Search Result
Results for "
5 alpha Reductase Inhibitors
" in MedChemExpress (MCE) Product Catalog:
2660
Inhibitors & Agonists
18
Biochemical Assay Reagents
120
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-157308
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 10 (compound a8) inhibits the activity of α-Syn aggregation with low IC50 value (1.08 μM). α-Synuclein inhibitor 10 exhibits good binding affinity to α-Syn residues. α-Synuclein inhibitor 10 can be used in the research of Parkinson's disease (PD) .
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- HY-152195
-
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Apoptosis
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Cancer
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ChoKα inhibitor-5 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-5 can inhibit HChoK α1 with an IC50 value of 0.64 μM. ChoKα inhibitor-5 also can induce apoptosis. ChoKα inhibitor-5 can be used for the research of cancer .
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- HY-152191
-
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Apoptosis
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Cancer
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ChoKα inhibitor-3 is a sulphur-containing choline kinase inhibitor. ChoKα inhibitor-3 can inhibit HChoK α1 with an IC50 value of 0.66 μM. ChoKα inhibitor-3 also can induce apoptosis. ChoKα inhibitor-3 can be used for the research of cancer .
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- HY-163519
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 13 is an inhibitor of α-synuclein (α-Syn). α-Synuclein inhibitor 13 inhibits the aggregation of α-Syn proteins and is able to break down formed fibers. It is mainly used in Parkinson's disease research .
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- HY-149509
-
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 9 (Compound 20C) is an α-Synuclein inhibitor. α-Synuclein inhibitor 9 binds to cavities in mature α-synuclein fibrils and reduces the β-sheet structure. α-Synuclein inhibitor 9 inhibits A53T α-Syn aggregation. α-Synuclein inhibitor 9 has neuroprotective effect, improves brain functional connection and relieves motor dysfunction.α-Synuclein inhibitor 9 can be used for Parkinson’s disease (PD) research. .
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- HY-147644
-
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 3 (Compound 7g) is a α-synuclein (α -Syn) aggregation inhibitor. α-Synuclein inhibitor 3 can be used for Parkinson’s disease research .
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-
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- HY-171254
-
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p38 MAPK
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Inflammation/Immunology
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p38-α MAPK-IN-9 (Compound 25a) is a p38-α MAPK inhibitor (Ki: 0.057 nM). p38-α MAPK-IN-9 inhibits LPS (HY-D1056) induced TNFα production in hPBMCs (IC50: 18 nM) .
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- HY-170331
-
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IFNAR
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Inflammation/Immunology
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IFNα-IN-1 (AJ2-18) is a IFNα inhibitor that inhibits IFN-α production. IFNα-IN-1 can be used for research of inflammation .
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- HY-153329
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TNF Receptor
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Others
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TNF-α-IN-9 (compound 48) is a analog of NDM-1 inhibitor-3 (HY-150758). TNF-α-IN-9 is a TNF-α inhibitor. TNF-α-IN-9 shows low inhibitory activity .
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- HY-N7563
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EBV
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Infection
Cancer
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α-Toxicarol is a potent inhibitor of EBV.α-Toxicarol significantly inhibits mouse skin tumor in vivo. α-Toxicarol inhibits the TPA-induced EBV-EA activation .
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- HY-160436
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-
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- HY-173210
-
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Apoptosis
TNF Receptor
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Cancer
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TNF-α-IN-22 (Compound 30) is a TNFα inhibitor. It can induce Apoptosis by inhibiting the downregulation of IkBα induced by TNFα and blocking the cell cycle. TNF-α-IN-22 can be used in the research of triple-negative breast cancer .
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- HY-170381
-
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α-synuclein
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Neurological Disease
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α-syn aggregation inhibitor-1 (Compound 2e) is an inhibitor for α-syn aggregation. α-syn aggregation inhibitor-1 inhibits the cell viability of SH-SY5Y .
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- HY-152552
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 8 is an active inhibitor of α-Synuclein with an IC50 value of 2.5 µM. α-Synuclein inhibitor 8 has highly inhibition on the aggregation and disaggregation of α-Synuclein fibers. α-Synuclein inhibitor 8 reduces the formation of inclusions in neurons that can repairs damage neurons and improves Parkinson’s disease (PD)-like symptoms. α-Synuclein inhibitor 8 has high antioxidant activity and low cytotoxicity .
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- HY-172807
-
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p38 MAPK
MAPKAPK2 (MK2)
CDK
Wee1
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Cancer
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p38α inhibitor 9 (Compound 2015) is a p38α inhibitor and blocks p38α’s enzymatic activity with an IC50 lower than 20 nM. p38α inhibitor 9 inhibits MK2 T334 phosphorylation. p38α inhibitor 9 activates Cdc25b and Cdc25c and simultaneously inactivates Wee1, leading to mitotic catastrophe, aneuploidy or polyploidy and DNA damage. p38α inhibitor 9 Inhibits colorectal cancer (CRC) metastasis .
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- HY-149331
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TNF Receptor
Caspase
NF-κB
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Inflammation/Immunology
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TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor with a KD value of 12.06 μM. TNF-α-IN-11 binds to TNF-α and blocks the activation of TNF-α-trigged caspase and NF-κB signaling pathway. TNF-α-IN-11 inhibits the phosphorylation of IκBα, as well as the nuclear translocation of NF κB p65. TNF-α-IN-11 can be used for research of TNF-α-mediated autoimmune diseases .
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- HY-D2360
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HIF/HIF Prolyl-Hydroxylase
HSP
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Cancer
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O-Carboranylphenoxyacetanilide is a HIF-1α inhibitor and inhibits HIF-1α activation. O-Carboranylphenoxyacetanilide inhibits transcriptional activity of HIF in HeLa cells (IC50: 0.74 μM). O-Carboranylphenoxyacetanilide inhibits HSP60 chaperone activity and HSP60 ATPase activity .
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- HY-N10306
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α-synuclein
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Neurological Disease
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Sycosterol A is a sterol-based α-synuclein (α-syn) inhibitor that targets α-synuclein aggregates and inhibits α-synuclein aggregation. Sycosterol A can be used in the study of anti-neurodegenerative diseases .
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- HY-157806
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 12 (compound 4ce) is an inhibitor of α-Syn (α-synuclein) aggregation and can be used in the study of neurological diseases .
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- HY-163145
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α-synuclein
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Neurological Disease
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α-Synuclein inhibitor 11 (compound 1) is a selective α-synuclein (α-syn) oligomer formation inhibitor. α-Synuclein inhibitor 11 does not inhibits tau 4R (isoforms 0N4R, 2N4R) or p-tau (isoform 1N4R). α-Synuclein inhibitor 11 can be used for Parkinson's disease (PD) research .
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- HY-149635
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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HIF-1α-IN-6 (compound 3s) is a HIF-1α inhibitor with IC50 values of 0.6 and 53.3 nM observed in MiaPaCa-2 and MDA-MB-231 cells. HIF-1α-IN-6 can inhibit HIF-1α expression by decreasing the level of HIF-1α mRNA .
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- HY-144178
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- HY-N8459
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α-CBD
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EBV
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Cancer
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α-Cembrenediol is a potent inhibitor of EBV.α-Cembrenediol inhibits the early antigen of the Epstein-Bar virus. α-Cembrenediol also has anti-tumour activity .
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- HY-136735
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IRE1
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Neurological Disease
Cancer
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IRE1α kinase-IN-1 is a highly selective IRE1α (ERN1) inhibitor, with an IC50 of 77 nM. IRE1α kinase-IN-1 displays 100-fold selectivity for IRE1α over the IRE1β isoform. IRE1α kinase-IN-1 inhibits ER stress-induced IRE1α oligomerization and autophosphorylation, and also inhibits IRE1α RNase activity (IC50=80 nM) .
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- HY-113038
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(R)-2-Hydroxyglutarate; (R)-2-Hydroxyglutaric acid; (R)-2-Hydroxypentanedioic acid
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Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
Cancer
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D-α-Hydroxyglutaric acid ((R)-2-Hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid binds and inhibits ATP synthase and inhibits mTOR signaling .
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- HY-110266
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GN44028
5 Publications Verification
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers .
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- HY-14571
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E7820
4 Publications Verification
ER68203-00
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Molecular Glues
Integrin
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Cancer
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E7820 (ER68203-00), an orally active aromatic sulfonamide derivative, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium. E7820 inhibits rat aorta angiogenesis with an IC50 of 0.11 μg/ml. E7820 modulates α-1, α-2, α-3, and α-5 integrin mRNA expression. Antiangiogenic and antitumor activity .
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- HY-119593
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- HY-19949
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- HY-111507
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PDGFR
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Cancer
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PDGFRα kinase inhibitor 1 is a highly selective type II PDGFRα kinase inhibitor with IC50s of 132 nM and 6115 nM for PDGFRα and PDGFRβ, respectively .
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- HY-161469
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- HY-160433
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- HY-162799
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Choline Kinase
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Cancer
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ChoKα inhibitor-6 (compound Fa22) is a less specific ChoKα1 inhibitor with antitumor activity .
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- HY-129434A
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Bacterial
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Infection
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4aα,7α,7aα-Nepetalactone exhibits antibacterial activity, and inhibits Escherichia coli, Pseudomonas aeruginosa, Staphylococcus aureus, Salmonella typhi and Enterococcus faecalis.
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- HY-151341
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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HIF-1/2α-IN-1 is an orally active HIF-2α inhibitor. HIF-1/2α-IN-1 inhibits HIF-2α activity with an IC50 value of 0.92 μM. HIF-1/2α-IN-1 also can decrease HIF-1α levels. HIF-1/2α-IN-1 can be used for the research of clear cell renal cell carcinoma (ccRCC) .
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- HY-148863
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Calcium Channel
Monoamine Transporter
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Inflammation/Immunology
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Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain .
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- HY-148862
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Calcium Channel
Monoamine Transporter
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Inflammation/Immunology
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Cavα2δ1&NET-IN-1 (Compound 59S) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-1 inhibits Cavα2δ-1 with a Ki of 112 nM. Cavα2δ1&NET-IN-1 inhibits NET with a Ki of 383 nM and IC50 of 67 nM. Cavα2δ1&NET-IN-1 can be used for research of pain .
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- HY-18509
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IRE1
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Cancer
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IRE1α kinase-IN-2 is a potent IRE1α kinase inhibitor, with an EC50 of 0.82 μM. IRE1α kinase-IN-2 inhibits IRE1α kinase autophosphorylation (IC50=3.12 μM). IRE1α kinase-IN-2 inhibits XBP1 mRNA splicing in the WT cell lines .
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- HY-101491
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PGC-1α
Autophagy
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Metabolic Disease
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SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes.
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- HY-15438
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GSK-3
Apoptosis
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Metabolic Disease
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SB 415286 is a potent and selective cell permeable inhibitor of GSK-3α, with an IC50 of 77.5 nM, and a Ki of 30.75 nM; SB 415286 is equally effective at inhibiting human GSK-3α and GSK-3β.
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- HY-100542
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Disodium (R)-2-hydroxyglutarate
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Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
Cancer
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D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling .
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- HY-144176
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-
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- HY-171297
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- HY-13671
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HIF-1α inhibitor; LW8
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HIF/HIF Prolyl-Hydroxylase
Apoptosis
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Cancer
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LW6 (HIF-1α inhibitor) is a novel HIF-1 inhibitor with an IC50 value of 4.4 μM, and it is also an inhibitor of MDH2. LW6 decreases HIF-1α protein expression without affecting HIF-1β expression.
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- HY-148264
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- HY-N10330
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HIF/HIF Prolyl-Hydroxylase
VEGFR
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Cancer
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7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer .
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- HY-162036
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Glycosidase
Amylases
Cholinesterase (ChE)
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Neurological Disease
Metabolic Disease
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α-Amylase/α-Glucosidase-IN-7 (Compound 3f) is a competitive α-glucosidase and α-amylase enzyme inhibitor with IC50 values of 18.52 and 20.25 µM, respectively. α-Amylase/α-Glucosidase-IN-7 can also effectively inhibit AChE and BChE, with IC50 values of 9.25 and 10.06 µM respectively. α-Amylase/α-Glucosidase-IN-7 can be used in diabetes and Alzheimer’s research .
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- HY-114423
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-
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- HY-100542R
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Disodium (R)-2-hydroxyglutarate (Standard)
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Reference Standards
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
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Neurological Disease
Inflammation/Immunology
Cancer
|
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D-α-Hydroxyglutaric acid (disodium) (Standard) is the analytical standard of D-α-Hydroxyglutaric acid (disodium). This product is intended for research and analytical applications. D-α-Hydroxyglutaric acid disodium (Disodium (R)-2-hydroxyglutarate) is the principal metabolite accumulating in neurometabolic disease D-2-hydroxyglutaric aciduria. D-α-Hydroxyglutaric acid disodium is a weak competitive antagonist of α-ketoglutarate (α-KG) and inhibits multiple α-KG-dependent dioxygenases with a Ki of 10.87 mM. D-α-Hydroxyglutaric acid disodium increases reactive oxygen species (ROS) production. D-α-Hydroxyglutaric acid disodium binds and inhibits ATP synthase and inhibits mTOR signaling .
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- HY-163598
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- HY-124079
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- HY-171051
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DGK
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Others
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DGKα-IN-9 (example 298) is an inhibitor of DGKα .
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- HY-152193
-
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Apoptosis
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Cancer
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ChoKα inhibitor-4 is a bioisosteric inhibitor of HChoK α1 (IC50=0.66 μM), with inhibitory and antiproliferative effect on cancer cells. ChoKα inhibitor-4 induces apoptosis via mitochondrial pathway, and reduces anti-apoptotic proteins expression .
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- HY-149085
-
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RAR/RXR
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Cancer
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XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome .
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- HY-153002
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-
- HY-146225
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Glycosidase
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Metabolic Disease
|
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α-Amylase/α-Glucosidase-IN-2 (compound 5) is a potent α-amylase and α-glucosidase dual inhibitor with IC50 values of 13.02, 13.09 µM for α-amylase and α-glucosidase, respectively. α-Amylase/α-Glucosidase-IN-2 has the potential for the research of diabetic complications .
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- HY-18874
-
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p38 MAPK
Autophagy
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Others
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p38-α MAPK-IN-1 is an inhibitor of MAPK14 (p38-α), with IC50 of 2300 nM in EFC displacement assay, and 5500 nM in HTRF assay .
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- HY-149081
-
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Estrogen Receptor/ERR
Cytochrome P450
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Cancer
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ERα degrader 6 (Compound 31q) is an ERα degrader (KI: 75 nM). ERα degrader 6 also inhibits ARO with an IC50 of 37.7 nM. ERα degrader 6 inhibits tumor growth in MCF-7 tumor xenograft model. ERα degrader 6 can be used for breast cancer research .
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- HY-163601
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-
- HY-111387
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-
- HY-163602
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- HY-162368
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Phospholipase
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Others
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cPLA2α-IN-2 (Compound 122) is an inhibitor of cytosolic phospholipase A2α (cPLA2α) .
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- HY-163600
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- HY-161293
-
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p38 MAPK
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Cancer
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p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor .
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- HY-163599
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-
- HY-163597
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- HY-163603
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- HY-173275
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PDGFR
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Cancer
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PDGFRα kinase inhibitor 3 (Compound L7) is a highly potent inhibitor targeting the PDGFRα D842V kinase with IC50s values of 23.8 nM and 2.1 nM in biochemical and cellular assays, respectively. PDGFRα kinase inhibitor 3 binds to the ATP-binding pocket of PDGFRα D842V to block its downstream signaling pathways and inhibit kinase activity. PDGFRα kinase inhibitor 3 can be used for gastrointestinal stromal tumors (GISTs) study .
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- HY-163439
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Amylases
Glycosidase
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Metabolic Disease
|
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α-Amylase/α-Glucosidase-IN-12 (compound 10k) is a dual inhibitor targeting α-glucosidase and α-amylase with IC50 of 34.52 nM and 24.62 nM, respectively. α-Amylase/α-Glucosidase-IN-12 is an inhibitor designed based on triazolo[4,3-b][1,2,4]triazine and has the potential to be used in diabetes research .
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- HY-P5881
-
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PKC
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Cardiovascular Disease
|
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PKCα (C2-4) inhibitor peptide is a PKCα specific inhibitor peptide that blocks the inhibition of IKr by the α1A adrenoreceptor agonist A-61603 (HY-101366) .
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- HY-161522
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Glycosidase
Carbonic Anhydrase
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Endocrinology
|
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α-Glucosidase-IN-63 (Compound 4d) is an inhibitor of α-Glucosidase (IC50=0.44 μM). α-Glucosidase-IN-63 inhibits hCA II with an activity of Ki= 7.0 nM. α-Glucosidase-IN-63 is orally effective. .
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- HY-113960
-
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Estrogen Receptor/ERR
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Cancer
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ERRα antagonist-1 (Compound A) is a selective and high affinity agonist for estrogen-related receptor α (ERRα). ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC50 values are 170 nM and 180 nM, respectively .
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- HY-172622
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-
- HY-147711
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Glycosidase
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Metabolic Disease
|
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α-Amylase/α-Glucosidase-IN-1 (compound 33) is a potent α-amylase/α-glucosidase inhibitor with IC50s of 2.01, 2.09 µM for α-amylase and α-glucosidase, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has the potential of anti hyperglycemia .
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- HY-159938
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p38 MAPK
Apoptosis
Bcl-2 Family
MDM-2/p53
Caspase
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Cancer
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p38α inhibitor 6 (compound 19) is a p38α inhibitor with the IC50 of 0.68 μM. p38α inhibitor 6 induces cell apoptosis and arrests cell cycle at G0 and G2/M phase. p38α inhibitor 6 decreases the TNF-α concentration as well as increased the expression of tumor suppressor gene p53, Bax/BCL-2 ratio and caspase 3/7 .
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- HY-18371
-
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HIF/HIF Prolyl-Hydroxylase
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Inflammation/Immunology
|
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TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ? 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression .
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- HY-168961
-
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Amylases
Glycosidase
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Metabolic Disease
|
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α-Amylase/α-Glucosidase-IN-18 (Compound 9g) is the inhibitor for α-Amylase and α-Glucosidase with IC50 of 49.17 nM and 10.71 nM. α-Amylase/α-Glucosidase-IN-18 can be used in research of type 2 diabetes mellitus .
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- HY-162287
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-
- HY-162286
-
-
- HY-18370
-
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HIF/HIF Prolyl-Hydroxylase
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Cancer
|
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HIF-2α-IN-3, an allosteric inhibitor of hypoxia inducible factor-2α (HIF-2α), exhibits an IC50 of 0.4 µM and a KD of 1.1 µM. Anticancer agent .
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- HY-114573
-
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IKK
Interleukin Related
TNF Receptor
RIP kinase
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Others
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TNF-α-IN-19 is an inhibitor of TNFα that can block the interaction between TNFαRI, TRADD, and RIP1, the EC50 values for TNFα, IL-1β, and IL-1β/TNFα are 2.451, 3.792 and 1.54 μM, respectively. TNF-α-IN-19 only inhibits the degradation of IκBα when cells are stimulated by TNFα and not by IL-1β .
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- HY-125840
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PT2977; MK-6482
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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Belzutifan (PT2977) is an orally active and selective HIF-2α inhibitor with an IC50 of 9 nM. Belzutifan, as a second-generation HIF-2α inhibitor, increases potency and improves pharmacokinetic profile. Belzutifan is a potential treatment for clear cell renal cell carcinoma (ccRCC) .
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- HY-U00459
-
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IRE1
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Cancer
|
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GSK2850163 is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
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- HY-U00459B
-
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IRE1
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Cancer
|
|
GSK2850163 hydrochloride is a novel inhibitor of inositol-requiring enzyme-1 alpha (IRE1α) which can inhibit IRE1α kinase activity and RNase activity with IC50s of 20 and 200 nM, respectively.
|
-
- HY-145419
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-4 (compound 6) is a potent IRE1α inhibitor with an Ki of 140 nM. IRE1α kinase-IN-4 is the ATP-competitive ligands of IRE1α .
|
-
- HY-B0141AS
-
|
Alfatradiol-d3; Epiestradiol-d3; Epiestrol-d3
|
5 alpha Reductase
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Alpha-Estradiol-d3 is the deuterium labeled Alpha-Estradiol. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
|
-
- HY-112535
-
-
- HY-145420
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-5 (compound 7) is a potent IRE1α inhibitor with an Ki of 98 nM. IRE1α kinase-IN-5 is the ATP-competitive ligands of IRE1α .
|
-
- HY-145418
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-3 (compound 2) is a potent IRE1α inhibitor with an Ki of 480 nM. IRE1α kinase-IN-3 is the ATP-competitive ligands of IRE1α .
|
-
- HY-P10223
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CRVIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 65 and 123 μM, respectively .
|
-
- HY-116836
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38α inhibitor 7 (compound 1) is an effective p38α inhibitor with oral efficacy and generally favorable pharmacokinetic properties .
|
-
- HY-100735
-
-
- HY-147668
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 6 (compound 3ge) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.70 μM and inhibition ratio at 30 μM of 94.4% .
|
-
- HY-12836
-
|
|
IFNAR
|
Inflammation/Immunology
|
|
IFN alpha-IFNAR-IN-1 is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR; inhibit MVA-induced IFN-α responses by BM-pDCs (IC50=2-8 uM).
|
-
- HY-147666
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2% .
|
-
- HY-147669
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 7 (compound 3gf) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.95 μM and inhibition ratio at 30 μM of 85.8% .
|
-
- HY-107532
-
|
NN-DNJ; Nonyl-DNJ
|
Glycosidase
|
Metabolic Disease
|
|
N-Nonyldeoxynojirimycin (NN-DNJ) is a potent inhibitor of alpha-glucosidase and alpha-1,6-glucosidase (IC50s, 0.42, 8.4 μM, respectively), inhibits glycogen breakdown .
|
-
- HY-147667
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.22 μM and inhibition ratio at 30 μM of 94.3% .
|
-
- HY-N8745
-
|
|
Fungal
|
Others
|
|
α-Peltatin is an aryl lignan. α-Peltatin has anticancer and antifungal activity. α-Peltatin inhibits DNA topoisomerase and tubulin polymerization .
|
-
- HY-153330
-
-
- HY-B0141AS1
-
-
- HY-N0127
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
Yohimbine hydrochloride is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.
|
-
- HY-162634
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-15 (compound 6C) is an oral bioactive inhibitor of α-Glucosidase and α-amylase, with the IC50s of 21 μM and 61 μM, respectively .
|
-
- HY-151466
-
|
|
HIF/HIF Prolyl-Hydroxylase
Monoamine Oxidase
|
Cancer
|
|
HIF-1α-IN-5 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-5 also inhibits MAO-A activity. HIF-1α-IN-5 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-5 can be used in the research of cancer .
|
-
- HY-15672
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Neurological Disease
Cancer
|
|
FM19G11 is a hypoxia-inducible factor-1-alpha (HIF-1α) inhibitor, and it inhibits hypoxia-induced luciferase activity with an IC50 of 80 nM in HeLa cells. FM19G11 modulates other signaling pathways, including mTOR and PI3K/Akt/eNOS, when the HIF-1α pathway is inactivated under normoxic conditions .
|
-
- HY-154972
-
|
|
Glycosidase
Amylases
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-3 (Compound 17) is an α-Amylase/α-Glucosidase dual inhibitor, with IC50s of 0.70 μM and 1.10 μM. α-Amylase/α-Glucosidase-IN-3 can be used for research of type-II diabetes mellitus .
|
-
- HY-149557
-
|
|
Glycosidase
Amylases
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-5 (compound 4l) is a dual inhibitor of α-glucosidase (Glucosidase) and α-amylase (Amylases) with IC50s of 5.96 μM and 1.62 μM, respectively. α-Amylase/α-Glucosidase-IN-4 has potential antidiabetic activity .
|
-
- HY-162673
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-16 (compound 15) is a potent dual inhibitor of α-amylase and α-Glucosidase with IC50 values of 0.8 and 1.2 μM, respectively. α-Amylase/α-Glucosidase-IN-16 can be used in the study of diabetes mellitus (DM) .
|
-
- HY-156380
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-6 (compound 5j) is a potent dual inhibitor of α-amylase and α-glucosidase, with IC50s of 17.0 and 40.1 µM, respectively. α-Amylase/α-Glucosidase-IN-6 exhibits anti-hyperglycemic activities .
|
-
- HY-155241
-
|
|
Glycosidase
Amylases
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-4 (compound 5) is a dual inhibitor of α-glucosidase (Glucosidase) and α-amylase (Amylases) with IC50s of 0.15 μM and 1.10 μM, respectively. α-Amylase/α-Glucosidase-IN-4 has potential antidiabetic activity .
|
-
- HY-14412
-
|
|
p38 MAPK
|
Cancer
|
|
p38α inhibitor 4 (compound 10) is a selective and allosteric p38α inhibitor with an IC50 value of 1.2 μM. p38α inhibitor 4 exhibits no activity against p38β, p38γ, and p38δ .
|
-
- HY-W013407
-
|
|
Tyrosine Hydroxylase
Thyroid Hormone Receptor
|
Neurological Disease
|
|
α-Methyltyrosine methyl ester hydrochloride is an orally active and competitive tyrosine hydroxylase inhibitor. α-Methyltyrosine methyl ester hydrochloride can inhibit the conversion of tyrosine to dopamine. α-Methyltyrosine methyl ester hydrochloride causes kidney damage and urethral calculi in rats. α-Methyltyrosine methyl ester hydrochloride can be used as a tool for sympathetic nervous system research .
|
-
- HY-149886
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-9 (compound 35r) is an inhibitor ofHIF-2α. HIF-2α-IN-9 inhibits VEGF-A (IC50=305 nM), and regulates growth-promoting genes in tumor cells, reactivates macrophage-mediated tumor immunity .
|
-
- HY-P10222
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CRLLIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 14.5 and 10.2 μM, respectively .
|
-
- HY-P10221A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Cyclo CKLIIF is a dual inhibitor for hypoxia inducible factor (HIF) 1 and 2, which disrupts the interaction of both HIF1-α and HIF2-α with HIF1-β, with affinity for HIF1-α and HIF2-α PAS-B domains KD of 2.6 and 2.2 μM, respectively .
|
-
- HY-155344
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-38 (Compound 11j) is a potent inhibitor of α-glucosidase inhibitor with IC50 of 12.44±0.38 μM.α-Glucosidase-IN-38 plays an important role in Diabetes mellitus (DM) .
|
-
- HY-161355
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-9 (compound 5h) is a dual inhibitor for both α-amylase (IC50 = 16.4 μM) and α-glucosidase (IC50 = 31.6 μM) enzymes .
|
-
- HY-N0127R
-
|
|
Adenosine Receptor
|
Endocrinology
|
|
Yohimbine Hydrochloride Standard is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.
|
-
- HY-138871
-
-
- HY-152473
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-6 (Compound 47d) is an inhibitor of DNA topoisomerase IIα/β. Topoisomerase IIα-IN-6 inhibits human topoisomerase IIα and human topoisomerase IIβ with IC50 values of 0.67 µM and 0.55 µM, respectively. Topoisomerase IIα-IN-6 has stable metabolism .
|
-
- HY-W019838
-
-
- HY-B0141AR
-
|
Alfatradiol(Standard); Epiestradiol(Standard); Epiestrol (Standard)
|
5 alpha Reductase
Endogenous Metabolite
Bacterial
|
Inflammation/Immunology
|
|
Alpha-Estradiol (Standard) is the analytical standard of Alpha-Estradiol. This product is intended for research and analytical applications. Alpha-Estradiol is a weak estrogen and a 5α-reductase inhibitor which is used as a topical medication in the treatment of androgenic alopecia.
|
-
- HY-162635
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-14 (compound 6E) is an oral bioactive inhibitor of α-amylase and α-glucosidase, with the IC50s of 45.53 μM and 27.73 μM, respectively .
|
-
- HY-142618
-
-
- HY-146032
-
-
- HY-146268
-
|
|
CaMK
|
Neurological Disease
|
|
CaMKIIα-IN-1 (Compound 4d) is an orally active Ca 2+/calmodulin-dependent protein kinase II α (CaMKIIα) inhibitor with a KD of 219 nM for CaMKIIα WT hub. CaMKIIα-IN-1 has good metabolic stability .
|
-
- HY-123076
-
|
PFN-α
|
MDM-2/p53
|
Neurological Disease
|
|
Pifithrin-α, p-Nitro, Cyclic (PFN-α) is cell-permeable and active-form p53 inhibitor. Pifithrin-α, p-Nitro, Cyclic is one order magnitude more active than Pifithrin-α in protecting cortical neurons exposed to Etoposide (ED50=30 nM). Pifithrin-α, p-Nitro, Cyclic behaves as a p53 posttranscriptional activity inhibitor. Pifithrin-α, p-Nitro, Cyclic do not prevent p53 phosphorylation on the S15 residue .
|
-
- HY-172211
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
Cancer
|
|
α-Amylase/α-Glucosidase-IN-17 (Compound 3) is an inhibitor of α-amylase and α-glucosidase, with IC50 values of 14.61 μM and 25.38 μM, respectively. α-Amylase/α-Glucosidase-IN-17 has certain inhibitory activity against A549 cancer cells. α-Amylase/α-Glucosidase-IN-17 has anti-tumor and anti-diabetic effects .
|
-
- HY-139043
-
|
|
Integrin
|
Inflammation/Immunology
|
|
6-B345TTQ is an α4 integrin inhibitor that inhibits α4-Leupaxin interaction. 6-B345TTQ can be used in inflammation research .
|
-
- HY-142659
-
|
|
IRE1
|
Cancer
|
|
IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.
|
-
- HY-157537
-
-
- HY-146752
-
|
|
Amylases
|
Others
|
|
α-Amylase-IN-1 is a potent α-amylase inhibitor with an IC50 of 4.46 μM .
|
-
- HY-U00376
-
-
- HY-70073
-
-
- HY-146424
-
-
- HY-12867
-
-
- HY-148860
-
|
HIF-2α-IN-8
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-8 is a potent and orally active HIF2α inhibitor with IC50 values of 9, 37, 246 nM for HIF2α SPA, HIF2α iScript, HIF2α HRE RGA, respectively. HIF-2α-IN-8 shows antitumor activity .
|
-
- HY-P3976
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is a blood pressure lowering peptide containing 4 amino acids. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine is an angiotensin-converting Enzyme (ACE) inhibitor. Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine can be used in research of high blood pressure .
|
-
![Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine](//file.medchemexpress.com/product_pic/hy-p3976.gif)
- HY-151344
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1/2α-IN-2 is an inhibitor of HIF-1/2α. HIF-1/2α-IN-2 decrease HIF-1/2α levels and induces iron starvation response by targeting Iron Sulfur Cluster Assembly 2 (ISCA2) .
|
-
- HY-136748
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-4 is a potent inhibitor of hypoxia inducible factor-2α (HIF-2α) translation, with an IC50 of 5 μM. HIF-2α-IN-4 decreases both constitutive and hypoxia-induced HIF-2α protein expression. HIF-2α-IN-4 links its 5'UTR iron-responsive element to oxygen sensing .
|
-
- HY-162364
-
|
|
p38 MAPK
|
Neurological Disease
|
|
p38-α MAPK-IN-7 (compound 4) is a p38α-MAPK inhibitor with an IC50 value of 98.7 nM. p38-α MAPK-IN-7 protects neuronal cells from dexamethasone-induced ROS production .
|
-
- HY-P5158
-
|
|
Adrenergic Receptor
|
Others
|
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
-
- HY-P5921
-
|
TsTx-Kα
|
Potassium Channel
|
Neurological Disease
|
|
Tityustoxin-Kα (TsTx-Kα) is an inhibitor of potassium voltage-gated channels. Tityustoxin-Kα shows a dose-dependent block of the sustained outward current in cultured hippocampal neurons .
|
-
- HY-N0242
-
|
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Inflammation/Immunology
Cancer
|
|
Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .
|
-
- HY-158826
-
|
RO 707179
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
EZN-2968 is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968, inhibits tumor cell growth.
|
-
- HY-158826A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
EZN-2968 sodium is an antisense oligonucleotide that specifically binds and inhibits the expression of HIF-1α mRNA. EZN-2968 sodium, inhibits tumor cell growth.
|
-
- HY-162390
-
|
|
Amylases
Glycosidase
|
Endocrinology
|
|
α-Amylase/α-Glucosidase-IN-11 (Compound 5d) is a isoxazolidine-isatin hybrid with significant antidiabetic activity. α-Amylase/α-Glucosidase-IN-11 competitively inhibits α-amylase (IC50 = 30.39 μM) and α-glucosidase (IC50 = 65.1 μM), two key digestive enzymes. α-Amylase/α-Glucosidase-IN-11 does not cross the blood-brain barrier .
|
-
- HY-162169
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-8 (Compound 7p) is a potent dual inhibitor of α-amylase and α-glucosidase, with IC50s of 10.19 and 10.33 μM, respectively. α-Amylase/α-Glucosidase-IN-8 has good anti-oxidant activity(IC50 = 14.93 μM). α-Amylase/α-Glucosidase-IN-8 can be used for the research of diabetes .
|
-
- HY-107850A
-
|
Allopregnanediol
|
GnRH Receptor
|
Endocrinology
|
|
5α-Pregnane-3α,20α-diol (Allopregnanediol) is a derivative of progesterone and is one of the various steroids secreted by the ovaries of rats. 5α-Pregnane-3α,20α-diol can significantly stimulate the release of luteinizing hormone (LH) in castrated rats that have been pre-treated with estrogen, while simultaneously inhibiting the secretion of follicle-stimulating hormone (FSH) .
|
-
- HY-N9699
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
8α-Hydroxyhirsutinolide is a sesquiterpene lactone. 8α-Hydroxyhirsutinolide inhibits TNF-α-induced NF-κB activity (IC50: 1.9 μM) and NO production. 8α-Hydroxyhirsutinolide can be isolated from Vernonia cinerea .
|
-
- HY-134471
-
|
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
TNF-α-IN-2 is a potent and orally active inhibitor of tumor necrosis factor alpha (TNFα), with an IC50 of 25 nM in the HTRF assay. TNF-α-IN-2 distorts the TNFα trimer upon binding, leading to aberrant signaling when the trimer binds to TNFR1. TNF-α-IN-2 can be used for the research of rheumatoid arthritis .
|
-
- HY-113038AS
-
|
2-Hydroxyglutarate-13C5 disodium; 2-Hydroxyglutaric acid-13C5 sodium; 2-Hydroxypentanedioic acid-13C5 disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) sodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid sodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-161782
-
|
|
Amylases
|
Metabolic Disease
|
|
α-Amylase-IN-7 (Compound 6e) is an inhibitor for α-Amylase with an IC50 of 40 μM. α-Amylase-IN-7 exhibits potential as an antidiabetic agent .
|
-
- HY-160437
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-16 is a potent TNFα inhibitor with an IC50 of <0.6 μM. TNF-α-IN-16 has antiinflammatory properties (WO2001072735A2; example 18) .
|
-
- HY-N11512
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-24 (Compound 13) is an α-Glucosidase inhibitor with an IC50 of 451 μM. α-Glucosidase-IN-24 can be isolated from Swertia kouitchensis .
|
-
- HY-160434
-
-
- HY-155372
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-39 is a potent inhibitor of α-glucosidase enzyme with an IC50 of 869.06 ppm. α-Glucosidase-IN-39 can used in study antidiabetic .
|
-
- HY-115978
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-2 (compound 5d) is a potent α-Glucosidase inhibitor with an IC50 of 9.48 µM. α-Glucosidase-IN-2 is an antidiabetic agent .
|
-
- HY-168644
-
-
- HY-163840
-
|
|
GDNF Receptor
|
Neurological Disease
|
|
GFRα2/3-IN-1 (Compound 16) is a selective GFRα2/3 inhibitor with IC50 values of 0.1 and 0.2 μM for GFRα2 and GFRα3, respectively. GFRα2 is a glial cell line-derived neurotrophic factor (GDNF) receptor related to GFRα1, GFRα2/3-IN-1 can be used for pain and itch research .
|
-
- HY-146156
-
-
- HY-12710
-
|
α-Yohimbine; Corynanthidine; Isoyohimbine
|
Adrenergic Receptor
|
Cancer
|
|
Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis .
|
-
- HY-P10265
-
|
|
Melanocortin Receptor
|
Others
|
|
Melanostatin, frog is an inhibitor for α-melanocyte-stimulating hormone (α-MSH) release, with an IC50 of 60 nM .
|
-
- HY-150960
-
-
- HY-B0141A
-
-
- HY-17537
-
|
|
IRE1
|
Cancer
|
|
APY29, an ATP-competitive inhibitor, is an allosteric modulator of IRE1α which inhibits IRE1α autophosphorylation by binding to the ATP-binding pocket with IC50 of 280 nM. APY29 acts as a ligand that allosterically activates IRE1α adjacent RNase domain .
|
-
- HY-115351
-
|
|
TNF Receptor
MMP
|
Inflammation/Immunology
|
|
GW-3333 is a potent and orally active TNF-alpha-converting enzyme (TACE) and matrix metalloproteinases (MMP) inhibitor. GW-3333 inhibits tumor necrosis factor-alpha (TNF-alpha) production. GW-3333 can be used in research of arthritis .
|
-
- HY-161764
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-67 (compound 5k) is a potent α-Glucosidase inhibitor with IC50 values of 0.31, 4.51 µM for alpha-glucosidase and alpha-amylase, respectively. α-Glucosidase-IN-67 has the potential for the research of type-2 diabetes .
|
-
- HY-114791
-
|
|
nAChR
|
Neurological Disease
|
|
Lobelanidine is an antagonist for nicotinic acetylcholine receptor (nAChR), which inhibits α7 nAChR response and α3β2/α3β4 nAChR responses, with IC50 of 2.8 and 8.2 μM .
|
-
- HY-149668
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-41 (compound 5o) is a potent α-glucosidase inhibitor. α-Glucosidase-IN-41 can arise the changed secondary structure of α-Glu to hinder enzyme catalytic activity. α-Glucosidase-IN-41 can be used for diabetes mellitus research .
|
-
- HY-163370
-
-
- HY-147813
-
-
- HY-N3002R
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
α-Arbutin (Standard) is the analytical standard of α-Arbutin. This product is intended for research and analytical applications. α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is emerging as popular and effective skin whiteners, acting as tyrosinase inhibitor .
|
-
- HY-169283
-
|
|
Carbonic Anhydrase
|
Metabolic Disease
|
|
α-Glycosidase-IN-2 (compound 8b) is a α-Glycosidase inhibitor with the Ki values of 74.16 nM and 6.09 nM for aldose reductase and α-glycosidase,respectively. α-Glycosidase-IN-2 can be used for study of
diabetes mellitus .
|
-
- HY-163660
-
|
|
Carbonic Anhydrase
|
Infection
|
|
Carbonic anhydrase inhibitor 23 (compound 40) is a potent inhibitor of carbonic anhydrase (CA), with the Ki of 617.2 nM and 434.1 nM for hCA I (α) and hCA II (α), respectively .
|
-
- HY-124647
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-1 is a PI3Kα inhibitor (IC50 < 0.5 nM), and also inhibits mTOR (IC50: 104 nM) .
|
-
- HY-149579
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-36 (compound 5g) is a potent α-glucosidase inhibitor, with an IC50 of 6.69 ± 0.18 μM, Ki and Kis of 1.65 μM and 4.54 μM, respectively. α-Glucosidase-IN-36 may inhibit α-glucosidase activity by binding with its active site as well as changing the secondary structure of α-glucosidase. α-Glucosidase-IN-36 can be used for type 2 diabetes mellitus (T2DM) research .
|
-
- HY-169406
-
|
|
Glycosidase
|
Cancer
|
|
α-Glucosidase-IN-76 (Compound 4r) is an inhibitor for α-glucosidase with an IC50 of 5.44 μM. α-Glucosidase-IN-76 scavenges ABTS+ free radicals with a TEAC value of 0.49. α-Glucosidase-IN-76 inhibits the proliferation of T24 bladder cancer cell with IC50 of 1.74 μM .
|
-
- HY-153017
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1 inhibitor-4 is a HIF-1 inhibitor (IC50: 560 nM). HIF-1 inhibitor-4 reduces the HIF-1α protein level without affecting its mRNA level .
|
-
- HY-170557
-
|
|
Topoisomerase
Apoptosis
Mitochondrial Metabolism
|
Cancer
|
|
Topoisomerase IIα-IN-10 (Compound 13r) is an inhibitor of Topoisomerase IIα. It binds to the active site of DNA when complexed with Topoisomerase IIα, and this binding is stabilized through interactions with DNA base pairs and amino acid residues. Topoisomerase IIα-IN-10 can induce Apoptosis by intercalating DNA and inhibiting Topoisomerase IIα, thereby disrupting the mitochondrial membrane potential and inhibiting the growth of HCT116 cell lines, with an IC50 of 4.37 μM against HCT116 cells. Topoisomerase IIα-IN-10 can be used for research in the field of cancer treatment .
|
-
- HY-170027
-
|
|
HIF/HIF Prolyl-Hydroxylase
AMPK
|
Cancer
|
|
LW1564 is an inhibitor for HIF-1α with an IC50 of 1.2 µM in HepG2. LW1564 inhibits mitochondrial respiration, reduces ATP production, stimulates HIF-1α degradation, and inhibits proliferation of various cancer cells with GI50 of 0.4-4.6 μM. LW1564 activates AMPK signaling pathway and inhibits lipid synthesis. LW1564 exhibits antitumor in HepG2 xenograft mouse model .
|
-
- HY-129113R
-
|
|
COX
|
Inflammation/Immunology
|
|
α-Chaconine (Standard) is the analytical standard of α-Chaconine. This product is intended for research and analytical applications. α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects .
|
-
- HY-113038B
-
|
2-Hydroxyglutarate; 2-Hydroxyglutaric acid; 2-Hydroxypentanedioic acid
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-P99153
-
|
MORAb-003
|
Antibiotic
|
Cancer
|
|
Farletuzumab (MORAb-003) is a potent folate receptor-alpha (FRα) inhibitor. Farletuzumab is a humanized monoclonal antibody with high affinity for FRα. Farletuzumab possesses growth-inhibitory functions on cells overexpressing FRα. Farletuzumab can be used in research of cancer .
|
-
- HY-113269
-
|
|
Drug Metabolite
|
Others
|
|
alpha-CEHC is a water-soluble metabolite of alpha-tocopherol (α-TOH) with potential antioxidant activity. alpha-CEHC slightly inhibits macrophage-induced low-density lipoprotein (LDL) oxidation, and its inhibitory potency is concentration-dependent .
|
-
- HY-158196
-
|
|
PERK
Apoptosis
|
Cancer
|
|
PERK/eIF2α activator 1 (compound V8) is a flavonoid with an anti-tumor activity. PERK/eIF2α activator 1 induces apoptosis and activates the PERK-eIF2α-ATF4 pathway. PERK/eIF2α activator 1 inhibits HepG2 cell proliferation with an IC50 value of 23 μM .
|
-
- HY-147823
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-6 (compound 18) is a competitive α-glucosidase inhibitor with an IC50 of 5.69 µM. α-Glucosidase-IN-6 has anti-diabetic potential .
|
-
- HY-170866
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-81 (Compound 5) is a potent α-Glucosidase inhibitor with an IC50 value of 5.30 μM. α-Glucosidase-IN-81 is promising for research of diabetes .
|
-
- HY-137144
-
|
ZB716
|
Estrogen Receptor/ERR
|
Cancer
|
|
Fulvestrant-3-boronic acid is an orally active ERα inhibitor, which binds to ERα competitively (IC50 = 4.1 nM) and effectively degrades ERα in breast cancer cells .
|
-
- HY-157488
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-46 is a potent α-glucosidase inhibitor with an IC50 of 26.0 μM. α-Glucosidase-IN-46 can be used for the research of type 2 diabetes .
|
-
- HY-N4275
-
|
|
Others
|
Cancer
|
|
Oleaside A is a polar cardenolide monoglycoside isolated from Nerium oleander, inhibits the induction of ICAM-1 induced by IL-1α and TNF-α, and has anti-tumor activity .
|
-
- HY-161318
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-52 (Compound 3h) is an α-glucosidase inhibitor with an IC50 of 2.8 μM. α-Glucosidase-IN-52 can be used for diabetes research .
|
-
- HY-115903A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-2 hydrochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation .
|
-
- HY-101491S
-
|
|
Isotope-Labeled Compounds
PGC-1α
Autophagy
|
Metabolic Disease
|
|
SR-18292-d9 is the deuterium labeled SR-18292 (HY-101491). SR-18292 is a PPAR gamma coactivator-1α (PGC-1α) inhibitor, which increases PGC-1α acetylation, suppresses gluconeogenic gene expression and reduces glucose production in hepatocytes .
|
-
- HY-116379
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
RS-100329 is an α1-adrenergic receptor (α1-AR) antagonist that effectively inhibits α1-adrenergic receptor-mediated contractions of lower urinary tract tissues in vitro and in vivo. RS-100329 can be used in the research of symptoms related to benign prostatic hyperplasia .
|
-
- HY-N12399
-
|
|
PKA
|
Inflammation/Immunology
|
|
Aplithianines A is a potent inhibitor against J-PKAcα with an IC50 of 1 μM , and inhibits wild-type PKA with an IC50 of 84 nM. Aplithianines A inhibits J-PKAcα catalytic activity by competitively binding to the ATP pocket .
|
-
- HY-162395
-
-
- HY-150959
-
-
- HY-B0194A
-
-
- HY-150961
-
-
- HY-145940
-
|
BRD3727
|
Casein Kinase
|
Cancer
|
|
BAY-204 is an inhibitor of Casein kinase 1 alpha and delta (CSNK1α and δ) useful for the research of proliferative disorders.
|
-
- HY-111376
-
-
- HY-B0194
-
-
- HY-162262
-
-
- HY-172195
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
FS-694 is the inhibitor for p38α with an IC50 of 0.2 nM. FS-694 inhibits the TNFα release in human whole blood with an IC50 of 35.0 nM .
|
-
- HY-150560
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-11 is a highly permeable competitive α-glucosidase inhibitor with the IC50 value of 0.56 μM. α-Glucosidase-IN-11 binds to Trp residues in α-glucosidase and regulates protein folding. α-Glucosidase-IN-11 can be used to regulate blood glucose levels .
|
-
- HY-156435
-
|
|
α-synuclein
|
Neurological Disease
|
|
tau protein/α-synuclein-IN-1 is a dual inhibitor of tau protein and α-synuclein. tau protein/α-synuclein-IN-1 reduces α-syn inclusions development in M17D neuroblastoma cells. tau protein/α-synuclein-IN-1 can be used in study Alzheimer’s disease .
|
-
- HY-171295
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38 Kinase inhibitor 7 (Comp:XXXIX) is the inhibitor for p38α with an IC50 of 5.25 nM. p38 Kinase inhibitor 7 inhibits TNFα production in cell THP-1 with an IC50 of 5.88 nM .
|
-
- HY-100047
-
|
|
Taste Receptor
|
Others
|
|
Nα,Nα-Bis(carboxymethyl)-L-lysine is a competitive inhibitor of bitter taste receptor 4, with an IC50 of 59 nM. Nα,Nα-Bis(carboxymethyl)-L-lysine can be used in bitter receptors related study .
|
-
- HY-113062
-
|
20-OH-P
|
Endogenous Metabolite
Cytochrome P450
|
Endocrinology
Cancer
|
|
20α-Dihydroprogesterone is the metabolite of Progesterone (HY-N0437). 20α-Dihydroprogesterone inhibits cell proliferation and migration in breast tissue. 20α-Dihydroprogesterone inhibits aromatase in cell MCF-7aro with IC50 about 5 μM .
|
-
- HY-160435
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-14 is a potent and selective TNFα inhibitor with an IC50 value of 1.1 µM. TNF-α-IN-14 shows antiinflammatory properties (WO2001072735A2; compound 12) .
|
-
- HY-147718
-
|
|
Glutaminase
|
Metabolic Disease
|
|
α-Glucosidase-IN-5 (compound 8) is a potent α-glucosidase inhibitor with an IC50 of 57.9 µM. α-Glucosidase-IN-5 has the potential for the research of diabetes mellitus .
|
-
- HY-151142
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-18 (7B) is an orally active α-glucosidase inhibitor with an IC50 value of 3.96 μM. α-Glucosidase-IN-18 has antidiabetic activity .
|
-
- HY-156576
-
|
|
DGK
|
Cancer
|
|
DGKα-IN-6 is a DGKα inhibitor with the IC50 of 1.377 nM, extracted from patent WO2022271650 (compound 143). DGKα-IN-6 has the potential for cancer study.
|
-
- HY-156577
-
|
|
DGK
|
Cancer
|
|
DGKα-IN-7 is a DGKα inhibitor with the IC50 of 6.225 nM, extracted from patent WO2022271684 (compound 100). DGKα-IN-7 has the potential for cancer study.
|
-
- HY-N11477
-
|
|
Glycosidase
|
Metabolic Disease
|
|
(2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid is a saponin that can be isolated from Rubus ellipticus var. obcordatus. (2α,3β,4α)-2,3,19-Trihydroxyurs-12-ene-23,28-dioic acid inhibits α-Glucosidase with an IC50 of 1.68 mM .
|
-
- HY-N10564
-
|
|
P-glycoprotein
|
Cancer
|
|
8α,9α-Epoxycoleon-U-quinone (compound 3) is a p-glycoprotein (P-gp) regulator that is selective for cancer cells (SI=2.0). 8α,9α-Epoxycoleon-U-quinone effectively inhibits P-gp activity in NCI-H460/R cells. 8α,9α-Epoxycoleon-U-quinone also reverses the resistance of cancer cells to Doxorubicin (DOX) (HY-15142A) and enhances the anticancer effect of DOX .
|
-
- HY-115903
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation .
|
-
- HY-113038AS1
-
|
2-Hydroxyglutarate-d4 disodium; 2-Hydroxyglutaric acid-d4 disodium; 2-Hydroxypentanedioic acid-d4 disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium . α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-P10850
-
|
|
TNF Receptor
NF-κB
Apoptosis
|
Inflammation/Immunology
|
|
PIYLGGVFQ is a peptide inhibitor for TNF-α. PIYLGGVFQ inhibits TNF-α-mediated apoptosis, NF-κB nuclear translocation and activation. PIYLGGVFQ exhibits anti-arthritic activity in the CIA mouse model .
|
-
- HY-118694
-
-
- HY-164259
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
AJM 290 is a Trx-1 inhibitor. AJM 290 is an inhibitor of the HIF-1α COOH-terminal transactivation domain, and blocks HIF-1 binding to DNA .
|
-
- HY-113038A
-
|
2-Hydroxyglutarate disodium; 2-Hydroxyglutaric acid disodium; 2-Hydroxypentanedioic acid disodium
|
Histone Demethylase
Endogenous Metabolite
|
Cancer
|
|
α-Hydroxyglutaric acid (2-Hydroxyglutarate) disodium is an α-hydroxy acid form of glutaric acid. α-Hydroxyglutaric acid disodium is a competitive inhibitor of multiple α-ketoglutarate-dependent dioxygenases, including histone demethylases and the TET family of 5-methlycytosine (5mC) hydroxylases .
|
-
- HY-157489
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-47 (compound 8H) is a non-competitive α-glucosidase (α-glucosidase) inhibitor with IC50 value is 38.2 μM and Ki value is 38.2 μM. α-Glucosidase-IN-47 can be used in diabetes research. .
|
-
- HY-112275
-
-
- HY-160458
-
|
|
PI3K
|
Others
|
|
PI3Kα-IN-17 (example 4) is a potent inhibitor of PI3Kα .
|
-
- HY-115746
-
-
- HY-156447
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-40 (compound 5) is a noncompetitive α-glucosidase enzyme inhibitor with an IC50 of 24.62 μM .
|
-
- HY-132179
-
-
- HY-153915
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-11 is a potent PI3Kα inhibitor with anticancer activity .
|
-
- HY-147879
-
-
- HY-163361
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-20 (compound 2) is a selective PI3Kα inhibitor .
|
-
- HY-156406
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PITCOIN4 is a highly selective Class II Alpha PI3K-C2α inhibitor. PITCOIN4 shows nanomolar inhibition of PI3K-C2α and >100-fold selectivity in a general kinase panel .
|
-
- HY-147965
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-10 (compound 13) is a potent α-glucosidase inhibitor, with an IC50 of 92.7 μM. α-Glucosidase-IN-10 can be used for type II diabetes research .
|
-
- HY-160027
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-alpha-IN-1 (compound 202) is an orally active inhibitor of TNF-alpha. TNF-alpha-IN-1 has anti-inflammatory activity which can used in study rheumatoid arthritis, psoriasis, and asthma .
|
-
- HY-172608
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
TNF-α-IN-24 (Example 15) is a TNF-α inhibitor with an IC50 of 4.1 nM. TNF-α-IN-24 can be used in study of inflammatory and autoimmune disorders such as rheumatoid arthritis and Crohn’s disease .
|
-
- HY-129348
-
|
|
IRE1
|
Cancer
|
|
IRE1α kinase-IN-10 (GP29) is an IRE1α kinase inhibitor. IRE1α kinase-IN-10 can be used for the research of endoplasmic reticulum stress-related diseases .
|
-
- HY-147964
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-9 (compound 7) is a potent α-glucosidase inhibitor, with an IC50 of 55.6 μM. α-Glucosidase-IN-9 can be used for type II diabetes research .
|
-
- HY-151135
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-15 (Compound 14B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.34 μM. α-Glucosidase-IN-15 shows antidiabetic activity .
|
-
- HY-18510
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-7 (compound 4) is an IRE1α kinase inhibitor. IRE1α kinase-IN-7 can be used for research of endoplasmic reticulum stress-related diseases .
|
-
- HY-151141
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-17 (Compound 12B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.79 μM. α-Glucosidase-IN-17 shows antidiabetic activity .
|
-
- HY-12836A
-
|
|
IFNAR
|
Inflammation/Immunology
|
|
IFN alpha-IFNAR-IN-1 hydrochloride is a nonpeptidic, low-molecular-weight inhibitor of the interaction between IFN-α and IFNAR. IFN alpha-IFNAR-IN-1 hydrochloride inhibits modified Vaccinia virus ankara (MVA)-induced IFN-α responses in murine bone-marrow-derived, Flt3- L-differentiated pDC cultures (BM-pDCs) (IC50=2-8 μM) .
|
-
- HY-149000
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-7 (Compound A12) is a potent PI3Kα inhibitor. PI3Kα-IN-7 also inhibits PI3Kβ. PI3Kα-IN-7 decreases cancer cells mitochondrial membrane potential and induces apoptosis .
|
-
- HY-148575
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-23 is an orally active α-Glucosidase inhibitor. α-Glucosidase-IN-23 decreases blood glucose by a-glucosidase inhibition with an IC50 value of 4.48 μM. α-Glucosidase-IN-23 can be used for the research of diabetes .
|
-
- HY-147100
-
|
|
PROTACs
Adrenergic Receptor
|
Cancer
|
|
α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research .
|
-
- HY-N4155
-
|
|
EBV
HIV Protease
HSV
|
Infection
Cancer
|
|
2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid, a natural ursane-type triterpene, is a potent inhibitor of HIV protease (HIV Protease). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid is also an inhibitor of the activation of Epstein-Barr virus early antigen (EBV-EA). 2α,19α-Dihydroxy-3-oxo-urs-12-en-28-oic acid displays an inhibitory activity against nitric oxide production in Lipopolysaccharide (Lipopolysaccharides)-activated RAW 264.7 cells .
|
-
- HY-110343
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
DBM 1285 dihydrochloride is an orally active TNF-α production inhibitor with anti-inflammatory effects. DBM 1285 dihydrochloride inhibits Lipopolysaccharide (LPS)-induced TNF-α secretion in various cells of macrophage/monocyte lineage .
|
-
- HY-121172
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
1,4-DPCA, a potent prolyl-4-hydroxylase inhibitor, is a collagen hydroxylation inhibitor in human foreskin fibroblasts with an IC50 of 2.4 µM. 1,4-DPCA inhibits prolyl-4-hydroxylases α isoforms stabilizes HIF-1α protein. 1,4-DPCA also inhibits factor inhibiting HIF (FIH) with an IC50 of 60 μM .
|
-
- HY-33549
-
|
|
Tyrosine Hydroxylase
|
Neurological Disease
Cancer
|
|
α-Methyl-p-tyrosine is a competitive inhibitor of tyrosine hydroxylase, which converts tyrosine into DOPA. α-Methyl-p-tyrosine is also an orally active inhibitor of catecholamine synthesis, inhibiting the hydroxylation of tyrosine into DOPA. α-Methyl-p-tyrosine can be used in research related to epilepsy, glaucoma, cancer, and other related diseases .
|
-
- HY-151921
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 33 is a potent p38α inhibitor. Anti-inflammatory agent 33 inhibits NO production. Anti-inflammatory agent 33 inhibits LPS-induced iNOS, COX-2, p-p38α, p-MK2 protein expression. Anti-inflammatory agent 33 shows anti-inflammatory activity .
|
-
- HY-151143
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-19 (Compound 6B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.63 μM. α-Glucosidase-IN-19 shows anti-diabetic activity .
|
-
- HY-N12664
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-54 (compound 2) is a α-glucosidase inhibitor with the IC50 of 0.011 mM, and can be isolated form Syzygium jambos (L.). α-Glucosidase-IN-54 can be used for study of diabetes .
|
-
- HY-P2978
-
|
|
Ser/Thr Protease
|
Neurological Disease
|
|
Alpha 1 Antichymotrypsin, Human Plasma is a serine protease inhibitor. Alpha 1 Antichymotrypsin, Human Plasma appears in the amyloid lesions of Alzheimer's disease. Alpha 1 Antichymotrypsin, Human Plasma can be used in Alzheimer's disease research .
|
-
- HY-161944
-
|
|
Amylases
|
Metabolic Disease
|
|
α-Amylase-IN-8 (compound 44) is an α-amylase inhibitor (IC50=58.1 μM). α-Amylase-IN-8 can be used in the research of type 2 diabetes .
|
-
- HY-157311
-
|
|
Glycosidase
|
Cancer
|
|
α-Glucosidase-IN-45 (compound 11E) is an inhibitor of α-glucosidase. α-Glucosidase-IN-45 is a novel indol-fused pyrano[2,3-D]pyrimidine compound .
|
-
- HY-169251
-
-
- HY-162599
-
|
|
TNF Receptor
|
Infection
Cancer
|
|
Spirohypertone B is a potent Tumor necrosis factor-α (TNF-α) inhibitor. Spirohypertone B protects L929 cells from death induced by co-incubation with TNF-α and Actinomycin D (HY-17559) .
|
-
- HY-163862
-
-
- HY-170548
-
|
|
Amylases
|
Metabolic Disease
|
|
α-Amylase-IN-10 (Compound 15n) is an inhibitor for α-Amylase with an IC50 of 5.00 µM. α-Amylase-IN-10 can be used for research of type 2 diabetes mellitus .
|
-
- HY-158697
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-65 (compound 5) is a Schiff base derivative of 3,4-dihydroxyphenylacetic acid. α-Glucosidase-IN-65 is a potent α-glucosidase inhibitor, with an IC50 of 12.84 μM .
|
-
- HY-173035
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-85 (Compound 8D1) is the inhibitor for α-Glucosidase with an IC50 of 5.43 μM. α-Glucosidase-IN-85 can be used in research of type 2 diabetes .
|
-
- HY-151145
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-21 (Compound 2B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 2.62 μM. α-Glucosidase-IN-21 shows anti-diabetic activity .
|
-
- HY-151144
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-20 (Compound 3B) is a potent, orally active α-glucosidase inhibitor with an IC50 of 3.01 μM. α-Glucosidase-IN-20 shows anti-diabetic activity .
|
-
- HY-119019
-
-
- HY-172758
-
|
|
Glycosidase
|
Others
|
α-Glucosidase-IN-89 (8g) is α-glucosidase inhibitor, with an IC50 of 0.5 μM and a Ki of 0.46 µM .
|
-
- HY-P10693
-
-
- HY-50855B
-
|
CX-4945 sodium salt
|
Casein Kinase
Autophagy
|
Cancer
|
|
Silmitasertib sodium salt is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
|
-
- HY-106720C
-
|
(+)-YM 09538
|
Adrenergic Receptor
|
Others
|
|
(+)-Amosulalol ((+)-YM 09538) is an isomer of Amosulalol (HY-106720), an orally active dual inhibitor of α1/β1-adrenergic receptors. Amosulalol exhibits antihypertensive activity by inhibiting α1-adrenergic receptors. Amosulalol reduces the reflex increase in heart rate and plasma renin activity (PRA) in spontaneously hypertensive rats (SHR) by inhibiting β1-adrenergic receptors.
|
-
- HY-106720B
-
|
(-)-YM 09538
|
Adrenergic Receptor
|
Others
|
|
(-)-Amosulalol ((-)-YM 09538) is an isomer of Amosulalol (HY-106720), an orally active dual inhibitor of α1/β1-adrenergic receptors. Amosulalol exhibits antihypertensive activity by inhibiting α1-adrenergic receptors. Amosulalol reduces the reflex increase in heart rate and plasma renin activity (PRA) in spontaneously hypertensive rats (SHR) by inhibiting β1-adrenergic receptors.
|
-
- HY-163360
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-19 (Compound 1) is a PI3Kα inhibitor with a targeted binding site at the p110α catalytic subunit. PI3Kα is one of the most common dysregulated kinases used in cancer research .
|
-
- HY-161999
-
|
|
Glycosidase
|
Metabolic Disease
Inflammation/Immunology
|
|
α-Glucosidase-IN-73 (compound 16b) is an α-Glucosidase inhibitor with IC50 of 0.158 μM. α-Glucosidase-IN-73 can activate PPAR γ. α-Glucosidase-IN-73 can be used in anti-diabetic and anti-inflammatory studies .
|
-
- HY-153474
-
|
|
IRE1
|
Others
|
|
IRE1α kinase-IN-8, a benzoheterocyclecarboxaldehyde derivative, is a potent IRE-1α inhibitor. IRE1α kinase-IN-8 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) .
|
-
- HY-W089785
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Methyl α-D-galactopyranoside monohydrate is an alpha-D-galactoside having a methyl substituent at the anomeric position. Methyl α-D-galactopyranoside inhibits debaryomyces hansenii UFV-1 extracellular and intracellular α-galactosidases with Ki values of 0.82 and 1.12 mM, respectively .
|
-
- HY-163066
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-44 (compound IT4) is an inhibitor of α-glucosidase with IC50 value of 2.35 μM. α-Glucosidase-IN-44 has an oral activity. α-Glucosidase-IN-44 suppresses fasting blood glucose levels in diabetic mice .
|
-
- HY-P99721
-
|
ABT-981
|
Interleukin Related
|
Inflammation/Immunology
|
|
Lutikizumab (ABT-981) is an anti-IL-1α and IL-1β dual variable domain immunoglobulin. Lutikizumab binds and inhibits IL-1α and IL-1β. Lutikizumab can be used for the research of osteoarthritis .
|
-
- HY-N1064
-
|
|
nAChR
|
Neurological Disease
|
|
Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2) .
|
-
- HY-151465
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-1α-IN-4 is a HIF-1α inhibitor with an IC50 value of 24 nM (in HEK293T cell). HIF-1α-IN-4 downregulates VEGF and PDK1 mRNA expressions under hypoxia. HIF-1α-IN-4 can be used in the research of cancer .
|
-
- HY-103204
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
RS100329 hydrochloride is a potent and selective α1A-adrenoceptor antagonist with pKi values of 9.6, 7.9 and 7.5 for α1A, α1D, and α1B, respectively. RS100329 hydrochloride inhibits reflex urethral contractions. RS100329 hydrochloride can be used in research of benign prostatic hyperplasia .
|
-
- HY-144699
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
|
-
- HY-12753A
-
|
SR35021 hydrochloride
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
|
-
- HY-157225
-
|
|
α-synuclein
|
Metabolic Disease
|
|
Brazilin-7-acetate (B-7-A) is an inhibitor of α-synuclein (α-Syn) aggregates. Brazilin-7-acetate inhibits the formation of α-synuclein fibril, mitigates cytotoxicity, and decreases oxidative stress. Brazilin-7-acetate can be used in the research of Parkinson's disease .
|
-
- HY-111022
-
|
Sephin1; IFB-088
|
Phosphatase
|
Infection
Inflammation/Immunology
|
|
Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect .
|
-
- HY-123009
-
|
|
HIF/HIF Prolyl-Hydroxylase
Histone Acetyltransferase
|
Cancer
|
|
KCN1 is a p300/HIF-1α interaction inhibitor. KCN1 inhibits HIF transcriptional activity by binding to the CH1 domain of p300 and preventing the p300/HIF-1α assembly. KCN1 exerts antitumor activities through cell cycle arrest .
|
-
- HY-168594
-
|
|
Glycosidase
NOD-like Receptor (NLR)
|
Neurological Disease
Metabolic Disease
|
|
α-Glucosidase/NLRP3-IN-1 (Compound 8) is a dual inhibitor of α-glucosidase and NLRP3, exhibiting an IC50 of 6.6 μM against α-glucosidase and inhibiting NLRP3 in multiple cell lines at a concentration of 100 μM. α-Glucosidase/NLRP3-IN-1 demonstrates neuroprotective and antidiabetic properties, and can be utilized in relevant research .
|
-
- HY-124314
-
|
|
DAGL
MAGL
|
Metabolic Disease
|
|
LEI-106 is a potent, dual sn-1-Diacylglycerol lipase α (DAGL-α)/ABHD6 inhibitor with an IC50 of 18 nM for DAGL-α and a Ki of 0.8 μM for ABHD6. LEI-106 inhibits the hydrolysis of [ 14C]-sn-1-oleoyl-2-arachidonoyl-glycerol, the natural substrate of DAGL-α, with a Ki of 0.7 μM .
|
-
- HY-146540
-
|
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
MDM-2/p53
|
Cancer
|
|
GEM-5 is a gemcitabine-based conjugate containing a HIF-1α inhibitor (YC-1) (IC50=30 nM). GEM-5 can significantly down-regulate the expression of HIF-1α and up-regulate the expression of tumor suppressor p53. GEM-5 induces the apoptosis of A2780 cells and inhibits tumor growth .
|
-
- HY-N8847R
-
|
|
Hippo (MST)
YAP
|
Cancer
|
|
α-Ionone (Standard) is the analytical standard of α-Ionone. This product is intended for research and analytical applications. α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
|
-
- HY-106954
-
|
Rec 15/2739; Recordati 15/2739; SB 216469
|
Adrenergic Receptor
|
Inflammation/Immunology
|
|
Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction .
|
-
- HY-147518
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38-α MAPK-IN-5 (compound 4e) is a potent p38α inhibitor with IC50s of 0.1 nM, 0.2 nM, 944 nM, 4100 nM for p38α, p38 β, p38γ, p38δ, respectively. p38-α MAPK-IN-5 has anti-inflammatory effect. p38-α MAPK-IN-5 has the potential for asthma and chronic obstructive pulmonary disease (COPD) research .
|
-
- HY-129453
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BOP sodium is a potent and selective dual α9β1/α4β1 integrin inhibitor with Kd values in the picomolar range. BOP sodium shows the rapid and preferential mobilization of hematopoietic stem cell (HSC) and progenitors. BOP sodium has little inhibitory activity on α4β7, α1β1, α2β1, and α5β1, αIIBβ3 integrins .
|
-
- HY-172586
-
|
|
GSK-3
PKA
|
Neurological Disease
Cancer
|
|
GSK-3α/β-IN-1 is GSK-3α/β inhibitor with IC50 s of 0.265 μM and 0.255 μM for GSK-3α and GSK-3β, respectively. GSK-3α/β-IN-1 also inhibits PKA with an IC50 of 0.188 μM. GSK-3α/β-IN-1 potently inhibits cell viability of three Glioblastoma (GBM) cell lines (IC50 : 3-6 μM, 72 h) with no toxicity to human astrocytes and good metabolic stability. GSK-3α/β-IN-1 has potential CNS activity in all-human blood-brain barrier (BBB) model of GBM .
|
-
- HY-131335
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38α inhibitor 2 is a highly potent and selective p38α MAPK inhibitor, with a pIC50 of 9.6. p38α inhibitor 2 inhibits the hERG ion channel (IC50=27 μM) and shows a promising selectivity profile when tested in a panel of 51 other protein kinases (<30% inhibition at 10 μM concentration) and a panel of 141 other biological targets .
|
-
- HY-W783267
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-35 (compound 1) is a kind of chromene. α-Glucosidase-IN-35 can be isolated from the aqueous extract of the aerial parts of Brickellia cavanillesii. α-Glucosidase-IN-35 is a potent inhibitor of α-glucosidase with an IC50 value of 0.169 mg/mL .
|
-
- HY-119971
-
|
|
Nuclear Hormone Receptor 4A/NR4A
|
Metabolic Disease
Cancer
|
|
BIM5078 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BIM5078 represses insulin promoter activity through HNF4α antagonism. BIM5078 can be used for the research of cancer and diabetes .
|
-
- HY-168465
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-83 (compound I-1) is a potent inhibitor of α-Glucosidase, with the IC50 of 1.49 μg/mL. α-Glucosidase-IN-83 shows reduction in blood glucose levels in vivo .
|
-
- HY-147777
-
|
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
14α-Demethylase/DNA Gyrase-IN-2 (Compound 6a) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-2 has antimicrobial activities .
|
-
- HY-N12689
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-56 (compound 1) is an orally active, potent α‐glucosidase inhibitor with an IC50 value of 45.86 μM. α-Glucosidase-IN-56 has potent anti-glycation activities .
|
-
- HY-W005598
-
|
|
Glycosidase
|
Metabolic Disease
|
|
2-Hydroxyquinoline is a potent α-glucosidase inhibitor with IC50 values of 64.4, 130.5 µg/mL for α-glucosidase and α-amylase, respectively. 2-Hydroxyquinoline has the potential for the research of diabetes .
|
-
- HY-N8120
-
-
- HY-U00313
-
-
- HY-131404
-
TPBM
1 Publications Verification
|
Estrogen Receptor/ERR
|
Cancer
|
|
TPBM is a potent estrogen receptor α (ERα) inhibitor with an IC50 value of 9 μM for 17β-estradiol (E2)-ERα. TPBM reduces E2·ERα recruitment to an endogenous estrogen-responsive gene. TPBM inhibits E2-dependent growth of ERα-positive cancer cells (IC50=5 μM). TPBM is not toxic to cells and does not affect estrogen-independent cell growth .
|
-
- HY-164102
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
|
-
- HY-117158
-
|
|
Adrenergic Receptor
|
Others
|
|
SKF 89748 is an α1-adrenergic receptor agonist with the activity of inhibiting food and water intake. SKF 89748 inhibits food and water intake in adult male rats with an ED50 of 0.37mg/kg for inhibiting food intake.
|
-
- HY-N11697
-
|
|
P-glycoprotein
|
Cancer
|
|
α-Cryptoxanthin is a natural carotenoid with anticancer effects. α-Cryptoxanthin inhibits multidrug resistance 1 (MDR1) mediated efflux pump .
|
-
- HY-156078
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .
|
-
- HY-159146
-
-
- HY-168495
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
α-Amylase-IN-12 (Compound 5e) is an α-amylase inhibitor (IC50: 0.15 mM) with a mixed inhibition. α-Amylase-IN-12 has an IC50 of 9.40 mM against α-glucosidase. α-Amylase-IN-12 promotes glucose uptake in yeast cells and exhibits significant antiglycation activity at high concentrations. α-Amylase-IN-12 can be used for the research of diabetes .
|
-
- HY-148922
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARα/γ agonist 2 is an orally active PPARα full agonist and PPARγ partial agonist. PPARα/γ agonist 2 activates PPARα and PPARγ with EC50 values of 0.95 μM and 0.91 μM respectively. PPARα/γ agonist 2 is also a PTP1B inhibitor. PPARα/γ agonist 2 is an anti-diabetic agent .
|
-
- HY-146144
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-IN-1 (Compound 3c) is a hypoxia-inducible factor (HIF)-1 inhibitor. HIF-IN-1 suppresses HIF-1α protein accumulation without affecting the levels of HIF-1α mRNA. HIF-IN-1 shows no obvious cytotoxicity .
|
-
- HY-N8847
-
|
alpha-Ionone
|
Hippo (MST)
YAP
Olfactory Receptor
Apoptosis
|
Cancer
|
|
α-Ionone (alpha-Ionone) is an activator of the olfactory receptor OR10A6. α-Ionone induces apoptosis by activating OR10A6 and increasing the phosphorylation of the LATS-YAP-TAZ signaling axis in the Hippo pathway. α-Ionone can inhibit tumor formation both in vivo and in vitro .
|
-
- HY-108469
-
BI-6015
4 Publications Verification
|
Orphan Receptor
|
Metabolic Disease
Cancer
|
|
BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes .
|
-
- HY-N0242R
-
|
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Inflammation/Immunology
Cancer
|
|
Fraxinellone (Standard) is the analytical standard of Fraxinellone. This product is intended for research and analytical applications. Fraxinellone is isolated from the root bark of the Rutaceae plant, Dictamnus dasycarpus. Fraxinellone is a PD-L1 inhibitor and inhibits HIF-1α protein synthesis without affecting HIF-1α protein degradation. Fraxinellone has the potential to be a valuable candidate for cancer treatment by targeting PD-L1 .
|
-
- HY-120675
-
SSTC3
2 Publications Verification
|
Casein Kinase
Wnt
|
Cancer
|
|
SSTC3 is a casein kinase 1α (CK1α) activator (Kd = 32 nM) that inhibits WNT signaling (EC50 = 30 nM). SSTC3 exhibits minimal gastrointestinal toxicity compared to other classes of WNT inhibitors .
|
-
- HY-162722
-
|
|
GSK-3
|
Others
|
|
GSK-3 inhibitor 6 (2) is a CNS penetrated GSK-3 inhibitor, with IC50 values of 29 nM and 24 nM for GSK-3α and GSK-3β, respectively .
|
-
- HY-19332
-
|
FR-900494
|
Glycosidase
|
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-105191
-
-
- HY-125713
-
|
|
Glycosidase
Enterovirus
|
Infection
|
|
Ganoderic acid Y is a α-glucosidase inhibitor with an IC50 of 170 μM for yeast α-glucosidase. Ganoderic acid Y inhibits enterovirus 71 (EV71) replication through blocking EV71 uncoating .
|
-
- HY-170588
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-78 (Compound 12m) is an inhibitor for α-glucosidase with a reversible, competitive IC50 6.0 μM. α-Glucosidase-IN-78 can be used in research of diabete for its hypoglycemic property .
|
-
- HY-N0901A
-
|
|
α-synuclein
|
Neurological Disease
Cancer
|
Corynoxine B is an alkaloid-based autophagy inducer and α-synuclein aggregation inhibitor that ameliorates Mn-induced dysregulation of autophagy and enhances α-synuclein (α-syn) clearance in Parkinson's disease mice .
|
-
- HY-162697
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-69 (compound 5k) is a competitive α-glucosidase inhibitor with an IC50 of 26.8 µM and a Ki value of 26.0 µM. α-Glucosidase-IN-69 has the potential for the diabetes research .
|
-
- HY-147778
-
|
|
Bacterial
DNA/RNA Synthesis
|
Infection
|
|
14α-Demethylase/DNA Gyrase-IN-1 (Compound 7c) is a potent inhibitor of 14α-Demethylase/DNA Gyrase. 14α-Demethylase/DNA Gyrase-IN-1 has antimicrobial activities .
|
-
- HY-162541
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-64 (compound 10) is a potent α-glucosidase inhibitor with an IC50 value of 8.62 µM. α-Glucosidase-IN-64 is a polycyclic polyprenylated acylphloroglucinol that can be isolated from hypericum beanii .
|
-
- HY-W342092
-
|
|
Biochemical Assay Reagents
Endogenous Metabolite
|
|
|
1,3,4,6-Tetrachloro-3α,6α-diphenylglycouril is a chemical agent that has the property of inhibiting enzyme activity in organisms. 1,3,4,6-Tetrachloro-3α,6α-diphenylglycouril is used as a potential anti-tumor agent in compound development. 1,3,4,6-Tetrachloro-3α,6α-diphenylglycouril has the effect of regulating cell signaling pathways and can be used to study cell biology. 1,3,4,6-Tetrachloro-3α,6α-diphenylglycouril is considered to be a potent compound that can exert biological activity under specific conditions.
|
-
- HY-110365
-
|
Sephin1 Carbonate; IFB-088 Carbonate
|
Phosphatase
|
Infection
|
|
Icerguastat (Sephin1) Carbonate, a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat Carbonate inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect .
|
-
- HY-162373
-
|
|
Amylases
Glycosidase
P-glycoprotein
|
Metabolic Disease
|
|
α-Amylase/α-Glucosidase-IN-10 (compound 5d) is an α-amylase and α-glucosidase inhibitor (IC50: 30.39 μM and 65.1 μM) with potential diabetes inhibitory effects. α-Amylase/α-Glucosidase-IN-10 exhibits high gastrointestinal (GI) absorption in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) prediction. While α-Amylase/α-Glucosidase-IN-10 acts as a substrate for P-gp and does not cross the blood-brain barrier (BBB), there may be a risk of central nervous system side effects .
|
-
- HY-161462
-
|
|
ERK
p38 MAPK
|
Cancer
|
|
ERK2/p38α MAPK-IN-1 (Compound 1, In silico Hit-2) is a potent and selective ERK2 and p38α MAPK inhibitor, with an IC50 of 82 μM for ERK2. ERK2/p38α MAPK-IN-1 binds to the allosteric site of ERK2 and p38α MAPK in distinct manners. ERK2/p38α MAPK-IN-1 can be used for the research of type 2 diabetes .
|
-
- HY-149654
-
-
- HY-149666
-
|
|
DGK
|
Cancer
|
|
BMS-496 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.09 (DGKα) and 0.006 μM (DGKζ) .
|
-
- HY-133807A
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
(Rac)-Benpyrine, a racemate of Benpyrine, is a potent and orally active TNF-α inhibitor. (Rac)-Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research .
|
-
- HY-149667
-
|
|
DGK
|
Cancer
|
|
BMS-332 is adualDGKα/ζlipid kinase inhibitor, with theIC50of 0.005 (DGKα) and 0.001 μM (DGKζ) .
|
-
- HY-14975
-
|
|
p38 MAPK
Autophagy
|
Cancer
|
|
R1487 Hydrochloride is a highly potent and selective p38α inhibitor, with Kd values of 0.2 nM and 29 nM for p38α and p38β, respectively .
|
-
- HY-131553R
-
|
|
Apoptosis
|
Cancer
|
|
D-α-Tocopherol Succinate (Standard) is the analytical standard of D-α-Tocopherol Succinate. This product is intended for research and analytical applications. D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer .
|
-
- HY-N0492S
-
-
- HY-U00244A
-
|
P2647 hydrochloride; BZQ hydrochloride; Benzoquinamide hydrochloride
|
Adrenergic Receptor
|
Cancer
|
|
Benzquinamide (P2647) is an antiemetic which can bind to the α2A, α2B, and α2C adrenergic receptors (α2-AR) with Ki values of 1,365, 691, and 545 nM, respectively. Benzquinamide also inhibits P-glycoprotein mediated drug efflux and potentiates anticancer agent cytotoxicity in multidrug resistant cells .
|
-
- HY-149341
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-28 (Compound 18) is a α-Glucosidase inhibitor (IC50: 0.62 μM, Ki: 3.93 μM). α-Glucosidase-IN-28 binds to α-glucosidase at the original binding site (OBS), and forms multiple hydrophobic interactions with nearby amino acids. α-Glucosidase-IN-28 can be used for research of diabetes and related diseases .
|
-
- HY-20070
-
|
|
TNF Receptor
|
Others
Inflammation/Immunology
|
|
BMS-566394 is a potent inhibitor of tumor necrosis factor-α (TNF-α) converting enzyme (TACE) that helps reduce the production of TNF-α, thereby alleviating inflammation and immune-mediated diseases and can be used in the study of inflammatory and autoimmune diseases .
|
-
- HY-120408
-
|
Atroscine
|
Adrenergic Receptor
|
Neurological Disease
|
|
(±)-Scopolamine (Atroscine) is the racemic modification of Scopolamine. (±)-Scopolamine inhibits α-adrenergic receptor activity. (±)-Scopolamine has Ki values of 33 μM and 7.25 nM for α1-adrenerg receptor and muscarinic cholinergic receptor, respectively .
|
-
- HY-154998
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-27 (compound 8l) is an α-glucosidase inhibitor (IC50=25.78 μM). α-Glucosidase-IN-27 has the potential to study type 2 diabetes (D2M) .
|
-
- HY-N12347
-
|
|
Others
|
Inflammation/Immunology
|
|
α-Glucosidase-IN-37 (Compound 11) moderately inhibits LPS-induced NO production with an IC50 value of 23.7 μM in macrophages. α-Glucosidase-IN-37 has weak inhibitory activity against α-Glucosidase .
|
-
- HY-146020
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-1 (compound 2) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-1 exhibits high antiproliferative activity against human cancer cell lines .
|
-
- HY-130264
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
HIF-2α-IN-2 is a hypoxia-inducible factors (HIF-2α) inhibitor extracted from patent WO2015035223A1, Compound 232, has an IC50 of 16 nM in scintillation proximity assay (SPA) .
|
-
- HY-130398
-
|
|
α-synuclein
|
Neurological Disease
|
|
Aerophobin-2 is a bromine compound, which can be isolated from sponge Verongia aerophoba. Aerophobin-2 inhibits aggregation of α-synuclein (α-syn) and phosphorylated α-synuclein (pSyn), exhibits neuroprotective efficacy .
|
-
- HY-106174
-
|
CS 891
|
5 alpha Reductase
|
Endocrinology
|
|
Lapisteride (CS 891) is an orally active 5α-reductase inhibitor. Lapisteride can inhibit 5α-reductaseactivity in the hair follicles (HF). Lapisteride can be used in prostatic hyperplasia and androgenic alopecia research .
|
-
- HY-N2882
-
|
|
HBV
|
Infection
|
|
Apigenin-4'-α-L-rhamnoside is a potent inhibitor of HBV. Apigenin-4'-α-L-rhamnoside inhibits the secretory level of HBV surface antigen (HBsAg) in HepG2.2.15 cells .
|
-
- HY-N6782
-
-
- HY-15893
-
|
Dimethyloxallyl Glycine
|
HIF/HIF Prolyl-Hydroxylase
Autophagy
|
Cancer
|
|
DMOG (Dimethyloxallyl Glycine) is a cell permeable and competitive inhibitor of HIF-PH, which results in HIF-1α stabilisation and accmulation?in vitro and in vivo . DMOG is an α-ketoglutarate analogue and inhibits α-KG-dependent hydroxylases. DMOG?acts as a pro-angiogenic agent and plays a protective role in experimental model of colitis and diarrhoea via HIF-1 related signal . DMOG induces cell autophagy .
|
-
- HY-172757
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-88 (Compound 3K) is an orally active and potent α-glucosidase inhibitor with an IC50 value of 6.40 µM. α-Glucosidase-IN-88 inhibits carbohydrate hydrolysis by blocking the enzyme's ability to break down glycosidic bonds, thereby reducing postprandial blood glucose levels. α-Glucosidase-IN-88 is promising for research of type 2 diabetes mellitus (T2DM) .
|
-
- HY-134664
-
|
|
Cytochrome P450
Monoamine Oxidase
|
Inflammation/Immunology
|
|
8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate is an irreversible CYP2A6 inhibitor with IC50s of 8.64 μM and 22.3 μM with pre-incubation and co-incubaition, respectively. 8α-(2-Methylacryloyloxy)-hirsutinolide-13-O-acetate also inhibits MAO-A and MAO-B with IC50s of 60.2 and 38.6 μM, respectively .
|
-
- HY-161140
-
|
|
PI3K
Wnt
|
Cancer
|
|
PI3Kα-IN-16 (Z86) is a novel PI3Kα inhibitor with an IC50 value of 4.28 μM. PI3Kα-IN-16 has potent inhibitory efficiency on PI3K-mediated CRCs growth and migration. PI3Kα-IN-16 also inhibits the Wnt signaling pathway .
|
-
- HY-152187
-
|
|
Topoisomerase
Apoptosis
|
Others
|
|
Topoisomerase IIα-IN-5 is a topoisomerase II (topo II) α catalytic inhibitor. Topoisomerase IIα-IN-5 intercalates into DNA and binds to the DNA minor groove. Topoisomerase IIα-IN-5 exhibits better efficacy and less genotoxicity than Etoposide (HY-13629) .
|
-
- HY-100740C
-
|
(1α,1'S,4β)-AZD3293; (1α,1'S,4β)-LY3314814
|
Beta-secretase
|
Neurological Disease
|
|
(1α,1'S,4β)-Lanabecestat ((1α,1'S,4β)-AZD3293) a less active enantiomer of Lanabecestat. Lanabecestat is a potent, orally active and blood-brain barrier penetrating BACE1 inhibitor with a Ki of 0.4 nM .
|
-
- HY-144696
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .
|
-
- HY-N6968R
-
|
|
NO Synthase
COX
|
Inflammation/Immunology
|
|
α-Humulene (Standard) is the analytical standard of α-Humulene. This product is intended for research and analytical applications. α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 μg/mL). α-Humulene inhibits COX-2 and iNOS expression .
|
-
- HY-U00326
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3Kα/mTOR-IN-1 is a potent PI3Kα/mTOR dual inhibitor, with an IC50 of 7 nM for PI3Kα in a cell assay, and Kis of 10.6 nM and 12.5 nM for mTOR and PI3Kα in a cell free assay , respectively.
|
-
- HY-P5082
-
|
|
α-synuclein
|
Neurological Disease
|
|
α-Synuclein 4554W is an inhibitor of α-Synuclein (aSyn) aggregation with associated toxicity. α-Synuclein 4554W consists of GIVNGVKA sequences, previously identified through intracellular library screening. α-Synuclein 4554W reduces fibril formation of aSyn mutants assocaited with Parkinson’s disease .
|
-
- HY-160116
-
|
|
Radionuclide-Drug Conjugates (RDCs)
Fluorescent Dye
α-synuclein
|
Neurological Disease
|
|
α-Synuclein aggregate binder 1 (Compound C05-05) is a specific binder for α-synuclein aggregates and can inhibit α-synuclein aggregation. α-Synuclein aggregate binder 1 can be used as a fluorescent probe (excitation wavelength 900 nm, detection wavelength 500-550 nm) for optical imaging, and can also inhibit α-synuclein fibril formation by blocking the aggregation process. α-Synuclein aggregate binder 1 can be used for positron emission tomography (PET) imaging after being labeled with 18F. α-Synuclein aggregate binder 1 can be used for visual diagnosis of brain lesions and mechanism research of neurodegenerative diseases such as Parkinson's disease and Lewy body dementia .
|
-
- HY-U00090
-
|
MOR 14; N-Methyl-1-deoxynojirimycin; N-Methylmoranolin
|
Glycosidase
|
Metabolic Disease
|
|
N-Methylmoranoline (MOR 14) is an α-glucosidase inhibitor.
|
-
- HY-N3962
-
-
- HY-145580
-
|
UCB0599; (R)-NPT200-11
|
α-synuclein
|
Neurological Disease
|
|
Minzasolmin (UCB0599; (R)-NPT200-11) is an orally active, blood-brain-permeable α-synuclein (α-Syn) inhibitor that selectively binds to α-Syn misfolded intermediates (such as oligomers) and inhibits aggregation and fibril formation by regulating their conformational stability. Minzasolmin can reduce the generation of pathological oligomers and block neurotoxic signaling, thereby reducing the abnormal accumulation of α-Syn in the brain. Minzasolmin significantly improved motor deficits, reduced neuroinflammatory markers, and α-Syn-related pathological deposition in transgenic mouse models .
|
-
- HY-130437
-
|
|
MDM-2/p53
TGF-β Receptor
Caspase
|
Infection
Metabolic Disease
|
|
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease .
|
-
- HY-129113
-
|
|
COX
|
Inflammation/Immunology
|
|
α-Chaconine inhibits the expressions of COX-2, IL-1β, IL-6, and TNF-α at the transcriptional level. α-Chaconine inhibits the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels and their promoter activities in RAW 264.7 macrophages. Anti-inflammatory effects .
|
-
- HY-170796
-
|
|
Amylases
|
Metabolic Disease
|
|
α-Amylase-IN-11 (compound C5f) is an α-Amylase inhibitor (IC50=0.56 μM) that can reduce the sugar level in vivo. α-Amylase-IN-11 has a moderate inhibitory effect on α-glucosidase (α-glucosidase), with IC50=11.03 μM. α-Amylase-IN-11 can significantly reduce the glucose concentration in a mouse model and has the potential for use in diabetes research .
|
-
- HY-131345
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-4 is a potent, selective and orally active inhibitor of PI3Kα, with an IC50 of 1.8 nM. PI3Kα-IN-4 has antitumor activity .
|
-
- HY-136347R
-
|
|
HMG-CoA Reductase (HMGCR)
Drug Metabolite
|
Cardiovascular Disease
|
|
3α-Hydroxy pravastatin (sodium) (Standard) is the analytical standard of 3α-Hydroxy pravastatin (sodium). This product is intended for research and analytical applications. 3α-Hydroxy pravastatin sodium is the major metabolite of Pravastatin. Pravastatin is a competitive HMG-CoA reductase inhibitor .
|
-
- HY-148866
-
|
|
Calcium Channel
|
Neurological Disease
Endocrinology
|
|
Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has Kis of 100-500 nM for human α2δ-1 subunit of Cav2.2 calcium channel and NET, respectively .
|
-
- HY-173393
-
|
|
LXR
|
Cancer
|
|
LXRα agonist 1 (Compound 40) is a selective LXRα agonist (EC50: 42 nM). LXRα agonist 1 also has a certain agonistic effect on LXRβ (EC50: 266 nM). LXRα agonist 1 promotes target gene transcription by stabilizing the ligand binding domain (LBD) of LXRα. LXRα agonist 1 exhibits potent antitumor effects in hepatocellular carcinoma cells when combined with the Raf inhibitor Sorafenib (HY-10201). LXRα agonist 1 can be used in the study of lipotoxic cancers .
|
-
- HY-P990126
-
|
|
Integrin
|
Others
|
|
Anti-Rat CD8α Antibody (OX-8) is a mouse-derived IgG1, κ type antibody inhibitor, targeting to rat CD8α.
|
-
- HY-114368A
-
|
AMG-18 Hydrochloride
|
IRE1
|
Inflammation/Immunology
|
|
Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
|
-
- HY-156454
-
-
- HY-50855
-
|
CX-4945
|
Casein Kinase
Autophagy
|
Cancer
|
|
Silmitasertib (CX-4945) is an orally bioavailable, highly selective and potent CK2 inhibitor, with IC50 values of 1 nM against CK2α and CK2α'.
|
-
- HY-W791671
-
|
|
Biochemical Assay Reagents
Apoptosis
|
Cancer
|
|
Aspergillus giganteus α-sarcin is a ribosome-inactivating protein that induces apoptosis in rhabdomyosarcoma cells. α-Sarcin is suitable for inducing apoptosis and inhibiting protein synthesis .
|
-
- HY-15969
-
Sal003
2 Publications Verification
|
Phosphatase
Apoptosis
|
Cancer
|
|
Sal003 is a potent, specific and cell-permeable inhibitor of the eukaryotic translation initiation factor 2α (eIF2α) phosphatase. Sal003 is a derivative of salubrinal .
|
-
- HY-114368
-
|
AMG-18
|
IRE1
|
Inflammation/Immunology
|
|
Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
|
-
- HY-P3835
-
|
|
DNA/RNA Synthesis
|
Endocrinology
|
|
Mating Factor α (1-6) is a mating factor produced by α-mating type cells of Saccharomyces cerevisiae and an acts as an inhibitor of the initiation of DNA synthesis in the cells .
|
-
- HY-10257
-
|
BAY 11-7083
|
NF-κB
Ferroptosis
Apoptosis
|
Cancer
|
|
BAY 11-7085 (BAY 11-7083) is an inhibitor of NF-κB activation and phosphorylation of IκBα; it stabilizes IκBα with an IC50 of 10 μM .
|
-
- HY-119264
-
|
|
HIF/HIF Prolyl-Hydroxylase
Ras
|
Cancer
|
|
PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .
|
-
- HY-119264A
-
|
|
HIF/HIF Prolyl-Hydroxylase
Ras
|
Cancer
|
|
PRLX-93936 dihydrochloride (Compound 16) is a HIF-1α inhibitor with anticancer activity. PRLX-93936 can inhibit the activated Ras pathway and can be used in the study of relapsed or refractory multiple myeloma .
|
-
- HY-156106
-
|
|
Ligands for E3 Ligase
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
VHL-IN-1 (compound 30) is a ubiquitin E3 ligase von Hippel-Lindau (VHL) inhibitor (dissociation constant Kd=37 nM) that stabilizes and induces HIF-1α transcriptional activity. VHL-IN-1 has potential as a HIF-1α stabilizer and degrader of proteolytically targeted chimeras (PROTACs) .
|
-
- HY-139804
-
-
- HY-W142080
-
|
α-Methyltryptophan
|
mTOR
Autophagy
Apoptosis
Amino Acid Derivatives
|
Metabolic Disease
Cancer
|
|
α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .
|
-
- HY-153475
-
|
|
IRE1
|
Cancer
|
|
IRE1α kinase-IN-9 (compound 2) is a potent IRE-1α inhibitor，exhibits an average IC50 value of <0.1 μM. IRE1α kinase-IN-9 can be used for research in diseases associated with the unfolded protein response or with regulated IRE1-dependent decay (RIDD) .
|
-
- HY-N0375R
-
|
|
Proteasome
NF-κB
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
18α-Glycyrrhetinic acid (Standard) is the analytical standard of 18α-Glycyrrhetinic acid. This product is intended for research and analytical applications. 18α-Glycyrrhetinic acid, a diet-derived compound, is an inhibitor of NF-kB and an activator of proteasome, which serves as pro-longevity and anti-aggregation factor in a multicellular organism. 18α-Glycyrrhetinic acid induces apoptosis .
|
-
- HY-12709
-
-
- HY-163572
-
|
|
PI4P5K
|
Cancer
|
|
PIP5K1α-IN-1 (Compound 3e) is an inhibitor for phosphatidylinositol 4-phosphate 5-kinase type I α (PIP5K1α) with an IC50 of 0.46 μM .
|
-
- HY-172139
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-25 (Compound Djh1) is a selective PI3Kα inhibitor. PI3Kα-IN-25 can be used in triple-negative breast cancer research .
|
-
- HY-131553
-
|
Vitamin E succinate
|
Apoptosis
|
Cancer
|
|
D-α-Tocopherol Succinate (Vitamin E succinate) is an antioxidant tocopherol and a salt form of vitamin E. D-α-Tocopherol Succinate inhibits Cisplatin (HY-17394)-induced cytotoxicity. D-α-Tocopherol Succinate can be used for the research of cancer .
|
-
- HY-151138
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-16 is a potent and orally active α-glucosidase inhibitor with an IC50 value of 3.28 μM. α-Glucosidase-IN-16 can reduce the level of blood glucose in Streptozotocin-induced diabetic rats. Antidiabetic activity .
|
-
- HY-149342
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-29 (compound 19) is a α-glucosidases inhibitor (IC50=1.21 μM, Ki=1.80 μM). α-Glucosidase-IN-29 ca be used for research of diabetes and related diseases .
|
-
- HY-173183
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-87 (Compound 11c) is an orally active α-glucosidase inhibitor with an IC50 value of 119.7 μM. α-Glucosidase-IN-87 has hypoglycemic activity and can be used in the research of metabolic diseases such as diabetes .
|
-
- HY-163907
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-71 (Compound 7h) is a competitive α-glucosidase inhibitor (IC50: 98.0 µM). α-Glucosidase-IN-71 can be used for research of carbohydrate-related diseases, especially type 2 diabetes mellitus .
|
-
- HY-149332
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-26 (Compound 7i) is an α-glucosidase inhibitor (IC50=4.63 µM). α-Glucosidase-IN-26 can be used in the study of type 2 diabetes mellitus (T2DM) .
|
-
- HY-163471
-
|
|
PDGFR
VEGFR
|
Cancer
|
|
PDGFRα/β/VEGFR-2-IN-1 (6f), a multiple PDGFRα/ and VEGFR-2 tyrosine kinase inhibitor, particularly targets PDGFRα, PDGFRβ, and VEGFR-2 kinases with Nano molar concentrations .
|
-
- HY-172138
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-84 (Compound 7j) is a competitive α-glucosidase inhibitor with an IC50 of 50 μM and a Ki of 32 μM. α-Glucosidase-IN-84 holds potential for use in the field of metabolic diseases, such as the study of type 2 diabetes .
|
-
- HY-161281
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-49 (compound C23) is a potent inhibitor of α-Glucosidase, with IC50 of 0.52 μM. α-Glucosidase-IN-49 has oral bioactivity that can reduce blood glucose and improve glucose tolerance in mice .
|
-
- HY-149409
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-31 (compound R1) is an orally active, potent α-Glucosidase inhibitor with an IC50 value of 10.1 μM. α-Glucosidase-IN-31 significantly reduces the blood glucose level and has antidiabetic activity .
|
-
- HY-152170
-
|
|
nAChR
|
Neurological Disease
|
|
bPiDI is a novel selective α6β2 nicotinic receptor antagonist. bPiDI inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
|
-
- HY-12650A
-
-
- HY-168598
-
|
|
Amylases
|
Metabolic Disease
|
|
α-Amylase-IN-9 (Compound 1i) is an inhibitor of α-Amylase with an IC50 value of 14.64 μM, which can be used in diabetes research .
|
-
- HY-P990160
-
|
|
CD3
|
Others
|
|
Anti-Rat TCR alpha/beta Antibody (R73) is a mouse-derived IgG1, κ type antibody inhibitor, targeting to rat TCR alpha/beta.
|
-
- HY-N2223
-
|
Ganodermadiol
|
Glycosidase
|
Metabolic Disease
|
|
Ganoderol B is a potent α-glucosidase inhibitor. Ganoderol B has high α-glucosidase inhibition with an IC50 of 48.5 μg/mL (119.8 μM) .
|
-
- HY-120823
-
-
- HY-W025799
-
|
N-Benzalaniline; N-Phenylbenzylimine
|
Histone Demethylase
|
Cancer
|
|
N-Benzylideneaniline is an inhibitor of xylinostilbene-α,β-dioxygenase (LSD) .
|
-
- HY-126306
-
-
- HY-N14914
-
-
- HY-170606
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-79 (Compound 4d9) is a non-competitive α-Glucosidase inhibitor with an IC50 of 2.11 μM, which is more potent than existing α-Glucosidase inhibitors such as Acarbose (HY-B0089) (IC50 of 327.0 μM) and HXH8r (IC50 of 15.32 μM). α-Glucosidase-IN-79 is non-cytotoxic to human normal hepatocyte (LO2) cells and shows good metabolic stability in rat plasma. α-Glucosidase-IN-79 holds promise for research into type 2 diabetes .
|
-
- HY-129389
-
|
|
Glycosyltransferase
|
Cancer
|
|
Benzyl-α-GalNAc is a potent O-glycosylation inhibitor. Benzyl-α-GalNAc effectively inhibits the proliferation and activation of LX-2 cells and suppresses the expression of collagen I/III, which has good potential for investigation in liver fibrosis. Benzyl-α-GalNAc also significantly enhances the anti-tumour activity of 5-FU (HY-90006) (e.g. pancreatic cancer) by inhibiting O-glycosylation .
|
-
- HY-161421
-
|
|
Glycosidase
|
Metabolic Disease
|
α-Glucosidase-IN-61 (Compd 1j), a competitive α-glucosidase inhibitor, demonstrates excellent inhibition with an IC50 of 0.73 μM. α-Glucosidase-IN-61 (Compd 1j) is used for the research of type 2 diabetes mellitus .
|
-
- HY-168462
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-82 (compound 8l) is a potent inhibitor of α-Glucosidase, with the IC50 of 13.66 μM. α-Glucosidase-IN-82 exhibits a 52-fold increase in inhibitory activity relative to Acarbose (HY-B0089) .
|
-
- HY-147801
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase IIα-IN-3 (Compound 12c) is a DNA intercalative topoisomerase-IIα inhibitor. Topoisomerase IIα-IN-3 arrests cell cycle at the G0/G1 phase and induces apoptosis .
|
-
- HY-14126
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BIO-1211 is a highly selective and orally active α4β1 (VLA-4) inhibitor, with IC50 values of 4 nM and 2 μM for α4β1 and α4β7, respectively .
|
-
- HY-N13173
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-70 (compound 9) is an α-glucosidase inhibitor (IC50=31.1 μM) isolated from the traditional Chinese herbal medicine Swertia mussotii. α-Glucosidase-IN-70 can be used in the research of diabetes .
|
-
- HY-N0877
-
|
|
Na+/K+ ATPase
|
Cancer
|
|
Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively . Anti-cancer activity .
|
-
- HY-N6602R
-
|
|
Apoptosis
Akt
mTOR
MMP
NO Synthase
COX
NF-κB
Autophagy
|
Inflammation/Immunology
Cancer
|
|
α-Solanine (Standard) is the analytical standard of α-Solanine. This product is intended for research and analytical applications. α-solanine, a bioactive component and one of the major steroidal glycoalkaloids in Solanum nigrum, has been observed to inhibit growth and induce apoptosis in cancer cells .
|
-
- HY-14305
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
BMS-582949 (compound 7k) is an orally active and highly selective p38α MAP kinase inhibitor, with IC50 values of 13 nM for p38α, and 50 nM for cellular TNFα. BMS-582949 can be used for research on rheumatoid arthritis .
|
-
- HY-148925
-
|
|
Glycosidase
|
Inflammation/Immunology
|
|
α-Amyrenone is a triterpenoid that occurs naturally in very low concentrations in several oleoresins from Brazilian Amazon species of Protium (Burseraceae). The mixture of α and β-amyrenone inhibits α-glucosidase, and can reduce mechanical hypersensitivity and paw-oedema induced by carrageenan .
|
-
- HY-122247
-
|
|
Kinesin
|
Cancer
|
|
PVZB1194 is a biphenyl-type
inhibitor of Kinesin-5 ATPase activity that binds to the α4/α6 site of the motor domain in a nucleotide competitive manner. PVZB1194 has an IC50 of 0.12 μM for KSP ATPase. PVZB1194 induces mitotic arrest with the formation of a monopolar spindle, and inhibits HeLa cells proliferatio (IC50: 5.5 μM). PVZB1194 can be used in the study of tumors .
|
-
- HY-138097
-
|
|
Chemerin Receptor
Aldehyde Dehydrogenase (ALDH)
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
|
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity .
|
-
- HY-107641
-
|
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications .
|
-
- HY-159179
-
|
|
Integrin
|
Inflammation/Immunology
|
|
α4 integrin receptor antagonist 3 (Compound 11) is an orally active α4integrin receptor antagonist. α4 integrin receptor antagonist 3 can inhibit the adhesion of K562 cells mediated by the interaction between α4β1/VCAM-1 and α4β7/MAdCAM-1, with IC50 values of 130 nM and 2 nM, respectively. α4 integrin receptor antagonist 3 has the potential to be used in the study of dextran sulfate sodium (DSS) colitis mouse model .
|
-
- HY-156018
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-13 (Compound 18a) is a PI3Kα inhibitor (IC50: 2.5 nM). PI3Kα-IN-13 induces tumor cell apoptosis. PI3Kα-IN-13 inhibits cancer cell proliferation with IC50s of 0.75 μM (MCF-7), 3.79 μM (HCT-116), 13.71 μM (MDA-MB-231), 9.85 μM (SW620), respectively. PI3Kα-IN-13 inhibits tumor cell colony formation, migration and invasion .
|
-
- HY-112401
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38 MAP Kinase Inhibitor IV is a highly specific ATP-competitive p38α MAPK inhibitor with IC50s of 0.13 and 0.55 μM for p38α and p38β MAPK, respectively .
|
-
- HY-121141
-
|
|
nAChR
|
Neurological Disease
|
|
Adiphenine is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine has anticonvulsant effects .
|
-
- HY-156571
-
|
|
DGK
|
Cancer
|
|
DGKα-IN-4 (example 432) is a DGKα inhibitor with the IC50 of 0.1 nM, extracted from patent WO2021105117. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-3 has the potential for cancer and immunology study.
|
-
- HY-156569
-
|
|
DGK
|
Inflammation/Immunology
Cancer
|
|
DGKα-IN-2 (example 48) is a DGKα inhibitor with the IC50 of 0.9 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
|
-
- HY-156570
-
|
|
DGK
|
Inflammation/Immunology
Cancer
|
|
DGKα-IN-3 (example 25) is a DGKα inhibitor with the IC50 of 283 nM, extracted from patent WO2021105115. DGKα-IN-2 significantly enhances the anti-tumor effect of anti-PD-1 by increasing the proliferation and function of T cells. DGKα-IN-2 has the potential for cancer and immunology study.
|
-
- HY-B0379A
-
|
|
nAChR
|
Neurological Disease
|
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
|
-
- HY-152479
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-7 is an DNA topoisomerase IIα inhibitor with an IC50 value of 7.7 µM. Topoisomerase IIα-IN-7 has broad-spectrum cytotoxicity to leukemia, lung, colon, melanoma, ovarian, kidney, prostate and breast cancer cells. Topoisomerase IIα-IN-7 has metabolic stability .
|
-
- HY-N0255R
-
|
|
Apoptosis
|
Others
|
|
alpha-Hederin (Standard) is the analytical standard of alpha-Hederin. This product is intended for research and analytical applications. alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway .
|
-
- HY-173130
-
|
|
Glycosidase
|
Metabolic Disease
Inflammation/Immunology
|
|
α-Glucosidase-IN-86 (Compound A4) is an orally active α-glucosidase inhibitor with an IC50 of 2.72 μM. α-Glucosidase-IN-86 has high safety in mice. α-Glucosidase-IN-86 can reduce fasting blood glucose levels, improve glucose tolerance, regulate blood lipids, and has antioxidant effects in diabetic mice. α-Glucosidase-IN-86 can be used for the research of diabetes .
|
-
- HY-U00179
-
-
- HY-17412S
-
|
|
Isotope-Labeled Compounds
Antibiotic
|
Others
|
|
Minocycline-d6 hydrochloride is deuterated labeled Minocycline hydrochloride (HY-17412). Minocycline hydrochloride is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor .
|
-
- HY-135530
-
|
|
Amylases
|
Metabolic Disease
|
|
Chinese gallotannin is a non-specific promiscuous α-amylase inhibitor with a Ki of 0.82 μg/mL for human salivary α-amylase. Chinese gallotannin can be used for the research of diabetes .
|
-
- HY-10231
-
-
- HY-15484
-
|
Pifithrin hydrobromide; PFTα hydrobromide
|
MDM-2/p53
Aryl Hydrocarbon Receptor
Ferroptosis
Apoptosis
|
Cancer
|
|
Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
|
-
- HY-103384
-
|
|
Casein Kinase
|
Cancer
|
|
TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .
|
-
- HY-10401
-
-
- HY-169117
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-74 (Compound 7d), an isatin-thiazole derivative, is a α-glucosidase inhibitor. α-Glucosidase-IN-74 exhibits antidiabetic activity by decreasing glycaemia and triglyceride levels in Streptozotocin (HY-13753)-induced diabetic animals .
|
-
- HY-170797
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-80 (Compound 10n) is a potent competitive inhibitor of α-glucosidase, with an IC50 of 48.4 μM. α-Glucosidase-IN-80 has good pharmacokinetic properties and toxicity profiles and can be used in the research of diabetes-related diseases .
|
-
- HY-130073
-
|
|
NF-κB
Apoptosis
|
Cancer
|
|
Amorfrutin A is the inhibition of NF-κB activation, that inhibits TNF-α-induced IκBα degradation, p65 nuclear translocation, and DNA-binding activity. Amorfrutin A promotes TNF-α-induced apoptosis in HeLa cell through promotion of caspase-3 and PARP proteolysis .
|
-
- HY-163975
-
|
|
Glycosidase
|
Cancer
|
|
α-Glucosidase-IN-72 (compound 5i) is a 2,4-dichloro-N-phenylacetamide derivative and an α-glucosidase inhibitor (IC50: 6 μM). α-Glucosidase-IN-72 does not follow Lipinski's "rule of five" and does not induce cancer .
|
-
- HY-116030
-
|
|
Integrin
|
Metabolic Disease
|
|
JNJ-26076713 is a potent and orally active alpha V integrin antagonist with IC50 values of 2.3 nM and 6.3 nM for alpha(V)beta(3) and alpha(V)beta(5), respectively. JNJ-26076713 inhibits retinal neovascularization .
|
-
- HY-W086896R
-
|
|
Drug Metabolite
|
Inflammation/Immunology
|
|
α-Demethylnaproxen (Standard) is the analytical standard of α-Demethylnaproxen. This product is intended for research and analytical applications. α-Demethylnaproxen is the major metabolite of Nabumetone (HY-B0559), Nabumetone is an orally active COX-2 inhibitor with anti-inflammatory activity .
|
-
- HY-100838
-
|
L-CCG III
|
EAAT
|
Neurological Disease
|
|
cis-α-(Carboxycyclopropyl)glycine (L-CCG III) is a potent, competitive glutamate uptake inhibitor. cis-α-(Carboxycyclopropyl)glycine is a substrate of glutamate transporters (GluT) (EC50: 13 μM, 2 μM for EAAT 1 and EAAT 2, respectively). cis-α-(Carboxycyclopropyl)glycine inhibits a Na +-dependent high-affinity L-glutamate uptake in glial plasmalemmal vesicles (GPV) and synaptosomes .
|
-
- HY-123955
-
|
|
Casein Kinase
CDK
Apoptosis
|
Cancer
|
|
Casein Kinase inhibitor A86 is a potent and orally active casein kinase 1α (CK1α) inhibitor. Casein Kinase inhibitor A86 also inhibits of CDK7 (TFIIH) and CDK9 (P-TEFb). Casein Kinase inhibitor A861 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
|
-
- HY-19707
-
|
IRE1 Inhibitor III
|
IRE1
|
Metabolic Disease
|
|
4μ8C (IRE1 Inhibitor III) is a small-molecule inhibitor of IRE1α.
|
-
- HY-126333
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase II inhibitor 1 (compound 89) is a highly efficient and selective topoisomerase IIα inhibitor .
|
-
- HY-10328
-
|
VX-745
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
Neflamapimod (VX-745) is a potent, blood-brain barrier penetrant, highly selective inhibitor of p38α inhibitor with an IC50 for p38α of 10 nM and for p38β of 220 nM. Neflamapimod (VX-745) possesses anti-inflammatory activity.
|
-
- HY-133718
-
|
(S)-Acarviosin
|
Amylases
|
Others
|
|
Acarviosin, a pseudodisaccharide moiety, is a part of the potent inhibitor of α-amylase .
|
-
- HY-153122A
-
-
- HY-123736
-
|
|
MMP
|
Others
|
|
Ro 32-7315 is a TNF-α converting enzyme (TACE) inhibitor .
|
-
- HY-19710
-
|
|
IRE1
|
Cancer
|
|
MKC3946 is a potent IRE1α inhibitor, used for cancer research.
|
-
- HY-12285
-
|
MLN1117; INK1117; TAK-117
|
PI3K
|
Cancer
|
|
Serabelisib (MLN1117) is a selective p110α inhibitor with an IC50 of 15 nM.
|
-
- HY-16560
-
|
Campathecin; (S)-(+)-Camptothecin; CPT
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM . 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 .
|
-
- HY-149008
-
|
|
Amylases
Cholinesterase (ChE)
|
Inflammation/Immunology
|
|
α-Amylase-IN-3 (Compound 4) is the inhibitor for α-Amylase, AChE and AChE with IC50s of 18.04 μM, 21.04 μM and 22.2 μM, respectively. α-Amylase-IN-3 exhibits antioxidant activity. α-Amylase-IN-3 can be used in research of diabetes and oxidative stress associated disease .
|
-
- HY-B0219A
-
|
|
Xanthine Oxidase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Allopurinol sodium is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 μM. Allopurinol sodium can be used in the research of hyperuricemia and gout. Allopurinol sodium decreases the expression of HIF-1α and HIF-2α protein. Allopurinol sodium shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .
|
-
- HY-B0219
-
|
|
Xanthine Oxidase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Allopurinol is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 μM. Allopurinol can be used in the research of hyperuricemia and gout. Allopurinol decreases the expression of HIF-1α and HIF-2α protein. Allopurinol shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .
|
-
- HY-162518
-
|
|
Kinesin
Microtubule/Tubulin
|
Cancer
|
|
Eg5-IN-3 (5) is an Eg5 inhibitor that targets the novel allosteric pocket (α4/α6/L11). Eg5-IN-3 (5) causes tubulin assembly distortion with irregular morphology, resulting in a typical mitotic arrest similar to Monastrol (HY-101071A) .
|
-
- HY-156091
-
|
|
PI3K
HDAC
|
Cancer
|
|
PI3Kα/HDAC6-IN-1 (compound 21j) is a dual PI3Kα/HDAC6 inhibitor with IC50 of 2.9 and 26 nM, respectively. PI3Kα/HDAC6-IN-1 also inhibits AKT(Ser473) phosphorylation and induces the accumulation of acetylated α-tubulin without affecting acetylated histones H3 and H4. PI3Kα/HDAC6-IN-1 efficiently inhibits L-363 cell line (IC50=0.17 μM) and has good anti-cancer activity .
|
-
- HY-146305
-
-
- HY-10822
-
|
BGC 945; ONX-0801
|
Thymidylate Synthase
|
Others
|
|
Idetrexed is a thymidylate synthase inhibitor specifically transported into alpha-folate receptor (alpha-FR)-overexpressing tumors. BGC 945 inhibited thymidylate synthase with a Ki of 1.2 nmol/L .
|
-
- HY-149533
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-34 (compound 7f) is a potent α-glucosidase inhibitor (IC50: 2.90 μM) and can be used in the study of type 2 diabetes and hyperglycemia .
|
-
- HY-B0942S
-
-
- HY-120337
-
|
|
Choline Kinase
|
Cancer
|
|
V-11-0711 is a potent and selective choline kinase alpha (ChoKα) inhibitor with an IC50 of 20 nM. V-11-0711 causes a reversible growth arrest in HeLa cells .
|
-
- HY-16031B
-
|
NSC710464 dihydrochloride
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
AFP464 (dihydrochloride) (NSC710464 (dihydrochloride)) is the hydrochloride form of AFP464 and is a potent HIF-1α inhibitor with an IC50 value of 0.25 μM. It is also an activator of aryl hydrocarbon receptor (AhR).
|
-
- HY-149532
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-33 (compound 7c) is a potent α-glucosidase inhibitor (IC50: 2.39 μM) and can be used in the study of type 2 diabetes and hyperglycemia .
|
-
- HY-N3115
-
|
|
Others
|
Inflammation/Immunology
|
|
Palbinone is a terpenoid isolated from the roots of Paeonia albiflora Pallas, potently inhibits 3α-hydroxysteroid dehydrogenase (3α-HSD), with an IC50 of 46 nM. Anti-inflammatory activity .
|
-
- HY-108531
-
|
|
RAR/RXR
|
Cancer
|
|
ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis .
|
-
- HY-108531A
-
|
|
RAR/RXR
|
Cancer
|
|
ER 50891 quarterhydrate is a potent antagonist of retinoic acid receptor α(RARα). ER 50891 quarterhydrate significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis .
|
-
- HY-W019838S
-
-
- HY-161968
-
|
|
EGFR
PI3K
|
Cancer
|
|
EGFR/PI3Kα-IN-1 (compound 30k) is a dual EGFR/PI3Kα inhibitor with IC50 values of 3.6 nM (EGFRL858R/T790M) and 30 nM (PI3Kα), respectively. EGFR/PI3Kα-IN-1 can inhibit tumor cell proliferation and has anticancer activity .
|
-
- HY-110208
-
BRD9876
1 Publications Verification
|
Kinesin
Microtubule/Tubulin
|
Cancer
|
|
BRD9876 is the “rigor” inhibitor that locks kinesin-5 (Eg5) in a state with enhanced microtubules (MTs) binding, leading to bundling and stabilization of MTs. BRD9876 interacts with the tyrosine 104 residue that is part of the α4-α6 allosteric binding pocket. BRD9876 specifically targets microtubule-bound Eg5 and selectively inhibits myeloma over CD34 cells. BRD9876 has the potential for multiple myeloma (MM) research .
|
-
- HY-N2566
-
|
|
DNA/RNA Synthesis
PI3K
Apoptosis
|
Cancer
|
|
Euscaphic acid, a DNA polymerase inhibitor, is a triterpene from the root of the R. alceaefolius Poir. Euscaphic inhibits calf DNA polymerase α (pol α) and rat DNA polymerase β (pol β) with IC50 values of 61 and 108 μM . Euscaphic acid induces apoptosis .
|
-
- HY-123954
-
|
Casein Kinase inhibitor A51
|
Casein Kinase
CDK
Apoptosis
|
Cancer
|
|
BTX-A51 (Casein Kinase inhibitor A51) is a potent and orally active casein kinase 1α (CK1α) inhibitor. BTX-A51 induces leukemia cell apoptosis, and has potent anti-leukemic activities .
|
-
- HY-12753AS
-
|
SR35021-d7 hydrochloride
|
Thyroid Hormone Receptor
Isotope-Labeled Compounds
|
Cardiovascular Disease
|
|
Debutyldronedarone-d7 hydrochloride is deuterated labeled Debutyldronedarone hydrochloride (HY-12753A). Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
|
-
- HY-12753AR
-
|
SR35021 (hydrochloride) (Standard)
|
Thyroid Hormone Receptor
|
Cardiovascular Disease
|
|
Debutyldronedarone (hydrochloride) (Standard) is the analytical standard of Debutyldronedarone (hydrochloride). This product is intended for research and analytical applications. Debutyldronedarone (SR35021) hydrochloride, the main metabolite of Dronedarone, is a selective thyroid hormone receptor α1 (TRα1) inhibitor. Debutyldronedarone hydrochloride inhibits T3 binding to TRα1 and TRβ1 by 77% and 25%, respectively. Debutyldronedarone hydrochloride can be used for the research of arrhythmic .
|
-
- HY-P5681
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Human α-Defensin 6, a 32-residue cysteine-rich peptide, can inhibit bacterial invasion and contribute to the mucosal immunity. Human α-Defensin 6 forms ordered self-assembly fibrils and nanonets that surround and entangle bacteria after stochastic binding to bacterial surface proteins. Human α-Defensin 6 also inhibits C. albicans biofilm formation .
|
-
- HY-115822
-
|
|
Amino Acid Decarboxylase
Glutathione S-transferase
|
Metabolic Disease
|
|
α-Fluoromethylhistidine dihydrochloride is a potent irreversible inhibitor of histidine decarboxylase (HDC) and glutathione S-transferase, demonstrating significant potential in studying histidine metabolism and drug metabolism processes. α-Fluoromethylhistidine dihydrochloride offers an effective approach to inhibit enzymes involved in these metabolic pathways. α-Fluoromethylhistidine dihydrochloride has implications for drug development by revealing off-target effects that may influence physiological drug metabolism and elimination mechanisms.
|
-
- HY-N3002
-
|
4-Hydroxyphenyl α-D-glucopyranoside
|
Tyrosinase
|
Neurological Disease
Metabolic Disease
Cancer
|
|
α-Arbutin (4-Hydroxyphenyl α-D-glucopyranoside) is a tyrosinase inhibitor, which is used as an effective skin whiteners. α-Arbutin is promising for research of various diseases such as hyperpigmentation disorders, types of cancers, central nervous system disorders, osteoporosis, diabetes .
|
-
- HY-152158
-
|
|
Glycosidase
|
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-133807
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research .
|
-
- HY-159945
-
|
|
α-synuclein
|
Neurological Disease
|
|
Tau Protein/α-synuclein-IN-2 (Compound 14T) is a blood-brain barrier penetrating tau and α-syn inhibitor. Through its thiourea linker structure, Tau Protein/α-synuclein-IN-2 dose-dependently reduces α-syn oligomerization. In biosensor cells, Tau Protein/α-synuclein-IN-2 prevents the seeding effect of tau aggregation. In the M17D neuroblastoma model, Tau Protein/α-synuclein-IN-2 exhibits anti-inclusion effects. Additionally, Tau Protein/α-synuclein-IN-2 reduces Aβ plaque formation. Tau Protein/α-synuclein-IN-2 holds promise for Alzheimer's disease and Parkinson's disease research.
|
-
- HY-105217
-
|
FCE 26073
|
5 alpha Reductase
|
Metabolic Disease
|
|
Turosteride is a selective 5 alpha-reductase inhibitor, with IC50 values of 55 and 53 nM for human and rat prostatic 5 alpha-reductases, respectively. Turosteride can reduce the prostate and seminal vesicle weights .
|
-
- HY-11087
-
|
SD-06
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
SD 0006 (SD-06) is an orally active, selective, ATP-competitive and potent diaryl pyrazole inhibitor of p38α MAP kinase, with an IC50 of 110 nM for p38α .
|
-
- HY-115840
-
|
|
Apoptosis
|
Cancer
|
|
ICL-CCIC-0019 is an inhibitor of choline kinase α (CHKα). ICL-CCIC-0019 induces G1 block, endoplasmic reticulum stress apoptosis in cancer cell lines .
|
-
- HY-12012
-
-
- HY-108623
-
|
CP-80,633
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Atizoram (CP-80,633), a cyclic nucleotide phosphodiesterase (PDE4) inhibitor, elevates plasma cyclic AMP levels and decreases tumor necrosis factor-α (TNFα) production in mice .
|
-
- HY-B0194S
-
-
- HY-16031
-
|
NSC710464 free base
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
AFP464 free base (NSC710464 free base), is an active HIF-1α inhibitor with an IC50 of 0.25 μM, also is a potent aryl hydrocarbon receptor (AhR) activator.
|
-
- HY-N0374
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Licochalcone C could inhibit α-glucosidase, with IC50s of <100 nM and 92.43 μM for α-glucosidase and protein tyrosine phosphatase 1B (PTP1B), respectively.
|
-
- HY-P99148
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Anti-Mouse/Rat/Rabbit TNF alpha Antibody (TN3-19.12) is an anti-mouse/rat/rabbit TNF alpha IgG antibody inhibitor derived from host Armenian Hamster.
|
-
- HY-N10413
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Diphlorethohydroxycarmalol, a kind of phlorotannin, is an orally active α-glucosidase and α-amylase inhibitor with IC50s of 0.16 mM and 0.53 mM, respectively. Diphlorethohydroxycarmalol has anti-diabetic activities .
|
-
- HY-171300
-
-
- HY-147767
-
|
|
PI3K
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
PI3Kα-IN-6 (Compound 5b) is a PI3Kα inhibitor. PI3Kα-IN-6 exhibits anticancer potential and no toxicity in normal cells. PI3Kα-IN-6 increases generation of ROS, reduces mitochondrial membrane potential (MMP) and induces apoptosis .
|
-
- HY-N7264
-
-
- HY-146021
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-2 (compound 5) is a potent DNA-binding ligands and topoisomerase IIα inhibitor. Topoisomerase IIα-IN-2 exhibits high antiproliferative activity against human cancer cell lines. Topoisomerase IIα-IN-2 significantly induces DNA damage and arrests cancer cells at G2/M phase .
|
-
- HY-N0328R
-
|
α-Mangostin (Standard)
|
Fungal
Reactive Oxygen Species
Bacterial
Apoptosis
Virus Protease
|
Cancer
|
|
alpha-Mangostin (Standard) is the analytical standard of alpha-Mangostin. This product is intended for research and analytical applications. alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
|
-
- HY-123349
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
5α-Hydroxy-6-keto cholesterol is major metabolite of β-epoxide (5α,6β-epoxycholesterol) during direct exposure of intact cultured human bronchial epithelial cells (16-HBE) to ozone. 5α-Hydroxy-6-keto cholesterol inhibits cholesterol synthesis with an IC50 of 350 nM .
|
-
- HY-170553
-
|
|
α-synuclein
|
Neurological Disease
|
|
ZPD-2 inhibits the aggregation of C-terminally truncated and full-length α-synuclein. ZPD-2 inhibits the formation and fibrillation of α-Syn, thereby preventing its propagation. ZPD-2 can be used in research of Parkinson's disease .
|
-
- HY-111255
-
SPD304
5 Publications Verification
|
TNF Receptor
|
Cancer
|
|
SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 μM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α .
|
-
- HY-111255A
-
|
|
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 μM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α .
|
-
- HY-123323
-
|
|
5 alpha Reductase
|
Endocrinology
|
|
MK-0434 is an orally active steroid 5α-reductase inhibitor. MK-0434 specifically inhibits steroid 5α-reductase, thereby reducing the level of dihydrotestosterone (DHT) in the body. MK-0434 can be used in the study of benign prostatic hyperplasia .
|
-
- HY-171301
-
-
- HY-157958
-
|
|
nAChR
|
Neurological Disease
|
|
α7 nAChR modulator-3 (Compound 6p) is a α7 nAChR positive allosteric Modulator with a IC50 value of 1.3 μM. α7 nAChR Modulator-3 can be used to inhibit auditory gating defects in a mouse schizophrenic model .
|
-
- HY-147708
-
|
|
Calcium Channel
|
Cancer
|
|
T-Type calcium channel inhibitor 2 (compound 6g) is a potent T-type calcium channel inhibitor with IC50s of 31.0, 83.1, 69.3 µM for Cav3.1 (α1G), Cav3.2 (α1H), Cav3.3 (α1I) (α1H), respectively. T-Type calcium channel inhibitor 2 shows cytotoxicity for A549, HCT-116 cells with IC50s of 5.0, 6.4 µM, respectively .
|
-
- HY-105997
-
|
|
p38 MAPK
|
Others
|
|
AZD 6703 is a p38α MAP kinase inhibitor with activity in inflammatory diseases.
|
-
- HY-164358
-
-
- HY-13261
-
A66
4 Publications Verification
|
PI3K
|
Cancer
|
|
A66 is a highly specific and selective p110α inhibitor with an IC50 of 32 nM.
|
-
- HY-153122
-
-
- HY-135674
-
|
|
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
SR-318 is a potent and highly selective p38 MAPK inhibitor with IC50s of 5 nM, 32 nM and 6.11 μM for p38α, p38β and p38α/β, respectively. SR-318 potently inhibits the TNF-α release in whole blood with an IC50 of 283 nM. SR-318 has anti-cancer and anti-inflammatory activity .
|
-
- HY-173039
-
|
|
Microtubule/Tubulin
Keap1-Nrf2
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
α-Tubulin polymerization-IN-1 (Compound 8l) is an inhibitor for α-Tubulin polymerization. α-Tubulin polymerization-IN-1 modulates the NRF2/KEAP-1 signaling pathway, induces ROS generation in PC-3 cell, thereby inducing apoptosis in PC-3. α-Tubulin polymerization-IN-1 inhibits the proliferation of PC-3 cell with a GI50 of 0.17 µM, arrests the cell cycle at G2/M phase. α-Tubulin polymerization-IN-1 exhibits antitumor efficacy in mouse model .
|
-
- HY-P10393
-
|
ERα (295-311)
|
Apoptosis
|
Cancer
|
|
ERα17p (ERα 295-311) is the epitope of the CaM binding site on the estrogen receptor α (ER), which interacts with calmodulin (CaM) in a calcium-dependent manner. ERα17p regulates the migration of cancer cells MCF-7, SK-BR-3, T47D, and MDA-MB-231 through Rho/ROCK and PI3K/Akt signaling pathways. ERα17p inhibits proliferations of breast cancer cells, induces apoptosis, and inhibits tumor growth in mouse models .
|
-
- HY-13281
-
|
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 hydrochloride induces apoptosis .
|
-
- HY-107834
-
PIK-75
5 Publications Verification
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 induces apoptosis .
|
-
- HY-116563
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-24 (WR23) is a PI3Kα inhibitor with an IC50 of 0.025 μM and exhibits a significant pAkt Ser473 suppression effect. PI3Kα-IN-24 can be utilized in cancer research .
|
-
- HY-156578
-
|
|
DGK
HIV
|
Infection
Cancer
|
|
DGKα-IN-8 (Example 51) is a DGKα inhibitor (IC50=22.491 nM; EC50=0.256 nM). DGKα-IN-8 can be used to study cancer, including solid tumors, and viral infections, such as HIV or hepatitis B virus infection .
|
-
- HY-144295
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3Kα-IN-5 (compound 6 ab) is a potent PI3Kα/mTOR inhibitor, with an IC50 of 0.7 nM and 3.3 nM, respectively. PI3Kα-IN-5 can be used for the research of colorectal cancer .
|
-
- HY-149313
-
|
|
Amylases
|
Metabolic Disease
|
|
α Amylase-IN-1 (Compound 11) is an α-Amylase inhibitor with an IC50 value of 0.5509 μM. α Amylase-IN-1 has antioxidant activity with an IC50 value of 53.49 μM for scavenging DPPH free radicals. IC50 can be used in the study of diabetes and oxidative stress-related diseases.
|
-
- HY-158370
-
|
|
Casein Kinase
|
Cancer
|
|
CK2-IN-11 (32) is an allosteric CK2 inhibitor, with high selectivity for CK2 with IC50 values of 19.3 nM and 15.6 nM for the CK2α2β2 and the CK2α′2β2 isoforms, respectively .
|
-
- HY-116446
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
Pironetin is an α/β unsaturated lactone isolated from Streptomyces species. Pironetin binds to α-tubulin and is a potent inhibitor of microtubule polymerization, and has cell cycle arrest and antitumor activity .
|
-
- HY-155030
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-25 (Compound (R)-8k) is a competitive inhibitor of α-glucosidase, with an IC50 of 1.19μM and can be used for anti-diabetic research .
|
-
- HY-10801
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
CAY10650 is a highly potent cytosolic phospholipase A2α (cPLA2α) inhibitor with an IC50 value of 12 nM. CAY10650 suppresses lipid droplets formation and PGE2 secretion .
|
-
- HY-108697A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
(Rac)-PT2399 (Compound 10e), the racemate of PT2399, acts as a potent and specific hypoxia-inducible factor 2a (HIF-2α) inhibitor with an IC50 of 0.01 μM .
|
-
- HY-N3706
-
|
|
Fungal
|
Infection
|
|
Dehydro-α-lapachone can be isolated from the methanol extract of stems of Catalpa ovata G Don. Dehydro-α-lapachone inhibits mycelial growth of Botrytis cinerea with IC50 value 0.41 mg/L .
|
-
- HY-161671
-
|
|
nAChR
|
Neurological Disease
Inflammation/Immunology
|
|
GAT2711 is a full agonist of α9 nAChR with an EC50 of 230 nM. GAT2711 shows 340-fold selective for α9 over α7 nAChRs. GAT2711 inhibits ATP-induced IL-1β release in THP-1 cells. GAT2711 retains full analgesic activity in α7 nAChR knockout mice .
|
-
- HY-173049
-
|
|
α-synuclein
|
Neurological Disease
|
|
2N4R Tau/α-Syn against-1 (Compound 4d) targets α-synuclein and tau protein, inhibits the fibrillation and oligomer formation of α-synuclein and tau proteins, exhibits disaggregation activity on Aβ fibers. 2N4R Tau/α-Syn against-1 can be used in research of Parkinson's disease and Alzheimer's disease .
|
-
- HY-173337
-
|
|
HSP
Interleukin Related
|
Cancer
|
|
HSP90α-IN-1 is a HSP90α inhibitor (IC50 = 111 nM) that exhibits senolytic activity across various cellular senescence models. HSP90α-IN-1 is related to the xanthinic family. HSP90α-IN-1 is involved in research on combating age-related inflammaging and diseases, including cancer, and possibly extend a healthy lifespan .
|
-
- HY-149427
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-12 (compound 13) is a highly selective PI3Kα inhibitor (IC50: 1.2 nM). PI3Kα-IN-12 inhibits HCT-116 and U87-MG with IC50s values of 0.83 and 1.25 μM, respectively. PI3Kα-IN-12 (40 mg/kg; IP) causes tumor regression in a U87-MG cell line xenograft mouse model .
|
-
- HY-12398A
-
|
|
VD/VDR
|
Metabolic Disease
Inflammation/Immunology
|
|
TEI-9648, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9648 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9648 also inhibits HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9648 has the potential for bone metabolism research .
|
-
- HY-19763
-
|
BEBT-908
|
PI3K
|
Cancer
|
|
Ifupinostat is a selective PI3Kα inhibitor extracted from patent US/20120088764A1, Compound 243, has an IC50<0.1 μM, PI3Kα inhibitor 1 also inhibits HDAC (0.1 μM≤IC50≤1 μM) .
|
-
- HY-149665
-
|
|
DGK
|
Cancer
|
|
BMS-684 is a selective DGKα inhibitor with an IC50 of 15 nM. BMS-684 inhibits DGKα kinase activity with >100-fold selectivity over the related DGK type I family members DGKβ and DGKγ. BMS-684 does not inhibit any of the other seven DGK isozymes .
|
-
- HY-128463S
-
|
|
COX
Reactive Oxygen Species
|
Metabolic Disease
|
|
N-tert-Butyl-α-phenylnitrone-d14 is the deuterium labeled N-tert-Butyl-α-phenylnitrone . N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier .
|
-
- HY-129619
-
|
|
SNIPERs
Estrogen Receptor/ERR
|
Cancer
|
|
SNIPER(ER)-87 consists of an inhibitor of apoptosis protein (IAP) ligand LCL161 derivative that is conjugated to the estrogen receptor α (ERα) ligand 4-hydroxytamoxifen by a PEG linker, and efficiently degrades the ERα protein (IC50=0.097 μM). SNIPER(ER)-87 preferentially recruits XIAP to ERα in the cells, and XIAP is the primary E3 ubiquitin ligase responsible for the SNIPER(ER)-87-induced ERα degradation .
|
-
- HY-107588
-
TC-I 15
1 Publications Verification
|
Integrin
|
Cardiovascular Disease
|
|
TC-I 15 (TC-I-15) is a type of allosteric collagen-binding integrin α2β1 inhibitor, and it also inhibits α1β1 and α11β1. TC-I 15 inhibits platelet adhesion to collagen and thrombus deposition. TC-I 15 prevents the formation of a pre-metastatic microenvironment by inhibiting the uptake of cancer-associated fibroblast (CAF) extracellular vesicles (EVs) by lung fibroblasts, which reduces the metastasis of salivary gland adenocystic carcinoma (SACC) to the lungs in mouse models, .
|
-
- HY-137038
-
|
TLCK hydrochloride
|
Caspase
Ser/Thr Protease
|
Cancer
|
|
N-alpha-Tosyl-Lys chloromethyl ketone hydrochloride (TLCK hydrochloride) is an irreversible inhibitor for serine protease, which inhibits trypsin and trypsin-like protease by alkylating histidine residues in their active site. N-alpha-Tosyl-Lys chloromethyl ketone hydrochloride inhibits caspase-3, caspase-6 and caspase-7, with IC50s of 12.0, 54.5 and 19.3 μM, respectively. N-alpha-Tosyl-Lys chloromethyl ketone hydrochloride induces apoptosis in cell HL-60, and inhibits the decrease in mitochondrial transmembrane potential during apoptosis .
|
-
- HY-125833
-
|
|
Cytochrome P450
Aryl Hydrocarbon Receptor
Apoptosis
|
Cancer
|
|
Alpha-Naphthoflavone is an orally active flavonoid that is a potent, competitive inhibitor of aromatase< b>aromatase. < b > IC < sub > 50 < / sub > < / b > and < b > K < sub > I < / sub > < / b > value were 0.5 and 0.2 microns. Alpha-Naphthoflavone can inhibit cell proliferation and induce apoptosis .
|
-
- HY-156567
-
|
|
DGK
|
Metabolic Disease
|
|
AMB639752 is a potent DGKα inhibitor. AMB639752 restores restimulation induced cell death (RICD) in SAP deficient lymphocytes by inhibiting DGKα in intact cells. AMB639752 can be used for X-linked lymphoproliferative disease 1(XLP-1) research .
|
-
- HY-128041
-
|
Hydroxyfarnesyl phosphate
|
Farnesyl Transferase
|
Others
|
|
α-hydroxy Farnesyl phosphonic acid is a nonhydrolyzable analog of farnesyl pyrophosphate which acts as a competitive inhibitor of farnesyl transferase (FTase). At concentrations greater than 1 μM, α-hydroxy farnesyl phosphonic acid inhibits the processing of Ras in Ha-ras-transformed NIH3T3 cells.
|
-
- HY-N15497
-
|
|
Reactive Oxygen Species
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Terpestacin is found in Phoma exigua var. heteromorpha. Terpestacin binds to UQCRB to inhibit the production of mitochondrial ROS and HIF-1α. Terpestacin inhibits tumor angiogenesis in the FM3A breast cancer cell xenograft mouse model. Terpestacin has antitumor activity and phytotoxicity .
|
-
- HY-159852
-
|
|
PI3K
Akt
|
Cancer
|
|
BBO-10203 (Compound 758) binds to the RBD region of PI3Kα, and inhibits the binding of K-, H-, and N-Ras to PI3Kα. BBO-10203 inhibits pAKT with an IC50 < 0.1 pM in BT474 cell .
|
-
- HY-N6968
-
|
Humulene; α-Caryophyllene
|
NO Synthase
COX
|
Inflammation/Immunology
|
|
α-Humulene is a main constituent of Tanacetum vulgare L. (Asteraceae) essential oil with anti-inflammation (IC50=15±2 μg/mL). α-Humulene inhibits COX-2 and iNOS expression .
|
-
- HY-143224
-
|
|
CD47
|
Cancer
|
|
NCGC00138783 is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 µM. NCGC00138783 directly blocks the interaction between CD47 and SIRPα axis .
|
-
- HY-U00037
-
|
PLA 725
|
Phospholipase
|
Inflammation/Immunology
|
|
Ecopladib is a sub-micromolar inhibitor of cytosolic phospholipase A2α (cPLA2α), with IC50s of 0.15 μM and 0.11 μM in the GLU micelle and rat whole blood assays, respectively.
|
-
- HY-16194
-
-
- HY-145678
-
-
- HY-112502B
-
|
Adenosine 5'-(α,β-methylene)diphosphate sodium
|
CD73
|
Cancer
|
|
MethADP (sodium salt) (Adenosine 5'-(α,β-methylene)diphosphate (sodium)) is a specific CD73 inhibitor.
|
-
- HY-163005
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-43 (compound AS14) is an α-glucosidase inhibitor (IC50: 4.32 μM) with acute hypoglycemic activity. α-Glucosidase-IN-43 exhibits safety and in vivo efficacy, is nontoxic to normal mouse fibroblasts, and is able to rescue streptozotocin (HY-13753)-induced diabetic rats. α-Glucosidase-IN-43 can be used to study postprandial hyperglycemia in diabetic patients .
|
-
- HY-E70299
-
|
ST3GAL5
|
TGF-beta/Smad
|
Cancer
|
|
ST3 β-Gal α-2,3-Sialyltransferase 5 (ST3GAL5) is a glycosphingolipid (GSL) biosynthetic enzyme that can inhibit TGF-β-induced epithelial-mesenchymal transition (EMT), invasion, and metastasis both in vivo and in vitro. ST3 β-Gal α-2,3-Sialyltransferase 5 can be used in cancer research .
|
-
- HY-B0135
-
|
|
NKCC
GABA Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-12399
-
MKC9989
1 Publications Verification
|
IRE1
|
Cancer
|
|
MKC9989 is a Hydroxy aryl aldehydes (HAA) inhibitor and also inhibits IRE1α with an IC50 of 0.23 to 44 μM.
|
-
- HY-N0255
-
|
α-Hederin
|
Apoptosis
|
Others
Cancer
|
|
alpha-Hederin (α-Hederin), a monodesmosidic triterpenoid saponin, exhibits promising antitumor potential against a variety of human cancer cell lines. alpha-Hederin could inhibit the proliferation and induce apoptosis of gastric cancer accompanied by glutathione decrement and reactive oxygen species generation via activating mitochondrial dependent pathway .
|
-
- HY-107553
-
|
|
HSP
Apoptosis
|
Cancer
|
|
Chetomin, an active component of Chaetomium globosum, is a heat shock protein 90/hypoxia-inducible factor 1 alpha (Hsp90/HIF1α) pathway inhibitor. Chetomin is a potent, nontoxic non-small cell lung cancer cancer stem cells (NSCLC CSC)-targeting molecule .
|
-
- HY-16716
-
|
RG1662; RO5186582
|
GABA Receptor
|
Neurological Disease
|
|
Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
|
-
- HY-163433
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-57 (Compound 10c) is a competitive and orally active α-glucosidase inhibitor with an IC50 value of 0.180 μM and a Ki of 0.15 μM. α-Glucosidase-IN-57 can reduce fasting and overall blood glucose levels in mice, and can be used for anti-diabetes research .
|
-
- HY-144695
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .
|
-
- HY-N0901AR
-
|
|
α-synuclein
|
Neurological Disease
Cancer
|
|
Corynoxine B Standard is an analytical standard for Corynoxine B. This product is intended for research and analytical applications. Corynoxine B is an alkaloid-type autophagy inducer and α-synuclein aggregation inhibitor that ameliorates Mn-induced dysregulation of autophagy and enhances the clearance of α-synuclein (α-syn) in Parkinson's disease mice .
|
-
- HY-168841
-
-
- HY-116248
-
|
|
RAR/RXR
Apoptosis
|
Cancer
|
|
Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity .
|
-
- HY-169411
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-77 (Compound H7) is a non-competitive inhibitor for α-glucosidase with an IC50 of 1.25 μM. α-Glucosidase-IN-77 lowers blood glucose levels, improves glucose tolerance, regulates intestinal microbiota, and exhibits hepatoprotective effect in mouse type 2 diabetes model .
|
-
- HY-147983
-
|
|
PI3K
Reactive Oxygen Species
Apoptosis
|
Cancer
|
|
PI3Kα-IN-8 (Compound 9g) is a selective PI3Kα inhibitor with an IC50 of 0.012 μM. PI3Kα-IN-8 increases intracellular reactive oxygen species level, decreases mitochondrial membrane potential and induces apoptosis .
|
-
- HY-N12650
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Kaempferol 3-O-alpha-L-(2, 3-di-Z-p-coumaroyl) rhamnoside (compound 42) is a flavonol that can be isolated from Platanus Occidentalis. Kaempferol 3-O-alpha-L-(2, 3-di-Z-p-coumaroyl) rhamnoside is an inhibitor of alpha-amylase and DPP IV .
|
-
- HY-117106
-
|
|
GABA Receptor
|
Others
|
|
PNU-107484A is a GABAA receptor ligand that exhibits target activity mechanisms dependent on α isoforms. In the α1β2γ2 subtype, PNU-107484A acts as a positive allosteric modulator, enhancing GABA-induced Cl - currents, while it inhibits the currents in the α3β2γ2 and α6β2γ2 subtypes. The half-maximal concentrations for the α1β2γ2, α3β2γ2, and α6β2γ2 subtypes are 3.1, 4.2, and 3.5 μM, respectively. PNU-107484A can be used as a probe to investigate the physiological roles of different α isoform subtypes .
|
-
- HY-168431
-
|
AVX420
|
Phospholipase
|
Cancer
|
|
GK420 (AVX420) is a potent inhibitor of cytosolic phospholipase A2α (cPLA2α), with the XI(50) of 0.0016. GK420 inhibits arachidonic acid release with the EC50 of 0.09 μM. GK420 plays an important role in cancer research .
|
-
- HY-15468
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
IOX2 is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 can be used in the study of thrombotic diseases .
|
-
- HY-10403
-
-
- HY-158341
-
|
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
|
IOX5 is a selective prolyl hydroxylase (PHD) inhibitor with an IC50 of 0.19 μM for PHD2. IOX5 stabilizes HIF-1α in acute myeloid leukemia (AML) cells, inhibits cell proliferation and induces apoptosis. IOX5 has anti-leukemia activity .
|
-
- HY-15468A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Cancer
|
|
IOX2 sodium is a specific prolyl hydroxylase-2 (PHD2) inhibitor with IC50 of 22 nM. IOX2 sodium regulates platelet function and arterial thrombosis by upregulating HIF-1α expression and inhibiting ROS production. IOX2 sodium can be used in the study of thrombotic diseases .
|
-
- HY-120111
-
|
MW01-18-150SRM
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
- HY-122094
-
-
- HY-16294
-
|
|
GSK-3
|
Cancer
|
|
LY2090314 is a potent inhibitor of glycogen synthase kinase-3 (GSK-3) with IC50 values of 1.5 nM and 0.9 nM for GSK-3α and GSK-3β, respectively.
|
-
- HY-N0375
-
-
- HY-P991265
-
|
|
Interleukin Related
|
Cancer
|
|
OSE-703 is a humanized monoclonal antibody inhibitor targeting interleukin-7 receptor α subunit (IL-7Rα). OSE-703 is promising for research of tumors and respiratory diseases .
|
-
- HY-B0942R
-
|
|
Reference Standards
nAChR
Bacterial
|
Neurological Disease
|
|
Benzethonium (chloride) (Standard) is the analytical standard of Benzethonium (chloride). This product is intended for research and analytical applications. Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes.
|
-
- HY-N7729
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
Sekikaic acid is an α-glucosidase (Glucosidase) and α-amylase (Amylases) inhibitor with hypolipidemic, antioxidant and antidiabetic activities. Sekikaic acid significantly reduces LDL, total cholesterol, and total glyceride levels and causes pancreatic beta cell regeneration .
|
-
- HY-138063
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Siegeskaurolic acid is an orally active anti-inflammatory agent. Siegeskaurolic acid inhibits the productions of nitric oxide (NO), prostaglandin E(2) (PGE(2)), tumor necrosis factor-alpha (TNF-alpha) and the activationon of nuclear factor-kappaB .
|
-
- HY-143268
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
HPA-IN-1 (Compound 1) is a potent and selective human pancreatic α-amylase (HPA) inhibitor with IC50 values of 12.0 μM and 410.4 μM against HPA and α-glucosidase, respectively .
|
-
- HY-108431
-
MN58b
1 Publications Verification
|
Apoptosis
|
Cancer
|
|
MN58b is a selective choline kinase α (CHKα) inhibitor, and results in inhibition of phosphocholine synthesis. MN58b reduces cell growth through the induction of apoptosis, and also has antitumoral activity .
|
-
- HY-N13195
-
|
|
5 alpha Reductase
|
Others
|
|
(15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one shows a 5a-reductase inhibitory activity with an IC50 value of 41.9 μM. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one inhibits the growth of the ventral prostate induced by testosterone in rat. (15α)-15,26-Dihydroxylanosta-7,9(11),24-trien-3-one is promising for research of benign prostatic hyperplasia (BPH) as well as other 5α-dihydrotestosterone (DHT)-related disorders, such as acne and male pattern baldness .
|
-
- HY-168185
-
|
|
Glycosidase
Phosphatase
Amylases
|
Metabolic Disease
|
|
α-glucosidase/PTP1B-IN-1 (compound 8a) is a potent α-glucosidase and PTP1B inhibitor with an IC50 value of 66.3 μM and 47.0 μM, respectively. α-glucosidase/PTP1B-IN-1 exhibits excellent activities against α-amylase with an IC50 of 30.62 μM. α-glucosidase/PTP1B-IN-1 can dock into the active pockets of α-glucosidase and PTP1B. α-glucosidase/PTP1B-IN-1 has potential to reduce the postprandial blood glucose and is used for Type 2 diabetes mellitus .
|
-
- HY-W263279
-
|
(E)-Wy-8678
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
(E)-Guanabenz ((E)-Wy-8678) is an orally active central α2-adrenoceptor agonist. (E)-Guanabenz has antihypertensive activity, acts via stimulating central α2-adrenoceptors, and reducing net sympathetic outflow into the periphery. (E)-Guanabenz also directly binds to and inhibits GADD34, and has neuroprotective activity. (E)-Guanabenz can be used for researching hypertension and Parkinson disease .
|
-
- HY-B0379AR
-
|
|
nAChR
|
Neurological Disease
|
|
Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
|
-
- HY-B0219R
-
|
|
Xanthine Oxidase
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Allopurinol (Standard) is the analytical standard of Allopurinol. This product is intended for research and analytical applications. Allopurinol is a potent and orally active xanthine oxidase inhibitor with an IC50 value of 0.2-50 μM. Allopurinol can be used in the research of hyperuricemia and gout. Allopurinol decreases the expression of HIF-1α and HIF-2α protein. Allopurinol shows anti-depressant and anti-nociception activity. Anti-leishmanial effect .
|
-
- HY-106720
-
|
YM 09538
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
|
-
- HY-16560S
-
|
Campathecin-d5; (S)-(+)-Camptothecin-d5; CPT-d5
|
Isotope-Labeled Compounds
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
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 . 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 .
|
-
- HY-162639
-
|
|
Glycosidase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
|
α-Glucosidase-IN-68 (Compound 2) is an inhibitor for α-Glucosidase, AChE, and BChE, with IC50 of 0.251, 0.774 and 0.793 μM, respectively. α-Glucosidase-IN-68 exhibits antioxidant efficacy, with IC50 of 0.69 μM and 0.02 μM, in DPPH and ABTS experiments. α-Glucosidase-IN-68 exhibits antidiabetic effect in Streptozotocin (HY-13753)-induced diabetic rat models .
|
-
- HY-167950
-
|
|
PPAR
|
Metabolic Disease
|
|
PPARα/γ agonist 5 is a dual PPARα/γ agonist with significant biological activity exhibited at low concentrations. The EC50 of PPARα/γ agonist 5 are 0.358μM and 1.21μM respectively, showing its potential in inhibiting type 2 diabetes and lipid metabolism disorders. PPARα/γ agonist 5 was selected for clinical development due to its high efficacy .
|
-
- HY-106720A
-
|
YM 09538 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Amosulalol (YM 09538) hydrochloride is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol hydrochloride exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol hydrochloride decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
|
-
- HY-115463
-
EB-3D
2 Publications Verification
|
AMPK
Apoptosis
|
Cancer
|
|
EB-3D is a potent and selective choline kinase α (ChoKα) inhibitor, with an IC50 of 1 μM for ChoKα1. EB-3D exerts effects on ChoKα expression, AMPK activation, apoptosis, endoplasmic reticulum stress and lipid metabolism. EB-3D exhibits a potent antiproliferative activity in a panel of T-leukemia cell lines. Anti-cancer activity .
|
-
- HY-168869
-
|
|
PROTACs
Estrogen Receptor/ERR
|
Cancer
|
|
Tamoxifen-PEG-Clozapine is an estrogen receptor α (ERα) PROTAC degrader. Tamoxifen-PEG-Clozapine degrades ERα via a ubiquitin-proteasome system that uses the ubiquitin protein ligase E3 component N-recognin 5. Tamoxifen-PEG-Clozapine can be used for the research of cancer . (Pink: ERα inhibitor (HY-W271653); Black: linker (HY-168870); Blue: CRBN Ligand (HY-G0021))
|
-
- HY-147712
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-4 (compound 7l) is a potent and orally active aPKC inhibitor with an IC50 of 0.52 µM. PKC-IN-4 inhibits TNF-α induced NF-κB activity in vitro. PKC-IN-4 blocks VEGF- and TNFα-induced permeability across the retinal vasculature .
|
-
- HY-148413
-
|
ISIS 3521 sodium
|
PKC
|
Cancer
|
|
Aprinocarsen (ISIS 3521) sodium, a specific antisense oligonucleotide inhibitor of protein kinase C-alpha (PKC-α). Aprinocarsen sodium is a 20-mer oligonucleotide, it regulates cell differentiation and proliferation. Aprinocarsen sodium inhibits the growth of human tumor cell lines in nude mice. Aprinocarsen sodium shows the value as a chemotherapeutic compound of human cancers .
|
-
- HY-131089
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
MC-VC-PABC-C6-α-Amanitin is an antibody agent conjugate consisting of an anticancer toxin alpha-Amanitin (HY-19610) and a monoclonal antibody MC-VC-PABC-C6. Among them, alpha-Amanitin is a potent inhibitor of RNA polymerase IIα. MC-VC-PABC-C6-α-Amanitin accurately targets HER2 receptors, specifically recognizes HER2-positive tumor cells. It is widely used in breast cancer and gastric cancer research .
|
-
- HY-122144
-
|
Teroxirone
|
Endogenous Metabolite
|
Cancer
|
|
α-Triglycidyl isocyanurate (Teroxirone) is an antitumor compound with activity to inhibit DNA replication. α-Triglycidyl isocyanurate exerts its anticancer effect by alkylating and cross-linking DNA. α-Triglycidyl isocyanurate is relatively stable in fresh human plasma and whole blood, showing good biocompatibility. The metabolism of α-Triglycidyl isocyanurate mainly occurs in rat liver and is metabolized through an NADPH-independent pathway. The cytotoxicity of α-Triglycidyl isocyanurate can be partially restored under specific conditions, suggesting the complexity of its metabolic pathway .
|
-
- HY-147954
-
|
|
Carbonic Anhydrase
Cholinesterase (ChE)
|
Neurological Disease
Metabolic 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-118525
-
|
|
HCV
PI4K
|
Infection
|
|
AL-9 is a inhibitor of PI4KIIIα, with the IC50 of 0.57 μM, that can inhibit HCV replication .
|
-
- HY-W273493
-
|
2-(4-Nitrobenzylidene)acetophenone
|
Proteasome
|
Inflammation/Immunology
|
|
4-Nitrochalcone (2-(4-Nitrobenzylidene)acetophenone) inhibits the proteasome, inhibits NF-κB activity induced by TNFα .
|
-
- HY-13864
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PF-4989216 is a potent and selective PI3Kα inhibitor with a Ki of 0.6 nM.
|
-
- HY-P2949
-
|
|
Potassium Channel
|
Cancer
|
|
Pandinotoxin Kα, isolated from the venom of Pandinus imperator, is the inhibitor of A-type potassium channel .
|
-
- HY-168058
-
|
|
Glycosidase
|
|
|
WXC-25 is an inhibitor of α-glucosidase with an IC50 value of 2.02 μM .
|
-
- HY-U00266
-
-
- HY-147078
-
-
- HY-145580A
-
|
(S)-UCB0599; (S)-NPT200-11
|
α-synuclein
|
Neurological Disease
|
|
(S)-Minzasolmin is an isomer of minzasolmin (HY-145580), an inhibitor of α-synuclein oligomerization .
|
-
- HY-N1901
-
-
- HY-135385
-
-
- HY-101272
-
|
|
PI3K
|
Cancer
|
|
GDC-0326 is a potent and selective PI3Kα inhibitor with a Ki of 0.2 nM.
|
-
- HY-137611A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
α,β-MTDP trisodium, a thymidylate analog, is a thymidine kinase inhibitor with a Ki of 23 µM .
|
-
- HY-148318
-
|
|
Casein Kinase
|
Cancer
|
|
CK2α-IN-1 (compound 2) is a selective CK2α inhibitor (IC50=7.0 µM; Ki=1.6 µM) that exhibits a non-ATP-competitive mode of action. CK2α-IN-1 exhibits good potential for anticancer studies .
|
-
- HY-N0877R
-
|
|
Na+/K+ ATPase
|
Cancer
|
|
Bufalin (Standard) is the analytical standard of Bufalin. This product is intended for research and analytical applications. Bufalin is an active component isolated from Chan Su, acts as a potent Na+/K+-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively . Anti-cancer activity .
|
-
- HY-158037
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-55 (Compound 8g) is an orally active and competitive alpha-glucosidase inhibitor, with IC50 and Ki values of 12.1 and 9.66 µM, respectively. α-Glucosidase-IN-55 can be used for the research into type 2 diabetes mellitus (T2DM) to improve blood sugar control and metabolic health .
|
-
- HY-116704
-
-
- HY-113209A
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Ent-8-Iso-15(S)-prostaglandin F2α is an isomer of 8-Isoprostaglandin F2α, with a better inhibiting activity in the whole blood platelet aggregation inhibition assay .
|
-
- HY-143224B
-
|
|
CD47
|
Cancer
|
|
NCGC00138783 TFA is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 μM. NCGC00138783 TFA directly blocks the interaction between CD47 and SIRPα axis .
|
-
- HY-15761
-
|
|
GSK-3
|
Neurological Disease
|
|
AZD2858 is a potent, orally active GSK-3 inhibitor, with IC50s of 0.9 and 5 nM for GSK-3α and GSK-3β, respectively, used in the research of fracture healing.
|
-
- HY-161751
-
|
|
GSK-3
|
Cancer
|
|
MJ34 is a potent inhibitor of GSK-3β and GSK-3α, with the IC50s of 15.4 nM and 31.5 nM, respectively. MJ34 plays an important role in cancer research
|
-
- HY-126683
-
|
|
Drug-Linker Conjugates for ADC
|
Cancer
|
|
Mal-C6-α-Amanitin is a agent-linker conjugate for ADC with potent antitumor activity by using α-Amanitin (an RNA polymerase II inhibitor), linked via the ADC linker Mal-C6.
|
-
- HY-120358
-
-
- HY-P99782
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Opinercept is a recombinant fusion protein comprising an TNFRSF1B fused to a human IgG1 Fc . Opinercept is a tumor necrosis factor-alpha (TNF-alpha) inhibitor. Opinercept can be used for the research of rheumatoid arthritis (RA) .
|
-
- HY-116301
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
CAY10502 is a potent, calcium-dependent cytosolic phospholipase A2 α (cPLA2α) inhibitor with an IC50 of 4.3 nM for isolated enzyme. CAY10502 can be used in the research of retinopathy and inflammatory diseases .
|
-
- HY-U00237B
-
|
|
Adrenergic Receptor
|
Others
|
|
L-771688 hydrochloride is a potent and highly selective α1A-adrenoceptor antagonist (Kd=43-90 pM). L-771688 hydrochloride is effective against cloned human, rat and dog α1A-adrenergic receptors. L-771688 exhibits high affinity (Ki ≤ 1 nM) and over 500-fold selectivity over the α1B and α1D isoforms. L-771688 potently antagonizes norepinephrine-induced responses at these receptors. Inhibits contractions induced by phenylephrine or A-61603 in rat, dog, human and monkey models .
|
-
- HY-N0492R
-
|
Thioctic acid (Standard); (±)-α-Lipoic acid (Standard); DL-α-Lipoic acid (Standard)
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
α-Lipoic Acid (Standard) is the analytical standard of α-Lipoic Acid. This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
|
-
- HY-B0532
-
|
|
Dopamine Receptor
Adrenergic Receptor
P-glycoprotein
CaMK
Influenza Virus
Autophagy
|
Neurological Disease
|
|
Trifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent α1-adrenergic receptor antagonist. Trifluoperazine is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis .
|
-
- HY-B0532A
-
|
|
Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
|
Neurological Disease
Cancer
|
|
Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .
|
-
- HY-145835
-
|
|
PERK
|
Cancer
|
|
PERK-IN-5 is a highly potent, selectively and orally bioavailable PERK inhibitor (IC50s of 2 and 9 nM for PERK and p-eIF2α, respectively). PERK-IN-5 can significantly inhibit tumor growth in the 786-O renal cell carcinoma xenograft tumor model .
|
-
- HY-18259
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
103D5R (Compound 15) is an inhibitor for the activation of hypoxia-inducible factor-1 (HIF-1) with an IC50 of 35 µM, through reduction of the HIF-1α protein synthesis. 103D5R inhibits the proliferation of LN229 with IC50 of 26 µM .
|
-
- HY-116626
-
|
|
NF-κB
p38 MAPK
MMP
|
Cancer
|
|
SM-7368 is a potent NF-kB inhibitor that targets downstream of MAPK p38 activation . SM-7368 inhibits TNF-α-induced MMP-9 upregulation. SM-7368 can be used for the research of chemotherapies targeting TNF-α-mediated tumor invasion and metastasis .
|
-
- HY-18759
-
|
|
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
|
BMS-751324 is a p38α MAPK inhibitor. BMS-751324 equips a precursor of carbamyl-methyl linkage, containing esters and phosphate functional groups derived from hydroxyphenylacetic acid (HPA). BMS-751324 effectively inhibits foot swelling and LPS-induced TNFα production in an arthritic rat model .
|
-
- HY-W014049
-
|
|
NO Synthase
|
Others
|
|
N'-Nitro-D-arginine, a nitric oxide synthesis inhibitor, also is a vasodilator that relaxes the smooth muscles and increases blood flow to the penis, improving erections. N'-Nitro-D-arginine also inhibits neutrophil migration by blocking receptors for tumour necrosis factor alpha (TNFα) and interleukin 8 (IL8) .
|
-
- HY-171290
-
|
|
Casein Kinase
p38 MAPK
|
Inflammation/Immunology
|
|
Casein kinase 1δ-IN-31 (Compound 16) is the inhibitor for casein kinase (CK) that inhibits CK1α, CK1δ, and p38α with IC50s of 196, 17, and 18 nM, respectively. Casein kinase 1δ-IN-31 inhibits Double Homeobox 4 (DUX4) with IC50 of 1200 nM .
|
-
- HY-106129
-
|
LY 320236
|
5 alpha Reductase
|
Endocrinology
Cancer
|
|
Izonsteride (Compound LY320236) is an inhibitor of 5α-reductase (IC50 = 11.6 nM for type I; 7.37 nM for type II). LY320236 inhibits the activity of steroid 5α-reductase, preventing the conversion of testosterone (T) to dihydrotestosterone (DHT). LY320236 can significantly inhibit the growth of LNCaP tumors in thymic mice without exhibiting obvious host toxicity .
|
-
- HY-P10437
-
|
human α1-AT(353-372)
|
HIV
|
Infection
|
|
VIRIP (human α1-AT(353-372)) is a HIV-1 inhibitor. VIRIP blocks the entry of HIV-1 by interacting with gp41 fusion peptide. VIRIP can be used for virus research .
|
-
- HY-N4121
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
Isocurcumenol, an estrogen receptor alpha (ERα) inhibitor isolated from Curcuma zedoaria Rhizomes, possesses anti-tumor acticity, with IC50 values of 99.1μg/mL and 178.2 μg/mL in DLA and KB cells, respectively .
|
-
- HY-15483
-
DY131
3 Publications Verification
GSK 9089
|
Estrogen Receptor/ERR
Smo
|
Endocrinology
Cancer
|
|
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ . DY131 also inhibits Smo signaling .
|
-
- HY-B0532S
-
-
- HY-143269
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
HPA-IN-2 (Compound 2a-1) is a potent and selective human pancreatic α-amylase (HPA) inhibitor with IC50 values of 8.2 μM and 450.7 μM against HPA and α-glucosidase, respectively .
|
-
- HY-B0392
-
-
- HY-P1793A
-
|
|
Opioid Receptor
Biochemical Assay Reagents
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
α-Casein (90-95) TFA is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) TFA inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) TFA inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) TFA activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) TFA can be used in the study of the mechanisms of allergic diseases and prostate cancer .
|
-
- HY-P1793
-
|
|
Opioid Receptor
Biochemical Assay Reagents
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
α-Casein (90-95) is a partial agonist of opioid receptors and a copper ion ligand, with opioid activity. α-Casein (90-95) inhibits the secretion of β-hexosaminidase by rat peritoneal mast cells (PMC) with IC50= 0.1 μM. α-Casein (90-95) inhibits the proliferation of prostate cancer cells LNCaP, DU145, and PC3 with IC50 of 0.94 nM, 137 nM, and 6.92 nM, respectively. α-Casein (90-95) activates Gi-like proteins through a membrane-assisted, receptor-independent pathway, or reversibly binds to opioid receptors, inducing intracellular calcium release and conformational changes, and exerts the activity of promoting mast cell secretion and inhibiting tumor cell proliferation. α-Casein (90-95) can be used in the study of the mechanisms of allergic diseases and prostate cancer .
|
-
- HY-136474
-
|
(±)-Amidephrine
|
Adrenergic Receptor
|
Endocrinology
|
|
Amidephrine is a selective agonist of alpha 1-adrenoceptor. Amidephrine inhibits inhibits monopulse field contraction of the vas deferens epithelium and prostate gland .
|
-
- HY-12398
-
|
|
VD/VDR
|
Metabolic Disease
Inflammation/Immunology
|
|
TEI-9647, a Vitamin D3 Lactone analogue, is a potent and specific vitamin D receptor (VDR) antagonist. TEI-9647 inhibits VDR/VDRE-mediated genomic actions of 1α,25(OH)2D3. TEI-9647 inhibits bone resorption and HL-60 cell differentiation induced by of 1α,25(OH)2D3. TEI-9647 has the potential for suppressing the excessive bone resorption and osteoclast formation in Paget's disease .
|
-
- HY-108645
-
|
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
AL 8697 is a specific and orally active p38α MAPK inhibitor with an IC50 of 6 nM. AL 8697 displays 14-fold greater inhibition of p38α compared to p38β (IC50=82 nM), and 300-fold selectivity for p38α over a panel of 91 kinases. Anti-inflammatory activity .
|
-
- HY-149086
-
|
|
RAR/RXR
Apoptosis
PARP
Bcl-2 Family
|
Cancer
|
|
BPA-B9 is a RXRα ligand and antagonist targeting the pRXRα-PLK1 interaction. BPA-B9 has excellent RXRα-binding affinity (KD=39.29 ± 1.12 nM). BPA-B9 inhibits the proliferation of cancer cells by inducing mitotic arrest and cell apoptosis .
|
-
- HY-W114419
-
-
- HY-U00458
-
K-80003
1 Publications Verification
TX-803
|
Akt
|
Cancer
|
|
K-80003 is a potent inhibitor of tRXRα-dependent Akt activation and cancer cell growth.
|
-
- HY-100337
-
WWL70
2 Publications Verification
|
MAGL
|
Neurological Disease
|
|
WWL70 is a selective alpha/beta hydrolase domain 6 (ABHD6) inhibitor with an IC50 of 70 nM.
|
-
- HY-19920
-
-
- HY-116034
-
-
- HY-16937
-
|
|
PI4P5K
|
Cancer
|
|
ISA-2011B is a PIP5K1α inhibitor with promising anticancer effects .
|
-
- HY-N13020
-
|
|
Others
|
Others
|
|
Scleropentaside D is a potent α-glycosidase inhibitor. Scleropentaside D has antioxidant activity .
|
-
- HY-173488
-
|
|
NF-κB
HIF/HIF Prolyl-Hydroxylase
Keap1-Nrf2
|
Cancer
|
|
NF-κB/HIF-1α-IN-1 (compound 9c) is a potent blocker of the NF-κB activation pathway and demonstrates selective anti-fibrotic activity. NF-κB/HIF-1α-IN-1 shows no significant cytotoxicity in NCI tumor cell lines. In rat models. NF-κB/HIF-1α-IN-1 has been shown to effectively ameliorate liver fibrosis by inhibiting the expression levels of NF-κB and HIF-1α, while simultaneously inducing the activation of Nrf2 .
|
-
- HY-150618
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-9 (compound 27) is a selective, long-acting and oral active PI3Kα inhibitor with IC50 values of 4.4, 128, 146 and 153 nM for PI3Kα, PI3Kγ, PI3Kδ and PI3Kβ, respectively. PI3Kα-IN-9 has antiproliferative activity and induces apoptosis. PI3Kα-IN-9 can be used for cancer research .
|
-
- HY-148908
-
|
|
TNF Receptor
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
TNF-α-IN-8 (compound I-42) is a TNF-α inhibitor. TNF-α-IN-8 is an isoindole-imide compound. TNF-α-IN-8 can be used for the research of cancer, heart disease, osteoporosis, inflammatory, allergic and autoimmune diseases . TNF-α-IN-8 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
|
-
- HY-163712
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
17-Epiestriol is an estrogen metabolite and a selective estrogen receptor (ER) β agonist. 17-epiestriol inhibits the mRNA and protein expression of the vascular cell adhesion molecule VCAM-1 induced by tumor necrosis factor α (TNFα). 17-epiestriol also inhibits TNFα-induced VCAM-1 expression and prevents NF-κB migration to the nucleus. 17-Epiestriol also induces the mRNA and protein expression of endothelial nitric oxide synthase .
|
-
- HY-U00460
-
|
|
IRE1
|
Cancer
|
|
3,6-DMAD hydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD hydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD hydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD hydrochloride can be used for research of cancer .
|
-
- HY-U00460B
-
|
|
IRE1
|
Cancer
|
|
3,6-DMAD dihydrochloride, an acridine derivative, is a potent IRE1α-XBP1s pathway inhibitor. 3,6-DMAD dihydrochloride promotes IL-6 secretion via the IRE1α-XBP1s pathway. 3,6-DMAD dihydrochloride inhibits IRE1α oligomerization and endoribonuclease (RNase) activity. 3,6-DMAD dihydrochloride can be used for research of cancer .
|
-
- HY-145452
-
|
5-Octyl 2-oxopentanedioate
|
E1/E2/E3 Enzyme
Histone Methyltransferase
|
Cancer
|
|
5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation .
|
-
- HY-N0492AR
-
|
Thioctic acid sodium (Standard); (±)-α-Lipoic acid sodium (Standard); DL-α-Lipoic acid sodium (Standard)
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
α-Lipoic Acid (sodium) (Standard) is the analytical standard of α-Lipoic Acid (sodium). This product is intended for research and analytical applications. α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation[1][2][3]. α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells[4]. α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1[5].
|
-
- HY-19279A
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
JTH-601 Free base is a novel alpha1-adrenoceptor antagonist that exhibits potent activity in inhibiting phenylephrine-induced contractions in lower urinary tract tissues. JTH-601 Free base competitively antagonizes alpha1-adrenoceptor-mediated contractile responses, demonstrating greater potency than prazosin or tamsulosin. JTH-601 Free base is anticipated to be effective in treating urinary outlet obstruction associated with benign prostatic hyperplasia.
|
-
- HY-16560R
-
|
Campathecin (Standard); (S)-(+)-Camptothecin (Standard); CPT (Standard)
|
Topoisomerase
ADC Cytotoxin
MicroRNA
Influenza Virus
Apoptosis
Fungal
Antibiotic
|
Infection
Cancer
|
|
Camptothecin (Standard) (Campathecin (Standard)) is the analytical standard of Camptothecin (HY-16560). This product is intended for research and analytical applications. Camptothecin (CPT), a kind of alkaloid, is a DNA topoisomerase I (Topo I) inhibitor with an IC50 of 679 nM. 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.
|
-
- HY-N8884
-
|
|
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-P5960
-
|
PTBP1 α3-helix derived peptide P6 TFA
|
DNA/RNA Synthesis
|
Others
|
|
PTBP1-RNA-binding inhibitor P6 (PTBP1 α3-helix derived peptide P6) TFA is a stapled peptide inhibitor of the splicing factor PTBP1, which inhibits alternative splicing events regulated by PTBP1. PTBP1 binds RNA through its RNA recognition motif .
|
-
- HY-13453
-
|
BAY 11-7821
|
IKK
Deubiquitinase
Autophagy
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
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-143224A
-
|
|
CD47
|
Cancer
|
|
NCGC00138783 free base is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 µM. NCGC00138783 free base directly blocks the interaction between CD47 and SIRPα axis .
|
-
- HY-164361
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
α-Gracinoic acid is a Chalcone (HY-121054) derivative with anti-inflammatory activity. α-Gracinoic acid inhibits nitric oxide production catalyzed by inducible nitric oxide synthase (iNOS) in lipopolysaccharide (LPS)-treated RAW 264.7 cells .
|
-
- HY-163739
-
|
|
α-synuclein
|
Neurological Disease
|
|
LETC is an orally active α-synuclein (α-Syn) aggregation inhibitor with an EC50 of 66 nM in transfected DH60.21 neuroblastoma cells. LETC can cross the blood-brain barrier. LETC can be used for the study of synucleinopathies .
|
-
- HY-115983
-
|
|
CD47
Apoptosis
|
Cancer
|
|
DMUP is a potent CD47-SIRPα axis inhibitor. DMUP induces apoptosis and increases the macrophage phagocytosis in A549 cells. DMUP decreases the expression of CD47 and SIRPα protein. DMUP shows antitumor activity .
|
-
- HY-128677
-
|
|
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-W112651
-
|
|
Glycosidase
Amylases
|
Metabolic Disease
|
|
2,4,6-Triphenylaniline has anti-diabetic activity and can be encapsulated in nano-emulsions (NE) to enhance stability and permeability. The NE loaded with 2,4,6-Triphenylaniline inhibits α-glucosidase and α-amylase .
|
-
- HY-138688
-
|
CDC
|
Lipoxygenase
|
Metabolic Disease
Cancer
|
|
Cinnamyl-3,4-dihydroxy-α-cyanocinnamate (CDC) is a potent 12/15-Lipoxygenases (LO) inhibitor. Cinnamyl-3,4-dihydroxy-α-cyanocinnamate has the potential for the research of type 1 diabetes mellitus .
|
-
- HY-155943
-
|
|
AMPK
|
Cancer
|
|
AMPK-IN-4 (compound 19) is a potent inhibitor of (AMPK(α1) and AMPK(α2) with IC50s of 393 nM and 141 nM, respectively. AMPK-IN-4 plays an important role in cancer research .
|
-
- HY-152089
-
-
- HY-107674
-
|
|
nAChR
|
Neurological Disease
|
|
bPiDDB is a potent nAChR antagonist. bPiDDB potently (IC50=2 nM) inhibits nicotine-evoked striatal dopamine (DA) release through an interaction with α6β2-containing nAChRs .
|
-
- HY-122058A
-
|
|
CXCR
HIV
|
Infection
Inflammation/Immunology
|
|
KRH-3955 hydrochloride is an orally bioavailable CXCR4 antagonist. KRH-3955 hydrochloride inhibits SDF-1α binding to CXCR4 with an IC50 of 0.61 nM. KRH-3955 hydrochloride is also a highly potent and selective inhibitor of X4 HIV-1, with an EC50 of 0.3 to 1.0 nM .
|
-
- HY-170879
-
|
|
p38 MAPK
JNK
|
Cancer
|
|
JD123 inhibits JNK1 activity and the expression of cJun (1-135). JD123 is a ATP-competitive p38-γ MAPK inhibitor, but not effect to ERK1, ERK2, or p38-α, p38-β or p38-δ. .
|
-
- HY-135902
-
|
NSC 377363
|
DNA/RNA Synthesis
|
Neurological Disease
|
|
Synucleozid (NSC 377363) is a potent inhibitor of the SNCA mRNA that encodes α-synuclein protein. Synucleozid selectively targets the α-synuclein mRNA 5′ UTR at the designed IRE site, decreases the amount of SNCA mRNA loaded into polysomes and thereby inhibits SNCA translation. Synucleozid has the potential for the investigation of Parkinson’s disease .
|
-
- HY-117798
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
LY 806303 is a potent and selective inhibitor of human α-thrombin. LY 806303 specifically acylates Ser-205 within the catalytic triad of α-thrombin on the heavy chain and a key site involved in the enzymatic activity of thrombin. The mechanism of action of LY 806303 as an enzyme inhibitor is through the specific acylation of this catalytic serine residue .
|
-
- HY-N12761
-
|
|
Phosphatase
Glycosidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Penpaxilloids A (Compound 1) is a non-competitive inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 8.60 μM. Penpaxilloids A can be isolated from the fungus Penicillium sp. ZYX-Z-143. Penpaxilloids A is also an α-glucosidase (α-glucosidase) inhibitor with anti-inflammatory activity .
|
-
- HY-107669
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR-IN-1 (hydrochloride) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-170541
-
|
|
Glucosylceramide Synthase (GCS)
|
Inflammation/Immunology
|
|
FUT8-IN-1 (Compound 37) is an inhibitor for α-1,6-fucosyltransferase (FUT8) with an KD of 49 nM and an IC50 of ca. 50 µM. FUT8-IN-1 generates a highly active naphthoquinone imine intermediate in the presence of FUT8, and inhibits the enzymatic activity of FUT8 .
|
-
- HY-19144
-
|
|
5 alpha Reductase
|
Others
|
|
ONO-3805 is an early lead compound of a non-steroidal 5α-reductase inhibitor, used to inhibit the conversion of testosterone to dihydrotestosterone, with potential effects in inhibiting benign prostatic hyperplasia.
|
-
- HY-150739A
-
-
- HY-13635A
-
|
MK-906 acetate
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (MK-906) acetate is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride acetate has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride acetate can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-161373
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
|
-
- HY-N0596
-
|
20(R)-Panaxadiol
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .
|
-
- HY-133807B
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
(R)-Benpyrine is the isomer of Benpyrine (HY-133807), and can be used as an experimental control. Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 μM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research .
|
-
- HY-155105
-
|
|
Glycosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-30 (compound 8c) is a potent, orally active, competitive inhibitor against α-glucosidase, with Ki of 40.0 µM and IC50 value of 49.0 µM. α-Glucosidase-IN-30 is non-cytotoxic against the cancer and normal cell lines MCF-7 and HDF, and can be used for Type 2 diabetes study .
|
-
- HY-122016A
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
BRD-4592 is an allosteric inhibitor targeting Mycobacterium tuberculosis tryptophan synthase (TrpAB). BRD-4592 binds at the α-β-subunit interface of TrpAB, with an IC50 of 70.9 nM for the α-subunit and 22.6 nM for the β-subunit .
|
-
- HY-108346
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
JX401 is a potent inhibitor of p38alpha, containing a 4-benzylpiperidine motif. p38alpha is hyperactive in inflammatory diseases, and various indications suggest that its inhibition would reverse inflammation. JX401 has the potential for the research of inflammation .
|
-
- HY-111055
-
|
|
GSK-3
|
Neurological Disease
|
|
BIP-135 is a potent and selective ATP-competitive GSK-3 inhibitor, with IC50s of 16 nM and 21 nM for GSK-3α and GSK-3β, respectively. BIP 135 exhibits neuroprotective effect .
|
-
- HY-118091B
-
|
|
5 alpha Reductase
|
Others
|
|
LY300503 is an enantiomer of LY191704. LY191704 is a human type I 5α-reductase inhibitor .
|
-
- HY-N3101
-
-
- HY-101068
-
-
- HY-116643
-
-
- HY-117721
-
-
- HY-N8251
-
-
- HY-N12790
-
|
Ananonin B
|
Glycosidase
|
Metabolic Disease
|
|
Arisanschinin D (Ananonin B) is an α-Glucosidase inhibitor and can be isolated from Schisandra arisanensis Hay .
|
-
- HY-136347
-
-
- HY-W014589
-
|
2,4-DTBP
|
Endogenous Metabolite
Fungal
Apoptosis
RAR/RXR
Amyloid-β
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of drugs and fragrances .
|
-
- HY-163679
-
|
|
Estrogen Receptor/ERR
Cytochrome P450
PROTACs
Apoptosis
|
Cancer
|
|
PROTAC ERα Degrader-9 (Compound 18c) is a dual-targeting PROTAC degrader, which degrades estrogen receptor α (ERα) and aromatase (ARO). PROTAC ERα Degrader-9 binds to ERα with a Ki of 0.25 μM, inhibits ARO with an IC50 of 4.6 μM. PROTAC ERα Degrader-9 inhibits the proliferation of MCF-7 wildtype (IC50=0.54 μM) and ERα mutants MCF-7 EGFR (IC50=0.075 μM), MCF-7 D538G (IC50=0.31 μM), MCF-7 Y537S (IC50=2.3 μM), downregulates the expressions of ERS1 and MYC. PROTAC ERα Degrader-9 arrests the cell cycle at G2/M, induces apoptosis in MCF-7. PROTAC ERα Degrader-9 exhibits antitumor efficacy in mouse models. (Pink: ligand for target protein (HY-163680); Black: linker (HY-W007559); Blue: ligand for E3 ligase (HY-112078))
|
-
- HY-158029
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-21 (compound 8) is a PI3Kα inhibitor, and its selectivity for PI3Kα is 10.41/16.99/37.53 times higher than PI3Kβ/γ/δ respectively (IC50: 96.89/568.24/397.48 nM ). PI3Kα-IN-21 inhibits cancer cell activity, proliferation, and migration, and induces mitochondrial apoptosis through the PI3K/Akt/mTOR pathway. PI3Kα-IN-21 exhibits in vivo antitumor potency in a mouse model of non-small cell lung cancer .
|
-
- HY-114454
-
INH14
4 Publications Verification
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IKK
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Inflammation/Immunology
Cancer
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INH14 is a cell permeable inhibitor of IKKα/IKKβ, with IC50s of 8.97 and 3.59 μM, respectively. INH14 inhibits the IKKα/β-dependent TLR inflammatory response. INH14 also inhibits downstream of TAK1/TAB1 and NF-kB pathways. Anti-inflammatory and anti-cancer activity .
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- HY-171277
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Casein Kinase
p38 MAPK
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Cancer
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Casein kinase 1δ-IN-27 (Compound 8) is the inhibitor for casein kinase 1 that inhibits CK1α, CK1δ, CK1ε, and p38α with IC50s of 22, 16.5, 9.41 and 14.8 nM, respectively. Casein kinase 1δ-IN-27 inhibits the DUX4 expression with an IC50 of 10 nM .
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- HY-15486
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Phosphatase
HSV
Autophagy
Apoptosis
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Infection
Inflammation/Immunology
Cancer
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Salubrinal is a cell-permeable and selective inhibitor of eIF2α dephosphorylation . Salubrinal acts as a dual-specificity phosphatase 2 (Dusp2) inhibitor and suppresses inflammation in anti-collagen antibody-induced arthritis . Salubrinal has antiviral activity against HSV-1 and inhibits dephosphorylation of eIF2α mediated by the HSV-1 protein ICP34.5 .
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- HY-117822
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GSK-3
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Neurological Disease
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BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
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- HY-P1259
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Proteasome
Bacterial
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Inflammation/Immunology
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PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
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- HY-19931
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COH29
4 Publications Verification
RNR Inhibitor COH29
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DNA/RNA Synthesis
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Cancer
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COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
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- HY-135902A
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NSC 377363 hydrochloride
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DNA/RNA Synthesis
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Neurological Disease
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Synucleozid hydrochloride (NSC 377363 hydrochloride) is a potent inhibitor of the?SNCA?mRNA?that encodes α-synuclein protein. Synucleozid selectively?targets the?α-synuclein?mRNA 5′ UTR at the designed IRE site, decreases the amount of?SNCA?mRNA loaded into polysomes and thereby inhibits?SNCA?translation. Synucleozid has the potential for the investigation of Parkinson’s disease .
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- HY-19731
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MiR-544 Inhibitor 1
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MicroRNA
Apoptosis
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Cancer
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SID 3712249 (MiR-544 Inhibitor 1) is a miR-544 biogenesis inhibitor. SID 3712249 binds directly to the precursor miRNA. SID 3712249 blocks production of the mature microRNA and decreases miR-544, HIF-1α, and ATM transcripts. SID 3712249 can be used in the research of cancers, such as breast cancer .
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- HY-101961
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AG 1288
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c-Kit
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Inflammation/Immunology
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Tyrphostin AG 1288 is a potent Tyrosine Kinase inhibitor. Tyrphostin AG 1288 inhibits ICAM1 expression and TNFα-mediated cytotoxicity in vitro .
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- HY-131504A
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Glycosidase
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Metabolic Disease
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Valienamine is the alpha-glucosidase inhibitor. Valienamine is the key functional component of many natural glycosidase inhibitors including the crop protectant validamycin A and the antidiabetic agent acarbose .
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- HY-13229
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Caspase
Apoptosis
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Cancer
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Boc-D-FMK is a cell-permeable, irreversible and broad spectrum caspase inhibitor. Boc-D-FMK inhibits apoptosis stimulated by TNF-α with an IC50 of 39 μM.
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- HY-P9926
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REGN-668; SAR-231893
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Interleukin Related
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Inflammation/Immunology
Cancer
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Dupilumab (REGN-668) is a fully human mAb to IL-4 receptor α (IL-4Rα) that inhibits both IL-4 and IL-13 signaling, markedly improved moderate-to-severe atopic dermatitis .
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- HY-112658
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Adrenergic Receptor
Adenosine Receptor
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Endocrinology
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p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM .
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- HY-145425
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IRE1
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Cancer
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PAIR2 is a potent and selective partial antagonist of IRE1α RNase. PAIR2 can completely occupy IRE1α’s ATP-binding site in cells and block the ability of a potent KIRA to inhibit XBP1 splicing .
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- HY-19383
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PTP 112
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Phosphatase
IKK
PPAR
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Metabolic Disease
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Ertiprotafib is an inhibitor of PTP1B, IkB kinase β (IKK-β), and a dual PPARα and PPARβ agonist, with an IC50 of 1.6 μM for PTP1B, 400 nM for IKK-β, an EC50 of ~1 μM for PPARα/PPARβ.
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- HY-114568
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- HY-159928
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- HY-P2601A
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CGRP Receptor
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Others
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Tyr-α-CGRP (human) TFA is an N-terminally extended human α-CGRP analog. Tyr-α-CGRP (human) TFA can bind to membrane preparations from rat brain and spleen with IC50 values of 0.2 nM and 0.5 nM, respectively, and induce positive chronotropic and inotropic effects in isolated guinea pig right and left atria with EC50 values of 282 nM and 74 nM, respectively. Tyr-α-CGRP (human) TFA also inhibits contractile responses in rat vas deferens with an EC50 value of 1.9 nM .
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- HY-B0135R
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NKCC
GABA Receptor
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Metabolic Disease
Cancer
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Furosemide (Standard) is the analytical standard of Furosemide. This product is intended for research and analytical applications. Furosemide is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
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- HY-149483
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nAChR
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Neurological Disease
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CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
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- HY-155113
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PROTACs
HSP
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Cancer
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PROTAC Hsp90α degrader 1 (Compound X10g) is a selective PROTAC Hsp90α degrader. PROTAC Hsp90α degrader 1 can be used for breast cancer research. PROTAC Hsp90α degrader 1 inhibits the proliferation of MDA-MB-231, MDA-MB-468, MCF-7, MX-1 cells with IC50s of 51.48 μM, 16.46 μM, 8.93 μM, 11.95 μM respectively .
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- HY-151453
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Topoisomerase
Apoptosis
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Cancer
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Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC50 value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer .
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- HY-156816
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Casein Kinase
DYRK
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Cancer
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ON 108600 is a inhibitor for CK2 (Casein Kinase2)/TNIK/DYRK1 , with the IC50s for DYRK1A/DYRKB, DYRK2, CK2α1/CK2α2, and TNIK of 0.016 μm/0.007 μM, 0.028 μM, 0.05 μM/0.005 μM, and 0.005 μM, respectively. ON 108600 has antitumor activity .
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- HY-P10404
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α-synuclein
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Others
Neurological Disease
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PDpep1.3 is a peptide inhibitor of α-synuclein that disrupts the direct interaction between α-synuclein and CHarged Multivesicular body Protein 2B (CHMP2B). As a result, PDpep1.3 restores the degradation function of endosomes and lysosomes, reduces the protein level and aggregation of α-synuclei, and protects dopaminergic neurons from α-synuclei-mediated degeneration. PDpep1.3 can be used to study neurodegenerative diseases and protein-protein interactions .
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- HY-A0009
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Galantamine hydrobromide
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Cholinesterase (ChE)
nAChR
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Neurological Disease
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Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
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- HY-128463
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COX
Reactive Oxygen Species
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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N-tert-Butyl-α-phenylnitrone is a nitrone-based free radical scavenger that forms nitroxide spin adducts. N-tert-Butyl-α-phenylnitrone inhibits COX2 catalytic activity. N-tert-Butyl-α-phenylnitrone has potent ROS scavenging, anti-inflammatory, neuroprotective, anti-aging and anti-diabetic activities, and can penetrate the blood-brain barrier .
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- HY-145904
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PDGFR
FLT3
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Cancer
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PDGFRα/FLT3-ITD-IN-3 (Compound 18d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of 0.153 and 0.004 μM, respectively. PDGFRα/FLT3-ITD-IN-3 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
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- HY-149085A
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RAR/RXR
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Cancer
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(E)-XS-060 is an isomer of XS-060. XS-060 is a RXRα antagonist. XS-060 inhibits pRXRα-PLK1 interaction. XS-060 induces RXRα-dependent mitotic arrest. XS-060 exhibits good antitumor activity against breast cancer, lung adenocarcinoma, and liver cancer .
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- HY-N11499
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Bacterial
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Infection
Inflammation/Immunology
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Myricetin 3-O-α-L-arabinopyranoside is a quercetin derivative and plant flavonoid with antioxidant, antibacterial and antiurease effects. Myricetin 3-O-α-L-arabinopyranoside inhibits A2E photooxidation-induced RPE cell death. Myricetin 3-O-α-L-arabinopyranoside is protective against retinal degeneration and protects against blue light (BL)-induced damage in RPE cells and mouse models .
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- HY-13635
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MK-906
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5 alpha Reductase
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Cancer
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Finasteride (MK-906) is an orally active and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
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- HY-145903
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PDGFR
FLT3
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Cancer
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PDGFRα/FLT3-ITD-IN-2 (Compound 13d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 20 and 1.654 μM, respectively. PDGFRα/FLT3-ITD-IN-2 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
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- HY-B0532AS
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Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
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Neurological Disease
Cancer
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Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .
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- HY-162601
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Histone Methyltransferase
HIF/HIF Prolyl-Hydroxylase
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Cancer
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D-01 is a dual-targeting inhibitor of HIF-1α and EZH2 (IC50: 4.86 μM and 0.99 μM respectively). D-01 inhibits the expression of H3K27me3 protein. D-01 inhibits the migration, clone and the invasion of A549 cells, and also inhibits tube formation of HUVECs. D-01 can be used for research of lung cancer .
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- HY-B0532B
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Dopamine Receptor
Adrenergic Receptor
P-glycoprotein
CaMK
Influenza Virus
Autophagy
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Infection
Neurological Disease
Cancer
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Trifluoperazine dimaleate, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dimaleate is a potent α1-adrenergic receptor antagonist. Trifluoperazine dimaleate is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dimaleate is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dimaleate can be used for the research of schizophrenia. Trifluoperazine dimaleate acts as a reversible inhibitor of influenza virus morphogenesis .
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- HY-117869
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- HY-142958
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- HY-101041
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(E)-Tyrphostin AG 556
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EGFR
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Inflammation/Immunology
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(E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production .
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- HY-106951
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L-733692
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5 alpha Reductase
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Cancer
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MK 386 (L-733692) is a selective 5-α-reductase I inhibitor, used for prostate cancer inhibition .
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- HY-134960
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- HY-U00206
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- HY-P10813
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- HY-117771A
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DAGL
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Metabolic Disease
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DO34 analog is a triazole DAGL(α) inhibitor extracted from patent WO2017096315 A1, compound 100.
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- HY-112910
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HSP
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Inflammation/Immunology
Cancer
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Grp94 Inhibitor-1 is a potent, selective Grp94 inhibitor with an IC50 value of 2 nM, and over 1000-fold selectivity to Grp94 against Hsp90α .
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- HY-169255
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- HY-143279
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Topoisomerase
Apoptosis
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Cancer
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Topoisomerase II inhibitor 3 (Compound 6 h ) is a acridone derivatives, as well as a Type II DNA topoisomerase (topo II) inhibitor , as a topo IIα/β inhibitor with the value of IC50 is 0.17 μM for topo IIα and the value of IC50 is 0.23 μM for topo IIβ subtypes, caused obvious DNA damage, and induced apoptosis by triggering the loss of mitochondrial membrane potential .
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- HY-P1259A
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Proteasome
Bacterial
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Inflammation/Immunology
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PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
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- HY-15544
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CCR
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Inflammation/Immunology
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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 .
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- HY-151382
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Casein Kinase
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Cancer
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CK2-IN-3 is a selective and potent CK2 inhibitor (Kd: 12 nM), with IC50 values of 1.51 μM (CK2α) and 7.64 μM (CK2α’). CK2-IN-3 can be used in the research of cancers .
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- HY-B0661AS1
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- HY-100947
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- HY-168759
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Progesterone Receptor
Drug Derivative
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Metabolic Disease
Cancer
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11α-Hydroxytestosterone is a deriviative of Hydrocortisone (HY-N0583), with the relative binding affinity to progesterone receptor of 9% (comparing to R5020 (HY-119384) 100%). 11α-Hydroxytestosterone inhibits the growth and differentiation of human decidual cells in culture .
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- HY-B0661AS
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- HY-12407
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VD/VDR
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Metabolic Disease
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ZK168281 is a 25-carboxylic ester 1α,25(OH)2D3 analog and a pure VDR antagonist with a Kd value of 0.1 nM. ZK168281 is an effective inhibitor of the coactivator (CoA) interaction of its receptor .
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- HY-137309
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HIV
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Others
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4-Deoxy-4α-phorbol is a tetracyclic diterpene found in E. desmondi. It has been used in the semisynthesis of inhibitors of the HIV-1-induced cytopathic effect on MT-4 cells and 4α-phorbol esters .
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- HY-108162A
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- HY-N14907
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Glycosidase
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Infection
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Panosialin wA can inhibit α,β-glucosidase and mannose glycosidase. Panosialin wA does not inhibit the influenza virus, but it has weak anti-microbial effect .
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- HY-N1159
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NF-κB
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Inflammation/Immunology
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Teuclatriol is an NF-κB inhibitor can be isolated from salvia mirzayanii, has anti-inflammatory effects. Teuclatriol inhibits TNF-α secretion in a dose-dependent manner .
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- HY-N14904
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Glycosidase
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Infection
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Panosialin D can inhibit α,β-glucosidase and mannose glycosidase. Panosialin D does not inhibit the influenza virus, but it has weak anti-microbial effect .
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- HY-162779
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PSMA
Elastase
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Others
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CDD-3290 (Compound 20) is a prostate-specific antigen (PSA) inhibitor with a Ki value of 216 nM. CDD-3290 also inhibits α-chymotrypsin and elastase .
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- HY-131345A
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PI3K
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Cancer
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(S)-PI3Kα-IN-4 is a potent inhibitor of PI3Kα, with an IC50 of 2.3 nM. (S)-PI3Kα-IN-4 shows 38.3-, 4.25-, and 4.93-fold selectivity for PI3Kα over PI3Kβ, PI3Kδ, and PI3Kγ, respectively. (S)-PI3Kα-IN-4 can be used for the research of cancer .
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- HY-120111A
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MW01-18-150SRM hydrochloride
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p38 MAPK
Autophagy
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Neurological Disease
Inflammation/Immunology
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MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
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- HY-N1029
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Mangiferitin
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Glycosidase
PPAR
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Infection
Inflammation/Immunology
Cancer
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Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM . Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively . Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
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- HY-139066
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Trichosanic acid
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TNF Receptor
GLUT
Proteasome
Tau Protein
PKC
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Neurological Disease
Metabolic Disease
Inflammation/Immunology
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Punicic acid is a bioactive compound of pomegranate seed oil. Punicic acid is an isomer of conjugated α-linolenic acid and ω-5 polyunsaturated fatty acids. Punicic acid has anti-inflammatory and antioxidant activities and can inhibit the expression of inflammatory mediators such as tumor necrosis factor α (TNF-α). Punicic acid can also reduce the formation of β-amyloid deposits and hyperphosphorylation of tau by increasing the expression of GLUT4 protein and inhibiting the overactivation of calpain, and is used to prevent and treat neurodegenerative diseases. In addition, punicic acid also has breast cancer inhibitor properties that depend on lipid peroxidation and PKC pathways .
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- HY-138071
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8αTGH
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STAT
Pyroptosis
Apoptosis
Reactive Oxygen Species
c-Myc
Bcl-2 Family
TrxR
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Cancer
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8α-Tigloyloxyhirsutinolide 13-O-acetate (8αTGH) is a potent and orally active STAT3 inhibitor. 8α-Tigloyloxyhirsutinolide 13-O-acetate induces early oxidative stress and pyroptosis, and late DNA damage, cell cycle arrest, apoptosis in the TNBC cells. 8α-Tigloyloxyhirsutinolide 13-O-acetate suppresses tumor cell growth in vitro and tumor growth in vivo .
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- HY-128942
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Drug-Linker Conjugates for ADC
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Cancer
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MAC glucuronide α-hydroxy lactone-linked SN-38 (Topoisomerase I inhibitor) is a stabilized lactone MAC glucuronide α-hydroxy lactone-linked SN-38 agent linker. MAC glucuronide α-hydroxy lactone-linked SN-38 is cytotoxic across L540cy cells and Ramos cells with IC50 values of 99 and 105 ng/mL, respectively .
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- HY-145902
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PDGFR
FLT3
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Cancer
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PDGFRα/FLT3-ITD-IN-1 (Compound 12d) is a potent inhibitor of PDGFRα/FLT3 with IC50s of more than 0.036 and 0.003 μM, respectively. PDGFRα/FLT3-ITD-IN-1 has the potential for the research of acute myeloid leukemia or chronic eosinophilic leukemia .
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- HY-169165
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Fungal
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Infection
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14α-Demethylase-IN-1 (compound 2e) is a 14α-demethylase inhibitor and can be used as an antifungal agent. 14α-Demethylase-IN-1 (48 h) exhibits MIC50 values of 2.47 μM, 1.23 μM, 19.70 μM, and 19.70 μM for C. albicans, C. parapsilosis, C. krusei, and C. glabrata, respectively .
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- HY-169737
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Glycosidase
Amylases
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Metabolic Disease
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Inulobiose is a difructan disaccharide that can be isolated from Pistacia vera L.. Inulobiose inhibits α-glycosidase and α-amylase activities with IC50s of 1.87 and 40.72 mg/mL, respectively. Inulobiose can be used for the research of diabetes and glomerular filtration rate testing .
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- HY-N0613
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NF-κB
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Inflammation/Immunology
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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 .
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- HY-160418
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PI3K
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Cancer
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PI3K-IN-51 is a PI3K inhibitor with IC50 values <500 nM for p120γ and p110δ/p85α (WO2016204429A1; Example 10) .
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- HY-110114
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Gue1654
1 Publications Verification
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Others
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Others
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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 .
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- HY-N0328
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α-Mangostin
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Reactive Oxygen Species
Apoptosis
Bacterial
Fungal
Virus Protease
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Cancer
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alpha-Mangostin (α-Mangostin) is a dietary xanthone with broad biological activities, such as antioxidant, anti-allergic, antiviral, antibacterial, anti-inflammatory and anticancer effects. It is an inhibitor of mutant IDH1 (IDH1-R132H) with a Ki of 2.85 μM.
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- HY-N15138
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Glycosidase
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Infection
Metabolic Disease
Inflammation/Immunology
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Sativanone is a compound that can be isolated from Dalbergia tonkinensis. Sativanone is a potent α-glucosidase inhibitor, with an EC50 of 0.357 mg/mL for rat α-glucosidase. Sativanone has antibacterial activity against Ralstonia solanacearum. Sativanone also has anti-senescent and antioxidant effects .
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- HY-156573
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DGK
|
Cancer
|
|
DGKα&ζ-IN-1 (Compound II) is a DGK target inhibitor. DGKα&ζ-IN-1 can enhance the function of T cells, and has a synergistic effect with PD-1, which has therapeutic effects IN both immune and tumor .
|
-
- HY-108606
-
PI-828
1 Publications Verification
|
PI3K
Casein Kinase
|
Cancer
|
|
PI-828 is a dual PI3K and casein kinase 2 (CK2) inhibitor with IC50s of 173 nM, 149 nM, and 1127 nM for p110α, CK2, and CK2α2 in lipid kinase assay, respectively .
|
-
- HY-19284
-
|
FK 687; TF 505
|
5 alpha Reductase
|
Endocrinology
|
|
FR-146687 (FK 687) is a selective and orally active 5α-reductase inhibitor with IC50s of 1.7 nM and 4.6 nM for rat and human 5α-reductases, respectively. FR-146687 shows no inhibitory effects on other steroid oxidoreductases .
|
-
- HY-120217
-
VH032
3 Publications Verification
|
Ligands for E3 Ligase
|
Cancer
|
|
VH032 is a VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. VH032 is a VHL/HIF-1α interaction inhibitor with a Kd
|
-
- HY-156681A
-
|
|
PI3K
|
Cancer
|
|
(S)-STX-478 is the S-enantiomer of STX-478. STX-478 is a selective inhibitor of PI3Kα mutants, preventing metabolic dysfunction and demonstrating antitumor activity in xenograft mouse models with PI3Kα mutant tumors .
|
-
- HY-N0492
-
|
Thioctic acid; (±)-α-Lipoic acid; DL-α-Lipoic acid
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
α-Lipoic Acid (Thioctic acid) is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
|
-
- HY-14648S3
-
|
|
Isotope-Labeled Compounds
Glucocorticoid Receptor
SARS-CoV
Autophagy
Complement System
Mitophagy
Bacterial
Antibiotic
|
Metabolic Disease
|
|
Dexamethasone-4,6α,21,21-d4 is the deuterium labeled Dexamethasone-4,6α,21,21. Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection. Dexamethasone inhibits production of exosomes containing inflammatory microRNA-155 in lipopolysaccharide-induced macrophage inflammatory responses.
|
-
- HY-123000
-
|
|
Biochemical Assay Reagents
|
|
|
4-Methylumbelliferyl 2-acetamido-2-deoxy-α-D-galactopyranoside is a fluorogenic substrate for studying the enzymatic activity of α-galactosidase. 4-Methylumbelliferyl 2-acetamido-2-deoxy-α-D-galactopyranoside is used to analyze enzyme activity in various biological samples, helping scientists gain insight into the function of the enzyme in vivo. 4-Methylumbelliferyl 2-acetamido-2-deoxy-α-D-galactopyranoside can also be used to screen potential compounds to inhibit or activate this enzyme.
|
-
- HY-N0492A
-
|
Thioctic acid sodium; (±)-α-Lipoic acid sodium; DL-α-Lipoic acid sodium
|
NF-κB
HIV
Mitochondrial Metabolism
Endogenous Metabolite
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
|
α-Lipoic Acid (Thioctic acid) sodium is an antioxidant, which is an essential cofactor of mitochondrial enzyme complexes. α-Lipoic Acid sodium inhibits NF-κB-dependent HIV-1 LTR activation . α-Lipoic Acid sodium induces endoplasmic reticulum (ER) stress-mediated apoptosis in hepatoma cells . α-Lipoic Acid sodium can be used with CPUL1 (HY-151802) to construct the self-assembled nanoaggregate CPUL1-LA NA, which has improved antitumor efficacy than CPUL1 .
|
-
- HY-165595
-
|
|
5 alpha Reductase
|
Endocrinology
|
|
The glutamic acid-alanine-glycine mixture is an orally active activator of testosterone 5α-reductase (5α-reductase). It promotes prostate function by enhancing the activity of 5α-reductase and increasing the levels of free amino acids. However, when combined with testosterone and estradiol (HY-B0141R), the glutamic acid-alanine-glycine mixture inhibits 5α-reductase activity and decreases the levels of free amino acids. The glutamic acid-alanine-glycine mixture can be used in research related to prostate function and endocrine disorders .
|
-
- HY-103248
-
|
Vengicide
|
IRE1
Fungal
Antibiotic
Apoptosis
CDK
|
Infection
Cancer
|
|
Toyocamycin (Vengicide) is an adenosine analog produced by Streptomyces diastatochromogenes, acts as an XBP1 inhibitor. Toyocamycin blocks RNA synthesis and ribosome function, and induces apoptosis. Toyocamycin affects IRE1α-XBP1 pathway, and inhibits XBP1 mRNA cleavage with an IC50 value of 80 nM with affecting IRE1α auto-phosphorylation. Toyocamycin specifically inhibits CDK9 with an IC50 value of 79 nM .
|
-
- HY-136693
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .
|
-
- HY-N0472
-
-
- HY-112619
-
TES-991
1 Publications Verification
|
Others
|
Metabolic Disease
|
|
TES-991 is a potent and selective human α Amino-β-carboxymuconate-ε-semialdehyde Decarboxylase (ACMSD) inhibitor, with an IC50 of 3 nM.
|
-
- HY-19610
-
|
α-Amatoxin
|
DNA/RNA Synthesis
ADC Cytotoxin
|
Cancer
|
|
α-Amanitin is the principal toxin of several deadly poisonous mushrooms, exerting its toxic function by inhibiting RNA-polymerase II.
|
-
- HY-17018A
-
|
ABT 200; A-75200 mesylate
|
Adrenergic Receptor
|
Neurological Disease
|
|
Napitane mesylate (ABT 200 mesylate) is an inhibitor for norepinephrine reuptake and an antagonist for presynaptic α2 receptor. Napitane mesylate exhibits antidepressant activity .
|
-
- HY-106253
-
-
- HY-12050
-
|
|
PDGFR
|
Cancer
|
|
CP-673451 is a potent and selective inhibitor of PDGFR with IC50s of 10 and 1 nM for PDGFRα and PDGFRβ, respectively.
|
-
- HY-G0008
-
|
Mebeverine metabolite O-desmethyl Mebeverine alcohol
|
Adrenergic Receptor
Drug Metabolite
|
Metabolic Disease
|
|
O-Desmethyl Mebeverine alcohol is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
|
-
- HY-N0694
-
|
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-16596
-
|
|
PI3K
|
Cancer
|
|
CNX-1351 is a potent and isoform-selective targeted covalent PI3Kα inhibitor with IC50 of 6.8 nM.
|
-
- HY-100470
-
|
|
PI3K
mTOR
|
Cancer
|
|
NSC781406 is a highly potent PI3K and mTOR inhibitor with an IC50 of 2 nM for PI3Kα.
|
-
- HY-N3625
-
|
Coronalonic acid
|
NF-κB
|
Inflammation/Immunology
|
|
Coronalolic acid, extract from the apical bud of Gardenia sootepenesis Hutch, inhibits TNF-α-induced NF-κB activity and NO production .
|
-
- HY-U00459A
-
|
|
IRE1
|
Others
|
|
GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
|
-
- HY-G0008A
-
|
Mebeverine metabolite O-desmethyl Mebeverine alcohol hydrochloride
|
Adrenergic Receptor
Drug Metabolite
|
Metabolic Disease
|
|
O-Desmethyl Mebeverine alcohol hydrochloride is a metabolite of Mebeverine, which is a potent α1 repector inhibitor, causing relaxation of the gastrointestinal tract.
|
-
- HY-U00125
-
|
|
5 alpha Reductase
|
Endocrinology
|
|
CGP-53153 is a steroidal inhibitor of 5 alpha reductase with IC50s of 36 and 262 nM in rat and human prostatic tissue, respectively.
|
-
- HY-160983
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
PHYLPA-8 is an inhibitor for DNA polymerase-α, which exhibits weak inhibitory activity for the stereochemistry of the fatty acid moiety and the cyclic phosphate .
|
-
- HY-145939
-
|
BRD5846
|
Casein Kinase
|
Cancer
|
|
BAY-888 is a selective CK1α/CSNK1A1 (casein kinase 1α) ATP-competitive inhibitor (IC50: 4 nM@10 μM ATP; 63 nM@1 mM ATP). BAY-888 blocks the negative regulation of p53 and other signaling pathways by CK1α, induces apoptosis and inhibits proliferation of tumor cells. BAY-888 has shown inhibitory efficacy against cancers such as acute myeloid leukemia (AML) in PRISM barcoded cell line screening and can mimic the effects of shRNA-mediated CK1α knockdown. BAY-888 is primarily used for the development of anticancer drugs for p53 wild-type tumors and for the study of the mechanisms of CK1α-related signaling pathways .
|
-
- HY-N3810
-
|
|
Tyrosinase
|
Others
|
|
ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid is an anti-melanin synthesis tyrosinase inhibitor, which can be isolated from Pteris fern. ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid regulates the melanogenesis transcription factor microphthalmia-associated transcription factor (MITF). The 11α-OH, 15-oxo and 16-en moieties of ent-11α-Hydroxy-15-oxokaur-16-en-19-oic acid are key fragments that inhibit melanin synthesis. The 19-COOH moiety has been implicated in the inhibition of cytotoxicity associated with 11α-OH KA and related compounds .
|
-
- HY-12987
-
-
- HY-150124A
-
|
|
Integrin
Apoptosis
|
Cancer
|
|
K34c hydrochloride is a potent and selective α5β1 integrin antagonist. By inhibiting α5β1 integrin, K34c hydrochloride reduces chemotherapy-induced premature senescence and promotes apoptosis. K34c hydrochloride can be used in glioblastoma research .
|
-
- HY-13076
-
|
|
GSK-3
|
Metabolic Disease
|
|
CHIR-98014 is a potent, cell-permeable GSK-3 inhibitor with IC50s of 0.65 and 0.58 nM for GSK-3α and GSK-3β, respectively; it shows less potent activities against cdc2 and erk2.
|
-
- HY-150124
-
|
|
Integrin
Apoptosis
|
Cancer
|
|
K34c is a potent and selective α5β1 integrin antagonist. By inhibiting α5β1 integrin, K34c reduces chemotherapy-induced premature senescence and promotes apoptosis. K34c can be used in glioblastoma research .
|
-
- HY-W005308
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
N-BOC-DL-serine methyl ester is a Serine derivative. N-BOC-DL-serine methyl ester is used for the synthesis of α,β-dehydro-α-amino acid. N-BOC-DL-serine methyl ester is also used for the synthesis of anti-cancer agent, such as quinazolinone derivative that inhibits PI3K activity, and tricyclic pyrolopyranopyridines that inhibits protein kinase activity .
|
-
- HY-110112
-
|
|
Integrin
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
BTT-3033 is an orally active conformation-selective inhibitor of α2β1 (EC50: 130 nM) by binding to the α2I domain. BTT-3033 inhibits platelet binding to collagen Ⅰ and cell proliferation, and induces cell apoptosis. BTT-3033 can be used in the research of prostate cancer, inflammation and cardiovascular disease .
|
-
- HY-160412
-
|
SAR-441566; TNFα activity modulator 3
|
TNF Receptor
|
Inflammation/Immunology
|
|
Balinatunfib (SAR-441566) is an orally active inhibitor of TNFR1 signaling. By binding to the central pocket of the soluble TNFα (sTNFα) trimer, Balinatunfib stabilizes an asymmetric conformation, blocking its binding to TNFR1 (without affecting TNFR2) and thus inhibiting downstream pathways. Balinatunfib has anti-inflammatory activity, and can be used in the study of autoimmune diseases .
|
-
- HY-156371
-
|
|
PI3K
|
Cardiovascular Disease
|
|
MIPS-21335 is an PI3KC2α inhibitor (IC50: 7 nM). MIPS-21335 also inhibits PI3KC2β, p110α, p110β and p110δ (IC50: 0.043, 0.140, 0.386, 0.742 μM). MIPS-21335 has antithrombotic effect .
|
-
- HY-151361
-
|
|
AMPK
|
Cancer
|
|
AMPK-IN-3 (compound 67) is a potent and selective AMPK inhibitor with IC50s of 60.7, 107 and 3820 nM for AMPK (α2), AMPK (α1) and KDR, respectively. AMPK-IN-3 inhibits AMPK does not affect cell viability or cause significant cytotoxicity in K562 cells. AMPK-IN-3 can be used in study of cancer .
|
-
- HY-172660
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
36R-D481 is a competitive and orthosteric antagonist of IL-36R, effectively inhibiting IL-36 signaling. 36R-D481 can inhibit IL-36α and IL-36γ but not IL-36β induced IL-8 release .
|
-
- HY-132205
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
DS45500853 is an estrogen-related receptor α (ERRα) agonist. DS45500853 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.80 μM. DS45500853 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
|
-
- HY-A0066A
-
|
Imidaline hydrochloride; NSC35110 hydrochloride
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
|
-
- HY-155956
-
|
|
Microtubule/Tubulin
Apoptosis
Bcl-2 Family
JNK
PARP
|
Cancer
|
|
GM-90257 is a microtubule acetylation inhibitor. GM-90257 binds directly to α-tubulin. GM-90257 prevents the recruitment of α-tubulin acetyltransferase 1 (αTAT1) to the K40 residue in α-tubulin. GM-90257 causes Apoptosis, downregulates BCl-2, and activates JNK and PARP. GM-90257 has anticancer activity against breast cancer .
|
-
- HY-16478
-
|
TAS-102; FTD/TPI
|
Nucleoside Antimetabolite/Analog
Thymidylate Synthase
|
Cancer
|
|
Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a potent and orally active nucleoside antitumor agent. The composition of Trifluridine/tipiracil hydrochloride mixture (TAS-102) is a 1:0.5 mixture (on a molar basis) of alpha,alpha,alpha-tri-fluorothymidine (FTD) and thymidine phosphorylase inhibitor (TPI). Trifluridine/tipiracil hydrochloride mixture (TAS-102) shows the antitumor activity mainly via the inhibition of thymidylate synthase (TS) and incorporation into DNA .
|
-
- HY-A0066
-
|
Imidaline; NSC35110
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Tolazoline (Imidaline) is an α-adrenergic receptor antagonist. Tolazoline inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
|
-
- HY-116701
-
|
|
Thyroid Hormone Receptor
|
Others
|
|
A 274 is an amiodarone analogue that has the activity of inhibiting the binding of T3 to α1- and β1-thyroid hormone receptors in vitro. Its IC50 values for inhibition of α1-T3R and β1-T3R are certain values (depending on the specific experimental results).
|
-
- HY-143201
-
|
|
Estrogen Receptor/ERR
|
Metabolic Disease
|
|
DS20362725 is an estrogen-related receptor α (ERRα) agonist. DS20362725 inhibits the binding between receptor-interacting protein 140 (RIP140) corepressor peptide (10 nM) and GST-ERRα ligand-binding domain (LBD; 1.2 μM) with an IC50 value of 0.6 μM. DS20362725 can be used for the research of metabolic disorders, including type 2 diabetes mellitus (T2DM) .
|
-
- HY-W030796R
-
|
|
Taste Receptor
|
Metabolic Disease
|
|
Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .
|
-
- HY-B0532AR
-
|
|
Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
|
Neurological Disease
Cancer
|
|
Trifluoperazine (dihydrochloride) (Standard) is the analytical standard of Trifluoperazine (dihydrochloride). This product is intended for research and analytical applications. Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .
|
-
- HY-154852
-
|
|
GSK-3
CDK
|
Neurological Disease
|
|
GSK-3 inhibitor 4 is an orally active and brain-penetrant inhibitor of GSK-3, CDK2, and CDK5, with IC50 values of 0.56 nM (GSK-3β), 0.45 nM (GSK-3α), 0.47 μM, and 0.68 μM, respectively. GSK-3 inhibitor 4 effectively reduces the phosphorylation level of Tau protein. GSK-3 inhibitor 4 can be used in Alzheimer's disease (AD) studies .
|
-
- HY-117921
-
|
|
Interleukin Related
|
Inflammation/Immunology
|
|
DA-E 5090 is an orally effective inhibitor of IL-1 production that can be converted into a pharmacologically active deacetylated form (DA-E5090) in vivo. In this study, the effects of DA-E5090 on IL-1 production in vitro were examined by LPS-stimulated human monocytes. The results showed that DA-E5090 could dose-dependently inhibit the production of IL-1α and IL-1β (1-10 μM) by LPS-stimulated human monocytes, as determined by LAF assay and ELISA. Northern blotting analysis showed that DA-E5090 inhibited the transcription of IL-1α and IL-1β mRNA.
|
-
- HY-157319
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-15 is a potent PI3Kα inhibitor with an IC50 of 0.15?μM. PI3Kα-IN-15 also has acceptable anti-proliferative activity (inhibits SKOV-3, T47D, NCI-H1975, NCI-H460, and MCF-7 growth with IC50 values of 26.6?μM, 7.9?μM,? 32.1?μM,? 17.7??μM, and 9.4??μM, respectively. PI3Kα-IN-15 can be used for cancer research .
|
-
- HY-13228
-
-
- HY-146163
-
|
|
Topoisomerase
Apoptosis
|
Cancer
|
|
Topoisomerase II inhibitor 7 (compound 3a) is a potent inhibitor of topoisomerase II alpha subtype, with an IC50 of 3.19 μM. Topoisomerase II inhibitor 7 can induce cell cycle arrest and apoptosis .
|
-
- HY-10401R
-
|
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
VX-702 (Standard) is the analytical standard of VX-702. This product is intended for research and analytical applications. VX-702 is a highly selective inhibitor of p38α MAPK, 14-fold higher potency against the p38α versus p38β .
|
-
- HY-P990281
-
|
|
Interleukin Related
|
Others
|
|
Anti-Mouse CD25/IL-2Rα Antibody (PC-61.5.3) is a rat-derived IgG1, λ type antibody inhibitor, targeting to mouse CD25/IL-2Rα.
|
-
- HY-N1919
-
|
Raubasine
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-168944
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
ABCB1-IN-4 (Compound C6z) is an orally active and potent dual α-amylase and α-glucosidase inhibitor with IC50 values of 1.63 μM and 0.14 μM, respectively. ABCB1-IN-4 is promising for research of diabetes .
|
-
- HY-N1919A
-
|
Raubasine hydrochloride
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-153980
-
|
|
RAR/RXR
COX
|
Inflammation/Immunology
|
|
K-80001 is an RXRα-binder and COX-1/2 inhibitor, with IC50s of with an IC50 of 82.9μM, 3.4μM, 1.2μM for RXRα, COX-1 and COX-2, respectively .
|
-
- HY-N2666
-
|
|
VEGFR
|
Cancer
|
|
5α-Hydroxycostic acid, a eudesmane-type sesquiterpene, is isolated from the herb Laggera alata. 5α-Hydroxycostic acid inhibits angiogenesis and suppresses breast cancer cell migration through regulating VEGF/VEGFR2 and Ang2/Tie2 pathways .
|
-
- HY-16196
-
|
IRC-110160
|
Microtubule/Tubulin
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
ENMD-1198 (IRC-110160), an orally active microtubule destabilizing agent, is a 2-methoxyestradiol analogue with antiproliferative and antiangiogenic activity. ENMD-1198 is suitable for inhibiting HIF-1alpha and STAT3 in human HCC cells and leads to reduced tumor growth and vascularization.
|
-
- HY-150739
-
-
- HY-16134A
-
|
MBI 3253 hydrochloride; MDL 28574 hydrochloride; MX3253 hydrochloride
|
Flavivirus
Dengue Virus
Glycosidase
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-16134
-
|
MBI 3253; MDL 28574; MX3253
|
Flavivirus
Dengue Virus
Glycosidase
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-16719
-
|
|
Cytochrome P450
|
Infection
|
|
Dapaconazole, as an antifungal agent, inhibits sterol 14α-demethylase cytochrome P450 activity with an IC50 of 1.4 μM .
|
-
- HY-16715
-
-
- HY-N15280
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Terrestrimine is a potent inhibitor of α-Glycosidase, with the IC50 of 225.83 μM. Terrestrimine plays an important role in metabolic disease research .
|
-
- HY-121687
-
|
α-(Hydroxyimino)benzenepropanoic acid
|
DNA/RNA Synthesis
|
Cancer
|
|
HIPP (α-(Hydroxyimino)benzenepropanoic acid) is an inhibitor for human C-terminal binding protein (CtBP), with IC50 of 745 nM and a Kd of 1.3 μM .
|
-
- HY-161262
-
|
|
FAP
|
Cancer
|
|
SB03178 is a fibroblast activation protein-alpha (FAP) inhibitor. SB03178 can be conjugated with DOTA and can be used for cancer research .
|
-
- HY-10822A
-
|
BGC 945 trisodium; Idetrexed trisodium; CB 300945 trisodium
|
Thymidylate Synthase
|
Cancer
|
|
ONX 0801 (BGC 945) trisodium is a thymidylate synthase (TS) inhibitor, targeted to α-folate receptor–overexpressing tumors .
|
-
- HY-112716
-
|
|
Amino Acid Derivatives
|
Cancer
|
|
N-alpha-Tosyl-L-lysine chloromethyl ketone (TLCK), a trypsin like protease inhibitor, sensitizes HeLa cells to Fas-mediated cell death.
|
-
- HY-N13137
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Timosaponin N is a natural steroidal saponin that inhibits the activity of α-Glucosidase. Timosaponin N can be used in diabetes-related research .
|
-
- HY-101028
-
-
- HY-139349
-
|
|
Endogenous Metabolite
|
Others
|
|
Finasteride carboxaldehyde (Compound M2) is the metabolite of 5α-reductase inhibitor Finasteride (HY-13635) in human bile and urine .
|
-
- HY-N3962R
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Glycyrrhisoflavone (Standard) is the analytical standard of Glycyrrhisoflavone. This product is intended for research and analytical applications. Glycyrrhisoflavone, an active prenylflavonoid, inhibits α-glucosidase .
|
-
- HY-148454
-
-
- HY-118712
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor WYE-23 is a mTOR inhibitor, and IC50 is 0.45 nM. It is selective to PI3Kα and IC50 is 661 nM. mTOR inhibitor WYE-23 has antitumor activity .
|
-
- HY-136010
-
|
|
RIP kinase
PROTACs
|
Inflammation/Immunology
|
|
RIP2 Kinase Inhibitor 4 is a potent and selective RIPK2 PROTAC. RIP2 Kinase Inhibitor 4 effectively degrades RIPK2 (pIC50 of 8) and inhibits the release of related TNF-α .
|
-
- HY-13635S
-
|
MK-906-d9
|
Isotope-Labeled Compounds
5 alpha Reductase
|
Cancer
|
|
Finasteride-d9 is deuterium labeled Finasteride. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-N0596R
-
|
|
PD-1/PD-L1
HIF/HIF Prolyl-Hydroxylase
STAT
|
Cancer
|
|
Panaxadiol (Standard) is the analytical standard of Panaxadiol. This product is intended for research and analytical applications. Panaxadiol (20(R)-Panaxadiol) is an orally active HIF-1α/STAT3 inhibitor. Panaxadiol can suppress HIF-1α and STAT3 then lead to downregulation of programmed cell death-ligand 1 (PD-L1) expression. Panaxadiol shows anticancer, cardioprotective, anti-arrhythmic, and antioxidative activities .
|
-
- HY-A0009S
-
|
Galantamine-d3 hydrobromide
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 μM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-170382
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
ER covalent antagonist-1 (Compound 39D) is the antagonist for estrogen receptor α (ERα). ER covalent antagonist-1 inhibits the proliferation of ERα-positive cell MCF-7 with an IC50 of 0.98 μM, arrests the cell cycle at G0/G1 phase, and induces apoptosis. ER covalent antagonist-1 exhibits antitumor efficacy in mouse model .
|
-
- HY-13635R
-
|
MK-906 (Standard)
|
5 alpha Reductase
|
Cancer
|
|
Finasteride (Standard) is the analytical standard of Finasteride. This product is intended for research and analytical applications. Finasteride (MK-906) is a potent and competitive 5α-reductase inhibitor, with an IC50 of 4.2 nM for type II 5α-reductase. Finasteride has approximately a 100-fold greater affinity for type II 5α-reductase enzyme than for the type I enzyme. Finasteride can be used for the research of benign prostatic hyperplasia (BPH) and androgenic alopecia .
|
-
- HY-P2358
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
PSMα3 is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA) .
|
-
- HY-12040
-
|
STA-4783
|
Reactive Oxygen Species
Apoptosis
Cuproptosis
|
Cancer
|
|
Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research .
|
-
- HY-148252
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
ADRA1D receptor antagonist 1 (free base) (compound (R)-9s) is an orally active, potent and selective human α1D-adrenoceptor (α1D-AR) antagonist (Ki=1.6 nM). ADRA1D receptor antagonist 1 (free base) dose-dependently inhibits bladder contraction with an IC30 value of 15 nM. ADRA1D receptor antagonist 1 (free base) can be used in studies of overactive bladder disorders such as urinary urgency, frequency and incontinence.
|
-
- HY-176060
-
|
|
Histamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
Cancer
|
|
Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis .
|
-
- HY-W009783A
-
|
|
HIV
Influenza Virus
|
Infection
Cancer
|
|
Deoxymannojirimycin hydrochloride is a selective class I α1,2-mannosidase inhibitor with an IC50 of 20 μM. Deoxymannojirimycin hydrochloride is also a N-linked glycosylation inhibitor. Deoxymannojirimycin hydrochloride has antiviral activity against HIV‐1 strains . Deoxymannojirimycin hydrochloride increases high mannose structures. Deoxymannojirimycin hydrochloride can be used for the study of liver cancer and colon cancer .
|
-
- HY-120111B
-
|
MW01-18-150SRM dihydrochloride dihydrate
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
- HY-110261
-
GS143
2 Publications Verification
|
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-164032
-
|
7α,11β-Dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate
|
GnRH Receptor
|
Endocrinology
|
|
Dimethandrolone undecanoate (7α,11β-Dimethyl-17β-hydroxyestr-4-en-3-one 17-undecanoate) exhibits withrogens and progesterone activity. Dimethandrolone undecanoate inhibits production of gonadotropins, suppresses testosterone production, and thus inhibits sperm production. Dimethandrolone undecanoate is potent for development of male hormone contraceptives .
|
-
- HY-13241A
-
|
LY2228820
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc .
|
-
- HY-106838A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
Org 6906 is a monoamine reuptake inhibitor that promotes monoaminergic neurotransmission by inhibiting the reuptake of noradrenaline, dopamine, and serotonin. Org 6906 is also an α2 Adrenergic Receptor antagonist, with a pKi value of 6.3 (using the selective α2 adrenergic receptor ligand [ 3H]rauwolscine as a ligand). Org 6906 exhibits antidepressant activity and can be used in research related to neurological disorders .
|
-
- HY-B0223
-
-
- HY-155211
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-13 (compound 9g), an aryl ureido compound, is a potent and selective mTOR inhibitor with an IC50 of 0.29 nM. mTOR inhibitor-13 also inhibits PI3K-α with an IC50 of 119 nM .
|
-
- HY-122958
-
|
|
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-P10898
-
-
- HY-N10132
-
|
|
nAChR
|
Infection
Neurological Disease
|
|
Microgrewiapine A is an antagonist of nAChR. Microgrewiapine A inhibits hα4β2 and hα3β4 activity with 60% and 70% inhibition, respectively. Microgrewiapine A has selective cytotoxic against HT-29 human colon cancer cells with an IC50 of 6.8 μM .
|
-
- HY-14282
-
|
|
Fungal
|
Infection
Inflammation/Immunology
|
|
Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi?in vitro?and?in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
|
-
- HY-155199
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD .
|
-
- HY-121638A
-
|
|
Apoptosis
DGK
|
Cancer
|
|
(5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
|
-
- HY-117845
-
|
LL-E19085α
|
Bacterial
Antibiotic
|
Infection
|
|
Citreamicin alpha (LL-E 19085-alpha) is an antibiotic whose in vitro antimicrobial activity against 429 clinical isolates of Gram-positive cocci has been tested by the agar dilution method. These microorganisms included 313 strains of Staphylococci and 116 strains of Streptococci. The in vitro activity of Citreamicin alpha was compared with that of ampicillin, amoxicillin, ceftriaxone, erythromycin, and vancomycin. For Staphylococci, the MIC values of Citreamicin alpha ranged from 0.12-4.0 μg/ml, and for Streptococcus pyogenes of the genus Streptococcus, it was 0.03-0.12 μg/ml. However, enterococci were relatively resistant, requiring 2.0 μg/ml of the agent to inhibit 64% of the 62 tested strains. The in vitro activity of this antibiotic was much better than that of ampicillin, amoxicillin, ceftriaxone, and erythromycin, but comparable or slightly inferior to that of vancomycin.
|
-
- HY-150687
-
|
|
ERK
|
Metabolic Disease
|
|
ZINC12409120 is a high selective ERK inhibitor. ZINC12409120 acts on disrupting FGF23:α-Klotho interaction to inhibit ERK activity with an IC50 of 5.0 μM .
|
-
- HY-15845
-
|
|
IRE1
|
Cancer
|
|
STF-083010 is a specific IRE1α inhibitor. STF-083010 inhibits Ire1 endonuclease activity, without affecting its kinase activity, after endoplasmic reticulum stress.
|
-
- HY-12348
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
LEO 29102 is a potent phosphodiesterase 4 (PDE4) inhibitor with an IC50 value of 5 nM. LEO 29102 inhibits TNFα release. LEO 29102 has the potential for the research of atopic dermatitis .
|
-
- HY-112182
-
|
DAS-DFGO-II
|
Src
p38 MAPK
Autophagy
|
Cancer
|
|
UM-164 (DAS-DFGO-II) is a highly potent inhibitor of c-Src with a Kd of 2.7 nM. UM-164 also potently inhibits p38α and p38β.
|
-
- HY-15704
-
LH846
1 Publications Verification
|
Casein Kinase
|
Cancer
|
|
LH846 is a selective inhibitor of CKIδ, with an IC50 of 290 nM, and less potently inhibits CKIα and CKIε, with IC50s of 2.5 μM and 1.3 μM, respectively.
|
-
- HY-171468
-
|
|
TNF Receptor
|
Cancer
|
|
CC-1069, a structural analog of thalidomide (HY-14658), is a TNF-α inhibitor that inhibits endothelial. CC-1069 can be used to study angiogenesis-dependent tumors such as gliomas .
|
-
- HY-14622
-
|
|
RIP kinase
|
Cancer
|
|
Necrostatin 2 is a potent necroptosis inhibitor. EC50 for inhibition of necroptosis in FADD-deficient Jurkat T cells treated with TNF-α is 0.05 μM. Necrostatin 2 is also a RIPK1 inhibitor.
|
-
- HY-170491
-
|
|
GSK-3
|
Infection
Neurological Disease
|
|
GSK-3β inhibitor 23 (Compound 11726169) is the inhibitor for glycogen synthase kinase-3, that inhibits GSK-3β and GSK-3α with IC50 of 12.1 nM and 18.8 nM. GSK-3β inhibitor 23 exhibits antiviral activity against HIV 1. GSK-3β inhibitor 23 exhibits good metabolic stablility in mouse/human liver microsomes and plasma, but poor Caco-2 permeability (which predicts low oral bioavailability) .
|
-
- HY-149054
-
|
|
GSK-3
Tau Protein
AAK1
Pim
PKC
|
Neurological Disease
|
|
GSK-3β inhibitor 13 (compound 47) is an orally active and potent GSK-3β inhibitor with blood-brain permeability. GSK-3β inhibitor 13 inhibits GSK-3β and GSK-3α with IC50s of 0.73 nM and 0.35 nM, respectively. GSK-3β inhibitor 13 significantly decreases the phosphorylation of tau (IC50=58 nM), which leads the formation of the neurofibrillary tangles associated with Alzheimer's disease .
|
-
- HY-162025
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-17 (Compound 9e) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 0.68 and 1359 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 40 nM .
|
-
- HY-162024
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-16 (Compound 9f) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 1.25 and 82 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 140 nM .
|
-
- HY-162023
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-10 (Compound 9c) is a selective inhibitor for mTOR. mTOR inhibitor-10 inhibits mTOR and PI3K-α, with IC50 of 0.7 and 825 nM. mTOR inhibitor-10 inhibits proliferation of LNCaP with IC50 of 87 nM .
|
-
- HY-154851
-
|
|
GSK-3
CDK
Tau Protein
|
Neurological Disease
|
|
GSK-3 inhibitor 3 is a selective, orally active and brain-penetrant inhibitor of GSK-3, with IC50s of 0.35 nM and 0.25 nM for GSK-3α and GSK-3β, respectively. GSK-3 inhibitor 3 lowers levels of tau protein phosphorylation at S396 in a triple-transgenic mouse Alzheimer’s disease model, with IC50 of 10 nM. GSK-3 inhibitor 3 can be used for neurological disease research .
|
-
- HY-N11530
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Kouitchenside G is a natural product that can be isolated from Swertia kouitchensis. Kouitchenside G inhibits α-Glucosidase with an IC50 of 956 μM .
|
-
- HY-13468
-
KW-2478
3 Publications Verification
|
HSP
|
Cancer
|
|
KW-2478 is an inhibitor of Hsp90α, with an IC50 of 3.8 nM, and has antitumor activity against various human hematological tumor cells.
|
-
- HY-N8816
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Stipuleanoside R2 inhibits NF-κB activation stimulated by TNFα in a dose-dependent manner with IC50 value of 4.1 μM .
|
-
- HY-168848
-
-
- HY-17018
-
|
ABT 200 free acid; A-75200
|
Adrenergic Receptor
|
Neurological Disease
|
|
Napitane (A 75200) is a groundbreaking catecholamine uptake inhibitor that exhibits inhibitory effects on α-adrenergic receptors and shows promise for antidepressant activity in depression research.
|
-
- HY-13535
-
|
|
Integrin
|
Cancer
|
|
ATN-161 is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
|
-
- HY-121401
-
|
(±)-Myrtenal
|
TNF Receptor
|
Cancer
|
|
Myrtenal ((±)-Myrtenal) is a monoterpene that acts as an antineoplastic agent. Myrtenal inhibits liver cancer by preventing DEN-PB-induced upregulation of TNF-α protein expression.
|
-
- HY-135386
-
-
- HY-15377
-
|
|
GABA Receptor
|
Neurological Disease
|
|
DL-Gabaculine hydrochloride is a neurotoxin that irreversibly inhibits bacterial pyridoxal phosphate linked γ-aminobutyric acid-α-ketoglutaric acid transaminase with a Ki of 2.86 μM .
|
-
- HY-N12263
-
|
|
Amylases
|
Metabolic Disease
|
|
3,5,6,7,8,4'-Hexamethoxyflavone is a inhibitor of α-Amylase with the inhibitory activity of 28.3% at 500 μM .
|
-
- HY-111365
-
|
|
Others
|
Metabolic Disease
|
|
TES-1025 is a potent and selective human α-amino-β-carboxymuconate-ε-semialdehyde decarboxylase (ACMSD) inhibitor with an IC50 of 13 nM .
|
-
- HY-19292
-
|
|
5 alpha Reductase
|
Endocrinology
|
|
AS-601811(compound 47) is a 5alpha-reductase 1 inhibitor with the IC50 of 20 nM and can be used for study of alopecia and hirsutism .
|
-
- HY-123120
-
|
|
Thrombin
|
Others
|
|
SA-152 is an organophosphorus inhibitor. SA-152 modulates the fibrinogen coagulation and TAME esterase activity of bovine α-thrombin .
|
-
- HY-13535A
-
|
ATN-161 TFA salt
|
Integrin
|
Cancer
|
|
ATN-161 trifluoroacetate salt is a novel integrin α5β1 antagonist, which inhibits angiogenesis and growth of liver metastases in a murine model.
|
-
- HY-N1470
-
|
|
Others
|
Metabolic Disease
|
|
Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM .
|
-
- HY-163501
-
|
|
PI3K
Akt
|
Cancer
|
|
PI3Kα-IN-23 (Compound 9) is an inhibitor of PI3Ka H1047R .
|
-
- HY-P10241
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
Ac-LEHD-CHO is an inhibitor for caspase 8/9. Ac-LEHD-CHO prevents GalN/TNF-α-induced hepatotoxicity and hepatocyte apoptosis .
|
-
- HY-17412S1
-
|
|
Isotope-Labeled Compounds
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Minocycline-d6 sulfate is deuterated labeled Minocycline (HY-17412A). Minocycline is an orally effective semi-synthetic tetracycline antibiotic and HIF-1α inhibitor that can penetrate the blood-brain barrier. Minocycline has bacteriostatic, anti-cancer, anti-inflammatory, neuroprotective properties and antidepressant effects.
|
-
- HY-131305
-
|
|
PKC
Apoptosis
|
Neurological Disease
|
|
HBDDE, a derivative of Ellagic acid, is an isoform-selective PKCα and PKCγ inhibitor with IC50s of 43 μM and 50 μM, respectively. HBDDE shows selective for PKCα/PKCγ over PKCδ, PKCβI and PKCβII isozymes. HBDDE induces neuronal apoptosis .
|
-
- HY-113649
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
AKB-6899, a prolyl hydroxylase domain 3 (PHD3) inhibitor, is a selective HIF-2α stabilizer. AKB-6899 also increases soluble form of the VEGF receptor (sVEGFR-1) production from GM-CSF-treated macrophages, and has antitumor and antiangiogenic effects .
|
-
- HY-P4191
-
|
MSPYSSDTTPCCFAYIARPLPRAHIKEYFYTSGKCSN
|
CCR
|
Inflammation/Immunology
|
|
Met-RANTES (human) is the antagonist for CCR1 and CCR5. Met-RANTES (human) inhibits chemokines human MIP-1α and MIP-1β with IC50 of 5 and 2 nM. Met-RANTES (human) reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA) .
|
-
- HY-N1881
-
|
|
Lipoxygenase
Glycosidase
|
Others
|
|
4',5-Dihydroxyflavone is a soybean LOX-1 and yeast α-Glucosidase inhibitor, with an Ki of 102.6 μM for soybean LOX-1 and an IC50 of 66 μM for yeast α-glucosidase. LOX-1 isshort for Lectin-like oxidized low-density lipoprotein receptor-1.
|
-
- HY-114865
-
|
|
RGS Protein
Calcium Channel
|
Neurological Disease
|
|
BMS-192364 is targeting the Gα-RGS interaction to produce an inactive Gα-RGS complex. BMS-192364 reduces urinary bladder contraction and exert RGS-agonist properties by increasing the action of GAPs on Gq proteins. BMS-192364 inhibits calcium flux .
|
-
- HY-131547
-
|
10-Ethenyl-19-norprogesterone
|
Progesterone Receptor
p38 MAPK
|
Endocrinology
|
|
Org OD 02-0 (10-Ethenyl-19-norprogesterone) is a membrane progesterone receptor α (mPRα)-specific agonist (IC50: 33.9 nM). Org OD 02-0 activates MAPK activity. Org OD 02-0 inhibits prolactin (PRL) secretion in the pituitary .
|
-
- HY-14415
-
|
|
REV-ERB
|
Neurological Disease
Metabolic Disease
|
|
SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease .
|
-
- HY-117082
-
|
GBL-5g
|
TNF Receptor
|
Inflammation/Immunology
|
|
UTL-5g (GBL-5g), an anti-inflammatory TNF-α inhibitor, has chemoprotective and liver radioprotective effects. UTL-5g lowers hepatotoxicity, nephrotoxicity, and myelotoxicity induced by Cisplatin through TNF-α inhibition among other factors .
|
-
- HY-123044
-
-
- HY-168130
-
|
|
TNF Receptor
Interleukin Related
|
Cardiovascular Disease
|
|
TNF-α/IL-1β-IN-1 (compund 11a) is an anti-inflammatory agent that reduces the expression of TNF-α and IL-1β, inhibits oxidative stress and cardiomyocyte apoptosis, has good activity against septic myocardial injury, and improves myocardial blood supply in vivo .
|
-
- HY-75095
-
|
S-(-)-α-Phenylethylamine; L-(-)-α-Methylbenzylamine
|
Drug Intermediate
Biochemical Assay Reagents
|
Neurological Disease
|
|
(S)-(-)-1-Phenylethanamine (S-(-)-α-Phenylethylamine; L-(-)-α-Methylbenzylamine) is a S-isomer of 1-Phenylethanamine (HY-W012848). 1-Phenylethanamine is a potential central nervous system stimulant and can be used to synthesize the tyrosine kinase inhibitor CLM3 (HY-164413) .
|
-
- HY-119424
-
-
- HY-126932
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
TTC-352 is an orally bioavailable selective human estrogen receptor (ER) α partial agonist (ShERPA). TTC-352 inhibits the growth of three ER+ breast cancer cells. TTC-352 induces tumor regression accompanied by exit of ERα from the nucleus to extranuclear sites .
|
-
- HY-B0661R
-
|
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin (Standard) is the analytical standard of Tamsulosin. This product is intended for research and analytical applications. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
|
-
- HY-10172
-
|
IKK2 Inhibitor V
|
IKK
|
Cancer
|
|
IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity . IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM .
|
-
- HY-32015
-
|
|
MAP3K
|
Inflammation/Immunology
|
|
Cot inhibitor-1 (compound 28) is a selective tumor progression loci-2 (Tpl2) kinase inhibitor with an IC50 of 28 nM. Cot inhibitor-1 shows an inhibition of TNF-alpha production in human whole blood with an IC50 of 5.7 nM .
|
-
- HY-121311
-
|
|
Serotonin Transporter
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Metrenperone is an inhibitor for 5-HT2 receptor. Metrenperone exhibits α1 and α2 antagonist activity as well as anti-H1 and anti-dopaminergic efficacy. Metrenperone can lower the blood pressure, enhances bradycardia in peripheral ischemia, inhibits serotonin-induced platelet aggregation, and antagonizes serotonin-mediated vasoconstriction. Metrenperone promotes the repair of acutely damaged collagen tissue .
|
-
- HY-151129
-
|
|
nAChR
|
Neurological Disease
|
|
nAChR-IN-1 (2,2,6,6-Tetramethylpiperidin-4-yl heptanoate) is a tetramethylpiperidine heptanoate, a selective nicotinic acetylcholine receptor (nAChR) inhibitor that inhibits nAChRs lacking α5, α6, or β3 subunits. nAChR-IN-1 has the effect of preventing nerve disorder, can be used for nicotinic acetylcholine receptor dysfunction or neurological disorders research .
|
-
- HY-150738
-
-
- HY-N10076
-
-
- HY-108162
-
|
|
COX
|
Inflammation/Immunology
|
|
Ataquimast free base is a COX-2 inhibitor that inhibits the release of leukotrienes, TNF-α and GM-CSF. Ataquimast free base can be used in the study of advanced receptor-positive breast cancer .
|
-
- HY-100339
-
GSK583
5 Publications Verification
|
RIP kinase
|
Endocrinology
|
|
GSK583 is a highly potent, orally active and selective inhibitor of RIP2 Kinase, with IC50 of 5 nM. GSK583 inhibits both TNF-α and IL-6 production with an IC50 value of 200 nM.
|
-
- HY-150738C
-
-
- HY-137613
-
|
|
HIV
|
Infection
Inflammation/Immunology
|
|
Sp-TTPαS is a competitivesterile alpha motif and HD domain containing protein 1 (SAMHD1) catalysis inhibitor. Sp-TTPαS competitively inhibits TTP hydrolysis with a Ki value of 46 µM .
|
-
- HY-N1425
-
|
|
Others
|
Metabolic Disease
|
|
Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2 μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract .
|
-
- HY-129571
-
-
- HY-169100
-
|
|
VEGFR
PI3K
Akt
mTOR
p38 MAPK
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
Antiproliferative agent-57 (compound M2) is a tumor angiogenesis inhibitor. Antiproliferative agent-57 inhibits the secretion of VEGF in SiHa cells under hypoxic conditions (IC50=0.68 μM) without inducing cytotoxicity. Antiproliferative agent-57 can modulate the PI3K/AKT/mTOR and MAPK signaling pathways in tumor cells to inhibit the expression of HIF-1α and VEGF in tumor tissues .
|
-
- HY-173416
-
|
|
NF-κB
p38 MAPK
ERK
JNK
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 100 (Compound (+)-4S-23) is an anti-inflammatory agent. Anti-inflammatory agent 100 inhibits MAPK and NF-κB signaling, and also inhibits NF-κB pathway by suppressing the phosphorylation of IκB-α and blocking nuclear translocation of phosphorylated p65. Anti-inflammatory agent 100 inhibits NO production (IC50: 0.5 μM) and TNF-α, IL-6, IL-1β secretion .
|
-
- HY-100603A
-
|
|
PI3K
PI4K
|
Infection
|
|
(S)-GSK-F1 (Compound 28) is an inhibitor for type III phosphatidylinositol 4-kinase α (PI4KIIIα). (S)-GSK-F1 inhibits PI4Kα, PI4Kβ, PI4Kγ, PI3Kα, PI3Kβ and PI3Kδ with pIC50 of 8.3, 6.0, 5.6, 5.6, 5.1 and 5.6, respectively. (S)-GSK-F1 exhibits anti-hepatitis C virus (HCV) activity through inhibition of HCV replication. (S)-GSK-F1 exhibits moderate pharmacokinetic characters in rat model .
|
-
- HY-14649S2
-
|
|
Isotope-Labeled Compounds
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
11-cis-Retinoic Acid-d5 is the deuterium labeled Retinoic acid. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[1][2].
|
-
- HY-P2358A
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
PSMα3 TFA is a peptide for manipulating DCs to become tolerogenic for DC vaccination strategies. PSMα3 TFA penetrates and modulates human monocyte-derived DCs by altering the TLR2- or TLR4-induced maturation, inhibiting pro- and anti-inflammatory cytokine production and reducing antigen uptake. PSMα3 TFA is an important toxin released by the most virulent strains of methicillin-resistant Staphylococcus aureus (MRSA) .
|
-
- HY-101144
-
|
TCD-717
|
Others
|
Cancer
|
|
RSM-932A (TCD-717) is a specific ChoKα inhibitor with IC50s of 1 and 33 μM for human recombinant ChoKα and ChoKβ enzymes, respectively. RSM-932A acts as the “first in humans” compound targeting ChoKα. RSM-932A is potent in vitro anti-proliferative and in vivo anti-tumoral activity against human xenografts in mice, showing high efficacy with low toxicity profiles .
|
-
- HY-A0009R
-
|
Galantamine (hydrobromide) (Standard)
|
nAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-133949
-
|
|
5 alpha Reductase
|
Endocrinology
|
|
8,11-Eicosadiynoic acid, an unsaturated fatty acid, is a steroid 5α-reductase inhibitor. 8,11-Eicosadiynoic acid can be used for the research of acne .
|
-
- HY-N0604
-
-
- HY-N15229
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Resinacein L is an inhibitor for α-glucosidase with an IC50 of 0.635 mM. Resinacein L slows down the digestion and absorption of carbohydrates, thereby decreasing postprandial blood glucose .
|
-
- HY-112502C
-
|
Adenosine 5'-(α,β-methylene)diphosphate triammonium
|
CD73
|
Cancer
|
|
MethADP (Adenosine 5'-(α,β-methylene)diphosphate) triammonium is a CD73 inhibitor. MethADP can be used for the research of ATP-adenosine pathway .
|
-
- HY-164905
-
|
|
DGK
|
Cancer
|
|
DGK-IN-8 (Example 34) is a DGK inhibitor, with IC50 of ≤ 20 nM for DGKα and ζ. DGK-IN-8 can be used for cancer research .
|
-
- HY-12495
-
-
- HY-114657
-
|
|
Neprilysin
|
Others
|
|
Benproperine is a new neprilysin B inhibitor composed of N-acyl-L-prolyl-L-valine, whose N-acyl moiety is α-isobutylsuccinic acid β-hydroxamic acid.
|
-
- HY-139830
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A-IN-1 is a triple inhibitor of Dyrk1A kinase activity (IC50 = 119 nM) and the aggregation of tau and α-syn oligomers.
|
-
- HY-139307
-
|
|
Tau Protein
|
Neurological Disease
|
|
MG-2119 is a potent monomeric tau and α-syn aggregation inhibitor. MG-2119 is a potential agent for neurological disorders research .
|
-
- HY-119657
-
|
|
Bacterial
|
Others
|
|
Cellocidin is an agricultural antibiotic with preventive effects against rice bacterial leaf blight and is thought to work by inhibiting the α-ketoglutarate-succinate system in Xanthomonas sp.
|
-
- HY-N9867
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Gnetifolin E is a resveratrol trimer derivative that can be isolated from Gnetum brunonianum. Gnetifolin E has anti-inflammatory activity, and inhibits TNF-α .
|
-
- HY-138992
-
|
|
Glycosidase
Endogenous Metabolite
|
Others
|
|
2,3-Indolobetulin is a pentacyclic triterpene and a derivative of betulin. 2,3-Indolobetulin can be used in the synthesis of α-glucosidase inhibitors .
|
-
- HY-15244A
-
|
BYL-719 hydrochloride
|
PI3K
|
Cancer
|
|
Alpelisib hydrochloride (BYL-719 hydrochloride) is a potent, orally active, and selective PI3Kα inhibitor with IC50s of 5 nM, 250 nM, 290 nM and 1200 nM for p110α, p110γ, p110δ, and p110β, respectively. Alpelisib hydrochloride (BYL-719 hydrochloride) shows antineoplastic activity .
|
-
- HY-116830
-
BRD0705
1 Publications Verification
|
GSK-3
|
Cancer
|
|
BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) research .
|
-
- HY-101755
-
-
- HY-118091
-
|
|
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-161429
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
Antidiabetic agent 5 (compound S1) is a antidiabetic agent. Antidiabetic agent 5 inhibits the activity of α-glucosidase and α-amylase with IC50 values of 3.91，8.89 μM，respectively. Antidiabetic agent 5 decreases sugar levels. Antidiabetic agent 5 has the potential for the research of type-II diabetes .
|
-
- HY-126052
-
|
|
COX
Tyrosinase
HDAC
|
Metabolic Disease
Cancer
|
|
Gnetol is a phenolic compound isolated from the root of Gnetum montanum . Gnetol potently inhibits COX-1 (IC50 of 0.78 μM) and HDAC. Gnetol is a potent tyrosinase inhibitor with an IC50 of 4.5 μM for murine tyrosinase and suppresses melanin biosynthesis. Gnetol has antioxidant, antiproliferative, anticancer and hepatoprotective activity. Gnetol also possesses concentration-dependent α-Amylase, α-glucosidase, and adipogenesis activities .
|
-
- HY-P0109
-
|
|
Cathepsin
|
Others
|
|
(S,S)-Z-FA-FMK is a cell-permeable, irreversible cathepsin B inhibitor. (S,S)-Z-FA-FMK blocks LPS-induced production of IL-1α and IL-1β. (S,S)-Z-FA-FMK can be used as a negative control for caspase-1 and caspase-2 inhibitors because it lacks an aspartic acid residue at the P1 position .
|
-
- HY-159491
-
|
|
Dipeptidyl Peptidase
Glycosidase
Amylases
|
Metabolic Disease
|
|
DPP-4-IN-11 (compound 10) is an orally active DPP-4 inhibitor (IC50=2.75 μM) with anti-type 2 diabetes activity. DPP-4-IN-11 exerts its glucose-lowering effect by inhibiting the activities of α-glucosidase (IC50=3.02 μM) and α-amylase (IC50=3.3 μM) .
|
-
- HY-164483
-
|
|
Akt
Trk Receptor
|
Cancer
|
|
HS-345 is a TrkA/Ak inhibitor with significant anti-pancreatic cancer effects. HS-345 inhibits the growth and proliferation of pancreatic cancer cells by targeting the TrkA/Akt signaling pathway, while also inducing apoptosis. Additionally, HS-345 suppresses blood vessel formation by decreasing the expression of HIF-1α and VEGF. HS-345 holds promise for research in pancreatic cancer .
|
-
- HY-119940
-
|
(rel)-MC180295
|
CDK
|
Cancer
|
|
MC180295 ((rel)-MC180295) is a potent and selective CDK9-Cyclin T1 inhibitor, with an IC50 of 5 nM, at least 22-fold more selective for CDK9 over other CDKs. MC180295 also inhibits GSK-3α and GSK-3β. MC180295 ((rel)-MC180295) has potent anti-tumor effect .
|
-
- HY-101855
-
|
Anle138b
|
Amyloid-β
|
Neurological Disease
|
|
Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
|
-
- HY-156586
-
|
ASN90
|
OGA
Tau Protein
|
Neurological Disease
|
|
Egalognastat (ASN90) is a selective, brain-penetrant and orally active O-GlcNAcase (OGA) enzyme inhibitor with an IC50 value of 10.2 nM. Egalognastat increases O-GlcNAcylation of intracellular proteins like tau and α-synuclein, preventing their aggregation and toxicity. Egalognastat does not inhibit hexosaminidase (Hex). Egalognastat can be used for the research of neurodegenerative diseases, such as tauopathies and α-synucleinopathies (e.g., Alzheimer’s disease and Parkinson’s disease) .
|
-
- HY-10580
-
|
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-15466
-
|
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-12030
-
PIK-90
4 Publications Verification
|
PI3K
DNA-PK
|
Cancer
|
|
PIK-90 is a DNA-PK and PI3K inhibitor, which inhibits p110α, p110γ and DNA-PK with IC50s of 11, 18 and 13 nM, respectively.
|
-
- HY-13862
-
AZD1080
5 Publications Verification
|
GSK-3
|
Neurological Disease
|
|
AZD1080 is a potent and selective GSK3 inhibitor. AZD1080 inhibits recombinant human GSK3α and GSK3β with pKi (IC50) of 8.2 (6.9 nM) and 7.5 (31 nM), respectively.
|
-
- HY-N7763
-
|
|
Glycosidase
|
Neurological Disease
|
|
Casuarictin is a potent and competitive α-glucosidase inhibitor with an IC50 of 0.21 μg/mL. Casuarictin is a presenilin stabilization factor like protein (PSFL) protein inhibitor. Casuarictin can be used for Alzheimer's disease research .
|
-
- HY-169053
-
|
|
IKK
NF-κB
|
Cancer
|
SU1261 is an IKK inhibitor with Ki values of 10 nM and 680 nM for IKKα and IKKβ, respectively. SU1261 can inhibit non-canonical NF-κB signaling in U2OS osteosarcoma cells .
|
-
- HY-136794
-
|
|
p38 MAPK
Epigenetic Reader Domain
|
Inflammation/Immunology
Cancer
|
|
SB-284851-BT is an inhibitor of BRD4/p38α/BRDT. SB-284851-BT inhibits BRD4-BD1 (IC50=1.7 µM), p38α (Kd=0.47 nM), BRDT (1) (IC50=18 µM) and BRD4 (1)(IC50=3.7 µM). SB-284851-BT reduces IL-8 production by inhibiting p38α, as well as inhibiting BRD4 to down-regulates c-Myc and NF-κB gene pathways in cancer. SB-284851-BT can combined with the bromine domain and extra terminal (BET) .
|
-
- HY-164662
-
|
|
mTOR
PI3K
|
Cancer
|
|
mTOR inhibitor-24 (comounp 9d) is a mTOR inhibitor, with IC50s of 0.34 nM (mTOR) and 324 nM (PI3K-α) respectively. mTOR inhibitor-24 inhibtis LNCaP cell proliferation (IC50: 180 nM) .
|
-
- HY-100575
-
|
Acriflavinium chloride 3,6-Acridinediamine mix
|
Fluorescent Dye
HIF/HIF Prolyl-Hydroxylase
Bacterial
SARS-CoV
Monocarboxylate Transporter
Fungal
|
Infection
Cancer
|
|
Acriflavine (Acriflavinium chloride) is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine is an antiseptic agent. Acriflavine is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2 .
|
-
- HY-W088075
-
|
Acriflavinium chloride hydrochloride
|
Fluorescent Dye
HIF/HIF Prolyl-Hydroxylase
Bacterial
SARS-CoV
Monocarboxylate Transporter
Fungal
|
Infection
Cancer
|
|
Acriflavine (Acriflavinium chloride) hydrochloride is a fluorescent acridine dye that can be used to label nucleic acid. Acriflavine hydrochloride is an antiseptic agent. Acriflavine hydrochloride is a potent HIF-1 inhibitor that prevents the dimerization of HIF-1α and HIF-1β subunits. Acriflavine hydrochloride inhibits the interaction between monocarboxylate transporter 4 (MCT4) and Basigin. Acriflavine hydrochloride is used in cancer research, such as breast cancer, brain tumor and chronic myeloid leukemia. Acriflavine hydrochloride is a potent papain-like protease (PLpro) inhibitor, which inhibits SARS-CoV-2 .
|
-
- HY-146066
-
|
|
nAChR
JAK
STAT
NO Synthase
|
Inflammation/Immunology
|
|
α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
|
-
- HY-W014589R
-
|
2,4-DTBP (Standard)
|
Endogenous Metabolite
Fungal
Apoptosis
RAR/RXR
Amyloid-β
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
2,4-Di-tert-butylphenol (Standard) is the analytical standard of 2,4-Di-tert-butylphenol (HY-W014589). This product is intended for research and analytical applications. 2,4-Di-tert-butylphenol (2,4-DTBP) is an orally active RXRα activator and a human estrogen receptor ligand with anti-inflammatory and antioxidant activities, which can induce apoptosis in tumor cells. 2,4-Di-tert-butylphenol can activate the RXRα subtype in LXRα/RXRα, PPARγ/RXRα, and hormone receptor β/RXRα. 2,4-Di-tert-butylphenol also has antiviral and antifungal activities, and has the potential to inhibit Aβ-induced neurotoxicity. 2,4-Di-tert-butylphenol can be used as an intermediate in the preparation of antioxidants and UV stabilizers, and is also used in the manufacture of pharmaceuticals and fragrances .
|
-
- HY-146066A
-
|
|
nAChR
JAK
STAT
NO Synthase
|
Others
|
|
(R)-α7 nAchR-JAK2-STAT3 agonist 1 is the R-enantiomer of α7 nAchR-JAK2-STAT3 agonist 1 (HY-146066). α7 nAchR-JAK2-STAT3 agonist 1 is a potent α7 nAchR-JAK2-STAT3 agonist, with an IC50 value of 0.32 μM for nitric oxide (NO). α7 nAchR-JAK2-STAT3 agonist 1 effectively suppresses the expression of iNOS, IL-1β, and IL-6 in murine RAW264.7 macrophages. α7 nAchR-JAK2-STAT3 agonist 1 can inhibit LPS-induced NO release, NF-κB activation and cytokine production. α7 nAchR-JAK2-STAT3 can be used for researching sepsis .
|
-
- HY-162677
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
MT-1207 is an orally active and selective adrenergic α1 and 5-HT2A receptor antagonist. MT-1207 shows IC50<0.1 nM, 0.15 nM, 1.40 nM and 0.27 nM for α1A, α1B, α1D and 5-HT2A, respectively. MT-1207 achieves an effective blood pressure (BP) reduction in the 2K2C rat model without damaging renal function. MT-1207 is a potent multitarget inhibitor with the potential for vasodilatation research .
|
-
- HY-120752
-
|
|
Prostaglandin Receptor
|
|
|
CAY10509 is a PGF2α analog and an inhibitor of the FP receptor with an IC50 of 30 nM. CAY10509 is promising for studying physiological regulatory mechanisms related to prostaglandins .
|
-
- HY-N0466R
-
|
|
Endogenous Metabolite
Glycosidase
|
Others
|
|
Rebaudioside A (Standard) is the analytical standard of Rebaudioside A. This product is intended for research and analytical applications. Rebaudioside A is a steviol glycoside and α-glucosidase inhibitor with an IC50 of 35.01 ug/mL.
|
-
- HY-N10835
-
|
|
Others
|
Inflammation/Immunology
|
|
Gnetumontanin B is a stilbenoid that can be found in Gnetum montanum f. megalocarpum. Gnetumontanin B inhibits TNF-α production with an IC50 value of 1.49 µM .
|
-
- HY-N10426
-
|
|
Glycosidase
|
Metabolic Disease
|
|
(+)-Cembrene A (Compound 5) is a α-glucosidase inhibitor with an IC50 of 30.31 μM. (+)-Cembrene A is nontoxic towards human normal hepatocyte (LO2) cells .
|
-
- HY-N9315
-
-
- HY-N6602
-
-
- HY-120215
-
|
|
MAGL
|
Metabolic Disease
|
|
KT203 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.31 nM in Neuro2A cells .
|
-
- HY-112502D
-
|
Adenosine 5'-(α,β-methylene)diphosphate trisodium
|
CD73
|
Cancer
|
|
MethADP (Adenosine 5'-(α,β-methylene)diphosphate) trisodium is a CD73 inhibitor. MethADP trisodium can be used for the research of ATP-adenosine pathway .
|
-
- HY-102040
-
|
(Z)-Hispidol
|
TNF Receptor
|
Inflammation/Immunology
|
|
Hispidol ((Z)-Hispidol) is a potential therapeutic for inflammatory bowel disease; inhibits TNF-α induced adhesion of monocytes to colon epithelial cells with an IC50 of 0.50 μM.
|
-
- HY-129131
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Chrysin 6-C-arabinoside 8-C-glucoside is a α±-glucosidase inhibitors which are widely used in the study for type 2 diabetes .
|
-
- HY-162637
-
|
|
Glycosidase
|
Metabolic Disease
|
|
CTL26 is a potent and orally active α-glucosidase inhibitor with an IC50 value of 2.81 µM. CTL26 shows anti-diabetic efficacy .
|
-
- HY-120177
-
|
|
MAGL
|
Others
|
|
KT182 is a potent and selective inhibitor of α/β-hydrolase domain containing 6 (ABHD6), with an IC50 of 0.24 nM in Neuro2A cells .
|
-
- HY-W031307
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase IIα-IN-8 (compound 15) is a weak human DNA topoisomerase IIa (htIIa) inhibitor, with an IC50 of 462 ± 38.0 μM .
|
-
- HY-117761
-
|
|
PPAR
|
Metabolic Disease
Cancer
|
|
MHY908 is a potent dual agonist of PPARα and PPARγ . MHY908 also inhibits melanogenesis through inhibition of mushroom tyrosinase activity .
|
-
- HY-15846
-
-
- HY-122786
-
|
|
Antibiotic
HIV
|
Infection
|
|
3-O-Methylviridicatin is an indole alkaloid. 3-O-Methylviridicatin inhibits TNF-alpha induced HIV replication with an IC50 of 2.5 μM .
|
-
- HY-N0629
-
-
- HY-109040
-
|
VT-1129
|
Fungal
Cytochrome P450
|
Infection
|
|
Quilseconazole (VT-1129) is a potent, orally active fungal Cyp51 (lanosterol 14-α-demethylase) inhibitor, binds tightly to cryptococcal CYP51, but weakly inhibits humans CYP450 enzymes .
|
-
- HY-103267A
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
S32826 is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 inhibits LPA release from adipocytes .
|
-
- HY-160930
-
|
|
p38 MAPK
Src
Syk
|
Inflammation/Immunology
|
|
TOP1288 is a narrow spectrum kinase inhibitor for P38α, Src and Syk kinase, with IC50 of 116nM, 24nM and 659nM, respectively. TOP1288 inhibits inflammatory cytokine release from inflamed biopsies and myofibroblasts .
|
-
- HY-N10002
-
|
|
Phosphatase
Glycosidase
|
Metabolic Disease
|
|
Caffeoyltryptophan is a competitive PTP1B inhibitor, with an IC50 of 16.99 μM. Caffeoyltryptophan can also inhibit α-glucosidase, linoleic acid peroxidation and haemolysis. Caffeoyltryptophan can be used for the research of type 2 diabetes .
|
-
- HY-171780
-
-
- HY-112456
-
|
|
IKK
|
Inflammation/Immunology
|
|
IKK2-IN-4 (compound 4) is a potent IKK-2 inhibitor, with an IC50 of 25 nM. IKK2-IN-4 can inhibit the LPS-induced production of TNFα in PBMCs .
|
-
- HY-126026
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-17 (Zinc5) is a NF-κB inhibitor. NF-κB-IN-17 inhibits TNF-α-induced NF-κB DNA binding activity in C2C12 cells .
|
-
- HY-12338
-
|
|
PI3K
Bcr-Abl
|
Cancer
|
|
ON 146040 is a potent PI3Kα and PI3Kδ (IC50≈14 and 20 nM, respectively) inhibitor. ON 146040 also inhibits Abl1 (IC50<150 nM).
|
-
- HY-12085
-
-
- HY-P10426
-
|
|
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
cyclo(CLLFVY) is an inhibitor for hypoxia inducible factor-1 (HIF-1), with IC50 of 19 μM (in U2OS) and 16 μM (in MCF-7). cyclo(CLLFVY) binds to the PAS-B domain of HIF-1α, inhibits HIF-1 dimerization and transcriptional activity. cyclo(CLLFVY) downregulates the expression of hypoxia response genes, such as VEGF and CAIX, exhibits antitumor against the HIF-1 associated cancers .
|
-
- HY-P1847
-
|
|
NF-κB
|
Cancer
|
|
IKKγ NBD Inhibitory Peptide is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits .
|
-
- HY-P0097A
-
|
Melanostatine-5 acetate salt
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5) acetate salt, a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 acetate salt is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 acetate salt inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-123936
-
|
|
NF-κB
IKK
|
Neurological Disease
Inflammation/Immunology
|
|
SR12343, an IKK/NF-κB inhibitor, is a NF-κB essential modulator (NEMO)-binding domain (NBD) mimetic. SR12343 inhibits TNF-α- and LPS-induced NF-κB activation by blocking the interaction between IKKβ and NEMO, with an IC50 of 37.02 μM for TNF-α-mediated NF-κB activation. SR12343 suppresses LPS-induced acute pulmonary inflammation in mice. SR12343 can be used for research of inflammatory and degenerative diseases .
|
-
- HY-N2199
-
|
|
Apoptosis
Autophagy
|
Cancer
|
|
Sotetsuflavone is a flavonoid that can be isolated from Cycas revolute. Sotetsuflavone inhibits migration and invasion of A549 cells by reversing EMT, and induces cell apoptosis and autophagy. Sotetsuflavone inhibits HIF-1α, VEGF, angiostatin, MMP-9, and MMP-13 expression in A549 cells. Sotetsuflavone also protects mice against Crohn's disease (CD)-like colitis. Sotetsuflavone can be used for research of NSCLC .
|
-
- HY-120475
-
|
ATH434
|
α-synuclein
|
Neurological Disease
|
|
PBT434 is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 has the potential for the research of Parkinson’s disease (PD) .
|
-
- HY-101562
-
|
GDC-0077; RG6114
|
PI3K
Apoptosis
|
Cancer
|
|
Inavolisib (GDC-0077) is a potent, orally active, and selective PI3Kα inhibitor (IC50=0.038 nM). Inavolisib exerts its activity by binding to the ATP binding site of PI3K, thereby inhibiting the phosphorylation of PIP2 to PIP3. Inavolisib is more selective for mutant versus wild-type PI3Kα. Inavolisib can be used for the study of breast cancer .
|
-
- HY-B0193A
-
|
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
|
-
- HY-B0723
-
|
FC-1271a
|
Estrogen Receptor/ERR
Caspase
|
Neurological Disease
Endocrinology
Cancer
|
|
Ospemifene (FC-1271a) is an orally active and non-estrogenic selective estrogen receptor modulator (SERM) with Ki values of 380 and 410 nM for estrogen receptor α (ERα) and ERβ, respectively. Ospemifene inhibits caspase-3 activity. Ospemifene inhibits neuronal degeneration, prevents bone loss, and increases vaginal weight and vaginal epithelial height. Ospemifene has anticancer activity against breast cancer .
|
-
- HY-P0097
-
|
Melanostatine-5
|
Melanocortin Receptor
|
Metabolic Disease
Endocrinology
Cancer
|
|
Nonapeptide-1 (Melanostatine-5), a peptide hormone, is a selective antagonist of MC1R (Ki: 40 nM). Nonapeptide-1 is a competitive α-MSH antagonist that potently inhibits intracellular cAMP and melanosome dispersion induced by α-MSH in melanocytes (IC50: 2.5 nM and 11 nM, respectively). Nonapeptide-1 inhibits melanin synthesis, and can be used in the research of skin pigmentation and regulation of steroid production in the adrenal gland, skin cancer .
|
-
- HY-18862
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
PF-03715455 is a potent inhaled p38 MAPK inhibitor. PF-03715455 shows some selectivity for p38α over p38β with respective IC50 values of 0.88 and 23 nM. PF-03715455 potently inhibits LPS-induced TNFα production in human whole blood (IC50=1.7 nM). PF-03715455 has potential for the treatment of COPD (chronic obstructive pulmonary disease) .
|
-
- HY-W013500
-
|
alpha-Nitrostilbene; α-Nitrostilbene; NSC 385
|
Histone Methyltransferase
|
Others
|
|
(1-Nitroethene-1,2-diyl)dibenzene (alpha-Nitrostilbene; α-Nitrostilbene) is an inhibitor of protein arginine methyltransferase 1 (PRMT1; IC50=11 μM in histone H4 methylation assay). It also inhibits histone H4 methylation by PRMT8, but not histone H3.1 methylation by CARM1 or Set7/9, at concentrations of 10 and 100 μM.
|
-
- HY-N11996
-
|
|
NO Synthase
NF-κB
|
Others
|
|
Aloenin aglycone (compound 13) is an NF-κB inhibitor that can be isolated from aloe exudate. Aloenin aglycone inhibits TNFα-induced NF-κB transcriptional activity (IC50: 18.7 μM). Aloenin aglycone (10 μM) also reduced inducible nitric oxide synthase (iNOS) and intercellular adhesion molecule 1 (ICAM-1) gene expression after treatment of HepG2 cells with 10 ng/mL TNFα .
|
-
- HY-W613220
-
-
- HY-162316
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-15 (compound 14r) is a potent NF-κB inhibitor. NF-κB-IN-15 decreases the NO levels and inhibits the release of IL-6, TNF-α, and IL-1β in LPS (HY-D1056) -induced cells. NF-κB-IN-15 inhibits LPS-induced phosphorylation of p65 and degradation of IκBα. NF-κB-IN-15 shows anti-inflammatory activity has the potential for the research of acute lung injury (ALI) .
|
-
- HY-108642B
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 dihydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 dihydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 dihydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
- HY-108642
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG 548 is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
- HY-108642A
-
|
|
p38 MAPK
Casein Kinase
|
Inflammation/Immunology
|
|
AMG-548 hydrochloride, an orally active and selective p38α inhibitor (Ki=0.5 nM), shows slightly selective over p38β (Ki=36 nM) and >1000 fold selective against p38γ and p38δ. AMG-548 hydrochloride is also extremely potent in the inhibition of whole blood LPS stimulated TNFα (IC50=3 nM) . AMG-548 hydrochloride inhibits Wnt signaling by directly inhibiting Casein kinase 1 isoforms δ and ε .
|
-
- HY-12707
-
-
- HY-B0661
-
|
(R)-(-)-YM12617 free base; LY253351 free base
|
Adrenergic Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin induces Apoptosis. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .
|
-
- HY-124242
-
|
|
Drug Derivative
|
Cancer
|
|
(S)-α-Methylbenzyl ricinoleamide (compound (R,S)-3d) is a fatty acid amide. (S)-α-Methylbenzyl ricinoleamide shows antiproliferative activity, inhibits the growth of human ovarian cancer cells NCI-ADR/RES and glioma cells U251 with GI50s of 1.9 μg/mL and 3.6 μg/mL, respectively .
|
-
- HY-12707A
-
-
- HY-N13177
-
|
|
Others
|
Inflammation/Immunology
|
|
25(S)Ruscogenin 3-O-α-L-rhamnopyranoside is from the fibrous roots of Ophiopogon japonicus and Liriope spicata var. prolifera. 25(S)Ruscogenin 3-O-α-L-rhamnopyranoside exhibits anti-inflammatory activity by inhibiting neutrophil responses to PMA (HY-18739), with an IC50 value of 1.13 μM .
|
-
- HY-12707B
-
-
- HY-148016
-
|
|
Protease Activated Receptor (PAR)
ERK
|
Inflammation/Immunology
|
|
I-287 is a orally active selective PAR2 inhibitor that acting as a negative allosteric regulator on Gαq and Gα12/13 activity and their downstream effectors. I-287 reduces Complete Freund's adjuvant (HY-153808)-induced inflammation in mice and can be used for inflammation/immunology research .
|
-
- HY-W153897
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
N-Methyltyramine is a protoalkaloid that can be isolated from various plant species. N-Methyltyramine is an α2-adrenoreceptor antagonist. N-Methyltyramine enhances appetite and digestion of foods by stimulating gastrin and pancreatic secretions. N-Methyltyramine can relax mouse small intestinal smooth muscle and inhibits small intestinal propulsion .
|
-
- HY-153091
-
|
|
Adrenergic Receptor
5-HT Receptor
Sigma Receptor
|
Neurological Disease
|
|
BMY 14802 is a sigma-1 receptor (σ1R) antagonist, as well as an agonist at serotonin (5-HT) 1A and adrenergic alpha-1 receptors. BMY 14802 inhibits abnormal involuntary movement (AIM) in rat Parkinson's disease (PD) model, with down-regulating the expression of AIM .
|
-
- HY-B0661A
-
|
(R)-(-)-YM12617; LY253351
|
Adrenergic Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .
|
-
- HY-12707C
-
-
- HY-14282A
-
|
|
Fungal
|
Infection
Inflammation/Immunology
|
|
(Z)-Lanoconazole is the Z configuration of Lanoconazole. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
|
-
- HY-15205
-
|
STA-9090
|
HSP
Apoptosis
|
Cancer
|
|
Ganetespib (STA-9090) is a heat shock protein 90 (HSP90) inhibitor which exhibits potent cytotoxicity in a wide variety of hematological and solid tumor cell lines. Ganetespib has antiangiogenic effects in colorectal cancer mediated through inhibition of HIF-1α and STAT3 .
|
-
- HY-32337
-
|
1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3
|
VD/VDR
Interleukin Related
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Tacalcitol (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) can promote normal bone growth by regulating calcium ions. Tacalcitol inhibits cancer cell proliferation and migration. Tacalcitol can be used in the research of inflammation, cancer, and skin diseases .
|
-
- HY-14649
-
|
Vitamin A acid; all-trans-Retinoic acid; ATRA
|
Organoid
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-P5038
-
|
c(GRGDSP)
|
Integrin
|
Cancer
|
|
Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) (c(GRGDSP)) is an RGD-containing inhibitory peptide. Cyclo(Gly-Arg-Gly-Asp-Ser-Pro) is a synthetic α5β1 integrin ligand that competitively inhibits the binding of invasin (Inv) to α5β1 integrin expressed on Caco-2 cells .
|
-
- HY-14649S3
-
|
Vitamin A acid-d6; all-trans-Retinoic acid-d6; ATRA-d6
|
Isotope-Labeled Compounds
RAR/RXR
PPAR
Autophagy
Endogenous Metabolite
|
Cancer
|
|
Retinoic acid-d6 is the deuterium labeled Retinoic acid[1]. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha[2][3][4][5][6][7].
|
-
- HY-N0787
-
|
4-Caffeoylquinic acid; 4-O-Caffeoylquinic acid
|
Endogenous Metabolite
NF-κB
Keap1-Nrf2
mTOR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
Cryptochlorogenic acid (4-Caffeoylquinic acid) is a naturally occurring phenolic acid compound with oral effectiveness, anti-inflammatory, antioxidant and anti-cardiac hypertrophy effects. Alleviating LPS (HY-D1056) and ISO (HY-B0468) by regulating proinflammatory factor expression, inhibiting NF-κB activity, promoting Nrf2 nuclear transfer, and regulating PI3Kα/Akt/ mTOR / HIF-1α signaling pathway Induced physiological stress response .
|
-
- HY-N6969A
-
|
|
Adrenergic Receptor
|
Cancer
|
|
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
|
-
- HY-N0234
-
|
7-O-Methylbavachin; Bavachinin A
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
Cancer
|
|
Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
|
-
- HY-126031
-
|
|
DAGL
|
Others
|
|
(R)-KT109 is a highly potent inhibitor of diacylglycerol lipase β (DAGLβ) with an IC50 of 0.79 nM and effectively blocks DAGLα-mediated hydrolysis of 1-stearoyl-2-arachidonoyl-sn-glycerol. Additionally, it demonstrates inhibitory activity against α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 of 2.51 nM, exhibiting greater potency for DAGLβ, DAGLα, and ABHD6 compared to its (S) isomer, (S)-KT109.
|
-
- HY-10255A
-
|
SU 11248
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-122858
-
|
|
PKC
|
Cancer
|
|
PKCiota-IN-2 (Compound 49) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively .
|
-
- HY-30235A
-
|
|
PGE synthase
Bacterial
TNF Receptor
|
Inflammation/Immunology
Cancer
|
|
Benzydamine hydrochloride is an orally administered prostaglandin synthesis inhibitor that has anti-inflammatory, analgesic, antipyretic, and antibacterial properties. Benzydamine hydrochloride can inhibit TNF-α, stabilize cell membranes, and reduce oxidative stress within cells .
|
-
- HY-P10704
-
|
|
Integrin
|
Cancer
|
|
C16Y is a short peptide and an inhibitor of integrins αvβ3 and α5β1. C16Y acts on the cell membrane and exerts its anticancer activity by inhibiting angiogenesis .
|
-
- HY-155459
-
|
|
Microtubule/Tubulin
Mitosis
|
Cancer
|
|
Tubulin polymerization-IN-57 (compound 5a) is a tubulin inhibitor and is an α-naphthoxy-substituted carbendazim (HY-13582) derivative. Tubulin polymerization-IN-57 induces mitotic arrest and inhibits cancer cell proliferation .
|
-
- HY-164515
-
|
|
Apoptosis
|
Cancer
|
|
ONC213 is an αKGDH inhibitor that suppresses mitochondrial respiration and elevates α-ketoglutarate levels by inhibiting αKGDH activity, leading to apoptosis (Apoptosis) in AML cells. ONC213 can be used in acute myeloid leukemia research .
|
-
- HY-30235
-
|
|
PGE synthase
TNF Receptor
Bacterial
|
Inflammation/Immunology
Cancer
|
|
Benzydamine is an orally administered prostaglandin synthesis inhibitor that has anti-inflammatory, analgesic, antipyretic, and antibacterial properties. Benzydamine can inhibit TNF-α, stabilize cell membranes, and reduce oxidative stress within cells .
|
-
- HY-122857
-
|
|
PKC
|
Cancer
|
|
PKCiota-IN-1 (compound 51) is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.7 nM. PKCiota-IN-1 also inhibits PKC-α and PKC-ε with IC50s of 45 nM and 450 nM, respectively .
|
-
- HY-122858A
-
|
|
PKC
|
Cancer
|
|
PKCiota-IN-2 formic is a potent PKCiota (PKC-ι) inhibitor with an IC50 of 2.8 nM. PKCiota-IN-2 formic also inhibits PKC-α and PKC-ε with IC50s of 71 nM and 350 nM, respectively .
|
-
- HY-115738
-
-
- HY-136644
-
|
|
Calcium Channel
|
Others
|
|
PD-217014-methyl ester is an α?δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity, and its anti-hyperalgesic effect is dose-dependent.
|
-
- HY-111630
-
|
|
Topoisomerase
|
Cancer
|
|
PluriSIn #2 is a selective transcriptional inhibitor of topoisomerase II α (TOP2A). PluriSIn #2 is a compound that selectively eliminates undifferentiated human pluripotent stem cells (hPSCs) .
|
-
- HY-19570A
-
|
S-(1,2-Dichlorovinyl)-L-cysteine hydrochloride
|
TNF Receptor
Drug Metabolite
|
Inflammation/Immunology
|
|
NSC 15830 (S-(1,2-Dichlorovinyl)-L-cysteine) hydrochloride is a nephrotoxin and metabolite of trichloroethylene. NSC 15830 hydrochloride inhibits pathogen-stimulated TNF-α .
|
-
- HY-161074
-
|
|
FAP
|
Cancer
|
|
PNT6555 is a fibroblast activation protein-α (FAP) inhibitor. PNT6555 has antitumor activity. PNT6555 can be used for imaging of FAP-positive tumors .
|
-
- HY-N1218
-
|
|
Glycosidase
Bcl-2 Family
|
Others
|
|
Stellasterol is a natural product. Stellasterol has high affinity towards Bcl-2 protein (Ki: 118.05 nM). Stellasterol is a weak α-glucosidase inhibitor .
|
-
- HY-10215
-
|
VER-52296; AUY922; NVP-AUY922
|
HSP
Autophagy
Apoptosis
|
Cancer
|
|
Luminespib (VER-52296) is a potent HSP90 inhibitor with IC50s of 7.8 and 21 nM for HSP90α and HSP90β, respectively .
|
-
- HY-19776
-
|
|
Phosphatase
|
Cancer
|
|
3α-Aminocholestane is a selective SH2 domain-containing inositol-5′-phosphatase 1 (SHIP1) inhibitor with an IC50 of ~2.5 μM.
|
-
- HY-W142119
-
|
|
Ser/Thr Protease
|
Neurological Disease
|
|
α-Methyl-DL-aspartic acid is a specific inhibitor of argininosuccinate synthase (ASS), and also is the rate-limiting enzyme for the recycling of 1-citrulline to 1-arginine .
|
-
- HY-12825
-
-
- HY-14316A
-
|
Ebanicline dihydrochloride; ABT-594 dihydrochloride
|
nAChR
|
Neurological Disease
|
|
Tebanicline dihydrochloride (Ebanicline dihydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. It inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
|
-
- HY-136644A
-
|
|
Calcium Channel
|
Others
|
|
PD-217014 is an α2δ ligand with visceral analgesic activity and can inhibit visceral hypersensitivity reactions. Its anti-allodynic effect is dose-dependent.
|
-
- HY-173001
-
|
|
Topoisomerase
|
Cancer
|
|
AuL1 is an inhibitor of topoisomerase IIα (Top II) with DNA-intercalating properties. AuL1 is cytotoxic to tumor cells and can be used in the research of anticancer agents .
|
-
- HY-118819
-
-
- HY-124339
-
-
- HY-W086896
-
-
- HY-14974
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
R 1487 is an orally active and highly selective p38α mitogen-activated protein kinase inhibitor. R 1487 can be used in the study of rheumatoid arthritis .
|
-
- HY-121944
-
|
|
Casein Kinase
Wnt
|
Others
|
|
Ricinine exhibits hepatoprotection in CCl4-induced liver damage. Ricinine is also a CK1α inhibitor, and may activate Wnt pathway .
|
-
- HY-N7637
-
|
|
Apoptosis
|
Cancer
|
|
Tubuloside B, one of the phenylethanoids isolated from the stems of Cistanche salsa, inhibits TNFα-induced apoptosis. Tubuloside B possesses antioxidative effects .
|
-
- HY-B2006
-
|
|
Phosphatase
Bacterial
|
Infection
|
|
Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide .
|
-
- HY-13743
-
|
Linomide; FCF89; ABR212616
|
TNF Receptor
|
Inflammation/Immunology
|
|
Roquinimex (Linomide; PNU212616; ABR212616) is a quinoline derivative immunostimulant which increases NK cell activity and macrophage cytotoxicity; inhibits angiogenesis and reduces the secretion of TNF alpha.
|
-
- HY-B0661S
-
-
- HY-N12688
-
|
|
Glycosidase
Amylases
|
Metabolic Disease
|
|
2,3-Dihydrocalodenin B (Compound 6) is a compound that can be isolated from Knema globularia. 2,3-Dihydrocalodenin B is a potent and non-competitive inhibitor against α-glucosidase and α-amylase, with IC50 values of 1.1 and 2.6 μM, respectively. 2,3-Dihydrocalodenin B can be used for the research of diabetes .
|
-
- HY-N2425
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
|
-
- HY-145275
-
|
|
Glycosidase
|
Infection
|
|
EB-0176 is a potent inhibitor of ER α-glucosidases (α-Glu) Iand II with IC50s of 0.6439 and 0.0011 μM, respectively. EB-0176 is a N-substituted derivative of valiolamine with broad-spectrum antiviral. EB-0176 has the potential for the reseach of broad-spectrum agent against the existing and emerging viruses .
|
-
- HY-155961
-
-
- HY-N7170
-
|
|
Glycosidase
|
Metabolic Disease
|
|
(-)-6β-Hydroxy-5β,8β,9β,10α-cleroda-3,13-dien-16,15-olid-18-oic acid (compound 4) is a α-Glucosidase inhibitor with an IC50 value of 577.7 µM .
|
-
- HY-12987S
-
-
- HY-125838
-
|
|
JNK
|
Neurological Disease
|
|
J30-8 is a potent and isoform-selective inhibitor of c-Jun N-terminal kinase 3 (JNK3) with an IC50 of 40 nM, which 2500-fold isoform selectivity against JNK1α1 and JNK2α2. J30-8 exhibits neuroprotective activity in vitro and potential for the treatment of neurodegenerative diseases .
|
-
- HY-163766
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Antiproliferative agent-51 (Compound 18h) exhibits inhibitory efficacy against estrogen receptor α (ERα) mediated transcription, with an IC50 of 1.6 nM. Antiproliferative agent-51 inhibits the proliferation of cancer cell ZR-75, with an IC50 of 0.031 μM. Antiproliferative agent-51 exhibits antitumor efficacy in mouse models .
|
-
- HY-P10600A
-
|
|
Ras
|
Others
|
|
BIMAX2 acetate is a high affinity nuclear localization signal (NLS) peptide. BIMAX2 acetate can mimic the activity of the classical nuclear localization signal (cNLS) and competitively bind to importin α, thereby inhibiting the binding of cNLS-cargo proteins to importin α. BIMAX2 acetate can be used to study the role of RBBP4 in regulating nuclear import efficiency and cell senescence .
|
-
- HY-12987R
-
|
R6238 (Standard)
|
Dopamine Receptor
Adrenergic Receptor
STAT
Parasite
|
Neurological Disease
Endocrinology
Cancer
|
|
Pimozide (Standard) is the analytical standard of Pimozide. This product is intended for research and analytical applications. Pimozide is a dopamine receptor antagonist, with Kis of 1.4 nM, 2.5 nM and 588 nM for dopamine D2, D3 and D1 receptors, respectively, and also has affinity at α1-adrenoceptor, with a Ki of 39 nM; Pimozide also inhibits STAT3 and STAT5.
|
-
- HY-N0613R
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Sauchinone (Standard) is the analytical standard of Sauchinone. This product is intended for research and analytical applications. 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-P10600
-
|
|
Ras
|
Others
|
|
BIMAX2 is a high affinity nuclear localization signal (NLS) peptide. BIMAX2 can mimic the activity of the classical nuclear localization signal (cNLS) and competitively bind to importin α, thereby inhibiting the binding of cNLS-cargo proteins to importin α. BIMAX2 can be used to study the role of RBBP4 in regulating nuclear import efficiency and cell senescence .
|
-
- HY-120300
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
UCM710 is an endocannabinoid (eCB) hydrolysis inhibitor that increases the levels of N-arachidonoyl ethanolamine and 2-arachidonoylglycerol in neurons. UCM710 inhibits fatty acid amide hydrolase and α/β-hydrolase domain 6, but not monoacylglycerol lipase .
|
-
- HY-135590
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 4-Monomethyl Ether (Compound 37) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 1 μM and a pIC50 of 6 .
|
-
- HY-135584
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Raloxifene 6-Monomethyl Ether (Compound 7) is a Raloxifene derivative that inhibits estrogen receptor α. Raloxifene 4-Monomethyl Ether inhibits MCF-7 cells with an IC50 of 250 nM and a pIC50 of 6.6 .
|
-
- HY-121638
-
|
|
Apoptosis
DGK
|
Inflammation/Immunology
Cancer
|
|
CU-3 is the racemate of (5Z,2E)-CU-3. (5Z,2E)-CU-3 is a potent and selective inhibitor against the α-isozyme of DGK with an IC50 value of 0.6 μM, competitively inhibits the affinity of DGKα for ATP with a Km value of 0.48 mM. (5Z,2E)-CU-3 targets the catalytic region, but not the regulatory region of DGKα. (5Z,2E)-CU-3 has antitumoral and proimmunogenic effects, enhances the apoptosis of cancer cells and the activation of T cells .
|
-
- HY-N12500
-
|
|
Glycosidase
|
Others
|
|
1'-O-Methyl neochebulinate, hydrolyzable tannin, is an α-glucosidase inhibitor with IC50 value of 59.5 μM, isolated from the fruits of Terminalia chebula Retz .
|
-
- HY-N0014
-
-
- HY-148231
-
-
- HY-11105
-
|
XL147 analogue
|
PI3K
Apoptosis
|
Cancer
|
|
Pilaralisib analogue (XL147 analogue) is a representative and selective PI3Kα inhibitor extracted from patent WO2012006552A1, Compound 147 in Table 1.
|
-
- HY-145564A
-
|
PF-07265803 hydrochloride
|
p38 MAPK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Emprumapimod (PF-07265803) hydrochloride is an orally active and selective inhibitor of p38α MAPK. Emprumapimod hydrochloride can be used for the research of dilated cardiomyopathy and acute inflammatory pain .
|
-
- HY-121811
-
-
- HY-12869
-
|
|
PI3K
|
Cancer
|
|
AZD8835 is a potent and selective inhibitor of PI3Kα and PI3Kδ with IC50s of 6.2 and 5.7 nM, respectively.
|
-
- HY-117771
-
DO34
2 Publications Verification
|
DAGL
|
Metabolic Disease
|
|
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.
|
-
- HY-14316B
-
|
Ebanicline hydrochloride; ABT-594 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Tebanicline hydrochloride (Ebanicline hydrochloride) is a nAChR modulator with potent, orally effective analgesic activity. Tebanicline hydrochloride inhibits the binding of cytisine to α4β2 neuronal nAChRs with a Ki of 37 pM .
|
-
- HY-147045
-
-
- HY-13689
-
|
Gö 6983; Goe 6983
|
PKC
|
Cancer
|
|
Go 6983 is a pan-PKC inhibitor against for PKCα, PKCβ, PKCγ, PKCδ and PKCζ with IC50 of 7 nM, 7 nM, 6 nM, 10 nM and 60 nM, respectively.
|
-
- HY-12340
-
|
|
PI3K
|
Cancer
|
|
ETP-46321 is a potent and orally bioavailable PI3Kα and PI3Kδ inhibitor with Kiapps of 2.3 and 14.2 nM, respectively.
|
-
- HY-N2270
-
|
|
p38 MAPK
ERK
IKK
|
Inflammation/Immunology
|
|
Chicanine is a lignan compound of Schisandra chinesis, inhibits LPS-induced phosphorylation of p38 MAPK, ERK 1/2 and IκB-α, with anti-inflammatory activity .
|
-
- HY-N1200
-
|
|
5 alpha Reductase
|
Inflammation/Immunology
|
|
Stigmasterol glucoside is a sterol isolated from P. urinaria with high antioxidant and anti-inflammatory activities , act as an inhibitor of 5α-reductase with an IC50 of 27.2 µM .
|
-
- HY-19708
-
-
- HY-12437
-
|
|
ROCK
|
Cancer
|
|
BDP5290 is a potent inhibitor of both ROCK and MRCK with IC50s of 5 nM, 50 nM, 10 nM and 100 nM for ROCK1, ROCK2, MRCKα and MRCKβ, respectively.
|
-
- HY-150601
-
-
- HY-124552
-
|
|
DNA/RNA Synthesis
Topoisomerase
|
Others
|
|
Epolactaene is a potent Topoisomerase II and DNA Polymerase inhibitor with IC50 values of 10, 25, 94 µM for Topoisomerase II, DNA Polymerase α, DNA Polymerase β, respectively .
|
-
- HY-163102
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
IA-14069 is a TNF-alpha inhibitor that exhibits anti-inflammatory properties while also influencing the production of pro-inflammatory cytokines, making it a valuable tool in colon cancer research.
|
-
- HY-B1111
-
-
- HY-13469
-
|
CUDC-305
|
HSP
|
Cancer
|
|
Debio 0932 (CUDC-305) is an orally active HSP90 inhibitor, with IC50s of 100 and 103 nM for HSP90α and HSP90β, respectively .
|
-
- HY-P10354
-
-
- HY-110193
-
SPP-86
2 Publications Verification
|
RET
|
Cancer
|
|
SPP-86 is a potent and selective cell permeable inhibitor of RET tyrosine kinase, with an IC50 of 8 nM. SPP-86 inhibits RET-induced phosphatidylinositide 3-kinases (PI3K)/Akt and MAPK signaling, also inhibits RET-induced estrogen receptorα (ERα) phosphorylation in MCF7 cells . SPP-86 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-158098
-
|
|
FGFR
|
Metabolic Disease
|
|
FGFR1 inhibitor-11 (compound 5g) binds to FGFR1, inactivation of its downstream ERK1/2 and IκBα/NF-κB signaling inhibited RANKL-induced osteoclastogenesis. FGFR1 inhibitor-11 has oral bioactivity .
|
-
- HY-100886
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth .
|
-
- HY-N7821
-
|
Aphidicolin 17-monoacetate
|
DNA/RNA Synthesis
|
Cancer
|
|
Aphidicolin 17-acetate is a selective eukaryotic DNA polymerase α inhibitor. Aphidicolin 17-acetate does not inhibit DNA polymerase β and γ. Aphidicolin 17-acetate markedly inhibits the in vivo DNA synthesis of sea urchin embryos and HeLa cells but not RNA and protein syntheses .
|
-
- HY-A0066AR
-
|
Imidaline hydrochloride (Standard); NSC35110 hydrochloride (Standard)
|
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Tolazoline (hydrochloride) (Standard) is the analytical standard of Tolazoline hydrochloride (HY-A0066A). This product is intended for research and analytical applications. Tolazoline hydrochloride (Imidaline hydrochloride) is an α-adrenergic receptor antagonist. Tolazoline hydrochloride inhibits Noradrenaline (HY-13715)-induced cell contraction, modulates vascular resistance, increases arterial pressure, and reverses bradycardia and tachypnea. Tolazoline hydrochloride can be used to study erectile dysfunction, α2-adrenergic receptor agonist-related poisoning, and skin vascular disease research .
|
-
- HY-159798
-
|
|
PROTACs
p38 MAPK
|
Cancer
|
|
NR-11c is a selective and potent p38α PROTAC degrader. NR-11c effectively degrades p38α in a variety of tumor cells. When administered intraperitoneally or intravenously to mice, NR-11c primarily acts in the liver. NR-11c can be used in cancer research. (Pink: p38α inhibitor 5 (HY-159799); Black: linker (HY-159800); Blue: VHL E3 ligase ligand (HY-112078)) .
|
-
- HY-135783
-
AT 1001
1 Publications Verification
|
nAChR
|
Neurological Disease
|
|
AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
|
-
- HY-P990090
-
|
CBP-201
|
Interleukin Related
|
Inflammation/Immunology
|
|
Rademikibart (CBP-201) is a human monoclonal antibody targeting IL-4Rα with a KD of 20.7 pM when binding to human IL-4Rα epitopes. Rademikibart does not bind to IL-4Rα from other species. Rademikibart inhibits IL-4 and IL-13-mediated STAT6 signaling, TF-1 cell proliferation and TARC production in PBMCs. Rademikibart has the potential for moderate-to-severe Th2 inflammatory diseases research .
|
-
- HY-N3602A
-
|
Rengyolone
|
TNF Receptor
NF-κB
NO Synthase
|
Inflammation/Immunology
|
|
rel-Cleroindicin F (Rengyolone) is a cyclohexyl acetyl compound that can be isolated from the fruit of forsythia and has anti-inflammatory activity. It strongly inhibits the production of nitric oxide (NO) and tumor necrosis factor-alpha (TNF-α). rel-Cleroindicin F does this by downregulating the activity of NF-κB and NF-κB kinases in RAW 264.7 cells stimulated by LPS (HY-D1056), thus inhibiting the expression of inducible nitric oxide synthase (NO Synthase) and nitric oxide production .
|
-
- HY-W009783
-
|
|
HIV
Influenza Virus
|
Infection
Cancer
|
|
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. 1-Deoxymannojirimycin hydrochloride has antiviral activity against HIV‐1 strains . 1-Deoxymannojirimycin hydrochloride increases high mannose structures. 1-Deoxymannojirimycin hydrochloride can be used for the study of liver cancer and colon cancer .
|
-
- HY-171279
-
|
|
p38 MAPK
Casein Kinase
Apoptosis
|
Inflammation/Immunology
|
|
Casein kinase 1δ-IN-29 (Compound 18) is the inhibitor for p38α and casein kinase 1 that inhibits p38α, CK1δ and CK1ε with IC50 of 0.041 µM, 0.005 µM and 0.447 µM, respectively. Casein kinase 1δ-IN-29 arrests cell cycle at subG1 phase, induces apoptosis in cell AC1-M88 .
|
-
- HY-161595
-
|
|
CDK
GSK-3
|
Cancer
|
|
CDK5-IN-4 (compound 4) is a potent multikinase type-II inhibitor targeting CDK5, with an IC50 of 9.8 μM. CDK5-IN-4 also inhibits GSK-3α, GSK-3β, CDK9, and CDK2, with IC50 values of 0.98, 4.00, 1.76, and 6.24 μM, respectively. CDK5-IN-4 can be used for glioblastoma research .
|
-
- HY-10320
-
|
BIRB 796
|
p38 MAPK
Raf
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Doramapimod (BIRB 796) is an orally active, highly potent p38 MAPK inhibitor, which has an IC50 for p38α=38 nM, for p38β=65 nM, for p38γ=200 nM, and for p38δ=520 nM. Doramapimod has picomolar affinity for p38 kinase (Kd=0.1 nM). Doramapimod also inhibits B-Raf with an IC50 of 83 nM .
|
-
- HY-17412A
-
-
- HY-159884
-
|
|
Tim3
TNF Receptor
IFNAR
|
Cancer
|
|
MG-T-19 is an effective TIM-3 inhibitor that can suppress the interaction of TIM-3 with PtdSer, CEACAM1, and Gal-9. MG-T-19 can increase the production of tumor necrosis factor-α (TNF-α) and interferon-γ (IFN-γ) in peripheral blood mononuclear cells (PBMCs) from healthy donors, and enhance the ability of PBMCs to inhibit the proliferation of Kasumi-1 cells (an acute myelogenous leukemia cell line) .
|
-
- HY-B0223R
-
|
|
Parasite
Microtubule/Tubulin
Autophagy
Apoptosis
Reactive Oxygen Species
VEGFR
HIF/HIF Prolyl-Hydroxylase
Antibiotic
Bacterial
|
Infection
Cancer
|
|
Albendazole (Standard) is the analytical standard of Albendazole. This product is intended for research and analytical applications. Albendazole (SKF-62979) is an orally active and broad-spectrum parasiticide with high effectiveness and low host toxicity, is used for the research of gastrointestinal parasites in humans and animals. Albendazole induces apoptosis and autophagy in cancer cells. Albendazole also inhibits tubulin polymerization and HIF-1α, VEGF expression, has antioxidant activity, and inhibits the glycolytic process in cancer cells .
|
-
- HY-17412
-
-
- HY-120475A
-
|
ATH434 mesylate
|
α-synuclein
|
Neurological Disease
|
|
PBT434 methanesulfonate is a potent, orally active and cross the blood-brain barrier α-synuclein aggregation inhibitor. PBT434 methanesulfonate can be used as a iron chelator and modulates transcellular iron trafficking. PBT434 methanesulfonate inhibits iron-mediated redox activity and iron-mediated aggregation of α-synuclein. PBT434 methanesulfonate prevents the loss of substantia nigra pars compacta neurons (SNpc). PBT434 methanesulfonate has the potential for the research of Parkinson’s disease (PD) .
|
-
- HY-N13157
-
|
|
P-glycoprotein
|
Cancer
|
|
11α-O-Benzoyl-12β-O-acetyltenacigenin B is a P-glycoprotein (Pgp) inhibitor derived from Marsdenia tenacissima and belongs to the Tenacigenin B (HY-N1168) derivatives. 11α-O-Benzoyl-12β-O-acetyltenacigenin B can inhibit multidrug resistance (MDR) caused by P-glycoprotein (Pgp) overexpression in HepG2/Dox cells and holds potential for research in the field of cancer .
|
-
- HY-P1847A
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
IKKγ NBD Inhibitory Peptide TFA is a highly specific inhibitor NF-κB inhibitor. IKKγ NBD Inhibitory Peptide TFA acts by disrupting the interaction between IKKγ/NEMO-binding domain (NBD) with IKKα and IKKβ, thus blocking TNF-α-induced NF-kB activation. IKKγ NBD Inhibitory Peptide TFA could significantly suppresses inflammation and ameliorate the cerebral ischemia-induced neurological deficits .
|
-
- HY-103109
-
|
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-B2169
-
|
|
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-157125
-
|
|
PI3K
Apoptosis
|
Cancer
|
|
PI3Kα-IN-14 (compound F8) is a selective PI3Kα inhibitor with an IC50 of 0.14 nM. PI3Kα-IN-14 induces a great decrease in mitochondrial membrane which caused cell cycle arrest at G1 phase and apoptosis in U87-MG cells. PI3Kα-IN-14 shows significant anti-proliferative activities against three tumor-derived cell lines (PC-3: IC50 of 0.28 μM; HCT-116: IC50 of 0.57 μM; and U87-MG: IC50 of 1.37 μM) .
|
-
- HY-12040S
-
|
STA-4783-d2
|
Isotope-Labeled Compounds
Reactive Oxygen Species
Apoptosis
Cuproptosis
|
Cancer
|
|
Elesclomol-d2 (STA-4783-d2) is a deuterium labeled Elesclomol (HY-12040). Elesclomol (STA-4783) is a potent copper ionophore and promotes copper-dependent cell death (cuproptosis). Elesclomol specifically binds ferredoxin 1 (FDX1) α2/α3 helices and β5 strand. Elesclomol inhibits FDX1-mediated Fe-S cluster biosynthesis. Elesclomol is an oxidative stress inducer that induces cancer cell apoptosis. Elesclomol is a reactive oxygen species (ROS) inducer. Elesclomol can be used for Menkes and associated disorders of hereditary copper deficiency research .
|
-
- HY-161150
-
-
- HY-101438
-
-
- HY-162768
-
|
|
HSP
|
Cancer
|
|
Grp94 Inhibitor-2 (compound 23), a cyclopropane analog, exhibits high affinity for glucose-regulated protein 94 (Grp94) with a Kd of 0.48 µM and 0.65 µM for Grp94 and Hsp90α, respectively .
|
-
- HY-103267
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
S32826 disodium is a potent autotaxin inhibitor, with an IC50 of 8.8 nM. S32826 disodium shows similar inhibitory effects at various autotaxin isoforms (α, β and γ). S32826 disodium inhibits LPA release from adipocytes .
|
-
- HY-145274
-
|
|
Glycosidase
|
Infection
|
|
EB-0156 is a potent inhibitor of ER α-glucosidases (α-Glu) Iand II with IC50s of 0.0479 and less than 0.001 μM, respectively. EB-0156 is a N-substituted derivative of valiolamine with broad-spectrum antiviral. EB-0156 has the potential for the reseach of broad-spectrum agent against the existing and emerging viruses .
|
-
- HY-106523
-
|
KT 210; K 351; Hypadil
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Nipradolol (KT-210; K-351) is a potent blocker of alpha-1-adrenergic receptors. Nipradolol inhibits the increase of intraocular pressure (IOP) in an albino rabbit model induced by Phenylephrine (HY-B0769). Nipradolo suppresses the noradrenaline (NA)-induced muscles contraction, also exhibits vasodilator activity on the dog coronary artery .
|
-
- HY-14282R
-
|
|
Fungal
|
Infection
Inflammation/Immunology
|
|
Lanoconazole (Standard) is the analytical standard of Lanoconazole. This product is intended for research and analytical applications. Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi in vitro and in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
|
-
- HY-12987S1
-
-
- HY-12987S2
-
-
- HY-110248
-
|
|
PI4K
HCV
|
Infection
|
|
MI 14 is a selective PI4KIIIβ inhibitor with IC50s of 54 nM, >100 μM, >100 μM for PI4KIIIβ, PI4KIIIα, PI4KIIα, respectively. MI 14 has antiviral activity against HCV 1b, CVB3, HRVM, HVC 2a .
|
-
- HY-N1987
-
|
|
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-144307
-
|
|
Aurora Kinase
PKC
|
Cancer
|
|
Aurora A/PKC-IN-1 (Compound 2e) is a potent dual inhibitor of Aurora A (AurA) and PKC (α, β1, β2, and θ) kinases with IC50s of 6.9 nM and 16.9 nM for AurA and PKCα, respectively. Aurora A/PKC-IN-1 has antiproliferative activity in breast cancer cells and antimetastatic activity .
|
-
- HY-P3567
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
(p-Iodo-Phe7)-ACTH (4-10) is a adrenocorticotrophic hormone (ACTH) derivative, which is produced and secreted by the anterior pituitary gland. (p-Iodo-Phe7)-ACTH (4-10) serves as a melanocortin (MC) receptor antagonist and inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats .
|
-
- HY-123459
-
|
ABT-232; NS-49; PNO-49B
|
Adrenergic Receptor
|
Endocrinology
|
|
Garomefrine hydrochlorid (ABT-232) is an α1A-adrenergic agonist with the potential to inhibit urinary incontinence. Garomefrine hydrochlorid showed the greatest contractility in pig nasal mucosal vessels. The biological activity of Garomefrine hydrochlorid has been shown to give it a competitive advantage compared to other drugs. The potency of Garomefrine hydrochlorid makes it a valuable research object in related research .
|
-
- HY-107531
-
|
|
GSK-3
|
Neurological Disease
Cancer
|
|
A 1070722 is a potent and selective glycogen synthase kinase 3 (GSK-3) inhibitor, with a Ki of 0.6 nM for both GSK-3α and GSK-3β. A 1070722 can penetrate the blood-brain barrier (BBB) and accumulates in brain regions, thus potential for PET radiotracer for the quantification of GSK-3 in brain. A 1070722 decreases spontaneous locomotion .
|
-
- HY-B0942
-
|
|
nAChR
Bacterial
Apoptosis
Caspase
|
Infection
Neurological Disease
Cancer
|
|
Benzethonium chloride inhibits nicotinic acetylcholine receptors in human recombinant α7 and α4β2 neurons in Xenopus laevis oocytes, which has antibacterial, anticancer, antisepsis and disinfection activity. Benzethonium chloride induced Apoptosis and activated caspases in cancer cell lines. Benzethonium chloride ablates the tumor-forming ability of FaDu cells, delays the growth of xenograft tumors in vivo .
|
-
- HY-N1919R
-
|
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-10255
-
|
SU 11248 Malate
|
PDGFR
VEGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib Malate (SU 11248 Malate) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib Malate, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-157161
-
|
|
11β-HSD
|
Cancer
|
|
11β-HSD2-IN-1 (compound CDSN) is a potent inhibitor of 11β-HSD2, inhibiting the metabolism of Cholestane-3β,5α,6β-triol (CT) in cells by 11β-HSD2 into the tumor promoter, carcinosterone. 11β-HSD2-IN-1 inhibits testosterone biosynthesis, thereby inhibiting MCF-7 cell proliferation. 11β-HSD2-IN-1 has immune activity and antiviral infection effects .
|
-
- HY-123542
-
|
|
Ser/Thr Protease
Apoptosis
|
Cancer
|
|
ONO-3403 is an orally active serine protease inhibitor. ONO-3403 inhibits the production of TNF-α and nitric oxide induced by LPS. ONO-3403 inhibits the cell growth and induces the apoptosis, and has an antitumor effect on malignant tumors .
|
-
- HY-100376
-
|
|
TNF Receptor
Apoptosis
|
Infection
Neurological Disease
|
|
CPI-1189 is an orally active TNF-α release inhibitor. CPI-1189 inhibits phosphorylation of p38. CPI-1189 can inhibit apoptosis. CPI-1189 can be used in the study of HIV and neurological diseases .
|
-
- HY-145330
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
NSC639828 is a potent inhibitor of DNA polymerase α with an IC50 of 70 μM. NSC639828 has high antitumor activity. NSC639828 has the potential for researching cancer disease .
|
-
- HY-136393
-
|
|
IKK
|
Inflammation/Immunology
|
|
IKK-IN-4 is a potent and selective IkappaB kinase 2 (IKKβ orIKK2) inhibitor, with IC50s of 45 and 650 nM for IKKβ and IKKα, respectively .
|
-
- HY-125287
-
|
(Rac)-UCB0599; NPT200-11
|
α-synuclein
|
Neurological Disease
|
|
(Rac)-Minzasolmin ((Rac)-UCB0599) is a brain penetrating inhibitor of accumulation of alpha-synuclein (ASYN) misfolding and aggregation. (Rac)-Minzasolmin can be used for research of Parkinson's disease .
|
-
- HY-132248
-
|
Lenalidomide 5'-amine
|
TNF Receptor
|
Inflammation/Immunology
|
|
C5 Lenalidomide (Lenalidomide 5'-amine) is a thalidomide analog and is a potent inhibitor of TNF-alpha production (IC50=100 μM in LPS stimulated human PBMC) .
|
-
- HY-10402
-
-
- HY-153320
-
|
|
MAP3K
|
Cancer
|
|
AZ-TAK1, an ATP-competitive small molecule inhibitor of TAK1, dephosphorylates TAK1, p38, and IκB-α in lymphoma cell lines .
|
-
- HY-105699
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
Napamezole is an α2A adrenergic receptor antagonist and a serotonin/norepinephrine uptake inhibitor. Napamezole increases the levels of monoamines in the brain by blocking monoamine uptake, which gives it antidepressant activity .
|
-
- HY-10539
-
|
LY317615 dihydrochloride
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) dihydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .
|
-
- HY-122221
-
-
- HY-N2989
-
|
|
NO Synthase
|
Inflammation/Immunology
|
|
3-O-Acetyl-16α-hydroxydehydrotrametenolic acid, an anti-inflammatory triterpenoid, inhibits NO production and iNOS expression in LPS-stimulated Raw264.7 cells .
|
-
- HY-14857
-
|
HCA2969
|
Integrin
|
Inflammation/Immunology
|
|
Carotegrast (HCA2969) is an orally active α4 integrin inhibitor with anti-inflammatory activity. Carotegrast can be used in the research of inflammation-related diseases, such as ulcerative colitis .
|
-
- HY-102076
-
|
|
Adrenergic Receptor
|
Others
|
|
0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP .
|
-
- HY-N4069
-
-
- HY-129121
-
|
|
MAGL
|
Neurological Disease
|
|
ML226 is a potent α/β hydrolase domain-containing protein 11 (ABHD11) inhibitor in vitro and in situ with IC50s of 15 and 0.68 nM, respectively .
|
-
- HY-10342
-
|
LY317615
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .
|
-
- HY-32018
-
|
|
MAP3K
|
Cancer
|
|
Cot inhibitor-2 is a potent, selective and orally active cot (Tpl2/MAP3K8) inhibitor with an IC50 of 1.6 nM. Cot inhibitor-2 inhibts TNF-α production in LPS-stimulated human whole blood with an IC50 of 0.3 μM .
|
-
- HY-120877
-
|
|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively . MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells . MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
|
-
- HY-N7064
-
|
|
Pyruvate Kinase
COX
STAT
TNF Receptor
NO Synthase
Interleukin Related
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Iminostilbene is a chemical precursor of carbamazepine. Additionally, Iminostilbene is an orally active inhibitor of PKM2 (Pyruvate Kinase M2) and COX2 (Cyclooxygenase-2). Iminostilbene exerts its effects by inhibiting PKM2 and its interaction with HIF-1α and STAT3, reducing COX2 and iNOS expression, and decreasing LPS-induced release of IL-1β, IL-6, TNF-α, and MCP-1, thereby suppressing macrophage-mediated inflammatory responses and improving myocardial ischemia/reperfusion (MI/R) injury. Iminostilbene holds promise for research in inflammation regulation, cardiovascular diseases (such as MI/R injury), and macrophage-mediated immune-related diseases .
|
-
- HY-154698
-
|
|
Nucleoside Antimetabolite/Analog
|
Cancer
|
|
Homouridine, is an uridine analogue. Homouridine serves as an intermediate to prepare MMP-2 inhibitor (compund I, IC50=150 μM). Homouridine derivate (compund I) also inhibits TNF-α binding to TNF-αR1 .
|
-
- HY-W016814
-
-
- HY-16187
-
|
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
|
EL-102 is a hypoxia-induced factor 1 (Hif1α) inhibitor. EL-102 induces apoptosis, inhibits tubulin polymerisation and shows activities against prostate cancer. EL-102 can be used for the research of cancer .
|
-
- HY-101438A
-
-
- HY-12085S
-
|
CC-10004-d5
|
Phosphodiesterase (PDE)
TNF Receptor
Apoptosis
|
Inflammation/Immunology
|
|
Apremilast-d5 is a deuterium labeled Apremilast. Apremilast is an orally available inhibitor of type-4 cyclic nucleotide phosphodiesterase (PDE-4) with an IC50 of 74 nM. Apremilast inhibits TNF-α release by lipopolysaccharide (LPS) with an IC50 of 104 nM .
|
-
- HY-161843
-
|
|
Necroptosis
RIP kinase
|
Inflammation/Immunology
|
|
Necroptosis-IN-4, a potent necroptosis inhibitor, is a RIP kinase 1 (RIPK1) inhibitor. Necroptosis-IN-4 has no inhibitory activity against RIPK3 and weak inhibitory activity against VEGFR1/2 and PDGFR-α .
|
-
- HY-18626
-
|
|
Topoisomerase
|
Cancer
|
|
NK 314 is an inhibitor for topoisomerase IIα, which generates the break of DNA double-strand. NK 314 arrests the cell cycle at G2 phase in human acute myeloid leukemia cells, inhibits the proliferation of CEM with IC90 of 55 nM .
|
-
- HY-100536
-
|
|
Wnt
|
Cancer
|
|
IWP-3 is an potent inhibitor of Wnt production with an IC50 of 40 nM. IWP-3 inhibits Porcupine (Porcn) function thereby blocking palmitoylation of Wnt proteins. IWP-3 inhibits CK1γ3 and CK1ε only moderately and does not inhibit CK1α .
|
-
- HY-10255AS
-
|
SU 11248-d10
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d10 is a deuterium labeled Sunitinib. Sunitinib is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-15495B
-
|
(3S)-CC-930 hydrochloride
|
JNK
ERK
p38 MAPK
EGFR
TNF Receptor
|
Inflammation/Immunology
|
|
(3S)-Tanzisertib (hydrochloride) ((3S)-CC-930 (hydrochloride)) is an orally active JNK inhibitor (IC50 values for JNK1, JNK2, and JNK3 are 61, 7, and 6 nM, respectively). (3S)-Tanzisertib (hydrochloride) selectively inhibits ERK1, p38α, and EGFR (IC50 = 0.48, 3.4, and 0.38 μM, respectively). (3S)-Tanzisertib (hydrochloride) inhibits LPS-induced TNFα production in an acute rat PK-PD model. (3S)-Tanzisertib (hydrochloride) can be used in idiopathic pulmonary fibrosis (IPF) research .
|
-
- HY-120793
-
|
TRB-N0224
|
Ras
Apoptosis
MMP
|
Inflammation/Immunology
Cancer
|
|
CMC2.24 (TRB-N0224), an orally active tricarbonylmethane agent, is effective against pancreatic tumor in mice by inhibiting Ras activation and its downstream effector ERK1/2 pathway. CMC2.24 is also a potent inhibitor of zinc-dependent MMPs with IC50s ranging from 2.0-69 μM. CMC2.24 alleviates osteoarthritis progression by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis via the NF-κB/HIF-2α axis .
|
-
- HY-162902
-
|
|
TGF-β Receptor
|
Cardiovascular Disease
|
|
ALK5-IN-82 is a potent and selective inhibitor against activin receptor-like kinase 5 (ALK5) with an IC50 value of 9.1 nM. ALK5-IN-82 inhibits the protein expression of α-smooth muscle actin (α-SMA), collagen I and tissue inhibitor of metalloproteinase 1 (TIMP-1)/matrix metalloproteinase 13 (MMP-13) in transforming growth factor-β-induced human umbilical vein endothelial cells. ALK5-IN-82 is promising for research of cardiac fibrosis .
|
-
- HY-W753806
-
|
UK 33274 hydrochloride
|
Akt
|
Cardiovascular Disease
|
|
Doxazosin hydrochloride (UK 33274 hydrochloride) is a compound used to inhibit hypertension and prostate hyperplasia, with activity that inhibits postsynaptic α1-adrenoceptors on vascular smooth muscle. Doxazosin hydrochloride can cause vasodilation, thereby reducing peripheral vascular resistance. Doxazosin hydrochloride was found to inhibit the proliferation and migration of hepatic stellate cells in a mouse liver fibrosis model. Doxazosin hydrochloride regulates fibrosis, autophagy, and apoptosis of hepatic stellate cells by activating the PI3K/Akt/mTOR signaling pathway. Doxazosin hydrochloride also blocks autophagic flux and induces apoptosis of hepatic stellate cells .
|
-
- HY-135680
-
|
I-OMe-AG 538
|
IGF-1R
|
Metabolic Disease
Cancer
|
|
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-170930
-
|
|
GABA Receptor
Sodium Channel
|
Neurological Disease
|
|
Anticonvulsant agent 9 (compound 4f) is an α1β2γ2 GABAA receptors activator. Anticonvulsant agent 9 activatesα1β2γ2 GABAA receptors with an EC50 of 1.24 μM. Anticonvulsant agent 9 inhibits the inactivation of Nav1.2 channels. Anticonvulsant agent 9 exhibits significant anticonvulsant activities .
|
-
- HY-16903
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-P99333
-
|
M200; Eos 200-4
|
Integrin
|
Cardiovascular Disease
Cancer
|
|
Volociximab (M200) is a chimeric human/murine IgG4 antibody IIA1 targeting integrin α5β1 (EC50=0.2 nM). Integrin α5β1 is a major fibronectin receptor involved in angiogenesis. Volociximab has antiangiogenic and antitumor activities and inhibits the proliferation of human umbilical vein vascular endothelial cells (HUVECs) .
|
-
- HY-B0155
-
|
SCH 417690; SCH-D; MK-7690 free base
|
CCR
HIV
|
Infection
Cancer
|
|
Vicriviroc (SCH 417690) is an orally active CCR5 antagonist with the IC50 of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC50 values of 0.91 nM and 16 nM,,respectively. Vicriviroc can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer .
|
-
- HY-163332
-
|
|
Glycosidase
Dipeptidyl Peptidase
Glutathione Peroxidase
|
Cardiovascular Disease
|
|
MPO-IN-6 (compound ADC) is an electrophile with good antioxidant and anti-inflammatory properties. MPO-IN-6 is a myeloperoxidase (MPO), dipeptidyl peptidase-4 (DPP-4), and α-glucosidase (α-GD) inhibitor with IC50s of 10 μM, 31.02 μM, and 46.05 μM, respectively. MPO-IN-6 is a potential cardiovascular preventive agent .
|
-
- HY-157217
-
|
|
Antifolate
|
Cancer
|
|
Antitumor agent-99 (compound 7) is an anticancer agent targeting FRα/β and PCFT. Antitumor agent-99 inhibits R2/PCFT4 (PCFT), RT16(FRα), and D4(FRβ) cells with IC50s of 51.46 nM, 2.53 nM, and 2.98 nM, respectively .
|
-
- HY-32337R
-
|
1,24(R)-Dihydroxyvitamin D3 (Standard); 1.alpha.,24R-Dihydroxyvitamin D3 (Standard)
|
VD/VDR
Interleukin Related
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Tacalcitol (Standard) is the analytical standard of Tacalcitol. This product is intended for research and analytical applications. Tacalcitol (1,24(R)-Dihydroxyvitamin D3; 1.alpha.,24R-Dihydroxyvitamin D3) can promote normal bone growth by regulating calcium ions. Tacalcitol inhibits cancer cell proliferation and migration. Tacalcitol can be used in the research of inflammation, cancer, and skin diseases.
|
-
- HY-P4191A
-
|
|
CCR
|
Inflammation/Immunology
|
|
Met-RANTES (human) acetate is the acetate form of Met-RANTES (human) (HY-P4191). Met-RANTES (human) acetate is the antagonist for CCR1 and CCR5. Met-RANTES (human) acetate inhibits chemokines human MIP-1α and MIP-1β with IC50 of 5 and 2 nM. Met-RANTES (human) acetate reduces bone destruction and ameliorates rats adjuvant-induced arthritis (AIA) .
|
-
- HY-116830A
-
|
|
GSK-3
|
Cancer
|
|
(Rac)-BRD0705 is a less active racemate of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
|
-
- HY-138678
-
|
|
Ligands for E3 Ligase
|
Cancer
|
|
(R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669) .
|
-
- HY-44809
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Izilendustat is a potent inhibitor of prolyl hydroxylase which can stabilize hypoxia inducible factor- 1 alpha (HIF- lα) and hypoxia inducible factor-2 (HIF-2). Izilendustat has the potential for researching diseases that relate to the body’s inmmune response like colitis and other inflammatory bowel diseases (extracted from patent WO2011057115A1 and WO2011057121A1) .
|
-
- HY-151966
-
|
|
PROTACs
IAP
Caspase
|
Cancer
|
|
TD1092 is a pan-IAP degrader, degrades cIAP1, cIAP2, and XIAP. TD1092 activates Caspase 3/7, and promotes cancer cells apoptosis via IAP degradation. TD1092 inhibits TNFα mediated NF-κB pathway and reduces the phosphorylation of IKK, IkBα, p65, and p38. TD1092 can act as PROTAC, and is used for cancer research .
|
-
- HY-N13095
-
|
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
(+)-Plakevulin A (Plakevulin A) is an oxylipin and can be isolated from an Okinawan sponge Plakortis sp. (+)-Plakevulin A inhibits the enzymatic activity of DNA polymerases α and δ. (+)-Plakevulin A induces apoptosis and shows anticancer activity .
|
-
- HY-N10606
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Uvagrandol potently inhibits α-glucosidase and porcine lipase (IC50: 15.2 μM, 11.2 μM respectively). Uvagrandol can be used in the research of Type 2 diabetes and obesity .
|
-
- HY-13514
-
|
|
PI3K
|
Cancer
|
|
TG 100713 is an inhibitor of PI3K, with IC50s of 24, 50, 165, and 215 nM for PI3Kδ, γ, α and β isoforms respectively .
|
-
- HY-10527
-
|
Bay 57-9352
|
c-Kit
PDGFR
VEGFR
|
Cancer
|
|
Telatinib (Bay 57-9352) is an orally active, small molecule inhibitor of VEGFR2, VEGFR3, PDGFα, and c-Kit with IC50s of 6, 4, 15 and 1 nM, respectively.
|
-
- HY-10527C
-
|
Bay 57-9352 mesylate
|
VEGFR
PDGFR
c-Kit
|
Cancer
|
|
Telatinib mesylate (Bay 57-9352 mesylate) is a potent and orally active VEGFR2, VEGFR3, PDGFα, and c-Kit inhibitor with IC50s of 6 nM, 4 nM, 15 nM and 1 nM, respectively .
|
-
- HY-124646
-
|
|
IRE1
|
Inflammation/Immunology
|
|
KIRA-7, an imidazopyrazine compound, binds the IRE1α kinase (IC50 of 110 nM) to allosterically inhibit its RNase activity. KIRA-7 has an anti-fibrotic effect .
|
-
- HY-144697
-
-
- HY-N10969
-
|
|
Others
|
Others
|
|
(+)-5,7,4'-Trimethoxyafzelechin is a derivative of (+)-Afzelechin HY-N2821. (+)-Afzelechin is an α-glucosidase activity inhibitor. (+)-Afzelechin can be isolated from rhizomes of Bergenia ligulata .
|
-
- HY-12299
-
|
Dual LCK/SRC inhibitor
|
Src
|
Cancer
|
|
WH-4-023 is a potent and selective dual Lck/Src inhibitor with IC50 of 2 nM/6 nM for Lck and Src kinase respectively; little inhibition on p38α and KDR.
|
-
- HY-103030
-
|
|
PI3K
|
Cancer
|
|
PI3K-IN-32 (compound 35) is a potent PI3K p110α inhibitor with an pIC50 of 6.85 .
|
-
- HY-13613
-
|
GG 745; GI 198745
|
5 alpha Reductase
Apoptosis
|
Cancer
|
|
Dutasteride (GG745) is a potent inhibitor of both 5α-reductase isozymes. Dutasteride may possess off-target effects on the androgen receptor (AR) due to its structural similarity to DHT .
|
-
- HY-100779
-
|
SMP 114
|
CaMK
Autophagy
|
Metabolic Disease
|
|
Rimacalib (SMP 114) is a Ca 2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor, with IC50s of ~1 μM for CaMKIIα to ~30 μM for CaMKIIγ .
|
-
- HY-N0234R
-
|
|
Amyloid-β
PPAR
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
|
Bavachinin (Standard) is the analytical standard of Bavachinin. This product is intended for research and analytical applications. Bavachinin is agonist of pan-peroxisome proliferator-activated receptor (PPAR), with the IC50 value of 21.043 μM, 12.819 μM, and 0.622 μM to PPAR-α, RRAR-β/δ, and PPAR-γ, respectively. Bavachinin is an inhibitor of HIF-1α. Bavachinin exhibits antitumor activity against non-small cell lung cancer by targeting RRAR-γ. Bavachinin is a natural compound with anti-inflammatory and anti-angiogenic activities. Bavachinin has orally bioactivity. .
|
-
- HY-44809A
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
Cancer
|
|
Izilendustat (hydrochloride) is a potent inhibitor of prolyl hydroxylase which stabilizes hypoxia inducible factor- 1 alpha (HIF- lα), as well as hypoxia inducible factor-2 (HIF-2). Izilendustat (hydrochloride) has the potential for the research of HIF- lα related diseases including Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, anemia, colitis, and other inflammatory bowel diseases (extracted from patent WO2011057115A1/WO2011057112A1/WO2011057121A1) .
|
-
- HY-16569S
-
-
- HY-N13716
-
|
|
DNA/RNA Synthesis
HIV
Reverse Transcriptase
|
Infection
|
|
Lucidenic acid O is a terpene compound, is a DNA polymerases inhibitor. Lucidenic lactone inhibits calf DNA polymerase-α, rat DNA polymerase-β, and HIV-1 reverse transcriptase with IC50 values of 42 μM, 99 μM, and 69 μM, respectively .
|
-
- HY-150073
-
|
|
PKA
|
Cancer
|
|
DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer .
|
-
- HY-13867A
-
|
GF109203X hydrochloride; Go 6850 hydrochloride
|
PKC
GSK-3
|
Metabolic Disease
Cancer
|
|
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-117603
-
|
|
Glucokinase
|
Infection
|
|
CM-10-18 is a potent and orally active inhibitor of both α-glucosidases I and II in vitro and in treated animals. CM-10-18 inhibits DENV infection of cultured human cells and reduces the peak viremia of DENV in mice .
|
-
- HY-169118
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
EGR-1-IN-2 (compound 2) is an EGR-1 inhibitor with anti-inflammatory activity. EGR-1-IN-2 inhibits the formation of EGR-1-DNA complexes induced by TNF-α in HaCaT cells .
|
-
- HY-N13712
-
|
|
DNA/RNA Synthesis
HIV
Reverse Transcriptase
|
Infection
|
|
Lucidenic lactone is a terpene compound, is a DNA polymerase inhibitor. Lucidenic lactone inhibits calf DNA polymerase-α, rat DNA polymerase-β, and HIV-1 reverse transcriptase with IC50 values of 42 μM, 99 μM, and 69 μM, respectively .
|
-
- HY-16569S1
-
-
- HY-13867
-
|
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-108646
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
SX 011 is a p38 inhibitor with IC50s of 9 nM and 90 nM against p38α and p38β, respectively. SX 011 also inhibits JNK-2 with an IC50 of 100 nM. SX-011 is orally bioavailable .
|
-
- HY-15244
-
|
BYL-719
|
PI3K
|
Cancer
|
|
Alpelisib (BYL-719) is a potent, selective, and orally active PI3Kα inhibitor. Alpelisib (BYL-719) shows efficacy in targeting PIK3CA-mutated cancer. Alpelisib (BYL-719) also inhibits p110α/p110γ/p110δ/p110β with IC50s of 5/250/290/1200 nM, respectively. Antineoplastic activity .
|
-
- HY-172888
-
|
|
Endogenous Metabolite
FAK
|
Cancer
|
|
SPP-037 is an orally active and selective inhibitor of ST6GAL1 (IC50: 3.59 μM). SPP-037 exhibits anti-MDA-MB-231 cell migration activity by inhibiting integrin α2,6-sialylation and integrin-FAK-paxillin pathway. SPP-037 has anti-tumor activity in MDA-MB-231 xenograft mouse model. SPP-037 can be used in breast cancer research .
|
-
- HY-P2657
-
|
|
HIF/HIF Prolyl-Hydroxylase
Proton Pump
Endogenous Metabolite
|
Cancer
|
|
Verucopeptin is a potent HIF-1 (IC50=0.22 μM) inhibitor and decreases the expression of HIF-1 target genes and HIF-1α protein levels. Verucopeptin strongly inhibits v-ATPase activity by directly targeting the v-ATPase ATP6V1G subunit but not ATP1V1B2 or ATP6V1D. Verucopeptin exhibits antitumor activity against multidrug resistance (MDR) cancers and can be used for cancer research.
|
-
- HY-B0193AR
-
|
|
Adrenergic Receptor
Autophagy
|
Cardiovascular Disease
Endocrinology
Cancer
|
|
Prazosin (hydrochloride) (Standard) is the analytical standard of Prazosin (hydrochloride). This product is intended for research and analytical applications. Prazosin hydrochloride is a well-tolerated, CNS-active α1-adrenergic receptor antagonist for the research of high blood pressure and alcohol use disorders . Prazosin hydrochloride potently inhibits Norepinephrine (NE)-stimulated 45Ca efflux with an IC50 of 0.15 nM .Prazosin hydrochloride inhibits organic cation transporters OCT-1 and OCT-3 with IC50s of 1.8, and 13 μM, respectively .
|
-
- HY-N13083
-
|
|
PCSK9
|
Cardiovascular Disease
|
|
PCSK9-IN-28 (Compound C11) is a PCSK9 inhibitor that can be isolated from Euphorbia esula. By binding to HNF1α, PCSK9-IN-28 inhibits PCSK9 transcription by binding to HNF1α and affecting its nuclear distribution, thereby enhancing LDLR and promoting LDL uptake. PCSK9-IN-28 exhibits significant lipid-lowering activity in the high-fat diet (HFD) mouse model and can be used in the study of hyperlipidemia .
|
-
- HY-170492
-
|
|
Epoxide Hydrolase
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
sEH inhibitor-19 (Compound (R)-14i) is an orally active inhibitor for soluble epoxide hydrolase (sEH) with an IC50 of 1.2 nM. sEH inhibitor-19 inhibits the expression of TNF-α and IL-6, exhibits anti-inflammatory activity in mouse acute pancreatitis or Carrageenan (HY-125474)-induced edema models .
|
-
- HY-10255AS1
-
|
|
Isotope-Labeled Compounds
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib-d4 is the deuterium labeled Sunitinib. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-112389
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
p38 MAP Kinase Inhibitor III (compound 7h) is a p38 MAPK inhibitor with an 50 of 0.9 μM. p38 MAP Kinase Inhibitor III also inhibits IL-1β and TNF-α release with 50 values of 0.37 μM and 0.044 μM, respectively .
|
-
- HY-143237
-
|
|
Phosphodiesterase (PDE)
|
Others
|
|
ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research .
|
-
- HY-N7095
-
|
CTZ
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftezole (CTZ) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole (CTZ) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity .
|
-
- HY-12774
-
IC261
4 Publications Verification
|
Casein Kinase
Apoptosis
|
Cancer
|
|
IC261 is a selective, ATP-competitive CK1 inhibitor, with IC50s of 1 μM, 1 μM, 16 μM for Ckiδ, Ckiε and Ckiα1, respectively.
|
-
- HY-111058
-
|
|
PI3K
|
Cancer
|
|
D-106669 (comppun 150) is a potent inhibitor of PI3Kα, with the IC50 of 0.129 μM. D-106669 plays an important role in cancer research .
|
-
- HY-N6575
-
-
- HY-111484A
-
|
SRN-927 Racemate
|
Estrogen Receptor/ERR
|
Cancer
|
|
GDC-0927 Racemate (SRN-927 Racemate) is an estrogen receptor (ER) degrader that can effectively inhibit the activity of ER-α with an IC50 value of 0.2 nM and can be used in diseases related to estrogen receptors.
|
-
- HY-W727627
-
|
|
Amylases
|
Metabolic Disease
|
|
5-O-Coumaroylquinic acid is a potent, reversible, non-competitive α-amylase inhibitor with an IC50 value of 69.39 μM. 5-O-Coumaroylquinic acid can be used in diabetes research .
|
-
- HY-N9075
-
|
|
Glycosidase
|
Cancer
|
|
9-(4′-Hydroxyphenyl)-2-methoxyphenalen-1-one is a phytoalexin and mixed competitive α-glucosidase inhibitor of Bacillus stearothermophilus (IC50: 3.86 mg/L) .
|
-
- HY-117393
-
|
|
PKC
|
Cancer
|
|
Bisindolylmaleimide III is a potent and selective inhibitor of protein kinase C (PKC). Bisindolylmaleimide III selectively interacts with either PKCα or ribosomal S6 protein kinase 1 after activation of these kinases .
|
-
- HY-N0907
-
-
- HY-13493
-
|
|
PDGFR
c-Kit
FLT3
|
Cancer
|
|
AC710 is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
|
-
- HY-10539B
-
|
LY317615 hydrochloride
|
PKC
Autophagy
Apoptosis
|
Cancer
|
|
Enzastaurin (LY317615) hydrochloride is a potent and selective PKCβ inhibitor with an IC50 of 6 nM, showing 6- to 20-fold selectivity over PKCα, PKCγ and PKCε .
|
-
- HY-120152
-
|
|
SphK
|
Inflammation/Immunology
|
|
SLP7111228 is a SphK1 inhibitor. SLP7111228 reduces LPS-induced TNFα and IL-1β production. SLP7111228 can be used in neuroinflammatory diseases research .
|
-
- HY-N7096
-
|
CTZ sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Ceftezole sodium (CTZ sodium) is a broad-spectrum cephem antibiotic against many species of gram-positive and gram-negative bacteria. Ceftezole sodium (CTZ sodium) is an alpha-glucosidase inhibitor with in vivo anti-diabetic activity .
|
-
- HY-118388
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour .
|
-
- HY-146128
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Anti-hyperglycemic agent-1 (compound 10) is a potent α-Glucosidase inhibitor, with an IC50 of 0.53 μM. Anti-hyperglycemic agent-1 can be used for diabetes research .
|
-
- HY-B0089
-
|
BAY g 5421
|
Glycosidase
|
Metabolic Disease
Cancer
|
|
Acarbose (BAY g 5421), antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
- HY-P2203A
-
|
|
Notch
|
Cancer
|
|
SAHM1 TFA is a Notch pathway inhibitor. SAHM1 TFA stabilizes hydrocarbon-stapled alpha helical peptide. SAHM1 TFA targets the protein-protein interface and prevents Notch complex assembly.
|
-
- HY-N1949
-
|
|
TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
Homoplantaginin is a flavonoid from a traditional Chinese medicine Salvia plebeia with antiinflammatory and antioxidant properties. Homoplantaginin could inhibit TNF-α and IL-6 mRNA expression, IKKβ and NF-κB phosphorylation.
|
-
- HY-107500
-
|
|
RAR/RXR
Autophagy
|
Others
|
|
UVI 3003 is a highly selective antagonist of retinoid X receptor (RXR), and inhibits xenopus and human RXRα in Cos7 cells, with IC50s of 0.22 and 0.24 μM, respectively.
|
-
- HY-124876
-
|
SC-D
|
α-synuclein
|
Neurological Disease
|
|
SynuClean-D (SC-D) is an inhibitor of α-synuclein aggregation, disrupts mature amyloid fibrils, prevents fibril propagation, and abolishes the degeneration of dopaminergic neurons in an animal model of Parkinson’s disease .
|
-
- HY-N11840
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Mortatarin F (Compound 1) is an inhibitor of α‑glucosidase with an IC50 of 8.7 μΜ. Mortatarin F is an renylated flavonoid that can be isolated from mulberry leaves and can be used for hypoglycemic research .
|
-
- HY-14305A
-
|
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
BMS-582949 hydrochloride is an orally active and highly selective p38α MAPK inhibitor, with an IC50 of 13 nM. BMS-582949 hydrochloride displays a significantly improved pharmacokinetic profile and is effective in inflammatory disease .
|
-
- HY-167877
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
PS-166276 is a highly potent and less cytotoxic inhibitor of p38. PS166276 has an IC50 of 28 nM at p38 kinase and 170 nM in the THP-1 TNFα assay .
|
-
- HY-13493A
-
|
|
PDGFR
|
Cancer
|
|
AC710 Mesylate is a potent PDGFR inhibitor with Kds of 0.6, 1.57, 1, 1.3, 1.0 nM for FLT3, CSF1R, KIT, PDGFRα and PDGFRβ, respectively.
|
-
- HY-136392
-
|
|
IKK
|
Inflammation/Immunology
|
|
IKK-IN-3 is a potent and selective IkappaB kinase 2 (IKK2 or IKKβ) inhibitor, with IC50s of 19 and 400 nM for IKK2 and IKK1 (or IKKα), respectively .
|
-
- HY-15174
-
|
BEZ235 Tosylate; NVP-BEZ 235 Tosylate
|
PI3K
mTOR
Autophagy
|
Cancer
|
|
Dactolisib Tosylate (BEZ235 Tosylate) is a dual PI3K and mTOR kinase inhibitor with IC50 values of 4, 75, 7, 5 nM for PI3Kα, β, γ, δ, respectively. Dactolisib Tosylate (BEZ235 Tosylate) inhibits mTORC1 and mTORC2.
|
-
- HY-70013
-
|
CB-7598
|
Cytochrome P450
|
Cancer
|
|
Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.
|
-
- HY-12046
-
PIK-93
4 Publications Verification
|
PI4K
PI3K
Virus Protease
|
Cancer
|
|
PIK-93 is the first potent, synthetic PI4K (PI4KIIIβ) inhibitor with IC50 of 19 nM, and also inhibits PI3Kγ and PI3Kα with IC50 of 16 nM and 39 nM, respectively.
|
-
- HY-171296
-
|
|
p38 MAPK
JNK
|
Inflammation/Immunology
|
|
p38 Kinase inhibitor 8 (Compound CCLXXVIII) is the orally active inhibitor for p38β and JNK2α2 with IC50s of 6.3 nM and 53.6 nM. p38 Kinase inhibitor 8 exhibits anti-inflammatory effect in rats collagen-induced arthritis models .
|
-
- HY-10683
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
- HY-B0155B
-
|
SCH 417690 malate; SCH-D malate; MK-7690
|
CCR
HIV
|
Infection
Cancer
|
|
Vicriviroc (SCH 417690) malate is an orally active CCR5 antagonist with the IC50 of 10 nM, and also inhibts MIP-1α and intracellular calcium release induced by the ligand RANTES (10 nM) with the IC50 values of 0.91 nM and 16 nM,,respectively. Vicriviroc malate can inhibits human immunodeficiency virus type 1 (HIV-1) infection, and can also used for study of cancer .
|
-
- HY-103457
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Y134 is a selective and orally active oestrogen receptor (ER) modulator (SERM), exhibits potent antagonist activity at ERα and ERβ. Y134 shows 121.1-fold selectivity for ERα (Ki=0.09 nM) over ERβ (Ki=11.31 nM). Y134 inhibits oestrogen-stimulated proliferation of ER-positive human breast cancer cells .
|
-
- HY-116830B
-
|
(R)-BRD0705
|
GSK-3
|
Cancer
|
|
BRD5648 ((R)-BRD0705) is a negative control of BRD0705. BRD0705 is a potent, paralog selective and orally active GSK3α inhibitor with an IC50 of 66 nM and a Kd of 4.8 μM. BRD0705 displays increased selectivity for GSK3α (8-fold) versus GSK3β (IC50 of 515 nM). BRD0705 can be used for acute myeloid leukemia (AML) .
|
-
- HY-B1116A
-
|
(-)-Metaraminol; (-)-erythro-Metaraminol; (-)-m-Hydroxynorephedrine
|
Adrenergic Receptor
|
Neurological Disease
|
|
Metaraminol ((-)-Metaraminol) is a sympathomimetic compound with activity that acts primarily at alpha-1 adrenergic receptors. Metaraminol is used to inhibit hypotension due to vasodilation, particularly in critically ill patients who do not respond well to volume resuscitation. Metaraminol may also be used as an adjunct to help improve cardiac contractility. The use of metaraminol may be supported by less evidence, but its effectiveness in specific situations remains of interest .
|
-
- HY-N11844
-
|
|
Amylases
|
Metabolic Disease
|
|
Quercetin 3-(6″-caffeoylsophoroside) is an orally active α-amylase inhibitor, with an IC50 of 73.66 μg/mL. Quercetin 3-(6″-caffeoylsophoroside) presents in thehydro-methanolic extract of Cardamine hirsuta Linn. Quercetin 3-(6″-caffeoylsophoroside) shows the antidiabetic activities by oxidative stress reduction and α-amylase inhibition. Quercetin 3-(6″-caffeoylsophoroside) can be used for diabetes mellitus research .
|
-
- HY-107371
-
|
NSC95682
|
IRE1
|
Inflammation/Immunology
Cancer
|
|
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) (Compound 3-5) is a selective and potent IRE-1α inhibitor with an IC50 value of 0.08 μM. 6-Bromo-2-hydroxy-3-methoxybenzaldehyde can be used for research on diseases associated with the unfolded protein response (UPR), such as cancer and autoimmune diseases .
|
-
- HY-B0661AR
-
|
|
Adrenergic Receptor
Apoptosis
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin (hydrochloride) (Standard) is the analytical standard of Tamsulosin hydrochloride (HY-B0661A). Tamsulosin hydrochloride ((R)-(-)-YM12617 free base) is an orally active antagonist of α1-adrenergic receptor. Tamsulosin hydrochloride induces Apoptosis. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth and inhibits inflammation in animal models .
|
-
- HY-B2169R
-
|
|
5-HT Receptor
Reference Standards
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone (Standard) is the analytical standard of Melperone (HY-B2169). This product is intended for research and analytical applications. Melperone is a butyrophenone with atypical antipsychotic properties. Melperone is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone is also a CYP2D6 inhibitor. Melperone can be used for the study of schizophrenia, and agitation in the elderly.
|
-
- HY-B2169S2
-
|
|
Isotope-Labeled Compounds
5-HT Receptor
Dopamine Receptor
Adrenergic Receptor
Cytochrome P450
|
Neurological Disease
|
|
Melperone-d4 hydrochloride is the deuterium labeled Melperone hydrochloride (HY-103109) . Melperone hydrochloride is a butyrophenone with atypical antipsychotic properties. Melperone hydrochloride is a multireceptor antagonist with Kds of 102 nM, 180 nM, 180 nM, and 150 nM for 5-HT2A, dopamine D2, α1-adrenergic, and α2-adrenergic receptors, respectively. Melperone hydrochloride has weak binding to histamine H1, 5-HT2C, 5-HT1A, 5-HT1D, and muscarinic receptors, with Kd values of 580 nM, 2100 nM, 2200 nM, 3400 nM, >10000 nM, respectively. Melperone hydrochloride is also a CYP2D6 inhibitor. Melperone hydrochloride can be used for the study of schizophrenia, and agitation in the elderly .
|
-
- HY-17617
-
|
Z-360
|
Cholecystokinin Receptor
Ephrin Receptor
Interleukin Related
VEGFR
HIF/HIF Prolyl-Hydroxylase
Akt
|
Neurological Disease
Cancer
|
|
Nastorazepide (Z-360) is an orally active 1,5-benzodiazepine derivative and gastrin/CCK-2 receptor antagonist. Nastorazepide inhibits the specific binding of [ 3H]CCK-8 to the human CCK-2 receptor with a Ki value of 0.47 nM. Nastorazepide inhibits IL-1β, ephrin B1, VEGF, and HIF-1alpha, reduces Akt and NR2B phosphorylation. Nastorazepide has antitumor activity against pancreatic cancer. Nastorazepide inhibits colorectal cancer liver metastasis and relieves pain .
|
-
- HY-155998
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NF-κB-IN-11 (Compound 3i) is a NF-κB inhibitor. NF-κB-IN-11 inhibits TNF-α induced activation of NF-κB pathway, and inhibits nuclear translocation of NF-κB. NF-κB-IN-11 down-regulates the expression levels of phosphor-IKK, IκBα, and NF-κB p65. NF-κB-IN-11 has anti-inflammatory activity, and alleviates dextran sulfate sodium-induced colitis in mice. NF-κB-IN-11 (p.o.) shows a MTD more than 1852 mg/kg in mice acute toxicity assay .
|
-
- HY-N10009
-
|
|
NF-κB
TNF Receptor
COX
ERK
p38 MAPK
Sirtuin
|
Inflammation/Immunology
|
|
Cudraflavone B is a prenylated flavonoid with anti-inflammatory and anti-tumor properties. Cudraflavone B is also a dual inhibitor of COX-1 and COX-2. Cudraflavone B blocks the translocation of nuclear factor κB (NF-κB) from the cytoplasm to the nucleus in macrophages. Thus, Cudraflavone B inhibits tumor necrosis factor α (TNFα) gene expression and secretion. Cudraflavone B also triggers the mitochondrial apoptotic pathway, activates NF-κB, the MAPK p38, and ERK, and induced the expression of SIRT1. Thus Cudraflavone B inhibits the growth of human oral squamous cell carcinoma cells .
|
-
- HY-169831
-
|
|
α-synuclein
|
Neurological Disease
|
|
HUP-55 is a prolyl endopeptidase inhibitor (IC50 = 5 nM). HUP-55 reduces the dimerization of α-synuclein in Neuro2a cells and induces autophagy (Autophagy) in HEK293 cells. It also decreases the increase in reactive oxygen species (ROS) production induced by hydrogen peroxide in SH-SY5Y cells at a concentration of 10 μM. In a mouse Parkinson’s disease model, HUP-55 (10 mg/kg) improves motor function (reduces the use frequency of the impaired paw) and decreases the levels of harmful oligomers of α-synuclein in the striatum caused by overexpression of α-synuclein .
|
-
- HY-13982
-
|
|
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
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-W015445
-
|
|
p38 MAPK
|
Metabolic Disease
|
|
SD-169 is an orally active ATP-competitive inhibitor of p38α MAPK, with an IC50 of 3.2 nM. SD-169 also weakly inhibits p38β MAPK with an IC50 of 122 nM. SD-169 prevents the development and progression of diabetes by inhibiting T cell infiltration and activation .
|
-
- HY-P0154
-
|
ε-V1-2; EAVSLKPT
|
PKC
|
Inflammation/Immunology
|
|
Epsilon-V1-2 (ε-V1-2), a PKCε-derived peptide, is a selective PKCε inhibitor. Epsilon-V1-2 inhibits the translocationof PKCε, but not α-, β-, and δPKC .
|
-
- HY-153701
-
|
|
JAK
|
Cancer
|
|
JAK-IN-26 (compound 2) is an orally active JAK inhibitor with good pharmacokinetic characteristics. JAK-IN-26 inhibits IFN-α2B-induced phosphorylation of STAT3 in Jurkat cells (IC50=17.2 nM) .
|
-
- HY-100544
-
FLLL32
5 Publications Verification
|
STAT
JAK
Apoptosis
|
Cancer
|
|
FLLL32, a synthetic analog of curcumina, is a JAK2/STAT3 dual inhibitor with anti-tumor activity. FLLL32 can inhibit the induction of STAT3 phosphorylation by IFNα and IL-6 in breast cancer cells .
|
-
- HY-126988
-
|
α-MAPI
|
Elastase
|
Others
|
|
SP-Chymostatin B (α-MAPI) is a strong inhibitor of many proteases, including chymotrypsin, papain, chymotrypsin-like serine proteinases, chymases, and lysosomal cysteine proteinases such as cathepsins A,B,C, H, and L. SP-Chymostatin B weakly inhibits human leucocyte elastase .
|
-
- HY-153416
-
|
|
Amyloid-β
|
Neurological Disease
|
|
QR-0217 is a potent Aβ1-40 aggregation inhibitor with an IC50 value of 7.5 µM. QR-0217 inhibits α-synuclein aggregation. QR-0217 reduces memory impairments caused by Aβ neurotoxicity .
|
-
- HY-N12138
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Flaccidoside III is a flavonoid and triterpenoid isolated from the aerial parts of N. sativa (Ranunculaceae). Flaccidoside III inhibits α-Glucosidase (IC50: 256.7 μM) and has potential antioxidant and antidiabetic activities .
|
-
- HY-W067427
-
|
|
IKK
|
Cancer
|
|
BAY32-5915 is a potent IKKα inhibitor with an IC50 value of 60 nM. BAY32-5915 has not affect Doxorubicin (HY-15142A)-induced NF-κB activation .
|
-
- HY-135307
-
|
Huanjunzuo
|
Fungal
|
Infection
|
|
SSF-109 is a broad-spectrum fungicide which has protective activity against plant disease. SSF-109 inhibits the biosynthesis of ergosterol at the 14α-demethylation step in Botrytis cinerea .
|
-
- HY-100207
-
|
CP21
|
GSK-3
|
Cancer
|
|
CP21R7 is potent GSK-3β inhibitor, with an IC50 of 1.8 nM; CP21R7 also shows inhibitory activitiy against PKCα, with an IC50 of 1900 nM.
|
-
- HY-15356
-
-
- HY-N15305
-
|
|
FXR
|
Inflammation/Immunology
|
|
Ferolin is the agonist for farnesoid X receptor (FXR) with an EC50 of 0.56 µM. Ferolin inhibits the expression of inflammatory genes (such as iNOS, IL-1β and TNFα) upon the FXR activation .
|
-
- HY-N0472R
-
|
|
TNF Receptor
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Geraniin (Standard) is the analytical standard of Geraniin. This product is intended for research and analytical applications. Geraniin is a TNF-α releasing inhibitor with numerous activities including anticancer, anti-inflammatory, and anti-hyperglycemic activities, with an IC50 of 43 μM.
|
-
- HY-151440
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 42 is an antifungal agent. Antifungal agent 42 has an inhibitory effect on lanosterol 14α-demethylase (CYP51) of C.alb.. Antifungal agent 42 inhibits biofilm formation .
|
-
- HY-103245
-
|
|
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-159799
-
|
|
p38 MAPK
|
Cancer
|
|
p38α inhibitor 5 (compound 1) is a PROTAC-type target protein ligand targeting p38 and can be used to synthesize NR-11c (HY-159798) .
|
-
- HY-N8947
-
|
|
Endogenous Metabolite
Glycosidase
|
Metabolic Disease
|
|
Glyurallin A (Compound 79) is isolated from the
naturalGlycyrrhiza uralensis. Glyurallin A inhibitsα-Glucosidase(HY-P2802)(IC50=0.3 μM). Glyurallin A
can be used in the study of anti-diabetes .
|
-
- HY-119248
-
|
MK-0767
|
PPAR
|
Metabolic Disease
|
|
KRP-297 is a PPARα and PPARγ agonist potentially for the research of type 2 diabetes and dyslipidemia. KRP-297 restores reduced lipid oxidation, and inhibits of enhanced lipogenesis and triglyceride accumulation in the liver.
|
-
- HY-N0694R
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Schisantherin A (Standard) is the analytical standard of Schisantherin A. This product is intended for research and analytical applications. Schisantherin A is a dibenzocyclooctadiene lignan. Schisantherin A inhibits p65-NF-κB translocation into the nucleus by IκBα degradation.
|
-
- HY-13812
-
-
- HY-14649R
-
|
Vitamin A acid (Standard); all-trans-Retinoic acid (Standard); ATRA (Standard)
|
Reference Standards
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid (Standard) is the analytical standard of Retinoic acid. This product is intended for research and analytical applications. Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha.
|
-
- HY-A0077
-
-
- HY-12707R
-
|
|
Dopamine Receptor
Adrenergic Receptor
Histone Methyltransferase
|
Neurological Disease
Endocrinology
Cancer
|
|
Piribedil (Standard) is the analytical standard of Piribedil. This product is intended for research and analytical applications. Piribedil is a potent and orally active dopamine D2 and dopamine D3 agonist. Piribedil is also a α2-adrenoceptors antagonist. Piribedil can inhibit MLL1 methyltransferase activity (EC50: 0.18 μM). Piribedil has the potential for the research of parkinson's disease, circulatory disorders, cancers .
|
-
- HY-11068
-
|
|
p38 MAPK
Autophagy
|
Inflammation/Immunology
|
|
SB 239063 is a potent, selective and orally active p38 MAPK inhibitor, exhibits an IC50 of 44 nM for recombinant purified human p38α, with equipotent inhibitory activity against p38α and p38β. SB 239063 has no effect on p38γ or p38δ. With anti-asthma activity and also be used to enhance memory which is impaired due to aging or medical conditions, such as, AD .
|
-
- HY-A0077S1
-
|
|
5-HT Receptor
Adrenergic Receptor
Apoptosis
Autophagy
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
Endocrinology
|
|
Perphenazine-d4 is the deuterium labeled Perphenazine. Perphenazine is a typical antipsychotic agent, inhibits 5-HT2Areceptor, Alpha-1A adrenergic receptor, Dopamine receptor D2/D3, D2L receptor, and Histamine H1 receptor, with Ki values of 5.6, 10, 0.765/0.13, 3.4, and 8 nM, respectively.
|
-
- HY-107589A
-
|
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 hydrate is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 hydrate selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 hydrate results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
|
-
- HY-107589
-
BIO5192
1 Publications Verification
|
Integrin
|
Inflammation/Immunology
|
|
BIO5192 is a selective and potent integrin α4β1 (VLA-4) inhibitor (Kd<10 pM). BIO5192 selectively binds to α4β1 (IC50=1.8 nM) over a range of other integrins. BIO5192 results in a 30-fold increase in mobilization of murine hematopoietic stem and progenitors (HSPCs) over basal levels .
|
-
- HY-100936
-
|
SQ 20009; EHT 0202 hydrochloride
|
Phosphodiesterase (PDE)
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Etazolate hydrochloride (SQ 20009) is an orally active, selective inhibitor of type 4 phosphodiesterase (PDE4) with an IC50 of 2 μM. Etazolate hydrochloride is a γ-aminobutyric acid A (GABAA) receptor regulator. Etazolate hydrochloride is an α-secretase activator and induced the production of soluble amyloid precursor protein (sAPPα). Etazolate hydrochloride, a pyrazolopyridine class derivative, increases cAMP levels. Etazolate hydrochloride has anxiolyticlike, antidepressant-like and anti-inflammatory effects .
|
-
- HY-B0135A
-
|
|
NKCC
GABA Receptor
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Furosemide sodium is a potent and orally active inhibitor of Na +/K +/2Cl - (NKCC) cotransporter, NKCC1 and NKCC2 . Furosemide sodium is also a GABAA receptors antagonist and displays 100-fold selectivity for α6-containing receptors than α1-containing receptors. Furosemide sodium acts as a loop diuretic and used for the study of congestive heart failure, hypertension and edema .
|
-
- HY-N11728
-
|
|
Amylases
Glycosidase
|
Metabolic Disease
|
|
2,7"-Phloroglucinol-6,6'-bieckol is an orally active dual α-amylase/α-glucosidase inhibitor with IC50 values of 6.94 μM and 23.35 μM respectively. 2,7"-Phloroglucinol-6, 6'-bieckol alleviates postprandial hyperglycemia in diabetic mice. 2,7"-Phloroglucinol-6,6'-bieckol can be used in diabetes research .
|
-
- HY-A0077A
-
-
- HY-P10869
-
|
|
Natriuretic Peptide Receptor (NPR)
|
Inflammation/Immunology
Cancer
|
|
dCNP binds to NPR-B/C receptor, activates cGMP signaling pathway, and regulates vascular function. dCNP exhibits anti-hypoxia property through downregulation of hypoxia-related genes expressions like HIF1α and HIF2α. dCNP inhibits the induction of tumor stroma and exhibits anti-fibrosis activity. dCNP upregulates CTLs, NK cells, and conventional type 1 dendritic cells in tumors, and activates immune responses .
|
-
- HY-P99025
-
|
TNX-650
|
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
Lebrikizumab (TNX-650) is an IgG4 humanized anti-interleukin-13 (IL-13) mAb with anti-itch effects that specifically binds to IL-13 in a non-receptor binding domain and inhibits its function. Lebrikizumab inhibits the IL-13 driven Th2 inflammatory response and blocks the signaling of IL-4Rα/IL-13Rα1. Lebrikizumab can be used for the research of asthma, atopic dermatitis and neuroinflammatory diseases .
|
-
- HY-W654013
-
|
|
Isotope-Labeled Compounds
Apoptosis
Potassium Channel
Antibiotic
Bacterial
MDM-2/p53
HIF/HIF Prolyl-Hydroxylase
Calcium Channel
|
Infection
|
|
Minocycline-d7 is deuterium labeled Minocycline. Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
|
-
- HY-N1940
-
|
Cycloicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
Cancer
|
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties . β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
|
-
- HY-N5112B
-
|
Isoarnebin I
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
Notch
NO Synthase
Bcl-2 Family
|
Cancer
|
|
β,β-Dimethylacrylshikonin (Isoarnebin I) is a naphthoquinone derivative that can be isolated from Lithospermum erythrorhizon Sieb. et Zucc. β,β-Dimethylacrylshikonin promotes angiogenesis by inducing eNOS, VEGF and HIF-1α expression through the PI3K-dependent pathway. β,β-Dimethylacrylshikonin inhibits Notch-1 activation. β,β-Dimethylacrylshikonin inhibtis tumor cell proliferation, induces tumor cell apoptosis, and inhibits tumor growth .
|
-
- HY-17412R
-
-
- HY-106012
-
|
|
PI4K
PI3K
|
Cancer
|
|
PI4K-IN-1 (compound 44) is a potent PI4KIII inhibitor, with pIC50 values of 9.0 and 6.6 for PI4KIIIα and PI4KIIIβ, respectively. PI4K-IN-1 also inhibits PI3Kα/β/γ/δ, with pIC50 values of 4.0/<3.7/5.0/<4.1, respectively .
|
-
- HY-N8936
-
|
|
Others
|
Inflammation/Immunology
|
|
Narchinol B (Compound 4) is a sesquiter penoid
compound. Narchinol B has anti-inflammatory effects. Narchinol B works by
inhibiting proinflammatory mediators, including prostaglandin E2 (PGE2),
inducible nitric oxide synthase (iNOS), and cyclooxygenase-2 (COX-2) proteins,
as well as proinflammatory cytokines, such as interleukin-1b, IL-6, and tumor
necrosis factor-α (TNF-α). Narchinol B significantly inhibits LPS-induced
overproduction of NO in BV2 cells (IC50=2.43 μM)
.
|
-
- HY-155721
-
|
22-(4′-Pyridinecarbonyl) jorunnamycin A
|
Akt
mTOR
|
Cancer
|
|
22-(4′-py)-JA is a semisynthetic derivative of junamycin A (JA) that can be isolated from the Thai blue sponge (Xestospongia sp.). 22-(4′-py)-JA has antimetastatic activity and can inhibit AKT/mTOR/p70S6K signaling. 22-(4′-py)-JA inhibits tumor cell invasion and tube formation in human umbilical vein endothelial cells (HUVEC), downregulates metalloproteinases (MMP-2 and MMP-9), hypoxia-inducible factor 1α (HIF-1α) and vascular endothelial growth factor (VEGF). 22-(4′-py)-JA has potent anticancer activity against non-small cell lung cancer (NSCLC) .
|
-
- HY-120877A
-
|
|
MARK
Salt-inducible Kinase (SIK)
AMPK
Apoptosis
|
Cancer
|
|
(R)-MRT199665 is an isomer of MRT199665 (HY-120877). MRT199665 is a potent and ATP-competitive, selective MARK/SIK/AMPK inhibitor with IC50s of 2/2/3/2 nM, 10/10 nM, and 110/12/43 nM for MARK1/MARK2/MARK3/MARK14, AMPKα1/AMPKα2, and SIK1/SIK2/SIK3, respectively. MRT199665 causes apoptosis in MEF2C-activated human acute myeloid leukemias (AML) cells. MRT199665 inhibits the phosphorylation of SIK substrate CRTC3 at S370 .
|
-
- HY-W143698
-
|
|
Bcr-Abl
c-Kit
PDGFR
|
Cancer
|
|
PDGFRα kinase inhibitor 2 (compound 1), an Imatinib (HY-15463) analogue, is a covalent and irreversible kinase inhibitor with IC50s of 6.95 μM, 2.45 μM, 1.39 μM for ABL1 wt, KIT wt, PDGFRR wt .
|
-
- HY-P1408
-
|
|
Integrin
|
Cancer
|
|
Obtustatin is a non-RGD disintegrin of 41 residues. Obtustatin can be isolated from Vipera lebetina obtusa venom. Obtustatin is a potent and selective inhibitor of the adhesion of integrin α1β1 to collagen IV. Obtustatin inhibits angiogenesis, and can be used for research of cancer .
|
-
- HY-149816
-
-
- HY-N0803
-
|
β-Myrcene
|
NF-κB
|
Others
|
|
Myrcene (β-Myrcene) is a type of aromatic compound that inhibits TNFα and NF-κB activity. Myrcene has anti-invasive action, inhibits cell cycle, and leads to cancer cell apoptosis. Myrcene has strong blood protection effect, anti-inflammation, and anti-inflammatory activity.
|
-
- HY-N1425R
-
|
|
Others
|
Metabolic Disease
|
|
Tiliroside (Standard) is the analytical standard of Tiliroside. This product is intended for research and analytical applications. Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2 μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract .
|
-
- HY-118717
-
|
|
mTOR
|
Cancer
|
|
mTOR inhibitor WYE-28 (compound 28) is a selective inhibitor of mTOR>/b< (IC50)=0.08 nM. mTOR inhibitor WYE-28 inhibits PI3Kα with an IC50 value of 6 nM. mTOR inhibitor WYE-28 shows a metabolic time (T1/2) in nude mouse microsomes of 13 min .
|
-
- HY-148043
-
|
|
Zinc Finger Protein
|
Others
|
|
Schnurri-3 inhibitor-1 is a potent schnurri-3 inhibitor which is an essential regulator of adult bone formation. Schnurri-3 inhibitor-1 can inhibit Shn3 with EF1alpha promoter in osteoblast cell line Shn3FFL with an AC50 value of 2.09 μM. Schnurri-3 inhibitor-1 can be used to research osteoporosis .
|
-
- HY-19667
-
|
DPC 333
|
TNF Receptor
|
Inflammation/Immunology
|
|
BMS-561392 is a TNF alpha-converting enzyme (TACE) inhibitor. BMS-561392 is also an ADAM17 blocker. BMS-561392 can be used for research of inflammatory bowel disease .
|
-
- HY-N0042
-
-
- HY-100398
-
|
|
PI3K
mTOR
|
Cancer
|
|
PF-04979064 is a potent and selective PI3K/mTOR dual kinase inhibitor with Kis of 0.13 nM and 1.42 nM for PI3Kα and mTOR, respectively.
|
-
- HY-N1120
-
|
(+)-Triptoquinone B
|
Interleukin Related
|
Inflammation/Immunology
|
|
Triptoquinone B ((+)-Triptoquinone B), a sesquiterpene alkaloid, is an interleukin-1 inhibitor. Triptoquinone B shows potent inhibitory activities against interleukin 1α and β releases for human peripheral mononuclear cells .
|
-
- HY-170578
-
|
|
Sirtuin
|
Neurological Disease
|
|
SIRT2-IN-17 (compound Z18) is a potent SIRT2 inhibitor. SIRT2-IN-17 reduces the expression of α-SMA and p-Smad2/3 .
|
-
- HY-109633A
-
|
|
PI3K
|
Others
|
|
PI3K-IN-18 (Compound 1) dihydrochloride is a 4-morpholino-2-phenylquinazoline derivative and an inhibitor of PI3K p110α .
|
-
- HY-P0224
-
|
fMLP; N-Formyl-MLF
|
TNF Receptor
|
Inflammation/Immunology
|
|
N-Formyl-Met-Leu-Phe (fMLP; N-Formyl-MLF) is a chemotactic peptide and a specific ligand of N-formyl peptide receptor (FPR). N-Formyl-Met-Leu-Ph is reported to inhibit TNF-alpha secretion.
|
-
- HY-N2110
-
|
|
Akt
|
Inflammation/Immunology
|
|
Phellopterin is a natural product isolated from Angelica dahurica. Phellopterin reduces TNF-alpha-induced VCAM-1 expression through regulation of the Akt and PKC pathway, which contributes to inhibit the adhesion of monocytes to endothelium .
|
-
- HY-N3643
-
-
- HY-139202
-
|
|
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-162929
-
|
|
TGF-β Receptor
|
Inflammation/Immunology
|
TP-DEA2, a predictable-release Triptolide (HY-32735) prodrug, block Bleomycin-induced pulmonary fibrosis and inflammation. TP-DEA2 significantly inhibits α-SMA production .
|
-
- HY-163830
-
|
DAD9
|
Dopamine Receptor
|
Neurological Disease
|
|
Pegasus (DAD9) is a potent dopamine receptor agonist. Pegasus shows antioxidant and anti-inflammatory properties. Pegasus inhibits α-Syn amyloid aggregation. Pegasus has the potential for the research of Parkinson’s disease .
|
-
- HY-113585
-
|
|
Endogenous Metabolite
|
Others
|
|
1,4-Dideoxy-1,4-imino-D-arabinitol hydrochloride is a naturally occurring pyrrolidine alkaloid that acts as an inhibitor of glycogen phosphorylase and α-glucosidases, and is sourced from Arachniodes standishii and Angylocalyx boutiqueanus.
|
-
- HY-168048
-
|
|
Proteasome
|
Cancer
|
|
ZINC09518833 is a α-ketoamide nonpeptidic proteasome inhibitor with an IC50 value of 12.4 μM. ZINC09518833 binds both primed and nonprimed sites of the proteasome. ZINC09518833 is promising for research of multiple myeloma (MM) .
|
-
- HY-15190
-
|
HSP-990
|
HSP
Apoptosis
|
Cancer
|
|
NVP-HSP990 is a potent, selective and orally active Hsp90 inhibitor, with IC50 values of 0.6, 0.8, and 8.5 nM for Hsp90α, Hsp90β, and Grp94, respectively.
|
-
- HY-N3431
-
|
|
Glycosidase
|
Metabolic Disease
|
|
Kaempferol-7-O-rhamnoside, isolated from Chimonanthus nitens Oliv. Leaves, is a potent α-glucosidase activity inhibitor. Kaempferol-7-O-rhamnoside has the potential for diabetes .
|
-
- HY-10403A
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
(aS)-PH-797804 is a selective p38 MAPK inhibitor with IC50 values for p38 α /β of 26 nM and 102 nM, respectively. (aS)-PH-797804 has anti-inflammatory activity .
|
-
- HY-113850
-
|
|
Aldose Reductase
|
Neurological Disease
Cancer
|
|
CPSA is a potent and competitive inhibitor against 20α-hydroxysteroid dehydrogenase (AKR1C1) with a Ki value of 0.86 nM. CPSA is promising for research of lung and endometrial cancers, premature birth and neuronal disorders .
|
-
- HY-106027
-
|
RO 31-3948
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Romazarit (RO 31-3948) is an anti-inflammatory agent with antirheumatic effect. Romazarit exhibits PPARα agonist activity. Romazarit (30 mg/kg) inhibits the development of hindpaw inflammation in an adjuvant arthritis model .
|
-
- HY-N12254
-
|
|
p38 MAPK
|
Others
|
|
Natsudaidain is a kind of polymethoxyflavone. Natsudaidain can be isolated from Citrus plants. Natsudaidain inhibits tumor necrosis factor-α and cyclooxygenase-2 production n by suppressing p38 MAPK phosphorylation on mast cells .
|
-
- HY-N14506
-
|
|
Amylases
|
Others
|
|
Gibbestatin B inhibits the expression of α-amylase induced by gibberellin in De-embryoned rice and barley (IC50 is 25-50 ppm), and has no anti-bacterial, anti-yeast and anti-fungal effects at 100 ppm .
|
-
- HY-12837
-
-
- HY-N15519
-
-
- HY-124722
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
OHM1 is an analog of HIF1α CTAD that inhibits its binding with p300/CBP. OHM1 targets CH1 domain with an affinity of 0.53 μM .
|
-
- HY-B0089A
-
|
Bay-g 5421 sulfate
|
Glycosidase
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Acarbose (BAY g 5421) sulfate, antihyperglycemic agent, is an orally active alpha-glucosidase inhibitor (IC50=11 nM). Acarbose sulfate can potentiate the hypoglycemic effects of sulfonylureas or insulin .
|
-
- HY-131616
-
|
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Ethyl α-eleostearate is isolated from the ethanolic extract of Pseudo-nitzschia australis (PAEE). The PAEE of Pseudomonas australis has anti-neuroinflammatory effects, inhibiting intracellular ROS as well as pro-inflammatory mediators and cytokines .
|
-
- HY-N8517
-
|
|
Glycosidase
Apoptosis
|
Infection
Metabolic Disease
Cancer
|
|
Malabaricone B, a naturally occurring plant phenolic, is an orally active α-glucosidase inhibitor with an IC50 of 63.7 µM. Malabaricone B has anticancer, antimicrobial, anti-oxidation and antidiabetic activities .
|
-
- HY-19498
-
|
SIM-688
|
NF-κB
|
Inflammation/Immunology
|
|
WAY-204688 is an estrogen receptor (ER-α) selective, orally active inhibitor of NF-κB transcriptional activity with an IC50 of 122 ± 30 nM for NF-κB-luciferase (NF-κB-luc) in HAECT-1 cells.
|
-
- HY-126414
-
|
|
Others
|
Inflammation/Immunology
|
|
Methylenedihydrotanshinquinone is a natural product that can be isolated from the dried root of S. miltiorrhiza. Methylenedihydrotanshinquinone has anti-inflammatory effect by inhibiting expression of TNF-α, IL-1β, and IL-8 .
|
-
- HY-15271
-
WYE-687
3 Publications Verification
|
mTOR
PI3K
|
Cancer
|
|
WYE-687 is an ATP-competitive mTOR inhibitor with an IC50 of 7 nM. WYE-687 concurrently inhibits activation of mTORC1 and mTORC2. WYE-687 also inhibits PI3Kα and PI3Kγ with IC50s of 81 nM and 3.11 μM, respectively.
|
-
- HY-15509
-
|
CNI-1493 free base; CPSI-2364
|
Interleukin Related
TNF Receptor
p38 MAPK
|
Inflammation/Immunology
Cancer
|
|
Semapimod, an inhibitor of proinflammatory cytokine production, can inhibit TNF-α, IL-1β, and IL-6. Semapimod inhibits TLR4 signaling (IC50≈0.3 μM). Semapimod inhibits p38 MAPK and nitric oxide production in macrophages. Semapimod has potential in a variety of inflammatory and autoimmune disorders .
|
-
- HY-10172R
-
|
IKK2 Inhibitor V (Standard)
|
Reference Standards
IKK
|
Cancer
|
|
IMD-0354 (Standard) is the analytical standard of IMD-0354. This product is intended for research and analytical applications. IMD-0354 (IKK2 Inhibitor V) is a selective IKKβ inhibitor which inhibits NF-κB activity . IMD0354 inhibits TNF-α induced NF-κB transcription activity with an IC50 of 1.2 uM .
|
-
- HY-10255AR
-
|
|
VEGFR
PDGFR
IRE1
Mitophagy
Autophagy
Apoptosis
|
Cancer
|
|
Sunitinib (Standard) is the analytical standard of Sunitinib. This product is intended for research and analytical applications. Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively . Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation .
|
-
- HY-170570
-
|
|
LXR
Stearoyl-CoA Desaturase (SCD)
Fatty Acid Synthase (FASN)
|
Cancer
|
|
PFM046 is the antagonist for liver X receptor (LXR), that inhibits the activation of LXRα and LXRβ with IC50 of 2.04 μM and 1.58 μM. PFM046 inhibits the expression of SCD1 and FASN, upregulates the expression of ABCA1, and exhibits antitumor efficacy in mouse models .
|
-
- HY-114730
-
|
|
IKK
|
Inflammation/Immunology
|
|
CGA-JK3 is CGA-JK3 is an ATP-competitive inhibitor of IKKβ-catalyzed kinase activity. CGA-JK3 inhibits IκBα phosphorylation in LPS (HY-D1056) - induced RAW 264.7 cells .
|
-
- HY-P1420
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM .
|
-
- HY-172110
-
|
|
EGFR
Akt
p38 MAPK
ERK
Apoptosis
|
Cancer
|
|
Apoptosis inducer 35 (Compound 6) is a multi-targeted inhibitor, that reduces the expressions of EGFR, AKT, ERK and P38-MAPKα. Apoptosis inducer 35 inhibits the proliferation of cancer cell A549 and Jurkat, arrests the cell cycle at S phase, and induces apoptosis .
|
-
- HY-150740A
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
ODN 21595 sodium is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 sodium inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 sodium reduces the expression of CD86 and HLA-DR. ODN 21595 sodium has the potential for the research of systemic lupus erythematosus (SLE) .
|
-
- HY-161328
-
|
|
α-synuclein
|
Neurological Disease
|
|
MAO-B-IN-31 (Compound 30) is an effective and selective inhibitor of monoamine oxidase B (monoamine oxidase B). The IC50 value is 41 nM. MAO-B-IN-31 also inhibits α-syn and tau aggregation. MAO-B-IN-31 has neuroprotective activity .
|
-
- HY-N0191
-
-
- HY-134103A
-
|
2′,3′-Dideoxyguanosine 5′-triphosphate trisodium
|
DNA/RNA Synthesis
|
Others
|
|
ddGTP (2′,3′-Dideoxyguanosine 5′-triphosphate) trisodium is one of 2',3'-dideoxyribonucleoside 5'-triphosphates (ddNTPs) that acts as chain-elongating inhibitor of DNA polymerase for DNA sequencing. ddGTP trisodium acts as an inhibitor or a substrate for DNA polymerase α .
|
-
- HY-150740
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
ODN 21595 is a Guanine-Modified TLR7 and TLR9 inhibitor. ODN 21595 inhibits the release of IFN-α and IL-6 with no cytotoxic. ODN 21595 reduces the expression of CD86 and HLA-DR. ODN 21595 has the potential for the research of systemic lupus erythematosus (SLE) .
|
-
- HY-153700
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
Estrogen receptor modulator 8 (compound 4) is an orally active inhibitor of Estrogen Receptor/ERR α (IC50=0.437 nM, MCF-7 cells). Estrogen receptor modulator 8 inhibits MCF-7 cells proliferation with an IC50 value of 0.1 nM .
|
-
- HY-149431
-
|
|
HSP
Potassium Channel
|
Cancer
|
|
NDNA4 (compound 17) is a selective inhibitor of Hsp90α (IC50: 0.34 μM). NDNA4 is a permanently charged analog with low membrane permeability and low cytotoxicity against Ovcar-8 and MCF-10A ((IC50 >100 μM)). NDNA4 prevents disruption of hERG channel maturation without generating a heat shock response or causing degradation of Hsp90α-dependent client proteins .
|
-
- HY-10620
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K-IN-22 is a PI3Kα/mTOR dual kinase inhibitor. PI3K-IN-22 has IC50s of 0.9, 0.6 nM for PI3Kα and mTOR, respectively. PI3K-IN-22 can be used for the research of cancer .
|
-
- HY-111379
-
|
|
DYRK
CDK
GSK-3
|
Neurological Disease
Metabolic Disease
Cancer
|
|
EHT 5372 is a highly potent and selective inhibitor of DYRK's family kinases with IC50s of 0.22, 0.28, 10.8, 93.2, 22.8, 88.8, 59.0, 7.44, and 221 nM for DYRK1A, DYRK1B, DYRK2, DYRK3, CLK1, CLK2, CLK4, GSK-3α, and GSK-3β, respectively .
|
-
- HY-N2425R
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
|
|
Rhodiosin (Standard) is the analytical standard of Rhodiosin. This product is intended for research and analytical applications. Rhodiosin is a double inhibitor of CYP2D6 and AChE, and can be isolated from Rhodiolis rhodiolis root. The IC50 for CYP2D6 is 0.761 μM, and the Ki is 0.769 μM. Rhodiosin has antioxidant and neuroprotective activity and can regulate HIF-1α signaling pathway to protect the central nervous system
|
-
- HY-B1734
-
|
16-DPA
|
FXR
5 alpha Reductase
Cytochrome P450
Drug Intermediate
|
Cardiovascular Disease
Cancer
|
|
16-Dehydropregnenolone acetate (16-DPA), a sterols compound, is an orally active 17α-hydroxylase and 5α-reductase inhibitor. 16-Dehydropregnenolone is also a potent bile acid receptor (BAR)/farnesoid X receptor (FXR) antagonist. 16-Dehydropregnenolone hypolipidemic and anticancer effects. 16-Dehydropregnenolone acetate (16-DPA) is the drug intermediate that can be used for synthesis of Dexamethasone (HY-14648) and related other steroidal pharmacophores .
|
-
- HY-136055
-
|
VH032-C5-COOH
|
E3 Ligase Ligand-Linker Conjugates
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
|
(S,R,S)-AHPC-C5-COOH (VH032-C5-COOH) is a synthesized E3 ligase ligand-linker conjugate, contains the VH032 VHL-based ligand and a linker to form PROTACs. VH-032 is a selective and potent inhibitor of VHL/HIF-1α interaction with a Kd of 185 nM, has the potential for the study of anemia and ischemic diseases .
|
-
- HY-168205
-
|
|
HSP
Apoptosis
|
Cancer
|
|
HSP90-IN-33 (compound 24e) is a potent Hsp90 inhibitor with Kd values of ≥200, 7.3 µM for Hsp90α, Hsp90β, respectively. HSP90-IN-33 induces apoptosis and cell cycle arrest at G0/G1 phase. HSP90-IN-33 decreases the protein expression of ERα, CDK4 and Akt .
|
-
- HY-19357
-
-
- HY-110282
-
|
|
Oxidative Phosphorylation
Mitochondrial Metabolism
|
Metabolic Disease
|
|
S3QEL-2, a suppressor of superoxide production from mitochondrial complex III, potently and selectively suppresses site IIIQo superoxide production (IC50=1.7 μM). S3QEL-2 does not affect oxidative phosphorylation, and normal electron flux. S3QEL-2 inhibits HIF-1α accumulation .
|
-
- HY-14649S5
-
|
Vitamin A acid-d3; all-trans-Retinoic acid-d3; ATRA-d3
|
Isotope-Labeled Compounds
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Cancer
|
|
Retinoic acid-d3 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
|
-
- HY-N6962
-
|
|
TRP Channel
COX
Bacterial
|
Infection
Neurological Disease
Metabolic Disease
|
|
α-Spinasterol is an orally taken antagonist of transient receptor potential vanilloid 1 ( TRPV1), and it's also an inhibitor of COX-1 and COX-2, with IC50 values of 16.17 μM and 7.76 μM, respectively. α-Spinasterol exhibits antibacterial, anti-inflammatory, antidepressant, and antioxidant effects, has the ability to cross the blood-brain barrier, and can improve diabetes in mice .
|
-
- HY-W013636S3
-
|
alpha-Ketoglutaric acid-13C
|
Isotope-Labeled Compounds
Endogenous Metabolite
Tyrosinase
|
Neurological Disease
Metabolic Disease
|
|
2-Ketoglutaric acid- 13C (Alpha-Ketoglutaric acid- 13C) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-W013636S4
-
|
alpha-Ketoglutaric acid-13C2
|
Isotope-Labeled Compounds
Tyrosinase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
|
|
2-Ketoglutaric acid- 13C2 (Alpha-Ketoglutaric acid- 13C2) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-114263
-
NXT629
3 Publications Verification
|
PPAR
|
Cancer
|
|
NXT629 is a potent, selective, and competitive PPAR-α antagonist, with an IC50 of 77 nM for human PPARα, shows high selectivity over other nuclear hormone receptor, such as PPARδ, PPARγ, ERβ, GR and TRβ, IC50s are 6.0, 15, 15.2, 32.5 and >100 μM, respectively . NXT629 has potent anti-tumor activity and inhibits experimental metastasis of cancer cell in animal models .
|
-
- HY-W153897R
-
|
|
Adrenergic Receptor
|
Metabolic Disease
|
|
N-Methyltyramine (Standard) is the analytical standard of N-Methyltyramine. This product is intended for research and analytical applications. N-Methyltyramine is a protoalkaloid that can be isolated from various plant species. N-Methyltyramine is an α2-adrenoreceptor antagonist. N-Methyltyramine enhances appetite and digestion of foods by stimulating gastrin and pancreatic secretions. N-Methyltyramine can relax mouse small intestinal smooth muscle and inhibits small intestinal propulsion .
|
-
- HY-B0683S
-
-
- HY-W013636R
-
|
alpha-Ketoglutaric acid (Standard); 2-Oxoglutaric acid (Standard)
|
Reference Standards
Tyrosinase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
|
|
2-Ketoglutaric acid (Standard) (Alpha-Ketoglutaric acid (Standard)) is the analytical standard of 2-Ketoglutaric acid (HY-W013636). This product is intended for research and analytical applications. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-14649S6
-
|
Vitamin A acid-d3-1; all-trans-Retinoic acid-d3-1; ATRA-d3-1
|
Isotope-Labeled Compounds
RAR/RXR
PPAR
Endogenous Metabolite
Autophagy
|
Metabolic Disease
Cancer
|
|
Retinoic acid-d3-1 is the deuterium labeled Retinoic acid (HY-14649). Retinoic acid is a metabolite of vitamin A that plays important roles in cell growth, differentiation, and organogenesis. Retinoic acid is a natural agonist of RAR nuclear receptors, with IC50s of 14 nM for RARα/β/γ. Retinoic acid bind to PPARβ/δ with Kd of 17 nM. Retinoic acid acts as an inhibitor of transcription factor Nrf2 through activation of retinoic acid receptor alpha .
|
-
- HY-W013636S
-
|
alpha-Ketoglutaric acid-13C5
|
Isotope-Labeled Compounds
Tyrosinase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
|
|
2-Ketoglutaric acid- 13C5 (Alpha-Ketoglutaric acid- 13C5) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-114216
-
|
|
Endogenous Metabolite
|
Infection
|
|
DBPR110 is a nonstructural protein 5A (NS5A) inhibitor with inhibitory activity against hepatitis C virus (HCV). DBPR110 exhibited a 50% effective concentration (EC50) of 3.9 ± 0.9 pM and a selectivity index value of over 12,800,000 by reducing HCV1b replicon reporter expression. DBPR110 also effectively reduced the activity of HCV2a replicon with an EC50 of 228.8 pM and a selectivity index value of over 173,130. DBPR110 showed synergy with interferon alpha (IFN-α), NS3 protease inhibitors, and NS5B polymerase inhibitors. The results of DBPR110 suggest that it may be an effective small molecule inhibitor against HCV NS5A .
|
-
- HY-170656
-
|
|
PI3K
mTOR
|
Cancer
|
|
PI3K/mTOR Inhibitor-17 (compound 5nh) is a potent inhibitor of PI3K/mTOR, with the inhibitor of 0.45 and 2.9 nM for PI3Kα and mTOR, respectively. PI3K/mTOR Inhibitor-17 plays an important role in cancer research .
|
-
- HY-159957
-
|
|
Histone Acetyltransferase
Estrogen Receptor/ERR
|
|
|
BAY-184 is a selective and orally active KAT6A and KAT6B inhibitor. BAY-184 inhibits KAT6A/KAT6B activity with an IC50 of 71 nM and 83 nM. respectively BAY-184 inhibits ERα transcriptional activity. BAY-184 inhibits proliferation of diverse breast cancer subtypes, and inhibits tumor growth .
|
-
- HY-B2006S
-
|
|
Isotope-Labeled Compounds
Phosphatase
Bacterial
|
Infection
|
|
Fenvalerate-d5 is the deuterium labeled Fenvalerate. Fenvalerate is a potent protein phosphatase 2B (calcineurin) inhibitor with an IC50 of 2-4 nM for PP2B-Aα. Fenvalerate is a pyrethroid ester insecticide and acaricide .
|
-
- HY-122464S1
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
Jasmonic acid-d5 is deuterium labeled (±)-Jasmonic acid. (±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
|
-
- HY-156140
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Naa50-IN-1 (Compound 4a) is a specific N-α-Acetyltransferase 50 (Naa50) inhibitor (IC50=7 mM). Naa50-IN-1 has potential in cancer research .
|
-
- HY-B0979
-
|
α-Lobeline hydrochloride; L-Lobeline hydrochloride
|
nAChR
Dopamine Transporter
|
Neurological Disease
|
|
Lobeline (α-Lobeline) hydrochloride is a brain-penetrant nicotinic receptor agonist. Lobeline hydrochloride increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline hydrochloride is effective in smoking cessation .
|
-
- HY-13223A
-
|
CP 868596-26
|
Autophagy
PDGFR
FLT3
|
Cancer
|
|
Crenolanib benzenesulfonate is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-114009
-
-
- HY-N13184
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
Giraldoid B is an active ingredient that can be isolated from Girald Daphne Bark. Giraldoid B can inhibit LPS induced NO and b>TNF-α production in RAW264.7 and has anti-inflammatory activity .
|
-
- HY-N0906
-
-
- HY-122521
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Sootepin D (compound 6), a triterpene from the apical bud of Gardenia sootepensis, inhibits TNF-α-induced NF-κB activity with an IC50 of 8.3μM. Sootepin D has anti-inflammatory activity .
|
-
- HY-135175
-
|
|
Adrenergic Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
Phenoprolamine hydrochloride is an adrenergic α1 receptor antagonist that exhibits potent antihypertensive effects. Phenoprolamine hydrochloride demonstrates neuroprotective and cardioprotective properties. Phenoprolamine hydrochloride inhibits CYP2D and CYP3A activities while down-regulating their mRNA transcription.
|
-
- HY-108647
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation .
|
-
- HY-B1423
-
|
α-Lobeline; L-Lobeline
|
nAChR
Dopamine Transporter
|
Neurological Disease
|
|
Lobeline (α-Lobeline) is a brain-penetrant nicotinic receptor agonist. Lobeline increases dopamine (DA) release by inhibiting DA uptake into synaptic vesicles, and altering presynaptic DA storage. Lobeline is effective in smoking cessation .
|
-
- HY-13223
-
|
CP-868596
|
FLT3
PDGFR
Autophagy
|
Cancer
|
|
Crenolanib is a potent and selective inhibitor of wild-type and mutant isoforms of the class III receptor tyrosine kinases FLT3 and PDGFRα/β with Kds of 0.74 nM and 2.1 nM/3.2 nM, respectively.
|
-
- HY-P1453
-
|
|
STAT
|
Cancer
|
|
CMD178 is a lead peptide that consistently reduced the expression of Foxp3 and STAT5 induced by IL-2/s IL-2Rα signaling and inhibits Treg cell development .
|
-
- HY-P1872
-
|
|
Bacterial
|
Infection
|
|
OV-1, sheep is an alpha-helical antimicrobial ovispirin peptide derived from SMAP29 peptide (sheep), which inhibits several antibiotic-resistant bacterial strains including mucoid and nonmucoid Pseudomonas aeruginosa .
|
-
- HY-122464S2
-
|
|
Isotope-Labeled Compounds
|
Others
|
|
(±)-Jasmonic acid-d5 is the deuterium labeled (±)-Jasmonic acid. (±)-Jasmonic acid is a plant growth regulator and a derivative of α-linolenic acid. (±)-Jasmonic acid decreases chlorophyll levels in green and etiolated barley leaf segments and inhibits elongation of rice seedlings.
|
-
- HY-148711
-
-
- HY-N1470R
-
|
|
Others
|
Metabolic Disease
|
|
Plantagoside (Standard) is the analytical standard of Plantagoside. This product is intended for research and analytical applications. Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM .
|
-
- HY-135808
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
BIZ 114 (Example 11) is a fatty acid derivative and potent inhibits the TNF-α activated NF-κΒ pathway. BIZ 114 has the potential to prevent and / or treat ophthalmic disorders such as retinal degenerative disorders and ocular inflammatory diseases .
|
-
- HY-100211
-
TAPI-2
4 Publications Verification
TNF Protease Inhibitor 2
|
MMP
SARS-CoV
|
Cancer
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TAPI-2 (TNF Protease Inhibitor 2) is a broad-spectrum inhibitor of matrix metalloprotease (MMP), tumour necrosis factorα-converting enzyme (TACE) and a disintegrin and metalloproteinase (ADAM), with an IC50 of 20 μM for MMP . TAPI-2 blocks the entry of infectious SARS-CoV .
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- HY-12085R
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![Lactalbumin B (50-53) Alpha [Lactorphin Alpha], bovine](http://file.medchemexpress.com/product_pic/hy-p3976.gif)
