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Results for "

BBB-penetrated

" in MedChemExpress (MCE) Product Catalog:

53

Inhibitors & Agonists

2

Fluorescent Dye

5

Peptides

1

Inhibitory Antibodies

2

Isotope-Labeled Compounds

2

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-163369
    HDAC6-IN-35

    		HDAC Cancer
    HDAC6-IN-35 (compound C4 (ZINC000077541942)) is a potent and BBB-penetrated HDAC6 inhibitor with the IC50 of 4.7 μM. HDAC6-IN-35 shows cell toxicity against MDA-MB-231 with EC50 of 40.6 μM .
    HDAC6-IN-35
  • HY-147669
    α-Synuclein inhibitor 7

    		Others Neurological Disease
    α-Synuclein inhibitor 7 (compound 3gf) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.95 μM and inhibition ratio at 30 μM of 85.8% .
    α-Synuclein inhibitor 7
  • HY-147666
    α-Synuclein inhibitor 4

    		Others Neurological Disease
    α-Synuclein inhibitor 4 (compound 3gh) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 0.98 μM and inhibition ratio at 30 μM of 91.2% .
    α-Synuclein inhibitor 4
  • HY-147667
    α-Synuclein inhibitor 5

    		Others Neurological Disease
    α-Synuclein inhibitor 5 (compound 4aa) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.22 μM and inhibition ratio at 30 μM of 94.3% .
    α-Synuclein inhibitor 5
  • HY-147668
    α-Synuclein inhibitor 6

    		Others Neurological Disease
    α-Synuclein inhibitor 6 (compound 3ge) is a potent and BBB-penetrated inhibitor of α-Synuclein (α-Syn) aggregation, with an IC50 of 1.70 μM and inhibition ratio at 30 μM of 94.4% .
    α-Synuclein inhibitor 6
  • HY-130630
    mGluR2 modulator 1

    		mGluR Neurological Disease
    mGluR2 modulator 1 (compound 95) is a potent and BBB-penetrated mGluR2 (metabotropic glutamate receptor-2) positive allosteric modulator, with an EC50 of 0.03 μM. mGluR2 modulator 1 can be used for psychosis research .
    mGluR2 modulator 1
  • HY-14759
    Aleplasinin

    PAZ-417

    		 PAI-1 Amyloid-β Neurological Disease
    Aleplasinin is an orally active, potent, BBB-penetrated and selectiveSERPINE1 (PAI-1, Plasminogen activator inhibitor-1) inhibitor. Aleplasinin increases amyloid-β (Aβ) catabolism and ameliorates amyloid-related pathology. Aleplasinin improves memory deficiency. Aleplasinin can be used for Alzheimer's disease research .
    Aleplasinin
  • HY-P2297
    TfR-T12

    		Transferrin Receptor Metabolic Disease
    TfR-T12 is a BBB-penetrated transferrin receptor (TfR) binding peptide, displaying a binding affinity in the nM range .
    TfR-T12
  • HY-147027
    PARP-1-IN-2

    		PARP Caspase Apoptosis Cancer
    PARP-1-IN-2 (compound 11g) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 149 nM. PARP1-IN-2 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549. PARP1-IN-2 can induce A549 cells apoptosis .
    PARP-1-IN-2
  • HY-P2297A
    TfR-T12 TFA

    		Transferrin Receptor Metabolic Disease
    TfR-T12 TFA is a BBB-penetrated transferrin receptor (TfR) binding peptide, displaying a binding affinity in the nM range .
    TfR-T12 TFA
  • HY-149253
    OY-201

    		Others Neurological Disease
    OY-201 is a potential and BBB-penetrated anti-ischemic stroke agent. OY-201 shows the good safety and neuroprotective activity in both in vitro and in vivo models .
    OY-201
  • HY-124813
    PDZ1i

    113B7

    		 FAK EGFR MMP Cancer
    PDZ1i is a potent, BBB-penetrated and specific MDA-9/Syntenin inhibitor. PDZ1i inhibits crucial GBM (glioblastoma multiforme) signaling involving FAK and EGFRvIII. PDZ1i reduces MMP secretion. PDZ1i can improve survival of brain tumor-bearing mice and reduce tumor invasion .
    PDZ1i
  • HY-145888
    Antioxidant agent-2

    		Amyloid-β Neurological Disease
    Antioxidant agent-2 (comp 3c), an BBB-penetrated antioxidant agent and a selective metal ions chelator, presents good neuroprotective effect and hepatoprotective effect for the study of Alzheimer’s disease .
    Antioxidant agent-2
  • HY-147681
    SUN13837

    		FGFR Neurological Disease
    SUN13837 is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. SUN13837 shows neuroprotective activity. SUN13837 can be used for neurodegenerative diseases research .
    SUN13837
  • HY-147683
    FGFR-IN-3

    		FGFR Neurological Disease
    FGFR-IN-3 (compound 6) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-3 shows neuroprotective activity. FGFR-IN-3 can be used for neurodegenerative diseases research .
    FGFR-IN-3
  • HY-146313
    BChE-IN-7

    		Cholinesterase (ChE) Neurological Disease
    BChE-IN-7 (compound 13) is a potent, selective, BBB-penetrated and reversible AChE and BChE inhibitor, with an IC50 of 0.06 μM (BChE). BChE-IN-7 can protect neuronal-like cells from toxic Aβ-species .
    BChE-IN-7
  • HY-10358
    MK-2206 dihydrochloride
    Maximum Cited Publications
    286 Publications Verification

    MK-2206 (2HCl)

    		 Organoid Akt Autophagy Apoptosis Cancer
    MK-2206 dihydrochloride (MK-2206 (2HCl)) is an orally active, BBB-penetrated allosteric AKT inhibitor with IC50s of 5 nM, 12 nM, and 65 nM for AKT1, AKT2, and AKT3, respectively. MK-2206 dihydrochloride induces autophagy .
    MK-2206 dihydrochloride
  • HY-145833A
    sEH/AChE-IN-4

    		Epoxide Hydrolase Cholinesterase (ChE) Neurological Disease Cancer
    sEH/AChE-IN-4 (compound (+)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 3.1 nM (hsEH), 1660 nM (hAChE), 179 nM (hBChE, human butyrylcholinesterase), 14.5 nM (msEH), and 102 nM (mAChE), respectively .
    sEH/AChE-IN-4
  • HY-147030
    PARP1-IN-8

    		PARP Cancer
    PARP1-IN-8 (compound 11c) is a potent and BBB-penetrated PARP1 inhibitor, with an IC50 of 97 nM. PARP1-IN-8 shows significantly potent anti-proliferative activity against Human lung adenocarcinoma epithelial cell line A549 .
    PARP1-IN-8
  • HY-145833
    sEH/AChE-IN-3

    		Epoxide Hydrolase Cholinesterase (ChE) Neurological Disease Cancer
    sEH/AChE-IN-3 (compound (−)-15) is a potent and BBB-penetrated dual inhibitor of sEH (soluble epoxide hydrolase) and AChE (acetylcholinesterase), with IC50 values of 0.4 nM (hsEH), 1.94 nM (hAChE), 615 (hBChE, human butyrylcholinesterase), 4.3 nM (msEH), and 2.61 nM (mAChE), respectively .
    sEH/AChE-IN-3
  • HY-116820
    OS-3-106

    		Dopamine Receptor Neurological Disease
    OS-3-106 is a potent, BBB-penetrated and selective dopamine D3 receptor (D3R) agonist. OS-3-106 binds with high affinity (Ki = 0.2 nM) at the D3R. OS-3-106 can be used for psychoactivator addiction research .
    OS-3-106
  • HY-147684
    FGFR-IN-7

    		FGFR Neurological Disease
    FGFR-IN-7 (compound 17) is an orally active, potent and BBB-penetrated FGFR (fibroblast growth factor receptor) modulator. FGFR-IN-7 shows neuroprotective activity. FGFR-IN-7 improves brain exposure and reduced risk of phospholidosis. FGFR-IN-7 can be used for neurodegenerative diseases research .
    FGFR-IN-7
  • HY-12678
    Entrectinib
    15+ Cited Publications

    NMS-E628; RXDX-101

    		 ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Cancer
    Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib
  • HY-147748
    COX-2-IN-17

    		COX Inflammation/Immunology
    COX-2-IN-17 (compound 10) is a potent and BBB-penetrated COX-2 (cyclooxygenase-2) inhibitor, with an IC50 of 0.02 μM. COX-2-IN-17 shows anti-inflammatory and analgesic activities. COX-2-IN-17 attenuates hyperalgesia in the neurogenic phase as well as the inflammatory phase .
    COX-2-IN-17
  • HY-147697
    LSD1-IN-21

    		Histone Demethylase TNF Receptor Inflammation/Immunology Cancer
    LSD1-IN-21 (compound 5a) is a potent and BBB-penetrated LSD1 (Lysine specific demethylase-1) inhibitor, with an IC50 of 0.956 µM. LSD1-IN-21 significantly reduces the pro-inflammatory cytokine TNF-α. LSD1-IN-21 shows good anticancer and anti-inflammatory activity .
    LSD1-IN-21
  • HY-146347
    MAO-B-IN-10

    		Monoamine Oxidase Amyloid-β Neurological Disease
    MAO-B-IN-10 (compound 4f) is a potent, selective, BBB-penetrated MAO-B (monoamine oxidase-B) inhibitor, with IC50 of 5.3 μM. MAO-B-IN-10 can inhibit (58.2%) and disaggregate (43.3%) self-mediated Aβ (amyloid β) aggregation. MAO-B-IN-10 can be use for Alzheimer’s disease research .
    MAO-B-IN-10
  • HY-19939S
    VX-984
    4 Publications Verification

    M9831

    		 DNA-PK Cancer
    VX-984 is an orally active, potent, selective and BBB-penetrated DNA-PK inhibitor. VX-984 efficiently inhibits NHEJ (non-homologous end joining) and increases DSBs (DNA double-strand breaks). VX-984 can be used for glioblastomas (GBM) and non-small cell lung cancer (NSCLC) research. VX-984 is a de novo deuterium .
    VX-984
  • HY-146678
    HDAC6-IN-5

    		HDAC Amyloid-β Cholinesterase (ChE) Neurological Disease
    HDAC6-IN-5 (compound 11b) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-5 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-5 can enhance neurite outgrowth without significant neurotoxicity .
    HDAC6-IN-5
  • HY-146679
    HDAC6-IN-6

    		HDAC Amyloid-β Cholinesterase (ChE) Neurological Disease
    HDAC6-IN-6 (compound 6a) is a potent and BBB-penetrated HDAC6 inhibitor, with an IC50 of 0.025 μM. HDAC6-IN-6 exhibits strong inhibitory activity against Aβ1-42 self-aggregation and AChE, with IC50 values of 3.0 and 0.72 μM. HDAC6-IN-6 can enhance neurite outgrowth without significant neurotoxicity .
    HDAC6-IN-6
  • HY-147851
    BACE1-IN-12

    		Beta-secretase Neurological Disease
    BACE1-IN-12 (compound 7g) is a potent and BBB-penetrated BACE1 inhibitor, with an IC50 of 8.9 µM. BACE1-IN-12 shows selective BuChE (butyrylcholinesterase) inhibitory activity with an IC50 of 3.2 µM. BACE1-IN-12 shows effective antioxidant effect with an IC50 of 10.2 μM (DPPH). BACE1-IN-12 might be served as a potential anti-Alzheimer agent .
    BACE1-IN-12
  • HY-17412
    Minocycline hydrochloride
    30+ Cited Publications

    		 Bacterial Antibiotic HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Potassium Channel Calcium Channel Infection Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
    Minocycline hydrochloride
  • HY-144765
    NF-κB-IN-4

    		NF-κB Apoptosis Neurological Disease Inflammation/Immunology
    NF-κB-IN-4 (compound 17) is a potent and BBB-penetrated NF-κB pathway inhibitor with blood brain barrier (BBB) permeability. NF-κB-IN-4 exhibits potential anti-neuroinflammatory activity with low toxicity. NF-κB-IN-4 can block the activation and phosphorylation of IκBα, reduce expression of NLRP3, and thus inhibit NF-κB activation. NF-κB-IN-4 can be used for neuroinflammation related diseases research .
    NF-κB-IN-4
  • HY-17412A
    Minocycline

    		Antibiotic Bacterial HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Potassium Channel Calcium Channel Infection Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Minocycline is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
    Minocycline
  • HY-147859
    BChE-IN-8

    		Amyloid-β Neurological Disease
    BChE-IN-8 (compound 20) is an orally active, potent and BBB-penetrated BChE (butyrylcholinesterase) inhibitor, with IC50 values of 0.15 nM (eqBChE, equine serum BChE) and 45.2 nM (hBChE), respectively. High stability of BChE-IN-8 contributes to significantly improved blood concentration and tissue exposure. BChE-IN-8 can exert neuro-protecting and cognition improving properties through multiple modulations, including cholinergic system, Aβ aggregation, neuropeptide levels. BChE-IN-8 can be used for Alzheimer's disease (AD) research .
    BChE-IN-8
  • HY-12678S
    Entrectinib-d4

    NMS-E628-d4; RXDX-101-d4

    		 ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Isotope-Labeled Compounds Cancer
    Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice .
    Entrectinib-d4
  • HY-17412R
    Minocycline hydrochloride (Standard)

    		Bacterial Antibiotic HIF/HIF Prolyl-Hydroxylase Apoptosis MDM-2/p53 Potassium Channel Calcium Channel Infection Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Minocycline (hydrochloride) (Standard) is the analytical standard of Minocycline (hydrochloride). This product is intended for research and analytical applications. Minocycline hydrochloride is an orally active, potent and BBB-penetrated semi-synthetic tetracycline antibiotic. Minocycline hydrochloride is a hypoxia-inducible factor (HIF)-1α inhibitor. Minocycline hydrochloride shows anti-cancer, anti-inflammatory, and glutamate antagonist effects. Minocycline hydrochloride reduces glutamate neurotransmission and shows neuroprotective properties and antidepressant effects. Minocycline hydrochloride inhibits bacterial protein synthesis through binding with the 30S subunit of the bacterial ribosome, resulting in a bacteriostatic effect .
    Minocycline hydrochloride (Standard)
  • HY-157333
    CYP51-IN-15

    		Parasite Cytochrome P450 Infection Inflammation/Immunology
    CYP51-IN-15 (9B) is a BBB penetrated Naegleria fowleri-specific CYP51 inhibitor, with an EC50 of 1.5 μM .
    CYP51-IN-15
  • HY-155024
    HAT-IN-8

    		Parasite Infection
    HAT-IN-8 (Compound 38) is a BBB-penetrable T. brucei inhibitor (EC50: 0.18 μM). HAT-IN-8 can be used for the research of Human African trypanosomiasis .
    HAT-IN-8
  • HY-119953
    BIBN-99

    		mAChR Neurological Disease
    BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
    BIBN-99
  • HY-153432
    TRV-7019

    		Cholinesterase (ChE) Neurological Disease
    TRV-7019 is a BBB-penetrable radioligand for brain imaging that target butyrylcholinesterase. TRV-7019 can be used for the diagnosis of an amyloid disease, multiple sclerosis, a brain tumor, or butyrylcholinesterase activity .
    TRV-7019
  • HY-146314
    MAO-B-IN-9

    		Monoamine Oxidase Amyloid-β Neurological Disease
    MAO-B-IN-9 (compound 16) is a potent, selective, BBB-penetrated, irreversible and time-dependent MAO-B (monoamine oxidase B) inhibitor, with an IC50 of 0.18 μM. MAO-B-IN-9 prevents Aβ1-42-induced neuronal cell death. MAO-B-IN-9 shows neuroprotective effects, which may be the result of its Aβ1-42 anti-aggregation effects . MAO-B-IN-9 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    MAO-B-IN-9
  • HY-124832
    δ-Secretase inhibitor 11

    		Caspase Amyloid-β Neurological Disease
    δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research .
    δ-Secretase inhibitor 11
  • HY-P2343
    BH3 hydrochloride

    		Apoptosis Cancer
    BH3 hydrochloride, a BBB penetrated peptide, provoke apoptosis either by direct activation of pro-apoptotic Bax/Bak or by neutralizing anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1 and A-1) via their BH3 domian .
    BH3 hydrochloride
  • HY-P3223
    Biphalin TFA

    		Opioid Receptor Neurological Disease
    Biphalin TFA, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores. Biphalin TFA has high affinity for opioid receptors. Biphalin TFA shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin TFA is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
    Biphalin TFA
  • HY-157400
    hMAO-B-IN-7

    		Monoamine Oxidase Neurological Disease
    hMAO-B-IN-7 (compound 11n) is a potent and blood–brain barrier (BBB) penetrable inhibitor of human monoamine oxidase-B (hMAO-B), with the IC50 value of 0.79±0.05 μM. hMAO-B-IN-7 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
    hMAO-B-IN-7
  • HY-D2268
    QM-FN-SO3

    		Fluorescent Dye Amyloid-β Neurological Disease
    QM-FN-SO3 is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 can be used for in vivo detection of Aβ plaques. QM-FN-SO3 has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
    QM-FN-SO3
  • HY-D2268A
    QM-FN-SO3 ammonium

    		Amyloid-β Fluorescent Dye Neurological Disease
    QM-FN-SO3 ammonium is a BBB-penetrable near-infrared (NIR) aggregation-induced emission (AIE)-active probe for Aβ plaques. QM-FN-SO3 ammonium can be used for in vivo detection of Aβ plaques. QM-FN-SO3 ammonium has ultra-high S/N ratio, binding affinity, and high-performance NIR emission .
    QM-FN-SO3 ammonium
  • HY-153434
    RIP1 kinase inhibitor 4

    		RIP kinase Cancer
    RIP1 kinase inhibitor 4 (Example 3) is a BBB-penetrable RIP1 kinase inhibitor (EC50: <100 nM). RIP1 kinase inhibitor 4 can be used for the research of cell programming necrosis-related diseases . RIP1 kinase inhibitor 4 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    RIP1 kinase inhibitor 4
  • HY-152671
    hMAO-B-IN-4

    		Monoamine Oxidase Neurological Disease
    hMAO-B-IN-4 (compound B10) is a selective, reversible and blood–brain barrier (BBB) penetrable human monoamine oxidase-B (hMAO-B) inhibitor with an IC50 value and a Ki value of 0.067 and 0.03 μM, respectively. hMAO-B-IN-4 inhibits hMAO-A with an IC50 value of 33.82 μM. hMAO-B-IN-4 can be used for Alzheimer’s disease (AD) and Parkinson’s disease (PD) research .
    hMAO-B-IN-4
  • HY-146691
    hMAO-B-IN-2

    		Monoamine Oxidase Neurological Disease
    hMAO-B-IN-2 (compound 6j) is an orally active, potent, selective and BBB penetrated and competitive reversible hMAO-B inhibitor, with an IC50 of 4 nM. hMAO-B-IN-2 shows low toxicity and good neuroprotective effects in SH-SY5Y cell. hMAO-B-IN-2 can be used for alzheimer’s disease research . hMAO-B-IN-2 is a click chemistry reagent, itcontains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    hMAO-B-IN-2

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