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GSK2646264

GSK2646264 (Compound 44) is a potent and selective spleen tyrosine kinase (SYK) inhibitor with a pIC50 of 7.1. GSK2646264 also inhibits other kinases with pIC50 values of 5.4, 5.4, 5.3, 5, 4.5, LCK, LRRK2, GSK3β, JAK2, VEGFR2, Aurora B and Aurora A, respectively. GSK2646264 is penetrable into the epidermis and dermis of the skin[1].

Product Specifications

CAS Number

[1398695-47-0]

UNSPSC

12352005

Target

Aurora Kinase; GSK-3; JAK; LRRK2; Src; Syk; VEGFR

Type

Reference compound

Related Pathways

Autophagy; Cell Cycle/DNA Damage; Epigenetics; JAK/STAT Signaling; PI3K/Akt/mTOR; Protein Tyrosine Kinase/RTK; Stem Cell/Wnt

Applications

COVID-19-anti-virus

Field of Research

Inflammation/Immunology

Assay Protocol

https://www.medchemexpress.com/gsk2646264.html

Purity

98.39

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

CC1=CC(COC2=C(C3=CC=C4CCNCCC4=C3)C(OC)=CC=C2)=NC=C1

Molecular Formula

C24H26N2O2

Molecular Weight

374.48

References & Citations

[1]Barker MD, et al. Discovery of potent and selective Spleen Tyrosine Kinase inhibitors for the topical treatment of inflammatory skin disease. Bioorg Med Chem Lett. 2018 Nov 15;28 (21) :3458-3462. |[2]Ramirez Molina C, et al. GSK2646264, a spleen tyrosine kinase inhibitor, attenuates the release of histamine in ex vivo human skin. Br J Pharmacol. 2019 Apr;176 (8) :1135-1142.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, protect from light)

Scientific Category

Reference compound1

Clinical Information

Phase 1

Isoform

Aurora A; Aurora B; GSK-3β; JAK2; VEGFR2/KDR/Flk-1

Available Sizes

Curated Selection

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