Drug intelligence / Profile preview

BIM SAHB

Development stage
Preclinical
Lead developer
Dana-Farber Cancer Institute
Modality
Peptides
Administration
Intravenous
01

Overview

BIM SAHB (Stabilized Alpha-Helix of BCL-2 domain) is a hydrocarbon-stapled peptide derived from the BH3 death domain of the pro-apoptotic protein BIM (BCL2L11). The SAHB technology utilizes a synthetic hydrocarbon bridge to cross-link the peptide backbone, reinforcing its alpha-helical conformation and significantly enhancing its metabolic stability, protease resistance, and cellular permeability compared to unmodified peptides. BIM SAHB acts as a potent pan-BH3 mimetic, capable of both directly activating the pro-apoptotic effectors BAX and BAK and neutralizing the full spectrum of anti-apoptotic BCL-2 family proteins, including BCL-2, BCL-XL, and MCL-1. In clinical research, it is primarily used as a functional probe in assays such as BH3 profiling and the SABRE (Single-cell Analysis of BAX REsponses) assay to measure mitochondrial priming and the maximal potential for BAX activation in cancer cells, which helps in predicting sensitivity or resistance to BCL-2 inhibitors like venetoclax.

Other names
BIM BH3 SAHBstapled BIM BH3 peptide
02

Targets

Bcl-w (B-cell lymphoma 2-like 2)BAKBFL-1 (BCL2-related protein A1)BAX (Apoptosis regulator BAX)BCL2L1 (B-cell lymphoma-extra large protein)MCL1 (Myeloid cell leukemia sequence 1)

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