LLC0424
LLC0424 is a potent and selective cereblon-based PROTAC nuclear receptor-binding SET domain-containing 2 (NSD2) degrader. LLC0424 effectively degraded NSD2 with a DC50 of 20 nM in RPMI-8402 cells. LLC0424 selectively induces NSD2 degradation in a cereblon- and proteasome-dependent fashion. (Blue: CRBN ligand (HY-14658), Black: linker (HY-40002) ; Pink: NSD2 inhibitor (HY-161575) ) [1].
Product Specifications
UNSPSC
12352005
Target
Histone Methyltransferase; PROTACs
Type
Reference compound
Related Pathways
Epigenetics; PROTAC
Applications
Cancer-programmed cell death
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/llc0424.html
Purity
98.42
Solubility
DMSO : ≥ 100 mg/mL
Smiles
O=C(N1)COC2=C1C=CC(C(N(C3CC3)CC4=CC=C(C(NC5=CC=C(C(NC6CCN(C7=CC8=C(C(N(C(C(N9)=O)CCC9=O)C8=O)=O)C=C7)CC6)=O)C=C5)=O)C=C4)=O)=C2
Molecular Formula
C45H41N7O9
Molecular Weight
823.85
References & Citations
[1]Lianchao Liu, et al. Discovery of LLC0424 as a Potent and Selective in Vivo NSD2 PROTAC Degrader. J Med Chem. 2024 May 9;67 (9) :6938-6951.
Shipping Conditions
Blue Ice
Storage Conditions
-20°C (Powder, stored under nitrogen)
Scientific Category
Reference compound1
Clinical Information
No Development Reported
Isoform
Cereblon; NSD2/MMSET/WHSC1
Available Sizes
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