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044975 K-252a CAS: 99533-80-9

Specifications
References
CAS Number
99533-80-9
Grade
Highly Purified
MDL Number
MFCD00161522
Molecular Formula
C27H21N3O5
Molecular Weight
467.47
EU Commodity Code
38220090
Shipping Temp
RT
Storage Temp
-20°C

K-252a is an antibiotic, PKC, PKA and PKG inhibitor. Shows neurotropic activity by inducing neurite outgrowth. Highly potent cell permeable CaM kinase and phosphorylase inhibitor. Tyrosine protein kinase inhibitor of the TRK family. Antiproliferative and apoptosis inducer. Cell cycle arrest inducer. Potential drug for psoriasis treatment.

Source
Isolated from Nonomuraea longicatena chiba
Synonyms
SF 2370; Antibiotic K 252a; Antibiotic SF 2370
CAS Number
99533-80-9
Molecular Weight
467.47
Molecular Formula
C27H21N3O5
Solubility
DMSO, methanol, methylene chloride, ethyl acetate, acetone. Insoluble in water.
Appearance
Supplied as a white to off-white powder.
Purity
≥98% (HPLC)
Storage and Stability
Store short term at 4°C. Keep cool and dry, and protect from light. For long term storage, store solutions at -20°C in the dark. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
Important Note
This product as supplied is intended for research use only, not for use in human, therapeutic or diagnostic applications without the expressed written authorization of United States Biological.
Toxicity and Hazards
 All products should be handled by qualified personnel only, trained in laboratory procedures.
References
1. K-252a, a potent inhibitor of protein kinase C from microbial origin: H. Kase, et al.; J. Antibiot. (Tokyo) 39, 1059 (1986)|2. 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)|3. 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)|4. Staurosporine, K-252 and UCN-01: potent but nonspecific inhibitors of protein kinases: U.T. Ruegg & G.M. Burgess; TIPS 10, 218 (1989) (Review)|5. K252a is a potent and selective inhibitor of phosphorylase kinase: L.H. Elliott, et al.; BBRC 171, 148 (1990)|6. 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)|7. 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)|8. Specific inhibition of NGF receptor tyrosine kinase activity by K-252a: K. Muroya, et al.; Biochim. Biophys. Acta 1135, 353 (1992)|9. 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)|10. Anti-proliferative effect of the kinase inhibitor K252a on human prostatic carcinoma cell lines: R. Delsite & D. Djakiew; J. Androl. 17, 481 (1996)|11. K252a and staurosporine microbial alkaloid toxins as prototype of neurotropic drugs: P. Lazarovici, et al.; Adv. Exp. Med. Biol. 391, 367 (1996) (Review)|12. K252a induces cell cycle arrest and apoptosis by inhibiting Cdc2 and Cdc25c: L.S. Chin, et al.; Cancer Invest. 17, 391 (1999)|13. K252a inhibits the oncogenic properties of Met, the HGF receptor: A. Morotti, et al.; Oncogene 21, 4885 (2002)|14. 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)|15. K252a inhibits proliferation of ovarian cancer cells by upregulating p21WAF1: N. Takai, et al.; Oncol. Rep. 14, 141 (2005)|16. 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)
USBio References
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