Drug intelligence / Profile preview

K-252a

Development stage
Preclinical
Modality
Metabolically Activated Prodrugs → Prodrugs/Conditional Activator Small Molecules → Small Molecules, Classical Binding Small Molecules → Small Molecules, Nucleic Acid-Directed Small Molecules → Small Molecules
Administration
Topical
01

Overview

**K-252a** is an indolocarbazole-based alkaloid and a staurosporine analog isolated from Nocardiopsis and Actinomadura species. It is a potent, broad-spectrum inhibitor of protein kinases, including protein kinase C (PKC), protein kinase A (PKA), protein kinase G (PKG), calcium/calmodulin-dependent kinase II (CaMKII), phosphorylase kinase, tropomyosin receptor kinases (Trk/NTRK family), myosin light-chain kinase, mixed-lineage protein kinase 3, FLT3 receptor tyrosine-protein kinase, and actin-regulating kinases. Its mechanism of action involves competitive inhibition at the ATP binding site of these kinases. At nanomolar concentrations it potently inhibits Trk receptors and blocks nerve growth factor signaling in neuronal cells. Preclinical research has explored its use as an antimicrobial agent and as a potential treatment for psoriasis; it also exhibits neuroprotective effects at low concentrations but can induce apoptosis by inhibiting cell cycle regulators such as Cdc2 and Cdc25[1][3][4][5][6][8].

Other names
k-252ak252ak 252aSF 2370SF2370SF-2370Antibiotic K 252aAntibiotic SF 2370
02

Targets

PDE1 (Phosphodiesterase 1)CAMK2D (Calcium/calmodulin-dependent protein kinase II delta)MAPK family (MAPK family detailed)MLCK (Myosin light chain kinase)PHKA2 (Phosphorylase Kinase)PKA (Cyclic amp-dependent protein kinase)PKC (Protein kinase C family)PKG (cGMP-dependent protein kinase I alpha)NTRK1 (Tropomyosin-related receptor kinase A)FLT3 (Fms related receptor tyrosine kinase 3)Trk (Trk receptor family)

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