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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.

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

CAS No.: 2059110-46-0
Formula: C₂₆H₃₀N₁₀O₃
Molecular Weight:530.58

Storage:

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

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
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Biological Activity

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)

All Epigenetic Reader Domain Isoforms :

In Vitro

BiBET (72 h) kills BRD4-dependent MV4.11 and MM.1S cells with pIC₅₀ = 9.5^[1].
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
Molecular Weight 530.58
Formula C₂₆H₃₀N₁₀O₃
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (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)
Handling Instructions (2659 KB)

References

[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.

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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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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
Chemical Information
Purity & Documentation
References

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BiBET

All Epigenetic Reader Domain Isoforms

Biological Activity

Description

IC50 & Target

In Vitro

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

BiBET Related Classifications

HY-123626 Related Classifications

Bioz

Keywords

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