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Chemical Structure| 1449277-10-4 Chemical Structure| 1449277-10-4

Structure of GNE-495
CAS No.: 1449277-10-4

Chemical Structure| 1449277-10-4

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

4.5 *For Research Use Only !

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Product Details of GNE-495

CAS No. :1449277-10-4
Formula : C22H20FN5O2
M.W : 405.42
SMILES Code : O=C(C1=C2C=CC(C3=CC=CC(F)=C3)=NC2=C(N)N=C1)NC4CN(C(C5CC5)=O)C4
MDL No. :MFCD30489735
InChI Key :FYXCIBJXJYBWPX-UHFFFAOYSA-N
Pubchem ID :89730041

Safety of GNE-495

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H332-H335
Precautionary Statements:P261-P280-P305+P351+P338

Related Pathways of GNE-495

MAPK

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
AsPC-1 2 µM 24 hours GNE-495 could not block MLK3 T738D-induced JNK and c-Jun activation Oncogene. 2021 Oct;40(43):6153-6165
PANC-1 2 µM 24 hours GNE-495 blocked TNFα-induced activation of JNK and c-Jun Oncogene. 2021 Oct;40(43):6153-6165
Capan-1 2 µM 24 hours GNE-495 blocked TNFα-induced activation of JNK and c-Jun Oncogene. 2021 Oct;40(43):6153-6165
A549 5 µM 48 hours Inhibited MAP4K4 levels and c-JUN phosphorylation, reversing the enhanced migration and invasion capabilities induced by HMMR overexpression Int J Biol Sci. 2025 Jan 21;21(4):1391-1409
H1299 5 µM 48 hours Inhibited MAP4K4 levels and c-JUN phosphorylation, reversing the enhanced migration and invasion capabilities induced by HMMR overexpression Int J Biol Sci. 2025 Jan 21;21(4):1391-1409
MR cells (radioresistant MCF-7 cells) 500 nM 48 hours To evaluate the cytotoxic effects of GNE-495 on MR cells, results showed GNE-495 significantly reduced the viability of MR cells. Sci Rep. 2024 Mar 28;14(1):7410
SR cells (radioresistant SK-BR-3 cells) 500 nM 48 hours To evaluate the cytotoxic effects of GNE-495 on SR cells, results showed GNE-495 significantly reduced the viability of SR cells. Sci Rep. 2024 Mar 28;14(1):7410

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mouse KPC mouse model Intraperitoneal injection 3 mg/kg body weight Daily for 3 months GNE-495 significantly extended the survival of KPC mice, reduced tumor burden, and induced tumor cell death Oncogene. 2021 Oct;40(43):6153-6165
BALB/c nude mice LUAD metastasis model Intraperitoneal injection 3 mg/kg Once daily for three weeks GNE-495 treatment effectively reversed the lung metastasis induced by HMMR overexpression Int J Biol Sci. 2025 Jan 21;21(4):1391-1409
Mice Retinal vascular development model Intraperitoneal injection 25 and 50 mg/kg Daily from P1 to P5 or P6 To evaluate the antiangiogenic effects of GNE-495 in vivo, results showed GNE-495 dose-dependently delayed retinal vascular outgrowth and induced abnormal retinal vascular morphology ACS Med Chem Lett. 2015 Jun 29;6(8):913-8

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.47mL

0.49mL

0.25mL

12.33mL

2.47mL

1.23mL

24.67mL

4.93mL

2.47mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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