Apoptosis Activator

Didesmethylrocaglamide, a derivative of Rocaglamide, is a potent eukaryotic initiation factor 4A (eIF4A) inhibitor. Didesmethylrocaglamide has potent growth-inhibitory activity with an IC₅₀ of 5 nM. Didesmethylrocaglamide suppresses multiple growth-promoting signaling pathways and induces apoptosis in tumor cells. Antitumor activity.

Lariciresinol is an orally active ingredient. Lariciresinol can be isolated from Arabidopsis thaliana. Lariciresinol inhibits α-glucosidase activity (IC₅₀ of 6.97 μM; K_i of 0.046 μM). Lariciresinol dereases Bcl-2, upregulates Bax and induces Apoptosis. Lariciresinol regulates TGF-β and NF-κB pathways. Lariciresinol has antitumor activity against liver cancer, gastric cancer, and breast cancer. Lariciresinol shows antifungal activity and anti-diabetic activity.

Uridine 5'-monophosphate-¹³C₉,¹⁵N₂ disodium is the ¹³C and ¹⁵N labeled Uridine 5'-monophosphate disodium salt (HY-W013175). Uridine 5'-monophosphate (5'-Uridylic acid) disodium salt is an orally active mitochondrial ATP-dependent potassium channel activator that has a protective effect on the heart. Uridine 5'-monophosphate disodium salt can promote the synthesis of CDP-choline and induce apoptosis in intestinal epithelial cells, which is beneficial for gut development and reduces diarrhea.

Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .

3-Methylxanthine is a blood-brain barrier-permeable cyclic GMP phosphodiesterase inhibitor, with an IC₅₀ of 920 μM against guinea pig cyclic GMP phosphodiesterase. 3-Methylxanthine relaxes the spontaneous tension of isolated guinea pig tracheal smooth muscle preparations. Through a DRD1-dependent pathway, 3-Methylxanthine upregulates the expression of γH2AX and activated caspase-3, downregulates the expression of Bcl-2, and enhances Cisplatin-induced apoptosis (apoptosis) in ovarian cancer cells both in vitro and in vivo. 3-Methylxanthine induces clonic convulsions in the central nervous system. 3-Methylxanthine is the major metabolite of Theophylline (HY-B0809). 3-Methylxanthine can be used in studies related to ovarian cancer and neurotoxic convulsions.

HG-7-85-01 is a type II ATP competitive inhibitor of wild-type and gatekeeper mutations forms of Bcr-Abl, PDGFRα, Kit, and Src kinases. HG-7-85-01 inhibits T315I mutant Bcr-Abl kinase, KDR and RET with IC₅₀s of 3 nM, 20 nM and 30 nM, and is only weak or no inhibition of other kinases (IC₅₀>2 μM). HG-7-85-01 inhibits the cell proliferation, which is mediated by the induction of apoptosis, and inhibition of cell-cycle progression.

LQZ-7F, a survivin dimerization inhibitor, induces spontaneous apoptosis and synergizes with Docetaxel in prostate cancer cells. LQZ-7F dose-dependently inhibits survival of both PC-3 and C4-2 cells with IC₅₀s of 2.99 and 2.47 µM, respectively.

TL4-12 is a selective MAP4K2/GCK inhibitor, dose-dependently downregulates IKZF1 and BCL-6 and leads to MM cell proliferation inhibition (IC₅₀=37 nM) accompanied by induction of apoptosis. TL4-12 can be used to overcome immunomodulatory agent resistance in multiple myeloma (MM).

MT 63-78 is a specific and potent direct AMPK activator with an EC₅₀ of 25 μM. MT 63–78 also induces cell mitotic arrest and apoptosis. MT 63-78 blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. MT 63-78 has antitumor effects.

PMV6-PEG4-BI2536 is an RIPTAC-like bifunctional molecule that promotes the formation of the p53^Y220C-PLK1 ternary complex (EC₅₀ = 1.4 μM). PMV6-PEG4-BI2536 causes PLK1 mislocalization and inhibits PLK1 activity, inducing G2/M phase arrest and apoptosis in p53^Y220C-mutant cells, while sparing cells with wild-type TP53. PMV6-PEG4-BI2536 can be used in research on uterine, gastric, pancreatic, prostate, and breast cancers harboring the p53^Y220C mutation. PMV6-PEG4-BI2536 is composed of PMV6 (a p53^Y220C mutant-binding ligand), PEG4 (a linker), and BI2536 (HY-159493) (a PLK inhibitor).

Bufarenogin induces intrinsic apoptosis via Bax and ANT cooperation.

Flubendiamide (NNI-0001) is an orally active phthalic diamide insecticide that acts by targeting insect ryanodine receptors (RyRs), causing insect muscle dysfunction, paralysis and death. Flubendiamide disrupts molting, metamorphosis and reproductive processes, induces oxidative stress by increasing the levels of ROS/RNS, MDA and 8OHdG and decreasing the levels of SOD, CAT and GST, activates the CncC/Maf apoptosis pathway, impairs calcium homeostasis, promotes adipogenesis, increases triglyceride accumulation, and upregulates the expression of regulatory factors for adipocyte differentiation and adipogenesis.

Benzarone is an oral inhibitor of human urate transporter 1 (hURAT1) with an IC₅₀ value of 2.8 μM, and it also acts as an uncoupler of oxidative phosphorylation. Benzarone can cause liver damage and promote cell apoptosis and necrosis. Benzarone can be used to lower serum uric acid levels and for research in vascular diseases.

CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 1 nM and a selectivity index (SI; COX-1 IC₅₀/COX-2 IC₅₀) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities.

ICCB280 is a potent inducer of C/EBPα. ICCB280 exhibits anti-leukemic properties including terminal differentiation, proliferation arrest, and apoptosis through activation of C/EBPα and affecting its downstream targets (such as C/EBPε, G-CSFR and c-Myc).

4-Methyldaphnetin is a precursor in the synthesis of derivatives of 4-methyl coumarin. 4-Methyldaphnetin has potent, selective anti-proliferative and apoptosis-inducing effects on several cancer cell lines. 4-Methyldaphnetin possesses radical scavenging property and strongly inhibits membrane lipid peroxidation.

Purpurin 18, a derivative of chlorophyll and a type of dihydroporphyrin, is used to produce photosensitizers. Purpurin 18 photodynamic therapy can induce cell apoptosis and has anti-tumor activity.

Maprotiline (hydrochloride) (Standard) is the analytical standard of Maprotiline (hydrochloride). Maprotiline (hydrochloride) (Standard) is a highly selective noradrenergic reuptake inhibitor that has strong antidepressant, antitumor and neuropathic pain-relieving effects. Maprotiline (hydrochloride) (Standard) induces cancer cell apoptosis by targeting the ERK signaling pathway and CRABP1.

JNJ-16241199 (R306465) is an orally active, selectivehydroxamate-based histone deacetylase (HDAC) inhibitor, with theIC₅₀of 3.3 nM and 23 nM for HDAC1and HDAC8, respectively.JNJ-16241199induces histone 3 acetylation and strongly increases the expression of p21^waf1, ^cip1 in A2780 ovarian carcinoma cells.JNJ-16241199 inducescell apoptosisand shows anticancer activityin a broad spectrum of human malignancies. JNJ-16241199 can be used for cancer study.

3-Methylxanthine (Standard) is the analytical standard of 3-Methylxanthine. This product is intended for research and analytical applications. 3-Methylxanthine is a blood-brain barrier-permeable cyclic GMP phosphodiesterase inhibitor, with an IC₅₀ of 920 μM against guinea pig cyclic GMP phosphodiesterase. 3-Methylxanthine relaxes the spontaneous tension of isolated guinea pig tracheal smooth muscle preparations. Through a DRD1-dependent pathway, 3-Methylxanthine upregulates the expression of γH2AX and activated caspase-3, downregulates the expression of Bcl-2, and enhances Cisplatin-induced apoptosis (apoptosis) in ovarian cancer cells both in vitro and in vivo. 3-Methylxanthine induces clonic convulsions in the central nervous system. 3-Methylxanthine is the major metabolite of Theophylline (HY-B0809). 3-Methylxanthine can be used in studies related to ovarian cancer and neurotoxic convulsions.