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Chymostatin

MCE China：Chymostatin

Brand：MedChemExpress (MCE)

Cat. No.HY-P3042

CAS：9076-44-2

Purity：99.0%

Storage：Sealed storage, away from moisture Powder -80°C 2 years -20°C 1 year *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Chymostatin is a SARS-CoV-2 Mpro inhibitor. Chymostatin up-regulates endocan and inhibits NF-κBp65 activity. Chymostatin reduces proinflammatory cytokines (IL-1β and IL-6) and HMGB1. Chymostatin shows protective effects against Paraquat-induced acute lung injury. Chymostatin exhibits anticancer activity against lung cancer.

In Vitro：Chymostatin (20-150 μM) inhibits cellular aggregation of activated human peripheral blood lymphocytes[2]. Chymostatin (50 μM, 1 h) combined with Aliskiren (HY-12176) to alleviate endoplasmic reticulum stress induced by lipid overload in kidney tubular cells HK2[3]. Chymostatin shows dose-dependent inhibition of COVID-19 Mpro activity with IC50 of 15.81 µM[4]. Chymostatin (up to 100 µM) does not show any cytotoxicity on normal mouse lung epithelial cells, where as it inhibits proliferation of human H441 lung cancer cells (KrasG12V mutant) with IC50 of 1.2 µM[4]. Chymostatin (20 µM) decreases protein breakdown in leg muscles from normal rodents and also in denervated and dystrophic muscles[5].

In Vivo：Chymostatin (2 mg/kg, i.p., 30 min before paraquat administration) shows protective effects against paraquat-induced acute lung injury in mice[1]. Chymostatin (2 mg/kg/h, i.v.) decreases heart rate, renal blood flow and increases IVR in 2K1C rats[6]. Chymostatin (2 mg/kg/h, i.v.) increases plasma potassium concentrations (17%) in UNX HS rats[6].. Chymostatin (1 mg/kg, i.p.) retards the decrease in locomotor activity and increases muscle protein in dystrophic mice[7].

IC50 & Target：NF-κB IL-6 IL-1β

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References：

[1]. Chen Yang, et al. Protective Effects of Chymostatin on Paraquat-Induced Acute Lung Injury in Mice. Inflammation  [Content Brief]

[2]. Lane JT, et al. Chymostatin inhibits cellular aggregation of activated human peripheral blood lymphocytes. Life Sci. 1980 Aug 11;27(6):451-6.  [Content Brief]

[3]. Qiu M, et al. Combination of Chymostatin and Aliskiren attenuates ER stress induced by lipid overload in kidney tubular cells. Lipids Health Dis. 2018 Jul 31;17(1):183.  [Content Brief]

[4]. Abstract LB074: Chymostatin, a cathepsin L inhibitor, inhibits lung cancer cell proliferation and COVID-19 Mpro in vitro.

[5]. Libby P, et al. Effects of chymostatin and other proteinase inhibitors on protein breakdown and proteolytic activities in muscle. Biochem J. 1980 Apr 15;188(1):213-20.  [Content Brief]

[6]. Roszkowska-Chojecka MM, et al. Effects of chymostatin, a chymase inhibitor, on blood pressure, plasma and tissue angiotensin II, renal haemodynamics and renal excretion in two models of hypertension in the rat. Exp Physiol. 2015 Sep;100(9):1093-105.  [Content Brief]

[7]. Komatsu K, et al. Beneficial effect of chymostatin on dystrophic mice. Exp Neurol. 1986 Jul;93(1):110-6.  [Content Brief]