Search Result
Results for "
inactivation inhibitor
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
8
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
-
- HY-121954
-
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Nec-1 (inactive control)
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Others
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Cancer
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Necrostatin-1 (Nec-1) (inactive control) is an inactive analog of Necrostatin-1 (HY-15760). Necrostatin-1 is a potent necroptosis inhibitor .
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-
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- HY-107657
-
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Myosin
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Others
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(+)-Blebbistatin is the inactive enantiomer of (–)-Blebbistatin. (–)-Blebbistatin is a selective inhibitor of myosin II ATPase .
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-
-
- HY-135846
-
-
-
- HY-120343
-
-
-
- HY-132926
-
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MAP4K
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Cancer
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HPK1-IN-8 is an allosteric, inactive conformation-selective inhibitor of full-length HPK1.
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-
-
- HY-148745
-
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HSP
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Cancer
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JG-258 is an inactive negative control for Hsp70 inhibitors .
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-
-
- HY-112382
-
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Others
|
Others
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Iso-olomoucine is an inactive stereoisomer of the CDK5 inhibitor olomoucine with IC50 >1 mM .
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-
-
- HY-139890
-
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Src
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Others
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DC-Srci-6649 is a c-Src kinase inhibitor that inhibits the phosphorylation and locks c-Src in the inactive state.
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-
-
- HY-113894
-
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Aurora Kinase
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Cancer
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Retreversine is an inactive control for Reversine. Reversine is a novel class of ATP-competitive Aurora kinase inhibitor .
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-
-
- HY-111744
-
|
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Others
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Metabolic Disease
|
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Deacetylanisomycin is a potent growth regulator in plants and an inactive derivative of Anisomycin. Anisomycin is a potent protein synthesis inhibitor .
|
-
-
- HY-16560B
-
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(R)-Campathecin; (R)-(+)-Camptothecin; (R)-CPT
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Others
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Others
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(R)-Camptothecin is an enantiomer of Camptothecin (CPT), is inactive as an inhibitor of the DNA religation reaction and consequently do not poison Top1 .
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-
-
- HY-100815
-
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iGluR
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Neurological Disease
|
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(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 .
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-
-
- HY-78131B
-
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(R)-Ibuprofen
|
NF-κB
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Inflammation/Immunology
Cancer
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(R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
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-
-
- HY-U00459A
-
|
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IRE1
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Others
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GSK2850163 S enantiomer is the inactive enantiomer of GSK2850163. GSK2850163 is an inositol-requiring enzyme-1 alpha (IRE1a) inhibitor.
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-
-
- HY-145081
-
|
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Others
|
Infection
|
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Pitnot-2 is an inactive analog of clathrin inhibitor Pitstop 2. Pitnot-2 can be used as negative control .
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-
-
- HY-130658
-
|
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Others
|
Metabolic Disease
|
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D-NMMA acetate is an inactive isomer of L-NMMA (HY-18732A). L-NMMA is a nitric oxide synthase inhibitor .
|
-
-
- HY-A0256
-
|
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Beta-lactamase
Antibiotic
Bacterial
|
Infection
Inflammation/Immunology
|
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Clavulanic acid is a naturally occurring powerful bacterial β-lactamases inhibitor for research of infections caused by bacteria, including infections of the ears. Clavulanic acid is active against a wide spectrum of gram-positive and gram-negative bacterias .
|
-
-
- HY-90009C
-
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ent-IC-351
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Phosphodiesterase (PDE)
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Cancer
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ent-Tadalafil (ent-IC-351), compound (6S,12aS), is a inactive cis-enantiomer of compound (6R,12aS). compound (6R,12aS) is a potent PDE5 inhibitor with an IC50 of 0.090 μM, while ent-Tadalafil is inactive at concentrations up to 10 µM .
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-
-
- HY-111176
-
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3-Phenyl-2-sulfanylpropanoic acid
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Others
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Others
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PD 145305 (3-Phenyl-2-sulfanylpropanoic acid) is an inactive analogue of PD150606. PD150606 is a selective calpain inhibitor .
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-
-
- HY-118202
-
|
(-)-Methoxyverapamil
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Others
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Cardiovascular Disease
|
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(-)-Gallopamil exerts a selective modulation of the fast voltage-dependent inactivation. (-)-Gallopamil inhibits efficiently Cav1.2 constructs formed by β-subunits (promoting fast voltage-dependent inactivation). (-)-Gallopamil also accelerates the voltage-dependent phase of ICa decay (as well as the voltage-dependent decay of Ba 2+ currents). (-)-Gallopamil is promising for research of antiarrhythmics .
|
-
-
- HY-118202A
-
|
(-)-Methoxyverapamil hydrochloride
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Others
|
Cardiovascular Disease
|
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(-)-Gallopamil (hydrochloride) exerts a selective modulation of the fast voltage-dependent inactivation. (-)-Gallopamil (hydrochloride) inhibits efficiently Cav1.2 constructs formed by β-subunits (promoting fast voltage-dependent inactivation). (-)-Gallopamil (hydrochloride) also accelerates the voltage-dependent phase of ICa decay (as well as the voltage-dependent decay of Ba 2+ currents). (-)-Gallopamil (hydrochloride) is promising for research of antiarrhythmics .
|
-
-
- HY-14347
-
|
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Others
|
Cancer
|
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EBE-A22 is a derivative of PD 153035 which can inhibit ErbB-1-phosphorylation, whereas EBE-A22 is inactive.
|
-
-
- HY-134673B
-
|
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METTL3
|
Others
|
|
UZH1b is an enantiomer of UZH1a (a METTL3 inhibitor). UZH1b is essentially inactive for METTL3 (IC50=28 µM) .
|
-
-
- HY-19714
-
XY1
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
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XY1 is an analog of SGC707 (SGC707 is a potent, selective PRMT3 inhibitor with an IC50 value of 31 nM), but XY1 is completely inactive against PRMT3.
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-
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- HY-18563
-
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HCV
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Infection
|
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4-Phenoxybenzylamine inhibits the function of the NS3 protein by stabilizing an inactive conformation with an IC50 of about 500 μM against FL NS3/4a.
|
-
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- HY-137117
-
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15-keto Prostaglandin E1
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Drug Metabolite
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Others
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15-keto-PGE1 is an inactive Prostaglandin E1 (PGE1) metabolite. Prostaglandin E1 induces vasodilation and inhibits platelet aggregation .
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-
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- HY-107477
-
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Epigenetic Reader Domain
|
Cancer
|
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GSK8573 is an inactive control compound for GSK2801 (acetyl-lysine competitive inhibitor of BAZ2A and BAZ2B bromodomains). GSK8573 has binding activity to BRD9 with a Kd value of 1.04 μM and is inactive against BAZ2A/B and other bromodomain familiy. GSK8573 can be used as a structurally related negative control compound in biological experiments .
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-
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- HY-118421
-
|
|
Parasite
HDAC
|
Infection
|
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Nullscript is a negative control for Scriptaid. Nullscript is a known inactive analog of Scriptaid . Scriptaid is a representative HDAC inhibitor . Nullscript inhibits Cryptosporidium (C. parvum) growth with the IC50 value of 2.1 μM .
|
-
-
- HY-15159
-
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Polo-like Kinase (PLK)
|
Cancer
|
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Cyclapolin 9 is a potent, selective and ATP-competitive polo-like kinase 1 (PLK1) inhibitor with an IC50 of 500 nM. Cyclapolin 9 is inactive against other kinases .
|
-
-
- HY-132203
-
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RIP kinase
|
Inflammation/Immunology
Cancer
|
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Necrostatin-34 (Nec-34), a RIPK1 kinase inhibitor, stabilizes RIPK1 kinase in an inactive conformation by occupying a distinct binding pocket in the kinase domain .
|
-
-
- HY-161955
-
|
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TMV
|
Infection
|
|
TMV-IN-11 (compound syn-3g) is a potent TMV inhibitor with high inactivation capacity (IC50: 120.7 μg/mL). TMV-IN-11 can effectively inhibit the expression of TMV .
|
-
-
- HY-15647
-
BRD9539
1 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
BRD9539 is a histone methyltransferase G9a inhibitor with an IC50 of 6.3 μM. BRD9539 also inhibits PRC2 activity and is inactive against SUV39H1, NSD2 and DNMT1 .
|
-
-
- HY-107621
-
|
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MEK
|
Cancer
|
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U0124, an inactive U0126 analog, has no effect on c-Fos and c-Jun protein or mRNA levels. U0126 is a MEK inhibitor. U0124 does not inhibit MEK at concentrations up to 100 μM .
|
-
-
- HY-123632
-
|
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Cytochrome P450
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Others
|
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(3S,5S)-Atorvastatin sodium salt is a pregnane X receptor (PXR) activator and the inactive enantiomer of Atorvastatin. Atorvastatin is an orally active HMG-CoA reductase inhibitor with lipid-lowering capabilities .
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-
-
- HY-112464
-
|
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Others
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Neurological Disease
|
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PKR Inhibitor, negative control is an inactive structural analog of RNA-dependent protein kinase (PKR) inhibitor, which can be used as a negative control. PKR Inhibitor, negative control can also inhibit LK-induced neuronal death, exhibiting significant neuroprotective effects .
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-
-
- HY-78131BS
-
|
(R)-Ibuprofen-d3
|
NF-κB
|
Inflammation/Immunology
Cancer
|
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(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
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-
-
- HY-B1386
-
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Bacterial
Carbonic Anhydrase
Sodium Channel
|
Infection
|
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Halazone is an atypical antimicrobial sulfonamide derivative and a carbonic anhydrase II inhibitor with a Kd value of 1.45 µM. Halazone protects sodium channels from inactivation. Halazone is widely used for disinfection of drinking water .
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-
-
- HY-131284
-
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Drug Metabolite
|
Others
|
|
(S)-Dehydro Venlafaxine is an inactive S-enantiomer of Dehydro Venlafaxine. Dehydro Venlafaxine is an impurity of Venlafaxine hydrochloride. Venlafaxine hydrochloride (Wy 45030 hydrochloride) is a potent serotonin (5-HT) / norepinephrine (NE) reuptake dual inhibitor .
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-
-
- HY-13633
-
|
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Aldose Reductase
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Metabolic Disease
Cancer
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Exisulind is an inactive metabolite of the nonsteroidal, anti-inflammatory agent sulindac . Exisulind inhibits aldose reductase with an IC50 of 367 nM in vitro and may contribute to the beneficial pharmacological effects of sulindac on type 2 diabetic complications .
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-
-
- HY-N0929
-
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COX
Reactive Oxygen Species
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Cancer
|
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Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities .
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-
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- HY-138935
-
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BI-425809
|
GlyT
|
Neurological Disease
|
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Iclepertin (BI-425809) is a potent, selective and orally active glycine transporter 1 (GlyT1) inhibitor. Iclepertin is inactive against GlyT2. Iclepertin can be used for Alzheimer disease and schizophrenia research .
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-
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- HY-160879
-
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Filovirus
|
Infection
|
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EBOV-IN-4 (compound 12), a benzothiazepine, is a potent Ebola virus (EBOV) inhibitor with 64.9% inhibitory for EBOV-GP-pseudotype virus (pEBOV) with 10 μM. EBOV-IN-4 is inactive with ASFV .
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-
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- HY-108437
-
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Wnt
|
Infection
Cancer
|
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exo-IWR-1, an inactive stereoisomer of Endo-IWR-1, is a negative control of IWR-1 (HY-12238). IWR-1 is a tankyrase inhibitor which inhibits Wnt/β-catenin signaling pathway .
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-
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- HY-113083
-
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APAP-glu
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Drug Metabolite
Endogenous Metabolite
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Others
|
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Acetaminophen glucuronide (APAP-glu) is an inactive glucuronide metabolite of Acetaminophen (HY-66005) . Acetaminophen is a selective cyclooxygenase-2 (COX-2) inhibitor and a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor .
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-
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- HY-125143
-
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MAGL
|
Metabolic Disease
|
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ABC34 is an inactive control compound of JJH260. ABC34 does not inhibit the fluorophosphonate reactivity or fatty acid esters of hydroxy fatty acid (FAHFA) hydrolysis activity of AIG1. ABC34 can inhibit both ABHD6 and PPT122 .
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-
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- HY-W409181
-
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Proteasome
|
Neurological Disease
|
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(Rac)-PD 151746 is the optically inactive racemate of PD 151746 (HY-19749). PD 151746 is a neuroprotective calpain inhibitor with Ki values of 0.26 μM (u-calpain) and 5.33 μM (m-calpain), respectively .
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-
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- HY-150070
-
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UCL-1397
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Others
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Neurological Disease
|
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Butabindide (UCL-1397) is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide inhibits TPP II to protect CCK-8 against inactivation .
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-
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- HY-158098
-
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FGFR
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Metabolic Disease
|
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FGFR1 inhibitor-11 (compound 5g) binds to FGFR1, inactivation of its downstream ERK1/2 and IκBα/NF-κB signaling inhibited RANKL-induced osteoclastogenesis. FGFR1 inhibitor-11 has oral bioactivity .
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-
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- HY-14200A
-
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TVP1022 mesylate; S-PAI mesylate
|
Monoamine Oxidase
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Neurological Disease
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(S)-Rasagiline (TVP1022) mesylate is the relatively inactive S-enantiomer form of Rasagiline mesylate. Rasagiline mesylate is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively .
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-
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- HY-119370
-
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Bcr-Abl
Apoptosis
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Cancer
|
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CHMFL-ABL-121 is a highly potent type II ABL kinase inhibitor with IC50s of 2 nM and 0.2 nM against purified inactive ABL wt and T315I kinase protein, respectively .
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- HY-N6893
-
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NF-κB
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Inflammation/Immunology
|
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Ergolide is a sesquiterpene lactone isolated from the dried flowers of Inula Britannica. Ergolide inhibits inducible nitric oxide synthase and cyclo-oxygenase-2 expression in RAW 264.7 macrophages through the inactivation of NF-κB .
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- HY-122700
-
|
|
Complement System
|
Inflammation/Immunology
|
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Factor D inhibitor 6 is a potent, highly selective and orally active factor D (FD) inhibitor with an IC50 of 30 nM and a Kd of 6 nM. Factor D inhibitor 6 is inactive against factor B, lassical and lectin complement-pathway activation, and a broad assay panel of receptors, ion channels, kinases and proteases .
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-
- HY-12349
-
|
|
Others
|
Infection
|
|
H1PVAT is a potent and selective inhibitor of poliovirus serotypes (PV-1, PV-2, PV-3), and inhibits early stage of the replication. H1PVAT interacts with viral capsid directly and protects PV against heat inactivation .
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- HY-107759
-
|
UCL-1397 oxalate
|
Others
|
Neurological Disease
|
|
Butabindide (UCL-1397) oxalate is a potent, selective tripeptidvl peptidase II (TPP II) inhibitor with Ki values of 7 nM and 10 μM for TPP II and TPP I, respectively. Butabindide oxalate inhibits TPP II to protect CCK-8 against inactivation .
|
-
- HY-15483
-
DY131
3 Publications Verification
GSK 9089
|
Estrogen Receptor/ERR
Smo
|
Endocrinology
Cancer
|
|
DY131 (GSK 9089) is a potent and selective ERRγ and ERRβ agonist. DY131displays inactive against ERRα, ERα and ERβ . DY131 also inhibits Smo signaling .
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- HY-W040030
-
|
|
Others
|
Metabolic Disease
Cancer
|
|
Hematin, an iron-containing porphyrin, inhibits the activity of clotting factors and also fibrin clot lysis through the mechanism of binding to and inactivation of hemostatic proteins . Hematin can be used for the research of acute porphyrias and cancer .
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-
- HY-P3892
-
|
|
PKC
|
Inflammation/Immunology
|
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Protein Kinase C (19-35) Peptide is the PKC pseudosubstrate inhibitor/region. Protein Kinase C (19-35) Peptide possibly blocks the substrate-binding site in its kinase domain, makes the cytoplasmic form of PKC inactive .
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-
- HY-126373
-
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SN-38G
|
Drug Metabolite
|
Cancer
|
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SN-38 glucuronide is an inactive metabolite of the anticancer active molecule Irinotecan (HY-16562) and has toxic effects on the gastrointestinal tract. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
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-
- HY-151239
-
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AR 00440993
|
Cytochrome P450
|
Cancer
|
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ONT-993 is an aliphatic hydroxylated metabolite. ONT-993 inhibits CYP2D6 (IC50=7.9 µM) and causes metabolism-dependent inactivation of CYP3A (KI=1.6 µM) .
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-
- HY-13896
-
|
|
EGFR
Autophagy
Apoptosis
|
Cancer
|
|
PD168393?is a potent, selective and cell-permeable inhibitor of EGFR tyrosine kinase and ErbB2. PD168393 irreversiblely inactivates EGF receptor ( IC50=0.7 nM) and is inactive against insulin receptor, PDGFR, FGFR and PKC .
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-
- HY-19675
-
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LT-NS 001; MX 1094
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COX
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Inflammation/Immunology
|
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Naproxen etemesil is a lipophilic, non-acidic, inactive proagent of naproxen that is hydrolysed to pharmacologically active Naproxen once absorbed. Naproxen is a COX-1 and COX-2 inhibitor with IC50s of 8.72 and 5.15 μM, respectively in cell assay.
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- HY-139984
-
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Btk
|
Neurological Disease
Inflammation/Immunology
|
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BIIB091 is a potent, selective, orally active and reversible BTK inhibitor, with an IC50 of <0.5 nM. BIIB091 binds the BTK protein to sequester TYR-551 into an inactive conformation with excellent affinity. BIIB091 can be used for the research of multiple sclerosis .
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- HY-123956
-
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IRAK
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Inflammation/Immunology
|
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HG-12-6 is a type II inhibitor of IRAK4. HG-12-6 shows preferential binding to unphosphorylated inactive IRAK4 with an IC50 of 165 nM. HG-12-6 can modulate IRAK4 activity in autoimmunity and inflammation .
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-
- HY-130149
-
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MRTX849
|
Ras
|
Cancer
|
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Adagrasib (MRTX849) is a potent, orally-available, and mutation-selective covalent inhibitor of KRAS G12C with potential antineoplastic activity. Adagrasib covalently binds to KRAS G12C at the cysteine at residue 12, locks the protein in its inactive GDP-bound conformation, and inhibits KRAS-dependent signal transduction .
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-
- HY-108847
-
|
|
TNF Receptor
Bacterial
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Inflammation/Immunology
Cancer
|
|
Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
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- HY-128777
-
|
|
VDAC
Apoptosis
|
Cancer
|
|
WEHI-9625 is a tricyclic sulfone, first-in-class inhibitor of apoptosis with an EC50 of 69 nM. WEHI-9625 binds to VDAC2 and promotes its ability to inhibit apoptosis driven by mouse BAK. WEHI-9625 is completely inactive against both human BAK and the closely related apoptosis effector BAX .
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-
- HY-136658
-
|
|
STAT
Apoptosis
|
Cancer
|
|
STAT3-IN-7 is a Sorafenib analogue and potently inhibits the phosphorylation of STAT3. STAT3-IN-7 induces cell apoptosis through SHP-1 dependent STAT3 inactivation. STAT3-IN-7 does not inhibit kinase activity and has anticancer effects .
|
-
- HY-114277
-
|
AMG-510
|
Ras
|
Cancer
|
|
Sotorasib (AMG-510) is a first-in-class, orally bioavailable, and selective KRAS G12C covalent inhibitor. Sotorasib irreversibly inhibits KRAS G12C by locking it in an inactive GDP-bound state. Sotorasib is the first KRAS G12C inhibitor in clinical development and leads to the regression of KRAS G12C tumors .
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-
- HY-P5872
-
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JZTX-XI
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin XI (JZTX-XI) is a sodium conductance inhibitor with an IC50 of 124 nM. Jingzhaotoxin XI slows the fast inactivation (EC50=1.18±0.2 μM) of Nav1.5 expressed in Chinese hamster ovary (CHO-K1) cells .
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-
- HY-P5772
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-II, a 32 amino acid residues including two acidic and two basic residues, is a neurotoxin. Jingzhaotoxin-II inhibits voltage-gated sodium channels (VGSC) that significantly slows rapid inactivation of TTX-resistant (TTX-R) VGSC on cardiac myocytes with the IC50 of 0.26 μM .
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-
- HY-147691
-
|
|
Glutathione Peroxidase
Potassium Channel
|
Inflammation/Immunology
|
|
MPO-IN-5 (compound 1) is a potent, irreversible MPO (myeloperoxidase) inhibitor. MPO-IN-5 inhibits MPO peroxidation and hERG binding, with IC50 values of 0.22 and 2.8 μM, respectively. MPO-IN-5 shows rapid kinetics of inhibition, with enzyme inactivation rate (kinact/Ki) of 23000 M −1s −1 .
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-
- HY-15779
-
|
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SphK
Apoptosis
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Cancer
|
|
K145 is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 µM and a Ki of 6.4 µM. K145 is inactive against SphK1 and other protein kinases. K145 induces cell apoptosis and has potently antitumor activity .
|
-
- HY-15779A
-
|
|
SphK
Apoptosis
|
Cancer
|
|
K145 hydrochloride is a selective, substrate-competitive and orally active SphK2 inhibitor with an IC50 of 4.3 μM and a Ki of 6.4 μM. K145 hydrochloride is inactive against SphK1 and other protein kinases. K145 hydrochloride induces cell apoptosis and has potently antitumor activity .
|
-
- HY-145928
-
|
GDC-6036
|
Ras
|
Cancer
|
|
Divarasib (GDC-6036) is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state.
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-
- HY-50683S
-
|
|
c-Met/HGFR
|
Cancer
|
|
JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
|
-
- HY-N0929R
-
|
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COX
Reactive Oxygen Species
|
Cancer
|
|
Hexahydrocurcumin (Standard) is the analytical standard of Hexahydrocurcumin. This product is intended for research and analytical applications. Hexahydrocurcumin is one of the major metabolites of curcumin and a selective, orally active COX-2 inhibitor. Hexahydrocurcumin is inactive against COX-1. Hexahydrocurcumin has antioxidant, anticancer and anti-inflammatory activities .
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-
- HY-B0185A
-
|
Lignocaine hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence . Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor .
|
-
- HY-108630
-
U-73343
4 Publications Verification
|
Phospholipase
|
Others
|
|
U-73343, works as a protonophore, is an inactive analog of U-73122 and can be used as a negative control. U-73343 dose-dependently inhibits acid secretion irrespective of the stimulant. U-73122 is a phospholipase C (PLC) and 5-LO (5-lipoxygenase) inhibitor with an IC50 of 1-2.1 μM for PLC .
|
-
- HY-151376
-
|
|
Proteasome
|
Infection
|
|
SAP2-IN-1 is a secreted aspartic protease 2 (SAP2) inhibitor and has potent SAP2 inhibitory activity with an IC50 value of 0.92 μM. SAP2-IN-1 also is a virulence factor inhibitor and is inactive in vitro. SAP2-IN-1 can be used for the research of infection .
|
-
- HY-113083R
-
|
|
Drug Metabolite
Endogenous Metabolite
|
Others
|
|
Acetaminophen glucuronide (Standard) is the analytical standard of Acetaminophen glucuronide. This product is intended for research and analytical applications. Acetaminophen glucuronide (APAP-glu) is an inactive glucuronide metabolite of Acetaminophen (HY-66005) . Acetaminophen is a selective cyclooxygenase-2 (COX-2) inhibitor and a potent hepatic N-acetyltransferase 2 (NAT2) inhibitor .
|
-
- HY-18901
-
|
|
RIP kinase
|
Inflammation/Immunology
|
|
RIPK1-IN-4 (compound 8) is a potent and selective type II kinase inhibitor of receptor interacting protein 1 (RIP1) kinase and binds to a DLG-out inactive form of RIP1 with an IC50s of 16 nM and 10 nM for RIP1 and ADP-Glo kinase .
|
-
- HY-B0589C
-
|
|
Cytochrome P450
|
Metabolic Disease
|
|
(3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids .
|
-
- HY-118387
-
|
|
Potassium Channel
|
Neurological Disease
|
|
AVE-0118 is a nonselective Kv1.5 blocker with an IC50 of 1.1 μM. AVE-0118 is a multichannel inhibitor with weak, micromolar activity against Kv1.5 and other ion channels. It is inactive against IKs, IKATP, and L-type Ca+ channels .
|
-
- HY-15517
-
KN-92
5 Publications Verification
|
Others
|
Cancer
|
|
KN-92 is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-15517A
-
|
|
Others
|
Cancer
|
|
KN-92 phosphate is an inactive derivative of KN-93, without CaM kinase inhibitory activity. KN-92 phosphate is intended to be used as a control compound in studies designed to elucidate the antagonist activities of KN-93. KN-93 is a cell-permeable, reversible and competitive CaMKII inhibitor .
|
-
- HY-N0314
-
-
- HY-N6691
-
|
3-Veratroylveracevine
|
Sodium Channel
|
Neurological Disease
|
|
Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39 µM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow .
|
-
- HY-121585
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
CAY10698 (compound 1) is a potent and selective inhibitor of 12-Lipoxygenase (12-LOX) with an IC50 of 5.1 μM. CAY10698 is inactive against 5-LOX, 15-LOX-1, 15-LOX-2 and COX-1/2 .
|
-
- HY-P3882
-
|
|
Amino Acid Derivatives
|
Neurological Disease
|
|
Fmoc-Ala-Glu-Gln-Lys-NH2 (AEQK) is a tetrapeptide. Fmoc-Ala-Glu-Gln-Lys-NH2 is the inactive control for Fmoc-Ala-Glu-Asn-Lys-NH2 (AENK) peptide inhibitor. AENK blocks proteolysis of UNC5C protein .
|
-
- HY-126373S1
-
|
SN-38G-13C6
|
Isotope-Labeled Compounds
|
Others
|
|
SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
|
-
- HY-145928B
-
|
GDC-6036 adipate
|
Ras
|
Cancer
|
|
Divarasib (GDC-6036) adipate is an orally bioavailable, highly potent, and selective KRAS G12C inhibitor with an IC50 of <0.01 μM. Divarasib covalently binds to the switch II (SW-II) pocket of KRAS G12C and irreversibly locks it in the inactive GDP-bound state .
|
-
- HY-111457
-
|
|
Others
|
Inflammation/Immunology
|
|
BAY-677 is an inactive control for BAY-678. BAY-678 is an orally bioavailable, highly potent, selective and cell-permeable inhibitor of human neutrophil elastase (HNE), with an IC50 of 20 nM . BAY-678 is also nominated as a chemical probe to the public via the Structural Genomics Consortium (SGC) .
|
-
- HY-145381
-
|
|
11β-HSD
|
Metabolic Disease
|
|
11β-HSD1-IN-6 is a an 11β-HSD-1 inhibitor. The 11β hydroxysteroid dehydrogenase enzymes (11β-HSDs) mediate the interconversion of the glucocorticoid (GC) corticosterone or cortisol to an inactive form, 11-dehydrocorticosterone (11-DHC) or Cortisone, respectively .
|
-
- HY-114865
-
|
|
RGS Protein
Calcium Channel
|
Neurological Disease
|
|
BMS-192364 is targeting the Gα-RGS interaction to produce an inactive Gα-RGS complex. BMS-192364 reduces urinary bladder contraction and exert RGS-agonist properties by increasing the action of GAPs on Gq proteins. BMS-192364 inhibits calcium flux .
|
-
- HY-120600
-
|
|
Necroptosis
Apoptosis
RIP kinase
|
Inflammation/Immunology
|
|
Sibiriline is a specific competitive inhibitor of RIPK1 that targets the RIPK1 ATP-binding site and locks it in an inactive conformation. Sibiriline inhibits TNF-induced RIPK1-dependent necroptosis and RIPK1-dependent apoptosis, but does not protect cells from caspase-dependent apoptosis. Sibiriline protects mice from concanavalin A-induced hepatitis and has the potential to inhibit immune-dependent hepatitis. .
|
-
- HY-10929
-
UNC0224
2 Publications Verification
|
Histone Methyltransferase
|
Cancer
|
|
UNC0224 is a potent and selective histone methyltransferase G9a inhibitor with a Ki of 2.6 nM, an IC50 of 15 nM and a Kd of 23 nM. UNC0224 also potently inhibits b>GLP with assay-dependent IC50 values of 20-58 nM. UNC0224 is inactive against SET7/9, SET8/PreSET7, PRMT3 and JMJD2E .
|
-
- HY-B0185
-
|
Lignocaine
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-B0185B
-
|
Lignocaine hydrochloride hydrate
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-P5781
-
|
|
Sodium Channel
|
Neurological Disease
|
|
δ-Theraphotoxin-Hm1b is a 42-amino acid peptide isolated from Togo starburst tarantula (Heteroscodra maculata) venom. δ-Theraphotoxin-Hm1b selectively inhibits inactivation of NaV1.1 but have no effect on NaV1.7 .
|
-
- HY-E70291
-
|
GALNT4
|
MAP3K
p38 MAPK
JNK
NF-κB
Endogenous Metabolite
|
Cancer
|
|
N-Acetylgalactosaminyltransferase 4 (GALNT4) is a glycosyltransferase capable of inhibiting the activation of ASK1. By directly binding to ASK1, N-Acetylgalactosaminyltransferase 4 suppresses its N-terminal dimerization and subsequent phosphorylation, leading to robust inactivation of downstream JNK/p38 and NF-κB signals, and thereby improving the prognosis of liver surgery .
|
-
- HY-114965
-
TP-064
5 Publications Verification
|
Histone Methyltransferase
|
Inflammation/Immunology
Cancer
|
|
TP-064 is a potent and selective proteinarginine methyltransferase 4 (PRMT4; CARM1) inhibitor (IC50 <10 nM). TP-064 inhibits dimethylation of BAF155 (IC50 of 340 nM) and MED12 (IC50 of 43 nM). TP-064 is inactive against the other family members except for PRMT6 (IC50 of 1.3 μM). TP-064 has anticancer activities .
|
-
- HY-100627
-
|
|
MEK
|
Cancer
|
|
APS-2-79 is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .
|
-
- HY-108706
-
|
|
Histone Demethylase
|
Cancer
|
|
KDM2A/7A-IN-1 is a first-in-class, selective and cell-permeable inhibitor of histone lysine demethylases KDM2A/7A, with an IC50 of 0.16 μM for KDM2A, exhibits 75 fold selevtivity over other JmjC lysine demethylases, and is inactive on methyl transferases, and histone acetyl transferases .
|
-
- HY-100627A
-
|
|
MEK
|
Cancer
|
|
APS-2-79 hydrochloride is a KSR-dependent MEK antagonist. APS-2-79 inhibits ATP biotin binding to KSR2 within the KSR2-MEK1 complexe with an IC50 of 120 nM. APS-2-79 makes the stabilization of the KSR inactive state antagonizes oncogenic Ras-MAPK signaling .
|
-
- HY-121329
-
|
AMA-1080; Ro 17-2301
|
Penicillin-binding protein (PBP)
Antibiotic
Bacterial
|
Infection
|
|
Carumonam (AMA-1080; Ro 17-2301) is a sulfonated monocyclic β-Lactam Antibiotic, targeting to penicillin-binding protein (PBP). Carumonam exerts highly activity against Enterobacteriaceae, Pseudomonas aeruginosa, and Haemophilus influenzae, while it weakly and even inactively inhibits Streptococcus pneumoniae and Staphylococcus aureus. Carumonam is resistant to beta-lactamase-mediated hydrolysis .
|
-
- HY-13868
-
|
|
Ras
|
Cancer
|
|
SCH-53870 is a Ras activation inhibitor that binds to the Ras-GDP complex, keeping the Ras protein in an inactive GDP-bound state and preventing it from switching to an active GTP-bound state. SCH-53870 affects cell signaling and cell proliferation by preventing the activation of Ras protein. SCH-53870 can be used in cancer research .
|
-
- HY-107779
-
|
|
Raf
|
Cancer
|
|
BI-882370 is a potent and selective RAF kinase inhibitor that binds to the ATP binding site of the kinase positioned in the DFG-out (inactive) conformation of the BRAF kinase. BI-882370 (BI 882370) inhibits the oncogenic BRAF V600E-mutant, the WT BRAF and CRAF kinases with IC50s of 0.4, 0.8, and 0.6 nM, respectively. BI-882370 also inhibits SRC family kinases .
|
-
- HY-15424
-
|
NSC 113939; 5-ITu
|
Adenosine Kinase
|
Cancer
|
|
5-Iodotubercidin (NSC 113939), an ATP mimetic, is a potent adenosine kinase inhibitor with an IC50 of 26 nM. 5-Iodotubercidin (NSC 113939) initiates glycogen synthesis in isolated hepatocytes by causing inactivation of phosphorylase and activation of glycogen synthase. 5-Iodotubercidin (NSC 113939) also inhibits CK1, insulin receptor tyrosine kinase, phosphorylase kinase, PKA, CK2, PKC and Haspin .
|
-
- HY-B0185AS1
-
|
Lignocaine-d6 hydrochloride
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
|
-
- HY-16926
-
|
|
Arp2/3 Complex
HIV
|
Infection
Cancer
|
|
CK-666 is a cell-permeable actin-related protein Arp2/3 complex inhibitor (IC50=12 μM). CK-666 binds to Arp2/3 complex, stabilizes the inactive state of the complex, blocking movement of the Arp2 and Arp3 subunits into the activated filament-like (short pitch) conformation .
|
-
- HY-113849
-
|
MLS000573151
|
Ras
|
Inflammation/Immunology
|
|
MLS-573151 (MLS000573151) is a selective GTPase Cdc42 inhibitor with an EC50 of 2 μM. MLS-573151 is inactive against other GTPases family members, such as Rab2, Rab7, H-Ras, Rac1, Rac 2 and RhoA wild-type. MLS-573151 acts by blocking the binding of GTP to Cdc42 .
|
-
- HY-78931A
-
|
|
Others
|
Cancer
|
|
(R,S,S,R,S)-Boc-Dap-NE is the inactive isomer of Boc-Dap-NE (HY-78931), and can be used as an experimental control. Boc-Dap-NE, is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-78931B
-
|
|
Others
|
Cancer
|
|
(S,S,S,S,R)-Boc-Dap-NE is the inactive isomer of Boc-Dap-NE (HY-78931), and can be used as an experimental control. Boc-Dap-NE, is an intermediate in the synthesis of Monomethyl auristatin E (HY-15162), which is an inhibitor of tubulin polymerization. Monomethyl auristatin E can be used to synthesize Antibody-Drug Conjugates (ADCs) as ADC Cytotoxin.
|
-
- HY-101125B
-
|
D-45
|
Others
|
Cancer
|
|
D-Moses (D-45) is an enantiomer of L-Moses (HY-101125). L-Moses (L-45) is a potent and selective p300/CBP-associated factor (PCAF) bromodomain (Brd) inhibitor. D-Moses shows no observable binding for PCAF Brd. D-Moses can be used as an inactive control compound to L-Moses .
|
-
- HY-121629
-
|
|
PDK-1
|
Cancer
|
|
PS210 is a potent and selective PDK1 activator with a Kd of 3 μM and targets the PIF-binding pocket of PDK1. PS210 is inactive against other protein kinases, including PDK1 downstream signaling components such as S6K, PKB/Akt or GSK3. In cells, the prodrug of PS210 (PS423) acts as a substrate-selective inhibitor of PDK1, inhibiting the phosphorylation and activation of S6K .
|
-
- HY-158107
-
|
|
Ras
|
Cancer
|
|
BBO-8520 is a direct small molecule covalent inhibitor targeting KRAS G12C with high oral availability. BBO-8520 has the characteristics of KRAS G12C (OFF) inhibitor and the function of blocking KRAS G12C (ON) signal. BBO-8520 inhibits cell proliferation by inhibiting KRAS G12C (ON) by binding GTP protein. BBO-8520 can block RAS-RAF1 interaction and return KRAS G12C to the inactive (OFF) state .
|
-
- HY-14200
-
|
TVP1022; S-PAI
|
Monoamine Oxidase
|
Neurological Disease
|
|
(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . (S)-Rasagiline 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-100764
-
|
|
Histone Demethylase
|
Cancer
|
|
YUKA1 is a potent and cell permeable Lysine demethylase 5A (KDM5A) inhibitor, with an IC50 of 2.66 μM, less active on KDM5C (IC50, 7.12 μM), and is inactive on KDM5B, KDM6A or KDM6B. YUKA1 increases H3K4me3 levels in human cells with anti-cancer activity .
|
-
- HY-145082
-
|
|
Others
|
Others
|
|
4-Sulfo-N-(4-aminobenzyl)-1,8-naphthalimide potassium is an inactive 1,8-Naphthalimide derivative. 4-Sulfo-N-(4-aminobenzyl)-1,8-naphthalimide potassium can be used as a negative control for the clathrin inhibitor 3-Sulfo-N-benzyl-1,8-naphthalimide, potassium salt .
|
-
- HY-N0314R
-
|
|
Interleukin Related
Prostaglandin Receptor
Apoptosis
|
Inflammation/Immunology
|
|
Pectolinarin (Standard) is the analytical standard of Pectolinarin. This product is intended for research and analytical applications. Pectolinarin possesses anti-inflammatory activity . Pectolinarin inhibits secretion of IL-6 and IL-8, as well as the production of PGE2 and NO. Pectolinarin suppresses cell proliferation and inflammatory response and induces apoptosis via inactivation of the PI3K/Akt pathway .
|
-
- HY-15154
-
NG 52
5 Publications Verification
Compound 52
|
CDK
|
Cancer
|
|
NG 52 is a potent, cell-permeable, selective, ATP-compatible and orally active Cdc28p and Pho85p kinase inhibitor with IC50s of 7 μM and 2 μM, respectively. NG 52 also inhibits the activity of phosphoglycerate kinase 1 (PGK1) with an IC50 of 2.5 μM. NG 52 is inactive against yeast kinases Kin28p, Srb10, and Cak1p .
|
-
- HY-B0780
-
-
- HY-B0185AS
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine-d10 (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride, an amide derivative, has the potential for the research of the ventricular arrhythmia[2].
|
-
- HY-B0185S1
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
|
-
- HY-134673
-
UZH1
3 Publications Verification
|
Apoptosis
|
Cancer
|
|
UZH1 is a racemate of UZH1a and UZH1b. UZH1a is a potent and selective METTL3 inhibitor, with an IC50 of 280 nM. UZH1b (IC50=28 µM) is essentially inactive. UZH1 can be used for epitranscriptomic modulation of cellular processes. UZH1 has antitumor activity. UZH1 also can be used as a chemical probe for studying METTL3 .
|
-
- HY-123090
-
|
|
11β-HSD
|
Metabolic Disease
|
|
11β-HSD1-IN-12 is a 11β-HSD1 inhibitor (Example 21 in reference patent). 11β-HSD1 regenerates active glucocorticoids from inactive forms and is important in regulating intracellular glucocorticoid concentration. 11β-HSD1-IN-12 can be used in the research of obesity and metabolic syndrome .
|
-
- HY-N6691R
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Veratridine (Standard) is the analytical standard of Veratridine. This product is intended for research and analytical applications. Veratridine (3-Veratroylveracevine) is a plant neurotoxin, a voltage-gated sodium channels (VGSCs) agonist. Veratridine inhibits the peak current of Nav1.7, with an IC50 of 18.39?μM. Veratridine regulates sodium ion channels mainly by activating sodium ion channels, preventing channel inactivation and increasing sodium ion flow .
|
-
- HY-101544
-
|
|
FGFR
|
Cancer
|
|
ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner .
|
-
- HY-B0185S
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
N-Oxide Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
|
-
- HY-B0185R
-
|
Lignocaine (Standard)
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (Standard) is the analytical standard of Lidocaine. This product is intended for research and analytical applications. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-B0185BR
-
|
|
Sodium Channel
MEK
ERK
NF-κB
Apoptosis
|
Cardiovascular Disease
Cancer
|
|
Lidocaine (hydrochloride hydrate) (Standard) is the analytical standard of Lidocaine (hydrochloride hydrate). This product is intended for research and analytical applications. Lidocaine (Lignocaine) hydrochloride hydrate inhibits sodium channels involving complex voltage and using dependence. Lidocaine hydrochloride hydrate decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride hydrate is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-12028
-
PD98059
Maximum Cited Publications
311 Publications Verification
|
MEK
ERK
Aryl Hydrocarbon Receptor
Autophagy
|
Cancer
|
|
PD98059 is a potent and selective MEK inhibitor with an IC50 of 5 µM. PD98059 binds to the inactive form of MEK, thereby preventing the activation of MEK1 (IC50 of 2-7 µM) and MEK2 (IC50 of 50 µM) by upstream kinases. PD98059 is a ERK1/2 signaling inhibitor. PD98059 is a ligand for the aryl hydrocarbon receptor (AHR), and suppresses TCDD binding (IC50 of 4 μM) and AHR transformation (IC50 of 1 μM). PD98059 also inhibits Mycobacterium bovis Bacillus CalmetteGuerin (BCG)-induced autophagy .
|
-
- HY-P5157
-
|
|
Potassium Channel
|
Neurological Disease
|
|
BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells .
|
-
- HY-P1928
-
|
|
Bcl-2 Family
|
Neurological Disease
Endocrinology
|
Humanin, an anti-apoptotic peptide of 24 amino acids, is a Bax inhibitor. Humanin prevents the translocation of Bax from cytosol to mitochondria, blocks Bax from the inactive to active conformation. Humanin is a mitochondria-associated peptide with a neuroprotective effect against AD-related neurotoxicity. Humanin also improves overall insulin sensitivity in animal. Humanin are related to aging .
Humanin analogue, in which the serine at position 14 is replaced by glycine, names HNG .
|
-
- HY-116423
-
|
|
NEKs
|
Cancer
|
|
JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 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-116423A
-
|
|
NEKs
|
Cancer
|
|
JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) 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-15335
-
|
|
MDM-2/p53
E1/E2/E3 Enzyme
|
Cancer
|
|
Nutlin-3b, the inactive form of Nutlin-3 (HY-50696), is a p53/MDM2 inhibitor with an IC50 of 13.6 μM. Nutlin-3b is 150 times less potent in binding to MDM2 than Nutlin-3a (HY-10029). Nutlin-3b is promising for research of cancers .
|
-
- HY-117026
-
|
|
Cytochrome P450
|
Metabolic Disease
Inflammation/Immunology
|
|
LKY-047, a Decursin derivative, is a potent and selective reversible competitive cytochrome P45022J2 (CYP2J2) inhibitor with an IC50 of 1.7 μM. LKY-047 is inactive against other human P450s, such as CYPs 1A2, 2A6, 2B6, 2C8, 2C9, 2C19, 2D6, 2E1, and 3A .
|
-
- HY-134581
-
|
M5049
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran is inactive against TLR3, TLR4 and TLR9. Enpatoran can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran exhibits excellent pharmacokinetic properties in vivo. Enpatoran can be used for both innate and adaptive autoimmunity blocking research .
|
-
- HY-135887
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
Autophagy
|
Cancer
|
|
ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect .
|
-
- HY-134581A
-
|
M5049 hydrochloride
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Enpatoran (M5049) hydrochloride is a potent, orally active and dual TLR7/8 inhibitor with IC50s of 11.1 nM and 24.1 nM in HEK293 cells, respectively. Enpatoran hydrochloride is inactive against TLR3, TLR4 and TLR9. Enpatoran hydrochloride can block molecule synthetic ligands and natural endogenous RNA ligands. Enpatoran hydrochloride exhibits excellent pharmacokinetic properties in vivo. Enpatoran hydrochloride can be used for both innate and adaptive autoimmunity blocking research .
|
-
- HY-120026
-
|
KB015
|
Thyroid Hormone Receptor
|
Neurological Disease
|
|
KB130015 (KB015) is an orally active and potent ThRα and ThRβ (Thyroid Hormone Receptor) inhibitor, with IC50 values of 4.5 and 5.1 μM, respectively. KB130015 has antiarrhythmic properties. KB130015 markedly slows the kinetics of inactivation of Na + channels. KB130015 opens large-conductance Ca 2+-activated K + channels and relaxes vascular smooth muscle .
|
-
- HY-P5455
-
|
|
LIM Kinase (LIMK)
|
Others
|
|
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)
|
-
- HY-112306
-
|
DCC-2618
|
c-Kit
PDGFR
FLT3
VEGFR
Apoptosis
|
Cancer
|
|
Ripretinib (DCC-2618) is an orally bioavailable, selective KIT and PDGFRA switch-control inhibitor. Ripretinib (DCC-2618) targets and binds to both wild-type and mutant forms of KIT and PDGFRA specifically at their switch pocket binding sites, thereby preventing the switch from inactive to active conformations of these kinases and inactivating their wild-type and mutant forms. Ripretinib (DCC-2618) also inhibits multiple other kinase targets, such as FLT3 and KDR (or VEGFR-2) . DCC-2618 exerts antineoplastic effect and induces apoptosis .
|
-
- HY-160478
-
|
|
Bcr-Abl
|
Cancer
|
|
GNF-6 (Compound 14) inhibits the gatekeeper threonine residue mutation of BCR-ABL-T315I with IC50s of 0.25 μM, 0.09 μM and 0.590 μM for c-ABL-T334I, BCR-ABL and BCR-ABL-T315I variants, respectively. GNF-6, an ATP competitive inhibitor, disrupts the assembly of the hydrophobic spine (a network of hydrophobic interactions), thereby locking the kinase in an inactive ‘DFG-out’ conformation .
|
-
- HY-128206
-
I3MT-3
4 Publications Verification
HMPSNE
|
Hippo (MST)
|
Metabolic Disease
|
|
I3MT-3 (HMPSNE) is a potent, selective, and cell-membrane permeable inhibitor of 3-Mercaptopyruvate sulfurtransferase (3MST) (IC50=2.7 μM). I3MT-3 is inactive for other H2S/sulfane sulfur-producing enzymes. I3MT-3 targets a persulfurated cysteine residue located in the active site of 3MST .
|
-
- HY-151486
-
|
|
GLUT
|
Cancer
|
|
GLUT1-IN-1 is a glucose transporter 1 (GLUT1) inhibitor and has a GLUT1-specific inactivation ability. GLUT1-IN-1 exhibits concentration-dependent cytotoxicity for HeLa, A549 and HepG2 cells with IC50 values of 5.49 μM, 11.14 μM, and 8.73 μM, respectively. GLUT1-IN-1 can be used for the research of photodynamic therapy (PDT) and severals cancer .
|
-
- HY-B0185G
-
|
Lignocaine
|
Apoptosis
Sodium Channel
MEK
ERK
NF-κB
|
Cancer
|
|
Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
-
- HY-149677
-
|
|
Mitochondrial Metabolism
|
Cancer
|
|
ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP) (EC50: 1.37?μM for α-casein hydrolysis by HsClpP). ZK53 is is inactive toward bacterial ClpP proteins. ZK53 induces apoptosis in H1703, H520 and SK-MES-1 cells. ZK53 induces dysregulation of mitochondrial functions in lung squamous cell carcinoma (LUSC) cells. ZK53 inhibits tumor growth in H1703 xenograft mouse model .
|
-
- HY-16183A
-
|
Echothiophate chloride
|
Others
|
Cardiovascular Disease
|
|
Echothiophate (Echothiophate) chloride is a highly effective, long-lasting cholinesterase inhibitor employed as a miotic for managing glaucoma. Echothiopate chloride forms a covalent bond with the serine residue at the active site of cholinesterase through its phosphate group, rendering the enzyme permanently inactive and necessitating the synthesis of new enzymes by the cell. Given its irreversible binding to cholinesterase and the extremely slow rate of hydrolysis, the effects of echothiophate can persist for a week or longer. Echothiopate chloride is utilized as an ocular antihypertensive agent in the treatment of chronic glaucoma and, in certain cases, accommodative esotropia.
|
-
- HY-162895
-
|
|
Polo-like Kinase (PLK)
Akt
CDK
Caspase
Apoptosis
|
Cancer
|
NL13 is a Polo-like kinase 4 (PLK4) inhibitor with an IC50 value of 2.32 μM. NL13 can inhibit the viability of PC3 and DU145 prostate cancer cells, with IC50 values of 3.51 μM and 2.53 μM, respectively. NL13 can lead to the inactivation of the AKT signaling pathway by downregulating CCNB1/CDK1, inducing G2/M cell cycle arrest, and triggering apoptosis through the cleavage of caspase-9/caspase-3. In prostate cancer mice, NL13 can inhibit tumor growth .
|
-
- HY-P5395
-
|
|
HIV
|
Others
|
|
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
|
-
- HY-136995
-
|
|
Others
|
Cardiovascular Disease
|
|
AFD-21 maleate is a drug with antiarrhythmic activity. AFD-21 maleate inhibits sodium channels by binding to sodium channels in an inactive state, with both use-dependent and voltage-dependent effects. The unbinding rate of AFD-21 maleate is similar to that of Class I antiarrhythmic drugs with moderate kinetics. AFD-21 maleate can cause a slight prolongation of the action potential duration and significantly reduce the maximum rise rate of the action potential at certain concentrations. AFD-21 maleate also showed use-dependent blocking effects as stimulation frequency increased .
|
-
- HY-101257
-
|
|
CDK
|
Cancer
|
|
YKL-5-124 is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
|
-
- HY-12545
-
|
PbTx-3
|
Sodium Channel
|
Inflammation/Immunology
|
|
Brevetoxin-3 (PbTx-3) is a potent allosteric voltage-gated Na +?channel activator and has multiple active centers (A-ring lactone, C-42 of R side chain) . Brevetoxin-3 (PbTx-3) has a high affinity to site 5 of the voltage-sensitive Na +?channels, inhibits the inactivation of Na + channels and prolongs the mean open time of these channels. Brevetoxin-3 (PbTx-3) repeated exposures can lead to prolonged airway hyperresponsiveness (AHR) and lung inflammation .
|
-
- HY-W088066
-
|
Phosphoric acid, sodium salt, hydrate (1:3:12)
|
Biochemical Assay Reagents
|
Others
|
|
Trisodium phosphate dodecahydrate is a corrosion inhibitor for iron in 0.1 M NaClO4, in both aerated and deaerated solutions. Trisodium phosphate dodecahydrate can be used as an excipient, such as pH regulator, buffer. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
|
-
- 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-101257B
-
|
|
CDK
|
Cancer
|
|
YKL-5-124 TFA is a potent, selective, irreversible and covalent CDK7 inhibitor with IC50s of 53.5 nM and 9.7 nM for CDK7 and CDK7/Mat1/CycH, respectively. YKL-5-124 TFA is >100-fold greater selective for CDK7 than CDK9 and CDK2, and inactive against CDK12 and CDK13. YKL-5-124 TFA induces a strong cell-cycle arrest, inhibits E2F-driven gene expression, and exhibits little effect on RNA polymerase II phosphorylation status .
|
-
- HY-N8380
-
|
|
Apoptosis
Autophagy
PI3K
Necroptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
(-)-Latifolin, a flavonoid, induces apoptotic cell death by targeting PI3K/AKT/mTOR/p70S6K signaling. (-)-Latifolin significantly inhibits the cell proliferation of oral squamous cell carcinoma (OSCC), and causes the anti-metastatic activities by effectively blocking cell migration, invasion, and adhesion via the inactivation of FAK/Src. (-)-Latifolin suppresses autophagic-related proteins and autophagosome formation. (-)-Latifolin inhibits necroptosis by dephosphorylating necroptosis-regulatory proteins (RIP1, RIP3, and MLKL). (-)-Latifolin has beneficial effects on anti-aging, anti-carcinogenic, anti-inflammatory, and cardio-protective activities .
|
-
- HY-100947A
-
|
|
PROTACs
Ligands for E3 Ligase
HIF/HIF Prolyl-Hydroxylase
|
Others
|
|
cis VH-298 is the cis form of VH-298 (HY-100947). VH-298 is a potent VHL:HIF-α interaction inhibitor, with a Kd value of 80-90 nM. cis VH-298 results in a significant loss of binding specificity of hydroxylated HIF-1a peptides to VHL in vitro. VH-298 leads to HIF-α accumulation inside HeLa cells, but cis VH-298 is inactive even at high concentrations (250 μM). VH-298 is an E3 ligase Ligand, and can be used for synthesis of PROTACs .
|
-
- HY-113438
-
|
|
AP-1
JNK
|
Inflammation/Immunology
|
|
15(S)-HPETE is a monohydroperoxy polyunsaturated fatty acid (PUFA) produced by the action of 15-lipoxygenase (15-LO) on arachidonic acid. It is either metabolized to 14,15-leukotriene A41 or reduced to 15(S)-HETE by peroxidases.2,1 15(S)-HpETE mediates a number of biological functions including the induction of c-fos and c-jun, and activation of AP-1.3 15(S)-HpETE inhibits prostacyclin synthesis in porcine aortic microsomes and bovine endothelial cells, and can cause the suicide inactivation of porcine 12-LO.
|
-
- HY-B1588
-
|
|
Amyloid-β
HIV
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties .
Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the treatment of chronic liver disease .
Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD .
Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop .
Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form.
Carbenoxolone has antiviral activity against DENV infection targeting the virus itself .
|
-
- HY-N3387
-
|
|
Apoptosis
NF-κB
Akt
MMP
|
Inflammation/Immunology
Cancer
|
|
Licoricidin (LCD) is isolated from Glycyrrhiza uralensis Fisch, possesses anti-cancer activities. Licoricidin (LCD) inhibit SW480 cells (IC50=7.2 μM) by inducing cycle arrest, apoptosis and autophagy, and is a potential chemopreventive or chemotherapeutic agent against colorectal cancer . Licoricidin (LCD) inhibits Lung Metastasis by inhibition of tumor angiogenesis and lymphangiogenesis as well as changes in the local microenvironment of tumor tissues the anticarcinogenic effect . Licoricidin enhanced gemcitabine-induced cytotoxicity in Osteosarcoma (OS) cells by inactivation of the Akt and NF-κB pathways in vitro and in vivo . Licoricidin blocks UVA-induced photoaging via ROS scavenging, limits the activity of MMP-1, it can be considered as an active ingredient in new topically applied anti-ageing formulations .
|
-
- HY-W011426
-
|
Propan-2-yl hexadecanoate
|
Biochemical Assay Reagents
Liposome
|
Others
|
|
Isopropyl palmitate is an fatty acid ester. Isopropyl palmitate can be used for design and characterization of bioactive bilayer films. The bilayer membrane not only has the ability to scavenge free radicals and inhibit lipid peroxidation, but also can inhibit the growth of known foodborne pathogens. Isopropyl palmitate can be used as an excipient, such as lubricant, oily carrier, solvent, controlled-release transdermal film. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
|
-
- HY-P1441A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
|
-
- HY-101522
-
|
|
EGFR
BMX Kinase
Btk
MEK
|
Cancer
|
|
CHMFL-EGFR-202 is a potent, irreversible inhibitor of epidermal growth factor receptor (EGFR) mutant kinase, with IC50s of 5.3 nM and 8.3 nM for drug-resistant mutant EGFR T790M and WT EGFR kinases, respectively. CHMFL-EGFR-202 exhibits ～10-fold selectivity for EGFR L858R/T790M against the EGFR wild-type in cells. CHMFL-EGFR-202 adopts a covalent “DFG-in-C-helix-out” inactive binding conformation with EGFR, with strong antiproliferative effects against EGFR mutant-driven nonsmall-cell lung cancer (NSCLC) cell lines .
|
-
- HY-B1167A
-
|
Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride
|
Others
|
Cardiovascular Disease
|
|
Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
|
-
- HY-B1588S
-
|
|
Amyloid-β
HIV
11β-HSD
|
Infection
Neurological Disease
Inflammation/Immunology
|
|
Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].
|
-
| Cat. No. |
Product Name |
Type |
-
- HY-B0185G
-
|
Lignocaine (GMP)
|
Fluorescent Dye
|
|
Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
| Cat. No. |
Product Name |
Type |
-
- HY-W011426
-
|
Propan-2-yl hexadecanoate
|
Drug Delivery
|
|
Isopropyl palmitate is an fatty acid ester. Isopropyl palmitate can be used for design and characterization of bioactive bilayer films. The bilayer membrane not only has the ability to scavenge free radicals and inhibit lipid peroxidation, but also can inhibit the growth of known foodborne pathogens. Isopropyl palmitate can be used as an excipient, such as lubricant, oily carrier, solvent, controlled-release transdermal film. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
|
-
- HY-B0185G
-
|
Lignocaine (GMP)
|
Biochemical Assay Reagents
|
|
Lidocaine (GMP) is Lidocaine (HY-B0185) produced by using GMP guidelines. GMP small molecules work appropriately as an auxiliary reagent for cell therapy manufacture. Lidocaine inhibits sodium channels involving complex voltage and using dependence . Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3882
-
|
|
Amino Acid Derivatives
|
Neurological Disease
|
|
Fmoc-Ala-Glu-Gln-Lys-NH2 (AEQK) is a tetrapeptide. Fmoc-Ala-Glu-Gln-Lys-NH2 is the inactive control for Fmoc-Ala-Glu-Asn-Lys-NH2 (AENK) peptide inhibitor. AENK blocks proteolysis of UNC5C protein .
|
-
- HY-P1928
-
|
|
Bcl-2 Family
|
Neurological Disease
Endocrinology
|
Humanin, an anti-apoptotic peptide of 24 amino acids, is a Bax inhibitor. Humanin prevents the translocation of Bax from cytosol to mitochondria, blocks Bax from the inactive to active conformation. Humanin is a mitochondria-associated peptide with a neuroprotective effect against AD-related neurotoxicity. Humanin also improves overall insulin sensitivity in animal. Humanin are related to aging .
Humanin analogue, in which the serine at position 14 is replaced by glycine, names HNG .
|
-
- HY-P1402
-
|
|
Peptides
|
Others
|
|
[Glu27]-PKC (19-36) is an inactive control for protein kinase C (PKC) (19-36). PKC (19-36) is a pseudosubstrate peptide inhibitor of protein kinase C, it may be responsible for maintaining the enzyme in the inactive form in the absence of allosteric activators such as phospholipids .
|
-
- HY-P3892
-
|
|
PKC
|
Inflammation/Immunology
|
|
Protein Kinase C (19-35) Peptide is the PKC pseudosubstrate inhibitor/region. Protein Kinase C (19-35) Peptide possibly blocks the substrate-binding site in its kinase domain, makes the cytoplasmic form of PKC inactive .
|
-
- HY-P5872
-
|
JZTX-XI
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin XI (JZTX-XI) is a sodium conductance inhibitor with an IC50 of 124 nM. Jingzhaotoxin XI slows the fast inactivation (EC50=1.18±0.2 μM) of Nav1.5 expressed in Chinese hamster ovary (CHO-K1) cells .
|
-
- HY-P5772
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Jingzhaotoxin-II, a 32 amino acid residues including two acidic and two basic residues, is a neurotoxin. Jingzhaotoxin-II inhibits voltage-gated sodium channels (VGSC) that significantly slows rapid inactivation of TTX-resistant (TTX-R) VGSC on cardiac myocytes with the IC50 of 0.26 μM .
|
-
- HY-P5781
-
|
|
Sodium Channel
|
Neurological Disease
|
|
δ-Theraphotoxin-Hm1b is a 42-amino acid peptide isolated from Togo starburst tarantula (Heteroscodra maculata) venom. δ-Theraphotoxin-Hm1b selectively inhibits inactivation of NaV1.1 but have no effect on NaV1.7 .
|
-
- HY-P5157
-
|
|
Potassium Channel
|
Neurological Disease
|
|
BmP02 is a selective Kv1.3 channel blocker and a highly-selective Kv4.2 modulator, which can be isolated from Chinese scorpion (Buthus martensi Karsch) venom. BmP02 also delays the inactivation of Kv4.2 in HEK293T cells, with an EC50 value of ~850 nM. BmP02 inhibits the transient outward potassium currents (Ito) in ventricular muscle cells .
|
-
- HY-P5455
-
|
|
LIM Kinase (LIMK)
|
Others
|
|
S3 Fragment is a biological active peptide. (This peptide contains the unique amino-terminal phosphorylation site of Xenopus ADF/cofilin, the LIM kinase (LIMK) phosphorylation site. LIMK1 is a key regulator of the actin cytoskeleton through its phosphorylation of ADF/cofilin at serine-3 for inactivation. This peptide is a fragment of the S3 peptide containing the serine-3 sequence of ADF/cofilin that has been widely used as an effective competitive inhibitor of LIMK1.)
|
-
- HY-P5395
-
|
|
HIV
|
Others
|
|
TAT-GluR23A Fusion Peptide is a biological active peptide. (This is the GluR23A sequence, a control inactive peptide used as a mutant counterpart to glutamate receptor endocytosis inhibitor (GluR23Y), connected to an 11 amino acid cell permeable HIV Trans-Activator of Transcription (TAT) protein transduction domain (PTD). GluR23A is derived from GluR23Y amino acids 869 to 877, with Ala substituted for Tyr, and thus lacking essential phosphorylation sites.Control peptide of HY-P2259)
|
-
- HY-P1441A
-
|
|
Sodium Channel
|
Neurological Disease
|
|
Mambalgin 1 TFA is a selective ASIC1a inhibitor (IC50 values are 192 and 72 nM for human ASIC1a and ASIC1a/1b dimer, respectively). Mambalgin 1 TFA binds to closed/inactive channel. Mambalgin 1 TFA is selective for ASIC1a over ASIC2a, ASIC3, TRPV1, P2X2, 5-HT3, Nav1.8, Cav3.2 and Kv1.2 channels. Mambalgin 1 TFA increases latency of withdrawal response in mouse tail-flick and paw-flick tests.
|
| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-108847
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TNF Receptor
Bacterial
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Inflammation/Immunology
Cancer
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Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-N0929
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- HY-113083
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- HY-N6893
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- HY-N0314
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- HY-N6691
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- HY-12545
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- HY-N0929R
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- HY-113083R
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- HY-N0314R
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- HY-N6691R
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- HY-N8380
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Structural Classification
Dalbergia hupeana Hance
Source classification
Phenols
Polyphenols
Plants
Fabaceae
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Apoptosis
Autophagy
PI3K
Necroptosis
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(-)-Latifolin, a flavonoid, induces apoptotic cell death by targeting PI3K/AKT/mTOR/p70S6K signaling. (-)-Latifolin significantly inhibits the cell proliferation of oral squamous cell carcinoma (OSCC), and causes the anti-metastatic activities by effectively blocking cell migration, invasion, and adhesion via the inactivation of FAK/Src. (-)-Latifolin suppresses autophagic-related proteins and autophagosome formation. (-)-Latifolin inhibits necroptosis by dephosphorylating necroptosis-regulatory proteins (RIP1, RIP3, and MLKL). (-)-Latifolin has beneficial effects on anti-aging, anti-carcinogenic, anti-inflammatory, and cardio-protective activities .
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- HY-N3387
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- HY-B1167A
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Cardiorythmine hydrochloride; (+)-Ajmaline hydrochloride
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Rauvolfia verticillata (Lour.) Baill.
Apocynaceae
Structural Classification
Natural Products
Source classification
Plants
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Others
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Ajmaline hydrochloride is a Class Ia antiarrhythmic agent. It inhibits HERG potassium channels with IC50s of 1.0 μmol/l and 42.3 μmol/l in HEK cells and moth spider oocytes respectively. The inhibitory effect of Ajmaline hydrochloride is rapid, reversible, and positive frequency dependent. It acts primarily on the open state of the HERG channel and may also be combined with the inactivated state. The inhibitory effect of ajmaline hydrochloride is dependent on aromatic residues in the S6 domain, and the sensitivity is significantly reduced in the inactivation-deficient HERG S620T channel. It can also slightly affect the activation voltage of HERG channels. Ajmaline hydrochloride's inhibitory effect on HERG channels may contribute to both its potent antiarrhythmic effects and its potential proarrhythmic risk.
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-78131BS
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(R)-(-)-Ibuprofen-d3 is the deuterium labeled (R)-(-)-Ibuprofen. (R)-(-)-Ibuprofen is the R enantiomer of Ibuprofen, inactive on COX, inhibits NF-κB activation; (R)-(-)-Ibuprofen exhibits anti-inflammatory and antinociceptive effects.
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- HY-B0185AS
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Lidocaine-d10 (hydrochloride) is the deuterium labeled Lidocaine hydrochloride. Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride, an amide derivative, has the potential for the research of the ventricular arrhythmia[2].
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- HY-B0185S1
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Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
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- HY-50683S
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JNJ-38877605-d1 (compound DO-2) is a highly selective MNNG HOS transforming (MET) inhibitor. JNJ-38877605-d1 is thought to diminish the formation of the Aldehyde Oxidase 1 inactive metabolite M3 .
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- HY-126373S1
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SN-38 glucuronide- 13C6 is the 13C labeled SN-38 glucuronide (HY-126373) . SN-38 glucuronide is an inactive metabolite of the cancer agent Irinotecan. Irinotecan is a topoisomerase I inhibitor which can be used for researching colon and rectal cancer .
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- HY-B0185AS1
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Lidocaine-d6 (hydrochloride) is deuterium labeled Lidocaine (hydrochloride). Lidocaine hydrochloride (Lignocaine hydrochloride) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine hydrochloride decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine hydrochloride is an amide derivative and a agent to treat ventricular arrhythmia and an effective tumor-inhibitor[2].
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- HY-B0185S
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N-Oxide Lidocaine-d10 is the deuterium labeled Lidocaine. Lidocaine (Lignocaine) inhibits sodium channels involving complex voltage and using dependence[1]. Lidocaine decreases growth, migration and invasion of gastric carcinoma cells via up-regulating miR-145 expression and further inactivation of MEK/ERK and NF-κB signaling pathways. Lidocaine is an amide derivative and has potential for the research of ventricular arrhythmia[2].
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- HY-B1588S
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Carbenoxolone-d4 is deuterium labeled Carbenoxolone. Carbenoxolone, a semi-synthetic derivative of glycyrrhetinic acid, has previously been used for the management of dyspepsia and peptic ulcer because of its anti-inflammatory properties[3]. Carbenoxolone, a general hemichannel and gap junction inhibitor, has the therapeutic potential of carbenoxolone in the research of chronic liver disease[2]. Carbenoxolone is a suitable candidate for the inhibition of Aβ42 aggregation and the therapeutic potential of Cbx against AD[1]. Carbenoxolone is small molecule Pannexin1 (Panx1,is an ATP release channel) inhibitor, attenuate Panx1 channel activity through modulation of the first extracellular loop[4].Carbenoxolone is an 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitor that converts inactive glucocorticoid into an active form. Carbenoxolone has antiviral activity against DENV infection targeting the virus itself[6].
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| Cat. No. |
Product Name |
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Classification |
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- HY-14200
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TVP1022; S-PAI
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Alkynes
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(S)-Rasagiline (TVP1022) is the relatively inactive S-enantiomer form of Rasagiline. Rasagiline is a highly potent selective irreversible MAO inhibitor with IC50s of 4.43 nM and 412 nM for rat brain MAO B and A activity, respectively . (S)-Rasagiline is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-116423
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Alkynes
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JH295 is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 inhibits cellular Nek2 via alkylation of Cys22. JH295 is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- HY-116423A
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Alkynes
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JH295 hydrate is a potent, irreversible and selective NIMA-related kinase 2 (Nek2) inhibitor with an IC50 of 770 nM. JH295 hydrate inhibits cellular Nek2 via alkylation of Cys22. JH295 hydrate is inactive against the mitotic kinases, Cdk1, Aurora B or Plk1, and does not perturb bipolar spindle assembly or the spindle assembly checkpoint . JH295 (hydrate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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| Cat. No. |
Product Name |
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Classification |
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- HY-W088066
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Phosphoric acid, sodium salt, hydrate (1:3:12)
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pH Modifiers
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Trisodium phosphate dodecahydrate is a corrosion inhibitor for iron in 0.1 M NaClO4, in both aerated and deaerated solutions. Trisodium phosphate dodecahydrate can be used as an excipient, such as pH regulator, buffer. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
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- HY-W011426
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Propan-2-yl hexadecanoate
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Solvents
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Isopropyl palmitate is an fatty acid ester. Isopropyl palmitate can be used for design and characterization of bioactive bilayer films. The bilayer membrane not only has the ability to scavenge free radicals and inhibit lipid peroxidation, but also can inhibit the growth of known foodborne pathogens. Isopropyl palmitate can be used as an excipient, such as lubricant, oily carrier, solvent, controlled-release transdermal film. Pharmaceutical excipients, or pharmaceutical auxiliaries, refer to other chemical substances used in the pharmaceutical process other than pharmaceutical ingredients. Pharmaceutical excipients generally refer to inactive ingredients in pharmaceutical preparations, which can improve the stability, solubility and processability of pharmaceutical preparations. Pharmaceutical excipients also affect the absorption, distribution, metabolism, and elimination (ADME) processes of co-administered drugs .
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