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My Cart> Small Molecule Compounds > Inhibitors & Antagonists & Agonists > DNA Damage & DNA Repai > DomatinostatCAS：910462-43-0
Molecular Formula：C23H21N5O3S
Molecular Weight：447.51
Storage：Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：Light yellow to brown Solid
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| CAS | 910462-43-0 |
| Name | Domatinostat |
| Molecular Formula | C23H21N5O3S |
| Molecular Weight | 447.51 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | Light yellow to brown Solid |
| Storage | Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD28155264 |
| SMILES | O=C(NC1=CC=CC=C1N)/C=C/C2=CN(S(=O)(C3=CC=C(C4=CN(C)N=C4)C=C3)=O)C=C2 |
| Target Point | HDAC1，2，3，11 |
| Passage | DNA Damage/DNA Repair;Epigenetics;NF-κB |
| Background | Domatinostat is a selective class I HDAC inhibitor. |
| Biological Activity | Domatinostat 是一种 I 型 HDAC 抑制剂，能够抑制 HDAC1，HDAC2，和 HDAC3 的活性，IC50 值分别为 1.20 μM，1.12 μM 和 0.57 μM；同时能够抑制组蛋白赖氨酸特异性脱甲基酶1 (Lysine specific demethylase 1) 的活性[1-4]。 |
| In Vitro | Domatinostat(4SC-202游离碱)甲苯磺酸盐显著降低所有上皮和间充质UC细胞系的增殖(IC500.15-0.51μM)，抑制克隆生长并诱导caspase活性[1]。 Domatinostat(4SC-202游离碱)甲苯磺酸盐在CRC细胞中激活细胞凋亡，而半胱天冬酶抑制剂(z-VAD-CHO和z-DVED-CHO)显著减轻托马斯定位(4SC-202游离碱)甲苯磺酸盐在CRC细胞中发挥的细胞毒性。同时，Domatinostat(4SC-202游离碱)甲苯磺酸盐诱导CRC细胞中显著的G2-M停滞。进一步的研究表明，AKT激活可能是Domatinostat甲苯磺酸盐的重要耐药因子。 Domatinostat(4SC-202游离碱)甲苯磺酸盐诱导的细胞毒性通过血清饥饿，AKT抑制(通过哌立福辛或MK-2206)或CRC细胞中的AKT1-shRNA敲低而显著增强。另一方面，组成型活性AKT1(CA-AKT1)的外源性表达降低了Domatinostat甲苯磺酸盐在HT-29细胞中的敏感性。值得注意的是，Domatinostat(4SC-202游离碱)以低浓度甲苯磺酸酯增强奥沙利铂诱导的体外抗CRC活性[2]。 Domatinostat(4SC-202游离碱)甲苯磺酸盐处理诱导针对已建立的HCC细胞系(HepG2，HepB3，SMMC-7721)和患者来源的原代HCC细胞的有效细胞毒性和增殖抑制活性。 Domatinostat(4SC-202游离碱)甲苯磺酸盐诱导细胞凋亡信号调节激酶1(ASK1)激活，导致其易位至线粒体并与Cyp-D物理结合[3]。 |
| In Vivo | 口服灌胃Domatinostat(4SC-202游离碱)抑制裸鼠中HT-29异种移植物的生长，当与奥沙利铂合用时，其活性进一步增强[2]。 |
| Data Literature Source | [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 [4]. S.W.Henning，et al. Preclinical characterization of 4SC-202，a noval isotype specific HDAC inhibitor. |
| Unit | Bottle |
| Specification | 2mg 5mg |
是一种选择性的I类HDAC抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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