SJ6986, GSPT1 molecular glue

Product Details

Formal Name: N-[2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindol-5-yl]-2-(trifluoromethoxy)benzenesulfonamide

Molecular Formula: C₂₀H₁₄F₃N₃O₅

Formula Weight: 433.3

CAS Number: 2765625-93-0

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to at least 40 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

GSPT1 molecular glue

Functions

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). 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.

Application Procedures

First dissolved in DMSO (40 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)