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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
431 Results for "
iBH3 profiling
" in MedChemExpress (MCE) Product Catalog:
Products (431)
431 Results for "iBH3 profiling" in MCE Product Catalog:
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-176287
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ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
Cat. No.: HY-177963
CAS No.: 2341941-41-9
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NV914 is an inhibitor of FTSJ1 (tryptophan tRNA-specific 2'-O-methyltransferase) that inhibits the methyltransferase activity of FTSJ1, induces translational readthrough of premature termination codons, and enables genes carrying nonsense mutations to synthesize full-length proteins. NV914 belongs to translational readthrough-inducing compounds (TRIDs). NV914 exhibits translational readthrough activity against nonsense mutations in in vitro systems, does not induce readthrough of natural termination codons, and restores CFTR protein expression. NV914 shows favorable acute oral tolerance in mice, with low health risks and good safety profiles. NV914 is applicable to research related to cystic fibrosis and Shwachman-Diamond syndrome [3].
Cat. No.: HY-179504
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PDE4B-IN-6 (compound 4i) is a potent and selective PDE4B inhibitor with an IC50 of 7.42 nM. PDE4B-IN-6 shows ~195- and ~169-fold selectivity for PDE4B over PDE4A (IC50 = 1540 nM) and PDE4C (IC50 = 1260 nM), respectively. PDE4B-IN-6 increases cAMP level and suppresses TNF-α expression. PDE4B-IN-6 shows favorable antioxidant profiles and low cytotoxicity. PDE4B-IN-6 can be used for chronic obstructive pulmonary disease (COPD) research .
Cat. No.: HY-180965
CAS No.: 3057939-64-4
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Pro-PEG3-BA is an EML4-ALK/EGFR PROTAC degrader, degrading EML4 ALK and EGFR mutant (L858R/T790M) with DC50 values of 0.42 and 13.50 μM, respectively. Pro-PEG3-BA hinders proliferation and induces cell cycle arrest and apoptosis of NSCLC cells in vitro. Pro-PEG3-BA shows safety profile and decreases EML4-ALK protein via rewiring the ubiquitin- proteasome system in vivo. Pro-PEG3-BA can be used for non-small cell lung cancer research [3].
Cat. No.: HY-180970
CAS No.: 2162120-55-8
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TD-004 is a potent ALK PROTAC degrader. TD-004 exhibits anti-ALK inhibitory activity with an IC50 of 0.11 µM and selectively inhibits the proliferation of SU-DHL-1 and H3122 cells (ALK-positive cancer cells) with IC50s of 0.058 µM and 0.28 µM, respectively. TD-004 induces degradation of ALK fusion proteins (NPM-ALK and EML4-ALK) via recruitment of the VHL E3 ligase and the proteasome pathway. TD-004 demonstrates significant tumor growth inhibition with a favorable safety profile in vivo. TD-004 can be used for the research of anaplastic large cell lymphoma and non-small cell lung cancer .
Cat. No.: HY-182014
CAS No.: 2408041-54-1
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TLC-2716 is an orally available, gut- and liver-restricted inhibitor against LXRα and LXRβ, with EC50 values of 7 nM and 15 nM, respectively. TLC-2716 represses LXRα/β transcriptional activity, downregulates genes involved in lipogenesis, lipid absorption and lipoprotein metabolism, and preserves peripheral reverse cholesterol transport. TLC-2716 reduces lipid accumulation, suppresses inflammation and fibrotic gene expression, enhances triglyceride-rich lipoprotein clearance, and improves glucose homeostasis and insulin sensitivity. TLC-2716 lowers serum and hepatic triglycerides, plasma cholesterol and other atherogenic lipid profiles in experimental models and humanized liver mice. TLC-2716 can be used for the research of dyslipidemia and related cardiometabolic disorders .
Cat. No.: HY-182244
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SERT/NET-IN-1 is a blood-brain barrier-permeable SERT and NET inhibitor, with an IC50 of 11.2 nM against human SERT and an IC50 of 32.0 nM against human NET. SERT/NET-IN-1 blocks 5-HT reuptake to enhance serotonergic signaling. SERT/NET-IN-1 also blocks norepinephrine reuptake to enhance central noradrenergic transmission and inhibits the ejaculatory reflex. SERT/NET-IN-1 prolongs ejaculatory latency, reduces ejaculation frequency and preserves sexual function. SERT/NET-IN-1 exhibits cross-species microsomal metabolic stability, shows acceptable oral brain exposure in rats, and has favorable safety profiles. SERT/NET-IN-1 can be used in studies related to premature ejaculation .
Cat. No.: HY-184292
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COX-2-IN-67 is an orally active, blood-brain barrier permeable multi-target inhibitor that potently targets COX-2 (IC50=0.07 μM), hCA IX (Ki=62.7 nM) and hBuChE (IC50=0.47 μM). COX-2-IN-67 alleviates oxidative stress and liver stress, improves glucose homeostasis and insulin sensitivity, and optimizes lipid profiles. Meanwhile, COX-2-IN-67 effectively reduces the levels of neuroinflammatory markers and improves hippocampus-dependent cognitive function in a high-fat diet-induced rat model. COX-2-IN-67 can be used for the research of metabolic dysfunction-associated mild cognitive impairment .
Cat. No.: HY-184652
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LRRK2/JNK3-IN-1 is a brain-penetrant multi-target inhibitor of LRRK2 (including G2019S mutant and wild-type) and JNK3, with enzymatic IC50 values of 3.90 nM against LRRK2 G2019S, 3.24 nM against wild-type LRRK2, and 22.1 nM against JNK3. LRRK2/JNK3-IN-1 displays favorable selectivity in a 97-kinase profiling screen, and also shows inhibitory activity against JNK1, JNK2, and MKNK2. LRRK2/JNK3-IN-1 can be used for the research of Parkinson's disease .
Cat. No.: HY-189393
CAS No.: 3089177-97-6
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RTY-406 is an orally active ABCB4/MDR3 and ABCB11/BSEP positive modulator. RTY-406 increases ABCB4/MDR3 and ABCB11/BSEP protein levels and functional output, elevates biliary phospholipid levels, enhances bile acid efflux, increases bile flow and micelle formation, reduces hepatic bile acids, and promotes cholesterol-to-bile-acid conversion. RTY-406 does not induce hepatocellular injury, maintains normal serum alanine transaminase and aspartate aminotransferase levels, and shows a favorable safety profile in cynomolgus monkeys. RTY-406 can be used for the research of primary sclerosing cholangitis and cholestasis .
Cat. No.: HY-D3198
CAS No.: 2351937-34-1
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NIR-fluorescent ceramide is a neutral near-infrared (NIF) fluorescent probe (λem=650 nm) based on the C-bridged nitrobenzoxadiazole SCOTfluor core, which enables visualization of lipid metabolic processes such as sphingolipid trafficking. The emission signal of NIR-fluorescent ceramide increases significantly in liposomal environments. NIR-fluorescent ceramide acts as an intracellular trafficking tracer, localizing to regions surrounding the endoplasmic reticulum and Golgi apparatus within a short period, and then translocating to recycling lysosomes over a longer period, thus enabling real-time visualization of sphingolipid trafficking and biological lipid functions in living cells. NIR-fluorescent ceramide also generates metabolic uptake profiles and provides multiple metabolic readouts in human cancer cell lines .
Cat. No.: HY-P0037
CAS No.: 136208-71-4
Synonyms: Org 30850ANT
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Cat. No.: HY-P11274
CAS No.: 3005889-81-3
Synonyms: Amycretin; NN 9487
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Cat. No.: HY-P11274A
Synonyms: Amycretin sodium; NN 9487 sodium
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Cat. No.: HY-P991015
CAS No.: 2921676-04-0
Synonyms: JNJ-78278343; KLCB-245
Cat. No.: HY-W766078
Synonyms: 1-b-D-Arabinofuranosyluracil-13C,15N2; Uracil 1-β-D-arabinofuranoside-13C,15N2
Cat. No.: HY-L219
58 compounds
Antimicrobial Peptides (AMPs), also known as antimicrobial peptides or antibiotic peptides, are a class of polypeptides encoded by specific genes in various biological cells and induced by external stimuli. They exhibit broad-spectrum bioactivity against bacteria, fungi, viruses, protozoa, and even tumor cells. AMPs serve as crucial effector molecules in the host's innate immune system.Due to their wide antimicrobial spectrum, low toxicity to normal cells of higher animals, high safety profile, low tendency to induce resistance, and additional benefits such as immune enhancement and antioxidant effects, antimicrobial peptides hold significant promise in new drug development.
MCE offers 58 types of antimicrobial peptides, which can be applied in high-throughput screening for research in anti-infection therapies, immunotherapy, anticancer drug development, and agricultural disease control.
Cat. No.: HY-L230
331 compounds
Kinases are enzymes that catalyze the addition of phosphate groups to substrate molecules, a process known as phosphorylation. Protein phosphorylation serves as a critical regulatory mechanism for numerous cellular processes, including cell division, metabolism, and signal transduction. The human genome encodes over 500 kinases, which collectively regulate approximately 50% of cellular functions. Due to their pivotal roles, kinases represent one of the most important target classes in drug development.
Kinase inhibitors can selectively block the activity of disease-associated kinases, making them valuable therapeutics for conditions such as cancer and inflammatory diseases. FDA-approved kinase inhibitors have undergone extensive preclinical and clinical studies, demonstrating high bioactivity, favorable safety profiles, and good bioavailability, rendering them suitable for investigating new therapeutic indications.
Cat. No.: HY-L261
167 compounds
MCE Classic FDA-Approved Drug Library features a curated selection of marketed drugs that have achieved the highest prescription volumes and greatest clinical impact in global practice since 2006. The collection covers eight major therapeutic areas, including cardiovascular diseases, oncology, metabolic disorders, infectious diseases, central nervous system disorders, respiratory diseases, digestive system diseases, and immunological conditions. All compounds have been validated through long‑term clinical use and possess well‑defined molecular targets, well‑established pharmacokinetic properties, quantifiable efficacy endpoints, and comprehensive toxicological safety profiles.
The library currently contains 167 representative drugs and is designed to serve as an efficient tool for drug repurposing, phenotypic screening, mechanism‑of‑action studies, and combination therapy strategy development.
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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
