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I-CBP112

Chemical Structure : I-CBP112

CAS No.: 1640282-31-0

I-CBP112 (I-CBP 112, CBP/p300 inhibitor)

Catalog No.: PC-45646Not For Human Use, Lab Use Only.

I-CBP112 is a specific and potent inhibitor of CBP/p300 bromodomain with Kd of 150-170 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

I-CBP112 is a specific and potent inhibitor of CBP/p300 bromodomain with Kd of 150-170 nM.
I-CBP112 displaces H3K56ac from the CBP binding site with an IC50 of 170 nM.
I-CBP112 demonstrates 37-fold and 132-fold selectivity over BRD4 BD1 and BRD4 BD2, respectively.
I-CBP112 increases the cytotoxic activity of JQ1 in leukemic cells.
I-CBP112 impaires the disease-initiating self-renewal leukemic cells in vitro and in vivo without causing significant cytotoxicity.

Physicochemical Properties

M.Wt 468.5851
Formula C27H36N2O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 32 mg/mL

Chemical Name/SMILES

1-Propanone, 1-[7-(3,4-dimethoxyphenyl)-2,3-dihydro-9-[[(3S)-1-methyl-3-piperidinyl]methoxy]-1,4-benzoxazepin-4(5H)-yl]-

References

1. Picaud S, et al. Cancer Res. 2015 Dec 1;75(23):5106-19.

2. Zucconi BE, et al. Biochemistry. 2016 Jul 12;55(27):3727-34.

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