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| Targets |
The primary target of p32 Inhibitor M36 is the p32 mitochondrial protein (also known as C1QBP), a multifunctional protein that plays a role in mitochondrial function, tumor progression, and protein-protein interactions. By binding directly to p32, M36 blocks its association with LyP-1, a tumor-homing peptide. This disruption affects tumor cell adhesion, migration, and signaling pathways involved in cancer development.
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| ln Vitro |
M36, a p32 inhibitor, has an IC50 of 77.9 μM in full medium, which is more efficient at inhibiting the growth of SF188 glioma cells when glucose levels are low (IC50 of 7.3 μM) [1]. M36, a p32 inhibitor, is specific to cells that overexpress p32 [1]. With an IC50 of 2.8 μM, p32 Inhibitor M36 is another strong neurosphere inhibitor developed from patients [1].
In vitro, p32 Inhibitor M36 is selective for p32-overexpressing cells. It inhibits SF188 glioma cell proliferation with an IC50 of 77.9 µM in complete media and is much more potent under low glucose conditions (IC50 of 7.3 µM). It is also a potent inhibitor of patient-derived neurospheres with an IC50 of 2.8 µM. The compound demonstrates specificity for cells that overexpress p32, making it a valuable tool for studying p32-dependent cancer cell metabolism and proliferation. |
| ln Vivo |
No detailed in vivo activity data is publicly available for p32 Inhibitor M36. As a mitochondrial protein inhibitor targeting p32, it may have potential for in vivo studies in oncology, particularly for tumors that overexpress p32. However, specific animal model studies have not been reported in the available literature. The compound is primarily used as a research tool for in vitro studies of p32 function and cancer cell biology.
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| Enzyme Assay |
No specific cell-free enzyme/receptor binding assay protocol is detailed for p32 Inhibitor M36. The primary mechanism involves direct protein-protein interaction inhibition: p32 Inhibitor M36 binds directly to purified p32 protein and inhibits its association with LyP-1. Binding affinity can be assessed using surface plasmon resonance (SPR), isothermal titration calorimetry (ITC), or fluorescence polarization-based competition assays with labeled LyP-1 peptide.
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| Cell Assay |
Cellular activity is assessed in p32-overexpressing cancer cell lines such as SF188 glioma cells and patient-derived neurospheres. Cells are cultured in complete media or low-glucose conditions, treated with serial dilutions of p32 Inhibitor M36, and cell proliferation is measured using standard viability assays (e.g., MTT, CellTiter-Glo). IC50 values are calculated from dose-response curves under different glucose conditions. Selectivity for p32-overexpressing cells can be confirmed by comparing efficacy in p32-high versus p32-low cell lines.
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| Animal Protocol |
No in vivo animal experimental protocol is publicly available for p32 Inhibitor M36. For similar mitochondrial protein inhibitors, typical in vivo studies involve intravenous or intraperitoneal administration in murine xenograft models of p32-overexpressing tumors, with endpoints including tumor volume measurement, survival analysis, and biomarker assessment.
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| ADME/Pharmacokinetics |
Molecular weight: 448.52 g/mol; molecular formula: C23H28N8O2. Purity: ≥98%. CAS No.: 802555-85-7. Appearance: white to off-white solid powder. LogP: -0.1. SMILES: O=C(NCCCNC(=O)Nc1cccc(c1)C1=NCCN1)Nc1cccc(c1)C1=NCCN1. Solubility: DMSO (5 mg/mL, 11.15 mM) with sonication and heating to 80°C recommended. Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year. Density: 1.39 g/cm³ (predicted).
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| Toxicity/Toxicokinetics |
No toxicity data is publicly available. As a research chemical probe targeting mitochondrial proteins, standard toxicological profiling (cytotoxicity in multiple cell lines, hERG assay, Ames test) would be required for further development. The compound is for research use only and not for human use.
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| References | |
| Additional Infomation |
p32 Inhibitor M36 is a research-grade compound, not approved for therapeutic use. It is primarily used as a pharmacological tool for studying p32 mitochondrial protein function, tumor cell metabolism, and cancer biology. No clinical trials or FDA approval have been reported. The compound is of interest in oncology research for exploring therapeutic targeting of tumor-specific markers and tumor microenvironment interactions. Its mechanism involves direct binding to p32 and inhibition of p32-LyP-1 association.
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| Molecular Formula |
C23H28N8O2
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| Molecular Weight |
448.520823478699
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| Exact Mass |
448.233
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| CAS # |
802555-85-7
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| PubChem CID |
416381
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| Appearance |
White to off-white solid powder
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| LogP |
-0.1
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
33
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| Complexity |
680
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(NCCCNC(NC1C=C(C2NCCN=2)C=CC=1)=O)NC1C=C(C2NCCN=2)C=CC=1
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| InChi Key |
HHFOXYBNULCICF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H28N8O2/c32-22(30-18-6-1-4-16(14-18)20-24-10-11-25-20)28-8-3-9-29-23(33)31-19-7-2-5-17(15-19)21-26-12-13-27-21/h1-2,4-7,14-15H,3,8-13H2,(H,24,25)(H,26,27)(H2,28,30,32)(H2,29,31,33)
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| Chemical Name |
1-[3-(4,5-dihydro-1H-imidazol-2-yl)phenyl]-3-[3-[[3-(4,5-dihydro-1H-imidazol-2-yl)phenyl]carbamoylamino]propyl]urea
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~5 mg/mL (~11.15 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 1.82 mg/mL (4.06 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 18.2 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.82 mg/mL (4.06 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 18.2 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2296 mL | 11.1478 mL | 22.2955 mL | |
| 5 mM | 0.4459 mL | 2.2296 mL | 4.4591 mL | |
| 10 mM | 0.2230 mL | 1.1148 mL | 2.2296 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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