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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
19 Results for "
BRET
" in MedChemExpress (MCE) Product Catalog:
Products (19)
19 Results for "BRET" 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 .
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6 Cited Publications
Cat. No.: HY-18743
CAS No.: 55779-48-1
Category:
Alkaloids Monophenols Animals Other Alkaloids Phenols Polyphenols Disease Research Fields Cancer
Target:
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 .
Synonyms: Coelenterazine 400a; Bisdeoxycoelenterazine
Cat. No.: HY-153948
CAS No.: 1936431-44-5
Research Areas:
CBP-IN-1 is a potent CBP inhibitor with an IC50 of 1.5 nM. CBP-IN-1 also inhibits CBP BRET and BRD4 (1), with IC50 values of 690 nM and 3100 nM, respectively. CBP-IN-1 can be used in oncology and immuno-oncology research .
Synonyms: MK-0751
Target:
Research Areas:
L-692429 (MK-0751) is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 binds to G protein-coupled receptor with a Ki of 63 nM .
Cat. No.: HY-175504
CAS No.: 932544-59-7
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MLS6357 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist. MLS6357 exhibits antagonist activity in the D3R-mediated and the BRET-based β-arrestin recruitment assay with IC50s of 13 and 14 μM, and no activity for other DAR subtypes (D1R/D2R/D4R/D5R) (IC50 > 100 μM). MLS6357 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 17 μM. MLS6357 can be used for the study of neuropsychiatric disorders, including substance use disorder .
Cat. No.: HY-118462A
CAS No.: 2320429-05-6
Synonyms: Coelenterazine 400a hydrochloride; Bisdeoxycoelenterazine hydrochloride
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Coelenteramine (Coelenterazine) 400a hydrochloride, a derivative of Coelenterazine, is a Renilla luciferase (RLuc) substrate. In the presence of Coelenteramine 400a hydrochloride, RLuc can emit blue light at 395 nm . Coelenteramine 400a hydrochloride will causes color change in the bioluminescence reaction of Rluc by replacing the sulfur and oxygen heteroatoms of the methylene bridge. Coelenteramine 400a hydrochloride provides higher signal resolution and can be used in the research of bioluminescence resonance energy transfer (BRET) .
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WF-47-JS03 is a potent, selective and brain-penetrantRET kinase inhibitor with IC50s of 1.7 nM and 5.3 nM for KIF5B-RET transfected Ba/F3 cells and CCDC6-RET transfected LC-2/ad lung cancer cells, respectively. WF-47-JS03 demonstrates >500-fold selectivity against kinase insert domain receptor (KDR) .
Cat. No.: HY-178061
CAS No.: 2598870-24-5
APS03118 is an orally active, potent and selective rearranged during transfection (RET) inhibitor. APS03118 broadly inhibits RET fusions and mutations (including G810, V804, L730, and Y806 variants), with IC50 values predominantly below 1 nM (0.095 nM for WT; ranging from 0.00438 to 5.72 nM for mutants), and demonstrates marked superiority against RET G810 mutations. APS03118 inhibits the entire RET signaling pathway (including RET, Shc, and ERK1/2), with >20-fold selectivity over most off-target kinases (except FLT3 and YES). APS03118 induces complete tumor regression in KIF5B-RET and CCDC6-RET V804 M patient derived xenografts (PDXs) and significantly prolongs survival in an intracranial CCDC6-RET metastasis mice model. APS03118 can be used for selective RET inhibitor (SRI)-resistant, RET-driven cancer research .
Cat. No.: HY-178964
CAS No.: 2760847-82-1
PROTAC RET Degrader 1 (Compound 20) is an orally active and blood-brain barrier-crossing RET PROTAC degrader with DC50 values for RET (WT), RET (G810S), RET (G810C), and RET (G810R) of 1.7, 3, 12, and 21 nM, respectively. PROTAC RET Degrader 1 exhibits potent anti-proliferative activity in cancer cell lines carrying oncogenic RET fusions (such as KIF5B-RET, CCDC6-RET) or mutations (such as RET (C634W)). PROTAC RET Degrader 1 shows significant anti-tumor activity in human tumor xenograft (PDX) mouse models. PROTAC RET Degrader 1 can be used for the study of RET-positive cancers Pink: RET ligand (HY-179308); Blue: CRBN ligand (HY-179307); Black: Linker) .
Cat. No.: HY-10957A
CAS No.: 169188-19-6
Synonyms: MK-0751 hydrochloride
Target:
Research Areas:
L-692429 (MK-0751) hydrochloride is a benzolactam derivative and a nonpeptidyl growth hormone secretagogue (GHS) agonist. L-692429 hydrochloride binds to G protein-coupled receptor with a Ki of 63 nM .
Cat. No.: HY-175505
CAS No.: 2894793-37-2
Target:
Research Areas:
Dopamine D3 receptor antagonist-3 is a D3 dopamine receptor (D3R)-selective positive allosteric modulator (PAM)-antagonist that can cross the blood-brain barrier. Dopamine D3 receptor antagonist-3 exhibits antagonist activity in the D3R-mediated β-arrestin recruitment assay with an IC50 and a Kd of 2.5 μM and 0.49 μM. amine D3 receptor antagonist-3 is also an antagonist in the D3R-mediated Go-BRET assay with an IC50 of 0.34 μM. Dopamine D3 receptor antagonist-3 can be used for the study of neuropsychiatric disorders, including substance use disorder .
Cat. No.: HY-170852
QZ2135 (compound 20) is a RET-targeted PROTAC degrader with in vivo antitumor properties in a Ba/F3-KIF5B-RET-G810C xenograft mouse model. The degradation activities of QZ2135 targeting KIF5B-RET have DC50 values of 4.7 nM (WT), 17.2 nM (V804M), and 73.8 nM (G810C), respectively. QZ2135 is composed of a target protein ligand (red part) RET ligand-3 (HY-170853), an E3 ligase ligand (blue part) Lenalidomide-F (HY-W039233), and a PROTAC Linker (black part) 7-Iodohept-1-yne (HY-W587352), in which the target protein ligand + linker form a conjugate RET Ligand-Linker Conjugate-1 (HY-170854) .
Cat. No.: HY-RS20716
Target:
Research Areas:
Dner Mouse Pre-designed siRNA Set A contains three designed siRNAs for Dner gene (Mouse), as well as a negative control, a positive control, and a FAM-labeled negative control.
Cat. No.: HY-179274
CAS No.: 2759727-47-2
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β2AR agonist 5 (Compound alpha-β2-008) is a β2AR agonist, with an EC50 value of 0.19 nM. β2AR agonist 5 induces the BRET signal. β2AR agonist 5 can be used in the research of asthma and chronic obstructive pulmonary disease .
Cat. No.: HY-108435R
CAS No.: 1936421-41-8
Research Areas:
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 .
Cat. No.: HY-108696R
CAS No.: 1936422-33-1
Research Areas:
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 .
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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
