| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg | |||
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| Targets |
UNC2170 targets 53BP1 (p53-binding protein 1), a methyl-lysine (Kme) binding protein that plays a critical role in the DNA damage response. 53BP1 binds to methylated histones at sites of DNA double-strand breaks and promotes non-homologous end joining (NHEJ) repair. By binding to 53BP1, UNC2170 acts as a ligand that modulates its function. The compound's selectivity for 53BP1 over other methyl-lysine reader proteins (at least 17-fold) makes it a valuable tool for studying the specific role of 53BP1 in DNA repair and genome stability.
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| ln Vitro |
When compared to hybrids that were left untreated or treated with UNC2892 (a negative control compound), hybrids treated with UNC-2170 (500 μM) showed a notable increase in soluble 53BP1. 53BP1 mutant B cells respond less favorably to UNC-2170 (30-100 μM; naïve splenocytes grown with LPS and IL-4 for 3.5 days) [1].
In vitro, UNC2170 is a functionally active fragment ligand of 53BP1 with an IC50 of 29 µM and a Kd of 22 µM. The compound demonstrates at least 17-fold selectivity for 53BP1 compared with nine other methyl-lysine reader proteins. Its binding affinity and selectivity have been characterized using biophysical and biochemical assays. The compound's ability to bind to 53BP1 and modulate its function has been demonstrated in vitro. |
| ln Vivo |
In vivo, UNC2170 has potential applications in studying the role of 53BP1 in the DNA damage response and genome stability. However, detailed in vivo efficacy data are limited. The compound is primarily used as a research tool for in vitro studies.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for UNC2170 involve measuring its binding affinity to 53BP1 using biophysical techniques such as surface plasmon resonance (SPR) or isothermal titration calorimetry (ITC). Competitive binding assays using fluorescently labeled methyl-lysine peptides are also performed to determine IC50 values. Selectivity profiling against a panel of methyl-lysine reader proteins is performed to confirm specificity.
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| Cell Assay |
In vitro cell-based experiments for UNC2170 are conducted using cells with defined DNA damage responses. Cells are treated with UNC2170, and the compound's effects on 53BP1 localization to DNA damage sites (e.g., ionizing radiation-induced foci) are assessed by immunofluorescence microscopy. DNA repair efficiency is measured using assays such as the γH2AX foci formation assay or reporter-based NHEJ assays.
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| Animal Protocol |
In vivo animal experiments for UNC2170 are performed in mouse models of DNA damage and genome instability. The compound is administered, and its effects on 53BP1 function, DNA repair, and tumorigenesis are assessed. However, detailed in vivo efficacy data are limited.
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| ADME/Pharmacokinetics |
UNC2170 Maleate is a small molecule (MW 313.23, free base) with suitable physicochemical properties for research use. The compound is supplied as the maleate salt. Detailed pharmacokinetic parameters are limited in available literature.
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| Toxicity/Toxicokinetics |
Preclinical toxicology data for UNC2170 are limited. The compound is supplied for laboratory research use only. As a modulator of 53BP1 function, potential effects on DNA repair and genome stability should be considered.
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| References |
[1]. Perfetti MT, et al. Identification of a fragment-like small molecule ligand for the methyl-lysine binding protein, 53BP1. ACS Chem Biol. 2015;10(4):1072-1081.
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| Additional Infomation |
UNC2170 Maleate is also known as UNC-2170. It is a research compound used primarily for studying the role of 53BP1 in the DNA damage response and for exploring the therapeutic potential of targeting 53BP1 in cancer. Its selectivity for 53BP1 over other methyl-lysine reader proteins makes it a valuable tool for dissecting the specific functions of 53BP1 in DNA repair and genome stability. The compound is not approved for clinical use.
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| Molecular Formula |
C18H25BRN2O5
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|---|---|
| Molecular Weight |
429.31
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| Exact Mass |
312.083
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| CAS # |
1648707-58-7
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| Appearance |
Colorless to light yellow viscous liquid
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
419.6±30.0 °C at 760 mmHg
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| Flash Point |
207.6±24.6 °C
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| Vapour Pressure |
0.0±1.0 mmHg at 25°C
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| Index of Refraction |
1.534
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| LogP |
2.99
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| SMILES |
BrC1=CC=CC(=C1)C(NCCCNC(C)(C)C)=O
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| Synonyms |
UNC 2170 Maleate; UNC-2170 Maleate; UNC2170 Maleate
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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 Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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) |
MEthanol : ~125 mg/mL (~399.07 mM)
DMSO : ~100 mg/mL (~319.25 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.98 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% 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 25.0 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: ≥ 2.5 mg/mL (7.98 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 25.0 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. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (7.98 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3293 mL | 11.6466 mL | 23.2932 mL | |
| 5 mM | 0.4659 mL | 2.3293 mL | 4.6586 mL | |
| 10 mM | 0.2329 mL | 1.1647 mL | 2.3293 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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