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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
3056 Results for "
modulating
" in MedChemExpress (MCE) Product Catalog:
Products (3056)
3056 Results for "modulating" in MCE Product Catalog:
Synonyms: 9α-Fludrocortisone (Standard); 9α-Fluorcortisol (Standard)
Research Areas:
Fludrocortisone (Standard) (9α-Fludrocortisone (Standard)) is the analytical standard of Fludrocortisone (HY-B1203). This product is intended for research and analytical applications. Fludrocortisone is an orally active mineralocorticoid and glucocorticoid receptor agonist. Fludrocortisone suppresses pro-inflammatory cytokine expression, reduces CCL2, IL-6, IL-8 levels, upregulates mineralocorticoid receptor (MR) expression, induces PI3K/Akt, GSK-3β, CREB, ERK1/2, mTOR phosphorylation, blocks Tau hyperphosphorylation, prevents apoptosis, promotes survival and proliferation, enhances renal sodium and water transport, increases plasma volume and blood pressure, reduces plasma potassium and renin activity, stimulates erythropoietin expression, modulates uterine receptivity genes, and reverses PP242-induced MUC1 upregulation. Fludrocortisone can be used for the research of congenital adrenal hyperplasia, postural hypotension, and adrenal insufficiency.
Cat. No.: HY-B1203S
Synonyms: 9α-Fludrocortisone-d5; 9α-Fluorcortisol-d5
Cat. No.: HY-B1203S1
Synonyms: 9α-Fludrocortisone-d2; 9α-Fluorcortisol-d2
Category:
Cat. No.: HY-N1989
CAS No.: 11028-00-5
Cat. No.: HY-N2492R
CAS No.: 19367-38-5
Synonyms: Methyl trans-p-coumarate (Standard)
Cat. No.: HY-P1889
CAS No.: 721885-31-0
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Bim BH3, Peptide IV is an Aβ42-binding peptide and the pro-apoptotic BH3 domain of the BIM protein. Bim BH3, Peptide IV binds Aβ42 with a Kd of 7.1 μM. Bim BH3, Peptide IV modulates Aβ42 structure, fibrillization pathways, aggregate morphology, and membrane interactions, inhibiting fibril formation while enhancing protofibril assembly. Bim BH3, Peptide IV promotes Aβ42 β-sheet formation and accelerates aggregation. Bim BH3, Peptide IV enhances Aβ42 membrane internalization and bilayer stiffening. Bim BH3, Peptide IV induces neuronal cell death by enhancing BH3-induced membrane interactions of Aβ42 prefibrillar species. Bim BH3, Peptide IV can be used for research on Alzheimer's disease .
Cat. No.: HY-P992072
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Cat. No.: HY-W014316R
CAS No.: 30007-47-7
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5-Bromo-5-nitro-1,3-dioxane (Standard) is the analytical standard of 5-Bromo-5-nitro-1,3-dioxane (HY-W014316). This product is intended for research and analytical applications. 5-Bromo-5-nitro-1,3-dioxane is a broad-spectrum antimicrobial agent active against Gram-positive bacteria, Gram-negative bacteria and fungi. 5-Bromo-5-nitro-1,3-dioxane oxidizes free thiol groups to their corresponding disulfides. 5-Bromo-5-nitro-1,3-dioxane induces intracellular substance leakage in Escherichia coli and Staphylococcus aureus. 5-Bromo-5-nitro-1,3-dioxane modulates the oxygen consumption of Escherichia coli and Staphylococcus aureus .
Cat. No.: HY-W049881
CAS No.: 2521-07-5
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9-Methyl-β-carboline is a monoamine oxidase inhibitor and dopaminergic modulator, with an IC50 of 1 μM against human MAO-A and an IC50 of 15.5 μM against human MAO-B. 9-Methyl-β-carboline possesses cognitive enhancement potential and can cross the blood-brain barrier. 9-Methyl-β-carboline increases dopamine levels by inhibiting monoamine oxidase activity and microglial proliferation. 9-Methyl-β-carboline activates PKA/PKC and mitochondrial respiratory chain complex I, promotes neurotrophic factor expression and reduces α-synuclein (α-synuclein) levels, thereby reversing neurotoxin-induced dopaminergic neuron damage. 9-Methyl-β-carboline also regulates the PI3K pathway and exerts an anti-proliferative effect on astrocytes. 9-Methyl-β-carboline is widely used in Parkinson's disease-related studies .
Cat. No.: HY-W680886
CAS No.: 152623-93-3
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6-APDB is a class of monoamine neurotransmitter releaser and Monoamine Transporter modulator that exerts selective effects on human monoamine transporters and acts as a partial agonist at 5-HT2 family receptors. For NET, 6-APDB has an IC50 of 0.56 μM and a Ki of 18 μM; for SERT, it has an IC50 of 2.3 μM and a Ki of 23 μM; for DAT, it has an IC50 of 33 μM and a Ki of >30 μM, and affinity for rat and mouse TAAR1, with Ki values of 1.0 μM and 0.21 μM, respectively. 6-APDB inhibits norepinephrine and 5-HT reuptake, mediates the release of three types of monoamine neurotransmitters, shows a dose-dependent biphasic locomotor effect in mice, and fully substitutes the discriminative stimulus effect of MDMA. 6-APDB shows no significant cytotoxicity at high concentrations, and possesses empathogenic psychoactivity, potential hallucinogenic effects, and behavioral effects associated with intermittent abuse .
Cat. No.: HY-L050
507 compounds
Protein ubiquitination is an enzymatic post-translational modification in which an ubiquitin protein is attached to a substrate protein. Ubiquitination involves three main steps: activation, conjugation, and ligation, performed by ubiquitin-activating enzymes (E1s), ubiquitin-conjugating enzymes (E2s), and ubiquitin ligases (E3s), respectively. Ubiquitination affects cellular processes such as apoptosis, cell cycle, DNA damage repair, and membrane transportation, etc. by regulating the degradation of proteins (via the proteasome and lysosome), altering the cellular localization of proteins, affecting proteins activity, and promoting or preventing protein-protein interactions. Deregulation of ubiquitin pathway leads to many diseases such as neurodegeneration, cancer, infection and immunity, etc.
MCE offers a unique collection of 507 small molecule modulators with biological activity used for ubiquitination research. Compounds in this library target the key enzymes in ubiquitin pathway. MCE Ubiquitination Compound Library is a useful tool for the research of ubiquitination regulation and the corresponding diseases.
Cat. No.: HY-L063
282 compounds
Chemical probes are simply reagents with high potency, selectivity and cell-permeability which play important roles in both fundamental and applied biological research. In their most common application, chemical probes can establish the tractability of a specific target. They are used to interrogate the relationship between a target and its phenotype (biological tractability) as well as an ability to modulate that phenotype using a small molecule. Otherwise, chemical probes also have had a major impact in enabling and accelerating discoveries along the path to pioneer medicines. They have helped to improve the understanding of targets and pathways and have created opportunities for proprietary drug discovery efforts to an extent that would not have been possible otherwise.
MCE provides a unique collection of 282 chemical probes with high potency (at least 100 nM potency), selectivity (at least 10-fold selectivity against any other target) and cell-permeability (at least 10 μM potency). MCE Chemical probe library is a useful tool for target identification and mechanism research.
Cat. No.: HY-D0485
CAS No.: 12224-02-1
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Fluorescent brightener 24 is a stilbene-type fluorescent brightener and fading regulator .
Cat. No.: HY-103430
CAS No.: 108179-91-5
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SKF-83566 hydrobromide is an orally active, blood-brain barrier-permeable D1/D5 dopamine receptor antagonist with a Ki value of approximately 0.4-0.56 nM.
SKF-83566 hydrobromide modulates locomotor behavior and spatial memory by blocking D1 receptors and inhibits glioblastoma progression by targeting the DRD1/c-Myc/UHRF1 pathway.
SKF-83566 hydrobromide acts as an inhibitor of the dopamine transporter (DAT) and adenylyl cyclase 2 (AC2).
SKF-83566 hydrobromide competitively binds to DAT to inhibit dopamine reuptake and non-competitively inhibits AC2 activity, thereby reducing cAMP accumulation.
SKF-83566 hydrobromide is used in research areas such as dopaminergic system mechanisms, learning and memory, targeted intervention for glioblastoma, AC2 pathophysiology, antiparasitic drug screening, and synaptic plasticity (the "gating effect") .
Cat. No.: HY-12502AR
CAS No.: 111011-76-8
Synonyms: NZ-105 hydrochloride monoethanolate (Standard); (±)-Efonidipine hydrochloride monoethanolate (Standard)
Research Areas:
Efonidipine (NZ-105) hydrochloride monoethanolate (Standard) is the analytical standard of Efonidipine hydrochloride monoethanolate (HY-12502AR). This product is intended for research and analytical applications. Efonidipine (NZ-105) hydrochloride monoethanolate 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 monoethanolate inhibits SARS-CoV-2 main protease. Efonidipine hydrochloride monoethanolate 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 monoethanolate reduces plasma aldosterone levels in vivo. Efonidipine hydrochloride monoethanolate 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 monoethanolate can be used for research in hypertension, heart failure, and disorders involving dysregulated steroid hormone synthesis .
YHO-13351 is an orally active ABCG2 inhibitor . YHO-13351 modulates the function of ABCG2, blocks BCRP-mediated compound efflux, downregulates the expression of breast cancer resistance protein at the post-transcriptional level, and reverses ABCG2-associated tolerance. YHO-13351 restores the toxicity of SN-38 to SN-38-resistant cancer cells and sensitizes cancer cells to Irinotecan. YHO-13351 is a water-soluble prodrug that is rapidly converted to YHO-13177 (HY-12757) in mice. YHO-13351 prolongs the median survival time of mice bearing cancer cell xenografts when combined with IMMU-132. YHO-13351 extends the survival time of tumor-bearing mice and inhibits the growth of xenograft tumors when combined with Irinotecan. YHO-13351 can be used for the research of breast cancer, gastric cancer, BCRP-mediated drug-resistant cancers, and cervical cancer .
Cat. No.: HY-16265A
CAS No.: 2514957-81-2
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JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
Cat. No.: HY-165587
CAS No.: 284464-83-1
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BM-573 is an orally active dual thromboxane A₂ (TXA₂) modulator with an IC50 of 1.3 nM. BM-573 possesses both thromboxane synthase (TxAS) inhibition and thromboxane receptor (TP) antagonistic effects. BM-573 can completely inhibit platelet aggregation induced by Arachidonic acid (HY-109590) or U-46619 (TXA₂ analogues). BM-573 completely blocks the generation of TXB₂ (the stable metabolite of TXA₂) in human platelets and does not inhibit cyclooxygenase (COX-1/COX-2), thus avoiding interference with other prostaglandin synthesis. BM-573 has an inhibitory effect on U-46619-induced contractions in rat gastric fundus smooth muscle (ED₅₀ = 4.2 μM), but has no effect on contractions caused by PGE₂, PGF₂α, or PGI₂. BM-573 can be used in the study of atherosclerosis, myocardial infarction, pulmonary hypertension and shock .
Cat. No.: HY-177797
CAS No.: 30439-19-1
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5-Methoxytryptoline acts as a modulator of the Serotonin transporter complex, as well as a ligand for the 5-HT2A and 5-HT2C receptors, with Ki values of 130 nM and 140 nM for the 5-HT2A and 5-HT2C receptors, respectively. 5-Methoxytryptoline inhibits the active uptake of Serotonin (HY-B1473A) and Tryptamine (HY-B2132) in platelets. 5-Methoxytryptoline induces behavioral excitation, cortical electroencephalographic desynchronization, and dose-dependent elevation of plasma prolactin, followed by behavioral sedation and partial recovery of cortical electroencephalographic voltage. 5-Methoxytryptoline antagonizes Reserpine (HY-N0480)-induced sedation, reduced locomotor activity, and hypothermia. 5-Methoxytryptoline exerts dose-dependent effects on behavior and cortical electroencephalographic activity in freely moving rats. 5-Methoxytryptoline can be used in depression-related research .
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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
