Apabetalone | RVX-208;RVX000222 | Epigenetic Reader Domain

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阿帕他隆 /Apabetalone {[allProObj[0].p_purity_real_show]}

货号：A161440 同义名： RVX-208;RVX000222

RVX-208 is an inhibitor of BET bromodomain BD2 with IC50 of 0.510 μM.

Apabetalone 化学结构
CAS号：1044870-39-4

Apabetalone 3D分子结构
CAS号：1044870-39-4

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Apabetalone 纯度/质量文件产品仅供科研

货号：A161440 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

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表观遗传阅读框亚型比较

产品名称	BET ↓ ↑	bromodomain ↓ ↑	BRPF ↓ ↑	CBP/beta-catenin ↓ ↑	p300/CBP ↓ ↑	其他靶点	纯度
MS436	++ BRD4 (2), Ki: 0.34 μM BRD4 (1), Ki: <0.085 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 (2), IC50: 33 nM BRD4 (1), IC50: 77 nM						98%
I-BET151	+ BRD4, IC50: 0.5 μM BRD3, IC50: 0.25 μM						98%
Molibresib	+++ BET proteins, IC50: 35 nM						99%+
I-BRD9	+++ BRD9, pIC50: 7.3 BRD4, pIC50: 5.3						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	++++ Brd3(BD2), Kd: 13 nM Brd2(BD2), Kd: 62 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	+ BRD41, IC50: 3070 nM BRD42, 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		++ 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			++ BRPF1, IC50: 80 nM BRPF2, IC50: 7.9 μM				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			++++ BRPF3, IC50: 260 nM BRPF1, IC50: 48 nM				99%+
E-7386				+++ CBP/beta-catenin, IC50: 0.0484 μM			97%
I-CBP112					++ p300, Kd: 167 nM CBP, Kd: 151 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	Nrf2,Ferroptosis,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。

Apabetalone 生物活性

靶点	BET BD2, IC50:0.51 μM
描述	RVX-208 is a derivative of the plant polyphenol resveratrol. It is a domain-selective inhibitor of BETs with 0.51μM and 87μM for BD2 and BD1, respectively. Inhibition of BD2 by RVX-208 only modestly affected BET-dependent gene transcription^[3]. RVX-208 at 60μM induced apoA-I mRNA and protein synthesis in HepG2 cells, leading to increased levels of pre-β-migrating and α-lipoprotein particles containing apoA-I (LpA-I) in spent media. Administration of RVX-208 at doses ranging in 15 to 60 mg/kg/day for 63 days increased serum apoA-I and HDL-C levels (60% and 97%, respectively) of african green monkeys. The levels of pre-β1-LpA-I and α1-LpA-I HDL-subparticles were increased as well as adenosine triphosphate binding cassette AI, adenosine triphosphate binding cassette G1, and scavenger receptor class B type I-dependent cholesterol efflux^[4].
作用机制	RVX-208 binds to the acetyl-lysine binding pocket in a peptide-competitive manner. It displaces BET proteins from chromatin.^[3]

Apabetalone 细胞研究

细胞系	浓度	检测类型	检测时间	活动说明	数据源
HepG2	~60 μM	Function assay		induces apoA-I mRNA and de novo synthesis of apoA-I.	20513599
U2OS	~5 μM	Function assay		displaces BET proteins from chromatin	24248379

Apabetalone 动物研究

Dose	Mice: 150 mg/kg^[3] (p.o., BID) African green monkey：7.5 mg/kg - 30 mg/kg^[4] (p.o., BID)
Administration	p.o.

Apabetalone 临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02586155	Diabetes Mellitus, Type 2 ... 展开 >> Coronary Artery Disease Cardiovascular Diseases 收起 <<	Phase 3	Recruiting	October 2018	Israel ... 展开 >> Lady Davis Carmel Medical Center Recruiting Haifa, Israel, 34362 Contact: Basil Lewis, MD 收起 <<
NCT01067820	Coronary Artery Disease	Phase 2	Completed	-	-
NCT00768274	Dyslipidemia ... 展开 >>Atherosclerosis Acute Coronary Syndrome Cardiovascular Disease 收起 <<	Phase 1 Phase 2	Completed	-	United States, Texas ... 展开 >> Covance Clinical Research Unit, Inc. Dallas, Texas, United States, 75247 收起 <<

Apabetalone 参考文献

[1]Picaud S, Wells C, et al. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9.

[2]Bailey D, Jahagirdar R, et al. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9.

[3]Picaud S, Wells C, Felletar I, Brotherton D, Martin S, Savitsky P, Diez-Dacal B, Philpott M, Bountra C, Lingard H, Fedorov O, Müller S, Brennan PE, Knapp S, Filippakopoulos P. RVX-208, an inhibitor of BET transcriptional regulators with selectivity for the second bromodomain. Proc Natl Acad Sci U S A. 2013 Dec 3;110(49):19754-9. doi: 10.1073/pnas.1310658110. Epub 2013 Nov 18. PMID: 24248379; PMCID: PMC3856850.

[4]Bailey D, Jahagirdar R, Gordon A, Hafiane A, Campbell S, Chatur S, Wagner GS, Hansen HC, Chiacchia FS, Johansson J, Krimbou L, Wong NC, Genest J. RVX-208: a small molecule that increases apolipoprotein A-I and high-density lipoprotein cholesterol in vitro and in vivo. J Am Coll Cardiol. 2010 Jun 8;55(23):2580-9. doi: 10.1016/j.jacc.2010.02.035. Erratum in: J Am Coll Cardiol. 2010 Aug 31;56(10):825. PMID: 20513599.

Apabetalone 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.70mL

0.54mL

0.27mL

13.50mL

2.70mL

1.35mL

27.00mL

5.40mL

2.70mL

Apabetalone 技术信息

CAS号	1044870-39-4
分子式	C₂₀H₂₂N₂O₅
分子量	370.399

别名	RVX-208;RVX000222
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

溶解度

DMSO: 35 mg/mL(94.49 mM)，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

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点

NCT02586155	Diabetes Mellitus, Type 2 ... 展开 >> Coronary Artery Disease Cardiovascular Diseases 收起 <<	Phase 3	Recruiting	October 2018	Israel ... 展开 >> Lady Davis Carmel Medical Center Recruiting Haifa, Israel, 34362 Contact: Basil Lewis, MD 收起 <<
NCT01067820	Coronary Artery Disease	Phase 2	Completed	-	-
NCT00768274	Dyslipidemia ... 展开 >>Atherosclerosis Acute Coronary Syndrome Cardiovascular Disease 收起 <<	Phase 1 Phase 2	Completed	-	United States, Texas ... 展开 >> Covance Clinical Research Unit, Inc. Dallas, Texas, United States, 75247 收起 <<
NCT01423188	Coronary Artery Disease ... 展开 >> Dyslipidemia 收起 <<	Phase 2	Completed	-	South Africa ... 展开 >> East Burger Street, Bloemfontein, South Africa, 9301 Westdene, Bloemfontein, South Africa, 9301 Goodwood, Cape Town, South Africa, 7460 Kraaifontein, Cape Town, South Africa, 7570 Pinelands, Cape Town, South Africa, 7405 Chatsworth, Durban, South Africa, 4092` Congella, Durban, South Africa, 4001 Merebank, Durban, South Africa, 4052 Sydenham, Durban, South Africa, 4091 Tongaat, Durban, South Africa, 4400 Umhlanga, Durban, South Africa, 4321 Lenasia, Johannesburg, South Africa, 1827 Halfway House, Midrand, South Africa, 1685 Die Wilgers, Pretoria, South Africa, 0041 Eloffsdal, Pretoria, South Africa, 0084 Kuils River, Western Cape, South Africa, 7580 Parow, Western Cape, South Africa, 7500 Somerset West, Western Cape, South Africa, 7130 Stellenbosch, Western Cape, South Africa, 7600 Worcester, Western Cape, South Africa, 6850 Bloemfontein, South Africa, 9301 Cape Town, South Africa, 7505 Cape Town, South Africa, 7925 Johannesburg, South Africa, 1460 Western Cape, South Africa, 7646 收起 <<
NCT03228940	Fabry Disease	Phase 1 Phase 2	Not yet recruiting	February 15, 2020	Canada, Nova Scotia ... 展开 >> Queen Elizabeth II Health Sciences Centre, Victoria General Site Not yet recruiting Halifax, Nova Scotia, Canada, B3H2Y9 Contact: Michael West, MD (902) 473-4023 mwets@dal.ca 收起 <<
NCT03160430	Kidney Failure, Chronic	Phase 1 Phase 2	Not yet recruiting	March 15, 2020	-
NCT01728467	Diabetes	Phase 2	Completed	-	Australia, Victoria ... 展开 >> Baker IDI Heart and Diabetes Institute 75 Commercial Road, Melbourne, Victoria, Australia, 3004 收起 <<
NCT01863225	Dyslipidemia ... 展开 >>Coronary Artery Disease 收起 <<	Phase 2	Terminated	-	Australia, South Australia ... 展开 >> Royal Adelaide Hospital / CMAX Adelaide, South Australia, Australia, 5000 收起 <<
NCT01058018	Atherosclerosis ... 展开 >> Coronary Artery Disease 收起 <<	Phase 2	Completed	-	United States, California ... 展开 >> Orange County Research Center Tustin, California, United States, 92780 收起 <<

阿帕他隆 /Apabetalone {[allProObj[0].p_purity_real_show]}

Apabetalone 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Apabetalone 质控信息

Apabetalone 生物活性

Apabetalone 细胞研究

Apabetalone 动物研究

Apabetalone 临床研究

Apabetalone 参考文献

Apabetalone 实验方案

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Apabetalone 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Apabetalone 质控信息

Apabetalone 生物活性

Apabetalone 细胞研究

Apabetalone 动物研究

Apabetalone 临床研究

Apabetalone 参考文献

Apabetalone 实验方案

Apabetalone 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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