Article · Wikipedia archive · Last revised Jul 14, 2026

K252a

K252a is an alkaloid isolated from Nocardiopsis bacteria. This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L).

Last revised
Jul 14, 2026
Read time
≈ 2 min
Length
345 w
Citations
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Source
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K252a
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Names
Preferred IUPAC name
Methyl (13S,14R,16R)-14-hydroxy-13-methyl-5-oxo-6,7,13,14,15,16-hexahydro-5H-13,16-epoxydiindolo[1,2,3-fg:3′,2′,1′-kl]pyrrolo[3,4-i][1,6]benzodiazocine-14-carboxylate
Identifiers
ChEMBL
ChemSpider
ECHA InfoCard 100.167.781
UNII
  • InChI=1S/C27H21N3O5/c1-26-27(33,25(32)34-2)11-18(35-26)29-16-9-5-3-7-13(16)20-21-15(12-28-24(21)31)19-14-8-4-6-10-17(14)30(26)23(19)22(20)29/h3-10,18,33H,11-12H2,1-2H3,(H,28,31)/t18?,26-,27-/m1/s1 checkY
    Key: KOZFSFOOLUUIGY-CYBHFKQVSA-N checkY
Properties1
C27H21N3O5
Molar mass 467.481 g·mol−1
Solubility in other solvents Soluble in DMSO, dichloromethane, and methanol
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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K252a is an alkaloid isolated from Nocardiopsis bacteria. This staurosporine analog is a highly potent cell permeable inhibitor of CaM kinase and phosphorylase kinase (IC50 = 1.8 and 1.7 nmol/L, respectively). At higher concentrations it is also an efficient inhibitor of serine/threonine protein kinases (IC50 of 10 to 30 nmol/L).23456789

K252a is reported to promote myogenic differentiation in C2 mouse myoblasts6 and has been shown to block the neuronal differentiation of rat pheochromocytoma PC12 cells by inhibition of trk tyrosine kinase activity.10

K252a has been reported in preclinical research as a potential treatment for psoriasis.11

K252a inhibits tyrosine phosphorylation of Trk A induced by NGF. PC12 cells were incubated in the presence or absence of 10 ng/ml NGF with or without various concentrations of K252a.

See also

See also

References

References

  1. K252a from Fermentek
  2. Ruegg, U.T. et al. (1989) Tips 10, 218.
  3. Eliot, L.H. et al. (1990) B.B.R.C. 171, 148.
  4. Simpson, D.l. et al. (1991) J. Neurosci. Res, 28, 148.
  5. Chin, L.S. et al. (1999) Cancer Invest. 17, 391.
  6. Tapley, P. et al. (1992) Oncogene 7, 371.
  7. Hashimoto, S. (1998) J. Cell Biol. 107, 1531.
  8. Kase, H. et al. (1987) B.B.R.C. 142, 436.
  9. Hirayama E. et al. (2001) B.B.R.C. 285, 1237.
  10. Borasio, G.D. Neurosci. Lett. (1990) 108, 207.
  11. Dubois Declercq, Sarah; Pouliot, Roxane (2013). "Promising New Treatments for Psoriasis". The Scientific World Journal 980419. doi:10.1155/2013/980419. PMC 3713318. PMID 23935446.
Further reading

Further reading