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GNF-2

SKU: orb1307386

Description

GNF-2 is a potent, selective inhibitor that targets Bcr-Abl through a unique allosteric, non-ATP-competitive mechanism. It is a valuable chemical probe for studying kinase signaling in chronic myeloid leukemia (CML) research, demonstrating activity in both cellular and animal models of the disease.

Research Area

Cardiovascular Research, Infectious Disease & Virology, Signal Transduction

Images & Validation

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GNF-2

Key Properties

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CAS Number778270-11-4
MW374.32
Purity98.00%
FormulaC18H13F3N4O2
SMILESNC(=O)c1cccc(c1)-c1cc(Nc2ccc(OC(F)(F)F)cc2)ncn1
TargetSARS-CoV,Bcr-Abl
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.34 mM);Ethanol:18.7 mg/mL (49.96 mM);DMSO:37.4 mg/mL (99.91 mM)

Bioactivity

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Target IC50
BCR-ABL (K562 cells):273 nM|BCR-ABL (SUP-B15 cells):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.
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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)
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Storage & Handling

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StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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Inhibitor, GNF 2, GNF2, GNF-2, inhibit, non-ATP competitive inhibitor, allosteric, BcrAbl, Bcr-Abl, Bcr-Abl (K562 cell line), Bcr-Abl (SUP-B15 cell line), bone erosion, Ba/F3.p185Y253H, Ba/F3.p210, Ba/F3.p210E255V, SARS coronavirus, SARS-CoV, SARSCoV

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Quality Guarantee

Quality Guarantee

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Compound Identifiers

PubChem CID
5311510 ↗

Key Properties

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No computed properties available.

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GNF-2 (orb1307386)

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% DMSO +
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% Tween 80 +
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1 ml x 10 mM (in DMSO)
$ 70.00
10 mg
$ 90.00
25 mg
$ 130.00
50 mg
$ 200.00
100 mg
$ 270.00
200 mg
$ 380.00
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