35898-87-4
Chemical Structure
Dilazep
- CAS No.: 35898-87-4
- Formula:C31H44N2O10
- Molecular Weight:604.69
IUPAC Name: (1,4-diazepane-1,4-diyl)bis(propane-3,1-diyl) bis(3,4,5-trimethoxybenzoate)
InChIKey: QVZCXCJXTMIDME-UHFFFAOYSA-N
SMILES: O=C(C1=CC(OC)=C(OC)C(OC)=C1)OCCCN2CCN(CCCOC(C3=CC(OC)=C(OC)C(OC)=C3)=O)CCC2
Biological Activity: Dilazep is a GATA2 inhibitor and an hENT1-mediated nucleoside transport inhibitor. Dilazep acts by blocking GATA2 chromatin recruitment and DNA binding, reducing GATA2 thermal stability, and inhibiting AR, c-MYC, the cell cycle, DNA replication/repair, and metastatic transcriptional programs; it also inhibits Adenosine (HY-B0228) reuptake and cardiac adenosine uptake, enhancing adenosine-induced coronary vasodilation. Dilazep can be used in research on atherosclerosis, ischemic heart disease, and castration-resistant prostate cancer[1][2][3][4][5][6][7].
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Dilazep | Dilazep is a GATA2 inhibitor and an hENT1-mediated nucleoside transport inhibitor. Dilazep acts by blocking GATA2 chromatin recruitment and DNA binding, reducing GATA2 thermal stability, and inhibiting AR, c-MYC, the cell cycle, DNA replication/repair, and metastatic transcriptional programs; it also inhibits Adenosine (HY-B0228) reuptake and cardiac adenosine uptake, enhancing adenosine-induced coronary vasodilation. Dilazep can be used in research on atherosclerosis, ischemic heart disease, and castration-resistant prostate cancer. | |||||||||||||||||||||
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References
- [1]. Telesnicki K. Assessing the impact of GATA2 inhibition on macrophage atherogenic activity (Doctoral dissertation, et al.
- [2]. Marzilli M, et al. Effects of dilazep on coronary and systemic hemodynamics in humans. American heart journal. 1984 Aug;108(2):276-85.
- [3]. Shrestha B, et al. Endothelin-1 gene expression in endothelial cells is potently inhibited by a vasodilator, dilazep. Hypertension research : official journal of the Japanese Society of Hypertension. 2004 Jun;27(6):409-15.
- [4]. Plagemann PG, et al. Species differences in sensitivity of nucleoside transport in erythrocytes and cultured cells to inhibition by nitrobenzylthioinosine, dipyridamole, dilazep and lidoflazine. Biochimica et biophysica acta. 1988 Apr 02;969(1):1-8.
- [5]. Hoque AN, et al. A study on dilazep: I. Mechanism of anti-ischemic action of dilazep is not coronary vasodilation but decreased cardiac mechanical function in the isolated, working rat heart. Japanese journal of pharmacology. 1995 Mar;67(3):225-32.
- [6]. Kaochar S, et al. Inhibition of GATA2 in prostate cancer by a clinically available small molecule. Endocrine-related cancer. 2021 Nov 24;29(1):15-31.
- [7]. Endres CJ, et al. Mutation of leucine-92 selectively reduces the apparent affinity of inosine, guanosine, NBMPR [S6-(4-nitrobenzyl)-mercaptopurine riboside] and dilazep for the human equilibrative nucleoside transporter, hENT1. The Biochemical journal. 2004 May 15;380(Pt 1):131-7. [Content Brief]
