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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
222 Results for "
type II inhibitor
" in MedChemExpress (MCE) Product Catalog:
Products (222)
222 Results for "type II inhibitor" in MCE Product Catalog:
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74 Cited Publications
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LY2109761 is an orally active, selective TGF-β receptor type I/II inhibitor with Kis of 38 nM and 300 nM, respectively.
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58 Cited Publications
MRTX1133 is a noncovalent, potent, and selective alkyne-based KRAS G12D inhibitor. MRTX1133 optimally fills the switch II pocket and extends three substituents to favorably interact with the protein, resulting in an estimated KD against KRAS G12D of 0.2 pM. MRTX1133 prevents SOS1-catalyzed nucleotide exchange and/or formation of the KRAS G12D/GTP/RAF1 complex, thereby inhibiting mutant KRAS-dependent signal transduction. MRTX1133 selectively inhibits KRAS G12D mutant, but not KRAS wild-type, tumor cells. MRTX1133 has single digit nanomolar activity in cellular assays and marked in vivo efficacy in tumor models harboring KRAS G12D mutations .
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27 Cited Publications
Cat. No.: HY-N6732
CAS No.: 99533-80-9
Synonyms: SF2370; Antibiotic K 252a; Antibiotic SF 2370
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Telmisartan is a potent, long lasting antagonist of angiotensin II type 1 receptor (AT1), selectively inhibiting the binding of 125I-AngII to AT1 receptors with IC50 of 9.2 nM.
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17 Cited Publications
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GW788388 is a potent and selective inhibitor of ALK5 with IC50 of 18 nM, and also inhibits TGF-β type II receptor and activin type II receptor activities, without inhibiting BMP type II receptor.
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17 Cited Publications
Barbadin is a novel and selective β-arrestin/β2-adaptin interaction inhibitor, has IC50 values of 19.1 μM for β-arrestin1 and 15.6 μM for β-arrestin2. Barbadin blocks agonist-promoted endocytosis of the prototypical β2-adrenergic, V2-vasopressin and angiotensin-II type-1 receptors. Barbadin can induce apoptosis .
13
Research Areas:
Cardiovascular Disease Neurological Disease Metabolic Disease
Enalapril (MK-421) is an orally active angiotensin-converting enzyme inhibitor. Enalapril blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology .
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Cardiovascular Disease Neurological Disease Metabolic Disease
Enalapril maleate (MK-421 maleate) is an orally active angiotensin-converting enzyme inhibitor. Enalapril maleate blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril maleate inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril maleate attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril maleate reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril maleate is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology .
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Gepotidacin (GSK2140944) is a novel triazaacenaphthylene bacterial type II topoisomerase inhibitor.
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12 Cited Publications
Cat. No.: HY-16742B
CAS No.: 1624306-20-2
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Gepotidacin mesylate hydrate is an orally active triazaacenaphthylene antibiotic and bacterial type II topoisomerase inhibitor. Gepotidacin mesylate hydrate inhibits bacterial DNA replication by blocking topoisomerase enzymes. Gepotidacin mesylate hydrate selectively inhibits topoisomerase IV and the B subunit of DNA gyrase .
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8 Cited Publications
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CP-91149 is a GP (glycogen phosphorylase) inhibitor. CP-91149 promotes glycogen resynthesis, but not its overaccumulation. CP-91149 has the potential for Type II (insulin-dependent) diabetes study .
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Cardiovascular Disease Metabolic Disease Endocrinology Cancer
Spironolactone is an aldosterone antagonist that acts on the aldosterone mineralocorticoid receptor (IC50=24 nM) and androgen receptor (IC50=77 nM), promotes podocyte autophagy and regulates pain. Spironolactone improves hypertension-related vascular hypertrophy and remodeling by reducing angiotensin II (Ang II)-induced inflammation, reduces aldosterone-induced vascular and soft tissue calcification through PIT1-dependent signaling, and alleviates vascular dysfunction in type II diabetic mice by reducing oxidative stress and restoring NO/GC signaling; at low concentrations, it and its metabolites can interfere with aldosterone biosynthesis in the adrenal cortex and inhibit voltage-dependent Ca 2+ channels to exert antihypertensive effects .
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Naporafenib (LXH254) is a potent, selective, orally active, type II BRAF and CRAF inhibitor, with IC50 values of 0.072 and 0.21 nM against CRAF and BRAF, respectively .
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6 Cited Publications
Cat. No.: HY-P1110
CAS No.: 185413-30-3
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6 Cited Publications
Synonyms: AT2 receptor agonist C21
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology
Buloxibutid (AT2 receptor agonist C21) is an orally active, selective angiotensin II type 2 receptor (AT2R) agonist, with a Ki value of 0.4 nM for porcine AT2R. Buloxibutid exerts effects such as vasodilation, anti-inflammation, anti-fibrosis (promoting the expression of collagenase MMP-13) and tissue repair mainly by activating the NO/cGMP pathway, inhibiting the pro-proliferative MAPK signaling, and suppressing the pro-fibrotic TGF-β/Smad pathway as well as the inflammatory NF-κB pathway. Buloxibutid can be used in research related to idiopathic pulmonary fibrosis, hypertension, and systemic sclerosis .
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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
