MK-0429
Based on 7 publication(s) in Google Scholar
MK-0429 (L-000845704) is an orally active, potent, selective and nonpeptide pan-integrin antagonist with IC50 values of 1.6 nM, 2.8 nM, 0.1 nM, 0.7 nM, 0.5 nM and 12.2 nM for αvβ1, αvβ3, αvβ5, αvβ6, αvβ8 and α5β1, respectively.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.50%
- CAS 番号: 227963-15-7
- 分子式: C23H29N5O4
- 分子量:439.51
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保管条件: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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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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MedChemExpress（MCE）の使用を引用している文献 MK-0429
More- Nat Immunol. 2023 Oct;24(10):1654-1670. [Abstract]
- Nat Commun. 2025 Apr 16;16(1):3629. [Abstract]
- Nat Commun. 2025 Apr 8;16(1):3322. [Abstract]
- Nat Commun. 2024 Nov 30;15(1):10422. [Abstract]
- J Clin Invest. 2022 Jul 1;132(13):e156994. [Abstract]
- Adv Biol (Weinh). 2026 Jun;10(6):e70133. [Abstract]
- Research Square Preprint. 2021 Dec.
Customer Validation & Images
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WB
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Cell Migration/Invasion Assay
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Flow Cytometry
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In Vivo Efficacy Study
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Cell Migration/Invasion Assay
生物活性
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αvβ1 1.6 nM (IC50, inhibition of fibronectin-binding ) |
αvβ3 2.8 nM (IC50, inhibition of vitronectin-binding) |
αvβ5 0.1 nM (IC50, inhibition of vitronectin-binding) |
αvβ6 0.7 nM (IC50, inhibition of LAP-binding) |
αvβ8 0.5 nM (IC50, inhibition of LAP-binding) |
α5β1 12.2 nM (IC50, inhibition of fibronectin-binding) |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
3 nM
Compound: 5; MK-0429
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Inhibition of human integrin alphavbeta3 expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen preincubated for 20 mins followed by phosphatase substrate addition and measured after 1 hr by spectrophotometry
Inhibition of human integrin alphavbeta3 expressed in HEK293 cells assessed as reduction in cell adhesion to fibrinogen preincubated for 20 mins followed by phosphatase substrate addition and measured after 1 hr by spectrophotometry
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[PMID: 31999923] |
| K562 | IC50 |
4.6 μM
Compound: MK-0429
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Antagonist activity at integrin alpha5beta1 in human K562 cells assessed as inhibition of cell adhesion
Antagonist activity at integrin alpha5beta1 in human K562 cells assessed as inhibition of cell adhesion
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[PMID: 22572578] |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B6D2F1 hybrid female mice[2]
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Dosage:100 or 300 mg/kg
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Administration:P.o., twice daily (b.i.d.), 2 weeks
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Result:MK-0429 at 100 and 300 mg/kg reduced the number of metastatic tumor colonies by 64 and 57%, respectively, and the high dose also reduced the tumor area by 60% as compared to the vehicle[2].
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 227963-15-7
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性状 Solid
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分子量 439.51
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分子式 C23H29N5O4
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Color White to off-white
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SMILES
O=C1N([C@H](C2=CC=C(OC)N=C2)CC(O)=O)CCN1CCCC3=NC4=C(C=C3)CCCN4
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別名
L-000845704
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Nat Immunol
Kunitz-type protease inhibitor TFPI2 remodels stemness and immunosuppressive tumor microenvironment in glioblastoma. [Abstract]2023 Oct;24(10):1654-1670. PMID: 37667051
MK-0429 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Oct;24(10):1654-1670. [Abstract]
MK-0429 (50 nM) decreased the protein expression of P-PLCγ1 and P-PKCζ in HMC3 microglia incubated with TFPI2 protein.
MK-0429 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Oct;24(10):1654-1670. [Abstract]
MK-0429 (1, 10, 25, 50 nM) decreased migration in HMC3, SIM-A9, and PrhMG incubated with TFPI2 protein.
MK-0429 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Oct;24(10):1654-1670. [Abstract]
MK-0429 (50 nM) reduced TFPI2-induced microglia immunosuppressive polarization as indicated by reduced expression of immunosuppressive markers CD206 and ARG1 in PrhMG cells.
MK-0429 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Oct;24(10):1654-1670. [Abstract]
MK-0429 (30 mg/kg; IP; every other day on day 7, and then received anti-PD1 treatment on days 11, 14 and 17) extend the survival of animal subjects bearing 005 GSC.
MK-0429 purchased from MedChemExpress. Usage Cited in: Nat Immunol. 2023 Oct;24(10):1654-1670. [Abstract]
MK-0429 (0, 1, 10, 20, 50 nM; 10 h) reduced the migration of PrhMG human HMC3 and mouse SIM-A9 microglia treated with TFPI2 protein (20 ng/mL).
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Nat Commun
An enzyme-proof glycan glue for extracellular matrix to ameliorate intervertebral disc degeneration. [Abstract]2025 Apr 16;16(1):3629. PMID: 40240357 -
Nat Commun
The integrin repertoire drives YAP-dependent epithelial:stromal interactions during injury of the kidney glomerulus. [Abstract]2025 Apr 8;16(1):3322. PMID: 40199893 -
Nat Commun
The dysadherin/MMP9 axis modifies the extracellular matrix to accelerate colorectal cancer progression. [Abstract]2024 Nov 30;15(1):10422. PMID: 39613801 -
J Clin Invest
Lymph node fibroblastic reticular cells preserve a tolerogenic niche in allograft transplantation through laminin α4. [Abstract]2022 Jul 1;132(13):e156994. PMID: 35775481 -
Adv Biol (Weinh)
2026 Jun;10(6):e70133. PMID: 42253270 -
溶剤 & 溶解度
DMSO : 100 mg/mL (227.53 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 2.78 mg/mL (6.33 mM; Need ultrasonic)
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
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 (4.73 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 (4.73 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.
For the following dissolution methods, please prepare the working solution directly:
It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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: PBS
Solubility: 7.14 mg/mL (16.25 mM); Clear solution; Need ultrasonic and warming and heat to 60°C
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.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (419 KB)
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取扱説明書 (2659 KB)
参考文献
[1]. Hutchinson JH, et al. Nonpeptide alphavbeta3 antagonists. 8. In vitro and in vivo evaluation of a potent alphavbeta3 antagonist for the prevention and treatment of osteoporosis. J Med Chem. 2003 Oct 23;46(22):4790-8. [Content Brief]
[2]. Pickarski M, et al. Orally active αvβ3 integrin inhibitor MK-0429 reduces melanoma metastasis. Oncol Rep. 2015 Jun;33(6):2737-45. [Content Brief]
[3]. Xiaoyan Zhou, et al. An integrin antagonist (MK-0429) decreases proteinuria and renal fibrosis in the ZSF1 rat diabetic nephropathy model. Pharmacol Res Perspect. 2017 Oct;5(5):e00354. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 2.2753 mL | 11.3763 mL | 22.7526 mL | 56.8815 mL |
| 5 mM | 0.4551 mL | 2.2753 mL | 4.5505 mL | 11.3763 mL | |
| DMSO | 10 mM | 0.2275 mL | 1.1376 mL | 2.2753 mL | 5.6882 mL |
| 15 mM | 0.1517 mL | 0.7584 mL | 1.5168 mL | 3.7921 mL | |
| 20 mM | 0.1138 mL | 0.5688 mL | 1.1376 mL | 2.8441 mL | |
| 25 mM | 0.0910 mL | 0.4551 mL | 0.9101 mL | 2.2753 mL | |
| 30 mM | 0.0758 mL | 0.3792 mL | 0.7584 mL | 1.8961 mL | |
| 40 mM | 0.0569 mL | 0.2844 mL | 0.5688 mL | 1.4220 mL | |
| 50 mM | 0.0455 mL | 0.2275 mL | 0.4551 mL | 1.1376 mL | |
| 60 mM | 0.0379 mL | 0.1896 mL | 0.3792 mL | 0.9480 mL | |
| 80 mM | 0.0284 mL | 0.1422 mL | 0.2844 mL | 0.7110 mL | |
| 100 mM | 0.0228 mL | 0.1138 mL | 0.2275 mL | 0.5688 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
MK-0429 関連分類
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