|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)是一种有效的，广谱matrix metalloprotease (MMP)（基质金属蛋白酶）抑制剂，作用于MMP-1， MMP-2， MMP-9， MMP-7和MMP-3，IC50分别为3 nM， 4 nM， 4 nM， 6 nM和20 nM。
To assess cleavage, 2 μg of pro-TNF-α was incubated with either 2 μg ADAM17 or 2 μg MMP9 in the presence or absence of inhibitor. Lanes are as follows: 1. Molecular weight markers, 2. Pro-TNF-α alone, 3. Pro-TNF-α + ADAM17, 4. pro-TNF-α+ ADAM17 + BB-94 (10 μM), 5. Pro-TNF-α + MMP9, 6. Pro-TNF-α + MMP9 + AB0041 (10 μM), 7. Pro-TNF-α+ MMP9 + BB-94 (10 μM), 8. Soluble TNF-α.
Ilomastat (GM6001, Galardin)是一种广谱matrix metalloprotease (MMP)（基质金属蛋白酶）抑制剂，作用于MMP-1， MMP-2， MMP-3， MMP-7， MMP-8， MMP-9， MMP-12， MMP-14，和MMP-26，Ki分别为0.4 nM， 0.5 nM， 27 nM， 3.7 nM， 0.1 nM， 0.2 nM， 3.6 nM， 13.4 nM，和0.36 nM。
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 是高效选择性的gelatinase抑制剂，其作用于MMP-2和MMP-9的Ki分别为13.9 nM 和 600 nM。
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)是一种广谱的 matrix metalloprotease (MMP) 抑制剂，对 MMP-9，MMP-1，MMP-2，MMP-14 和 MMP-7 的 IC50 分别为 3 nM，5 nM，6 nM，9 nM 和 13 nM。Phase 3。
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.