Bfl-1-IN-7
Bfl-1-IN-7 is an orally active and selective Bfl-1 inhibitor with an IC50 value of 0.015 μM. Bfl-1-IN-7 activates caspase 3/7, and when combined with the Mcl-1 inhibitor AZD5991 (HY-101533), it reduces the viability of lymphoma cells. Bfl-1-IN-7 can be used in lymphoma-related studies.
For research use only. We do not sell to patients.
- Formula: C24H26F3N3O3
- Molecular Weight:461.48
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All Caspase Isoforms
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Biological Activity
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Bfl-1 0.015 μM (IC50) |
Caspase-3 |
Caspase-7 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SU-DHL-1 | EC50 |
0.31 μM
|
Induction of caspase activation (a marker of apoptosis) in SU-DHL-1 lymphoma cells when combined with Mcl-1 inhibitor AZD5991, measured after 6-hour incubation.
Induction of caspase activation (a marker of apoptosis) in SU-DHL-1 lymphoma cells when combined with Mcl-1 inhibitor AZD5991, measured after 6-hour incubation.
|
41432228 |
| SU-DHL-1 | EC50 |
0.21 μM
|
Reduction of SU-DHL-1 lymphoma cell viability measured after 24-hour incubation.
Reduction of SU-DHL-1 lymphoma cell viability measured after 24-hour incubation.
|
41432228 |
| KARPAS-422 | EC50 |
>10 μM
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Lack of cell viability reduction in Bfl-1-null Karpas-422 cells, with no effect observed at concentrations up to 10 μM after 24-hour incubation.
Lack of cell viability reduction in Bfl-1-null Karpas-422 cells, with no effect observed at concentrations up to 10 μM after 24-hour incubation.
|
41432228 |
Bfl-1-IN-7 (compound 25) potently and selectively inhibits purified Bfl-1 protein with an IC50 of 0.015 μM. When combined with the Mcl-1 inhibitor AZD5991 (HY-101533), it induces caspase activation in SU-DHL-1 lymphoma cells with an EC50 of 0.31 μM[1].
Bfl-1-IN-7 (0.2-20 μM; 4 h) covalently labels the C55 residue of Bfl-1 in LY10 lymphoma cells in a dose-dependent and selective manner, with extremely low off-target activity against BTK C481[1].
Bfl-1-IN-7 potently inhibits Bfl-1 in biochemical FRET assays, with a mean pIC50 of 7.809; in combination with AZD5991, it induces caspase 3/7 activation in SU-DHL-1 cells, with a mean pEC50 of 6.503[1].
Bfl-1-IN-7 covalently binds to purified Bfl-1 in a concentration- and time-dependent manner, and its observed rate constant increases with the elevation of compound concentration[1].
Bfl-1-IN-7 reduces the viability of SU-DHL-1 lymphoma cells, with an EC50 of 0.21 μM at 24 h[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 461.48
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Formula C24H26F3N3O3
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SMILES
C=CC(N([C@@H](C)C1=CC=C(NC([C@@H]2CCC[C@H]2N)=O)C=C1)C3=CC=C(OC(F)(F)F)C=C3)=O
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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)