pro-apoptotic

The compound, tumor-targeted pro-apoptotic peptide (CNGRC-GG-D(KLAKLAK)2), functions as an anti-tumor agent by disrupting mitochondrial membranes to induce apoptosis, demonstrating anticancer efficacy in mice [1].

Pasireotide (SOM230) acetate is a long-acting cyclohexapeptide growth hormone inhibitory hormone analog with antisecretory, antiproliferative, and proapoptotic activities.Pasireotide (SOM230) acetate inhibits the secretion of GH, IGF-I, and ACTH, and can be used in the study of acromegaly and Cushing's disease. Pasireotide (SOM230) acetate also enhances the agonist activity of growth inhibitory receptors, with pKi of 8.2, 9.0, 9.1, <7.0 and 9.9 for sst1, 2, 3, 4 and 5, respectively.

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].

HKPao (Hunter-killer peptide ao) is a biologically active peptide with dual functionality, exhibiting anti-obesity and anti-tumor pro-apoptotic activities by inducing cytochrome c release from vesicles, thus significantly contributing to cellular apoptosis [1].

Bim BH3 is a bioactive peptide that belongs to the pro-apoptotic Bcl-2 family of proteins.

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.

r8 Bid BH3, a biologically active peptide, is a pro-apoptotic member of the BH3-only subset within the BCL-2 family proteins, pivotal in regulating apoptosis. This compound exhibits lethality towards Bcl-2-expressing human leukemia cell lines, indicating its promise as a potential cancer therapeutic. The peptide is conjugated with poly-D-arginine (denoted by rrrrrrrr), enhancing cellular uptake.

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.

This Bim peptide belongs to the pro-apoptotic group of the Bcl-2 family of proteins.

Bim BH3, Peptide IV TFA is a 26-site residue of BH3 protein Bim, belonging to the pro-apoptotic group of bcl-2 protein family.

Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 3 μM), and induces cell cycle arrest. Promotes activation of caspase-3 and exhibits pro-apop

Cell-permeable peptide cleaved from protease-activated receptor 1 (PAR1) upon receptor activation. Attenuates endothelial cell migration and proliferation (IC50 ~ 20 μM), and induces cell cycle arrest. Promotes activation of caspase-3 and exhibits pro-apo

P160 peptide is a breast cancer-targeting peptide that binds to the keratin 1 (KRT1) receptor in breast cancer cells, with a Kd of approximately 1.1 μM. It shows significant potential for targeted drug delivery to breast cancer cells. P160 peptide enhances the cellular uptake and anticancer activity of the pro-apoptotic antimicrobial peptide MccJ25 (microcin J25). It is applicable in cancer research studies.

The LinTT1 peptide is a tumor-penetrating peptide with the amino acid sequence AKRGARST. It targets peritoneal cancer (PC) by binding to the p32 (gC1qR) receptor. The LinTT1 can associate with iron oxide nanohelical (NWs) structures to form a nanocarrier that is taken up by peritoneal cancer cells in vitro and penetrates mitochondria; it also shows significant tumor-targeting and penetration effects in vivo in mice. Furthermore, LinTT1-functionalized nanocarriers combined with the pro-apoptotic peptide [D(KLAKLAK)2] demonstrate substantial tumor inhibition in a mouse peritoneal tumor model. LinTT1 peptide holds promise as a delivery vehicle for peritoneal cancer research.