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TR-FRET assay

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Bcl-2 Family (1) C-type Lectin-like Receptors (CTLRs) (1) CDK (1) E1/E2/E3 Enzyme (1) Epigenetic Reader Domain (9) Estrogen Receptor/ERR (2) Fluorescent Dye (2) FXR (3) G protein-coupled Bile Acid Receptor 1 (1) Histone Acetyltransferase (8) Histone Demethylase (1) IAP (1) Interleukin Related (1) Keap1-Nrf2 (3) Ligands for E3 Ligase (2) PPAR (1) Reactive Oxygen Species (ROS) (1) Reference Standards (4) TNF Receptor (1)
By Research Areas:	Cancer (18) Inflammation/Immunology (10) Metabolic Disease (1)
Click Chemistry:	PROTAC Synthesis (1)

Inhibitors & Agonists

Fluorescent Dyes

Peptides

Click Chemistry

Targets Recommended: Biochemical Assay Reagents

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 .

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 .

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.

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 K_d 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) .

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.

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 .

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 .

HY-157558

KDRLKZ-1 8SGE	Ligands for E3 Ligase	Others
KDRLKZ-1 is a KLHDC2 ligand (K_d = 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 .

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 .

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 .

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 .

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

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 .

HY-186126

CDK2 modulator 1	CDK	Cancer
CDK2 modulator 1 is a CDK2 modulator with an EC₅₀ < 100 nM and an E_max > 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 .

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 .

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.

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.

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 .

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 .

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 .

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 .

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 .

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 .

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 .

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) .

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 .

HY-181530

IAP ligand 6	IAP	Cancer
IAP ligand 6 (A250) is an IAP ligand with a K_a 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 .

JQ1-FITC TFA	Fluorescent Dyes
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) .

Cat. No.	Product Name	Target	Research Area

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 .

Cat. No.	Product Name		Classification

HY-181530

IAP ligand 6		PROTAC Synthesis
IAP ligand 6 (A250) is an IAP ligand with a K_a 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 .

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