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CAS No. :
MCE 国际站:SID 26681509 quarterhydrate
产品活性:SID 26681509 quarterhydrate 是一种有效的,可逆的,竞争性的,选择性的人组织蛋白酶 L (human cathepsin L) 抑制剂,IC50 为 56 nM。SID 26681509 quarterhydrate 抑制 Plasmodium falciparum 的体外繁殖,并抑制 Leishmania major,IC50 分别为 15.4 μM 和 12.5 μM。SID 26681509 quarterhydrate 对组织蛋白酶 G 没有抑制活性。
研究领域:Metabolic Enzyme/Protease | Anti-infection
作用靶点:Cathepsin | Parasite
In Vitro: After a 4 hr preincubation with cathepsin L, SID 26681509 becomes more potent, demonstrating an IC50 of 1.0 nM. SID 26681509 is determined to be a slow-binding and slowly reversible competitive inhibitor. Through a transient kinetic analysis for single-step reversibility, inhibition rate constants are kon = 24,000 M-1s-1 and koff = 2.2 × 10-5 s-1 (Ki = 0.89 nM). Molecular docking studies are undertaken using the experimentally-derived X-ray crystal structure of papain/CLIK-148.
SID 26681509 inhibits papain and cathepsins B, K, S, and V with IC50 values determined after one hour ranging from 618 nM to 8.442 μM. SID 26681509 shows no inhibitory activity against the serine protease cathepsin G.
SID 26681509 inhibits cathepsin V activity with an IC50 value of 0.5 μM. SID 26681509 (1-30 μM) blocks high-mobility group box 1 (HMGB1)-induced TNF-α production dose dependently without altering cell viability.
In Vivo: SID 26681509 treatment significantly improves survival in murine models of sepsis and reduces liver damage following warm liver ischemia/reperfusion (I/R) models.
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