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Ligand K-252a

Basic Ligand Information

Molecular Structure

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Roles as Enzyme Ligand

Inhibitor in Enzyme-catalyzed Reactions (9 results)

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Show Inhibitors (9 entries)

EC NUMBER

COMMENTARY

LITERATURE

ENZYME 3D STRUCTURE

2.7.10.1

complete inhibition at 200 nM

704659

-

2.7.11.1

-

662578

4wsq, 3D-view

2.7.11.1

-

662578

5m5a, 3D-view

2.7.11.1

-

708481

4wsq, 3D-view

2.7.11.1

-

708481

5m5a, 3D-view

2.7.11.1

4 entries

2.7.11.13

strong inhibition

662271

-

2.7.11.17

inhibits CaM-KII

664865

-

2.7.11.19

microbial broth product, highly selective

492139

-

7.1.2.1

a potent inhibitor of protein kinase

713257

-

3D Structure of Enzyme-Ligand-Complex (PDB) (8 results)

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Show 3D Structure of Enzyme-Ligand-Complex (PDB) (8 entries)

EC NUMBER

ENZYME 3D STRUCTURE

2.7.1.112

1r0p, 3D-view

2.7.10.2

5m5a, 3D-view

2.7.11.1

4wsq, 3D-view

2.7.11.1

5m5a, 3D-view

2.7.11.1

4wsq, 3D-view

2.7.11.1

5m5a, 3D-view

2.7.11.1

4 entries

2.7.11.10

4kik, 3D-view

2.7.12.2

3eqf, 3D-view

Enzyme Kinetic Parameters

IC₅₀ Value (2 results)

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Show IC50 Value (2 entries)

EC NUMBER

IC50 VALUE

IC50 VALUE MAXIMUM

COMMENTARY

LITERATURE

2.7.11.1

0.0000028

-

mutant enzyme G2019S

708481

2.7.11.1

0.0000036

-

wild type enzyme

708481

2.7.11.1

2 entries

References & Links

Literature References (7)

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Show Reference (7 entries)

BRENDA REFERENCE ID

PUBMED ID

TITLE

YEAR

AUTHORS

JOURNAL

VOLUME

PAGES

492139

2393389

K252a is a potent and selective inhibitor of phosphorylase kinase

1990

Elliott, L.H.; Wilkinson, S.E.; Sedgwick, A.D.; Hill, C.H.; Lawton, G.; Davis, P.D.; Nixon, J.S.

Biochem. Biophys. Res. Commun.

171

148-154

662271

15272003

Serine and threonine phosphorylation of the low density lipoprotein receptor-related protein by protein kinase Calpha regulates endocytosis and association with adaptor molecules

2004

Ranganathan, S.; Liu, C.X.; Migliorini, M.M.; Von Arnim, C.A.; Peltan, I.D.; Mikhailenko, I.; Hyman, B.T.; Strickland, D.K.

J. Biol. Chem.

279

40536-40544

662578

12884127

AfsR as an integrator of signals that are sensed by multiple serine/threonine kinases in Streptomyces coelicolor A3(2)

2003

Horinouchi, S.

J. Ind. Microbiol. Biotechnol.

30

462-467

664865

16083343

Calcium/calmodulin-dependent protein kinases as potential targets in cancer therapy

2005

Rodriguez-Mora, O.; LaHair, M.M.; Howe, C.J.; McCubrey, J.A.; Franklin, R.A.

Expert Opin. Ther. Targets

9

791-808

704659

20212045

Excitation-transcription coupling via calcium/calmodulin-dependent protein kinase/ERK1/2 signaling mediates the coordinate induction of VGLUT2 and Narp triggered by a prolonged increase in glutamatergic synaptic activity

2010

Doyle, S.; Pyndiah, S.; De Gois, S.; Erickson, J.D.

J. Biol. Chem.

285

14366-14376

708481

19076219

Investigation of leucine-rich repeat kinase 2: enzymological properties and novel assays

2009

Anand, V.S.; Reichling, L.J.; Lipinski, K.; Stochaj, W.; Duan, W.; Kelleher, K.; Pungaliya, P.; Brown, E.L.; Reinhart, P.H.; Somberg, R.; Hirst, W.D.; Riddle, S.M.; Braithwaite, S.P.

FEBS J.

276

466-478

713257

20516032

Biochemical characterization of in vitro phosphorylation and dephosphorylation of the plasma membrane H+-ATPase

2010

Hayashi, Y.; Nakamura, S.; Takemiya, A.; Takahashi, Y.; Shimazaki, K.; Kinoshita, T.

Plant Cell Physiol.

51

1186-1196

Links to other databases for K-252a

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Show Links (1 entry)

ChEBI

PubChem