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A-3 hydrochloride

Names

[ CAS No. ]:
78957-85-4

[ Name ]:
A-3 hydrochloride

[Synonym ]:
a-3 hydrochloride

Biological Activity

[Description]:

A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively[1].

[Related Catalog]:

Signaling Pathways >> Epigenetics >> PKC
Signaling Pathways >> Neuronal Signaling >> CaMK
Signaling Pathways >> Protein Tyrosine Kinase/RTK >> PKA
Research Areas >> Others
Signaling Pathways >> Stem Cell/Wnt >> PKA
Signaling Pathways >> Cell Cycle/DNA Damage >> Casein Kinase
Signaling Pathways >> Stem Cell/Wnt >> Casein Kinase
Signaling Pathways >> TGF-beta/Smad >> PKC

[Target]

CK1:80 μM (Ki)

CK2:5.1 μM (Ki)

PKC:47 μM (Ki)

PKA:4.3 μM (Ki)


[In Vitro]

A-3 hydrochloride inhibits MLC-kinase competitively with respect to ATP and that the Ki value is 7.4 μM. A-3 is also a competitive inhibitor of cAMP-dependent protein kinase, cGMP-dependent protein kinase, protein kinase C, casein kinase I, and casein kinase II, with respect to ATP, exhibits Ki values of 4.3 μM, 3.8 μM, 47 μM, 80 μM, and 5.1 μM, respectively[1].

[References]

[1]. Inagaki M, et al. Naphthalenesulfonamides as calmodulin antagonists and protein kinase inhibitors. Mol Pharmacol. 1986 Jun;29(6):577-81.

Chemical & Physical Properties

[ Melting Point ]:
173-176ºC

[ Molecular Formula ]:
C12H14Cl2N2O2S

[ Molecular Weight ]:
321.22300

[ Exact Mass ]:
320.01500

[ PSA ]:
80.57000

[ LogP ]:
4.70420

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi: Irritant;

[ Risk Phrases ]:
36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

Related Compounds