Search Result
Results for "
submicromolar
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-128207
-
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Orphan Receptor
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Cancer
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SID7970631, as an isoquinolinone analog, is a potent and selective submicromolar SF-1 inhibitor (IC50=255 nM). SID7970631 can be used for the research of cancer .
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- HY-144290
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GSK-3
DYRK
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Neurological Disease
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ARN25068 is a sub-micromolar inhibitor of the three protein kinases, GSK-3β, FYN and DYRK1A to tackle tau hyperphosphorylation .
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- HY-U00037
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PLA 725
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Phospholipase
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Inflammation/Immunology
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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.
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- HY-111192
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IPR-803
2 Publications Verification
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Ser/Thr Protease
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Cancer
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IPR-803 is a potent inhibitor of the uPAR·uPA protein-protein interaction (PPI). IPR-803 binds directly to uPAR with sub-micromolar affinity. IPR-803 displays anti-tumor activity .
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- HY-132905
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Parasite
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Infection
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Antileishmanial agent-2 shows submicromolar antileishmanial activity (IC50 = 0.29 μM) and a very high selectivity index with respect to mammalian cells.
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- HY-N8857
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Reactive Oxygen Species
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Others
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Parvifolixanthone A is a xanthone compound that can be isolated from Garcinia parvifolia. Parvifolixanthone A exhibits antioxidant activity with IC50 of submicromolar level (0.18–0.38 μM) .
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- HY-139823A
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Histone Methyltransferase
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Others
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PRMT5-IN-11 is a promising structure-dependent inhibition of the protein methyltransferase PRMT5:MEP50 complex in the (sub)micromolar range.
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- HY-157728
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E1/E2/E3 Enzyme
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Inflammation/Immunology
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ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research .
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- HY-168262
-
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Parasite
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Infection
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Antitrypanosomal agent 22 (compound 13) is a nitrothienylazine compound with trypanosomaticidal efficacy. Antitrypanosomal agent 22 shows leishmanicidal and trypanocidal with in vitro submicromolar activities, and devoid of toxicity on mammalian cells are uncovered .
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- HY-P3426
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Beta-secretase
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Cancer
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BACE1-IN-10 is a potent BACE1 Inhibitor. BACE1-IN-10 shows sub-micromolar activity against recombinant BACE1 (rBACE1) .
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- HY-141844
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HDAC
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Cancer
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HDAC/BET-IN-1 displays submicromolar inhibitory activity against HDAC1 and 6 (IC50 = 0.163 μM and 0.067 μM), and BRD4 (Ki = 0.076 μM), and possess potent antileukemia activity.
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- HY-16662
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Ras
Apoptosis
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Cancer
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Oncrasin-1 is a potent and effective anticancer inhibitor that kills various human lung cancer cells with K-Ras mutations at low or submicromolar concentrations; also led to abnormal aggregation
of PKCι in nucleus of sensitive cells but not in resistant cells.
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- HY-121647
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Parasite
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Others
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Nopol is a quinoline derivative based on nopol that has inhibitory activity against the asexual blood stage of Plasmodium falciparum. Derivatives with different structures have different activities against different Plasmodium strains, and some derivatives have submicromolar EC50 values in specific strains.
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- HY-15611
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CRM1
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Cancer
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KPT-185 is an orally bioavailable and selective inhibitor of CRM1 and displays potent antiproliferative properties at submicromolar concentrations (IC50=100-500 nM), induces apoptosis, cell-cycle arrest, and myeloid differentiation in AML cell lines and patient blasts .
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- HY-139364
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PGE synthase
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Others
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mPGES1-IN-4 (compound 32) is a polysubstituted pyrimidine compound and a submicromolar PGE2 production inhibitor. It exerts its anti-inflammatory effect mainly by inhibiting mPGES-1 and has a significant inhibitory effect on the acute inflammation model in vivo.
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- HY-139365
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PGE synthase
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Others
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mPGES1-IN-5 (compound 18) is a polysubstituted pyrimidine compound and a submicromolar PGE2 production inhibitor. It exerts its anti-inflammatory effect mainly by inhibiting mPGES-1 and has a significant inhibitory effect on the acute inflammation model in vivo.
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- HY-113734
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Others
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Others
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CM026 is a selective aldehyde dehydrogenase 1A1 inhibitor with submicromolar inhibitory activity against aldehyde dehydrogenase 1A1. Its inhibitory mechanism is related to binding to the aldehyde binding pocket and utilizing a unique glycine residue. It can be used as a chemical tool to study the role of this enzyme in disease.
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- HY-146702
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Bacterial
Thymidylate Synthase
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Infection
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MtTMPK-IN-8 (compound 27) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor. MtTMPK-IN-8 has sub-micromolar activity against mycobacteria (MICs = 0.78~9.4 μM) without significant cytotoxicity. MtTMPK-IN-8 can be used for researching tuberculosis .
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- HY-146703
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Bacterial
Thymidylate Synthase
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Infection
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MtTMPK-IN-9 (compound 28) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 48 μM. MtTMPK-IN-9 has sub-micromolar activity against mycobacteria (MICs = 6.25~9.4 μM) without significant cytotoxicity. MtTMPK-IN-9 can be used for researching tuberculosis .
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- HY-146701
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Bacterial
Thymidylate Synthase
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Infection
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MtTMPK-IN-7 (compound 26) is a moderate M. tuberculosis thymidylate kinase (MtbTMPK) inhibitor with an IC50 value of 47 μM. MtTMPK-IN-7 has sub-micromolar activity against mycobacteria (MICs = 2.3~4.7 μM) without significant cytotoxicity. MtTMPK-IN-7 can be used for researching tuberculosis .
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- HY-10844
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Pretomanid
Maximum Cited Publications
6 Publications Verification
PA-824; (S)-PA 824
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Bacterial
Antibiotic
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Infection
Cancer
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Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
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- HY-12993
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RSV604
2 Publications Verification
A-60444
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RSV
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Infection
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RSV604 (A-60444) is an inhibitor of respiratory syncytial virus (RSV) replication. RSV604 targets the nucleocapsid protein, with a Kd of 1.6 μM. RSV604 displays submicromolar activity against numerous clinical isolates of both the A and B subtypes of RSV (average EC50s=0.8 μM) .
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- HY-144648
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SARS-CoV
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Infection
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Mpro/PLpro-IN-1 (Compound 29) is a potent inhibitor of M pro/PL pro. Mpro/PLpro-IN-1 is a dual acting SARS-CoV-2 proteases inhibitor featuring micromolar inhibitory potency versus M pro (IC50 = 1.72 μM) and submicromolar potency versus PL pro (IC50 = 0.67 μM) .
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- HY-170313
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GLUT
Apoptosis
Reactive Oxygen Species
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Cancer
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GLUT-1-IN-4 (Compound 13) is the p53 protein-dependent inhibitor for GLUT-1 glucose transporter. GLUT-1-IN-4 inhibits the proliferation of multiple cancer cells with IC50 in submicromolar levels. GLUT-1-IN-4 arrests the cell cycle, stimulates oxidative stress, and induces apoptosis .
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- HY-133119
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Bacterial
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Infection
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PK150, an analogue of Sorafenib, shows oral bioavailability and antibacterial activity against several pathogenic strains at submicromolar concentrations. PK150 inhibits Gram-positive Methicillin-sensitive S. aureus (MSSA), Methicillin-resistant S. aureus (MRSA), Vancomycin intermediate S. aureus (VISA) with MICs of 0.3, 0.3-1, 0.3 μM, respectively .
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- HY-10844S
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Isotope-Labeled Compounds
Bacterial
Antibiotic
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Infection
Cancer
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Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL[1][2].
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- HY-10844S1
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PA-824-d5; (S)-PA 824-d5
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Antibiotic
Bacterial
Isotope-Labeled Compounds
|
Infection
Cancer
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Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
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- HY-10844R
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Bacterial
Antibiotic
|
Infection
Cancer
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Pretomanid (Standard) is the analytical standard of Pretomanid. This product is intended for research and analytical applications. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
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- HY-128341
-
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ERK
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Cardiovascular Disease
Cancer
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ERK5-IN-2 is an orally active, sub-micromolar, selective ERK5 inhibitor with IC50s of 0.82 μM, 3 μM for ERK5 and ERK5 MEF2D, respectively. ERK5-IN-2 does not interact with the BRD4 bromodomain. ERK5-IN-2 suppresses both tumor xenograft growth and basic fibroblast growth factor (bFGF) driven Matrigel plug angiogenesis .
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- HY-126250
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Phosphodiesterase (PDE)
Parasite
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Infection
Inflammation/Immunology
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NPD1335 is a Trypanosoma brucei phosphodiesterase B1 (TbrPDEB1) inhibitor with submicromolar activities against T. brucei parasites. NPD1335 displays a greatly improved cytotoxicity profile. NPD1335 increases intracellular cAMP levels and results in the distortion of the cell cycle and cell death . NPD-1335 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-161732
-
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Bcl-2 Family
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Cancer
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GQN-B37-E is a potent selective binder and inhibitor of MCL-1. GQN-B37-E binds to the BH3-domain-binding pocket in MCL-1. GQN-B37-E exhibits binding affinity for MCL-1 at the submicromolar range (Ki = 0.6 μM) without apparent binding to BCL-2 or BCL-XL .
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- HY-124388
-
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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PDE4-IN-20 is a selective submicromolar phosphodiesterase-4 (PDE4) inhibitor with anti-TNF-α properties. PDE4-IN-20 exhibits significant biological activity in vitro and in vivo. The mechanism of action of PDE4-IN-20 is supported by molecular modeling studies, which reveal its binding mode with PDE4. PDE4-IN-20 was optimized in further conformational analysis and showed pharmacological characteristics similar to those of known PDE4 inhibitors .
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- HY-161356
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SARS-CoV
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Infection
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BPR3P0128 is an orally active, non-nucleoside RNA-dependent RNA polymerase (RdRp) inhibitor that has been shown to inhibit the activity of various SARS-CoV-2 variants. The EC50 for SARS-CoV-2 and HCoV-229E are 0.62 µM and 0.14 µM. BPR3P0128 demonstrates effective anti-pancoronavirus activity within the submicromolar range. PR3P0128 shows synergistic antiviral activity when combined with Remdesivir (HY-104077) .
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- HY-163746
-
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Cholinesterase (ChE)
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Neurological Disease
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BuChE-IN-11 (Compound 3b-1) is an selective BuChE inhibitor with an IC50 of 0.44 μM for hBuChE. BuChE-IN-11 has high blood-brain barrier permeability and exhibits strong antioxidant activity due to its free radical scavenging properties. BuChE-IN-11 interacts with the choline binding site, acetyl binding site, and peripheral anionic site, exhibiting submicromolar BuChE inhibitory activity and preventing β-amyloid (Aβ) self-aggregation. BuChE-IN-11 holds promise for research in the field of Alzheimer's disease .
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- HY-153738
-
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ERK
|
Cancer
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ERK1/2 inhibitor 9 (Probe 1) is a covalent ERK1/2 inhibitor. ERK1/2 inhibitor 9 shows sub-micromolar activity in cells (A375 GI50=0.47 μM). ERK1/2 inhibitor 9 causes the downregulation of phospho-ERK1/2. ERK1/2 inhibitor 9 tagged trans-cyclo-octene (TCO) and Tz-Thalidomide (tetrazine tagged Thalidomide) can form the corresponding ERK-CLIPTAC to elicit degradation of ERK1/2 .
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- HY-120072
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PF-74
|
HIV
|
Infection
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PF-3450074 (PF-74) is a specifical inhibitor of?HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle . CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
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- HY-118607
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Potassium Channel
Parasite
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Infection
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VU041 is a first submicromolar-affinity inhibitor of Anopheles (An.) gambiae and Aedes (Ae.) aegypti inward rectifier potassium 1 (Kir1) channels with IC50 values of 2.5?μM and 1.7?μM, respectively. VU041 inhibits appreciably is mammalian Kir2.1 (IC50 of 12.7?μM), and has less inhibitory effect on mammalian Kir1.1, Kir4.1, Kir6.2/SUR1, and Kir7.1. VU041 also induces impaired Malpighian tubule function .
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-
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- HY-112363
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RP107
|
CDK
GSK-3
ERK
JNK
CFTR
|
Inflammation/Immunology
Cancer
|
Aloisine A (RP107) is a a potent cyclin-dependent kinase (CDK) inhibitor with IC50s of 0.15 μM, 0.12 μM, 0.4 μM, 0.16 μM for CDK1/cyclin B, CDK2/cyclin A, CDK2/cyclin E, CDK5/p35, respectively. Aloisine A ininhibits GSK-3α (IC50=0.5 μM) and GSK-3β (IC50=1.5 μM). Aloisine A stimulates wild-type CFTR and mutated CFTR, with submicromolar affinity by a cAMP-independent mechanism. Aloisine A has the potential for CFTR-related diseases, including cystic fibrosis research .
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Cat. No. |
Product Name |
Type |
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- HY-157013
-
|
Fluorescent Dyes/Probes
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UR-MB-355, a GPR3 ligand, binds to GPR3 and closely related receptors, GPR6 and GPR12, with similar submicromolar affinities .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3426
-
|
Beta-secretase
|
Cancer
|
BACE1-IN-10 is a potent BACE1 Inhibitor. BACE1-IN-10 shows sub-micromolar activity against recombinant BACE1 (rBACE1) .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
-
- HY-10844S
-
|
Pretomanid-d4 is the deuterium labeled Pretomanid. Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL[1][2].
|
-
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- HY-10844S1
-
|
Pretomanid-d5 is deuterated labeled Pretomanid (HY-10844). Pretomanid (PA-824) is an antibiotic used for the research of multi-drug-resistant tuberculosis affecting the lungs. Pretomanid exhibits a sub-micromolar MIC against M. tuberculosis (MTB). The MIC values of PA-824 against a panel of MTB pan-sensitive and Rifampin mono-resistant clinical isolates range from 0.015 to 0.25 μg/mL.
|
-
Cat. No. |
Product Name |
|
Classification |
-
- HY-168262
-
|
|
Alkynes
|
Antitrypanosomal agent 22 (compound 13) is a nitrothienylazine compound with trypanosomaticidal efficacy. Antitrypanosomal agent 22 shows leishmanicidal and trypanocidal with in vitro submicromolar activities, and devoid of toxicity on mammalian cells are uncovered .
|
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