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I-CBP112 hydrochloride

SKU: orb1303026

Description

I-CBP112 is a potent and selective small molecule inhibitor of the CBP/p300 bromodomains. It reduces the leukemia-initiating potential of MLL-AF9+ AML cells in vitro and in vivo and shows synergistic effects with BET inhibitors like JQ1 and chemotherapeutics such as doxorubicin in oncology research.

Research Area

Epigenetics & Chromatin

Images & Validation

Key Properties

CAS Number2147701-33-3
MW505.05
Purity99.69% (May vary between batches)
FormulaC27H37ClN2O5
SMILESO(C[C@@H]1CN(C)CCC1)C2=C3C(=CC(=C2)C4=CC(OC)=C(OC)C=C4)CN(C(CC)=O)CCO3.Cl
TargetEpigenetic Reader Domain
SolubilityDMSO:60 mg/mL (118.8 mM)

Bioactivity

In Vivo
I-CBP112 markedly and dose-dependently reduces the leukemia-initiating potential of mLL-AF9+ AmL cells 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 possibilities for combinatorial treatment of leukemia and potentially other cancers.
In Vitro
I-CBP112 markedly increases acetylation by p300 at the histone H3K18 and H3K23 sites. I-CBP112 stimulated H3K18ac by ~3-fold, and induced enhances acetylation of these same sites by CBP as well as at H4K5. The EC50s of activation of I-CBP112 on CBP- and p300-mediated H3K18 acetylation are ~2 μM. In mouse and human leukemia cell lines, I-CBP112 causes substantially impaired colony formation and induces cellular differentiation without significant cytotoxicity. In BioMAP primary cell panel, I-CBP112 results in a unique response on cytokine and marker protein expression.

Storage & Handling

StoragePure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

CBP/p300, Leukemia cell, CBP/p300, Prostate cancer cell, Inhibitor, I-CBP 112 Hydrochloride, I-CBP112, ICBP112 hydrochloride, I-CBP112 Hydrochloride, I-CBP-112 hydrochloride, I-CBP-112 Hydrochloride, I CBP112 hydrochloride, Epigenetic Reader Domain, EpigeneticReaderDomain, inhibit
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Quality Guarantee

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Key Properties

No computed properties available.

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I-CBP112 hydrochloride (orb1303026)

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% DMSO +
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% Tween 80 +
%

Available Sizes

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1 mg
$ 130.00
2 mg
$ 190.00
5 mg
$ 290.00
1 ml x 10 mM (in DMSO)
$ 520.00
10 mg
$ 520.00
25 mg
$ 820.00
50 mg
$ 1,120.00
100 mg
$ 1,500.00
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