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GW280264X

Names

[ CAS No. ]:
866924-39-2

[ Name ]:
GW280264X

Biological Activity

[Description]:

GW280264X is the mixed ADAM10/TACE (ADAM17) metalloproteinases inhibitor. GW280264X potently blocks TACE (ADAM17) and ADAM10 with IC50s of 8.0 nM and 11.5 nM, respectively[1]. ADAM10 and 17 modulate the immunogenicity of glioblastoma-initiating cells[2].

[Related Catalog]:

Research Areas >> Cancer
Research Areas >> Inflammation/Immunology
Signaling Pathways >> Metabolic Enzyme/Protease >> MMP

[Target]

ADAM17:8 nM (IC50)

ADAM10:11.5 nM (IC50)


[In Vitro]

The proliferation of GS-7 cells was significantly reduced upon treatment with GW280264X or ADAM10/17 co-knockdown[2]. Cell Viability Assay[2] Cell Line: Glioblastoma-initiating cells (GIC) GS-7 cells Concentration: 0.1, 1, and 3 µM Incubation Time: 48 hours Result: Proliferation of GIC is inhibited through inhibition of ADAM10 and ADAM17.

[In Vivo]

Pharmacological inhibition of ADAM10 and ADAM17 improves functional recovery after spinal cord injury (SCI)[3]. Animal Model: C57BL/6 mice[3] Dosage: 100  µg/kg Administration: I.p. injected; every day for one week starting 4 h post-surgery Result: Showed significantly improved functional recovery compared to the control group.

[References]

[1]. Christian Hundhausen, et al. The disintegrin-like metalloproteinase ADAM10 is involved in constitutive cleavage of CX3CL1 (fractalkine) and regulates CX3CL1-mediated cell-cell adhesion. Blood. 2003 Aug 15;102(4):1186-95.

[2]. Fabian Wolpert, et al. A disintegrin and metalloproteinases 10 and 17 modulate the immunogenicity of glioblastoma-initiating cells. Neuro Oncol. 2014 Mar;16(3):382-91.

[3]. Daniela Sommer, et al. ADAM17-deficiency on microglia but not on macrophages promotes phagocytosis and functional recovery after spinal cord injury. Brain Behav Immun. 2019 Aug;80:129-145.

Chemical & Physical Properties

[ Density]:
1.229±0.06 g/cm3

[ Molecular Formula ]:
C28H41N5O6S

[ Molecular Weight ]:
575.72

Related Compounds