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C1382Level 5

K 252a

**Semantic type:** Organic Chemical|Pharmacologic Substance

**Definition:** An indolocarbazole-based alkaloid and staurosporine analog isolated from Nocardiopsis and Actinomadura species, with kinase inhibiting activity. K252a inhibits a wide variety of enzymes, including, but not limited to, protein kinase A (PKA), C (PKC) and G (PKG), calcium (Ca2+)/calmodulin-dependent kinase type II (CaMKII), phosphorylase kinase (PhK), tropomyosin receptor kinase (Trk; neurotrophic tyrosine receptor kinase; NTRK), myosin light-chain kinase (MLCK; MYLK), mixed-lineage protein kinase 3 (MLK3), receptor-type tyrosine-protein kinase FLT3 (CD135; fms-like tyrosine kinase 3; fetal liver kinase-2; FLK2) and actin-regulating kinase PRK1 (PAK1). Inhibition of these kinases prevents the activation of signaling pathways in which these kinases play a key role.

**Synonyms:** - 9,1-Epoxy-1H-diindolo(1,2,3-fg:3',2',1'-kl)pyrrolo(3,4-i)(1,6)benzodiazocine-10-carboxylic acid, 2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-, methyl ester, (9-alpha,10-beta,12-alpha)- - Antibiotic K 252A - Antibiotic SF 2370 - K-252a - K252A - K252A - Protein Kinase Inhibitor K252a - SF 2370

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