PROTAC BRD4 Degrader-23
PROTAC BRD4 Degrader-23 is a visible light-regulated BRD4 PROTAC degrader, with DC50 values of 6871 nM and < 30 nM in the dark and under light exposure, respectively; its IC50 values are 1172 nM and 140 nM under the corresponding conditions. PROTAC BRD4 Degrader-23 shows inhibited activity in dark environments, and recovers BRD4 degradation ability upon irradiation with 405 nm visible light. PROTAC BRD4 Degrader-23 inhibits tumor cell proliferation in a visible light-dependent manner. PROTAC BRD4 Degrader-23 can be used in studies of BRD4-dependent B-cell lymphoma.
(Pink: BRD4 ligand (HY-78695); Blue: VHL ligand (HY-175797); Black: linker (HY-141209)).
For research use only. We do not sell to patients.
- Formula: C62H69ClN10O10S2
- Molecular Weight:1213.86
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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
Description
IC50 & Target
[1]|
BRD4 < 30 nM (DC50) |
VHL |
In Vitro
PROTAC BRD4 Degrader-23 (Compound 17) undergoes efficient photolysis upon exposure to 405 nm visible light in a cell-free system, producing MZ1 (HY-107425)[1].
PROTAC BRD4 Degrader-23 exhibits an anti-proliferative IC50 of 1172 nM against Namalwa cells under dark conditions; after irradiation with 405 nm visible light (3 min), this activity is significantly enhanced, with the IC50 decreasing to 140 nM, which is comparable to the activity of MZ1[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 1213.86
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Formula C62H69ClN10O10S2
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SMILES
O=C(NCCOCCOCCOCC(N[C@@H](C(C)(C)C)CN1[C@H](C(N(CC2=CC=C(C3=C(C)N=CS3)C=C2)CC4=CC(C(C=CC=C5)=C5O6)=C6C=C4[N+]([O-])=O)=O)C[C@@H](O)C1)=O)C[C@@H]7N=C(C8=CC=C(Cl)C=C8)C(C(C)=C(C)S9)=C9N%10C7=NN=C%10C
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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)