102052-95-9 Usage
Description
3-deazaneplanocin, also known as DZNep, is a cell-permeable compound that functions as a potent histone methyltransferase inhibitor. It is capable of decreasing global histone methylation and selectively induces apoptosis in multiple cancer cell lines without affecting normal cells. DZNep has shown the ability to inhibit EZH2-mediated trimethylation of K27 on histone H3, leading to the induction of cell-cycle regulatory genes and cell death regulators in certain cell cultures. Additionally, it has been identified as an S-adenosyl-L-homocysteine (AdoHcy) hydrolase inhibitor and has potential applications in enhancing angiogenesis and inducing pluripotent stem cells.
Uses
Used in Oncology Research and Cancer Treatment:
3-deazaneplanocin is used as a histone methyltransferase inhibitor for its ability to selectively induce apoptosis in various cancer cell lines, including OCI-AML3 and HL-60, without affecting normal cells. It modulates the expression of polycomb group proteins and increases the percentage of apoptotic cells, demonstrating potential as a therapeutic agent in cancer treatment.
Used in Drug Combination Therapy:
In combination with other compounds such as panobinostat (PS), 3-deazaneplanocin is used to enhance the effectiveness of cancer treatment. The co-treatment of DZNep and PS has been shown to decrease cell viability in OCI-AML3 and HL-60 cultures more effectively than DZNep alone, suggesting a synergistic effect in combating cancer.
Used in Cellular Reprogramming:
3-deazaneplanocin is used as a component in chemical cocktails to induce pluripotent stem cells (CiPSCs) from somatic cells. Its role in this process highlights its potential in the field of regenerative medicine and stem cell research.
Used in Angiogenesis Research:
3-deazaneplanocin is used to enhance angiogenesis in mouse models of limb ischemia. This application underscores its potential in the study and treatment of vascular-related diseases and conditions.
Overall, 3-deazaneplanocin is a versatile compound with significant applications in various fields, particularly in oncology, cellular reprogramming, and angiogenesis research. Its ability to selectively target cancer cells and modulate gene expression makes it a promising candidate for further investigation and development in these areas.
Biochem/physiol Actions
Cell permeable: yes
References
1) Miranda?et al.?(2009),?DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation; Mol. Cancer Ther.,?8?1579
2) Tan?et al.?(2007),?Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells; Genes Dev.,?21?1050
3) Hou?et al. (2013),?Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds; Science,?341?651
4) Mitic?et al. (2015),?EZH2 modulates angiogenesis in vitro and in a mouse model of limb ischemia; Mol. Ther.,?23?32
Check Digit Verification of cas no
The CAS Registry Mumber 102052-95-9 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,0,2,0,5 and 2 respectively; the second part has 2 digits, 9 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 102052-95:
(8*1)+(7*0)+(6*2)+(5*0)+(4*5)+(3*2)+(2*9)+(1*5)=69
69 % 10 = 9
So 102052-95-9 is a valid CAS Registry Number.
InChI:InChI=1/C12H14N4O3/c13-12-9-7(1-2-14-12)16(5-15-9)8-3-6(4-17)10(18)11(8)19/h1-3,5,8,10-11,17-19H,4H2,(H2,13,14)/t8-,10-,11+/m1/s1
