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BBB

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284

Inhibitors & Agonists

1

Screening Libraries

8

Fluorescent Dye

3

Biochemical Assay Reagents

25

Peptides

5

Inhibitory Antibodies

10

Natural
Products

16

Isotope-Labeled Compounds

5

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-151657
    Spermine(N3BBB)

    		ADC Linker Others
    Spermine(N3BBB) is a click chemistry reagent containing an azide group and can be used for various biochemical studies .
    Spermine(N3<em>BBB</em>)
  • HY-119624
    MOMIPP

    		PIKfyve Cancer
    MOMIPP, a macropinocytosis inducer, is a PIKfyve inhibitor. MOMIPP penetrates the blood-brain barrier (BBB) .
    MOMIPP
  • HY-146141
    EphA2 agonist 2

    		Ephrin Receptor Cancer
    EphA2 agonist 2 (Lead compound) is a selective EphA2 agonist with antitumor activities. EphA2 agonist 2 can cross the BBB .
    EphA2 agonist 2
  • HY-147982
    GABA-AT-IN-1

    		GABA Receptor Neurological Disease
    GABA-AT-IN-1 (Compound 6) is a γ-aminobutyric acid aminotransferase (GABA-AT) inhibitor and significantly elevates the mouse brain GABA level. GABA-AT-IN-1 has the ability to cross the BBB and can be used as an anticonvulsant .
    GABA-AT-IN-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-137501
    306-O12B-3

    		Others Others
    306-O12B-3 is a lipidoid that can efficiently deliver ASO both in vitro and in vivo. 306-O12B-3 is used to transport small molecule drugs across the blood-brain barrier (BBB) .
    306-O12B-3
  • HY-162277
    BuChE-IN-10

    		Cholinesterase (ChE) Neurological Disease
    BuChE-IN-10 (compound 7p) is an inhibitor of BuChE (eqBuChE IC50 = 4.68 nM, huBuChE IC50 = 9.12 nM). BuChE-IN-10 has anti-neuroinflammatory activity and exhibits high BBB permeability .
    BuChE-IN-10
  • HY-18406
    HSP70-IN-4

    		HSP Cancer
    HSP70-IN-4 (Compound YM-01) is an Hsp70 inhibitor with an IC50 of 3.2 μM. HSP70-IN-4 is not BBB permeable .
    HSP70-IN-4
  • HY-155271
    hCAXII-IN-7

    		Carbonic Anhydrase Others
    hCAXII-IN-7 (compound 6e) is a hCA XII inhibitor. hCAXII-IN-7 has BBB permeability. hCAXII-IN-7 induces 786-0, SF-539 and HS 578 T cells apoptotic .
    hCAXII-IN-7
  • 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-126429
    Nav1.1 activator 1

    		Sodium Channel Neurological Disease
    Nav1.1 activator 1 (compound 4), a highly potent Nav1.1 activator with BBB penetration, increases decay time constant τ of Nav1.1 currents at 0.03 μM along with significant selectivity against Nav1.2, Nav1.5, and Nav1.6 .
    Nav1.1 activator 1
  • HY-146668
    AChE/BChE-IN-8

    		Cholinesterase (ChE) Neurological Disease
    AChE/BChE-IN-8 (Compound 5a) is an uncompetitive AChE and mixed BChE inhibitor with Ki values of 0.788 μM and 2.364 μM against Electrophorus electricus AChE (EeAChE) and equine BChE (eqBChE), respectively. AChE/BChE-IN-8 can cross the BBB and has low cytotoxicity .
    AChE/BChE-IN-8
  • HY-150545
    AChE-IN-21

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-21 (Compound I-8) is a potent, selective and orally active AChE inhibitor with an IC50 of 2.66 nM. AChE-IN-21 displays excellent BBB permeability in vitro .
    AChE-IN-21
  • HY-149820
    MAO-B-IN-22

    		Monoamine Oxidase Neurological Disease
    MAO-B-IN-22 (compound 6h) is a potent MAO-B inhibitor with an IC50 of 0.014 μM. MAO-B-IN-22 has high antioxidant activity, good metal chelating ability, proper BBB permeability and significant neuroprotective effect .
    MAO-B-IN-22
  • HY-136731
    APE1-IN-1

    		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-147870
    COX-2-IN-22

    		COX Cholinesterase (ChE) Beta-secretase Neurological Disease Inflammation/Immunology
    COX-2-IN-22 (Compound 4h) is a COX-2 inhibitor with an IC50 of 8.6 µM. COX-2-IN-22 also inhibits AChE, BChE, β-Secretase, LOX-5 and DPPH with IC50 values of 2.8, 6.3, 15.3, 13.9 and 6.8 µM, respectively. COX-2-IN-22 can cross BBB .
    COX-2-IN-22
  • HY-105155
    Lobradimil

    RMP 7

    		 Bradykinin Receptor Cancer
    Lobradimil (RMP 7), a synthetic bradykinin analog, is a potent and selective bradykinin B2 receptor agonist (Ki: 0.54 nM). Lobradimil increases the permeability of the BBB. Lobradimil can be used in the research of brain tumors .
    Lobradimil
  • HY-A0168
    Regadenoson
    1 Publications Verification

    CVT-3146

    		 Adenosine Receptor Cardiovascular Disease
    Regadenoson (CVT-3146) is a selective A2A adenosine receptor agonist and vasodilator that increases coronary blood flow, can be used in study of myocardial perfusion imaging. Regadenoson also increases the permeability of the blood-brain barrier (BBB) in rodents, can be used to study increased delivery of agents to the human CNS .
    Regadenoson
  • HY-134494
    MS48107

    		GPR68 Neurological Disease
    MS48107 is a potent and selective positive allosteric modulator of G protein-coupled receptor 68 (GPR68). MS48107 is selective for GPR68 over the closely related proton GPCRs, neurotransmitter transporters, and hERG ion channels. MS48107 can readily cross the blood-brain barrier (BBB) in mice .
    MS48107
  • 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-146142
    AChE/BuChE-IN-2

    		Cholinesterase (ChE) Amyloid-β Neurological Disease
    AChE/BuChE-IN-2 (Compound 5f) is an orally active AChE and BuChE inhibitor with IC50 values of 0.72 μM and 0.16 μM, respectively. AChE/BuChE-IN-2 shows a non-competitive inhibition with AChE and shows potent self-induced β-amyloid (Aβ) aggregation inhibition with an IC50 of 62.52 μM. AChE/BuChE-IN-2 can cross the BBB .
    AChE/BuChE-IN-2
  • HY-109502S
    10-OH-NBP-d4

    		Isotope-Labeled Compounds Neurological Disease
    10-OH-NBP-d4 is deuterium labeled 10-OH-NBP. 10-OH-NBP is a Butylphthalide (3-n-Butylphthalide; NBP; HY-B0647) hydroxylated metabolite and can penetrates the blood-brain barrier (BBB). Butylphthalide exerts neuroprotective effects and has potential for cerebral ischemia research[1].
    10-OH-NBP-d4
  • HY-146664
    AChE/BChE-IN-4

    		Cholinesterase (ChE) Neurological Disease
    AChE/BChE-IN-4 (BMC-3) is a dual AChE and BChE inhibitor with IC50 values of 792 nM and 2.2 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-4 can cross the BBB .
    AChE/BChE-IN-4
  • HY-146665
    AChE/BChE-IN-5

    		Cholinesterase (ChE) Neurological Disease
    AChE/BChE-IN-5 (BMC-16) is a dual AChE and BChE inhibitor with IC50 values of 266 nM and 10.6 nM against human AChE (hAChE) and human BChE (hBChE), respectively. AChE/BChE-IN-5 can cross the BBB .
    AChE/BChE-IN-5
  • HY-128868G
    FITC-Dextran (MW 150000)

    		Fluorescent Dye Others
    FITC-Dextran (MW 150000) is a fluorescent probe for fluorescein isothiocyanate (FITC) dextran (Ex=491 nm; Em=518 nm). FITC-Dextran (MW 150000) can be used as a marker to reveal heat shock-induced cell damage and to study the early and late stages of apoptosis. FITC-Dextran (MW 150000) can be used in perfusion studies in animals or in fluorescence microlymphography, to study processes that affect the permeability of the blood brain barrier (BBB) . FITC-Dextran (MW 150000) can be used as fluorescent probe to study cell permeability .
    FITC-Dextran (MW 150000)
  • HY-13779A
    J147

    		Monoamine Oxidase Dopamine Transporter Neurological Disease
    J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. J147 can pass the blood brain barrier (BBB). J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter. J147 plays an impotant role in Alzheimer’s disease (AD) .
    J147
  • HY-B1334A
    Perhexiline maleate

    		Mitochondrial Metabolism Apoptosis Cardiovascular Disease Cancer
    Perhexiline maleate is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline maleate induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline maleate can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline maleate can be used in the research of cancers, and cardiovascular disease like angina .
    Perhexiline maleate
  • HY-B1334
    Perhexiline

    		Mitochondrial Metabolism Apoptosis Cardiovascular Disease Cancer
    Perhexiline is an orally active CPT1 and CPT2 inhibitor that reduces fatty acid metabolism. Perhexiline induces mitochondrial dysfunction and apoptosis in hepatic cells. Perhexiline can cross the blood brain barrier (BBB) and shows anti-tumor activity. Perhexiline can be used in the research of cancers, and cardiovascular disease like angina .
    Perhexiline
  • HY-149941
    hNTS1R agonist-1

    		Neurotensin Receptor Neurological Disease
    hNTS1R agonist-1 (Compound 10) is a BBB permeable hNTS1R full agonist (Ki: 6.9 nM) . hNTS1R agonist-1 increases motor function and memory in a mouse model of Parkinson's disease (PD). hNTS1R agonist-1 is a Neurotensin(8-13) analog and is a neuroprotective agent .
    hNTS1R agonist-1
  • HY-108625
    SHA 68
    1 Publications Verification

    		 Neuropeptide Y Receptor Neurological Disease
    SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia .
    SHA 68
  • HY-147939
    AChE/BuChE-IN-3

    		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 .
    AChE/BuChE-IN-3
  • HY-144660
    AChE-IN-7

    		Cholinesterase (ChE) Neurological Disease
    AChE-IN-7 (Compound 16) is a selective and potent inhibitor of acetylcholinesterase (eeAChE IC50 = 0.045 μM; eeBuChE IC50 = 19.68 μM). AChE-IN-7 is safe in vivo and in vitro, and shows good overall pharmacokinetic performance and high bioavailability (F = 55.5%). AChE-IN-7 also has high BBB permeability .
    AChE-IN-7
  • HY-151962
    JNK3 inhibitor-5

    		JNK Apoptosis GSK-3 p38 MAPK Neurological Disease
    JNK3 inhibitor-5 (Compound 22b) is a potent and selective JNK3 inhibitor with an IC50 of 0.379 nM. JNK3 inhibitor-5 effectively protects the neuronal cells against amyloid beta-induced apoptosis. JNK3 inhibitor-5 has a high cell permeability and is predicted as BBB permeable .
    JNK3 inhibitor-5
  • HY-10096
    TCS2002

    		GSK-3 Neurological Disease
    TCS2002 (Compound 9b) is a highly selective, orally bioavailable and potent GSK-3β inhibitor with the IC50 of 35 nM. TCS2002 shows good pharmacokinetic profiles including favorable BBB penetration. TCS2002 can be used for the research of Alzheimer’s disease .
    TCS2002
  • HY-143244
    Monoamine Oxidase B inhibitor 1

    		Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 1 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 0.02 nM. Monoamine Oxidase B inhibitor 1 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 1 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
    Monoamine Oxidase B inhibitor 1
  • HY-143245
    Monoamine Oxidase B inhibitor 2

    		Monoamine Oxidase Neurological Disease
    Monoamine Oxidase B inhibitor 2 is a potent, reversible, orally active and selective monoamine oxidase B (MAO-B) inhibitor with an IC50 of 1.33 nM. Monoamine Oxidase B inhibitor 2 has antioxidant and anti-neuroinflammatory activities. Monoamine Oxidase B inhibitor 2 can across the blood-brain barrier (BBB), and can be used for Parkinson’s disease study .
    Monoamine Oxidase B inhibitor 2
  • HY-150639
    Everafenib

    		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-146399
    AChE/BChE-IN-9

    		Cholinesterase (ChE) ROS Kinase Neurological Disease
    AChE/BChE-IN-9 (Compound 7a) is a potent, orally active AChE and BChE inhibitor with IC50 values of 5.74 μM and 14.05 μM against hAChE and eqBChE, respectively. AChE/BChE-IN-9 is also an efficacious antioxidant with an IC50 of 57.35 μM. AChE/BChE-IN-9 is able to chelate iron and modulates aggregation of amyloid β1-42. AChE-IN-16 can cross the BBB .
    AChE/BChE-IN-9
  • HY-151261
    HDAC6-IN-13

    		HDAC Inflammation/Immunology
    HDAC6-IN-13 (Compound 35m) is a potent, highly selective, orally active HDAC6 inhibitor with an IC50 of 0.019 μM. HDAC6-IN-13 also inhibits HDAC1, HDAC2 and HDAC3 with IC50s of 1.53, 2.06 and 1.03 μM, respectively. HDAC6-IN-13 shows significant BBB permeability and anti-inflammatory activity .
    HDAC6-IN-13
  • HY-158148
    CSF1R-IN-23

    		c-Fms Neurological Disease Inflammation/Immunology
    CSF1R-IN-23 (Compound 7dri) is a selective inhibitor for colony-stimulating factor-1 receptor (CSF1R), with IC50 of 36.1 nM. CSF1R-IN-23 serves as antineuroinflammatory agent in mouse model. CSF1R-IN-23 is blood brain barrier (BBB) permeable .
    CSF1R-IN-23
  • 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-144388
    ChE/Aβ1-42-IN-1

    		Cholinesterase (ChE) Amyloid-β Neurological Disease
    ChE/Aβ1-42-IN-1 (compound 28) is a potent ChE and Aβ1-42 aggregation inhibitor with IC50s of 0.062, 0.767 and 1.227 µM for AChE, BuChE and Aβ1-42 aggregation, respectively. ChE/β1-42-IN-1 shows excellent BBB penetration. ChE/Aβ1-42-IN-1 is a potent multi-targeted anti-Alzheimer's agent .
    ChE/Aβ1-42-IN-1
  • HY-144389
    hAChE/Aβ1-42-IN-1

    		Cholinesterase (ChE) Amyloid-β Neurological Disease
    hAChE/Aβ1-42-IN-1 (Compound 16) is a potent inhibitor of hAChE and Aβ1-42 aggregation. hAChE/Aβ1-42-IN-1 shows acceptable relative safety upon hepG2 cell line and excellent BBB penetration with wide safety margin. hAChE/Aβ1-42-IN-1 has the potential for the research of Alzheimer disease (AD) .
    hAChE/Aβ1-42-IN-1
  • HY-33009
    AS057278

    		Others Neurological Disease
    AS057278 is a potent, selective, orally active and blood-brain barrier (BBB) penetrant non-peptidic D-amino acid oxidase (DAAO) inhibitor with an IC50 value of 0.91 μM and EC50 of 2.2-3.95 μM. AS057278 can normalize phencyclidine (PCP)-induced prepulse inhibition in mice. AS057278 can be used for researching schizophrenia .
    AS057278
  • 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-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-115681
    (2R/S)-6-PNG
    1 Publications Verification

    6-Prenylnaringenin; (±)-6-Prenylnaringenin

    		 Calcium Channel Neurological Disease
    (2R/S)-6-PNG (6-Prenylnaringenin) is a potent and reversible Cav3.2 T-type Ca 2+ channels (T-channels) blocker. (2R/S)-6-PNG can penetrate the blood-brain barrier (BBB). (2R/S)-6-PNG suppresses neuropathic and visceral pain in mice .
    (2R/S)-6-PNG
  • HY-147395
    GPR52 agonist-1

    		GPR52 Neurological Disease
    GPR52 agonist-1 is a potent, orally active and blood-brain barrier (BBB) penetrant GPR52 agonist with an pEC50 value of 7.53. GPR52 agonist-1 affects cAMP accumulation through direct interaction with GPR52. GPR52 agonist-1 can significantly suppress Methamphetamine-induced hyperactivity in mice. Antipsychotic activity .
    GPR52 agonist-1
  • HY-14327
    FAUC 213

    		Dopamine Receptor Neurological Disease
    FAUC 213 is an orally active and highly selective dopamine D4 receptor complete antagonist with a Ki of 2.2 nM for hD4.4. FAUC 213 has less activity on D2 and D3 receptors (Kis of 3.4 μM, 5.3 μM for hD2, hD3, respectively). FAUC 213 can cross the blood-brain barrier (BBB). FAUC 213 exhibits atypical antipsychotic characteristic .
    FAUC 213
  • HY-13779
    (E/Z)-J147

    		Monoamine Oxidase Dopamine Transporter Neurological Disease
    (E/Z)-J147 is an exceptionally potent, orally active, neuroprotective agent for cognitive enhancement. (E/Z)-J147 can readily pass the blood brain barrier (BBB). (E/Z)-J147 can inhibit monoamine oxidase B (MAO B) and the dopamine transporter with EC50 values of 1.88 μM and 0.649 μM, respectively. (E/Z)-J147 has potential for the treatment of Alzheimer’s disease (AD) .
    (E/Z)-J147

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