All AbMole products are for research use only, cannot be used for human consumption.
CWHM-12 is a potent inhibitor of αV integrins with IC50 values of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1, respectively. CWHM-12 demonstrates high potency against all of the five possible β subunit binding partners (αvβ1, αvβ3, αvβ5, αvβ6 and αvβ8) in in vitro ligand-binding assays.
In vivo, CWHM-12 significantly reduces liver fibrosis even after fibrotic disease have been established. Digital image quantitation demonstrates significantly reduced p-SMAD3 signaling in the livers of CWHM-12 treated mice compare to controls, demonstrating that the protection from CCl4-induced hepatic fibrosis observed in CWHM-12 treated mice is due at least in part to a reduction in TGF-β activation by αv integrins. Besides, administration of CWHM-12 significantly inhibited progression of pulmonary fibrosis.
Chin Med J (Engl). 2021 Apr 20;134(9):1093-1100.
Role of osteopontin in diet-induced brown gallstone formation in rats
CWHM-12 purchased from AbMole
Cell Experiment | |
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Cell lines | The stably transfected human 293 cells over-expressing human αvβ3 or αvβ5 |
Preparation method | The stably transfected human 293 cells over-expressing human αvβ3 or αvβ5 are pre-incubated in HBSS buffer containing 200 μM MnCl2 for 30 min at 37°C with 3-fold dilutions of compound (e.g., CWHM-12). Each sample is then added to triplicate wells of a 96-well plate which has been coated overnight at 4°C with a predetermined optimal concentration of purified vitronectin, washed, blocked by 1 hr incubation with BSA, and washed again. Cells are allowed to attach for 30 min at 37°C, and non-adherent cells are removed by washing. Remaining attached cells are measured by endogenous alkaline phosphatase activity using para-nitrophenyl phosphate and reading absorbance signal at 405 nM. |
Concentrations | |
Incubation time | 90 min |
Animal Experiment | |
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Animal models | Wild type C57/BL6 mice, Itgav(flox/flox) mice and itgb8(flox/flox) mice |
Formulation | 50% DMSO (in sterile water) |
Dosages | 100 mg/kg/day |
Administration | delivered by implantable ALZET osmotic minipumps |
Molecular Weight | 590.47 |
Formula | C26H32BrN5O6 |
CAS Number | 1564286-55-0 |
Solubility (25°C) | DMSO: 10 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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