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KZR-261

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].

Product Specifications

CAS Number

[2376747-46-3]

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

Curated Selection

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