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| 5mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
UNC1215 (UNC-1215) is a potent and selective antagonist of L3MBTL3, a member of the MBT (malignant brain tumor) family of methyllysine (Kme) reading domain, with potential antineoplastic activity. It inhibits L3MBTL3 with an IC50 of 40 nM and a Kd of 120 nM.
| ln Vitro |
UNC1215 binds L3MBTL3 with ad of 120 nM, competitively displacing mono- or dimethyllysine-containing peptides, and is greater than 50-fold more powerful toward L3MBTL3 than other members of the MBT family while also displaying selectivity over more than 200 other reader domains studied. X-ray crystallography discovered a unique 2:2 polyvalent form of interaction between UNC1215 and L3MBTL3. In cells, UNC1215 is nontoxic and directly binds L3MBTL3 via the Kme-binding pocket of the MBT domains. UNC1215 increases the cellular mobility of GFP-L3MBTL3 fusion proteins, and point mutations that affect the Kme-binding function of GFP-L3MBTL3 phenocopy the effects of UNC1215 on localization[1].
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| ln Vivo |
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| References | |||
| Additional Infomation |
[3-anilino-4-[oxo-[4-(1-pyrrolidinyl)-1-piperidinyl]methyl]phenyl]-[4-(1-pyrrolidinyl)-1-piperidinyl]methanone is a member of benzamides and a N-acylpiperidine.
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| Molecular Formula |
C32H43N5O2
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| Molecular Weight |
529.72
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| Exact Mass |
529.341
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| CAS # |
1415800-43-9
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| Related CAS # |
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| PubChem CID |
57339144
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
712.1±60.0 °C at 760 mmHg
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| Flash Point |
384.5±32.9 °C
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| Vapour Pressure |
0.0±2.3 mmHg at 25°C
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| Index of Refraction |
1.640
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| LogP |
3.37
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
39
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| Complexity |
803
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
PQOOIERVZAXHBP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H43N5O2/c38-31(36-20-12-27(13-21-36)34-16-4-5-17-34)25-10-11-29(30(24-25)33-26-8-2-1-3-9-26)32(39)37-22-14-28(15-23-37)35-18-6-7-19-35/h1-3,8-11,24,27-28,33H,4-7,12-23H2
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| Chemical Name |
(2-(phenylamino)-1,4-phenylene)bis((4-(pyrrolidin-1-yl)piperidin-1-yl)methanone)
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| Synonyms |
UNC-1215, UNC 1215, UNC1215
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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 |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.83 mg/mL (1.57 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 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 0.83 mg/mL (1.57 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 8.3 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: ≥ 0.83 mg/mL (1.57 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 | 1.8878 mL | 9.4389 mL | 18.8779 mL | |
| 5 mM | 0.3776 mL | 1.8878 mL | 3.7756 mL | |
| 10 mM | 0.1888 mL | 0.9439 mL | 1.8878 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.
UNC1215 is a potent antagonist of L3MBTL3.Nat Chem Biol.2013 Mar;9(3):184-91. |
X-ray crystal structure of the UNC1215-3MBT complex.Nat Chem Biol.2013 Mar;9(3):184-91. |
UNC1215 binds a small set of Kme reader proteins with lower affinity than L3MBTL3.Nat Chem Biol.2013 Mar;9(3):184-91. |
UNC1215 potently antagonizes 3MBT localization in cells.Nat Chem Biol.2013 Mar;9(3):184-91. |
UNC1215 binds and co-localizes with full length L3MBTL3 (a) UNC1215 conjugated to the cell-permeable merocyanine dye, mero-76, co-localizes with GFP-FLMBT in HEK293 cells (scale bar, 10 μm; green is GFP-FLMBT, red is merocyanine-UNC1215, and blue is Hoechst dye). (b) FLMBT binds to biotin-UNC1215 (5 nmol).Nat Chem Biol.2013 Mar;9(3):184-91. |
Identification of BCLAF1 as a novel L3MBTL3 protein interactor (a) In U2OS cells, 3MBT colocalizes with BCLAF1 (top panel; green is GFP-3MBT, red is BCLAF, and blue is DAP1). Upon treatment with UNC1215, the 3MBT and BCLAF1 nuclear foci are noticeably disrupted (bottom panel). (b) Immunoprecipitation experiments in cells transfected with flag-3MBT or flag-FLMBT show that UNC1215 disrupts the interaction between 3MBT and BCLAF1 and also reduces the interaction between FLMBT and BCLAF1.Nat Chem Biol.2013 Mar;9(3):184-91. |
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