1. Epigenetics
  2. Epigenetic Reader Domain

BI-7273 

Cat. No.: HY-100351 Purity: 99.65%
Handling Instructions

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

For research use only. We do not sell to patients.
BI-7273 Chemical Structure

BI-7273 Chemical Structure

CAS No. : 1883429-21-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 145 In-stock
5 mg USD 132 In-stock
10 mg USD 228 In-stock
25 mg USD 456 In-stock
50 mg USD 720 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM.

IC50 & Target

IC50: 19 nM (BRD9), 117 nM (BRD7)[1]
Kd: 0.75 nM (BRD9), 0.3 nM (BRD7)[1]

In Vitro

BI-7273 is a selective, and cell-permeable BRD9 inhibitor, with an IC50 and a Kd of 19 and 0.75 nM; also shows high effect on BRD7, with an IC50 and a Kd of 117 nM and 0.3 nM. BI-7273 also has slight activity against a panel of kinases such as CECR2, BRPF1, BRD1, CREBBP, EP300, FALZ, TAF1(2) and TAF1L(2), with Kds of 8.8 nM, 210 nM, 2600 nM, 8600 nM, 10000 nM, 850 nM, 1000 nM, and 1200 nM, respectively. BI-7273 (1 μM) is active in U2OS cell lines. BI-7273 blocks EOL-1 cell proliferation with EC50 of 1400 nM[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.8296 mL 14.1479 mL 28.2957 mL
5 mM 0.5659 mL 2.8296 mL 5.6591 mL
10 mM 0.2830 mL 1.4148 mL 2.8296 mL
Please refer to the solubility information to select the appropriate solvent.
Kinase Assay
[1]

His-tagged BRD9 is immobilized to a density of 2000-4000 RUs on flow cells 3 and 4 of a Biacore NTA-chip. Carbonic anhydrase II is immobilized at a similar density on flow cell 2 and a blank reference surface is generated on flow cell 1. The buffer is then switched to assay buffer (HBS-P+ = 10 mM HEPES, pH 7.4, 150 mM NaCl, 0.05 % P20 + 5 % DMSO) and the chip equilibrated for several hours before use for Kd determinations. To be able to correct for differences in bulk solvent refractive index caused by small variations in the DMSO concentration solvent correction samples are included at the beginning and end of the run. Compounds (BI-7273, etc.) are injected in concentration series (1:1 dilutions, 7 different concentrations), starting with a maximum concentration that is approximately 10-20-fold higher than the expected Kd. The concentration series are prepared in 96-well plates. In the case that the dilution window chosen for a particular compound does not appropriately bracket the Kd of the compound the measurement is repeated with an optimized starting concentration. Positive and negative control samples are included at regular intervals to be able to monitor the performance of the assay. CBS is used as a positive control for carbonic anhydrase II to check for integrity of the reference protein at regular intervals. To correct for the excluded volume effect a DMSO calibration series is prepared and the calibration samples are measured at the beginning and end of each run. Kd values are determined and averaged[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[1]

Cells are grown in 50 µL medium for 7 days starting with 500 and with 1000 cells per well of a 384 well plate in the presence of varying concentrations of compound (BI-7273, etc.) before measuring viability via cellular ATP levels using the cell titer glow assay[1].
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

353.41

Formula

C₂₀H₂₃N₃O₃

CAS No.

1883429-21-7

SMILES

CN(C)CC1=C(OC)C=C(C(C2=C3C=NC=C2)=CN(C)C3=O)C=C1OC

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 10 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
BI-7273
Cat. No.:
HY-100351
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