SJ6986

SKU: orb1303132

Description

SJ6986 is a potent, selective, and orally bioavailable molecular glue degrader of GSPT1/2, achieving maximal degradation (Dmax 99%) with a DC50 of 2.1 nM. This compound is a valuable chemical probe for investigating targeted protein degradation mechanisms in oncology research, supporting both in vitro and in vivo studies of cancers dependent on GSPT1/2 function.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2765625-93-0
• MW: 497.4
• Purity: 99.73%
• Formula: C₂₀H₁₄F₃N₃O₇S
• SMILES: O=C1N(C(=O)C=2C1=CC(NS(=O)(=O)C3=C(OC(F)(F)F)C=CC=C3)=CC2)C4C(=O)NC(=O)CC4
• Target: Others,Molecular Glues
• Solubility: DMSO:55 mg/mL (110.57 mM);10% DMSO+90% Saline:2.5 mg/mL (5.03 mM)

Bioactivity

• In Vivo:
  SJ6986 shows t 1/2 of 3.44 h by intravenous injection of 3 mg/kg and t max of 0.25 h by oral administration (%F = 84) of 10 mg/kg in CD1 mice .
• In Vitro:
  SJ6986 demonstrates potency with EC50 values at 1.5 nM, 0.4 nM, 726 nM, 336 nM, and 3583 nM in the MV4-11, MHH-CALL-4, MB002, MB004, and HD-MB03 cell lines respectively . In MV4-11 cells, under conditions of a 0-100 μM concentration range and a 3-day incubation, an EC50 of 1.5 nM was observed, indicating significant inhibition of cell proliferation . Additionally, Western Blot analysis in the same cell line, with a concentration range of 0-10 μM over 4 and 24 hours, revealed a dose- and time-dependent reduction in GSPT1 protein levels, further confirming the compound's efficacy .

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

SJ 6986, SJ6986, SJ-6986

Compound Identifiers

PubChem CID

155925914