Remodelin | Histone Acetyltransferase Inhibitor | AmBeed-信号通路专用抑制剂

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Remodelin {[allProObj[0].p_purity_real_show]}

货号：A691133

Remodelin is a potent and selective inhibitor of the acetyl-transferase protein NAT10.

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Type	HazMat fee for 500 gram (Estimated)
Excepted Quantity	USD 0.00
Limited Quantity	USD 15-60
Inaccessible (Haz class 6.1), Domestic	USD 80+
Inaccessible (Haz class 6.1), International	USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic	USD 100+
Accessible (Haz class 3, 4, 5 or 8), International	USD 200+

Remodelin 化学结构
CAS号：949912-58-7

Remodelin 3D分子结构
CAS号：949912-58-7

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Remodelin 纯度/质量文件产品仅供科研

货号：A691133 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。

Remodelin 生物活性

描述

Remodelin is an orally active and selective inhibitor of acetyltransferase NAT10. Remodelin inhibits NAT10 activitity and slows DNA replication and suppresses growth of prostate cancer cells.Additionally, Remodelin curtails the development of prostate cancer and hepatocellular carcinoma in xenograft models and prolongs the lifespan in models of Hutchinson-Gilford Progeria Syndrome (HGPS)^[1].^[2].^[3].^[4].

体外研究

When applied in concentrations ranging from 10 to 40 μΜ over a period of 1 to 7 days, Remodelin systematically diminishes NAT10 activity and cell growth in a concentration-responsive manner across both AR-positive and AR-negative prostate cancer cell types^[2].

At a dosage of 20 μΜ for a duration of 24 hours, it specifically reduces NAT10 activity and decelerates DNA synthesis in prostate cancer cells^[2].

Moreover, a 7-day treatment with Remodelin at 1 μΜ lessens nuclear abnormalities and bolsters genomic integrity in LmnaG609G/G609G fibroblasts^[3].

Remodelin 参考文献

[1]Larrieu D, et al. Chemical inhibition of NAT10 corrects defects of laminopathic cells. Science. 2014 May 2;344(6183):527-32.

[2]Ma N, et.al. Inhibition of N-Acetyltransferase 10 Suppresses the Progression of Prostate Cancer through Regulation of DNA Replication. Int J Mol Sci. 2022 Jun 12;23(12):6573.

[3]Balmus G, et.al. Targeting of NAT10 enhances healthspan in a mouse model of human accelerated aging syndrome. Nat Commun. 2018 Apr 27;9(1):1700.

[4]Zhang X, et.al. N-Acetyltransferase 10 Enhances Doxorubicin Resistance in Human Hepatocellular Carcinoma Cell Lines by Promoting the Epithelial-to-Mesenchymal Transition. Oxid Med Cell Longev. 2019 Jul 1;2019:7561879.

Remodelin 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.54mL

0.71mL

0.35mL

17.71mL

3.54mL

1.77mL

35.42mL

7.08mL

3.54mL

Remodelin 技术信息

CAS号	949912-58-7
分子式	C₁₅H₁₄N₄S
分子量	282.363

别名
运输	蓝冰

存储条件

粉末 Keep in dark place,Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 120 mg/mL(424.98 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

Remodelin {[allProObj[0].p_purity_real_show]}

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Remodelin 参考文献

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