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UMB-32 

Cat. No. M28737
UMB-32  Structure
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Quality Control & Documentation
Biological Activity

UMB-32, a potent, selective BRD4 inhibitor, binds BRD4 with the Kd of 550 nM, and IC50 of 637 nM. UMB-32 also shows potency against TAF1, a bromodomain-containing transcription factor.

Chemical Information
Molecular Weight 361.44
Formula C21H23N5O
CAS Number 1635437-39-6
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] Huachao Huang, et al. Front Microbiol. A Novel Bromodomain Inhibitor Reverses HIV-1 Latency through Specific Binding with BRD4 to Promote Tat and P-TEFb Association

[2] Michael R McKeown, et al. J Med Chem. Biased multicomponent reactions to develop novel bromodomain inhibitors

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  Catalog
Abmole Inhibitor Catalog




Keywords: UMB-32  supplier, Epigenetic Reader Domain, inhibitors, activators


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