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Chemical Structure| 1374601-40-7 Chemical Structure| 1374601-40-7

Structure of BRD4770
CAS No.: 1374601-40-7

Chemical Structure| 1374601-40-7

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BRD4770 is an inhibitor of histone methyltransferase G9a with IC50 of 6.3 μM and it can induce cell senescence.

Synonyms: HMTase Inhibitor VI

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Product Details of BRD4770

CAS No. :1374601-40-7
Formula : C25H23N3O3
M.W : 413.47
SMILES Code : O=C(C1=CC=C2N(CCCC3=CC=CC=C3)C(NC(C4=CC=CC=C4)=O)=NC2=C1)OC
Synonyms :
HMTase Inhibitor VI
MDL No. :MFCD23143627
InChI Key :UCGWYCMPZXDHNR-UHFFFAOYSA-N
Pubchem ID :72193870

Safety of BRD4770

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of BRD4770

epigenetics

Isoform Comparison

Biological Activity

Target
  • Histone Methyltransferase

In Vitro:

Cell Line
Concentration Treated Time Description References
PANC-1 cells 2.5 μM 3 days induces senescence and cell death, dependent on p53 status Cell Death Dis. 2013 Jun 27;4(6):e690.
mouse embryo fibroblasts (MEFs) 20 μM 48 h BRD4770 augmented Keap1 and NF-κB p50 binding and inhibited H3K9me2 deposition at virus induced genes in MEFs with intact Keap1. Immunology. 2022 Sep;167(1):105-121
LIPC cells 1.25 and 2.5μM To evaluate the effect of BRD4770 in combination with prexasertib on LIPC cell growth, showing synergistic reduction in cell viability. Mol Cancer Res. 2020 Mar;18(3):448-462
Mia-Paca2 cells 0.62–2.5μM 72 h To evaluate the effect of BRD4770 alone on Mia-Paca2 cell growth, showing partial inhibition of cell growth within 72 h. Mol Cancer Res. 2020 Mar;18(3):448-462
L3.6 cells 0.62–2.5μM 72 h To evaluate the effect of BRD4770 alone on L3.6 cell growth, showing partial inhibition of cell growth within 72 h. Mol Cancer Res. 2020 Mar;18(3):448-462
BxPC3 cells 0.62–2.5μM 72 h To evaluate the effect of BRD4770 alone on BxPC3 cell growth, showing partial inhibition of cell growth within 72 h. Mol Cancer Res. 2020 Mar;18(3):448-462
Diaporthe longicolla 100 nM 21 days To evaluate the effect of BRD4770 on the metabolic profiling of Diaporthe longicolla, results showed increased inhibition zone against S. aureus and MRSA, and enhanced antioxidant activity in the crude extract from cultures treated with 100 nM BRD4770. Front Microbiol. 2021 Sep 17;12:725463
PANC-1 cells 5 μM 24 h BRD4770 reduced di- and trimethylation levels of H3K9 and increased monomethylation level without inducing apoptosis ACS Chem Biol. 2012 Jul 20;7(7):1152-7
Primary human aortic vascular smooth muscle cells (p-HAVSMCs) 5 μM 48 h To evaluate the effect of BRD4770 on p-HAVSMCs proliferation, results showed that BRD4770 inhibited cell proliferation by blocking G2/M phase. Hum Cell. 2023 Sep;36(5):1672-1688
Rabbit aortic vascular smooth muscle cells (RAVSMCs) 5 μM 48 h To evaluate the effect of BRD4770 on RAVSMCs proliferation, results showed that BRD4770 inhibited cell proliferation by blocking G2/M phase. Hum Cell. 2023 Sep;36(5):1672-1688

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 mice Carotid artery wire injury model Intraperitoneal injection 1 mg/kg Once daily for 28 days To evaluate the effect of BRD4770 on vascular intimal hyperplasia, results showed that BRD4770 significantly alleviated restenosis of injured carotid arteries. Hum Cell. 2023 Sep;36(5):1672-1688
NU/J mice Subcutaneous and orthotopic xenograft models Subcutaneous injection 10mg/kg 3 times per week for 14 days To evaluate the effect of BRD4770 alone or in combination with prexasertib on subcutaneous and orthotopic xenograft models, showing significant reduction in tumor growth with combination therapy. Mol Cancer Res. 2020 Mar;18(3):448-462

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.42mL

0.48mL

0.24mL

12.09mL

2.42mL

1.21mL

24.19mL

4.84mL

2.42mL

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