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GW779439X

Name: GW779439X
Brand: TargetMol
SKU: T8866
Price: 473 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 97.87%

货号 T8866Cas号 551919-98-3

GW779439X 属于吡唑并吡啶类，是一种金黄色葡萄球菌 PASTA 激酶 Stk1抑制剂。它是一种AURKA 抑制剂，可通过 caspases 3/7 诱导细胞凋亡。

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GW779439X

一键复制产品信息

很棒

纯度: 97.87%

货号 T8866Cas号 551919-98-3

GW779439X 属于吡唑并吡啶类，是一种金黄色葡萄球菌 PASTA 激酶 Stk1抑制剂。它是一种AURKA 抑制剂，可通过 caspases 3/7 诱导细胞凋亡。

规格	价格	库存
1 mg	¥ 473	现货
2 mg	¥ 688	现货
5 mg	¥ 1,130	现货
10 mg	¥ 1,890	现货
25 mg	¥ 3,180	现货
50 mg	¥ 4,690	现货
100 mg	¥ 6,690	现货
1 mL x 10 mM (in DMSO)	¥ 1,170	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

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纯度: 97.87%

颜色: 红色

性状: Solid

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资源下载:

COA LCMS HNMR 产品操作手册

产品介绍

GW779439X AI Summary

GW779439X exhibits significant and diverse bioactivity across various biological targets and assays. It potently inhibits CDK4 (IC50 = 6.0 nM), CDK2 (IC50 = 4.0 nM), and GSK3-beta (IC50 = 16.0 nM), and shows notable binding affinity for CDK4, GSK-3 beta, mTOR, and Pim1 with Kd values ranging from 4.5 nM to 63.0 nM. Additionally, it demonstrates high inhibition levels against human HepG2 cells, plasmodial strains (Plasmodium falciparum 3D7 and Dd2), and Mycobacterium tuberculosis PknB, with IC50 values ranging up to 1500.0 nM and Ki values, indicating strong immunomodulatory and antimicrobial potential. GW779439X also exhibits cytotoxic effects on human THP-1 cells (CC50 < 50.0 nM) and zebrafish embryos (0% survival at 5 uM). It possesses moderate lipophilicity with a logD value of 3.71 and demonstrates antitrypanosomal activity against Trypanosoma brucei brucei Lister 427 (EC50 = 15.85 nM). In assays involving thermal stability and protein stabilization, it interacts with CLK proteins, affecting their melting temperatures, which indicates potential modulation of splicing factors. Moreover, GW779439X has moderate effects in kinase inhibition assays including IKK-alpha, IKK-epsilon, Mer Kinase, PIP5K1, and TBK1, suggesting a broad kinase inhibitory profile. It also affects cell viability differentially across cell lines like HEK293T, human fibroblasts, and U2OS, indicating possibly complex, cell-type-specific growth interactions. Therefore, GW779439X represents a multifaceted bioactive agent with implications in kinase inhibition, antimicrobial activity, and potential therapeutic cytotoxicity, warranting further investigation for its various biological effects and therapeutic opportunities..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述

GW779439X is a pyrazolopyridazine compound that inhibits the S. aureus kinase Stk1 and Aurora kinase A (AURKA). It restores the efficacy of β-lactam antibiotics against methicillin-resistant (MRSA) and methicillin-susceptible (MSSA) S. aureus, often re-sensitizing resistant strains. This antibacterial potentiation is achieved through the induction of apoptosis via caspase-3/7 pathway activation.

化学信息

分子量	454.45
分子式	C₂₂H₂₁F₃N₈
CAS No.	551919-98-3
Smiles	CN1CCN(CC1)c1ccc(Nc2nccc(n2)-c2cnn3ncccc23)cc1C(F)(F)F
密度	no data available

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 4.55 mg/mL (10.01 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.2005 mL	11.0023 mL	22.0046 mL	110.0231 mL
5 mM	0.4401 mL	2.2005 mL	4.4009 mL	22.0046 mL
10 mM	0.2200 mL	1.1002 mL	2.2005 mL	11.0023 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。