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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
37 Results for "
TR-FRET
" in MedChemExpress (MCE) Product Catalog:
Products (37)
37 Results for "TR-FRET" in MCE Product Catalog:
7
7 Publications Verification
Research Areas:
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 .
6
6 Cited Publications
Research Areas:
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 .
2
2 Cited Publications
Research Areas:
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.
1
1 Cited Publications
Research Areas:
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.
1
1 Cited Publications
Cat. No.: HY-155659
Purity: 99.86%
Target:
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4A7C-301 is a blood-brain barrier-permeable Nurr1 agonist, with IC50 values of 48.22 nM and 107.71 nM for binding to Nurr1-LBD in the [ 3H]-CQ competition assay and TR-FRET assay, respectively. The EC50 of 4A7C-301 for activating Nurr1 transcriptional activity is 6.53 μM, and its EC50 in N27-A dopaminergic cells is approximately 0.2 μM. 4A7C-301 binds directly to Nurr1-LBD, enhances the transcriptional function of Nurr1, and restores the reduction of Nurr1 protein induced by MPP + or αSyn. 4A7C-301 alleviates oxidative stress and mitochondrial dysfunction, protects midbrain dopaminergic neurons, inhibits microglial activation, and restores impaired autophagic flux. 4A7C-301 can be used in studies related to neuroprotection and Parkinson's disease .
1
1 Cited Publications
Research Areas:
ERRα ligand 2 is a ERRα ligand with a target IC50 of 5.67 nM. PROTAC ERRα ligand 2 blocks the protein-protein interaction between ERRα and PGC-1α. PROTAC ERRα ligand 2 can be used for synthesis of PROTACs .
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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) .
Cat. No.: HY-A0298
CAS No.: 2238821-31-1
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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 .
Cat. No.: HY-D2413
CAS No.: 2770675-66-4
Synonyms: BODIPY FL PEG4-VH032
Cat. No.: HY-155312
Research Areas:
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 .
Cat. No.: HY-114411
CAS No.: 2316832-86-5
Target:
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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 .
Cat. No.: HY-157558
Synonyms: 8SGE
Target:
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KDRLKZ-1 (8SGE) is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 0.36 μM), with an IC50 of 0.21 μM and 0.31 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-1 binds to the substrate-binding pocket of the KLHDC2 kelch domain, mimics the interaction of natural substrates and displaces them. KDRLKZ-1 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-1 can be used in scaffold ligand research for PROTAC degraders targeting KLHDC2 .
Cat. No.: HY-160501
CAS No.: 3068546-95-9
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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 .
Cat. No.: HY-157559
Target:
Research Areas:
KDRLKZ-2 is a small-molecule ligand of KLHDC2 E3 ligase (Kd = 95 nM), with an IC50 of 68 nM and 0.1 μM in alphaLISA and TR-FRET assays, respectively. KDRLKZ-2 binds to the substrate-binding pocket of the kelch domain of KLHDC2, mimics the interaction of natural substrates and displaces them. KDRLKZ-2 acts as an oligomer disruptor, regulates the oligomerization of the KLHDC2-EloB-EloC complex, and induces the dissociation of tetramers into smaller components. KDRLKZ-2 can be used in scaffold ligand studies of PROTAC degraders targeting KLHDC2 .
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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 .
Cat. No.: HY-176955
CAS No.: 2376991-14-7
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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 .
Cat. No.: HY-168536
CAS No.: 3086104-39-1
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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) .
Cat. No.: HY-149245
CAS No.: 2456295-45-5
Target:
Research Areas:
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 .
Cat. No.: HY-168713
CAS No.: 2920000-23-1
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Research Areas:
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
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
