Ralimetinib(Synonyms: LY2228820)

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Ralimetinib (Synonyms: LY2228820)

Ralimetinib (LY2228820) 是一种有效、选择性、ATP-竞争性的 p38 MAPK α/β 抑制剂,IC50 值分别为 5.3 和 3.2 nM。Ralimetinib (LY2228820) 选择性地抑制 MK2 (Thr334) 磷酸化,但对 p38α MAPK,JNK,ERK1/2,c-Jun,ATF2 或 c-Myc 的磷酸化水平无作用。

Ralimetinib(Synonyms: LY2228820)

Ralimetinib Chemical Structure

CAS No. : 862505-00-8

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Ralimetinib 的其他形式现货产品:

Ralimetinib dimesylate

生物活性

Ralimetinib (LY2228820) is a potent and selective, ATP-competitive inhibitor of p38 MAPK α/β, with IC50s of 5.3 and 3.2 nM, respectively. Ralimetinib (LY2228820) selectively inhibits phosphorylation of MK2 (Thr334), with no effect on phosphorylation of p38α MAPK, JNK, ERK1/2, c-Jun, ATF2, or c-Myc[1].

IC50 & Target[1]

p38β MAPK

3.2 nM (IC50)

p38α MAPK

5.3 nM (IC50)

Clinical Trial

分子量

420.53

Formula

C24H29FN6

CAS 号

862505-00-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Campbell RM, et al. Characterization of LY2228820 dimesylate, a potent and selective inhibitor of p38 MAPK with antitumor activity. Mol Cancer Ther. 2014 Feb;13(2):364-74.

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