1. Protein Tyrosine Kinase/RTK
  2. Bcr-Abl
  3. PROTAC BCR-ABL1 ligand 1

PROTAC BCR-ABL1 ligand 1 

Cat. No.: HY-130297
Handling Instructions

PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1.

For research use only. We do not sell to patients.

PROTAC  BCR-ABL1 ligand 1 Chemical Structure

PROTAC BCR-ABL1 ligand 1 Chemical Structure

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Description

PROTAC BCR-ABL1 ligand 1, compound GMB-475, is the ligand of PROTAC that allosterically targets BCR-ABL1 protein and recruits the E3 ligase Von Hippel-Lindau, resulting in ubiquitination and subsequent degradation of BCR-ABL1[1].

In Vitro

GMB-475 (0-10 μM) exhibits cell proferation with IC50 values of 1.11,1.98,0.37 μM for BCR-ABL1 WT, T315I, G250E cells, respectively[1].
GMB-475 (0-30 μM) induces the degradation of BCR-ABL1 and c-ABL1 with concomitant inhibition of downstream signaling via the STAT5 pathway, in a dose- and time-dependent fashion in the context of both K562 and Ba/F3 cells[1].

Western Blot Analysis[1]

Cell Line: K562 and Ba/F3 cells
Concentration: 0-30 μM
Incubation Time:
Result: Decreased p-STAT5 expression.
Molecular Weight

347.29

Formula

C₁₇H₁₂F₃N₃O₂

SMILES

OC1=CC=C(C2=NC=NC(NC3=CC=C(OC(F)(F)F)C=C3)=C2)C=C1

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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.

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Keywords:

PROTAC BCR-ABL1 ligand 1Bcr-AblInhibitorinhibitorinhibit

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PROTAC BCR-ABL1 ligand 1
Cat. No.:
HY-130297
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