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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
1979 Results for "
Highly selective
" in MedChemExpress (MCE) Product Catalog:
Products (1979)
1979 Results for "Highly selective" in MCE Product Catalog:
Cat. No.: HY-B0377G
CAS No.: 76824-35-6
Synonyms: MK-208 (GMP)
Research Areas:
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
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.
Cat. No.: HY-118156
CAS No.: 155238-60-1
L-699333 is a 5-lipoxygenase (5-LO) inhibitor belonging to the thieno[2,3,4-cd]indole class. This compound has a 2-ethoxybutyric acid side chain and is a potent inhibitor of the biosynthesis of 5-HPETE and LTB4 produced from human 5-LO, with ICm values of 22 nM, 7 nM, and 3.8 pM for human neutrophils and whole blood, respectively. L-699333 has shown anti-inflammatory and antiasthmatic effects in a variety of animal models, including rat pleurisy models, antigen-induced wheezing models, and awake macaque and sheep asthma models. Its inhibition of 5-LO is highly selective, with higher ICm values or stronger competitive inhibition in FLAP binding assays compared to inhibition of human 15-LO, porcine 12-LO, and ram epididymal cyclooxygenase. The racemic enantiomer 14g of L-699333 is the most potent enantiomer to date, with inhibitory effects similar to those of the known MK-0591, which has been shown in clinical trials to inhibit the biochemical effects of LTB4 biosynthesis in vitro and LTE4 excretion in urine.
Cat. No.: HY-12017C
CAS No.: 1159490-83-1
Target:
PF-04217903 phosphate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd value of 4.5 nM. PF-04217903 phosphate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 phosphate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 phosphate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 phosphate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 phosphate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis) .
Cat. No.: HY-B0377R
CAS No.: 76824-35-6
Synonyms: MK-208 (Standard)
Research Areas:
Famotidine (Standard) (MK-208 (Standard)) is the analytical standard of Famotidine (HY-B0377). This product is intended for research and analytical applications. Famotidine (MK-208) is an orally active and highly selective histamine H2 receptor antagonist. It inhibits gastric acid secretion by blocking the Gs signaling pathway, and regulates intracellular cAMP and ERK pathways. Famotidine inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine scavenges DPPH and nitric oxide free radicals, alleviates oxidative stress damage in gastric tissue, inhibits proMMP-9, improves vascular endothelial permeability, and restores the normal physiological functions of neutrophils and eosinophils. Famotidine crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
Cat. No.: HY-B0377S1
Synonyms: MK-208-13C
Cat. No.: HY-W707517
CAS No.: 2707433-64-3
Synonyms: MK-208-d4
Cat. No.: HY-W777002
CAS No.: 1185241-48-8
Synonyms: MK-208-13C3
Cat. No.: HY-L083
3,806 compounds
Mutations in oncogenes and tumor suppressor genes can modify multiple signaling pathways and in turn cell metabolism, which facilitates tumorigenesis. The paramount hallmark of tumor metabolism is “aerobic glycolysis” or the Warburg effect, coined by Otto Warburg in 1926, in which cancer cells produce most of energy from glycolysis pathway regardless of whether in aerobic or anaerobic condition. Usually, cancer cells are highly glycolytic (glucose addiction) and take up more glucose than do normal cells from outside. The increased uptake of glucose is facilitated by the overexpression of several isoforms of membrane glucose transporters (GLUTs). Likewise, the metabolic pathways of glutamine, amino acid and fat metabolism are also altered. Recent trends in anti-cancer drug discovery suggests that targeting the altered metabolic pathways of cancer cells result in energy crisis inside the cancer cells and can selectively inhibit cancer cell proliferation by delaying or suppressing tumor growth.
MCE provides a unique collection of 3,806 compounds which cover various tumor metabolism-related signaling pathways. These compounds can be used for anti-cancer metabolism targets identification, validation as well anti-cancer drug discovery.
Cat. No.: HY-L908
1,244 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 Lead-like Covalent Screening Library offers a valuable resource of 1,049 lead-like compounds with commonly used covalent warheads. These warheads, such as acrylamide, activated terminal alkyne, acyloxymethyl ketone, and boronic acid, are capable of reacting with specific amino acid residues, including cysteine, lysine, serine, and histidine. The inclusion of these reactive warheads in the library allows researchers to explore the potential of covalent inhibition, a powerful approach in drug discovery.
Synonyms: 15-Deoxy-Δ12,14-PGD2
Research Areas:
15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is a metabolite of prostaglandin D₂ (PGD₂) (HY-101988), which can undergo further dehydration metabolism to 15-deoxy-Δ12,14-PGJ₂. 15-deoxy-Δ12,14-Prostaglandin D2 is a highly selective agonist for DP2 receptor and PPARγ. 15-deoxy-Δ12,14-Prostaglandin D2 causes morphological changes in eosinophils and migration of type II innate lymphoid cells (ILC2). 15-deoxy-Δ12,14-Prostaglandin D2 has a growth inhibitory effect on prostate cancer cells expressing PPARγ, induces cell cycle arrest and promotes apoptosis. 15-deoxy-Δ12,14-Prostaglandin D2 can be used in related research on asthma and prostate cancer .
Cat. No.: HY-12017B
CAS No.: 1159490-85-3
Target:
PF-04217903 phenolsulfonate is an orally active, highly selective ATP-competitive c-Met kinase inhibitor with a Ki value of 4.8 nM and a Kd value of 4.5 nM. PF-04217903 phenolsulfonate blocks c-Met and HGF signaling pathways, inhibits MET phosphorylation, and blocks downstream MAPK, PI3K/AKT and PLCγ1 pathways. PF-04217903 phenolsulfonate suppresses tumor proliferation, survival, migration, invasion, angiogenesis and metastasis, induces apoptosis, and enhances efferocytosis, Annexin A1 expression and resolution of inflammation. PF-04217903 phenolsulfonate retains activity against several c-Met mutants (M1131T, V1220I, H1094R). PF-04217903 phenolsulfonate increases the incidence of subarachnoid hemorrhage and reduces survival rate without altering aneurysm formation, and also prevents lymph node metastasis induced by VEGF inhibition. PF-04217903 phenolsulfonate is applicable to research related to tumors (pancreas, stomach, lung, brain, colon, breast, kidney, melanoma, etc.), intracranial aneurysms and inflammatory diseases (gouty arthritis, neutrophilic pleuritis) .
Cat. No.: HY-B0377S
CAS No.: 2744683-81-4
Synonyms: MK-208-13C,d3
Cat. No.: HY-117947
CAS No.: 1809336-19-3
Target:
Research Areas:
(R)-OR-S1 is an isomer of OR-S1. The dual ZH1/2 inhibitors OR-S1 and OR-S2 exhibit strong inhibitory activity against both EZH1 and EZH2. OR-S1 and OR-S2 are highly selective methyltransferase inhibitors against EZH1 and EZH2, and they have very similar molecular features. Therefore, we investigated the effect of OR-S1 on acute myeloid leukemia (AML). We found that OR-S1 was able to induce cell differentiation and apoptosis in AML cells. These findings encouraged us to investigate whether functional LT-HSCs could survive PRC2-targeted therapy with OR-S1 or OR-S1 combined with cytarabine. The results showed that OR-S1 did not cause significant myelosuppression, and BM cells treated with the combination therapy were able to undergo normal hematopoiesis even 4 months after treatment. Therefore, temporary inhibition of EZH1 and EZH2 is clinically tolerable, making this combination therapy suitable for AML patients. AML is generally believed to originate from myeloid progenitor cells that inherit a large number of biological properties.
Cat. No.: HY-119820
CAS No.: 135354-02-8
Synonyms: SR57746A free base
Target:
Akt Dopamine Receptor Trk Receptor 5-HT Receptor PKC JNK ERK
Research Areas:
Xaliproden (SR57746) free base is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden free base activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden free base also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden free base exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden free base also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden free base can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
Cat. No.: HY-170524
CAS No.: 3052313-73-9
Research Areas:
TDI-015051 is a highly selective, orally active antiviral agent that targets the coronavirus NSP14 guanine-N7 methyltransferase. TDI-015051 binds to substrates in a non-competitive manner and forms a stable ternary complex, precisely blocking the capping and methylation processes of viral mRNA. TDI-015051 potently inhibits a variety of coronaviruses (including SARS-CoV-2 and MERS). By impairing viral replication and translation and inducing a moderate type I interferon-mediated immune response, it significantly reduces pulmonary viral load and exhibits a synergistic effect with Nirmatrelvir (HY-138687). In addition, TDI-015051 does not inhibit non-coronavirus methyltransferases, and the drug-resistant mutations it induces impair viral fitness, demonstrating excellent antiviral properties and safety. TDI-015051 can be used for research on COVID-19 and the replication mechanism of coronaviruses .The IC50 values of TDI-015051 against SARS-CoV-2, α-hCoV-NL63, α-hCoV-229E, β-hCoV-MERS are 0.15 nM, 1.7 nM, 2.6 nM and 3.6 nM, respectively, and the Ka value against SARS-CoV-2 is 0.061 nM .
Cat. No.: HY-L036P
6,121 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 6,121 small molecules including identified covalent inhibitors and other molecules having common covalent reactive groups as warheads, such as acrylamides, activated terminal acetylenes, sulfonyl fluorides/esters, cloracetamides, alkyl halides, epoxides, aziridines, disulfides, etc.
MCE Covalent inhibitor Library plus, with more powerful screening capability, further complement Covalent inhibitor Library (HY-L036) by adding some fragment compounds with covalent warheads.
Cat. No.: HY-14604R
CAS No.: 90494-79-4
Synonyms: SR57746A (Standard); SR57746 hydrochloride (Standard)
Research Areas:
Xaliproden (hydrochloride) (Standard) is the analytical standard of Xaliproden (hydrochloride). This product is intended for research and analytical applications. Xaliproden (SR57746) hydrochloride (SR57746A) is an orally active, highly selective 5-HT1A receptor agonist. Xaliproden hydrochloride activates pertussis toxin-sensitive G protein-coupled signaling cascades, as well as the PKC, ERK1/ERK2, Akt and p21 Ras/MEK-1 pathways. Xaliproden hydrochloride also downregulates the JNK/p66/c-Jun signaling pathway, induces phosphorylation of the shc adaptor protein, regulates extracellular dopamine and 5-HT levels, and induces [ 35S]GTPγS labeling in rat brain structures rich in 5-HT1A receptors. Xaliproden hydrochloride exerts neurotrophic, neuroprotective, renoprotective, anti-inflammatory, anti-apoptotic, anti-fibrotic and analgesic effects. Xaliproden hydrochloride also enhances NGF-induced neurite outgrowth, promotes motor neuron survival, attenuates renal tubular injury and inhibits chemotherapy-induced mechanical allodynia, without activating or altering NGF-induced TrkA receptor activation. Xaliproden hydrochloride can be used in the research of motor neuron disease, diabetic nephropathy, chemotherapy-induced peripheral neuropathy, amyotrophic lateral sclerosis, Alzheimer's disease, acute tonic nociceptive pain, inflammatory pain, depression and anxiety .
Cat. No.: HY-116028S1
CAS No.: 2750534-91-7
Synonyms: 15-Deoxy-Δ12,14-PGD2-d4
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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
