SKI 178 |
| カタログ番号GC44896 |
SKI 178 は、強力なスフィンゴシン キナーゼ 1 (SphK1) および SphK2 阻害剤です。 SKI 178 は、薬剤感受性および多剤耐性癌細胞株 (すなわち、MTR3、NCI-ADR、および HL60/VCR 細胞) の両方において、1.8 ～ 0.1 μM の範囲の IC50 濃度で細胞毒性を示します。 SKI 178 は、ヒト急性骨髄性白血病細胞株において CDK1 依存的にアポトーシスを誘導します。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1259484-97-3
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
SKI 178 is an inhibitor of sphingosine kinase 1 (SPHK1) and SPHK2. Though previously thought to be selective for SPHK1, cellular thermal shift assay results demonstrate direct target engagement of both SPHK1 and SPHK2 in HEK293 cells overexpressing either SPHK1 or SPHK2. It inhibits SPHK1 by 59.6% when used at a concentration of 10.7 µM and inhibits the production of sphingosine-1-phosphate in A549 cells. SKI 178 is cytotoxic to a variety of cancer cell lines including PANC-1, A549, U251, and MCF-7 cells (IC50s = 0.1, 0.3, 0.5, and 1.3 µM, respectively). It prolongs mitosis and induces cell death through the intrinsic apoptotic pathway in a CDK1-dependent manner. SKI 178 (20 mg/kg every other day) reduces the number of white blood cells to a normal range and increases survival in an MLL-AF9 acute myeloid leukemia (AML) mouse xenograft model. It also destabilizes and inhibits microtubule polymerization in an SPHK-independent manner.
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *