BRD3308 | HDAC3 Inhibitor | AmBeed-信号通路专用抑制剂

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BRD3308 {[allProObj[0].p_purity_real_show]}

货号：A822432

BRD3308 is a highly selective inhibitor of histone deacetylase 3 (HDAC3) with an IC50 value of 65 nM for HDAC3 vs.

BRD3308 化学结构
CAS号：1550053-02-5

BRD3308 3D分子结构
CAS号：1550053-02-5

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BRD3308 纯度/质量文件产品仅供科研

货号：A822432 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: • JACS Au, 2024. Ambeed. [ A148168 ]; • JMC, 2024. Ambeed. [ A187643 ]; • JMC, 2024. Ambeed. [ A341145 , A633512 , A607865 , A167774 ]; • Biomacromolecules, 2024. Ambeed. [ A110759 ]; • Biomacromolecules, 2024. Ambeed. [ A203543 ]; 更多 >

组蛋白去乙酰化酶亚型比较

产品名称	HD1 ↓ ↑	HD2 ↓ ↑	HDAC ↓ ↑	HDAC1 ↓ ↑	HDAC10 ↓ ↑	HDAC11 ↓ ↑	HDAC2 ↓ ↑	HDAC3 ↓ ↑	HDAC4 ↓ ↑	HDAC5 ↓ ↑	HDAC6 ↓ ↑	HDAC7 ↓ ↑	HDAC8 ↓ ↑	HDAC9 ↓ ↑	其他靶点	纯度
Givinostat HCl monohydrate	++++ HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM	+++ HD2, IC50: 10 nM														{[allProObj[0].p_purity_real_show]}
MC1568	++ HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM															{[allProObj[0].p_purity_real_show]}
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													{[allProObj[0].p_purity_real_show]}
Scriptaid			✔													{[allProObj[0].p_purity_real_show]}
Valproic acid sodium			✔												Autophagy	{[allProObj[0].p_purity_real_show]}
AR-42			+++ HDAC, IC50: 30 nM													{[allProObj[0].p_purity_real_show]}
Dacinostat			+++ HDAC, IC50: 32 nM													{[allProObj[0].p_purity_real_show]}
CUDC-101			++++ HDAC, IC50: 4.4 nM	++++ HDAC1, IC50: 4.5 nM	+++ HDAC10, IC50: 26.1 nM		+++ HDAC2, IC50: 12.6 nM	++++ HDAC3, IC50: 9.1 nM	+++ HDAC4, IC50: 13.2 nM	+++ HDAC5, IC50: 11.4 nM	++++ HDAC6, IC50: 5.1 nM	+ HDAC7, IC50: 373 nM	++ HDAC8, IC50: 79.8 nM	++ HDAC9, IC50: 67.2 nM	HER2,EGFR	{[allProObj[0].p_purity_real_show]}
M344			++ HDAC, IC50: 100 nM													{[allProObj[0].p_purity_real_show]}
Splitomicin			+ Sir2p, IC50: 60 μM													{[allProObj[0].p_purity_real_show]}
Panobinostat			++++ HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM													{[allProObj[0].p_purity_real_show]}
Sodium 4-Phenylbutyrate			✔													{[allProObj[0].p_purity_real_show]}
Vorinostat			+++ HDAC, IC50: ~10 nM													{[allProObj[0].p_purity_real_show]}
Curcumin			✔												Nrf2,NF-κB	{[allProObj[0].p_purity_real_show]}
Belinostat			+++ HDAC, IC50: 27 nM													{[allProObj[0].p_purity_real_show]}
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								{[allProObj[0].p_purity_real_show]}
Valproic acid				+ HDAC1, IC50: 0.4 mM												{[allProObj[0].p_purity_real_show]}
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								{[allProObj[0].p_purity_real_show]}
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								{[allProObj[0].p_purity_real_show]}
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					{[allProObj[0].p_purity_real_show]}
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									{[allProObj[0].p_purity_real_show]}
Parthenolide				✔											p53,NF-κB	{[allProObj[0].p_purity_real_show]}
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								{[allProObj[0].p_purity_real_show]}
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								{[allProObj[0].p_purity_real_show]}
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					{[allProObj[0].p_purity_real_show]}
Fimepinostat				++++ HDAC1, IC50: 1.7 nM	++++ HDAC10, IC50: 2.8 nM	++++ HDAC11, IC50: 5.4 nM	++++ HDAC2, IC50: 5.0 nM	++++ HDAC3, IC50: 1.8 nM			+++ HDAC6, IC50: 27 nM					{[allProObj[0].p_purity_real_show]}
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								{[allProObj[0].p_purity_real_show]}
Santacruzamate A							++++ HDAC2, IC50: 119 pM									{[allProObj[0].p_purity_real_show]}
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								{[allProObj[0].p_purity_real_show]}
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						{[allProObj[0].p_purity_real_show]}
Tasquinimod									✔							{[allProObj[0].p_purity_real_show]}
CAY10603											++++ HDAC6, IC50: 2 pM					{[allProObj[0].p_purity_real_show]}
Tubastatin A											+++ HDAC6, IC50: 15 nM					{[allProObj[0].p_purity_real_show]}
Tubacin											++++ HDAC6, IC50: 4 nM					{[allProObj[0].p_purity_real_show]}
ACY-738											++++ HDAC6, IC50: 1.7 nM					{[allProObj[0].p_purity_real_show]}
Nexturastat A											++++ HDAC6, IC50: 5 nM					{[allProObj[0].p_purity_real_show]}
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			{[allProObj[0].p_purity_real_show]}
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			{[allProObj[0].p_purity_real_show]}
PCI-34051													+++ HDAC8, IC50: 10 nM			{[allProObj[0].p_purity_real_show]}
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			{[allProObj[0].p_purity_real_show]}
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			{[allProObj[0].p_purity_real_show]}
Abexinostat				++++ HDAC1, Ki: 7 nM	+++ HDAC10, IC50: 24 nM		+++ HDAC2, Ki: 19 nM	++++ HDAC3/SMRT, Ki: 8.2 nM			+++ HDAC6, Ki: 17 nM		+ HDAC8, IC50: 280 nM			{[allProObj[0].p_purity_real_show]}
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			{[allProObj[0].p_purity_real_show]}
HPOB				+ HDAC1, IC50: 2.9 μM	+ HDAC10, IC50: 3.0 μM		+ HDAC2, IC50: 4.4 μM	+ HDAC3, IC50: 1.7 μM			++ HDAC6, IC50: 56 nM		+ HDAC8, IC50: 2.8 μM			{[allProObj[0].p_purity_real_show]}
Quisinostat 2HCl				++++ HDAC1, IC50: 0.11 nM	++++ HDAC10, IC50: 0.46 nM	++++ HDAC11, IC50: 0.37 nM	++++ HDAC2, IC50: 0.33 nM	++++ HDAC3, IC50: 4.86 nM	++++ HDAC4, IC50: 0.64 nM	++++ HDAC5, IC50: 3.69 nM			++++ HDAC8, IC50: 4.26 nM			{[allProObj[0].p_purity_real_show]}
Domatinostat				+ HDAC1, IC50: 1.20 μM	+ HDAC10, IC50: 21 μM	+ HDAC11, IC50: 9.7 μM	+ HDAC2, IC50: 1.12 μM	+ HDAC3, IC50: 0.57 μM		+ HDAC5, IC50: 11.3 μM				+ HDAC9, IC50: 50 μM		{[allProObj[0].p_purity_real_show]}
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		{[allProObj[0].p_purity_real_show]}
Pracinostat				++ HDAC1, IC50: 49 nM	+++ HDAC10, IC50: 40 nM	++ HDAC11, IC50: 93 nM	++ HDAC2, IC50: 96 nM	+++ HDAC3, IC50: 43 nM	++ HDAC4, IC50: 56 nM	+++ HDAC5, IC50: 47 nM	+ HDAC6, IC50: 1.008 μM	++ HDAC7, IC50: 137 nM	++ HDAC8, IC50: 140 nM	++ HDAC9, IC50: 70 nM		{[allProObj[0].p_purity_real_show]}
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 nM		{[allProObj[0].p_purity_real_show]}
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。

BRD3308 生物活性

描述

Selective histone deacetylases (HDAC) are a family of enzymes that regulate the transcription of cellular and viral genes. HDAC inhibitors have emerged as anti-latency therapeutic options for persistent HIV-1 infection. BRD3308 is a highly selective, small-molecule inhibitor of HDAC3 with an IC50 value of 54nM. BRD3308 is 23-fold more selective for HDAC3 over HDAC1 (IC50=1.26μM) and HDAC2 (IC50=1.34μM). The IC50 values of BRD3308 for HDAC4–9 are above 33μM. Treatment of 2D10 cells with 10–30µM BRD3308 for 12 hours increased the expression of HIV-1. The overnight exposure of patients’ resting CD4+ T cells to 15µM BRD3308 induced viral outgrowth. Treatment of PBMCs with various concentrations of BRD3308 (5, 10, 15, or 30µM) for 24 hours did not significantly decrease cell viability compared with vehicle-treated controls^[3]. In male ZDF rats, a model of type 2 diabetes, administration with BRD3308 (5mg/kg, i.p.) every second day starting from 7 weeks of age prior to the development of hyperglycemia significantly lowered glycemia by 61% and increased average steady-state glucose-infusion rate compared to vehicle-treated group. The plasma insulin concentration was 84% higher in BRD3308-treated rats. The pancreatic islet area in BRD3308-treated animals was also significantly larger than that in the control group^[4].

BRD3308 参考文献

[1]Dirice E, Ng R, et al. Isoform-selective inhibitor of histone deacetylase 3 (HDAC3) limits pancreatic islet infiltration and protects female nonobese diabetic mice from diabetes. J Biol Chem. 2017 Aug 31. pii: jbc.M117.804328.

[2]Wagner FF, Lundh M, et al. An Isochemogenic Set of Inhibitors To Define the Therapeutic Potential of Histone Deacetylases in β-Cell Protection. ACS Chem Biol. 2016 Feb 19;11(2):363-74.

[3]Barton KM, Archin NM, Keedy KS, Espeseth AS, Zhang YL, Gale J, Wagner FF, Holson EB, Margolis DM. Selective HDAC inhibition for the disruption of latent HIV-1 infection. PLoS One. 2014 Aug 19;9(8):e102684.

[4]Lundh M, Galbo T, Poulsen SS, Mandrup-Poulsen T. Histone deacetylase 3 inhibition improves glycaemia and insulin secretion in obese diabetic rats. Diabetes Obes Metab. 2015 Jul;17(7):703-7.

BRD3308 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.48mL

0.70mL

0.35mL

17.40mL

3.48mL

1.74mL

34.81mL

6.96mL

3.48mL

BRD3308 技术信息

CAS号	1550053-02-5
分子式	C₁₅H₁₄FN₃O₂
分子量	287.289

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 250 mg/mL(870.2 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

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BRD3308 生物活性

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最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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