Go6976

別名: PD406976

目錄號(hào)：S7119 Purity: 99.34%

Go6976 (PD406976)是一種強(qiáng)效的PKC抑制劑，其對(duì)PKC (老鼠大腦), PKCα, and PKCβ1的IC50分別為7.9nM，2.3 nM, 和 6.2 nM 。此外，也是JAK2 和 Flt3的強(qiáng)抑制劑。

Go6976 Chemical Structure

CAS: 136194-77-9

規(guī)格	價(jià)格	庫(kù)存
5mg	1615.81	現(xiàn)貨
25mg	4053.02	現(xiàn)貨
100mg	10565.1	現(xiàn)貨
1g	40868.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.34%

99.34

Go6976相關(guān)產(chǎn)品

相關(guān)靶點(diǎn)	PKCα PKCβ PKCγ PKCδ PKCε PKCζ PKCη PKCθ PKCι	點(diǎn)擊展開(kāi)
相關(guān)產(chǎn)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	點(diǎn)擊展開(kāi)
相關(guān)化合物庫(kù)	激酶抑制劑庫(kù) PI3K/Akt 抑制劑庫(kù) MAPK抑制劑庫(kù) 細(xì)胞周期化合物庫(kù) TGF-beta/Smad信號(hào)通路庫(kù)	點(diǎn)擊展開(kāi)

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系	實(shí)驗(yàn)類(lèi)型	給藥濃度	活性描述	文獻(xiàn)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
點(diǎn)擊查看更多細(xì)胞系數(shù)據(jù)

生物活性

產(chǎn)品描述

靶點(diǎn)

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

體外研究(In Vitro)
體外研究活性	Go6976對(duì)Ca(2+)不依賴性PKC亞型δ，ε，和ζ的激酶活性沒(méi)有作用。^[1]除了WT JAK2，Go6976也會(huì)抑制突變型血液惡性腫瘤(JAK2 V617F 和 TEL-JAK2)，且具有抗突變型FLT3的活性。在AML細(xì)胞中，Go6976將FLT3-ITD樣品中的存活率降低到對(duì)照組的55%，F(xiàn)LT3-WT樣品中降低為69%。^[2] Go 6976有效抑制苔蘚抑素1，腫瘤壞死因子α和白細(xì)胞介素6誘導(dǎo)的HIV-1。^[3]
激酶實(shí)驗(yàn)	PKC 活性試驗(yàn)
激酶實(shí)驗(yàn)	簡(jiǎn)而言之，對(duì)于測(cè)量大鼠腦中的PKCα，PKCβ1 和 PKC，200 μl試驗(yàn)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 二硫蘇糖醇，1 μg 磷脂酰絲氨酸，0.2 μg 二油精，40 μg 組蛋白H_i，10 μM [γ-³²P]ATP (1 μCi/ml)，和5-10 單位 (pmol of Pi/min) PKC。加入[γ-³²P]ATP開(kāi)始測(cè)定，在30℃下培養(yǎng)5分鐘，加入2 ml 8.5% H₃PO₄停止測(cè)定，通過(guò)0.45-μm硝化纖維素過(guò)濾器過(guò)濾，并使用閃爍計(jì)數(shù)器進(jìn)行評(píng)估。
細(xì)胞實(shí)驗(yàn)	細(xì)胞系	原代 AML 細(xì)胞
	濃度	1 μM
	孵育時(shí)間	48小時(shí)
	方法	細(xì)胞以2×10⁵每點(diǎn)懸浮在200 μl RPMI/10% FCS。研究下的抑制劑以近似濃度加入，細(xì)胞在37℃，5% CO₂下培養(yǎng)48小時(shí)。MTS活性通過(guò)CellTiter試劑盒根據(jù)制造商說(shuō)明進(jìn)行測(cè)量。結(jié)果表示為對(duì)照組(沒(méi)有抑制劑的細(xì)胞組)的百分比。
實(shí)驗(yàn)圖片	檢測(cè)方法	檢測(cè)指標(biāo)	實(shí)驗(yàn)圖片	PMID
	Western blot	p-EGFR / EGFR / p-AKT / AKT / p-ERK / ERK / p-S6 / S6		23229345
	Immunofluorescence	p62 / LAMP2		29794026

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	Go6976 (2.5 mg/kg i.p.)，作為PKD抑制劑，通過(guò)抑制MAPKs活化作用以減少TNF-α產(chǎn)生，而有效防止LPS/D:-GalN誘導(dǎo)的急性肝損傷，并顯著提高LPS/D-GalN攻擊的小鼠的存活率。^[4]
動(dòng)物實(shí)驗(yàn)	Animal Models	LPS/D-GalN-攻擊的小鼠
	Dosages	2.5 mg/kg
	Administration	i.p.

參考文獻(xiàn)
[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. + 展開(kāi)

參考文獻(xiàn)

[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.

+ 展開(kāi)

化學(xué)信息&溶解度

分子量	377.42	分子式	C₂₄H₁₈N₄O
CAS號(hào)	136194-77-9	SDF	Download Go6976 SDF
Smiles	CN1C2=CC=CC=C2C3=C4C(=C5C6=CC=CC=C6N(C5=C31)CCC#N)CNC4=O
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1年-80°C溶于溶劑
儲(chǔ)存條件(自收到貨起)	3年-20°C粉狀	儲(chǔ)備液保存和期限建議分裝儲(chǔ)備液，避免反復(fù)凍融！	1個(gè)月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 44.7 mg/mL ( (118.43 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 25 mg/mL ( (66.23 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計(jì)算器分子量計(jì)算器

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

給藥劑量 mg/kg 動(dòng)物平均體重 g 每只動(dòng)物給藥體積 μL 動(dòng)物數(shù)量只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH₂O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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