|2-((4-氯苯基)氨基)噻唑-4-甲酸乙酯|CsnPharm

CAS No.: 165682-93-9

O4I2 Catalog No. CSN10949

Synonyms: O4I2

O4I2 is an Oct3/4 inducer which can induce expression of pluripotent-associated genes.

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生物活性

实验方案

技术信息

生物活性

描述Oct3/4 (Octamer-binding transcription factor 4), also referred to POU5F1, Oct4A, Oct3, or Oct4, is a member of the POU family of transcription factors1 expressed specifically in pluripotent cells, including embryonic stem cells (ESCs) and induced pluripotent stem cells (iPSCs), it plays important role in regulation of the cellular pluripotency core network^[2]. O4I2, an azaindole derivative, was reported to enhance Oct3/4 activation. AZ study showed that O4I2 demonstrated the highest Oct3/4 activation in HEK-Oct3/4 reporter cells in 3.5-fold at 20 μM after 72 h of treatment; After 72 h treatment with 20 μM in HEK293 cells, the immunoblot results revealed a clear accumulation of Oct3/4 and an increased level of Nanog protein, and analysis by qRTPCR suggested a significant induction of stemness-associated genes after stimulation with O4I2, including Oct3/4, Nanog, and Sox2, while the level of Lin28 remained unaffected and Rex1 was even reduced. In human primary skin fibroblasts (HFs), qRT-PCR analysis detected a marked increase of Oct3/ 4 expression, the induction of Lin28 and Rex1 and a moderate activation of Nanog after 48 h treatment with 20 μM O4I2. Moreover, immunocytochemistry detected coexpression of Oct3/4 and Sox2 as well as Nanog and Klf4 in HF cells treated with O4I2 for 5 days. O4I2 can also promote Oct3/4 accumulation in embryonal carcinoma NCCIT cells (NCCIT-Oct3/4) and HeLa cells ^[3].
作用机制O4I2 promotes Oct3/4 expression by activating its promoter site but also stabilize the Oct3/4 protein, which regulates of the cellular pluripotency core network^[3].
参考文献

[1] Cheng X, Yoshida H, et al. Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4. J Med Chem. 2015 Aug 13;58(15):5742-50.
[2] Oct4
[3] Cheng X, Yoshida H, Raoofi D, Saleh S, Alborzinia H, Wenke F, Göhring A, Reuter S, Mah N, Fuchs H, Andrade-Navarro MA, Adjaye J, Gul S, Utikal J, Mrowka R, Wölfl S. Ethyl 2-((4-Chlorophenyl)amino)thiazole-4-carboxylate and Derivatives Are Potent Inducers of Oct3/4. J Med Chem. 2015 Aug 13;58(15):5742-50. doi: 10.1021/acs.jmedchem.5b00226. Epub 2015 Jul 23.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 3.5367 mL
- 17.6837 mL
- 35.3674 mL
- 5 mM
- 0.7073 mL
- 3.5367 mL
- 7.0735 mL
- 10 mM
- 0.3537 mL
- 1.7684 mL
- 3.5367 mL

技术信息

CAS号

165682-93-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C12H11ClN2O2S

运输

蓝冰

分子量

282.75

别名

O4I2

溶解度

DMSO	330.0 mg/mL (1167.1 mM)
Water	insoluble

动物实验配方

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