Search Result
Results for "
Adp Inhibitors
" in MedChemExpress (MCE) Product Catalog:
3
Biochemical Assay Reagents
18
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-108360
-
-
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- HY-16929
-
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LAT-A
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Arp2/3 Complex
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Cancer
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Latrunculin A (LAT-A), found in the red sea sponge Latrunculia magnifica, is a G-actin polymerization inhibitor. Latrunculin A binds to actin monomers and inhibits polymerization of actin with Kds of 0.1, 0.4, 4.7 μM and 0.19 μM for ATP-actin, ADP-Pi-actin, ADP-actin and G-actin, respectively. Latrunculin A has effective anti-metastatic properties for cancer research. Latrunculin A blocks cell migration .
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-
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- HY-112473
-
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NAV-2729
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Ras
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Cancer
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Grassofermata is a dual Arf1/Arf6 activation inhibitor. ADP ribosylation factors (Arfs) are members of the Arf family of GTP-binding proteins of the Ras superfamily.
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-
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- HY-113432
-
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2PY
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Endogenous Metabolite
PARP
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Metabolic Disease
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Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
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-
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- HY-N2522
-
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Gummiferin dipotassium
|
Mitochondrial Metabolism
Calcium Channel
Reactive Oxygen Species (ROS)
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Neurological Disease
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Carboxyatractyloside dipotassium is a diterpenoid. Carboxyatractyloside dipotassium can be isolated from plants of the genus Xanthium. Carboxyatractyloside dipotassium is an ADP/ATP carrier inhibitor, inhibiting mitochondrial ADP/ATP transport. Carboxyatractyloside dipotassium promotes ROS production, induces Ca 2+ release, and leads to mitochondrial dysfunction. Carboxyatractyloside dipotassium induces lethargy, weakness, and epileptic seizures in rats .
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-
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- HY-N1502
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Gummiferin tripotassium
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Mitochondrial Metabolism
Reactive Oxygen Species (ROS)
Calcium Channel
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Neurological Disease
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Carboxyatractyloside tripotassium is a diterpenoid. Carboxyatractyloside tripotassium can be isolated from plants of the genus Xanthium. Carboxyatractyloside tripotassium is an ADP/ATP carrier inhibitor, inhibiting mitochondrial ADP/ATP transport. Carboxyatractyloside tripotassium promotes ROS production, induces Ca 2+ release, and leads to mitochondrial dysfunction. Carboxyatractyloside tripotassium induces lethargy, weakness, and epileptic seizures in rats .
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-
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- HY-N7765
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HCV
Bacterial
Apoptosis
Fungal
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Infection
Inflammation/Immunology
Cancer
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Oenothein B is a dimeric macrocyclic ellagitannin and has widely pharmacological activities, including antioxidant, anti-inflammatory, antifungal, anti-HCV, and antitumor properties. Oenothein B is a potent and specific inhibitor of poly(ADP-ribose) glycohydrolase .
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-
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- HY-15284
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PCR 4099
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P2Y Receptor
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Cardiovascular Disease
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Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
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-
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- HY-153920
-
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ABSK021
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c-Fms
c-Kit
PDGFR
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Cancer
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Pimicotinib (ABSK021) is a selective and orally active CSF1R inhibitor with an IC50 value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib exhibits anti-tumor activity .
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-
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- HY-B2174
-
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Acrinol
|
Bacterial
|
Infection
|
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Ethacridine lactate (Acrinol) is a widely used antiseptic and abortifacient. Ethacridine lactate is effective against Staphylococcus aureus and other gram-positive cocci. Ethacridine lactate is also a poly(ADP-ribose) glycohydrolase (PARG) inhibitor .
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-
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- HY-B0889
-
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Acrinol monohydrate
|
Bacterial
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Infection
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Ethacridine lactate (Acrinol) monohydrate is a widely used antiseptic and abortifacient. Ethacridine lactate monohydrate is effective against Staphylococcus aureus and other gram-positive cocci. Ethacridine lactate monohydrate is also a poly(ADP-ribose) glycohydrolase (PARG) inhibitor .
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-
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- HY-101020
-
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2-Picolinamide
|
PARP
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Metabolic Disease
|
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Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells .
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-
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- HY-15284A
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PCR 4099 hydrochloride
|
P2Y Receptor
|
Cardiovascular Disease
|
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Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and proagent, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
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-
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- HY-146248B
-
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Poly(ADP-ribose) Glycohydrolase (PARG)
SARS-CoV
Protease Activated Receptor (PAR)
|
Metabolic Disease
|
|
TFMU-ADPr diammonium is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr diammonium can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr diammonium binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr diammonium can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr diammonium is also applicable to COVID-19-related research .
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- HY-107867
-
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P2Y Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
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(±)-Clopidogrel bisulfate is a platelet P2Y12 receptor inhibitor and an adenosine diphosphate (ADP) receptor antagonist. (±)-Clopidogrel bisulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel bisulfate reduces vascular inflammation and angiotensin II induced-abdominal aortic aneurysm progression. (±)-Clopidogrel bisulfate has anti-inflammatory effects .
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-
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- HY-134216
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-
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- HY-U00422
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K-756
2 Publications Verification
|
PARP
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Cancer
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K-756 is a direct and selective tankyrase (TNKS) inhibitor, which inhibits the ADP-ribosylation activity of TNKS1 and TNKS2 with IC50s of 31 and 36 nM, respectively.
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-
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- HY-125989
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2-MeSAMP; 2-Methylthioadenosine 5′-monophosphate; 2-Methylthioadenosine 5′-phosphate
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P2Y Receptor
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Cardiovascular Disease
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2-Methylthio-AMP (2-MeSAMP) is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP is an inhibitor of ADP-dependent platelet aggregation .
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- HY-W250153
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P2Y Receptor
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Cardiovascular Disease
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Adenosine 3'-phosphate 5'-phosphosulfate lithium, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
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- HY-133531
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Poly(ADP-ribose) Glycohydrolase (PARG)
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Cancer
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PDD00017272 is an inhibitor of poly(ADP-ribose) glycohydrolase (PARG) (EC50=4.8 nM) and an activator of PARP1/2. PDD00017272 inhibits its activity of hydrolyzing poly(ADP-ribose) (pADPr), resulting in the accumulation of pADPr on chromatin, interfering with DNA damage repair and replication processes, and inducing PARP1/2-dependent cytotoxicity. PDD00017272 can be used in cancer models with DNA repair defects (such as BRCA mutations) or resistance to PARP inhibitors. PDD00017272 has a PARG expression level-correlated inhibitory potency with EC50 of 9.2 nM (PARG cells), the tumor cells with lower PARG expression are more sensitive .
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- HY-178208
-
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Poly(ADP-ribose) Glycohydrolase (PARG)
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Cancer
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MDOLL-0286 is a selective Poly(ADP-ribose) Glycohydrolase (PARG) (ARH3) inhibitor with an IC50 of 2.3μM. MDOLL-0286 can inhibit ARH3’s poly-ADP-ribose hydrolytic activity on cellular substrates. MDOLL-0286 can inhibit DNA damage response. MDOLL-0286 can be used for the research of cancer .
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- HY-G0023
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Niraparib carboxylic acid metabolite M1; M1 metabolite of niraparib
|
Drug Metabolite
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Others
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Niraparib metabolite M1 is a metabolite of niraparib, and the latter one acts as a novel poly(ADP-Ribose) polymerase (PARP) inhibitor.
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-
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- HY-133530
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-
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- HY-146248
-
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SARS-CoV
Poly(ADP-ribose) Glycohydrolase (PARG)
Protease Activated Receptor (PAR)
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Infection
|
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TFMU-ADPr is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr is also applicable to COVID-19-related research .
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- HY-W051513
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PARP
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Others
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2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with 0.20 mM .
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- HY-164090
-
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P2Y Receptor
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Cardiovascular Disease
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Adenosine 3'-phosphate 5'-phosphosulfate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
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- HY-135846
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-
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- HY-115666
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-
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- HY-P2325
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Biochemical Assay Reagents
ROCK
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Neurological Disease
Metabolic Disease
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Exoenzyme C3, clostridium botulinum, is a mono-ADP-ribosylating enzyme. Exoenzyme C3, clostridium botulinum specifically modifies RhoA, B, and C by transferring ADP-ribose to them, thereby inactivating these GTPases. Exoenzyme C3, clostridium botulinum can induce neuronal axonal and dendritic growth, inhibit macrophage migration, and regulate cytoskeletal dynamics. Exoenzyme C3, clostridium botulinum can be used in the research of spinal cord injury and diabetic painful neuropathy .
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- HY-122184
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HSP
Apoptosis
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Cancer
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PET-16 is a selective HSP70 inhibitor that binds to an allosteric pocket of the substrate-binding domain. PET-16 inhibits the ability of HSP70 to cycle between ATP-bound and ADP-bound states. PET-16 induces apoptosis in multiple myeloma .
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- HY-Z0283S
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Benzenecarboxamide-15N; Phenylamide-15N
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Endogenous Metabolite
PARP
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Others
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Benzamide- 15N is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP) .
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- HY-D1107
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PARP
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Others
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NCT-TFP is PARP probe used to identifying Poly(ADP-ribose) polymerases (PARP) inhibitors (extracted from patent US20190331688A1) .
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- HY-122041
-
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Apoptosis
Poly(ADP-ribose) Glycohydrolase (PARG)
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Cancer
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Ethacridine is a poly(ADP-ribose) glycohydrolase (PARG) inhibitor and an activator of the transcriptional coactivator. Ethacridine induces thyroid cancer cells apoptosis and promotes differentiation in thyroid follicular cells .
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- HY-15284S2
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PCR 4099-d4
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P2Y Receptor
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Cardiovascular Disease
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Prasugrel-d4 is the deuterium labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
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- HY-136501
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P2Y Receptor
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Cardiovascular Disease
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MRS2395, an dipivaloyl derivative, is a potent P2Y12 receptor antagonist. MRS2395 inhibits ADP-induced platelet activation with a Ki of 3.6 μM. MRS2395 inhibits cAMP induced by ADP in rat platelets in the presence of PGE1 with an IC50 of 7 µM. MRS2395 enhances platelet dense granule release in response to TRAP-6 .
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- HY-N7614
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Schidigerasaponin F2; Timosaponin AII
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Others
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Cardiovascular Disease
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Anemarrhenasaponin A2 (Schidigerasaponin F2) is a steroidal saponin isolated from the rhizomes of Anemarrhena asphodeloides. Anemarrhenasaponin A2 inhibits ADP-induced platelet aggregation .
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- HY-146248A
-
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Poly(ADP-ribose) Glycohydrolase (PARG)
SARS-CoV
Protease Activated Receptor (PAR)
|
Others
|
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TFMU-ADPr triethylamine is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr triethylamine can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr triethylamine binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr triethylamine can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr triethylamine is also applicable to COVID-19-related research .
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- HY-N9422
-
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P2Y Receptor
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Cardiovascular Disease
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Adenosine 3'-phosphate 5'-phosphosulfate triethylamine, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate triethylamine can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate triethylamine is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate triethylamine can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
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- HY-131831A
-
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N6-benzyl Adp sodium
|
ATP Synthase
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Cancer
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6-Bn-ADP (N6-benzyl ADP) sodium is a derivative of Adenosine 5'-diphosphate (ADP) (HY-W010918) that inhibits ATP hydrolysis. 6-Bn-ADP sodium inhibits the ATPase activities of Mortalin, Hsc70, and Hsp70 protein with Kis of 86.51 μM, 294.5 μM, and 1612 μM, respectively .
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-
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- HY-167927
-
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CVL218
|
PARP
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Cancer
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Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
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-
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- HY-148710
-
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PARP
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Inflammation/Immunology
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ARTD10/PARP10-IN-2 (compound 19) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 ARTD1/PARP1 with IC50s of 2.0 μM, and 9.7 μM, respectively .
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-
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- HY-153920A
-
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ABSK021 hydrochloride
|
c-Fms
c-Kit
PDGFR
|
Cancer
|
|
Pimicotinib (ABSK021) hydrochloride is a selective and orally active CSF1R inhibitor with an IC50 value of 19.48 nM (determined by inhibiting ADP production). Pimicotinib hydrochloride exhibits anti-tumor activity .
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-
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- HY-137673
-
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NADH Dehydrogenase
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Others
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2'-Deoxy-NAD+ is a noncompetitive NAD+ inhibitor with a Ki of 32 μM. 2'-Deoxy-NAD+ can be utilized as a substrate to study the ADP-ribosyl transfer reaction .
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-
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- HY-153581
-
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PARP
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Others
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ARTD3/PARP3-IN-1 is an unselective inhibitor of diphtheria toxin-like ADP-ribosyltransferase 3 (ARTD3)/PARP3 .
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-
-
- HY-N1717
-
-
-
- HY-15048
-
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PARP
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Inflammation/Immunology
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GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrates strong anti-inflammatory effects that reduces inflammatory cell infiltration, histological injury. GPI 15427 also diminishes the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats .
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- HY-177631A
-
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DT01 sodium; coDbait sodium
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Poly(ADP-ribose) Glycohydrolase (PARG)
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Cancer
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Etidaligide sodium, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation
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-
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- HY-W250153A
-
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P2Y Receptor
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Cardiovascular Disease
|
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Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
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-
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- HY-N13135
-
|
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Others
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Cardiovascular Disease
|
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Kadsutherin G (compound 3) is a lignin isolated from Kadsura. Kadsutherin G inhibits adenosine diphosphate (ADP)-induced platelet aggregation by 33.1 % .
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-
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- HY-110043
-
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P2Y Receptor
|
Cardiovascular Disease
|
|
(±)-Clopidogrel hydrochloride is an antithrombotic agent that is ADP-selective and orally available. (±)-Clopidogrel hydrochloride inhibits platelet aggregation by inhibiting the binding of ADP to its platelet receptors .
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- HY-N13134
-
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Others
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Cardiovascular Disease
|
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Kadsutherin F (compound 2) is a lignin that can be isolated from Kadsura. Kadsutherin F has an inhibitory effect on adenosine diphosphate (ADP)-induced platelet aggregation with an inhibition rate of 49.47% .
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- HY-174447
-
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PARP
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Cancer
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ADP-ribose/PARP-IN-1 (Compound Ex.16) is a conjugated compound. ADP-ribose/PARP-IN-1 contains disease targeting moieties, PARP inhibitor moieties, cleavable linkers, chelators. ADP-ribose/PARP-IN-1 targets specific targets through the disease targeting moiety and selectively delivers PARP inhibitors to tumor cells. The cleavable linker of ADP-ribose/PARP-IN-1 releases the PARP inhibitor under appropriate conditions, inhibiting PARP to prevent DNA damage repair, while the radionuclide carried by the chelator exerts a killing effect. ADP-ribose/PARP-IN-1 can be used in the research of prostate cancer .
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- HY-131776A
-
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2-Chloroadenosine 5′-diphosphate sodium
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Adenylate Cyclase
HSP
|
Cardiovascular Disease
|
|
2-Chloro-ADP (2-Chloroadenosine 5′-diphosphate) sodium is a Adenosine 5'-diphosphate (ADP; HY-W010918) derivative that induces human platelet aggregation and inhibits stimulated adenylate cyclase . 2-Chloro-ADP sodium inhibits mortalin nucleotide-binding domain (NBD) with a Ki of 45.05 μM .
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-
- HY-131776
-
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2-Chloroadenosine 5′-diphosphate
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Adenylate Cyclase
HSP
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Cardiovascular Disease
|
|
2-Chloro-ADP (2-Chloroadenosine 5′-diphosphate) sis a Adenosine 5'-diphosphate (ADP; HY-W010918) derivative that induces human platelet aggregation and inhibits stimulated adenylate cyclase . 2-Chloro-ADP inhibits mortalin nucleotide-binding domain (NBD) with a Ki of 45.05 μM .
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- HY-134318B
-
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DNA/RNA Synthesis
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Others
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8-Azido-ADP (disodium) is a covalent-binding inhibitor of mitochondrial adenine nucleotide translocation. 8-Azido-ADP (disodium) causes irreversible inhibition of adenine nucleotide exchange in a light-dependent reaction. 8-Azido-ADP (disodium) inhibits the normal state 4 → 3 transitions of mitochondrial respiration induced by ADP . 8-Azido-ADP (disodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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- HY-156623
-
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PARP
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Cancer
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|
Lerzeparib is an (ADP-ribose) polymerase (PARP) inhibitor, with antineoplastic activity .
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- HY-120311
-
-
- HY-107867S1
-
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Isotope-Labeled Compounds
P2Y Receptor
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Inflammation/Immunology
|
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(Rac)-Clopidogrel hydrogen-d9 sulfate is the deuterium labeled (±)-Clopidogrel (bisulfate) (HY-107867). (±)-Clopidogrel bisulfate is a platelet P2Y12 receptor inhibitor and an adenosine diphosphate (ADP) receptor antagonist. (±)-Clopidogrel bisulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel bisulfate reduces vascular inflammation and angiotensin II induced-abdominal aortic aneurysm progression. (±)-Clopidogrel bisulfate has anti-inflammatory effects .
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-
- HY-U00223
-
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PARP
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Cancer
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WD2000-012547 is a selective poly(ADP-ribose)-polymerase (PARP-1) inhibitor with a pKi of 8.221.
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-
- HY-107867S2
-
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Isotope-Labeled Compounds
P2Y Receptor
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Cardiovascular Disease
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Clopidogrel- 13C,d3 sulfate is the deuterium and 13C-labeled (±)-Clopidogrel (bisulfate) (HY-107867). (±)-Clopidogrel bisulfate is a platelet P2Y12 receptor inhibitor and an adenosine diphosphate (ADP) receptor antagonist. (±)-Clopidogrel bisulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel bisulfate reduces vascular inflammation and angiotensin II induced-abdominal aortic aneurysm progression. (±)-Clopidogrel bisulfate has anti-inflammatory effects .
|
-
- HY-142657
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-7 is an inhibitor of poly(ADP-ribose) polymerase-1 (PARP1) as an anticancer agent.
|
-
- HY-116850
-
|
EG626; Phthalazinol; SC-32840
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Oxagrelate is a specific inhibitor of cyclic adenosine monophosphate phosphodiesterase and exhibits concentration-dependent inhibition of collagen- and ADP-induced platelet aggregation in vitro .
|
-
- HY-P1702
-
|
|
Integrin
|
Others
|
|
GR83895 is a RGD based peptide, and inhibits ADP-induced platelet aggregation of human gel-filtered platelets (IC50= 0.9 μM) .
|
-
- HY-168345
-
|
|
DNA/RNA Synthesis
|
Others
|
|
Ap4dT is an inhibitor for human adenylate kinase isozyme 1 (hAK1), that inhibits the ATP and ADP synthesis with IC50s of 42 μM and 38 μM .
|
-
- HY-168345A
-
|
|
DNA/RNA Synthesis
|
Others
|
|
Ap4dT is an inhibitor for human adenylate kinase isozyme 1 (hAK1), that inhibits the ATP and ADP synthesis with IC50s of 42 μM and 38 μM .
|
-
- HY-15284B
-
|
PCR 4099 (Maleic acid)
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (PCR 4099) Maleic acid is a thienopyridine and proagent, inhibits platelet function. Prasugrel Maleic acid is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
|
-
- HY-137673A
-
|
|
NADH Dehydrogenase
|
Others
|
|
2'-Deoxy-NAD+ sodium is a noncompetitive NAD+ inhibitor with a Ki of 32 μM. 2'-Deoxy-NAD+ sodium can be utilized as a substrate to study the ADP-ribosyl transfer reaction .
|
-
- HY-103064
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
2-Methylthio-AMP sodium is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP sodium is an inhibitor of ADP-dependent platelet aggregation .
|
-
- HY-W552525
-
|
|
Phosphorylase
|
Infection
|
|
Deoxyadenosine diphosphate sodium is a nucleoside diphosphate, in which the nucleoside is deoxyadenosine. Deoxyadenosine diphosphate sodium participates in DNA synthesis and repair. Deoxyadenosine diphosphate sodium acts as the inhibitor of polynucleotide phosphorylase, interfers with the polymerization of ADP and CDP .
|
-
- HY-N2522R
-
|
Gummiferin dipotassium (Standard)
|
Reference Standards
Mitochondrial Metabolism
Calcium Channel
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
Carboxyatractyloside (dipotassium) (Standard) is the analytical standard of Carboxyatractyloside dipotassium (HY-N2522). This product is intended for research and analytical applications. Carboxyatractyloside dipotassium is a diterpenoid. Carboxyatractyloside dipotassium can be isolated from plants of the genus Xanthium. Carboxyatractyloside dipotassium is an ADP/ATP carrier inhibitor, inhibiting mitochondrial ADP/ATP transport. Carboxyatractyloside dipotassium promotes ROS production, induces Ca 2+ release, and leads to mitochondrial dysfunction. Carboxyatractyloside dipotassium induces lethargy, weakness, and epileptic seizures in rats .
|
-
- HY-174836
-
|
|
PARP
|
Cancer
|
|
ZINC000081009201 is a potent poly(ADP-ribose) polymerase 1 (PARP1) inhibitor with an IC50 value of 1.4767 μM. ZINC000081009201 is promising for research of triple-negative breast cancer (TNBC) .
|
-
- HY-15284S1
-
|
PCR 4099-d3
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel-d3 is the deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
|
-
- HY-15284S
-
|
PCR 4099-d5
|
Isotope-Labeled Compounds
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel-d5 is deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
|
-
- HY-101020R
-
|
2-Picolinamide (Standard)
|
Reference Standards
PARP
|
Metabolic Disease
|
|
Picolinamide (Standard) is the analytical standard of Picolinamide. This product is intended for research and analytical applications. Picolinamide (2-Picolinamide) is an inhibitor of Poly(ADP-ribose) synthetase of nuclei from rat pancreatic islet cells .
|
-
- HY-113113
-
|
13,14-Dihydroprostaglandin E1
|
Endogenous Metabolite
|
Metabolic Disease
|
|
13,14-Dihydro PGE1 is a metabolite of PGE1 (Prostaglandin E1) which inhibits the ADP-induced platelet aggregation (ID50 = 10.8 ng/mL platelet rich plasma) .
|
-
- HY-160943A
-
|
|
SARS-CoV
|
Infection
|
|
F594-1001 (compound 6) hydrochloride is a potent and highly selective SARS-CoV-2 Mac1-ADP-ribose inhibitor with IC50s of 8.5 μM, 68 μM and 45 μM for SARS-CoV-2 in AS, FP, and FRET assays, respectively. F594-1001 hydrochloride directly binds to SARS-CoV-2 Mac1 and exhibits a dose-dependent inhibition of Mac1 ADP-ribosylhydrolase activity .
|
-
- HY-160943
-
|
|
SARS-CoV
|
Infection
|
|
F594-1001 (compound 6) is a potent and highly selective SARS-CoV-2 Mac1-ADP-ribose inhibitor with IC50s of 8.5 μM, 68 μM and 45 μM for SARS-CoV-2 in AS, FP, and FRET assays, respectively. F594-1001 directly binds to SARS-CoV-2 Mac1 and exhibits a dose-dependent inhibition of Mac1 ADP-ribosylhydrolase activity .
|
-
- HY-125989B
-
|
2-MeSAMP diTEA; 2-Methylthioadenosine 5′-monophosphate diTEA; 2-Methylthioadenosine 5′-phosphate diTEA
|
P2Y Receptor
|
Cardiovascular Disease
|
|
2-Methylthio-AMP (2-MeSAMP) diTEA is a selective and direct P2Y12 antagonist. 2-Methylthio-AMP diTEA is an inhibitor of ADP-dependent platelet aggregation .
|
-
- HY-126643
-
|
|
Mitochondrial Metabolism
|
Others
Cancer
|
|
Wedeloside is a diterpenoid amino glycoside isolated from the plant Wedelia asperrima. Wedeloside is capable of inhibiting ADP-stimulated respiration in mitochondria and possesses potential anti-tumor activity. Wedeloside is applicable in drug development and toxicological research .
|
-
- HY-113723
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2298? is a potent acyclic P2Y1 receptor antagonist with a Ki of 29.6 nM. MRS2298 inhibits the ADP-induced aggregation of human platelets with an IC50 of 62.8 nM. MRS2298 inhibits Ca 2+ rise in platelets with an IC50 of 810 nM .
|
-
- HY-E70252
-
|
S-1-Pyrenebutanoate-CoA; Coenzyme A,S-1-pyrenebutanoate
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
1-Pyrenebutanoyl-CoA is a type of coenzyme A that can non-competitively inhibit (Ki = 2 μM) phosphorylating (ADP-stimulated) respiration in rat liver mitochondria, and competitively inhibit (Ki = 2.1 μM and 15 μM) carnitine palmitoyl-CoA transferase and octanoyl-CoA transferase .
|
-
- HY-15284R
-
|
PCR 4099 (Standard)
|
Reference Standards
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (Standard) is the analytical standard of Prasugrel. This product is intended for research and analytical applications. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
|
-
- HY-15284AR
-
|
PCR 4099 hydrochloride (Standard)
|
Reference Standards
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel (hydrochloride) (Standard) is the analytical standard of Prasugrel (hydrochloride). This product is intended for research and analytical applications. Prasugrel hydrochloride (PCR 4099 hydrochloride), a thienopyridine and proagent, inhibits platelet function. Prasugrel hydrochloride is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
|
-
- HY-15284S3
-
|
PCR 4099-13C6
|
Isotope-Labeled Compounds
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel-13C6 is a deuterated labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
|
-
- HY-136142
-
|
|
Drug Metabolite
|
Others
|
|
Prasugrel chloride impurity is a catp impurity of Prasugrel, exacted from patent US20130345428A1, line 0053. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
|
-
- HY-116613
-
-
- HY-11024
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
ADP receptor-IN-1 (compound 21) is a platelet ADP receptor inhibitor. ADP receptor-IN-1 shows both IC50 values <10 μM at a platelet ADP receptor binding assay and aggregation using a platelet-rich plasma assay .
|
-
- HY-N17403
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
Decuroside IV is a coumarin-glycoside inhibitor that can be found in the roots of Peucedanum decursivum Maxim. Decuroside IV inhibits secondary wave aggregation of human platelets induced by ADP .
|
-
- HY-W209106
-
-
- HY-177420
-
-
- HY-182303
-
|
CATR
|
Methionine Adenosyltransferase (MAT)
|
Neurological Disease
|
|
Carboxyatractyloside (CATR) is a tight-binding inhibitor of adenine nucleotide translocase, and represents the major toxic component of Xanthium sibiricum. Carboxyatractyloside competes with ADP for binding to the translocase, blocks the translocation of ADP/ATP across the inner mitochondrial membrane, and thereby inhibits ADP-stimulated respiration. In the presence of Cyclosporin A (HY-B0579), Carboxyatractyloside still induces permeability transition in liver mitochondria of aged rats, exhibiting significant hepatotoxicity and nephrotoxicity. Carboxyatractyloside is widely used in studies related to hepatotoxicity, nephrotoxicity and Alzheimer's disease .
|
-
- HY-15283AS1
-
|
(±)-Clopidogrelum-d4
|
Isotope-Labeled Compounds
P2Y Receptor
|
Cardiovascular Disease
Inflammation/Immunology
|
|
(±)-Clopidogrel-d4 ((±)-Clopidogrelum-d4) is the deuterium labeled (±)-Clopidogrel (HY-107867). (±)-Clopidogrel is a platelet P2Y12 receptor inhibitor and an adenosine diphosphate (ADP) receptor antagonist. (±)-Clopidogrel inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel reduces vascular inflammation and angiotensin II induced-abdominal aortic aneurysm progression. (±)-Clopidogrel has anti-inflammatory effects .
|
-
- HY-150119
-
|
|
Sirtuin
|
Endocrinology
|
|
2'/3'-O-Acetyl-ADP-ribose sodium is an inhibitor of cell division and oocyte maturation. 2'/3'-O-Acetyl-ADP-ribose sodium causes delay or arrest of oocyte maturation and blastomere division in embryos. 2'/3'-O-Acetyl-ADP-ribose sodium is produced by Sir2 family deacetylases during the coupling of histone/protein deacetylation with β-NAD+ cleavage. In neutral or weakly alkaline aqueous solutions, the direct enzymatic product forms of 2'/3'-O-Acetyl-ADP-ribose sodium, namely the 2'-O-acetyl form and the 3'-O-acetyl form, undergo intramolecular lactone exchange reaction and interconvert with each other .
|
-
- HY-155865
-
|
|
Kinesin
|
Cancer
|
|
CCT368772 (compound 35) is a selective kinesin HSET inhibitor (HSET ADP-Glo IC50 = 0.019 μM). CCT368772 exhibits selectivity over Eg5 (Eg5 ADP-Glo IC50 >200 μM) . CCT368772 (compound 152) can be used for the study of hyperproliferative diseases and disorders such as cancer .
|
-
- HY-N19129
-
|
|
Others
|
Others
|
|
Macrostemonoside E is a steroidal glycoside present in Allium macrostemon Bunge, which inhibits ADP-induced aggregation of human platelets in vitro (IC50=0.417 mM) .
|
-
- HY-167848
-
|
XL-118
|
Others
|
Cardiovascular Disease
|
|
DMP-728 free base (XL-118) is a highly potent and selective GPIIb/IIIa antagonist with antiplatelet and antithrombotic activities. DMP-728 free base can inhibit ADP-induced human platelet aggregation in vitro, with an IC50 of 46 nmol/L, and can significantly reduce the interaction between fibrinogen and human platelets or Binding of purified human GPIIb/IIIa receptors. DMP-728 free base exhibits dose-dependent antiplatelet effects in anesthetized mongrel dogs, effectively inhibiting ADP-induced platelet aggregation and prolonging template bleeding time .
|
-
- HY-W041672
-
|
|
PARP
|
Cancer
|
|
PD128763 is a selective poly(ADP-ribose) polymerase inhibitor. PD128763 results in an enhancement of Streptozotocin (HY-13753)-induced cytotoxicity. PD128763 can be used in leukemia research .
|
-
- HY-N17823
-
|
|
Others
|
Inflammation/Immunology
|
|
Plantagoside A (Compound 3) is a phenylethanoid glycoside found in Plantago asiatica. Plantagoside A has antioxidant activity and can inhibit lipid peroxidation in rat liver microsomes induced by ADP and NADPH with an IC50 of 0.54 μM .
|
-
- HY-165434
-
|
EL 784
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
Naxaprostene is a prostacyclin analogue. Naxaprostene was much more selective for IP receptors and tended towards partial agonism. Naxaprostene inhibits ADP-induced platelet aggregation. It has been shown to prevent rabbit carotid artery thrombosis.
|
-
- HY-108360R
-
|
|
Reference Standards
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
PDD 00017273 (Standard) is the analytical standard of PDD 00017273 (HY-108360). This product is intended for research and analytical applications. PDD 00017273 is a potent inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG), with an IC50 of 26 nM, and a Kd of 1.45 nM .
|
-
- HY-N17826
-
-
- HY-177631
-
|
DT01; coDbait
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
Etidaligide, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation of H2A
|
-
- HY-177100
-
|
|
PARP
|
Others
|
|
Lotixparib (Example 1) is an inhibitor of poly(ADP-ribose)polymerase-1 (PARP-1). Lotixparib has cytoprotective effect against a retinal disease. Lotixparib can be studied in research for PARP-1-associated diseases .
|
-
- HY-113096
-
|
PGD1
|
Endogenous Metabolite
|
Metabolic Disease
|
|
Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
|
-
- HY-N10272
-
|
|
Fungal
Bacterial
|
Infection
|
|
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in rat liver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation .
|
-
- HY-122048
-
|
AR-C67085MX; PSB 0413; FPL 67085
|
P2Y Receptor
|
Cardiovascular Disease
|
|
AR-C67085 (PSB 0413; FPL 67085) is a potent platelet P2T receptor antagonist with an pIC50 value of 8.60. AR-C67085 inhibits ADP-induced platelet aggregation .
|
-
- HY-137924
-
JA2131
1 Publications Verification
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
JA2131 is a small molecular inhibitor of Poly(ADP-ribose) Glycohydrolase (PARG) (IC50=0.4 μM). JA2131 regulate DNA damage responses, causes replication fork stalling and cancer cell death .
|
-
- HY-148709
-
|
|
PARP
|
Inflammation/Immunology
|
|
ARTD10/PARP10-IN-1 (compound 23) is a potent and non-selective PARP inhibitor, targeting to mono-ADP-ribosyltransferases ARTD7/PARP15, ARTD8/PARP14, ARTD10/PARP10 and poly(ADP-ribose) polymerase-1 (ARTD1/PARP1) with IC50s of 1.7 μM, 1.6 μM, 0.8 μM, and 4.4 μM, respectively .
|
-
- HY-12762
-
QS11
2 Publications Verification
|
β-catenin
Wnt
Arf Family GTPase
|
Cancer
|
|
QS11 is an inhibitor of ARFGAP1 (ADP-ribosylation factor GTPase-activating protein 1), with an EC50 of 1.5 μM. QS11 activates Wnt/β-catenin signaling through an effect on protein trafficking. QS11 inhibits migration of ARFGAP overexpressing breast cancer cells .
|
-
- HY-119860
-
|
ONO 41483
|
Drug Derivative
|
Cardiovascular Disease
|
|
Ataprost (ONO 41483) is an orally active Carboprostacyclin (HY-112322) analogue. Ataprost exhibits 2.6 times more active than Carboprostacyclin in inhibiting ADP-induced platelet aggregation in vitro. Ataprost has the ability to relieve coronary spasm .
|
-
- HY-123490
-
|
INS50589
|
P2Y Receptor
|
Inflammation/Immunology
|
|
Regrelor disodium (INS 50589) is a platelet P2Y12 receptor antagonist. Regrelor disodium is a well-tolerated, reversible ADP competitive antagonist. Regrelor disodium inhibits cell proliferation. Regrelor disodium can be used in inflammation-related research .
|
-
- HY-112433A
-
|
|
NF-κB
Drug Isomer
|
Inflammation/Immunology
|
|
(S)-NIK SMI1 is the isomer of NIK SMI1 (HY-112433), and can be used as an experimental control. NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM.
|
-
- HY-150207
-
|
|
PARP
|
Inflammation/Immunology
|
|
RBN-3143 is a potent and NAD+-competitive catalytic PARP14 inhibitor with an IC50 value of 4 nM. RBN-3143 inhibits PARP14-mediated ADP-ribosylation and stabilizes PARP14 in cell lines. RBN-3143 can be used in research of lung inflammation .
|
-
- HY-U00235
-
|
|
Integrin
|
Inflammation/Immunology
|
|
SR121566A is a novel non-peptide Glycoprotein IIb/IIIa (GP IIb-IIIa) antagonist, which can inhibit ADP-, arachidonic acid- and collagen-induced human platelet aggregation with IC50s of 46±7.5, 56±6 and 42±3 nM, respectively.
|
-
- HY-108657
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 is a selective and high affinity P2Y1 receptor antagonist, with a Ki of 2.5 nM and an IC50 of 51.6 nM. MRS2279 competitively inhibits ADP-promoted platelet aggregation with an apparent affnity (pKB=8.05) .
|
-
- HY-113371
-
|
Methylcitric acid
|
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Methylcitric acid (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate .
|
-
- HY-B0887BR
-
|
(-)-trans-NRDC-143 (Standard); (1S)-trans-Permethrin (Standard)
|
Insecticide
Reference Standards
|
Others
|
|
Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for research and analytical applications. Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart .
|
-
- HY-128760
-
COH34
1 Publications Verification
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
COH34 is a potent and specific poly(ADP-ribose) glycohydrolase (PARG) inhibitor with an IC50 of 0.37 nM. COH34 binds to the catalytic domain of PARG (Kd=0.547 μM), thereby prolonging PARylation at DNA lesions and trapping DNA repair factors .
|
-
- HY-113432R
-
|
2PY (Standard)
|
Reference Standards
Endogenous Metabolite
PARP
|
Metabolic Disease
|
|
Nudifloramide (Standard) is the analytical standard of Nudifloramide. This product is intended for research and analytical applications. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
|
-
- HY-112658
-
|
|
Adrenergic Receptor
Adenosine Receptor
|
Endocrinology
|
|
p-Iodoclonidine hydrochloride is a partial agonist of α2-adrenergic receptor. p-Iodoclonidine hydrochloride also has minimal agonist activity in inhibiting adenylate cyclase in platelet membranes, and potentiates ADP induced platelet aggregation with an EC50 of 1.5 μM .
|
-
- HY-100540
-
|
GCA
|
Enterovirus
|
Infection
Cancer
|
|
Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1 . Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species .
|
-
- HY-127111
-
|
|
ATP Citrate Lyase
|
Cancer
|
|
NDI-091143 is a potent and high-affinity human ATP-citrate lyase (ACLY) inhibitor with an IC50 of 2.1 nM (ADP-Glo assay), a Ki of 7.0 nM and a Kd of 2.2 nM. NDI-091143 inhibits ACLY catalysis allosterically, by stabilizing large conformational changes in the citrate domain that indirectly block the binding and recognition of citrate .
|
-
- HY-W419570
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
(Rac)-BX 048 is a BX 048 racemate. BX 048 is a P2Y12 receptor antagonist. BX 048 inhibits ADP-induced platelet aggregation in human, dog and rat whole blood. BX 048 also inhibits Arachidonic acid (HY-109590) induced platelet aggregation (IC50 of 15 μM) .
|
-
- HY-152949
-
|
|
Myosin
|
Neurological Disease
|
|
Myosin V-IN-1 (compound 8) is a potent and selective Myosin V inhibitor, with a Ki of 6 μM. Myosin V-IN-1 shows acute inhibition of myosin V. Myosin V-IN-1 slows the actin-activated myosin V ATPase by specifically inhibiting ADP release from the actomyosin complex .
|
-
- HY-123669A
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
Trans-R-138727 is the trans isomer of R-138727 (HY-123669). R-138727 is the active metabolite of the antiplatelet agent Prasugrel (HY-15284). R-138727 is an irreversible inhibitor for the platelet receptor P2Y12, and inhibits ADP-induced platelet activation and aggregation .
|
-
- HY-W009276
-
|
Methyl GLA
|
Apoptosis
|
Cancer
|
|
γ-Linolenic Acid methyl ester (Methyl GLA) is an esterified version of γ-Linolenic Acid (GLA), which is an ω-6 fatty acid, serves as melanoma cell proliferation inhibitors. γ-Linolenic Acid methyl ester inhibits ADP-induced blood platelet aggregation and induces apoptosis .
|
-
- HY-121881
-
|
|
HSP
|
Cancer
|
|
PU3 is an Hsp90 inhibitor that competes with geldanamycin (GM) and others for the conserved ATP/ADP pocket of Hsp90. PU3 also induces degradation of proteins such as Her2 and inhibits breast cancer cell growth by causing retinoblastoma protein hypophosphorylation, G1 arrest, and cell differentiation. PU3 has the potential to be a cancer inhibitor. .
|
-
- HY-108657A
-
|
|
P2Y Receptor
|
Neurological Disease
|
|
MRS2279 diammonium is a selective and high affinity P2Y1 receptor antagonist, with a Ki value of 2.5 nM and an IC50 value of 51.6 nM. MRS2279 diammonium competitively inhibits ADP-promoted platelet aggregation with an pKb value of 8.05 .
|
-
- HY-N14932
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Aggreceride A is a platelet aggregation inhibitor. Aggreceride A shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen .
|
-
- HY-132157
-
|
|
PARP
|
Cancer
|
|
8-Chloroquinazolin-4-ol is a poly (ADP-ribose) polymerase-1 (PARP-1) inhibitor with an IC50 value of 5.65 μM. 8-Chloroquinazolin-4-ol can be used in cancer-related research .
|
-
- HY-W686186
-
|
|
Drug Metabolite
P2Y Receptor
|
Cardiovascular Disease
|
|
Prasugrel hydroxy thiolactone (compound M18) is a metabolite of Prasugrel (HY-15284). Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits Adenosine 5'-diphosphate (ADP, HY-W010918)-induced platelet aggregation .
|
-
- HY-167927S
-
|
|
Isotope-Labeled Compounds
PARP
|
Cancer
|
|
Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
|
-
- HY-171789
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
PARG-IN-7 (Example 38) is a Poly ADP-ribose glycohydrolase (PARG) inhibitor (IC50: < 0.1 μM). PARG-IN-7 inhibits cell viability of HCC1806-XRCC1 KD (knock down) cells with an IC50 < 1 μM. PARG-IN-7 can be used for cancer research .
|
-
- HY-19175
-
|
FR-144633
|
Thrombin
Integrin
|
Cardiovascular Disease
|
|
FK 633 (FR-144633) is a fibrinogen inhibitor and peptide mimetic GPⅡbⅡa receptor antagonist. FK 633 has anti-platelet and anti-thrombotic effects. FK 633 inhibits ADP-, collagen-, thrombin-, and PAF-induced platelet aggregation with IC50 values of 103, 87, 98, and 239 nM, respectively .
|
-
- HY-162237
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-13 (compound 28) is a selective inhibitor for receptor-interacting serine/threonine-protein kinase 1 (RIPK1), the inhibitory activity is measured by ADP-Glo Kinase Assay with a pKi of 7.66. RIPK1-IN-13 inhibits human leukaemia cells U937 with a pIC50 of 7.2 .
|
-
- HY-121497
-
|
3-MBA
|
PARP
Bacterial
|
Cancer
|
|
3-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells . 3-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum) .
|
-
- HY-113371A
-
|
Methylcitric acid trisodium
|
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Methylcitric acid trisodium (Methylcitric acid trisodium) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid trisodium accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid trisodium markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate .
|
-
- HY-N14933
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Aggreceride B is a platelet aggregation inhibitor. Aggreceride B shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen .
|
-
- HY-113432S
-
|
|
Endogenous Metabolite
PARP
|
Metabolic Disease
|
|
Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
|
-
- HY-N14934
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Cardiovascular Disease
|
|
Aggreceride C is a platelet aggregation inhibitor. Aggreceride C shows an inhibitory activity against aggregation induced by Adenosine 5'-diphosphate (ADP) (HY-W010918), Arachidonic acid (HY-109590) and PAF (platelet activating factor), but was less active against aggregation induced by collagen .
|
-
- HY-112433
-
|
|
NF-κB
|
Inflammation/Immunology
|
|
NIK SMI1 is a potent, selective NF-κB inducing kinase (NIK) inhibitor, which inhibits NIK-catalyzed hydrolysis of ATP to ADP with IC50 of 0.23±0.17 nM. NIK SMI1 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-18901
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase .
|
-
- HY-134280
-
|
Nicotinamide 8-Br-hypoxanthine dinucleotide
|
Drug Derivative
|
Others
|
|
8-Br-NHD+ (Nicotinamide 8-Br-hypoxanthine dinucleotide) is a derivative of NAD+ (nicotinamide adenine dinucleotide) that acts as a potential substrate, competitive inhibitor or modulator of enzymes that interact with β-NAD+. 8-Br-NHD+ can be used to synthesize a cyclic ADP nucleotide (cADPR) analog .
|
-
- HY-134556
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
2'-Hydroxyflavanone is a flavanone that can inhibit cancer cell proliferation, induce apoptosis, and reduce inflammation. 2'-Hydroxyflavanone shows inhibitory effect on platelet aggregation caused by two inducers with IC50s 47.8 μM arachidonic acid (AA) and 147.2 μM aenosine diphosphate (ADP) .
|
-
- HY-14206
-
|
|
PARP
|
Cancer
|
|
NU 1085 is a potent poly(ADP-ribose) polymerase (PARP) inhibitor with a Ki of 6 nM. NU 1085 shows strong cytotoxicity to cancer cells (LC50 = 83-94 μM) and can enhance the anticancer effect of Temozolomide (HY-17364). NU 1085 can be used for the research of cancer, such as lung cancer .
|
-
- HY-129522
-
|
CZ-48
|
Toll-like Receptor (TLR)
|
Neurological Disease
|
|
Sulfo-ara-F-NMN (CZ-48) is a mimetic of nicotinamide mononucleotide (NMN). Sulfo-ara-F-NMN acts selectively, activating SARM1 but inhibiting CD38 (IC50 around 10 μM). Sulfo-ara-F-NMN induces intracellular cyclic ADP-ribose (cADPR) production .
|
-
- HY-137742
-
|
|
ULK
Autophagy
|
Cancer
|
|
SBP-7455 is a potent, high affinity and orally active dual ULK1/ULK2 autophagy inhibitor with IC50s of 13 nM and 476 nM in the ADP-Glo assays, respectively. SBP-7455 potently inhibits ULK1/2 enzymatic activity and can be used for triple-negative breast cancer (TNBC) research .
|
-
- HY-111557
-
YM-254890
Maximum Cited Publications
17 Publications Verification
|
P2Y Receptor
|
Cardiovascular Disease
|
|
YM-254890 is a selective Gαq/11 protein inhibitor isolated from Chromobacterium sp. YM-254890 shows no inhibition of other G protein subtypes. YM-254890 inhibits platelet aggregation induced by ADP by blocking the P2Y1 signal transduction pathway, with an IC50 value below 0.6 μM .
|
-
- HY-167686
-
|
Homopisatin
|
Integrin
|
Cardiovascular Disease
|
|
Variabilin (Homopisatin) is a potent RGD-containing antagonist of glycoprotein IIb-IIIa and platelet aggregation inhibitor from the hard tick Dermacentor variabilis. Variabilin potently inhibits platelet aggregation induced by the platelet agonists ADP, collagen, and thrombin receptor peptide SFLLRNP. Variabilin also blocks platelet adhesion to immobilized Fg. In addition, Variabilin inhibits binding of purified human GPIIb-IIIa to immobilized Fg .
|
-
- HY-B0889R
-
|
Acrinol monohydrate (Standard)
|
Reference Standards
Bacterial
|
Infection
|
|
Ethacridine (lactate monohydrate) (Standard) is the analytical standard of Ethacridine (lactate monohydrate). This product is intended for research and analytical applications. Ethacridine lactate (Acrinol) monohydrate is a widely used antiseptic and abortifacient. Ethacridine lactate monohydrate is effective against Staphylococcus aureus and other gram-positive cocci. Ethacridine lactate monohydrate is also a poly(ADP-ribose) glycohydrolase (PARG) inhibitor .
|
-
- HY-108658
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
MRS2500 tetraammonium is a potent, selective and stable antagonist of the P2Y1 receptor (Ki=0.78 nM for recombinant human P2Y1 receptor). MRS2500 tetraammonium inhibits the ADP-induced aggregation of human platelets with an IC50 value of 0.95 nM. Antithrombotic activity .
|
-
- HY-15045A
-
|
|
PARP
|
Cancer
|
|
INO-1001 mesylate is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 mesylate is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death . INO-1001 mesylate has anti-tumor effects .
|
-
- HY-155348
-
|
|
PARP
|
Cancer
|
|
Ru3 is a poly(ADP-ribose) polymerase 1 inhibitor. Ru3 induces apoptosisin MCF-7 cells by multiple modes, inclusive of inducing DNA damage, suppressing DNA damage repair, disturbing cell cycle distribution, decreasing the mitochondrial membrane potential, and increasing the intracellular reactive oxygen species levels .
|
-
- HY-P2764
-
Apyrase
3 Publications Verification
|
NTPDase
|
Inflammation/Immunology
|
|
Apyrase is an Nucleoside triphosphate diphosphohydrolase (NTPDase). Apyrase can hydrolyze extracellular adenosine triphosphate (ATP) and adenosine diphosphate (ADP). Apyrase can inhibit Stx2 toxin release of enterohemorrhagic Escherichia coli (EHEC) infection and protect the intestinal barrier function. Apyrase can be used for the research of infection and inflammation, such as hemorrhagic colitis .
|
-
- HY-15045
-
|
|
PARP
|
Cancer
|
|
INO-1001 is a potent and selective poly (ADP-ribose) polymerase (PARP) inhibitor. INO-1001 is a potent enhancer of radiation sensitivity and enhances radiation-induced cell killing by interfering with DNA repair mechanisms, resulting in necrotic cell death . INO-1001 has anti-tumor effects .
|
-
- HY-105692
-
|
|
PARP
|
Neurological Disease
|
|
DR2313 is a potent, selective, competitive and brain-penetrant inhibitor of poly(ADP-ribose) polymerase (PARP), with IC50s of 0.20 μM and 0.24 μM for PARP-1 and PARP-2, respectively. DR2313 exhibits neuroprotective effects on ischemic injuries in vitro and in vivo .
|
-
- HY-100540A
-
|
(Rac)-GCA
|
Enterovirus
|
Infection
|
|
(Rac)-Golgicide A ((Rac)-GCA) is a racemate of Golgicide A. Golgicide A (GCA) is a potent, highly specific, and reversible inhibitor of the cis-Golgi ADP-ribosylation factor guanine nucleotide exchange factors (ArfGEF) GBF1 .Golgicide A drastically reduced replication of coxsackievirus B3 (CVB3) and other human enterovirus species .
|
-
- HY-112175R
-
|
N-Omega-acetylhistamine (Standard)
|
Reference Standards
Histamine Receptor
Endogenous Metabolite
|
Inflammation/Immunology
Endocrinology
|
|
Ethacridine (lactate monohydrate) (Standard) is the analytical standard of Ethacridine (lactate monohydrate). This product is intended for research and analytical applications. Ethacridine lactate (Acrinol) monohydrate is a widely used antiseptic and abortifacient. Ethacridine lactate monohydrate is effective against Staphylococcus aureus and other gram-positive cocci. Ethacridine lactate monohydrate is also a poly(ADP-ribose) glycohydrolase (PARG) inhibitor .
|
-
- HY-105514
-
|
|
Drug Derivative
|
Cardiovascular Disease
|
|
KP-10614 is a potent, orally active platelet aggregation inhibitor. KP-10614 inhibits platelet aggregation induced by ADP with IC50 of 1 nM. KP-10614 causes dose-dependent inhibition of ex vivo platelet aggregation in rats. KP-10614 shows antithrombotic effects in various thrombosis models. KP-10614 can be used for thrombotic diseases research .
|
-
- HY-P992446
-
|
|
NTPDase
|
Cancer
|
|
PUR001 is a monoclonal antibody targeting NTPDase 1 (CD39). PUR001 blocks the hydrolysis of extracellular ATP and ADP into AMP by inhibiting CD39, reduces the production of immunosuppressive adenosine, and increases extracellular ATP concentration to activate anti-tumor immune responses. PUR001 can be used in studies related to solid tumors .
|
-
- HY-123786
-
|
|
Apoptosis
Caspase
|
Cancer
|
|
NSC745887 (compound 25) is an inhibitor that targets DNA topoisomerase cleavage, activates the caspase-8/9-caspase-3-poly (ADP-ribose) polymerase cascade, and induces apoptosis in cancer cells. NSC745887 enhances γH2AX expression and causes DNA fragmentation leading to DNA damage .
|
-
- HY-182499
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-56 (Compound RCY) is an I-labeled poly(ADP−ribose) polymerase (PARP1) inhibitor. PARP1-IN-56 can be radiolabeled with 211At or 125I for use as an α-emitting radiotherapeutic agent. PARP1-IN-56 can be used for the research of cancer .
|
-
- HY-148754
-
|
|
PARP
|
Cancer
|
|
PARP10-IN-3 is a selective mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 480 nM for human PARP10. PARP10-IN-3 reveals potent inhibition on PARP2 and PARP15 with IC50s of 1.7 μM for human PARP2 and human PARP15, respectively .
|
-
- HY-N1462
-
|
|
Chloride Channel
Autophagy
mTOR
AMPK
|
Cardiovascular Disease
Metabolic Disease
Cancer
|
|
Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
|
-
- HY-176456
-
|
|
PARP
|
Inflammation/Immunology
Cancer
|
|
PARP14 inhibitor 2 (Compound 3) is an orally active and highly selective PARP14 inhibitor with an IC50 value of <30 nM. PARP14 inhibitor 2 inhibits the mono-ADP-ribosyltransferase activity of PARP14 and regulates IFN-γ and IL-4 signaling, reversing protumor macrophage polarization and inhibiting anti-tumor inflammatory responses. PARP14 inhibitor 2 is promising for research of PARP14-related diseases such as tumors, atopic dermatitis and autoimmune diseases .
|
-
- HY-124371
-
|
|
Phosphodiesterase (PDE)
|
Cardiovascular Disease
|
|
Amentoflavone hexaacetate is a 3,5-cyclic nucleotide phosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects .
|
-
- HY-152696
-
|
|
Xanthine Oxidase
Nucleoside Antimetabolite/Analog
|
Others
|
|
6-O-Methylinosine is a hypoxanthine analogue. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-168023
-
|
|
NOD-like Receptor (NLR)
|
Inflammation/Immunology
|
|
NOD1/-IN-1 (Compound 2) is a potent RIPK2 inhibitor with an IC50 value of 0.65 nM determined by ADP-Glo assays. NOD1/-IN-1 selectively inhibits the NOD1 pathway (with an IC50 of 33 nM for NOD1), blocking the production of pro-inflammatory cytokines and thereby reducing inflammation. NOD1/-IN-1 is applicable for research in the field of colitis .
|
-
- HY-184191
-
|
|
Phosphoglycerate Kinase (PGK)
|
Cancer
|
|
PGK1-IN-3 is an orally active PGK1 inhibitor with human PGK1 IC50 values of 0.48 μM and human PGK1 Kd of 63 nM. PGK1-IN-3 binds to the ADP-binding pocket of PGK1, inhibits glycolysis, and reduces glucose consumption and lactate production. PGK1-IN-3 can be used for the research of pancreatic cancer .
|
-
- HY-B0097
-
|
5-Fluorouracil 2'-deoxyriboside
|
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Infection
Cancer
|
|
Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
|
-
- HY-178468
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-47 (Compound 35) is a highly selective PARP1 inhibitor (IC50 <100 nM). PARP1-IN-47 blocks poly(ADP-ribosyl)ation and disrupts DNA damage repair pathways to induce tumor cell apoptosis. PARP1-IN-47 is promising for research of solid tumors and hematological malignancies .
|
-
- HY-113371S
-
|
Methylcitric acid-d3
|
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Methylcitric acid-d3 is the deuterium labeled 2-Methylcitric acid. 2-Methylcitric acid (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate .
|
-
- HY-Z0283
-
|
Benzenecarboxamide; Phenylamide
|
Endogenous Metabolite
PARP
|
Others
|
|
Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
|
-
- HY-10885
-
|
ABT-472
|
PARP
|
Cancer
|
|
A-620223 succinate (ABT-472) is an orally available poly(ADP-ribose) polymerase (PARP) inhibitor. A-620223 succinate (ABT-472) exhibits very good potency against the PARP-1 enzyme with a Ki value of 8 nM and an EC50 value of 3 nM in whole cell assay, making it useful in cancer research .
|
-
- HY-17459
-
|
(S)-(+)-Clopidogrel bisulfate; (S)-(+)-Clopidogrel hydrogen sulfate
|
Cytochrome P450
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
|
Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively . Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation ．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor .
|
-
- HY-W039271
-
|
2-Chloro-6-O-methyl-inosine
|
Nucleoside Antimetabolite/Analog
Xanthine Oxidase
|
Cancer
|
|
2-Chloro-6-methoxypurine riboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-154017
-
|
|
Nucleoside Antimetabolite/Analog
Xanthine Oxidase
|
Cancer
|
|
2′-C-Methyl-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-164717
-
|
|
Poly(ADP-ribose) Glycohydrolase (PARG)
|
Cancer
|
|
FORX-428 is a selective and orally active Poly (ADP-ribose) glycohydrolase (PARG) inhibitor. FORX-428 exhibits strong and reversible binding to the catalytic domain of human PARG, and thereby inhibits PARG´s enzymatic activity. FORX-428 leads to the excessive accumulation of PAR chains and activates DNA damage and replication stress responses. FORX-428 selectively inhibits the proliferation of various cancer cell lines, including breast, ovarian, and gastric cancer .
|
-
- HY-148300
-
|
|
P2Y Receptor
|
Cardiovascular Disease
|
|
AR-C66096 is a potent and selective antagonist of the Gi-coupled P2Y12 receptor. AR-C66096 suppresses platelet thrombus stability under physiological flow conditions. AR-C66096 inhibits ADP-induced aggregation in whole blood aggregometry. AR-C66096 can be used for antithrombotic research .
|
-
- HY-113432S2
-
|
2PY-13C,d3
|
Isotope-Labeled Compounds
Endogenous Metabolite
PARP
|
Metabolic Disease
|
|
Nudifloramide- 13C,d3 (2PY- 13C,d3) is the 13C- and deuterium labeled Nudifloramide (HY-113432). Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
|
-
- HY-155807
-
|
|
STAT
JAK
Apoptosis
|
Cancer
|
|
DPP is a Platinum(IV) complex, bearing pterostilbene-derived axial ligand. DPP inhibit the JAK2-STAT3 pathway in breast cancer (BC) cells with antiproliferative activity, and activates caspase-3 and cleaved poly ADP-ribose polymerase to induces apoptosis. DPP promotes the maturation and antigen presentation of dendritic cells, and exhibits in vivo safety .
|
-
- HY-181158
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-52 is a poly(ADP-ribose) polymerase-1 (PARP-1) inhibitor that forms stable interactions with the PARP-1 active site. PARP1-IN-52 exerts anticancer activity against breast cancer cells. PARP1-IN-52 can be used for the research of breast cancer .
|
-
- HY-148753
-
|
|
PARP
|
Cancer
|
|
PARP10-IN-2 is a potent mono‐ADP‐ribosyltransferase PARP10 inhibitor with an IC50 of 3.64 μM for human PARP10. PARP10-IN-2 reveals potent inhibition on PARP2 and PARP15 with IC50s of 27 μM and 11 μM for human PARP2 and human PARP15, respectively .
|
-
- HY-137626
-
|
|
P2Y Receptor
|
Others
|
|
Sp-ATPαS is a regulator of ATP-binding proteins. Sp-ATPαS is a competitive antagonist of the human P2Y1 receptor, which can inhibit the calcium signal induced by ADP. Sp-ATPαS is metabolically more stable than ATP . Sp-ATPαS can be used to study the binding patterns of metals and nucleotides in enzymatic reactions.
|
-
- HY-161570
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-12 (compound 1) inhibits the activity of LRRK2 G20195 (IC50=0.45 nM), LRRK2 WT (IC50=1.1 nM) and LRRK2 WT ADP-Glo (IC50=0.46 nM). LRRK2-IN-12 can be used for Alzheimer's Disease research .
|
-
- HY-N5021
-
|
AHSYB
|
Others
|
Neurological Disease
|
|
Anhydrosafflor yellow B (AHSYB) is a quinochalcone C-glycoside isolated from Carthamus tinctorius. Anhydrosafflor yellow B inhibits ADP-induced platelet aggregation, exhibits significant anti-oxidative effects in vitro, and possesses certain activity against H2O2-induced cytotoxicity in cultured PC12 cells and primary neuronal cells .
|
-
- HY-182246
-
|
|
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
MC2050 is a selective PARP-1 inhibitor with an IC50 of 119 nM. MC2050 functionally inhibits PARP-1 activity, including hyperactivation induced by oxidative stress, and reduces the poly (ADP-ribosyl) ation level of histone H1. MC2050 protects neuroblastoma cells from oxidative stress-mediated cell death induced by hydrogen peroxide. MC2050 is applicable to research related to neuroblastoma and Burkitt lymphoma .
|
-
- HY-171543
-
|
|
PARP
|
Cancer
|
|
PARP1-IN-37 (Compound 8) is an orally active and selective poly(ADP-ribose) polymerase 1 and 2 (PARP1/2) inhibitor with an IC50 value of 24 nM for PARP1. PARP1-IN-37 inhibits PARP activity in cells with an EC50 value of 3.7 μM. PARP1-IN-37 is promising for research of BRCA-mutated tumors, such as breast and ovarian cancers .
|
-
- HY-B1263
-
|
|
Environmental Pollutants
Bacterial
Fungal
|
Infection
Neurological Disease
|
|
Chlorobutanol is an orally active and potent inhibitor of platelet aggregation and release and a pharmaceutical preservative with antibacterial activity. Chlorobutanol inhibits thromboxane B2 formation, ATP release, and elevation of cytosolic free calcium caused by collagen, ADP, epinephrine, arachidonic acid and thrombin. Chlorobutanol is active against a wide variety of Gram-positive and Gram-negative bacteria, and several mold spores and fungi. Chlorobutanol is widely used in food and cosmetic industry .
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- HY-154393
-
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Nucleoside Antimetabolite/Analog
Xanthine Oxidase
|
Cancer
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2-Chloro-2'-deoxy-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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- HY-125209
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DNA/RNA Synthesis
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Cancer
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TH5427 is a promising, targeted inhibitor that can be used to further study NUDT5 activity and ADP-ribose metabolism. TH5427, blocks progestin-dependent, PAR-derived nuclear ATP synthesis and subsequent chromatin remodeling, gene regulation and proliferation in breast cancer cells. NUDT5 is recently identified as a rheostat of hormone-dependent gene regulation and proliferation in breast cancer cells .
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-
- HY-175986
-
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Prostaglandin Receptor
|
Inflammation/Immunology
|
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IP receptor agonist 1 (compound 6c-14S) is an orally active I prostanoid receptor agonist, with an IC50 of 0.15 μM for inhibiting platelet aggregation induced by ADP (HY-W010918,300 μM) in rabbit platelet-rich plasma. IP receptor agonist 1 can be used for study of Pulmonary arterial hypertension .
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- HY-137626A
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P2Y Receptor
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Others
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Sp-ATPαS tetrasodium is a thiophosphonate analogue of ATP. Sp-ATPαS tetrasodium is a competitive antagonist of the human P2Y1 receptor and can inhibit the calcium signal induced by ADP. Sp-ATPαS tetrasodium has higher metabolic stability than ATP. Sp-ATPαS tetrasodium can be used to study the binding mode of metal-nucleotide in enzymatic reactions .
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- HY-W051513R
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Reference Standards
PARP
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Others
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|
2-Methylquinazolin-4-ol (Standard) is the analytical standard of 2-Methylquinazolin-4-ol. This product is intended for research and analytical applications. 2-Methylquinazolin-4-ol is a potent competitive poly(ADP-ribose) synthetase inhibitor, with a Ki of 1.1 μM. 2-Methylquinazolin-4-ol mammalian aspartate transcarbamylase (ATCase) inhibitor, with 0.20 mM[1][2].
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- HY-121497R
-
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3-MBA (Standard)
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PARP
Bacterial
Reference Standards
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Cancer
|
|
3-Methoxybenzamide (Standard) is the analytical standard of 3-Methoxybenzamide. This product is intended for research and analytical applications. 3-Methoxybenzamide (3-MBA), an inhibitor of ADP-ribosyltransferase (ADPRTs) and PARP, inhibits cell division in Bacillus subtilis, leading to filamentation and eventually lysis of cells . 3-Methoxybenzamide (3-MBA) enhances in vitro plant growth, microtuberization, and transformation efficiency of blue potato (Solanum tuberosum L. subsp. andigenum) .
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- HY-W009276R
-
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Methyl GLA (Standard)
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Reference Standards
Apoptosis
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Cancer
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|
γ-Linolenic Acid methyl ester (Standard) is the analytical standard of γ-Linolenic Acid methyl ester. This product is intended for research and analytical applications. γ-Linolenic Acid methyl ester (Methyl GLA) is an esterified version of γ-Linolenic Acid (GLA), which is an ω-6 fatty acid, serves as melanoma cell proliferation inhibitors. γ-Linolenic Acid methyl ester inhibits ADP-induced blood platelet aggregation and induces apoptosis .
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- HY-119992
-
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PARP
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Cancer
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CEP-6800 is an inhibitor of PARP-1 with chemopotentiating ability. CEP-6800 attenuates irinotecan (HY-16562)- and Temozolomide (HY-17364)-induced poly(ADP-ribose) accumulation in LoVo as well as HT29 xenografts. CEP-6800 can suppress Calu-6 tumor growth. CEP-6800 can be studied in anti-cancer research .
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- HY-113096S
-
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PGD1-d4
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
|
Prostaglandin D1-d4 (PGD1-d4) is deuterium labeled Prostaglandin D1. Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
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- HY-W141392
-
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Nucleoside Antimetabolite/Analog
Xanthine Oxidase
Phosphoramidites
|
Cancer
|
|
2'-Fluoro-5'-O-DMT-2'-deoxyinosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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- HY-W392836
-
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Nucleoside Antimetabolite/Analog
Xanthine Oxidase
Phosphoramidites
|
Cancer
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2'-O-Methyl-5'-O-dmt-inosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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- HY-152678
-
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Nucleoside Antimetabolite/Analog
Xanthine Oxidase
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Cancer
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6-Methoxypurine-9-β-D-5’(R)-C-methylriboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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- HY-N1462R
-
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Reference Standards
Chloride Channel
Autophagy
mTOR
AMPK
|
Cardiovascular Disease
Metabolic Disease
Cancer
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Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for use in research and analytical applications. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
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- HY-B0097R
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5-Fluorouracil 2'-deoxyriboside (Standard)
|
Reference Standards
Nucleoside Antimetabolite/Analog
DNA/RNA Synthesis
Bacterial
CMV
HSV
Apoptosis
|
Infection
Cancer
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Floxuridine (Standard) is the analytical standard of Floxuridine. This product is intended for research and analytical applications. Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
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- HY-W711852
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Benzenecarboxamide-d5; Phenylamide-d5
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Isotope-Labeled Compounds
PARP
Endogenous Metabolite
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Others
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Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
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- HY-Z0283R
-
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Benzenecarboxamide (Standard); Phenylamide (Standard)
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Reference Standards
Endogenous Metabolite
PARP
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Others
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|
Benzamide (Standard) is the analytical standard of Benzamide. This product is intended for research and analytical applications. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
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- HY-17459R
-
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(S)-(+)-Clopidogrel bisulfate (Standard); (S)-(+)-Clopidogrel hydrogen sulfate (Standard)
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Reference Standards
Cytochrome P450
P2Y Receptor
|
Cardiovascular Disease
Cancer
|
|
Clopidogrel (hydrogen sulfate) (Standard) is the analytical standard of Clopidogrel (hydrogen sulfate). This product is intended for research and analytical applications. Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively . Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation ．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor .
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- HY-17459S
-
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(S)-(+)-Clopidogrel bisulfate-d3; (S)-(+)-Clopidogrel-d3 hydrogen sulfate
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P2Y Receptor
Cytochrome P450
|
Cardiovascular Disease
|
|
Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate . Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor .
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- HY-122658
-
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MB-1
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Mitochondrial Metabolism
|
Metabolic Disease
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MitoBloCK-1 (MB-1) is an inhibitor that blocks the import of substrates that use the TIM22 import pathway. MitoBloCK-1 inhibits import by preventing binding of substrate to tim9/10 complex to the substrate, thus the substrate failed to be reach the TIM22 translocon. MitoBloCK-1 inhibits protein import of TIM22 substrates into mitochondria. MitoBloCK-1 attenuates the import of the carrier proteins including the ADP/ATP and phosphate carriers. MitoBloCK-1 also inhibits the import of an additional carrier protein, PiC, and the outer membrane protein Tom40 .
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-
- HY-150062
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SARS-CoV
|
Infection
|
|
SARS-CoV-2 nsp3-IN-1 (Compound 15c) is a Mac1 (SARS-CoV-2 nsp3 macrodomain) inhibitor with the IC50 value of 6.1 μM. SARS-CoV-2 nsp3-IN-1 can inhibit Mac1 ADP-ribosylhydrolase activity. SARS-CoV-2 nsp3-IN-1 demonstrates notable selectivity for coronavirus macrodomains, especially towards SARS-CoV-2 Mac1 .
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- HY-168024
-
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RIP kinase
NOD-like Receptor (NLR)
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Inflammation/Immunology
|
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NOD1/2-IN-1 (Compound 18) is a potent RIPK2 inhibitor with an IC50 value of 1.4 nM, as determined by the ADP-Glo assay. NOD1/2-IN-1 blocks the production of pro-inflammatory cytokines by inhibiting the NOD1/NOD2 pathways, with IC50 values of 18 nM and 170 nM for NOD1 and NOD2, respectively, thereby reducing inflammatory responses. NOD1/2-IN-1 can be used in studies related to colitis .
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- HY-134273A
-
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8-Bromo-dGTP sodium
|
Nucleoside Antimetabolite/Analog
|
Others
|
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8-Br-dGTP (8-Bromo-dGTP) sodium (Compound 5), an 8-brominated purine nucleotide, is a syn-oriented analog of dGTP. 8-Br-dGTP sodium can be hydrolyzed by the enzyme hMTH1 protein (HY-P74740). 8-Br-dGTP sodium inhibits dGTP-activated ADP reduction with a Ki of 56 μM. 8-Br-dGTP sodium has no significant genotoxicity and mutagenic potentials during DNA synthesis .
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- HY-136778
-
|
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PARP
Reactive Oxygen Species (ROS)
Bcl-2 Family
Caspase
ERK
p38 MAPK
|
Cardiovascular Disease
|
|
INH2BP is a poly(ADP-ribose) polymerase (PARP) inhibitor with antioxidant and anti-apoptotic activities. INH2BP reduces the production of intracellular reactive oxygen species (ROS), modulates the expression of apoptosis-related proteins such as Bax, Bcl-2 and cleaved caspase-3 and enhances cell survival through the activation of the ERK1/2 and p38 MAPK signaling pathways. INH2BP is promising for research of cardiovascular diseases .
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-
- HY-113113S
-
|
13,14-Dihydroprostaglandin E1-d4; PGE0-d4
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Metabolic Disease
|
|
13,14-Dihydro PGE1-d4 (13,14-Dihydroprostaglandin E1-d4) is deuterium labeled 13,14-Dihydro PGE1. 13,14-Dihydro PGE1 is a metabolite of PGE1 (Prostaglandin E1) which inhibits the ADP-induced platelet aggregation (ID50 = 10.8 ng/mL platelet rich plasma) .
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- HY-139039
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PROTACs
CDK
|
Cancer
|
|
BSJ-4-116 is a PROTAC connected by ligands for Cereblon and CDK. BSJ-4-116 is a highly potent and selective CDK12 degrader (PROTAC) with an IC50 of 6 nM. BSJ-4-116 downregulates DDR genes through a premature termination of transcription, primarily through increasing poly(adenylation). BSJ-4-116 exhibits potent antiproliferative effects, alone and in combination with the poly(ADP-ribose) polymerase inhibitor Olaparib (HY-10162) .
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- HY-119725
-
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Environmental Pollutants
Insecticide
|
Infection
|
|
Tetradifon is a broad-spectrum organochlorine insecticide and an inhibitor of the mitochondrial oligomycin sensitivity conferring protein (OSCP), which can be used to control a variety of mites. Tetradifon inhibits energy-related activities such as ADP-stimulated respiration, DNP and Mg 2+-stimulated ATPase, with an IC50 of 4.5-27 nmoL/mg mitochondrial protein. Tetradifon exerts oligomycin-like activity by inhibiting the oxidative phosphorylation process, inducing oxidative stress and interfering with bone metabolism. Tetradifon is currently mainly used in the research of mitochondrial function regulation, bone remodeling mechanism and nephrotoxicity of environmental pollutants .
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-
- HY-78263
-
MNS
3 Publications Verification
NSC 170724; 5-(2-Nitrovinyl)benzodioxole
|
Src
Syk
NOD-like Receptor (NLR)
Integrin
PANoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
MNS (NSC 170724), the beta-nitrostyrene derivative, is an orally active tyrosine kinase inhibitor, a broad-spectrum antiplatelet agent, and a PANoptosis inhibitor. MNS inhibits Src, Syk, and FAK with IC50 of 27.3, 2.8, and 97.6 μM, respectively. MNS inhibits NLRP3 inflammasome and β1 integrin. MNS completely inhibits U46619, ADP-, arachidonic acid-, collagen-, and thrombin-induced platelet aggregation with IC50 values of 2.1, 4.1, 5.8, 7.0, and 12.7 μM, respectively. MNS is cytotoxic to a variety of cells .
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- HY-100847
-
|
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PARP
|
Cancer
|
|
AZ0108 is an inhibitor for poly ADP-ribose polymerase (PARP), which inhibits PARP1, PARP2, PARP3, PARP6, TNKS1, TNKS2, with IC50s of <0.03, <0.03, 2.8, 0.083, 3.2, >3 μM, respectively. AZ0108 prevents centrosome clustering with an EC50 of 0.053 μM, and exhibits cytotoxicity in cell OCI-LY-19 with GI50 of 0.017 μM. AZ0108 exhibits good in vivo pharmacokinetic characters in rat/mouse models .
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-
- HY-120380
-
|
|
MOFs
PARP
|
Neurological Disease
|
|
FeTMPyP is an orally active poly (ADP-ribose) polymerase (PARP) inhibitor. FeTMPyP inhibits cell death, nitrotyrosine formation, and depolarization of mitochondrial transmembrane potential. FeTMPyP reduces homocysteine-induced nitrosative stress and partially restores TFEB protein and mRNA levels. FeTMPyP improves functional and behavioral deficits caused by chronic constriction injury in rats. FeTMPyP alleviates acute cerebral infarction in a rat model of middle cerebral artery occlusion with mild hyperglycemia. FeTMPyP can be used in studies related to neuropathic pain, renal aging, ischemic penumbra, and hyperglycemic stroke .
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-
- HY-178150
-
|
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Wee1
|
Cancer
|
|
WEE1-IN-14 (Compound 14) is a selective WEE1 inhibitor (IC50: 0.5 nM in L-RB-FEP calculations, 1.0 nM in ADP-Glo kinase assay). Inhibition of Wee1 in cancer cells disrupts the G2-M checkpoint, removes the regulatory controls on the cell cycle, and leads to early onset of mitotic failure followed by apoptosis of tumor cells. Therefore, WEE1-IN-14 is a useful tool for studying cancer biology .
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-
- HY-124253
-
|
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p97
|
Cancer
|
|
SMDC818909 is an indole amide-derived uncompetitive inhibitor targeting p97 AAA+ ATPase, with an IC50 of 3.5 μM and a Ka of 9.1 μM. SMDC818909 binds to the D2 ATPase domain of p97, preferentially associates with the ADP-bound conformation of p97, allosterically blocks the ATP hydrolysis cycle of p97, and inhibits its mediated intracellular protein homeostasis regulatory function. SMDC818909 is applied to the research and development of p97-targeted antitumor drugs, as well as studies on cancer-related proteotoxic stress mechanisms .
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-
- HY-141867
-
|
Z-Phe-Phe-FMK
|
Cathepsin
MEK
Caspase
DNA/RNA Synthesis
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
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- HY-N0466
-
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Glycosidase
HMG-CoA Reductase (HMGCR)
Fatty Acid Synthase (FASN)
LDLR
|
Others
|
|
Rebaudioside A is an orally effective steviol glycoside with high sweetness. Rebaudioside A acts as an inhibitor of α-glucosidase with an IC50 value of 35.01 μg/mL. Rebaudioside A increases the ATP/ADP ratio in β cells in a glucose-dependent manner, thereby inhibiting KATP channels, leading to membrane depolarization, calcium influx, and ultimately stimulating insulin secretion. Rebaudioside A activates the SREBP signaling pathway by inhibiting HMGCR, the rate-limiting enzyme in cholesterol synthesis, resulting in increased expression of LDLR on the cell surface, thus promoting the uptake of LDL-C in the blood. Rebaudioside A can be used for studies on blood glucose and lipid regulation as well as anti-obesity .
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-
- HY-125217
-
|
|
PARP
|
Cancer
|
|
PARP10-IN-1 is a PARP10 inhibitor with an IC50 of 1.8 μM, 2.7 μM, and >10-fold selectivity over most PARP family members, excluding PARP7 and PARP16.PARP10-IN-1 inhibits PARP10-mediated mono-ADP-ribosylation, including auto-MARylation of PARP10 and MARylation of its protein targets.PARP10-IN-1 is membrane permeable and inhibits PARP10-dependent MARylation in human embryonic kidney cells.PARP10-IN-1 can be used for the research of cancer .
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-
- HY-183548
-
|
|
PARP
|
Inflammation/Immunology
|
|
XW-17 is a PARP14 inhibitor with an IC50 of 3.03 nM and selectivity over other PARP family members.XW-17 suppresses PARP14-mediated mono-ADP-ribosylation, engages and stabilizes endogenous PARP14 protein.XW-17 attenuates skin lesions and decreases expression of IL-4, IL-13, IgE, and IL-17A in an atopic dermatitis-like mouse model.XW-17 can be used for the research of atopic dermatitis .
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-
- HY-N6969A
-
|
|
Adrenergic Receptor
|
Cancer
|
|
Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
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-
- HY-115862
-
|
|
Adenosine Receptor
PARP
Aurora Kinase
|
Cardiovascular Disease
Cancer
|
|
Benzo[c][1,8]naphthyridin-6(5H)-one exhibits low micromolar affinity to human adenosine receptor (AR) A1 and hA2A, with Ki of 4.6 and 4.8 μM. Benzo[c][1,8]naphthyridin-6(5H)-one is inhibitor for poly ADP-ribose polymerase-1 (PARP-1) and aurora kinase A, with IC50 of 0.311 and 5.5 μM .
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-
![Benzo[c][1,8]naphthyridin-6(5H)-one](//file.medchemexpress.com/product_pic/hy-115862.gif)
- HY-113841
-
|
|
Others
Sodium Channel
Potassium Channel
|
Cardiovascular Disease
Inflammation/Immunology
|
|
RS-87337 is an orally active piperazine-amidine hybrid class Ia (inhibiting Vmax, IC50 = 17 μM)/class III (prolonging ADP90, EC15 = 2 μM) antiarrhythmic agent with selectivity for ventricular conduction . RS-87337 inhibits cardiac sodium channel, thereby reducing the maximum depolarization rate of action potential, with moderate onset and recovery kinetics. RS-87337 reduces cardiac outward potassium conductance (I_K), thus prolonging action potential duration. RS-87337 is applicable to research related to arrhythmia, ventricular arrhythmia, ventricular fibrillation, and myocardial ischemia-reperfusion injury .
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-
- HY-115501
-
|
|
Ser/Thr Protease
|
Cancer
|
(E)-FOBISIN101 is a 14-3-3 protein-protein interaction (14-3-3 protein-protein interaction) inhibitor, with IC50 values of 9.3 and 16.4 μM for disrupting the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively. (E)-FOBISIN101 inhibits the binding of 14-3-3 to Raf-1 and proline-rich AKT substrate, and neutralizes the ability of 14-3-3 to activate exotoxin S ADP-ribosyltransferase. (E)-FOBISIN101 is applicable to 14-3-3-mediated cancer research .
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-
- HY-W766548
-
|
5-Fluorouracil 2'-deoxyriboside-13C,15N2
|
Isotope-Labeled Compounds
Apoptosis
Nucleoside Antimetabolite/Analog
CMV
HSV
Bacterial
DNA/RNA Synthesis
|
Cancer
|
|
Floxuridine- 13C, 15N2 (5-Fluorouracil 2'-deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled Floxuridine (HY-B0097). Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
|
-
- HY-N1910
-
|
|
SARS-CoV
Virus Protease
Succinate Receptor 1
ERK
|
Infection
Neurological Disease
|
|
4'-O-Methylbavachalcone is an orally active prenylated flavonoid that inhibits the activity of SARS-CoV papain-like protease (PLpro), with an IC50 of 10.1 μM and a Ki of 4.6 μM. 4'-O-Methylbavachalcone inhibits poly (ADP-ribose) polymerase-mediated cell death (parthanatos), reduces cerebral infarct volume, binds to the orthosteric site of SUCNR1, blocks the interaction between succinate and SUCNR1, inhibits SUCNR1 activity, blocks the nuclear translocation of NFATc4, suppresses the activation of the ERK1/2 signaling pathway, inhibits cardiomyocyte hypertrophy and restores the expression of α-actinin. 4'-O-Methylbavachalcone can be used in studies related to ischemic stroke, SARS-CoV and cardiomyocyte hypertrophy .
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-
- HY-119725R
-
|
|
Reference Standards
Insecticide
|
Infection
|
|
Tetradifon (Standard) is the analytical standard of Tetradifon (HY-119725). This product is intended for research and analytical applications. Tetradifon is a broad-spectrum organochlorine insecticide and an inhibitor of the mitochondrial oligomycin sensitivity conferring protein (OSCP), which can be used to control a variety of mites. Tetradifon inhibits energy-related activities such as ADP-stimulated respiration, DNP and Mg 2+-stimulated ATPase, with an IC50 of 4.5-27 nmoL/mg mitochondrial protein. Tetradifon exerts oligomycin-like activity by inhibiting the oxidative phosphorylation process, inducing oxidative stress and interfering with bone metabolism. Tetradifon is currently mainly used in the research of mitochondrial function regulation, bone remodeling mechanism and nephrotoxicity of environmental pollutants .
|
-
- HY-N0466R
-
|
|
Reference Standards
Glycosidase
HMG-CoA Reductase (HMGCR)
Fatty Acid Synthase (FASN)
LDLR
|
Others
|
|
Rebaudioside A (Standard) is the analytical standard of Rebaudioside A. This product is intended for research and analytical applications. Rebaudioside A is an orally effective steviol glycoside with high sweetness. Rebaudioside A acts as an inhibitor of α-glucosidase with an IC50 value of 35.01 μg/mL. Rebaudioside A increases the ATP/ADP ratio in β cells in a glucose-dependent manner, thereby inhibiting KATP channels, leading to membrane depolarization, calcium influx, and ultimately stimulating insulin secretion. Rebaudioside A activates the SREBP signaling pathway by inhibiting HMGCR, the rate-limiting enzyme in cholesterol synthesis, resulting in increased expression of LDLR on the cell surface, thus promoting the uptake of LDL-C in the blood. Rebaudioside A can be used for studies on blood glucose and lipid regulation as well as anti-obesity.
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- HY-13614
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Microtubule/Tubulin
Apoptosis
Caspase
|
Cardiovascular Disease
Cancer
|
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E7974 is a selective inhibitor of α-tubulin (α-tubulin) with an IC50 of 3.9 μM. E7974 disrupts mitotic spindle formation, induces G2-M phase cell cycle arrest, initiates apoptosis, activates caspase-3, and induces poly (ADP-ribose) polymerase cleavage. E7974 reduces the area of choroidal neovascularization in mouse models, and exerts anti-angiogenic effects when loaded in modified micelles. E7974 can be used in research related to cancer and choroidal neovascularization .
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- HY-Y1094
-
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Chloro(1,5-cyclooctadiene)rhodium(I) dimer
|
Biochemical Assay Reagents
|
Cardiovascular Disease
|
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[Rh(cod)Cl]2 (Chloro(1,5-cyclooctadiene)rhodium(I) dimer) is a rhodium (I) organometallic dimer complex. [Rh(cod)Cl]2 can inhibit platelet-activating factor-mediated platelet aggregation with IC50 values of 5.2 and 43.3 μM in washed rabbit platelets and human platelet-rich plasmas. [Rh(cod)Cl]2 also can inhibit thrombin-, ADP (HY-W010918)- and collagen-induced aggregation with IC50 values of 16.7, 162 and 69.8 μM. [Rh(cod)Cl]2 can be used for the research of cardiovascular disease, such as thrombosis .
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-
![[Rh(cod)Cl]2](//file.medchemexpress.com/product_pic/hy-y1094.gif)
- HY-W195984
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Phosphoglycerate Kinase (PGK)
|
Cancer
|
|
Z57346765 is an inhibitor that targets the ADP-binding pocket of PGK1, with a Kd of 20.9 μM for human PGK1, and exhibits anticancer activity. Z57346765 reduces the activity of the metabolic enzyme PGK1 during glycolysis, regulates lipid peroxidation and cancer cell proliferation, and promotes lipid peroxidation in cervical cancer cells. Z57346765 inhibits the proliferation of cervical cancer and clear cell renal cell carcinoma cells in xenograft mouse models, and induces the expression of genes associated with cell metabolism, DNA replication and cell cycle. Z57346765 is used in research related to cervical cancer, clear cell renal cell carcinoma and breast cancer .
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-
- HY-172747
-
|
|
PARP
|
Cancer
|
|
TNKS-2-IN-3 (Compound 5) is a selective competitive tankyrase 2 (TNKS2) inhibitor with an IC50 value of 0.3 nM, showing over 20-fold selectivity over TNKS1 and more than 100-fold selectivity over PARP1/2. TNKS-2-IN-3 stabilizes axin and suppresses the Wnt/β-catenin pathway by inhibiting TNKS2-mediated ADP-ribosylation, exhibiting antiproliferative activity in colorectal cancer cells. TNKS-2-IN-3 is proming for rasearch of solid tumors with aberrant Wnt pathway activation, such as colorectal cancer .
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-
- HY-137288
-
|
17-Phenyl-PGD2
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
17-Phenyl-18,19,20-trinor-PGD2 (17-Phenyl-PGD2) is an analogue of prostaglandin D2 (PGD2; HY-101988). 17-Phenyl-18,19,20-trinor-PGD2 is a potent inhibitor of platelet aggregation caused by aenosine diphosphate (ADP), with the IC50 of 8.4 μM (PGD2 IC50 = 18.6 nM). 17-Phenyl-18,19,20-trinor-PGD2 is a weak agonist of cyclic AMP accumulation .
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-
- HY-106394
-
|
|
P-glycoprotein
|
Cardiovascular Disease
|
|
TP-9201 is a platelet glycoprotein (GP) IIb/IIIa receptor antagonist. TP-9201 inhibits the interaction between GPIIb/IIIa and fibrinogen, thereby suppressing platelet aggregation. TP-9201 exhibits similar inhibitory activity on adenosine diphosphate (ADP) (HY-W010918)-induced platelet aggregation in humans, baboons, and dogs (IC50 = 1-3 μM), while showing lower activity in rabbits (IC50 = 45 μM) and rats (IC50 = 20 μM). TP-9201can be used in studies related to the prevention of rethrombosis after arterial thrombolysis .
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-
- HY-122026
-
|
PF-367
|
GSK-3
|
Neurological Disease
|
|
PF-04802367 (PF-367) is a highly selective GSK-3 inhibitor with an IC50 of 2.1 nM based on a recombinant human GSK-3β enzyme assay and 1.1 nM based on ADP-Glo assay. PF-04802367 shows desirable central nervous system (CNS) properties and potency. PF-04802367 is equally effective at inhibition of the two known GSK-3 isoforms (GSK-3α and GSK-3β) with IC50 values of 10.0 and 9.0 nM in mobility shift assays, respectively .
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- HY-N6801
-
|
|
Caspase
Apoptosis
Bcl-2 Family
|
Infection
Inflammation/Immunology
Cancer
|
|
Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia .
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-
- HY-176060
-
|
|
Histamine Receptor
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
Cancer
|
|
Platelet aggregation-IN-3 (Compound 5) is a ligand for H2 histamine receptors, α2(A,C)-adrenergic receptors (α2-AR), and 5-HT2(B,C) serotonin receptors. Platelet aggregation-IN-3 can inhibit platelet aggregation induced by ADP and collagen and can also modulate tumour cell-induced platelet aggregation (TCIPA). Platelet aggregation-IN-3 is promising for research of antiplatelet therapy in cardiovascular diseases and the prevention of cancer-related thrombosis and tumour metastasis .
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-
- HY-181004
-
|
|
CDK
|
Cancer
|
|
PKMYT1-IN-13 is a potent, orally active and selective PKMYT1 inhibitor that inhibits PKMYT1 with IC50 values < 10.0 nM in ADP-Glo assay and 19.9 nM in NanoBRET cellular assay. PKMYT1-IN-13 exhibits high selectivity over WEE1. PKMYT1-IN-13 shows selective antiproliferative activity in CCNE1-amplified cells, while showing minimal wild-type effects. PKMYT1-IN-13 shows antitumor efficacy in HCC1569 mouse xenografts. PKMYT1-IN-13 can be used for the research of CCNE1-amplified cancers, such as gastric, ovarian, and breast cancer .
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-
- HY-149454
-
|
|
P2Y Receptor
|
Cancer
|
|
P2Y1/P2Y12 antagonist-1 (compound 24w) is an orally available dual inhibitor of P2Y1 and P2Y12 with antiplatelet activity. P2Y1/P2Y12 antagonist-1 inhibits ADP-induced platelet aggregation in rabbit plasma with an IC50 of 4.23 μM. P2Y1/P2Y12 antagonist-1 exhibits potent inhibitory effects in rat thrombosis model.
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-
- HY-N6801S
-
|
|
Isotope-Labeled Compounds
Caspase
Apoptosis
Bcl-2 Family
|
Infection
Inflammation/Immunology
Cancer
|
|
Nivalenol- 13C15 is the 13C labeled Nivalenol (HY-N6801) . Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia.
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-
- HY-175290
-
|
|
Arf Family GTPase
|
Cancer
|
|
Arf1-GEFs-IN-1 is a potent and orally active ADP-ribosylation factor 1- guanine nucleotide exchange factors (Arf1-GEFs) inhibitor with an IC50 value of 40.85 μM against CT26 cells. Arf1-GEFs-IN-1 primarily mediates tumor regression by triggering anti-tumor immune responses, rather than through direct cytotoxicity. Arf1-GEFs-IN-1 effectively promotes CCL5 expression, demonstrates excellent in vivo efficacy. Arf1-GEFs-IN-1 can be used for the study of colon cancer .
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-
- HY-B0764A
-
|
Dibutyryl cAMP hemicalcium; DBcAMP hemicalcium
|
PKA
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
Cancer
|
|
Bucladesine (Dibutyryl cAMP; DBcAMP) hemicalcium is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation .
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-
- HY-B0764
-
|
Dibutyryl cAMP sodium; DBcAMP sodium
|
PKA
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Bucladesine (Dibutyryl cAMP; DBcAMP) sodium is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation .
|
-
- HY-B0764B
-
|
Dibutyryl cAMP; DBcAMP
|
PKA
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Bucladesine (Dibutyryl cAMP; DBcAMP) is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation .
|
-
- HY-N6801R
-
|
|
Reference Standards
Caspase
Apoptosis
Bcl-2 Family
|
Infection
Inflammation/Immunology
Cancer
|
|
Nivalenol (Standard) is the analytical standard of Nivalenol (HY-N6801). This product is intended for research and analytical applications. Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia.
|
-
- HY-B0764R
-
|
Dibutyryl cAMP sodium (Standard); DBcAMP sodium (Standard)
|
Reference Standards
PKA
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Bucladesine (Dibutyryl cAMP; DBcAMP) sodium (Standard) is the analytical standard of Bucladesine sodiumn (HY-B0764). This product is intended for research and analytical applications. Bucladesine is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation .
|
-
- HY-P11467
-
|
|
Bacterial
p38 MAPK
NF-κB
PERK
JNK
|
Cardiovascular Disease
Infection
|
|
Gy-CATH is an anionic antimicrobial peptide. Gy-CATH activates MAPK and NF-κB signaling pathways (elevated levels of phospho-ERK, -p38, -JNK, -p65, and -IκBα). Gy-CATH upregulates the expression levels of three physiological anticoagulant pathways. Gy-CATH inhibits ADP-, Collagen-, and PMA-induced platelet aggregation. Gy-CATH has no direct antimicrobial activity, but shows significant preventive abilities against mice infected with Staphylococcus aureus, Escherichia coli, and Methicillin (HY-121544)-resistant Staphylococcus aureus. Gy-CATH exhibits potent immunomodulatory activity, enhancing macrophage-and neutrophil-mediated bactericidal functions. Gy-CATH significantly reduces the extent of pulmonary fibrin deposition and prevents thrombosis in mice .
|
-
- HY-B0764G
-
|
Dibutyryl cAMP sodium; DBcAMP sodium
|
PKA
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Bucladesine (Dibutyryl cAMP; DBcAMP) sodium (GMP) is a Bucladesine sodium (HY-B0764) produced by using GMP guidelines. Bucladesine (Dibutyryl cAMP; DBcAMP) is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation .
|
-
- HY-125209A
-
|
|
Apoptosis
PARP
DNA/RNA Synthesis
|
Cancer
|
|
TH5427 hydrochloride is a NUDT5 inhibitor with a human target IC50 of 29 nM, ~690-fold selectivity over MTH1 in vitro, and selective functional inhibition over other NUDIX hydrolases including NUDT9 .TH5427 hydrochloride binds to the active site of NUDT5, blocking enzymatic activity related to ADP-ribose metabolism and PAR-derived ATP synthesis .TH5427 hydrochloride blocks progestin-dependent nuclear ATP synthesis, impairs progestin-induced chromatin remodeling, inhibits histone H1 displacement, disrupts progestin-dependent gene regulation, and abrogates progestin-dependent proliferation in breast cancer cells .TH5427 hydrochloride functions as a versatile probe to study nuclear ATP dynamics and ADP-ribose-related metabolism in cells .TH5427 hydrochloride engages NUDT5 at physiological temperatures, as demonstrated by Drug Affinity Responsive Target Stability (DARTS) assay .TH5427 hydrochloride stabilizes NUDT5 against thermal denaturation in cell lysates and intact cells, as shown by cellular thermal shift assay (CETSA) .TH5427 hydrochloride functionally inhibits NUDT5 activity, leading to downstream effects on oxidative DNA damage and DNA replication in triple-negative breast cancer (TNBC) cells .TH5427 hydrochloride suppresses proliferation of TNBC cells without inducing cell death or apoptosis, slows DNA replication in TNBC cells, promotes accumulation of oxidative DNA lesions, and triggers DNA damage response in TNBC cells .TH5427 hydrochloride suppresses growth of TNBC cells in vitro, inhibits growth of TNBC xenograft tumors in nude mice in vivo, and shows greater potency against TNBC cell lines compared to ER-positive and normal-like breast cell lines .TH5427 hydrochloride can be used for the research of breast cancer and triple-negative breast cancer .
|
-
- HY-W010918R
-
|
Adenosine diphosphate (Standard); Adp (Standard)
|
Reference Standards
Endogenous Metabolite
|
Others
|
|
Adenosine 5'-diphosphate (Standard) is the analytical standard of Adenosine 5'-diphosphate. This product is intended for research and analytical applications. Adenosine 5'-diphosphate (Adenosine diphosphate) is a nucleoside diphosphate. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. Adenosine 5'-diphosphate induces human platelet aggregation and inhibits stimulated adenylate cyclase by an action at P2T-purinoceptors.
In Vitro: Adenosine 5'-diphosphate consists of the pyrophosphate group, the pentose sugar ribose, and the nucleobase adenine. Adenosine 5'-diphosphate is the product of ATP dephosphorylation by ATPases. ADP is converted back to ATP by ATP synthases. ATP is an important energy transfer molecule in cells. Adenosine 5'-diphosphate is utilized in a wide number of cellular processes, including respiration, biosynthetic reactions, motility, and cell division.
|
-
- HY-175675
-
|
|
P2Y Receptor
Keap1-Nrf2
|
Cardiovascular Disease
Neurological Disease
|
|
P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration.
P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca 2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction .
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-
- HY-137325A
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
2-Chloro-ATP sodium (2-Chloro ATP) is an adenine nucleotide and an analog of ATP. It is an antagonist of the purinergic P2Y1 receptor and inhibits intracellular calcium mobilization induced by ADP (HY-W010918) in Jurkat cells expressing the human receptor (Ki=2.3 μM). 2-Chloro-ATP sodium is an agonist of the purinergic P2X receptor and induces inward currents in HEK293 cells expressing human bladder smooth muscle or rat PC12 forms of the receptor (EC50=0.5 and 2.5 μM). 2-Chloro-ATP sodium induces relaxation of precontracted guinea pig cecal strips in a concentration-dependent manner. 2-Chloro-ATP sodium has been used to study the substrate specificity of cyclic nucleotide-dependent protein kinases such as protein kinase A (PKA) and PKG.
|
-
- HY-183765
-
|
|
PARP
Pyruvate Kinase
|
Cancer
|
|
PARP1/PKM2-IN-1 is a dual PARP1/PKM2 inhibitor, with an IC50 of 39.5 nM against PARP1, and IC50 values of 261 nM (recombinant PKM2) and 50 nM (dimeric PKM2) against PKM2. PARP1/PKM2-IN-1 reduces the dimerization of PKM2 and decreases its nuclear accumulation level. PARP1/PKM2-IN-1 also selectively downregulates PKM2 mRNA and impairs poly (ADP-ribose)-mediated nuclear retention of PKM2. PARP1/PKM2-IN-1 exhibits antiproliferative activity and inhibits the formation of 3D cancer spheroids. PARP1/PKM2-IN-1 can be used in research related to mammary adenocarcinoma, triple-negative breast cancer, BRCA1-mutant triple-negative breast cancer, and prostate adenocarcinoma .
|
-
- HY-116028
-
|
15-Deoxy-Δ12,14-PGD2
|
Endogenous Metabolite
Prostaglandin Receptor
PPAR
Src
|
Cardiovascular Disease
|
|
15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2), a metabolite of PGD2 (HY-101988), is an agonist of prostaglandin receptor 2 (DP2). 15-deoxy-Δ12,14-Prostaglandin D2 binds to DP2 (Ki=50 nM) and induces eosinophil activation (EC50=8 nM). 15-deoxy-Δ12,14-Prostaglandin D2 also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), inducing PPARγ-mediated transcription. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is cytotoxic to L1210 murine leukemia cells (IC50=0.3 μg/ml) and inhibits ADP-induced platelet aggregation (IC50=320 ng/mL).
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-
| Cat. No. |
Product Name |
Type |
-
- HY-146248
-
|
|
Fluorescent Dyes
|
|
TFMU-ADPr is a selective reporter substrate of SARS-CoV-2 Macro1 (IC50=0.59 μM), with an excitation wavelength (λEx) of 385 nm, and an emission wavelength (λEm) of 502 nm (or 495 nm). TFMU-ADPr can also undergo enzymatic hydrolysis with Poly(ADP-ribose) Glycohydrolase (PARG) sourced from human, Tetrahymena thermophila and ADP-ribosylhydrolase 3 from human to release fluorophores, thereby directly reporting total poly (ADP-ribose) hydrolase activity. TFMU-ADPr binds to the ADPr-binding site of SARS-CoV-2 Macro1, and its TFMU moiety inserts into the narrow hydrophobic groove of this protein. TFMU-ADPr can thus be used to evaluate small-molecule inhibitors targeting PAR hydrolases under in vitro conditions, to investigate the regulatory mechanisms of ADP-ribosyl catabolic enzymes, or to detect PAR hydrolase activity in whole-cell lysate assays. TFMU-ADPr is also applicable to COVID-19-related research .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W250153
-
|
|
Biochemical Assay Reagents
|
|
Adenosine 3'-phosphate 5'-phosphosulfate lithium, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
|
-
- HY-W250153A
-
|
|
Biochemical Assay Reagents
|
|
Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
|
-
- HY-N10272
-
|
|
Biochemical Assay Reagents
|
|
Avenaciolide is an antifungal bis-γ-lactone found in Aspergillus avenaceus. Avenaciolide has also antibacterial action. Avenaciolide is a specific inhibitor of glutamate transport in rat liver mitochondria. Avenaciolide interferes with the ability of ADP to stimulate the rate of glutamate oxidation .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-141867
-
|
Z-Phe-Phe-FMK
|
Cathepsin
MEK
Caspase
DNA/RNA Synthesis
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Z-FF-FMK (Z-Phe-Phe-FMK) is a cell-permeable, irreversible, and cysteine protease inhibitor targeting cathepsin-L. Z-FF-FMK inhibits angiotensin II-induced MEK activation in vascular walls, aortic medial remodeling, blood pressure elevation, and upregulation of cystatin C in aortic walls. Z-FF-FMK prevents β-amyloid-mediated caspase-3 activation, poly (ADP-ribose) polymerase cleavage, DNA fragmentation, and apoptosis of cortical neurons (apoptosis). Z-FF-FMK can be used in research related to hypertension and Alzheimer's disease .
|
-
- HY-P1702
-
|
|
Integrin
|
Others
|
|
GR83895 is a RGD based peptide, and inhibits ADP-induced platelet aggregation of human gel-filtered platelets (IC50= 0.9 μM) .
|
-
- HY-P11467
-
|
|
Bacterial
p38 MAPK
NF-κB
PERK
JNK
|
Cardiovascular Disease
Infection
|
|
Gy-CATH is an anionic antimicrobial peptide. Gy-CATH activates MAPK and NF-κB signaling pathways (elevated levels of phospho-ERK, -p38, -JNK, -p65, and -IκBα). Gy-CATH upregulates the expression levels of three physiological anticoagulant pathways. Gy-CATH inhibits ADP-, Collagen-, and PMA-induced platelet aggregation. Gy-CATH has no direct antimicrobial activity, but shows significant preventive abilities against mice infected with Staphylococcus aureus, Escherichia coli, and Methicillin (HY-121544)-resistant Staphylococcus aureus. Gy-CATH exhibits potent immunomodulatory activity, enhancing macrophage-and neutrophil-mediated bactericidal functions. Gy-CATH significantly reduces the extent of pulmonary fibrin deposition and prevents thrombosis in mice .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P992446
-
|
|
NTPDase
|
Cancer
|
|
PUR001 is a monoclonal antibody targeting NTPDase 1 (CD39). PUR001 blocks the hydrolysis of extracellular ATP and ADP into AMP by inhibiting CD39, reduces the production of immunosuppressive adenosine, and increases extracellular ATP concentration to activate anti-tumor immune responses. PUR001 can be used in studies related to solid tumors .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-111557
-
-
-
- HY-16929
-
-
-
- HY-N1462
-
-
-
- HY-113432
-
-
-
- HY-N2522
-
-
-
- HY-N1502
-
-
-
- HY-N7765
-
-
-
- HY-N0466
-
-
-
- HY-113371
-
-
-
- HY-Z0283
-
-
-
- HY-134216
-
-
-
- HY-N1910
-
-
-
- HY-N6801
-
|
|
Infection
Structural Classification
Microorganisms
Classification of Application Fields
Terpenoids
Sesquiterpenes
Inflammation/Immunology
Disease Research Fields
Source Classification
|
Caspase
Apoptosis
Bcl-2 Family
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Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia .
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- HY-W051513
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- HY-N5021
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- HY-W010918R
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- HY-113432R
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- HY-113371A
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- HY-N7614
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-
- HY-N1717
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- HY-134556
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- HY-N0466R
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Structural Classification
Trifolium hybridum L.
Terpenoids
Diterpenoids
Plants
Compositae
Endogenous metabolite
Source Classification
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Reference Standards
Glycosidase
HMG-CoA Reductase (HMGCR)
Fatty Acid Synthase (FASN)
LDLR
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Rebaudioside A (Standard) is the analytical standard of Rebaudioside A. This product is intended for research and analytical applications. Rebaudioside A is an orally effective steviol glycoside with high sweetness. Rebaudioside A acts as an inhibitor of α-glucosidase with an IC50 value of 35.01 μg/mL. Rebaudioside A increases the ATP/ADP ratio in β cells in a glucose-dependent manner, thereby inhibiting KATP channels, leading to membrane depolarization, calcium influx, and ultimately stimulating insulin secretion. Rebaudioside A activates the SREBP signaling pathway by inhibiting HMGCR, the rate-limiting enzyme in cholesterol synthesis, resulting in increased expression of LDLR on the cell surface, thus promoting the uptake of LDL-C in the blood. Rebaudioside A can be used for studies on blood glucose and lipid regulation as well as anti-obesity.
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- HY-N6801R
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Structural Classification
Microorganisms
Terpenoids
Sesquiterpenes
Source Classification
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Reference Standards
Caspase
Apoptosis
Bcl-2 Family
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Nivalenol (Standard) is the analytical standard of Nivalenol (HY-N6801). This product is intended for research and analytical applications. Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia.
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- HY-N13135
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- HY-N13134
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- HY-120311
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- HY-N2522R
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Gummiferin dipotassium (Standard)
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other families
Terpenoids
Diterpenoids
Plants
Source Classification
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Reference Standards
Mitochondrial Metabolism
Calcium Channel
Reactive Oxygen Species (ROS)
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Carboxyatractyloside (dipotassium) (Standard) is the analytical standard of Carboxyatractyloside dipotassium (HY-N2522). This product is intended for research and analytical applications. Carboxyatractyloside dipotassium is a diterpenoid. Carboxyatractyloside dipotassium can be isolated from plants of the genus Xanthium. Carboxyatractyloside dipotassium is an ADP/ATP carrier inhibitor, inhibiting mitochondrial ADP/ATP transport. Carboxyatractyloside dipotassium promotes ROS production, induces Ca 2+ release, and leads to mitochondrial dysfunction. Carboxyatractyloside dipotassium induces lethargy, weakness, and epileptic seizures in rats .
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- HY-126643
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- HY-N10272
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- HY-B0887BR
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(-)-trans-NRDC-143 (Standard); (1S)-trans-Permethrin (Standard)
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Microorganisms
Source Classification
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Insecticide
Reference Standards
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Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for research and analytical applications. Atractyloside potassium salt is a toxic diterpenoid glycoside that can be isolated from the fruits of Xanthium sibiricum. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart .
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- HY-N14932
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- HY-N14933
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- HY-N14934
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- HY-167686
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Homopisatin
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Structural Classification
Natural Products
Plants
Dalbergia variabilis
Fabaceae
Source Classification
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Integrin
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Variabilin (Homopisatin) is a potent RGD-containing antagonist of glycoprotein IIb-IIIa and platelet aggregation inhibitor from the hard tick Dermacentor variabilis. Variabilin potently inhibits platelet aggregation induced by the platelet agonists ADP, collagen, and thrombin receptor peptide SFLLRNP. Variabilin also blocks platelet adhesion to immobilized Fg. In addition, Variabilin inhibits binding of purified human GPIIb-IIIa to immobilized Fg .
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- HY-112175R
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- HY-124371
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Flavonoids
Viburnaceae
Plants
Biflavones
Viburnum lantana L.
Source Classification
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Phosphodiesterase (PDE)
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Amentoflavone hexaacetate is a 3,5-cyclic nucleotide phosphodiesterase inhibitor with antiplatelet aggregation activity. Amentoflavone hexaacetate can inhibit the aggregation of eluted human platelets induced by ADP or collagen. Amentoflavone hexaacetate can also inhibit the cAMP phosphodiesterase activity in human platelets. Amentoflavone hexaacetate can significantly increase the cAMP level of platelets in the presence of prostaglandin E1. Amentoflavone hexaacetate has anti-angiogenic and anti-metastatic effects .
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- HY-W051513R
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- HY-N1462R
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Structural Classification
Terpenoids
Pterocarpus soyauxii Taub.
Diterpenoids
Plants
Compositae
Source Classification
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Reference Standards
Chloride Channel
Autophagy
mTOR
AMPK
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Atractyloside (potassium salt) (Standard) is the analytical standard of Atractyloside (potassium salt). This product is intended for use in research and analytical applications. Atractyloside potassium salt is a powerful and specific inhibitor of mitochondrial ADP/ATP transport. Atractyloside potassium salt inhibits chloride channels from mitochondrial membranes of rat heart. Atractyloside potassium salt activates autophagy, inhibits ANT2, mTOR and promotes the activation of p-AMPK. Atractyloside potassium salt has anti-cancer effects on non-small cell lung cancer and can inhibit liver steatosis. Atractylodesin potassium salt has nephrotoxicity .
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- HY-Z0283R
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- HY-N6969A
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Alkaloids
Other Alkaloids
Stephania epigaea Lo
Plants
Menispermaceae
Source Classification
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Adrenergic Receptor
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Dicentrine hydrochloride is a drug with anti-inflammatory and anti-cancer activity. Dicentrine hydrochloride exerts its effects by enhancing TNF-α-induced apoptosis in A549 lung adenocarcinoma cells. Dicentrine hydrochloride increases caspase-8, -9, -3 and poly(ADP-ribose) polymerase (PARP) activities. Dicentrine hydrochloride inhibits TNF-α-induced invasion and migration of A549 cells. Dicentrine hydrochloride significantly inhibited the TNF-α-activated TAK1, p38, JNK and Akt signaling pathways, and reduced the transcriptional activities of NF-κB and AP-1 .
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- HY-N17403
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- HY-N19129
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- HY-N17823
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- HY-N17826
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-113432S
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Nudifloramide-d3 (2PY-d3) is the deuterium labeled Nudifloramide. Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
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- HY-Z0283S
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Benzamide- 15N is a 15N-labeled Benzamide. Benzamide inhibits poly(ADP-ribose) polymerase (PARP) .
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- HY-15284S2
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Prasugrel-d4 is the deuterium labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
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- HY-113371S
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2-Methylcitric acid-d3 is the deuterium labeled 2-Methylcitric acid. 2-Methylcitric acid (Methylcitric acid) is an endogenous metabolite in the 2-methylcitric acid cycle. 2-Methylcitric acid accumulates in methylmalonic and propionic acidemias and acts as a marker metabolite. 2-Methylcitric acid markedly inhibits ADP-stimulated and uncoupled respiration in mitochondria supported by glutamate .
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- HY-N6801S
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Nivalenol- 13C15 is the 13C labeled Nivalenol (HY-N6801) . Nivalenol, a trichothecene mycotoxin that can be produced by Fusarium graminearum, is a fungal metabolite present in agricultural product. Nivalenol modulates apoptotic pathway, cell cycle regulation, Bax, ERK, caspase-3, and poly-ADP-ribose synthase activity in macrophages. Nivalenol inhibits ribosomal peptidyltransferase site, protein synthesis, DNA synthesis, and cell proliferation. Nivalenol induces late-stage apoptotic morphological changes, reduces cellular metabolism, and decreases cell proliferation in erythroleukemia cells. Nivalenol induces lymphocyte apoptosis in murine thymus, spleen, and Peyer's patches. Nivalenol can be used for the research of erythroleukemia.
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- HY-W711852
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Benzamide-d5 (Benzenecarboxamide-d5) is deuterium labeled Benzamide. Benzamide (Benzenecarboxamide) is a potent poly(ADP-ribose) polymerase (PARP) inhibitor. Benzamide has protective activity against both glutamate- and methamphetamine (METH)-induced neurotoxicity in vitro. Benzamide can attenuate the METH-induced dopamine depletions and exhibits neuroprotective activity in mice, also has no acute effect on striatal dopamine metabolism and does not reduce body temperature .
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- HY-W766548
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Floxuridine- 13C, 15N2 (5-Fluorouracil 2'-deoxyriboside- 13C, 15N2) is the 13C- and 15N-labeled labeled Floxuridine (HY-B0097). Floxuridine (5-Fluorouracil 2'-deoxyriboside) is a pyrimidine analog and known as an oncology antimetabolite. Floxuridine inhibits Poly(ADP-Ribose) polymerase and induces DNA damage by activating the ATM and ATR checkpoint signaling pathways in vitro. Floxuridine is a extreamly potent inhibitor for S. aureus infection and induces cell apoptosis . Floxuridine has antiviral effects against HSV and CMV .
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- HY-107867S1
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(Rac)-Clopidogrel hydrogen-d9 sulfate is the deuterium labeled (±)-Clopidogrel (bisulfate) (HY-107867). (±)-Clopidogrel bisulfate is a platelet P2Y12 receptor inhibitor and an adenosine diphosphate (ADP) receptor antagonist. (±)-Clopidogrel bisulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel bisulfate reduces vascular inflammation and angiotensin II induced-abdominal aortic aneurysm progression. (±)-Clopidogrel bisulfate has anti-inflammatory effects .
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- HY-107867S2
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Clopidogrel- 13C,d3 sulfate is the deuterium and 13C-labeled (±)-Clopidogrel (bisulfate) (HY-107867). (±)-Clopidogrel bisulfate is a platelet P2Y12 receptor inhibitor and an adenosine diphosphate (ADP) receptor antagonist. (±)-Clopidogrel bisulfate inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel bisulfate reduces vascular inflammation and angiotensin II induced-abdominal aortic aneurysm progression. (±)-Clopidogrel bisulfate has anti-inflammatory effects .
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-
- HY-15284S1
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Prasugrel-d3 is the deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
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-
-
- HY-15284S
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Prasugrel-d5 is deuterium labeled Prasugrel. Prasugrel (PCR 4099), a thienopyridine and prodrug, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
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- HY-15284S3
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Prasugrel-13C6 is a deuterated labeled Prasugrel . Prasugrel (PCR 4099), a thienopyridine and proagent, inhibits platelet function. Prasugrel is an orally active and potent P2Y12 receptor antagonist, and inhibits ADP-induced platelet aggregation .
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- HY-167927S
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Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
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- HY-113096S
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Prostaglandin D1-d4 (PGD1-d4) is deuterium labeled Prostaglandin D1. Prostaglandin D1 is a prostanoid which causes contractile and relaxant on isolated human pial arteries, it is also an inhibitor of ADP-induced platelet aggregation with an IC50 value of 320 ng/ml. Prostaglandin D1 can be used for metabolic research .
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- HY-17459S
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Clopidogrel-d3 (hydrogen sulfate) is the deuterium labeled Clopidogrel hydrogen sulfate . Clopidogrel hydrogen sulfate is an antiplatelet agent to prevent blood clots. Clopidogrel hydrogen sulfate inhibits CYP2B6 and CYP2C19 with IC50s of 18.2 nM and 524 nM, respectively. Clopidogrel hydrogen sulfate is a potent antithrombotic agent that inhibits ADP-induced platelet aggregation．Clopidogrel hydrogen sulfate also is an orally active P2Y(12) inhibitor .
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- HY-113113S
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13,14-Dihydro PGE1-d4 (13,14-Dihydroprostaglandin E1-d4) is deuterium labeled 13,14-Dihydro PGE1. 13,14-Dihydro PGE1 is a metabolite of PGE1 (Prostaglandin E1) which inhibits the ADP-induced platelet aggregation (ID50 = 10.8 ng/mL platelet rich plasma) .
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- HY-15283AS1
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(±)-Clopidogrel-d4 ((±)-Clopidogrelum-d4) is the deuterium labeled (±)-Clopidogrel (HY-107867). (±)-Clopidogrel is a platelet P2Y12 receptor inhibitor and an adenosine diphosphate (ADP) receptor antagonist. (±)-Clopidogrel inhibits the binding of ADP to its receptors on the membranes of platelet cells, and blocks ADP-mediated activation of the glycoprotein GPIIb/IIIa complex. (±)-Clopidogrel reduces vascular inflammation and angiotensin II induced-abdominal aortic aneurysm progression. (±)-Clopidogrel has anti-inflammatory effects .
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- HY-113432S2
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Nudifloramide- 13C,d3 (2PY- 13C,d3) is the 13C- and deuterium labeled Nudifloramide (HY-113432). Nudifloramide (2PY) is one of the end products of nicotinamide-adenine dinucleotide (NAD) degradation. Nudifloramide significantly inhibits poly(ADP-ribose) polymerase (PARP-1) activity in vitro .
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| Cat. No. |
Product Name |
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Classification |
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- HY-134318B
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Azide
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8-Azido-ADP (disodium) is a covalent-binding inhibitor of mitochondrial adenine nucleotide translocation. 8-Azido-ADP (disodium) causes irreversible inhibition of adenine nucleotide exchange in a light-dependent reaction. 8-Azido-ADP (disodium) inhibits the normal state 4 → 3 transitions of mitochondrial respiration induced by ADP . 8-Azido-ADP (disodium) is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-W250153
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Nucleotide Analogs
Adenine Nucleotide
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Adenosine 3'-phosphate 5'-phosphosulfate lithium, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
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-
- HY-164090
-
|
|
|
Nucleotide Analogs
Adenine Nucleotide
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|
Adenosine 3'-phosphate 5'-phosphosulfate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
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-
- HY-W141392
-
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Phosphoramidites
Hypoxanthine
|
|
2'-Fluoro-5'-O-DMT-2'-deoxyinosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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-
- HY-152696
-
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|
|
Nucleoside Analogs
Inosine
|
|
6-O-Methylinosine is a hypoxanthine analogue. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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-
- HY-177631A
-
|
DT01 sodium; coDbait sodium
|
|
Antisense Oligonucleotides
|
|
Etidaligide sodium, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation
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-
- HY-W250153A
-
|
|
|
Nucleotide Analogs
Adenine Nucleotide
|
|
Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate, an adenine nucleotide derivative, is a selective P2Y1 antagonist with no effect on P2Y2, P2Y4, or P2Y6 receptors. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can competitive inhibit ADP-induced platelet aggregation, as well as the ability of ADP to cause shape change and increases in Ca 2+ in platelets, but had no effect on the inhibition of stimulated adenylate cyclase by ADP. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate is a co-substrate used for the sulfonation of glycans. Adenosine 3'-phosphate 5'-phosphosulfate lithium hydrate can be used for Golgi-resident PAP-specific 3'-phosphatase-coupled sulfotransferase assays, which as donor substrate to transfer a sulfonate group .
|
-
- HY-177631
-
|
DT01; coDbait
|
|
Antisense Oligonucleotides
|
|
Etidaligide, an AsiDNA, a first-in-class DNA repair inhibitor designed to prevent the repair of DNA damage in tumour cells. It also activates DNA-dependent protein kinase (DNA-PK) and poly (ADP-ribose) polymerase enzymes that induce phosphorylation of H2A
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-
- HY-W392836
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|
Phosphoramidites
Hypoxanthine
|
|
2'-O-Methyl-5'-O-dmt-inosine-3'-CE-phosphoramidite is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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-
- HY-154017
-
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|
|
Nucleoside Analogs
Inosine
|
|
2′-C-Methyl-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-154393
-
|
|
|
Nucleoside Analogs
Inosine
|
|
2-Chloro-2'-deoxy-6-O-methylinosine is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
|
-
- HY-152678
-
|
|
|
Nucleoside Analogs
|
|
6-Methoxypurine-9-β-D-5’(R)-C-methylriboside is a hypoxanthine analog. Hypoxanthine is a kind of purine base mainly present in muscle tissue. And it is a metabolite produced by purine oxidase acting on xanthine. Hypoxanthine has typical anti-inflammatory effects and is a potential endogenous poly(ADP-ribose) polymerase (PARP) inhibitor. It is cytoprotective by inhibiting PAPR activity, inhibiting peroxynitrite-induced mitochondrial depolarization and secondary superoxide production. Hypoxanthine can also be used as an indicator of hypoxia .
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| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-B0764G
-
|
Dibutyryl cAMP sodium; DBcAMP sodium
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PKA
Reactive Oxygen Species (ROS)
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Bucladesine (Dibutyryl cAMP; DBcAMP) sodium (GMP) is a Bucladesine sodium (HY-B0764) produced by using GMP guidelines. Bucladesine (Dibutyryl cAMP; DBcAMP) is a membrane-permeable 3′, 5′-cyclic adenosine monophosphate (cAMP) analog. Bucladesine selectively activates cAMP dependent protein kinase (PKA) by increasing the intracellular level of cAMP. Bucladesine significantly attenuates MDMA-induced increases in hippocampal mitochondrial ROS formation, mitochondrial outer membrane damage, cytochrome c release, and hippocampal ADP/ATP ratio, thereby improving spatial learning and memory impairments. Bucladesine exhibit anti-nociceptive and anti-inflammation effect. Bucladesine can inhibit cancer cells proliferation, induce apoptosis. Bucladesine can be used for the researches of neurological disease, cancer, inflammation .
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