MCE 的所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务。

Domatinostat tosylate

CAS No. : 1186222-89-8

MCE 国际站：Domatinostat tosylate

产品活性：Domatinostat tosylate (4SC-202) 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。

研究领域：Cell Cycle/DNA Damage  |  Epigenetics  |  Apoptosis

作用靶点：HDAC  |  Apoptosis

In Vitro: Domatinostat tosylate significantly reduces proliferation of all epithelial and mesenchymal UC cell lines (IC₅₀ 0.15-0.51 μM), inhibits clonogenic growth and induces caspase activity. Domatinostat tosylate provokes apoptosis activation in CRC cells, while caspase inhibitors (z-VAD-CHO and z-DVED-CHO) significantly alleviate Domatinostat tosylate-exerted cytotoxicity in CRC cells. Meanwhile, Domatinostat tosylate induces dramatic G2-M arrest in CRC cells. Further studies show that AKT activation might be an important resistance factor of Domatinostat tosylate. Domatinostat tosylate-induced cytotoxicity is dramatically potentiated with serum starvation, AKT inhibition (by perifosine or MK-2206), or AKT1-shRNA knockdown in CRC cells. On the other hand, exogenous expression of constitutively active AKT1 (CA-AKT1) decreases the sensitivity by Domatinostat tosylate in HT-29 cells. Notably, Domatinostat tosylate, at a low concentration, enhances oxaliplatin-induced in vitro anti-CRC activity. Domatinostat tosylate treatment induces potent cytotoxic and proliferation-inhibitory activities against established HCC cell lines (HepG2, HepB3, SMMC-7721) and patient-derived primary HCC cells. Domatinostat tosylate induces apoptosis signal-regulating kinase 1 (ASK1) activation, causing it translocation to mitochondria and physical association with Cyp-D.

In Vivo: Oral gavage of Domatinostat tosylate inhibits HT-29 xenograft growth in nude mice, and when combined with oxaliplatin, its activity is further strengthened.

相关产品：SY-5609  |  BRD4 Inhibitor-18  |  8α-Tigloyloxyhirsutinolide 13-O-acetate  |  AAPK-25  |  Dutasteride-¹³C₆  |  Oleic acid-¹³C  |  Anticancer agent 120  |  Abacavir sulfate  |  Meloxicam-d₃-1  |  YF479  |  Thailanstatin D  |  SB-218078  |  Toyocamycin  |  Sorafenib-d₄  |  Busulfan  |  PTC-028  |  Dinaciclib  |  CR-1-31-B  |  142I5  |  Farudodstat  |  Ecteinascidin 770  |  AT9283  |  Staurosporine  |  SNS-032  |  AZA1  |  Antitumor agent-96  |  Bleomycin A5  |  Xevinapant  |  Mangiferin  |  Cambinol

热门产品线：重组蛋白  |  化合物库  |  天然产物  |  荧光染料  |  PROTAC  |  同位素标记物  |  寡核苷酸  |  抗体  |  点击化学

Trending products：Recombinant Proteins  |  Bioactive Screening Libraries  |  Natural Products  |  Fluorescent Dye  |  PROTAC  |  Isotope-Labeled Compounds  |  Oligonucleotides  |  Antibodies  |  Click Chemistry

品牌介绍:
•   MCE (MedChemExpress) 拥有200 多种全球独家化合物库，我们致力于为全球科研客户提供前沿最全的高品质小分子活性化合物；
•   50,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领；
•   产品种类涵盖各种重组蛋白，多肽，常用试剂盒 ，更有 PROTAC、ADC 等特色产品，广泛应用于新药研发、生命科学等科研项目；
•   提供虚拟筛选，离子通道筛选，代谢组学分析检测分析，药物筛选等专业技术服务；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种顶级期刊及制药专利收录了MCE客户的科研成果；
•   专业团队跟踪最新的制药及生命科学研究进展，为您提供全球最新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。