Search Result
Results for "
<i>Valeriana officinalis<_i> Linn.
" in MCE Product Catalog:
1235
Inhibitors & Agonists
36
Biochemical Assay Reagents
53
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
-
- HY-N8136
-
|
Volvalerenic acid A
|
Others
|
Others
|
|
Volvalerenic acid A is a germacrane-type sesquiterpenoid that can be found in the roots of Valeriana officinalis var. latifolia.
|
-
- HY-N0331
-
|
Ziyuglycoside I
|
MDM-2/p53
Apoptosis
|
Cancer
|
|
Ziyuglycoside I isolated from S. officinalis root, has anti-wrinkle activity, and increases the expression of type I collagen. Ziyuglycoside I could be used as an active ingredient for cosmetics. Ziyuglycoside I triggers cell cycle arrest and apoptosis mediated by p53, it can be a potential agent candidate for treating triple-negative breast cancer (TNBC).
|
-
- HY-147986
-
|
hCA I-IN-2
|
Carbonic Anhydrase
|
Cancer
|
|
hCA I-IN-2 (Compound 6d) is a selective human carbonic anhydrase I (hCA I) inhibitor with Ki values of 18.8, 375.1, 1721 and 283.9 nM against hCA I, hCA II, hCAIX and hCAXII, respectively.
|
-
- HY-147985
-
|
hCA I-IN-1
|
Carbonic Anhydrase
|
Cancer
|
|
hCA I-IN-1 (Compound 6q) is a human carbonic anhydrase I (hCA I) inhibitor with Ki values of 38.3, 716.4, 940.1 and 192.8 nM against hCA I, hCA II, hCAIX and hCAXII, respectively.
|
-
- HY-146437
-
|
Topoisomerase I inhibitor 6
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 6 (Compound 3) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 6 is able to trap DNA-Top1 cleavage complex and found to be less cytotoxic in non-cancerous cell line. Topoisomerase I inhibitor 6 has the potential for the research of cancer diseases.
|
-
- HY-149002
-
|
Topoisomerase I/II inhibitor 4
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
|
-
- HY-N2795
-
|
9-Hydroxycalabaxanthone
Xanthone I
|
Parasite
Bacterial
|
Infection
|
|
9-Hydroxycalabaxanthone (Xanthone I) is a known xanthone isolated from Garcinia mangostana Linn. 9-Hydroxycalabaxanthone has quorum-sensing inhibitory, anti-microbial, and anti-malarial activities (IC50=1.2-1.5 µM).
|
-
- HY-146497
-
|
Topoisomerase I inhibitor 7
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 7 (Compound 8) is a potent inhibitor of Topoisomerase I. Topoisomerase I inhibitor 7 significantly inhibits tumor growth (up to 79%) and increases the lifespan (153%) of mice bearing P388 lymphoma transplants. Topoisomerase I inhibitor 7 indicates prospects for further search of new antitumor agent candidates among the heteroarene-fused anthraquinones.
|
-
- HY-150685
-
-
- HY-153340
-
|
I-152
|
Keap1-Nrf2
|
Metabolic Disease
|
|
I-152 is a conjugate containing N-acetyl-cysteine (NAC) and cysteamine (MEA). I-152 activates NRF2 and ATF4 signals. I-152 has anti-proliferative properties.
|
-
- HY-E70040
-
-
- HY-143265
-
|
Topoisomerase I inhibitor 2
|
Topoisomerase
Apoptosis
Caspase
|
Cancer
|
|
Topoisomerase I inhibitor 2 (ZML-8) is a highly selective inhibitor of DNA topoisomerase I (Top1). Topoisomerase I inhibitor 2 inhibits Top1 activity and results DNA damage. Topoisomerase I inhibitor 2 blocks G2/M phase and induces apoptosis, exhibits anti-tumor effect.
|
-
- HY-153365
-
|
I-138
|
Deubiquitinase
|
Cancer
|
|
I-138 is an orally active compound structurally related to ML323 (HY-17543). I-138 and ML-323 are potent reversible inhibitors of USP1-UAF1. I-138 displays synergistic binding with ubiquitin and mutual exclusive binding with ML323. I-138 induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells, increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells. I-138 ablates USP1 autocleavage in cells.
|
-
- HY-136538
-
|
LQZ-7I
|
Survivin
|
Cancer
|
|
LQZ-7I is a survivin-targeting inhibitor. LQZ-7I inhibits survivin dimerization. LQZ-7I orally effectively inhibits xenograft tumor growth and induces survivin loss in tumors.
|
-
- HY-N11172
-
|
Schibitubin I
|
Others
|
Neurological Disease
|
|
Schibitubin I is a lignin. Schibitubin I has neuroprotective activity. Schibitubin I can be isolated from the fruits of Schisandra bicolor var. tuberculata.
|
-
- HY-107301
-
-
- HY-P1768
-
|
Urechistachykinin I
Uru-TK I
|
Bacterial
|
Infection
|
|
Urechistachykinin I (Uru-TK I), an invertebrate tachykinin-related peptides (TRPs) isolated from echiuroid worms, shows antimicrobial activities without a hemolytic effect.
|
-
- HY-N2013
-
|
Aristolactam I
Aristololactam; Aristolactam
|
Caspase
Apoptosis
|
Inflammation/Immunology
|
|
Aristololactam I (AL-I), is the main metabolite of aristolochic acid I (AA-I), participates in the processes that lead to renal damage.
Aristololactam I (AL-I) directly injures renal proximal tubule cells, the cytotoxic potency of AL-I is higher than that of AA-I and that the cytotoxic effects of these molecules are mediated through the induction of apoptosis in a caspase-3-dependent pathway.
|
-
- HY-N11455
-
-
- HY-117793
-
-
- HY-107588
-
|
TC-I 15
|
Integrin
|
Cardiovascular Disease
|
|
TC-I 15 (TC-I-15) is an allosteric, collagen-binding integrin α2β1 inhibitor with IC50 values of 26.8 μM and 0.4 μM for GFOGER and GLOGEN, respectively. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition.
|
-
- HY-143402
-
|
Topoisomerase I/II inhibitor 2
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer.
|
-
- HY-15167
-
-
- HY-P1777
-
|
IGF-I (24-41)
Insulin-like Growth Factor I (24-41)
|
IGF-1R
|
Metabolic Disease
Inflammation/Immunology
|
|
IGF-I (24-41) (Insulin-like Growth Factor I (24-41)) is amino acids 24 to 41 fragment of IGF-I. IGF-I, a 70 aa polypeptide hormone, is a trophic factor for both neurons and glial cells. IGF-I is partly responsible for systemic growth hormone (GH) activities. IGF-I has anabolic, antioxidant, anti-inflammatory and cytoprotective actions. IGF-I (24-41) regulates somatic growth and behavioral development.
|
-
- HY-145840
-
-
- HY-110078
-
|
Eeyarestatin I
|
p97
Apoptosis
|
Cancer
|
|
Eeyarestatin I, a potent endoplasmic reticulum-associated protein degradation (ERAD) inhibitor, is a potent protein translocation inhibitor. Eeyarestatin I inhibits Sec61 translocon. Eeyarestatin I targets the p97-associated deubiquitinating process (PAD) and inhibits atx3-dependent deubiquitination. Eeyarestatin I interferes at a step prior to proteasomal degradation. Eeyarestatin I induces cell death via the proapoptotic protein NOXA and has anticancer effects.
|
-
- HY-112134A
-
|
(R)-CSN5i-3
|
Others
|
Cancer
|
|
(R)-CSN5i-3 is the (R)-enantiomer of CSN5i-3. CSN5i-3 is a potent, selective and orally available inhibitor of CSN5.
|
-
- HY-W019806
-
-
- HY-N2541
-
-
- HY-115735
-
|
SKI-I
|
SphK
Apoptosis
|
Cancer
|
|
SKI-I is a potent and selective inhibitor of human sphingosine kinase (SK), with an IC50 of 1.2 μM for ST-hSK. SKI-I also inhibits hERK2 (IC50=11 μM). SKI-I induces apoptosis in tumor cell lines.
|
-
- HY-148093
-
|
PM-81I
|
STAT
|
Cancer
Inflammation/Immunology
|
|
PM-81I is a potent STAT6 inhibitor (targeting the SH2 structural domain) that effectively reduces STAT6 phosphorylation levels. PM-81I can be used in studies of allergic lung disease, allergic rhinitis, chronic obstructive pulmonary disease or cancer[1].
|
-
- HY-N8355
-
|
Beauveriolide I
|
Endogenous Metabolite
|
Infection
|
|
Beauveriolide I is the metabolite of Entomopathogenic Fungi Beauveria sp.. Beauveriolide I (1) exhibits moderate insecticidal activities against Spodoptera litura and Callosobruchus chinensis.
|
-
- HY-N1939
-
|
Icariside I
Icarisid I
|
Others
|
Others
|
|
Icariside I is a metabolite of Icarlin, which could regulate bone remodeling and is recognized as an effective agent for the treatment of osteoporosis.
|
-
- HY-N0887
-
-
- HY-N0407
-
|
Picroside I
6'-Cinnamoylcatalpol
|
STAT
|
Inflammation/Immunology
|
|
Picroside I is the major ingredient of Picrorhiza scrophulariiflora. Picrorhiza scrophulariiflora is a high value medicinal herb due to rich source of hepatoprotective metabolites, Picroside-I and Picroside-II. Picroside I is a promising agent for the management of asthma. Picroside I reduces the inflammation significantly at its higher dose. Picroside I also downregulates pSTAT6 and GATA3 expressions. Picroside I dose-dependently increases the serum levels of IFN-γ.
|
-
- HY-N1985
-
|
Acetylastragaloside I
|
Parasite
|
Infection
|
|
Acetylastragaloside I is a glycoside that can be isolated from the roots of Astragalus baibutensis. Acetylastragaloside I is the first cycloartane-type triterpene with remarkable trypanocidal activity with IC50 values of 9.5 and 5.0 μg/mL for T. brucei rhodesiense and T. cruzi, respectively. Acetylastragaloside I can be used for the research of trypanosome infection.
|
-
- HY-100838A
-
|
L-CCG-I
|
mGluR
|
Metabolic Disease
|
|
L-CCG-I is an extended isomer of conformationally restricted glutamate analog. L-CCG-I also is a potent agonist for mGluR2 with an EC50 value of 0.3 nM. L-CCG-I can be used for the research of mGluR family.
|
-
- HY-P1777A
-
|
IGF-I (24-41) (TFA)
Insulin-like Growth Factor I (24-41) (TFA)
|
IGF-1R
|
Metabolic Disease
Inflammation/Immunology
|
|
IGF-I (24-41) (Insulin-like Growth Factor I (24-41)) TFA is amino acids 24 to 41 fragment of IGF-I. IGF-I TFA, a 70 aa polypeptide hormone, is a trophic factor for both neurons and glial cells. IGF-I TFA is partly responsible for systemic growth hormone (GH) activities. IGF-I TFA has anabolic, antioxidant, anti-inflammatory and cytoprotective actions. IGF-I (24-41) TFA regulates somatic growth and behavioral development.
|
-
- HY-N0047
-
|
Polyphyllin I
|
JNK
mTOR
Akt
PDK-1
Autophagy
Apoptosis
|
Cancer
|
|
Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.
|
-
- HY-100383
-
|
BH3I-1
BHI1; BH 3I1
|
Bcl-2 Family
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
|
-
- HY-N7022
-
|
Eclalbasaponin I
|
Others
|
Cancer
|
|
Eclalbasaponin I is isolated from Eclipta prostrata L with antitumor activity. Eclalbasaponin I inhibits the proliferation of hepatoma cell smmc-7721 with an IC50 value of 111.1703 μg/ml.
|
-
- HY-148092
-
|
(S)-PM-43I
|
STAT
|
Cancer
Inflammation/Immunology
|
|
(S)-PM-43I is a potent STAT6 inhibitor and can reduce STAT6 phosphorylation level. (S)-PM-43I can be used in allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease and cancer research[1].
|
-
- HY-145859
-
-
- 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-N3071
-
|
Picrasidine I
|
Apoptosis
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Picrasidine I is an anti-inflammatory and anti-osteoclastogenic dimeric alkaloid that can be isolated from Picrasma quassioides. Picrasidine I inducs cell cycle arrest, and triggers cell apoptosis by downregulats ERK and Akt pathways. Picrasidine I inhibits the activation of MAPKs, NF-κB and ROS generation, and suppresses the expression of c-Fos and NFATc1.
|
-
- HY-N7141
-
-
- HY-118044
-
-
- HY-P1773A
-
|
IGF-I (30-41) (TFA)
Insulin-like Growth Factor I (30-41) (TFA)
|
IGF-1R
|
Metabolic Disease
Inflammation/Immunology
|
|
IGF-I (30-41) (TFA) is amino acids 30 to 41 fragment of Insulin-like Growth Factor I (IGF-I). IGF-I is partly responsible for systemic GH activities although it possesses a wide number of own properties (anabolic, antioxidant, anti-inflammatory and cytoprotective actions).
|
-
- HY-119016A
-
|
SK1-I hydrochloride
BML-258 hydrochloride
|
SphK
|
Cancer
|
|
SK1-I hydrochloride (BML-258 hydrochloride), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I hydrochloride shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I hydrochloride enhances autophagy and has antitumor activity.
|
-
- HY-119016
-
|
SK1-I
BML-258
|
SphK
|
Cancer
|
|
SK1-I (BML-258), an analog of sphingosine, is an isozyme-specific competitive SPHK1 inhibitor with a Ki value of 10 µM. SK1-I shows no activity at SPHK1 PKCα, PKCδ, PKA, AKT1, ERK1, EGFR, CDK2, IKKβ or CamK2β. SK1-I enhances autophagy and has antitumor activity.
|
-
- HY-147649
-
-
- HY-B0175
-
-
- HY-N3921
-
|
Gancaonin I
|
Others
|
Cancer
|
|
Gancaonin I, an Isoflavone, exhibits moderate inhibition on human carboxylesterase 2 (hCES2A) with IC50 of 1.72 μM. Gancaonin I inhibits hCES2A-mediated fluorescein diacetate (FD) hydrolysis.
|
-
- HY-147647
-
-
- HY-107284
-
-
- HY-N1085
-
-
- HY-N0612
-
-
- HY-N2999
-
-
- HY-141881
-
|
PROTAC-O4I2
|
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC-O4I2 is a PROTAC targets splicing factor 3B1 (SF3B1). PROTAC-O4I2 induces FLAG-SF3B1 degradation with an IC50 value of 0.244 μM in K562 cells. PROTAC-O4I2 also induces cellular apoptosis in K562 WT cells.
|
-
- HY-N11461
-
|
LNnDFH I
Lacto-N-neo-difucohexaose I
|
Others
|
Others
|
|
LNnDFH I is a natural product that can be isolated from human urine.
|
-
- HY-138181
-
|
Contezolid phosphoramidic acid
MRX-I phosphoramidic acid
|
Others
|
Others
|
|
Contezolid phosphoramidic acid is an intermediate in the synthesis of proagents of antibacterial oxazolidinone agent MRX-I. Contezolid phosphoramidic acid is extracted from patent WO2015127316A1, Intermediate 3, Method I.
|
-
- HY-147648
-
-
- HY-110199
-
|
TC-I 2014
|
TRP Channel
|
Neurological Disease
|
|
TC-I 2014 (compound 5) is a potent and orally active Benzimidazole-containing transient receptor potential melastatin 8 (TRPM8) antagonist, with IC50 values of 0.8 nM, 3.0 nM and 4.4 nM for canine, human and rat channels respectively. TC-I 2014 exhibits antiallodynic properties in pain models.
|
-
- HY-N2466A
-
|
Melanotan I acetate
MT-I acetate; [Nle4,D-Phe7]-α-MSH acetate
|
Melanocortin Receptor
|
Cancer
|
|
Melanotan I acetate is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I acetate is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I acetate can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I acetate can be used for sunlight-induced skin cancers research.
|
-
- HY-N2466
-
|
Melanotan I
MT-I; [Nle4,D-Phe7]-α-MSH
|
Melanocortin Receptor
|
Cancer
|
|
Melanotan I is a potent non-selective melanocortin receptor (MCR) agonist. Melanotan I is a synthetic analogue of α-melanocyte stimulating hormone (α-MSH) that stimulates melanogenesis. Melanotan I can induce skin tanning by mimicking the actions of a-MSH on the melanocortin type 1 receptors (MC1R) of melanocytes. Melanotan I can be used for sunlight-induced skin cancers research.
|
-
- HY-N8183
-
-
- HY-N3030
-
-
- HY-76293
-
|
I2906
|
Bacterial
|
Infection
|
|
I2906 showed antimycobacterial and cytotoxic activity against mycobacterium tuberculosis.
|
-
- HY-144061
-
|
INSCoV-601I(1)
|
SARS-CoV
|
Infection
|
|
INSCoV-601I(1) is a potent inhibitor of M pro (3CL pro). Proteases (PL pro and 3CL pro) are involved with transcription and replication of the virus. INSCoV-601I(1) has the potential for the research of SARS-CoV-2 infection (extracted from patent WO2021219089A1).
|
-
- HY-135680
-
|
I-OMe-Tyrphostin AG 538
I-OMe-AG 538
|
IGF-1R
|
Cancer
Metabolic Disease
|
|
I-OMe-Tyrphostin AG 538 (I-OMe-AG 538) is a specific inhibitor of IGF-1R (insulin-like growth factor-1 receptor tyrosine kinase). I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and is preferentially cytotoxic to nutrient-deprived PANC1 cells. I-OMe-Tyrphostin AG 538 is an ATP-competitive inhibitor of phosphatidylinositol-5-phosphate 4-kinase α (PI5P4Kα), with an IC50 of 1 µM.
|
-
- HY-141627
-
-
- HY-148761
-
|
PSMA I&T
|
Others
|
Cancer
|
|
PSMA I&T is a potent PSMA (prostate-specific membrane antigen) inhibitor. PSMA I&T can be used for SPECT/CT imaging and radionuclide research of prostate cancer (PCa).
|
-
- HY-N6579
-
-
- HY-15167A
-
-
- HY-N2286
-
-
- HY-N4213
-
-
- HY-125684
-
-
- HY-D1116
-
|
MitoMark Red I
|
Fluorescent Dye
|
Others
|
|
MitoMark Red I is a fluorescent mitochondrial marker. MitoMark Red I is a red fluorescent dye which accumulates in mitochondria in viable cells and has an excitation wavelength of 578 nm and emission of 599 nm.
|
-
- HY-N5082
-
-
- HY-N5095
-
-
- HY-N11450
-
-
- HY-44157
-
|
ALS-I
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
ALS-I, an acid-Liable surfactant, is adopted for in-solution enzymatic digestions, can help to solubilize hydrophobic proteins. ALS-I is significantly enhanced peptide recovery for mass spectrometry (MS) mapping in the study of the proteomes of regenerating rat retina and mouse brain.
|
-
- HY-131318
-
|
Lenalidomide-I
|
Ligands for E3 Ligase
|
Cancer
|
|
Lenalidomide-I (Compound 72), an analog of cereblon (CRBN) ligand Lenalidomide for E3 ubiquitin ligase, is used in the recruitment of CRBN protein. Lenalidomide-I can be connected to the ligand for protein by a linker to form PROTACs, such as the PROTAC BET degrader QCA570 (HY-112609).
|
-
- HY-P2200
-
|
Siamycin I
BMY-29304
|
HIV
Antibiotic
|
Infection
Inflammation/Immunology
|
|
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research.
|
-
- HY-148058
-
|
Topoisomerase I inhibitor 8
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 8 is a potent topoisomerase I inhibitor. Topoisomerase I inhibitor 8 is a hexacyclic analogue of camptothecin, and displays cytotoxic effect against tumor cells.
|
-
- HY-P3934
-
-
- HY-151894
-
|
I-BET432
|
Epigenetic Reader Domain
|
Cancer
|
|
I-BET432 is a BET inhibitor. I-BET432 inhibits BRD4 N-terminal bromodomain (BD1) and the C-terminal bromodomain (BD2) with pIC50 values of 7.5 and 7.2, respectively. I-BET432 can be used as an oral candidate quality molecule for the research of multiple oncology and inflammatory diseases.
|
-
- HY-146180
-
|
FSDD0I
|
FAP
|
Cancer
|
|
FSDD0I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD0I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-D1148
-
|
HKGreen-4I
|
Fluorescent Dye
|
Others
|
|
HKGreen-4I is a highly sensitive green fluorescent probe for the specific detection of H2O2 in living cells with a maximum excitation wavelength and emission wavelength of 520 nm and 543 nm, respectively.
|
-
- HY-146181
-
|
FSDD1I
|
FAP
|
Cancer
|
|
FSDD1I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD1I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-146182
-
|
FSDD3I
|
FAP
|
Cancer
|
|
FSDD3I is an albumin-binding fibroblast activation protein (FAP) ligand. FSDD3I can be labeled with 68Ga and 177Lu for single photon emission computed tomography (SPECT) imaging.
|
-
- HY-128206
-
|
I3MT-3
HMPSNE
|
Hippo (MST)
|
Metabolic Disease
|
|
I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST.
|
-
- HY-143266
-
|
Topoisomerase I inhibitor 3
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 3 (Compound ZML-14) is a topoisomerase I inhibitor and can interact with topoisomerase I-DNA complex. Topoisomerase I inhibitor 3 induces HepG2 cell apoptosis and arrests cell cycle at G2/M phase.
|
-
- HY-P1542
-
|
Urotensin I
Catostomus urotensin I
|
CRFR
|
Cardiovascular Disease
Endocrinology
|
|
Urotensin I (Catostomus urotensin I), a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively.
|
-
- HY-N3983
-
-
- HY-D0140
-
|
Chromoionophore I
ETH 5294
|
Fluorescent Dye
|
Others
|
|
Chromoionophore I (ETH 5294) is a hydrophobic pH indicator. Chromoionophore I is used as a transmissive or fluorescent probe molecule in many types of hydrophobic sensor membranes. Chromoionophore I is oil-soluble.
|
-
- HY-148170
-
|
L-I-OddU
|
EBV
DNA/RNA Synthesis
Nucleoside Antimetabolite/Analog
|
Infection
|
|
L-I-OddU, a L-5'-halo- dioxolane nucleoside analogue, is a potent and selective anti-Epstein-Barr virus (EBV) agent with an EC50 value of 0.03μM. L-I-OddU has low cytotoxicity with a CC50 value of 1000 nM. L-I-OddU has antiviral activity by suppressing replicative EBV DNA and viral protein synthesis.
|
-
- HY-P1839
-
|
Angiotensin I/II (1-5)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-5 is a peptide that contains the amino acids 1-5, which is converted from Angiotensin I/II. Angiotensin I is formed by the action of renin on angiotensinogen. Angiotensin II is produced from angiotensin I. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-124211S
-
-
- HY-N0201
-
|
Atractylenolide I
|
Toll-like Receptor (TLR)
JAK
STAT
|
Cancer
|
|
Atractylenolide I is a sesquiterpene derived from the rhizome of Atractylodes macrocephala, possesses diverse bioactivities, such as neuroprotective, anti-allergic, anti-inflammatory and anticancer properties. Atractylenolide I reduces protein levels of phosphorylated JAK2 and STAT3 in A375 cells, and acts as a TLR4-antagonizing agent.
|
-
- HY-N7026
-
|
Celosin I
|
Others
|
Metabolic Disease
|
|
Celosin I, an oleanane-type triterpenoid saponin isolated from the seeds of Celosia argentea L, could be used as chemical markers for the quality control of C. argentea seeds. Celosin I exhibits significant hepatoprotective effect on carbon tetrachloride-induced and N,N-dimethylformamide-induced hepatotoxicity in mice.
|
-
- HY-144774
-
|
Topoisomerase I inhibitor 5
|
Topoisomerase
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Topoisomerase I inhibitor 5 is an effective topoisomerase inhibitor with IC50 value of. Topoisomerase I inhibitor 5 can interfere with DNA and significantly inhibit the activity of Topoisomerase I. Topoisomerase I inhibitor 5 can arrest cell cycle at the G1 phase and induce MCF-7 cells apoptosis. Topoisomerase I inhibitor 5 has potency in reversing P-gp-mediated resistance to Adriamycin.
|
-
- HY-P1396
-
-
- HY-124012
-
|
PCNA-I1
|
DNA/RNA Synthesis
|
Cancer
|
|
PCNA-I1 is a potent PCNA (proliferating cell nuclear antigen) inhibitor. PCNA-I1 directly binds PCNA trimers with a Kd of 0.41 μM and exhibits antitumor activity both in vitro and in vivo.
|
-
- HY-107300
-
-
- HY-N6889
-
-
- HY-N8343
-
-
- HY-146654
-
|
Glyoxalase I inhibitor 2
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 2 (compound 26) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 0.5 µM. Glyoxalase I inhibitor 2 has the potential for the research of depression and anxiety.
|
-
- HY-111237
-
|
Butyrolactone I
Olomoucin
|
CDK
|
Cancer
|
|
Butyrolactone I is an ATP-competitive inhibitor of CDK1 as a secondary metabolite from A. terreus. Butyrolactone I has antitumor effects in non-small cell lung, small cell lung, and prostate cancer cell lines.
|
-
- HY-146656
-
-
- HY-N0745
-
|
Senkyunolide I
|
Caspase
|
Inflammation/Immunology
|
|
Senkyunolide I, isolated from Ligusticum chuanxiong Hort, is an anti-migraine compound. Senkyunolide I protects rat brain against focal cerebral ischemia-reperfusion injury by up-regulating p-Erk1/2, Nrf2/HO-1 and inhibiting caspase 3.
|
-
- HY-146655
-
|
Glyoxalase I inhibitor 3
|
Glyoxalase (GLO)
|
Cancer
|
|
Glyoxalase I inhibitor 3 (compound 22g) is a potent glyoxalase I (GLO1) inhibitor with an IC50 of 0.011 µM. Glyoxalase I inhibitor 3 has the potential for the research of depression and anxiety.
|
-
- HY-N10414
-
|
Primulic acid I
Primulasaponin 1; Primula acid I
|
Others
|
Others
|
|
Primulic acid I (Primulasaponin 1) is a plant-derived triterpenoid saponin with one sugar chain (monodesmoid).
|
-
- HY-W073080
-
-
- HY-W127791
-
-
- HY-W127800
-
-
- HY-107400
-
|
B I09
|
IRE1
|
Cancer
|
|
B I09 is an IRE-1 RNase inhibitor, with an IC50 of 1230 nM.
|
-
- HY-19541A
-
|
I-CBP112 hydrochloride
|
Epigenetic Reader Domain
|
Cancer
|
|
I-CBP112 hydrochloride is a selective inhibitor of CBP/P300 that directly binds their bromodomains (Kds = 142 and 625 nM, respectively). I-CBP112 significantly reduces the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. I-CBP112 increases the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.
|
-
- HY-107202A
-
|
Poly (I:C):Kanamycin (1:1)
|
Toll-like Receptor (TLR)
|
Infection
|
|
Poly (I:C):Kanamycin (1:1) is a mixture of poly (I:C) and kanamycin. Poly(I:C) is a synthetic double-stranded RNA (dsRNA), which is a Toll-like receptor 3 (TLR3) agonist. Kanamycin is positively charged (poly-NH3) and can thus neutralize the negative charge of Poly I:C and thereby stabilized the molecule.
|
-
- HY-135748
-
|
Polyinosinic-polycytidylic acid sodium
Poly(I:C) sodium
|
Toll-like Receptor (TLR)
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Polyinosinic-polycytidylic acid (Poly(I:C)) sodium is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid sodium can directly trigger cancer cells to undergo apoptosis.
|
-
- HY-134958
-
|
Polyinosinic-polycytidylic acid potassium
Poly(I:C) potassium
|
Toll-like Receptor (TLR)
Apoptosis
|
Cancer
Inflammation/Immunology
|
|
Polyinosinic-polycytidylic acid potassium (Poly(I:C) potassium) is a synthetic analog of double-stranded RNA and an agonist of toll-like receptor 3 (TLR3) and retinoic acid inducible gene I (RIG-I)-like receptors (RIG-I and MDA5). Polyinosinic-polycytidylic acid sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses, and to alter the tumor microenvironment. Polyinosinic-polycytidylic acid potassium can directly trigger cancer cells to undergoApoptosis.
|
-
- HY-P1829
-
|
Angiotensin I/II (1-6)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II 1-6 contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. The precursor angiotensinogen is cleaved by renin to form angiotensin I. Angiotensin I ishydrolyzed by angiotensin-converting enzyme (ACE) to form the biologically active angiotensin II. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-19915
-
-
- HY-103078A
-
|
I-XW-053 sodium
|
HIV
|
Infection
|
|
I-XW-053 sodium is a potent HIV-1 inhibitor with an IC50 value of 164.2 μM. I-XW-053 sodium is a novel antiviral that targets a unique site on the HIV-1 CA protein and inhibits by affecting virus uncoating[1] .
|
-
- HY-N7532
-
-
- HY-N3775
-
-
- HY-112476
-
|
PRL-3 Inhibitor I
|
Phosphatase
|
Cancer
|
|
PRL-3 Inhibitor I is a potent PRL-3 inhibitor with an IC50 of 0.9 μM. PRL-3 Inhibitor I shows a reduced invasion in cell-based assay.
|
-
- HY-124813
-
|
PDZ1i
113B7
|
FAK
EGFR
MMP
|
Cancer
|
|
PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion.
|
-
- HY-146653
-
-
- HY-P1194
-
|
Spantide I
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
|
-
- HY-125733
-
|
Thiocillin I
|
Bacterial
Antibiotic
|
Infection
|
|
Thiocillin I is a thiopeptide antibiotic and has in vitro antibacterial activity against Gram-positive bacterial strains. The MIC values of Thiocillin I against S. aureus 1974149, E. faecalis 1674621, B. subtilis ATCC 6633 and S. pyogenes 1744264 are 2 μg/mL, 0.5 μg/mL, 4 μg/mL and 0.5 μg/mL, respectively.
|
-
- HY-100341
-
|
M2I-1
|
Others
|
Others
|
|
M2I-1 is a Mad2 inhibitor targeting the binding of Mad2 to Cdc20, an essential protein-protein interaction (PPI) within the spindle assembly checkpoint (SAC).
|
-
- HY-18975
-
|
I-BRD9
|
Epigenetic Reader Domain
|
Cancer
Inflammation/Immunology
|
|
I-BRD9 is a selective cellular chemical probe of bromodomain-containing protein 9 (BRD9) with pIC50 value of 7.3 μM. I-BRD9 has high selectivity for bromodomain and extra terminal domain (BET) family and highly homologous bromodomain-containing protein 7 (BRD7). I-BRD9 can be used to identify genes regulated by BRD9 in Kasumi-1 cells involved in oncology and immune response pathways.
|
-
- HY-143301
-
|
Topoisomerase I inhibitor 4
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I inhibitor 4 (compound 7a) is a topoisomerase I inhibitor. Topoisomerase I inhibitor 4 inhibits HepG2, A549, MCF-7 and HeLa cancer cells proliferation with IC50s of 1.20, 2.09, 1.56 and 1.92 μM, respectively. Topoisomerase I inhibitor 4 can be used for the research of cancer.
|
-
- HY-18772
-
|
O4I2
|
Oct3/4
|
Others
|
|
O4I2 is a potent Oct3/4 inducer. O4I2 induces the expression of pluripotent-associated genes Lin28, Sox2 and Nanog, and suppresses Rex1.
|
-
- HY-152086
-
|
DRP1i27
|
Dynamin
|
Cardiovascular Disease
|
|
DRP1i27 is a potent inhibitor of human Drp1 (dynamin-related protein 1). DRP1i27 binds to the GTPase site of Drp1, with hydrogen bonds to Gln34 and Asp218. DRP1i27 targets Drp1-mediated mitochondrial fission in cell line models and protects against simulated ischemia-reperfusion injury.
|
-
- HY-146504
-
|
Topoisomerase I/II inhibitor 3
|
Topoisomerase
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
Topoisomerase I/II inhibitor 3 (compound 7) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 3 can inhibit cell proliferation, invasion and migration, and induce apoptosis by inhibiting PI3K/Akt/mTOR signaling pathway. Topoisomerase I/II inhibitor 3 can be used for liver cancer research.
|
-
- HY-139865
-
-
- HY-117426
-
|
MO-I-500
|
Others
|
Cancer
|
|
MO-I-500 is a pharmacological of FTO inhibitor with an IC50 of 8.7 μM for the inhibition of purified FTO demethylase catalyzing demethylation of an artificial small methylated substrate. MO-I-500 can be used for the research of rare panresistant triple-negative inflammatory breast cancer.
|
-
- HY-N8331
-
-
- HY-R01687
-
|
hsa-miR-548i mimic
|
MicroRNA
|
Cancer
|
|
hsa-miR-548i mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R03056
-
|
mmu-miR-344i mimic
|
MicroRNA
|
Cancer
|
|
mmu-miR-344i mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R04367
-
|
rno-miR-344i mimic
|
MicroRNA
|
Cancer
|
|
rno-miR-344i mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R03472
-
|
mmu-miR-669i mimic
|
MicroRNA
|
Cancer
|
|
mmu-miR-669i mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R00852
-
|
hsa-miR-378i mimic
|
MicroRNA
|
Cancer
|
|
hsa-miR-378i mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-P1542B
-
|
Urotensin I TFA
Catostomus urotensin I TFA
|
CRFR
|
Endocrinology
Cardiovascular Disease
|
|
Urotensin I (Catostomus urotensin I) TFA, a CRF-like neuropeptide, acts as an agonist of CRF receptor with pEC50s of 11.46, 9.36 and 9.85 for human CRF1, human CRF2 and rat CRF2α receptors in CHO cells, and Kis of 0.4, 1.8, and 5.7 nM for hCRF1, rCRF2α and mCRF2β receptors, respectively.
|
-
- HY-W008867
-
-
- HY-P1396A
-
-
- HY-P1073
-
|
ProTx-I
|
Calcium Channel
Sodium Channel
Potassium Channel
|
Cancer
|
|
ProTx-I, a venom toxin of the tarantula Thrixopelma pruriens, is a potent, selective CaV3.1 channel blocker with IC50 values of 0.2 μM and 31.8 μM for hCaV3.1 and hCaV3.2 respectively. ProTx-I is also a potent blocker for voltage-gated Na + channels and inhibits KV 2.1 channels.
|
-
- HY-N7052
-
|
Tubulysin I
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Tubulysin I is a highly cytotoxic peptide isolated from the myxobacterial species Archangium geophyra and Angiococcus disciformis. Tubulysin displays extremely potent cytotoxic activity in mammalian cells, including multidrug-resistant cell lines, with IC50 values in the lower nanomolar range. Tubulysin I is a cytotoxic activity tubulysin which inhibits tubulin polymerization and leads to cell cycle arrest and apoptosis.
|
-
- HY-148152
-
-
- HY-142520
-
-
- HY-112405
-
|
BPIQ-I
PD 159121
|
EGFR
|
Cancer
|
|
BPIQ-I (PD 159121) is a potent and ATP-competitive EGFR tyrosine kinase inhibitor.. BPIQ-I shows anti-proliferative actively.
|
-
- HY-N0940
-
-
- HY-113318
-
-
- HY-N2102
-
|
Tenacissoside I
|
Others
|
Cancer
|
|
Tenacissoside I is a C21 steroid from the Marsdenia tenacissima, which is detected at relatively high level in M. tenacissima.
|
-
- HY-112134
-
|
CSN5i-3
|
Others
|
Cancer
|
|
CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
|
-
- HY-18771
-
-
- HY-124691
-
|
D-I03
|
DNA/RNA Synthesis
|
Cancer
|
|
D-I03 is a selective RAD52 inhibitor with a Kd of 25.8 µM. D-I03 specifically inhibits RAD52-dependent single-strand annealing (SSA) and D-loop formation with IC50s of 5 µM and 8 µM, respectively. D-I03 suppresses growth of BRCA1- and BRCA2-deficient cells and inhibits formation of damage-induced RAD52 foci, but does not effect on RAD51 foci induced by Cisplatin.
|
-
- HY-P0324
-
|
Parasin I
|
Bacterial
|
Infection
|
|
Parasin I is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
|
-
- HY-P1829A
-
|
Angiotensin I/II (1-6) (TFA)
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Angiotensin I/II (1-6) TFA contains the amino acids 1-6 and is converted from Angiotensin I/II peptide. The precursor angiotensinogen is cleaved by renin to form angiotensin I. Angiotensin I ishydrolyzed by angiotensin-converting enzyme (ACE) to form the biologically active angiotensin II. Angiotensin II has been investigated for the treatment, basic science, and diagnostic of Hypertension, Renin Angiotensin System, and Idiopathic Membranous Nephropathy.
|
-
- HY-P3572
-
|
Adipokinetic hormone I (Locusta migratoria)
Lom-AKH-I
|
Endogenous Metabolite
|
Endocrinology
|
|
Adipokinetic hormone I (Locusta migratoria) (Lom-AKH-I) is a insect adipokinetic hormone (AKH), enhances fat body cAMP levels in vitro. Insect adipokinetic hormones (AKHs) controls flight-directed mobilization of carbohydrate and lipid from fat body stores, which depends on AKH receptor(s) coupling to cAMP formation and glycogen phosphorylase activation via the stimulatory guanine nucleotide-binding protein (Gs).
|
-
- HY-N5042
-
-
- HY-N4246
-
|
Bacopaside I
|
Others
|
Neurological Disease
|
|
Bacopaside I, a saponin isolated from Bacopa monnieri, exbibits antioxidant properties and free radical scavenging capacity and exerts antidepressant-like effect.
|
-
- HY-N10111
-
-
- HY-W073069
-
-
- HY-N5032
-
-
- HY-128044
-
|
Ftase inhibitor I
B581
|
Farnesyl Transferase
|
Cancer
|
|
Ftase inhibitor I (B581) is a potent, selective and peptidomimetic farnesyl transferase (FTase) inhibitor. Ftase inhibitor I shows selectivity for FTase over geranylgeranyl isoprenoid (Ras-GG) or the fatty acid myristate (Myr-Ras).
|
-
- HY-P1194A
-
|
Spantide I TFA
|
Neurokinin Receptor
|
Inflammation/Immunology
|
|
Spantide I TFA, a substance P analog, is a selective NK1 receptor antagonist, with Ki values of 230 nM and 8150 nM for NK1 and NK2 receptor, respectively. Spantide I provides an approach to reduce type 1 and enhance the type 2 cytokine IL-10 in the infected cornea, leading to a significant reduction in corneal perforation.
|
-
- HY-N0432
-
|
Astragaloside I
Astrasieversianin IV; Cyclosieversioside B
|
Wnt
β-catenin
|
Metabolic Disease
|
Astragaloside I, one of the main active ingredients in Astragalus membranaceus, has osteogenic properties. Astragaloside I stimulates osteoblast differentiation through the Wnt/β-catenin signaling pathway.
|
-
- HY-N9317
-
-
- HY-P1097
-
-
- HY-150755
-
-
- HY-A0126
-
|
Epoprostenol
Prostaglandin I2; Prostacyclin
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Epoprostenol (Prostaglandin I2), the synthetic form of the natural prostaglandin derivative Prostacyclin (Prostaglandin I2), is registered worldwide for the treatment of Pulmonary arterial hypertension (PAH. Epoprostenol is used in pulmonary hypertension and transplantation as a potent inhibitor of platelet aggregation.
|
-
- HY-W008452
-
-
- HY-W006103
-
-
- HY-N11529
-
-
- HY-15146
-
|
NSC 74859
S3I-201
|
STAT
|
Cancer
|
|
NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM.
|
-
- HY-108905
-
|
Mecasermin
Human IGF-I; FK 780
|
IGF-1R
|
Metabolic Disease
|
|
Mecasermin (Human IGF-I; FK 780) is a recombinant human insulin-like growth factor I (IGF-I). Mecasermin has the potential for the study of the growth failure of growth hormone (GH) insensitivity caused by GH receptor defects or GH-inhibiting antibodies.
|
-
- HY-148152A
-
-
- HY-135748A
-
|
Poly (I:C):Kanamycin (1:1) (sodium)
|
Toll-like Receptor (TLR)
Apoptosis
|
Cancer
Infection
|
|
Poly (I:C):Kanamycin (1:1) sodium is an isometric complex of Poly (I:C) (HY-135748) and Kanamycin (HY-16566). Poly(I:C) sodium, a synthetic analog of double-stranded RNA, is a TLR3 and retinoic acid-inducible gene I receptor (RIG-I and b>MDA5) agonist. Poly(I:C) sodium can be used as a vaccine adjuvant to enhance innate and adaptive immune responses and induce apoptosis in cancer cells. Kanamycin is an orally active antibacterial agent (Gram-negative/positive bacteria) that inhibits translocation and causes miscoding by binding to the 70S ribosomal subunit. Kanamycin shows good inhibitory activity against Mycobacterium tuberculosis (susceptible and drug-resistant) and Klebsiella pneumoniae, and can be used in the research of tuberculosis and pneumonia.
|
-
- HY-50713
-
-
- HY-W013714
-
-
- HY-W007615
-
-
- HY-W019776
-
|
Sudan I-d5
Solvent Yellow 14-d5
|
Bacterial
|
Infection
|
|
Sudan I-d5 is a the deuterated Sudan I. Sudan I is a diazo-conjugate red dye and can be used as an additive to products such as oils, solvents or polishes. Sudan I inhibits growth of bacterial strains Clostridium perfringens and L. rhamnosus[1].
|
-
- HY-W008452S
-
|
H-Tyr(3-I)-OH-13C6
|
Endogenous Metabolite
|
Metabolic Disease
|
|
H-Tyr(3-I)-OH- 13C6 is the 13C-labeled H-Tyr(3-I)-OH. H-Tyr(3-I)-OH is a potent and effective tyrosine hydroxylase inhibitor. H-Tyr(3-I)-OH is an intermediate in the production of thyroid hormones and has a role as a human or mouse metabolite[1][2].
|
-
- HY-103351
-
-
- HY-P1593
-
-
- HY-P1270
-
|
α-Conotoxin Im-I
|
nAChR
|
Neurological Disease
|
|
α-Conotoxin Im-I is a selective α7/α9 nAChR antagonist, blocking α7 nicotinic receptors with the highest apparent affinity, while having an 8-fold lower affinity for homomeric α9 nicotinic receptors. α-Conotoxin Im-I is toxic and induces seizures in rodents. α-Conotoxin Im-I is a tool for studying neuronal nAChR.
|
-
- HY-N6724
-
|
Altertoxin I
Dihydroalterperylenol
|
Others
|
Metabolic Disease
|
|
Altertoxin I (Dihydroalterperylenol) is a quinone-type mycotoxin produced by Alternaria alternata fungi, which is mutagenic and cytotoxic, and can weakly disrupts metabolic communication.
|
-
- HY-W127440
-
-
- HY-W096157
-
-
- HY-W096156
-
-
- HY-N0697
-
-
- HY-N10206
-
|
11-epi-Chaetomugilin I
|
Endogenous Metabolite
|
Cancer
|
|
11-epi-Chaetomugilin I is a metabolite found in Chaetomium globosum. 11-epi-Chaetomugilin I exhibits significant cytotoxic activity against the murine P388 leukemia cell line, the human HL-60 leukemia cell line, the murine L1210 leukemia cell line, and the human KB epidermoid carcinoma cell line.
|
-
- HY-13032B
-
-
- HY-D0024
-
|
Sudan I
Solvent Yellow 14
|
Bacterial
|
Others
|
|
Sudan I (Solvent Yellow 14) is a diazo-conjugate red dye and can be used as an additive to products such as oils, solvents or polishes. Sudan I inhibits growth of bacterial strains Clostridium perfringens and L. rhamnosus.
|
-
- HY-112546
-
-
- HY-138620
-
-
- HY-P0324A
-
|
Parasin I TFA
|
Bacterial
|
Infection
|
|
Parasin I (TFA) is a 19-amino acid histone H2A-derived peptide isolated from the skin of the catfish, and shows antimicrobial activity.
|
-
- HY-101387
-
|
rel-ACPT-I
|
mGluR
|
|
|
rel-ACPT-I is an agonist of group III mGluRs with diverse biological activities including neuroprotective, anticonvulsant, and anxiolytic-like effects.
|
-
- HY-A0126A
-
|
Epoprostenol sodium
Prostaglandin I2 sodium salt; Prostacyclin sodium salt; Flolan
|
Endogenous Metabolite
|
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-R03182
-
|
mmu-miR-466i-5p mimic
|
MicroRNA
|
Cancer
|
|
mmu-miR-466i-5p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R00014
-
|
hsa-let-7i-5p mimic
|
MicroRNA
|
Cancer
|
|
hsa-let-7i-5p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R00013
-
|
hsa-let-7i-3p mimic
|
MicroRNA
|
Cancer
|
|
hsa-let-7i-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-R03181
-
|
mmu-miR-466i-3p mimic
|
MicroRNA
|
Cancer
|
|
mmu-miR-466i-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
|
-
- HY-19760
-
|
I-BET282
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
|
-
- HY-I0512
-
|
Sofosbuvir impurity I
|
HCV
|
Infection
|
|
Sofosbuvir impurity I, an diastereoisomer of Sofosbuvir, is the impurity of Sofosbuvir. Sofosbuvir (PSI-7977) is an inhibitor of HCV RNA replication, demonstrates potent anti-hepatitis C virus activity.
|
-
- HY-N5004
-
-
- HY-126548
-
-
- HY-P1032
-
-
- HY-W011472
-
-
- HY-W009284
-
-
- HY-W016028
-
-
- HY-N0890
-
|
Tubeimoside I
Tubeimoside-1; Lobatoside-H
|
Apoptosis
|
Cancer
|
|
Tubeimoside I(Lobatoside-H) is an extract from Chinese herbal medicine Bolbostemma paniculatum (MAXIM.
|
-
- HY-19541
-
-
- HY-N6854
-
|
Mogroside I A1
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside I A1 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-N6853
-
|
Mogroside I E1
|
Others
|
Cancer
Metabolic Disease
|
|
Mogroside I E1 is a triterpenoid glycoside and a nonsugar sweetener. Mogrosides are sweeter than sucrose. Mogrosides exhibit antioxidant, antidiabetic and anticancer activities.
|
-
- HY-P2643
-
-
- HY-P1593A
-
-
- HY-149012
-
-
- HY-P3673
-
|
Lamprey LH-RH I
|
GnRH Receptor
|
Endocrinology
|
|
Lamprey LH-RH I is a gonadotropin-releasing hormone, elevates plasma steroid levels and stimulates ovulation in the lamprey without biological activity in other animal models.
|
-
- HY-13329
-
-
- HY-B1411
-
|
i-Inositol
myo-Inositol; meso-Inositol
|
Endogenous Metabolite
|
Others
|
|
i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
|
-
- HY-D0929
-
-
- HY-N0134
-
-
- HY-N10418
-
|
Isorhapontin
|
Fungal
|
Infection
|
|
Isorhapontin is an antifungal agent. Isorhapontin inhibits the hydrolytic activity of Trichoderma cellobiohydrolase I (CBH I) with a Ki of 57.2 μM. Isorhapontin also inhibits the activity of Trichoderma endoglucanase I.
|
-
- HY-P1336
-
-
- HY-P2416
-
-
- HY-P3064
-
|
Scyllatoxin
Leiurotoxin I
|
Potassium Channel
|
Neurological Disease
|
|
Scyllatoxin (Leiurotoxin I) is a peptide toxin, it can be isolated from the venom of the scorpion (Leiurus quinquestriatus hebraeus). Scyllatoxin is a blocker of small-conductance KCa (SK) channel. Scyllatoxin enhances both norepinephrine (NE) and epinephrine (Epi) release in vivo.
|
-
- HY-19760B
-
|
I-BET282E
|
Epigenetic Reader Domain
|
Inflammation/Immunology
|
|
I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).
|
-
- HY-B1411S1
-
-
- HY-128026
-
-
- HY-P99619
-
|
Finotonlimab
SCT-I10A
|
PD-1/PD-L1
|
Cancer
|
|
Finotonlimab (SCT-I10A) is a recombinant humanised IgG PD-1 antibody. Finotonlimab has the potential for solid tumors or lymphomas research.
|
-
- HY-136460
-
|
Calcium ionophore I
ETH 1001
|
Calcium Channel
|
Others
|
|
Calcium ionophore I (ETH 1001) is a selective Ca 2+ ionophore for biological membranes. Calcium ionophore I can be used in Ca2+-selective microelectrodes that can be used for quantitative intracellular measurements of resting Ca2+-activities and of slowly changing Ca2+-levels.
|
-
- HY-A0104B
-
|
HPMC (Type I,Viscosity:100mPa.s)
Hypromellose (Type I,Viscosity:100mPa.s); (Hydroxypropyl)methyl cellulose (Type I,Viscosity:100mPa.s); Celacol HPM 5000 (Type I,Viscosity:100mPa.s)
|
Biochemical Assay Reagents
|
Others
|
|
Hypromellose (Type I,Viscosity:100mPa.s) is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-A0104D
-
|
HPMC (Type I,Viscosity:4000mPa.s)
Hypromellose (Type I,Viscosity:4000mPa.s); (Hydroxypropyl)methyl cellulose (Type I,Viscosity:4000mPa.s); Celacol HPM 5000 (Type I,Viscosity:4000mPa.s)
|
Biochemical Assay Reagents
|
Others
|
|
Hydroxypropylmethylcellulose (Type I,Viscosity:4000mPa.s) is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-A0104C
-
|
HPMC (Type I,Viscosity:400mPa.s)
Hypromellose (Type I,Viscosity:400mPa.s); (Hydroxypropyl)methyl cellulose (Type I,Viscosity:400mPa.s); Celacol HPM 5000 (Type I,Viscosity:400mPa.s)
|
Biochemical Assay Reagents
|
Others
|
|
Hydroxypropylmethylcellulose (Type I,Viscosity:400mPa.s) is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-A0104A
-
|
HPMC (Type I,Viscosity:30mPa.s)
Hypromellose (Type I,Viscosity:30mPa.s); (Hydroxypropyl)methyl cellulose (Type I,Viscosity:30mPa.s); Celacol HPM 5000 (Type I,Viscosity:30mPa.s)
|
Biochemical Assay Reagents
|
Others
|
|
Hydroxypropylmethylcellulose (Type I,Viscosity:30mPa.s) is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-B1411S
-
|
i-Inositol-d6
myo-Inositol-d6; meso-Inositol-d6
|
Endogenous Metabolite
|
Others
|
|
i-Inositol-d6 is the deuterium labeled i-Inositol. i-Inositol is a chemical compound, associated lipids are found in many foods, in particular fruit, especially cantaloupe and oranges.
|
-
- HY-N7761
-
|
Trijuganone B
Tetrahydro tanshinone I
|
Others
|
Cancer
|
|
Trijuganone B (Tetrahydro tanshinone I) can be extracted from from the roots of Salvia miltiorrhiza f. alba. Trijuganone B inhibits the proliferation of leukemia cells.
|
-
- 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-13867A
-
|
Bisindolylmaleimide I hydrochloride
GF109203X hydrochloride; Go 6850 hydrochloride
|
PKC
GSK-3
|
Cancer
Metabolic Disease
|
|
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor.
|
-
- HY-13867
-
|
Bisindolylmaleimide I
GF109203X; Go 6850
|
PKC
GSK-3
|
Metabolic Disease
Cancer
|
|
Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor.
|
-
- HY-N8086
-
-
- HY-N0011
-
-
- HY-N4290
-
-
- HY-W110927
-
-
- HY-W110884
-
-
- 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-P3730
-
-
- HY-107613A
-
|
R 59-022 hydrochloride
DKGI-I hydrochloride; Diacylglycerol kinase inhibitor I hydrochloride
|
PKC
5-HT Receptor
|
Cancer
Infection
Inflammation/Immunology
|
|
R 59-022 (DKGI-I) hydrochloride is a DGK inhibitor (IC50: 2.8 µM). R 59-022 hydrochloride inhibits the phosphorylation of OAG to OAPA. R 59-022 hydrochloride is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 hydrochloride potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-107613
-
|
R 59-022
DKGI-I; Diacylglycerol kinase inhibitor I
|
PKC
5-HT Receptor
|
Inflammation/Immunology
|
|
R 59-022 (DKGI-I) is a DGK inhibitor (IC50: 2.8 µM). R 59-022 inhibits the phosphorylation of OAG to OAPA. R 59-022 is a 5-HT Receptor antagonist, and activates protein kinase C (PKC). R 59-022 potentiates thrombin-induced diacylglycerol production in platelets and inhibits phosphatidic acid production in neutrophils.
|
-
- HY-N10917
-
|
Xanthohumol I
|
Cholinesterase (ChE)
|
Cancer
Infection
|
|
Xanthohumol I, a chalkone, is a derivative of Xanthohumol (HY-N1067). Xanthohumol is a Cholinesterase (ChE) inhibitor, which inhibits acetylcholinesterase (AChE) and butyrylcholinesterase (BChE) wih IC50s of 71.34 μM and 32.67 μM, respectively. The hydroxy compound of Xanthohumol (3-hydroxy-xanthohumol), also shoes inhibitory effect on AChE and BChE with IC50s of 51.25 μM and 63.07 μM.
|
-
- HY-107202
-
-
- HY-13032
-
-
- HY-P0269
-
|
Magainin 1
Magainin I
|
Bacterial
Fungal
Antibiotic
|
Infection
|
|
Magainin 1 (Magainin I) is an antimicrobial and amphipathic peptide isolated from the skin of Xenopus laevis. Magainin 1 exhibits antibiotic activity against numerous Gram-negative and Gram-positive bacteria.
|
-
- HY-110106
-
-
- HY-13235
-
-
- HY-107443
-
-
- HY-P3653
-
|
α-Conotoxin M I
|
mAChR
nAChR
|
Neurological Disease
|
|
α-Conotoxin M I is a potent and selective inhibitor of mAChR and α1β1γδ nAChR, but has no effect on nicotine-stimulated dopamine release. α-Conotoxins are small, disulfide-rich peptides that competitively inhibit muscle and neuronal nicotinic AChRs.
|
-
- HY-W110910
-
-
- HY-D0293
-
-
- HY-N0170
-
-
- HY-141488
-
-
- HY-P0269A
-
|
Magainin 1 TFA
Magainin I TFA
|
Bacterial
Fungal
Antibiotic
|
Infection
|
|
Magainin 1 TFA (Magainin I TFA) is an antimicrobial and amphipathic peptide isolated from the skin of Xenopus laevis. Magainin 1 TFA exhibits antibiotic activity against numerous Gram-negative and Gram-positive bacteria.
|
-
- HY-50730
-
-
- HY-N5112B
-
|
β,β-Dimethylacrylshikonin
Isoarnebin I
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative isolated from Lithospermum erythrorhizon Sieb. et Zucc. , promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway.β,β-Dimethylacrylshikonin has anti-tumor activity.
|
-
- HY-100738
-
-
- HY-16721
-
|
Cyclopropavir
Filociclovir; ZSM-I-62; MBX-400
|
CMV
HSV
|
Infection
|
|
Cyclopropavir (Filociclovir; ZSM-I-62; MBX-400) is a broad-spectrum anti-herpesvirus compound, has good antiviral activity against cytomegalovirus (CMV), herpes simplex virus (HHV)-6 and HHV-8 with EC50s of 0.7 μM to 8 μM.
|
-
- HY-W110794
-
-
- HY-154408
-
-
- HY-N0510
-
|
Aristolochic acid A
Aristolochic acid I; TR 1736
|
NF-κB
|
Cancer
|
|
Aristolochic acid A (Aristolochic acid I; TR 1736) is the main component of plant extract Aristolochic acids, which are found in various herbal plants of genus Aristolochia and Asarum. Aristolochic acid A significantly reduces both activator protein 1 (AP-1) and NF-κB activities. Aristolochic acid A reduces BLCAP gene expression in human cell lines.
|
-
- HY-16229
-
|
GGTI-2154
|
ROS Kinase
Apoptosis
|
Cancer
|
|
GGTI-2154 is a potent and selective inhibitor of geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 can be used for the research of cancer.
|
-
- HY-16229A
-
|
GGTI-2154 hydrochloride
|
ROS Kinase
Apoptosis
|
Cancer
|
|
GGTI-2154 hydrochloride is a potent and selective inhibitor geranylgeranyltransferase I (GGTase I), with an IC50 of 21 nM. GGTI-2154 hydrochloride shows more than 200-fold selectivity for GGTase I over FTase (IC50=5600 nM). GGTI-2154 hydrochloride can be used for the research of cancer.
|
-
- HY-18964
-
|
MG-101
Calpain inhibitor I; Ac-LLnL-CHO; ALLN
|
Proteasome
Apoptosis
|
Cancer
|
|
MG-101 (ALLN) is an inhibitor of cysteine proteases which inhibits calpain I, calpain II, cathepsin B and cathepsin L with Kis of 190, 220, 150 and 500 pM, respectively. MG-101 induces apoptosis and inhibits tumor growth, it can be used for the research of colon cancer.
|
-
- HY-N10149
-
-
- HY-P3884
-
-
- HY-P99530
-
|
Valanafusp alfa
AGT-181; HIRMAb-IDUA
|
Insulin Receptor
|
Metabolic Disease
|
|
Valanafusp alfa (AGT-181) is a brain penetrating recombinant fusion protein of a chimeric monoclonal antibody against the human insulin receptor (HIR) and human iduronidase (IDUA). Valanafusp alfa can be used for the research of Mucopolysaccharidosis type I (MPS I) .
|
-
- HY-P2972
-
-
- HY-B1359
-
|
Methylene blue trihydrate
C.I. Basic Blue 9 trihydrate
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Parasite
|
Cancer
Infection
Neurological Disease
|
|
Methylene blue trihydrate (C.I. Basic Blue 9 trihydrate) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue trihydrate is a vasopressor and is often used as a dye in several medical procedures. Methylene blue trihydrate has antinociception, antimalarial, antidepressant and anxiolytic activity effects. Methylene Blue trihydrate has the potential for methemoglobinemias, neurodegenerative disorders and ifosfamide-induced encephalopathytreatment.
|
-
- HY-118581
-
|
Coralyne chloride
|
Topoisomerase
|
Cancer
|
|
Coralyne chloride is a protoberberine alkaloid with potent anti-cancer activities. Coralyne chloride acts as a potent topoisomerase I poison and induces Top I mediated DNA cleavage. Coralyne chloride can be used for preparing coralyne derivatives as DNA binding fluorescent probes.
|
-
- HY-12484
-
|
BMH-21
|
DNA/RNA Synthesis
|
Cancer
|
|
BMH-21 is a first-in-class DNA intercalator which inhibits RNA polymerase I (Pol I) transcription. BMH-21 possesses anticancer activity.
|
-
- HY-103559
-
|
HexylHIBO
|
mGluR
|
Neurological Disease
|
|
HexylHIBO is a potent group I mGluR antagonist with Kbs of 140 and 110 μM at mGlu1a and mGlu5a receptors, respectively. HexylHIBO decreased sEPSC in rat.
|
-
- 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-13622A
-
|
Elomotecan
BN 80927 free base
|
Topoisomerase
|
Cancer
|
|
Elomotecan (BN 80927 free base) is a potent inhibitor of topoisomerases I and II. Elomotecan is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II.
|
-
- HY-N3488
-
|
Isodiospyrin
|
Topoisomerase
Bacterial
Fungal
|
Cancer
Infection
|
|
Isodiospyrin, a natural dimeric naphthoquinone, is a human DNA topoisomerase I (Topoisomerase) inhibitor. Isodiospyrin can prevent both DNA relaxation and kinase activities of human topoisomerase I. Isodiospyrin shows anticancer, antibacterial and antifungal activities.
|
-
- HY-13622
-
|
Elomotecan hydrochloride
BN 80927
|
Topoisomerase
|
Cancer
|
|
Elomotecan hydrochloride (BN 80927) is a potent inhibitor of topoisomerases I and II. Elomotecan hydrochloride (BN 80927) is a camptothecin analog belonging to the homocamptothecin family (hCPT). Elomotecan hydrochloride (BN 80927) reduces the proliferation of different tumor cells with higher potency than other anticancer agents of reference targeting topoisomerases I and II.
|
-
- HY-13218
-
|
Acitazanolast
WP-871
|
Others
|
Inflammation/Immunology
|
|
Acitazanolast is an orally active antiallergic agent, can inhibit histamine release. Acitazanolast can be used in study of type I anaphylaxis (immediate) caused by IgE antibodies.
|
-
- HY-145707
-
-
- HY-W010452
-
-
- HY-113378
-
-
- HY-17020A
-
-
- HY-17020
-
-
- HY-148161
-
|
L82-G17
|
DNA/RNA Synthesis
|
Cancer
|
|
L82-G17 is an uncompetitive DNA ligase I (Lig I)-selective inhibitor. L82-G17 inhibits the third step of the ligation reaction, phosphodiester bond formation. L82-G17can be used as a probe of the catalytic activity.
|
-
- HY-12071
-
|
LDN193189
DM-3189
|
TGF-β Receptor
|
Cancer
|
|
LDN193189 is a potent selective BMP type I receptor (BMP I) inhibitor. LDN-193189 efficiently inhibits transcriptional activity of the BMP type I receptors ALK2 and ALK3 with IC50 values of 5 nM and 30 nM, respectively. LDN-193189 can be used for the research of bone morphogenetic protein signalling, such as fibrodysplasia ossificans progressiva.
|
-
- HY-N4104
-
|
Agaric acid
Agaricinic Acid
|
Mitochondrial Metabolism
|
Metabolic Disease
|
|
Agaric acid (Agaricinic Acid) is obtained from various plants of the fungous tribe, i.e. Polyporus officinalis and Polyporus igniarius. Agaric acid induces mitochondrial permeability transition through its interaction with the adenine nucleotide translocase. Agaric acid promotes efflux of accumulated Ca 2+, collapse of transmembrane potential, and mitochondrial swelling. Agaric acid is used to regulate lipid metabolism.
|
-
- HY-111898
-
|
Epirosmanol
|
Others
|
Cancer
|
|
Epirosmanol is a nature diterpene lactone from S. officinalis. Epirosmanol shows anti-cancer activity and inhibits melanin biosynthesis against melanoma cells. Epirosmanol also exhibits DPPH radical scavenging activity.
|
-
- HY-D0983
-
-
- HY-16560
-
-
- HY-13418
-
|
Dorsomorphin dihydrochloride
Compound C dihydrochloride; BML-275 dihydrochloride
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) dihydrochloride is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
|
-
- HY-13418A
-
|
Dorsomorphin
Compound C; BML-275
|
AMPK
TGF-β Receptor
Autophagy
|
Cancer
|
|
Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
|
-
- HY-W010452S1
-
-
- HY-W010452S2
-
-
- HY-145304
-
|
DX3-235
|
Mitochondrial Metabolism
|
Cancer
|
|
DX3-235 is an oxidative phosphorylation (OXPHOS) inhibitor. DX3-235 shows nanomolar inhibition of complex I function and ATP production in a galactose-containing medium resulting in significant cytotoxicity.
|
-
- HY-13611
-
|
Diflomotecan
BN 80915
|
Topoisomerase
|
Cancer
|
|
Diflomotecan (BN 80915) is a potent and orally active inhibitor of topoisomerase I. Diflomotecan (BN 80915) causes enhanced plasma stability and has the superior preclinical anti-tumour activity compared with other established compounds.
|
-
- HY-139202
-
|
XVA143
|
Integrin
|
Inflammation/Immunology
|
|
XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo.
|
-
- HY-116933
-
-
- HY-148820
-
-
- HY-152218
-
|
Clathrin-IN-4
|
Dynamin
|
Neurological Disease
|
|
Clathrin-IN-4 (compound 8b), a Wiskostatin (HY-12534) analogue, is a potent inhibitor of clathrin mediated endocytosis with an IC50 of 2.1 μM. Clathrin-IN-4 is a dynamin I GTPase activity inhibitor with an IC50 of 9.1 μM.
|
-
- HY-D0971
-
|
Pyronin Y
Pyronine G; C.I. 45005
|
DNA Stain
|
Others
|
|
Pyronin Y (Pyronine G) is a cationic dye that intercalates RNA and has been used to target cell structures including RNA, DNA and organelles. Pyronin Y forms fluorescent complexes with double-stranded nucleic acids (especially RNA) enabling semi-quantitative analysis of cellular RNA. Pyronin Y can be used to identify specific RNA subspecies of ribonuclear proteins complexes in live cells. Storage: protect from light.
|
-
- HY-145303
-
-
- HY-134315
-
|
8-Nitroguanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
8-Nitroguanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-N0173
-
|
Cinchonidine
α-Quinidine
|
Serotonin Transporter
Parasite
|
Infection
|
|
Cinchonidine (α-Quinidine) is a cinchona alkaloid found in Cinchona officinalis and Gongronema latifolium. A building block used in asymmetric synthesis in organic chemistry. Weak inhibitor of serotonin transporter (SERT) with Kis of 330, 4.2, 36, 196, 15 μM for dSERT, hSERT, hSERT I172M, hSERT S438T, hSERT Y95F, respectively. Antimalarial activities.
|
-
- HY-154332
-
|
8-(Phenylmethoxy)guanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
8-(Phenylmethoxy)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-137406
-
|
1,2'-O-Dimethylguanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
1,2'-O-Dimethylguanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154506
-
|
N2-Phenoxyacetylguanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
N2-Phenoxyacetylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154361
-
|
TLR7 agonist 13
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
TLR7 agonist 13 is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152430
-
|
8-Hydroxymethyl guanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
8-Hydroxymethyl guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152610
-
|
3′-C-Methylguanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
3′-C-Methylguanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152517
-
|
8-(Methylthio)guanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
8-(Methylthio)guanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152652
-
|
5’(R)-C-Methylguanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
5’(R)-C-Methylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152478
-
|
3’-β-C-Ethynylguanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3’-β-C-Ethynylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-N9251
-
-
- HY-P1630
-
|
Buforin II
|
Bacterial
|
Infection
|
|
Buforin II, derived from buforin I, a protein isolated from the stomach of the Asian toad Bufo bufo gargarizans, is a potent antimicrobial peptide. Buforin II has antimicrobial activity against a broad spectrum of Gram-positive and Gram-negative bacteria.
|
-
- HY-B0825A
-
|
Fenpyroximate
|
Parasite
Mitochondrial Metabolism
|
Infection
|
|
Fenpyroximate is an acaricide and insecticide against many mites and insect pests of agricultural crops and ornamentals. Fenpyroximate is also a strong inhibitor of bovine heart mitochondrial NADH-ubiquinone oxidoreductase (complex I), binds to the ND5 subunit.
|
-
- HY-152216
-
|
Dynamin IN-2
|
Dynamin
|
Neurological Disease
|
|
Dynamin IN-2 (compound 43), a Wiskostatin (HY-12534) analogue, is a potent dynamin inhibitor, with an IC50 of 1.0 μM for dynamin I GTPase. Dynamin IN-2 also blocks clathrin mediated endocytosis (CME), with an IC50 of 9.5 μM.
|
-
- HY-N0822
-
|
Shikonin
C.I. 75535; Isoarnebin 4
|
Chloride Channel
Pyruvate Kinase
NF-κB
TNF Receptor
HIV
AIM2
|
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-154111
-
|
8-(N-Boc-aminomethyl)guanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
8-(N-Boc-aminomethyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152673
-
|
9-(β-D-Xylofuranosyl)guanine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
9-(β-D-Xylofuranosyl)guanine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152742
-
|
8-(N,N-Dimethylaminomethyl)guanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
8-(N,N-Dimethylaminomethyl)guanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-N1068
-
-
- HY-152993
-
|
2′-Deoxy-N-(2-furanylmethyl)guanosine
|
Others
|
Others
|
|
2′-Deoxy-N-(2-furanylmethyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-128139
-
|
2'-C-Methylguanosine
2'-C-beta-Methylguanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
2'-C-Methylguanosine (2'-C-beta-Methylguanosine) is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152991
-
|
6-Deoxo-8-oxo-3’-deoxy-guanosine
|
Others
|
Others
|
|
2′-Deoxy-N-(2-furanylmethyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152493
-
|
3’-O-(2-Methoxyethyl)guanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
3’-O-(2-Methoxyethyl)guanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-18600A
-
-
- HY-18600
-
-
- HY-103660
-
-
- HY-B1229
-
-
- HY-144641
-
-
- HY-144640
-
-
- HY-154482
-
|
N2-iso-Butyroyl-3’-O-methylguanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
N2-iso-Butyroyl-3’-O-methylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154448
-
|
3,5-Bis-O-(2,4-dichlorobenzyl)guanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3,5-Bis-O-(2,4-dichlorobenzyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154336
-
|
N-[2-[4-(1-Methylethyl)phenoxy]acetyl]guanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
N-[2-[4-(1-Methylethyl)phenoxy]acetyl]guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154349
-
|
N2-iso-Butyroyl-2’-O-propargylguanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
N2-iso-Butyroyl-2’-O-propargylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154549
-
|
3’-O-MOE-G(iBu)-2’-phosphoramidite
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3’-O-MOE-G(iBu)-2’-phosphoramidite is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152797
-
|
N4-Desmethyl-N5-Methyl wyosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
N4-Desmethyl-N5-Methyl wyosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154484
-
|
3’-O-Me-G(iBu)-2’-phosphoramidite
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
3’-O-Me-G(iBu)-2’-phosphoramidite is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152684
-
|
2′-O-2-Propyn-1-ylguanosine
|
Nucleoside Antimetabolite/Analog
|
Others
|
|
2′-O-2-Propyn-1-ylguanosine is a guanosine analogue. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-153368
-
-
- HY-101380A
-
-
- HY-116448
-
-
- HY-B2171A
-
|
Carubicin hydrochloride
Carminomycin hydrochloride; Carminomicin I hydrochloride
|
Apoptosis
|
Cancer
Infection
|
|
Carubicin hydrochloride is a microbially-derived compound. Carubicin hydrochloride is an effective inhibitor of VHL-defective (VHL−/−) CCRCC cell proliferation. Carubicin hydrochloride also induces apoptosis by a mechanism independent of p53 or hypoxia-inducible factor HIF2. Carubicin hydrochloride has the potential for the research of cancer diseases.
|
-
- HY-N6798
-
|
Myriocin
Thermozymocidin; ISP-I
|
HCV
Antibiotic
|
Infection
|
|
Myriocin (Thermozymocidin), a fungal metabolite could be isolated from Myriococcum albomyces, Isaria sinclairi and Mycelia sterilia, is a potent inhibitor of serine-palmitoyl-transferase (SPT) and a key enzyme in de novo synthesis of sphingolipids. Myriocin suppresses replication of both the subgenomic HCV-1b replicon and the JFH-1 strain of genotype 2a infectious HCV, with an IC50 of 3.5 µg/mL for inhibiting HCV infection.
|
-
- 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-N0864
-
|
Macranthoidin B
Macranthoiside I
|
Others
|
Cancer
|
|
Macranthoidin B is a major bioactive saponin in rat plasma after oral administration of extraction of saponins from Flos Lonicerae.
|
-
- HY-N6790
-
|
Nonactin
Ammonium ionophore I
|
Potassium Channel
Mitochondrial Metabolism
Bacterial
Influenza Virus
Apoptosis
Antibiotic
|
Cancer
Infection
|
|
Nonactin is a naturally occurring macrotetrolide antibiotic from Streptomyces griseus. Nonactin acts as an ionophore for monovalent cations, including K +, and NH4 +. Nonactin is able to uncouple the oxidative phosphorylation (OXPHOS) of mitochondria. Nonactin selectively induces apoptosis in cell lines harboring active mutant β-catenin. Nonactin inhibits the surface expression of endogenous HSP60.
|
-
- HY-B2171
-
|
Carubicin
Carminomycin; Carminomicin I
|
Apoptosis
|
Cancer
Infection
|
|
Carubicin (Carminomycin) is a microbially-derived compound. Carubicin is an effective inhibitor of VHL-defective (VHL−/−) CCRCC cell proliferation. Carubicin also induces apoptosis by a mechanism independent of p53 or hypoxia-inducible factor HIF2. Carubicin has the potential for the research of cancer diseases.
|
-
- HY-135780
-
-
- HY-144106
-
-
- HY-152988
-
|
N2-iso-Butyroyl-7'-O-DMT-morpholinoguanine
|
Others
|
Others
|
|
N2-iso-Butyroyl-7'-O-DMT-morpholinoguanine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-152992
-
|
7-Cyano-7-deaza-2'-deoxy guanosine
|
Others
|
Others
|
|
7-Cyano-7-deaza-2'-deoxy guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154547
-
|
N2-iso-Butyroyl-3’-O-(methoxyethyl)guanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
N2-iso-Butyroyl-3’-O-(methoxyethyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-141889
-
-
- HY-152545
-
|
N1,N2-Dimethyl-2’-O-methylguanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
N1,N2-Dimethyl-2’-O-methylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154350
-
|
5'-O-DMT-N2-isobutyryl-2'-O-propargylguanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
5'-O-DMT-N2-isobutyryl-2'-O-propargylguanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-154606
-
|
2'-F-2'-ara-N2-ibu-dG Phosphoramidite
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
2'-F-2'-ara-N2-ibu-dG Phosphoramidite is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-W073825
-
|
N2-iso-Butyryl-2'-O-(2-methoxyethyl)guanosine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
N2-iso-Butyryl-2'-O-(2-methoxyethyl)guanosine is a guanosine analog. Some guanosine analogs have immunostimulatory activity. In some animal models, they also induce type I interferons, producing antiviral effects. Studies have shown that the functional activity of guanosine analogs is dependent on the activation of Toll-like receptor 7 (TLR7).
|
-
- HY-115984
-
-
- HY-B1102
-
|
Evans Blue
Direct Blue 53; C.I. 23860
|
EAAT2
|
Others
|
|
Evans Blue is a potent inhibitor of L-glutamate uptake via the membrane bound excitatory amino acid transporter (EAAT).
|
-
- HY-D0932
-
|
Sudan IV
Solvent Red 24; C.I. 26105
|
Fluorescent Dye
|
Others
|
|
Sudan IV is a lysochrome (fat-soluble dye) diazo dye used for the staining of lipids, triglycerides and lipoproteins on frozen paraffin sections.
|
-
- HY-16562
-
|
Irinotecan
(+)-Irinotecan; CPT-11; VAL-413(free base)
|
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex.
|
-
- HY-132827
-
-
- HY-132893
-
-
- HY-18600AS
-
|
Azimilide-d8 dihydrochloride
NE-10064-dd8 (dihydrochloride)
|
Potassium Channel
|
Cardiovascular Disease
|
|
Azimilide-d8 (dihydrochloride) is the deuterium labeled Azimilide dihydrochloride. Azimilide Dihydrochloride (NE-10064 Dihydrochloride) is a class III antiarrhythmic compound, inhibits I(Ks) and I(Kr) in guinea-pig cardiac myocytes and I(Ks) (minK) channels expressed in Xenopus oocytes.
|
-
- HY-154548
-
-
- HY-154507
-
-
- HY-N7269
-
-
- HY-15481
-
-
- HY-146385
-
|
hCAI/II-IN-1
|
Carbonic Anhydrase
|
Cancer
|
|
hCAI/II-IN-1 (Compound 3h) is a human carbonic anhydrase I and II (hCA I/II) inhibitor with IC50 values of 0.047 µM and 0.024 µM against hCA I and hCA II, respectively.
|
-
- HY-N11537
-
-
- HY-N10495
-
|
Seconeolitsine
|
Antibiotic
Bacterial
Topoisomerase
|
Infection
|
|
Seconeolitsine, an antibiotic, and is an inhibitor of targeting topoisomerase I (TopA). Seconeolitsine also is a new antimicrobial agent that can inhibit S. pneumoniae growth. Seconeolitsine can inhibit TopA relaxation activity with an IC50 value of 17 μM. Seconeolitsine can be used for the research of S. pneumoniae infections resistant to other antibiotics.
|
-
- HY-152547
-
-
- HY-154464
-
-
- HY-N7555
-
-
- HY-112275
-
-
- HY-13217
-
|
Vanoxerine dihydrochloride
GBR-12909 dihydrochloride; I893 dihydrochloride
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine dihydrochloride (GBR-12909 dihydrochloride) binds to the target site on the dopamine transporter (DAT).
|
-
- HY-N10181
-
-
- HY-P1934
-
|
Cyclo(Phe-Pro)
Cyclo(phenylalanylprolyl); A-64863
|
HCV
|
Infection
|
|
Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)), a Vibrio vulnificus quorum-sensing molecule, inhibits retinoic acid-inducible gene-I (RIG-I) polyubiquitination, through its specific interaction with RIG-I, to blunt IRF-3 activation and type-I IFN production. Cyclo(Phe-Pro) (Cyclo(phenylalanylprolyl)) enhances susceptibility to hepatitis C virus (HCV), as well as Sendai and influenza viruses.
|
-
- HY-108938
-
|
SDZ285428
|
Cytochrome P450
Fungal
Parasite
|
Infection
|
|
SDZ285428 is a CYP51 inhibitor. SDZ285428 inhibits Trypanosoma cruzi (TC) CYP51 with I/E2 <1 (5 min) and I/E2=9 (1 h). SDZ285428 inhibits Trypanosoma brucei (TB) CYP51 with I/E2 <1 (5 min) and I/E2=35 (1 h).
|
-
- HY-154351
-
-
- HY-154483
-
-
- HY-139170
-
|
CAY10746
|
ROCK
|
Metabolic Disease
|
|
CAY10746 is a selective Rho kinase (ROCK) inhibitor. CAY10746 has inhibitory activity for ROCK I, ROCK II with IC50 values of 0.014 μM and 0.003 μM, respectively. CAY10746 can be used for the research of diabetic retinopathy (DR).
|
-
- HY-144468
-
-
- HY-N7089
-
|
Benzoyleneurea
|
Bacterial
|
Infection
|
|
Benzoyleneurea possesses anti-bacterial activity. Benzoyleneurea scaffold can be used in the synthesis of novel protein geranylgeranyltransferase-I (PGGTase-I) inhibitors.
|
-
- HY-106668
-
|
Isepamicin
Sch 21420
|
Antibiotic
Bacterial
|
Infection
|
|
Isepamicin (Sch 21420) is an aminoglycoside antibacterial. Isepamicin has better activity against strains producing type I 6'-acetyltransferase. Isepamicin’s antibacterial spectrum includes Enterobacteriaceae and staphylococci. Anaerobes, Neisseriaceae and streptococci are resistant. Isepamicin exhibits a strong concentration-dependent bactericidal effect, a long post-antibiotic effect (several hours) and induces adaptive resistance.
|
-
- HY-12598
-
|
(S)-3,5-DHPG
|
mGluR
|
Neurological Disease
|
|
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 µM and 3.9 µM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.
|
-
- HY-145483
-
-
- HY-N1013
-
-
- HY-W008719
-
|
MPP+ iodide
|
Mitochondrial Metabolism
|
Neurological Disease
|
|
MPP+ iodide, a toxic metabolite of the neurotoxin MPTP, causes symptom of Parkinson's disease in animal models by selectively destroying dopaminergic neurons in substantia nigra. MPP+ iodide is taken up by the dopamine transporter into dopaminergic neurons where it exerts its neurotoxic action on mitochondria by affecting complex I of the respiratory chain. MPP+ iodide is also a high affinity substrate for the serotonin transporter (SERT).
|
-
- HY-138746
-
|
EGFR-IN-15
|
EGFR
|
Cancer
|
|
EGFR-IN-15 (compound I-005) is a EGFR inhibitor with an IC50 of 4 nM. EGFR-IN-15 can be used for oncological diseases research.
|
-
- HY-19990
-
-
- HY-144466
-
-
- HY-100530B
-
-
- HY-100530C
-
-
- HY-13456
-
|
LY-404187
|
iGluR
|
Neurological Disease
|
|
LY-404187 is a potent, selective and centrally active positive allosteric modulator of AMPA receptors, with the EC50s of 5.65, 0.15, 1.44, 1.66 and 0.21 µM for GluR1i, GluR2i, GluR2o, GluR3i and GluR4i, respectively. LY-404187 has therapeutic potential in a number of psychiatric disorders and neurodegenerative diseases.
|
-
- HY-147135
-
|
TEAD-IN-3
|
YAP
|
Cancer
|
|
TEAD-IN-3 (compound I-177) is a potent TEAD transcription factor inhibitor. TEAD-IN-3 can be used for the research of proliferative diseases (such as cancer) .
|
-
- HY-139316
-
-
- HY-145587
-
-
- HY-123052
-
-
- HY-B0817
-
|
Pyridaben
|
Parasite
|
Infection
|
|
Pyridaben is a mitochondrial electron transport inhibitor (METI) acaricide that promotes the formation of damaging oxygen and nitrogen radicals. Pyridaben selectively inhibits complex I (NADH dehydrogenase) with an IC50 value of 2.4 nM (assay sites: rat liver and bovine heart mitochondria). Pyridaben also significantly inhibits rat mitochondrial mtNOS function.
|
-
- HY-112037
-
|
IACS-010759
IACS-10759
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 is an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 inhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 has the potential for relapsed/refractory AML and solid tumors research.
|
-
- HY-N3741
-
|
Didrovaltrate
Didrovaltratum
|
Others
|
Cancer
|
|
Didrovaltrate (Didrovaltratum) can be isolated from the roots of Valeriana wallichii D.C. Didrovaltrate is an antitumor agent with cytotoxicity.
|
-
- HY-N0718
-
-
- HY-110005
-
-
- HY-W008343
-
|
1,3-Dimethyluracil
|
Endogenous Metabolite
|
Metabolic Disease
|
|
1,3-Dimethyluracil is a pyrimidone derives from a uracil. 1,3-Dimethyluracil found occasionally in human urine. 1,3-Dimethyluracil shows inhibition activity against hCA I and hCA II (human carbonic anhydrase) with Ki of 316.2 μM and 166.4 μM, respectively.
|
-
- HY-N6621
-
|
Hippeastrine
|
Topoisomerase
|
Cancer
|
|
Hippeastrine, an active alkaloid, exhibits a good dose-dependent inhibitory effect against topoisomerase I (Top I) with an IC50 at 7.25 μg/mL. Antiproliferative and anticancer activities.
|
-
- HY-145107
-
-
- HY-10257
-
-
- HY-136150
-
|
Methyl carnosate
|
Bacterial
|
Infection
|
|
Methyl camosate is a diterpene isolated from Salvia officinalis or Rosmarinus officinalis. Methyl camosate has potent antioxidant and anti-bacterial activity.
|
-
- HY-N7938
-
-
- HY-N3710
-
|
Dehydrocrenatidine
Kumujian G; O-Methylpicrasidine I
|
JAK
Apoptosis
|
Cancer
Neurological Disease
|
Dehydrocrenatidine, a natural alkaloid, is a specific JAK inhibitor. Dehydrocrenatidine inhibits voltage-gated sodium channels and ameliorates mechanic allodia in a rat model of neuropathic pain.
|
-
- HY-10324
-
-
- HY-13960
-
-
- HY-112037A
-
|
IACS-010759 hydrochloride
IACS-10759 hydrochloride
|
Mitochondrial Metabolism
Apoptosis
|
Cancer
|
|
IACS-010759 hydrochlorideis an orally active, potent mitochondrial complex I of oxidative phosphorylation (OXPHOS) inhibitor. IACS-010759 hydrochlorideinhibits proliferation and induces apoptosis in models of brain cancer and acute myeloid leukemia (AML) reliant on OXPHOS. IACS-010759 hydrochloride has the potential for relapsed/refractory AML and solid tumors research.
|
-
- HY-10432
-
|
A 83-01
|
TGF-β Receptor
|
Cancer
|
|
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-16562S1
-
-
- HY-142518
-
|
EGFR-IN-26
|
VEGFR
|
Cancer
|
|
EGFR-IN-26 is a EGFR inhibitor extracted from patent WO2019162323A1 compound I-028. EGFR-IN-26 can be used for the research of cancer.
|
-
- HY-16562S
-
|
Irinotecan-d10
(+)-Irinotecan-d10; CPT-11-d10; VAL-413-d10
|
Topoisomerase
Autophagy
|
Cancer
|
|
Irinotecan-d10 is a deuterium labeled Irinotecan ((+)-Irinotecan). Irinotecan ((+)-Irinotecan) is a topoisomerase I inhibitor, preventing religation of the DNA strand by binding to topoisomerase I-DNA complex[1].
|
-
- HY-15871
-
|
GGTI298 Trifluoroacetate
|
Ras
Apoptosis
|
Cancer
|
|
GGTI298 Trifluoroacetate is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, which can inhibit Rap1A with IC50 of 3 μM; little effect on Ha-Ras with IC50 of >20 μM.
|
-
- HY-101692
-
-
- HY-N2063
-
-
- HY-W008820
-
|
Glutaric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I.
|
-
- HY-148099
-
|
USP1-IN-2
|
Deubiquitinase
|
Cancer
|
|
USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of less than about 50 nM.
|
-
- HY-131334
-
|
AMPK activator 4
|
AMPK
|
Metabolic Disease
|
|
AMPK activator 4 is a potent AMPK activator without inhibition of mitochondrial complex I. AMPK activator 4 selectively activates AMPK in the muscle tissues. AMPK activator 4 dose-dependently improves glucose tolerance in normal mice, and significantly lowers fasting blood glucose level and ameliorates insulin resistance in db/db diabetic mice. Anti-hyperglycemic effect.
|
-
- HY-D0256
-
|
Direct Black 38
Chlorazol Black E; Ferristatin II disodium; C.I. 30235
|
DNA/RNA Synthesis
|
Others
|
|
Direct Black 38 (Chlorazol Black E) is an azo dye. Direct Black 38 induces unscheduled DNA synthesis in liver and micronucleus in bone marrow of rats in vivo. Storage: protect from light.
|
-
- HY-148094
-
-
- HY-150545
-
-
- HY-113970A
-
|
Nebracetam hydrochloride
WEB 1881 FU hydrochloride
|
mAChR
|
Neurological Disease
|
|
Nebracetam hydrochloride, a nootropic M1-muscarinic agonist, induces a rise of intracellular Ca 2+ concentration. Nebracetam hydrochloride exhibits an EC50 of 1.59 mM for elevating [Ca 2+]i.
|
-
- HY-N6661
-
|
Verbenone
(-)-Verbenone
|
Others
|
Infection
|
|
Verbenone ((-)-Verbenone) is a natural terpene in leaves of the tree, Verbena officinalis. Verbenone has anti-aggregation pheromone and interrupts the attraction of bark beetles to their aggregation pheromones.
|
-
- HY-16231
-
|
GGTI-2418
|
ROS Kinase
Apoptosis
|
Cancer
|
|
GGTI-2418 is a highly potent, competitive, and selective geranylgeranyltransferase I (GGTase I) inhibitor. GGTI-2418 inhibits GGTase I and FTase activities with IC50s of 9.5 nM and 53 μM, respectively. GGTI-2418 also increases p27(Kip1) and induces significant regression of breast tumors.
|
-
- HY-W062216
-
|
2-Aminoimidazole
|
Bacterial
Arginase
|
Infection
|
|
2-Aminoimidazole is a potent antibiofilm agent that can be used as an adjuvant to antimicrobial. 2-aminoimidazoles disrupts the ability of bacteria to protect themselves by inhibiting biofilm formation and genetically-encoded antibiotic resistance traits. 2-Aminoimidazole is also a weak noncompetitive inhibitor of human arginase I with a Ki of 3.6 mM.
|
-
- HY-14821
-
-
- HY-U00232
-
-
- HY-148095
-
-
- HY-15466
-
|
Izorlisib
CH5132799
|
PI3K
|
Cancer
|
|
Izorlisib (CH5132799) is a selective class I PI3K inhibitor. Izorlisib inhibits class I PI3Ks, particularly PI3Kα, with an IC50 of 14 nM.
|
-
- HY-152244
-
|
PARP7-IN-14
|
PARP
|
Cancer
|
|
PARP7-IN-14 (I-1) is a potent and selective PARP7 inhibitor with an IC50 value of 7.6 nM. PARP7-IN-14 has anticancer activity.
|
-
- HY-125930A
-
|
T-2513 hydrochloride
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
T-2513 hydrochloride is a selective topoisomerase I inhibitor. T-2513 hydrochloride binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
|
-
- HY-125930
-
|
T-2513
|
Topoisomerase
DNA/RNA Synthesis
|
Cancer
|
|
T-2513 is a selective topoisomerase I inhibitor. T-2513 binds covalently to and stabilizes the topoisomerase I-DNA complex and inhibits DNA replication and RNA synthesis, ultimately leading to cell death.
|
-
- HY-147107
-
|
OfHex1-IN-2
|
Others
|
Others
|
|
OfHex1-IN-2 (compound I-79) is a potent β-N-acetylhexosaminidase OfHex1 inhibitor. OfHex1-IN-2 can be used in control of insect.
|
-
- HY-100876
-
|
GGTI298
|
Ras
Apoptosis
|
Cancer
|
|
GGTI298 is a CAAZ peptidomimetic geranylgeranyltransferase I (GGTase I) inhibitor, strongly inhibiting the processing of geranylgeranylated Rap1A with little effect on processing of farnesylated Ha-Ras, with IC50 values of 3 and > 20 μM in vivo, respectively.
|
-
- HY-112197
-
-
- HY-E70008
-
|
Lumbokinase capsules
|
Sirtuin
|
Inflammation/Immunology
|
|
Lumbokinase capsules attenuates myocardial ischemia-reperfusion (I-R) injury through the activation of Sirt1 signaling, and thus enhances autophagic flux and reduces I-R-induced oxidative damage, inflammation and apoptosis.
|
-
- HY-143545
-
|
RET-IN-8
|
RET
|
Cancer
|
|
RET-IN-8 is a rearranged during transfection (RET) kinase inhibitor extracted from patent WO2021093720A1 compound I-1. RET-IN-8 can be used for the research of cancer.
|
-
- HY-19825
-
|
Rebeccamycin
|
Topoisomerase
ADC Cytotoxin
Antibiotic
|
Cancer
|
|
Rebeccamycin, an antitumor antibiotic, inhibits DNA topoisomerase I. Rebeccamycin appears to exert its primary antineoplastic effect by poisoning topoisomerase I and has negligible effect on protein kinase C and topoisomerase II.
|
-
- HY-107578
-
|
Macbecin
Macbecin I; NSC 330499
|
HSP
|
Cancer
|
|
Macbecin is a stable HSP90 inhibitor by binding to the ATP-binding site with an IC50 of 2 μM and a Kd of 0.24 μM. Macbecin exhibits antitumor and cytocidal activities.
|
-
- 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-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-13217A
-
|
Vanoxerine
GBR 12909; I893
|
Dopamine Transporter
|
Neurological Disease
|
|
Vanoxerine (GBR-12909) is a competitive, potent, and highly selective dopamine reuptake inhibitor (Ki=1 nM). Vanoxerine (GBR-12909) binds to the target site on the dopamine transporter (DAT).
|
-
- HY-N10791
-
|
Neobritannilactone B
|
Others
|
Infection
|
|
Neobritannilactone B, a sesquiterpene, can be isolated from the chloroform fraction of the I. britannica. Neobritannilactone B is cytotoxic. Other extracts of I. britannica are also Dihydrofolate reductase (DHFR) inhibitors, which inhibit Shigella dysenteriae type 1.
|
-
- HY-P2983
-
-
- HY-19332
-
|
Kifunensine
FR-900494
|
Others
|
Inflammation/Immunology
|
|
Kifunensine, a potent and selective inhibitor of class I α-mannosidases isolated from Actinomycete, prevents α-mannosidases I from trimming mannose residues on glycoproteins. Kifunensine inhibits ERAD.
|
-
- HY-15320
-
-
- HY-139315
-
|
PROTAC IRAK4 degrader-4
|
PROTACs
IRAK
|
Cancer
|
|
PROTAC IRAK4 degrader-4 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-127.
|
-
- HY-128829
-
-
- HY-107593
-
|
PS-1145 dihydrochloride
|
IKK
|
Inflammation/Immunology
|
|
PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats.
|
-
- HY-139317
-
|
PROTAC IRAK4 degrader-6
|
PROTACs
IRAK
|
Cancer
|
|
PROTAC IRAK4 degrader-6 is a Cereblon-based PROTAC as interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1, compound I-172.
|
-
- HY-W008820S
-
|
Glutaric acid-d6
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Glutaric acid-d6 is the deuterium labeled Glutaric acid. Glutaric acid is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
|
-
- HY-N4165
-
|
Arnidiol
|
Others
|
Others
|
|
Arnidiol is a pentacyclic triterpene isolated from Barleria Longiflora Linn F..
|
-
- HY-D0256A
-
-
- HY-113133
-
|
Kojibiose
|
Glucosidase
|
Infection
Metabolic Disease
Inflammation/Immunology
|
|
Kojibiose, an orally active prebiotic disaccharide, can specifically inhibit the activity of α-glucosidase I. kojibiose is a proliferation factor for Bifidobacterium, lactic acid bacteria, and eubacteria. kojibiose is a low-calorie sweetener capable of increasing the absorption of iron. Kojibiose exhibits antitoxic activity. Kojibiose reduces hepatic expression of inflammatory markers in vivo.
|
-
- HY-14812
-
-
- HY-U00159
-
-
- HY-13768A
-
-
- HY-N5028
-
-
- HY-N10115
-
-
- HY-105661
-
-
- HY-B0483
-
-
- HY-P0030
-
-
- HY-146115
-
|
TRK-IN-19
|
Trk Receptor
|
Cancer
|
|
TRK-IN-19 (Compound I-10 ) is a potent inhibitor of TRK (TRKA IC50 = 1.1 nM, TRKA G595R IC50 = 5.3 nM). TRK-IN-19 has the potential for the research of cancer diseases.
|
-
- HY-145046
-
|
SOS1-IN-3
|
Ras
|
Cancer
|
|
SOS1-IN-3 is a potent SOS1 (son of sevenless homolog 1) inhibitor with an IC50 of 5 nM. SOS1-IN-3 has anticancer effects (WO2019122129A1; compound I-1).
|
-
- HY-147093
-
|
vc-PAB-DMEA-PNU159682
|
ADC Linker
|
Cancer
|
|
vc-PAB-DMEA-PNU159682 (compound I.47) can be used to synthesize the ADC molecule based on Sulfomaleimide-based Linker. vc-PAB-DMEA-PNU159682 has good serum stability.
|
-
- HY-50856S
-
|
Deuruxolitinib
CTP-543; Ruxolitinib d8; Deuterated Ruxolitinib
|
JAK
|
Inflammation/Immunology
|
|
Deuruxolitinib, a deuterated Ruxolitinib (HY-50856), modulates the activity of JAK1/JAK2. Deuruxolitinib can be used for the research hair loss disorders (from patent WO2017192905A1, compound I).
|
-
- HY-12071G
-
|
LDN193189
DM-3189
|
TGF-β Receptor
|
Cancer
|
|
LDN193189 (DM-3189) (GMP) is LDN193189 (HY-12071) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. LDN193189 is selective BMP type I receptor inhibitor.
|
-
- HY-N8054
-
-
- HY-75161
-
|
(-)-Menthol
|
TRP Channel
Endogenous Metabolite
|
Cancer
|
|
(-)-Menthol is a key component of peppermint oil that binds and activates transient receptor potential melastatin 8 (TRPM8), a Ca 2+-permeable nonselective cation channel, to increase [Ca 2+]i. Antitumor activity.
|
-
- HY-U00432
-
-
- HY-18008
-
-
- HY-13566A
-
-
- HY-W008820S2
-
|
Glutaric acid-d2
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Glutaric acid-d2 is the deuterium labeled Glutaric acid. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
|
-
- HY-W008820S1
-
|
Glutaric acid-d4
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Glutaric acid-d4 is the deuterium labeled Glutaric acid. Glutaric acid, C5 dicarboxylic acid, is an intermediate during the catabolic pathways of lysine and tryptophan. Glutaric acid affects pericyte contractility and migration. Glutaric acid is an indicator of glutaric aciduria type I[1][2][3].
|
-
- HY-13686
-
|
PQ401
|
IGF-1R
Apoptosis
|
Cancer
|
|
PQ401 is a potent inhibitor of IGF-IR signaling. PQ401 inhibits IGF-I-stimulated IGF-IR autophosphorylation with an IC50 of 12.0 μM in a series of studies in MCF-7 cells. PQ401 is effective at inhibiting IGF-I-stimulated growth of MCF-7 cells (IC50, 6 μM). PQ401 is a potential agent for breast and other IGF-I-sensitive cancers. PQ401 induces caspase-mediated apoptosis.
|
-
- HY-110243
-
|
CAIX Inhibitor S4
|
Carbonic Anhydrase
|
Cancer
|
|
CAIX Inhibitor S4 is a potent and selective inhibitor of carbonic anhydrase IX/XII (CA IX/XII), with a Ki of 7 nM and 2 nM, respectively. CAIX Inhibitor S4 also inhibits CA II and CA I (Ki=546 and 5600 nM, respectively). CAIX Inhibitor S4 can inhibit the number of lung metastasis in orthotopic MDA-MB-231 mouse model without affecting primary tumor growth.
|
-
- HY-N0510A
-
|
Aristolochic acid sodium salt
Aristolochic acid I sodium; TR 1736 sodium; Sodium aristolochate
|
Biochemical Assay Reagents
|
Others
|
|
Aristolochic acid sodium salt (Sodium aristolate 1) is a component of some Chinese herbal medicines and is responsible for nephrotoxicity. It is a proagent that is activated by reduction of nitro groups to amines, resulting in the formation of cytotoxic DNA adducts.
|
-
- HY-100904
-
-
- HY-B1416A
-
-
- HY-15588
-
|
L189
|
DNA/RNA Synthesis
|
Cancer
|
|
L189 is a DNA ligase inhibitor. L189 has inhibition effect for DNA Ligase I, III and IV with IC50 values of 5 μM, 9 μM and 5 μM, respectively. L189 has no cytotoxicity and individually increase cell death. L189 can be used for the research of cancer.
|
-
- HY-16228
-
-
- HY-16568
-
-
- HY-100052
-
-
- HY-147829
-
|
hCAXII-IN-2
|
Carbonic Anhydrase
|
Cancer
|
|
hCAXII-IN-2 (compound 5i) is a potent human carbonic anhydrase XII (hCA XII) and hCA IX inhibitor with Ki values of 84.2 nM and 268.5 nM, respectively. hCAXII-IN-2 shows less active against hCA I and hCA II.
|
-
- HY-143766
-
|
Cap-dependent endonuclease-IN-13
|
Influenza Virus
|
Infection
|
|
Cap-dependent endonuclease-IN-13 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-13 has the potential for the research of influenza virus infection (only influenza A) (extracted from patent WO2021180147A1, compound I-1).
|
-
- HY-114147
-
-
- HY-143752
-
|
Cap-dependent endonuclease-IN-8
|
Influenza Virus
|
Infection
|
|
Cap-dependent endonuclease-IN-8 is a potent inhibitor of cap-dependent endonuclease (CEN). Cap-dependent endonuclease-IN-8 inhibits replication of orthomyxoviruses (including influenza A, influenza B and influenza C) (extracted from patent CN111410661A, compound I-196).
|
-
- HY-136546
-
|
Stafia-1
|
STAT
|
Cancer
|
|
Stafia-1 is a potent STAT5a inhibitor (K i=10.9 μM, IC50=22.2 μM). Stafia-1 displays high selectivity over STAT5b and other STAT family members.
|
-
- HY-123159
-
|
AKI603
|
Aurora Kinase
|
Cancer
|
|
AKI603 is an inhibitor of Aurora kinase A (AurA), with an IC50 of 12.3 nM. AKI603 is developed to overcome resistance mediated by BCR-ABL-T315I mutation. AKI603 exhibits strong anti-proliferative activity in leukemic cells.
|
-
- HY-N0925
-
|
Tetrahydroberberine
Canadine
|
Dopamine Receptor
|
Neurological Disease
|
|
Tetrahydroberberine is an isoquinoline alkaloid isolated from corydalis tuber; has micromolar affinity for dopamine D(2) (pK(i) = 6.08) and 5-HT(1A) (pK(i) = 5.38) receptors but moderate to no affinity for other relevant serotonin receptors (5-HT(1B), 5-HT(1D), 5-HT(3), and 5-HT(4); pK(i) < 5.00).
|
-
- HY-D0914
-
-
- HY-100904A
-
-
- HY-147037
-
|
AMPK activator 7
|
AMPK
|
Metabolic Disease
Cardiovascular Disease
|
|
AMPK activator 7 (compound I-3-24) is a an AMPK activator with the EC50 of 8.8 nM. AMPK activator 7 can be used for the research of diseases involving AMPK, particularly diseases such as type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia and/or hypertension.
|
-
- HY-16259
-
-
- HY-100486
-
|
BTTAA
|
Others
|
Others
|
|
BTTAA is a Cu(I)-stabilizing ligand, whch performs potently with ubiquitin Glu18AzF.
|
-
- HY-18350
-
-
- HY-B0788A
-
-
- HY-13758
-
-
- HY-P1445
-
-
- HY-N3181
-
|
Nodosin
|
Others
|
Others
|
|
Nodosin is a diterpenoid isolated from Isodon trichocarpus Kudo and I. Japonicus HARA.
|
-
- HY-B0788
-
|
LY2409881
|
IKK
|
Cancer
|
|
LY2409881 is a selective IκB kinase β (IKK2) inhibitor with an IC50 of 30 nM.
|
-
- HY-N6905
-
-
- HY-13758A
-
-
- HY-148819
-
-
- HY-P1366
-
|
des-Gln14-Ghrelin
|
GHSR
|
Metabolic Disease
|
|
des-Gln14-Ghrelin is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
|
-
- HY-130515
-
|
Cdc7-IN-3
|
CDK
|
Cancer
|
|
Cdc7-IN-3 (compound I-A) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-146094
-
|
Antitumor agent-63
|
Topoisomerase
|
Cancer
|
|
Antitumor agent-63 (Compound 40), a 20 (S)-O-linked camptothecin (CPT) glycoconjugate, is an antitumor agent without toxicity towards normal cells. Antitumor agent-63 shows high stability and very weak direct topoisomerase I (Topo I) inhibition.
|
-
- HY-144310
-
|
DX3-213B
|
Mitochondrial Metabolism
|
Cancer
|
|
DX3-213B is a highly potent, orally active oxidative phosphorylation (OXPHOS) complex I inhibitor (IC50=3.6 nM). DX3-213B impairs ATP generation (IC50=11 nM), and blocks MIA PaCa-2 cell growth (GI50=11 nM). DX3-213B is used for the research of the pancreatic cancer.
|
-
- HY-130516
-
|
Cdc7-IN-4
|
CDK
|
Cancer
|
|
Cdc7-IN-4 (compound I-C) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-C. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-115999
-
|
Carbonic anhydrase inhibitor 12
|
Carbonic Anhydrase
|
Cancer
|
|
Carbonic anhydrase inhibitor 12 is a potent CA II inhibitor, also has inhibitory activity in CA I (Kis of 1.72 and 271 nM in CA II and CA I, respectively). Carbonic anhydrase inhibitor 12 has potent anticancer activity against different cancer cell lines.
|
-
- HY-149036
-
-
- HY-130517
-
|
Cdc7-IN-5
|
CDK
|
Cancer
|
|
Cdc7-IN-5 (compound I-B) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-B. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-P1366A
-
|
des-Gln14-Ghrelin TFA
|
GHSR
|
Metabolic Disease
|
|
des-Gln14-Ghrelin TFA is a second endogenous ligand for the growth hormone secretagogue receptor. a). des-Gln14-ghrelin potently induces increases in [Ca 2+]i in CHO-GHSR62 cells, with an EC50 of 2.4 nM.
|
-
- HY-130519
-
|
Cdc7-IN-7
|
CDK
|
Cancer
|
|
Cdc7-IN-7 (compound I-E) is a potent Cdc7 kinase inhibitor extracted from patent WO2019165473A1, compound I-E. Cdc7 is a serine-threonine protein kinase enzyme which is essential for the initiation of DNA replication in the cell cycle.
|
-
- HY-139833
-
-
- HY-151472
-
|
hCAIX/XII-IN-6
|
Carbonic Anhydrase
|
Infection
|
|
hCAIX/XII-IN-6 is an orally active carbonic anhydrase (CA) inhibitor. hCAIX/XII-IN-6 inhibits human CA isoforms hCA I, II, IV, IX, and XII with Ki values of 6697 nM, 2950 nM, 4093 nM, 4.1 nM and 7.7 nM, respectively. hCAIX/XII-IN-6 can be used for the research of rheumatoid arthritis (RA).
|
-
- HY-145080
-
|
Dynole 2−24
|
Dynamin
|
Neurological Disease
|
|
Dynole 2−24 is an indole-based dynamin GTPase inhibitor (IC50=0.56 μM for dynamin I). Dynole 2−24 is nontoxic and shows increased potency against dynamin I and II in vitro and in cells (IC₅₀(CME)=1.9 μM). Dynole 2−24 also shows 4.4-fold selectivity for dynamin I. Dynole 2−24 is active in-cell inhibitor of clathrin-mediated endocytosis. CME: Clathrin mediated endocytosis
|
-
- HY-P9913
-
-
- HY-W040226
-
|
Indigo carmine
Indigotindisulfonate sodium; C.I.Acid Blue 74
|
Fluorescent Dye
|
Cancer
|
|
Indigo carmine is an efficient reagent for the determination of ozone by chemlluminescence (CL).
|
-
- HY-139254
-
|
Indirubin-3′-oxime
IDR3O; I3O
|
CDK
GSK-3
JNK
|
Neurological Disease
|
|
Indirubin-3′-oxime (IDR3O), a synthetic derivative of indirubin, is a potent inhibitor of cyclin-dependent kinases (CDKs) and glycogen synthase kinase 3β (GSK3β). Indirubin-3′-oxime directly inhibits the activity of all three isoforms of JNK (JNK1, JNK2, and JNK3), with IC50s of 0.8 μM, 1.4 μM, and 1.0 μM, respectively. Indirubin-3′-oxime can enhance height growth via activation of Wnt/β-catenin signaling in chondrocytes.
|
-
- HY-15508
-
|
JANEX-1
WHI-P131; Jak3 inhibitor I
|
JAK
|
Cancer
|
|
JANEX-1 (WHI-P131) is a potent and specific JAK3 inhibitor (estimated Ki=2.3 μM). JANEX-1 (WHI-P131) shows potent JAK3-inhibitory activity (IC50 of 78 μM), does not inhibit JAK1 and JAK2.
|
-
- HY-145350
-
-
- HY-16273A
-
-
- HY-W015346
-
-
- HY-13618
-
|
Edotecarin
J 107088; PF 804950
|
Topoisomerase
|
Cancer
|
|
Edotecarin is a potent inhibitor of topoisomerase I that can induces single-strand DNA cleavage, with IC50 of 50 nM.
|
-
- HY-128946
-
|
CL2A-SN-38
|
Drug-Linker Conjugates for ADC
|
Cancer
Inflammation/Immunology
|
|
CL2A-SN-38 is a agent-linker conjugate composed of a potent a DNA Topoisomerase I inhibitor SN-38 and a linker CL2A to make antibody agent conjugate (ADC). CL2A-SN-38 provides significant and specific antitumor effects against a range of human solid tumor types. CL2A-SN-38 uses hydrolyzable linker to deliver active agents within tumor cells and in the tumor microenvironment, resulting in bystander effects.
|
-
- HY-N8347
-
|
Dalbergin
|
Others
|
Others
|
|
Dalbergin is a composition of the extract from the Dalbergia Sissoo Linn. knot wood. Dalbergin demonstrats notable antioxidant ability.
|
-
- HY-119748
-
-
- HY-131108
-
-
- HY-N1390
-
|
Syringaldehyde
|
COX
|
Metabolic Disease
Inflammation/Immunology
|
|
Syringaldehyde is a polyphenolic compound belonging to the group of flavonoids and is found in different plant species like Manihot esculenta and Magnolia officinalis. Syringaldehyde moderately inhibits COX-2 activity with an IC50 of 3.5 μg/mL. Anti-hyperglycemic and anti-inflammatory activities.
|
-
- HY-13565
-
|
Becatecarin
NSC 655649; BMS 181176; BMY 27557
|
Topoisomerase
|
Cancer
|
|
Becatecarin is a rebeccamycin analog with antitumor effects. Becatecarin intercalates into DNA and inhibites the catalytic activity of topoisomerases I/II.
|
-
- HY-N2331
-
-
- HY-134864
-
-
- HY-151565
-
-
- HY-16562A
-
-
- HY-N0275
-
-
- HY-105713
-
|
Sulochrin
|
Bacterial
|
Infection
|
|
Sulochrin is a metabolite produced by Aspergillus terreus var. aureus. I. Sulochrin has antimicrobial activities.
|
-
- HY-101954A
-
|
Inarigivir ammonium
ORI-9020 ammonium; SB-9000 ammonium
|
HBV
|
Infection
Inflammation/Immunology
|
|
Inarigivir (ORI-9020) ammonium is a dinucleotide antiviral drug that can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir (ORI-9020) ammonium acts as a RIG-I (Retinoic acid-inducible gene-I) agonist to activate cellular innate immune responses.
|
-
- HY-144452
-
|
Immunoproteasome inhibitor 1
|
Proteasome
|
Cancer
|
|
Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases.
|
-
- HY-153008
-
|
BCR-ABL-IN-7
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-7 (compound 4) is a WT and T315I mutant ABL kinases inhibitor. BCR-ABL-IN-7 effectively inhibits activities of WT and T315I mutant ABL kinases. BCR-ABL-IN-7 can be used for the research of chronic myeloid leukemia (CML) research.
|
-
- HY-N2015
-
-
- HY-P1533
-
-
- HY-P2285
-
-
- HY-U00314
-
-
- HY-100309
-
-
- HY-15775
-
-
- HY-12777
-
-
- HY-14394
-
|
TBB
NSC 231634; Casein Kinase II Inhibitor I
|
Casein Kinase
|
Cancer
|
|
TBB is a cell-permeable and ATP-competitive CK2 inhibitor with an IC50 of 0.15 μM for rat liver CK2.
|
-
- HY-147922
-
|
hCAI/II-IN-2
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
|
hCAI/II-IN-2 (compound 2b) is a potent dual hCA I/II inhibitor with Ki values of 40.97, 15.15 and 61.88 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-2 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
|
-
- HY-147923
-
|
hCAI/II-IN-3
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
|
hCAI/II-IN-3 (compound 5b) is a potent dual hCA I/II inhibitor with Ki values of 51.25, 13.15 and 42.18 nM for hCA I, hCA II and hCA Ⅸ. hCAI/II-IN-3 possesses anti-hypoxic activity against acute mountain sickness (AMS) and low cellular activity.
|
-
- HY-147414
-
|
Vamotinib
PF-114
|
Bcr-Abl
|
Cancer
|
|
Vamotinib (PF-114) is a potent, selective and orally active tyrosine kinase inhibitor. Vamotinib inhibits the autophosphorylation of BCR/ABL and BCR/ABL-T315I. Vamotinib induces apoptosis. Vamotinib shows anti-proliferative and anti-tumor activity. Vamotinib has the potential for the research of resistant philadelphia chromosome-positive (Ph+) leukemia.
|
-
- HY-125817
-
|
BI-3406
|
Ras
p38 MAPK
|
Cancer
|
|
BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC50 of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity.
|
-
- HY-13012
-
|
RepSox
E-616452; SJN 2511
|
TGF-β Receptor
|
Metabolic Disease
|
|
RepSox (E-616452) is a potent and selective transforming growth factor-beta receptor I/activin like kinase 5 (TGF-β-RI/ALK5) inhibitor. RepSox inhibits ALK5 autophosphorylation with an IC50 value of 4 nM. RepSox can be used for the research of obesity and associated metabolic diseases such as type 2 diabetes.
|
-
- HY-B0063
-
|
Gimatecan
ST1481
|
Topoisomerase
|
Cancer
|
|
Gimatecan (ST1481) is a potent topoisomerase I inhibitor. Gimatecan is an orally bioavailable camptothecin analogue with antitumor activity.
|
-
- HY-W052011
-
|
Ruzinurad
HR011303
|
URAT1
|
Metabolic Disease
|
|
Ruzinurad is a highly selective URATl inhibitor (WO2020088641, compound I). Ruzinurad can be used in the study of hyperuricemia.
|
-
- HY-118091B
-
|
LY300503
|
Others
|
Others
|
|
LY300503 is an enantiomer of LY191704. LY191704 is a human type I 5α-reductase inhibitor.
|
-
- 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-15144
-
|
Trichostatin A
TSA
|
HDAC
|
Cancer
|
|
Trichostatin A (TSA) is a potent and specific inhibitor of HDAC class I/II, with an IC50 value of 1.8 nM for HDAC.
|
-
- HY-N8469
-
-
- HY-100495
-
-
- HY-12075
-
-
- HY-P99509
-
-
- HY-13226
-
|
Galunisertib
LY2157299
|
TGF-β Receptor
|
Cancer
|
|
Galunisertib (LY2157299) is an oral and selective TGF-β receptor type I (TGF-βRI) kinase inhibitor with an IC50 of 56 nM.
|
-
- HY-152157
-
|
HIV-1 inhibitor-52
|
HIV
|
Infection
|
|
HIV-1 inhibitor-52 is a potent broad-spectrum HIV-1 activity inhibitor with EC50s of 1.6 nM-6.4 nM for WT HIV-1, HIV-1 V370A, HIV-1 ΔV370, HIV-1 V362I/V370A, HIV-1 T332S/V362I/prR41G, HIV-1 A326T/V362I/V370A, HIV-1 R361K/V362I/L363M.
|
-
- HY-N7604
-
-
- HY-145424
-
|
CDK7-IN-10
|
CDK
|
Others
|
|
CDK7-IN-10 is a CDK7 inhibitor with an IC50 of less than 100 nM, extracted from patent WO2021016388A1, compound I-1. CDK7-IN-10 is useful in inhibiting the activity of a kinase. CDK7-IN-10 has the potential of inhibiting cell growth and inducing cell apoptosis.
|
-
- HY-N4237
-
|
Saikogenin D
|
Prostaglandin Receptor
Potassium Channel
|
Inflammation/Immunology
|
|
Saikogenin D is isolated from Bupleurum chinense, has anti-inflammatory effects. Saikogenin D activates epoxygenases that converts arachidonic acid to epoxyeicosanoids and dihydroxyeicosatrienoic acids, and the metabolites secondarily inhibit prostaglandin E2 (PGE2) production. Saikogenin D results in an elevation of [Ca 2+]i due to Ca 2+ release from intracellular stores.
|
-
- HY-146657
-
-
- HY-U00248
-
|
LMP744
MJ-III65; NSC706744
|
Topoisomerase
|
Cancer
|
|
LMP744 (MJ-III65) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
|
-
- HY-W012382
-
-
- HY-N0694
-
|
Schisantherin A
Gomisin-C; Schizantherin-A; Wuweizi ester-A
|
NF-κB
|
Inflammation/Immunology
|
|
Schisantherin A is a dibenzocyclooctadiene lignan. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
|
-
- HY-Y0801
-
-
- HY-U00248A
-
|
LMP744 hydrochloride
MJ-III65 hydrochloride; NSC706744 hydrochloride
|
Topoisomerase
|
Cancer
|
|
LMP744 hydrochloride (MJ-III65 hydrochloride) is a DNA intercalator and Topoisomerase I (Top1) inhibitor with antitumor activity.
|
-
- HY-113005
-
-
- HY-N1987
-
|
Cucurbitacin IIb
|
Apoptosis
|
Inflammation/Immunology
|
|
Cucurbitacin IIb is an active component isolated from Hemsleya amabilis, induces apoptosis with anti-inflammatory activity. Cucurbitacin IIb inhibits phosphorylation of STAT3, JNK and Erk1/2, enhances the phosphorylation of IκB and NF-κB (p65), blocks nuclear translocation of NF-κB (p65) and decreases mRNA levels of IκBα and TNF-α.
|
-
- HY-147678
-
|
GPR40 agonist 5
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
GPR40 agonist 5 (compound I-14) is an orally active and potent GPR40 (G protein coupled receptor 40) agonist, with an EC50 of 47 nM. GPR40 agonist 5 decreases the levels of blood glucose and improves the glucose tolerance. GPR40 agonist 5 has sufficient effectiveness for the control of hyperglycemia state in type 2 diabetic mice.
|
-
- HY-12083
-
|
PPY-A
|
Bcr-Abl
|
Cancer
|
|
PPY-A is a potent T315I mutant and wild-type Abl kinases inhibitor with IC50s of 9 and 20 nM, respectively. PPY-A inhibits Ba⁄F3 cells transformed with wild-type Abl and Abl T315I mutantl with IC50s of 390 and 180 nM, respectively. PPY-A can be used for the research of chronic myeloid leukemia (CML).
|
-
- HY-N8884
-
|
Coelonin
|
PTEN
Akt
NF-κB
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Coelonin is a dihydrophenanthrene with anti-inflammation activity. Coelonin inhibits LPS-induced PTEN phosphorylation. Coelonin inhibits NF-κB activation and p27Kip1 degradation by regulating the PI3K/AKT pathway negatively. Coelonin can inhibit IκBα phosphorylation and degradation and increases the expression of IκBα protein.
|
-
- 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-12383
-
|
Pelubiprofen
|
COX
|
Inflammation/Immunology
Neurological Disease
|
|
Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects.
|
-
- HY-144715
-
|
HIV-1 inhibitor-17
|
HIV
|
Infection
|
|
HIV-1 inhibitor-18 (compound V-25i) is a potent HIV-1 capsid inhibitor with an EC50 value of 2.57 μM for HIV-1 NL4-3. HIV-1 inhibitor-18 has certain cytotoxicity (MT-4 cells CC50 >8.55).
|
-
- 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-N0602
-
-
- HY-13783
-
|
BIBF0775
|
TGF-β Receptor
|
Cancer
|
|
BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.
|
-
- HY-B1756
-
-
- HY-13670
-
|
Lurtotecan
GI147211; OSI-211
|
Topoisomerase
|
Cancer
|
|
Lurtotecan (GI147211; OSI-211), a semisynthetic Camptothecin analog, is a topoisomerase I inhibitor. Lurtotecan has anticancer effects.
|
-
- HY-13631AS
-
|
Exatecan-d5 mesylate
DX8951f-d5; Exatecan-d5 (mesylate); Deuterated labeled Exatecan (mesylate)
|
Topoisomerase
|
Cancer
|
|
Exatecan-d5 (mesylate) is deuterium labeled Exatecan mesylate. Exatecan mesylate is a DNA topoisomerase I inhibitor, with an IC50 of 0.975 μg/mL[1].
|
-
- HY-106895
-
-
- HY-121232
-
-
- HY-19637
-
|
SW044248
|
Topoisomerase
|
Cancer
|
|
SW044248 is a non-canonical topoisomerase I inhibitor, and selectively toxic for certain non-small cell lung cancer (NSCLC) cell lines.
|
-
- HY-N10367
-
|
Corydamine
|
Topoisomerase
|
Cancer
|
|
Corydamine, 3-arylisoquinoline alkaloid, is a potent DNA topoisomerase I/II inhibitor. Corydamine has anti-cancer activity.
|
-
- HY-123450
-
|
S116836
|
Bcr-Abl
Apoptosis
PDGFR
|
Cancer
|
|
S116836, a potent, orally active BCR-ABL tyrosine kinase inhibitor, blocks both wild-type as well as T315I Bcr-Abl. S116836 arrests the cells in the G0/G1 phase of cell cycle, induces apoptosis, increases ROS production, and decreases GSH production in BaF3/WT and BaF3/T315I cells. S116836 also inhibits SRC, LYN, HCK, LCK and BLK, and receptor tyrosine kinases such as FLT3, TIE2, KIT, PDGFR-β. Antitumor activies.
|
-
- HY-P3883
-
-
- HY-110261
-
|
GS143
|
IKK
E1/E2/E3 Enzyme
NF-κB
|
Inflammation/Immunology
|
|
GS143 is a selective IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCF βTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
|
-
- HY-P1934A
-
|
Cyclo(L-Phe-L-Pro)
|
Fungal
IFNAR
Reactive Oxygen Species
|
Cancer
Inflammation/Immunology
Infection
|
|
Cyclo(L-Phe-L-Pro), isolated from Pseudomonas fluorescens and Pseudomonas alcaligenes cell-free culture supernatants is an antifungal cyclic dipeptide. Cyclo(L-Phe-L-Pro) inhibits IFN-β production by interfering with retinoic-acid-inducible gene-I (RIG-I) activation. Cyclo(L-Phe-L-Pro) exhibits free-radical scavenging activity with the IC50 of 24 µM in the DPPH assay.
|
-
- HY-129966
-
|
PROTAC IRAK4 degrader-1
|
PROTACs
IRAK
|
Cancer
|
|
PROTAC IRAK4 degrader-1 is a Cereblon-based PROTAC interleukin-1 receptor-associated kinase 4 (IRAK4) degrader extracted from patent US20190192668A1 Compound I-210, makes <20%, >20-50%, and >50% IRAK4 degradation at 0.01, 0.1, and 1 μM in OCI-LY-10 cells, respectively.
|
-
- HY-147925
-
|
hCAI/II-IN-4
|
Carbonic Anhydrase
|
Others
|
|
hCAI/II-IN-4 (compound 6d) is a potent dual hCA I/II inhibitor with Ki values of 16.95, 15.22 and 27.04 nM for hCA I, hCA II and hCA Ⅸ, respectively. hCAI/II-IN-4 has anti-hypoxia activities and low toxicity. hCAI/II-IN-4 can be used for acute mountain sickness (AMS) research.
|
-
- HY-P1533A
-
-
- HY-115915
-
|
TS010
|
Glyoxalase (GLO)
|
Cancer
|
|
TS010 is a potent inhibitor of GLO-I with IC50 of 0.57 μM. TS010 has the potential for the research of cancer disease.
|
-
- HY-111634
-
|
Epsilon-momfluorothrin
|
Others
|
Cancer
|
|
Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats.
|
-
- HY-145471
-
-
- HY-W145658
-
-
- HY-114161
-
-
- HY-13631
-
|
Exatecan
DX-8951
|
Topoisomerase
|
Cancer
|
|
Exatecan (DX-8951) is a DNA topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL), and can be used in cancer research.
|
-
- HY-126142
-
-
- HY-18310
-
|
NIBR-17
|
PI3K
|
Cancer
|
|
NIBR-17 is a pan-class I PI3K inhibitor with suitable pharmacokinetic properties and inhibits tumor growth.
|
-
- HY-13432
-
|
Nanatinostat
CHR-3996
|
HDAC
|
Cancer
|
|
Nanatinostat (CHR-3996) is a potent, class I selective and orally active histone deacetylase (HDAC) inhibitor with an IC50 of 8 nM.
|
-
- HY-75342
-
-
- HY-101489A
-
|
GZD856 formic
|
PDGFR
Bcr-Abl
Apoptosis
|
Cancer
|
|
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
|
-
- HY-101489
-
|
GZD856
|
PDGFR
Bcr-Abl
Apoptosis
|
Cancer
|
|
GZD856 formic is a potent and orally active PDGFRα/β inhibitor, with IC50s of 68.6 and 136.6 nM, respectively. GZD856 formic is also a Bcr-Abl T315I inhibitor, with IC50s of 19.9 and 15.4 nM for native Bcr-Abl and the T315I mutant. GZD856 formic has antitumor activity.
|
-
- HY-143273
-
|
DENV-IN-6
|
HIV
DNA/RNA Synthesis
|
Infection
|
|
DENV-IN-6 is a potent DENV (I-IV) inhibitor with EC50s of 17.5, 13.20, 6.8 and 11.41 μM for the inhibition of DENV (I-IV) replication, respectively. DENV-IN-6 also exhibits activity of anti-HIV-1IIIB (EC50=0.0181 µM; CC50=64.92 µM).
|
-
- HY-137460
-
|
Vodobatinib
K0706
|
Bcr-Abl
|
Cancer
|
|
Vodobatinib (K0706) is a potent, third generation and orally active Bcr-Abl1 tyrosine kinase inhibitor with an IC50 of 7 nM. Vodobatinib exhibits activity against most BCR-ABL1 point mutants, and has no activity against BCR-ABL1T315I. Vodobatinib can be used for chronic myeloid leukemia (CML) research.
|
-
- HY-147833
-
|
ALK-IN-22
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
ALK-IN-22 (compound I-24) is a potent ALK inhibitor with IC50 values of 2.3, 3.7 and 2.9 nM for ALK, ALK L1196M and ALK G1202R, respectively. ALK-IN-22 down-regulated the phosphorylation of ALK and its downstream proteins. ALK-IN-22 induces apoptosis. ALK-IN-22 can be used for tumor research.
|
-
- HY-13631A
-
-
- HY-113166
-
-
- HY-13566AS
-
|
Belotecan-d7 hydrochloride
|
Topoisomerase
|
Cancer
|
|
Belotecan-d7 (hydrochloride) is the deuterium labeled Belotecan hydrochloride. Belotecan hydrochloride (CKD-602 hydrochloride), a Topoisomerase I inhibitor, is a synthetic camptothecin derivative[1][2].
|
-
- HY-113005A
-
-
- HY-12163
-
|
Entinostat
MS-275; SNDX-275
|
HDAC
Autophagy
Apoptosis
|
Cancer
|
|
Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively.
|
-
- HY-114161A
-
-
- HY-139070
-
-
- HY-111451
-
|
Tuvusertib
M1774; ATR inhibitor 1
|
ATM/ATR
|
Cancer
|
|
Tuvusertib (ATR inhibitor 1) is a ATR inhibitor extracted from patent WO2015187451A1, compound I-l, with a Ki value below 1 μΜ.
|
-
- HY-100409
-
|
PHCCC
|
mGluR
|
Cancer
|
|
PHCCC is a Group I mGluR antagonist with an IC50 of 3 μM. PHCCC is a selective positive modulator of mGlu4 receptor. Antiparkinsonian effect.
|
-
- HY-107133
-
-
- HY-N7603
-
-
- HY-N0799
-
|
Protodioscin
|
Endogenous Metabolite
|
Cancer
|
|
Protodioscin, a major steroidal saponin in Trigonella foenum-graecum Linn., has been shown to exhibit multiple biological actions, such as anti-hyperlipidemia, anti-cancer, sexual effects and cardiovascular properties.
|
-
- HY-W145693
-
-
- HY-P1075
-
|
CALP3
|
Calcium Channel
|
Cancer
Neurological Disease
|
|
CALP3, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
|
-
- HY-Y0051
-
|
5-Hydroxymethylfurfural
2-Hydroxymethyl-5-furfural; 2-Formyl-5-hydroxymethylfuran
|
Fungal
|
Others
|
|
5-Hydroxymethylfurfural (2-Hydroxymethyl-5-furfural), derived from Cornus officinalis, inhibits yeast growth and fermentation as stressors.
|
-
- HY-145788
-
-
- HY-P4044
-
-
- HY-146348
-
|
Tuberculosis inhibitor 5
|
Bacterial
|
Infection
|
|
Tuberculosis inhibitor 5 (Compound 11i) is a potent antimycobacterial biphenyl analogue without noticeable cytotoxicity. Tuberculosis inhibitor 5 is an anti-tuberculosis agent.
|
-
- HY-P99478
-
-
- HY-112729
-
|
HC-056456
3,4-Bis(2-thienoyl)-1,2,5-oxadiazole-N-oxide
|
Calcium Channel
|
Others
|
|
HC-056456 is an effective but not perfectly-selective blocker of CatSper channels. The [Na +]i rise is slowed by HC-056456 (IC50~3 µM).
|
-
- HY-16711
-
-
- HY-U00068
-
-
- HY-13277
-
-
- HY-15542A
-
|
FRAX597
|
PAK
|
Cancer
|
|
FRAX597 is a potent group I p21-activated Kinases (PAKs) inhibitor with IC50 of 8, 13 and 19 nM for PAK1, 2 and 3.
|
-
- HY-131958
-
|
D942
|
AMPK
|
Cancer
|
|
D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth.
|
-
- HY-N0629
-
-
- HY-13251
-
-
- HY-N0622
-
-
- 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-16560S
-
|
Camptothecin-d5
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Cancer
Infection
|
|
Camptothecin-d5 is the deuterium labeled Camptothecin. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM[1]. Camptothecin (CPT) exhibits powerful antineoplastic activity against colorectal, breast, lung and ovarian cancers, modulates hypoxia-inducible factor-1α (HIF-1α) activity by changing microRNAs (miRNA) expression patterns in human cancer cells[2][3].
|
-
- HY-124662
-
|
IHVR-19029
|
Glucosidase
|
Infection
|
|
IHVR-19029 is a potent endoplasmic reticulum (ER) α-glucosidases I and II inhibitor, with an IC50 of 0.48 μM for ER a-glucosidase I. IHVR-19029 efficiently blocks the replication of several hemorrhagic fever viruses, such as Dengue virus (DENV), Ebola virus (EBOV) and Rift Valley fever virus. The combination of IHVR-19029 with Favipiravir (HY-14768) improves the antiviral efficacy.
|
-
- HY-101170
-
|
BU224 hydrochloride
|
Imidazoline Receptor
Apoptosis
TNF Receptor
|
Inflammation/Immunology
Neurological Disease
|
|
BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research.
|
-
- HY-P1075A
-
|
CALP3 TFA
|
Calcium Channel
|
Cancer
Neurological Disease
|
|
CALP3 TFA, a Ca 2+-like peptide, is a potent Ca 2+ channel blocker that activates EF hand motifs of Ca 2+-binding proteins. CALP3 TFA can functionally mimic increased [Ca 2+]i by modulating the activity of Calmodulin (CaM), Ca 2+ channels and pumps. CALP3 TFA has the potential in controlling apoptosis in diseases such as AIDS or neuronal loss due to ischemia.
|
-
- HY-N0648
-
|
Monotropein
|
Others
|
Inflammation/Immunology
|
|
Monotropein is an iridoid glycoside isolated Morinda officinalis. Monotropein inhibits the expression of inflammatory mediators in dextran sulfate sodium (DSS)-induced colitis mouse model.
|
-
- HY-N6008
-
|
7-O-Methyl morroniside
|
Others
|
Others
|
|
7-O-Methyl morroniside is an iridoid glycoside (IG) extracted from Cornus officinalis fructus, used in many traditional Chinese medicines.
|
-
- HY-P2921
-
|
Urate oxidase
Uox
|
Endogenous Metabolite
|
Others
|
|
Urate oxidase (Uox), i.e., uricase, is often used in biochemical studies. Urate oxidase is a peroxisomal enzyme that catalyzes the oxidation of uric acid to allantoin in most mammals.
|
-
- HY-18623
-
|
VI 16832
|
Others
|
Cancer
|
|
VI 16832 is a broad spectrum Type I kinase inhibitor which can be used as an enrichment tool for the comparative expression analysis of protein kinases in different cancer cell lines.
|
-
- HY-100223
-
-
- HY-147400
-
-
- HY-126373
-
|
SN-38 glucuronide
SN-38G
|
Drug Metabolite
|
Cancer
|
|
SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer.
|
-
- HY-N8488
-
|
Anhydro-6-epiophiobolin A
|
Others
|
Others
|
|
Anhydro-6-epiophiobolin A, an analog of Ophiobolin A, is a potent inhibitor of photosynthesis (I50s of 6.1 and 1 mM for photosynthesis in Chlorella and Spinach, respectively).
|
-
- HY-W007648
-
|
Methyl 3-aminopropanoate hydrochloride
β-Alanine methyl ester hydrochloride
|
Others
|
Others
|
|
Methyl 3-aminopropanoate hydrochloride is prepared by esterification of Β-Alanine (I). Methyl 3-aminopropanoate hydrochloride can be used in the synthesis of bidentate pyridine-acid ligand.
|
-
- HY-136773
-
-
- HY-W013158
-
|
Trimethyloctadecylammonium bromide
|
Dynamin
|
Infection
|
|
Trimethyloctadecylammonium bromide is an inhibitor of dynamin, with an IC50 value of 1.9 μM for dynamin I. Trimethyloctadecylammonium bromide exhibits antibacterial activity against Staphylococcus aureus.
|
-
- HY-110363
-
-
- HY-P1853
-
-
- HY-146365
-
|
HIV-1 inhibitor-30
|
HIV
|
Infection
Inflammation/Immunology
|
|
HIV-1 inhibitor-30 (compound 10i) is a potent HIV-1 inhibitor with an EC50 value of 40 nM and an IC50 value of 80 nM for HIV-1 RT DNA polymerase. HIV-1 inhibitor-30 has highly antiretroviral activity against seven non-nucleoside reverse transcriptase inhibitor (NNRTI)-resistant HIV-1 strains (RT-K103N; RT-Y181C; RT-K103N,Y181C; RT-L100I,K103N; RT-Y188L; RT-K103N,G190A; RT-K103N,V108I) with IC50s of 0.04~1.42 μM. HIV-1 inhibitor-30 can be used for researching AIDS.
|
-
- HY-148385
-
|
Ganglioside GM2
|
Others
|
Cancer
|
|
Ganglioside GM2 is a human tumor antigen (OFA-I-1). Ganglioside GM2 is the major lysosomal storage compound of Tay-Sachs disease.
|
-
- HY-133667
-
|
Bromoiodoacetamide
|
Apoptosis
|
Cancer
|
|
Bromoiodoacetamide is a kind of iodinated haloacetamides (I-HAcAms), with cytotoxicity. Bromoiodoacetamide induces cytotoxicity by via reactive oxygen species (ROS) accumulation and apoptosis in HepG-2 cells.
|
-
- HY-N10438
-
-
- HY-128589
-
|
CHMFL-KIT-033
|
c-Kit
|
Cancer
|
|
CHMFL-KIT-033 is a potent and selective inhibitor of c-KIT T670I mutant for gastrointestinal stromal tumors (GISTs), with an IC50 of 0.045 μM.
|
-
- HY-B0199A
-
-
- HY-78349
-
|
A 77-01
|
TGF-β Receptor
|
Cancer
|
|
A 77-01 is a potent inhibitor of transforming growth factor (TGF)-β type I receptor superfamily activin-like kinase ALK5 with an IC50 of 25 nM.
|
-
- HY-136773A
-
-
- HY-113623
-
|
Pyrenophorol
|
Others
|
Others
|
|
Pyrenophorol is a C9H12O3 compound isolated in low yield from culture filtrates of the phytopathogenic fungus Stemphylium radicinum, C.M.I. 105654.
|
-
- HY-N1201
-
-
- HY-129721
-
|
Acid Red 26
Ponceau MX; xylidine ponceau 2R (C.I. 16150)
|
Biochemical Assay Reagents
|
Others
|
|
Acid Red 26 is a biochemical reagent that can be used as a biological material or organic compound for life science related research.
|
-
- HY-151547
-
|
MRS4719
|
P2X Receptor
|
Neurological Disease
|
|
MRS4719 is a potent P2X4 receptor antagonist with an IC50 value of 0.503 μM for human P2X4 receptor. MRS4719 can reduce infarct volume and reduce brain atrophy, showing neuroprotective and neuro-rehabilitative activities in ischemic stroke model. MRS4719 also reduces ATP-induced [Ca 2+]i influx in primary human monocyte-derived macrophages. MRS4719 can be used to research ischemic stroke.
|
-
- HY-152955
-
|
STING agonist-22
|
STING
|
Infection
Inflammation/Immunology
|
|
STING agonist-22 (CF501) is a potent non-nucleotide STING agonist. STING agonist-22 is a adjuvant by activating STING to induce the type I interferon (IFN-I) response and proinflammatory cytokine production. STING agonist-22 can be used as an adjuvant to boost the original protein vaccine, producing potent, broad, and long-term immune protection. STING agonist-22 can be used for SARS-CoV-2 variants and sarbecovirus diseases research.
|
-
- HY-12383S
-
|
Pelubiprofen-13C,d3
|
Isotope-Labeled Compounds
COX
|
Inflammation/Immunology
Neurological Disease
|
|
Pelubiprofen- 13C,d3 is the 13C- and deuterium labeled Pelubiprofen. Pelubiprofen, an orally active and non-steroidal anti-inflammatory drug, is a member of the 2-arylpropionic acid family and has relatively selective effects on COX-2 activity. Pelubiprofen inhibits COX activity and the transforming growth factor-β activated kinase 1-IκB kinase β-NF-κB pathway, and has significant anti-inflammatory and analgesic effects[1].
|
-
- HY-108608
-
|
o-3M3FBS
|
Others
|
Others
|
|
o-3M3FBS is the negative control of m-3M3FBS. o-3M3FBS inhibits inward and outward currents via mechanisms independent of PLC acting in an antagonistic manner. In contrast, o-3M3FBS also causes an increase in [Ca 2+]i in an agonistic manner.
|
-
- HY-151742
-
|
Norbornene-methyl-NHS
|
ADC Linker
|
Others
|
|
Norbornene-methyl-NHS is a click chemistry reagent containing a TCO group. Dienophile for conjugation via Diels-Alder-reaction, i.e. copper-free click reaction with tetrazines.
|
-
- HY-13555
-
|
β-Lapachone
ARQ-501; NSC-26326
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
β-Lapachone (ARQ-501;NSC-26326) is a naturally occurring O-naphthoquinone, acts as a topoisomerase I inhibitor, and induces apoptosis by inhibiting cell cycle progression.
|
-
- HY-113005S
-
-
- HY-N2198
-
|
Podocarpusflavone A
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Podocarpusflavone A is a DNA topoisomerase I inhibitor. Podocarpusflavone A has moderated anti-proliferative activity and induces cell apoptosis in MCF-7. Podocarpusflavone A is developing anti-tumor agents.
|
-
- HY-16134A
-
|
Celgosivir hydrochloride
MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride
|
Glucosidase
HCV
HIV
|
Infection
|
|
Celgosivir hydrochloride (MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
|
-
- HY-128380
-
|
Dibenamine hydrochloride
N-(2-Chloroethyl)dibenzylamine hydrochloride
|
Adrenergic Receptor
|
Metabolic Disease
|
|
Dibenamine hydrochloride is a competitive and irreversible adrenergic blocking agent and is known to modify the pharmacological effects of epinephrine. Dibenamine hydrochloride cause a significant increase in the rate of destruction of I-epinephrine in the mouse.
|
-
- HY-N0733S2
-
-
- HY-P1118
-
-
- HY-N2270
-
-
- HY-16134
-
|
Celgosivir
MBI 3253; MDL 28574; MX3253
|
Glucosidase
HCV
HIV
|
Infection
|
|
Celgosivir (MBI 3253; MDL 28574; MX3253) is an α-glucosidase I inhibitor; inhibits bovine viral diarrhoea virus (BVDV) with an IC50 of 1.27 μM in in vitro assay.
|
-
- HY-P1104A
-
|
FC131 TFA
|
CXCR
HIV
|
Infection
|
|
FC131 TFA is a CXCR4 antagonist, inhibits [ 125I]-SDF-1 binding to CXCR4, with an IC50 of 4.5 nM. Anti-HIV activity.
|
-
- HY-N7262
-
|
Hydroxyvalerenic acid
|
Others
|
Cancer
|
|
Hydroxyvalerenic acid is isolated from Verbena officinalis, has a low toxicity with IC50 values of 123 and 165 μM against GLC4 and COLO 320 cells, respectively.
|
-
- HY-N1402
-
|
Oxysophoridine
Sophoridine N-oxide
|
Apoptosis
|
Inflammation/Immunology
|
|
Oxysophoridine (Sophoridine N-oxide) is a bioactive alkaloid extracted from the Sophora alopecuroides Linn. Oxysophoridine (Sophoridine N-oxide) shows anti inflammatory, anti oxidative stress and anti apoptosis effects.
|
-
- HY-12293
-
|
LY2857785
|
CDK
Apoptosis
|
Cancer
|
|
LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
|
-
- HY-107568
-
-
- HY-145078
-
-
- HY-N0642
-
|
α-L-Rhamnose monohydrate
|
Others
|
Infection
Metabolic Disease
Cancer
|
|
α-L-Rhamnose monohydrate is a component of the plant cell wall pectic polysaccharides rhamnogalacturonan I and rhamnogalacturonan II. α-L-Rhamnose monohydrate is also a component of bacterial polysaccharides where it plays an important role in pathogenicity.
|
-
- HY-13955
-
-
- HY-153320
-
|
AZ-TAK1
|
MAP3K
|
Cancer
|
|
AZ-TAK1, an ATP-competitive small molecule inhibitor of TAK1, dephosphorylates TAK1, p38, and IκB-α in lymphoma cell lines.
|
-
- HY-18819
-
|
BCR-ABL-IN-2
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-2 is an inhibitor of BCR-ABL1 tyrosine kinase, with IC50s of 57 nM, 773 nm for ABL1 native and ABL1 T315I, respectively.
|
-
- HY-13592
-
|
HDAC-IN-7
Chidamide impurity
|
HDAC
|
Cancer
|
|
HDAC-IN-7 (Chidamide impurity) is an impurity of Chidamide. Chidamide is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor.
|
-
- HY-P1118A
-
-
- HY-100183
-
-
- HY-144376
-
-
- HY-10339
-
-
- HY-13462
-
|
LY-364947
HTS466284
|
TGF-β Receptor
|
Cancer
|
|
LY-364947 (HTS466284) is a potent ATP-competitive inhibitor of TGFβR-I with IC50 of 59 nM, and exhibits 7-fold selectivity over TGFβR-II.
|
-
- HY-N2608
-
|
7-O-Ethylmorroniside
|
Others
|
Metabolic Disease
|
|
7-O-Ethylmorroniside is a iridoid glucoside from the fruit of Cornus officinalis which is a traditional medicine in China and used for the reserch of kidney diseases, including diabetic nephropathy.
|
-
- HY-U00450
-
-
- HY-N0116
-
|
Hematoxylin
Natural Black 1; Haematoxylin
|
Amyloid-β
|
Others
|
|
Hematoxylin (Natural Black 1), a naturally occurring flavonoid compound derived from Caesalpinia sappan Linn.. Hematoxylin is a nuclear stain in histology and is also a potent Aβ42 fibrillogenesis inhibitor with an IC50 of 1.6 µM.
|
-
- HY-130272
-
|
Anti-MI/R injury agent 1
|
Others
|
Cardiovascular Disease
|
|
Anti-MI/R injury agent 1 (compound 18), a Panaxatriol derivative, is an orally active, potent anti-myocardial ischemia/reperfusion (anti-MI/R) injury agent. Anti-MI/R injury agent 1 enhances oxygen-glucose deprivation and reperfusion (OGD/R)-induced cardiomyocyte injury cell viability. Anti-MI/R injury agent 1 can markedly reduce myocardial infarction size, decrease circulating cardiac troponin I (cTnI) leakage, and alleviate cardiac tissue damage in the rats.
|
-
- HY-143557
-
|
Trk-IN-7
|
Trk Receptor
|
Cancer
|
|
Trk-IN-7 (compound I-6) is a potent TRK inhibitor with IC50s of ranging from 0.25-10 nM for TRKA, TRKB and TRKC, respectively. Trk-IN-7 shows inhibition against EML4-ALK (IC50<15 nM) ALK G1202R, ALK C1156Y, ALK R1275Q, ALK F1174L, ALK L1197M, and ALK G1269A (IC50=5-50 nM).
|
-
- HY-147955
-
|
hCAI/II-IN-5
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Metabolic Disease
Neurological Disease
|
|
hCAI/II-IN-5 (compound MZ8) is a potent hCA I and hCA II (human carbonic anhydrase isoenzymes I and II) inhibitor, with IC50 values of 37.88 and 45.23 nM, respectively. hCAI/II-IN-5 also shows inhibition profile against α-Glycosidase and AChE, with IC50 values of 48.98 and 420.14 nM, respectively. hCAI/II-IN-5 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.
|
-
- HY-13522
-
|
Fimepinostat
CUDC-907
|
PI3K
HDAC
Apoptosis
|
Cancer
|
|
Fimepinostat (CUDC-907) potently inhibits class I PI3Ks as well as classes I and II HDAC enzymes with an IC50 of 19/54/39 nM and 1.7/5.0/1.8/2.8 nM for PI3Kα/PI3Kβ/PI3Kδ and HDAC1/HDAC2/HDAC3/HDAC10 , respectively.
|
-
- HY-P1295
-
|
Urocortin, human
Urocortin (human); Human urocortin; Human urocortin 1; Human urocortin I
|
CRFR
|
Neurological Disease
Endocrinology
|
|
Urocortin, human, a 40-aa neuropeptide, acts as a selective agonist of endogenous CRF2 receptor, with Kis of 0.4, 0.3, and 0.5 nM for hCRF1, rCRF2α and mCRF2β, respectively.
|
-
- HY-131338
-
-
- HY-109165A
-
-
- HY-13631D
-
|
Dxd
Exatecan derivative for ADC
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
Dxd (Exatecan derivative for ADC) is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a).
|
-
- HY-P1016A
-
-
- HY-109165
-
-
- HY-19348
-
|
Pimelic Diphenylamide 106
RGFA-8; TC-H 106; Histone Deacetylase Inhibitor VII
|
HDAC
|
Cancer
|
|
Pimelic Diphenylamide 106 is a slow, tight-binding inhibitor of class I HDAC (HDAC 1, 2, and 3, with IC50 values of 150 nM , 760nM, and 370 nM, respectively), demonstrating no activity against class II HDACs.
|
-
- HY-147124
-
|
RIG012
|
IFNAR
|
Cancer
Infection
|
|
RIG012 is a potent RIG-I inhibitor with an IC50 of 0.71 μM using the NADH-coupled ATPase assay. RIG012 inhibits IFN-β and ISG hRsad2 expression.
|
-
- HY-D0980
-
|
Biotin-DADOO
Biotinyl-3,6-dioxaoctanediamine; EZ-Link Amine-PEO2-Biotin
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Biotin-DADOO is a biotinylation reagent, which can be used to synthesize a biotin-estradiol conjugate (i.e., biotin-DADOO-estradiol) to develop a direct, broad range enzyme immunoassay to measure plasma estradiol concentrations.
|
-
- HY-N4191
-
|
Isorosmanol
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Isorosmanol is an abietane-type diterpene isolated from Rosmarinus officinalis L. aerial parts, with antioxidant, neuroprotective and neurotrophic effects. Isorosmanol inhibits AChE activity and melanin synthesis.
|
-
- HY-N3446
-
|
IVHD-valtrate
|
Apoptosis
|
Cancer
|
|
IVHD-valtrate, an active Valeriana jatamansi derivative, is against human ovarian cancer cells in vitro and in vivo. IVHD-valtrate induces cancer cells apoptosis and arrests the ovarian cancer cells in the G2/M phase. IVHD-valtrate has the potential to be a novel chemotherapeutic agent for the human ovarian cancer research.
|
-
- HY-116100
-
-
- HY-112441
-
-
- HY-112951
-
|
ChX710
|
STING
|
Cancer
|
|
ChX710 could prime the type I interferon response to cytosolic DNA, which induces the ISRE promoter sequence, specific cellular Interferon-Stimulated Genes (ISGs), and the phosphorylation of Interferon Regulatory Factor (IRF) 3.
|
-
- HY-142920
-
-
- HY-146441
-
-
- HY-16200
-
-
- HY-W020033S
-
-
- HY-145513
-
|
CL2-MMT-SN38
|
Topoisomerase
|
Cancer
|
|
CL2-MMT-SN38 is a SN-38 derivative. SN-38, an anticancer agent, is an active metabolite of the Topoisomerase I inhibitor Irinotecan (CPT-11).
|
-
- HY-151730
-
|
(Me)Tz-butanoic acid
|
ADC Linker
|
Others
|
|
(Me)Tz-butanoic acid is a click chemistry reagent containing an azide. (Me)Tz-butanoic acid is tetrazine linker for conjugation via Diels-Alder-reaction, i.e. copper-free Click reaction with dienophiles.
|
-
- HY-D1705
-
-
- HY-130278
-
|
MitoPQ
MitoParaquat
|
ROS Kinase
|
Cancer
|
|
MitoPQ is a mitochondria-targeted redox cycler. MitoPQ produces superoxide by redox cycling at the flavin site of complex I, selectively increasing superoxide production within mitochondria. MitoPQ can be used in antioxidant study.
|
-
- HY-10529
-
-
- HY-N0332
-
-
- HY-N0163
-
-
- HY-125990
-
|
SLC13A5-IN-1
|
Sodium Channel
|
Metabolic Disease
Cardiovascular Disease
|
|
SLC13A5-IN-1 is a selective sodium-citrate co-transporter (SLC13A5) inhibitor. SLC13A5-IN-1 completely blocks the uptake of 14C-citrate with an IC50 value of 0.022 μM in HepG2 cells. SLC13A5-IN-1 has the potential for the treatment of metabolic and/or cardiovascular diseases. SLC13A5-IN-1 is extracted from patent WO2018104220A1, Compound I-5.
|
-
- HY-146336
-
|
PARP1/2/TNKS1/2-IN-1
|
PARP
Apoptosis
|
Cancer
|
|
PARP1/2/TNKS1/2-IN-1 (Compound I-9) is a dual PARP-1, PARP-2, TNKS1 and TNKS2 inhibitor with IC50 values of 0.25 nM, 1.2 nM, 13.5 nM and 4.15 nM against PARP-1, PARP-2, TNKS1 and TNKS2, respectively. PARP1/2/TNKS1/2-IN-1 exhibits favorable synergistic antitumor efficacy and induces apoptosis.
|
-
- HY-A0116
-
-
- HY-147790
-
|
MDH1-IN-1
|
Others
|
Cancer
|
|
MDH1-IN-1 (Compound 5i) is a potent inhibitor of MDH1 with an IC50 of 6.79 μM. MDH1-IN-1 has the potential for the research of cancer diseases.
|
-
- HY-153011
-
-
- HY-W012382S
-
|
N-Acetyl-L-tyrosine-d3
|
Endogenous Metabolite
|
|
|
N-Acetyl-L-tyrosine-d3 is the deuterium labeled N-Acetyl-L-tyrosine. N-Acetyl-L-tyrosine originates from tyrosine through an AA acetylase, is associated with aromatic L-amino acid decarboxylase deficiency and tyrosinemia I.
|
-
- HY-136742
-
-
- HY-B0109
-
|
Dorzolamide
L671152; MK507
|
Carbonic Anhydrase
|
Cancer
|
Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
|
-
- HY-N0847
-
|
Micheliolide
|
NF-κB
|
Others
|
|
Micheliolide could effectively attenuate the high glucose-stimulated activation of NF-κB, the degradation of IκBα, and the expression of MCP-1, TGF-β1 and FN in rat mesangial cells (MCs).
|
-
- HY-123390
-
|
DB07107
|
Bcr-Abl
Akt
|
Cancer
|
|
DB07107 is a potent agent resistant T315I mutant Bcr-Abl tyrosine kinase inhibitor. DB07107 is also a potent Akt1 inhibitor with an IC50 value of 360 nM.
|
-
- HY-B0109A
-
|
Dorzolamide hydrochloride
L671152 hydrochloride; MK507 hydrochloride
|
Carbonic Anhydrase
|
Others
|
Dorzolamide (L671152) hydrochloride is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity.
|
-
- HY-A0116A
-
-
- HY-103245
-
|
Cl-4AS-1
|
Androgen Receptor
|
Cancer
|
|
Cl-4AS-1, a potent steroidal androgen receptor (AR) agonist (IC50 = 12 nM), is also an inhibitor of 5α-reductase types I and II (IC50 = 6 and 10 nM, respectively).
|
-
- HY-N0141
-
|
Parthenolide
(-)-Parthenolide
|
NF-κB
Autophagy
Mitophagy
Apoptosis
|
Cancer
|
|
Parthenolide is a sesquiterpene lactone found in the medicinal herb Feverfew. Parthenolide exhibits anti-inflammatory activity by inhibiting NF-κB activation; also inhibits HDAC1 protein without affecting other class I/II HDACs.
|
-
- HY-I0096
-
-
- HY-19529
-
-
- HY-N1039A
-
|
Manool
|
Others
|
Cancer
|
|
Manool is a diterpene from Salvia officinalis. Manool induces selective cytotoxicity in cancer cells. Manool arrests the cancer cells at the G(2)/M phase of the cell cycle.
|
-
- HY-P1104
-
|
FC131
|
CXCR
HIV
|
Infection
|
|
FC131 is a potent CXCR4 antagonist. FC131 inhibits [ 125I]-SDF-1 binding to CXCR4 with an IC50 of 4.5 nM. FC131 has anti-HIV activity.
|
-
- HY-13566
-
|
Belotecan
CKD-602 free base
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Belotecan (CKD-602 free base) is a DNA topoisomerase I inhibitor. Belotecan induces cell apoptosis and cell-cycle arrest. Belotecan is a camptothecin analogue with anti-tumor effects, it can be used for the research of cancer.
|
-
- HY-114192
-
|
TGFβRI-IN-1
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-1 is an oral active and selective TGFβ receptor type I (TGFβRI) kinase inhibitor, with IC50 values of 2 nM and 7.6 μM for TGFβRI and TGFβRII, respectively .
|
-
- HY-144268
-
|
hCAII-IN-7
|
Carbonic Anhydrase
|
Cancer
|
|
hCAII-IN-7 (Compound R-13) is a potent human carbonic anhydrase (hCA) inhibitor with Kis of 60.7, 320.7, 2298, and 35.2 nM for hCA I, II, IV and IX, respectively.
|
-
- HY-118922
-
|
IW927
|
TNF Receptor
|
Inflammation/Immunology
|
|
IW927 is a potent small molecule antagonist that blocks the binding of TNF-α to TNFRc1 with an IC50 value of 50 nM and disrupts TNFα-induced IκB phosphorylation with an IC50 value of 600 nM.
|
-
- HY-13768C
-
|
Topotecan hydrochloride hydrate
SKF 104864A hydrochloride hydrate; NSC 609669 hydrochloride hydrate
|
Topoisomerase
Apoptosis
Autophagy
|
Cancer
|
|
Topotecan hydrochloride hydrate is an orally active and potent Topoisomerase I inhibitor. Topotecan hydrochloride hydrate induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan hydrochloride hydrate shows anticancer activity.
|
-
- HY-101653
-
-
- HY-109109
-
|
Alteminostat
CKD-581
|
HDAC
Apoptosis
|
Cancer
|
|
Alteminostat (CKD-581) is a potent HDAC inhibitor. Alteminostat inhibits the class I-II HDAC family via histone H3 and tubulin acetylation. Alteminostat can be used for lymphoma and multiple myeloma research.
|
-
- HY-111188
-
|
A55453
|
Adrenergic Receptor
|
Others
|
|
A55453 is a prazosin analogue and a potent α1-adrenergic antagonist. 125I-A55453 is a high-affinity alpha 1-adrenergic receptor probe.
|
-
- HY-101392
-
|
Harmane
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
|
Cancer
Neurological Disease
|
|
Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively). Harmane exhibits comutagenic effect.
|
-
- HY-146307
-
|
TrxR-IN-3
|
TrxR
|
Cancer
|
|
TrxR-IN-3 (Compound 2c) is a potent inhibitor of TrxR. TrxR-IN-3 exhibits potent antiproliferative activities against five human cancer cell lines, especially against breast tumor cells. TrxR-IN-3 increases ROS levels and resulted in marked apoptosis by regulating apoptosis-related proteins expressed in the breast cancer cells. TrxR-IN-3 also triggers the formation of autophagosomes and autolysosomes by promoting the expression of LC3-II and Beclin-1 and diminishing the expression of LC3-I and p62 proteins.
|
-
- HY-147954
-
|
α-Glycosidase-IN-1
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Metabolic Disease
Neurological Disease
|
|
α-Glycosidase-IN-1 (compound MZ7) is a potent α-GLY (α-Glycosidase) inhibitor, with an IC50 of 44.72 nM and a KI of 41.74 nM. α-Glycosidase-IN-1 also shows inhibition profile against human carbonic anhydrase isoenzymes I and II (hCA I and hCA II), and acetylcholinesterase (AChE), with IC50 values of 104.87, 100.04, and 654.87 nM, respectively. α-Glycosidase-IN-1 can be used for the research of many diseases such as diabetes, Alzheimer’s disease, heart failure, ulcer, and epilepsy.
|
-
- HY-153013
-
|
SN38-COOH
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
SN38-COOH is used for the synthesis of antibody-drug conjugates (ADCs). SN-38 is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 inhibits DNA and RNA synthesis.
|
-
- HY-P2952
-
|
Adenylate
AMPK; Myokinase; Adk
|
Endogenous Metabolite
|
Others
|
|
Adenylate (Adk), i.e., myokinase, is a phosphotransferase enzyme, is often used in biochemical studies. Adenylate catalyzes the interconversion of adenosine phosphates. Adenylate monitors phosphate nucleotide levels inside the cell, it plays an important role in cellular energy homeostasis.
|
-
- HY-P2455
-
|
LLO (91-99)
Listeriolysin O (91-99)
|
Bacterial
|
Inflammation/Immunology
|
|
LLO (91-99) (Listeriolysin O (91-99)), an exotoxin, is a class I MHC-restricted T-cell epitopes of listeriolysin (LLO). LLO (91-99) is an essential antigen for induction of T-cell mediated immunity in vivo.
|
-
- HY-148668A
-
-
- HY-147608
-
-
- HY-147061
-
|
2-Deoxyribose 5-phosphate disodium
|
Others
|
Others
|
|
2-Deoxyribose 5-phosphate disodium is a substrate of 2-deoxyribose-5-phosphate aldolase (DERA). DERA belongs to the class I aldolases and catalyzes the reversible aldol condensation reaction without any cofactors.
|
-
- HY-129997
-
|
Luteolinidin chloride
|
CD38
|
Inflammation/Immunology
|
|
Luteolinidin is a natural deoxyanthocyanidin, isolated from Sorghum bicolor . 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-152217
-
-
- HY-A0166A
-
|
Cilastatin sodium
MK0791 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct.
|
-
- HY-115686
-
-
- HY-W020033
-
|
Lanosterol
|
Endogenous Metabolite
|
Neurological Disease
|
|
Lanosterol is an intermediate of cholesterol synthesis and use of lanosterol induces ubiquitination and degradation of a rate-controlling enzyme of cholesterol synthesis, i.e., HMG CoA reductase. Lanosterol suppresses the aggregation and cytotoxicity of misfolded proteins linked with neurodegenerative diseases.
|
-
- HY-119370
-
|
CHMFL-ABL-121
|
Bcr-Abl
Apoptosis
|
Cancer
|
|
CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively.
|
-
- HY-A0166
-
|
Cilastatin
MK0791
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct.
|
-
- HY-12508
-
|
CMPDA
|
iGluR
|
Neurological Disease
|
|
CMPDA is a positive allosteric modulator of AMPA receptors with EC50s of 45.4 ± 4.2 nM/63.4 ± 5.6 nM for GluA2i/GluA2o receptor.
|
-
- HY-146206
-
|
HCAIX-IN-1
|
Carbonic Anhydrase
|
Cancer
|
|
HCAIX-IN-1 (compound 21e) is a potent and selective HCAIX inhibitor with KIs of 694.9, 126.6, 3.3, 9.8 nM for hCA I, hCA II, hCA IX, hCA XII, respectively.
|
-
- HY-148668
-
-
- HY-N6057
-
|
Obtusin
|
Monoamine Oxidase
|
Neurological Disease
|
|
Obtusin, isolated from Cassia obtusifolia Linn seed, is a highly selective and competitive human monoamine oxidase-A (hMAO-A) inhibitor with an IC50 of 11.12 μM and a Ki of 6.15 μM. Obtusin plays a preventive role in neurodegenerative diseases, especially anxiety and depression.
|
-
- HY-N0013
-
-
- HY-100406
-
|
(S)-MCPG
(+)-MCPG
|
mGluR
|
Neurological Disease
|
|
(S)-MCPG ((+)-MCPG) is a potent group I/II metabotropic glutamate receptor (mGluRs) antagonist and the active isomer of (RS)-MCPG (HY-100371). (S)-MCPG can be used for the study of the function of mGluRs in spatial learning.
|
-
- HY-13744
-
|
Rubitecan
RFS 2000; 9-Nitrocamptothecin
|
Topoisomerase
|
Cancer
|
|
Rubitecan (RFS 2000), a Camptothecin derivative, is an orally active topoisomerase I inhibitor with broad antitumor activity, and induces protein-linked DNA single-strand breaks, thereby blocking DNA and RNA synthesis in dividing cells.
|
-
- HY-121309
-
|
Doxorubicinone
Adriamycin aglycone; Adriamycinone
|
Endogenous Metabolite
|
Cancer
|
|
Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
|
-
- HY-151470
-
|
Chitinase-IN-5
|
Parasite
|
Others
|
|
Chitinase-IN-5 (8i) is a potent chitinase OfChi-h inhibitor with an IC50 value of 0.051 μM. Chitinase-IN-5 shows good insecticidal activity, it can be used for the research of green pest control and management.
|
-
- HY-19915A
-
-
- HY-12163S
-
|
Entinostat-d4
MS-275-d4; SNDX-275-d4
|
Apoptosis
Autophagy
HDAC
|
Cancer
|
|
Entinostat-d4 is the deuterium labeled Entinostat[1]. Entinostat is an oral and selective class I HDAC inhibitor, with IC50s of 243 nM, 453 nM, and 248 nM for HDAC1, HDAC2, and HDAC3, respectively[2].
|
-
- HY-P3674
-
|
LH-RH (7-10)
|
GnRH Receptor
|
Endocrinology
|
|
LH-RH (7-10) is a tetrapeptide, one of major degradation products of luteinising-hormone releasing hormone (LHRH) via pituitary and hypothalamus. LH-RH (7-10) produced in macrophages, type I-like and type II pneumocytes.
|
-
- HY-128575
-
|
BNC375
|
nAChR
|
Neurological Disease
|
|
BNC375 is a potent, selective, and orally available type I positive allosteric modulator of α7 nAChRs with an EC50 of 1.9 μM. BNC375 exhibits good CNS-agent like properties and clinical candidate potential. .
|
-
- HY-151173
-
-
- HY-100372
-
|
E4CPG
(RS)-ECPG
|
mGluR
|
Neurological Disease
|
|
E4CPG ((RS)-ECPG) is a Group I/Group II metabotropic glutamate receptor (mGluR) antagonist. E4CPG can inhibit the paired-pulse ratio of monosynaptic inhibitory postsynaptic currents (IPSC) potentiation.
|
-
- HY-13631DS
-
|
Dxd-d5
Exatecan-d5 derivative for ADC
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
Dxd-d5 is a deuterium labeled Dxd. Dxd is a potent DNA topoisomerase I inhibitor, with an IC50 of 0.31 μM, used as a conjugated drug of HER2-targeting ADC (DS-8201a) [1].
|
-
- HY-N6800A
-
-
- HY-N7496
-
|
Odoroside A
|
Apoptosis
|
Cancer
|
|
Odoroside A is an active ingredient extracted from the leaves of Nerium oleander Linn. Odoroside A has anti-cancer activity. Odoroside A could induce apoptosis and cell cycle arrest through ROS/p53 signaling pathway, leading to the tumor cell death.
|
-
- HY-N1926
-
|
Dihydrocoumarin
Hydrocoumarin; Chroman-2-one
|
Sirtuin
|
Cancer
|
|
Dihydrocoumarin is a compound found in Melilotus officinalis. Dihydrocoumarin is a yeast Sir2p inhibitor. Dihydrocoumarin also inhibits human SIRT1 and SIRT2 with IC50s of 208 μM and 295 μM, respectively.
|
-
- HY-101392S1
-
|
Harmane-d2
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
|
Cancer
Neurological Disease
|
|
Harmane-d2 is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
|
-
- HY-13453
-
|
BAY 11-7082
BAY 11-7821
|
IKK
Deubiquitinase
Autophagy
Apoptosis
NF-κB
|
Cancer
Inflammation/Immunology
|
|
BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
|
-
- HY-101392S
-
|
Harmane-d1
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
|
Cancer
Neurological Disease
|
|
Harmane-d is the deuterium labeled Harmane. Harmane, a β-Carboline alkaloid (BCA), is a potent neurotoxin that causes severe action tremors and psychiatric manifestations. Harmane shows 1000-fold selectivity for I1-Imidazoline receptor (IC50=30 nM) over α2-adrenoceptor (IC50=18 μM). Harmane is also a potent and selective inhibitor of monoamine oxidase (MAO) (IC50s=0.5 and 5 μM for human MAO A/B, respectively)[1][2][3][4].
|
-
- HY-N4267
-
|
Yangambin
|
Calcium Channel
|
Infection
Cardiovascular Disease
|
|
Yangambin, a furofuran lignan, is already isolated from plants such as member of the Annonaceae family, including species of the genus Rollinia: R. pickeli, R. exalbidaand R. mucosa, as well from the Magnolia biondii. Yangambin, a selective PAF receptor antagonist, inhibits Ca 2+ influx through voltage-gated Ca 2+ channels, leading to the reduction in [Ca 2+]i in vascular smooth muscle cells and consequent peripheral vasodilation. Yangambin exhibits the antiallergic activity against β-hexosaminidase release with an IC50 of 33.8 μM and for anti-inflammatory activity with an IC50 of 37.4 μM.
|
-
- HY-147988
-
-
- 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-117554
-
|
BRD9757
|
HDAC
|
Cancer
|
|
BRD9757 is a potent, capless and selective HDAC6 inhibitor with an IC50 of 30 nM. BRD9757 shows excellent selectivity toward HDAC6 versus the class I (>20-fold) and class II (>400-fold) HDACs.
|
-
- HY-P1338
-
|
PL-017
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats.
|
-
- HY-P3424
-
-
- HY-N2237
-
-
- HY-P1569
-
|
LCMV gp33-41
|
Arenavirus
|
Inflammation/Immunology
|
|
LCMV gp33-41, the carboxyl-extended 11-aa-long peptide, is an lymphocytic choriomeningitis virus sequence restricted by MHC class I H-2Db molecules and presented to cytotoxic T lymphocytes.
|
-
- HY-B0615A
-
|
Moricizine Hydrochloride
EN 313; Ethmosine; Ethmozin
|
Others
|
Cardiovascular Disease
|
|
Moricizine Hydrochloride (EN 313) is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period.
|
-
- HY-A0276A
-
|
Gentamicin
|
Antibiotic
Bacterial
|
Infection
|
|
Gentamicin, an orally active aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. Gentamicin inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-127026A
-
|
Quinaprilat hydrate
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Quinaprilat hydrate is a non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat hydrate specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat hydrate acts as anti-hypertensive agent and vasodilator.
|
-
- HY-120758
-
|
SEL24-B489
|
Pim
FLT3
Apoptosis
|
Cancer
|
SEL24-B489 is a potent, type I, orally active, dual PIM and FLT3-ITD inhibitor, with Kd values of 2 nM for PIM1, 2 nM for PIM2 and 3 nM for PIM3, respectively.
|
-
- HY-146693
-
|
CJJ300
|
TGF-β Receptor
|
Cancer
|
|
CJJ300 is a transforming growth factor-β (TGF-β) inhibitor with an IC50 of 5.3 µM. CJJ300 inhibits TGF-β signaling by disrupting the formation of the TGF-β-TβR-I-TβR-II signaling complex.
|
-
- HY-N6865
-
|
Groenlandicine
|
Topoisomerase
|
Cancer
Metabolic Disease
|
|
Groenlandicine is a protoberberine alkaloid isolated from Coptidis Rhizoma. Groenlandicine exhibits moderate inhibitory effect with IC50 value of 154.2 μM for human recombinant aldose reductase (HRAR). Groenlandicine selectively induces topoisomerase I-mediated DNA cleavage.
|
-
- HY-13634B
-
-
- HY-113378S
-
|
3-Hydroxybutyric acid-d4 sodium
β-Hydroxybutyric acid-d4 (sodium)
|
Endogenous Metabolite
|
Metabolic Disease
|
|
3-Hydroxybutyric acid-d4 (sodium) is the deuterium labeled 3-Hydroxybutyric acid. 3-Hydroxybutyric acid (β-Hydroxybutyric acid) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid can modulate the properties of membrane lipids[1].
|
-
- HY-W008351S
-
|
L-Ribose-13C
|
Isotope-Labeled Compounds
Antibiotic
|
Cancer
|
|
L-Ribose- 13C is the 13C labeled L-Ribose. L-Ribose, a non-naturally occurring pentose, is an ideal starting material for use in synthesizing L-nucleosides analogues. Many anticancer and antiviral agents are synthesized based on a backbone of L-Ribose and i
|
-
- HY-P4551
-
-
- HY-131233
-
|
Anti-virus agent 1
Remdesivir isopropyl ester analog
|
Antibiotic
|
Infection
|
|
Anti-virus agent 1 (compound 4i), a phosphoramidate proagent of GS-5734 (HY-104077; Remdesivir), has potent antiviral activity. Anti-virus agent 1 is used for the research of coronavirus and Ebola virus (EBOV).
|
-
- HY-N6714
-
|
Alternariol
|
Topoisomerase
|
Cancer
Infection
|
|
Alternariol is a mycotoxin produced by Alternaria species. AOH inhibits the catalytic activity of topoisomerase I and topoisomerase II enzymes. Alternariol exhibits a variety of therapeutic and biological properties such as phytotoxicity, cytotoxicity, anti-HIV, anti-cancer, and anti-microbial properties.
|
-
- HY-118091A
-
|
Bexlosteride
LY300502
|
Others
|
Cancer
|
|
Bexlosteride (LY300502) is a benzoquinolinone human type I 5α-reductase inhibitor. Bexlosteride shows metabolic inhibitory, antiproliferative, and antisecretory effects in LNCaP human prostatic adenocarcinoma cell cultures. Bexlosteride can be used for the research of prostatic cancer.
|
-
- HY-128677
-
|
NCC007
|
Casein Kinase
|
Neurological Disease
|
|
NCC007 is a dual casein kinase Iα (CKIα) and δ (CKIδ) inhibitor with IC50s of 1.8 and 3.6 μM, respectively. NCC007 can be used in research of modulating mammalian circadian rhythms.
|
-
- HY-150041
-
|
TL4830031
|
TAM Receptor
|
Cancer
|
|
TL4830031 (compound 8i), a quinolone antibiotic derivatives, is a potent Axl inhibitor with an IC50 value of 26 nM. TL4830031 inhibits the phosphorylation of Axl. TL4830031 inhibits cell invasion and migration. TL4830031 can be used for cancer research.
|
-
- HY-115916
-
|
NOS-IN-2
|
NO Synthase
|
Inflammation/Immunology
|
|
NOS-IN-2 (Compound 4i) is a potent, selective, imidamide derived NOS inhibitor with an IC50 against iNOS of 20 µM, without inhibiting eNOS. NOS-IN-2 has little toxicity and can be used for studying inflammatory disorders.
|
-
- HY-146355
-
|
hCAII-IN-2
|
Carbonic Anhydrase
|
Cancer
|
|
hCAII-IN-2 (Compound 11f) is a cytosolic human carbonic anhydrase (hCA) inhibitor with Ki values of 261.4, 3.8, 19.6 and 45.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively.
|
-
- HY-13768
-
|
Topotecan
SKF 104864A; NSC 609669
|
Topoisomerase
Autophagy
Apoptosis
|
Cancer
|
|
Topotecan (SKF 104864A; NSC 609669) is an orally active and potent Topoisomerase I inhibitor. Topotecan induces cell cycle arrest in G0/G1 and S phases and promotes apoptosis. Topotecan shows anticancer activity.
|
-
- HY-10583
-
-
- HY-P1569A
-
|
LCMV gp33-41 TFA
|
Arenavirus
|
Inflammation/Immunology
|
|
LCMV gp33-41 (TFA), the carboxyl-extended 11-aa-long peptide, is an lymphocytic choriomeningitis virus sequence restricted by MHC class I H-2Db molecules and presented to cytotoxic T lymphocytes.
|
-
- HY-150700
-
|
RLX-33
|
ERK
|
Metabolic Disease
|
|
RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome.
|
-
- HY-150070
-
|
Butabindide
UCL-1397
|
Others
|
Neurological Disease
|
|
Butabindide (UCL-1397) is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide inhibits TPP II to protect CCK-8 against inactivation.
|
-
- HY-135845
-
|
TP3011
CH0793011
|
Topoisomerase
|
Cancer
|
|
TP3011 (CH0793011) is an active metabolite of CH-0793076 and is a potent topoisomerase I inhibitor equipotent as SN38. TP3011 is against cancer cell lines growth with IC50s at the range sub-nanomolar in vitro.
|
-
- HY-P1338A
-
|
PL-017 TFA
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats.
|
-
- HY-115755
-
|
Thio-ITP
6-Thioinosine 5′-triphosphate; 6-Mercaptopurine-riboside-5'-triphosphate; 6-Thio-ITP
|
DNA/RNA Synthesis
|
Cancer
|
|
Thio-ITP (6-Thioinosine 5′-triphosphate) is an RNA polymerase activity competitive inhibitor. Thio-ITP has a high apparent affinity for the polymerases (RNA polymerase I Ki: 40.9 μM; RNA polymerase II Ki: 38.0 μM).
|
-
- HY-131057
-
-
- HY-A0276
-
|
Gentamicin sulfate
|
Bacterial
Antibiotic
|
Infection
Cancer
|
|
Gentamicin sulfate, an orally active aminoglycoside antibiotic, inhibits the growth of both gram-positive and gram-negative bacteria and to inhibit several strains of mycoplasma in tissue culture. Gentamicin sulfate inhibits DNase I with an IC50 of 0.57 mM.
|
-
- HY-P2093
-
|
S961
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
|
-
- HY-N0029
-
|
Forsythoside B
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Forsythoside B is a phenylethanoid glycoside isolated from Forsythia suspensa (Thunb.) Vahl, a Chinese folk medicinal plant for treating inflammatory diseases and promoting blood circulation. Forsythoside B could inhibit TNF-alpha, IL-6, IκB and modulate NF-κB.
|
-
- HY-N11536
-
|
erythro-Austrobailignan-6
|
Topoisomerase
Apoptosis
|
Cancer
|
|
erythro-Austrobailignan-6 is an orally active anti-cancer agent. erythro-Austrobailignan-6 inhibits DNA topoisomerase I and II activity. erythro-Austrobailignan-6 induces cell apoptosis and increases phosphorylation of p38 and JNK.
|
-
- HY-116055
-
|
(2R)-Glycerol-O-β-D-galactopyranoside
3-O-β-D-Galactopyranosyl-sn-glycerol
|
Others
|
Others
|
|
(2R)-Glycerol-O-β-D-galactopyranoside (3-O-β-D-Galactopyranosyl-sn-glycerol) is a good substrate for all three components of the lac operon, i.e. β-galactosidase, the lactose transporter and thiogalactoside transacetylase.
|
-
- HY-P2093B
-
|
S961 acetate
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 acetate is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
|
-
- HY-13704
-
|
SN-38
NK012
|
Topoisomerase
ADC Cytotoxin
Autophagy
|
Cancer
|
|
SN-38 (NK012) is an active metabolite of the Topoisomerase I inhibitor Irinotecan. SN-38 (NK012) inhibits DNA and RNA synthesis with IC50s of 0.077 and 1.3 μM, respectively.
|
-
- HY-114303
-
|
CM-675
|
Phosphodiesterase (PDE)
HDAC
|
Neurological Disease
|
|
CM-675 is a dual phosphodiesterase 5 (PDE5) and class I histone deacetylases-selective inhibitor, with IC50 values of 114 nM and 673 nM for PDE5 and HDAC1, respectively. CM-675 has potential to treat Alzheimer’s disease.
|
-
- HY-13323
-
|
CX-5461
|
DNA/RNA Synthesis
|
Cancer
|
|
CX-5461 is a potent and oral rRNA synthesis inhibitor. It inhibits RNA polymerase I-driven transcription of rRNA with IC50s of 142, 113, and 54 nM in HCT-116, A375, and MIA PaCa-2 cells, respectively.
|
-
- HY-106784
-
|
Ajoene
|
Fungal
Apoptosis
|
Cancer
Infection
|
|
Ajoene, a garlic-derived compound, is an antithrombotic and antifungal agent. Ajoene inhibits proliferation and induces apoptosis of human leukaemia CD34-negative cells including HL-60, U937, HEL and OCIM-I. Anticancer activities.
|
-
- HY-127026
-
|
Quinaprilat
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Quinaprilat is an orally active non-mercapto Angiotensin Converting Enzyme (ACE) inhibitor, the active metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits the degradation of bradykinin. Quinaprilat acts as anti-hypertensive agent and vasodilator.
|
-
- HY-136741
-
|
BOT-64
|
IKK
|
Inflammation/Immunology
|
|
BOT-64 is an inhibitory κB (IκB) kinase β (IKKβ) inhibitor with an IC50 of 1 µM. BOT-64 blocks lipopolysaccharide-induced nuclear factor-κB activation and nuclear factor-κB-regulated inflammatory gene transcription.
|
-
- HY-100435
-
|
Oxaquin
MCB-3837; DNV3837
|
Bacterial
|
Infection
|
|
Oxaquin (MCB-3837) is a injectable proagent that is rapidly converted to the active substance MCB3681 in vivo following intravenous (i.v.) administration, active against Gram-positive bacterial species. Oxaquin (MCB-3837) itself has no antimicrobial effects.
|
-
- HY-144107
-
|
HCV-IN-34
|
HCV
|
Infection
|
|
HCV-IN-34 (compound 3i) is an orally active and potent HCV entry inhibitor. HCV-IN-35 shows excellent antiviral activity, with an EC50 of 0.010 μM and a CC50 (half-maximal cytotoxic concentration) of 8.23 μM.
|
-
- HY-133114
-
-
- HY-70063
-
|
Buparlisib
BKM120; NVP-BKM120
|
PI3K
Apoptosis
|
Cancer
|
|
Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.
|
-
- HY-14180
-
|
PHA 408
|
IKK
|
Inflammation/Immunology
|
|
PHA 408 (PHA-408) is a potent, selective and orally active IκB kinase-2 (IKK-2) inhibitor. PHA 408 is a powerful anti-inflammatory agent against lipopolysaccharide (LPS)- and cigarette smoke (CS)-mediated lung inflammation.
|
-
- HY-A0230A
-
|
Spirapril hydrochloride
SCH 33844 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril (SCH 33844) hydrochloride is a potent angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
|
-
- HY-10432A
-
|
A 83-01 sodium
|
TGF-β Receptor
|
Cancer
|
|
A 83-01 sodium is a potent inhibitor of TGF-β type I receptor ALK5 kinase, ALK4 and ALK7, with IC50s of 12 nM, 45 nM and 7.5 nM against the transcription induced by ALK5, ALK4 and ALK7, respectively.
|
-
- HY-113607
-
|
Asimicin
Bullatacin
|
Mitochondrial Metabolism
Parasite
|
Cancer
Infection
|
|
Asimicin (Bullatacin) is antitumor acetogenin that can be isolated from the bark and seeds of the pawpaw tree, Asimina trilobal Dunal. Asimicin inhibits mitochondrial respiration through the inhibition of complex I. Asimicin shows toxicity to Aphis gossypii, mosquito larvae and mammalian.
|
-
- HY-109015S
-
|
Tucidinostat-d4
Chidamide-d4; HBI-8000-d4; CS 055-d4
|
HDAC
|
Cancer
|
|
Tucidinostat-d4 is the deuterium labeled Tucidinostat. Tucidinostat is a potent and orally bioavailable HDAC enzymes class I (HDAC1/2/3) and class IIb (HDAC10) inhibitor, with IC50s of 95, 160, 67 and 78 nM, respectively[1].
|
-
- HY-100371
-
|
(RS)-MCPG
alpha-MCPG
|
mGluR
|
Neurological Disease
|
|
(RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
|
-
- HY-145929
-
-
- HY-101954
-
|
Inarigivir
ORI-9020; SB-9000
|
HBV
|
Infection
|
|
Inarigivir (ORI-9020) is a dinucleotide antiviral drug that can significantly reduce liver HBV DNA in transgenic mice expressing hepatitis B virus. Inarigivir (ORI-9020) act as a RIG-I agonist to activate cellular innate immune responses.
|
-
- HY-100530D
-
|
Rp-cAMPS sodium salt
|
PKA
|
Neurological Disease
|
|
Rp-cAMPS sodium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS sodium salt is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-112062
-
|
POL1-IN-1
|
DNA/RNA Synthesis
|
Cancer
|
|
POL1-IN-1 is a RNA polymerase 1 (POL1, also known as Pol I) inhibitor with an IC50 of less than 0.5 uM. POL1-IN-1 inhibits ribosome biogenesis by inhibiting POL1 transcription.
|
-
- HY-100530A
-
|
Rp-cAMPS
|
PKA
|
Neurological Disease
|
|
Rp-cAMPS, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-15778A
-
-
- HY-13687
-
|
IKK 16
|
IKK
LRRK2
|
Inflammation/Immunology
|
|
IKK 16 is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.
|
-
- HY-A0210
-
-
- HY-N2306
-
|
Aclacinomycin A
Aclarubicin
|
Topoisomerase
DNA/RNA Synthesis
Proteasome
Antibiotic
|
Cancer
|
|
Aclacinomycin A (Aclarubicin) is an orally active and potent anthracycline antitumor antibiotic. Aclacinomycin A is an inhibitor of topoisomerase I and II. Aclacinomycin A inhibits synthesis of nucleic acid, especially RNA. Aclacinomycin A might inhibit the 26S protease complex as well as the ubiquitin-ATP-dependent proteolysis.
|
-
- HY-P2093A
-
|
S961 TFA
|
Insulin Receptor
|
Metabolic Disease
|
|
S961 TFA is an high-affinity and selective insulin receptor (IR) antagonist with IC50s of 0.048, 0.027, and 630 nM for HIR-A, HIR-B, and human insulin-like growth factor I receptor (HIGF-IR) in SPA-assay, respectively.
|
-
- HY-146979
-
|
hA2A/hCA XII modulator 1
|
Adenosine Receptor
Carbonic Anhydrase
|
Cancer
|
|
hA2A/hCA XII modulator 1 (compound 14), a triazolopirazine, is a potent hA2A adenosine receptor (hA2AAR) antagonist with Kis of 6.4 nM, 4.819 μM, >30 μM for hA2AAR, hA1AR, hA3AR, respectively. hA2A/hCA XII modulator 1 is a potent human carbonic anhydrase XII (hCA XII) inhibitor with Kis of 6.2 nM, 46 nM, 466 nM, 8.351 μM for hCA XII, hCA II, hCA IX and hCA I, respectively. hA2A/hCA XII modulator 1 has the potential for cancer research.
|
-
- HY-146201
-
|
PDE4B/7A-IN-1
|
Phosphodiesterase (PDE)
|
Others
|
|
1 a /5-hydroxynitrile rubber 7 receptor antagonist (5-HT1 a k i = 8 nm, kb= 0.04 nm; 5-nitrile rubber 7K I = 451 nm, kb= 460 nm) has pde4b/pde7a inhibitory activity (PDE4B ic50= 80.4 μ M; Pde7a chip 50= 151.3 μ M）。 Compound 22 has a very good ability of passive penetration of biofilm and high metabolic stability in vitro. In addition, 22's pharmacological evaluation showed its pre cognitive and antidepressant properties in rat behavioral tests.
|
-
- HY-B0109S
-
|
Dorzolamide-d5
|
Carbonic Anhydrase
|
Cancer
|
|
Dorzolamide-d5 is the deuterium labeled Dorzolamide. Dorzolamide (L671152) is a potent carbonic anhydrase II inhibitor, with IC50 values of 0.18 nM and 600 nM for red blood cell CA-II and CA-I respectively. Dorzolamide possesses anti-tumor activity[1][2].
|
-
- HY-W010452S
-
|
3-Hydroxybutyric acid-d2 sodium
β-Hydroxybutyric acid-d2 sodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
3-Hydroxybutyric acid-d2 (sodium) is the deuterium labeled 3-Hydroxybutyric acid sodium[1]. 3-Hydroxybutyric acid sodium (β-Hydroxybutyric acid sodium) is a metabolite that is elevated in type I diabetes. 3-Hydroxybutyric acid sodium can modulate the properties of membrane lipids[2].
|
-
- HY-107759
-
|
Butabindide oxalate
UCL-1397 oxalate
|
Others
|
Neurological Disease
|
|
Butabindide (UCL-1397) oxalate is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide oxalate inhibits TPP II to protect CCK-8 against inactivation.
|
-
- HY-109191A
-
|
Sovesudil hydrochloride
PHP-201 hydrochloride; AMA0076 hydrochloride
|
ROCK
|
Neurological Disease
|
|
Sovesudil (PHP-201) hydrochloride is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil hydrochloride lowers intraocular pressure (IOP) without inducing hyperemia.
|
-
- HY-13955S1
-
-
- HY-10195
-
|
Ruboxistaurin
LY333531
|
PKC
|
Metabolic Disease
|
|
Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC50 of 5.9 nM.
|
-
- HY-152257
-
|
HPK1-IN-31
|
MAP4K
|
Cancer
Inflammation/Immunology
|
|
HPK1-IN-31 (compound 5i) is an orally active hematopoietic progenitor kinase 1 (HPK1) inhibitor with an IC50 value of 0.8 nM. HPK1-IN-31 has anti-tumour activity and has great potential for immunoresearch.
|
-
- HY-13026
-
|
Idelalisib
CAL-101; GS-1101
|
PI3K
Autophagy
|
Cancer
|
|
Idelalisib (CAL-101; GS-1101) is a highly selective and orally bioavailable p110δ inhibitor with an IC50 of 2.5 nM, showing 40- to 300-fold selectivity for p110δ over other PI3K class I enzymes.
|
-
- HY-109191
-
|
Sovesudil
PHP-201; AMA0076
|
ROCK
|
Others
|
|
Sovesudil (PHP-201) is a potent, ATP-competitive, locally acting Rho kinase (ROCK) inhibitor with IC50s of 3.7 and 2.3 nM for ROCK-I and ROCK-II, respectively. Sovesudil lowers intraocular pressure (IOP) without inducing hyperemia.
|
-
- HY-10195B
-
|
Ruboxistaurin hydrochloride
LY333531 hydrochloride
|
PKC
|
Metabolic Disease
|
|
Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM.
|
-
- HY-139983
-
|
SDH-IN-1
|
Fungal
|
Infection
|
|
SDH-IN-1 (compound 4i) is a succinate dehydrogenase (SDH) inhibitor with an IC50 of 4.53 μM. SDH-IN-1 has potent antifungal activities. SDH-IN-1 displays potent activity against S. sclerotiorum (EC50 of 0.14 mg/L).
|
-
- HY-126359
-
-
- HY-13323A
-
|
CX-5461 dihydrochloride
|
DNA/RNA Synthesis
|
Cancer
|
|
CX-5461 dihydrochloride is a potent and orally bioavailable inhibitor of Pol I-mediated rRNA synthesis, with IC50s of 142 nM in HCT-116, 113 nM in A375, and 54 nM in MIA PaCa-2 cells, and shows little or no effect on Pol II (IC50 ≥25 μM).
|
-
- HY-13955S
-
-
- HY-19615B
-
|
MS023 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
MS023 dihydrochloride is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
|
-
- HY-19615
-
|
MS023
|
Histone Methyltransferase
|
Cancer
|
|
MS023 is a potent, selective, and cell-active inhibitor of human type I protein arginine methyltransferases (PRMTs) inhibitor, with IC50s of 30, 119, 83, 4 and 5 nM for PRMT1, PRMT3, PRMT4, PRMT6, and PRMT8, respectively.
|
-
- HY-148034
-
|
Plm IV inhibitor-1
|
Others
|
Infection
|
|
Plm IV inhibitor-1 (compound 6) is a potent plasmepsin IV (Plm IV) inhibitor with IC50s of 4.1, 0.80, 0.25, 0.35 µM for Plm I, Plm II, Plm IV, Cat D, respectively.
|
-
- HY-14776
-
|
Quarfloxin
CX-3543
|
DNA/RNA Synthesis
|
Cancer
|
|
Quarfloxin (CX-3543), a fluoroquinolone derivative with antineoplastic activity, targets and inhibits RNA pol I activity, with IC50 values in the nanomolar range in neuroblastoma cells. Quarfloxin disrupts the interaction between the nucleolin protein and a G-quadruplex DNA structure in the ribosomal DNA (rDNA) template.
|
-
- HY-N0191
-
-
- HY-W033577
-
|
Tricarbonyldichlororuthenium(II) dimer
CORM-2
|
Others
|
Inflammation/Immunology
|
|
Tricarbonyldichlororuthenium(II) dimer is a pharmacological donor of CO releasing. CO releases from Tricarbonyldichlororuthenium(II) dimer prevents gastric mucosal oxidative damage induced by ischemia/reperfusion (I/R) improving gastric blood flow (GBF), decreasing DNA oxidation and inflammatory response on systemic level.
|
-
- HY-N0613
-
|
Sauchinone
|
NF-κB
|
Inflammation/Immunology
|
|
Sauchinone is a diastereomeric lignan isolated from Saururus chinensis (Saururaceae). Sauchinone inhibits LPS-inducible iNOS, TNF-α and COX-2 expression through suppression of I-κBα phosphorylation and p65 nuclear translocation. Sauchinone has anti-inflammatory and antioxidant activity.
|
-
- HY-15544
-
|
CCR1 antagonist 10
|
CCR
|
Inflammation/Immunology
|
|
CCR1 antagonist 10 (example 1) is a potent and orally active CCR1 antagonist. CCR1 antagonist 10 inhibits 125I-MIP-1α binding to THP-1 cell membranes with an Ki value of 2.3 nM.
|
-
- HY-12071A
-
|
LDN193189 Tetrahydrochloride
|
TGF-β Receptor
|
Cancer
|
|
LDN193189 Tetrahydrochloride is a selective BMP type I receptor inhibitor, which efficiently inhibits ALK2 and ALK3 (IC50=5 nM and 30 nM, respectively), with weaker effects on ALK4, ALK5 and ALK7 (IC50≥500 nM).
|
-
- HY-125331
-
|
DRF-1042
|
Topoisomerase
ADC Cytotoxin
|
Cancer
|
|
DRF-1042 is an orally active derivative of Camptothecin. DRF-1042 acts to inhibit DNA topoisomerase I. DRF-1042 shows good anticancer activity against a panel of human cancer cell lines including multi-agent resistance (MDR) phenotype.
|
-
- HY-149035
-
|
PAA4
|
Others
|
Cancer
|
|
PAA4 is a methide carbon-centered polynuclear Au(I) clusters. PAA4 shows antiproliferative activity. PAA4 increases the expression of pH2AX in a time dependent manner. PAA4 shows anti-tumor effect in orthotopic bladder cancer mouse model.
|
-
- HY-110114
-
|
Gue1654
|
Others
|
Others
|
|
Gue1654 is a modulator of OXE-R. Gue1654 inhibits Gβγ but not Gα signaling triggered upon activation of Gα(i)-βγ by the chemoattractant receptor OXE-R. Gue1654 does not interfere nonspecifically with signaling directly at or downstream of Gβγ.
|
-
- HY-100530
-
|
Rp-cAMPS triethylammonium salt
|
PKA
|
Neurological Disease
|
|
Rp-cAMPS triethylammonium salt, a cAMP analog, is a potent, competitive cAMP-induced activation of cAMP-dependent PKA I and II (Kis of 12.5 µM and 4.5 µM, respectively) antagonist. Rp-cAMPS triethylammonium salt is resistant to hydrolysis by phosphodiesterases.
|
-
- HY-119608
-
|
GSK854
|
Others
|
Cardiovascular Disease
|
|
GSK854 is a potent Inhibitor of Troponin I-Interacting Kinase (TNNI3K). GSK854 is a suitable lead for identifying new cardiac medicines and have been employed as in vivo tools in investigational studies aimed at defining the role of TNNI3K within heart failure.
|
-
- HY-A0116S1
-
-
- HY-13955S2
-
-
- HY-114782
-
-
- HY-P1110
-
|
AF12198
|
Interleukin Related
|
Inflammation/Immunology
|
|
AF12198 is a potent, selective and specific peptide antagonist for human type I interleukin-1 receptor (IL1-R1) (IC50=8 nM) but not the human type II receptor (IC50=6.7 µM) or the murine type I receptor (IC50>200 µM). AF12198 inhibits IL-1-induced IL-8 production (IC50=25 nM) and IL-1-induced intercellular adhesion molecule-1 (ICAM-1) expression (IC50=9 nM) in vitro. AF12198 has anti-inflammatory activities and blocks responses to IL-1 in vivo.
|
-
- HY-136190
-
|
TRPC6-PAM-C20
|
TRP Channel
|
Neurological Disease
|
|
TRPC6-PAM-C20 is a selective positive allosteric modulator (PAM) of TRPC6 channels. TRPC6-PAM-C20 is a potent enhancer of channel activation, enabling low basal concentrations of DAG to induce activation of the ion channel. TRPC6-PAM-C20 induces increases in intracellular Ca 2+ concentrations ([Ca 2+]i) in TRPC6-expressing HEK293 cells with an EC50 of 2.37 μM. TRPC6-PAM-C20 can be used as a valuable tool to selectively exaggerate TRPC6-dependent signals.
|
-
- HY-143494
-
|
RSV/IAV-IN-3
|
RSV
Influenza Virus
|
Infection
|
|
RSV/IAV-IN-3 (compound 14'i) is a dual inhibitor of respiratory syncytial virus (RSV) and influenza A virus (IAV) with EC50 values of 2.92 µM and 1.90 µM,respectively. RSV/IAV-IN-3 has antiviral effect against H1N1 and H3N2 with EC50 values of 3.25 µM and 1.50 µM in MDCK cells, respectively. RSV/IAV-IN-3 significantly inhibits the activity of luciferase in a dose-dependent manner, with an EC50 of 3.89 µM. RSV/IAV-IN-3 inhibits IAV infectivity and RdRp activity. RSV/IAV-IN-3 inhibits IAV and RSV replication at the post-entry stage.
|
-
- HY-P2977
-
|
N-Acetylneuraminate lyase (CgNal)
Sialic acid aldolase (CgNal)
|
Endogenous Metabolite
|
Others
|
|
N-Acetylneuraminate lyase (CgNal) (Sialic acid aldolase (CgNal)) is a class I aldolase, is often used in biochemical studies. N-Acetylneuraminate lyase (CgNal) catalyzes the reversible condensation of pyruvate with N-acetyl-d-mannosamine (ManNAc) to yield the sialic acid N-acetylneuraminic acid (Neu5Ac).
|
-
- HY-P2450
-
|
Leucinostatin A
Antibiotic P168
|
Fungal
Antibiotic
|
Cancer
Infection
|
|
Leucinostatin A (Antibiotic P168) is a nonapeptide exerting a remarkable activity especially against Candida albicans and Cryptococcus neoformans. Leucinostatin A is a hydrophobic nonapeptide antibiotic. Leucinostatin A inhibits prostate cancer growth through reduction of insulin-like growth factor-I expression in prostate stromal cells. Antiprotozoal activies.
|
-
- HY-100620
-
|
RPR121056
APC
|
Topoisomerase
Cholinesterase (ChE)
|
Cancer
|
|
RPR121056 (APC) is a metabolite of Irinotecan (CPT-11), which is generated by CYP3A4. Irinotecan (CPT-11) is an antineoplastic agent that inhibits topoisomerase type I, causing cell death, and is widely used in the treatment of colorectal cancer. Irinotecan also directly inhibits AChE.
|
-
- HY-101037
-
|
Sarcosine
N-Methylglycine; Sarcosin
|
Endogenous Metabolite
GlyT
|
Cancer
|
|
Sarcosine (N-Methylglycine), an endogenous amino acid, is a competitive glycine transporter type I (GlyT1) inhibitor and N-methyl-D-aspartate (NMDA) receptor co-agonist. Sarcosine increases the glycine concentration, resulting in an indirect potentiation of the NMDA receptor. Sarcosine is commonly used for the research of schizophrenia.
|
-
- HY-100954
-
-
- HY-101535
-
|
ARP101
|
MMP
|
Cancer
|
|
ARP101 is a potent and selective inhibitor matrix metalloproteinase-2 (MMP-2). ARP101 induces autophagy-associated cell death in cancer cells. ARP101 is effective in inducing the formation of autophagosome and conversion of LC3I into LC3II.
|
-
- HY-121309S
-
|
Doxorubicinone-d3
Adriamycin aglycone-d3; Adriamycinone-d3
|
Endogenous Metabolite
|
Cancer
|
|
Doxorubicinone-d3 is the deuterium labeled Doxorubicinone. Doxorubicinone is a metabolite of an anti-cancer chemotherapy agent Doxorubicin[1]. Doxorubicin is a potent human DNA topoisomerase I and topoisomerase II inhibitor with IC50s of 0.8 μM and 2.67 μM, respectively.
|
-
- HY-147840
-
|
HDAC-IN-41
|
HDAC
|
Cancer
|
|
HDAC-IN-41 (Compound 7c) is a selective, orally active class I HDAC inhibitor with IC50 values of 0.62, 1.46 and 0.62 μM against HDAC1, HDAC2 and HDAC3, respectively. HDAC-IN-41 shows NO releasing activity.
|
-
- HY-100748
-
|
Zabadinostat
CXD101
|
HDAC
|
Cancer
|
|
Zabadinostat (CXD101) is a potent, selective and orally active class I HDAC inhibitor with IC50s of 63 nM, 570 nM and 550 nM for HDAC1, HDAC2 and HDAC3, respectively. Zabadinostat has no activity against HDAC class II. Zabadinostat has antitumor activity.
|
-
- HY-149017
-
|
Apoptosis inducer 7
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 7 (Compound 5I) induces apoptosis in cancer cells. Apoptosis inducer 7 inducrs cleavage of PARP, caspases, down-regulation of anti-apoptotic protein c-Flip and up regulation of pro-apoptotic protein Noxa. Apoptosis inducer 7 exhibits antitumor activity.
|
-
- HY-139909
-
|
CL2E-SN38
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
CL2E-SN-38, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor.
|
-
- HY-146008
-
|
hCAII-IN-3
|
Carbonic Anhydrase
|
Cancer
|
|
hCAII-IN-3 (Compound 16) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 403.8, 5.1, 10.2 and 5.2 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-2 shows anticancer activity.
|
-
- HY-12512
-
|
cGAMP
Cyclic GMP-AMP; 3',3'-cGAMP
|
STING
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-142690
-
|
HDAC-IN-27
|
HDAC
|
Cancer
|
|
HDAC-IN-27 (Compound 11h) is a potent, selective and orally active HDAC Class I inhibitor, with IC50 values ranging from 0.43 nM to 3.01 nM for HDAC1-3. HDAC-IN-27 shows anti-acute myeloid leukemia (AML) activity.
|
-
- HY-147521
-
|
Antitumor photosensitizer-3
|
Necroptosis
|
Cancer
|
|
Antitumor photosensitizer-3 (Compound I) is a chlorin derivative. Antitumor photosensitizer-3 induces tumor cells apoptosis and necrosis under 650 nm laser irradiation. Antitumor photosensitizer-3 exhibits lower skin photo-toxicity than positive reference m-THPC in vivo.
|
-
- HY-118467
-
|
Benzolamide
CL11366
|
Carbonic Anhydrase
|
Neurological Disease
|
|
Benzolamide (CL11366) is a potent carbonic anhydrase (CA) inhibitor, with Kis of 15 nM, 9 nM, 94 nM and 78 nM for hCA I, hCA II, EcoCAγ and VchCAγ, respectively. Benzolamide also inhibits CAS3, with a Ki of 54 nM. Benzolamide can be used for the research of glaucoma and seizures.
|
-
- HY-N8448
-
|
3,4-Di-O-caffeoyl quinic acid methyl ester
Macroantoin F
|
RSV
|
Infection
|
|
3,4-Di-O-caffeoyl quinic acid methyl ester (Macroantoin F) is a dicaffeoyl derivative isolated from the rhizome of Elephantopus scaber Linn. 3,4-Di-O-caffeoyl quinic acid methyl ester exhibited in vitro antiviral activity against respiratory syncytial virus (< a href=" " class="link-product" target="_blank">RSV) with an IC50 value of 0.78 μg/mL.
|
-
- HY-A0259
-
|
Floctafenine
|
COX
|
Inflammation/Immunology
|
|
Floctafenine, a nonsteroidal anti-inflammatory agent (NSAID), acts as an effective analgesic agent. Floctafenine is an inhibitor of COX-1 and COX-2 activities in vitro,showing a slightly higher potency towards COX-I. Floctafenine is used for the research of short term pain research.
|
-
- HY-50847
-
|
ZSTK474
|
PI3K
Autophagy
|
Cancer
|
|
ZSTK474 is an ATP-competitive pan-class I PI3K inhibitor with IC50s of 16 nM, 44 nM, 4.6 nM and 49 nM for PΙ3Κα, PI3Kβ, PI3Kδ and PI3Kγ, respectively.
|
-
- HY-114170
-
|
ML604440
|
Proteasome
|
Inflammation/Immunology
|
|
ML604440 is a specific and cell-permeable Proteasome β1i (LMP2) subunit inhibitor. ML604440 can be used in experimental colitis, EAE and autoimmune disease research. ML604440 shows synergistic effects and advantageous when combined with LMP7 inhibitor.
|
-
- HY-146260
-
|
NVP-CLR457
|
PI3K
|
Cancer
|
|
NVP-CLR457 (compound 40) is an orally active, potent and balanced pan-class I PI3K inhibitor. NVP-CLR457 shows a clear dose-dependent PK/PD/efficacy relationship. NVP-CLR457 has antitumor activity.
|
-
- HY-107096
-
|
CH-0793076
TP3076
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076), a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 is efficacious against cells expressing BCRP (breast cancer resistance protein).
|
-
- HY-18351
-
|
Indotecan
LMP-400; NSC-724998
|
Topoisomerase
|
Cancer
Infection
|
|
Indotecan (LMP-400), an indenoisoquinoline derivative, is a potent Topoisomerase I inhibitor, with IC50s of 300, 1200, 560 nM for P388, HCT116, MCF-7 cell lines, respectively. Indotecan prevents the relaxation of supercoiled DNA and can be used for the research of visceral leishmaniasis.
|
-
- HY-16012
-
|
Domatinostat tosylate
4SC-202
|
HDAC
Apoptosis
|
Cancer
|
|
Domatinostat tosylate (4SC-202) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
|
-
- HY-127026S
-
|
Quinaprilat-d5
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Quinaprilat-d5 is a deuterium-labeled Quinaprilat. Quinaprilat is a nonsulfhydryl ACE inhibitor, the active diacid metabolite of Quinapril. Quinaprilat specifically blocks the conversion of angiotensin I to the vasoconstrictor angiotensin II and inhibits bradykinin degradation. Quinaprilat primarily acts as a vasodilator, decreasing total peripheral and renal vascular resistance[1].
|
-
- HY-A0230
-
|
Spirapril
SCH 33844
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Spirapril is a potent and cross the blood-brain barrier angiotensin converting enzyme (ACE) inhibitor with antihypertensive activity. Spirapril competitively binds to ACE and prevents the conversion of angiotensin I to angiotensin II. Spirapril is an orally active proagent of Spiraprilat and can be used for the research of hypertension, congestive heart failure.
|
-
- HY-139909A
-
|
CL2E-SN38 TFA
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
CL2E-SN-38 TFA, a highly releasable and structurally stable antibody-SN-38-conjugate, is a part of the antibody drug conjugate (ADC). SN-38, the active metabolite of Irinotecan from camptothecins, is an Topoisomerase I inhibitor.
|
-
- HY-152138
-
|
Antituberculosis agent-8
|
Bacterial
Fungal
|
Infection
|
|
Antituberculosis agent-8 (Compound 9i) is an antitubercular agent with an MIC of 3.53 μM (1.6 μg/mL) against M. tuberculosis H37Rv. Antituberculosis agent-8 also shows good antifungal activity against A. niger with an MIC of 62.50 μM.
|
-
- HY-147270
-
|
MC-VA-PAB-Exatecan
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-VA-PAB-Exatecan is a agent-linker conjugate for ADC. MC-VA-PAB-Exatecan contains the ADC linker (peptide MC-VA-PAB) and a DNA topoisomerase I inhibitor Exatecan (HY-13631). MC-VA-PAB-Exatecan synthesized ADC shows good antitumor activity.
|
-
- HY-148029
-
|
Dazostinag disodium
TAK-676
|
STING
|
Cancer
|
|
Dazostinag disodium (TAK-676) is an agonist of STING, triggering the activation of STING signaling pathway and type I interferons. Dazostinag disodium is also a modulator of immune system, resulting complete regressions and durable memory T-cell immunity. Dazostinag disodium promotes durable IFN-dependent antitumor immunity.
|
-
- HY-125773
-
|
β-cyano-L-Alanine
Beta-cyano-l-alanine
|
Endogenous Metabolite
|
Neurological Disease
|
|
β-cyano-L-Alanine (Beta-cyano-l-alanine), a nitrile of widespread occurrence in higher plants, is enzymatically produced by cyanoalanine synthase from cyanide and cysteine as substrates. β-cyano-L-Alanine abolishes the protective effect of ethanol on cerebral ischemia/reperfusion (I/R) injury.
|
-
- HY-N4130
-
|
25S-Inokosterone
|
Others
|
Inflammation/Immunology
|
|
25S-Inokosterone is a phytoecdysone in the roots of two same species of A. bidentata Blume and A. japonica Nakai, and two different species of C. capitata Moq and C. officinalis Kuan. 25S-Inokosterone has the potential for the LPS-induced acute kidney injury research.
|
-
- HY-110385
-
|
cGAMP disodium
Cyclic GMP-AMP disodium; 3',3'-cGAMP disodium
|
STING
Endogenous Metabolite
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) disodium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-B1471
-
|
Fluorometholone acetate
|
Carbonic Anhydrase
|
Inflammation/Immunology
|
|
Fluorometholone acetate is a synthetic glucocorticoid corticosteroid and a corticosteroid ester. Fluorometholone acetate potently inhibits carbonic anhydrase (CA) with IC50s of 2.18 μM and 17.5 μM for hCA-I and hCA-II, respectively. Fluorometholone acetate has anti-inflammatory effect and has the potential for external ocular inflammation research.
|
-
- HY-P99843
-
|
Datopotamab
CDP7657
|
ADC Antibody
|
Cancer
|
|
Datopotamab (CDP7657) is an antibody targeting to TROP2. Datopotamab can be used to synthesize Datopotamab deruxtecan (HY-141598), TROP2-directed antibody-drug conjugate (ADC). Datopotamab deruxtecan consists of DNA topoisomerase I inhibitor Deruxtecan (HY-13631E) and Datopotamab.
|
-
- HY-W009783
-
|
1-Deoxymannojirimycin hydrochloride
|
HIV
Influenza Virus
|
Infection
|
|
1-Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. 1-Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor and inhibits HIV‐1 strains. 1-Deoxymannojirimycin hydrochloride has antiviral activity.
|
-
- HY-13521
-
|
SB-505124
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 is a selective inhibitor of TGF-β Receptor type I receptors (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-122958
-
|
Peucedanocoumarin III
|
α-synuclein
|
Neurological Disease
|
|
Peucedanocoumarin III is an inhibitor of α-synuclein and Huntington protein aggregates that enhances the clearance of nuclear and cytoplasmic β23 aggregates and prevents cytotoxicity induced by disease-associated proteins (i.e., mutant Huntington proteins and α-synuclein). Peucedanocoumarin III may be used in Parkinson's disease research.
|
-
- HY-146541
-
|
FGFR4-IN-10
|
FGFR
|
Cancer
|
|
FGFR4-IN-10 (compound 5a) is a potent and selective FGFR4 inhibitor with an IC50 value of 70.7 nM. FGFR4-IN-10 shows no inhibition against other FGFR family members, i.e. FGFR1, FGFR2 and FGFR3.
|
-
- HY-146007
-
|
hCAIX-IN-17
|
Carbonic Anhydrase
|
Cancer
|
|
hCA IX-IN-1 (Compound 6f) is a human carbonic anhydrase (hCA) inhibitor with Ki values of 331.4, 28.4, 9.4 and 17.8 nM against hCA I, hCA II, hCA IX and hCA XII, respectively. hCA IX-IN-1 shows anticancer activity.
|
-
- HY-148035
-
|
Plm IV inhibitor-2
|
Parasite
|
Infection
|
|
Plm IV inhibitor-2 (compound 3) is a potent digestive vacuole plasmepsins IV (Plm IV) inhibitor with IC50 values of 24 nM, 70 nM and 0.3 μM for Plm IV, II and I, respectively. Plm IV inhibitor-2 can be used to research malaria caused by Plasmodium parasites.
|
-
- HY-13982
-
|
JSH-23
|
NF-κB
|
Cancer
Metabolic Disease
Inflammation/Immunology
|
|
JSH-23 is an NF-κB inhibitor which inhibits NF-κB transcriptional activity with an IC50 of 7.1 μM in lipopolysaccharide (LPS)-stimulated macrophages RAW 264.7. JSH-23 inhibits nuclear translocation of NF-κB p65 without affecting IκBα degradation.
|
-
- HY-120234
-
|
Z-LLNle-CHO
Z-Leu-Leu-Nle-CHO; GSII
|
γ-secretase
Proteasome
Apoptosis
|
Cancer
|
|
Z-LLNle-CHO (Z-Leu-Leu-Nle-CHO) is a γ-secretase inhibitor I. Z-LLNle-CHO induces caspase and ROS-dependent apoptosis by blocking the Akt-mediated pro-survival pathway. Z-LLNle-CHO can be used in cancer research, such as breast cancer and leukaemia.
|
-
- HY-14852
-
|
Tafamidis
|
Transthyretin (TTR)
|
Neurological Disease
|
|
Tafamidis is a potent and selective transthyretin (TTR) stabilizer, shows comparable potency and efficacy to the mutumant homotetramers V30M-TTR, V122I-TTR and wild type WT-TTR, with EC50s of 2.7-3.2 μM. Tafamidis inhibits amyloidogenesis.
|
-
- HY-13687A
-
|
IKK 16 hydrochloride
|
IKK
LRRK2
|
Inflammation/Immunology
|
|
IKK 16 hydrochloride is a selective IκB kinase (IKK) inhibitor for IKK2, IKK complex and IKK1 with IC50s of 40 nM, 70 nM and 200 nM, respectively. IKK16 also inhibits leucine-rich repeat kinase-2 (LRRK2) with an IC50 of 50 nM.
|
-
- HY-16100
-
|
BI 99179
|
Fatty Acid Synthase (FASN)
|
Cancer
Metabolic Disease
|
|
BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats.
|
-
- HY-110385A
-
|
cGAMP diammonium
Cyclic GMP-AMP diammonium; 3',3'-cGAMP diammonium
|
STING
Endogenous Metabolite
|
Inflammation/Immunology
|
|
cGAMP (Cyclic GMP-AMPP) diammonium functions as an endogenous second messenger in metazoans and triggers interferon production in response to cytosolic DNA. cGAMP diammonium activates stimulator of interferon genes (STING), which activates a signaling cascade leading to the production of type I interferons and other immune mediators.
|
-
- HY-117066
-
|
CL075
3M002
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
CL075 (3M002) is a selective TLR8 agonist with immunomodulating properties. CL075 triggers a MyD88-dependent signaling pathway to elicit production of inflammatory cytokines and type I interferons (IFNs) via activation of NF-κB and IRF7, respectively.
|
-
- HY-101647
-
|
Intoplicine
RP 60475
|
Topoisomerase
|
Cancer
|
|
Intoplicine (RP 60475), an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA.
|
-
- HY-106218
-
|
Flurocitabine
5-Fluorocyclocytidine; 5'-Fluorocyclocytidine
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Flurocitabine (5-Fluorocyclocytidine) is a fluorinated anlydride analog of cytosine arabinoside, partially hydrolysecl in vivo into two active antitumor substances (arabinosyl-tluorocytosine (ara-FC) and arabinosyl-fluorouracil (ara-FU)). Flurocitabine (5-Fluorocyclocytidine) has antitumor activity during phase I studies in acute leukemia and solid tumors.
|
-
- HY-129421
-
|
PA-9
|
Others
|
Inflammation/Immunology
Neurological Disease
|
|
PA-9 is a pituitary adenylate cyclase-activating polypeptide (PACAP) type I (PAC1) receptor antagonist. PA-9 dose dependently inhibits PACAP-induced cAMP elevation with an IC50 of 5.6 nM. PA-9 can be used for the research of neuropathic and/or inflammatory pain.
|
-
- HY-P4109
-
|
vMIP-II (1-21)
NT21MP; V1 peptide
|
CXCR
|
Cancer
Inflammation/Immunology
|
|
vMIP-II (1-21) is a CXCR4 antagonist. vMIP-II has broad-spectrum interaction with CC and CXC chemokine receptors. vMIP-II (1-21) binds with CXCR4 with an IC50 value of 190 nM for competing with CXCR4 binding of 125I-SDF-1R.
|
-
- HY-13521A
-
|
SB-505124 hydrochloride
|
TGF-β Receptor
|
Cancer
|
|
SB-505124 hydrochloride is a selective inhibitor of TGF-β Receptor type I receptor (ALK4, ALK5, ALK7), with IC50s of 129 nM and 47 nM for ALK4, ALK5, respectively, but it does not inhibit ALK1, 2, 3, or 6.
|
-
- HY-16012A
-
|
Domatinostat
4SC-202 free base
|
HDAC
Apoptosis
|
Cancer
|
|
Domatinostat (4SC-202 free base) is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. It also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).
|
-
- HY-16952A
-
|
Bepridil hydrochloride hydrate
(±)-Bepridil hydrochloride hydrate; Org 5730 hydrochloride hydrate
|
Calcium Channel
|
Cardiovascular Disease
|
|
Bepridil hydrochloride hydrate ((±)-Bepridil hydrochloride hydrate) is a non-selective, long-acting Ca + channel antagonist and Na +, K + channel inhibitor, with antianginal and type I antiarrhythmic effects. Bepridil hydrochloride hydrate also acts as a cardiac Na +/Ca2 + exchange (NCX1) inhibitor. Bepridil hydrochloride hydrate can be used for the research of cardiovascular disorders.
|
-
- HY-B1099
-
|
Hycanthone
|
DNA/RNA Synthesis
Topoisomerase
Parasite
|
Infection
|
|
Hycanthone is a thioxanthenone DNA intercalator and inhibits RNA synthesis as well as the DNA topoisomerases I and II. Hycanthone inhibits nucleic acid biosynthesis and inhibits apurinic endonuclease-1 (APE1) by direct protein binding with a KD of 10 nM. Hycanthone is a bioactive metabolite of Lucanthone (HY-B2098) and has anti-schistosomal agent.
|
-
- HY-135780A
-
-
- HY-W111226
-
|
Fmoc-His(3-Me)-OH
|
Amino Acid Derivatives
Amyloid-β
|
Cardiovascular Disease
|
|
Fmoc-His(3-Me)OH derives Histidine-associating compounds with biological activity. Fmoc-His(3-Me)OH, with Fmoc-citrulline-OH, Fmoc-His(1-Me)-OH together, forms tri-peptides and shows vasodilating effect with EC50s of 2.7-4.7 mM in 1.0 mM Phenylephrine (PE)-contracted aorta rings. Fmoc-His(3-Me)OH (resin) also makes Methyl-His-Gly-Lys (His(3-Me)-Gly-Lys), thus acts as an [Ca 2+]i inhibitor. Fmoc-His(3-Me)OH methylates NAHIS02, making it unable to block the Alzheimer's Aβ channel.
|
-
- HY-A0236A
-
|
Aprindine hydrochloride
|
Potassium Channel
|
Cardiovascular Disease
|
|
Aprindine hydrochloride is a class I-b anti-arrhythmic agent and a?hERG channel blocker with an IC50 of 0.23 μM. Aprindine hydrochloride has inhibitory effects on Na +/Ca 2+ exchanger currents, which is partly responsible for their antiarrhythmic and cardioprotective effects. Aprindine hydrochloride is widely used for trial and ventricular tachyarrhythmias research research.
|
-
- HY-D0162
-
|
Malachite green oxalate
|
IKK
NF-κB
Apoptosis
|
Cancer
|
|
Malachite green oxalate is a triphenylmethane dye which can be used to detect the release of phosphate in enzymatic reactions. Malachite green oxalate is also a potent and selective inhibitor of IKBKE, and inhibits its downstream targets such as IκBα, p65 and IRF3. Malachite green oxalate exhibits antitumor activity in vitro and in vivo.
|
-
- HY-146780
-
|
TGFβRI-IN-4
|
TGF-β Receptor
|
Cancer
|
|
TGFβRI-IN-4 is a highly potent and orally active TGFβ receptor type I (TGFβRI) inhibitor, with IC50s of 44 nM and 42.5 nM for ALK5 and NIH3T3. TGFβRI-IN-4 can suppress tumor growth and tumor weight in tumor xenograft model.
|
-
- HY-50514
-
|
AT9283
|
JAK
Aurora Kinase
Bcr-Abl
FLT3
Apoptosis
Autophagy
|
Cancer
|
|
AT9283 is a multi-targeted kinase inhibitor with potent activity against Aurora A/B, JAK2/3, Abl (T315I) and Flt3 (IC50s ranging from 1 to 30 nM). AT9283 inhibits growth and survival of multiple solid tumors in vitro and in vivo.
|
-
- HY-147836
-
-
- HY-10195BS
-
|
Ruboxistaurin-d6 hydrochloride
|
PKC
|
Metabolic Disease
|
|
Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM). Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].
|
-
- HY-134723
-
|
DBCO-PEG4-GGFG-Exatecan
DBCO-PEG4-GGFG-DX8951
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
DBCO-PEG4-GGFG-Exatecan (DBCO-PEG4-GGFG-DX8951) is a agent-linker conjugate for ADC with potent antitumor activity by using DX8951 (a DNA topoisomerase I inhibitor), linked via the cleavable ADC linker DBCO-PEG4-GGFG.
|
-
- HY-147307
-
-
- HY-114233
-
|
MC-GGFG-Exatecan
MC-GGFG-DX8951
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-GGFG-Exatecan (MC-GGFG-DX8951) is a agent-linker conjugate for ADC. MC-GGFG-Exatecan is a DX8951 (a DNA topoisomerase I inhibitor) derivative with protease cleavable MC-GGFG linker. MC-GGFG-Exatecan shows antitumor activity and can be used to prepare DX8951 antibody conjugate (ADC).
|
-
- HY-10964
-
|
Vadimezan
DMXAA; ASA-404
|
STING
IFNAR
Influenza Virus
|
Cancer
Infection
|
|
Vadimezan (DMXAA; ASA-404), the tumor vascular disrupting agent (tumor-VDA), is a murine agonist of the stimulator of interferon genes (STING) and also a potent inducer of type I IFNs and other cytokines. Vadimezan has anti-influenza virus H1N1-PR8 activities.
|
-
- HY-120994A
-
|
Rp-8-CPT-cAMPS
|
PKA
|
Inflammation/Immunology
Neurological Disease
|
|
Rp-8-CPT-cAMPS, a cAMP analog, is a potent and competitive antagonist of cAMP-induced activation of cAMP-dependent PKA I and II. Rp-8-CPT-cAMPS preferentially selects site A of RI compares to site A of RII and site B of RII compares to site B of RI.
|
-
- HY-147970
-
|
Antifungal agent 34
|
Fungal
|
Infection
|
|
Antifungal agent 34 (compound 6i) is a potent antifungal agent. Antifungal agent 34 shows a potent antifungal activity against Candida albicans, with a MIC of 4 µg/mL. Antifungal agent 34 shows significant inhibition on Candida albicans hyphae and biofilm development. Antifungal agent 34 exhibits no cytotoxicity to mammalian cells.
|
-
- HY-152158
-
|
α-Glucosidase-IN-22
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-22 (compound 7i), a benzimidazole, is a potent α-glucosidase inhibitor with an IC50 of 0.64 μM. α-Glucosidase-IN-22 is a potent anti-diabetic agent and has the potential for type 2 diabetes mellitus (T2DM) research.
|
-
- HY-145909
-
|
BRD4 Inhibitor-17
|
Epigenetic Reader Domain
|
Cancer
|
|
BRD4 Inhibitor-17 (Compound 5i) is a potent inhibitor of BRD4 with an IC50 of 0.33 μM. BRD4 Inhibitor-17 plays crucial role in regulating transcription of inflammatory, proliferation and cell cycle genes. BRD4 Inhibitor-17 serves as potential antidotes for arsenicals.
|
-
- HY-P2918
-
|
Glucose 6-phosphate isomerase
GPI; Phosphoglucose Isomerase
|
Endogenous Metabolite
|
Others
|
|
Glucose 6-phosphate isomeras (GPI), i.e., phosphoglucose isomerase/phosphoglucoisomerase (PGI) or phosphohexose isomerase (PHI), is often used in biochemical studies. Glucose 6-phosphate isomeras is a highly conserved glycolytic and dimeric enzyme. Glucose 6-phosphate isomeras catalyzes the reversible isomerization of glucose-6-phosphate to fructose-6-phosphate.
|
-
- HY-120118
-
|
Metarrestin
ML246
|
DNA/RNA Synthesis
|
Cancer
|
|
Metarrestin (ML246) is an orally active, first-in-class and specific perinucleolar compartment inhibitor. Metarrestin disrupts the nucleolar structure and inhibits RNA polymerase (Pol) I transcription, at least in part by interacting with the translation elongation factor eEF1A2. Metarrestin blocks metastatic development and extends survival in mouse cancer models.
|
-
- HY-126307
-
|
Urolithin B
|
NF-κB
JNK
ERK
Akt
AMPK
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Urolithin B is one of the gut microbial metabolites of ellagitannins, and has anti-inflammatory and antioxidant effects. Urolithin B inhibits NF-κB activity by reducing the phosphorylation and degradation of IκBα, and suppresses the phosphorylation of JNK, ERK, and Akt, and enhances the phosphorylation of AMPK. Urolithin B is also a regulator of skeletal muscle mass.
|
-
- HY-P1256C
-
|
JMV 449 acetate
|
Neurotensin Receptor
|
Neurological Disease
|
|
JMV 449 acetate is a potent neurotensin receptor agonist. JMV 449 acetate shows an IC50 of 0.15 nM for inhibition of 125I-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 acetate has highly potent and long-lasting hypothermic and analgesic effects in the mouse.
|
-
- HY-B0615AS
-
|
Moricizine-d8(Hydrochloride)
EN 313-d8; Ethmosine-d8; Ethmozin-d8
|
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Moricizine-d8 (Hydrochloride) is the deuterium labeled Moricizine Hydrochloride (HY-B0615A). Moricizine Hydrochloride is an orally active Class I antiarrhythmic agent. Moricizine Hydrochloride decreases the maximum rate of phase 0 depolarization; increases rates of phase 2 and 3 repolarization, decreases action potential duration, and decreases effective refractory period[1][2].
|
-
- HY-15180
-
|
Buparlisib Hydrochloride
BKM120 Hydrochloride; NVP-BKM120 Hydrochloride
|
PI3K
Apoptosis
|
Cancer
|
|
Buparlisib Hydrochloride (BKM120 Hydrochloride) is a pan-class I PI3K inhibitor, with IC50 of 52 nM/166 nM/116 nM/262 nM for p110α/p110β/p110δ/p110γ, respectively.
|
-
- HY-P1985A
-
|
Notch 1 TFA
|
Notch
|
Cancer
Cardiovascular Disease
|
|
Notch 1 TFA (Notch homolog 1, translocation-associated) can encode a member of the NOTCH family of proteins. Members of this Type I transmembrane protein family share structural characteristics including an extracellular domain consisting of multiple epidermal growth factor-like (EGF) repeats, and an intracellular domain consisting of multiple different domain types.
|
-
- HY-16526
-
|
Pilaralisib
XL-147; SAR245408
|
PI3K
|
Cancer
|
|
Pilaralisib (XL147; SAR245408) is a potent and highly selective class I PI3Ks inhibitor with IC50s of 39 nM, 383 nM, 23 nM and 36 nM for PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ.
|
-
- HY-118091
-
|
LY191704
|
5 alpha Reductase
|
Endocrinology
|
|
LY191704, as a benzoquinolinone, is a potent, nonsteroidal, noncompetitive and selective human type I 5α-reductase inhibitor. LY191704 is a racemic mixture of the compounds LY300502 and LY300503. LY191704 may be useful in the research of human endocrine disorders associated with overproduction of dihydrotestosterone (DHT) by 5α-reductase type 1.
|
-
- HY-107096B
-
|
CH-0793076 TFA
TP3076 TFA
|
Topoisomerase
|
Cancer
|
|
CH-0793076 (TP3076) TFA, a hexacyclic camptothecin analog, is active drug and major metabolite of TP300. CH-0793076 TFA inhibits DNA topoisomerase I with an IC50 of 2.3 μM. CH-0793076 TFA is efficacious against cells expressing BCRP (breast cancer resistance protein).
|
-
- HY-101647A
-
|
Intoplicine dimesylate
RP 60475 dimesylate
|
Topoisomerase
|
Cancer
|
|
Intoplicine (RP 60475) dimesylate, an antitumor derivative in the 7H-benzo[e]pyrido[4,3-b]indole series, is a DNA topoisomerase I and II inhibitor. Intoplicine dimesylate strongly binds DNA (KA = 2 x 10 5 /M) and thereby increases the length of linear DNA.
|
-
- HY-12278
-
|
K02288
|
TGF-β Receptor
|
Others
|
|
K02288 is a potent bone morphogenetic protein (BMP) type I receptor inhibitor with IC50s of 1.8, 1.1, 6.4 nM for ALK1, ALK2 and ALK6, respectively. K02288 shows slightly weaker inhibition against ALK3 and ALK6 with IC50s of of 5-34 nM.
|
-
- HY-142922
-
|
BCR-ABL-IN-4
|
Bcr-Abl
|
Cancer
|
|
BCR-ABL-IN-4 is a BCR-ABL inhibitor with anticancer effects. BCR-ABL-IN-4 inhibits the cancer cell growth with IC50 values of 0.67 nM and 16 nM for K562 cells and BCR-ABL T315I transfected Ba/F3 cells, respectively (WO2021143927A1; compound 11).
|
-
- HY-P1256
-
|
JMV 449
|
Neurotensin Receptor
|
Neurological Disease
|
|
JMV 449 is a potent neurotensin receptor agonist. JMV 449 shows an IC50 of 0.15 nM for inhibition of [ 125I]-neurotensin binding to neonatal mouse brain and an EC50 of 1.9 nM in contracting the guinea-pig ileum. JMV 449 has highly potent and long-lasting hypothermic and analgesic effects in the mouse.
|
-
- HY-15666
-
|
Olverembatinib
GZD824; HQP1351
|
Bcr-Abl
|
Cancer
|
|
Olverembatinib (GZD824) is a potent and orally active pan-Bcr-Abl inhibitor. Olverembatinib potently inhibits a broad spectrum of Bcr-Abl mutants. Olverembatinib strongly inhibits native Bcr-Abl and Bcr-Abl T315I with IC50s of 0.34 nM and 0.68 nM, respectively. Olverembatinib has antitumor activity.
|
-
- HY-120994
-
-
- HY-122942
-
-
- HY-B1451
-
|
Imidapril hydrochloride
TA-6366
|
Angiotensin-converting Enzyme (ACE)
MMP
|
Metabolic Disease
Cardiovascular Disease
|
|
Imidapril hydrochloride (TA-6366) is an orally active angiotensin-converting enzyme (ACE) and MMP-9 inhibitor. Imidapril hydrochloride suppresses the conversion of angiotensin I to angiotensin II and thereby reduces total peripheral resistance and systemic blood pressure. Imidapril hydrochloride can be used for hypertension, type 1 diabetic, nephropathy and chronic heart failure research.
|
-
- HY-100446
-
