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LY2228820

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Catalog No.
A5566
p38 MAP激酶抑制剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,200.00
现货
5mg
¥ 900.00
现货
25mg
¥ 3,600.00
现货
100mg
¥ 9,500.00
现货

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Background

LY2228820 is a potent, selective, ATP-competitive small-molecule inhibitor inhibiting α- and β-isoforms of p38 MAPK with IC(50) values of 5.3nM and 3.2 nM, respectively1.

In multiple myeloma (MM) cell lines, LY2228820 enhanced the cytotoxicity of bortezomiba via reducing bortezomib-induced phosphorylation of heat shock protein 27 (HSP27). LY2228820 significantly reduced IL-6 secretion from BM mononuclear cells (BMMNCs) and long term cultured-BM stromal cells (LT-BMSCs). Besides, LY2228820 can also inhibit secretion of macrophage inflammatory protein-1a (MIP-1a) in BMMNCs, CD138+ patient MM cells and normal CD14+ osteoclast cells 2.

Studies in mice implanted with B16-F10 melanoma showed that orally administered LY2228820 can effectively suppress the tumor-phospho-MK2 expression. Treatment of LY2228820 caused a significant tumor growth delay in A549 NSCLC xenograft models1.

References:
1. Campbell RM1, Anderson BD, Brooks NA, Brooks HB, Chan EM, De Dios A, Gilmour R, Graff JR, Jambrina E, Mader M, McCann D, Na S, Parsons SH, Pratt SE, Shih C, Stancato LF, Starling JJ, Tate C, Velasco JA, Wang Y, Ye XS.Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity. Mol Cancer Ther. 2014 Feb;13(2):364-74.
2. Ishitsuka K1, Hideshima T, Neri P, Vallet S, Shiraishi N, Okawa Y, Shen Z, Raje N, Kiziltepe T, Ocio EM, Chauhan D, Tassone P, Munshi N, Campbell RM, Dios AD, Shih C, Starling JJ, Tamura K, Anderson KC. p38 mitogen-activated protein kinase inhibitor LY2228820 enhances bortezomib-induced cytotoxicity and inhibits osteoclastogenesis in multiple myeloma; therapeutic implications. Br J Haematol. 2008 May;141(5):598-606.

文献引用

1.Jaco I, Annibaldi A, et al. "MK2 Phosphorylates RIPK1 to Prevent TNF-Induced Cell Death." Mol Cell. 2017 Jun 1;66(5):698-710.e5. PMID:28506461

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt612.74
Cas No.862507-23-1
FormulaC24H29FN6.2CH4O3S
Solubility≥30.65mg/mL in DMSO, ≥9.9 mg/mL in EtOH with ultrasonic, ≥45 mg/mL in H2O with ultrasonic
Chemical Name5-[2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)imidazo[4,5-b]pyridin-2-amine;methanesulfonic acid
SDFDownload SDF
Canonical SMILESCC(C)(C)CN1C2=C(C=CC(=N2)C3=C(N=C(N3)C(C)(C)C)C4=CC=C(C=C4)F)N=C1N.CS(=O)(=O)O.CS(=O)(=O)O
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验[1]:

细胞系

HeLa细胞

溶解方法

在DMSO中的溶解度大于30.7 mg/mL。为了获得更高的浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。

反应条件

9.8 nM-10 μM,1 h

应用

LY2228820是一个强效并且具有选择性的p38 MAPK α和β亚型的抑制剂,IC50分别为5.3和3.2 nmol/L。在茴香霉素刺激的HeLa细胞中,LY2228820有效抑制p38α MAPK底物MK2 (Thr334)的磷酸化。在小鼠腹腔巨噬细胞中,LY2228820减少LPS/IFN-γ诱导的TNF-α分泌。

动物实验[2]:

动物模型

雌性无胸腺裸鼠

剂量

口服给药,20和40 mg/kg,每天三次

应用

在无胸腺裸鼠中,LY2228820可减少血红蛋白的含量。在耳朵血管生成模型中,LY2228820处理导致VEGF-A刺激的血管形成显著减少,表明LY2228820处理使血管生成受到损伤。

注意事项

请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。

References:

[1]. Campbell R M, Anderson B D, Brooks N A, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity[J]. Molecular cancer therapeutics, 2014, 13(2): 364-374.

[2]. Tate C M, Blosser W, Wyss L, et al. LY2228820 dimesylate, a selective inhibitor of p38 mitogen-activated protein kinase, reduces angiogenic endothelial cord formation in vitro and in vivo[J]. Journal of Biological Chemistry, 2013, 288(9): 6743-6753.

生物活性

Description LY2228820是新型的和有效的p38 MAPK抑制剂,其IC50值为7 nM。
靶点 p38α          
IC50 7 nM          

质量控制

化学结构

LY2228820

相关生物数据

LY2228820

相关生物数据

LY2228820

相关生物数据

LY2228820