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MK2-IN-3

Name: MK2-IN-3
Brand: TargetMol
SKU: T9034
Price: 316 CNY
Availability: InStock
Rating: 5 (10 reviews)

Synonyms: MK2 Inhibitor III

货号 T9034Cas号 724711-21-1 一键复制产品信息纯度: 99.01%

很棒

MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM)，能够抑制 U937 细胞及体内 TNFα 的生成。

MK2-IN-3

一键复制产品信息

很棒

纯度: 99.01%

货号 T9034Cas号 724711-21-1

别名 MK2 Inhibitor III

MK2-IN-3 (MK2 Inhibitor III) 是选择性的 MAPKAP-K2 (MK-2)抑制剂(IC50:8.5 nM)，能够抑制 U937 细胞及体内 TNFα 的生成。

规格	价格	库存
1 mg	¥ 316	现货
5 mg	¥ 708	现货
10 mg	¥ 1,180	现货
25 mg	¥ 2,020	现货
50 mg	¥ 2,920	现货
100 mg	¥ 4,190	现货
200 mg	¥ 5,650	现货
1 mL x 10 mM (in DMSO)	¥ 533	现货

库存状态实时更新，以官网显示为准，现货产品可直接加购物车下单

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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

选择批次:

纯度: 99.01%

颜色: 白色

性状: Solid

资源下载: COA LCMS HNMR 产品操作手册

产品介绍

MK2-IN-3 AI Summary

MK2-IN-3 is a multifunctional kinase inhibitor with notable bioactivities. It shows strong inhibitory activity against MK2, MK3, MK5, and ERK2, with IC50 values ranging from 8.5 to 3440.0 nM but has lower activity against MNK1 and TNFalpha production in U937 cells and poor activity against kinases such as p38alpha, JNK2, IKK2, CDK2, MSK1, and MSK2 (IC50 values > 200,000 nM). In detailed bioactivity assays, it inhibits human recombinant MK2 with an IC50 of 8.5 nM and shows an EC50 of 49.0 nM. Further, it possesses a permeability of 6.0 nm/s by PAMPA and 5.0 nm/s across human Caco-2 cells, with a kinetic solubility of 0.0 μg/mL at pH 7.4. The compound has a short half-life in human (0.5833 hr) and rat (0.6667 hr) liver microsomes, with a high plasma protein binding of 99.7%. In an in vivo rat acute model of inflammation, MK2-IN-3 demonstrates a 20.0% inhibition at a 20 mg/kg dose one hour before an LPS challenge, though less effective (0.1%) when administered two hours prior. It also shows anti-inflammatory activity in human THP1 cells showing 38.0% inhibition of LPS-induced TNFalpha production at 10 µM. Overall, MK2-IN-3 demonstrates diverse kinase inhibitory activities, with particularly high potency against MK2, and a significant but varying anti-inflammatory effect..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	MK2-IN-3 (MK2 Inhibitor III) is a potent, cell-permeable inhibitor of mitogen-activated protein kinase-activated protein kinase 2 (MAPKAP-K2 or MK-2) and can be used for the treatment of rheumatoid arthritis
靶点活性	ERK2:3.44 μM (IC50), MNK1:5.7 μM (IC50), MK3:210 nM (IC50), MK2:8.5 nM (IC50), MK5:81 nM (IC50)
别名	MK2 Inhibitor III

化学信息

分子量	340.38
分子式	C₂₁H₁₆N₄O
CAS No.	724711-21-1
Smiles	O=C1NCCc2[nH]c(cc12)-c1ccnc(c1)-c1cnc2ccccc2c1
密度	1.318 g/cm3 (Predicted)

储存&溶解度

存储

溶解度信息

DMSO: 9 mg/mL (26.44 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.9379 mL	14.6895 mL	29.3789 mL	146.8946 mL
5 mM	0.5876 mL	2.9379 mL	5.8758 mL	29.3789 mL
10 mM	0.2938 mL	1.4689 mL	2.9379 mL	14.6895 mL
20 mM	0.1469 mL	0.7345 mL	1.4689 mL	7.3447 mL

该溶液配制表仅适用于固体产品。对于液体产品，请根据标明的浓度或密度计算稀释方案。

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。