K-252a

• Description:

  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 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.

• Shipping Conditions:

  Blue Ice

• Storage Conditions:

  -20°C, 3 years (Powder)

• Scientific Category:

  Natural Products

• Clinical Information:

  No Development Reported

• Isoform:

  CaMK II

• CAS Number:

  [99533-80-9]