2. Epigenetics Stem Cell/Wnt Cell Cycle/DNA Damage Apoptosis Autophagy
  3. Epigenetic Reader Domain Casein Kinase Apoptosis Autophagy
  4. BRD4/CK2-IN-1

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)

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BRD4/CK2-IN-1 Chemical Structure

BRD4/CK2-IN-1 Chemical Structure

CAS No. : 2756851-99-5

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Based on 1 publication(s) in Google Scholar

BRD4/CK2-IN-1 Related Antibodies

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Description

BRD4/CK2-IN-1 is the first highly effective and oral active dual-target inhibitor of BRD4/CK2 (bromodomain-containing protein 4/casein kinase 2), with IC50s of 180 nM and 230 nM for BRD4 and CK2, respectively. BRD4/CK2-IN-1 has strong anticancer activity without obvious toxicities. BRD4/CK2-IN-1 induces apoptosis and autophagy-associated cell death in triple-negative breast cancer (TNBC)[1]

IC50 & Target[1]

BRD4

180 nM (IC50)

CK2

230 nM (IC50)

Cellular Effect
Cell Line Type Value Description References
MDA-MB-231 IC50
2.66 μM
Compound: 44e
Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-231 cells incubated for 24 hrs by MTT assay
[PMID: 34908415]
MDA-MB-468 IC50
3.52 μM
Compound: 44e
Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay
Antiproliferative activity against human MDA-MB-468 cells incubated for 24 hrs by MTT assay
[PMID: 34908415]
In Vitro

BRD4/CK2-IN-1 (compound 44e) (0-25 μM; 24 hours) has anti-proliferation effect with IC50s of 2.66 and 3.52 μM in MDA-MB-231 and MDA-MB-468 cells, respectively[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently induces apoptosis of MDA-MB-231 and MDA-MB-468 cells[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) dose-dependently downregulates Bcl-2 but upregulates Bax and cleaved caspase-3[1].
BRD4/CK2-IN-1 (0-10 μM; 24 hours) significantly downregulates the autophagy substrate p62 and up-regulated beclin-1 and LC3II in MDA-MB-231 and MDA-MB[1].

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

BRD4/CK2-IN-1 Related Antibodies

Cell Viability Assay[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 0, 0.19, 0.39, 0.78, 1.56, 3.13, 6.25, 12.5, 25 μM
Incubation Time: 24 hours
Result: Showed anti-proliferative rates in MDA-MB-231 and MDA-MB-468 cells (IC50 = 2.66 and 3.52 μM, respectively).

Apoptosis Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Dose-dependently induced apoptosis of MDA-MB-231 and MDA-MB-468 cells.

Western Blot Analysis[1]

Cell Line: MDA-MB-231, MDA-MB-468 cells
Concentration: 0, 2.5, 5, 10 μM
Incubation Time: 24 hours
Result: Dose-dependently downregulated Bcl-2 but upregulated Bax and cleaved caspase-3.

Cell Line:
Concentration:
Incubation Time:
Result:
In Vivo

BRD4/CK2-IN-1 (25 and 50 mg/kg; intragastric administration; daily for 19 days) inhibits tumor growth in TNBC xenograft models[1].
BRD4/CK2-IN-1 (25 and 50mg/kg; intragastric administration; daily for 19 days) shows weak toxicity measured by body weight loss in the MDA-MB-231 and MDA-MB-468 xenograft models[1].
Preliminary Assessment of Pharmacokinetics (PK) profile of BRD4/CK2-IN-1[1].

Parameter iv (1 mg/kg) po (10 mg/kg)
T1/2 (h) 4.21±0.57 5.14±0.71
Cmax (ng/mL) 237±11 206±6
AUC0-t (ng·h/mL) 579±49 2079±130
AUC0-∞ (ng·h/mL) 588±36 2090±146
VZ (L/kg) 21.1±2.6
CL ((mL/min)/kg) 57.4±1.3
F (%) 32.5

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

Animal Model: Female nude mice (BALB/c, 6-8 weeks, 20-22 g) bearing MDA-MB-231 cells[1]
Dosage: 25 and 50 mg/kg
Administration: Intragastric administration; daily for 19 days
Result: Had the most pronounced tumor growth inhibition (TGI) (63.8%) in the MDA-MB-231 xenograft tumor model at 50 mg/kg.
Molecular Weight

564.03

Formula

C29H30ClN5O5
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C1C2=C(OC)C=C(OC)C=C2N=C(C3=CC=C(OCC(NC4=CC(Cl)=C(N5CCN(C)CC5)C=C4)=O)C=C3)N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 20 mg/mL (35.46 mM; ultrasonic and warming and adjust pH to 3 with HCl 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 1.7730 mL 8.8648 mL 17.7296 mL
5 mM 0.3546 mL 1.7730 mL 3.5459 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. 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)

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

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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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
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. 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 1.7730 mL 8.8648 mL 17.7296 mL 44.3239 mL
5 mM 0.3546 mL 1.7730 mL 3.5459 mL 8.8648 mL
10 mM 0.1773 mL 0.8865 mL 1.7730 mL 4.4324 mL
15 mM 0.1182 mL 0.5910 mL 1.1820 mL 2.9549 mL
20 mM 0.0886 mL 0.4432 mL 0.8865 mL 2.2162 mL
25 mM 0.0709 mL 0.3546 mL 0.7092 mL 1.7730 mL
30 mM 0.0591 mL 0.2955 mL 0.5910 mL 1.4775 mL
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BRD4/CK2-IN-1 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/CK2-IN-12756851-99-5Epigenetic Reader DomainCasein KinaseApoptosisAutophagyBRD4CK2anticanceranti-proliferationtumor growthtoxicityTNBCbreastMDA-MB-231MDA-MB-468Inhibitorinhibitorinhibit

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