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PU141 

Cat. No. M28805
PU141  Structure
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Quality Control & Documentation
Biological Activity

PU141 is a selected pyridoisothiazolone HAT inhibitor. PU141 is selective toward CBP and p300. PU141 induces cellular histone hypoacetylation and inhibits growth of several neoplastic cell lines originating from different tissues. Anticancer activity.

Chemical Information
Molecular Weight 310.29
Formula C14H9F3N2OS
CAS Number 168334-34-7
Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Jaganathan Ramakrishnan, et al. J Biomol Struct Dyn. Investigation of intermolecular interactions and binding mechanism of PU139 and PU141 molecules with p300 HAT enzyme via molecular docking, molecular dynamics simulations and binding free energy analysis

[2] J M Gajer, et al. Oncogenesis. Histone acetyltransferase inhibitors block neuroblastoma cell growth in vivo

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  Catalog
Abmole Inhibitor Catalog




Keywords: PU141  supplier, Histone Acetyltransferase, inhibitors, activators


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