Search Result
Results for "
active substrate
" in MedChemExpress (MCE) Product Catalog:
12
Biochemical Assay Reagents
13
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-108666
-
|
Adenosine-5'-O-3-thiotriphosphate tetralithium salt; Adenosine 5'-[γ-thio]triphosphate tetralithium salt
|
Eukaryotic Initiation Factor (eIF)
P2Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
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ATPγS (tetralithium salt) is a P2Y11 receptor agonist, an antioxidant and a neuroprotective agent. ATPγS (tetralithium salt) can be used as a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A. ATPγS (tetralithium salt) is active in ATP hydrolysis .
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-
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- HY-162001
-
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CDK
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Cancer
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INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research .
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- HY-B0804
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Nadolol
5 Publications Verification
SQ-11725
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Adrenergic Receptor
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Cardiovascular Disease
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Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research .
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- HY-W012241
-
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Endogenous Metabolite
PROTAC Linkers
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Metabolic Disease
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Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
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-
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- HY-105124A
-
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Ro 3-4787 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
Endocrinology
|
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Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
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-
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- HY-105124
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-
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- HY-W012145
-
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Others
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Metabolic Disease
|
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TMPD dihydrochloride, a readily oxidizable compound, is an enzymatically convert redox active substrate molecule. TMPD dihydrochloride is also an electron donor and serves as a reducing cosubstrate for heme peroxidases . TMPD dihydrochloride is also a complex IV substrate .
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-
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- HY-111338
-
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Cholinesterase (ChE)
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Neurological Disease
|
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Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .
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- HY-W011834
-
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HCV
DNA/RNA Synthesis
|
Infection
|
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2'-O-Methylcytidine is an orally active 2'-substituted nucleoside as a inhibitor of HCV replication with antiviral activity. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
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- HY-19593
-
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Fungal
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Infection
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Nikkomycin Z is a nucleoside peptide and an orally active antifungal agent. Nikkomycin Z inhibits chitin synthesis by acting as a competitive analogue of the chitin synthase substrate UDP-N-acetylglucosamine. Nikkomycin Z has antifungal activity .
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- HY-113362
-
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Antibiotic
Bacterial
Fungal
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Infection
|
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Petroselinic acid, a positional isomer of oleic acid, is isolated from the vegetable oil of Coriandrum sativum fruits. Petroselinic acid is used as substrate for sophorolipid fermentation. Petroselinic acid inhibits the biofilm formation in microorganisms, exhibits antibacterial and antifungal activities. Petroselinic acid is orally active [4.
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-
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- HY-120111
-
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MW01-18-150SRM
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
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MW150 (MW01-18-150SRM) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
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- HY-107597
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Halicin
2 Publications Verification
SU3327
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JNK
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Metabolic Disease
Inflammation/Immunology
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Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt kinase .
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- HY-A0279A
-
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Mikamycin B; Mikamycin IA
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Bacterial
Antibiotic
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Infection
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Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus .
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- HY-113335
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Coprocholic acid
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Endogenous Metabolite
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Inflammation/Immunology
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Trihydroxycholestanoic acid is an endogenous metabolite present in Blood that can be used for the research of Zellweger Syndrome, Refsum Disease, D Bifunctional Protein Deficiency and Infantile Refsum Disease .
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- HY-N7136
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-
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- HY-15779A
-
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SphK
Apoptosis
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Cancer
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K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity .
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- HY-P10605
-
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Akt
GSK-3
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Cancer
|
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GSK3β-peptide is a substrate mimetic peptide of glycogen synthase kinase 3-β (GSK3-β) that can bind to the active site of GSK3-β and mimic the behavior of a real substrate. GSK3β-peptide can be used to develop substrate mimetic inhibitors of Akt as potential anticancer drugs .
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- HY-128878
-
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Cholecystokinin Receptor
P-glycoprotein
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Metabolic Disease
Endocrinology
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Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .
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- HY-135867E
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CHIKV
Endogenous Metabolite
Enterovirus
HCV
Topoisomerase
SARS-CoV
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Infection
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NHC-triphosphate tetraammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form . NHC-triphosphate tetraammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA .
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- HY-D1686
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Biotin-16-UTP tetralithium
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DNA Stain
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Others
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Biotin-16-UTP is an active substrate for RNA polymerase. Biotin-16-UTP can replace UTP in the in vitro transcription reaction for RNA labeling .
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- HY-P5376
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S-2586
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Ser/Thr Protease
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Others
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MeOSuc-Arg-Pro-Tyr-pNA (S-2586) is a biological active peptide. (chymotrypsin substrate)
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-
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- HY-122439
-
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Mevinolinic acid; MSD803
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HMG-CoA Reductase (HMGCR)
Drug Metabolite
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Metabolic Disease
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Lovastatin acid (Mevinolinic acid; MSD803), an active metabolite of Lovastatin (HY-N0504), is a potent competitive HMG-CoA reductase inhibitor with a Ki of 0.6 nM. Lovastatin acid acts as a competitive inhibitor with respect to substrate HMG-CoA, interfering cholesterol synthesis. Lovastatin acid can be used for the research of hypercholesterolemia .
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- HY-119101
-
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CCR
Potassium Channel
P-glycoprotein
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Inflammation/Immunology
|
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AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis .
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- HY-P5432
-
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IRAK-1 (360-380)
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IRAK
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Others
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IRAK-4 Peptide substrate (IRAK-1 (360-380)) is a biological active peptide. (This is a substrate peptide for Interleukin-1 Receptor-Associated Kinase (IRAK) 4)
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- HY-P10042
-
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Ribosomal S6 Kinase (RSK)
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Others
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S6K Substrate is a substrate for active protein kinases, including CLK2, MRCKalpha, MRCKbeta, p70S6K, ROCK1, ROCK2, RSK1, RSK3, PIM1 .
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- HY-P5426
-
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Bcr-Abl
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Others
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Abl protein tyrosine kinase substrate is a biological active peptide. (Abltide is a peptide substrate for Abl Kinase (Abl protein tyrosine kinase), a partner in the gag-Abl fusion protein of the Abelson murine leukemia virus. Used in Western blot and kinase assay.)
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- HY-P5430
-
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DYRK
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Others
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DYRKtide is a biological active peptide. (Dyrktide is designed as the optimal substrate sequence efficiently phosphorylated by DYRK1A, which is a dual-specificity protein kinase that is thought to be involved in brain development.)
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- HY-134423S
-
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Isotope-Labeled Compounds
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Others
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Stearoyl coenzyme A- 13C18 (lithium) is the 13C labeled Stearoyl coenzyme A lithium . Stearoyl coenzyme A (Stearoyl-CoA) lithium is an active compound that can be used as a substrate for the determination of stearoyl-Coenzyme desaturase in microsomes .
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- HY-122661
-
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MPH
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PARP
Apoptosis
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Cancer
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Mefuparib hydrochloride (MPH) is an orally active, substrate-competitive and selective PARP1/2 inhibitor with IC50s of 3.2 nM and 1.9 nM, respectively. Mefuparib hydrochloride induces apoptosis and possesses prominent anticancer activity in vitro and in vivo .
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- HY-D1584
-
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Phospholipase
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Others
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C12 NBD sphingomyelin is an active derivative of Sphingomyelin (HY-113498) that is tagged with fluorescent C12 nitrobenzoxadiazole (C12 NBD). C12 NBD sphingomyelin can be used as a sphingomyelinase substrate for studying the metabolism and transport of sphingomyelins (Ex=470 nm, Em=525 nm) .
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- HY-W017445
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Fungal
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Infection
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Homogentisic acid lactone (Compound 1) is a fungal metabolite with fungicidal activity, which is found in the fungus WF5. Homogentisic acid lactone is active against the plant pathogenic fungus F. graminearum. Homogentisic acid lactone can be used as a substrate in the determination of serum paraoxonase/arylesterase 1 (PON1) activity .
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- HY-D1686B
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DNA Stain
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Others
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Biotin-16-UTP tetrasodium is an active substrate for RNA polymerase. Biotin-16-UTP tetrasodium can replace UTP in the in vitro transcription reaction for RNA labeling .
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- HY-P0320
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Phosphatase
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Others
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EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
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- HY-P5431
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Insulin Receptor
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Others
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Insulin receptor (1142-1153), pTyr1150 is a biological active peptide. (Peptide used as insulin receptor tyrosine kinase substrate.)
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- HY-167805
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Biochemical Assay Reagents
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D-Glucose 6-phosphate potassium is a biologically active compound that has the activity of being a substrate for glucose-6-phosphate isomerase. D-Glucose 6-phosphate potassium can participate in the sugar metabolism process and promote the production and utilization of energy in cells.
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- HY-16137
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Cephaloglycin
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Bacterial
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Infection
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Cefaloglycin (Cephaloglycin) is an orally active nephrotoxic β-lactam cephalosporin antibiotic with antibacterial activity. Cefaloglycin is activity against Gram-Positive cocci other than enterococci. Cefaloglycin is toxic to mitochondrial substrate uptake and respiration .
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- HY-116750
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Tyrosinase
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Others
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6-Hydroxykaempferol, a flavonoid, is a competitive tyrosinase inhibitor with an IC50 value of 124 μM. 6-Hydroxykaempferol has a Ki value of 148 μM relative to L-DOPA as a substrate and effectively inhibits the activity of the enzyme by binding to the active site of the enzyme .
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- HY-135867
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- HY-134361
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- HY-P5450
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PDK-1
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Others
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PDKtide, a biological active peptide is a substrate for Phosphatidylinositide-Dependent Kinase 1 (PDK1) .
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- HY-P3477
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Fluorescent Dye
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Others
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Mca-PLA-Nva-Dap(Dnp)-AR-NH2 is a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) .
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- HY-P5450A
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PDK-1
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Others
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PDKtide TFA, a biological active peptide, is a substrate for phosphatidylinositide-dependent kinase 1 (PDK1) .
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- HY-137834A
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- HY-P5374
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Elastase
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Others
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MeOSuc-AAPV-AFC is a biological active peptide. (A highly specific neutrophil elastase substrate, Abs/Em=380/500 nm.)
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- HY-P5355
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Fluorescent Dye
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Others
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Z-Gly-Gly-Arg-AFC is a biological active peptide. (Plasminogen Activator Acrosine Substrate, fluorescent Z-Gly-Gly-Arg-AFC)
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- HY-116188
-
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Others
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Inflammation/Immunology
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HX1 is a potent reversible myeloperoxidase (MPO) inhibitor with an IC50 value of 50 nM. HX1 is bound within the active site cavity above the heme and blocks the substrate channel. HX1 is promising for research of inflammatory diseases .
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- HY-W002801
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Biochemical Assay Reagents
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Others
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2-Benzyloxyphenylboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research. 2-Benzyloxyphenylboronic acid is also a substrate used in asymmetric Suzuki coupling reactions. 2-Benzyloxyphenylboronic acid can be utilized in the synthesis of other active compounds .
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- HY-15779
-
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SphK
Apoptosis
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Cancer
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K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity .
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- HY-D1575
-
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Fluorescent Dye
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Others
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C6 NBD galactosylceramide is an active derivative of galactosylceramide that is tagged with fluorescent C6 nitrobenzoxadiazole (C6 NBD). C6 NBD galactosylceramide can be used as a substrate for neutral β-glycosylceramidase (GCase) to study intracellular localization and metabolism of galactosylceramide (Ex=nm, Em=525) .
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- HY-P0266B
-
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Ac-SdKP acetate
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Angiotensin-converting Enzyme (ACE)
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Inflammation/Immunology
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N-Acetyl-Ser-dAsp-Lys-Pro (Ac-SdKP) acetate is a specific substrate for the N-terminal active site of angiotensin-converting enzyme (ACE). N-Acetyl-Ser-dAsp-Lys-Pro acetate is a natural inhibitor of pluripotent hematopoietic stem cell proliferation. Anti-inflammatory and antifibrotic properties .
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- HY-135867A
-
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CHIKV
Endogenous Metabolite
Enterovirus
HCV
Topoisomerase
|
Infection
|
|
NHC-triphosphate tetrasodium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a triphosphate form . NHC-triphosphate tetrasodium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA .
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- HY-P5434
-
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JAK3 Peptide substrate
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JAK
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Others
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Jak3tide (JAK3 Peptide substrate) is a biological active peptide. (This peptide is a substrate for Jak3. It may be used used in kinase assays. Jak3tide contains the phosphorylation site at Tyr7.)
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- HY-P10042A
-
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Ribosomal S6 Kinase (RSK)
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Others
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S6K Substrate acetate is a substrate for active protein kinases, including CLK2, MRCKalpha, MRCKbeta, p70S6K, ROCK1, ROCK2, RSK1, RSK3, PIM1 .
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- HY-P1906
-
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CDK
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Neurological Disease
|
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[pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM .
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![[pThr3]-CDK5 Substrate](//file.medchemexpress.com/product_pic/hy-p1906.gif)
- HY-P5440
-
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ERK
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Others
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ERKtide is a biological active peptide. (ERKtide is a peptide substrate for ERK2. Extracellular regulated protein kinase 2 (ERK2) is a eukaryotic protein kinase whose activity is regulated by mitogenic stimuli.)
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- HY-135867F
-
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CHIKV
Endogenous Metabolite
Enterovirus
HCV
Topoisomerase
SARS-CoV
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Infection
|
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NHC-diphosphate triammonium is an active phosphorylated intracellular metabolite of β-d-N4-Hydroxycytidine (NHC) (HY-125033) as a diphosphate form . NHC-diphosphate triammonium is a weak alternative substrate for the viral polymerase and can be incorporated into HCV replicon RNA .
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- HY-P5377
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Cathepsin K substrate
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Ser/Thr Protease
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Others
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Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
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- HY-134423
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Stearoyl-CoA lithium
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Biochemical Assay Reagents
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Others
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Stearoyl coenzyme A (Stearoyl-CoA) lithium is an active compound that can be used as a substrate for the determination of stearoyl-Coenzyme desaturase in microsomes .
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- HY-N7263
-
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Cholinesterase (ChE)
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Neurological Disease
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Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes .
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- HY-P5447
-
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Phosphatase
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Others
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RRLIEDAEpYAARG is a biological active peptide. (Phosphatase substrate.)
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- HY-P5449
-
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- HY-P5428
-
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CDK
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Others
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Cdc2 kinase substrate is a biological active peptide. (The native peptide HATPPKKKRK is a substrate for cyclin-dependent protein kinase 1 (CDC2; CDK1).)
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- HY-P0320B
-
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Phosphatase
Biochemical Assay Reagents
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Others
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EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
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- HY-P0320A
-
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Phosphatase
Biochemical Assay Reagents
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Others
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EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
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- HY-P5385
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Angiotensin Receptor
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Others
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Renin substrate, angiotensinogen (1-14), rat is a biological active peptide. (This peptide is derived from rat angiotensinogen amino acid residues 1-14. It is a synthetic renin substrate.)
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- HY-P5386
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- HY-P5456
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PKC
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Others
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KRPpSQRHGSKY-NH2 is a biological active peptide. (This is a phosphorylated PKC substrate peptide)
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- HY-P5433F
-
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Insulin Receptor
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Others
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IRS-1 Peptide, FAM labeled is a biological active peptide. (Insulin receptor substrate)
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- HY-P3476
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Fluorescent Dye
Caspase
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Cancer
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Mca-VDQVDGW-Lys(Dnp)-NH2 is a fluorogenic substrate of caspase-7. Mca-VDQVDGW-K(Dnp)-NH2 can be used to quantify caspase-7 activity.
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- HY-P5467
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ROCK
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Others
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S6(229-239), Amide, biotinalyted is a biological active peptide. (substrate for Rho-Kinase II)
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- HY-P1906A
-
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CDK
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Neurological Disease
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[pThr3]-CDK5 Substrate TFA is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM .
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![[pThr3]-CDK5 Substrate TFA](//file.medchemexpress.com/product_pic/hy-p1906a.gif)
- HY-P4891
-
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Angiotensin Receptor
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Others
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Angiotensin (1-12) (human) is an endogenous substrate for the production of biologically active angiotensin peptides by a non-renin-dependent mechanism .
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- HY-114599
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Endogenous Metabolite
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Others
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8-iso Prostaglandin A1 is an active substrate for Arabidopsis thaliana OPR3 (AtOPR3), with a KM of 22 μM .
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- HY-P5526
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Casein Kinase
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Others
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CCK1-specific peptide substrate is a biological active peptide. (This peptide sequence is based on rabbit muscle glycogen synthase with Ser7 phosphorylated. It is a peptide substrate for Casein Kinase I (CK1). CK1 phosphorylates Ser10. Ser7 is phosphorylated by PKA in vivo.)
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- HY-153859
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Biochemical Assay Reagents
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Others
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Ser-SNAC TFA is a small-molecule substrate for NRPS C domains. As for NRPSs, refers to nonribosomal peptide synthetases, are large multidomain proteins to catalyze the formation of biologically active natural products. Ser-SNAC TFA can be used for characterizing the substrate specificity of C domain-catalyzed peptide bond formation .
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- HY-P2716
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MMP
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Others
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Mca-Arg-Pro-Lys-Pro-Tyr-Ala-Nva-Trp-Met-Lys(Dnp)-NH2 is a biological active peptide. (MMP substrate)
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- HY-W283888
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Biochemical Assay Reagents
β-glucuronidase
|
Others
|
|
5-Bromo-4-chloro-1H-indol-3-yl nonanoate is a fluorescent substrate used to detect enzymes. The substrate reacts with various enzymes to produce a fluorescent product, which has been shown to be active against β-galactosidase, α-chymotrypsin, and β-glucuronidase.
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-
- HY-128878R
-
|
|
Cholecystokinin Receptor
P-glycoprotein
Reference Standards
|
Metabolic Disease
Endocrinology
|
|
Dexloxiglumide (Standard) is the analytical standard of Dexloxiglumide. This product is intended for research and analytical applications. Dexloxiglumide is an orally active and selective cholecystokinin type A (CCKA) receptor antagonist. Dexloxiglumide is the active enantiomer of Loxiglumide, inhibits smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8). Dexloxiglumide exhibits moderate Caco-2 permeability that is polarized, concentration dependent, and pH dependent. Dexloxiglumide increases MRP1-substrate fluorescein uptake. Dexloxiglumide can be studied in research for gastrointestinal diseases and tumors .
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-
- HY-P5356
-
|
Plasmin substrate
|
Fluorescent Dye
|
Others
|
|
H-D-Val-Leu-Lys-AFC (Plasmin substrate) is a biological active peptide. (This is a fluorescent plasmin substrate, Abs/Em=380/500 nm.Plasmin belongs to the family of serine proteases. It plays a key role in fibrinolysis by dissolving fibrin in blood clots. Besides fibrinolysis, plasmin is also involved in such physiological and pathological processes as wound healing, liver repair, and the maintenance of liver homeostasis.)
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-
- HY-P5415
-
|
|
HIV
|
Others
|
|
DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is a biological active peptide. (DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is also called HIV protease substrate I in some literature. It is widely used for the continuous assay for HIV protease activity. The 11-Kd protease (PR) encoded by the human immunodeficiency virus 1 (HIV-1) is essential for the correct processing of viral polyproteins and the maturation of infectious virus, and is therefore a target for the design of selective acquired immunodeficiency syndrome (AIDS) therapeutics. The FRET-based fluorogenic substrate is derived from a natural processing site for HIV-1 PR. Incubation of recombinant HIV-1 PR with the fluorogenic substrate resulted in specific cleavage at the Tyr-Pro bond and a time-dependent increase in fluorescence intensity that is linearly related to the extent of substrate hydrolysis. The fluorescence quantum yields of the HIV-1 PR substrate in the FRET assay increased by 40.0- and 34.4-fold, respectively, per mole of substrate cleaved. Because of its simplicity and precision in the determination of reaction rates required for kinetic analysis, this substrate offers many advantages over the commonly used HPLC or electrophoresis-based assays for peptide substrate hydrolysis by retroviral PRs. Abs/Em = 340nm/490nm.)
|
-
- HY-E70798
-
|
|
ERK
|
Cancer
|
|
ERK2 is a serine/threonine-specific protein kinase capable of phosphorylating multiple protein substrates within a cell. Biotin-ERK2 Recombinant Human Active Protein Kinase is obtained by expressing ERK2 proteins and is biotinylated .
|
-
- HY-105124AR
-
|
Ro 3-4787 hydrochloride (Standard)
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Bufuralol (hydrochloride) (Standard) is the analytical standard of Bufuralol (hydrochloride). This product is intended for research and analytical applications. Bufuralol (Ro 3-4787) hydrochloride is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
|
-
- HY-P10808
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
RSRGVFF (FOXP3 inhibitor P60) is a mixed-type angiotensin-converting enzyme (ACE) inhibitor with blood-brain barrier permeability, boasting an IC50 value of 5.01 μM . RSRGVFF is capable of binding to both active and non-active sites of ACE and its substrate HHL complex, thus reducing the catalytic activity of ACE. RSRGVFF can be further utilized for research on lowering hypertension .
|
-
- HY-A0279AR
-
|
Mikamycin B (Standard); Mikamycin IA (Standard)
|
Reference Standards
Bacterial
Antibiotic
|
Infection
|
|
Pristinamycin IA (Standard) is the analytical standard of Pristinamycin IA. This product is intended for research and analytical applications. Pristinamycin IA (Mikamycin B) is a cycle-peptidic macrolactone antibiotic. Pristinamycin IA is a substrate of P-glycoprotein and inhibits its function. Pristinamycin IA is active against StaphyloEoccus and Srreptococcus[1].
|
-
- HY-P5323
-
|
|
Bacterial
|
Others
|
|
Dabcyl-AGHDAHASET-Edans is a biological active peptide. (This is a type I signal peptidase (SPase1) substrate peptide labeled with EDANS/ DABCYL FRET pair, and contains a crucial cleavage site derived from the C-terminal region of the Staphylococcus epidermidis pre-SceD protein. Abs/Em = 340/490 nm.)
|
-
- HY-137854
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Naphthol AS-BI N-acetyl-β-D-glucosaminide acts as a substrate and reacts directly with N-acetyl-β-glucosaminidase enzyme. Naphthol AS-BI N-acetyl-β-D-glucosaminide can detect and localize the active region of N-acetyl-β-glucosaminidase enzyme visually .
|
-
- HY-B2072AR
-
|
|
Reference Standards
Antibiotic
Bacterial
|
Infection
|
|
Cefadroxil (hydrate) (Standard) is the analytical standard of Cefadroxil (hydrate). This product is intended for research and analytical applications. Cefadroxil hydrate (BL-S 578 hydrate) is an orally active and first-generation cephalosporin with a broad spectrum antibacterial activity. Cefadroxil hydrate (BL-S 578 hydrate) also acts as a substrate of the peptide transporter PEPT1 and PEPT2 .
|
-
- HY-105470
-
|
|
Bacterial
|
Infection
|
|
BMY-28271 is an orally active cephalosporin. BMY-28271 has a widely expanded spectrum with high activity against gram-positive and gram-negative bacteria. BMY-28271 is a poor substrate for various beta-lactamases. BMY-28271 can be used for the research of infection .
|
-
- HY-110196
-
|
|
Histone Methyltransferase
|
Others
|
|
(S)-PFI-2 hydrochloride is an inhibitor of lysine methyltransferase SETD7 and is approximately 500-fold more active than its enantiomer (R)-PFI-2. (R)-PFI-2 is a cofactor-dependent and substrate-competitive inhibitor. (R)-PFI-2 can occupy the substrate peptide binding groove of SETD7 (including the catalytic lysine binding channel) and interact with the cofactor The donor methyl group is in direct contact. However, (S)-PFI-2 was not observed to have the same interaction as (R)-PFI-2 .
|
-
- HY-143903
-
|
|
PIN1
|
Cancer
|
|
ZL-Pin13 is a high potent cell-active covalent inhibitor targeting the Pin1 (Peptidyl-Prolyl Isomerase NIMA-Interacting-1) with an IC50 of 67 nM. ZL-Pin13 effectively inhibits the proliferation and downregulated the Pin1 substrates in MDA-MB-231 cells .
|
-
- HY-134136
-
|
|
Endogenous Metabolite
|
Others
|
|
Octanoyl coenzyme A is an enoyl-CoA hydratase binder. Octanoyl coenzyme A binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
|
-
- HY-170569
-
|
|
Dipeptidyl Peptidase
Cytochrome P450
P-glycoprotein
|
Metabolic Disease
|
|
Cetagliptin is an orally active inhibitor for dipeptidyl peptidase 4 (DPP-4) and CYP2D6 (IC50 of 6 µM). Cetagliptin is a substrate for P-glycoprotein. Cetagliptin reduces the GLP-1 degradation, maintains the level of postprandial blood sugar, and can be used in type 2 diabetes mellitus research .
|
-
- HY-P2820D
-
|
|
Biochemical Assay Reagents
|
Others
|
|
β-Phosphoglucomutase (EC 5.4.2.6) requires Mg2+ and phosphorylation of an aspartate residue at the active site. The enzyme is able to autophosphorylate itself with its substrate β-D-glucose 1-phosphate.
|
-
- HY-E70933
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Protease, Streptomyces griseus, exhibits broad substrate specificity. Its active site consists of one aspartic acid residue, one histidine residue, and one serine residue. Protease tends to hydrolyze the peptide bond on the carboxyl side of glutamate or aspartate.
|
-
- HY-181175
-
|
|
Glycosidase
|
Metabolic Disease
|
|
OMJ-4 is a mutant alpha-mannosidase modulator. OMJ-4 can restore mutant alpha-mannosidase's catalytic function, and induces changes in compactness and active-site flexibility to improve substrate accommodation. OMJ-4 acts as an inducer of substrate reactivity, increasing the reactivity of mannose disaccharide bound to mutant alpha-mannosidase. OMJ-4 reduces the activation energy required for the enzymatic reaction of mutant alpha-mannosidase. OMJ-4 can be used for the research of alpha-mannosidosis .
|
-
- HY-E71248
-
|
|
Biochemical Assay Reagents
|
Others
|
|
α-Rhamnosidase 78A, Streptomyces avermitilis (EC 3.2.1.40) is a thermostable Alpha-L-Rhamnosidase (Naringinase, RhamA) that catalyzes the cleavage of the bond between terminal L (+)-rhamnose and the aglycone of rhamnose-containing glycosides. The enzyme is very active on naringin but has also substantial activity with hesperidin as substrate.
|
-
- HY-105560
-
|
|
Bacterial
Beta-lactamase
|
Infection
|
|
Cefcanel is an orally active cephalosporin and antibacterial agent. Cefcanel inhibits growth of methicillin-susceptible Staphylococcus aureus, methicillin-susceptible Staphylococcus epidermidis, Haemophilus influenzae, Moraxella catarrhalis. Cefcanel acts as a substrate hydrolyzed by TEM-1, TEM-3, and Moraxella Bro-1 beta-lactamases .
|
-
- HY-N9440
-
|
|
Drug Metabolite
|
Inflammation/Immunology
Cancer
|
|
7-Hydroxycoumarin glucuronide is a transport substrate and main human coumarin metabolite. 7-Hydroxycoumarin glucuronide undergoes ATP-dependent efflux transport via MRP3 and MRP4. 7-Hydroxycoumarin glucuronide undergoes active transport processes for urinary excretion and is primarily excreted into urine in humans.
|
-
- HY-105124R
-
|
Ro 3-4787 (Standard)
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Bufuralol (Standard) is the analytical standard of Bufuralol (HY-105124). This product is intended for research and analytical applications. Bufuralol (Ro 3-4787) is a potent non-selective, orally active β-adrenoreceptor antagonist with partial agonist activity. Bufuralol hydrochloride is a CYP2D6 probe substrate .
|
-
- HY-113362R
-
|
|
Reference Standards
Antibiotic
Bacterial
Fungal
|
Infection
|
|
Petroselinic acid (Standard) is the analytical standard of Petroselinic acid. This product is intended for research and analytical applications. Petroselinic acid, a positional isomer of oleic acid, is isolated from the vegetable oil of Coriandrum sativum fruits. Petroselinic acid is used as substrate for sophorolipid fermentation. Petroselinic acid inhibits the biofilm formation in microorganisms, exhibits antibacterial and antifungal activities. Petroselinic acid is orally active [4.
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-
- HY-P5435
-
|
|
Ser/Thr Kinase
|
Others
|
|
LKBtide is a biological active peptide. (This is a peptide substrate that is phosphorylated by Serine/Threonine kinase 11 (STK11), also known as LKB1. LKBtide is derived from sucrose non-fermenting 1 (SNF1) protein kinase, which is normally activated by the LKB1/AMP-activated protein kinase (AMPK) signaling pathway.)
|
-
- HY-B0777
-
|
CL301423
|
Antibiotic
BCRP
P-glycoprotein
Parasite
|
Infection
Neurological Disease
|
|
Moxidectin (CL301423) is an orally active and brain-penetrant macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-P5371
-
|
|
Thrombin
|
Others
|
|
TFLLRNPNDK-NH2 is a biological active peptide. (This peptide is a thrombin receptor activating peptide. This PAR-1 agonist peptide reversibly binds to PAR-1 mimicking the 'tethered ligand' that thrombin makes available through proteolytic cleavage of substrate. It is also known to cause increase in liquid and protein permeability much like thrombin.)
|
-
- HY-134136B
-
|
S-Octanoate-CoA triammonium; S-Octanoate-coenzyme A triammonium
|
Biochemical Assay Reagents
|
Others
|
|
Octanoyl coenzyme A triammonium is an enoyl-CoA hydratase binder. Octanoyl coenzyme A triammonium binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
|
-
- HY-B1746
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Pyridoxamine 5′-phosphate is the active form of vitamin B6 bound to phosphoric acid. Pyridoxamine 5′-phosphate is the aminated form of Pyridoxal 5'-?phosphate monohydrate (HY-W011727A) and as co-factor of a variety of enzymes central metabolite, potent antioxidant, vitamin B6 vitamer and enzyme substrate. Pyridoxamine 5′-phosphate can be interconverted with pyridoxal 5'-phosphate hydrate .
|
-
- HY-174905
-
|
QY201
|
JAK
Cytochrome P450
|
Inflammation/Immunology
|
|
Quecitinib (QY201) is an orally active JAK1/TYK2 dual inhibitor. Quecitinib is also a substrate of cytochrome P450 3A and is mainly metabolized to mono-oxide and glucuronidation products. Quecitinib has favorable pharmacokinetic properties as well as safety. Quecitinib can be used in the research of atopic dermatitis and other autoimmune diseases .
|
-
- HY-114511
-
|
|
Factor VIIa
|
Cardiovascular Disease
|
|
BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT) .
|
-
- HY-122142
-
|
S-2366
|
APC
Factor XI
Biochemical Assay Reagents
|
Others
|
|
Pyr-Pro-Arg-pNA (S2366) is a chromogenic peptide substrate for Factor XI and Activated protein C (APC). Pyr-Pro-Arg-pNA can induce noncompetitive inhibition of factor XI activation through occupancy of the active site of the factor XIa-light chain. Pyr-Pro-Arg-pNA can be used for measurement of APC amidolytic activity .
|
-
- HY-145779
-
|
H-γ-Glu-Met-OH; γ-Glu-Met
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
H-Glu(Met-OH)-OH (H-γ-Glu-Met-OH; γ-Glu-Met) is a DPP-IV inhibitor with an IC50 of 2.11 mM. H-Glu(Met-OH)-OH binds to DPP-IV’s active site to block substrate binding. H-Glu(Met-OH)-OH can be used for the research of type 2 diabetes .
|
-
- HY-B0804R
-
|
SQ-11725 (Standard)
|
Reference Standards
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Nadolol (Standard) is the analytical standard of Nadolol. This product is intended for research and analytical applications. Nadolol (SQ-11725) is a non-selective and orally active β-adrenergic receptors blocker and is a substrate of organic anion transporting polypeptide 1A2 (OATP1A2). Nadolol has the the potential for high blood pressure, angina pectoris and vascular headaches research .
|
-
- HY-W090942
-
|
|
Endogenous Metabolite
Sodium Channel
|
Others
|
|
Z-Gly-Gly-Phe-OH is a substrate for pepsin and thermolysin. Z-Gly-Gly-Phe-OH has an IC50 of 15.8 μM for open sodium channels under pepsin catalysis. Z-Gly-Gly-Phe-OH forms peptide bonds with amine components (such as H-Leu-NHPh) through enzyme-catalyzed condensation reactions, and is active as an intermediate in peptide synthesis .
|
-
- HY-120111A
-
|
MW01-18-150SRM hydrochloride
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW-150 hydrochloride (MW01-18-150SRM hydrochloride) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 hydrochloride (MW01-18-150SRM hydrochloride) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
- HY-134561
-
|
6A-8tFP
|
Prion Protein
|
Infection
|
|
6-Amino-8-trifluoromethylphenanthridine (6A-8tFP) is an antiprion agent and a derivative of 6-aminophenanthridine (HY-135189). It inhibits protein folding activity of the ribosome (PFAR) when used at a concentration of 150 μM.2 6A-8tFP directly competes with protein substrates for the ribosomal active site.
|
-
- HY-14405
-
|
GW679769
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
|
|
Casopitant (GW679769) is a potent, selective, brain-penetrant and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant antagonizes the emetic effects of Substance P (HY-P0201). Casopitant is also a substrate and weak to moderate inhibitor of CYP3A4. Casopitant is indicated for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
|
-
- HY-160019
-
|
|
Deubiquitinase
Mitophagy
|
Neurological Disease
|
|
MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine .
|
-
- HY-E70743
-
|
|
MASTL
|
Cancer
|
|
MASTL kinase is a master regulator of mitosis, essential for ensuring that mitotic substrate phosphorylation is correctly maintained. It achieves this through the phosphorylation of alpha-endosulfine and subsequent inhibition of the tumor suppressor PP2A-B55 phosphatase. MASTL Recombinant Human Active Protein Kinase is a recombinant MASTL protein that can be used to study MASTL-related functions .
|
-
- HY-122142A
-
|
S-2366 hydrochloride
|
APC
Factor XI
Biochemical Assay Reagents
|
Others
|
|
Pyr-Pro-Arg-pNA (S2366) hydrochloride is a chromogenic peptide substrate for Factor XI and Activated protein C (APC). Pyr-Pro-Arg-pNA hydrochloride can induce noncompetitive inhibition of factor XI activation through occupancy of the active site of the factor XIa-light chain. Pyr-Pro-Arg-pNA hydrochloride can be used for measurement of APC amidolytic activity .
|
-
- HY-P10422
-
|
ML-peptide, Multi-Leucine (ML)-peptide
|
Autophagy
|
Cancer
|
|
Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
|
-
- HY-111338R
-
|
|
Cholinesterase (ChE)
Reference Standards
|
Neurological Disease
|
|
Tacrine (Standard) is the analytical standard of Tacrine. This product is intended for research and analytical applications. Tacrine is an effective oral acetylcholine (AChE) inhibitor (IC50 = 109 nM) and also acts as an active substrate for CYP1A2. Tacrine can restore cognitive dysfunction in elderly rats. Tacrine can cause liver toxicity and is used in research related to Alzheimer's disease .
|
-
- HY-181937
-
|
|
Monoamine Oxidase
Reactive Oxygen Species (ROS)
NO Synthase
Interleukin Related
|
Neurological Disease
|
|
Multi-target kinase-IN-10 (Compound 6l) is an orally active, blood-brain barrier-permeable, selective, reversible, and competitive MAO-B inhibitor with an IC50 of 0.0053 μM. Multi-target kinase-IN-10 competes with substrates for binding to the active site of MAO-B, chelates Cu 2+ ions, inhibits Cu 2+-induced ROS production, and reduces the release of NO, TNF-α, and IL-1β. Multi-target kinase-IN-10 ameliorates Parkinson's disease .
|
-
- HY-W062835
-
|
|
Src
|
Cancer
|
|
CGP77675 is an orally active and potent inhibitor of Src family kinases. CGP77675 inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively), and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 5-20, 40, 20, 150, 1000, 310, and 290 nM, respectively. Anticancer activity .
|
-
- HY-P10422A
-
|
ML-peptide, Multi-Leucine (ML)-peptide triacetate
|
Autophagy
|
Cancer
|
|
Multi-Leu peptide (ML-peptide) triacetate is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide triacetate can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide triacetate can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
|
-
- HY-P5438
-
|
|
Btk
c-Kit
FAK
FLT3
Insulin Receptor
|
Others
|
|
Srctide is a biological active peptide. (This is a peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR).)
|
-
- HY-G0017A
-
|
Norimatinib mesylate; Imatinib metabolite N-Desmethyl imatinib mesylate; CGP 74588 mesylate
|
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
|
N-Desmethyl imatinib mesylate (Norimatinib mesylate) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib mesylate binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib mesylate induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib mesylate exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib mesylate can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
- HY-G0017
-
|
Norimatinib; Imatinib metabolite N-Desmethyl imatinib; CGP 74588
|
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
|
N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib shows significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) models with mild SARS-CoV-2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
- HY-13463A
-
|
AKR-501 maleate; E5501 maleate; YM477 maleate
|
Thrombopoietin Receptor
Cytochrome P450
ERK
STAT
|
Inflammation/Immunology
Cancer
|
|
Avatrombopag (AKR-501) maleate is an orally active, non-peptide thrombopoietin receptor (TPO receptor) agonist (EC50: 3.3 nM). Avatrombopag maleate mimics the biological activity of TPO. Avatrombopag maleate increases platelet production by activating intracellular signaling systems and promotes the production of platelets and megakaryocytes from hematopoietic precursor cells. Avatrombopag maleate is a substrate for cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-W012241S1
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
|
Dodecanedioic acid-d4 is the deuterium labeled Dodecanedioic acid (HY-W012241). Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
- HY-D1460
-
|
|
Bacterial
β-glucuronidase
|
Infection
|
|
Fluorescein Di-β-D-Glucuronide is an orally active fluorescent probe substrate and an indicator of β-glucuronidase (βG) activity in intestinal bacteria. Fluorescein Di-β-D-Glucuronide can be used for non-invasive time-lapse optical imaging of βG activity in intestinal bacteria in nude mice. Fluorescein Di-β-D-Glucuronide supports the quantitative analysis of bacterial βG enzyme activity and inhibition .
|
-
- HY-W062835A
-
|
|
Src
|
Cancer
|
|
CGP77675 hydrate is an orally active and potent inhibitor of Src family kinases. CGP77675 hydrate inhibits phosphorylation of peptide substrates and autophosphorylation of purified Src (IC50s of 5-20 and 40 nM, respectively),and also inhibits Src, EGFR, KDR, v-Abl, and Lck with IC50s of 0.02, 0.15, 1.0, 0.31, and 0.29 μM, respectively. Anticancer activity .
|
-
- HY-13463
-
|
AKR-501; E5501; YM477
|
Thrombopoietin Receptor
|
Inflammation/Immunology
Cancer
|
|
Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-120111B
-
|
MW01-18-150SRM dihydrochloride dihydrate
|
p38 MAPK
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
|
MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) is a selective, CNS penetrant, and orally active inhibitor of p38α MAPK with a Ki of 101 nM. MW-150 dihydrochloride dihydrate (MW01-18-150SRM dihydrochloride dihydrate) inhibits the ability of the endogenous p38α MAPK to phosphorylate an endogenous substrate MK2 in activated glia .
|
-
- HY-W011297
-
|
Arachidonic acid methyl ester
|
PKC
|
Metabolic Disease
|
|
Methyl arachidonate is a protein kinase C activator and also an orally active substrate that undergoes esterase-mediated hydrolysis. Methyl arachidonate indirectly activates protein kinase C via eicosanoid metabolites generated through the arachidonic acid metabolic pathway, exerting effects via cyclooxygenase products at low concentrations and via lipoxygenase products at high concentrations. Methyl arachidonate can be used in studies related to lipodystrophy .
|
-
- HY-P5344
-
|
Fluorigenic PEXEL peptide
|
Parasite
|
Others
|
|
Dabcyl-LNKRLLHETQ-Edans (Fluorigenic PEXEL peptide) is a biological active peptide. (This FRET substrate peptide for Plasmepsin V (PMV) is derived from the conserved Plasmodium Export Element (PEXEL) motif of Histidine-Rich Protein II (HRPII). PMV is an ER aspartic protease that recognizes and cleaves the RXL sequence within the PEXEL motif of proteins exported by human malaria parasite Plasmodium falciparum, allowing them to translocate into host erythrocytes.)
|
-
- HY-B0777R
-
|
CL301423 (Standard)
|
Antibiotic
BCRP
P-glycoprotein
Parasite
Reference Standards
|
Infection
|
|
Moxidectin (Standard) is the analytical standard of Moxidectin. This product is intended for research and analytical applications. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-13463B
-
|
AKR-501 hydrochloride; E5501 hydrochloride; YM477 hydrochloride
|
Thrombopoietin Receptor
|
Cardiovascular Disease
Cancer
|
|
Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-W012241S
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
|
Dodecanedioic acid-d20 is the deuterium labeled Dodecanedioic acid (HY-W012241). Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
- HY-P4931
-
|
|
MMP
|
Cancer
|
|
Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 (FS-6) is a fluorescent peptide that is a quenched MMP peptide substrate. Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 can be used for real-time quantification of MMP enzymatic activity. Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 is an elongated peptide of MMP substrate (FS-1) and is active against collagenases (MMP-1, MMP-8, MMP-13 ) and MT1-MMP with higher specificity constants than FS-1 . (Ex/Em=325 nm/400 nm)
|
-
- HY-14405A
-
|
GW679769B
|
Neurokinin Receptor
Cytochrome P450
|
Neurological Disease
Cancer
|
|
Casopitant mesylate (GW679769B) is a potent, selective, brain permeable and orally active neurokinin 1 (NK1) receptor antagonist. Casopitant mesylate is a second in the class of antiemetics that acts to antagonise the emetogenic effect of Substance P (HY-P0201). Casopitant mesylate is also a substrate and a weak-to-moderate inhibitor of CYP3A4. Casopitant mesylate can be used for chemotherapy-induced nausea and vomiting (CINV) and postoperative nausea and vomiting (PONV) .
|
-
- HY-146237
-
|
CC-99282
|
Ligands for E3 Ligase
Molecular Glues
|
Cancer
|
|
Golcadomide (CC-99282) is a potent and orally active CRBN E3 ligase modulator (CELMoD). Golcadomide interacts with the CRL4 CRBN E3 ubiquitin ligase substrate receptor CRBN, inducing the recruitment and ubiquitin-mediated proteasomal degradation of the transcription factors Ikaros and Aiolos. Golcadomide shows potential for research in cancer-related fields, including chronic lymphocytic leukemia (CLL) and non-Hodgkin lymphoma (NHL) .
|
-
- HY-B2029
-
|
|
Insecticide
Cholinesterase (ChE)
|
Infection
Inflammation/Immunology
|
|
Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis .
|
-
- HY-W777762
-
|
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
|
Dodecanedioic Acid- 13C12 is the 13C-labeled Dodecanedioic acid (HY-W012241). Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
- HY-P5525
-
|
Autocamtide-3 Derived Inhibitory Peptide
|
CaMK
|
Others
|
|
AC3-I, myristoylated is a biological active peptide. (This is a myristoylated form of Autocamtide-3-Derived Inhibitory Peptide (AC3-I), a highly specific inhibitor of Calmodulin-Dependent Protein Kinase ll (CaMKII) that is resistant to proteolysis. AC3-I is derived from Autocamtide-3, a substrate for CaMKII, with the Thr-9 phosphorylation site substituted with Ala.)
|
-
- HY-183978
-
|
|
Renin
|
Cardiovascular Disease
|
|
KRI-1314 is an orally active human renin inhibitor with selectivity for primate renin over non-primate renin. KRI-1314 competitively inhibits the binding of recombinant human renin to its substrate, reduces plasma renin activity, lowers blood pressure, and exhibits high stability in tissue homogenates. KRI-1314 is applicable to research on renin-dependent hypertension and hypertension-related studies .
|
-
- HY-W012241R
-
|
|
Reference Standards
Endogenous Metabolite
|
Metabolic Disease
|
|
Dodecanedioic acid (Standard) is the analytical standard of Dodecanedioic acid (HY-W012241). This product is intended for research and analytical applications. Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
- HY-107597R
-
|
SU3327 (Standard)
|
Reference Standards
JNK
|
Metabolic Disease
Inflammation/Immunology
|
|
Halicin (Standard) is the analytical standard of Halicin (HY-107597). This product is intended for research and analytical applications. Halicin (SU3327) is a potent, selective and substrate-competitive JNK inhibitor with an IC50 of 0.7 μM. Halicin also inhibits protein-protein interactions between JNK and JNK Interacting Protein (JIP) with an IC50 of 239 nM. Halicin shows less active against p38α and Akt Kinase .
|
-
- HY-170322
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Metabolic Disease
Cancer
|
|
TDO2-IN-1 is a selective TDO2 inhibitor. TDO2-IN-1 binds to the active pocket, heme-binding pocket and substrate-binding pocket of apo-TDO2, interacts with key residues, competitively inhibits heme insertion, and suppresses intracellular TDO2 activity. TDO2-IN-1 can be used in research related to cancer, metabolism and other fields .
|
-
- HY-17367
-
-
- HY-B0306
-
|
Protionamide
|
Bacterial
|
Infection
|
|
Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
|
-
- HY-W115752
-
|
Diamine sulfate (99%)
|
PEPCK
Aldehyde Dehydrogenase (ALDH)
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Hydrazine sulfate is an orally active PEPCK inhibitor. Hydrazine sulfate inhibits PEPCK and low-Km ALDH. Hydrazine sulfate impairs gluconeogenesis and enhances the protective effect of energy substrates against MPP + toxicity. Hydrazine sulfate exacerbates liver damage in rats when combined with Ethanol. Hydrazine sulfate can be used in the research of shock, non-small cell lung cancer, colorectal cancer and Parkinson's disease .
|
-
- HY-P11302
-
|
|
CHIKV
Virus Protease
|
Infection
|
|
DABCYL-RAGGYIFS-(E-EDANS)-NH2, an octapeptide, is a FRET-based substrate peptide of CHIKV nsP2protease with highly sensitivity. DABCYL-RAGGYIFS-(E-EDANS)-NH2 can be cleaved by the active CHIKV nsP2protease, separating fluorophore and quencher and resulting in an increase of fluorescence signal. DABCYL-RAGGYIFS-(E-EDANS)-NH2 can used for the determination of CHIKV nsP2protease activity .
|
-
- HY-139577
-
|
IMB-1018972; IMB-101
|
Mitochondrial Metabolism
|
Cardiovascular Disease
Metabolic Disease
|
|
Ninerafaxstat (IMB-1018972) is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat can be used for research on cardiovascular diseases .
|
-
- HY-131131
-
|
|
Fluorescent Dye
|
Others
|
|
5-CFDA-AM is a cell-permeable esterase substrate that can be used as an active probe to measure enzyme activity and cell membrane integrity. 5-CFDA-AM is electroneutral and can enter the cell at a lower concentration than CFDA, where it is hydrolysed by intracellular esterases to produce carboxyfluorescein, which contains an additional negative charge and can be better retained in the cell. 5-CFDA-AM can be used to detect cell viability .
|
-
- HY-167920
-
|
S-Sulfoglutathione
|
Endogenous Metabolite
|
Cancer
|
|
Glutathione sulfonate (S-Sulfoglutathione) is a multifunctional bioactive compound that inhibits angiogenesis and tumor growth. Glutathione sulfonate is a competitive inhibitor of glutathione S-transferase and is involved in the detoxification process and the binding of a variety of exogenous and endogenous compounds. Glutathione sulfonate acts in the substrate binding site of Escherichia coli glutathione S-transferase, affecting the catalytic mechanism. The structural characteristics of Glutathione sulfonate contribute to its inhibitory effect by hydrogen bonding in the active center of the enzyme .
|
-
- HY-G0017S1
-
|
Norimatinib-d4; Imatinib metabolite N-Desmethyl imatinib-d4; CGP 74588-d4
|
Isotope-Labeled Compounds
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
|
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
- HY-119601
-
|
|
Phosphodiesterase (PDE)
|
Cancer
|
|
GRI918013 (compound 1) is a selective and competitive autotaxin (ATX/NPP2) inhibitor with anti-invasive and anti-metastatic activity. GRI918013 competitively binds to ATX, blocking lipid substrates such as lysophosphatidylcholine (LPC) from entering the ATX active site, thereby inhibiting ATX-mediated hydrolysis of LPC to lysophosphatidic acid (LPA), and consequently inhibiting ATX-LPA axis-related tumor cell invasion and metastasis. GRI918013 inhibits ATX-mediated hydrolysis of the LPL substrate FS-3 (IC50=31.42 nM, Ki=12.98 nM). GRI918013 can be used in research on cancer invasion and metastasis, such as melanoma, and can also serve as a tool compound for ATX-LPA axis-related diseases such as fibrotic diseases, neuropathic pain, and cholestatic pruritus .
|
-
- HY-145561
-
|
BLD-0409; PAT-409
|
Phosphodiesterase (PDE)
LPL Receptor
|
Inflammation/Immunology
Cancer
|
|
Cudetaxestat (BLD-0409; PAT-409) is an orally active and noncompetitive autotaxin (ATX) inhibitor. Cudetaxestat inhibits the activity of ATX, reduces the production of LPA, and thereby blocks the signal transduction of the ATX-LPA axis. Cudetaxestat can still maintain nanomolar-level biochemical efficacy even when the concentration of the LPC substrate increases. Cudetaxestat can be used for the study of various diseases related to LPA including fibrosis, tumor metastasis, inflammation and autoimmune diseases, etc .
|
-
- HY-W011834R
-
|
|
Reference Standards
HCV
DNA/RNA Synthesis
|
Infection
|
|
2'-O-Methylcytidine (Standard) is the analytical standard of 2'-O-Methylcytidine. This product is intended for research and analytical applications. 2'-O-Methylcytidine is an orally active 2'-substituted nucleoside as a inhibitor of HCV replication with antiviral activity. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
|
-
- HY-122643
-
|
|
Bacterial
|
Infection
|
|
NITD-916, a 4-hydroxy-2-pyridone derivative, is an orally active mycobacterial enoyl reductase InhA inhibitor with an IC50 of 570 nM. NITD-916 forms a ternary complex with InhA and NADH to block access to the fatty acyl substrate binding pocket. NITD-916 inhibition of InhA reduces the synthesis of mycolic acids and results in cell death. NITD-916 has potent anti-tuberculosis effects .
|
-
- HY-108666R
-
|
Adenosine-5'-O-(3-thiotriphosphate) tetralithium salt (Standard); Adenosine 5'-[γ-thio]triphosphate tetralithium salt (Standard)
|
Reference Standards
Eukaryotic Initiation Factor (eIF)
P2Y Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
ATPγS tetralithium salt (Standard) is the analytical standard of ATPγS (tetralithium salt) (HY-108666). This product is intended for research and analytical applications. ATPγS (tetralithium salt) is a P2Y11 receptor agonist, an antioxidant and a neuroprotective agent. ATPγS (tetralithium salt) can be used as a substrate for the nucleotide hydrolysis and RNA unwinding activities of eukaryotic translation initiation factor eIF4A. ATPγS (tetralithium salt) is active in ATP hydrolysis .
|
-
- HY-182567
-
|
|
NAMPT
|
Cancer
|
|
Nampt-IN-19 is an orally active and non-substrate nicotinamide phosphoribosyltransferase (NAMPT) inhibitor with a human Ki of 5.6 nM. Nampt-IN-19 blocks NAD + biosynthesis from Nicotinamide (HY-B0150). Nampt-IN-19 acts as an antiproliferative agent in cancer cells. Nampt-IN-19 has preclinical pharmacokinetic properties supporting oral antitumor activity in mouse xenograft models. Nampt-IN-19 can be used for the research of colorectal cancer .
|
-
- HY-137846A
-
|
|
Acetyl-CoA Carboxylase
OAT
|
Metabolic Disease
Inflammation/Immunology
|
|
PF-05221304 tromethamine is an orally active, liver-directed and dual ACC1/ACC2 inhibitor with IC50s of 7.5 nM for rat ACC1, 8.2 nM for rat ACC2. PF-05221304 tromethamine is a substrate for organic anion transport polypeptides. PF-05221304 tromethamine directly improves a variety of non-alcoholic fatty liver (NAFL) and non-alcoholic steatohepatitis (NASH) pathogenic factors .
|
-
- HY-B0777S
-
|
CL-301423-d3
|
Isotope-Labeled Compounds
BCRP
Parasite
Antibiotic
P-glycoprotein
|
Infection
|
|
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
- HY-153510
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Neurological Disease
Inflammation/Immunology
|
|
PHD-1-IN-2 is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase domain 1 (PHD-1) with an IC50 of 0.07 μM. PHD-1-IN-2 acts as a substrate of MDR1 in MDR1-MDCK cell monolayer assays. PHD-1-IN-2 can be used in the research of ischemia, inflammatory responses and neurodegenerative diseases, such as inflammatory bowel disease and ischemia-reperfusion injury .
|
-
- HY-13463BS
-
|
AKR-501-d8 hydrochloride; E5501-d8 hydrochloride; YM477-d8 hydrochloride
|
Isotope-Labeled Compounds
Thrombopoietin Receptor
|
Cardiovascular Disease
|
|
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-182440
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AZD3783 is an orally active, blood-brain barrier-penetrant 5-HT1B receptor antagonist. AZD3783 reverses agonist-induced hypothermia, inhibits separation-induced vocalizations in guinea pig pups, and acts as a moderately permeable glycoprotein substrate with moderate clearance. AZD3783 inhibits hERG channel activity. AZD3783 is applicable for research on depression, anxiety disorders, and other psychiatric diseases associated with serotonergic neurotransmission .
|
-
- HY-13463BR
-
|
AKR-501 hydrochloride (Standard); E5501 hydrochloride (Standard); YM477 hydrochloride (Standard)
|
Thrombopoietin Receptor
Reference Standards
|
Cardiovascular Disease
Cancer
|
|
Avatrombopag (hydrochloride) (Standard) is the analytical standard of Avatrombopag (hydrochloride). This product is intended for research and analytical applications. Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-N1420
-
|
L-Rhamnose
|
Environmental Pollutants
Endogenous Metabolite
PKA
MMP
Interleukin Related
|
Infection
Metabolic Disease
Cancer
|
|
Rhamnose (L-Rhamnose ) is an orally active deoxysugar. Rhamnose can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. 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 shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
|
-
- HY-W099538
-
|
Dilauryl 3,3'-Thiodipropionate
|
Environmental Pollutants
Biochemical Assay Reagents
|
Others
|
|
Dilauryl thiodipropionate (DLTDP), which is a sulfur-containing antioxidant commonly used to stabilize polymers and plastics against degradation caused by heat, oxygen, and UV light, acts to scavenge free radicals and others that may cause polymer chain scission and cross-linked active substances, in addition, DLTDP has been used as an additive to lubricants, oils and other industrial fluids to improve their oxidation stability, the long hydrocarbon chain in DLTDP makes it low volatility and compatible with many materials and Good compatibility with substrates.
|
-
- HY-13463R
-
|
AKR-501 (Standard); E5501 (Standard); YM477 (Standard)
|
Reference Standards
Thrombopoietin Receptor
|
Inflammation/Immunology
Cancer
|
|
Avatrombopag (Standard) is the analytical standard of Avatrombopag. This product is intended for research and analytical applications. Avatrombopag (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag mimics the biological activities of TPO. Avatrombopag increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-175795
-
|
|
Tyrosinase
Bacterial
Antibiotic
|
Infection
|
|
Tyrosinase activator-1 (Compound 7A) is a Tyrosinase activator. Tyrosinase activator-1 significant antibacterial activity against gram-positive bacteria, such as MRSA, Staphylococcus aureus ATCC653 and Enterococcus faecium with MICs of 12.5-20 μM. Tyrosinase activator-1 activates tyrosinase by competitively occupying the binding site of L-DOPA on the surface of tyrosinase without interfering with the substrate binding at the active center. Tyrosinase activator-1 can be used for bacterial infections and antibiotics development research .
|
-
- HY-153667
-
|
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
MK-2305 is an orally active GPR40 partial agonist with an EC50 of 6 nM in rats. MK-2305 mediates glucose-stimulated insulin secretion and inhibits endogenous glucose production by reducing gluconeogenesis from tricarboxylic acid (TCA) cycle substrates. MK-2305 increases plasma insulin levels under hyperglycemic and glucose-stimulated conditions, reduces fasting blood glucose, and improves glucose homeostasis. MK-2305 can be used in studies related to type 2 diabetes .
|
-
- HY-N1420A
-
|
L-Rhamnose monohydrate
|
Endogenous Metabolite
MMP
Interleukin Related
PKA
|
Infection
Metabolic Disease
Cancer
|
|
Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
|
-
- HY-13463AR
-
|
AKR-501 maleate (Standard); E5501 maleate (Standard); YM477 maleate (Standard)
|
Thrombopoietin Receptor
Cytochrome P450
ERK
STAT
Reference Standards
|
Inflammation/Immunology
Cancer
|
|
Avatrombopag (maleate) (Standard) is the analytical standard of Avatrombopag (maleate). This product is intended for research and analytical applications. Avatrombopag maleate (AKR-501) is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag maleate mimics the biological activities of TPO. Avatrombopag maleate increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag maleate is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
- HY-B2228
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
Proteinase, Aspergillus oryzae is a serine protease that hydrolyzes peptide bonds in protein substrates, preferring alkaline conditions (optimal pH 10.5). It efficiently degrades casein, poly-L-glutamic acid, and poly-L-lysine, with activity irreversibly inhibited by diisopropylfluorophosphate (DFP) and potato inhibitor. This enzyme catalyzes proteolysis via serine residues in its active site, finding applications in food processing (e.g., soy sauce fermentation), detergents, and leather industries due to its high yield in solid-state fermentation and cost-effective production.
|
-
- HY-139577A
-
|
MB-1018972 trihydrochloride; IMB-101 trihydrochloride
|
Mitochondrial Metabolism
|
Cardiovascular Disease
Metabolic Disease
|
|
Ninerafaxstat trihydrochloride (IMB-1018972 trihydrochloride) is the trihydrochloride salt form of Ninerafaxstat (HY-139577). Ninerafaxstat trihydrochloride is a novel orally active cardiac mitochondrial drug that restores myocardial energy homeostasis. Ninerafaxstat trihydrochloride competitively inhibits 3-ketoacyl-CoA thiolase (3-KAT) to partially suppress fatty acid oxidation, and shifts cardiac energy metabolism from free fatty acid oxidation to glucose oxidation, regulating myocardial substrate utilization and thereby improving cardiac efficiency. Ninerafaxstat trihydrochloride can be used for research on cardiovascular diseases .
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-
- HY-133708
-
|
Glucogallin; 1-O-Galloyl-β-D-glucose
|
Aldose Reductase
Reactive Oxygen Species (ROS)
NF-κB
PDGFR
SOD
|
Neurological Disease
Metabolic Disease
|
|
β-Glucogallin is an orally active and selective aldose reductase (AKR1B1) inhibitor with an IC50 value of 58 μM when using Glyceraldehyde (HY-128748) as AKR1B1 substrate. β-Glucogallin reduces ROS, PDGF, RAGE, and NF-κB. β-Glucogallin increases SOD. β-Glucogallin has antioxidant and hepatoprotective effects. β-Glucogallin can be used in retinal research .
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-
- HY-17367R
-
|
BMS-232632 (Standard)
|
Reference Standards
HIV
HIV Protease
SARS-CoV
Cytochrome P450
P-glycoprotein
Endogenous Metabolite
|
Infection
Cancer
|
|
Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
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-
- HY-17367A
-
-
- HY-G0017S
-
|
Norimatinib-d8; Imatinib metabolite N-Desmethyl imatinib-d8; CGP 74588-d8
|
Isotope-Labeled Compounds
Drug Metabolite
P-glycoprotein
Apoptosis
|
Neurological Disease
Cancer
|
|
N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
- HY-156735
-
|
|
17β-HSD
|
Cancer
|
|
HSD17B13-IN-2 is an HSD17B13 inhibitor with human IC50 values of 0.18 μM (with β-estradiol as substrate) and 0.25 μM (with Leukotriene B4 as substrate), and it exhibits selectivity for human HSD17B11. HSD17B13-IN-2 binds to the active site of HSD17B13 in an NAD +-dependent manner, interacts with the bound NAD + cofactor, and stabilizes human HSD17B13 protein to prevent its aggregation. HSD17B13-IN-2 reduces the conversion of β-estradiol to estrone in cellular assays. HSD17B13-IN-2 can be used in studies related to nonalcoholic fatty liver disease .
|
-
- HY-G0017R
-
|
Norimatinib (Standard); Imatinib metabolite N-Desmethyl imatinib (Standard); CGP 74588 (Standard)
|
Reference Standards
Drug Metabolite
P-glycoprotein
Apoptosis
|
Others
|
|
N‑Desmethyl imatinib (Standard) is the analytical standard of N‑Desmethyl imatinib (Norimatinib) (HY-G0017R). This product is intended for research and analytical applications. N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
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-
- HY-W127711
-
|
|
Phosphatase
Lipase
|
Metabolic Disease
Inflammation/Immunology
|
Fast Blue B Salt, Dye content ~95% is a diazo dye, primarily used as a chromogenic substrate in biochemical analysis. Fast Blue B Salt, Dye content ~95% is the coupling agent for the histochemical demonstration of proteases. Fast Blue B Salt, Dye content ~95% can be used for the detection of acid phosphatase in Clostridium perfringens, and also for the determination of lipase activity. Fast Blue B Salt, Dye content ~95% reacts directly with the active hydroxyl groups in phenolic compounds to determine the content of phenolic substances .
|
-
- HY-128895A
-
|
|
Mitochondrial Metabolism
Quinone Reductase
|
Metabolic Disease
|
|
KL1333 hydrochloride is an orally active NAD + modulator that reacts with NAD(P)H:quinone oxidoreductase 1 (NQO1) as a substrate, leading to increased intracellular NAD + levels through NADH oxidation. Elevated NAD + levels trigger activation of SIRT1 and AMPK, and subsequently activate PGC-1α. KL1333 hydrochloride improves energy metabolism and mitochondrial dysfunction in mitochondrial encephalomyopathy, lactic acidosis, and stroke-like episodes (MELAS) fibroblasts. KL1333 hydrochloride protects against cisplatin-induced ototoxicity in mouse cochlear cultures .
|
-
- HY-176001
-
|
|
Dipeptidyl Peptidase
|
Inflammation/Immunology
Cancer
|
|
DPP8/9-IN-1 (Compound 16) is a selective covalent inhibitor of dipeptidyl peptidases 8 and 9 (DPP8/9) with IC50 values of 14 and 298 nM, respectively. DPP8/9-IN-1 binds irreversibly to the active site serine (S730 in DPP9) via a phosphonate warhead and blocks substrate binding to inhibit DPP8/9-mediated protein processing. DPP8/9-IN-1 is promising for research of cancers and inflammatory diseases .
|
-
- HY-N1181
-
-
- HY-126077
-
MTI-31
1 Publications Verification
LXI-15029
|
mTOR
|
Inflammation/Immunology
Cancer
|
|
MTI-31 (LXI-15029) is a potent, orally active and highly selective inhibitor of mTORC1 and mTORC2. MTI-31 is selective for mTOR (Kd: 0.20 nM) versus PIK3CA, PIK3CB and PIK3G with >5,000 fold selectivity in mTOR binding assays. MTI-31 shows an IC50 of 39 nM for mTOR in LANCE assay of mTOR substrate phosphorylation with 100 μM ATP. MTI-31 can be used for the research of breast cancer .
|
-
- HY-165444
-
|
NGD-913
|
GABA Receptor
|
Neurological Disease
|
|
CP-615003 is a potent and subtype-selective partial agonist of GABAA receptor (GABAA receptor) (Ki = 1.1 μM). CP-615003 is mainly converted into the active metabolite CP-900725 through oxidative deamination in monkeys and humans, and the latter also has GABAA receptor affinity. CP-615003 is a substrate of P-glycoprotein (P-gp/MDR1), resulting in severe limitation of its penetration into the central nervous system (CNS). CP-615003 can be used for the study of CNS-related indications .
|
-
- HY-178124
-
|
|
Deubiquitinase
|
Neurological Disease
Cancer
|
|
Huib32 is a potent small-molecule inhibitor of USP32 (IC50 = 21.2 nM), exhibiting high selectivity over other closely related deubiquitinating enzymes (DUBs), such as USP8/10/16, UCHL1 and OTUB2. Huib32 reversibly inhibits USP32 by covalently binding to the active site Cys743, which enhances substrate ubiquitination, alters endosomal morphology, and mimics USP32 depletion. Huib32 can be used for breast, ovarian, and lung cancer and Alzheimer's and Parkinson’s diseases research .
|
-
- HY-162495
-
|
|
CCR
Calcium Channel
Arrestin
P-glycoprotein
|
Inflammation/Immunology
Cancer
|
|
IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation .
|
-
- HY-B0306S
-
|
Protionamide-d5
|
Isotope-Labeled Compounds
Bacterial
|
Infection
|
|
Prothionamide-d5 is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
|
-
- HY-W879508
-
|
BXT-51072
|
Cytochrome P450
Glutathione Peroxidase
|
Inflammation/Immunology
|
|
ALT-2074 (BXT-51071) is an orally active catalytic analogue of glutathione peroxidase. ALT-2074 is an inhibitor of human CYP3A, with its IC50 value ranging from 2.0 to 2.6 μM. ALT-2074 shows only a weak inhibitory effect on CYP3A in vivo, suggesting that it may not significantly affect the metabolism of CYP3A substrate drugs. ALT-2074 can be used to study inflammatory diseases characterized by reactive oxygen species, such as acute coronary syndrome .
|
-
- HY-17367S5
-
-
- HY-N0419
-
|
Quercetin-7-O-β-D-glucopyranoside
|
Glycosidase
c-Kit
MMP
VEGFR
Aurora Kinase
|
Metabolic Disease
Cancer
|
|
Quercimeritrin (Quercetin-7-O-β-D-glucopyranoside) is an orally active α-glucosidase inhibitor (with an IC50 of 79.88 μM against the Saccharomyces cerevisiae enzyme) and a P-gp substrate, with anti-angiogenic and antioxidant activities. Quercimeritrin does not cross the blood-brain barrier and does not inhibit cytochrome P450 enzymes. Quercimeritrin precisely binds to and inhibits the active sites of c-Kit, MMP-2, Aurora-A kinases and α-glucosidase, thereby disrupting target functions. Quercimeritrin effectively regulates postprandial blood glucose and also exhibits significant anti-angiogenic activity, which inhibits endothelial cell proliferation and microvascular growth. Quercimeritrin can be used in the research of diabetes and breast cancer .
|
-
- HY-182311
-
|
|
Aldose Reductase
Glycosidase
|
Metabolic Disease
|
|
ALR2/α-Glucosidase-IN-1 (Compound 4) is a competitive ALR2 inhibitor and competitive α-glucosidase inhibitor, with an IC50 of 0.250 μM against ALR2 and an IC50 of 0.561 μM against α-glucosidase. ALR2/α-Glucosidase-IN-1 binds to the active sites of ALR2 and α-glucosidase, and inhibits enzymatic activity by competing with their respective substrates. ALR2/α-Glucosidase-IN-1 can be used in diabetes-related research .
|
-
- HY-164401
-
|
|
DNA Alkylator/Crosslinker
Apoptosis
|
Cancer
|
|
QBS10072S is a LAT1-selective substrate with blood-brain barrier permeability that inhibits tumor growth. QBS10072S enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces interstrand DNA cross-linking and cell apoptosis, and reduces leptomeningeal dissemination. QBS10072S can be used in studies related to glioblastoma multiforme, diffuse intrinsic pontine glioma, triple-negative breast cancer brain metastases, and aggressive T-cell lymphoma .
|
-
- HY-134599
-
|
|
Biochemical Assay Reagents
|
Cancer
|
|
(2E)-TCO-PNB ester is an active reaction substrate with the properties of trans-cyclooctene derivatives. The core chemical property of (2E)-TCO-PNB ester is its ability to undergo efficient inverse electron-demand Diels-Alder (IEDDA) cycloaddition with tetrazine groups. (2E)-TCO-PNB ester can be used in ligation reactions to verify the integrity of tetrazine groups, and also serves as a key synthetic raw material for the preparation of the prodrug TCO-DOX. (2E)-TCO-PNB ester is applied in research related to drug synthesis and bioorthogonal chemistry .
|
-
- HY-113493
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
4-Pyridoxic acid is an endogenous substrate of renal organic anion transporters (OAT1/3) and a catabolite of vitamin B6. 4-Pyridoxic acid is excreted through OAT1/3-mediated tubular active secretion, which can reflect OAT1/3 activity. Elevated plasma concentrations of 4-Pyridoxic acid are associated with decreased OAT1/3 activity in chronic kidney disease (CKD) and can be used as a biomarker to reflect the severity of knee osteoarthritis (KOA) and lumbar spondylosis (LS) .
|
-
- HY-N1420AR
-
|
L-Rhamnose monohydrate (Standard)
|
Reference Standards
Endogenous Metabolite
MMP
Interleukin Related
PKA
|
Infection
Metabolic Disease
Cancer
|
|
Rhamnose monohydrate (Standard) is the analytical standard of Rhamnose monohydrate (HY-N1420A). Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
|
-
- HY-148290
-
|
|
PROTACs
IRAK
|
Cancer
|
|
KTX-951 is an orally active IRAK4 and IMiD (Ikaros/Aiolos) substrates PROTAC degrader (Kd = 3.5 nM). KTX-951 has DC50s of 13 nM, 14 nM and 13 nM for IRAK4, Ikaros and Aiolos, respectively. KTX-951 has IC50 of 35 nM for OCl-Ly10 CTG. KTX-951 has antitumor activity.(Pink: IRAK4 ligand-12 (HY-48932); Black: Linker (HY-W382009); Blue: CRBN Ligand Pomalidomide (HY-10984)) .
|
-
- HY-155995
-
|
MK-905
|
Biochemical Assay Reagents
|
Cancer
|
|
Pro-905 is a phosphite peptide with antitumor activity. Pro-905 delivers the active nucleotide antimetabolite thioguanosine monophosphate (TGMP) to the tumor. Pro-905 effectively prevents incorporation of purine salvage substrates into nucleic acids and inhibits colony formation in human malignant peripheral nerve sheath tumors (MPNST) cells. Pro-905 inhibits purine salvage incorporation to nucleic acids and prevents cell growth. Pro-905 inhibits the growth of MPNST and enhances the anti-tumor efficacy of JHU395 (HY-124778) .
|
-
- HY-174128
-
|
|
ERK
Apoptosis
|
Cancer
|
|
Multi-target kinase-IN-5 (Compound 23) is an orally active ERK1/2 inhibitor (IC50 values are 3.04 nM and 1.57 nM, respectively). Multi-target kinase-IN-5 significantly inhibits cancer cell proliferation, migration and invasion, and induces cell apoptosis and cell cycle arrest. Multi-target kinase-IN-5 inhibits the phosphorylation of ERK1/2 and downregulates the activity of its downstream substrate RSK to exert anti-tumor effects. Multi-target kinase-IN-5 can be used in cancer research .
|
-
- HY-N2464
-
|
Amylotetraose; Fujioligo 450; α-1,4-Tetraglucose
|
TNF Receptor
Endogenous Metabolite
Bacterial
Integrin
NF-κB
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Maltotetraose can serve as a substrate for enzyme-linked assays to measure amylase activity in biological fluids. Maltotetraose has oral active, and reduces TNF-α-induced inflammatory responses by inhibiting NF-κB activity and decreasing ICAM-1 expression. Maltotetraose also inhibits PDGF-induced vascular smooth muscle cell migration and neovascularization. Additionally, Maltotetraose derivatives can function as probes for detecting bacterial infections by targeting the maltodextrin transporter. With good long-term safety, Maltotetraose holds promise for research in atherosclerosis-related diseases .
|
-
- HY-10289
-
|
RO-4876904
|
Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
|
Metabolic Disease
|
|
Carmegliptin (RO-4876904) is an orally active and potent DPP IV inhibitor with a human DPP IV IC50 of 6.8 nM. Carmegliptin binds to the S1 pocket of DPP IV, blocks the degradation of GLP 1, potentiates endogenous GLP 1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin acts as a substrate for human P glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin can be used for the research of type 2 diabetes, non insulin dependent diabetes mellitus .
|
-
- HY-B0306R
-
|
Protionamide (Standard)
|
Reference Standards
Bacterial
|
Infection
|
|
Prothionamide (Standard) is the analytical standard of Prothionamide (HY-B0306). This product is intended for research and analytical applications. Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
|
-
- HY-W348485
-
|
|
mTOR
|
Cancer
|
|
WRX606 is an orally active nonrapalog inhibitor for mTOR complex 1 (mTORC1M). WRX606 inhibits the phosphorylation of mTORC1 substrate S6 kinase 1 (S6K1) (IC50 = 10 nM) and eukaryotic translation initiation factor 4E binding protein (p-4E-BP1) (IC50 = 0.27 μM) in MCF-7 cells. WRX606 suppresses tumor growth in mice without promotion of metastasis. WRX606 can be studied in research as an antitumor agent .
|
-
- HY-10289A
-
|
RO-4876904 hydrochloride
|
Dipeptidyl Peptidase
GLP Receptor
P-glycoprotein
|
Metabolic Disease
|
|
Carmegliptin hydrochloride (RO-4876904 hydrochloride) is an orally active and potent DPP‑IV inhibitor with a human DPP‑IV IC50 of 6.8 nM. Carmegliptin hydrochloride binds to the S1 pocket of DPP‑IV, blocks the degradation of GLP‑1, potentiates endogenous GLP‑1, increases plasma insulin levels, alleviates hyperglycemia, improves glucose tolerance. Carmegliptin hydrochloride acts as a substrate for human P‑glycoprotein without inhibiting the transporter, shows low in vitro cell permeability. Carmegliptin hydrochloride can be used for the research of type 2 diabetes, non‑insulin‑dependent diabetes mellitus .
|
-
- HY-164401A
-
|
|
EAAT
DNA/RNA Synthesis
DNA Alkylator/Crosslinker
|
Cancer
|
|
QBS10072S dihydrochloride is a LAT1-selective substrate with blood-brain barrier permeability that inhibits tumor growth. QBS10072S dihydrochloride enters LAT1-expressing tumor cells via LAT1-mediated active transport, induces interstrand DNA cross-linking and cell apoptosis, and reduces leptomeningeal dissemination. QBS10072S dihydrochloride can be used in studies related to glioblastoma multiforme, diffuse intrinsic pontine glioma, triple-negative breast cancer brain metastases, and aggressive T-cell lymphoma .
|
-
- HY-P992275
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
Anti-Nicastrin Antibody (A5226A) is a monoclonal antibody against Nicastrin and an inhibitor of γ-secretase. Anti-Nicastrin Antibody (A5226A) recognizes the fully glycosylated mature presenilin enhancer in the active γ-secretase complex and inhibits its activity via competition for substrate binding. Anti-Nicastrin Antibody (A5226A) abrogates the growth of cancer cells dependent on γ-secretase activity. Anti-Nicastrin Antibody (A5226A) serves as an imaging tool to visualize the endocytic trafficking of active γ-secretase, and also acts as a detection reagent to evaluate the endocytic efficiency of γ-secretase. Anti-Nicastrin Antibody (A5226A) can be used in studies related to non-small cell lung cancer, T-cell acute lymphoblastic leukemia and Alzheimer's disease .
|
-
- HY-137129
-
|
|
Dihydrofolate reductase (DHFR)
|
Cancer
|
|
10-Formyl-7,8-dihydrofolic acid is a biologically active folic acid and growth promoter. 10-Formyl-7,8-dihydrofolic acid serves as a substrate for aminoimidazolecarboxamide ribonucleotide transformylase and dihydrofolate reductase (DHFR) to support catalytic reactions (with detection wavelengths of 552 nm and 340 nm, respectively). 10-Formyl-7,8-dihydrofolic acid not only promotes the growth of leukemia cells, but also effectively reverses the growth inhibition induced by antifolate drugs under folate-deficient conditions. 10-Formyl-7,8-dihydrofolic acid can be used in the research of leukemia .
|
-
- HY-178777
-
|
|
PROTACs
BCL6
|
Cancer
|
|
BCL6-760 is an orally active BCL-6 PROTAC degrader with an EC50 of 0.8 nM. BCL6-760 only degrades BCL6 and has no effect on other CRBN substrates. BCL6-760 demonstrates significant efficacy in the orthotopic xenograft mouse model of OCI-LY-1 tumors. BCL6-760 can be used in the research of diffuse Large B-cell Lymphoma (DLBCL) (Pink: BCL-6 ligand (HY-179317); Blue: CRBN ligand (HY-179305); Black: Linker) .
|
-
- HY-B1302
-
|
|
P-glycoprotein
PARP
Caspase
Apoptosis
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Quinidine hydrochloride monohydrate is an orally active antiarrhythmic agent. Quinidine hydrochloride monohydrate reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride monohydrate exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride monohydrate alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride monohydrate can be used in studies related to uterine sarcoma and seizures .
|
-
- HY-W099538R
-
|
Dilauryl 3,3'-Thiodipropionate (Standard)
|
Biochemical Assay Reagents
Reference Standards
|
Others
|
|
Dilauryl thiodipropionate (Standard) is the analytical standard of Dilauryl thiodipropionate. This product is intended for research and analytical applications. Dilauryl thiodipropionate (DLTDP), which is a sulfur-containing antioxidant commonly used to stabilize polymers and plastics against degradation caused by heat, oxygen, and UV light, acts to scavenge free radicals and others that may cause polymer chain scission and cross-linked active substances, in addition, DLTDP has been used as an additive to lubricants, oils and other industrial fluids to improve their oxidation stability, the long hydrocarbon chain in DLTDP makes it low volatility and compatible with many materials and Good compatibility with substrates.
|
-
- HY-D3182
-
|
|
Fluorescent Dye
Aldehyde Dehydrogenase (ALDH)
|
Cancer
|
|
AldeRed 588-A is a fluorescent labeling reagent and a substrate for aldehyde dehydrogenase (ALDH). AldeRed 588-A is metabolized by functionally active ALDH enzymes, thereby specifically labeling viable ALDH bright cell populations with red-shifted fluorescence. AldeRed 588-A supports one-step isolation and sorting of ALDH-expressing cells (including normal stem cells and cancer stem cells), and can be used in combination with green fluorophores for multicolor experimental applications. AldeRed 588-A is widely applicable to research related to various cancers such as bladder cancer, breast cancer, and head and neck cancer .
|
-
- HY-18719A
-
|
|
Estrogen Receptor/ERR
Drug Metabolite
PKC
Akt
Apoptosis
|
Neurological Disease
Cancer
|
|
Endoxifen Z-isomer hydrochloride, an orally active Tamoxifen (HY-13757A) metabolite, is a selective estrogen receptor modulator with 100-fold more potency than its parent agent, Tamoxifen. Endoxifen Z-isomer hydrochloride inhibits PKCβ1 kinase activity. Endoxifen Z-isomer hydrochloride attenuates PKCβ1-activated AKT Ser473 phosphorylation, diminishes AKT substrate phosphorylation, and induces Apoptosis. Endoxifen Z-isomer hydrochloride exhibits anticancer activity against hormone-resistant metastatic breast cancer .
|
-
- HY-18719
-
|
|
Estrogen Receptor/ERR
Drug Metabolite
PKC
Akt
Apoptosis
|
Neurological Disease
Cancer
|
|
Endoxifen Z-isomer hydrochloride, an orally active Tamoxifen (HY-13757A) metabolite, is a selective estrogen receptor modulator with 100-fold more potency than its parent agent, Tamoxifen. Endoxifen Z-isomer inhibits PKCβ1 kinase activity. Endoxifen Z-isomer attenuates PKCβ1-activated AKT Ser473 phosphorylation, diminishes AKT substrate phosphorylation, and induces Apoptosis. Endoxifen Z-isomer exhibits anticancer activity against hormone-resistant metastatic breast cancer .
|
-
- HY-W115674
-
|
|
P-glycoprotein
PARP
Caspase
Apoptosis
Potassium Channel
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Quinidine hydrochloride is an orally active antiarrhythmic agent. Quinidine hydrochloride reduces the expression level of P-gp, inhibits P-gp-mediated efflux, increases the intracellular accumulation of P-gp substrates, induces PARP cleavage and Caspase-3 activation, and elevates the proportion of Apoptotic cells at the sub-G1 phase. Quinidine hydrochloride exerts sustained block and open-channel block effects on IK(f). Quinidine hydrochloride alters the urinary metabolic ratio of Amphetamine, modulates the Pentylenetetrazol-induced seizure threshold, and regulates the anticonvulsant effect of Dextromethorphan. Quinidine hydrochloride can be used in studies related to uterine sarcoma and seizures .
|
-
- HY-162874
-
|
|
STING
IFNAR
|
Cancer
|
|
diABZI-V/C-DBCO is a STING agonist with an EC50 of 1.47 nM. diABZI-V/C-DBCO activates the STING pathway, induces the production of IFN-I, and stimulates the secretion of IFN-β. diABZI-V/C-DBCO serves as a substrate for cathepsin B, and releases active diABZI-amine via cathepsin B-mediated cleavage. In an orthotopic mouse model of breast cancer, diABZI-V/C-DBCO increases serum IFN-β levels and the frequency of granzyme B + CD8 + T cells. diABZI-V/C-DBCO is applicable to research related to triple-negative breast cancer .
|
-
- HY-N1181R
-
-
- HY-126848
-
|
D-1-O-G
|
Drug Metabolite
SOD
COX
Reactive Oxygen Species (ROS)
OAT
|
Inflammation/Immunology
|
|
Diclofenac acyl glucuronide (D-1-O-G) is an orally active glucuronide metabolite of Diclofenac (HY-15036). Diclofenac acyl glucuronide exhibits SOD inhibitory activity, COX-1 inhibitory activity (IC50 = 0.620 μM), and COX-2 inhibitory activity (IC50 = 2.91 μM). Diclofenac acyl glucuronide induces reactive oxygen species (ROS) production and acts as a substrate of OATP2B1. Diclofenac acyl glucuronide induces small intestinal ulcers . Diclofenac acyl glucuronide can be used in research related to intestinal diseases and small intestinal ulcers .
|
-
- HY-A0069A
-
|
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Histamine Receptor
Cytochrome P450
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Neurological Disease
Metabolic Disease
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Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .
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- HY-182019
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HDAC
SHMT
Apoptosis
Reactive Oxygen Species (ROS)
Ferroptosis
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Cancer
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HDAC11-IN-5 is a selective, potent and orally active HDAC11 inhibitor with an IC50 of 0.021 μM. HDAC11-IN-5 increases fatty acylation levels of substrate SHMT2 in AML cells. HDAC11-IN-5 induces apoptosis, G1 phase cell cycle arrest, ferroptosis, ROS production and terminal myeloid differentiation in AML cells. HDAC11-IN-5 demonstrates anti-tumor potency in an MLL-AF9-induced mouse AML model. HDAC11-IN-5 can be used for the research of cancer, such as acute myeloid leukemia .
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- HY-A0069
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Histamine Receptor
Cytochrome P450
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Neurological Disease
Metabolic Disease
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Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
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- HY-103586
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DNA/RNA Synthesis
SARS-CoV
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Infection
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GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
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- HY-162495A
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Drug Isomer
CCR
Calcium Channel
Arrestin
P-glycoprotein
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Inflammation/Immunology
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(S)-IDOR-1117-2520 is the S-isomer of IDOR-1117-2520 (HY-162495). IDOR-1117-2520 is an orally active, potent, selective and reversible CCR6 antagonist. IDOR-1117-2520 antagonizes the CCL20-mediated calcium flow (IC50 = 63 nM) and inhibits β-arrestin recruitment to human CCR6 (IC50 = 30 nM) in cells expressing recombinant human CCR6. IDOR-1117-2520 is found to be a substrate of P-gp/MDR1. IDOR-1117-2520 can be used in the research of autoimmune diseases and skin inflammation .
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- HY-103586A
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DNA/RNA Synthesis
SARS-CoV
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Infection
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GS-441524 hydrochloride is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 hydrochloride competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 hydrochloride inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 hydrochloride reduces viral RNA levels in cats. GS-441524 hydrochloride can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
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- HY-175590
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Dipeptidyl Peptidase
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Metabolic Disease
|
|
DPP-4-IN-17 is an orally active and selective dipeptidyl peptidase-4 (DPP-4) inhibitor with an IC50 value of 0.12 nM. DPP-4-IN-17 increases the enzyme's Km value (75.73 μM vs. 27.18 μM of substrate alone) and reduces catalytic efficiency. DPP-4-IN-17 reduces blood glucose levels and reverses weight loss in Streptozotocin (STZ) (HY-13753)/Nicotinamide (NA) (HY-B0150)-induced diabetic rats. DPP-4-IN-17 can be used for the study of type 2 diabetes mellitus (T2DM) .
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- HY-183147A
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Amino acid Transporter
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Cancer
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LAT1-IN-2 hydrochloride is an orally active anticancer agent, as well as a LAT1 substrate and tubulin-binding agent. LAT1-IN-2 hydrochloride relies on LAT1 for cellular uptake, disrupts microtubule formation by binding to the colchicine site of tubulin, and induces actin depolymerization to transform cells into a spherical shape. LAT1-IN-2 hydrochloride effectively inhibits tumor growth in xenograft mice. Compared with Etoposide (HY-13629), LAT1-IN-2 hydrochloride shows higher distribution in tumor tissues, lower distribution in major organs, and better tolerability. LAT1-IN-2 hydrochloride has been applied in studies related to esophageal cancer .
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- HY-A0069AS
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Isotope-Labeled Compounds
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
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Doxylamine-d5 is deuterium labeled Doxylamine (HY-A0069A). Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .
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- HY-W010991
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FAPGG
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Angiotensin-converting Enzyme (ACE)
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Others
|
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N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
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![N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly](//file.medchemexpress.com/product_pic/hy-w010991.gif)
- HY-182372
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Epoxide Hydrolase
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Neurological Disease
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SH-11037 is a potent inhibitor of soluble epoxide hydrolase (sEH) and docks to the substrate binding cleft in the sEH hydrolase domain. SH-11037 dose-dependently suppresses angiogenesis in the choroidal sprouting assay ex vivo and inhibited ocular developmental angiogenesis in zebrafish larvae. SH-11037 reduces choroidal neovascularisation lesion volume in the laser-induced CNV mouse model. SH-11037 synergises with anti-VEGF treatments in vitro and in vivo. SH-11037 induces G2/M phase blockade and retains retinal endothelial cell viability at active concentrations without overt toxicity. SH-11037 can be used for the research of retinal neovascularization and ocular neovascularization .
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- HY-103586R
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|
|
Reference Standards
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524 (Standard) is the analytical standard of GS-441524 (HY-103586). GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
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- HY-E70631
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PI3K
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Cancer
|
|
PIP5K1A phosphorylates PI4P to synthesize the important signalling phospholipid PI(4,5)P2. This phospholipid also serves as the substrate for PI3K for conversion into PI(3,4,5)P3 to stimulate cell growth and survival. PIP5K1A has been directly implicated in breast cancer and prostate cancer. PIP5K1A Recombinant Human Active Lipid Kinase is a recombinant PIP5K1A protein that can be used to study PIP5K1A-related functions .
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- HY-103586S2
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Isotope-Labeled Compounds
DNA/RNA Synthesis
SARS-CoV
|
Infection
|
|
GS-441524-d is the deuterium labeled GS-441524 (HY-103586). GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
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- HY-153321
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NX-5948; BTK-IN-24
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PROTACs
Btk
|
Inflammation/Immunology
Cancer
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Bexobrutideg (NX-5948) is an orally active chimeric targeting molecule (CTM) that induces specific BTK protein degradation by the cereblon E3 ligase (CRBN) complex without degradation of other cereblon neo-substrates. Bexobrutideg mediates potent anti-inflammatory activity via BTK degradation with resultant inhibition of B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models that contain either wild-type BTK or BTKi-resistant mutations. Bexobrutideg is efficacious in a mouse collageninduced arthritis (CIA) model. Bexobrutideg can cross the blood brain barrier (BBB). Bexobrutideg is a PROTAC composed of the ligand for target protein, a linker, and a cereblon E3 ligase (CRBN) complex (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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- HY-119323
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Fluorescent Dye
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Others
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7-Azido-4-methylcoumarin is a selective coumarin-based fluorescent probe for hydrogen sulfide (H2S). In the presence of H2S, the aromatic azido group of 7-Azido-4-methylcoumarin is selectively reduced to produce the fluorescently active 7-amino-4-methylcoumarin (AMC). 7-Azido-4-methylcoumarin binds to the coumarin/phenol-binding site of BSA, the aglycone-binding site of UGT1A6, and the substrate-binding site of SULT1A1, respectively. 7-Azido-4-methylcoumarin retains its fluorescent properties after covalent binding, acts as a fluorescent H2S probe, and does not react with cysteine, homocysteine or glutathione (Ex/Em = 340/445 nm) .
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- HY-182355
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|
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Methylenetetrahydrofolate Dehydrogenase (MTHFD)
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Cancer
|
|
MTHFD2-IN-7 is an orally active, selective MTHFD2 inhibitor with IC50 values of 0.038 μM and 7.44 μM against human hMTHFD1 and hMTHFD2, respectively. MTHFD2-IN-7 exerts its function by binding to the substrate-binding site of MTHFD2 and maintaining interactions with NAD+. Verified by TSA and DARTS assays, MTHFD2-IN-7 not only binds effectively to the target protein, but also possesses Caco-2 permeability and liver microsomal metabolic stability. MTHFD2-IN-7 exhibits favorable pharmacokinetic properties in mice. MTHFD2-IN-7 also significantly inhibits cancer cell proliferation and reduces tumor volume, and serves as a promising small-molecule tool for acute myeloid leukemia research .
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- HY-17026A
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dFdCTP
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
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- HY-17026E
-
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dFdCTP trisodium
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Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
|
Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate trisodium cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate trisodium shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate trisodium partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate trisodium disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate trisodium can be used for the research of pancreatic cancer and non-small cell lung cancer .
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- HY-A0069S
-
|
|
Isotope-Labeled Compounds
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
|
Doxylamine-d5 succinate is deuterium labeled Doxylamine succinate (HY-A0069A). Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
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-
- HY-159805
-
|
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CDK
|
Cancer
|
|
CDK2-IN-31 is a CCNE1:CDK2 complex inhibitor with an IC50 of 0.13 μM. CDK2-IN-31 binds to a cryptic allosteric pocket at the CCNE1:CDK2 interface, inducing structural rearrangements of the CDK2 A-loop that disrupt the kinase's active conformation and interfere with substrate binding. CDK2-IN-31 inhibits phosphorylation of retinoblastoma protein 1 (RB1) in CCNE1-dependent ovarian cancer cells. CDK2-IN-31 impairs coenrichment of protein PRC1 with CCNE1-N112C:CDK2 complexes. CDK2-IN-31 can be used for the research of ovarian cancer .
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- HY-A0069R
-
|
|
Reference Standards
Histamine Receptor
Cytochrome P450
|
Neurological Disease
Metabolic Disease
|
|
Doxylamine succinate (Standard) is the analytical standard of Doxylamine succinate (HY-A0069). This product is intended for research and analytical applications. Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
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- HY-153321A
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|
(R,R)-NX-5948; (R,R)-BTK-IN-24
|
Drug Isomer
PROTACs
Btk
|
Inflammation/Immunology
Cancer
|
|
(R,R)-Bexobrutideg is the (R,R)-enantiomer of Bexobrutideg (HY-153321). Bexobrutideg (NX-5948) is an orally active PROTAC that induces specific BTK protein degradation via a cereblon E3 ligase (CRBN) complex without degrading other cereblon neo substrates. Bexobrutideg mediates potent anti-inflammatory activity through BTK degradation, thereby inhibiting B cell activation. Bexobrutideg exhibits potent tumor growth inhibition in TMD8 xenograft models containing wild-type BTK or BTKi resistance mutations. Bexobrutideg is effective in a mouse model of collagen-induced arthritis (CIA). Bexobrutideg can cross the blood-brain barrier. NX-5948 consists of a target protein ligand, a linker, and a VHL E3 ubiquitin ligase (Red: BTK ligand (HY-170324); Blue: CRBN ligand (HY-171893); Black: linker) .
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- HY-13687A
-
|
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IKK
LRRK2
P-glycoprotein
PKD
NF-κB
TNF Receptor
Interleukin Related
|
Cardiovascular Disease
Inflammation/Immunology
|
|
IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway .
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- HY-13687
-
IKK 16
Maximum Cited Publications
29 Publications Verification
|
IKK
LRRK2
P-glycoprotein
PKD
NF-κB
TNF Receptor
Interleukin Related
|
Cardiovascular Disease
Inflammation/Immunology
|
|
IKK 16 is an orally active IKK inhibitor. IKK 16 shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway .
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- HY-183118
-
|
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CDK
Apoptosis
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Neurological Disease
Cancer
|
|
CID-078 is an orally active macrocyclic cyclin A and cyclin B inhibitor. CID-078 binds cyclin hydrophobic patches, disrupting interactions of cyclin A-Cdk2 with E2F1 and cyclin B-Cdk1 with Myt1, and selectively targets RxL binding motifs to block complex-substrate interactions. CID-078 induces DNA damage, G2/M cell cycle arrest, apoptosis, mitotic catastrophe, spindle assembly checkpoint activation, and neomorphic cyclin B-CDK2 complex formation, driving synthetic lethality in E2F-driven cancer cells. CID-078 can be used for the research of small cell lung cancer, non-small cell lung cancer, triple negative breast cancer, advanced solid tumors, luminal HR +/HER 2- breast cancer, RB1-altered solid tumors, and neuroblastoma .
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-
- HY-13687R
-
|
|
IKK
LRRK2
Reference Standards
P-glycoprotein
PKD
NF-κB
TNF Receptor
Interleukin Related
|
Inflammation/Immunology
|
|
IKK 16 (Standard) is the analytical standard of IKK 16. This product is intended for research and analytical applications. IKK 16 hydrochloride is an orally active IKK inhibitor. IKK 16 hydrochloride shows IC50s of 40 nM, 70 nM, 200 nM, and 50 nM for IKK2, IKK complex, IKK1, and LRRK 2, respectively. IKK 16 hydrochloride is also a pan-PKD inhibitor, inhibiting PKD1, PKD2, and PKD3 with IC50s of 153.9, 115, and 99.7 nM, respectively. IKK 16 hydrochloride is also an ABCB1 inhibitor, interfering with the binding of ABCB1 to its substrates. IKK 16 hydrochloride protects against LPS (HY-D1056)-induced multiple organ dysfunction by reducing the acute inflammatory response induced by endotoxin exposure. IKK 16 hydrochloride can restore renal function and alleviate fibrosis in acute kidney injury. IKK 16 hydrochloride attenuates cardiac dysfunction associated with polymicrobial sepsis in mice with type 2 diabetes mellitus (T2DM) by inhibiting the NF-κB pathway.
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- HY-16265A
-
|
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Ephrin Receptor
PDGFR
VEGFR
|
Cancer
|
|
JI-101 hydrochloride is an orally active angiogenesis inhibitor and anticancer agent with 55% oral bioavailability in Sprague Dawley rats, high permeability, and no P-gp substrate activity .JI-101 hydrochloride modulates angiogenesis signaling pathways in tumor vessel beds, downregulates EphB4, targets EphB4, VEGFR-2, and PDGFR-β, and inhibits multiple stages of tumor angiogenesis .JI-101 hydrochloride exerts activity against cancer cells and xenografts, exhibits mild to moderate inhibition of CYP3A4, and shows stability in pre-clinical and human liver microsomes .JI-101 hydrochloride undergoes rapid oral absorption in Sprague Dawley rats, has extensive tissue distribution with preferred lung uptake, and is excreted via bile with mono- and di-hydroxy metabolites, with feces as the primary elimination route .JI-101 hydrochloride can be used for the research of ovarian cancer and solid tumors .
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- HY-W039897
-
|
α-Methyl-D-mannoside
|
Environmental Pollutants
Bacterial
|
Infection
|
|
Methyl α-D-mannopyranoside (α-Methyl-D-mannoside) is a methyl glycoside derivative and conformational stabilizer of α-D-mannopyranose. The glycosidic bond conformation of Methyl α-D-mannopyranoside is significantly affected by the environment. In aqueous solution, Methyl α-D-mannopyranoside stabilizes into a trans conformation via intermolecular hydrogen bonds; in the gas phase, however, steric interactions drive Methyl α-D-mannopyranoside to prefer a clockwise gauche conformation. Methyl α-D-mannopyranoside also serves as a major component of secondary cell wall polymers in some bacteria and an active precursor site for virus-targeted glycoproteins. Methyl α-D-mannopyranoside acts as an acceptor substrate for alternansucrase, mediating the transfer of D-glucopyranosyl groups to generate a variety of glycosylated oligosaccharide products, with methyl α-D-glucopyranosyl-(1→6)-α-D-mannopyranoside as the main component. Methyl α-D-mannopyranoside is applicable to studies on bacterial pathogenic mechanisms associated with mannose-specific fimbrial lectins .
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-
- HY-W021016
-
|
(S,S)-Ph-BPE
|
Biochemical Assay Reagents
|
Others
|
|
(+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane ((S,S)-Ph-BPE) is a chiral bisphosphine ligand and catalyst. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane acts as a chiral ligand in rhodium-catalyzed reductive hydroformylation of alkenyl boronic esters, enabling enantiodivergent synthesis of chiral γ-boryl alcohols. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane forms chiral nickel-phosphine complexes to mediate asymmetric hydrogenation of aliphatic γ- and δ-keto acids; protons promote substrate C=O bond activation and stereoselectivity control via hydrogen bonding. (+)-1,2-Bis ((2S,5S)-2,5-diphenylphospholano)ethane forms a monodentate nickel complex, which serves as the active species for asymmetric hydrogenation of aliphatic keto acids .
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- HY-162275
-
|
|
Histone Demethylase
Histone Methyltransferase
STAT
|
Cancer
|
|
JMJD1C-IN-1 is an orally active and selective inhibitor of JMJD1C (IC50 = 0.59 μM, Kd = 1.96 μM). JMJD1C-IN-1 inhibits the binding of JMJD1C to H3K9me2 peptide substrate in the HTRF assay (IC50 = 1.47 μM). JMJD1C-IN-1 disrupts intratumoral regulatory T (Treg) cell fitness by dual mechanisms: promoting H3K9me2 accumulation to downregulate PD1 expression and reducing STAT3 demethylation to enhance STAT3 activation. JMJD1C-IN-1 demonstrates dose-dependent antitumor efficacy in multiple mouse tumor models (MCA205 fibrosarcoma, B16-F10 melanoma, LLC lung cancer, Hepa1-6 hepatocellular carcinoma, CT26 colorectal cancer). JMJD1C-IN-1 can be used for the study of tumor immunotherapy by selectively targeting intratumoral Treg cells .
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- HY-109061A
-
|
YH25448 mesylate hydrate; GNS-1480 mesylate hydrate
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
|
Cancer
|
|
Lazertinib (YH25448; GNS-1480) mesylate hydrate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate hydrate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate hydrate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate hydrate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate hydrate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
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- HY-109061B
-
|
YH25448 mesylate; GNS-1480 mesylate
|
TRP Channel
EGFR
Akt
ERK
Apoptosis
|
Cancer
|
|
Lazertinib (YH25448; GNS-1480) mesylate is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib mesylate exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib mesylate induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib mesylate competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib mesylate is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
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- HY-109061
-
|
YH25448; GNS-1480
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (YH25448; GNS-1480) is an orally active, blood-brain barrier permeable third-generation EGFR tyrosine kinase inhibitor, as well as an ABCB1/ABCG2 inhibitor and a TRPA1 activator. Lazertinib exhibits IC50 values of 0.4 mM and 0.2 mM against human ABCB1 and ABCG2, respectively. By inhibiting mutant EGFR signaling, EGFR phosphorylation and the downstream ERK/AKT pathway, as well as upregulating surface expression of EGFR/MET, Lazertinib induces cell cycle arrest, apoptosis, spontaneous calcium responses, hyperexcitability of dorsal root ganglion (DRG) neurons, and TRPA1-dependent pain-like behaviors. Lazertinib competitively binds to the substrate-binding sites of ABCB1/ABCG2, stimulates their ATPase activity without altering their expression or plasma membrane localization, thereby enhancing ADCC activity, acting as a chemosensitizer, and reversing ABCB1-mediated multidrug resistance. It exerts antitumor activity as a single agent or in combination with other drugs. Lazertinib is applicable to research related to non-small cell lung cancer, multidrug-resistant cancers, and paresthesia .
|
-
- HY-170524
-
|
|
SARS-CoV
DNA Methyltransferase
Cytochrome P450
|
Infection
|
|
TDI-015051 is a highly selective, orally active antiviral agent that targets the coronavirus NSP14 guanine-N7 methyltransferase. TDI-015051 binds to substrates in a non-competitive manner and forms a stable ternary complex, precisely blocking the capping and methylation processes of viral mRNA. TDI-015051 potently inhibits a variety of coronaviruses (including SARS-CoV-2 and MERS). By impairing viral replication and translation and inducing a moderate type I interferon-mediated immune response, it significantly reduces pulmonary viral load and exhibits a synergistic effect with Nirmatrelvir (HY-138687). In addition, TDI-015051 does not inhibit non-coronavirus methyltransferases, and the drug-resistant mutations it induces impair viral fitness, demonstrating excellent antiviral properties and safety. TDI-015051 can be used for research on COVID-19 and the replication mechanism of coronaviruses .The IC50 values of TDI-015051 against SARS-CoV-2, α-hCoV-NL63, α-hCoV-229E, β-hCoV-MERS are 0.15 nM, 1.7 nM, 2.6 nM and 3.6 nM, respectively, and the Ka value against SARS-CoV-2 is 0.061 nM .
|
-
- HY-W657887
-
|
|
Histone Methyltransferase
GSK-3
Tau Protein
Amyloid-β
Glucocorticoid Receptor
Androgen Receptor
Adrenergic Receptor
|
Neurological Disease
|
|
GSK-3β/G9a-IN-1 (Compound T2) is an orally active, selective, blood-brain-barrier permeable, competitive G9a (substrate-competitive, IC50: 1.1 μM) and GSK-3β (ATP competitive, IC50: 0.8 μM) inhibitor. GSK-3β/G9a-IN-1 is a potent H3K9me2 inhibitor that reshapes chromatin landscape. GSK-3β/G9a-IN-1 lowers tau phosphorylation, reduces Aβ aggregation. GSK-3β/G9a-IN-1 displays inhibition toward glucocorticoid receptor, androgen receptor, and alpha-2A adrenergic receptor. GSK-3β/G9a-IN-1 also upregulates SAGA complex members such as Eny2 and Sgf29. GSK-3β/G9a-IN-1 markedly improves memory, restores social behaviors, and increases synaptic complexity in late-onset Alzheimer’s disease .
|
-
- HY-172368
-
|
|
PROTACs
Histone Methyltransferase
IKZF Family
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
PROTAC CARM1/IKZF3 degrader-1 (Compound 074) inhibits CARM1, reduces the methylation level of its substrate BAF155. PROTAC CARM1/IKZF3 degrader-1 is the PROTAC degrader for IKZF 1/3 through a CRBN-dependent pathway. PROTAC CARM1/IKZF3 degrader-1 inhibits the expression of MYC protein, thereby inhibiting the proliferation of a variety of multiple myeloma cells. PROTAC CARM1/IKZF3 degrader-1 induces apoptosis in cell H929. PROTAC CARM1/IKZF3 degrader-1 overcomes immunomodulatory drugs (IMiD, such as pomalidomide) resistance. PROTAC CARM1/IKZF3 degrader-1 can be used in cancer and immunology research . (Pink: ligand for target protein CARM1/IKZF3 ligand 1 (HY-172369); Active form of target protein ligand: EZM 2302 (HY-111109); Black: linker (HY-21999); Blue: ligand for E3 ligase Cereblon Thalidomide 4-fluoride (HY-41547))
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-W010991
-
|
FAPGG
|
Fluorescent Dyes
|
|
N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
|
-
- HY-W127711
-
|
|
Fluorescent Dyes
|
Fast Blue B Salt, Dye content ~95% is a diazo dye, primarily used as a chromogenic substrate in biochemical analysis. Fast Blue B Salt, Dye content ~95% is the coupling agent for the histochemical demonstration of proteases. Fast Blue B Salt, Dye content ~95% can be used for the detection of acid phosphatase in Clostridium perfringens, and also for the determination of lipase activity. Fast Blue B Salt, Dye content ~95% reacts directly with the active hydroxyl groups in phenolic compounds to determine the content of phenolic substances .
|
-
- HY-131131
-
|
|
Fluorescent Dyes
|
|
5-CFDA-AM is a cell-permeable esterase substrate that can be used as an active probe to measure enzyme activity and cell membrane integrity. 5-CFDA-AM is electroneutral and can enter the cell at a lower concentration than CFDA, where it is hydrolysed by intracellular esterases to produce carboxyfluorescein, which contains an additional negative charge and can be better retained in the cell. 5-CFDA-AM can be used to detect cell viability .
|
-
- HY-D1686
-
|
Biotin-16-UTP tetralithium
|
Fluorescent Dyes
|
|
Biotin-16-UTP is an active substrate for RNA polymerase. Biotin-16-UTP can replace UTP in the in vitro transcription reaction for RNA labeling .
|
-
- HY-D1584
-
|
|
Fluorescent Dyes
|
|
C12 NBD sphingomyelin is an active derivative of Sphingomyelin (HY-113498) that is tagged with fluorescent C12 nitrobenzoxadiazole (C12 NBD). C12 NBD sphingomyelin can be used as a sphingomyelinase substrate for studying the metabolism and transport of sphingomyelins (Ex=470 nm, Em=525 nm) .
|
-
- HY-D1686B
-
|
|
Fluorescent Dyes
|
|
Biotin-16-UTP tetrasodium is an active substrate for RNA polymerase. Biotin-16-UTP tetrasodium can replace UTP in the in vitro transcription reaction for RNA labeling .
|
-
- HY-D1460
-
|
|
Fluorescent Dyes
|
|
Fluorescein Di-β-D-Glucuronide is an orally active fluorescent probe substrate and an indicator of β-glucuronidase (βG) activity in intestinal bacteria. Fluorescein Di-β-D-Glucuronide can be used for non-invasive time-lapse optical imaging of βG activity in intestinal bacteria in nude mice. Fluorescein Di-β-D-Glucuronide supports the quantitative analysis of bacterial βG enzyme activity and inhibition .
|
-
- HY-137834A
-
|
|
Fluorescent Dyes
|
|
Gly-Pro-AMC is a biological active peptide. (This is a fluorescent dipeptidylaminopeptidase IV substrate, Abs/Em=353/442 nm.)
|
-
- HY-D1575
-
|
|
Fluorescent Dyes
|
|
C6 NBD galactosylceramide is an active derivative of galactosylceramide that is tagged with fluorescent C6 nitrobenzoxadiazole (C6 NBD). C6 NBD galactosylceramide can be used as a substrate for neutral β-glycosylceramidase (GCase) to study intracellular localization and metabolism of galactosylceramide (Ex=nm, Em=525) .
|
-
- HY-D3182
-
|
|
Fluorescent Dyes
|
|
AldeRed 588-A is a fluorescent labeling reagent and a substrate for aldehyde dehydrogenase (ALDH). AldeRed 588-A is metabolized by functionally active ALDH enzymes, thereby specifically labeling viable ALDH bright cell populations with red-shifted fluorescence. AldeRed 588-A supports one-step isolation and sorting of ALDH-expressing cells (including normal stem cells and cancer stem cells), and can be used in combination with green fluorophores for multicolor experimental applications. AldeRed 588-A is widely applicable to research related to various cancers such as bladder cancer, breast cancer, and head and neck cancer .
|
| Cat. No. |
Product Name |
Type |
-
- HY-B2228
-
|
|
Biochemical Assay Reagents
|
|
Proteinase, Aspergillus oryzae is a serine protease that hydrolyzes peptide bonds in protein substrates, preferring alkaline conditions (optimal pH 10.5). It efficiently degrades casein, poly-L-glutamic acid, and poly-L-lysine, with activity irreversibly inhibited by diisopropylfluorophosphate (DFP) and potato inhibitor. This enzyme catalyzes proteolysis via serine residues in its active site, finding applications in food processing (e.g., soy sauce fermentation), detergents, and leather industries due to its high yield in solid-state fermentation and cost-effective production.
|
-
- HY-W127711
-
|
|
Biochemical Assay Reagents
|
Fast Blue B Salt, Dye content ~95% is a diazo dye, primarily used as a chromogenic substrate in biochemical analysis. Fast Blue B Salt, Dye content ~95% is the coupling agent for the histochemical demonstration of proteases. Fast Blue B Salt, Dye content ~95% can be used for the detection of acid phosphatase in Clostridium perfringens, and also for the determination of lipase activity. Fast Blue B Salt, Dye content ~95% reacts directly with the active hydroxyl groups in phenolic compounds to determine the content of phenolic substances .
|
-
- HY-134136A
-
|
|
Biochemical Assay Reagents
|
|
Octanoyl coenzyme A lithium is an enoyl-CoA hydratase binder. Octanoyl coenzyme A lithium binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
|
-
- HY-W115752
-
|
Diamine sulfate (99%)
|
Biochemical Assay Reagents
|
|
Hydrazine sulfate is an orally active PEPCK inhibitor. Hydrazine sulfate inhibits PEPCK and low-Km ALDH. Hydrazine sulfate impairs gluconeogenesis and enhances the protective effect of energy substrates against MPP + toxicity. Hydrazine sulfate exacerbates liver damage in rats when combined with Ethanol. Hydrazine sulfate can be used in the research of shock, non-small cell lung cancer, colorectal cancer and Parkinson's disease .
|
-
- HY-W099538
-
|
Dilauryl 3,3'-Thiodipropionate
|
Biochemical Assay Reagents
|
|
Dilauryl thiodipropionate (DLTDP), which is a sulfur-containing antioxidant commonly used to stabilize polymers and plastics against degradation caused by heat, oxygen, and UV light, acts to scavenge free radicals and others that may cause polymer chain scission and cross-linked active substances, in addition, DLTDP has been used as an additive to lubricants, oils and other industrial fluids to improve their oxidation stability, the long hydrocarbon chain in DLTDP makes it low volatility and compatible with many materials and Good compatibility with substrates.
|
-
- HY-167805
-
|
|
Biochemical Assay Reagents
|
|
D-Glucose 6-phosphate potassium is a biologically active compound that has the activity of being a substrate for glucose-6-phosphate isomerase. D-Glucose 6-phosphate potassium can participate in the sugar metabolism process and promote the production and utilization of energy in cells.
|
-
- HY-W002801
-
|
|
Biochemical Assay Reagents
|
|
2-Benzyloxyphenylboronic acid is a biochemical reagent that can be used as a biological material or organic compound for life science related research. 2-Benzyloxyphenylboronic acid is also a substrate used in asymmetric Suzuki coupling reactions. 2-Benzyloxyphenylboronic acid can be utilized in the synthesis of other active compounds .
|
-
- HY-134423
-
|
Stearoyl-CoA lithium
|
Biochemical Assay Reagents
|
|
Stearoyl coenzyme A (Stearoyl-CoA) lithium is an active compound that can be used as a substrate for the determination of stearoyl-Coenzyme desaturase in microsomes .
|
-
- HY-W283888
-
|
|
Biochemical Assay Reagents
|
|
5-Bromo-4-chloro-1H-indol-3-yl nonanoate is a fluorescent substrate used to detect enzymes. The substrate reacts with various enzymes to produce a fluorescent product, which has been shown to be active against β-galactosidase, α-chymotrypsin, and β-glucuronidase.
|
-
- HY-137854
-
|
|
Biochemical Assay Reagents
|
|
Naphthol AS-BI N-acetyl-β-D-glucosaminide acts as a substrate and reacts directly with N-acetyl-β-glucosaminidase enzyme. Naphthol AS-BI N-acetyl-β-D-glucosaminide can detect and localize the active region of N-acetyl-β-glucosaminidase enzyme visually .
|
-
- HY-134136
-
|
|
Biochemical Assay Reagents
|
|
Octanoyl coenzyme A is an enoyl-CoA hydratase binder. Octanoyl coenzyme A binds to the active site of enoyl-CoA hydratase, occupies the binding pocket for the fatty acid tail of the enzyme's substrate, and induces a conformational shift in a flexible protein loop via its longer octanoyl chain, forming an open channel leading to the inter-trimer gap .
|
-
- HY-W099538R
-
|
Dilauryl 3,3'-Thiodipropionate (Standard)
|
Biochemical Assay Reagents
|
|
Dilauryl thiodipropionate (Standard) is the analytical standard of Dilauryl thiodipropionate. This product is intended for research and analytical applications. Dilauryl thiodipropionate (DLTDP), which is a sulfur-containing antioxidant commonly used to stabilize polymers and plastics against degradation caused by heat, oxygen, and UV light, acts to scavenge free radicals and others that may cause polymer chain scission and cross-linked active substances, in addition, DLTDP has been used as an additive to lubricants, oils and other industrial fluids to improve their oxidation stability, the long hydrocarbon chain in DLTDP makes it low volatility and compatible with many materials and Good compatibility with substrates.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-W010991
-
|
FAPGG
|
Angiotensin-converting Enzyme (ACE)
|
Others
|
|
N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly (FAPGG) is a specific substrate of angiotensin converting enzyme (ACE) with a Ki of 2.546×10 -4 M. It is used as a chromogenic probe for quantitative detection of ACE activity. N-[3-(2-Furyl)acryloyl]-Phe-Gly-Gly can be hydrolyzed by ACE to generate N-[3-(2-furyl)acryloyl]-Phe (FAP) and Gly-Gly, and the ACE inhibitory effect is monitored by photometry. FAPGG competitively binds to the active center of ACE and is a key tool for screening ACE inhibitors such as Captopril (HY-B0368) and Dioscorin. Its reversible mechanism of action supports hypertension research and drug development targeting the renin-angiotensin system .
|
-
- HY-P4931
-
|
|
MMP
|
Cancer
|
|
Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 (FS-6) is a fluorescent peptide that is a quenched MMP peptide substrate. Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 can be used for real-time quantification of MMP enzymatic activity. Mca-Lys-Pro-Leu-Gly-Leu-Dap(Dnp)-Ala-Arg-NH2 is an elongated peptide of MMP substrate (FS-1) and is active against collagenases (MMP-1, MMP-8, MMP-13 ) and MT1-MMP with higher specificity constants than FS-1 . (Ex/Em=325 nm/400 nm)
|
-
- HY-P10605
-
|
|
Akt
GSK-3
|
Cancer
|
|
GSK3β-peptide is a substrate mimetic peptide of glycogen synthase kinase 3-β (GSK3-β) that can bind to the active site of GSK3-β and mimic the behavior of a real substrate. GSK3β-peptide can be used to develop substrate mimetic inhibitors of Akt as potential anticancer drugs .
|
-
- HY-P5353
-
|
IKVAV sequence; Laminin A-chain fragment
|
Peptides
|
Others
|
|
PA22-2 (IKVAV sequence; Laminin A-chain fragment) is a biological active peptide. (This peptide is derived from mouse laminin a1 . Cell matrix substrate constituted with this peptide can promote neurite outgrowth.)
|
-
- HY-P5376
-
|
S-2586
|
Ser/Thr Protease
|
Others
|
|
MeOSuc-Arg-Pro-Tyr-pNA (S-2586) is a biological active peptide. (chymotrypsin substrate)
|
-
- HY-P5481
-
|
|
Peptides
|
Others
|
|
DABCYL-LPETG-EDANS is a biological active peptide. (This 5-amino acid peptide is a sortase substrate, C-terminal sorting signal. Sortase cleaves surface proteins at the LPXTG motif and catalyzes the formation of an amide bond between the carboxyl group of threonine and the amino group of cell-wall crossbridges. Sortases are a family of Gram-positive transpeptidases responsible for anchoring surface protein virulence factors to the peptidoglycan cell wall layer. Cleavage of this FRET substrate by sortase reveals the fluorescent signal, Abs/Em = 340/490 nm.)
|
-
- HY-P10422A
-
|
ML-peptide, Multi-Leucine (ML)-peptide triacetate
|
Autophagy
|
Cancer
|
|
Multi-Leu peptide (ML-peptide) triacetate is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide triacetate can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide triacetate can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
|
-
- HY-P5438
-
|
|
Btk
c-Kit
FAK
FLT3
Insulin Receptor
|
Others
|
|
Srctide is a biological active peptide. (This is a peptide substrate for many protein kinases, such as Blk, BTK, cKit, EPHA1, EPHB2, EPHB3, ERBB4, FAK, Flt3, IGF-1R, ITK, Lck, MET, MUSK, Ret, Src, TIE2, TrkB, VEGF-R1 (Flt-1) and VEGF-R2 (KDR).)
|
-
- HY-P5375
-
|
|
Peptides
|
Others
|
|
O-Linked GlcNAc transferase substrate is a biological active peptide. (A peptide substrate of O-linked GlcNAc transferase (OGT), a eukaryotic glycosyltransferase that uses UDP-GlcNAc as a glycosyl donor.)
|
-
- HY-P5432
-
|
IRAK-1 (360-380)
|
IRAK
|
Others
|
|
IRAK-4 Peptide substrate (IRAK-1 (360-380)) is a biological active peptide. (This is a substrate peptide for Interleukin-1 Receptor-Associated Kinase (IRAK) 4)
|
-
- HY-P10042
-
|
|
Ribosomal S6 Kinase (RSK)
|
Others
|
|
S6K Substrate is a substrate for active protein kinases, including CLK2, MRCKalpha, MRCKbeta, p70S6K, ROCK1, ROCK2, RSK1, RSK3, PIM1 .
|
-
- HY-P5426
-
|
|
Bcr-Abl
|
Others
|
|
Abl protein tyrosine kinase substrate is a biological active peptide. (Abltide is a peptide substrate for Abl Kinase (Abl protein tyrosine kinase), a partner in the gag-Abl fusion protein of the Abelson murine leukemia virus. Used in Western blot and kinase assay.)
|
-
- HY-P5348
-
|
|
Peptides
|
Others
|
|
Ac-LEHD-pNA is a biological active peptide. (Caspase-9 substrate; pNA (4-nitroaniline)-derived caspase substrates are widely used for the colorimetric detection of various caspase activities. Cleavage of pNA peptides by caspases generates pNA that is monitored colorimetrically at ~405 nm. pNA has maximum absorption around 408 nm.)
|
-
- HY-P5430
-
|
|
DYRK
|
Others
|
|
DYRKtide is a biological active peptide. (Dyrktide is designed as the optimal substrate sequence efficiently phosphorylated by DYRK1A, which is a dual-specificity protein kinase that is thought to be involved in brain development.)
|
-
- HY-P0320
-
|
|
Phosphatase
|
Others
|
|
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
|
-
- HY-P5431
-
|
|
Insulin Receptor
|
Others
|
|
Insulin receptor (1142-1153), pTyr1150 is a biological active peptide. (Peptide used as insulin receptor tyrosine kinase substrate.)
|
-
- HY-P5529
-
|
|
Peptides
|
Others
|
|
2Abz-GLQRALEI-Lys(Dnp)-NH2 is a biological active peptide. (C4 P4-P4′ substrate)
|
-
- HY-W436471
-
|
|
Peptides
|
Others
|
|
H-Ala-Pro-AFC is a biological active peptide. (This is a fluorescent peptide, Abs/Em=380/500nm. It is a substrate for dipeptidyl peptidase IV (DPP IV) and Xaa-Pro dipeptidase.)
|
-
- HY-P5429
-
|
|
Peptides
|
Others
|
|
DNA-PK Substrate is a biological active peptide. (A substrate for DNA-dependent protein kinase (DNA-PK), phosphorylation. DNA-PK is essential for the repair of DNA double-strand breaks. This peptide corresponding to 11–24 amino acids of human p53 with threonine 18 and serine 20 changed to alanine is used as a substrate for the assay of DNA-PK activityPyroglutamyl (pGlu) peptides may spontaneously form when either Glutamine (Q) or Glutamic acid (E) is located at the sequence N-terminus. The conversion of Q or E to pGlu is a natural occurrence and in general it is believed that the hydrophobic γ-lactam ring of pGlu may play a role in peptide stability against gastrointestinal proteases. Pyroglutamyl peptides are therefore considered a normal subset of such peptides and are included as part of the peptide purity during HPLC analysis.)
|
-
- HY-P5435
-
|
|
Ser/Thr Kinase
|
Others
|
|
LKBtide is a biological active peptide. (This is a peptide substrate that is phosphorylated by Serine/Threonine kinase 11 (STK11), also known as LKB1. LKBtide is derived from sucrose non-fermenting 1 (SNF1) protein kinase, which is normally activated by the LKB1/AMP-activated protein kinase (AMPK) signaling pathway.)
|
-
- HY-145779
-
|
H-γ-Glu-Met-OH; γ-Glu-Met
|
Dipeptidyl Peptidase
|
Metabolic Disease
|
|
H-Glu(Met-OH)-OH (H-γ-Glu-Met-OH; γ-Glu-Met) is a DPP-IV inhibitor with an IC50 of 2.11 mM. H-Glu(Met-OH)-OH binds to DPP-IV’s active site to block substrate binding. H-Glu(Met-OH)-OH can be used for the research of type 2 diabetes .
|
-
- HY-P2668
-
|
|
Peptides
|
Others
|
|
Cdk5 Substrate is a biological active peptide. (substrate for the cdc2 protein kinase)
|
-
- HY-P5450
-
|
|
PDK-1
|
Others
|
|
PDKtide, a biological active peptide is a substrate for Phosphatidylinositide-Dependent Kinase 1 (PDK1) .
|
-
- HY-P3477
-
|
|
Fluorescent Dye
|
Others
|
|
Mca-PLA-Nva-Dap(Dnp)-AR-NH2 is a fluorogenic substrate for matrix metalloproteinase-2 (MMP-2) .
|
-
- HY-P5450A
-
|
|
PDK-1
|
Others
|
|
PDKtide TFA, a biological active peptide, is a substrate for phosphatidylinositide-dependent kinase 1 (PDK1) .
|
-
- HY-137834A
-
-
- HY-P5374
-
|
|
Elastase
|
Others
|
|
MeOSuc-AAPV-AFC is a biological active peptide. (A highly specific neutrophil elastase substrate, Abs/Em=380/500 nm.)
|
-
- HY-P5433
-
|
|
Peptides
|
Others
|
|
IRS1-derived peptide is a biological active peptide. (This is a peptide fragment (979-989) of the insulin receptor substrate-1 containing the sequence motif YMXM known to bind to the two domains of SH2 on the 85kDa subunit of phosphoinositide 3-kinase.)
|
-
- HY-P5355
-
|
|
Fluorescent Dye
|
Others
|
|
Z-Gly-Gly-Arg-AFC is a biological active peptide. (Plasminogen Activator Acrosine Substrate, fluorescent Z-Gly-Gly-Arg-AFC)
|
-
- HY-P0266B
-
|
Ac-SdKP acetate
|
Angiotensin-converting Enzyme (ACE)
|
Inflammation/Immunology
|
|
N-Acetyl-Ser-dAsp-Lys-Pro (Ac-SdKP) acetate is a specific substrate for the N-terminal active site of angiotensin-converting enzyme (ACE). N-Acetyl-Ser-dAsp-Lys-Pro acetate is a natural inhibitor of pluripotent hematopoietic stem cell proliferation. Anti-inflammatory and antifibrotic properties .
|
-
- HY-P11302
-
|
|
CHIKV
Virus Protease
|
Infection
|
|
DABCYL-RAGGYIFS-(E-EDANS)-NH2, an octapeptide, is a FRET-based substrate peptide of CHIKV nsP2protease with highly sensitivity. DABCYL-RAGGYIFS-(E-EDANS)-NH2 can be cleaved by the active CHIKV nsP2protease, separating fluorophore and quencher and resulting in an increase of fluorescence signal. DABCYL-RAGGYIFS-(E-EDANS)-NH2 can used for the determination of CHIKV nsP2protease activity .
|
-
- HY-P5507
-
|
Erktide
|
Peptides
|
Others
|
|
ERK2 Substrate (Erktide) is a biological active peptide. (Erktide is a peptide substrate for ERK2 (extracellular regulated protein kinase 2) whose activity is regulated by mitogenic stimuli.)
|
-
- HY-P5434
-
|
JAK3 Peptide substrate
|
JAK
|
Others
|
|
Jak3tide (JAK3 Peptide substrate) is a biological active peptide. (This peptide is a substrate for Jak3. It may be used used in kinase assays. Jak3tide contains the phosphorylation site at Tyr7.)
|
-
- HY-P10042A
-
|
|
Ribosomal S6 Kinase (RSK)
|
Others
|
|
S6K Substrate acetate is a substrate for active protein kinases, including CLK2, MRCKalpha, MRCKbeta, p70S6K, ROCK1, ROCK2, RSK1, RSK3, PIM1 .
|
-
- HY-P1906
-
|
|
CDK
|
Neurological Disease
|
|
[pThr3]-CDK5 Substrate is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM .
|
-
- HY-P5440
-
|
|
ERK
|
Others
|
|
ERKtide is a biological active peptide. (ERKtide is a peptide substrate for ERK2. Extracellular regulated protein kinase 2 (ERK2) is a eukaryotic protein kinase whose activity is regulated by mitogenic stimuli.)
|
-
- HY-P5377
-
|
Cathepsin K substrate
|
Ser/Thr Protease
|
Others
|
|
Abz-HPGGPQ-EDDnp (Cathepsin K substrate) is a biological active peptide. (Cathepsins are a class of globular lysosomal proteases, playing a vital role in mammalian cellular turnover. They degrade polypeptides and are distinguished by their substrate specificities. Cathepsin K is the lysosomal cysteine protease involved in bone remodeling and resorption. It has potential as a drug target in autoimmune diseases and osteoporosis.This FRET peptide can be used to monitor selectively cathepsin K activity in physiological fluids and cell lysates. Abz-HPGGPQ-EDDnp [where Abz represents o-aminobenzoic acid and EDDnp represents N -(2, 4-dinitrophenyl)-ethylenediamine], a substrate initially developed for trypanosomal enzymes, is efficiently cleaved at the Gly-Gly bond by cathepsin K. This peptide is resistant to hydrolysis by cathepsins B, F, H, L, S and V, Ex/Em=340 nm/420 nm.)
|
-
- HY-P10422
-
|
ML-peptide, Multi-Leucine (ML)-peptide
|
Autophagy
|
Cancer
|
|
Multi-Leu peptide (ML-peptide) is a potent inhibitor of PACE4 (Ki=22 nM). Multi-Leu peptide can competitively bind to the active site of PACE4 by simulating the substrate sequence of PACE4, thereby inhibiting its catalytic activity. Multi-Leu peptide can be used to study the specific mechanism of PACE4 in the development of prostate cancer .
|
-
- HY-P5525
-
|
Autocamtide-3 Derived Inhibitory Peptide
|
CaMK
|
Others
|
|
AC3-I, myristoylated is a biological active peptide. (This is a myristoylated form of Autocamtide-3-Derived Inhibitory Peptide (AC3-I), a highly specific inhibitor of Calmodulin-Dependent Protein Kinase ll (CaMKII) that is resistant to proteolysis. AC3-I is derived from Autocamtide-3, a substrate for CaMKII, with the Thr-9 phosphorylation site substituted with Ala.)
|
-
- HY-P5447
-
|
|
Phosphatase
|
Others
|
|
RRLIEDAEpYAARG is a biological active peptide. (Phosphatase substrate.)
|
-
- HY-P5449
-
-
- HY-P5428
-
|
|
CDK
|
Others
|
|
Cdc2 kinase substrate is a biological active peptide. (The native peptide HATPPKKKRK is a substrate for cyclin-dependent protein kinase 1 (CDC2; CDK1).)
|
-
- HY-P0320B
-
|
|
Phosphatase
Biochemical Assay Reagents
|
Others
|
|
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
|
-
- HY-P0320A
-
|
|
Phosphatase
Biochemical Assay Reagents
|
Others
|
|
EGF Receptor Substrate 2 (Phospho-Tyr5) acetate, a biologically active peptide, is a tyrosine phosphate substrate. EGF Receptor Substrate 2 (Phospho-Tyr5) acetate can be used to detect protein tyrosine phosphatases activity .
|
-
- HY-P5385
-
|
|
Angiotensin Receptor
|
Others
|
|
Renin substrate, angiotensinogen (1-14), rat is a biological active peptide. (This peptide is derived from rat angiotensinogen amino acid residues 1-14. It is a synthetic renin substrate.)
|
-
- HY-P5445
-
|
|
Peptides
|
Others
|
|
Neurogranin 28-43 is a biological active peptide. (selective PKC substrate)
|
-
- HY-P5386
-
-
- HY-P5456
-
|
|
PKC
|
Others
|
|
KRPpSQRHGSKY-NH2 is a biological active peptide. (This is a phosphorylated PKC substrate peptide)
|
-
- HY-P5433F
-
|
|
Insulin Receptor
|
Others
|
|
IRS-1 Peptide, FAM labeled is a biological active peptide. (Insulin receptor substrate)
|
-
- HY-P3476
-
|
|
Fluorescent Dye
Caspase
|
Cancer
|
|
Mca-VDQVDGW-Lys(Dnp)-NH2 is a fluorogenic substrate of caspase-7. Mca-VDQVDGW-K(Dnp)-NH2 can be used to quantify caspase-7 activity.
|
- HY-P5473
-
|
|
Peptides
|
Others
|
|
EA2 is a biological active peptide. (This is a peptide substrate for polypeptide N-acetylgalactosaminyltransferase (polypeptide GalNAc-T).)
|
- HY-P5467
-
|
|
ROCK
|
Others
|
|
S6(229-239), Amide, biotinalyted is a biological active peptide. (substrate for Rho-Kinase II)
|
- HY-P1906A
-
|
|
CDK
|
Neurological Disease
|
|
[pThr3]-CDK5 Substrate TFA is an effective Phospho-Thr3CDK5 Substrate. [pThr3]-CDK5 Substrate is derived from the sequence of the histone H1 peptide that docks in the active site of CDK5. [pThr3]-CDK5 Substrate is phosphorylated by CDK5 with a Km value of 6 µM .
|
- HY-P4891
-
|
|
Angiotensin Receptor
|
Others
|
|
Angiotensin (1-12) (human) is an endogenous substrate for the production of biologically active angiotensin peptides by a non-renin-dependent mechanism .
|
- HY-P5512
-
|
|
Peptides
|
Others
|
|
MUC5AC-3 is a biological active peptide. (glycopeptide transferase, ppGaNTase-T9 substrate)
|
- HY-P5511
-
|
|
Peptides
|
Others
|
|
MUC5AC-3/13 is a biological active peptide. (glycopeptide transferase, ppGaNTase-T9 substrate)
|
- HY-P5526
-
|
|
Casein Kinase
|
Others
|
|
CCK1-specific peptide substrate is a biological active peptide. (This peptide sequence is based on rabbit muscle glycogen synthase with Ser7 phosphorylated. It is a peptide substrate for Casein Kinase I (CK1). CK1 phosphorylates Ser10. Ser7 is phosphorylated by PKA in vivo.)
|
- HY-P5454
-
|
|
Peptides
|
Others
|
|
RS Domain derived peptide is a biological active peptide. (This peptide is a substrate for Clk/Sty and is phosphorylated by Clk/Sty protein kinase (Km=102 microM).)
|
- HY-P2716
-
|
|
MMP
|
Others
|
|
Mca-Arg-Pro-Lys-Pro-Tyr-Ala-Nva-Trp-Met-Lys(Dnp)-NH2 is a biological active peptide. (MMP substrate)
|
- HY-P5326
-
|
|
Peptides
|
Others
|
|
EDANS-CO-CH2-CH2-CO-ALERMFLSFP-Dap(DABCYL)OH is a biological active peptide. (Plasmepsin I substrate)
|
- HY-P5530
-
|
|
Peptides
|
Others
|
|
2Abz-SVARTLLV-Lys(Dnp)-NH2 is a biological active peptide. (C1-inhibitor P4-P4′ substrate)
|
- HY-P5356
-
|
Plasmin substrate
|
Fluorescent Dye
|
Others
|
|
H-D-Val-Leu-Lys-AFC (Plasmin substrate) is a biological active peptide. (This is a fluorescent plasmin substrate, Abs/Em=380/500 nm.Plasmin belongs to the family of serine proteases. It plays a key role in fibrinolysis by dissolving fibrin in blood clots. Besides fibrinolysis, plasmin is also involved in such physiological and pathological processes as wound healing, liver repair, and the maintenance of liver homeostasis.)
|
- HY-P5510
-
|
HCV NS3 protease substrate
|
Peptides
|
Others
|
|
Ac-Asp-Glu-Asp(EDANS)-Glu-Glu-Abu-ψ-(COO)Ala-Ser-Lys(DABCYL)-NH2 (HCV NS3 protease substrate) is a biological active peptide. (This peptide is a HCV protease substrate incorporating an ester bond between residues P1 and P1. Due to ready transesterification of the scissile bond to the acyl-enzyme intermediate, this substrate shows very high kcat/Km values, enabling detection of activity with subnanomolar nonstructural protein 3 (NS3 protease) concentrations. It is widely used for the continuous assay of NS3 protease activity. Substrate cleavage is proportional to the enzyme concentration with a detection limit for NS3 between 1 nM and 250 pM.
|
- HY-P5415
-
|
|
HIV
|
Others
|
|
DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is a biological active peptide. (DABCYL-GABA-Ser-Gln-Asn-Tyr-Pro-Ile-Val-Gln-EDANS is also called HIV protease substrate I in some literature. It is widely used for the continuous assay for HIV protease activity. The 11-Kd protease (PR) encoded by the human immunodeficiency virus 1 (HIV-1) is essential for the correct processing of viral polyproteins and the maturation of infectious virus, and is therefore a target for the design of selective acquired immunodeficiency syndrome (AIDS) therapeutics. The FRET-based fluorogenic substrate is derived from a natural processing site for HIV-1 PR. Incubation of recombinant HIV-1 PR with the fluorogenic substrate resulted in specific cleavage at the Tyr-Pro bond and a time-dependent increase in fluorescence intensity that is linearly related to the extent of substrate hydrolysis. The fluorescence quantum yields of the HIV-1 PR substrate in the FRET assay increased by 40.0- and 34.4-fold, respectively, per mole of substrate cleaved. Because of its simplicity and precision in the determination of reaction rates required for kinetic analysis, this substrate offers many advantages over the commonly used HPLC or electrophoresis-based assays for peptide substrate hydrolysis by retroviral PRs. Abs/Em = 340nm/490nm.)
|
- HY-P10808
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
RSRGVFF (FOXP3 inhibitor P60) is a mixed-type angiotensin-converting enzyme (ACE) inhibitor with blood-brain barrier permeability, boasting an IC50 value of 5.01 μM . RSRGVFF is capable of binding to both active and non-active sites of ACE and its substrate HHL complex, thus reducing the catalytic activity of ACE. RSRGVFF can be further utilized for research on lowering hypertension .
|
- HY-P5323
-
|
|
Bacterial
|
Others
|
|
Dabcyl-AGHDAHASET-Edans is a biological active peptide. (This is a type I signal peptidase (SPase1) substrate peptide labeled with EDANS/ DABCYL FRET pair, and contains a crucial cleavage site derived from the C-terminal region of the Staphylococcus epidermidis pre-SceD protein. Abs/Em = 340/490 nm.)
|
- HY-P5371
-
|
|
Thrombin
|
Others
|
|
TFLLRNPNDK-NH2 is a biological active peptide. (This peptide is a thrombin receptor activating peptide. This PAR-1 agonist peptide reversibly binds to PAR-1 mimicking the 'tethered ligand' that thrombin makes available through proteolytic cleavage of substrate. It is also known to cause increase in liquid and protein permeability much like thrombin.)
|
- HY-P5527F
-
|
|
Peptides
|
Others
|
|
FAM-CSKtide is a biological active peptide. (This is a FAM labeled peptide substrate (Abs/Em = 494/521 nm) for C-terminal Src kinase (Csk) and many other kinases such as Axl, cKit, ERBB4, Fes, Flt3, IGF-1 R, MET, MUSK, PYK2, Ret, TIE2, TrkA, VEGF-R1 and VEGF-R2.)
|
- HY-P5344
-
|
Fluorigenic PEXEL peptide
|
Parasite
|
Others
|
|
Dabcyl-LNKRLLHETQ-Edans (Fluorigenic PEXEL peptide) is a biological active peptide. (This FRET substrate peptide for Plasmepsin V (PMV) is derived from the conserved Plasmodium Export Element (PEXEL) motif of Histidine-Rich Protein II (HRPII). PMV is an ER aspartic protease that recognizes and cleaves the RXL sequence within the PEXEL motif of proteins exported by human malaria parasite Plasmodium falciparum, allowing them to translocate into host erythrocytes.)
|
- HY-P5528
-
|
|
Peptides
|
Others
|
|
2Abz-SLGRKIQIK(Dnp)-NH2 is a biological active peptide. (This peptide is a second complement component (C2), the physiological substrate for the proenzyme Cls, first complement component. The complement system is a central component of host defense but can also contribute to the inflammation seen in pathological conditions. The C1s protease of the C1 complex initiates the host defense pathway. This peptide employs 2Abz/Dnp FRET pair for quantitation of complement enzyme activity.)
|
- HY-P5466
-
|
|
Peptides
|
Others
|
|
S6(229-239) is a biological active peptide. (This is a synthetic peptide substrate for S6 kinase shown to be phosphorylated by protein kinase c with phosphorylation site identified at Ser235)
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P992275
-
|
|
γ-secretase
|
Neurological Disease
Cancer
|
|
Anti-Nicastrin Antibody (A5226A) is a monoclonal antibody against Nicastrin and an inhibitor of γ-secretase. Anti-Nicastrin Antibody (A5226A) recognizes the fully glycosylated mature presenilin enhancer in the active γ-secretase complex and inhibits its activity via competition for substrate binding. Anti-Nicastrin Antibody (A5226A) abrogates the growth of cancer cells dependent on γ-secretase activity. Anti-Nicastrin Antibody (A5226A) serves as an imaging tool to visualize the endocytic trafficking of active γ-secretase, and also acts as a detection reagent to evaluate the endocytic efficiency of γ-secretase. Anti-Nicastrin Antibody (A5226A) can be used in studies related to non-small cell lung cancer, T-cell acute lymphoblastic leukemia and Alzheimer's disease .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-N1420
-
-
-
- HY-W012241
-
-
-
- HY-17367
-
-
-
- HY-133708
-
-
-
- HY-N2464
-
-
-
- HY-N1181
-
-
-
- HY-B1302
-
-
-
- HY-N1420A
-
-
-
- HY-17026E
-
|
dFdCTP trisodium
|
Structural Classification
Natural Products
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
|
Gemcitabine triphosphate (dFdCTP) trisodium is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate trisodium cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate trisodium shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate trisodium partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate trisodium disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate trisodium can be used for the research of pancreatic cancer and non-small cell lung cancer .
|
-
-
- HY-113362
-
-
-
- HY-17367A
-
-
-
- HY-N0419
-
-
-
- HY-113493
-
-
-
- HY-A0279A
-
-
-
- HY-113335
-
-
-
- HY-N7136
-
-
-
- HY-B1746
-
-
-
- HY-17026A
-
|
dFdCTP
|
Structural Classification
Natural Products
Classification of Application Fields
Endogenous metabolite
Disease Research Fields
Source Classification
Cancer
|
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
|
Gemcitabine triphosphate (dFdCTP) is the active metabolite of Gemcitabine (HY-17026). The mechanism of Gemcitabine triphosphate cell-killing is its competition with cytidine triphosphate during DNA replication, which results in the inhibition of chain elongation. Gemcitabine triphosphate shows a Ki of 11.2 μM against DNA polymerase α and 14.4 μM against DNA polymerase ε. Gemcitabine triphosphate partially inhibits dCMP deaminase and acts as a substrate for DNA synthesis to incorporate into cellular DNA and RNA. Gemcitabine triphosphate disrupts DNA and RNA synthesis, arrests cell cycle in G0/G1 and S phases, triggers apoptosis, reduces tumor cell proliferation. Gemcitabine triphosphate can be used for the research of pancreatic cancer and non-small cell lung cancer .
|
-
-
- HY-126848
-
-
-
- HY-122439
-
-
-
- HY-137129
-
-
-
- HY-W017445
-
|
|
Monophenols
Microorganisms
Phenols
Source Classification
|
Fungal
|
|
Homogentisic acid lactone (Compound 1) is a fungal metabolite with fungicidal activity, which is found in the fungus WF5. Homogentisic acid lactone is active against the plant pathogenic fungus F. graminearum. Homogentisic acid lactone can be used as a substrate in the determination of serum paraoxonase/arylesterase 1 (PON1) activity .
|
-
-
- HY-N1420AR
-
|
L-Rhamnose monohydrate (Standard)
|
Structural Classification
Microorganisms
other families
Plants
Saccharides
Monosaccharides
Source Classification
|
Reference Standards
Endogenous Metabolite
MMP
Interleukin Related
PKA
|
|
Rhamnose monohydrate (Standard) is the analytical standard of Rhamnose monohydrate (HY-N1420A). Rhamnose monohydrate (L-Rhamnose monohydrate) is an orally active deoxysugar. Rhamnose monohydrate can inhibit levels of pro-inflammatory interleukin and matrix metalloproteinases (MMPs) in skin aging models. Rhamnose can promote the phosphorylation levels of PKA substrates and HSL in SVF-derived adipocytes, stimulating PKA signaling. Rhamnose monohydrate can act against obesity in mice by stimulating fat dopamine receptors and inducing thermogenesis. Rhamnose monohydrate shows anti-aging effects. Rhamnose monohydrate can be used in the study of Ehrlich’s solid tumors and sarcomas .
|
-
-
- HY-116750
-
-
-
- HY-135867
-
-
-
- HY-135867A
-
-
-
- HY-W012241R
-
|
|
Structural Classification
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
|
|
Dodecanedioic acid (Standard) is the analytical standard of Dodecanedioic acid (HY-W012241). This product is intended for research and analytical applications. Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
-
- HY-N1181R
-
-
-
- HY-135867F
-
-
-
- HY-N7263
-
|
|
Alkaloids
other families
Plants
Source Classification
|
Cholinesterase (ChE)
|
|
Galanthamine N-Oxide is an alkaloid obtained from the bulbs of Zephyranthes concolor. Galanthamine N-Oxide inhibits electric eel acetylcholinesterase (AChE) with an EC50 of 26.2 μM. Galanthamine N-Oxide is a prominent inhibitor of substrate accommodation in the active site of the Torpedo californica AChE (TcAChE), hAChE and hBChE enzymes .
|
-
-
- HY-A0279AR
-
-
-
- HY-113362R
-
-
-
- HY-17367R
-
-
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-134423S
-
|
|
|
Stearoyl coenzyme A- 13C18 (lithium) is the 13C labeled Stearoyl coenzyme A lithium . Stearoyl coenzyme A (Stearoyl-CoA) lithium is an active compound that can be used as a substrate for the determination of stearoyl-Coenzyme desaturase in microsomes .
|
-
-
- HY-B0777S
-
|
|
|
Moxidectin-d3 (CL-301423-d3) is deuterium labeled Moxidectin. Moxidectin (CL301423) is an orally active macrolide (ML) anthelmintic for the prevention and control of heartworms and roundworms. Moxidectin is also a substrate of BCRP and P-glycoprotein (P-gp) in vivo, and is secreted into breast milk and effluxed from the host and parasite mediated by Bcrp1 and P-gp. This may be related to the presence of chemical residues in milk .
|
-
-
- HY-G0017S
-
|
|
|
N-Desmethyl imatinib-d8 is a deuterium labeled Imatinib metabolite N-Desmethyl Imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
-
- HY-W012241S1
-
|
|
|
Dodecanedioic acid-d4 is the deuterium labeled Dodecanedioic acid (HY-W012241). Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
-
- HY-13463BS
-
|
|
|
Avatrombopag-d8 (hydrochloride) is deuterium labeled Avatrombopag (hydrochloride). Avatrombopag (AKR-501) hydrochloride is an orally active, nonpeptide thrombopoietin (TPO) receptor agonist (EC50=3.3 nM). Avatrombopag hydrochloride mimics the biological activities of TPO. Avatrombopag hydrochloride increases platelet production by activating the intracellular signaling system, and promotes production of platelets and megakaryocytes from hemopoietic precursor cells. Avatrombopag hydrochloride is a substrate of cytochrome P450 (CYP) 2C9 and CYP3A .
|
-
-
- HY-W012241S
-
|
|
|
Dodecanedioic acid-d20 is the deuterium labeled Dodecanedioic acid (HY-W012241). Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
-
- HY-W777762
-
|
|
|
Dodecanedioic Acid- 13C12 is the 13C-labeled Dodecanedioic acid (HY-W012241). Dodecanedioic acid is an orally active straight-chain dicarboxylic acid. As an alternative energy substrate between lipids and carbohydrates, Dodecanedioic acid can be rapidly oxidized during exercise, reducing muscle fatigue without stimulating insulin secretion. Dodecanedioic acid also exhibits blood glucose-lowering activity in non-insulin-dependent diabetes mellitus .
|
-
-
- HY-G0017S1
-
|
|
|
N-Desmethyl imatinib-d4 is the deuterium-labeled N-Desmethyl imatinib (HY-G0017). N‑Desmethyl imatinib (Norimatinib) is an active metabolite of Imatinib (HY-15463), a selective c‑Abl inhibitor, and a substrate of P‑glycoprotein. N-Desmethyl imatinib binds to the c-Abl catalytic domain to prevent substrate phosphorylation, inhibits c-Abl-mediated α-synuclein activation and downstream inflammatory signaling pathways. N-Desmethyl imatinib induces apoptosis in K562 human leukemia cells. N-Desmethyl imatinib exhibits significantly elevated plasma levels in gastrointestinal stromal tumor (GIST) settings following mild SARS CoV 2 infection. N-Desmethyl imatinib can be used for the research of Parkinson’s disease, gastrointestinal stromal tumor, and chronic myeloid leukemia .
|
-
-
- HY-B0306S
-
|
|
|
Prothionamide-d5 is deuterium labeled Prothionamide (HY-B0306). Prothionamide is an orally active thioamide antibacterial agent. Prothionamide is a substrate of OCT1 with a Km value of 805.8 μM. Prothionamide reacts with NAD to form a covalent adduct, with the adduct being a tight-binding inhibitor of Mycobacterium tuberculosis and Mycobacterium leprae InhA. Prothionamide can effectively inhibit the growth of Mycobacterium tuberculosis (MIC = ~0.5 µg/mL) and Mycobacterium leprae. Prothionamide is used in the research of tuberculosis and leprosy .
|
-
-
- HY-17367S5
-
|
|
|
Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CL pro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death .
|
-
-
- HY-A0069AS
-
|
|
|
Doxylamine-d5 is deuterium labeled Doxylamine (HY-A0069A). Doxylamine is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine is orally active, possessing analgesic and hypnotic activities. Doxylamine enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine can be used for the research of nausea, allergy, insomnia .
|
-
-
- HY-A0069S
-
|
|
|
Doxylamine-d5 succinate is deuterium labeled Doxylamine succinate (HY-A0069A). Doxylamine succinate is a first-generation antihistamine and acts as a histamine H1 receptor antagonist. Doxylamine succinate is orally active, possessing analgesic and hypnotic activities. Doxylamine succinate enhances the activities of CYP2B, CYP2A, CYP3A and thyroxine-glucuronosyltransferase via promoting substrate hydroxylation and thyroxine metabolic pathways. Doxylamine succinate decreases serum thyroxine (T4) level and elevates serum thyroid-stimulating hormone (TSH) level. Doxylamine succinate induces liver enlargement and increases the activities of hepatic microsomal cytochrome P450, cytochrome b5 and NADPH-cytochrome c reductase. Doxylamine succinate can be used for the research of nausea, allergy, insomnia .
|
-
-
- HY-103586S2
-
|
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GS-441524-d is the deuterium labeled GS-441524 (HY-103586). GS-441524 is a potent, orally active and CNS-penetrant viral RNA-dependent RNA polymerase inhibitor. GS-441524 competes with natural nucleosides to block viral RNA transcription as an alternative substrate and RNA chain terminator. GS-441524 inhibits the replication of feline infectious peritonitis virus, African swine fever virus, and severe acute respiratory syndrome coronavirus 2. GS-441524 reduces viral RNA levels in cats. GS-441524 can be used in research related to feline infectious peritonitis, African swine fever, and coronavirus disease 2019 (COVID-19) .
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| Cat. No. |
Product Name |
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Classification |
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- HY-162874
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DBCO
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diABZI-V/C-DBCO is a STING agonist with an EC50 of 1.47 nM. diABZI-V/C-DBCO activates the STING pathway, induces the production of IFN-I, and stimulates the secretion of IFN-β. diABZI-V/C-DBCO serves as a substrate for cathepsin B, and releases active diABZI-amine via cathepsin B-mediated cleavage. In an orthotopic mouse model of breast cancer, diABZI-V/C-DBCO increases serum IFN-β levels and the frequency of granzyme B + CD8 + T cells. diABZI-V/C-DBCO is applicable to research related to triple-negative breast cancer .
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- HY-119323
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Labeling and Fluorescence Imaging
Azide
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7-Azido-4-methylcoumarin is a selective coumarin-based fluorescent probe for hydrogen sulfide (H2S). In the presence of H2S, the aromatic azido group of 7-Azido-4-methylcoumarin is selectively reduced to produce the fluorescently active 7-amino-4-methylcoumarin (AMC). 7-Azido-4-methylcoumarin binds to the coumarin/phenol-binding site of BSA, the aglycone-binding site of UGT1A6, and the substrate-binding site of SULT1A1, respectively. 7-Azido-4-methylcoumarin retains its fluorescent properties after covalent binding, acts as a fluorescent H2S probe, and does not react with cysteine, homocysteine or glutathione (Ex/Em = 340/445 nm) .
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| Cat. No. |
Product Name |
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Classification |
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- HY-W011834
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Nucleoside Analogs
Cytidine
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2'-O-Methylcytidine is an orally active 2'-substituted nucleoside as a inhibitor of HCV replication with antiviral activity. 2'-O-Methylcytidine inhibits RNA-dependent RNA polymerase (NS5B)-catalyzed RNA synthesis in vitro, in a manner that is competitive with substrate nucleoside triphosphate .
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- HY-177582
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Nucleotide Analogs
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N1-Methyl-GTP is a nucleotide analog of GTP. N1-Methyl-GTP shows a half-maximal inhibitory concentration of 8.1 μM and an inhibition constant of 1.5 μM against yeast RTPase. N1-Methyl-GTP can be used as a probe molecule to explore the structural flexibility of the active site of RNA triphosphatase and the mechanism of substrate recognition .
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