CBP/p300 bromodomain inhibitor (IC50values are 0.142-0.17 and 0.625μM for CBP and p300 respectively). Selective for CBP and p300 over ATAD2, BAZ2B, BRD2(2), BRD4(1), PB1(5), PCAF, PHIP(2) and TIF1αbromodomains in a BLI assay. Accelerates FRAP recovery in
Storage Temp
Store at -20°C,Desiccated
Shipped In
Ice chest + Ice pads
Grade
Moligand™
Action Type
INHIBITOR
Mechanism of action
Inhibitor of CREB binding protein;Inhibitor of E1A binding protein p300
Product Description
I-CBP112 is a potent and selective CBP/p300 inhibitor with dissociation constant (KD) of 151 ± 6 nM and 167 ± 8 nM for CBP and p300, respectively.
Soluble in DMSO, the highest concentration (mg / ml): 94, the highest concentration (mm): 200.60; Soluble in H2O, the highest concentration (mg / ml): 94, the highest concentration (mm): 200.60; Dissolved in ethanol, the highest concentration (mg / ml): 9
1.Zeng L, Zhang Q, Gerona-Navarro G, Moshkina N, Zhou MM. (2008) Structural basis of site-specific histone recognition by the bromodomains of human coactivators PCAF and CBP/p300.. Structure, 16 (4):(643-52). [PMID:18400184]
2.Iyer NG, Ozdag H, Caldas C. (2004) p300/CBP and cancer.. Oncogene, 23 (24):(4225-31). [PMID:15156177]
3.Kalkhoven E. (2004) CBP and p300: HATs for different occasions.. Biochem Pharmacol, 68 (6):(1145-55). [PMID:15313412]
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J2130447