A potent inhibitor of PKA
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KT 5720

Item No. 10011011

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3,9,10,11,12-hexahydro-10S-hydroxy-9-methyl-1-oxo-9R,12S-epoxy-1H-diindolo[1,2,3-fg:3',2',1'-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid, hexyl ester
CAS Number
108068-98-0
Molecular Formula
C32H31N3O5
Formula Weight
537.6
Purity
≥98%
Formulation (Request formulation change)
A clear film
Solubility(Learn about Variance in Solubility)
DMSO: 1 mg/mlMethanol: 5 mg/ml
SMILES
C[C@@]1([C@](O)(C(OCCCCCC)=O)C2)N(C3=CC=CC=C43)C5=C4C(CNC6=O)=C6C(C7=CC=CC=C87)=C5N8[C@H]2O1
InChi Code
InChI=1S/C32H31N3O5/c1-3-4-5-10-15-39-30(37)32(38)16-23-34-21-13-8-6-11-18(21)25-26-20(17-33-29(26)36)24-19-12-7-9-14-22(19)35(28(24)27(25)34)31(32,2)40-23/h6-9,11-14,23,38H,3-5,10,15-17H2,1-2H3,(H,33,36)/t23-,31+,32+/m0/s1
InChi Key
ZHEHVZXPFVXKEY-RUAOOFDTSA-N
Origin
Bacterium/Nocardiopsis sp.
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    50 µg

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    Product Description

    Protein kinase A (PKA) regulates multiple signal transduction events via protein phosphorylation and is integral to all cellular responses involving the cyclic AMP second messenger system. KT 5720 is one of a family of compounds synthesized by the fungus Nocardiopsis sp. It blocks PKA signaling through competitive inhibition of ATP with a Ki value of 60 nM.1 Reported IC50 values vary widely depending upon ATP concentration tested and can range from 56 nM (low ATP) to 3 µM (physiologic ATP).2,3 Non-specific effects of KT 5720 include inhibition of phosphorylase kinase, PDK1, MEK, MSK1, PKBα, and GSK3β at concentrations as effective as or more potent than that for inhibition of PKA.2,3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kase, H., Iwahashi, K., Nakanishi, S., et al. K-252 compounds, novel and potent inhibitors of protein kinase C and cyclic nucleotide-dependent protein kinases. Biochem. Biophys. Res. Commun. 142(2), 436-440 (1987).

    2. Davies, S.P., Reddy, H., Caivano, M., et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem. J. 351(1), 95-105 (2000).

    3. Murray, A.J. Pharmacological PKA inhibition: All may not be what it seems. Sci. Signal. 1(22), (2008).