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Chemical Structure : PREX-in1
Catalog No.: PC-20881Not For Human Use, Lab Use Only.
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.
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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.
PREX-in1 is selective for P-Rex1 and P-Rex2 over a panel of other Rho-GEFs.
PREX-in1 (10 uM) inhibits PIP3-stimulated Rac-GEF activity of full-length P-Rex1 and P-Rex2 in liposome-based in vitro GEF activity assay.
PREX-in1 also inhibits P-Rex1 in the mant-GTP assay (IC50=10 uM), but not EHop-016.
PREX-in1 inhibits P-Rex Rac-GEFs, but not a selection of other Rho-GEFs.
PREX-in1 (10 uM) affects the cell cycle in a similar manner to NSC23766, induces cell death in HEK-293 cells.
PREX-in1 (1 uM) inhibits the P-Rex1-dependent spreading of endothelial cells in response to PDGF stimulation.
PREX-in1 (1 uM) inhibits the P-Rex1 dependent production of ROS in mouse neutrophils stimulated with the chemoattractant fMLP.
| M.Wt | 444.88 | |
| Formula | C24H17ClN4O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. C D Lawson, et al. Small GTPases. 2022 Jan;13(1):307-326.
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