KZR-261 [CAS 2376747-46-3]

KZR-261 is a Sec61 inhibitor. KZR-261 directly binds to the Sec61 channel to potently inhibit the biogenesis of a subset of Sec61 client proteins. KZR-261 has a broad antitumor activity (such as colorectal pancreas and prostate cancer), along with the activation of an endoplasmic reticulum stress response, with minimal adverse effects on normal cells. KZR-261 significantly induces apoptosis of H929 cells. KZR-261 potently inhibits tumor growth in multiple xenograft tumor mice models with good tolerance[1].

[2376747-46-3]

C38H61FN6O5S2

765.06

O=S(N1CCCN(CCCN(C[C@H](C1)C)S(N2C[C@H](N([C@@H](C2)C)C3=CC(OC)=CC(F)=C3)C)(=O)=O)CC4CCCCC4)(C5=CC=C(C=C5)N(C)C)=O

Apoptosis; Caspase; Sec61

Caspase 3; Caspase 7

Room temperature