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Cat. No.: HY-19760B

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I-BET282E

I-BET282E is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282E shows pIC₅₀s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD).

For research use only. We do not sell to patients.

CAS No.: 2885162-99-0
Formula: C₂₆H₃₄N₄O₇S
Molecular Weight:546.64

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (271 KB)

I-BET282E Chemical Structure

CAS No.: 2885162-99-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

All Epigenetic Reader Domain Isoforms :

In Vitro

I-BET282E has a weak inhibition of the hERG potassium ion channel (pIC₅₀ 4.4-5.1 in a variety of assay formats). I-BET282E shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

I-BET282E (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Cl_b, LBF, Vss, t_1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively^[1].
I-BET282E (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC_0-t, C_max and T_max values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS No. 2885162-99-0
Molecular Weight 546.64
Formula C₂₆H₃₄N₄O₇S
SMILES

CS(=O)(O)=O.COC1=C(C=C(C2=C1)N=CC3=C2N([C@H](C)COC)C(C4CCOCC4)=N3)C5=C(ON=C5C)C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Jones KL, et al. Discovery of a Novel Bromodomain and Extra Terminal Domain (BET) Protein Inhibitor, I-BET282E, Suitable for Clinical Progression. J Med Chem. 2021;64(16):12200-12227. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Keywords

100 mg

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