MC-25B
MC-25B is a DCAF16-recruiting FKBP12 PROTAC degrader with a DC50 of 0.35 μM. MC-25B promotes the formation of a ternary complex with DCAF16 and nuclear-localized FKBP12_NLS, thereby mediating DCAF16-dependent degradation of FKBP12_NLS via the proteasome and Cullin-RING ligase pathway.
(Pink: FKBP12 ligand (HY-170988); Blue: DCAF16 ligand (HY-170986); Black: linker (HY-128844)).
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- Fòrmula: C72H98ClN7O14
- Peso molecular:1321.04
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Almacenamiento:
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
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
FKBP12 0.35 μM (DC50) |
In Vitro
MC-25B (1 μM; 24 h) induces selective, DCAF16-dependent degradation of FKBP12 in HEK293T cells expressing FLAG-FKBP12_NLS, with only one identified DCAF16-independent off-target effect[1].
MC-25B (1-2 μM; 8 h) induces the degradation of FLAG-FKBP12_NLS in HEK293T cells expressing the DCAF16_3Cys mutant (retaining only C177−179), confirming that this cysteine cluster plays a critical role in MC-25B-mediated degradation[1].
MC-25B (incubated for 72 h) inhibits the viability of HEK293T cells, with an IC50 value of 2.2 μM[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 overexpressing HA-DCAF16 and FLAG-FKBP12_NLS
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Concentration:0.1 μM, 0.2 μM, 0.5 μM, 1 μM, 2 μM, 5 μM
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Incubation Time:8 h
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Result:Induced dose-dependent degradation of FLAG-FKBP12_NLS, with a maximum degradation (Dmax) of 89% and a half-maximal degradation concentration (DC50) of 0.35 μM.
Chemical Information
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Peso molecular 1321.04
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Fòrmula C72H98ClN7O14
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SMILES
O=C(CN1CCN(C2=CC=CC(C(N3CC(CC4=CC=CC=C4)C(N(C5CC5)C(CCl)=O)CC3)=O)=C2)CC1)NCCCOCCOCCOCCCNC(COC6=CC=CC([C@H](OC([C@@H]7CCCCN7C(C(C(C)(C)CC)=O)=O)=O)CCC8=CC(OC)=C(OC)C=C8)=C6)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MC-25B Related Classifications
HY-170983 Related Classifications
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