LDC000067是一种高选择性CDK9抑制剂，IC50值为44±10 nM。

LDC000067 is a highly specific and selective CDK9 inhibitor with an IC50 value of 44±10 nM.

LDC000067 reduces Ser2-P, induces p53 activation and leads to apoptosis in mESCs. In addition, LDC067 also dose-dependently inhibits P-TEFb-dependent de novo?RNA synthesis of cellular genes.[1]

The fluorescence resonance energy transfer (FRET)-based LANCE Ultra KinaSelect Ser/Thr kit is used to determine IC50 values for various CDK inhibitors. Briefly, a specific ULight MBP peptide substrate (50 nM final concentration) is phosphorylated by a CDK-cyclin pair in buffer (50 mM HEPES-KOH pH 7.5, 10 mM MgCl2, 1 mM EGTA, 2 mM dithiothreitol) containing ATP at the concentration of the Km values of the individual kinases for 1 h at room temperature. Subsequently, phosphorylation is detected by addition of specific Eu-labelled anti-phospho-antibodies (2 nM), which upon binding to the phosphopeptide give rise to a FRET signal. FRET signals are then recorded[1].

1073485-20-7

C18H18N4O3S

370.43

(3-(6-(2-甲氧基苯基)嘧啶-4-基氨基)苯基)甲烷磺酰胺;LDC067;LDC000067

Ethanol:<1 mgml
DMSO:69 mg/mL (186.3 mM)
H2O:<1 mgml
Powder: -20°C for 3 years
In solvent: -80°C for 2 years