Search Result
Results for "
penetration inhibitor
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
7
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13011
-
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CH5424802; RO5424802; RG7853
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Anaplastic lymphoma kinase (ALK)
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Neurological Disease
Cancer
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Alectinib (CH5424802; RO5424802; RG7853) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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- HY-13318
-
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GS 4071; Ro 64-0802; Oseltamivir carboxylate
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Influenza Virus
Drug Metabolite
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Infection
Neurological Disease
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Oseltamivir acid (GS 4071), the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .
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- HY-100788
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2-PMPA
5 Publications Verification
2-(Phosphonomethyl)pentanedioic acid
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Carboxypeptidase
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Neurological Disease
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2-PMPA (2-(Phosphonomethyl)pentanedioic acid) is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA is applicable to the research of neurological diseases .
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- HY-101855
-
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Anle138b
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Amyloid-β
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Neurological Disease
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Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
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- HY-13011A
-
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CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride
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Anaplastic lymphoma kinase (ALK)
|
Neurological Disease
Cancer
|
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Alectinib (CH5424802; RO5424802; RG7853) Hydrochloride is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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- HY-17595
-
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Parasite
Apoptosis
Microtubule/Tubulin
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Infection
Cancer
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Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
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-
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- HY-12599
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-
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- HY-148811
-
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ICP-723
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c-Met/HGFR
Trk Receptor
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Cancer
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Zurletrectinib is a brain-penetrant, orally active TRK inhibitor (TRKA IC50 = 0.81 nM; TRKB IC50 = 0.145 nM; TRKC IC50 = 0.184 nM). Zurletrectinib exhibits stronger activity as a consequence of its augmented binding affinity for TRK kinases. Zurletrectinib exhibits higher activity against most TRK inhibitor resistance mutations (13 out of 18 mutations). Zurletrectinib can be used for the study of glioma .
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- HY-N2345
-
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Histone Acetyltransferase
Toll-like Receptor (TLR)
Androgen Receptor
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Inflammation/Immunology
Cancer
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Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .
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- HY-16712
-
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TGF-β Receptor
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Cancer
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LDN-214117 is an orally active ALK2 inhibitor with well-tolerated and good brain penetration. LDN-214117 has a high selectivity and low cytotoxicity for ALK2 with an IC50 value of 24 nM. LDN-214117 also is a specific bone morphogenetic proteins (BMPs) signaling inhibitor and has relatively selective inhibition for BMP6 with an IC50 value of 100 nM. LDN-214117 can be used for the research of fibrodysplasia ossificans progressiva (FOP), diffuse intrinsic pontine glioma (DIPG) .
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- HY-175715
-
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Mitochondrial Metabolism
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Neurological Disease
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NRG1271 is an orally active mitochondrial permeability transition pore (mPTP) inhibitor with blood-brain barrier penetration. NRG1271 can be used for the study of Neurological Disease .
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- HY-120619
-
|
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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BMS-193885 is a selective neuropeptide Y1 receptor antagonist (Ki=3.3 nM) that competitively blocks the receptor to inhibit NPY-mediated appetite regulation signaling pathways, reduce food intake and inhibit weight gain. BMS-193885 has good blood-brain barrier penetration and is mainly used in the study of obesity and related metabolic diseases .
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- HY-100788C
-
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2-(Phosphonomethyl)pentanedioic acid sodium
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Carboxypeptidase
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Neurological Disease
|
|
2-PMPA (2-(Phosphonomethyl)pentanedioic acid) sodium is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA sodium shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA sodium is applicable to the research of neurological diseases .
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- HY-130121
-
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OGA
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Neurological Disease
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MK-8719 is a highly potent and selective O-GlcNAcase (OGA) inhibitor (Ki=7.9 nM for hOGA) with excellent CNS penetration .
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- HY-B0848
-
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Environmental Pollutants
Bacterial
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Infection
Metabolic Disease
|
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Tricyclazole is a pentaketone melanin biosynthesis inhibitor and a unique fungicide for controlling rice blast. Tricyclazole alters the structure and function of fungal cell walls, reduces fungal pathogenicity and penetration, and causes dose-dependent liver damage in animals .
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-
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- HY-109189
-
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BPI-7711
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EGFR
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Cancer
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Rezivertinib (BPI-7711) is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib has excellent central nervous system (CNS) penetration and has antitumor activity .
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- HY-116578
-
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EXP999; RP9965
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Dopamine Receptor
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Neurological Disease
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Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
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- HY-131943
-
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Methylenetetrahydrofolate Dehydrogenase (MTHFD)
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Neurological Disease
Cancer
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DS44960156 is a selective MTHFD2 inhibitor with moderate to low blood-brain barrier penetration (IC50=1.6 μM, Ki=1.23 μM). DS44960156 specifically binds to the active site of MTHFD2, disrupts redox homeostasis and blocks serine-mediated one-carbon metabolism, thereby increasing the NAD +/NADH ratio and ROS levels. DS44960156 not only effectively inhibits the proliferation of glioma cells, but also enhances the sensitivity of cells to glutamine starvation-induced death. DS44960156 binds to plasma proteins, shows no mutagenicity, carcinogenicity or acute oral toxicity, and serves as a research agent for glioblastoma multiforme and other cancers .
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- HY-164782
-
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HDAC
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Neurological Disease
Metabolic Disease
Cancer
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PT3 is a selective inhibitor of HDAC3 with an IC50 value of 0.25 μM. PT3 exhibits good brain penetration ability and bioavailability upon oral administration. PT3 can be used in the research of Alzheimer’s disease .
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-
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- HY-100238
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-
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- HY-122559
-
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mGluR
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Neurological Disease
|
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BMS-984923, a potent mGluR5 silent allosteric modulator (SAM), with exquisite binding affinity (Ki = 0.6 nM), exhibits good oral bioavailability and BBB penetration. BMS-984923 potently inhibits the PrPC-mGluR5 interaction and prevents pathological Aβo signaling without affecting physiological glutamate signaling .
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- HY-147405
-
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PF-07284890; ARRY-461
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Raf
ERK
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Cancer
|
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Tinlorafenib (PF-07284890) is the orally active inhibitor for BRAF and CRAF with IC50s of 5.8 nM and 4.1 nM. Tinlorafenib (Compound 10) inhibits V600E mutated BRAF and V600K mutanted BRAF with IC50s of 4.25 nM and 2.7 nM. Tinlorafenib can cross the blood brain barrier. Tinlorafenib demonstrates CNS penetration and can be used in the research of BRAF-associated malignant and benign tumors of the CNS as well as extracranial malignancies .
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- HY-13318S
-
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GS 4071-d3; Ro 64-0802-d3; Oseltamivir carboxylate-d3
|
Isotope-Labeled Compounds
Influenza Virus
Drug Metabolite
|
Infection
|
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Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid (HY-13318). Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .
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-
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- HY-18060
-
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TC-5619
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nAChR
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Neurological Disease
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Bradanicline (TC-5619) is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
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- HY-138668
-
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TRP Channel
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Neurological Disease
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JW-65 is a selective TRPC3 channel inhibitor with favorable blood-brain barrier penetration. JW-65 directly binds to human TRPC3 protein and modulates calcium signaling to reduce seizure susceptibility. JW-65 reduces seizure incidence, severity, and duration while prolonging seizure latency in multiple seizure models. JW-65 alleviates Aβ‑induced neuronal damage. JW-65 serves as a valuable tool for research on epilepsy, seizure disorders, and Alzheimer’s disease .
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- HY-171955
-
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Lipoxygenase
Apoptosis
Reactive Oxygen Species (ROS)
FAK
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Cancer
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LXG6403 is an orally active and irreversible LOX inhibitor (IC50 = 1.3 μM). LXG6403 is ~3.5-fold more specific for LOX than LOXL2 and does not inhibit LOXL1. LXG6403 inhibits FAK signaling and induces ROS generation and DNA damage, leading to G1 arrest and apoptosis in chemoresistant triple-negative breast cancer (TNBC) cell lines. LXG6403 alters the extracellular matrix (ECM) and collagen structure, reducing collagen cross-linking and deposition, thereby increasing drug penetration and reducing tumor stiffness. LXG6403 overcomes Doxorubicin (HY-15142) resistance in chemoresistant TNBC PDX in vivo and can be used to study high-stiffness resistant tumors .
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- HY-101789
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Sodium Channel
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Neurological Disease
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Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration .
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- HY-W110888
-
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GLUT
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Neurological Disease
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Brilliant Yellow, a diazo-containing sulfonic aci, is also a potent VGLUT-specific inhibitor. Brilliant Yellow is membrane-impermeable. However, there are some Brilliant Yellow analogs with low cytotoxicity and cell penetration. Brilliant Yellow analogs work on glutamatergic transmission in hippocampal neurons .
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- HY-13011S
-
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CH5424802-d8; RO5424802-d8; AF802-d8
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Isotope-Labeled Compounds
Anaplastic lymphoma kinase (ALK)
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Cancer
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Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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- HY-148825
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-
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- HY-145313
-
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Tau Protein
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Neurological Disease
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TTBK1-IN-2 (compound 29) is a potent Tau-Tubulin kinase (TTBK1) inhibitor with IC50s of 0.24 and 4.22 µM, respectively. TTBK1-IN-2 reveals good brain penetration in vivo and is able to reduce TDP-43 phosphorylation not only in cell cultures but also in the spinal cord of transgenic TDP-43 mice .
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- HY-175278
-
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NOD-like Receptor (NLR)
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Neurological Disease
Inflammation/Immunology
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BAL-1516 is an orally active NLRP3 inhibitor with human NLRP3 Kd of 14.2 nM, mouse NLRP3 Kd of 200 nM, and blood-brain barrier penetration.BAL-1516 binds to a surface groove of the NLRP3 nucleotide-binding domain, contacts FISNA and WHD subdomains, forms three hydrogen bonds to the peripheral β-strand of the triple-ATPase, and does not alter NLRP3 ATP-hydrolysis activity.BAL-1516 shows specificity for NLRP3 over other NOD-like receptors, directly binds mouse NLRP3, and inhibits inflammasome formation in monocytes and microglia .
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- HY-161275
-
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EGFR
Akt
ERK
Ribosomal S6 Kinase (RSK)
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Cancer
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BI-4732 is an orally active, reversible, ATP-competitive EGFR inhibitor with blood-brain barrier penetration. BI-4732 inhibits the kinase activity of EGFR L858R, T790M and C797S with IC50 values of 1 nM while sparing EGFR wild-type. BI-4732 inhibits EGFR and reduces the phosphorylation of AKT, ERK, and S6K. BI-4732 demonstrates excellent intracranial anti-tumor efficacy in YU-1097 xenograft model harboring EGFR_E19del/T790M/C797S. BI-4732 can be used for the study of non-small cell lung cancer (NSCLC) .
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- HY-10096
-
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GSK-3
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Neurological Disease
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TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
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- HY-N12614
-
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SHP1
Phosphatase
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Metabolic Disease
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Diorcinol is a potent SHP1 inhibitor with an IC50 value of 0.96 μM. Diorcinol can be isolated from Aspergillus sydowii. Diorcinol has good blood-brain barrier penetration and can be used for diabetes research .
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- HY-167876
-
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PI3K
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Cancer
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PQR514 is a potent PI3K inhibitor with anticancer activity. PQR514 is able to inhibit cancer cell proliferation. PQR514 showed significant antitumor activity in the OVCAR-3 xenograft model, with the required concentration being approximately one-eighth that of PQR309. PQR514 has good pharmacokinetic properties and minimal brain penetration, making it an optimized candidate compound for inhibiting systemic tumors .
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- HY-17595R
-
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Reference Standards
Parasite
Apoptosis
Microtubule/Tubulin
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Infection
Cancer
|
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Mebendazole (Standard) is the analytical standard of Mebendazole. This product is intended for research and analytical applications. Mebendazole is a highly effective, broad-spectrum antihelmintic against nematode infestations. Mebendazole also exhibits inhibitory effect against glioblastoma multiforme (GBM), inhibits Hedgehog pathway and tubulin polymerization. Mebendazole is orally active and can cross CNS penetration .
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- HY-108460
-
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TRP Channel
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Neurological Disease
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A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .
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- HY-13011AR
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CH5424802 Hydrochloride (Standard); RO5424802 Hydrochloride (Standard); AF-802 Hydrochloride (Standard)
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Anaplastic lymphoma kinase (ALK)
Reference Standards
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Cancer
|
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Alectinib (Hydrochloride) (Standard) is the analytical standard of Alectinib (Hydrochloride). This product is intended for research and analytical applications. Alectinib Hydrochloride (CH5424802 Hydrochloride; RO5424802 Hydrochloride; AF-802 Hydrochloride) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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- HY-W395779
-
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Filovirus
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Infection
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EBOV-IN-1 (com 3.47) is an adamantane dipeptide piperazine and an inhibitor of Ebola virus (EBOV). EBOV-IN-1 targets Niemann-Pick C1 (NPC1) and inhibits its binding to the EBOV glycoprotein (GP) that activates and mediates viral penetration into host cells, thereby inhibiting EBOV infection. EBOV-IN-1 inhibits pseudotyped EBOV infection with an IC50 of 13 nM .
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- HY-115925
-
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SHP2
Phosphatase
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Cancer
|
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SHP2-IN-9 is a specific SHP2 inhibitor (IC50 =1.174 μM) with enhanced blood–brain barrier penetration. SHP2-IN-9 shows 85-fold more selective for SHP2 than SHP1. SHP2-IN-9 inhibits SHP2-mediated cell signal transduction and cancer cell proliferation, and inhibits the growth of cervix cancer tumors and glioblastoma growth in vivo .
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- HY-10104
-
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Beta-secretase
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Neurological Disease
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GRL-8234 is a potent β-secretase (BACE1) inhibitor with blood-brain barrier penetration (Ki = 1.8 nM). GRL-8234 can rescue age-related cognitive decline in Tg2576 mice. GRL-8234 can be used in the research related to Alzheimer's disease (AD) .
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-
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- HY-139300A
-
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HMPL-813 succinate
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EGFR
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Cancer
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Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) 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-102043
-
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Phosphodiesterase (PDE)
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Neurological Disease
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PDM-631 is a selective and orally active PDE2A inhibitor with blood-brain barrier penetration. PDM-631 exhibits potent inhibitory activity against human and rat recombinant PDE2A with IC50 values of 1.5 nM and 4.2 nM, respectively. PDM-631 increases cGMP levels in the rat cerebral cortex. PDM-631 can be used for the study of schizophrenia and neurodegenerative disorders .
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- HY-W010203
-
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Fungal
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Infection
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2-Decanone is an antifungal agent. 2-Decanone inhibits pathogen mycelial growth, spore germination, and appressorium formation. 2-Decanone downregulates spore germination-related genes (MfBmp1) and penetration structure formation genes (MfPls1), inducing reactive oxygen species (ROS) accumulation to trigger mitochondrial damage and subsequent spore apoptosis. 2-Decanone is promising for research of postharvest disease control in fruits and vegetables .
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- HY-126047
-
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NF-κB
Beta-secretase
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Neurological Disease
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(S)-(-)-Anatabine is an NFκB/BACE-1 inhibitor with blood-brain barrier penetration. (S)-(-)-Anatabine inhibits NFκB activation via phosphorylation of its p65 subunit. (S)-(-)-Anatabine inhibits BACE-1 transcription and reduces BACE-1 protein levels. (S)-(-)-Anatabine lowers production of Aβ1-40 and Aβ1-42 by reducing β-cleavage of amyloid precursor protein without affecting α-cleavage. (S)-(-)-Anatabine can be used for the research of Alzheimer's disease .
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- HY-144389
-
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Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
|
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hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD) .
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- HY-100788R
-
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2-(Phosphonomethyl)pentanedioic acid (Standard)
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Reference Standards
Carboxypeptidase
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Neurological Disease
|
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2-PMPA (2-(Phosphonomethyl)pentanedioic acid) Standard is the analytical standard of 2-PMPA (HY-100788). This product is intended for research and analytical applications. 2-PMPA (2-(Phosphonomethyl)pentanedioic acid) sodium is a glutamate carboxypeptidase II (GCPII) inhibitor with an IC50 of 0.0003 μM. 2-PMPA sodium shows low blood-brain barrier penetration. 2-PMPA sodium blocks the hydrolysis of NAAG, regulates glutamate levels in the brain and neurovascular coupling. 2-PMPA sodium is applicable to the research of neurological diseases.
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- HY-174811
-
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PROTACs
Epigenetic Reader Domain
PD-1/PD-L1
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Inflammation/Immunology
Cancer
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PROTAC BRD4 Degrader-33 is an enzyme activated clickable BRD4 PROTAC degrader with favorable tumor microenvironment-response. PROTAC BRD4 Degrader-33 has superior tumor tissue penetration capabilities and efficiently inhibits PD-L1 protein expression. PROTAC BRD4 Degrader-33 shows potent anti-tumoral immunomodulation activity in 4T1 tumor-bearing mice model . Pink: BRD4 ligand (HY-174812); Blue: CRBN ligase ligand (HY-10984); Black: linker
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- HY-167927
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CVL218
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PARP
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Cancer
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Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
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- HY-114320
-
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TM-10
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Cholinesterase (ChE)
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Neurological Disease
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BuChE-IN-TM-10 (TM-10) is a potent butyrylcholinesterase (BuChE) inhibitor, with an IC50 of 8.9 nM. BuChE inhibitor 1 inhibits and disaggregates self-induced Aβ aggregation, exhibiting potent antioxidant activity and good blood-brain barrier (BBB) penetration. Has potential to treat Alzheimer’s disease .
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- HY-168563
-
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Cholinesterase (ChE)
FAAH
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Neurological Disease
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BuChE-IN-15 (compound D12) is a selective BuChE/FAAH dual inhibitor with and show IC50 values of 81 and 400 nM for hBuChE and hFFAH, respectively. BuChE-IN-15 possesses good BBB penetration, and shows neuroprotection.BuChE-IN-15 can be used for study of Alzheimer .
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- HY-10550B
-
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XR9576 dimesylate
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P-glycoprotein
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Cardiovascular Disease
Others
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Tariquidar dimesylate (XR9576 dimesylate) is a P-glycoprotein (P-gp) inhibitor. Tariquidar dimesylate increases the concentration of the drug in the brain by binding to P-glycoprotein, preventing it from transporting the drug from inside to outside the brain. Tariquidar dimesylate can be used in the study of blood-brain barrier penetration and multidrug resistance .
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- HY-15112
-
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Prolyl Endopeptidase (PREP)
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Infection
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JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096) .
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- HY-13011S1
-
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CH5424802-d6; RO5424802-d6; AF802-d6
|
Isotope-Labeled Compounds
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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-
- HY-13011R
-
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CH5424802 (Standard); RO5424802 (Standard); RG7853 (Standard)
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Reference Standards
Anaplastic lymphoma kinase (ALK)
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Cancer
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Alectinib (CH5424802; RO5424802; RG7853) (Standard) is the analytical standard of Alectinib. This product is intended for research and analytical applications. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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-
- HY-181067
-
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MEK
ERK
|
Cancer
|
|
IK-595 is a MEK1/MEK2 inhibitor with high affinity (7.39 nM).IK-595 blocks EGF-induced ERK1/2 phosphorylation in AsPC-1 cells with IC50 value of 0.1 nM. IK-595 has oral activity and blood-brain barrier penetration. IK-595 can be used for the research of Ras/MAPK pathway-altered cancers .
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-
- HY-175299
-
|
|
Hedgehog
Apoptosis
DNA Methyltransferase
|
Cancer
|
|
Hedgehog IN-11 is an orally active Hedgehog inhibitor. Hedgehog IN-11 downregulates the expression of O6-methylguanine-DNA methyltransferase (MGMT) to impair the Temozolomide (TMZ) (HY-17364) resistance by inhibiting the Hedgehog pathway. Hedgehog IN-11 shows improved inhibition of cell migration and invasion, and induced cell apoptosis in TMZ-resistant GBM cell lines. Hedgehog IN-11 is predicted by computer simulation to have good blood-brain barrier penetration. Hedgehog IN-11 can be used for the study of glioblastoma (GBM) .
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-
- HY-105369
-
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|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
KF-20444 is an orally active ALK inhibitor with blood-brain barrier penetration. KF-20444 exhibits strong inhibitory activity against ALK fusion proteins (EML4-ALK) and ALK resistance mutations (including L1196M, G1202R, and F1174L). KF-20444 effectively suppresses the phosphorylation of ALK in ALK-driven cancer cell lines, thereby inhibiting cancer cell proliferation and inducing apoptosis. KF-20444 demonstrates anti-tumor efficacy in mouse models bearing ALK-positive non-small cell lung cancer (NSCLC) or neuroblastoma. KF-20444 can be used for the study of ALK-driven malignancies .
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-
- HY-115727
-
-
- HY-117776
-
|
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ICMT
|
Cancer
|
|
CAY10677 (compound 15) is a potent ICMT inhibitor that inhibits cancer cell proliferation. CAY10677 has good PAMPA penetration .
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-
- HY-101076
-
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|
Phosphatase
|
Metabolic Disease
|
|
L-690488 is a proagent of L-690330 and is a selective inositol monophosphatase (IMPase) inhibitor. L-690488 has more effective cell penetration than L-690330 .
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-
- HY-152632
-
|
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Cholinesterase (ChE)
|
Neurological Disease
|
|
BuChE-IN-7 is a highly selective inhibitor of hBuChe and eqBuChE with IC50 values of 40 nM, 80 nM respectively. BuChE-IN-7 can promote cognitive with blood-brain penetration and improves situational and phobic memory, showing preference for new things .
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-
- HY-147013
-
|
|
Influenza Virus
Orthopoxvirus
|
Infection
|
|
Caprochlorone has antiviral activity against orthopoxvirus. Caprochlorone can inhibit cell penetration by virus, also delays release of newly formed virus from the cell. Caprochlorone decreases the titers of influenza virus in infected-mice lungs .
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-
- HY-168241
-
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Cholinesterase (ChE)
5-HT Receptor
|
Infection
|
|
Flucopride (Compound 4a) is an AChE inhibitor (IC50: 24 nM), and a partial 5-HT4R agonist (Ki: 9.6 nM for (h)5-HT4R). Flucopride promotes the non-amyloidogenic processing of APP in COS-7 transiently expressing (h)5-HT4R (EC50: 23.0 nM). Flucopride may has good gastrointestinal track (GIT) penetration, and blood-brain barrier (BBB) cross-membrane penetration (PAMPA assay) .
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-
- HY-10030
-
|
PF-2545920 succinate
|
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
Mardepodect succinate (PF-2545920 succinate) is a potent and specific phosphodiesterase 10A (PDE10A) inhibitor with potential activity in the treatment of schizophrenia. Mardepodect succinate has been further optimized to improve brain penetration and compound-like properties for use in schizophrenia research .
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-
- HY-119063
-
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Carbonic Anhydrase
|
Others
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|
L-645151 is a carbonic anhydrase inhibitor with ocular penetration and hypotensive activity. L-645151 lowers the elevated intraocular pressure (IOP) of o-chymotripsinized (o-CT) rabbit eyes. L-645151 is promising for research of an ocular hypotensive agent .
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-
- HY-161380
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 96 (Compound WZ-2) is an antifungal agent with good blood-brain barrier permeability and brain penetration. Antifungal agent 96 inhibits the growth of C. neoformans H99 and C. albicans 0304103 with MIC values of 0.016 and 32 μg/mL, respectively .
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-
- HY-167927S
-
|
|
Isotope-Labeled Compounds
PARP
|
Cancer
|
|
Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
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-
- HY-161029
-
|
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Cholinesterase (ChE)
|
Neurological Disease
|
|
T14-A24 is an orally active, reversible, competitive, and selective AChE inhibitor (Ki=22 nM, IC50=6 nM). T14-A24 has benign BBB penetration, remarkable neuroprotective effect, and safe toxicological profile .
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-
- HY-163131
-
|
|
Glucosylceramide Synthase (GCS)
|
Neurological Disease
|
|
Glucosylceramide synthase-IN-4 (compound 12) is a potent glucosylceramide synthase (GCS) inhibitor, with an IC50 of 6.8 nM. Glucosylceramide synthase-IN-4 shows excellent PK properties and stability in human hepatocytes. Glucosylceramide synthase-IN-4 has good CNS penetration and acceptable PXR selectivity .
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-
- HY-143413
-
|
|
Amyloid-β
|
Neurological Disease
Inflammation/Immunology
|
|
BuChE-IN-2 is an excellent butyrylcholinesterase (BuChE) inhibitor (IC50s of 1.28 μM and 0.67 μM for BuChE and NO). BuChE-IN-2 can inhibit the aggregation of Aβ, ROS formation and chelate Cu 2+, exhibiting proper blood-brain barrier (BBB) penetration. BuChE-IN-2 has potential to research Alzheimer’s disease .
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-
- HY-144695
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-1 (Compound b1) is a dual Dyrk1A and α-synuclein aggregation inhibitor with IC50 values of 177 nM and 10.5 µM, respectively. Dyrk1A/α-synuclein-IN-1 has high predictive CNS penetration and neuroprotective effect .
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-
- HY-144696
-
|
|
DYRK
|
Neurological Disease
|
|
Dyrk1A/α-synuclein-IN-2 (Compound b20) is a dual Dyrk1A and α-synuclein aggregation inhibitor with an IC50 of 7.8 µM for α-synuclein. Dyrk1A/α-synuclein-IN-2 has high predictive CNS penetration and neuroprotective effect .
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-
- HY-174381
-
|
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Cholinesterase (ChE)
Amyloid-β
Tau Protein
|
Neurological Disease
|
|
BChE-IN-41 is a highly selective Butyrylcholinesterase (BChE) inhibitor (IC50 =12 nM, Ki = 6.6 nM). BChE-IN-41 has high brain penetration with a brain-to-plasma ratio of 9.0. BChE-IN-41 has pro-cognitive effects on mice with AD-like symptoms induced by Scopolamine (HY-N0296) and Aβ1-42 .
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-
- HY-14205
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
NW-1772 (methanesulfonate) (compound 22b) is a potent and selective monoamine oxidase (MAO) B inhibitor. NW-1772 has some advantages, such as rapid blood-brain barrier penetration, short-acting and reversible inhibitory activity, slight inhibition of selected cytochrome P450s, and low in vitro toxicity. NW-1772 can be used for the research of neurodegenerative diseases .
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-
- HY-163514
-
|
|
Cholinesterase (ChE)
DYRK
|
Neurological Disease
|
|
hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research .
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-
- HY-152171
-
|
|
Monoamine Transporter
|
Neurological Disease
|
|
GZ-11608 is a potent and selective vesicular monoamine transporter-2 (VMAT2) inhibitor with high affinity (Ki = 25 nM). GZ-11608 decreases methamphetamine-induced dopamine release from isolated synaptic vesicles from brain dopaminergic neurons. GZ-11608 exhibits rapid brain penetration and without neurotoxicity. GZ-11608 can be used for the research of methamphetamine use disorder .
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-
- HY-147999
-
|
|
Bacterial
Fungal
Cytochrome P450
|
Infection
|
|
GlcN-6-P Synthase-IN-1 (Compound 4d) is a Glucosamine-6-phosphate (GlcN-6-P) synthase inhibitor with an IC50 of 3.47 μM. GlcN-6-P Synthase-IN-1 exhibits significant antimicrobial activity. GlcN-6-P Synthase-IN-1 has good penetration in the CNS and is able to inhibit the cytochrome P450, CYP3A4 isoform .
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-
- HY-156736
-
|
|
17β-HSD
|
Cancer
|
|
HSD17B13-IN-3 (compound 2) is a potent hydroxysteroid 17ß-dehydrogenase 13 (HSD17B13) inhibitor with IC50s of 0.38 μM and 0.45 μM in biochemical assays using both β-estradiol or Leukotriene B4 (LTB4) as substrate and NAD + as cofactor. HSD17B13-IN-3 shows low cell penetration .
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-
- HY-18060A
-
|
TC-5619 hydrochloride
|
nAChR
|
Neurological Disease
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline hydrochloride exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline hydrochloride possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline hydrochloride requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline hydrochloride is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
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-
- HY-N2345R
-
|
|
Reference Standards
Histone Acetyltransferase
Toll-like Receptor (TLR)
Androgen Receptor
|
Inflammation/Immunology
Cancer
|
|
Procyanidin B3 (Standard) is the analytical standard of Procyanidin B3. This product is intended for research and analytical applications. Procyanidin B3 is a natural product with antioxidant activity and oral bioavailability, possessing good blood-brain barrier penetration. Procyanidin B3 is a selective inhibitor of histone acetyltransferase (HAT). By inhibiting p300 HAT-mediated acetylation of the androgen receptor (androgen receptor). Procyanidin B3 alleviates intervertebral disc degeneration (IVDD) by inhibiting the formation of the TLR4/MD-2 complex. Procyanidin B3 can be used in research on prostate cancer and arthritis .
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-
- HY-143994S
-
|
|
Isotope-Labeled Compounds
Dopamine Receptor
|
Neurological Disease
|
|
Metopimazine-d6 hydrochloride is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
|
-
- HY-144388
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and Aβ1-42 aggregation inhibitor with IC50s of 0.062, 0.767 and 1.227 µM for AChE, BuChE and Aβ1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent .
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-
- HY-175648
-
|
|
Parasite
|
Infection
|
|
Antiparasitic agent-28 is an orally active, selective inhibitor of Toxoplasma gondii phenylalanine tRNA synthetase (TgcPheRS) with blood-brain barrier penetration. Antiparasitic agent-28 inhibits the growth of T. gondii tachyzoites (TgME49-Fluc strain) an (EC50 = 1 nM) and T. gondii bradyzoites (Tg68nLuc strain) induced by alkaline (EC50 = 3 nM) and glutamine-rich medium (EC50 = 0.1 nM). Antiparasitic agent-28 demonstrates potent anti-toxoplasmosis efficacy in mice infected with TgME49-Fluc tachyzoites. Antiparasitic agent-28 can be used for the study of Toxoplasma gondii infection .
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-
- HY-159958
-
|
|
Potassium Channel
|
Neurological Disease
|
|
KNa1.1-IN-2 (Compound Z05) is a selective KNa1.1 channel inhibitor with blood-brain barrier penetration, particularly effective against the hERG channel. KNa1.1-IN-2 works by binding to the KNa1.1 channel and blocking the channel activity induced by Gain-of-function (GOF) mutations, effectively intervening in KCNT1-related epilepsy. Additionally, KNa1.1-IN-2 inhibits the GOF mutant Y796H. KNa1.1-IN-2 holds promise for research into KCNT1-related epilepsy disorders .
|
-
- HY-203862
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Polyquaternium-51 is a hydrophilic polymeric zwitterion with counter ions, and an artificial cell membrane-mimicking material with high biocompatibility. Polyquaternium-51 functions as a penetration inhibitor and exfoliation efficacy reducer. Polyquaternium-51 can be used as cosmetic moisturizing ingredient, and can be used as coating biological scaffolds .
|
-
- HY-N9722
-
|
|
HSP
|
Cancer
|
|
Dehydroherbarin is a selective inhibitor targeting HSP90α with blood-brain barrier penetration. Dehydroherbarin interferes with key pathways of tumor cell survival by binding to HSP90α, while exerting moderate antibacterial and anti-hepatitis A virus activities and inhibiting tumor cell migration. Dehydroherbarin can be used in research on tumors such as breast cancer .
|
-
- HY-182358
-
|
|
Apoptosis
|
Cancer
|
|
TMLZ-G46 is an orally active ZNF207 inhibitor with blood-brain barrier penetration ability, with a Kd value of 68 nM. TMLZ-G46 inhibits cancer cell proliferation, stemness, migration and invasion, induces G0/G1 cell cycle arrest and apoptosis, and suppresses colony formation. TMLZ-G46 can be used in glioma research .
|
-
- HY-109189A
-
|
BPI-7711 hydrochloride
|
EGFR
|
Cancer
|
|
Rezivertinib (BPI-7711) hydrochloride is an orally active, highly selective and irreversible third-generation EGFR tyrosine kinase inhibitor (TKI). Rezivertinib hydrochloride exhibits high potency against the common activation EGFR and the resistance T790M mutations. Rezivertinib hydrochloride has excellent central nervous system (CNS) penetration and has antitumor activity, such as non-small cell lung cancer (NSCLC) .
|
-
- HY-101789R
-
|
|
Reference Standards
Sodium Channel
|
Neurological Disease
|
|
Nav1.7-IN-3 (Standard) is the analytical standard of Nav1.7-IN-3 (HY-101789). This product is intended for research and analytical applications. Nav1.7-IN-3 is a selective, orally bioavailable voltage-gated sodium channel Nav1.7 inhibitor with an IC50 of 8 nM. Pain relief. Limited CNS penetration .
|
-
- HY-100238R
-
-
- HY-183805
-
|
|
5-HT Receptor
FAAH
|
Neurological Disease
|
|
5-HT6R/FAAH modulator 2 is a dual 5-HT6R antagonist and FAAH inhibitor with human 5-HT6R pKi 7.24, human FAAH pIC50 5.47, and blood-brain barrier penetration.5-HT6R/FAAH modulator 2 modulates serotonergic signaling, blocks 5-HT6R function, inhibits endocannabinoid degradation via FAAH catalytic activity suppression.5-HT6R/FAAH modulator 2 exhibits neuroprotective effects against mitochondrial dysfunction, amyloid-β, and glutamate-induced toxicity, reverses memory deficits.5-HT6R/FAAH modulator 2 shows reduced cytotoxicity relative to oxygen-containing lead compounds.5-HT6R/FAAH modulator 2 can be used for the research of Alzheimer's disease .
|
-
- HY-101855R
-
|
Anle138b (Standard)
|
Reference Standards
Amyloid-β
|
Neurological Disease
|
|
Emrusolmin (Standard) (Anle138b (Standard)) is the analytical standard of Emrusolmin (HY-101855). This product is intended for research and analytical applications. Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
|
-
- HY-18060B
-
|
TC-5619 tosylate
|
nAChR
|
Inflammation/Immunology
|
|
Bradanicline (TC-5619) tosylate is an orally active agonist of α7 nAChR with moderate blood-brain barrier penetration. Bradanicline tosylate exhibits high affinity and subtype selectivity for human α7 nAChR. Bradanicline tosylate possesses antitussive activity that depends on sustained receptor binding and activation. Bradanicline tosylate requires systemic administration to dose-dependently inhibit cough induced by citric acid, bradykinin and inhaled nicotine. Bradanicline tosylate is well tolerated in preclinical studies and is widely used in research related to chronic refractory cough .
|
-
- HY-108460R
-
|
|
Reference Standards
TRP Channel
|
Neurological Disease
|
|
A-784168 (Standard) is the analytical standard of A-784168 (HY-108460). This product is intended for research and analytical applications. A-784168 is a potent and orally active inhibitor of vanilloid receptor type 1 (TRPV1). Vanilloid receptor type 1 (TRPV1) is a ligand-gated nonselective cation channel that is considered to be an important integrator of various pain stimuli such as endogenous lipids, capsaicin, heat, and low pH. A-784168 has good CNS penetration .
|
-
- HY-106021
-
|
ILX651 free base
|
Microtubule/Tubulin
Prolyl Endopeptidase (PREP)
|
Cancer
|
|
Tasidotin (ILX651 free base) is a tubulin inhibitor and competitive Prolyl Endopeptidase (PREP) inhibitor, with an IC50 of 10 μM against bovine tubulin. Tasidotin exhibits high cerebrospinal fluid penetration in non-human primates. Tasidotin antagonizes microtubule assembly and induces an extended assembly lag phase, thereby inhibiting mitosis and cell proliferation, and exerts cytotoxic and oncolytic effects on cancer cells. Tasidotin is metabolized into polypeptides and proline inside cells, and its in vivo metabolism is mediated by prolyl endopeptidase. Tasidotin can be applied in research related to Burkitt's lymphoma, breast cancer, leukemia, melanoma, central nervous system malignancies and various solid tumors .
|
-
- HY-181711
-
|
|
NO Synthase
|
Neurological Disease
Cancer
|
|
nNOS-IN-6 is a human neuronal nitric oxide synthase (hnNOS) inhibitor with a human hnNOS Ki of 16 nM, ~1800-fold selectivity over human eNOS, ~2900-fold selectivity over human iNOS, and a rat nNOS Ki of 34 nM.nNOS-IN-6 exhibits high effective permeability in PAMPA-BBB assays, crosses the blood-brain barrier, and shows sustained systemic exposure, low clearance, and robust brain penetration in mouse in vivo pharmacokinetic studies.nNOS-IN-6 can be used for the research of neurodegenerative diseases, melanoma .
|
-
- HY-175824
-
|
|
iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
|
|
PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
|
-
- HY-W010203S1
-
|
|
Isotope-Labeled Compounds
Fungal
|
Infection
|
|
2-Decanone-d5-1 is the deuterium labeled 2-Decanone (HY-W010203). 2-Decanone is an antifungal agent. 2-Decanone inhibits pathogen mycelial growth, spore germination, and appressorium formation. 2-Decanone downregulates spore germination-related genes (MfBmp1) and penetration structure formation genes (MfPls1), inducing reactive oxygen species (ROS) accumulation to trigger mitochondrial damage and subsequent spore apoptosis. 2-Decanone is promising for research of postharvest disease control in fruits and vegetables .
|
-
- HY-P10861
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 can be used for research on tau-related diseases such as Alzheimer's disease .
|
-
- HY-P10861A
-
|
|
Tau Protein
|
Neurological Disease
|
|
RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 acetate inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 acetate mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 acetate suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 acetate can be used for research on tau-related diseases such as Alzheimer's disease .
|
-
- HY-184078
-
|
|
Drug Derivative
Indoleamine 2,3-Dioxygenase (IDO)
Tau Protein
iGluR
|
Neurological Disease
|
|
8-F-2-(Me-Pip-Me)-Tryptanthrin is a tryptanthrin derivative with blood-brain barrier penetration. 8-F-2-(Me-Pip-Me)-Tryptanthrin protects neurons from Aβ-induced apoptosis, inhibits Aβ-induced Tau protein hyperphosphorylation and neuronal synaptic damage, and improves learning and memory abilities in Alzheimer's disease mice. 8-F-2-(Me-Pip-Me)-Tryptanthrin can be used for the research of nervous system diseases, including diseases related to abnormal Tau protein phosphorylation and abnormal PSD-95 function .
|
-
- HY-123859
-
|
|
Casein Kinase
FLT3
CDK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
SR-2890 is a highly selective, ATP-competitive inhibitor of casein kinase CK1δ and CK1ε, with IC50 values of 4 nM and 44 nM, respectively, and a Ki of 14 nM for CK1δ. SR-2890 exhibits antiproliferative effects. SR-2890 blocks the serine/threonine kinase activity of CK1δ and weakly inhibits a few off-target kinases such as FLT3, CDK4. SR-2890 has an oral bioavailability of 10% and a blood-brain barrier penetration rate of <1%. SR-2890 demonstrates stable in vitro metabolism and favorable in vivo pharmacokinetic properties, effectively inhibiting the growth of human A375 melanoma cells. SR-2890 can be used in melanoma research and is also a useful compound for studying CK1δ/ε-related diseases such as Alzheimer's disease .
|
-
- HY-177477
-
|
|
Drug Derivative
Cadherin
β-catenin
|
Cardiovascular Disease
Cancer
|
|
2,5-Epidithia-3,6-dioxopiperazine (Formula 15) is a derivative of Epidithiodioxopiperazine (ETP). 2,5-Epidithia-3,6-dioxopiperazine improves intracellular penetration and restores the activity of 2-Cys-Prx (especially Peroxiredoxin II (PrxII)) of form simulation in cells. 2,5-Epidithia-3,6-dioxopiperazine inhibits PDGF-induced proliferation and migration in vascular smooth muscle cells while promoting these actions in endothelial cells with VEGF induction. 2,5-Epidithia-3,6-dioxopiperazine effectively inhibits the proliferation and migration and lung metastasis of melanoma cells. 2,5-Epidithia-3,6-dioxopiperazine can be used for vascular diseases such as hypertension, angina pectoris and myocardial infarction research .
|
-
- HY-182060
-
|
|
Phosphodiesterase (PDE)
Bcl-2 Family
NO Synthase
Apoptosis
|
Inflammation/Immunology
|
|
PDE4B/D-IN-5 (Compound P32) is a peripherally restricted, oral active inhibitor of PDE4B and PDE4D with extremely low blood-brain barrier penetration, with IC50 values of 3.4 nM and 2.2 nM, respectively. PDE4B-IN-8 inhibits the production of TNF-α. PDE4B/D-IN-5 significantly reduces the Bax/Bcl2 ratio, and alleviates oxidative stress by decreasing MPO activity and NO levels. PDE4B/D-IN-5 exhibits anti-inflammatory, antioxidant, and anti-apoptotic activities. PDE4B/D-IN-5 can be used for the research of acute lung injury .
|
-
- HY-116578S
-
|
EXP999-d6; RP9965-d6
|
Isotope-Labeled Compounds
Dopamine Receptor
|
Neurological Disease
|
|
Metopimazine-d6 (EXP999-d6; RP9965-d6) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
|
-
- HY-103504
-
|
|
GABA Receptor
|
Neurological Disease
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(S)-SNAP5114 is a non-covalent murine GABA transporter inhibitor with blood-brain barrier penetration ability, which exhibits significant subtype-selective inhibitory activity against mGAT4 (pIC50=5.71, pKi=4.56), much higher than its effects on mGAT1, mGAT2 and mGAT3. (S)-SNAP5114 elevates extracellular GABA concentrations by blocking the GABA reuptake mechanism, thereby enhancing thalamus-specific GABAergic signaling and exerting potential neuromodulatory effects. (S)-SNAP5114 is widely used in studies related to epilepsy, neuropathic pain, anxiety and depression, and various neurodegenerative diseases .
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- HY-175188
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BPN-0027490
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Myosin
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Neurological Disease
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MT-110 (BPN-0027490) is a non-muscle myosin NMIIB-selective inhibitor with high brain penetration and favorable safety profile. MT-110 specifically disrupts NMIIB-dependent actin dynamics in dendritic spines, while it exerts no significant adverse effects on cardiac myosin II and cardiac functions (such as cardiac output and heart rate) at tested concentrations. A single administration of MT-110 produces long-lasting (sustained for several weeks) blockade of methamphetamine motivation associated with environmental cues. MT-110 exhibits extremely high specificity, with no interference with cocaine motivation, hippocampus-dependent memory, fear memory, or locomotor and anxiety-like behaviors. MT-110 serves as a valuable tool compound for investigating the mechanisms of methamphetamine use disorder .
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- HY-179227
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HDAC
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Neurological Disease
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HDAC6 ligand-7 (Compound 16a) is a positron emission tomography (PET) tracer for the deacetylase 6 (HDAC6) enzyme with a Kd value of 1.66 nM. HDAC6 ligand-7 exhibits excellent HDAC6 inhibitory activity, with IC50 values of 2.7 and 3.7 nM for hHDAC6 and mHDAC6, respectively, and has high selectivity for HDAC1/4/7/8. HDAC6 ligand-7 after being radioactively labeled with fluorine-18, [¹⁸F]HDAC6 ligand-7 shows varying degrees of radioactive uptake in PET, which can reflect the specific binding to HDAC6. HDAC6 ligand-7 can be used for the study of HDAC6 imaging .
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- HY-184021
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CD38
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Neurological Disease
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A-8531 is an orally active CD38 inhibitor with IC50 values of 1.10 nM against human CD38, IC50 values of 2.93 nM against mouse CD38, and a human Ka of 0.32 nM. A-8531 exerts its inhibitory activity via its 4-pyridine reactive warhead interacting with the CD38 substrate NAD +, and binds stably to CD38 only in the presence of NAD +, with a binding KD of 0.32 nM as detected by SPR. A-8531 dose-dependently increases NAD + levels in mouse skin, lung and liver tissues, while simultaneously reducing the contents of NAM and ADPR in these tissues. A-8531 derivative A-3190 (HY-184206) has blood-brain barrier penetration. A-8531 can be used in studies related to neurodegenerative diseases .
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- HY-175675
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P2Y Receptor
Keap1-Nrf2
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Cardiovascular Disease
Neurological Disease
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P2Y1 antagonist 4 is a selective P2Y1 receptor antagonist with excellent blood-brain barrier (BBB) penetration.
P2Y1 antagonist 4 inhibits P2Y1 receptor-mediated cytosolic Ca 2+ increase (IC50 = 1.95 μM) and platelet aggregation (IC50 = 3.24 μM) induced by ADP in rabbit washed platelets. P2Y1 antagonist 4 significantly upregulates the level of nuclear Nrf2 protein in H2O2-treated HT22 cells. P2Y1 antagonist 4 reduces myocardial infarct size in a mouse acute myocardial infarction (MI) model. P2Y1 antagonist 4 can be used for the study of ischemic stroke and myocardial infarction .
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- HY-P10914
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MDM-2/p53
Autophagy
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Inflammation/Immunology
Cancer
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D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
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- HY-185743
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Antibody-Drug Conjugates (ADCs)
Folate Receptor (FR)
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Cancer
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ZW-191 is an antibody-drug conjugate (ADC) targeting folate receptor α (FRα). ZW-191 consists of ZW-191 Antibody (HY-P992515) as the antibody component and MC-GGFG-AM-(10Me-11F-Camptothecin) (HY-153360) as the linker-payload component. ZW-191 possesses excellent tumor sphere penetration, cellular internalization and payload delivery capabilities, and can release a topoisomerase 1 inhibitor inside tumor cells to inhibit tumor cell activity. ZW-191 exerts a potent bystander effect on both antigen-positive and antigen-negative cells. ZW-191 exhibits prominent activity in xenograft models of cell lines with different FRα expression levels. ZW-191 can be used in studies related to ovarian cancer, non-small cell lung cancer, endometrial cancer and triple-negative breast cancer .
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| Cat. No. |
Product Name |
Type |
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- HY-W110888
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Biochemical Assay Reagents
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Brilliant Yellow, a diazo-containing sulfonic aci, is also a potent VGLUT-specific inhibitor. Brilliant Yellow is membrane-impermeable. However, there are some Brilliant Yellow analogs with low cytotoxicity and cell penetration. Brilliant Yellow analogs work on glutamatergic transmission in hippocampal neurons .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P10861A
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Tau Protein
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Neurological Disease
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RI-AG03 acetate is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 acetate inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 acetate mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 acetate suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 acetate can be used for research on tau-related diseases such as Alzheimer's disease .
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- HY-P10861
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Tau Protein
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Neurological Disease
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RI-AG03 is a proteolytically stable tau aggregation inhibitor that crosses the blood-brain barrier and exhibits oral efficacy. RI-AG03 inhibits tau aggregation and promotes the formation of alternative amorphous aggregates that are non-amyloidogenic. RI-AG03 mediates cellular uptake through direct membrane penetration and macropinocytosis, and its conjugation with cell-penetrating peptide sequences (CPPs) enhances the binding of cells to liposomes. RI-AG03 suppresses aggregation-dependent neurodegenerative and behavioral phenotypes, and extends the lifespan of Drosophila models of tauopathy. RI-AG03 can be used for research on tau-related diseases such as Alzheimer's disease .
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- HY-P10914
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MDM-2/p53
Autophagy
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Inflammation/Immunology
Cancer
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D-CopA3 is the inhibitor for MDM2 and the activator for p53 signaling pathway. D-CopA3 exhibits cytotoxicity in colorectal cancer cells HCT-116, LoVo, and RKO (IC50=15-18 μM), induces JNK/Beclin-1 mediated autophagy. D-CopA3 downregulates the expression of cell cycle inhibitory protein p21Cip1/Waf1, enhances the mucosal barrier function and reduces penetration of inflammatory mediators. D-CopA3 exhibits anti-inflammtory activity in mouse C. difficile toxin A-induced acute enteritis models and DSS (HY-116282)-induced chronic colitis models. D-CopA3 exhibits antitumor efficacy in mouse HCT-116 xenograft models .
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- HY-175824
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iGluR
NO Synthase
Apoptosis
Reactive Oxygen Species (ROS)
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Neurological Disease
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PSD-95/nNOS PPI-IN-1 is a inhibitor targeting the PSD-95/nNOS interaction with potential blood-brain barrier penetration. PSD-95/nNOS PPI-IN-1 binds to the PSD-95 PDZ2 domain with high affinity (Ki = 19.45 μM). PSD-95/nNOS PPI-IN-1 inhibits glutamate-induced excitotoxicity by reducing intracellular ROS levels and inhibiting apoptosis. PSD-95/nNOS PPI-IN-1 significantly reduces cerebral infarct volume in rat tMCAO models. PSD-95/nNOS PPI-IN-1 can be used for the study of acute ischemic stroke .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
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- HY-13318S
-
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Oseltamivir acid-d3 is a deuterium labeled Oseltamivir acid (HY-13318). Oseltamivir acid, the active metabolite of Oseltamivir phosphate, is an orally bioavailable, potent and selective inhibitor of influenza virus neuraminidase (IC50=2 nM) with activity against both influenza A and B viruses. Oseltamivir acid has an extremely weak ability to penetrate the BBB under normal physiological conditions, but its blood-brain barrier penetration is significantly enhanced under inflammatory conditions .
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- HY-13011S
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Alectinib-d8 is the deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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- HY-13011S1
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Alectinib-d6 is deuterium labeled Alectinib. Alectinib (CH5424802) is a potent, selective, and orally available ALK inhibitor with an IC50 of 1.9 nM and a Kd value of 2.4 nM (in an ATP-competitive manner), and also inhibits ALK F1174L and ALK R1275Q with IC50s of 1 nM and 3.5 nM, respectively . Alectinib demonstrates effective central nervous system (CNS) penetration .
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- HY-167927S
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Mycophenolic Acid-d3 Acyl-Beta-D-glucuronide is the deuterium labeled Mefuparib (HY-167927). Mefuparib (CVL218) is a poly ADP-ribose polymerase (PARP) inhibitor used in cancer research that exhibits potent brain penetration due to its high protein binding.
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- HY-143994S
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Metopimazine-d6 hydrochloride is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
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- HY-116578S
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Metopimazine-d6 (EXP999-d6; RP9965-d6) is the deuterium labeled Metopimazine (HY-116578). Metopimazine (EXP999; RP9965) is a phenothiazine, orally available, selective dopamine D2 receptor antagonist that does not penetrate the blood-brain barrier. Metopimazine blocks dopamine D2 receptors in the chemoreceptor trigger zone and the periphery, thereby inhibiting nausea and vomiting. Metopimazine is indicated for chemotherapy-induced nausea and vomiting, and has low central side effects due to its poor brain penetration. The use of metopimazine in acute gastroenteritis may have potential risks .
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- HY-W010203S1
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2-Decanone-d5-1 is the deuterium labeled 2-Decanone (HY-W010203). 2-Decanone is an antifungal agent. 2-Decanone inhibits pathogen mycelial growth, spore germination, and appressorium formation. 2-Decanone downregulates spore germination-related genes (MfBmp1) and penetration structure formation genes (MfPls1), inducing reactive oxygen species (ROS) accumulation to trigger mitochondrial damage and subsequent spore apoptosis. 2-Decanone is promising for research of postharvest disease control in fruits and vegetables .
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| Cat. No. |
Product Name |
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Classification |
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- HY-139300A
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HMPL-813 succinate
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Alkynes
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Epitinib succinate is an orally active and selective epidermal growth factor receptor tyrosine kinase inhibitor (EGFR-TKI) designed for optimal brain penetration. Epitinib succinate can be used for the research of cancer . Epitinib (succinate) 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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