1503 Results for "

antagonistic activity

" in MedChemExpress (MCE) Product Catalog:
Products (1503)

1503 Results for "antagonistic activity" in MCE Product Catalog:

158
158 Publications Verification
Cat. No.: HY-112693
CAS No.: 941987-60-6
Purity:  99.78%
Target:  

STING

Research Areas:  

Inflammation/Immunology

H-151 is a potent, selective and covalent antagonist of STING that has noteworthy inhibitory activity both in cells and in vivo. H-151 reduces TBK1 phosphorylation and suppresses STING palmitoylation. H-151 can be used for the research of autoinflammatory disease .
loading...
    loading...
120
120 Cited Publications
Cat. No.: HY-12684
CAS No.: 301326-22-7
Purity:  99.96%
Research Areas:  

Cancer

CH-223191 is a potent and specific antagonist of aryl hydrocarbon receptor (AhR). CH-223191 inhibits TCDD-mediated nuclear translocation and DNA binding of AhR, and inhibits TCDD-induced luciferase activity with an IC50 of 0.03 μM .
loading...
    loading...
66
66 Cited Publications
Cat. No.: HY-N0184
CAS No.: 1405-86-3
Synonyms: Glycyrrhizin
Glycyrrhizic acid is a triterpenoid saponinl, acting as a direct HMGB1 antagonist, with anti-tumor, anti-diabetic activities.
loading...
    loading...
59
59 Cited Publications
Cat. No.: HY-13004
CAS No.: 376348-65-1
Purity:  99.88%
Synonyms: UK-427857
Target:  

CCR HIV

Maraviroc (UK-427857) is a selective CCR5 antagonist with activity against human HIV.
loading...
    loading...
41
41 Cited Publications
Cat. No.: HY-N0219
CAS No.: 485-49-4
Synonyms: (+)-Bicuculline
Bicuculline ((+)-Bicuculline) is A competing neurotransmitter GABAA receptor antagonist (IC50=2 μM). Bicuculline also blocks Ca 2+ activating potassium (SK) channels and subsequently blocks slow post-hyperpolarization (slow AHP). Bicuculline has anticonvulsant activity. Bicuculline can be used to induce seizures in mice .
loading...
    loading...
30
30 Cited Publications
Cat. No.: HY-50674
CAS No.: 1262238-11-8
Target:  

CCR

INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
loading...
    loading...
28
28 Cited Publications
Cat. No.: HY-100001
CAS No.: 130495-35-1
Purity:  ≥99.01%
SKF-96365 hydrochloride is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 hydrochloride reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 hydrochloride inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 hydrochloride inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 hydrochloride induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 hydrochloride alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 hydrochloride reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 hydrochloride inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 hydrochloride is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
loading...
    loading...
28
28 Cited Publications
Cat. No.: HY-125942
CAS No.: 162849-90-3
SKF-96365 is a TRPC channel antagonist and store-operated calcium entry (SOCE) inhibitor. SKF-96365 reduces calcium ion influx by inhibiting the activity and expression of TRPC6, STIM1 and Orai1. SKF-96365 inhibits voltage-gated sodium current (cardiac INa/NaV1.5) and slows myocardial conduction. SKF-96365 inhibits phosphorylation/activation of CaMKIIγ and suppresses the downstream AKT signaling pathway. SKF-96365 induces G2/M phase cell cycle arrest, apoptosis and cytoprotective autophagy in colorectal cancer cells. SKF-96365 alleviates allergic rhinitis symptoms by reducing inflammatory cytokine levels. SKF-96365 reduces intracellular calcium overload, inhibits Homer1 expression, prevents nuclear damage and suppresses apoptosis. SKF-96365 inhibits the growth of colorectal cancer xenografts in nude mice . SKF-96365 is applicable to research related to allergic rhinitis, colorectal cancer, Parkinson's disease, persistent spontaneous nociception and hyperalgesia .
loading...
    loading...
23
23 Cited Publications
Cat. No.: HY-15068
CAS No.: 118876-58-7
Purity:  99.82%
Synonyms: FG9202
Target:  

iGluR

Research Areas:  

Neurological Disease

NBQX (FG9202) is a highly selective and competitive AMPA receptor antagonist. NBQX has neuroprotective and anticonvulsant activity .
loading...
    loading...
23
23 Cited Publications
Cat. No.: HY-15068A
CAS No.: 479347-86-9
Purity:  98.00%
Synonyms: FG9202 disodium
Target:  

iGluR

Research Areas:  

Neurological Disease

NBQX disodium (FG9202 disodium) is a highly selective and competitive AMPA receptor antagonist. NBQX disodium has neuroprotective and anticonvulsant activity .
loading...
    loading...
20
20 Cited Publications
Cat. No.: HY-N0382
CAS No.: 548-83-4
Synonyms: Norizalpinin; 3,5,7-Trihydroxyflavone
Galangin (Norizalpinin) is an agonist/antagonist of the arylhydrocarbon receptor. Galangin (Norizalpinin) also shows inhibition of CYP1A1 activity.
loading...
    loading...
19
19 Cited Publications
Cat. No.: HY-100506
CAS No.: 1320346-97-1
Purity:  99.43%
Target:  

Integrin

Research Areas:  

Cancer

GLPG0187 is a broad spectrum integrin receptor antagonist with antitumor activity; inhibits αvβ1-integrin with an IC50 of 1.3 nM . GLPG0187 inhibits migrasome biogenesis without cytotoxicity .
loading...
    loading...
18
18 Cited Publications
Cat. No.: HY-101254
CAS No.: 117946-91-5
Purity:  100.0%
Synonyms: N-0774
Target:  

Melatonin Receptor

Research Areas:  

Neurological Disease

Luzindole (N-0774) is a selective melatonin receptor antagonist. Luzindole preferentially targets MT2 (Mel1b) over MT1 (Mel1a) with Ki values of 10.2 and 158 nM for human MT2 and MT1, respectively. Luzindole suppresses experimental autoimmune encephalomyelitis (EAE), and exerts antidepressant-like activity .
loading...
    loading...
18
18 Cited Publications
Cat. No.: HY-P0299
CAS No.: 283609-79-0
Target:  

TGF-β Receptor

Research Areas:  

Cancer

LSKL, Inhibitor of Thrombospondin (TSP-1) is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) can readily crosse the blood-brain barrier .
loading...
    loading...
18
18 Cited Publications
Cat. No.: HY-P0299A
CAS No.: 2828433-17-4
Target:  

TGF-β Receptor

Research Areas:  

Cancer

LSKL, Inhibitor of Thrombospondin (TSP-1) TFA is a latency-associated protein (LAP)-TGFβ derived tetrapeptide and a competitive TGF-β1 antagonist. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA inhibits the binding of TSP-1 to LAP and alleviates renal interstitial fibrosis and hepatic fibrosis. LSKL, Inhibitor of Thrombospondin (TSP-1) TFA suppresses subarachnoid fibrosis via inhibition of TSP-1-mediated TGF-β1 activity, prevents the development of chronic hydrocephalus and improves long-term neurocognitive defects following subarachnoid hemorrhage (SAH). LSKL, Inhibitor of Thrombospondin (TSP-1) TFA can readily crosse the blood-brain barrier .
loading...
    loading...
17
17 Cited Publications
Cat. No.: HY-14415
CAS No.: 1254944-66-5
Purity:  99.94%
Target:  

REV-ERB

SR8278 is a REV-ERBα antagonist and inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47 μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm. SR8278 also can be used for the research of Duchenne muscular dystrophy and Alzheimer's disease .
loading...
    loading...
17
17 Cited Publications
Cat. No.: HY-108357
CAS No.: 157-03-9
Purity:  99.98%
Synonyms: L-6-Diazo-5-oxonorleucine; DON
6-Diazo-5-oxo-L-nor-Leucine (L-6-Diazo-5-oxonorleucine; DON) is a glutamine antagonist that irreversibly inhibits the catabolic effect of glutamine. 6-Diazo-5-oxo-L-nor-Leucine shows good anticancer activity (especially in pancreatic cancer) and reduces the self-renewal potential and metastatic capacity of tumour cells. 6-Diazo-5-oxo-L-nor-Leucine also possesses antibacterial and antiviral activity .
loading...
    loading...
16
16 Cited Publications
Cat. No.: HY-101106
CAS No.: 80306-38-3
Purity:  99.38%
Target:  

RAR/RXR

Research Areas:  

Neurological Disease Cancer

AR7 is an atypical RARA/RARα (retinoic acid receptor, alpha) antagonist. AR7 specifically activates chaperone-mediated-autophagy (CMA) activity without affecting macroautophagy .
loading...
    loading...
16
16 Cited Publications
Cat. No.: HY-126010
CAS No.: 2253744-54-4
Purity:  99.93%
Target:  

Piezo Channel

Research Areas:  

Others

Dooku1 is a reversibly Yoda1 antagonist with IC50 value of 1.3 μM and 1.5 μM for 2 μM Yoda1-induced Ca 2+ entry HEK 293 cells and HUVECs, respectively. Dooku1 can disrupt Yoda1-induced Piezo1 channel activity and inhibit Yoda1-induced relaxation of aorta. Dooku1 can be used for vascular physiology and disease research .
loading...
    loading...
16
16 Cited Publications
Cat. No.: HY-14564A
CAS No.: 156223-05-1
Purity:  99.65%
Synonyms: DMXB-A; DMBX-anabaseine
Target:  

nAChR 5-HT Receptor

Research Areas:  

Inflammation/Immunology

GTS-21 dihydrochloride is a selective alpha7 nicotinic acetylcholine receptor (α7-nAChR) agonist with anti inflammatory and cognition enhancing activities. GTS-21 dihydrochloride is also a α4β2 (Ki=20 nM for humanα4β2) and 5-HT3A receptor (IC50=3.1 μM) antagonist .
loading...
    loading...