Molecular Formula | C12H14Cl2N2O2S |
Molar Mass | 321.22 |
Melting Point | 173-176°C |
Solubility | DMSO: 24mg/mL |
Appearance | solid |
Color | white |
Storage Condition | -20°C |
In vitro study | A-3 hydrochloride inhibits MLC-kinase competitively with respect to ATP and that the K i 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 K i values of 4.3 μM, 3.8 μM, 47 μM, 80 μM, and 5.1 μM, respectively. |
Hazard Symbols | Xi - Irritant![]() |
Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36 - Wear suitable protective clothing. |
WGK Germany | 3 |
biological activity | A-3 hydrochloride are potent, cell-penetrating, reversible, and ATP-competitive non-selective antagonists targeting multiple kinases. A- 3 hydrochloride is an inhibitor of PKA (Ki = 4.3 µM), casein kinase II (Ki = 5.1 µM), and myosin light chain kinase (MLCK) (Ki = 7.4 µM). The A- 3 hydrochloride also inhibited the activity of PKC and casein kinase I with Ki of 47 µM and 80 µM, respectively. |
target | CK1 80 μM (Ki) CK2 5.1 μM (Ki) PKC 47 μM (Ki) PKA 4.3 μM (Ki) |
in vitro study | A- 3 hydrochloride inhibits MLC-kinase competitively with respect to ATP and that K I value is 7.4 μ m. a -3 is also a competitive inhibitor of cAMP-dependent protein kinase, cGMP-dependent protein, protein kinase C, casein kinase I, and casein kinase II, with respect to ATP, exhibits K I values of 4.3 μM, 3.8 μM, 47 μM, 80 μM, and 5.1 μM, respectively. |