Search Result
Results for "
Alpha reductase Inhibitors
" in MedChemExpress (MCE) Product Catalog:
2177
Inhibitors & Agonists
13
Biochemical Assay Reagents
89
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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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 estrogen-related receptor α (ERRα) antagonist. 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. ERRα antagonist-1 does not inhibit the interaction of either ERRβ or ERRγ with PGC-1α and PGC-1β coactivator, and also does not inhibit interaction of ERα or ERβ with PGC-1α or SRC-1 .
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-
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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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-
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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-163519
-
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α-synuclein
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Neurological Disease
|
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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-
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- HY-149509
-
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α-synuclein
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Neurological Disease
|
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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-
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- HY-147644
-
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Others
|
Neurological Disease
|
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-157308
-
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α-synuclein
|
Neurological Disease
|
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-153329
-
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TNF Receptor
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Others
|
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
-
|
EBV
|
Infection
Cancer
|
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
-
-
-
- HY-149331
-
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TNF Receptor
Caspase
NF-κB
|
Inflammation/Immunology
|
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-152552
-
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α-synuclein
|
Neurological Disease
|
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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-
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- HY-D2360
-
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HIF/HIF Prolyl-Hydroxylase
HSP
|
Cancer
|
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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-
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- HY-157806
-
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α-synuclein
|
Neurological Disease
|
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-149635
-
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HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
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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-
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- HY-163145
-
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α-synuclein
|
Neurological Disease
|
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-14571
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E7820
4 Publications Verification
ER68203-00
|
Molecular Glues
Integrin
|
Cancer
|
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-110266
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GN44028
5 Publications Verification
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
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-136735
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IRE1
|
Neurological Disease
Cancer
|
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
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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-N8459
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α-CBD
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EBV
|
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-119593
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-
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- HY-129434A
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Bacterial
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Infection
|
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-160433
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- HY-161469
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-
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- HY-111507
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PDGFR
|
Cancer
|
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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-
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- HY-151341
-
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HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
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-101491
-
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PGC-1α
Autophagy
|
Metabolic Disease
|
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-148862
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Calcium Channel
Monoamine Transporter
|
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-148863
-
|
Calcium Channel
Monoamine Transporter
|
Inflammation/Immunology
|
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-18509
-
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IRE1
|
Cancer
|
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-162799
-
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Others
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Cancer
|
ChoKα inhibitor-6 (compound Fa22) is a less specific ChoKα1 inhibitor with antitumor activity .
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- HY-162800
-
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Others
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Cancer
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ChoKα inhibitor-7 (compound PL48) is a less specific ChoKα1 inhibitor with antitumor activity .
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- HY-15438
-
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GSK-3
Apoptosis
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Metabolic Disease
|
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
|
Reactive Oxygen Species
ATP Synthase
mTOR
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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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- HY-N10330
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HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
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
-
|
Glucosidase
Amylases
Cholinesterase (ChE)
|
Neurological Disease
Metabolic Disease
|
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-148264
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-
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- HY-13671
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HIF-1α inhibitor; LW8
|
HIF/HIF Prolyl-Hydroxylase
Apoptosis
|
Cancer
|
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-114423
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-
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- HY-19949
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-
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- HY-163598
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-
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- HY-124079
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-
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- HY-146225
-
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Glucosidase
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Metabolic Disease
|
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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-
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- HY-149085
-
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RAR/RXR
|
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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-
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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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-
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- HY-149081
-
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Estrogen Receptor/ERR
Cytochrome P450
|
Cancer
|
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-152193
-
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Others
|
Cancer
|
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-111387
-
-
- HY-153002
-
-
- HY-161293
-
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p38 MAPK
|
Cancer
|
p38-α MAPK-IN-6 (compound 3a) is a p38α mitogen-activated protein kinase inhibitor .
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- HY-162368
-
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Phospholipase
|
Others
|
cPLA2α-IN-2 (Compound 122) is an inhibitor of cytosolic phospholipase A2α (cPLA2α) .
|
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- HY-163597
-
-
- HY-163599
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-
- HY-163600
-
-
- HY-163601
-
-
- HY-163602
-
-
- HY-163603
-
-
- HY-18371
-
|
HIF/HIF Prolyl-Hydroxylase
|
Inflammation/Immunology
|
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-147711
-
|
Glucosidase
|
Metabolic Disease
|
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-163439
-
|
Amylases
Glucosidase
|
Metabolic Disease
|
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-18370
-
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
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-161522
-
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Glucosidase
Carbonic Anhydrase
|
Endocrinology
|
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-P5881
-
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PKC
|
Cardiovascular Disease
|
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-162286
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-
- HY-162287
-
-
- HY-14929A
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GR181413A
|
Others
|
Others
|
Migalastat hydrochloride (GR181413A) is a potent and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A.
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- 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 .
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- HY-112535
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-
- HY-B0141AS
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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.
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- HY-145418
-
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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 .
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- 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 .
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-
- HY-145420
-
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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 .
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- HY-125840
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PT2977; MK-6482
|
HIF/HIF Prolyl-Hydroxylase
|
Cancer
|
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
-
|
IRE1
|
Cancer
|
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
|
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.
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- HY-N1820
-
-
- HY-153330
-
-
- HY-N8745
-
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Fungal
|
Others
|
α-Peltatin is an aryl lignan. α-Peltatin has anticancer and antifungal activity. α-Peltatin inhibits DNA topoisomerase and tubulin polymerization .
|
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- HY-N0127
-
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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.
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-
- HY-162634
-
|
Amylases
Glucosidase
|
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-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 .
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-
- HY-163840
-
|
Others
|
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. GFRα2/3-IN-1 can be used to study pain and itch .
|
-
- HY-154972
-
|
Glucosidase
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
-
|
Glucosidase
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-155241
-
|
Glucosidase
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-156380
-
|
Amylases
Glucosidase
|
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-162673
-
|
Amylases
Glucosidase
|
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-100735
-
-
- HY-107532
-
NN-DNJ; Nonyl-DNJ
|
Glucosidase
|
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-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-147669
-
|
Others
|
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-147666
-
|
Others
|
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-147667
-
|
Others
|
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-147668
-
|
Others
|
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-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-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-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-B0141AS1
-
-
- HY-161355
-
|
Amylases
Glucosidase
|
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-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-155344
-
|
Glucosidase
|
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-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
Glucosidase
|
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-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-142618
-
-
- 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-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-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-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 .
|
-
- HY-148860
-
|
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-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-162169
-
|
Amylases
Glucosidase
|
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-162390
-
|
Amylases
Glucosidase
|
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-70073
-
-
- HY-12867
-
-
- HY-U00376
-
-
- HY-142659
-
|
IRE1
|
Cancer
|
IRE1α kinase-IN-6 is a potent IRE1α inhibitor with an IC50 value of 4.4 nM.
|
-
- HY-146752
-
|
Others
|
Others
|
α-Amylase-IN-1 is a potent α-amylase inhibitor with an IC50 of 4.46 μM .
|
-
- HY-146424
-
-
- HY-157537
-
-
- HY-14929
-
GR181413A free base
|
Others
|
Others
|
Migalastat (GR181413A free base) is an orally active and competitive inhibitor of α-galactosidase A (α-Gal A) with an IC50 of 0.04 μM for human α-Gal A .
|
-
- 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-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-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-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-149668
-
|
Glucosidase
|
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-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-161764
-
|
Amylases
Glucosidase
|
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-115978
-
|
Glucosidase
|
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-N11512
-
|
Glucosidase
|
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-155372
-
|
Glucosidase
|
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-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-160434
-
-
- 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-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-B0141A
-
-
- HY-146156
-
-
- HY-150960
-
-
- HY-P99148
-
-
- HY-12710
-
α-Yohimbine; Corynanthidine; Isoyohimbine
|
Adrenergic Receptor
|
Cancer
|
Rauwolscine is a selective α2-adrenoceptor antagonist that inhibits tumor growth and induces apoptosis .
|
-
- HY-P99782
-
-
- 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-149579
-
|
Glucosidase
|
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-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-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-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-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-124647
-
|
PI3K
|
Cancer
|
PI3Kα-IN-1 is a PI3Kα inhibitor (IC50 < 0.5 nM), and also inhibits mTOR (IC50: 104 nM) .
|
-
- 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-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
-
|
Others
|
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-147823
-
|
Glucosidase
|
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-157488
-
|
Glucosidase
|
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
-
|
Glucosidase
|
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-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-150560
-
|
Glucosidase
|
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-107371
-
NSC95682
|
IRE1
|
Cancer
|
6-Bromo-2-hydroxy-3-methoxybenzaldehyde (NSC95682) is an IRE-1α inhibitor with an IC50 of 0.08 μM, extracted from patent WO 2008154484 A1, IRE-lα inhibitor compound 3-5.
|
-
- 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-B0194A
-
-
- HY-B0194
-
-
- HY-111376
-
-
- 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-150959
-
-
- HY-150961
-
-
- HY-162262
-
-
- HY-162395
-
-
- 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-N11477
-
|
Glucosidase
|
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-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-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-113038AS
-
2-Hydroxyglutarate-13C5 disodium; 2-Hydroxyglutaric acid-13C5 sodium; 2-Hydroxypentanedioic acid-13C5 disodium
|
Histone Demethylase
Endogenous Metabolite
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Cancer
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α-Hydroxyglutaric acid- 13C5 (sodium) is the 13C labeled α-Hydroxyglutaric acid sodium[1]. 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[2].
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- HY-147718
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Glutaminase
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Metabolic Disease
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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 .
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- HY-151142
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Glucosidase
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Metabolic Disease
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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 .
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- HY-156576
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DGK
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Cancer
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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.
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- HY-156577
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DGK
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Cancer
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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.
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- HY-121615
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Alpha-Phellandrene
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Fungal
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Infection
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α-Phellandrene (alpha-Phellandrene) has antifungal activity. α-Phellandrene significantly inhibits the hyphal growth of P. cyclopium, destroys their cell membrane integrity and causes leakage of cellular components .
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- HY-160435
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TNF Receptor
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Inflammation/Immunology
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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) .
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- HY-N12399
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PKA
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Inflammation/Immunology
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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 .
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- HY-113062
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20-OH-P
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Endogenous Metabolite
Cytochrome P450
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Endocrinology
Cancer
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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 .
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- HY-113038A
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2-Hydroxyglutarate disodium; 2-Hydroxyglutaric acid disodium; 2-Hydroxypentanedioic acid disodium
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Histone Demethylase
Endogenous Metabolite
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Cancer
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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 .
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- HY-157489
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Glucosidase
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Metabolic Disease
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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. .
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- HY-156406
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PI3K
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Inflammation/Immunology
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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 .
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- HY-147100
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PROTACs
Adrenergic Receptor
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Cancer
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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 .
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- HY-112275
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- HY-132179
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- HY-115746
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- HY-147879
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- HY-153915
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PI3K
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Cancer
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PI3Kα-IN-11 is a potent PI3Kα inhibitor with anticancer activity .
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- HY-156447
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Glucosidase
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Metabolic Disease
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α-Glucosidase-IN-40 (compound 5) is a noncompetitive α-glucosidase enzyme inhibitor with an IC50 of 24.62 μM .
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- HY-160458
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PI3K
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Others
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PI3Kα-IN-17 (example 4) is a potent inhibitor of PI3Kα .
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- HY-163361
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PI3K
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Cancer
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PI3Kα-IN-20 (compound 2) is a selective PI3Kα inhibitor .
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- HY-147964
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Glucosidase
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Metabolic Disease
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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 .
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- HY-147965
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Glucosidase
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Metabolic Disease
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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 .
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- HY-151141
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Glucosidase
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Metabolic Disease
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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 .
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- HY-151135
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Glucosidase
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Metabolic Disease
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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 .
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- HY-18510
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IRE1
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Others
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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 .
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- HY-160027
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TNF Receptor
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Inflammation/Immunology
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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 .
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- HY-129348
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IRE1
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Cancer
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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 .
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- HY-113038AS1
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2-Hydroxyglutarate-d4 disodium; 2-Hydroxyglutaric acid-d4 disodium; 2-Hydroxypentanedioic acid-d4 disodium
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Histone Demethylase
Endogenous Metabolite
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Cancer
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α-Hydroxyglutaric acid-d4 (disodium) is the deuterium labeled α-Hydroxyglutaric acid disodium[1]. 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[2].
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- HY-118694
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- HY-164259
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-148575
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Glucosidase
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Metabolic Disease
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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 .
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- HY-12836A
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IFNAR
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Inflammation/Immunology
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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) .
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- HY-149000
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PI3K
Apoptosis
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Cancer
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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 .
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- HY-N4155
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EBV
HIV Protease
HSV
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Infection
Cancer
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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 .
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- HY-144699
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Estrogen Receptor/ERR
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Cancer
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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 .
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- HY-151465
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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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 .
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- HY-103204
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Adrenergic Receptor
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Endocrinology
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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 .
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- HY-151145
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Glucosidase
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Metabolic Disease
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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 .
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- HY-151143
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Glucosidase
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Metabolic Disease
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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 .
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- HY-151144
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Glucosidase
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Metabolic Disease
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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 .
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- HY-157311
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Glucosidase
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Cancer
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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 .
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- HY-N12664
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Glucosidase
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Metabolic Disease
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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 .
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- HY-158697
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Glucosidase
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Metabolic Disease
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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 .
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- HY-162599
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TNF Receptor
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Infection
Cancer
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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) .
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- HY-163862
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- HY-161944
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Amylases
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Metabolic Disease
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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 .
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- HY-169251
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- HY-N1064
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nAChR
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Neurological Disease
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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) .
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- HY-P99721
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ABT-981
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Interleukin Related
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Inflammation/Immunology
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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 .
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- HY-153474
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IRE1
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Others
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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) .
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- HY-163066
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Glucosidase
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Metabolic Disease
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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 .
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- HY-163360
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PI3K
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Cancer
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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 .
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- HY-161999
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Glucosidase
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Metabolic Disease
Inflammation/Immunology
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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 .
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- HY-19763
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PI3Kα inhibitor 1
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PI3K
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Cancer
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BEBT-908 (PI3Kα inhibitor 1) 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) .
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- HY-N8847R
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Hippo (MST)
YAP
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Cancer
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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 .
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