Apoptosis Inducer

Paroxetine-d₂ (BRL29060-d₂) is the deuterated-labeled Paroxetine (HY-122272). Paroxetine (BRL29060) is an orally active and selective serotonin reuptake inhibitor (SSRI) and apoptosis inducer with blood-brain barrier permeability. Paroxetine inhibits nitric oxide synthase and CYP2D6, induces desensitization of 5-HT1A/1B/1D autoreceptors, downregulates 5-HT2 receptors, and promotes the production of inflammatory cytokines. Paroxetine is a weak norepinephrine (NE) uptake inhibitor and possesses antitumor activity. Paroxetine is widely used in research concerning depression, obsessive-compulsive disorder, panic disorder, social phobia, generalized anxiety disorder, post-traumatic stress disorder, premenstrual dysphoric disorder, hot flashes, and related conditions.

AKT-IN-21 (compound C36) is a potent AKT inhibitor with broad-spectrum cytotoxicity and anticancer activity. AKT-IN-21 also blocks the cell cycle and induces apoptosis of cancer cells by down-regulating the PI3K/AKT pathway.

PFKL-IN-1 is an orally active PFKL inhibitor, with a human-derived IC₅₀ value of 52.63 nM and a K_d of 0.24 μM. PFKL-IN-1 directly binds to PFKL and inhibits its enzymatic activity. PFKL-IN-1 inhibits glycolysis, induces apoptosis and suppresses cell proliferation in breast cancer cells. PFKL-IN-1 exhibits antitumor efficacy in mouse models and enhances the therapeutic effect of anti-PD-L1 agents. PFKL-IN-1 can be used in breast cancer-related research.

(Rac)-Idroxioleic acid (Standard) is the analytical standard of (Rac)-Idroxioleic acid. This product is intended for research and analytical applications. (Rac)-Idroxioleic acid (2-Hydroxyoleic acid) is a synthetic oleic acid (OA) derivative that binds to the plasma membrane and alters lipid organization. (Rac)-Idroxioleic acid has anti-tumor effect[1].

Sertaconazole (FI7056 free base) is a broad-spectrum topical antifungal agent, exhibits anti-inflammatory activity via activation of a p38-COX-2-PGE2 pathway. Sertaconazole is also a microtubule inhibitor, shows antiproliferative effect, induces apoptosis and autophagy, and can also inhibit the migration of cells.

Anticancer agent 72 (compound 8c) is a potent inhibitor of K⁺ channel. Anticancer agent 72 induces apoptosis.

Polyphyllin I (Standard) is the analytical standard of Polyphyllin I. This product is intended for research and analytical applications. Polyphyllin I is a bioactive constituent extracted from Paris polyphylla, has strong anti-tumor activity. Polyphyllin I is an activator of the JNK signaling pathway and is an inhibitor of PDK1/Akt/mTOR signaling. Polyphyllin I induces autophagy, G2/M phase arrest and apoptosis.

Topoisomerase I/II-IN-1 is a dual inhibitor of topoisomerase I/II. Topoisomerase I/II-IN-1 induces G2/M arrest and apoptosis in cancer cells by upregulating p53, p21, and Bax mRNA levels, caspase-3 protein levels, and the Bax/Bcl-2 ratio, while downregulating Bcl-2. Topoisomerase I/II-IN-1 is useful in the study of various cancers, including melanoma, renal cancer, colorectal cancer, and breast cancer.

MYRA-A is a potent apoptosis inducer in a Myc-dependent manner. MYRA-A inhibits Myc transactivation and interferes with the DNA-binding activity of Myc family proteins. MYRA-A inhibits cell viability.

BMI-1026 is a cyclin-dependent kinase 1 (Cdk1) inhibitor with IC₅₀ of 2.3 nM. BMI-1026 induces apoptosis by arresting the G2-M phase.

FLT3-IN-31 (compound 10q) is a potent FLT3 inhibitor with IC₅₀ values of 0.16, 2.4 nM for FLT3, FLT3-D835Y, resprctively. FLT3-IN-31 shows antiproliferation activity. FLT3-IN-31 decreases the protein expression of p-FLT3, P-STAT5, P-ERK. FLT3-IN-31 induces apoptosis and cell cycle arrest at G1 phase. FLT3-IN-31 shows antitumor activity.

Anticancer agent 56 (compound 4d) is a potent anti-cancer agent with agent-likeness properties, possessing anticancer activity against several cancer cell lines (IC₅₀<3 μM). Anticancer agent 56 induces cell cycle arrest at G2/M phase and triggers mitochondrial apoptosis pathway. Anticancer agent 56 acts by accumulation of ROS, up regulation of BAX, down regulation of Bcl-2 and activation of caspases 3, 7, 9.

Apoptosis inducer 49 is a selective apoptosis inducer with high specificity against CCRF-CEM leukemia cells (IC₅₀ = 2.68 μM). Apoptosis inducer 49 enhances RNA synthesis and replication stress, activates the Chk1-p21 axis, leading to S-phase arrest. Apoptosis inducer 49 can inhibit Bcl-2 and activate caspase-3. Apoptosis inducer 49 can be used for the study of Leukemia.

Autophagy-IN-2 (Compound 7h) is an autophagic flux inhibitor. Autophagy-IN-2 induces cancer cell apoptosis and can be used for triple-negative breast cancer research.

N-Desmethyldauricine is a NF-κB p65 inhibitor and apoptosis inducer. N-Desmethyldauricine reduces the protein expression level of p65, induces apoptosis, arrests the cell cycle at the G0/G1 phase, attenuates intercellular adhesion, and inhibits the growth of 3D spheroids of triple-negative breast cancer. N-Desmethyldauricine can be used in studies related to triple-negative breast cancer.

FLT3-IN-39 (Compound W4) is a selective FLT3 inhibitor, with an IC₅₀ value of 16.0 nM against FLT3-ITD and an IC₅₀ value of 20.4 nM against FLT3-D835Y. FLT3-IN-39 inhibits FLT3-ITD and FLT3-D835Y mutant kinases. FLT3-IN-39 induces G0/G1 cell cycle arrest and Apoptosis in cancer cells, and reduces intracellular ROS levels. FLT3-IN-39 exhibits anti-tumor activity against acute myeloid leukemia.

Cucurbitacin F is a tetracyclic protostane-type triterpenoid with low toxicity, antibacterial and anti-inflammatory activities, and is also a related compound of Cucurbitacin B (HY-N0416). Cucurbitacin F widely exists in plants such as Cucurbitaceae plants, Quisqualis indica and Sorbaria sorbifolia. Cucurbitacin F acts as an actin aggregator and reduces cell viability in a dose-dependent manner. Cucurbitacin F induces apoptosis by triggering G2/M phase cell cycle arrest and activating the caspase-3-dependent apoptosis.

ALK-IN-33 (Compound 8q) is an orally active ALK inhibitor with an IC₅₀ of 1.61 nM. ALK-IN-33 exhibits significant selective killing effect on ALK-positive cancer cells. ALK-IN-33 induces cell cycle arrest and apoptosis, effectively weakening the migration, invasion and long-term survival ability of cancer cells. ALK-IN-33 can be used for research on non-small cell lung cancer

FLT3/HDAC-IN-3 is a dual inhibitor of FLT3 and HDAC. FLT3/HDAC-IN-3 potently inhibits FLT3 (IC₅₀ = 14 nM), HDAC1 (IC₅₀ = 27 nM), HDAC6 (IC₅₀ = 20 nM), and FLT3^D853Y (IC₅₀ = 55 nM), exhibits weak activity against HDAC8, and shows no activity against HDAC4. FLT3/HDAC-IN-3 possesses kinase selectivity, plasma stability, and stability in human liver microsomes. FLT3/HDAC-IN-3 demonstrates anti-proliferative effects in a variety of hematological malignancy cell lines. FLT3/HDAC-IN-3 shows efficacy in the Jeko-1 xenograft model without observed significant toxicity. FLT3/HDAC-IN-3 can be used in the study of hematological malignancies.

7-epi-Isogarcinol is a polycyclic polyprenylated acylphloroglucinol (PPAP), with moderate antiproliferative activity. 7-epi-Isogarcinol blocks STAT3 signaling pathway, to induce apoptosis and inhibit cell migration.