CWHM-12
Based on 10 publication(s) in Google Scholar
CWHM-12 is a potent inhibitor of αV integrins with IC50s of 0.2, 0.8, 1.5, and 1.8 nM for αvβ8, αvβ3, αvβ6, and αvβ1.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.94%
- CAS. Nr.: 1564286-55-0
- Formel: C26H32BrN5O6
- Molecular Weight:590.47
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) CWHM-12
More- Cell. 2021 Sep 16;184(19):4919-4938.e22. [Abstract]
- Gastroenterology. 2026 Feb 27:S0016-5085(25)06526-6. [Abstract]
- Gut. 2022 Jan;71(1):55-67. [Abstract]
- Adv Fiber Mater. 2025 Dec 22.
- Adv Sci (Weinh). 2025 Oct 30:e01602. [Abstract]
- Cells. 2022 Jan 11;11(2):237. [Abstract]
- Glia. 2023 Feb;71(2):245-258. [Abstract]
- Sci Rep. 2021 Mar 15;11(1):5885. [Abstract]
- PLoS One. 2025 Jul 18;20(7):e0328263. [Abstract]
- bioRxiv. 2025 Sep 21.
Customer Validation & Images
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Cell Imaging/Staining
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Others
Biologische Aktivität
IC50: 0.2 nM (αvβ8), 0.8 nM (αvβ3), 1.5 nM (αvβ6), 1.8 nM (αvβ1), 61 nM (αvβ5)[1]
CWHM-12 (CWHM 12) also less potently inhibits αvβ5 (IC50=61 nM) and αIIbβ3/α2β1/α10β1 (IC50>5000 nM). 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, with somewhat less potency against αvβ5 than against the other αv integrins[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 1564286-55-0
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Appearance Solid
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Molecular Weight 590.47
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Formel C26H32BrN5O6
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Color White to light brown
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SMILES
O=C(CNC(C1=CC(NC2=NCC(O)CN2)=CC(O)=C1)=O)N[C@H](C3=CC(C(C)(C)C)=CC(Br)=C3)CC(O)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (10)
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Journal Impact Factor
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Most Recent
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Cell
Directed evolution of a family of AAV capsid variants enabling potent muscle-directed gene delivery across species. [Abstract]2021 Sep 16;184(19):4919-4938.e22. PMID: 34506722
CWHM-12 purchased from MedChemExpress. Usage Cited in: Cell. 2021 Sep 16;184(19):4919-4938.e22. [Abstract]
In vitro transduction efficiency in human primary myotubes treated with different concentrations of CWHM-12 pan-integrin ɑV antagonists and transduced with AAV9- or MyoAAV 1A-CK8-Nluc.
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Gastroenterology
Activation of the Integrin αV-YAP-CTGF Axis in Liver Sinusoidal Endothelial Cells Promotes Liver Fibrogenesis, Leading to Portal Hypertension and Liver Carcinogenesis in Congestive Hepatopathy. [Abstract]2026 Feb 27:S0016-5085(25)06526-6. PMID: 41758081
CWHM-12 purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2026 Feb 27:S0016-5085(25)06526-6. [Abstract]
The p-FAK/FAK and YAP/p-YAP ratios were calculated. CTGF expression in HP-stimulated TMNK-1 cells treated with CWHM-12, verteporfin, a YAP inhibitor that disrupts YAP-TEA domain factor (TEAD) interactions, or YAP/TAZ short interfering RNA (siRNA).
CWHM-12 purchased from MedChemExpress. Usage Cited in: Gastroenterology. 2026 Feb 27:S0016-5085(25)06526-6. [Abstract]
CWHM-12 (100 mg/kg/d). Western blot images of phosphorylated YAP (p-YAP) and YAP.
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Gut
Activated intestinal muscle cells promote preadipocyte migration: a novel mechanism for creeping fat formation in Crohn's disease. [Abstract]2022 Jan;71(1):55-67. PMID: 33468536 -
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Adv Sci (Weinh)
Cancer Immunotherapy via Disruption of Integrin αvβ3 and CD47 Costabilization on Cancer Cell Surface. [Abstract]2025 Oct 30:e01602. PMID: 41168993
CWHM-12 purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Oct 30:e01602. [Abstract]
Representative images from live cell microscopy phagocytosis assays of Protonex Red+ MDA‐MB‐231 cells treated with the integrin αv inhibitor CWHM‐12 (4 µM).
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Cells
Wnt5A and TGFβ1 Converges through YAP1 Activity and Integrin Alpha v Up-Regulation Promoting Epithelial to Mesenchymal Transition in Ovarian Cancer Cells and Mesothelial Cell Activation. [Abstract]2022 Jan 11;11(2):237. PMID: 35053353
CWHM-12 purchased from MedChemExpress. Usage Cited in: Cells. 2022 Jan 11;11(2):237. [Abstract]
The Wnt5A overexpressing OVCAR-3 (C3/OVCAR-3) and SKOV-3 clones (C9/SKOV-3) were treated with CWHM-12 (10 μM) for 24 h.Immunoblot of TGFβ1, pSmad2/3, YAP1 determined in MCAs OvCa cells.
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Glia
2023 Feb;71(2):245-258. PMID: 36106533 -
Sci Rep
Wnt5A modulates integrin expression in a receptor-dependent manner in ovarian cancer cells. [Abstract]2021 Mar 15;11(1):5885. PMID: 33723319 -
PLoS One
Odontogenesis-associated phosphoprotein (ODAPH) Promotes Ameloblast adhesion and alkaline phosphatase (ALP) expression via LAMC2/ ITGB6/TGF-β1 signaling pathway. [Abstract]2025 Jul 18;20(7):e0328263. PMID: 40680053 -
Lösungsmittel & Löslichkeit
DMSO : 100 mg/mL (169.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (3.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (3.52 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
Functions of integrins αvβ1, αvβ8, α2β1 and α10β1 are measured using cell-free receptor-ligand interaction assays using purified recombinant human integrins. Ligands used are human fibronectin for αvβ1, human LAP for αvβ8, bovine collagen II for α2β1, and murine laminin I for α10β1. 96-well plates are coated with the predetermined optimal concentration of ligand overnight, washed 3X with TBS+++ (25 mM Tris pH7.4, 137 mM NaCl, 2.7 mM KCl, 1 mM MgCl2, 1 mM MnCl2, 1mM CaCl2), and blocked with TBS+++/1%BSA. Purified integrin is diluted in TBS+++/0.1%BSA with or without compounds (e.g., CWHM-12), and the solution added to empty wells of the washed ligand-coated plate according to a standard template, with each sample repeated in triplicate. After incubation for 2 hr at room temperature, the plate is washed 3X with TBS+++. Biotin-labeled antibody against the αv subunit (αvβ1, αvβ8 assays) or β1 subunit (α2β1, α10β1 assays) is applied for 1 hr. The plate is washed 3X with TBS/0.1%BSA. Streptavidin-conjugated horseradish peroxidase is added to the wells, and the plate incubated for 20 min at room temperature. Following a 3X TBS+++ wash, bound integrin is detected using streptavidin-conjugated horseradish peroxidase and TMB substrate with absorbance measured at 650 nm. For assay of αIIbβ3 (IIbIIIa) function, plates are coated with the purified human integrin overnight, washed 3X with TBS+++, and blocked with TBS+++/1%BSA. Alexa Fluor647-labeled purified human fibrinogen is diluted in TBS+++/0.1%BSA with or without compounds, and the solutions are added to the integrin-coated plate. After 2 hr incubation, the plate is washed 3X with TBS+++, and bound ligand is detected by absorbance measured at 640/668nm. For all assays, concentration-response curves are constructed by non-linear regression analysis and IC50 values are calculated using GraphPad Prism software[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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. The same procedure is used to measure adhesion of αvβ6-expressing human HT-29 cells to purified human latency associated peptide, and α5β1-expressing human K562 cells to human plasma fibronectin. In all cell-based assays, binding by the expected integrin is verified by testing activity of corresponding isotype-matched positive (function-blocking) and negative control antibodies[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
The mTmG (Td tomato/EGFP) and Ai14 (Rosa-CAG-LSL-tdTomato-WPRE) mice are used and crossed with Pdgfrb-Cre mice. Wild type C57/BL6 mice, Itgavflox/flox mice and itgb8flox/flox mice are used. Mice used for all experiments are 8-12 weeks old and are housed under specific pathogen-free conditions. For all studies CWHM-12 and CWHM-96 are solubilized in 50% DMSO (in sterile water) and dosed to 100 mg/kg/day. Drug or vehicle (50% DMSO) are delivered by implantable ALZET osmotic minipumps. For CCl4-induced fibrosis, pumps are inserted subcutaneously either before the first dose of CCl4 (prophylactic) or after 3 weeks of treatment (therapeutic) and livers are harvested after 6 weeks. For Bleomycin-induced fibrosis pumps are inserted 14 days after treatment with Bleomycin or saline and lungs are harvested at 28 days (therapeutic only).
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Henderson NC, et al. Targeting of αv integrin identifies a core molecular pathway that regulates fibrosis in several organs. Nat Med. 2013 Dec;19(12):1617-24. [Content Brief]
[2]. Basta J, Robbins L, Stout L, Prinsen MJ, Griggs DW, Rauchman M. Pharmacologic inhibition of RGD-binding integrins ameliorates fibrosis and improves function following kidney injury. Physiol Rep. 2020;8(7):e14329. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.6936 mL | 8.4678 mL | 16.9357 mL | 42.3392 mL |
| 5 mM | 0.3387 mL | 1.6936 mL | 3.3871 mL | 8.4678 mL | |
| 10 mM | 0.1694 mL | 0.8468 mL | 1.6936 mL | 4.2339 mL | |
| 15 mM | 0.1129 mL | 0.5645 mL | 1.1290 mL | 2.8226 mL | |
| 20 mM | 0.0847 mL | 0.4234 mL | 0.8468 mL | 2.1170 mL | |
| 25 mM | 0.0677 mL | 0.3387 mL | 0.6774 mL | 1.6936 mL | |
| 30 mM | 0.0565 mL | 0.2823 mL | 0.5645 mL | 1.4113 mL | |
| 40 mM | 0.0423 mL | 0.2117 mL | 0.4234 mL | 1.0585 mL | |
| 50 mM | 0.0339 mL | 0.1694 mL | 0.3387 mL | 0.8468 mL | |
| 60 mM | 0.0282 mL | 0.1411 mL | 0.2823 mL | 0.7057 mL | |
| 80 mM | 0.0212 mL | 0.1058 mL | 0.2117 mL | 0.5292 mL | |
| 100 mM | 0.0169 mL | 0.0847 mL | 0.1694 mL | 0.4234 mL |
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