A-3 hydrochloride 是靶向多种激酶 (kinase) 的强效、细胞渗透的、可逆的、ATP 竞争性的非选择性拮抗剂。A-3 hydrochloride 是针对 PKA (Ki=4.3 µM)，酪蛋白激酶 II (Ki=5.1 µM) 和肌球蛋白轻链激酶 (MLCK) (Ki=7.4 µM) 的抑制剂。A-3 hydrochloride 还抑制 PKC 和酪蛋白激酶 I 的活性，Ki 分别为 47 µM 和 80 µM。
货号:ajcx29090
CAS:78957-85-4
分子式:C12H14Cl2N2O2S
分子量：321.22
溶解度:DMSO: 125 mg/mL (389.14 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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].

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].

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