Apoptosis Inducer

Diuvaretin is an antimalarial agent and a C-phenylated dihydrochalcone. Diuvaretin can be isolated from the roots of U. acuminata. Diuvaretin increases the activity of Caspase-3 and triggers Apoptosis. Diuvaretin exhibits antiparasitic activity against Plasmodium falciparum. Diuvaretin can be used in the research of promyelocytic leukemia and malaria.

Linichlorin A is a p27^Kip1 ubiquitination inhibitor that blocks p27^Kip1 degradation by inhibiting the Skp2-Cks1–p27^Kip1 interaction. Linichlorin A shows selective antiproliferative activity against tumor cells. Linichlorin A induces apoptosis in leukemia cells via cytochrome c release, caspase activation and PARP cleavage. Linichlorin A can be used in the study of leukemia, melanoma, cervical cancer and breast cancer.

Emavusertib tosylate (CA-4948 tosylate) is the tosylate salt form of Emavusertib (HY-135317). Emavusertib tosylate is an orally active inhibitor for IRAK4 (IC₅₀=57 nM) and FLT3. Emavusertib tosylate 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 tosylate exhibits antitumor activity in mouse model.

Thalidomide-O-amido-C4-NH2 TFA (Standard) is the analytical standard of Thalidomide-O-amido-C4-NH2 TFA (HY-103613). This product is intended for research and analytical applications. Thalidomide-O-amido-C4-NH2 TFA (Cereblon Ligand-Linker Conjugates 6 TFA) is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology.

Phenformin (Phenethylbiguanide) (Standard) is the analytical standard of Phenformin (HY-16397). This product is intended for research and analytical applications. Phenformin (Phenethylbiguanide) is an orally active biguanide hypoglycemic agent. Phenformin inhibits mitochondrial respiratory chain complex I, leading to an increased AMP/ATP ratio, activation of AMPK, and subsequent inhibition of the mTOR pathway, thereby suppressing cell proliferation, inducing apoptosis and autophagy. Phenformin inhibits cancer stem cells (CSCs) and possesses potent antitumor potential.

Methotrexate disodium (Standard) (Amethopterin disodium (Standard); CL14377 disodium (Standard); WR19039 disodium (Standard)) is the analytical standard of Methotrexate disodium (HY-14519A). This product is intended for research and analytical applications. Methotrexate disodium (Amethopterin disodium; CL14377 disodium; WR19039 disodium) is an orally active antifolate (Antifolate). Methotrexate disodium inhibits dihydrofolate reductase (DHFR), blocks tetrahydrofolate production, suppresses purine/pyrimidine synthesis and transmethylation, and causes intracellular accumulation of AICAR. Methotrexate disodium promotes extracellular adenosine release, regulates the cytokine network, and inhibits the alarmin function of HMGB1. Methotrexate disodium induces apoptosis and cytotoxicity, upregulates the expression of iNOS and COX-2, suppresses hippocampal neurogenesis, and induces pulmonary fibrosis. Methotrexate disodium is used in the research of various immune and inflammation-related diseases such as arthritis, psoriasis, systemic lupus erythematosus, as well as pulmonary fibrosis and breast cancer.

Kinetin riboside (Standard) is the analytical standard of Kinetin riboside. This product is intended for research and analytical applications. Kinetin riboside, a cytokinin analog, can induce apoptosis in cancer cells. It inhibits the proliferation of HCT-15 cells with an IC50 of 2.5 μM.

Isoliensinine is a bisbenzylisoquinoline alkaloid extracted from the seed embryo of Nelumbo nucifera, with anti-oxidant and anti-inflammatory and anti-cancer activities. Isoliensinine induces apoptosis in triple-negative human breast cancer cells.

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).