Search Result
Results for "
AS model mice
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
6
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-125850
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- HY-162683
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CDK
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Neurological Disease
Cancer
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(S)-PHA533533 is a cyclin-dependent kinase 2 (CDK2) inhibitor. (S)-PHA533533 shows anti-tumor activity and can induce widespread neuronal UBE3A expression in angelman syndrome model mice .
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- HY-111792
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CRX-601
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Toll-like Receptor (TLR)
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Inflammation/Immunology
Cancer
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GSK1795091 (CRX-601), an immunologic stimulator, is a synthetic TLR4 agonist. Antitumor activity. GSK1795091 can be used as a vaccine adjuvant to enhance both mucosal and systemic immunity to influenza virus vaccines. Not only, GSK1795091 inhibits tumor growth and increases the survival in mice model, but results in long term survival in influenza challenge model in mice .
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- HY-N1149
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(-)-Tilifodiolide
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Others
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Others
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Tilifodiolide ((-)-Tilifodiolide) is a lactone, which can be isolated from the roots of Salvia tiliaefolia. Tilifodiolide has anti-inflammatory activity in mice model .
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- HY-163346
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Others
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Metabolic Disease
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TPEG-P is an enzyme-activated intramolecular hydrogen bond (IMHB) enhanced probe, developed for ALP detection in cells and mice models of DILI .
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- HY-106471
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Propyldazine
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Others
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Cardiovascular Disease
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Pildralazine (Propyldazine) is a hydralazinelike antihypertensive vasodilator containing a free hydrazine group. Pildralazine is orally active, has no significant carcinogenicity in mice model .
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- HY-125850R
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Drug Metabolite
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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 .
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- HY-126426
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DNA Methyltransferase
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Cardiovascular Disease
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CBHcy is an inhibitor for betaine-homocysteine S-methyltransferase (BGMT), with an IC50 of 0.09 μM. CBHcy upregulates the plasma total homocysteine and causes transient hyperhomocysteinemia in mice model .
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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-161926
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PPAR
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Metabolic Disease
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YGT-31 is a modulator for PPARγ with an IC50 of 1.72 μM, and a Ki of 0.62 μM. YGT-31 reduces blood glucose levels and improves insulin resistance in db/db mice type 2 diabetes models, through inhibition of CDK5-mediated PPARγ-Ser273 phosphorylation. YGT-31 exhibits anti-hepatic steatosis effect in mice non-alcoholic fatty liver disease (NAFLD) model .
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- HY-113354S
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Endogenous Metabolite
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Neurological Disease
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Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1][2].
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- HY-122604
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Others
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Neurological Disease
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PF-DcpSi is a mRNA decapping scavenger enzyme (DcpS) inhibitor (IC50: 0.11 nM). PF-DcpSi (30 mg/kg,i.p.) ameliorates the disease phenotype in a mice model of spinal muscular atrophy (SMA) .
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- HY-121365
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Others
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Infection
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Forphenicinol is an immunomodulator and a derivative of the bacterial metabolite forphenicine. It increases the phagocytosis of yeast by peritoneal macrophages isolated from thioglycolate-stimulated mice. Forphenicinol (100 μg/animal) prevents cyclophosphamide-induced suppression of delayed-type hypersensitivity (DTH), as well as enhances DTH in response to the hapten oxazolone or sheep red blood cells in mice. It enhances the bactericidal activity of macrophages against P. aeruginosa in mice when administered at a dose of 0.5 mg/kg.2 Forphenicinol (15.6-1,000 μg/animal) increases survival in a mouse model of P. aeruginosa infection. It also inhibits tumor growth in S180 sarcoma and IMC carcinoma mouse xenograft models when administered at doses ranging from 0.05 to 5 mg/kg per day.
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- HY-101194
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Tin-protoporphyrin IX; Sn-Protoporphyrin; SnPPIX
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Reactive Oxygen Species
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Cancer
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Tin protoporphyrin IX dichloride (SnPPIX) is a potent Heme oxygenase-1 (HO-1) inhibitor. Tin protoporphyrin IX dichloride sensitizes pancreatic ductal adenocarcinoma (PDAC) tumors to chemotherapy in mice model .
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- HY-N0031
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Others
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Inflammation/Immunology
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Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation .
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- HY-N3312
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Endogenous Metabolite
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Infection
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Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
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- HY-110303
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XAC dihydrochloride
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Adenosine Receptor
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Neurological Disease
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Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model .
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- HY-12095
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Cannabinoid Receptor
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Neurological Disease
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CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
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- HY-110262
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MAP3K
p38 MAPK
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Inflammation/Immunology
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MSC 2032964A is an orally active, selective inhibitor for apoptosis signal-regulating kinase 1(ASK1) with IC50 of 96 nM. MSC 2032964A preserves the visual responses in EAE mice model and exhibits potency in ameliorating the neuroinflammation .
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- HY-149480
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PROTACs
Estrogen Receptor/ERR
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Cancer
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ERD-3111 (Compound 44) is an orally active PROTAC ERα degrader (DC50: 0.5 nM). ERD-3111 inhibits tumor growth in the parental MCF-7 xenograft model with wild-type ER and two clinically relevant ESR1 mutated mice model. ERD-3111 can be used in the research of ER+ breast cancer .
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- HY-109120
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A4250
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Apical Sodium-Dependent Bile Acid Transporter
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Metabolic Disease
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Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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- HY-135042
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Toll-like Receptor (TLR)
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Neurological Disease
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CAY10614 is a potent TLR4 antagonist. CAY10614 inhibits the lipid A-induced activation of TLR4, with an IC50 of 1.675 μM. CAY10614 can improve survival of mice in lethal endotoxin shock model .
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- HY-14364
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Histamine Receptor
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Inflammation/Immunology
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A-987306 is a potent and oral bioavailable histamine H4 antagonist, with Kis of 3.4 nM and 5.8 nM for rat H4, and human H4. A-987306 shows anti-inflammatory activity in mice peritonitis model .
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- HY-P99216
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PF-04360365; RN 1219
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EGFR
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Neurological Disease
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Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease .
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- HY-13513
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U-104
5 Publications Verification
SLC-0111
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Carbonic Anhydrase
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Cancer
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U-104 (SLC-0111) is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with Ki values of 45.1 nM and 4.5 nM, respectively. U-104 shows a significant delay in tumor growth in mice model .
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- HY-156566
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Epigenetic Reader Domain
PROTACs
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Cancer
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PROTAC BRD4 Degrader-21 (Comp 74) is a PROTAC degrader of BRD4. PROTAC BRD4 Degrader-21 displays significant tumor growth inhibition in tumor -bearing xenograft models in mice and can be used for anticancer research .
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- HY-162477
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Cathepsin
Apoptosis
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Cancer
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TS-24 is an inhibitor for cathepsin S, with an IC50 of 4.3 μM. TS-24 exhibits radiosensitizing activity in wild type breast cancer susceptibility gene 1 (BRCA1) and in TNBC xenograft mice model, through induction of apoptosis .
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- HY-161618
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JAK
EGFR
PI3K
IGF-1R
GSK-3
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Inflammation/Immunology
Endocrinology
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MJ04 is a selective inhibitor for Janus Kinase 3 (JAK 3) with an IC50 of 2.03 nM. MJ04 inhibits T cell differentation and inhibits the proinfammatory cytokines in Lipopolysaccharides (HY-D1056)‑induced macrophages. MJ04 exhibits good pharmacokinetic characters in mice, promotes hair growth in DHT-induced androgenetic alopecia (AGA) in athymic mice model, without significant toxicity (LD50 >2 g/kg) .
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- HY-147529
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mGluR
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Neurological Disease
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mGluR2 modulator 3 (compound 1) is a potent mGluR2 positive allosteric modulator with an EC50 value of 0.87 μM. mGluR2 modulator 3 has activity in psychosis disease models such as methamphetamine-induced hyperactivity and mescaline-induced scratching in mice .
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- HY-158093
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NOD-like Receptor (NLR)
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Inflammation/Immunology
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NIC-12 is a potent NLRP3 inhibitor. NIC-12 selectively reduces circulating IL-1ß levels in the LPS-endotoxemia mice model. NIC-12 inhibits NLRP3 inflammasome activation in mouse macrophages .
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- HY-100827
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LF22-0542
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Bradykinin Receptor
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Inflammation/Immunology
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Safotibant (LF22-0542) is a selective antagonist for kinin B1 receptor (BKB1R), with Ki of 0.35 and 6.5 nM, for human and mouse BKB1R, respectively. Safotibant exhibits analgesic and anti-inflammatory property in mice model .
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- HY-114611
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IRE1
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Metabolic Disease
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BDM44768 is an inhibitior of IDE. BDM44768 exacerbates ER stress-induced IRE1 activation and promotes lipid accumulation in hepatocytes. BDM44768 potentiates activation of the IRE1 pathway in the liver and exacerbates liver lipid accumulation in an acute mice model of ER stress .
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- HY-149708
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ICMT
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Others
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UCM-13207 (compound 21) is a selective ICMT inhibitor that ameliorates basic progeria-like features. UCM-13207 can improve the survival rate of LmnaG609G/G609G mice in the mouse premature aging model .
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- HY-113354
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Endogenous Metabolite
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Neurological Disease
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Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-144361
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Apoptosis
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Cancer
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Antitumor agent-44 (Compound 5n) disrupts the mitochondrial homeostasis, induces cell cycle arrest and apoptosis in human adenocarcinoma cells. Antitumor agent-44 (Compound 5n) possesses good anti-tumor activity in a lung-cancer-cell xenograft mice model .
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- HY-145829
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JAK
Apoptosis
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Inflammation/Immunology
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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 .
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- HY-147014
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CMV
Orthopoxvirus
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Infection
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Cyclic HPMPC is a potent antiviral agent. Cyclic HPMPC can increase arterial oxygen saturation levels in lethal vaccinia virus (IHD strain)-infected mice. Cyclic HPMPC improves the outcome of congenital guinea pig cytomegalovirus (GPCMV) infection and decreases viral replication in guinea pig model .
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- HY-154974
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Liposome
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Cancer
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LNP Lipid-8 (11-A-M) is an ionizable lipid, which can be used for lipid nanoparticles (LNP) to deliver siRNA to T cells without targeting to ligands. LNP LIPs-8 loaded with GFP siRNA (siGFP), and significantly causes GFP gene silencing in mice model .
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- HY-149429
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PPAR
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Metabolic Disease
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PPARδ agonist 9 (compound 21) is a PPARδ agonist (EC50: 3.6 nM). PPARδ agonist 9 has in vivo efficacy, reducing serum levels of MCP-1 in mice and significantly inhibiting atherosclerosis progression in the LDLr-KO model (inhibition rate: 50-60%) .
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- HY-N0031R
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Others
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Inflammation/Immunology
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Plantamajoside (Standard) is the analytical standard of Plantamajoside. This product is intended for research and analytical applications. Plantamajoside is a phenylpropanoid glycoside isolated from Plantago asiatica L.(Plantaginaceae). Plantamajoside has protective effects on LPS-induced acute lung injury (ALI) mice model. Plantamajoside has the potential for the treatment of pulmonary inflammation .
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- HY-N3312R
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Endogenous Metabolite
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Infection
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Matairesinol (Standard) is the analytical standard of Matairesinol. This product is intended for research and analytical applications. Matairesinol confers anti-allergic effects in an allergic dermatitis mouse model. DfE-induced changes in IL-4 and IFN-γ mRNA expression in the ears of NC/Nga mice were reversed by matairesinol application .
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- HY-13659
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NSC 650426
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Antibiotic
Bcl-2 Family
Apoptosis
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Infection
Cancer
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KRN5500 (NSC 650426), a Spicamycin (HY-127130) derivative and a nucleoside-like antibiotic with anti-tumor activity. KRN5500 also induces apoptosis via the down-regulation of Bcl-2 expression. KRN5500 shows a significant efficacy in the human tumor xenograft model in mice .
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- HY-D2279
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Fluorescent Dye
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Inflammation/Immunology
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NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively .
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- HY-158311
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RANKL/RANK
p38 MAPK
NF-κB
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Endocrinology
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Anti-osteoporosis agent-8 (Compound 4aa) is an inhibitor for RANKL, which inhibits RANKL-induced osteoclastogenesis and osteoclast differentiation (IC50 is 2.41 μM) in cells RAW264.7. Anti-osteoporosis agent-8 ameliorates bone loss in an ovariectomized (OVX) mice model .
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- HY-P10580
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Tie
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Infection
Metabolic Disease
Inflammation/Immunology
Cancer
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Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
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- HY-103327
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Cannabinoid Receptor
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Metabolic Disease
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MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
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- HY-109120S
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- HY-164320
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Others
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Cancer
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Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
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- HY-66005
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- HY-144070
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Others
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Cancer
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ErSO-DFP is an anticipatory unfolded protein response (a-UPR) activator. ErSO-DFP has enhanced selectivity for estrogen receptor alpha-positive (ERα+) cancer cells with a wider selectivity window than ErSO.ErSO-DFP displays antitumor activity and leads to profound regression of MCF-7 tumors in mice model .
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- HY-143420
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Phosphodiesterase (PDE)
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Inflammation/Immunology
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ATX inhibitor 15 (compound 30), a indole-based carbamate derivative, is a potent autotaxin (ATX) inhibitor with an IC50 of 2.17 nM. ATX inhibitor 15 inhibits in vivo ATX and the gene expression of pro-fibrotic factors. ATX inhibitor 15 has lung protection effects in Bleomycin challenged mice lung fibrosis model .
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- HY-143237
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Phosphodiesterase (PDE)
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Others
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ATX inhibitor 11 (compound 13c) is a potent ATX (autotaxin) inhibitor, with an IC50 of 2.7 nM. ATX inhibitor 11 can typically alleviate the severity of fibrosis tissues and effectively reduce the deposition of fibrotic biomarker α-SMA in mice fibrosis model. ATX inhibitor 11 can be used for lung fibrosis research .
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- HY-N11872
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Others
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Neurological Disease
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Suffruticosol A is a neuroprotective agent that restores scopolamine-induced cellular neurodegenerative damage. Suffruticosol A ameliorates hippocampal cholinergic deficits and partially enhances BDNF signaling. Suffruticosol A has neuromodulatory effects in a Scopolamine (HY-N0296)-induced model, restoring memory and cognitive performance in mice. Suffruticosol A can be isolated from seeds of P. lactiflora .
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- HY-109120S1
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- HY-161458
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GSK-3
Tau Protein
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Neurological Disease
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GSK-3β inhibitor 16 (compound 7c) is a GSK-3β inhibitor with the IC50 of 4.68 nM. GSK-3β inhibitor 16 decreases Tau hyperphosphorylated aggregate and alleviates cognitive impairments in the Scopolamin (HY-N0296)-induced model in mice .
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- HY-159088
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Opioid Receptor
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Neurological Disease
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KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with Ki of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED50 of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .
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- HY-N0088
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Acetovanillone
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NADPH Oxidase
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Metabolic Disease
Inflammation/Immunology
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Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
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- HY-117370
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AZ1
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Deubiquitinase
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Cancer
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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 .
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- HY-103089
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5-HT Receptor
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Neurological Disease
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LY393558 is a potent and orally active inhibitor of the 5-HT transporter and an antagonist of 5-HT1B and 5-HT1D receptors. LY393558 increase the extracellular levels of 5-HT in mice model frontal cortex. LY393558 can be used for researching depression .
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- HY-117924
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Autophagy enhancer-67
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Autophagy
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Neurological Disease
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AUTEN-67 (Autophagy enhancer-67) is an orally active autophagy enhancer and MTMR14 inhibitor. AUTEN-67 has anti-aging and neuroprotective effects. AUTEN-67 protects neurons from stress-induced cell death. AUTEN-67 also restores nesting behavior in a mice model of Alzheimer disease .
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- HY-161425
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Apoptosis
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Cancer
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Antitumor agent-149 (Compound 3) is an analogue of Echinomycin (HY-106101). Antitumor agent-149 inhibits HIF-1α-mediated transcription. Antitumor agent-149 induces cancer cell apoptosis. Antitumor agent-149 inhibits tumor growth in SW620 xenograft mice model .
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- HY-169018
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- HY-160887
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5-HT Receptor
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Neurological Disease
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FPT, a 2-Aminotetralin, is an efficacious partial agonist at 5-HT1AR, a full agonist at 5-HT1BR and 5-HT1DR with EC50s of 39.3 nM, 1.2 nM, 0.5 nM, respectively. FPT is a weak agonist at 5-HT7R. FPT shows in vivo efficacy as an antiepileptic in Fmr1 knockout mice and has anxiolytic-like and prosocial effects in Fmr1 knockout mice and other mouse models .
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- HY-110190
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ML396
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mGluR
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Neurological Disease
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VU0422288 (ML396) is a positive allosteric modulator of group III mGluRs. VU0422288 inhibits mGluRs with EC50s of 125 nM, 146 nM, and 108 nM for mGluR4, mGluR7, and mGluR8, respectively in calcium mobilization assays. VU0422288 reverses deficits in contextual fear memory, social recognition, and apneas in Rett syndrome (RTT) model mice .
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- HY-126477
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NNK
1 Publications Verification
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Endogenous Metabolite
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Cancer
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NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser 70 and c-Myc at Thr 58 and Ser 62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
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- HY-156109
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PDHK
Mitochondrial Metabolism
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Cancer
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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 .
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- HY-158374
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IRAK
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Inflammation/Immunology
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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 .
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- HY-15815
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Epigenetic Reader Domain
Apoptosis
CDK
HIV
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Cancer
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Bromosporine is a potent BET inhibitor with an IC50 value of 2.1 μM for PCAF. Bromosporine can arrest cell cycle and induce apoptosis in cancer cells. Bromosporine exhibits excellent antitumor activity in xenograft mice model when combined with 5-FU (HY-90006). Bromosporine can increase CDK9 T-loop phosphorylation in HIV-1 latency models, resulting the protection of reactivate HIV-1 replication from latency. Bromosporine can be used to research colorectal cancer, acute myeloid leukemia (AML) and AIDS .
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- HY-N6967
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(-)-α-Bisabolol
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Apoptosis
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Neurological Disease
Inflammation/Immunology
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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 .
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- HY-113354S1
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Isotope-Labeled Compounds
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Neurological Disease
|
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Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
|
-
- HY-155032
-
|
|
P-glycoprotein
|
Cancer
|
|
P-gp inhibitor 15 (compound 7a) is a nonsubstrate inhibitor of P-glycoprotein (Pgp). P-gp inhibitor 15 inhibits Pgp-ATPase activity，and interfers Pgp-mediated Rhodamine123 efflux. P-gp inhibitor 15 also enhances the inhibitory efficacy of Paclitaxel (HY-B0015)，inhibits tumor progress in nude mice KBV xenograft tumors model .
|
-
- HY-153903
-
|
|
Others
|
Others
|
|
RASP-IN-1 (compound A) is a lipophili ccompound used for macular degeneration inhibition. RASP-IN-1 is biologically active in the retina of the rabbit's eye. Thirty minutes after IP treatment with 14C-RASP-IN-1 (10 mg/kg)，the Cmax amount of 14C-RASP-IN-1 in the posterior eye cup is 14.36 μg/g in mice model .
|
-
- HY-156120
-
|
|
CD38
|
Metabolic Disease
|
|
CD38 inhibitor 3 (compound 1) is a potent CD38 inhibitor (IC50=11 nM). CD38 inhibitor 3 can promote mitochondrial biogenesis, reduce lactate levels, and increase NAD+ content and Nrf2 expression. In a model of mitochondrial myopathy, CD38 inhibitor 3 increases muscle contraction/development and improves exercise tolerance in Pus1 -/- mice .
|
-
- HY-161373
-
|
|
PI3K
|
Cancer
|
|
PI3Kα-IN-22 (Compound 17) is an orally active, potent and selective inhibitor of PI3Kα H1047R, with an IC50 of 1 nM for pAKT T47D AlphaLISA. PI3Kα-IN-22 can induce tumor regressions in the HCC1954 tumor model in mice .
|
-
- HY-162646
-
|
|
Thrombin
|
Cardiovascular Disease
|
|
FXIIa-IN-5 (Compound 4J) is an orally active, selective inhibitor for factor XIIa (FXIIa), with IC50 of 21 nM. FXIIa-IN-5 inhibits the intrinsic coagulation pathways, and exhibits anti-inflammatory and antithrombotic activity in Carrageenan (HY-125474)-induced mice thrombosis models. FXIIa-IN-5 exhibits moderate pharmacokinetic characteristics and slightly toxicity (at 100 mg/kg) .
|
-
- HY-114169
-
|
|
Discoidin Domain Receptor
|
Inflammation/Immunology
Cancer
|
|
WRG-28 is a selective, extracellularly acting DDR2 allosteric inhibitor, with an IC50 of 230 nM. WRG-28 inhibits tumor invasion, migration and tumor-supporting effects of cancer-associated fibroblasts (CAFs). WRG-28 inhibits metastatic breast tumor cell colonization in the lungs. WRG-28 also shows good activity of relieving rheumatoid arthritis in CAIA model of mice .
|
-
- HY-125639
-
|
(rac)-AR-13324 M1 metabolite
|
PKC
ROCK
|
Cardiovascular Disease
|
|
(rac)-AR-13503 ((rac)-AR-13324 M1 metabolite) is the isoform of AR-13503 (HY-12798C). AR-13503 a ROCK/PKC inhibitor, inhibiting angiogenesis and enhancing retinal pigment epithelium (RPE) permeability. AR-13503 also inhibits the formation of aberrant neovascularization (NV) in oxygen-induced retinopathy (OIR) model in mice .
|
-
- HY-155028
-
|
|
FGFR
|
Cancer
|
|
FGFR-IN-11 (compound I-5) is an orally active and covalent FGFR inhibitor with IC50 values of 9.9 nM (FGFR1), 3.1 nM (FGFR2), 16 nM (FGFR3), and 1.8 nM (FGFR4), respectively. FGFR-IN-11 inhibits multiple cancer cell proliferation with nanomolar activity. FGFR-IN-11 inhibits tumor growth significantly in xenograft mice models .
|
-
- HY-155193
-
|
|
Others
|
Inflammation/Immunology
|
|
XY-52 (Compound 32) is a Stimulation-2 (ST2) inhibitor, with an IC50 value of 5.68 μM in AlphaLISA assay, and 4.59 μM in HEK-Blue assay. XY-52 increases proinflammatory T-cell proliferation. XY-52 reduces the plasma sST2 and IFNγ biomarkers in the graft versus host disease (GVHD) mice model .
|
-
- HY-157082
-
|
|
Enterovirus
|
Infection
|
|
ZHSI-1 is an EV71 (Enterovirus 71) inhibitor that inhibits EV71/CVA16 replication and virus-induced pyroptosis associated with viral pathogenesis. ZHSI-1 effectively prevents EV71 infection in neonatal and young mice in animal models. ZHSI-1 can be used to study viral infections such as hand, foot and mouth disease (HFMD) .
|
-
- HY-162312
-
|
|
Deubiquitinase
Apoptosis
|
Cancer
|
|
LLK203 is a potent USP2/USP8 dual-target inhibitor with IC50s of 0.89 μM and 0.52 μM, respectively. LLK203 leads a degradation of ERα and induces apoptosis of breast cancer MCF-7 cells. LLK203 demonstrates antitumor activities against the 4T1 tumor mice model .
|
-
- HY-12443
-
|
|
Casein Kinase
|
Neurological Disease
|
|
PF-5006739 is a potent and selective inhibitor of CK1δ/ε with IC50s of 3.9 nM and 17.0 nM, respectively. PF-5006739 is a potential therapeutic agent for a range of psychiatric disorders with low nanomolar in vitro potency for CK1δ/ε and high kinome selectivity. PF-5006739 attenuats opioid agent-seeking behavior in a rodent operant reinstatement model in animals in a dose-dependent manner . PF-5006739 improves glucose tolerance in both diet-induced obesity (DIO) and genetic (ob/ob) mice models of obesity .
|
-
- HY-125172
-
|
Polyglutamine Aggregation inhibitor III
|
Others
|
Others
|
|
C2-8 is an inhibitor of polyglutamine (polyQ) aggregation (IC50s=25 and 0.05 μM for recombinant HDQ51 and in PC12 cells, respectively). It also inhibits polyQ aggregation in organotypic hippocampal slice cultures isolated from R6/2 transgenic mice and reduces neurodegeneration in a dose-dependent manner in a Drosophila model of Huntington's disease. C2-8 (100 and 200 mg/kg) reduces huntingtin aggregate size, reduces neuronal atrophy, and improves motor performance in a rotarod test in the R6/2 transgenic mouse model of Huntington's disease.
|
-
- HY-15096
-
|
FJ-776
|
Fluorescent Dye
HSP
|
Cancer
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-126124
-
AP39
3 Publications Verification
|
Others
|
Cardiovascular Disease
Neurological Disease
|
|
AP39 is a triphenylphosphonium derivatised anethole dithiolethione and mitochondria-targeting hydrogen sulfide (H2S) donor. AP39 increases intracellular H2S levels. AP39 exerts cytoprotective effects and maintains mitochondrial DNA integrity under oxidative stress conditions. AP39 protects against myocardial reperfusion injury in mice model and has the potential for Alzheimer's disease research .
|
-
- HY-134923
-
CA77.1
2 Publications Verification
|
Autophagy
|
Neurological Disease
|
|
CA77.1 is a potent, brain-penetrant and orally active chaperone-mediated autophagy (CMA) activator with favorable pharmacokinetics. CA77.1 is a derivative of AR7 (HY-101106) and can increase the expression of the lysosomal receptor LAMP2A in lysosomes. CA77.1 improves behavior and neuropathology in PS19 mice model and can be used for alzheimer's disease research .
|
-
- HY-108790
-
|
Peginterferon β-1a
|
Apoptosis
|
Neurological Disease
Cancer
|
|
Peginterferon beta-1a (Peginterferon β-1a) is the first pegylated interferon beta-1a molecule. Peginterferon beta-1a induces cancer cells apoptosis and shows anti-tumor activities in nude mice models. Peginterferon beta-1a can be used for the research of cancer and multiple sclerosis (RMS) .
|
-
- HY-149984
-
|
|
Monoamine Oxidase
|
Neurological Disease
Inflammation/Immunology
|
|
MAO-B-IN-21 is an excellent MAO-B inhibitor with antioxidant activity and anti-Aβ aggregation activity. MAO-B-IN-21 also exhibits metal-ion chelating ability, anti-neuroinflammation (NO, TNF-α), neuroprotective activity and BBB permeability. MAO-B-IN-21 significantly improves the memory and cognitive impairment in Aβ1-42 induced Alzheimer's disease mice model .
|
-
- HY-158315
-
|
|
Dipeptidyl Peptidase
|
Inflammation/Immunology
|
|
NZ-97 is an inhibitor for dipeptidyl peptidase 4 (DPP4) with an IC50 of 18 nM. NZ-97 exhibits a low initial plasma exposure with Cmax of 0.13 µM, which is eliminated in 8 h. NZ-97 ameliorates damage in the Lipopolysaccharides (HY-D1056)-induced lung injury and Bleomycin (HY-108345)-induced lung fibrosis in mice model .
|
-
- HY-164546
-
|
|
STAT
Apoptosis
|
Cancer
|
WB436B is a highly selective STAT3 inhibitor. WB436B can selectively inhibit STAT3-Tyr705 phosphorylation and the expression of STAT3 target genes, showing cytotoxic effects on pancreatic cancer cells and inducing apoptosis. WB436B can suppress tumor growth and metastasis in pancreatic cancer mouse models, extending the survival of tumor-bearing mice .
|
-
- HY-15344
-
|
|
Others
|
Neurological Disease
Metabolic Disease
|
|
Ketone monoester is an orally available ketone monoester that serves as a source of nutritional ketones. Ketone monoester increases plasma beta-hydroxybutyrate, acetoacetate, blood glucose, blood sodium, and blood creatinine levels in mouse models. Ketone monoester has the potential to improve athletic performance and endurance in animals. Ketone monoester partially prevents myasthenia in septic mice. Ketone monoester may also be used to study Parkinson's disease or diabetes .
|
-
- HY-15698A
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 dihydrochloride is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 dihydrochloride is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 dihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-121495
-
|
|
Parasite
|
Infection
|
|
BKI-1369 is a bumped kinase inhibitor (BKI). BKI-1369 increases human Ether-a-go-go-related gene (hERG)-inhibitory activity with an IC50 of 1.52 μM. BKI-1369 reduces the parasite burden and diseases severity in the gnotobiotic pig model. BKI-1369 has been well characterized for potency, stability, metabolism, toxicity, pharmacokinetics and is potent against C. parvum in infected mice and calves .
|
-
- HY-146401
-
|
|
CXCR
|
Cancer
|
|
CXCR4 antagonist 6 (compound 46) is a potent CXCR4 antagonist with an IC50 value of 79 nM. CXCR4 antagonist 6 inhibits CXCL12 induced cytosolic calcium flux (IC50 = 0.25 nM). CXCR4 antagonist 6 significantly mitigates CXCL12/CXCR4 mediated cell migration. CXCR4 antagonist 6 exhibits marked efficacy in a cancer metastasis model in mice .
|
-
- HY-147720A
-
|
|
γ-secretase
|
Neurological Disease
|
|
γ-Secretase modulator 11 hydrochloride (compound 1o) is a potent and orally active γ-secretase modulator with an IC50 of 0.029 µM. γ-Secretase modulator 11 hydrochloride induces a robust reduction in brain Aβ42 levels. γ-Secretase modulator 11 hydrochloride rescues cognitive deficits exhibited by AD model mice. γ-Secretase modulator 11 hydrochloride has the potential for the research of alzheimer's disease .
|
-
- HY-P99583
-
|
MEDI4893
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
|
-
- 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-15698
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 is a potent and orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively . CRT0066101 is also a potent PIM2 inhibitor with an IC50 of ~135.7 nM. CRT0066101 exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-158316
-
|
|
Others
|
Others
|
|
BTL-MK (Compound 19) an orally active antiallergic agent, that inhibits degranulation of mast cells with an IC50 of 6.7 μM, through binding to the inhibitory receptor FcγRIIB. BTL-MK improves the metaboilic stability in human liver microsomes. BTL-MK ameliorates the allergic response in Ovalbumins (HY-W250978)-induced food allergy mice model. BTL-MK exhibits a good pharmacokinetic character with metabolic stability .
|
-
- HY-N0088R
-
|
|
NADPH Oxidase
|
Metabolic Disease
Inflammation/Immunology
|
|
Apocynin (Standard) is the analytical standard of Apocynin. This product is intended for research and analytical applications. Apocynin is a selective NADPH-oxidase inhibitor with an IC50 of 10 μM . Apocynin improves acute lung inflammation in Carrageenan (HY-125474)-induced pleurisy mice model . Apocynin can also be used for cancer research . Apocynin reverses the aging process in mesenchymal stem cells to promote osteogenesis and increases bone mass .
|
-
- HY-16561S1
-
|
trans-Resveratrol-13C6; SRT501-13C6
|
Isotope-Labeled Compounds
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
|
-
- HY-16561S
-
|
trans-Resveratrol-d4; SRT501-d4
|
Isotope-Labeled Compounds
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
|
-
- HY-153808
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .
|
-
- HY-143402
-
|
|
Topoisomerase
|
Cancer
|
|
Topoisomerase I/II inhibitor 2 (compound 1a) is a potent Topoisomerase inhibitor (IC50= 9.82 μM on Huh7 cells and 6.83 μM on LM9 cells). Topoisomerase I/II inhibitor 2 has dual inhibition on DNA topoisomerase I/II, also can obviously reduce the growth of xenograft tumor in mice model. Topoisomerase I/II inhibitor 2 has the potential value in researching liver cancer .
|
-
- HY-124727
-
|
|
JAK
Apoptosis
|
Cancer
|
|
ZT55 is an orally active and highly-selective JAK2 inhibitor with an IC50 value of 0.031 μM. ZT55 inhibits the proliferation of JAK2 V617F-expressing HEL cell lines and induces apoptosis and cycle arrest. ZT-55 also effectively inhibits the growth of HEL xenograft tumours in a mice model. ZT-55 can be used in studies of myeloproliferative neoplasms, polycythemia vera and primary thrombocythemia .
|
-
- HY-149838
-
|
|
NF-κB
|
Cancer
|
|
NF-κB-IN-9 is a nuclear factor kappa B (NF-κB) targeting sonosensitizer (λex/λem=489/628 nm). NF-κB-IN-9 exhibits strong inhibition on NF-κB signaling due to its two resveratrol units in one molecule. NF-κB-IN-9 has anti-tumor activity and shows remarkable sonocytotoxicity against cancer cells. NF-κB-IN-9 has biosafety in eenograft mice model.
|
-
- HY-155525
-
|
|
PPAR
|
Metabolic Disease
Inflammation/Immunology
|
|
Anti-NASH agent 1 (compound 3d)，a derivative of Elafibranor (HY-16737)，is a potent agonist of PPAR-α/δ，targeting to nonalcoholic steatohepatitis (NASH). Anti-NASH agent 1 (3-10 mg/kg; 4 weeks) improves hyperlipidemia，liver fat degeneration and liver inflammation in Methionine-choline deficiency (MCD) induced NASH mice model. Anti-NASH agent 1 shows low liver toxicity and potent liver protection effect .
|
-
- HY-P5875
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
|
-
- HY-118282
-
|
|
PGE synthase
|
Endocrinology
|
|
mPGES-1-IN-2 (compound III) is a benzimidazole-based mPGES-1 inhibitor that also inhibits adipophysin PGD synthase (I-PGDS) (5 μM, IR=60 %). mPGES-1-IN-2 reduces PGE2 production and tends to reduce levels of other prostaglandins. mPGES-1-IN-2 effectively inhibits acute inflammation in an air sac model stimulated by Carrageenan (HY-125474) in mice .
|
-
- HY-164036
-
|
|
Antibiotic
Bacterial
|
Infection
|
|
Lolamicin is a Gram-negative specific antibiotic. Lolamicin is active against more than 130 multidrug-resistant clinical isolates, has shown efficacy in multiple mouse models of acute pneumonia and sepsis infection, and protects the gut microbiome of mice against secondary infection with Clostridium difficile. The selective killing of pathogenic gram-negative bacteria by Lolamicin is a result of the low sequence homology of pathogenic bacteria and symbiotic bacteria. Lolamicin can be used in the study of infection caused by Gram-negative pathogens .
|
-
- HY-162710
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
LTA4H-IN-5 (Compound H122) is an orally active inhibitor for leukotriene A4 hydrolase (LTA4H), that inhibits the LTA4H aminopeptidase and LTA4H hydrolase with IC50 of 0.38 nM and 16.93 nM. LTA4H-IN-5 exhibits good pharmacokinetic characteristics in C57 mice and ameliorates the DNBS-induced ulcerative enteritis in rat models .
|
-
- HY-15698B
-
|
|
PKD
Pim
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
CRT0066101 trihydrochloride is the trihydrochloride salt form of CRT0066101 (HY-15698). CRT0066101 trihydrochloride is an orally active PKD inhibitor with IC50 values of 1 nM, 2.5 nM and 2 nM for PKD1, PKD2, and PKD3, respectively. CRT0066101 trihydrochloride is also an inhibitor for PIM2 with an IC50 of ~135.7 nM. CRT0066101 trihydrochloride exhibits anti-inflammatory activity in mice LPS (HY-D1056)-induced lung injury models, and has anticancer effects .
|
-
- HY-126477R
-
|
|
Endogenous Metabolite
|
Cancer
|
|
NNK (Standard) is the analytical standard of NNK. This product is intended for research and analytical applications. NNK is a nicotine-nitrosated derivative. NNK simultaneously stimulates Bcl2 phosphorylation exclusively at Ser70 and c-Myc at Thr58 and Ser62 through activation of both ERK1/2 and PKCα . NNK induces survival and proliferation of human lung cancer cells. NNK can be used for lung cancer mice model structure .
|
-
- 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-14162
-
|
|
FLAP
|
Inflammation/Immunology
|
AM103 (free acid) is a selective FLAP inhibitor that can block the first step of the LT pathway, which is 5-LO activation. AM103 (free acid) can inhibit the production of LTB4 and cysteinyl leukotrienes (CysLT). AM103 (free acid) has anti-inflammatory activity in a mouse model of chronic lung inflammation and can extend the survival time of mice injected with platelet-activating factor. AM103 (free acid) can be used for research on respiratory diseases such as asthma .
|
-
- HY-B1350A
-
|
Sodium fusidate; SQ-16360
|
Bacterial
Antibiotic
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Fusidic acid sodium salt is an orally available antibacterial agent that inhibits bacterial protein synthesis by preventing the release of translation elongation factor G (EF-G) from ribosomes. Fusidic acid sodium salt inhibits the inhibitory and activating effects of interleukins IL-1 and IL-6 on glucose-induced insulin production and exhibits antidiabetic effects in a rat model. Fusidic acid sodium salt improves the symptoms of colitis in rats and inhibits the growth of Toxoplasma gondii and Listeria monocytogenes EGD in vitro, but not in mice .
|
-
- HY-101117
-
|
|
Histone Methyltransferase
|
Cancer
|
|
EED226 is a polycomb repressive complex 2 (PRC2) inhibitor, which binds to the K27me3-pocket on embryonic ectoderm development (EED) and shows strong antitumor activity in xenograft mice model . EED226 is a potent, selective, and orally bioavailable EED inhibitor . EED226 inhibits PRC2 with an IC50 of 23.4 nM when the H3K27me0 peptide is used as a substrate in the in vitro enzymatic assays .
|
-
- HY-N1420
-
|
L-Rhamnose
|
Endogenous Metabolite
MMP
Interleukin Related
PKA
|
Cancer
|
|
Rhamnose (L-Rhamnose) is an orally active deoxysugar that is widely found in plants and bacteria. Rhamnose can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models, showing anti-aging effects. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose is also used in cancer research .
|
-
- HY-145628
-
|
|
Sigma Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
CM398 is a highly selective, orally active sigma-2 receptor ligand (Ki=0.43 nM), with high sigma-1/sigma-2 selectivity rato (1000-fold). CM398 shows notable affinity for dopamine (Ki=32.90 nM) and serotonin transporters (Ki=244.2 nM). CM398 shows promising anti-inflammatory analgesic effects in the formalin model of inflammatory pain in mice .
|
-
- HY-146494
-
|
|
Androgen Receptor
|
Cancer
|
|
Androgen receptor antagonist 5 (compound 42f) is a potent androgen receptor (AR) antagonist with an IC50 value of 6.17 μM. Androgen receptor antagonist 5 can effectively impair AR nuclear translocation, reducing the levels of nuclear AR, and disrupts AR-mediated gene regulation. Androgen receptor antagonist 5 has antiproliferative activity against LNCaP and exhibits antitumor activity in LNCaP xenograft tumor mice model. Androgen receptor antagonist 5 can be used for researching prostate cancer .
|
-
- HY-150562
-
|
|
CDK
|
Cancer
|
|
CDK9-IN-19 is a highly potent and selective CDK9 inhibitor with an IC50 value of 2.0 nM. CDK9-IN-19 has excellent cellular antiproliferative activity, moderate pharmacokinetic property and low hERG inhibition. CDK9-IN-19 significantly induces tumour growth inhibition in an MV4-11 xenograft mice model. CDK9-IN-19 can be used for researching acute myeloid leukaemia (AML) .
|
-
- HY-150596
-
|
|
Apoptosis
Bcl-2 Family
JNK
|
Cancer
|
|
CT1-3 is a potent anticancer agent. CT1-3 induces mitochondria-mediated apoptosis by regulating JNK/Bcl-2/Bax/XIAP pathway. CT1-3 suppresses the epithelial mesenchymal transition (EMT) potential of human cancer cells (HCCs) via regulating the E-cadherin/Snail axis, thus inhibits tumorigenesis. CT1-3 has a strong antitumor effect in mice model and exhibits no significant hepatic and renal toxicity .
|
-
- HY-151155
-
|
|
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
ALK-IN-23 is a potent ALK inhibitor with IC50 values of 1.6 nM, 0.71 nM and 1.3 nM for ALK WT, ALK L1196M and ALK G1202R. ALK-IN-23 can block cell cycle in G2 phase and induce apoptosis. ALK-IN-23 inhibits cancer cell migration and colony formation in vitro. ALK-IN-23 exhibits antitumor activity in H2228 xenograft nude mice model with hypotoxicity .
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- HY-153369
-
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Guanylate Cyclase
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Cardiovascular Disease
Neurological Disease
|
|
BAY-747 is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model .
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- HY-162596
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BA-1049
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ROCK
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Neurological Disease
|
|
NRL-1049 (BA-1049) is a ROCK2 selective inhibitor (IC50: 0.59 µM and 26 µM for ROCK2 and ROCK1 respectively). NRL-1049 reduces Lysophosphatidic acid induced ROCK activation in endothelial cells. NRL-1049 reduces lesion volume and hemorrhagic transformation in a mouse model of cavernous angiomas. NRL-1049 also preserves the BBB and suppresses seizures after brain injury, and inhibits hemorrhagic transformation after ischemic stroke in mice .
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-
- HY-162640
-
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ROR
|
Cancer
|
|
ROR1-IN-1 (Compound 19h) is an inhibitor for receptor tyrosine kinase-like orphan receptor 1 (ROR 1) with Ki of 0.10 μM. ROR1-IN-1 inhibits proliferation of cancer cells H1975, A549 and MDA-MB-231, with IC50 of 0.36 μM, 1.37 μM and 0.47 μM. ROR1-IN-1 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
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-
- HY-162645
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TAM Receptor
|
Inflammation/Immunology
Cancer
|
|
BPR5K230 is a dual inhibitor for the receptor tyrosine kinase MER and AXL, with IC50 of 4.1 nM and 9.2 nM. BPR5K230 inhibits the proliferation of Ba/F3-MER with IC50 of 5 nM. BPR5K230 exhibits good pharmacokinetic characteristics in mice, exhibits anti-inflammatory and antitumor against 4T1, MDA-MB-231, MC38 and Hepa1?6 in mouse models .
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- HY-139659
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PROTACs
Androgen Receptor
Progesterone Receptor
Apoptosis
|
Cancer
|
|
ARD-61 is a highly potent, effective and specific PROTAC androgen receptor (AR) degrader. ARD-61 potently and effectively induces AR and progesterone receptors (PR) degradation in AR+ cancer cell lines. ARD-61 induces apoptosis and effectively induces tumor growth inhibition in the MDA-MB-453 xenograft model in mice . ARD-61 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-143880
-
|
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Mas-related G-protein-coupled Receptor (MRGPR)
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Neurological Disease
|
|
MRGPRX1 agonist 4 (compound 1t) is a potent and orally active Mas-related G protein-coupled receptor X1 (MRGPRX1) positive allosteric modulator with an EC50 value of 0.1 μM. MRGPRX1 agonist 4 has good metabolic stability and oral bioavailability. MRGPRX1 agonist 4 can reduce behavioral heat hypersensitivity in a neuropathic pain model humanized MRGPRX1 mice. MRGPRX1 agonist 4 can be used for researching neuropathic pain .
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-
- HY-147720
-
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γ-secretase
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Neurological Disease
|
|
5-{8-[(3,4'- difluoro [1,1'- biphenyl]-4-yl) methoxy] - 2-methylimidazo [1,2-a] pyridin-3-yl}-n-methylpyridin-2-formamide (1o) showed high potency in vitro and brain exposure, inducing brain a β 42 levels were significantly reduced and showed undetectable inhibition of cytochrome P450 enzymes. In addition, compound 1o showed excellent anti cognitive deficit effect in AD model mice.
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-
- HY-117006
-
E1231
1 Publications Verification
1-{4-[2-(5-Methylfuran-2-yl)quinoline-4-carbonyl]piperazin-1-yl}ethan-1-one
|
Sirtuin
|
Cardiovascular Disease
|
|
E1231 is an orally active activator of Sirtuin 1 (SIRT1) (EC50=0.83 μM), to modulate cholesterol and lipid metabolism. E1231 interactes with SIRT1 (KD=9.61 μM) and deacetylated liver X receptor-alpha (LXRα), and increases ATP-binding cassette transporter A1 (ABCA1) expression. E1231 also reduces atherosclerotic plaque development in ApoE -/- mice model. E1231 can be used for research in cholesterol and lipid disorder-related diseases .
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-
- HY-162033
-
|
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Others
|
Others
|
|
PAT1inh-A0030 is a selective PAT1 (SLC26A6) inhibitor (IC50= 1.0 μM). PAT1inh-A0030 inhibits fluid absorption in the ileum of wild-type and cystic fibrosis (CF) mice (CftrdelF508/delF508) in a closed-loop model of intestinal fluid absorption. PAT1inh-A0030 can be used in the study of intestinal diseases related to CF .
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-
- HY-164102
-
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TNF Receptor
NF-κB
|
Inflammation/Immunology
|
|
TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
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-
- HY-161833
-
|
|
Interleukin Related
TNF Receptor
|
Inflammation/Immunology
|
|
HSP90-IN-31 (compound Be01) causes reduction of CD80 and CD86 expression on dendritic cells (DCs). HSP90-IN-31 decreases the production of pro-inflammatory cytokines (IL-6, TNF-α, and IL-1β) in BMDC and peritoneal macrophages stimulated by LPS (HY-D1056). Under the delayed-type hypersensitivity (DTH) mice model, HSP90-IN-31 reduces ear swelling and pro-inflammatory cytokines in the spleen .
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-
- HY-111817A
-
|
|
Parasite
|
Infection
|
|
(Rac)-ACT-451840 is an isomer of ACT-451840 that exhibits significant antimalarial effects. (Rac)-ACT-451840 exhibits significant antimalarial activity against P. berghei-infected mice at a dose of 20 mg/kg (ED90=13 mg/kg), and has an inhibitory effect at a dose of 300 mg/kg. The ED90 of (Rac)-ACT-451840 in the P. falciparum humanized immunodeficient mouse model is 3.7 mg/kg. (Rac)-ACT-451840 is similar to artemisinin, with a rapid onset of action but requires repeated high doses.
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-
- HY-116330
-
|
|
Calcium Channel
TRP Channel
|
Neurological Disease
Inflammation/Immunology
|
|
Hyperforin is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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-
- HY-107513
-
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mGluR
|
Neurological Disease
Cancer
|
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
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-
- HY-155226
-
|
|
FLT3
Apoptosis
|
Cancer
|
|
FLT3-IN-21 (compound LC-3) is a potent FLT3 inhibitor (IC50: 8.4 nM) and induces apoptosis. FLT3-IN-21 can arrest the cell cycle in the G1 phase and inhibit the proliferation of FLT3-ITD-positive AML cells MV-4-11 (IC50: 5.3 nM). In mice, FLT3-IN-21 (10 mg/kg/d) inhibited tumor growth in the MV-4-11 xenograft model (TGI=92.16%) .
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-
- HY-117707
-
|
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Raf
|
Cancer
|
|
EBI-907 is an orally active and highly potent B-Raf V600E inhibitor. EBI-907 demonstrates excellent A375 and Colo-205 cellular antiproliferative activity with IC50 values of 13 nM and 14 nM, respectively. EBI-907 can also cause tumor regression in a B-Raf V600E-dependent Colo-205 tumor xenograft model of mice. EBI-907 is promising for research of melanoma and B-Raf V600E associated cancers .
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-
- HY-16561
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Resveratrol
Maximum Cited Publications
87 Publications Verification
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
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- HY-116330A
-
|
Hyperforin DCHA
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TRP Channel
Calcium Channel
|
Neurological Disease
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
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- HY-18099
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S1RA
1 Publications Verification
E-52862
|
Sigma Receptor
5-HT Receptor
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Neurological Disease
|
|
S1RA (E-52862) is a highly selective σ1 receptor (σ1R) antagonist with Kis of 17 nM and 23.5 nM for human σ1R and guinea pig σ1R, respectively. S1RA has Moderate antagonistic activity for human 5-HT2B receptor (Ki= 328 nM). S1RA has antinociceptive effects in neuropathic pain models. S1RA prevents mechanical and cold hypersensitivity in Oxaliplatin (HY-17371)-treated mice .
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-
- HY-100555
-
|
|
HSP
|
Infection
Cancer
|
|
CH5138303 is a potent and orally active Hsp90 inhibitor. CH5138303 shows high binding affinity for N-terminal Hsp90α, with Kd of 0.52 nM. CH5138303 shows potent anti-proliferative activity against human cancer cell lines (HCT116 and NCI-N87), with IC50 values of 0.098 and 0.066 μM, respectively. CH5138303 shows high oral bioavailability in mice (F=44.0%). CH5138303 shows potent antitumor efficacy in a human NCI-N87 gastric cancer xenograft model .
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-
- 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 .
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-
- HY-155199
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE1-IN-5 (Compound 10c) is a selective PDE1C inhibitor (IC50: 15 nM). PDE1-IN-5 has anti- inflammatory activity, and inhibits expression of iNOS, TNF-α, IL-1α, IL-1β, and IL-6 induced by LPS. PDE1-IN-5 has anti-inflammatory bowel disease (IBD) effects in the dextran sodium sulfate (DSS)-Induced colitis mice model. PDE1-IN-5 can be used for research of IBD .
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-
- HY-161781
-
|
|
HSP
EGFR
Akt
Survivin
|
Cancer
|
|
HVH-2930 is an inhibitor for heat shock protein 90 (HSP90). HVH-2930 inhibits cell viability of BT474 (Trastuzumab (HY-P9907) sensitive) and JIMT-1 (Trastuzumab (HY-P9907) resistant), with IC50 of 6.86 μM and 4.42 μM, through downregulation of HSP90 clients HER2, p-HER2, AKT, p-AKT, cyclin D1 and survivin. HVH-2930 exhibits antitumor efficacy in mouse models. HVH-2930 exhibits good pharmacokinetic characteristics in mice .
|
-
- HY-16561G
-
|
trans-Resveratrol; SRT501
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-123237
-
|
|
c-Met/HGFR
FLT3
Trk Receptor
Apoptosis
Autophagy
|
Cancer
|
|
KRC-108, an aminopyridine, is an orally active multiple kinase inhibitor with IC50s of 80 nM, 23 nM, 3 nM, 70 nM, 30 nM, 39 nM for c-Met, c-Met M1250T, c-Met Y1230D, Ron, Flt3 and TrkA, respectively. KRC-108 induces cell cycle arrest, apoptotic cell death, and autophagy. KRC-108 exhibits anti-tumor activity in vivo in HT29 colorectal cancer, NCI-H441 lung cancer xenograft models in athymic BALB/c nu/nu mice .
|
-
- HY-161953
-
|
|
OGA
|
Neurological Disease
|
|
O-GlcNAcase-IN-2 (compound 81) is an orally effective, blood-brain barrier-permeable OGA inhibitor (IC50=4.93 nM). O-GlcNAcase-IN-2 can increase the O-GlcNAcylation level of proteins and phosphorylation of tau (p-Ser199, p-Thr205 and p-Ser396) in the OA-damaged SH-SY5Y cell model. O-GlcNAcase-IN-2 can also improve cognitive impairment in APP/PS1 mice and has potential anti-Alzheimer's disease (AD) effects .
|
-
- 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-145774
-
|
|
PD-1/PD-L1
|
Cancer
|
|
PD-1/PD-L1-IN-23 is a potent and orally active inhibitor of PD-1/PD-L1. PD-1/PD-L1-IN-23 is an ester proagent of L7. L7 is a benzo[c][1,2,5]oxadiazole derivative and biologically evaluated as inhibitors of PD-L1. PD-1/PD-L1-IN-23 displays significant antitumor effects in tumor models of syngeneic and PD-L1 humanized mice .
|
-
- HY-156792
-
|
|
Others
|
Cancer
|
|
RIOK2-IN-1 (com 4) is a potent and selective RIOK2 inhibitor (Kd=150 nM), but has low cellular activity (IC50=14,600 nM). RIOK2 is an atypical kinase associated with a variety of human cancers and is involved in ribosome maturation and cell cycle progression. The small molecule inhibitor CQ211 (HY-147655), an improvement of RIOK2-IN-1 as the lead compound, has good in vivo and in vitro activity, inhibits the proliferation of MKN-1 and HT-29 cancer cells, and can xenograft MKN in mice -1 model inhibits tumor progression .
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-
- HY-16561R
-
|
trans-Resveratrol (Standard); SRT501 (Standard)
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
Infection
Inflammation/Immunology
Cancer
|
|
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
- HY-W017540
-
|
|
ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
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-
- HY-116330AR
-
|
|
TRP Channel
Calcium Channel
|
Neurological Disease
|
|
Hyperforin (dicyclohexylammonium salt) (Standard) is the analytical standard of Hyperforin (dicyclohexylammonium salt). This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
|
-
- HY-145836
-
|
|
FGFR
|
Cancer
|
|
FGFR4-IN-8 (Compound 7v) is an ATP-competitive, highly selective covalent inhibitor of wild-type and gatekeeper mutant FGFR4. FGFR4-IN-8 exhibits excellent potency against FGFR4, FGFR4 V550L, FGFR4 V550M and FGFR4 C552S with IC50s of 0.5, 0.25, 1.6, 931 nM, respectively. FGFR4-IN-8 exhibits potent antiproliferative activity against Hep3B hepatocellular carcinoma cells with the IC50 value of 29 nM. FGFR4-IN-8 demonstrates modest in vivo antitumor efficacy in nude mice bearing the Huh-7 xenograft model .
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-
- HY-N0976
-
|
11b-Hydroxy-11b,1-dihydromedicarpin
|
Interleukin Related
|
Inflammation/Immunology
|
|
1,11b-Dihydro-11b-hydroxymedicarpin (11b-Hydroxy-11b,1-dihydromedicarpin) is a pterocarpan from Ononis viscosa subsp. breviflora is a Medicarpin derivative . Medicarpin, a natural pterocarpan, heals cortical bone defect by activation of Notch and Wnt canonical signaling pathways . Medicarpin prevents arthritis in post-menopausal conditions by arresting the expansion of TH17 cells and pro-inflammatory cytokines. Medicarpin down-regulates pro-inflammatory cytokines like TNF-α, IL-6 and IL-17A, while up-regulates anti-inflammatory cytokine IL-10 in arthritis (CIA) model of mice .
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-
- HY-123929
-
|
|
MDM-2/p53
Wnt
IKK
Apoptosis
Caspase
|
Cancer
|
|
PAWI-2 is a p53-Activator and Wnt Inhibitor. PAWI-2 inhibits β3-KRAS signaling independent of KRAS. PAWI-2 selectively inhibits phosphorylation of TBK1. PAWI-2 activates apoptosis (activation of caspase-3/7), and induces PARP cleavage. PAWI-2 promotes optineurin translocation into the nucleus and causes G2/M arrest. PAWI-2 reverses cancer stemness and overcomes drug resistance in an integrin β3 KRAS-dependent human pancreatic cancer stem cells (hPCSCs). PAWI-2 inhibits growth of tumors from hPCSCs in orthopic xenograft mice model .
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-
- HY-118243
-
|
|
Others
|
Others
|
|
KMS88009 is a potent small molecule that directly interferes with the formation of amyloid-β oligomers, thereby preserving cognitive behavior when used preventively and reversing cognitive behavior decline when used therapeutically. Oral administration of KMS88009 around the onset of Alzheimer's disease symptoms significantly reduced the assembly of amyloid-β oligomers and improved cognitive behavior in the APP/PS1 double transgenic mouse model. This unique dual mode of action suggests that KMS88009 may be a powerful therapeutic candidate for the treatment of Alzheimer's disease. In an evaluation, the physicochemical properties, pharmacokinetics and toxicity of this anti-amyloidogenic small molecule KMS88009 were studied, as well as post-mortem analysis of APP/PS1 TG mice after behavioral testing.
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- 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-N6972
-
|
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine is a natural product that can be isolated from the plant Stephania cephalantha Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46 µM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
- 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-N6972R
-
|
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
Infection
Inflammation/Immunology
Cancer
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
- HY-125726
-
|
(3'-sulfo)Galβ-Cer(d18:1/24:1); N-Nervonoyl Sulfatide; C24:1 Sulfatide
|
Others
|
Inflammation/Immunology
|
|
Sulfo galactosylceramide (N-Nervonoyl Sulfatide; C24:1 Sulfatide) is a member of the sulfatide class of glycolipids. It is the predominate sulfatide species in mature myelin, and it accumulates at a higher rate than C24 3’-sulfo galactosylceramide in rat cerebellum from seven to 32 days of age when active myelination occurs. It interacts with C-type lectins and immunoglobulin-like receptors with the highest affinity for LMIR5. It induces production of MCP-1 in basophils but not mast cells and increases the activation of NFAT in a reporter assay via LMIR5. Sulfo galactosylceramide is an immunodominant species in myelin, is bound by CD1d in vitro, and increases proliferation in isolated mouse splenocytes. It reduces symptoms and increases survival in a mouse model of chronic relapsing-remitting experimental autoimmune encephalomyelitis (EAE) when used at a dose of 20 μg. It also decreases the number of inflammatory lesions and infiltrating mononuclear cells in the lumbar spinal cord of EAE mice. As this product is derived from a natural source, there may be variations in the sphingoid backbone.
|
-
- 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-B2167R
-
|
|
Endogenous Metabolite
|
Neurological Disease
Cancer
|
|
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-15096
-
|
FJ-776
|
Dyes
|
|
MKT-077 (FJ-776), a highly water-soluble mitochondrial dye, has significant antitumor activity . MKT-077 exhibits low cytotoxicity, and inhibits broad-spectrum human cancer cell lines (colon cancer, breast cancer, pancreatic cancer). MKT-077 inhibits the growth of tumor in nude mice enograft tumor model. Ex/Em=488/543 nm .
|
-
- HY-D2279
-
|
|
Fluorescent Dyes/Probes
|
|
NFL-NH2 is a mitochondrial-targeted near-infrared ratiometric fluorescent probe. NFL-NH2 can rapidly detect NO levels associated with the inflammatory damage degree in rheumatoid arthritis (RA) mice models by ratiometric fluorescence imaging. The excitation wavelength and emission wavelength are 650 nm and 780 nm, respectively .
|
-
- HY-16561G
-
|
trans-Resveratrol (GMP); SRT501 (GMP)
|
Fluorescent Dye
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
| Cat. No. |
Product Name |
Type |
-
- HY-16561G
-
|
trans-Resveratrol (GMP); SRT501 (GMP)
|
Biochemical Assay Reagents
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P5521
-
|
|
Peptides
|
Cardiovascular Disease
|
|
mLR12 is a Trem1 inhibitory peptide. mLR12 decreases aortic rupture rate in BAPN-induced Thoracic aortic aneurysm and dissection (TAAD) mice model .
|
-
- HY-P4094
-
CTP
1 Publications Verification
|
Peptides
|
Cardiovascular Disease
|
|
CTP is a cardiac targeting peptide. CTP transduces cardiomyocytes in vitro. CTP leads to efficient and specific transduction of heart tissue in mice model. CTP can be used to deliver therapeutic peptides, proteins and nucleic acid specifically to the heart .
|
-
- HY-P10136
-
|
human TREM-2 182-190
|
Peptides
|
Inflammation/Immunology
|
|
IA9 (human TREM-2 182-190) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model .
|
-
- HY-P10136A
-
|
human TREM-2 182-190 TFA
|
Peptides
|
Inflammation/Immunology
|
|
IA9 TFA (human TREM-2 182-190 TFA) is a TREM-2 inhibitor , and can diminish release of proinflammatory cytokines and dramatically suppressed joint inflammation and damage in collagen-Induced Arthritis (CIA) mice model .
|
-
- HY-105063
-
|
|
Peptides
|
Metabolic Disease
Inflammation/Immunology
|
|
DiaPep277 is a 24 amino acid peptide derived from positions 437-460 in HSP60. DiaPep277 arrests the progression of β-cell destruction in NOD mice. DiaPep277 has an immune modulatory effect on diabetogenic T cells in animal models of diabetes .
|
-
- HY-P5581
-
|
|
Peptides
|
Infection
Inflammation/Immunology
Cancer
|
|
Alloferon 1 is an antiviral and antitumoral peptide. Alloferon 1 stimulates natural cytotoxicity of human peripheral blood lymphocytes. Alloferon 1 also induces IFN synthesis, and enhances antiviral and antitumor resistance in mice. Alloferon 1 also shows anti-inflammatory activity in λ-carrageenan-induced paw edema model. Alloferon 1 can be isolated from the blood of the blow fly Calliphora vicina (Diptera) .
|
-
- HY-P4650
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Tyrosylhistidine is a dipeptide consisting of tyrosine and histidine (Tyr-His). Tyrosylhistidine is an orally active antihypertensive peptide. Tyrosylhistidine reduces blood pressure in mice in a model of spontaneous hypertension .
|
-
- 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-P10580
-
|
|
Tie
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Vasculotide, an angiopoietin-1 mimetic, is a Tie-2 activator and induces Tie-2 phosphorylation. Vasculotide has anti-inflammatiory effect and anti-permeability. Vasculotide ameliorates endotoxin-induced endothelial barrier dysfunction. Vasculotide promotes angiogenesis in a mouse model of diabetic ulcer. Vasculotide protects mice from vascular leakage and reduces mortality in murine abdominal sepsis. Vasculotide decreases microvascular leakage and improves microcirculatory perfusion in a rat model of hemorrhagic shock .
|
-
- HY-P10109A
-
|
hG6PI (325-339) (hydrochloride)
|
Peptides
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) hydrochloride is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) hydrochloride primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) hydrochloride induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
|
-
- HY-P10109
-
|
|
Peptides
|
Inflammation/Immunology
|
|
G6PI 325-339 (human) is an efficient inducer of arthritis in B10.Q mice. G6PI 325-339 (human) primes Th1 and Th17 cells cross-reacted with the murine G6PI protein. G6PI 325-339 (human) induces arthritis model operating through a T and B cell-dependent pathway but without antibody effector mechanisms .
|
-
- HY-P5875
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 ameliorates the injury in mice myocardial ischemia/reperfusion (I/R) models .
|
-
- HY-P5396
-
|
|
Peptides
|
Others
|
|
GAD65 (524-543) is a biological active peptide. (This is amino acids 524 to 543 fragment of glutamic acid decarboxylase 65 (GAD65). It is one of the first fragments of this islet antigen to induce proliferative T cell responses in the non-obese diabetic (NOD) mouse model of spontaneous autoimmune diabetes. This peptide is a specific, possibly low affinity, stimulus for the spontaneously arising diabetogenic T cell clone BDC2.5. Immunization with p524–543 increases the susceptibility of the NOD mice to type 1 diabetes induced by the adoptive transfer of BDC2.5 T cells.)
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99216
-
|
PF-04360365; RN 1219
|
EGFR
|
Neurological Disease
|
|
Ponezumab (PF-04360365) is a humanised anti-amyloid IgG2 monoclonal antibody. Ponezumab reduces Aβ levels in the central nervous system and improves performance in mice in various models of learning and memory. Ponezumab can be used in study of Alzheimer's disease .
|
-
- HY-P99922
-
|
|
Inhibitory Antibodies
|
Cancer
|
|
Encelimab is an anti-LAG3 antibody. Encelimab blocks the interaction between LAG-3 and MHC II, and enhances T-cell activation. Encelimab alone or in combination with an anti-PD-1 antibody reduces tumor size in a lymphoma mice model (A20 cell xenograft) .
|
-
- HY-P99583
-
|
MEDI4893
|
Bacterial
|
Infection
Inflammation/Immunology
|
|
Suvratoxumab (MEDI4893) is a long-acting, high-affinity human anti-α-toxin monoclonal antibody (IgG1κ type). Suvratoxumab potently neutralizes α-toxin, a key S. aureus virulence factor. Suvratoxumab improves survival and reduces lung injury in an immunocompromised mice model of pneumonia. Suvratoxumab also enhances the antibacterial activity of Vancomycin (HY-B0671) or Linezolid (HY-10394) .
|
-
- 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-125850
-
-
-
- HY-N0031
-
-
-
- HY-N3312
-
-
-
- HY-113354
-
-
-
- HY-66005
-
-
-
- HY-N1149
-
-
-
- HY-125850R
-
-
-
- HY-N0031R
-
-
-
- HY-N3312R
-
-
-
- HY-N11872
-
-
-
- HY-N0088
-
-
-
- HY-126477
-
-
-
- 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-N0088R
-
-
-
- HY-126477R
-
-
-
- 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-B1350A
-
-
-
- HY-N1420
-
-
-
- HY-116330
-
-
-
- HY-16561
-
Resveratrol
Maximum Cited Publications
87 Publications Verification
trans-Resveratrol; SRT501
|
Structural Classification
Classification of Application Fields
Anti-aging
Source classification
Vitis vinifera cv. Zalema
Plants
Vitaceae
Infection
Microorganisms
Functional Molecules
Sunscreen
Research of Health Products
Phenols
Polyphenols
Cosmetic Research
Inflammation/Immunology
Disease Research Fields
Cancer
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
|
Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
-
- HY-116330A
-
|
Hyperforin DCHA
|
Structural Classification
Natural Products
Guttiferae
Source classification
Hyperlcurn perforatum L.
Plants
|
TRP Channel
Calcium Channel
|
|
Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
|
-
-
- HY-P99744
-
|
TAK-573
|
Classification of Application Fields
Disease Research Fields
Cancer
|
CD38
|
|
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 .
|
-
-
- HY-16561R
-
|
trans-Resveratrol (Standard); SRT501 (Standard)
|
Infection
Functional Molecules
Classification of Application Fields
Sunscreen
Anti-aging
Source classification
Research of Health Products
Cosmetic Research
Plants
Inflammation/Immunology
Disease Research Fields
Cancer
|
IKK
Autophagy
Mitophagy
Sirtuin
Apoptosis
Bacterial
Fungal
Antibiotic
Keap1-Nrf2
|
|
Resveratrol (Standard) is the analytical standard of Resveratrol. This product is intended for research and analytical applications. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator . Resveratrol is a potent pregnane X receptor (PXR) inhibitor . Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model . Resveratrol increases production of NO in endothelial cells .
|
-
-
- HY-116330AR
-
|
|
Structural Classification
Natural Products
Guttiferae
Source classification
Hyperlcurn perforatum L.
Plants
|
TRP Channel
Calcium Channel
|
|
Hyperforin (dicyclohexylammonium salt) (Standard) is the analytical standard of Hyperforin (dicyclohexylammonium salt). This product is intended for research and analytical applications. Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca2+ levels by activating Ca2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt also shows diverse pharmacological activities including anti-depression, anti-tumor, anti-dementia, anti-diabetes. Hyperforin dicyclohexylammonium salt modulates γδ T cells to secret IL-17α, improves Imiquimod (HY-B0180)-induced psoriasis-like mice model .
|
-
-
- HY-N0976
-
-
-
- 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-N6972
-
-
-
- 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 .
|
-
-
- HY-N6972R
-
|
|
Structural Classification
Alkaloids
Stephania cepharantha Hayata
Plants
Isoquinoline Alkaloids
Menispermaceae
Stephania japonica (Thunb.) Miers
|
Autophagy
SARS-CoV
Cytochrome P450
Apoptosis
Parasite
|
|
Cepharanthine (Standard) is the analytical standard of Cepharanthine. This product is intended for research and analytical applications. Cepharanthine is a natural product that can be isolated from the plant Stephania?cephalantha?Hayata. Cepharanthine has anti-severe acute respiratory syndrome coronavirus 2 (anti-SARS-CoV-2) activities. Cepharanthine has good effective in suppressing viral proliferation (half maximal (50%) inhibitory concentration (IC50) and 90% inhibitory concentration (IC90) values of 1.90 and 4.46?μM . Cepharanthine can also effectively reverses P-gp-mediated multidrug resistance in K562 cells and increase enhances the sensitivity of anticancer agents in xenograft mice model . Cepharanthine shows inhibitory effects of human liver cytochrome P450 enzymes CYP3A4, CYP2E1 and CYP2C9. Cepharanthine has antitumor, anti-inflammatory and antinociceptive effects .
|
-
-
- 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-B2167R
-
|
|
Structural Classification
Human Gut Microbiota Metabolites
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Disease markers
Endogenous metabolite
Cardiovascular System Disorder
|
Endogenous Metabolite
|
|
Docosahexaenoic acid (Standard) is the analytical standard of Docosahexaenoic acid. This product is intended for research and analytical applications. Docosahexaenoic Acid (DHA) is an omega-3 fatty acid abundantly present brain and retina. It can be obtained directly from fish oil and maternal milk.
In Vitro: Docosahexaenoic acid (DHA) is essential for the growth and functional development of the brain in infants. DHA is also required for maintenance of normal brain function in adults. The inclusion of plentiful DHA in the diet improves learning ability and memory . DHA is an essential requirement in every step of brain development like neural cell proliferation, migration, differentiation, synaptogenesis. The multiple double bonds and unique structure allow DHA to impart special membrane characteristics for effective cell signaling. Many development disorders like dyslexia, autism spectrum disorder, attention deficit hyperactivity disorder, schizophrenia etc. are causally related to decreased level of DHA . DHA is a potent RXR ligand inducing robust RXR activation already at low micro molar concentrations. The EC50 for RXRα activation by DHA is about 5-10 μM fatty acid .
In Vivo: Docosahexaenoic acid administration over 10 weeks significantly reduces the number of reference memory errors, without affecting the number of working memory errors, and significantly increases the docosahexaenoic acid content and the docosahexaenoic acid/arachidonic acid ratio in both the hippocampus and the cerebral cortex . DHA treatment exerts neuroprotective actions on an experimental mouse model of PD. There is a decrease tendency in brain lipid oxidation of MPTP mice but it does not significantly .
|
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-113354S
-
|
|
|
Anserine-d4 is the deuterium labeled Anserine. Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice[1][2].
|
-
-
- HY-16561S
-
|
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Resveratrol-d4 is the deuterium labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
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- HY-109120S
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Odevixibat-d5 is deuterated labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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- HY-109120S1
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Odevixibat- 13C6 is 13C labeled Odevixibat (HY-109120). Odevixibat (A4250) is a selective and orally active ileal apical sodium-dependent bile acid transporter (ASBT) inhibitor. Odevixibat decreases cholestatic liver and bile duct injury in mice model. Odevixibat has the potential for the treatment of primary biliary cirrhosis .
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- HY-113354S1
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Anserine-d4 hydrochloride is the deuterium labeled Anserine (HY-113354). Anserine, a methylated form of Carnosine, is an orally active, natural Histidine-containing dipeptide found in skeletal muscle of vertebrates. Anserine is not cleaved by serum carnosinase and act as biochemical buffers, chelators, antioxidants, and anti-glycation agents. Anserine improves memory functions in Alzheimer's disease (AD)-model mice .
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- HY-16561S1
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Resveratrol- 13C6 is the 13C-labeled Resveratrol. Resveratrol (trans-Resveratrol; SRT501), a natural polyphenolic phytoalexin that possesses anti-oxidant, anti-inflammatory, cardioprotective, and anti-cancer properties. Resveratrol (SRT 501) has a wide spectrum of targets including mTOR, JAK, β-amyloid, Adenylyl cyclase, IKKβ, DNA polymerase. Resveratrol also is a specific SIRT1 activator[1][2][3][4]. Resveratrol is a potent pregnane X receptor (PXR) inhibitor[5]. Resveratrol is an Nrf2 activator, ameliorates aging-related progressive renal injury in mice model[6]. Resveratrol increases production of NO in endothelial cells[7].
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- HY-154974
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Cationic Lipids
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LNP Lipid-8 (11-A-M) is an ionizable lipid, which can be used for lipid nanoparticles (LNP) to deliver siRNA to T cells without targeting to ligands. LNP LIPs-8 loaded with GFP siRNA (siGFP), and significantly causes GFP gene silencing in mice model .
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- HY-153808
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Adjuvant
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Complete Freund's adjuvant (CFA) is an immunoadjuvant emulsified with antigen by its discoverer Jules T. Freund to enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA) stimulates a strong and durable immune response and can be used to induce persistent inflammatory pain models in mice, experimental autoimmune myocarditis (EAM) models, and more. Incomplete Freund's adjuvant (IFA) (HY-153808A) is another type of Freund's Adjuvant that stimulates a weaker immune response .
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- HY-153834
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Aptamers
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GTI-2040, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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- HY-153834A
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Aptamers
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GTI-2040 sodium, a 20-mer phosphorothioate oligonucleotide, was designed to hybridize to the mRNA sequence of human ribonucleotide reductase R2. GTI-2040 sodium has been shown to inhibit human cancer cell proliferation by downregulation of R2 expression in vitro and to significantly inhibit tumor growth in xenograft models of human cancer in mice.
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