E7820 | RBM39 molecular glue

CAS:
 289483-69-8
Catalog Number:
 10-3935
E7820 chemical structure Focus Biomolecules

Available Options

Size:PriceQuantity 
5 mg$50.00
25 mg$175.00

E7820 (289483-69-8) is an angiogenesis inhibitor that suppresses expression of integrins α2, α3, α5, and ß1.1 Broad-spectrum antitumor and antiangiogenic effects are mainly mediated via integrin α2 suppression.2 E7820 has been identified as a molecular glue that induces proteasomal degradation of the U2AF-related splicing factor CAPERα (RBM39) via CRL4DCAF15 mediated ubiquitination in human cancer cell lines.3,4  E7820 has also been shown to induce degradation of the aryl hydrocarbon receptor nuclear translator (ARNT), a protein essential in maintaining cellular homeostasis in response to environmental stress.5

References/Citations:

  1. Funahashi et al. (2002), Sulfonamide derivative, E7820, is a unique angiogenesis inhibitor suppressing an expression of integrin alpha2 subunit on endothelium; Cancer Res. 62 6116
  2. Semba et al. (2004), An angiogenesis inhibitor E7820 shows broad-spectrum tumor growth inhibition in a xenograft graft: possible value of integrin alpha2 on platelets as a biological marker; Clin. Cancer Res. 10 1430
  3. Uehara et al. (2017), Selective degradation of splicing factor CAPERα by anticancer sulfonamides; Nat. Chem. Biol. 13 675
  4. Faust et al. (2020), Structural complementarity facilitates E7820-mediated degradation of RBM39 by DCAF15; Nat. Chem. Biol. 16 7
  5. Kim et al. (2020), Aryl Sulfonamides Induce Degradation of Aryl Hydrocarbon Receptor Nuclear Translocator through CRL4DCAF15 E3 Ligase; Mol. Cells 43 935
CAS:
289483-69-8
Catalog Number:
10-3935
Activity:
RBM39 molecular glue
Chemical Names:
N-(3-Cyano-4-methyl-1H-indol-7-yl)-3-cyanobenzenesulfonamide
Molecular Weight:
336.37
Molecular Formula:

C17H12N4O2S

Solubility:
Soluble in DMSO (>25 mg/ml)
Physical Properties:
White solid
Purity:

98% HPLC
NMR: (Conforms)

Storage Temperature:
-20°C
Stability:
Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. 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

20% OFF

For Postdoc
Customers!