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I-BRD9

Cat. No. M8567
I-BRD9 Structure
Size Price Availability Quantity
10mg USD 145  USD145 In stock
50mg USD 550  USD550 In stock
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Biological Activity

I-BRD9 is a selective cellular chemical probe for bromodomain-containing protein 9 (BRD9), thought to be a member of the chromatin remodelling SWI/SNF BAF complex, which plays a fundamental role in gene expression regulation. I-BRD9 has a pIC50 value of 7.3 with greater than 700-fold selectivity over the BET family and 200-fold over the highly homologous bromodomain-containing protein 7 (BRD7) and greater than 70-fold selectivity against a panel of 34 bromodomains. For full characterization details, please visit the I-BRD9 probe summary on the Structural Genomics Consortium (SGC) website.

To learn about other SGC chemical probes for epigenetic targets, visit sigma.com/sgc

Chemical Information
Molecular Weight 497.55
Formula C22H22F3N3O3S2
CAS Number 1714146-59-4
Form Solid
Solubility (25°C) DMSO: 20 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
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] Lixin Zhou, et al. Targeting BRD9 by I-BRD9 efficiently inhibits growth of acute myeloid leukemia cells

[2] Qin Zhou, et al. The bromodomain containing protein BRD-9 orchestrates RAD51-RAD54 complex formation and regulates homologous recombination-mediated repair

[3] Jing Su, et al. Insight into selective mechanism of class of I-BRD9 inhibitors toward BRD9 based on molecular dynamics simulations

[4] Katja F Krmer, et al. BRD9 Inhibition, Alone or in Combination with Cytostatic Compounds as a Therapeutic Approach in Rhabdoid Tumors

[5] Natalie H Theodoulou, et al. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition

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Keywords: I-BRD9 supplier, Epigenetic Reader Domain, inhibitors, activators


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