Product Description: SJ44236 is the PROTAC degrader for BET that degrades BRD2 (DC50 = 0.127 nM), BRD3 and BRD4. SJ44236 exhibits cytotoxicity in cell MV4-11 and HD-MB03 with IC50s of 0.12 nM and 0.92 nM. SJ44236 downregulates the expression of c-Myc, upregulates the expression of p53. SJ44236 exhibits a good orally bioavailability of 45% in mice[1]. (Pink: ligand for target protein JQ-1 carboxylic acid (HY-78695); Black: linker (HY-W012935); Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189))
Applications: Cancer-programmed cell death
Formula: C40H45ClN8O3S
References: [1]Actis M, et al., Evaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs. J Med Chem. 2025 Feb 13;68(3):3591-3611.
Molecular Weight: 753.36
Research Area: Cancer
Target: Epigenetic Reader Domain;PROTACs
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