K145 (hydrochloride)

产品编号: DC9625 Featured
K145 (hydrochloride)
结构式
1449240-68-9
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中国地区超过5000个高品质化合物库存
应用领域
K145 hydrochloride 是一种选择性的,具有底物竞争性和口服活性的 SphK2 抑制剂,IC50 为 4.3 µM,Ki 为 6.4 µM。K145 hydrochloride 对 SphK1 和其他蛋白激酶没有活性。K145 hydrochloride 可诱导细胞凋亡,并具有强大的抗肿瘤活性。
Cas No.: 1449240-68-9
名称:
别名: SphK2 inhibitor;K 145 hydrochloride;K-145 hydrochloride
SMILES: O=C(N(CCN)C/1=O)SC1=C/CCC2=CC=C(OCCCC)C=C2.[H]Cl
分子式: C18H25ClN2O3S
分子量: 384.9207
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: K145 is a selective SphK2 inhibitor with an IC50 of 4.30±0.06 μM , while no inhibition of SphK1 at concentrations up to 10 μM. in vitro: K145 inhibited the activity of SphK2 in a dose-dependent manner with an IC50 of 4.30±0.06 uM , while no inhibition of SphK1 at concentrations up to 10 uM was observed. 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 down-stream ERK and Akt signaling pathways. in vivo: K145 also significantly inhibited the growth of U937 tumors in nude mice by both intraperitoneal and oral administration, thus demonstrating its in vivo efficacy as a potential lead anticancer agent.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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