Go6976

别名: PD406976

目录号：S7119 Purity: 99.34%

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

规格	价格	库存
5mg	1615.81	现货
25mg	4053.02	现货
100mg	10565.1	现货
1g	40868.1	现货
更大包装有超大折扣
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产品质控

批次：纯度： 99.34%

99.34

Go6976相关产品

相关靶点	PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ PKCι	点击展开
相关产品	Go 6983 Sotrastaurin (AEB071) Enzastaurin Bisindolylmaleimide I (GF109203X) PMA (Phorbol 12-myristate 13-acetate) Bisindolylmaleimide IX (Ro 31-8220) Mesylate Ruboxistaurin (LY333531) HCl Rottlerin PKC-theta inhibitor Chelerythrine Chloride (NSC 646662) Darovasertib (LXS-196) Epsilon-V1-2 Dequalinium Chloride Myricitrin VTX-27 Chelerythrine	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

细胞实验数据示例

细胞系	实验类型	给药浓度	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

靶点

JAK2 ^[2] (Cell-free assay)	FLT3 ^[2] (Cell-free assay)	PKCα ^[1] (Cell-free assay)	PKCβ1 ^[1] (Cell-free assay)	PKC ^[1] (Rat brain)
		2.3 nM	6.2 nM	7.9 nM

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
激酶实验	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H_i，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.

参考文献
[1] Martiny-Baron G, er al. J Biol Chem. 1993, 268(13), 9194-9197. [2] Grandage VL, et al. Br J Haematol. 2006, 135(3), 303-316. [3] Qatsha KA, et al. Proc Natl Acad Sci U S A. 1993, 90(10), 4674-4678. [4] Duan GJ, et al. Inflamm Res. 2011, 60(4), 357-366. + 展开

参考文献

[4] Duan GJ, et al. Inflamm Res. 2011, 60(4), 357-366.

+ 展开

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)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1年-80°C溶于溶剂
储存条件(自收到货起)	3年-20°C粉状	储备液保存和期限建议分装储备液，避免反复冻融！	1个月-20°C溶于溶剂

体外溶解度
批次：

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

DMSO : 25 mg/mL ( (66.23 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

体内溶解度
批次：

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

摩尔浓度计算器

质量	浓度	体积	分子量
=	×	×

稀释计算器分子量计算器

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）

给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 μL 动物数量只

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）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

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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* 必填项

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