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IACS-9571

Cat. No. M28871
IACS-9571 Structure
Synonym:

ASIS-P040

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Quality Control & Documentation
Biological Activity

IACS-9571 is a potent and selective inhibitor of TRIM24 and BRPF1, with IC50 of 8 nM for TRIM24, and Kds of 31 nM and 14 nM for TRIM24 and BRPF1, respectively.

Chemical Information
Molecular Weight 642.76
Formula C32H42N4O8S
CAS Number 1800477-30-8
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] Riley M Horvath, et al. Sci Rep. Inhibition of the TRIM24 bromodomain reactivates latent HIV-1

[2] Mingzhi Han, et al. J Transl Med. Pharmacological targeting of Tripartite Motif Containing 24 for the treatment of glioblastoma

[3] Srikanth Appikonda, et al. J Biol Chem. Cross-talk between chromatin acetylation and SUMOylation of tripartite motif-containing protein 24 (TRIM24) impacts cell adhesion

[4] Yanai Zhan, et al. Epigenetics Chromatin. Development of novel cellular histone-binding and chromatin-displacement assays for bromodomain drug discovery

[5] Wylie S Palmer, et al. J Med Chem. Structure-Guided Design of IACS-9571, a Selective High-Affinity Dual TRIM24-BRPF1 Bromodomain Inhibitor

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Keywords: IACS-9571, ASIS-P040 supplier, Epigenetic Reader Domain, inhibitors, activators


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