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Chemical Structure| 1714146-59-4 Chemical Structure| 1714146-59-4

Structure of I-BRD9
CAS No.: 1714146-59-4

Chemical Structure| 1714146-59-4

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I-BRD9 is a BRD9 bromodomain inhibitor with pIC50 value of 7.3 and pKd of 8.7. BRD9 fuctions as part of the SWI/SNF complex in chromatin remolding .

Synonyms: GSK602

4.5 *For Research Use Only !

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Product Details of I-BRD9

CAS No. :1714146-59-4
Formula : C22H22F3N3O3S2
M.W : 497.55
SMILES Code : N=C(C(S1)=CC2=C1C(C3=CC=CC(C(F)(F)F)=C3)=CN(CC)C2=O)NC(CC4)CCS4(=O)=O
Synonyms :
GSK602
MDL No. :MFCD28952791
InChI Key :WRUWGLUCNBMGPS-UHFFFAOYSA-N
Pubchem ID :91668541

Safety of I-BRD9

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P301+P310
Class:6.1
UN#:2811
Packing Group:

Related Pathways of I-BRD9

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD9, pIC50:7.3

    BRD4, pIC50:5.3

In Vitro:

Cell Line
Concentration Treated Time Description References
KD 8.1 µM, 7.1 µM 72h and 144h Evaluate the effect of I-BRD9 on KD cell proliferation, IC50 values decreased over time Int J Mol Sci. 2017 Jul 16;18(7):1537.
G401 13.4 µM, 6.1 µM 72h and 144h Evaluate the effect of I-BRD9 on G401 cell proliferation, IC50 values decreased over time Int J Mol Sci. 2017 Jul 16;18(7):1537.
Chla266 13.3 µM, 24.7 µM 72h and 144h Evaluate the effect of I-BRD9 on Chla266 cell proliferation, IC50 values varied over time Int J Mol Sci. 2017 Jul 16;18(7):1537.
BT16 11.2 µM 72h Evaluate the effect of I-BRD9 on BT16 cell proliferation, IC50 value was 11.2 µM Int J Mol Sci. 2017 Jul 16;18(7):1537.
BT12 21.2 µM, 8.2 µM 72h and 144h Evaluate the effect of I-BRD9 on BT12 cell proliferation, showing decreased IC50 over time Int J Mol Sci. 2017 Jul 16;18(7):1537.
U2OS 10 or 20 µM 36 h To evaluate the effect of I-BRD9 on HR activity. Results showed that I-BRD9 significantly inhibited HR activity. Nat Commun. 2020 May 26;11(1):2639.
OVCAR8 10 or 20 µM 36 h To evaluate the effect of I-BRD9 on HR and NHEJ activity. Results showed that I-BRD9 significantly inhibited HR activity but had no significant effect on NHEJ activity. Nat Commun. 2020 May 26;11(1):2639.
Kasumi-1 cells 10 μM 6 h Identify genes selectively regulated by BRD9 bromodomain inhibition, involved in oncology and immune response pathways J Med Chem. 2016 Feb 25;59(4):1425-39.
UTSM cells 5-25 µM 48 h Evaluate the effect of I-BRD9 on UTSM cell proliferation, showing dose-dependent inhibition of cell proliferation Int J Mol Sci. 2024 Jan 11;25(2):905.
HuLM cells 1-25 µM 48 h Evaluate the effect of I-BRD9 on HuLM cell proliferation, showing dose-dependent inhibition of cell proliferation Int J Mol Sci. 2024 Jan 11;25(2):905.
Leishmania donovani promastigotes 0-30 μM 5 days To evaluate the effect of I-BRD9 on the cell viability of Leishmania donovani promastigotes. Results showed that I-BRD9 had minimal inhibitory activity on promastigote growth at concentrations up to 30 μM. ACS Infect Dis. 2023 Nov 10;9(11):2340-2357.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
NOD-SCID mice Ovarian cancer xenograft model Intraperitoneal injection 40 mg/kg 3 times per week for 8 times To evaluate the effect of I-BRD9 on tumor growth. Results showed that the combination of I-BRD9 and olaparib significantly delayed tumor growth. Nat Commun. 2020 May 26;11(1):2639.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.01mL

0.40mL

0.20mL

10.05mL

2.01mL

1.00mL

20.10mL

4.02mL

2.01mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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