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PKC&ROCK

Staurosporine (62996-74-1)

Staurosporine is a potent PKC inhibitor for PKCα, PKCγ and PKCη with IC50 of2 nM, 5 nM and 4 nM, less potent to PKCδ (20 nM), PKCε (73 nM) and little active to PKCζ (1086 nM) in cell-free assays. Also shows inhibitory activities on other kinases, such as PKA, PKG, S6K, CaMKII, etc….

Not Intended for Therapeutic Use. For research use only.

CAS: 62996-74-1 Category

Staurosporine (62996-74-1) Description:

Staurosporine, also known as antibiotic AM-2282 or STS, is a potent, non-selective inhibitor of protein kinases, including protein kinase C with promising anti-cancer activity. Staurosporine is a natural product originally isolated in 1977 from the bacterium Streptomyces staurosporeus. Staurosporine was discovered to have biological activities ranging from anti-fungal to anti-hypertensive. The main biological activity of staurosporine is the inhibition of protein kinases through the prevention of ATP binding to the kinase. Staurosporine is a prototypical ATP-competitive kinase inhibitor in that it binds to many kinases with high affinity.

Staurosporine (62996-74-1) Specifications:

Product Name Staurosporine
Synonym AM-2282; AM2282; AM 2282; STS; Antibiotic 230; CGP 41251; CGP41251; CGP-41251; CCRIS 3272; Staurosporine; Staurosporin.
Chemical Name (5S,6R,7R,9R)-6-methoxy-5-methyl-7-(methylamino)-6,7,8,9,15,16-hexahydro-5H,14H-17-oxa-4b,9a,15-triaza-5,9-methanodibenzo[b,h]cyclonona[jkl]cyclopenta[e]-as-indacen-14-one
Drug Class Inhibitor
Purity ≥98% (HPLC)
CAS Number 62996-74-1
Molecular Formula C28H26N4O3
Molecular Weight 466.54
Monoisotopic Mass 466.20049 g/mol
MDL number MFCD00077402
InChIKey HKSZLNNOFSGOKW-FYTWVXJKSA-N
InChi Code InChI=1S/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)/t17-,20-,26-,28+/m1/s1
SMILES CO[[email protected]@H]1[[email protected]@H](C[[email protected]@H]2N3C4=C(N(C5=CC=CC=C56)[[email protected]@]1(C)O2)C6=C7CNC(C7=C4C8=CC=CC=C83)=O)NC
Form Solid powder
Color Pale yellow
Solubility  Soluble in DMSO, not in water
Storage Temp.  4°C
Shelf life >2 years if stored properly
Handling Protect from light and moisture
Application A potent, non-selective inhibitor of protein kinases

 


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RIDADR NONH for all modes of transport

References:

[1]. Alkylation of Staurosporine to Derive a Kinase Probe for Fluorescence Applications. Disney AJ, Kellam B, Dekker LV. ChemMedChem. 2016 May 6;11(9):972-9. doi: 10.1002/cmdc.201500589. Epub 2016 Mar 23. PMID: 27008372

[2]. Suppressing activity of staurosporine from Streptomyces sp. MJM4426 against rice bacterial blight disease. Cheng J, Park SB, Kim SH, Yang SH, Suh JW, Lee CH, Kim JG. J Appl Microbiol. 2016 Apr;120(4):975-85. doi: 10.1111/jam.13034. Epub 2016 Mar 1. PMID: 26678243.

[3]. Staurosporine analogs promote distinct patterns of process outgrowth and polyploidy in small cell lung carcinoma cells. Gallala H, Winter J, Veit N, Nowak M, Perner S, Courts C, Kraus D, Janzen V, Probstmeier R. Tumour Biol. 2015 Apr;36(4):2725-35. doi: 10.1007/s13277-014-2897-6. Epub 2014 Dec 7. PMID: 25487614

[4]. Histone H4 is cleaved by granzyme A during staurosporine-induced cell death in B-lymphoid Raji cells. Lee PY, Park BC, Chi SW, Bae KH, Kim S, Cho S, Kang S, Kim JH, Park SG. BMB Rep. 2016 Oct;49(10):560-565. PMID: 27439606

[5]. Staurosporine induces apoptosis and necroptosis in cultured rat astrocytes. Šimenc J, Lipnik-Štangelj M. Drug Chem Toxicol. 2012 Oct;35(4):399-405. doi: 10.3109/01480545.2011.633087. Epub 2012 Feb 29. PMID: 22372834.

1 review for Staurosporine (62996-74-1)

  1. Cofttek

    Never had such good experience before,The Staurosporine (62996-74-1) is high purity,also customer service is pretty nice !gotta try!!

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