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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
571 Results for "
low selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (571)
571 Results for "low selectivity" in MCE Product Catalog:
Cat. No.: HY-B0696S1
Synonyms: NO050328-d4; NO328-d4; TGB-d4
Cat. No.: HY-B1398S
CAS No.: 1329792-51-9
Synonyms: 4-Aminoantipyrine-d3
Research Areas:
Ampyrone-d3 is the deuterium labeled Ampyrone (HY-B1398). Ampyrone (4-Aminophenazone; 4-Aminoantipyrine) is a reversible and low-damage optical clearing agent and non-selective COX inhibitor based on UV absorption properties. Ampyrone can improve the optical transmittance of mouse skin and other tissues. Ampyrone can induce tissue refractive index matching by enhancing UV absorption, reduce light scattering, and achieve tissue transparency in vivo. Ampyrone reduces the synthesis of prostaglandin PGE2, thereby exerting anti-inflammatory, analgesic and antipyretic effects. Ampyrone inhibits DNA damage, cell apoptosis and immune cell phagocytosis induced by Doxorubicin (HY-15142A) and Cisplatin (HY-17394), etc., and participates in the regulation of toxicity in tumor chemotherapy .
Cat. No.: HY-D3614
CAS No.: 2890606-81-0
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ERβ-targeted NIR probe P5 is an ERβ-selective fluorescent probe that binds preferentially to ERβ over ERα, enabling near-infrared fluorescence imaging of ERβ in living cells and in vivo. ERβ-targeted NIR probe P5 supports measurement of ERβ diffusion coefficient via fluorescence recovery after photobleaching. ERβ-targeted NIR probe P5 shows low cytotoxicity across multiple cell types, preserves ERβ expression, accumulates at ERβ-overexpressing tumor sites in vivo, and exhibits minimal fluorescence fluctuation across varied pH and cellular analyte conditions. ERβ-targeted NIR probe P5 can be used for the research of prostate cancer .
Cat. No.: HY-N0667S
CAS No.: 1217464-18-0
Cat. No.: HY-N0667S7
CAS No.: 781596-75-6
Synonyms: (-)-Asparagine-13C4,15N2; Asn-13C4,15N2; Asparamide-13C4,15N2
Cat. No.: HY-P5640
CAS No.: 179264-81-4
Cat. No.: HY-W017443S
CAS No.: 202406-87-9
Cat. No.: HY-W017443S2
CAS No.: 2483829-30-5
Cat. No.: HY-W017443S3
Cat. No.: HY-W017443S4
CAS No.: 768348-44-3
Synonyms: (-)-Asparagine-13C4; Asn-13C4; Asparamide-13C4
Cat. No.: HY-L110
100 compounds
Cyclic peptides are polypeptide chains taking cyclic ring structure, which exhibit diverse biological activities, such as antibacterial activity, immunosuppressive activity and anti-tumor activity. Cyclic peptides, with the features of good binding affinity, target selectivity and low toxicity, show great success as therapeutics. Multiple cyclic peptides are currently in clinical use, for examples, gramicidin and tyrocidine with bactericidal activity, cyclosporin A with immunosuppressive activity, and vancomycin with antibacterial activity. Furthermore, cyclic peptides usually have the sufficient size and a balanced conformational flexibility/rigidity for binding to flat protein-protein interaction (PPI) interfaces, which have potential to develop PPI drugs.
MCE offers a unique collection of 100 cyclic peptides, all of which have good bioactivities. MCE Cyclic Peptide Library is a powerful tool for drug discovery and PPI inhibitor screening.
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D3/5-HT receptor modulator-1 (compound 5i) is a selective dopamine D3 receptor and 5-HT2A receptor antagonist and a partial 5-HT1A receptor agonist. D3/5-HT receptor modulator-1 shows Ki values of 4.5 nM, 11.9 nM, and 15.3 nM for dopamine D3, 5-HT2A, and 5-HT2A receptors. D3/5-HT receptor modulator-1 has a low affinity for dopamine D2 receptors, 5-HT2C receptors, and hERG channels. D3/5-HT receptor modulator-1 has an atypical antipsychotic profile .
Cat. No.: HY-134092
CAS No.: 131391-65-6
Synonyms: N-Methyl-LTC4
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N-Methyl Leukotriene C4 (N-Methyl-LTC4) is a non-metabolizable LTC4 analog and a selective cysteinyl leukotriene receptor 2 (CysLT2) agonist, with an EC50 of 46.1 nM for mouse CysLT2 and an EC50 value of 122.3 nM for human CysLT2. N-Methyl Leukotriene C4 shows low potency against CysLT1. N-Methyl Leukotriene C4 activates human and mouse CysLT2 receptors, triggering calcium signaling, β-arrestin-2 binding to phosphorylated receptors, vascular leakage, hypotension, tachycardia, contraction of guinea pig ileum and trachea, mild bronchoconstriction, as well as hypertension associated with peripheral vasoconstriction. N-Methyl Leukotriene C4 can be used in research on asthma, rhinitis, sinusitis, cerebral inflammation and edema, pulmonary arterial hypertension, and cardiovascular diseases .
Cat. No.: HY-13590
CAS No.: 402857-58-3
CEP-7055 (compound 21) is a novel vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase inhibitor with potent inhibitory activity. Studies have found that the inhibitor activity can be significantly improved by optimizing the R9 substituent. Compound 21 has potent low nanomolar inhibition of human VEGF-R tyrosine kinase and shows good selectivity against multiple tyrosine and serine/threonine kinases. N,N-dimethylglycine ester 40 was prepared to improve its water solubility and oral bioavailability. In animal pharmacokinetic studies, a significant increase in the plasma level of 21 was observed after oral administration of 40. Compound 21 showed significant in vivo antitumor activity in multiple tumor models and has entered phase I clinical trials as a water-soluble N,N-dimethylglycine ester proagent of 40 (CEP-7055).
Cat. No.: HY-15334
CAS No.: 402857-39-0
CEP-5214, derived from a new indenopyrrolocarbazole template, is a potent inhibitor of vascular endothelial growth factor R2 (VEGF-R2) tyrosine kinase. Structurally, it features optimal substitutions at positions 9 (ethoxymethyl) and 12 (hydroxypropyl) on the indeno[2,1-a]pyrrolo[3,4-c]carbazole-5-one scaffold, leading to high potency against VEGF-R2 (IC50 8 nM). Compound 21 (CEP-5214) exhibits low-nanomolar inhibition of human VEGF-R tyrosine kinases (IC50 4 nM for VEGF-R2/KDR), with good selectivity over other kinases. The compound demonstrated significant cellular and in vivo antitumor activity across various models and advanced into phase I clinical trials as a water-soluble prodrug (CEP-7055) to enhance oral bioavailability .
Cat. No.: HY-184964
CAS No.: 3041997-77-4
Research Areas:
NF-κB-IN-22 is an inhibitor targeting IKKβ, IκBα and NF-κB p65. NF-κB-IN-22 selectively inhibits the proliferation, migration and invasion of various cancer cells, arrests the cell cycle, and suppresses tumor growth in vivo, while exhibiting low toxicity to normal cells. NF-κB-IN-22 induces DNA damage, ROS production and apoptosis through endoplasmic reticulum stress and mitochondrial apoptotic pathways. NF-κB-IN-22 inhibits the phosphorylation of IKKβ, IκBα and NF-κB p65, blocks the NF-κB signaling pathway, and suppresses the nuclear translocation of NF-κB p65. NF-κB-IN-22 reverses the resistance to cisplatin (HY-17394). NF-κB-IN-22 can be used in research related to lung cancer, gastric cancer and liver cancer .
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Ampyrone (4-Aminophenazone) (Standard) is the analytical standard of Ampyrone (HY-B1398). This product is intended for research and analytical applications. Ampyrone (4-Aminophenazone; 4-Aminoantipyrine) is a reversible and low-damage optical clearing agent and non-selective COX inhibitor based on UV absorption properties. Ampyrone can improve the optical transmittance of mouse skin and other tissues. Ampyrone can induce tissue refractive index matching by enhancing UV absorption, reduce light scattering, and achieve tissue transparency in vivo. Ampyrone reduces the synthesis of prostaglandin PGE2, thereby exerting anti-inflammatory, analgesic and antipyretic effects. Ampyrone inhibits DNA damage, cell apoptosis and immune cell phagocytosis induced by Doxorubicin (HY-15142A) and Cisplatin (HY-17394), etc., and participates in the regulation of toxicity in tumor chemotherapy .
Cat. No.: HY-N19899
CAS No.: 910050-51-0
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Cat. No.: HY-P991959
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Cat. No.: HY-135283
CAS No.: 212481-66-8
Synonyms: A-216546
Target:
Endothelin Receptor NOD-like Receptor (NLR) Reactive Oxygen Species (ROS) Pyroptosis Interleukin Related
Research Areas:
ABT-546 (A-216546) is an orally active ETA receptor antagonist, with Ki values of 0.46 nM and 13000 nM for human ETA and ETB receptors, respectively, and exhibits >25000-fold selectivity over the ETB receptor. ABT-546 effectively inhibits ET-1 (HY-P0202)-induced phosphoinositide hydrolysis (IC50 = 0.59 nM) and arachidonic acid release (IC50 = 3.03 nM), and antagonizes ET-1-induced contraction in isolated vascular rings. ABT-546 crosses the placental barrier but shows extremely low fetal exposure, with a favorable safety profile. ABT-546 inhibits ET-1-induced pressor response and downregulates the NLRP3/ROS/GSDMD-mediated pyroptosis pathway. ABT-546 can be used for research on abdominal aortic aneurysm .
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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
