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RhoA inhibitor CL16

Chemical Structure : RhoA inhibitor CL16

CAS No.: 790725-79-0

RhoA inhibitor CL16

Catalog No.: PC-25414Not For Human Use, Lab Use Only.

RhoA inhibitor CL16 is a specific small molecule covalent inhibitor with binding IC50 of 440 nM, targets the unique Cys16 on RhoA subfamily, effectively disrupts GTP binding and inhibits RhoA activity in CRC cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

RhoA inhibitor CL16 is a specific small molecule covalent inhibitor with binding IC50 of 440 nM, targets the unique Cys16 on RhoA subfamily, effectively disrupts GTP binding and inhibits RhoA activity in CRC cells.
CL16 exhibits high specificity over other Rho family proteins, shows no observable binding with Rac1 and Cdc42.
CL16 binding with RhoA Cys16 prohibits RhoA-GTP binding and RhoA-GEF interactions.
CL16 (10 uM) is more effective than Rhosin (Cat# PC-43133) on inhibition of RhoA activity in CRC cells.
CL16 exhibits anticancer and antimetastatic effects on CRC through RhoA downregulation, has cytotoxic IC50 of 3.32 uM for HCT116 cells, but not normal colon fibroblast CCD-18Co cells.
CL16 (10 mg/kg, i.p. injection) significantly inhibited tumor growth of HCT116 xenograft, HT29 xenograft and SW620 xenograft.

Physicochemical Properties

M.Wt 328.75
Formula C17H13ClN2O3
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-(3-(benzofuran-2-yl)-5-(furan-2-yl)-4,5-dihydro-1H-pyrazol-1-yl)-2-chloroethan-1-one

References

1. Koo TY, et al. Cell Chem Biol. 2025 Sep 2:S2451-9456(25)00255-7.

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