2853 Results for "

Cell Signaling

" in MedChemExpress (MCE) Product Catalog:
Products (2853)

2853 Results for "Cell Signaling" in MCE Product Catalog:

Cat. No.: HY-18719S
CAS No.: 1584173-54-5
Endoxifen-d5 (Z-isomer) is the deuterated-labeled Endoxifen (Z-isomer methanesulfonate) (HY-18719H). Endoxifen-d5 Z-isomer 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-d5 Z-isomer 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-d5 Z-isomer 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-189649
CAS No.: 3133922-71-8
Research Areas:  

Cancer

PI3K/HDAC-IN-5 is a dual PI3K/HDAC inhibitor. PI3K/HDAC-IN-5 inhibits PI3Kα, PI3Kβ, PI3Kγ, and PI3Kδ (IC50 values of 25.41, 134.52, 166.75, and 41.58 nM, respectively) and inhibits downstream PI3K/AKT signaling. PI3K/HDAC-IN-5 inhibits HDAC6, HDAC8, and HDAC11 (IC50 values of 29.35, 157.27, and 382.26 nM, respectively), increases α-tubulin and SMC3 acetylation, while not affecting histone H3/H4 acetylation. PI3K/HDAC-IN-5 induces S phase cell cycle arrest and apoptosis, and inhibits the proliferation of cervical cancer cell lines. PI3K/HDAC-IN-5 can be used for research on cervical cancer .
loading...
    loading...
Cat. No.: HY-N7653
CAS No.: 529-51-1
Azaleatin is an orally active inhibitor of hQC, NS2B-NS3 protease and E. coli β-glucuronidase, with IC50 values of 1.1 μM, 38.00 μg/mL and 0.57 μM, respectively. Azaleatin inhibits the activities of NF-κB, MyD88, JAK1, TLR4, STAT3, IL-1β, IL-6, COX-2, TNF-α and β-glucuronidase, blocks pro-inflammatory signaling pathways, reduces the levels of ROS, MDA and uric acid, elevates the levels of GPx, GSR, GST, SOD, CAT, HO-1 and GSH, scavenges free radicals and exerts reducing capacity. Azaleatin inhibits the expression of pro-apoptotic proteins Bax, Caspase-9 and Caspase-3, and upregulates the expression of anti-apoptotic protein Bcl-2. Azaleatin reduces the levels of cardiac injury markers, restores cardiac histological structure, inhibits Aβ aggregation, dengue protease activity, hepatic stellate cell proliferation and cancer cell growth, and also exhibits antibacterial activity. Azaleatin can be used in studies related to subchronic cardiotoxicity, Alzheimer's disease, dengue fever, hyperuricemia, liver fibrosis, gastric cancer and bacterial infections .
loading...
    loading...
Cat. No.: HY-P10414
Synonyms: KP1 (human)
Target:  

TGF-β Receptor

Research Areas:  

Infection Endocrinology

Klotho-derived peptide 1 (KP1 (human)) is a polypeptide with multiple activities including senescence inhibition and renal protection. Klotho-derived peptide 1 binds to TβR2 and ATAD3A, with a Kd value of 1.41 μM for binding to human TβR2 and a Kd value of 0.319 μM for binding to ATAD3A. By binding to TβR2, Klotho-derived peptide 1 blocks the TGF-β/Smad3 and downstream TGF-β signaling pathways, inhibits the expression of miR-223-3p, induces the expression of lncRNA-TUG1, restores endogenous Klotho at the post-transcriptional level, inhibits cellular senescence markers, fibroblast activation and renal tubular epithelial cell apoptosis, blocks cytochrome c release and caspase activation, maintains the integrity of mitochondrial ultrastructure, and restores mitochondrial protein levels. Klotho-derived peptide 1 enters renal tubular epithelial cells via endocytosis, protects against nephrotoxic and hypoxic injuries, and recapitulates the renal protective and anti-fibrotic effects of full-length Klotho. Klotho-derived peptide 1 can be used in research related to kidney diseases such as chronic kidney disease and SARS-CoV-2-associated acute kidney injury .
loading...
    loading...
Cat. No.: HY-P10414A
Synonyms: KP1 (human) hydrochloride
Target:  

TGF-β Receptor

Research Areas:  

Infection Endocrinology

Klotho-derived peptide 1 hydrochloride (KP1 (human) hydrochloride) is a polypeptide with multiple activities including senescence inhibition and renal protection. Klotho-derived peptide 1 hydrochloride binds to TβR2 and ATAD3A, with a Kd value of 1.41 μM for binding to human TβR2 and a Kd value of 0.319 μM for binding to ATAD3A. By binding to TβR2, Klotho-derived peptide 1 hydrochloride blocks the TGF-β/Smad3 and downstream TGF-β signaling pathways, inhibits the expression of miR-223-3p, induces the expression of lncRNA-TUG1, restores endogenous Klotho at the post-transcriptional level, inhibits cellular senescence markers, fibroblast activation and renal tubular epithelial cell apoptosis, blocks cytochrome c release and caspase activation, maintains the integrity of mitochondrial ultrastructure, and restores mitochondrial protein levels. Klotho-derived peptide 1 hydrochloride enters renal tubular epithelial cells via endocytosis, protects against nephrotoxic and hypoxic injuries, and recapitulates the renal protective and anti-fibrotic effects of full-length Klotho. Klotho-derived peptide 1 hydrochloride can be used in research related to kidney diseases such as chronic kidney disease and SARS-CoV-2-associated acute kidney injury .
loading...
    loading...
Cat. No.: HY-P992076
Anti-Candida auris β-1,3-glucans Antibody (2G8) is an antibody targeting Candida auris β-1,3-glucans, and also acts as an inhibitor of AChE and TGF-β receptor 2. Anti-Candida auris β-1,3-glucans Antibody (2G8) also targets fungal cell wall components, effectively inhibits fungal growth and interferes with capsule formation, thereby significantly reducing the fungal load in mouse tissues. Anti-Candida auris β-1,3-glucans Antibody (2G8) not only blocks TGF-β receptor binding to inhibit the Smad signaling pathway, reduces fibroblast activation and collagen deposition, but also induces epithelial differentiation of tumor cells and reduces pancreatic tumor metastasis. Anti-Candida auris β-1,3-glucans Antibody (2G8) specifically binds to the conserved N-linked glycoepitope on AChE to inhibit its activity without interfering with BChE, and can be used in studies of cryptococcosis and related tumor mechanisms .The isotype control is Human IgG1 kappa, Isotype Control (HY-P99001).
loading...
    loading...
Cat. No.: HY-L001V
34,325 compounds
A unique collection of 34,325 bioactive compounds including natural products, enzyme inhibitors, receptor ligands, and drugs for high throughput screening (HTS) and high content screening (HCS).
Cat. No.: HY-10952
CAS No.: 357605-73-3
Research Areas:  

Cancer

ONO-AE2-227 is an orally active EP4 receptor antagonist. ONO-AE2-227 blocks PGE2-mediated EP4 signaling by competitively antagonizing PGE2-induced cAMP elevation, and binds to EP4/EP3 with mouse Ki values of 2.7/21 nM. ONO-AE2-227 reduces aberrant crypt foci and intestinal polyp development, and inhibits intestinal polyp formation. ONO-AE2-227 enhances LPS-induced TNF-alpha release from human alveolar macrophages by blocking endogenous PGE2, blocks PGE2-induced ICAM-1 expression and leukocyte-endothelial adhesion, and attenuates PGE2-induced monocyte adhesion to brain endothelial cells. ONO-AE2-227 can be used for research on colon cancer .
loading...
    loading...
Cat. No.: HY-16265A
CAS No.: 2514957-81-2
Research Areas:  

Cancer

JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
loading...
    loading...
Cat. No.: HY-175042
Synonyms: Ins(1,3,4,5,6)P5 ammonium salt; 1,3,4,5,6-IP5 ammonium salt
Target:  

Akt

Research Areas:  

Cancer

D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) (Ins(1,3,4,5,6)P5 (ammonium salt)) is an isomer of inositol phosphate that acts as a small and soluble second messenger in the transmission of cellular signals. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) can bind to the PH domain of Grp1 with a Kd of 590 nM. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) can inhibit the phosphorylation and kinase activity of Akt/PKB, inducing apoptosis in ovarian, lung, and breast cancer cells. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) exhibits antiangiogenic activity in vitro and blocks capillary tube formation of HUVEC. D-myo-Inositol-1,3,4,5,6-pentaphosphate (ammonium salt) exerts antitumor effects against cancer xenografts in nude mice .
loading...
    loading...
Cat. No.: HY-B0110
CAS No.: 60282-87-3
Synonyms: SHB 331; WL 70
Gestodene (SHB 331; WL 70) is an orally active synthetic progestogen compound of the 19-nortestosterone class. Gestodene binds with high affinity to the progesterone receptor, inhibits 5α-reductase, binds to androgen and aldosterone receptors, and inactivates CYP3A. Gestodene acts as a positive allosteric modulator of PAR1, enhances PAR1-mediated signaling pathways, and is capable of increasing the activation potency of PAR1-AP toward PAR1, thereby promoting ERK1/2 phosphorylation, receptor internalization, cell morphological changes, and human platelet aggregation. Gestodene and its A-ring reduced metabolites promote the proliferation, differentiation, and mineralization of neonatal rat osteoblasts. Gestodene itself has no binding capacity for estrogen receptors, and this osteogenic activity depends on intracellular metabolism to generate A-ring reduced products with estrogen-like agonistic activity. Gestodene is useful for research on diseases related to progesterone secretion and diseases related to thrombosis .
loading...
    loading...
Cat. No.: HY-B0377A
CAS No.: 125193-62-6
Synonyms: MK-208 hydrochloride
Famotidine hydrochloride (MK-208 hydrochloride) 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 hydrochloride inhibits TLR3-mediated inflammatory pathways, and reduces the expression of various inflammatory mediators and interferon-related genes. Famotidine hydrochloride 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 hydrochloride crosses intestinal epithelial cells via facilitated diffusion and passive diffusion, blocks paracellular cation transport, and increases intestinal transepithelial electrical resistance. Famotidine hydrochloride reduces serum levels of transaminases and alkaline phosphatase, exerts analgesic effects and gastric protective effects simultaneously. Famotidine hydrochloride can be used in studies related to COVID-19, liver injury and acute gastric ulcer .
loading...
    loading...
Cat. No.: HY-D3187
CAS No.: 2484831-02-7
HMRef-αMan is a substrate-based green fluorescent probe (Ex/Em=465 nm/515 nm) targeting MAN2C1 (α-mannosidase). HMRef-αMan can be specifically cleaved by MAN2C1 to generate a highly fluorescent product, which thus gets activated to produce green fluorescence in malignant breast tissues, benign lesions and living cancer cells. The signal intensity of HMRef-αMan is directly correlated with MAN2C1 activity, and it can effectively detect tiny breast cancer lesions with a diameter of less than 1 mm. When used in combination with the red-emitting γ-glutamyl transpeptidase (GGT) probe gGlu-2OMe SiR600 (HY-D3188), HMRef-αMan enables precise optical differentiation of breast tissue types via a dual-color imaging strategy. HMRef-αMan has been widely used in the research of breast diseases such as breast cancer, fibroadenoma, phyllodes tumor and various types of papilloma .
loading...
    loading...
Cat. No.: HY-N16300
CAS No.: 3091879-75-0
Target:  

Fluorescent Dye

Research Areas:  

Others

Mito-laurdan (bromide) is a Fluorescent dye for mitochondrial membrane fluidity and packing measurement. It depends on membrane potential for targeting: it contains a cationic triphenylphosphonium moiety that accumulates at the inner mitochondrial membrane due to the membrane's negative potential, connected via a 3-carbon linker. As a solvatochromic dye derived from Laurdan (HY-D0080), it retains the characteristic mechanism where fluorescence emission shifts based on membrane packing: in more fluid, loosely packed membranes, greater water penetration leads to increased dipolar relaxation and a bathochromic red shift in emission, while more ordered membranes show a blue-shifted emission; these shifts are quantified using generalized polarization, calculated from emission intensities in ordered and disordered spectral windows. Its excitation wavelength is 352 nm, with emission detected in ordered (409-463 nm) and disordered (473-516 nm) spectral windows. It localizes specifically to mitochondria in HeLa cells, showing high signal overlap with MitoTracker Deep Red, and can detect changes in inner mitochondrial membrane fluidity .
loading...
    loading...
Cat. No.: HY-Y0317I
CAS No.: 7757-82-6
Synonyms: Disodium sulfate, meets analytical specification of Ph. Eur. BP USP
Sodium sulfate anhydrous (Disodium sulfate), meets analytical specification of Ph. Eur. BP USP is an orally active multifunctional ionic salt that serves as a protein precipitant, collagen fibril bundling inducer, and chlorine-free sodium source. Sodium sulfate anhydrous, meets analytical specification of Ph. Eur. BP USP promotes collagen fibril bundling to increase matrix pore size, alters cancer cell morphology and regulates their migration direction via geometric signals, and separates plasma/serum proteins or concentrates proteins at 37°C without causing thermal denaturation. In poultry farming applications, Sodium sulfate anhydrous, meets analytical specification of Ph. Eur. BP USP improves laying performance and eggshell quality, and is safe and effective at an addition level of 0.3-1.5%, while a high concentration of 3.0% causes negative physiological effects. Sodium sulfate anhydrous, meets analytical specification of Ph. Eur. BP USP can be widely applied in scientific research on cervical cancer and related fields .
loading...
    loading...
Cat. No.: HY-L062
2,593 compounds

Neurotransmitter (NT) receptors, also known as neuroreceptors, are a broadly diverse group of membrane proteins that bind neurotransmitters for neuronal signaling. There are two major types of neurotransmitter receptors: ionotropic and metabotropic. Ionotropic receptors are ligand-gated ion channels, meaning that the receptor protein includes both a neurotransmitter binding site and an ion channel. The binding of a neurotransmitter molecule (the ligand) to the binding site induces a conformational change in the receptor structure, which opens, or gates, the ion channel. The term “metabotropic receptors” is typically used to refer to transmembrane G-protein-coupled receptors. Metabotropic receptors trigger second messenger-mediated effects within cells after neurotransmitter binding.

In some neurological diseases, the neurotransmitter receptor itself appears to be the target of the disease process. Many neuroactive drugs act by modifying neurotransmitter receptors. A better understanding of neurotransmitter receptor changes in disease may lead to improvements in therapy.

MCE designs a unique collection of 2,593 compounds targeting a variety of neurotransmitter receptors. MCE Neurotransmitter Receptor Compound Library is a useful tool for neurological diseases drug discovery.

Cat. No.: HY-L008
738 compounds

The Janus kinase (JAK)/signal transducer and activator of transcription (STAT) pathway is central to signaling by cytokine receptors, a superfamily of more than 30 transmembrane proteins that recognize specific cytokines, and is critical in blood formation and immune response. Canonical JAK/STAT signaling begins with the association of cytokines and their corresponding transmembrane receptors. Activated JAKs then phosphorylate latent STAT monomers, leading to dimerization, nuclear translocation, and DNA binding. In mammals, there are four JAKs (JAK1, JAK2, JAK3, TYK2) and seven STATs (STAT1, STAT2, STAT3, STAT4, STAT5a, STAT5b, STAT6). Since the JAK/STAT pathway plays a major role in many fundamental processes, such as apoptosis and inflammation, dysfunctional proteins in the pathway may lead to a number of diseases. For example, alterations in JAK/STAT signalling can result in cancer and diseases affecting the immune system, such as severe combined immunodeficiency disorder (SCID).

MCE provides 738 compounds that can be used in the study of the JAK/STAT signaling pathway and related diseases.

Cat. No.: HY-L046
2,468 compounds

Cardiovascular diseases (CVDs) are a group of disorders of the heart and blood vessels which include coronary heart disease, cerebrovascular disease, peripheral arterial disease, rheumatic heart disease, etc. CVDs are the number 1 cause of death globally. Smoking, unhealthy nutrition, aging population, lack of physical activity, arterial hypertension, or diabetes can promote cardiovascular disease like myocardial infarction or stroke. It is multifactorial and encompasses a multitude of mechanisms, such as eNOS uncoupling, reactive oxygen species formation, chronic inflammatory disorders and abnormal calcium homeostasis. Antioxidant, anti-inflammatory and anti-diabetes agents may reduce the cardiovascular disease risk.

MCE supplies a unique collection of 2,468 compounds with confirmed anti-cardiovascular activity. These compounds mainly target metabolic enzyme, membrane transporter, ion channel, inflammation related signaling pathways. MCE Anti-Cardiovascular Disease Compound Library can be used for cardiovascular diseases related research and high throughput and high content screening for new drugs.

Cat. No.: HY-L074
3,404 compounds

Breast cancer is the most frequent cancer among women, impacting 2.1 million women each year, and also causes the greatest number of cancer-related deaths among women. Surgery is usually the first type of treatment for breast cancer, which is usually followed by chemotherapy or radiotherapy or, in some cases, hormone or targeted therapies, especially for metastatic breast cancer (MBC).

Breast cancer is a heterogeneous disease, which is categorized into 3 major subtypes based on the presence or absence of molecular markers for estrogen or progesterone receptors and human epidermal growth factor 2 (ERBB2; formerly HER2): hormone receptor positive/ERBB2 negative (70% of patients), ERBB2 positive (15%-20%), and triple-negative (tumors lacking all 3 standard molecular markers; 15%). Different intrinsic subtypes exhibit different tumor behavior with different prognoses, and may require specific targeted therapies to maximize treatment effectiveness. Otherwise, some signaling pathways also play important roles in the development of breast cancer, such as NF-κB Signaling Pathway, TGF-beta Signaling Pathway, PI3K/AKT/mTOR signaling pathway and Notch Signaling Pathway. These signaling pathways offer ideal targets for development of new targeted therapies for breast cancer.

MCE supplies a unique collection of 3,404 compounds with identified and potential anti-breast cancer activity. MCE Anti-Breast Cancer Compound Library is a useful tool for anti-breast cancer drugs screening.

Cat. No.: HY-172889
CAS No.: 3085191-45-0
Target:  

PI3K HDAC Apoptosis mTOR Akt

Research Areas:  

Cancer

PI3K/HDAC-IN-4 (Compound 31f) is a PI3K/HDAC dual inhibitor (IC50: 0.2μM). PI3K/HDAC-IN-4 shows high selectivity for HDAC1-3 (IC50 values of 75.5 nM, 70.9 nM, and 1.9 nM, respectively). PI3K/HDAC-IN-4 is a potent PIK3 inhibitor with IC50 values of 2.5 nM, 80.5 nM, 10.0 nM, and 57.2 nM for PI3Kα, β, δ, and γ, respectively. PI3K/HDAC-IN-4 significantly induces tumor cell apoptosis by simultaneously inhibiting the PI3K/AKT/mTOR signaling pathway and HDAC1-3. PI3K/HDAC-IN-4 exhibits potent antiproliferative activity in a variety of tumor cell lines (e.g., MV4-11, Jeko-1, HL60, and MCF-7, with IC50 values of 0.2, 0.9, 0.8, and 1.5 μM, respectively). PI3K/HDAC-IN-4 can be used in the study of lymphoma and leukemia .
loading...
    loading...