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BBB penetrate

" in MedChemExpress (MCE) Product Catalog:

89

Inhibitors & Agonists

2

Fluorescent Dye

6

Peptides

1

Inhibitory Antibodies

3

Isotope-Labeled Compounds

2

Click Chemistry

2

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P10235
    Cyclic AC253

    		Amylin Receptor Neurological Disease
    Cyclic AC253 is an antagonist for amylin receptor, with IC50 of 0.3 μM. Cyclic AC253 exhibits neuroprotective efficacy against Aβ toxicity and abrogates Aβ-induced impairment of hippocampal long-term potentiation. Cyclic AC253 penetrate blood-brain barrier (BBB) .
    Cyclic AC253
  • HY-134228
    4-Hydroperoxyifosfamide

    		Biochemical Assay Reagents Cancer
    4-Hydroperoxyifosfamide is an anticancer agent that can penetrate the blood-brain barrier (BBB) .
    4-Hydroperoxyifosfamide
  • HY-119624
    MOMIPP

    		PIKfyve Cancer
    MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB) .
    MOMIPP
  • 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-164401
    QBS10072S

    		Others Cancer
    QBS10072S is a bifunctional chemotherapeutic agent, through combination of a cytotoxin and a selective LAT1 transporter substrate. QBS10072S exhibits cytotoxicity in MDA-MB-231 cell and antitumor efficacy in mice. QBS10072S is blood-brain barrier (BBB) penetrable .
    QBS10072S
  • HY-162757
    Anticonvulsant agent 5

    		GABA Receptor Sodium Channel Neurological Disease
    Anticonvulsant agent 5 (Compound 5c) exhibits high affinity for GABAA receptors and NaV1.3 receptors. Anticonvulsant agent 5 shows anticonvulsant efficacy in mice psychomotor epilepsy test with an ED50 of 107 mg/kg. Anticonvulsant agent 5 exhibits neuroprotective activity against Kainic acid (HY-N2309) with an IC50 of 113 μM. Anticonvulsant agent 5 is blood-brain barrier (BBB) penetrable .
    Anticonvulsant agent 5
  • HY-122462
    Ladirubicin

    PNU-159548

    		 DNA/RNA Synthesis Cancer
    Ladirubicin (PNU-159548) is a derivative of Daunorubicin (HY-13062A). Ladirubicin exhibits DNA intercalation and DNA alkylating properties, inhibits DNA replication and transcription, causes DNA damage, and thereby exhibits antitumor efficacy. Ladirubicin exhibits the potential to penetrate the blood-brain barrier (BBB) for its high lipophilicity. Ladirubicin exhibits toxicity through suppression of bone marrow activity .
    Ladirubicin
  • HY-164284
    LK-2

    		Others Neurological Disease
    LK-2 is an antagonist for ASIC1a with a Kd of 1.9 μM. LK-2 reduces glutamate-induced ASIC1a current-enhancement with an IC50 of 6.6 μM. LK-2 exhibits neuroprotective efficacy in mouse ischemic stroke model, with improved motor and coordination skills. LK-2 is blood-brain barrier (BBB) penetrable .
    LK-2
  • HY-163909
    AChE-IN-72

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-72 (Compound 13a) is an inhibitor for acetylcholinesterase (AChE) with an IC50 of 0.59 μM. AChE-IN-72 inhibits BChE with an IC50 of 5.02 μM. AChE-IN-72 exhibits radical scavenging with IC50 of 5.88 μM. AChE-IN-72 exhibits iron-chelating property, inhibits Aβ1−42 aggregation, and inhibits NLRP3 inflammasome activation. AChE-IN-72 ameliorates memory impairment in Betaine (HY-B0710)-induced AD mouse model. AChE-IN-72 is blood-brain barrier (BBB) penetrable .
    AChE-IN-72
  • HY-162565
    CDD-2807

    		STK33 CDK RET Endocrinology
    CDD-2807 is an inhibitor for serine/threonine kinase 33 (STK33) with IC50 of 9.2 nM. CDD-2807 exhibits no significant toxicity in mice and can cross the blood-testis barrier without accumulating in the brain. CDD-2807 induces a reversible contraceptive effect and has potential for the development of the male contraceptive .
    CDD-2807
  • 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-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-121191
    Bisnorcymserine

    N1,N8-Bisnorcymserine; (-)-Bisnorcymserine

    		 Cholinesterase (ChE) Neurological Disease
    Bisnorcymserine ((-)-Bisnorcymserine) is an inhibitor for butyrylcholinesterase (BChE) with an IC50 of 0.228 nM. Bisnorcymserine reduces the levels of amyloid-β peptide (Aβ), exhibits ameliorates the Alzheimer’s Disease in elderly rat models. Bisnorcymserine is blood-brain barrier penetrate .
    Bisnorcymserine
  • 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-158820
    Cosdosiran

    QPI-1007

    		 Small Interfering RNA (siRNA) Caspase Cardiovascular Disease
    Cosdosiran is a chemically modified siRNA designed to temporarily inhibit expression of the caspase 2 protein and can be used for the study of nonarteritic anterior ischemic optic neuropathy and other optic neuropathies such as glaucoma that result in the death of retinal ganglion cells.?
    Cosdosiran
  • HY-158820A
    Cosdosiran sodium

    QPI-1007 sodium

    		 Small Interfering RNA (siRNA) Caspase Cardiovascular Disease
    Cosdosiran sodium is a chemically modified siRNA designed to temporarily inhibit expression of the caspase 2 protein and can be used for the study of nonarteritic anterior ischemic optic neuropathy and other optic neuropathies such as glaucoma that result in the death of retinal ganglion cells.?
    Cosdosiran sodium
  • HY-E70364
    IgdE protease

    		Biochemical Assay Reagents Inflammation/Immunology
    IgdE protease is a cysteine protease, which is initially isolated from Streptococcus agalactiae. IgdE protease digests monoclonal antibodies (mAbs) of the IgG1 type specifically at their upper hinge region, produces Fc/2, hinge peptide dimers, and Fab fragment. IgdE protease can be used in disulfide bonds and free thiol analysis, as it requires no reducing agents for cleavage .
    IgdE protease
  • 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-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-125602
    MNI-444

    		Adenosine Receptor Neurological Disease
    MNI-444 is a BBB-penetrable ligand of adenosine 2A receptor (A2AR). A2AR is a potential non-dopaminergic target for the research of Parkinson’s disease .
    MNI-444
  • HY-13909
    RGFP966
    30+ Cited Publications

    		 HDAC Cancer
    RGFP966 is a highly selective HDAC3 inhibitor with an IC50 of 80 nM and shows no inhibition to other HDACs at concentrations up to 15 μM. RGFP966 can penetrate the blood brain barrier (BBB).
    RGFP966
  • 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-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-101059
    FGIN 1-27

    		Others Neurological Disease
    FGIN 1-27, an indoleacetamide, is a specific peripheral benzodiazepine receptor (PBR) ligand with a Ki of 5.0 nM. FGIN 1-27 can penetrate the blood brain barrier (BBB). FGIN 1-27 inhibits the onset of Isoniazid-induced convulsions .
    FGIN 1-27
  • 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-143877
    NN-390

    		HDAC Cancer
    NN-390 is a potent and selective HDAC6 inhibitor, with an IC50 of 9.8 nM. NN-390 penetrates the blood-brain barrier (BBB). NN-390 shows study potential in metastatic Group 3 MB (medulloblastoma) .
    NN-390
  • 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-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-147821
    CB1-IN-2

    		Cannabinoid Receptor Metabolic Disease
    CB1-IN-2 (Compound 4g) is a selective CB1 inhibitor with an IC50 of 0.644 μM. CB1-IN-2 can penetrates BBB and might cause CNS side effect similar with Rimonabant .
    CB1-IN-2
  • HY-110180
    VU0409106

    		mGluR Neurological Disease
    VU0409106 is a potent and selective mGlu5 negative allosteric modulator (NAM) with an IC50 of 24 nM. VU0409106 shows anxiolytic effects in rat models in a concentration-dependent manner. VU0409106 also penetrates the blood-brain barrier (BBB) .
    VU0409106
  • HY-151152
    AChE-IN-24

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-24 is a potent AChE inhibitor and can penetrate the BBB. AChE-IN-24 has the mighty inhibitory activity to hAChE with an IC50 value of 0.053 μM. AChE-IN-24 can be used for the research of Alzheimer s disease (AD) .
    AChE-IN-24
  • HY-10358
    MK-2206 dihydrochloride
    Maximum Cited Publications
    315 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-111136
    BL-1020 mesylate

    		GABA Receptor 5-HT Receptor Dopamine Receptor Histamine Receptor Neurological Disease
    BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
    BL-1020 mesylate
  • 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-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-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-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-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-132310
    MAGL-IN-4

    		MAGL Neurological Disease
    MAGL-IN-4 is an orally active, selective and reversible monoacylglycerol lipase (MAGL) inhibitor with an IC50 of 6.2 nM. MAGL-IN-4 can penetrate the blood-brain barrier (BBB). MAGL-IN-4 enhances endocannabinoid signaling mostly by the increase in the level of 2-AG via selective MAGL inhibition in the brain .
    MAGL-IN-4
  • 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-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

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