ITSA-1 | HDAC | AmBeed-信号通路专用抑制剂

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ITSA-1 {[allProObj[0].p_purity_real_show]}

货号：A879167

ITSA-1是一种组蛋白去乙酰化酶（HDAC）激活剂，可以对抗曲霉素A（TSA）诱导的细胞周期停滞、组蛋白乙酰化和转录激活。

ITSA-1 化学结构
CAS号：200626-61-5

ITSA-1 3D分子结构
CAS号：200626-61-5

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ITSA-1 纯度/质量文件产品仅供科研

货号：A879167 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-B (Maize), IC50: 3.4 μM HD1-A (Maize), IC50: 100 nM															{[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	EGFR,HER2	{[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 (Reh cells), IC50: 20 nM HDAC (MOLT-4 cells), IC50: 5 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				✔											NF-κB,p53	{[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。

ITSA-1 生物活性

描述

ITSA-1 acts as HDAC activator and counteracts the effects of trichostatin A on cell cycle arrest, histone acetylation, and transcriptional activation. Treatment with ITSA-1 at a concentration of 50 μM in A549 cells helps restore the TSA-arrested cell population to a normal cell cycle distribution and is capable of maintaining cell cycle rescue over extended periods. Additionally, a 50 μM ITSA-1 treatment for 5 hours in A549 cells decreases apoptosis in cells treated with TSA. When applied to A549 and murine ES cells for 2 hours, ITSA-1 at the same concentration suppresses TSA-induced histone acetylation, with the suppression effect only noticeable when ITSA-1 is administered simultaneously with or after TSA treatment. Furthermore, a 30-minute treatment with ITSA-1 at 50 μM in murine ES cells inhibits TSA-induced transcription^[1].

ITSA-1 动物研究

Animal study

Administering ITSA-1 at a dose of 0.5 mg/kg via intraperitoneal injection three times a week for eight weeks in CBS^+/- mice modulates deacetylation activity and reduces the expression of IL-6 and TNF-α, consequently diminishing histone acetylation-dependent inflammatory signaling^[2].

ITSA-1 参考文献

[1]Koeller KM et al. Chemical genetic modifier screens: small molecule trichostatin suppressors as probes of intracellular histoneand tubulin acetylation. Chem Biol. 2003 May;10(5):397-410.

[2]Behera J, et al. Hydrogen Sulfide Promotes Bone Homeostasis by Balancing Inflammatory Cytokine Signaling in CBS-Deficient Mice through an Epigenetic Mechanism. Sci Rep. 2018 Oct 15;8(1):15226.

ITSA-1 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

3.42mL

0.68mL

0.34mL

17.12mL

3.42mL

1.71mL

34.23mL

6.85mL

3.42mL

ITSA-1 技术信息

CAS号	200626-61-5
分子式	C₁₃H₇Cl₂N₃O
分子量	292.12

别名
运输	蓝冰

存储条件

粉末 Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 30 mg/mL(102.7 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

ITSA-1 {[allProObj[0].p_purity_real_show]}

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全球学术期刊中引用的产品

ITSA-1 质控信息

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ITSA-1 参考文献

ITSA-1 实验方案

ITSA-1 技术信息

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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