BIRD-2

Description

Product name: BIRD-2

Catalog#: 1809062

Synonyms: TAT-IDP(DD/AA),Bcl-2-IP3R Disruptor-2,

CAS NO.:

Sequence: RKKRRQRRRGGNVYTEIKCNSLLPLAAIVRV

Modifications:

M.W:3650.13

M.F.:C157H280N58O40S

Purity: 95% by HPLC

Counter ion: Trifluoroacetate

Format: Lyophilized powder

Description: Currently there is no therapeutic agent designed to target the BH4 domain of Bcl-2. Therefore, to selectively target Bcl-2-IP3R interaction, we developed a synthetic peptide corresponding to the IP3R binding site for Bcl-2. This peptide disrupts Bcl-2-IP3R interaction, reversing Bcl-2′s inhibition of IP3-induced Ca2+ elevation and decreasing cell survival, without disturbing the binding of pro-apoptotic proteins by Bcl-2. Elimination of a potential protease cleavage site produced a more potent version of this peptide capable of inducing Ca2+-mediated apoptosis in primary human CLL cells (but not in normal human lymphocytes) and in diffuse large B-cell lymphoma cell lines. Here we call this peptide BIRD-2 (Bcl-2-IP3R Disruptor-2). BIRD-2 binds directly to the BH4 domain of Bcl-2, functioning as a decoy peptide to competitively inhibit Bcl-2 interaction with IP3Rs, reversing Bcl-2′s control over IP3R-mediated Ca2+ release and thereby inducing high amplitude intracellular Ca2+ elevations that trigger apoptosis.BIRD-2 is capable of inducing death in HMCLs that are resistant to both the BH3 mimetic agents ABT-263 and ABT-199 and to the Btk inhibitor Ibrutinib.

UniProt ID:

 

Usage: For Scientific Research Use Only, Not for Human Use.