PROTAC BRD4 Degrader-32
PROTAC BRD4 Degrader-32 is a CRBN-recruiting PROTAC degrader targeting BRD4 (DC50=0.2 nM in HEK293 cells). PROTAC BRD4 Degrader-32 exhibits an IC50 of 0.05 μM against human CRBN and an IC50 of 22 nM against human BRD4. PROTAC BRD4 Degrader-32 induces reduced degradation of CK1α and WIZ, causes low-level degradation of IKZF1, and does not regulate GSPT1. PROTAC BRD4 Degrader-32 holds promise for research on BRD4-related cancers (such as hematological malignancies).
(Pink: BRD4 ligand (HY-13960); Blue: Cereblon ligand (HY-W072954); Black: linker (HY-176450)).
For research use only. We do not sell to patients.
- Formula: C42H42ClN5O5
- Molecular Weight:732.27
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Storage:
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
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
BRD4 0.2 nM (DC50) |
Cereblon 0.05 nM (IC50) |
BRD4 22 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | DC50 |
0.20 nM
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BRD4 degradation in CRISPR-engineered HEK293 HiBit-BRD4 cells assessed after 24-hour incubation at 37 °C with 5% CO2 by HiBiT degradation assay.
BRD4 degradation in CRISPR-engineered HEK293 HiBit-BRD4 cells assessed after 24-hour incubation at 37 °C with 5% CO2 by HiBiT degradation assay.
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acs.jmedchem.4c03157 |
| OCI-Ly3 | DC50 |
2.0 nM
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BRD4 degradation in OCI-Ly3 cells assessed after 8-hour incubation by data-independent acquisition (DIA) proteomics assay.
BRD4 degradation in OCI-Ly3 cells assessed after 8-hour incubation by data-independent acquisition (DIA) proteomics assay.
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acs.jmedchem.4c03157 |
In Vitro
PROTAC BRD4 Degrader-32 (compound 22) achieves a maximum degradation rate of 98% within 24 h in HEK293 HiBit-BRD4 cells[1].
PROTAC BRD4 Degrader-32 exhibits an IC50 of 37 nM for CRBN binding in live cells and an IC50 of 56 nM in lysed cells[1].
PROTAC BRD4 Degrader-32 (0.65 nM-10 μM; 2 h, 4 h, 8 h, 24 h) potently degrades BRD4 in OCI-Ly3 cells, with a DC50 of 2.0 nM, a maximum degradation rate of 76% at 8 h, and an early degradation effect observable as early as 4 h[1].
PROTAC BRD4 Degrader-32 (0.65 nM-10 μM; 24 h) exhibits superior neo-substrate selectivity in OCI-Ly3 cells, with no significant CK1α degradation, reduced WIZ degradation activity, low IKZF1 degradation level, and no regulatory effect on GSPT1 after 24 hours[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:OCI-Ly3
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Concentration:0.65 nM-10 μM
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Incubation Time:24 h
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Result:Improved neosubstrate selectivity in OCI-Ly3 cells, with no meaningful CK1α degradation, reduced WIZ degradation potency, low IKZF1 degradation, and no GSPT1 modulation.
Chemical Information
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Molecular Weight 732.27
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Formula C42H42ClN5O5
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SMILES
ClC1=CC=C(N[C@@H]2C[C@H](C)N(C(C)=O)C3=C2C=C(C4=CC=C(C(NCCCCC5=CC=C6C(CN(C(CCC(N7)=O)C7=O)C6=O)=C5)=O)C=C4)C=C3)C=C1
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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)
PROTAC BRD4 Degrader-32 Related Classifications
HY-176449 Related Classifications
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