104 Results for "

reversible activator

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

104 Results for "reversible activator" in MCE Product Catalog:

Cat. No.: HY-14930A
CAS No.: 862189-96-6
Purity:  99.85%
Synonyms: SK-3530 dihydrochloride
Mirodenafil (SK3530) dihydrochloride is an orally active, potent, reversible, and selective phosphodiesterase 5 (PDE5) inhibitor. Mirodenafil dihydrochloride is a glucocorticoid receptor (GR) modulator Mirodenafil dihydrochloride activates the Wnt/β-catenin signaling pathway by downregulating Dkk1 expression. Mirodenafil dihydrochloride can be used for the research of erectile dysfunction (ED), Alzheimer’s disease (AD) and systemic sclerosis (SSc) .
loading...
    loading...
Cat. No.: HY-134356
CAS No.: 3031-94-5
Purity:  99.95%
Synonyms: AICAR-5'-MP
AICA-riboside, 5′-phosphate is AICA riboside with a phosphate group. The functions of AICA riboside include: 1) conversion into AMP mimetic to selectively activate AMPK; 2) competition with adenosine for the uptake of nucleoside transporters, reversible blocking of adenosine reuptake, increasing extracellular adenosine concentration, and indirectly activating adenosine A1 receptors. AICA riboside is involved in metabolic regulation (promoting catabolism and inhibiting anabolism) and adenosine-dependent neuroprotection (inhibiting excitatory synaptic transmission). AICA riboside can be used in the study of metabolic diseases (such as diabetes and obesity) and neurological diseases (such as ischemia and epilepsy), and has central nervous system protective activity .
loading...
    loading...
Cat. No.: HY-100671
CAS No.: 321695-57-2
Purity:  99.44%
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 .
loading...
    loading...
Cat. No.: HY-W923198
CAS No.: 480439-15-4
Synonyms: Methacryloyloxy fluorescein
Fluorescein O-methacrylate (Methacryloyloxy fluorescein) is a pH-responsive fluorescent monomeric dye. Fluorescein O-methacrylate exhibits pH-responsive fluorescence properties: its fluorescence is activated under alkaline conditions and quenched under neutral or acidic conditions; reversible switching of fluorescence is achievable by adjusting the pH of the solution. Fluorescein O-methacrylate can be used as a monomer for the synthesis of amphiphilic fluorescein polymers. These polymers can self-assemble into stable polymer nanoparticles with enhanced aqueous-phase fluorescence, and also enable the conjugation of nanoparticles with amine-containing biomolecules to support sensitive optical detection of biomarkers (Ex/Em = 490/520 nm) .
loading...
    loading...
Cat. No.: HY-B0916
CAS No.: 114-26-1
Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests .
loading...
    loading...
Cat. No.: HY-N0430
CAS No.: 3486-66-6
Synonyms: Coptisin
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
loading...
    loading...
Cat. No.: HY-18200
CAS No.: 751475-53-3
Synonyms: E5555; ER-172594-00
Atopaxar (E5555) is a potent, orally active, selective and reversible thrombin receptor protease-activated receptor-1 (PAR-1) antagonist. Atopaxar, an antiplatelet agent, interferes with platelet signaling. Atopaxar can be used for the research of atherothrombotic disease .
loading...
    loading...
Cat. No.: HY-162333
CAS No.: 2842012-69-3
BAL-0028 is a reversible inhibitor of NLRP3 activation with an IC50 value of 25 nM. BAL-0028 binds closely to the NACHT domain of the NLRP3 with KD values of 104-123 nM. BAL-0028 can inhibit the secretion of IL-1β and has anti-inflammatory activity .
loading...
    loading...
Cat. No.: HY-153508
CAS No.: 2098490-06-1
Target:  

Chloride Channel

Research Areas:  

Others

ANO1-IN-4 (Compound 10bm) is a reversible inhibitor for calcium-activated chloride channel transmembrane protein 16A (TMEM16A, also known as ANO1) with an IC50 of 0.030 µM. ANO1-IN-4 exhibits good metabolic stability in rat liver microsomes. ANO1-IN-4 inhibits spontaneous contraction in mouse isolated ileum .
loading...
    loading...
Cat. No.: HY-122236
CAS No.: 342595-74-8
Purity:  99.52%
Research Areas:  

Cancer

UMK57 is a MCAK activator and kinetochore-microtubule destabilizer. UMK57 enhances MCAK-dependent microtubule depolymerization, increases kinetochore-microtubule turnover, reduces chromosome mis-segregation and lagging chromosomes, and inhibits cancer cell proliferation. UMK57 triggers adaptive resistance in Aurora B cancer cells via reversible Aurora B signaling pathway alterations. UMK57 can be used for the research of solid tumors .
loading...
    loading...
Cat. No.: HY-106901A
CAS No.: 34433-31-3
Purity:  98.47%
Synonyms: HI-6
Research Areas:  

Neurological Disease

Asoxime dichloride (HI-6) is an orally active thiosemicarbazone-based antidote. Asoxime dichloride is a reversible inhibitor of AChE, and its core mechanism of action is to re-activate AChE inhibited by nerve toxins, thereby restoring the cholinergic nerve function. Asoxime dichloride significantly restores the function of poisoned muscles without reactivating AChE. Asoxime dichloride is an antagonist of acetylcholine receptors (AChRs), including nicotinic receptor and α7 nAChR. Asoxime dichloride can serve as an effective immunomodulator, improving the immune effect of the nervous system .
loading...
    loading...
Cat. No.: HY-108464A
CAS No.: 1161-94-0
Purity:  98.1%
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 .
loading...
    loading...
Cat. No.: HY-133178
CAS No.: 131086-98-1
Purity:  99.72%
Synonyms: 3,4,8,9-Tetrahydroxy urolithin
Urolithin D (3,4,8,9-Tetrahydroxy urolithin) is a colonic metabolite of Ellagitannins and a competitive, reversible, and selective antagonist of the EphA receptor. Urolithin D inhibits EphA2-ephrin-A1 binding with an IC50 of 0.9 μM. Urolithin D is also a potent antioxidant that scavenges free radicals and repairs oxidized DNA damage. Additionally, Urolithin D suppresses triglyceride accumulation and promotes fatty acid oxidation by activating the AMPK signaling pathway. Urolithin D can be used for research on tumors, metabolic, and inflammatory diseases .
loading...
    loading...
Cat. No.: HY-149906
CAS No.: 153021-75-1
Synonyms: GEM91
Target:  

HIV mRNA

Research Areas:  

Infection

Trecovirsen (GEM91) is an antiviral agent targeting HIV gag mRNA, which hybridizes with complementary HIV gag mRNA at the initiation site. Trecovirsen induces a reversible, dose-dependent prolongation of activated partial thromboplastin time via its polyanionic property. Trecovirsen is applicable to research related to HIV infection .
loading...
    loading...
Cat. No.: HY-19638
CAS No.: 163706-06-7
Synonyms: AR-C69931MX
Cangrelor (AR-C69931MX), an adenosine triphosphate analogue, is an intravenous, reversible and selective platelet P2Y12 antagonist, with prompt and potent antiplatelet effects. Cangrelor directly blocks adenosine diphosphate (ADP)-induced activation and aggregation of platelets. Cangrelor is also a nonspecific GPR17 antagonist .
loading...
    loading...
Cat. No.: HY-177106
CAS No.: 1945941-72-9
Target:  

Drug Intermediate Ras

Research Areas:  

Cancer

ADT-1004 is an orally active prodrug of ADT-007 (HY-157887). ADT-007 is a reversible, highly potent and selective pan-RAS inhibitor that binds to the nucleotide-free conformation of RAS proteins and blocks their GTP activation, thereby inhibiting the downstream MAPK and AKT signaling pathways. ADT-1004 can be used for the research of pancreatic ductal adenocarcinoma .
loading...
    loading...
Cat. No.: HY-N7007
CAS No.: 55881-96-4
Sclareol glycol is a blood-brain barrier-permeable, reversible adenylate cyclase (AC) activator. Sclareol glycol induces dose-dependent changes in body temperature, regulates convulsive seizures and spontaneous activity. Sclareol glycol interacts with GABAergic transmission, thereby affecting dopamine-related behaviors. Sclareol glycol can be used in studies related to convulsive seizures, aggressive responses, thermoregulation, etc .
loading...
    loading...
Cat. No.: HY-107146
CAS No.: 371131-16-7
Purity:  99.84%
Synonyms: P1pal-7
PZ-128 (P1pal-7), a cell-penetrating lipopeptide pepducin, is a first-in-class, specific and reversible protease-activated receptor-1 (PAR1) antagonist. PZ-128 targets the cytoplasmic surface of PAR1 and interrupts signaling to internally-located G (PAR1-G) proteins. PZ-128 has antiplatelet, anti-metastatic, anti-angiogenic and anticancer effects .
loading...
    loading...
Cat. No.: HY-139664A
CAS No.: 2170140-50-6
Purity:  98.97%
Target:  

DNA Methyltransferase

Research Areas:  

Cancer

(R)-GSK-3685032 is the R-enantiomer of GSK-3685032 (HY-139664) and is a potent, non-covalent, reversible DNMT1-selective inhibitor with an IC50 of 0.036 μM against DNMT1. (R)-GSK-3685032 preferentially binds DNMT1 in a hemimethylated DNA context, inhibits DNA methylation maintenance by occupying the DNMT1 active site loop that inserts into DNA and by interacting with the target recognition domain, thereby inducing DNA hypomethylation and transcriptional activation. (R)-GSK-3685032 is useful for research on DNMT1, acute myeloid leukemia, and B cell humoral immunity .
loading...
    loading...
Cat. No.: HY-W020958
CAS No.: 14284-93-6
Synonyms: Tris(acetylacetonato)ruthenium (III)
Ru (acac) 3 (Tris (acetylacetonato) ruthenium (III)) is a caspase-3 activator and Apoptosis inducer. Ru (acac) 3 exerts growth inhibitory effects on various cell lines in vitro by inhibiting DNA/RNA synthesis and inducing mild reversible S-phase cell cycle arrest. Ru (acac) 3 is commonly used in research related to ovarian cancer, osteosarcoma, cervical cancer, melanoma, and other fields .
loading...
    loading...