Search Result
Results for "
non-competitive
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
19
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-103547
-
|
GCGR
|
Metabolic Disease
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L-168049 is a potent, selective, orally active and non-competitive glucagon receptor antagonist with IC50s of 3.7 nM, 63 nM, and 60 nM for human, murine, and canine glucagon receptors, respectively .
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-
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- HY-102094
-
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mGluR
|
Neurological Disease
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(E/Z)-SIB-1893 is a racemic compound of (E)-SIB-1893 and (Z)-SIB-1893 isomers. (E)-SIB-1893 is a selective non-competitive metabotropic glutamate subtype 5 receptor (mGluR5) antagonist .
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-
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- HY-149404
-
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Reactive Oxygen Species
Tyrosinase
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Others
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Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) is a potent, non-competitive tyrosinase inhibitor with an IC50 value of 49.33 ± 2.64 µM and Ki value of 31.25 ± 0.25 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) have the highest radical scavenging activity to reduce the production of reactive oxygen species (ROS) with an IC50 value of 25.39 ± 0.77 µM. Non-competitive tyrosinase inhibitor (Tyrosinase-IN-12) can be used for anti-browning substances in the food and agricultural sectors .
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-
-
- HY-B1413
-
-
-
- HY-14166
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L 663536
|
FLAP
Leukotriene Receptor
PPAR
Apoptosis
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Cancer
|
MK-886 (L 663536) is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 is also a non-competitive PPARα antagonist and can induce apoptosis .
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-
-
- HY-138165
-
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Others
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Others
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Ac-Phe-NH2 is a non-competitive inhibitor of polyubiquitin chain elongation at Ki value of 8 mM by destabilizing the active trimer .
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-
-
- HY-168108
-
|
Fungal
|
Infection
|
Antifungal agent 115 (compound 8n) is a non-competitive chitin synthase (CHS) inhibitor with an IC50 of 93 μM. Antifungal agent 115 demonstrates good selectivity and broad-spectrum antifungal activity, exhibiting significant efficacy against drug-resistant fungi. Antifungal agent 115 can be utilized in fungi infection research .
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-
-
- HY-122646
-
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Deubiquitinase
MDM-2/p53
|
Cancer
|
USP7-IN-2 (compound 4) is a non-competitive USP7 inhibitor with an IC50 of 6 nM. USP7-IN-2 causes degradation of MDM2, stabilization of p53 and induction of p21 in multiple cell lines, and can be utilized in cancer research .
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-
-
- HY-156029
-
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Others
|
Cancer
|
IA1-8H2 is a non-covalent, non-competitive inhibitor of PHPT1 (IC50: 3.4 μM). IA1-8H2 can be used for research of lung cancer, hepatocarcinoma, and renal cancer .
|
-
-
- HY-14166A
-
L 663536 sodium salt
|
PPAR
Apoptosis
Leukotriene Receptor
FLAP
|
Cancer
|
MK-886 (L 663536) sodium salt is a potent, cell-permeable and orally active FLAP (IC50 of 30 nM) and leukotriene biosynthesis (IC50s of 3 nM and 1.1 μM in intact leukocytes and human whole blood, respectively) inhibitor. MK-886 sodium salt is also a non-competitive PPARα antagonist and can induce apoptosis .
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-
-
- HY-115939
-
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Bacterial
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Infection
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Urease-IN-2 (compound 8g) is a non-competitive urease inhibitor with an IC50 of 0.94 μM and a Ki of 1.6 μM. Urease-IN-2 inhibits the Jack bean urease (JBU) in a non-competitive manner .
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-
-
- HY-110097
-
CNS 1102
|
iGluR
|
Neurological Disease
|
Aptiganel hydrochloride (Cerestat) is a non-competitive NMDA receptor antagonist with neuroprotective effect.
|
-
-
- HY-W010510
-
-
-
- HY-12371
-
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mGluR
|
Neurological Disease
|
VU0431316 is a potent and selective non-competitive antagonist of mGlu5 with an IC50 value of 24 nM .
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-
-
- HY-100979
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HDMPPA
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mAChR
|
Others
|
W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
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-
-
- HY-Y0504
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Hegzadesil; Trimethylamine hydrochloric acid; Trimethylamine monohydrochloride
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Metabolic Disease
|
Trimethylammonium chlorideIt is an endogenous metabolite that inhibits deacetylation. Trimethylammonium chlorideIs a non-competitive inhibitor of acetylcholinesterase .
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-
-
- HY-149888
-
-
-
- HY-N12427
-
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Tyrosinase
|
Cancer
|
Litchinol B (compound 2) is a non-competitive tyrosinase inhibitor with an inhibition constant of 5.70 μM .
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-
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- HY-50672
-
|
Kinesin
Apoptosis
Lipoxygenase
|
Cancer
|
MK-0731 is a selective, non-competitive and allosteric kinesin spindle protein (KSP) inhibitor with an IC50 of 2.2 nM and a pKa of 7.6. MK-0731 is >20,000 fold selectivity against other kinesins. MK-0731 induces mitotic arrest and induces apoptosis in tumors. MK-0731 provides significant antitumor efficacy .
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-
-
- HY-163974
-
-
-
- HY-15084
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(+)-MK 801 Maleate
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iGluR
|
Neurological Disease
|
Dizocilpine maleate (MK-801 maleate) is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
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-
-
- HY-117672
-
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Phosphatase
|
Others
|
L-671776 can be isolated from a fungal strain (ATCC 20928B), is a non-competitive inhibitor of IMPase .
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-
-
- HY-12042A
-
AS703026 hydrochloride; MSC1936369B hydrochloride
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MEK
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Cancer
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Pimasertib hydrochloride is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
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-
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- HY-116554
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-
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- HY-164371
-
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Androgen Receptor
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Cancer
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(+)-JJ-74-138, a novel non-competitive androgen receptor (AR) antagonist, is capable of inhibiting Enzalutamide-resistant CRPC .
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-
-
- HY-12042
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AS703026; MSC1936369B
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MEK
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Cancer
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Pimasertib (AS703026) is a highly selective, ATP non-competitive allosteric orally available MEK1/2 inhibitor .
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-
-
- HY-15251
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-
-
- HY-101356
-
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mGluR
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Neurological Disease
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CPCCOEt is a low affinity, selective, non-competitive and reversible antagonist of metabotropic glutamate receptor 1b (mGluR1b) .
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-
-
- HY-148394
-
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Others
|
Infection
Cancer
|
UCK2 Inhibitor-1 (Compound 20874830-2) is a non-competitive UCK2 inhibitor with an IC50 of 4.7 µM .
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-
-
- HY-113730
-
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Others
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Others
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VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
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-
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- HY-163879
-
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Monoamine Oxidase
Reactive Oxygen Species
Ferroptosis
|
Neurological Disease
|
hMAO-B-IN-9 (Compound 25c) is a non-competitive inhibitor for monoamine oxidase B (MAO-B) with an IC50 of 1.58 µM (hMAO-B). hMAO-B-IN-9 forms complex with iron ions as a chelator, and inhibits Erastin (HY-15763)-induced ferroptosis. hMAO-B-IN-9 exhibits antioxidant activity by downregulating the level of reactive oxygen species (ROS). hMAO-B-IN-9 improves cognitive function in mice, without significant toxicity (30 mg/kg). hMAO-B-IN-9 is blood-brain barrier permeable, according to the in silico prediction .
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-
-
- HY-W015309
-
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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-
-
- HY-W107464
-
G6PDi-1
2 Publications Verification
|
PDI
|
Metabolic Disease
Inflammation/Immunology
|
G6PDi-1 is a reversible and non-competitive glucose-6-phosphate dehydrogenase (G6PD) inhibitor with an IC50 of 0.07 μM for human G6PD. G6PDi-1 depletes NADPH most strongly in lymphocytes. G6PDi-1 markedly decreases inflammatory cytokine production in T cells .
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-
-
- HY-N1470
-
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Others
|
Metabolic Disease
|
Plantagoside, isolated from the seeds of Plantago asiatica, is a specific and non-competitive inhibitor for jack bean α-mannosidase, with an IC50 of 5 μM .
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-
-
- HY-116530
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-
-
- HY-103557
-
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mGluR
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Neurological Disease
|
Ro 64-5229 is a selective, non-competitive mGlu2 antagonist. RO 64-5229 reduces the presynaptic inhibitory effect of Neuroligin 1 .
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-
-
- HY-12542
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F 368
|
Calcium Channel
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
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-
-
- HY-12503
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CFM-2
1 Publications Verification
|
iGluR
|
Neurological Disease
Cancer
|
CFM-2 is a potent and selective non-competitive AMPAR antagonist . CFM-2 possesses anticonvulsant activity in various models of seizures .
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-
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- HY-19715
-
-
-
- HY-107716
-
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iGluR
|
Neurological Disease
|
Ro 8-4304 hydrochloride is a potent NMDA receptor antagonist. Ro 8-4304 hydrochloride is a NR2B selective, non-competitive, voltage-independent antagonist .
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-
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- HY-164264
-
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iGluR
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Neurological Disease
|
Caged MK801 (cMK801) is a selective, non-competitive, irreversible NMDA receptor open-channel blocker. NVOC cages are neuro pharmocologically compatible .
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-
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- HY-N0235
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(S)-(+)-Bakuchiol
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Carboxylesterase
p38 MAPK
Autophagy
UGT
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
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-
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- HY-124569
-
|
iGluR
|
Neurological Disease
|
NAB-14 is a potent, selective, orally active and non-competitive GluN2C/2D antagonists with an IC50 of 580 nM for GluN1/GluN2D. NAB-14 shows >800-fold selective for recombinant GluN2C and GluN2D over GluN2A and GluN2B. NAB-14 can cross the blood-brain-barrier .
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-
-
- HY-B1655
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R 6218; Redeptin
|
Calcium Channel
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Neurological Disease
|
Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic agent used for schizophrenia.
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-
-
- HY-19519A
-
DF 2156A
|
CXCR
|
Infection
Inflammation/Immunology
|
Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma .
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-
-
- HY-12542A
-
Dantrolene sodium hydrate
|
Calcium Channel
Autophagy
|
Others
|
Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
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-
-
- HY-116564
-
|
Parasite
GABA Receptor
|
Infection
|
Lotilaner is a parasiticide, acts as a potent non-competitive antagonist of insects GABACl receptors, with an IC50 of 23.84 nM for Drosophila melanogaster GABA receptor. No effect on a dog GABAA receptor .
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-
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- HY-121966
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Riparin III
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Others
|
Cancer
|
Riparin is a nonspecific smooth muscle relaxant. Riparin inhibits CaCl2-induced contractions in a reversible and non-competitive manner and can be used in spasmolytic studies .
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-
-
- HY-W015309R
-
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Neurological Disease
Metabolic Disease
Cancer
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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-
-
- HY-119611A
-
-
- HY-19519
-
DF 2156A free base
|
CXCR
|
Inflammation/Immunology
Cancer
|
Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma .
|
-
- HY-B0199A
-
RS 61443 hydrochloride; TM-MMF hydrochloride
|
Endogenous Metabolite
Bacterial
|
Cancer
|
Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
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-
- HY-155837
-
|
Others
|
Metabolic Disease
|
hPL-IN-2 (compound 2u) is a potent, reversible, and non-competitive inhibitor of pancreatic lipase (IC50: 1.63 μM) and can be used in anti-obesity research .
|
-
- HY-120650
-
|
FAAH
|
Infection
|
CAY10435 is a β-ketooxazapyridine, selective FAAH inhibitor with antimicrobial activity. CAY10435 binds non-competitively to the FAAH of Dictyostelium discoideum with a Kd value of 0.57 nM .
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-
- HY-W010510R
-
|
Endogenous Metabolite
Arginase
|
Metabolic Disease
|
DL-Norvaline (Standard) is the analytical standard of DL-Norvaline. This product is intended for research and analytical applications. DL-Norvaline, a derivative of L-norvaline, L-norvaline is a non-competitive inhibitor of arginase.
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-
- HY-10017
-
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (Ki) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
|
-
- HY-N2197
-
|
nAChR
|
Neurological Disease
|
Hirsuteine is an indole alkaloid extracted from Uncaria rhynchophylla. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes .
|
-
- HY-N6054
-
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
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-
- HY-N12736
-
|
Phosphatase
|
Metabolic Disease
|
Dehydrodanshenol A is a non-competitive inhibitor of Protein tyrosine phosphatase 1B (PTP1B), with an IC50 value of 8.5 μM. Dehydrodanshenol A can be used in diabetes-related research .
|
-
- HY-Y0504R
-
|
Endogenous Metabolite
Cholinesterase (ChE)
|
Metabolic Disease
|
Trimethylammonium chloride (Standard) is the analytical standard of Trimethylammonium chloride. This product is intended for research and analytical applications. Trimethylammonium chlorideIt is an endogenous metabolite that inhibits deacetylation. Trimethylammonium chlorideIs a non-competitive inhibitor of acetylcholinesterase .
|
-
- HY-18689
-
|
iGluR
|
Neurological Disease
|
SYM2206 is a potent and non-competitive AMPA receptor antagonist, with an IC50 of 1.6 μM. SYM2206 blocks Nav1.6-mediated persistent currents .
|
-
- HY-N6650
-
|
Phosphatase
|
Metabolic Disease
|
Isotanshinone IIA, an abietane-type diterpene metabolite, could non-competitively inhibit Protein Tyrosine Phosphatase 1B (PTP1B) activity with an IC50 0f 11.4 μM.
|
-
- HY-119611
-
-
- HY-122200
-
JS399-19
|
Myosin
Fungal
|
Infection
|
Phenamacril (JS399-19) inhibits activity of myosin I non-competitively with an IC50 of 360 nM through suppression of the ATPase activity, exhibits therefore an antifungal efficacy towards Fusarium species .
|
-
- HY-12542R
-
|
Calcium Channel
Autophagy
|
Neurological Disease
Inflammation/Immunology
|
Dantrolene (Standard) is the analytical standard of Dantrolene. This product is intended for research and analytical applications. Dantrolene is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene is a direct-acting skeletal muscle relaxant. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-121787
-
OLC20
|
Others
|
Others
|
OX1a (OLC20) is an Orco antagonist with non-competitive activity that inhibits the activation of oxygen odor receptors (ORs). OX1a is able to reduce the activation of ORs by competitively inhibiting the effects of Orco agonists. OX1a also shows non-competitive inhibition of odor molecules, which may affect the olfactory-mediated behavior of insects. Through structural optimization, OX1a analogs have shown higher antagonistic potency, indicating that this type of compound may have application potential in a wide range of insect species .
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-
- HY-N0235R
-
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
Infection
Metabolic Disease
Inflammation/Immunology
Cancer
|
Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
|
-
- HY-15084A
-
(-)-MK-801 maleate
|
iGluR
|
Neurological Disease
|
(-)-Dizocilpine maleate ((-)-MK-801 maleate) is a less active (-)-enantiomer of Dizocilpine. (-)-Dizocilpine maleate is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with a Ki of 211.7 nM. (-)-Dizocilpine maleate has antidepressant effects .
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-
- HY-N10488
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-11 (compound 10) is a potent, selective and non-competitive BChE (butyrylcholinesterase) inhibitor, with an IC50 of 2.1 μM. BChE-IN-11 can be used for Alzheimer's disease (AD) research .
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-
- HY-155569
-
|
Fungal
|
Infection
|
Chitin synthase inhibitor 13 (compound 12g) is a non-competitive inhibitor of chitin synthase, with an IC50 of 106.7 μM. Chitin synthase inhibitor 13 exhibits a broad-spectrum of antifungal activity .
|
-
- HY-W727627
-
|
Amylases
|
Metabolic Disease
|
5-O-Coumaroylquinic acid is a potent, reversible, non-competitive α-amylase inhibitor with an IC50 value of 69.39 μM. 5-O-Coumaroylquinic acid can be used in diabetes research .
|
-
- HY-10017A
-
|
CXCR
|
Inflammation/Immunology
Endocrinology
|
(R)-SCH 546738 is the R-isomer of SCH 546738 (HY-10017). SCH 546738 is an orally active and non-competitive antagonist for CXCR3 with Ki of 0.4 nM for human CXCR3 receptor .
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-
- HY-U00448
-
|
Others
|
Cancer
|
ADDA 5 hydrochloride is a partial non-competitive inhibitor of cytochrome c oxidase (CcO), with IC50s of 18.93 μM and 31.82 μM for purified CcO from human glioma and bovine heart, respectively.
|
-
- HY-103568
-
|
mGluR
|
Neurological Disease
|
YM-298198 hydrochloride is a high-affinity, selective, orally active, and non-competitive antagonist of metabotropic glutamate receptor type 1 (mGluR1). YM-298198 hydrochloride can be used for the research of neurological disorders .
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-
- HY-120566
-
|
Others
|
Neurological Disease
Inflammation/Immunology
Cancer
|
PSB-16131 is a potent inhibitor of human NTPDase2, exhibiting non-competitive inhibition with an IC50 of 539 nM. PSB-16131 has the potential to be a novel therapeutic agent for the treatment of inflammation, neurodegenerative diseases, and cancer.
|
-
- HY-12542AR
-
|
Calcium Channel
Autophagy
|
Others
|
Dantrolene (sodium hemiheptahydrate) (Standard) is the analytical standard of Dantrolene (sodium hemiheptahydrate). This product is intended for research and analytical applications. Dantrolene sodium hemiheptahydrate is an orally active, non-competitive glutathione reductase inhibitor with a Ki of 111.6 μM and an IC50 of 52.3 μM. Dantrolene sodium hemiheptahydrate is a ryanodine receptor (RyR) antagonist and Ca2+ signaling stabilizer. Dantrolene sodium hemiheptahydrate is a direct-acting skeletal muscle relaxant. Dantrolene sodium hemiheptahydrate can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome .
|
-
- HY-13206
-
|
mGluR
|
Neurological Disease
|
MTEP hydrochloride is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP hydrochloride shows antidepressant and anxiolytic-like effects. MTEP hydrochloride can be used for Parkinson's disease research .
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-
- HY-W015309S
-
|
iGluR
|
Neurological Disease
|
Decanoic acid-d3 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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-
- HY-W015309S2
-
|
iGluR
|
Neurological Disease
|
Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-W015309S1
-
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iGluR
|
Neurological Disease
|
Decanoic acid-d199 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-W015309S3
-
|
iGluR
|
Neurological Disease
|
Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
|
-
- HY-107700
-
GV 150526A
|
iGluR
|
Cardiovascular Disease
|
Gavestinel (GV 150526A) is a potent, selective, orally active and non-competitive antagonist of NMDA receptor. Gavestinel binds to the glycine site of the NMDA receptor, with a pKi of 8.5. Gavestinel can be used for the research of acute ischemic stroke .
|
-
- HY-153629
-
|
Ferroptosis
|
Cancer
|
FSEN1 is a potent and non-competitive FSP1 inhibitor with an IC50 value of 313 nM. FSEN1 triggers iron death in cancer cells by inhibiting FSP1. FSEN1 can be used in research of cancer .
|
-
- HY-126133
-
|
Ras
|
Cardiovascular Disease
Others
|
AM-001 is a non-competitive inhibitor of Epac1 that blocks the activation of Rap1, a downstream effector of Epac1, in cultured cells. AM-001 can be used in heart disease-related research .
|
-
- HY-12219
-
Trodusquemine; Aminosterol-1436
|
Phosphatase
|
Endocrinology
|
MSI-1436 is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of appr 1 μM, 200-fold preference over TCPTP (IC50, 224 μM).
|
-
- HY-13848
-
KAND567
|
CX3CR1
CXCR
|
Inflammation/Immunology
Endocrinology
|
AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively .
|
-
- HY-12219A
-
Trodusquemine lactate; Aminosterol-1436 lactate
|
Phosphatase
|
Endocrinology
|
MSI-1436 lactate is a selective, non-competitive inhibitor of the enzyme protein-tyrosine phosphatase 1B (PTP1B), with an IC50 of 1 μM, 200-fold preference over TCPTP (IC50 of 224 μM).
|
-
- HY-135891
-
|
CCR
|
Neurological Disease
|
AZD2423 is a potent, selective, orally bioavailable, and non-competitive CCR2 chemokine receptor negative allosteric modulator. AZD2423 has an IC50 of 1.2 nM for CCR2 Ca 2+ flux .
|
-
- HY-B0690
-
-
- HY-N3090
-
|
Cytochrome P450
|
Metabolic Disease
|
Peucedanol is a non-competitive inhibitor of CYP3A4 with a Ki value of 4.07 μM and a competitive inhibitor of CYP1A2 and CYP2D6 with Ki values of 3.39 μM and 6.77 μM, respectively .
|
-
- HY-103566
-
|
mGluR
EGFR
|
Neurological Disease
|
LY456236 is a selective, non-competitive and orally active mGlu1 receptor antagonist that inhibits phosphoinositide hydrolysis with an IC50 of 0.145 μM. LY456236 also inhibits EGFR with an IC50 of 0.91 μM .
|
-
- HY-15251A
-
(Rac)-Repertaxin; (Rac)-DF 1681Y
|
Others
|
Inflammation/Immunology
Endocrinology
Cancer
|
(Rac)-Reparixin is the isomer of Reparixin (HY-15251), and can be used as an experimental control. Reparixin is a non-competitive allosteric inhibitor of the chemokine receptors CXCR1 and CXCR2 activation with IC50s of 1 and 100 nM, respectively.
|
-
- HY-107694
-
(Rac)-MK-801
|
Others
|
Others
|
(Rac)-Dizocilpine ((Rac)-MK-801) is the racemate of Dizocilpine (HY-15084B). Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist .
|
-
- HY-101116
-
|
GCGR
|
Metabolic Disease
|
GLP-1R Antagonist 1 (compound 5d) is an orally active, CNS penetrant and non-competitive antagonist of glucagon-like peptide 1 receptor (GLP-1R), with an IC50 of 650 nM .
|
-
- HY-14854
-
ATI-5923
|
Others
|
Cardiovascular Disease
|
Tecarfarin (ATI-5923) is an orally active and non-competitive vitamin K epoxide reductase (VKOR) antagonist, and impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X . Tecarfarin has the antithrombotic activity .
|
-
- HY-135878
-
|
Adenylate Cyclase
Adrenergic Receptor
|
Metabolic Disease
|
2',5'-Dideoxyadenosine is a potent and non-competitive adenylyl cyclase inhibitor via binding the P-site with an IC50 of 3 µM . 2',5'-Dideoxyadenosine is a nucleoside analog and exerts a potent antiadrenergic action in heart .
|
-
- HY-148395
-
|
Dihydroorotate Dehydrogenase
|
Cancer
|
UCK2 Inhibitor-2 is a non-competitive uridine-cytidine kinase 2 (UCK2) inhibitor with an IC50 value of 3.8 µM. UCK2 Inhibitor-2 can suppress uridine salvage in cells .
|
-
- HY-N2463
-
|
Indoleamine 2,3-Dioxygenase (IDO)
|
Cancer
|
Kushenol E is a class of flavonoids isolated from Sophora flavescens and is a non-competitive indoleamine 2,3-dioxygenase 1 (IDO1) inhibitor with an IC50 of 7.7 µM and a Ki of 9.5 µM, has anti-tumor activity .
|
-
- HY-14854A
-
ATI-5923 sodium
|
Others
|
Metabolic Disease
|
Tecarfarin sodium (ATI-5923 sodium) is a novel orally active non-competitive vitamin K epoxide reductase (VKOR) antagonist, impairs the activation of the vitamin K-dependent clotting factors II, VII, IX and X .
Tecarfarin sodium has the antithrombotic activity .
|
-
- HY-126015
-
|
Acyltransferase
|
Metabolic Disease
|
P053 is a potent, non-competitive and selective ceramide synthase 1 (CerS1) inhibitor wirh an IC50 of 0.5 μM. P053 acts as an endogenous inhibitor of mitochondrial fatty acid oxidation in muscle. Whole-body adiposity regulator .
|
-
- HY-N9506
-
|
GABA Receptor
|
Neurological Disease
|
Anisatin, a pure toxic substance isolated from the seeds of a Japanese plant (Illicium anisatum) acts as a picrotoxin-like, non-competitive GABA antagonist. Anisatin suppresses GABA-induced currents in a concentration-dependent manner with an EC50 of ~1.10 μM .
|
-
- HY-162107
-
|
DYRK
|
Neurological Disease
|
Dyrk1A-IN-6 (compound 7cc) is an EGCG-like non-competitive inhibitor of DYRK1A. Dyrk1A-IN-6 can be used to alleviate cognitive defects in Down syndrome models .
|
-
- HY-N4193
-
|
Acyltransferase
|
Cardiovascular Disease
|
Glabrol (Compound 1), One isoprenyl flavonoid was isolated from ethanol extract of licorice roots, is a potent and non-competitive Acyl-coenzyme A: cholesterol acyltransferase (ACAT) inhibitor with an IC50 value of 24.6 μM for rat liver microsomal ACAT activity .
|
-
- HY-N7377
-
|
Glucosidase
|
Metabolic Disease
|
Butyl isobutyl phthalate is isolated from the rhizoid of Laminaria japonica. Butyl isobutyl phthalate is a non-competitive α-glucosidase inhibitor with an IC50 value of 38 μM. Butyl isobutyl phthalate shows a hypoglycemic effect and has the potential for diabetes treatment .
|
-
- HY-P1271
-
|
nAChR
|
Cardiovascular Disease
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-12881
-
SL-820715
|
iGluR
|
Neurological Disease
|
Eliprodil(SL-820715) is a non-competitive NR2B-NMDA receptor antagonist(IC50=1 uM), less potent for NR2A- and NR2C-containing receptors(IC50> 100 uM).
|
-
- HY-15257A
-
AFQ-056 racemate
|
mGluR
|
Neurological Disease
|
Mavoglurant racemate (AFQ-056 racemate) is the racemate of Mavoglurant. Mavoglurant is a novel, non-competitive mGlu5 receptor antagonist . Mavoglurant (racemate) 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-15756
-
|
Phosphatase
|
Metabolic Disease
|
PTP1B-IN-4 is a non-competitive allosteric inhibitor of the protein tyrosine phosphatase PTP1B, with an IC50 of 8 μM. PTP1B-IN-4 is potentail for the research of obesity and diabetes .
|
-
- HY-15084B
-
MK-801
|
iGluR
|
Neurological Disease
|
Dizocilpine (MK-801), a potent anticonvulsant, is a selective and non-competitive NMDA receptor antagonist, with a Kd of 37.2 nM in rat brain membranes. Dizocilpine acts by binding to a site located within the NMDA associated ion channel and thus prevents Ca 2+ flux .
|
-
- HY-N10489
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
BChE-IN-12 (compound 12) is a potent butyrylcholinesterase (BChE) non-competitive inhibitor with an IC50 value of 2.3 μM. BChE-IN-12 can be isolated from Bletilla striata. BChE-IN-12 can be used for the research of Alzheimer's disease (AD) .
|
-
- HY-107525
-
|
EAAT
|
Neurological Disease
|
(±)-HIP-A is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-A is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-A can be used in the study of neurological diseases .
|
-
- HY-E70252
-
|
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-N6054R
-
|
Parasite
Topoisomerase
|
Infection
Inflammation/Immunology
|
Niranthin (Standard) is the analytical standard of Niranthin. This product is intended for research and analytical applications. Niranthin, a lignan with a wide spectrum of pharmacological activities. Niranthin is a potent and non-competitive inhibitor of heterodimeric type IB topoisomerase of L. donovani. Niranthin can be used for the research of drug-resistant leishmaniasis research.
|
-
- HY-108474
-
AG 337
|
Thymidylate Synthase
|
Cancer
|
Nolatrexed dihydrochloride (AG 337) is a non-competitive lipophilic inhibitor of thymidylate synthase, interacts at the folate cofactor binding site of the enzyme, with a Ki of 11 nM for human thymidylate synthase . Nolatrexed dihydrochloride (AG 337) induces cell cycle arrest in S phase of cancer cells. Anti-cancer activity .
|
-
- HY-111926
-
|
Others
|
Metabolic Disease
|
N6-Methyladenosine 5'-monophosphate disodium salt is an activator of glycogen phosphorylase b, with a Ka value of 22 µM . N6-Methyladenosine 5'-monophosphate disodium salt is a non-competitive rat adenylate kinase II inhibitor .
|
-
- HY-P1271A
-
|
nAChR
|
Cardiovascular Disease
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-129137
-
Cy 3-soph
|
Others
|
Others
|
Cyanidin 3-sophoroside chloride is a potent non-competitive reversible polyphenol oxidase (PPO) inhibitor. Also, Cyanidin 3-sophoroside chloride can be used as an anti-browning agent to inhibit the degree of PPO browning, enhance the antioxidant damage capacity of fruits and prolong the storage period .
|
-
- HY-162893
-
|
Glucosidase
|
Metabolic Disease
|
SX29 is an orally active non-competitive α-glucosidase inhibitor with an IC50 value of 2.12 μM. SX29 exhibits hypoglycemic activity, and oral administration of SX29 can reduce blood glucose levels and improve glucose tolerance in diabetic mice .
|
-
- HY-160604
-
FPL 12924; PR 934-423; FPL 13592
|
iGluR
|
Neurological Disease
|
Remacemide (FPL 12924) is an orally active, non-competitive, low-affinity NMDA receptor antagonist. Remacemide shows neuroprotection activity in animal models of hypoxia and ischemic stroke. Remacemide is also an anticonvulsant, and can be used in Parkinson's disease and Huntington's disease research .
|
-
- HY-101043
-
|
Sigma Receptor
iGluR
|
Neurological Disease
|
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .
|
-
- HY-157489
-
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-47 (compound 8H) is a non-competitive α-glucosidase (α-glucosidase) inhibitor with IC50 value is 38.2 μM and Ki value is 38.2 μM. α-Glucosidase-IN-47 can be used in diabetes research. .
|
-
- HY-B0199AS
-
RS 61443-d4 hydrochloride; TM-MMF-d4 hydrochloride
|
Bacterial
Endogenous Metabolite
Isotope-Labeled Compounds
|
Cancer
|
Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
|
-
- HY-139158
-
|
HIV
|
Infection
|
Ainuovirine is a second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). Ainuovirine inhibits HIV replication by non-competitively binding to HIV reverse transcriptase and blocking the reverse transcription process of viral RNA. Ainuovirine can be used for human immunodeficiency virus (HIV) type 1 infection .
|
-
- HY-134525
-
|
iGluR
|
Others
|
Ro 8-4304 is a non-competitive, voltage-independent and state-dependent antagonist for NMDA receptor. Ro 8-4304 inhibits 10 μM NMDA-induced currents and 100 μM NMDA-induced currents with IC50s of 2.3 μM and 0.36 μM .
|
-
- HY-114203
-
-
- HY-107524
-
|
EAAT
|
Neurological Disease
|
(±)-HIP-B is a non-competitive excitatory amino acid transporter (EAAT) blocker that effectively blocks Glu uptake (IC50=17-18 μM). (±)-HIP-B is also a lead compound against ischemia-induced neuronal degeneration. (±)-HIP-B can be used in the study of neurological diseases .
|
-
- HY-N3136
-
|
Histamine Receptor
|
Others
|
Onitin is a natural product, that can be isolated from Onychium siliculosum. Onitin is also a non-competitive antagonist of histamine. Onitin shows activity in blocking the peristaltic reflex of the guinea-pig ileum, in inhibition of the responses of guinea-pig ileum to histamine and of inhibition of the responses of guinea-pig tracheal muscle to histamine .
|
-
- HY-N1919
-
Raubasine
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-13965
-
ML161
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM . Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo .
|
-
- HY-121515
-
|
Phosphatase
|
Metabolic Disease
|
DPM-1001 is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 has anti-diabetic property .
|
-
- HY-121515A
-
|
Phosphatase
|
Metabolic Disease
|
DPM-1001 trihydrochloride is a potent, specific, orally active and non-competitive inhibitor of protein-tyrosine phosphatase (PTP1B) with an IC50 of 100 nM. DPM-1001 trihydrochloride is an analog of the specific PTP1B inhibitor MSI-1436. DPM-1001 trihydrochloride has anti-diabetic property .
|
-
- HY-Y0413
-
Diacetyl monoxime; DAM
|
Na+/K+ ATPase
Myosin
|
Metabolic Disease
|
Biacetyl monoxime (Diacetyl monoxime), a myosin ATPase inhibitor, is a skeletal and cardiac muscle contraction inhibitor. Biacetyl monoxime is also a well-characterized non-competitive inhibitor of chemical and motile activity of skeletal muscle myosin-II. Biacetyl monoxime induces sarcoplasmic reticulum Ca 2+ release .
|
-
- HY-N1919A
-
Raubasine hydrochloride
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
Ajmalicine (Raubasine) hydrochloride is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine hydrochloride is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine hydrochloride also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-13859
-
L-FMAU
|
HBV
DNA/RNA Synthesis
Orthopoxvirus
|
Infection
|
Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
|
-
- HY-W424730
-
|
Others
|
Others
|
HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
|
-
- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Beta-secretase
|
Neurological Disease
Cancer
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
-
- HY-15703
-
QNZ46
1 Publications Verification
|
iGluR
|
Neurological Disease
|
QNZ46 is a NR2C/NR2D-selective NMDA receptor non-competitive antagonist (IC50 values are 3, 6, 229, and >300, >300 μM for NR2D, NR2C, NR2A, NR2B, and GluR1, respectively).
|
-
- HY-107526
-
(Rac)-NFPS
|
GlyT
|
Neurological Disease
|
NFPS is a selective, non-competitive glycine transporter-1 (GlyT1) inhibitor with IC50s of 2.8 nM and 9.8 nM for hGlyT1 and rGlyT1, respectively . NFPS exerts neuroprotection via glyR alpha1 subunit in the rat model of transient focal cerebral ischaemia and reperfusion .
|
-
- HY-P1178
-
|
Trk Receptor
|
Neurological Disease
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-146333
-
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
|
TRAP-6-IN-1 (Compound 8) is a dual collagen and TRAP-6 inhibitor with IC50 values of 17.12 µM and 11.88 µM against collagen and TRAP-6, respectively. TRAP-6-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner .
|
-
- HY-161913
-
|
Dopamine Transporter
|
Neurological Disease
|
AC-4-248 is an atypical non-competitive dopamine transporter (DAT) inhibitor and reduces the potency of cocaine to inhibit DAT. AC-4-248 is a non-selective inhibitor of SLC6 transporters with IC50 values for hDAT, hSERT, and hNET of 45.5 μM, 96.2 μM, and 250 μM, respectively .
|
-
- HY-119097
-
|
mGluR
|
Neurological Disease
|
LY456066 is a selective non-competitive metabotropic glutamate receptors (mGluR1) antagonist with an IC50 value of 52.0 nM. LY456066 is effective in rodent models of anxiolysis and nociception. LY456066 reduces hyperalgesia and the amount of licking and flinching following formalin injection, which is promising for research of analgesics for chronic pain .
|
-
- HY-120020
-
|
Others
|
Others
|
LY-395153 is an AMPA receptor enhancer with the activity of binding to AMPA receptors. LY-395153 can bind to natural and recombinant AMPA receptors, and its binding is affected by AMPA receptor agonists and can be competitively or non-competitively inhibited by some compounds. It is a useful probe for marking unique regulatory sites of AMPA receptors.
|
-
- HY-17395S
-
TDT 067-d3 hydrochloride
|
Isotope-Labeled Compounds
Fungal
Bacterial
Antibiotic
|
Infection
|
Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
|
-
- HY-17395AS
-
TDT 067-d7
|
Isotope-Labeled Compounds
Fungal
Bacterial
Antibiotic
|
Infection
|
Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
|
-
- HY-133146
-
|
Phosphatase
Apoptosis
|
Inflammation/Immunology
|
DJ001 is a highly specific, selective and non-competitive protein tyrosine phosphatase-σ (PTPσ) inhibitor with an IC50 of 1.43 μM. DJ001 displays no inhibitory activity against other phosphatases, with only modest inhibitory activity against Protein Phosphatase 5. DJ001 promotes promote hematopoietic stem cell regeneration .
|
-
- HY-103195
-
NKY80
1 Publications Verification
|
Adenylate Cyclase
|
Metabolic Disease
|
NKY80 is a potent, selective and non-competitive adenylyl cyclase (AC) type V isoform inhibitor with IC50s of 8.3 µM, 132 µM and 1.7 mM for type V, III and II, respectively. NKY80 is a non-nucleoside quinazolinone and regulates the AC catalytic activity in heart and lung tissues .
|
-
- HY-131350
-
|
Proteasome
Parasite
|
Infection
|
LXE408 is an orally active, non-competitive and kinetoplastid-selective proteasome inhibitor. LXE408 has an IC50 of 0.04 μM for L. donovani proteasome and an EC50 of 0.04 μM for L. donovani. LXE408 has a low propensity to cross the blood brain barrier. LXE408 has the potential for visceral leishmaniasis (VL) research .
|
-
- HY-136026
-
BLU-5937
|
P2X Receptor
|
Inflammation/Immunology
|
Camlipixant (BLU-5937) a potent, selective, non-competitive and orally active P2X3 homotrimeric receptor antagonist with an IC50 of 25 nM against hP2X3 homotrimeric. Camlipixant shows potent anti-tussive effect and no taste alteration. Camlipixant can be used for the research of unexplained, refractory chronic cough .
|
-
- HY-149716
-
|
Phosphodiesterase (PDE)
|
Cancer
|
MEY-003 is an Autotaxin(ATX) inhibitor with EC50s of 460 nM and 1.09 μM for hATX-β and hATX-ɣ (analysis with LPC18:1). MEY-003 behaves as a non-competitive inhibitor with K iof 432 nM. MEY-003 can be used for targeted ATX-related disease research .
|
-
- HY-N12761
-
|
Phosphatase
Glucosidase
|
Metabolic Disease
Inflammation/Immunology
|
Penpaxilloids A (Compound 1) is a non-competitive inhibitor of protein tyrosine phosphatase 1B (PTP1B) with an IC50 value of 8.60 μM. Penpaxilloids A can be isolated from the fungus Penicillium sp. ZYX-Z-143. Penpaxilloids A is also an α-glucosidase (α-glucosidase) inhibitor with anti-inflammatory activity .
|
-
- HY-107001
-
(S)-DPC 961; DMP 961
|
HIV
Reverse Transcriptase
|
Infection
|
DPC 961 (DMP 961) is a non-nucleoside reverse transcriptase inhibitor (NNRTI). DPC 961 is a potent and specific inhibitor of HIV-1 reverse transcriptase, which inhibits the activity of HIV-1 reverse transcriptase in a non-competitive manner, thereby preventing viral replication. DPC 961 can be used for research on AIDS .
|
-
- HY-162884
-
|
Others
|
Infection
|
EcGUS-IN-1 (Compound E-9) is a non-competitive β-glucuronidase inhibitor, with an IC50 of 2.68 μM and a Ki value of 1.64 μM. EcGUS-IN-1 can improve gastrointestinal adverse events (GIAE) caused by Escherichia coli infection by inhibiting E. coli β-glucuronidase activity .
|
-
- HY-133596
-
|
Potassium Channel
GABA Receptor
|
Neurological Disease
|
12,14-Dichlorodehydroabietic acid, a chlorinated resin acid, is a potent Ca 2+-activated K + (BK) channel opener. 12,14-Dichlorodehydroabietic acid blocks GABA-dependent chloride entry in mammalian brain and operates as a non-competitive GABAA antagonist. 12,14-Dichlorodehydroabietic acid increases cytosolic free Ca 2+ and stimulates transmitter release .
|
-
- HY-P1178A
-
|
Trk Receptor
|
Neurological Disease
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-162059
-
|
Pim
Apoptosis
Caspase
|
Cancer
|
Pim-1 kinase inhibitor 10 (compound 13a) is a both competitive and non-competitive inhibitor of PIM-1/2 kinase. Pim-1 kinase inhibitor 10 can induce cell apoptosis and exhibits anticancer activity. Pim-1 kinase inhibitor 10 also induces caspase 3/7 activation .
|
-
- HY-10572A
-
(R)-DMP 266; (R)-EFV; (R)-L-743726
|
Reverse Transcriptase
|
Infection
|
(R)-Efavirenz ((R)-DMP 266) is a non-nucleoside reverse transcriptase inhibitor that acts by non-competitive inhibition of the viral enzyme. (R)-Efavirenz can be metabolized by CYP2B6 to 8-hydroxyefavirenz in a highly stereoselective manner. (R)-Efavirenz is promising to be a useful probe for the CYP2B6 active site and catalytic mechanisms .
|
-
- HY-B0379A
-
|
nAChR
|
Neurological Disease
|
Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
|
-
- HY-B1126
-
|
iGluR
|
Neurological Disease
|
Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases .
|
-
- HY-N10096
-
|
Parasite
|
Infection
|
Epoxyazadiradione is a limonoid purified from neem (Azadirachta indica) fruits. Epoxyazadiradione inhibits the tautomerase activity of MIF of both human (huMIF) and malaria parasites (Plasmodium falciparum (PfMIF) and Plasmodium yoelii (PyMIF)) non-competitively in a reversible fashion (Ki, 2.11-5.23 μM). Epoxyazadiradione has the potential against proinflammatory reactions induced by MIF of both malaria parasites and human .
|
-
- HY-117769
-
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
|
GSK837149A is a selective inhibitor of human Fatty Acid Synthase (FASN) targeting the KR domain. GSK837149A has reversible inhibition effect on FASN and selectivity for type I FASN (Ki=30 nM). GSK837149A is also a competitive inhibitor of NADPH and a non-competitive inhibitor of acetoacetyl-CoA. GSK837149A can be used for the research of obesity and breast cancer .
|
-
- HY-13206A
-
|
mGluR
|
Neurological Disease
|
MTEP is a potent, non-competitive and highly selective mGluR5 antagonist, with an IC50 of 5 nM and a Ki of 16 nM. MTEP shows antidepressant and anxiolytic-like effects. MTEP can be used for Parkinson's disease research . MTEP 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-114511
-
|
Factor VIIa
|
Cardiovascular Disease
|
BMS-593214 is an active site-directed factor (F) VIIa inhibitor. BMS-593214 shows antithrombotic and antihaemostatic properties. BMS-593214 is a direct competitive inhibitor of human FVIIa and a non-competitive inhibitor of Viia-activated substrate FX. BMS-593214 prevents electroinduced carotid artery thrombosis (AT) and wire induced vena cava thrombosis (VT) .
|
-
- HY-155240
-
|
Tyrosinase
|
Cancer
|
Tyrosinase-IN-13 (compound 3c), a derivative of Flurbiprofen (HY-10582), is a potent, non-competitive tyrosinase inhibitor (IC50=68 μM; Ki=36.3 μM). Tyrosinase-IN-13 is cytotoxic against hepatocellular carcinoma (HepG2), colorectal cancer (HT-29), and melanoma (B16F10) .
|
-
- HY-N12688
-
|
Glucosidase
Amylases
|
Metabolic Disease
|
2,3-Dihydrocalodenin B (Compound 6) is a compound that can be isolated from Knema globularia. 2,3-Dihydrocalodenin B is a potent and non-competitive inhibitor against α-glucosidase and α-amylase, with IC50 values of 1.1 and 2.6 μM, respectively. 2,3-Dihydrocalodenin B can be used for the research of diabetes .
|
-
- HY-Y0258A
-
|
Bacterial
Sodium Channel
|
Neurological Disease
|
Benzocaine (hydrochloride) is an orally active local agent that can suppress or relieve pain, that acts on voltage-gated Na + channels at a common receptor, with an IC50 value of 0.8 mM at +30 mV. Additionally, Benzocaine (hydrochloride) non-competitively inhibits Ca-ATPase binding with Ca 2+, with an IC50 of 47.1 mM. Benzocaine (hydrochloride) can be used in research within the field of neuromuscular regulation .
|
-
- HY-P10571
-
|
Melanocortin Receptor
|
Endocrinology
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-15469
-
|
P2X Receptor
|
Neurological Disease
|
GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .
|
-
- HY-17387
-
Huperzine A
|
Cholinesterase (ChE)
Apoptosis
iGluR
|
Neurological Disease
|
(-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
|
-
- HY-B0091
-
CD271
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
|
-
- HY-B0091A
-
CD 271 sodium salt
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Adapalene (CD271) sodium salt, a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene sodium salt is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene sodium salt also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene sodium salt exhibits anti-tumor activity .
|
-
- HY-N0063
-
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CL pro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-15470
-
|
P2X Receptor
|
Neurological Disease
|
GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
|
-
- HY-103550
-
|
mGluR
|
Neurological Disease
|
A-841720 is a potent, non-competitive and selective mGlu1 receptor antagonist with an IC50 of 10 nM for human mGlu1 receptor. A-841720 displays 34-fold selectivity over mGlu5 (IC50 of 342 nM), and no significant activity at a range of other neurotransmitter receptors, ion channels, and transporters. A-841720 has the potential for chronic pain research .
|
-
- HY-149308
-
|
Macrophage migration inhibitory factor (MIF)
|
Infection
|
MKA031 (compound 6y) is a non-competitive MIF inhibitor with an IC50 value of 1.7 μM. MKA031 (compound 6y) interferes with MIF/AIF interaction, MIF nuclear translocation, and N-methyl-N'-nitro-N-nitrosoguanidine (MNNG)-induced dependent cell death. MKA031 can be used in the study of chronic hepatitis C virus infection .
|
-
- HY-N1919R
-
|
Adrenergic Receptor
Cholinesterase (ChE)
|
Neurological Disease
Endocrinology
|
Ajmalicine (Standard) is the analytical standard of Ajmalicine. This product is intended for research and analytical applications. Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
|
-
- HY-13716
-
(S,R)-Noscapine
|
Opioid Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
|
-
- HY-B0369A
-
|
iGluR
|
Neurological Disease
|
Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases .
|
-
- HY-12542S
-
F 368-13C3
|
Isotope-Labeled Compounds
Glutathione Reductase
|
Neurological Disease
Inflammation/Immunology
|
Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
|
-
- HY-116096
-
15(R)-Prostaglandin E1; 15-Epiprostaglandin E1
|
15-PGDH
|
Others
|
15-epi-PGE1 (15R-Prostaglandin E1; 15-Epiprostaglandin E1) is a stereoisomer of PGE1 (HY-B0131) but with less biological activity . 15-epi-PGE1 is a non-competitive inhibitor for human placental 15-Hydroxyprostaglandin dehydrogenase (15-PGDH) with an IC50 of 170 μM .
|
-
- HY-111291
-
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
ICI 169369 (free base) is an orally active, selective and non-competitive antagonist against 5HT receptor. ICI 169369 (free base) blunts the vasopressin (AVP), but not the ACTH, prolactin or growth hormone reponses to insulin-induced hypoglycaemia. ICI 169369 (free base) blocks centrally mediated 5-HT responses and lowers portal pressure in portal hypertensive rats .
|
-
- HY-17395
-
TDT 067 hydrochloride
|
Fungal
Bacterial
Antibiotic
|
Infection
|
Terbinafine hydrochloride (TDT 067 hydrochloride) is an orally active and potent antifungal agent. Terbinafine hydrochloride is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine hydrochloride also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine hydrochloride 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-17395A
-
TDT 067
|
Fungal
Bacterial
Antibiotic
|
Infection
|
Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine 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-13457
-
TCN 201
1 Publications Verification
|
iGluR
|
Neurological Disease
|
TCN 201 is a potent, selective and non-competitive antagonist of GluN1/GluN2A NMDA receptor, with a pIC50 of 6.8. TCN 201 is selective for GluN1/GluN2A NMDA receptor over GluN1/GluN2B NMDA receptor (pIC50<4.3) .
|
-
- HY-146142
-
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB .
|
-
- HY-157382
-
|
Cholinesterase (ChE)
Amyloid-β
MMP
|
Neurological Disease
|
AChE-IN-51 (compound 8C) is an orally active, non-competitive inhibitor of AChE and BChE (IC50: 84 nM, 97 nM). It also inhibits MMP-2 and amyloid Aβ1-42 aggregates (IC50: 724 nM, 302 nM). AChE-IN-51 has low cytotoxicity and in silico predicted blood-brain barrier permeability. Can be used for research on diseases such as Alzheimer's disease (AD) .
|
-
- HY-129636
-
(E)-GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
CLH304a (compound 14) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a decreases GABA-induced IP3 production with an IC50 of 37.9 μM. CLH304a has no effect on other GPCR Class C members such as mGluR1, mGluR2, and mGluR5. CLH304a acts on the heptahelical domain of GB2 subunits and non-competitively inhibits the effect of agonists with inverse agonist properties. CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptor .
|
-
- HY-N0241
-
|
Cholinesterase (ChE)
|
Metabolic Disease
|
Rhodionin, isolated from the root of Rhodiola crenulata, is a specific non-competitive cytochrome P450 2D6 inhibitor with an IC50 of 0.761 μM and a Ki of 0.769 μM . Rhodionin exhibits potent, dose-dependent inhibitory effects on acetylcholinesterase (AChE) with IC50 ranged from 57.50 to 2.43 μg/mL . Rhodionin exhibits potent DPPH free radical scavenging activities, with an IC50 of 19.49 μM .
|
-
- HY-123872
-
|
p97
|
Cancer
|
MSC1094308 is a non-competitive and reversible VPS4B/p97 (VCP) (I/II type AAA ATPase) allosteric inhibitor, with IC50 values of 0.71 μM and 7.2 μM for VPS4B and p97, respectively . MSC1094308 inhibits the D2 ATPase activity by binding to a agentable hotspot of p97. MSC1094308 can be used in study of cancer .
|
-
- HY-143288
-
|
NTPDase
|
Infection
Inflammation/Immunology
Cancer
|
NTPDase-IN-2 (compound 5g) is a selective NTPDase inhibitor with IC50s of 0.04 and 2.27 µM for h-NTPDase-2/-8, respectively. NTPDase-IN-2 non-competitively inhibits h-NTPDase-1/-2 with a Km of 74 µM for h-NTPDase-2. NTPDase-IN-2 can be used in studies of cancer, immunologic disorders as well as bacterial infections .
|
-
- HY-115827
-
|
Others
|
Others
|
AH22921 is an EP4 prostaglandin receptor antagonist with the activity of antagonizing the activation of adenylate cyclase by prostaglandins in CHO cells. AH22921 can shift the PGE2 concentration-response curve to the right in CHO cells. It is a non-competitive antagonist that is selective for EP4 receptors and has an antagonistic effect on EP4 receptors in CHO cells, but does not affect the PGE2 concentration-response curve in NPE cells containing EP2 receptors.
|
-
- HY-118061
-
|
Others
|
Infection
|
VCC234718 is a molecule with mycobacterial growth inhibitory activity, specifically targeting Mycobacterium tuberculosis (Mtb). The primary molecular target of VCC234718 is inosine monophosphate dehydrogenase (GuaB2), and it inhibits the growth of Mtb by affecting the function of this enzyme. VCC234718 inhibits GuaB2 with a K value of 100 nM and exhibits non-competitive inhibition with IMP and NAD+. VCC234718 exerts its inhibitory effect by directly interacting with IMP and binding at the NAD+ site .
|
-
- HY-B0091S
-
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].
|
-
- HY-N4110
-
|
Cytochrome P450
NF-κB
Interleukin Related
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
Friedelin is derived from the leaves of Maytenus ilicifolia (Mart). Friedelin is an orally active non-competitive inhibitor of CYP3A4, with IC50 and Ki values of 10.79 μM and 6.16 μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1, with IC50 and Ki values of 22.54 μM and 18.02 μM, respectively. Friedelin can be used in research related to inflammation, neurological diseases, and metabolic disorders .
|
-
- HY-146332
-
|
Others
|
Cardiovascular Disease
|
Collagen-IN-1 (compound 3), an ortho-carbonyl hydroquinone derivative, is a selective inhibitor on collagen. Collagen-IN-1 inhibits agonist-induced platelet aggregation in a non-competitive manner with an IC50 value of 1.77 μM. Collagen-IN-1 reduces the expression of P-selectin, activation of glycoprotein IIb/IIIa, and release of adenosine triphosphate and CD63 from platelet. Collagen-IN-1 has the potential for platelet-related thrombosis diseases research .
|
-
- HY-17395B
-
TDT 067 lactate
|
Antibiotic
Fungal
Bacterial
|
Infection
|
Terbinafine lactate (TDT 067 lactate) is an orally active and potent antifungal agent. Terbinafine lactate is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine lactate also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine (lactate) 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-143287
-
|
NTPDase
|
Infection
Inflammation/Immunology
Cancer
|
NTPDase-IN-1 (compound 5a) is a selective NTPDase inhibitor with IC50s of 0.05, 0.23 and 0.54 µM for h-NTPDase-1/-2/-8, respectively. NTPDase-IN-1 non-competitively inhibits h-NTPDase-1/-2 with a Km of 21 µM for h-NTPDase-1. NTPDase-IN-1 can be used in studies of cancer, immunologic disorders as well as bacterial infections .
|
-
- HY-148396
-
|
DNA/RNA Synthesis
|
Infection
Cancer
|
UCK2 Inhibitor-3 is a non-competitive inhibitor of uridine-cytidine kinase 2 (UCK2, a pyrimidine salvage enzyme) with an IC50 value of 16.6 μM. UCK2 can replace dihydroorotate dehydrogenase (DHODH), in a certain extent, in infected or rapidly dividing cells to continue efficient uridine salvage. UCK2 Inhibitor-3 also inhibits DNA polymerase eta and kappa with IC50s of 56 μM and 16 μM .
|
-
- HY-B1126S
-
|
iGluR
|
Neurological Disease
|
Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
|
-
- HY-149300
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
SB-1436 is an Cholinesterase (ChE) inhibitor, inhibits acetylcholinesterase (AChE), butyrylcholinesterase (BChE) and recombinant human acetylcholinesterase (rHuAChE) with IC50s of 0.176, 0.37 and 0.08 μM, respectively. SB-1436 inhibits AChE and BChE in a non-competitive manner with Kis of 0.046 and 0.115 μM, respectively. SB-1436 significantly stops the self-aggregation of Aβ, and can be used for neurological disease research .
|
-
- HY-B0091R
-
CD271 (Standard)
|
RAR/RXR
Autophagy
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Adapalene (Standard) is the analytical standard of Adapalene. This product is intended for research and analytical applications. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity .
|
-
- HY-B0379AR
-
|
nAChR
|
Neurological Disease
|
Adiphenine (hydrochloride) (Standard) is the analytical standard of Adiphenine (hydrochloride). This product is intended for research and analytical applications. Adiphenine hydrochloride is a non-competitive inhibitor of nicotinic acetylcholine receptor (nAChR), with an IC50s of 1.9, 1.8, 3.7, and 6.3 μM for α1, α3β4, α4β2, and α4β4, respectively. Adiphenine hydrochloride has anticonvulsant effects .
|
-
- HY-N0063R
-
|
SARS-CoV
HBV
|
Infection
Metabolic Disease
Cancer
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
- HY-123311
-
|
Adrenergic Receptor
|
Endocrinology
|
CP59430 is an azide analog of the α-adrenaline receptor antagonist Prazosin (HY-B0193). P59430 behaves as a competitive antagonist of α1-adrenaline receptor before photolysis. After photolysis, it specifically and irreversibly labels α1-adrenaline receptor and exhibits non-competitive antagonist activity. CP59430 can be used for the study of receptor molecular characterization .
|
-
- HY-13716R
-
|
Opioid Receptor
Apoptosis
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier [4] .
|
-
- HY-12826
-
|
Beta-lactamase
Bcl-2 Family
Bacterial
|
Cancer
|
IMB-XH1 is an inhibitor of myeloid cell factor 1 (Mcl-1) . IMB-XH1 is a non-competitive Delhi metallo-β-lactamase (NDM-1) inhibitor. The IC50s of IMB-XH1 against metallo-β-lactamases NDM-1, IMP-4, ImiS and L1 are 0.4637 μM, 3.980 μM, 0.2287 μM and 1.158 μM, respectively .
|
-
- HY-15257
-
AFQ056
|
mGluR
|
Neurological Disease
|
Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease . Mavoglurant 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-N2278
-
Leachianone E
|
Tyrosinase
Glucosidase
|
Cancer
|
Kushenol A (Leachianone E) is isolated from the root of Sophora flavescent. Kushenol A is a non-competitive tyrosinase inhibitor to block the conversion of L-tyrosine to L-DOPA, shows IC50 and Kivalues of 1.1 μM and 0.4 μM, respectively . Kushenol A is a flavonoid antioxidant, has inhibitory effects on alpha-glucosidase (IC50: 45 μM; Ki: 6.8 μM) and β-amylase . Kushenol A is confirmed as potential inhibitors of enzymes targeted by cosmetics for skin whitening and aging .
|
-
- HY-107641
-
α-Cyano-4-hydroxycinnamate
|
Monocarboxylate Transporter
|
Metabolic Disease
|
α-Cyano-4-hydroxycinnamic acid (α-Cyano-4-hydroxycinnamate) is a potent and non-competitive inhibitor of monocarboxylate transporters (MCTs). α-Cyano-4-hydroxycinnamic acid inhibits mitochondrial pyruvate transporter with a Ki of 6.3 μM. α-Cyano-4-hydroxycinnamic acid is used as a matrix to facilitate peptide ionization in matrix-assisted laser desorption/ionization time-of-flight (MALDI-TOF) mass spectrometry applications .
|
-
- HY-108662
-
2,2'-Pyridylisatogen tosylate
|
P2Y Receptor
|
Inflammation/Immunology
|
PIT (2,2'-Pyridylisatogen tosylate) is a selective and non-competitive antagonist of P2Y1 receptor with an IC50 value of 0.14 μM for human P2Y1 receptor. PIT antagonizes P2Y1 receptor signaling without affecting nucleotide binding. PIT is an irreversible antagonist of responses to ATP at metabotropic purinoceptors (of the P2Y family) in some smooth muscles. PIT can be used for the research of chronic bronchitis and asthma .
|
-
- HY-P4160
-
THG113.31; ILGHXDYK
|
Prostaglandin Receptor
|
Endocrinology
|
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
|
-
- HY-17387S1
-
Huperzine A-d4
|
iGluR
Cholinesterase (ChE)
Apoptosis
Isotope-Labeled Compounds
|
Neurological Disease
|
(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
|
-
- HY-17395AR
-
|
Fungal
Bacterial
Antibiotic
|
Infection
|
Terbinafine (Standard) is the analytical standard of Terbinafine. This product is intended for research and analytical applications. Terbinafine (TDT 067) is an orally active and potent antifungal agent. Terbinafine is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine 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-17395R
-
|
Fungal
Bacterial
Antibiotic
|
Infection
|
Terbinafine hydrochloride (Standard) is the analytical standard of Terbinafine hydrochloride. This product is intended for research and analytical applications. Terbinafine hydrochloride (TDT 067 hydrochloride) is an orally active and potent antifungal agent. Terbinafine hydrochloride is a potent non-competitive inhibitor of squalene epoxidase from Candida, with a Ki of 30 nM. Terbinafine hydrochloride also shows antibacterial activity against certain Gram-positive and Gram-negative bacteria . Terbinafine hydrochloride 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-13716S
-
|
Isotope-Labeled Compounds
Apoptosis
Opioid Receptor
|
Cancer
|
Noscapine-13C,d3 is a deuterated labeled Noscapine . Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
|
-
- HY-B0369AR
-
|
iGluR
|
Neurological Disease
|
Orphenadrine (citrate) (Standard) is the analytical standard of Orphenadrine (citrate). This product is intended for research and analytical applications. Orphenadrine citrate is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine citrate relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine citrate is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases .
|
-
- HY-12755
-
CID-2950007
|
Ras
Apoptosis
|
Cancer
|
ML141 (CID-2950007) is a potent, allosteric, selective and reversible non-competitive inhibitor of Cdc42 GTPase. ML141 inhibits Cdc42 wild type and Cdc42 Q61L mutant with EC50s of 2.1 and 2.6 μM, respectively. ML141 shows low micromolar potency and selectivity against other members of the Rho family of GTPases (Rac1, Rab2, Rab7). ML141 do not show cytotoxicity in multiple cell lines .
|
-
- HY-N1860
-
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
3-O-Methylquercetin (3-MQ) is a major component from the plant Rhamnus nakaharai and has antiviral activity and potential antiasthmatic efficacy. 3-O-Methylquercetin inhibits total cAMP and cGMP-phosphodiesterase (PDE). The IC50 values of 3-O-Methylquercetin (3-MQ) against PDE1-PDE5 are in the range of 1.6-86.9 μM. 3-O-Methylquercetin is a non-competitive inhibitor of PDE2 and a competitive inhibitor of PDE4 .
|
-
- HY-17353
-
|
Telomerase
Apoptosis
|
Cancer
|
BIBR 1532 is a potent, selective and non-competitive telomerase inhibitor with IC50 of 100 nM in a cell-free assay.
|
-
- HY-160250
-
|
UGT
|
Metabolic Disease
|
UGT1A1-IN-1 (compound 2) is a non-competitive inhibitor of UGT1A1, which can inhibit the 1-O-glucuronidation process mediated by UGT1A1 with a Ki value of 5.02 μM. UGT1A1-IN-1 (compound 2) can bind on UGT1A1 at the same ligand-binding site as bilirubin (HY-N0323). UGT1A1-IN-1 can serve as a ‘turn-on’ fluorescent probe substrate for UGT1A1 .
|
-
- HY-15410
-
|
iGluR
|
Others
|
Gacyclidine, a non competitive N-methyl-D-aspartate (NMDA) antagonist, can be used in the study of spinal cord injuries .
|
-
- HY-15410A
-
|
iGluR
|
Others
|
Gacyclidine hydrochloride, a non competitive N-methyl-D-aspartate (NMDA) antagonist, can be used in the study of spinal cord injuries .
|
-
- HY-160785
-
|
Others
|
Others
|
TREX1-IN-1 (Compound 180) is a TREX1 inhibitor with an IC50 value for hTREX1 less than 0.1 μM .
|
-
- HY-100513A
-
|
Apoptosis
DNA/RNA Synthesis
Antibiotic
|
Cancer
|
Dehydroaltenusin is a small molecule selective inhibitor of eukaryotic DNA polymerase α, a type of antibiotic produced by a fungus with an IC50 value of 0.68 μM. The inhibitory mode of action of dehydroaltenusin against mammalian pol α activity is competitive with respect to the DNA template primer (Ki=0.23 μM) and non-competitive with respect to the 2'-deoxyribonucleoside 5'-triphosphate substrate (Ki=0.18 μM) . Dehydroaltenusin arrests the cancer cell cycle at the S-phase and triggers apoptosis . Dehydroaltenusin possesses anti-tumor activity against human adenocarcinoma tumor in vivo .
|
-
- HY-P5846
-
MT3
|
mAChR
Adrenergic Receptor
|
Neurological Disease
|
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
|
-
- HY-103490
-
EDHS-206
|
MAP3K
Apoptosis
|
Infection
Inflammation/Immunology
Cancer
|
Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFα stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 μM) .
|
-
- HY-116973
-
|
HIV
|
Infection
|
L-738372 is a non-competitive reversible inhibitor of HIV-1 reverse transcriptase (RT) with an inhibition constant (Ki) of 140 nM against dTTP. When combined with any nucleoside analogs (such as azidothymidine triphosphate, didexoyinosine triphosphate, or didexoycytidine triphosphate), L-738372 exhibits synergistic inhibition of RT activity. L-738372 has 2-3 times more inhibitory potency against the azidothymidine-resistant RT (D67N, K70R, T215Y, K219Q) compared to the wild-type RT. L-738372 holds promise for research in the field of HIV virus treatment .
|
-
- HY-N0226
-
|
Cholinesterase (ChE)
Beta-secretase
|
Neurological Disease
Metabolic Disease
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
|
-
- HY-147711
-
|
Glucosidase
|
Metabolic Disease
|
α-Amylase/α-Glucosidase-IN-1 (compound 33) is a potent α-amylase/α-glucosidase inhibitor with IC50s of 2.01, 2.09 µM for α-amylase and α-glucosidase, respectively. Kinetic studies predict that α-Amylase/α-Glucosidase-IN-1 has the potential of anti hyperglycemia .
|
-
- HY-N0226A
-
|
Cholinesterase (ChE)
Beta-secretase
Reactive Oxygen Species
|
Neurological Disease
Metabolic Disease
|
Epiberberine chloride is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine chloride has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and may protect against Alzheimer disease . Epiberberine chloride inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberine has the potential effect in the research of diabetic disease .
|
-
- HY-103316A
-
Ned 19
2 Publications Verification
|
Calcium Channel
|
Cancer
|
Ned 19 is a selective membrane-permeant non competitive NAADP antagonist and inhibits NAADP-mediated Ca 2+ signaling, with an IC50 of 65 nM . Ned 19 strongly inhibits tumor growth and vascularization as well as lung metastases in mice .
|
-
- HY-B1311
-
SKF-525A; U-5446; RP-5171
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
|
-
- HY-N1386
-
-
- HY-119950
-
-
- HY-115375
-
|
Others
|
Neurological Disease
|
50595 hydrochloride is a selective noncompetitive cisapride antagonist that interferes with the activity of cisapride and BRL 24924. R 50595 hydrochloride has no effect on the response to electrical stimulation at concentrations up to 3 X 10(-7) M. R 50595 hydrochloride antagonizes the effects of cisapride and BRL 24924 in a noncompetitive manner. R 50595 hydrochloride completely abolishes the effects of 5-HT at a concentration of 3 X 10(-7) M and also antagonizes the effects of 5-HT in a noncompetitive manner .
|
-
- HY-B1311R
-
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
Proadifen (hydrochloride) (Standard) is the analytical standard of Proadifen (hydrochloride). This product is intended for research and analytical applications. Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases [4] .
|
-
- HY-P5987
-
Myr-CaMKIINtide
|
CaMK
|
Neurological Disease
|
Calmodulin Kinase IINtide, Myristoylated (Myr-CaMKIINtide) is a selective and noncompetitive inhibitor of CaMKII .
|
-
- HY-111549
-
|
Others
|
Cancer
|
Bragsin1 is a potent, selective and noncompetitive inhibitor of the ArfGEF BRAG2, inhibits Arf GTPase activation, with an IC50 of 3 μM. Bragsin1 binds to PH domain of BRAG2, and is a noncompetitive interfacial inhibitor. Bragsin1 has no effect on the Sec7 domain of human ArfGEFs. Anti-cancer activity .
|
-
- HY-110132
-
-
- HY-P5175
-
|
mAChR
|
Neurological Disease
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
|
-
- HY-168220
-
|
Deubiquitinase
|
Cancer
|
FX-171-C is a noncompetitive Deubiquitinase inhibitor with an IC50 of 1.4 µM .
|
-
- HY-152032
-
|
Histone Demethylase
|
Cancer
|
LSD1-IN-23 is a competitive/non-competitive mixed inhibitor of lysine specific demethylase 1 (LSD1). LSD1-IN-23 has LSD1 inhibitory activity with an IC50 value of 0.58 μM. LSD1-IN-23 can be used for the research of neuroblastoma (NB) .
|
-
- HY-124101
-
|
Histone Methyltransferase
|
Cancer
|
PDAT is a noncompetitive indolethylamine-N-methyltransferase (INMT) inhibitor with a Ki of 84 μM for rabbit lung INMT (rabINMT) .
|
-
- HY-13986
-
VX-497; MMPD
|
Flavivirus
Dengue virus
HBV
HCV
|
Infection
|
Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.
|
-
- HY-102095
-
|
mGluR
|
Neurological Disease
|
SIB-1757 is a highly selective and noncompetitive antagonist of mGlu5 receptor with an IC50 of 0.4 μM .
|
-
- HY-10809
-
RG1678; RO4917838
|
GlyT
|
Neurological Disease
|
Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
|
-
- HY-W015611
-
|
Endogenous Metabolite
|
Metabolic Disease
|
L-(+)-Arabinose selectively inhibits intestinal sucrase activity in a noncompetitive manner and suppresses the plasma glucose increase due to sucrose ingestion.
|
-
- HY-138630
-
-
- HY-146156
-
-
- HY-113261A
-
|
Others
|
Neurological Disease
|
(Rac)-Oleoylcarnitine is an endogenous acylcarnitine and a potential noncompetitive inhibitor of glycine transporter 2 (GLYT2) that can be used as a pain suppressant.
|
-
- HY-164144
-
|
Others
|
Cancer
|
EPZ033294 is an inhibitor of SYMD2 (IC50 is 3.9 nM). SYMD2 itself has catalytic activity and can methylate the lysine residue of BTF3 to BTF3me1, which was experimentally demonstrated by detecting an IC50 of 2.9 nM for inhibition of BTF3ME1 by SYMD2, indicating an active inhibition of SYMD2 by EPZ033294. EPZ033294 (0-50 µM) has an inhibitory effect on SYMD2 and a concentration-dependent inhibitory effect in 293T .
|
-
- HY-N6793
-
|
Microtubule/Tubulin
|
Cancer
|
Phomopsin A is a cyclic hexapeptide mycotoxin isolated from the fungus Phomopsis leptostomiformis. Phomopsin A is a noncompetitive inhibitor of the binding of radiolabeled vincristine to tubulin .
|
-
- HY-103391
-
|
Others
|
Metabolic Disease
|
Qc1 is a reversible and noncompetitive threonine dehydrogenase (TDH) inhibitor. Qc1 can be used for the research of Metabolic disease .
|
-
- HY-129305
-
AHR-9377
|
Serotonin Transporter
|
Neurological Disease
|
Tampramine fumarate is a potent, selective, noncompetitive NE reuptake inhibitor. Tampramine fumarate has antidepressant activity. Tampramine fumarate can be used in research of depression .
|
-
- HY-100356
-
CNS 1102 free base
|
iGluR
|
Neurological Disease
|
Aptiganel (CNS 1102 (free base)), peptide, is a noncompetitive NMDA antagonist with cerebroprotective effects. Aptiganel can be used for the research of stroke .
|
-
- HY-156447
-
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-40 (compound 5) is a noncompetitive α-glucosidase enzyme inhibitor with an IC50 of 24.62 μM .
|
-
- HY-101809
-
CNS 5161A
|
iGluR
|
Cardiovascular Disease
|
CNS-5161 hydrochloride is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
- HY-100792
-
|
Bacterial
|
Cancer
|
URB602 is a selective monoacylglycerol lipase (MGL) inhibitor, which inhibits rat brain MGL with IC50 of 28±4 μM through a noncompetitive mechanism.
|
-
- HY-B1786
-
-
- HY-101809A
-
|
iGluR
|
Cardiovascular Disease
|
CNS-5161 is a novel NMDA ion-channel antagonist that interacts with the NMDA receptor/ion channel site to produce a noncompetitive blockade of the actions of glutamate.
|
-
- HY-169113
-
|
Others
|
Cancer
|
EPZ032597 is a selective and noncompetitive SMYD2 inhibitor with an IC50 value of 16 nM. EPZ032597 is promising for research of pancreatic ductal adenocarcinoma .
|
-
- HY-N3266
-
|
Tyrosinase
|
Cancer
|
Methyl rosmarinate is a noncompetitive tyrosinase inhibitor which is isolated from Rabdosia serra, with an IC50 of 0.28 mM for mushroom tyrosinase, and also inhibits a-glucosidase .
|
-
- HY-N0826
-
-
- HY-N9919
-
|
Others
|
Others
|
Glyasperin C is a potent and reversible noncompetitive inhibitor of neuraminidase with an IC50 of 20% at 200 μM. Glyasperin C is a polyphenol isolated from the roots of Glycyrrhiza uralensis .
|
-
- HY-11095
-
-
- HY-N3394
-
|
Others
|
Infection
|
Lecanoric acid is a histidine-decarboxylase inhibitor isolated from fungus. The inhibition by lecanoric acid is competitive with histidineand noncompetitive with pyridoxal phosphate. Lecanoric acid did not inhibit aromatic amino acid decarboxylase .
|
-
- HY-19363
-
-
- HY-100967
-
Homodimaprit dihydrochloride
|
Histone Methyltransferase
|
Neurological Disease
|
SKF 91488 (Homodimaprit) dihydrochloride is a potent and noncompetitive histamine N-methyltransferase inhibitor with a Ki value of 0.9 microM. SKF 91488 dihydrochloride inhibits the methylation of labeled histamine in mice .
|
-
- HY-16934
-
|
Cholinesterase (ChE)
|
Neurological Disease
|
ML352 is a noncompetitive inhibitor of the presynaptic choline transporter (CHT) with Ki
values of 92 and 166 nM for HEK293 cells expressing human CHT and mouse forebrain synaptosomes, respectively .
|
-
- HY-137673
-
|
Others
|
Others
|
2'-Deoxy-NAD+ is a noncompetitive inhibitor for NAD + with a Ki of 32 μM. 2'-Deoxy-NAD+ can be utilized as a substrate to study the ADP-ribosyl transfer reaction .
|
-
- HY-107781
-
-
- HY-101785
-
-
- HY-B0591
-
|
iGluR
|
Neurological Disease
|
Memantine is an orally active, noncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonist. Memantine can be used for the research of moderate-to-severe Alzheimer's disease (AD) .
|
-
- HY-P1095
-
Caspase-3 Inhibitor VII
|
Caspase
|
Cardiovascular Disease
Neurological Disease
|
Ivachtin (Caspase-3 Inhibitor VII; compound 7a) is a nonpeptide, noncompetitive and reversibl caspase-3 inhibitor with an IC50 of 23 nM. Ivachtin has modest selectivity for the remaining caspases .
|
-
- HY-P1289A
-
|
PKC
|
Others
|
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM .
|
-
- HY-P1289
-
|
PKC
|
Others
|
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM .
|
-
- HY-151151
-
|
Parasite
|
Infection
|
Trypanothione synthetase-IN-3 is a noncompetitive mixed hyperbolic Trypanothione synthetase (TryS) inhibitor (Ki: 0.8 μM). Trypanothione synthetase-IN-3 can be used in the study of parasites, such as L. infantum .
|
-
- HY-107697
-
|
iGluR
|
Neurological Disease
|
N20C hydrochloride is a selective and noncompetitive open NMDA receptor open channel blocker, with micromolar affinity, fast on-off blockade kinetics, and strong voltage dependence. Neuroprotective activity .
|
-
- HY-110278
-
|
mGluR
|
Neurological Disease
|
ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity .
|
-
- HY-P1289C
-
|
PKC
|
Others
|
[Ala113]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM .
|
-
- HY-P1289B
-
|
PKC
|
Others
|
[Ala107]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM .
|
-
- HY-107603
-
|
iGluR
|
Neurological Disease
|
NS3763 is a selective and noncompetitive GLUK5 receptor antagonist with an IC50 of 1.6 µM. NS3763 does not show significant antagonistic properties on GLUK6, AMPA or NMDA receptors .
|
-
- HY-119727
-
|
Ser/Thr Protease
|
Cardiovascular Disease
|
WNK-IN-1 (compound 7) is a ATP noncompetitive With-No-Lysine (WNK) kinase inhibitor (IC50=95 nM). WNK-IN-1 can be used to regulate cardiovascular homeostasis .
|
-
- HY-133732
-
GEA 654 hydrochloride; A03 hydrochloride
|
Serotonin Transporter
5-HT Receptor
iGluR
|
Neurological Disease
|
Alaproclate (GEA 654) hydrochloride is a selective and orally active serotonin re-uptake inhibitor (SSRI). Alaproclate hydrochloride also acts as a potent, reversible and noncompetitive antagonist of the NMDA receptor coupled ion flow .
|
-
- HY-10809A
-
RG1678 (R enantiomer); RO4917838 (R enantiomer)
|
GlyT
|
Neurological Disease
|
Bitopertin R enantiomer (RG1678 R enantiomer; RO4917838 R enantiomer) is the R-enantiomer of Bitopertin. Bitopertin is a potent, noncompetitive glycine reuptake inhibitor, inhibits glycine uptake at human GlyT1 with a concentration exhibiting IC50 of 25 nM.
|
-
- HY-N1425
-
|
Others
|
Metabolic Disease
|
Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2? μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract .
|
-
- HY-139319
-
|
Lactate Dehydrogenase
|
Cancer
|
LDHA-IN-3 (compound 2), as a selenobenzene compound, is a potent, noncompetitive lactate dehydrogenase (LDHA) inhibitor (IC50=145.2 nM). LDHA-IN-3 can be used for the research of cancer .
|
-
- HY-13986A
-
(R)-VX-497; (R)-MMPD
|
Others
|
Infection
|
(R)-Merimepodib is the isomer of Merimepodib (HY-13986), and can be used as an experimental control. Merimepodib (VX-497) is a noncompetitive and oral inhibitor of inosine monophosphate dehydrogenase (IMPDH) with broad spectrum antiviral activities.
|
-
- HY-112535
-
-
- HY-N2394
-
|
Others
|
Inflammation/Immunology
|
Emodin-1-O-β-D-glucopyranoside, isolated from medicinal plant Polygonum cuspidatum Sieb. & Zucc, is a potent and noncompetitive bacterial neuraminidase (BNA) inhibitor with an IC50 of 0.85 μM .
|
-
- HY-101370
-
|
Others
|
Metabolic Disease
|
2-Methylthio-ATP tetrasodium is a non-specific P2-receptor agonist. 2-Methylthio-ATP tetrasodium causes noncompetitive inhibition of ADP-induced human platelet aggregation .
|
-
- HY-119591
-
|
GABA Receptor
|
Neurological Disease
|
BPDBA is a selective and noncompetitive betaine/GABA transporter (BGT-1) inhibitor with IC50s of 20 μM and 35 μM against human BGT-1 and mouse GAT2, respectively .
|
-
- HY-15187
-
ARRY-520
|
Kinesin
Apoptosis
|
Cancer
|
Filanesib (ARRY-520) is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-137067
-
IMT1B
5 Publications Verification
LDC203974
|
DNA/RNA Synthesis
|
Cancer
|
IMT1B (LDC203974) is an orally active, noncompetitive and specific allosteric inhibitor of mitochondrial RNA polymerase (POLRMT) and inhibits mitochondrial DNA (mtDNA) expression. IMT1B has anti-tumour effects .
|
-
- HY-B1786S
-
cis-Sulindac sulfide-d3
|
γ-secretase
|
Neurological Disease
|
Sulindac sulfide-d3 is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
|
-
- HY-W015611R
-
|
Endogenous Metabolite
|
Metabolic Disease
|
L-(+)-Arabinose (Standard) is the analytical standard of L-(+)-Arabinose. This product is intended for research and analytical applications. L-(+)-Arabinose selectively inhibits intestinal sucrase activity in a noncompetitive manner and suppresses the plasma glucose increase due to sucrose ingestion.
|
-
- HY-B0157AS
-
-
- HY-B1395
-
|
nAChR
Histamine Receptor
|
Cardiovascular Disease
Neurological Disease
|
Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
|
-
- HY-B1395A
-
|
nAChR
Histamine Receptor
|
Cardiovascular Disease
Neurological Disease
|
Mecamylamine is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine is also a ganglionic blocker. Mecamylamine can across the blood-brain barrier. Mecamylamine can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
|
-
- HY-103567
-
|
mGluR
|
Neurological Disease
|
Desmethyl-YM-298198 hydrochloride is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 hydrochloride has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
|
-
- HY-103567A
-
|
mGluR
|
Neurological Disease
|
Desmethyl-YM-298198 is a high-affinity, selective, and noncompetitive mGluR1 antagonist (IC50: 16 nM). Desmethyl-YM-298198 has analgesic effect in Streptozotocin (HY-13753)-induced hyperalgesic mice .
|
-
- HY-110237
-
|
P2X Receptor
Calcium Channel
|
Cardiovascular Disease
|
BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
|
-
- HY-15187C
-
ARRY-520 hydrochloride
|
Kinesin
Apoptosis
|
Neurological Disease
|
Filanesib (ARRY-520) hydrochloride is a selective and noncompetitive kinesin spindle protein (KSP) inhibitor, with an IC50 of 6 nM for human KSP. Filanesib induces cell death by apoptosis in vitro. Filanesib has potent anti-proliferative activity .
|
-
- HY-106818A
-
AJ-2615
|
Acyltransferase
Calcium Channel
|
Cardiovascular Disease
Metabolic Disease
|
Monatepil maleate (AJ-2615) is a potent and orally active Ca 2+-channel antagonist and a noncompetitive ACAT inhibitor. Monatepil maleate decreases blood pressure and improves plasma lipid metabolism. Monatepil maleate has the potential for the research of hyperlipidemia .
|
-
- HY-N0826R
-
-
- HY-110067
-
-
- HY-154964
-
|
RSV
|
Infection
|
RSV L-protein-IN-2 (Compound A) is a noncompetitive RSV polymerase inhibitor (IC50: 4.5 μM). RSV L-protein-IN-2 shows antiviral activity against long RSV strains (EC50: 1.3 μM) .
|
-
- HY-154967
-
|
RSV
|
Infection
|
RSV L-protein-IN-4 (Compound C) is a noncompetitive RSV polymerase inhibitor (IC50: 0.88 μM). RSV L-protein-IN-4 shows antiviral activity against RSV strains (EC50: 0.25 μM) .
|
-
- HY-B1786R
-
|
Drug Metabolite
γ-secretase
|
Neurological Disease
|
Sulindac sulfide (Standard) is the analytical standard of Sulindac sulfide. This product is intended for research and analytical applications. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
|
-
- HY-113786
-
|
Histone Methyltransferase
|
Cancer
|
EZH2-IN-21 is a potent inhibitor of the histone lysine methyltransferase enhancer of zeste homologue 2 (EZH2) with anticancer activity. EZH2-IN-21 is competitive with the cofactor SAM and noncompetitive with peptide or nucleosome substrates .
|
-
- HY-B0591S
-
|
Isotope-Labeled Compounds
iGluR
|
Neurological Disease
|
Memantine-d3 (hydrochloride) is deuterium labeled Memantine. Memantine is an orally active, noncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonist. Memantine can be used for the research of moderate-to-severe Alzheimer's disease (AD)[1][2][3].
|
-
- HY-100405
-
|
mGluR
|
Neurological Disease
|
FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1 .
|
-
- HY-156659
-
|
Phosphatase
|
Others
|
NC1 is a noncompetitive and allosteric lymphoid-specific tyrosine phosphatase (LYP) inhibitor, with a Ki value 4.3 μM. NC1 inhibits LYP by restricting the movement of the WPD-loop. NC1 inhibits LYP-mediated TCR signaling in T cells .
|
-
- HY-15185
-
PF-3084014
|
γ-secretase
Apoptosis
|
Cancer
|
Nirogacestat (PF-3084014) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
|
-
- HY-B0438
-
|
Bacterial
Antibiotic
|
Infection
|
Spectinomycin dihydrochloride is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM - .
|
-
- HY-B1494
-
|
Chloride Channel
GABA Receptor
|
Neurological Disease
|
Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM .
|
-
- HY-B1828
-
|
Antibiotic
Bacterial
|
Infection
|
Spectinomycin is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin is also a noncompetitive inhibitor of td intron RNA .
|
-
- HY-137673A
-
|
Others
|
Others
|
2'-Deoxy-NAD+ sodium is the sodium salt form of 2'-Deoxy-NAD+ (HY-137673). 2'-Deoxy-NAD+ sodium is a noncompetitive inhibitor of NAD+ with a Ki of 32 μM. 2'-Deoxy-NAD+ sodium can be used as a substrate to study ADP-ribosyl transfer reactions.
|
-
- HY-124957
-
|
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
β-NETA is a potent and noncompetitive choline acetyltransferase (ChA; IC50=76 μM) and cholinesterase (ChE; IC50=40 µM) inhibitor. β-NETA weakly inhibits acetylcholinesterase (AChE; IC50=1 mM) .
|
-
- HY-110036
-
-
- HY-120901
-
|
SHP2
|
Cancer
|
II-B08 is a reversible and noncompetitive SHP2 inhibitor (IC50: 5.5 μM, 15.7, 14.3 μM for SHP2, SHP1, PTP1B). II-B08 can be used for cancer research .
|
-
- HY-B0569
-
|
nAChR
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
Hexamethonium Bromide is a non-selective ganglionic nicotinic-receptor antagonist (nAChR) antagonist, with mixed competitive and noncompetitive activity. Hexamethonium Bromide has anti-hypertensive activity. Hexamethonium Bromide attenuates sympathetic activity and blood pressure in spontaneously hypertensive animal models .
|
-
- HY-108341
-
|
Acyltransferase
|
Metabolic Disease
|
PF-06424439 is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
- HY-135976
-
|
P2X Receptor
|
Neurological Disease
Inflammation/Immunology
|
P2X3 antagonist 34 is a potent, selective and orally active P2X3 homotrimeric receptor antagonist with IC50s of 25 nM, 92 nM and 126 nM for human P2X3, rat P2X3 and guinea pig P2X3 receptors, respectively. P2X3 antagonist 34 is less active against human, rat and guinea pig P2X2/3 heterotrimeric receptors. P2X3 antagonist 34 has strong anti-tussive effect .
|
-
- HY-B1828A
-
Spectinomycin hydrochloride hydrate
|
Bacterial
Antibiotic
|
Infection
|
Spectinomycin dihydrochloride pentahydrate is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride pentahydrate acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride pentahydrate is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM - .
|
-
- HY-15185B
-
PF-3084014 dihydrobromide; PF-03084014 dihydrobromide
|
γ-secretase
Apoptosis
|
Cancer
|
Nirogacestat dihydrobromide (PF-3084014 dihydrobromide) is a reversible, orally bioavailable, noncompetitive, and selective γ-secretase inhibitor with an IC50 of 6.2 nM. Inhibition of Notch signaling by Nirogacestat dihydrobromide while minimizing gastrointestinal toxicity presents a promising approach for research of Notch receptor-dependent cancers .
|
-
- HY-110036A
-
L768242 hydrochloride
|
Cannabinoid Receptor
|
Neurological Disease
|
GW-405833 (L768242) hydrochloride is a potent, selective cannabinoid receptor 2 (CB2) agonist with an EC50 of 50.7 nM. GW-405833 hydrochloride also behaves as a noncompetitive CB1 antagonist. GW-405833 hydrochloride suppresses inflammatory and neuropathic pain .
|
-
- HY-N1425R
-
|
Others
|
Metabolic Disease
|
Tiliroside (Standard) is the analytical standard of Tiliroside. This product is intended for research and analytical applications. Tiliroside, a glycosidic flavonoid, possesses anti-diabetic activities. Tiliroside is a noncompetitive inhibitor of α-amylase with a Ki value of 84.2? μM. Tiliroside inhibits carbohydrate digestion and glucose absorption in the gastrointestinal tract .
|
-
- HY-W928617
-
|
Antibiotic
Bacterial
|
Infection
|
Spectinomycin sulfate hydrate is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin sulfate hydrate acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin sulfate hydrate is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM - .
|
-
- HY-103392
-
BCX2600
|
Cytochrome P450
|
Neurological Disease
|
Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively.
|
-
- HY-103234A
-
|
iGluR
|
Neurological Disease
|
GYKI 52466 dihydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 dihydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 dihydrochloride can be used in Parkinson's disease research .
|
-
- HY-108341A
-
|
Acyltransferase
|
Metabolic Disease
|
PF-06424439 methanesulfonate is an oral, potent and selective imidazopyridine diacylglycerol acyltransferase 2 (DGAT2) inhibitor with an IC50 of 14 nM . PF-06424439 methanesulfonate is slowly reversible, time-dependent inhibitor, which inhibits DGAT2 in a noncompetitive mode with respect to the acyl-CoA substrate .
|
-
- HY-103374
-
(-)-Eseroline phenylcarbamate; (-)-Phenserine
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
Phenserine ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine improves cognitive performance and attenuates the progression of Alzheimer's disease .
|
-
- HY-139134
-
-
- HY-103234
-
|
iGluR
|
Neurological Disease
|
GYKI 52466 is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 can be used in Parkinson's disease research .
|
-
- HY-107509
-
|
mGluR
|
Neurological Disease
|
LY2389575 hydrochloride is a selective and noncompetitive mGlu3 negative allosteric modulator (NAM), with an IC50 value of 190 nM. LY2389575 hydrochloride induces an increase in Mrc1 levels. LY2389575 hydrochloride also independently amplifies Amyloid beta (Aβ) toxicity and can be used in study of Alzheimer's disease .
|
-
- HY-103234B
-
|
iGluR
|
Neurological Disease
|
GYKI 52466 hydrochloride is an orally active, highly selective and noncompetitive AMPA/kainate receptor antagonist with the IC50 values of 7.5 and 11μM, respectively. GYKI 52466 hydrochloride has good blood brain barrier permeability and anticonvulsant effect. GYKI 52466 hydrochloride can be used in Parkinson's disease research .
|
-
- HY-106697
-
ICI 128436
|
Aldose Reductase
|
Metabolic Disease
|
Ponalrestat (ICI 128436) is an orally active, selective and noncompetitive aldose reductase (AKR1B1; ALR) inhibitor. Ponalrestat selectively inhibits ALR2 (Ki=7.7 nM) over ALR1 (Ki=60 μM). Ponalrestat inhibits the conversion of glucose to sorbitol .
|
-
- HY-P99191
-
NI-0501
|
IFNAR
|
Inflammation/Immunology
|
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
|
-
- HY-B1558A
-
MCI-2016
|
Monoamine Oxidase
|
Neurological Disease
|
Bifemelane hydrochloride (MCI-2016) is a potent, selective and competitive inhibitor of monoamine oxidase A (MAO-A), with a Ki of 4.20 μM. Bifemelane hydrochloride also inhibits MAO-B noncompetitively with a Ki of 46.0 μM. Bifemelane hydrochloride has a potent antidepressant activity and can be used for the research of cognitive and emotional disturbances related to cerebrovascular disease .
|
-
- HY-125296
-
|
GABA Receptor
|
Neurological Disease
|
Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
|
-
- HY-B1395R
-
|
nAChR
Histamine Receptor
|
Cardiovascular Disease
Neurological Disease
|
Mecamylamine (hydrochloride) (Standard) is the analytical standard of Mecamylamine (hydrochloride). This product is intended for research and analytical applications. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist. Mecamylamine hydrochloride is also a ganglionic blocker. Mecamylamine hydrochloride can across the blood-brain barrier. Mecamylamine hydrochloride can be used in the research of neuropsychiatric disorders, hypertension, antidepressant area .
|
-
- HY-B0986
-
4-Hexylresorcinol
|
Parasite
Bacterial
Apoptosis
Glucosidase
Endogenous Metabolite
|
Infection
Metabolic Disease
Cancer
|
Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage .
|
-
- HY-N0319
-
|
Cytochrome P450
|
Cancer
|
Salvianolic acid C is a noncompetitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2), with Kis of 4.82 μM and 5.75 μM for CYP2C8 and CYP2J2, respectively.
|
-
- HY-111550
-
|
Others
|
Cancer
|
Bragsin2 is a potent, selective and noncompetitive nucleotide exchange factor BRAG2 inhibitor, with an IC50 of 3 μM. Bragsin2 binds at the interface between the PH domain of BRAG2 and the lipid bilayer, leads BRAG2 unable to activate lipidated Arf GTPase. Bragsin2 affects breast cancer stem cells .
|
-
- HY-18663B
-
|
iGluR
|
Neurological Disease
|
CP-465022 hydrochloride is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes .
|
-
- HY-W062216
-
|
Bacterial
Arginase
|
Infection
|
2-Aminoimidazole is a potent antibiofilm agent that can be used as an adjuvant to antimicrobial. 2-aminoimidazoles disrupts the ability of bacteria to protect themselves by inhibiting biofilm formation and genetically-encoded antibiotic resistance traits. 2-Aminoimidazole is also a weak noncompetitive inhibitor of human arginase I with a Ki of 3.6 mM .
|
-
- HY-43913
-
|
Eukaryotic Initiation Factor (eIF)
|
Others
|
(R)-eIF4A3-IN-2 is a less active enantiomer of eIF4A3-IN-2. eIF4A3-IN-2 is a highly selective and noncompetitive eukaryotic initiation factor 4A-3 (eIF4A3) inhibitor with an IC50 of 110 nM .
|
-
- HY-18663A
-
|
iGluR
|
Neurological Disease
|
CP-465022 Maleate is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes .
|
-
- HY-18663
-
|
iGluR
|
Neurological Disease
|
CP-465022 is a potent, and selective noncompetitive AMPA receptor antagonist with anticonvulsant activity. CP-465022 is against Kainate-induced response with an IC50 of 25 nM in rat cortical neurons. CP-465022 provides a new tool to investigate the role of AMPA receptors in physiological and pathophysiological processes .
|
-
- HY-103374A
-
(-)-Eseroline phenylcarbamate tartrate; (-)-Phenserine (+)-tartrate
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
Phenserine tartrate ((-)-Eseroline phenylcarbamate) is a derivative of Physostigmine and is a potent, noncompetitive, long-acting and selective AChE inhibitor. Phenserine tartrate reduces β-amyloid precursor protein (APP) and β-amyloid peptide (Aβ) formation. Phenserine tartrate improves cognitive performance and attenuates the progression of Alzheimer's disease .
|
-
- HY-100815
-
|
Others
|
Neurological Disease
|
(R)-AMPA is an inactive AMPA receptor ligand that inhibits the release of excitatory amino acids from neurons. (R)-AMPA is inactive in experiments that enhance the release of [3H]D-aspartate induced by electrical stimulation. (R)-AMPA is inhibited by competitive and noncompetitive AMPA receptor selective antagonists in response to AMPA and glutamate .
|
-
- HY-118091
-
|
5 alpha Reductase
|
Endocrinology
|
LY191704, as a benzoquinolinone, is a potent, nonsteroidal, noncompetitive and selective human type I 5α-reductase inhibitor. LY191704 is a racemic mixture of the compounds LY300502 and LY300503. LY191704 may be useful in the research of human endocrine disorders associated with overproduction of dihydrotestosterone (DHT) by 5α-reductase type 1 .
|
-
- HY-132189
-
|
P-glycoprotein
|
Cancer
|
Laniquidar (R101933) is a noncompetitive, third generation P-glycoprotein (P-gp) inhibitor with an IC50 of 0.51 μM. Laniquidar can be used for modulating multidrug resistance transporters . Laniquidar can also be used for studying acute myeloid leukemia (AML) and myelodysplastic syndrome (MDS) . Laniquidar has limited oral bioavailability .
|
-
- HY-114234A
-
|
Beta-secretase
|
Neurological Disease
|
TAK-070 Free base is a noncompetitive and orally active BACE1 inhibitor (IC50: 3.15 μM). TAK-070 Free base can be used for research of Alzheimer’s disease (AD). TAK-070 Free base inhibits brain levels of soluble Aβ, and improves cognitive impairments in AD model .
|
-
- HY-B1494R
-
|
Chloride Channel
GABA Receptor
|
Neurological Disease
|
Picrotoxinin (Standard) is the analytical standard of Picrotoxinin. This product is intended for research and analytical applications. Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors. Picrotoxinin inhibits α1β2γ2L GABAA receptor with an IC50 of 1.15 μM .
|
-
- HY-B1395S1
-
|
Isotope-Labeled Compounds
nAChR
|
Neurological Disease
|
Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
|
-
- HY-117370
-
AZ1
|
Deubiquitinase
|
Cancer
|
USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model .
|
-
- HY-162073
-
|
Influenza Virus
|
Infection
|
ZIKV-IN-8 (Compound 9b) is a noncompetitive Zika virus (ZIKV) inhibitor. ZIKV-IN-8 shows the best anti-ZIKV activity with a selectivity index of 22.4. ZIKV-IN-8 has significant inhibition of ZIKV with an IC50 value of 25.6 μM. ZIKV-IN-8 can be used for the research of ZIKV infection .
|
-
- HY-103713
-
SP-2577
|
Histone Demethylase
|
Cancer
|
Seclidemstat is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat can be used for the research of Ewing Sarcoma .
|
-
- HY-103392S
-
|
Isotope-Labeled Compounds
Cytochrome P450
|
Neurological Disease
|
Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
|
-
- HY-N1029
-
Mangiferitin
|
Glucosidase
PPAR
|
Infection
Inflammation/Immunology
Cancer
|
Norathyriol (Mangiferitin) is a natural metabolite of Mangifera. Norathyriol inhibits α-glucosidase in a noncompetitive manner with an IC50 of 3.12 μM . Norathyriol inhibits PPARα, PPARβ, and PPARγ with IC50s of 92.8 µM, 102.4 µM, and 153.5 µM, respectively . Antioxidant, anticancer, antimicrobial, anti-inflammatory, anti-bacterial activities.
|
-
- HY-139451
-
|
Others
|
Neurological Disease
|
ELOVL6-IN-1 is a potent, orally active and selective ELOVL6 inhibitor. ELOVL6-IN-1 dose-dependently inhibits mouse ELOVL6 activities, with an IC50 value of 0.350 μM. ELOVL6-IN-1 inhibits ELOVL6 in a noncompetitive manner for malonyl-CoA (Ki=994 nM) and palmitoyl-CoA .
|
-
- HY-A0016
-
SR 33589
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4 .
|
-
- HY-13290
-
|
CaMK
P2X Receptor
|
Metabolic Disease
Cancer
|
KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
|
-
- HY-14609
-
|
mGluR
|
Neurological Disease
|
MPEP Hydrochloride is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP Hydrochloride has anxiolytic-or antidepressant-like effects . MPEP (Hydrochloride) 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-14609A
-
MPEP
3 Publications Verification
|
mGluR
|
Neurological Disease
|
MPEP is a potent, selective, noncompetitive, orally active and systemically active mGlu5 receptor antagonist, with an IC50 of 36 nM for completely inhibiting quisqualate-stimulated phosphoinositide (PI) hydrolysis. MPEP has anxiolytic-or antidepressant-like effects . MPEP 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-N1430
-
trans-Oxyresveratrol
|
Tyrosinase
HSV
Autophagy
|
Others
|
Oxyresveratrol (trans-Oxyresveratrol) is a potent naturally occurring antioxidant and free radical scavenger (IC50 of 28.9 μM against DPPH free radicals). Oxyresveratrol is potent and noncompetitive tyrosinase inhibitor with an IC50 value of 1.2 μM for mushroom tyrosinase. Oxyresveratrol is effective against HSV-1, HSV-2 and varicella-zoster virus, and has neuroprotective effects .
|
-
- HY-136650
-
F-ara-ATP
|
Nucleoside Antimetabolite/Analog
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Fludarabine triphosphate (F-ara-ATP), the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis .
|
-
- HY-B1828AR
-
Spectinomycin hydrochloride hydrate (Standard)
|
Bacterial
Antibiotic
|
Infection
|
Spectinomycin (dihydrochloride pentahydrate) (Standard) is the analytical standard of Spectinomycin (dihydrochloride pentahydrate). This product is intended for research and analytical applications. Spectinomycin dihydrochloride pentahydrate is a broad-spectrum antibiotic and inhibits the growth of a variety of gram-positive and gram-negative organisms. Spectinomycin dihydrochloride pentahydrate acts by selectively targeting to the bacterial ribosome and interrupting protein synthesis. Spectinomycin dihydrochloride pentahydrate is also a noncompetitive inhibitor of td intron RNA with an Ki value of 7.2 mM - .
|
-
- HY-P1259
-
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-103713A
-
SP-2577 mesylate
|
Histone Demethylase
|
Cancer
|
Seclidemstat (SP-2577) mesylate is a potent noncompetitive and reversible KDM1A (LSD1) inhibitor (Ki=31 nM, IC50=13 nM). Seclidemstat mesylate promotes antitumor immunity in switch/sucrose nonfermentable (SWI/SNF) complex mutated ovarian cancer, as well as inhibit virus production, viral DNA replication, and late gene expression. Seclidemstat mesylate can be used for the research of Ewing Sarcoma .
|
-
- HY-144396
-
|
SHP2
Phosphatase
Akt
Apoptosis
|
Cancer
|
SHP2-IN-8 is a highly potent, selective, and cellularly active allosteric SHP2 inhibitor with IC50 value of 23 nM and Ki of 22 nM. SHP2-IN-8 is reversible and noncompetitive. SHP2-IN-8 causes a significant thermal shift with the ΔTm of 7.01 ℃. SHP2-IN-8 induces the apoptosis and inhibits the phosphorylation of AKT in Hela cells .
|
-
- HY-136650A
-
F-ara-ATP trisodium
|
Nucleoside Antimetabolite/Analog
Drug Metabolite
DNA/RNA Synthesis
Apoptosis
|
Cancer
|
Fludarabine triphosphate (F-ara-ATP) trisodium, the active metabolite of Fludarabine (HY-B0069), is a potent, noncompetitive and specific inhibitor of DNA primase, with an IC50 of 2.3 μM and a Ki of 6.1 μM. Fludarabine triphosphate trisodium inhibits DNA synthesis by blocking DNA primase and primer RNA formation. Fludarabine triphosphate trisodium inhibits ribonucleotide reductase and DNA polymerase and ultimately leads to cellular apoptosis .
|
-
- HY-B0986R
-
|
Parasite
Bacterial
Apoptosis
Glucosidase
Endogenous Metabolite
|
Infection
Metabolic Disease
Cancer
|
Hexylresorcinol (Standard) is the analytical standard of Hexylresorcinol. This product is intended for research and analytical applications. Hexylresorcinol (4-Hexylresorcinol) is a natural compound found in plants with antimicrobial, anthelmintic, antiseptic and antitumor activities. Hexylresorcinol can induce apoptosis in squamous carcinoma cells. Hexylresorcinol is a reversible and noncompetitive inhibitor of α-glucosidase. Hexylresorcinol has protective effects against oxidative DNA damage .
|
-
- HY-125296R
-
|
GABA Receptor
|
Neurological Disease
|
Fipronil sulfone (Standard) is the analytical standard of Fipronil sulfone. This product is intended for research and analytical applications. Fipronil sulfone is the major metabolite of Fipronil.Fipronil sulfone selectively inhibits GABA receptor with IC50 of 175 nM (assayed by displacement of 4′-ethynyl-4-n-[2,3-3H2]- propylbicycloorthobenzoate ([3H]EBOB) from the noncompetitive blocker site).
|
-
- HY-B0157A
-
HC 20511 fumarate
|
Histamine Receptor
Endogenous Metabolite
SARS-CoV
Influenza Virus
|
Inflammation/Immunology
Endocrinology
Cancer
|
Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .
|
-
- HY-12895
-
SKI V
1 Publications Verification
|
SphK
PI3K
Apoptosis
|
Cancer
|
SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity .
|
-
- HY-P1259A
-
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-134539
-
IMT1
3 Publications Verification
|
Oxidative Phosphorylation
Mitochondrial Metabolism
DNA/RNA Synthesis
|
Metabolic Disease
Cancer
|
IMT1 is a first-in-class specific and noncompetitive human mitochondrial RNA polymerase (POLRMT) inhibitor. IMT1 causes a conformational change of POLRMT, which blocks substrate binding and transcription in a dose-dependent way in vitro. IMT1 reduces deoxynucleoside triphosphate levels and citric acid cycle intermediates, resulting in a marked depletion of cellular amino acid levels. IMT1 has the potential for mitochondrial transcription disorders related diseases .
|
-
- HY-144267
-
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
Metabolic Disease
|
Glucosylceramide synthase-IN-2 (compound T-690) is a potent, brain-penetrant and orally active glucosylceramide synthase (GCS) inhibitor with IC50s of 15 nM and 190 nM for human GCS and mouse GCS, respectively.Glucosylceramide synthase-IN-2 exhibits noncompetitive type inhibition with C8-ceramide and UDP-glucose.Glucosylceramide synthase-IN-2 can be used for Gaucher's disease research .
|
-
- HY-145827
-
|
Microtubule/Tubulin
|
Cancer
|
KIF18A-IN-4 is a moderately potent ATP and microtubule (MT) noncompetitive KIF18A inhibitor (IC50=6.16 μM). KIF18A-IN-4 has selectivity against a large panel of mitotic kinesins and kinases, and does not show any direct effects on tubulin assembly. KIF18A-IN-4 exhibits anti-tumor activity .
|
-
- HY-B0157
-
-
- HY-N0319R
-
|
Cytochrome P450
|
Cancer
|
Salvianolic acid C (Standard) is the analytical standard of Salvianolic acid C. This product is intended for research and analytical applications. Salvianolic acid C is a noncompetitive Cytochrome P4502C8 (CYP2C8) inhibitor and a moderate mixed inhibitor of Cytochrome P45022J2 (CYP2J2), with Kis of 4.82 μM and 5.75 μM for CYP2C8 and CYP2J2, respectively.
|
-
- HY-N4110R
-
|
Cytochrome P450
|
Metabolic Disease
|
Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54? μM and 18.02 μM, respectively .
|
-
- HY-118175
-
|
Others
|
Others
|
RG 14921, a compound structurally related to erbstatin, was investigated for its mechanism of inhibition of epidermal growth factor (EGF) receptor tyrosine kinase and CAMP-dependent kinase activity by kinetic analysis. Both compounds are slow-binding inhibitors of EGF receptor kinase. Erbstatin inhibits EGF receptor kinase as a partially competitive inhibitor relative to ATP and peptide substrates, suggesting that it binds at different positions in the enzyme's ATP- and peptide substrate-binding sites, thereby reducing the enzyme's binding affinity for both substrates. In contrast, the derivative RG 14921 inhibits EGF receptor kinase activity as a noncompetitive inhibitor relative to ATP and peptide substrates. Structurally related compounds exhibit different modes of inhibition, suggesting that the catalytic center of the receptor kinase domain may have a dynamic and possibly extended structure. Erbstatin and RG 14921 exerted similar effects on CAMP-dependent protein kinase activity. In this system, both compounds exhibited strong inhibition and acted in a competitive inhibition manner with ATP and a noncompetitive inhibition manner with peptide substrates.
|
-
- HY-107711
-
|
iGluR
|
Neurological Disease
|
DQP-1105 is a potent noncompetitive NMDA receptor antagonist. DQP-1105 inhibits GluN2C- and GluN2D-containing receptors (IC50=7.0 and 2.7 μM, respectively). The IC50 values are at least 50-fold lower than those for recombinant GluN2A-, GluN2B-, GluA1-, or GluK2-containing receptors .
|
-
- HY-A0016S
-
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4[1][2][3][4].
|
-
- HY-N1483
-
|
Potassium Channel
|
Cardiovascular Disease
|
Guanfu base A is an antiarrhythmic alkaloid isolated from Aconitum coreanum and is a potent noncompetitive CYP2D6 inhibitor, with a Ki of 1.20 μM in human liver microsomes (HLMs) and a Ki of 0.37 μM for the human recombinant form (rCYP2D6). Guanfu base A is also a potent competitive inhibitor of CYP2D in monkey (Ki of 0.38 μM) and dog (Ki of 2.4 μM) microsomes . Guanfu base A also inhibits HERG channel current .
|
-
- HY-128358
-
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 µM .
|
-
- HY-100386
-
PCR 5332
|
Cytochrome P450
|
Cardiovascular Disease
|
Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
|
-
- HY-156078
-
|
Glucosidase
|
Metabolic Disease
|
α-Glucosidase-IN-32 (compound f26) is a reversible, noncompetitive and orally active α-glucosidase inhibitor with an IC50 value of 3.07 μM. α-Glucosidase-IN-32 complex with α-glucosidase through hydrogen bonds and hydrophobic interactions, led to changes in the conformation and secondary strictures of α-glucosidase and further the inhibition of the enzymatic activity. α-Glucosidase-IN-32 can be used for diabetic disease research .
|
-
- HY-A0016R
-
|
mAChR
Sodium Channel
Calcium Channel
Adrenergic Receptor
Cytochrome P450
Autophagy
|
Cardiovascular Disease
|
Dronedarone (Standard) is the analytical standard of Dronedarone. This product is intended for research and analytical applications. Dronedarone (SR 33589), a derivative of amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone is a substrate for and a moderate inhibitor of CYP3A4 .
|
-
- HY-N1430R
-
|
Tyrosinase
HSV
Autophagy
|
Others
|
Oxyresveratrol (Standard) is the analytical standard of Oxyresveratrol. This product is intended for research and analytical applications. Oxyresveratrol (trans-Oxyresveratrol) is a potent naturally occurring antioxidant and free radical scavenger (IC50 of 28.9 μM against DPPH free radicals). Oxyresveratrol is potent and noncompetitive tyrosinase inhibitor with an IC50 value of 1.2 μM for mushroom tyrosinase. Oxyresveratrol is effective against HSV-1, HSV-2 and varicella-zoster virus, and has neuroprotective effects .
|
-
- HY-13207
-
PR-957
|
Proteasome
Bacterial
HIV
|
Infection
Inflammation/Immunology
|
ONX-0914 (PR-957) is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
|
-
- HY-13560
-
AVN-944
4 Publications Verification
VX-944
|
Arenavirus
DNA/RNA Synthesis
Apoptosis
Caspase
Bcl-2 Family
|
Infection
Cancer
|
AVN-944 (VX-944) is an orally active, potent, selective, noncompetitive and specific inhibitor of IMPDH (inosine monophosphate dehydrogenase). AVN-944 is an essential rate-limiting enzyme in de novo guanine nucleotide synthesis. AVN-944 is also an inhibitor of arenavirus RNA synthesis, and blocks arenavirus infection. AVN-944 has broad anti-cancer activities, and can be used for multiple myeloma (MM) and acute myeloid leukemia (AML) research .
|
-
- HY-129636A
-
GABAB receptor antagonist 1
|
GABA Receptor
ERK
|
Neurological Disease
|
(E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
|
-
- HY-138097
-
|
Chemerin Receptor
Aldehyde Dehydrogenase (ALDH)
Cholinesterase (ChE)
Apoptosis
|
Cancer
|
α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC50 of 9 μM. α-NETA is a potent ALDH1A1 (IC50=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC50=84 µM) and acetylcholinesterase (AChE; IC50=300 µM). α-NETA has anti-cancer activity .
|
-
- HY-P5876
-
ProADM N20(bovine, porcine); PAMP-20(bovine, porcine)
|
nAChR
|
Neurological Disease
|
Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a potent and noncompetitive hypotensive and catecholamine release-inhibitory peptide released from chromaffin cells. Proadrenomedullin (N-20) (bovine, porcine) inhibits catecholamine secretion with an IC50 of 350 nM in PC12 pheochromocytoma cells. Proadrenomedullin (N-20) (bovine, porcine) also blocks (EC50≈270 nM) nicotinic cholinergic agonist desensitization of catecholamine release, as well as desensitization of nicotinic signal transduction ( 22Na + uptake) .
|
-
- HY-B0157AR
-
|
Histamine Receptor
Endogenous Metabolite
SARS-CoV
Influenza Virus
|
Inflammation/Immunology
Endocrinology
Cancer
|
Ketotifen (fumarate) (Standard) is the analytical standard of Ketotifen (fumarate). This product is intended for research and analytical applications. Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .
|
-
- HY-13207A
-
PR-957 TFA
|
Proteasome
Bacterial
HIV
|
Infection
Inflammation/Immunology
|
ONX-0914 (PR-957) TFA is a selective inhibitor of low-molecular mass polypeptide-7 (LMP7), the chymotrypsin-like subunit of the immunoproteasome. ONX-0914 TFA blocks cytokine production and attenuates progression of experimental arthritis. ONX-0914 TFA is a noncompetitive irreversible inhibitor of the mycobacterial proteasome (Ki=5.2 μM). ONX-0914 TFA reactivates latent HIV-1 through p-TEFb activation mediated by HSF-1 .
|
-
- HY-118814
-
|
Others
|
Neurological Disease
|
YM928 is an orally active and noncompetitive α-Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) receptor antagonist. YM928 inhibits AMPA receptor-mediated toxicity in primary rat hippocampal cultures with an IC50 value of 2 μM. YM928 blocks AMPA-induced intracellular calcium influx with an IC50 value of 3 μM and antagonizes AMPA-induced inward currents with an IC50 value of 1 μM. YM928 is promising for research of neurological disorders .
|
-
- HY-12882A
-
|
iGluR
Potassium Channel
|
Neurological Disease
|
Ifenprodil tartrate is a typical noncompetitive NMDA receptor antagonist. Ifenprodil tartrate exerts high affinity at NR1A/NR2B receptors (IC50=0.34 μM) over 400-fold than at NR1A/NR2A receptors (IC50=146 μM) . Ifenprodil tartrate inhibits GIRK (Kir3), reduces inward currents through the basal GIRK activity. Ifenprodil tartrate has the potential to be a cerebral vasodilator .
|
-
- HY-100386S
-
PCR 5332-d4
|
Isotope-Labeled Compounds
Cytochrome P450
|
Cardiovascular Disease
|
Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
|
-
- HY-112345
-
|
FGFR
PDGFR
EGFR
Src
|
Cancer
|
PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC50s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC50=0.18 µM). PD-089828 also inhibits MAPK with an IC50 of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity .
|
-
- HY-150260
-
|
Bacterial
|
Infection
|
SA09-Cu is a noncompetitive and potent NDM-1 inhibitor with an IC50 of 9.6 nM. SA09-Cu can convert NDM-1 into an inactive state by oxidizing the Zn(II)-thiolate site of the enzyme and avoids to be reduced by intracellular thiols of bacteria. SA09-Cu exhibits excellent inhibition against a series of clinical NDM-1-producing carbapenem-resistant Enterobacteriaceae (CRE) in restoring the Meropenem (HY-13678) effect, and slows down the development of carbapenem resistance .
|
-
- HY-107513
-
|
mGluR
|
Neurological Disease
Cancer
|
BAY 36-7620 is a potent and noncompetitive antagonist of mGlu1 Receptor (IC50=0.16 μM) with inverse agonist activity. BAY 36-7620 inhibits tumor growth and prolongs the survival of mice with tumors by inhibiting mGlu1 receptor. BAY 36-7620 suppresses AKT phosphorylation in A549 tumors. BAY 36-762 has neuroprotective effect in acute subdural hematoma rat model.BAY 36-7620 is used in non-small cell lung cancer and breast cancer research .
|
-
- HY-100386R
-
|
Cytochrome P450
|
Cardiovascular Disease
|
Ticlopidine (Standard) is the analytical standard of Ticlopidine. This product is intended for research and analytical applications. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively.
|
-
- HY-N7536
-
|
TRP Channel
|
Others
|
Voacangine is an antagonist for TRPV1 and TRPM8 but as an agonist for TRPA1 (EC50=8 μM). Voacangine competitively blockes capsaicin binding to TRPV1 (IC50=50 μM). Voacangine competitively inhibits the binding of menthol to TRPM8 (IC50=9 μM) and it shows noncompetitive inhibition against icilin (IC50=7 μM). Voacangine selectively abrogates chemical agonist-induced TRPM8 activation and did not affect cold-induced activation. Voacangine is an alkaloid isolated from the root bark of Voacanga africana .
|
-
- HY-P5158
-
|
Adrenergic Receptor
|
Others
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
-
- HY-100401A
-
CS-505
|
Acyltransferase
|
Cardiovascular Disease
|
Pactimibe sulfate (CS-505) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe sulfate (CS-505) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe sulfate (CS-505) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe sulfate (CS-505) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe sulfate (CS-505) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
|
-
- HY-100401
-
CS-505 free base
|
Acyltransferase
|
Cardiovascular Disease
|
Pactimibe (CS-505 free base) is a dual ACAT1/2 inhibitor with IC50s of 4.9 μM and 3.0 μM, respectively. Pactimibe (CS-505 free base) inhibits ACAT with IC50s of 2.0 μM, 2.7 μM, 4.7 μM in the liver, macrophages and THP-1 cells, respectively . Pactimibe (CS-505 free base) noncompetitively inhibits oleoyl-CoA with a Ki value of 5.6 μM. Moreover, Pactimibe (CS-505 free base) obviously inhibits cholesteryl ester formation with an IC50 of 6.7 μM. Pactimibe (CS-505 free base) possesses anti-atherosclerotic potential with lowering plasma cholesterol activity .
|
-
- HY-P2200
-
BMY-29304
|
HIV
Antibiotic
|
Infection
Inflammation/Immunology
|
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
|
-
- HY-155238
-
|
GABA Receptor
|
Neurological Disease
|
E2730 is a noncompetitive but selective inhibitor of gamma-aminobutyric acid (GABA) transporter 1 (GAT1) with orally available and antiepileptic activity. E2730-mediated GAT1 inhibition is positively correlated with environmental GABA levels and selectively inhibits GAT1-mediated GABA uptake. E2730 (5-50 mg/kg; po) in rat amygdala ignition model, and in mouse cornea ignition (5-50 mg/kg), drug resistance 6Hz-44mA has demonstrated in vivo efficacy in models of psychomotor epilepsy (5-50 mg/kg), fragile X syndrome (2.5-300 mg/kg), and Dravet syndrome (10 mg/kg, 20 mg/kg) .
|
-
- HY-12031B
-
|
Others
|
Inflammation/Immunology
|
(2Z,3Z)-U0126 is a selective inhibitor of MEK1 and MEK2, demonstrating potent antiinflammatory effects by noncompetitively inhibiting AP-1 transcriptional activity with IC50 values of 72 nM for MEK1 and 58 nM for MEK2. (2Z,3Z)-U0126 also inhibits anchorage-independent growth of Ki-ras-transformed rat fibroblasts by blocking both the extracellular signal-regulated kinase and mammalian target of rapamycin pathways. Additionally, (2Z,3Z)-U0126 can undergo isomerization and cyclization, resulting in various products that show reduced affinity for MEK and diminished AP-1 inhibition compared to the parent compound.
|
-
- HY-151096
-
|
CXCR
|
Inflammation/Immunology
|
ACT-660602 is an orally active antagonist of chemokine receptor (CXCR3) with an IC50 value of 204 nM. ACT-660602 inhibits T-cell migration and shows efficacy in acute lung ingury model. ACT-660602 can be used for autoimmune diseases research .
|
-
- HY-162633
-
|
Deubiquitinase
|
Cancer
|
USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer .
|
-
- HY-N2735
-
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA) inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitory activities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
|
-
- HY-12882
-
RC 61-91; NP-120
|
Others
|
Neurological Disease
|
Ifenprodil (RC 61-91) is a noncompetitive NMDA receptor antagonist with anti-excitotoxic activity. Ifenprodil significantly improves long-term sensorimotor and spatial learning deficits in mice after acute subarachnoid hemorrhage. Ifenprodil reduces neuronal cell death in the basal cortex and CA1 region of the hippocampus induced by experimental subarachnoid hemorrhage. Ifenprodil attenuates Ca2+ overload in basal cortical cells and mitochondria, as well as brain edema in blood-brain barrier damage and early brain injury. Ifenprodil reduces the intracellular Ca2+ increase and apoptosis of primary cortical neurons under conditions of high glutamate concentrations. Ifenprodil also reduces the increase in endothelial permeability caused by high glutamate concentrations in human brain microvascular endothelial cells. Ifenprodil also inhibits GIRK channels and interacts with α1-adrenergic, 5-HT, and σ receptors .
|
-
Cat. No. |
Product Name |
Type |
-
- HY-15908
-
BCA
5 Publications Verification
Disodium bicinchoninate
|
Biochemical Assay Reagents
|
BCA (Disodium bicinchoninate) is an orally active and non-competitive Beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitor with an IC50 value of 28 µM, a Ki value of 43 µM. BCA shows anticancer activity. BCA has the potential for the research of Alzheimer's disease (AD) .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1271
-
|
nAChR
|
Cardiovascular Disease
|
Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-P1271A
-
|
nAChR
|
Cardiovascular Disease
|
Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
|
-
- HY-P1178
-
|
Trk Receptor
|
Neurological Disease
|
Cyclotraxin B, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-P4160
-
THG113.31; ILGHXDYK
|
Prostaglandin Receptor
|
Endocrinology
|
PDC31 (THG113.31; ILGHXDYK) is an allosteric and non-competitive inhibitor of FP Prostaglandin Receptor. PDC31 is the D-amino acid-based oligopeptide, is used for smooth muscle contractile agent. PDC31 decreases the strength and duration of uterine contractions in vivo, which can be used for research of preterm labor and primary dysmenorrhea (PD). PDC31 also enhances Ca 2+-dependent large-conductance K +-channel in human myometrial cells .
|
-
- HY-P1178A
-
|
Trk Receptor
|
Neurological Disease
|
Cyclotraxin B TFA, a cyclic peptide, is a highly potent and selective TrkB inhibitor without altering the binding of BDNF. Cyclotraxin B TFA non-competitively inhibits BDNF-induced TrkB activity with an IC50 of 0.30 nM. Cyclotraxin B TFA can crosse the blood-brain-barrier and has analgesic and anxiolytic-like behavioral effects .
|
-
- HY-P10571
-
|
Melanocortin Receptor
|
Endocrinology
|
GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
|
-
- HY-P5846
-
MT3
|
mAChR
Adrenergic Receptor
|
Neurological Disease
|
Muscarinic toxin 3 (MT3) is a potent and non-competitive mAChR and adrenoceptors antagonist with pIC50s of 6.71, 8.79, 8.86, 7.57, 8.13, 8.49, <6.5, 7.29 against M1, M4, α1A, α1B, α1D,α2A,α2B and α2C receptors, respectively. Muscarinic toxin 3 displays prominent adrenoceptor activity .
|
-
- HY-P5987
-
Myr-CaMKIINtide
|
CaMK
|
Neurological Disease
|
Calmodulin Kinase IINtide, Myristoylated (Myr-CaMKIINtide) is a selective and noncompetitive inhibitor of CaMKII .
|
-
- HY-P5175
-
|
mAChR
|
Neurological Disease
|
Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
|
-
- HY-P1289A
-
|
PKC
|
Others
|
[Ala107]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM .
|
-
- HY-P1289
-
|
PKC
|
Others
|
[Ala113]MBP(104-118) is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM .
|
-
- HY-P1289C
-
|
PKC
|
Others
|
[Ala113]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 28-62 μM .
|
-
- HY-P1289B
-
|
PKC
|
Others
|
[Ala107]MBP(104-118) TFA is an noncompetitive peptide inhibitors of protein kinase C (PKC), with IC50s ranging from 46-145 μM .
|
-
- HY-P1831
-
ProAM N20, Human; PAMP-20, human
|
Peptides
|
Neurological Disease
|
Proadrenomedullin (1-20), human is a potent hypotensive and catecholamine release–inhibitory peptide released from chromaffin cells with an IC50 of ~350 nM for catecholamine secretion in PC12 pheochromocytoma cells, acting in a noncompetitive manner specifically at the nicotinic cholinergic receptor .
|
-
- HY-P1259
-
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-P1259A
-
|
Proteasome
Bacterial
|
Inflammation/Immunology
|
PR-39 TFA, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 TFAreversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 TFA stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
|
-
- HY-P5876
-
ProADM N20(bovine, porcine); PAMP-20(bovine, porcine)
|
nAChR
|
Neurological Disease
|
Proadrenomedullin (N-20) (ProADM N20) (bovine, porcine) is a potent and noncompetitive hypotensive and catecholamine release-inhibitory peptide released from chromaffin cells. Proadrenomedullin (N-20) (bovine, porcine) inhibits catecholamine secretion with an IC50 of 350 nM in PC12 pheochromocytoma cells. Proadrenomedullin (N-20) (bovine, porcine) also blocks (EC50≈270 nM) nicotinic cholinergic agonist desensitization of catecholamine release, as well as desensitization of nicotinic signal transduction ( 22Na + uptake) .
|
-
- HY-P5158
-
|
Adrenergic Receptor
|
Others
|
Conopeptide rho-TIA is a peptide derived from the venom contained in the predatory sea snail Conus tulipa, has highly selective and noncompetitive inhibitor at human α1B-Adrenergic Receptor. Conopeptide rho-TIA acts a competitive inhibitor at human α1A-Adrenergic Receptor and α1D-Adrenergic Receptor. Conopeptide rho-TIA binds to each subtype and may provide useful information for the development of novel α1-Adrenergic Receptor subtype-selective drugs .
|
-
- HY-P2200
-
BMY-29304
|
HIV
Antibiotic
|
Infection
Inflammation/Immunology
|
Siamycin I (BMY-29304), a 21-residue tricyclic peptide, is a secondary metabolite in actinomycetes. Siamycin I is a HIV fusion inhibitor with ED50s of 0.05 to 5.7 μM for acute HIV type 1 (HIV-1) and HIV-2 infections. Siamycin I inhibits the gelatinase and gelatinase biosynthesis-activating pheromone (GBAP) signaling via the FsrC-FsrA two-component regulatory system in a noncompetitive manner. Siamycin I suppresses the expression of both fsrBDC and gelE-sprE transcripts. Siamycin I, a lasso peptide, interacts with lipid II and inhibits cell wall biosynthesis. Siamycin I, an antibiotic, has the potential for enterococcal infections research .
|
Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99191
-
NI-0501
|
IFNAR
|
Inflammation/Immunology
|
Emapalumab (NI-0501) is a human monoclonal IgG1 antibody that noncompetitively inhibits IFN-γ. Emapalumab binds with high affinity (Kd= 1.4 pM) to both free IFN-γ as well as IFN-γ bound to its receptor. Emapalumab can be used in research of hemophagocytic lymphohistiocytosis (HLH) .
|
Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-W010510
-
-
-
- HY-Y0504
-
-
-
- HY-W015309
-
-
-
- HY-N1470
-
-
-
- HY-N0235
-
-
-
- HY-N12427
-
-
-
- HY-117672
-
-
-
- HY-W015309R
-
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
-
- HY-B0199A
-
-
-
- HY-W010510R
-
-
-
- HY-N2197
-
-
-
- HY-N6054
-
-
-
- HY-N12736
-
-
-
- HY-Y0504R
-
-
-
- HY-N6650
-
-
-
- HY-N0235R
-
|
Structural Classification
Monophenols
Leguminosae
Source classification
Phenols
Psoralea corylifolia L.
Plants
|
Carboxylesterase
p38 MAPK
Autophagy
UGT
|
Bakuchiol (Standard) is the analytical standard of Bakuchiol. This product is intended for research and analytical applications. Bakuchiol is a phytoestrogen that can be obtained from psoralen seeds. Bakuchiol has been proven to be a non-competitive inhibitor of multiple enzymes, including UDP-glucuronosyltransferase 2B7 (UGT2B7) and human carboxylesterase 2 (hCE2) , with IC50s values of 40.9 μM and 7.28 μM, respectively. Bakuchiol exhibits significant research and application potential in areas such as anti-inflammatory , antibacterial , antitumor therapies, as well as drug metabolism regulation.
|
-
-
- HY-N10488
-
-
-
- HY-W727627
-
-
-
- HY-N3090
-
-
-
- HY-N2463
-
-
-
- HY-N9506
-
-
-
- HY-N4193
-
-
-
- HY-N7377
-
-
-
- HY-N10489
-
-
-
- HY-N6054R
-
-
-
- HY-129137
-
Cy 3-soph
|
Rosaceae
Plants
Prunus cerasus L.
|
Others
|
Cyanidin 3-sophoroside chloride is a potent non-competitive reversible polyphenol oxidase (PPO) inhibitor. Also, Cyanidin 3-sophoroside chloride can be used as an anti-browning agent to inhibit the degree of PPO browning, enhance the antioxidant damage capacity of fruits and prolong the storage period .
|
-
-
- HY-114203
-
-
-
- HY-N3136
-
-
-
- HY-N1919
-
-
-
- HY-N1919A
-
-
-
- HY-N12761
-
-
-
- HY-N10096
-
-
-
- HY-N12688
-
-
-
- HY-17387
-
-
-
- HY-N0063
-
-
-
- HY-N1919R
-
-
-
- HY-13716
-
-
-
- HY-N0241
-
-
-
- HY-N4110
-
-
-
- HY-N0063R
-
|
Structural Classification
Punica granatum L.
Source classification
Phenols
Polyphenols
Punicaceae
Plants
|
SARS-CoV
HBV
|
Punicalagin (Standard) is the analytical standard of Punicalagin. This product is intended for research and analytical applications. Punicalagin is a polyphenol ingredient isolated from Pomegranate (Punica granatum L.) or the leaves of Terminalia catappa L.. Punicalagin is a reversible and non-competitive 3CLpro inhibitor and inhibits SARS-CoV-2 replication in vitro. Punicalagin is an anti-hepatitis B virus (HBV) agent and has antioxidant, anti-inflammatory, and anticancer effects. Punicalagin has the potential for the research of COVID-19 .
|
-
-
- HY-13716R
-
|
Structural Classification
Alkaloids
Source classification
Quinoline Alkaloids
Papaver somniferum Linn.
Plants
Papaveraceae
|
Opioid Receptor
Apoptosis
|
Noscapine (Standard) is the analytical standard of Noscapine. This product is intended for research and analytical applications. Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier [4] .
|
-
-
- HY-N2278
-
-
-
- HY-N1860
-
-
-
- HY-100513A
-
-
-
- HY-N0226
-
|
Alkaloids
Source classification
Ranunculaceae
Coptis chinensis Franch.
Plants
Isoquinoline Alkaloids
|
Cholinesterase (ChE)
Beta-secretase
|
Epiberberine is an alkaloid isolated from Coptis chinensis, acts as a potent AChE and BChE inhibitor, and a non-competitive BACE1 inhibitor, with IC50s of 1.07, 6.03 and 8.55 μM, respectively. Epiberberine has antioxidant activity, with peroxynitrite ONOO - scavenging effect (IC50, 16.83 μM), and can be used for the research of Alzheimer disease . Epiberberine inhibits the early stage of differentiation of 3T3-L1 preadipocytes, downregulates the Raf/MEK1/2/ERK1/2 and AMPKα/Akt pathways . Epiberberinecan be used for the research of diabetic disease .
|
-
-
- HY-N0226A
-
-
-
- HY-N1386
-
-
-
- HY-W015611
-
-
-
- HY-113261A
-
|
Microorganisms
Source classification
|
Others
|
(Rac)-Oleoylcarnitine is an endogenous acylcarnitine and a potential noncompetitive inhibitor of glycine transporter 2 (GLYT2) that can be used as a pain suppressant.
|
-
-
- HY-N6793
-
-
- HY-N3266
-
-
- HY-N0826
-
-
- HY-N9919
-
-
- HY-N3394
-
-
- HY-N1425
-
-
- HY-N2394
-
-
- HY-W015611R
-
-
- HY-N0826R
-
-
- HY-B0438
-
-
- HY-B1494
-
-
- HY-N1425R
-
-
- HY-B0986
-
-
- HY-N0319
-
-
- HY-W062216
-
-
- HY-B1494R
-
-
- HY-N1029
-
-
- HY-N1430
-
-
- HY-B0986R
-
-
- HY-B0157A
-
-
- HY-B0157
-
-
- HY-N0319R
-
-
- HY-N4110R
-
|
Structural Classification
Natural Products
Celastraceae
Maytenus ilicifolia
Plants
|
Cytochrome P450
|
Friedelin (Standard) is the analytical standard of Friedelin. This product is intended for research and analytical applications. Friedelin is isolated from isolated from the leaves of Maytenus ilicifolia(Mart). Friedelin is a noncompetitive inhibitor of CYP3A4 with IC50 and Kivalues of 10.79 ?μM and 6.16? μM, respectively. Friedelin is also a competitive inhibitor of CYP2E1 with IC50 and Ki values of 22.54? μM and 18.02 μM, respectively .
|
-
- HY-N1483
-
-
- HY-N1430R
-
|
Structural Classification
other families
Stilbenes
Source classification
Phenols
Polyphenols
Plants
|
Tyrosinase
HSV
Autophagy
|
Oxyresveratrol (Standard) is the analytical standard of Oxyresveratrol. This product is intended for research and analytical applications. Oxyresveratrol (trans-Oxyresveratrol) is a potent naturally occurring antioxidant and free radical scavenger (IC50 of 28.9 μM against DPPH free radicals). Oxyresveratrol is potent and noncompetitive tyrosinase inhibitor with an IC50 value of 1.2 μM for mushroom tyrosinase. Oxyresveratrol is effective against HSV-1, HSV-2 and varicella-zoster virus, and has neuroprotective effects .
|
-
- HY-B0157AR
-
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Histamine Receptor
Endogenous Metabolite
SARS-CoV
Influenza Virus
|
Ketotifen (fumarate) (Standard) is the analytical standard of Ketotifen (fumarate). This product is intended for research and analytical applications. Ketotifen (HC 20-511) fumarate is an orally active second-generation noncompetitive histamine 1 (H1) receptor blocker and mast cell stabilizer. Ketotifen fumarate can block 6-phosphogluconate dehydrogenase (PGD) in vitro. Ketotifen fumarate also has antiviral activity against SARS-CoV-2 and Influenza virus. Ketotifen fumarate can be used to the research of autoimmune encephalomyelitis (EAE) and asthma attack prevention .
|
-
- HY-12882A
-
-
- HY-N7536
-
-
- HY-N2735
-
|
Structural Classification
Leguminosae
Caesalpinia sappan L.
Source classification
Phenols
Polyphenols
Plants
|
Influenza Virus
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7,3',4'-Trihydroxy-3-benzyl-2H-chromene is an reversible noncompetitive neuraminidase (NA) inhibitor. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be isolated from the dried heartwood of Caesalpinia sappan L. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene has potent NAs inhibitory activities with IC50 values of 34.6 µM [H1N1], 39.5 µM [H3N2], and 50.5µM [H9N2], respectively. 7,3',4'-Trihydroxy-3-benzyl-2H-chromene can be used for the research of influenza virus .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-W015309S
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Decanoic acid-d3 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-W015309S1
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Decanoic acid-d199 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-W015309S3
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Decanoic acid-d5 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-17395S
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Terbinafine-d3 (hydrochloride) is the deuterium labeled Terbinafine hydrochloride. Terbinafine hydrochloride (TDT 067 hydrochloride) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine hydrochloride also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
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- HY-12542S
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Dantrolene- 13C3 is the 13C3 labeled Dantrolene. Dantrolene (F368), a muscle relaxant, non-competitively inhibits human erythrocyte glutathione reductase. Ki and IC50 values are 111.6 μM and 52.3 μM, respectively. Dantrolene is a ryanodine receptor antagonist and Ca2+ signaling stabilizer. Dantrolene can be used for the research of muscle spasticity, malignant hyperthermia, Huntington's disease and other neuroleptic malignant syndrome.
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- HY-W015309S2
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Decanoic acid-d2 is the deuterium labeled Decanoic acid. Decanoic acid, a component of medium chain triclycerides, is a brain-penetrant and non-competitive inhibitor of AMPA receptor. Decanoic acid has antiseizure effects[1][2][3].
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- HY-B0199AS
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Mycophenolate Mofetil-d4 hydrochloride is deuterated labeled Mycophenolate mofetil hydrochloride (HY-B0199A). Mycophenolate mofetil (RS 61443) hydrochloride is a immunosuppressant, a non-competitive, selective and reversible inhibitor of inosine monophosphate dehydrogenase (IMPD) type I/II with IC50s of 39 nM and 27 nM, respectively.
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- HY-17395AS
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Terbinafine-d7 is the deuterium labeled Terbinafine. Terbinafine (TDT 067) is an antifungal medication used to treat fungal infections. It is a potent non-competitive inhibitor of squalene epoxidase from Candida with a Ki of 30 nM[1][2]. Terbinafine also antibacterial activity against certain Gram-positive and Gram-negative bacteria[3].
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- HY-B0091S
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Adapalene-d3 is the deuterium labeled Adapalene. Adapalene (CD271), a third-generation synthetic retinoid, is widely used for the research of acne. Adapalene is a potent RAR agonist, with AC50s of 2.3 nM, 9.3 nM, and 22 nM for RARβ, RARγ, RARα, respectively. Adapalene also inhibits the enzymatic activity of GOT1 in a non-competitive manner. Adapalene exhibits anti-tumor activity[1][2][3].
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- HY-B1126S
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Orphenadrine-d3 (hydrochloride) is the deuterium labeled Orphenadrine hydrochloride[1]. Orphenadrine hydrochloride is an orally active and non-competitive NMDA receptor antagonist (crosses the blood-brain barrier) with a Ki of 6.0 μM. Orphenadrine hydrochloride relieves stiffness, pain and discomfort due to muscle strains, sprains or other injuries. Orphenadrine hydrochloride is also used to relieve tremors associated with parkinson's disease. Orphenadrine citrate has good neuroprotective properties, can be used in studies of neurodegenerative diseases[2][3].
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- HY-17387S1
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(-)-Huperzine A-d4 hydrochloride is deuterated labeled (-)-Huperzine A (HY-17387). (-)-Huperzine A (Huperzine A) is an alkaloid isolated from Huperzia serrata, with neuroprotective activity. (-)-Huperzine A is a potent, highly specific, reversible and blood-brain barrier penetrant inhibitor of acetylcholinesterase (AChE), with an IC50 of 82 nM. (-)-Huperzine A also is non-competitive antagonist of N-methyl-D-aspartate glutamate (NMDA) receptor. (-)-Huperzine A is developed for the research of neurodegenerative diseases, including Alzheimer’s disease .
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- HY-13716S
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Noscapine-13C,d3 is a deuterated labeled Noscapine . Noscapine ((S,R)-Noscapine) is an orally active phthalideisoquinoline alkaloid with potent antitussive. Noscapine exerts its antitussive effects by activating sigma opioid receptors and is a non-competitive Bradykinin inhibitor. Noscapine disrupts microtubule dynamics, induces mitotic arrest and apoptosis. Noscapine possesses anticancer, neuroprotective, anti-inflammatory activities, and can cross the blood-brain barrier .
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- HY-B1786S
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Sulindac sulfide-d3 is deuterium labeled Sulindac sulfide. Sulindac sulfide is a noncompetitive γ-secretase inhibitor, with an IC50 of 20.2 μM for γ42-secretase activity.
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- HY-B0157AS
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Ketotifen-d3 (fumarate) is the deuterium labeled Ketotifen fumarate. Ketotifen (HC 20511) fumarate is a second-generation noncompetitive H1-antihistamine and mast cell stabilizer, which is used to prevent asthma attacks[1][2].
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- HY-B0591S
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Memantine-d3 (hydrochloride) is deuterium labeled Memantine. Memantine is an orally active, noncompetitive N-methyl-D-aspartate receptor (NMDAR) antagonist. Memantine can be used for the research of moderate-to-severe Alzheimer's disease (AD)[1][2][3].
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- HY-B1395S1
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Mecamylamine (hydrochloride)- 13C4, 15N is the 13C-labeled and 15N-labeled Mecamylamine hydrochloride. Mecamylamine hydrochloride is an orally active, nonselective, noncompetitive nAChR antagonist that can treat various neuropsychiatric disorders. Mecamylamine hydrochloride is originally used as a ganglionic blocker in treating hypertension. Mecamylamine hydrochloride can easily crosses the blood-brain barrier[1][2].
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- HY-103392S
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Stiripentol-d9 is the deuterium labeled Stiripentol. Stiripentol (STP) is an anticonvulsant agent, which can inhibit N-demethylation of CLB to NCLB mediatated by CYP3A4 (noncompetitively) and CYP2C19 (competitively) with Ki of 1.59±0.07 and 0.516±0.065 μM and IC50 of 1.58 and 3.29 μM, respectively[1][2].
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- HY-A0016S
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Dronedarone-d6 (hydrochloride) is the deuterium labeled Dronedarone. Dronedarone hydrochloride, a derivative of Amiodarone (HY-14187), is a class III antiarrhythmic agent for the study of atrial fibrillation (AF) and atrial flutter. Dronedarone hydrochloride is a potent blocker of multiple ion currents, including potassium current, sodium current, and L-type calcium current, and exhibits antiadrenergic effects by noncompetitive binding to β-adrenergic receptors. Dronedarone hydrochloride is a substrate for and a moderate inhibitor of CYP3A4[1][2][3][4].
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- HY-100386S
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Ticlopidine-d4 is the deuterium labeled Ticlopidine. Ticlopidine (PCR 5332), an antithrombotic proagent, acts as an allosteric, noncompetitive inhibitor of CD39 with the IC50 of 81.7 μM. Ticlopidine blocks several NTPDase isoenzymes with IC50s of 170 μM and 149 μM for NTPDase2 and NTPDase3, respectively[1]. Ticlopidine is an inhibitor of CYP2C19 human liver cytochrome. Ticlopidine inhibits CYP2C9 and CYP3A4 with IC50s of 26.0 and 32.3 μM, respectively[2][3].
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Cat. No. |
Product Name |
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Classification |
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- HY-123311
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Azide
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CP59430 is an azide analog of the α-adrenaline receptor antagonist Prazosin (HY-B0193). P59430 behaves as a competitive antagonist of α1-adrenaline receptor before photolysis. After photolysis, it specifically and irreversibly labels α1-adrenaline receptor and exhibits non-competitive antagonist activity. CP59430 can be used for the study of receptor molecular characterization .
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Cat. No. |
Product Name |
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Classification |
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- HY-13859
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L-FMAU
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Nucleosides and their Analogs
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Clevudine (L-FMAU), a nucleoside analog of the unnatural L-configuration, has potent anti-HBV activity with long half-life, low toxicity. Clevudine is a non-competitive inhibitor that is not incorporated into the viral DNA but rather binds to the polymerase. Clevudine is active against cowpox virus respiratory infection in mice .
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