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Cat. No.: HY-16984

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GNE-4997

GNE-4997 is a potent and selective interleukin-2-inducible T-cell kinase (ITK) inhibitor with a K_i of 0.09 nM, and the correlation between the basicity of solubilizing elements in GNE-4997 and off-target antiproliferative effects reduces cytotoxicity.

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

CAS No.: 1705602-02-3
Formula: C₂₅H₂₇F₂N₅O₃S
Molecular Weight:515.58

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (273 KB)

GNE-4997 Chemical Structure

CAS No.: 1705602-02-3

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

Ki: 0.09 nM (ITK)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Hepatocyte	IC₅₀	>100 μM Compound: 28, GNE-4997	Cytotoxicity against hepatocytes (unknown origin) Cytotoxicity against hepatocytes (unknown origin)	[PMID: 25844760]
Jurkat	IC₅₀	0.004 μM Compound: 28, GNE-4997	Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins Inhibition of ITK in TCR stimulated human Jurkat T cells assessed as reduction of PLC-gamma phosphorylation preincubated for 30 mins followed by TCR induction for 2 mins	[PMID: 25844760]
Jurkat	IC₅₀	12 μM Compound: 28, GNE-4997	Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay Cytotoxicity against human Jurkat T cells without TCR stimulation assessed as cell viability by ATPlite assay	[PMID: 25844760]

In Vitro

GNE-4997 inhibits PLC-γ phosphorylation in Jurkat cells by T-cell receptor stimulation with an IC₅₀ of 4 nM ^[1].

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

Chemical Information

CAS No. 1705602-02-3
Molecular Weight 515.58
Formula C₂₅H₂₇F₂N₅O₃S
SMILES

O=C(C1=NNC2=C1C[C@H](C3(F)F)[C@@]3(C)C2)NC4=CN([C@H](C5=CC=CC=C5)[C@@H]6S(CCCC6)(=O)=O)N=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Burch JD, et al. Tetrahydroindazoles as Interleukin-2 Inducible T-Cell Kinase Inhibitors. Part II. Second-Generation Analogues with Enhanced Potency, Selectivity, and Pharmacodynamic Modulation in Vivo. J Med Chem. 2015 May 14;58(9):3806-16. [Content Brief]

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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.

Keywords

100 mg

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