K-252a

K-252a, a staurosporine analog, inhibits protein kinase, with IC50 values of 470 nM, 140 nM, 270 nM, and 1.7 nM for PKC, PKA, Ca2+/calmodulin-dependent kinase type II, and phosphorylase kinase, respectively[1][2]. K-252a is a potent inhibitor (IC50 of 3 nM) of the tyrosine protein kinase (TRK) activity of the NGF receptor gp140trk, the product of the trk protooncogene[3].

Product Specifications

CAS Number

[99533-80-9]

Product Name Alternative

SF2370; Antibiotic K 252a; Antibiotic SF 2370

UNSPSC

12352005

Hazard Statement

H360, H371

Target

Antibiotic; Autophagy; CaMK; PKA; PKC; Trk Receptor

Type

Natural Products

Related Pathways

Anti-infection; Autophagy; Epigenetics; Neuronal Signaling; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt; TGF-beta/Smad

Applications

COVID-19-immunoregulation

Field of Research

Infection; Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/k-252a.html

Purity

99.45

Solubility

DMSO : 50 mg/mL (ultrasonic; warming)

Smiles

O=C(NC1)C2=C1C3=C4C5=C2C6=C(C=CC=C6)N5[C@](C[C@]7(O)C(OC)=O)([H])O[C@]7(C)N4C8=C3C=CC=C8

Molecular Formula

C27H21N3O5

Molecular Weight

467.47

Precautions

H360, H371

References & Citations

[1]Yasuzawa, T., et al. The structures of the novel protein kinase C inhibitors K-252a, b, c AND d Journal of Antibiotics 39 (8), 1072-1078 (1986) .|[2]Davis, P.D., et al. Inhibitors of protein kinase C. 1.1 2,3-bisarylmaleimides Journal of Medicinal Chemistry 35, 177-184 (1992) .|[3]Tapley P, et al. K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors. Oncogene. 1992 Feb;7 (2) :371-81.|[4]Qingxia Chen, et al. LncRNA LINC00641 Sponges miR-497-5p to Ameliorate Neural Injury Induced by Anesthesia via Up-Regulating BDNF. Front Mol Neurosci. 2020 Jun 30;13:95.|[5]S Hashimoto, et al. K-252a, a potent protein kinase inhibitor, blocks nerve growth factor-induced neurite outgrowth and changes in the phosphorylation of proteins in PC12h cells. J Cell Biol. 1988 Oct;107 (4) :1531-9.|[6]Rui Zhang, et al. Tenacissoside H promotes neurological recovery of cerebral ischaemia/reperfusion injury in mice by modulating inflammation and oxidative stress via TrkB pathway. Clin Exp Pharmacol Physiol. 2021 May;48 (5) :757-769.