您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > HA-100(hydrochloride)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
HA-100(hydrochloride)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
HA-100(hydrochloride)图片
CAS NO:210297-47-5
规格:98%
分子量:350.3
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
inhibitor of protein kinases (PKs)
CAS:210297-47-5
分子式:C13H15N3O2S ? 2HCl
分子量:350.3
纯度:98%
存储:Store at -20°C

Background:

HA-100 is a dechlorinated analogue of 1-(8-chloro-5-isoquinolinesulfonyl)piperazine (HA-156). HA-100 is an inhibitor of protein kinases (PKs) including PKA, PKC, and PKG [1].


Protein kinases are enzymes that can phosphorylate other proteins. Phosphorylation of proteins usually results in a functional change of the target protein (substrate) by changing enzyme activity, cellular location, or association with other proteins. Protein kinases operate in a large number of distinct signaling pathways, especially those involved in signal transduction. Protein kinases have also existed in bacteria and plant [2].


HA-100 inhibited the activity of PKA, PKC, and PKG with the IC50 values of 8, 12, and 4 μM, respectively. It showed less activity in blocking the activity of myosin light chain kinase with the IC50 of 240 μM [1]. HA-100 markedly decreased the affinity for MLC-kinase. HA-100 did not inhibit myosin light chain phosphorylation in platelets exposed to collagen significantly [1].


Reference:
[1] Hagiwara M, Inagaki M, Watanabe M, et al.  Selective modulation of calcium-dependent myosin phosphorylation by novel protein kinase inhibitors, isoquinolinesulfonamide derivatives[J]. Molecular pharmacology, 1987, 32(1): 7-12.
[2] Krebs E G.  Protein kinases[J]. Current topics in cellular regulation, 1972, 5: 99-133.