PROTAC BRD2 BD1 Degrader-1
PROTAC BRD2 BD1 Degrader-1 is a potent and selective BRD2 BD1 PROTAC degrader, with a DC50 of 65 nM, an EC50 of 423 nM, and a Kd of 69 nM against BRD2 BD1. PROTAC BRD2 BD1 Degrader-1 induces the formation of a ternary complex between the BET bromodomain and the VHL E3 ubiquitin ligase complex, triggering VCB-dependent degradation of the target bromodomain. PROTAC BRD2 BD1 Degrader-1 can be used in cancer research.
(Pink: BRD2 BD1 ligand (HY-175679); Blue: VHL ligand (HY-125845); Black: linker).
For research use only. We do not sell to patients.
- Formula: C51H66N12O4S
- Molecular Weight:943.21
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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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Biological Activity
Description
IC50 & Target
[1]|
BRD2 BD1 65 nM (DC50) |
BRD4 BD1 224 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | EC50 |
81 nM
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Induction of ternary complex formation between SmBiT-tagged BRD2 BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
Induction of ternary complex formation between SmBiT-tagged BRD2 BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
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40792622 |
| HEK-293T | EC50 |
138 nM
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Induction of ternary complex formation between SmBiT-tagged BRD3 BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
Induction of ternary complex formation between SmBiT-tagged BRD3 BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
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40792622 |
| HEK-293T | EC50 |
190 nM
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Induction of ternary complex formation between SmBiT-tagged BRD4 BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
Induction of ternary complex formation between SmBiT-tagged BRD4 BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
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40792622 |
| HEK-293T | EC50 |
92 nM
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Induction of ternary complex formation between SmBiT-tagged BRDT BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
Induction of ternary complex formation between SmBiT-tagged BRDT BD1 and VHL-LgBiT fusion protein in HEK293T cells measured as normalized relative light units after 22 hour post-transfection incubation and 2 hour compound treatment by NanoBiT assay.
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40792622 |
| HEK-293T | DC50 |
65 nM
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Degradation of HiBiT-tagged BRD2 BD1 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
Degradation of HiBiT-tagged BRD2 BD1 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
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40792622 |
| HEK-293T | DC50 |
224 nM
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Degradation of HiBiT-tagged BRD4 BD1 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
Degradation of HiBiT-tagged BRD4 BD1 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
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40792622 |
| HEK-293T | DC50 |
312 nM
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Degradation of HiBiT-tagged BRDT BD1 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
Degradation of HiBiT-tagged BRDT BD1 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
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40792622 |
| HEK-293T | DC50 |
358 nM
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Degradation of HiBiT-tagged BRD2 BD2 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
Degradation of HiBiT-tagged BRD2 BD2 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
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40792622 |
| HEK-293T | DC50 |
363 nM
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Degradation of HiBiT-tagged BRD4 BD2 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
Degradation of HiBiT-tagged BRD4 BD2 in HEK293T cells expressing VHL measured as luminescence after 24 hour post-transfection incubation, 6 hour pre-incubation, and 17 hour compound treatment by HiBiT protein degradation assay.
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40792622 |
In Vitro
PROTAC BRD2 BD1 Degrader-1 (Compound 21-1) (up to 10 μM; 1 h) induces the formation of a ternary complex between BRD2 BD1 and VCB in a cell-free system, with an EC50 of 423 nM[1].
PROTAC BRD2 BD1 Degrader-1 (up to 20 μM) binds BRD2 BD1 with high affinity in the presence of VCB in a cell-free system, with a KD of 69 nM[1].
PROTAC BRD2 BD1 Degrader-1 (up to 30 μM; 2-17 h) induces the formation of a ternary complex between BRD2 BD1 and VHL (with an EC50 of 81 nM), selectively degrades BRD2 BD1 (with a DC50 of 65 nM), and causes no cytotoxicity in HEK293T cells[1].
PROTAC BRD2 BD1 Degrader-1 (0.01-10 μM; 20 h) selectively degrades endogenous BRD2 protein in HEK293T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HEK293T cells
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Concentration:0.01, 0.1, 1, 10 μM
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Incubation Time:20 h
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Result:Specifically degraded endogenous BRD2 protein at 100 nM, while degradation of BRD3 and BRD4 was only observed at concentrations >1 μM (indicating a >10-fold selectivity for BRD2).
Chemical Information
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Molecular Weight 943.21
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Formula C51H66N12O4S
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SMILES
CC1=CC=CC2=C1CCN(C2)C3=NC(N4CCC(CC4)CCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C=C6)C7=C(N=CS7)C)=O)O)=O)=O)=NC(N8CCC(C8)C9=NC=CN9C)=N3
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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 BRD2 BD1 Degrader-1 Related Classifications
HY-175678 Related Classifications
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