K-252aA cell permeable protein kinase inhibitor

K-252a (CAS 99533-80-9)

K-252a | CAS 99533-80-9 is rated 5.0 out of 5 by 2.
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Synonym: SF 2370; K252a
Application: A cell permeable protein kinase inhibitor
CAS Number: 99533-80-9
Purity: ≥97%
Molecular Weight: 467.49
Molecular Formula: C27H21N3O5
* Refer to Certificate of Analysis for lot specific data (including water content).
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K-252a is a metabolite originally isolated from 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.


References

1. Kase, H., et al. 1986. J. Antibiot. 39: 1059-1065. PMID: 3759657
2. Kase, H., et al. 1987. Biochem. Biophys. Res. Commun. 142: 436-440. PMID: 3028414
3. Hashimoto, Y., et al. 1991. Biochem. Biophys. Res. Commun. 181: 423-429. PMID: 1659814
4. Tapley, P., et al. 1992. Oncogene. 7: 371-381. PMID: 1312698
5. Cheng, B., et al. 1994. J. Neurochem. 62: 1319-1329. PMID: 7510777
6. Glicksman, M.A., et al. 1995. J. Neurochem. 64: 1502-1512. PMID: 7891076

Physical State :
Solid
Solubility :
Soluble in DMSO (1 mg/ml), DMF (1 mg/ml), Chloroform, Dichloromethane, and Methanol.
Storage :
Store at -20° C
Boiling Point :
~685.3° C at 760 mmHg (Predicted)
Density :
~1.7 g/cm3 (Predicted)
Refractive Index :
n20D 1.84
IC50 :
trk tyrosine kinase family members: IC50 = 3 nM
Ki Data :
PKC: Ki= 25 nM
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
RTECS :
NZ0550000
PubChem CID :
11612445
MDL Number :
MFCD00161522
SMILES :
C[C@]12[C@@](CC(O1)N3C4=CC=CC=C4C5=C6C(=C7C8=CC=CC=C8N2C7=C53)CNC6=O)(C(=O)OC)O

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Certificate of Analysis

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K-252a  Product Citations

See how others have used K-252a. Click on the entry to view the PubMed entry .

Citations 1 to 4 of 4 total

PMID: # 28495385  Moosavi, F. et al. 2017. Bioorg. Med. Chem. 25: 3235-3246.

PMID: # 18955270  Hattori, N. et al. 2010. Evid Based Complement Alternat Med. 7: 63-8.

PMID: # 17266195  Hudkins, RL. et al. 2007. J. Med. Chem. 50: 433-441.

PMID: # 17396254  Kim, SY. et al. 2007. Appl. Microbiol. Biotechnol. 75: 1119-1126.

Citations 1 to 4 of 4 total
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Rated 5 out of 5 by from 暂时没有问题 给客户的实验室采购的,如果老师用后有问题会来评论,之前一直有采购SANTA 的东西,服务还是不错的。
Date published: 2017-09-27
Rated 5 out of 5 by from Kim et al Kim et al. (PubMed ID 17396254) used K-25a, a cell permeable protein kinase inhibitor, to inactivate a Chromobacterium gene encoding enzymes that catalyze tryptophan decarboxylation and condensation in violacein biosynthesis. -SCBT Publication Review
Date published: 2015-04-05
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