Molecular structure of K-252a, CAS Number: 99533-80-9
K-252a (CAS 99533-80-9)
See product citations (19)
Alternate Names:
SF 2370; K252a
Application:
K-252a is A cell permeable protein kinase inhibitor
CAS Number:
99533-80-9
Purity:
≥97%
Molecular Weight:
467.49
Molecular Formula:
C27H21N3O5
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
* Refer to Certificate of Analysis for lot specific data.
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SDS & Certificate of Analysis
K-252a is a metabolite that can be found in the culture broth of Nocardiopsis sp.. Experiments have shown that at high concentrations this compound is an ATP-competitive inhibitor of cyclic nucleotide-dependent protein kinases. More specifically, K-252a has been found to be a potent inhibitor of PKA, PKC (protein kinase C) activity (IC50 = 32.9 nM), Ser/Thr kinase, CaMKII, MYLK, and Met. K-252a is able to bind neuroblastoma, promoting survival of primary neuronal cultures and induction of neurite outgrowth in SH-SY5Y neuroblastoma cells, along with phosphorylation of tyrosine kinase. Additionally, K-252a also has demonstrated the ability to block neuronal differentiation of rat pheochromocytoma pC12 cells induced by nerve growth factor (NGF) at high concentrations. At very low concentrations (10fM-10nM), K-252a has been noted to prolong the survival of septal, hippocampal, and cortical neurons deprived of glucose. K-252a is an inhibitor of Cdc2, Cdc25, cGKI, PHK, Trk A and PKN.
K-252a (CAS 99533-80-9) References
- K252a is a selective inhibitor of the tyrosine protein kinase activity of the trk family of oncogenes and neurotrophin receptors. | Tapley, P., et al. 1992. Oncogene. 7: 371-81. PMID: 1312698
- Effect of K-252a and abscisic acid on the efflux of citrate from soybean roots. | Shen, H., et al. 2004. J Exp Bot. 55: 663-71. PMID: 14754917
- Potent and preferential inhibition of Ca2+/calmodulin-dependent protein kinase II by K252a and its derivative, KT5926. | Hashimoto, Y., et al. 1991. Biochem Biophys Res Commun. 181: 423-9. PMID: 1659814
- K-252a inhibits nerve growth factor-induced trk proto-oncogene tyrosine phosphorylation and kinase activity. | Berg, MM., et al. 1992. J Biol Chem. 267: 13-6. PMID: 1730579
- K-252a inhibits the response of tomato cells to fungal elicitors in vivo and their microsomal protein kinase in vitro. | Grosskopf, DG., et al. 1990. FEBS Lett. 275: 177-80. PMID: 2261987
- K-252a, a potent protein kinase inhibitor, blocks nerve growth factor-induced neurite outgrowth and changes in the phosphorylation of proteins in PC12h cells. | Hashimoto, S. 1988. J Cell Biol. 107: 1531-9. PMID: 2844830
- K-252a, a novel microbial product, inhibits smooth muscle myosin light chain kinase. | Nakanishi, S., et al. 1988. J Biol Chem. 263: 6215-9. PMID: 2966151
- K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. | Kase, H., et al. 1987. Biochem Biophys Res Commun. 142: 436-40. PMID: 3028414
- K-252a: a specific inhibitor of the action of nerve growth factor on PC 12 cells. | Koizumi, S., et al. 1988. J Neurosci. 8: 715-21. PMID: 3339434
- K-252a, a potent inhibitor of protein kinase C from microbial origin. | Kase, H., et al. 1986. J Antibiot (Tokyo). 39: 1059-65. PMID: 3759657
- Staurosporine, K-252a, and K-252b stabilize calcium homeostasis and promote survival of CNS neurons in the absence of glucose. | Cheng, B., et al. 1994. J Neurochem. 62: 1319-29. PMID: 7510777
- K-252a induces tyrosine phosphorylation of the focal adhesion kinase and neurite outgrowth in human neuroblastoma SH-SY5Y cells. | Maroney, AC., et al. 1995. J Neurochem. 64: 540-9. PMID: 7830046
- K-252a promotes survival and choline acetyltransferase activity in striatal and basal forebrain neuronal cultures. | Glicksman, MA., et al. 1995. J Neurochem. 64: 1502-12. PMID: 7891076
Inhibitor of:
AANAT, AKAP 150, BIN2, C1orf51, C4orf18, CaMKII, CaMKIIN1, CapZIP, casein kinase IIβ, CASKIN2, Cdc2, Cdc25, cGKI, CHIC1, CLEC-2A, CLK2, cPKC βI, CREB-2, CRMP-2, EG628475, EG639396, FAM171B, FAM186B, FAM26E, FAM50B, GDNF, GFRα-4, GFRA (GDNF family receptor alpha), GKAP, GPATCH1, HDDC2, HIPK1, HIPK3, ICA1L, JM4, KBTBD8, Lingo-4, LRRTM2, MAST3, MAST4, Met, MYLK, Neurofascin, neuroligin 2, NGF, NTN, Ost1, OTTMUSG00000010173, PASK, Pbx2, Per 2, PHK, PKA, PKC, PKN, PSD, R3HDM4, Radixin, ROPN1L, S-100A5, Sad-1, SART-3, SEMA4B, Ser/Thr Protein Kinase, Sil, SLITRK6, SLMAP, Synapsin Ia, Synapsin IIIa, TBX19, tetranectin, Trk A, Trk B, TSSK 3, TTBK1, TULA, Twinfilin-2, V3R 11, V3R 4, VRK3, WIBG, ZFP105, and ZNF10.Activator of:
β-1,3-Gal-T6, δ-catenin, 1700016H13Rik, ANKRD58, Antxrl, Barhl2, BM88, BRINP2, BXDC5, C1orf66, Cbl-3, CGI-69, CLK1, Contactin 6, CPEB2, DCAMKL3, Dok-7, EXD, FIR, GDE2, Gm239, Gm98, granzyme F, Liprin α4, LOC440338, LRRTM4, MAP-2C, Mg29, MYT1L, NAIP6, Neudesin, Neurensin-2, Neurexophilin-3, Neuro D2, Neuron navigator 3, NF-H, Ninjurin-2, Nolz-1, OLFM1, OR1D4, OTX1, PCDHA13, PCDHGB6, PRDM8, Prop-1, RBM46, RBMX2, Ribosomal Protein S13, Ribosomal Protein S2, SEZ6, SorCS2, Synapsin Ia, Synaptotagmin IV, SYNDIG1, TAFA3, TAFA5, TEF, Teneurin-1, TFIIA-β, TMEM175, TRAX, TRIM9, Trk C, TRK-T3, VAX1, and VWC2L.Ordering Information
| Product Name | Catalog # | UNIT | Price | Qty | FAVORITES | |
K-252a, 100 µg | sc-200517 | 100 µg | $129.00 | |||
K-252a, 500 µg | sc-200517B | 500 µg | $214.00 | |||
K-252a, 1 mg | sc-200517A | 1 mg | $498.00 |