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UNC10245380

Chemical Structure : UNC10245380

CAS No.:

UNC10245380 (UNC5380)

Catalog No.: PC-22593Not For Human Use, Lab Use Only.

UNC10245380 (UNC5380) is a small molecule ligand/inhibitor of Calcium and Integrin Binding protein 1 (CIB1) with IC50 of 8.0 uM in TR-FRET displacement assay, selectively kills CIB1 depletion-sensitive TNBC cells.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

UNC10245380 (UNC5380) is a small molecule ligand/inhibitor of Calcium and Integrin Binding protein 1 (CIB1) with IC50 of 8.0 uM in TR-FRET displacement assay, selectively kills CIB1 depletion-sensitive TNBC cells.
UNC10245380 shows significant cell killing activity in both CIB1-depletion-sensitive (MDA-MB-461, and MDA-MB-468) cell lines.
UNC10245380 shows no activity in the CIB1-depletion-insensitive (MDA-MB-231) cell line.
UNC10245380 also shows >90% dose-dependent cell death of MDA-468 TNBC cells over 48 h, indicating a more robust and rapid cell death than CIB1 shRNA depletion by 72 h.
UNC10245380 inhibits AKT and ERK phosphorylation in CIB1 depletion-sensitive, but not insensitive cell lines.
) upregulates γH2AX and inhibits AKT and ERK phosphorylation in CIB1 depletion-sensitive, but not insensitive cell lines.
UNC10245380 closely parallels the CIB1 depletion cell death and signaling phenotypes in TNBC cells.

Physicochemical Properties

M.Wt 578.13
Formula C30H32ClN5O3S
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

N-(2-chlorobenzyl)-4-((2-((2-((5-methyl-1H-pyrazol-3-yl)amino)-2-oxoethyl)thio)-4-oxo-3,4-dihydroquinolin-3-yl)methyl)cyclohexane-1-carboxamide

References

1. An Y, et al. Nat Commun. 2024 Jul 2;15(1):5564.

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