Apoptosis Inducer

Rasagiline (mesylate) (Standard) is the analytical standard of Rasagiline (mesylate). This product is intended for research and analytical applications. Rasagiline (R-AGN1135) mesylate is a highly potent selective irreversible mitochondrial monoamine oxidase (MAO) inhibitor with IC₅₀s of 4.43?nM and 412?nM for rat brain MAO B and A activity, respectively. Rasagiline (mesylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

Sampangine is an alkaloid that induces apoptosis by inducing cell cycle arrest in the G0/G1 phase. Sampangine can inhibit the biosynthesis of heme.

Flonoltinib maleate is a potent and orally active dual JAK2/FLT3 inhibitor with IC₅₀ values of 0.7 nM, 4 nM, 26 nM and 39 nM for JAK2, FLT3, JAK1 and JAK3, respectively. JAK2/FLT3-IN-1 has anti-cancer activity.

Pomalidomide-¹³C₅ (CC-4047-¹³C₅) is ¹³C labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.

Amsacrine lactate (m-AMSA lactate) is a Topoisomerase II inhibitor. Amsacrine lactate intercalates into DNA. Amsacrine lactate induces Ca²⁺-mediated inactivation of ERK, and also downregulates AKT, promoting MCL1 downregulation mediated by GSK3β via reducing the phosphorylation level of GSK3β. Amsacrine lactate induces Apoptosis by activating Caspase-9 and Caspase-3. Amsacrine lactate blocks HERG potassium channels in the open/inactivated state. Amsacrine lactate induces chromosomal aberrations and sister chromatid exchanges, and inhibits the synthesis of RNA and DNA. Amsacrine lactate exhibits anti-leukemic activity. Amsacrine lactate causes cardiac repolarization disorders, QT interval prolongation, ventricular arrhythmias, and increases the risk of sudden cardiac death. Amsacrine lactate can be used in research related to acute myeloid leukemia, lymphoma and progressive malignancies.

CP-724714 succinate is an orally active and selective HER2 tyrosine kinase inhibitor with an IC₅₀ of 10 nM. CP-724714 succinate inhibits HER2 receptor autophosphorylation and blocks the downstream Ras-Raf-Mek-Erk signaling pathway, thereby inducing cell cycle arrest and apoptosis in tumor cells. CP-724714 succinate exhibits antiviral activity and inhibits various porcine diarrheal coronaviruses, including SADS-CoV (IC₅₀ of 0.91 μM). CP-724714 succinate is an inhibitor of the hepatic transport receptors OATP1B1/MDR1/BSEP, and can enter hepatocytes via active uptake and trigger the accumulation of drugs and bile acids within hepatocytes. CP-724714 succinate can be used in research related to HER2-overexpressing breast cancer and porcine diarrheal coronavirus infection.

m-3M3FBS (Standard) is the analytical standard of m-3M3FBS. This product is intended for research and analytical applications. m-3M3FBS is a potent phospholipase C (PLC) activator. m-3M3FBS stimulates superoxide generation in human neutrophils, upregulates intracellular calcium concentration, and stimulates inositol phosphate generation in various cell lines. m-3M3FBS induces monocytic leukemia cell apoptosis.

1-Adamantylphosphaethyne (1-(2-Phosphaethynyl)adamantane) is a compound with potential biological activity and can be used as a catalyst in organic synthesis. 1-Adamantylphosphaethyne has shown the ability to induce cell apoptosis in compound development, which helps in anti-tumor inhibition. 1-Adamantylphosphaethyne can also be used as an efficient reaction intermediate to promote the progress of various chemical reactions.

KW-2449 (Standard) is the analytical standard of KW-2449 (HY-10339). This product is intended for research and analytical applications. KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC₅₀s of 6.6, 14, 4 and 48 nM, respectively.

Prednisone-d₇ (Dehydrocortisone-d₇) is deuterium labeled Prednisone. Prednisone (Adasone) is a corticosteroid agent with anti-inflammatory and immunosuppressive effects that can be used to study diseases related to systemic lupus erythematosus.

BPR1J-340 is a potent FLT3 inhibitor with an IC₅₀ of ~25 nM. BPR1J-340 inhibits the phosphorylation of FLT3 and STAT5 and triggered apoptosis in FLT3-ITD⁺ acute myeloid leukemia (AML) cells. BPR1J-340 exhibits significant anti-tumor activities.

R406 (Standard) is the analytical standard of R406 (HY-12067). This product is intended for research and analytical applications. R406 is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a K_i of 30 nM, potently inhibits Syk K_inase activity in vitro with an IC₅₀ of 41 nM, measured at an ATP concentration corresponding to its K_m value. R406 reduces immune complex-mediated inflammation. R406 also inhibits Lyn (IC₅₀=63 nM) and Lck (IC₅₀=37 nM).

HS-438 is a potent and selective BCR-ABL inhibitor. HS-438 shows antiproliferative activity. HS-438 decreases the expression of phosphorylation of BCR-ABL (Tyr177). HS-438 induces apoptosis and cell cycle arrest at G0/G1 phase. HS-438 shows antitumor activity. HS-438 has the potential for the research of chronic myeloid leukemia (CML).

Eltrombopag-d₃ (SB-497115-d₃) is deuterium labeled Eltrombopag. Eltrombopag (SB-497115) is an orally active thrombopoietin receptor nonpeptide agonist. Eltrombopag owns thrombopoietic activity, and has been used to research low blood platelet counts with chronic immune thrombocytopenia. Eltrombopag can be used for the research of cardiovascular. Eltrombopag also has highly inhibitory effects against multidrug resistant Staphylococcus aureus. Eltrombopag can induce apoptosis in hepatocellular carcinomab (HCC) as well.

Endoxifen Z-isomer methanesulfonate is an orally active selective PKCβ1 inhibitor with an IC₅₀ of 360 nM against human PKCβ1. It also acts as an estrogen receptor modulator and antiestrogen. Endoxifen Z-isomer methanesulfonate binds to and blocks ERα, ERβ and PKCβ1, inhibits estrogen and PI3K/AKT/mTORC1 signaling pathways, suppresses the expression of genes associated with cell cycle, cell proliferation and extracellular matrix remodeling, and induces apoptosis, reactive oxygen species (ROS) production and hypoxic features. Endoxifen Z-isomer methanesulfonate inhibits tumor growth in breast tumor and glioblastoma models, reduces bone turnover and blood lipid levels, and does not require metabolism via CYP2D6. It can be used in research related to ER⁺ breast cancer, invasive breast cancer, glioblastoma multiforme, type I bipolar disorder, desmoid tumor, gynecological malignancies, melanoma and hormone receptor-positive solid tumors.

Imipramine-d4-1 is the deuterium labeled Imipramine (HY-W010179). Imipramine is an orally active tertiary amine tricyclic antidepressant. Imipramine is a Fascin1 inhibitor with antitumor activities. Imipramine also inhibits serotonin transporter with an IC₅₀ value of 32 nM. Imipramine stimulates U-87MG glioma cells autophagy and induces HL-60 cell apoptosis. Imipramine shows neuroprotective and immunomodulatory effects.

Mitoguazone (Standard) is the analytical standard of Mitoguazone. This product is intended for research and analytical applications. Mitoguazone (Methylglyoxal-bis(guanylhydrazone)) is a synthetic polycarbonyl derivative with potent antineoplastic activity. Mitoguazone is a brain-penetrant and competitive S-adenosyl-methionine decarboxylase (SAMDC) inhibitor that disrupts polyamine biosynthesis. Mitoguazone induces cell apoptosis. Mitoguazone inhibits HIV DNA integration into the cellular DNA in both monocytes and macrophages. Mitoguazone has the potential for acute leukemia, Hodgkin's and non-Hodgkin's lymphoma treatment.

Nimbolide (Standard) is the analytical standard of Nimbolide. This product is intended for research and analytical applications. Nimbolide is a triterpene compound that can be isolated from neem (Azadirachta indica), possesses anticancer and antiproliferative activity. Nimbolide induces tumor cell apoptosis by inhibiting NF-κB and CDK4/CDK6 kinase. Nimbolide suppresses the Wnt, PI3K-Akt, MAPK and JAK-STAT signaling pathways.

BGC638 is a thymidylate synthase inhibitor with a K_i value of 0.24 nM. BGC638 binds to α-FR with high affinity and enters cells via receptor-mediated endocytosis, thereby potently inhibiting thymidylate synthase to block DNA synthesis and ultimately induce apoptosis. BGC638 is applicable to studies related to α-FR-overexpressing tumors and epithelial carcinomas (ovarian cancer and endometrial cancer).

L-Ascorbic acid (sodium salt) (Standard) is the analytical standard of L-Ascorbic acid (sodium salt). This product is intended for research and analytical applications. L-Ascorbic acid sodium salt (Sodium ascorbate), an electron donor, is an endogenous antioxidant agent. L-Ascorbic acid sodium salt selectively inhibits Cav3.2 channels with an IC50 of 6.5 μM. L-Ascorbic acid sodium salt is also a collagen deposition enhancer and an elastogenesis inhibitor.