Chemical Structure
K-252a [99533-80-9]
AG-CN2-0019
Overview
- SupplierAdipoGen Life Sciences
- Product NameK-252a [99533-80-9]
- Delivery Days Customer10
- CAS Number99533-80-9
- CertificationResearch Use Only
- Estimated Purity>98%
- Molecular FormulaC27H21N3O5
- Molecular Weight467.5
- Scientific DescriptionAntibiotic [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]. - Chemical. CAS: 99533-80-9. Formula: C27H21N3O5. MW: 467.5. Isolated from Nonomuraea longicatena chiba. 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. Apoptosis inducer. Cell cycle arrest inducer. Potential drug for psoriasis treatment.
- 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
- Storage Instruction-20°C,2°C to 8°C
- UNSPSC12352200
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)