TargetMol

I-CBP112 hydrochloride

Product Code:
 
TAR-T4247
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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CodeSizePrice
TAR-T4247-1mg1mg£137.00
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TAR-T4247-2mg2mg£189.00
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TAR-T4247-5mg5mg£270.00
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TAR-T4247-1mL1 mL * 10 mM (in DMSO)£449.00
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TAR-T4247-10mg10mg£449.00
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TAR-T4247-25mg25mg£691.00
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TAR-T4247-50mg50mg£938.00
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TAR-T4247-100mg100mg£1,243.00
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Further Information

Bioactivity:
I-CBP112 is a selective inhibitor of the bromodomain-containing transcription factors. I-CBP112 (1 mM) has little activity against other bromodomains. I-CBP112 targets the CBP/p300 bromodomains. I-CBP112 significantly reduced the leukemia-initiating potential of MLL-AF9(+) acute myeloid leukemia cells in a dose-dependent manner in vitro and in vivo. Interestingly, I-CBP112 increased the cytotoxic activity of BET bromodomain inhibitor JQ1 as well as doxorubicin.
CAS:
2147701-33-3
Formula:
C27H37ClN2O5
Molecular Weight:
505.05
Pathway:
Chromatin/Epigenetic
Purity:
0.9798
SMILES:
Cl.CCC(=O)N1CCOc2c(C1)cc(cc2OC[C@H]1CCCN(C)C1)-c1ccc(OC)c(OC)c1
Target:
Epigenetic Reader Domain

References

Zucconi BE, et al. Modulation of p300/CBP Acetylation of Nucleosomes by Bromodomain LigandI-CBP112. Biochemistry. 2016 Jul 12;55(27):3727-34. 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.