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12754
K252a
Activators & Inhibitors
Chemical Modulators

K252a #12754

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K252a: Image 1

Chemical structure of K252a.

K252a: Image 2

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).

K252a: Image 3

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).

Product Usage Information

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.

Product Description

Molecular Weight 467.47 g/mol
Purity

>99%

Molecular Formula

C27H21N3O5

CAS 97161-97-2
Solubility Soluble in DMSO at 100mg/ml.

Background

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.

Limited Uses

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Products are labeled with For Research Use Only or a similar labeling statement and have not been approved, cleared, or licensed by the FDA or other regulatory foreign or domestic entity, for any purpose. Customer shall not use any Product for any diagnostic or therapeutic purpose, or otherwise in any manner that conflicts with its labeling statement. Products sold or licensed by CST are provided for Customer as the end-user and solely for research and development uses. Any use of Product for diagnostic, prophylactic or therapeutic purposes, or any purchase of Product for resale (alone or as a component) or other commercial purpose, requires a separate license from CST. Customer shall (a) not sell, license, loan, donate or otherwise transfer or make available any Product to any third party, whether alone or in combination with other materials, or use the Products to manufacture any commercial products, (b) not copy, modify, reverse engineer, decompile, disassemble or otherwise attempt to discover the underlying structure or technology of the Products, or use the Products for the purpose of developing any products or services that would compete with CST's products or services, (c) not alter or remove from the Products any trademarks, trade names, logos, patent or copyright notices or markings, (d) use the Products solely in accordance with CST's Product Terms of Sale and any applicable documentation, and (e) comply with any license, terms of service or similar agreement with respect to any third party products or services used by Customer in connection with the Products.

For Research Use Only. Not For Use In Diagnostic Procedures.
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To Purchase # 12754S
Product # Size Price
12754S
100 µg $ 149