JY-21
JY-21 is a BRD4 PROTAC degrader active against both long and short BRD4 isoforms. JY-21 binds to TRIM28, RACK1, LMO7 and FUS to induce proteasomal degradation of BRD4 isoforms (DC50: 5.944 μM for long BRD4 isoform; 3.797 μM for short BRD4 isoform). JY-21 is applicable to research related to triple-negative breast cancer.
(Pink: BRD4 ligand (HY-78695); Blue: Ligands for E3 Ligase ligand (HY-174994); Black: linker (HY-151862)).
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- 화학식: C42H50ClN11O4SSi
- 분자량:868.52
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
All PROTACs Isoforms
More
Biological Activity
제품 설명
IC50 & Target
[1]|
BRD4 3.797 μM (DC50) |
BRD4 5.944 μM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MDA-MB-231 | DC50 |
5.944 μM
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Degradation of BRD4 long isoform in human MDA-MB-231 triple-negative breast cancer cells after 24 h incubation measured by Western blot degradation assay.
Degradation of BRD4 long isoform in human MDA-MB-231 triple-negative breast cancer cells after 24 h incubation measured by Western blot degradation assay.
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40566838 |
| MDA-MB-231 | DC50 |
3.797 μM
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Degradation of BRD4 short isoform in human MDA-MB-231 triple-negative breast cancer cells after 24 h incubation measured by Western blot degradation assay.
Degradation of BRD4 short isoform in human MDA-MB-231 triple-negative breast cancer cells after 24 h incubation measured by Western blot degradation assay.
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40566838 |
In Vitro
JY-21 (0.1-20 μM; 24 h) potently degrades the long isoform of BRD4 (DC50 = 5.944 μM) and the short isoform of BRD4 (DC50 = 3.797 μM) in MDA-MB-231 cells[1].
JY-21 (5 μM; 24 h) induces BRD4 degradation in MDA-MB-231 cells via a proteasome-dependent pathway[1].
JY-21 (10 μM; 2 h) binds to the E3 ubiquitin ligases TRIM28, RACK1, LMO7 and FUS, thereby mediating BRD4 degradation in MDA-MB-231 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells
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Concentration:0.1, 1, 5, 10, 20 μM
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Incubation Time:24 h
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Result:Significantly degraded BRD4 protein at 5 μM.
Reduced levels of the long isoform of BRD4 with a DC50 of 5.944 μM and a Dmax of 70.64% at 20 μM.
Reduced levels of the short isoform of BRD4 with a DC50 of 3.797 μM and a Dmax of 76.40% at 20 μM.
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Cell Line:MDA-MB-231 human triple-negative breast cancer cells
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Concentration:5 μM
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Incubation Time:24 h
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Result:Induced BRD4 degradation when used alone.
Had the BRD4-degrading effect completely blocked by pretreatment with MG132, restoring BRD4 protein levels to those of DMSO-treated controls.
Chemical Information
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분자량 868.52
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화학식 C42H50ClN11O4SSi
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SMILES
CC1=C(C(C(C2=CC=C(C=C2)Cl)=N[C@H]3CC(NCCCN4C=C(N=N4)COC5=CC=C(C([N+]([O-])=O)=C5)/N=N/C#C[Si](C(C)C)(C(C)C)C(C)C)=O)=C(N6C3=NN=C6C)S1)C
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
JY-21 Related Classifications
HY-174975 Related Classifications
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