1. PROTAC Stem Cell/Wnt Cell Cycle/DNA Damage
  2. Molecular Glues Casein Kinase
  3. 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.

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IBA-11

IBA-11 Chemical Structure

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Description

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[1].

IC50 & Target[1]

CK1α

 

Cereblon

 

In Vitro

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.

Western Blot Analysis[1]

Cell Line: MV-4-11, Mino
Concentration: 0.1, 0.5, 2.5 nM
Incubation Time: 8 h
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.

Western Blot Analysis[1]

Cell Line: Mino
Concentration: 500 nM
Incubation Time: 2, 4, 8, 16 h
Result: Induced near-complete depletion of CK1α within 2 h of treatment.
Induced time-dependent degradation.
Molecular Weight

437.40

Formula

C22H17F2N5O3

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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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
IBA-11
Cat. No.:
HY-182800
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