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Ro 31-8220 mesylate
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产品介绍
产品介绍
产品信息
抗原名称
PKCα ,PKCβ2 ,PKCβ1 ,PKCε ,PKCγ
商品描述
Ro 31-8220 mesylate (Bisindolylmaleimide IX) is a pan-PKC inhibitor with IC50 of 5 nM, 24 nM, 14 nM, 27 nM, and 24 nM for PKC-α, PKC-βI, PKC-βII, PKC-γ, and PKC-ε, respectively.
分子量
553.65
纯度
>98%
可溶性
DMSO : 55.4 mg/mL (100 mM)
Ethanol : 2.8 mg/mL (5 mM)
Ethanol : 2.8 mg/mL (5 mM)
外观
Powder
In vitro(体外研究)
Ro 31-8220 inhibits rat brain PKC activity with IC50 of 23 nM, and does not show any high degree of selectivity between PKC-α, PKC-β, PKC-γ, and PKC-ε. Ro 31-8220 also inhibits MSK1, MAPKAPK1, RSK, GSK3β and S6K1 with a potency similar to that for PKC. In addition, Ro 31-8220 inhibits voltage-dependent Na+ channels. Ro 31-8220 alters cellular protein kinase C localization and potently inhibits growth of A549 and MCF-7 cells with IC50 of 0.78 μM and 0.897 μM, respectively. RO 31-8220 enhances epinephrine-induced platelet aggregation in catecholamine hypo-responsive platelets by enhancing Akt phosphorylation. Ro 31-8220 significantly decreases apoE secretion from primary human macrophages by inhibiting vesicular transport of apoE to the plasma membrane without significantly affecting apoE mRNA or apoE protein levels.
In vivo(体内研究)
In MLP−/− Mice, Ro 31-8220 (6 mg/kg/d, s.c.) results in a significant increase in cardiac contractility.
背景
别名
Ro 31-8220 methanesulfonate; Bisindolylmaleimide IX mesylate,Ro318220
分子式
C25H23N5O2S·CH4O3S
CAS号
138489-18-6
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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