3-Deazaneplanocin A HCl | DZNep hydrochloride | EZH2 Inhibitor (GMP)

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3-去氮腺嘌呤A盐酸盐 /3-Deazaneplanocin A HCl {[allProObj[0].p_purity_real_show]}

货号：A746301 同义名： DZNep hydrochloride;3-Deazaneplanocin hydrochloride

3-Deazaneplanocin A (DZNep) 能够抑制s -腺苷-l-同型半胱氨酸水解酶 (AHCY)。3-Deazaneplanocin A HCl是一种强效组蛋白甲基转移酶 EZH2 抑制剂。

3-Deazaneplanocin A HCl 化学结构
CAS号：120964-45-6

3-Deazaneplanocin A HCl 3D分子结构
CAS号：120964-45-6

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3-Deazaneplanocin A HCl 纯度/质量文件产品仅供科研

货号：A746301 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

组蛋白甲基转移酶亚型比较
表观遗传阅读框亚型比较

产品名称	Histone Methyltransferase ↓ ↑	纯度
BRD4770	✔	99%+
UNC1999	+++ EZH1, IC50: 45 nM EZH2, IC50: 2 nM	99%+
EPZ005687	++ EZH2, Ki: 24 nM	98+%
EPZ015666	+++ PRMT5, Ki: 5 nM	99%+
3-Deazaneplanocin A HCl	++++ S-adenosylhomocysteine hydrolase, Ki: 50 pM	99%+
Tazemetostat	+++ EZH2, IC50: 11 nM EZH2, Ki: 2.5 nM	98%
GSK126	++ EZH2, IC50: 9.9 nM	99%+
MI-3	+ Menin-MLL, IC50: 648 nM	98%
MM-102	++ MLL1, IC50: 0.4 μM	99%
EI1	++ Ezh2 (wild-type), IC50: 15 nM EZH2 (Y641F), IC50: 13 nM	98%
SGC0946	++++ DOT1L, IC50: 0.3 nM	99%+
PFI-2 HCl	++++ SETD7, Ki: 0.33 nM SETD7, IC50: 2 nM	99%+
Pinometostat	++++ DOT1L, Ki: 80 pM	99%+
EPZ004777	+++ DOT1L, IC50: 0.4 nM	99%+
Entacapone	++ COMT, IC50: 151 nM	95%
UNC0379	+ SETD8, IC50: 7.9 μM	99%+
Menin-MLL inhibitor MI-2	+ Menin-MLL, IC50: 446 nM	98%
GSK343	+++ EZH1, IC50: 240 nM EZH2, IC50: 4 nM	99%+
BIX-01294 3HCl	+ G9a, IC50: 2.7 μM	99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (1), Ki: <0.085 μM BRD4 (2), Ki: 0.34 μM						99%+
CPI-203	+++ BRD4, IC50: 37 nM						98+%
GSK1324726A	+++ BRD4, IC50: 22 nM BRD2, IC50: 31 nM						99%+
PFI-1	++ BRD4, IC50: 0.22 μM BRD2, IC50: 98 nM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						98%
I-BET151	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD4, pIC50: 5.3 BRD9, pIC50: 7.3						99%+
BI-7273	++++ BRD7, IC50: 117 nM BRD9, IC50: 19 nM						99+%
Pelabresib	+++ BRD4-BD1, IC50: 39 nM						98%
ARV-825	+++ BRD4 BD2, Kd: 28 nM BRD4 BD1, Kd: 90 nM						99%+
Birabresib							99%+
BI 2536	+++ BRD4, Kd: 37 nM					c-Myc	99%+
Bromosporine	++ BRD2, IC50: 0.29 μM BRD9, IC50: 0.122 μM	++++ CECR2, IC50: 17 nM					99%+
XMD8-92	++ BRD4 (1), Kd: 170 nM						99%+
Mivebresib	✔						99%+
BI-9564	++++ BRD7, Kd: 73 nM BRD9, Kd: 5.9 nM	++ CECR2, Kd: 77 nM					98%
AZD5153 6-Hydroxy-2-naphthoic acid	++++ FL-BRD4, IC50: 5 nM						99%+
PLX51107	++++ BRD4 BD2, Kd: 1.7 nM BRD3 BD1, Kd: 2.1 nM						99%+
FL-411	+ BRD4(1), IC50: 0.43 μM						99%+
ABBV-744	✔						99%+
dBET6	++++ BRD4, IC50: 14 nM						99%+
dBET1	++++ BRD4, IC50: 20 nM						99%+
MZ1	++++ Brd2(BD2), Kd: 62 nM Brd3(BD2), Kd: 13 nM						99%+
dBET57	+ BRD4_BD1, DC50: 500 nM						99%+
SF2523	+ BRD4, IC50: 241 nM					DNA-PK	99%+
INCB054329	++++ BRD3-BD1, IC50: 9 nM BRD4-BD1, IC50: 119 nM						99%
INCB-057643	✔						99%+
(E/Z)-ZL0420	+++ BRD4 BD2, IC50: 32 nM BRD4 BD1, IC50: 27 nM						99%+
BMS-986158	✔						99%+
BRD4 Inhibitor-10	++++ BRD4-BD1, IC50: 5 nM BRD4-BD2, IC50: 41 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	98%
ODM-207	✔						99%
GSK778	+++ BRD4-BD1, IC50: 143 nM BRD2-BD1, IC50: 75nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD4_BD2, IC50: 214 nM BRD3_BD2, IC50: 98 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2B, Kd: 136 nM BAZ2A, Kd: 257 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					98%
PFI-3		+++ SMARCA4, Kd: 55 nM SMARCA2A, Kd: 72 nM					99%+
UNC1215		+++ L3MBTL3- D274A, IC50: 3.5 μM L3MBTL3, IC50: 120 nM					99%+
EED226		++ EED, Kd: 82 nM PRC2, Kd: 114 nM					99%+
BRD9539		✔					98%
UNC926		+ L3MBTL1, Kd: 3.9 μM					99%
666-15		++ CREB, IC50: 81 nM					99%+
UNC6852		+ EED, IC50: 247 nM					98%
BAZ1A-IN-1		+ BAZ1A, Kd: 0.52 μM					99%+
PFI-4			++ BRPF2, IC50: 7.9 μM BRPF1, IC50: 80 nM				99%+
OF-1			++ BRPF2, Kd: 500 nM BRPF1B, Kd: 100 nM				99%+
GSK-5959			++ BRPF2, pIC50: 5.2 BRPF3, pIC50: 7.1				99%
GSK6853			++++ BRPF1, pIC50: 8.1				99%+
NI-42			++++ BRPF1, IC50: 48 nM BRPF3, IC50: 260 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			97%
I-CBP112					++ CBP, Kd: 151 nM p300, Kd: 167 nM		98+%
Histone Acetyltransferase Inhibitor II					+ p300, IC50: 5 μM		98%
C646					+ p300/CBP, Ki: 400 nM		99%+
Anacardic Acid					+ PCAF, IC50: 5 μM p300/CBP, IC50: 8.5 μM		99%+
SGC-CBP30					++++ CREBBP, IC50: 21 nM EP300, IC50: 38 nM		99%+
Nordihydroguaiaretic acid					✔	HER2,IGF-1R	99%+
Curcumin					+ p300, IC50: ~25 μM	Ferroptosis,Nrf2,NF-κB	98%
PF-CBP1 HCl					++ CREBBP, IC50: 125nM p300/CBP, IC50: 363nM		97%
CPI-637					+++ EP300, IC50: 0.051 μM CBP, IC50: 0.03 μM		99%+
Foscenvivint					✔	β-catenin	99%+
A-485					++ p300 HAT, IC50: 0.06 μM		99%+
GNE-781	+ BRD4(1), IC50: 5100 nM				++++ CBP, IC50: 0.94 nM		98%
NEO2734	+++ BET, IC50: <30 nM				+++ p300/CBP, IC50: <30 nM		99%+
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。

3-Deazaneplanocin A HCl 生物活性

靶点	Histone Methyltransferase S-adenosylhomocysteine hydrolase, Ki:50 pM
描述	3-Deazaneplanocin A is a cyclopentanyl analog of 3-deazaadenosine that potently interferes with SAH, a component of the methionine cycle, which causes cellular SAH levels to increase, thus repressing the activity of S-adenosyl-l-methionine–dependent histone lysine methyltransferase activity^[1]. Thus, the effect of 3-Deazaneplanocin A in inhibiting histone methylation is not specific to EZH2. Treatment with 5 μM of 3-Deazaneplanocin A for 72h led to a global decrease in most histone examined, including H3K27me3, H3K9me2, H3K79me3, H4K20me3, H3K4me3, H3K9me1, H3R2me2 and H3K27me1, with most reduction on H3K27me3 and H4K20me3, in MCF-7 cells, as well as slight decrease of EZH2^[1]. Treatment with 5 µM 3-Deazaneplanocin A for 48 and 72h depletes EZH2 proteins as well as inhibits histone H3-K27 methylation, and induces apoptotic cell death in MCF-7 and HCT116 cells. 3-Deazaneplanocin A treatment removes the binding of PRC2 to their target genes and increases the binding of RNA Pol II, thus increases recruitment of RNA Pol II and transcriptional activation of these PRC2 target genes, such as FBXO32, LAMB3, PLAU, and PPP1R15A, in MCF-7 cells, MDA-MB-468, SK-BR-3 and T47D cell lines sensitive to DZNep-induced cell death^[2]. Recently, it was found that 3-Deazaneplanocin A can enhance Oct4 expression in chemically induced pluripotent stem cells^[3].
作用机制	Deazaneplanocin A is a cyclopentanyl analog of 3-deazaadenosine, thus functioning as a SAH hydrolase inhibitor of methyltransferases^[1].

3-Deazaneplanocin A HCl 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
human A549 cells		Cytotoxic assay	72 h	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=1.4 μM.	26010585
human HCT116 cells		Cytotoxic assay	72 h	Cytotoxicity against human HCT116 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=0.26 μM.	26010585
human MDA-MB-231 cells		Cytotoxic assay	72 h	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay， IC50=0.3 μM.	26010585
human PC3 cells		Cytotoxic assay	72 h	Cytotoxicity against human PC3 cells assessed as inhibition of cell proliferation after 72 hrs by sulforhodamine B assay, IC50=9.39 μM.	26010585

3-Deazaneplanocin A HCl 动物研究

Dose

Mice^[4]: 1 mg/kg (i.p.); min = 3.75 mg/kg , max = 25 mg/kg (s.c.)

Administration

i.p., s.c.

Pharmacokinetics

Animal	Rats^[5]
Dose	5 mg/kg
Administration	i.v.
T_1/2	1 h
Vss	0.63 L
CL	0.59 L/h
AUC_0→12h	2.7 h·μg/ml

3-Deazaneplanocin A HCl 参考文献

[1]Miranda TB, Cortez CC, et al. DZNep is a global histone methylation inhibitor that reactivates developmental genes not silenced by DNA methylation. Mol Cancer Ther. 2009 Jun;8(6):1579-88.

[2]Tan J, Yang X, et al. Pharmacologic disruption of Polycomb-repressive complex 2-mediated gene repression selectively induces apoptosis in cancer cells. Genes Dev. 2007 May 1;21(9):1050-63. Epub 2007 Apr 16.

[3]Hou P, Li Y, et al. Pluripotent stem cells induced from mouse somatic cells by small-molecule compounds. Science. 2013 Aug 9;341(6146):651-4.

[4]Fiskus W, Wang Y, et al. Combined epigenetic therapy with the histone methyltransferase EZH2 inhibitor 3-deazaneplanocin A and the histone deacetylase inhibitor panobinostat against human AML cells. Blood. 2009 Sep 24;114(13):2733-43.

[5]Sun F, Lee L, et al. Preclinical pharmacokinetic studies of 3-deazaneplanocin A, a potent epigenetic anticancer agent, and its human pharmacokinetic prediction using GastroPlus™. Eur J Pharm Sci. 2015 Sep 18;77:290-302.

3-Deazaneplanocin A HCl 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.35mL

0.67mL

0.33mL

16.74mL

3.35mL

1.67mL

33.48mL

6.70mL

3.35mL

3-Deazaneplanocin A HCl 技术信息

CAS号	120964-45-6
分子式	C₁₂H₁₅ClN₄O₃
分子量	298.726

别名	DZNep hydrochloride;3-Deazaneplanocin hydrochloride;2,3-DMMC;3-Deazaneplanocin A (hydrochloride);NSC 617989 HCl;DZNeP HCl;NSC 617989 hydrochloride;3-Deazaneplanocin A hydrochloride
运输	蓝冰

存储条件

液体 -20°C:3个月-80°C:12个月

粉末 Inert atmosphere,Store in freezer, under -20°C

溶解度

H₂O: 50 mg/mL(167.38 mM)，配合低频超声助溶

动物实验配方

3-去氮腺嘌呤A盐酸盐 /3-Deazaneplanocin A HCl {[allProObj[0].p_purity_real_show]}

3-Deazaneplanocin A HCl 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

3-Deazaneplanocin A HCl 质控信息

3-Deazaneplanocin A HCl 生物活性

3-Deazaneplanocin A HCl 细胞研究

3-Deazaneplanocin A HCl 动物研究

3-Deazaneplanocin A HCl 参考文献

3-Deazaneplanocin A HCl 实验方案

3-Deazaneplanocin A HCl 技术信息

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3-去氮腺嘌呤A盐酸盐 /3-Deazaneplanocin A HCl {[allProObj[0].p_purity_real_show]}

3-Deazaneplanocin A HCl 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

3-Deazaneplanocin A HCl 质控信息

3-Deazaneplanocin A HCl 生物活性

3-Deazaneplanocin A HCl 细胞研究

3-Deazaneplanocin A HCl 动物研究

3-Deazaneplanocin A HCl 参考文献

3-Deazaneplanocin A HCl 实验方案

3-Deazaneplanocin A HCl 技术信息

最近浏览的产品

大规格询价

摩尔计算器

靶点

总药量计算器

工作液计算器

细胞研究

临床研究

确认信息

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3-Deazaneplanocin A HCl 纯度/质量文件产品仅供科研