Scientific Reviews
Product Guides
Blogs
Topics
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
11 Results for "
VHL-dependent
" in MedChemExpress (MCE) Product Catalog:
Products (11)
11 Results for "VHL-dependent" in MCE Product Catalog:
1
1 Cited Publications
Target:
Research Areas:
GNE-987 is a VHL-dependent BRD4 PROTAC degrader. GNE-987 exhibits picomolar cell BRD4 degradation activity (DC50=0.03 nM for EOL-1 AML cell line). GNE-987 binds equipotently to the BD1 and BD2 bromodomains of BRD4 with low nanomolar affinities (IC50=4.7 and 4.4 nM, respectively). GNE-987 can be used for the research of cancer .
YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd of 35 nM. YX-02-030 recruits the VHL E3 ligase to form a ternary complex, leading to ubiquitination and proteasome-mediated degradation of MDM2. YX-02-030 inhibits MDM2-p53 and VHL-HIF1α binding with IC50 values of 63 and 1350 nM. YX-02-030 activates TAp73, upregulates p53 family target genes and induces apoptosis. YX-02-030 demonstrates on-target efficacy in TNBC xenograft-bearing mice, extending survival without normal cell toxicity .
Target:
Research Areas:
PROTAC_ERRα is a potent and selective ERRα PROTAC degrader (DC50: ~100 nM in MCF-7 cells). PROTAC_ERRα recruits the VHL E3 ubiquitin ligase to ERRα, inducing ERRα ubiquitination and proteasomal degradation in a VHL-dependent manner. PROTAC_ERRα can be used in breast cancer-related research .
Cat. No.: HY-155506
PROTAC NAMPT Degrader-32 is a PROTAC degrader targeting NAMPT with an IC50 of 2.14 nM. PROTAC NAMPT Degrader-32 induces proteasome-dependent degradation of NAMPT and induces apoptosis in ovarian cancer cells (apoptosis). PROTAC NAMPT Degrader-32 can be used in research related to ovarian cancer .
Cat. No.: HY-179582
Target:
Research Areas:
PROTAC DNPH1 Degrader 1 is a potent PROTAC DNPH1 degrader with a DC50 of 28 nM. PROTAC DNPH1 Degrader 1 mediates proteasome- and VHL-dependent DNPH1 knockdown, drives DNPH1 ubiquitination and proteasomal degradation. PROTAC DNPH1 Degrader 1 can be used for the research of brca1 mutant cancer .
Cat. No.: HY-178467
PROTAC FAK degrader 4 is a potent FAK PROTAC degrader with a DC50 of 3.6 nM. PROTAC FAK degrader 4 induces FAK ubiquitination and degradation via the VHL-dependent ubiquitin-proteasome pathway. PROTAC FAK degrader 4 inhibits cell proliferation, colony formation, migration and invasion. Combination of PROTAC FAK degrader 4 with Cisplatin (HY-17394) enhances chemosensitivity. PROTAC FAK degrader 4 can be used in research related to breast cancer .
Cat. No.: HY-158684A
CAS No.: 3049077-01-9
Target:
Research Areas:
(4R,5S)-YX-02-030 is an isomer of YX-02-030 (HY-158684). YX-02-030 is a VHL-dependent MDM2 PROTAC degrader with a Kd value of 35 nM .
Cat. No.: HY-189269
PROTAC JNK1 Degrader-2 is a VHL-recruiting JNK1 PROTAC degrader with a DC50 of 4.90 nM. It selectively induces JNK1 degradation via the VHL-dependent ubiquitin-proteasome pathway and inhibits TGF-β1-induced epithelial-mesenchymal transition. PROTAC JNK1 Degrader-2 can be used for research on organ fibrosis and tumor metastasis .
Cat. No.: HY-181134
CAS No.: 2715104-46-2
PROTAC HMGCR Degrader-2 is a HMGCR PROTAC degrader with an IC50 value of 0.25 μM. PROTAC degrades HMGCR-2 in Insig-silenced HepG2 cells with a DC50 of 0.12 μM. PROTAC HMGCR Degrader-2 takes PROTAC HMGCR Degrader-1 (HY-171823) as the oral prodrug. PROTAC HMGCR Degrader-2 degrades HMGCR by the VHL-dependent ubiquitin-proteasome system and reduces cellular cholesterol in HepG2 cells. PROTAC CDK2/4/6 Degrader-2 can be used for hyperlipidemia research .
Cat. No.: HY-171823
CAS No.: 2715104-45-1
Target:
Research Areas:
PROTAC HMGCR Degrader-1 is an orally active HMGCR PROTAC degrader with IC50 of 1.32 μM. PROTAC HMGCR Degrader-1 is a lactone prodrug of PROTAC HMGCR Degrader-2 (HY-181134). PROTAC HMGCR Degrader-1 achieves high plasma exposure of the active ingredient leading to robust HMGCR degradation and demonstrating promising cholesterol-lowering efficacy in vivo. PROTAC HMGCR Degrader-1 can be used for hyperlipidemia research .
Cat. No.: HY-187136
CAS No.: 3004503-11-8
Research Areas:
EZH2-IN-13-CO-C9-COOH is a target protein ligand-linker conjugate. EZH2-IN-13-CO-C9-COOH can be used to synthesize PROTAC NUCC-0226272 (HY-157844) .
- 1
-
-
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
