Home Angiogenesis PROTAC chemical - Bcr-Abl chemical - E3 Ligase chemical GMB-475 For research use only.

GMB-475

GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.

GMB-475 Chemical Structure

GMB-475 Chemical Structure

CAS: 2490599-18-1

Purity & Quality Control

Batch: Purity: 99.58%
99.58

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Biological Activity

Description GMB-475 is a proteolysis-targeting chimera (PROTAC) that allosterically targets BCR-ABL1 protein and recruit the E3 ligase Von Hippel-Lindau (VHL), resulting in ubiquitination and subsequent degradation of the oncogenic fusion protein.
Targets
BCR-ABL1 [1] E3 ligase [1]
In vitro
In vitro

GMB-475 induces rapid proteasomal degradation and inhibition of downstream biomarkers, such as STAT5 in both human CML K562 cells and murine Ba/F3 cells expressing BCR-ABL1. GMB-475 inhibits the proliferation of certain clinically relevant BCR-ABL1 kinase domain point mutants and further sensitizes Ba/F3 BCR-ABL1 cells to inhibition by imatinib, while demonstrating no toxicity toward Ba/F3 parental cells.[1]
Cell Research Cell lines K562 cell line, Ba/F3 murine cell lines (Ba/F3 BCR-ABL1 cells, Ba/F3 parental cells)
Concentrations 0.001-0.300 μM, 5 μM
Incubation Time 3 days, 8 h
Method

Cell viability assay: Cell lines and patient samples are exposed to dose ranges of GMB-475 (0.001-0.300 μM) and incubated for 3 days at 37°C, 5% CO2 and subjected to a CellTiter 96 AQueous One solution cell proliferation assay. Reverse phase protein arrays (RPPA): K562 cells are treated with DMSO, GMB-475 (5 μM) for 8 h in duplicate, washed twice with PBS and lysed in RPPA lysis buffer.

Chemical Information & Solubility

Molecular Weight 861.93 Formula

C43H46F3N7O7S
CAS No. 2490599-18-1 SDF --
Smiles CC1=C(SC=N1)C2=CC=C(CNC(=O)C3CC(O)CN3C(=O)C(NC(=O)COCCOC4=CC=C(C=C4)C5=CC(=NC=N5)NC6=CC=C(OC(F)(F)F)C=C6)C(C)(C)C)C=C2
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (116.01 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 50 mg/mL

Water : Insoluble


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In vivo
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