-2 proteins with high affinity.
|
-
- HY-N7124
-
|
Benzyl acetate
|
Others
|
Others
|
|
Benzyl acetate is a constituent of jasmin and of the essential oils of ylang-ylang and neroli. Natural sources of Benzyl acetate include varieties of flowers like jasmine (Jasminum), and fruits like pear, apple.
|
-
- HY-W046353
-
|
2-Methoxycinnamaldehyde
o-Methoxycinnamaldehyde
|
Apoptosis
|
Cancer
|
|
2-Methoxycinnamaldehyde (o-Methoxycinnamaldehyde) is a natural compound of Cinnamomum cassia, with antitumor activity. 2-Methoxycinnamaldehyde inhibits proliferation and induces apoptosis by mitochondrial membrane potential (ΔΨm) loss, activation of both caspase-3 and caspase-9. 2-Methoxycinnamaldehyde effectively inhibits platelet-derived growth factor (PDGF)-induced HASMC migration.
|
-
- HY-129039
-
|
Butyrolactone 3
|
Histone Acetyltransferase
|
Cancer
|
|
Butyrolactone 3 is a specifical small-molecule inhibitor of the histone acetyltransferase Gcn5 (IC50=100 μM), which has a high affinity to the Gcn5 enzyme comparable to that of its natural substrate, histone H3. Butyrolactone 3 shows weak inhibitory on CBP (IC50=0.5 mM)
|
-
- HY-N0192
-
|
Arbutin
β-Arbutin
|
Tyrosinase
|
Cancer
|
|
Arbutin (β-Arbutin) is a competitive inhibitor of tyrosinase in melanocytes, with Ki app values of 1.42 mM for monophenolase; 0.9 mM for diphenolase. Arbutin is also used as depigmenting agents. Arbutin is a natural polyphenol isolated from the bearberry plant Arctostaphylos uvaursi, possesses with anti-oxidant, anti-inflammatory and anti-tumor properties.
|
-
- HY-N0146
-
-
- HY-119424
-
-
- HY-136203
-
-
- HY-103700B
-
|
(Rac)-Azide-phenylalanine
|
Others
|
Others
|
|
(Rac)-Azide-phenylalanine is a racemate of Azide-phenylalanine. Azide-phenylalanine is a phenylalanine derivative and a non-natural amino acid. Azide-phenylalanine can be site-specifically incorporated into proteins and used to label proteins.
|
-
- HY-N0471
-
|
L-Hyoscyamine
Daturine
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine (Daturine), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine is a levo-isomer to Atropine (HY-B1205).
|
-
- HY-W024604
-
-
- HY-136204
-
-
- HY-N1283
-
|
Seneciphyllinine
|
Others
|
Metabolic Disease
|
|
Seneciphyllinine, a pyrrolizidine alkaloid, is isolated from the roots of Gynura japonica. Pyrrolizidine alkaloids are highly hepatotoxic natural chemicals that produce irreversible chronic and acute hepatotoxic effects on human beings.
|
-
- HY-N0849
-
|
Dictamine
Dictamnine; Dectamine
|
Apoptosis
Bacterial
Fungal
|
Infection
|
|
Dictamnine (Dictamine) has the ability to exert cytotoxicity in human cervix, colon, and oral carcinoma cells; A natural plant product has been reported to have antimicrobial activity against bacteria and fungi.
|
-
- HY-N0901
-
|
Corynoxine
|
Autophagy
|
Cancer
Neurological Disease
|
|
Corynoxine, a tetracyclic oxindole alkaloid, is isolated from the hooks of Uncaria macrophylla. Corynoxine is a natural autophagy enhancer that promotes the clearance of alpha-synuclein via Akt/mTOR pathway.
|
-
- HY-N6661
-
|
Verbenone
(-)-Verbenone
|
Others
|
Infection
|
|
Verbenone ((-)-Verbenone) is a natural terpene in leaves of the tree, Suregada zanzibariensis Verdc. Verbenone has anti-aggregation pheromone and interrupts the attraction of bark beetles to their aggregation pheromones.
|
-
- HY-B2114
-
|
Escin
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Escin, a natural compound of triterpenoid saponins isolated from horse chestnut (Aesculus hippocastanum) seeds, can be used as a vasoprotective anti-inflammatory, anti-edematous and anti-nociceptive agent.
|
-
- HY-W002272
-
|
Isocytosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
Isocytosine is a non-natural nucleobase and an isomer of cytosine. It is used in combination with Isoguanine in studies of unnatural nucleic acid analogues of the normal base pairs in DNA and used as a nucleobase of hachimoji RNA.
|
-
- HY-107324
-
|
β-Elemene
(-)-β-Elemene; Levo-β-elemene
|
Apoptosis
|
Cancer
|
|
β-Elemene ((-)-β-Elemene; Levo-β-elemene) is isolated from natural plant Curcuma wenyujin with an antitumor activity. β-Elemene can induce cell apoptosis.
|
-
- HY-111830
-
|
Lignin
Lignine
|
Others
|
Others
|
|
Lignin (Lignine) is a natural complex biopolymer with biodegradable and biocompatible. Lignin is the main component of plant cell walls and is a renewable aromatic polymer. Lignin has strongly antioxidant activity.
|
-
- HY-N0417
-
|
Cucurbitacin E
α-Elaterin; α-Elaterine
|
CDK
Autophagy
|
Cancer
|
|
Cucurbitacin E is a natural compound which from the climbing stem of Cucumic melo L. Cucurbitacin E significantly suppresses the activity of the cyclin B1/CDC2 complex.
|
-
- HY-N0901B
-
|
Corynoxine hydrochloride
|
Autophagy
|
Cancer
Neurological Disease
|
|
Corynoxine hydrochloride, a tetracyclic oxindole alkaloid, is isolated from the hooks of Uncaria macrophylla. Corynoxine hydrochloride is a natural autophagy enhancer that promotes the clearance of alpha-synuclein via Akt/mTOR pathway.
|
-
- HY-13821
-
|
Epoxomicin
BU-4061T
|
Proteasome
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Epoxomicin (BU-4061T) is an epoxyketone-containing natural product and a potent, selective and irreversible proteasome inhibitor. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier. Epoxomicin has strongly antitumor and anti-inflammatory activity.
|
-
- HY-N0240
-
|
Herbacetin
|
Others
|
Cancer
|
|
Herbacetin is a natural flavonoid from flaxseed, exerts various pharmacological activities, including antioxidant, anti-inflammatory and anticancer effects. Herbacetin is an Ornithine decarboxylase (ODC) allosteric inhibitor, directly binds to Asp44, Asp243, and Glu384 on ODC. Ornithine decarboxylase (ODC) is a rate-limiting enzyme in the first step of polyamine biosynthesis.
|
-
- HY-17389
-
|
Genipin
(+)-Genipin
|
Autophagy
|
Cancer
Metabolic Disease
Inflammation/Immunology
Neurological Disease
|
|
Genipin ((+)-Genipin) is a natural crosslinking reagent derived from Gardenia jasminoides Ellis fruits. Genipin inhibits UCP2 (uncoupling protein 2) in cells. Genipin has a variety of bioactivities, including modulation on proteins, antitumor, anti-inflammation, immunosuppression, antithrombosis, and protection of hippocampal neurons. Genipin also can be used for type 2 diabetes research.
|
-
- HY-120878
-
|
CXCR2-IN-2
|
CXCR
|
Inflammation/Immunology
|
|
CXCR2-IN-2 is a selective, brain penetrant, and orally bioavailable CXCR2 antagonist (IC50=5.2 nM/1 nM in β-arrestin assay/CXCR2 Tango assay, respectively). CXCR2-IN-2 displays ~730-fold selectivity over CXCR1 and >1900-fold selectivity over all other chemokine receptors. CXCR2-IN-2 inhibits human whole blood Gro-α induced CD11b expression with an IC50 of 0.04 μM.
|
-
- HY-N0360
-
|
Dihydrotanshinone I
|
SARS-CoV
|
Cardiovascular Disease
|
|
Dihydrotanshinone I is a natural compound extracted from Salvia miltiorrhiza Bunge which has been widely used for treating cardiovascular diseases. Dihydrotanshinone I exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-N0876
-
|
Arenobufagin
|
Others
|
Cancer
|
|
Arenobufagin is a natural bufadienolide from toad venom; has potent antineoplastic activity against HCC HepG2 cells as well as corresponding multidrug-resistant HepG2/ADM cells.
|
-
- HY-N7029
-
|
3',4',5',5,7-Pentamethoxyflavone
|
Others
|
Cancer
|
|
3',4',5',5,7-Pentamethoxyflavone, a natural flavonoid extracted from Rutaceae plants, sensitizes chemoresistant cancer cells to chemotherapeutic drugs by inhibition of Nrf2 pathway.
|
-
- HY-N2445
-
|
Flavokawain C
|
Apoptosis
|
Cancer
|
|
Flavokawain C is a natural chalcone found in Kava root. Flavokawain C exerts cytotoxicity against human cancer cell lines, with an IC50 of 12.75 μM for HCT 116 cells.
|
-
- HY-114360
-
|
Taurohyodeoxycholic acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Taurohyodeoxycholic acid is the tauroconjugated form of Hyodeoxycholic acid (HDCA, a dihydroxylated natural bile acid). Taurohyodeoxycholic acid induces a biliary phospholipid secretion and suggests a hepatoprotective potential. Taurohyodeoxycholic acid also can promote gallstone dissolution.
|
-
- HY-N6038
-
|
Gartanin
|
Others
|
Cancer
|
|
Gartanin is a natural xanthone of mangosteen, with antioxidant, anti-inflammatory, antifungal, neuroprotective and antineoplastic properties. Gartanin induces cell cycle arrest and autophagy and suppresses migration in human glioma cells.
|
-
- HY-N7650
-
|
Dihydroseselin
|
Others
|
Others
|
|
Dihydroseselin is a derivative of 7-hydroxycoumarin (HY-N0573). 7-hydroxycoumarin, a natural product of the coumarin family, is a fluorescing compound which can be used as a sunscreen agent
|
-
- HY-N0163
-
-
- HY-N0370
-
|
Bergapten
5-Methoxypsoralen
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Bergapten is a natural anti-inflammatory and anti-tumor agent isolated from bergamot essential oil, other citrus essential oils and grapefruit juice. Bergapten is inhibitory towards mouse and human CYP isoforms.
|
-
- HY-15724A
-
|
Vercirnon sodium
GSK-1605786 sodium; CCX282-B sodium; Traficet-EN sodium
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK1605786A) sodium is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon sodium inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon sodium is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon sodium is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-15724
-
|
Vercirnon
GSK-1605786; CCX282-B; Traficet-EN
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
Vercirnon (GSK1605786A) is an orally bioavailable, selective, and potent antagonist of CCR9. Vercirnon inhibits CCR9-mediated Ca 2+ mobilization and chemotaxis on Molt-4 cells with IC50 values of 5.4 and 3.4 nM, respectively. Vercirnon is selective for CCR9 over CCR1-12 and CX3CR1-7 (IC50s>10 µM for all). Vercirnon is an equipotent inhibitor of CCL25-directed chemotaxis of both splice forms of CCR9 (CCR9A and CCR9B) with IC50 values of 2.8 and 2.6 nM, respectively.
|
-
- HY-N0551
-
|
Wedelolactone
|
Caspase
Lipoxygenase
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Wedelolactone, a natural product from Ecliptae herba, suppresses LPS-induced caspase-11 expression by directly inhibiting the IKK Complex. Wedelolactone inhibits 5-lipoxygenase (5-Lox) (IC50~2.5 μM) activity by an oxygen radical scavenging mechanism. Wedelolactone induces caspase-dependent apoptosis in prostate cancer cells via downregulation of PKCε without inhibiting Akt. Anti-cancer, anti-inflammatory, and antioxidant activities.
|
-
- HY-W013715A
-
-
- HY-106950
-
|
Fosfructose
Diphosphofructose; Esafosfan; FDP
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Fosfructose (Diphosphofructose;Esafosfan;FDP) is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.
|
-
- HY-13407
-
|
Gossypol
BL 193
|
Bcl-2 Family
|
Cancer
|
|
Gossypol, a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
|
-
- HY-18569
-
|
3-Indoleacetic acid
Indole-3-acetic acid; 3-IAA
|
Endogenous Metabolite
|
Others
|
|
3-Indoleacetic acid (Indole-3-acetic acid) is the most common natural plant growth hormone of the auxin class. It can be added to cell culture medium to induce plant cell elongation and division.
|
-
- 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-N2572
-
|
Nepetin
6-Methoxyluteolin
|
Others
|
Inflammation/Immunology
|
|
Nepetin (6-Methoxyluteolin) is a natural flavonoid isolated from Eupatorium ballotaefolium HBK with potent anti-inflammatory activities. Nepetin inhibits IL-6, IL-8 and MCP-1 secretion with IC50 values of 4.43 μM, 3.42 μM and 4.17 μM, respectively in ARPE-19 cells.
|
-
- HY-18085S
-
|
Quercetin D5
|
PI3K
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Quercetin D5 is a deuterium labeled Quercetin. Quercetin, a natural flavonoid, is a stimulator of recombinant SIRT1 and also a PI3K inhibitor with IC50 of 2.4 μM, 3.0 μM and 5.4 μM for PI3K γ, PI3K δ and PI3K β, respectively.
|
-
- 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-N0471A
-
|
L-Hyoscyamine sulfate
Daturine sulfate
|
mAChR
|
Neurological Disease
|
|
L-Hyoscyamine sulfate (Daturine sulfate), a natural plant tropane alkaloid, is a potent and competitive muscarinic receptor (MR) antagonist. L-Hyoscyamine sulfate is a levo-isomer to Atropine (HY-B1205).
|
-
- HY-N2050
-
-
- 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-N6850
-
|
Calenduloside E
|
HSP
Endogenous Metabolite
|
|
|
Calenduloside E (CE) is a natural pentacyclic triterpenoid saponin extracted from Aralia elata. Calenduloside E (CE) has anti-apoptotic potent by targeting heat shock protein 90 (Hsp90).
|
-
- HY-N5083
-
|
Saponarin
|
Others
|
Inflammation/Immunology
|
|
Saponarin is a natural flavonoid isolated from Gypsophila trichotoma, with antioxidant, anti-inflammatory and hepatoprotective activities. Saponarin activates AMPK in a calcium-dependent manner, thus regulating gluconeogenesis and glucose uptake.
|
-
- HY-N6969
-
|
Dicentrine
|
Adrenergic Receptor
|
Endocrinology
|
|
Dicentrine is a natural product isolated from the plant Lindera megaphylla with antihypertensive effect. Dicentrine is an α1-adrenoceptor antagonist which has effective against human hyperplastic prostates.
|
-
- HY-100560
-
|
Abscisic acid
(S)-(+)-Abscisic acid; ABA
|
Endogenous Metabolite
Proton Pump
|
Metabolic Disease
|
|
Abscisic acid ((S)-(+)-Abscisic acid), an orally active phytohormone in fruits and vegetables, is an endogenously produced mammalian hormone. Abscisic acid is a growth inhibitor and can regulate many aspects of plant growth and development. Abscisic acid inhibits proton pump (H +-ATPase) and leads to the plasma membrane depolarization in a Ca 2+-dependent manner. Abscisic acid, a LANCL2 natural ligand, is a potent insulin-sensitizing compound and has the potential for pre-diabetes, type 2 diabetes and metabolic syndrome.
|
-
- HY-108584
-
|
Flindokalner
BMS-204352
|
Potassium Channel
|
Neurological Disease
|
|
Flindokalner (BMS-204352) is a potassium channel modulator. Flindokalner is a positive modulator of all neuronal Kv7 channel subtypes expressed in HEK293 cells. Flindokalner is also a large conductance calcium-activated K channel (BKca) positive modulator. Flindokalner shows a negative modulatory activity at Kv7.1 channels (Ki=3.7 μM), and acts as a negative modulator of GABAA receptors. Flindokalner shows anxiolytic efficacy in vivo.
|
-
- HY-N6882
-
-
- HY-N7247
-
|
Thiochrome
|
mAChR
|
Metabolic Disease
|
|
Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
|
-
- HY-N7117
-
-
- 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-N4093
-
|
Astringin
trans-Astringin
|
Others
|
Cancer
|
|
Astringin (trans-Astringin) is a natural glycoside found in the bark of Picea sitchensis and Picea abies (Norway spruce), in Vitis vinifera cell cultures and in wine. Astringin has potent antioxidant capacity and cancer-chemopreventive activity.
|
-
- HY-B0234
-
|
Estrone
E1; Oestrone
|
Estrogen Receptor/ERR
Endogenous Metabolite
|
Endocrinology
Cancer
|
|
Estrone (E1) is a natural estrogenic hormone. Estrone is the main representative of the endogenous estrogens and is produced by several tissues, especially adipose tissue. Estrone is the result of the process of aromatization of androstenedione that occurs in fat cells.
|
-
- HY-119412
-
|
Biliatresone
|
Others
|
Metabolic Disease
|
|
Biliatresone is a natural toxin isolated from Dysphania glomulifera and D. littoralis. Biliatresone, a 1,2-diaryl-2-propenone class of isoflavonoid, produces extrahepatic biliary atresia in a zebrafish model.
|
-
- HY-N7072
-
-
- HY-N7020
-
|
Cinobufaginol
|
Others
|
Cancer
|
|
Cinobufaginol is a natural bufadienolide isolated from toad venom which has been widely used for centuries in China to treat different diseases, especially for cancer. Cinobufaginol potently inhibits the activity against human nasopharyngeal carcinoma cell lines with IC50s of 803 μΜ and 1.270 μΜ for CNE-1 and CNE-2Z, respectively.
|
-
- HY-114325
-
-
- HY-W009708
-
|
Bis(2-methyl-3-furyl)disulfide
|
Others
|
Others
|
|
Bis(2-methyl-3-furyl)disulfide, compound (2), is intended to provide a flavoring compound to enhance a natural feeling, a fresh feeling and a milk-rich feeling of a milk-related product.
|
-
- HY-17510
-
|
Gossypol (acetic acid)
(±)-Gossypol-acetic acid; BL-193 (acetic acid)
|
Bcl-2 Family
|
Cancer
|
|
Gossypol acetic acid ((±)-Gossypol-acetic acid), a natural product isolated from cottonseeds and roots, binds to Bcl-xL protein and Bcl-2 protein with Kis of 0.5-0.6 μM and 0.2-0.3 mM, respectively.
|
-
- HY-N0723
-
|
Neomangiferin
|
Others
|
Metabolic Disease
|
|
Neomangiferin is a natural C-glucosyl xanthone isolated from m the dried rhizome of Anemarrhena asphodeloides. Neomangiferin has significant therapeutic effects on high-fat diet-induced nonalcoholic fatty liver disease (NAFLD) in rats.
|
-
- HY-N2359
-
|
Chelerythrine
|
PKC
Bcl-2 Family
Apoptosis
Autophagy
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
Chelerythrine is a natural alkaloid, acts as a potent and selective Ca 2+/phospholopid-dependent PKC antagonist, with an IC50 of 0.7 μM. Chelerythrine has antitumor, antidiabetic and anti-inflammatory activity. Chelerythrine inhibits the BclXL-Bak BH3 peptide binding with IC50 of 1.5 μM and displaces Bax from BclXL. Chelerythrine triggers apoptosis and autophagy.
|
-
- HY-106950A
-
|
Fosfructose trisodium
Diphosphofructose trisodium; Esafosfan trisodium; FDP trisodium
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Fosfructose trisodium (Diphosphofructose trisodium;Esafosfan trisodium;FDP trisodium) is a cytoprotective natural sugar phosphate for the potential treatment of cardiovascular ischemia, sickle cell anemia and asthma. It acts by stimulating anaerobic glycolysis which generates adenosine triphosphate under ischemic conditions.
|
-
- HY-W016784
-
-
- HY-N4253
-
|
Kudinoside D
|
Others
|
Metabolic Disease
|
|
Kudinoside D is a main natural component of triterpenoid saponin derived from Ilex kudingcha. Kudinoside D suppresses adipogenesis through modulation of the AMPK pathway in 3T3-L1 adipocytes.
|
-
- HY-15731
-
-
- HY-A0282
-
|
L-Ornithine L-aspartate
|
Others
|
Metabolic Disease
|
|
L-Ornithine L-aspartate is a stable salt of two natural nonessential L-amino acids: ornithine and aspartic acid. L-Ornithine L-aspartate lowers blood ammonia concentration and to eliminate symptoms of hepatic encephalopathy associated with liver cirrhosis.
|
-
- HY-121271
-
|
Kadsurin
|
Others
|
Inflammation/Immunology
|
|
Kadsurin, a natural compound from the stems of Kadsura heteroclita (Schizandraceae), results in significant decreases of CCL4- induced lipid-peroxidation products, such as thiobarbituric acid reactive substances (TBA-RS), conjugated dienes and fluorescent products in the liver of mice.
|
-
- HY-N0295
-
|
Protocatechualdehyde
Catechaldehyde; Protocatechuic aldehyde; Rancinamycin IV
|
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
|
|
Protocatechualdehyde (Catechaldehyde), a natural polyphenol compound isolated from the roots of radix Salviae Miltiorrhizae, is associated with a wide variety of biological activities and has been widely used in medicine as an antioxidant, anti-aging, an antibacterial and anti-inflammatory agent.
|
-
- HY-W011241
-
|
Cinchonine hydrochloride
(8R,9S)-Cinchonine hydrochloride; LA40221 hydrochloride
|
Apoptosis
Parasite
|
Cancer
|
|
Cinchonine hydrochloride ((8R,9S)-Cinchonine hydrochloride) is a natural alkaloid present in Cinchona bark, with antimalarial activity. Cinchonine hydrochloride activates endoplasmic reticulum (ER) stress-induced apoptosis in human liver cancer cells.
|
-
- HY-12597
-
|
Quisqualic acid
L-Quisqualic acid
|
iGluR
mGluR
|
Neurological Disease
|
|
Quisqualic acid (L-Quisqualic acid), a natural analog of glutamate, is a potent and pan two subsets (iGluR and mGluR) of excitatory amino acid (EAA) agonist with an EC50 of 45 nM and a Ki of 10 nM for mGluR1R. Quisqualic acid is isolated from the fruits of Quisqualis chinensis.
|
-
- HY-N0511
-
|
Aristolochic acid B
|
Others
|
Cancer
|
|
Aristolochic acid B is one of the major components of Aristolochic acids (AA) which are natural products derived from taxa in the Aristolochiaceae. Aristolochic acid is known to be a potent mutagen and carcinogen. Aristolochic acid B showes more carcinogenic risk than Aristolochic acid A in vivo.
|
-
- HY-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-N6959
-
|
Osmundacetone
|
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
|
|
Osmundacetone is a natural product isolated from Osmundae Rhizoma, with neuroprotective and anti-apoptotic effects. Osmundacetone has DPPH scavenging activity and protects neurological cell from oxidative stress. Osmundacetone can be a potential agent for the research of neurodegenerative diseases.
|
-
- HY-113046
-
|
5-Methyltetrahydrofolic acid
5-Methyl THF
|
Endogenous Metabolite
|
Metabolic Disease
|
|
5-Methyltetrahydrofolic acid (5-Methyl THF) is a biologically active form of folic acid. 5-Methyltetrahydrofolic acid is a methylated derivate of tetrahydrofolate. 5-Methyltetrahydrofolic acid is the predominant natural dietary folate and the principal form of folate in plasma and cerebrospinal fluid.
|
-
- HY-15464
-
|
(R)-(-)-Gossypol
AT-101; R-(-)-gossypol acetic acid
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
(R)-(-)-Gossypol (AT-101) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
|
-
- HY-134581
-
|
Enpatoran
M5049
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) is an orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran can block both innate and adaptive autoimmunity. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran (M5049) can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran (M5049) inhibits cytokine release, causing great potency in pharmacokinetic/pharmacodynamic properties.
|
-
- HY-N0530
-
|
Dryocrassin ABBA
Dryocrassin
|
Influenza Virus
Bacterial
|
Infection
|
|
Dryocrassin ABBA (Dryocrassin) is a flavonoid natural product derived from Dryopteris crassirhizoma, with antiviral and antibacterial activities. Dryocrassin ABBA exhibits antiviral activity against H5N1 avian influenza virus. Dryocrassin ABBA inhibits the coagulase activity of Staphylococcus aureus vWbp. Dryocrassin ABBA suppresses immunostimulatory function of dendritic cells and prolongs skin allograft survival.
|
-
- HY-N4201
-
|
β-Hydroxyisovalerylshikonin
|
EGFR
Src
|
Cancer
|
|
Beta-hydroxyisovalerylshikonin is a natural product isolated from Lithospermium radix, acts as a potent inhibitor of protein tyrosine kinases (PTK), with IC50s of 0.7μM and 1μM for EGFR and v-Src receptor, respectively. Beta-hydroxyisovalerylshikonin is effective against a wide variety of tumor cell lines, and most efficiently induces cell-death in NCI-H522 and DMS114 cells.
|
-
- HY-N1131
-
|
Triacetonamine
2,2,6,6-Tetramethyl-4-piperidone
|
Others
|
Others
|
|
Triacetonamine is used as an intermediate for the synthesis of pharmaceutical products, pesticides and photostabilizers for polymers. Triacetonamine is an artifact of plant and fungal extracts using acetone and ammonium hydroxide or natural occurrence of ammonium salts in various steps of the isolation procedures. TAA is the main component of the pyrolysis oil.
|
-
- HY-N2099
-
|
Onjisaponin B
|
Autophagy
|
Neurological Disease
|
|
Onjisaponin B is a natural product derived from Radix Polygalae. Onjisaponin B enhances autophagy and accelerates the degradation of mutant α-synuclein and huntingtin in PC-12 cells, and exbibits potential therapeutic effects on Parkinson disease and Huntington disease.
|
-
- HY-D0020
-
|
2,2'-Bipyridine
|
Others
|
Infection
|
|
2,2'-Bipyridine is the unique molecular scaffold of the bioactive natural products represented by caerulomycins (CAEs) and collismycins (COLs). 2,2'-Bipyridine is extensively used as the core structure of many chelating ligands by acting as a bridge in the arrangement of the catalytic center.
|
-
- 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-W030319
-
-
- HY-15464A
-
|
(R)-(-)-Gossypol acetic acid
AT-101 (acetic acid); (-)-Gossypol acetic acid; (R)-Gossypol acetic acid
|
Bcl-2 Family
Autophagy
|
Cancer
|
|
(R)-(-)-Gossypol acetic acid (AT-101 (acetic acid)) is the levorotatory isomer of a natural product Gossypol. AT-101 is determined to bind to Bcl-2, Mcl-1 and Bcl-xL proteins with Kis of 260±30 nM, 170±10 nM, and 480±40 nM, respectively.
|
-
- HY-N2228
-
|
(-)-Epigallocatechin-3-(3''-O-methyl) gallate
(-)-EGCG-3''-O-ME
|
Others
|
Cancer
|
|
(-)-Epigallocatechin-3-(3''-O-methyl) gallate is a natural product isolated from the tea leaf, with strong antioxidative activity. (-)-Epigallocatechin-3-(3''-O-methyl) gallate has a strong cytotoxic activity for rat cancer cells.
|
-
- HY-N6861
-
|
Lucidenic acid B
|
Apoptosis
|
Cancer
|
|
Lucidenic acid B is a natural compound isolated from Ganoderma lucidum, induces apoptosis of cancer cells, and causes the activation of caspase-9 and caspase-3, and cleavage of PARP. Lucidenic acid B does not affect the cell cycle profile, or the number of necrotic cells.
|
-
- 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-18980
-
|
Rottlerin
MAllotoxin; NSC 56346; NSC 94525
|
PKC
Autophagy
Apoptosis
|
Infection
Cancer
|
|
Rottlerin, a natural product purified from Mallotus Philippinensis, is a specific PKC inhibitor, with IC50 values for PKCδ of 3-6 μM, PKCα,β,γ of 30-42 μM, PKCε,η,ζ of 80-100 μM. Rottlerin acts as a direct mitochondrial uncoupler, and stimulates autophagy by targeting a signaling cascade upstream of mTORC1. Rottlerin induces apoptosis via caspase 3 activation.
|
-
- HY-N0136
-
|
Taxifolin
(+)-Dihydroquercetin; (+)-Taxifolin
|
Autophagy
Tyrosinase
|
Inflammation/Immunology
|
|
Taxifolin ((+)-Dihydroquercetin) exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
|
-
- HY-N1389
-
|
Carmine
Carmine red
|
Others
|
Inflammation/Immunology
|
|
Carmine (Carmine red), a natural red dye extracted from the dried females of the insect Dactylopius coccus var. Costa (cochineal). Carmine is a widely used food additive. Carmine provokes both an immediate hypersensitivity and a delayed systemic response with cutaneous expression.
|
-
- HY-N2375
-
|
L-Quebrachitol
|
Wnt
β-catenin
|
Metabolic Disease
|
|
L-Quebrachitol is a natural product isolated from many plants, promotes osteoblastogenesis by uppregulation of BMP-2, runt-related transcription factor-2 (Runx2), MAPK (ERK, JNK, p38α), and Wnt/β-catenin signaling pathway.
|
-
- HY-N2621
-
|
Evodol
|
Others
|
Inflammation/Immunology
|
|
Evodol is a natural product isolated from the dried and nearly ripe fruits of Euodia rutaecarpa. Evodol shows inhibitory activity against NO production. Evodol possesses larvicidal activity against the Asian tiger mosquitoes with a LC50 value of 32.43 μg/ml.
|
-
- HY-N6711
-
|
Equisetin
|
HIV Integrase
|
Infection
|
|
Equisetin is an N-methylserine-derived acyl tetramic acid isolated from a terrestrial fungus Fusarium equiseti NRRL 5537. Equisetin is a tetramate-containing natural product with antibiotic and cytotoxic activity. Equisetin inhibits the growth of Gram-positive bacteria and HIV-1 integrase activity but shows no activity against Gram-negative bacteria. Equisetin is a Quorum-sensing inhibitor (QSI) that attenuates QS-regulated virulence phenotypes in P. aeruginosa without affecting the growth of bacterias, serves as a leading compound for the treatment of P. aeruginosa infections.
|
-
- HY-14602
-
|
Tramiprosate
Homotaurine; 3-Amino-1-propanesulfonic acid
|
Amyloid-β
|
Cancer
|
|
Tramiprosate (Homotaurine), an orally active and brain-penetrant natural amino acid found in various species of red marine algae. Tramiprosate binds to soluble Aβ and maintains Aβ in a non-fibrillar form. Tramiprosate is also a GABA analog and possess neuroprotection, anticonvulsion and antihypertension effects.
|
-
- HY-B1125
-
-
- HY-125098
-
|
Illudin S
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
Infection
|
|
Illudin S, a cytotoxic Illudin, is a natural sesquiterpene with strong anti-tumour and antiviral activities. Illudin S has genotoxic activities. Illudin S blocks the G1-S phase interface of the cell cycle in human leukemia cells.
|
-
- HY-N0733
-
-
- HY-N0393
-
|
Glabridin
|
PPAR
Reactive Oxygen Species
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Glabridin is a natural isoflavan from Glycyrrhiza glabra, binds to and activates PPARγ, with an EC50 of 6115 nM. Glabridin exhibits antioxidant, anti-bacterial, anti-nephritic, anti-diabetic, anti-fungal, antitumor, anti-inflammatory, antiosteoporotic, cardiovascular protective, neuroprotective and radical scavenging activities.
|
-
- HY-W015371
-
|
Ethyl phenylacetate
|
Others
|
Others
|
|
Ethyl phenylacetate is a natural flavouring ingredien, and its sensory threshold is near 73 µg/L. Ethyl phenylacetate is a “greener" solvent with low toxicity. Ethyl phenylacetate is a non-mutagenic and is a Kosher food additive. Ethyl phenylacetate gives to the wines a strong honey-like character.
|
-
- 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-N0279
-
-
- HY-B1000A
-
|
L-SelenoMethionine
|
Endogenous Metabolite
Apoptosis
|
Cancer
|
|
L-SelenoMethionine, an L-isomer of Selenomethionine, is a major natural food-form of selenium. L-SelenoMethionin is a cancer chemopreventive agent that can reduce cancer incidence by dietary supplementation and induce apoptosis of cancer cells. L-SelenoMethionine also can increase expression of glutathione peroxidase.
|
-
- HY-B0867
-
|
2,4-D Butyl ester
|
Others
|
Others
|
|
2,4-D Butyl ester is an organic phenoxy herbicide and used to control woody broad-leaf weeds. 2,4-D butyl ester produces its herbicidal effect by mimicking natural plant growth hormones causing plants to grow too rapidly to survive.
|
-
- HY-N0136A
-
|
(±)-Taxifolin
(±)-Dihydroquercetin
|
Autophagy
Tyrosinase
|
Inflammation/Immunology
|
|
(±)-Taxifolin ((±)-Dihydroquercetin) is the racemate of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
|
-
- HY-N0022
-
|
Isoacteoside
Isoverbascoside
|
Others
|
Metabolic Disease
|
|
Isoacteoside is a natural compound which exhibit significant inhibition of advanced glycation end product formation with IC50 values of 4.6-25.7 μM, compared with those of aminoguanidine (IC50=1,056 μM) and quercetin (IC50=28.4 μM) as positive controls.
|
-
- HY-N6002
-
|
3'-Hydroxypterostilbene
|
Apoptosis
Autophagy
|
Cancer
|
|
3'-Hydroxypterostilbene, a natural pterostilbene analogue, effectively inhibits the growth of human colon cancer cells (IC50s of 9.0, 40.2, and 70.9 µM for COLO 205, HCT-116, and HT-29 cells, respectively) by inducing apoptosis and autophagy. 3'-Hydroxypterostilbene inhibits the PI3K/Akt/mTOR/p70S6K, and p38MAPK pathways and activates the ERK1/2, JNK1/2 MAPK pathways.
|
-
- HY-N7516
-
|
4'-Hydroxy-2,4-dimethoxychalcone
|
Parasite
Bacterial
Fungal
|
Infection
|
|
4'-Hydroxy-2,4-dimethoxychalcone is a natural chalcone derivatives in the red herbal resin of Dracaena cochinchinensis. 4'-Hydroxy-2,4-dimethoxychalcone displays a wide range of biological activities including antimalarial, antiprotozoal, antibacterial, antifungal activity.
|
-
- HY-N1478
-
|
Gardenoside
|
Others
|
Neurological Disease
|
|
Gardenoside is a natural compound found in Gardenia fruits, with hepatoprotective properties. Gardenoside suppresses the pain of chronic constriction injury by regulating the P2X3 and P2X7 receptors. Gardenoside has an inhibitory effect on free fatty acids (FFA)-induced cellular steatosis.
|
-
- HY-N0136B
-
|
(-)-Taxifolin
(-)-Dihydroquercetin
|
Others
|
Inflammation/Immunology
|
|
(-)-Taxifolin is the less active enantiomer of Taxifolin. Taxifolin exhibits important anti-tyrosinase activity. Taxifolin exhibits significant inhibitory activity against collagenase with an IC50 value of 193.3 μM. Taxifolin is an important natural compound with antifibrotic activity. Taxifolin is a free radical scavenger with antioxidant capacity.
|
-
- HY-113354
-
|
Anserine
|
Endogenous Metabolite
|
Neurological Disease
|
|
Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice.
|
-
- HY-N0655
-
-
- HY-N0539
-
|
Calceolarioside B
|
Others
|
Cancer
|
|
Calceolarioside B is a natural product isolated from Stauntonia hexaphylla leaves. Calceolarioside B exhibits significant inhibitory activity against rat lens aldose reductase (RLAR) with an IC50 of 23.99 μM. Calceolarioside B displays inhibitory effect on DPPH radical scavenging activity with an IC50 of 94.60 μM .
|
-
- HY-N0487
-
-
- HY-W087919
-
|
5-Methyl-2-furanmethanol
|
Others
|
Others
|
|
5-Methyl-2-furanmethanol is a natural product that can be isolated from the essential oil of D. rupicola Biv.. 5-Methyl-2-furanmethanol also acts as a oxidative product of 2,5 dimethylfuran (DMF) by cytochrome P450 (CYP).
|
-
- HY-N0646
-
|
Silydianin
|
Phosphatase
|
Cancer
|
|
Silydianin is an active constituent of Silybium marianum, with exhibit anti-collagenase, antitumor and anti-elastase activities. Silydianin is a natural protein tyrosine phosphatase 1B (PTP1B) with an IC50 of 17.38 μM. Silydianin has inhibitory effect on the in vitro production and release of oxidative products.
|
-
- HY-N0446
-
|
10-Methoxycamptothecin
|
Others
|
Cancer
|
|
10-Methoxycamptothecin is a natural bioactive derivative of camptothecin (CPT) isolated from Camptotheca acuminata, and has been confirmed to possess high anti-cancer properties. 10-Methoxycamptothecin has higher cytotoxicity than 10-hydroxycamptothecin by testing antitumor activity against 2774 cell lines.
|
-
- HY-N0424
-
|
Cycloastragenol
Cyclogalagenin; Cyclogalegenin; Cyclogalegigenin
|
Telomerase
|
Others
|
|
Cycloastragenol is a natural tetracyclic triterpenoid, is identified when screening Astragalus membranaceus extracts for active ingredients with antiaging properties. Cycloastragenol is a potent telomerase activator in neuronal cells. Cycloastragenol also has other pharmacological effects, including anti-inflammatory and anti-oxidative properties.
|
-
- HY-P1422
-
|
Spadin
|
Potassium Channel
|
Neurological Disease
|
|
Spadin, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin binds specifically to TREK-1 with an affinity of 10 nM. Spadin is an efficient antidepressant in mice.
|
-
- HY-N0501
-
|
11-oxo-mogroside V
|
Reactive Oxygen Species
|
Metabolic Disease
|
|
11-oxo-mogroside V is a natural sweetener, isolated from the fruits of Momordica grosvenori, exhibits strong antioxidant activity. It exhibits significant inhibitory effects on reactive oxygen species (O2 -, H2O2 and *OH) with EC50 of 4.79, 16.52, and 146.17 μg/mL, respectively.
|
-
- HY-19975
-
|
RN-1734
|
TRP Channel
|
Neurological Disease
|
|
RN-1734 is selective antagonist of the TRPV4 channel, completely antagonizes 4αPDD-mediated activation of TRPV4 with comparable, low micromolar IC50s for all three species (hTRPV4: 2.3 μM, mTRPV4: 5.9 μM, rTRPV4: 3.2 μM). RN-1734 clearly decreases the production of tumor necrosis factor α (TNF-α) and interleukin 1β (IL-1β) without altering the number of olig2-positive cells.
|
-
- HY-112811
-
|
PROTAC CDK9 degrader-2
|
PROTAC
CDK
|
Cancer
|
|
PROTAC CDK9 degrader-2 (compounds 11c) is a potent and selective CDK9 degrader based on PROTAC, with an IC50 of 17 μM in MCF-7 cell lines. Natural product Wogonin binds ubiquitin E3 ligase cereblon (CRBN) via a linker to form PROTAC.
|
-
- HY-107784
-
|
Ectoine
|
Bacterial
|
Inflammation/Immunology
|
|
Ectoine is a natural cell protectant, an amino acid derivate produced by bacteria living under extremely harsh environmental conditions. Ectoine serves as an osmoregulatory compatible solute, increasing the hydration of the skin surface and stabilizing lipid layers, which is useful in skincare. Ectoine demonstrates a good safety profile for the treatment of allergic rhinitis.
|
-
- HY-W001160
-
|
5-Hydroxyindole
|
Others
|
Others
|
|
5-Hydroxyindole, a hydroxylated indole, can be found in a vast array of pharmacologically active agents and natural products. 5-Hydroxyindole slows desensitization of the 5-HT3 receptor-mediated ion current in N1E-115 neuroblastoma cells.
|
-
- HY-N7384
-
-
- HY-126403
-
|
Ethoxylated hydrogenated castor oil
PEG-40 hydrogenated castor oil; Macrogolglycerol hydroxystearate; Castor oil, hydrogenated, polyethoxylated
|
Others
|
Others
|
|
Ethoxylated hydrogenated castor oil (PEG-40 hydrogenated castor oil) is a combination of synthetic polyethylene glycol (PEG) with natural castor oil. Ethoxylated hydrogenated castor oil can be used to emulsify and solubilize oil-in-water (o/w) emulsions. Ethoxylated hydrogenated castor oil can be used as a cosolvent in vivo.
|
-
- HY-N6966
-
-
- HY-16561
-
|
Resveratrol
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Cancer
Infection
Inflammation/Immunology
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator. Resveratrol is a potent pregnane X receptor (PXR) inhibitor. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model. Resveratrol increases production of NO in endothelial cells.
|
-
- HY-113629
-
|
2-Keto-D-Glucose
D-Glucosone; D-Arabino-hexos-2-ulose
|
Others
|
Infection
|
|
2-Keto-D-Glucose (D-Glucosone) is a key intermediate in a secondary metabolic pathway leading to the antibiotic Cortalcerone. 2-Keto-D-Glucose is also an intermediate in the conversion of D-glucose into D-fructose. 2-Keto-D-Glucose is found in various natural sources, including fungi, algae, and shellfish.
|
-
- HY-N1131B
-
|
Triacetonamine monohydrate
2,2,6,6-Tetramethyl-4-piperidone monohydrate
|
Others
|
Others
|
|
Triacetonamine (2,2,6,6-Tetramethyl-4-piperidone) monohydrate is used as an intermediate for the synthesis of pharmaceutical products, pesticides and photostabilizers for polymers. Triacetonamine monohydrate is an artifact of plant and fungal extracts using acetone and ammonium hydroxide or natural occurrence of ammonium salts in various steps of the isolation procedures. Triacetonamine monohydrate is the main component of the pyrolysis oil.
|
-
- HY-P1422A
-
|
Spadin TFA
|
Potassium Channel
|
Neurological Disease
|
|
Spadin TFA, a natural peptide derived from a propeptide released in blood, is able to block the TREK-1 (KCNK2 or K2P2.1) channel activity. Spadin TFA binds specifically to TREK-1 with an affinity of 10 nM. Spadin TFA is an efficient antidepressant in mice.
|
-
- HY-W027968
-
|
Coumarin-3-carboxylic Acid
2-Oxochromene-3-carboxylic acid
|
Others
|
Cancer
|
|
Coumarin-3-carboxylic acid (2- Oxochromene-3-carboxylic acid) is an important initial compound for the synthesis of coumarins which are well known natural products for their diverse biological activities. Lanthanide complexes of Coumarin-3-carboxylic acid exhibit antiproliferative activity towards K-562 cell line.
|
-
- 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-125959
-
|
Ucf-101
|
Apoptosis
|
Neurological Disease
Cardiovascular Disease
|
|
Ucf-101 is a selective and competitive inhibitor of pro-apoptotic protease Omi/HtrA2, with an IC50 of 9.5 μM for His-Omi. Ucf-101 exhibits very little activity against various other serine proteases (IC50>200 μM). Ucf-101 has a natural red fluorescence at 543 nm that is used to monitor its ability to enter mammalian cells. Ucf-101 has a significant cardioprotective effect against MI/R injury and also has certain neuroprotective effect.
|
-
- 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-109714
-
|
3,4-Benzocoumarin
|
Others
|
Inflammation/Immunology
|
|
3,4-Benzocoumarin is a kind of the expanded structure of coumarin derivatives.Coumarin is a chemical compound in the benzopyrone chemical class that can be found in many natural species. Coumarins possess variety of biological activities and unique photophysical properties. 3,4-Benzocoumarin, a AOH‐like compound , has the sensibility of the antibody with an IC50 of 919.2 ng/mL.
|
-
- HY-10015
-
|
PAP-1
5-(4-Phenoxybutoxy)psoralen
|
Potassium Channel
|
Inflammation/Immunology
|
|
PAP-1 (5-(4-Phenoxybutoxy)psoralen) is a potent, selective, and orally active Kv1.3 blocker (EC50=2 nM). PAP-1 blocks Kv1.3 in a use-dependent manner and acts by preferentially binding to the C-type inactivated state of the channel. PAP-1 exhibits 23-fold selectivity over Kv1.5 (EC50=45 nM), and further displays 33- to 125-fold selectivity over all other Kv1-family channels. PAP-1 does not exhibit cytotoxic or phototoxic effects.
|
-
- HY-108596
-
|
BL-1249
|
Potassium Channel
|
Inflammation/Immunology
|
|
BL-1249 is a nonsteroidal anti-inflammatory drug (NSAID) and a potassium channel activator. BL-1249 potently activates K2P2.1 (TREK-1) and K2P10.1 (TREK-2) with EC50 values of 5.5 μM and 8.0 μM, respectively. BL-1249 extracellular application activates all TREK subfamily members but has no effect on other K2P subfamilies. BL-1249 exhibits more selective for the bladder (EC50 of 1.26 μM) than vascular tissue (EC50 of 21.0 μM).
|
-
- HY-B0837
-
|
Emamectin Benzoate
MK-244
|
Parasite
GABA Receptor
Reactive Oxygen Species
Apoptosis
|
Infection
Neurological Disease
|
|
Emamectin Benzoate (MK-244), a mixture of the natural Avermectin B1a and B1b, is an orally active nervoussystem toxicant by binding g-aminobutyric (GABA) receptor in insects. Emamectin Benzoate is one of semi-synthetic derivative of Avermectin (HY-15311) with a broadspectrum of insecticidal and acaricidal activity. Emamectin Benzoate induces ROS-mediated DNA damage and cell apoptosis.
|
-
- HY-N2229
-
|
Rhapontigenin
|
Cytochrome P450
Fungal
Bacterial
|
Cancer
Infection
Inflammation/Immunology
|
|
Rhapontigenin is a natural analog of resveratrol with anticancer, antioxidant, antifungal and antibacterial activities. Rhapontigenin is amechanism-based, potent and selective cytochrome P450 1A1 inactivator (IC50
= 400 nM). Rhapontigenin exhibits 400-fold and 23-fold selectivity for P450 1A1 over P450 1A2 and P450 1B1, respectively.
|
-
- HY-N2329
-
-
- HY-131997
-
|
2'MeO6MF
|
GABA Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
2'MeO6MF is a brain-penetrant positive allosteric modulator at α2β1γ2L and all α1-containing GABAA receptors. 2'MeO6MF also can directly activate α2β2/3 and α2β2/3γ2L GABAA receptors. 2'MeO6MF has anxiolytic and sedative effects. 2'MeO6MF offers neuroprotection and improved functional recovery and dampens the stroke-induced inflammatory response.
|
-
- HY-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-123275A
-
|
H-D-Phe-Pip-Arg-pNA hydrochloride
S-2238 hydrochloride
|
Others
|
Others
|
|
H-D-Phe-Pip-Arg-pNA (S-2238) hydrochloride, a chromogenic substrate, is patterned after the N-terminal portion of the A alpha chain of fibrinogen, which is the natural substrate of thrombin. H-D-Phe-Pip-Arg-pNA hydrochloride is specific for thrombin and is used to measure antithrombin-heparin cofactor (AT-III). The AT-III assay using H-D-Phe-Pip-Arg-pNA hydrochloride is sensitive, accurate, and easy to perform.
|
-
- HY-123275C
-
|
H-D-Phe-Pip-Arg-pNA dihydrochloride
S-2238 dihydrochloride
|
Others
|
Others
|
|
H-D-Phe-Pip-Arg-pNA (S-2238) dihydrochloride, a chromogenic substrate, is patterned after the N-terminal portion of the A alpha chain of fibrinogen, which is the natural substrate of thrombin. H-D-Phe-Pip-Arg-pNA dihydrochloride is specific for thrombin and is used to measure antithrombin-heparin cofactor (AT-III). The AT-III assay using H-D-Phe-Pip-Arg-pNA dihydrochloride is sensitive, accurate, and easy to perform.
|
-
- HY-N0594
-
|
Deacetylasperulosidic Acid
|
Interleukin Related
|
Inflammation/Immunology
|
|
Deacetylasperulosidic acid (DAA) is a major phytochemical constituent of Morinda citrifolia fruit. Deacetylasperulosidic acidhas antioxidant activity by increasing superoxide dismutase activity. Deacetylasperulosidic acid has anticlastogenic activity, suppressing the induction of chromosome aberrations in hamster ovary cells and mice. Deacetylasperulosidic acid prevents 4-nitroquinoline 1-oxide (4NQO) induced DNA damage in vitro, suppresses IL-2 production along with the activation of natural killer cells.
|
-
- HY-P0063
-
|
Copper tripeptide
GHK-Cu
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Copper tripeptide (GHK-Cu), a naturally occurring tripeptide, is first isolated from human plasma, but can be found in saliva and urine. During wound healing, Copper tripeptide may be freed from existing extracellular proteins via proteolysis and serves as a chemoattractant for inflammatory and endothelial cells. Copper tripeptide has been shown to increase messenger RNA production for collagen, elastin, proteoglycans, and glycosaminoglycans in fibroblasts. Copper tripeptide is a Natural Modulator of Multiple Cellular Pathways in Skin Regeneration.
|
-
- HY-W009310
-
|
9-cis-Retinal
|
Endogenous Metabolite
|
Others
|
|
9-cis-Retinal is a natural retinoid. Dietary 9-cis-β-carotene generates 9-cis-retinoids via cleavage into 9-cis-retinal. 9-cis Retinal binds to cellular retinol-binding protein-I (CRBP-I) and CRBP-II with Kds of 8 nM and 5 nM, respectively. 9-cis-Retinal expedites differentiation and maturation of rod photoreceptors in retinal organoids.
|
-
- HY-121222
-
|
alpha-Bisabolol
|
Apoptosis
|
Cancer
|
|
alpha-Bisabolol is a nontoxic sesquiterpene alcohol present in natural essential oil, with anticancer activity. alpha-Bisabolol exerts selective anticancer effect on A549 NSCLC cells (IC50=15 μM) via induction of cell cycle arrest, mitochondrial apoptosis and inhibition of PI3K/Akt signalling pathways. alpha-Bisabolol also strongly induces apoptosis in glioma cells.
|
-
- HY-105231
-
|
Bryostatin 1
|
PKC
HIV
|
Cancer
Infection
Inflammation/Immunology
Neurological Disease
|
|
Bryostatin 1 is a natural macrolide isolated from the bryozoan Bugula neritina and is a potent and central nervous system (CNS)-permeable PKC modulator. Bryostatin 1 binds to the isolated C1 domain of Munc13-1 and the full-length Munc13-1 protein with Kis of 8.07 nM and 0.45 nM, respectively. Bryostatin 1 has anti-cancer, anti-inflammatory, neuroprotective, anti-HIV-1 infection properties.
|
-
- HY-N0166
-
-
- 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-137471
-
|
RBPJ Inhibitor-1
RIN1
|
Notch
|
Cancer
|
|
RBPJ Inhibitor-1 (RIN1), the first RBPJ inhibitor, blocks the functional interaction of RBPJ with SHARP. RBPJ Inhibitor-1 (RIN1) inhibits NOTCH-dependent tumor cell proliferation.
|
-
- HY-131344
-
|
mTOR inhibitor-8
|
mTOR
Autophagy
|
Cancer
|
|
mTOR inhibitor-8 is an mTOR inhibitor and autophagy inducer. mTOR inhibitor-8 inhibits the activity of mTOR via FKBP12 and induces autophagy of A549 human lung cancer cells.
|
-
- HY-136123
-
|
Tubulin inhibitor 8
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 8 (Compound 33b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 8 inhibits tubulin polymerization with an IC50 of 0.73 μM. Tubulin inhibitor 8 inhibits K562 cell growth with an IC50 of 14 nM.
|
-
- HY-136122
-
|
Tubulin inhibitor 7
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 7 (Compound 33c) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 7 inhibits tubulin polymerization with an IC50 of 0.52 μM. Tubulin inhibitor 7 inhibits K562 cell growth with an IC50 of 11 nM.
|
-
- HY-136121
-
|
Tubulin inhibitor 6
|
Microtubule/Tubulin
|
Cancer
|
|
Tubulin inhibitor 6 (Compound 14b) is a tubulin inhibitor and a potent inhibitor of multiple cancer cell lines. Tubulin inhibitor 6 inhibits tubulin polymerization with an IC50 of 0.87 μM. Tubulin inhibitor 6 inhibits K562 cell growth with an IC50 of 840 nM.
|
-
- HY-112851
-
-
- HY-112812
-
-
- HY-18353
-
|
mTOR inhibitor-3
|
mTOR
|
Cancer
|
|
mTOR inhibitor-3 is a remarkably selective mTOR inhibitor with a Ki of 1.5 nM. mTOR inhibitor-3 suppresses mTORC1 and mTORC2 in cellular and in vivo pharmacokinetic (PK)/pharmacodynamic (PD) experiments.
|
-
- HY-B0552A
-
-
- HY-112911
-
-
- HY-B0552
-
-
- HY-112722
-
-
- HY-137497
-
|
KRAS inhibitor-9
|
Ras
Apoptosis
|
Cancer
|
|
KRAS inhibitor-9, a potent KRAS inhibitor (Kd=92 μM), blocks the formation of GTP-KRAS and downstream activation of KRAS. KRAS inhibitor-9 binds to KRAS G12D, KRAS G12C and KRAS Q61H protein with a moderate binding affinity. KRAS inhibitor-9 causes G2/M cell cycle arrest and induces apoptosis. KRAS inhibitor-9 selectively inhibits the proliferation of NSCLC cells with KRAS mutation but not normal lung cells.
|
-
- HY-D0843
-
|
N-Ethylmaleimide
NEM
|
Cathepsin
Deubiquitinase
|
Others
|
|
N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor.
|
-
- HY-101275
-
-
- HY-13278A
-
-
- HY-111370
-
|
mTOR inhibitor-2
|
mTOR
|
Cancer
|
|
mTOR inhibitor-2 is a highlt potent, selective and oral mTOR inhibitor with an IC50 of 7 nM. mTOR inhibitor-2 inhibits cellular phosphorylation of mTORC1 (pS6 and p4E-BP1) and mTORC2 (pAKT (S473)) substrates.
|
-
- HY-119369
-
-
- HY-111412
-
-
- HY-21141
-
|
Cysteine protease inhibitor-2
|
Cathepsin
|
Cancer
|
|
Cysteine protease inhibitor-2 is a cysteine protease inhibitor extracted from patent US20070032499A1, compound 12. Cysteine protease inhibitor-2 inhibits the cells growth of DCT116 and PC3 cells with GI50 values of 6.5 μM and 4.4 μM, respectively.
|
-
- HY-17541A
-
-
- HY-17541
-
-
- HY-112914
-
-
- HY-70005
-
-
- HY-130260
-
-
- HY-128703
-
-
- HY-10442
-
-
- HY-138295
-
|
KRAS inhibitor-10
|
Ras
|
Cancer
|
|
KRAS inhibitor-10 selectively and effectively inhibit RAS proteins, and particularly KRAS proteins. KRAS inhibitor-10 is an orally active anti-cancer agent and can be used for cancer research, such as pancreatic cancer, breast cancer, multiple myeloma, leukemia and lung cancer. KRAS inhibitor-10 is a tetrahydroisoquinoline compound (compound 11) extracted from patent WO2021005165 A1.
|
-
- HY-12186
-
|
3-Deazaneplanocin A hydrochloride
DZNep hydrochloride; NSC 617989 hydrochloride; 3-Deazaneplanocin hydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
3-Deazaneplanocin A hydrochloride (DZNep hydrochloride) is a potent histone methyltransferase EZH2 inhibitor. 3-Deazaneplanocin A hydrochlorideis a potent S-adenosylhomocysteine hydrolase (AHCY) inhibitor.
|
-
- HY-112807
-
|
SGLT inhibitor-1
|
SGLT
|
Metabolic Disease
|
|
SGLT inhibitor-1 is a potent dual inhibitor of sodium glucose co-transporter proteins (SGLTs), inhibits hSGLT1 and hSGLT2 with IC50s of 43 nM and 9 nM, respectively.
|
-
- HY-128722
-
-
- HY-110101
-
-
- HY-12202
-
-
- HY-B0543
-
-
- HY-10421
-
-
- HY-B0385
-
-
- HY-32015
-
|
Cot inhibitor-1
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM.
|
-
- HY-P0017
-
-
- HY-112843
-
|
CNT2 inhibitor-1
|
Others
|
Others
|
|
CNT2 inhibitor-1 is a potent concentrative nucleoside transporter 2 Inhibitor (CNT2), with an IC50 of 640 nM for hCNT2.
|
-
- HY-115514A
-
|
BRK inhibitor P21d hydrochloride
|
Others
|
Cancer
|
|
BRK inhibitor P21d hydrochloride is a potent breast tumor kinase (BRK/PTK6) inhibitor with an IC50 of 30 nM. BRK inhibitor P21d hydrochloride inhibits p-SAM68 with an IC50 of 52 nM. BRK inhibitor P21d hydrochloride can be used to evaluate the in vivo activity of BRK inhibitors in xenograft breast tumor models.
|
-
- HY-128859
-
|
EMT inhibitor-2
|
Cytochrome P450
|
Metabolic Disease
|
|
EMT inhibitor-2 (Compound 1) inhibits epithelial-mesenchymal transition (EMT) induced by substances such as IL-1β and TGF-β released from the immunocytes. EMT inhibitor-2 inhibits CYP3A4 testosteron and CYP2C9 with IC50s of 49.72 and 5.54 μM, respectively.
|
-
- HY-136279
-
|
TrxR inhibitor D9
|
Apoptosis
|
Cancer
|
|
TrxR inhibitor D9 is a potent and selective inhibitor of thioredoxin reductase (TrxR), with an EC50 of 2.8 nM. TrxR inhibitor D9 has the capability to inhibit tumor proliferation both in vitro and in vivo.
|
-
- HY-101297
-
|
Z-IETD-FMK
Z-IE(OMe)TD(OMe)-FMK
|
Caspase
|
Cancer
|
|
Z-IETD-FMK (Z-IE(OMe)TD(OMe)-FMK) is a selective and cell permeable caspase-8 inhibitor. Z-IETD-FMK is also a granzyme B inhibitor.
|
-
- HY-100732
-
|
Cambinol
|
Sirtuin
Apoptosis
Phospholipase
|
Cancer
|
|
Cambinol is a SIRT1 and SIRT2 inhibitor with IC50 values of 56 μM and 59 μM, respectively. Cambinol is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-128917
-
-
- HY-15182
-
-
- HY-112474
-
-
- HY-119372
-
-
- HY-13662
-
-
- HY-13662A
-
-
- HY-128617
-
|
Legumain inhibitor 1
|
Others
|
Cancer
|
|
Legumain inhibitor 1 is a potent and selective Legumain inhibitor with an IC50 of 3.6 nM. Legumain inhibitor 1 can be used for cancer research.
|
-
- HY-119937
-
-
- HY-15253
-
-
- HY-112390A
-
|
Syk Inhibitor II
|
Syk
5-HT Receptor
|
Inflammation/Immunology
|
|
Syk Inhibitor II is a potent, high selective and ATP-competitive Syk inhibitor with an IC50 of 41 nM. Syk Inhibitor II inhibits 5-HT release from RBL-cells with an IC50 of 460 nM. Syk Inhibitor II shows less potent against other kinases and has anti-allergic effect.
|
-
- HY-122723
-
|
GOT1 inhibitor-1
|
Others
|
Cancer
|
|
GOT1 inhibitor-1 (compound 2c), a tryptamine-based derivative, acts as a novel, potent and non-covalent inhibitor of glutamate oxaloacetate transaminase 1 (GOT1) with an IC50 of 8.2 uM. GOT1 inhibitor-1 can be used for the research of pancreatic ductal adenocarcinoma (PDAC).
|
-
- HY-13973A
-
-
- HY-104051
-
-
- HY-111347A
-
-
- HY-131100
-
-
- HY-135890
-
-
- HY-15444
-
-
- HY-114317
-
|
MARK4 inhibitor 1
|
Apoptosis
|
Cancer
|
|
MARK4 inhibitor 1 is a potent microtubule affinity-regulating kinase 4 (MARK4) inhibitor, with an IC50 of 1.54 μM. MARK4 inhibitor 1 inhibits cancer cell proliferation, metastasis and induces apoptosis.
|
-
- HY-15002
-
|
AST 487
NVP-AST 487
|
RET
FLT3
VEGFR
c-Kit
Bcr-Abl
|
Cancer
|
|
AST 487 is a RET kinase inhibitor with IC50 of 880 nM, inhibits RET autophosphorylation and activation of downstream effectors, also inhibits Flt-3 with IC50 of 520 nM.
|
-
- HY-135864
-
|
KRAS inhibitor-6
|
Ras
|
Cancer
|
|
KRAS inhibitor-6 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound A.
|
-
- HY-135866
-
|
KRAS inhibitor-8
|
Ras
|
Cancer
|
|
KRAS inhibitor-8 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound C.
|
-
- HY-135826
-
|
Necroptosis-IN-1
|
RIP kinase
|
Cancer
|
|
Necroptosis-IN-1, an analog of Necrostatin-1 (HY-15760), is a potent necroptosi inhibitor. Necroptosis-IN-1 is a RIPK inhibitor.
|
-
- HY-111408
-
-
- HY-100463
-
-
- HY-135865
-
|
KRAS inhibitor-7
|
Ras
|
Cancer
|
|
KRAS inhibitor-7 is a potent KRAS G12C inhibitor, extracted from patent WO2017087528A1, compound B.
|
-
- HY-112607
-
|
Tubulin inhibitor 1
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulin inhibitor 1 is a tubulin inhibitor, inhibits tubulin polymerization. Tubulin inhibitor 1 shows potent anti-tumor activity, casues cellular mitotic arrest in the G2/M phase, and induces cellular apoptosis.
|
-
- HY-124798
-
-
- HY-32018
-
|
Cot inhibitor-2
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM.
|
-
- HY-118810
-
-
- HY-B0884
-
-
- HY-112569
-
-
- HY-B0884A
-
-
- HY-15167
-
-
- HY-112906
-
-
- HY-50856A
-
-
- HY-104022
-
-
- HY-117262
-
-
- HY-U00410
-
-
- HY-13276
-
-
- HY-B0218
-
-
- HY-106067A
-
-
- HY-N6717
-
|
Tentoxin
|
Others
|
Infection
|
|
Tentoxin is a cyclic tetrapeptide isolated from Alternaria tenuis, acts as a herbicide, causes seedling chlorosis, inhibits cyclic photophosphorylation and functions as an energy transfer inhibitor.
|
-
- HY-17542
-
|
PLpro inhibitor
|
SARS-CoV
|
Infection
|
|
PLpro inhibitor is a potent inhibitor of papain-like protease (PLpro) with an IC50 of 2.6 µM. PLpro inhibitor inhibits SARS-CoV-2 PLpro with an IC50 of 5.0 µM and an EC50 of 21.0 µM.
|
-
- HY-126328
-
|
PKC-theta inhibitor 1
|
PKC
|
Inflammation/Immunology
|
|
PKC-theta inhibitor 1 is the PKCθ inhibitor with an Ki value of 6 nM, inhibits IL-2 production in vivo with an IC50 of 0.19 μM. PKC-theta inhibitor 1 demonstrates a reduction of symptoms in a mouse model of multiple sclerosis.
|
-
- HY-15760
-
-
- HY-N1504
-
|
Loureirin B
|
PAI-1
Potassium Channel
ERK
JNK
|
Metabolic Disease
|
|
Loureirin B, a flavonoid extracted from Dracaena cochinchinensis, is an inhibitor of plasminogen activator inhibitor-1 (PAI-1), with an IC50 of 26.10 μM; Loureirin B also inhibits KATP, the phosphorylation of ERK and JNK, and has anti-diabetic activity.
|
-
- HY-13662B
-
|
(R)-Lansoprazole
Dexlansoprazole
|
Proton Pump
|
Inflammation/Immunology
|
|
(R)-Lansoprazole is the R enantiomer of Lansoprazole, Lansoprazole (AG 1749) is an orally active proton pump inhibitor which prevents the stomach from producing acid. Lansoprazole (AG 1749) is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-131705
-
-
- HY-10217
-
-
- HY-P1029
-
-
- HY-15604
-
-
- HY-N0565
-
-
- HY-15183
-
-
- HY-U00387
-
-
- HY-107986
-
-
- HY-10249A
-
-
- HY-100962
-
|
(E)-AG 99
(E)-Tyrphostin 46; (E)-Tyrphostin AG 99
|
EGFR
|
Cancer
|
|
(E)-AG 99 ((E)-Tyrphostin 46) is a potent EGFR inhibitor.
|
-
- HY-N0565A
-
-
- HY-108322
-
-
- HY-112270
-
-
- HY-50880
-
-
- HY-N2221
-
-
- HY-14657
-
-
- HY-101932
-
-
- HY-N6902
-
-
- HY-U00319
-
-
- HY-15825
-
|
IWP L6
Porcn Inhibitor III
|
Porcupine
|
Cancer
|
|
IWP L6 (Porcn Inhibitor III) is a Porcn inhibitor with an EC50 of 0.5 nM.
|
-
- HY-15604A
-
-
- HY-112269
-
-
- HY-128723
-
-
- HY-50879
-
-
- HY-104032
-
-
- HY-10172
-
|
IMD-0354
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity. IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM.
|
-
- HY-136270
-
|
ATR inhibitor 2
|
ATM/ATR
|
Cancer
|
|
ATR inhibitor 2 is an ATP-competitive, orally active, and selective ATR inhibitor, with a Ki of <150 pM. ATR inhibitor 2 potently inhibits ATR-driven phosphorylated checkpoint kinase-1 (Chk1) phosphorylation with an IC50 of 8 nM. Antitumor activity.
|
-
- HY-103310
-
-
- HY-122856
-
|
AZ12601011
|
TGF-β Receptor
|
Cancer
|
|
AZ12601011 is an orally active, selective TGFBR1 kinase inhibitor with an IC50 of 18 nM and a Kd of 2.9 nM. AZ12601011 inhibits phosphorylation of SMAD2 via selectively inhibiting ALK4, TGFBR1, and ALK7. AZ12601011 inhibits mammary tumor growth .
|
-
- HY-50900
-
-
- HY-B0083
-
|
Leflunomide
HWA486; RS-34821; SU101
|
Others
|
Cancer
|
|
Leflunomide is a pyrimidine synthesis inhibitor, inhibiting dihydroorotate dehydrogenase, and acts as a disease-modifying antirheumatic drug.
|
-
- HY-101474A
-
|
Zanubrutinib
BGB-3111
|
Btk
|
Cancer
|
|
Zanubrutinib (BGB-3111) is a selective Bruton tyrosine kinase (Btk) inhibitor.
|
-
- HY-16569
-
-
- HY-N7592
-
|
Arjunetin
|
Others
|
Others
|
|
Arjunetin, isolated from Terminalia arjuna, is an insect feeding-deterrent and growth inhibitor.
|
-
- HY-W008923
-
-
- HY-12238
-
|
IWR-1
endo-IWR 1; IWR-1-endo
|
Wnt
|
Cancer
|
|
IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway.
|
-
- HY-100110
-
|
KNK437
Heat Shock Protein Inhibitor I
|
HSP
|
Cancer
|
|
KNK437 is a HSP inhibitor, and inhibits the induction of HSP105, HSP70, and HSP40.
|
-
- HY-135384
-
-
- HY-106638
-
-
- HY-101791
-
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
|
|
Gentamicin sulfate, an aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. It inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-N0518
-
|
Toddalolactone
|
PAI-1
|
Cardiovascular Disease
|
|
Toddalolactone, a main component of Toddalia asiatica, inhibits the activity of recombinant human plasminogen activator inhibitor-1 (PAI-1), with an IC50 value of 37.31 μM.
|
-
- HY-16657
-
-
- HY-19931
-
|
COH29
RNR Inhibitor COH29
|
DNA/RNA Synthesis
|
Cancer
|
|
COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
|
-
- HY-119808
-
-
- HY-128729
-
|
DNA2 inhibitor C5
|
Others
|
Cancer
|
|
DNA2 inhibitor C5 is a potent, competitive and specific inhibitor of DNA2 nuclease activity with an IC50 of 20 μM. DNA2 inhibitor C5 inhibits nuclease, DNA dependent ATPase, helicase, and DNA binding activities of DNA2. DNA2 inhibitor C5 is a promising lead compound to develop sensitizers for cancer chemotherapeutics that cause replication stress.
|
-
- HY-P2478
-
-
- HY-13624A
-
|
Epirubicin hydrochloride
4'-Epidoxorubicin hydrochloride
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin hydrochloride (4'-Epidoxorubicin hydrochloride), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin hydrochloride inhibits DNA and RNA synthesis. Epirubicin hydrochloride is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-P2477
-
-
- HY-15358
-
|
ALK inhibitor 2
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 2 (compound 18) is a potent pyrimidin ALK inhibitor. ALK inhibitor 2 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=37 nM) and focal adhesion kinase (FAK; IC50=5 nM).
|
-
- HY-10917
-
|
GW2580
|
c-Fms
|
Inflammation/Immunology
Cancer
|
|
GW2580 is an orally bioavailable and selective inhibitor of c-Fms kinase which completely inhibits human cFMS kinase in vitro at 0.06 μM. GW2580 acts as a competitive inhibitor of ATP binding to the cFMS kinase and inhibits colony-stimulating-factor-1 signaling.
|
-
- HY-15357
-
|
ALK inhibitor 1
|
ALK
FAK
|
Cancer
|
|
ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM).
|
-
- HY-13624
-
|
Epirubicin
4'-Epidoxorubicin
|
DNA/RNA Synthesis
Topoisomerase
Apoptosis
|
Cancer
|
|
Epirubicin (4'-Epidoxorubicin), a semisynthetic L-arabino derivative of doxorubicin, has an antineoplastic agent by inhibiting Topoisomerase. Epirubicin inhibits DNA and RNA synthesis. Epirubicin is a Forkhead box protein p3 (Foxp3) inhibitor and inhibits regulatory T cell activity.
|
-
- HY-13417A
-
|
AICAR phosphate
Acadesine phosphate; AICA Riboside phosphate
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR phosphate (Acadesine phosphate) is an adenosine analog and a AMPK activator. AICAR phosphate regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR phosphate is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-113951
-
-
- HY-124718
-
|
p32 Inhibitor M36
M36
|
PKC
|
Cancer
|
|
p32 inhibitor M36 (M36) is a p32 mitochondrial protein inhibitor, which binds directly to p32 and inhibits p32 association with LyP-1.
|
-
- HY-13417
-
|
AICAR
Acadesine; AICA Riboside
|
AMPK
Autophagy
YAP
Mitophagy
|
Cancer
|
|
AICAR (Acadesine) is an adenosine analog and a AMPK activator. AICAR regulates the glucose and lipid metabolism, and inhibits proinflammatory cytokines and iNOS production. AICAR is also an autophagy, YAP and mitophagy inhibitor.
|
-
- HY-B0113A
-
|
Omeprazole sodium
H 16868 sodium
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole sodium (H 16868 sodium), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole sodium shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole sodium also inhibits growth of Gram-positive and Gram-negative bacteria. Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-12072
-
|
Lck Inhibitor
|
Src
|
Inflammation/Immunology
|
|
Lck Inhibitor is a potent, orally active Lck (lymphocyte specific kinase) inhibitor with IC50s of 7, 2.1, 4.2 and 200 nM for Lck, Lyn, Src and Syk kinases, respectively. Lck Inhibitor shows >1000-fold selectivity for Lck over MAPK, CDK and RSK family representatives. Lck Inhibitor inhibits T cell proliferation and in vivo models of arthritis.
|
-
- HY-P1398
-
-
- HY-P1260
-
-
- HY-19797A
-
-
- HY-131101
-
|
Nor-Acetildenafil
|
Others
|
Others
|
|
Nor-Acetildenafil is an Acetildenafil derivative. Acetildenafil is a synthetic agent which acts as a phosphodiesterase inhibitor.
|
-
- HY-10846
-
-
- HY-18930
-
|
NU6300
|
CDK
|
Cancer
|
|
NU6300 is the first covalent, irreversible and ATP-competitive CDK2 inhibitor.
|
-
- HY-W013478
-
-
- HY-10451S
-
-
- HY-15700
-
-
- HY-101429
-
|
RG13022
Tyrphostin RG13022
|
EGFR
|
Cancer
|
|
RG13022 is a tyrosine kinase inhibitor; inhibits the autophosphorylation reaction of the EGF receptor with an IC50 of 4 μM.
|
-
- HY-B1877
-
|
Nitrofen
|
Others
|
Cancer
|
|
Nitrofen is a selective contact herbicide. Nitrofen is a retinal dehydrogenase and protoporphyrinogen oxidase inhibitor.
|
-
- HY-N2219
-
-
- HY-19795
-
|
ML240
|
p97
|
Cancer
|
|
ML240 is a potent p97 inhibitor, inhibiting p97 ATPase with IC50 value of 100 nM.
|
-
- HY-112639
-
-
- HY-112913
-
-
- HY-100600
-
|
BGG463
K03859
|
CDK
|
Others
|
|
BGG463 (K03859) is an orally active type II CDK2 inhibitor.
|
-
- HY-N2117
-
|
Isoginkgetin
|
MMP
|
Cancer
|
|
Isoginkgetin is a MMP-9 inhibitor, also a Pre-mRNA Splicing Inhibitor with IC 50 of 30 uM.
|
-
- HY-136461
-
-
- HY-P2564
-
-
- HY-15222
-
-
- HY-14196
-
-
- HY-17396
-
-
- HY-14440
-
|
MP7
PDK1 inhibitor
|
PDK-1
|
Cancer
|
|
MP7 (PDK1 inhibitor) is a phosphoinositide-dependent kinase-1 (PDK1) inhibitor.
|
-
- HY-50670
-
-
- HY-U00145
-
-
- HY-10255A
-
|
Sunitinib
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-114309
-
-
- HY-111429
-
|
YAP/TAZ inhibitor-1
|
YAP
|
Cancer
|
|
YAP/TAZ inhibitor-1 is a YAP/TAZ inhibitor extracted from patent WO2017058716A1, Compound 1, has an IC50 of <0.100 μΜ in firefly luciferase assay.
|
-
- HY-120859A
-
|
Zidebactam sodium salt
WCK-5107 sodium salt
|
Bacterial
|
Infection
|
|
Zidebactam sodium salt (WCK-5107 sodium salt) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-120859
-
|
Zidebactam
WCK-5107
|
Bacterial
|
Infection
|
|
Zidebactam (WCK-5107) is a potent β-lactamase inhibitor. Zidebactam also is a penicillin-binding protein2 (PBP2) inhibitor with an IC50 of 0.26 μg/mL.
|
-
- HY-118355
-
|
ALLM
Calpain inhibitor II
|
Proteasome
Cathepsin
|
Neurological Disease
|
|
ALLM (Calpain inhibitor II) is a potent inhibitor of calpain and cathepsin proteases. ALLM inhibits neuronal cell death and improves chronic neurological function after spinal cord injury (SCI).
|
-
- HY-126331
-
-
- HY-101019
-
|
Ossirene
AS101
|
Interleukin Related
Caspase
|
Cancer
Inflammation/Immunology
|
|
Ossirene (AS101), an immunomodulatory tellurium compound, is a potent IL-1β inhibitor. Ossirene abolishes phosphorylation of STAT3 by inhibiting IL-10. Ossirene potently inhibits Caspase-1 and is used for the autoimmune diseases and certain malignancies.
|
-
- HY-100932
-
|
ML-9
|
Myosin
|
Cancer
|
|
ML-9 is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-B0113
-
|
Omeprazole
H 16868
|
Proton Pump
Autophagy
Bacterial
Phospholipase
|
Cancer
Infection
Metabolic Disease
|
|
Omeprazole (H 16868), a proton pump inhibitor (PPI), is available for treatment of acid-related gastrointestinal disorders. Omeprazole shows competitive inhibition of CYP2C19 activity with a Ki of 2 to 6 μM. Omeprazole also inhibits growth of Gram-positive and Gram-negative bacteria.Omeprazole is a potent brain penetrant neutral sphingomyelinase (N-SMase) inhibitor (exosome inhibitor).
|
-
- HY-N0565B
-
|
Doxycycline (hyclate)
Doxycycline hydrochloride hemiethanolate hemihydrate; WC2031
|
Antibiotic
MMP
Bacterial
|
Infection
|
|
Doxycycline (hyclate) (Doxycycline hydrochloride hemiethanolate hemihydrate), an antibiotic, is an orally active and broad-spectrum metalloproteinase (MMP) inhibitor.
|
-
- HY-15699A
-
-
- HY-B2063
-
|
Chlorobenzuron
|
Others
|
Infection
|
|
Chlorobenzuron is a chitin synthetase inhibitor, acts as an insecticide. Chlorobenzuron can inhibit larvae development and pupate.
|
-
- HY-N1447
-
-
- HY-15167A
-
-
- HY-112634
-
-
- HY-133248
-
-
- HY-13972
-
-
- HY-15699
-
-
- HY-118165
-
-
- HY-B1596
-
-
- HY-P1260A
-
-
- HY-103593A
-
-
- HY-15842
-
-
- HY-103593
-
|
LCL521
|
Phospholipase
|
Cancer
|
|
LCL521 is an acid ceramidase (ACDase) inhibitor. LCL521 also inhibits the lysosomal acid sphingomyelinase (ASMase).
|
-
- HY-I0637
-
-
- HY-16187
-
-
- HY-133247
-
-
- HY-D0886
-
-
- HY-18965
-
-
- HY-12277
-
|
AZ191
|
DYRK
|
Cancer
|
|
AZ191 is a potent inhibitor that selectively inhibits DYRK1B with IC50 of 17 nM.
|
-
- HY-107451
-
-
- HY-107485
-
-
- HY-14174
-
-
- HY-N7511
-
-
- HY-N4294
-
-
- HY-B2007
-
-
- HY-100498
-
|
GSK2256098
|
FAK
Apoptosis
|
Cancer
|
|
GSK2256098 is a selective FAK kinase inhibitor, which inhibits growth and survival of pancreatic ductal adenocarcinoma cells.
|
-
- HY-14445
-
-
- HY-19707
-
-
- HY-112822
-
|
ON-013100
|
CDK
|
Cancer
|
|
ON-013100, an antineoplastic drug, acts a mitotic inhibitor that could inhibit Cyclin D1 expression.
|
-
- HY-100456
-
-
- HY-111493
-
-
- HY-50706A
-
|
Selumetinib sulfate
AZD6244 sulfate; ARRY-142886 sulfate
|
MEK
Apoptosis
|
Cancer
|
|
Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.
|
-
- HY-105917
-
|
Endovion
NS3728
|
Chloride Channel
|
Others
|
|
Endovion (NS3728) is a pharmacological anion channel inhibitor (like chloride channel) and the specific VRAC/VSOAC blocker. Endovion (NS3728) is also an Anoctamin-1 (ANO 1) channel inhibitor.
|
-
- HY-10326
-
|
GW788388
|
TGF-β Receptor
|
Cancer
|
|
GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
|
-
- HY-125997
-
|
BTK inhibitor 10
|
Btk
|
Inflammation/Immunology
|
|
BTK inhibitor 10 is a potent and orally active Bruton kinase (BTK) inhibitor, extracted from patent WO2018145525, example 33. BTK inhibitor 10 has a potential for rheumatoid arthritis treatment.
|
-
- HY-13228
-
-
- HY-126288
-
|
ERK1/2 inhibitor 2
|
ERK
|
Cancer
|
|
ERK1/2 inhibitor 2 (Example 1) is a potent dual ERK1/2 inhibitor. ERK1/2 inhibitor 2 has anti-cancer activity.
|
-
- HY-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-119935
-
-
- HY-10227
-
|
Bortezomib
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity.
|
-
- HY-10255
-
|
Sunitinib Malate
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-17367
-
|
Atazanavir
BMS-232632
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Infection
Cancer
|
|
Atazanavir (BMS-232632) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir (BMS-232632) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-N8533
-
|
Sodium Camptothecin
|
DNA/RNA Synthesis
|
Cancer
Infection
|
|
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and, intracellularly, causes breaks in preformed viral DNA.
|
-
- HY-13985
-
-
- HY-12031A
-
-
- HY-U00453
-
-
- HY-112910
-
|
Grp94 Inhibitor-1
|
HSP
|
Cancer
Infection
|
|
Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α.
|
-
- HY-15339
-
|
CVT-313
Cdk2 Inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation.
|
-
- HY-13984
-
|
Mutant EGFR inhibitor
|
EGFR
|
Cancer
|
|
Mutant EGFR inhibitor is a potent and selective mutant EGFR inhibitor extracted from patent WO 2013014448 A1; inhibits EGFR L858R, EGFR Exon 19 deletion and EGFR T790M.
|
-
- HY-22166
-
-
- HY-W047428
-
-
- HY-112451
-
-
- HY-U00377
-
-
- HY-15217
-
-
- HY-15859
-
|
Atglistatin
|
ATGL
|
Metabolic Disease
|
|
Atglistatin is a selective adipose triglyceride lipase (ATGL) inhibitor which inhibits lipolysis with an IC50 of 0.7 μM in vitro.
|
-
- HY-77521
-
-
- HY-13502
-
-
- HY-119938
-
-
- HY-107994
-
-
- HY-70027A
-
-
- HY-N2567
-
|
(±)-Decursinol
|
Bacterial
|
Cancer
|
|
(±)-Decursinol is a potent FtsZ inhibitor. (±)-Decursinol inhibits B. anthracis FtsZ polymerization with an IC50 of 102 μM.
|
-
- HY-128962
-
-
- HY-13278
-
-
- HY-112860
-
-
- HY-A0116S
-
-
- HY-13060
-
-
- HY-101474
-
|
(±)-Zanubrutinib
(±)-BGB-3111
|
Btk
|
Cancer
|
|
(±)-Zanubrutinib ((±)-BGB-3111) is a potent, selective and orally available Bruton's tyrosine kinase (Btk) inhibitor.
|
-
- HY-124594
-
-
- HY-19731
-
-
- HY-101462
-
-
- HY-B0902A
-
|
Rufloxacin hydrochloride
MF-934 hydrochloride
|
Bacterial
|
Infection
|
|
Rufloxacin hydrochloride (MF-934 hydrochloride) is a fluoroquinolone antibacterial, inhibits B-cell differentiation in human mononuclear cells, inhibits Topo.
|
-
- HY-101963
-
-
- HY-115213
-
-
- HY-70073
-
-
- HY-15775
-
-
- HY-13502A
-
-
- HY-W010538
-
-
- HY-70003
-
-
- HY-112720
-
-
- HY-116767
-
|
BLT-1
Block lipid transport-1
|
HCV
|
Metabolic Disease
Inflammation/Immunology
|
|
BLT-1, a thiosemicarbazone copper chelator, is a selective scavenger receptor B, type 1 (SR-BI) inhibitor. BLT-1 inhibits the transfer of lipids between high-density lipoproteins (HDL) and cells mediated by SR-BI. BLT-1 is a potent HCV entry inhibitor.
|
-
- HY-10439
-
|
HPGDS inhibitor 1
|
PGE synthase
|
Inflammation/Immunology
|
|
HPGDS inhibitor 1 is a potent, selective and orally active Hematopoietic Prostaglandin D Synthase (HPGDS) inhibitor with an IC50s of 0.6 nM and 32 nM in enzyme and cellular assays, respectively. HPGDS inhibitor 1 does not inhibit human L-PGDS, mPGES, COX-1, COX-2, or 5-LOX.
|
-
- HY-P1111
-
|
Lyn peptide inhibitor
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-100932A
-
|
ML-9 Free Base
|
Myosin
|
Cancer
|
|
ML-9 (Free Base) is a selective and potent inhibitor of Akt kinase, inhibits myosin light-chain kinase (MLCK) and stromal interaction molecule 1 (STIM1) activity. ML-9 (Free Base) inhibits inhibits MLCK, PKA and PKC activity with Ki values of 4, 32 and 54 μM, respectively. ML-9 (Free Base) induces autophagy by stimulating autophagosome formation and inhibiting their degradation.
|
-
- HY-135318
-
|
NBDHEX
|
Glutathione Peroxidase
Apoptosis
Autophagy
|
Cancer
|
|
NBDHEX is a potent glutathione S-transferase P1-1 (GSTP1-1) inhibitor. NBDHEX induces apoptosis of tumor cells. NBDHEX acts as an anticancer agent by inhibiting GSTs catalytic activity, avoiding inconvenience of the inhibitor extrusion from the cell by specific pumps and disrupting the interaction between the GSTP1-1 and key signaling effectors. NBDHEX can also act as late-phase autophagy inhibitor.
|
-
- HY-121172
-
|
1,4-DPCA
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM.
|
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
|
Cancer
|
|
Shikonin is a major component of a Chinese herbal medicine named zicao. Shikonin is a potent TMEM16A chloride channel inhibitor with an IC50 of 6.5 μM. Shikonin is a specific pyruvate kinase M2 (PKM2) inhibitor and can also inhibit TNF-α and NF-κB pathway. Shikonin decreases exosome secretion through the inhibition of glycolysis. Shikonin inhibits AIM2 inflammasome activation.
|
-
- HY-100816
-
|
Rbin-1
Ribozinoindole-1
|
Phosphatase
|
Metabolic Disease
|
|
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
|
-
- HY-120675
-
|
SSTC3
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors.
|
-
- HY-100556
-
|
Tie2 kinase inhibitor 1
|
Others
|
Cancer
|
|
Tie2 kinase inhibitor 1 (compound 5) is a potent, selective Tie2 kinase inhibitor with an IC50 of 250 nM. Tie2 kinase inhibitor 1 has anti-cancer activity.
|
-
- HY-112715
-
-
- HY-14165
-
-
- HY-124793A
-
|
GAK inhibitor 49 hydrochloride
|
Others
|
Infection
|
|
GAK inhibitor 49 hydrochloride is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 hydrochloride also shows binding to RIPK2.
|
-
- HY-19727A
-
-
- HY-129167
-
-
- HY-128918
-
|
SIS17
|
HDAC
|
Others
|
|
SIS17 is a mammalian histone deacetylase 11 (HDAC 11) inhibitor with an IC50 value of 0.83 μM, inhibits the demyristoylation HDAC11 substrate, serine hydroxymethyl transferase 2, without inhibiting other HDACs.
|
-
- HY-124793
-
|
GAK inhibitor 49
|
Others
|
Infection
|
|
GAK inhibitor 49 is a potent, ATP-competitive and highly selective cyclin G associated kinase (GAK) inhibitor with a Ki of 0.54 nM and a cell IC50 of 56 nM. GAK inhibitor 49 also shows binding to RIPK2.
|
-
- HY-B0879A
-
|
Suramin sodium salt
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor. Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-B0879
-
|
Suramin
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Cancer
Infection
Cardiovascular Disease
|
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor. Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM). Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM). Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor.Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent.
|
-
- HY-P0081
-
-
- HY-133110
-
|
Afatinib N-Oxide
|
Others
|
Others
|
|
Afatinib N-Oxide is a impurity of Afatinib dimaleate in oxidative degradation. Afatinib dimaleate is an irreversible EGFR family inhibitor.
|
-
- HY-15798
-
-
- HY-114418
-
-
- HY-N5038
-
|
Mauritianin
|
Topoisomerase
|
Cancer
|
|
Mauritianin is a kaempferol glycoside isolated from the flowers and leaves of Acalypha indica. Mauritianin is a topoisomerase I inhibitor.
|
-
- HY-13606
-
|
Dacinostat
NVP-LAQ824; LAQ824
|
HDAC
Autophagy
|
Cancer
|
|
Dacinostat is a potent HDAC inhibitor, with an IC50 of 32 nM; Dacinostat also inhibits HDAC1 with an IC50 of 9 nM, and used in cancer research.
|
-
- HY-13256
-
-
- HY-P1452A
-
-
- HY-Y0882
-
-
- HY-16420
-
|
R112
|
Syk
|
Inflammation/Immunology
|
|
R112 is an ATP-competitive inhibitor of Syk kinase with a Ki of 96 nM. R112 inhibits Syk kinase activity with an IC50 of 226 nM.
|
-
- HY-111919
-
-
- HY-15588
-
-
- HY-B0830
-
|
Isoprocarb
|
AChE
|
Neurological Disease
|
|
Isoprocarb is carbamate insecticide that widely used to control rice paddy lice and leafhopper. Isoprocarb is also an AChE inhibitor.
|
-
- HY-12054A
-
-
- HY-114423
-
-
- HY-16931
-
|
SMIFH2
|
Others
|
Cancer
|
|
SMIFH2 is a formin specific inhibitor. SMIFH2 inhibits actin polymerization by Formins and affects the actin cytoskeleton.
|
-
- HY-10809
-
|
Bitopertin
RG1678; RO4917838
|
GlyT
|
Neurological Disease
|
|
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
|
-
- HY-19609
-
-
- HY-131268
-
-
- HY-N6619A
-
|
Lycoramine
|
AChE
|
Neurological Disease
|
|
Lycoramine, a dihydro-derivative of galanthamine, is isolated from Lycoris radiate. Lycoramine is a potent acetylcholinesterase (AChE) inhibitor.
|
-
- HY-104028
-
-
- HY-12814A
-
-
- HY-12814
-
|
TH588
|
DNA/RNA Synthesis
|
Cancer
|
|
TH588 is first-in-class nudix hydrolase family inhibitor that potently and selectively engage and inhibit the MTH1 (IC50= 5 nM).
|
-
- HY-111506
-
-
- HY-12420
-
|
JNJ-47117096 hydrochloride
MELK-T1 hydrochloride
|
MELK
FLT3
|
Cancer
|
|
JNJ-47117096 hydrochloride is potent and selective MELK inhibitor, with an IC50 of 23 nM, also effectively inhibits Flt3, with an IC50 of 18 nM.
|
-
- HY-16982
-
|
Cercosporamide
(-)-Cercosporamide
|
Fungal
MNK
|
Cancer
Infection
|
|
Cercosporamide is a highly potent, ATP-competitive Pkc1 kinase inhibitor, with an IC50 of <50 nM and a Ki of <7 nM. Cercosporamide is a unique Mnk inhibitor.
|
-
- HY-136347
-
-
- HY-13280
-
-
- HY-18928
-
|
FAK inhibitor 5
|
FAK
|
Cancer
|
|
FAK inhibitor 5 (compound 2) is a novel allosteric FAK inhibitor, with IC50 values in the low micromolar range.
|
-
- HY-N4186
-
-
- HY-103002
-
|
SU5408
VEGFR2 Kinase Inhibitor I
|
VEGFR
|
Cardiovascular Disease
|
|
SU5408 (VEGFR2 Kinase Inhibitor I) is a potent and cell-permeable inhibitor of VEGFR2 kinase with an IC50 of 70 nM.
|
-
- HY-B0497B
-
-
- HY-131446
-
|
Chk1-IN-5
|
Checkpoint Kinase (Chk)
|
Cancer
|
|
Chk1-IN-5 is a potent checkpoint kinase 1 (Chk1) inhibitor. Chk1-IN-5 inhibits Chk1 phosphorylation and inhibits tumor growth in colon cancer xenograft model.
|
-
- HY-50202
-
|
Etomoxir
(R)-(+)-Etomoxir
|
Apoptosis
|
Cancer
Metabolic Disease
|
|
Etomoxir ((R)-(+)-Etomoxir) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-50202A
-
|
Etomoxir sodium salt
(R)-(+)-Etomoxir sodium salt
|
Apoptosis
|
Metabolic Disease
Cancer
|
|
Etomoxir sodium salt ((R)-(+)-Etomoxir sodium salt) is an irreversible inhibitor of carnitine palmitoyltransferase 1a (CPT-1a), inhibits fatty acid oxidation (FAO) through CPT-1a and inhibits palmitate β-oxidation in human, rat and guinea pig.
|
-
- HY-117491
-
-
- HY-124416
-
|
ML604086
|
CCR
|
Inflammation/Immunology
Endocrinology
|
|
ML604086 is a selective CCR8 inhibitor, inhibiting CCL1 binding to CCR8 on circulating T-cells. ML604086 inhibits CCL1 mediated chemotaxis and increases in intracellular Ca 2+ concentrations.
|
-
- HY-103490
-
|
Takinib
|
MAP3K
Apoptosis
|
Cancer
|
|
Takinib is a potent and selective TAK1 inhibitor with an IC50 of 9.5 nM, which inhibits autophosphorylated and non-phosphorylated TAK1 that binds within the ATP-binding pocket and inhibits by slowing down the rate-limiting step of TAK1 activation.
|
-
- HY-17367A
-
|
Atazanavir sulfate
BMS-232632 sulfate
|
HIV
HIV Protease
Cytochrome P450
P-glycoprotein
|
Cancer
Infection
|
|
Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
|
-
- HY-122866
-
|
ZT-12-037-01
|
Ras
|
Cancer
|
|
ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM.
|
-
- HY-109574
-
|
Raf inhibitor 2
|
Raf
|
Cancer
|
|
Raf inhibitor 2 is a potent raf kinase (IC50<1.0 μM) inhibitor, compound 32, extracted from patent EP1003721B1. Raf inhibitor 2 can be used for cancer research.
|
-
- HY-100227
-
|
E 64c
|
Cathepsin
SARS-CoV
|
Metabolic Disease
|
|
E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.
|
-
- HY-66004
-
|
4-Acetamidophenyl acetate
|
Others
|
Inflammation/Immunology
|
|
4-Acetamidophenyl acetate is an impurity of Acetaminophen (paracetamol). Acetaminophen, an analgesic drug, is a selective COX-2 inhibitor (IC50=25.8 μM), and is a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor.
|
-
- HY-115502
-
|
BCI
(E)-BCI
|
Phosphatase
|
Cancer
Inflammation/Immunology
|
|
BCI is an allosteric inhibitor of dual specificity phosphatase (DUSP). BCI specifically inhibits DUSP6 and DUSP1 with EC50s of 13.3 and 8.0 μM in cells, respectively. BCI does not inhibit DUSP5.
|
-
- HY-80003
-
|
QL47
|
Btk
|
Cancer
Infection
|
|
QL47, a broad-spectrum antiviral agent, inhibits dengue virus and other RNA viruses. QL47 selectively inhibits eukaryotic translation. QL47 is a potent covalent inhibitor of BTK with an IC50 of 7 nM.
|
-
- HY-133019
-
-
- HY-P1045
-
|
187-1, N-WASP inhibitor
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-124653
-
|
HSP27 inhibitor J2
J2
|
HSP
|
Cancer
|
|
HSP27 inhibitor J2 (J2) is a HSP27 inhibitor, which significantly induces abnormal HSP27 dimer formation and inhibits a production of HSP27 giant polymers, thereby having an effect of inhibiting a chaperone function of the HSP27 and reducing a cell protection function thereof. HSP27 inhibitor J2 (J2) remarkably enhances the antiproliferative activity of 17-AAG and sensitizes cisplatin-induced lung cancer cell growth inhibition.
|
-
- HY-P1045A
-
|
187-1, N-WASP inhibitor TFA
|
Arp2/3 Complex
|
Others
|
|
187-1, N-WASP inhibitor TFA, a 14-aa cyclic peptide, is an allosteric neural Wiskott-Aldrich syndrome protein (N-WASP) inhibitor. 187-1, N-WASP inhibitor TFA potently inhibits actin assembly induced by phosphatidylinositol 4,5-bisphosphate (PIP2) with an IC50 of 2 μM. 187-1, N-WASP inhibitor TFA prevents the activation of Arp2/3 complex by N-WASP by stabilizing the autoinhibited state of the protein.
|
-
- HY-P1111A
-
|
Lyn peptide inhibitor TFA
|
Src
Interleukin Related
|
Inflammation/Immunology
|
|
Lyn peptide inhibitor TFA is a potent and cell-permeable inhibitor of Lyn-coupled IL-5 receptor signaling pathway, while keeping other signals intact. Lyn peptide inhibitor TFA blocks Lyn activation and inhibits the binding of Lyn tyrosine kinase to βc subunit of IL-3/GM-CSF/IL-5 receptors. Lyn peptide inhibitor TFA can be used for study of asthma, allergic, and other eosinophilic disorders.
|
-
- HY-15766A
-
|
GNE-617 hydrochloride
|
NAMPT
|
Cancer
|
|
GNE-617 hydrochloride is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-12399
-
|
MKC9989
|
IRE1
|
Cancer
|
|
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
|
-
- HY-112280
-
-
- HY-10247
-
|
BRAF inhibitor
|
Raf
|
Cancer
|
|
BRAF inhibitor is a B-Raf inhibitor extracted from patent WO/2011103196 A1, Compound P-0850.
|
-
- HY-12726A
-
-
- HY-109565
-
|
ASTX660
|
IAP
|
Cancer
|
|
ASTX660 is an orally bioavailable dual antagonist of cellular inhibitor of apoptosis protein (cIAP) and X-linked inhibitor of apoptosis protein (XIAP).
|
-
- HY-108820
-
-
- HY-108817
-
-
- HY-10978
-
-
- HY-13452
-
-
- HY-119459
-
|
Fluopyram
|
Fungal
|
Infection
|
|
Fluopyram is a succinate dehydrogenase inhibitor fungicide, inhibits the growth of F. virguliforme isolates with mean EC50 of 3.35 µg/mL.
|
-
- HY-10162S
-
-
- HY-U00370
-
-
- HY-111489A
-
-
- HY-17421A
-
-
- HY-135383A
-
-
- HY-128977
-
-
- HY-12000
-
|
AG490
Tyrphostin AG490; Tyrphostin B42
|
EGFR
STAT
JAK
Autophagy
|
Cancer
|
|
AG490 (Tyrphostin AG490) is a tyrosine kinase inhibitor that inhibits EGFR, Stat-3 and JAK2/3.
|
-
- HY-A0122
-
-
- HY-111446
-
-
- HY-17381
-
-
- HY-N6031
-
|
Dendrophenol
|
NF-κB
|
Cancer
|
|
Dendrophenol, isolated from the stem of Dendrobium loddigesii Rolfe, act as a NF-κB inhibitor. Antineoplastic activity.
|
-
- HY-Y0172
-
-
- HY-13026S
-
|
Idelalisib D5
CAL-101 D5; GS-1101 D5
|
PI3K
Autophagy
|
Cancer
|
|
Idelalisib D5 is a deuterium labeled Idelalisib. Idelalisib is a highly selective and orally bioavailable p110δ inhibitor.
|
-
- HY-108941
-
|
Salicyl-AMS
|
Bacterial
|
Infection
|
|
Salicyl-AMS is a mycobactin biosynthesis inhibitor which can also inhibit M. tuberculosis growth in vitro under iron-limited conditions.
|
-
- HY-15282
-
-
- HY-B0806
-
|
Proguanil
|
Parasite
Antifolate
|
Infection
|
|
Proguanil, an antimalarial prodrug, is metabolized to the active metabolite Cycloguanil (HY-12784). Proguanil is a dihydrofolate reductase (DHFR) inhibitor.
|
-
- HY-N2597
-
-
- HY-B0806A
-
-
- HY-112297
-
-
- HY-13420
-
-
- HY-100736
-
|
ML348
GNF-Pf-1127
|
Phospholipase
|
Cancer
|
|
ML348 is a selective and reversible lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2.
|
-
- HY-15202
-
|
Binimetinib
MEK162; ARRY-162; ARRY-438162
|
MEK
Autophagy
|
Cancer
|
|
Binimetinib (MEK162) is an oral and selective MEK1/2 inhibitor. Binimetinib (MEK162) inhibits MEK with an IC50 of 12 nM.
|
-
- HY-102007
-
|
Gamitrinib TPP
|
HSP
|
Cancer
|
|
Gamitrinib TPP is a Gamitrinib (GA) mitochondrial matrix inhibitor. Gamitrinib TPP is a mitochondrial targeted HSP90 inhibitor with anti-cancer activity.
|
-
- HY-12726
-
-
- HY-N1724
-
-
- HY-15766
-
|
GNE-617
|
NAMPT
|
Metabolic Disease
Cancer
|
|
GNE-617 is a specific NAMPT inhibitor that inhibits the biochemical activity of NAMPT with an IC50 of 5 nM and exhibits efficacy in xenograft models of cancer.
|
-
- HY-111489B
-
-
- HY-126253
-
|
BI-4916
|
Others
|
Cancer
|
|
BI-4916 is a prodrug of BI-4924. BI-4924 is a NADH/NAD +-competitive PHGDH inhibitor.
|
-
- HY-136485
-
-
- HY-B1863
-
|
Iprobenfos
|
Fungal
|
Infection
|
|
Iprobenfos is an organophosphorus fungicide and is widely used to control the rice blast fungus. Iprobenfos is also a choline biosynthesis inhibitor.
|
-
- HY-B0882
-
|
Edrophonium chloride
|
AChE
|
Neurological Disease
|
|
Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-135899
-
|
SIRT7 inhibitor 97491
|
Sirtuin
Apoptosis
|
Cancer
|
|
SIRT7 inhibitor 97491, a potent SIRT7 inhibitor with an IC50 of 325 nM, reduces deacetylase activity of SIRT7 in a dose-dependent manner. SIRT7 inhibitor 97491 prevents tumor progression by increasing p53 stability through acetylation at K373/382. SIRT7 inhibitor 97491 promotes apoptosis through caspase pathway..
|
-
- HY-B2145
-
|
Ilaprazole sodium
IY-81149 sodium
|
Proton Pump
TOPK
|
Cancer
Inflammation/Immunology
|
|
Ilaprazole (IY-81149) sodium is an orally active proton pump inhibitor. Ilaprazole sodium irreversibly inhibits H +/K +-ATPase in a dose-dependent manner with an IC50 of 6 μM in rabbit parietal cell preparation. Ilaprazole sodium is used for the research of gastric ulcers. Ilaprazole sodium is also a potent TOPK (T-lymphokine-activated killer cell-originated protein kinase) inhibitor.
|
-
- HY-107412
-
|
Proteasome inhibitor IX
PS-IX; AM114
|
Proteasome
|
Cancer
|
|
Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM. Proteasome inhibitor IX exhibits HCT116 p53 +/+ cells growth inhibitory activity with an IC50 value of 1.49 μM. Proteasome inhibitor IX has potent anticancer activity.
|
-
- HY-130795
-
|
GSK-3β inhibitor 2
|
GSK-3
|
Neurological Disease
|
|
GSK-3β inhibitor 2 (Compound 3) is a potent, selective and orally active GSK-3β inhibitor with an IC50 of 1.1 nM. GSK-3β inhibitor 2 can cross the blood-brain barrier. GSK-3β inhibitor 2 has the potential for Alzheimer's disease.
|
-
- HY-10255AS
-
|
Sunitinib D10
SU 11248 D10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib D10 (SU 11248 D10) is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation.
|
-
- HY-124726
-
|
Aumitin
|
Autophagy
|
Cancer
Neurological Disease
|
|
Aumitin is a diaminopyrimidine-based autophagy inhibitor which inhibits mitochondrial respiration by targeting complex I. Aumitin inhibits starvation- and rapamycin induced autophagy dose dependently with IC50s of 0.12 μM and 0.24 μM, respectively.
|
-
- HY-19727
-
-
- HY-N7674A
-
|
Angoline hydrochloride
|
STAT
|
Cancer
|
|
Angoline hydrochloride is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline hydrochloride inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-P1290
-
|
PKA Inhibitor Fragment (6-22) amide
PKI-(6-22)-amide
|
PKA
|
Neurological Disease
|
|
PKA Inhibitor Fragment (6-22) amide is an inhibitor of cAMP-dependent protein kinase A (PKA), with a Ki of 2.8 nM. PKA Inhibitor Fragment (6-22) amide can significantly reverse low-level morphine antinociceptive tolerance in mice.
|
-
- HY-N7674
-
|
Angoline
|
STAT
|
Cancer
|
|
Angoline is a potent and selective IL6/STAT3 signaling pathway inhibitor with an IC50 of 11.56 μM. Angoline inhibits STAT3 phosphorylation and its target gene expression, and inhibits cancer cell proliferation.
|
-
- HY-109019
-
|
Vorolanib
CM082; X-82
|
VEGFR
PDGFR
|
Cancer
Cardiovascular Disease
|
|
Vorolanib (CM082) is an orally active, potent multikinase VEGFR/PDGFR inhibitor. Vorolanib is a potent ATP-binding cassette (ABC) transporter inhibitor. Vorolanib is an angiogenesis inhibitor and has antitumor activity combined with ZD1839 (HY-50895).
|
-
- HY-12054
-
|
Hesperadin
|
Aurora Kinase
Autophagy
Influenza Virus
Parasite
|
Cancer
|
|
Hesperadin is an ATP competitive indolinone inhibitor of Aurora A and B. Hesperadin inhibits Aurora B with an IC50 of 250 nM. Hesperadin inhibits the growth of Trypanosoma brucei by blocking nuclear division and cytokinesis. Hesperadin also is a broad-spectrum influenza antiviral.
|
-
- HY-100734
-
-
- HY-123772
-
|
CDK5 inhibitor 20-223
|
CDK
|
Cancer
|
|
CDK5 inhibitor 20-223 is a potent CDK2 and CDK5 inhibitor with IC50s of 6.0 and 8.8 nM, respectively. CDK5 inhibitor 20-223 is an effective anti-colorectal cancer (CRC) agent.
|
-
- HY-100899
-
-
- HY-101705
-
-
- HY-N6619
-
-
- HY-109877
-
-
- HY-100299
-
-
- HY-P2470
-
-
- HY-B0106
-
-
- HY-50710
-
|
KU-0063794
|
mTOR
|
Cancer
|
|
KU-0063794 is a potent and specific mTOR inhibitor, inhibiting both the mTORC1 and mTORC2 complexes with IC50s of 10 nM.
|
-
- HY-137239
-
-
- HY-100303A
-
|
FR194738
|
Others
|
Metabolic Disease
|
|
FR194738 is a squalene epoxidase inhibitor. FR194738 inhibits squalene epoxidase activity in HepG2 cell homogenates with an IC50 of 9.8 nM.
|
-
- HY-50946
-
-
- HY-15886
-
-
- HY-112131
-
-
- HY-19326
-
-
- HY-12971
-
|
Nampt-IN-1
LSN3154567
|
NAMPT
|
Cancer
|
|
Nampt-IN-1 (LSN3154567) is a potent and selective NAMPT inhibitor. Nampt-IN-1 inhibits purified NAMPT with an IC50 of 3.1 nM.
|
-
- HY-130255
-
-
- HY-101479
-
|
Iclaprim
AR-100
|
Bacterial
|
Infection
|
|
Iclaprim is a new selective bacterial Dihydrofolate inhibitor, which can inhibit the growth of S. aureus (MRSA) with an MIC90 of 0.06 μg/mL.
|
-
- HY-70027
-
-
- HY-108900A
-
-
- HY-N5118
-
|
Chimonanthine
(-)-Chimonanthine
|
Tyrosinase
|
Cancer
|
|
Chimonanthine is an alkaloid of Chimonanthus praecox, inhibits tyrosinase and tyrosine-related protein-1 mRNA expression, amd inhibits melanogenesis.
|
-
- HY-U00049
-
-
- HY-16904
-
|
RI-2
|
RAD51
|
Cancer
|
|
RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
|
-
- HY-130760
-
-
- HY-103036
-
-
- HY-111410
-
-
- HY-10862
-
|
FAAH inhibitor 1
Benzothiazole analog 3
|
FAAH
Autophagy
|
Cancer
|
|
FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM.
|
-
- HY-13256A
-
|
Desmethyl Erlotinib
OSI-420 free base; CP-373420
|
Drug Metabolite
|
Cancer
|
|
Desmethyl Erlotinib (OSI-420 free base) is an active metabolite of Erlotinib. Erlotinib is a potent EGFR tyrosin kinase inhibitor.
|
-
- HY-15231
-
-
- HY-15735
-
