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dBET1 is a hybrid molecule that combines (+)-JQ1 and thalidomide. It induces cereblon-dependent BET protein degradation in vitro (EC50: 430 nM) and induces apoptosis.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $48 | In Stock | |
5 mg | $106 | In Stock | |
10 mg | $173 | In Stock | |
25 mg | $297 | In Stock | |
50 mg | $475 | In Stock | |
100 mg | $723 | In Stock | |
500 mg | $1,490 | In Stock | |
1 mL x 10 mM (in DMSO) | $172 | In Stock |
Description | dBET1 is a hybrid molecule that combines (+)-JQ1 and thalidomide. It induces cereblon-dependent BET protein degradation in vitro (EC50: 430 nM) and induces apoptosis. |
Targets&IC50 | BET:430 nM (EC50) |
In vitro | dBET1 induced a potent and superior inhibitory effect on MV4;11 cell proliferation at 24 hours (measured by ATP content, IC50 = 0.14 μM, compared to IC50 = 1.1 μM with JQ1) consistent with the reported, pronounced inhibitory effect of RNA silencing of BRD4 in this and other models of MLL-rearranged leukemia. |
Molecular Weight | 785.27 |
Formula | C38H37ClN8O7S |
Cas No. | 1799711-21-9 |
Smiles | CC=1C2=C(N3C([C@H](CC(NCCCCNC(COC4=C5C(C(=O)N(C5=O)C6C(=O)NC(=O)CC6)=CC=C4)=O)=O)N=C2C7=CC=C(Cl)C=C7)=NN=C3C)SC1C |
Relative Density. | 1.55 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO: 50 mg/mL H2O: Insoluble Ethanol: 5 mg/mL |
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