BRD4 Inhibitor-20

Name: BRD4 Inhibitor-20
Brand: MedChemExpress
SKU: HY-146208
Rating: 4.5 (1 reviews)

Cat. No.: HY-146208 Purity: 99.00%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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

CAS No. : 2490311-14-1

Size	Price	Stock	Quantity
5 mg	USD 190	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 310	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 620	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 990	In-stock	Estimated Time of Arrival: December 31
100 mg		Get quote
200 mg		Get quote

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Based on 1 publication(s) in Google Scholar

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Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target^[1]

BRD4 BD1

19 nM (IC₅₀)

BRD4 BD2

28 nM (IC₅₀)

BRD2 (BD1)

24 nM (IC₅₀)

BRD2 (BD2)

18 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HL-60	IC₅₀	1.35 μM Compound: 12j	Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay Antiproliferative activity against human HL60 cells incubated for 72 hrs by CCK8 assay	[PMID: 32883643]
HT-29	IC₅₀	4.75 μM Compound: 12j	Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human HT29 cells incubated for 72 hrs by MTT assay	[PMID: 32883643]
WI-38	IC₅₀	44.07 μM Compound: 12j	Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay Antiproliferative activity against human WI-38 cells incubated for 72 hrs by MTT assay	[PMID: 32883643]

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.

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)
C_max(μg/L)	-	2175
T_max(h)	-	1.00
t_1/2(h)	1.56	3.59
CL_z/F (L/h/kg)	0.68	1.03
AUC_0−t(μg/L*h)	7296	14384
AUC_0−∞(μg/L*h)	7340	14600
F (%)	-	66%

Molecular Weight

358.41

Formula

C₁₈H₁₈N₂O₄S

CAS No.

2490311-14-1

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
10 mM	0.2790 mL	1.3951 mL	2.7901 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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Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

μL

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.00%

Select Batch:

Data Sheet (280 KB) SDS (251 KB)

COA (252 KB) HNMR (270 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Yu Xu, et al. Design, synthesis and biological evaluation of indole-2-one derivatives as potent BRD4 inhibitors. Eur J Med Chem. 2020 Dec 15;208:112780. [Content Brief]

Complete Stock Solution Preparation Table

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