ICRF-193 

ICRF-193 is a DNA Topoisomerase II inhibitor. (S,S)- and (R,R)-isomers ICRF-193 make up an racemic mixture, ICRF-196 (HY-118590A). ICRF-193 can inhibit DNA syntheses and induces apoptosis. ICRF-193 exhibits anti-cancer and anti-inflammation effects. ICRF-193 shows cardioprotective effect against anthracycline toxicity to cardiomyocytes. ICRF-193 can be used for the researches of cancer, infection, inflammation and cardiovascular disease, such as acute promyelocytic leukemia^{[1][2][3][4][5][6]}.

ICRF-193 (10-100 μM, 2 h) 会在表达组蛋白 H2A-RFP、α-微管蛋白 Atb2-GFP 和纺锤体极体蛋白 Sid4-GFP 的裂殖酵母细胞中诱导有丝分裂缺陷^[1]。
ICRF-193 (100 μM. 2 h) 会抑制其自身诱导的纺锤体断裂，并在裂殖酵母细胞中诱导染色体分离不均等^[1]。
ICRF-193 (100 μM, 4 h) 会改变 cdc11-123 裂殖酵母突变体的核形态和 DNA 含量^[1]。
ICRF-193 (100 μM, 8 h) 会降低野生型裂殖酵母的细胞活力^[1]。
ICRF-193 (5 days) 会抑制人急性早幼粒细胞白血病 (APL) 细胞系 (NB4, HT-93) 和其他髓系白血病细胞系 (HL-60, U937) 的生长，其 IC₅₀ 值为 0.21-0.26 μM^[2]。
ICRF-193 (0.1-0.2 μM, 5 days) 会诱导 NB4、HT-93、HL-60 和 U937 细胞的粒细胞分化^[2]。
ICRF-193 (0.2 μM, 48 h) 会显著下调 NB4 细胞中 PML-RAR 融合蛋白的水平，并上调 p21 和 RARβ 的水平^[2]。
ICRF-193 (10 μM) 可抑制停滞在静止期 (G0) 的细胞重新进入 S 期，并抑制小鼠脾细胞中的 DNA 合成^[3]。
ICRF-193 (150 nM, 72 h) 可抑制 LPS (HY-D1056) 诱导的人巨噬细胞中 IL-1β 的分泌^[4]。
ICRF-193 可减少 Etoposide (HY-13629) 诱导的 DNA 片段化，并诱导小鼠胸腺细胞凋亡^[6]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

282.30

C₁₂H₁₈N₄O₄

21416-88-6

固体

White to off-white

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*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

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储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-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。

• [1]. Nakazawa N, et al. ICRF-193, an anticancer topoisomerase II inhibitor, induces arched telophase spindles that snap, leading to a ploidy increase in fission yeast. Genes Cells. 2016 Sep;21(9):978-93.  [Content Brief]

  [2]. Niitsu N, et al. The catalytic DNA topoisomerase II inhibitor ICRF-193 and all-trans retinoic acid cooperatively induce granulocytic differentiation of acute promyelocytic leukemia cells: candidate drugs for chemo-differentiation therapy against acute promyelocytic leukemia. Exp Hematol. 2002 Nov;30(11):1273-82.  [Content Brief]

  [3]. Hossain MS, et al. ICRF-193, a catalytic inhibitor of DNA topoisomerase II, inhibits re-entry into the cell division cycle from quiescent state in mammalian cells. Genes Cells. 2002 Mar;7(3):285-94  [Content Brief]

  [4]. Brindle A, et al. The Bisdioxopiperazine ICRF-193 Attenuates LPS-induced IL-1β Secretion by Macrophages. Inflammation. 2024 Feb;47(1):84-98.  [Content Brief]

  [5]. Jirkovská A, et al. Structure-Activity Relationship Study of Dexrazoxane Analogues Reveals ICRF-193 as the Most Potent Bisdioxopiperazine against Anthracycline Toxicity to Cardiomyocytes Due to Its Strong Topoisomerase IIβ Interactions. J Med Chem. 2021 Apr 8;64(7):3997-4019.  [Content Brief]

  [6]. Tanimoto C, et al. ICRF-193 modifies etoposide-induced apoptosis in thymocytes. Acta Med Okayama. 1995 Dec;49(6):281-6.  [Content Brief]