PKC-IN-1
目录号: PL09886 纯度: ≥98%
CAS No. :1046787-18-1
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中文名称
PKC-IN-1
中文别名
[(2S,5R)-2,5-二甲基-4-[(四氢-2H-吡喃-4-基)甲基]-1-哌嗪基][3-[(5-氟-2-甲基-4-嘧啶基)氨基]-4,6-二氢-6,6-二甲基吡咯并[3,4-c]吡唑-5(1H)-基]甲酮;[(2S,5R)-2,5-二甲基-4-[(四氢-2H-吡喃-4-基)甲基]-1-哌嗪基][3-[(5-氟-2-甲基-4-嘧啶基)氨基]-4,6-二氢-6,6-二甲基吡咯并[3,4-C]吡唑-5(1H)-基]甲酮;化合物PKC-IN-1
英文名称
PKC-IN-1
英文别名
PKC-IN-1;5-{[(2S,5R)-2,5-dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)piperazin-1-yl]carbonyl}-N-(5-fluoro-2-methylpyrimidin-4-yl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-amine;[(2S,5R)-2,5-Dimethyl-4-[(tetrahydro-2H-pyran-4-yl)methyl]-1-piperazinyl][3-[(5-fluoro-2-methyl-4-pyrimidinyl)amino]-4,6-dihydro-6,6-dimethylpyrrolo[3,4-c]pyrazol-5(1H)-yl]methanone;CS-2112;Methanone, [(2S,5R)-2,5-dimethyl-4-[(tetrahydro-2H-pyran-4-yl)methyl]-1-piperazinyl][3-[(5-fluoro-2-methyl-4-pyrimidinyl)amino]-4,6-dihydro-6,6-dimethylpyrrolo[3,4-c]pyrazol-5(1H)-yl]-
Cas No.
1046787-18-1
分子式
C25H37FN8O2
分子量
500.61
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PKC-IN-1 是一种有效的,ATP-竞争性的,可逆的 PKC 抑制剂,对人 PKCβ 和 PKCα 的 Ki 值分别为 5.3 和 10.4 nM,对人 PKCα,PKCβI,PKCβII,PKCθ,PKCγ,PKC mu 和 PKCε 的 IC50 值分别为 2.3,8.1,7.6,25.6,57.5,314,808 nM。
生物活性
PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with K i s of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC 50 s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.
性状
Solid
IC50 & Target[1][2]
Human PKCα 2.3 nM (IC50) Human PKCβII 7.6
体外研究(In Vitro)
PKC-IN-1 (Compound A) is a potent, ATP-competitive and reversible of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PKC-IN-1 (Compound A; 15 and 30 mg/kg, p.o., bid (twice a day)) dose-dependently and significantly reduces maximum EAE severity and end severity in autoimmune encephalitis (EAE) model in Lewis rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
参考文献
[1]. Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1.
溶解度数据
In Vitro: DMSO : ≥ 25 mg/mL (49.94 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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