Search Result
Results for "
cell penetrant
" in MedChemExpress (MCE) Product Catalog:
2
Biochemical Assay Reagents
16
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-114153
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c-Fms
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Neurological Disease
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PLX5622 is a highly selective brain penetrant and orally active CSF1R inhibitor (IC50=0.016 μM; Ki=5.9 nM). PLX5622 allows for extended and specific microglial cells elimination, preceding and during pathology development. PLX5622 demonstrates desirable PK properties in varies animals. PLX5622 is predominantly administered via ad libitum diets with a dose of 1200 ppm .
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- HY-B0568
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Ferroptosis
HCV
Apoptosis
COX
Histone Demethylase
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Cardiovascular Disease
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
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- HY-17363
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- HY-13902
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VE-822; VX-970; M6620
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ATM/ATR
Apoptosis
STING
Caspase
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Infection
Metabolic Disease
Cancer
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Berzosertib (VE-822) is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
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- HY-P9999
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RG6102; RO-7126209
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Amyloid-β
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Neurological Disease
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Trontinemab (RG6102) is a brain-penetrant, anti-amyloid, bispecific and humanizedized IgG1-κ antibody, targeting to Aβ plaques and transferrin receptor 1 (TFR1). Trontinemab binds to fibrillar Aβ as well as Aβ plaques triggering plaque clearance by engaging immune cells on Alzheimer disease (AD) brain sections. Trontinemab also shows specific affinity to cynomolgus and human TFR1 .
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- HY-109566
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- HY-11063
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- HY-N2332A
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MLA citrate
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nAChR
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Neurological Disease
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Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .
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- HY-109521A
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Manganese(Ⅱ) chloride tetrahydrate, molecular biology grade,≥99.0% (KT)
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Biochemical Assay Reagents
Histone Acetyltransferase
HDAC
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Neurological Disease
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Manganese chloride (tetrahydrate), molecular biology grade,≥99.0% (KT) is an orally active and a blood-brain barrier penetrant compound. It affects the activities of multiple enzymes in cells, such as regulating the activities of histone acetyltransferase (HAT) and histone deacetylase (HDAC), thereby affecting gene expression. It has multiple activities such as neurotoxicity, embryotoxicity, and reproductive toxicity. It is currently mainly used in neurodegenerative diseases and toxicology research.
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- HY-12776
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GSK805
5 Publications Verification
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ROR
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Inflammation/Immunology
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GSK805 is an orally active and CNS penetrant RORγt inhibitor. GSK805 inhibits RORγ and Th17 cells differentiation with pIC50 values of 8.4 and >8.2. GSK805 inhibits the function of Th17 cells. GSK805 can be used for the research of immunity .
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- HY-112870
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Alflutinib; Furmonertinib; AST2818
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EGFR
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Cancer
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Firmonertinib (Alflutinib; Furmonertinib) is an orally active, mutant-selective, and highly brain penetrant EGFR inhibitor. Firmonertinib inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
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- HY-W015309
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Environmental Pollutants
Endogenous Metabolite
iGluR
Glutaminase
c-Met/HGFR
Tyrosinase
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Neurological Disease
Metabolic Disease
Cancer
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Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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- HY-18750
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AZD3759
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EGFR
Apoptosis
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Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
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Zorifertinib (AZD3759) is a potent, orally active, BBB-penetrant, EGFR inhibitor. At Km ATP concentrations, the IC50s are 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively. Zorifertinib induces cancer cell apoptosis. Zorifertinib has antitumor activity, and can be used for NSCLC, HCC etc. research .
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- HY-145899
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PKC
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Cancer
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PKN1/2-IN-1 is a potent cell permeabilizer and selective PKN1/2 inhibitor with IC50 values of 16 nM and 210 nM for PKN1 and PKN2, respectively, and Ki values of 8 nM and 108 nM, respectively. PKN1/2-IN-1 exhibits strong intracellular PKN2 binding capacity in NanoBRET assays (IC50 = 2.1 μM). PKN1/2-IN-1 can be used to study physiological processes such as tumor cell migration .
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- HY-B0688
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Dapsone
4 Publications Verification
4,4′-Diaminodiphenyl sulfone; DDS
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Antibiotic
Parasite
Bacterial
Reactive Oxygen Species (ROS)
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Infection
Inflammation/Immunology
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Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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- HY-17383
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Antifolate
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Cardiovascular Disease
Neurological Disease
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Levomefolate calcium is a synthetic calcium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate calcium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate calcium does not significantly increase folate concentrations in breast milk. Levomefolate calcium can be used for the research of neural tube defects and megaloblastic anemia .
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- HY-W674241
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Endogenous Metabolite
Apoptosis
Bcl-2 Family
Reactive Oxygen Species (ROS)
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Neurological Disease
Cancer
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4-Ethylphenyl sulfate is an orally active and brain-penetrant gut microbial metabolite. 4-Ethylphenyl sulfate downregulates Bcl2 expression, upregulates Bax expression, and induces cancer cell apoptosis via the endogenous apoptotic pathway. 4-Ethylphenyl sulfate induces G2/M cell cycle arrest and reactive oxygen species (ROS) production. 4-Ethylphenyl sulfate impairs oligodendrocyte maturation, reduces oligodendrocyte-neuron interactions, decreases axonal myelination levels, and shifts the oligodendrocyte population toward immature precursor cells. 4-Ethylphenyl sulfate alters brain region-specific neural activity and functional connectivity in mice, and correlates with anxiety-like behaviors in mice .
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- HY-B0534
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Ro111163
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Monoamine Oxidase
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Neurological Disease
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Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
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- HY-116761
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GSK467
5 Publications Verification
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Histone Demethylase
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Cancer
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GSK467 is a cell penetrant and selective KDM5B (JARID1B or PLU1) inhibitor with a Ki of 10 nM and an IC50 of 26 nM. GSK467 shows 180-fold selectivity for KDM4C and no measurable inhibitory effects toward KDM6 or other Jumonji family members .
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- HY-112870A
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Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate
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EGFR
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Inflammation/Immunology
Cancer
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Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation .
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- HY-106634
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Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG
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HIV
Apoptosis
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Infection
Cancer
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Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
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- HY-B0335
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GEA 6414
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COX
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Infection
Neurological Disease
Inflammation/Immunology
Cancer
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Tolfenamic Acid (GEA 6414) is a CNS-penetrant non-steroidal anti-inflammatory and anti-cancer agent, selectively inhibits COX-2, with an IC50 of 13.49 μM (3.53 μg/mL) in LPS-treated (COX-2) canine DH82 monocyte/macrophage cells, but shows no effect on COX-1.
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- HY-131881
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mAChR
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Neurological Disease
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JHU37160 is a potent and brain-penetrant DREADD agonist, with EC50s of 18.5 nM and 0.2 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37160 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
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- HY-109192
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SAR442168; PRN2246
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Btk
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Neurological Disease
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Tolebrutinib (SAR442168) is a potent, selective, orally active and brain-penetrant inhibitor of Bruton tyrosine kinase (BTK), with IC50s of 0.4 and 0.7 nM in Ramos B cells and in HMC microglia cells, respectively. Tolebrutinib exhibits efficacy in central nervous system immunity. Tolebrutinib can be used for the research of multiple sclerosis (MS) .
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- HY-132846
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TAS0953/HM06
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RET
Apoptosis
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Cancer
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Vepafestinib (TAS0953/HM06) is a next-generation brain-penetrant, selective and orally active RET inhibitor with an IC50 value of 0.33 nM. Vepafestinib inhibits the phosphorylation of RET and its downstream signaling pathways, thus blocking the growth and signal transduction of tumor cells and inducing cell cycle arrest and apoptosis. Vepafestinib can be used in the research of various RET-driven cancers, such as non-small cell lung cancer, thyroid cancer and other disease areas .
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- HY-136731
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DNA/RNA Synthesis
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Cancer
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APE1-IN-1 is a potent and blood-brain barrier (BBB) penetrant apurinic/apyrimidinic (AP) endonuclease 1 (APE1) inhibitor with an IC50 value of 2 μM. APE1-IN-1 can potentiate the cytotoxicity of the alkylating agents Methylmethane sulfonate and Temozolomide (HY-17364) to cancer cells .
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- HY-119939
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CHDI00390576
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HDAC
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Cancer
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CHDI-390576, a potent, cell permeable and CNS penetrant class IIa histone deacetylase (HDAC) inhibitor with IC50s of 54 nM, 60 nM, 31 nM, 50 nM for class IIa HDAC4, HDAC5, HDAC7, HDAC9, respectively, shows >500-fold selectivity over class I HDACs (1, 2, 3) and ~150-fold selectivity over HDAC8 and the class IIb HDAC6 isoform .
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- HY-45661
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NUV-422
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CDK
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Neurological Disease
Cancer
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Inixaciclib (NUV-422) is a blood-brain barrier-penetrant inhibitor of CDK2, CDK4 and CDK6. Inixaciclib inhibits cancer cell growth. Inixaciclib induces anti-tumor activity in xenograft models of glioblastoma, CDK4/CDK6 inhibitor-resistant HR + HER2 - metastatic breast cancer, and anti-androgen-resistant prostate cancer. Inixaciclib can be used for the research of relapsed or metastatic castration-resistant prostate cancer .
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- HY-102050
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Phosphodiesterase (PDE)
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Neurological Disease
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PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .
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- HY-133016
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MetAP
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Cardiovascular Disease
Cancer
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M8891 is an orally active, reversible and brain penetrant Methionine Aminopeptidase-2 (MetAP-2) inhibitor with an IC50 of 54 nM and a Ki of 4.33 nM. M8891 does not inhibit MetAP-1 (IC50>10 µM) . M8891 inhibits growth of primary endothelial cells as well as tumor cells and demonstrates antiangiogenic and antitumoral activity .
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- HY-103565
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AMN082
1 Publications Verification
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mGluR
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Neurological Disease
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AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
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- HY-178324
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TREM receptor
Syk
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Neurological Disease
Inflammation/Immunology
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T2M-010 is a potent, brain-penetrant TREM2 agonist (Kd = 0.83 μM). T2M-010 activates receptor-proximal signaling, inducing SYK phosphorylation in TREM2-expressing cells, and promotes microglial phagocytosis. T2M-010 can be used for the study of protective microglial responses relevant to Alzheimer’s disease (AD) .
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- HY-175802
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HYBI-084
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WDR5
Potassium Channel
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Inflammation/Immunology
Cancer
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HBI-2375 (HYBI-084) is a brain-penetrant WDR5 inhibitor with an IC50 of 4.48 nM. HBI-2375 binds to the WINR5 and disrupts MLL1-WDR5 protein-protein interactions. HBI-2375 inhibits cancer cells proliferation and shows anti-tumor activity in AML mouse models, and increases tumor CD8 + cytotoxic T lymphocyte infiltration. HBI-2375 inhibits hERG with an IC50 of 17 µM .
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- HY-112068
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HIF/HIF Prolyl-Hydroxylase
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Cancer
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DM-NOFD is a cell penetrant, prodrug of NOFD a potent and selective inhibitor of an asparaginyl hydroxylase FIH (factor-inhibiting HIF) .
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- HY-B0568R
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Reference Standards
Ferroptosis
HCV
Apoptosis
COX
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Infection
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Endocrinology
Cancer
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Deferiprone (Standard) is the analytical standard of Deferiprone. This product is intended for research and analytical applications. Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
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- HY-133554
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- HY-17363S1
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Autophagy
HIV
Keap1-Nrf2
Endogenous Metabolite
Reactive Oxygen Species (ROS)
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Cancer
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Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate . Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .
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- HY-B2029
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Insecticide
Cholinesterase (ChE)
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Infection
Inflammation/Immunology
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Phosalone is an orally active, blood-brain barrier penetrant Insecticide and acaricide. Phosalone inhibits the activity of Acetylcholinesterase. Phosalone acts as a substrate for detoxifying esterases. Phosalone induces symptoms of cholinergic hyperactivity, toxic reactions, mortality, oxidative stress, and changes in pro-inflammatory protein levels, and exerts toxic effects on colonic tissues and cells. Phosalone controls pistachio psyllids. Phosalone can be used in studies related to colitis .
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- HY-P10019
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NLY01
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GCGR
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Neurological Disease
Inflammation/Immunology
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Pegsebrenatide (NLY01) is a blood-brain barrier-penetrant GLP-1R agonist. Pegsebrenatide alleviates retinal inflammation and neuronal death secondary to ocular hypertension . Pegsebrenatide significantly delays onset and reduces disease severity in experimental autoimmune encephalomyelitis . Pegsebrenatide inhibits the formation of A1 reactive astrocytes in nerve cells and reduces the loss of retinal ganglion cells and dopaminergic neurons. Pegsebrenatide exerts neuroprotective effects in a mouse model of Parkinson's disease by directly preventing microglia-mediated conversion of astrocytes to the A1 neurotoxic phenotype. Pegsebrenatide can be used for research on glaucoma, Parkinson's disease, and multiple sclerosis .
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- HY-118140
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Cannabinoid Receptor
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Neurological Disease
Inflammation/Immunology
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ZCZ011 is a potent and brain-penetrant cannabinoid 1 (CB1) receptor positive allosteric modulator. ZCZ011 potentiates binding of CP55,940 to the CB1 receptor, enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells. ZCZ011 can be used for researching neuropathic and inflammatory pain .
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- HY-11063R
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FTY720 free base (Standard)
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Reference Standards
LPL Receptor
PAK
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Inflammation/Immunology
Cancer
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Fingolimod (Standard) is the analytical standard of Fingolimod. This product is intended for research and analytical applications. Fingolimod (FTY720 free base) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
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- HY-124761
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Polo-like Kinase (PLK)
Autophagy
Mitosis
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Cancer
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Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9 μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5 μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis. Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors .
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- HY-131891
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mAChR
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Neurological Disease
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JHU37152 is a potent and brain-penetrant DREADD agonist, with EC50s of 5 nM and 0.5 nM for hM3Dq and hM4Di DREADDs in HEK-293 cells, respectively. JHU37152 exhibits selective [ 3H]Clozapine displacement from DREADDs and not from other Clozapine-binding sites in mice brain tissue .
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- HY-178164
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Apoptosis
Akt
mTOR
STAT
NF-κB
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Cancer
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HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (KD = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC) .
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- HY-19916
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BAL-101553
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Microtubule/Tubulin
Checkpoint Kinase (Chk)
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Cancer
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Lisavanbulin (BAL-101553) is the prodrug of the microtubule targeting agent Avanbulin (BAL 27862) (HY-106008). Lisavanbulin is a BBB-penetrant and orally active antitumor agent, especially in tumors that express high levels of end-binding protein 1. Lisavanbulin has ability to target tumor cell proliferation and affects the tumor microenvironment by reducing tumor microvasculature. Lisavanbulin is also a spindle assembly checkpoint activator. Lisavanbulin induces cell cycle arrest and subsequent death or aberrant chromosome segregation. Lisavanbulin can be studied in research for diffuse large B cell lymphoma (DLBCL) and glioblastoma .
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- HY-176537
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Microtubule/Tubulin
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Cancer
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RGN6024 is a brain-penetrant, orally active and reversible small molecule tubulin destabilizer. RGN6024 inhibits microtubule polymerization both in biochemical and cellular assays, binds to the colchicine binding pocket of β-tubulin (SPR: Kd = 6.7 μM; tryptophan assay: Kd = 7.4 μM), and triggers G2/M arrest in glioblastoma (GB) cells. RGN6024 retains activity in βIII-tubulin overexpressing cells. RGN6024 inhibits tumor growth in a GB xenograft mouse model. RGN6024 can be used for the study of glioblastoma (GB) .
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- HY-173066
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PROTACs
Indoleamine 2,3-Dioxygenase (IDO)
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Cancer
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NU227326 is a blood-brain barrier penetrant IDO1 PROTAC degrader, with a DC50 of 4.5 nM in HiBiT degradation assays. NU227326 degrades IDO1 in U87 and GBM43 cells, with DC50 values of 7.1 nM and 11.8 nM, respectively (WB assays). NU227326 is applicable to research related to glioblastoma, prostate cancer, triple-negative breast cancer, pancreatic cancer, and ovarian cancer .
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- HY-W674241A
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Endogenous Metabolite
Apoptosis
Bcl-2 Family
Reactive Oxygen Species (ROS)
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Neurological Disease
Cancer
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4-Ethylphenyl sulfate sodium is an orally active and brain-penetrant gut microbial metabolite. 4-Ethylphenyl sulfate sodium downregulates Bcl2 expression, upregulates Bax expression, and induces cancer cell apoptosis via the endogenous apoptotic pathway. 4-Ethylphenyl sulfate sodium induces G2/M cell cycle arrest and reactive oxygen species (ROS) production. 4-Ethylphenyl sulfate sodium impairs oligodendrocyte maturation, reduces oligodendrocyte-neuron interactions, decreases axonal myelination levels, and shifts the oligodendrocyte population toward immature precursor cells. 4-Ethylphenyl sulfate sodium alters brain region-specific neural activity and functional connectivity in mice, and correlates with anxiety-like behaviors in mice .
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- HY-119351
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- HY-17363R
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- HY-B0688S2
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4,4′-Diaminodiphenyl sulfone-13C12; DDS-13C12
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Isotope-Labeled Compounds
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species (ROS)
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Infection
Inflammation/Immunology
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Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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- HY-N6685
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- HY-11063S
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FTY720 free based-d4
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LPL Receptor
PAK
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Inflammation/Immunology
Cancer
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Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
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- HY-120596
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PPAR
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Neurological Disease
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PPARδ/γ agonist 1 sodium is a chemically unique and brain penetrant dual PPAR delta/gamma agonist. PPARδ/γ agonist 1 sodium can be used for the research of Alzheimer’s disease .
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- HY-B0688S
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4,4′-Diaminodiphenyl sulfone-d8; DDS-d8
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Antibiotic
Parasite
Bacterial
Reactive Oxygen Species (ROS)
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Infection
Inflammation/Immunology
Cancer
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Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases .
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- HY-119282
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mGluR
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Neurological Disease
|
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AZD6538 is a potent, selective and brain penetrant mGluR5 negative allosteric modulator. AZD6538 inhibits DHPG (HY-12598A)-stimulated intracellular Ca2+ release in HEK cells expressing rat or human mGluR5, with IC50 values of 3.2 and 13.4 nM for rat mGluR5 and human mGluR5, respectively. AZD6538 can be used for the research of neuropathic pain .
|
-
- HY-131958
-
|
|
AMPK
|
Cancer
|
|
D942 is a cell penetrant AMPK activator and partially inhibits the mitochondrial complex I. In multiple myeloma cells, D942 inhibits cell growth .
|
-
- HY-114926
-
|
|
MAGL
|
Neurological Disease
|
|
KT185 is an orally-bioavailable, brain-penetrant and selective ABHD6 inhibitor, with an IC50 0.21 nM in Neuro2A cells .
|
-
- HY-150791
-
|
|
Reactive Oxygen Species (ROS)
DNA/RNA Synthesis
|
Cancer
|
|
FLDP-5 is a blood-brain barrier (BBB) penetrant curcuminoid analogues. FLDP-5 can induce production of ROS (Reactive Oxygen Species), DNA damage and cell cycle S phase arrest. FLDP-5 exhibits highly potent tumour-suppressive effects with anti-proliferative and anti-migratory activities on LN-18 cells .
|
-
- HY-16491
-
|
DJ-927
|
Microtubule/Tubulin
|
Cancer
|
|
Tesetaxel (DJ-927) is an orally active and brain-penetrant taxane tubulin inhibitor. Tesetaxel inhibits tubulin depolymerization with an IC50 of 0.44 μM. Tesetaxel inhibits cancer cells proliferation and shows potent antitumor activity against P-glycoprotein-positive cancer cells. Tesetaxel can be used for the research of cancer, such as solid tumors, liver metastasis, and advanced breast cancer .
|
-
- HY-163737
-
|
|
Microtubule/Tubulin
|
Cancer
|
|
ST-401, a microtubule-targeting agent (MTA), is a brain-penetrant microtubule (MT) assembly inhibitor. ST-401 disrupts microtubule (MT) function through gentle and reverisible reduction in MT assembly that triggers mitotic delay and cell death in interphase. ST-401 shows a potent antitumor activity .
|
-
- HY-178969
-
|
|
FAK
Pyk2
Apoptosis
|
Neurological Disease
Cancer
|
|
GZD-257 is a brain-penetrant, ATP-competitive FAK inhibitor (IC50 = 14.3 nM), performing 4.77-fold selectivity with FAK to Pyk2 (IC50 = 68.2 nM). GZD-257 can significantly induce apoptosis of U118MG cells and arrest the cell cycle at the G2/M phase. GZD-257 can be used for the study of Glioblastoma (GBM) .
|
-
- HY-178048
-
|
|
Autophagy
|
Neurological Disease
|
|
Neuroprotective agent 13 is a brain-penetrant 1H-benzo[d]imidazoles compound with neuroprotective effect. Neuroprotective agent 13 can activate autophagy and clear SCMAS accumulation from iPSC-derived neural progenitor cells. Neuroprotective agent 13 can be used for the research of neurological disease, such as neuronal ceroid lipofuscinoses (NCLs) .
|
-
- HY-18750A
-
|
AZD3759 hydrochloride
|
EGFR
Apoptosis
|
Cancer
|
|
Zorifertinib (AZD3759) hydrochloride is a potent, orally active, BBB-penetrant, EGFR inhibitor (IC50s: 0.3, 0.2, and 0.2 nM for EGFR wt, EGFR L858R, and EGFR exon 19Del, respectively). Zorifertinib hydrochloride induces cancer cell apoptosis. Zorifertinib hydrochloride has antitumor activity, and can be used for NSCLC, HCC etc. research .
|
-
- HY-150639
-
|
|
Raf
|
Cancer
|
|
Everafenib is a potent and blood-brain barrier (BBB) penetrant BRAF inhibitor, also inhibits MAPK signaling. Everafenib has inhibitory activity against a panel of V600EBRAF melanoma cell lines with IC50 values of 2-10 nM, which is better than Dabrafenib (HY-14660) and Vemurafenib (HY-12057). Everafenib has efficacy in an intracranial mouse model of metastatic melanoma .
|
-
- HY-174212
-
|
|
Apoptosis
|
Cancer
|
|
MXC-017 is a blood-brain barrier (BBB)-penetrant apoptosis inducer that directly targets Vimentin (VIM). MXC-017 prevents radiation-induced glioma stem cell (GSC) formation, while promoting G0/G1 cell cycle arrest and apoptosis. MXC-017 exhibits minimal off-target effects and shows no significant cytotoxicity. MXC-017 significantly prolongs median survival when used in combination with radiation therapy in glioblastoma (GBM) mouse models.
|
-
- HY-B0688S1
-
|
4,4′-Diaminodiphenyl sulfone-d4; DDS-d4
|
Isotope-Labeled Compounds
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species (ROS)
|
Infection
Inflammation/Immunology
|
|
Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-103565A
-
|
|
mGluR
|
Neurological Disease
|
|
AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-106634R
-
|
Methylglyoxal-bis(guanylhydrazone) (Standard); MGBG (Standard); Methyl-GAG (Standard)
|
Reference Standards
HIV
Apoptosis
|
Infection
Cancer
|
|
Mitoguazone (Standard) is the analytical standard of Mitoguazone. This product is intended for research and analytical applications. Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment .
|
-
- HY-B0568S
-
|
|
Isotope-Labeled Compounds
HCV
Ferroptosis
|
Cardiovascular Disease
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Deferiprone-d3 is the deuterium labeled Deferiprone (HY-B0568). Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
|
-
- HY-W641657
-
|
|
Drug Metabolite
|
Metabolic Disease
|
|
Desmonomethylpromazine is the brain-penetrant demethylated metabolite of Promazine (HY-B1225A). Desmonomethylpromazine can enter red blood cells and tissues through passive diffusion, distributes in tissues such as lung, liver, and kidney in rats .
|
-
- HY-115458
-
|
|
Microtubule/Tubulin
Apoptosis
|
Cancer
|
|
6-MOMIPP is a brain-penetrant microtubule disruptor that targets the colchicine site on β-tubulin. 6-MOMIPP can induce mitotic arrest and cell apoptosis. 6-MOMIPP has broad activity against the viability of multiple glioblastoma, melanoma and lung carcinoma cell lines. 6-MOMIPP can be used for the research of cancer .
|
-
- HY-B0534S1
-
|
Ro111163-d4
|
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-11063S1
-
|
FTY720-d4
|
LPL Receptor
PAK
|
Inflammation/Immunology
Cancer
|
|
Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant .
|
-
- HY-B0534R
-
|
Ro111163 (Standard)
|
Reference Standards
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide (Standard) is the analytical standard of Moclobemide. This product is intended for research and analytical applications. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-W714513
-
|
|
mGluR
|
Neurological Disease
|
|
VU0469650 hydrochloride is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 1 (mGluR1). VU0469650 hydrochloride inhibits glutamate-induced calcium flux in cells expressing human mGluR1 (IC50= 99 nM). VU0469650 hydrochloride is promising for research of central nervous system diseases such as anxiety, addiction, and epilepsy .
|
-
- HY-167893
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
AGH-107 is a high selective and brain-penetrant agonist of 5-HT7 receptor, with a Ki of 6 nM and EC50 of 19 nM. AGH-107 exhibits high selectivity over related CNS targets, high metabolic stability and low toxicity in HEK-293 and HepG2 cell cultures .
|
-
- HY-B0534S
-
|
Ro111163-d8
|
Isotope-Labeled Compounds
Monoamine Oxidase
|
Neurological Disease
|
|
Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
|
-
- HY-178052
-
|
|
Autophagy
|
Neurological Disease
|
|
Neuroprotective agent 14 is a brain-penetrant 1H-benzo[d]imidazoles compound with neuroprotective effect. Neuroprotective agent 14 can activate autophagy and clear SCMAS accumulation from iPSC-derived neural progenitor cells. Neuroprotective agent 14 can be used for the research of neurological disease, such as neuronal ceroid lipofuscinoses (NCLs) .
|
-
- HY-N6685S1
-
-
- HY-17383A
-
|
|
Antifolate
|
Neurological Disease
|
|
Levomefolate disodium is a synthetic disodium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate disodium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate disodium does not significantly increase folate concentrations in breast milk. Levomefolate disodium can be used for the research of neural tube defects and megaloblastic anemia .
|
-
- HY-N6685R
-
|
3-AcDON (Standard); 3-ADON (Standard)
|
Reference Standards
Endogenous Metabolite
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
3-Acetyldeoxynivalenol (3-AcDON; 3ADON) (Standard) is the analytical standard of 3-Acetyldeoxynivalenol (HY-N6685). This product is intended for research and analytical applications. 3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative, is a brain-penetrant Fusarium mycotoxin. 3-Acetyldeoxynivalenol induces mRNA expression and production of inflammatory chemokine IL-8 in intestinal cells .
|
-
- HY-B0688R
-
|
4,4′-Diaminodiphenyl sulfone (Standard); DDS (Standard)
|
Reference Standards
Antibiotic
Parasite
Bacterial
Reactive Oxygen Species (ROS)
|
Infection
Inflammation/Immunology
|
|
Dapsone (Standard) is the analytical standard of Dapsone. This product is intended for research and analytical applications. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-101349
-
|
|
Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
|
Neurological Disease
Cancer
|
|
L 741742 is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 can be used for the research of schizophrenia and glioblastoma .
|
-
- HY-101349A
-
|
|
Dopamine Receptor
Apoptosis
Autophagy
PDGFR
ERK
mTOR
|
Neurological Disease
Cancer
|
|
L 741742 hydrochloride is a highly selective and brain-penetrant D4 dopamine receptor antagonist, with Ki values of 3.5 nM, 770 nM and >1700 nM for human D4, D3 and D2 receptors, respectively. L 741742 hydrochloride suppresses PDGFRβ, ERK1/2, and mTOR signaling pathways, and impairs autophagic flux while disrupting lysosomal function.L 741742 hydrochloride induces G0/G1 cell-cycle arrest and apoptosis, promotes neuronal differentiation of normal human neural stem cells, selectively inhibits growth and clonogenic potential of glioblastoma neural stem cells and primary glioblastoma tumor cells, exerts synergistic effects with Temozolomide (TMZ) (HY-17364) against glioblastoma neural stem cells in vitro, and inhibits glioblastoma neural stem cell xenograft growth in immunocompromised mice. L 741742 hydrochloride can be used for the research of schizophrenia and glioblastoma .
|
-
- HY-176942
-
|
ROS1-IN-3
|
ROS Kinase
Trk Receptor
|
Cancer
|
|
YP0322 (ROS1-IN-3) is a potent orally active, selective, and CNS-penetrant ROS1 inhibitor. JYP0322 selectively inhibits human wild-type ROS1 and human ROS1 G2032R with IC50s of 0.37 and 0.3 nM, respectively, showing 6-130-fold selectivity over TRKA, TRKB, and TRKC. JYP0322 inhibits proliferation of ROS1 fusion-expressing cells, and inhibits tumor growth in mouse xenograft models. JYP0322 can be used for the research of non-small cell lung cancer (NSCLC) .
|
-
- HY-13764A
-
|
|
Calcium Channel
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca 2+ influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal .
|
-
- HY-B0688S3
-
|
4,4′-Diaminodiphenyl sulfone-15N2; DDS-15N2
|
Isotope-Labeled Compounds
Antibiotic
Reactive Oxygen Species (ROS)
Bacterial
Parasite
|
Infection
Inflammation/Immunology
|
|
Dapsone- 15N2 (4,4′-Diaminodiphenyl sulfone- 15N2) is 15N labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
|
-
- HY-141425
-
|
|
P-glycoprotein
|
Cancer
|
|
NSC73306, a thiosemicarbazone, is a cell penetrant, cytotoxic agent that exhibits greater toxicity against cells expressing functional P-gp (P-glycoprotein) than against other cells .
|
-
- HY-182402
-
|
|
Carboxylesterase (CES)
Wnt
|
|
|
Notum-IN-2 is a partially brain-penetrant Notum carboxyl-esterase inhibitor with an IC50 of 18 nM. Notum-IN-2 can be used as a chemical tool for exploring Wnt signalling in cells .
|
-
- HY-102050R
-
|
|
Reference Standards
Phosphodiesterase (PDE)
|
Neurological Disease
|
|
PF-05085727 (Standard) is the analytical standard of PF-05085727 (HY-102050). This product is intended for research and analytical applications. PF-05085727 is a potent, selective and brain penetrant inhibitor of cGMP-dependent PDE2A (IC50=2 nM). PF-05085727 inhibits PDE2A >4,000-fold selectivity over PDE1 and PDE3-11 .
|
-
- HY-13902A
-
|
VE-822 hydrochloride; VX-970 hydrochloride; M6620 hydrochloride
|
ATM/ATR
Apoptosis
STING
Caspase
|
Neurological Disease
Cancer
|
|
Berzosertib (VE-822) hydrochloride is an orally active, CNS-penetrant, and selective ATR kinase inhibitor. Berzosertib hydrochloride blocks ATR kinase activity, abrogates G2/M cell cycle checkpoint, impairs DNA damage repair. Berzosertib hydrochloride induces apoptosis, inhibnits conlony migration, inhibits cell proliferation, and activates cGAS-STING axes in cancer cells. Berzosertib hydrochloride can be used for the research of cancers, such as head and neck squamous cell carcinoma, and colorectal cancer .
|
-
- HY-182943
-
|
|
Btk
Fc Receptor (FcR)
|
Neurological Disease
Inflammation/Immunology
|
|
BTK-IN-49 is a selective, orally active and brain-penetrant BTK inhibitor with an IC50 of 0.14 nM. BTK-IN-49 binds to BTK and blocks B-cell receptor and Fcγ receptor signaling. BTK-IN-49 inhibits the proliferation of CNS-compartmentalized B-cells and FcγR-induced microglial proliferation in a BTK-dependent manner. BTK-IN-49 can be used for the study of multiple sclerosis .
|
-
- HY-177895
-
|
|
EGFR
|
Cancer
|
|
IAM1363 is a selective, irreversible and brain-penetrant HER2 inhibitor. IAM1363 shows over 1,000-fold selectivity for HER2 compared to EGFR. IAM1363 can be used for the study of advanced HER2 cancers, such as HER2-driven non-small cell lung cancer (NSCLC) .
|
-
- HY-N2332
-
|
MLA
|
nAChR
|
Neurological Disease
|
|
Methyllycaconitine (MLA) is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine can be used for neurological disease research, such as Alzheimer’s disease .
|
-
- HY-183682
-
|
|
EGFR
p38 MAPK
ERK
Akt
|
Cancer
|
|
AZ14289671 is an orally active, blood-brain barrier-penetrant tyrosine kinase (tyrosine kinase) inhibitor (TKI) that specifically targets non-small cell lung cancer (NSCLC) harboring EGFR exon 20 insertion mutations (EGFR Exon20Ins), while largely sparing wild-type EGFR to reduce off-target toxicities such as rash and diarrhea. AZ14289671 inhibits the downstream MAPK/ERK/AKT pathway, suppressing tumor cell proliferation, survival and migration. AZ14289671 can be used for NSCLC research .
|
-
- HY-180997
-
|
|
Amyloid-β
|
Neurological Disease
|
|
Aβ aggregation-IN-5 is a brain-penetrant amyloid-β aggregation inhibitor. Aβ aggregation-IN-5 inhibits Aβ aggregation/oligomerization, rescues cells from AB/ROS toxicity and reduces microglial activation/NO production. Aβ aggregation-IN-5 reduces amyloid burden, neuroinflammation, microglial activation in APP/PSEN1 mice. Aβ aggregation-IN-5 can be used for the research of Alzheimer's disease .
|
-
- HY-112870AS
-
|
Alflutinib-d3 mesylate; Furmonertinib-d3 mesylate; AST2818-d3 mesylate
|
Isotope-Labeled Compounds
EGFR
|
Inflammation/Immunology
Cancer
|
|
Firmonertinib-d3 (Alflutinib-d3) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.
|
-
- HY-180214
-
|
|
HDAC
|
Cardiovascular Disease
Neurological Disease
|
|
HDAC6-IN-69 is a brain-penetrant and highly selective HDAC6 inhibitor with an IC50 of 4.0 nM. HDAC6-IN-69 shows >176-fold against other HDAC isoforms. HDAC6-IN-69 engages the target in neuronal cells by dose-dependently upregulating acetylated α-tubulin in virto. HDAC6-IN-69 has neuroprotective effect and can be used for ischemic stroke research .
|
-
- HY-183116
-
|
|
Molecular Glues
Anaplastic lymphoma kinase (ALK)
|
Cancer
|
|
TRI-611 is a brain-penetrant, orally active molecular glue degrader targeting ALK. TRI-611 engages ALK via a distal degron, forms a ternary complex with CRBN, triggers ALK polyubiquitination and degradation, including TKI-resistant ALK fusion proteins. TRI-611 inhibits ALK downstream signaling pathways, induces anti-proliferative effects in ALK-positive cancer cells. TRI-611 induces regression of ALK-positive non-small cell lung cancer tumors in preclinical xenograft models. TRI-611 can be used for the research of ALK-positive non-small cell lung cancer, including TKI-refractory tumors and central nervous system metastases .
|
-
- HY-17383R
-
|
|
Reference Standards
Antifolate
|
Cardiovascular Disease
Neurological Disease
|
|
Levomefolate calcium (Standard) is the analytical standard of Levomefolate calcium. This product is intended for research and analytical applications. Levomefolate calcium is a synthetic calcium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate calcium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate calcium does not significantly increase folate concentrations in breast milk. Levomefolate calcium can be used for the research of neural tube defects and megaloblastic anemia .
|
-
- HY-W015309R
-
|
|
Reference Standards
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-176254
-
|
|
Histone Demethylase
Amyloid-β
|
Neurological Disease
|
|
LSD1-IN-43 is a highly selective, reversible, orally active and brain-penetrant LSD1 inhibitor with an IC50 value of 0.8 μM. LSD1-IN-43 has low inhibitory activity against MAO-A and MAO-B, two homologs of LSD1. LSD1-IN-43 significantly inhibits Aβ aggregation and enhances Aβ-induced neuronal cell viability. LSD1-IN-43 can be used for the study of Alzheimer’s disease (AD).
|
-
- HY-103565R
-
|
|
Reference Standards
mGluR
|
Neurological Disease
|
|
AMN082 (Standard) is the analytical standard of AMN082. This product is intended for research and analytical applications. AMN082, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-125339
-
|
|
COMT
Apoptosis
|
Neurological Disease
Cancer
|
|
Ro 41-0960 is a CNS-penetrant, orally active catechol-O-methyl transferase (COMT) inhibitor. Ro 41-0960 reduces dopamine catabolism, increases striatal dopamine and DOPAC levels, decreases striatal HVA levels, induces apoptosis, inhibits proliferation and extracellular matrix formation in uterine fibroid cells. Ro 41-0960 arrests or shrinks uterine fibroid lesions in rats. Ro 41-0960 can be used for the research of Parkinson’s disease, uterine leiomyomas, and breast cancer .
|
-
- HY-17383S
-
|
|
Isotope-Labeled Compounds
Antifolate
|
Cardiovascular Disease
Neurological Disease
|
|
Levomefolate- 13C5 calcium)is the 13C-labeled Levomefolate calcium (HY-17383). Levomefolate calcium is a synthetic calcium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate calcium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate calcium does not significantly increase folate concentrations in breast milk. Levomefolate calcium can be used for the research of neural tube defects and megaloblastic anemia .
|
-
- HY-153268
-
|
BDTX-1535; EGFR-IN-76
|
EGFR
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Silevertinib (BDTX-1535) is an irreversible, brain-penetrant, selective and orally active EGFR inhibitor with wild-type EGFR-sparing. Silevertinib targets key EGFR resistance mutations, including the kinase domain (C797S, L718Q, G724S, S768I), extracellular domain (EGFRvIII, A289X), and EGFR amplification. Silevertinib exerts anti-tumor activity with well tolerated in vivo. Silevertinib can be used for non-small cell lung cancer (NSCLC) and glioblastoma (GBM) research .
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-
- HY-147939
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Cancer
|
|
AChE/BuChE-IN-3 is a potent and blood-brain barrier (BBB) penetrant AChE and BuChE dual inhibitor with IC50s of 0.65 μM and 5.77 μM for AChE and BuChE. AChE/BuChE-IN-3 also inhibits Aβ1-42 aggregation. AChE/BuChE-IN-3 has effectively neuroprotective activities and nearly no toxicity on SH-SY5Y cells. AChE/BuChE-IN-3 can be used for researching Alzheimer's disease .
|
-
- HY-172429A
-
|
ORIC-114 hemihydrate
|
EGFR
|
Neurological Disease
Cancer
|
|
Enozertinib (ORIC-114) hemihydrate is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib hemihydrate exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib hemihydrate induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib hemihydrate can be used for the research of solid tumors and NSCLC .
|
-
- HY-180807
-
|
|
p38 MAPK
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
ERK
JNK
|
Cardiovascular Disease
Neurological Disease
|
|
MAPK-IN-6 (compound 116B) is a CNS-penetrant compound that inhibits the MAPK signaling pathway. MAPK-IN-6 reduces oxidative stress in SH-SY5Y neuronal cells by reducing ROS, restoring mitochondrial function, and inhibiting MAPK-driven inflammation. MAPK-IN-6 demonstrates profound neuroprotective efficacy in a rat tBCCAO/R model via ERK-P38-JNK signaling. MAPK-IN-6 can be used as a neuroprotective agent in ischemic stroke research .
|
-
- HY-172429
-
|
ORIC-114
|
EGFR
|
Neurological Disease
Cancer
|
|
Enozertinib (ORIC-114) is an orally active, CNS-penetrant, highly selective and irreversible dual EGFR/HER2 inhibitor that exhibits potent and targeted inhibition of exon 20 insertion mutations. Enozertinib exhibits high kinome selectivity for the EGFR family of receptors to reduce off-target kinase liabilities. Enozertinib induces tumor regression and demonstrates antitumor activity in central nervous system and non-small cell lung cancer (NSCLC) tumor models. Enozertinib can be used for the research of solid tumors and NSCLC .
|
-
- HY-180197
-
|
|
PKC
iGluR
Reactive Oxygen Species (ROS)
|
Cardiovascular Disease
Neurological Disease
|
|
PICK1 PDZ-IN-1 (Compound 6b) is a selective and brain-penetrant protein interacting with C kinase 1 (PICK1) PDZ domain inhibitor with a Ki of 27.73 μM. PICK1 PDZ-IN-1 can competitively inhibit the interaction between PICK1 and the GluA2 subunit of AMPA receptors. PICK1 PDZ-IN-1 can increase the survival rate of HT22 cells and primary cortical neuron cells induced by glutamate and inhibit ROS production. PICK1 PDZ-IN-1 exhibits neuroprotective effect and reduces the area of cerebral infarction. PICK1 PDZ-IN-1 can be used for the research of ischemic stroke .
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-
- HY-181073
-
|
|
Apoptosis
Necroptosis
NF-κB
p38 MAPK
|
Neurological Disease
Cancer
|
|
Apoptosis/necroptosis inducer 1 is an orally active and brain-penetrant apoptosis and necroptosis inducer. Apoptosis/necroptosis inducer 1 induces mitochondria-dependent (intrinsic pathway) apoptosis. Apoptosis/necroptosis inducer 1 induces necroptosis by activating the TNF-α/NF-κB/MAPK signaling pathway. Apoptosis/necroptosis inducer 1 exhibits antiproliferative activity in glioblastoma cell lines and multiple solid tumor types. Apoptosis/necroptosis inducer 1 inhibits growth of orthotopic glioblastoma in animal models and improves survival rate. Apoptosis/necroptosis inducer 1 can be used for the research of glioblastoma .
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-
- HY-109061R
-
|
YH25448 (Standard); GNS-1480 (Standard)
|
Apoptosis
Akt
TRP Channel
EGFR
ERK
Reference Standards
|
Infection
Neurological Disease
Metabolic Disease
Cancer
|
|
Lazertinib (Standard) is the analytical standard of Lazertinib (HY-109061). This product is intended for research and analytical applications. Lazertinib (YH25448) is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib can be used in the study of non-small cell lung cancer .
|
-
- HY-101304
-
|
S-isopropyl ITU; IPTU
|
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
S-Isopropylisothiourea hydrobromide (S-isopropyl ITU; IPTU) is a blood-brain barrier (BBB) penetrant NOS inhibitor with IC50 values of 0.66, 0.75 and 0.29 μM against mouse spinal cord, cerebellar, bovine aortic and porcine endothelial cell NOS. S-Isopropylisothiourea exhibits a significant blood pressure-raising effect without damaging the perfusion of vital organs and can also inhibit the late-phase pain response induced by formalin. S-Isopropylisothiourea hydrobromide is used in the researchs for hemorrhagic shock and pain response based on NOS .
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-
- HY-165428
-
|
|
CXCR
Arrestin
|
Inflammation/Immunology
|
|
SCH-900875 is an orally active, brain-penetrant and selective CXCR3 receptor inhibitor, which also shows high selectivity over CXCR1 and CXCR2 receptors. SCH-900875 binds to CXCR3, blocking the binding of ligands CXCL9, CXCL10, and CXCL11, inhibiting downstream G protein and β-arrestin signaling pathways to suppress inflammatory cell migration. SCH-900875 is promising for research of autoimmune diseases (rheumatoid arthritis, multiple sclerosis) and inflammatory disorders (psoriasis, inflammatory bowel disease) .
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-
- HY-W266188
-
|
|
Isotope-Labeled Compounds
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Decanoic acid- 13C is the 13C-labeled Decanoic acid (HY-W015309). Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
|
-
- HY-109061BR
-
|
YH25448 mesylate (Standard); GNS-1480 mesylate (Standard)
|
Reference Standards
|
Cancer
|
|
Lazertinib mesylate (Standard) is the analytical standard of Lazertinib (mesylate) (HY-109061B). This product is intended for research and analytical applications. Lazertinib (YH25448) mesylate is a potent, selective, CNS-penetrant, orally available and irreversible EGFR tyrosine Kinase inhibitor, exhibiting high selectivity for activating (EGFRm) and T790M resistance mutations. Lazertinib mesylate inhibits phosphorylation of EGFR, AKT and ERK, leading to apoptosis and suppression of tumor growth in mouse H1975-luc brain metastasis xenograft models. Lazertinib mesylate can be used in the study of non-small cell lung cancer .
|
-
- HY-103537A
-
|
|
γ-secretase
Amyloid-β
|
Neurological Disease
|
|
BIIB042 is a potent, orally active, brain-penetrant, and selective γ-secretase modulator (GSM). BIIB042 reduces Aβ42 and increases Aβ38 levels in cells. BIIB042 significantly reduces brain Aβ42 levels in CF-1 mice and Fischer rats, as well as plasma Aβ42 levels in cynomolgus monkeys. BIIB042 reduces Aβ42 levels and Aβ plaque burden in Tg2576 mice. BIIB042 can be used for alzheimer's disease (AD) research .
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-
- HY-178148
-
|
|
Androgen Receptor
|
Endocrinology
Cancer
|
|
AR antagonist 17 is a selective, orally active, low brain-penetrant Androgen Receptor (AR) antagonist (IC50 = 0.010 μM), effectively blocking AR dimerization and nuclear translocation, and demonstrating potent efficacy in several castration-resistant prostate cancer (CRPC) cells. AR antagonist 17 showed superior efficacy against variant drug-resistant AR mutants. AR antagonist 17 can inhibit tumor growth in an LNCaP xenograft model without apparent toxicity. AR antagonist 17 can be used for the study of castration-resistant prostate cancer (CRPC) .
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-
- HY-182254
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
AChE/BChE-IN-35, Tacrine (HY-111338) derivative, is a brain-penetrant dual AChE/BChE inhibitor with an Electric Eel AChE IC50 of 123.66 nM, human AChE IC50 of 122.34 nM, and equine BChE IC50 of 488.00 nM. AChE/BChE-IN-35 undergoes LAT1-mediated active transport across cell membranes. AChE/BChE-IN-35 exhibits enhanced brain exposure with slower brain tissue elimination. AChE/BChE-IN-35 can be used for the research of alzheimer's disease .
|
-
- HY-P10862
-
|
|
Exosomes
Virus Protease
|
Infection
Cancer
|
AH-D peptide is a brain-penetrant antiviral agent disrupting highly curved lipid membranes. AH-D peptide exhibits broad-spectrum antiviral activity against ZIKV, Dengue virus, Chikungunya virus, yellow fever virus and Japanese encephalitis virus, with
IC50 values of 11.9, 12.5, 35.7, 206 and 136 nM, respectively. AH-D peptide reduces the viral load in the brain, suppresses inflammation, protects neurons, and does not damage the blood brain barrier. AH-D peptide restores antitumor immunity by decreasing circulating PD-L1 + exosomes, reducing intratumoral immunosuppressive cells (regulatory T cells, myeloid-derived suppressor cells), and enhancing T cell function. AH-D peptide inhibits membrane-enveloped viruses and cancer cell metastasis in vivo. AH-D peptide exhibits no immunogenicity and has negligible effects on normal tissues. AH-D peptide can be used for research in Zika virus and other mosquito-borne viruses, cancer immunotherapy and metastasis .
|
-
- HY-113357
-
|
|
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .
|
-
- HY-179599
-
|
|
DYRK
EGFR
|
Neurological Disease
Cancer
|
|
Dyrk1A-IN-15 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 19 nM. Dyrk1A-IN-15 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-15 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-15 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-15 has potential for glioblastoma (GBM) research .
|
-
- HY-182328
-
|
|
Amyloid-β
|
Neurological Disease
|
|
BTA-EG6 is a brain-penetrant aggregated amyloid-β (Aβ) peptide binder with a Kd of 290 nM for Aβ1-42. BTA-EG6 binds to aggregated Aβ and forms protein-resistive coatings that block interactions between Aβ and catalase. BTA-EG6 protects neuroblastoma cells from Aβ-induced toxicity and oxidative stress, and inhibits Aβ-induced increases in cellular hydrogen peroxide (H2O2) levels. BTA-EG6 can be used for the research of alzheimer’s disease (AD) .
|
-
- HY-179600
-
|
|
DYRK
EGFR
|
Neurological Disease
Cancer
|
|
Dyrk1A-IN-16 is a selective, brain-penetrant and ATP-competitive Dyrk1A inhibitor with a IC50 of 53 nM. Dyrk1A-IN-16 displays high selectivity across a broad kinase panel (specific for DYRK kinases) with nanomolar potency. Dyrk1A-IN-16 impairs neurosphere self-renewal, cell invasion, and EGFR stability in vitro. Dyrk1A-IN-16 inhibits tumor growth and prolongs survival in vivo. Dyrk1A-IN-16 has potential for glioblastoma (GBM) research .
|
-
- HY-178939
-
|
|
EGFR
Akt
PERK
Apoptosis
|
Neurological Disease
Cancer
|
|
EGFR-IN-181 is an orally active, potent, brain-penetrant EGFRL858R/T790M/C797S triple mutations inhibitor (IC50 = 1.32 nM). EGFR-IN-181 can inhibit EGFR phosphorylation (p-EGFR) and phosphorylation of its downstream signaling proteins AKT (p-AKT) and ERK (p-ERK). EGFR-IN-181 can induce apoptosis and cause G2 phase arrest. EGFR-IN-181 can be used for the study of non-small cell lung cancer (NSCLC) and brain metastases .
|
-
- HY-156438
-
|
NT-0796
|
NOD-like Receptor (NLR)
Interleukin Related
|
Neurological Disease
|
|
Ruvonoflast (NT-0796) is an orally active, selective and CNS-penetrant NLRP3 inflammasome inhibitor. Ruvonoflast inhibits IL-1β release in human PBMC cells with an IC50 value of 0.32 nM. Ruvonoflast is an isopropyl ester that undergoes intracellular conversion to Ruvonoflast, the carboxylic acid active species. Ruvonoflast reverses high fat diet-induced obesity, systemic inflammation and astrogliosis in the diet-induced obesity mouse model. Ruvonoflast is promising for research of neurodegenerative disorders, including Alzheimer’s disease, Parkinson’s disease, multiple sclerosis, and amyotrophic lateral sclerosis .
|
-
- HY-N1983
-
|
|
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
- HY-103565AR
-
|
|
Reference Standards
mGluR
|
Neurological Disease
|
|
AMN082 (free base) (Standard) is the analytical standard of AMN082 (free base). This product is intended for research and analytical applications. AMN082 free base, a selective, orally active, and brain penetrant mGluR7 agonist, directly activates receptor signaling via an allosteric site in the transmembrane domain. AMN082 free base potently inhibits cAMP accumulation and stimulates GTPγS binding (EC50 values, 64-290 nM) at transfected mammalian cells expressing mGluR7. AMN082 free base shows selectivity over other mGluR subtypes and selected ionotropic glutamate receptors. Antidepressant effects .
|
-
- HY-D0714
-
|
2,3,5-Triphenyltetrazolium chloride; TPTZ; TTC
|
Biochemical Assay Reagents
|
Cardiovascular Disease
|
|
Tetrazolium Red (2,3,5-Triphenyltetrazolium chloride; TTC) is a not brain-penetrant, colorless, water-soluble dye that is reduced by mitochondrial enzymes to a deep red, water-insoluble compound (formazan) mainly in the mitochondria of living cells. Tetrazolium Red is used to observe the activity of dehydrogenase, and it turns colorless to red when exposed to hydrogen. Tetrazolium Red distinguishes between surviving and infarcted brain tissue after stroke. Tetrazolium Red has been used to stain heart tissue to measure the extent of acute lesions and also used to stain brain tissue to detect the size of the infarcted area. The absorption wavelength of Tetrazolium Red is 570 nm .
|
-
- HY-16561
-
-
- HY-161104
-
|
|
Potassium Channel
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Kv2.1-IN-1 is an orally active and blood-brain barrier penetrant Kv2.1 inhibitor with an IC50 of 0.07 μM. Kv2.1-IN-1 exhibits a selectivity >130 fold over other K +, Na +, and Ca 2+ ion channels. Kv2.1-IN-1 decreases the apoptosis of HEK293 cells induced by H2O2. Kv2.1-IN-1 produces significant neuroprotection efficacy in middle cerebral artery occlusion (MCAO) rat. Kv2.1-IN-1 can be used for the study of ischemic stroke .
|
-
- HY-13906
-
|
(+)-Largazole
|
HDAC
|
Neurological Disease
Cancer
|
|
Largazole ((+)-Largazole) is a potent, selective, orally active and brain-penetrant class I HDAC inhibitor found in marine cyanobacteria. Largazole shows an IC50 of 0.07 nM for HDAC2. Largazole releases its active form Largazole thiol (HY-170890) after hydrolysis. Largazole has a strong inhibitory effect on SF-268, SF-295 and SH-SY5Y cells, with IC50 values of 62, 68 and 102 nM respectively Largazole can upregulate the tumor suppressor gene Pax6 to inhibit the proliferation, invasion and colony formation of glioblastoma cells. Largazole can significantly upregulated brain-derived neurotrophic factor BDNF, neuronal transcription factor Pax6, and μ-opioid receptor gene Oprm1. Largazole exerts antitumor and neuroprotective effects. Largazole can be used for researches of Glioblastoma and Alzheimer’s disease .
|
-
- HY-W009300
-
|
4-OHE1
|
Endogenous Metabolite
Estrogen Receptor/ERR
Sirtuin
MDM-2/p53
PDI
Ferroptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
Metabolic Disease
Cancer
|
|
4-Hydroxyestrone (4-OHE1) is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .
|
-
- HY-175770
-
|
|
Isocitrate Dehydrogenase (IDH)
PDK-1
Apoptosis
|
Cancer
|
|
mIDH1-IN-2 is a brain-penetrant isocitrate dehydrogenase 1 (IDH1) inhibitor. mIDH1-IN-2 shows subnanomolar potency against IDH1 R132H and R132C (IC50 = 80.0 and 58.0 nM) and minimal activity against wt-IDH1/2. mIDH1-IN-2 also inhibits PDK1 (IC50 = 0.61 μM) and reduces PDH phosphorylation dose-dependently. mIDH1-IN-2 can inhibit cells proliferation, induces S phase arrest and promotes apoptosis. mIDH1-IN-2 can be used for the research of cancer, such as glioma .
|
-
- HY-113357R
-
|
|
Reference Standards
Endogenous Metabolite
|
Neurological Disease
Inflammation/Immunology
|
|
m-Coumaric acid (Standard) is the analytical standard of m-Coumaric acid. This product is intended for research and analytical applications. m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .
|
-
- HY-103100
-
|
|
5-HT Receptor
Epigenetic Reader Domain
Akt
Ribosomal S6 Kinase (RSK)
FOXO
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
SB-699551 is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 can be used for the research of anxiety, breast cancer, and Alzheimer's disease .
|
-
- HY-13324
-
|
RTA 402; NSC 713200; CDDO Methyl ester
|
Keap1-Nrf2
SARS-CoV
Virus Protease
|
Cardiovascular Disease
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Bardoxolone (CDDO; RTA 401) methyl is an orally active and blood-brain-barrier-penetrant activator of Nrf2 and an inhibitor of SARS-CoV-2 3CL protease. Bardoxolone methyl inhibits SARS-CoV-2 replication in Vero cells with an EC50 value of 0.29 μM. Bardoxolone methyl increases levels of pNrf2 and HO-1, inhibits inflammatory mediators like pNFκB and MCP-1. Bardoxolone methyl activates the Nrf2 pathway to enhance antioxidant and anti-inflammatory responses, inhibits viral replication, and improves mitochondrial function. Bardoxolone methyl can be used in research on chemotherapy-induced neuropathic pain (CINP), COVID-19, and chronic kidney disease (CKD) .
|
-
- HY-179177
-
|
|
DYRK
CDK
Tau Protein
Amyloid-β
|
Neurological Disease
|
|
AO-365/43472821 is a selective, brain-penetrant Dual-specificity tyrosine phosphorylation-regulated kinase 1A (DYRK1A) inhibitor (IC50 = 0.29 μM) and shows a significant inhibitory effect on (CDC-like kinase 1) CLK1 (IC50 = 0.08 μM). AO-365/43472821 could protect the human neuroblastoma cell line SH-SY5Y from Okadaic acid (HY-N6785) (OA)-induced injury. AO-365/43472821 decreased tau (pSer396)/tau and Aβ1-42 protein expression. AO-365/43472821 can be used for the study of Alzheimer's disease .
|
-
- HY-P10580A
-
|
|
Cadherin
Tie
Claudin
PI3K
Akt
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Vasculotide TFA is a blood-brain barrier (BBB)-penetrant Tie2 agonist. Vasculotide TFA binds to a unique domain of Tie2, induces receptor clustering to drive phosphorylation, activates downstream PI3K/Akt and eNOS pathways, enhances inter-endothelial cell junctions (such as VE-cadherin and claudin-5), and inhibits inflammatory adhesion molecules, ultimately stabilizing the vascular endothelial barrier and reducing its permeability . Vasculotide TFA alleviates pulmonary microvascular leakage and microcirculatory dysfunction caused by cardiopulmonary bypass, acts as an adjuvant radioprotective agent to reduce acute radiation dermatitis, and promotes BBB recovery after focused ultrasound (FUS). Combination of Vasculotide TFA with antibiotics reduces lung injury .
|
-
- HY-P10580
-
|
|
Tie
PI3K
Akt
Cadherin
Claudin
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Vasculotide is a blood-brain barrier (BBB)-penetrant Tie2 agonist. Vasculotide binds to a unique domain of Tie2, induces receptor clustering to drive phosphorylation, activates downstream PI3K/Akt and eNOS pathways, enhances inter-endothelial cell junctions (such as VE-cadherin and claudin-5), and inhibits inflammatory adhesion molecules, ultimately stabilizing the vascular endothelial barrier and reducing its permeability . Vasculotide alleviates pulmonary microvascular leakage and microcirculatory dysfunction caused by cardiopulmonary bypass, acts as an adjuvant radioprotective agent to reduce acute radiation dermatitis, and promotes BBB recovery after focused ultrasound (FUS). Combination of Vasculotide with antibiotics reduces lung injury .
|
-
- HY-N1983R
-
|
|
Reference Standards
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
- HY-163121
-
|
|
Glycosyltransferase
TGF-β Receptor
FAK
Galectin
Collagen
|
Endocrinology
Cancer
|
|
PST3.1a is an orally active and brain-penetrant N-acetylglucosamine glycosyltransferase (MGAT5) inhibitor with a human IC50 of 2 µM. PST3.1a inhibits TGFβR and FAK signaling pathway activity. PST3.1a alters β1,6-GlcNAc N-glycans and microtubule/microfilament integrity, increases OLIG2 expression, and inhibits proliferation, migration, invasiveness, and clonogenic capacities of glioblastoma initiating cells. PST3.1a reduces invasive and proliferative capacity of glioblastoma initiating cells in orthotopic graft models, increases overall survival of orthotopic graft model mice. PST3.1a blunts MGAT5 overexpression, decreases renal fibrosis via collagen 1, collagen 4, and galectin 3 downregulation in a rat chronic kidney disease model. PST3.1a can be used for the research of glioblastoma multiforme and chronic kidney disease .
|
-
- HY-N2392
-
|
|
Parasite
Lipoxygenase
Opioid Receptor
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Interleukin Related
TNF Receptor
PGE synthase
COX
|
Infection
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE2, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease .
|
-
- HY-136700
-
|
|
5-HT Receptor
Akt
|
Neurological Disease
Cancer
|
|
SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease .
|
-
- HY-128879A
-
|
|
Phosphodiesterase (PDE)
GSK-3
Tau Protein
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
|
|
VP3.15 dihydrobromide is a highly potent, orally bioavailable, and CNS-penetrant PDE7-GSK3 dual inhibitor, with IC50 values of 1.59 μM and 0.88 μM against PDE7 and GSK3, respectively . VP3.15 dihydrobromide elevates intracellular cAMP levels, suppresses immune responses, enhances remyelination, limits excessive tau phosphorylation, and alleviates neuroinflammation and neuronal loss. VP3.15 dihydrobromide promotes oligodendrocyte precursor cell differentiation, improves in vivo remyelination, inhibits autoimmune encephalomyelitis, and mitigates germinal matrix-intraventricular hemorrhage-related brain injury, cerebral atrophy, ventricular enlargement, and cognitive impairment. VP3.15 dihydrobromide can be used in research related to multiple sclerosis and germinal matrix-intraventricular hemorrhage .
|
-
- HY-W009300S
-
|
4-OHE1-d4
|
Endogenous Metabolite
Isotope-Labeled Compounds
Estrogen Receptor/ERR
Sirtuin
MDM-2/p53
PDI
Ferroptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
Metabolic Disease
Cancer
|
|
4-Hydroxyestrone (4-OHE1)-d4 is the deuterium labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .
|
-
- HY-181889
-
|
|
Ras
|
Cancer
|
|
KRAS G12C-IN-75 is an orally active, blood-brain barrier penetrant KRAS G12C inhibitor with an IC50 of 0.53 nM. KRAS G12C-IN-75 attenuates active transport mediated by P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP). KRAS G12C-IN-75 inhibits tumor growth, regulates the expression of downstream MAPK target genes DUSP6 and SPRY4, and exhibits dose-dependent KRAS G12C alkylation in KRAS G12C-positive xenograft models. KRAS G12C-IN-75 can be used for research related to non-small cell lung cancer .
|
-
- HY-W009300S1
-
|
4-OHE1-13C6
|
Isotope-Labeled Compounds
Endogenous Metabolite
Estrogen Receptor/ERR
Sirtuin
MDM-2/p53
PDI
Ferroptosis
Reactive Oxygen Species (ROS)
|
Neurological Disease
Metabolic Disease
Cancer
|
|
4-Hydroxyestrone (4-OHE1)- 13C6 is a 13C-labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .
|
-
- HY-N0430
-
|
Coptisin
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
- HY-181613
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
5-HT2A&5-HT2C agonist-3 (compound 4e) is an orally bioavailable and blood-brain barrier penetrant agonist of 5-HT2A and 5-HT2C. 5-HT2A&5-HT2C agonist-3 increases intracellular calcium levels in cells overexpressing 5-HT2A or 5-HT2C receptors, and shows no activity against 5-HT2B receptors. 5-HT2A&5-HT2C agonist-3 can be used for the research of neuropsychiatric disorders .
|
-
- HY-178356
-
|
|
Cholinesterase (ChE)
nAChR
Interleukin Related
TNF Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
BChE-IN-44 is a potent, brain-penetrant, highly selective BChE inhibitor [equine BChE IC50 = 18.00 pM, human BChE IC50 = 1.50 nM]. BChE-IN-44 shows neuroprotective effects against the Aβ1-42-induced injury model and inhibitory effects on Aβ1-42 self-aggregation. BChE-IN-44 reduces the levels of inflammatory factors (NO, IL-6, and TNF-α) in Lipopolysaccharides (HY-D1056)-induced BV2 cells. BChE-IN-44 can significantly ameliorate Scopolamine (HY-N0296)-induced cognition impairment. BChE-IN-44 exhibits capacity in the regulation of BChE and acetylcholine levels in the mouse hippocampus. BChE-IN-44 can be used for the study of Alzheimer’s disease (AD) .
|
-
- HY-N0430A
-
|
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
- HY-181160
-
|
|
JNK
Wnt
β-catenin
Amyloid-β
Reactive Oxygen Species (ROS)
Beclin1
GSK-3
Beta-secretase
|
Neurological Disease
|
|
JNK3/Wnt/β-catenin modulator-1 is a brain-penetrant JNK3 inhibitor and Wnt/β-catenin activator. JNK3/Wnt/β-catenin modulator-1 decreases Aβ1-42 production and reduced ROS generation. JNK3/Wnt/β-catenin modulator-1 inhibits the activation of JNK and Puma, promotes Beclin-1 expression, reduces GSK-3β and BACE1 expression and activates Wnt/β-catenin signaling. JNK3/Wnt/β-catenin modulator-1 improves cognitive and memory performance, attenuates histopathological brain damage, preserves structure of hippocampal pyramidal cells and cerebral cortical neurons. JNK3/Wnt/β-catenin modulator-1 can be used for the research of Alzheimer's disease .
|
-
- HY-181559S
-
|
AG06827
|
mAChR
|
Neurological Disease
|
|
VU6025733 (AG06827) is a highly selective, orally active and blood-brain barrier-penetrant positive allosteric modulator of the muscarinic acetylcholine receptor subtype M4 (M4 mAChR). VU6025733 exerts a potentiating effect on acetylcholine-induced receptor activation with an EC50 of 23 nM for hM4 and 55 nM for rM4. VU6025733 shows high selectivity over other muscarinic acetylcholine receptor subtypes, dose-dependently reduces amphetamine-induced hyperlocomotion in rats. VU6025733 is applicable to the research of schizophrenia, Parkinson's disease, and Alzheimer's disease .
|
-
-
-
HY-L028
-
|
|
1,096 compounds
|
|
The blood-brain barrier (BBB) is the complex network of brain microvessels. It protects the brain from the external bloodstream environment and supplies the brain with the required nutrients for normal function. However, blood-brain barrier is also the obstacle to deliver beneficial drugs to treat CNS (central nervous system) diseases or brain tumors, as it has the least permeable capillaries in the entire body due to physical barriers (tight junctions). Therefore, it is crucial to discover drugs which can cross this barrier for the treatment of brain-based diseases, such as Alzheimer’s disease (AD), Parkinson’s disease (PD) and epilepsy.
MCE offers a unique collection of 1,096 compounds with confirmed CNS-Penetrant property. It’s a useful tool for the discovery of drugs used for brain diseases, such as brain tumors, mental disorders, and neurodegenerative diseases.
|
-
-
HY-L093
-
|
|
454 compounds
|
|
Food additives are substances added to food to maintain or improve its safety, freshness, taste, texture, or appearance. All food additives used in food undergo a safety assessment, which includes rigorous testing, before they are approved, so all food additives are generally recognized as safe substances.
MCE supplies 454 approved food additives which are safe substances and can be used for drug discovery and other research.
|
-
-
HY-L061
-
|
|
5,259 compounds
|
|
Most of the drugs that are available in the marketplace are administered via the oral route, which is a convenient and cost effective route of administration. Thus, oral bioavailability is one of the key considerations in drug design and development. A high oral bioavailability reduces the amount of an administered drug necessary to achieve a desired pharmacological effect and therefore could reduce the risk of side-effects and toxicity. A poor oral bioavailability can result in low efficacy and higher inter-individual variability and therefore can lead to unpredictable response to a drug. Low oral bioavailability in clinical trials is a major reason for drug candidates failing to reach the market.
MCE offers a unique collection of 5,259 compounds with confirmed high oral bioavailability. MCE Orally Active Compound Library is a useful tool for discovering new drugs with oral bioavailability.
|
| Cat. No. |
Product Name |
Type |
-
- HY-D0714
-
|
2,3,5-Triphenyltetrazolium chloride; TPTZ; TTC
|
Biochemical Assay Reagents
|
|
Tetrazolium Red (2,3,5-Triphenyltetrazolium chloride; TTC) is a not brain-penetrant, colorless, water-soluble dye that is reduced by mitochondrial enzymes to a deep red, water-insoluble compound (formazan) mainly in the mitochondria of living cells. Tetrazolium Red is used to observe the activity of dehydrogenase, and it turns colorless to red when exposed to hydrogen. Tetrazolium Red distinguishes between surviving and infarcted brain tissue after stroke. Tetrazolium Red has been used to stain heart tissue to measure the extent of acute lesions and also used to stain brain tissue to detect the size of the infarcted area. The absorption wavelength of Tetrazolium Red is 570 nm .
|
-
- HY-109521A
-
|
Manganese(Ⅱ) chloride tetrahydrate, molecular biology grade,≥99.0% (KT)
|
Biochemical Assay Reagents
|
|
Manganese chloride (tetrahydrate), molecular biology grade,≥99.0% (KT) is an orally active and a blood-brain barrier penetrant compound. It affects the activities of multiple enzymes in cells, such as regulating the activities of histone acetyltransferase (HAT) and histone deacetylase (HDAC), thereby affecting gene expression. It has multiple activities such as neurotoxicity, embryotoxicity, and reproductive toxicity. It is currently mainly used in neurodegenerative diseases and toxicology research.
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P10580
-
|
|
Tie
PI3K
Akt
Cadherin
Claudin
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Vasculotide is a blood-brain barrier (BBB)-penetrant Tie2 agonist. Vasculotide binds to a unique domain of Tie2, induces receptor clustering to drive phosphorylation, activates downstream PI3K/Akt and eNOS pathways, enhances inter-endothelial cell junctions (such as VE-cadherin and claudin-5), and inhibits inflammatory adhesion molecules, ultimately stabilizing the vascular endothelial barrier and reducing its permeability . Vasculotide alleviates pulmonary microvascular leakage and microcirculatory dysfunction caused by cardiopulmonary bypass, acts as an adjuvant radioprotective agent to reduce acute radiation dermatitis, and promotes BBB recovery after focused ultrasound (FUS). Combination of Vasculotide with antibiotics reduces lung injury .
|
-
- HY-P10019
-
|
NLY01
|
GCGR
|
Neurological Disease
Inflammation/Immunology
|
|
Pegsebrenatide (NLY01) is a blood-brain barrier-penetrant GLP-1R agonist. Pegsebrenatide alleviates retinal inflammation and neuronal death secondary to ocular hypertension . Pegsebrenatide significantly delays onset and reduces disease severity in experimental autoimmune encephalomyelitis . Pegsebrenatide inhibits the formation of A1 reactive astrocytes in nerve cells and reduces the loss of retinal ganglion cells and dopaminergic neurons. Pegsebrenatide exerts neuroprotective effects in a mouse model of Parkinson's disease by directly preventing microglia-mediated conversion of astrocytes to the A1 neurotoxic phenotype. Pegsebrenatide can be used for research on glaucoma, Parkinson's disease, and multiple sclerosis .
|
-
- HY-P10862
-
|
|
Exosomes
Virus Protease
|
Infection
Cancer
|
AH-D peptide is a brain-penetrant antiviral agent disrupting highly curved lipid membranes. AH-D peptide exhibits broad-spectrum antiviral activity against ZIKV, Dengue virus, Chikungunya virus, yellow fever virus and Japanese encephalitis virus, with
IC50 values of 11.9, 12.5, 35.7, 206 and 136 nM, respectively. AH-D peptide reduces the viral load in the brain, suppresses inflammation, protects neurons, and does not damage the blood brain barrier. AH-D peptide restores antitumor immunity by decreasing circulating PD-L1 + exosomes, reducing intratumoral immunosuppressive cells (regulatory T cells, myeloid-derived suppressor cells), and enhancing T cell function. AH-D peptide inhibits membrane-enveloped viruses and cancer cell metastasis in vivo. AH-D peptide exhibits no immunogenicity and has negligible effects on normal tissues. AH-D peptide can be used for research in Zika virus and other mosquito-borne viruses, cancer immunotherapy and metastasis .
|
-
- HY-P10580A
-
|
|
Cadherin
Tie
Claudin
PI3K
Akt
|
Cardiovascular Disease
Infection
Inflammation/Immunology
|
|
Vasculotide TFA is a blood-brain barrier (BBB)-penetrant Tie2 agonist. Vasculotide TFA binds to a unique domain of Tie2, induces receptor clustering to drive phosphorylation, activates downstream PI3K/Akt and eNOS pathways, enhances inter-endothelial cell junctions (such as VE-cadherin and claudin-5), and inhibits inflammatory adhesion molecules, ultimately stabilizing the vascular endothelial barrier and reducing its permeability . Vasculotide TFA alleviates pulmonary microvascular leakage and microcirculatory dysfunction caused by cardiopulmonary bypass, acts as an adjuvant radioprotective agent to reduce acute radiation dermatitis, and promotes BBB recovery after focused ultrasound (FUS). Combination of Vasculotide TFA with antibiotics reduces lung injury .
|
| Cat. No. |
Product Name |
Target |
Research Area |
Image |
-
- HY-P9999
-
|
RG6102; RO-7126209
|
Amyloid-β
|
Neurological Disease
|
|
Trontinemab (RG6102) is a brain-penetrant, anti-amyloid, bispecific and humanizedized IgG1-κ antibody, targeting to Aβ plaques and transferrin receptor 1 (TFR1). Trontinemab binds to fibrillar Aβ as well as Aβ plaques triggering plaque clearance by engaging immune cells on Alzheimer disease (AD) brain sections. Trontinemab also shows specific affinity to cynomolgus and human TFR1 .
|
-
(5)
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-16561
-
-
-
- HY-17363
-
-
-
- HY-W015309
-
-
-
- HY-N2392
-
|
|
Cardiovascular Disease
Alkaloids
Structural Classification
other families
Classification of Application Fields
Other Alkaloids
Phenols
Polyphenols
Plants
Disease Research Fields
Source Classification
|
Parasite
Lipoxygenase
Opioid Receptor
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Interleukin Related
TNF Receptor
PGE synthase
COX
|
|
Kukoamine A, a spermine alkaloid, is an orally active and brain-penetrant component found in the root barks of Lycium chinense (L. chinense) Miller. Kukoamine A inhibits purified Crithidia fasciculata trypanothione reductase and soybean lipoxygenase, activates μ-opioid receptor. Kukoamine A can inhibt cancer cell proliferation, migration and invasion, cause G0/G1 phase cell cycle arrest and induce apoptosis. Kukoamine A exerts neuroprotective effect and can induce autophagy . Kukoamine A inhibits LPS (HY-D1056)-induced NO, ROS, PGE2, TNF-α, IL-1β, IL-6 production and COX-2 activity. Kukoamine A reverses palmitic acid-induced insulin resistance, lipid accumulation, and oxidative stress via downregulation of Srebp-1c. Kukoamine A can be used for the research of cancer, infection, inflammation, metabolic and neurological disease, such as glioblastoma and Parkinson's disease .
|
-
-
- HY-113357
-
-
-
- HY-N1983
-
|
|
Structural Classification
Classification of Application Fields
Asclepiadaceae
Cynanchum otophyllum Schneid．
Cynanchum auriculatum Royle ex Wight
Plants
Disease Research Fields
Steroids
Source Classification
Cancer
|
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
|
Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
-
- HY-N0430
-
|
Coptisin
|
Alkaloids
Structural Classification
Classification of Application Fields
Coptis chinensis Franch.
Ranunculaceae
Metabolic Disease
Quinoline Alkaloids
Plants
Disease Research Fields
Source Classification
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
|
Coptisine is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine can be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
-
- HY-N0430A
-
|
|
Alkaloids
Structural Classification
Chelidonium majus
Classification of Application Fields
Metabolic Disease
Quinoline Alkaloids
Plants
Disease Research Fields
Papaveraceae
Source Classification
|
Indoleamine 2,3-Dioxygenase (IDO)
NF-κB
p38 MAPK
PI3K
Akt
Apoptosis
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
DNA/RNA Synthesis
ROCK
LDLR
|
|
Coptisine Sulfate is an orally active and brain-penetrant alkaloid found in Coptis chinensis. Coptisine Sulfate is a reversible, uncompetitive IDO inhibitor with a Ki of 5.8 μM and an IC50 of 6.3 μM. Coptisine Sulfate suppresses neuroinflammation, reduces Aβ plaque burden and shows neuroprotective activity. Coptisine Sulfate shows anti-inflammation activity by blocking NF-κB, MAPK, and PI3K/Akt activation. Coptisine Sulfate inhibits cancer cells proliferation, induces DNA damage, G2/M phase cell cycle arrest, apoptosis, ROS production and mitochondrial dysfunction. Coptisine Sulfate inhibits Rho/ROCK pathway activation, reduces arrhythmia, limits cardiac injury marker release, reduces infarct size, and preserves cardiac function in rat myocardial ischemia/reperfusion models. Coptisine Sulfate downregulates HMGCR and upregulates LDLR and CYP7A1 to modulate cholesterol metabolism, reduces abnormal serum lipid levels, and promotes fecal bile acid excretion. Coptisine Sulfate be used for the research of cancer, hypercholesterolemia, Alzheimer’s disease, inflammatory disorders and cardiovascular disease .
|
-
-
- HY-W674241A
-
-
-
- HY-W009300
-
-
-
- HY-17363R
-
-
-
- HY-N6685
-
-
-
- HY-13906
-
|
(+)-Largazole
|
Structural Classification
Natural Products
Microorganisms
Source Classification
|
HDAC
|
|
Largazole ((+)-Largazole) is a potent, selective, orally active and brain-penetrant class I HDAC inhibitor found in marine cyanobacteria. Largazole shows an IC50 of 0.07 nM for HDAC2. Largazole releases its active form Largazole thiol (HY-170890) after hydrolysis. Largazole has a strong inhibitory effect on SF-268, SF-295 and SH-SY5Y cells, with IC50 values of 62, 68 and 102 nM respectively Largazole can upregulate the tumor suppressor gene Pax6 to inhibit the proliferation, invasion and colony formation of glioblastoma cells. Largazole can significantly upregulated brain-derived neurotrophic factor BDNF, neuronal transcription factor Pax6, and μ-opioid receptor gene Oprm1. Largazole exerts antitumor and neuroprotective effects. Largazole can be used for researches of Glioblastoma and Alzheimer’s disease .
|
-
-
- HY-113357R
-
|
|
Structural Classification
Monophenols
Microorganisms
Ketones, Aldehydes, Acids
Phenols
Endogenous metabolite
Source Classification
|
Reference Standards
Endogenous Metabolite
|
|
m-Coumaric acid (Standard) is the analytical standard of m-Coumaric acid. This product is intended for research and analytical applications. m-Coumaric acid is a polyphenol metabolite from caffeic acid, formed by the gut microflora and the amount in human biofluids is diet-dependant. m-Coumaric acid is a BBB-penetrant metabolite of chlorogenic acid. m-Coumaric acid stimulates the cerebral nerves in vitro. m-Coumaric acid can evoke neurite outgrowth in hippocampal neuronal cells. m-Coumaric acid can promote neuronal differentiation. m-Coumaric acid increases spontaneous locomotor activity in mice by acting on the central nervous system. m-Coumaric acid inhibits the oxidation of L-dopa by epidermis tyrosinase. m-Coumaric acid attenuates non-catalytic protein glycosylation in retinas of diabetic rats .
|
-
-
- HY-N1983R
-
|
|
Structural Classification
Asclepiadaceae
Cynanchum otophyllum Schneid．
Cynanchum auriculatum Royle ex Wight
Plants
Steroids
Source Classification
|
Reference Standards
Apoptosis
Autophagy
Reactive Oxygen Species (ROS)
Mitochondrial Metabolism
PARP
Caspase
Bcl-2 Family
VEGFR
FAK
WDR5
p38 MAPK
JNK
PPAR
|
|
Caudatin (Standard) is the analytical standard of Caudatin (HY-N1983). This product is intended for research and analytical applications. Caudatin is an orally active and brain-penetrant C-21 steroidal found in Cynanchum bungei decne with a variety of biological activities. Caudatin can inhibit cell proliferation, migration, invasion, cause cell phase arrest, induce apoptosis, autophagy, ROS prodution and loss of mitochondrial membrane potential. Caudatin activates PARP, caspase-3, -7, -9, upregulates pro-apoptotic Bad and Bax and downregulates anti-apoptotic Bcl-2 and Bcl-XL. Caudatin suppresses VEGF, FAK phosphorylation, upregulates p21, p27, DR5 protein expression, activates the p38 MAPK, JNK and PPARα/TFEB-mediated autophagy-lysosomal signaling pathways. Caudatin can be used for the research of cancer, inflammation and neurological disease, such as glioma and Alzheimer's disease .
|
-
-
- HY-N6685R
-
-
-
- HY-13764A
-
|
|
Alkaloids
Stephania japonica var. discolor (Blume) Forman
Plants
Menispermaceae
Alkaloid Dimers
Source Classification
|
Calcium Channel
|
|
dl-Tetrandrine is an orally active and brain-penetrant calcium channel blocker that inhibits voltage-dependent calcium channels. dl-Tetrandrine selectively blocks Ca 2+ influx with an IC50 value of approximately 1-10 μM. dl-Tetrandrine exerts anti-inflammatory, immunosuppressive, and anti-arrhythmic activities by inhibiting intracellular calcium overload, and can reverse multidrug resistance in tumor cells. dl-Tetrandrine is promising for research of autoimmune diseases (such as rheumatoid arthritis), cardiovascular diseases, and tumor drug resistance reversal .
|
-
-
- HY-W015309R
-
|
|
Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Endogenous metabolite
Source Classification
|
Reference Standards
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
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Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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- HY-N2332
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Chemical Structure |
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- HY-17363S1
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Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate . Dimethyl fumarate (DMF) is an orally active and brain-penetrant Nrf2 activator and induces upregulation of antioxidant gene expression. Dimethyl fumarate induces necroptosis in colon cancer cells through GSH depletion/ROS increase/MAPKs activation pathway, and also induces cell autophagy. Dimethyl fumarate can be used for multiple sclerosis research .
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- HY-W266188
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Decanoic acid- 13C is the 13C-labeled Decanoic acid (HY-W015309). Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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- HY-B0688S2
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Dapsone- 13C12 is the 13C12 labeled Dapsone (HY-B0688). Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities. Dapsone exerts effective antileprosy activity and inhibits folate synthesis in cell extracts of M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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- HY-11063S
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Fingolimod-d4 is the deuterium labeled Fingolimod. Fingolimod (FTY720 free base) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod also is a pak1 activator, a immunosuppressant .
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- HY-B0688S
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Dapsone-d8 is a deuterium labeled Dapsone. Dapsone is an orally active and blood-brain penetrant sulfonamide antibiotic with antibacterial, antigenic and anti-inflammatory activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone can be used as an anticonvulsant and also in the research of skin and glioblastoma diseases .
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- HY-B0688S1
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Dapsone-d4 is the deuterium labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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- HY-B0568S
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Deferiprone-d3 is the deuterium labeled Deferiprone (HY-B0568). Deferiprone is a potent, orally active, brain-penetrant, cell-penetrant, skin-permeable, free iron chelating agent. Deferiprone inhibits the proliferation and migration, and stimulates apoptosis in tumor cell. Deferiprone can inhibit KDM. Deferiprone has antianemic, neuroprotective, anti-inflammatory, antioxidant, and antidotal activity. Deferiprone can be used in cancer, cardiovascular disease, infection, inflammation, and neurological disease study .
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- HY-B0534S1
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Moclobemide-d4 is deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
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- HY-11063S1
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Fingolimod-d4 (hydrochloride) is the deuterium labeled Fingolimod hydrochloride. Fingolimod hydrochloride (FTY720) is a brain-penetrant sphingosine 1-phosphate (S1P) antagonist with an IC50 of 0.033 nM in K562 and NK cells. Fingolimod hydrochloride (FTY720) also is a pak1 activator, a immunosuppressant .
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- HY-B0534S
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Moclobemide-d8 (Ro111163-d8) is the deuterium labeled Moclobemide. Moclobemide (Ro111163) is a brain-penetrant and reversible monoamine oxidase (MAO-A) inhibitor with an IC50 of 6.061 μM for hMAO-A .Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
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- HY-N6685S1
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3-Acetyldeoxynivalenol (3-AcDON; 3ADON)- 13C17 is the 13C labeled 3-Acetyldeoxynivalenol (HY-N6685). 3-Acetyldeoxynivalenol, a trichothecene mycotoxin deoxynivalenol (DON) acetylated derivative, is a brain-penetrant Fusarium mycotoxin. 3-Acetyldeoxynivalenol induces mRNA expression and production of inflammatory chemokine IL-8 in intestinal cells .
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- HY-B0688S3
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Dapsone- 15N2 (4,4′-Diaminodiphenyl sulfone- 15N2) is 15N labeled Dapsone. Dapsone (4,4′-Diaminodiphenyl sulfone) is an orally active and blood-brain penetrant sulfonamide antibiotic with bacteriostatic, antimycobacterial and antiprotozoal activities . Dapsone?exerts effective antileprosy activity?and inhibits folate synthesis in cell extracts of?M. leprae. Dapsone is used for dermatologic disorder research, including leprosy, dermatitis herpetiformis, acne vulgaris et al .
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- HY-17383S
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Levomefolate- 13C5 calcium)is the 13C-labeled Levomefolate calcium (HY-17383). Levomefolate calcium is a synthetic calcium salt of L-5-methyltetrahydrofolate and an orally active and brain-penetrant folate supplement. Levomefolate calcium incorporates into body folate pools to increase plasma and red blood cell folate levels over time. Levomefolate calcium does not significantly increase folate concentrations in breast milk. Levomefolate calcium can be used for the research of neural tube defects and megaloblastic anemia .
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- HY-W009300S
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4-Hydroxyestrone (4-OHE1)-d4 is the deuterium labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .
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- HY-W009300S1
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4-Hydroxyestrone (4-OHE1)- 13C6 is a 13C-labeled 4-Hydroxyestrone (HY-W009300). 4-Hydroxyestrone is a brain-penetrant estrogen metabolite. 4-Hydroxyestrone shows neuroprotective effects involving increased cytoplasmic localization of p53 resulting from SIRT1-mediated p53 deacetylation. 4-Hydroxyestrone relies on PDI to mediate its protective effect against chemically induced ferroptosis in estrogen receptor-negative cancer cells. 4-Hydroxyestrone inhibits lipid peroxidation and lipid-ROS accumulation. 4-Hydroxyestrone blocks preovulatory luteinizing hormone surges in Rattus norvegicus. 4-Hydroxyestrone can be used for the researches of neurodegeneration, breast cancer and endocrine disease .
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- HY-112870AS
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Firmonertinib-d3 (Alflutinib-d3) mesylate is the deuterium labeled Firmonertinib mesylate (HY-112870A). Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and blood-brain barrier penetrant EGFR inhibitor. Firmonertinib mesylate inhibits EGFR active mutations as well as the T790M acquired resistant mutation. Firmonertinib mesylate has the potential for the research of cancer diseases, especially advanced non-small cell lung cancer (NSCLC) with EGFR ex20ins mutation.
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- HY-178164
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Alkynes
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HBS-101 is a selectively, orally active, brain-penetrant, Midkine (MDK) inhibitor (KD = 38.4 nM). HBS-101 significantly reduces cell viability, clonogenic survival, and invasiveness and increases apoptosis. HBS-101 involves suppression of the Akt/mTOR, STAT3, and NF-κB pathways. HBS-101 can be used for the study of Triple-negative breast cancer (TNBC) .
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