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Staurosporine, 1 mg  

Staurosporine, 1 mg

Staurosporine from Streptomyces staurosporeus (antibiotic AM-2282)

cell permeable general inhibitor of protein kinases

More details

PKI-STSP-001

Availability: on stock

255,00 €

Background: The cell permeable staurosporine (staurosporin), isolated from Streptomyces staurosporeus, is one of the most potent and widely used inhibitors of protein kinases initially proposed to inhibit protein kinase C (IC50 = 5 nM). Later it was shown that staurosporine has a much broader specificity for various protein kinases including PKA (IC50 = 15 nM), PKG (18 nM), CaMKII (20 nM), S6K (5 nM), MLCK (21 nM), SRC (6 nM), FGR (2 nM), LYN (20 nM) and SYK (16 nM). In contrast it has a relatively low potency for ERK1 (1.5 µM), CSK (2 µM), IGF-IR (6.2 µM), CK2 (19.5 µM) and CK1 (>100µM).

Chemical formula: C28H26N4O3
Molecular weight: 466.5 g/mol
Purity: >98% (TLC, HPLC)
Solubility: soluble in DMSO, methanol and ethyl acetate
Appearance: off-white to light yellow powder
Handling: Toxic. May be carcinogenic. Wear gloves and mask when handling product. Protect from light
CAS Number: 62996-74-1

Also available predissolved at 10 mM in our kinase inhibitor Set (AGC group).

BIAFFIN – SERVICES:

Use our - SPR Binding Assay of BIAFFIN for comprehensive kinetic characterization of your small molecule kinase inhibitors. 

PKA_Ca_Staurosporine.png

Figure: Real-time kinetic analysis of kinase inhibitor Staurosporine binding to PKA Cα using surface plasmon resonance.

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Product specific literature references:

Tamaoki T, Nomoto H, Takahashi I, Kato Y, Morimoto M, Tomita F (1986) "Staurosporine, a potent inhibitor of phospholipid/Ca++dependent protein kinase" Biochem. Biophys. Res. Commun. 135(2):397-402

Nakano H, Kobayashi E, Takahashi I, Tamaoki T, Kuzuu Y, Iba H (1987) "Staurosporine inhibits tyrosine-specific protein kinase activity of Rous sarcoma virus transforming protein p60" J. Antibiot. (Tokyo) 40(5):706-8

Meggio F, Donella Deana A, Ruzzene M et al. (1995) "Different susceptibility of protein kinases to staurosporine inhibition. Kinetic studies and molecular bases for the resistance of protein kinase CK2" Eur J Biochem. 234(1):317-22

Yamaki K, Ohuchi K (1999) "Participation of protein kinases in staurosporine-induced interleukin-6 production by rat peritoneal macrophages" Br J Pharmacol. 127(6):1309-16.

Product Citations:

Boonpawa R, Spenkelink A, Punt A, Rietjens IMCM. (2017) "Physiologically based kinetic modeling of hesperidin metabolism and its use to predict in vivo effective doses in humans." Mol Nutr Food Res. 61(8).

PLEASE NOTE: This product is designed for research purposes and can only be delivered to academic and business customers.