K145 hydrochloride 是选择性的，底物竞争性的和口服有效的SphK2抑制剂，IC50为 4.3 μM，Ki为 6.4 μM。它可诱导细胞凋亡，显示出强大的抗肿瘤活性。

K145 hydrochloride is a selective sphk2 inhibitor with substrate competitiveness and oral activity, with IC50 of 4.3 μM and Ki of 6.4 μM. K145 hydrochloride can induce apoptosis and has strong antitumor activity.

K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30 uM. The Lineweaver-Burk analysis revealed a Ki of 6.4±0.7 uM for SphK2 and indicated that K145 is a substrate competitive inhibitor (with sphingosine). K145 accumulates in U937 cells, suppresses the S1P level, and inhibits SphK2. K145 also exhibited inhibitory effects on the growth of U937 cells as well as apoptotic effects in U937 cells, and that these effects may be through the inhibition of downstream ERK and Akt signaling pathways.

1449240-68-9

C18H25ClN2O3S

384.92

K145盐酸盐

H2O:125 mg/mL (324.74 mM),Need ultrasonic and warming
H2O:125 mg/mL (324.74 mM),Need ultrasonic and warming
DMSO:48 mg/mL (124.7 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years