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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
2407 Results for "
decrease
" in MedChemExpress (MCE) Product Catalog:
Products (2407)
2407 Results for "decrease" in MCE Product Catalog:
Art. -Nr.: HY-169433
Target:
Forschungsgebiete:
Naph-Se-TMZ is a PROTAC-like HDAC1 degrader. Naph-Se-TMZ induces ROS-dependent reduction in HDAC1 protein expression and total HDAC activity, and decreases cell viability in a dose-dependent manner. Naph-Se-TMZ exhibits activity in both TMZ-sensitive and TMZ-resistant glioma cells, and its cytotoxicity is reversed by the ROS scavenger N-acetylcysteine (HY-B0215). Naph-Se-TMZ can be used in studies related to glioblastoma .
Naph-Se-TMZ consists of a target protein ligand (red segment): Temozolomide (HY-17364), a DNA intercalator (blue segment): Nitro-Naphthalimide-C2-acylamide (HY-169437), and a molecular linker (black segment). Meanwhile, the activity control for the target protein ligand is Temozolomide-amino hydrochloride (HY-169439), and the DNA intercalator+linker is NNISC-2 (HY-169438).
Naph-Se-TMZ consists of a target protein ligand (red segment): Temozolomide (HY-17364), a DNA intercalator (blue segment): Nitro-Naphthalimide-C2-acylamide (HY-169437), and a molecular linker (black segment). Meanwhile, the activity control for the target protein ligand is Temozolomide-amino hydrochloride (HY-169439), and the DNA intercalator+linker is NNISC-2 (HY-169438).
Art. -Nr.: HY-17357S
CAS. Nr.: 1246814-53-8
Synonyms: AHR-9434-d5; AL-6515-d5
Art. -Nr.: HY-176036
CAS. Nr.: 3070323-06-4
Target:
Forschungsgebiete:
MS1262 is a blood-brain barrier-permeable, selective inhibitor of histone methyltransferases G9a (EHMT2) and GLP (EHMT1), with an IC50 of 19 nM and a Kd of 74 nM against G9a, and an IC50 of 6 nM and a Kd of 19 nM against GLP. MS1262 reduces the dimethylation level of histone H3 lysine 9 and decreases the size of Aβ plaques. MS1262 restores hippocampal long-term potentiation (LTP) and miniature excitatory postsynaptic current (sEPSC) frequency, ameliorates spatial memory deficits, and reverses anxiety-like and depression-like behaviors in AD model mice. MS1262 reverses the expression/phosphorylation levels of early AD biomarkers, providing support for stage-specific diagnosis of AD. MS1262 reduces the risk of thrombus rupture. MS1262 can be used in research related to Alzheimer's disease, colorectal cancer, and triple-negative breast cancer .
Art. -Nr.: HY-181576
CAS. Nr.: 3115784-59-0
Target:
Forschungsgebiete:
ROCK2-IN-14 is an orally active, selective ROCK2 inhibitor (IC50=4.8 nM) with 212-fold selectivity over ROCK1 (IC50=1.01 μM). By inhibiting the ROCK2/S100A9 signaling pathway, ROCK2-IN-14 downregulates S100A9 expression, inhibits NM2 phosphorylation and restores cytoskeletal abnormalities. Furthermore, ROCK2-IN-14 reduces inflammatory cytokine levels, alleviates skin inflammation and exerts anti-inflammatory activity. ROCK2-IN-14 also significantly inhibits ear thickening in a mouse model of atopic dermatitis (AD), and decreases the levels of IgE, TNF-α, IL-6 and TSLP. ROCK2-IN-14 can be used for research on atopic dermatitis .
Art. -Nr.: HY-181726
Target:
Forschungsgebiete:
BRAFV600E/ABL2-IN-2 is a dual BRAFV 600E and ABL2 kinase inhibitor, with an IC50 of 0.088 μM against human BRAFV 600E and an IC50 of 0.3 μM against human ABL2. BRAFV600E/ABL2-IN-2 reduces the phosphorylation levels of downstream ERK1/2 and CrkL in melanoma cells. BRAFV600E/ABL2-IN-2 decreases the expression of P-glycoprotein (P-glycoprotein) in melanoma cells. BRAFV600E/ABL2-IN-2 induces G1 cell cycle arrest and apoptosis (Apoptosis) in melanoma cells. BRAFV600E/ABL2-IN-2 is applicable to relevant research on melanoma .
Art. -Nr.: HY-18234
CAS. Nr.: 55123-66-5
Leupeptin is a broad-spectrum protease inhibitor . By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin can be used in research on chronic inflammatory diseases and skin tumorigenesis .
Art. -Nr.: HY-182366
Target:
Forschungsgebiete:
EED-IN-5 is an orally active, EZH2-selective trisubstituted pyridine-based EED-H3K27me3 inhibitor and immunomodulator with anti-inflammatory activity. The IC50 value of EED-IN-5 against EED is 28.21 nM. In mouse models, EED-IN-5 preferentially and persistently accumulates in lymph nodes after oral administration. By reducing the H3K27me3 level of dendritic cells and inhibiting their migration, EED-IN-5 decreases the infiltration of specific dendritic cells, macrophages and T cells into the spinal cord and brain. EED-IN-5 exhibits hERG inhibitory activity, shows negative results in the Mini-Ames test, and causes no obvious toxicity upon long-term high-dose administration. EED-IN-5 can be used for the research of multiple sclerosis .
Art. -Nr.: HY-182469
Target:
Lactate Dehydrogenase AMPK FOXO Interleukin Related Reactive Oxygen Species (ROS) TNF Receptor Bcl-2 Family Caspase Apoptosis
Forschungsgebiete:
FuBIG is an iminoguanidine derivative with neuroprotective effects. FuBIGL inhibits L-LDH activation and reduces lactate production. FuBIGL exerts protective effects on inflammatory nerve cells, upregulates the expressions of AMPK, pAMPK and FOXO3, and activates the AMPK pathway in cells. FuBIG exerts anti-inflammatory effects by reducing pro-inflammatory cytokines (IL-6, IL-1β, TNF-α) and increasing the anti-inflammatory cytokine IL-10. FuBIG maintains mitochondrial membrane potential, alleviates mitochondrial dysfunction, reduces ROS production, and relieves oxidative stress. FuBIG upregulates Bcl-2, downregulates Bax and Caspase-3, and inhibits cell apoptosis (apoptosis). FuBIG improves metabolic disorders in diabetic mice, decreases the levels of LDL-C, ALT and AST, and increases HDL-C level simultaneously. FuBIG can be used in the research of diabetic neuroinflammation .
Art. -Nr.: HY-183478
CAS. Nr.: 39740-82-4
Target:
Ser/Thr Protease Cathepsin Autophagy SARS-CoV Atg8/LC3 NO Synthase COX p62 Arginase PTEN NF-κB PI3K Akt p38 MAPK ERK Reactive Oxygen Species (ROS)
Forschungsgebiete:
Leupeptin hydrochloride is a broad-spectrum protease inhibitor . By inhibiting the activation of the PTEN/PI3K/Akt/NF-κB/ERK1/2/p38 signaling pathway, Leupeptin hydrochloride significantly reduces LPS-induced NO and ROS production, mitochondrial membrane potential hyperpolarization, phagocytic activity, pro-inflammatory cytokine release, and M1 polarization in mouse peritoneal macrophages, and reverses autophagic flux impairment. It also decreases Concanavalin A (HY-P2149)-induced proliferation index of mouse splenic lymphocytes and the Th1/IL-10 and Th2/IL-10 cytokine ratios, thereby modulating innate and adaptive immune responses. Leupeptin hydrochloride inhibits blood coagulation and tumorigenesis in mouse skin. Leupeptin hydrochloride can be used in research on chronic inflammatory diseases and skin tumorigenesis .
Art. -Nr.: HY-187097
Forschungsgebiete:
SARS-CoV-2 3CLpro-IN-40 is a SARS-CoV-2 3CL pro inhibitor with an IC50 of 2.041 μM. SARS-CoV-2 3CLpro-IN-40 reduces the expression level of viral nucleocapsid protein and the expression levels of proinflammatory cytokines (IL-6, TNF-α and IFN-β). SARS-CoV-2 3CLpro-IN-40 decreases the RNA level of infectious bronchitis virus. SARS-CoV-2 3CLpro-IN-40 inhibits SARS-CoV-2 infection. SARS-CoV-2 3CLpro-IN-40 reduces the replication level of HCoV-OC43. SARS-CoV-2 3CLpro-IN-40 is applicable to research related to coronavirus infection .
Art. -Nr.: HY-187719
CAS. Nr.: 318262-42-9
Target:
Forschungsgebiete:
NIK-12192 is an orally active inhibitor of vacuolar H +-ATPase. NIK-12192 reduces intracellular pH, decreases lysosomal volume and acidity, and alters the intracellular localization of V-ATPase by inhibiting proton pumps . NIK-12192 induces αvβ5 integrin polarization, cytoskeletal disruption, cell detachment, anoikis-mediated delayed apoptosis and necrosis, a delayed reduction in mitochondrial membrane potential, and lysosomal/phagosomal accumulation. NIK-12192 inhibits tumor cell migration, invasion, and three-dimensional spheroid growth, and enhances the activity of Topotecan (HY-13768). NIK-12192 suppresses spontaneous lung metastasis in vivo. NIK-12192 is used in research related to colon cancer, ovarian cancer, lung cancer, breast cancer, renal cancer, prostate cancer, acute myeloid leukemia, and melanoma .
Art. -Nr.: HY-189214
Target:
Forschungsgebiete:
eNOS activator-1 is an orally active, blood-brain barrier permeable endothelial nitric oxide synthase (eNOS) activator. eNOS activator-1 upregulates eNOS mRNA expression, enhances endogenous NO biosynthesis, and activates the eNOS signaling pathway to maintain blood-brain barrier integrity. eNOS activator-1 upregulates the protein expression levels of PI3K, AKT, p-PI3K, and p-AKT. eNOS activator-1 reduces oxidative stress levels by decreasing lipid peroxidation and restoring antioxidant enzyme activities. eNOS activator-1 upregulates the expression of tight junction proteins ZO-1 and occludin, increases Cav-1 expression, and inhibits MMP-9-mediated blood-brain barrier disruption. eNOS activator-1 can be used in the research of ischemic stroke .
Art. -Nr.: HY-189470
Forschungsgebiete:
Nav1.2-IN-4 is a blood-brain barrier-penetrant NaV1.2 inhibitor (IC50 = 31.21 μM). Nav1.2-IN-4 preferentially blocks the inactivated state of the neuronal voltage-gated sodium channel NaV1.2, inhibiting persistent and resurgent sodium currents associated with epileptogenesis. Nav1.2-IN-4 restores the GABA-glutamate balance by enhancing GABA and reducing glutamate. Nav1.2-IN-4 reduces oxidative stress in brain tissue by increasing GSH and decreasing MDA. Nav1.2-IN-4 protects mice against MES-induced tonic hindlimb extensor seizures and attenuates hippocampal neuronal degeneration in the PTZ kindling model. Nav1.2-IN-4 can be used for research on epilepsy .
Forschungsgebiete:
3-Bromocarbazole is an inhibitor of the aryl hydrocarbon receptor (AHR). 3-Bromocarbazole induces the mRNA expression of CYP1A1 and CYP1B1, with EC50 values of 2500 nM and 1100 nM, respectively. 3-Bromocarbazole inhibits motor neuron axon length by downregulating the mRNA transcription levels of α1-tubulin, Gap43, Syn2a and shha in zebrafish larvae. 3-Bromocarbazole reduces central nervous system neurogenesis by downregulating the mRNA transcription levels of elavl3, nrd, mbp and gfap in zebrafish larvae. 3-Bromocarbazole induces developmental neurotoxicity and decreases body length in zebrafish larvae or embryos; at high concentrations, it also reduces hatching rate, and increases mortality and malformation rate. 3-Bromocarbazole can be used in studies related to developmental neurotoxicity and breast cancer .
Forschungsgebiete:
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
Art. -Nr.: HY-B0011AR
CAS. Nr.: 148408-66-6
Synonyms: RP-56976 Trihydrate (Standard)
Forschungsgebiete:
Docetaxel Trihydrate (Standard) (RP-56976 Trihydrate (Standard)) is the analytical standard of Docetaxel Trihydrate (HY-B0011A). This product is intended for research and analytical applications. Docetaxel Trihydrate (RP-56976 Trihydrate) is an orally active tubulin stabilizer with antitumor activity. Docetaxel Trihydrate is a P-glycoprotein substrate and is metabolized by CYP3A to inactive products. Docetaxel Trihydrate binds tubulin, promotes tubulin polymerization, and inhibits microtubule depolymerization. Docetaxel Trihydrate induces aberrant mitosis followed by necrotic-like cell death at low concentrations, and induces G2/M mitotic arrest and drives apoptosis at high concentrations. Docetaxel Trihydrate induces renal injury/renal alterations, sex-dependent granule toxicity/uptake, low cardiac delivery, and decreased hepatic SOD/increased catalase/hepatotoxicity. Docetaxel Trihydrate can be used in cancer-related research .
Art. -Nr.: HY-B0011AS
Synonyms: RP-56976-d5 trihydrate
Forschungsgebiete:
Docetaxel-d5 trihydrate (RP-56976-d5 trihydrate) is the deuterated-labeled Docetaxel trihydrate (HY-B0011A). Docetaxel Trihydrate (RP-56976 Trihydrate) is an orally active tubulin stabilizer with antitumor activity. Docetaxel Trihydrate is a P-glycoprotein substrate and is metabolized by CYP3A to inactive products. Docetaxel Trihydrate binds tubulin, promotes tubulin polymerization, and inhibits microtubule depolymerization. Docetaxel Trihydrate induces aberrant mitosis followed by necrotic-like cell death at low concentrations, and induces G2/M mitotic arrest and drives apoptosis at high concentrations. Docetaxel Trihydrate induces renal injury/renal alterations, sex-dependent granule toxicity/uptake, low cardiac delivery, and decreased hepatic SOD/increased catalase/hepatotoxicity. Docetaxel Trihydrate can be used in cancer-related research .
Art. -Nr.: HY-B0426A
CAS. Nr.: 140462-76-6
Synonyms: ALO4943A; KW4679
Target:
Forschungsgebiete:
Infection Neurological Disease Metabolic Disease Inflammation/Immunology
Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 + and CD8 + T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .
Art. -Nr.: HY-D3144
CAS. Nr.: 2713577-11-6
Target:
Forschungsgebiete:
RhBIV is a thermosensitive rhodamine B (RhB)-derived fluorescent probe that fluorescently labels cellular mitochondria and detects mitochondrial temperature in vitro and in vivo. RhBIV contains a quaternized rhodamine B core, which confers a positive charge for binding to the negatively charged mitochondrial membrane, and an ortho-substituted electron-donating piperidine group; at lower temperatures, RhBIV forms an unstable ion pair form under kinetic control and exhibits strong fluorescence, whereas elevated temperature disrupts or partially interrupts the ion pair form, favoring formation of the conjugated RhBV form and leading to loss of fluorescence. RhBIV exhibits decreased fluorescence responsiveness with increasing temperature over the range of 20-42°C. RhBIV enables biological imaging of cells and mice, mitochondrial thermogenesis imaging, dynamic observation in mitochondrial thermogenesis imaging experiments, and non-invasive imaging of mitochondrial function in living animals (Ex/Em = 520/592 nm) .
Art. -Nr.: HY-D3525
Target:
Forschungsgebiete:
BDL-E5 is a fluorescent probe for detecting live induced pluripotent stem cells at the early reprogramming stage. Its detection mechanism involves specific binding to authentic reprogramming cells, which exhibit increased expression of pluripotency and epithelial genes and decreased expression of mesenchymal genes compared to non-reprogramming cells; it appears to co-localize more significantly with the Golgi complex than other organelle markers in reprogramming cells, and it does not require washing after staining to reduce background signals; fluorescence is generated upon binding to these early reprogramming cells, with positive cells appearing 7 days before iPS colonies are visible and stain positive for the conventional pluripotent marker TRA-1-60, and sorting BDL-E5-positive cells enriches populations that generate higher numbers and quality of iPS colonies. Its detection wavelength is Ex/Em = 578/599 nm .
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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
