mt cell

LDN-212854 (BMP Inhibitor III), a novel BMP inhibitor, exhibits greater selectivity for BMP versus the TGF-β type I receptors; possesses differences towards ALK2(IC50=1.3 nM) versus ALK1/3 compared to other inhibitors.

D77 is anti-HIV-1 inhibitor. D77 inhibits HIV-1(IIIB) replication by EC50 value of 23.8 μg/ml in MT-4 cell (5.03 μg/ml for C8166 cells).

MT 63-78 is a specific and effective direct AMPK activator (EC50: 25 μM) that blocks prostate cancer growth by inhibiting the lipogenesis and mTORC1 pathways. It has antitumor effects and induces cell mitotic arrest and apoptosis.

Antitumor agent-163 (Compound 3) serves as a photosensitizer in molecular-targeted photodynamic therapy (MT-PDT) aimed at carbonic anhydrase IX (CAIX). Under illumination at 540 nm, Antitumor agent-163 inactivates CAIX protein through singlet oxygen generation without affecting internal standard proteins such as α-tubulin, β-actin, and proliferating cell nuclear antigen (PCNA). It induces cell membrane damage and reduces cell viability with IC50 values of 0.2 μM for A549 and 0.05 μM for U87MG. Furthermore, Antitumor agent-163 demonstrates antitumor activity in mouse models.

Boromycin is a boron-containing macrolide antibiotic that has been found in Streptomyces. Boromycin inhibits growth of B. subtilis (MIC = 0.05 μg/ml) and induces efflux of potassium ions from B. subtilis without affecting Na+/K+-ATPase activity. It decreases the synthesis of protein, RNA, and DNA in B. subtilis when used at a concentration of 0.05 μg/ml. It inhibits the growth of B. halodurans (MIC = 10 ng/ml) and inhibits the futalosine pathway of menaquinone synthesis in B. halodurans. Boromycin (3.4 nM) reverses bleomycin-induced cell cycle arrest at the G2 phase in Jurkat cells. It inhibits replication of the HIV-1 strains LAV-1 and RF and the HIV-2 strain LAV-2 in MT-4 cells (IC50s = 0.008, 0.11, and 0.007 μM, respectively). It also inhibits replication of a clinical isolate of HIV-1, strain KK-1, in MT-4 cells and peripheral blood mononuclear cells (PBMCs; IC50s = 0.14 and <0.1 μM, respectively).

1,4-Dicaffeoylquinic acid has antioxidant activity.1,4-Dicaffeoylquinic acid is a potent and highly selective class of HIV-1 integrase inhibitors, inhibitsHIV-1 replication in MT-2 cell culture at non-toxic concentrations.

KRH-1636 is an orally active, selective and extremely potent CXC chemokine receptor 4 antagonist. KRH-1636 exhibits a potent and selective anti-HIV-1 activity. KRH-1636 efficiently blocked replication of various T cell line-tropic (X4) HIV type 1 (HIV-1) in MT-4 cells and peripheral blood mononuclear cells through the inhibition of viral entry and membrane fusion via the CXC chemokine receptor (CXCR)4 coreceptor but not via CC chemokine receptor 5. KRH-1636 also inhibits binding of the CXC chemokine, stromal cell-derived factor 1alpha, to CXCR4 specifically and subsequent signal transduction. KRH-1636 prevented monoclonal antibodies from binding to CXCR4 without down-modulation of the coreceptor. KRH-1636 seems to be a promising agent for the treatment of HIV-1 infection.

Blinatumomab (AMG-10,MT-103) is a CD19/CD3 bispecific B-cell and T-cell binding antibody that directs T-cells to attack cancer cells by binding to both CD3 on T-cells and CD19 on cancer cells, and is used in acute lymphoblastic leukemia and non-Hodgkin's lymphoma.

ST-401, a microtubule-targeting agent (MTA), functions as a brain-penetrant microtubule (MT) assembly inhibitor. It disrupts microtubule (MT) function by gently and reversibly reducing MT assembly, which leads to mitotic delay and interphase cell death. ST-401 demonstrates potent antitumor activity.

SHLP-3, a mitochondrial-derived peptide encoded by the 16S ribosomal RNA gene (MT-RNR2), enhances cellular vitality and reduces cell death (apoptosis) in NIT-1β insulinoma cells and 22Rv1 human prostate cancer cells. This peptide boosts mitochondrial function by increasing mitochondrial oxygen consumption rate (OCR), cellular ATP, and reducing the capacity to produce ROS, thereby providing cellular protection. SHLP-3 is utilized in research on diabetes and cancer.