UNC1999 | EZH1/2 Inhibitor | AmBeed-信号通路专用抑制剂

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UNC1999 {[allProObj[0].p_purity_real_show]}

货号：A108081

UNC1999 is a potent, orally bioavailable and selective inhibitor of EZH2 and EZH1 with IC50 of 2 nM and 45 nM, respectively.

UNC1999 化学结构
CAS号：1431612-23-5

UNC1999 3D分子结构
CAS号：1431612-23-5

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UNC1999 纯度/质量文件产品仅供科研

货号：A108081 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: • Cell Host Microbe, 2024. Ambeed. [ A163338 ]; • Cancer Res., 2024. Ambeed. [ A295334 ]; • J. Pharm. Investig., 2024. Ambeed. [ A221527 , A691302 , A272538 , A187261 ]; • J. Fungi, 2024, 10(11): 751. Ambeed. [ A796919 ]; • JBC, 2024, 107935. Ambeed. [ A194396 ]; 更多 >

表观遗传阅读框亚型比较
组蛋白甲基转移酶亚型比较

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						99+%
GSK1324726A	+++ BRD2, IC50: 31 nM BRD4, IC50: 22 nM						99%+
PFI-1	++ BRD2, IC50: 98 nM BRD4, IC50: 0.22 μM						98%
Apabetalone	+ BD2, IC50: 0.51 μM						99%
(+)-JQ1	+++ BRD4 (1), IC50: 77 nM BRD4 (2), IC50: 33 nM						98%
I-BET151	+ BRD3, IC50: 0.25 μM BRD4, IC50: 0.5 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	++++ BRD9, Kd: 5.9 nM BRD7, Kd: 73 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 BD1, IC50: 27 nM BRD4 BD2, IC50: 32 nM						99%+
BMS-986158	✔						99%+
BRD4 Inhibitor-10	++++ BRD4-BD2, IC50: 41 nM BRD4-BD1, IC50: 5 nM						97%
A1874	✔						99%+
Y06036	++ BRD4 (1), Kd: 82 nM						99%+
Alobresib	✔					NF-κB	98%
ODM-207	✔						99%
GSK778	+++ BRD2-BD1, IC50: 75nM BRD4-BD1, IC50: 143 nM						97%
SRX3207	+ BRD42, IC50: 3070 nM BRD41, IC50: 3070 nM					Syk	98%
GSK046	+++ BRD3_BD2, IC50: 98 nM BRD4_BD2, IC50: 214 nM						98%
GSK620	✔						97%
Thalidomide-NH-C4-NH-Boc	✔						98%
Trotabresib	✔						99%
NHWD-870	✔						98%
CFT8634	++++ BRD9, DC50: 3 nM						98%
GSK2801		++ BAZ2A, Kd: 257 nM BAZ2B, Kd: 136 nM					99%+
KG-501		✔					99%+
UNC 669		+ L3MBTL4, IC50: 6 μM L3MBTL3, IC50: 35 μM					98%
PFI-3		+++ SMARCA2A, Kd: 72 nM SMARCA4, Kd: 55 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					++++ EP300, IC50: 38 nM CREBBP, IC50: 21 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。

产品名称	Histone Methyltransferase ↓ ↑	纯度
BRD4770	✔	99%+
UNC1999	+++ EZH2, IC50: 2 nM EZH1, IC50: 45 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	+++ EZH2, IC50: 4 nM EZH1, IC50: 240 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。

UNC1999 生物活性

靶点	Histone Methyltransferase EZH2, IC50:2 nM EZH1, IC50:45 nM
描述	EZH2 or EZH1 is the catalytic subunit of the polycomb repressive complex 2 that catalyzes methylation of histone H3 lysine 27 (H3K27), which cause the gene expression silence. UNC1999 is a dual inhibitor of EZH2 and EZH1 with IC50 values of 2 nM and 45 nM (measured by PRC2 enzymatic activity)，respectively, and is over 1000-fold selective for other HMTs^[1]. UNC1999 (72h exposure) exhibited dose-dependent reductions in H3K27me3 with an IC50 value of 124 ± 11 nM in MCF10A cells bearing the WT EZH2 enzyme. The treatment of MCF7 cells with UNC1999 at 5,000 nM for 72 h almost completely removed the H3K27me3 mark but did not have significant effects on cellular levels of EZH2. UNC1999 selectively killed EZH2-mutant DLBCL cells with heterozygous for Y641 point mutations. Exposure of UNC1999 for 8 days displayed dose-dependent inhibition of cell proliferation with an EC50 of 633 ± 101 nM in DB cells, while 5,000 nM UNC1999 can completely killed DB cells. UNC1999 may be a good probe for EZH2 for biotinylated UNC1999 can be used to pull down EZH2 from cell lysates and UNC1999–dye conjugate co-localizes with EZH2 in live cells^[2]. Oral administration of UNC1999 (50 mg/kg, twice daily) starting from 7 days post-transplantation prolongs survival of a well-defined murine leukemia model bearing MLL-AF9, with significantly decreased H3K27me3 and elevated their p16Ink4a or p19Arf expression in cells isolated from bone marrow and spleen^[3].
作用机制	UNC1999 is a SAM-competitive inhibitor of EZH2 and EZH1^[2].

UNC1999 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 MCF10A cells		Function assay	72 h	Inhibition of EZH2 in human MCF10A cells assessed as reduction of H3K27me3 level after 72 hrs by Western blot analysis, IC50=0.124 μM	25406853
human MCF10A cells		Cytotoxic assay		Cytotoxicity against human MCF10A cells assessed as cell viability by Alamar Blue assay, EC50=19.2 μM	25406853

UNC1999 动物研究

Dose

Mice: min = 15 mg/kg, max = 150 mg/kg^[2] (i.p.); 50 mg/kg^[4] (p.o.)

Administration

i.p., p.o.

Pharmacokinetics

Animal	Mice^[2]
Dose	15 mg/kg 50 mg/kg
Administration	i.p. p.o.
C_max	9700 nM (i.p.) 4700 nM (p.o.)

UNC1999 参考文献

[1]UNC1999 A chemical probe for EZH2/1

[2]Konze KD, Ma A, et al. An orally bioavailable chemical probe of the Lysine Methyltransferases EZH2 and EZH1. ACS Chem Biol. 2013;8(6):1324-34.

[3]Xu B, On DM, et al. Selective inhibition of EZH2 and EZH1 enzymatic activity by a small molecule suppresses MLL-rearranged leukemia. Blood. 2015 Jan 8;125(2):346-57.

[4]Inhibitors of Protein Methyltransferases and Demethylases

UNC1999 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

1.76mL

0.35mL

0.18mL

8.78mL

1.76mL

0.88mL

17.55mL

3.51mL

1.76mL

UNC1999 技术信息

CAS号	1431612-23-5
分子式	C₃₃H₄₃N₇O₂
分子量	569.74

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Sealed in dry,2-8°C

溶解度

DMSO: 105 mg/mL(184.29 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

动物实验配方

IP 2% DMSO+2% Tween80+40% PEG300+water 8 mg/mL clear

PO 0.5% CMC-Na 20 mg/mL suspension

UNC1999 {[allProObj[0].p_purity_real_show]}

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