I-CBP112( I-CBP112 | I-CBP-112 | I-CBP 112 )

Catalog No. M12486 CAS No. 1640282-31-0

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Product Name

I-CBP112
Note

Research use only, not for human use.
Brief Description

A specific and potent inhibitor of CBP/p300 bromodomain with Kd of 150-170 nM.
Description

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

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In Vivo

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Synonyms

I-CBP112 | I-CBP-112 | I-CBP 112
Pathway

Chromatin/Epigenetic
Target

HAT
Recptor

CBP/p300(Leukemiacell)
Research Area

Cancer
Indication

——

CAS Number

1640282-31-0
Formula Weight

468.5851
Molecular Formula

C27H36N2O5
Purity

>98% (HPLC)
Solubility

DMSO: ≥ 32 mg/mL
SMILES

CCC(N1CCOC2=C(OC[C@@H]3CN(C)CCC3)C=C(C4=CC=C(OC)C(OC)=C4)C=C2C1)=O
Chemical Name

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

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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