[CAS NO. 1640282-31-0] I-CBP112

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PRODUCTS SPECIFICATIONS [1640282-31-0]

Catalog

HY-19541

Brand

MCE

CAS

1640282-31-0

DESCRIPTION [1640282-31-0]

Overview

MDL	-
Molecular Weight	468.59
Molecular Formula	C27H36N2O5
SMILES	COC1=C(OC)C=C(C2=CC(OC[C@H]3CCCN(C)C3)=C(OCCN(C(CC)=O)C4)C4=C2)C=C1

For research use only. We do not sell to patients.

2 Publications Citing Use of MCE

Summary

I-CBP112 is a specific and potent acetyl-lysine competitive protein-protein interaction inhibitor, that inhibits the CBP/p300 bromodomains, enhances acetylation by p300.

IC50 & Target

IC50: 5.5±1.1 μM (CBP/p300, Leukemia cell); 9.1±1.2 μM (CBP/p300, Prostate cancer cell) ^[1]

In Vitro

I-CBP112 significantly enhances acetylation by p300 at the histone H3K18 and H3K23 sites. I-CBP112 stimulated H3K18ac by ~3-fold, I-CBP112 induced enhances acetylation of these same sites by CBP as well as at H4K5. The EC ₅₀ ’s of activation of I-CBP112 on p300- and CBP-mediated H3K18 acetylation are ~2 μM ^[1] . Exposure of human and mouse leukemic cell lines to I-CBP112 results in substantially impaired colony formation and induces cellular differentiation without significant cytotoxicity. Exposure of the BioMAP primary cell panel to I-CBP112 results in a unique response on cytokine and marker protein expression ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

I-CBP112 significantly reduces the leukemia-initiating potential of mLL-AF9+ AmL cells in a dose-dependent manner in vitro and in vivo. The synergistic effects of I-CBP112 and current standard therapy (doxorubicin) as well as emerging treatment strategies (BET inhibition) provide new opportunities for combinatorial treatment of leukemia and potentially other cancers ^[2] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

1M HCl : 100 mg/mL ( 213.41 mM ; ultrasonic and adjust pH to 1 with HCl)

DMSO : ≥ 32 mg/mL ( 68.29 mM )

* "≥" means soluble, but saturation unknown.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1341 mL	10.6703 mL	21.3406 mL
5 mM	0.4268 mL	2.1341 mL	4.2681 mL
10 mM	0.2134 mL	1.0670 mL	2.1341 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution
2.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

Solubility: ≥ 2.5 mg/mL (5.34 mM); Clear solution

* All of the co-solvents are available by MCE.