Go6976
别名: PD406976
Go6976 (PD406976)是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。
Go6976 Chemical Structure
CAS: 136194-77-9
客户使用Selleck的Go6976发表文献33篇
产品质控
Go6976相关产品
| 相关靶点 | PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ PKCι | 点击展开 |
|---|---|---|
| 相关化合物库 | 激酶抑制剂库 PI3K/Akt 抑制剂库 MAPK抑制剂库 细胞周期化合物库 TGF-beta/Smad信号通路库 | 点击展开 |
相关信号通路图
PKC抑制剂选择性比较
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| primary microglial cells | Function assay | 1.3 uM | Suppression of IFN-gamma-induced PKCalpha/beta2 nuclear translocation in Sprague-Dawley rat primary microglial cells at 1.3 uM by Western blotting | 17395590 | |
| primary microglial cells | Function assay | 1.3 uM | Suppression of IFN-gamma-induced IFN-gamma regulatory factor 1 nuclear translocation in Sprague-Dawley rat primary microglial cells at 1.3 uM by Western blotting | 17395590 | |
| Vero | Cytotoxicity assay | Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability measured on day 5 post dose by MTS/PMS based microscopic analysis, CC50=6μM. | 28689975 | ||
| primary microglial cells | Function assay | Inhibition of IFN-gamma-induced IFN-gamma regulatory factor levels in Sprague-Dawley rat primary microglial cells by Western blotting | 17395590 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells | 29435139 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| MG 63 (6-TG R) | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells | 29435139 | ||
| NB1643 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB1643 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for A673 cells) | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-MC cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for NB-EBc1 cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for BT-37 cells | 29435139 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for TC32 cells | 29435139 | ||
| U-2 OS | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for U-2 OS cells | 29435139 | ||
| Rh41 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells | 29435139 | ||
| Saos-2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Saos-2 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for OHS-50 cells | 29435139 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SK-N-SH cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Go6976 (PD406976)是一种强效的PKC抑制剂，其对PKC (老鼠大脑), PKCα, and PKCβ1的IC50分别为7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的强抑制剂。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Go6976对Ca(2+)不依赖性PKC亚型δ，ε，和ζ的激酶活性没有作用。[1]除了WT JAK2，Go6976也会抑制突变型血液恶性肿瘤(JAK2 V617F 和 TEL-JAK2)，且具有抗突变型FLT3的活性。在AML细胞中，Go6976将FLT3-ITD样品中的存活率降低到对照组的55%，FLT3-WT样品中降低为69%。[2] Go 6976有效抑制苔藓抑素1，肿瘤坏死因子α和白细胞介素6诱导的HIV-1。[3] | |||
|---|---|---|---|---|
| 激酶实验 | PKC 活性试验 | |||
| 简而言之，对于测量大鼠脑中的PKCα，PKCβ1 和 PKC，200 μl试验混合物包含50 mM HEPES (pH7.5)，5 mM MgCl2，1 mM EDTA，1.25 mM EGTA，1.32 mM CaC12，1 mM 二硫苏糖醇，1 μg 磷脂酰丝氨酸，0.2 μg 二油精，40 μg 组蛋白Hi，10 μM [γ-32P]ATP (1 μCi/ml)，和5-10 单位 (pmol of Pi/min) PKC。加入[γ-32P]ATP开始测定，在30℃下培养5分钟，加入2 ml 8.5% H3PO4停止测定，通过0.45-μm硝化纤维素过滤器过滤，并使用闪烁计数器进行评估。 | ||||
| 细胞实验 | 细胞系 | 原代 AML 细胞 | ||
| 浓度 | 1 μM | |||
| 孵育时间 | 48小时 | |||
| 方法 | 细胞以2×105每点悬浮在200 μl RPMI/10% FCS。研究下的抑制剂以近似浓度加入，细胞在37℃，5% CO2下培养48小时。MTS活性通过CellTiter试剂盒根据制造商说明进行测量。结果表示为对照组(没有抑制剂的细胞组)的百分比。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | p-EGFR / EGFR / p-AKT / AKT / p-ERK / ERK / p-S6 / S6 |
|
23229345 | |
| Immunofluorescence | p62 / LAMP2 |
|
29794026 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Go6976 (2.5 mg/kg i.p.)，作为PKD抑制剂，通过抑制MAPKs活化作用以减少TNF-α产生，而有效防止LPS/D:-GalN诱导的急性肝损伤，并显著提高LPS/D-GalN攻击的小鼠的存活率。[4] | |
|---|---|---|
| 动物实验 | Animal Models | LPS/D-GalN-攻击的小鼠 |
| Dosages | 2.5 mg/kg | |
| Administration | i.p. | |
化学信息&溶解度
| 分子量 | 377.42 | 分子式 | C24H18N4O |
| CAS号 | 136194-77-9 | SDF | Download Go6976 SDF |
| Smiles | CN1C2=CC=CC=C2C3=C4C(=C5C6=CC=CC=C6N(C5=C31)CCC#N)CNC4=O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 44.7 mg/mL ( (118.43 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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