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CWHM-12

Cat. No. M8975

All AbMole products are for research use only, cannot be used for human consumption.

CWHM-12 Structure
Size Price Availability Quantity
2mg USD 80  USD80 In stock
5mg USD 110  USD110 In stock
10mg USD 190  USD190 In stock
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Quality Control & Documentation
Biological Activity

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.

Product Citations
Customer Product Validations & Biological Datas
Source Chin Med J (Engl) (2021). Figure 6. CWHM12 (Abmole Bioscience Inc, Houston, TX, USA)
Method Cell culture
Cell Lines BRL cell line
Concentrations -
Incubation Time 1 h
Results TNF-a content differed between the groups (F = 1041, P < 0.01), with the OPN group showing a significant elevation compared with normal saline (t = 56.59, P < 0.01), the CWHM12 + OPN group showing a significant reduction compared with the OPN group (t = -44.21, P < 0.01), and the CD44-Ab + OPN group showing a significant reduction, relative to both OPN (t = -23.63, P < 0.01) and NS-IgG + OPN groups (t = -18.40, P < 0.01).
Protocol (for reference only)
Cell Experiment
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
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
Chemical Information
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
References

[1] Henderson NC, et al. Nat Med. Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs.

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Keywords: CWHM-12 supplier, Integrin, inhibitors, activators

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