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Results for "

TR-FRET

" in MedChemExpress (MCE) Product Catalog:

33

Inhibitors & Agonists

3

Fluorescent Dye

1

Peptides

1

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108435
    GNE-049
    Maximum Cited Publications
    7 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively .
    GNE-049
  • HY-108696
    GNE-781
    5 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .
    GNE-781
  • HY-101027
    GSK 4027
    2 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Inflammation/Immunology Cancer
    GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK 4027
  • HY-152231
    BODIPY FL thalidomide

    		Fluorescent Dye Ligands for E3 Ligase Others
    BODIPY FL thalidomide is a high-affinity and selective human cereblon (CRBN)-targeting fluorescent probe with a Kd of 3.6 nM. BODIPY FL thalidomide enables use as a probe in time-resolved fluorescence resonance energy transfer (TR-FRET) binding assays for cereblon ligands. BODIPY FL thalidomide supports development of highly sensitive, selective, stable cereblon TR-FRET binding assays (Ex/Em = 502/510 nm) .
    BODIPY FL thalidomide
  • HY-101027A
    GSK4028
    1 Publications Verification

    		 Epigenetic Reader Domain Histone Acetyltransferase Inflammation/Immunology Cancer
    GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK4028
  • HY-A0298
    EZH2-IN-2

    		Histone Methyltransferase Cancer
    EZH2-IN-2 (Example 69) is a EZH2 inhibitor with an IC50 and a TR-FRET IC50 of 64 nM and 20 nM. EZH2-IN-2 can be used for the research of cancer or precancerous condition related to EZH2 activity .
    EZH2-IN-2
  • HY-139561
    KDM2B-IN-2

    		Histone Demethylase Inflammation/Immunology Cancer
    KDM2B-IN-2, a potent histone demethylase (kdm2b) inhibitor with an IC50 of 0.021 μM in a KDM2B TR-FRET assay. KDM2B-IN-2 can be used for hyperproliferative diseases research .
    KDM2B-IN-2
  • HY-D2413
    BODIPY FL VH032

    BODIPY FL PEG4-VH032

    		 Fluorescent Dye Others
    BODIPY FL VH032 is a high-affinity VHL fluorescent probe with a Kd value of 3.01 nM. BODIPY FL VH032 consists of von Hippel-Lindau (VHL) ligand VH032 (HY-120217) and BODIPY FL (HY-43520). BODIPY FL VH032 can be used for time-resolved fluorescence resonance energy transfer (TR-FRET) detection for high-throughput identification and characterization of VHL ligands with maximum excitation emission wavelength: 504/520 nm .
    BODIPY FL VH032
  • HY-155312
    NKG2D-IN-2

    		C-type Lectin-like Receptors (CTLRs) Cancer
    NKG2D-IN-2 (compound 47) is a natural killer group 2D receptor (NKG2D) inhibitor with IC50s of 0.1 µM and 0.2 µM in NKG2D/MICA and ULBP6 TR-FRET assays, respectively .
    NKG2D-IN-2
  • HY-157558
    KDRLKZ-1

    8SGE

    		 Ligands for E3 Ligase Others
    KDRLKZ-1 is a KLHDC2 ligand (Kd = 0.36 μM), with IC50s of 0.21 μM and 0.31 μM in alphaLISA and time-resolved fluorescence resonance energy transfer (TR-FRET) displacement assays .
    KDRLKZ-1
  • HY-114411
    ERRγ inverse agonist 1

    		Estrogen Receptor/ERR Cancer
    ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC50 value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer .
    ERRγ inverse agonist 1
  • HY-160501
    DS17

    		Molecular Glues CDK Cancer
    DS17 is a molecular glue that acts as a potent degrader of cyclin K, with an EC50 of 13 nM. DS17 plays an important role in cancer research .
    DS17
  • HY-D2274
    EZH2-AF647

    		Fluorescent Dye Others
    EZH2-AF647 is a fluorescent probe derived from UNC2239 that improves receptor TR-FRET properties by using Alexa 647 dye .
    EZH2-AF647
  • HY-153114
    HEC96719

    		FXR Inflammation/Immunology
    HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis .
    HEC96719
  • HY-176955
    ER degrader 12

    		Estrogen Receptor/ERR Cancer
    ER degrader 12 (Example 1) is an estrogen receptor (ER) degrader with IC50 values for ERα and ERβ of 2.3 and 80.2 nM respectively (TR-FRET experiment). ER degrader 12 inhibits the proliferation of MCF-7 cells, with an IC50 of 1.53 nM. ER degrader 12 can be used for research on breast cancer .
    ER degrader 12
  • HY-168536
    SJ46411

    		Ligands for E3 Ligase Cancer
    SJ46411 is a potent ligand for KLHDC2, with a Kd of ~260 nM measured by isothermal titration calorimetry (SPR Kd = 0.5 μM, TR-FRET IC50 = 3.9 μM, ΔTm = 6.0 °C) .
    SJ46411
  • HY-149245
    Keap1-Nrf2-IN-15

    		Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-15 (Compound 24a) is a potent Keap1-Nrf2 protein-protein interaction inhibitor with IC50s of 77 nM and 2.5 nM in FP assay and TR-FRET assay, respectively .
    Keap1-Nrf2-IN-15
  • HY-168713
    LZ-007

    		FXR Metabolic Disease
    LZ-007 is an agonist for farnesoid X receptor (FXR) with an EC50 of 51 nM measuring by TR-FRET assay, or an EC50 of 76 nM in HepG2 cell. LZ-007 exhibits good pharmacokinetic characheristics in SD rats. LZ-007 ameliorates western diet and CCl4 (HY-Y0298)-induced mice metabolic dysfunction-associated steatohepatitis
    LZ-007
  • HY-146578
    Keap1-Nrf2-IN-8

    		Keap1-Nrf2 Inflammation/Immunology
    Keap1-Nrf2-IN-8 (compound 12d) is a potent Keap1-Nrf2 PPI (Keap1-Nrf2 protein−protein interaction) inhibitor with IC50s of 64.5 nM and 14.2 nM for FP and TR-FRET assays, respectively. Keap1-Nrf2-IN-8 significantly increases the mRNA levels of Nrf2 downstream genes, GSTM3, HMOX2 and NQO1 .
    Keap1-Nrf2-IN-8
  • HY-186126
    CDK2 modulator 1

    		CDK Cancer
    CDK2 modulator 1 is a CDK2 modulator with an EC50 < 100 nM and an Emax > 100% of positive control in a TR-FRET proximity assay. CDK2 modulator 1 induces ternary complex formation with CDK2/CCNE1 and CRBN. CDK2 modulator 1 can be used for the research of cancer .
    CDK2 modulator 1
  • HY-162096
    Keap1-Nrf2-IN-17

    		Keap1-Nrf2 Cancer
    Keap1-Nrf2-IN-17 (compound 18) is a potent inhibitor of Keap1-Nrf2 protein-protein interaction .
    Keap1-Nrf2-IN-17
  • HY-101027R
    GSK 4027 (Standard)

    		Epigenetic Reader Domain Reference Standards Histone Acetyltransferase Inflammation/Immunology Cancer
    GSK 4027 (Standard) is the analytical standard of GSK 4027 (HY-101027). This product is intended for research and analytical applications. GSK 4027 is a chemical probe for the PCAF/GCN5 bromodomain with an pIC50 of 7.4±0.11 for PCAF in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK 4027 (Standard)
  • HY-101027AR
    GSK4028 (Standard)

    		Epigenetic Reader Domain Reference Standards Histone Acetyltransferase Inflammation/Immunology Cancer
    GSK4028 (Standard) is the analytical standard of GSK4028 (HY-101027A). This product is intended for research and analytical applications. GSK4028 is the enantiomeric negative control of GSK4027, which is a PCAF/GCN5 bromodomain chemical probe, the pIC50 of GSK4028 is 4.9 in a time-resolved fluorescence resonance energy transfer (TR-FRET) assay.
    GSK4028 (Standard)
  • HY-108435R
    GNE-049 (Standard)

    		Reference Standards Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-049 (Standard) is the analytical standard of GNE-049 (HY-108435). This product is intended for research and analytical applications. GNE-049 is a highly potent and selective CBP inhibitor with an IC50 of 1.1 nM in TR-FRET assay. GNE-049 also inhibits BRET and BRD4(1) with IC50s of 12 nM and 4200 nM, respectively .
    GNE-049 (Standard)
  • HY-181345
    OP-1690

    		Estrogen Receptor/ERR Cancer
    OP-1690 is a complete estrogen receptor (ERα) antagonist (CERAN), with pIC50 values of 7.5 and 7.9 in alkaline phosphatase (AP) activity assay and TR-FRET assay, respectively. OP-1690 modulates receptor function by inducing ERα tetramerization, effectively induces ERα degradation, inhibits target gene transcription, but exhibits low antiproliferative potency. OP-1690 can be used for breast cancer research .
    OP-1690
  • HY-108696R
    GNE-781 (Standard)

    		Reference Standards Epigenetic Reader Domain Histone Acetyltransferase Cancer
    GNE-781 (Standard) is the analytical standard of GNE-781 (HY-108696). This product is intended for research and analytical applications. GNE-781 is an orally active, highly potent and selective CBP inhibitor with an IC50 of 0.94 nM in TR-FRET assay. GNE-781 also inhibits BRET and BRD4(1) with IC50s of 6.2 nM and 5100 nM, respectively. GNE-781 displays antitumor activity in an MOLM-16 AML xenograft model .
    GNE-781 (Standard)
  • HY-182026
    FXR agonist 17

    		FXR G protein-coupled Bile Acid Receptor 1 TNF Receptor Reactive Oxygen Species (ROS) Inflammation/Immunology
    FXR agonist 17 is an orally active, steroidal FXR agonist with EC50 values of 42.2 nM (TR-FRET) and 176.4 nM (luciferase reporter assay), respectively. FXR agonist 17 activates TGR5 (EC50 = 2.6 μM) but does not activate hMRGPRX4. FXR agonist 17 exerts anti-inflammatory, hepatoprotective and antifibrotic effects, improves the non-alcoholic steatohepatitis (NAFLD) activity score and reduces the severity of liver fibrosis. FXR agonist 17 can be used for the research of NAFLD, cholestatic liver disease and liver fibrosis .
    FXR agonist 17
  • HY-183344
    IL-1β-IN-4

    		Interleukin Related Inflammation/Immunology
    IL-1β-IN-4 is a selective IL-1β competitive binder. IL-1β-IN-4 interferes with the interaction between IL-1β and its cognate receptor IL-1R1, with an IC50 of 8.3 μM. IL-1β-IN-4 can be used in studies related to inflammatory and immune diseases .
    IL-1β-IN-4
  • HY-182449
    CCT365386

    		Bcl-2 Family Cancer
    CCT365386 is a BCL6 inhibitor. CCT365386 serves as an optimized lead compound for cell-active BCL6 degraders (including CCT369260 (HY-129188)). CCT365386 can be used in the research of B-cell lymphoma .
    CCT365386
  • HY-P11621
    JWP24

    		E1/E2/E3 Enzyme Cancer
    JWP24 is the first cell membrane-permeable peptide inhibitor of MAGE-A4, with an IC50 of 200 nM against human MAGE-A4. JWP24 binds to intracellular targets while retaining binding activity, disrupts the interaction between MAGE-A4 and RAD18, and does not induce cytotoxicity at effective concentrations. JWP24 is applicable for cancer-related research .
    JWP24
  • HY-122222
    MRL20

    		PPAR Others
    MRL20 is a PPARγ constitutive and allosteric agonist. MRL20 enhances the interaction between PPARγ and the co-activating peptide of TRAP220, with its EC50 being 10 nM. Even after being covalently blocked in the constitutive pocket by GW9662 (HY-16578) or T0070907 (HY-13202), MRL20 can still strengthen the interaction between PPARγ and TRAP220, with EC50 values of 176 and 440 nM respectively. MRL20 fails to completely inhibit its cell activation effect. MRL20 can be used to study the allosteric regulatory mechanism of PPARγ .
    MRL20
  • HY-D3393
    JQ1-FITC TFA

    		Fluorescent Dye Epigenetic Reader Domain Cancer
    JQ1-FITC TFA is a BRD4-binding fluorescent tracer. JQ1-FITC TFA binds to BRD4 BD1, BD2, recombinant bromodomains, and endogenous BRD4 in cell lysates. JQ1-FITC TFA can be used for the research of breast cancer and cancer (Ex/Em = 495/525 nm) .
    JQ1-FITC TFA
  • HY-181530
    IAP ligand 6

    		IAP Cancer
    IAP ligand 6 (A250) is an IAP ligand with a Ka value of 0.1 μM for the human XIAP BIR3 domain. IAP ligand 6 binds to the XIAP BIR3 domain and serves as an alkynylpyridine scaffold for the preparation of TEAD degraders that recruit IAP. IAP ligand 6 is applicable to research related to mesothelioma .
    IAP ligand 6

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