Powder: -20°C for 3 years | In solvent: -80°C for 1 year
GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 30.00 | |
2 mg | In stock | $ 38.00 | |
5 mg | In stock | $ 61.00 | |
10 mg | In stock | $ 101.00 | |
25 mg | In stock | $ 203.00 | |
50 mg | In stock | $ 369.00 | |
100 mg | In stock | $ 549.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 66.00 |
Description | GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl. |
Targets&IC50 | BCR-ABL (K562 cell lines):273 nM, BCR-ABL (SUP-B15 cell lines):268 nM |
In vivo | GNF-2, at a concentration of 1 μM, induces apoptosis in Ba/F3.p210 and Ba/F3.p210E255V cells and significantly reduces phosphorylated Stat5 levels in Ba/F3.p210 cells. It inhibits Bcr-abl tyrosine phosphorylation in a dose-dependent manner, with an IC50 value of 267 nM. Furthermore, 10 μM GNF-2 inhibits BCR-Abl-dependent cell proliferation, requiring the BCR and/or c-Abl SH3 and/or SH2 domains, and significantly suppresses CrkII tyrosine phosphorylation in a dose-dependent manner. GNF-2 demonstrates an inhibition effect on CrkII phosphorylation in cells expressing c-AblG2A, with an IC50 of 0.051 μM, and inhibits autophosphorylation and proliferation in cells expressing p210Bcr-Abl and its mutants, BafF3. When combined with GNF-5 (20 nM), GNF-2 (8 nM) shows a synergistic effect in inhibiting Abl64-515 kinase activity. It also exhibits dose-dependent inhibitory effects on the growth of Bcr-abl positive cells (IC50 values: 273 nM for K562 and 268 nM for SUP-B15) and Ba/F3.p210E255V and Ba/F3.p185Y253H cells, with IC50 values of 268 nM and 194 nM, respectively. |
Kinase Assay | Binding assay: Recombinant proteins (100 nM for each construct) or immunoprecipitated proteins are diluted in kinase buffer (20 mM HEPES (pH 7.4), 50 mM KCl, 0.1% CHAPS, 30 mM MgCl2, 2 mM MnCl2, 1 mM DTT, and 1% glycerol). Aliquots of the diluted proteins are preincubated with either DMSO or compounds for 30 min at room temperature and then added to K-LISA PTK EAY reaction plates. The kinase reaction is initiated by adding 0.1 mM ATP and is allowed to proceed for 30 min at room temperature. The phosphorylation of GST-Abltide is monitored by SDS-PAGE and phosphorimaging analysis or autoradiography. |
Cell Research | Cells (0.3-0.6 × 106 per mL) are plated in duplicate or triplicate in 96-well plates containing increasing GNF-2 concentrations (5 nM–10 μM). After incubation at 37 ℃ in 5% CO2 for 48 hours, the effect of GNF-2 on cell viability is determined by the MTT colorimetric dye reduction method. Inhibition of cell proliferation is calculated as a percentage of growth of DMSO-treated cells, and IC50 values are determined with Microsoft Excel XLfit3.(Only for Reference) |
Synonyms | GNF2 |
Molecular Weight | 374.32 |
Formula | C18H13F3N4O2 |
CAS No. | 778270-11-4 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 37.4 mg/mL (100 mM)
Ethanol: 18.7 mg/mL (50 mM)
You can also refer to dose conversion for different animals. More
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GNF-2 778270-11-4 Angiogenesis Cytoskeletal Signaling Microbiology/Virology Tyrosine Kinase/Adaptors Bcr-Abl SARS-CoV SARS coronavirus allosteric non-ATP competitive inhibitor Ba/F3.p185Y253H Ba/F3.p210E255V Ba/F3.p210 bone erosion Inhibitor GNF2 GNF 2 inhibit inhibitor