MM-102 TFA
(Synonyms: HMTase Inhibitor IX TFA) 目录号 : GC36632
An inhibitor of WDR5/MLL interactions
Cas No.:1883545-52-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
WD-repeat protein 5 (WDR5) is a scaffold protein commonly involved in the formation of nucleosome-modifying protein complexes with histones.1 It serves as a component of a mixed-lineage leukemia (MLL) methyltransferase complex that targets histone 3 at lysine 4 to upregulate transcription.2 MM-102 is a potent WDR5/MLL interaction inhibitor (IC50 = 2.4 nM).3 It has been shown to block MLL1 methyltransferase activity, reducing the expression of HoxA9 and Meis-1 genes, which are both critical MLL1 target genes in MLL1 fusion protein-mediated leukemogenesis.3 MM-102 can also inhibit cell growth and induce apoptosis in leukemia cells harboring MLL1 fusion proteins.3
1.Migliori, V., Mapelli, M., and Guccione, E.On WD40 proteins: Propelling our knowledge of transcriptional control?Epigenetics7(8)815-822(2012) 2.Guccione, E., Bassi, C., Casadio, F., et al.Methylation of histone H3R2 by PRMT6 and H3K4 by an MLL complex are mutually exclusiveNature449(7164)933-937(2007) 3.Karatas, H., Townsend, E.C., Cao, F., et al.High-affinity, small-molecule peptidomimetic inhibitors of MLL1/WDR5 protein-protein interactionJ. Am. Chem. Soc.135(2)669-682(2013)
| Cas No. | 1883545-52-5 | SDF | |
| 别名 | HMTase Inhibitor IX TFA | ||
| Canonical SMILES | O=C(C1(NC([C@@H](NC(C(NC(C(C)C)=O)(CC)CC)=O)CCCNC(N)=N)=O)CCCC1)NC(C2=CC=C(F)C=C2)C3=CC=C(F)C=C3.FC(F)(F)C(O)=O | ||
| 分子式 | C37H50F5N7O6 | 分子量 | 783.83 |
| 溶解度 | DMSO: ≥ 100 mg/mL (127.58 mM) | 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.2758 mL | 6.3789 mL | 12.7579 mL |
| 5 mM | 0.2552 mL | 1.2758 mL | 2.5516 mL |
| 10 mM | 0.1276 mL | 0.6379 mL | 1.2758 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。