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Chemical Structure| 1300031-49-5 Chemical Structure| 1300031-49-5

Structure of I-BET151
CAS No.: 1300031-49-5

Chemical Structure| 1300031-49-5

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I-BET-151 is a selective BET inhibitor for BRD2, BRD3 and BRD4 with IC50 of 0.5 μM, 0.25 μM, and 0.79 μM in cell-free assays, respectively.

Synonyms: GSK1210151A

4.5 *For Research Use Only !

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Product Details of I-BET151

CAS No. :1300031-49-5
Formula : C23H21N5O3
M.W : 415.44
SMILES Code : O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3
Synonyms :
GSK1210151A
MDL No. :MFCD22124472
InChI Key :VUVUVNZRUGEAHB-CYBMUJFWSA-N
Pubchem ID :52912189

Safety of I-BET151

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P264-P270-P301+P310-P321-P330-P405-P501
Class:6.1
UN#:2811
Packing Group:

Related Pathways of I-BET151

epigenetics

Isoform Comparison

Biological Activity

Target
  • BET

    BRD4, IC50:0.5 μM

    BRD3, IC50:0.25 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
293TRex cells 5 μM 48 hours To examine the effect of I-BET151 on telomerase activity, results showed no significant effect on telomerase activity PMC5737673
BECs 50 μM from A0h to R24h or from R0h to R48h I-BET151 significantly affected liver size, as assessed by fabp10a: DsRed expression PMC4718879
A2058 cells 1 μM 72 hours To test the inhibitory effect of I-BET151 on A2058 cell proliferation, results showed that ascorbate pretreatment enhanced the activity of I-BET151. PMC5771981
1205Lu cells 1 μM 72 hours To test the inhibitory effect of I-BET151 on 1205Lu cell proliferation, results showed that ascorbate pretreatment enhanced the activity of I-BET151. PMC5771981
C8161 cells 1 μM 72 hours To test the inhibitory effect of I-BET151 on C8161 cell proliferation, results showed that ascorbate pretreatment enhanced the activity of I-BET151. PMC5771981
SK-MEL-28 cells 1 μM 72 hours To test the inhibitory effect of I-BET151 on SK-MEL-28 cell proliferation, results showed that ascorbate pretreatment enhanced the activity of I-BET151. PMC5771981
SK-MEL-2 cells 1 μM 72 hours To test the inhibitory effect of I-BET151 on SK-MEL-2 cell proliferation, results showed that ascorbate pretreatment enhanced the activity of I-BET151. PMC5771981
human pancreatic progenitors 1 μM 7 days promote the expansion of PDX1 and NKX6.1 double-positive pancreatic progenitors PMC8865776

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Humanized mice HIV-1 YU2 infection model Injection 10 mg/kg Every other day, throughout the experimental period To evaluate whether I-BET151 combined with antibodies can reduce viral rebound. Results showed that I-BET151 alone did not significantly reduce viral rebound. PMC4163911
mice CDE diet model injection 50 mg/kg Daily for 8 weeks JQ1 greatly reduced oval cell number and proliferation in mice fed a CDE diet PMC4718879
Mice Xenotransplant model of disseminated human MLL-AF4 leukemia Intraperitoneal injection 30 mg/kg Daily for 14 days I-BET151 demonstrated significant therapeutic efficacy in two distinct mouse models of MLL leukemia, providing survival benefits. PMC3679520
mice TNF-induced inflammatory osteolysis model intraperitoneal injection 30 mg/kg Daily, continuous treatment I-BET151 significantly inhibited in vivo osteoclastogenesis and associated bone erosion, reducing serum TRAP levels and osteoclast numbers. PMC4249944

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.41mL

0.48mL

0.24mL

12.04mL

2.41mL

1.20mL

24.07mL

4.81mL

2.41mL

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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