2. Epigenetics
  3. Epigenetic Reader Domain
  4. I-BET282

I-BET282 

Cat. No.: HY-19760 Purity: 99.12%
COA Handling Instructions

I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 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.

I-BET282 Chemical Structure

I-BET282 Chemical Structure

CAS No. : 1422554-34-4

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 99 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 99 In-stock
Solid
5 mg USD 90 In-stock
10 mg USD 150 In-stock
50 mg USD 450 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of I-BET282:

I-BET282 Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

I-BET282 is a pan-inhibitor of all eight BET bromodomains, and selectivity over other representative bromodomain-containing proteins. I-BET282 shows pIC50s ranging 6.4-7.7 for BRD2 (BD1/BD2), BRD2 (BD1/BD), BRD3 (BD1/BD), and BRD4 (BD1/BD)[1].

In Vitro

I-BET282 has a weak inhibition of the hERG potassium ion channel (pIC50 4.4-5.1 in a variety of assay formats). I-BET282 shows a low potential to inhibit CYP proteins in vitro, with no evidence of time-dependent inhibition of 2D6 or 3A4[1].

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

I-BET282 Related Antibodies
In Vivo

I-BET282 (Male CD1 Mice; 3 mg/kg-p.o.; 1 mg/kg-i.v.) treatment shows the Clb, LBF, Vss, t1/2 (i.v.), and F values of 23 mL/min/kg, 19%, 1.9 L/kg, and 51%, respectively. I-BET282 (Male Wistar Han Rats; 1 mg/kg; p.o.) treatment shows the AUC0-t, Cmax and Tmax values of 467 ng h/mL, 125 ng/mL, and 1 hour, respectively[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

450.53

Appearance

Solid

Formula

C25H30N4O4
CAS No.
SMILES

COC1=C(C2=C(C)ON=C2C)C=C(N=CC3=C4N(C(C5CCOCC5)=N3)[C@@H](COC)C)C4=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (221.96 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2196 mL 11.0980 mL 22.1961 mL
5 mM 0.4439 mL 2.2196 mL 4.4392 mL
10 mM 0.2220 mL 1.1098 mL 2.2196 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (5.55 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation
References
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I-BET282 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

I-BET2821422554-34-4Epigenetic Reader Domainoncologyimmuno-inflammatoryareaspanInhibitorinhibitorinhibit

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