Cbl-b inhibitor 25

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Chemical Structure : Cbl-b inhibitor 25

Catalog No.: PC-21631Not For Human Use, Lab Use Only.

Cbl-b inhibitor 25 is a potent, selective inhibitor of RING finger E3 ligase Cbl-b with IC50 of 15 nM in TR-FRET assays.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

Cbl-b inhibitor 25 is a potent, selective inhibitor of RING finger E3 ligase Cbl-b with IC50 of 15 nM in TR-FRET assays.
Cbl-b inhibitor 25 induces IL-2 production with EC50 of 0.41 uM in a T-cell IL-2 secretion assay.
Cbl-b inhibitor 25 binds to the TKB/RING domain of Cbl-b.
Cbl-b inhibitor 25 increases hosphorylated-PLCγ (pPLCγ) and inhibits Cbl-b ubiquitination of ZAP70, arrests E3 ligase function on downstream TCR signaling proteins as well as its own autoubiquitination.

Physicochemical Properties

M.Wt	469.55
Formula	C27H27N5O3
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
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Solubility	10 mM in DMSO
Chemical Name/SMILES	2-(((S)-2-methylmorpholino)methyl)-N-((S)-2-oxo-5-phenyl-2,3-dihydro-1H-pyrido[3,4-e][1,4]diazepin-3-yl)benzamide

References

1. Jeffrey A Boerth, et al. ACS Med Chem Lett. 2023 Nov 17;14(12):1848-1856.

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