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102052-95-9

中文名稱 (1S,2R,5R)-5-(4-氨基-1H-咪唑并[4,5-C]吡啶-1-基)-3-羥甲基-3-環(huán)戊烯-1,2-二醇
英文名稱 3-deazaneplanocin
CAS 102052-95-9
分子式 C12H14N4O3
分子量 262.26
MOL 文件 102052-95-9.mol
更新日期 2024/12/10 09:06:35
102052-95-9 結(jié)構(gòu)式 102052-95-9 結(jié)構(gòu)式

基本信息

中文別名
3-去氮腺嘌呤
(1S,2R,5R)-5-(4-氨基-1H-咪唑并[4,5-C]吡啶-1-基)-3-羥甲基-3-環(huán)戊烯-1,2-二醇
英文別名
CS-825
NSC 617989
3-deazaneplanocin
3-deazaneplanocin(DzNep)
3-Deazaneplanocin A (DZNeP)
3-Deazaneplanocin A HCl salt
3-Deazaneplanocin A ?iDZNep?j
NSC 617989 3-deazaneplanocin(DzNep)
InSolution EZH2 Inhibitor, DZNep - CAS 102052-95-9 - Calbiochem
(1S,2R,5R)-5-(4-aMino-1H-iMidazo[4,5-c]pyridin-1-yl)-3-(hydroxyM

物理化學(xué)性質(zhì)

沸點624.1±65.0 °C(Predicted)
密度1.75
儲存條件= -70C
溶解度可溶于 DMSO(高達 20 mg/ml)
酸度系數(shù)(pKa)13.52±0.70(Predicted)
形態(tài)液體
顏色米色
水溶解性溶于水
穩(wěn)定性可在-20°C下的DMSO溶液保存長達1個月。

常見問題列表

生物活性
3-Deazaneplanocin A (DZNep) 是一種有效的組蛋白甲基轉(zhuǎn)移酶 (histone methyltransferase,EZH2) 抑制劑。3-Deazaneplanocin A 是一種有效的 S-腺苷同型半胱氨酸水解酶 (AHCY) 抑制劑。
靶點

EZH2

體外研究

3-Deazaneplanocin A is a potent histone methyltransferase EZH2 inhibitor. Treatment of OCI-AML3 cells with 3-Deazaneplanocin A (1.0 μM) results in a significant increase in accumulation of cells in the G 0 /G 1 phase (58.5%) with a concomitant decrease in the number of cells in S phase (35.2%) and G 2 /M phases (6.3%) of the cell cycle (P<0.05). Treatment with 3-Deazaneplanocin A (200 nM to 2.0 μM) for 48 hours, dose dependently, inhibits colony growth of OCI-AML3 and HL-60 cells. 3-Deazaneplanocin A reduces the expression of EZH2, especially after 72 hours (e.g. 48%, 32% and 36% reduction of EZH2 in PANC-1, MIA-PaCa-2 and LPc006 cells, respectively). 3-Deazaneplanocin A shows minimal growth inhibition in PANC-1 cells. More than 50% of these cells are still growing after exposure at the highest concentration (20 μM). MIA-PaCa-2 and LPc006 cells are much more sensitive, with IC 0 values of 1±0.3 and 0.1±0.03 μM, respectively. 3-Deazaneplanocin A causes dose-dependent inhibition of cell proliferation of NSCLC cell lines, and the IC 0 values range from 0.08 to 0.24 μM.

體內(nèi)研究

The survival of NOD/SCID mice with acute myeloid leukemia (AML) due to HL-60 cells is significantly higher, if treated with 3-Deazaneplanocin A and Panobinostat (PS) compare to treatment with PS, 3-Deazaneplanocin A, or vehicle alone (P<0.05). Median survival is as follows: control, 36 days; PS, 42 days; 3-Deazaneplanocin A, 43 days; and 3-Deazaneplanocin A plus PS, 52 days. There is a progressive increase in weight of rats treated with physiological saline in a time-dependent manner (the mean growth rate=3.19% per day). Administration of 20 mg/kg 3-Deazaneplanocin A not only markedly reduces the relative weight of the rats compare to the initial weight (?2.0%, ?4.9% and ?1.2%) in the first three days post-treatment, but also suppresses the weight growth rate to 2.6% per day from the fourth day onwards post-dose.

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