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142D6

Chemical Structure : 142D6

CAS No.: 2410953-19-2

142D6

Catalog No.: PC-20879Not For Human Use, Lab Use Only.

142D6 is a potent, Lys-covalent pan-IAP inhibitor, targets the BIR3 domain of the inhibitor of the apoptosis protein (IAP) family with IC50 of 43/21/21 nM for XIAP/cIAP1/cIAP2, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

142D6 is a potent, Lys-covalent pan-IAP inhibitor, targets the BIR3 domain of the inhibitor of the apoptosis protein (IAP) family with IC50 of 43/21/21 nM for XIAP/cIAP1/cIAP2, respectively.
142D6 targets XIAP-BIR3 residue Lys 299. similar potency to the clinical candidate LCL161 against breast cancer cell line MDA-MB-231with the EC50 values of 44 and 37 nM in the cell viability assays, respectively, and with EC50 values of 61 and 57 nM in the apoptosis assays, respectively.
142D6 is chemically stable in buffer and plasma and reacted covalently in a very selective way.

Physicochemical Properties

M.Wt 552.66
Formula C26H37FN4O6S
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

O=S(OC1=CC=CC2=C1CC[C@H]2NC([C@H]3N(C([C@H](C4CCCCC4)NC([C@@H](NC)C)=O)=O)CCC3)=O)(F)=O

References

1. Udompholkul P, et al. J Med Chem. 2023 Jun 1. doi: 10.1021/acs.jmedchem.3c00467.

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