Scientific Reviews
Product Guides
Blogs
Topics
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
6719 Results for "
Blocker
" in MedChemExpress (MCE) Product Catalog:
Products (6719)
6719 Results for "Blocker" in MCE Product Catalog:
Cat. No.: HY-P990269
Target:
Research Areas:
Cat. No.: HY-P990270
Target:
Research Areas:
Cat. No.: HY-P992056
Cat. No.: HY-P992076
Cat. No.: HY-L929
2,527 compounds
In drug discovery and development (R&D) area, target binding and druggability optimization are core processes. Among these attributes, high solubility is critical for a compound to achieve druggability, as it directly impacts the progress of drug R&D. Superior solubility ensures the rapid dissolution and uniform distribution of drug molecules in vivo, thereby enhancing bioavailability and effectively mitigating issues such as suboptimal efficacy, increased dosage requirements, or exacerbated toxic and side effects arising from insufficient solubility.
From the perspective of medicinal chemistry, high-solubility drug fragments serve as high-quality "molecular building blocks". Based on these fragments, lead compounds with potential druggability can be rapidly screened out, which significantly shortens the drug R&D cycle and reduces R&D costs. Meanwhile, the high-solubility drug fragment library can provide diverse options for drug development in different therapeutic areas, offer solutions for the solubility defects of existing clinical drugs, and facilitate the development of novel, highly effective targeted drugs with higher bioavailability and better safety profiles.
MCE has collected and compiled 2,527 experimentally validated small-molecule fragments with high solubility. These fragments can be directly used for drug molecular design, providing high-quality pre-validated solubility fragments that significantly improve the efficiency of lead compound screening and accelerate the progress of drug R&D.
Synonyms: (9S,13R)-12-OPDA
Cat. No.: HY-153552
CAS No.: 2758337-19-6
NH2-UAMC1110 is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose-response, and has been used for tumor diagnosis. NH2-UAMC1110 introduces an active amino group into its structure, enabling it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.), thereby synthesizing molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling processes. Its key activity is high targeting and high affinity, and its core function is to be coupled with bifunctional chelators (such as DOTA, DATA5m) as a targeting module. NH2-UAMC1110 can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis .
NH2-UAMC1110 TFA is an aminobutoxy derivative of the fibroblast activation protein (FAP) inhibitor UAMC1110 (HY-100684), and is a precursor compound for the synthesis of FAP inhibitor probes, not directly used in bioactivity experiments. For example, NH2-UAMC1110 TFA is involved in the synthesis of the radiotracer FAPI-QS, which exhibits high tumor selectivity and high dose effect, and has been used in tumor diagnosis. NH2-UAMC1110 TFA structurally incorporates an active amino group, allowing it to form covalent bonds with various molecules (such as DOTA, DATA5m, radionuclide chelators, etc.) to synthesize molecular imaging probes or targeted compounds with the ability to target FAP. NH2-UAMC1110 TFA specifically binds to the FAP active site, inhibiting its proline-selective serine protease activity (including dipeptidyl peptidase and endopeptidase activity), blocking FAP-mediated tissue remodeling-related processes. Its key activity is high targeting and high affinity, and its core function is to act as a targeting module coupled with bifunctional chelators (such as DOTA, DATA5m). NH2-UAMC1110 TFA can be applied to diagnostic imaging studies of tumors expressing FAP (such as colorectal cancer, pancreatic cancer, etc.), and also provides molecular tools for targeted research of FAP-related diseases with high FAP expression, such as fibrosis and arthritis .
Cat. No.: HY-178172
Research Areas:
AF9/ENL-DOT1L/AF4 PPI-IN-1 is a potent AF9/ENL and histone methyltransferase DOT1L/AF4 protein-protein interactions (PPI) inhibitor. AF9/ENL-DOT1L/AF4 PPI-IN-1 can inhibit the AF9-DOT1L (IC50 = 1.5 μM), AF9-AF4 (IC50 = 1 μM), ENL-AF4 (IC50 = 1.2 μM) interactions. AF9/ENL-DOT1L/AF4 PPI-IN-1 can suppress the expression of Mixed lineage leukemia (MLL) target genes Myc and Meis1 and selectively block the proliferation of MLL-r and several other leukemia cells. AF9/ENL-DOT1L/AF4 PPI-IN-1 exhibits significant antitumor activities in a mouse model of MLL-r leukemia without overt toxicities. AF9/ENL-DOT1L/AF4 PPI-IN-1 can be used for the study of MLL-r leukemia .
Cat. No.: HY-N2259R
CAS No.: 19431-84-6
Synonyms: (+)-Curcumenol (Standard)
Cat. No.: HY-P990171
Target:
Research Areas:
Cat. No.: HY-P990172
Target:
Research Areas:
Cat. No.: HY-P990252
Target:
Research Areas:
Cat. No.: HY-P99145A
Target:
Research Areas:
Cat. No.: HY-L940
5,818 compounds
Owing to the widespread transmission and frequent mutation of viral diseases, as well as the continuous emergence of new viruses and drug-resistant strains, antiviral drug development is facing increasingly stringent requirements. Antiviral compound libraries serve as important tools for drug screening, mechanism research and development, enabling the discovery and investigation of various antiviral drugs.
These compounds act through diverse antiviral mechanisms, targeting key steps in viral replication, assembly and invasion. They exert antiviral effects by inhibiting viral nucleic acid synthesis, blocking viral protein processing, and preventing viral binding to host cells. This library covers various types of antiviral compounds, including nucleosides, non-nucleosides, protease inhibitors and integrase inhibitors. It supports research on influenza virus, herpes virus, hepatitis virus, emerging respiratory viruses and other pathogens, and enables high-throughput screening of novel antiviral candidates to rapidly identify potential active compounds against diverse viruses. It also facilitates mechanistic studies to elucidate drug-target interactions and viral resistance mechanisms, and supports the screening of effective compounds against mutant strains for research on viral variation and drug resistance.
This antiviral library consists of 6,804 compounds with lead-like physicochemical properties. The core sources of the compounds include analogs of known antiviral molecues with a similarity score ≥ 0.6. MCE has collected more than 1450 antiviral molecules. As a small-molecule collection with both activity potential and structural modifiability, it provides strong support for antiviral drug research and development.
Cat. No.: HY-123996
CAS No.: 20041-64-9
Research Areas:
3-Ethoxy-5,6-dibromosalicylaldehyde is an IRE1/ERN1 inhibitor, with an IC50 of 0.12 μM, a Ki of 71-88 nM, and a Kd of 100 nM against the ribonuclease activity of hIRE1α, as well as an IC50 of 4.8 μM against yeast Ire1. It shows selectivity toward IRE1 ribonuclease. 3-Ethoxy-5,6-dibromosalicylaldehyde blocks the IRE1/ERN1-mediated unfolded protein response (UPR) signaling pathway, including XBP-1 mRNA splicing, induction of XBP1 target genes, and activation of MAPK8/9/10, but does not alter the phosphorylation level of IRE1α or the PERK/ATF6 pathway. 3-Ethoxy-5,6-dibromosalicylaldehyde inhibits chikungunya virus replication, induces growth arrest, apoptosis and clonogenic inhibition in pancreatic cancer cells, reduces FB1 (Fumonisin B1) (HY-N6719)-induced autophagy and cell death, regulates PGG-induced senescence and apoptosis, and alleviates Sorafenib (HY-10201)-induced vacuolization and damage in hepatic stellate cells. 3-Ethoxy-5,6-dibromosalicylaldehyde can be used in research related to chikungunya virus infection, pancreatic cancer, FB1-induced nephrotoxicity, liver cancer, breast cancer, lung cancer and liver fibrosis .
Cat. No.: HY-N16980
CAS No.: 2292113-33-6
Target:
Cat. No.: HY-D3117
CAS No.: 2146114-18-1
Target:
Research Areas:
MBCB is a two-photon Fluorescent probe for dual-detection of mitochondrial SO₂ derivatives and viscosity. For SO₂ derivatives detection, the probe utilizes a Michael addition mechanism: nucleophilic addition of SO₂ derivatives to the C=C bond between the carbazole skeleton and 3-methylbenzothiazolium moiety destroys the strong intramolecular charge transfer (ICT) system between these groups, while enhancing the weak ICT system between the benzothiazole group and carbazole framework; this causes the red emission at 600 nm to decrease and the blue emission at 434 nm to increase, creating a ratiometric response based on the I₄₃₄ₙₘ/I₆₀₀ₙₘ intensity ratio. For viscosity detection, in low-viscosity environments, steric hindrance creates a twisted ICT (TICT) system with weak fluorescence, while in high-viscosity environments, intramolecular rotation is blocked, the TICT state is disrupted, and the strong ICT system is recovered, leading to a strong red emission at 567 nm with negligible change to the short-wavelength emission at 415 nm, creating a ratiometric response based on the I₅₆₇ₙₘ/I₄₁₅ₙₘ intensity ratio that has a logarithmic linear relationship with viscosity. The probe has excitation/emission wavelengths of Ex/Em = 351/434, 600 nm for SO₂ derivatives detection and Ex/Em = 351/567 nm for viscosity detection, with two-photon excitation at 740 nm for bioimaging; it also exhibits good mitochondrial targeting ability with a Pearson's colocalization coefficient of 0.93 when paired with Mito-Tracker Green. The probe shows high sensitivity and selectivity for SO₂ derivatives, has low cell cytotoxicity, and can be applied to detect exogenous/endogenous HSO₃⁻ in living cells and in vivo, as well as visualize mitochondrial viscosity changes induced by nystatin[1].
Cat. No.: HY-118828AS
CAS No.: 2692624-08-9
Synonyms: (9S,13R)-12-OPDA-d5
Target:
Isotope-Labeled Compounds Lipoxygenase PGE synthase Keap1-Nrf2 IKK NF-κB NO Synthase Interleukin Related
Research Areas:
(9S,13R)-12-Oxo phytodienoic acid-d5 ((9S,13R)-12-OPDA-d5) is the deuterated-labeled (9S,13R)-12-Oxo phytodienoic acid (HY-118828A). (9S,13R)-12-Oxo phytodienoic acid ((9S,13R)-12-OPDA) is a mPGES-1 inhibitor and Nrf2 activator. (9S,13R)-12-Oxo phytodienoic acid selectively inhibits mPGES-1 expression and reduces inducible PGE2 production without affecting COX-1 or COX-2. (9S,13R)-12-Oxo phytodienoic acid inhibits the phosphorylation of IKKβ, IκBα, and NF-κB (p65), blocks the nuclear translocation of p65, increases the nuclear translocation of Nrf2, and upregulates HO-1 expression. (9S,13R)-12-Oxo phytodienoic acid inhibits the differentiation of M0 macrophages toward the M1 phenotype and promotes differentiation toward the M2 phenotype. (9S,13R)-12-Oxo phytodienoic acid decreases the levels of NO, PGE2, IL-1β, IL-6, iNOS, and PGD2. (9S,13R)-12-Oxo phytodienoic acid can be used for inflammation research .
-
-
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
