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Cat. No.: HY-123626

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BiBET

BiBET is a selective BRD4 inhibitor with a pK_d of 11 for BRD4 (1,2). BiBET downregulates c-Myc. BiBET can be used in cancer research.

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CAS No.: 2059110-46-0
Formule: C₂₆H₃₀N₁₀O₃
Masse moléculaire:530.58

Stockage:

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

Data Sheet (279 KB)

BiBET Chemical Structure

CAS No.: 2059110-46-0

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Use of MCE Products

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
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Activité biologique

Description

BiBET is a selective BRD4 inhibitor with a pK_d of 11 for BRD4 (1,2). BiBET downregulates c-Myc. BiBET can be used in cancer research^[1]^[2]^[3].

IC₅₀ & Target

^[1]

BRD4(BD1BD2)

11 (pKd)

BRD4(1)

8.1 (pKd)

BRD4(2)

7.3 (pKd)

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In Vitro

Anti-cancerOthers

Anti-cancer

BiBET (72 h) kills BRD4-dependent MV4.11 and MM.1S cells with pIC₅₀ = 9.5^[1].

Others

BiBET (10 μM) engages BRD4(1,2) with pK_d = 11 in BROMOscan, compared with pK_d = 8.1 for BRD4(1) and pK_d = 7.3 for BRD4(2)^[1].
BiBET (1 mM) induces conformational compaction of BRD4(1,2), producing a faster-sedimenting species with s_20,w = 2.8 S at 1:1 and dimeric species at 2:1^[1].
BiBET (1 μM) is selective for BET BRDs and shows no detectable kinase activity at 1 μM, with the most potent off-target 5HT1B EC₅₀ = 0.93 μM^[1].
BiBET (50 nM) downregulates c-Myc in MM.1S cells with pEC₅₀ = 9.2 and maintains knockdown for 16 h after washout^[1].
BiBET (0.05 μM; 24 h) induces transcriptional changes in K-562, MM.1S, and MV-4-11 cells that are highly correlated with BET inhibition^[1].

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

Western Blot Analysis^[1]

Cell Line:

MM.1S
Concentration:

50 nM
Incubation Time:

2, 4, 16 h after compound washout
Result:

Downregulated c-Myc.

Chemical Information

CAS No. 2059110-46-0
Masse moléculaire 530.58
Formule C₂₆H₃₀N₁₀O₃
SMILES

CN(CCOC1=CC=C(C2CCN(C3=NN4C(C=C3)=NN=C4OC)CC2)C=C1)C5=NN6C(C=C5)=NN=C6OC
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage

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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Waring MJ, et al. Potent and selective bivalent inhibitors of BET bromodomains. Nature chemical biology. 2016 Dec;12(12):1097-1104. [Content Brief]

[2]. Guan X. Discovery of Fluorescence Polarization Probes and Inhibitors for Testis-Specific Bromodomain and Extra-Terminal (BRDT) Proteins[J]. 2020.

[3]. Watts E. Design and Synthesis of Dual KinaseBromodomain Inh ibitors Targeting ALK and BRD4[J]. 2019.

Calculators

Calculateur de molarité

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

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Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Pureté et documentation
Références

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BiBET

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Activité biologique

Description

IC50 & Target

In Vitro

Chemical Information

Pureté et documentation

Références

Calculators

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BiBET Related Classifications

HY-123626 Related Classifications

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