62996-74-1 Usage
Uses
1. Used in Anticancer Applications:
Staurosporine is used as an anticancer agent for its potent antitumor activity, inducing apoptosis in a variety of cell lines. It acts as a protein Kinase C inhibitor and inhibits various kinases, including protein kinase C, tyrosine kinase, CDK2/cyclin A, and CDK4/cyclin D. At submicromolar concentrations, staurosporine also inhibits both IKKalpha and IKKbeta, making it a valuable compound in the fight against cancer.
2. Used in Cellular Research:
Staurosporine is used as a research tool in the field of cellular biology for its ability to arrest normal cells at the G1 checkpoint. This property makes it a useful compound for studying cell cycle regulation and the mechanisms underlying cell growth and division.
3. Used in Drug Discovery:
Due to its potent inhibition of various protein kinases, staurosporine is used in drug discovery as a lead compound for the development of new therapeutic agents targeting kinase-related diseases, including cancer and other proliferative disorders.
4. Used in Enzyme Inhibition Studies:
Staurosporine is used as an inhibitor of various kinases, such as CaM kinase, myosin light chain kinase, protein kinase A, protein kinase C, and protein kinase G, in enzyme inhibition studies. This application helps researchers understand the roles of these enzymes in cellular processes and their potential as therapeutic targets.
5. Used in Platelet Aggregation Research:
Staurosporine is used in the study of platelet aggregation, as it inhibits platelet aggregation induced by collagen or ADP but has no effect on thrombin-induced platelet aggregation. This selective inhibition property makes it a valuable tool for investigating the mechanisms underlying platelet activation and aggregation in various pathological conditions.
Biological Activity
Broad spectrum protein kinase inhibitor. Enzymes inhibited include protein kinase C (IC 50 = 3 nM), protein kinase A (IC 50 = 7 nM), p 60v-src tyrosine protein kinase (IC 50 = 6 nM) and CaM kinase II (IC 50 = 20 nM). Also available as part of the Mixed Kinase Inhibitor Tocriset? .
References
1) Omura et al. (1977) A new alkaloid AM-2282 of Streptomyces origin taxonomy, fermentation, isolation and preliminary characterization; J. Antibiot., 30 275
2) Ruegg and Burgess (1989) Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases; Trends in Pharmacological Science 10 218
Check Digit Verification of cas no
The CAS Registry Mumber 62996-74-1 includes 8 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 5 digits, 6,2,9,9 and 6 respectively; the second part has 2 digits, 7 and 4 respectively.
Calculate Digit Verification of CAS Registry Number 62996-74:
(7*6)+(6*2)+(5*9)+(4*9)+(3*6)+(2*7)+(1*4)=171
171 % 10 = 1
So 62996-74-1 is a valid CAS Registry Number.
InChI:InChI=1/C28H26N4O3/c1-28-26(34-3)17(29-2)12-20(35-28)31-18-10-6-4-8-14(18)22-23-16(13-30-27(23)33)21-15-9-5-7-11-19(15)32(28)25(21)24(22)31/h4-11,17,20,26,29H,12-13H2,1-3H3,(H,30,33)/p+1/t17-,20-,26-,28+/m1/s1
62996-74-1Relevant articles and documents
PROCESS FOR THE PURIFICATION OF INDOLE CARBAZOLE ALKALOIDS
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Page/Page column 16, (2021/09/11)
Disclosed is a process for the purification of staurosporine (1), which comprises salification of staurosporine (1) (Formula (1)) by treatment with a mineral acid to give a precipitated salt, isolation of the staurosporine (1) precipitated salt, treatment of the staurosporine (1) isolated salt with an organic base, and isolation of staurosporine (1). Also disclosed are novel polymorphic forms of the mono- and bis-hydrochloride salts of staurosporine (1).
COMPOUNDS FOR IMMUNOPOTENTIATION
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Page/Page column 140, (2010/02/15)
Methods of stimulating an immune response and treating patients responsive thereto with 3,4-di(1H-indol-3-yl)-1H-pyrrole-2,5-diones, staurosporine analogs, derivatized pyridazines, chromen-4-ones, indolinones, quinazolines, nucleoside analogs, and other small molecules are disclosed.
Design and implementation of an efficient synthetic approach to pyranosylated indolocarbazoles: Total synthesis of (+)-RK286c, (+)-MLR-52, (+)-staurosporine, and (-)-TAN-1030a
Wood, John L.,Stoltz, Brian M.,Goodman, Steven N.,Onwueme, Kenolisa
, p. 9652 - 9661 (2007/10/03)
A total synthesis of the natural products (+)-staurosporine (2), (+)-RK286c (3), (-)-TAN-1030a (4), and (+)-MLR-52 (5) has been achieved. The synthetic strategy involves the stereoselective ring expansion of a furanosylated indolocarbazole [(+)-8] to a pyranosylated congener [(+)-12] that serves as a common intermediate in the production of 2-5.
Staurosporine and ent-staurosporine: The first total syntheses, prospects for a regioselective approach, and activity profiles
Link,Raghavan, Subharekha,Gallant, Michel,Danishefsky, Samuel J.,Chou,Ballas, Lawrence M.
, p. 2825 - 2842 (2007/10/03)
The total syntheses of staurosporine and ent-staurosporine have been achieved. Both glycosidic bonds were built from glycal precursors. The first was constructed by intermolecular coupling of an indole anion with a 1,2-anhydrosugar derived from an endo-glycal by direct epoxidation. The second bond was assembled from an exo-glycal by intramolecular iodoglycosylation.
