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Biological Activity: I-CBP112 directly binds the bromodomains of CREBBP and EP300 with aKD of 0.5 and 0.625 µM, respectively. It shows weak cross-reactivity with bromodomain andextra-terminal (BET) proteins and no reactivity with other bromodomain-containing proteins.
Description: I-CBP112 (Hydrochloride) is a selective inhibitor of cAMP responsive-elementbinding protein (CREBBP) and E1A binding protein p3000 (EP3000). The inhibitor has beenshown to decrease EZH2 activity and to inhibit trimethylation of lysine 27 on histone H3 incultured human AML HL-60 and OCI-AML3 cells. It has the same effect on primary AML cells ina dose-dependent manner.
Solubility: Soluble in DMSO, ethanol, and dimethylformamide at approximately 16 mg/ml.
Storage Stability: Store at or below -20°C for up to two years. Protect stock solutions from moisture. Avoid freeze/thaw cycles.
Supplied As: A crystalline solid
Target: CREBBP, EP3000
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
References: 1. Iver, N.G. et al.,Oncogene. 2004;23(24):4225-4231.
2. Petrij, F. et al., Nature. 1995;376(6538):348-351
3. Vizmanos, J.L. et al., Gene Chromsome Canc. 2003;36:402-405
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