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
 |
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). |
| 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 |
| Molecular Weight | 590.47 |
| Formula | C26H32BrN5O6 |
| CAS Number | 1564286-55-0 |
| Solubility (25°C) | DMSO ≥ 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Integrin Products |
|---|
| Cilengitide
Cilengitide (EMD 121974, NSC 707544) is a selective inhibitor of αvβ3 integrin and αvβ5 integrin with IC50 of 1 nM and 140 nM, respectively. |
| A-205804
A-205804 is a potent and selective inhibitor of E-selectin and ICAM-1 expression with IC50 of 20 nM and 25 nM respectively. |
| RGD
RGD (Arg-Gly-Asp) Peptides is a cell adhesion motif which can mimic cell adhesion proteins and bind to integrins. |
| Tirofiban
Tirofiban (L700462) is a selective and reversible platelet integrin receptor (Gp IIb/IIIa) antagonist that inhibits fibrinogen binding to this receptor and has antithrombotic activity. Tirofiban induces proliferation and migration on endothelial cell by inducing production of VEGF. |
| ATN-161 TFA
ATN-161 TFA salt is a novel small peptide inhibitor of integrin α5β1; a beta integrin antagonist with antitumor activity. |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
