Apoptosis Inducer

(S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-N(Me)-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-N(Me)-Boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.

Topoisomerase IIα-IN-4 (F2) is a non-intercalative ATP-competitive human DNA topoisomerase II inhibitor with an IC₅₀ value of 3.8 and 10.1 μM for TopoIIα and TopoIIβ, respectively. Topoisomerase IIα-IN-4 shows potent potency in apoptosis induction and cell cycle arrest in HepG2 cells. Topoisomerase IIα-IN-4 exhibits strong antitumor activities against human cancer cell lines, it can be used for the research of cancer.

VEGFR-2-IN-70 is a potent VEGFR-2 inhibitor with an IC₅₀ of 18.04 nM. VEGFR-2-IN-70 exhibits cytotoxicity against A549 and MCF-7 cancer cells with IC₅₀ values of 0.43 μM and 3.8 μM, respectively. VEGFR-2-IN-70 induces G1 cell cycle arrest and apoptosis in lung cancer cells. VEGFR-2-IN-70 is useful in cancer research.

Antitumor agent-201 (Compound 10) is a chloride transport activator that targets the Golgi apparatus. Its EC₅₀ for promoting the transmembrane transport of chloride ions is 1.53 mol%, and its IC₅₀ against HepG2 cells is 7.13 μM. Antitumor agent-201 exerts its anti-cancer activity by selectively acting on the Golgi apparatus, disrupting the chloride ion homeostasis within it, reducing the expression of key proteins such as GM130 and GRASP55, altering the structure and function of the Golgi apparatus, triggering Autophagy of the Golgi apparatus, and further inducing Apoptosis of cancer cells and arresting cancer cells in the G2/M phase. Antitumor agent-201 can be used in the research field of cancer diseases.

Topoisomerase II inhibitor 23 is a potent topoisomerase II inhibitor (IC₅₀ = 0.94 μM). Topoisomerase II inhibitor 23 shows high selectivity and exceptional cytotoxic activity in MCF-7, HepG2, and HCT116 cells. Topoisomerase II inhibitor 23 induces cell cycle arrest at the G1 phase, leading to inhibition of cell proliferation. Topoisomerase II inhibitor 2 induces apoptosis by up-regulating the pro-apoptotic Bax level and down-regulating the anti-apoptotic Bcl-2 level.

TMLB-C16 is a potent and orally active B3GAT3 inhibitor with a K_D of 3.962 μM. TMLB-C16 suppresses proliferation and migration, and induces cell cycle arrest and apoptosis in MHCC-97H (IC₅₀ = 6.53 μM) and HCCLM3 cells (IC₅₀ = 6.22 μM). TMLB-C16 inhibits tumor growth in both MHCC-97H and HCCLM3 xenograft tumor mouse models without causing obvious toxicity. TMLB-C16 can be used for hepatocellular carcinoma research.

TZEP7 is an EGFR kinase inhibitior in cancer cells. TZEP7 exhibits cytotoxic effects against cancer cell lines and induces apoptosis. TZEP7 demonstrates downregulation of antiapoptotic Bcl-2, upregulation of pro-apoptotic Bax, and increases caspase levels. TZEP7 is promising for research of anticancer agent.

Thalidomide-4-NH-PEG2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.

Cholicamideβ (GMP) is a GMP grade of Cholicamideβ. Cholicamideβ (compound 6) is a self-assembling, small molecule, cancer vaccine adjuvant. Cholicamideβ can form virus-like particles with low cytotoxicity. Cholicamideβ, upon binding to peptide antigens, enhances antigen presentation by dendritic cells and induces antigen-specific T cells. Cholicamideβ can induce apoptosis and necrosis.

C2 L-Erythro ceramide (d18:1/2:0) is a cell-permeable sphingolipid. C2 L-Erythro ceramide (d18:1/2:0) induces cell cycle arrest in the G0/G1 phase and inhibits cell growth.

VEGFR-2/P-gp-IN-2 is a VEGFR-2 inhibitor (IC₅₀ = 126.4 nM) and P-glycoprotein inhibitor. VEGFR-2/P-gp-IN-2 induces G1 phase cell cycle arrest and Apoptosis. VEGFR-2/P-gp-IN-2 can be used for research on cervical cancer.

Antitumor agent-80 (compound 11) is an orally active and potent antitumor agent. Antitumor agent-80 induces apoptosis in tumor cells.

Ketoprofen-d₄ is the deuterium labeled Ketoprofen. Ketoprofen (RP-19583) is a non-steroidal antiinflammatory agent, acting as a potent inhibitor of COX, with IC₅₀s of 2 nM and 26 nM for COX-1 and COX-2 in human blood monocytes, respectively.

Anticancer agent 55 is a potent anticancer agent. Anticancer agent 55 shows anticancer activity via reducing the cell viability and cell migration in a dose-dependent manner. Anticancer agent 55 induces apoptosis. Anticancer agent 55 has the potential for the research of prostate cancer and breast cancer.

IDH1/2-IN-1 (Compound 6b) serves as a dual inhibitor of IDH1(R132H)/IDH2(R140Q) with IC₅₀ values of 0.22 μM and 1.6 μM, respectively. IDH1/2-IN-1 effectively inhibits tumor growth by suppressing tumor cell proliferation and enhancing host defense through the activation of antioxidant enzymes. Additionally, IDH1/2-IN-1 reduces inflammation and promotes apoptosis, demonstrating robust antitumor activity. IDH1/2-IN-1 holds potential for research in leukemia.

Nampt-IN-16 (Compound 9a) is an orally active NAMPT inhibitor with an IC₅₀ of 0.15 μM. Nampt-IN-16 can reduce intracellular NAD⁺ and ATP levels. Nampt-IN-16 can inhibit the proliferation, migration, and invasion, induce cell cycle arrest and apoptosis, and alter cellular metabolism of gastric cancer cells. Nampt-IN-16 can be used in the research of tumors such as gastric cancer.

Antitumor photosensitizer-4 (compound 10b) is a potent tyrosine kinase inhibitor (TKI) targeting ABCG2. Antitumor photosensitizer-4 is a photosensitizer (PS) consisting of a conjugate of dasatinib (HY-10181) and imatinib (HY-15463). Antitumor photosensitizer-4 induces apoptosis and ROS production and exhibits strong phototoxicity to HepG2 and B16-F10 cells.

VEGFR-2-IN-19 (Compound 15b) is a potent VEGFR2 inhibitor. VEGFR-2-IN-19 induces cell apoptosis and increases intracellular reactive oxygen species level. VEGFR-2-IN-19 can be used as an anticancer agent.

Betulin (Standard) is the analytical standard of Betulin. This product is intended for research and analytical applications. Betulin (Trochol), is a sterol regulatory element-binding protein (SREBP) inhibitor with an IC50 of 14.5 μM in K562 cell line.

Axl-IN-18 (compound 25c) is a potent and selective type II AXL inhibitor. Axl-IN-18 shows excellent AXL inhibitory activity (IC₅₀=1.1 nM) and 343-fold selectivity over the highly homologous kinase MET in biochemical assays (IC₅₀=377 nM). Axl-IN-18 significantly inhibits AXL-driven cell proliferation, dose-dependently suppresses 4T1 cell migration and invasion, and induces apoptosis. Axl-IN-18 shows noticeable antitumor efficacy in a BaF3/TEL-AXL xenograft model.