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GW280264X

  Cat. No.:  DC43797   Featured
Chemical Structure
866924-39-2
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More than 5000 active chemicals with high quality for research!
Field of application
Inhibitor of of the metalloproteinase ADAM17; Inhibitor of the constitutive and the PMA-inducible CX3CL1 cleavage, blocking TACE as well as ADAM10
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
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.
MSDS
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MSDS_27410_DC43797_866924-39-2
COA
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Cat. No. Product name Field of application
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DC31074 Isopropyl myristate Isopropyl myristate is the ester of isopropyl alcohol and myristic acid.
DC74583 ZK53 ZK53 is a selective activator of mitochondrial caseinolytic protease P (HsClpP). It exhibits an EC50 of 1.37 μM for α-casein hydrolysis by HsClpP. ZK53 treatment allosterically activates HsClpP to uncontrollably degrade the essential mitochondrial proteins and is inactive toward bacterial ClpP proteins.
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DC74557 PREX-in1 PREX-in1 is a specific small-molecule inhibitor of P-Rex1 and P-Rex2 Rac-GEF activity with IC50 of 4.5 uM (P-Rex1 DHPH Rac-GEF activity) in liposome-based GEF assay, inhibits P-Rex1 and P-Rex2 through their catalytic DH domain.
DC74555 GYS32661 GYS32661 (GYS 32661) is a potent Rac inhibitor capable of inhibiting both Rac1 and Rac1b, inhibited activated Rac1 with IC50 of 1.18 uM in in vitro pull-down assays.
DC74539 L557-0155 L557-0155 is a small molecule inhibitor of VSIG-8, prevents VSIG-8 binding to VISTA, promotes cytokine production and cell proliferation in PBMCs and suppresses melanoma growth.
DC74528 K284 K284 is a selective small molecule inhibitor of chitinase 3 like1 (CHI3L1) with strong binding affinity (Kd=-9.7 kcal·mol-1), inhibits lung metastasis by blocking IL-13Rα2-mediated JNK-AP-1 signals.
DC74247 AG-946 AG-946 (AG946) is a potent, allosteric activator of wild-type and mutant RBC-specific form of pyruvate kinase (PKR) with AC50 of 5 nM for human wild-type PK, 4.3 nM and 6.9 nM for mutated K410E and R510Q PK proteins, resepctively.
DC74241 Rebecsinib Rebecsinib (17S-FD-895) is a selective small-molecule inhibitor of splicing-mediated ADAR1 activation, prevents leukemia stem cell generation.
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