|S7155||Batimastat (BB-94)||<1 mg/mL||96 mg/mL||<1 mg/mL|
|S8072||NSC 405020||<1 mg/mL||52 mg/mL||52 mg/mL|
|S4163||Doxycycline Hyclate||100 mg/mL||100 mg/mL||<1 mg/mL|
|S7157||Ilomastat (GM6001, Galardin)||<1 mg/mL||78 mg/mL||8 mg/mL|
|S7430||SB-3CT||<1 mg/mL||61 mg/mL||10 mg/mL|
|S7156||Marimastat (BB-2516)||<1 mg/mL||54 mg/mL||7 mg/mL|
|S2333||Nobiletin||<1 mg/mL||81 mg/mL||3 mg/mL|
Batimastat (BB-94) is a potent, broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-9, MMP-7 and MMP-3 with IC50 of 3 nM, 4 nM, 4 nM, 6 nM and 20 nM, respectively. Also inhibits the activitity of other metalloproteases, such as ADAM17.
Proliferation indices of SU-pcGBM2 cells exposed to plain medium (aCSF) or active conditioned medium generated in the presence or absence of pan-MMP inhibitor (BAT).
NSC 405020 is a noncatalytic inhibitor of MT1-MMP, directly interacts with PEX domain of MT1-MMP, affects PEX homodimerization but not catalytic activity of MT1-MMP.
Doxycycline is a member of the tetracycline antibiotics group, and is commonly used to treat a variety of infections. It is also an inhibitor of matrix metallo-proteinases (MMP).
Ilomastat (GM6001, Galardin) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-1, MMP-2, MMP-3, MMP-7, MMP-8, MMP-9, MMP-12, MMP-14, and MMP-26 with Ki of 0.4 nM, 0.5 nM, 27 nM, 3.7 nM, 0.1 nM, 0.2 nM, 3.6 nM, 13.4 nM, 0.36 nM, respectively.
ARPE-19 cells were seeded on Millicell inserts for growth to form the monolayer. Monolayers were treated with or without recombinant HIV-1 gp120 glycoprotein during the last 2 days of cell culture. Some samples were pretreated with anti-DC-SIGN antibodies or GM6001 before incubation with gp120. A, the TEER value was measured. B, the paracellular permeability for FITC-dextran flux was assessed. Date represent mean ± S.D. *, p < 0.05; **, p < 0.01; ***, p < 0.001. Ω, ohm.
SB-3CT is an effective and selective gelatinase inhibitor with Ki of 13.9 nM and 600 nM for MMP-2 and MMP-9, respectively.
B) Representative immunoblot and quantitative analysis of the effect of SB-3CT on the decrease in claudin-5 (25 kDa) and (C) AQP4 (35 kDa) expressions induced by MDMA at 1 h (n=4-6).
Marimastat (BB-2516) is a broad spectrum matrix metalloprotease (MMP) inhibitor for MMP-9, MMP-1, MMP-2, MMP-14 and MMP-7 with IC50 of 3 nM, 5 nM, 6 nM, 9 nM and 13 nM, respectively. Phase 3.
Nobiletin, a citrus flavonoid isolated from citrus peels like in tangerine, which has anti-inflammatory and anti-tumor activities.
NOB modulates Cps1 mRNA and protein expression. a Total protein extracts were prepared from liver samples collected from the four diet/treatment groups of wild-type mice at the indicated circadian time points (n = 3). Western blotting analysis was performed using anti-CPS1 antibody. RC regular chow, HFD high-fat diet, Veh vehicle, NOB Nobiletin. The results shown are representative of three independent experiments. See Additional file 1: Figure S1A for quantitative analysis. b Immunohistochemical staining of CPS1 in liver sections from mice with the indicated diet and treatment at ZT2. c Real-time RT-PCR analysis of Cps1 in liver samples collected as in (a). Data are presented as mean ± SEM (n = 3). Two-way ANOVA with Bonferroni post-hoc tests shows significant statistical differences between HFD.Veh and other three groups (p < 0.0001). d Western blotting analysis of protein lysates of liver samples collected at ZT 6 and 18 from mice with the indicated diet and treatment (n = 3). HPD indicates high-protein diet. The images shown to the left are representative of three independent experiments. Quantitation of Western blots was carried out and the results, presented as mean ± SEM, are shown in the lower panel. Two-way ANOVA with Bonferroni post-hoc tests, RC vs. HPD, ***p < 0.001. e Real-time qPCR analysis was carried out using total RNAs extracted from the liver samples described in (d). The results are presented as mean ± SEM. Two-way ANOVA with Bonferroni post-hoc tests, RC vs. HPD, *p < 0.05.