SJ44236 

SJ44236 is a BET PROTAC degrader with activity against BRD2, BRD3 and BRD4 (DC₅₀ = 127 pM). SJ44236 induces ubiquitination and proteasomal degradation by forming a ternary complex with BET proteins and CRBN-DDB1. SJ44236 downregulates c-Myc, upregulates p53 and reduces cancer cell viability. SJ44236 can be used for the research of leukemia and medulloblastoma^[1]. (Pink: BET ligand (HY-78695); Blue: Cereblon ligand (HY-W890189); Black: linker (HY-W012935)).

SJ44236 (1×10^-10 to 1×10² μM; 24 h) potently degrades BRD4 in HiBiT-BRD4 HEK293 LgBiT stable cells with a Dmax₅₀ of 0.19 nM, achieving 96.9% maximal degradation sustained for over 20 h with no impact on cell viability^[1].
SJ44236 (0.001-100 nM; 4 h) degrades endogenous BRD4 in MV4-11 cells with a DC₅₀ of 0.127 nM after 4 h of treatment, consistent with its potency in engineered HEK293 cells^[1].
SJ44236 (72 h) potently inhibits the proliferation of MV4-11 cells with an IC₅₀ of 0.12 nM and HD-MB03 cells with an IC₅₀ of 0.92 nM after 72 h of treatment^[1].
SJ44236 (100 nM; 4 h) induces over 90% degradation of BRD2, BRD3, and BRD4 in MV4-11 cells after 4 h of treatment at 100 nM, alongside expected downstream regulation of c-Myc (down) and p53 (up)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

SJ44236 (3-10 mg/kg; i.v., p.o.; single dose) exhibits favorable in vivo pharmacokinetic properties in female CD1 mice, including 45% oral bioavailability, low clearance, and rapid oral absorption^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

753.36

C₄₀H₄₅ClN₈O₃S

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Actis M, et al. Evaluation of Cereblon-Directing Warheads for the Development of Orally Bioavailable PROTACs. J Med Chem. 2025;68(3):3591-3611.  [Content Brief]