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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
9373 Results for "
Competive Inhibitors
" in MedChemExpress (MCE) Product Catalog:
Products (9373)
9373 Results for "Competive Inhibitors" in MCE Product Catalog:
54
54 Publications Verification
Synonyms: Alvocidib Hydrochloride; L86-8275 Hydrochloride; HMR-1275 Hydrochloride
Flavopiridol Hydrochloride (Alvocidib Hydrochloride) is a broad inhibitor of CDK, competing with ATP to inhibit CDKs including CDK1, CDK2, CDK4 with IC50s of 30, 170, 100 nM, respectively.
31
Target:
Research Areas:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
Sitagliptin (MK-0431) is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin can be used for the study of 1-type and 2-type diabetes .
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31 Cited Publications
Synonyms: MK-0431 phosphate
Target:
Research Areas:
Sitagliptin (MK-0431) phosphate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate can be used for the study of 1-type and 2-type diabetes .
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31 Cited Publications
Synonyms: MK-0431 phosphate monohydrate
Target:
Research Areas:
Sitagliptin (MK-0431) phosphate monohydrate is an orally active and highly selective DPP4 inhibitor with an IC50 value of 19 nM. Sitagliptin phosphate monohydrate blocks the degradation of glucagon-like peptide-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) by competing inhibition mechanism (Kᵢ = 1 nM), thereby increasing the level of active incretin. Sitagliptin phosphate monohydrate can also directly stimulate the secretion of GLP-1 by intestinal L cells by activating the cAMP/PKA and ERK1/2 pathways, and this effect is independent of DPP-4. Sitagliptin phosphate monohydrate shows protective effects on pancreatic islet grafts in 1-type diabetes models. Sitagliptin phosphate monohydrate can be used for the study of 1-type and 2-type diabetes .
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27 Cited Publications
Target:
Research Areas:
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 .
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27 Cited Publications
Cat. No.: HY-108239
CAS No.: 1392399-03-9
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Research Areas:
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 .
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27 Cited Publications
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Research Areas:
GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
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27 Cited Publications
Cat. No.: HY-103586A
CAS No.: 2378280-82-9
Target:
Research Areas:
GS-441524 hydrochloride is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 hydrochloride competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 hydrochloride inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 hydrochloride reduces viral RNA levels in cats. GS-441524 hydrochloride can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
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Target:
Sulfamethoxazole (Ro 4-2130) is a sulfonamide antibiotic with a widespread antibacterial activity. Sulfamethoxazole inhibits bacterial folate metabolism by competing with 4-Aminobenzoic acid (HY-B1008) (PABA) to act on dihydropteroate synthetase and dihydropteroate reductase. Sulfamethoxazole can be used for the study of urinary tract infections (UTIs), prostatitis, and bronchitis .
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Sulfamethoxazole (Ro 4-2130) sodium is a sulfonamide antibiotic with a widespread antibacterial activity. Sulfamethoxazole sodium inhibits bacterial folate metabolism by competing with 4-Aminobenzoic acid (HY-B1008) (PABA) to act on dihydropteroate synthetase and dihydropteroate reductase. Sulfamethoxazole sodium can be used for the study of urinary tract infections (UTIs), prostatitis, and bronchitis .
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23 Cited Publications
Synonyms: Ro 4-2130 1000 µg/mL in methanol
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Research Areas:
Sulfamethoxazole (Ro 4-2130) 1000 μg/mL in methanol is a sulfonamide antibiotic with a widespread antibacterial activity. Sulfamethoxazole 1000 μg/mL in methanol inhibits bacterial folate metabolism by competing with 4-Aminobenzoic acid (HY-B1008) (PABA) to act on dihydropteroate synthetase and dihydropteroate reductase. Sulfamethoxazole 1000 μg/mL in methanol can be used for the study of urinary tract infections (UTIs), prostatitis, and bronchitis .
15
15 Cited Publications
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Research Areas:
SN-011 is a potent and selective mouse and human STING inhibitor, with an IC50 of 76 nM for STING signaling. SN-011 competes with cyclic dinucleotide (CDN) for the binding pocket of the STING dimer, blocking CDN binding and STING activation. SN-011 can be used for the research of STING-driven autoimmune and inflammatory disease .
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12 Cited Publications
Target:
Research Areas:
CU-CPT22 is a potent protein complex of toll-like receptor 1 and 2 (TLR1/2) inhibitor, and competes with the synthetic triacylated lipoprotein (Pam3CSK4) binding to TLR1/2 with a Ki of 0.41 µM. CU-CPT22 blocks Pam3CSK4-induced TLR1/2 activation with an IC50 of 0.58 µM .
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Research Areas:
Fludarabine (phosphate) is an analogue of adenosine and deoxyadenosine, which is able to compete with dATP for incorporation into DNA and inhibit DNA synthesis.
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9 Cited Publications
Research Areas:
FIDAS-5 is a potent and orally active methionine S-adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 2.1 μM. FIDAS-5 effectively competes against S-adenosylmethionine (SAM) for MAT2A binding. FIDAS-5 has anticancer activities .
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9 Cited Publications
Synonyms: 2'-Deoxycytidine monohydrochloride; Deoxycytidine hydrochloride; NSC 83251
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7
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7 Cited Publications
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IOX4 is a selective HIF prolyl-hydroxylase 2 (PHD2) inhibitor with an IC50 value of 1.6 nM, induces HIFα in cells and in wildtype mice with marked induction in the brain tissue. IOX4 competes with and displaces 2-oxoglutarate (2OG) at the active site of PHD2 .
5
PF-3450074 (PF-74) is a specifical inhibitor of HIV-1 capsid protein (CA) and displays a broad-spectrum inhibition of HIV isolates with submicromolar potency (EC50=8-640 nM). PF-3450074 (PF-74) acts at an early stage of HIV-1 infection, inhibits viral replication by directly competing with the binding of CPSF6 and NUP153, and blocks the uncoating, assembly, and the reverse transcription steps of the viral life cycle . CPSF6: nuclear host factors cleavage and polyadenylation specific factor 6; NUP153: nucleoporin 153.
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
