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GS-444217

产品编号 T5190 CAS 1262041-49-5

别名: GS 444217, GS444217

GS-444217 是一种可口服的选择性 ATP 竞争性凋亡信号调节激酶 1 抑制剂，IC50为 2.87 nM。

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GS-444217, CAS 1262041-49-5

规格	价格/CNY	货期
1 mg	￥ 872	现货
5 mg	￥ 2,390	现货
10 mg	￥ 3,490	现货
25 mg	￥ 5,690	现货
50 mg	￥ 7,960	现货
100 mg	￥ 10,700	现货
1 mL * 10 mM (in DMSO)	￥ 2,630	现货

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纯度: 99.58%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	GS-444217 is a selective ATP-competitive inhibitor of apoptosis signal-regulating kinase 1 (ASK1, IC50: 2.87 nM).
靶点活性	ASK1:2.87 nM (cell free)
体外活性	GS-444217 demonstrated high selectivity for binding to ASK1 versus the other kinases in the panel. The affinity of GS-444217 for ASK1 (KD = 4.1 nM) was 53-fold greater than the affinity for DYRK1A (KD = 220 nM) and 104-fold greater than the affinity for RSK4 (KD = 430 nM). Treatment with GS-444217 reduced ASK1 phosphorylation and prevented the phosphorylation of MKK3/6, MKK4, p38, and JNK at concentrations of 0.3 μM and above with full suppression of ASK1 activity at 1 μM. GS-444217 reduced ASK1 activity within 5 minutes of addition to the cultures, reaching a maximum level of inhibition by 30 minutes. Removal of GS-444217 from the cultures resulted in reactivation of ASK1 autophosphorylation within 10 minutes and near-complete recovery 2 hours after drug washout [1].
体内活性	Treatment with GS-444217 abrogated p38 MAPK activation in diabetic kidneys but had no effect upon hypertension in Nos3(-/-) mice. Early intervention with GS-444217 significantly inhibited diabetic glomerulosclerosis and reduced renal dysfunction but had no effect on the development of albuminuria. Late intervention with GS-444217 improved renal function and halted the progression of glomerulosclerosis, renal inflammation, and tubular injury despite having no effect on established albuminuria [2]. One dose of GS-444217 (30 mg/kg) given 30 minutes before administration of auranofin (30 mg/kg) suppressed the activation of ASK1, p38, and JNK in renal cortex. Auranofin administration induced mRNA expression of inflammatory cytokines (Il1b, Ccl2, and Cxcl2) and increased caspase activity in the kidney, and these downstream effects of ASK1 activation were inhibited by GS-444217. Comparing plasma concentrations of GS-444217 with the corresponding phosphorylated p38 (p-p38) signal in kidney, GS-444217 had an in vivo EC50 of approximately 1.6 μM for inhibiting the ASK1 pathway in rodent kidney [1].
细胞实验	Human embryonic kidney cells (HEK293T) were infected with full-length human ASK1 adenovirus or with an inactive truncated ASK1 adenovirus (K709R mutant with N-terminally truncated protein) as a negative control using the following conditions: (a) dose response: cells were infected for 24 hours followed by incubation for 2 hours with 0.001, 0.003, 0.01, 0.03, 0.1, 0.3, 1, 3, and 10 μM GS-444217; (b) kinetics: after cells were infected for 24 hours, 1 μM GS-444217 was added to cells for 1, 5, 10, or 30 minutes or 1, 2, or 4 hours; (c) off-rate kinetics: cells were infected for 24 hours followed by incubation with GS-444217 for 30 minutes. After 30 minutes, medium was replaced with serum-free medium without compound and incubated for 0, 10, or 30 minutes or 1, 2, or 4 hours [1].
动物实验	Male Sprague-Dawley rats (176–200 g, 7–8 weeks old) were randomly assigned to weight-matched treatment groups: (a) sham procedure, n = 8; (b) ischemia 30 minutes, n = 8; (c) ischemia 30 minutes plus GS-444217 (30 mg/kg, p.o.), n = 8. Bilateral renal occlusion was performed on anesthetized rats held at 37°C for 30 minutes. After recovering from anesthesia, rats were placed in metabolic cages for a 24-hour collection of urine. Sham rats underwent midline incision with surgery duration of 30 minutes but were not subjected to occlusion. Necropsy was performed on all rats 24 hours after surgery to collect kidneys and blood. Renal I/R studies were performed at Physiogenix Inc. Serum was analyzed for creatinine and blood urea nitrogen concentrations on a clinical chemistry analyzer. The right kidney was fixed in formalin and stained with H&E to assess tubular necrosis by pathology and with TUNEL to detect apoptotic cells [1].

别名	GS 444217, GS444217
分子量	411.46
分子式	C23H21N7O
CAS No.	1262041-49-5

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 55 mg/mL (133.67 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.4304 mL	12.1518 mL	24.3037 mL	60.7592 mL
	5 mM	0.4861 mL	2.4304 mL	4.8607 mL	12.1518 mL
	10 mM	0.243 mL	1.2152 mL	2.4304 mL	6.0759 mL
	20 mM	0.1215 mL	0.6076 mL	1.2152 mL	3.038 mL
	50 mM	0.0486 mL	0.243 mL	0.4861 mL	1.2152 mL
	100 mM	0.0243 mL	0.1215 mL	0.243 mL	0.6076 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

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

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参考文献

1. Liles JT, et al. ASK1 contributes to fibrosis and dysfunction in models of kidney disease. J Clin Invest. 2018 Oct 1;128(10):4485-4500. 2. Tesch GH, et al. ASK1 Inhibitor Halts Progression of Diabetic Nephropathy in Nos3-Deficient Mice. Diabetes. 2015 Nov;64(11):3903-13.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

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5% DMSO+30% PEG300+5% Tween 80+60% 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 50 μL DMSO (母液浓度为 40 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。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GS-444217 1262041-49-5 Apoptosis MAPK ASK GS 444217 GS444217 inhibit MAP kinase kinase kinase, MEKK, MAPKKK MAP3K Inhibitor inhibitor

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GS-444217

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

相关产品

相关化合物库

剂量换算

体内实验配液计算器

技术支持

Keywords