GW280264X

Cas No.:	866924-39-2
Chemical Name:	GW 280264X
Synonyms:	GW280264X;AOB3632;Benzyl ((S)-5-((2R,3S)-3-(N-hydroxyformamido)-2-isobutylhexanamido)-6-oxo-6-(thiazol-2-ylamino)hexyl)carbamate;CID 91885425;Carbamic acid, N-[(5S)-5-[[(2R,3S)-3-(formylhydroxyamino)-2-(2-methylpropyl)-1-oxohexyl]amino]-6-oxo-6-(2-thiazolylamino)hexyl]-, phenylmethyl ester;GW280264X，Carbamic acid;GW-280264X,inhibit,GIC,Inhibitor,immunotherapy,metalloproteinases,Matrix metalloproteinases,ADAM10,TACE,immunogenicity,glioblastoma,Mixed,MMP,GW280264X,ADAM17,stem
SMILES:	S1C=CN=C1NC([C@H](CCCCNC(=O)OCC1C=CC=CC=1)NC([C@H](CC(C)C)[C@H](CCC)N(C=O)O)=O)=O
Formula:	C28H41N5O6S
M.Wt:	575.720045804977
Purity:	>98%
Sotrage:	0°C (short term), -20°C (long term), desiccated

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].
Target:	ADAM17:8 nM (IC50) ADAM10:11.5 nM (IC50)
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.
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.
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.