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Results for "

heterodimerization

" in MedChemExpress (MCE) Product Catalog:

27

Inhibitors & Agonists

7

Peptides

3

Inhibitory Antibodies

1

Natural
Products

1

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-D0844
    Glutathione oxidized
    5+ Cited Publications

    L-Glutathione oxidized; GSSG; Oxiglutatione

    		 Endogenous Metabolite Reactive Oxygen Species (ROS) Metabolic Disease
    Glutathione oxidized (L-Glutathione oxidized) is produced by the oxidation of glutathione. Detoxification of reactive oxygen species is accompanied by production of glutathione oxidized. Glutathione oxidized can be used for the research of sickle cells and erythrocytes .
    Glutathione oxidized
  • HY-B0527A
    Amitriptyline hydrochloride
    5+ Cited Publications

    		 Serotonin Transporter 5-HT Receptor mAChR Histamine Receptor Adrenergic Receptor Trk Receptor Sodium Channel Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline hydrochloride is an orally active tricyclic antidepressant (TCA). Amitriptyline hydrochloride mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline hydrochloride is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline hydrochloride can reduce inflammation, angiogenesis and fibrosis. Amitriptyline hydrochloride binds to DAT (with Ki = 2.58 μM). Amitriptyline hydrochloride has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline hydrochloride can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline hydrochloride
  • HY-P99412
    Lusvertikimab
    1 Publications Verification

    OSE-127

    		 Interleukin Related Cancer
    Lusvertikimab (OSE-127) is a humanized IL7R monoclonal antibody. Lusvertikimab is not internalized by target cells and prevents IL7R heterodimerization and subsequent downstream signaling. Lusvertikimab has anti-leukemic efficacy and has the potential for B cell precursor acute lymphoblastic leukemia (BCP-ALL) research .
    Lusvertikimab
  • HY-B0527
    Amitriptyline
    5+ Cited Publications

    		 Serotonin Transporter Trk Receptor Sodium Channel 5-HT Receptor Histamine Receptor Adrenergic Receptor mAChR Potassium Channel Dopamine Transporter Apoptosis Neurological Disease Inflammation/Immunology Endocrinology
    Amitriptyline is an orally active tricyclic antidepressant (TCA). Amitriptyline mainly exerts its antidepressant effect by blocking SERT (Ki = 3.45 nM) and NET (Ki = 13.3 nM), thereby increasing the concentrations of 5-hydroxytryptamine (5-HT) and norepinephrine (NE) in the synaptic cleft. Amitriptyline is also an agonist at α2A and TrkA/TrkB receptors, thereby exerting analgesic and neurotrophic activities (inhibiting cell apoptosis). Amitriptyline can reduce inflammation, angiogenesis and fibrosis. Amitriptyline binds to DAT (with Ki = 2.58 μM). Amitriptyline has high affinity for a series of receptors and can antagonize muscarinic cholinergic receptors (M1/M2/M3/M4/M5 receptors) (Ki = 11-24 nM), H1 receptors (Ki = 0.5-1.1 nM), adrenergic α1 receptors (Ki = 4.4 nM), etc., resulting in a series of side effects. Amitriptyline can block sodium channels and hERG potassium channel (IC50 = 4.78 μM) and it has cardiotoxicity .
    Amitriptyline
  • HY-116248
    Ro 41-5253
    3 Publications Verification

    		 RAR/RXR Apoptosis Cancer
    Ro 41-5253 is an orally active selective retinoic acid receptor alpha (RARα) antagonist. Ro 41-5253 can bind RARα without inducing transcription or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 can inhibit cancer cell proliferation and induce apoptosis, has antitumor activity .
    Ro 41-5253
  • HY-110266
    GN44028
    5+ Cited Publications

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    GN44028 is a potent and orally active hypoxia inducible factor (HIF)-1α inhibitor, with an IC50 of 14 nM. GN44028 inhibits hypoxia-induced HIF-1α transcriptional activity without suppressing HIF-1α mRNA expression, HIF-1α protein accumulation, or HIF-1α/HIF-1β heterodimerization. GN44028 can be used in the research of cancers .
    GN44028
  • HY-114421
    FKBP12 PROTAC dTAG-13
    Maximum Cited Publications
    9 Publications Verification

    dTAG-13

    		 PROTACs FKBP Cancer
    FKBP12 PROTAC dTAG-13 (dTAG-13), a PROTAC-based heterobifunctional degrader, is a selective degrader of FKBP12 F36V with expression of FKBP12F36V in-frame with a protein of interest. FKBP12 PROTAC dTAG-13 effectively engages FKBP12 F36V and CRBN, thereby selectively degrading FKBP12 F36V .
    FKBP12 PROTAC dTAG-13
  • HY-159644
    Casdatifan

    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-103689
    Cucurbit[8]uril

    		Biochemical Assay Reagents Others
    Cucurbit[8]uril is a potent, low toxicity and orally active supramolecular inducer of protein heterodimerization. Cucurbit[8]uril induces heterodimerization of methylviologen and naphthalene functionalized proteins. Cucurbit[8]uril can induce energy transfer .
    Cucurbit[8]uril
  • HY-18371
    TC-S 7009
    1 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Inflammation/Immunology
    TC-S 7009 is a potent and selective HIF-2α inhibitor with a Kd of 81 nM. TC-S 7009 is more selective for HIF-2α than HIF-1α (Kd ? 5 μM). TC-S 7009 disrupts HIF-2α heterodimerization, decreases DNA-binding activity, and reduces HIF-2α target gene expression .
    TC-S 7009
  • HY-P1420
    TAT-cyclo-CLLFVY
    2 Publications Verification

    		 HIF/HIF Prolyl-Hydroxylase Cancer
    TAT-cyclo-CLLFVY is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM .
    TAT-cyclo-CLLFVY
  • HY-128845
    PROTAC CRBN Degrader-1

    		PROTACs E1/E2/E3 Enzyme Cancer
    PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other . (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))
    PROTAC CRBN Degrader-1
  • HY-126316
    Zapalog
    1 Publications Verification

    		 FKBP Others
    Zapalog is a photocleavable small-molecule heterodimerizer that can be used to repeatedly initiate, and instantaneously terminate, a physical interaction between two target proteins. Zapalog dimerizes any two proteins tagged with the FKBP and DHFR domains until exposure to light causes its photolysis .
    Zapalog
  • HY-160053
    Gint4.T aptamer sodium

    		PDGFR Cancer
    Gint4.T aptamer sodium is a nuclease-resistant RNA aptamer-based antagonist targeting platelet-derived growth factor receptor beta (PDGFRβ) (Kd: 9.6 nM). Gint4.T aptamer sodium inhibits PDGFRβ heterodimerization and EGFR transactivation. It can significantly inhibit cell migration and proliferation, induce differentiation and prevent tumor growth in vivo. Gint4.T aptamer sodium specifically inhibits PDGFRβ-mediated tropism of mesenchymal stem cells (MSCs) toward the tumor microenvironment .
    Gint4.T aptamer sodium
  • HY-112374
    NPAS3-IN-1

    		HIF/HIF Prolyl-Hydroxylase Neurological Disease
    NPAS3-IN-1 is a potent inhibitor of NPAS3-ARNT heterodimerization and regulates NPAS3 transcription by disrupting the heterodimerization of NPAS3 with ARNT at the cellular level .
    NPAS3-IN-1
  • HY-149085
    XS-060

    		RAR/RXR Cancer
    XS-060 is a potent anticancer agent and RXRα antagonist. XS-060 significantly induces RXRα-dependent mitotic arrest by inhibiting pRXRα-PLK1 interaction. XS-060 inhibits p-RXRα interaction with PLK1 but has no effect on RXRα heterodimerization with RARγ. XS-060 inhibits the in situ interaction between p-RXRα and PLK1 at the centrosome .
    XS-060
  • HY-118998
    TX2-121-1

    		PROTACs EGFR ERK Akt Cancer
    TX2-121-1 is a potent and selective Her3 (ErbB3) degrader that contains a hydrophobic adamantane moiety. TX2-121-1 has an IC50 of 49 nM for Her3. TX2-121-1 inhibits Her3-dependent signaling and heterodimerization of Her3. TX2-121-1 has the ability to inhibit cell proliferation. TX2-121-1 can be used in the study of tumors. (Pink: Her3 inhibitor (HY-164988); Black: Linker; Blue: Adamantane (HY-N2427)) .
    TX2-121-1
  • HY-162793
    RdRP-IN-8

    		DNA/RNA Synthesis Influenza Virus Infection
    RdRP-IN-8 (compound 45) is an anti-influenza virus compound. RdRP-IN-8 inhibits viral RNA-dependent RNA polymerase (RdRP) activity by disrupting heterodimerization of PA and PB1 subunits (EC50=0.13 μM) .
    RdRP-IN-8
  • HY-P11272
    Tasronetide

    FTX-101

    		 VEGFR Neurological Disease
    Tasronetide (FTX-101) is a highly selective inhibitor toward the NRP1/Plexin-A1 receptor system, and displays no significant activity on other targets. Tasronetide intercalates within the transmembrane domains of Plexin-A1 and NRP1 of oligodendrocytes, interferes with the heterodimerization of the co-receptor system, effectively disrupts the NRP1/Plexin-A1 receptor complex and mitigates the inhibitory influence of Sema3A on oligodendrocyte migration and differentiation, thereby facilitating increased myelin sheathing around axons. Tasronetide is designed to enhance the recruitment and maturation of oligodendrocyte precursors and can be used for Chronic Op c Neuropathy research .
    Tasronetide
  • HY-P1420A
    TAT-cyclo-CLLFVY TFA

    		HIF/HIF Prolyl-Hydroxylase Cancer
    TAT-cyclo-CLLFVY TFA is a cyclic peptide inhibitor of HIF-1 heterodimerization that inhibits hypoxia signaling in cancer cells. TAT-cyclo-CLLFVY TFA disrupts HIF-1α/HIF-1β protein-protein interaction with an IC50 of 1.3 μM .
    TAT-cyclo-CLLFVY TFA
  • HY-P3223A
    Biphalin acetate

    		Opioid Receptor Neurological Disease
    Biphalin acetate, a BBB-penetrable opioid peptide analog, contains two active enkephalin pharmacophores.Biphalin acetate has high affinity for opioid receptors. Biphalin acetate shows analgesic effect in acute, neuropathic, and chronic animal pain models. Biphalin acetate is also an antiviral, antiproliferative, anti-inflammatory, and neuroprotective agent .
    Biphalin acetate
  • HY-P991243
    MP-RM-1

    		EGFR Akt Cancer
    MP-RM-1 is an antibody-based, non-competitive ErbB-3 inhibitor with a Kd value of 32.7 nM. MP-RM-1 inhibits both ligand-dependent and ligand-independent ErbB-3 activation, blocks ErbB-2/ErbB-3 heterodimerization, induces ErbB-3 internalization and degradation, and suppresses the phosphorylation of downstream Akt. MP-RM-1 exerts its antagonistic effect through a non-competitive mechanism. MP-RM-1 inhibits tumor growth in melanoma and prostate cancer xenograft models in nude mice and reduces the proliferative activity of tumor cells .
    MP-RM-1
  • HY-155543
    Anticancer agent 135

    		Androgen Receptor Cancer
    Anticancer agent 135 (compound 26h) is a potent androgen receptor (AR) antagonist. Anticancer agent 135 can effectively block AR nuclear translocation and inhibit AR/AR-V7 heterodimerization, thereby inhibiting downstream gene transcription. Anticancer agent 135 displays potent robust efficacy in prostate cancer xenograft models .
    Anticancer agent 135
  • HY-121671
    TBTC

    		RAR/RXR Neurological Disease
    TBTC is a selective agonist with the activity of improving behavioral deficits in Alzheimer's disease model mice. TBTC can effectively activate the heterodimerization of RXRα with LXRα or PPARγ. TBTC stimulates the expression of apoE, ABCA1, and ABCG1 genes and reduces Aβ content in cells and animal models .
    TBTC
  • 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
  • HY-103689R
    Cucurbit[8]uril (Standard)

    		Biochemical Assay Reagents Reference Standards Others
    Cucurbit uril (Standard) is the analytical standard of Cucurbit uril (HY-103689). This product is intended for research and analytical applications. Cucurbit uril is a potent, low toxicity and orally active supramolecular inducer of protein heterodimerization. Cucurbit uril induces heterodimerization of methylviologen and naphthalene functionalized proteins. Cucurbit uril can induce energy transfer .
    Cucurbit<sup>[8]</sup>uril (Standard)
  • HY-P991881
    KY1070

    		TGF-β Receptor Hepcidin Ferroportin Cardiovascular Disease
    KY1070 is a fully human anti-BMP6 antibody with a Kd of 0.00014 μM against the human BMP6. It exhibits high specificity for BMP6, showing no cross-reactivity with other members of the BMP family, and effectively inhibits BMP6-induced BMP receptor heterodimerization and hepcidin expression. KY1070 modulates Ferroportin expression on erythroid progenitor cells and accelerates erythropoiesis. In rodent anemia models, KY1070 reduces the required dose of erythropoietin (EPO) when used in combination with EPO and enhances the responsiveness of mice with chronic kidney disease (CKD)-associated anemia to EPO treatment. KY1070 is applicable for research on anemia of chronic disease [1] [2].
    KY1070

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