I-CBP112 --- p300/CBP Bromodomain Inhibitor


Catalog No. size PriceQuantity
M60128-2D 10 mM in DMSO (0.427 mL) $139
M60128-2S 2mg solid $139
M60128-10S 10 mg solid $556

Description

I-CBP112 is a highly potent and selective p300/CBP bromodomain inhibitor (IC50 ~0.14-0.17 µM for CBP and ~0.625 µM for p300). It binds CBP and p300 bromodomains directly, and has excellent selectivity against the entire bromodomain family in a BLI assay. It accelerated FRAP recovery at 1 µM and no significant cytotoxicity up to 50 μM in U2OS cells. p300 and CBP are transcriptional co-activators that modulate DNA replication, DNA repair, cell growth, transformation, and development. Both p300 and CBP contain bromodomains, which mediate their binding to acetylated lysine residues on histones and other proteins. Chromosomal translocations of p300 or CBP with MOZ, MLL have been observed in acute myeloid leukemia. CBP has also been associated with Amyotrophic lateral sclerosis (ALS), a neurodegenerative disease with progressive degeneration of motor neurons in the brain and spinal cord, Alzheimer's disease and polyglutamine diseases such as Spinal and Bulbar Muscular Atrophy and Huntington’s disease.

Product information

CAS Number: 1640282-31-0

Molecular Weight: 468.59

Formula: C27H36N2O5

Chemical Name: (S)-1-(7-(3,4-dimethoxyphenyl)-9-((1-methylpiperidin-3-yl)methoxy)-2,3-dihydrobenzo[f][1,4]oxazepin-4(5H)-yl)propan-1-one

Smiles: CN1CCC[C@@H](C1)COC1=CC(=CC2CN(CCOC=21)C(=O)CC)C1=CC(OC)=C(C=C1)OC

InChiKey: YKNAKDFZAWQEEO-IBGZPJMESA-N

InChi: InChI=1S/C27H36N2O5/c1-5-26(30)29-11-12-33-27-22(17-29)13-21(20-8-9-23(31-3)24(14-20)32-4)15-25(27)34-18-19-7-6-10-28(2)16-19/h8-9,13-15,19H,5-7,10-12,16-18H2,1-4H3/t19-/m0/s1

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 50 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

I-CBP112 was used at 1-10 µM final concentration in various in vitro assays.

References:

  1. Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34.
  2. Picaud S, et al. Generation of a Selective Small Molecule Inhibitor of the CBP/p300 Bromodomain for Leukemia Therapy. Cancer Res. 2015 Dec 1;75(23):5106-19.

Products are for research use only. Not for human use.


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