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Results for "

cell penetrant

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55

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6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145899

    PKC Cancer
    PKN1/2-IN-1 is a potent, cell penetrant and selective PKN2 (PRK2) inhibitor (IC50=16 nM; Ki=8 nM) .
    PKN1/2-IN-1
  • HY-12776
    GSK805
    3 Publications Verification

    ROR Inflammation/Immunology
    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 .
    GSK805
  • HY-118140

    Cannabinoid Receptor Neurological Disease Inflammation/Immunology
    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 .
    ZCZ011
  • HY-119351

    HIF/HIF Prolyl-Hydroxylase Others
    BNS is a cell penetrant, potent and selective PHD2 (prolyl-hydroxylase 2) inhibitor .
    BNS
  • HY-109566
    AZD1390
    5+ Cited Publications

    ATM/ATR Inflammation/Immunology Cancer
    AZD1390 is a potent, highly selective, orally bioavailable, brain-penetrant ATM inhibitor with an IC50 of 0.78 nM in cell .
    AZD1390
  • 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 .
    KT185
  • HY-B0568
    Deferiprone
    35+ Cited Publications

    Ferroptosis HCV Apoptosis COX Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Endocrinology Cancer
    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 .
    Deferiprone
  • 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 .
    D942
  • HY-B0568R

    Ferroptosis HCV Apoptosis COX Infection Cardiovascular Disease Neurological Disease Inflammation/Immunology Endocrinology Cancer
    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 .
    Deferiprone (Standard)
  • HY-P10651

    Bacterial Infection
    Lifeact peptide is a fusion structure of BP100 bound to actin. BP100 (KKLFKKILKYL-amide) is an antimicrobial peptide against plant pathogens that acts as a fast and effective cell penetrant to transport fluorescent test cargo into the cytoplasm of plant cell walls .
    Lifeact peptide
  • HY-B0534

    Ro111163

    Monoamine Oxidase Neurological Disease
    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.
    Moclobemide
  • HY-133554

    MAP3K p38 MAPK Inflammation/Immunology
    ASK1-IN-1 is a CNS-penetrant ASK1 (apoptosis signal-regulating kinase 1) inhibitor, with good potency (cell IC50=138 nM; Biochemical IC50=21 nM) .
    ASK1-IN-1
  • HY-17363
    Dimethyl fumarate
    25+ Cited Publications

    Keap1-Nrf2 Reactive Oxygen Species HIV Autophagy Endogenous Metabolite Infection Neurological Disease Inflammation/Immunology Cancer
    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 .
    Dimethyl fumarate
  • HY-14569
    CDPPB
    1 Publications Verification

    mGluR Neurological Disease
    CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents .
    CDPPB
  • HY-109192
    Tolebrutinib
    5 Publications Verification

    SAR442168; PRN2246

    Btk Neurological Disease
    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) .
    Tolebrutinib
  • HY-148787

    SAR443820; DNL788

    RIP kinase Neurological Disease Inflammation/Immunology
    Oditrasertib (SAR443820) is an orally active and brain-penetrant receptor-interacting protein kinase 1 (RIPK1) inhibitor with an IC50 value lower than 100 nM. Oditrasertib could make nerve cells more resistant to the pathology and slow down the disease. Oditrasertib can be used for the research of neurodegenerative diseases involving inflammation or cell death .
    Oditrasertib
  • 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[1].Moclobemide up-regulates proliferation of hippocampal progenitor cells in chronically stressed mice.
    Moclobemide-d4
  • HY-133016

    MetAP Cardiovascular Disease Cancer
    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 .
    M8891
  • HY-150791

    Reactive Oxygen Species 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 .
    FLDP-5
  • HY-102050

    Phosphodiesterase (PDE) Neurological Disease
    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 .
    PF-05085727
  • HY-B0534R

    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.
    Moclobemide (Standard)
  • HY-17363R

    Keap1-Nrf2 Reactive Oxygen Species HIV Autophagy Endogenous Metabolite Infection Neurological Disease Inflammation/Immunology Cancer
    Dimethyl fumarate (Standard) is the analytical standard of Dimethyl fumarate. This product is intended for research and analytical applications. 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 .
    Dimethyl fumarate (Standard)
  • HY-116761
    GSK467
    3 Publications Verification

    Histone Demethylase Cancer
    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 .
    GSK467
  • 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.
    Moclobemide-d8
  • 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 .
    ST-401
  • 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 .
    AGH-107
  • HY-124761

    Polo-like Kinase (PLK) Autophagy Cancer
    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 .
    Poloppin
  • HY-17363S1

    Autophagy HIV Keap1-Nrf2 Endogenous Metabolite Reactive Oxygen Species Cancer
    Dimethyl fumarate-d2 is the deuterium labeled Dimethyl fumarate[1]. 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[2][3].
    Dimethyl fumarate-d2
  • HY-136731

    DNA/RNA Synthesis Cancer
    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 .
    APE1-IN-1
  • HY-112870A
    Firmonertinib mesylate
    3 Publications Verification

    Alflutinib mesylate; Furmonertinib mesylate; AST2818 mesylate

    EGFR Cancer
    Firmonertinib (Alflutinib; Furmonertinib) mesylate is is an orally active, mutant-selective, and highly brain 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 .
    Firmonertinib mesylate
  • HY-114153
    PLX5622
    Maximum Cited Publications
    50 Publications Verification

    c-Fms Neurological Disease
    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
  • HY-131891

    mAChR Neurological Disease
    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 .
    JHU37152
  • HY-112870
    Firmonertinib
    3 Publications Verification

    Alflutinib; Furmonertinib; AST2818

    EGFR Cancer
    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 .
    Firmonertinib
  • HY-B0688
    Dapsone
    2 Publications Verification

    4,4′-Diaminodiphenyl sulfone; DDS

    Antibiotic Parasite Bacterial Reactive Oxygen Species Infection Inflammation/Immunology
    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 .
    Dapsone
  • HY-131881
    JHU37160
    1 Publications Verification

    mAChR Neurological Disease
    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 .
    JHU37160
  • HY-B0688S

    4,4′-Diaminodiphenyl sulfone-d8; DDS-d8

    Antibiotic Parasite Bacterial Reactive Oxygen Species Infection Inflammation/Immunology Cancer
    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[1]. 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[2][3][4][5].
    Dapsone-d8
  • 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 .
    Everafenib
  • HY-18750A

    AZD3759 hydrochloride

    EGFR Apoptosis Cancer
    Zorifertinib (AZD3759) hydrochloride is a potent, orally active, central nervous system-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 .
    Zorifertinib hydrochloride
  • HY-18750
    Zorifertinib
    5+ Cited Publications

    AZD3759

    EGFR Apoptosis Cancer
    Zorifertinib (AZD3759) is a potent, orally active, central nervous system-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 .
    Zorifertinib
  • HY-106634
    Mitoguazone
    1 Publications Verification

    Methylglyoxal-bis(guanylhydrazone); MGBG; Methyl-GAG

    HIV Apoptosis Infection Cancer
    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 .
    Mitoguazone
  • HY-120596

    PPAR Neurological Disease
    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 .
    PPARδ/γ agonist 1 sodium
  • HY-119282

    mGluR Neurological Disease
    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 .
    AZD6538
  • HY-B0688S1

    4,4′-Diaminodiphenyl sulfone-d4; DDS-d4

    Antibiotic Parasite Bacterial Reactive Oxygen Species 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[1]. 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[2][3].
    Dapsone-d4
  • HY-103565

    mGluR Neurological Disease
    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 .
    AMN082
  • 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 plaques and transferrin receptor 1 (TFR1). Trontinemab binds to fibrillar as well as plaques triggering plaque clearance by engaging immune cells on Alzheimer disease (AD) brain sections. Trontinemab also shows specific affinity to cynomolgus and human TFR1 .
    Trontinemab
  • HY-W015309
    Decanoic acid
    1 Publications Verification

    iGluR Tyrosinase c-Met/HGFR Glutaminase Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
    Decanoic acid
  • HY-119939

    HDAC Cancer
    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 .
    CHDI-390576
  • HY-B0688R

    Antibiotic Parasite Bacterial Reactive Oxygen Species 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 .
    Dapsone (Standard)
  • 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 .
    AMN082 free base
  • HY-B0688S2

    4,4′-Diaminodiphenyl sulfone-13C12; DDS-13C12

    Isotope-Labeled Compounds Antibiotic Parasite Bacterial Reactive Oxygen Species Infection Inflammation/Immunology
    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 .
    Dapsone-13C12

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