GNE-495

Name: GNE-495
Brand: MedChemExpress
SKU: HY-100343
Rating: 5.0 (10 reviews)

Cat. No.: HY-100343 Purity: 99.49%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC₅₀ of 3.7 nM.

For research use only. We do not sell to patients.

CAS No. : 1449277-10-4

Size	Stock	Quantity
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
25 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
200 mg	Get quote
500 mg	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 10 publication(s) in Google Scholar

Other Forms of GNE-495:

GNE-495 (Standard) Get quote

10 Publications Citing Use of MCE GNE-495

In Vivo Efficacy Study

Cell Migration/Invasion Assay

: GNE-495 purchased from MedChemExpress. Usage Cited in: Cancer Lett. 2026 Feb 16:218336.; GNE-495 (3 mg/kg; i.p.; once daily for 3 weeks) reduced tumor burden in KPC (Pdx1-Cre x LSL-KRAS^G12D x LSL-TP53^R172H) mice.

: GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]; GNE-495 (0.2-10 µM; 24 h) dramatically diminished the expression of MAP4K4 in Huh7 and PLC/PRF/5 cells.

: GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]; GNE-495 (2 µM; 24 h). Representative images and quantification of the Huh7 and PLC/PRF/5 cells in the wound-healing migration assays.

: GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]; GNE-495 (2 µM; 24 h). Representative images and quantification of the migration and invasion of the Huh7 and PLC/PRF/5 cells in the Transwell assays.

: GNE-495 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2024 Jun;11(24):e2306671. [Abstract]; Protein expression of EMT‐associated proteins in HCC and PLC/PRF/5 cells treated with GNE-495 (2 µM; 24 h).

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MAP4K Isoform Specific Products:

View All Isoforms

MAP4K2/GCK MAP4K3/GLK MAP4K4/HGK MAP4K5/KHS1 MAP4K6/MINK1 MAP4K7/TNIK MAP4K1/HPK1

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

GNE-495 is a potent and selective MAP4K4 inhibitor with an IC₅₀ of 3.7 nM.

IC₅₀ & Target^[1]

MAP4K4

3.7 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
HUVEC	IC₅₀	0.057 nM Compound: 13, GNE-495	Anti-angiogenesis activity in HUVEC assessed as inhibition of cell migration Anti-angiogenesis activity in HUVEC assessed as inhibition of cell migration	[PMID: 26288693]

In Vitro

GNE-495 is a potent and selective MAP4K4 inhibitor with efficacy in retinal angiogenesis. GNE-495 shows the best balance of MAP4K4 inhibition, permeability, microsomal stability, and cellular potency^[1].

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

In Vivo

GNE-495 is administered intraperitoneally to neonatal mouse pups at high doses: 25 and 50 mg/kg. GNE-495 shows good in vivo profile in all species tested, with low clearances, moderate terminal half-lives, and reasonable oral exposure levels (F=37-47%)^[1].

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

Molecular Weight

405.42

Formula

C₂₂H₂₀FN₅O₂

CAS No.

1449277-10-4

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C1=C2C=CC(C3=CC=CC(F)=C3)=NC2=C(N)N=C1)NC4CN(C(C5CC5)=O)C4

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Solvent & Solubility

In Vitro:

DMSO : 2.17 mg/mL (5.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4666 mL	12.3329 mL	24.6658 mL
5 mM	0.4933 mL	2.4666 mL	4.9332 mL
10 mM	---	---	---

View the Complete Stock Solution Preparation Table

* 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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: 2% DMSO 40% PEG300 5% Tween-80 53% PBS
Solubility: 1 mg/mL (2.47 mM); Suspended solution; Need ultrasonic
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

This protocol yields a clear solution of ≥ 0.22 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.2 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

This protocol yields a clear solution of ≥ 0.22 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (2.2 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 4

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 0.22 mg/mL (0.54 mM); Clear solution

This protocol yields a clear solution of ≥ 0.22 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 (2.2 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.49%

Select Batch:

Data Sheet (279 KB) SDS (393 KB)

COA (252 KB) LCMS (96 KB)

Handling Instructions (2659 KB)

References

[1]. Ndubaku CO et al. Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis. ACS Med Chem Lett. 2015 Jun 29;6(8):913-8. [Content Brief]

Animal Administration
^[1]

Rats, Mice and Pups ^[1]
For the brain cassette study, three male Sprague-Dawley (SD) rats are dosed with intravenous (IV) bolus of six test compounds (e.g., GNE-495; 0.5 mg/kg). For the mouse PK study, female CD-1 mice are administered IV bolus doses of GNE-495 (1 mg/kg). In addition, female CD-1 mice are administered GNE-495 (5 mg/kg) via oral (PO) gavage. A dosing volume of 2 mL/kg is used for the rat brain cassette PK and 5 mL/kg is used for all other dosing. Animals are not fasted prior to dose administration, and water and food are available ad libitum. Following administration of the compound of interest, three blood samples (~60 μL) are collected at each time point from individual mice up to either 9 or 24 hours post-dose using a serial sampling approach. Immediately upon collection, the blood is mixed with K2EDTA and stored on ice or in a chilled Kryorack prior to centrifugation to obtain plasma. Within 1 hr of collection, blood samples are centrifuged at approximately 1000-2000× g for 10-15 min at 4°C, and plasma is harvested. The plasma samples are stored at -70 to -80°C until analysis. For neonate PK, 3-day old CD1 pups are injected with 25 mg/kg and 50 mg/kg GNE-495 intraperitoneally, blood samples are collected at the time points indicated, retinas are collected one hour post-dose and snap frozen in liquid nitrogen and stored at -80°C until analysis. Plasma and retinal lysate concentrations are determined by LC/MS/MS.

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

References

[1]. Ndubaku CO et al. Structure-Based Design of GNE-495, a Potent and Selective MAP4K4 Inhibitor with Efficacy in Retinal Angiogenesis. ACS Med Chem Lett. 2015 Jun 29;6(8):913-8. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4666 mL	12.3329 mL	24.6658 mL	61.6644 mL
DMSO	5 mM	0.4933 mL	2.4666 mL	4.9332 mL	12.3329 mL

GNE-495 Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GNE-4951449277-10-4GNE495GNE 495MAP4KMAPK Kinase Kinase KinaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

GNE-495

Customer Review

Other Forms of GNE-495:

GNE-495 Related Antibodies

10 Publications Citing Use of MCE GNE-495

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All MAP4K Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

GNE-495 Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

GNE-495 Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report