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Chemical Structure| 1936422-33-1 Chemical Structure| 1936422-33-1

Structure of GNE-781
CAS No.: 1936422-33-1

Chemical Structure| 1936422-33-1

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GNE-781 is an effective, orally active, and selective CBP inhibitor, with an IC50 of 0.94 nM in TR-FRET assays. GNE-781 also inhibits BRET and BRD4 (1) with IC50 values of 6.2 nM and 5100 nM, respectively.

Synonyms: GNE-781

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Product Details of GNE-781

CAS No. :1936422-33-1
Formula : C27H33F2N7O2
M.W : 525.59
SMILES Code : CN1N=CC(C2=C(C(F)F)C=C3N(CCCC3=C2)C4=NN(C5CCOCC5)C6=C4CN(CC6)C(NC)=O)=C1
Synonyms :
GNE-781
MDL No. :MFCD31693834

Safety of GNE-781

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319
Precautionary Statements:P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Related Pathways of GNE-781

epigenetics

Isoform Comparison

Biological Activity

Target
  • p300/CBP

    CBP, IC50:0.94 nM

  • BET

    BRD4(1), IC50:5100 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
JJN3 cells 40 nM 72 h POM + G781 significantly reduced MYC and IRF4 protein levels PMC10772542
KMS11 cells 40 nM 72 h POM + G781 significantly reduced MYC and IRF4 protein levels PMC10772542
human myeloma cell lines (HMCL) 40 nM 24 h G781 downregulated IRF4 and MYC more consistently and to similar degrees PMC10772542
MCF10A-EGR2-Luc cells 100 nM 1 h To study the effect of GNE-781 on EGF-induced EGR2 transcription. Results showed that GNE-781 enhanced EGR2 reporter activity. PMC8682737
MCF10A-DUSP1-Luc cells 100 nM 1 h To study the effect of GNE-781 on EGF-induced DUSP1 transcription. Results showed that GNE-781 dampened the early induction phase of DUSP1. PMC8682737

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Vk*MYC mouse model Oral 3.75 mg/kg and 15 mg/kg Twice daily for 2 weeks High-dose G781 (15 mpk) was more effective than low-dose G781 in reducing M-spikes, but showed dose toxicity PMC10772542

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.90mL

0.38mL

0.19mL

9.51mL

1.90mL

0.95mL

19.03mL

3.81mL

1.90mL

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
 

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