ICRF-193 CAS: 21416-68-2
MF: C12H18N4O4
MW: 282.30
A bisdioxopiperazine which induces apoptosis and erythroid differentiation.

ICRF-193 (CAS 21416-68-2)

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同义词: 4,4'-(1,2-Dimethyl-1,2-ethanediyl)bis-2,6-piperazinedione
应用; A bisdioxopiperazine which induces apoptosis and erythroid differentiation
CAS号码: 21416-68-2
纯度: ≥95%
分子量: 282.30
分子式: C12H18N4O4
Supplemental Information: This is classified as a Dangerous Good for transport and may be subject to additional shipping charges.
* 参考分析证明 大量特定数据 (包括水 含量).
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ICRF-193, a bisdioxopiperazine, is a catalytic noncleavable complex-forming inhibitor of DNA Topo II (topoisomerase II) that does not produce protein-linked DNA strand breaks. This compound has been shown to induce erythroid differentiation and apoptosis. Mechanistic studies suggest that ICRF-193 affects the caspase-3 activation/cleavage pathway of cell growth and associates with ATR-dependent inhibition of polo-like kinase (plk) 1 kinase activity and a decrease in cyclin B1 phosphorylation. ICRF-193 is an inhibitor of Topo II beta.


参考文献

1. Iguchi, K., et al. 1999. Biochem. Pharmacol. 57: 1105-1111. PMID: 11230797
2. Hasinoff, B.B., et al. 2001. Mol. Pharmacol. 59: 453-461. PMID: 11179439
3. Deming, P.B., et al. 2002. J. Biol. Chem. 277: 36832-36838. PMID: 12147700
4. Hajji, N., et al. 2003. Mutat. Res. 530: 35-46. PMID: 14563529
5. Park, I. and Avraham, H.K. 2006. Exp. Cell Res. 312: 1996-2008. PMID: 16630610

外观 :
Powder
物理状态 :
Solid
溶解度 :
Soluble in DMSO (4 mg/ml).
保存 :
Store at -20° C
熔点 :
301.66° C (Predicted)
沸点 :
526.73° C at 760 mmHg (Predicted)
密度 :
1.31 g/cm3 (Predicted)
折射率 :
n20D 1.54
IC50 :
DNA topoisomerase II alpha: IC50 = 13.9 µM (Homo sapiens); DNA topoisomerase II beta: IC50 = 13.9 µM (Homo sapiens)
pK值 :
pKa: 10.699, pKb: 2.953
仅供科研使用。不可用于诊断或治疗。
德国水公害等级 :
3
RTECS :
TL6380200
PubChem CID :
115150
MDL 号码 :
MFCD01702964
SMILES :
CC(C(C)N1CC(=O)NC(=O)C1)N2CC(=O)NC(=O)C2

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引用1 - 66

PMID: # 31270138  2019. J. Cell Biol. 218: 2492-2513.

PMID: # 29765039  2018. Nat Commun. 9: 1908.

PMID: # 27829144  Su, KC. et al. 2016. Cell Rep. 17: 1728-1738.

PMID: # 26518113  Yan, YX. et al. 2015. Eur. J. Cell Biol. 94: 626-41.

PMID: # 24324754  Lambert, LJ. et al. 2013. PloS one. 8: e82110.

PMID: # 23995680  King, IF. et al. 2013. Nature. 501: 58-62.

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