1-(5-ISOQUINOLINYLSULFONYL)-2-METHYL-PIPERAZINE Chemical Properties

Boiling point:

495.3±55.0 °C(Predicted)

Density 

1.277±0.06 g/cm3(Predicted)

storage temp. 

2-8°C

solubility 

ethanol: 20 mg/mL

pka

7.69±0.40(Predicted)

form 

Solid

color 

White to light yellow

BRN 

5482740

Safety Information

WGK Germany 

3

RTECS 

TL9305000

F 

10

Toxicity

LD50 intravenous in mouse: 94mg/kg

MSDS

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1-(5-ISOQUINOLINYLSULFONYL)-2-METHYL-PIPERAZINE Usage And Synthesis

Uses

Protein kinase inhibitor H-7 is a potent inhibitor of protein kinase C (PKC) and cyclic nucleotide dependent protein kinase, with a Ki of 6 μM for PKC[1].

Definition

ChEBI: A member of the class of N-sulfonylpiperazines that is 2-methylpiperazine substituted at position 1 by a 5-isoquinolinesulfonyl group.

Biological Activity

Protein kinase inhibitor. IC 50 values for inhibition of PKC, PKG, PKA and myosin light chain kinase are 6.0, 5.8, 3.0 and 97.0 μ M respectively.

IC 50

PKC: 6 μM (Ki)

References

[1] Hidaka H, et, al. Isoquinolinesulfonamides, novel and potent inhibitors of cyclic nucleotide dependent protein kinase and protein kinase C. Biochemistry. 1984 Oct 9;23(21):5036-41. DOI:10.1021/bi00316a032

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