Apoptosis Inducer

Tamoxifen-d₃ hydrochloride is deuterated labeled Tamoxifen (Citrate) (HY-13757). Tamoxifen Citrate (ICI 46474) is an orally active, selective estrogen receptor modulator (SERM) which blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells.Tamoxifen Citrate is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen Citrate also potent inhibits infectious EBOV Zaire and Marburg (MARV) with IC₅₀ of 0.1 μM and 1.8 μM, respectively. Tamoxifen Citrate activates autophagy and induces apoptosis.Tamoxifen Citrate also can induce gene knockout of CreER(T2) transgenic mouse.

Lactucin is an anti-inflammatory agent. Lactucin induces cancer cell apoptosis. Lactucin also shows analgesic, anticancer and antimalarial activities.

5'-O-Tritylthymidine is an inhibitor of TK-2 and inhibits angiogenesis. 5'-O-Tritylthymidine targets FAK-Mdm-2 interactions, decreasing cell viability and increasing apoptosis.

Ibuprofen-d₃ ((±)-Ibuprofen-d₃) sodium is the deuterium labeled Ibuprofen sodium (HY-78131C). Ibuprofen sodium is an orally active, selective COX-1 inhibitor with an IC₅₀ value of 13 μM. Ibuprofen sodium inhibits cell proliferation, angiogenesis, and induces cell apoptosis. Ibuprofen sodium is a nonsteroidal anti-inflammatory agent and a nitric oxide (NO) donor. Ibuprofen sodium can be used in the research of pain, swelling, inflammation, infection, immunology, cancers.

Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research.

PLK1-IN-13 is a selective and orally active PLK1 inhibitor (IC₅₀: 0.27 nM). PLK1-IN-13 also inhibits PLK2 (IC₅₀: 12.72 nM) and PLK3 (IC₅₀: 4.12 nM). PLK1-IN-13 arrests cell at G2 phase, induces apoptosis and down-regulates the transcription of the proliferation-related oncogene c-MYC. PLK1-IN-13 inhibits tumor growth, and can be used for research of acute myeloid leukemia (AML).

Groenlandicine, a protoberberine alkaloid, is a cholinesterase inhibitor (AChE (IC₅₀ = 0.54 μM), BChE (IC₅₀ = 3.32 μM)). Groenlandicine non-competitively inhibits BACE1 (IC₅₀ = 19.68 μM, K_i = 21.2) and inhibits RLAR (IC₅₀ = 140.1 μM), HRAR (IC₅₀ = 154.2 μM), and total ROS generation (IC₅₀ = 51.78 μM) in vitro. Groenlandicine suppresses osteosarcoma cell proliferation while promoting apoptosis. Groenlandicine inhibits the tumor growth when combined with Cisplatin (HY-17394). Groenlandicine can be used for the study on osteosarcoma, Alzheimer's disease and diabetes mellitus .

YJ9069 is a CDK12/CDK13 PROTAC degrader. YJ9069 induces proteasome-dependent degradation of CDK12 and CDK13, and inhibits serine 2 phosphorylation of RNA polymerase II (RNA polymerase II). YJ9069 triggers gene length-dependent transcription elongation defects, reduces the expression of DNA damage response genes, and induces DNA damage, cell cycle arrest and apoptosis. YJ9069 inhibits tumor growth in prostate cancer models. YJ9069 can be used for the research of prostate cancer, Ewing sarcoma and breast cancer.

Atractylenolide III (Standard) is the analytical standard of Atractylenolide III. This product is intended for research and analytical applications. Atractylenolide III (ICodonolactone) is the main component of Atractylodes rhizome and has the activity of inducing apoptosis in lung cancer cells. Atractylenolide III is an orally active gastroprotective agent.

Troglitazone-d₄ is deuterium labeled Troglitazone. Troglitazone is a PPARγ agonist, with EC50s of 550 nM and 780 nM for human and murine PPARγ receptor, respectively.

Protoapigenone is an antineoplastic agent isolated from ferns. Protoapigenone has significant inhibitory activity against Hep G2, Hep 3B, MCF-7, A549 and MDAMB-231, with IC₅₀s values of 1.60, 0.23, 0.78, 3.88 and 0.27 μg/mL respectively.

ERα antagonist 1 (Compound 19d) is a potent, selective, covalent estrogen receptor α (ERα) antagonist. ERα antagonist 1 induces apoptosis and cell cycle G0/G1 phase arrest in MCF-7 cells.

PRMT7-IN-2 (A33) is a selective PRMT7 inhibitor with an IC₅₀ of 0.50 μM. PRMT7-IN-2 arrests cell cycle at G0/G1 phase, induces cell apoptosis, and inhibits cell growth in vivo and in vitro. PRMT7-IN-2 decreases the monomethylarginine level of PRMT7, increases expression of epithelial marker (E-cadherin, and reduces expression of mesenchymal markers such as N-cadherin, Vimentin, and ZEB2.

Arctigenin (Standard) is the analytical standard of Arctigenin. This product is intended for research and analytical applications. Arctigenin ((-)-Arctigenin), a biologically active lignan, can be used as an antitumor agent. Arctigenin exhibits potent antioxidant, anti-inflammatory and antiviral (influenza A virus) activities. Arctigenin can be used for the research of metabolic disorders, and central nervous system dysfunctions.

Thiamine-d₃ (hydrochloride) is the deuterium labeled Thiamine hydrochloride. Thiamine hydrochloride (Thiamine chloride hydrochloride) is an essential micronutrient needed as a cofactor for many central metabolic enzymes.

Asparanin A is an apoptosis inducer with anticancer activity. Asparanin A induces cell cycle arrest in the G0/G1 phase through mitochondria and PI3K/AKT signaling pathways, inhibiting cancer cell growth. Asparanin A also demonstrated in vivo efficacy in a mouse xenograft model of Ishikawa endometrial carcinoma, significantly inhibiting tumor growth.

KSRP-IN-1 (compound 8) is a KSRP inhibitor that induces Apoptosis and cell cycle arrest. KSRP-IN-1 has antitumor activity.

KH16 is a potent and low nanomolar HDAC inhibitor. KH16 is against class I HDACs HDAC1, HDAC2, and HDAC3, with IC₅₀ values ranging from 6 to 34 nM. KH16 induces cell apoptosis and is against tumor cells with various gene expression patterns.