CLIK-148
CLIK-148 is a highly selective, irreversible and orally active cysteine protease inhibitor, primarily targeting Cathepsin L. CLIK-148 effectively inhibits the Cathepsin L-dependent degradation of HMG-CoA reductase in the endoplasmic reticulum (ER) membrane. CLIK-148 inhibits the processing of proCCK by Cathepsin L, thereby reducing the production of CCK8 (HY-P0093). CLIK-148 inhibits the degradation of type I collagen by osteoclasts' secreted Cathepsin L, reducing tumor-induced bone metastasis and malignant hypercalcemia. CLIK-148 can be used for the studies of bone metabolism disorders and regulation of neuropeptide processing.
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- No. CAS: 215098-90-1
- Fòrmula: C22H26N4O4
- Peso molecular:410.47
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Chemical Information
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Actividad biológica
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cathepsin L |
CLIK-148 (100 nM-10 μM) at a concentration of 100 nM in rat liver, potently and specifically inhibits Cathepsin L activity, while exhibits almost no inhibition against Cathepsin B and C at 1 μM, and demonstrates only weak inhibition towards Cathepsin S and K at a concentration of 10 μM[1].
CLIK-148 (50 μM, 24 h) inhibits the activity of Cathepsin L, thereby blocking the generation of CCK9 from proCCK and ultimately reducing the production of CCK8 in pituitary AtT-20 cells[2].
CLIK-148 (1-10 nM, 72 h) effectively inhibit the degradation of bone collagen mediated by human and mouse osteoclasts activated by TNF-α[3].
CLIK-148 (100 μM) effectively protects HMG-CoA reductase from pathological degradation in the context of C100 cell necrotic injury[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
CLIK-148 (50 mg/kg, p.o., once daily for 7 days) effectively prevents and treats malignant hypercalcemia caused by tumors in mice[3].
CLIK-148 (32-128 mg/kg, p.o. or i.v., once daily for 7 days) effectively inhibit the direct bone metastasis and local bone destruction of colon cancer cells[3].
CLIK-148 (100-200 mg/kg, p.o., once daily for 14 days) specifically inhibits the process by which cancer cells metastasize through the bloodstream to the bones in mice[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:LJC-1 cells induced direct bone metastasis and local bone resorption model of cancer established in CDF1 mice[3]
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Dosage:5 mg/kg
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Administration:Oral administration (p.o.), once daily for 7 days
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Result:Significantly reduced the serum calcium level in mice.
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Animal Model:Colon tumor 26 PMF-15 cells induced hypercalcemia of malignancy model established in CDF1 mice[3]
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Dosage:32, 64 and 128 mg/kg
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Administration:Oral administration (p.o.) or intravenous injection (i.v.), once daily for 7 days
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Result:Significantly inhibited the decline of calcium content and protect the bones.
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Animal Model:Melanoma A375 cells induced distant bone metastasis model established in CDF1 mice[3]
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Dosage:100 and 200 mg/kg
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Administration:Oral administration (p.o.), once daily for 14 days
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Result:Reduced the area of the metastatic lesion significantly to 1.0 mm². Did not inhibit the metastasis of cancer cells to other organs such as the liver, muscles, and gums.
Chemical Information
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No. CAS 215098-90-1
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Peso molecular 410.47
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Fòrmula C22H26N4O4
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SMILES
CN(C)C([C@H](CC1=CC=CC=C1)NC([C@@H]2[C@H](O2)C(NCCC3=CC=CC=N3)=O)=O)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Katunuma N, et al. Structure based development of novel specific inhibitors for cathepsin L and cathepsin S in vitro and in vivo. FEBS Lett. 1999 Sep 10;458(1):6-10. [Content Brief]
[2]. Beinfeld MC, et al. Cathepsin L plays a major role in cholecystokinin production in mouse brain cortex and in pituitary AtT-20 cells: protease gene knockout and inhibitor studies. Peptides. 2009 Oct;30(10):1882-91. [Content Brief]
[3]. Katunuma N, et al. Structure-based design of specific cathepsin inhibitors and their application to protection of bone metastases of cancer cells. Arch Biochem Biophys. 2002 Jan 15;397(2):305-11. [Content Brief]
[4]. Moriyama T, et al. 3-hydroxy-3-methylglutaryl coenzyme A reductase is sterol-dependently cleaved by cathepsin L-type cysteine protease in the isolated endoplasmic reticulum. Arch Biochem Biophys. 2001 Feb 15;386(2):205-12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
CLIK-148 Related Classifications
HY-164634 Related Classifications
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