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BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties.

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|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
| Description | BRD4 degrader-6 is a dimeric BDR4PROTAC class degrader with a DC50 of less than 0.1 μM. It effectively induces the ubiquitination and degradation of BDR4, exhibiting anticancer properties. |
| Targets&IC50 | BRD4:<0.1 μM(DC50) |
| In vitro | BRD4 degrader-6 (example 1) is effective in degrading BRD4 in BRD4 HiBiT cells, with a DC₅₀ of less than 0.11 μM, following a pretreatment of 1.5 nM for 2 hours and an additional treatment for 24 hours. The compound relies on the reversibility of its bonds to dissociate into monomers both in vitro and in vivo, allowing cellular entry, subsequent reformation into dimers within the cells, and subsequent binding to the target protein, which leads to ubiquitin-proteasome degradation of the target protein. |
| Molecular Weight | 1152.67 |
| Formula | C61H71BClN9O7S2 |
| Cas No. | 3055207-38-7 |
| Smiles | C(CNC(C[C@H]1C=2N(C3=C(C(=N1)C4=CC=C(Cl)C=C4)C(C)=C(C)S3)C(C)=NN2)=O)[C@]56[C@](C[C@@]7(C(C)(C)[C@]5(C7)[H])[H])(OB(O6)C8=C(CCC(N[C@H](C(=O)N9[C@H](C(NCC%10=CC=C(C=C%10)C%11=C(C)N=CS%11)=O)C[C@@H](O)C9)C(C)(C)C)=O)C=CC=C8)[H] |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. |
Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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