Search Result
Results for "
Reversible inhibitor
" in MedChemExpress (MCE) Product Catalog:
4
Biochemical Assay Reagents
39
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-126388
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- HY-124346
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Others
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Metabolic Disease
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T-3364366 is a reversible, slow-binding, thienopyrimidinone delta-5 desaturase (D5D) inhibitor with IC50s of 1.9 nM and 2.1 nM in HepG2 and RLN-10 cells, respectively. T-3364366 exhibits potent D5D (IC500=19 nM) inhibitory activity and excellent selectivity away from delta-6 desaturase (D6D, IC50=6200 nM) and delta-9 desaturase (stearoyl-CoA desaturase, SCD,50 >10000 nM) in the enzymatic activity assay .
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- HY-149527
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- HY-157778
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SARS-CoV
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Infection
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MK-7845 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 of 8.7 nM .
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-
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- HY-149595
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Histone Demethylase
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Cancer
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LSD1-UM-109 is a ighly potent and reversible LSD1 inhibitor with an IC50 of 3.1 nM. LSD1-UM-109 inhibits cell growth with IC50 values of 0.6 nM in the MV4;11 acute leukemia cell line and 1.1 nM in the H1417 small-cell lung cancer cell line .
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- HY-145373
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Btk
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Inflammation/Immunology
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BMS-986143 is an orally active, reversible BTK inhibitor with an IC50 of 0.26 nM. BMS-986143 also inhibits TEC, BLK, BMX, TXK FGR, YES1, ITK with IC50s of 3 nM, 5 nM, 7 nM, 10 nM, 15 nM,19 nM, 21 nM, respectively. BMS-986143 can be used for the research of autoimmune diseases .
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- HY-161066
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Ras
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Cancer
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KRAS G13D-IN-1 (compound 41) is a selective and covalently reversible inhibitor of KRAS G13D (IC50: 0.41 nM). The selectivity for KRAS G13D is 29-fold against KRAS wild type. KRAS G13D-IN-1 is an inhibitor of the GDP state and targets the SWII binding pocket of KRAS G13D. KRAS G13D-IN-1 inhibits KRAS binding to GDP and turns on/off downstream signaling cascades .
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- HY-N13041
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Monoamine Oxidase
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Neurological Disease
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Acacetin 7-O-(6-O-malonylglucoside) is a monoamine oxidase inhibitor with strong inhibitory effects on monoamine oxidase A (MAO-A) and monoamine oxidase B (MAO-B) with IC50 values of 2.34 and 1.87 μM, respectively. Acacetin 7-O-(6-O-malonylglucoside) is a reversible MAO inhibitor that can be used in the research of neurodegenerative diseases and affective disorders .
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- HY-115902
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FGFR
Apoptosis
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Cancer
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FGFR4-IN-7 (Compound C3) is a covalent reversible FGFR4 inhibitor with an IC50 value of 0.42 μM. FGFR4-IN-7 induces apoptosis via the FGFR4 signaling pathway blockage. FGFR4-IN-7 can be used for the research of hepatocellular carcinoma (HCC) .
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- HY-16731
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EVT 302; RG1577; RO4602522
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Monoamine Oxidase
Reactive Oxygen Species
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Neurological Disease
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Sembragiline (EVT 302) is a potent, selective and reversible monoamine oxidase B (MAO-B) inhibitor. Sembragiline reduces the metabolism of dopamine and other amine neurotransmitters by inhibiting the activity of the MAO-B enzyme, thereby potentially increasing the concentration of these neurotransmitters in the brain. Inhibition of the MAO-B enzyme also reduces the formation of toxic reactive oxygen species (ROS) that play a role in the pathological process of AD. Sembragiline has good oral activity and blood-brain barrier permeability. Sembragiline can be used in studies of AD, especially in patients with AD who show increased MAO-B activity .
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- HY-132831
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Somalix; RO-7486967; IZD334
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NOD-like Receptor (NLR)
Interleukin Related
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Neurological Disease
Inflammation/Immunology
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Selnoflast (RO7486967), formerly somalix/RG6418/IZD334, is an orally active, potent, selective and reversible small molecule NLRP3 inflammasome inhibitor. Selnoflast is a potent inhibitor of IL-1β release stimulated by NLRP3 activation in human Alzheimer's disease (AD) monocyte-derived macrophages. Selnoflast is promising for research of AD and systemic inflammatory diseases, such as ulcerative colitis and chronic obstructive pulmonary disease
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- HY-164002
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Btk
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Others
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PF-303 is a potent, oral inhibitor of Bruton's tyrosine kinase (BTK) (IC50=0.64 nM). The melamine portion of PF-303 forms a covalent bond with BTK's Cys481, which is reversible and exhibits a high selectivity compared to irreversible covalent BTK inhibitors. PF-303 can be used to model and study the effects of BTK inhibition on the mature immune system, including effects on B-cell subsets, antibody responses, and T-cell-mediated activation .
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- HY-143881
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FGFR
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Cancer
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FGFR4-IN-6 (Compound 9ka) is a covalently reversible FGFR4 inhibitor with an IC50 value of 5.4 nM. FGFR4-IN-6 also exhibits good oral pharmacokinetic properties. FGFR4-IN-6 induces significant tumor regressions in a xenograft mouse model of Hep3B2.1-7 HCC cell line without an obvious sign of toxicity . FGFR4-IN-6 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-147862
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EGFR
Apoptosis
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Cancer
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EGFR-IN-62 (compound 9h) is a potent and reversible EGFR kinase inhibitor, with IC50 values of 10 nM (L858R/T790 M), 29 nM (WT), and 242 nM (L858R/T790 M/C797S), respectively. EGFR-IN-62 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.53 and 1.56 μM, respectively. EGFR-IN-62 induces dose-dependent apoptosis process, G1/G0-phase arrestation, and the inhibition of motility on A549 and/or H1975 cell lines .
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- HY-B0882
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- HY-B1413
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- HY-B0884
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- HY-B0884A
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- HY-U00042
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- HY-14260
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- HY-N1937
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Celastrol methyl ester
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Bacterial
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Cancer
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Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.
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- HY-10836
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Parasite
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Others
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Cruzain-IN-1 is a covalent and reversible Cruzain inhibitor, with an IC50 of 10 nM.
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- HY-116290
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Squalestatin S1
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Others
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Others
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Zaragozic acid A is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase .
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- HY-103351
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- HY-70075
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RGS Protein
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Cancer
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CCG-63808 is a reversible inhibitor of regulator of G-protein signaling (RGS) proteins.
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- HY-B1206
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- HY-14196
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- HY-112465
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PKA
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Cancer
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H-8 (dihydrochloride) is a cell-permeable, reversible and ATP-competitive PKA inhibitor .
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- HY-116026
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- HY-116290A
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Squalestatin S1 trisodium
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Others
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Others
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Zaragozic acid A trisodium is a fungal metabolite that acts as a reversible competitive inhibitor of squalene synthase .
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- HY-127109A
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- HY-101769
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Dipeptidyl Peptidase
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Cancer
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UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
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- HY-18690A
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- HY-14947
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MKI 833
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MEK
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Cancer
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Balamapimod (MKI 833) is a reversible Ras/Raf/MEK inhibitor with potential anti-tumor activity.
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- HY-15723
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Ras
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Cancer
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NSC 23766 is a cell-permeable, reversible and specific inhibitor of Rac GTPase, used for cancer treatment.
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- HY-116533
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MAPKAPK2 (MK2)
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Cancer
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RMM-46 is a selective and reversible covalent inhibitor for MSK/RSK-family kinases .
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- HY-108551
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- HY-127109
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- HY-119774
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- HY-148535
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Proteasome
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Neurological Disease
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Calpain Inhibitor XI is a reversible covalent inhibitor of calpain-1. Calpain Inhibitor XI can be used for the research of neurodegenerative disorders .
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- HY-14984
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GSNOR
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Inflammation/Immunology
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N6022 is a potent, selective, reversible, and efficacious S-Nitrosoglutathione reductase(GSNOR) inhibitor with IC50 of 8 nM.
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- HY-B0207AS
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Cholinesterase (ChE)
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Others
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Pyridostigmine-d6 (bromide) is the deuterium labeled Pyridostigmine, which is a parasympathomimetic and a reversible cholinesterase inhibitor.
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- HY-100178
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- HY-112411
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EGFR
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Cancer
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PD 174265 is a potent, cell-permeable, reversible, and selective inhibitor of EGFR with an IC50 of 450 pM .
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- HY-152212
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- HY-157040
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- HY-112333
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- HY-N0918
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Demethoxyyangonin; 5,6-Dehydrokavain
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Monoamine Oxidase
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Others
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Desmethoxyyangonin is one of the six major kavalactones found in the Piper methysticum (kava) plant; reversible inhibitor of MAO-B.
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- HY-100975
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- HY-101793
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Btk
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Inflammation/Immunology
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BMS-935177 is a potent and selective reversible inhibitor of Bruton’s tyrosine kinase (Btk) with an IC50 of 3 nM.
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- HY-120868
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MetAP
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Metabolic Disease
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TP-004 is a potent and reversible inhibitor of methionine aminopeptidase 2 (MetAP2), with an IC50 of 6 nM .
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- HY-113568
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- HY-B0882R
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Cholinesterase (ChE)
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Neurological Disease
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Edrophonium (chloride) (Standard) is the analytical standard of Edrophonium (chloride). This product is intended for research and analytical applications. Edrophonium chloride is a reversible inhibitor of acetylcholinesterase.
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- HY-16904
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RI-2
1 Publications Verification
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RAD51
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Cancer
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RI-2 is a reversible RAD51 inhibitor, with an IC50 of 44.17 μM, and specifically inhibits homologous recombination repair in human cells.
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- HY-P10149
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Caspase
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Cancer
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Ac-IEPD-CHO is a reversible granzyme B inhibitor with a Ki of 80 nM . Ac-IEPD-CHO is also a caspase-8 inhibitor .
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- HY-150587
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ERK
NF-κB
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Inflammation/Immunology
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Anti-inflammatory agent 31 (enone 17) is a kind of andrographolide derivatives, is a anti-inflammatory agent. Anti-inflammatory agent 31 inhibits NF-κB activation by upstream blockade of PI3K/Akt and ERK1/2 MAPK activation. Anti-inflammatory agent 31 shows recovery effective of the intracellular GSH levels and protective effect on liver .
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- HY-15465
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CaMK
Autophagy
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Cancer
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KN-93 is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
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- HY-15465A
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CaMK
Autophagy
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Cancer
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KN-93 hydrochloride is a cell-permeable, reversible and competitive inhibitor calmodulin-dependent kinase type II (CaMKII) with a Ki of 370 nM.
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- HY-B0555A
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Beta-lactamase
Bacterial
Antibiotic
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Infection
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Nafcillin sodium monohydrate, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium monohydrate can be used for the research of staphylococcal infections .
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- HY-18682
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LCR-263
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Polo-like Kinase (PLK)
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Cancer
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Centrinone (LCR-263) is a selective and reversible inhibitor of polo-like kinase 4 (PLK4) with a Ki of 0.16 nM.
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- HY-B0590A
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- HY-13447A
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- HY-101856
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Btk
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Inflammation/Immunology
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BMS-986142 is a potent and highly selective reversible inhibitor of Bruton's tyrosine kinase (BTK) with an IC50 of 0.5 nM.
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- HY-19908
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Elastase
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Metabolic Disease
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BAY-85-8501 is a selective, reversible and potent inhibitor of Human Neutrophil Elastase (HNE), with an IC50 of 65 pM.
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- HY-117226A
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Histone Demethylase
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Others
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GSK 690 (Hydrochloride) is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
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- HY-B0207AS1
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- HY-B0555B
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- HY-117226
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Histone Demethylase
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Cancer
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GSK 690 is a reversible inhibitor of lysine specific demethylase 1 (LSD1), with a Kd value of 9 nM and a biochemical IC50 of 37 nM.
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- HY-13447
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- HY-P5936
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DEVD-CHO-CPP 32
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Caspase
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Cancer
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Ac-AAVALLPAVLLALLAP-DEVD-CHO (DEVD-CHO-CPP 32) is a potent and reversible caspase-3 inhibitor .
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- HY-50877
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GSK461364A
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Polo-like Kinase (PLK)
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Cancer
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GSK461364 is a selective, reversible and ATP-competitive Polo-like kinase 1 (PLK1) inhibitor with a Ki value of 2.2 nM.
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- HY-101770
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Microtubule/Tubulin
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Cancer
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BTB-1 is a potent, selective and reversible mitotic motor protein Kif18A inhibitor with an IC50 of 1.69 μM.
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- HY-138630
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- HY-10270
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TGN 255
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Thrombin
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Cardiovascular Disease
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Flovagatran (TGN 255) is a potent and reversible thrombin inhibitor (Ki: 9 nM). Flovagatran can be used in the research of arterial and venous thrombosis .
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- HY-P1403
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Potassium Channel
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Others
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Tertiapin LQ is a specific and reversible renal outer medullary potassium ROMK1 (Kir1.1) channel inhibitor .
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- HY-10869
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FAAH
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Metabolic Disease
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OL-135 is a CNS penetrant, selective, and reversible of FAAH inhibitor. OL-135 exhibits analgesic activity .
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- HY-10271
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TGN 255 sodium
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Thrombin
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Cardiovascular Disease
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Flovagatran (TGN 255) sodium is a potent and reversible thrombin inhibitor (Ki: 9 nM). Flovagatran sodium can be used in the research of arterial and venous thrombosis .
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- HY-122415
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Antibiotic
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Infection
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Tunicamine is a high carbohydrate antibiotic that is part of the structure of Tunicamycin. Tunicamycin is a nucleoside antibiotic and a reversible polyprenol-phosphate inhibitor .
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- HY-169249
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Z1620764636
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Potassium Channel
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Metabolic Disease
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Aekatperone is a reversible KATP channel inhibitor, with an IC50 of 9 μM. Aekatperone can be used for the research of congenital hyperinsulinism (CHI) .
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- HY-115899
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- HY-124158
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Proton Pump
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Metabolic Disease
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KR-60436 is a reversible H +/K +-ATPase inhibitor. KR-60436 can potently inhibit the metabolism of CYP1A2 substrates .
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- HY-101578
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Monoamine Oxidase
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Neurological Disease
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2614W94 is a selective, reversible inhibitor of monoamine oxidase-A with a competitive mechanism of inhibition and IC50 of 5 nM and Ki of 1.6 nM with serotonin as substrate.
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- HY-13805
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AGL 1879
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Src
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Cancer
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PP2 is a reversible and ATP-competitive Src family kinases inhibitor with IC50s of 4 and 5 nM for Lck and Fyn, respectively.
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- HY-I0020
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(-)-Narwedine; Narwedin
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Cholinesterase (ChE)
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Neurological Disease
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Galanthaminone (Narwedin) is a competitive and reversible cholinesterase (AChE) inhibitor; is used for the treatment of mild to moderate Alzheimer's disease and various other memory impairments.
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- HY-10163AS
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BIBR-953-d4 hydrochloride
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Thrombin
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Cardiovascular Disease
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Dabigatran-d4 (hydrochloride) is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
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- HY-100244
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- HY-B0590S1
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- HY-112166
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PRN1008
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Btk
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Metabolic Disease
Cancer
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Rilzabrutinib (PRN1008) is a reversible covalent, selective and oral active inhibitor of Bruton’s Tyrosine Kinase (BTK), with an IC50 of 1.3 nM.
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- HY-118994
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Phospholipase
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Neurological Disease
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ARN19874 is a selective, reversible uncompetitive N-acylphosphatidylethanolamine phospholipase D (NAPE-PLD) activity inhibitor with an IC50 of ~34 μM .
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- HY-103391
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Others
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Metabolic Disease
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Qc1 is a reversible and noncompetitive threonine dehydrogenase (TDH) inhibitor. Qc1 can be used for the research of Metabolic disease .
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- HY-155945
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Others
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Others
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Firefly luciferase-IN-1 (compound 48) is a highly potent and reversible inhibitor of firefly luciferase with an IC50 value of 0.25 nM .
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- HY-157038
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MAGL
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Inflammation/Immunology
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MAGL-IN-8 (compound 13) is a reversible monoacylglycerol lipase (MAGL) inhibitor, with an IC50 of 2.5 ± 0.4 nM for hMAGL .
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- HY-14486
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PRT060128 potassium
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P2Y Receptor
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Inflammation/Immunology
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Elinogrel (PRT060128) potassium is a reversible, competitive and orally active P2Y12 antagonist. Elinogrel potassium inhibits thrombosis .
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- HY-129314
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- HY-B0207AR
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Cholinesterase (ChE)
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Neurological Disease
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Pyridostigmine (bromide) (Standard) is the analytical standard of Pyridostigmine (bromide). This product is intended for research and analytical applications. Pyridostigmine bromide is a reversible cholinesterase inhibitor.
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- HY-168506
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YAP
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Cancer
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MSC-1254 is a reversible, selective and covalent TEAD1 inhibitor. MSC-1254 can be used for the study of cancer .
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- HY-70035
-
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FXV673
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Factor Xa
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Cardiovascular Disease
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Otamixaban(FXV673) is a potent (Ki = 0.5 nM), selective, rapid acting, competitive and reversible fXa inhibitor that effectively inhibits both free and prothrombinase-bound fXa.
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- HY-100679
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- HY-100679A
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- HY-132808
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SAR 444727; PRN473
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Btk
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Inflammation/Immunology
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Atuzabrutinib (SAR 444727) is a potent, selective reversible inhibitor of Btk (Bruton's tyrosine kinase) inhibitor. Atuzabrutinib inhibits neutrophil recruitment via inhibition of macrophage antigen-1 signalling .
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- HY-100919
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WIN 8077 chloride
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Cholinesterase (ChE)
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Others
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Ambenonium (WIN 8077) chloride is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium chloride inhibits human AChE with an IC50 value of 0.7 nM (hAChE) .
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- HY-152201
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Btk
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Cancer
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BTK-IN-18 is a potent, reversible BTK inhibitor with an IC50 of 0.002 µM. BTK-IN-18 inhibits both CD69 and CD86 in vivo .
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- HY-17020
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- HY-112423
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- HY-114503
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DNA/RNA Synthesis
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Cancer
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NSAH is a reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
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- HY-146649
-
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Parasite
Cathepsin
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Infection
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LmCPB-IN-1 (compound 35) is a potent and reversible covalent Leishmania mexicana cysteine protease B (LmCPB) inhibitor with a pKi of 9.7 .
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- HY-150717
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-
- HY-13020
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-
- HY-119721
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-
- HY-76409
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FXV673 hydrochloride
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Factor Xa
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Inflammation/Immunology
|
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Otamixaban (FXV673) is a potent, selective, rapid-acting, competitive, and reversible fXa inhibitor (Ki=0.5 nM) that effectively inhibits both free and prothrombinase-bound fXa .
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- HY-17020A
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- HY-134358
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CD38
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Neurological Disease
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Ara-F-NAD+ is an arabino analogue of NAD +. Ara-F-NAD+ is a potent, reversible and slow-binding CD38 NADase inhibitor .
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- HY-134358A
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CD38
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Neurological Disease
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Ara-F-NAD+ sodium is an arabino analogue of NAD +. Ara-F-NAD+ sodium is a potent, reversible and slow-binding CD38 NADase inhibitor .
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- HY-157042
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MAGL
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Inflammation/Immunology
Cancer
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MAGL-IN-11 (compound 29) is a selective and reversible MAGL inhibitor. MAGL-IN-11 has the potential to study inflammation, cancer and antioxidants .
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- HY-N1937R
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Bacterial
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Cancer
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Pristimerin (Standard) is the analytical standard of Pristimerin. This product is intended for research and analytical applications. Pristimerin is a potent and reversible monoacylglycerol lipase (MGL) inhibitor with an IC50 of 93 nM.
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- HY-124235
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Na+/K+ ATPase
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Others
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SK&F 97574 hydrochloride is a reversible inhibitor for H+/K+ ATPase, that reduces gastric acid secretion and promotes the healing of acid-related upper gastrointestinal ulcers .
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- HY-165132
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(S)-Floramultine; (S)-Bechuanine; Merenderine
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Others
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Others
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Floramultine ((S)-Floramultine) is a compound isolated from plants with cholinergic activity. It is a moderately potent reversible inhibitor of cholinesterase and has a certain specificity for different cholinesterases.
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- HY-13050A
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AZD-8931 fumarate
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EGFR
|
Cancer
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Sapitinib fumarate is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
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- HY-B0882S
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Cholinesterase (ChE)
|
Neurological Disease
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
- HY-129111
-
EACC
3 Publications Verification
|
Autophagy
|
Infection
Neurological Disease
|
|
EACC is a reversible autophagy inhibitor, which can block autophagic flux. EACC selectively inhibits the translocation of autophagosome-specific SNARE Stx17 thereby blocking autophagosome-lysosome fusion .
|
-
- HY-146958
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-8 is a potent reversible MAO-B inhibitor and an inhibitor of microglial production of neuroinflammatory mediator. MAO-B-IN-8 can be used for neurodegenerative disease research .
|
-
- HY-141473
-
|
Malonyl coenzyme A tetralithium
|
Endogenous Metabolite
Mitochondrial Metabolism
|
Metabolic Disease
|
|
Malonyl CoA (Malonyl coenzyme A) tetralithium is a substrate for fatty acid biosynthesis and an inhibitor of fatty acid oxidation. Malonyl CoA tetralithium is also a reversible inhibitor of mitochondrial carnitine palmitoyltransferase (CPT) 1 .
|
-
- HY-100526
-
|
|
Hippo (MST)
|
Cancer
|
|
XMU-MP-1 is a reversible and selective MST1/2 inhibitor with IC50s of 71.1 and 38.1 nM, respectively .
|
-
- HY-12631
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
BMS-654457 is a small-molecule, reversible inhibitor of factor XIa (FXIa), binding with human and rabbit FXIa with Kis of 0.2 and 0.42 nM, respectively.
|
-
- HY-N0826
-
-
- HY-137573
-
|
CC-90010
|
Epigenetic Reader Domain
|
Cancer
|
|
CC-90010 (compound 1) is a reversible and orally active BET inhibitor. CC-90010 is applied in the study for advanced solid tumors .
|
-
- HY-N9919
-
|
|
Others
|
Others
|
|
Glyasperin C is a potent and reversible noncompetitive inhibitor of neuraminidase with an IC50 of 20% at 200 μM. Glyasperin C is a polyphenol isolated from the roots of Glycyrrhiza uralensis .
|
-
- HY-112553
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
HZ52 is a potent, reversible 5-lipoxygenase inhibitor, blocking leukotriene synthesis with an IC50 of 0.7 μM in intact human polymorphonuclear leukocytes .
|
-
- HY-B0555
-
|
|
Beta-lactamase
Antibiotic
Bacterial
|
Infection
|
|
Nafcillin, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin exhibits bactericidal activity, and can be used for the research of staphylococcal infections .
|
-
- HY-121851
-
|
SB 641257
|
Proton Pump
|
Inflammation/Immunology
|
|
Revaprazan (SB 641257) is a reversible proton pump inhibitor with significant anti-inflammatory effects. Revaprazan can be used for chronic gastric inflammation research .
|
-
- HY-19415
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
|
-
- HY-19415A
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 hydrochloride is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
|
-
- HY-19415B
-
|
|
Phospholipase
|
Metabolic Disease
|
|
SB-435495 ditartrate is a potent, selective, reversible, non-covalent and orally active Lp-PLA2 inhibitor with an IC50 of 0.06 nM .
|
-
- HY-155613
-
|
|
Caspase
|
Cancer
|
|
M867 is a selective and reversible inhibitor of caspase-3 with an IC50 of 1.4 nM and Ki of 0.7 nM. M867 has anti apoptotic activity .
|
-
- HY-114991
-
|
|
HPPD
|
Others
|
|
Leptospermone is a competitive, reversible inhibitor for p-Hydroxyphenylpyruvate dioxygenase (HPPD), with an IC50 of 12.1 μM. Leptospermone exhibits herbicidal activity for its bleaching effect .
|
-
- HY-163052
-
|
SL-573
|
Others
|
Others
|
|
Ciproquazone (SL-573) is a compound that inhibits prostaglandin biosynthesis. Its relative inhibitory potency is between that of indomethacin and aspirin, and its inhibition of prostaglandin biosynthesis is reversible.
|
-
- HY-15339
-
|
Cdk2 inhibitor III
|
CDK
|
Cancer
|
|
CVT-313 (Cdk2 Inhibitor III) is a potent, selective, reversible, and ATP-competitive inhibitor of CDK2 with IC50 of 0.5 μM. CVT-313 inhibits CDC5L phosphorylation .
|
-
- HY-N8533
-
|
|
DNA/RNA Synthesis
|
Infection
Cancer
|
|
Sodium Camptothecin is a plant alkaloid, with antitumor activity. Sodium Camptothecin is a reversible inhibitor of RNA synthesis. Sodium Camptothecin is an effective inhibitor of adenovirus replication. Sodium Camptothecin inhibits DNA synthesis and causes breaks in intracellular preformed viral DNA .
|
-
- HY-10453
-
|
MLN2238
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
|
-
- HY-135008
-
J14
1 Publications Verification
|
Reactive Oxygen Species
|
Cancer
|
|
J14 is a reversible sulfiredoxin inhibitor with an IC50 of 8.1 μM. J14 induces oxidative stress (intracellular ROS accumulation) by inhibiting sulfiredoxin, leading to cytotoxicity and cancer cell death .
|
-
- HY-10273
-
|
AZD0837; Atecegatran fexenetil
|
Thrombin
|
Cardiovascular Disease
|
|
Atecegatran metoxil is a oral anticoagulant, which inhibits thrombin factor II and is used in thromboembolic disorders. In vivo, Atecegatran metoxil is converted to AR-H067637, a selective and reversible direct thrombin inhibitor.
|
-
- HY-N0793A
-
-
- HY-14574
-
|
|
Aurora Kinase
VEGFR
|
Cancer
|
|
PF-03814735 is a potent, orally available, ATP-competitive and reversible aurora A and aurora B inhibitor with IC50s of 0.8 and 0.5 nM, respectively.
|
-
- HY-10452
-
|
MLN9708
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
|
-
- HY-16709
-
|
|
Deubiquitinase
|
Cancer
|
|
USP7-IN-1 is a selective and reversible inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 77 μM, and can be used for the research of cancer.
|
-
- HY-114086
-
|
|
PDI
|
Cardiovascular Disease
|
|
ML359 is a potent, selctive and reversible inhibitor of protein disulfide isomerase (PDI), with an IC50 of 250 nM. ML359 can prevent thrombus formation in vivo .
|
-
- HY-123863
-
|
|
FAAH
|
Neurological Disease
|
|
SSR411298 is an orally active, selective and reversible fatty acid amide hydrolase (FAAH) inhibitor. SSR411298 has the potential for post-traumatic stress disorder research .
|
-
- HY-139603
-
|
|
YAP
|
Cancer
|
|
MYF-01-37 is a covalent TEAD inhibitor targeting Cys380. MYF-01-37 has a reversible inhibition on YAP/TEAD interaction .
|
-
- HY-116437
-
|
|
EGFR
|
Cancer
|
|
Selatinib is a reversible and orally active dual EGFR and ErbB2 inhibitor with IC50s of 13 nM and 22.5 nM, respectively. Selatinib has anticancer effects .
|
-
- HY-103058
-
-
- HY-155836
-
|
|
Lipase
|
Metabolic Disease
|
|
hPL-IN-1 (compound 2t) is a reversible inhibitor of pancreatic lipase (PL) (IC50=1.86 μM) for anti-obesity research .
|
-
- HY-117126
-
|
|
Bacterial
|
Infection
|
|
BTZ-N3 is a potent reversible and noncovalent inhibitor of decaprenylphosphoryl-β-d-ribose 2′ oxidase (DprE1) that shows anti-tuberculosis activity .
|
-
- HY-N0457A
-
|
(-)-Chicoric acid; trans-Caffeoyltartaric acid
|
HIV Integrase
HIV
Endogenous Metabolite
|
Infection
Cancer
|
|
L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
|
-
- HY-103261
-
|
|
Proton Pump
|
Endocrinology
|
|
SCH28080 is a reversible, K +-competitive inhibitor of the gastric H,K-ATPase, with a Ki of 0.12 μM. SCH28080 is an effective inhibitor of acid secretion in vivo and with anti-gastric ulcer activity .
|
-
- HY-118533A
-
|
WIN 8077 dichloride tetrahydrate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Ambenonium (WIN 8077) dichloride tetrahydrate is an orally active and reversible inhibitor of Acetyicholinesterase (AChE) with high affinity. Ambenonium dichloride tetrahydrate inhibits human AChE with an IC50 value of 0.7 nM (hAChE) .
|
-
- HY-100816
-
Rbin-1
2 Publications Verification
Ribozinoindole-1
|
Phosphatase
|
Metabolic Disease
|
|
Rbin-1 is a potent, reversible, and specific chemical inhibitor of eukaryotic ribosome biogenesis. Rbin-1 inhibits the ATPase with GI50 of 136 nM. Rbin-1 is a potent and selective chemical inhibitor of Midasin (Mdn1).
|
-
- HY-15313
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-10458
-
|
VS-6062 besylate
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) besylate is a potent ATP-competitive, reversible inhibitor of FAK and Pyk2 kinase, with an IC50 of 1.5 nM and 13 nM, respectively .
|
-
- HY-15313B
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 Hcl is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-13050
-
|
AZD-8931
|
EGFR
|
Cancer
|
|
Sapitinib (AZD-8931) is a reversible, ATP competitive EGFR inhibitor of with IC50s of 4, 3 and 4 nM for EGFR, ErbB2 and ErbB3 in cells, respectively.
|
-
- HY-15313C
-
|
|
Histone Demethylase
|
Cancer
|
|
CBB1007 trihydrochloride is a cell-permeable amidino-guanidinium compound that acts as a potent, reversible and substrate competitive LSD1 selective inhibitor (IC50 = 5.27 μM for hLSD1).
|
-
- HY-N0793
-
-
- HY-B1007
-
|
|
Sodium Channel
Others
|
Neurological Disease
|
|
Butacaine is a reversible nerve conduction blocker. Butacaine acts on the nervous system and nerve fibers, can cause both sensory and motor paralysis. Butacaine inhibits the NavBh currents .
|
-
- HY-14838
-
|
BIA 5-453
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Etamicastat (BIA 5-453) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM . Etamicastat can be used in the research of cardiovascular diseases .
|
-
- HY-B1318
-
|
Trisodium phosphonoformate; Phosphonoformic acid trisodium salt
|
DNA/RNA Synthesis
|
Infection
|
|
Foscarnet sodium (Trisodium phosphonoformate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet sodium is an antiherpesvirus agent used in cytomegalovirus retinitis .
|
-
- HY-14838A
-
|
BIA 5-453 hydrochloride
|
Dopamine β-hydroxylase
|
Cardiovascular Disease
|
|
Etamicastat hydrochloride (BIA 5-453 hydrochloride) is a potent and reversible dopamine-β-hydroxylase (DBH) inhibitor with an IC50 value of 107 nM . Etamicastat can be used in the research of cardiovascular diseases .
|
-
- HY-137463
-
-
- HY-144813
-
|
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
|
Gü2602 is a potent, reversible cathepsin K (CatK) inhibitor with a Ki of 0.013 nM for mature CatK (mCatK). Gü2602 suppresses the autocatalytic activation of the cathepsin K zymogen .
|
-
- HY-148520
-
|
|
Others
|
Metabolic Disease
|
|
QM295 is an endoplasmic reticulum oxidation 1 (ERO1) inhibitor with selectively reversible thiol reactivity. QM295 can be used for the research of endoplasmic reticulum stress .
|
-
- HY-15386
-
|
MD 780515
|
Monoamine Oxidase
|
Metabolic Disease
|
|
Cimoxatone (MD 780515) is a reversible, selectively and orally active type A monoamine oxidase (MAO-A) inhibitor. Cimoxatone enhances the anorectic action of Serotonin (HY-B1473A) .
|
-
- HY-123814
-
-
- HY-121966
-
|
Riparin III
|
Others
|
Cancer
|
|
Riparin is a nonspecific smooth muscle relaxant. Riparin inhibits CaCl2-induced contractions in a reversible and non-competitive manner and can be used in spasmolytic studies .
|
-
- HY-163175
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-24 is a selective and reversible BChE inhibitor with an IC50 of 9 nM. BChE-IN-24 can be used for the research of Alzheimer’s disease and related neurodegenerative disorders .
|
-
- HY-N1102
-
|
6-Hydroxypeganine
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Vasicinol is a reversible inhibitor of sucrase (IC50: 250 μM). Vasicinol is a HbF inducer. Vasicinol also inhibits Angiotensin-converting Enzyme (ACE). Vasicinol is apyrroquinazoline alkaloid that can be isolated from Adhatoda vasica .
|
-
- HY-18763
-
|
Ibustrin
|
COX
|
Cardiovascular Disease
|
|
Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes .
|
-
- HY-18763A
-
|
Ibustrin sodium
|
COX
|
Cardiovascular Disease
|
|
Indobufen sodium is a platelet aggregation inhibitor. Indobufen sodium is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen sodium suppresses thromboxane A2 (TxA2) synthesis. Indobufen sodium down-regulates tissue factor (TF) in monocytes .
|
-
- HY-104032
-
|
|
RSV
|
Infection
Metabolic Disease
|
|
Ac-CoA Synthase Inhibitor1 is a potent, reversible acetate-dependent acetyl-CoA synthetase 2 (ACSS2) inhibitor with an IC50 of 0.6 µM . Ac-CoA Synthase Inhibitor1 inhibits the respiratory syncytial virus (RSV) .
|
-
- HY-129301
-
|
|
BCRP
|
Cancer
|
|
CCTA-1523 is a potent, selective, reversible and orally active ABCG2 inhibitor. CCTA-1523 shows cytotoxicity. CCTA-1523 shows anticancer activity .
|
-
- HY-10459
-
|
VS-6062
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-B0555BS
-
-
- HY-20403
-
|
VS-6062(hydrochloride)
|
FAK
Pyk2
|
Cancer
|
|
PF-562271 (VS-6062) hydrochloride is a potent, ATP-competitive and reversible FAK and Pyk2 kinase inhibitor with IC50s of 1.5 nM and 13 nM, respectively .
|
-
- HY-B0199A
-
|
RS 61443 hydrochloride; TM-MMF hydrochloride
|
Endogenous Metabolite
Bacterial
|
Cancer
|
|
Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-N3474
-
|
|
Carboxylesterase
|
Others
|
|
Isolicoflavonol potently inhibits hCES2A (Human carboxylesterase 2)-mediated fluorescein diacetate hydrolysis in a reversible and mixed inhibition manner, with Ki values less than 1.0 μM .
|
-
- HY-153662
-
|
|
Ras
|
Cancer
|
|
TH-Z816 is a reversible inhibitor againstKRAS(G12D)mutation with an IC50 value of 14 μM, which can be used in cancer research .
|
-
- HY-155837
-
|
|
Lipase
|
Metabolic Disease
|
|
hPL-IN-2 (compound 2u) is a potent, reversible, and non-competitive inhibitor of pancreatic lipase (IC50: 1.63 μM) and can be used in anti-obesity research .
|
-
- HY-109122
-
|
ACT-246475
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Selatogrel (ACT-246475) is a reversible and selective P2Y12 receptor antagonist which inhibits platelet aggregation with an IC50 of 8 nM. Selatogrel exhibits antithrombotic efficacy .
|
-
- HY-14248
-
|
CGS 20267
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
- HY-100736
-
ML348
4 Publications Verification
GNF-Pf-1127
|
Phospholipase
|
Cancer
|
|
ML348 (GNF-Pf-1127) is a selective and reversible acyl-protein thioesterase 1 (APT1)/lysophospholipase 1 (LYPLA1) inhibitor with an IC50 of 210 nM, and barely inhibits LYPLA2 .
|
-
- HY-110253
-
|
HIV-1 inhibitor 18A
|
HIV
|
Infection
|
|
18A (HIV-1 inhibitor 18A) is a reversible broad-spectrum HIV-1 inhibitor. 18A exhibits broad inhibitory activity against multiple HIV-1 strains by blocking the function of Env .
|
-
- HY-19651A
-
|
TAK-147
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .
|
-
- HY-19651B
-
|
TAK-147 fumarate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .
|
-
- HY-17388
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
(±)-Huperzine A, an active Lycopodium alkaloid extracted from traditional Chinese herb, is a potent, selective and reversible acetylcholinesterase (AChE) inhibitor and has been widely used in China for the treatment of Alzheimer's disease (AD).
|
-
- HY-13917
-
|
VS-4718; SR-2516
|
FAK
Apoptosis
|
Cancer
|
|
PND-1186 (VS-4718) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 selectively promotes tumor cell apoptosis .
|
-
- HY-10530
-
|
ASLAN001; ARRY-334543
|
EGFR
|
Cancer
|
|
Varlitinib (ASLAN001) is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively .
|
-
- HY-P1081
-
|
|
Proteasome
|
Inflammation/Immunology
|
|
Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for μ-calpain and cathepsin L, respectively .
|
-
- HY-P1081A
-
|
|
Proteasome
|
Inflammation/Immunology
|
|
Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively .
|
-
- HY-13917A
-
|
VS-4718 hydrochloride; SR-2516 hydrochloride
|
FAK
Apoptosis
|
Cancer
|
|
PND-1186 hydrochloride (VS-4718 hydrochloride) is a potent, highly-specific and reversible inhibitor of FAK with an IC50 of 1.5 nM. PND-1186 hydrochloride selectively promotes tumor cell apoptosis .
|
-
- HY-139032
-
-
- HY-144812
-
|
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
|
Gü1303 is a potent, reversible, slow-binding cathepsin K (CatK) inhibitor with a Ki of 0.91 nM for mature CatK (mCatK). Gü1303 suppresses the autocatalytic activation of the cathepsin K zymogen .
|
-
- HY-10530A
-
|
ASLAN001 tosylate; ARRY-334543 tosylate
|
EGFR
|
Cancer
|
|
Varlitinib (ASLAN001) tosylate is a potent, reversible, small molecule pan-EGFR inhibitor with IC50s of 7, 2, 4 nM for HER1, HER2 and HER4, respectively .
|
-
- HY-A0166
-
|
MK0791
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
|
-
- HY-133511
-
|
|
Phosphatase
|
Cancer
|
|
MLS000544460 is a highly selective and reversible Eya2 phosphatase inhibitor with a Kd of 2.0 μM and an IC50 of 4 μM. MLS000544460 inhibit Eya2 phosphatase mediated cell migration and has anti-cancer activity .
|
-
- HY-A0166A
-
|
MK0791 sodium
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin sodium (MK0791 sodium) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin sodium inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin sodium is an antibacterial adjunct .
|
-
- HY-18336
-
|
|
CFTR
|
Cardiovascular Disease
|
|
GlyH-101 is a potent CFTR inhibitor. GlyH-101 also is a potent and reversible inhibitor of the VSORC conductance. GlyH-101 shows antiproliferative activity. GlyH-101 inhibits CFTR-like current and VSORC current .
|
-
- HY-10163
-
|
BIBR 953; BIBR 953ZW
|
Thrombin
|
Cardiovascular Disease
Cancer
|
|
Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
|
-
- HY-109079A
-
|
DWP14012 hydrochloride; Fexuprazan hydrochloride
|
Proton Pump
|
Metabolic Disease
|
|
Abeprazan hydrochloride (DWP14012 hydrochloride) is a potassium-competitive acid blocker. Abeprazan hydrochloride inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan hydrochloride is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
|
-
- HY-109079
-
|
DWP14012; Fexuprazan
|
Proton Pump
|
Metabolic Disease
|
|
Abeprazan (DWP14012) is a potassium-competitive acid blocker. Abeprazan inhibits H +, K +- ATPase by reversible potassium-competitive ionic binding with no acid activation required. Abeprazan is developed as a potential alternative to proton pump inhibitor for the treatment of acid-related diseases .
|
-
- HY-12293
-
|
|
CDK
Apoptosis
|
Cancer
|
|
LY2857785 is a type I reversible and competitive ATP kinase inhibitor against CDK9 (IC50 11 nM) and other transcription kinases CDK8 (IC50 16 nM), and CDK7 (IC50 246 nM).
|
-
- HY-100655
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
O-Desmethyl apixaban is a metabolite of Apixaban (BMS-562247-01) . Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively .
|
-
- HY-12853
-
|
|
Reactive Oxygen Species
|
Others
|
|
Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .
|
-
- HY-145339
-
|
|
Others
|
Neurological Disease
Inflammation/Immunology
|
|
ARN19702 is a selective, orally active, reversible, and brain-penetrant N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 230 nM for human NAAA. ARN19702 has pain relief effects .
|
-
- HY-120337
-
|
|
Others
|
Cancer
|
|
V-11-0711 is a potent and selective choline kinase alpha (ChoKα) inhibitor with an IC50 of 20 nM. V-11-0711 causes a reversible growth arrest in HeLa cells .
|
-
- HY-146305
-
-
- HY-146318
-
-
- HY-121422
-
|
|
MAGL
Histamine Receptor
|
Inflammation/Immunology
|
|
JZP-361 is a potent, reversible and selective inhibitor of human recombinant MAGL (hMAGL) with an IC50 of 46 nM. JZP-361 also shows antihistaminergic activities and can be used for asthma research .
|
-
- HY-152009
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 3CLpro-IN-7 is a reversible covalent SARS-CoV-2 3CL protease inhibitor with an IC50 value of 1.4 µM .
|
-
- HY-N2181A
-
|
|
Cytochrome P450
|
Inflammation/Immunology
Cancer
|
|
DL-Acetylshikonin is a non-selective, reversible cytochrome P450 inhibitor with IC50 values of 1.4-4.0 μM. DL-Acetylshikonin has anti-cancer and anti-inflammatory activities .
|
-
- HY-133732
-
|
GEA 654 hydrochloride; A03 hydrochloride
|
Serotonin Transporter
5-HT Receptor
iGluR
|
Neurological Disease
|
|
Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow .
|
-
- HY-P4989
-
|
|
Biochemical Assay Reagents
|
Infection
|
|
Type A Allatostatin III (allatostatin 3) is a blood-brain barrier permeable and reversible neuropeptide that inhibits hormone synthesis in juvenile female cockroaches. Type A Allatostatin III can be used in pesticide research .
|
-
- HY-19219
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
BMS-189664 is a potent, selective, and orally active reversible inhibitor of a-thrombin, with an IC50 of 0.046 μM. BMS-189664 can be used for arterial and venous thrombosis research .
|
-
- HY-129980
-
|
|
PKC
|
Neurological Disease
|
|
NPC-15437 dihydrochloride is a selective, penetrable and reversible protein kinase C (PKC) inhibitor, with an IC50 of 19 μM. NPC-15437 dihydrochloride interferes with mechanisms underlying memory consolidation .
|
-
- HY-B0555AR
-
|
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Nafcillin (sodium monohydrate) (Standard) is the analytical standard of Nafcillin (sodium monohydrate). This product is intended for research and analytical applications. Nafcillin sodium monohydrate, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium monohydrate can be used for the research of staphylococcal infections .
|
-
- HY-116026R
-
|
|
Drug Metabolite
Cholinesterase (ChE)
|
Neurological Disease
|
|
3-Hydroxycarbofuran (Standard) is the analytical standard of 3-Hydroxycarbofuran. This product is intended for research and analytical applications. 3-Hydroxycarbofuran, a major metabolite of Carbofuran, is a reversible acetylcholinesterase (AChE) inhibitor .
|
-
- HY-B0555BR
-
|
|
Beta-lactamase
Antibiotic
Bacterial
|
Infection
|
|
Nafcillin (sodium) (Standard) is the analytical standard of Nafcillin (sodium). This product is intended for research and analytical applications. Nafcillin sodium, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium can be used for the research of staphylococcal infections .
|
-
- HY-19219A
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
BMS-189664 hydrochloride is a potent, selective, and orally active reversible inhibitor of a-thrombin, with an IC50 of 0.046 μM. BMS-189664 hydrochloride can be used for arterial and venous thrombosis research .
|
-
- HY-124464
-
-
- HY-122632
-
|
|
Hedgehog
|
Cancer
|
|
Ciliobrevin D is a cell-permeable, reversible and specific inhibitor of AAA+ ATPase motor cytoplasmic dynein. Ciliobrevin D inhibits Hedgehog (Hh) signaling and primary cilia formation. Ciliobrevin D inhibits dynein-dependent microtubule gliding and ATPase activity in vitro .
|
-
- HY-110067
-
-
- HY-101945
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
A-69412 is a reversible, specific inhibitor of the 5-lipoxygenase (5-LO). A-69412 has the potential to treat asthma and ulcerative colitis, and possibly other inflammatory and allergic conditions.
|
-
- HY-W016645
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
4-Diethylaminobenzaldehyde is a reversible aldehyde dehydrogenases (ALDHs) inhibitor, with a Ki of 4 nM for ALDH1. 4-Diethylaminobenzaldehyde displays potent anti-androgenic effect (IC50= 1.71μM) .
|
-
- HY-114503A
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
(E/Z)-NSAH is an isoform of NSAH (HY-114503), which is reversible and competitive nonnucleoside ribonucleotide reductase (RR) inhibitor, with cell-free IC50 of 32 μM and cell-based IC50 of ~250 nM, respectively .
|
-
- HY-W727627
-
|
|
Amylases
|
Metabolic Disease
|
|
5-O-Coumaroylquinic acid is a potent, reversible, non-competitive α-amylase inhibitor with an IC50 value of 69.39 μM. 5-O-Coumaroylquinic acid can be used in diabetes research .
|
-
- HY-19833
-
|
|
Cytochrome P450
|
Cancer
|
|
CFG920 is an orally active, nonsteroidal, reversible dual CYP17 and CYP11B2 inhibitor. CFG920 has the potential for metastatic castration-resistant prostate cancer research .
|
-
- HY-144323
-
|
|
PROTACs
PERK
|
Cancer
|
|
YF135 is an efficient and reversible-covalent KRAS G12C PROTAC. YF135 is designed and synthesized by tethering KRAS G12C inhibitor 48 (compound 6d) as the ligand, and basing on the scaffold of MRTX849 linkage VHL ligand. YF135 significantly induces the degradation of KRAS G12C in a reversible manner and decreases phospho-ERK level through the E3 ligase VHL mediated proteasome pathway .
|
-
- HY-108341
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
- HY-13520
-
|
Oncodazole; R17934
|
Microtubule/Tubulin
Bcr-Abl
CRISPR/Cas9
Autophagy
Apoptosis
|
Cancer
|
|
Nocodazole (Oncodazole) is a rapidly-reversible inhibitor of microtubule. Nocodazole binds to β-tubulin and disrupts microtubule assembly/disassembly dynamics, which prevents mitosis and induces apoptosis in tumor cells. Nocodazole inhibits Bcr-Abl, and activates CRISPR/Cas9.
|
-
- HY-14879A
-
|
NXL-104
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
|
-
- HY-14879B
-
|
NXL-104 hydrate
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Avibactam sodium (NXL-104) hydrate is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
|
-
- HY-101456
-
|
4-Chloro-DL-phenylalanine methyl ester hydrochloride
|
Tryptophan Hydroxylase
5-HT Receptor
|
Neurological Disease
|
|
PCPA methyl ester hydrochloride (4-Chloro-DL-phenylalanine methyl ester hydrochloride), a reversible tryptophan hydroxylase inhibitor, is a serotonin (5-HT) synthesis inhibitor. PCPA methyl ester hydrochloride crosses the blood brain barrier and reduces 5-HT central availability .
|
-
- HY-150643
-
|
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
RSK2-IN-2 (Compound 25) is a reversible covalent inhibitor of the RPS6KA3 (RSK2) kinase. RSK2-IN-2 is also described to inhibit MSK1, MSK2 and RSK3 .
|
-
- HY-17543
-
|
|
Deubiquitinase
|
Cancer
|
|
ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
|
-
- HY-B0534
-
|
Ro111163
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-18690
-
|
AG-221
|
Isocitrate Dehydrogenase (IDH)
|
Cancer
|
|
Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively.
|
-
- HY-144689
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-3 (compound 45a) is a potent, selective, time-dependent and pseudoirreversible BChE inhibitor, with an IC50 of 56.9 nM. BChE-IN-3 also shows marginal and reversible (not time-dependent) inhibition of AChE .
|
-
- HY-118795
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
SC-22716 is a potent, competitive, reversible inhibitor of human LTA4 hydrolase, with an IC50 of 0.20 µM. SC-22716 has potential for the research of inflammatory bowel disease (IBD) and psoriasis .
|
-
- HY-W013256
-
|
Trisodium phosphonoformate hexahydrate; Phosphonoformic acid trisodium salt hexahydrate
|
DNA/RNA Synthesis
|
Infection
|
|
Foscarnet trisodium hexahydrate (Trisodium phosphonatoformate hexahydrate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet trisodium hexahydrate is an antiherpesvirus agent used in cytomegalovirus retinitis .
|
-
- HY-14179
-
PPQ-102
3 Publications Verification
CFTR inhibitor
|
CFTR
|
Others
|
|
PPQ-102 (CFTR Inhibitor) is a reversible CFTR inhibitor that completely inhibits CFTR chloride currents (IC50 ~90 nM). PPQ-102 is not affected by membrane potential-dependent cell allocation or blocking efficiency (uncharged at physiological pH) and effectively prevents cyst enlargement in polycystic kidney disease .
|
-
- HY-113963
-
|
|
Apoptosis
|
Cancer
|
|
Ac- IETD- CHO is a potent, reversible inhibitor of granzyme B and caspase-8. Ac- IETD- CHO inhibits Fas-mediated apoptotic cell death, hemorrhage, and liver failure. Ac- IETD- CHO also inhibits cytotoxic T lymphocytes induced cell death .
|
-
- HY-18780
-
RR6
2 Publications Verification
|
Others
|
Cancer
|
|
RR6 is a potent, selective, reversible, competitive and orally active vanin inhibitor with an IC50 of 540 nM for recombinant vanin-1. RR6 also potently inhibits human, bovine and rat serum pantetheinase with IC50 values of 40 nM, 41 nM and 87 nM, respectively .
|
-
- HY-13867
-
|
GF109203X; Go 6850
|
PKC
GSK-3
|
Metabolic Disease
Cancer
|
|
Bisindolylmaleimide I (GF109203X) is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I is also a GSK-3 inhibitor .
|
-
- HY-14879
-
|
NXL-104 free acid
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Avibactam (NXL-104) free acid is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
|
-
- HY-100817
-
|
|
Phosphatase
|
Others
|
|
Rbin-2 is a potent, reversible and selective inhibitor of Midasin (Mdn1), an enzyme belonging to the AAA+ (ATPases associated with diverse cellular activities) protein family. Rbin-2 inhibits eukaryotic ribosome biogenesis and is a powerful probe for the eukaryotic ribosome assembly .
|
-
- HY-130126
-
|
SCO-792
|
Enteropeptidase
|
Others
|
|
Sucunamostat hydrate (SCO-792) is an orally active and reversible enteropeptidase inhibitor with IC50s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrate can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo .
|
-
- HY-14879C
-
|
NXL-104 dihydrate
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Avibactam sodium (NXL-104) dihydrate is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
|
-
- HY-132841A
-
|
SCO-792 hydrochloride
|
Enteropeptidase
|
Metabolic Disease
|
|
Sucunamostat (SCO-792) hydrochloride is an orally active and reversible enteropeptidase inhibitor with IC50s of 4.6 nM and 5.4 nM for rat enteropeptidase and human enteropeptidase, respectively. Sucunamostat hydrochloride can slowly dissociate from enteropeptidase in vitro and inhibit protein digestion in vivo .
|
-
- HY-13867A
-
|
GF109203X hydrochloride; Go 6850 hydrochloride
|
PKC
GSK-3
|
Metabolic Disease
Cancer
|
|
Bisindolylmaleimide I (GF109203X) hydrochloride is a cell-permeable and reversible PKC inhibitor (IC50 of 20 nM, 17 nM, 16 nM, and 20 nM for PKCα, PKCβI, PKCβII, and PKCγ. Bisindolylmaleimide I hydrochloride is also a GSK-3 inhibitor .
|
-
- HY-B0590
-
|
Ro 1-9569
|
Monoamine Transporter
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease .
|
-
- HY-50667S
-
|
BMS-562247-01-13C,d3
|
Factor Xa
|
Cardiovascular Disease
|
|
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
|
-
- HY-10716A
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
|
-
- HY-15958
-
VBY-825
1 Publications Verification
|
Cathepsin
|
Inflammation/Immunology
Cancer
|
|
VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects .
|
-
- HY-W013571
-
|
Cuminic acid
|
Fungal
|
Infection
|
|
4-Isopropylbenzoic acid, an aromatic monoterpenoid, is isolated from the stem bark of Bridelia retusa. 4-Isopropylbenzoic acid exhibits antifungal activities. 4-Isopropylbenzoic acid is also a reversible and uncompetitive inhibitor of mushroom tyrosinase .
|
-
- HY-115062
-
|
|
Phospholipase
|
Metabolic Disease
|
|
MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-B0590E
-
|
Ro 1-9569 mesylate
|
Monoamine Transporter
|
Neurological Disease
|
|
Tetrabenazine (Ro 1-9569) mesylate is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine mesylate can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease .
|
-
- HY-151875
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
MurA-IN-3 is a reversible pyrrolidinedione-based MurA inhibitor. MurA-IN-3 has inhibitory activity for MurA with an IC50 value of 4.5 μM. MurA-IN-3 also has antibacterial activity .
|
-
- HY-W087937
-
|
Benzenecarboximidamide hydrochloride hydrate
|
Ser/Thr Protease
|
Cancer
|
|
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
|
-
- HY-149477
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
IHC3 is a competitive and reversible MAO-B inhibitor (IC50: 1.672 μM). IHC3 can interact with the amino acid Cys172 of MAO-B. IHC3 can be used for neurological diseases research .
|
-
- HY-10716
-
|
|
GlyT
|
Neurological Disease
|
|
PF-03463275 hydrochloride is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 hydrochloride has the potential for Schizophrenia research .
|
-
- HY-16420
-
|
|
Syk
|
Inflammation/Immunology
|
|
R112 is a fast and reversible inhibitor of spleen tyrosine kinase (Syk) kinase. R112 inhibits Syk kinase activity with an IC50 value of 226 nM and a Ki value of 96 nM. R112 inhibits IgE-FcεRI signaling pathway. R112 can be used for the research of allergic rhinitis .
|
-
- HY-108341A
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
- HY-124366
-
|
|
Others
|
Infection
Cancer
|
|
Slingshot inhibitor D3 is a potent, selective, reversible and competitive inhibitor of Slingshot. The IC50 value for Slingshot 1 is 3 μM and the Ki value for Slingshot 2 is 3.9 μM. Slingshot inhibitor D3 has similar inhibitory activities toward both Slingshot 1 and Slingshot 2 .
|
-
- HY-19651
-
|
TAK-147 free base
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .
|
-
- HY-13945
-
NVP 231
2 Publications Verification
|
Apoptosis
|
Cancer
|
|
NVP 231 is a potent, specific, and reversible ceramide kinase (CerK) inhibitor(IC50=12 nM) that competitively inhibits binding of ceramide to CerK . NVP 231 induces cell apoptosis by increasing DNA fragmentation and caspase-3 and caspase-9 cleavage .
|
-
- HY-127105A
-
|
LNP023 hydrochloride
|
Complement System
|
Metabolic Disease
Inflammation/Immunology
|
|
LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM .
|
-
- HY-106405
-
|
BIA 3-202
|
COMT
|
Metabolic Disease
|
|
Nebicapone (BIA 3-202), a reversible catechol-O-methyltransferase (COMT) inhibitor, is mainly metabolized by glucuronidation. Nebicapone is mainly peripherally acting inhibitor that decreases the biotransformation of L-DOPA to 3-O-methyl-DOPA by inhibition of COMT, and it is potential for the treatment of Parkinson's disease .
|
-
- HY-120394
-
|
|
Fatty Acid Synthase (FASN)
Apoptosis
|
Cancer
|
|
TVB-3166 is an orally-available, reversible, and selective fatty acid synthase (FASN) inhibitor with IC50s of 42 nM and 81 nM for biochemical FASN and cellular palmitate synthesis, respectively. TVB-3166 induces apoptosis, and inhibits in-vivo xenograft tumor growth .
|
-
- HY-16946
-
|
|
Acetyl-CoA Carboxylase
|
Metabolic Disease
|
|
CP-610431 is a reversible, ATP-uncompetitive, isozyme-nonselective acetyl-CoA carboxylase (ACC) inhibitor. CP-610431 inhibits ACC1 and ACC2 with IC50s of ~50 nM. CP-610431 can be used for the research of metabolic syndrome .
|
-
- HY-119423
-
|
|
MMP
|
Cancer
|
|
MMP Inhibitor II (compound 4e) is a potent, reversible pan-MMP inhibitor with IC50 values of 24 nM, 18.4 nM, 30 nM, and 2.7 nM for MMP-1,MMP-3, MMP-7, and MMP-9, respectively .
|
-
- HY-10227
-
|
PS-341; LDP-341; NSC 681239
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
|
-
- HY-50667
-
|
BMS-562247-01
|
Factor Xa
|
Cardiovascular Disease
Cancer
|
|
Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases .
|
-
- HY-B0034
-
|
E2020
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
|
-
- HY-102034
-
|
|
Complement System
|
Inflammation/Immunology
|
|
Complement factor D-IN-1 is a potent and selective small-molecule reversible factor d inhibitor, with IC50s of 0.006 and 0.05 μM in FD Thioesterolytic Fluorescent Assay and a MAC Deposition Assay, respectively.
|
-
- HY-117421A
-
|
|
Histone Methyltransferase
DNA Methyltransferase
|
Cancer
|
|
CM-579 trihydrochloride is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
|
-
- HY-100642
-
|
Ro 40-7591
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease .
|
-
- HY-117421
-
|
|
Histone Methyltransferase
DNA Methyltransferase
|
Cancer
|
|
CM-579 is a first-in-class reversible, dual inhibitor of G9a and DNMT, with IC50 values of 16 nM, 32 nM for G9a and DNMT, respectively. Has potent in vitro cellular activity in a wide range of cancer cells .
|
-
- HY-N4143
-
|
|
Phosphatase
|
Metabolic Disease
|
|
Cyanidin 3-arabinoside is a selective and reversible protein tyrosine phosphatase 1B (PTP1B) inhibitor, with an IC50 of 8.91 μM. Cyanidin 3-arabinoside is potential for the research of type 2 diabetes .
|
-
- HY-133016A
-
|
|
MetAP
|
Others
|
|
(R)-M8891 (compound R-9) is a less active isomer of M8891. M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor .
|
-
- HY-157136
-
|
|
CRM1
COX
c-Myc
Survivin
|
Cancer
|
|
LFS-1107 is a reversible CRM1 inhibitor (Kd: 12.5 pM). LFS-1107 can selectively eliminate extranodal natural killer/T cell lymphoma (ENKTL) cells and can be used for cancer research .
|
-
- HY-116188
-
|
|
Others
|
Inflammation/Immunology
|
|
HX1 is a potent reversible myeloperoxidase (MPO) inhibitor with an IC50 value of 50 nM. HX1 is bound within the active site cavity above the heme and blocks the substrate channel. HX1 is promising for research of inflammatory diseases .
|
-
- HY-10453R
-
|
|
Proteasome
Autophagy
|
Cancer
|
|
Ixazomib (Standard) is the analytical standard of Ixazomib. This product is intended for research and analytical applications. Ixazomib (MLN2238) is a selective, potent, and reversible proteasome inhibitor, which inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 of 3.4 nM (Ki of 0.93 nM).
|
-
- HY-16693
-
|
|
Others
|
Cardiovascular Disease
Others
|
|
LDN-27219 is a reversible, slow-binding inhibitor of TGase. LDN-27219 inhibits human TGase with an IC50 value of 0.6 μM. LDN-27219 effectively decreases blood pressure and induces vasodilation, it can be used for the research of cardiovascular disease .
|
-
- HY-126075A
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2 .
|
-
- HY-108552
-
MG-115
1 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
|
MG-115 is a potent and reversible proteasome inhibitor, with Kis of 21 nM and 35 nM for 20S and 26S proteasome, respectively. MG-115 specifically inhibit the chymotrypsin-like activity of the proteasome, induces p53-dependent apoptosis .
|
-
- HY-18763S
-
|
Ibustrin-d5
|
Isotope-Labeled Compounds
COX
|
Cardiovascular Disease
|
|
Indobufen-d5 is deuterium labeled Indobufen. Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes[1].
|
-
- HY-129137
-
|
Cy 3-soph
|
Others
|
Others
|
|
Cyanidin 3-sophoroside chloride is a potent non-competitive reversible polyphenol oxidase (PPO) inhibitor. Also, Cyanidin 3-sophoroside chloride can be used as an anti-browning agent to inhibit the degree of PPO browning, enhance the antioxidant damage capacity of fruits and prolong the storage period .
|
-
- HY-70074
-
|
|
RGS Protein
|
Inflammation/Immunology
Cancer
|
|
CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM .
|
-
- HY-12036
-
|
|
PI3K
mTOR
Apoptosis
|
Cancer
|
|
GSK1059615 is a dual inhibitor of PI3Kα/β/δ/γ (reversible) and mTOR with IC50 of 0.4 nM/0.6 nM/2 nM/5 nM and 12 nM, respectively.
|
-
- HY-15497
-
AZD7687
1 Publications Verification
|
Acyltransferase
|
Metabolic Disease
|
|
AZD7687 is a potent, selective, reversible and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor with an IC50 of 80 nM for human DGAT1. AZD7687 can be used for type 2 diabetes mellitus and obesity research .
|
-
- HY-P0322
-
|
EMD 56574
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption .
|
-
- HY-N1581
-
|
Nigakilactone D
|
Parasite
|
Infection
Endocrinology
|
|
Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .
|
-
- HY-139031
-
-
- HY-103462
-
-
- HY-10715
-
|
|
GlyT
|
Neurological Disease
|
|
SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38 nM, respectively). SSR504734 shows anti-schizophrenia, anti-anxiety and anti-depression activities .
|
-
- HY-151919
-
|
|
FAAH
|
Inflammation/Immunology
|
|
FAAH-IN-7 is a reversible and potent FAAH inhibitor with an IC50 value of 8.29 nM. FAAH-IN-7 suppresses oxidative stress in 1321N1 astrocytes and exhibits notable neuroprotective effect in ex vivo neuroinflammation model .
|
-
- HY-120017
-
|
MD-370503
|
Monoamine Oxidase
|
Neurological Disease
|
|
Befloxatone (MD-370503) is an orally active, selective and reversible inhibitor of Monoamine Oxidase A (MAO-A) (IC50=4 nM). Befloxatone increases the tissue level of monoamine, striatal dopamine and cortical norepinephrine. Befloxatone has antidepressant potential .
|
-
- HY-15958A
-
|
|
Others
|
Cancer
|
|
(S,R,R)-VBY-825 is the isomer of VBY-825 (HY-15958), and can be used as an experimental control. VBY-825 is a novel reversible inhibitor of cathepsin with high inhibition of cathepsin B, L, S and V.
|
-
- HY-163624
-
|
|
Bcl-2 Family
|
Cancer
|
|
Bfl-1-IN-2 (Compound 13) is a reversible and covalent inhibitor of Bfl-1 (IC50: 4.3 μM). Bfl-1-IN-2 acts by binding to Cys55 of Bfl-1 .
|
-
- HY-N0826R
-
-
- HY-P1346
-
|
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain .
|
-
- HY-115537
-
|
|
Apoptosis
|
Cancer
|
|
NAE-IN-M22 is a potent, selective and reversible inhibitor of NEDD8 activating enzyme (NAE), with potency in micromolar range. NAE-IN-M22 inhibits multiple cancer cell lines and induces apoptosis in A549 cells. NAE-IN-M22 also can inhibit tumor growth in vivo .
|
-
- HY-N6722
-
|
Tridolgosir
|
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Swainsonine (Tridolgosir) is an natural indolizidine alkaloid, a potent and reversible α-mannosidase inhibitor. Swainsonine induces apoptosis and cell cycle arrest at G2/M phase. Swainsonine shows anti-tumor activity .
|
-
- HY-119361
-
|
(Rac)-Deoxysappanone B 7,4' dimethyl ether
|
Microtubule/Tubulin
|
Cancer
|
|
(Rac)-Deox B 7,4, a homoisoflavanoid compound, inhibits microtubule polymerization via binding near the colchicine site and promote reversible G2 arrest. (Rac)-Deox B 7,4 possesses nanomolar anti-leukemic activity .
|
-
- HY-10253
-
|
Tyrphostin AG 1024
|
IGF-1R
Insulin Receptor
Apoptosis
|
Endocrinology
Cancer
|
|
AG1024 (Tyrphostin AG 1024) is a reversible, competitive and selective IGF-1R inhibitor with an IC50 of 7 μM. AG1024 inhibits phosphorylation of IR (IC50=57 μM). AG1024 induces apoptosis and has anti-cancer activity .
|
-
- HY-P1346A
-
|
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain .
|
-
- HY-100413
-
|
|
Proton Pump
|
Inflammation/Immunology
|
|
CS-526 is a potent, selective, reversible and orally active acid pump antagonist. CS-526 inhibits H +,K +-ATPase activity. CS-526 inhibits gastric acid secretion and prevents esophageal lesions. CS-526 has the potential for the research of gastroesophageal reflux disease .
|
-
- HY-18763R
-
|
|
COX
|
Cardiovascular Disease
|
|
Indobufen (Standard) is the analytical standard of Indobufen. This product is intended for research and analytical applications. Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes .
|
-
- HY-155612A
-
|
|
Caspase
|
Neurological Disease
|
|
(Rac)-M826 is the racemate of M826 (HY-155612). M826 is a selective and reversible inhibitor for caspase-3 with an IC50 of 0.005 μM. M826 inhibits apoptosis in cell NT2. M826 can be used for nervous system diseases research .
|
-
- HY-147860
-
|
|
EGFR
|
Cancer
|
|
EGFR-IN-61 (compound 22a) is a potent EGFR kinase inhibitor, with IC50 values of 42 nM (L858R/T790 M), 137 nM (L858R/T790 M/C797S), and 743 nM (WT), respectively. EGFR-IN-61 shows antiproliferative activity against A549 and H1975 cell lines, with IC50 values of 2.14 and 1.82 μM, respectively .
|
-
- HY-122249
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
MT-7 is a potent mitotic inhibitor. MT-7 shows antiproliferative activity. MT-7 induces cell cycle arrest at G2/M phase. MT-7 induces specific, reversible mitotic arrest and inhibits the polymerization of cellular microtubules .
|
-
- HY-14248R
-
|
|
Cytochrome P450
Autophagy
|
Cancer
|
|
Letrozole (Standard) is the analytical standard of Letrozole. This product is intended for research and analytical applications. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer .
|
-
- HY-N0457AR
-
|
|
HIV Integrase
HIV
Endogenous Metabolite
|
Infection
Cancer
|
|
L-Chicoric Acid (Standard) is the analytical standard of L-Chicoric Acid. This product is intended for research and analytical applications. L-Chicoric Acid ((-)-Chicoric acid) is a dicaffeoyltartaric acid and a potent, selective and reversible HIV-1 integrase inhibitor with an IC50 of ~100 nM. L-Chicoric Acid inhibits HIV-1 replication in tissue culture .
|
-
- HY-11002
-
|
|
ATM/ATR
|
Cancer
|
|
CP-466722 is a rapidly reversible inhibitor of ATM, with an IC50 of 0.41 μM, and has no effects on PI3K or closely related PI3K-like protein kinase (PIKK) family members.
|
-
- HY-13030
-
-
- HY-100514
-
-
- HY-112215
-
|
ARQ-531; MK-1026
|
Btk
|
Inflammation/Immunology
Cancer
|
|
ARQ 531 (MK-1026) is a reversible non-covalent and orally active inhibitor of Bruton’s Tyrosine Kinase (BTK), with IC50s of 0.85 nM and 0.39 nM for WT-BTK and C481S-BTK, respectively.
|
-
- HY-112885A
-
|
Nω-Hydroxy-nor-L-arginine acetate
|
Arginase
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
nor-NOHA acetate (Nω-Hydroxy-nor-L-arginine acetate) is a specific and reversible arginase inhibitor, induces apoptosis in ARG2-expressing cells under hypoxia but not normoxia. Anti-leukemic activity, effective in endothelial dysfunction, immunosuppression and metabolism .
|
-
- HY-P0322A
-
|
EMD 56574 TFA
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK TFA (EMD 56574 TFA) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK TFA is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK TFA is used to study the role of integrins in bone formation and resorption .
|
-
- HY-146313
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species .
|
-
- HY-151591
-
|
|
Phosphatase
|
Metabolic Disease
|
|
SPAA-52 is an orally active, competitive and reversible low-molecular-weight protein tyrosine phosphatase (LMW-PTP) inhibitor (IC50=4 nM, Ki=1.2 nM). SPAA-52 can be used in diabete research .
|
-
- HY-123490
-
|
INS50589
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Regrelor disodium (INS 50589) is a platelet P2Y12 receptor antagonist. Regrelor disodium is a well-tolerated, reversible ADP competitive antagonist. Regrelor disodium inhibits cell proliferation. Regrelor disodium can be used in inflammation-related research .
|
-
- HY-N0793R
-
|
|
Cholinesterase (ChE)
|
Infection
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Protopine (Standard) is the analytical standard of Protopine. This product is intended for research and analytical applications. Protopine (Corydinine), an isoquinoline alkaloid, is a specific reversible and competitive inhibitor of acetylcholinesterase. Protopine exhibits anti-inflammation, anti-microbial, anti-angiogenic and anti-tumour activity .
|
-
- HY-126175
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Neostigmine iodide is a reversible acetylcholinesterase inhibitor with muscle tone-enhancing activity. Neostigmine iodide is primarily used to improve muscle function in patients with myasthenia gravis. Neostigmine iodide is also used in routine anesthesia to reverse the effects of nondepolarizing muscle relaxants such as rocuronium .
|
-
- HY-103353
-
|
|
Cathepsin
Parasite
|
Infection
Cancer
|
|
SID 26681509 is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G .
|
-
- HY-144452
-
|
|
Proteasome
|
Cancer
|
|
Immunoproteasome inhibitor 1 is a potent, reversible, time-independent immunoproteasome and proteasome inhibitor (Kis of 1.18, 0.27, 1.91 μM in β5c, β1i, β5i submits, respectively). Immunoproteasome inhibitor 1 can be used for the research of certain neoplastic diseases .
|
-
- HY-10163S1
-
|
BIBR 953-d3; BIBR 953ZW-d3
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-10163S
-
|
BIBR 953-d4; BIBR 953ZW-d4
|
Isotope-Labeled Compounds
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-149515
-
|
|
Monoamine Oxidase
|
Cancer
|
|
MAO-IN-3 (Compound 5) is a reversible and competitive MAO inhibitor (Ki: 0.6 and 0.2 μM for MAO A and MAO B). MAO-IN-3 inhibits LN-229 glioblastoma cell proliferation with an IC50 of 0.8 μM. MAO-IN-3 can be used for cancer research .
|
-
- HY-162333
-
-
- HY-A0166R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin (Standard) is the analytical standard of Cilastatin. This product is intended for research and analytical applications. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct .
|
-
- HY-119185
-
|
|
Others
|
Cancer
|
|
AZD-6605 is a potent, reversible inhibitor of MMP2, MMP9, MMP12 and MMP13 with excellent selectivity. During drug development, AZD-6605 was optimized for activity, solubility and DMPK properties against MMP13 by replacing the zinc hydroxide binding group associated with historical inhibitors .
|
-
- HY-10285
-
|
BMS-477118
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
|
-
- HY-15185
-
|
PF-3084014
|
γ-secretase
Apoptosis
|
Cancer
|
|
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
|
-
- HY-B0423
-
|
Eustigmin bromide; Neoserine bromide
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Neostigmine (Eustigmin) Bromide is an orally active and reversible cholinesterase inhibitor that acts on myasthenia gravis to prolong and intensify the muscarinic and nicotinic effects of acetylcholine. Neostigmine Bromide can be used in anesthesia to reverse the neuromuscular blockade produced by competitive neuromuscular blockers .
|
-
- HY-125286
-
|
|
CD73
|
Cancer
|
|
AB-680 is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
|
-
- HY-10285A
-
|
BMS-477118 hydrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin hydrate (BMS-477118 hydrate) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrate has the peotential for type 2 diabetes mellitus research .
|
-
- HY-131342
-
|
|
Btk
|
Inflammation/Immunology
|
|
BIIB068 is a potent, selective, reversible and orally active BTK inhibitor with an IC50 of 1 nM and a Kd of 0.3 nM. BIIB068 shows more >400-fold selective for BTK than other kinases. BIIB068 has the potential for autoimmune diseases research .
|
-
- HY-16448
-
|
BMS-477118 hydrochloride
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research .
|
-
- HY-139984
-
|
|
Btk
|
Neurological Disease
Inflammation/Immunology
|
|
BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis .
|
-
- HY-126125
-
|
|
GSK-3
|
Neurological Disease
Metabolic Disease
|
|
CHIR-98023 is a potent, selective and reversible inhibitor of GSK3, with IC50s of 10 nM and 6.7 nM for GSK3α and GSK3β, respectively. CHIR-98023 can improve insulin action and glucose metabolism .
|
-
- HY-143244
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
|
-
- HY-143245
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
|
-
- HY-12041
-
|
|
JNK
Autophagy
Apoptosis
Ferroptosis
|
Cancer
|
|
SP600125 is an orally active, reversible, and ATP-competitive JNK inhibitor with IC50s of 40, 40 and 90 nM for JNK1, JNK2 and JNK3, respectively. SP600125 is a potent ferroptosis inhibitor. SP600125 induces the transformation of bladder cancer cells from autophagy to apoptosis .
|
-
- HY-15945
-
DBeQ
3 Publications Verification
JRF 12
|
p97
Autophagy
Apoptosis
|
Cancer
|
|
DBeQ is a selective, potent, reversible, and ATP-competitive p97 inhibitor, with an IC50 value of 1.5 μM and 1.6 μM for p97(wt) and p97(C522A), respectively; DBeQ also inhibits Vps4 with an IC50 of 11.5 μM.
|
-
- HY-B0590B
-
|
(+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine
|
Monoamine Transporter
|
Cancer
|
|
(+)-Tetrabenazine ((+)-TBZ; (3R,11bR)-TBZ; (3R,11bR)-Tetrabenazine) is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2), inhibits transport by VMAT2 with 10-fold greater potency than transport by VMAT1.
|
-
- HY-B0856
-
|
|
Fungal
Tyrosinase
Antibiotic
|
Infection
|
|
Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL . Validamycin A shows potent inhibitory activity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM . Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM .
|
-
- HY-N2554
-
|
Ostenol
|
Monoamine Oxidase
|
Neurological Disease
|
|
Osthenol (Ostenol), a prenylated coumarin isolated from the dried roots of Angelica pubescens, is selective, reversible, and competitive human monoamine oxidase-A (hMAO-A) inhibitor (Ki=0.26 µM). Osthenol potently inhibits recombinant hMAO-A with an IC50 of 0.74 µM and shows a high selectivity index for hMAO-A versus hMAO-B .
|
-
- HY-123517
-
|
|
Enterovirus
|
Infection
|
|
DC07090 dihydrochloride is a low toxicity, potent, reversible and competitive non-peptidyl human enterovirus 71 3C protease inhibitor with an IC50 and a Ki value for 21.72 μM and 23.29 μM. DC07090 dihydrochloride could also inhibit coxsackievirus A16 (CVA16) replication with an EC50 value of 27.76 μM .
|
-
- HY-108716
-
|
CBS9106; SL-801
|
CRM1
Apoptosis
|
Cancer
|
|
CBS9106 (SL-801) is a reversible oral CRM1 inhibitor with CRM1 degrading and antitumor activities. CBS9106, inhibits CRM1-dependent nuclear export, causing arrest of the cell cycle and inducing apoptosis in a time- and dose-dependent manner for a broad spectrum of cancer cells .
|
-
- HY-10163R
-
|
|
Thrombin
|
Cardiovascular Disease
Cancer
|
|
Dabigatran (Standard) is the analytical standard of Dabigatran. This product is intended for research and analytical applications. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM) .
|
-
- HY-108466
-
|
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Ro 08-2750 is a non-peptide and reversible nerve growth factor (NGF) inhibitor which binds to NGF, and with an IC50 of ~ 1 µM. Ro 08-2750 inhibits NGF binding to p75 NTR selectively over TRKA . Ro 08-2750 is a selective MSI RNA-binding activity inhibitor, with an IC50 of 2.7 μM .
|
-
- HY-103353A
-
|
|
Cathepsin
Parasite
|
Infection
Cancer
|
|
SID 26681509 quarterhydrate is a potent, reversible, competitive, and selective inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 quarterhydrate inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 quarterhydrate shows no inhibitory activity against cathepsin G .
|
-
- HY-W013636C
-
|
Alpha-Ketoglutaric acid potassium
|
Tyrosinase
|
Metabolic Disease
|
|
2-Ketoglutaric acid potassium (Alpha-Ketoglutaric acid potassium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid potassium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid potassium is a reversible inhibitor of tyrosinase with an IC50 value of 15 mM .
|
-
- HY-W013636
-
|
Alpha-Ketoglutaric acid
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-100540
-
|
GCA
|
Enterovirus
|
Infection
Cancer
|
|
Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1 . Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species .
|
-
- HY-N6608
-
|
Eserine
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning .
|
-
- HY-125286A
-
|
|
CD73
|
Cancer
|
|
AB-680 ammonium is a highly potent, reversible and selective inhibitor of CD73 (an ecto-nucleotidase), with a Ki of 4.9 pM for hCD73, displays >10,000-fold selectivity over related ecto-nucleotidases CD39. Anti-tumor activity .
|
-
- HY-143438
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
2-PAT, an analogue of Rasagiline and Selegiline, a reversible MAO-A inhibitor with an IC50 of 0.721 µM. 2-PAT is an inactivator of MAO-B with an IC50 of 14.6 µM. 2-PAT has the potential for Parkinson’s disease and depression research .
|
-
- HY-108342
-
|
|
JAK
|
Inflammation/Immunology
|
|
PF-00956980 is a reversible pan-JAK inhibitor with IC50 values of 2.2, 23.1 and 59.9 μM for JAK1, JAK2 and JAK3, respectively. PF-00956980 can be used in the research of lung and skin inflammatory diseases .
|
-
- HY-W099579
-
|
Kojic dipalmitate
|
Tyrosinase
|
Endocrinology
|
|
Kojic acid dipalmitate (Kojic dipalmitate) is a derivative of Kojic acid (HY-W050154), a fungal metabolite that can be produced by species of Aspergillus, Acetobacter and Penicillium. Kojic acid dipalmitate is a slow and reversible competitive inhibitor of tyrosinase. Kojic acid dipalmitate can be used for skin‐lightening agent research .
|
-
- HY-120901
-
|
|
SHP2
|
Cancer
|
|
II-B08 is a reversible and noncompetitive SHP2 inhibitor (IC50: 5.5 μM, 15.7, 14.3 μM for SHP2, SHP1, PTP1B). II-B08 can be used for cancer research .
|
-
- HY-112885C
-
|
Nω-Hydroxy-nor-L-arginine dihydrochloride
|
Apoptosis
Arginase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
nor-NOHA dihydrochloride is a selective and reversible arginase inhibitor. nor-NOHA dihydrochloride induces apoptosis in ARG2-expressing cells under hypoxia. nor-NOHA dihydrochloride has anti-leukemic activity. nor-NOHA dihydrochloride can used in study endothelial dysfunction, immunosuppression and metabolism .
|
-
- HY-169239
-
|
|
MAGL
|
Cancer
|
|
MAGL-IN-20 (compound ±34) is a reversible monoacylglycerol lipase (MAGL) inhibitor. MAGL-IN-20 exhibits appreciable antiproliferative activities against several cancer cells, including H460, HT29, CT-26, Huh7 and HCCLM-3.
|
-
- HY-135396
-
|
|
Proteasome
Apoptosis
|
Cancer
|
|
(1S,2S)-Bortezomib is an enantiomer of Bortezomib. Bortezomib is a cell-permeable, reversible, and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki of 0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is an anti-cancer agent and the first therapeutic proteasome inhibitor to be used in humans .
|
-
- HY-10227S
-
|
PS-341-d8; LDP-341-d8; NSC 681239-d8
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].
|
-
- HY-W013636A
-
|
Alpha-Ketoglutaric acid Sodium
|
Tyrosinase
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Ketoglutaric acid Sodium (Alpha-Ketoglutaric acid Sodium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid Sodium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid Sodium is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-120062
-
|
|
Fatty Acid Synthase (FASN)
|
Cancer
|
|
TVB-3664 is an orally available, reversible, potent, selective and highly bioavailable fatty acid synthase (FASN) inhibitor, with IC50 values of 18 nM and 12 nM for human and mouse cell palmitate synthesis, respectively. TVB-3664 significantly reduces tubulin palmitoylation and mRNA expression .
|
-
- HY-W013636B
-
|
|
Tyrosinase
Endogenous Metabolite
|
Metabolic Disease
|
|
Calcium 2-oxoglutarate is an intermediate in the production of ATP or GTP in the Krebs cycle. Calcium 2-oxoglutarate also acts as the major carbon skeleton for nitrogen-assimilatory reactions. Calcium 2-oxoglutarate is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-133130
-
|
|
MAGL
|
Neurological Disease
|
|
JNJ-42226314 is a competitive, highly selective and reversible non-covalent monoacylglycerol lipase (MAGL) inhibitor. JNJ-42226314 demonstrates dose-dependent enhancement of the major endocannabinoid 2-arachidonoylglycerol (2-AG) as well as efficacy in models of neuropathic and inflammatory pain .
|
-
- HY-139535
-
|
CG-806
|
FLT3
Btk
Apoptosis
|
Cancer
|
|
Luxeptinib (CG-806) is an orally active, reversible, first-in-class, non-covalent and potent pan-FLT3/pan-BTK inhibitor. Luxeptinib induces cell cycle arrest, apoptosis or autophagy in acute myeloid leukemia cells .
|
-
- HY-139664
-
|
|
DNA Methyltransferase
|
Cancer
|
|
GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-B0534S1
-
|
Ro111163-d4
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-162315
-
|
|
MAGL
|
Neurological Disease
|
|
MAGL-IN-16 (compound 27) is an oral active, selective and reversible MAGL inhibitor with the IC50 value of 10.3 nM. MAGL-IN-16 can increase the level of 2-AG and shows antidepressant effect in mouse depressed model caused by chronic restraint stress .
|
-
- HY-112885
-
|
Nω-Hydroxy-nor-L-arginine
|
Apoptosis
Arginase
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
nor-NOHA is a selective and reversible arginase inhibitor. nor-NOHA induces apoptosis in ARG2-expressing cells under hypoxia. nor-NOHA has anti-leukemic activity. nor-NOHA can used in study of endothelial dysfunction, immunosuppression and metabolism .
|
-
- HY-12853R
-
|
|
Reactive Oxygen Species
|
Others
|
|
Mesotrione (Standard) is the analytical standard of Mesotrione. This product is intended for research and analytical applications. Mesotrione is a herbicide belongs to the benzoylcyclohexanedione family. Mesotrione is a potent and competitive and reversible inhibitor of HPPD enzyme. Mesotrione is selective to maize due to rapid metabolism and relative high tolerance by the susceptible crop plant .
|
-
- HY-114895
-
|
|
GlyT
|
Neurological Disease
|
|
SSR504734 free base is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 (IC50=18, 15, and 38?nM, respectively). SSR504734 free base shows anti-schizophrenia, anti-anxiety and anti-depression activities .
|
-
- HY-133016
-
|
|
MetAP
|
Cardiovascular Disease
Cancer
|
|
M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
|
-
- HY-117769
-
|
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
|
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer .
|
-
- HY-14879AR
-
|
|
Beta-lactamase
Bacterial
Antibiotic
|
Infection
|
|
Avibactam (sodium) (Standard) is the analytical standard of Avibactam (sodium). This product is intended for research and analytical applications. Avibactam sodium (NXL-104) is a covalent and reversible non-β-lactam β-lactamase inhibitor which inhibits β-lactamase TEM-1 and CTX-M-15 with IC50s of 8 nM and 5 nM, respectively .
|
-
- HY-14248S
-
|
|
Isotope-Labeled Compounds
Cytochrome P450
Autophagy
|
Cancer
|
|
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].
|
-
- HY-118628
-
|
N-(p-Amylcinnamoyl) anthranilic acid; ACA
|
Phospholipase
TRP Channel
|
Cardiovascular Disease
|
|
(E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is a broad spectrum Phospholipase A2 (PLA2) inhibitor and TRP channel blocker . (E/Z)-BML264 (N-(p-amylcinnamoyl) Anthranilic Acid) is also an effective reversible inhibitor of calcium-activated chloride channels, has potential to treat arrhythmia .
|
-
- HY-15816A
-
|
BVD-523 hydrochloride; VRT752271 hydrochloride
|
ERK
|
Cancer
|
|
Ulixertinib hydrochloride (BVD-523 hydrochloride) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib hydrochloride inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
|
-
- HY-126075
-
|
|
E1/E2/E3 Enzyme
|
Cancer
|
|
WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2 .
|
-
- HY-120139
-
KMH-233
1 Publications Verification
|
Others
|
Cancer
|
|
KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-120019
-
|
L-709049
|
Interleukin Related
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO is also a caspase-1 inhibitor. Ac-YVAD-CHO can suppress the production of mature IL-lβ .
|
-
- HY-120019A
-
|
L-709049 acetate
|
Interleukin Related
Caspase
Apoptosis
|
Inflammation/Immunology
|
|
Ac-YVAD-CHO (L-709049) acetate is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO acetate is also a caspase-1 inhibitor. Ac-YVAD-CHO acetate can suppress the production of mature IL-lβ .
|
-
- HY-10163S2
-
|
BIBR 953-13C6; BIBR 953ZW-13C6
|
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
|
-
- HY-15695
-
|
NSC 3056
|
Bacterial
Apoptosis
Dipeptidyl Peptidase
Aminopeptidase
Antibiotic
|
Cancer
|
|
Puromycin aminonucleoside (NSC 3056) is the aminonucleoside portion of the antibiotic puromycin, and used in nephrosis animal models . Puromycin aminonucleoside induces apoptosis . Puromycin aminonucleoside is a reversible inhibitor of dipeptidyl peptidase II and cytosol alanyl aminopeptidase . Puromycin aminonucleoside induces secretion of cell migrasome .
|
-
- HY-100027A
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A). An homogeneous population of high affinity binding sites for [ 3H]Ro 41-1049 is found in membrane preparations from human frontal cortex and placenta (Kd values of 16.5 and 64.4 nM, respectively) .
|
-
- HY-102046
-
FM-381
1 Publications Verification
|
JAK
|
Inflammation/Immunology
|
|
FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
|
-
- HY-15185B
-
|
PF-3084014 dihydrobromide; PF-03084014 dihydrobromide
|
γ-secretase
Apoptosis
|
Cancer
|
|
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
|
-
- HY-129944
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
MJ33-OH is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-111538
-
|
|
MAGL
|
Cancer
|
|
MAGL-IN-1 is a potent, selective, reversible and competitive inhibitor of MAGL, with an IC50 of 80 nM. MAGL-IN-1 exhibits anti-proliferative effects against human breast, colorectal, and ovarian cancer cells. MAGL-IN-1 blocks MAGL in cell-based as well as in vivo assays .
|
-
- HY-121467A
-
|
Z-338; YM443
|
Cholinesterase (ChE)
|
Others
Metabolic Disease
Inflammation/Immunology
|
|
Acotiamide hydrochloride is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide hydrochloride can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide hydrochloride has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
|
-
- HY-121467
-
|
Z-338 free base; YM443 free base
|
Cholinesterase (ChE)
|
Metabolic Disease
Inflammation/Immunology
|
|
Acotiamide is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with an IC50 of 1.79 μM. Acotiamide can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
|
-
- HY-160168
-
-
- HY-P10169
-
|
|
Proteasome
|
Others
|
|
Acetyl-Calpastatin(184-210)(human), Negative Control is a control scramble peptide of Acetyl-Calpastatin(184-210)(human) (HY-P1081). Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor .
|
-
- HY-B0199AS
-
|
RS 61443-d4 hydrochloride; TM-MMF-d4 hydrochloride
|
Bacterial
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
|
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-10227R
-
|
|
Proteasome
NF-κB
Apoptosis
Autophagy
|
Cancer
|
|
Bortezomib (Standard) is the analytical standard of Bortezomib. This product is intended for research and analytical applications. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity .
|
-
- HY-B0532
-
|
|
Dopamine Receptor
Adrenergic Receptor
P-glycoprotein
CaMK
Influenza Virus
Autophagy
|
Neurological Disease
|
|
Trifluoperazine, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine is a potent α1-adrenergic receptor antagonist. Trifluoperazine is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine can be used for the research of schizophrenia. Trifluoperazine acts as a reversible inhibitor of influenza virus morphogenesis .
|
-
- HY-B0532A
-
|
|
Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
|
Neurological Disease
Cancer
|
|
Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis .
|
-
- HY-162675
-
|
|
GSK-3
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
COB-187 is a potent, ATP-competitive and selective inhibitor of GSK-3β. COB-187 inhibits GSK-3 through a reversible and Cysteine (Cys)-199-dependent mechanism. COB-187 inhibits LPS induced cytokine production and SARS-CoV-2 spike protein-induced CXCL10 production .
|
-
- HY-100859
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-5 (Compound 4e) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 121 nM. LSD1-IN-5 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1 .
|
-
- HY-100860
-
|
|
Histone Demethylase
|
Cancer
|
|
LSD1-IN-6 (Compound 4m) is a potent and reversible inhibitor of lysine-specific demethylase 1 (LSD1), with an IC50 of 123 nM. LSD1-IN-6 increases dimethylated Lys4 of histone H3, shows no effect on expression of LSD1 .
|
-
- HY-129944A
-
|
|
Phospholipase
|
Inflammation/Immunology
|
|
MJ33-OH lithium is a metabolite of MJ33. MJ33 is an active-site-directed, specific, competitive, and reversible phospholipase A2 (PLA2) inhibitor. MJ33 blocks the calcium-independent phospholipase A2 (iPLA2) activity of Prdx6 .
|
-
- HY-120824
-
|
|
COX
|
Inflammation/Immunology
|
|
Mofezolac, a non-steroidal anti-inflammatory drug (NSAID), is a selective, reversible and orally active COX-1 inhibitor with an IC50 of 1.44 nM. Mofezolac shows weak inhibitory activity on COX-2 (IC50 of 447 nM). Mofezolac can relieve pain and has anti-inflammatory activities .
|
-
- HY-W083062
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-5(B15) is a potent, selective and reversible inhibitor of human monoamine oxidase hMAO-B with IC50 of 0.12 μM. hMAO-B-IN-5 can pass through the blood-brain barrier and can be used in the research of neurodegenerative diseases .
|
-
- HY-161029
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (Ki=22 nM, IC50=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .
|
-
- HY-B0534R
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide (Standard) is the analytical standard of Moclobemide. This product is intended for research and analytical applications. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-14721A
-
|
EMD-1214063 hydrochloride
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (EMD-1214063) hydrochloride is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib hydrochloride inhibits c-Met phosphorylation and induces autophagy. Tepotinib hydrochloride has antitumor effects .
|
-
- HY-13007
-
|
PF-03758309
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-15237
-
|
SL0101
|
Ribosomal S6 Kinase (RSK)
|
Cancer
|
|
SL 0101-1 (SL0101), a kaempferol glycoside, isolated from the tropical plant F. refracta, is a cell-permeable, selective, reversible, ATP-competitive p90 Ribosomal S6 Kinase (RSK) inhibitor, with an IC50 of 89 nM . SL 0101-1 (SL0101) is a selective RSK1/2 inhibitor, with a Ki of 1 μM .
|
-
- HY-130173
-
|
|
Bacterial
Fungal
Na+/K+ ATPase
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Bafilomycin C1 is a macrolide antibiotic isolated from Streptomyces sp. Bafilomycin C1 is a potent, specific and reversible inhibitor of vacuolar-type H +-ATPases (V-ATPases). Bafilomycin C1 inhibits growth of gram-positive bacteria and fungi . Bafilomycin C1 induces cell apoptosis and can be used for the study of hepatocellular carcinoma (HCC) .
|
-
- HY-13007B
-
|
PF-03758309 dihydrochloride
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) dihydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 dihydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-13007A
-
|
PF-03758309 hydrochloride
|
PAK
Apoptosis
|
Cancer
|
|
PF-3758309 (PF-03758309) hydrochloride is a potent, orally available, and reversible ATP-competitive inhibitor of PAK4 (Kd= 2.7 nM; Ki=18.7 nM). PF-3758309 hydrochloride has the expected cellular functions of a PAK4 inhibitor: inhibition of anchorage-independent growth, induction of apoptosis, cytoskeletal remodeling, and inhibition of proliferation .
|
-
- HY-117596
-
UNC569
1 Publications Verification
|
TAM Receptor
|
Cancer
|
|
UNC569 is a potent, reversible, ATP-competitive and orally active Mer kinase inhibitor with an IC50 of 2.9 nM and a Ki of 4.3 nM. UNC569 also inhibits Axl and Tyro3 with IC50s of 37 nM and 48 nM, respectively. UNC569 can be used for acute lymphoblastic leukemia (ALL) and atypical teratoid/rhabdoid tumors research
|
-
- HY-10163S3
-
|
BIBR 953-13C,d3; BIBR 953ZW-13C,d3
|
Isotope-Labeled Compounds
Thrombin
|
Cardiovascular Disease
|
|
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
- HY-A0166S
-
|
MK0791-15N,d3
|
Bacterial
Antibiotic
|
Infection
|
|
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
|
-
- HY-113604
-
|
|
TGF-β Receptor
|
Cancer
|
Pentabromopseudilin (PBrP) is a marine antibiotic isolated from the marine bacteria Pseudomonas bromoutilis and Alteromonas luteoviolaceus. PBrP exhibits antimicrobial, anti-tumour and phytotoxic activities. PBrP is a reversible and allosteric inhibitor of myosin Va (MyoVa). PBrP also is a potent inhibitor of transforming growth factor-β (TGF-β) activity. PBrP can be used for the research of fibrotic diseases and cancer .
|
-
- HY-149889
-
|
|
Apoptosis
EGFR
|
Cancer
|
|
EGFR-IN-78 (compound A5)，a 2-aminopyrimidine derivative，is a reversible inhibitor of EGFR C797S-TK，and also an inducer of apoptosis. EGFR-IN-78 shows anti-proliferative activity，inhibits EGFR phosphorylation and arrests cell cycle at G2/M phase .
|
-
- HY-14721
-
|
EMD-1214063
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation and induces autophagy. Tepotinib has antitumor effects .
|
-
- HY-120631A
-
|
|
Others
|
Others
|
|
BMS-538305 hydrochloride is a potent and selective inhibitor of dipeptidyl peptidase IV (DPP-IV), exhibiting strong biological activity by forming a reversible covalent complex with the enzyme. BMS-538305 hydrochloride demonstrates its mechanism of action through the covalent attachment between the nitrile carbon of the inhibitor and the enzyme residue S630, as unveiled by the X-ray crystal structure analysis.
|
-
- HY-18637
-
|
|
Deubiquitinase
Apoptosis
|
Neurological Disease
|
|
LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
|
-
- HY-B0034S1
-
|
E2020-d4
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Donepezil-d4 (hydrochloride) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
|
-
- HY-N1919
-
|
Raubasine
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-23460
-
|
4-Ethynyl-L-phenylalanine
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-112885B
-
|
Nω-Hydroxy-nor-L-arginine monoacetate
|
Arginase
|
Metabolic Disease
|
|
nor-NOHA monoacetate is a selective and reversible arginase inhibitor. nor-NOHA monoacetate induces apoptosis in ARG2-expressing cells under hypoxia. nor-NOHA monoacetate has anti-leukemic activity. nor-NOHA monoacetate can used in study of endothelial dysfunction, immunosuppression and metabolism .
|
-
- HY-23460A
-
|
4-Ethynyl-L-phenylalanine hydrochloride
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-B1266
-
|
Eserine salicylate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning .
|
-
- HY-115747
-
|
|
Histone Demethylase
|
Cancer
|
|
Namoline, a γ-pyrone, is a selective and reversible Lysine-specific demethylase 1 (LSD1) inhibitor with an IC50 of 51 μM in a HRP-coupled enzymatic assay. Namoline impairs LSD1 demethylase activity and blocks cell proliferation. Namoline has the potential for androgen-dependent prostate cancer research .
|
-
- HY-143264
-
|
|
FAAH
MAGL
|
Neurological Disease
|
|
FAAH/MAGL-IN-2 is a potent, reversible, orally active, and cross the blood-brain barrier FAAH and MAGL inhibitor with IC50s of 11 nM and 36 nM (Kis of 28 nM and 60 nM), respectively . FAAH/MAGL-IN-2 has the potential to research neuropathic pain without causing locomotion impairment .
|
-
- HY-118424
-
|
|
iGluR
|
Neurological Disease
|
|
JNJ-55511118 is a highly potent, reversible, and selective AMPA receptor inhibitor selective for TARP-γ8. JNJ-55511118 fully displaces the radioligand (20 nM) with the Ki of 26 nM in competition binding experiments. JNJ-55511118 is a tool molecule with potential therapeutic utility as an anticonvulsant or neuroprotectant .
|
-
- HY-B0034S
-
|
E2020-d5
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
|
-
- HY-N1919A
-
|
Raubasine hydrochloride
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-152104
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-9 (Compound 19) is a potent, reversible and orally active FGFR inhibitor with an IC50 of 17.1, 29.6, 30.7, 46.7 and 64.3 nM against FGFR4 WT, FGFR3, FGFR4 V550L, FGFR2 and FGFR1, respectively .
|
-
- HY-143329
-
-
- HY-N9933
-
|
TβMCA
|
FXR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Tauro-β-muricholic acid (TβMCA) is a trihydroxylated bile acid. Tauro-β-muricholic acid is a competitive and reversible FXR antagonist (IC50 = 40 μM). Tauro-β-muricholic acid has antiapoptotic effect. Tauro-β-muricholic acid inhibits bile acid-induced hepatocellular apoptosis by maintaining the mitochondrial membrane potential .
|
-
- HY-B0590R
-
|
|
Monoamine Transporter
|
Neurological Disease
|
|
Tetrabenazine (Standard) is the analytical standard of Tetrabenazine. This product is intended for research and analytical applications. Tetrabenazine (Ro 1-9569) is a reversible inhibitor of the vesicular monoamine transporter VMAT2 with the Kd value of 1.34 nM. Tetrabenazine can be used for research on diseases related to hyperactive movement disorders such as Huntington's disease .
|
-
- HY-100558
-
Bafilomycin A1
Maximum Cited Publications
465 Publications Verification
BafA1
|
Proton Pump
Autophagy
Antibiotic
Bacterial
Apoptosis
|
Infection
Cancer
|
|
Bafilomycin A1 (BafA1) is a specific and reversible inhibitor of vacuolar H +-ATPase (V-ATPase) with IC50 values of 4-400 nmol/mg. Bafilomycin A1, a macrolide antibiotic, is also used as an autophagy inhibitor at the late stage. Bafilomycin A1 blocks autophagosome-lysosome fusion and inhibits acidification and protein degradation in lysosomes of cultured cells. Bafilomycin A1 induces apoptosis .
|
-
- HY-119307
-
|
TMI-005
|
MMP
TNF Receptor
|
Cancer
|
|
Apratastat (TMI-005) is an orally active, non-selective and reversible TACE/MMPs inhibitor, can inhibit inhibit the release of TNF-α. Apratastat has the potential to overcome radiotherapy-resistance in non-small cell lung cancer (NSCLC) . Apratastat is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-P1259
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-117822
-
|
|
GSK-3
|
Neurological Disease
|
|
BRD0209 is a potent, selective and dual inhibitor of GSK3α/β inhibitor (GSK3α IC50 = 19 nM; GSK3β IC50 = 5 nM). BRD0209 is also a reversible ATP-competitive inhibitor with fast-off kinetics (Ki = 4.2 nM, respectively). BRD0209 is a tricyclic pyrazolotetrahydroquinolinone compound. BRD0209 has the potential for the research of mood disorder diseases .
|
-
- HY-156441
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-65 (compound 2f (81)) is a potent,orally active and reversible SARS-CoV-2 entry inhibitor. SARS-CoV-2-IN-65 inhibits the pseudovirus entry in a ACE2-dependent pathway, via mainly inhibiting RBD:ACE2 interaction and TMPRSS2 activity in Calu-3 cells .
|
-
- HY-103713
-
|
SP-2577
|
Histone Demethylase
|
Cancer
|
|
Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma .
|
-
- HY-107794
-
|
Disodium clodronate tetrahydrate
|
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl - competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
|
-
- HY-118567
-
|
BMOV
|
SHP2
Phosphatase
|
Metabolic Disease
|
|
Bis(maltolato)oxovanadium(IV) (BMOV) is a potent, reversible, competitive and orally active pan-PTP (protein tyrosine phosphatases) inhibitor. Bis(maltolato)oxovanadium(IV) inhibits HCPTPA, PTP1B, HPTPβ and SHP2 with IC50s of 126 nM, 109 nM, 26 nM and 201 nM, respectively. Bis(maltolato)oxovanadium(IV) is a potent insulin sensitizer .
|
-
- HY-123564
-
|
|
Others
|
Others
|
|
Mcl1-IN-7 (compound 11) is a reversible covalent inhibitor of Mcl-1 with the activity of inhibiting Mcl-1. By covalently targeting the non-catalytic lysine side chain of Mcl-1, it has higher potency than non-covalent counterparts and can be used to develop Mcl-1 inhibitory compounds and study related biological phenomena.
|
-
- HY-10521
-
|
SB-480848
|
Phospholipase
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Darapladib (SB-480848) is an orally active, selective and reversible Lp-PLA2 inhibitor (IC50=0.25 nM). Darapladib can trigger irreversible actions on glioma cell apoptosis and induce cycle arrest. Darapladib can be used in the study of atherosclerosis and cancer .
|
-
- HY-15517
-
KN-92
5 Publications Verification
|
Others
|
Cancer
|
|
KN-92 is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-15517A
-
|
|
Others
|
Cancer
|
|
KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 phosphate is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-16214
-
|
LDHA inhibitor FX11
|
Lactate Dehydrogenase
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
FX-11 is a potent, selective, reversible and competitive lactate dehydrogenase A (LDHA) inhibitor, with a Ki of 8 μM. FX-11 reduces ATP levels and induces oxidative stress, ROS production and cell death. FX-11 shows antitumor activity in lymphoma and pancreatic cancer xenografts .
|
-
- HY-117290
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
BMS-962212 is a direct, reversible, selective factor XIa (FXIa) inhibitor . BMS-962212 is well tolerated, with fast onset of pharmacodynamic (PD) responses and rapid elimination. BMS-962212 increases exposure dependently in activated partial thromboplastin time, and decreases exposure dependently in FXI clotting activity .
|
-
- HY-N2320
-
|
Eserine hemisulfate
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine hemisulfate (Eserine hemisulfate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine hemisulfate can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine hemisulfate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine hemisulfate is also an antidote for anticholinergic poisoning .
|
-
- HY-115944
-
|
|
Btk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BTK-IN-9 is a reversible BTK inhibitors with potent antiproliferative activity in mantle cell lymphoma. BTK-IN-9 specifically disturbs mitochondrial membrane potential and increases reactive oxygen species level in Z138 cells. BTK-IN-9 also induces cell apoptosis in Z138 cells .
|
-
- HY-147953
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-13 (compound 12a) is a highly potent, reversible and blood-brain barrier (BBB) penetrant MAO-B inhibitor with an IC50 value of 10 nM. MAO-B-IN-13 has neuroprotective and antioxidant activity. MAO-B-IN-13 can be used for researching Parkinson’s disease .
|
-
- HY-147328
-
|
|
Apoptosis
|
Cancer
|
|
LCS3 is a reversible and uncompetitive glutathione disulfide reductase (GSR) and thioredoxin reductase 1 (TXNRD1) inhibitor (IC50=3.3 µM and 3.8 µM, respectively). LCS3 shows anti-tumor activity, and induces apoptosis. LCS3 can be used in lung adenocarcinoma (LUAD) research .
|
-
- HY-N4037
-
|
(-)-Homopterocarpin; 3,9-Dimethoxypterocarpan
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
Homopterocarpin is an isoflavonoid that can be isolated from Pterocarpus erinaceus. Homopterocarpin has hepatoprotective and antioxidant properties. Homopterocarpin is a competitive reversible inhibitor of human monoamine oxidase-B with an IC50 and a Ki of 0.72 and 0.21 μM for hMAO-B, respectively. Homopterocarpin can be used for the research of liver injury and oxidative stress .
|
-
- HY-50667R
-
|
|
Factor Xa
|
Cardiovascular Disease
Cancer
|
|
Apixaban (Standard) is the analytical standard of Apixaban. This product is intended for research and analytical applications. Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases .
|
-
- HY-B0034R
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
Cancer
|
|
Donepezil (Hydrochloride) (Standard) is the analytical standard of Donepezil (Hydrochloride). This product is intended for research and analytical applications. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE . Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity .
|
-
- HY-114737
-
|
|
Bacterial
|
Infection
|
|
L-573655 is a reversible inhibitor of UDP-3-O-[R-3-hydroxymyristoyl]-GlcNAc deacetylase with an IC50 value of 8.5 μM. L-573655 possesses antibacterial activity against a wild-type strain of E. coli. with MIC values of 200-400 μg/mL .
|
-
- HY-100655R
-
|
|
Drug Metabolite
|
Cardiovascular Disease
|
|
O-Desmethyl apixaban (Standard) is the analytical standard of O-Desmethyl apixaban. This product is intended for research and analytical applications. O-Desmethyl apixaban is a metabolite of Apixaban (BMS-562247-01) . Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively .
|
-
- HY-116171
-
|
|
Proteasome
|
Cardiovascular Disease
Neurological Disease
|
|
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I (μ-calpain, Ki=19 nM). (Rac)-Calpain Inhibitor XII has lower affinities for calpain II (m-calpain, Ki=120 nM) and cathepsin B (Ki=750 nM). (Rac)-Calpain Inhibitor XII has the potential for studying the role of calpains in diverse processes, including neutrophil chemotaxis, neuronal signaling, and cardiac response to injury .
|
-
- HY-B0607
-
|
NTBC; Nitisone; SC0735
|
HPPD
|
Metabolic Disease
|
|
Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-B0986
-
|
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
Endogenous Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage .
|
-
- HY-127105
-
|
LNP023
|
Complement System
|
Metabolic Disease
Inflammation/Immunology
|
|
Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
|
-
- HY-N0313
-
|
|
MAGL
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Euphol is a tetracyclic triterpene alcohol isolated from the sap of Euphorbia tirucalli with anti-mutagenic, anti-inflammatory and immunomodulatory effects, orally active. Euphol inhibits the monoacylglycerol lipase (MGL) activity via a reversible mechanism (IC50=315 nM). MGL inhibition in the periphery modulates the endocannabinoid system to block the development of inflammatory pain .
|
-
- HY-100642S
-
|
Ro 40-7591 d7
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone-d7 is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
- HY-125365
-
|
|
Bacterial
Reactive Oxygen Species
Antibiotic
|
Infection
|
|
Rifamycin S, a quinone, is an antibiotic against Gram-positive bacteria (including MRSA). Rifamycin S is the oxidized forms of a reversible oxidation-reduction system involving two electrons. Rifamycin S generates reactive oxygen species (ROS) and inhibits microsomal lipid peroxidation. Rifamycin S can be used for tuberculosis and leprosy .
|
-
- HY-15999A
-
|
PRT062070 hydrochloride; PRT2070 hydrochloride
|
Syk
JAK
|
Cancer
|
|
Cerdulatinib hydrochloride (PRT062070) is a selective, oral active and reversible ATP-competitive inhibitor of dual SYK and JAK, with IC50s of 32 nM, 0.5 nM, 12 nM, 6 nM and 8 nM for SYK and Tyk2, JAK1, 2, 3, respectively. Cerdulatinib hydrochloride could be used to research autoimmune disease and B-cell malignancies .
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-
- HY-132310
-
|
|
MAGL
|
Neurological Disease
|
|
MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
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-
- HY-100540A
-
|
(Rac)-GCA
|
Enterovirus
|
Infection
|
|
(Rac)-Golgicide A ((Rac)-GCA) is a racemate of Golgicide A. Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1 .Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species .
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-
- HY-115750
-
|
|
NO Synthase
|
Neurological Disease
|
|
Nω-allyl-L-arginine is a competitive and reversible inhibitor of bovine brain nitric oxide synthase (nNOS). Nω-allyl-L-arginine can inactivate nNOS in a time-dependent manner. Nω-allyl-L-arginine also is a substrate, producing L-arginine, acrolein, and H2O .
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-
- HY-153365
-
|
|
Deubiquitinase
|
Cancer
|
|
I-138 is an orally active, reversible inhibitor of USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM), structurally related to ML323 (HY-17543). I-138 induces monoubiquitination of FANCD2 and PCNA in cells and eliminates USP1 autocleavage in cells .
|
-
- HY-149528
-
|
|
Monoamine Oxidase
Cholinesterase (ChE)
|
Cancer
|
|
MAO-B-IN-24 (compound 11h) is a selective, reversible, competitive inhibitor of MAO-B (IC50: 1.60 μM). MAO-B-IN-24 also inhibited MAO-A (22.42 μM); at 10 μM concentration, it also reduced AChE and BChE activities to 54.58% and 88.43% .
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-
- HY-B0534S
-
|
Ro111163-d8
|
Isotope-Labeled Compounds
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
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-
- HY-162565
-
|
|
STK33
CDK
RET
|
Endocrinology
|
|
CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC50 of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive .
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-
- HY-N1581R
-
|
|
Parasite
|
Infection
Endocrinology
|
|
Quassin (Standard) is the analytical standard of Quassin. This product is intended for research and analytical applications. Quassin (Nigakilactone D) is a bioactive triterpenoid from stem bark extract of Quassia amara. Quassin inhibits P. falciparum with an IC50 of 0.15 μM. Quassin possesses reversible antifertility, anti-estrogenic and anti-plasmodial activity .
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-
- HY-W013256R
-
|
|
DNA/RNA Synthesis
|
Infection
|
|
Foscarnet (trisodium hexahydrate) (Standard) is the analytical standard of Foscarnet (trisodium hexahydrate). This product is intended for research and analytical applications. Foscarnet trisodium hexahydrate (Trisodium phosphonatoformate hexahydrate) is a viral DNA polymerase activity inhibitor, leading to reversible suppression of viral replication. Foscarnet trisodium hexahydrate is an antiherpesvirus agent used in cytomegalovirus retinitis .
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-
- HY-P1259A
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
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-
- HY-19840
-
|
GS-9857
|
HCV Protease
|
Infection
Cancer
|
|
Voxilaprevir (GS-9857) is a noncovalent, reversible inhibitor of HCV NS3/4A protease inhibitor (PI) with pangenotypic antiviral activity . Voxilaprevir inhibits genotype 1b and 3a wild-type NS3 proteases with Ki values of 0.038 nM and 0.066 nM, respectively . Voxilaprevir is an orally active direct-acting antiviral agent (DAA) and can be used for HCV infection research .
|
-
- HY-124704
-
|
|
Others
|
Neurological Disease
|
|
Chst15-IN-1 is a potent reversible covalent Chst15 inhibitor. Chst15-IN-1 effectively inhibits chondroitin sulfate-E (CS-E) sulfation levels and other closely related glycosaminoglycans (GAG) sulfotransferases. Chst15-IN-1, as a selective sulfotransferase inhibitor, can diminish the inhibitory effects of chondroitin sulfate proteoglycans (CSPGs), and can be used for the stimulation of neuronal repair .
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-
- HY-N12763
-
|
SNH
|
Bacterial
Renin
|
Inflammation/Immunology
|
|
Sodium new houttuyfonate (SNH) is a partially reversible NDM-1 inhibitor with an IC50 of 14.2 μM. Sodium new houttuyfonate is an inhibitor against renin and angiotensin I converting enzyme (ACE). Sodium new houttuyfonate can recover the antibacterial activity of Meropenem (HY-13678) against E. coli BL21/pET15b-blaNDM-1 .
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-
- HY-15816
-
|
BVD-523; VRT752271
|
ERK
|
Cancer
|
|
Ulixertinib (BVD-523; VRT752271) is a potent, orally active, highly selective, ATP-competitive and reversible covalent inhibitor of ERK1/2 kinases, with an IC50 of <0.3 nM against ERK2. Ulixertinib (BVD-523; VRT752271) inhibits the phosphorylated ERK2 (pERK) and downstream kinase RSK (pRSK) in an A375 melanoma cell line .
|
-
- HY-18010
-
|
|
Btk
BCRP
|
Inflammation/Immunology
|
|
PCI 29732 is a potent, orally active, reversible BTK inhibitor with Ki app values of 8.2, 4.6, and 2.5 nM for BTK, Lck and Lyn, respectively. PCI 29732 shows only modest inhibitory activity against Itk, another Tec family kinase. PCI 29732 inhibits the function of ABCG2 by competitively binding to the ATP-binding site of ABCG2 .
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-
- HY-N0063
-
|
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
|
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CL pro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
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-
- HY-50887
-
|
|
Cathepsin
|
Metabolic Disease
|
|
L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC50s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively . L-873724 also exhibits an IC50 of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption .
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-
- HY-161700
-
|
|
Cytochrome P450
|
Cancer
|
|
BMS-737 (compound 33) is a non-steroidal, reversible small molecule inhibitor. BMS-737 exhibits 11-fold selectivity for CYP17 lyase over CYP17 hydroxylase. BMS-737 is designed to inhibit castration-resistant prostate cancer (CRPC) and significantly reduces testosterone levels without significant effects on orrodermal hormone and glucocorticoid levels .
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-
- HY-113725
-
|
|
Others
|
Others
|
|
L 668411 is a β-lactone inhibitor with activity against 3-hydroxy-3-methylglutaryl-CoA synthase and cholesterol biosynthesis. L 668411 inhibits rat liver cytosolic 3-hydroxy-3-methylglutaryl-CoA synthase and [14C] acetate incorporation into sterols in cultured Hep G2 cells, and the inhibition appears to be irreversible in cells but reversible in cultured cells and animals.
|
-
- HY-B0532AS
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
Adrenergic Receptor
CaMK
P-glycoprotein
Influenza Virus
Autophagy
|
Neurological Disease
Cancer
|
|
Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis[1][2][3][4][5].
|
-
- HY-B0532B
-
|
|
Dopamine Receptor
Adrenergic Receptor
P-glycoprotein
CaMK
Influenza Virus
Autophagy
|
Infection
Neurological Disease
Cancer
|
|
Trifluoperazine dimaleate, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dimaleate is a potent α1-adrenergic receptor antagonist. Trifluoperazine dimaleate is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dimaleate is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dimaleate can be used for the research of schizophrenia. Trifluoperazine dimaleate acts as a reversible inhibitor of influenza virus morphogenesis .
|
-
- HY-125039
-
|
|
Glutathione Peroxidase
|
Cardiovascular Disease
Neurological Disease
|
|
N-Acetyl lysyltyrosylcysteine amide is a potent, reversible, specific, and non-toxic tripeptide inhibitor of myeloperoxidase (MPO). N-Acetyl lysyltyrosylcysteine amide effectively inhibits MPO generation of toxic oxidants in vivo. N-Acetyl lysyltyrosylcysteine amide reduces neuronal damage and preserves brain tissue and neurological function in the stroked brain. N-Acetyl lysyltyrosylcysteine amide inhibits MPO-dependent hypochlorous acid (HOCl) generation, protein nitration, and LDL oxidation .
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-
- HY-162573
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 5 (Compound 16d) is a selective and reversible inhibitor for monoamine oxidase B (hMAO-B) with an IC50 of 67.3 nM and a Ki of 82.5 nM. Monoamine Oxidase B inhibitor 5 exhibits good pharmacokinetic characters and weak toxicity in rats model. Monoamine Oxidase B inhibitor 5 alleviates MPTP-induced (HY-15608) motor impairment in Parkinson’s mouse model. Monoamine Oxidase B inhibitor 5 is blood-brain barrier (BBB) penetrate .
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-
- HY-10285R
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Saxagliptin (Standard) is the analytical standard of Saxagliptin. This product is intended for research and analytical applications. Saxagliptin (BMS-477118) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin has the peotential for type 2 diabetes mellitus research .
|
-
- HY-N6608S
-
|
Eserine-d3
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
|
-
- HY-16482
-
|
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
|
|
Teglicar is a selective and reversible orally active liver isoform of carnitine palmitoyl-transferase 1 (L-CPT1) inhibitor with an IC50 value of 0.68 μM and a Ki value of 0.36 μM. Teglicar has a potential antihyperglycemic propert. Teglicar can be used for the research of diabetes and neurodegenerative disease including Huntington's disease (HD) .
|
-
- HY-B2155
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
Inflammation/Immunology
|
|
Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
|
-
- HY-100642S1
-
|
Ro 40-7591-d4
|
Isotope-Labeled Compounds
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone-d4 is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
- HY-146039
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE-IN-15 (Compound 3d) is a reversible human acetylcholinesterase (huAChE) (IC50=6.8 μM) and human butyrylcholinesterase (huBChE) (IC50=16.1 μM) inhibitor. AChE-IN-15 shows significant antioxidant potency, AChE-IN-15 can be used for the research of Alzheimer’s disease .
|
-
- HY-117884
-
|
|
Apoptosis
|
Cancer
|
|
(Rac)-CCT 250863 (compound rac-21) is a selective and reversible NEK 2 inhibitor with an IC50 of 0.073 µM. (Rac)-CCT 250863 shows good effects of inducing cell cycle arrest and also can antiproliferative in cells (Pomalidomide sensitive/resistant). (Rac)-CCT 250863 induces apoptosis when combines with Pomalidomide .
|
-
- HY-155137
-
|
|
Monoamine Oxidase
Reactive Oxygen Species
|
Neurological Disease
|
|
CHBO4 is a potent, reversible, competitive, and selective hMAO-B inhibitor with an IC50 value of 0.031 μM in CHBO subseries and an Ki value of 0.010 ± 0.005 μM. CHBO4 reduce cell damage by scavenging intracellular reactive oxygen species (ROS). CHBO4 can be used for Parkinson's Disease (PD) research .
|
-
- HY-155612
-
|
|
Caspase
|
Neurological Disease
|
|
M826 is a potent, selective and reversible non-peptide caspase-3 inhibitor with an IC50 value of 0.005 μM for enzymatic activity against caspase-3. M826 displays potent anti-apoptotic activity in animal models in vitro and in vivo. M826 can be used for nervous system diseases research .
|
-
- HY-161125
-
|
|
Others
|
Others
|
|
(+)-JQ1-OH is the major metabolite of (+)-JQ1(HY-13030). (+)-JQ-1 (JQ1) is a potent, specific, and reversible BET bromodomain inhibitor, with IC50s of 77 and 33 nM for the first and second bromodomain (BRD4(1/2)). (+)-JQ-1 also activates autophagy .
|
-
- HY-10235
-
|
VX-950
|
HCV Protease
HCV
SARS-CoV
|
Infection
|
|
Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide . Telaprevir inhibits SARS-CoV-2 3CL pro activity .
|
-
- HY-12248
-
|
CB-839
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat inuduces autophagy and has antitumor activity .
|
-
- HY-106934
-
|
BCX 34
|
Nucleoside Antimetabolite/Analog
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Peldesine (BCX 34) is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
|
-
- HY-106934A
-
|
BCX 34 dihydrochloride
|
Nucleoside Antimetabolite/Analog
HIV
|
Infection
Inflammation/Immunology
Cancer
|
|
Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research .
|
-
- HY-12248A
-
|
CB-839 hydrochloride
|
Glutaminase
Autophagy
|
Cancer
|
|
Telaglenastat (CB-839) hydrochloride is a first-in-class, selective, reversible and orally active glutaminase 1 (GLS1) inhibitor. Telaglenastat hydrochloride selectively inhibits GLS1 splice variants KGA (kidney-type glutaminase) and GAC (glutaminase C) compared to GLS2. The IC50s are 23 nM and 28 nM for endogenous glutaminase in mouse kidney and brain, respectively. Telaglenastat hydrochloride inudces autophagy and has antitumor activity .
|
-
- HY-16373
-
|
LNK-754; OSI-754
|
Farnesyl Transferase
|
Cancer
|
|
CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL . CP-609754 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-103713A
-
|
SP-2577 mesylate
|
Histone Demethylase
|
Cancer
|
|
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma .
|
-
- HY-W040468
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
2-Phenyl-2-(1-piperidinyl)propane is a selective and reversible human CYP2B6 inhibitor with an IC50 of 5.1 μM and a Ki of 5.6. 2-Phenyl-2-(1-piperidinyl)propane inhibits CYP2D6 (IC50=74 μM), CYP3A (IC50=200 μM) .
|
-
- HY-144396
-
|
|
SHP2
Phosphatase
Akt
Apoptosis
|
Cancer
|
|
SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells .
|
-
- HY-116866
-
|
|
Lipoxygenase
Fungal
|
Infection
Inflammation/Immunology
|
|
Sclerotiorin is a reversible and uncompetitive inhibitor against soybean lipoxygenase-1 (LOX-1) (IC50: 4.2 μM). Sclerotiorin also shows antioxidant activity by scavenging free radical (ED50: 0.12 μM), and nonenzymatic lipid peroxidation inhibition activity. Sclerotiorin has antifungal activity, and also inhibits platelet aggregation. Sclerotiorin can be purified from the fermented broth of Penicillium frequentans .
|
-
- HY-B0856R
-
|
|
Fungal
Tyrosinase
Antibiotic
|
Infection
|
|
Validamycin A (Standard) is the analytical standard of Validamycin A. This product is intended for research and analytical applications. Validamycin A, a fungicidal, is an agricultural antibiotic. Validamycin A is originally isolated from Streptomyces hygroscopicus var. limoneus. Validamycin A inhibits the growth of A. flavus, with a MIC of 1 μg/mL . Validamycin A shows potent inhibitory activity against trehalase of Rhizoctonia solani, with an IC50 of 72 μM . Validamycin A is a reversible tyrosinase inhibitor, with a Ki of 5.893 mM .
|
-
- HY-120039
-
|
|
Elastase
|
Inflammation/Immunology
|
|
(R)-MDL-101146 is the R-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis .
|
-
- HY-120039A
-
|
|
Elastase
|
Inflammation/Immunology
|
|
(S)-MDL-101146 is the S-isomer of MDL-101146. MDL-101146 is an orally active, competitive and reversible inhibitor against human neutrophil elastase (HNE) with a Ki value of 25 nM. MDL-101146 inhibits HNE-induced hemorrhage in hamsters. MDL-101146 is promising for research of emphysema, rheumatoid arthritis, chronic bronchitis, cystic fibrosis, adult respiratory distress syndrome and glomerulonephritis .
|
-
- HY-100671
-
|
|
Histone Acetyltransferase
STAT
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
L002 is a potent, cell permeable, reversible and specific acetyltransferase p300 (KAT3B) inhibitor with an?IC50?of 1.98 μM . L002 binds the acetyl-CoA pocket and competitively inhibits the FATp300 catalytic domain, blocks histone acetylation and p53 acetylation, and inhibits STAT3 activation . L002 has the potential for hypertension‐induced cardiac hypertrophy and fibrogenesis treatment .
|
-
- HY-14292
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
NVP-DPP728 is a potent, reversible and nitrile-dependent dipeptidyl peptidase IV (DPP-IV) inhibitor. NVP-DPP728 can inhibit human DPP-IV amidolytic activity with a Ki of 11 nM. NVP-DPP728 inhibits degradation of glucagon-like peptide-1 (GLP-1) and thereby potentiates insulin release in response to glucose intake. NVP-DPP728 can be used for researching diabetes .
|
-
- HY-100707
-
|
|
DNA-PK
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
IC 86621 is a potent DNA-dependent protein kinase (DNA-PK) inhibitor, with an IC50 of 120 nM. IC 86621 also acts as a selective and reversible ATP-competitive inhibitor.IC 86621 inhibits DNA-PK mediated cellular DNA double-strand break (DSB) repair (EC50=68 µM). IC 86621 increases DSB-induced antitumor activity without cytotoxic effects. IC 86621 can protects rheumatoid arthritis (RA) T cells from apoptosis .
|
-
- HY-14721R
-
|
|
c-Met/HGFR
Autophagy
|
Cancer
|
|
Tepotinib (Standard) is the analytical standard of Tepotinib. This product is intended for research and analytical applications. Tepotinib (EMD-1214063) is an orally active and highly selective, reversible, ATP-competitive c-Met inhibitor with an IC50 of 3 nM, >200-fold selective for c-Met than IRAK4, TrkA, Axl, IRAK1, and Mer. Tepotinib inhibits c-Met phosphorylation. Tepotinib has antitumor effects .
|
-
- HY-14930A
-
-
- HY-18620
-
DZ2002
1 Publications Verification
|
Others
|
Inflammation/Immunology
|
|
DZ2002 is an orally active, reversible and low-cytotoxic type III SAHH inhibitor (Ki=17.9 nM), with good immunosuppressive activity. DZ2002 prevents the development of experimental dermal fibrosis by reversing the profibrotic phenotype of various cell types. DZ2002 can be used in studies of autoimmune diseases such as lupus syndrome and systemic sclerosis .
|
-
- HY-18962
-
AMI-1
5 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
AMI-1 is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
|
-
- HY-19801
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Neurological Disease
|
|
CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects .
|
-
- HY-114237
-
|
|
Sodium Channel
|
Neurological Disease
|
|
GDC-0276 is a potent, selective, reversible and orally active NaV1.7 inhibitor with an IC50 value of 0.4 nM. GDC-0276 is well tolerated and exhibits a good pharmacokinetic profile. GDC-0276 has the potential for the treatment of pain and to address shortcomings of existing pain medications, such as addiction and off-target side effects .
|
-
- HY-14930
-
-
- HY-14892
-
|
LC15-0444
|
Dipeptidyl Peptidase
|
Metabolic Disease
Cancer
|
|
Gemigliptin (LC15-0444 ) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin exhibits potent anti-glycation properties. Gemigliptin can be used for the research of advanced glycation end products (AGE)-related diabetic complications .
|
-
- HY-139664A
-
|
|
DNA Methyltransferase
|
Cancer
|
|
(R)-GSK-3685032 is the R-enantiomer of GSK-3685032. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-18690S
-
|
AG-221-d6
|
Isotope-Labeled Compounds
|
Others
|
|
Enasidenib-d6 (AG-221-d6)is the deuterium labeledEnasidenib(HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
|
-
- HY-100642R
-
|
|
COMT
|
Neurological Disease
|
|
3-O-Methyltolcapone (Standard) is the analytical standard of 3-O-Methyltolcapone. This product is intended for research and analytical applications. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease .
|
-
- HY-129923
-
|
|
Others
|
Neurological Disease
|
|
(R)-Omeprazole sodium is a gastric acid resistant compound with activity to inhibit gastric acid secretion. (R)-Omeprazole sodium is metabolized in vivo, and its metabolism is primarily affected by cytochrome P450 enzymes. The interaction between (R)-Omeprazole sodium and mannitol may affect its bioavailability in formulations. (R)-Omeprazole sodium exhibits reversible direct and metabolism-dependent inhibition of CYP2C19 .
|
-
- HY-19261
-
|
|
Others
|
Metabolic Disease
|
|
T-0632 is a CCK A receptor antagonist that exhibits significant pharmacological properties in in vitro studies. T-0632 competitively inhibits the binding of [125I]CCK-8 to rat pancreatic CCK A receptors with a K_i value of 0.24 nM, which is significantly lower than the K_i value for guinea pig CCK B receptors. T-0632 has higher selectivity in inhibiting CCK-8-stimulated pancreatic enzyme release, with an IC_50 value of 5.0 nM, which is more advantageous than L-364,718 and loxiglumide. In rabbit gallbladder smooth muscle, the antagonistic effects of T-0632 and loxiglumide are reversible, while L-364,718 shows a persistent inhibitory effect. These results indicate that T-0632 is a highly potent, reversible and more selective CCK A receptor antagonist.
|
-
- HY-10580
-
|
6-Bromoindirubin-3'-oxime; BIO; MLS 2052
|
GSK-3
CDK
Apoptosis
|
Cancer
|
|
GSK 3 Inhibitor IX (6-Bromoindirubin-3'-oxime; BIO) is a potent, selective, reversible and ATP-competitive inhibitor of GSK-3α/β and CDK1-cyclinB complex with IC50s of 5 nM/320 nM/80 nM for (GSK-3α/β)/CDK1/CDK5, respectively.
|
-
- HY-14201
-
|
Ro 19-6327
|
Monoamine Oxidase
|
Neurological Disease
|
|
Lazabemide (Ro 19-6327) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide ?inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and?alzheimer′s disease .
|
-
- HY-123872
-
|
|
p97
|
Cancer
|
|
MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
|
-
- HY-14202
-
|
Ro 19-6327 hydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
|
Lazabemide hydrochloride (Ro 19-6327 hydrochloride) is a selective, reversible inhibitor of monoamine oxidase B (MAO-B) (IC50=0.03 μM) but less active for MAO-A (IC50>100 μM). Lazabemide inhibits monoamine uptake at high concentrations, the IC50 values are 86 μM, 123 μM and >500 μM for noradrenalin, serotonin and dopamine uptake, respectively. Lazabemide can be used for the research of parkinson and alzheimer′s disease .
|
-
- HY-141513
-
NH-3
3 Publications Verification
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
NH-3 is an orally active, reversible thyroid hormone receptor (THR) antagonist with an IC50 of 55 nM. NH-3, a derivative of the selective thyromi-metic GC-1, inhibits binding of thyroid hormones to their receptor and that inhibits cofactor recruitment . NH-3 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-135457
-
|
|
Phosphatase
|
Cancer
|
|
JMS-053 is a potent, selective and reversible PTP4A inhibitor, with IC50s of 29.1 nM, 48.0 nM, 34.7 nM, 92.6 nM, and 207.6 nM for PTP4A1, PTP4A2, PTP4A3, CDC25B, and DUSP3, respectively. JMS-053 can inhibit cancer cell migration and spheroid growth in vitro, attenuate in vivo ovarian tumor growth .
|
-
- HY-155108
-
|
|
Arginase
|
Cancer
|
|
OATD-02 is an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and 2. OATD-02 is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 abolishes tumor immunosuppression induced by both arginases. OATD-02 can be used for melanoma study .
|
-
- HY-143330
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
|
-
- HY-13814
-
|
|
Deubiquitinase
Autophagy
Apoptosis
|
Cancer
|
|
PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis .
|
-
- HY-109124
-
|
VNRX-5133
|
Beta-lactamase
Bacterial
|
Infection
|
|
Taniborbactam (VNRX-5133) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam is against Gram-negative bacteria .
|
-
- HY-118700
-
|
Guanidinobiotin
|
NO Synthase
|
Neurological Disease
|
|
2-Iminobiotin (Guanidinobiotin) is a biotin (vitamin H or B7) analog. 2-Iminobiotin is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5μM for murine iNOS and rat n-cNOS, respectively . 2-Iminobiotin superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage .
|
-
- HY-117853
-
|
ABT-761; VIA-2291
|
Lipoxygenase
|
Cardiovascular Disease
|
|
Atreleuton (ABT-761) is a selective, reversible, and orally bioavailable 5-Lipoxygenase (5-LO) inhibitor. Atreleuton (ABT-761) exhibits potent and selective inhibition of leukotriene formation . Atreleuton is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-109124A
-
|
VNRX-5133 hydrochloride
|
Beta-lactamase
Bacterial
|
Infection
|
|
Taniborbactam hydrochloride (VNRX-5133 hydrochloride) is a reversible and selective boronic acid-containing pan-spectrum β-lactamase inhibitor with IC50s of 8-530 nM. Taniborbactam hydrochloride has IC50s of 30 nM, 32 nM, 42 nM, 20 nM for KPC-2, AmpC, OXA-48, and VIM-2. Taniborbactam hydrochloride is against Gram-negative bacteria .
|
-
- HY-18263A
-
|
SB-656933
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-18962A
-
|
|
Histone Methyltransferase
|
Cancer
|
|
AMI-1 free acid is a potent, cell-permeable and reversible inhibitor of protein arginine N-methyltransferases (PRMTs), with IC50s of 8.8 μM and 3.0 μM for human PRMT1 and yeast-Hmt1p, respectively. AMI-1 free acid exerts PRMTs inhibitory effects by blocking peptide-substrate binding .
|
-
- HY-18263C
-
|
SB-656933 tosylate
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin tosylate (SB-656933 tosylate) is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin tosylate inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin tosylate has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-N10096
-
|
|
Parasite
|
Infection
|
|
Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human .
|
-
- HY-146312
-
|
|
Cholinesterase (ChE)
Monoamine Oxidase
|
Neurological Disease
|
|
AChE/BChE/MAO-B-IN-1 (Compound 10) is a reversible and non-time-dependent AChE, BChE and MAO-B inhibitor with IC50 values of 7.31, 0.56 and 26.1 μM for hAChE, hBChE and hMAO-B, respectively. AChE/BChE/MAO-B-IN-1 can cross the BBB and shows neuroprotective effects without cytotoxicity .
|
-
- HY-150249
-
|
|
DNA Methyltransferase
|
Cancer
|
|
GSK3735967 is an selective, reversible, non-nucleoside inhibitor of DNMT1 with an IC50 value of 40 nM. GSK3735967 contains a planar dicyanopyridine core that can specifically embed DNMT1 bound hemimethylated CpG dinucleotides. GSK3735967 has three binding sites, one of which can bind to histone H4K20me3 .
|
-
- HY-50667S1
-
|
BMS-562247-01-d3
|
Isotope-Labeled Compounds
|
Others
|
|
Apixaban-d3 (BMS-562247-01-d3)is the deuterium labeledApixaban(HY-50667) . Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases .
|
-
- HY-155181
-
|
|
Others
|
Cancer
|
|
hCES2-IN-1 (Compound 24) is a reversible and selective hCES2 inhibitor (IC50: 6.72 μM). hCES2-IN-1 reduces the level of hCES2 in living cells. hCES2-IN-1 is effective against Irinotecan (HY-16562)-induced delayed diarrhea and DSS-induced ulcerative colitis .
|
-
- HY-18263
-
|
SB-656933 hydrochloride
|
CXCR
Interleukin Related
|
Inflammation/Immunology
|
|
Elubrixin (SB-656933) hydrochloride is a potent, selective, competitive, reversible and orally active CXCR2 antagonist and an IL-8 receptor antagonist. Elubrixin hydrochloride inhibits neutrophil CD11b upregulation (IC50 of 260.7 nM) and shape change (IC50 of 310.5 nM). Elubrixin hydrochloride has the potential for inflammatory diseases research, such as inflammatory bowel disease and airway inflammation .
|
-
- HY-13281
-
|
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 hydrochloride is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 hydrochloride inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 hydrochloride induces apoptosis .
|
-
- HY-113952
-
|
(-)-Actinonin
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
Infection
Cancer
|
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities .
|
-
- HY-101925
-
CM-272
3 Publications Verification
|
Histone Methyltransferase
DNA Methyltransferase
Apoptosis
|
Cancer
|
|
CM-272 is a first-in-class, potent, selective, substrate-competitive and reversible dual G9a/DNA methyltransferases (DNMTs) inhibitor with antitumor activities. CM-272 inhibits G9a, DNMT1, DNMT3A, DNMT3B and GLP with IC50s of 8 nM, 382 nM, 85 nM, 1200 nM and 2 nM, respectively. CM-272 inhibits cell proliferation and promotes apoptosis, inducing IFN-stimulated genes and immunogenic cell death .
|
-
- HY-15425
-
|
Sphingosine Kinase 1 inhibitor II
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 induces apoptosis, necrosis, and autophagy .
|
-
- HY-15425B
-
|
Sphingosine Kinase 1 inhibitor II hydrochloride
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 hydrochloride (Sphingosine Kinase 1 Inhibitor II hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 hydrochloride is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 hydrochloride induces apoptosis, necrosis, and autophagy .
|
-
- HY-107834
-
PIK-75
4 Publications Verification
|
DNA-PK
PI3K
Apoptosis
|
Cancer
|
|
PIK-75 is a reversible DNA-PK and p110α-selective inhibitor, which inhibits DNA-PK, p110α and p110γ with IC50s of 2, 5.8 and 76 nM, respectively. PIK-75 inhibits p110α >200-fold more potently than p110β (IC50=1.3 μM) . PIK-75 induces apoptosis .
|
-
- HY-148825
-
-
- HY-112291
-
|
|
p38 MAPK
Src
PKC
|
Inflammation/Immunology
|
|
SB 220025 is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 µM, respectively. SB 220025 inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
|
-
- HY-155848
-
|
|
Phosphatase
|
Cancer
|
|
LYP-IN-4 (compound D14) is a reversible and selective inhibitor of lymphotyrosine phosphatase (LYP) (Ki=1.34 μM, IC50=3.52μM). LYP-IN-4 inhibits LYP to regulate TCR signaling, up-regulates PD-1/PD-L1 expression, and enhance anti-tumor immunity. LYP-IN-4 activates T cells and inhibits M2 macrophage polarization, inhibits tumor growth in MC38 isogenic mouse models.
|
-
- HY-131667
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase)-mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy .
|
-
- HY-112291A
-
|
|
p38 MAPK
Src
PKC
|
Inflammation/Immunology
|
|
SB 220025 trihydrochloride is a reversible, orally active, cell-permeable, ATP-competitive and selective human p38 MAPK inhibitor (IC50 = 60 nM). SB 220025 trihydrochloride also inhibits p56 Lck and PKC with IC50 values of 3.5 and 2.89 μM, respectively. SB 220025 trihydrochloride inhibits the expression of IL-8 gene in response to globular adiponectin (gAd), reduces inflammatory cytokine production and inhibits angiogenesis. SB 220025 trihydrochloride effectively prevents the progression of arthritis in a chronic inflammatory disease model and can be used in the study of inflammation .
|
-
- HY-10235S
-
|
VX-950-d4
|
Isotope-Labeled Compounds
HCV Protease
HCV
SARS-CoV
|
Infection
|
|
Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
|
-
- HY-144680
-
|
ZL-2313
|
EGFR
|
Cancer
|
|
BLU-945 is a potent, highly selective, reversible and orally active epidermal growth factor receptor (EGFR) tyrosine kinase inhibitor (TKIs). BLU-945 can effectively inhibit EGFR with L858R and/or exon 19 deletion mutation, T790M mutation and C797S mutation. BLU-945 can be used for the research of lung cancer including non-small cell lung cancer (NSCLC) .
|
-
- HY-152671
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
|
-
- HY-155107
-
|
|
Mitochondrial Metabolism
Bacterial
|
Infection
|
|
ND-011992 is a reversible, selective quinazoline-type inhibitor targeting quinone reductases and quinol oxidases. ND-011992 inhibits respiratory complex I and bo3 oxidase in addition to bd-I and bd-II oxidases in E. coli strain BL21*Δcyo with the IC50 of 0.12, 2.47, 0.63 and 1.3 μM, respectively. ND-011992 can be used for tuberculosis study .
|
-
- HY-120139A
-
|
|
Others
|
Cancer
|
|
(R)-KMH-233 is the isomer of KMH-233 (HY-120139), and can be used as an experimental control. KMH-233, a potent, reversible and selective l-type amino acid transporter 1 (LAT1) inhibitor, inhibits the uptake of LAT1 substrate, l-leucin (IC50=18 μM) as well as cell growth. KMH-233 significantly potentiates the efficacy of Bestatin and Cisplatin even at low concentrations (25 μM) .
|
-
- HY-N0063R
-
|
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-10200
-
|
|
IGF-1R
Insulin Receptor
|
Endocrinology
Cancer
|
|
BMS-754807 is a potent and reversible IGF-1R/IR inhibitor (IC50=1.8 and 1.7 nM, respectively; Ki=<2 nM for both). BMS-754807 also shows potent activities against Met, RON, TrkA, TrkB, AurA, and AurB with IC50 values of 6, 44, 7, 4, 9, and 25 nM, respectively .
|
-
- HY-13290
-
|
|
CaMK
P2X Receptor
|
Metabolic Disease
Cancer
|
|
KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
|
-
- HY-17369
-
|
L700462 hydrochloride monohydrate; MK383 hydrochloride monohydrate
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-17387
-
|
Huperzine A
|
Cholinesterase (ChE)
Apoptosis
iGluR
|
Neurological Disease
|
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
|
-
- HY-17369B
-
|
L700462; MK383
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-100414
-
|
BYK61359
|
Proton Pump
|
Metabolic Disease
|
|
Soraprazan (BYK61359) is a selective, reversible K-competitive inhibitor of the H,K-ATPase (Ki=6.4 nM), with an IC50 of 0.19 μM in gastric glands. Soraprazan binds to the H,K-ATPase with a Kd of 28.27 nM. Soraprazan shows immediate inhibition of acid secretion and is more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases .
|
-
- HY-B0563B
-
|
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ropivacaine hydrochloride is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain management in vivo .
|
-
- HY-16718
-
|
PF-00251802
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
|
Dagrocorat (PF-00251802) is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat can be used for the research of rheumatoid arthritis .
|
-
- HY-D0004
-
|
Azure B chloride
|
Monoamine Oxidase
|
Neurological Disease
|
|
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
|
-
- HY-B0563
-
|
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .
|
-
- HY-14892A
-
|
LC15-0444 tartrate
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
Gemigliptin tartrate (LC15-0444 tartrate) is a highly selective, reversible and competitive dipeptidyl peptidase-4 (DPP-4) inhibitor, with an IC50 of 10.3 nM for human recombinant DPP-4. Gemigliptin tartrate exhibits potent anti-glycation properties. Gemigliptin tartrate can be used for the research of advanced glycation end products (AGE)-related diabetic complications .
|
-
- HY-129388A
-
|
CC-90011; LSD1-IN-7
|
Histone Demethylase
|
Cancer
|
|
Pulrodemstat (CC-90011) is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. Pulrodemstat is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. Pulrodemstat induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-16718A
-
|
PF-00251802 hydrochloride
|
Glucocorticoid Receptor
Cytochrome P450
|
Inflammation/Immunology
Endocrinology
|
|
Dagrocorat (PF-00251802) hydrochloride is an orally active and selective high-affinity partial agonist of the glucocorticoid receptor. Dagrocorat hydrochloride is also a time-dependent reversible inhibitor of CYP3A (IC50=1.3 μM in human liver microsomes) and CYP2D6 (Ki=0.57 μM in human liver microsomes). Dagrocorat hydrochloride can be used for the research of rheumatoid arthritis .
|
-
- HY-17369A
-
|
L700462 hydrochloride; MK383 hydrochloride
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (L700462) hydrochloride is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-14205
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
NW-1772 (methanesulfonate) (compound 22b) is a potent and selective monoamine oxidase (MAO) B inhibitor. NW-1772 has some advantages, such as rapid blood-brain barrier penetration, short-acting and reversible inhibitory activity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. NW-1772 can be used for the research of neurodegenerative diseases .
|
-
- HY-N1919R
-
|
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
|
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-W013636R
-
|
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid (Standard) is the analytical standard of 2-Ketoglutaric acid. This product is intended for research and analytical applications. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-116765
-
|
|
Others
|
Neurological Disease
|
|
MAO-B-IN-35 is a potent, selective, reversible monoamine oxidase B (MAO-B) inhibitor with high inhibitory activity. MAO-B-IN-35 can exhibit high selectivity and potency at a small molecule scale. MAO-B-IN-35 is designed and synthesized so that it can be efficiently obtained during standard synthesis procedures and has superior physical and chemical properties .
|
-
- HY-169228
-
|
|
Btk
|
Cancer
|
|
WS-11 is a non-covalent reversible BTK inhibitor with IC50s of 3.9 nM and 2.2 nM for wild type, C481S mutation BTK, respectively. WS-11 can form strong π-π interaction with PHE540 and form p-π interaction with LYS430 within the active pocket, besides the strong hydrogen bonds .
|
-
- HY-136813
-
|
|
Beta-secretase
Amyloid-β
Cholinesterase (ChE)
|
Neurological Disease
|
Multitarget AD inhibitor-1 is a selective and reversible butyrylcholinesterase (BuChE) inhibitor with IC50s of 7.22 μM and 1.55 μM for hBuChE and eqBuChE (BuChE from equine serum), respectively. Multitarget AD inhibitor-1 inhibits β-secretase (IC50hBACE-1=41.60 μM), amyloid β aggregation (IC50Aβ=3.09 μM), tau aggregation. Multitarget AD inhibitor-1, a diphenylpropylamine derivative, has the potential for multifunctional disease-modifying anti-Alzheimer’s research .
|
-
- HY-145015
-
|
HM43239
|
FLT3
Apoptosis
|
Cancer
|
|
Tuspetinib (HM43239) is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-145015A
-
|
HM43239 hydrate
|
FLT3
Apoptosis
|
Cancer
|
|
Tuspetinib (HM43239) hydrate is an orally active and selective FLT3 inhibitor with IC50s of 1.1 nM, 1.8 nM and 1.0 nM for FLT3 WT, FLT3 internal tandem duplication (ITD) and FLT3 D835Y kinases, respectively. Tuspetinib hydrate inhibits the kinase activity of FLT3 as a reversible type I inhibitor and modulates p-STAT5, p-ERK, SYK, JAK1/2, and TAK1. Tuspetinib hydrate inhibits the proliferation and induces the apoptosis of leukemic cells .
|
-
- HY-135081
-
|
N-4AIA
|
Others
|
Others
|
|
N-(4-acetamidophenyl)-indomethacin amide (N-4-AIA) is one of several aromatic amides of indomethacin reported to be potent and selective reversible inhibitors of COX-2.1 N-4-AIA inhibits human recombinant and ovine COX-2 with IC50 values of 0.12 and 0.625 μM, respectively. It is about 400 times less potent as an inhibitor of human recombinant COX-1 and 80 times less potent as an inhibitor of ovine COX-1 than ovine COX-2.
|
-
- HY-15425A
-
|
Sphingosine Kinase 1 inhibitor II Citrate
|
SphK
LPL Receptor
Apoptosis
Autophagy
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM. PF-543 Citrate is >100-fold selectivity for SPHK1 over SPHK2. PF-543 Citrate is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM. PF-543 Citrate induces apoptosis, necrosis, and autophagy .
|
-
- HY-A0009
-
|
Galantamine hydrobromide
|
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-B0563A
-
|
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ropivacaine hydrochloride monohydrate is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain?management in vivo .
|
-
- HY-16903
-
|
|
PKC
|
Inflammation/Immunology
|
|
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
|
-
- HY-100867A
-
|
TAK-659 monohydrochloride; CB-659 monohydrochloride
|
Syk
FLT3
|
Cancer
|
|
TAK-659 hydrochloride is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 hydrochloride induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-100867
-
|
TAK-659; CB-659
|
Syk
FLT3
|
Cancer
|
|
TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL) .
|
-
- HY-129388B
-
|
CC-90011 benzenesulfonate; LSD1-IN-7 benzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
CC-90011 benzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 benzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 benzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-118700A
-
|
Guanidinobiotin hydrobromide
|
NO Synthase
|
Neurological Disease
|
|
2-Iminobiotin hydrobromide (Guanidinobiotin hydrobromide) is a biotin (vitamin H or B7) analog. 2-Iminobiotin hydrobromide is a reversible nitric oxide synthases inhibitor with Kis of 21.8 and 37.5 μM for murine iNOS and rat n-cNOS, respectively . 2-Iminobiotin hydrobromide superimposes on hypothermia protects human neuronal cells from hypoxia-induced cell damage .
|
-
- HY-123319A
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Antofloxacin is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
|
-
- HY-123319
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Antofloxacin hydrochloride is a well tolerate, orally active and broad-spectrum 8-amino-fluoroquinolone with potent antibacterial activities. Antofloxacin hydrochloride shows superior antibacterial activity against gyrA mutation-positive H. pylori strains, especially in Asn87- mutated strains, compared to levofloxacin. Antofloxacin hydrochloride is a weak, reversible inhibitor of CYP1A2 for the research of infections caused by a diverse group of bacterial species .
|
-
- HY-144677
-
|
|
EGFR
Apoptosis
|
Cancer
|
|
pan-HER-IN-2 (Compound C6) is a reversible, orally active pan-HER inhibitor with IC50 values of 0.72, 2.0, 8.2 and 75.1 nM against EGFR, HER4, EGFR T790M/L858R and HER2, respectively. pan-HER-IN-2 induces apoptosis and shows antitumor activities .
|
-
- HY-150702
-
|
|
MAGL
|
Neurological Disease
Inflammation/Immunology
|
|
MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease .
|
-
- HY-W013636S
-
|
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid- 13C5 is the 13C labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
|
-
- HY-W013636S1
-
|
Alpha-Ketoglutaric acid-d4
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid-d4 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
|
-
- HY-W013636S2
-
|
|
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid-d6 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
|
-
- HY-139664B
-
|
|
Others
|
Cancer
|
|
(S)-GSK-3685032 is the isomer of GSK-3685032 (HY-139664), and can be used as an experimental control. GSK-3685032 is a non-time-dependent, noncovalently, first-in-class reversible DNMT1-selective inhibitor, with an IC50 of 0.036 μM. GSK-3685032 induces robust loss of DNA methylation, transcriptional activation, and cancer cell growth inhibition .
|
-
- HY-B0986R
-
|
|
Parasite
Bacterial
Apoptosis
Glucosidase
Endogenous Metabolite
|
Infection
Metabolic Disease
Cancer
|
|
Hexylresorcinol (Standard) is the analytical standard of Hexylresorcinol. This product is intended for research and analytical applications. Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage .
|
-
- HY-W013636S4
-
|
Alpha-Ketoglutaric acid-13C2
|
Isotope-Labeled Compounds
Tyrosinase
Endogenous Metabolite
|
Others
|
|
2-Ketoglutaric acid-13C2 is a deuterated labeled 2-Ketoglutaric acid . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-B1266R
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
Physostigmine (salicylate) (Standard) is the analytical standard of Physostigmine (salicylate). This product is intended for research and analytical applications. Physostigmine salicylate (Eserine salicylate) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine salicylate crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine salicylate can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine salicylate is also an antidote for anticholinergic poisoning .
|
-
- HY-B0607R
-
|
NTBC (Standard); Nitisone (Standard); SC56735 (Standard)
|
HPPD
|
Metabolic Disease
|
|
Nitisinone (Standard) is the analytical standard of Nitisinone. This product is intended for research and analytical applications. Nitisinone is an orally active, competitive and reversible 4-hydroxyphenylpyruvate dioxygenase (4-HPPD) inhibitor with an IC50 of 173 nM. Nitisinone promotes tyrosine accumulation in a dose-dependent manner. nitisinone can be used in studies of hereditary tyrosinemia type 1 (HT-1) (a rare genetic disorder) and albinism .
|
-
- HY-103371
-
|
|
Chloride Channel
Potassium Channel
|
Neurological Disease
|
|
DCPIB is a selective, reversible and potent inhibitor of volume-regulated anion channels (VRAC). DCPIB voltage-dependently activates potassium channels TREK1 and TRAAK, and inhibits TRESK, TASK1 and TASK3 (IC50s: 0.14, 0.95, 50.72 μM, respectively). DCPIB is also a selective blocker of swelling-induced chloride current (ICl,swell), with an IC50 of 4.1 μM. DCPIB is a useful tool for investigating structure-function studies of K2P channels .
|
-
- HY-W008566
-
|
Norharman; β-Carboline
|
Monoamine Oxidase
Endogenous Metabolite
|
Infection
Neurological Disease
Cancer
|
|
Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC50 values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings .
|
-
- HY-17623
-
|
CJ-12420; RQ-00000004
|
Proton Pump
Potassium Channel
Na+/K+ ATPase
|
Inflammation/Immunology
|
Tegoprazan (CJ-12420), a potassium-competitive acid blocker, is a reversible, orally active and highly selective inhibitor of gastric H +/K +-ATPase. Tegoprazan inhibits gastric acid secretion and motility against porcine, canine and human H +/K +-ATPase with IC50 values ranging from 0.29-0.52 μM in vitro. Tegoprazan significantly improves colitis and enhances the intestinal epithelial barrier function in mice. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
|
-
- HY-115669
-
|
Antibiotic A 15104 Y; PClP
|
Myosin
TGF-β Receptor
|
Cancer
|
|
Pentachloropseudilin (Antibiotic A 15104 Y; PClP) is a reversible and allosteric potent inhibitor of Myo1s (class 1 myosins) with IC50s range from 1 to 5 μM for mammalian class-1 myosins and greater than 90 μM for class-2 and class-5 myosins. Pentachloropseudilin is a potent inhibitor of transforming growth factor-β (TGF-β)-stimulated signaling, with an IC50 of 0.1 to 0.2 μM for TGF-β .
|
-
- HY-120502
-
|
|
Lipoxygenase
Leukotriene Receptor
|
Inflammation/Immunology
|
|
5-LOX-IN-6 (compound 11a) is a direct and reversible inhibitor of 5-lipoxygenase (5-LO). 5-LOX-IN-6 inhibits 5-LO activity in human neutrophils and recombinant human 5-LO with IC50 values of 0.23 and 0.086 µM, respectively. 5-LOX-IN-6 prevents leukotriene biosynthesis. 5-LOX-IN-6 can be used for inflammatory and allergic disorders research .
|
-
- HY-W269511
-
|
|
Others
|
Neurological Disease
|
|
NW-1689 is a process-related impurity of safinamide mesilate (SAFM). SAFM is a drug used to treat Parkinson's disease (PD). It is a highly selective and reversible inhibitor of monoamine oxidase-B (MAO-B) and also blocks sodium channels and N-type calcium channels. These effects of SAFM help reduce the breakdown of dopamine and inhibit the release of glutamate. NW-1689 has a similar chemical structure to SAFM and has some similar pharmacological effects as SAFM, and can be used in Parkinson's disease research .
|
-
- HY-107794R
-
|
|
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Clodronate (disodium tetrahydrate) (Standard) is the analytical standard of Clodronate (disodium tetrahydrate). This product is intended for research and analytical applications. Clodronate disodium tetrahydrate (Disodium clodronate tetrahydrate) is first-generation bisphosphonate, with anti-osteoporotic, anti-inflammatory and analgesic effects. Clodronate disodium tetrahydrate is a selective, potent, reversible and Cl-competitive vesicular nucleotide transporter (VNUT) inhibitor, with an IC50 of 15.6 nM. Clodronate disodium tetrahydrate inhibits vesicular ATP release from neurons and reduces chronic neuropathic and inflammatory pain .
|
-
- HY-160843
-
|
|
Apoptosis
|
Cancer
|
|
N-ω-chloroacetyl-L-ornithine (NCAO) is a potent reversible competitive ornithine decarboxylase (ODC) inhibitor that exerts cytotoxic and antiproliferative effects on tumor cell lines with EC50 values ranging from 1 to 50.6 µM. NCAO induces tumor cell Apoptosis and inhibits tumor cell migration in vitro. NCAO also exhibits a potent antitumor activity against both solid and ascitic tumors in a mouse model using the myeloma (Ag8) cell line. NCAO is promising for research of antitumor agents .
|
-
- HY-10683
-
|
|
PI3K
mTOR
|
Cancer
|
|
PKI-402 is a selective, reversible, ATP-competitive inhibitor of PI3K, including PI3K-α mutants, and mTOR (IC50=2, 3, 7,14 and 16 nM for PI3Kα, mTOR, PI3Kβ, PI3Kδ and PI3Kγ).
|
-
- HY-107367
-
|
S-22611
|
EGFR
|
Cancer
|
|
Epertinib (S-22611) is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib shows potent antitumor activity . Epertinib is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-107367A
-
|
S-22611 hydrochloride
|
EGFR
|
Cancer
|
|
Epertinib (S-22611) hydrochloride is a potent, orally active, reversible, and selective tyrosine kinase inhibitor of EGFR, HER4 and HER2, with IC50s of 1.48 nM, 2.49 nM and 7.15 nM, respectively. Epertinib hydrochloride shows potent antitumor activity . Epertinib (hydrochloride) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-146165
-
|
|
Beta-lactamase
Bacterial
|
Infection
|
|
Metallo-β-lactamase-IN-8 (compound 17) is a potent, reversible and competitive broad-spectrum inhibitor of metallo-β-lactamases (MβLs), with IC50s of 1.3 μM, 5.7 μM, 9.8 μM, and 9.9 μM for L1, ImiS, IMP-1 and VIM-2, respectively. Metallo-β-lactamase-IN-8 exhibits antibacterial activity .
|
-
- HY-149581
-
|
|
Bacterial
|
Infection
|
|
DprE1-IN-9 (compound B18) is an effective reversible DprE1 inhibitor and can bind to the receptor cavity of DprE1. DprE1-IN-9 shows strong antimycobacterial activity not only against non-pathogenic strain H37Ra (MIC=0.18 µg/mL) but also against pathogenic H37Rv and the clinical MDR and XDR isolates .
|
-
- HY-157394
-
|
|
Cholinesterase (ChE)
|
Inflammation/Immunology
|
|
eeAChE/eqBuChE-IN-1 (compound 3F) is a reversible dual eeAChE/eqBuChE inhibitor with IC50s of 1.3?μM and 0.81?μM, respectively. eeAChE/eqBuChE-IN-1 exhibits anti-inflammatory activity. eeAChE/eqBuChE-IN-1 also shows neuroprotective effect on Aβ25-35-induced PC12 cell injury .
|
-
- HY-125365R
-
|
|
Bacterial
Reactive Oxygen Species
Antibiotic
|
Infection
|
|
Rifamycin S (Standard) is the analytical standard of Rifamycin S. This product is intended for research and analytical applications. Rifamycin S, a quinone, is an antibiotic against Gram-positive bacteria (including MRSA). Rifamycin S is the oxidized forms of a reversible oxidation-reduction system involving two electrons. Rifamycin S generates reactive oxygen species (ROS) and inhibits microsomal lipid peroxidation. Rifamycin S can be used for tuberculosis and leprosy .
|
-
- HY-B0879
-
|
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor .Suramin efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-129388
-
|
CC-90011 Methylbenzenesulfonate; LSD1-IN-7 Methylbenzenesulfonate
|
Histone Demethylase
|
Cancer
|
|
CC-90011 Methylbenzenesulfonate is a potent, selective, reversible and orally active inhibitor of lysine specific demethylase-1 (LSD1) with an IC50 of 0.25 nM. CC-90011 Methylbenzenesulfonate is less enzymatic inhibition against LSD2, MOA-A, and MAO-B. CC-90011 Methylbenzenesulfonate induces acute myeloid leukemia (AML) and small cell lung cancer (SCLC) cells differentiation and has potent anticancer activity .
|
-
- HY-125957
-
|
|
PKA
Casein Kinase
CaMK
PKC
|
Others
|
|
A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 μM), casein kinase II (Ki=5.1 μM) and myosin light chain kinase (MLCK) (Ki=7.4 μM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 μM and 80 μM, respectively .
|
-
- HY-B0563C
-
|
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Ropivacaine mesylate is a long-acting amide local anaesthetic agent for a spinal block and effectively blocks neuropathic pain. Ropivacaine blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibressup>[1] . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane .
|
-
- HY-130983
-
|
|
Btk
Ligands for Target Protein for PROTAC
|
Cancer
|
|
N-piperidine Ibrutinib hydrochloride (Compound 1) is a reversible Ibrutinib derivative. N-piperidine Ibrutinib hydrochloride is a potent BTK inhibitor with IC50s of 51.0 and 30.7 nM for WT BTK and C481S BTK, respectively . N-piperidine Ibrutinib hydrochloride can be used as a BTK ligand in the synthesis of a series of PROTACs, such as SJF620 (HY-133137). SJF620 is a potent PROTAC BTK degrader with a DC50 of 7.9 nM .
|
-
- HY-103352
-
|
L-235
|
Cathepsin
|
Metabolic Disease
|
|
L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss .
|
-
- HY-76474A
-
|
|
Apoptosis
Syk
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 hydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 hydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell. BAY 61-3606 hydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates. BAY 61-3606 hydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells.
|
-
- HY-112828
-
|
|
DAGL
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
LEI105 is a potent, highly selective and reversible dual diacylglycerol lipase (DAGL)-α/DAGL-β inhibitor. LEI105 reduces 2-arachidonoylglycerol levels in Neuro2A cells. LEI105 also reduces cannabinoid CB1-receptor-mediated short-term synaptic plasticity in a mouse hippocampal slice model. LEI105 is promising for research of diseases, such as obesity, related metabolic disorders and neuroinflammation .
|
-
- HY-10230
-
|
PKC412; CGP 41251
|
PKC
VEGFR
c-Kit
NO Synthase
Apoptosis
|
Cancer
|
|
Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
|
-
- HY-12755
-
|
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-108464A
-
|
|
Sodium Channel
TRP Channel
|
Metabolic Disease
Inflammation/Immunology
|
|
Phenamil methanesulfonate, an analog of Amiloride (HY-B0285), is a more potent and less reversible epithelial sodium channel (ENaC) blocker with an IC50 of 400 nM . Phenamil methanesulfonate is also a competive inhibitor of TRPP3 and inhibits TRPP3-mediated Ca 2+ transport with an IC50 of 140 nM in a Ca 2+ uptake assay . Phenamil methanesulfonate is an intriguing small molecule to promote bone repair by strongly activating BMP signaling pathway . Phenamil methanesulfonate is used for the research of cystic fibrosis lung disease .
|
-
- HY-103312
-
|
(-)-Xestospongin C
|
Calcium Channel
Apoptosis
|
Neurological Disease
|
|
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca 2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca 2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca 2+ signaling in neuronal and nonneuronal cells .
|
-
- HY-U00346A
-
|
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
TS-021 is a selective, orally active, reversible and long-acting DPP-IV inhibitor, and exhibits significant inhibition selectivity against DPP-8 (> 600 fold), DPP-9 (> 1200 fold) and other peptidases (> 15,000 fold). TS-021 inhibits DPP-IV activity in human plasma with an IC50 value of 5.34 nM. TS-021 has long-term persistent plasma drug concentration and potent antihyperglycemic activity, and increases in the active form of GLP-1 .
|
-
- HY-133233
-
|
1-Palmitylthio-2-palmitoylamido-1,2-dideoxy-sn-glycero-3-phosphorylcholine
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Thioetheramide-PC is a structurally modified phospholipid that functions as a competitive, reversible inhibitor of secretory phospholipase A2 (sPLA2). The IC50 value for thioetheramide-PC is 2 μM at a substrate concentration of 0.5 mM.1 In addition to binding to the catalytic site of sPLA2, thioetheramide-PC also binds to the activator site of this enzyme. The binding of thioetheramide-PC to the activator site is tighter than its binding to the catalytic site. The result of this dual interaction is that at low concentrations thioetheramide-PC may activate phospholipase activity rather than inhibiting it.
|
-
- HY-155108B
-
|
|
Arginase
|
Cancer
|
|
OATD-02 hydrochloride is the hydrochloride salt form of OATD-02 (HY-155108). OATD-02 hydrochloride an orally active, competitive, reversible, noncovalent dual inhibitor of Arginase1 and Arginase2. OATD-02 hydrochloride is a slow offset inhibitor, blocking intracellular arginases with IC50s of 20 nM (hARG1), 39 nM (hARG2), 39 nM (mARG1), and 28 nM (rARG1), respectively. OATD-02 hydrochloride bolishes tumor immunosuppression induced by both arginases. OATD-02 hydrochloride can be used for melanoma study .
|
-
- HY-B0879A
-
|
Suramin hexasodium salt
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
|
-
- HY-14280
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-14280A
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone sodium salt is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone sodium salt inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone sodium salt is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 μM). Entacapone sodium salt can be used for the research of Parkinson's disease . Entacapone sodium salt serves as as a inhibit of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-163445
-
|
|
NAMPT
|
Cancer
|
|
NAMPT activator-6 is a NAMPT activator, a regulatory molecule for the optical control system of NAMPT and NAD+. NAMPT activator-6 can be used to design efficient photoswitchable proteolysis-targeting chimeras (PS-PROTACs) to achieve up-down reversible regulation of NAMPT and NAD+ in a light-dependent manner and reduce the toxicity associated with inhibitor-based PS-PROTACs. PS-PROTAC can be used to achieve antitumor activity, NAMPT, and NAD+ modulation in vivo via optical manipulation .
|
-
- HY-76474
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM and an IC50 of 10 nM . BAY 61-3606 reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-14985
-
|
|
Syk
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
BAY 61-3606 dihydrochloride is an orally available, ATP-competitive, reversible and highly selective Syk inhibitor with a Ki of 7.5 nM an IC50 of 10 nM . BAY 61-3606 dihydrochloride reduces ERK1/2 and Akt phosphorylation in neuroblastoma cell . BAY 61-3606 dihydrochloride induces a large decrease of Syk phosphorylation in K-rn cell lysates . Bay 61-3606 dihydrochloride sensitizes TRAIL-induced apoptosis by downregulating Mcl-1 in breast cancer cells .
|
-
- HY-128717
-
|
EPZ019997
|
Histone Methyltransferase
|
Cancer
|
|
GSK3368715 (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
|
-
- HY-128717A
-
|
EPZ019997 dihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 dihydrochloride (EPZ019997 dihydrochloride) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
|
-
- HY-131014
-
|
|
JAK
|
Inflammation/Immunology
|
|
FM-479 is the negative control of FM-381 (HY-102046) and has no activity on JAK3 or other kinases . FM-381 is a potent covalent reversible inhibitor of JAK3 targeting the unique Cys909. FM-381 has an IC50 of 127 pM for JAK3, with 410, 2700 and 3600-fold selectivity over JAK1, JAK2 and TYK2, respectively.
|
-
- HY-117026
-
|
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
|
|
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
|
-
- HY-117825
-
|
|
Potassium Channel
|
Neurological Disease
|
|
RU-TRAAK-2 is a completely reversible TRAAK (TWIK-related arachidonic acid-stimulated K + channel) inhibitor. RU-TRAAK-2 exerts no activity for non-K2P channels (Kv1.2, Slo1 and GIRK2) . RU-TRAAK-2 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-44062
-
|
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
G9a-IN-1 (Compound 113) is a G9a protein inhibitor. G9A/EHMT2 is a nuclear histone lysine methyltransferase that catalyzes histone H3 lysine 9 dimethylation (H3K9me2), which is a reversible modification generally associated with transcriptional gene silencing. G9a-IN-1 can be used for the research of autoimmune disorders or cancer .
|
-
- HY-W107464
-
G6PDi-1
2 Publications Verification
|
PDI
|
Metabolic Disease
Inflammation/Immunology
|
|
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM for human G6PD. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells .
|
-
- HY-B0563S1
-
|
|
Isotope-Labeled Compounds
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
|
-
- HY-128717B
-
|
EPZ019997 trihydrochloride
|
Histone Methyltransferase
|
Cancer
|
|
GSK3368715 trihydrochloride (EPZ019997) is an orally active, reversible, and S-adenosyl-L-methionine (SAM) uncompetitive type I protein arginine methyltransferases (PRMTs) inhibitor (IC50=3.1 nM (PRMT1), 48 nM (PRMT3), 1148 nM (PRMT4), 5.7 nM (PRMT6), 1.7 nM (PRMT8)). GSK3368715 trihydrochloride (EPZ019997) produces a shift in arginine methylation states, alters exon usage, and has strong anti-cancer activity .
|
-
- HY-W013636S3
-
|
Alpha-Ketoglutaric acid-13C
|
Isotope-Labeled Compounds
|
Others
|
|
2-Ketoglutaric acid- 13C (Alpha-Ketoglutaric acid- 13C) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
|
-
- HY-156078
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .
|
-
- HY-161321
-
|
|
Phosphatase
Insulin Receptor
Akt
|
Metabolic Disease
|
|
PTP1B-IN-24 (Compound 9) is a reversible PTP1B inhibitor with an IC50 value of 1.4 μM, and PTP1B-IN-24 can enhance the thermal stability of PTP1B. PTP1B-IN-24 can restore PA- (HY-N0830) induced insulin resistance by increasing the phosphorylation levels of IRS1 and AKT .
|
-
- HY-17369BR
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (Standard) is the analytical standard of Tirofiban. This product is intended for research and analytical applications. Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-17369R
-
|
|
Integrin
|
Cardiovascular Disease
|
|
Tirofiban (hydrochloride monohydrate) (Standard) is the analytical standard of Tirofiban (hydrochloride monohydrate). This product is intended for research and analytical applications. Tirofiban (L700462) hydrochloride monohydrate is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban hydrochloride monohydrate induces proliferation and migration on endothelial cell by inducing production of VEGF. Tirofiban hydrochloride monohydrate can significantly reduces myocardial no-reflow and ischemia-reperfusion injury by alleviating myocardial microvascular structural and endothelial dysfunction in the ischemic area .
|
-
- HY-B2155R
-
|
|
Cholinesterase (ChE)
|
Metabolic Disease
Inflammation/Immunology
|
|
Acotiamide (monohydrochloride trihydrate) (Standard) is the analytical standard of Acotiamide (monohydrochloride trihydrate). This product is intended for research and analytical applications. Acotiamide monohydrochloride trihydrate is an orally active, selective and reversible acetylcholinesterase (AChE) inhibitor, with IC50 of 1.79 μM. Acotiamide monohydrochloride trihydrate can enhance gastric contractility and accelerate delayed gastric emptying. Acotiamide monohydrochloride trihydrate has the potential for the research of functional dyspepsia involving gastric motility dysfunction and intestinal inflammatory .
|
-
- HY-138143
-
|
Chromozym-TH
|
Fluorescent Dye
|
Others
|
|
N-(p-Tosyl)-GPR-pNA acetate (Chromozym-TH) is a chromogenic substrate targeting the synthetic peptides Hirunorm IV and Hirunorm V and can be used to detect the dissociation constants (KI) of both peptides. Hirunorm IV and Hirunorm V are reversible inhibitors of amidolytic thrombin activity. By varying the peptide concentration at a fixed concentration of the chromogenic substrate N-(p-Tosyl)-GPR-pNA acetate, the dissociation constants determined were 0.134 nM (Hirunorm IV) and 0.245 nM (Hirunorm V) .
|
-
- HY-B0563R
-
|
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ropivacaine (Standard) is the analytical standard of Ropivacaine. This product is intended for research and analytical applications. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is used for the research of neuropathic pain management .
|
-
- HY-18299
-
|
NG 95
|
CDK
Parasite
|
Infection
Cancer
|
|
Purvalanol B (NG 95) is a potent, selective, reversible and ATP-competitive inhibitor CDK, with IC50s of 6 nM, 6 nM, 9 nM, 6 nM for cdc2-cyclin B, CDK2-cyclin A, CDK2-cyclin E and CDK5-p35, respectively. Purvalanol B shows selectivity for CDK over a range of other protein kinases (IC50>1000 nM). Purvalanol B inhibits the growth a chloroquine-resistant strain of P. falciparum .
|
-
- HY-119944
-
JND3229
1 Publications Verification
|
EGFR
|
Cancer
|
|
JND3229 is a reversible EGFR C797S inhibitor with IC50 values of 5.8, 6.8 and 30.5 nM for EGFR L858R/T790M/C797S, EGFR WT and EGFR L858R/T790M, respectively. JND3229 has good anti-proliferative activity and can effectively inhibit tumour growth in vivo. JND3229 can be used in cancer research, especially in non-small cell carcinoma .
|
-
- HY-153128
-
|
|
DOCK
|
Inflammation/Immunology
|
|
DOCK2-IN-1 (compound 3), a CPYPP (HY-110100) analogue, is an inhibitor of DOCK2 as well (IC50=19.1 μM). DOCK2-IN-1 binds to DOCK2 DHR-2 domain in a reversible manner to inhibits its catalytic activity. DOCK2-IN-1 blocks the activation of both chemokine receptor- and antigen receptor-mediated Rac in lymphocytes. DOCK2-IN-1 significantly suppresses chemotactic response and T cell activation .
|
-
- HY-18200A
-
|
E5555 hydrochloride; ER-172594-00 hydrochloride
|
Protease Activated Receptor (PAR)
JAK
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Atopaxar hydrochloride (E5555 hydrochloride) is the hydrochloride salt form of Atopaxar (HY-18200). Atopaxar hydrochloride is an orally active, selective and reversible antagonist for thrombin receptor protease-activated receptor-1 (PAR-1). Atopaxar hydrochloride is the inhibitor for Janus kinase 1 (JAK1) and JAK2, which inhibits the JAK-STAT with EC50 of 5.90 μM in A549. Atopaxar hydrochloride inhibits the cell viability of A549 (IC50=7.02 μM), arrests the cell cycle at G1 phase and induces apoptosis. Atopaxar hydrochloride exhibits antiplatelet and antitumor activities. Atopaxar hydrochloride can be used for the research of atherothrombotic disease .
|
-
- HY-D0976
-
|
|
P2X Receptor
HIV
|
Infection
|
|
NF279 is a potent selective and reversible P2X1 receptor antagonist, with an IC50 of 19 nM. NF279 displays good selectivity over P2X2, P2X3 (IC50=1.62 μM), P2X4 (IC50>300 μM). NF279 is a dual HIV-1 coreceptor inhibitor that interferes with the functional engagement of CCR5 and CXCR4 by Env .
|
-
- HY-A0009S
-
|
Galantamine-d3 hydrobromide
|
Isotope-Labeled Compounds
Cholinesterase (ChE)
nAChR
|
Neurological Disease
|
|
Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
|
-
- HY-152005
-
|
|
SARS-CoV
|
Infection
|
|
SARS-CoV-2 3CLpro-IN-6 is a reversible covalent inhibitor of SARS-CoV-2 3CL protease. SARS-CoV-2 3CLpro-IN-6 has potent inhibitory activity for SARS-CoV-2 3CL pro with an IC50 value of 4.9 μM. SARS-CoV-2 3CLpro-IN-6 can be used for the research of coronavirus disease 2019 (COVID-19) .
|
-
- HY-128129
-
|
|
Urea Transporter
|
Metabolic Disease
|
|
UT-B-IN-1 (UTBINH-14) is a reversible, competitive and selective urea transporter-B (UT-B) inhibitor with IC50 values of 10 and 25 nM for human and mouse UT-B, respectively. UT-B-IN-1 shows low toxicity and high selectivity for UT-B over UT-A isoforms. UT-B-IN-1 increases urine output and reduces urine osmolality of mice. UT-B-IN-1 can be used for diuretic mechanism research .
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-
- HY-B0563BS
-
|
|
Isotope-Labeled Compounds
|
Neurological Disease
|
|
Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain?management in vivo .
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-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
nAChR
Cholinesterase (ChE)
|
Neurological Disease
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
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-
- HY-17387S1
-
|
Huperzine A-d4
|
iGluR
Cholinesterase (ChE)
Apoptosis
Isotope-Labeled Compounds
|
Neurological Disease
|
|
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
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-
- HY-B0563AR
-
|
|
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Ropivacaine (hydrochloride monohydrate) (Standard) is the analytical standard of Ropivacaine (hydrochloride monohydrate). This product is intended for research and analytical applications. Ropivacaine hydrochloride monohydrate is a potent sodium channel blocker and blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for regional anesthesia and neuropathic pain management in vivo .
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-
- HY-D0004R
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Azure B (Standard) is the analytical standard of Azure B. This product is intended for research and analytical applications. Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
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-
- HY-B0879AR
-
|
|
Phosphatase
Sirtuin
Reverse Transcriptase
Topoisomerase
SARS-CoV
Parasite
Apoptosis
|
Infection
Cardiovascular Disease
Cancer
|
|
Suramin (sodium salt) (Standard) is the analytical standard of Suramin (sodium salt). This product is intended for research and analytical applications. Suramin sodium salt (Suramin hexasodium salt) is a reversible and competitive protein-tyrosine phosphatases (PTPases) inhibitor . Suramin sodium salt is a potent inhibitor of sirtuins: SirT1 (IC50=297 nM), SirT2 (IC50=1.15 μM), and SirT5 (IC50=22 μM) . Suramin sodium salt is a competitive inhibitor of reverse transcriptase (DNA topoisomerase II: IC50=5 μM) . Suramin sodium salt is a potent SARS-CoV-2 RNA-dependent RNA polymerase (RdRp) inhibitor . Suramin sodium salt efficiently inhibits IP5K and is an antiparasitic, anti-neoplastic and anti-angiogenic agent .
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-
- HY-10230R
-
|
|
PKC
VEGFR
c-Kit
NO Synthase
Apoptosis
|
Cancer
|
|
Midostaurin (Standard) is the analytical standard of Midostaurin. This product is intended for research and analytical applications. Midostaurin (PKC412; CGP 41251) is an orally active, reversible multi-targeted protein kinase inhibitor. Midostaurin inhibits PKCα/β/γ, Syk, Flk-1, Akt, PKA, c-Kit, c-Fgr, c-Src, FLT3, PDFRβ and VEGFR1/2 with IC50s ranging from 22-500 nM . Midostaurin also upregulates endothelial nitric oxide synthase (eNOS) gene expression. Midostaurin shows powerful anticancer effects .
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-
- HY-110137A
-
|
DB75; NSC 305831
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Furamidine (DB75) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 µM, 283 µM, and >400 µM, respectively). Furamidine is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine is also an antiparasite agent .
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-
- HY-110137
-
|
DB75 dihydrochloride; NSC 305831 dihydrochloride
|
Histone Methyltransferase
Phosphodiesterase (PDE)
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Furamidine dihydrochloride (DB75 dihydrochloride) is a selective protein arginine methyltransferase 1 (PRMT1) inhibitor with an IC50 of 9.4 μM. Furamidine dihydrochloride is selective for PRMT1 over PRMT5, PRMT6, and PRMT4 (CARM1) (IC50s of 166 μM, 283 μM, and >400 μM, respectively). Furamidine dihydrochloride is a potent, reversible and competitive tyrosyl-DNA phosphodiesterase 1 (TDP-1) inhibitor. Inhibition of TDP-1 by Furamidine dihydrochloride is effective both with single- and double-stranded DNA substrates but is slightly stronger with the duplex DNA. Furamidine dihydrochloride is also an antiparasite agent .
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-
- HY-120826
-
|
|
Monoamine Oxidase
Adenosine Receptor
|
Neurological Disease
|
|
A2AAR/hMAO-B-IN-1 (compoudn 17) is a non-xanthine dual-target inhibitor targeting the A2A adenosine receptor (A2AAR) (IC50: 34.9 nM) andMAO-B (Ki: 39.5 nM, human). A2AAR/hMAO-B-IN-1 inhibits A2AAR-induced cAMP accumulation and exhibits competitive, reversible inhibition of MAO-B. A2AAR/hMAO-B-IN-1 can be used in the study of neurodegenerative diseases such as Parkinson's disease (PD) .
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-
- HY-W008566R
-
|
|
Monoamine Oxidase
Endogenous Metabolite
|
Infection
Neurological Disease
Cancer
|
|
Norharmane (Standard) is the analytical standard of Norharmane. This product is intended for research and analytical applications. Norharmane (Norharman), a β-carboline alkaloid, is a potent and reversible monoamine oxidase inhibitor, with IC50 values of 6.5 and 4.7 μM for MAO-A and MAO-B, respectively. Norharmane causes antidepressant responses. Norharmane is also a prospective anti-cancer photosensitizer. Norharmane alters polar auxin transport (PAT) by inhibiting PIN2, PIN3 and PIN7 transport proteins, thus causing a significant inhibitory effect on the growth of Arabidopsis thaliana seedlings .
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-
- HY-18957C
-
|
BGB-283 hydrochloride
|
Others
|
Cancer
|
|
Lifirafenib hydrochloride (BGB-283 hydrochloride) is a novel, reversible B-RAFV600E inhibitor with antitumor activity. Lifirafenib has shown potent antitumor activity against solid tumors with B-RAFV600E mutations, such as melanoma, thyroid cancer, and low-grade serous ovarian cancer. Lifirafenib exhibits selective cytotoxicity in vitro, preferentially inhibiting the proliferation of cancer cells with B-RAFV600E and EGFR mutations/amplification. Lifirafenib can achieve dose-dependent inhibition of tumor growth in animal models, accompanied by partial and complete tumor shrinkage .
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-
- HY-14280S
-
|
|
COMT
|
Neurological Disease
|
|
Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
|
-
- HY-123035
-
|
|
HSP
Akt
EGFR
|
Endocrinology
|
|
Gamendazole, an indazole carboxylic acid (ICA), is an orally active, selective HSP90AB1 (HSP90BETA) and EEF1A1 (eEF1A) inhibitor. Gamendazole binds to the C-terminal nucleotide binding pocket of HSP90 and cause downregulation of clients AKT1 and ERBB2, but stabilizes the HSP90 heterocomplex. Gamendazole specifically inhibits the actin bundling function of EEF1A1, but does not bind to the nucleotide docking pocket nor inhibits the ribosome charging or protein translation functions of EEF1A1. Gamendazole, an antispermatogenic compound with antifertility effects, has the potential for reversible non-hormonal male contraceptive agent research .
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-
- HY-70057
-
|
FCE 26743; EMD 1195686
|
Monoamine Oxidase
|
Neurological Disease
|
|
Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
|
-
- HY-17623S
-
|
CJ-12420-d6; RQ-00000004-d6
|
Proton Pump
Na+/K+ ATPase
|
Metabolic Disease
|
|
Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
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-
- HY-P5272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
|
-
- HY-10587
-
|
|
Histone Methyltransferase
Autophagy
|
Cancer
|
|
BIX-01294 is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 has antitumor activity in recurrent tumor cells .
|
-
- HY-108239
-
|
|
Histone Methyltransferase
Autophagy
|
Cancer
|
|
BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells .
|
-
- HY-158732
-
|
|
Monoamine Oxidase
|
Inflammation/Immunology
|
|
MAO-B-IN-33 (compound C3) is a potent, reversible and selective monoamine oxidase-B (MAO-B) inhibitor with an IC50 of 0.021 μM and 26.805 μM for MAO-B and MAO-A, respectively. The selectivity of MAO-B-IN-33 is attributed to the steric clash arising from the residue differences between Phe208 (MAO-A) and Ile199 (MAO-B). MAO-B-IN-33 inhibits cerebral MAO-B activity and alleviates MPTP (HY-15608)-induced dopaminergic neuronal loss in the mouse. MAO-B-IN-33 has the potential for Parkinson's disease research .
|
-
- HY-14280R
-
|
|
COMT
|
Neurological Disease
Cancer
|
|
Entacapone (Standard) is the analytical standard of Entacapone. This product is intended for research and analytical applications. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease . Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders .
|
-
- HY-W027553
-
|
NIK-247 free base
|
Cholinesterase (ChE)
Potassium Channel
Sodium Channel
|
Neurological Disease
Metabolic Disease
|
|
Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
|
-
- HY-B1033
-
|
|
5-HT Receptor
Dopamine Receptor
Sodium Channel
|
Neurological Disease
|
|
Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
|
-
- HY-111790
-
M3258
1 Publications Verification
|
Proteasome
Apoptosis
|
Cancer
|
|
M3258 is an orally bioavailable, potent, reversible and highly selective immunoproteasome subunit LMP7 (β5i) inhibitor. M3258 exerts high biochemical (IC50=3.6 nM) and cellular (IC50=3.4 nM) potency against the LMP7 subunit. M3258 shows strong antitumor efficacy in multiple myeloma xenograft models. M3258 leads to a significant and prolonged suppression of tumor LMP7 activity and ubiquitinated protein turnover and the induction of apoptosis in multiple myeloma cells .
|
-
- HY-N6789
-
KT5720
3 Publications Verification
|
PKA
|
Neurological Disease
Cancer
|
|
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
|
-
- HY-70057A
-
|
FCE 26743 mesylate; EMD 1195686 mesylate
|
Monoamine Oxidase
|
Cardiovascular Disease
Neurological Disease
|
|
Safinamide (FCE 26743; EMD 1195686) mesylate is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 nM) . Safinamide mesylate also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide mesylate has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke et.al .
|
-
- HY-146691
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-130612
-
|
|
Epigenetic Reader Domain
PROTACs
|
Cancer
|
|
PROTAC BRD2/BRD4 degrader-1 (compound 15) is a potent and selective BET protein BRD4 and BRD2 degrader, connected by ligands for Cereblon and BET. PROTAC BRD2/BRD4 degrader-1 rapidly induces reversible, long-lasting, and unexpectedly selective removal of BRD4 and BRD2 over BRD3. It effectively inhibits solid tumors with low cytotoxic effect. PROTAC BRD2/BRD4 degrader-1 is composed of the BET inhibitor, a linker, and the ligand thalidomide for cereblon (CRBN)/cullin 4A .
|
-
- HY-155010
-
|
|
Steroid Sulfatase
|
Metabolic Disease
|
|
Steroid sulfatase/17β-HSD1-IN-5 is a irreversible inhibitor of steroid sulfatase (STS) .Steroid sulfatase/17β-HSD1-IN-5 is a reversible and selective inhibitor of 7β-hydroxysteroid dehydrogenase type1 (17β-HSD1), with IC50s of 43 nM and 6.2μM for 17β-HSD1 and 17β-HSD2, respectively. Steroid sulfatase/17β-HSD1-IN-5 can be used for metabolic disease (especially for endometriosis) research .
|
-
- HY-B0653A
-
|
(S)-(-)-Bupivacaine monohydrochloride
|
Sodium Channel
Ferroptosis
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Levobupivacaine hydrochloride ((S)-(-)-Bupivacaine monohydrochloride) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine hydrochloride exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine hydrochloride can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine hydrochloride is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine hydrochloride can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
- HY-B0653
-
|
(S)-(-)-Bupivacaine
|
Sodium Channel
Ferroptosis
|
Neurological Disease
Cancer
|
|
Levobupivacaine ((S)-(-)-Bupivacaine) is a long-acting amide local agent that can suppress or relieve pain. Levobupivacaine exerts agent that can suppress or relieve pain. and analgesic effects through reversible blockade of neuronal sodium channel. Levobupivacaine can inhibit impulse transmission and conduction in cardiovascular and other tissues, possessing certain cardiac and CNS toxicity. Levobupivacaine is metabolized by hepatic cytochrome P450 (CYP450) enzymes in vivo. Levobupivacaine can also induce ferroptosis by miR-489-3p/SLC7A11 signaling in gastric cancer .
|
-
- HY-108548
-
|
Rp-8-Bromo-PET-cGMPS
|
Others
|
Inflammation/Immunology
|
|
Rp-8-bromo-PET-Cyclic GMPS (Rp-8-bromo-PET-cGMPS) is an analog of cyclic GMP (cGMP). It is a cell permeable, competitive, and reversible inhibitor of cGMP-dependent protein kinases (cGKs) that blocks activation of cGKI and cGKII by cGMP (Kis=35 and 30 nM). It less potently inhibits protein kinase A (Ki=11 μM) and cGMP-induced activation of cyclic nucleotide-gated channels (IC50=25 μM). In the absence of cGMP stimulation, Rp-8-bromo-PET-cGMPS can act as a partial agonist of cGKI (Ki=1 μM). Rp-8-bromo-PET-cGMPS is resistant to hydrolysis by phosphodiesterase 11.
|
-
- HY-70057S1
-
|
FCE 26743-d4-1; EMD 1195686-d4-1
|
Isotope-Labeled Compounds
Monoamine Oxidase
|
Neurological Disease
|
|
Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
|
-
- HY-70057R
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Safinamide (Standard) is the analytical standard of Safinamide. This product is intended for research and analytical applications. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM) . Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al .
|
-
- HY-116973
-
|
|
HIV
|
Infection
|
|
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
|
-
- HY-W205529
-
|
|
Others
|
Neurological Disease
|
|
RO 16-6491 Free base is a selective, reversible inhibitor of monoamine oxidase type B (MAO-B), exhibiting high affinity and specificity for binding sites in human frontal cortex mitochondria and platelet membranes. RO 16-6491 demonstrates a fast dissociation of bound radioactivity at 20 degrees C, indicating its dynamic binding properties. RO 16-6491 also acts as a substrate for MAO-B, suggesting that its oxidation may produce a stable intermediate responsible for its potent inhibitory effects. RO 16-6491 serves as an excellent radioligand probe for investigating the regional tissue distribution of MAO-B in various physiological and pathological states.
|
-
- HY-162633
-
|
|
Deubiquitinase
|
Cancer
|
|
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
|
-
- HY-B1167A
-
|
Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride
|
Others
|
Cardiovascular Disease
|
|
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
|
-
- HY-147100
-
|
|
PROTACs
Adrenergic Receptor
|
Cancer
|
|
α1A-AR Degrader 9c (compound 9c) is a potent, selective and reversible α1A-AR (Adrenergic receptor) PROTAC degrader, with a DC50 of 2.86 μM. α1A-AR Degrader 9c induces α1A-AR degradation can be attributed to proteasomal degradation. α1A-AR Degrader 9c inhibits the proliferation of PC-3 cells, with an IC50 of 6.12 μM. α1A-AR Degrader 9c shows antitumor activity, and can be used for prostate cancer research .
|
-
- HY-138232
-
|
LTNAM
|
Others
|
Neurological Disease
|
|
Lys-psi(CH2NH)-Trp(Nps)-OMe is a lysine-tryptophan (Nps) pseudodipeptide analog. It is obtained by replacing the peptide bond in the Lys-Trp(Nps) molecule with an aminomethylene bond and has analgesic activity. Lys-psi(CH2NH)-Trp(Nps)-OMe induces a dose-dependent and naloxone-reversible analgesia after intracerebroventricular administration in mice, and its analgesic effect lasts longer than that of the original compound. It protects methionine enkephalin from degradation in rat striatal slices and binds to low-dose opioid peptides to produce analgesia. Lys-psi(CH2NH)-Trp(Nps)-OMe effectively inhibits brain aminopeptidase activity both in vitro and in vivo. The enhanced resistance of this pseudodipeptide to proteolysis may explain its prolonged analgesic activity.
|
-
- HY-N2735
-
|
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA) inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitory activities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
|
-
- HY-162812
-
|
|
Apoptosis
Cholinesterase (ChE)
Tau Protein
Ferroptosis
Histamine Receptor
|
Neurological Disease
|
|
H3R antagonist 4 (compound 11L) was a dual inhibitor of cholinesterase and histamine receptor (H3R), with corresponding IC50 of 7.04 μM (eeAChE), 9.73 μM (hAChE)(reversible) and 1.09 nM (H3R) , respectively. H3R antagonist 4 inhibited the aggregation of Aβ1-42 induced by itself and Cu 2+ (95.48% and 88.63%) , and degraded the Aβ1-42 fibrils induced by itself and Cu 2+ (80.16% and 89.30%) . H3R antagonist 4 chelate biometals such as Cu 2+, Zn 2+, Al 3+, and Fe 2+. H3R antagonist 4 significantly reduced tau protein hyperphosphorylation induced by Aβ1-42 and inhibited RSL-3-induced apoptosis and ferroptosis in PC12 cells. H3R antagonist 4 had the best blood-brain barrier permeability and intestinal absorption in hCMEC/D3 and hPepT1-MDCK cells.H3R antagonist 4 ameliorates learning and memory impairment in a mouse model of Alzheimer's disease induced by scopolamine (HY-N0296) .
|
-
-
-
HY-L081
-
|
|
117 compounds
|
|
Protein phosphorylation is a key post-translational modification underlying the regulation of many cellular processes. Phosphatases and kinases contribute to the regulation of protein phosphorylation homeostasis in the cell. This reversible regulation of protein phosphorylation is critical for the proper control of a wide range of cellular activities, including cell cycle, proliferation and differentiation, metabolism, cell-cell interactions, etc.
Protein phosphatases have evolved in separate families that are structurally and mechanistically distinct. Based on substrate specificity and functional diversity, protein phosphatases are classified into two superfamilies: Protein serine/threonine phosphatases and Protein tyrosine phosphatases. Ser/Thr phosphatases are metalloenzymes belonging to two major gene families termed PPP (phosphoprotein phosphatase) and PPM (metal-dependent protein phosphatases), whereas protein tyrosine phosphatases (PTPs) belong to distinct classes of enzymes that utilize a phospho-cysteine enzyme intermediate as a part of their catalytic action.
MCE supplies a unique collection of 117 phosphatase inhibitors that mainly targeting protein tyrosine phosphatases (PTPs) and serine/threonine-specific protein phosphatases. MCE Phosphatase Inhibitor Library is a useful tool for phosphatase drug discovery and related research.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D0004
-
|
Azure B chloride
|
Dyes
|
|
Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
|
-
- HY-D0004R
-
|
|
Dyes
|
|
Azure B (Standard) is the analytical standard of Azure B. This product is intended for research and analytical applications. Azure B is a cationic dye and the major metabolite of Methylene blue. Azure B is used in making Azure eosin stains for blood smear staining. Azure B is a high-potency, selective and reversible inhibitor of monoamine oxidases (MAO)-A, with IC50s of 11 and 968 nM for recombinant human MAO-A and MAO-B, respectively. Azure B possesses significant antidepressant-like effects .
|
| Cat. No. |
Product Name |
Type |
-
- HY-126388
-
|
|
Enzyme Substrates
|
|
Trypsin Inhibitor, soybean is a potent and reversible inhibitor of trypsin .
|
-
- HY-W087937
-
|
Benzenecarboximidamide hydrochloride hydrate
|
Biochemical Assay Reagents
|
|
Benzamidine (Benzenecarboximidamide) hydrochloride hydrate is a reversible competitive trypsin-like serine proteases inhibitor with Kis of 20, 21, 97, 110, 320 and 750 μM against Tryptase, Trypsin, uPA, Factor Xa, Thrombin and tPA, respectively .
|
-
- HY-163624
-
|
|
Biochemical Assay Reagents
|
|
Bfl-1-IN-2 (Compound 13) is a reversible and covalent inhibitor of Bfl-1 (IC50: 4.3 μM). Bfl-1-IN-2 acts by binding to Cys55 of Bfl-1 .
|
-
- HY-W013636C
-
|
Alpha-Ketoglutaric acid potassium
|
Biochemical Assay Reagents
|
|
2-Ketoglutaric acid potassium (Alpha-Ketoglutaric acid potassium) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid potassium also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid potassium is a reversible inhibitor of tyrosinase with an IC50 value of 15 mM .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10149
-
|
|
Caspase
|
Cancer
|
|
Ac-IEPD-CHO is a reversible granzyme B inhibitor with a Ki of 80 nM . Ac-IEPD-CHO is also a caspase-8 inhibitor .
|
-
- HY-P1081
-
|
|
Proteasome
|
Inflammation/Immunology
|
|
Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for μ-calpain and cathepsin L, respectively .
|
-
- HY-P0322
-
|
EMD 56574
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK (EMD 56574) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK (EMD 56574) is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK is used to study the role of integrins in bone formation and resorption .
|
-
- HY-P5936
-
|
DEVD-CHO-CPP 32
|
Caspase
|
Cancer
|
|
Ac-AAVALLPAVLLALLAP-DEVD-CHO (DEVD-CHO-CPP 32) is a potent and reversible caspase-3 inhibitor .
|
-
- HY-P1403
-
|
|
Potassium Channel
|
Others
|
|
Tertiapin LQ is a specific and reversible renal outer medullary potassium ROMK1 (Kir1.1) channel inhibitor .
|
-
- HY-P1081A
-
|
|
Proteasome
|
Inflammation/Immunology
|
|
Acetyl-Calpastatin(184-210)(human) TFA is a potent, selective and reversible calpain inhibitor with Ki values of 0.2 nM and 6 μM for µ-calpain and cathepsin L, respectively .
|
-
- HY-P4989
-
|
|
Biochemical Assay Reagents
|
Infection
|
|
Type A Allatostatin III (allatostatin 3) is a blood-brain barrier permeable and reversible neuropeptide that inhibits hormone synthesis in juvenile female cockroaches. Type A Allatostatin III can be used in pesticide research .
|
-
- HY-P1193
-
|
|
Peptides
|
Neurological Disease
|
|
GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist . GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats .
|
-
- HY-113963
-
|
|
Apoptosis
|
Cancer
|
|
Ac- IETD- CHO is a potent, reversible inhibitor of granzyme B and caspase-8. Ac- IETD- CHO inhibits Fas-mediated apoptotic cell death, hemorrhage, and liver failure. Ac- IETD- CHO also inhibits cytotoxic T lymphocytes induced cell death .
|
-
- HY-P1346
-
|
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
APETx2, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain .
|
-
- HY-P1346A
-
|
|
Sodium Channel
|
Neurological Disease
Inflammation/Immunology
|
|
APETx2 TFA, a sea anemone peptide from Anthopleura elegantissima, is a selective and reversible ASIC3 inhibitor, with an IC50 of 63 nM. APETx2 directly inhibits the ASIC3 channel by acting at its external side. APETx2 could reverses acid‐induced and inflammatory pain .
|
-
- HY-P0322A
-
|
EMD 56574 TFA
|
Integrin
|
Cardiovascular Disease
Metabolic Disease
|
|
GRGDSPK TFA (EMD 56574 TFA) is a peptide incluing Arg-Gly-Asp (RGD). GRGDSPK TFA is an competitive and reversible inhibitory peptide for inhibiting integrin-fibronectin binding. GRGDSPK TFA is used to study the role of integrins in bone formation and resorption .
|
-
- HY-120019
-
|
L-709049
|
Interleukin Related
Apoptosis
Caspase
|
Inflammation/Immunology
|
|
Ac-YVAD-CHO (L-709049) is a potent, reversible, specific tetrapeptide interleukin-lβ converting enzyme (ICE) inhibitor with mouse and human Ki values of 3.0 and 0.76 nM. Ac-YVAD-CHO is also a caspase-1 inhibitor. Ac-YVAD-CHO can suppress the production of mature IL-lβ .
|
-
- HY-P10169
-
|
|
Proteasome
|
Others
|
|
Acetyl-Calpastatin(184-210)(human), Negative Control is a control scramble peptide of Acetyl-Calpastatin(184-210)(human) (HY-P1081). Acetyl-Calpastatin(184-210)(human) is a potent, selective and reversible calpain inhibitor .
|
-
- HY-P1259
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-P1259A
-
|
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-P5272
-
|
|
Bacterial
|
Inflammation/Immunology
|
|
Histatin-3 TFA, a 32 amino acid peptide, possesses powerful antimicrobial properties. Histatin-3 TFA behaves as a substrate for proprotein convertase 1 (PC1), being cleaved by this endoprotease primarily at a site carboxy terminal to the single Arg25 residue (HRGYR decrease SN). Histatin-3 TFA is a moderately potent, reversible and competitive inhibitor of the furin-mediated cleavage of the pentapeptide pGlu-Arg-Thr-Lys-Arg-MCA fluorogenic substrate, with an estimated inhibition constant Ki of 1.98 μM .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-N12763
-
-
- HY-N0063
-
-
- HY-16482
-
-
- HY-116866
-
|
|
Structural Classification
Natural Products
Microorganisms
Source classification
|
Lipoxygenase
Fungal
|
|
Sclerotiorin is a reversible and uncompetitive inhibitor against soybean lipoxygenase-1 (LOX-1) (IC50: 4.2 μM). Sclerotiorin also shows antioxidant activity by scavenging free radical (ED50: 0.12 μM), and nonenzymatic lipid peroxidation inhibition activity. Sclerotiorin has antifungal activity, and also inhibits platelet aggregation. Sclerotiorin can be purified from the fermented broth of Penicillium frequentans .
|
-
- HY-B0856R
-
-
- HY-N10096
-
-
- HY-113952
-
|
(-)-Actinonin
|
Infection
Structural Classification
Natural Products
Microorganisms
Classification of Application Fields
Source classification
Disease Research Fields
|
Aminopeptidase
Bacterial
MMP
Apoptosis
Antibiotic
|
|
Actinonin ((-)-Actinonin) is a naturally occurring antibacterial agent produced by Actinomyces. Actinonin inhibits aminopeptidase M, aminopeptidase N and leucine aminopeptidase. Actinonin is a potent reversible peptide deformylase (PDF) inhibitor with a Ki of 0.28 nM. Actinonin also inhibits MMP-1, MMP-3, MMP-8, MMP-9, and hmeprin α with Ki values of 300 nM, 1,700 nM, 190 nM, 330 nM, and 20 nM, respectively. Actinonin is an apoptosis inducer. Actinonin has antiproliferative and antitumor activities .
|
-
- HY-N0063R
-
|
|
Structural Classification
Punica granatum L.
Source classification
Phenols
Polyphenols
Punicaceae
Plants
|
SARS-CoV
HBV
|
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-17387
-
-
- HY-N1919R
-
-
- HY-W013636R
-
-
- HY-A0009
-
|
Galantamine hydrobromide
|
Structural Classification
Alkaloids
Other Alkaloids
Plants
Amaryllidaceae
|
Cholinesterase (ChE)
nAChR
|
|
Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-B0986R
-
-
- HY-W008566
-
-
- HY-125365R
-
-
- HY-103312
-
|
(-)-Xestospongin C
|
Alkaloids
Piperidine Alkaloids
Structural Classification
Animals
Source classification
|
Calcium Channel
Apoptosis
|
|
Xestospongin C ((-)-Xestospongin C) is a selective, reversible inositol 1,4,5-trisphosphate receptor (IP3R) inhibitor. Xestospongin C acts as an inhibitor of the sarcoplasmic/endoplasmic reticulum Ca 2+ ATPase (SERCA) pump of internal stores. Xestospongin C blocks IP3-induced Ca 2+ release from cerebellar microsomes with an IC50 of 358 nM. Xestospongin C is a valuable tool for investigating the structure and function of IP3Rs and Ca 2+ signaling in neuronal and nonneuronal cells .
|
-
- HY-A0009R
-
|
Galantamine hydrobromide (Standard)
|
Structural Classification
Alkaloids
Other Alkaloids
Source classification
Plants
Amaryllidaceae
|
nAChR
Cholinesterase (ChE)
|
|
Galanthamine (hydrobromide) (Standard) is the analytical standard of Galanthamine (hydrobromide). This product is intended for research and analytical applications. Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD) .
|
-
- HY-W008566R
-
-
- HY-B1167A
-
|
Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride
|
Rauvolfia verticillata (Lour.) Baill.
Apocynaceae
Structural Classification
Natural Products
Source classification
Plants
|
Others
|
|
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
|
-
- HY-N2735
-
|
|
Structural Classification
Leguminosae
Caesalpinia sappan L.
Source classification
Phenols
Polyphenols
Plants
|
Influenza Virus
|
|
7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA) inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitory activities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0207AS
-
|
|
|
Pyridostigmine-d6 (bromide) is the deuterium labeled Pyridostigmine, which is a parasympathomimetic and a reversible cholinesterase inhibitor.
|
-
-
- HY-50667S
-
|
|
|
Apixaban- 13C,d3 is a deuterium and 13C labeled Apixaban. Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively[1].
|
-
-
- HY-10163S1
-
|
|
|
Dabigatran-d3 is the deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
-
- HY-B0207AS1
-
|
|
|
Pyridostigmine-d3 (bromide) is the deuterium labeled Pyridostigmine bromide. Pyridostigmine bromide is a parasympathomimetic and a reversible cholinesterase inhibitor.
|
-
-
- HY-10163AS
-
|
|
|
Dabigatran-d4 (hydrochloride) is deuterium labeled Dabigatran, which is a reversible and selective, direct thrombin inhibitor (DTI) with a Ki value of 4.5 nM.
|
-
-
- HY-B0590S1
-
|
|
|
(+)-Tetrabenazine-d6 is the deuterium labeled (+)-Tetrabenazine. (+)-Tetrabenazine is a reversible inhibitor of vesicular monoamine transporter 2 (VMAT-2).
|
-
-
- HY-B0882S
-
|
|
|
Edrophonium-d5 (chloride) is the deuterium labeled Edrophonium chloride. Edrophonium chloride is a readily reversible acetylcholinesterase inhibitor; prevents breakdown of the neurotransmitter acetylcholine and acts by competitively inhibiting the enzyme acetylcholinesterase, mainly at the neuromuscular junction.
|
-
-
- HY-B0555BS
-
|
|
|
Nafcillin-d5 (sodium) is the deuterium labeled Nafcillin sodium. Nafcillin sodium, an antibiotic, is a reversible inhibitor of β-lactamase. Nafcillin sodium can be used for the research of staphylococcal infections[1][2].
|
-
-
- HY-18763S
-
|
|
|
Indobufen-d5 is deuterium labeled Indobufen. Indobufen is a platelet aggregation inhibitor. Indobufen is a reversible platelet cyclooxygenase (Cox) activity inhibitor. Indobufen suppresses thromboxane A2 (TxA2) synthesis. Indobufen down-regulates tissue factor (TF) in monocytes[1].
|
-
-
- HY-10163S
-
|
|
|
Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
-
- HY-10227S
-
|
|
|
Bortezomib-d8 is the deuterium labeled Bortezomib. Bortezomib (PS-341) is a reversible and selective proteasome inhibitor, and potently inhibits 20S proteasome (Ki=0.6 nM) by targeting a threonine residue. Bortezomib disrupts the cell cycle, induces apoptosis, and inhibits NF-κB. Bortezomib is the first proteasome inhibitor anticancer agent. Anti-cancer activity[1][2].
|
-
-
- HY-B0534S1
-
|
|
|
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
-
- HY-14248S
-
|
|
|
Letrozole-d4 (CGS 20267-d4) is the deuterium labeled Letrozole. Letrozole (CGS 20267) is a potent, selective, reversible and orally active non-steroidal inhibitor of aromatase, with an IC50 of 11.5 nM. Letrozole selective inhibits estrogen biosynthesis, and can be used for the research of breast cancer[1][2][3].
|
-
-
- HY-10163S2
-
|
|
|
Dabigatran- 13C6 is the 13C labeled Dabigatran[1]. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[2][3].
|
-
-
- HY-B0199AS
-
|
|
|
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
-
- HY-10163S3
-
|
|
|
Dabigatran- 13C,d3 is the 13C- and deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].
|
-
-
- HY-A0166S
-
|
|
|
Cilastatin- 15N,d3 is a 15N-labeled and deuterium labeled Cilastatin. Cilastatin (MK0791) is a reversible, competitive renal dehydropeptidase I inhibitor with an IC50 of 0.1 μM. Cilastatin inhibits the bacterial metallob-lactamase enzyme CphA with an IC50 of 178 μM. Cilastatin is an antibacterial adjunct[1][2][3].
|
-
-
- HY-B0034S1
-
|
|
|
Donepezil-d4 (hydrochloride) is the deuterium labeled Donepezil hydrochloride. Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
|
-
-
- HY-B0034S
-
|
|
|
Donepezil-d5 (hydrochloride) is deuterium labeled Donepezil (Hydrochloride). Donepezil Hydrochloride (E2020) is a reversible, selective AChE inhibitor with an IC50 of 6.7 nM for AChE activity. Donepezil shows high selectivity for AChE over BuChE[1]. Donepezil exhibits neuroprotective effect on Aβ42 neurotoxicity[2].
|
-
-
- HY-100642S
-
|
|
|
3-O-Methyltolcapone-d7 is a deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
|
-
-
- HY-B0534S
-
|
|
|
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
-
- HY-B0532AS
-
|
|
|
Trifluoperazine-d3 (dihydrochloride) is deuterium labeled Trifluoperazine (dihydrochloride). Trifluoperazine dihydrochloride, an antipsychotic agent, acts by blocking central dopamine receptors. Trifluoperazine dihydrochloride is a potent α1-adrenergic receptor antagonist. Trifluoperazine dihydrochloride is a potent NUPR1 inhibitor exerting anticancer activity. Trifluoperazine dihydrochloride is a calmodulin inhibitor, and also inhibits P-glycoprotein. Trifluoperazine dihydrochloride can be used for the research of schizophrenia. Trifluoperazine dihydrochloride acts as a reversible inhibitor of influenza virus morphogenesis[1][2][3][4][5].
|
-
-
- HY-N6608S
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Physostigmine-d3 is the deuterium labeled Physostigmine. Physostigmine (Eserine) is a reversible acetylcholinesterase (AChE) inhibitor. Physostigmine can crosses the blood-brain barrier and stimulates central cholinergic neurotransmission. Physostigmine can reverse memory deficits in transgenic mice with Alzheimer's disease. Physostigmine is also an antidote for anticholinergic poisoning[1][2][3][4].
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- HY-100642S1
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3-O-Methyltolcapone-d4 is the deuterium labeled 3-O-Methyltolcapone. 3-O-Methyltolcapone (Ro 40-7591) is a metabolite of Tolcapone. Tolcapone is an orally active, reversible, selective and potent COMT inhibitor. Tolcapone crosses the blood-brain barrier, and can be used for treatment of Parkinson's disease[1][2].
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- HY-18690S
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Enasidenib-d6 (AG-221-d6)is the deuterium labeledEnasidenib(HY-18690) . Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2 R140Q and IDH2 R172K, respectively .
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- HY-50667S1
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Apixaban-d3 (BMS-562247-01-d3)is the deuterium labeledApixaban(HY-50667) . Apixaban (BMS-562247-01) is a highly selective, reversible and orally active inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively . Apixaban is in development for the prevention and treatment of various thromboembolic diseases .
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- HY-10235S
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Telaprevir-d4 is the deuterium labeled Telaprevir. Telaprevir (VX-950) is a highly selective, reversible, and potent peptidomimetic inhibitor of the HCV NS3-4A protease, the steady-state inhibitory constant (Ki) of Telaprevir is 7 nM against a genotype 1 (H strain) NS3 protease domain plus a NS4A cofactor peptide[1][2][3]. Telaprevir inhibits SARS-CoV-2 3CLpro activity[4].
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- HY-W013636S
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2-Ketoglutaric acid- 13C5 is the 13C labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
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- HY-W013636S1
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2-Ketoglutaric acid-d4 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
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- HY-W013636S2
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2-Ketoglutaric acid-d6 is the deuterium labeled 2-Ketoglutaric acid[1]. 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM)[2].
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- HY-W013636S4
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2-Ketoglutaric acid-13C2 is a deuterated labeled 2-Ketoglutaric acid . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
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- HY-B0563S1
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Ropivacaine-d7 is deuterium labeled Ropivacaine. Ropivacain is a potent sodium channel blocker. Ropivacain blocks impulse conduction via reversible inhibition of sodium ion influx in nerve fibrese[1][2]. Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane[3]. Ropivacaine is used for the research of neuropathic pain management[1].
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- HY-W013636S3
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2-Ketoglutaric acid- 13C (Alpha-Ketoglutaric acid- 13C) is a 13C labeled 2-Ketoglutaric acid (HY-W013636) . 2-Ketoglutaric acid (Alpha-Ketoglutaric acid) is an intermediate in the production of ATP or GTP in the Krebs cycle. 2-Ketoglutaric acid also acts as the major carbon skeleton for nitrogen-assimilatory reactions. 2-Ketoglutaric acid is a reversible inhibitor of tyrosinase (IC50=15 mM) .
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- HY-A0009S
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Galanthamine-d3 (hydrobromide) is deuterium labeled Galanthamine (hydrobromide). Galanthamine hydrobromide (Galantamine hydrobromide) is a selective, reversible, competitive, alkaloid AChE inhibitor, with an IC50 of 0.35 µM. Galanthamine hydrobromide is a potent allosteric potentiating ligand (APL) of human α3β4, α4β2, α6β4 nicotinic receptors ( nAChRs). Galanthamine hydrobromide is developed for the research of Alzheimer's disease (AD)[1][2][3].
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- HY-B0563BS
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Ropivacaine-d7 hydrochloride is a deuterium labeled Ropivacaine (hydrochloride) (HY-B0563B) . Ropivacaine hydrochloride is a potent?sodium channel?blocker and blocks impulse conduction via reversible inhibition of?sodium ion influx?in nerve fibrese . Ropivacaine is also an inhibitor of K2P (two-pore domain potassium channel) TREK-1 with an IC50 of 402.7 μM in COS-7 cell's membrane . Ropivacaine is widely used for neuropathic pain?management in vivo .
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- HY-17387S1
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(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
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- HY-14280S
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Entacapone-d10 is the deuterium labeled Entacapone. Entacapone is a potent, reversible, peripherally acting and orally active catechol-O-methyltransferase (COMT) inhibitor. Entacapone inhibits COMT from rat brain, erythrocytes and liver with IC50 values of 10 nM, 20 nM, and 160 nM, respectively. Entacapone is selective for COMT over other catecholamine metabolizing enzymes, including MAO-A, MAO-B, phenolsulphotransferase M (PST-M) and PST-P (IC50s>50 µM). Entacapone can be used for the research of Parkinson's disease[1]. Entacapone serves as a inhibitor of FTO demethylation with an IC50 of 3.5 μM, can be used for the research of metabolic disorders[2].
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- HY-17623S
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Tegoprazan (CJ-12420; RQ-00000004), a potassium-competitive acid blocker, is a reversible, oral active and highly selective inhibitor of gastric H+/K+-ATPase that could control gastric acid secretion and motility, with IC50 values ranging from 0.29-0.52 μM for porcine, canine, and human H +/K +-ATPases in vitro. Tegoprazan significantly improves colitis in mice and enhances the intestinal epithelial barrier function. Tegoprazan is promising for research of Inflammatory bowel, gastric acid-related, motilityimpaired diseases .
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- HY-70057S1
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Safinamide-d4-1 is deuterium labeled Safinamide. Safinamide is a potent, selective, and reversible monoamine oxidase B (MAO-B) inhibitor (IC50=0.098 µM) over MAO-A (IC50=580 µM)[1]. Safinamide also blocks sodium channels and modulates glutamate (Glu) release, showing a greater affinity at depolarized (IC50=8 µM) than at resting (IC50=262 µM) potentials. Safinamide has neuroprotective and neurorescuing effects and can be used for the study of parkinson disease, ischemia stroke etc.al[2][3].
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Classification |
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- HY-23460
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4-Ethynyl-L-phenylalanine
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Alkynes
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p-Ethynylphenylalanine (4-Ethynyl-L-phenylalanine) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine 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-23460A
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4-Ethynyl-L-phenylalanine hydrochloride
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Alkynes
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p-Ethynylphenylalanine hydrochloride (4-Ethynyl-L-phenylalanine hydrochloride) is a potent, selective, reversible and competitive inhibitor of tryptophan hydroxylase (TPH), with a Ki of 32.6 μM . p-Ethynylphenylalanine (hydrochloride) 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-16373
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LNK-754; OSI-754
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Alkynes
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CP-609754 (LNK-754) is a potent and reversible farnesyltransferase inhibitor with potential anticancer activity.The IC50 for inhibiting farnesylation of recombinant human H-Ras is 0.57 ng/mL and recombinant K-Ras is 46 ng/mL . CP-609754 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-146691
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Alkynes
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hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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