SJ6986 | GSPT1 molecular glue

CAS:
 2765625-93-0
Catalog Number:
 10-3933

Available Options

Size:PriceQuantity 
5 mg$55.00
25 mg$180.00

SJ6986 (2765625-93-0) is a potent (IC50 = 15 nM for Cereblon; EC50 = 1.5 nM for MV4-11 AML cells), selective, and orally bioavailable molecular glue degrader of the small GTPases G1 to S phase transition 1/2 (GSPT1/2).1 It displayed selectivity for GPST1/2 over 9000 other proteins including the classic cereblon substrates IKZF1 (Ikaros) and IZKF3 (Aiolos). SJ6986 displayed efficacy against acute lymphoblastic leukemia cell lines and xenografts.2

References/Citations:

  1. Nishiguchi et al. (2021), Identification of Potent, Selective, and Orally Bioavailable Small-Molecule GSPT1/2 Degraders from a Focused Library of Cereblon Modulators; J. Med. Chem. 64 7296
  2. Chang et al. (2023), The orally bioavailable GSPT1/2 degrader SJ6986 exhibits in vivo efficacy in acute lymphoblastic leukemia; Blood 142 629
CAS:
2765625-93-0
Catalog Number:
10-3933
Activity:
GSPT1 molecular glue
Chemical Names:
N-[2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]-2-(trifluoromethoxy)benzenesulfonamide
Molecular Weight:
433.34
Molecular Formula:

C20H14F3N3O5

Solubility:
Soluble in DMSO (at least 40 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