Apoptosis Inducer

WK88-1 is an apoptosis inducer and Hsp90 client protein inhibitor with antiproliferative and immunomodulatory activities. WK88-1 inhibits signaling pathways such as PI3K/Akt and NF-κB, and induces mitochondrial dysfunction and cell cycle arrest. WK88-1 effectively suppresses cancer cell migration and invasion, and reverses various EGFR mutations and resistance to Gefitinib (HY-50895). WK88-1 also regulates the differentiation of monocytes and dendritic cells, blocks the expression of multiple chemokines, inhibits immune cell migration and M1 marker transcription, and restores impaired endocytic activity. WK88-1 has been used in studies of breast cancer, non-small cell lung cancer with various EGFR mutations or Met amplification, and atherosclerosis and other related diseases.

(-)-Alkannin, found in Alkanna tinctoria, is used as a food coloring. (-)-Alkannin shows anticancer activity, arrests cell cycle, and induces apoptosis. (-)-Alkannin improves hepatic inflammation in a Rho-kinase pathway.

MKC-1 (Standard) is the analytical standard of MKC-1. This product is intended for research and analytical applications. MKC-1 (Ro-31-7453) is an orally active and potent cell cycle inhibitor with broad antitumor activity. MKC-1 inhibits the Akt/mTOR pathway. MKC-1 arrests cellular mitosis and induces cell apoptosis by binding to a number of different cellular proteins including tubulin and members of the importin β family.

Isovalerylcarnitine chloride (Standard) is the analytical standard of Isovalerylcarnitine chloride (HY-145542). This product is intended for research and analytical applications. Isovalerylcarnitine chloride is a metabolite of leucine. Isovalerylcarnitine can specifically activate calpain in human neutrophils. Isovalerylcarnitine chloride inhibits tumor cell proliferation and induces apoptosis. Elevated circulating levels of Isovalerylcarnitine chloride are negatively correlated with reduced lung cancer risk.

ENMD-2076 (Standard) is the analytical standard of ENMD-2076 (HY-10987A). This product is intended for research and analytical applications. ENMD-2076 is a multi-targeted K_inase inhibitor with IC₅₀s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, K_dR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively.

Torin 2 (Standard) is the analytical standard of Torin 2 (HY-13002). This product is intended for research and analytical applications. Torin 2 is an mTOR inhibitor with EC₅₀ of 0.25 nM for inhibiting cellular mTOR activity, and exhibits 800-fold selectivity over PI3K (EC₅₀: 200 nM). Torin 2 also inhibits DNA-PK with an IC₅₀ of 0.5 nM in the cell free assay. Torin 2 can suppress both mTORC1 and mTORC2.

Irbesartan-d₇ hydrochloride is deuterated labeled Irbesartan hydrochloride (HY-B0202A). Irbesartan (SR-47436) hydrochloride is an orally active Ang II type 1 (AT1) receptor blocker (ARB). Irbesartan hydrochloride can relax the blood vessels, low blood pressure and increase the supply of blood and oxygen to the heart. Irbesartan hydrochloride can be used for the research of high blood pressure, heart failure, and diabetic kidney disease.

Sildenafil (Standard) is the analytical standard of Sildenafil. This product is intended for research and analytical applications. Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

Oxidopamine hydrochloride (Standard) is the analytical standard of Oxidopamine hydrochloride (HY-B1081). This product is intended for research and analytical applications. Oxidopamine (6-OHDA) hydrochloride is an antagonist of the neurotransmitter dopamine. Oxidopamine hydrochloride is a widely used neurotoxin and selectively destroys dopaminergic neurons. Oxidopamine hydrochloride promotes COX-2 activation, leading to PGE₂ synthesis and pro-inflammatory cytoK_ine IL-1β secretion. Oxidopamine hydrochloride can be used for the research of ParK_inson’s disease (PD), attention-deficit hyperactivity disorder (ADHD), and Lesch-Nyhan syndrome.

Melflufen hydrochloride (Standard) is the analytical standard of Melflufen hydrochloride (HY-105019A). This product is intended for research and analytical applications. Melflufen (Melphalan flufenamide) hydrochloride, a dipeptide proagent of Melphalan, is an alkylating agent. Melflufen hydrochloride shows antitumor activity against multiple myeloma (MM) cells and inhibits angiogenesis. Melflufen hydrochloride induces irreversible DNA damage and cytotoxicity in MM cells.

Pralatrexate (Standard) is the analytical standard of Pralatrexate. This product is intended for research and analytical applications. Pralatrexate is an antifolate and is a potent dihydrofolate reductasean (DHFR) inhibitor with a Ki of 13.4 pM. Pralatrexate is a substrate for folylpolyglutamate synthetase with improved cellular uptake and retention. Pralatrexate has antitumor activities and has the potential for relapsed/refractory T-cell lymphoma treatment. Pralatrexate is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

PB28 dihydrochloride (Standard) is the analytical standard of PB28 (dihydrochloride) (HY-108511). This product is intended for research and analytical applications. PB28 dihydrochloride, a cyclohexylpiperazine derivative, is a high affinity and selective sigma 2 (σ2) receptor agonist with a K_i of 0.68 nM. PB28 dihydrochloride is also a σ1 antagonist with a K_i of 0.38 nM. PB28 dihydrochloride is less affinity for other receptors. PB28 dihydrochloride inhibits electrically evoked twitch in guinea pig bladder and ileum with EC₅₀ values of 2.62 μM and 3.96 μM, respectively. PB28 dihydrochloride can modulate SARS-CoV-2-human protein-protein interaction. PB28 dihydrochloride induces caspase-independent apoptosis and has antitumor activity.

Zoledronic acid-d₅ is deuterated labeled Zoledronic Acid (HY-13777). Zoledronic Acid (Zoledronate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic Acid inhibits the differentiation and apoptosis of osteoclasts. Zoledronic Acid also has anti-cancer effects.

PIK-C98 is a potent and selective PI3K inhibitor, with IC₅₀s of 0.59, 1.64, 3.65, and 0.74 μM for α, β, δ, and γ isoforms, respectively. PIK-C98 inhibits all class I PI3Ks but has no effects on AKT or mTOR activity. PIK-C98 interferes with the ATP-binding pockets of PI3Ks by forming H-bonds and arene-H interactions with specific amino acid residues. PIK-C98 induces apoptosis by inhibiting PI3K. PIK-C98 can be used for the research of multiple myeloma.

Galloflavin potassium is a novel lactate dehydrogenase inhibitor that can be used for the research of cancer. Galloflavin inhibits aerobic glycolysis in PLC/PRF/5 cells and triggers cell death via apoptosis.

Mps-BAY2a (Standard) is the analytical standard of Mps-BAY2a (HY-110242). This product is intended for research and analytical applications. Mps-BAY2a is a monopolar spindle 1 (MPS1) inhibitor with an IC₅₀ of 1 nM against human MPS1. Mps-BAY2a induces mitotic aberrations and apoptosis in cancer cells.

ABT-737 (Standard) is the analytical standard of ABT-737 (HY-50907). This product is intended for research and analytical applications. ABT-737, a BH3 mimetic, is a potent Bcl-2, Bcl-x_L and Bcl-w inhibitor with EC₅₀s of 30.3 nM, 78.7 nM, and 197.8 nM, respectively. ABT-737 induces the disruption of the BCL-2/BAX complex and BAK-dependent but BIM-independent activation of the intrinsic apoptotic pathway. ABT-737 induces autophagy and has the potential for acute myeloid leukemia (AML) research.

Mitoxantrone-d₈ (hydrochloride) (Mitozantrone-d₈ (hydrochloride)) is deuterium labeled Mitoxantrone (dihydrochloride). Mitoxantrone dihydrochloride is a potent topoisomerase II inhibitor. Mitoxantrone dihydrochloride also inhibits protein kinase C (PKC) activity with an IC₅₀ of 8.5 μM. Mitoxantrone dihydrochloride induces apoptosis of B-CLL (B-chronic lymphocytic leukaemia) cells. Mitoxantrone dihydrochloride shows antitumor activity. Mitoxantrone dihydrochloride also has anti-orthopoxvirus activity with EC₅₀s of 0.25 μM and and 0.8 μM for cowpox and monkeypox, respectively.

Estramustine (Standard) is the analytical standard of Estramustine. This product is intended for research and analytical applications. Estramustine is an antineoplastic agent. Estramustine depolymerizes microtnbules by binding to tubulin 1, exhibits antimitotic activity with an IC50 value of ~16 μM for mitosis of DU 145 cells. Estramustine blocks cells at mitosis in prostate tumor xenografts.

trans-Chalcone (Standard) is the analytical standard of trans-Chalcone (HY-Y0598). This product is intended for research and analytical applications. trans-Chalcone, isolated from Aronia melanocarpa skin, is a biphenolic core structure of flavonoids precursor. trans-Chalcone is a potent fatty acid synthase (FAS) and α-amylase inhibitor. trans-Chalcone causes cellcycle arrest and induces apoptosis in the breastcancer cell line MCF-7. trans-Chalcone has antifungal and anticancer activity.