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
- Protocols
- 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 |
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| 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. Further protocols information, click here.
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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.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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