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14-3-3 eta/YWHAH Inhibitors

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Targets Recommended:
製品番号 製品名 Target 研究分野 構造式
  • HY-14184
    Macitentan
    10+ Cited Publications

    ACT-064992

    Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
    Macitentan
  • HY-A0013
    Bosentan
    Maximum Cited Publications
    30 Publications Verification

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    Bosentan is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
    Bosentan
  • HY-10088
    Zibotentan
    1 Publications Verification

    ZD4054

    Endothelin Receptor Apoptosis Endocrinology Cancer
    Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research .
    Zibotentan
  • HY-15403
    Atrasentan
    5+ Cited Publications

    ABT-627; (+)-A 127722; A-147627

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    Atrasentan (ABT-627) is an endothelin receptor antagonist with IC50 of 0.0551 nM for ETA .
    Atrasentan
  • HY-122815

    Fusicoccin A

    Apoptosis Cancer
    Fusicoccin (Fusicoccin A), a fungal pytotoxin, is a stabilizer of specific 14-3-3 protein-protein interactions. Fusicoccin sabilizes H +-ATPase/14-3-3 cmplex in pants, maintaining the enzyme in activated state. Fusicoccin also stabilizes 14-3-3 protein interactions with binding partners containing a C-terminal 14-3-3 recognition motif (a mode 3 motif), such as ERα, GPIbα, TASK3, CTFR, and p53. Fusicoccin induces apoptosis in cancer cells and has anticancer activity .
    Fusicoccin
  • HY-A0013A
    Bosentan hydrate
    Maximum Cited Publications
    30 Publications Verification

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    Bosentan hydrate is a competitive and dual antagonist of endothelin-1 (ET) for the ETA and ETB receptors with Ki of 4.7 nM and 95 nM in human SMC, respectively.
    Bosentan hydrate
  • HY-115501

    Ser/Thr Protease Cancer
    (E)-FOBISIN101 is a 14-3-3 protein-protein interaction (14-3-3 protein-protein interaction) inhibitor, with IC50 values of 9.3 and 16.4 μM for disrupting the binding of 14-3-3ζ or 14-3-3γ to PRAS40, respectively. (E)-FOBISIN101 inhibits the binding of 14-3-3 to Raf-1 and proline-rich AKT substrate, and neutralizes the ability of 14-3-3 to activate exotoxin S ADP-ribosyltransferase. (E)-FOBISIN101 is applicable to 14-3-3-mediated cancer research .
    (E)-FOBISIN101
  • HY-12307
    (-)-Indolactam V
    2 Publications Verification

    Indolactam V

    PKC Cancer
    (-)-Indolactam V is a PKC activator, with Kis of 3.36 nM, 1.03 μM for η-CRD2 (PKCη surrogate peptide), γ-CRD2 (PKCγ surrogate peptide), and Kds of 5.5 nM (η-C1B), 7.7 nM (ε-C1B), 8.3 nM (δ-C1B), 18.9 nM (β-C1A-long), 20.8 nM (α-C1A-long), 137 nM (β-C1B), 138 nM (γ-C1A), 213 nM (γ-C1B), and has antitumor activity.
    (-)-Indolactam V
  • HY-101985
    BV02
    3 Publications Verification

    Bacterial PARP Caspase Apoptosis Autophagy Akt Infection Neurological Disease Inflammation/Immunology
    BV02 is a 14-3-3 inhibitor and an antibacterial agent. BV02 enhances the cleavage of PARP and caspase-3. BV02 induces Apoptosis, Autophagy, and enhances Akt activation. BV02 has anti-B. melitensis infection and epilepsy-promoting effects. BV02 can also be used in colitis research.
    BV02
  • HY-15403A
    Atrasentan hydrochloride
    5+ Cited Publications

    ABT-627 hydrochloride; (+)-A 127722 hydrochloride; A-147627 hydrochloride

    Endothelin Receptor Cardiovascular Disease Endocrinology Cancer
    Atrasentan hydrochloride (ABT-627 hydrochloride) is a selective endothelin A receptor antagonist with an IC50 of 0.0551 nM for ETA .
    Atrasentan hydrochloride
  • HY-12462

    GSK-3 Keap1-Nrf2 Ferroptosis IKK Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    WS3 is an allosteric inhibitor of 14-3-3 (14-3-3ζ: Kd = 2.29 μM). WS3 activates GSK3β by disrupting the binding of 14-3-3-pGSK3β, promotes the ubiquitination and degradation of NRF2, and inhibits the NRF2-ARE signaling pathway (IC50 = 135 nM). It exerts antioxidant inhibition and chemotherapeutic/ferroptosis sensitizing effects in tumors with hyperactivated NRF2. WS3 binds to EBP1/IKKε and promotes the proliferation of β cells and retinal pigment epithelial (RPE) cells, which can be applied to islet regeneration and RPE expansion transplantation . WS3 is applicable to research related to age-related macular degeneration, retinal degeneration and non-small cell lung cancer .
    WS3
  • HY-B1433

    S 9780

    Angiotensin-converting Enzyme (ACE) Cardiovascular Disease
    Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research .
    Perindoprilat
  • HY-17352

    Ro 61-1790; VML 588; AXV-034343

    Endothelin Receptor Cardiovascular Disease
    Clazosentan (Ro 61-1790) is a selective endothelin A (ETA) receptor antagonist. Clazosentan inhibits ET-1-mediated vasoconstriction. Clazosentan prevents cerebral vasospasm, vasospasm-related cerebral infarction .
    Clazosentan
  • HY-177590

    MMP Others
    14-3-3-IN-2 is a 14-3-3 protein inhibitor with an IC50 of 15 nM. 14-3-3-IN-2 can disrupt the interaction of 14-3-3α with aminopeptidase N and down-regulate 14-3-3α increased MMP-1 mRNA levels .
    14-3-3-IN-2
  • HY-15895S

    ACT-132577-d4

    Isotope-Labeled Compounds Endothelin Receptor Cardiovascular Disease Endocrinology
    Aprocitentan-d4 is a deuterium labeled Aprocitentan. Aprocitentan is a major and pharmacologically active metabolite of Macitentan. Aprocitentan is an orally active dual ETA/ETB antagonist with IC50s of 3.4 nM and 987 nM, and pA2 valus of 6.7 and 5.5, respectively. Aprocitentan is an antihypertensive agent .
    Aprocitentan-d4
  • HY-P1380A

    Apoptosis Bcl-2 Family Caspase Cancer
    Difopein TFA is a 14-3-3 protein inhibitor. Difopein TFA acts as an apoptosis inducer, regulates apoptosis-related proteins, downregulates Bcl-2, upregulates Bax, activates caspase-9 and caspase-3, and induces nuclear fragmentation, membrane-enclosed apoptotic bodies and DNA ladder formation. Difopein TFA serves as a tumor growth inhibitor, which inhibits the proliferation of glioma cells and induces their apoptosis in in vivo nude mouse models. Difopein TFA is applicable to glioma-related research .
    Difopein TFA
  • HY-NP143

    Biochemical Assay Reagents Neurological Disease
    Nerve Growth Factor 2.5S, murine submaxillary gland is a neurotrophic polypeptide required for normal growth and development of sympathetic and embryonic sensory neurons and certain cholinergic neurons in the central nervous system. Nerve Growth Factor 2.5S, murine submaxillary gland has only β-subunit , and shows nerve growth-promoting activity .
    Nerve Growth Factor 2.5S,murine submaxillary gland
  • HY-17351

    RO 610612

    Endothelin Receptor Cardiovascular Disease Neurological Disease Endocrinology Cancer
    Tezosentan (RO 610612) is an endothelin (ET) receptor antagonist, with pA2s of 9.5, 7.7 for ETA and ETB receptors, respectively.
    Tezosentan
  • HY-P1039A

    PHCVPRDLSWLDLEANMCLP TFA

    Raf Cancer
    R18 TFA is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1 .
    R18 TFA
  • HY-P0202A
    Endothelin 1 (swine, human) TFA
    Maximum Cited Publications
    8 Publications Verification

    ET-1 (swine, human) TFA

    Endothelin Receptor Cardiovascular Disease
    Endothelin 1 (swine, human) (ET-1) TFA is a synthetic peptide with the sequence of human and swine Endothelin 1, which is a potent endogenous vasoconstrictor. Endothelin 1 TFA acts through two types of receptors ETA and ETB .
    Endothelin 1 (swine, human) TFA
  • HY-146302
    14-3-3η Protein inhibitor 1
    2 Publications Verification

    Apoptosis Cancer
    14-3-3η Protein inhibitor 1 (Compound C11) is a 14-3-3η protein inhibitor with a KD of 35 µM. 14-3-3η Protein inhibitor 1 shows inhibitory activities against several typical human liver cancer cell lines. 14-3-3η Protein inhibitor 1 induces cell apoptosis and G1-S cell cycle arrest with good metabolic stability .
    14-3-3η Protein inhibitor 1
  • HY-117664

    DNA/RNA Synthesis Cancer
    PNR-7-02 is a dual Rev1 and human DNA polymerase η (hpol η) inhibitor, with an IC50 value of 8 μM against hpol η. PNR-7-02 binds to hpol η to disrupt the orientation of template DNA and block the catalytic function of hpol η. When used in combination with Cisplatin (HY-17394), PNR-7-02 induces DNA damage and replication stress in cells with intact hpol η function. PNR-7-02 can be used in mechanism studies related to chronic myeloid leukemia and ovarian cancer .
    PNR-7-02
  • HY-15404

    Lu-135252

    Endothelin Receptor Cardiovascular Disease Endocrinology
    Darusentan (Lu-135252) is a selective endothelin receptor A (ET-A) receptor antagonist, which binds with a Ki of 1.4 nM to the ET-A receptor and a Ki of 184 nM to ET-B receptor, respectively with a 100-fold selectivity for ETA rather than ETB receptors . Darusentan competes for radiolabeled endothelin binding in rat aortic vascular smooth muscle cells (RAVSMs) membranes with single-site kinetics, exhibiting a Ki of 13 nM .
    Darusentan
  • HY-119757

    SU1433; AG1433

    PDGFR VEGFR Cancer
    Tyrphostin AG1433 (SU1433) is a tyrosine kinases inhibitor. AG1433 is also a selective PDGFRβ and VEGFR-2 (Flk-1/KDR) inhibitor with IC50s of 5.0 μM and 9.3 μM, respectively. Tyrphostin AG1433 prevents blood vessel formation .
    Tyrphostin AG1433
  • HY-14184S

    ACT-064992-d4

    Isotope-Labeled Compounds Endothelin Receptor Apoptosis Cardiovascular Disease
    Macitentan-d4 is a deuterium labeled Sulfamethoxazole. Macitentan is an orally active, non-peptide dual ETA and ETB (endothelin) receptor antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
    Macitentan-d4
  • HY-14184R

    ACT-064992 (Standard)

    Reference Standards Endothelin Receptor Apoptosis Cardiovascular Disease Endocrinology Cancer
    Macitentan (Standard) is the analytical standard of Macitentan. This product is intended for research and analytical applications. Macitentan (ACT-064992) is an orally active, non-peptide dual ETA and ETB (endothelin receptor) antagonist. Macitentan has the potential for idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH) .
    Macitentan (Standard)
  • HY-169905

    Molecular Glues Others
    GR-14-3-3 stabilizer-1 (compound 10) is a molecular glue stabilizer that can be used to prepare molecular glues targeting glucocorticoids (GR) and block the interaction between GR and 14-3-3 .
    GR–14-3-3 stabilizer-1
  • HY-N1433

    Bacterial Infection Inflammation/Immunology
    Phytolaccagenin, a triterpenoid saponin, is the active component of Radix Phytolaccae. Phytolcaccagenin has antifungal activity, anti-inflammatory activity and lower toxicity
    Phytolaccagenin
  • HY-R00278

    MicroRNA Cancer
    hsa-miR-143-3p mimics are small, chemically synthesized double-stranded RNAs that mimic endogenous miRNAs and enable miRNA functional analysis by up-regulation of miRNA activity.
    hsa-miR-143-3p mimic
    hsa-miR-143-3p mimic
  • HY-W1005067

    Molecular Glues Hippo (MST) Estrogen Receptor/ERR Others
    EN171 is a covalent ligand that covalently targets both C38 and C96 on 14-3-3 to enhance 14-3-3 interactions with ERα, YAP and TAZ, leading to impaired estrogen receptor and Hippo pathway transcriptional activity. EN171 can not only be used as a molecular glue to enhance native protein interactions but can also be used as a covalent 14-3-3 recruiter in heterobifunctional molecules to sequester nuclear neo-substrates such as BRD4 and BLC6 into the cytosol .
    EN171
  • HY-130326

    Ru(η6-p-cymene)Cl2(pta)

    Apoptosis Caspase Cardiovascular Disease Cancer
    RAPTA-C (Ru(η6-p-cymene)Cl2(pta)) acts as an anti-cancer and anti-angiogenic agent. RAPTA-C exhibits anti-metastatic, anti-angiogenic, and anti-tumoral activities through protein and histone-deoxyribonucleic acid alterations. RAPTA-C exhibits cell growth inhibition by triggering G(2)/M phase arrest in cancer cells. RAPTA-C also enhances the levels of p53 and triggers the mitochondrial Apoptotic pathway, resulting in cytochrome C release and caspase-9 activation. RAPTA-C reduces the growth of tumors with the inhibition of angiogenesis in a ovarian carcinoma model .
    RAPTA-C
  • HY-B1433R

    S 9780 (Standard)

    Angiotensin-converting Enzyme (ACE) Reference Standards Cardiovascular Disease
    Perindoprilat (Standard) is the analytical standard of Perindoprilat. This product is intended for research and analytical applications. Perindoprilat (S 9780) is an angiotensin-converting enzyme (ACE) inhibitor with the IC50 value ranging from 1.5 to 3.2 nM. Perindoprilat can be used in hypertension research .
    Perindoprilat (Standard)
  • HY-P2496

    Endothelin Receptor Fluorescent Dye NF-κB COX Prostaglandin Receptor Apoptosis TNF Receptor Interleukin Related MMP Cardiovascular Disease Inflammation/Immunology Cancer
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled is an Endothelin-1 conjugated with Alexa Fluor 488 (HY-D1304). Endothelin-1 is an endogenous vasoconstrictor and agonist of ETA/ETB receptor. Endothelin 1 (swine, human) exerts effects including promoting mitosis, angiogenesis, tumor invasion and metastasis, and inhibiting apoptosis. Endothelin 1 (swine, human) induces inflammation and oxidative stress by activating the NF-κB pathway. Endothelin 1 (swine, human), Alexa Fluor 488-labeled is specifically designed for fluorescence imaging, flow cytometry or receptor localization studies, and can be used in research related to sepsis, atherosclerosis, systemic inflammatory response syndrome, cancer and congestive heart failure .
    Endothelin 1 (swine, human), Alexa Fluor 488-labeled
  • HY-156786

    Reactive Oxygen Species (ROS) Influenza Virus SARS-CoV HSV Infection
    TLD-1433 is the fourth-generation ruthenium (II) based photodynamic compound (PDC). TLD-1433 is activated by green light (525 ± 25 nm) and efficiently generates ROS to achieve pathogen inactivation. After photoinactivation, TLD-1433 significantly induces lipid peroxidation of the cell membrane, which can directly damage the integrity of the viral envelope. TLD-1433 has ID50 for enveloped viruses (such as H1N1 influenza virus, coronavirus OC43, HSV-1, Zika virus) is as low as nanomolar level; for non-enveloped viruses (such as adenovirus Ad5, mammalian rotavirus MRV), a concentration of micro-molar level is required for inactivation. TLD-1433 has antigen retention property and can be used for the preparation of inactivated vaccines .
    TLD-1433
  • HY-P1039

    PHCVPRDLSWLDLEANMCLP

    Raf Cancer
    R18 is a peptide antagonists of 14-3-3, with a KD of 70-90 nM. R18 efficiently blocks the binding of 14-3-3 to the kinase Raf-1, a physiological ligand of 14-3-3, and effectively abolished the protective role of 14-3-3 against phosphatase-induced inactivation of Raf-1 .
    R18
  • HY-123744

    Endothelin Receptor Cardiovascular Disease Neurological Disease
    PD-156707 is an orally active, nonpeptide and selective Endothelin-A receptor antagonist. PD-156707 binds to human ET-A and ET-B receptors with Ki values of 0.17 nM and 133.8 nM, respectively. PD-156707 shows reversal of established chronic hypoxic pulmonary hypertension in rats. PD-156707 can be used for the study of diseases associated with abnormal ET-A receptor activation, particularly pulmonary hypertension, stroke, and heart failure .
    PD-156707
  • HY-175872

    Estrogen Receptor/ERR Molecular Glues Others
    14-3-3σ/ERα stabilizer-2 (Compound 41) is a covalent 14-3-3σ/ERα stabilizer with a Kd of 10.1 nM. 14-3-3σ/ERα stabilizer-2 significantly decreases the dissociation rate of ERα, stabilizing the binary ERα/14-3-3σ interaction. 14-3-3σ/ERα stabilizer-2 can be used for molecular glues research .
    14-3-3σ/ERα stabilizer-2
  • HY-106994A

    YM598

    Endothelin Receptor Cardiovascular Disease Inflammation/Immunology Cancer
    Nebentan potassium (YM598) is a potent, selective and orally active non-peptide endothelin ETA receptor antagonist through the modification of Bosentan (HY-A0013). Nebentan potassium inhibits [ 125I] endothelin-1 binding to cloned human endothelin ETA and ETB receptor, with Ki of 0.697 nM and 569 nM, respectively . YM598 can ameliorate the progression of cor pulmonale and myocardial infarction in vivo .
    Nebentan potassium
  • HY-169081

    PROTACs Molecular Glues Others
    QS-57 is a PROTAC targeting BRD4. QS-57 can be used as a 14-3-3 molecular glue. (Red: EN171 (HY-W1005067), black: (2-Aminoethyl) carbamic acid (HY-W398806), Blue: JQ-1 (carboxylic acid) (HY-78695)) .
    QS-57
  • HY-162838

    Estrogen Receptor/ERR Others
    TCF199 is an allosteric stabilizer that stabilizes the 14-3-3/TAZ peptide interaction, binding to the 14-3-3ζ/E R α peptide and 14-3-3ζ/Chibby peptide. TCF199 has a Kd value of 122 μM for its interaction with 14-3-3/TAZ .
    TCF199
  • HY-135283

    A-216546

    Endothelin Receptor Cardiovascular Disease Endocrinology
    ABT-546 (A-216546), a chemical probe, is a potent, highly selective and active endothelin ETA receptor antagonist with a Ki of 0.46 nM for [ 125I]endothelin-1 binding to cloned human endothelin ETA. ABT-546 is >25,000-fold more selective for the ETA receptor than for the ETB receptor. ABT-546 blocks endothelin-1-induced arachidonic acid release and phosphatidylinositol hydrolysis with IC50 of 0.59 nM and 3 nM, respectively .
    ABT-546
  • HY-13711

    Endothelin Receptor Cardiovascular Disease
    S-1255 is an orally active and highly selective endothelin ETA receptor antagonist (Kd=0.39 nM). S-1255 blocks vasoconstriction and sustains hypotensive effects in hypertensive rats. S-1255 is promising for research of hypertension and cardiovascular disorders .
    S-1255
  • HY-118497

    Endothelin Receptor Cardiovascular Disease Metabolic Disease
    BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
    BMS 182874
  • HY-161611

    YAP Others
    14-3-3-IN-1 (Compound 2) is an inhibitor for 14-3-3 proteins in Arabidopsis thaliana, with an IC50 of 1.21 μM. 14-3-3-IN-1 exhibits different inhibitory activities against different 14-3-3 isomers. 14-3-3-IN-1 promotes the closure of stomata on leaves .
    14-3-3-IN-1
  • HY-P5885

    PKC Others
    PKCη pseudosubstrate inhibitor,myristoylated is cell permeable and can be used to study the mechanism of action of PKCη .
    PKCη pseudosubstrate inhibitor,myristoylated
  • HY-156125

    Estrogen Receptor/ERR Others
    14-3-3σ/ERα stabilizer-1 (Compound 181) is a covalent 14-3-3σ/ERα stabilizer. 14-3-3σ/ERα stabilizer-1 can be used for research of molecular glues .
    14-3-3σ/ERα stabilizer-1
  • HY-19210

    Endothelin Receptor Cardiovascular Disease
    SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
    SB-209670
  • HY-19263

    Endothelin Receptor Cardiovascular Disease
    BMS-193884 is a selective, orally active, and competitive ETA antagonist with 10000-fold greater affinity for the human ETA receptor (Ki=1.4 nM) than for the ETB receptor .
    BMS-193884
  • HY-153463

    SC0062

    Endothelin Receptor Cardiovascular Disease Neurological Disease Metabolic Disease Inflammation/Immunology
    Diosuxentan is an inhibitor of ETA. Diosuxentan can be used in research for cardiovascular, renal and neuronal inflammation diseases .
    Diosuxentan
  • HY-10383

    Endothelin Receptor Cardiovascular Disease Metabolic Disease
    J-104132 (L-753037) is a potent, orally active, selective and competitive ETA/ETB receptor antagonist with Ki of 0.034 nM for ETA and 0.104 nM for ETB receptors. J-104132 inhibits Endothelin-1 (ET-1) (HY-P71446)-induced signaling and vascular contractions in vitro. J-104132 alleviates hypertension, vascular remodeling, and diabetic endothelial dysfunction in vivo by dual ETA/ETB blockade. J-104132 can be used for research on diabetic vascular complications [1][3].
    J-104132

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