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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
DC33635 DODAP DODAP, also known as 1,2-Dioleoyl-3-dimethylammonium-propane, is a cationic lipid. It has been used as a component in liposomes that can be used to encapsulate siRNA, immunostimulatory oligodeoxynucleotides, antisense oligonucleotides, or chemotherapeutic agents for in vitro and in vivo delivery.
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.
DC74576 Fluorofurimazine Fluorofurimazine is a novel furimazine analogue, with increased aqueous solubility enabling higher signal emission than furimazine for bioluminescence imaging. Fluorofurimazine enables higher substrate loading and improved optical imaging sensitivity in in-vivo.
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.
DC74225 YB-537 YB-537 (YB537) is a potent, highly specific quinone reductase 2 (QR2) inhibitor with IC50 of 3 nM, shows no activity against QR1 (IC50>10 uM).
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