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UK-370106

CAS No. : 230961-21-4

MCE 站：UK-370106

产品活性：UK-370106 是一种有效且高度选择性的 MMP-3 (IC₅₀ 为 23 nM) 和 MMP-12 (IC₅₀ 为 42 nM) 抑制剂，效力比 MMP-1，MMP-2，MMP-9 和 MMP-14 高 1200 倍以上，比 MMP-13 高约 100 倍。UK-370106 有效抑制 MMP-3 对 [³H]-fibronectin 的裂解 (IC₅₀ 为 320 nM)，并且对角质形成细胞迁移影响很小。

研究领域：Metabolic Enzyme/Protease

作用靶点：MMP

In Vitro: The potency of UK-370106 (compound 7) for the inhibition of MMP-13 is 2.3 ?M, some 100-fold less potent than its inhibition of MMP-3. UK-370106 is found to be inactive (IC₅₀ > 100 ?M) vs zinc metalloproteases PCP and TACE and possesses the following inhibitory potencies vs MMP-2 (IC₅₀ of 34.2 ?M), MMP-7 (IC₅₀ of 5.8 ?M), MMP-8 (IC₅₀ of 1.75 ?M), MMP-9 (IC₅₀ of 30.4 ?M) and MMP-14 (IC₅₀ of 66.9 ?M).
UK-370106 potently inhibits cleavage of [³H]-fibronectin by MMP-3 (IC₅₀ of 320 nM) but does not inhibit cleavage of [³H]-gelatin by either MMP-2 or -9 up to the highest concentration tested (100 ?M).
UK-370106 is not cytotoxic to, nor affected proliferation of, fibroblasts, keratinocytes, or endothelial cells at 50-100 ?M in vitro.

In Vivo: Following iv (rat; 2 mg/kg) or topical administration to dermal wounds (rabbit), UK-370106 (compound 7) is cleared rapidly (t_1/2 = 23 min) from plasma, but slowly (t_1/2 approximately 3 days) from dermal tissue. In a model of chronic dermal ulcers, topical administration of UK-370106 for 6 days substantially inhibits MMP-3 ex vivo.

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