2. Epigenetics
  3. Epigenetic Reader Domain
  4. BRD4 Inhibitor-20

BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer.

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

BRD4 Inhibitor-20 Chemical Structure

BRD4 Inhibitor-20 Chemical Structure

CAS No. : 2490311-14-1

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10 mg USD 310 In-stock
25 mg USD 620 In-stock
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Based on 1 publication(s) in Google Scholar

BRD4 Inhibitor-20 Related Antibodies

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Description

BRD4 Inhibitor-20 is a potent orally active bromodomain protein 4 (BRD4) inhibitor. BRD4 Inhibitor-20 has inhibitory activity for BRD4 (BD1) and BRD4 (BD2) with IC50 values of 19 nM and 28 nM, respectively. BRD4 Inhibitor-20 also has anti-proliferation activities in cancer cell lines. BRD4 Inhibitor-20 can be used for the research of kinds of cancer, such as colon cancer[1].

IC50 & Target[1]

BRD4 BD1

19 nM (IC50)

BRD4 BD2

28 nM (IC50)

BRD2 (BD1)

24 nM (IC50)

BRD2 (BD2)

18 nM (IC50)

In Vitro

BRD4 Inhibitor-20 (compound 12j) exhibits excellent BRD4 inhibitory activities (BD1, IC50=19 nM; BD2, IC50=28 nM) and inhibitory activities against BRD2 (BD1, IC50=24 nM; BD2, IC50=18 nM)[1].
BRD4 Inhibitor-20 (0.5, 2.5, 5.0 μM; 24 h) reduces the expression of c-Myc[1].
BRD4 Inhibitor-20 (72 h) has anti-proliferation potency with IC50 values of 4.75 μM, 1.35 μM and 44.07 μM in HT-29, HL-60 and WI-38 cells, respectively[1].
BRD4 Inhibitor-20 (2.5, 5.0, 10.0 μM; 24 h) can arrest the cell-cycle progression of HT-29 cells into the G1 phase[1].

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

BRD4 Inhibitor-20 Related Antibodies

Western Blot Analysis[1]

Cell Line: HT-29 cells
Concentration: 0.5, 2.5, 5.0 μM
Incubation Time: 24 h
Result: Displayed profound inhibitory effects on c-Myc protein expression.

Cell Proliferation Assay[1]

Cell Line: HT-29, HL-60 and WI-38 cells
Concentration:
Incubation Time: 72 h
Result: Possessed strong anti-proliferative activity and weak toxicity.

Cell Cycle Analysis[1]

Cell Line: HT-29 cell lines
Concentration: 2.5, 5.0, 10.0 μM
Incubation Time: 24 h
Result: Arrested the cell-cycle progression of the cell line into the G1 phases and the percentage of cells in G1 phase after treatment under concentrations of 2.5, 5.0 and 10.0 μM were 85.98%, 86.49% and 86.05%, respectively.
In Vivo

BRD4 Inhibitor-20 (compound 12j) (i.v., 5 mg/kg; p.o, 15mg/kg) exhibits favorable oral pharmacokinetic propertie[1].

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

Animal Model: rats[1]
Dosage: 5 mg/kg, 15 mg/kg
Administration: intravenous dosing (iv) or oral dosing (po)
Result:
PK Parameters iv (5 mg/kg) po (15 mg/kg)
Cmax(μg/L) - 2175
Tmax(h) - 1.00
t1/2(h) 1.56 3.59
CLz/F (L/h/kg) 0.68 1.03
AUC0−t(μg/L*h) 7296 14384
AUC0−∞(μg/L*h) 7340 14600
F (%) - 66%
Molecular Weight

358.41

Formula

C18H18N2O4S
CAS No.
Appearance

Solid

Color

Brown to reddish brown

SMILES

O=C1NC2=CC=C(C=C2/C1=C(C)\C)NS(=O)(C3=C(C=CC=C3)OC)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (348.76 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7901 mL 13.9505 mL 27.9010 mL
5 mM 0.5580 mL 2.7901 mL 5.5802 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7901 mL 13.9505 mL 27.9010 mL 69.7525 mL
5 mM 0.5580 mL 2.7901 mL 5.5802 mL 13.9505 mL
10 mM 0.2790 mL 1.3951 mL 2.7901 mL 6.9753 mL
15 mM 0.1860 mL 0.9300 mL 1.8601 mL 4.6502 mL
20 mM 0.1395 mL 0.6975 mL 1.3951 mL 3.4876 mL
25 mM 0.1116 mL 0.5580 mL 1.1160 mL 2.7901 mL
30 mM 0.0930 mL 0.4650 mL 0.9300 mL 2.3251 mL
40 mM 0.0698 mL 0.3488 mL 0.6975 mL 1.7438 mL
50 mM 0.0558 mL 0.2790 mL 0.5580 mL 1.3951 mL
60 mM 0.0465 mL 0.2325 mL 0.4650 mL 1.1625 mL
80 mM 0.0349 mL 0.1744 mL 0.3488 mL 0.8719 mL
100 mM 0.0279 mL 0.1395 mL 0.2790 mL 0.6975 mL
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BRD4 Inhibitor-20 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.

Keywords:

BRD4 Inhibitor-202490311-14-1Epigenetic Reader Domainbromodomain protein 4 (BRD4)BD1BD2cancer cell linescancercolon cancerInhibitorinhibitorinhibit

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