Drug intelligence / Profile preview

7-oxo-staurosporine

Development stage
Preclinical
Modality
Small Molecules
Administration
Not Clinically Established; Used In Vitro, Possible Intravenous Or Intraperitoneal In Preclinical Research
01

Overview

7-oxo-staurosporine is a **small molecule antibiotic** originally isolated from *Streptomyces platensis*[1][3][7]. It is an oxidized analogue of staurosporine and is highly fluorescent[5]. Its mechanism of action centers on **potent inhibition of protein kinases** including protein kinase C (PKC), protein kinase A (PKA), phosphorylase kinase, epidermal growth factor receptor (EGFR), and c-Src, with nanomolar IC50 values[1][3][9][5]. 7-oxo-staurosporine interferes with the cell cycle by inducing G2/M phase arrest and exhibits cytotoxicity against various tumor cell lines (including resistant and susceptible leukemia cells) and antifungal activity against the mycelial form of certain Candida species[1][2][5]. The compound has also demonstrated Ras mislocalization activity independently of PKC inhibition[6]. As an analogue of UCN-01 and staurosporine, 7-oxo-staurosporine shows comparable antitumor activity but is mainly used in research settings.

Other names
7-oxo Staurosporine7-OxostaurosporineOxostaurosporine7-Oxo StaurosporinLCM76-LLCM-76-LLCM 76-L
02

Targets

EGFR (Epidermal growth factor receptor)PHKA2 (Phosphorylase Kinase)PKA (Cyclic amp-dependent protein kinase)SRC (Proto-oncogene tyrosine-protein kinase Src)PRKCD (Protein kinase C delta)PRKCQ (Protein kinase C theta)

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