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PROTAC CRBN Degrader-1

PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other[1]. (Blue: VHL ligand (S, R, S) -AHPC (HY-125845) ; Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846) ; Black: Linker (HY-128847) )

Product Specifications

CAS Number

[2358775-70-7]

UNSPSC

12352005

Target

E1/E2/E3 Enzyme; PROTACs

Type

Reference compound

Related Pathways

Metabolic Enzyme/Protease; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/protac-crbn-degrader-1.html

Purity

98.77

Solubility

DMSO : 100 mg/mL (ultrasonic)

Smiles

O=C(NC1=O)CCC1N(C2=O)C(C3=C2C(NCCNC(COCCCCCOCCOCCCCCOCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6)C=C5)=O)=O)=O)=O)=CC=C3)=O

Molecular Formula

C53H72N8O13S

Molecular Weight

1061.25

References & Citations

[1]Girardini M, et al. Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs. Bioorg Med Chem. 2019 Jun 15;27 (12) :2466-2479.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, stored under nitrogen)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

Cereblon; von Hippel-Lindau (VHL)

Available Sizes

Curated Selection

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