TargetMol

GI254023X

Product Code:
 
TAR-T7522
Product Group:
 
Inhibitors and Activators
Supplier:
 
TargetMol
Regulatory Status:
 
RUO
Shipping:
 
cool pack
Storage:
 
-20℃
1 / 1
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This product comes from: Austria.
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Further Information

Bioactivity:
GI254023X is a potent MMP9 and ADAM10 inhibitor (IC50s: 2.5 and 5.3 nM) with 100-fold selectivity for the α-secretase ADAM10 over ADAM17 (TACE). GI254023X can remarkably inhibit the proliferation and induce the apoptosis of H929 cells. Its mechanism may be associated with inbihition of Notch1 activation.
CAS:
260264-93-5
Formula:
C21H33N3O4
Molecular Weight:
391.5
Pathway:
Proteases/Proteasome; Immunology/Inflammation
Purity:
0.9856
SMILES:
O=C(N[C@H](C(NC)=O)C(C)(C)C)[C@@H]([C@@H](N(C=O)O)C)CCCC1=CC=CC=C1
Target:
MMP; Immunology/Inflammation related

Documents

References

Shackleton B, et al. Inhibition of ADAM10 promotes the clearance of A? across the BBB by reducing LRP1 ectodomain shedding. Fluids Barriers CNS. 2016 Aug 8;13(1):14. Verena V. Metz, et al. Induction of RAGE Shedding by Activation of G Protein-Coupled Receptors. PLoS One. 2012. N Milosch, et al. Holo-APP and G-protein-mediated signaling are required for sAPPa-induced activation of the Akt. Cell Death Dis. 2014 Aug 28;5:e1391. M J M Gooden, et al. Elevated serum CXCL16 is an independent predictor of poor survival in ovarian cancer and may reflect pro-metastatic ADAM protease activity. British Journal of Cancer (2014) 110, 1535?1544.