I-CBP112 (Hydrochloride)

Catalog #
27336
$240 *
Size: 5 mg
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Description

I-CBP112 (Hydrochloride) is a selective inhibitor of cAMP responsive-element binding protein (CREBBP) and E1A binding protein p3000 (EP3000). The inhibitor has been shown to decrease EZH2 activity and to inhibit trimethylation of lysine 27 on histone H3 in cultured human AML HL-60 and OCI-AML3 cells. It has the same effect on primary AML cells in a dose-dependent manner.

This product has been cited 2 times.

Synonyms
ICBP112, ICBP
Product Info
Storage and Usage
Citations2
Supplied As
A crystalline solid
Target(s)
CREBBP, EP3000
Formula
C27H36N2O5
MW
505.1 Da
Solubility
Soluble in DMSO, ethanol, and dimethylformamide at approximately 16 mg/ml.
Biological Activity
I-CBP112 directly binds the bromodomains of CREBBP and EP300 with a KD of 0.5 and 0.625 μM, respectively. It shows weak cross-reactivity with bromodomain and extra-terminal (BET) proteins and no reactivity with other bromodomain-containing proteins.
CAS Registry #
NA
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