Scientific Reviews
Product Guides
Blogs
Topics
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
3095 Results for "
Modulator
" in MedChemExpress (MCE) Product Catalog:
Products (3095)
3095 Results for "Modulator" in MCE Product Catalog:
Cat. No.: HY-175505
CAS No.: 2894793-37-2
Target:
Research Areas:
Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kd of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder .
Cat. No.: HY-176287
Target:
Research Areas:
ARN25657 is a dual-acting D3R/GSK-3β modulator. ARN25657 has both partial D3R agonist activity (EC50 = 15.2 nM, Ki =1.5 nM) and potent GSK-3β inhibitor activity (IC50 = 19.3 nM). ARN25657 exhibits excellent GSK-3β selectivity over FYN, PKA, and CDK5/p35. ARN25657 inhibits P-glycoprotein (P-gP)-mediated acetoxymethyl calcein efflux and improves in vitro ADME properties while maintaining a balanced dual-target profile. ARN25657 is useful for studying bipolar disorder and related neuropsychiatric disorders .
Cat. No.: HY-176561
CAS No.: 2421119-78-8
Target:
Research Areas:
IOR-160 is a dual inhibitor of casein kinase 2 (CK2) and HDACs. IOR-160 exhibits high selectivity for CK2 (IC50 = 1.7 nM) and broad inhibitory activity against HDAC (HDAC 1, 2, 3, and 6 with IC50s of 3.3 nM, 24.0 nM, 3.9 nM, and 13.0 nM, respectively, with low activity for HDAC8). IOR-160 modulates key cellular signaling pathways by inhibiting AKT phosphorylation and increasing acetylated α-tubulin. IOR-160 inhibits tumor growth and reduces tumor burden through dual CK2/HDAC inhibition. IOR-160 is indicated for use in triple-negative breast cancer research .
Cat. No.: HY-178041
CAS No.: 3106588-54-6
Research Areas:
BRD4-BD1/2-IN-3 (Compound B6) is a selective BRD4 BD2 inhibitor with an IC50 of 0.41 nM for BRD4 BD2 over BRD4 BD1. BRD4-BD1/2-IN-3 significantly inhibits the LPS (HY-D1056)-induced expression of IL-6. BRD4-BD1/2-IN-3 shows anti-inflammatory activities by modulating the TNF and NF-κB signaling pathway. BRD4-BD1/2-IN-3 can be used for inflammatory diseases research .
Cat. No.: HY-178053
CAS No.: 1191937-43-5
Research Areas:
AHR agonist 10 is a potent AHR agonist (EC50 = 2.01 nM). AHR agonist 10 can elevate the transcript levels of key AHR downstream pathway target genes, including CYP1A1 and CYP1B1. AHR agonist 10 can downregulate the expression levels of CD36, IL-18 and shows low cytotoxicity (>40 μM) to normal cells. AHR agonist 10 can suppress the expression of CCL5, CCL20, IL-6, IL-8, S100A9, TLR4, TNF-α, and TNFR1, demonstrating that AHR agonist 10 effectively modulate inflammatory responses through AHR dependent signaling pathways. AHR agonist 10 can be used for psoriasis research .
Cat. No.: HY-178169
CAS No.: 2773475-11-7
Research Areas:
ETI60 is an orally active, selective TLR inhibitor that targets the nucleoside-binding Site I on TLR7 (IC50 = 0.68 μM) and TLR9 (IC50 = 0.12 μM), sparing surface TLRs (including TLR1/TLR2, TLR2/TLR6, TLR4 and TLR5). ETI60 potently inhibits endosomal TLR-mediated pro-inflammatory signaling with nanomolar activity in cellular, biophysical and in vivo assays. ETI60 modulates the expression of genes associated with inflammation. ETI60 effectively ameliorates symptoms in mouse models of psoriasis, and systemic lupus erythematosus (SLE). ETI60 can be used for autoimmune and inflammatory diseases research .
Cat. No.: HY-178912
Research Areas:
Anti-MRSA agent 39 is an orally active ClpX modulator that binds Staphylococcus aureus caseinolytic protease X (SaClpX) with high affinity (Kd = 3.6 μM). Anti-MRSA agent 39 exerts antibacterial effects through temperature-dependent inhibition of cell division. Anti-MRSA agent 39 elicits profound metabolic dysregulation in methicillin-resistant Staphylococcus aureus (MRSA), manifesting as significantly reduced ATP levels, elevated reactive oxygen species (ROS), and decreased NAD+/NADH ratio, and accelerates bacterial lysis rates in MRSA ATCC 33591. Anti-MRSA agent 39 significantly increases the proportion of MRSA cells in the mitotic phase, and the cells exhibit obvious morphological abnormalities. Anti-MRSA agent 39 can be used for the study of invasive MRSA infections .
Cat. No.: HY-180400
CAS No.: 1426293-61-9
Target:
Research Areas:
PAM-2 is a potent, orally active, CNS-penetrant selective α7 nAChR positive allosteric modulator (human α7 nAChR EC50: 39 μM, rat α7 nAChR EC50: 12 μM) with anti-nociceptive and anti-inflammatory activity. PAM-2 exhibits selectivity over α9α10 nAChR (IC50 = 174 μM) and CaV2.2 channel (IC50 = 89 μM). PAM-2 decreases Streptozotocin (STZ) (HY-13753)- and Oxaliplatin (HY-17371)-inducned nuroparhic pain in mice by α7 nAChR potentiation. PAM-2 can be used for the research of neuropathic pain .
Cat. No.: HY-181606
Research Areas:
Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is a dual MDM2 and α5β1 integrin modulator. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 acts as an antiproliferative agent, apoptosis inducer and cell cycle regulator, induces reactivation of p53 and upregulation of p21, redistributes glioblastoma cells from the G0/G1 phase to the G2/M phase, and enhances apoptosis. Cyclo (phg-isoDGR-k)-PEG4-non-cleavable-SAR405838 is applicable to the research of glioblastoma .
Cat. No.: HY-181710
LASSBio-2337 is a dual pan-PI3K/mTOR inhibitor with an mTOR IC50 of 5.8 μM.LASSBio-2337 functionally modulates mTOR and all PI3K isoforms.LASSBio-2337 acts as a cytotoxic agent in leukemia cells, including multidrug-resistant populations.LASSBio-2337 spares nontumor human peripheral blood mononuclear cells.LASSBio-2337 displays moderate PAMPA-GIT permeability.LASSBio-2337 shows low metabolic stability in rat liver microsomes.LASSBio-2337 is aqueous insoluble.LASSBio-2337 can be used for the research of acute lymphoblastic leukemia, chronic myelogenous leukemia, breast cancer .
Cat. No.: HY-182722
CAS No.: 2388536-21-6
Target:
Research Areas:
UT-105 is an orally active, selective androgen receptor (AR) degrader. UT-105 binds to the N-terminal domain of AR, inhibits the transactivation of AR, blocks the recruitment of AR to androgen response elements, and induces AR degradation. UT-105 inhibits the JAK-STAT signaling pathway, including reducing the expression of interferon-stimulated genes, inhibiting the phosphorylation of STAT1 and STAT3, and blocking the recruitment of STAT1 to response elements. UT-105 exhibits anticancer activity against AR-positive triple-negative breast cancer (TNBC). UT-105 can be used in the research of selective androgen receptor modulator-resistant ER-positive breast cancer and triple-negative breast cancer .
Cat. No.: HY-183326
CAS No.: 2013542-44-2
Synonyms: IDMF
Target:
Research Areas:
Isosorbide di-(methyl fumarate) (IDMF), topical DMF (HY-17363) derivative, is an NRF2/ARE pathway activator. Isosorbide di-(methyl fumarate) downregulates ANCR targets, modulates epithelial differentiation, represses proinflammatory cytokine genes, IL-17A- and TNF-induced keratinocyte genes, psoriatic skin lesion-specific genes, and immune response genes. Isosorbide di-(methyl fumarate) stimulates oxidative stress response gene transcription, reduces erythema and scaling in Imiquimod (HY-B0180)-induced psoriasiform lesions. Isosorbide di-(methyl fumarate) exhibits no genotoxicity or radiation sensitivity in skin fibroblasts, is nonirritating and nonsensitizing in rodent models. Isosorbide di-(methyl fumarate) can be used for the research of psoriasis vulgaris .
Cat. No.: HY-183723
Research Areas:
GAA-4OH is a potent and irreversible dihydroceramide desaturase-1 (DES1) inhibitor with an IC50 of 0.6 μM and a Ki of 139.5 nM. GAA-4OH undergoes oxidation to form a reactive iminoquinone that covalently blocks DES1’s catalytic cavity, causing permanent enzyme inactivation. GAA-4OH modulates sphingolipid balance by reducing ceramide-to-dihydroceramide ratios in liver tissue. GAA-4OH improves liver steatosis, inflammation, fibrosis, and reduces pro-inflammatory and pro-fibrogenic gene expression. GAA-4OH can be used for the research of metabolic dysfunction-associated steatotic liver disease (MASLD) .
Cat. No.: HY-184654
CAS No.: 2169267-60-9
Target:
Synaptic Vesicle Proteins NF-κB ERK Akt HIF/HIF Prolyl-Hydroxylase Interleukin Related MyD88 TNF Receptor Caspase Formyl Peptide Receptor (FPR)
Research Areas:
MR-39 is a FPR2 agonist (EC50 = 3.9 μM). MR-39 activates FPR2 to promote neuroinflammation resolution (downregulates IL-1β and TNF-α, modulates NF-κB), upregulates synaptic proteins (synaptic proteins) and improves dendritic spine morphology. MR-39 inhibits MAPK/ERK and AKT phosphorylation in glioblastoma, induces S-phase arrest, and suppresses migration, angiogenesis, and hypoxic adaptation. MR-39 reduces Aβ plaque burden via inhibiting MyD88/NF-κB and NLRP3 inflammasome. MR-39 can be used for research on autism spectrum disorder, Alzheimer's disease, and glioblastoma .
Cat. No.: HY-185075
CAS No.: 3008577-34-9
Synonyms: LY4050784
Target:
Research Areas:
FHD-909 (LY4050784) is an orally active and selective SMARCA2 (BRM) ATPase inhibitor. FHD-909 potently inhibits purified BRM ATPase with an IC50 of 0.0025 μM and exhibits 35.69-fold selectivity for BRM over purified SMARCA4 (BRG1) ATPase. FHD-909 induces synthetic lethality, suppresses cell proliferation, modulates target gene expression, and achieves remarkable tumor growth inhibition and regression in SMARCA4-mutant cancer cells and xenograft models. FHD-909 can be used for the research of SMARCA4/BRG1-mutant cancers, advanced solid tumors, and BAF complex-related disorders .
Cat. No.: HY-188136
Target:
Research Areas:
ASO-4625 is a 20-nucleotide gapmer antisense oligonucleotide with a full phosphorothioate backbone and 2'-O-(2-methoxy) ethyl ribose modifications, which targets BCL2 mRNA and BCL2L1 mRNA. ASO-4625 downregulates Bcl-2 expression via an RNase H-dependent antisense mechanism with 100% complementarity, and downregulates Bcl-xL expression via the same mechanism with three mismatches. ASO-4625 induces Apoptosis and acts as a chemosensitizer. ASO-4625 does not significantly modulate the expression of Bcl-W, survivin, Akt, or p53 mRNA. ASO-4625 can be used in studies of breast cancer and non-small cell lung cancer .
Cat. No.: HY-189393
CAS No.: 3089177-97-6
Target:
Research Areas:
RTY-406 is an orally active ABCB4/MDR3 and ABCB11/BSEP positive modulator. RTY-406 increases ABCB4/MDR3 and ABCB11/BSEP protein levels and functional output, elevates biliary phospholipid levels, enhances bile acid efflux, increases bile flow and micelle formation, reduces hepatic bile acids, and promotes cholesterol-to-bile-acid conversion. RTY-406 does not induce hepatocellular injury, maintains normal serum alanine transaminase and aspartate aminotransferase levels, and shows a favorable safety profile in cynomolgus monkeys. RTY-406 can be used for the research of primary sclerosing cholangitis and cholestasis .
Cat. No.: HY-19888
CAS No.: 1001389-72-5
Target:
Research Areas:
GSK-1482160 is an orally active and blood-brain barrier penetrant P2X7 receptor (P2X7R) negative allosteric modulator with pIC50s of 8.5 (human) and 6.5 (rat). GSK-1482160 reduces the efficacy of ATP at the P2X7 receptor without affecting its affinity, thereby inhibiting the release of IL-1β. GSK-1482160 is an effective radioligand and can be labeled with radioactive isotopes like 11C or 18F to image P2X7R. GSK-1482160 can be used for the studies of chronic joint pain and chronic constriction injury (CCI) .
Cat. No.: HY-A0144AR
CAS No.: 943-17-9
Research Areas:
Etilefrine (Standard) is the analytical standard of Etilefrine. This product is intended for research and analytical applications. Etilefrine is a sympathetic nerve agonist and AMPK activator that selectively targets α1/β1 adrenergic receptors. Etilefrine stimulates α1 adrenergic receptors, leading to contraction of vascular smooth muscle and increased peripheral resistance. Etilefrine also stimulates β1 receptors to enhance myocardial contractility and increase heart rate, thereby increasing blood pressure and improving cardiac output. Etilefrine also bidirectionally regulates the AMPK/Akt pathway and modulates the phosphorylation levels. Etilefrine can be used in cardiovascular research, such as postural hypotension, chylothorax, and improving low cardiac output .
-
-
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
