| 货号 | 12754S |
| 使用方法 | K252a is supplied as a lyophilized powder. For a 1 mM stock, reconstitute the 100 μg in 213.9 µl DMSO. Working concentrations and length of treatment can vary depending on the desired effect, but it is typically used as a pretreatment at 0.1-1 µM for 0.5-1 hr prior to treating with a stimulator. Soluble in DMSO at 100 mg/ml; poorly soluble in ethanol. |
| 供应商 | CST |
| 背景 | Originally isolated from the soil fungi Nocardiopisis sp., K252a is a staurosporine analog that inhibits various protein kinases through competition with the ATP binding site (1,2). K252a is a reversible cell-permeable, potent inhibitor of phosphorylase kinase (IC50 = 1.7 nM), protein kinase A (PKA) (IC50= 140 nM), and protein kinase C (PKC) (IC50 = 470 nM) (3,4). K252a is also known to inhibit protein kinase G and CaM kinase II (5,6). K252a inhibits nerve growth factor induced Trk activation (IC50= 3 nM), as well as downstream signaling (5,7,8). K252a is reported to induce apoptosis and cell cycle arrest through cdc25 and cdc2 inhibition (9). |
| 存放说明 | -20C |
| 纯度 | >99% |
| 计算分子量 | 467.47 g/mol |
| 参考文献 | 1 . Kase, H. et al. (1986) J Antibiot (Tokyo) 39, 1059-65. 2 . Kase, H. et al. (1987) Biochem Biophys Res Commun 142, 436-40. 3 . Elliott, L.H. et al. (1990) Biochem Biophys Res Commun 171, 148-54. 4 . Davis, P.D. et al. (1992) J Med Chem 35, 177-84. 5 . Koizumi, S. et al. (1988) J Neurosci 8, 715-21. 6 . Hashimoto, Y. et al. (1991) Biochem Biophys Res Commun 181, 423-9. 7 . Berg, M.M. et al. (1992) J Biol Chem 267, 13-6. 8 . Tapley, P. et al. (1992) Oncogene 7, 371-81. 9 . Chin, L.S. et al. (1999) Cancer Invest 17, 391-5. |
Chemical structure of K252a. | |
Western blot analysis of extracts from PC-12 cells, serum-starved overnight and untreated or treated with Human β-Nerve Growth Factor (hβ-NGF) #5221 (100 ng/ml, 5 min) either with or without K252a pretreatment (1 hr) at the indicated concentrations, using Phospho-TrkA (Tyr490) Antibody #9141 (upper) or β-Actin (D6A8) Rabbit mAb #8457 (lower). | |
Western blot analysis of extracts from HeLa cells, serum-starved overnight and untreated or treated with TPA #4174 (200 nM, 15 min) either with or without K252a pretreatment (1 hr) at the indicated concentrations, using Phospho-MARCKS (Ser167/170) (D13E4) XP® Rabbit mAb #8722 (upper) or MARCKS (D88D11) XP®Rabbit mAb #5607 (lower). |
