tBID 

tBID is a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2) with an IC₅₀ of  0.33 µM.

IC50: 0.33 µM (HIPK2)^[1]

Homeodomain-interacting protein kinase 2 (HIPK2) is a Ser/Thr kinase controlling cell proliferation and survival. TBID, displays toward HIPK2 unprecedented efficacy (IC₅₀=0.33 µM) and selectivity (Gini coefficient 0.592 out of a panel of 76 kinases). The two other members of the HIPK family, HIPK1 and HIPK3, are also inhibited by TBID albeit less efficiently than HIPK2. The mode of action of TBID is competitive with respect to ATP, consistent with modelling. TBID interacts with the hinge region through hydrophobic interactions between Val 213, Val 261, Phe 277, Leu 280, Met 331, Ile 345, and the tetrabromine moiety, while the symmetric nitrogen atom at position 3 interacts with the catalytic Lys 228, thus playing a crucial role in the binding architecture^[1].

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

528.78

C₁₁H₃Br₄N₃O₂

1639895-85-4

Solid

Light yellow to yellow

O=C1N(C2=NC=CN2)C(C3=C(Br)C(Br)=C(Br)C(Br)=C31)=O

Room temperature in continental US; may vary elsewhere.

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

• [1]. Cozza G, et al. Synthesis and properties of a selective inhibitor of homeodomain-interacting protein kinase 2 (HIPK2). PLoS One. 2014 Feb 24;9(2):e89176.  [Content Brief]