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alpha blocker

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539

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6

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46

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Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-N6782
    Oligomycin
    Maximum Cited Publications
    105 Publications Verification

    Oxidative Phosphorylation ATP Synthase Fungal Antibiotic Infection Cancer
    Oligomycin, an antifungal antibiotic, is an inhibitor of H +-ATP-synthase. Oligomycin blocks oxidative phosphorylation and the electron transport chain. Oligomycin inhibits HIF-1alpha expression in hypoxic tumor cells .
    Oligomycin
  • HY-A0070A
    Liothyronine
    35+ Cited Publications

    Triiodothyronine; 3,3',5-Triiodo-L-thyronine; T3

    Thyroid Hormone Receptor Endogenous Metabolite Endocrinology Cancer
    Liothyronine is an active form of thyroid hormone. Liothyronine binds to thyroid hormone receptors TRα and TRβ with Kis of 2.33 and 2.29 nM for hTRα and hTRβ, respectively. Liothyronine also binds to PVR and blocks the interaction of TIGIT/PVR .
    Liothyronine
  • HY-N0127
    Yohimbine Hydrochloride
    15+ Cited Publications

    Adrenergic Receptor Endocrinology
    Yohimbine hydrochloride is an alpha-2 renal adenomatase receptor inhibitor, blocking pre- and post-contact alpha-2 renal adenomatase receptors, causing the release of renal adenoma and multiple sclerosis.
    Yohimbine Hydrochloride
  • HY-15484
    Pifithrin-α hydrobromide
    95+ Cited Publications

    Pifithrin hydrobromide; PFTα hydrobromide

    MDM-2/p53 Aryl Hydrocarbon Receptor Ferroptosis Apoptosis Cancer
    Pifithrin-α hydrobromide is a p53 inhibitor which blocks its transcriptional activity and prevents cells from apoptosis. Pifithrin-α hydrobromide is also an aryl hydrocarbon receptor (AhR) agonist.
    Pifithrin-α hydrobromide
  • HY-101855

    Anle138b

    Amyloid-β Neurological Disease
    Emrusolmin (Anle138b), an oligomeric aggregation inhibitor, blocks the formation of pathological aggregates of prion protein (PrPSc) and of α-synuclein (α-syn). Emrusolmin strongly inhibits oligomer accumulation, neuronal degeneration, and disease progression in vivo. Emrusolmin has low toxicity and an excellent oral bioavailability and blood-brain-barrier penetration. Emrusolmin blocks Aβ channels and rescues disease phenotypes in a mouse model for amyloid pathology .
    Emrusolmin
  • HY-108434
    Ceapin-A7
    20+ Cited Publications

    ATF6 Neurological Disease Metabolic Disease
    Ceapin-A7 is a selective blocker of ATF6α signaling in response to ER stress, with an IC50 of 0.59 μM. Ceapin-A7 can be used to explore both the mechanism of activation of ATF6α and its role in pathological settings .
    Ceapin-A7
  • HY-P1264
    α-Bungarotoxin
    Maximum Cited Publications
    7 Publications Verification

    nAChR Neurological Disease
    α-Bungarotoxin is a competitive antagonist at nicotinic acetylcholine receptors (nAChRs). α-Bungarotoxin, a selective α7 receptor blocker, blocks α7 currents with an IC50 of 1.6 nM and has no effects on α3β4 currents at concentrations up to 3 μM .
    α-Bungarotoxin
  • HY-W142080

    α-Methyltryptophan

    mTOR Autophagy Apoptosis Amino Acid Derivatives Metabolic Disease Cancer
    α-Methyl-DL-tryptophan (α-Methyltryptophan), a tryptophan derivative, is a selective SLC6A14 blocker. In estrogen receptor (ER)-positive breast cancer cells, α-Methyl-DL-tryptophan inhibits mTOR and activates autophagy and apoptosis. α-Methyl-DL-tryptophan also has the effect of reducing weight .
    α-Methyl-DL-tryptophan
  • HY-N1919
    Ajmalicine
    2 Publications Verification

    Raubasine

    Adrenergic Receptor Cholinesterase (ChE) Neurological Disease Endocrinology
    Ajmalicine (Raubasine) is a potent adrenolytic agent which preferentially blocks α1-adrenoceptor. Ajmalicine is an reversible but non-competitive nicotine receptor full inhibitor, with an IC50 of 72.3 μM. Ajmalicine also can be used as anti-hypertensive, and serpentine, with sedative activity .
    Ajmalicine
  • HY-111255
    SPD304
    5+ Cited Publications

    TNF Receptor Cancer
    SPD304 is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 μM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α .
    SPD304
  • HY-10122
    Silodosin
    5 Publications Verification

    KAD 3213; KMD 3213

    Adrenergic Receptor Bacterial Endocrinology Cancer
    Silodosin (KAD 3213; KMD 3213) is a potent, selective and orally active α1A-adrenergic receptor (α1A-AR) blocker. Silodosin exhibits high affinity for α1A-AR (Ki=0.036 nM), over 162-fold and 50-fold than for α1B-AR and α1D-AR with Ki values of 21 nM and 2.0 nM, respectively. Silodosin is an effective and well-tolerated agent, it can be used for the investigation of LUTS/BPH .
    Silodosin
  • HY-173405

    Ras PI3K Akt Cancer
    VVD-699 is a covalent blocker of the RAS-p110α interaction with oral activity. VVD-699 inhibits activation of PI3Kα (IC50: 104 nM in H358 cells) . VVD-699 inhibits phosphorylated AKT. VVD-699 can be used for the research of KRAS mutant/amplified cancer .
    VVD-699
  • HY-B0006B

    (S)-BM 14190

    Adrenergic Receptor Cardiovascular Disease
    (S)-Carvedilol, the S-enantiomer of Carvedilol, is a non-selective β/α-1 blocker. (S)-Carvedilol exerts protection against the vascular or cardiac toxicity of Doxorubicin (DOX) .
    (S)-Carvedilol
  • HY-B0362A
    Phentolamine mesylate
    5+ Cited Publications

    Phentolamine methanesulfonate

    Adrenergic Receptor Cardiovascular Disease Endocrinology Cancer
    Phentolamine mesylate (Phentolamine methanesulfonate) is a reversible, non-selective, and orally active blocker of α1 and α2 adrenergic receptor that expands blood vessels to reduce peripheral vascular resistance. Phentolamine mesylate can be used for the research of pheochromocytoma-related hypertension, heart failure and erectile dysfunction .
    Phentolamine mesylate
  • HY-P99950

    ALX148

    CD47
    Evorpacept (ALX148) is a high-affinity CD47-blocking fusion protein with an inactive human immunoglobulin Fc region. Evorpacept binds to CD47, blocks the interaction of the CD47-SIRPα immune checkpoint, and inhibits the binding of wild-type SIRPα to CD47. Evorpacept is applicable to research related to acute myeloid leukemia .
    Evorpacept
  • HY-132996

    Biochemical Assay Reagents Others
    4-Isothiocyanatophenyl α-D-Mannopyranoside, an organic isothiocyanate, is a building block and reagent which is used for preparing neoglycoproteins .
    4-Isothiocyanatophenyl α-D-Mannopyranoside
  • HY-159644

    AB521

    HIF/HIF Prolyl-Hydroxylase VEGFR Cancer
    Casdatifan (AB521) is an orally active and selective allosteric small-molecule inhibitor of hypoxia-inducible factor 2α (HIF-2α). Casdatifan inhibits pro-tumor gene transcription by blocking the heterodimerization of HIF-2α with ARNT, and significantly suppresses tumor growth in clear cell renal cell carcinoma (ccRCC) models either as a monotherapy or in combination with agents such as Zimberelimab (HY-P99109). Casdatifan is applicable for the research of ccRCC .
    Casdatifan
  • HY-156106

    HIF/HIF Prolyl-Hydroxylase Ligands for E3 Ligase E1/E2/E3 Enzyme Cancer
    VHL-IN-1 (Compound 30) is an E3 ligase VHL inhibitor with a Kd value of 37 nM. VHL-IN-1 blocks VHL-mediated ubiquitination and degradation of HIF-1α. VHL-IN-1 stabilizes the protein levels of HIF-1α and hydroxylated HIF-1α, and induces the transcriptional activity of HIF-1α. VHL-IN-1 can be used for PROTAC development. VHL-IN-1 is applicable for cancer research .
    VHL-IN-1
  • HY-44809

    HIF/HIF Prolyl-Hydroxylase Bacterial Cardiovascular Disease Infection Inflammation/Immunology
    Izilendustat is a potent prolyl hydroxylase inhibitor. Izilendustat competitively inhibits HIFPH2 activity, blocks HIF-1α degradation, stabilizes HIF-1α and HIF-2α proteins, and upregulates downstream target gene expression. Izilendustat can reduce intestinal inflammation and damage, enhance the ability of phagocytes to clear pathogens, and improve ischemia-related pathological phenotypes. Izilendustat can be used for the research of inflammatory bowel disease, ischemic vascular disease and anemia .
    Izilendustat
  • HY-N7259

    JNK p38 MAPK Apoptosis Inflammation/Immunology
    (+)-Isomenthone is an enantiomer form of Menthone (HY-N2381). (+)-Isomenthone blocks TNF-α-triggered activation of the JNK and p38 MAPK pathways.(+)-Isomenthone inhibits TNF-α-mediated reductions in cell viability, increases in apoptosis, and downstream apoptotic events linked to pathway activation.(+)-Isomenthone protects human dermal fibroblasts against TNF-α-induced cell death under serum-deprived conditions .
    (+)-Isomenthone
  • HY-115840

    Apoptosis Cancer
    ICL-CCIC-0019 is an inhibitor of choline kinase α (CHKα). ICL-CCIC-0019 induces G1 block, endoplasmic reticulum stress apoptosis in cancer cell lines .
    ICL-CCIC-0019
  • HY-135783
    AT 1001
    1 Publications Verification

    nAChR Neurological Disease Metabolic Disease Inflammation/Immunology
    AT 1001 is an orally effective α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) antagonist with a Ki value of 2.64 nM. AT 1001 reversibly blocks Epibatidine (HY-101078)-induced inward currents in HEK cells transfected with α3β4 nAChR. AT 1001 dose-dependently blocks nicotine self-administration behavior in rats, alleviates gluten-induced gastrointestinal symptoms, blocks tight junction toxin-induced immune responses, and reduces the incidence of type 1 diabetes in rats. AT 1001 can be used in the research of nicotine addiction and celiac disease .
    AT 1001
  • HY-P99223

    MEDI-575

    PDGFR Cancer
    Tovetumab (MEDI-575) is an anti-PDGFRα monoclonal antibody that selectively blocks the PDGFRα signal transduction. Tovetumab can be used in the research of glioblastoma and non-small cell lung cancer (NSCLC) .
    Tovetumab
  • HY-125713

    Glycosidase Enterovirus Infection
    Ganoderic acid Y is a α-glucosidase inhibitor with an IC50 of 170 μM for yeast α-glucosidase. Ganoderic acid Y inhibits enterovirus 71 (EV71) replication through blocking EV71 uncoating .
    Ganoderic acid Y
  • HY-133807
    Benpyrine
    3 Publications Verification

    TNF Receptor Inflammation/Immunology
    Benpyrine is a highly specific and orally active TNF-α inhibitor with a KD value of 82.1 μM. Benpyrine tightly binds to TNF-α and blocks its interaction with TNFR1, with an IC50 value of 0.109 µM. Benpyrine has the potential for TNF-α mediated inflammatory and autoimmune disease research .
    Benpyrine
  • HY-108530

    RAR/RXR Cancer
    MM11253 is a potent and selective RARγ antagonist with an IC50 of 44 nM. MM11253 has lower inhibition of RARα, RARβ and RXRα. MM11253 blocks the growth inhibitory effects of RARγ-selective agonists .
    MM11253
  • HY-111255A
    SPD304 dihydrochloride
    5+ Cited Publications

    TNF Receptor Inflammation/Immunology Cancer
    SPD304 dihydrochloride is a selective TNF-α inhibitor, which promotes dissociation of TNF trimers and therefore blocks the interaction of TNF and its receptor. SPD304 has an IC50 of 22 μM for inhibiting in vitro TNF receptor 1 (TNFR1) binding to TNF-α .
    SPD304 dihydrochloride
  • HY-14282
    Lanoconazole
    1 Publications Verification

    Fungal Infection Inflammation/Immunology
    Lanoconazole is a potent and orally active imidazole antifungal agent, shows a broad spectrum of activity against fungi?in vitro?and?in vivo . Lanoconazole interferes with ergosterol biosynthesis by inhibiting sterol 14-alpha demethylase and blocking fungal membrane ergosterol biosynthesis. Lanoconazole can be used for the investigation of dermatophytosis and onychomycosis .
    Lanoconazole
  • HY-115903
    HIF-1α-IN-2
    4 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-2 is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 suppresses HIF-1α expression by blocking transcription and protein translation .
    HIF-1α-IN-2
  • HY-101437
    Ralfinamide
    1 Publications Verification

    FCE-26742A

    Sodium Channel Neurological Disease
    Ralfinamide (FCE-26742A) is an orally available Na + blocker derived from α-aminoamide, with function of suppressing pain .
    Ralfinamide
  • HY-114333

    1-Octyl 2-oxopentanedioate

    HIF/HIF Prolyl-Hydroxylase Metabolic Disease Cancer
    Octyl-α-ketoglutarate (1-Octyl 2-oxopentanedioate) is a stable, cell-permeable form of α-ketoglutarate which accumulates rapidly in HEK293 cells with a dysfunctional tricarboxylic acid (TCA) cycle, stimulating prolyl hydroxylase (PHD) activity. In addition, Octyl-α-ketoglutarate competitively blocks succinate- or fumarate-mediated inhibition of PHD .
    Octyl-α-ketoglutarate
  • HY-143224B

    CD47 Cancer
    NCGC00138783 TFA is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 μM. NCGC00138783 TFA directly blocks the interaction between CD47 and SIRPα axis .
    NCGC00138783 TFA
  • 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-164102

    TNF Receptor NF-κB Inflammation/Immunology
    TNF-α-IN-18 (Compound 61) is an inhibitor for TNF-α (IC50 of 1.8 μM), that inhibits TNF signaling pathway through block of NF-kB migration from cytoplasm to nucleus. TNF-α-IN-18 exhibits slight cytotoxicity to mouse fibroblast LM cell, with a CC50 >50 μM. TNF-α-IN-18 ameliorates the TNF- or Lipopolysaccharide (HY-D1056)-induced sepsis in mouse models. TNF-α-IN-18 protects mice from rheumatoid arthritis .
    TNF-α-IN-18
  • HY-P5694

    HPV Parasite Infection
    Human α-defensin 5 is an antiviral peptide. Human α-defensin 5 blocks infection of non-enveloped viruses, including AdV, HPV, and polyomaviruses (IC50: 0.6-1.25 μM for HPV16). Human α-defensin 5 can bind to the viral capsid and blocks escape of the virus from the endosome. Human α-defensin 5 increases HIV binding to the cell surface. Human α-defensin 5 also has parasiticidal activity .
    Human α-defensin 5
  • HY-P2707

    α-DTX

    Sodium Channel Potassium Channel Neurological Disease
    α-Dendrotoxin (α-DTX) is a voltage-gated K + channel blocker and an acid-sensing ion channel (ASIC) inhibitor. α-Dendrotoxin blocks Kv1.1, Kv1.2, Kv1.6 and D-type (ID) voltage-gated K + channels, and reversibly inhibits slowly inactivating potassium currents. α-Dendrotoxin induces epilepsy-related behaviors in mice. α-Dendrotoxin can be used in studies related to tonic-clonic seizures .
    α-Dendrotoxin
  • HY-115903A
    HIF-1α-IN-2 hydrochloride
    4 Publications Verification

    HIF/HIF Prolyl-Hydroxylase Cancer
    HIF-1α-IN-2 hydrochloride is an effective HIF-1α inhibitor with anticancer potencies (IC50s of 28 nM and 15 nM in MDA-MB-231 and MiaPaCa-2 cells, respectively). HIF-1α-IN-2 hydrochloride suppresses HIF-1α expression by blocking transcription and protein translation .
    HIF-1α-IN-2 hydrochloride
  • HY-P11097

    CD47 Cancer
    Pep-20 is a CD47/SIRPα blocking peptide with KD values of 2.91 and 3.63 μM for human and mouse CD47, respectively. IC50 values for blocking the human and mouse CD47/SIRPα interaction are 24.56 and 12.03 μM, respectively. Pep-20 has antitumor activity .
    Pep-20
  • HY-101656

    RMI81968

    Adrenergic Receptor Cardiovascular Disease
    Medroxalol (RMI81968) is an orally active adrenergic receptor antagonist, blocks α- and β-adrenergic receptors. Medroxalol shows antihypertensive and vasodilating effects .
    Medroxalol
  • HY-134858

    A1AT modulator 1

    Serpin Ser/Thr Protease Metabolic Disease
    GSK716 (A1AT modulator 1) is an orally active Z α1-antitrypsin (Z-A1AT) inhibitor with a pIC50 of 8.3. GSK716 binds a cryptic Z α1-antitrypsin pocket, stabilizes monomeric folding intermediates, blocks polymerization, and increases monomer secretion. GSK716 acts on select sensitive α1-antitrypsin variants but fails to affect resistant variants. GSK716 can be used for the research of α1-antitrypsin deficiency and α1-antitrypsin deficiency-associated liver disease .
    GSK716
  • HY-121045

    KO 1366

    Adrenergic Receptor Cardiovascular Disease
    Bunitrolol hydrochloride is an orally active β-adrenergic blocker that has a high affinity for β-adrenergic receptors. Bunitrolol hydrochloride exerts significant β-receptor antagonist activity and has weak α1-blocking activity. Bunitrolol hydrochloride is mainly used in the study of cardiovascular diseases such as hypertension and angina pectoris, and is also used in placental transport research .
    Bunitrolol
  • HY-115038

    α-synuclein Neurological Disease
    ELN484228 is a blocker of α-synuclein which is a key protein in Parkinson’s disease.
    ELN484228
  • HY-P5881

    PKC Cardiovascular Disease
    PKCα (C2-4) inhibitor peptide is a PKCα specific inhibitor peptide that blocks the inhibition of IKr by the α1A adrenoreceptor agonist A-61603 (HY-101366) .
    PKCα (C2-4) inhibitor peptide
  • HY-B0193AS

    Adrenergic Receptor Isotope-Labeled Compounds Neurological Disease
    Prazosin-d8 hydrochloride is the deuterium labeled Prazosin hydrochloride. Prazosin hydrochloride is an alpha-adrenergic blocker .
    Prazosin-d8 hydrochloride
  • HY-149331

    TNF Receptor Caspase NF-κB Inflammation/Immunology
    TNF-α-IN-11 (Compound 10) is a TNF-α inhibitor with a KD value of 12.06 μM. TNF-α-IN-11 binds to TNF-α and blocks the activation of TNF-α-trigged caspase and NF-κB signaling pathway. TNF-α-IN-11 inhibits the phosphorylation of IκBα, as well as the nuclear translocation of NF κB p65. TNF-α-IN-11 can be used for research of TNF-α-mediated autoimmune diseases .
    TNF-α-IN-11
  • HY-101041

    (E)-Tyrphostin AG 556

    EGFR Inflammation/Immunology
    (E)-AG 556 is a highly selective EGFR inhibitor and also blocks LPS-induced TNF-α production .
    (E)-AG 556
  • HY-143224

    CD47 Cancer
    NCGC00138783 is a selective inhibitor targeting CD47/SIRPα axis, with an IC50 of 50 µM. NCGC00138783 directly blocks the interaction between CD47 and SIRPα axis .
    NCGC00138783
  • HY-U00365

    5-HT Receptor Adrenergic Receptor Cardiovascular Disease Endocrinology
    5-HT2 antagonist 1 is a potent antagonist of 5-HT2 receptor, with weak α1 adrenoceptor blocking activity.
    5-HT2 antagonist 1
  • HY-12718

    Adrenergic Receptor Cardiovascular Disease
    (±)-WB 4101 is a highly selective α1-adrenergic receptor antagonist. (±)-WB 4101 blocks norepinephrine-induced vascular smooth muscle contraction to exert antihypertensive and benign prostatic hyperplasia (BPH)-relieving effects. (±)-WB 4101 is promising for research of hypertension and BPH .
    (±)-WB 4101

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