| Identification | Back Directory | [Name]
INDEX NAME NOT YET ASSIGNED | [CAS]
2362575-45-7 | [Synonyms]
| [Molecular Formula]
C51H69N7O10S | [MDL Number]
MFCD32705129 | [Molecular Weight]
972.2 |
| Chemical Properties | Back Directory | [Boiling point ]
1152.7±65.0 °C(Predicted) | [density ]
1.265±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
Soluble in DMSO | [form ]
Solid | [pka]
10.75±0.40(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Uses]
CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544))[1]. | [Biological Activity]
CRBN-6-5-5-VHL is a cell-permeable and highly potent heterodimerizer comprising E3 ligases recruiting ligandsnamelypomalidomide and VH032-amine th at efficiently knocks down Cereblon (CRBN). CRBN-6-5-5-VHL readily forms heteroternary complex and selectively induces CRBN ubiquitination and proteasomal degradation over VHL in a time- and dose-dependent fashion (0.001 to 1 μM). Higher concentrations (10 μM) causes the degradation of neo-substrates IKZF1 and IKZF3 with no effect on pVHL30 or pVHL19 levels. | [IC 50]
Cereblon: 1.5 nM (DC50) | [storage]
Store at -20°C | [References]
[1] Christian Steinebach, et al. PROTAC-mediated crosstalk between E3 ligases. Chem Commun (Camb). 2019 Feb 5;55(12):1821-1824. DOI:10.1039/c8cc09541h |
|
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|