6719 Results for "

Blocker

" in MedChemExpress (MCE) Product Catalog:
Products (6719)

6719 Results for "Blocker" in MCE Product Catalog:

Cat. No.: HY-179041
CAS No.: 924851-91-2
SZ0232 is a selective mPGES-2 inhibitor. SZ0232 binds to the active site of mPGES-2 via hydrogen bonds and π-π stacking, reduces the production of prostaglandin E2 (PGE2) and blocks the PGE2-EP3 pathway. SZ0232 regulates Ferroptosis by activating the heme-dependent p53/SLC7A11/GPX4 axis, inhibits lipid peroxidation, and protects renal tubules. SZ0232 enhances glucose-stimulated insulin secretion, inhibits β-cell senescence, and improves glucose homeostasis. SZ0232 reduces renal lipid accumulation, alleviates fibrosis, and ameliorates renal dysfunction in diabetic mice. SZ0232 inhibits renal cyst growth in polycystic kidney disease models. SZ0232 exhibits an insulinotropic effect that strengthens with the increase of animal age. SZ0232 can be used in studies related to type 2 diabetes, acute kidney injury, diabetic kidney disease, and autosomal dominant polycystic kidney disease .
loading...
    loading...
Cat. No.: HY-183684
Target:  

RET VEGFR PDGFR Akt ERK

Research Areas:  

Endocrinology Cancer

RET-IN-33 is a moderately selective inhibitor of RET mutants. RET-IN-33 potently inhibits G810 mutants, with IC50 values of 4.43 nM (G810R), 3.28 nM (G810C) and 0.51 nM (G810S), respectively. RET-IN-33 also inhibits other RET mutants: V804M (IC50 0.73 nM), V804L (IC50 0.36 nM), Y806H (IC50 0.74 nM) and M918T (IC50 0.55 nM). RET-IN-33 also inhibits other kinases, with an IC50 of 1.50 nM against VEGFR2 and 1.60 nM against PDGFRα. RET-IN-33 blocks the autophosphorylation of RET mutants and the downstream SHC/AKT/ERK signaling pathway. RET-IN-33 selectively inhibits the proliferation of RET-driven cell models without affecting non-RET-dependent or normal cells. RET-IN-33 exhibits dose-dependent antitumor efficacy in RET-driven xenograft models. RET-IN-33 can be used for the research of medullary thyroid carcinoma, papillary thyroid carcinoma and non-small cell lung cancer .
loading...
    loading...
Cat. No.: HY-18719H
CAS No.: 1032008-71-1
Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC50 of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER + breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors .
loading...
    loading...
Cat. No.: HY-50896R
CAS No.: 183321-74-6
Synonyms: CP-358774 (Standard); NSC 718781 (Standard); OSI-774 (Standard)
Erlotinib Standard (CP-358774 Standard) is the analytical standard of Erlotinib (HY-50896). This product is intended for research and analytical applications. Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis .
loading...
    loading...
Cat. No.: HY-50896S
CAS No.: 1034651-23-4
Synonyms: CP-358774-d6; NSC 718781-d6; OSI-774-d6
Erlotinib-d6 (CP-358774-d6) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions .
loading...
    loading...
Cat. No.: HY-50896S1
CAS No.: 1211107-68-4
Synonyms: CP-358774-13C6; NSC 718781-13C6; OSI-774-13C6
Erlotinib- 13C6 (CP-358774- 13C6) is the 13C-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions .
loading...
    loading...
Cat. No.: HY-50896S2
CAS No.: 1130852-41-3
Synonyms: CP-358774-d4; NSC 718781-d4; OSI-774-d4
Erlotinib-d4 (CP-358774-d4) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, fibronectin, α-SMA, collagen deposition, and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, pancreatic cancer, renal fibrosis, and other conditions .
loading...
    loading...
Cat. No.: HY-50896S3
CAS No.: 1266656-97-6
Synonyms: CP-358774-d8; NSC 718781-d8; OSI-774-d8
Erlotinib-d8 (CP-358774-d8) is the deuterated-labeled Erlotinib (HY-50896). Erlotinib (CP-358774) is a selective, orally active EGFR tyrosine kinase inhibitor. Erlotinib also acts as a substrate and inhibitor of OATP2B1, with an IC50 of approximately 0.079 μM for inhibiting OATP2B1-mediated uptake of estrone 3-sulfate. Erlotinib blocks EGFR phosphorylation, downstream signal transduction, as well as the growth and proliferation of cancer cells. Erlotinib inhibits MMP-10-mediated renal injury, fibrotic lesions, the ERK1/2, GSK-3β and β-catenin signaling pathways, as well as the deposition of fibronectin, α-SMA, collagen and renal injury markers. Erlotinib is metabolized via CYP3A to produce the active metabolite OSI-420. Erlotinib can be used in research related to non-small cell lung cancer, gastric cancer, papillary renal cell carcinoma, EGFR inhibitor resistance and renal fibrosis .
loading...
    loading...
Cat. No.: HY-B0331AR
CAS No.: 76095-16-4
Synonyms: MK-421 maleate (Standard)
Enalapril maleate (Standard) (MK-421 maleate (Standard)) is the analytical standard of Enalapril maleate (HY-B0331A). This product is intended for research and analytical applications. Enalapril maleate is an orally active angiotensin-converting enzyme inhibitor. Enalapril maleate blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril maleate inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril maleate attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril maleate reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril maleate is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology .
loading...
    loading...
Cat. No.: HY-B0331S1
CAS No.: 1356847-94-3
Synonyms: MK-421-d3
Enalapril-d3 (MK-421-d3) is the deuterated-labeled Enalapril (HY-B0331). Enalapril is an orally active angiotensin-converting enzyme inhibitor. Enalapril blocks the conversion of angiotensin I to angiotensin II, regulates the renin-angiotensin system, reduces preload and afterload, and decreases plasma angiotensin II levels. Enalapril inhibits apoptosis, reduces nitric oxide metabolite levels, stabilizes endothelial cells, enhances endothelial antioxidant defense, scavenges reactive oxygen species (ROS), and alleviates neuronal damage. Enalapril attenuates glutathione depletion, protein/lipid oxidation, tissue damage, and type III collagen immunolabeling in organs of diabetic rats. Enalapril reduces systolic blood pressure and urinary albumin excretion, and delays the progression of diabetic cardiac/renal injury. Enalapril is used in research related to asymptomatic left ventricular dysfunction, congestive heart failure, Alzheimer's disease, diabetes mellitus, acute myocardial infarction, atrial fibrillation, hypertension, cerebral ischemia, chronic heart failure, and single-ventricle physiology .
loading...
    loading...
Cat. No.: HY-B0426AS2
Synonyms: ALO4943A-d6 hydrochloride; KW4679-d6 hydrochloride
Olopatadine-d6 (ALO4943A-d6; KW4679-d6) hydrochloride is deuterium-labeled Olopatadine (hydrochloride) (HY-B0426A). Olopatadine hydrochloride (ALO4943A; KW4679) is an orally active histamine H1 receptor antagonist and mast cell stabilizer. Olopatadine hydrochloride exerts antiallergic effects by blocking histamine H1 receptor-mediated activities. Olopatadine hydrochloride inhibits exocytosis, chemokine release, F-actin polymerization, CXCL10-induced calcium influx, and T cell chemotactic activity. Olopatadine hydrochloride also reduces the expression levels of CXCR3 on the surface of CD4 + and CD8 + T cells. Olopatadine hydrochloride inhibits scratching behavior, improves dermatitis scores, and suppresses intraepidermal neurite outgrowth. Olopatadine hydrochloride simultaneously decreases the levels of inflammatory markers, growth factors, histamine, and specific IgE, while increasing the expression of ErbB3A/HER3A. Olopatadine hydrochloride can be used in research related to seasonal pollinosis, chronic rhinitis, urticaria, allergic conjunctivitis, alopecia areata, and atopic dermatitis .
loading...
    loading...
Cat. No.: HY-N0515R
CAS No.: 945619-74-9
Ophiopogonin D (Standard) is the analytical standard of Ophiopogonin D. This product is intended for research and analytical applications. Ophiopogonin D can be isolated from the tubers of Ophiopogon japonicus, is a rare naturally occurring C29 steroidal glycoside. Ophiopogonin D is a CYP2J3 inducer that significantly inhibits Ang II induced NF-κB nuclear translocation, IκBα down-regulation, intracellular Ca2+ overload and activation of pro-inflammatory cytokines by increasing the expression of CYP2J2/EETs and PPARα in human umbilical vein endothelial cells (HUVECs). Ophiopogonin D can inhibit isteoclastic differentiation in RAW264.7 cells. Ophiopogonin D has protective effect as an antioxidant in H2O2-induced endothelial injury. Ophiopogonin D blocks ERK signaling cascades. Ophiopogonin D alleviates high-fat diet-induced metabolic syndrome and changes the structure of gut microbiota in mice. Ophiopogonin D has been used against inflammatory, metabolic and cardiovascular diseases .
loading...
    loading...
Cat. No.: HY-N1510
CAS No.: 22149-35-5
Kaempferol 3-O-gentiobioside is an orally active flavonoid, with a Ka value of 57 µM against human NOTCH1 and an IC50 value of 50 μM against α-glucosidase. Kaempferol 3-O-gentiobioside inhibits the NOTCH signaling pathway. It downregulates the expression of TLR4 and NLRP3, and suppresses the activation and nuclear translocation of NF-κB. Kaempferol 3-O-gentiobioside inhibits the expression of MUC5AC, reduces nitrite and ROS levels, and attenuates excessive mucus secretion. It exhibits antibacterial activity, reducing the formation and growth of MRSA biofilms. Kaempferol 3-O-gentiobioside blocks the TGF-β/ALK5/Smad signaling pathway and inhibits epithelial-mesenchymal transition. It suppresses the proliferation, migration, invasion and metastatic growth of tumor cells. Kaempferol 3-O-gentiobioside alleviates airway inflammation and mucus hypersecretion in mice with allergic asthma . It reduces the volume of ovarian cancer xenografts in mice. Kaempferol 3-O-gentiobioside can be used in research related to allergic asthma, diabetes, MRSA infection, breast cancer, gastric cancer and ovarian cancer .
loading...
    loading...
Cat. No.: HY-N1746
CAS No.: 270249-38-2
Synonyms: 2'-O-Methylkurarinone
(2S)-2'-Methoxykurarinone (2'-O-Methylkurarinone) is a flavanone natural product found in the roots of Sophora flavescens, possessing anti-sepsis, inhibitory effects on osteoclast differentiation and bone resorption, anti-inflammatory, and anti-Plasmodium activities. (2S)-2'-Methoxykurarinone exhibits an EC50 = 2.4 μM against the FCR-3 strain of Plasmodium falciparum. In sepsis models, (2S)-2'-Methoxykurarinone modulates immune cell function and inhibits inflammation and oxidative stress. In bone-related models, (2S)-2'-Methoxykurarinone blocks osteoclast differentiation and bone resorption, and inhibits RANKL-mediated Akt, p38, and JNK signaling pathways. In skin inflammation models, (2S)-2'-Methoxykurarinone inhibits NF-κB pathway activation, upregulates HO-1 expression, and suppresses CCL27 chemokine production in HaCaT cells. (2S)-2'-Methoxykurarinone is useful for research on osteoporosis, sepsis, inflammatory skin diseases (such as atopic dermatitis and allergic contact dermatitis), and malaria .
loading...
    loading...
Cat. No.: HY-N2896
CAS No.: 465-00-9
Arjunolic acid is an orally active, multifunctional bioactive compound. Arjunolic acid exhibits free radical scavenging activity, as well as fungal and bacterial activities. Arjunolic acid induces apoptosis (Apoptosis) in various cancer cells. Arjunolic acid protects hepatocytes against induced oxidative stress and apoptosis by reducing reactive oxygen species and inhibiting NF-κB activation. Arjunolic acid regulates pancreatic dysfunction in type 2 diabetic rats by blocking the activation of the TLR-4/MyD88 and canonical Wnt pathways. Arjunolic acid inhibits neuroinflammation and ameliorates depressive behaviors via the SIRT1/AMPK/Notch1 signaling pathway in microglia. Arjunolic acid improves Crohn's disease-like colitis by restoring gut microbiota composition and inhibiting TLR4 signaling. Arjunolic acid suppresses osteosarcoma progression by inhibiting Wnt3a-mediated M2 polarization of macrophages. Arjunolic acid ameliorates diabetic retinopathy via the autophagy pathway regulated by AMPK/mTOR/HO-1. Arjunolic acid is applicable to research related to type 2 diabetes, organ toxicity, depression, Crohn's disease, osteosarcoma, diabetic retinopathy, and testicular dysfunction .
loading...
    loading...
Cat. No.: HY-P990144

Target:  

Integrin

Research Areas:  

Inflammation/Immunology Cancer

Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) is an anti-mouse/human VLA-4/CD49d IgG2b monoclonal antibody. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can reduce VLA-4 positive cells. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can inhibit the migration of Tc1 cells to tumors. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) inhibits the retention of leukemia cells in the spleen and bone marrow by blocking VLA-4. Anti-Mouse/Human VLA-4/CD49d Antibody (PS/2) can be used for research on inflammation conditions and cancer such as experimental autoimmune encephalomyelitis (EAE), melanoma and leukemia .
loading...
    loading...
Cat. No.: HY-P990290
Anti-Mouse CD16/CD32 (LALA-PG) Antibody (2.4G2) is a mouse-derived IgG2a κ type antibody inhibitor, targeting to mouse CD16/CD32. Anti-Mouse CD16/CD32 (LALA-PG) Antibody (2.4G2) is a chimeric antibody of the original 2.4G2 antibody (HY-P99125). Anti-Mouse CD16/CD32 (LALA-PG) Antibody (2.4G2) contains the LALA-PG mutation region. Anti-Mouse CD16/CD32 (LALA-PG) Antibody (2.4G2) can block the combination of CD16 and FcγRs. Anti-Mouse CD16/CD32 (LALA-PG) Antibody (2.4G2) can be used for the researches of immunology and cardiovascular disease.
loading...
    loading...
Cat. No.: HY-P992059

Target:  

CD1

Research Areas:  

Cancer

Anti-Mouse CD1d Antibody (1B1) is an antibody targeting mouse CD1d (Kd=12.5 nM). By inserting into the lipid-binding groove of CD1d, Anti-Mouse CD1d Antibody (1B1) overlaps with the binding sites of type I and type II NKT cell receptors (TCR), thereby effectively blocking TCR-mediated interactions. Anti-Mouse CD1d Antibody (1B1) activates antigen-presenting cells such as dendritic cells and macrophages, induces them to release IL-12p70, and increases the levels of key cytokines including IL-12, IFN-γ and IFN-α in mouse serum. Anti-Mouse CD1d Antibody (1B1) can be used in studies related to renal cancer, breast cancer and colon adenocarcinoma. When combined with anti-DR5 or anti-CD137 antibodies and chemotherapeutic drugs, Anti-Mouse CD1d Antibody (1B1) exhibits significant tumor inhibitory and even eradication effects in mice .
loading...
    loading...
Cat. No.: HY-118594R
CAS No.: 632-93-9
Research Areas:  

Metabolic Disease

Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate (Standard) is the analytical standard of Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate (HY-118594). This product is intended for research and analytical applications. Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate is an orally active porphyrin inducer and ferrochelatase inhibitor. Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate can induce small bile duct obstruction in mice, resulting in blocked bile excretion and causing cholestasis. Long-term use of Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate can cause damage to bile duct epithelial cells, inflammatory responses, and liver fibrosis. Diethyl 2,4,6-trimethyl-1,4-dihydropyridine-3,5-dicarboxylate can be used to simulate the pathological features of cholestatic liver diseases such as sclerosing cholangitis (PSC).
loading...
    loading...
Cat. No.: HY-13689G
CAS No.: 133053-19-7
Go 6983 GMP is Go 6983 (HY-13689) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. Go 6983 is a dual inhibitor targeting Suv39h1/2 (KMT1A/KMT1B) and PKC, as well as a transcriptional activator capable of inducing DNA hypomethylation. Go 6983 stimulates the transcription of Prdm14 by reducing Suv39h1/2 protein levels, decreasing histone modifications in the Prdm14 promoter region, and increasing the recruitment of RNA polymerase II. Go 6983 induces genome-wide DNA hypomethylation by inhibiting de novo methyltransferase expression and increasing Tet1/Tet2 levels, thereby promoting self-renewal and pluripotency maintenance of stem cells. Meanwhile, Go 6983 can block PKC-mediated signaling pathways to reduce the expression of EMT-related genes and eliminate the upregulation of antioxidant genes downstream of NRF2. Go 6983 is mainly used in mechanism studies related to myocardial ischemia/reperfusion injury .
loading...
    loading...