I-BET282E 

I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC₅₀s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD)^[1].

I-BET282E has a weak inhibition of the hERG potassium ion channel (pIC₅₀ 4.4-5.1 in a variety of assay formats). I-BET282E shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4^[1].

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

I-BET282E (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Cl_b, LBF, Vss, t_1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively^[1].
I-BET282E (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC_0-t, C_max and T_max values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively^[1].

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

546.64

C₂₆H₃₄N₄O₇S

2885162-99-0

CS(=O)(O)=O.COC1=C(C=C(C2=C1)N=CC3=C2N([C@H](C)COC)C(C4CCOCC4)=N3)C5=C(ON=C5C)C

Room temperature in continental US; may vary elsewhere.

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

• [1]. Jones KL, et al. Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression. J Med Chem. 2021;64(16):12200-12227.  [Content Brief]