bak bh3

This peptide, generated from the BH3 domain of Bak (Flu-BakBH3), has been shown to have high-affinity binding to a surface pocket of the Bcl-XL protein that is required for its death antagonist function.

Bak BH3 (72-87), TAMRA-labeled, is a bioactive peptide.

BH3I-2' is a cell-permeable BH3 mimetic. BH3I-2' induces apoptosis by specifically preventing BH3 domain-mediated interactions between pro-apoptotic and anti-apoptotic members of the Bcl-2 family, thereby blocking the interaction between Bcl-x and Bak BH3 by targeting the Bcl-x binding pocket.

JY-1-106 is a BH3 α-helix mimetic, inducing apoptosis in a subset of cancer cells (lung cancer, colon cancer and mesothelioma) by disrupting Bcl-xL and Mcl-1 protein-protein interactions with Bak.

1. Chelerythrine (Broussonpapyrine) may have antimanic effect . 2. Chelerythrine can inhibit telomerase activity. 3. Chelerythrine is a well-known protein kinase C inhibitor . 4. Chelerythrine has potential antiproliferative and antitumor effects.

PUMA BH3 (TFA), a peptide from the BH3 domain of the p53 upregulated modulator of apoptosis (PUMA), directly activates Bak with a dissociation constant (Kd) of 26 nM [1].

BH3 hydrochloride, a peptide that crosses the blood-brain barrier, induces apoptosis either through direct activation of the pro-apoptotic proteins Bax/Bak or by inhibiting anti-apoptotic Bcl-2 proteins (Bcl-2, Bcl-XL, Bcl-w, Mcl-1, and A-1) through their BH3 domain [1][2].

Bid BH3 (80-99) is a biologically active peptide and a pro-apoptotic member of the 'BH3-only' (BOPS) subset within the BCL-2 protein family, crucial in apoptosis regulation. It interacts with Bcl-2, Bax, and Bak to initiate their activation or inactivation, inducing cell death. Bid translocates from the cytosol to the mitochondrial membrane as part of its mechanism. Pyroglutamyl (pGlu) peptides, which can arise from Glutamine (Q) or Glutamic acid (E) at the N-terminus, have a hydrophobic γ-lactam ring that enhances stability and provides resistance to gastrointestinal proteases. These peptides are recognized variants in peptide analyses, including HPLC purity assessments.

PUMA BH3, a peptide that includes the BH3 domain from the p53-upregulated modulator of apoptosis (PUMA) and activates the pro-apoptotic protein Bak, demonstrates binding affinity to Bak with dissociation constants (Kds) of 290 nM in HEPES buffer and 26 nM in CHAPS buffer. This interaction with Bak induces its homo-oligomerization and facilitates Bak-mediated membrane permeabilization.

Mcl-1 inhibitor 17 is an effective inhibitor of the Mcl-1 protein. Mcl-1 is a critical anti-apoptotic member of the Bcl-2 family, frequently overexpressed in various malignancies, where it suppresses apoptosis by sequestering pro-apoptotic proteins such as Bak and Bax. Mcl-1 inhibitor 17 functions by competitively binding to the BH3-binding groove of Mcl-1, thereby releasing pro-apoptotic factors and restoring apoptotic sensitivity in cancer cells. This compound is utilized for research into cancer and other diseases associated with Mcl-1 dysregulation.

BRD-810 is a highly selective MCL1 inhibitor (Kd=0.3 nM) capable of inducing tumour cell apoptosis, suitable for studying haematological malignancies and solid tumours. BRD-810 binds the BH3 groove of MCL1, activates Caspase, and disrupts the MCL1-BAK complex in cancer cells (IC50=1.2 nM).

ABT 737-d8 is the deuterated form of ABT-737, a BH3 mimetic and potent inhibitor of Bcl-2, Bcl-xL, and Bcl-w, with EC50 values of 30.3 nM, 78.7 nM, and 197.8 nM respectively. ABT-737 disrupts the BCL-2/BAX complex and activates the intrinsic apoptotic pathway in a BAK-dependent and BIM-independent manner. Additionally, ABT-737 induces autophagy and shows potential for research in acute myeloid leukemia (AML).

PUMA BH3 (TFA) is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide, acts as a direct activator of Bak, with a Kd of 26 nM.

PUMA BH3 is a p53 upregulated modulator of apoptosis (PUMA) BH3 domain peptide that acts as a direct activator of Bak with a Kd of 26 nM. PUMA proteins bind Bcl-2, localize to the mitochondria, and induce cytochrome C release and apoptosis in response to p53, potentially mediating p53-induced apoptosis.

PUMA BH3 acetate (PUMA BH3 Free base) is a p53 positive regulator of apoptosis (PUMA) BH3 domain polypeptide that acts as a direct activator of Bak with a Kd of 26 nM.

Bid BH3 peptide, a small peptide derived from the Bid protein, binds to and activates the pro-apoptotic proteins Bax and Bak, leading to mitochondrial outer membrane permeabilization (MOMP) and cell apoptosis (apoptosis). This peptide is utilized in research on mitochondrial bioenergetics.