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

BRD4/CK2-IN-1 

Cat. No.: HY-145260
Handling Instructions

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)

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

BRD4/CK2-IN-1 Chemical Structure

BRD4/CK2-IN-1 Chemical Structure

CAS No. : 2756851-99-5

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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)

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].

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

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

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.
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Storage

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

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