Search Result
Results for "
attenuation
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
19
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-157014
-
|
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Tryptophan Hydroxylase
|
Cancer
|
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TPT-004 is a TPH inhibitor. TPT-004 has superior pharmacokinetic and pharmacodynamic properties. TPT-004 also has good efficacy in preclinical models of peripheral serotonin attenuation and colorectal tumor growth .
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-
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- HY-112780
-
UC2288
5 Publications Verification
|
MDM-2/p53
Apoptosis
|
Cancer
|
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UC2288 is a potent and orally active p21 attenuator (relatively selective activity for p21), which is synthesized based Sorafenib (HY-10201). UC2288 potently inhibits cancer cell growth by inducing apoptosis. UC2288 has no inhibition of VEGFR2 and Raf kinases even at 10 μM .
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-
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- HY-N3349
-
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Others
|
Others
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Lyoniresinol is a lignan isolated from the Tarenna attenuata with antioxidant activities. Lyoniresinol has radical scavenging activities against DPPH with an IC50 of 82.4 μM .
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-
-
- HY-B1010
-
-
-
- HY-125096
-
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Glucocorticoid Receptor
|
Metabolic Disease
Inflammation/Immunology
|
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C108297 is a selective glucocorticoid receptor (GR) modulator (GR binding Ki 0.7 nM; GR reporter gene functional Ki 0.6 nM). C108297 attenuates obesity by reducing caloric intake and increasing lipolysis and fat oxidation, and in addition attenuates inflammation .
|
-
-
- HY-125850
-
-
-
- HY-162050
-
|
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Sirtuin
|
Neurological Disease
|
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8AQ?Cu?5Iu is an activator of SIRT1. 8AQ?Cu?5Iu exhibits neuroprotective effects by
modulating the SIRT1/3-FOXO3a signaling pathway. 8AQ?Cu?5Iu can used in study attenuating neurodegenerative diseases .
|
-
-
- HY-W728005
-
|
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SARS-CoV
|
Infection
|
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Covidcil-19 (compound C5) avidly binds to the revised attenuator hairpin structure of the SARS-CoV-2 frameshifting element (FSE) with a Kd of 11 nM. Covidcil-19 stabilizes the hairpin’s folded state and impairs frameshifting in cells. Covidcil-19 reduces frameshifting efficiency of the SARS-CoV-2 FSE and does not affect SARS-CoV-2 FSE RNA levels. Covidcil-19 inhibits a process essential for SARS-CoV-2 viral propagation .
|
-
-
- HY-N3349A
-
|
|
Reactive Oxygen Species
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Others
|
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(-)-Lyoniresinol is a lignan isolated from the Tarenna attenuata with antioxidant activities. (-)-Lyoniresinol has radical scavenging activities against DPPH with an IC50 of 82.4 μM .
|
-
-
- HY-156972
-
|
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Opioid Receptor
|
Metabolic Disease
|
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NOP agonist-1(compound 4) is a nociceptin opioid receptor (NOP) partial agonist. NOP agonist-1attenuate parkinsonian disabilities in 6-OHDA hemilesioned rats .
|
-
-
- HY-18649B
-
|
BCX4430 dihydrochloride; Immucillin-A dihydrochloride
|
Flavivirus
|
Infection
|
|
Galidesivir (BCX4430; Immucillin-A) dihydrochloride is a broad-spectrum RNA virus inhibitor that can inhibit Ebola and yellow fever virus (Flavivirus) infections. Galidesivir has potent antiviral activity against tick-borne encephalitis virus (TBEV) and also inhibits the proliferation of many other medically important flaviviruses .
|
-
-
- HY-P1020
-
-
-
- HY-N7019
-
|
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Others
|
Cancer
|
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19-Hydroxybufalin is a bufadienolide, inhibits epithelial-mesenchymal transition and attenuates the migration and invasion of PC3 cells .
|
-
-
- HY-P1020A
-
-
-
- HY-139703
-
|
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Others
|
Inflammation/Immunology
|
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Se-DMC attenuates complete Freund’s adjuvant (CFA)-induced inflammatory response, nociception, and neurobehavioral deficits in mice.
|
-
-
- HY-139678
-
|
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Opioid Receptor
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Others
|
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SC13 is a novel mitragynine analog with low-efficacy Mu opioid receptor agonism that displays antinociception with attenuated adverse effects.
|
-
-
- HY-N10386
-
-
-
- HY-N1302
-
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Apoptosis
|
Cancer
|
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Shizukaol D is a dimeric sesquiterpene isolated from Chloranthus serratus. Shizukaol D induces apoptosis and attenuated Wnt signalling .
|
-
-
- HY-P3434
-
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Pyroptosis
|
Inflammation/Immunology
|
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Ac-FEID-CMK is a potent zebrafish-specific GSDMEb-derived peptide inhibitor.
Ac-FEID-CMK can attenuate the mortality and kidney injury during septic shock. Ac-FEID-CMK inhibits pyroptosis and attenuates septic AKI (acute kidney injury) in vivo. Ac-FEID-CMK can suppress the caspy2-mediated noncanonical inflammasome pathway .
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-
-
- HY-P0237
-
|
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Kallikrein
|
Cancer
|
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KKI-5 is a specific inhibitor of tissue kallikrein. KKI-5 can attenuate breast cancer cell invasion .
|
-
-
- HY-121188
-
|
Dibromo-dodecenyl-methylsulfimide
|
Cytochrome P450
|
Cardiovascular Disease
|
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DDMS (Dibromo-dodecenyl-methylsulfimide) is a selective 20-HETE production inhibitor. DDMS attenuates the vasodilatory response to sodium nitroprusside (SNP) .
|
-
-
- HY-N10359
-
-
-
- HY-137863
-
|
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Others
|
Inflammation/Immunology
|
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Pemirolast is an orally active antiallergic agent. Pemirolast attenuates paclitaxel hypersensitivity reactions, can be used for bronchial asthma and conjunctivitis research - .
|
-
-
- HY-P3434A
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
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Ac-FEID-CMK TFA is a potent zebrafish-specific GSDMEb-derived peptide inhibitor.
Ac-FEID-CMK TFA can attenuate the mortality and kidney injury during septic shock. Ac-FEID-CMK TFA inhibits pyroptosis and attenuates septic AKI (acute kidney injury) in vivo. Ac-FEID-CMK TFA can suppress the caspy2-mediated noncanonical inflammasome pathway .
|
-
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- HY-N3196
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
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Neotuberostemonine, one of the main antitussive alkaloids in the root of Stemona tuberosa Lour, attenuates bleomycin-induced pulmonary fibrosis by suppressing the recruitment and activation of macrophages .
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-
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- HY-P0237A
-
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Kallikrein
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Cancer
|
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KKI-5 (TFA) is a specific inhibitor of tissue kallikrein. KKI-5 (TFA) can attenuate breast cancer cell invasion .
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-
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- HY-N0663
-
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Potassium Channel
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Neurological Disease
|
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Talatisamine, a aconitum alkaloid, is specific K + channel blocker. Talatisamine attenuates beta-amyloid oligomers induced neurotoxicity in cultured cortical neurons .
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-
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- HY-111064
-
-
-
- HY-W014102
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-
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- HY-129531
-
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Others
|
Neurological Disease
|
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MuRF1-IN-1 is a muscle ring finger 1 (MuRF1) inhibitor that attenuates skeletal muscle atrophy and dysfunction in cardiac cachexia .
|
-
-
- HY-N10119
-
|
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p38 MAPK
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Neurological Disease
|
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Ganoderterpene A attenuates LPS-induced inflammation and apoptosis via suppressing MAPK and TLR-4/NF-κB pathways in BV-2 cells.
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-
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- HY-121441
-
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Estrogen Receptor/ERR
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Inflammation/Immunology
|
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Fispemifene, an orally active selective estrogen receptor modulator with anti-inflammatory and antiestrogenic action, attenuates glandular inflammation in an animal model of chronic nonbacterial prostatitis .
|
-
-
- HY-125850R
-
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Drug Metabolite
|
Inflammation/Immunology
|
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Berberrubine (chloride) (Standard) is the analytical standard of Berberrubine (chloride). This product is intended for research and analytical applications. Berberrubine chloride is an active metabolite of berberine, attenuates ulcerative colitis in mice model .
|
-
-
- HY-110152
-
|
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mGluR
|
Neurological Disease
|
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LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
-
- HY-N0474
-
-
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- HY-125169
-
|
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Autophagy
Atg4
|
Cancer
|
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NSC 185058 is an inhibitor of ATG4B, a major cysteine protease. Inhibition of ATG4B using NSC 185058 markedly attenuates autophagic activity .
|
-
-
- HY-121239
-
|
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NF-κB
|
Neurological Disease
Inflammation/Immunology
Cancer
|
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Lemnalol is a potent agent for neuropathic pain. Lemnalol possesses potent anti-inflammatory, analgesic and anti-tumor activities. Lemnalol has the capacity to attenuate hyperalgesia and allodynia by modulation of neuroinflammatory processes in neuropathy. Lemnalol modulates LPS-induced alterations of left atrial (LA) calcium homeostasis and blocks the NF-κB pathways, which may contribute to the attenuation of lipopolysaccharide (LPS)-induced arrhythmogenesis and neuropathic pain. Lemnalolis a ylangene-type sesquiterpenoid compound, isolated from Lemnalia cervicorni .
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-
-
- HY-114368A
-
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AMG-18 Hydrochloride
|
IRE1
|
Inflammation/Immunology
|
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Kira8 Hydrochloride (AMG-18 Hydrochloride) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
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-
-
- HY-114368
-
|
AMG-18
|
IRE1
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Inflammation/Immunology
|
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Kira8 (AMG-18) is a mono-selective IRE1α inhibitor that allosterically attenuates IRE1α RNase activity with an IC50 of 5.9 nM .
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-
-
- HY-108564
-
|
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Prostaglandin Receptor
|
Cardiovascular Disease
|
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L 655240 is thromboxane antagonist. L 655240 attenuates early ischemia- and reperfusion-induced arrhythmias in a canine model of coronary artery occlusion. L 655240 also involves in cancer and autoimmune disorders .
|
-
-
- HY-103290
-
|
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Bradykinin Receptor
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Others
|
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R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
-
- HY-131929
-
|
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NO Synthase
|
Inflammation/Immunology
|
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AE-ITU dihydrobromide is the dihydrobromide form of AE-ITU. AE-ITU dihydrobromide is a selective inhibitor for inducible NO synthase (iNOS), and attenuates the liver dysfunction caused by endotoxaemia in rats .
|
-
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- HY-139373
-
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5-Methyl-2-HOBA hydrochloride
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Angiotensin Receptor
|
Cardiovascular Disease
|
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2-(Aminomethyl)-4-methylphenol (5-methyl-2-HOBA) hydrochloride is an isoketal scavenger that attenuates the hypertensive response to angiotensin II .
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- HY-12212
-
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RTA 408
|
Keap1-Nrf2
STING
Apoptosis
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Inflammation/Immunology
Cancer
|
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Omaveloxolone (RTA 408) is an antioxidant inflammation modulator (AIM), which activates Nrf2 and suppresses nitric oxide (NO). Omaveloxolone attenuates osteoclastogenesis by inhibiting STING dependent NF-κb signaling.
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-
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- HY-101455
-
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Calcium Channel
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Metabolic Disease
|
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CDN1163 is an allosteric sarco/endoplasmic reticulum Ca 2+-ATPase (SERCA) activator that improves Ca 2+ homeostasis. CDN1163 attenuates diabetes and metabolic disorders .
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-
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- HY-128578
-
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PDHK
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Metabolic Disease
Inflammation/Immunology
|
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KPLH1130 is a specific pyruvate dehydrogenase kinase (PDK) inhibitor, blocks macrophage polarization and attenuates proinflammatory responses. KPLH1130 improves glucose tolerance in HFD-fed mice .
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-
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- HY-N6673
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-
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- HY-N0341
-
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Sirtuin
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Metabolic Disease
|
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Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots . Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades .
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-
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- HY-N1109
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Uvaol
1 Publications Verification
|
Endogenous Metabolite
|
Inflammation/Immunology
|
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Uvaol, a triterpene present in olives and virgin olive oil, possesses anti-inflammatory properties and antioxidant effects. Uvaol attenuates pleuritis and eosinophilic inflammation in ovalbumin-induced allergy in mice .
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-
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- HY-113556
-
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NF-κB
Keap1-Nrf2
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Inflammation/Immunology
|
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Sappanone A is a homoisoflavanone which exhibits anti-inflammatory effects via modulation of Nrf2 and NF-κB. Sappanone can attenuate allergic airway inflammation in Ovalbumin-induced asthma .
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- HY-P10312
-
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GLP Receptor
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Metabolic Disease
|
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SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC50 of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models .
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- HY-164451
-
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γ-secretase
Notch
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Cancer
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GSI-18 is a γ-secretase inhibitor with anticancer activity. GSI-18 attenuates anchorage-independent growth in pancreatic cancer cells by inhibiting Notch signaling .
|
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- HY-10081
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GS-6201
1 Publications Verification
CVT-6883
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Adenosine Receptor
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Inflammation/Immunology
|
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GS-6201 (CVT-6883) is a selective adenosine A2B receptor antagonist. GS-6201 displays high affinity and selectivity for the human adenosine A2B receptors (Ki=22 nM) . GS-6201 reduces caspase-1 activity in the heart, and attenuates cardiac remodeling after acute myocardial infarction (AMI) in the mouse . GS-62013 attenuates the airway reactivity induced by NECA, AMP, or allergen in sensitized mice .
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- HY-119304
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-
- HY-101848
-
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Fungal
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Infection
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Latrunculin B, an antimicrobial marine alkaloid, is an actin polymerization inhibitor. Latrunculin B regulates pulmonary vein electrophysiological characteristics and attenuates stretch-induced arrhythmogenesis. Antifungal and antiprotozoal activity .
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- HY-N8152
-
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Reactive Oxygen Species
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Inflammation/Immunology
|
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Randialic acid B, a triterpenoid compound, is a formyl peptide receptor 1 (FPR1) antagonist. Randialic acid B blocks FPR1 in human neutrophils and attenuates psoriasis-like inflammation in vivo .
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-
- HY-112248A
-
-
- HY-123856
-
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Phosphatase
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Neurological Disease
|
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MY10 is a potent and orally active receptor protein tyrosine phosphatase (RPTPβ/ζ) inhibitor. MY10 attenuates binge-like ethanol consumption and ethanol reward .
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-
- HY-N1151
-
-
- HY-P5888
-
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Myr‐PKCɛ-
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PKC
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Inflammation/Immunology
|
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PKCε inhibitor peptide,myristoylated (Myr‐PKC -) is a cell permeable myristic acid conjugated PKC peptide inhibitor that attenuates NO release in cultured human umbilical vein endothelial cells (HUVECs) .
|
-
- HY-129738
-
|
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Others
|
Cardiovascular Disease
|
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I942 is a first in class, selective non-cyclic nucleotide (NCN) EPAC1 agonist. I942 can attenuate proinflammatory cytokine signalling normally associated with cardiovascular diseases .
|
-
- HY-P4201
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
|
-
- HY-162605
-
|
|
STAT
HSP
|
Cancer
|
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CYD0682 is an analog of Oridonin (HY-N0004). CYD0682 attenuates STAT3 activation and ECM production via an HSP90 pathway in hepatic stellate cells .
|
-
- HY-138233
-
|
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p97
|
Neurological Disease
Inflammation/Immunology
|
|
KUS121, a valosin-containing protein (VCP, p97) modulator with significant neuroprotective effects, attenuates ischemic retinal cell death via suppressing endoplasmic reticulum stress .
|
-
- HY-B1078
-
-
- HY-108531
-
|
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RAR/RXR
|
Cancer
|
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ER-50891 is a potent antagonist of retinoic acid receptor α(RARα). ER-50891 significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis .
|
-
- HY-146706
-
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Bacterial
|
Infection
|
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PqsR-IN-2 (Compound 19) is a potent PqsR (Pseudomonas aeruginosa quorum sensing transcriptional regulator) inhibitor. PqsR-IN-1 attenuates pyocyanin production and has very low cytotoxicity .
|
-
- HY-146705
-
|
|
Bacterial
|
Infection
|
|
PqsR-IN-1 (Compound 18) is a potent PqsR (Pseudomonas aeruginosa quorum sensing transcriptional regulator) inhibitor. PqsR-IN-1 attenuates pyocyanin production and has very low cytotoxicity .
|
-
- HY-118694
-
-
- HY-108531A
-
|
|
RAR/RXR
|
Cancer
|
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ER 50891 quarterhydrate is a potent antagonist of retinoic acid receptor α(RARα). ER 50891 quarterhydrate significantly attenuates ATRA's inhibitive effects on BMP 2-induced osteoblastogenesis .
|
-
- HY-N1546
-
|
|
Others
|
Inflammation/Immunology
|
|
Protoplumericin A is a bioactive ingredient of Plumeria obtusa L. attenuates. Protoplumericin A mitigated lipopolysaccharide (LPS) -induced acute lung injury in mice. Protoplumericin A can be used to study the LPS-induced anti-inflammatory effect .
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-
- HY-N12740
-
|
|
MEK
ERK
|
Others
|
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Napyradiomycin B4 is a Napyradiomycin derivative, which inhibits the RANKL-induced MEK-ERK signaling pathway. Napyradiomycin B4 attenuates osteoclastogenesis and prevents alveolar bone destruction in experimental periodontitis .
|
-
- HY-105094
-
|
NC 1300O3
|
Na+/K+ ATPase
|
Inflammation/Immunology
|
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Leminoprazole (NC 1300O3) is an inhibitor for acid pump, H + K +-ATPase,. Leminoprazole stimulates the secretion and synthesis of gastric mucus, attenuates gastric ulcers. Leminoprazole is orally active .
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-
- HY-163482
-
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Parasite
|
Infection
|
|
ELQ-596 is a quinolone derivative, that exhibits antimicrobial activity against several protozoan parasites, including the intraerythrocytic parasites Plasmodium and Babesia. ELQ-596 attenuates babesiosis in immunosuppressed mice .
|
-
- HY-163484
-
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Parasite
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Infection
|
|
ELQ-650 is a quinolone derivative, that exhibits antimicrobial activity against several protozoan parasites, including the intraerythrocytic parasites Plasmodium and Babesia. ELQ-650 attenuates babesiosis in immunosuppressed mice .
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-
- HY-B1892
-
-
- HY-N3883
-
|
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Autophagy
|
Neurological Disease
Cancer
|
|
Euxanthone, a xanthone derivative, attenuates Aβ1-42-induced oxidative stress and apoptosis by triggering autophagy. Euxanthone exhibits anti-neoplastic and neuroprotective activities .
|
-
- HY-E70008
-
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Sirtuin
|
Inflammation/Immunology
|
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Lumbokinase attenuates myocardial ischemia-reperfusion (I-R) injury through the activation of Sirt1 signaling, and thus enhances autophagic flux and reduces I-R-induced oxidative damage, inflammation and apoptosis .
|
-
- HY-153675
-
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PIN1
|
Metabolic Disease
|
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BCPA is a Pin1 regulator without cytotoxicity. BCPA attenuates the reduction of Pin1 protein to inhibit receptor activator of RANKL-induced osteoclastogenesis. BCPA regulates osteoclast activation, used to osteoporosis research .
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-
- HY-155205
-
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Cholecystokinin Receptor
|
Neurological Disease
|
|
GV150013X is an antagonist for cholecystokinin-2/gastrin receptor (CCK2R), with Ki of 2.29 nM. GV150013X attenuates central nervous disorders, such as anxiety and panic disorder .
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-
- HY-144026S
-
-
- HY-100080
-
|
|
Sodium Channel
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Neurological Disease
|
|
A-887826 is a potent, selective, oral bioavailable and voltage-dependent Na(v)1.8 sodium channel blocker with an IC50 of 11 nM . A-887826 attenuates neuropathic tactile allodynia in vivo .
|
-
- HY-N7126
-
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Potassium Channel
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Neurological Disease
|
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Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K ⁺ channel pathway .
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-
- HY-N2477
-
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Apoptosis
NF-κB
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Inflammation/Immunology
Cancer
|
|
Taraxerol is isolated from Taraxacum mongolicum, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis .
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-
- HY-107627
-
|
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Melanocortin Receptor
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Inflammation/Immunology
|
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MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
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-
- HY-123506
-
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Src
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Neurological Disease
Inflammation/Immunology
|
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Fenlean, a natural squamosamide derivative, is a Src tyrosine kinase inhibitor. Fenlean can inhibit over-activated microglia and protect dopaminergic neurons. Fenlean can attenuate neuroinflammation in Parkinson's disease models .
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-
- HY-B0756
-
-
- HY-N9487
-
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(-)-α-Phellandrene
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
(R)-(-)-α-Phellandrene ((-)-α-Phellandrene) is an the (R)-(-)-stereoisomer of α-phellandrene. α-phellandrene is an orally active cyclic monoterpene that attenuates inflammatory response, and induces DNA damage .
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-
- HY-107505
-
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mGluR
|
Neurological Disease
|
|
CBiPES hydrochloride is a mGlu2 receptor positive allosteric modulator (EC50: 92.8 nM). CBiPES hydrochloride attenuates stress-induced hyperthermia and PCP-induced hyperlocomotor activity. CBiPES hydrochloride can be used for research of neurological disease .
|
-
- HY-154795
-
|
|
Caspase
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
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Magnesium isoglycyrrhizinate hydrate is the active component found in licorice plant (Glycyrrhiza glabra). Magnesium isoglycyrrhizinate hydrate exhibits anti-inflammatory activity through NLRP3 inflammasome pathway, and attenuates the chronic obstructive pulmonary disease in rats .
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-
- HY-P99842A
-
|
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TNF Receptor
|
Inflammation/Immunology
|
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Dapirolizumab is a monoclonal antibodi against CD40 ligand. Dapirolizumab targets CD40L, blocks its interaction with CD40 receptors, and inhibits adaptive immune activation. Dapirolizumab attenuates systemic lupus erythematosus .
|
-
- HY-W062702
-
|
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nAChR
|
Neurological Disease
|
|
BMS-933043 is a potent and selective α7 nACh receptor partial agonist. BMS-933043 attenuates the cognitive impairment in mice and can be utilized in research related to cognitive dysfunction in schizophrenia .
|
-
- HY-B0661A
-
-
- HY-W015422
-
|
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PARP
|
Metabolic Disease
|
|
1,5-Isoquinolinediol is a potent PARP inhibitor, with an IC50 of 0.18-0.37 μM. 1,5-Isoquinolinediol attenuates diabetes-induced NADPH oxidase-derived oxidative stress in retina .
|
-
- HY-N0608
-
|
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NF-κB
|
Inflammation/Immunology
|
|
Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation .
|
-
- HY-122049
-
-
- HY-107505A
-
|
|
mGluR
|
Neurological Disease
|
|
CBiPES is a potent mGlu2 positive allosteric modulator with an EC50 value of 92.8 nM. CBiPES attenuates stress-induced hyperthermia and Phencyclidine-induced hyperlocomotor activity. CBiPES can be used for research of neurological diseases .
|
-
- HY-121007
-
|
Web2170
|
Others
|
Others
|
|
Bepafant (Web2170) is a platelet-activating factor (PAF) antagonist that protects against anaphylactic lethality in active and passive anaphylaxis models in mice and guinea pigs in a dose-dependent manner and attenuates bronchoconstriction and blood pressure changes in anaphylaxis.
|
-
- HY-19589
-
-
- HY-108647
-
|
|
p38 MAPK
|
Inflammation/Immunology
|
|
EO 1428 is a highly specific inhibitor of p38 of the aminobenzophenone class. EO 1428 (1 μM ) markedly attenuates LPS-induced tumor necrosis factor α-converting enzyme (TACE) activity up-regulation .
|
-
- HY-162325
-
-
- HY-116033
-
|
|
Ser/Thr Protease
|
Inflammation/Immunology
|
|
BMS-363131 is a selective inhibitor for tryptase, with an IC50 <1.7 nM. BMS-363131 is hydrolytic stable at pH=7 and pH=9. BMS-363131 attenuates the astham in a guinea pig model .
|
-
- HY-13708
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
SUN C5174 is an antagonist for 5-HT2 receptor with a mild sympathomimetic efficacy. SUN C5174 attenuates disorders in various experimental models of peripheral circulatory disturbance, and exhibits good pharmacokinetic properties .
|
-
- HY-111256
-
|
|
mGluR
|
Neurological Disease
|
|
A-850002 is a metabotropic glutamate receptor (mGluR) antagonist (IC50=27 nM) that significantly attenuates spontaneous pain behavior after skin incision in rats. A-850002 can be used for analgesia research .
|
-
- HY-W018791
-
|
DDB
|
HBV
Autophagy
Cytochrome P450
Atg8/LC3
p62
P-glycoprotein
|
Infection
Cardiovascular Disease
Cancer
|
|
Bifendate (DDB), extracted from Schisandrae chinensis, is an orally active anti-HBV agent against chronic hepatitis B. Bifendate inhibits ATG5-dependent autophagy and attenuates oleic acid-induced lipid accumulation with anti-oxidant properties in vitro. Bifendate can decrease alanine transaminase (ALT) level in mice. Bifendate attenuates hepatic steatosis in cholesterol/bile salt- and high-fat diet-induced hypercholesterolemia in mice. Bifendate potently increases the activity of cytochrome proteins (CYPs) and reverse P-gp-mediated multi-drug resistance (MDR) .
|
-
- HY-B0661
-
-
- HY-P1010
-
|
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-W014941
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats .
|
-
- HY-151392
-
|
|
Others
|
Neurological Disease
Inflammation/Immunology
|
|
LPA5 antagonist 2 (compound 65) is a high aqueous solubility LPA5 (lysophosphatidic acid receptor 5) antagonist. LPA5 antagonist 2 significantly attenuates nociceptive hypersensitivity and it can be used for the research of inflammatory and neuropathic pains .
|
-
- HY-B0149
-
|
cyclocapron
|
IGF-1R
AMPK
MMP
Mitophagy
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Tranexamic acid (cyclocapron), a cyclic analog of lysine, is an orally active antifibrinolytic agent. Tranexamic acid attenuates the effects of severe trauma, inhibits urokinase plasminogen activator and ameliorates dry wrinkles. Tranexamic acid can used for the research of hemostasis .
|
-
- HY-N0595
-
|
Genistine; Genistoside; Genistein 7-O-β-D-glucopyranoside
|
Estrogen Receptor/ERR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway .
|
-
- HY-103243
-
TCPOBOP
3 Publications Verification
|
Bcl-2 Family
|
Cancer
|
|
TCPOBOP is a constitutive androstane receptor (CAR) agonist that induces robust hepatocyte proliferation and hepatomegaly without any liver injury or tissue loss . TCPOBOP attenuates Fas-induced murine liver injury by altering Bcl-2 proteins .
|
-
- HY-N0608A
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
(Rac)-Myrislignan is the racemate of Myrislignan. Myrislignan, a lignan isolated from Myristica fragrans Houtt, possesses anti-inflammatory activities. Myrislignan attenuates LPS-induced inflammation reaction in murine macrophage cells through inhibition of NF-kB signalling pathway activation .
|
-
- HY-110067
-
-
- HY-153723
-
|
|
Ras
|
Cancer
|
|
BI-2493 is a structural analogue of BI-2865 and a highly selective and orally active pan-KRAS inhibitor. BI-2493 can attenuate tumor growth. BI-2493 can be used for cancer iseases research .
|
-
- HY-145721A
-
|
GED-0301 sodium
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice .
|
-
- HY-N0474R
-
|
|
NF-κB
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Tyrosol (Standard) is the analytical standard of Tyrosol. This product is intended for research and analytical applications. Tyrosol is a derivative of phenethyl alcohol. Tyrosol attenuates pro-inflammatory cytokines from cultured astrocytes and NF-κB activation. Anti-oxidative and anti-inflammatory effects .
|
-
- HY-A0143
-
-
- HY-100999
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats .
|
-
- HY-P1010A
-
|
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-13706A
-
|
TM30089
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
CAY10471 (TM30089) is a potent, selective, and orally active prostaglandin D2 receptor CRTH2 antagonist. CAY10471 attenuates the progression of tubulointerstitial fibrosis and chronic contact hypersensitivity (CHS) in animal model .
|
-
- HY-138936
-
SSK1
1 Publications Verification
|
p38 MAPK
Apoptosis
|
Inflammation/Immunology
|
|
SSK1, a senescence-specific killing compound, is a β-galactosidase-targeted proagent attenuates inflammation. SSK1 is activated by lysosomal β-galactosidase and selectively killed senescent cells through the activation of p38 MAPK and induction of apoptosis .
|
-
- HY-143464
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
BChE-IN-4 is a potent and cross the blood-brain barrier BChE inhibitor. BChE-IN-4 attenuates learning and memory deficits caused by cholinergic deficit in mouse model. BChE-IN-4 has the potential for the research of alzheimer’s disease .
|
-
- HY-163409
-
|
|
β-catenin
|
Inflammation/Immunology
Cancer
|
|
CKG012 is an inhibitor for Wnt/βcatenin signaling pathway. CGK012 inhibits release of HMGB1 and transcription of β-catenin, exhibits attenuating activities against cecal ligation and puncture (CLP)-induced sepsis and multiple myeloma cancer .
|
-
- HY-117091
-
|
|
Others
|
Neurological Disease
Inflammation/Immunology
|
|
DDD-028 is a potent non-opioid, non-cannabinoid analgesic which attenuates neuropathic and inflammatory pain without the possible side effects or abuse potential associated with opioid or cannabinoid activities. DDD-028 can be utilized in analgesic research .
|
-
- HY-101247
-
|
|
mGluR
|
Neurological Disease
|
|
MTPG is a potent mGluR2 and mGluR3 antagonist. MTPG can block the induction of brain ischemic tolerance induced by cerebral ischemic preconditioning. MTPG also significantly attenuates the inhibitory effect of L-CCG-1 on the KCl-evoked dopamine release .
|
-
- HY-P99961
-
|
JS004
|
CD28
|
Cancer
|
|
Tifcemalimab (JS004) is a humanized anti-BTLA (B and T lymphocyte attenuation factor) monoclonal antibody. Tifcemalimab blocks the interaction of HVEM-BTLA by binding to BTLA, and thus blocks the inhibitory signaling pathway mediated by BTLA. Tifcemalimab can be used in research of cancer .
|
-
- HY-109094
-
|
EC-18
|
Others
|
Inflammation/Immunology
|
|
Mosedipimod is a monoacetyldiaglyceride that can be isolated from Cervus nippon Temminck. Mosedipimod is an orally active Toll-Like Receptor signaling inhibitor. Mosedipimod attenuates airway infammation by reducing myeloperoxidase expression in lung tissue. Mosedipimod is used in chronic obstructive pulmonary disease research .
|
-
- HY-155475
-
|
|
mTOR
|
Cardiovascular Disease
|
|
mTORC1-IN-2 (compound H3) is a NO donor compound that alleviates vasodilation and attenuates myocardial hypoxic injury. mTORC1-IN-2 upregulates TSC2-P expression and inhibits mTORC1 expression .
|
-
- HY-N0341R
-
|
|
Sirtuin
|
Metabolic Disease
|
|
Scopolin (Standard) is the analytical standard of Scopolin. This product is intended for research and analytical applications. Scopolin is a coumarin isolated from Arabidopsis thaliana (Arabidopsis) roots . Scopolin attenuated hepatic steatosis through activation of SIRT1-mediated signaling cascades .
|
-
- HY-116266
-
|
|
Others
|
Others
|
|
RS 67333 is a 5-HT4R agonist with stress-preventive activity. RS 67333 attenuates stress-induced body weight changes and prevents depression- and anxiety-like behaviors in two mouse strains tested in different stress models.
|
-
- HY-108943
-
|
|
Others
|
Others
|
|
Sabinene is an naturally occurring bicyclic monoterpene which can be used as flavorings, perfume additives, fine chemicals, and advanced biofuels. Sabinene is also an orally active compound to attenuates skeletal muscle atrophy and regulates ROS-mediated MAPK/MuRF-1 pathways .
|
-
- HY-100581
-
CORM-3
1 Publications Verification
|
NF-κB
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
CORM-3, a carbon monoxide-releasing molecule, attenuates NF-κB p65 nuclear translocation, reduces ROS generation and enhances intracellular glutathione and superoxide dismutase levels. CORM-3 reduces NLRP3 inflammasome activation .
|
-
- HY-101529
-
|
HOE-402(free base)
|
LDLR
|
Cardiovascular Disease
|
|
Imanixil (HOE-402 free base) is an inducer of the LDL receptor (LDLR). Imanixil (HOE-402 free base) is also a potent cholesterol-lowering compound, which inhibits very low density-lipoprotein (VLDL) production, and consequently attenuates atherosclerosis development .
|
-
- HY-115467
-
|
|
HSP
|
Metabolic Disease
|
|
MitoBloCK-10 (MB-10) is the first small molecule modulator to attenuate protein-associated motor (PAM) complex activity. MitoBloCK-10 (MB-10) inhibits Tim44 (C-terminal domain) binding to the precursor and to Hsp70 .
|
-
- HY-139048
-
|
|
iGluR
|
Neurological Disease
|
|
Fluoroethylnormemantine, a derivative of Memantine, is an antagonist of the N-methyl-D-aspartate (NMDA) receptor. [ 18F]-Fluoroethylnormemantine can be used as a positron emission tomography (PET) tracer. Fluoroethylnormemantine exhibits anti-amnesic, neuroprotective, antidepressant-like and fear-attenuating effects .
|
-
- HY-139048A
-
|
|
iGluR
|
Neurological Disease
|
|
Fluoroethylnormemantine hydrochloride, a derivative of Memantine, is an antagonist of the N-methyl-D-aspartate (NMDA) receptor. [ 18F]-Fluoroethylnormemantine hydrochloride can be used as a positron emission tomography (PET) tracer. Fluoroethylnormemantine hydrochloride exhibits anti-amnesic, neuroprotective, antidepressant-like and fear-attenuating effects .
|
-
- HY-145721
-
|
GED-0301
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice .
|
-
- HY-151569
-
|
|
HDAC
Apoptosis
|
Inflammation/Immunology
|
|
SAHA-OH is a selective HDAC6 inhibitor (IC50=23 nM), shows a 10- to 47-fold selectivity for HDAC6 compared to HDAC 1, 2, 3, and 8. SAHA-OH shows anti-inflammatory activity, and attenuates macrophage apoptosis .
|
-
- HY-P3785
-
|
|
PKA
|
Neurological Disease
|
|
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .
|
-
- HY-101079
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with Kis of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .
|
-
- HY-P10148
-
|
Ac-[Leu28,31]-NPY (24-36)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .
|
-
![N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)](//file.medchemexpress.eu/product_pic/hy-p10148.gif)
- HY-W014102R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
L-Alanyl-L-glutamine (Standard) is the analytical standard of L-Alanyl-L-glutamine. This product is intended for research and analytical applications. L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-164461
-
|
|
Trk Receptor
|
Cancer
|
|
AZD6918 is an orally active and selective Trk tyrosine kinase inhibitor. AZD6918 induces cell death as a single agent and attenuates BDNF/TrkB-induced protection from Etoposide (HY-13629) in vitro. AZD6918 can be used for the research of neuroblastoma .
|
-
- HY-B0569
-
|
|
nAChR
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .
|
-
- HY-P1401
-
|
|
PKC
|
Metabolic Disease
|
|
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response .
|
-
- HY-117832
-
-
- HY-141552
-
FC9402
1 Publications Verification
|
Mitochondrial Metabolism
Others
|
Cardiovascular Disease
|
|
FC9402 is a potent and selective sulfide quinone oxidoreductase (SQOR) inhibitor extracted from patent WO 2020/146636 A1. FC9402 attenuates TAC-induced cardiomyocyte hypertrophy and left ventricle (LV) fibrosis. FC9402 can be used for cardiovascular regulation .
|
-
- HY-108624
-
-
- HY-B1078R
-
|
Cephazolin (sodium) (Standard)
|
Bacterial
Antibiotic
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Cefazolin (sodium) (Standard) is the analytical standard of Cefazolin (sodium). This product is intended for research and analytical applications. Cefazolin sodium is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin sodium has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
|
-
- HY-10450
-
|
BMS-512148
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-B0661AS
-
-
- HY-W015782
-
|
|
Tyrosinase
|
Metabolic Disease
|
|
4-Ethylresorcinol, a derivative of resorcinol, can act as substrates of tyrosinase. 4-Ethylresorcinol possess hypopigmentary effects. 4-Ethylresorcinol attenuates mRNA and protein expression of tyrosinase-related protein (TRP)-2, and possessed antioxidative effect by inhibiting lipid peroxidation .
|
-
- HY-B0661AS1
-
-
- HY-114869
-
DPQ
1 Publications Verification
|
PARP
|
Neurological Disease
|
|
DPQ is a potent PARP-1 inhibitor. DPQ can reduce the N-methyl-d-aspartate (NMDA)-induced PARP activation, restoring ATP to near control levels and significantly attenuating neuronal injury in the severe NMDA exposure model. DPQ can be used for researching neuroprotection .
|
-
- HY-146319
-
-
- HY-154829A
-
|
|
Neuropeptide FF Receptor
|
Inflammation/Immunology
|
|
AC-099 hydrochloride (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 hydrochloride attenuates spinal nerve ligation-induced hypersensitivity in rats .
|
-
- HY-154829
-
|
|
Neuropeptide FF Receptor
|
Inflammation/Immunology
|
|
AC-099 (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 attenuates spinal nerve ligation-induced hypersensitivity in rats .
|
-
- HY-B1892R
-
|
|
Antibiotic
Bacterial
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Cefazolin (Standard) is the analytical standard of Cefazolin. This product is intended for research and analytical applications. Cefazolin (Cephazolin) is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
|
-
- HY-W016733
-
|
H-D-Cit-OH
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
D-Citrulline (H-D-Cit-OH) is a stereoisomer of L-citrulline (HY-N0391). D-Citrulline significantly attenuates polymorphonuclear leukocyte (PMN)-induced cardiac contractile dysfunction in the isolated perfused rat heart subjected to ischemia/reperfusion via a non-NO-mediated mechanism .
|
-
- HY-106809
-
|
BMS-181168
|
Others
|
Neurological Disease
|
|
BMY-21502 (BMS-181168) is a pyrrolidinone derivative with memory- and cognition-enhancing activities. BMS-181168 attenuates hypoxia-induced deterioration in brain function, as delta/theta decreases, alpha activity increases and the centroid of the combined delta/theta waves is accelerated .
|
-
- HY-P3112
-
|
|
Bombesin Receptor
|
Neurological Disease
|
|
ICI 216140 is a GRP/bombesin receptor 2 antagonist with the IC50 of 2 nM. ICI 216140 can reduce Bombesin (HY-P0195)-stimulated pancreatic amylase secretion and attenuates Bombesin (HY-P0195)-stimulated increases in blood pressure .
|
-
- HY-100459
-
|
|
RET
|
Metabolic Disease
Inflammation/Immunology
|
|
GSK3179106 is an orally active and selective RET kinase inhibitor with IC50s of 0.4 nM, 0.2 nM for human RET and rat RET, respectively. GSK3179106 has the potential for irritable bowel syndrome (IBS) through the attenuation of post-inflammatory and stress-induced visceral hypersensitivity .
|
-
- HY-14858
-
|
SLV 320
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats .
|
-
- HY-119917
-
|
|
p38 MAPK
MEK
Bacterial
|
Infection
Cancer
|
|
Gossypetin is a hexahydroxylated flavonoid and is a potent mitogen-activated protein kinase kinase (MKK)3 and MKK6 inhibitor with strongly attenuates the MKK3/6-p38 signaling pathway, has various pharmacological activities, including antioxidant, antibacterial and anticancer activities .
|
-
- HY-103374
-
|
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease .
|
-
- HY-N5130
-
|
|
Others
|
Neurological Disease
|
|
Effusol, a phenolic constituent from Juncus effuses, exhibits potent scavenging activity for DPPH and ABTS radicals, with IC50 values of 79 μM and 2.73 μM, respectively. Effusol rescues CA1 LTP attenuated by corticosterone, defending the hippocampal function against stress-induced cognitive decline .
|
-
- HY-156443
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
YG1702 is a potent ALDH18A1-specific inhibitor. YG1702 attenuates the growth of MYCN-amplified NB and down-regulates MYCN. YG1702 physically interacts with ALDH18A1 with a high affinity and might potentially affect its enzymatic activity .
|
-
- HY-N2477R
-
|
|
Apoptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Taraxerol (Standard) is the analytical standard of Taraxerol. This product is intended for research and analytical applications. Taraxerol is isolated from Taraxacum mongolicum, and has anti-inflammtory and anti-cancer effects. Taraxerol attenuates acute inlammation through inhibition of NF-κB signaling pathway. Taraxerol induces cell apoptosis .
|
-
- HY-N7126R
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Citronellal (Standard) is the analytical standard of Citronellal. This product is intended for research and analytical applications. Citronellal is a monoterpenea from the essential oils in various aromatic species of plants, with depressant, and antinociceptive properties. Citronellal attenuates mechanical nociception, mediated in part by the NO-cGMP-ATP-sensitive K? channel pathway .
|
-
- HY-124873
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
SERCA2a activator 1 (Compound A) is a sarco/endoplasmic reticulum Ca 2+-dependent ATPase 2a (SERCA2a) activator. SERCA2a activator 1 attenuates phospholamban inhibition and enhances the systolic and diastolic functions of the heart. SERCA2a activator 1 can be used for heart failure .
|
-
- HY-N2638
-
|
|
Apoptosis
|
Cardiovascular Disease
|
|
Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
|
-
- HY-126390
-
|
NSC 150117
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
(E/Z)-BCI (NSC 150117) is a dual-specificity phosphatase 6 (DUSP6) inhibitor with anti-inflammatory activities. (E/Z)-BCI attenuates LPS-induced inflammatory mediators and ROS production in macrophage cells via activating the Nrf2 signaling axis and inhibiting the NF-κB pathway .
|
-
- HY-145829
-
|
|
JAK
Apoptosis
|
Inflammation/Immunology
|
|
Tofacitinib precursor-1 is an effective and oral active precursor to mitigate the systemic adverse effects of Tofacitinib. Tofacitinib precursor-1 can effectively attenuate the oxazolone-induced colitis in mice model with low toxicity. Tofacitinib precursor-1 is a potential drug candidate for the research of ulcerative colitis .
|
-
- HY-136093B
-
|
IM156 free base; HL156A free base; HL271 free base
|
Mitochondrial Metabolism
|
Cancer
|
|
Lixumistat (IM156) is a novel biguanide mitochondrial protein complex 1 inhibitor of oxidative phosphorylation (OXPHOS) with anti-tumor activity. Lixumistat regulates OXPHOS to attenuate mitochondrial metabolic reprogramming and inhibit lung fibrosis. Lixumistat also suppresses B-cell activation to alleviate systemic lupus erythematosus .
|
-
- HY-149700
-
|
|
ROCK
MMP
STAT
|
Others
|
|
ROCK2-IN-7 is a kinase inhibitor targeting to ROCK2. ROCK2-IN-7 inhibits ROCK2/pSTAT3 Signaling. ROCK2-IN-7 suppresses systemic immunity activation and attenuates inflammation in psoriasis model .
|
-
- HY-B0661AR
-
|
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin (hydrochloride) (Standard) is the analytical standard of Tamsulosin (hydrochloride). This product is intended for research and analytical applications. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models .
|
-
- HY-W654098
-
|
|
Isotope-Labeled Compounds
Antibiotic
Bacterial
|
Inflammation/Immunology
|
|
Cefazolin- 13C2, 15N (sodium) is 13C and 15N labeled Cefazolin (sodium). Cefazolin sodium is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin sodium has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD).
|
-
- HY-N0293
-
|
Peoniflorin
|
HSP
|
Infection
Neurological Disease
Cancer
|
|
Paeoniflorin is a heat shock protein-inducing compound and commonly exists in the plants of Paeoniaceae family, with various biological activities, including anticancer activity, anti-inflammatory activity, enhancing cognition and attenuating learning impairment, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, and reducing blood viscosity .
|
-
- HY-B0673
-
|
AMR69
|
TGF-beta/Smad
CCR
|
Inflammation/Immunology
Cancer
|
|
Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
|
-
- HY-N0496
-
|
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
|
Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway. Ruscogenin exerts significant anti-inflammatory and anti-thrombotic activities. Ruscogenin has orally bioactivity .
|
-
- HY-132280
-
|
U 74006F free base
|
Antibiotic
|
Infection
Neurological Disease
|
|
Tirilazad is a nonglucocorticoid, 21-aminosteroid that inhibits lipid peroxidation. Tirilazad can attenuate brain or spinal cord injury caused by trauma, stroke, ischemia and reperfusion injury. Tirilazad has antiviral activities against nCoV. Tirilazad is neuroprotective for ischaemic stroke, can be used for subarachnoid hemorrhage research .
|
-
- HY-P5182
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
|
-
- HY-161362
-
|
|
PI3K
|
Cancer
|
|
SR-3-65 (compound 6) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. SR-3-65 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
|
-
- HY-158017
-
|
|
PI3K
|
Cancer
|
|
WXM-1-170 (compound 10) is a Indisulam (HY-13650) derivative,and inhibits the migration of gastric cancer cells. WXM-1-170 attenuates PI3K/AKT/GSK-3β/β-catenin signaling pathway .
|
-
- HY-158408
-
|
|
ULK
Mitophagy
|
Neurological Disease
|
|
NZ-66 is a UNC-51-like kinase 1 (ULK1) targeting chimera, which is used to achieve proximity-induced and ULK1-dependent degradation of mitochondria. NZ-66 induces mitophagy. NZ-66 is potential for attenuating neurodegenerative disorders .
|
-
- HY-106973A
-
|
CHF 1035
|
Dopamine Receptor
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Nolomirole (CHF 1035) hydrochloride is an orally active and selective DA2 dopaminergic receptor/α2-adrenoceptor agonist. Nolomirole attenuates the heart failure signs in the Monocrotaline (HY-N0750)-induced congestive heart failure model. Nolomirole increases cardiac output .
|
-
- HY-124583
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PF-4363467, a dopamine D3/D2 receptor antagonist, attenuates opioid drug-seeking behavior without
concomitant D2 side effects. PF-4363467 exhibits Ki values of 3.1 nM and 692 nM for D3R and D2R .
|
-
- HY-170655
-
|
|
PDI
Integrin
|
Cardiovascular Disease
|
|
PDI-IN-4 (Compound 14d) is an inhibitor of protein disulfide isomerase, with an IC50 value of 0.48 μM. PDI-IN-4 suppresses platelet aggregation and thrombus formation by attenuating GPIIb/IIIa activation without significantly causing cytotoxicity. PDI-IN-4 can be used in research on thrombosis .
|
-
- HY-B0011
-
|
RP-56976
|
Microtubule/Tubulin
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity .
|
-
- HY-P1098
-
Ac2-26
4 Publications Verification
|
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue .
|
-
- HY-P1098A
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue .
|
-
- HY-N6901
-
|
|
Epigenetic Reader Domain
|
Metabolic Disease
|
|
Luteolin 7-sulfate is isolated from Phyllospadix iwatensis Makino, a marine plant. Luteolin 7-sulfate attenuates TYR gene expression through the intervention of a cAMP-responsive element binding protein (CREB)- and microphthalmia-associated transcription factor (MITF)-mediated signaling pathway, leading to the decreased melanin synthesis .
|
-
- HY-114657A
-
|
|
Arp2/3 Complex
|
Inflammation/Immunology
Cancer
|
|
Benproperine phosphate is an orally active, potent actin-related protein 2/3 complex subunit 2 (ARPC2) inhibitor. Benproperine phosphate attenuates the actin polymerization rate of action polymerization nucleation by impairing Arp2/3 function. Benproperine phosphate has the potential for a cough suppressant and suppresses cancer cell migration and tumor metastasis .
|
-
- HY-155737
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
ET receptor antagonist 1 (compound 16h) is an orally active ET receptor antagonist (IC50=0.18 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 1 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-155738
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
ET receptor antagonist 2 (compound 16j) is an orally active ET receptor antagonist (IC50=0.22 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 2 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-155739
-
|
|
Estrogen Receptor/ERR
|
Cardiovascular Disease
|
|
ET receptor antagonist 3 (compound 17d) is an orally active ET receptor antagonist (IC50=0.26 nM), which can be used for research in pulmonary arterial hypertension (PAH). ET receptor antagonist 3 attenuates monocrotaline (HY-N0750) induced PAH in rat model .
|
-
- HY-103375
-
|
|
CRFR
|
Neurological Disease
|
|
SN003 is a reversible antagonist of corticotropin releasing factor receptor 1 (CRFR 1) (IC50 = 241 nM) that displays more than 1000-fold selectivity over CRFR 2. SN003 suppresses CRF-induced ACTH release in vitro. SN003 attenuates depressive-like behavior in rat .
|
-
- HY-118821
-
|
|
CRFR
|
Metabolic Disease
|
|
JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, attenuates hippocampal noradrenaline release, visceral perception, adrenocorticotropic hormone release, and anxiety after acute colorectal distention in rats. JTC-017 blocks stress-induced changes in colonic motility after chronic colorectal distention in rats .
|
-
- HY-110134
-
|
|
Constitutive Androstane Receptor
|
Metabolic Disease
|
|
S07662 is a human constitutive androstane receptor (hCAR) inhibitor with an IC50 of 0.7 μM. S07662 recruits the corepressor NCoR in cell-based assays and attenuate the expression of CYP2B6 mRNA in human primary hepatocytes induced by phenytoin (HY-B0448) and CITCO (HY-103244) .
|
-
- HY-A0143A
-
|
DGLA sodium; all-cis-8,11,14-Eicosatrienoic acid sodium
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid (DGLA; all-cis-8,11,14-Eicosatrienoic acid) sodium is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid (sodium) attenuates atherosclerosis in the apolipoprotein E deficient mouse model system .
|
-
- HY-B0149R
-
|
cyclocapron (Standard)
|
IGF-1R
AMPK
MMP
Mitophagy
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Tranexamic acid (Standard) is the analytical standard of Tranexamic acid. This product is intended for research and analytical applications. Tranexamic acid (cyclocapron), a cyclic analog of lysine, is an orally active antifibrinolytic agent. Tranexamic acid attenuates the effects of severe trauma, inhibits urokinase plasminogen activator and ameliorates dry wrinkles. Tranexamic acid can used for the research of hemostasis .
|
-
- HY-128142
-
|
|
PKD
PKC
|
Cardiovascular Disease
|
|
PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC50 value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure .
|
-
- HY-163533
-
|
|
VEGFR
|
Inflammation/Immunology
|
|
CPD-002 is an inhibitor for vascular endothelial growth factor receptor 2 (VEGFR 2), that inhibits angiogenesis through inhibition of VEGFR2/PI3K/AKT signaling pathway. CPD-002 exhibits anti-inflammatory activity and attenuates rheumatoid arthritis .
|
-
- HY-B0661R
-
|
|
Adrenergic Receptor
Endogenous Metabolite
|
Neurological Disease
Endocrinology
Cancer
|
|
Tamsulosin (Standard) is the analytical standard of Tamsulosin. This product is intended for research and analytical applications. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
|
-
- HY-N0595R
-
|
|
Estrogen Receptor/ERR
Apoptosis
|
Metabolic Disease
Cancer
|
|
Genistin (Standard) is the analytical standard of Genistin. This product is intended for research and analytical applications. Genistin (Genistine), an isoflavone belonging to the phytoestrogen family, is a potent anti-adipogenic and anti-lipogenic agent. Genistin attenuates cellular growth and promotes apoptotic cell death breast cancer cells through modulation of ERalpha signaling pathway .
|
-
- HY-103374A
-
|
(-)-Eseroline phenylcarbamate tartrate; (-)-Phenserine (+)-tartrate
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
Phenserine tartrate ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine tartrate reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine tartrate improves cognitive performance and attenuates the progression of Alzheimer's disease .
|
-
- HY-19867A
-
|
TG-0054 hydrobromide
|
CXCR
|
Cardiovascular Disease
Inflammation/Immunology
Endocrinology
Cancer
|
|
Burixafor hydrobromide (TG-0054 hydrobromide) is an orally bioavailable and potent antagonist of CXCR4 and a well anti-angiogenic drug that is of potential value in treating choroid neovascularization . Burixafor hydrobromide (TG-0054 hydrobromide) mobilizes mesenchymal stem cells, attenuates inflammation, and preserves cardiac systolic function in a porcine model of myocardial infarction .
|
-
- HY-101364
-
|
|
mGluR
NF-κB
ERK
Akt
|
Cardiovascular Disease
Inflammation/Immunology
|
|
CHPG is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells . CHPG protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways .
|
-
- HY-101364A
-
|
|
mGluR
NF-κB
ERK
Akt
|
Neurological Disease
Inflammation/Immunology
|
|
CHPG sodium salt is a selective mGluR5 agonist, and attenuates SO2-induced oxidative stress and inflammation through TSG-6/NF-κB pathway in BV2 microglial cells . CHPG sodium salt protects against traumatic brain injury (TBI) in vitro and in vivo by activation of the ERK and Akt signaling pathways. .
|
-
- HY-N5025
-
|
|
P2X Receptor
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects. Bullatine A is a potent P2X7 antagonist, inhibits ATP-induced cell death/apoptosis and P2X receptor-mediated inflammatory responses . Bullatine A attenuates pain hypersensitivity, regardless of the pain models employed .
|
-
- HY-N6869
-
|
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-N7363
-
|
(-)-Isolongifolene
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Isolongifolene ((-)-Isolongifolene) is a tricyclic sesquiterpene isolated from Murraya koenigii. Isolongifolene attenuates Rotenone-induced oxidative stress, mitochondrial dysfunction and apoptosis through the regulation of PI3K/AKT/GSK-3β signaling pathways. Isolongifolene has antioxidant, anti-inflammatory, anticancer and neuroprotective properties .
|
-
- HY-N4042
-
|
|
PI3K
ERK
|
Inflammation/Immunology
Cancer
|
|
Hirsutenone is an active botanical diarylheptanoid present in Alnus species and exhibits many biological activities, including anti-inflammatory, anti-tumor promoting and anti-atopic dermatitis effects. Hirsutenone attenuates adipogenesis by binding directly to PI3K and ERK1 in a non-ATP competitive manner. Hirsutenone can be used for the study of obesity .
|
-
- HY-P1428A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-108355
-
|
|
PKC
|
Cancer
|
|
R59949 is a pan diacylglycerol kinase (DGK) inhibitor with an IC50 of 300 nM. R59949 strongly inhibits the activity of type I DGK α and γ and moderately attenuates the activity of type II DGK θ and κ. R59949 activates protein kinase C (PKC) by enhancing the levels of the endogenous ligand diacyl glycerol .
|
-
- HY-136093
-
|
HL271; IM156 hydrochloride; HL156A hydrochloride
|
Oxidative Phosphorylation
AMPK
|
Neurological Disease
Cancer
|
|
Lixumistat (HL271) hydrochloride (IM156 hydrochloride; HL156A hydrochloride), a chemical derivative of Metformin (HY-B0627), is a potent AMPK activator that increases AMPK phosphorylation. Lixumistat hydrochloride attenuates aging-associated cognitive impairment in animal model . Lixumistat hydrochloride is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors .
|
-
- HY-138537
-
|
|
IKK
|
Cancer
|
|
NF-κB-IN-1, a 4-arylidene crucumin analogue, is a potent NF-κB signaling pathway inhibitor. NF-κB-IN-1 directly inhibits IKK to block NF-κB activation. NF-κB-IN-1 effectively inhibits the viability of lung cancer cells and attenuates the clonogenic activity of A549 cells .
|
-
- HY-100448A
-
|
|
Prostaglandin Receptor
TGF-beta/Smad
|
Endocrinology
|
|
Butaprost is a selective prostaglandin E receptor (EP2) agonist with an EC50 of 33 nM and a Ki of 2.4 μM for murine EP2 receptor. Butaprost is less activity against murine EP1, EP3 and EP4 receptors. Butaprost attenuates fibrosis by hampering TGF-β/Smad2 signalling .
|
-
- HY-113314
-
|
|
Endogenous Metabolite
|
Cancer
|
|
AFMK, antioxidant metabolite of Melatonin, attenuates X-ray-induced oxidative damage to DNA, proteins and lipids in mice. AFMK is a poorer scavenger. The pKa of AFMK at physiological pH is 8.7. Antioxidant capacity . AFMK improves the anti-tumor effect of Gemcitabine in PANC-1 cells through the modulation of apoptotic pathway .
|
-
- HY-N8472
-
|
|
GABA Receptor
|
Infection
|
|
Chrodrimanin B, a metabolite of a fungal, is a potent, non-open-channel-blocking antagonist on?B.?mori GABAR RDL with an IC50?of 1.13 nM. Chrodrimanin B attenuates the peak current amplitude of the GABA response of RDL with an IC50?of 1.66 nM.?Chrodrimanin B, a meroterpenoid, shows insecticidal activity .
|
-
- HY-107640
-
|
|
MMP
|
Cancer
|
|
WAY-170523 is a potent and selective MMP-13 (matrix metalloproteinase-13) inhibitor, with an IC50 of 17 nM. WAY-170523 can directly attenuate ERK1/2 phosphorylation. WAY-170523 inhibits the invasion of PC-3 cells, can be used for prostate cancer research .
|
-
- HY-146168
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Nrf2 activator-5 (compound 1) is a potent Nrf2 activator that can attenuate H2O2-induced oxidative stress and LPS-stimulated inflammation in BV-2 microglial cells. Nrf2 activator-5 exhibits antioxidant and anti-inflammatory activities .
|
-
- HY-122070
-
|
U 74006F
|
Antibiotic
|
Infection
Neurological Disease
|
|
Tirilazad mesylate (U 74006F) is a nonglucocorticoid, 21-aminosteroid that inhibits lipid peroxidation. Tirilazad mesylate can attenuate brain or spinal cord injury caused by trauma, stroke, ischemia and reperfusion injury. Tirilazad mesylate has antiviral activities against nCoV. Tirilazad mesylate is neuroprotective for ischaemic stroke, can be used for subarachnoid hemorrhage research .
|
-
- HY-P5182A
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
|
-
- HY-19126
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Infection
Cardiovascular Disease
|
|
CL-184005 is an antagonist for platelet-activating factor (PAF), that inhibits the PAF-induced platelet aggregation with IC50 of 600 nM and 510 nM, in human and rabbit platelet-rich plasma. CL-184005 protects the rats from endotoxin-induced gastrointestinal damage and hypotension. CL-184005 exhibits potential attenuating Gram-negative bacterial sepsis .
|
-
- HY-19216
-
|
SKP 450
|
Potassium Channel
|
Cardiovascular Disease
|
|
KR-30450 (SKP 450) is a potent K +ATP opener, and a potassium channel activator. KR-30450 exerts more potent cardioprotective effects than Lemakalim (HY-14255). KR-30450 significantly improves reperfusion cardiac function. KR-30450 significantly attenuates reperfusion contracture and lactate dehydrogenase release .
|
-
- HY-12678
-
|
NMS-E628; RXDX-101
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-19824
-
|
|
Autophagy
|
Cancer
|
|
3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC50s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD + and NADH. 3PO can be used for the research of cancer .
|
-
- HY-101415
-
|
Ubiquinone Q9; CoQ9; Ubiquinone 9
|
Apoptosis
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis .
|
-
- HY-101467A
-
|
G1T28 hydrochloride
|
CDK
|
Cancer
|
|
Trilaciclib (G1T28) hydrochloride is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. Trilaciclib hydrochloride can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib hydrochloride attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
|
-
- HY-101467
-
|
G1T28
|
CDK
|
Cancer
|
|
Trilaciclib (G1T28) is an orally active CDK4/6 inhibitor with IC50 values of 1 nM and 4 nM for CDK4 and CDK6, respectively. . Trilaciclib can effectively inhibit tumor cell proliferation and reduce the hematological toxicity caused by chemotherapy. Trilaciclib attenuates apoptosis and myelosuppression induced by 5FU (HY-90006) chemotherapy .
|
-
- HY-128872
-
|
EHP-101; VCE-004.8
|
PPAR
Cannabinoid Receptor
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
Inflammation/Immunology
|
|
Etrinabdione (EHP-101; VCE-004.8) is an orally active, specific PPARγ and CB2 receptor dual agonist. Etrinabdione inhibits prolyl-hydroxylases (PHDs) and activates the HIF pathway. Etrinabdione, a semi-synthetic multitarget cannabinoquinoid, has potent anti-inflammatory activity. Etrinabdione attenuates adipogenesis and prevents diet-induced obesity .
|
-
- HY-119039
-
RU-301
1 Publications Verification
|
TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
RU-301 is a pan TAM inhibitor that blocks Gas6-induced TAM activation and tumorigenicity. RU-301 significantly reduces nonalcoholic steatohepatitis (NASH) fibrosis, along with attenuates ERK activation and TGFβ1 expression. RU-301 can be used in studies of cancer and nonalcoholic steatohepatitis .
|
-
- HY-117370
-
|
AZ1
|
Deubiquitinase
|
Cancer
|
|
USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model .
|
-
- HY-121246
-
|
AKF-PD
|
PI3K
Akt
|
Inflammation/Immunology
|
|
Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway .
|
-
- HY-B0673S
-
|
AMR69-d5
|
TGF-beta/Smad
CCR
|
Inflammation/Immunology
Cancer
|
|
Pirfenidone-d5 is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
|
-
- HY-Z0283
-
|
Benzenecarboxamide; Phenylamide
|
Endogenous Metabolite
PARP
|
Others
|
|
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
|
-
- HY-P2320
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release .
|
-
- HY-136093A
-
|
IM156; HL156A; HL271 acetate
|
Oxidative Phosphorylation
AMPK
|
Neurological Disease
Cancer
|
|
Lixumistat (IM156; HL156A; HL271) acetate, a chemical derivative of Metformin (HY-B0627), is a potent and orally active AMPK activator that increases AMPK phosphorylation. Lixumistat (acetate) attenuates aging-associated cognitive impairment in animal model . Lixumistat (acetate) is a potent oxidative phosphorylation (OXPHOS) inhibitor which can be used for the research of solid tumors .
|
-
- HY-126415
-
|
|
Na+/K+ ATPase
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
Magnesium Lithospermate B, is a derivative of caffeic acid tetramer and an inhibitor of Na+/K+ ATPase, which can be extracted from Salviae miltiorrhizae. Magnesium Lithospermate B is widely used for the research of cardiovascular diseases, and it can protect against glucose-induced intracellular oxidative damage. Magnesium Lithospermate B also suppresses neuroin?ammation and attenuates neurodegeneration .
|
-
- HY-108492
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
TC-SP 14 (compound 14) is an orally active and potent S1P1 agonist (EC50 = 0.042 μM) with minimal activity at S1P3 (EC50 = 3.47 μM). TC-SP 14 significantly reduces blood lymphocyte counts and attenuates a delayed type hypersensitivity (DTH) response to antigen challenge .
|
-
- HY-147748
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC50 of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase .
|
-
- HY-135046
-
|
|
DNA/RNA Synthesis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
MTOB sodium is a potent C-terminal binding protein (CtBP) inhibitor. MTOB sodium attenuates repetitive head injury-elicited neurologic dysfunction and neuroinflammation via inhibition of the transactivation activity of CtBP1 and CtBP2. MTOB sodium antagonizes the transcriptional regulatory activity of CtBP1 and CtBP2 by eviction from their target promoters in breast cancer cell lines .
|
-
- HY-148853
-
|
|
HuR
|
Others
|
|
SRI-42127 is a HuR translocation inhibitor. HuR is an RNA regulator that binds to AREs, and HuR translocations promote the production of inflammatory cytokines in glial cells. However, SRI-42127 can destroy mRNA stability and inhibit gene promoter activation. SRI-42127 also inhibits microglial cell activation and attenuates recruitment/chemotaxis of neutrophils and monocytes .
|
-
- HY-122070A
-
|
U 74006F hydrate
|
Antibiotic
|
Infection
Metabolic Disease
|
|
Tirilazad mesylate hydrate is the hydrate form of Tirilazad mesylate (HY-122070). Tirilazad mesylate is a nonglucocorticoid, 21-aminosteroid that inhibits lipid peroxidation. Tirilazad mesylate can attenuate brain or spinal cord injury caused by trauma, stroke, ischemia and reperfusion injury. Tirilazad mesylate has antiviral activities against nCoV. Tirilazad mesylate is neuroprotective for ischaemic stroke, can be used for subarachnoid hemorrhage research .
|
-
- HY-124243
-
|
17-Phenyl trinor prostaglandin F2α cyclopropyl methyl amide
|
Prostaglandin Receptor
|
Others
|
|
N-Cyclopropyl methyl bimatoprost (17-Phenyl trinor prostaglandin F2α cyclopropyl methyl amide) is an analog of Bimatoprost (HY-12956). N-Cyclopropyl methyl bimatoprost is an agonist for Prostaglandin F2α Receptor (FP receptor). N-Cyclopropyl methyl bimatoprost is potent to reduce the intraocular pressure and attenuate the glaucoma .
|
-
- HY-125156
-
|
BMS-801576
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Dapagliflozin-3-O-β-D-glucuronide (BMS-801576) is the metabolite of Dapagliflozin (HY-10450), and is formed in the liver and kidney by uridine diphosphate glucuronosyltransferase-1A9 (UGT1A9). Dapagliflozin is a selective inhibitor for SGLT2, that can be used to improve glycemic control and attenuate type 2 diabetes .
|
-
- HY-116145
-
|
|
Tyrosinase
NF-κB
|
Inflammation/Immunology
|
|
MHY884 is a tyrosinase inhibitor that suppresses UVB-induced activation of NF-κB signaling pathway through the downregulation of oxidative stress. MHY884 suppresses oxidative stress in the melanoma cells and attenuates UVB-induced oxidative stress, resulting in reduced NF-κB activity in irradiated mice. MHY884 is promising for research of UVB-induced skin damage .
|
-
- HY-12145
-
|
|
Others
|
Neurological Disease
|
|
CP-99994 hydrochloride is a high-affinity NK1 antagonist that exhibits the biological activity of preventing colorectal sensitization in the context of visceral hypersensitivity. CP-99994 hydrochloride reduces colorectal hypersensitivity induced by acetic acid injections in a model of bladder-colon cross-sensitization. CP-99994 hydrochloride attenuates the neuroglial interactions and MAPK-p38 phosphorylation associated with visceral hypersensitivity.
|
-
- HY-B1892S1
-
-
- HY-11062
-
Icilin
1 Publications Verification
AG-3-5
|
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a "super-cooling agent" . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response .
|
-
- HY-B0792
-
|
|
LRRK2
|
Neurological Disease
|
|
CZC-54252 is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. CZC-54252 attenuates G2019S LRRK2-induced human neuronal injury with an EC50 of ~1 nM. CZC-54252 has a neuroprotective activity .
|
-
- HY-15079
-
|
GYKI-53773; LY-300164
|
iGluR
Apoptosis
|
Neurological Disease
Cancer
|
|
Talampanel (LY300164) is an orally and selective α-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptor antagonis with anti-seizure activity . Talampanel (IVAX) has neuroprotective effects in rodent stroke models . Talampanel attenuates caspase-3 dependent apoptosis in mouse brain .
|
-
- HY-101761
-
|
|
PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM and induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-12680
-
PRN694
1 Publications Verification
|
Itk
|
Inflammation/Immunology
|
|
PRN694 is an irreversible, highly selective and potent covalent interleukin-2-inducible T-cell kinase (ITK) and resting lymphocyte kinase (RLK) dual inhibitor with IC50s of 0.3 nM and 1.4 nM, respectively. PRN694 exhibits extended target residence time on ITK and RLK, enabling durable attenuation of effector cells in vitro and in vivo .
|
-
- HY-111747
-
|
|
Bacterial
|
Infection
Cardiovascular Disease
|
|
TBAJ-587, a potent anti-tuberculosis agent, inhibits M.tb strain H37Rv growth with MIC90s of 0.006 and <0.02 μg/mL in MABA and LORA assay, respectively. TBAJ-587 inhibits hERG channel minimally, attenuates inhibition of the cardiac potassium channel protein coded by the hERG, which is important for cardiac repolarization .
|
-
- HY-107818
-
|
|
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
4-Hydroxychalcone is a chalcone metabolite with anti-angiogenic and anti-inflammatory activities. 4-Hydroxychalcone suppresses angiogenesis by suppression of growth factor pathway with no signs of cytotoxicity . 4-Hydroxychalcone inhibits TNF-α induced NF-κB pathway activation and activates BMP signaling, reduces resistant hypertension (RH) by attenuating hyperaldosteronism and renal injury in mice .
|
-
- HY-N0148A
-
|
Rutoside hydrate; Quercetin 3-O-rutinoside hydrate
|
Amyloid-β
Autophagy
Apoptosis
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Rutin (Rutoside) hydrate is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin hydrate can cross the blood brain barrier. Rutin hydrate attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress .
|
-
- HY-19345
-
|
NSC13316
|
Others
|
Cancer
|
|
Vacquinol-1 (NSC13316) is a MKK4-specific activator that activates MAPK pathways . Vacquinol-1 specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model . Vacquinol-1 also induces apoptosis in hepatocellular carcinoma (HCC)cell .
|
-
- HY-N10587
-
|
|
Others
|
Inflammation/Immunology
|
|
Catechin 7-O-beta-D-glucopyranoside is an orally active natural product found in Ulmus davidiana and Paeonia obovata. Catechin 7-O-β-D-glucopyranoside shows antioxidant and anti-inflammatory activities, and attenuates mitochondrial dysfunction. Catechin 7-O-beta-D-glucopyranoside can be used in intestinal inflammatory disease research .
|
-
- HY-44307
-
|
|
Ferroptosis
|
Cancer
|
|
84-B10 is a 3-phenylglutaric acid derivative. 84-B10 inhibits cisplatin (HY-17394) induced tubular ferroptosis. 84-B10 attenuates cisplatin-induced mitochondrial damage and oxidative stress. 84-B10 ameliorates cisplatin-induced acute kidney injury (AKI) .
|
-
- HY-19345A
-
|
NSC13316 dihydrochloride
|
Others
|
Cancer
|
|
Vacquinol-1 (NSC13316) dihydrochloride is a MKK4-specific activator that activates MAPK pathways . Vacquinol-1 dihydrochloride specifically induces human glioblastoma cell (GC) death, attenuates tumor progression and prolongs survival in a glioblastoma multiforme (GBM) mouse model . Vacquinol-1 dihydrochloride also induces apoptosis in hepatocellular carcinoma (HCC)cell .
|
-
- HY-156109
-
|
|
PDHK
Mitochondrial Metabolism
|
Cancer
|
|
PDK-IN-2 (Compound 1F) is a PDK inhibitor (IC50: 68 nM). PDK-IN-2 inhibits the cellular expression of PDK1 and PDK4. PDK-IN-2 enhances mitochondrial bioenergetics, attenuates glycolytic phenotypes, and induces cell apoptosis in the mitochondrial pathway. PDK-IN-2 inhibits tumor growth in 4T1 syngeneic mice model .
|
-
- HY-P5874
-
|
|
Calcium Channel
|
Inflammation/Immunology
|
|
Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .
|
-
- HY-149724
-
|
|
STING
NO Synthase
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 65 (compound 29) is a Hederagonic acid derivative with potent anti-inflammatory activity. Anti-inflammatory agent 65 inhibits nitric oxide (NO) release. Anti-inflammatory agent 65 inhibits the nuclear translocation of IRF3 and p65, and disrupts the STING/IRF3/NF-κB signaling pathway, thereby attenuating the inflammatory response .
|
-
- HY-155463
-
|
|
NOD-like Receptor (NLR)
Interleukin Related
|
Inflammation/Immunology
|
|
NLRP3-IN-25 (compound 32) is an orally available NLRP3 inhibitor with anti-inflammatory activity. NLRP3-IN-25 attenuates renal injury in doxorubicin-induced glomerulonephritis in mice. NLRP3-IN-25 inhibits IL-1β secretion in THP-1 cells with an IC50 of 21 nM .
|
-
- HY-163507
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK5-IN-79 (compound 57) is an ALK inhibitor with anticancer activity, by blocking TGF-β1/SMAD signaling pathway. ALK5-IN-79 attenuates the production of extracellular matrix (ECM) and deposition of collagen. ALK5-IN-79 exhibits adequate pharmacokinetic (PK) properties and good in vivo tolerance.
|
-
- HY-16485
-
|
TD-6424 hydrochloride
|
Antibiotic
Bacterial
|
Infection
|
|
Telavancin hydrochloride is the hydrochloride form of Telavancin (HY-112959). Telavancin hydrochloride is a semisynthetic derivative of vancomycin, and exhibits antibacterial efficacy through inhibition of cell wall synthesis and disruption of cell membrane barrier function. Telavancin hydrochloride is efficient against antibiotic resistant S. aureus strains MRSA, VISA, and hVISA. Telavancin hydrochloride attenuates gram positive bacteria induced complicated skin and skin structure infections (cSSSI) .
|
-
- HY-158374
-
|
|
IRAK
|
Inflammation/Immunology
|
|
BIO-8169 is a selective inhibitor for interleukin receptor-associated kinase 4 (IRAK 4), with an IC50 of 0.23 nM. BIO-8169 exhibits good pharmacokinetic character, reduces the production of pro-inflammatory cytokines, and attenuates the autoimmune encephalomyelitis in EAE mice model. BIO-8169 exhibits good blood brain penetrant with a rat Kpu,u of 0.7 .
|
-
- HY-10450R
-
|
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin (Standard) is the analytical standard of Dapagliflozin. This product is intended for research and analytical applications. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-161663
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Phosphodiesterase-IN-2 (Compound C7) is a selective, orally active inhibitor for phosphodiesterase 10A (PDE10A), with an IC50 of 11.9 nM. Phosphodiesterase-IN-2 improves the stability of liver microsomes, and lowers BBB permeability. Phosphodiesterase-IN-2 exhibits good pharmacokinetic characters, and attenuates isoprenaline (HY-108353)-induced cardiac hypertrophic in mouse models .
|
-
- HY-161892
-
|
|
FABP
|
Metabolic Disease
Inflammation/Immunology
|
|
FABP4-IN-4 (Compound 30) is an orally active inhibitor for FABP, with IC50 of 1.18 μM for FABP 1. FABP4-IN-4 improves the glucose tolerance, reduces the level of blood glucose, plasma lipids and hepatic inflammatory factors, attenuates hepatic steatosis, and exhibits anti-inflammatory effects in mouse diet-induced obesity models .
|
-
- HY-10450S5
-
|
|
Isotope-Labeled Compounds
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin- 13C6-1 is 13C labeled Dapagliflozin. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-B0661S
-
-
- HY-50754
-
|
|
γ-secretase
|
Neurological Disease
|
|
gamma-secretase modulator 2 is a potent and selective γ-secretase modulator for treatment of Alzheimer's disease
IC50 value:
Target: γ-secretase
γ-secretase modulator is modulation of the action of γ-secretase so as to Selectively attenuate production of Aβ(1-42) and hence find use in treatment or prevention of diseases associated with deposition of Aβ in the brain.
|
-
- HY-B0011A
-
|
RP-56976 Trihydrate
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM . Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis .
|
-
- HY-B0011S
-
|
RP-56976-d9
|
Microtubule/Tubulin
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity[1][3].
|
-
- HY-N6967
-
|
(-)-α-Bisabolol
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-124796
-
|
|
Bacterial
|
Infection
|
|
QStatin is a potent and selective inhibitor of SmcR (V. harveyi LuxR homologue) with an EC50 of 208.9 nM, binding tightly to SmcR and changes the flexibility of the protein, thereby altering its transcription regulatory activity. QStatin shows pan-QS (Vibrio quorum sensing) inhibitor activity in diverse Vibrio species and attenuates their virulence in an aquatic host. QStatin may be a sustainable antivibriosis agent useful in aquacultures .
|
-
- HY-N0107
-
|
|
Apoptosis
Autophagy
mTOR
Akt
|
Cardiovascular Disease
|
|
Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR . Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis . Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction .
|
-
- HY-B0792A
-
|
|
LRRK2
|
Neurological Disease
|
|
CZC-54252 hydrochloride is a potent and selective LRRK2 inhibitor with IC50s of 1.28 nM and 1.85 nM for wild-type and G2019S LRRK2, respectively. G2019S LRRK2-induced human neuronal injury is attenuated by CZC-54252 hydrochloride with an EC50 of ~1 nM.CZC-54252 hydrochloride has a neuroprotective activity .
|
-
- HY-123671
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
CYM2503 is a putative GalR2-positive allosteric modulator. CYM2503 increases the latency to first electrographic seizure and decreases the total time in seizure. CYM2503 also attenuates electroshock-induced seizures in mice. Galanin receptors type 1 (GalR1) and/or type 2 (GalR2) represent unique pharmacological targets for the research of seizures and epilepsy .
|
-
- HY-101446
-
|
|
Trk Receptor
ERK
Apoptosis
|
Neurological Disease
|
|
HIOC is a potent and selective activator of TrkB (tropomyosin related kinase B) receptor. HIOC can pass the blood-brain and blood-retinal barriers.HIOC activates TrkB/ERK pathway and decreases neuronal cell apoptosis. HIOC attenuates early brain injury after SAH (subarachnoid hemorrhage). HIOC shows protective activity in an animal model for light-induced retinal degeneration .
|
-
- HY-W152604
-
|
Cyclo(leu-gly)
|
Dopamine Receptor
|
Neurological Disease
|
|
Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity. Cyclo(glycyl-L-leucyl) inhibits the development of Morphine induced pain relief as well as dopamine receptor supersensitivity in rats. Cyclo(glycyl-L-leucyl) has the potential for the prevention of tardive and/or L-DOPA (HY-N0304)-induced dyskinesias .
|
-
- HY-N11648
-
|
|
Apoptosis
Caspase
|
Inflammation/Immunology
Cancer
|
|
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
|
-
- HY-155782
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
Zharp2-1 is an oral effective RIPK2 inhibitor, highly associated with inflammatory bowel disease (IBD). Zharp2-1 blocker muramyl dipeptide (MDP) induces growth of mononuclear cells and induces inflammatory cell factor infection. Zharp2-1 attenuates MDP-induced small inguinal peritonitis, or ameliorates by DNBS-induced large inguinal conjunctivitis .
|
-
- HY-128439
-
|
|
DYRK
|
Cancer
|
|
BT173 is a potent homeodomain interacting protein kinase 2 (HIPK2) inhibitor. BT173 binds to HIPK2 does not inhibit HIPK2 kinase activity but rather, interfered allosterically with the ability of HIPK2 to associate with Smad3. BT173 attenuates renal fibrosis through suppression of the TGF-β1/Smad3 pathway .
|
-
- HY-163030
-
|
|
Elastase
NF-κB
p38 MAPK
Bacterial
|
Infection
Inflammation/Immunology
|
|
LasB-IN-1 (compound 5f) is a potent and orally active inhibitor of LasB (IC50 = 8.7 μM). LasB-IN-1 effectively attenuates elastase production and biofilm formation by P. aeruginosa while alleviating the inflammatory response through downregulating MAPK and NF-κB pathways. LasB-IN-1 is potential to be a novel anti-infective candidate against drug-resistant infections .
|
-
- HY-101761A
-
|
|
PAI-1
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
TM5441 is an orally bioavailable inhibitor of plasminogen activator inhibitor-1 (PAI-1), has IC50 values between 13.9 and 51.1 μM. TM5441 induces intrinsic apoptosis in several human cancer cell lines. TM5441 attenuates Nω-nitro-l-arginine methyl ester-induced cardiac hypertension and vascular senescence .
|
-
- HY-163280
-
|
|
NAMPT
|
Neurological Disease
|
|
JGB-1-155 is a positive allosteric modulators (N-PAMs), which enhances the activity of nicotinamide phosphoribosyltransferase NAMPT with EC50 of 3.29 μM. JGB-1-155 counteracts the oxidative stress, through upregulating the NAD + in THP-1 human monocytes. JGB-1-155 attenuates TNFα-induced ROS in HT-22 cells .
|
-
- HY-162430
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 206 (Compound 10e) is a indolylacryloyl-derived oxacins, which exhibits broad antibacterial spectrum with MIC of 0.25-1 μg/mL. Antibacterial agent 206 reduces the exopolysaccharide, eliminates the biofilm, and thus attenuates the drug resistance. Antibacterial agent 206 exhibits antibacterial activity through destory of membrane integrity, accumulation of reactive oxygen species ROS, and inhibition of DNA replication .
|
-
- HY-161620
-
|
|
IRAK
|
Inflammation/Immunology
|
|
DW18134 is an inhibitor for interleukin receptor-associated kinase 4 (IRAK 4) with an IC50 of 11.2 nM. DW18134 inhibits phosphorylation of IRAK4 and IKK, downregulates the secretion of TNF-α and IL-6. DW18134 attenuates the Lipopolysaccharides (HY-D1056)-induced peritonitis and DSS-induced colitis in mouse models, and protects the intestinal barrier function .
|
-
- HY-B0673R
-
|
|
TGF-beta/Smad
CCR
|
Inflammation/Immunology
Cancer
|
|
Pirfenidone (Standard) is the analytical standard of Pirfenidone. This product is intended for research and analytical applications. Pirfenidone (AMR69) is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities .
|
-
- HY-N0293R
-
|
|
HSP
|
Infection
Neurological Disease
Cancer
|
|
Paeoniflorin (Standard) is the analytical standard of Paeoniflorin. This product is intended for research and analytical applications. Paeoniflorin is a heat shock protein-inducing compound and commonly exists in the plants of Paeoniaceae family, with various biological activities, including anticancer activity, anti-inflammatory activity, enhancing cognition and attenuating learning impairment, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, and reducing blood viscosity .
|
-
- HY-N2638R
-
|
|
Apoptosis
|
Cardiovascular Disease
|
|
Ilexsaponin A (Standard) is the analytical standard of Ilexsaponin A. This product is intended for research and analytical applications. Ilexsaponin A, isolated from the root of Ilex pubescens, attenuates ischemia-reperfusion-induced myocardial injury through anti-apoptotic pathway. Ilexsaponin A can reduce myocardial infarct size, lower the serum levels of LDH, AST and CK-MB, increase cellular viability and inhibit apoptosis in hypoxia/reoxygenation cardiomyocytes .
|
-
- HY-N0496R
-
|
|
NOD-like Receptor (NLR)
|
Cardiovascular Disease
|
|
Ruscogenin (Standard) is the analytical standard of Ruscogenin. This product is intended for research and analytical applications. Ruscogenin, an important steroid sapogenin derived from Ophiopogon japonicus, attenuates cerebral ischemia-induced blood-brain barrier dysfunction by suppressing TXNIP/NLRP3 inflammasome activation and the MAPK pathway. Ruscogenin exerts significant anti-inflammatory and anti-thrombotic activities. Ruscogenin has orally bioactivity .
|
-
- HY-16689
-
|
|
Potassium Channel
|
Others
|
|
VU 0240551 is a potent neuronal K-Cl cotransporter KCC2 inhibitor (IC50=560 nM) and is selective versus NKCC1. VU 0240551 also inhibits hERG and L-type Ca 2+ channels. VU 0240551 attenuates GABA-induced hyperpolarization of P cells, produces a positive shift in the P cell GABA reversal potential and enhances P cell synaptic transmission .
|
-
- HY-N0774
-
|
|
ERK
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
|
-
- HY-P1410
-
|
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
|
-
- HY-12363
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
U-69593 is a potent and selective κ1-opioid receptor agonist . U-69593 attenuates addictive agent-induced behavioral sensitization in the rat . U-69593 reduces anxiety and enhances spontaneous alternation memory in mice . U-69593 reduces calcium-dependent dialysate levels of dopamine and glutamate in the ventral striatum .
|
-
- HY-120657
-
|
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
|
|
9-PAHSA is an orally available anti-inflammatory lipid that lowers blood sugar and reduces inflammation. 9-PAHSA also improved carotid vascular calcification and attenuates cardiac hypertrophy and dysfunction in db/db mice. 9-PAHSA increases the viability of steatosis primary mouse hepatocytes (PMH). 9-PAHSA can be used in research on diabetes, inflammation, and cardiovascular disease .
|
-
- HY-B0011R
-
|
RP-56976 (Standard)
|
Microtubule/Tubulin
Apoptosis
Endogenous Metabolite
|
Cancer
|
|
Docetaxel (Standard) is the analytical standard of Docetaxel. This product is intended for research and analytical applications. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity .
|
-
- HY-162429
-
|
|
Bacterial
|
Infection
|
|
Antibacterial agent 205 (Compound 10d) is a indolylacryloyl-derived oxacins, which exhibits broad antibacterial spectrum with MIC of 0.25-0.5 μg/mL. Antibacterial agent 205 reduces the exopolysaccharide, eliminates the biofilm, and thus attenuates the drug resistance. Antibacterial agent 205 exhibits antibacterial activity through destory of membrane integrity, accumulation of reactive oxygen species ROS, and inhibition of DNA replication .
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-
- HY-121152
-
-
- HY-14266A
-
|
|
Apoptosis
Reverse Transcriptase
Autophagy
HIV
|
Infection
|
|
Dapivirine hydrochloride is a non-nucleoside reverse transcriptase inhibitor with antitumor activity. Dapivirine hydrochloride attenuates the proliferation of glioblastoma cells and induces apoptosis. Dapivirine hydrochloride modulates autophagy and activates Akt, Bad, and SAPK/JNK signaling pathways. Dapivirine hydrochloride has shown inhibitory effects on glioma cell growth both in vitro and in vivo. Dapivirine hydrochloride is also a promising drug candidate for topical microbial agents for the prevention of sexual transmission of HIV-1 .
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-
- HY-119467
-
|
|
Ser/Thr Protease
|
Cancer
|
|
MDK0734 is a selective inhibitor that inhibits feline hepsin B endopeptidase and exopeptidase activities. MDK0734 demonstrated efficacy in a cell-based in vitro tumor invasion model, significantly attenuating the invasive ability of MCF-10A neoT cells. MDK0734 provides new potential inhibitors for the development of clinically useful compounds targeting the deleterious effects of feline hepsin B in cancer progression .
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-
- HY-D0067
-
|
DEAC; Coumarin D 1421; D 1421
|
Monocarboxylate Transporter
|
Cancer
|
|
7ACC1 (DEAC; Coumarin D 1421; D 1421) is a monocarboxylate transporter 1 (MCT-1)/MCT-4 specifc blocker. 7ACC1 attenuates renal cancer cell proliferation, migration, invasion and down-regulates the levels of MCT1/MCT4 expression and extracellular lactate. 7ACC1 is promising for research of cancers .
|
-
- HY-B1118
-
|
RP-14539; PM-185184
|
Parasite
Antibiotic
Bacterial
|
Infection
|
|
Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
|
-
- HY-B1331
-
|
Cyromazin; CGA-72662
|
Endogenous Metabolite
Parasite
|
Neurological Disease
Metabolic Disease
|
|
Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
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-
- HY-B1671
-
|
|
GABA Receptor
Sodium Channel
Calcium Channel
|
Neurological Disease
Metabolic Disease
|
|
(+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na + and Ca 2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
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-
- HY-P1410A
-
|
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
|
-
- HY-145196
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats .
|
-
- HY-121246S
-
|
AKF-PD-d3
|
Isotope-Labeled Compounds
Akt
PI3K
|
Inflammation/Immunology
|
|
Fluorofenidone-d3 is deuterium labeled Fluorofenidone. Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway[1][2].
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-
- HY-B1118A
-
|
RP-14539 hemihydrate; PM-185184 hemihydrate
|
Antibiotic
Bacterial
Parasite
|
Infection
|
|
Secnidazole (RP-14539) hemihydrate is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole hemihydrate, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole hemihydrate has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole hemihydrate can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
|
-
- HY-124056
-
|
|
CXCR
|
Cancer
|
|
AZ10397767 is an orally active, selective CXCR2 receptor antagonist with an IC50 of 1 nM. AZ10397767 attenuates the Oxaliplatin (HY-17371)-induced NF-κB transcriptional activity and potentiates Oxaliplatin-induced apoptosis in androgen-independent prostate cancer (AIPC) cells. AZ10397767 significantly inhibits neutrophil recruitment into tumors which then adversely affects tumor growth in vitro and in vivo .
|
-
- HY-155491
-
|
|
Bacterial
|
Cancer
|
|
Antibacterial agent 166 (Compound 19q), a derivative of Nitisinone (HY-B0607), is a selective and orally active Fusobacterium nucleatum inhibitor with a MIC50 of 1 μg/mL. Antibacterial agent 166 effectively attenuates the migratory ability of MC-38 cells induced by Fusobacterium nucleatum. Antibacterial agent 166 is a promising anti-F. nucleatum lead compound and can be used for colorectal cancer (CRC) research .
|
-
- HY-162280
-
|
|
PROTACs
RANKL/RANK
Nuclear Factor of activated T Cells (NFAT)
Btk
|
Cancer
|
|
PROTAC BTK Degrader-9 (compound 23) is a PROTAC degrader that effectively targets BTK. PROTAC BTK Degrader-9 downregulates the BTK-PLCγ2-Ca 2+-NFATc1 signaling pathway activated by RANKL. Thus, PROTAC BTK Degrader-9 was able to inhibit osteoclastogenesis and attenuate alveolar bone resorption in a mouse periodontitis model .
|
-
- HY-123480
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
EGIS-7625 is a selective and competitive 5-HT2B inhibitor with pKi values of 9.0, 6.2, 7.7 for 5-HT2B, 5-HT2A, 5-HT2C, respective. EGIS-7625 partially attenuates m-chlorophenylpiperazine-induced hypomotility and hypophagia .
|
-
- HY-111093
-
|
|
CaMK
|
Neurological Disease
|
|
Protein kinase inhibitor 8 (Compound CK59) is a calmodulin-dependent protein kinase II (CaMKII) inhibitor. By inhibiting the activity of CaMKII, Protein kinase inhibitor 8 can attenuate the cytotoxicity induced by perfluorooctane sulfonic acid (PFOS) and alleviate the downregulation of GLT-1 expression caused by PFOS, thereby reducing neuronal damage. Protein kinase inhibitor 8 may be useful in research related to neurodegenerative diseases .
|
-
- HY-N6869R
-
|
|
Antibiotic
PPAR
Bacterial
Fungal
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-70050A
-
|
GR 68755; GR 68755X
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Alosetron (GR 68755) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-70050C
-
|
GR 68755C; GR 68755 Hydrochloride; GR 68755X Hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-N0148
-
|
Rutoside; Quercetin 3-O-rutinoside
|
Amyloid-β
Autophagy
Apoptosis
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Rutin (Rutoside) is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin is also a CBR1 inhibitor, which can cross the blood brain barrier. Rutin attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress .
|
-
- HY-126252
-
|
|
ROR
Interleukin Related
|
Inflammation/Immunology
|
|
A-9758 is a RORγ ligand and a potent, selective RORγt inverse agonist (IC50=5 nM), and exhibits robust potency against IL-17A release. A-9758 is effective in suppressing both Th17 differentiation and Th17 effector function. A-9758 significantly attenuates IL-23 driven psoriasiform dermatitis and is effective in blocking skin and joint inflammation .
|
-
- HY-100848
-
|
|
EGFR
|
Cancer
|
|
TX1-85-1 is an irreversible Her3 (ErbB3) inhibitor with an IC50 of 23 nM. TX1-85-1 is also the first selective Her3 ligand, which forms a covalent bond with Cys721 located in the ATP-binding site of Her3. TX1-85-1 induces partial degradation of Her3 protein and attenuates Her3-dependent signaling .
|
-
- HY-112671
-
|
RTA dh404
|
Keap1-Nrf2
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB . CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats .
|
-
- HY-135457
-
|
|
Phosphatase
|
Cancer
|
|
JMS-053 is a potent, selective and reversible PTP4A inhibitor, with IC50s of 29.1 nM, 48.0 nM, 34.7 nM, 92.6 nM, and 207.6 nM for PTP4A1, PTP4A2, PTP4A3, CDC25B, and DUSP3, respectively. JMS-053 can inhibit cancer cell migration and spheroid growth in vitro, attenuate in vivo ovarian tumor growth .
|
-
- HY-P99008
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Atibuclimab, is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab can be used for the research of amyotrophic lateral sclerosis . Atibuclimab attenuates LPS-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist .
|
-
- HY-P3960
-
|
|
Thyroid Hormone Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS .
|
-
- HY-152142
-
|
|
JNK
|
Neurological Disease
|
|
DN-1289 is an orally active and selective inhibitor of dual leucine zipper kinase (DLK; IC50=17 nM) and leucine zipper-bearing kinase (LZK; IC50=40 nM). DN-1289 results significant attenuation of optic nerve crush (ONC)-induced p-c-Jun in mice model. DN-1289 has excellent in vivo plasma half-life and blood-brain barrier permeability .
|
-
- HY-120485
-
|
IRFI-016
|
p38 MAPK
ERK
PKC
|
Cardiovascular Disease
|
|
Raxofelast (IRFI-016) is an antioxidant agent in various models of ischemia-reperfusion injury. Raxofelast has antiproliferative activity in H2O2-stimulated rat aortic smooth muscle cells. Raxofelast attenuates the activation of mitogen-activating protein kinase (MAPK), ERK kinase 1, 2 (MEK1,2) and protein kinase C (PKC) without affecting Ras expression .
|
-
- HY-12678R
-
|
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
|
Cancer
|
|
Entrectinib (Standard) is the analytical standard of Entrectinib. This product is intended for research and analytical applications. Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-B1328R
-
|
|
Endogenous Metabolite
Keap1-Nrf2
|
Neurological Disease
Cancer
|
|
Pyridoxine (Standard) is the analytical standard of Pyridoxine. This product is intended for research and analytical applications. Pyridoxine (Pyridoxol) is a pyridine derivative. Pyridoxine exerts antioxidant effects in cell model of Alzheimer's disease via the Nrf-2/HO-1 pathway.
In Vitro: Pyridoxine exerts a protective potential against AD, attenuates ROS levels, decreases the expressions of cytoplasmic Nrf2, and upregulates whole-cell HO-1 expression .
|
-
- HY-Z0283R
-
|
|
Endogenous Metabolite
PARP
|
Others
|
|
Benzamide (Standard) is the analytical standard of Benzamide. This product is intended for research and analytical applications. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
|
-
- HY-168705
-
|
|
Bacterial
|
Infection
|
|
Anti-MRSA agent 20 (Compound a4) is an anti-microbial agent (MIC: < 0.03125 μg/mL) against MRSA). Anti-MRSA agent 20 binds to the ribosomal peptidyl transferase center and inhibits bacterial survival by inhibiting MRSA toxin synthesis and bacterial division. Anti-MRSA agent 20 significantly reduces the MRSA load in the lungs and attenuates lung injury in the MRSA-infected mice (ED50 = 6.48 mg/kg) .
|
-
- HY-B0075
-
|
N-Acetyl-5-methoxytryptamine
|
Melatonin Receptor
Autophagy
Mitophagy
Endogenous Metabolite
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
|
-
- HY-18555
-
TMPA
2 Publications Verification
|
Nuclear Hormone Receptor 4A/NR4A
AMPK
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
TMPA is a high-affinity Nur77 antagonist that binds to Nur77 leading to the release and shuttling of LKB1 in the cytoplasm to activate AMPKα. TMPA effectively lowers blood glucose and attenuates insulin resistance in type II db/db, high-fat diet and streptozotocin-induced diabetic mice. TMPA reduces RICD (restimulation-induced cell death) in human T cells, can also be used in studies of cancer and T-cell apoptosis dysregulation .
|
-
- HY-101561
-
|
BLU-285
|
c-Kit
PDGFR
|
Cancer
|
|
Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
|
-
- HY-109086
-
|
JNJ-40346527; JNJ-527
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
|
|
Edicotinib (JNJ-40346527) is a potent, selective, brain penetrant and orally active colony-stimulating factor-1 receptor (CSF-1R) inhibitor with an IC50 of 3.2 nM. Edicotinib exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively . Edicotinib limits microglial expansion and attenuates microglial proliferation and neurodegeneration in mice. Edicotinib has the potential for Alzheimer’s disease and rheumatoid arthritis research .
|
-
- HY-A0143S
-
|
DGLA-d6; all-cis-8,11,14-Eicosatrienoic acid-d6
|
Endogenous Metabolite
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
|
-
- HY-101193
-
|
Zn(II)-protoporphyrin IX; ZnPP; Zinc Protoporphyrin-9
|
Reactive Oxygen Species
Endogenous Metabolite
Apoptosis
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
|
-
- HY-123611
-
|
RX-5902
|
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase (P-p68) and a potent first-in-class anti-cancer agent. Supinoxin interacts with Y593 phosphorylated-p68 and attenuates the nuclear shuttling of β-catenin. Supinoxin induces cell apoptosis and inhibits growth of TNBC cancer cell lines with IC50s ranging from 10 nM to 20 nM .
|
-
- HY-11052A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
Trap-101 hydrochloride is a potent, selective and competitive antagonist of NOP receptors over classical opioid receptors. Trap-101 stimulates GTPγ 35S binding to CHOhNOP membranes with pKi values of 8.65, 6.60, 6.14 and <5 for NOP, μ-, κ-, and δ-opioid receptors, respectively. Trap-101 attenuates motor deficits in a rat model of parkinson's disease and can be used for the research of nervous system diseases .
|
-
- HY-B0011AS
-
|
RP-56976-d5 trihydrate
|
Isotope-Labeled Compounds
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM[1]. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis[1][3].
|
-
- HY-120553
-
|
|
Apoptosis
|
Neurological Disease
|
|
B355252, a phenoxy thiophene sulfonamide small molecule, is a potent NGF receptor agonist. B355252 potentiates NGF-induced neurite outgrowth. B355252 protects ischemic neurons from neuronal loss by attenuating DNA damage, reducing ROS production and the LDH level, and preventing neuronal apoptosis. B355252 has anti-apoptotic effects in glutamate-induced excitotoxicity, as well as in a murine hippocampal cell line (HT22) model of Parkinson disease (PD) .
|
-
- HY-146351
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC-IN-38 (compound 13) is a potent HDAC inhibitor. HDAC-IN-38 shows similar micro-molar inhibitory activity toward HDAC1, 2, 3, 5, 6, and 8. HDAC-IN-38 increases cerebral blood flow (CBF), attenuates cognitive impairment, and improves hippocampal atrophy. HDAC-IN-38 also increases the level of histone acetylation (H3K14 or H4K5) .
|
-
- HY-120349
-
|
|
p38 MAPK
JNK
Apoptosis
Reactive Oxygen Species
|
Cancer
|
|
LL-Z1640-4 is a potent p38/JNK signaling inhibitor. LL-Z1640-4 significantly diminishes p38 and JNK activation in HCC cells transfected with MLK4 siRNA. LL-Z1640-4 markedly attenuates ROS production induced by MLK4 knockdown. LL-Z1640-4 significantly reduces the apoptotic cells in HCC cells transfected with siMLK4 .
|
-
- HY-P99165
-
|
|
IGF-1R
TSH Receptor
|
Endocrinology
|
|
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .
|
-
- HY-P1698
-
|
AB-103
|
Bacterial
CD28
|
Infection
Inflammation/Immunology
Cancer
|
|
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs) .
|
-
- HY-123982
-
|
|
Others
|
Neurological Disease
|
|
SOD1-Derlin-1 inhibitor-2 (compound 56-59) is an inhibitor of SOD1-Derlin-1 interaction. SOD1-Derlin-1 inhibitor-2 attenuates the interactions between Derlin-1 and SOD1 mut. SOD1-Derlin-1 inhibitor-2 can be used for the research of amyotrophic lateral sclerosis (ALS) .
|
-
- HY-148552
-
|
|
p38 MAPK
ERK
NF-κB
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 35 (compound 5a27) is an orally active curcumin analogue with anti-inflammatory activity. Anti-inflammatory agent 35 blocks mitogen-activated protein kinase (MAPK) signaling and p65 nuclear translocation of NF-kB. Anti-inflammatory agent 35 also inhibits yellow neutrophil infiltration and pro-inflammatory cytokine production. Anti-inflammatory agent 35 significantly attenuates lipopolysaccharide (LPS)-induced acute lung injury (ALI) in vivo .
|
-
- HY-143327
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
PROTAC BRD4 Degrader-16 is a potent PROTAC BRD4 Degrader, with IC50 values of 34.58 nM (BRD4 (BD1)) and 40.23 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-16 ignificantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-16 significantly induces apoptosis in MV-4-11 cells .
|
-
- HY-149472
-
|
|
NF-κB
PI3K
|
Inflammation/Immunology
|
|
Anti-osteoporosis agent-4 (Compound 11h) inhibits differentiation of primary osteoclasts. Anti-osteoporosis agent-4 attenuates RANKL-induced osteoclastogenesis. Anti-osteoporosis agent-4 inhibits osteoclast formation with an IC50 value of 358.29 nM. Anti-osteoporosis agent-4 inhibits PI3K/AKT and IκBα/NF-κB signaling pathway activation .
|
-
- HY-163355
-
|
|
COX
Lipoxygenase
NF-κB
|
Inflammation/Immunology
|
|
COX-2/15-LOX-IN-5 (Compound 4f) is a dual inhibitor of COX-2/15-LOX. COX-2/15-LOX-IN-5 attenuates increased NF-κB activation in RAW 264.7 macrophages mediated by lipopolysaccharide (HY-D1056). COX-2/15-LOX-IN-5 has anti-inflammatory and antioxidant activities .
|
-
- HY-101415R
-
|
|
Apoptosis
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Coenzyme Q9 (Standard) is the analytical standard of Coenzyme Q9. This product is intended for research and analytical applications. Coenzyme Q9 (Ubiquinone Q9), the major form of ubiquinone in rodents, is an amphipathic molecular component of the electron transport chain that functions as an endogenous antioxidant. Coenzyme Q9 attenuates the diabetes-induced decreases in antioxidant defense mechanisms. Coenzyme Q9 improves left ventricular performance and reduces myocardial infarct size and cardiomyocyte apoptosis .
|
-
- HY-N6967R
-
|
|
Apoptosis
|
Neurological Disease
Inflammation/Immunology
|
|
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-159484
-
|
|
HSP
Guanylate Cyclase
|
Cardiovascular Disease
|
|
Hsp110/sGC-modulator-1 (compound 17i), an orally active Hsp110/sGC dual-target regulator, exhibits optimal Hsp110 and sGC molecular activities as well as remarkable cell malignant phenotypes inhibitory and vasodilatory effects. Hsp110/sGC-modulator-1 (compound 17i) attenuates pulmonary vascular remodeling and right ventricular hypertrophy via Hsp110 suppression .
|
-
- HY-123411
-
|
BCI 632
|
mGluR
|
Neurological Disease
|
MGS0039 is a type II group mGluR antagonist. MGS0039 has a high affinity for mGluR2 and mGluR3, with Ki values of 2.2 nM and 4.5 nM, respectively. MGS0039 can attenuate the inhibitory effect of glutamate-induced cyclic AMP formation triggered by Forskolin (HY-15371) in CHO cells expressing mGluR2/mGluR3. MGS0039 shows antidepressant-like activity in rats .
|
-
- HY-118575
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
DR-4004 is a 5-HT7 receptor antagonist that attenuates the decreased level of performance produced by mCPP and the performance levels after p-chloroamphetamine (PCA) lesion of the 5-HT system. DR-4004 also reverses amnesia induced by Scopolamine (HY-N0296) and Dizocilpine (HY-15084B). DR-4004 is promising for research of schizophrenia, cognitive deficits and atypical antipsychotic agents .
|
-
- HY-109086A
-
|
JNJ-40346527 hydrochloride; JNJ-527 hydrochloride
|
c-Fms
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Edicotinib hydrochloride is a potent, selective, brain penetrant and orally active?colony-stimulating factor-1 receptor (CSF-1R)?inhibitor with an IC50 of 3.2 nM. Edicotinib hydrochloride exhibits less inhibitory effects on KIT and FLT3 with IC50 values of 20 nM and 190 nM, respectively . Edicotinib hydrochloride limits microglial expansion and attenuates microglial proliferation and neurodegeneration?in mice. Edicotinib hydrochloride has the potential for Alzheimer’s disease and rheumatoid arthritis research .
|
-
- HY-121299
-
|
mCPBG
|
5-HT Receptor
|
Neurological Disease
|
|
m-Chlorophenylbiguanide (mCPBG) is a potent high-affinity agonist of the 5-HT3 receptor, exhibiting an inhibitory effect on long-term potentiation (LTP) in the mossy fiber-CA3 system. mCPBG attenuates the magnitude of LTP at concentrations of 0.3-1 microM, demonstrating its role in modulating synaptic plasticity. Additionally, the impact of mCPBG on LTP is reversible by the GABAA receptor antagonist bicuculline, indicating a connection between its action and GABAergic neurotransmission.
|
-
- HY-13207
-
|
PR-957
|
Proteasome
Bacterial
HIV
|
Infection
Inflammation/Immunology
|
|
ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
|
-
- HY-N1584
-
|
RU-19110
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-W012974
-
|
β-Aminoisobutyric acid; BAIBA
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
3-Aminoisobutyric acid (β-Aminoisobutyric acid) has anti-inflammatory and antioxidant effects. 3-Aminoisobutyric acid increases the expression of brown adipocyte-specific genes in white adipose tissue and fatty acid β-oxidation in hepatocytes. 3-Aminoisobutyric acid attenuates insulin resistance and inflammation induced by palmitate or a high fat diet via an AMPK–PPARδ-dependent pathway in mice. 3-Aminoisobutyric acid is a catabolic metabolite of thymine and valine in skeletal muscle .
|
-
- HY-59291
-
|
|
Endogenous Metabolite
Amino Acid Derivatives
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Levacetylleucine, an orally bioavailable and brain-penetrant endogenous metabolite, is an acetylated derivative of amino acid leucine. Levacetylleucine is the active form of N-acetyl-leucine (NAL). Levacetylleucine attenuates neuronal death and neuroinflammation in the cortical tissue of mice. Levacetylleucine also potentially improves ameliorates lysosomal and metabolic dysfunction. Levacetylleucine improves compensation of postural symptoms after unilateral chemical labyrinthectomy (UL) in rats. Levacetylleucine is promising for research of neurological manifestations of Niemann-Pick disease type C, traumatic brain injury and neurodegeneration prevention .
|
-
- HY-N2118
-
|
|
PPAR
PKA
Akt
p38 MAPK
ERK
|
Metabolic Disease
|
|
Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity .
|
-
- HY-117482
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-W014421
-
|
|
TRP Channel
|
Neurological Disease
|
|
AP-18, a potent and selective TRPA1 inhibitor, blocks activation of TRPA1 by 50 μM Cinnamaldehyde with an IC50 of 3.1 μM and 4.5 μM for human and mouse TRPA1, respectively. AP-18 reverses complete Freund's adjuvant (CFA)-induced mechanical hyperalgesia in mice. AP-18 attenuated 30 μM AITC-induced Yo-Pro uptake in a concentration-dependent manner, with an IC50 of 10.3 μM .
|
-
- HY-117482A
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-P1435
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-B1118S2
-
|
RP-14539-d4; PM-185184-d4
|
Bacterial
Parasite
Antibiotic
|
Infection
|
|
Secnidazole-d4 is the deuterium labeled Secnidazole[1]. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
|
-
- HY-143328
-
|
|
PROTACs
Epigenetic Reader Domain
Apoptosis
|
Cancer
|
|
PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells .
|
-
- HY-N10330
-
|
|
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
Cancer
|
|
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer .
|
-
- HY-P1698B
-
|
AB-103 TFA
|
Bacterial
CD28
|
Infection
Inflammation/Immunology
Cancer
|
|
Reltecimod (AB-103) TFA is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod TFA has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod TFA modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod TFA can be used to research necrotizing soft-tissue infections (NSTIs) .
|
-
- HY-145491
-
|
|
ERK
NF-κB
|
Inflammation/Immunology
|
|
Resolvin D5 is a prolytic mediator (SPM) with anti-inflammatory activity derived from oxidized lipids DHA. Resolvin D5 inhibits Th17 cell differentiation and promotes regulatory T cell differentiation, and inhibits CD4+ T cell proliferation. Resolvin D5 attenuates osteoclast differentiation and interferes with osteoclastogenesis. Resolvin D5 also regulates ERK phosphorylation and nuclear translocation of NF-kappaB. Resolvin D5 could be used in rheumatoid arthritis research .
|
-
- HY-157992
-
-
- HY-B1118R
-
|
|
Parasite
Antibiotic
Bacterial
|
Infection
|
|
Secnidazole (Standard) is the analytical standard of Secnidazole. This product is intended for research and analytical applications. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis .
|
-
- HY-124219
-
|
17-Phenoxy trinor PGF2α ethyl amide
|
Prostaglandin Receptor
|
Others
|
|
17-Phenoxy trinor prostaglandin F2α ethyl amide (17-Phenoxy trinor PGF2α ethyl amide) is an analog of Bimatoprost (HY-12956). 17-Phenoxy trinor prostaglandin F2α ethyl amide is an agonist for Prostaglandin F2α Receptor (FP receptor). 17-Phenoxy trinor prostaglandin F2α ethyl amide is potent to reduce the intraocular pressure and attenuate the glaucoma .
|
-
- HY-161668
-
|
|
Ligands for E3 Ligase
Ferroptosis
|
Cancer
|
|
Ru-Poma is a Ru(II)-based photosensitizer, which attenuates Cisplatin (HY-17394)-resistant tumor through photodynamic therapy (PDT). Ru-Poma photodegrades CRBN through a Pomalidomide (HY-10984) moiety. Ru-Poma induces ferroptosis, through an increase in lipid peroxide, downregulation of GPX4 and GAPDH expression. Ru-Poma exhibits cytotoxicity in A549, with IC50 of 18.46 μM and 0.37 μM in dark and upon irradiation, respectively .
|
-
- HY-165098
-
|
β-Aminoisobutyric acid sodium salt; BAIBA sodium salt
|
Endogenous Metabolite
|
Cardiovascular Disease
Metabolic Disease
|
|
3-Aminoisobutyric acid (β-Aminoisobutyric acid) sodium salt has anti-inflammatory and antioxidant effects. 3-Aminoisobutyric acid sodium salt increases the expression of brown adipocyte-specific genes in white adipose tissue and fatty acid β-oxidation in hepatocytes. 3-Aminoisobutyric acid sodium salt attenuates insulin resistance and inflammation induced by palmitate or a high fat diet via an AMPK–PPARδ-dependent pathway in mice. 3-Aminoisobutyric acid sodium salt is a catabolic metabolite of thymine and valine in skeletal muscle .
|
-
- HY-B1671R
-
|
|
GABA Receptor
Sodium Channel
Calcium Channel
|
Neurological Disease
Metabolic Disease
|
|
(+)-Kavain (Standard) is the analytical standard of (+)-Kavain. This product is intended for research and analytical applications. (+)-Kavain, a main kavalactone extracted from Piper methysticum, has anticonvulsive properties, attenuating vascular smooth muscle contraction through interactions with voltage-dependent Na+ and Ca2+ channels . (+)-Kavain is shown to bind at the α4β2δ GABAA receptor and potentiate GABA efficacy . (+)-Kavain is used as a treatment for inflammatory diseases, its anti-inflammatory action has been widely studied .
|
-
- HY-B0011AR
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
Docetaxel (Trihydrate) (Standard) is the analytical standard of Docetaxel (Trihydrate). This product is intended for research and analytical applications. Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule?depolymerization with an IC50 value of 0.2 μM . Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of?bcl-2?and?bcl-xL?gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis .
|
-
- HY-B1331R
-
|
|
Endogenous Metabolite
Parasite
|
Neurological Disease
Metabolic Disease
|
|
Cyromazine (Standard) is the analytical standard of Cyromazine. This product is intended for research and analytical applications. Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
|
-
- HY-N0774R
-
|
|
ERK
COX
MMP
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Isofraxidin (Standard) is the analytical standard of Isofraxidin. This product is intended for research and analytical applications. Isofraxidin, a coumarin component from Acanthopanax senticosus, inhibits MMP-7 expression and cell invasion of human hepatoma cells. Isofraxidin inhibits the phosphorylation of ERK1/2 in hepatoma cells . Isofraxidin attenuates the expression of iNOS and COX-2, Isofraxidinalso inhibits TLR4/myeloid differentiation protein-2 (MD-2) complex formation .
|
-
- HY-107719
-
|
|
iGluR
|
Neurological Disease
|
|
D-AP7 is a specific NMDA receptor antagonist with inhibitory activity against epileptiform activity. D-AP7 attenuated neuronal activation in spot activity by reducing the duration and number of exogenously induced bursts. D-AP7 also increased the amplitude of secondary action potentials, which may restore neuronal activity in some epileptiform bursts. D-AP7 showed anxiogenic effects and impaired memory consolidation in passive avoidance learning .
|
-
- HY-N1584C
-
|
RU-19110 lactate
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone lactate, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone lactate is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone lactate is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone lactate has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-N0107R
-
|
|
Apoptosis
Autophagy
mTOR
Akt
|
Cardiovascular Disease
|
|
Cyclovirobuxine D (Standard) is the analytical standard of Cyclovirobuxine D. This product is intended for research and analytical applications. Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR . Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis . Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction .
|
-
- HY-N6871
-
|
|
Bacterial
IKK
Ferroptosis
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-14536
-
|
Basic Blue 9; CI-52015; Methylthioninium chloride
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Infection
Neurological Disease
Cancer
|
|
Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
-
- HY-10450A
-
|
BMS-512148 (2S)-1,2-propanediol, hydrate
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-N0457
-
|
Cichoric acid; Dicaffeoyltartaric acid
|
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
|
|
Chicoric acid (Cichoric acid), an orally active dicaffeyltartaric acid, induces reactive oxygen species (ROS) generation. Chicoric acid inhibits cell viability and induces mitochondria-dependent apoptosis in 3T3-L1 preadipocytes through ROS-mediated PI3K/Akt and MAPK signaling pathways. Chicoric acid increases glucose uptake, improves insulin resistance, and attenuates glucosamine-induced inflammation. Chicoric acid has antidiabetic properties and antioxidant, anti-inflammatory effects .
|
-
- HY-N1584A
-
|
RU-19110 hydrobromide
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-106353
-
|
|
mAChR
Endogenous Metabolite
|
Neurological Disease
|
|
Smilagenin (SMI) is a small-molecule steroidal sapogenin from Anemarrhena asphodeloides and Pelargonium hortorum widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases .
Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density .
Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD .
|
-
- HY-113402A
-
|
γ-Glutamylcysteine TFA
|
Interleukin Related
TNF Receptor
Endogenous Metabolite
|
Inflammation/Immunology
|
|
Gamma-glutamylcysteine (γ-Glutamylcysteine) TFA, an intermediate in glutathione (GSH) synthesis, is a dipeptide served as an essential cofactor for the antioxidant enzyme glutathione peroxidase (GPx). Gamma-glutamylcysteine TFA also upregulates the level of the anti-inflammatory cytokine IL-10 and reduces the levels of the pro-inflammatory cytokines (TNF-α, IL-6, and IL-1β). Gamma-glutamylcysteine TFA attenuates the changes in metalloproteinase activity in oligomeric Aβ40-treated astrocytes .
|
-
- HY-P1435A
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds TFA is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds TFA can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-P1723A
-
|
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
|
-
- HY-13207A
-
|
PR-957 TFA
|
Proteasome
Bacterial
HIV
|
Infection
Inflammation/Immunology
|
|
ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
|
-
- HY-141882
-
|
|
Atg8/LC3
Autophagy
|
Infection
Inflammation/Immunology
Cancer
|
|
DC-LC3in-D5 acts as an autophagy inhibitor by attenuating LC3B lipidation. DC-LC3in-D5 binds with LC3B. DC-LC3in-D5 disrupts the LC3B-LBP2 interaction with an IC50 of 200 nM. DC-LC3in-D5 may contribute to anti-HCV or combination researchs in cancer through inhibiting autophagy .
|
-
- HY-150026
-
|
|
VEGFR
PDGFR
FGFR
c-Kit
Akt
Src
Apoptosis
|
Cancer
|
|
Multi-kinase-IN-2 (compound 7h) is an orally active and potent angiokinase inhibitor. Multi-kinase-IN-2 exhibits excellent inhibitory activity against angiokinases including VEGFR-1/2/3, PDGFRα/β, and FGFR-1, as well as LYN and c-KIT kinases. Multi-kinase-IN-2 significantly attenuates phosphorylation of AKT and ERK proteins. Multi-kinase-IN-2 induces cell apoptosis. Multi-kinase-IN-2 shows anticancer activity .
|
-
- HY-D0958
-
|
Basic Blue 9 hydrate; CI-52015 hydrate; Methylthioninium chloride hydrate
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Infection
Inflammation/Immunology
Cancer
|
|
Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
-
- HY-149483
-
|
|
nAChR
|
Neurological Disease
|
|
CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
|
-
- HY-12678S
-
|
NMS-E628-d4; RXDX-101-d4
|
ROS Kinase
Trk Receptor
Anaplastic lymphoma kinase (ALK)
Autophagy
Isotope-Labeled Compounds
|
Cancer
|
|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
|
-
- HY-N1584B
-
|
RU-19110 hydrochloride
|
Calcium Channel
DNA/RNA Synthesis
Parasite
Sodium Channel
TGF-beta/Smad
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-70050CR
-
|
GR 68755C (Standard); GR 68755 (Hydrochloride) (Standard); GR 68755X (Hydrochloride) (Standard)
|
5-HT Receptor
|
Neurological Disease
|
|
Alosetron (Hydrochloride) (Standard) is the analytical standard of Alosetron (Hydrochloride). This product is intended for research and analytical applications. Alosetron Hydrochloride (GR 68755C) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride is used for the research of irritable bowel syndrome (IBS). Alosetron blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-101561R
-
|
|
c-Kit
PDGFR
|
Cancer
|
|
Avapritinib (Standard) is the analytical standard of Avapritinib. This product is intended for research and analytical applications. Avapritinib (BLU-285) is a highly potent, selective, and orally active KIT and PDGFRA activation loop mutant kinases inhibitor with IC50s of 0.27 and 0.24 nM for KIT D816V and PDGFRA D842V, respectively. Avapritinib (BLU-285) binds the active conformation of the kinase and shows antitumor activity. Avapritinib (BLU-285) attenuates the transport function of both ABCB1 and ABCG2 .
|
-
- HY-N0148R
-
|
|
Amyloid-β
Autophagy
Apoptosis
Endogenous Metabolite
|
Inflammation/Immunology
Cancer
|
|
Rutin (Standard) is the analytical standard of Rutin. This product is intended for research and analytical applications. Rutin (Rutoside) is a flavonoid found in many plants and shows a wide range of biological activities including anti-inflammatory, antidiabetic, antioxidant, neuroprotective, nephroprotective, hepatoprotective and reducing Aβ oligomer activities. Rutin is also a CBR1 inhibitor, which can cross the blood brain barrier. Rutin attenuates vancomycin-induced renal tubular cell apoptosis via suppression of apoptosis, mitochondrial dysfunction, and oxidative stress .
|
-
- HY-161674
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 4 (compound 1l) is a selective inhibitor of human monoamine oxidase-B (hMAO-B) (IC50=8.3 nM). Monoamine Oxidase B inhibitor 4 also has anti-neuroinflammatory and low neurotoxicity. Monoamine Oxidase B inhibitor 4 can inhibit the release of NO, TNF-α and IL-1β stimulated by LPS and Aβ1-42, and can also attenuate Aβ(1-42)-induced cytotoxicity .
|
-
- HY-124870
-
|
|
HIV
|
Infection
|
|
N.41 is an antiviral agent. N.41 protects APOBEC3G (an antiviral factor) from HIV Vif protein-mediated degradation. N.41 inhibits the Vif-A3G interaction and increases cellular A3G levels and incorporation of A3G into virions, thereby attenuating virus infectivity in a Vif-dependent manner. N.41 inhibits HIV-1 viral replication in PBMCs (IC50: 8.4 μM) .
|
-
- HY-P10851
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
HVEM(14-39) is a B- and T-lymphocyte attenuator (BTLA) peptide inhibitor. HVEM (14-39) can be combined with BTLA with a KD of 0.102 μM. HVEM(14-39) enhances the activation and proliferation of T cells by regulating the expression of BTLA and HVEM in T cells, and promotes the transformation of cells into effector memory T cells. HVEM(14-39) inhibits tumor cell proliferation and promotes late apoptosis. HVEM(14-39) has immunomodulatory effects and can be used in the study of cancer .
|
-
- HY-169858
-
|
|
PGE synthase
|
Inflammation/Immunology
|
|
Prostaglandin E2 Inhibitor 3 (Compound 3) is a selectivity microsomal prostaglandin E synthase-1 (mPGES-1) inhibitor (IC50 = 0.2 µM). Prostaglandin E2 Inhibitor 3 has higher selectivity for mPGES-1 than cyclooxygenases (COX)-1/2, 5-lipoxygenase (5-LO), and soluble epoxide hydrolase (sEH). Prostaglandin E2 Inhibitor 3 has anti-inflammatory activity and can attenuate zymosan-induced peritoneal leukocyte migration in mice .
|
-
- HY-10071
-
Y-27632
Maximum Cited Publications
300 Publications Verification
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-17606
-
|
ACT-334441
|
LPL Receptor
|
Inflammation/Immunology
|
|
Cenerimod (ACT-334441) is a potent, selective and orally active S1P1 receptor modulator, with an EC50 of 1 nM. Cenerimod shows more than 36 fold selctivity for hS1P1 over hS1P2, hS1P3, hS1P4, and hS1P5 receptor subtypes (EC50s=>10000, 228, 2134, and 36 nM, respectively). Cenerimod can attenuate murine experimental autoimmune encephalomyelitis (EAE) and murine sclerodermatous .
|
-
- HY-D0938
-
|
CFSE; 5(6)-Carboxyfluorescein diacetate succinimidyl ester; 5(6)-CFDA N-succinmidyl ester
|
Fluorescent Dye
|
Others
|
|
CFDA-SE is a fluorescent dye that can penetrate the cell membrane. It can react with the free amine group in the cytoskeleton protein inside the cell, and finally form a protein complex with fluorescence. After entering the cell, CFDA-SE locates in the cell membrane, cytoplasm and nucleus, and the fluorescence staining is strongest in the nucleus .
CFDA-SE dye can be uniformly inherited by the cells with cell division and proliferation, and its attenuation is proportional to the number of cell divisions. This phenomenon can be detected and analyzed by flow cytometry under the excitation light of 488 nm, and can be used to detect the proliferation of cells .
|
-
- HY-B0075S2
-
|
N-Acetyl-5-methoxytryptamine-d7
|
Melatonin Receptor
Autophagy
Mitophagy
Endogenous Metabolite
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Melatonin-d7 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress[5].
|
-
- HY-B0075S1
-
|
N-Acetyl-5-methoxytryptamine-d3
|
Melatonin Receptor
Autophagy
Mitophagy
Endogenous Metabolite
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress[5].
|
-
- HY-N6789
-
KT5720
3 Publications Verification
|
PKA
|
Neurological Disease
Cancer
|
|
KT5720 is a potent, cell-permeable, specific, reversible and ATP-competitive PKA inhibitor (IC50=3.3 μM). KT5720 is effective in reversing MDR1-mediated multidrug resistance. KT5720 also reduces the excitability of dorsal root ganglion (DRG) neurons by attenuating Hyperpolarization-activated cyclic nucleotide-gated (HCN) channel activity and reducing intracellular Ca2 + concentrations. KT5720 can be used in the study of haematological malignancies as well as HCN and DRG neuron-related diseases .
|
-
- HY-N0755
-
|
|
Insulin Receptor
GLUT
NF-κB
p38 MAPK
Autophagy
|
Metabolic Disease
Endocrinology
Cancer
|
|
Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines .
|
-
- HY-124619
-
|
|
FKBP
HIV
|
Infection
Neurological Disease
|
|
GPI-1046 is a immunophilin ligand without antibiotic action and attenuates ethanol intake in part through the upregulation of glutamate transporter 1 (GLT1) in PFC and NAc-core. GPI-1046 is an analog of FK506, which is an immunophilin ligand that has been shown neuroprotective effects in neurodegenerative disease models . GPI-1046 readily crosses the blood-brain barrier and promotes the regeneration of dopamine (DA) cells in the CNS in association with functional recovery in rodent models . GPI-1046 improves HIV-associated injury of peripheral nerves .
|
-
- HY-107428
-
|
|
MMP
|
Cardiovascular Disease
|
|
PD-166793 is a potent, selective, orally active and wide‐broad spectrum inhibitor of MMP, exhibiting nanomolar potency against MMP-2, MMP-3 and MMP-13 (IC50=4, 7, and 8 nM, respectively) and micromolar potency vs MMP-1, -7 and -9 (IC50=6.0, 7.2, and 7.9 μM, respectively). PD-166793 can attenuate left ventricular remodeling and dysfunction in a rat model of progressive heart failure .
|
-
- HY-121035
-
|
7-Bromoindirubin-3-Oxime
|
CDK
GSK-3
|
Neurological Disease
|
|
7BIO (7-Bromoindirubin-3-Oxime) is the derivate of indirubin. 7BIO (7-Bromoindirubin-3-Oxime) has inhibitory effects against cyclin-dependent kinase-5 (CDK5) and glycogen synthase kinase-3β (GSK3β). 7BIO (7-Bromoindirubin-3-Oxime) inhibits Aβ oligomer-induced neuroinflammation, synaptic impairments, tau hyper-phosphorylation, activation of astrocytes and microglia, and attenuates Aβ oligomer-induced cognitive impairments in mice [1].
|
-
- HY-130437
-
|
|
MDM-2/p53
TGF-β Receptor
Caspase
|
Infection
Metabolic Disease
|
|
p-nitro-Pifithrin-α, a cell-permeable analog of pifithrin-α, is a potent p53 inhibitor. p-nitro-Pifithrin-α suppresses p53-mediated TGF-β1 expression in HK-2 cells. p-nitro-Pifithrin-α inhibits the activation of caspase-3 by Zika virus (ZIKV) strains. p-nitro-Pifithrin-α attenuates steatosis and liver injury in mice fed a high-fat diet [4].
non-alcoholic fatty liver disease .
|
-
- HY-19210
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
|
-
- HY-161261
-
|
|
AAK1
SARS-CoV
|
Infection
|
|
SARS-CoV-2-IN-81 (compound 12e) is a potent AAK1 inhibitor with an IC50 value of 9.38 nM. SARS-CoV-2-IN-81 shows anti-viral property against SARS-CoV-2. SARS-CoV-2-IN-81 attenuates AAK1-induced phosphorylation of AP2M1 threonine 156 and disrupts the direct interaction between AP2M1 and ACE2, ultimately inhibiting SARS-CoV-2 infection .
|
-
- HY-10071A
-
|
|
Organoid
ROCK
Apoptosis
|
Cancer
|
|
Y-27632 hydrochloride hydrate is an orally active, ATP-competitive inhibitor of ROCK-I and ROCK-II, with Kis of 220 and 300 nM, respectively. Y-27632 hydrochloride hydrate attenuates Doxorubicin-induced apoptosis of human cardiac stem cells. Y-27632 hydrochloride hydrate also suppresses dissociation-induced apoptosis of murine prostate stem/progenitor cells. Y-27632 hydrochloride hydrate primes human induced pluripotent stem cells (hIPSCs) to selectively differentiate towards mesendodermal lineage via epithelial-mesenchymal transition-like modulation .
|
-
- HY-N2118R
-
|
|
PPAR
PKA
Akt
p38 MAPK
ERK
|
Metabolic Disease
|
|
Bilobetin (Standard) is the analytical standard of Bilobetin. This product is intended for research and analytical applications. Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity .
|
-
- HY-121621
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
RO5101576 is a potent LTB4 receptor antagonist with activity to inhibit LTB4-induced calcium mobilization and chemotaxis of human neutrophils. RO5101576 significantly attenuated LTB4-induced pulmonary eosinophilia in guinea pigs. RO5101576 inhibited allergen- and ozone-induced pulmonary neutrophilia in nonhuman primates with efficacy comparable to that of budesonide. RO5101576 had no effect on LPS-induced neutrophilia in guinea pigs and cigarette smoke-induced neutrophilia in mice and rats. RO5101576 performed well in toxicology studies and was well tolerated .
|
-
- HY-B0075R
-
|
N-Acetyl-5-methoxytryptamine (standard); Melatonin
|
Melatonin Receptor
Autophagy
Mitophagy
Endogenous Metabolite
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Melatonin (Standard) is the analytical standard of Melatonin. This product is intended for research and analytical applications. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties . Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation . Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress .
|
-
- HY-N1584R
-
|
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (Standard) is the analytical standard of Halofuginone. This product is intended for research and analytical applications. Halofuginone (RU-19110), a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-N0469R
-
|
|
Endogenous Metabolite
Virus Protease
HSV
|
Infection
Metabolic Disease
Inflammation/Immunology
|
L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
|
-
- HY-70050
-
|
GR 68755 (Hydrochloride(1:X)); GR 68755X (Hydrochloride(1:X))
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Alosetron (GR 68755) Hydrochloride(1:X) is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron Hydrochloride(1:X) is used for the research of irritable bowel syndrome (IBS). Alosetron Hydrochloride(1:X) blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron Hydrochloride(1:X) attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-70050B
-
|
GR 68755 ((Z)-2-butenedioate); GR 68755X ((Z)-2-butenedioate)
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Alosetron (GR 68755) (Z)-2-butenedioate is a potent and highly selective serotonin 5-HT3 receptor antagonist. Alosetron (Z)-2-butenedioate is used for the research of irritable bowel syndrome (IBS). Alosetron (Z)-2-butenedioate blocks the fast 5HT3-mediated depolarisation of guinea-pig myenteric and submucosal neurons, with IC50 at ~55 nM. Alosetron (Z)-2-butenedioate attenuates the visceral nociceptive effect of rectal distension in conscious or anaesthetised dogs. Anti-inflammatory effects .
|
-
- HY-16915
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
RPR-260243, a potent activator of human ether-a-go-go-related gene (hERG), slows deactivation and attenuates inactivation of hERG1 channels. RPR260243-modified HERG currents are inhibited by Dofetilide (IC50=58 nM). RPR260243 displays no activator-like effects on other voltage-dependent ion channels, including the closely related ERG3 K+ channel . RPR-260243 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N0668
-
|
|
GLUT
Amylases
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase) .
|
-
- HY-N2360
-
|
|
E1/E2/E3 Enzyme
Apoptosis
MMP
ClpP
|
Infection
Inflammation/Immunology
Cancer
|
|
Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity .
|
-
- HY-101016
-
|
|
Cytochrome P450
Apoptosis
|
Cardiovascular Disease
|
|
17-ODYA is a CYP450 ω-hydroxylase inhibitor. 17-ODYA is also a potent inhibitor (IC50<100 nM) of the formation of 20-hydroxyeicosatetraenoic acid (20-HETE), epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids by rat renal cortical microsomes incubated with arachidonic acid. 17-ODYA completely attenuates the isoproterenol (ISO)-induced apoptosis, and necrosis in cultured cardiomyocytes . 17-ODYA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-136208
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a Ki of 0.47 nM and a Kb of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; Ki=36.56 nM and Kb=9.43 nM) and κ-opioid receptor (KOR; Ki=5.31 nM and Kb=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control .
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-
- HY-Y0121
-
|
|
Parasite
VEGFR
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Ethyl cinnamate, an orally active chemical constituent of the rhizome of Kaempferia galanga, exhibits anti-cancer, nematocidal, sedative and vasorelaxant activities. Ethyl cinnamate is a fragrance ingredient used as a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues. Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2 signal pathway in colorectal cancer. Ethyl cinnamate inhibits the tonic contractions induced by high K+ and phenylephrine (PE) with respective IC50 values of 0.30 mM and 0.38 mM in rat aorta .
|
-
- HY-100206
-
|
|
AMPK
|
Neurological Disease
|
|
5α-Androstane-3β,5,6β-triol is a neuroprotectant. 5α-Androstane-3β,5,6β-triol can remarkably reverse intracellular acidification and alleviate neuronal injury through the inhibition of AMPK signaling. 5α-Androstane-3β,5,6β-triol remarkably reduced the infarct volume and attenuated neurologic impairment in acute ischemic stroke models of middle cerebral artery occlusion in vivo .
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-
- HY-W016412
-
-
- HY-P99744
-
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TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
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-
- HY-155517
-
|
|
NOD-like Receptor (NLR)
Pyroptosis
|
Inflammation/Immunology
|
|
INF200 (compound 5) is a sulfonylurea-based inhibitor of NLRP3 and NLRP3-mediated pyroptosis. INF200 has beneficial cardiometabolic effects in rat model of high-fat diet (HFD)-induced metaflammation，and shows anti-inflammatory activity to (10 μM) decreases IL-1β release in human macrophages. INF200 improves glucose and lipid profiles，and attenuates systemic inflammation and biomarkers of cardiac dysfunction (particularly BNP). INF200 also improves myocardial damage-dependent ischemia/reperfusion injury (IRI) in hemodynamic evaluation .
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-
- HY-156104
-
|
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PROTACs
CaMK
|
Neurological Disease
|
|
CaMKIIα-PHOTAC is a photochemically targeted chimera (PHOTAC) targeting Ca2+/calmodulin-dependent protein kinase II α (CaMKIIα). Molecules such as PHOTAC can catalyze the ubiquitination and degradation of target proteins through the endogenous proteasome under specific wavelengths of light. CaMKIIα-PHOTAC reduces synaptic function under light conditions, and it attenuates the intensity of evoked field excitatory postsynaptic potentials in the mouse hippocampus in response to physiological stimuli. CaMKIIα-PHOTAC plays a critical role in maintaining long-term potentiation and memory capacity in subcellular dendritic domains .
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-
- HY-101193S
-
|
Zn(II)-protoporphyrin IX-d2,15N2; ZnPP-d2,15N2; Zinc Protoporphyrin-9-d2,15N2
|
Apoptosis
Endogenous Metabolite
Reactive Oxygen Species
Isotope-Labeled Compounds
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Zinc Protoporphyrin-d2, 15N2 is 15N and deuterated labeled Zinc Protoporphyrin (HY-101193). Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
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-
- HY-N1584BR
-
|
|
Calcium Channel
DNA/RNA Synthesis
Parasite
Sodium Channel
TGF-beta/Smad
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (hydrochloride) (Standard) is the analytical standard of Halofuginone (hydrochloride). This product is intended for research and analytical applications. Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM. Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity. Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects [4] .
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-
- HY-168086
-
|
|
PD-1/PD-L1
Histone Demethylase
|
Infection
Inflammation/Immunology
|
|
LSD1-IN-35 (Compound Z-1) is a selective LSD1 Inhibitor (IC50: 108 nM). LSD1-IN-35 inhibits the demethylation on H3K4me1/2. LSD1-IN-35 is an immunomodulator. LSD1-IN-35 promotes response of gastric cancer cells to T-cell killing effect by decreasing PD-L1 expression and further attenuates the PD-1/PD-L1 interaction .
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-
- HY-N0457R
-
|
|
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
|
|
Chicoric acid (Standard) is the analytical standard of Chicoric acid. This product is intended for research and analytical applications. Chicoric acid (Cichoric acid), an orally active dicaffeyltartaric acid, induces reactive oxygen species (ROS) generation. Chicoric acid inhibits cell viability and induces mitochondria-dependent apoptosis in 3T3-L1 preadipocytes through ROS-mediated PI3K/Akt and MAPK signaling pathways. Chicoric acid increases glucose uptake, improves insulin resistance, and attenuates glucosamine-induced inflammation. Chicoric acid has antidiabetic properties and antioxidant, anti-inflammatory effects .
|
-
- HY-171031
-
|
|
GSK-3
Apoptosis
Caspase
Bcl-2 Family
Reactive Oxygen Species
|
Neurological Disease
|
|
TFGF-18 is a GSK-3β inhibitor (IC50: 0.59 μM). TFGF-18 inhibits LPS-induced microglia activation and proinflammatory mediators release via inhibiting GSK-3β and downstream p65/NF-κB signaling. TFGF-18 inhibits neuronal apoptosis and oxidative stress, inhibits expressions of Bax, caspase3 and cleaved-caspase3 and increases the expression of Bcl-2. TFGF-18 has neuroprotection effect, inhibit neuroinflammation and attenuates cognitive impairment .
|
-
- HY-N0807
-
|
|
MMP
NF-κB
JAK
Keap1-Nrf2
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced rat liver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis .
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-
- HY-N0946
-
|
(-)-Pinoresinol 4-O-β-D-glucopyranoside
|
Glycosidase
|
Metabolic Disease
|
|
(-)-Pinoresinol 4-O-glucoside ((-)-Pinoresinol 4-O-β-D-glucopyranoside) is a potent and orally active α-glucosidase inhibitor with an IC50 value of 48.13 µM. (-)-Pinoresinol 4-O-glucoside increases cell migration and early differentiation of pre-osteoblasts. (-)-Pinoresinol 4-O-glucoside increases protein level of BMP2, p-Smad1/5/8, RUNX2. (-)-Pinoresinol 4-O-glucoside attenuates oxidative stress, hyperglycemia and hepatic toxicity. (-)-Pinoresinol 4-O-glucoside has the potential for the research of osteoporosis and periodontal disease .
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-
- HY-130311
-
|
2-Monolinolein; 2-Monolinoleoylglycerol
|
Cannabinoid Receptor
|
Neurological Disease
|
|
2-Linoleoyl glycerol (2-Monolinolein; 2-Monolinoleoylglycerol) is a monoacylglycerol that is an antagonist and partial agonist at the type 1 cannabinoid CB1 receptor. The potency of 2-Linoleoyl glycerol can be enhanced by JZL195 (HY-15250), an inhibitor of FAAH and MAGL, and inhibited by the CB1 antagonist AM251 (HY-15443) and Cannabidiol. As a CB1 antagonist, 2-Linoleoyl glycerol does not enhance, but only attenuates, the activity of the CB1/CB2 receptor ligands cannabinoids (AEA) and 2-arachidonoylglycerol (2-AG) .
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-
- HY-N1584AR
-
|
|
DNA/RNA Synthesis
TGF-beta/Smad
Parasite
Sodium Channel
Calcium Channel
|
Infection
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Halofuginone (hydrobromide) (Standard) is the analytical standard of Halofuginone (hydrobromide). This product is intended for research and analytical applications. Halofuginone (RU-19110) hydrobromid, a Febrifugine derivative, is a competitive prolyl-tRNA synthetase inhibitor with a Ki of 18.3 nM . Halofuginone hydrobromid is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity . Halofuginone hydrobromid is also a potent pulmonary vasodilator by activating Kv channels and blocking voltage-gated, receptor-operated and store-operated Ca 2+ channels. Halofuginone hydrobromid has anti-malaria, anti-inflammatory, anti-cancer, anti-fibrosis effects .
|
-
- HY-158688
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kδ-IN-21 (Compound 31) is a selective inhibitor for phosphoinositide 3-kinases δ (PI3Kδ), with an IC50 of 13.6 nM. PI3Kδ-IN-21 inhibits proliferation and differentation of T cells through PI3K/AKT/mTOR signaling pathway. PI3Kδ-IN-21 exhibits good pharmacokinetic characters in rat model, and attenuates the experimental autoimmune encephalomyelitis in myelin oligodendrocyte glycoprotein (MOG)-induced EAE model .
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-
- HY-D0958R
-
|
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Infection
Inflammation/Immunology
Cancer
|
|
Methylene blue (hydrate) (Standard) is the analytical standard of Methylene blue (hydrate). This product is intended for research and analytical applications. Methylene blue (Basic Blue 9) hydrate is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue hydrate through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue hydrate is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue hydrate is a Tau aggregation inhibitor. Methylene blue hydrate reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
-
- HY-N0755R
-
|
|
Insulin Receptor
GLUT
NF-κB
p38 MAPK
Autophagy
|
Metabolic Disease
Endocrinology
Cancer
|
|
Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines .
|
-
- HY-14536A
-
|
Basic Blue 9 (purity≥70%); CI-52015 (purity≥70%); Methylthioninium chloride (purity≥70%)
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Infection
Neurological Disease
Cancer
|
|
Methylene blue (purity≥70%) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue (purity≥70%) is a vasopressor and is often used as a dye in several medical procedures. Methylene blue (purity≥70%) through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue (purity≥70%) is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue (purity≥70%) is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
-
- HY-14536R
-
|
|
Guanylate Cyclase
Monoamine Oxidase
NO Synthase
Microtubule/Tubulin
|
Infection
Neurological Disease
Cancer
|
|
Methylene Blue (Standard) is the analytical standard of Methylene Blue. This product is intended for research and analytical applications. Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
-
- HY-149127
-
|
ASC-JM17; ALZ-003
|
Keap1-Nrf2
Androgen Receptor
HSP
Mitophagy
|
Metabolic Disease
|
|
Rosolutamide (ASC-JM17), a curcumin analog, is an orally active, potent Nrf1 and Nrf2 activator. Rosolutamide activates Nrf1, Nrf2 and heat shock factor 1 (Hsf1), thereby activating the expression of proteasome subunits, antioxidant enzymes and molecular chaperones. Rosolutamide degrades the polyglutamine (polyQ) androgen receptor (AR) via the ubiquitin-proteasome pathway and improves motor function in mouse models of spinal and bulbar muscular atrophy (SBMA). Rosolutamide improves mitochondrial function and promotes autophagy, decreases mutant protein aggregates, and attenuates intracellular/mitochondrial reactive oxygen species (ROS) levels .
|
-
- HY-N3584
-
|
Chonglou Saponin VII
|
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
Cancer
|
|
Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
|
-
- HY-N2037A
-
|
Norcoclaurine hydrochloride
|
MAP3K
MDM-2/p53
ROS Kinase
Apoptosis
|
Infection
Cardiovascular Disease
Endocrinology
Cancer
|
|
Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-124832
-
|
|
Caspase
Amyloid-β
|
Neurological Disease
|
|
δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
|
-
- HY-132225
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
SB 206553 is a 5-HT2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B) and 7.8 nM (5-HT2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .
|
-
- HY-N0668R
-
|
|
GLUT
Amylases
NF-κB
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Rubusoside (Standard) is the analytical standard of Rubusoside. This product is intended for research and analytical applications. Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase) .
|
-
- HY-Y0121R
-
|
|
Parasite
VEGFR
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Ethyl cinnamate (Standard) is the analytical standard of Ethyl cinnamate. This product is intended for research and analytical applications. Ethyl cinnamate, an orally active chemical constituent of the rhizome of Kaempferia galanga, exhibits anti-cancer, nematocidal, sedative and vasorelaxant activities. Ethyl cinnamate is a fragrance ingredient used as a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues. Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2 signal pathway in colorectal cancer. Ethyl cinnamate inhibits the tonic contractions induced by high K+ and phenylephrine (PE) with respective IC50 values of 0.30 mM and 0.38 mM in rat aorta .
|
-
- HY-N2037AR
-
|
|
MAP3K
MDM-2/p53
ROS Kinase
Apoptosis
|
Infection
Cardiovascular Disease
Endocrinology
Cancer
|
|
Higenamine (hydrochloride) (Standard) is the analytical standard of Higenamine (hydrochloride). This product is intended for research and analytical applications. Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-10450AR
-
|
|
SGLT
|
Metabolic Disease
Cancer
|
|
Dapagliflozin ((2S)-1,2-propanediol, hydrate) (Standard) is the analytical standard of Dapagliflozin ((2S)-1,2-propanediol, hydrate). This product is intended for research and analytical applications. Dapagliflozin ((2S)-1,2-propanediol, hydrate) is the S-enantiomer of Dapagliflozin 1,2-propanediol, hydrate. Dapagliflozin ((2S)-1,2-propanediol, hydrate), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin ((2S)-1,2-propanediol, hydrate) induces HIF1 expression and attenuates renal IR injury .
|
-
- HY-N2037AS1
-
|
Norcoclaurine-d4-1 hydrochloride; Demethyl-Coclaurine-d4-1 hydrochloride
|
Isotope-Labeled Compounds
MAP3K
MDM-2/p53
Apoptosis
ROS Kinase
|
Infection
Cardiovascular Disease
Endocrinology
Cancer
|
|
Higenamine-d4-1 (Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-N0847
-
|
|
NF-κB
PI3K
Akt
TGF-beta/Smad
|
Inflammation/Immunology
Cancer
|
|
Micheliolide is a sesquiterpene lactone with anti-cancer and anti-inflammatory effects, which is derived from Michelia compressa and Michelia champaca. Micheliolide can attenuate high glucose-stimulated NF-κB activation, IκBα degradation, and the expression of MCP-1, TGF-β1, and FN in mouse mesangial cells. Micheliolide inhibits LPS (HY-D1056)-induced activation of NF-κB and PI3K/Akt/p70S6K pathways to play an anti-inflammatory role. Micheliolide inhibits dextran sodium sulphate (DSS) (HY-116282)-induced inflammatory intestinal disease, colitis-associated cancer and rheumatic arthritis .
|
-
- HY-155297
-
|
FLA-136
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
|
-
- HY-B1588
-
|
|
Amyloid-β
HIV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties .
Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the treatment of chronic liver disease .
Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD .
Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .
Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form.
Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .
|
-
- HY-N3584R
-
|
|
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
Cancer
|
|
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
|
-
- HY-12882
-
|
RC 61-91; NP-120
|
iGluR
|
Neurological Disease
|
|
Ifenprodil (RC 61-91) is a noncompetitive NMDA receptor antagonist with anti-excitotoxic activity. Ifenprodil significantly improves long-term sensorimotor and spatial learning deficits in mice after acute subarachnoid hemorrhage. Ifenprodil reduces neuronal cell death in the basal cortex and CA1 region of the hippocampus induced by experimental subarachnoid hemorrhage. Ifenprodil attenuates Ca2+ overload in basal cortical cells and mitochondria, as well as brain edema in blood-brain barrier damage and early brain injury. Ifenprodil reduces the intracellular Ca2+ increase and apoptosis of primary cortical neurons under conditions of high glutamate concentrations. Ifenprodil also reduces the increase in endothelial permeability caused by high glutamate concentrations in human brain microvascular endothelial cells. Ifenprodil also inhibits GIRK channels and interacts with α1-adrenergic, 5-HT, and σ receptors .
|
-
- HY-B1588S
-
|
|
Amyloid-β
HIV
11β-HSD
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].
|
-
- HY-15026
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
ATB-429, a novel H2S-releasing derivative of mesalamine, demonstrates significant anti-nociceptive and anti-inflammatory effects in models of irritable bowel syndrome (IBS). By releasing hydrogen sulfide (H2S), ATB-429 modulates colorectal distension-induced hypersensitivity in both healthy and postcolitic rats. It attenuates abdominal withdrawal responses and suppresses spinal c-Fos mRNA expression, indicating its potential to alleviate pain associated with gastrointestinal inflammation. Moreover, ATB-429 down-regulates colonic cyclooxygenase-2 and interleukin-1β mRNA expression, effects not observed with mesalamine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, as evidenced by reversal of ATB-429's effects with glibenclamide. These findings suggest ATB-429 could offer therapeutic benefits for managing painful intestinal disorders linked to inflammation .
|
-
- HY-15616
-
|
|
Melanocortin Receptor
|
Cancer
|
|
BMS-470539 is a synthetic MC-1R agonist with potent anti-inflammatory properties. BMS-470539 selectively activates human and murine MC-1R with EC50 values ??of 16.8 nM and 11.6 nM, respectively. In vitro studies have shown that BMS-470539 is able to dose-dependently inhibit TNF-alpha-induced NF-kB activation in human melanoma cells expressing MC-1R. In vivo, subcutaneous injection of BMS-470539 into BALB/c mice effectively inhibited LPS-induced TNF-alpha production with an ED50 of approximately 10 μmol/kg and a pharmacodynamic half-life of approximately 8 hours. It also significantly reduced leukocyte infiltration in a lung inflammation model and attenuated paw swelling in a delayed-type hypersensitivity model, highlighting its efficacy as an anti-inflammatory agent through MC-1R modulation .
|
-
- HY-N2037
-
|
Norcoclaurine; Demethyl-Coclaurine
|
MAP3K
MDM-2/p53
Adrenergic Receptor
ROS Kinase
Apoptosis
|
Cardiovascular Disease
Endocrinology
|
|
Higenamine (Norcoclaurine), a β2-AR agonist with antioxidant capability, is a key component of the Chinese herb aconite root that prescribes for treating symptoms of heart failure in the oriental Asian countries. Higenamine is also a α1-adrenergic receptor antagonist with hypotensive effect. is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine protects myocyte Apoptosis and ischemia/reperfusion (I/R) injury through selective activation of beta2-adrenergic receptor (β2-AR). Higenamine also reduces I/R-induced myocardial infarction in mice. Higenamine can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-101480
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Xylamidine is a peripheral 5-HT receptor antagonist used to investigate possible peripheral appetite suppressant effects of 5-hydroxytryptophan (5-HTP) and fenfluramine. In a 1-hour food intake test, xylamidine attenuated the decrease in food intake induced by 5-HT and 5-HTP, but had no effect on fenfluramine, suggesting that the appetite suppressant effect of 5-HTP is mediated in part through peripheral 5-HT receptors. Microstructural analysis revealed that 5-HTP and fenfluramine induced a decrease in food intake rate and a reduction in feeding batch size. Xylamidine reversed the effects of 5-HTP on food intake rate and induced a slight increase in feeding batch size itself, thus, the peripheral effect of 5-HTP appears to be to slow food intake rate. No effect of xylamidine on fenfluramine-induced changes in feeding was observed. The results suggest that the appetite suppressant effects of 5-HTP and fenfluramine are differentiated based on the peripheral effects of 5-HTP. The peripheral effects of 5-HTP are distinct from the previously reported 5-HT-induced decreases in feeding batch size and duration. Possible mechanisms underlying the differences in peripheral effects of 5-HT and 5-HTP are discussed.
|
-
- HY-D0186R
-
|
|
Endogenous Metabolite
Thymidylate Synthase
|
Infection
|
2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
|
-
-
-
HY-L004
-
|
|
2,377 compounds
|
|
DNA is prone to numerous forms of damage that can injure cells and impair fitness. Cells have developed an array of mechanisms to repair these injuries. Proliferating cells are especially vulnerable to DNA damage due to the added demands of cellular growth and division. Cell cycle checkpoints represent integral components of DNA repair that coordinate cooperation between the machinery of the cell cycle and several biochemical pathways that respond to damage and restore DNA structure. By delaying progression through the cell cycle, checkpoints provide more time for repair before the critical phases of DNA replication, when the genome is replicated, and of mitosis, when the genome is segregated. Loss or attenuation of checkpoint function may increase spontaneous and induced gene mutations and chromosomal aberrations by reducing the efficiency of DNA repair.
MCE owns a unique collection of 2,377 cell cycle/DNA damage-related compounds which can be used in the research of the same.
|
| Cat. No. |
Product Name |
Type |
-
- HY-14536
-
|
Basic Blue 9; CI-52015; Methylthioninium chloride
|
Chromogenic Assays
|
|
Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
-
- HY-D0938
-
|
CFSE; 5(6)-Carboxyfluorescein diacetate succinimidyl ester; 5(6)-CFDA N-succinmidyl ester
|
Fluorescent Dyes/Probes
|
|
CFDA-SE is a fluorescent dye that can penetrate the cell membrane. It can react with the free amine group in the cytoskeleton protein inside the cell, and finally form a protein complex with fluorescence. After entering the cell, CFDA-SE locates in the cell membrane, cytoplasm and nucleus, and the fluorescence staining is strongest in the nucleus .
CFDA-SE dye can be uniformly inherited by the cells with cell division and proliferation, and its attenuation is proportional to the number of cell divisions. This phenomenon can be detected and analyzed by flow cytometry under the excitation light of 488 nm, and can be used to detect the proliferation of cells .
|
-
- HY-14536A
-
|
Basic Blue 9 (purity≥70%); CI-52015 (purity≥70%); Methylthioninium chloride (purity≥70%)
|
Chromogenic Assays
|
|
Methylene blue (purity≥70%) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue (purity≥70%) is a vasopressor and is often used as a dye in several medical procedures. Methylene blue (purity≥70%) through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue (purity≥70%) is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue (purity≥70%) is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
-
- HY-14536R
-
|
|
Chromogenic Assays
|
|
Methylene Blue (Standard) is the analytical standard of Methylene Blue. This product is intended for research and analytical applications. Methylene blue (Basic Blue 9) is a guanylyl cyclase (sGC), monoamine oxidase A (MAO-A) and NO synthase (NOS) inhibitor. Methylene blue is a vasopressor and is often used as a dye in several medical procedures. Methylene blue through the nitric oxide syntase/guanylate cyclase signalling pathway to reduce prepulse inhibition. Methylene blue is a REDOX cycling compound and able to cross the blood-brain barrier. Methylene blue is a Tau aggregation inhibitor. Methylene blue reduces cerebral edema, attenuated microglial activation and reduced neuroinflammation .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W016412
-
|
CoQ0
|
Enzyme Substrates
|
|
Coenzyme Q0 (CoQ0) is a potent, oral active ubiquinone compound can be derived from Antrodia cinnamomea. Coenzyme Q0 induces apoptosis and autophagy, suppresses of HER-2/AKT/mTOR signaling to potentiate the apoptosis and autophagy mechanisms. Coenzyme Q0 regulates NFκB/AP-1 activation and enhances Nrf2 stabilization in attenuation of inflammation and redox imbalance. Coenzyme Q0 has anti-angiogenic activity through downregulation of MMP-9/NF-κB and upregulation of HO-1 signaling .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3434A
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
|
Ac-FEID-CMK TFA is a potent zebrafish-specific GSDMEb-derived peptide inhibitor.
Ac-FEID-CMK TFA can attenuate the mortality and kidney injury during septic shock. Ac-FEID-CMK TFA inhibits pyroptosis and attenuates septic AKI (acute kidney injury) in vivo. Ac-FEID-CMK TFA can suppress the caspy2-mediated noncanonical inflammasome pathway .
|
-
- HY-P0237A
-
|
|
Kallikrein
|
Cancer
|
|
KKI-5 (TFA) is a specific inhibitor of tissue kallikrein. KKI-5 (TFA) can attenuate breast cancer cell invasion .
|
-
- HY-W014102
-
-
- HY-103290
-
|
|
Bradykinin Receptor
|
Others
|
|
R715 is a selective bradykinin B1 receptor antagonist. R715 significantly attenuates the hyperalgesic effect developed in Streptozotocin(HY-13753)-diabetic mice .
|
-
- HY-P1020
-
-
- HY-P1020A
-
-
- HY-P3434
-
|
|
Pyroptosis
|
Inflammation/Immunology
|
|
Ac-FEID-CMK is a potent zebrafish-specific GSDMEb-derived peptide inhibitor.
Ac-FEID-CMK can attenuate the mortality and kidney injury during septic shock. Ac-FEID-CMK inhibits pyroptosis and attenuates septic AKI (acute kidney injury) in vivo. Ac-FEID-CMK can suppress the caspy2-mediated noncanonical inflammasome pathway .
|
-
- HY-P0237
-
|
|
Kallikrein
|
Cancer
|
|
KKI-5 is a specific inhibitor of tissue kallikrein. KKI-5 can attenuate breast cancer cell invasion .
|
-
- HY-P10312
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
SPN009 (Sequence 3) is a GLP-1 Receptor agonist, with EC50 of 2.84 nM. SPN009 attenuates the type II diabetes in DB/DB mice models .
|
-
- HY-P2052
-
|
|
Peptides
|
Others
|
|
AWL 60 is a compound with SP antagonist and weak opioid agonist properties, which can antagonize SP-agonists in vitro and attenuate the decrease in blood pressure caused by SP-agonists in vivo.
|
-
- HY-P5888
-
|
Myr‐PKCɛ-
|
PKC
|
Inflammation/Immunology
|
|
PKCε inhibitor peptide,myristoylated (Myr‐PKC -) is a cell permeable myristic acid conjugated PKC peptide inhibitor that attenuates NO release in cultured human umbilical vein endothelial cells (HUVECs) .
|
-
- HY-P4201
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
|
-
- HY-118694
-
-
- HY-107627
-
|
|
Melanocortin Receptor
|
Inflammation/Immunology
|
|
MCL0020 is a potent and selective melanocortin MC4 receptor antagonist, with an IC50 of 11.63 nM. MCL0020 dose-dependently and significantly attenuates restraint stress-induced anorexia without affecting food intake .
|
-
- HY-P1010
-
|
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-P1010A
-
|
|
Caspase
Apoptosis
|
Neurological Disease
Cancer
|
|
Z-LEHD-FMK TFA is a selective and irreversible inhibitor of caspase-9, protects against lethal reperfusion injury and attenuates apoptosis. Z-LEHD-FMK TFA exhibits the neuroprotective effect in a rat model of spinal cord trauma .
|
-
- HY-P3785
-
|
|
PKA
|
Neurological Disease
|
|
PKI(5-22)amide is the active inhibitory fragment of the inhibitor of the cyclic AMP-dependent protein kinase (PKA). PKI(5-22)amide inhibits PKA activation, but fails to attenuate homologous desensitization of CRF1 receptors .
|
-
- HY-P10089
-
|
|
Peptides
|
Inflammation/Immunology
|
|
TREM-1 inhibitory peptide M3 is a ligand-dependent TREM-1 antagonist. TREM-1 inhibitory peptide M3 can inhibit systemic and pulmonary pro-inflammatory cytokine and chemokine production and attenuate acute lung injury .
|
-
- HY-P10148
-
|
Ac-[Leu28,31]-NPY (24-36)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .
|
-
- HY-W014102R
-
|
|
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
|
|
L-Alanyl-L-glutamine (Standard) is the analytical standard of L-Alanyl-L-glutamine. This product is intended for research and analytical applications. L-Alanyl-L-glutamine, a glutamine dipeptide, is benefit for the antioxidant system, attenuating inflammation, and may modulate the heat shock protein (HSP) response in catabolic situations .
|
-
- HY-P10498
-
|
|
Peptides
|
Neurological Disease
|
|
[Des-Tyr1]-gamma-Endorphin is a neuropeptide, which can be found in human cerebrospinal fluid. [Des-Tyr1]-gamma-Endorphin exhibits antidepressant efficacy, facilitates the extinction of active avoidance and attenuates the passive avoidance behavior in rats .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-P1401
-
|
|
PKC
|
Metabolic Disease
|
|
Protein Kinase C (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C (PKC), with an IC50 of 0.18 μM. Protein Kinase C (19-36) markedly attenuated vascular hyperproliferation and hypertrophy as well as glucose-induced suppression of natriuretic peptide receptor response .
|
-
- HY-W016733
-
|
H-D-Cit-OH
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
D-Citrulline (H-D-Cit-OH) is a stereoisomer of L-citrulline (HY-N0391). D-Citrulline significantly attenuates polymorphonuclear leukocyte (PMN)-induced cardiac contractile dysfunction in the isolated perfused rat heart subjected to ischemia/reperfusion via a non-NO-mediated mechanism .
|
-
- HY-P3112
-
|
|
Bombesin Receptor
|
Neurological Disease
|
|
ICI 216140 is a GRP/bombesin receptor 2 antagonist with the IC50 of 2 nM. ICI 216140 can reduce Bombesin (HY-P0195)-stimulated pancreatic amylase secretion and attenuates Bombesin (HY-P0195)-stimulated increases in blood pressure .
|
-
- HY-P5182
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
HsTX1, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1, an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM inhibits TEM cell activation and attenuates inflammation in autoimmunity .
|
-
- HY-P1098
-
Ac2-26
4 Publications Verification
|
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue .
|
-
- HY-P1098A
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
Ac2-26 TFA, an active N-terminal peptide of annexin A1 (AnxA1), attenuates ischemia-reperfusion-induced acute lung injury. Ac2-26 also decreases AnxA1 protein expression, inhibits the activation of NF-κB and MAPK pathways in the injured lung tissue .
|
-
- HY-P1428A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-P5182A
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
HsTX1 (TFA) toxin, from the scorpion Heterometrus spinnifer, is a 34-residue, C-terminally amidated peptide cross-linked by four disulfide bridges. HsTX1 (TFA) is an the inhibitor of potassium channel, with IC50 for Kv1.3 of 12 pM and inhibits TEM cell activation and attenuates inflammation in autoimmunity .
|
-
- HY-P2320
-
|
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
IDR-1 is an antimicrobial peptide that is active against Gram-positive and Gram-negative bacteria. IDR-1 counters infection by selective modulation of innate immunity without obvious toxicities. IDR-1 has anti-inflammatory and anti-infective properties, enhances the levels of monocyte chemokines, and attenuates pro-inflammatory cytokine release .
|
-
- HY-P5874
-
|
|
Calcium Channel
|
Inflammation/Immunology
|
|
Myr-TAT-CBD3 is CRMP2-CaV2.2 interaction inhibitor. Myr-tat-CBD3 can significantly attenuate carrageenan-induced thermal hypersensitivity and reverse thermal hypersensitivity induced in a rat model of postoperative pain. Myr-TAT-CBD3 can be used to study inflammation and postoperative pain .
|
-
- HY-W152604
-
|
Cyclo(leu-gly)
|
Dopamine Receptor
|
Neurological Disease
|
|
Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity. Cyclo(glycyl-L-leucyl) inhibits the development of Morphine induced pain relief as well as dopamine receptor supersensitivity in rats. Cyclo(glycyl-L-leucyl) has the potential for the prevention of tardive and/or L-DOPA (HY-N0304)-induced dyskinesias .
|
-
- HY-P1410
-
GsMTx4
Maximum Cited Publications
47 Publications Verification
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
GsMTx4 is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
|
-
- HY-P5389
-
|
|
Peptides
|
Others
|
|
Connexin mimetic peptide 40GAP27 is a biological active peptide. (This peptide corresponds to the GAP27 domain of the second extracellular loop of dominant vascular connexin (Cx40), designated as 40Gap 27. It was used to investigate mechanisms through which oxidant stress impairs communication via gap junctions. When administered, 40Gap27attenuates endothelium-dependent subintimal smooth muscle hyperpolarization.)
|
-
- HY-P1410A
-
GsMTx4 TFA
Maximum Cited Publications
47 Publications Verification
|
TRP Channel
Piezo Channel
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
GsMTx4 TFA is a spider venom peptide that selectively inhibits cationic-permeable mechanosensitive channels (MSCs) belonging to the Piezo and TRP channel families. GsMTx4 TFA also blocks cation-selective stretch-activated channels (SACs) , attenuates lysophosphatidylcholine (LPC)-induced astrocyte toxicity and microglial reactivity. GsMTx4 TFA is an important pharmacological tool for identifying the role of these excitatory MSCs in normal physiology and pathology .
|
-
- HY-P3960
-
|
|
Thyroid Hormone Receptor
Endogenous Metabolite
|
Neurological Disease
|
|
(Glu2)-TRH, a metabolically stable analogue of Thyrotropin-releasing hormone (TRH; HY-P0002), is a negative modulator for the cholinergic effect of TRH in the mouse brain. (Glu2)-TRH significantly attenuates TRH-induced hippocampal extracellular acetylcholine release. (Glu2)-TRH is not metabolized by thyroliberinase. (Glu2)-TRH manifests neuroprotective, antidepressant, anticonvulsant in the CNS .
|
-
- HY-P1698
-
|
AB-103
|
Bacterial
CD28
|
Infection
Inflammation/Immunology
Cancer
|
|
Reltecimod (AB-103) is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod can be used to research necrotizing soft-tissue infections (NSTIs) .
|
-
- HY-P1435
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-P1698B
-
|
AB-103 TFA
|
Bacterial
CD28
|
Infection
Inflammation/Immunology
Cancer
|
|
Reltecimod (AB-103) TFA is a T-cell-specific surface glycoprotein CD28 (TP44) antagonist. Reltecimod TFA has beneficial effects against different bacterial infections, their exotoxins and endotoxins, and ionizing radiation. Reltecimod TFA modulates the inflammatory response by targeting and attenuating the critical CD28/B7-2 co-stimulatory pathway, without inhibiting it. Reltecimod TFA can be used to research necrotizing soft-tissue infections (NSTIs) .
|
-
- HY-P1435A
-
|
|
NADPH Oxidase
|
Cardiovascular Disease
Cancer
|
|
NoxA1ds TFA is a potent and highly selective NADPH oxidase 1 (NOX1) inhibitor (IC50=20 nM). NoxA1ds TFA inhibits NOX1-derived O 2- production in HT-29 human colon cancer cells. NoxA1ds TFA attenuates VEGF-induced human pulmonary artery endothelial cell migration under hypoxic conditions in vitro. NoxA1ds TFA can be used in the study of hypertension, atherosclerosis and tumors .
|
-
- HY-P1723A
-
|
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
|
-
- HY-P10851
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
HVEM(14-39) is a B- and T-lymphocyte attenuator (BTLA) peptide inhibitor. HVEM (14-39) can be combined with BTLA with a KD of 0.102 μM. HVEM(14-39) enhances the activation and proliferation of T cells by regulating the expression of BTLA and HVEM in T cells, and promotes the transformation of cells into effector memory T cells. HVEM(14-39) inhibits tumor cell proliferation and promotes late apoptosis. HVEM(14-39) has immunomodulatory effects and can be used in the study of cancer .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99842A
-
|
|
TNF Receptor
|
Inflammation/Immunology
|
|
Dapirolizumab is a monoclonal antibodi against CD40 ligand. Dapirolizumab targets CD40L, blocks its interaction with CD40 receptors, and inhibits adaptive immune activation. Dapirolizumab attenuates systemic lupus erythematosus .
|
-
- HY-P99961
-
|
JS004
|
CD28
|
Cancer
|
|
Tifcemalimab (JS004) is a humanized anti-BTLA (B and T lymphocyte attenuation factor) monoclonal antibody. Tifcemalimab blocks the interaction of HVEM-BTLA by binding to BTLA, and thus blocks the inhibitory signaling pathway mediated by BTLA. Tifcemalimab can be used in research of cancer .
|
-
- HY-P99008
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Atibuclimab, is a chimeric monoclonal antibody directed against CD14 and is composed of murine variable and human IgG4 Fc regions. Atibuclimab can be used for the research of amyotrophic lateral sclerosis . Atibuclimab attenuates LPS-induced symptoms and strongly inhibits LPS-induced proinflammatory cytokine release, while only delaying the release of the anti-inflammatory cytokines soluble TNF receptor type I and IL-1 receptor antagonist .
|
-
- HY-P99165
-
|
|
IGF-1R
TSH Receptor
|
Endocrinology
|
|
Teprotumumab is an IGF-1 receptor (IGF-1R) blocking human monoclonal antibody. Teprotumumab binds to the ligand binding extracellular α-subunit domain of IGF-1R. Teprotumumab inhibits TSH and IGF-1 action in fibrocytes. Teprotumumab attenuates TSH-dependent IL-6 and IL-8 expression and Akt phosphorylation. Teprotumumab can be used for thyroid-associated ophthalmopathy research .
|
-
- HY-P99744
-
|
TAK-573
|
CD38
|
Inflammation/Immunology
Cancer
|
|
Modakafusp alfa (TAK-573) is a humanized, anti-CD38 IgG4 monoclonal antibody fused to 2 attenuated IFNα2b molecules, which delivers interferon-alpha to CD38-expressing cells. Modakafusp alfa has direct anti-proliferative activity on multiple myeloma (MM) cancer cells in vitro and induces robust and durable antitumor responses in MM xenograft tumor models. Modakafusp alfa in combination with anti-PD-1 antibodies induces immunomodulation and antitumor responses with good tolerance in mice .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
- HY-B0661R
-
-
- HY-N0595R
-
-
- HY-N5025
-
-
- HY-N6869
-
-
- HY-N7363
-
-
- HY-N4042
-
-
- HY-113314
-
-
- HY-N8472
-
-
- HY-101415
-
-
- HY-Z0283
-
-
- HY-126415
-
-
- HY-107818
-
-
- HY-N0148A
-
-
- HY-N10587
-
-
- HY-N6967
-
|
(-)-α-Bisabolol
|
Structural Classification
other families
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Apoptosis
|
|
Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-N0107
-
-
- HY-N11648
-
|
|
Triterpenes
Structural Classification
Microorganisms
Terpenoids
Source classification
|
Apoptosis
Caspase
|
|
Ganoderic acid T1 is a deacetylated derivative of Ganoderic acid T. Ganoderic acid T1 attenuates antioxidant defense system and induces apoptosis of cancer cells. Ganoderic acid T1 decreases mitochondrial membrane potential and activates caspase-9 and caspase-3, to trigger apoptosis. Ganoderic acid T1 also increases the generation of intracellular ROS to produce pro-oxidant activities and cytotoxicity .
|
-
- HY-N0293R
-
|
|
Structural Classification
Other Monoterpenes
Paeonia lactiflora Pall.
Terpenoids
Source classification
Plants
Paeoniaceae
|
HSP
|
|
Paeoniflorin (Standard) is the analytical standard of Paeoniflorin. This product is intended for research and analytical applications. Paeoniflorin is a heat shock protein-inducing compound and commonly exists in the plants of Paeoniaceae family, with various biological activities, including anticancer activity, anti-inflammatory activity, enhancing cognition and attenuating learning impairment, anti-oxidative stress, antiplatelet aggregation, expansion of blood vessels, and reducing blood viscosity .
|
-
- HY-N2638R
-
-
- HY-N0496R
-
-
- HY-N0774
-
-
- HY-120657
-
-
- HY-B0011R
-
-
- HY-121152
-
-
- HY-B1331
-
|
Cyromazin; CGA-72662
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Parasite
|
|
Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
|
-
- HY-B1671
-
-
- HY-N6869R
-
|
|
Structural Classification
Microorganisms
other families
Terpenoids
Source classification
Diterpenoids
Plants
|
Antibiotic
PPAR
Bacterial
Fungal
|
|
Dehydroabietic acid (Standard) is the analytical standard of Dehydroabietic acid. This product is intended for research and analytical applications. Dehydroabietic acid is a diterpene resin acid that can be isolated from Pinus and Picea. Dehydroabietic acid has anti-bacterial, anti-fungal, anti-inflammatory, and anticancer activities. Dehydroabietic acid is a dual PPAR-α/γ agonist and PPAR-γ partial agonist, which can attenuate insulin resistance (IR) and hepatic steatosis induced by HFD-consumption in mice .
|
-
- HY-N0148
-
-
- HY-P3960
-
-
- HY-B1328R
-
-
- HY-Z0283R
-
-
- HY-B0075
-
-
- HY-101193
-
-
- HY-101415R
-
-
- HY-N6967R
-
|
|
Structural Classification
other families
Terpenoids
Sesquiterpenes
Source classification
Plants
|
Apoptosis
|
|
Levomenol (Standard) is the analytical standard of Levomenol. This product is intended for research and analytical applications. Levomenol ((-)-α-Bisabolol), a monocyclic sesquiterpene alcohol, exerts antioxidant, anti-inflammatory, and anti-apoptotic activities. Levomenol also has neuroprotective effects and prevents neuronal damage and memory deficits through reduction of proinflammatory markers induced by permanent focal cerebral ischemia in mice. Levomenol attenuates nociceptive behaviour and central sensitisation in a rodent model of trigeminal neuropathic pain. Orally active .
|
-
- HY-N1584
-
-
- HY-W012974
-
-
- HY-59291
-
-
- HY-N2118
-
-
- HY-N10330
-
|
|
Structural Classification
Animals
Source classification
Phenols
|
HIF/HIF Prolyl-Hydroxylase
VEGFR
|
|
7-Hydroxyneolamellarin A is a natural product that could be derived from sponge Dendrilla nigra. 7-Hydroxyneolamellarin A is a potent hypoxia-inducible factor-1α (HIF-1α) inhibitor. 7-Hydroxyneolamellarin A attenuates the accumulation of hypoxia-inducible factor-1α (HIF-1α) protein and inhibits vascular epidermal growth factor (VEGF) transcriptional activity. 7-Hydroxyneolamellarin A can be used in research of cancer .
|
-
- HY-145491
-
|
|
Structural Classification
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
ERK
NF-κB
|
|
Resolvin D5 is a prolytic mediator (SPM) with anti-inflammatory activity derived from oxidized lipids DHA. Resolvin D5 inhibits Th17 cell differentiation and promotes regulatory T cell differentiation, and inhibits CD4+ T cell proliferation. Resolvin D5 attenuates osteoclast differentiation and interferes with osteoclastogenesis. Resolvin D5 also regulates ERK phosphorylation and nuclear translocation of NF-kappaB. Resolvin D5 could be used in rheumatoid arthritis research .
|
-
- HY-B1671R
-
-
- HY-B1331R
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Parasite
|
|
Cyromazine (Standard) is the analytical standard of Cyromazine. This product is intended for research and analytical applications. Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
|
-
- HY-N0774R
-
-
- HY-N0107R
-
|
|
Structural Classification
Alkaloids
Buxaceae
Other Alkaloids
Plants
Buxus microphylla S.et Z.var. Sinica Rehd.et Wils.
|
Apoptosis
Autophagy
mTOR
Akt
|
|
Cyclovirobuxine D (Standard) is the analytical standard of Cyclovirobuxine D. This product is intended for research and analytical applications. Cyclovirobuxine D (CVB-D) is the main active component of the traditional Chinese medicine Buxus microphylla. Cyclovirobuxine D induces autophagy and attenuates the phosphorylation of Akt and mTOR . Cyclovirobuxine D inhibits cell proliferation of gastric cancer cells through suppression of cell cycle progression and inducement of mitochondria-mediated apoptosis . Cyclovirobuxine D is beneficial for heart failure induced by myocardial infarction .
|
-
- HY-N6871
-
|
|
Infection
Structural Classification
Colophony
Classification of Application Fields
Pinaceae
Ketones, Aldehydes, Acids
Metabolic Disease
Plants
Inflammation/Immunology
Disease Research Fields
|
Bacterial
IKK
Ferroptosis
|
Abietic acid, an orally active diterpene isolated from Colophony, displays significant anti-proliferative, anti-inflammatory, anti-obesity effect, bacteriostatic, cell cycle arresting and pro-apoptotic activities. Abietic acid inhibits lipoxygenase activity for allergy. Abietic acid enhances cell migration and tube formation in HUVECs. Abietic acid induces significant angiogenic potential, which is associated with upregulation of extracellular signal-regulated kinase (ERK) and p38 expression. Abietic acid attenuates sepsis-induced lung injury by inhibiting nuclear factor kappa-light-chain-enhancer of activated B cells (NF-κB) pathway to inhibit M1 macrophage polarization. Abietic acid exhibits a positive effect against liver injury by attenuating inflammation and ferroptosis. Abietic acid shows accelerated wound closure in a mouse model of cutaneous wounds. Abietic acid significantly reduces the proliferation and growth of NSCLC cells by IKKβ inhibition.Additionally, Abietic acid ameliorates psoriasis-like inflammation and modulates gut microbiota in mice. Abietic acid is promising for research in non-small-cell lung cancer (NSCLC), liver injury-related deseases and psoriasis .
|
-
- HY-N0457
-
-
- HY-N1584A
-
-
- HY-106353
-
-
- HY-113402A
-
-
- HY-N0148R
-
-
- HY-N0755
-
-
- HY-N2118R
-
|
|
Structural Classification
Flavonoids
Ginkgoaceae
Source classification
Phenols
Polyphenols
Plants
Biflavones
Ginkgo biloba
|
PPAR
PKA
Akt
p38 MAPK
ERK
|
|
Bilobetin (Standard) is the analytical standard of Bilobetin. This product is intended for research and analytical applications. Bilobetin, an active component of Ginkgo biloba, can reduce blood lipids and improve the effects of insulin. Bilobetin ameliorated insulin resistance, increased the hepatic uptake and oxidation of lipids, reduced very-low-density lipoprotein triglyceride secretion and blood triglyceride levels, enhanced the expression and activity of enzymes involved in β-oxidation and attenuated the accumulation of triglycerides and their metabolites in tissues. Bilobetin also increased the phosphorylation, nuclear translocation and activity of PPARα accompanied by elevated cAMP level and PKA activity .
|
-
- HY-B0075R
-
-
- HY-N1584R
-
-
- HY-N0469R
-
|
|
Structural Classification
Microorganisms
Source classification
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
|
Endogenous Metabolite
Virus Protease
HSV
|
L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
|
-
- HY-N0668
-
-
- HY-N2360
-
-
- HY-Y0121
-
-
- HY-N0457R
-
|
|
Structural Classification
other families
Source classification
Other Phenylpropanoids
Phenols
Polyphenols
Phenylpropanoids
Plants
|
Reactive Oxygen Species
Apoptosis
|
|
Chicoric acid (Standard) is the analytical standard of Chicoric acid. This product is intended for research and analytical applications. Chicoric acid (Cichoric acid), an orally active dicaffeyltartaric acid, induces reactive oxygen species (ROS) generation. Chicoric acid inhibits cell viability and induces mitochondria-dependent apoptosis in 3T3-L1 preadipocytes through ROS-mediated PI3K/Akt and MAPK signaling pathways. Chicoric acid increases glucose uptake, improves insulin resistance, and attenuates glucosamine-induced inflammation. Chicoric acid has antidiabetic properties and antioxidant, anti-inflammatory effects .
|
-
- HY-N0807
-
-
- HY-N0946
-
|
(-)-Pinoresinol 4-O-β-D-glucopyranoside
|
Structural Classification
Artemisia selengensis Turcz. ex Bess.
Source classification
Plants
Compositae
Saccharides
Monosaccharides
|
Glycosidase
|
|
(-)-Pinoresinol 4-O-glucoside ((-)-Pinoresinol 4-O-β-D-glucopyranoside) is a potent and orally active α-glucosidase inhibitor with an IC50 value of 48.13 µM. (-)-Pinoresinol 4-O-glucoside increases cell migration and early differentiation of pre-osteoblasts. (-)-Pinoresinol 4-O-glucoside increases protein level of BMP2, p-Smad1/5/8, RUNX2. (-)-Pinoresinol 4-O-glucoside attenuates oxidative stress, hyperglycemia and hepatic toxicity. (-)-Pinoresinol 4-O-glucoside has the potential for the research of osteoporosis and periodontal disease .
|
-
- HY-N1584AR
-
-
- HY-N0755R
-
|
|
Structural Classification
Rhus succedanea
Flavonoids
Flavones
Plants
Anacardiaceae
|
Insulin Receptor
GLUT
NF-κB
p38 MAPK
Autophagy
|
|
Rhoifolin (Standard) is the analytical standard of Rhoifolin. This product is intended for research and analytical applications. Rhoifolin is a flavone glycoside can be isolated from Rhus succedanea. Rhoifolin has anti-diabetic effect acting through enhanced adiponectin secretion, tyrosine phosphorylation of insulin receptor-β and glucose transporter 4 (GLUT 4) translocation. Rhoifolin has an anti-inflammatory action via multi-level regulation of inflammatory mediators. Rhoifolin ameliorates titanium particle-stimulated osteolysis and attenuates osteoclastogenesis via RANKL-induced NF-κB and MAPK pathways. Rhoifolin also has cytotoxic activity against different cancer cell lines .
|
-
- HY-N3584
-
-
- HY-N2037A
-
-
- HY-N0668R
-
|
|
Structural Classification
other families
Terpenoids
Source classification
Diterpenoids
Plants
|
GLUT
Amylases
NF-κB
|
|
Rubusoside (Standard) is the analytical standard of Rubusoside. This product is intended for research and analytical applications. Rubusoside is a diterpene glycoside that is also a sweetener and solubilizer with anti-angiogenic, anti-cancer, anti-obesity, anti-allergic and anti-asthmatic effects. Rubusoside attenuates airway hyperresponsiveness and reduces inflammatory cells in bronchoalveolar lavage fluid (BALF), reducing OVA (HY-W250978)-induced airway inflammation. Rubusoside also prevents palmitic acid-induced lipotoxicity in pancreatic INS-1 cells, reduces the transport of human glucose transporters GLUT-1 and fructose GLUT-5, and inhibits NF-κB and α-amylase (α-amylase) .
|
-
- HY-Y0121R
-
|
|
Structural Classification
Kaempferia galanga L.
Microorganisms
Source classification
Other Phenylpropanoids
Phenylpropanoids
Plants
Zingiberaceae
|
Parasite
VEGFR
Apoptosis
|
|
Ethyl cinnamate (Standard) is the analytical standard of Ethyl cinnamate. This product is intended for research and analytical applications. Ethyl cinnamate, an orally active chemical constituent of the rhizome of Kaempferia galanga, exhibits anti-cancer, nematocidal, sedative and vasorelaxant activities. Ethyl cinnamate is a fragrance ingredient used as a food flavor and additive for cosmetic products. Ethyl cinnamate is also an excellent clearing reagent for mammalian tissues. Ethyl cinnamate suppresses tumor growth through anti-angiogenesis by attenuating VEGFR2 signal pathway in colorectal cancer. Ethyl cinnamate inhibits the tonic contractions induced by high K+ and phenylephrine (PE) with respective IC50 values of 0.30 mM and 0.38 mM in rat aorta .
|
-
- HY-N2037AR
-
|
|
Alkaloids
Structural Classification
Source classification
Phenols
Polyphenols
Plants
Lauraceae
Isoquinoline Alkaloids
Lindera aggregata (Sims) Kosterm.
|
MAP3K
MDM-2/p53
ROS Kinase
Apoptosis
|
|
Higenamine (hydrochloride) (Standard) is the analytical standard of Higenamine (hydrochloride). This product is intended for research and analytical applications. Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
|
-
- HY-N0847
-
-
- HY-N3584R
-
|
|
Structural Classification
Liliaceae
Source classification
Trillium tschonoskii Maxim.
Plants
Steroids
|
Akt
p38 MAPK
P-glycoprotein
Bcl-2 Family
Caspase
PARP
Autophagy
Apoptosis
|
|
Paris saponin VII (Standard) is the analytical standard of Paris saponin VII. This product is intended for research and analytical applications. Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia .
|
-
- HY-N2037
-
-
- HY-D0186R
-
|
|
Structural Classification
Natural Products
Immune System Disorder
Microorganisms
Source classification
Disease markers
Endogenous metabolite
|
Endogenous Metabolite
Thymidylate Synthase
|
2'-Deoxyuridine (Standard) is the analytical standard of 2'-Deoxyuridine. This product is intended for research and analytical applications. 2’-deoxyuridine is a brain-penetrant pyrimidines nucleotide that is associated with nervous system diseases. 2'-Deoxyuridine could increase chromosome breakage and results in a decreased thymidylate synthetase activity. 2'-Deoxyuridine is a precursor in the synthesis of Edoxudine (HY-B1011) and also an analogue of 5-ethynyl-2'-deoxyuridine, EdU (HY-118411). 2’-deoxyuridine reduces microglial activation and improve oxidative stress damage by modulating glycolytic metabolism on the Aβ25-35-induced brain injury, which is promising for research of Alzheimer’s disease (AD) .
In Vitro:The interaction between the 2-deoxyuridine and the column increases the duration of retention of 2-deoxyuridine .
Gradient elution with sodium acetate buffer-ACN eluent on two ZIC-HILIC homemade columns separates 2-deoxyuridine in under 9 min .
In Vivo:2'-Deoxyuridine (34.42 ng/mL, gavage, 15 min) passes the blood-brain barrier (BBB) to enter the hippocampus of mice brain .
2'-Deoxyuridine (20 mg/kg, gavage, daily for 4 weeks) improves cognition and memory loss and attenuates the damage to the hippocampus in Aβ25-35-induced mice model .
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-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-B0673S
-
|
|
|
Pirfenidone-d5 is a deuterium labeled Pirfenidone. Pirfenidone is an antifibrotic agent that attenuates CCL2 and CCL12 production in fibrocyte cells. Pirfenidone has growth-inhibitory effect and reduces TGF-β2 protein levels in human glioma cell lines. Pirfenidone also has anti-inflammatory activities[1][2][3].
|
-
-
- HY-144026S
-
|
|
|
9-PAHSA-d9 is the deuterium labeled 9-PAHSA (HY-120657). 9-PAHSA, an endogenous fatty acid, reduces blood glucose levels and attenuates inflammation .
|
-
-
- HY-B0661AS
-
|
|
|
Tamsulosin-d5 (hydrochloride) is the deuterium labeled Tamsulosin hydrochloride. Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
|
-
-
- HY-B0661AS1
-
|
|
|
Tamsulosin-d4 (hydrochloride) is deuterium labeled Tamsulosin (hydrochloride). Tamsulosin hydrochloride ((R)-(-)-YM12617) is an inhibitor of α1-adrenergic receptor. Tamsulosin hydrochloride is used for the research of prostatic hyperplasia. Tamsulosin hydrochloride attenuates abdominal aortic aneurysm growth in animal models[1].
|
-
-
- HY-W654098
-
|
|
|
Cefazolin- 13C2, 15N (sodium) is 13C and 15N labeled Cefazolin (sodium). Cefazolin sodium is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin sodium has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD).
|
-
-
- HY-B1892S1
-
|
|
|
Cefazolin- 13C2, 15N (Cephazolin- 13C2, 15N) is 13C and 15N labeled Cefazolin. Cefazolin (Cephazolin) is a first-generation cephalosporin antibiotic and can be used in varieties of bacterial infections research . Cefazolin has anti-inflammatory effect and can attenuate post-operative cognitive dysfunction (POCD) .
|
-
-
- HY-10450S5
-
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|
Dapagliflozin- 13C6-1 is 13C labeled Dapagliflozin. Dapagliflozin (BMS-512148), a new type of agent used to treat diabetes mellitus (DM), is a competitive sodium/glucose cotransporter 2 (SGLT2) inhibitor, which results in excretion of glucose into the urine . Dapagliflozin induces HIF1 expression and attenuates renal IR injury .
|
-
-
- HY-B0661S
-
|
|
|
Tamsulosin-d4 ((R)-(-)-YM12617 (free base)-d4) is deuterium labeled Tamsulosin. Tamsulosin ((R)-(-)-YM12617 free base) is an inhibitor of α1-adrenergic receptor. Tamsulosin is used for the research of prostatic hyperplasia. Tamsulosin attenuates abdominal aortic aneurysm growth in animal models .
|
-
-
- HY-B0011S
-
|
|
|
Docetaxel-d9 is the deuterium labeled Docetaxel. Docetaxel (RP-56976) is a microtubule depolymerization inhibitor, with an IC50 of 0.2 μM. Docetaxel attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel arrests the cell cycle at G2/M and leads to cell apoptosis. Docetaxel has anti-cancer activity[1][3].
|
-
-
- HY-121246S
-
|
|
|
Fluorofenidone-d3 is deuterium labeled Fluorofenidone. Fluorofenidone (AKF-PD), an analogue of AMR69, shows equivalent antifibrotic activity, lower toxicity and longer half-life. Fluorofenidone (AKF-PD) attenuates the progression of renal interstitial fibrosis partly by suppressing NADPH oxidase and extracellular matrix (ECM) deposition via the PI3K/Akt signalling pathway[1][2].
|
-
-
- HY-A0143S
-
|
|
|
Dihomo-γ-linolenic acid-d6 (DGLA-d6) is the deuterium labeled Dihomo-γ-linolenic acid. Dihomo-γ-linolenic acid (all-cis-8,11,14-Eicosatrienoic acid) is a 20-carbon ω-6 fatty acid, with anti-inflammatory and anti-proliferative activities. Dihomo-γ-linolenic acid attenuates atherosclerosis in the apolipoprotein E deficient mouse model system[1][2][3].
|
-
-
- HY-B0011AS
-
|
|
|
Docetaxel-d5 (trihydrate) is the deuterium labeled Docetaxel (Trihydrate). Docetaxel Trihydrate (RP-56976 Trihydrate) is an antineoplastic agent and inhibits microtubule depolymerization with an IC50 value of 0.2 μM[1]. Docetaxel Trihydrate is a semisynthetic analog of taxol and attenuates the effects of bcl-2 and bcl-xL gene expression. Docetaxel Trihydrate arrests the cell cycle at G2/M and leads to cell apoptosis[1][3].
|
-
-
- HY-B1118S2
-
|
|
|
Secnidazole-d4 is the deuterium labeled Secnidazole[1]. Secnidazole (RP-14539) is an orally active azole antibiotic and a imidazole mitigator of Serratia marcescens virulence. Secnidazole, as an analog of acylhomoserine lactones, effectively inhibits QS resulting in the attenuation of Pseudomonas aeruginosa pathogenesis. Secnidazole has antimicrobial activity against many anaerobic Gram-negative and Gram-positive bacterial species in vitro. Secnidazole can be used for the research of various diseases, such as amoebiasis and giardiasis, and bacterial vaginitis[1][2][3].
|
-
-
- HY-12678S
-
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|
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
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-
- HY-B0075S2
-
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Melatonin-d7 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress[5].
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-
- HY-B0075S1
-
|
|
|
Melatonin-d3 is the deuterium labeled Melatonin. Melatonin is a hormone made by the pineal gland that can activates melatonin receptor. Melatonin plays a role in sleep and possesses important antioxidative and anti-inflammatory properties[1][2][3]. Melatonin is a novel selective ATF-6 inhibitor and induces human hepatoma cell apoptosis through COX-2 downregulation[4]. Melatonin attenuates palmitic acid-induced (HY-N0830) mouse granulosa cells apoptosis via endoplasmic reticulum stress[5].
|
-
-
- HY-101193S
-
|
|
|
Zinc Protoporphyrin-d2, 15N2 is 15N and deuterated labeled Zinc Protoporphyrin (HY-101193). Zinc Protoporphyrin (Zn(II)-protoporphyrin IX) is an orally active and competitive heme oxygenase-1 (HO-1) inhibitor and markedly attenuates the protective effects of Phloroglucinol (PG) against H2O2 . Zinc Protoporphyrin is used as a screening marker of iron deficiency in individual pregnant women and children, but also to assess population iron status in combination with haemoglobin concentration . Zinc Protoporphyrin has anti-cancer activity .
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-
-
- HY-N2037AS1
-
|
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Higenamine-d4-1 (Norcoclaurine-d4-1) hydrochloride is deuterium labeled Higenamine (hydrochloride). Higenamine hydrochloride is a selective LSD1 inhibitor (IC50=1.47 μM) that can be isolated from aconite. Higenamine hydrochloride has anti-inflammatory and antibacterial activity. Higenamine (Norcoclaurine) can attenuate IL-1β-induced Apoptosis through ROS-mediated PI3K/Akt signaling pathway. Higenamine hydrochloride protects brain cells from oxygen deprivation. Higenamine can promote bone formation in osteoporosis through the SMAD2/3 pathway. Higenamine hydrochloride can be used to study cancer, inflammation, cardiorenal syndrome and other diseases .
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- HY-B1588S
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Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].
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- HY-101016
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Alkynes
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17-ODYA is a CYP450 ω-hydroxylase inhibitor. 17-ODYA is also a potent inhibitor (IC50<100 nM) of the formation of 20-hydroxyeicosatetraenoic acid (20-HETE), epoxyeicosatrienoic acids and dihydroxyeicosatrienoic acids by rat renal cortical microsomes incubated with arachidonic acid. 17-ODYA completely attenuates the isoproterenol (ISO)-induced apoptosis, and necrosis in cultured cardiomyocytes . 17-ODYA is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-145721A
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GED-0301 sodium
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Antisense Oligonucleotides
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Mongersen sodium is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen sodium restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen sodium can attenuate Crohn's disease-like experimental colitis in mice .
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- HY-145721
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GED-0301
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Antisense Oligonucleotides
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Mongersen (GED-0301) is a specific and orally active SMAD7 antisense oligonucleotide. Mongersen restores TGF-β1 activity leading to inhibition of inflammatory signals. Mongersen can attenuate Crohn's disease-like experimental colitis in mice .
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