Search Result
Results for "
uncompetitive
" in MedChemExpress (MCE) Product Catalog:
1
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-N1882
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Cytochrome P450
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Metabolic Disease
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4,5-Dimethoxycanthin-6-one is a potent and uncompetitive inhibitor of CYP1A2-mediated phenacetin O-deethylation with an IC50 value of 1.7μM and a Ki value of 2.6 μM. 4,5-Dimethoxycanthin-6-one, as an alkaloid, is isolated from the wood of Picrasma quassioides BENNET (Simaroubaceae) .
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- HY-19966
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Kinesin
Apoptosis
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Cancer
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K858 Racemic is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM.
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- HY-113568
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- HY-125969
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Histone Acetyltransferase
Fungal
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Infection
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Rtt109 inhibitor 1 (Compound 1) is an inhibitor for histone acetyltransferase Rtt109 through a tight binding, uncompetitive system. Rtt109 inhibitor 1 exhibits antifungal activity through acetylation at H3K56 site .
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- HY-151813
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Others
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Cancer
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NNMT-IN-4 (compound 38) is a selective, uncompetitive and membrane permeability nicotinamide N-methyltransferase (NNMT) inhibitor with IC50 values of 42 and 38 nM in vitro biochemical and cell-based assays, respectively. NNMT-IN-4 shows favorable PK/PD and safety profiles as well as excellent oral bioavailability and pharmaceutical properties. NNMT-IN-4 can be used as a vivo chemical probe of NNMT .
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- HY-150621
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Others
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Cancer
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AS1134900 is a highly selective, allosteric and uncompetitive NADP +-dependent malic enzyme 1 (ME1) inhibitor .
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- HY-162474
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- HY-12058
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ARRY-424704; ARRY-704
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MEK
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Cancer
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AZD8330 (ARRY-424704) is a potent, uncompetitive MEK1/MEK2 inhibitor, with an IC50 of 7 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-N0430
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- HY-158021
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Tyrosinase
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Cancer
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Tyrosinase-IN-26 (compound 13) is a uncompetitive tyrosinase inhibitor with the an IC50 value of 68.86 µM. Tyrosinase-IN-26 can suppresses melanogenesis .
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- HY-N0430A
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- HY-12989
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- HY-103081
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Bacterial
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Infection
Cancer
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β-Glucuronidase-IN-1 is a potent, selective, uncompetitive, and orally active E. coli bacterial β-glucuronidase inhibitor, exhibiting an IC50 and a Ki of 283 nM and 164 nM, respectively .
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- HY-151338
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Cholinesterase (ChE)
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Neurological Disease
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AChE-IN-25 is a potent, selective and uncompetitive acetylcholinesterase (AChE) inhibitor (IC50=2.95 µM). AChE-IN-25 can be used in Alzheimer's disease research .
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- HY-147661
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Antifolate
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Infection
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DHFR-IN-2 (compound 4e) is a potent and uncompetitive inhibitor for MtDHFR (dihydrofolate reductase from M. tuberculosis), with an IC50 of 7 μM. DHFR-IN-2 can be used for tuberculosis (TB) research .
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- HY-W013571
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Fungal
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Infection
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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 .
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- HY-15587
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DNA/RNA Synthesis
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Cancer
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L82 is a selective and uncompetitive DNA ligase 1 (DNA Lig1) inhibitor (hLig1 IC50=12 μM). L82 shows anti-proliferative activity to breast cancer cells .
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- HY-B0421
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- HY-B0421A
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- HY-147216A
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Lactate Dehydrogenase
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Metabolic Disease
Inflammation/Immunology
Cancer
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AXKO-0046 dihydrochloride, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor. AXKO-0046 dihydrochloride has LDHB inhibitory activity with an EC50 value of 42 nM. AXKO-0046 dihydrochloride can be used for the research of cancer metabolism .
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- HY-107695
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FPL 12924AA
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iGluR
Sodium Channel
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Neurological Disease
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Remacemide hydrochloride (FPL 12924AA), a moderate inhibitor of the Na + channel, is a weak uncompetitive NMDA receptor antagonist with IC50s of 68 μM and 76 μM for MK-801 binding and NMDA currents, respectively . Remacemide hydrochloride is an anticonvulsant agent .
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- HY-147216
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Lactate Dehydrogenase
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Cancer
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AXKO-0046, indole derivative, is an uncompetitive Lactate dehydrogenase B (LDHB) selective inhibitor.AXKO-0046 has LDHB inhibitory activity with an EC50 value of 42 nM.AXKO-0046 can be used for the research of cancer metabolism .
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- HY-155238
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GABA Receptor
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Neurological Disease
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E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
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- HY-106408A
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Salfaprodil; Neu2000 potassium
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iGluR
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Neurological Disease
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Nelonemdaz (Salfaprodil) potassium is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz potassium is also a free radical scavenger. Nelonemdaz potassium has excellent neuroprotection against NMDA- and free radical-induced cell death .
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- HY-146588
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iGluR
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Neurological Disease
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NMDA receptor antagonist 4 (IIc) is a uncompetitive, voltage-dependent, orally active NMDAR blocker, with an IC50 of 1.93 µM. NMDA receptor antagonist 4 shows a positive predicted blood-brain-barrier (BBB) permeability, and can be studied in Alzheimer's disease .
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- HY-112711
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Atg4
Autophagy
Cathepsin
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Cancer
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LV-320 is a potent and uncompetitive ATG4B inhibitor with an IC50 of 24.5 µM and a Kd of 16 µM. LV-320 inhibits ATG4B enzymatic activity, blocks autophagic flux in cells, and is stable, non-toxic and active in vivo .
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- HY-16946
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Acetyl-CoA Carboxylase
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Metabolic Disease
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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 .
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- HY-106408
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Salfaprodil free base; Neu2000
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iGluR
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Neurological Disease
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Nelonemdaz (Salfaprodil free base) is an NR2B-selective and uncompetitive antagonist of N-methyl-D-aspartate (NMDA). Nelonemdaz is also a free radical scavenger. Nelonemdaz has excellent neuroprotection against NMDA- and free radical-induced cell death .
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- HY-N7389B
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Endogenous Metabolite
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Metabolic Disease
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GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
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- HY-N7389A
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Endogenous Metabolite
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Metabolic Disease
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GDP-α-D-mannose disodium is the donor substrate for mannosyltransferases and the precursor of GDP-β-L-fucose. GDP-α-D-mannose disodium gives a competitive inhibition with respect to GTP (Ki 14.7 μM) and an uncompetitive inhibition with respect to mannose-1-P (Ki 115 μM) .
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- HY-107385
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ONO-9302; SKF105657
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5 alpha Reductase
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Cancer
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Epristeride (ONO-9302) is a selective, specific and orally active uncompetitive inhibitor of human steroid 5 alpha-reductase isoform 2. Epristeride has inhibitory effects for SR isoenzymes types 2 with Ki value of 0.7-2 nM. Epristeride can be used for the research of prostatic hyperplasia and acne .
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- HY-150504
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Others
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Inflammation/Immunology
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ERAP2-IN-1 (compound 61) is an uncompetitive ERAP2 inhibitor. ERAP2-IN-1 specifically inhibits the ERAP2 peptide hydrolysis activity, inhibiting Arg-AMC hydrolysis with an IC50 of 27 μM and model peptide hydrolysis with an IC50 of 44 μM .
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- HY-146668
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Cholinesterase (ChE)
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Neurological Disease
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AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity .
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- HY-147328
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Apoptosis
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Cancer
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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 .
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- HY-N0736
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- HY-15610
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RG 7421; MEK inhibitor 1
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MEK
Apoptosis
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Cancer
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GDC-0623 (RG 7421) is a potent, ATP-uncompetitive inhibitor of MEK1 (Ki=0.13 nM, +ATP), and displays 6-fold weaker potency against HCT116 (KRAS (G13D), EC50=42 nM) versus A375 (BRAF V600E, EC50=7 nM).
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- HY-N7683
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Glucosidase
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Metabolic Disease
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Prunetin 5-O-β-D-glucopyranoside is an isoflavone isolated from extracts of Potentilla astracanica. Prunetin 5-O-β-D-glucopyranoside is a potent and uncompetitive inhibitor of α-glucosidase, with an IC50 of 56.05 μg/mL. Prunetin 5-O-β-D-glucopyranoside can be used for the research of type-2 diabetes .
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- HY-144778
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Indoleamine 2,3-Dioxygenase (IDO)
Apoptosis
Bcl-2 Family
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Cancer
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IDO1/TDO-IN-1 (30) is a potent dual IDO1 (uncompetitive, Ki of 0.23 μM) and TDO (competitive, Ki of 0.73 μM) inhibitor. IDO1/TDO-IN-1 (30) significantly promotes cell apoptosis through the potential mitochondria-mediated Bcl-2/Bax pathway .
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- HY-148161
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DNA/RNA Synthesis
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Cancer
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L82-G17 is an uncompetitive DNA ligase I (Lig I)-selective inhibitor. L82-G17 inhibits the third step of the ligation reaction, phosphodiester bond formation. L82-G17can be used as a probe of the catalytic activity .
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- HY-N1457
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P-glycoprotein
Cytochrome P450
Ferroptosis
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Metabolic Disease
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Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A .
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- HY-116866
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Lipoxygenase
Fungal
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Infection
Inflammation/Immunology
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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 .
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- HY-B0421S2
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Mycophenolate-13C17
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Isotope-Labeled Compounds
Flavivirus
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Cancer
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Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
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- HY-128717
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EPZ019997
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Histone Methyltransferase
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Cancer
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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 .
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- HY-128717A
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EPZ019997 dihydrochloride
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Histone Methyltransferase
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Cancer
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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 .
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- HY-128717B
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EPZ019997 trihydrochloride
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Histone Methyltransferase
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Cancer
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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 .
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- HY-N0110
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- HY-N0110A
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- HY-N0110B
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- HY-N0110R
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Apoptosis
Virus Protease
Indoleamine 2,3-Dioxygenase (IDO)
Parasite
Bacterial
Aurora Kinase
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Cancer
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Palmatine (chloride) (Standard) is the analytical standard of Palmatine (chloride). This product is intended for research and analytical applications. Palmatine chloride is an orally active and irreversible indoleamine 2,3-dioxygenase 1 (IDO-1) inhibitor with IC50s of 3 μM and 157μM against HEK 293-hIDO-1 and rhIDO-1, respectively. Palmatine chloride can also inhibit West Nile virus (WNV) NS2B-NS3 protease in an uncompetitive manner with an IC50 of 96 μM. Palmatine chloride shows anti-cancer, anti-oxidation, anti-inflammatory, neuroprotection, antibacterial, anti-viral activities .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
Cat. No. |
Product Name |
Chemical Structure |
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- HY-B0421S2
-
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Mycophenolic acid-13C17 (Mycophenolate-13C17) is the 13C labeled Mycophenolic acid (HY-B0421). Mycophenolic acid is a potent uncompetitive inosine monophosphate dehydrogenase (IMPDH) inhibitor with an EC50 of 0.24 μM. Mycophenolic acid demonstrates antiviral effects against a wide range of RNA viruses including influenza. Mycophenolic acid is an immunosuppressive agent. Antiangiogenic and antitumor effects.
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