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PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC), a selective Mcl-1 inhibitor. By hijacking the CRBN ubiquitin ligase to form a ternary complex with the target protein, it induces Mcl-1 ubiquitination. It can be used for cancer research.

| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $79 | In Stock | |
| 5 mg | $189 | In Stock | |
| 10 mg | $318 | In Stock | |
| 25 mg | $673 | In Stock | |
| 50 mg | $1,080 | In Stock | |
| 100 mg | $1,730 | In Stock | |
| 200 mg | $2,330 | In Stock |
| Description | PROTAC Mcl1 degrader-1 is a Cereblon ligand-based targeted chimeric protein degrader (PROTAC), a selective Mcl-1 inhibitor. By hijacking the CRBN ubiquitin ligase to form a ternary complex with the target protein, it induces Mcl-1 ubiquitination. It can be used for cancer research. |
| Targets&IC50 | MCL1:0.78 μM, Bcl-2:0.54 μM |
| In vitro | PROTAC Mcl1 degrader-1 (Compound C3) induces ubiquitination of Mcl-1 and promotes its proteasomal degradation by binding the Mcl-1 inhibitor S1-6 (with μM range affinity) to the E3 ligase cereblon (CRBN) ligand, pomalidomide.PROTAC Mcl1 degrader-1 selectively targets Mcl-1, a member of the Bcl-2 family, with an IC50 of 078 μM. PROTAC Mcl1 degrader-1 selectively targets Mcl-1 (a member of the Bcl-2 family) with an IC50 of 0.78 μM, and also inhibits Bcl-2 with an IC50 of 0.54 μM. [1] PROTAC Mcl1 degrader-1 (0-10 μM; 0-24 hours) selectively reduces Mcl-1 and Bcl-2 protein levels in HeLa cells by a time- and concentration-dependent mechanism. [1] PROTAC Mcl1 degrader-1 (0-2 μM; 24 hours) exhibits cytotoxic effects on H23 cells. [1] |
| Molecular Weight | 909.84 |
| Formula | C45H45BrN6O8S |
| Cas No. | 2163793-38-0 |
| Smiles | O=C1NC(=O)C(N2C(=O)C=3C=CC=C(NCCCCCCNC(=O)CCCCC(=O)NCCN4C(=O)C5=CC=CC=6C(SC7=CC=C(Br)C=C7)=CC=C(C4=O)C56)C3C2=O)CC1 |
| Relative Density. | no data available |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||
| Solubility Information | DMSO: 40 mg/mL (43.96 mM), Sonication is recommended. | |||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (2.2 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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