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Product Details

Pomalidomide | Cereblon ubiquitination inhibitor

Thalidomide analog. Inhibits cereblon (CRBN) an E3 ubiquitin ligase, IC50 ~3 μM for CRBN-DDB1 complex.1 Displays antiangiogenic and immunomodulatory activity in vivo potently inhibiting the production of TNFα and IL-2.2 Promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome.3 Conjugation with other ligands is a strategy to target proteins for in vivo proteasomal degradation via PROTACS.4,5

References/Citations
1) Lopez-Girona et al. (2012), Cereblon is direct protein target for immunomodulatory and antiproliferative activities of lenalidomide and pomalidomide; Leukemia, 26 2326
2) Zhu et al. (2013), Molecular mechanism of action of immune-modulatory drugs thalidomide, lenalidomide and pomalidomide in multiple myeloma; Leukemia Lymphoma, 54 683
3) Donovan et al. (2018), Thalidomide promotes degradation of SALL4, a transcription factor implicated in Duane Radial Ray syndrome; Elife, 7 e38430
4) Winter et al. (2015), DRUG DEVELOPMENT. Phthalimide conjunction as a strategy for in vivo target protein degradation; Science, 348 1376
5) Lohbeck and Miller (2016), Practical synthesis of a phthalimide-based Cereblon ligand to enable PROTAC development; Bioorg. Med. Chem. Lett., 26 5260

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Catalog#  10-2768-0020

$50.00
Quantity
Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee.
 
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CAS:
19171-19-8
Catalog Number:
10-2768
Activity:
Cereblon ubiquination inhibitor
Chemical Name:
1,3-Dioxo-2-(2,6-dioxopiperidin-3-yl)-4-aminoisoindoline; 3-amino-N-(2,6-dioxo-3-piperidyl)phthalamide
Molecular Weight:
273.24
Molecular Formula:
C13H11N3O4
Solubility:
Soluble in DMSO (up to 50 mg/ml).
Physical Properties:
Yellow solid
Purity:
98% by TLC
NMR (Conforms)
Storage Temperature:
-20° (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO may be stored at -20° for up to 1 month.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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