328968-36-1 Usage
Uses
Used in Oncology:
C646 is used as an inhibitor for histone acetyltransferase p300 and may be a potential candidate for treating AML1-ETO (AE) positive acute myeloid leukemia (AML). It has been shown to inhibit cellular proliferation, reduce colony formation, evoke partial cell cycle arrest in the G1 phase, and induce apoptosis in AE-positive AML cell lines and primary blasts isolated from leukemic mice and AML patients.
Used in Neuroscience:
C646 has been utilized in studying the role of p300 in chronic neuropathic pain in rats with chronic constriction injury. Its effects on enhancing fear extinction memory and synaptic plasticity in mice also indicate its potential application in the field of neuroscience for understanding and treating various neurological disorders.
Used in Drug Development:
As a potent and selective inhibitor of p300/CBP histone acetyltransferases, C646 serves as a valuable tool in drug development for targeting specific molecular pathways involved in cancer and other diseases. Its cell permeable property allows for easier study and potential therapeutic application in various research and clinical settings.
Biochem/physiol Actions
C646 is a potent, cell permeable and selective inhibitor of p300 and CBP (p300/CBP) histone acetyltransferases. Inhibition of p300/CBP by C646 affects the activity of a variety of transcriptional factors such as NF-κB, p53 and MyoD that are associated with physiology, disease processes, hippocampal synaptic plasticity, spatial memory and contextual fear.
References
1) Bowers et al. (2010), Virtual ligand screening of the p300/CBP histone acetyltransferase: identification of a selective small molecule inhibitor; Chem. Biol., 17 471
2) Santer et al. (2011), Inhibition of the acetyltransferases p300 and CBP reveals a targetable function for p300 in the survival and invasion pathways of prostate cancer cell lines; Mol. Cancer Ther., 10 1644
3) Marek et al. (2011), Paradoxical enhancement of fear extinction memory and synaptic plasticity by inhibition of the histone acetyltransferase p300; J. Neurosci.., 31 7486
4) Min et al. (2010), Acetylation of tau inhibits its degradation and contributes to tauopathy; Neuron, 67 953
Check Digit Verification of cas no
The CAS Registry Mumber 328968-36-1 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 3,2,8,9,6 and 8 respectively; the second part has 2 digits, 3 and 6 respectively.
Calculate Digit Verification of CAS Registry Number 328968-36:
(8*3)+(7*2)+(6*8)+(5*9)+(4*6)+(3*8)+(2*3)+(1*6)=191
191 % 10 = 1
So 328968-36-1 is a valid CAS Registry Number.
328968-36-1Relevant academic research and scientific papers
Methods and Compositions for Modulating P300/CBP Activity
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Page/Page column 20-21, (2010/09/05)
The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.
