Buy a SimpleChIP Kit and Try our New SimpleChIP® Universal qPCR Master Mix (88989P) for Free | Get The Code >>
12754
K252a

K252a #12754

Western Blotting

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).

Learn more about how we get our images
Western Blotting

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).

Learn more about how we get our images
Structure

Chemical structure of K252a.

Learn more about how we get our images

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.

Storage:

Store lyophilized or in solution at -20ºC, desiccated. Protect from light. In lyophilized form, the chemical is stable for 24 months. Once in solution, use within 3 months to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Molecular Weight:

467.47 g/mol

Purity:

>99%

Molecular Formula:

C27H21N3O5

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).

  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.
For Research Use Only. Not For Use In Diagnostic Procedures.

Cell Signaling Technology is a trademark of Cell Signaling Technology, Inc.
XP is a registered trademark of Cell Signaling Technology, Inc.

News from the Bench

Discover what’s going on at CST, receive our latest application notes and tips, read our science features, and learn about our products.

Subscribe

To Purchase # 12754S

View sizes
Product # Size Price
12754S
100 µg $ 142.0