proapoptotic

NSC 146109 hydrochloride is an activator of p53 targeting MDMX. NSC 146109 hydrochloride can be used for studies on breast cancer.

Tributyrin (Glyceryl tributyrate), a neutral short-chain fatty acid triglyceride, is a stable and rapidly absorbed prodrug of Butyric Acid. It diffuses through biological membranes and is metabolized by intracellular lipases, releasing effective butyrate directly into cells in vivo, exhibiting potent proapoptotic, antiproliferative, and differentiation-inducing effects.

NVP-ADW742 (ADW) is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

Rilmenidine Phosphate is a selective I(1) imidazoline receptor agonist, used to treat hypertension.

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.

RGD-Targeted Proapoptotic Peptide is a peptide that preferentially binds to integrins at sites of tumor angiogenesis through its C-terminal RGD-4C sequence (ACDCRGDCFC).

d-(KLAKLAK)2 is an antimicrobial and antitumor peptide, notable within the group of antimicrobial peptides, and exhibits strong anticancer properties. It kills bacteria by disrupting their cell membranes, causing leakage of cell contents. Additionally, d-(KLAKLAK)2 inhibits tumor cell proliferation by inducing apoptosis through mitochondrial swelling and membrane damage.

SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.

UCF 101 is a specific inhibitor of HtrA2 and reduces apoptosis in PC12 cells.

CAY10526 (BTH) is a selective mPGES-1 inhibitor that acts as an inhibitor of the NF-κB signaling pathway.

α-Thujone is an inhibitor of ACh with an IC50 value of 24.7μM.

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].

Adipotide as a prototype in a new class of candidate drugs that may be useful for treating obesity in humans

RH01386 is a small molecule that prevents ER stress-induced β cell dysfunction and death, inhibits proapoptotic gene expression, and restores ER stress-impaired glucose-stimulated insulin secretion responses, showing potential for type 2 diabetes treatment.

Phytohemagglutinin (PHA-M) is a lectin, isolated from the red kidney bean , induces apoptosis via increasing proapoptotic protein Bax and activating caspases-3. Anti-tumor activity

Pasireotide pamoate is a stable cyclohexapeptide somatostatin mimic. Pasireotide pamoate exhibits antisecretory, antiproliferative, and proapoptotic activity.

LBW242 is a 3-mer and Smac mimetic and is an effective and orally active proapoptotic IAP inhibitor. LBW242 has activity against multiple myeloma and potentiates TRAIL- and anticancer drug-mediated cell death of ovarian cancer cells. LBW242 displays effec

cRIPGBM, a proapoptotic derivative of RIPGBM, selectively induces apoptosis in GBM cancer stem cells (CSCs) by targeting receptor-interacting protein kinase 2 (RIPK2), demonstrating an EC50 of 68 nM in GBM-1 cells [1].

CLM3, a pyrazolopyrimidine derivative, functions as a multitargeted tyrosine kinase inhibitor. It exhibits antiproliferative and proapoptotic activities on endothelial and cancer cells, activities that are synergistically enhanced by SN38. The primary mechanism of action for CLM3 involves the inhibition of phosphorylation in tyrosine kinases such as VEGFR-2, EGFR, and RET, along with their associated signaling pathways.

Sepantronium bromide (YM155) is a small-molecule proapoptotic agent with potential antineoplastic activity.

BAM 7 is a direct and specific activator of proapoptotic Bax (EC50: 3.3 μM).

Azadirone is a limonoid tetranortriterpene. Azadirone can sensitize cancer cells to tumor necrosis factor-related apoptosis-inducing ligand (TRAIL) through ROS-ERK-CHOP-mediated up-regulation of DR4 and DR5 signaling, down-regulation of cell survival prot

Ganglioside GM3 is a monosialoganglioside that demonstrates antiproliferative and proapoptotic effects in tumor cells by modulating cell adhesion, proliferation, and differentiation. It suppresses angiogenesis and reduces proliferation and migration of human umbilical vein endothelial cells (HUVECs) when used at a concentration of 20 μM via inhibition of VEGFR2 and Akt phosphorylation. Ganglioside GM3 induces dissociation of the insulin receptor-caveolin-1 complex from lipid microdomains, functioning as an inhibitor of insulin signaling and contributing to insulin resistance in adipocytes. Ganglioside GM3 mixture contains ganglioside GM3 molecular species with C18:1 and C20:1 fatty acyl chains.

CAY10503 is a proapoptotic, antiproliferative compound that is able to arrest cell cycle progression in the G0-G1 phase. CAY10503 inhibits the growth of HL60, multidrug resistant HL60R, and K562 cells with IC50 values of 7.0, 23, and 20 μM, respectively. Accumulation of HL60 cells in G0-G1 occurred within eight hours following treatment with 50 μM CAY10503, whereas 10 μM CAY10503 required 96 hours for cell cycle arrest to appear. CAY10503 also induces differentiation of HL60 cells into the following positive cells: CD14 (monocytic marker) as well as CD11b and CD11c (granulocytic markers). Approximately 60% of HL60 cells exposed to 10 μM CAY10503 expressed these markers within 72 hours.