Staurosporine, 5mg

Product#: FNK-BLK-0590-5mg
$792.62
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Staurosporine (5mg)


Cat No: FNK-BLK-0590-5mg

Product ID and Size
 
Cat No. Description Size Link
FNK-BLK-0590-100µg Staurosporine 100μg Mammalian Cell Culture, Animal Cell Culture-Classic Media, Diagnocine
FNK-BLK-0590-1mg Staurosporine 1mg Mammalian Cell Culture, Animal Cell Culture-Classic Media, Diagnocine
FNK-BLK-0590-5mg Staurosporine 5mg Mammalian Cell Culture, Animal Cell Culture-Classic Media, Diagnocine


Description

Staurosporine was originally isolated from a culture broth of Saccharothrix aerocolonigenes subsp. staurosporeus AM-2282 while screening for microbial alkaloids. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive1). The structure and absolute configuration of staurosporine was elucidated by X-ray crystallographic analysis 2–4). The first total synthesis was reported by Danishefsky et al5). Furthermore, Sturosporine was found to inhibit protein kinase C, IC50 =2.7 nM (rat brain)6) . Staurosporine was also found to be a potent relaxant of rabbit aortic strips contracted by various agonists7) . Staurosporine exerts it's biological effect by interacting, or binding, with a biological target such as a kinase through the prevention of ATP binding to the kinase. This is achieved through the stronger affinity of staurosporine to the ATP-binding site on the kinase. This image was obtained by crystallisation of the kinase with staurosporine followed by x-ray diffraction8) .
Staurosporine analogues, 7-Hydroxy-Staurosporine(UCN01) and N-Benzyl-Staurosporine(CGP 41251) are currently under clinical investigation as potential anticancer drugs9) .


Origin: from Saccharothrix aerocolonigenes subsp. staurosporeus AM-2282

CAS Registry Number: 62996-74-1

Appearance: Pale yellow crystals

Molecular Formula/ Weight: C28H26N4O3=466.20

Melting Point: 205-210˚C(dec.)

Purity: >98% by HPLC

Solubility: Sol. in DMSO, DMF, Slightly sol. in MeOH, Chloroform

Handling and Storage: Store at -20℃.


References:
  1. S. ?mura et al., J.Antibiot., 30, 275 (1977).
  2. A. Furusaki et al., J.Chem.Soc., Chem.Commun., 1978, 800 (1978).
  3. A. Furusaki et al., Bull Chem.Soc.Jpn., 55, 3681 (1982).
  4. N. Funato et al., Tetrahedron Lett., 35, 1251 (1994).
  5. J. T. Link et al., J.Am.Chem.Soc., 117, 552 (1995).
  6. T. Tamaoki et al., Biochem.Biophys.Res.Commun., 135, 397 (1986).
  7. Y. Sasaki et al., Eur.J.Phamacol., 202, 367 (1991).
  8. L. Prade, et al., Structure (London) 5, 1627-1637 (1997).
  9. G. Caravatti et al., Med.Chem.Lett., 4, 399 (1994).
  10. H. Nakano & S. ?mura, J.Antibiot., 62, 17 (2009).

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