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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Chemical Structure| 866924-39-2 Chemical Structure| 866924-39-2

Structure of GW280264X
CAS No.: 866924-39-2

Chemical Structure| 866924-39-2

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GW280264X is an effective inhibitor of metalloproteinases ADAM10 and ADAM17 with IC50 values of 8.0 nM and 11.5 nM, respectively. This compound can modulate immunogenicity and has potential applications in studies of glioblastoma-initiating cells, relevant for cancer and immunotherapy research.

4.5 *For Research Use Only !

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Product Details of GW280264X

CAS No. :866924-39-2
Formula : C28H41N5O6S
M.W : 575.72
SMILES Code : O=C(OCC1=CC=CC=C1)NCCCC[C@H](NC([C@H](CC(C)C)[C@@H](N(C=O)O)CCC)=O)C(NC2=NC=CS2)=O
MDL No. :MFCD33023416

Safety of GW280264X

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H228-H315-H319
Precautionary Statements:P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
Class:4.1
UN#:1325
Packing Group:

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
BV2 cells 10 μM 12 hours Evaluate the synergistic effect of GW280264X and desmosterol on the erythrophagocytosis ability of BV2 cells, showing that GW280264X and desmosterol at 10 μM significantly enhanced the phagocytic ability of BV2 cells. Theranostics. 2024 Jan 1;14(1):283-303
GS-9 cells 3 μM 48 hours To evaluate the effect of ADAM10 and ADAM17 inhibitors on ULBP2 cell surface expression, results showed significant upregulation of ULBP2 Neuro Oncol. 2014 Mar;16(3):382-91
GS-7 cells 3 μM 48 hours To evaluate the effect of ADAM10 and ADAM17 inhibitors on ULBP2 cell surface expression, results showed significant upregulation of ULBP2 Neuro Oncol. 2014 Mar;16(3):382-91
OVCAR-8 3 μM 48 hours ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis Cancers (Basel). 2021 Apr 23;13(9):2039
SKOV-3 3 μM 48 hours ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis Cancers (Basel). 2021 Apr 23;13(9):2039
HEY 3 μM 48 hours ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis Cancers (Basel). 2021 Apr 23;13(9):2039
Igrov-1 3 μM 48 hours ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis Cancers (Basel). 2021 Apr 23;13(9):2039
A2780 3 μM 48 hours ADAM17 inhibition significantly reduced cell viability and enhanced cisplatin-induced apoptosis Cancers (Basel). 2021 Apr 23;13(9):2039
human microvascular endothelial cells (HMVEC-L) 10 μM 24 hours Inhibition of LPS-induced endothelial permeability increase and IL-8-induced neutrophil transendothelial migration EMBO Mol Med. 2012 May;4(5):412-23
Adam10/17 −/− mEFs 0.5 μM to 10 μM 2 hours GW280264X effectively inhibited ADAM9 activity at concentrations as low as 0.5 μM and increasing inhibition was observed at concentrations between 1 and 10 μM. Biochem J. 2017 Apr 13;474(9):1467-1479
human hepatic stellate cells (HSC) 3 μM GW280264X partially inhibited the release of soluble CX3CL1 from IFN-γ stimulated HSC, suggesting the involvement of other proteases. J Cell Mol Med. 2009 Aug;13(8A):1526-35
Human umbilical vein endothelial cells (HUVECs) 10 μM 30 minutes GW280264X inhibits ADAM10 and ADAM17, significantly increasing cell-surface EMCN protein levels to 231% of the vehicle control, indicating a critical role of ADAM10 in maintaining EMCN cell-surface levels. J Biol Chem. 2020 May 8;295(19):6641-6651

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice LPS-induced acute lung injury model Intranasal 40 mg/kg Single dose, observed at 4 and 24 hours GW280264X significantly reduced LPS-induced vascular permeability increase, edema formation, release of TNF-α and IL-6, and pulmonary leukocyte recruitment EMBO Mol Med. 2012 May;4(5):412-23
C57BL/6 mice Acute ischemic stroke model Intranasal administration 0.25, 0.5, 1.0, or 1.5 μg/μL Immediately after surgery, continuous observation GW280264x inhibits the metalloprotease activity of ADAM17, preventing CX3CL1 from being sheared into its soluble form, thereby promoting microglial polarization from M1 to M2 phenotype Neural Regen Res. 2023 May;18(5):1033-1039

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.74mL

0.35mL

0.17mL

8.68mL

1.74mL

0.87mL

17.37mL

3.47mL

1.74mL

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