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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
1349 Results for "
High Selectivity
" in MedChemExpress (MCE) Product Catalog:
Products (1349)
1349 Results for "High Selectivity" in MCE Product Catalog:
Target:
Research Areas:
α-Glucosidase, rice is a GH31 glycoside hydrolase in rice seeds, with high selectivity for α-1,4-glycosidic bonds. α-Glucosidase, rice can be inhibited by rice husk extracts (IC50 = 1.25 μg/mL) and steroidal components (IC50 = 1.83 μg/mL). α-Glucosidase, rice exists in two major isoforms, among which isoform II is more sensitive to inhibitors. α-Glucosidase, rice can directly bind to and degrade starch granules in rice seeds. α-Glucosidase, rice can form ONG2-I and ONG2-II via post-translational proteolysis. α-Glucosidase, rice can be used in type 2 diabetes research .
Cat. No.: HY-L180
655 compounds
Mitochondrial autophagy refers to the selective encapsulation and degradation of damaged mitochondria by cells through the autophagy mechanism, thereby maintaining mitochondrial and cellular homeostasis. The concept of mitochondrial autophagy has received extensive attention since it was proposed. Current studies have shown that the mechanisms of mitochondrial autophagy can generally be divided into two categories: Ubiquitin-dependent pathways and Ub-independent pathways. In addition, mitochondrial autophagy is a research hotspot related to the pathogenesis of neurodegenerative diseases, cardiovascular diseases, cancer, metabolic diseases and other clinical diseases. Therefore, high-throughput screening based on mitochondrial autophagy can effectively screen out compounds that are closely related to the occurrence of diseases and analyze their mechanisms.
MCE can provide a library of 655 mitophagy compounds, which can be used for drug development and mechanism research in cancer, immunity, infection and other hot research fields.
Cat. No.: HY-L033
370 compounds
Peptidomimetics are compounds whose essential elements (pharmacophore) mimic a natural peptide or protein in 3D space and which retain the ability to interact with the biological target and produce the same biological effect. Peptidomimetics are designed to circumvent some of the problems associated with a natural peptide: e.g. stability against proteolysis (duration of activity) and poor bioavailability. Certain other properties, such as receptor selectivity or potency, often can be substantially improved. The design and synthesis of peptidomimetics are most important because of the dominant position peptide and protein-protein interactions play in molecular recognition and signaling, especially in living systems. Hence mimics have great potential in drug discovery.
MCE Peptidomimetic Library contains 370 compounds including peptoid, α-helix mimetics, β-turn/sheets mimetics, etc. This library is an indispensable tool of structure-activity relationships in drug discovery.
Cat. No.: HY-118917
CAS No.: 297730-05-3
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VX-148 is an orally active immunosuppressant, which is a non-competitive inosine-5'-monophosphate dehydrogenase (IMPDH) inhibitor with Ki values for IMPDH Ⅱ and IMPDH Ⅰ of 6 and 14 nM respectively. VX-148 can significantly inhibit the proliferation of human peripheral blood mononuclear cells (PBMC) stimulated by T-cell mitogen (PHA) or B-cell mitogen (SPAS). VX-148 has high selectivity for lymphocytes (such as L1210, Jurkat T cells, and Raji B cells), but has no significant toxicity to non-lymphoid cells. VX-148 can inhibit antibody responses in mouse models and significantly prolong the survival time of transplanted skin in allogeneic skin transplantation models. VX-148 can be used in the research of autoimmune diseases (such as rheumatoid arthritis, psoriasis) and organ transplantation anti-rejection .
Cat. No.: HY-132893
CAS No.: 2830555-70-7
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AZ14145845 is an orally active dual-target type 1½ kinase inhibitor of Mer/Axl, which inhibits Mer kinase (pIC50 = 9.0) and Axl kinase (pIC50 = 7.9) with high selectivity over Flt3 and Tyro3. AZ14145845 suppresses Mer- and Axl-dependent proliferation in Ba/F3 cells and inhibits efferocytosis in macrophages. AZ14145845 reduces the phagocytosis of photoreceptor outer segments by polarized human retinal epithelial cells. AZ14145845 inhibits tumor growth and induces tumor regression in vivo, and its combination with anti-PD1 antibody and ionizing radiation improves the survival rate of mice with colorectal cancer. AZ14145845 causes retinal degeneration in mice, with pathological changes similar to those in MERTK loss-of-function models. AZ14145845 can be used in studies related to retinal degeneration, lymphoma and colorectal cancer .
Cat. No.: HY-13323B
CAS No.: 2101314-20-7
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CX-5461 hydrochloride is a selective, orally active RNA polymerase I inhibitor. CX-5461 hydrochloride disrupts the formation of the SL1-rDNA complex, thereby blocking the transcription initiation of ribosomal RNA without altering the activity of RNA polymerase II, DNA replication, or protein translation processes. CX-5461 hydrochloride upregulates the expression of p21, MDM2, Sestrin1/2, and phosphorylated AMPKα, and reduces the level of phosphorylated Akt. CX-5461 hydrochloride induces G2/G2/M cell cycle arrest, Autophagy, Apoptosis, and cellular senescence, and activates CHK1, CHK2, and RPA. CX-5461 hydrochloride can be used in research related to osteosarcoma, cervical cancer, hematologic malignancies, high-grade serous ovarian cancer, and solid tumors .
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TMDJ-035 is a high-affinity, selective RyR2 inhibitor with an EC50 of 0.0130 μM. TMDJ-035 reduces RyR2 protein expression without affecting action potential-induced Ca 2+ transients. TMDJ-035 decreases ATP content and intracellular Ca 2+ levels. TMDJ-035 inhibits arrhythmias in a CPVT mouse model carrying mutant RyR2s. TMDJ-035 has no effect on electrocardiogram parameters or cardiac systolic function. TMDJ-035 exacerbates heart failure in mouse myocardial infarction models and hypoxic cardiomyocytes by altering cardiac function, causing tissue damage, promoting inflammatory infiltration, collagen deposition, and changes in Myosin heavy chain/actin expression. TMDJ-035 can be used in studies related to heart failure, catecholaminergic polymorphic ventricular tachycardia, and arrhythmias .
Cat. No.: HY-150537
CAS No.: 2412364-73-7
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AChE/GSK-3β-IN-1 (compound GT15) is a potent, dual AChE/GSK-3β inhibitor with IC50 values of 1.2, 149.8 and 22.4 nM for hAChE , hBChE and hGSK-3β, respectively. AChE/GSK-3β-IN-1 penetrates the blood-brain barrier (BBB). AChE/GSK-3β-IN-1 has high kinase selectivity profiles for the CMGC kinase family. AChE/GSK-3β-IN-1 occupies the ATP binding site of DYRK1A. AChE/GSK-3β-IN-1 inhibits ROS expression and reduces oxidative stress. AChE/GSK-3β-IN-1 can be used for Alzheimer’s disease research .
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-173523
CAS No.: 3054009-82-1
KI-CDK9d-32 is a selective CDK9 PROTAC degrader (IC50 = 3 nM; DC50 = 0.89 nM). KI-CDK9d-32 induces CDK9 degradation via the ubiquitin-proteasome pathway to abrogates CDK9 enzymatic and scaffolding functions, downregulates MYC expression and MYC-dependent signaling, represses TNF-alpha signaling pathways activity and pre-rRNA levels. KI-CDK9d-32 disrupts nucleolar homeostasis, blocks cell cycle progression and cellular translation by reducing 4EBP1 phosphorylation, and elicits cancer cell cytotoxicity in a CRBN-dependent manner, while high ABCB1 activity attenuates the efficacy. KI-CDK9d-32 can be used for the research of acute lymphoblastic leukemia, rhabdomyosarcoma, pancreatic adenocarcinoma .
Cat. No.: HY-178958
CAS No.: 3122526-69-3
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PPAR agonist 7 is an orally active pan-PPAR agonist, demonstrating potent activation of all three subtypes, PPARα (EC50 = 1.51 μM), PPARδ (EC50 = 1.11 μM), and PPARγ (EC50 = 3.14 μM). PPAR agonist 7 significantly enhances glucose uptake in adipocytes while exhibiting minimal adipogenic activity. PPAR agonist 7 can suppress PPARγ Ser273 phosphorylation in white adipose tissue and upregulate insulin-sensitizing genes. PPAR agonist 7 does not cause weight gain or fluid retention in high-fat diet (HFD)/
Streptozotocin (HY-13753) (STZ)-induced type 2 diabetes mellitus (T2DM) models. PPAR agonist 7 has selective modulation of PPAR signaling pathways without activation of adipogenic gene programs. PPAR agonist 7 can be used for the study of diabetes .
Cat. No.: HY-180406
CAS No.: 1262495-12-4
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NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2, with pKi values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration. NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors. NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor, thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal .
Cat. No.: HY-181532
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IAP ligand 8 is an ASX-series, non-peptidic SMAC mimetic and IAP binder with high cell permeability. IAP ligand 8 selectively targets cIAP1-BIR3, XIAP-BIR2 (with a KD of 15.8 nM for both). IAP ligand 8 serves as an IAP ligand moiety to synthesize IAP-recruiting protein degrader (IPD) (HY-181590). This IPD simultaneously forms two ternary complexes, cIAP1-A538-TEAD1 and XIAP-A538-TEAD1, and efficiently degrades TEAD1 via a dual E3 recruitment mechanism, while inducing the autodegradation of cIAP1. IAP ligand 8 and its series of degraders are applicable to targeted research on Hippo pathway-dysregulated cancers such as NF2-mutant mesothelioma .
Cat. No.: HY-181964
CAS No.: 3023465-19-9
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KRAS G12C-IN-77 is an orally active and selective KRAS G12C covalent dual-state inhibitor that binds with high affinity to both GDP-bound (inactive state) and GTP-bound (active state) KRAS G12C (IC50 = 133 nM). KRAS G12C-IN-77 rapidly inhibits ERK1/2 phosphorylation, induces the formation of covalent adducts with endogenous KRAS G12C, suppresses the expression of MAPK pathway genes, and inhibits the proliferation of KRAS G12C-mutant cells. KRAS G12C-IN-77 is applicable to research related to KRAS G12C-mutant solid tumors, including pancreatic ductal adenocarcinoma and non-small cell lung cancer .
Cat. No.: HY-182287
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PRDX1-IN-4 is a PRDX1 inhibitor with an IC50 of 122 nM against human targets and high subtype selectivity. PRDX1-IN-4 covalently binds to PRDX1 to promote ROS accumulation. PRDX1-IN-4 inhibits NLRP3 inflammasome activation, blocks hepatic stellate cell activation and reduces collagen deposition. PRDX1-IN-4 induces apoptosis in activated hepatic stellate cells. PRDX1-IN-4 has good safety profile, with no significant body weight loss or hepatotoxicity observed in mice at a dose of 20 mg/kg. PRDX1-IN-4 ameliorates CCl4-induced liver injury and liver fibrosis in mice at a dose of 1 mg/kg. PRDX1-IN-4 can be used for the research of liver fibrosis .
Cat. No.: HY-187473
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PARP1-IN-58 is a ROS-responsive prodrug constructed based on a natural stilbene scaffold, and its active parent nucleus 24c acts as a selective PARP-1 inhibitor. PARP1-IN-58 only hydrolyzes to release the active parent compound in the high-ROS microenvironment of tumors; the active parent compound competitively binds to PARP-1 and blocks DNA single-strand damage repair, upregulates intracellular ROS levels, reduces mitochondrial membrane potential, and thereby induces cell cycle arrest and mitochondria-dependent apoptosis. PARP1-IN-58 exerts potent proliferation-inhibiting effects on BRCA-deficient breast cancer cells under simulated tumor oxidative stress conditions, and exhibits tumor growth inhibitory activity in breast cancer xenograft models. PARP1-IN-58 can be used in cancer-related research .
Cat. No.: HY-D3090
CAS No.: 2757682-04-3
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NRLD is a lipid droplet-targeting solvatochromic fluorescent probe developed based on Nile Red (HY-D0718), which can target lipid droplets and sense the non-polar lipid microenvironment inside lipid droplets. NRLD exhibits superior lipid droplet-targeting selectivity compared to the parent Nile Red dye in HeLa cell imaging. NRLD achieves detection relying on the solvatochromic effect generated by excited-state charge transfer, and its emission wavelength shifts according to the local polarity changes of the microenvironment it locates in: the more compact and ordered the lipid packing and the lower the environmental polarity, the more blue-shifted the emission; the looser the lipid packing or the stronger the hydration and the higher the environmental polarity, the more red-shifted the emission. NRLD shows blue shift in the non-polar oil core of lipid droplets and red shift in high-polarity environments such as phosphate buffer .
Cat. No.: HY-U00134R
CAS No.: 2179-37-5
Synonyms: Bencyclane (Standard); Benzcyclan (Standard)
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Benzcyclane (Standard) is the analytical standard of Benzcyclane (HY-U00134). This product is intended for research and analytical applications. Benzcyclane (Bencyclane; Benzcyclan) is a vasodilator with serotonin receptor antagonism. Benzcyclane exerts atypical serotonin antagonistic effects in rabbit superior mesenteric arteries. Benzcyclane relaxes high K +-induced contractions in rabbit basilar arteries and superior mesenteric arteries, and selectively inhibits sympathetic nerve stimulation-induced contractions in rabbit pulmonary arteries. Benzcyclane exerts non-competitive norepinephrine antagonistic effects in rabbit superior mesenteric arteries, and slightly reduces the maximum contractile response induced by histamine. Benzcyclane relaxes smooth muscles, induces transient hypotension, inhibits thrombosis, and accelerates blood fibrinolytic activity. Benzcyclane increases cerebral glucose content/uptake, enhances hypoxia tolerance in mice, and increases cerebral blood supply in dogs. Benzcyclane is applicable to studies related to cerebral vascular circulation .
Cat. No.: HY-L256
100 compounds
In modern drug discovery and chemical biology research, the azide group (-N3) is an important functional moiety that is widely used in click chemistry, biomolecular labeling, drug delivery systems, and prodrug design due to its unique reactivity and bioorthogonality.
The MCE Azide Structural Compound Library contains 100 compounds featuring -N3 functional groups. It is designed for the construction of click chemistry reaction systems and the subsequent development of functional molecules. This library enables the rapid assembly of targeting ligands, linkers, and functional molecular modules, thereby accelerating PROTAC assembly, optimization of antibody-drug conjugate (ADC) linkers, and the development of biological labeling probes. In addition, the high reaction selectivity and excellent biocompatibility of the azide group allow it to maintain stable reactivity even in complex biological environments, improving controllability and efficiency in drug design. It serves as an indispensable molecular tool in modern medicinal chemistry and chemical biology research.
Cat. No.: HY-L036
1,618 compounds
Small molecule covalent inhibitors, or irreversible inhibitors, are a type of inhibitors that exert their biological functions by irreversibly binding to target through covalent bonds. Compared with non-covalent inhibitors, covalent inhibitors have obvious advantages in bioactivity, such that covalent warheads can target rare residues of a particular target protein, thus leading to the development of highly selective inhibitors and achieving a more complete and continued target occupancy in living systems. In recent years, the distinct strengths of covalent inhibitors in overcoming drug resistance had been recognized. However, toxicity can be a real challenge related to this class of therapeutics due to their potential for off-target reactivity and has led to these drugs being disfavored as a drug class. The drug design and optimization of covalent inhibitors has become a hot spot in drug discovery.
MCE covalent inhibitor library contains 1,618 small molecules including identified covalent inhibitors and other bioactive molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, Sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.
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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
