SJ995973 is a potent BET-targeting PROTAC (proteolysis-targeting chimera) designed to induce degradation of BET family proteins (BRD2, BRD3, BRD4). It recruits an E3 ligase (commonly VHL) to BET proteins, leading to their ubiquitination and proteasomal degradation. In biochemical and cellular assays, SJ995973 shows DC₅₀ values (degradation concentration 50%) of around 5–10 nM for BRD4, with efficient degradation observed within 4–6 hours of treatment. It achieves over 90% degradation of BRD4 at concentrations as low as 30 nM in cancer cell lines. SJ995973 also suppresses downstream oncogenic targets like MYC with an IC₅₀ of ~20–50 nM in proliferation assays across BET-sensitive tumor models (e.g., hematologic malignancies, NUT midline carcinoma).
MedKoo Cat#: 208026
Name: SJ995973
CAS#: 2882065-25-8
Chemical Formula: C37H40ClN7O5S
Exact Mass: 729.2500
Molecular Weight: 730.28
Elemental Analysis: C, 60.85; H, 5.52; Cl, 4.85; N, 13.43; O, 10.95; S, 4.39
The following data is based on the product molecular weight 730.28 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
