UNC1215
(Synonyms: UNC 1215;UNC-1215) 目录号 : GC16794
Potent L3MBTL3 domain inhibitor
Cas No.:1415800-43-9
Sample solution is provided at 25 µL, 10mM.
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UNC1215 is a selective inhibitor of L3MBTL3 with IC50 value of 40 nM [1].
L3MBTL3 is a member of the MBT (malignant brain tumor) family of methyl-lysine reader proteins and is reported to play an important role in haematopoiesis and cancer biology. And it is reported that inhibition of L3MBTL3 can be regarded as a promising target used in clinic [2].
UNC1215 is a potent L3MBTL3 inhibitor and has a more potent inhibitory ability than other MBT family members. When tested with HEK293 cells transfected with a GFP fusion protein of the 3 MBT domains of L3MBTL3, UNC1215 treatment decreased the recovery time in a dose responsive manner via binding and co-localizing L3MBTL3 [1]. Using AlphaScreen○R methylated histone peptide competition assay, UNC1215 showed high antagonism ability to L3MBTL3 with IC50 value of 24±7.6 nM [3]. As the first potent and selective inhibitor for methyl-lysine reader protein-L3MBTL3-UNC1215 showed highly selective inhibitor ability via antagonizing the mono- and dimethyl-lysine reading function of L3MBTL3 [2].
References:
1. James, L.I., et al., Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain. Nat Chem Biol, 2013. 9(3): p. 184-91.
2. James, L.I., et al., Small-molecule ligands of methyl-lysine binding proteins: optimization of selectivity for L3MBTL3. J Med Chem, 2013. 56(18): p. 7358-71.
3. Camerino, M.A., et al., The structure-activity relationships of L3MBTL3 inhibitors: flexibility of the dimer interface. Medchemcomm, 2013. 4(11): p. 1501-1507.
| Cell experiment [1]: | |
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Cell lines |
Human embryonic kidney 293 cells transfected with a GFP fusion protein of the three MBT domains of L3MBTL3 (GFP-3MBT) |
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Preparation method |
The solubility of this compound in DMSO is >26.05 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
EC50: 50–100 nM |
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Applications |
Treatment with UNC1215 decreased the recovery time fluorescence intensity following photobleaching in a dose-responsive manner, with the EC50 of 50–100 nM, indicating that UNC1215 promoted diffusibility of GFP-3MBT within the nucleus. UNC1215 competed with cellular factors for binding of the MBT domains at concentrations well below 1 μM. UNC1215 showed potent effects on the subnuclear localization of GFP-3MBT, with an IC50 of approximately 500 nM for disruption of foci formation. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. James L I, Barsyte-Lovejoy D, Zhong N, et al. Discovery of a chemical probe for the L3MBTL3 methyllysine reader domain[J]. Nature chemical biology, 2013, 9(3): 184-191. | |
| Cas No. | 1415800-43-9 | SDF | |
| 别名 | UNC 1215;UNC-1215 | ||
| 化学名 | [3-anilino-4-(4-pyrrolidin-1-ylpiperidine-1-carbonyl)phenyl]-(4-pyrrolidin-1-ylpiperidin-1-yl)methanone | ||
| Canonical SMILES | C1CCN(C1)C2CCN(CC2)C(=O)C3=CC(=C(C=C3)C(=O)N4CCC(CC4)N5CCCC5)NC6=CC=CC=C6 | ||
| 分子式 | C32H43N5O2 | 分子量 | 529.72 |
| 溶解度 | ≥ 26.05 mg/mL in DMSO, ≥ 4.94 mg/mL in EtOH with ultrasonic and warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet