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WM-1119

产品编号 T4679 CAS 2055397-28-7

别名: WM1119

WM-1119 是一种强选择性KAT6A 抑制剂，在淋巴瘤细胞中测得对 KAT6A 的IC50值为 0.25 μM，对 KAT6A，KAT5和KAT7 的结合KD 值分别为 2 nM、2.2 μM 和0.5 μM。

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WM-1119, CAS 2055397-28-7

规格	价格/CNY	货期
1 mg	￥ 221	现货
5 mg	￥ 493	现货
10 mg	￥ 659	现货
25 mg	￥ 1,230	现货
50 mg	￥ 1,930	现货
100 mg	￥ 3,720	现货
500 mg	￥ 7,880	现货
1 mL * 10 mM (in DMSO)	￥ 530	现货

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纯度: 96.59%

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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	WM-1119 is a highly potent, selective KAT6A/B inhibitor
靶点活性	KAT5:2.2 μM(KD), KAT7:0.5 μM(KD), KAT6A:0.25 μM, KAT6A:2 nM(KD)
体外活性	WM-1119 induces cell cycle exit and cellular senescence without causing DNA damage. WM-1119 is 1,100-fold and 250-fold more active against KAT6A than against KAT5 or KAT7, respectively, and so shows greater specificity for KAT6A than does WM-8014. The testing of WM-1119 at 1 μM and 10 μM against a pharmacological panel of 159 diverse biological targets reveal no affinity. Treatment of MEFs with WM-1119 results in cell cycle arrest in G1 and a senescence phenotype similar to that seen upon treatment with WM-8014. Notably, the activity of WM-1119 in this cell-based assay is an order of magnitude greater than WM-8014 and WM-1119 is able to induce cell cycle arrest at 1 μM. Treatment with WM-8014 or WM-1119 inhibits the proliferation of the EMRK1184 lymphoma cells in vitro, WM-1119 (IC50=0.25 μM) is ninefold more active than WM-8014 (IC50=2.3 μM), as expected on the basis of reduced protein binding
体内活性	Male C57BL/6-albino (B6(Cg)-Tyrc-2J/J) mice are injected intravenously with 100,000 EMRK1184 cells transfected with a luciferase-expression construct. Lymphoma growth is monitored. Three days after the lymphomacell transplant, all mice show luciferase activity, which indicate the expansion of lymphoma cells. Mice are then divided randomly into WM-1119-treatment with different conentrations (1, 2.5, 5, 10 μM) and vehicle-control groups. Because WM-1119 is rapidly cleared after intraperitoneal injection, with the plasma concentration decreasing to below 1 μM after 4-6 h cohorts of mice are injected every 8 h (three times per day, two cohorts of three mice per treatment group) or every 6 h (four times per day, two cohorts of three and six mice per treatment group).By day 14, the cohorts that are treated four times per day with WM-1119 have arrested tumour growth, with the exception of one mouse that does not respond. Spleen weights in the WM-1119-treatment group (treated four times per day) are substantially lower than spleen weights in the vehicle-treated group, and not significantly different from those of tumour-free eight-weekold mice. Treatment with WM-1119 three times per day leads to a significant reduction in tumour burden and spleen weight, but is not as effective as treatment four times per day. WM-1119 is well-tolerated; mice show no generalized ill effects and weight loss is not observed. WM-1119 treatment has no effect on haematocrit, erythrocytes or platelet numbers, but there is overall leukopenia. The proportion and overall number of tumour cells is substantially reduced by WM-1119 treatment (four times per day).
动物实验	Male C57BL/6-albino (B6(Cg)-Tyrc-2J/J) mice are injected intravenously with 100,000 EMRK1184 cells transfected with a luciferase-expression construct. Lymphoma growth is monitored. Three days after the lymphomacell transplant, all mice show luciferase activity, which indicate the expansion of lymphoma cells. Mice are then divided randomly into WM-1119-treatment with different conentrations (1, 2.5, 5, 10 μM) and vehicle-control groups. Because WM-1119 is rapidly cleared after intraperitoneal injection, with the plasma concentration decreasing to below 1 μM after 4-6 h cohorts of mice are injected every 8 h (three times per day, two cohorts of three mice per treatment group) or every 6 h (four times per day, two cohorts of three and six mice per treatment group).By day 14, the cohorts that are treated four times per day with WM-1119 have arrested tumour growth, with the exception of one mouse that does not respond. Spleen weights in the WM-1119-treatment group (treated four times per day) are substantially lower than spleen weights in the vehicle-treated group, and not significantly different from those of tumour-free eight-weekold mice. Treatment with WM-1119 three times per day leads to a significant reduction in tumour burden and spleen weight, but is not as effective as treatment four times per day. WM-1119 is well-tolerated; mice show no generalized ill effects and weight loss is not observed. WM-1119 treatment has no effect on haematocrit, erythrocytes or platelet numbers, but there is overall leukopenia. The proportion and overall number of tumour cells is substantially reduced by WM-1119 treatment (four times per day).

别名	WM1119
分子量	389.38
分子式	C18H13F2N3O3S
CAS No.	2055397-28-7

存储

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

溶解度

DMSO: 150 mg/mL (385.23 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	2.5682 mL	12.8409 mL	25.6819 mL	64.2046 mL
	5 mM	0.5136 mL	2.5682 mL	5.1364 mL	12.8409 mL
	10 mM	0.2568 mL	1.2841 mL	2.5682 mL	6.4205 mL
	20 mM	0.1284 mL	0.642 mL	1.2841 mL	3.2102 mL
	50 mM	0.0514 mL	0.2568 mL	0.5136 mL	1.2841 mL
	100 mM	0.0257 mL	0.1284 mL	0.2568 mL	0.642 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)

溶液体积

质量

配液浓度

参考文献

1. Baell JB et al. Inhibitors of histone acetyltransferases KAT6A/B induce senescence and arrest tumour growth. Nature. 2018 Aug;560(7717):253-257.

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

WM-1119 2055397-28-7 Chromatin/Epigenetic Histone Acetyltransferase WM 1119 HATs HAT Inhibitor inhibit WM1119 inhibitor

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WM-1119

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