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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
128 Results for "
blockade
" in MedChemExpress (MCE) Product Catalog:
Products (128)
128 Results for "blockade" in MCE Product Catalog:
Cat. No.: HY-131691
CAS No.: 76991-05-4
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NMDAR blocker 1 is an NMDA receptor channel blocker with an IC50 of 5.0 μM. NMDAR blocker 1 exhibits fast on-off blockade kinetics and strong voltage dependence, and does not compete with glutamate or glycine. NMDAR blocker 1 prevents glutamate/NMDA-induced intracellular Ca 2+ overload, modulates the glutamate-nitric oxide-cGMP pathway. NMDAR blocker 1 prevents in vitro excitotoxic neurodegeneration of cultured cerebellar and hippocampal neurons. NMDAR blocker 1 attenuates excitotoxic insult in an mouse model of hyperammonemia-induced excitotoxicity. NMDAR blocker 1 can be used for the research of neurodegenerative diseases .
Cat. No.: HY-184574
HDAC-IN-104 is a potent and selective class I Histone deacetylases (HDAC) inhibitor with an IC50 of 25 nM. HDAC-IN-104 exerts potent antiproliferative and antitumor effects by inhibiting glycolysis and OXPHOS via blockade of the PI3K/AKT signaling pathway, and these effects are synergistically enhanced when combined with the FMS-like tyrosine kinase 3 (FLT3) inhibitor Quizartinib (AC220) (HY-13001). HDAC-IN-104 induces significant early and late apoptosis. HDAC-IN-104 can be used for acute myeloid leukemia (AML) research .
Cat. No.: HY-119800
CAS No.: 86487-64-1
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Setoperone is an orally active and potent 5-HT₂ receptor antagonist and a moderate dopamine D₂ receptor blocker. Setoperone dissociates from the receptors relatively quickly, but it is easily "captured" by serotonin receptors in the body, resulting in persistent receptor inhibition even after elution. Setoperone can be used to study the negative symptoms of type II schizophrenia and associated mood disorders .
Cat. No.: HY-183845
CAS No.: 2639366-75-7
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HTL0039732 is an orally active antagonist of the prostaglandin EP4 receptor (Prostaglandin E2 Receptor EP4). HTL0039732 reverses PGE2-induced differentiation toward M2-like macrophages. HTL0039732 exhibits efficacy in syngeneic tumor models and acts synergistically with PD-1/PD-L1 pathway blockers. HTL0039732 can be used for the research of advanced solid tumors .
Cat. No.: HY-180891
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Multitarget AD-IN-4 (compound IIIj) is a multitarget-directed ligand (MTDL), with the ability to simultaneously inhibit ChE enzymes (EeAChE IC50 = 0.157 μM, eqBuChE IC50 = 0.147 μM, hAChE IC50 = 1.551 μM, hBuChE IC50 = 2.152 μM), exhibit antioxidant activity, provide neuroprotection, and inhibit calcium channels (Ca 2+ channel blockade: IC50 = 30.59 μM). Multitarget AD-IN-4 reverses Scopolamine (HY-N0296)-induced amnesia in a mouse model. Multitarget AD-IN-4 can be used for Alzheimer’s disease (AD) research .
XMU-MP-2 is a selective BRK/PTK6 inhibitor with an IC50 of 5.4 nM. XMU-MP-2 inhibits the proliferation of BRK-positive breast cancer cells and induces apoptosis. XMU-MP-2 is applicable to breast cancer-related research .
Cat. No.: HY-178016
CAS No.: 3097193-89-7
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H3R antagonist 8 is a selective nonimidazole histamine H3 receptor antagonist (IC50 = 0.35 μM). H3R antagonist 8 exhibits hERG channel blockade activity (IC50 = 0.67 μM). H3R antagonist 8 inhibits seizures by antagonizing H3 receptor. H3R antagonist 8 reduces tonic hind limb extension (THLE) in mice in the maximal electroshock seizure (MES) model (ED50 = 20.21 mg/kg) and and shortens pentylenetetrazol (PTZ)-induced total movement distance in AB strain zebrafish larvae. H3R antagonist 8 can be used for the study of epilepsy .
Cat. No.: HY-180548
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MRC37 is a high-affinity TRIM21 ligand with a Kd of 0.4 µM. MRC37 targets the IgG Fc-binding pocket in the PRYSPRY domain of TRIM21, mimics the "HHNY" epitope, and inhibits substrate-induced aggregation and activation of TRIM21 via competitive blockade of antibody binding. MRC37 effectively blocks TRIM21-mediated antiviral immunity (such as adenovirus neutralization) and Trim-Away targeted protein degradation without cytotoxicity. MRC37 antagonizes TRIMTAC activity, and its multiple modification sites do not affect target binding, making it suitable as a degrader warhead for research on viral immunity and neurodegenerative diseases such as tauopathies .
Cat. No.: HY-13654
CAS No.: 878204-96-7
IPI-269609 is an orally effective Smoothed (SMO) inhibitor that targets the Hedgehog (Hh) signaling pathway. IPI-269609 specifically reduces the ALDH-bright (high aldehyde dehydrogenase activity) cell subset, which is considered the "cancer stem cells" in pancreatic cancer. IPI-269609 significantly inhibits the migration and colony formation of pancreatic cancer cells. IPI-269609 effectively inhibits pancreatic cancer metastasis in a mouse model. IPI-269609 can be used for pancreatic cancer research .
Cat. No.: HY-P2265A
CAS No.: 2896737-31-6
Cat. No.: HY-175188
CAS No.: 2404652-82-8
Synonyms: BPN-0027490
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MT-110 (BPN-0027490) is a non-muscle myosin NMIIB-selective inhibitor with high brain penetration and favorable safety profile. MT-110 specifically disrupts NMIIB-dependent actin dynamics in dendritic spines, while it exerts no significant adverse effects on cardiac myosin II and cardiac functions (such as cardiac output and heart rate) at tested concentrations. A single administration of MT-110 produces long-lasting (sustained for several weeks) blockade of methamphetamine motivation associated with environmental cues. MT-110 exhibits extremely high specificity, with no interference with cocaine motivation, hippocampus-dependent memory, fear memory, or locomotor and anxiety-like behaviors. MT-110 serves as a valuable tool compound for investigating the mechanisms of methamphetamine use disorder .
Cat. No.: HY-182372
CAS No.: 1638153-78-2
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SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
Cat. No.: HY-188081
CAS No.: 3112733-78-2
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YH-36400 is an orally bioavailable inhibitor of HIF-1α and HIF-2α. YH-36400 disrupts the dimerization of HIF-1α and HIF-1β and triggers proteasomal degradation, thereby inhibiting the transcriptional activities of HIF-1 and HIF-2. YH-36400 reduces the expression of PD-L1 and CD73, reprograms the tumor immune microenvironment, inhibits angiogenesis, and can be used in combination with immune checkpoint blockade therapy. YH-36400 is applicable to research related to breast cancer, lung cancer, melanoma, pancreatic cancer, colorectal cancer, prostate cancer, and head and neck squamous cell carcinoma .
Cat. No.: HY-B0653AS
Synonyms: (S)-(–)-Bupivacaie-d9hydrochloride
Cat. No.: HY-P991740
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Cat. No.: HY-12502B
CAS No.: 111011-53-1
Synonyms: NZ-105 hydrochloride; (±)-Efonidipine hydrochloride
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Efonidipine (NZ-105) hydrochloride is an orally active dual L-type and T-type calcium channel blocker (CCB) with IC50 values of 1.8 and 350 nM, respectively. Efonidipine hydrochloride inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride modulates adrenal steroidogenesis by increasing the expression of steroidogenic acute regulatory protein (StAR), dbcAMP-or angiotensin II-induced StAR mRNA expression and DHEA-S production, while suppressing the biosynthesis of aldosterone and cortisol. Efonidipine hydrochloride reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride improves cardiac function in heart failure models by inhibiting T-type calcium channels (via both tonic and use-dependent blockade), independently of blood pressure reduction. Efonidipine hydrochloride can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
Cat. No.: HY-169232
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Cat. No.: HY-P992353
Cat. No.: HY-P99916
CAS No.: 2449199-61-3
Synonyms: AMG-427
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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
