KZR-261

• Description:

  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].

• UNSPSC:

  12352005

• Target:

  Apoptosis; Caspase; Sec61

• Related Pathways:

  Apoptosis; Membrane Transporter/Ion Channel

• Field of Research:

  Cancer

• Smiles:

  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

• Molecular Formula:

  C38H61FN6O5S2

• Molecular Weight:

  765.06

• References & Citations:

  [1]Lowe E, et al. Preclinical characterization of novel multi-client inhibitors of Sec61 with broad antitumor activity. J Pharmacol Exp Ther. 2025 Jun 14;392 (8) :103634.

• Shipping Conditions:

  Room temperature

• Scientific Category:

  Reference compound1

• Clinical Information:

  No Development Reported

• Isoform:

  Caspase 3; Caspase 7

• CAS Number:

  2376747-46-3