Apoptosis Inducer

Cranberry Extract is the extract of Cranberry, with content of 25% -50% Proanthocyanidins. Cranberry Extract exhibits anti-virus and antimicrbiol activity. Cranberry Extract suppresses fungal growth and biofilm formation. Cranberry Extract reduces NF-κB p65 phosphorylation, and PI3K/AKT signaling; increases caspase-8/9 activity to induce apoptosis, modulates oxidative stress, inflammation, and lipid profiles. Cranberry Extract exerts antiproliferative effects and induces cell cycle arrest. Cranberry Extract can be used for the research of infection and cancers.

Acyclovir (Aciclovir) hydrochloride is a potent, orally active antiviral agent. Acyclovir hydrochloride has antiherpetic activity with IC₅₀ values of 0.85 μM and 0.86 μM for HSV-1 and HSV-2, respectively. Acyclovir hydrochloride induces cell cycle perturbation and apoptosis. Acyclovir hydrochloride prevents bacterial infections during induction therapy for acute leukaemia.

Neridronate (Standard) is the analytical standard of Neridronate (HY-119443). This product is intended for research and analytical applications. Neridronate is a bisphosphonate. Bisphosphonates initiate the Apoptotic process. Neridronate sodium reduces the levels of bone resorption, bone turnover markers, the degree of back pain, and the risk of fractures. Neridronate inhibits capillary tube formation. Neridronate itself has weak anticancer activity, but liposomal encapsulation enhances this activity. Neridronate can be used in research related to demineralizing metabolic bone diseases, thalassemia-associated osteoporosis, chronic inflammatory diseases, cancer, and osteogenesis imperfecta.

ISRIB (trans-isomer) (Standard) is the analytical standard of ISRIB (trans-isomer) (HY-12495). This product is intended for research and analytical applications. ISRIB (trans-isomer) is a potent inhibitor of PERK with an IC₅₀ of 5 nM. ISRIB potently reverses the effects of eIF2α phosphorylation (IC₅₀=5 nM).

Alexidine (dihydrochloride) (Standard) is the analytical standard of Alexidine (dihydrochloride). This product is intended for research and analytical applications. Alexidine dihydrochloride is an anticancer agent that targets a mitochondrial tyrosine phosphatase, PTPMT1, in mammalian cells and causes mitochondrial apoptosis. Alexidine dihydrochloride has antifungal and antibiofilm activity against a diverse range of fungal pathogens.

Schisandronic acid is a triterpenoid antioxidant and anticancer agent extracted from Schisandra chinensis, which has potent cytotoxicity against human breast cancer cells, especially MCF-7. Schisandronic acid induces apoptosis and reduces cell viability in a time-dependent manner (MCF-7, IC50=8.06 μM). Schisandronic acid can upregulate active caspase-3 expression and cleave PARP, reduce the generation of reactive oxygen species and exhibit antioxidant effects.

Emavusertib maleate (CA-4948 maleate) is the maleate salt form of Emavusertib (HY-135317). Emavusertib maleate is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib maleate inhibits NF-κB and MyD88 signaling pathways, reduces the generation of pro-inflammatory cytokines like IL-6 and IL-10, thereby exhibiting anti-inflammatory and anti-proliferative activities against cancer cells, leading to cell apoptosis. Emavusertib maleate exhibits antitumor activity in mouse model.

TAK-243 (Standard) is the analytical standard of TAK-243 (HY-100487). This product is intended for research and analytical applications. TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.

Tizanidine (Standard) is the analytical standard of Tizanidine (HY-B0194). This product is intended for research and analytical applications. Tizanidine, a skeletal muscle relaxant, is an orally effective central α₂-adrenoceptor agonist (IC₅₀ = 6.9 nmol). Tizanidine primarily exerts muscle relaxation effects by inhibiting the release of excitatory amino acids (glutamate and aspartate) from the presynaptic terminals of spinal cord interneurons. Tizanidine has anti-injury activity and can inhibit gastrointestinal (GI) transport. Tizanidine can inhibit the proliferation, migration, and invasion of lung cancer cells and induce cell apoptosis by upregulating Nischarin and inhibiting the AKT and Wnt3a/β-catenin signaling pathways. Tizanidine can be used to treat spasticity caused by diseases such as multiple sclerosis (MS), stroke, and spinal cord injury (SCI).

Tabersonine hydrochloride is a selective, orally active NLRP3 inhibitor. Tabersonine hydrochloride directly binds to the NACHT domain of NLRP3, inhibiting its ATPase activity and oligomerization, thereby blocking ASC spot formation and caspase-1 activation, and reducing the release of pro-inflammatory cytokines such as IL-1β. Tabersonine hydrochloride also inhibits K63-linked ubiquitination of TRAF6, blocking NF-κB, PI3K/Akt, and p38 MAPK signaling pathways. Tabersonine hydrochloride can inhibit inflammatory responses, induce apoptosis of liver cancer cells through mitochondrial pathways and death receptor pathways, reduce mitochondrial membrane potential, promote cytochrome c release, and activate caspase proteins. Tabersonine hydrochloride is mainly used in the study of NLRP3-driven inflammatory diseases (such as acute lung injury, sepsis, peritonitis) and tumors such as liver cancer.

MK-2206 (Standard) is the analytical standard of MK-2206 (HY-108232). This product is intended for research and analytical applications. MK-2206 is an orally active, highly potent and selective allosteric Akt inhibitor, with IC₅₀s of 8, 12, and 65 nM for Akt1, Akt2, and Akt3, respectively. Many breast cancer cell lines, and PIK3CA-mutant and cell lines with PTEN loss are sensitive to MK-2206. MK-2206 has anticancer activities.

WT-161 (Standard) is the analytical standard of WT-161 (HY-100871). This product is intended for research and analytical applications. WT-161 is a potent and selective HDAC6 inhibitor with an IC50 of 0.40 nM. WT-161 also inhibits metallo-β-lactamase domain-containing protein 2 (MBLAC2).

Gemcitabine monophosphate (Standard) is the analytical standard of Gemcitabine monophosphate (HY-108932). This product is intended for research and analytical applications. Gemcitabine monophosphate (Gemcitabine 5′-phosphate) is one of the active intermediates of Gemcitabine (HY-17026). Gemcitabine monophosphate has a synergistic anti-cancer effect and can be delivered by formulating it into nanoparticles.

Zibotentan (Standard) is the analytical standard of Zibotentan. This product is intended for research and analytical applications. Zibotentan (ZD4054) is a potent, selective and orally active endothelin A (ETA) receptor antagonist with a Ki of 13 nM. Zibotentan has no inhibitory effect on ETB. Zibotentan has anticancer effects and can be used for castration-resistant prostate cancer (CRPC) research.

Licoflavanone (3′-Prenylnaringenin) is a flavanone with antioxidant, anti-inflammatory and anticancer activities. Licoflavanone can be isolated from the leaf extract of Glycyrrhiza glabra. Licoflavanone downregulates the mTOR/PI3K/AKT signaling pathway to inhibit the proliferation, migration and invasion of cancer cells, while activates Bax, Bad and multiple caspase enzymes to induce apoptosis. Its anti-inflammatory effect is manifested by reducing the nuclear translocation of NF-κB, decreasing the phosphorylation levels of p38, JNK and ERK1/2, thereby inhibiting the expression of nitric oxide, proinflammatory cytokines, COX-2 and iNOS. Licoflavanone is used in studies on nasopharyngeal carcinoma and related mechanisms.

Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pK_is of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer.

MK-4101 (Standard) is the analytical standard of MK-4101 (HY-100036). This product is intended for research and analytical applications. MK-4101 is a Smoothened (SMO) antagonist (IC50 of 1.1 μM for 293 cells ) and also a potent inhibitor of the hedgehog pathway (IC50 of 1.5 μM for mouse cells; IC50 of 1 μM for KYSE180 oesophageal cancer cells). MK-4101 has robust antitumor activity that inhibits tumor cell proliferation and induces extensive apoptosis.

Selumetinib (sulfate) (Standard) is the analytical standard of Selumetinib (sulfate). This product is intended for research and analytical applications. Selumetinib (AZD6244) is selective, non-ATP-competitive oral MEK1/2 inhibitor, with an IC50 of 14 nM for MEK1. Selumetinib (AZD6244) inhibits ERK1/2 phosphorylation.

SDH-IN-32 is a succinate dehydrogenase (SDH) inhibitor with an IC₅₀ of 2.74 μM. SDH-IN-32 exhibits excellent antifungal activity. SDH-IN-32 can destroy the cell membrane structure and increase the permeability of the cell membrane. SDH-IN-32 can decrease the mitochondrial membrane potential (MMP), thereby inducing cell apoptosis and inhibiting the normal growth of mycelia. SDH-IN-32 can be used for the research of infection.

Thalidomide-NH-CH2-COOH TFA is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-NH-CH2-COOH TFA can be connected to the ligand for protein by a linker to form PROTACs, such as THAL-SNS-032 (HY-123937).