20S Proteasome-IN-2,2028300-31

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20S Proteasome-IN-2

CAS No. : 2028300-31-2

MCE 国际站：20S Proteasome-IN-2

产品活性：20S Proteasome-IN-2 是人 20S proteasome 抑制剂。20S Proteasome-IN-2 对它的 β5 亚基具有高选择性，IC₅₀ 为 0.18 μM。20S Proteasome-IN-2 在体内外均有抗肿瘤细胞增殖的作用，并将细胞周期阻滞在 G2/M 期。

研究领域：Metabolic Enzyme/Protease

作用靶点：Proteasome

In Vitro: 20S Proteasome-IN-2 (compoun 11m) inhibits 20S proteasome by forming no irreversible covalent modification on it.
20S Proteasome-IN-2 (compoun 11m) (1.56, 3.13, 6.25, 12.5, and 25 μM) shows high binding affinity with purified human 20S proteasome, the equilibrium dissociation constants is 4.8 μM.
20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) inhibits tumor cells in a low concerntration with IC₅₀ values of 0.88, 0.77, 0.67, 0.73, 1.3, 0.57, and 0.28 μM for A375, BGC-823, Hela, HT-29, A549, PCM1E8, HCT-116, resepectively.
20S Proteasome-IN-2 (compoun 11m) (0-1.5 μM; 24 hours) arrests the cell cycle at G2/M.

In Vivo: 20S Proteasome-IN-2 (compoun 11m) is (i.v.; 5 mg/kg; single injection) rapidly cleared from the plasma with an average terminal plasma half-life of 14 min, thus it exhibits extensive tissue permeability and low clearance rate (CL) of 2.0 L/h/k, and is largely eliminated extrahepatically.
20S Proteasome-IN-2 (compoun 11m) (i.v.; 10 mg/kg; twice one week; 4 weeks) shows antitumor efficacy combat solid tumors.
Pharmacokinetic parameters of 20S Proteasome-IN-2 (compoun 11m)

Administrations	Cmax (μg/L)	AUC0-t (μg/L•h)	T1/2 (min)	MRT (min)	CL (L/h/kg)	Vss (L/kg)
iv, 5 mg/kg	2007	680	13.83	20.20	2.0	0.66

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