IBA-11
IBA-11 is a selective CRBN-dependented CK1α molecular glue degrader. IBA-11 binds to the canonical tri-tryptophan pocket of CRBN, forming a ternary complex with CK1α to mediate its degradation. IBA-11 induces CRBN-dependent ubiquitin-proteasome system-mediated degradation of CK1α. IBA-11 exhibits cytotoxicity against cancer cells. IBA-11 demonstrates in vitro metabolic stability in rat liver microsomes and minimal hERG inhibition. IBA-11 can be used for the research of cancer, such as acute myeloid leukemia.
For research use only. We do not sell to patients.
- Formula: C22H17F2N5O3
- Molecular Weight:437.40
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
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CK1α |
Cereblon |
IBA-11 binds to CRBN with an IC50 of 2285 nM in a cell-free TR-FRET assay[1].
IBA-11 potently inhibits the viability of MV-4-11 cells with an IC50 of 82.11 nM, and shows minimal activity in MM.1S and Mino cells[1].
IBA-11 (0.1-2.5 nM; 8 h) induces dose-dependent degradation of CK1α, but not IKZF1/2/3 or GSPT1, in MV-4-11 and Mino cells[1].
IBA-11 (500 nM; 2-16 h) induces rapid, near-complete degradation of CK1α in Mino cells within 2 h[1].
IBA-11 (500 nM; 3 h) induced CK1α degradation in Mino cells is dependent on the CRBN-mediated ubiquitin-proteasome system, as confirmed by rescue with MLN4924 (HY-70062), PS341 (HY-10227), and MG132 (HY-13259) [1].
IBA-11 (0.2-2 μM) induced CK1α degradation is strictly CRBN-dependent, as degradation is abolished in CRBN-knockout HEK293T cells[1].
IBA-11 has favorable in vitro metabolic stability in rat liver microsomes and a low risk of cardiac toxicity, as indicated by minimal hERG inhibition (IC50 >40 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MV-4-11, Mino
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Concentration:0.1, 0.5, 2.5 nM
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Incubation Time:8 h
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Result:Induced dose-dependent degradation of CK1α in both MV-4-11 and Mino cells.
Left IKZF1/2/3 and GSPT1 largely unaffected across all tested concentrations.
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Cell Line:Mino
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Concentration:500 nM
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Incubation Time:2, 4, 8, 16 h
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Result:Induced near-complete depletion of CK1α within 2 h of treatment.
Induced time-dependent degradation.
Chemical Information
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Molecular Weight 437.40
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Formula C22H17F2N5O3
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SMILES
O=C1CCC(N2NC(C=C(C3=CN(C)C(C4=CC(F)=CC(F)=C4)=N3)C=C5)=C5C2=O)C(N1)=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)