LY243246(Synonyms: (6S)-DDATHF)

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LY243246 (Synonyms: (6S)-DDATHF)

LY243246 ((6S)-DDATHF) 是 DDATHF 的 6S 非对映异构体,是一种有效的 5′-磷酸核糖基甘氨酰胺甲酰基转移酶 ((GAR transformylase)) 的竞争性抑制剂。6R- 和 6S-DDATHF 非对映异构体是非常相似和等效的抗代谢物,可抑制从头生物嘌呤化学合成。

LY243246(Synonyms: (6S)-DDATHF)

LY243246 Chemical Structure

CAS No. : 106400-18-4

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生物活性

LY243246 ((6S)-DDATHF), the 6S diastereomer of DDATHF, is a potent competitive inhibitor of 5’-phosphoribosylglycinamide formyltransferase (GAR transformylase). 6R- and 6S-diastereomers of DDATHF are remarkably similar and equiactive antimetabolites inhibitory to de novo purine synthesis[1].

体外研究
(In Vitro)

LY243246 ((6S)-DDATHF) is a growth inhibitor of mouse L1210 leukemia cells (IC50=29 nM). Both diastereomers of DDATHF are found to be efficient substrates for folylpolyglutamate synthetase of both mouse and human origin (6R- and 6S-diastereomers of DDATHF: Km=7.1 and 9.3 μM for mouse liver folylpolyglutamate synthetase, respectively)[1].
Both the 6R and 6S diastereomers of DDATHF are also cytotoxic to mammalian cells in a stereospecific manner. The cytotoxic potency of (6R)-DDATHF towards different cell lines varied by approximately 14-fold and that of (6S)-DDATHF by as much as 156-fold. Compared to (6R)-DDATHF, (6S)-DDATHF is 6.0- and 7.2-fold more cytotoxic to human WiDr colon adenocarcinoma and Chinese hamster ovary (CHO) cells, respectively, and only 1.5- and 2.0-fold more cytotoxic to human T24 bladder carcinoma and mouse L1210 leukemia cells, respectively. However, compared to (6S)-DDATHF, (6R)-DDATHF was 8.7- and 6.9-fold more cytotoxic to C3H/10T1/2 clone 8 and clone 16 mouse fibroblasts, respectively[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

443.45

Formula

C21H25N5O6

CAS 号

106400-18-4

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]. Moran RG, et al. The 6S- and 6R-diastereomers of 5, 10-dideaza-5, 6, 7, 8-tetrahydrofolate are equiactive inhibitors of de novo purine synthesis. J Biol Chem. 1989;264(35):21047-21051.

    [2]. Lehman NL. The stereospecific cytotoxic potency of (6R) and (6S)-5,10- dideazatetrahydrofolate correlates with cellular folylpolyglutamate synthetase levels. Biochimie. 1995;77(4):273-278.

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