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SJ44236

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 ; Black: linker (HY-W012935) ; Blue: ligand for E3 ligase Cereblon E3 ligase Ligand 54 (HY-W890189) )

Product Specifications

UNSPSC

12352005

Target

Epigenetic Reader Domain; PROTACs

Related Pathways

Epigenetics; PROTAC

Applications

Cancer-programmed cell death

Field of Research

Cancer

Smiles

O=C(C[C@@H]1N=C(C2=C(N3C1=NN=C3C)SC(C)=C2C)C4=CC=C(Cl)C=C4)N5CCC(CC5)CN6CCN(C7=CC=C(C=C7)C8C(NC(CC8)=O)=O)CC6

Molecular Formula

C40H45ClN8O3S

Molecular Weight

753.36

References & Citations

[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.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Frequently Asked Questions

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