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PRGL493

CAS No. : 2479378-45-3

MCE 站：PRGL493

产品活性：PRGL493 是一种高效、选择性的长链酰基辅酶 a 合成酶 4 (ACSL4) 抑制剂。PRGL493 在乳腺和前列腺细胞及动物模型中均可阻断细胞增殖和肿瘤生长。PRGL493 用于癌症研究。

研究领域：Others

作用靶点：Others

In Vitro: Acyl-CoA synthetase 4 (ACSL4) is an isoenzyme of the fatty acid ligase-coenzyme-A family taking part in arachidonic acid metabolism ａnd steroidogenesis.
PRGL493 ([³H]-AA (0.5 µCi/ml in serumfree medium) for 3 h; 48 hours) signifcantly inhibits the activity of ACSL4 in all three cell lines (MDA-MB-231, PC-3 ａnd MA-10 Leydig cells), as evidenced by a reduction in AA-CoA levels.But PRGL493 has no effects on ACSL4 protein expression.
PRGL493 (20-100 μM; 72 hours) inhibits the proliferation of highly aggressive breast ａnd prostate cancer cells at an IC₅₀ of 23 µM ａnd 27 µM, respectively.

In Vivo: PRGL493 (intraperitoneal injection; 250 μg/Kg; 43 ａnd 34 consecutive days) decreases tumor volumes ａnd inhibits tumor growth. Additionally, this compound results in a decrease in Ki67 protein expression ａnd increases ER ａnd AR expression in breast ａnd prostate xenograft tumors, respectively.

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