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GNF-2

Catalog No. T1817 CAS 778270-11-4

Synonyms: GNF2

GNF-2 is a highly selective non-ATP competitive inhibitor of Bcr-Abl.

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GNF-2, CAS 778270-11-4

Pack Size	Availability	Price/USD
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

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Purity: 99.08%

Purity: 98%

Biological Description

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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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 37.4 mg/mL (100 mM)

Ethanol: 18.7 mg/mL (50 mM)

References and Literature

1. Adrián FJ, et al. Nat Chem Biol, 2006, 2(2), 95-102 2. Choi Y, et al. J Biol Chem, 2009, 284(42), 292005-292014. 3. Zhang J, et al. Nature, 2010, 463(7280), 501-506. 4. Fabbro D, et al. Biochim Biophys Acta, 2010, 1804(3), 454-462.

Related compound libraries

This product is contained In the following compound libraries：

Highly Selective Inhibitor Library Inhibitor Library Tyrosine Kinase Inhibitor Library Kinase Inhibitor Library Anti-Cancer Compound Library Cytoskeletal Signaling Pathway Compound Library Anti-Cancer Metabolism Compound Library Fluorochemical Library Apoptosis Compound Library Bioactive Compounds Library Max

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

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

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