- 商品介绍
- 规格参数
- 包装参数
General description
A cell-permeable hydroxymethylpyrrolidine compound that acts as a high affinity (Kd = 5 nM, kofft1/2 = 8.5 min), but poor, sphingosine kinase-1/SphK1 substrate (1/1,500 of sphingosine processivity) and potently inhibits against SphK1-catalyzed sphingosine-to-S1P conversion (IC50 = 2.0 nM; [sphingosine] = 3 µM) in a reversible, sphingosine-, but not ATP-, competitive manner (Ki = 3.6 nM), exhibiting 132-fold selectivity over SphK2, no affinity toward S1P receptors (S1P1, S1P2, S1P3, S1P5), and much reduced or no inhibitory activity against a panel of 46 other lipid and protein kinases (IC50 >10 µM), including the structurally related diacylglyerol kinase α/DAGKα (3.7% inhibition at 10 µM). PF-543 exposure in 1483 squamous cultures is reported to result in intracellular S1P depletion (by 90% upon 1 h 200 nM or 7 d 1 µM drug exposure) with concomitant elevation of sphingosine level and no detectable cytotoxicity (1 µM for 7 to 9 d in 1483, A549, Jurkat, LN229, MCF7, or U937 cultures). Also active in human whole blood assays in the presence human & bovine serum proteins (IC50 = 26.7 nM against cellular C17-S1P formation from exogenously added 20 µM C17-sphingosine in 10 min with 30 min drug preincubation).
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Schnute, M.E., et al. 2012. Biochem. J.444, 79.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| Quality Segment | 100 |
| assay | ≥95% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | off-white |
| solubility | DMSO: 50 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | O=S(C1=CC=CC=C1)(CC2=CC(C)=CC(OCC3=CC=C(CN4[C@@H](CO)CCC4)C=C3)=C2)=O |
| InChI | 1S/C27H31NO4S/c1-21-14-24(20-33(30,31)27-7-3-2-4-8-27)16-26(15-21)32-19-23-11-9-22(10-12-23)17-28-13-5-6-25(28)18-29/h2-4,7-12,14-16,25,29H,5-6,13,17-20H2,1H3/t25-/m1/s1 |
| InChI key | NPUXORBZRBIOMQ-RUZDIDTESA-N |
| 长度(mm) | |
| 宽度(mm) | |
| 高度(mm) | |
| 重量(kg) |
-
询价
-
询价
-
¥ 2528.88
-
¥ 1683.78
-
¥ 1451.54
-
询价
-
询价
-
询价
-
¥ 6330.00
-
¥ 3290.05
-
瓶顶过滤器-500ml容量,MF75TM系列，聚苯乙烯外壳，75mmSFCA滤膜，孔径0.2um,适合瓶颈尺寸45mm，12/箱，291-4520，Nalgene，Thermofisher，赛默飞世尔¥ 2856.42
-
¥ 20380.83
-
¥ 2151.46
-
¥ 1301.36
-
¥ 3852.13
-
¥ 1196.14
-
¥ 1783.21
-
¥ 787.34
-
¥ 46052.83
-
询价
微信小程序
7X24小时在线咨询