LY2228820

目录号: GC16835纯度: >99.50%同义词: 5-[2-(叔丁基)-4-(4-氟苯基)-1H-咪唑-5-基]-3-(2,2-二甲基丙基)-3H-咪唑并[4,5-B]吡啶-2-胺甲磺酸盐,LY2228820 dimesylate

A potent inhibitor of p38α MAP kinase

Cas No.: 862507-23-1

规格	价格	库存	数量
1mg	¥279.00	现货	1
5mg	¥684.00	现货	1
10mg	¥1,170.00	现货	1
50mg	¥2,610.00	现货	1
100mg	¥3,870.00	现货	1
10mM (in 1mL DMSO)	¥923.00	现货	1

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文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例

Nature
641, 529–536 (2025)
Nature
628, 630–638 (2024)
Nature
632, 686–694 (2024)
Nature
618, 1017–1023 (2023)
Nature
610, 366–372 (2022)
Cell
187(9):2288-2304 (2024)
Cell
183(7):1867-1883 (2020)
Science
388(6745) (2025)
Science
387(6739) (2025)
Science
387(6734) (2025)
Cell Research
35, 97–116 (2025)
Cell Research
34, 683–706 (2024)
Cell Research
33, 273–287 (2023)
Cell Research
33, 546–561 (2023)
Cell Research
33, 904–922 (2023)
Cell Research
31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment [1]:
Cell lines	HeLa cells
Preparation method	The solubility of this compound in DMSO is > 30.7 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.
Reacting condition	9.8 nM-10 µM, 1 h
Applications	LY2228820 is a potent and selective inhibitor of the α- and β-isoforms of p38 MAPK with IC50 values of 5.3 and 3.2 nmol/L, respectively. In anisomycin-stimulated HeLa cells, LY2228820 efficiently inhibited phosphorylation of p38α MAPK substrate, MK2 (Thr334). LY2228820 also decreased TNF-α secretion induced by LPS/IFN-γ in mouse peritoneal macrophages.
Animal experiment [2]:
Animal models	Athymic nude female mice
Dosage form	Oral administration, 20 and 40 mg/kg，three times daily
Application	LY2228820 reduced hemoglobin content in athymic nude mice. LY2228820 treatment resulted in a significant reduction of VEGF-A-stimulated vascularization in an ear angiogenesis model, indicating LY2228820 treatment impaired neoangiogenesis.
Other notes	Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.
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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号

862507-23-1

同义词

5-[2-(叔丁基)-4-(4-氟苯基)-1H-咪唑-5-基]-3-(2,2-二甲基丙基)-3H-咪唑并[4,5-B]吡啶-2-胺甲磺酸盐,LY2228820 dimesylate

化学名

5-[2-tert-butyl-4-(4-fluorophenyl)-1H-imidazol-5-yl]-3-(2,2-dimethylpropyl)imidazo[4,5-b]pyridin-2-amine;methanesulfonic acid

SMILES

CC(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

分子式

C₂₄H₂₉FN₆.2CH₄O₃S

分子量

612.74 g/mol

溶解性

≥ 30.65mg/mL in DMSO, ≥ 9.9 mg/mL in EtOH with ultrasonic, ≥ 45 mg/mL in Water with ultrasonic

保存条件

Store at -20°C

General tips

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。

Shipping Condition

评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

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