AGX51 |
رقم الكتالوجGC38590
One-Click Copy Product Info
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AGX51 هو الأول من نوعه في فئته (مثبطات بروتينات ربط / تمايز الحمض النووي)يثبط AGX51 تفاعل Id1-E47 ، مما يؤدي إلى تدهور المعرفات بوساطة اليوبيكويتين ، وتوقف نمو الخلايا ، ويقلل من قابلية البقاءيثبط AGX51 خطوط خلايا TNBC مع IC50s بحوالي 25 ميكرومتريمكن استخدام AGX51 لأبحاث السرطان
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 330834-54-3
Sample solution is provided at 25 µL, 10mM.
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AGX51 is the first pan-Id (DNA binding/differentiation protein inhibitor) antagonist and degrader. It inhibits the interaction between Id1 and E47 protein, induces ubiquitin-mediated degradation of Ids protein, thereby inhibiting cell growth and reducing cell viability[1]. AGX51 can inhibit the formation of pathological ocular neovascularization and can also be used in cancer research[2, 3].
In vitro, AGX51 (0-60μM) treatment of breast cancer cell lines (4T1 and nine other cell lines) for 24-72h significantly inhibited cell growth and viability[4]. AGX51 (0-40μM) treatment of INA-6 BRE-luc cells reduced luciferase activity after BMP9 treatment, and this reduction was not dependent on cell death[5]. AGX51 (40μM) treatment of MDA-MB-231 cells for 72h significantly inhibited cell proliferation and significantly reduced Ki67 expression[6].
In vivo, AGX51 (15mg/kg) was intraperitoneally injected into mice bearing MDA-MB-231 cell xenografts for 12 days, significantly inhibiting tumor growth[6]. AGX51 (30mg/kg) was intraperitoneally injected into mice bearing low oscillatory shear stress (OSS)-mediated atherosclerosis for 4 weeks, significantly inhibiting the expression of ID1 protein, reducing foam cells, restoring intimal thickness, and inhibiting lipid and collagen fiber deposition caused by OSS[7].
References:
[1] Lighter D J. Characterization of the Inhibitor of Differentiation (ID) Family in Ovarian Cancer[D]. San Diego State University, 2023.
[2] Wojnarowicz P M, e Silva R L, Ohnaka M, et al. A small-molecule pan-id antagonist inhibits pathologic ocular neovascularization[J]. Cell reports, 2019, 29(1): 62-75. e7.
[3] Zhong G, Wang Y, Wang Q, et al. Discovery of novel ID2 antagonists from pharmacophore-based virtual screening as potential therapeutics for glioma[J]. Bioorganic & Medicinal Chemistry, 2021, 49: 116427.
[4] Wojnarowicz P M, Escolano M G, Huang Y H, et al. Anti-tumor effects of an ID antagonist with no observed acquired resistance[J]. NPJ Breast Cancer, 2021, 7(1): 58.
[5] Møen J. FKBP12 and regulation of ALK2-and ALK3-ligand activity in multiple myeloma cells[D]. NTNU, 2024.
[6] Toro C D, Real S M, Laurito S R, et al. Exploring ID4 as a Driver of Aggression and a Therapeutic Target in Triple-Negative Breast Cancer[J]. bioRxiv, 2025: 2025.02. 07.637072.
[7] Jun Q, Yang X, Wang B, et al. ID1 protein inhibitor depresses low-oscillating shear stress-mediated EndMT and atherosclerosis by Snail and Wnt/β-catenin signalling pathways[J]. 2024.
| Cell experiment [1]: | |
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Cell lines |
4T1 cells and nine other breast cancer cell lines representing the major breast cancer subtypes (ER+, HER2+, and TNBC) |
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Preparation Method |
Cells were treated with AGX51 (0, 5, 10, 20, 40, 60μM) and incubated for 24, 48, and 72h, each condition was done in triplicate. At each time point, 40µL of MTT reagent (5mg/mL) was added per well and the cells were incubated for 4h. |
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Reaction Conditions |
0, 5, 10, 20, 40, 60μM; 24, 48, 72h |
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Applications |
AGX51 treatment of cancer cell lines impairs cell growth and viability. |
| Animal experiment [2]: | |
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Animal models |
ApoE-/- mice |
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Preparation Method |
5 oscillating shear stress (OSS) ApoE-/- mice were intraperitoneally injected with the ID1 inhibitor AGX51 at a dose of 30mg/kg body weight for 4 weeks as the experimental group. The other 5 OSS ApoE-/- mice were intraperitoneally injected with the same amount of DMSO as the Ctrl group, and the mice were euthanized by excessive chloral hydrate. The samples were taken from the origin of the left common carotid artery at the aortic arch to the root of the bifurcation of the internal and external carotid arteries. After serial sectioning, oil red O, H&E Staining, Masson staining, immunohistochemistry, and immunofluorescence staining were performed. |
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Dosage form |
30mg/kg; 4 weeks; i.p. |
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Applications |
AGX51 (30mg/kg) can effectively inhibit the expression of ID1 protein. After AGX51 treatment, foam cells were significantly reduced and the degree of intimal thickening was restored. AGX51 can inhibit OSS-induced lipid deposition and collagen fiber deposition. |
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References: |
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| Cas No. | 330834-54-3 | SDF | |
| Canonical SMILES | CCC(N(CCC(C1=CC=C(OCO2)C2=C1)C3=CC=CC=C3OC)CC4=CC=CC=C4)=O | ||
| Formula | C27H29NO4 | M.Wt | 431.52 |
| الذوبان | DMSO: 250 mg/mL (579.35 mM); Ethanol: 100 mg/mL (231.74 mM); Water: < 0.1 mg/mL (insoluble) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3174 mL | 11.5869 mL | 23.1739 mL |
| 5 mM | 463.5 μL | 2.3174 mL | 4.6348 mL |
| 10 mM | 231.7 μL | 1.1587 mL | 2.3174 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: An oil
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)