104 Results for "

competitive manner

" in MedChemExpress (MCE) Product Catalog:
Products (104)

104 Results for "competitive manner" in MCE Product Catalog:

44
44 Publications Verification
Cat. No.: HY-13011
CAS No.: 1256580-46-7
Purity:  99.78%
Synonyms: CH5424802; RO5424802; RG7853
Alectinib (CH5424802; RO5424802; RG7853) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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44
44 Publications Verification
Cat. No.: HY-13011A
CAS No.: 1256589-74-8
Purity:  99.92%
Synonyms: CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
Alectinib (CH5424802; RO5424802; RG7853) Hydrochloride is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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12
12 Cited Publications
Cat. No.: HY-10119
CAS No.: 618385-01-6
Purity:  99.79%
Synonyms: SCH 530348
Vorapaxar (SCH 530348), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar (SCH 530348) inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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12
12 Cited Publications
Cat. No.: HY-100201
CAS No.: 1982372-88-2
Purity:  99.73%
Research Areas:  

Cancer

A-196 is a potent and selective inhibitor of SUV420H1 and SUV420H2 with IC50 values of 25 nM and 144 nM, respectively. A-196 inhibits SUV4-20 biochemically in a substrate-competitive manner. A-196 represents a first-in-class chemical probe of SUV4-20 to investigate the role of histone methyltransferases in genomic integrity .
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12
12 Cited Publications
Cat. No.: HY-10119A
CAS No.: 705260-08-8
Purity:  99.81%
Synonyms: SCH 530348 sulfate
Vorapaxar sulfate (SCH 530348 sulfate), an antiplatelet agent, is a selective, orally active, and competitive thrombin receptor protease-activated receptor (PAR-1) antagonist (Ki=8.1 nM). Vorapaxar sulfate inhibits thrombin receptor-activating peptide (TRAP)-induced platelet aggregation in a dose-dependent manner .
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7
7 Cited Publications
Cat. No.: HY-15959
CAS No.: 1313725-88-0
Synonyms: Volitinib; HMPL-504; AZD-6094
Target:  

c-Met/HGFR

Research Areas:  

Cancer

Savolitinib (AZD-6094) is a potent, highly selective, and orally bioavailable c-Met inhibitor with IC50 s of 5 nM and 3 nM for c-Met and p-Met, respectively. Savolitinib (AZD-6094) selectively binds to and inhibits the activation of c-Met in an ATP-competitive manner, and disrupts c-Met signal transduction pathways. Antineoplastic activity .
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5
5 Cited Publications
Cat. No.: HY-B0091
CAS No.: 106685-40-9
Synonyms: CD271
Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
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5
5 Cited Publications
Cat. No.: HY-B0091A
CAS No.: 911110-93-5
Synonyms: CD 271 sodium salt
Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity .
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3
3 Cited Publications
Cat. No.: HY-P1178
CAS No.: 1203586-72-4
Target:  

Trk Receptor p38 MAPK

Research Areas:  

Neurological Disease

Cyclotraxin B is a BBB-penetrable and selective TrkB inhibitor. Cyclotraxin B inhibits BDNF-induced TrkB activity in a non-competitive manner, with an IC50 of 0.30 nM. Cyclotraxin B has analgesic and anxiolytic effects .
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3
3 Cited Publications
Cat. No.: HY-N5072
CAS No.: 17817-31-1
Synonyms: 4',6,7-Trihydroxyisoflavone
Desmethylglycitein (4',6,7-Trihydroxyisoflavone), a metabolite of daidzein, sourced from Glycine max with antioxidant, and anti-cancer activities. Desmethylglycitein binds directly to CDK1 and CDK2 in vivo, resulting in the suppresses CDK1 and CDK2 activity . Desmethylglycitein is a direct inhibitor of protein kinase C (PKC)α, against solar UV (sUV)-induced matrix matrix metalloproteinase 1 (MMP1) . Desmethylglycitein binds to PI3K in an ATP competitive manner in the cytosol, where it inhibits the activity of PI3K and downstream signaling cascades, leading to the suppression of adipogenesis in 3T3-L1 preadipocytes .
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2
2 Cited Publications
Cat. No.: HY-B0607
CAS No.: 104206-65-7
Synonyms: NTBC; Nitisone; SC0735
Target:  

HPPD

Research Areas:  

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 .
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2
2 Cited Publications
Cat. No.: HY-B1324
CAS No.: 64211-46-7
Synonyms: Ro 13-8996
Research Areas:  

Infection Cancer

Oxiconazole (Ro 13-8996) nitrate is a broad spectrum anti-fungal agent which can inhibit the growth of Candida, Aspergillus and Trichophyton. Oxiconazole nitrate is also a highly efficacious activator of CYP3A4 transactivation, which could be antagonized by Rifampicin (HY-B0272) in a competitive manner. Oxiconazole nitrate exhibits inhibitory effect against colorectal cancer (CRC) via peroxiredoxin-2 (PRDX2)-mediated autophagy arrest .
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2
2 Cited Publications
Cat. No.: HY-106840
CAS No.: 118101-09-0
Purity:  99.93%
L-365260 is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors. L-365260 can enhance Morphine analgesia and prevents Morphine tolerance .
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2
2 Cited Publications
Cat. No.: HY-W007686
CAS No.: 3251-69-2
Synonyms: Imidazolyl-4-acetic acid hydrochloride
Imidazoleacetic acid hydrochloride is a γ-aminobutyric acid receptor agonist. Imidazoleacetic acid hydrochloride inhibits GABA-T in a non-competitive manner, with a Ki value of 0.34 mM. Imidazoleacetic acid hydrochloride increases total free GABA in brain .
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2
2 Cited Publications
Cat. No.: HY-106840A
Purity:  99.75%
L-365260 hemihydrate is an orally active and selective antagonist of non-peptide gastrin and brain cholecystokinin receptor (CCK-B), with Kis of 1.9 nM and 2.0 nM, respectively. L-365260 hemihydrate interacts in a stereoselective and competitive manner with guinea pig stomach gastrin and brain CCK receptors .
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1
1 Cited Publications
Cat. No.: HY-107522
CAS No.: 205309-81-5
Purity:  99.54%
Target:  

EAAT

Research Areas:  

Neurological Disease

DL-TBOA is a potent non-transportable inhibitor of excitatory amino acid transporters with IC50s of 70 μM, 6 μM and 6 μM for excitatory amino acid transporter-1 (EAAT1), EAAT2 and EAAT3, respectively. DL-TBOA inhibits the uptake of [ 14C]glutamate in COS-1 cells expressing the human EAAT1 and EAAT2 with Ki valuesof 42 μM and 5.7 μM, respectively. DL-TBOA blocks EAAT4 and EAAT5 in a competitive manner with Ki values of 4.4 μM and 3.2 μM, respectively .
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1
1 Cited Publications
Cat. No.: HY-N4183
CAS No.: 72357-31-4
Licoflavone C is a broad-spectrum antiviral inhibitor with estrogen-like properties. Licoflavone C binds to viral endonuclease (CEN) and inhibits the replication of various bunyaviruses including severe fever with thrombocytopenia syndrome virus (SFTSV) and lymphocytic choriomeningitis virus in a non-substrate competitive manner. The IC50 values of Licoflavone C against SFTSV CEN and SFTSV CEN are 35.5 μM and 135.8 μM, respectively, and its Kd value against SFTSV CEN is 9.53 μM. After viral entry into cells, Licoflavone C reduces viral loads in mouse tissues in a dose-dependent manner, and exhibits extremely low cytotoxicity and genotoxicity. Licoflavone C induces apoptosis by increasing caspase 3/7 activity, blocks the cell cycle, and alleviates chemotherapy-induced chromosomal damage. Licoflavone C is applicable to the research on severe fever with thrombocytopenia syndrome and related viral infection mechanisms .
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1
1 Cited Publications
Cat. No.: HY-N10403
CAS No.: 5976-61-4
Synonyms: 4-Hydroxy-17β-estradiol
4-Hydroxyestradiol (4-Hydroxy-17β-estradiol) is an endogenous metabolite of Estradiol (HY-B0141). 4-Hydroxyestradiol is carcinogenic and shows mutagenic activity in breast epithelial cells. 4-Hydroxyestradiol inhibits the binding of Estradiol to the estrogen receptor in a competitive manner, with a Ki of 0.48 nM .
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1
1 Cited Publications
Cat. No.: HY-114641A
CAS No.: 192581-24-1
Purity:  99.44%
Target:  

Leukotriene Receptor

Research Areas:  

Inflammation/Immunology

BIIL-260 hydrochloride is a potent and long-acting orally active leukotriene B(4) receptor LTB4 antagonist, with anti-inflammatory activity. BIIL-260 hydrochloride interacts with the LTB4 receptor in a saturable, reversible, and competitive manner, has high affinity to the LTB4 receptor on isolated human neutrophil cell membranes with Ki values of 1.7 nM .
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1
1 Cited Publications
Cat. No.: HY-101169
CAS No.: 170964-68-8
Purity:  99.93%
Target:  

Monoamine Oxidase

Research Areas:  

Neurological Disease

Tetrindole mesylate is a selective inhibitor of monoamine oxidase A (MAO A). Tetrindole mesylate inhibits rat brain mitochondrial MAO A in a competitive manner with a Ki value of 0.4 μM and inhibits MAO B with a Ki of 110 μM. Tetrindole mesylate has antidepressant activity .
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