Domatinostat | 4SC-202 free base | Apoptosis Inducer | AmBeed-信号通路专用抑制剂

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Domatinostat {[allProObj[0].p_purity_real_show]}

货号：A161236 同义名： 4SC-202 free base;4SC-202

Domatinostat is a selective class I HDAC inhibitor with IC50 of 1.20 μM, 1.12 μM, and 0.57 μM for HDAC1, HDAC2, and HDAC3, respectively. Also displays inhibitory activity against Lysine specific demethylase 1 (LSD1).

Domatinostat 化学结构
CAS号：910462-43-0

Domatinostat 3D分子结构
CAS号：910462-43-0

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Domatinostat 纯度/质量文件产品仅供科研

货号：A161236 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, 2024, 101755. Ambeed. [ A399663 ]; • EMBO J., 2024. Ambeed. [ A295334 ]; • JMC, 2024, 67(20): 18265-18289. Ambeed. [ A538667 , A341145 , A117430 , A172297 ]; • JMC, 2024. Ambeed. [ A210558 , A1518164 ]; • Cell Death Discov., 2024, 10, 436. Ambeed. [ A384235 ]; 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														99%+
MC1568	++ HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM															96%
Trichostatin A			++++ HDAC, IC50: ~1.8 nM													99%+
Scriptaid			✔													99%+
Valproic acid sodium			✔												Autophagy	97%
AR-42			+++ HDAC, IC50: 30 nM													99%+
Dacinostat			+++ HDAC, IC50: 32 nM													98+%
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	99%+
M344			++ HDAC, IC50: 100 nM													99%+
Splitomicin			+ Sir2p, IC50: 60 μM													95%
Panobinostat			++++ HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM													98%
Sodium 4-Phenylbutyrate			✔													98%
Vorinostat			+++ HDAC, IC50: ~10 nM													98%
Curcumin			✔												NF-κB,Nrf2	98%
Belinostat			+++ HDAC, IC50: 27 nM													98%
RG-2833				++ HDAC1, Ki: 32 nM				++ HDAC3, Ki: 5 nM								98%
Valproic acid				+ HDAC1, IC50: 0.4 mM												98%
BG45				+ HDAC1, IC50: 2 μM			+ HDAC2, IC50: 2.2 μM	+ HDAC3, IC50: 289 nM								99%+
Entinostat				+ HDAC1, IC50: 0.51 μM				+ HDAC3, IC50: 1.7 μM								98%
Resminostat				+++ HDAC1, IC50: 42.5 nM				++ HDAC3, IC50: 50.1 nM			++ HDAC6, IC50: 71.8 nM					98+%
Romidepsin				+++ HDAC1, IC50: 36 nM			+++ HDAC2, IC50: 47 nM									99%+
Parthenolide				✔											NF-κB,p53	97% HPLC
Tacedinaline				+ HDAC1, IC50: 0.9 μM			+ HDAC2, IC50: 0.9 μM	+ HDAC3, IC50: 1.2 μM								98%
Mocetinostat				++ HDAC1, IC50: 0.15 μM		+ HDAC11, IC50: 0.59 μM	+ HDAC2, IC50: 0.29 μM	+ HDAC3, IC50: 1.66 μM								98%
WT-161				++++ HDAC1, IC50: 8.35 nM			+++ HDAC2, IC50: 15.4 nM				++++ HDAC6, IC50: 0.4 nM					99%+
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					99%+
Tucidinostat				++ HDAC1, IC50: 95 nM	++ HDAC10, IC50: 78 nM		++ HDAC2, IC50: 160 nM	++ HDAC3, IC50: 67 nM								99%+
Santacruzamate A							++++ HDAC2, IC50: 119 pM									99%+
(E,E)-RGFP966								++ HDAC3, IC50: 80 nM								99%+
LMK-235									+++ HDAC4, IC50: 11.9 nM	++++ HDAC5, IC50: 4.2 nM						99%+
Tasquinimod									✔							99%+
CAY10603											++++ HDAC6, IC50: 2 pM					98%
Tubastatin A											+++ HDAC6, IC50: 15 nM					98%
Tubacin											++++ HDAC6, IC50: 4 nM					99%+
ACY-738											++++ HDAC6, IC50: 1.7 nM					99%+
Nexturastat A											++++ HDAC6, IC50: 5 nM					99%+
BRD73954											+++ HDAC6, IC50: 36 nM		++ HDAC8, IC50: 120 nM			98%
Tubastatin A HCl											+++ HDAC6, IC50: 15 nM		+ HDAC8, IC50: 854 nM			98%
PCI-34051													+++ HDAC8, IC50: 10 nM			99%+
Ricolinostat				++ HDAC1, IC50: 58 nM			++ HDAC2, IC50: 48 nM	++ HDAC3, IC50: 51 nM			++++ HDAC6, IC50: 4.7 nM		++ HDAC8, IC50: 100 nM			99%+
Droxinostat								+ HDAC3, IC50: 16.9 μM			+ HDAC6, IC50: 2.47 μM		+ HDAC8, IC50: 1.46 μM			99%+
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			98%+
Citarinostat				+++ HDAC1, IC50: 35 nM			+++ HDAC2, IC50: 45 nM	+++ HDAC3, IC50: 46 nM			++++ HDAC6, IC50: 2.6 nM		++ HDAC8, IC50: 137 nM			99%+
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			97%
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			99+%
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		99%+
TMP269									++ HDAC4, IC50: 157 nM	++ HDAC5, IC50: 97 nM		+++ HDAC7, IC50: 43 nM		+++ HDAC9, IC50: 23 nM		99%+
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		99%+
TMP195									++ HDAC4, Ki: 59 nM	++ HDAC5, Ki: 60 nM		+++ HDAC7, Ki: 26 nM		+++ HDAC9, Ki: 15 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。

Domatinostat 生物活性

靶点	HDAC10 HDAC10, IC50:21 μM HDAC3 HDAC3, IC50:0.57 μM HDAC9 HDAC9, IC50:50 μM HDAC11 HDAC11, IC50:9.7 μM
描述	Domatinostat (4SC-202 free base) tosylate has been identified as a significant inhibitor of proliferation across both epithelial and mesenchymal urinary carcinoma (UC) cell lines, showcasing IC50 values ranging from 0.15 to 0.51 μM. Domatinostat also induces apoptosis in colorectal cancer (CRC) cells, a process which can be notably mitigated by caspase inhibitors such as z-VAD-CHO and z-DVED-CHO, suggesting its cytotoxic effects are, in part, mediated through caspase activation. Additionally, Domatinostat induces a significant G2-M phase arrest in CRC cells. Research suggests that AKT activation might play a crucial role in resistance to Domatinostat's cytotoxic effects. The cytotoxicity induced by Domatinostat is greatly enhanced under conditions of serum starvation, inhibition of AKT (via perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. Conversely, the expression of constitutively active AKT1 (CA-AKT1) can reduce the sensitivity to Domatinostat in HT-29 cells. Remarkably, at low concentrations, Domatinostat can augment the anti-CRC activity of oxaliplatin in vitro. In the context of hepatocellular carcinoma (HCC), Domatinostat exhibits potent cytotoxic and anti-proliferative effects against both established HCC cell lines (such as HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. It activates apoptosis signal-regulating kinase 1 (ASK1), which then moves to mitochondria and physically associates with Cyp-D, indicating a pathway through which Domatinostat induces apoptosis in HCC cells.
体内研究	Moreover, oral administration of Domatinostat inhibits the growth of HT-29 xenografts in nude mice, an effect that is significantly enhanced when combined with oxaliplatin. This synergistic effect highlights Domatinostat's potential as a powerful component of combination therapies for cancer treatment, particularly in colorectal and hepatocellular carcinomas.
体外研究	Domatinostat (4SC-202 free base) tosylate has been identified as a significant inhibitor of proliferation across both epithelial and mesenchymal urinary carcinoma (UC) cell lines, showcasing IC50 values ranging from 0.15 to 0.51 μM. Domatinostat also induces apoptosis in colorectal cancer (CRC) cells, a process which can be notably mitigated by caspase inhibitors such as z-VAD-CHO and z-DVED-CHO, suggesting its cytotoxic effects are, in part, mediated through caspase activation. Additionally, Domatinostat induces a significant G2-M phase arrest in CRC cells. Research suggests that AKT activation might play a crucial role in resistance to Domatinostat's cytotoxic effects. The cytotoxicity induced by Domatinostat is greatly enhanced under conditions of serum starvation, inhibition of AKT (via perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. Conversely, the expression of constitutively active AKT1 (CA-AKT1) can reduce the sensitivity to Domatinostat in HT-29 cells. Remarkably, at low concentrations, Domatinostat can augment the anti-CRC activity of oxaliplatin in vitro. In the context of hepatocellular carcinoma (HCC), Domatinostat exhibits potent cytotoxic and anti-proliferative effects against both established HCC cell lines (such as HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. It activates apoptosis signal-regulating kinase 1 (ASK1), which then moves to mitochondria and physically associates with Cyp-D, indicating a pathway through which Domatinostat induces apoptosis in HCC cells.

Domatinostat 动物研究

Animal Administration	Mice: min = 80 mg/kg^[1], max = 120 mg/kg^[2]
Dose	Mice: min = 80 mg/kg^[1] (p.o.), max = 120 mg/kg^[2] (p.o.)
Administration	p.o.

Domatinostat 参考文献

[1]Pinkerneil M, et al. Evaluation of the Therapeutic Potential of the Novel Isotype Specific HDAC Inhibitor 4SC-202 in Urothelial Carcinoma Cell Lines. Target Oncol. 2016 Dec;11(6):783-798.

[2]Zhijun H, et al. Pre-clinical characterization of 4SC-202, a novel class I HDAC inhibitor, against colorectal cancer cells. Tumour Biol. 2016 Aug;37(8):10257-67.

[3]Fu M, et al. 4SC-202 activates ASK1-dependent mitochondrial apoptosis pathway to inhibit hepatocellular carcinoma cells. Biochem Biophys Res Commun. 2016 Mar 4;471(2):267-73

Domatinostat 实验方案

计算器

存储液制备

1mg

5mg

10mg

1 mM

5 mM

10 mM

2.23mL

0.45mL

0.22mL

11.17mL

2.23mL

1.12mL

22.35mL

4.47mL

2.23mL

Domatinostat 技术信息

CAS号	910462-43-0
分子式	C₂₃H₂₁N₅O₃S
分子量	447.51

别名	4SC-202 free base;4SC-202
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,2-8°C

溶解度

DMSO: 55 mg/mL(122.9 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

2% DMSO+30% PEG 300+5% Tween 80+water 10 mg/mL

Domatinostat {[allProObj[0].p_purity_real_show]}

Domatinostat 纯度/质量文件产品仅供科研

全球学术期刊中引用的产品

Domatinostat 质控信息

Domatinostat 生物活性

Domatinostat 动物研究

Domatinostat 参考文献

Domatinostat 实验方案

Domatinostat 技术信息

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HDAC10	HDAC10, IC50:21 μM
HDAC3	HDAC3, IC50:0.57 μM
HDAC9	HDAC9, IC50:50 μM
HDAC11	HDAC11, IC50:9.7 μM
HDAC5	HDAC5, IC50:11.3 μM
HDAC2	HDAC2, IC50:1.12 μM
HDAC1	HDAC1, IC50:1.20 μM

Domatinostat {[allProObj[0].p_purity_real_show]}

Domatinostat 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

Domatinostat 质控信息

Domatinostat 生物活性

Domatinostat 动物研究

Domatinostat 参考文献

Domatinostat 实验方案

Domatinostat 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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Domatinostat 纯度/质量文件产品仅供科研