Apoptosis Inducer

Caspase-3 activator 5 (Compound 11) is a caspase-3 activator. Caspase-3 activator 5 reduces MRP1 levels and induces Apoptosis through Caspase-3 activation. Caspase-3 activator 5 exhibits anticancer activity against leukemia, cervical cancer, and breast cancer. Caspase-3 activator 5 shows no antibacterial or antifungal effects.

CAIX/CDK-2-IN-1 is a dual-acting inhibitor of carbonic anhydrase IX (CA IX) and cyclin-dependent kinase-2 (CDK-2) with IC₅₀ values of 0.29 μM and 0.32 μM. The zein nanoparticls of CAIX/CDK-2-IN-1 can induce cancer cells apoptosis. CAIX/CDK-2-IN-1 can be used for the research of cancer, such as lung cancer.

EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC₅₀s of 17.18 and 64.74 nM against EGFR^L858R/T790M and EGFR^WT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma.

FGFR-IN-23 (Compound 9p) is a covalent pan FGFR inhibitor with IC₅₀s of 14, 4.2, 5 and 220 nM for FGFR1, FGFR2, FGFR3 and FGFR4, respectively. FGFR-IN-23 also has potent inhibitory activity against gatekeeper mutants, such as FGFR1^V561M and FGFR3^V555M. FGFR-IN-23 suppresses the activation of FGFR-mediated signaling and induces apoptosis. FGFR-IN-23 shows significant antitumor efficacy in RT112 xenograft mouse models. FGFR-IN-23 can be used for cancers and its drug resistance research.

LVTX-8 is a peptide toxin, exacted from Lycosa vittata. LVTX-8 has potent anticancer and and anti-metastasis activities towards lung cancer with strong cytotoxicity. LVTX-8 significantly induces apoptosis and inhibits the proliferation, invasion and migration of lung cancer cells through P53 hypoxia pathways and integrin signaling. LVTX-8 significantly inhibits the tumor growth and metastasis in A549/H460 xenograft mice model.

Pycnidione is a natural small-molecule compound isolated from fungi. Pycnidione inhibits stromelysin/MMP3, targets cyclin D1/E, induces G1 phase arrest, modulates survivin, affects caspase-8/3, targets PAI-1, inhibits topoisomerases, and induces HIF-1α accumulation/nuclear translocation and DNA binding/reporter gene transactivation and erythropoietin expression. Pycnidione induces apoptosis, reactive oxygen species (ROS) generation, and mitochondrial membrane potential collapse. Pycnidione can be used for research on lung cancer.

4-tert-Octylphenol (Standard) is the analytical standard of 4-tert-Octylphenol. This product is intended for research and analytical applications. 4-tert-Octylphenol, a endocrine-disrupting chemical, is an estrogenic agent. 4-tert-Octylphenol is also a biodegradation product of non-ionic surfactants alkylphenol polyethoxylates. 4-tert-Octylphenol induces apoptosis in neuronal progenitor cells in offspring mouse brain. 4-tert-Octylphenol reduces bromodeoxyuridine (BrdU), mitotic marker Ki67, and phospho-histone H3 (p-Histone-H3), resulting in a reduction of neuronal progenitor proliferation. 4-tert-Octylphenol disrupts brain development and behavior in mice, which is promising for reserch of immune response, neuro-related diseases and ethology.

Zoledronic acid (monohydrate) (Standard) is the analytical standard of Zoledronic acid (monohydrate). This product is intended for research and analytical applications. Zoledronic acid monohydrate (Zoledronate monohydrate) is a third-generation bisphosphonate (BP), with potent anti-resorptive activity. Zoledronic acid monohydrate inhibits the differentiation and apoptosis of osteoclasts. Zoledronic acid monohydrate also has anti-cancer effects.

CDK2-IN-32 (Compound 5g) is a selective CDK2 inhibitor with an IC₅₀ of 0.21 μM. CDK2-IN-32 shows cytotoxicity against Vero cells with an IC₅₀ of 28.52 μM.

c-Met/HDAC-IN-4 is a dual inhibitor of c-Met/HDAC. The IC₅₀ value of c-Met/HDAC-IN-4 for c-Met is 28.92 nM. c-Met/HDAC-IN-4 can induce G₀/G₁ phase cell cycle arrest and apoptosis in MDA-MB-231 breast cancer cells, and it inhibits the proliferation and invasion of breast cancer cell lines.

CDK1-IN-8 is a CDK1 inhibitor. CDK1-IN-8 inhibits cell migration, induces apoptosis, and arrests the cell cycle at the G2/M phase. CDK1-IN-8 leads to a significant downregulation of CDK1 protein levels in HepG2 cells. CDK1-IN-8 can be used for the study of hepatocellular carcinoma.

Tyrosine kinase-IN-11 (Compound 4b) is a tyrosine kinase inhibitor. Tyrosine kinase-IN-11 decreases general tyrosine kinase activity, selectively inhibits PDGFR-β, SRC, and c-MET kinases. Tyrosine kinase-IN-11 induces apoptosis, accompanied by reduced ERK signalings. Tyrosine kinase-IN-11 exhibits selective anticancer activity against pancreatic cancer and renal cancer.

EGFR-IN-175 is an orally active and selective EGFR^{L858R/T790M/C797S} inhibitor with an IC₅₀ of 18.94 nM. EGFR-IN-175 can induce cell apoptosis and cause G1 phase arrest. EGFR-IN-175 can downregulate p-EGFR, p-AKT, and p-ERK expression. EGFR-IN-175 can be used for the research of cancer, such as lung cancer.

PIN1-IN-8 is a covalent inhibitor of Pin1, with IC₅₀ values of 4.19 μM and 1.54 μM against purified Pin1 and Pin1 enzymatic activity, respectively. PIN1-IN-7 exerts antiproliferative effects and induces apoptosis by downregulating c-Myc and Cyclin D1. PIN1-IN-7 can be used in the research of triple-negative breast cancer.

Schisandrin C (Standard) (Schizandrin-C (Standard)) is the analytical standard of Schisandrin C (HY-N0690). This product is intended for research and analytical applications. Schisandrin C (Schizandrin-C) is a phytochemical lignan isolated from Schizandra chinensis. Schisandrin C has diverse biological activities, including anticancer, anti-inflammatory and antioxidant effects. Schisandrin C is a molecular glue. Schisandrin C can be used for cancer, alzheimer’s disease, and liver diseases research. Schisandrin C induces cell apoptosis.

Lss-11 is a topoisomerase inhibitor. LSS-11 enhances cell death in cancer cells by inducing apoptosis through increasing the DR5 protein level and PARP1 cleavage. LSS-11 dose-dependently reduces STAT3 phosphorylation, downregulates its target genes MDR1 and MRP1, reduces P-gp protein expressionwithout affecting P-gp transport function. Lss-11 is a chemosensitizer and shows synergistic anticancer effect with Paclitaxel (HY-B0015). Lss-11 can be used for the research of paclitaxel-resistant lung cancer.

KRAS-IN-64 is a KRAS inhibitor that inhibits KRAS translation by binding to and stabilizing the G-quadruplex in the 5'-UTR of KRAS mRNA, exhibits antiproliferative activity in KRAS-mutant cancer cells, and induces cell cycle arrest, non-apoptotic cell death, and PARP cleavage-mediated apoptosis (apoptosis). KRAS-IN-64 can be used for research on pancreatic cancer.

9(S)-HODE-¹³C₁₈ ((+)-α-Dimophecolic acid-¹³C₁₈) is ¹³C labeled 9S-HODE. 9S-HODE (Alpha-dimorphecolic acid) is an octadecadienoic acid and the main active derivative of linoleic acid, which can reduce the viability of HL-60 cells and induce apoptosis. 9S-HODE is rich in lipid peroxidation (LPO) products and is almost an ideal marker for LPO.

Nanatinostat (CHR-3996) TFA is a potent, class I selective and orally active HDAC inhibitor with IC₅₀s of 3 nM, 4 nM, and 7 nM for HDAC1, HDAC2, and HDAC3, respectively. Nanatinostat TFA has low activity against HDAC5 (IC₅₀ of 200 nM) and HDAC6 (IC₅₀ of 2100 nM). Nanatinostat TFA induces apoptosis in myeloma cells. Nanatinostat TFA has potent anticancer effects, such as myeloma, advanced solid tumours and colorectal cancer.

IHMT-15137 is a BMX inhibitor with an IC₅₀ of 26.97 nM. IHMT-15137 covalently binds to BMX Cys496 within the ATP-binding pocket, inhibits BMX phosphorylation at Tyr566, and disrupts the BMX-ERK1/2-Cyclin D1/CDK4/6-E2F1 signaling axis. IHMT-15137 reduces E2F1 protein stability via decreased Ser332/337 phosphorylation, increased ubiquitination, and ubiquitin-proteasome pathway degradation. IHMT-15137 induces cell cycle arrest, apoptosis, DNA damage, and suppresses cell migration and invasion. IHMT-15137 can be used for the research of small cell lung cancer.