推薦產品
化驗
≥98% (HPLC)
形狀
powder
顏色
white to beige
溶解度
DMSO: 10 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
CN(C1)CCC[C@@H]1COC2=CC(C3=CC=C(OC)C(OC)=C3)=CC4=C2OCCN(C(CC)=O)C4
InChI
1S/C27H36N2O5/c1-5-26(30)29-11-12-33-27-22(17-29)13-21(20-8-9-23(31-3)24(14-20)32-4)15-25(27)34-18-19-7-6-10-28(2)16-19/h8-9,13-15,19H,5-7,10-12,16-18H2,1-4H3/t19-/m0/s1
InChI 密鑰
YKNAKDFZAWQEEO-IBGZPJMESA-N
應用
I-CBP112 has been used in cell culture and sample preparation, to verify the acetylation of VPS34 (vacuolar protein sorting 34), by p300 at K29, K771 and K781 and to diminish synergistic gene expression.
生化/生理作用
I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300 (IC50 = 0.142 and 0.625 μM, respectively). I-CBP112 has little activity against other bromodomains at concentrations up to 1 mM. For full characterization details, please see I-CBP112 on the Structural Genomics Consortium (SGC) website.
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc
I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors CREBBP (CBP) and EP300.
I-CBP112 is also known as (1-[7-(3,4-dimethoxyphenyl)-9-{[(3S)-1-methylpiperidin-3-yl]-methoxy}-2,3,4,5-tetrahydro-1,4-benzoxazepin-4-yl]propan-1-one). It has the ability to induce full-length p300/CBP nucleosome acetylation. It is a competitive inhibitor of acetyl-lysine. I-CBP112 regulates transcription of key inflammatory genes.
特點和優勢
I-CBP112 is an epigenetic chemical probe available through a partnership with the Structural Genomics Consortium (SGC). To learn more and view other SGC epigenetic probes, visit sigma.com/SGC.
This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.
其他說明
I-CBP112 has been expertly reviewed and recommended by the Chemical Probes Portal. For more information, please visit the I-CBP112 probe summary on the Chemical Probes Portal website.
相關產品
產品號碼
描述
訂價
訊號詞
Warning
危險聲明
危險分類
Aquatic Acute 1 - Aquatic Chronic 1
儲存類別代碼
11 - Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Generation of a selective small molecule inhibitor of the CBP/p300 bromodomain for leukemia therapy.
Picaud S, et al.
Cancer Research, 75(23), 5106-5119 (2015)
Time-Resolved Analysis Reveals Rapid Dynamics and Broad Scope of the CBP/p300 Acetylome.
Weinert BT, et al.
Cell, 174(1), 231-244 (2018)
Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain Ligand I-CBP112.
Zucconi BE, et al.
Biochemistry, 55(27), 3727-3734 (2016)
VPS34 Acetylation Controls Its Lipid Kinase Activity and the Initiation of Canonical and Non-canonical Autophagy.
Su H, et al.
Molecular Cell, 67(6), 907-921 (2017)
Synergistic gene expression during the acute phase response is characterized by transcription factor assisted loading.
Goldstein I, et al.
Nature Communications, 8(1), 1849-1849 (2017)
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