Apoptosis Inducer

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.

Flunisolide (Standard) is the analytical standard of Flunisolide. This product is intended for research and analytical applications. Flunisolide is a corticosteroid, which is an orally active glucocorticoid receptor activator with anti-inflammatory activity. Flunisolide can induce eosinophil apoptosis, and is used for the research of asthma or rhinitis, and inflammation.

Cyflumetofen (Standard) is the analytical standard of Cyflumetofen (HY-W663938). This product is intended for research and analytical applications. Cyflumetofen is a non-systemic acylacetonitrile Acaricide. Cyflumetofen interferes with the Wnt/β-catenin signaling pathway, induces Apoptosis, and reduces the level of tight junction proteins. Cyflumetofen upregulates the expression of Pink1, Parkin and Lrrk2 genes associated with the pathogenesis of Parkinson's disease in zebrafish larvae. Cyflumetofen induces developmental toxicity and oxidative stress in zebrafish larvae, damages neurons, reduces motor activity, alters brain tissue structure, and disrupts blood-brain barrier structure. Cyflumetofen exhibits acaricidal activity against spider mites. Cyflumetofen can be used in studies related to Parkinson's disease and infestations by spider mites (Tetranychus urticae, Tetranychus kanzawai, Panonychus citri).

Etretinate (Standard) is the analytical standard of Etretinate. This product is intended for research and analytical applications.

Fluoxastrobin is a fungicide. By binding to NAD-dependent epimerase/dehydratase, Fluoxastrobin interferes with electron transport, reduces ATP production and inhibits mycelial growth, thereby effectively controlling foliar diseases of tea plants. Fluoxastrobin induces oxidative stress by increasing ROS levels and lipid peroxidation, causes DNA damage and promotes apoptosis; meanwhile, it shows high acute toxicity to Danio rerio embryos and larvae. Fluoxastrobin can be used in research related to tea foliar diseases (including tea red leaf spot and tea gray leaf spot).

Estradiol cypionate (Standard) is the analytical standard of Estradiol cypionate. This product is intended for research and analytical applications. Estradiol cypionate is the 17β-cypionate ester of Estradiol, which inhibits ET-1 synthesis by acting on estrogen receptors.

Lenalidomide-d₄ (CC-5013-d₄) is the d₄-labeled Lenalidomide (HY-A0003). Lenalidomide (CC-5013) is an orally active immunomodulatory agent that binds CRBN as a molecular glue to alter substrate specificity, inducing ubiquitination and proteasome-dependent degradation of IKZF1, IKZF3 and CK1α. Lenalidomide induces apoptosis by degrading IKZF1/3, and activates p53 by degrading CK1α. Lenalidomide promotes IL-2 release and effector functions of CD8⁺ T/NK cells, while inhibiting TNF-α secretion and M1-type pyroptosis. Lenalidomide can be used in research related to hematological malignancies, acute liver failure and acute kidney injury.

(±)-Enitociclib (Standard) is the analytical standard of (±)-Enitociclib (HY-103019A). This product is intended for research and analytical applications. (±)-Enitociclib ((±)-BAY-1251152) is the racemic mixture of Enitociclib (HY-103019E). Enitociclib is a selective CDK9 inhibitor and apoptosis inducer. Enitociclib inhibits CDK9 activity and reduces the phosphorylation of Ser2 in the carboxyl-terminal domain (CTD) of RNA polymerase Pol II, thereby downregulating the transcription of key oncogenes such as MYC and MCL1. Enitociclib has anti-proliferative activity targeting MYC+ lymphoma and multiple myeloma (MM) cells, and has synergistic effects with Bortezomib (HY-10227) and Lenalidomide (HY-A0003), and can be used in the research of hematological malignancies.

Cladribine-¹⁵N (2-Chloro-2′-deoxyadenosine-¹⁵N) is ¹⁵N labeled Cladribine. Cladribine (2-Chloro-2′-deoxyadenosine), a purine nucleoside analog, is an orally active adenosine deaminase inhibitor. Cladribine functions as an inhibitor of DNA synthesis to block the repair of the damaged DNA. Cladribine can inhibit DNA methylation. Cladribine has anti-lymphoma activity. Cladribine can be used for the research of several hematologic malignancies and multiple sclerosis.

Decitabine methanesulfonate (5-Aza-2'-deoxycytidine methanesulfonate) is an orally active Deoxycytidine analogue antimetabolite and DNA methyltransferase inhibitor. Decitabine methanesulfonate incorporates into DNA in place of cytosine can covalently trap DNA methyltransferase to DNA causing irreversible inhibition of the enzyme. Decitabine methanesulfonate induces cell G2/M arrest and cell Apoptosis. Decitabine has potent anticancer activity.

DW532 is a dual inhibitor of tubulin and tyrosine kinase, with IC₅₀ values of 4.9 μM and 5.5 μM against EGFR and VEGFR2, respectively, and a K_D of 3.6 μM for tubulin. DW532 induces cell cycle arrest at the G₂/M phase, triggers cell apoptosis via caspase-related pathways, and inhibits angiogenesis. DW532 can be used for research related to cancers (e.g., breast cancer).

Ro-3306 (Standard) is the analytical standard of Ro-3306 (HY-12529). This product is intended for research and analytical applications. Ro-3306 is a potent and selective inhibitor of CDK1, with K_is of 20 nM, 35 nM and 340 nM for CDK1, CDK1/cyclin B1 and CDK2/cyclin E, respectively.

Acanthoic acid (NP1302) is an orally active pimarane-type diterpenoid. Acanthoic acid is isolated from the root bark of Araliaceae family plant Eleutherococcus senticosus (Siberian ginseng). Acanthoic acid activates LXR and FXR. Acanthoic acid activates the AMPK-LKB1, SIRT1, and p38 MAPK signaling pathways and increases the phosphorylation level of ACC. Acanthoic acid downregulates the expression of SREBP-1, CYP2E1, HIF-1α, and PPARγ, and upregulates the expression of PPARα. Acanthoic acid induces Apoptosis by activating Caspase-3, promoting PARP cleavage, and downregulating Bcl-xL. Acanthoic acid exhibits antioxidant, anti-fibrotic, and hepatoprotective effects. It reduces lipid accumulation and lipogenesis. Acanthoic acid is used in studies on non-alcoholic fatty liver disease, alcoholic liver disease, acute promyelocytic leukemia, and Acetaminophen-induced hepatotoxicity.