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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
43 Results for "
h2 blocker
" in MedChemExpress (MCE) Product Catalog:
Products (43)
43 Results for "h2 blocker" in MCE Product Catalog:
8
8 Publications Verification
Research Areas:
Cardiovascular Disease Neurological Disease Inflammation/Immunology Cancer
GY4137 is a sustained-release H2S donor possessing vasodilatory, antihypertensive, and anti-inflammatory activities. GY4137 can inhibit cell growth, induce apoptosis, and cause cell cycle arrest by blocking the STAT3 pathway, demonstrating potent anticancer activity .
7
Research Areas:
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 .
6
6 Cited Publications
Research Areas:
XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .
2
2 Cited Publications
Cat. No.: HY-N0515
CAS No.: 945619-74-9
1
1 Cited Publications
Cat. No.: HY-121970
CAS No.: 27031-00-1
Target:
Phosphoglycerate Dehydrogenase (PHGDH) Reactive Oxygen Species (ROS) HIF/HIF Prolyl-Hydroxylase
Research Areas:
iGP-1 is a cell-permeable, selective mixed inhibitor of mitochondrial sn-glycerol-3-phosphate dehydrogenase (mGPDH), with IC50s of 6.3 μM and 13.6 μM for rat mGPDH activity and H2O2 production, respectively. iGP-1 specifically blocks the mitochondrial component of the glycerophosphate shuttle without affecting cytosolic GPDH. iGP-1 not only inhibits cell proliferation and glutaminolysis, and enhances glycolysis, but also significantly alters key cellular physiological processes such as apoptosis, ROS production, HIF-1α stability and mitochondrial membrane potential. iGP-1 remains active in neutrophil cultures under both normoxic and hypoxic conditions, and serves as an ideal probe for glycerol-3-phosphate metabolic mechanisms. iGP-1 has been applied to studies on prostate cancer and related metabolic pathways .
1
1
1 Cited Publications
Target:
Research Areas:
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
Cat. No.: HY-124834
CAS No.: 75483-04-4
Target:
Research Areas:
Nrf2 activator-10 (Compound AI-1) is a PI3K-dependent inducer for antioxidant response element (ARE) (EC50 is 2.7 μM) and an activator for Nrf2. Nrf2 activator-10 modifies Keap1, blocks Cul3-Keap1 ubiquitin ligase complex, activates the transcription of Nrf2. Nrf2 activator-10 protects cells from H2O2-induced apoptosis.
Cat. No.: HY-P990193
Target:
Research Areas:
Cat. No.: HY-P99135
Target:
Research Areas:
Cat. No.: HY-N0515R
CAS No.: 945619-74-9
Cat. No.: HY-122860
CAS No.: 2300981-68-2
SKLB-C05 is a novel selective, orally active TOPK inhibitor, with an IC50 of 0.5 nM. SKLB-C05 selectively inhibit TOPK kinase. SKLB-C05 induces Apoptosis, downregulates c-Myc, γ-H2AX, activates p53, blocks FAK/Src medicated migration-related signaling. SKLB-C05 disturbs cell mitosis. SKLB-C05 shows anticancer activity only against TOPK-positive colorectal cancer .
Cat. No.: HY-124517
CAS No.: 34970-69-9
Research Areas:
Burimamide is a blocker of histamine H2-receptor. Burimamide inhibits gastric acid secretion evoked by Pentagastrin (HY-A0261) or Gastrin. Burimamide also has alpha-adrenoceptor blocking activity. Burimamide in combination with the H1-receptor antagonist Mepyramine (HY-B1281) shows anti-inflammatory activity in a rat paw edema model induced by Compound 48/80 (HY-115768) .
Cat. No.: HY-138794A
CAS No.: 2417089-73-5
Target:
Research Areas:
(Rac)-XL177A is the racemic isomer of XL177A (HY-138794). XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .
Cat. No.: HY-W707517
CAS No.: 2707433-64-3
Synonyms: MK-208-d4
Cat. No.: HY-B0377S
CAS No.: 2744683-81-4
Synonyms: MK-208-13C,d3
Cat. No.: HY-160979
CAS No.: 96153-56-9
Synonyms: DA-5047
Target:
Research Areas:
Bisfentidine is an H2 receptor antagonist, Bisfentidine can block the H2 receptor on the cells of the stomach wall, and reduce the secretion of stomach acid. Bisfentidine binds to cytochrome P-450 in liver microsomes and affects drug metabolism. Bisfentidine can be used in the study of metabolic processes of drugs, lipid peroxidation processes and peptic ulcers diseases .
Cat. No.: HY-168766
CAS No.: 199854-00-7
Target:
Research Areas:
O-Acetylsalicylhydroxamic acid is an acetylation inhibitor of prostaglandin H2 synthase that can suppress PGE2 synthesis in the body and block the cyclooxygenase activity of PGHS in vitro. O-Acetylsalicylhydroxamic acid requires the presence of the active site residue Ser-529 to act on human PGHS-1; the S529A mutant is resistant to the inactivation effects of this inhibitor .
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 .
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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
