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α subunits

" in MedChemExpress (MCE) Product Catalog:

201

Inhibitors & Agonists

2

Screening Libraries

5

Fluorescent Dyes

1

Biochemical Assay Reagents

12

Peptides

21

Inhibitory Antibodies

19

Natural
Products

2

Recombinant Proteins

27

Isotope-Labeled Compounds

20

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N0877
    Bufalin
    Maximum Cited Publications
    9 Publications Verification

    Na+/K+ ATPase Cancer
    Bufalin is an active component isolated from Chan Su, acts as a potent Na +/K +-ATPase inhibitor, binds to the subunit α1, α2 and α3, with Kd of 42.5, 45 and 40 nM, respectively . Anti-cancer activity .
    Bufalin
  • HY-12650
    Mirogabalin
    5 Publications Verification

    DS5565

    Calcium Channel Neurological Disease
    Mirogabalin (DS-5565) is a novel, preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS.
    Mirogabalin
  • HY-108006
    Mirogabalin besylate
    5 Publications Verification

    DS 5565 besylate

    Calcium Channel Neurological Disease
    Mirogabalin besylate is a selective and orally available ligand for the α2δ subunit of voltage-gated calcium channels, with Kds of 13.5 nM, 22.7 nM, 27 nM, and 47.6 nM for human α2δ-1, human α2δ-2, rat α2δ-1, and rat α2δ-2, respectively.
    Mirogabalin besylate
  • HY-W013706

    ITP trisodium salt; Inosine triphosphate trisodium salt

    Endogenous Metabolite Metabolic Disease
    Inosine-5'-triphosphate trisodium salt is a nucleotide analogue that acts on multiple G proteins and is widely used in G protein-related research. It can bind to the α -subunit of G proteins and participate in G protein-mediated signal transduction as a substitute for GTP. Its mechanism of action is to interact with the nucleotide-binding site of the G protein α -subunit, affecting the activity and function of G proteins. In the research field, it is mainly used to explore the role of the G protein signaling pathway in cellular physiological and pathological processes. For example, in HL-60 leukemia cells, its impact on G protein-mediated signal transduction can be studied .
    Inosine-5'-triphosphate trisodium salt
  • HY-19931
    COH29
    5 Publications Verification

    RNR Inhibitor COH29

    DNA/RNA Synthesis Cancer
    COH29 (RNR Inhibitor COH29) is a potent ribonucleotide reductase (RNR) inhibitor with anticancer activity. COH29 inhibits α and β subunit of RNR with IC50s of 16 μM.
    COH29
  • HY-142240

    HSK16149

    Calcium Channel Neurological Disease
    Crisugabalin is an orally active, selective ligand for the α2δ subunit of voltage-gated calcium channels, with a target IC50 of 3.96 nM in rats. Crisugabalin inhibits the binding of [ 3H]gabapentin to the αsubunit, reduces calcium influx, decreases neuronal excitability, and impairs nociceptive transmission. Crisugabalin alleviates mechanical allodynia, neuropathic pain and inflammatory pain in rats, and reduces phase II pain behaviors. Crisugabalin can be used in research related to chronic pain, neuropathic pain, diabetic neuropathy, fibromyalgia, inflammatory pain, diabetic peripheral neuropathy and postherpetic neuralgia.
    Crisugabalin
  • HY-P5766

    nAChR
    AChRα(97-116) is a synthetic peptide corresponding to the 97-116 region of the rat acetylcholine receptor α-subunit, and also an inducer of autoimmune diseases. AChRα(97-116) can be used in studies related to experimental autoimmune myasthenia gravis .
    AChRα(97-116)
  • HY-10233
    Gaboxadol hydrochloride
    1 Publications Verification

    Lu 02-030 hydrochloride; THIP hydrochloride

    GABA Receptor Neurological Disease
    Gaboxadol hydrochloride (Lu 02-030 hydrochloride) is a potent agonist of the GABAA receptor and an antagonist of GABAC receptors (IC50=25 μM). Gaboxadol hydrochloride displays a partial agonist efficacy on subunit α1β2γ2 with an ED50 value of 143 μM, a full agonist efficacy at α5 subunit (ED50=28-129 μM) and a superagonist efficacy at α4β3δ (ED50=6 μM). Gaboxadol hydrochloride is a non-opioid agent .
    Gaboxadol hydrochloride
  • HY-111022
    Icerguastat
    3 Publications Verification

    Sephin1; IFB-088

    Phosphatase Infection Inflammation/Immunology
    Icerguastat (Sephin1), a derivative of Guanabenz lacking the α2-adrenergic activity, is a selective inhibitor of the phosphatase regulatory subunit PPP1R15A (R15A). Icerguastat inhibits eIF2α dephosphorylation, thereby prolonging the protective response. Anti-prion effect .
    Icerguastat
  • HY-16716
    Basmisanil
    1 Publications Verification

    RG1662; RO5186582

    GABA Receptor Neurological Disease
    Basmisanil (RG1662) is a highly selective orally active α subunit-containing GABAA receptors (GABAAα5) negative allosteric modulator (NAMs). Basmisanil can inhibit GABAA-α5 with a Ki value of 5 nM and IC50 value of 8 nM, respectively. Basmisanil can be used for the research of multiple cognitive and psychiatric disorders .
    Basmisanil
  • HY-W013150

    GABA Receptor Neurological Disease
    Alpidem, an anxiolytic agent, is an orally active and brain-penetrant GABAA receptor ligand, binds to α1β2γ2 subunit-containing GABAA receptors (IC50 of 17 nM) over α5β2γ2 subunit-containing GABAA receptors (IC50 of >10 μM). Alpidem modulates calcium-induced mitochondrial permeability transition, induces glutathione depletion and hepatocyte necrosis, potentiates TNF-α toxicity, inhibits marble-burying and locomotor activity, enhances stressed rodent feeding behavior, and exerts anticonvulsant effects. Alpidem can be used for the research of anxiety, anxiety disorders, and convulsions .
    Alpidem
  • HY-W002112

    Nornicotine

    Endogenous Metabolite Drug Metabolite nAChR β-catenin Cardiovascular Disease Neurological Disease
    (±)-Nornicotine is a major metabolite of Nicotine. (±)-Nornicotine is a partial nAChRs agonist, specifically activating receptor subtypes containing α7 and α6 subunits. (±)-Nornicotine disrupts β-catenin and ZO-1, and induces F-actin depolymerization. (±)-Nornicotine supports self-administration behavior. (±)-Nornicotine can be used in the research of atherosclerosis, Alzheimer's disease, and schizophrenia .
    (±)-Nornicotine
  • HY-P5985
    mSIRK
    2 Publications Verification

    ERK Others
    mSIRK (G-Protein βγ Binding Peptide) is an cell-permeable activator of ERK1/2, with EC50 of 2.5-5 μM. mSIRK disrupts the interaction between α and βγ subunits and promotes α subunit dissociation without stimulating nucleotide exchange .
    mSIRK
  • HY-14426
    L-655708
    4 Publications Verification

    GABA Receptor Neurological Disease
    L-655708 is a potent α5 subunit-selective GABAA receptor inverse agonist (Ki=0.45 nM).
    L-655708
  • HY-16579
    Etifoxine hydrochloride
    3 Publications Verification

    HOE 36-801 hydrochloride

    GABA Receptor Neurological Disease
    Etifoxine hydrochloride, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine hydrochloride reveals anxiolytic and anticonvulsant properties in rodents .
    Etifoxine hydrochloride
  • HY-P4279

    Angiotensin-converting Enzyme (ACE) Cholinesterase (ChE) Cardiovascular Disease
    Ovalbumin (154-159) is a protein fragment consisting of residues 154-159 of chicken ovalbumin. Ovalbumin (154-159) is also a poorly conserved sequence (Thr-Asn-Gly-Ile-Ile-Arg) in the α-subunit of the Torpedo acetylcholine receptor, located within the α150-164 epitope region, and exhibits significant angiotensin-converting enzyme (ACE) inhibitory activity .
    Ovalbumin (154-159)
  • HY-120874

    PF-06372865; CVL-865

    GABA Receptor Neurological Disease
    Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .
    Darigabat
  • HY-W012123

    GABA Receptor Endogenous Metabolite Neurological Disease
    3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals . 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits .
    3,4,5-Trimethoxycinnamic acid
  • HY-16579A
    Etifoxine
    3 Publications Verification

    HOE 36-801

    GABA Receptor Neurological Disease
    Etifoxine, a non-benzodiazepine GABAergic compound, is a positive allosteric modulator of α1β2γ2 and α1β3γ2 subunit-containing GABAA receptors. Etifoxine reveals anxiolytic and anticonvulsant properties in rodents .
    Etifoxine
  • HY-P99524

    GBR500

    Integrin Neurological Disease Inflammation/Immunology
    Vatelizumab (GBR500) is a monoclonal antibody that targets the α2 subunit (CD49b) of very late antigen 2 (VLA-2). Vatelizumab can be used for research on multiple sclerosis .
    Vatelizumab
  • HY-153967
    BLU0588
    2 Publications Verification

    PKA Cancer
    BLU0588 is an orally active, potent and selective PRKACA (protein kinase cAMP-activated catalytic subunit alpha) kinase inhibitor, with an IC50 of 1 nM and dissociation constant (Kd) of 4 nM. BLU0588 can be used for fibrolamellar carcinoma (FLC) research .
    BLU0588
  • HY-P5623
    RVG
    1 Publications Verification

    RVG29; RDP; Rabies Virus Glycoprotein-29

    nAChR Interleukin Related Neurological Disease Inflammation/Immunology
    RVG (RVG29) is a blood-brain barrier-permeable peptide derived from rabies virus glycoprotein, which binds to the α-7 subunit of neuronal nicotinic acetylcholine receptor (AchR). RVG efficiently delivers drugs to nerve cells and antigen-presenting cells in a targeted manner, and enhances the efficiency of antigen presentation and drug delivery .
    RVG
  • HY-P9947
    Efalizumab
    1 Publications Verification

    Integrin Others
    Efalizumab is a targeted T cell modulator, and is a humanized monoclonal antibody of CD11a, the α subunit of LFA-1. Efalizumab inhibits T cell activation, cutaneous T cell trafficking, and T cell adhesion to keratinocytes, can be used for plaque psoriasis research .
    Efalizumab
  • HY-100991

    ZK 39106; LSU-65

    GABA Receptor Neurological Disease
    FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of β-adrenoceptors in mouse cerebral cortex .
    FG 7142
  • HY-E70373

    Biochemical Assay Reagents Others
    λ Protein phosphatase is a serine/threonine phosphatase encoded by bacteriophage Lambda. λ Protein phosphatase is activated with requirement for divalent cations, such as Mn 2+. λ Protein phosphatase is able to dephosphorylate casein, adenovirus E1A protein, and the α subunit of phosphorylase kinase
    λ Protein phosphatase
  • HY-P99031

    CAM 3001

    c-Fms Cardiovascular Disease Inflammation/Immunology
    Mavrilimumab (CAM 3001) is a monoclonal antibody that binds to the α subunit of the granulocyte-macrophage colony stimulating factor (GM-CSF) receptor and blocks intracellular signalling downstream of GM-CSF. GM-CSF might be a mediator of the hyperactive inflammatory response associated with respiratory failure and death .
    Mavrilimumab
  • HY-W017387
    Sodium α-ketoisocaproate
    1 Publications Verification

    Sodium 4-methyl-2-oxopentanoate; 2-Ketoisocaproic acid sodium salt

    Branched Chain Amino Acid Transaminase (BCAT) Potassium Channel Na+/Ca2+ Exchanger Metabolic Disease
    Sodium α-ketoisocaproate (Sodium 4-methyl-2-oxopentanoate) is an insulin secretagogue. Sodium α-ketoisocaproate undergoes transamination catalyzed by BCAT and BCATm to produce α-ketoglutarate and leucine; it also binds to the SUR1 site to inhibit KATP channel activity, but does not directly affect the Kir6.2 subunit. Sodium α-ketoisocaproate regulates Ca 2+ influx. Sodium α-ketoisocaproate exerts insulinotropic activity in pancreatic islets and intact mouse pancreata with sufficient BCATm expression. Sodium α-ketoisocaproate can be used in research related to type 2 diabetes .
    Sodium α-ketoisocaproate
  • HY-103511

    GABA Receptor Neurological Disease
    TCS1105 is a benzodiazepine ligand with agonist for α2-subunit containing GABAA receptors and antagonist for α1-subunit containing GABAA receptors. TCS1105 reduces anxiety-like behavior in mice. TCS1105 enhances offensive behavior and social dominance. TCS1105 blocks Sema3A induced AGC (axonal growth cones) collapse in a concentration-dependent fashion .
    TCS1105
  • HY-102076

    Adrenergic Receptor Others
    0990CL is a specific heterotrimeric Gαi subunit inhibitor by direct interaction with Gαi. 0990CL is able to block α2AR mediated regulation of cAMP .
    0990CL
  • HY-P990086

    RG-6292; RO-7296682

    Interleukin Related Cancer
    Vopikitug is an IgG1-kappa, anti-IL2RA (interleukin 2 receptor alpha subunit, IL-2RA, TAC, p55, CD25) homo sapiens monoclonal antibody. Vopikitug shows antineoplastic activity .
    Vopikitug
  • HY-149483

    nAChR Neurological Disease
    CVN417 is an orally active α6 subunit-containing nAChR antagonist, modulating phasic dopaminergic neurotransmission in an impulse-dependent manner. CVN417 inhibits Ca(2+) effluents mediated by nAChR subunits with IC50s of 0.086 μM (α6), 2.56 μM (α3) and 0.657 μM (α4), respectively. CVN417 attenuates resting tremor in Rodent models, displays the potential to improve movement dysfunction, in conditions such as Parkinson's disease .
    CVN417
  • HY-P5623B
    RVG TFA
    1 Publications Verification

    RVG29 TFA; RDP TFA; Rabies Virus Glycoprotein-29 TFA

    Bacterial Infection
    RVG TFA is a peptide derived from Rabies Virus Glycoprotein that binds to the α-7 subunit of nicotinic acetylcholine receptors (AchR) of neuronal cells. RVG enhances delivery of Mycobacterium tuberculosis antigens to antigen-presenting cells .
    RVG TFA
  • HY-NP144

    Biochemical Assay Reagents Neurological Disease
    Nerve Growth Factor 7S, murine submaxillary gland is an α2β2γ2 complex in which the β-NGF dimer (the active neurotrophin) is associated with two α-NGF and two γ-NGF subunits .
    Nerve Growth Factor 7S,murine submaxillary gland
  • HY-P2558

    GSK-3 Others
    GSK3 Substrate, α, β subunit is peptide substrate for glycogen synthase kinase-3 (GSK-3) and can be used to measure GSK-3 activity .
    GSK3 Substrate, α, β subunit
  • HY-153584

    GABA Receptor Neurological Disease
    MRK-898 is an orally active GABA(A) receptor modulator. MRK-898 binds to α1, α2, α3 or α5 subunit of GABA(A) receptor with Ki values of 1.2 nM, 1.0 nM, 0.73 nM, and 0.50 nM, respectively. However, α1-containing GABA(A) receptors are identified as the "sedative" and α2- and/or α3-containing receptors as the "anxiolytic" subtype(s) .
    MRK-898
  • HY-164728

    Calcium Channel Neurological Disease
    Pregabalin diacid is an impurity of Pregabalin, a lipophilic GABA (γ-aminobutyric acid) analog with anxiolytic and anticonvulsant activity. Pregabalin may act on the α(2)β subunit of voltage-dependent calcium channels, which are widely distributed in the peripheral and central nervous systems. Pregabalin can effectively induce hypoalgesia and improve behavioral disorders .
    Pregabalin diacid
  • HY-19371

    GABA Receptor Neurological Disease
    Lorediplon is a novel non-benzodiazepine drug acting as a GABAA receptor modulator, differentially active at the alpha1-subunit, associated with promoting sleep.
    Lorediplon
  • HY-148866

    Calcium Channel Neurological Disease Endocrinology
    Cavα2δ1&NET-IN-3 (example 216) is an inhibitor of the subunit α2δ of voltage-gated calcium channels (VGCC) and noradrenaline transporter (NET). Cavα2δ1&NET-IN-3 has Kis of 100-500 nM for human α2δ-1 subunit of Cav2.2 calcium channel and NET, respectively .
    Cavα2δ1&NET-IN-3
  • HY-103384

    Casein Kinase Cancer
    TMCB is a selective, ATP-competitive CK2 (casein kinase II) inhibitor with distinct Ki values of 83 nM and 21 nM for the two different catalytic CK2 subunits α and α', respectively .
    TMCB
  • HY-150073

    PKA Cancer
    DS01080522 is a Protein Kinase cAMP-Activated Catalytic Subunit Alpha (PRKACA) inhibitor. DS01080522 inhibits PRKACA kinase activity and CREB phosphorylation with IC50s of 0.8 nM and 66 nM, respectively. DS01080522 can be used for the research of cancer .
    DS01080522
  • HY-P1259

    Proteasome Bacterial Inflammation/Immunology
    PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor. PR-39 reversibly binds to the α7 subunit of the proteasome and blocks degradation of NF-κB inhibitor IκBα by the ubiquitin-proteasome pathway. PR-39 stimulates angiogenesis, inhibits inflammatory responses and significant reduces myocardial infarct size in mice .
    PR-39
  • HY-122016A

    Bacterial Infection Inflammation/Immunology
    BRD-4592 is an allosteric inhibitor targeting Mycobacterium tuberculosis tryptophan synthase (TrpAB). BRD-4592 binds at the α-β-subunit interface of TrpAB, with an IC50 of 70.9 nM for the α-subunit and 22.6 nM for the β-subunit .
    BRD-4592
  • HY-P990959

    Apoptosis Inflammation/Immunology
    Lesigercept is a recombinant fusion protein comprising an FcERI (IgE Fc receptor subunit alpha) fused to a human IgG4 Fc .
    Lesigercept
  • HY-W012123R

    Reference Standards GABA Receptor Endogenous Metabolite Neurological Disease
    3,4,5-Trimethoxycinnamic acid is a phenylpropanoid isolated from the roots of Polygala tenuifolia WILLD, with anti-stress effect, prolonging the sleeping time in animals . 3,4,5-Trimethoxycinnamic acid increases expression of GAD65 and γ-subunit of GABAA receptor, but shows no effect on the amounts of α-, β-subunits .
    3,4,5-Trimethoxycinnamic acid (Standard)
  • HY-12650S

    DS5565-13C2,d1 (Mixture of Diastereomers)

    Isotope-Labeled Compounds Others
    Mirogabalin- 13C2,d1 (Mixture of Diastereomers) is a 13C and deuterium labeled Mirogabalin. Mirogabalin (DS-5565) is a preferentially selective α2δ-1 ligand characterized by high potency and selectivity to the α2δ-1 subunit of voltage-sensitive calcium channel complexes in the CNS .
    Mirogabalin-13C2,d1 (Mixture of Diastereomers)
  • HY-P5549

    Bacterial Fungal Infection
    Hb 98-114, the amino acids 98-114 of the alpha subunit of bovine hemoglobin, is an antimicrobial peptide. Hb 98-114 is active against several yeast and filamentous fungi (MIC: 2.1 μM-12.5 μM) .
    Hb 98–114
  • HY-148863

    Calcium Channel Monoamine Transporter Inflammation/Immunology
    Cavα2δ1&NET-IN-2 (Compound 45CS) is a dual inhibitor of the α2δ‑1 subunit of voltage-gated calcium channels (Cavα2δ-1) and the norepinephrine transporter (NET). Cavα2δ1&NET-IN-2 inhibits Cavα2δ-1 with a Ki of 454 nM. Cavα2δ1&NET-IN-2 inhibits NET with a Ki of 59 nM and IC50 of 7 nM. Cavα2δ1&NET-IN-2 can be used for research of pain .
    Cavα2δ1&NET-IN-2
  • HY-E70547A

    Biochemical Assay Reagents Cardiovascular Disease
    Murine Factor XIII is a natural coagulation factor present in plasma, composed of two identical α subunits and two identical β subunits .
    Murine Factor XIII
  • HY-U00388

    Calcium Channel Neurological Disease
    α2δ ligand 1 is a ligand to the α2δ-1 subunit of voltage-sensitive calcium channel, extracted from patent US20040186177.
    α2δ ligand 1
  • HY-12650A

    (rel)-DS5565

    Calcium Channel Neurological Disease
    (rel)-Mirogabalin ((rel)-DS5565) is a voltage-dependent calcium channel inhibitor that acts on the α2δ-1 subunit .
    (rel)-Mirogabalin

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