JQ1-JX5
JQ1-JX5 is a DCAF16-based BRD4 PROTAC degrader. JQ1-JX5 covalently modifies Cys58 of DCAF16, promotes ternary complex formation with BRD4, enables BRD4 ubiquitination and proteasomal degradation. JQ1-JX5 induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM. JQ1-JX5 can be used for the research of cancer, such as acute myeloid leukemia.
(Pink: BRD4 ligand (HY-78695); Blue: DCAF16 ligand (HY-W005799); Black: linker).
For research use only. We do not sell to patients.
- Formula: C29H24ClN7O2S2
- Molecular Weight:602.13
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All PROTACs Isoforms
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Biological Activity
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BRD4 |
DCAF16 |
JQ1-JX5 (1.0 μM; 3-36 h) induces time-dependent degradation of BRD4 long and short isoforms in AGS cells with DC50 of 43.97 and 16.77 nM, and ~90% loss of both isoforms achieved by 24 hours[1].
JQ1-JX5 (0.01-5 μM; 12 h) induces degradation of BRD4 long and short isoforms in AGS, MDA-MB-453, AsPC1, MV-4-11, MDA-MB-231, and HEK293T cells[1].
JQ1-JX5 inhibits AGS cells proliferation with an IC50 of 0.4993 μM[1].
JQ1-JX5 mediates the degradation of BRD4 by covalent recruitment of DCAF16[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:AGS cancer cells
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Concentration:1.0 μM
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Incubation Time:3, 6, 9, 12, 24, 36 h
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Result:Induced time-dependent degradation of BRD4, with detectable reduction in both long and short isoforms within 3 h.
Caused ~90% loss of both BRD4 isoforms after 24 h of treatment.
Led to near-complete depletion of both BRD4 isoforms after 36 h.
Chemical Information
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Molecular Weight 602.13
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Formula C29H24ClN7O2S2
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SMILES
CC1=NN=C2[C@@H](N=C(C3=C(N21)SC(C)=C3C)C4=CC=C(C=C4)Cl)CC(NCCOC5=CC=C6N=C(SC6=C5)C#N)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)