Cat. No.: HY-11007

GNF-2

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GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM .

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Pureté: 99.82%
CAS No.: 778270-11-4
Formule: C₁₈H₁₃F₃N₄O₂
Masse moléculaire:374.32

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

GNF-2 Chemical Structure

CAS No.: 778270-11-4

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (3)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC₅₀ of 138 nM ^[1].

IC₅₀ & Target^[1]

BCR-ABL1

Voir tous les produits spécifiques à Isoform Bcr-Abl :

Abl
Bcr-Abl

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	>10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing FIt3-ITD kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing FIt3-ITD kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	>10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-JAK1 kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-JAK1 kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	>10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing Tel-PDGFRbeta kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	>10 μM Compound: 2, GNF-2	Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing TPR-MET kinase assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against mouse BA/F3 Bcr-abl negative cells expressing TPR-MET kinase assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	138 nM Compound: 2, GNF-2	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	194 nM Compound: 2, GNF-2	Growth inhibition of mouse BA/F3 cells transfected with p210 Bcr-abl Y253H mutant Growth inhibition of mouse BA/F3 cells transfected with p210 Bcr-abl Y253H mutant	[PMID: 16415863]
BaF3	IC₅₀	2367 nM Compound: 2, GNF-2	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A334l mutant assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	IC₅₀	268 nM Compound: 2, GNF-2	Growth inhibition of mouse BA/F3 cells transfected with p210 Bcr-abl E255V mutant Growth inhibition of mouse BA/F3 cells transfected with p210 Bcr-abl E255V mutant	[PMID: 16415863]
BaF3	IC₅₀	3269 nM Compound: 2, GNF-2	Growth inhibition of mouse BA/F3 cells expressing Bcr-abl H396P mutant Growth inhibition of mouse BA/F3 cells expressing Bcr-abl H396P mutant	[PMID: 16415863]
BaF3	IC₅₀	752 nM Compound: 2, GNF-2	Growth inhibition of mouse BA/F3 cells expressing Bcr-abl M351T mutant Growth inhibition of mouse BA/F3 cells expressing Bcr-abl M351T mutant	[PMID: 16415863]
BaF3	IC₅₀	>10000 nM Compound: 2, GNF-2	Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay Antiproliferation activity against mouse BA/F3 cells expressing Bcr-abl A337N mutant assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
BaF3	EC₅₀	>10 μM Compound: 1	Cytotoxicity against mouse BA/F3 cells Cytotoxicity against mouse BA/F3 cells	[PMID: 20828158]
BaF3	EC₅₀	>10 μM Compound: 1	Inhibition of Bcr-Abl E505K mutant in mouse BA/F3 cells assessed as cell growth inhibition Inhibition of Bcr-Abl E505K mutant in mouse BA/F3 cells assessed as cell growth inhibition	[PMID: 20828158]
BaF3	EC₅₀	>10 μM Compound: 1	Inhibition of Bcr-Abl T315I mutant in mouse BA/F3 cells assessed as cell growth inhibition Inhibition of Bcr-Abl T315I mutant in mouse BA/F3 cells assessed as cell growth inhibition	[PMID: 20828158]
BaF3	EC₅₀	0.14 μM Compound: 1	Inhibition of Bcr-Abl in mouse BA/F3 cells Inhibition of Bcr-Abl in mouse BA/F3 cells	[PMID: 20828158]
BaF3	EC₅₀	0.6 μM Compound: 1	Inhibition of Bcr-Abl E225K mutant in mouse BA/F3 cells assessed as cell growth inhibition Inhibition of Bcr-Abl E225K mutant in mouse BA/F3 cells assessed as cell growth inhibition	[PMID: 20828158]
BaF3	GI₅₀	0.14 μM Compound: Fig 5b, Cpd 13	Antiproliferative activity against mouse BaF3 cells expressing Bcr-Abl assessed as cell growth inhibition Antiproliferative activity against mouse BaF3 cells expressing Bcr-Abl assessed as cell growth inhibition	[PMID: 35609336]
HL-60	IC₅₀	>10 μM Compound: 2, GNF-2	Antiproliferative activity against human HL60 Bcr-abl negative cells assessed as cell viability after 48 hrs by MTT assay Antiproliferative activity against human HL60 Bcr-abl negative cells assessed as cell viability after 48 hrs by MTT assay	[PMID: 16415863]
Jurkat	IC₅₀	>10 μM Compound: 2, GNF-2	Antiproliferative activity against human Jurkat Bcr-abl negative cells assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against human Jurkat Bcr-abl negative cells assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
K562	IC₅₀	0.273 μM Compound: 2, GNF-2	Antiproliferative activity against human K562 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against human K562 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]
SUP-B15	IC₅₀	0.268 μM Compound: 2, GNF-2	Antiproliferative activity against human SUP-B15 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay Antiproliferative activity against human SUP-B15 expressing Bcr-abl assessed as proliferation after 48 hrs by MTT assay	[PMID: 16415863]

In Vitro

GNF-2 selectively inhibits Bcr-abl-dependent cell proliferation. GNF-2 (0.005-10 μM; 48 hours) specifically inhibits the proliferation of the Bcr-abl-expressing cells with an IC₅₀ of 138 nM and not show any cytotoxic effects on the nontransformed cells at concentrations of up to 10 μM. GNF-2 (0.005-10 μM; 48 hours) causes a dose-dependent growth inhibition of the Bcr-abl-positive cell lines with IC₅₀ values of 273 nM (K562) and 268 nM (SUP-B15). GNF-2 (0.005-10 μM; 48 hours) inhibits E255V and Y253H mutant Bcr-abl cell growth (IC₅₀ values of 268 and 194 nM, respectively)^[1].
GNF-2 (1-10 μM; 48 hours) induces apoptosis of Bcr-abl-transformed cells^[1].
GNF-2 (0.1-10 μM; 90 minutes) inhibits the cellular tyrosine phosphorylation of Bcr-abl in a dose-dependent manner with an IC₅₀ of 267 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay^[1]

Cell Line:

Ba/F3.p210, Ba/F3.p210^E255V and Ba/F3.p185^Y253H cells
Concentration:

0.005, 0.01, 0.1, 1, 10 μM
Incubation Time:

48 hours
Result:

Inhibited Bcr-abl-transformed cells proliferation.

Apoptosis Analysis^[1]

Cell Line:

Ba/F3.p210 and Ba/F3.p210^E255V cells
Concentration:

1, 10 μM
Incubation Time:

48 hours
Result:

Increased number of Ba/F3.p210 cells undergoing apoptosis at 1 μM for 48 h.
Ba/F3.p210^E255V underwent apoptotic death after 48 h incubation in the presence of 1 μM or higher concentration.

Western Blot Analysis^[1]

Cell Line:

Ba/F3.p210 and Ba/F3.p210^E255V cells
Concentration:

0.1, 1, 10 μM
Incubation Time:

90 minutes
Result:

Decreased the autophosphorylation levels at a concentration of 1 μM and were barely detectable at 10 μM, whereas the level of total Bcr-abl remained unchanged.
Induced a significant decrease in the levels of p-Stat5 (at Y694) at 1 μM in Ba/F3.p210 and Ba/F3.p210^E255V cells.

In Vivo

GNF-2 (10 mg/kg; i.p. for 8 days) protects LPS (5 mg/kg) induced bone erosion in mice. GNF-2 protects the LPS induced bone loss and abrogates the LPS-induced decreases of bone volume/tissue volume (BV/TV) of LPS-treated mice^[2].
GNF-2 prevents the LPS-induced increases of N.Oc/B.Pm, the percentage of Oc.S/BS, and the percentage of ES/BS^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Eight-week-old C57/BL6 mice were administered i.p. injections of LPS (5 mg/kg)^[2]
Dosage:

10 mg/kg
Administration:

I.p. injections for 8 days; 1 day before and every day after the LPS injection
Result:

Prevented inflammatory bone destruction in vivo.

Chemical Information

CAS No. 778270-11-4
Appearance Solid
Masse moléculaire 374.32
Formule C₁₈H₁₃F₃N₄O₂
Color White to off-white
SMILES

O=C(C1=CC=CC(C2=CC(NC3=CC=C(OC(F)(F)F)C=C3)=NC=N2)=C1)N
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (3)

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Journal Impact Factor

Nature

Inhibitors supercharge kinase turnover through native proteolytic circuits. [Abstract]

2026 Jan;649(8098):1032-1041. PMID: 41299171
Nucleic Acids Res

COVID19 Drug Repository: text-mining the literature in search of putative COVID19 therapeutics. [Abstract]

2021 Jan 8;49(D1):D1113-D1121. PMID: 33166390
bioRxiv

Ras-Responsive Element Binding Protein 1 regulates survival of Group 3 medulloblastoma. [Abstract]

2025 Jul 21:2025.07.16.665230. PMID: 40777316

Solvant et solubilité

In Vitro:

DMSO : ≥ 100 mg/mL (267.15 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6715 mL

13.3576 mL

26.7151 mL

5 mM

0.5343 mL

2.6715 mL

5.3430 mL

10 mM

0.2672 mL

1.3358 mL

2.6715 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

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Elemental Analysis Report (2659 KB)
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Références

[1]. Adrián FJ, et al. Allosteric inhibitors of Bcr-abl-dependent cell proliferation. Nat Chem Biol. 2006 Feb;2(2):95-102. [Content Brief]

[2]. Kim HJ, et al. The tyrosine kinase inhibitor GNF-2 suppresses osteoclast formation and activity. J Leukoc Biol. 2013 Oct 15. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6715 mL	13.3576 mL	26.7151 mL	66.7878 mL
	5 mM	0.5343 mL	2.6715 mL	5.3430 mL	13.3576 mL
	10 mM	0.2672 mL	1.3358 mL	2.6715 mL	6.6788 mL
	15 mM	0.1781 mL	0.8905 mL	1.7810 mL	4.4525 mL
	20 mM	0.1336 mL	0.6679 mL	1.3358 mL	3.3394 mL
	25 mM	0.1069 mL	0.5343 mL	1.0686 mL	2.6715 mL
	30 mM	0.0891 mL	0.4453 mL	0.8905 mL	2.2263 mL
	40 mM	0.0668 mL	0.3339 mL	0.6679 mL	1.6697 mL
	50 mM	0.0534 mL	0.2672 mL	0.5343 mL	1.3358 mL
	60 mM	0.0445 mL	0.2226 mL	0.4453 mL	1.1131 mL
	80 mM	0.0334 mL	0.1670 mL	0.3339 mL	0.8348 mL
	100 mM	0.0267 mL	0.1336 mL	0.2672 mL	0.6679 mL

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GNF-2

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Publications Citing Use of MedChemExpress (MCE) GNF-2

Voir tous les produits spécifiques à Isoform Bcr-Abl

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GNF-2

Cytoskeleton Compound Library

Anti-Alzheimer's Disease Compound Library

Anti-Blood Cancer Compound Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Anti-Infection Compound Library

Kinase Inhibitor Library

Protein Tyrosine Kinase Compound Library

Anti-Cancer Compound Library

Antiviral Compound Library

Publications Citing Use of MedChemExpress (MCE) GNF-2

Voir tous les produits spécifiques à Isoform Bcr-Abl

Activité biologique

Chemical Information

Publications (3)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

GNF-2 Related Classifications

HY-11007 Related Classifications