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ICCB280

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Chemical Structure| 2041072-41-5 同义名 : -
CAS号 : 2041072-41-5
货号 : A1375546
分子式 : C23H18N2O4
纯度 : 99%+
分子量 : 386.4
MDL号 : MFCD11113794
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 85 mg/mL(219.98 mM)，配合低频超声助溶，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：
生物活性
描述 The C/EBP proteins form a family of transcription factors with at least seven members. These proteins consist of three structural components which include a C-terminal leucine-zipper, a basic DNA-binding region and a N-terminal transactivating region. Dimerization through the leucine-zipper leads to formation of homo- and heterodimers which then bind with their two basic regions to often non-symmetric DNA-sequences in the promoter/enhancer regions of a variety of genes. Expression of C/EBP is prominent in adipocytes, hepatocytes and monocytes/macrophages, and here these proteins are involved in tissue-specific gene expression. Target genes for C/EBP include those for acute phase response genes in liver cells and for cytokine genes in monocytes/macrophages[3]. C/EBP alpha is concentrated in the upper epidermis in a predominantly cytoplasmic location within cells, whereas the highest levels of C/EBP beta and CHOP are seen in the mid-epidermis, mainly within nuclei. High levels of C/EBP beta and CHOP (but not C/EBP alpha) are also observed in hair follicles and sebaceous glands[4]. C/EBPalpha is a particularly potent regulator of cell-cycle exit and is induced in terminally differentiating adipocytes and myeloid cells, where it also activates differentiation-specific genes. The growth-inhibiting activity of C/EBPalpha suppresses tumorigenesis in myeloid cells and possibly other tissues[5]. ICCB280 was capable of inducing differentiation and apoptosis of ATRA-resistant patient blasts strongly signify that the activity of this compound can overcome resistance to other current therapies for AML with an unfavorable prognosis. ICCB280 (10 μM; 2-8 d) increases the C/EBPα expression (mRNA and protein) and modulates its target genes in HL-60 cells. ICCB280 (0.1-50 μM; 48 h) suppresses the HL-60 cell growth, with an IC50 of 8.6 μM[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.59mL

0.52mL

0.26mL

12.94mL

2.59mL

1.29mL

25.88mL

5.18mL

2.59mL
参考文献

[1]Radomska HS, Jernigan F, Nakayama S, et al. A Cell-Based High-Throughput Screening for Inducers of Myeloid Differentiation. J Biomol Screen. 2015;20(9):1150-1159.

[2]Sridhar R, Takei H, Syed R, Kobayashi IS, Hui LB, Kamal A, Tenen DG, Kobayashi SS. Styryl Quinazolinones as Potential Inducers of Myeloid Differentiation via Upregulation of C/EBPα. Molecules. 2018 Aug 3;23(8):1938. doi: 10.3390/molecules23081938. PMID: 30081475; PMCID: PMC6222906.

[3]A Wedel,et al. The C/EBP family of transcription factors. Immunobiology.1995 Jul;193(2-4):171-85.

[4]E V Maytin,et al. Transcription factors C/EBP alpha, C/EBP beta, and CHOP (Gadd153) expressed during the differentiation program of keratinocytes in vitro and in vivo. J Invest Dermatol. 1998 Mar;110(3):238-46.

[5]Peter F Johnson. Molecular stop signs: regulation of cell-cycle arrest by C/EBP transcription factors. J Cell Sci. 2005 Jun 15;118(Pt 12):2545-55.