K252C

Names

[ Name ]:
K252C

[Synonym ]:
staurosporine aglycon
Staurosporinone,K-252c
Staurosporinone
K-252C
STAUROSPORINE AGLYCONE

Biological Activity

[Description]:

K-252c, a staurosporine analog isolated from Nocardiopsis sp., is a cell-permeable PKC inhibitor, with an IC50 of 2.45 µM. K-252c induces apoptosis in human chronic myelogenous leukemia cancer cells. K-252c also inhibits β-lactamase, chymotrypsin, and malate dehydrogenase[1][2][3].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC

Research Areas >> Cancer

Research Areas >> Infection

Signaling Pathways >> TGF-beta/Smad >> PKC

Signaling Pathways >> Anti-infection >> Bacterial

[Target]

IC50: 2.45 µM (PKC)[1].

[References]

[1]. Pereira, E.R., et al. Structure-activity relationships in a series of substituted indolocarbazoles: Topoisomerase I and protein kinase C inhibition and antitumoral and antimicrobial properties J. Med. Chem. 39(22), 4471-4477 (1996).

[2]. Liu, R., et al. Two indolocarbazole alkaloids with apoptosis activity from a marine-derived actinomycete Z2039-2 Arch. Pharm. Res. 30(3), 270-274 (2007).

[3]. Zimmermann, A., et al. Indolocarbazoles exhibit strong antiviral activity against human cytomegalovirus and are potent inhibitors of the pUL97 protein kinase Antiviral Res. 48(1), 49-60 (2000).

[4]. McGovern, S.L., et al. Kinase inhibitors: Not just for kinases anymore Journal of Medicinal Chemistry 46, 1478-1483 (2003).

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₀H₁₃N₃O

[ Molecular Weight ]:
311.33700

[ Exact Mass ]:
311.10600

[ PSA ]:
60.68000

[ LogP ]:
4.52780

Safety Information

[ Safety Phrases ]:
22-24/25

[ WGK Germany ]:
3

[ HS Code ]:
2933990090

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Customs

[ HS Code ]: 2933990090

[ Summary ]:
2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%