1639895-85-4

中文名称:

1639895-85-4

中文同义词:

HIPK2抑制剂(TBID)

英文名称:

tBID

英文同义词:

tBID;1H-Isoindole-1,3(2H)-dione, 4,5,6,7-tetrabromo-2-(1H-imidazol-2-yl)-

CAS号:

1639895-85-4

分子式:

C11H3Br4N3O2

分子量:

528.78

EINECS号:

相关类别:

细胞生物学试剂

Mol文件:

1639895-85-4.mol

生物活性

tBID 是同源结构域相互作用蛋白激酶2 (HIPK2) 的选择性抑制剂，IC50值为 0.33 μM。

靶点

IC50: 0.33 µM (HIPK2)

体外研究

Homeodomain-interacting protein kinase 2 (HIPK2) is a Ser/Thr kinase controlling cell proliferation and survival. TBID, displays toward HIPK2 unprecedented efficacy (IC 50 =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.