K-252a

Specifications / Handling

More Information
Product Details
Synonyms	SF 2370; Antibiotic K 252a; Antibiotic SF 2370
Product Type	Chemical
Properties
Formula	C₂₇H₂₁N₃O₅
MW	467.5
CAS	99533-80-9
RTECS	NZ0550000
Source/Host Chemicals	Isolated from Nocardiopsis sp.
Purity Chemicals	≥98% (HPLC)
Appearance	White to slight yellow powder.
Solubility	Soluble in DMSO, methanol, methylene chloride, ethyl acetate or acetone. Insoluble in water.
InChi Key	KOZFSFOOLUUIGY-SOLYNIJKSA-N
Smiles	[H][C@]12C[C@](O)(C(=O)OC)[C@](C)(O1)N1C3=C(C=CC=C3)C3=C4CNC(=O)C4=C4C5=C(C=CC=C5)N2C4=C13
Shipping and Handling
Shipping	AMBIENT
Short Term Storage	+4°C
Long Term Storage	-20°C
Handling Advice	Keep cool and dry. Protect from light.
Use/Stability	Stable for at least 2 years after receipt when stored at -20°C. Store solutions at -20°C in the dark.
Documents
MSDS	Download PDF
Product Specification Sheet
Datasheet	Download PDF

Product-specific References

Description

Antibiotic [1].
PKC, PKA and PKG inhibitor [1, 2, 4].
Shows neurotropic activity by inducing neurite outgrowth [3, 8, 11,16].
Highly potent cell permeable CaM kinase [6] and phosphorylase inhibitor [5].
Tyrosine protein kinase inhibitor of the TRK family [7].
Antiproliferative [9, 10, 13, 15].
Apoptosis inducer [12, 16].
Cell cycle arrest inducer [12].
Potential drug for psoriasis treatment [14].

Product References

K-252a, a potent inhibitor of protein kinase C from microbial origin: H. Kase, et al.; J. Antibiot. (Tokyo) 39, 1059 (1986)
K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases: H. Kase, et al.; BBRC 142, 436 (1987)
K-252a: a specific inhibitor of the action of nerve growth factor on PC 12 cells: s. Koizumi, et al.; J. Neurosci. 8, 715 (1988)
Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989) (Review)
K252a is a potent and selective inhibitor of phosphorylase kinase: L.H. Elliott, et al.; BBRC 171, 148 (1990)
Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926: Y. Hashimoto, et al.; BBRC 181, 423 (1991)
K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors: P. Tapley, et al.; Oncogene 7, 371 (1992)
Specific inhibition of NGF receptor tyrosine kinase activity by K-252a: K. Muroya, et al.; Biochim. Biophys. Acta 1135, 353 (1992)
K252a: a new blocker of the cell-cycle at G1 phase in a human hepatoma cell line: T. Nakayama, et al.; Experientia 49, 876 (1993)
Anti-proliferative effect of the kinase inhibitor K252a on human prostatic carcinoma cell lines: R. Delsite & D. Djakiew; J. Androl. 17, 481 (1996)
K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996) (Review)
K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c: L.S. Chin, et al.; Cancer Invest. 17, 391 (1999)
K252a inhibits the oncogenic properties of Met, the HGF receptor: A. Morotti, et al.; Oncogene 21, 4885 (2002)
K252a, a high-affinity nerve growth factor receptor blocker, improves psoriasis: an in vivo study using the severe combined immunodeficient mouse-human skin model: S.P. Raychaudhuri, et al.; J. Invest. Dermatol. 122, 812 (2004)
K252a inhibits proliferation of ovarian cancer cells by upregulating p21WAF1: N. Takai, et al.; Oncol. Rep. 14, 141 (2005)
K252a suppresses neuronal cells apoptosis through inhibiting the translocation of Bax to mitochondria induced by the MLK3/JNK signaling after transient global brain ischemia in rat hippocampal CA1 subregion: Q. Wang, et al.; J. Recept. Signal. Transduct. Res. 31, 307 (2011)

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