A PROTAC that drives CRBN degradation
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PROTAC CRBN Degrader-1

Item No. 41878

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N1-(2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)amino)ethyl)-N20-((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)-3,9,12,18-tetraoxaicosanediamide
CAS Number
2358775-70-7
Synonyms
  • PROTAC Cereblon Degrader-1
  • Proteolysis-targeting Chimera Cereblon Degrader-1
  • Proteolysis-targeting Chimera CRBN Degrader-1
Molecular Formula
C53H72N8O13S
Formula Weight
1061.3
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly soluble: 0.1-1 mg/mlDMSO: Sparingly soluble: 1-10 mg/ml
SMILES
CC(C)(C)[C@@H](C(N1C[C@@H](C[C@H]1C(NCC2=CC=C(C3=C(C)N=CS3)C=C2)=O)O)=O)NC(COCCCCCOCCOCCCCCOCC(NCCNC4=C5C(C(N(C5=O)C6CCC(NC6=O)=O)=O)=CC=C4)=O)=O
InChi Code
InChI=1S/C53H72N8O13S/c1-34-46(75-33-57-34)36-16-14-35(15-17-36)29-56-48(66)41-28-37(62)30-60(41)52(70)47(53(2,3)4)58-44(65)32-74-25-10-6-8-23-72-27-26-71-22-7-5-9-24-73-31-43(64)55-21-20-54-39-13-11-12-38-45(39)51(69)61(50(38)68)40-18-19-42(63)59-49(40)67/h11-17,33,37,40-41,47,54,62H,5-10,18-32H2,1-4H3,(H,55,64)(H,56,66)(H,58,65)(H,59,63,67)/t37-,40?,41+,47-/m1/s1
InChi Key
PEZCAXDTKNFUCR-CTMFSBKBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $138

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    5 mg

    $585

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    Product Description

    PROTAC CRBN degrader-1 is a proteolysis-targeting chimera (PROTAC) that contains VHL ligand 1 (Item No. 21591) conjugated to the cereblon (CRBN) inhibitor pomalidomide (Item No. 19877).1 It induces degradation of CRBN in HeLa cells with a half-maximal degradation concentration (DC50) value of 200 nM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Girardini, M., Maniaci, C., Hughes, S.J., et al. Cereblon versus VHL: Hijacking E3 ligases against each other using PROTACs. Bioorg. Med. Chem. 27(12), 2466-2479 (2019).