LY243246

价格：询价

品牌：MedChemExpress(MCE) 品牌认证

货号：HY-117058

产品详情

LY243246

CAS No. : 106400-18-4

MCE 国际站：LY243246

产品活性：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。

研究领域：Cell Cycle/DNA Damage

作用靶点：Antifolate

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: K_m=7.1 and 9.3 μM for mouse liver folylpolyglutamate synthetase, respectively).
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.